AU2023263496A1

AU2023263496A1 - Nucleoside phosphoramidate prodrugs

Info

Publication number: AU2023263496A1
Application number: AU2023263496A
Authority: AU
Inventors: Nagarathnam Dhanapalan; Du Jinfa; Joseph Sofia Michael; Wang Peiyuan
Original assignee: Gilead Pharmasset LLC
Current assignee: Gilead Pharmasset LLC
Priority date: 2007-03-30
Filing date: 2023-11-09
Publication date: 2023-11-30
Also published as: AU2012241173B2; AU2012241173A1

Abstract

Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following 5 structure: R2 0 R3b Base R3aN P- 0 0 C0 2R 4 ORR6 Y X Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I. 10

Description

NUCLEOSIDE PHOSPHORAMIDATE PRODRUGS

This application was filed on March 25, 2008, as a PCT International Patent

application in the name of Pharmasset, Inc., a U.S. national corporation, applicant for the

designation of all countries except the US, and Michael Joseph Sofia, a citizen of the U.S.;

Jinfa Du, a citizen of the U.S.; Peiyuan Wang, a citizen of the People's Republic of China;

and Dhanapalan Nagarathnam, a citizen of the U.S.; applicants for the designation of the US

only, this application is a divisional application of Australian Patent Application No.

2021202327, which in turn is a divisional application of Australian Patent Application No.

2017261454, which in turn is a divisional application of Australian Patent Application No.

2016213882, which in turn is a divisional application of Australian Patent Application No.

2014215983, which in turn is a divisional application of Australian Patent Application No.

2012241173, which in turn is a divisional application of Australian Patent Application No.

2008232827, and claims priority to U.S. Provisional Application Nos. 60/909,315, filed

March 30, 2007; 60/982,309, filed October 24, 2007; and U.S. Non-Provisional Application

No. 12/053,015, filed March 21, 2008. The contents of each of the above-noted applications

is hereby incorporated by reference in its entirety.

Field of Invention

The present invention pertains to nucleoside phosphoramidates and their use as agents for

treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral

replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV

replication and for treatment of hepatitis C infection in mammals. The invention provides

novel chemical compounds, and the use of these compounds alone or in combination with

other antiviral agents for treating HCV infection.

Background

Hepatitis C virus (HCV) infection is a major health problem that leads to chronic liver

disease, such as cirrhosis and hepatocellular carcinoma, in a substantial number of infected

individuals, estimated to be 2- 15 % of the world's population. There are an estimated 4.5

million infected people in the United States alone, according to the U.S. Center for Disease

Control. According to the World Health Organization, there are more than 200 million

infected individuals worldwide, with at least 3 to 4 million people being infected each year.

Once infected, about 20% of people clear the virus, but the rest can harbor HCV the rest of

their lives. Ten to twenty percent of chronically infected individuals eventually develop

liver-destroying cirrhosis or cancer. The viral disease is transmitted parenterally by

contaminated blood and blood products, contaminated needles, or sexually and vertically

from infected mothers or carrier mothers to their offspring. Current treatments for HCV

infection, which are restricted to immunotherapy with recombinant interferon-a alone or in

combination with the nucleoside analog ribavirin, are of limited clinical benefit. Moreover,

there is no established vaccine for HCV. Consequently, there is an urgent need for

improved therapeutic agents that effectively combat chronic HCV infection.

The HCV virion is an enveloped positive-strand RNA virus with a single

oligoribonucleotide genomic sequence of about 9600 bases which encodes a polyprotein of

about 3,010 amino acids. The protein products of the HCV gene consist of the structural

proteins C, El, and E2, and the non-structural proteins NS2, NS3, NS4A and NS4B, and

NS5A and NS5B. The nonstructural (NS) proteins are believed to provide the catalytic

machinery for viral replication. The NS3 protease releases NS5B, the RNA-dependent RNA

polymerase from the polyprotein chain. HCV NS5B polymerase is required for the

synthesis of a double-stranded RNA from a single-stranded viral RNA that serves as a

template in the replication cycle of HCV. Therefore, NS5B polymerase is considered to be

an essential component in the HCV replication complex (K. Ishi, et al, Heptology, 1999, 29:

1227-1235; V. Lohmann, et al., Virology, 1998, 249: 108-118). Inhibition of HCV NS5B polymerase prevents formation of the double-stranded HCV RNA and therefore constitutes an attractive approach to the development of HCV-specific antiviral therapies.

HCV belongs to a much larger family of viruses that share many common features.

FlaviviridaeViruses

The Flaviviridae family of viruses comprises at least three distinct genera: pestiviruses,

which cause disease in cattle and pigs;flavivruses, which are the primary cause of diseases

such as dengue fever and yellow fever; and hepaciviruses, whose sole member is HCV. The

flavivirus genus includes more than 68 members separated into groups on the basis of

serological relatedness (Calisher et al., J Gen. Virol, 1993,70,37-43). Clinical symptoms

vary and include fever, encephalitis and hemorrhagic fever (Fields Virology, Editors: Fields,

B. N., Knipe, D. M., and Howley, P. M., Lippincott-Raven Publishers, Philadelphia, PA,

1996, Chapter 31, 931-959). Flaviviruses of global concern that are associated with human

disease include the Dengue Hemorrhagic Fever viruses (DHF), yellow fever virus, shock

syndrome and Japanese encephalitis virus (Halstead, S. B., Rev. Infect. Dis., 1984, 6, 251

264; Halstead, S. B., Science, 239:476-481, 1988; Monath, T. P., New Eng. J. Med, 1988,

319, 64 1-643).

The pestivirus genus includes bovine viral diarrhea virus (BVDV), classical swine fever

virus (CSFV, also called hog cholera virus) and border disease virus (BDV) of sheep

(Moennig, V. et al. Adv. Vir. Res. 1992, 41, 53-98). Pestivirus infections of domesticated

livestock (cattle, pigs and sheep) cause significant economic losses worldwide. BVDV

causes mucosal disease in cattle and is of significant economic importance to the livestock

industry (Meyers, G. and Thiel, H.J., Advances in Virus Research, 1996, 47, 53-118;

Moennig V., et al, Adv. Vir. Res. 1992, 41, 53-98). Human pestiviruses have not been as

extensively characterized as the animal pestiviruses. However, serological surveys indicate

considerable pestivirus exposure in humans.

Pestiviruses and hepaciviruses are closely related virus groups within the Flaviviridae

family. Other closely related viruses in this family include the GB virus A, GB virus A-like

agents, GB virus-B and GB virus-C (also called hepatitis G virus, HGV). The hepacivirus

group (hepatitis C virus; HCV) consists of a number of closely related but genotypically

distinguishable viruses that infect humans. There are at least 6 HCV genotypes and more

than 50 subtypes. Due to the similarities between pestiviruses and hepaciviruses, combined

with the poor ability of hepaciviruses to grow efficiently in cell culture, bovine viral diarrhea

virus (BVDV) is often used as a surrogate to study the HCV virus.

The genetic organization of pestiviruses and hepaciviruses is very similar. These positive

stranded RNA viruses possess a single large open reading frame (ORF) encoding all the

viral proteins necessary for virus replication. These proteins are expressed as a polyprotein

that is co- and post-translationally processed by both cellular and virus-encoded proteinases

to yield the mature viral proteins. The viral proteins responsible for the replication of the

viral genome RNA are located within approximately the carboxy-terminal. Two-thirds of

the ORF are termed nonstructural (NS) proteins. The genetic organization and polyprotein

processing of the nonstructural protein portion of the ORF for pestiviruses and hepaciviruses

is very similar. For both the pestiviruses and hepaciviruses, the mature nonstructural (NS)

proteins, in sequential order from the amino-terminus of the nonstructural protein coding

region to the carboxy-terminus of the ORF, consist of p7, NS2, NS3, NS4A, NS4B, NS5A,

and NS5B.

The NS proteins of pestiviruses and hepaciviruses share sequence domains that are

characteristic of specific protein functions. For example, the NS3 proteins of viruses in both

groups possess amino acid sequence motifs characteristic of serine proteinases and of

helicases (Gorbalenya et al., Nature, 1988, 333, 22; Bazan and Fletterick Virology,

1989,171,637-639; Gorbalenya et al., Nucleic Acid Res.,1989, 17, 3889-3897). Similarly, the

NS5B proteins of pestiviruses and hepaciviruses have the motifs characteristic of RNA- directed RNA polymerases (Koonin, E.V. and Dolja, V.V., Crir. Rev. Biochem. Molec. Biol.

1993, 28, 375-430).

The actual roles and functions of the NS proteins of pestiviruses and hepaciviruses in the

lifecycle of the viruses are directly analogous. In both cases, the NS3 serine proteinase is

responsible for all proteolytic processing of polyprotein precursors downstream of its

position in the ORF (Wiskerchen and Collett, Virology, 1991, 184, 341-350; Bartenschlager

et al., J Virol. 1993, 67, 3835-3844; Eckart et al. Biochem. Biophys. Res. Comm. 1993,192,

399-406; Grakoui et al., J Virol. 1993, 67, 2832-2843; Grakoui et al., Proc. Natl. Acad Sci.

USA 1993, 90, 10583-10587; Hijikata et al., J Virol. 1993, 67, 4665-4675; Tome et al., J

Virol., 1993, 67, 4017-4026). The NS4A protein, in both cases, acts as a cofactor with the

NS3 serine protease (Bartenschlager et al., J Virol. 1994, 68, 5045-5055; Failla et al., J

Virol. 1994, 68, 3753-3760; Xu et al., J Virol., 1997, 71:53 12-5322). The NS3 protein of

both viruses also functions as a helicase (Kim et al., Biochem. Biophys. Res. Comm., 1995,

215, 160-166; Jin and Peterson, Arch. Biochem. Biophys., 1995, 323, 47-53; Warrener and

Collett, J Virol. 1995, 69,1720-1726). Finally, the NS5B proteins of pestiviruses and

hepaciviruses have the predicted RNA-directed RNA polymerases activity (Behrens et al.,

EMBO, 1996, 15, 12-22; Lechmann et al., J Virol., 1997, 71, 8416-8428; Yuan et al.,

Biochem. Biophys. Res. Comm. 1997,232,231-235; Hagedom, PCT WO 97/12033; Zhong

et al, J Virol., 1998, 72, 9365-9369).

Currently, there are limited treatment options for individuals infected with hepatitis C virus.

The current approved therapeutic option is the use of immunotherapy with recombinant

interferon-a alone or in combination with the nucleoside analog ribavirin. This therapy is

limited in its clinical effectiveness and only 50% of treated patients respond to therapy.

Therefore, there is significant need for more effective and novel therapies to address the

unmet medical need posed by HCV infection.

A number of potential molecular targets for drug development of direct acting antivirals as anti -HCV therapeutics have now been identified including, but not limited to, the NS2-NS3 autoprotease, the N3 protease, the N3 helicase and the NS5B polymerase. The RNA dependent RNA polymerase is absolutely essential for replication of the single-stranded, positive sense, RNA genome and this enzyme has elicited significant interest among medicinal chemists.

Inhibitors of HCV NS5B as potential therapies for HCV infection have been reviewed: Tan,

S.-L., et al., Nature Rev. Drug Discov., 2002, 1, 867-881; Walker, M.P. et al., Exp. Opin.

InvestigationalDrugs, 2003, 12, 1269-1280; Ni, Z-J., et al., Current Opinion in Drug

Discovery and Development, 2004, 7, 446-459; Beaulieu, P. L., et al., Current Opinion in

InvestigationalDrugs, 2004, 5, 838-850; Wu, J., et al., CurrentDrug Targets-Infectious

Disorders,2003, 3, 207-219; Griffith, R.C., et al, Annual Reports in Medicinal Chemistry,

2004, 39, 223-237; Carrol, S., et al., Infectious Disorders-DrugTargets, 2006, 6, 17-29.

The potential for the emergence of resistant HCV strains and the need to identify agents with

broad genotype coverage supports the need for continuing efforts to identify novel and more

effective nucleosides as HCV NS5B inhibitors.

Nucleoside inhibitors of NS5B polymerase can act either as a non-natural substrate that

results in chain termination or as a competitive inhibitor which competes with nucleotide

binding to the polymerase. To function as a chain terminator the nucleoside analog must be

taken up by the cell and converted in vivo to a triphosphate to compete for the polymerase

nucleotide binding site. This conversion to the triphosphate is commonly mediated by

cellular kinases which imparts additional structural requirements on a potential nucleoside

polymerase inhibitor. Unfortunately, this limits the direct evaluation of nucleosides as

inhibitors of HCV replication to cell-based assays capable of in situ phosphorylation.

In some cases, the biological activity of a nucleoside is hampered by its poor substrate

characteristics for one or more of the kinases needed to convert it to the active triphosphate

form. Formation of the monophosphate by a nucleoside kinase is generally viewed as the rate limiting step of the three phosphorylation events. To circumvent the need for the initial phosphorylation step in the metabolism of a nucleoside to the active triphosphate analog, the preparation of stable phosphate prodrugs has been reported. Nucleoside phosphoramidate prodrugs have been shown to be precursors of the active nucleoside triphosphate and to inhibit viral replication when administered to viral infected whole cells (McGuigan, C., et al., J. Med. Chem., 1996, 39, 1748-1753; Valette, G., et al., J. Med. Chem., 1996, 39, 1981

1990; Balzarini, J., et al., Proc. NationalAcad Sci USA, 1996, 93, 7295-7299; Siddiqui, A.

Q., et al., J Med. Chem., 1999, 42, 4122-4128; Eisenberg, E. J., et al., Nucleosides,

Nucleotides and Nucleic Acids, 2001, 20, 1091-1098; Lee, W.A., et al., Antimicrobial

Agents and Chemotherapy, 2005, 49, 1898); US 2006/0241064; and WO 2007/095269.

Also limiting the utility of nucleosides as viable therapeutic agents is their sometimes poor

physicochemical and pharmacokinetic properties. These poor properties can limit the

intestinal absorption of an agent and limit uptake into the target tissue or cell. To improve

on their properties prodrugs of nucleosides have been employed. It has been demonstrated

that preparation of nucleoside phosphoramidates improves the systemic absorption of a

nucleoside and furthermore, the phosphoramidate moiety of these "pronucleotides" is

masked with neutral lipophilic groups to obtain a suitable partition coefficient to optimize

uptake and transport into the cell dramatically enhancing the intracellular concentration of

the nucleoside monophosphate analog relative to administering the parent nucleoside alone.

Enzyme-mediated hydrolysis of the phosphate ester moiety produces a nucleoside

monophosphate wherein the rate limiting initial phosphorylation is unnecessary.

SUMMARY OF THE INVENTION

The present invention is directed toward novel phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:

R2 0 R3b Bs R3a P 0 0 Base

C0 2 R4 OR 1 R5 R6

Y X

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least oneofC1-6alkyl,C2-6alkenyl,C2-6alkynyl,C1-6alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6haloalkyl, -N(Rl')2, C1-6acylamino, -NHSO2C1-6alkyl, -SO2N(R 1 ')2,COR1 ", and-SO2C-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to,C1-20 alkyl, Ci-io alkyl, orCI-6alkyl, R1"is -OR' or -N(Rl')2);

(b) R2 is hydrogen, C 1-10 alkyl, R3a or R3 band R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3aR3 bNHR, where n is 2 to 4 and R1, R3a, an d R3b;

(c) R3a and R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, C1-6hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and arylC1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl,C1-6 alkoxy, halogen, nitro and cyano; (ii) R3a and R3 both areC1-6alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms (v)R3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen orC1-6alkyl and R3 " is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3,CH2CH3,CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3,CH2CO2H, CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3, CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2,CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph),

CH2SH, or lower cycloalkyl and R3 is H, where R3 'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or N(R 3')2);

(d) R4 is hydrogen, CI-10 alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(e) R 5 is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., (CH2)pOH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R 5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, CI-4 alkyl, C24 alkenyl, C24 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(CI- 4 alkyl), OC(O)O(CI- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI- 4 alkyl), O(C 2-4 alkenyl), S(C- 4 acyl), S(CI- 4 alkyl), S(C 2 -4 alkynyl), S(C 2-4 alkenyl), SO(CI- 4 acyl), SO(C- 4 alkyl), SO(C 2-4 alkynyl), SO(C 2 4 alkenyl), S0 2 (C- 4 acyl), S0 2 (C- 4 alkyl), S 2 (C 2 - 4 alkynyl), S 2 (C 2 - 4

alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(C-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(C 1-4 acyl), O(C- 4 alkyl), O(C 2-4 alkenyl), S(C- 4 acyl), S(C- 4 alkyl), S(C 2- 4 alkynyl), S(C 2 4 alkenyl), SO(CI- 4 acyl), SO(C- 4 alkyl), SO(C 2-4 alkynyl), SO(C 2-4 alkenyl), S0 2 (C 1 -4 acyl), S0 2 (C1 -4 alkyl), S0 2(C 2 -4 alkynyl), S0 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl), OS(O) 2 (CI-4 alkyl), OS(O) 2 (C 2 -4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

the base is a naturally occurring or modified purine or pyrimidine base represented by the following structures:

_ o

R9 0 R10 0

R8 N R8 NH Z N NNH

R7 N O R7 N << N R N N NH2

a b c d

wherein

Z is N or CR 12 ;

R 7, R,R 9 , R 1 0, and R 1 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl of CI-C6, halogenated (F, Cl, Br, I) lower alkyl of C1-C6, lower alkenyl of C2 -C, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6, lower alkynyl of C2-C6 such as CaCH, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of C1-C6, halogenated (F, Cl, Br, I) lower alkoxyof C1-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R',

wherein R' is an optionally substituted alkyl , which includes, but is not limited to, an optionally substituted C1-2o alkyl, an optionally substituted Ci-io alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C2-C6, an optionally substituted lower alkenyl of C2-C6, or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C()(C- 2 alkyl), C(O)(Ci-io alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

R 12 is H, halogen (including F, Cl, Br, I), OH, OR', SH, SR', NH2, NHR', NR'2, N02 lower alkyl of C1-C6, halogenated (F, Cl, Br, I) lower alkylof C1-C6, lower alkenylof C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6 , lower alkynyl of C2-C6, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of CI-C6, halogenated (F, Cl, Br, I) lower alkoxy of C1-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that when base is represented by the structure c with R1 being hydrogen, R 12 is not a: (i) -C-C-H, (ii) -C=CH2, or (iii) -N02.

DEFINITIONS

1 _

The phrase "a" or "an" entity as used herein refers to one or more of that entity; for example, a compound refers to one or more compounds or at least one compound. As such, the terms "a" (or "an"), "one or more", and "at least one" can be used interchangeably herein.

The phrase "as defined herein above" refers to the first definition provided in the Summary of the Invention.

The terms "optional" or "optionally" as used herein means that a subsequently described event or circumstance may but need not occur, and that the description includes instances where the event or circumstance occurs and instances in which it does not. For example, "optional bond" means that the bond may or may not be present, and that the description includes single, double, or triple bonds.

The term "independently" is used herein to indicate that a variable is applied in any one instance without regard to the presence or absence of a variable having that same or a different definition within the same compound. Thus, in a compound in which R appears twice and is defined as "independently carbon or nitrogen", both R's can be carbon, both R's can be nitrogen, or one R' can be carbon and the other nitrogen.

The term "alkenyl" refers to an unsubstituted hydrocarbon chain radical having from 2 to 10 carbon atoms having one or two olefinic double bonds, preferably one olefinic double bond. The term "C2-N alkenyl" refers to an alkenyl comprising 2 to N carbon atoms, where N is an integer having the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term "C2-io alkenyl" refers to an alkenyl comprising 2 to 10 carbon atoms. The term "C2-4 alkenyl" refers to an alkenyl comprising 2 to 4 carbon atoms. Examples include, but are not limited to, vinyl, 1-propenyl, 2-propenyl (allyl) or 2-butenyl (crotyl).

The term "halogenated alkenyl" refers to an alkenyl comprising at least one of F, Cl, Br, and I.

The term "alkyl" refers to an unbranched or branched chain, saturated, monovalent hydrocarbon residue containing 1 to 30 carbon atoms. The term "Ci-M alkyl" refers to an alkyl comprising 1 to M carbon atoms, where M is an integer having the following values: 2,3,4,5,6,7, 8,9, 10, 11, 12,13, 14, 15, 16, 17,18, 19,20,21,22,23,24,25,26,27,28, 29, or 30. The term "CI-4 alkyl" refers to an alkyl containing 1 to 4 carbon atoms. The term "lower alkyl" denotes a straight or branched chain hydrocarbon residue comprising 1 to 6 carbon atoms. "C1-20 alkyl" as used herein refers to an alkyl comprising 1 to 20 carbon atoms. "Ci-io alkyl" as used herein refers to an alkyl comprising 1 to 10 carbons. Examples of alkyl groups include, but are not limited to, lower alkyl groups include methyl, ethyl,

1 1 _ propyl, i-propyl, n-butyl, i-butyl, t-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl. The term (ar)alkyl or (heteroaryl)alkyl indicate the alkyl group is optionally substituted by an aryl or a heteroaryl group respectively.

The term "cycloalkyl" refers to an unsubstituted or substituted carbocycle, in which the carbocycle contains 3 to 10 carbon atoms; preferably 3 to 8 carbon atoms; more preferably 3 to 6 carbon atoms (i.e., lower cycloalkyls). Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, 2-methyl-cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

The term "cycloalkyl alkyl" refers to an additionally unsubstituted or substituted alkyl substituted by a lower cycloalkyl. Examples of cycloalkyl alkyls include, but are not limited to, any one of methyl, ethyl, propyl, i-propyl, n-butyl, i-butyl, t-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl that is substituted with cyclopropyl, 2-methyl cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

The term "cycloheteroalkyl" refers to an unsubstituted or substituted heterocycle, in which the heterocycle contains 2 to 9 carbon atoms; preferably 2 to 7 carbon atoms; more preferably 2 to 5 carbon atoms. Examples of cycloheteroalkyls include, but are not limited to, aziridin-2-yl, N-Ci-3-alkyl-aziridin-2-yl, azetidinyl, N-C1-3-alkyl-azetidin-m'-yl, pyrrolidin-m'-yl, N-Ci-3-alkyl-pyrrolidin-m'-yl, piperidin-m'-yl, and N-C-3-alkyl-piperidin m'-yl, where m' is 2, 3, or 4 depending on the cycloheteroalkyl. Specific examples of N-Ci 3-alkyl-cycloheteroalkyls include, but are not limited to, N-methyl-aziridin-2-yl, N-methyl azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-2-yl, N-methyl-piperidin-3-yl, and N-methyl-piperidin-4-yl. In the instance of R4, the point of attachment between the cycloheteroalkyl ring carbon and the oxygen occurs at any one of m'

The term "heterocycle" refers to an unsubstituted or substituted heterocycle containing carbon, hydrogen, and at least one of N, 0, and S, where the C and N can be trivalent or tetravalent, i.e., sp2 - or sp 3-hybridized. Examples of heterocycles include, but are not limited to, aziridine, azetidine, pyrrolidine, piperidine, imidazole, oxazole, piperazine, etc. In the instance of piperazine, as related to R1 0 for NR'2, the corresponding opposite nitrogen atom of the piperazinyl is substituted by a lower alkyl represented by the following structure:

lovwralkyl-N N

Preferably, the opposite nitrogen of the piperazinyl is substituted by a methyl group.

_1 _

The term "halogenated alkyl" (or "haloalkyl") refers to an unbranched or branched chain alkyl comprising at least one of F, Cl, Br, and I. The term "Ci-M haloalkyl" refers to an alkyl comprising 1 to M carbon atoms that comprises at least one of F, Cl, Br, and I, where M is an integer having the following values: 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30. "C1-3 haloalkyl" refers to a haloalkyl comprising 1 to 3 carbons and at least one of F, Cl, Br, andI. The term "halogenated lower alkyl" (or "lower haloalkyl") refers to a haloalkyl comprising 1 to 6 carbon atoms and at least one of F, Cl, Br, and I. Examples include, but are not limited to, fluoromethyl, chloromethyl, bromomethyl, iodomethyl, difluoromethyl, dichloromethyl, dibromomethyl, diiodomethyl, trifluoromethyl, trichloromethyl, tribromomethyl, triiodomethyl, 1 fluoroethyl, 1-chloroethyl, 1-bromoethyl, 1-iodoethyl, 2-fluoroethyl, 2-chloroethyl, 2 bromoethyl, 2-iodoethyl, 2,2-difluoroethyl, 2,2-dichloroethyl, 2,2-dibromomethyl, 2-2 diiodomethyl, 3-fluoropropyl, 3-chloropropyl, 3-bromopropyl, 2,2,2-trifluoroethyl or 1,1,2,2,2-pentafluoroethyl.

The term "alkynyl" refers to an unbranched or branched hydrocarbon chain radical having from 2 to 10 carbon atoms, preferably 2 to 5 carbon atoms, and having one triple bond. The term "C2-N alkynyl" refers to an alkynyl comprising 2 to N carbon atoms, where N is an integer having the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term "C C2-4 alkynyl" refers to an alkynyl comprising 2 to 4 carbon atoms. The term "C2-io alkynyl" refers to an alkynyl comprising 2 to 10 carbons. Examples include, but are limited to, ethynyl, 1 propynyl, 2-propynyl, 1-butynyl, 2-butynyl or 3-butynyl.

The term "halogenated alkynyl" refers to an unbranched or branched hydrocarbon chain radical having from 2 to 10 carbon atoms, preferably 2 to 5 carbon atoms, and having one triple bond and at least one of F, Cl, Br, and I.

The term "cycloalkyl" refers to a saturated carbocyclic ring comprising 3 to 8 carbon atoms, i.e. cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl. The term "C3-7 cycloalkyl" as used herein refers to a cycloalkyl comprising 3 to 7 carbons in the carbocyclic ring.

The term "alkoxy" refers to an -0-alkyl group or an -0-cycloalkyl group, wherein alkyl and cycloalkyl are as defined above. Examples of -0-alkyl groups include, but are not limited to, methoxy, ethoxy, n-propyloxy, i-propyloxy, n-butyloxy, i-butyloxy, t-butyloxy. "Lower alkoxy" as used herein denotes an alkoxy group with a "lower alkyl" group as previously defined. "C1-10 alkoxy" refers to an-O-alkyl wherein alkyl is Ci-io. Examples of -0

_i l _ cycloalkyl groups include, but are not limited to, -O-c-propyl, -O-c-butyl, -O-c-pentyl, and O-c-hexyl.

The term "halogenated alkoxy" refers to an -0-alkyl group in which the alkyl group comprises at least one of F, Cl, Br, and I.

The term "halogenated lower alkoxy" refers to an -O-(lower alkyl) group in which the lower alkyl group comprises at least one of F, Cl, Br, and I.

The term "amino acid" includes naturally occurring and synthetic a, P y or 6 amino acids, and includes but is not limited to, amino acids found in proteins, i.e. glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine. In a preferred embodiment, the amino acid is in the L-configuration. Alternatively, the amino acid can be a derivative of alanyl, valinyl, leucinyl, isoleucinyl, prolinyl, phenylalaninyl, tryptophanyl, methioninyl, glycinyl, serinyl, threoninyl, cysteinyl, tyrosinyl, asparaginyl, glutaminyl, aspartoyl, glutaroyl, lysinyl, argininyl, histidinyl, p-alanyl, P valinyl, p-leucinyl, p-isoleucinyl, p-prolinyl, p-phenylalaninyl, p-tryptophanyl, p methioninyl, p-glycinyl, p-serinyl, p-threoninyl, p-cysteinyl, p-tyrosinyl, p-asparaginyl, p glutaminyl, p-aspartoyl, p-glutaroyl, p-lysinyl, p-argininyl or p-histidinyl. When the term amino acid is used, it is considered to be a specific and independent disclosure of each of the esters of a, P y or 6 glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine in the D and L-configurations.

The term "aminoacyl" includes N,N-unsubstituted, N,N-monosubstituted, and N,N disubstituted derivatives of naturally occurring and synthetic a, P y or 6 amino acyls, where the amino acyls are derived from amino acids. The amino-nitrogen can be substituted or unsubstituted. When the amino-nitrogen is substituted, the nitrogen is either mono- or di substituted, where the substituent bound to the amino-nitrogen is a lower alkyl or an alkaryl. In the instance of its use for Y, the expression "O(aminoacyl)" is used. It is understood that the C3' carbon of the ribose is bound to the oxygen "0",which is then bound to the carbonyl carbon of the aminoacyl.

The terms "alkylamino" or "arylamino" refer to an amino group that has one or two alkyl or aryl substituents, respectively.

The term "protected," as used herein and unless otherwise defined, refers to a group that is added to an oxygen, nitrogen, or phosphorus atom to prevent its further reaction or for other

_ 1A purposes. A wide variety of oxygen and nitrogen protecting groups are known to those skilled in the art of organic synthesis. Non-limiting examples include: C(O)-alkyl, C(O)Ph, C(O)aryl, CH3, CH2-alkyl, CH2-alkenyl, CH2Ph, CH2-aryl, CH20-alkyl, CH2O-aryl, S02 alkyl, S02-aryl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, and 1,3-(1,1,3,3 tetraisopropyldisiloxanylidene).

The term "aryl," as used herein, and unless otherwise specified, refers to substituted or unsubstituted phenyl (Ph), biphenyl, or naphthyl, preferably the term aryl refers to substituted or unsubstituted phenyl. The aryl group can be substituted with one or more moieties selected from among hydroxyl, F, Cl, Br,I, amino, alkylamino, arylamino, alkoxy, aryloxy, nitro, cyano, sulfonic acid, sulfate, phosphonic acid, phosphate, and phosphonate, either unprotected, or protected as necessary, as known to those skilled in the art, for example, as taught in T.W. Greene and P.G. M. Wuts, "Protective Groups in Organic Synthesis," 3rd ed., John Wiley & Sons, 1999.

The terms "alkaryl" or "alkylaryl" refer to an alkyl group with an aryl substituent, such as benzyl. The terms "aralkyl" or "arylalkyl" refer to an aryl group with an alkyl substituent.

The term "di(lower alkyl)amino-lower alkyl" refers to a lower alkyl substituted by an amino group that is itself substituted by two lower alkyl groups. Examples include, but are not limited to, (CH3)2NCH2, (CH3)2NCH2CH2, (CH3)2NCH2CH2CH2, etc. The examples above show lower alkyls substituted at the terminus carbon atom with an N,N-dimethyl-amino substituent. These are intended as examples only and are not intended to limit the meaning of the term "di(lower alkyl)amino-lower alkyl" so as to require the same. It is contemplated that the lower alkyl chain can be substituted with an N,N-di(lower alkyl)-amino at any point along the chain, e.g., CH3CH(N-(ower alkyl)2)CH2CH2.

The term "halo," as used herein, includes chloro, bromo, iodo and fluoro.

The term "acyl" refers to a substituent containing a carbonyl moiety and a non-carbonyl moiety. The carbonyl moiety contains a double-bond between the carbonyl carbon and a heteroatom, where the heteroatom is selected from among 0, N and S. When the heteroatom is N, the N is substituted by a lower alkyl. The non-carbonyl moiety is selected from straight, branched, and cyclic alkyl, which includes, but is not limited to, a straight, branched, or cyclic C1-2o alkyl, Ci-io alkyl, or lower alkyl; alkoxyalkyl, including methoxymethyl; aralkyl, including benzyl; aryloxyalkyl, such as phenoxymethyl; or aryl, including phenyl optionally substituted with halogen (F, Cl, Br, I), hydroxyl, Ci to C4 alkyl, or Ci to C4 alkoxy, sulfonate esters, such as alkyl or aralkyl sulphonyl, including

_1 r _ methanesulfonyl, the mono, di or triphosphate ester, trityl or monomethoxytrityl, substituted benzyl, trialkylsilyl (e.g. dimethyl-t-butylsilyl) or diphenylmethylsilyl. When at least one aryl group is present in the non-carbonyl moiety, it is preferred that the aryl group comprises a phenyl group.

The term "lower acyl" refers to an acyl group in which the non-carbonyl moiety is lower alkyl.

The term "purine" or "pyrimidine" base includes, but is not limited to, adenine, N alkylpurines, N-acylpurines (wherein acyl is C(O)(alkyl, aryl, alkylaryl, or arylalkyl), N benzylpurine, N6 -halopurine, N6 -vinylpurine, N 6 -acetylenic purine, N6 -acyl purine, N' hydroxyalkyl purine, N-allcylaminopurine, N-thioallcyl purine, N2 -alkylpurines, N2 -alkyl 6-thiopurines, thymine, cytosine, 5-fluorocytosine, 5-methylcytosine, 6-azapyrimidine, including 6-azacytosine, 2- and/or 4-mercaptopyrmidine, uracil, 5-halouracil, including 5 fluorouracil, C5 -alkylpyrimidines, C5 -benzylpyrimidines, C5 -halopyrimidines, C5 vinylpyrimidine, C5 -acetylenic pyrimidine, C5 -acyl pyrimidine, C5 -hydroxyalkyl purine, C5 amidopyrimidine, C5 -cyanopyrimidine, ,C 5 -iodopyrimidine, C-lodo-pyrimidine, C5 -Br vinyl pyrimidine, C6 -Br-vinyl pyrimidine, C5 -nitropyrimidine, C5 -amino-pyrimidine, N2 alkylpurines, N2 -alkyl-6-thiopurines, 5-azacytidinyl, 5-azauracilyl, triazolopyridinyl, imidazolopyridinyl, pyrrolopyrimidinyl, and pyrazolopyrimidinyl. Purine bases include, but are not limited to, guanine, adenine, hypoxanthine, 2,6-diaminopurine, and 6-chloropurine. Functional oxygen and nitrogen groups on the base can be protected as necessary or desired. Suitable protecting groups are well known to those skilled in the art, and include trimethylsilyl, dimethylhexylsilyl, t-butyldimethylsilyl, and t-butyldiphenylsilyl, trityl, alkyl groups, and acyl groups such as acetyl and propionyl, methanesulfonyl, and p toluenesulfonyl.

The term "tautomerism" and "tautomers" have their accepted plain meanings.

The term "P'" means that the phosphorous atom is chiral and that it has a corresponding Cahn-Ingold-Prelog designation of "R" or "S" which have their accepted plain meanings. It is contemplated that compounds of the formula I are racemic because the chirality at phosphorous. Applicants contemplate use of the racemate and/or the resolved enantiomers. In some instances, an asterisk does not appear next to the phosphoroamidate phosphorous atom. In these instances, it is understood that the phosphorous atom is chiral and that one of ordinary skill understands this to be so unless the substituents bound to the phosphorous exclude the possibility of chirality at phosphorous, such as in P(O)Cl 3 .

_1 r _

DETAILED DESCRIPTION OF THE INVENTION

An aspect of the invention is directed to a compound, its salts, hydrates, solvates, crystalline forms, and the like represented by formula I:

Base R3b 2

R3a N- - O

C0 2 R4 OR1 R R6

Y X

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one ofC1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, C1-6 acylamino, -NHSO2C1-6 alkyl, -SO2N(R"')2, COR", and -SO2C-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or C1-6 alkyl, Rl" is -OR'or -N(Rl')2);

(b) R2 is hydrogen, C 1-10 alkyl, R3a or R3 band R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3aR3 bNHR, where n is 2 to 4 an and R1, R3a, d R3b;

(c) R3a and R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, C1-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl C1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C1-6

alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are C1-6 alkyl; (iii) R 3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v)R 3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or C1-6 alkyl and R3 " is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3,

CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-2o alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or N(R 3')2);

(d) R4 is hydrogen, Ci-io alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(C-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(C 1-4 acyl), O(CI- 4 alkyl), O(C 2-4 alkenyl), S(C- 4 acyl), S(C- 4 alkyl), S(C -2 4 alkynyl), S(C 2 4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2-4 alkynyl), SO(C 2-4 alkenyl), S0 2 (C 1 -4 acyl), S0 2 (C1 -4 alkyl), S0 2(C 2 -4 alkynyl), S0 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl), OS(O) 2 (CI-4 alkyl), OS(O) 2 (C 2 -4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4

alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

12 _

R9 0 R10 0

R8 R8 NH NH

R 7 R N No N 0 N 7 O O N R N N NH2

a b c d

wherein

Z is N or CR 12 ;

As can be appreciated from the structure represented by formula I above, there are myriad ways to express the several embodiments and aspects of each embodiment of the present

10 _ invention. As seen below, the inventors have disclosed certain embodiments directed to the compound of formula I, each having several aspects, based on the identity of the modified purine or pyrimidine base. This is not intended to be an explicit or implicit admission that the three embodiments are independent or distinct nor should it be interpreted as such. Rather, it is intended to convey information so that the full breadth of the present invention can be understood. Furthermore, the following embodiments, and aspects thereof, are not meant to be limiting on the full breadth of the invention as recited by the structure of formula I.

A first embodiment of the invention is directed to a compound represented by formula I-1:

R9

R8

R7 N 0 R2 0 R 3b *

R3a N P 0 0

C0 2 R 4 OR 1 R6

Y X

I-1

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, CI-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, CI-6 acylamino, -NHSO2C1-6 alkyl, -SO2N(R"')2, COR", and -SO2CI-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or CI-6 alkyl, Rl" is -OR'or -N(Rl')2);

(b) R2 is hydrogen, C 1-10 alkyl, R3a or R3 band R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3 aR3 bNHR, where n is 2 to 4 and R1 , R3a, and R3b-

(c) R 3 and R 3 are (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, CI-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl CI-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C-6 alkoxy, halogen, nitro and cyano; (ii) R3 and R3b both are C-6 alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R 3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v)R 3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or C1-6 alkyl and R3 " is -OR' or -N(R 3 ')2); (vi) R3 a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or N(R 3')2);

(d) R4 is hydrogen, CI-10 alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)-amino, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, Cl, Br,I, NH2, or N3;

(h) Y is OH, H, Ci-4 alkyl, C24 alkenyl, C24 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(CI-4 alkyl), OC(O)O(CI-4 alkyl), OC(O)O(C2-4 alkynyl), OC(O)O(C2-4 alkenyl),

_ 1 _

OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI-4 alkyl), O(C2-4 alkenyl), S(CI-4 acyl), S(CI-4 alkyl), S(C2-4 alkynyl), S(C2-4 alkenyl), SO(CI-4 acyl), SO(C-4 alkyl), SO(C2-4

alkynyl), SO(C24 alkenyl), S02(CI-4 acyl), S02(C-4 alkyl), S2(C2-4 alkynyl), S2(C2-4 alkenyl), OS(O)2(CI-4 acyl), OS(O)2(C-4 alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(C-4 alkyl), NH(C24 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(C-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(C 1-4 acyl), O(CI- 4 alkyl), O(C 2-4 alkenyl), S(C- 4 acyl), S(C- 4 alkyl), S(C 2- 4 alkynyl), S(C 2 4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2-4 alkynyl), SO(C 2-4 alkenyl), S02(C1-4 acyl), S02(C1-4 alkyl), S02(C2-4 alkynyl), S0 2 (C 2-4 alkenyl), OS(O) 2 (CI- 4 acyl), OS(O)2(C-4 alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

(i) R 7, R,R 9 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenylof C2-C, CO2H, CO2R', CONH2, CONHR', CONR'2, wherein R'is a CI-2o alkyl; a C1-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

A first aspect of the first embodiment is directed to a compound represented by formula I-1

wherein

(a) R 1 is hydrogen, n-alkyl or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least oneof C1-6 alkyl, CI-6 alkoxy, F, Cl, Br, I, nitro, cyano, C-6 haloalkyl;

(b) R2 is hydrogen or CH3;

(c) R3 a and R3 bare independently (i) R3 is hydrogen and R3b and R2 together are (CH2) so as to form a cyclic ring that includes the adjoining N and C atoms (v)R3b is hydrogen and R 3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where cis I to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3' is independently hydrogen or C1-6 alkyl and R 3" is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2,

CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), or CH2SH and R3 is H;

(d) R4 is hydrogen, Ci-io alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, C-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(e) R 5 is H, CN, CH3, vinyl, OCH3, OCH2CH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I, with the provisos that when X is OH , base is cytosine and R6 is H, R 5 cannot be N3;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, Cl, Br,I, NH2, or N3;

(h) Y is OH, H, Ci-4 alkyl, vinyl, N3, CN, Cl, Br, F, I, O(C- 6 acyl), O(C- 4 alkyl), NH2, NH(C1-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(C-4 alkyl)2, N(C-18

acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, OC(O)O(C1- 4 alkyl), OC(O)O(C1- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-4 haloalkyl, O(aminoacyl), O(CI- 4 acyl), O(C- 4 alkyl), O(C 2 - 4 alkenyl), S(CI-4 acyl), S(CI- 4 alkyl), S(C 2 - 4 alkynyl), S(C 2 -4 alkenyl), SO(C- 4 acyl), SO(CI-4 alkyl), SO(C 2 -4 alkynyl), SO(C 2 -4 alkenyl), SO 2 (C- 4 acyl), SO 2 (C- 4 alkyl), SO 2 (C 2 - 4 alkynyl), SO 2 (C 2 -4 alkenyl), OS(O) 2 (C-4 acyl), OS(O) 2 (C-4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, or N(CI-4 acyl)2;

(i) R 7, R,R 9 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl, halogenated (F, Cl, Br,I) lower alkyl, lower alkenylof C2-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, wherein R'is a C1-20 alkyl; a C1-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

A second aspect of the first embodiment is directed to a compound represented by formula I 1

wherein

(a) R 1 is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a C1-3 alkyl, a C1-3 alkoxy, F, Cl, Br, I, nitro, cyano, and a C1-3 haloalkyl;

(b) R 2 is hydrogen or CH3;

(c) R3 a and R3 bare independently (i) R3 is hydrogen and R3b and R2 together are (CH2) so as to form a cyclic ring that includes the adjoining N and C atoms (v)R3b is hydrogen and R 3 and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where cis 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3' is independently hydrogen or CI-6 alkyl and R3" is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), or CH2SH and R3b is H;

(d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I, with the provisos that when X is OH , base is cytosine and R6 is H, R5 cannot be N3;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2, or O(aminoacyl);

(i) R7 and R8 are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; and

(j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(C1-20 alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(O)(C1-20 alkyl), which include but are not limited to NHC(O)(CH2)sCH3, and N(C(O)(CH2)sCH3)2, which include but is not limited to N(C(O)(CH2)sCH3)2, where s is an integer selected from 0,1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,and19.

A third aspect of the first embodiment is directed to a compound represented by formula I-1

wherein

(a) R' is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CH3-qX, where X is F, Cl, Br, or I, and q is 1-3;

(b) R2 is hydrogen or CH3;

(c) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H;

(d) R4 is hydrogen, CH3, Et, Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, NH2, or N3;

(i) R7 and R8 are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3,

CONH2, CONHCH3, or CON(CH3)2, wherein R' is a CI-2o alkyl; a C-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl'; and

A fourth aspect of the first embodiment is directed to a compound represented by formula I 2

R9

R8 ~N

R7 N 0 R2 0 3 R b

R3a N- P

4 C0 2R ORR

Y X

1-2

wherein

(a) R 1 is hydrogen, methyl, ethyl, n-propyl, i-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CH3-qX, where X is F, Cl, Br, or I, and q is 1-3;

(b) R2 is hydrogen or CH3;

(c) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3,

CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3' is H;

(d) R4 is hydrogen, CI-10 alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(e) R5 is H, CN, CH3, OCH3, CH2OH, CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I, with the provisos that when X is OH , base is cytosine and R' is H, R5 cannot be N3;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3;

(i) R7 and R8 are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R'is a CI-2o alkyl; a C-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl; and

(j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(C1-20 alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(O)(C1-20 alkyl), which include but are not limited to NHC(O)(CH2)sCH3, and and N(C(O)(CH2)sCH3, which include but is not limited to N(C(O)(CH2)sCH3)2, where s is an integer selected from 0,1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,and19.

A fifth aspect of the first embodiment is directed to a compound represented by formula 1-2

wherein

(a) R 1 is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p chloro-phenyl, p-fluorophenyl;

(b) R2 is hydrogen or CH3;

(c) R3aisHandR 3 is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl;

(e) R' is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, or O(aminoacyl);

(i) R 7 and R' are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R'is a C1-20 alkyl; a C1-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl; and

(j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(Ci-2 o alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(O)(CI-2 alkyl), which include but are not limited to NHC(O)(CH2)sCH3, and N(C(O)(CH2)sCH3)2, which include but is not limited to N(C(O)(CH2)sCH3)2, where s is an integer selected from 0,1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,and19.

A sixth aspect of the first embodiment is directed to a compound represented by formula1-2

wherein

(b) R2 is hydrogen or CH3;

(c) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl;

(d) R 4 is hydrogen, Ci-io alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(e) R' is H, OMe, CN, CH2F, F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, or N3;

(h) Y is H, OH, CH3, F, Cl, Br, I, or N3, OCH3, OC(O)CH3, or O(aminoacyl);

(i) R 7 and R' are independently H, F, Br, SCH3, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; and

(j) R9 is selected from among OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, OC(O)(CI- 2 o alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(O)(CI-2

alkyl), which include but are not limited to NHC(O)(CH2)sCH3, and N(C(O)(CH2)sCH3)2, which include but is not limited to N(C(O)(CH2)sCH3)2, where s is an integer selected from 0,1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,and19.

A seventh aspect of the first embodiment is directed to a compound represented by formula 1-2

wherein

(b) R2 is hydrogen;

(d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(e) R 5 is H;

_10

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, or N3;

(h) Y is OH, OCH3, OC(O)CH3, orO(aminoacyl);

(i) R7 and R' are independently H, F, Br, SCH3, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2; and

(j) R9 is selected from among OH, OCH3, NH2, NHCH3, N(CH3)2, OC(O)(CI-2o alkyl), which include but are not limited to OC(O)(CH2)sCH3, NHC(O)(CI-2o alkyl), which include but are not limited to NHC(O)(CH2)sCH3, and N(C(O)(CH2)sCH3)2, which include but is not limited to N(C(O)(CH2)sCH3)2, where s is an integer selected from among 0, 1, 2, 3, 4, 5, 6, 7,8,9,10,11,12,13,14,15,16,17,18,and19.

An eighth aspect of the first embodiment is directed to a compound represented by formula 1-2

wherein

(a) R 1 is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R2 is hydrogen;

(e) R' is H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, or N3;

(h) Y is OH, OCH3, OC(O)CH3, orO(aminoacyl);

(i) R7 and R' are independently H, F, Br, SCH3, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2;

A second embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula b above, wherein R, R2, R3 a, R3 , R4

, R', R6, X, Y, R7, and Rare defined in the Summary of the Invention section above.

A first aspect of the second embodiment is directed to a compound represented by formula I 3

0

R8 NH

R3b R2 R7 N R 0 N N - P 0 0 0 N R3a

C0 2R 4 OR 1 R6

Y X

1-3

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one ofC1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, C1-6 acylamino, -NHSO2C-6 alkyl, -SO2N(R"')2, COR", and -SO2C-6

alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or C1-6 alkyl, R" is -OR'or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3 a and R3 are (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, C1-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl C1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C-6 alkoxy, halogen, nitro and cyano; (ii) R3 and R3b both are C-6 alkyl; (iii) R3 and R 3 together are(CH2)fso as to form a spiro ring; (iv) R3 is hydrogen and R 3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v)R 3b is hydrogen and R 3 and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or CI-6 alkyl and R3 " is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3 b is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or N(R 3')2);

(e) R' is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., (CH2)pOH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R 5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, Cl, Br,I, NH2, or N3;

(h) Y is OH, H, CI-4 alkyl, C24 alkenyl, C24 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(C1-4 alkyl), OC(O)O(C1-4 alkyl), OC(O)O(C2-4 alkynyl), OC(O)O(C2-4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(C-4 alkyl), O(C2-4 alkenyl), S(C-4 acyl), S(C1-4 alkyl), S(C2-4 alkynyl), S(C2-4 alkenyl), SO(C1-4 acyl), SO(C-4 alkyl), SO(C2-4

alkynyl), SO(C24 alkenyl), S02(C1-4 acyl), S2(C-4 alkyl), S02(C2-4 alkynyl), S02(C2-4 alkenyl), OS(O)2(CI-4 acyl), OS(O)2(C-4 alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(C1-4 acyl), N(C1-4 alkyl)2, or N(Ci-18 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C- 4 alkyl), C(O)O(C- 4 alkyl), C(O)O(C 2 - 4 alkynyl), C(O)O(C 2 -4 alkenyl), O(CI-4 acyl), O(CI- 4 alkyl), O(C 2 -4 alkenyl), S(CI- 4 acyl), S(CI- 4 alkyl), S(C 2 -4 alkynyl), S(C 2 -4 alkenyl), SO(CI- 4 acyl), SO(CI- 4 alkyl), SO(C2-4 alkynyl), SO(C 2-4 alkenyl), S0 2 (C 1 -4 acyl), S0 2 (C- 4 alkyl), S0 2 (C 2- 4 alkynyl), S0 2 (C 2- 4 alkenyl), OS(O) 2 (C- 4 acyl), OS(O) 2 (C 1-4 alkyl), OS(O) 2 (C 2 -4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, or N(CI-4 acyl)2;

(i) R7 and R8 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenylof C2-C, CO2H, CO2R', CONH2, CONHR', CONR'2, wherein R'is a C1-20 alkyl; a C1-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

The second aspect of the second embodiment is directed to a compound represented by formula 1-3

wherein

(b) R2 is hydrogen or CH3;

(c) R3 a and R3 bare independently (i) R3 is hydrogen and R3b and R2 together are (CH2) so as to form a cyclic ring that includes the adjoining N and C atoms (v)R3b is hydrogen and R 3 and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where cis I to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3' is independently hydrogen or C1-6 alkyl and R 3" is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), or CH2SH and R3b is H;

(e) R' is H, CN, CH3, vinyl, OCH3, OCH2CH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, Ci-4 alkyl, vinyl, N3, CN, Cl, Br, F, I, O(C- 6 acyl), O(C- 4 alkyl), NH2, NH(C1-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(C-4 alkyl)2, N(C-18 acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, OC(O)O(C1- 4 alkyl), OC(O)O(C1- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(CI- 4 acyl), O(C- 4 alkyl), O(C 2 - 4 alkenyl), S(CI-4 acyl), S(CI- 4 alkyl), S(C 2 - 4 alkynyl), S(C 2 -4 alkenyl), SO(C- 4 acyl), SO(CI-4 alkyl), SO(C 2 -4 alkynyl), SO(C 2 -4 alkenyl), SO 2 (C 1 -4 acyl), SO 2 (C 1 -4 alkyl), SO 2 (C 2 -4

alkynyl), SO 2 (C 2 -4 alkenyl), OS(O) 2 (C-4 acyl), OS(O) 2 (C-4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2,

N(CI-4 acyl)2;

(i) R7 and R8 are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl, halogenated (F, Cl, Br,I) lower alkyl, lower alkenylof C2-C, CO2H, CO2R', CONH2, CONHR', CONR'2, wherein R'is a C1-20 alkyl; a C1-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

The third aspect of the second embodiment is directed to a compound represented by formula 1-3

wherein

(b) R2 is hydrogen, CH3, R3 a or R3' and R2 together are (CH2)3 so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3aR3 NHR, where n is 2 to 4 and R1 ,

R3 a, and R3 bare as defined herein;

(c) R3 a and R3' are independently (i) R3a is hydrogen and R3b and R2 together are (CH2) so as to form a cyclic ring that includes the adjoining N and C atoms (v)R3b is hydrogen and R 3 and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where cis I to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R3' is independently hydrogen or CI-6 alkyl and R3" is -OR' or -N(R 3')2); (vi) R3 is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, halogen, NH2, or N3

(h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3, NH2, NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3), N(CH3)2, N(C(O)CH3)2;

(i) R7 and R8 are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2.

The fourth aspect of the second embodiment is directed to a compound represented by formula 1-3

wherein

(b) R2 is hydrogen or CH3;

(d) R4 is hydrogen, CH3, Et, Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(e) R' is H, CN, CH3, OCH3, CH2OH, CH2(halo), such as CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, NH2, or N3;

(i) R7 and R8 are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R'is a CI-2o alkyl; a C-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

The fifth aspect of the second embodiment is directed to a compound represented by formula 1-4

R8 NH

R3b R2 0 R7 N 0 R3a N- - O

OR1 R5%6 C0 2R 4 R

Y X

1-4

wherein

(b) R2 is hydrogen or CH3;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, halogen, including F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3;

(i) R 7 and R' are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R'is a CI-2o alkyl; a C-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl,

The sixth aspect of the second embodiment is directed to a compound represented by formula 1-4

wherein

(b) R2 is hydrogen or CH3;

(c) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

The seventh aspect of the second embodiment is directed to a compound represented by formula 1-4 wherein

(a) R' is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p chloro-phenyl, p-fluorophenyl;

(b) R 2 is hydrogen or CH3;

(e) R 5 is H, OMe, CN, CH2F, F, Cl, Br, or I;

(f) R' is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(i) R7 and R8 are independently H, F, Br, SCH3, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2;

The eighth aspect of the second embodiment is directed to a compound represented by formula 1-4

wherein

(b) R2 is hydrogen;

(d) R4 is hydrogen, CH3, Et, Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl- pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(e) R 5 is H;

(f) R' is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(i) R7 and R8 are independently H, F, Br, SCH3, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2.

The ninth aspect of the second embodiment is directed to a compound represented by formula 1-4

wherein

(b) R2 is hydrogen;

(e) R 5 is H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, or N3;

(h) Y is OH, OCH3, or OC(O)CH3;

A third embodiment of the invention is directed to a compound represented by formula I in

-AOn which the base is a structure represented by formulac above, wherein R,R, R3 , R3 ,R4, R', R6, X, Y, Z, Ro, R1 1, and R 12 are defined in the Summary of the Invention section above; with the proviso that R1 1 is not H.

A first aspect of the third embodiment is directed to a compound represented by formula 1-5

R1a z

N R3b R2

R3a N 00 N - O O N C0 2R 4 OR R6 1

Y X

1-5

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one ofC1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, C1-6 acylamino, -NHSO2C1-6 alkyl, -SO2N(R"')2, COR", and -SO2C-6

alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or C1-6 alkyl, Rl" is -OR'or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3a and R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, C1-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl C1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C1-6 alkoxy, halogen, nitro and cyano; (ii) R3a and R3b both are C1-6 alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v)R 3b is hydrogen and R3a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or C1-6 alkyl and R3 " is -OR' or -N(R 3 ')2); (vi) R3a is H and R3b is from H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph,

A1 _

CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3a is CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3 b is H, where R3 'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, C-10 alkyl, or CI-6 alkyl, R3" is -OR'or -N(R3')2);

(d) R4 is hydrogen, Ci-io alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(e) R 5 is H, a lower alkyl, CN, vinyl, 0-(lower alkyl), hydroxyl lower alkyl, i.e., (CH2)pOH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R6 is H, R5 cannot be N3 and when X is OH, R6 is CH3 or CH2F and B is a purine base, R 5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, CI-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(CI- 4 alkyl), OC(O)O(CI- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI- 4 alkyl), O(C 2 - 4 alkenyl), S(C- 4 acyl), S(CI- 4 alkyl), S(C 2 - 4 alkynyl), S(C 2 -4 alkenyl), SO(CI- 4 acyl), SO(C- 4 alkyl), SO(C 2 - 4 alkynyl), SO(C 2 -4 alkenyl), S0 2 (C- 4 acyl), S0 2 (C- 4 alkyl), S 2 (C 2 - 4 alkynyl), S 2 (C 2 - 4

alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(Ci-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(CI- 4 acyl), O(CI- 4 alkyl), O(C 2 -4 alkenyl), S(CI- 4 acyl), S(C- 4 alkyl), S(C 2 -4 alkynyl), S(C 2 -4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2 -4 alkynyl), SO(C 2 -4 alkenyl), S0 2 (C 1 -4 acyl), S0 2 (C1 -4 alkyl), S0 2(C 2 -4 alkynyl), S0 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl),

-A')-

OS(O)2(C-4 alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4

alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

(i) R 1 0 and R 1 1are independently H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl of C1-C6, halogenated (F, Cl, Br, I) lower alkylof C1-C6, lower alkenylof C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6, lower alkynyl of C2-C6 such as CaCH, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of CI-C6, halogenated (F, Cl, Br, I) lower alkoxy of C1-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R1 0 is OH and R 1 is not NH2;

wherein R' is an optionally substituted alkyl , which includes, but is not limited to, an optionally substituted C1-2o alkyl, an optionally substituted Ci-io alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C2-C6, an optionally substituted lower alkenyl of C2-C6, or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C()(C-2o alkyl), C(O)(Ci-io alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

(j) Z is N or CR 12 ; and

R 12 is an H, halogen (including F, Cl, Br, I), OH, OR', SH, SR', NH2, NHR', NR'2, N02 lower alkyl of C1-C6, halogenated (F, Cl, Br, I) lower alkylof C1-C6, lower alkenylof C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6 , lower alkynyl of C2-C6, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of CI-C6, halogenated (F, Cl, Br, I) lower alkoxy ofC1-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'.

A second aspect of the third embodiment is directed to a compound represented by formula 1-5

wherein

(b) R2 is hydrogen or CH3;

(c) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH,

CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl;

(d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H.

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

(i) R 10 and R 1 1 are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R 1 0 is OH and R1 1 is not NH2;

wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

(j) Z is N or CR 12 ; and

R 12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkyl of Ci C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'.

A third aspect of the third embodiment is directed to a compound represented by formula1-5

wherein

(b) R2 is hydrogen or CH3;

-AA-

(d) R 4 is hydrogen, CH3, Et, Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(e) R' is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R' is CH3 or CH2F, R 5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(i) Rio and R" are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R 1 0 is OH and R1 1 is not NH2;

(j) Z is N or CR 12 ; and

A fourth aspect of the third embodiment is directed to a compound represented by formula I 5

wherein

(b) R2 is hydrogen;

(e) R' is H, with the provisos that when X is OH, R' is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(i) Ri and R" are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R 1 0 is OH and R1 1 is not NH2;

(j) Z is N or CR 12 ; and

A fifth aspect of the third embodiment is directed to a compound represented by formula1-5

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

A sixth aspect of the third embodiment is directed to a compound represented by formula 1-5

wherein

(b) R2 is hydrogen or CH3;

-A'7

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

(i) R 1 0 is NH2 and R1 is H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R';

(j) Z is N or CR 12 ; and

A seventh aspect of the third embodiment is directed to a compound represented by formula 1-5

wherein

(b) R2 is hydrogen or CH3;

(e) R 5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br,I, NH2 or N3;

A S2-

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(i) Rio is NH2 and R" is H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R';

(j) Z is N or CR 12 ; and

An eighth aspect of the third embodiment is directed to a compound represented by formula 1-5

wherein

(b) R2 is hydrogen;

(d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl;

(e) R 5 is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

_ AO_ wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

(j) Z is N or CR 12 ; and

A ninth aspect of the third embodiment is directed to a compound represented by formula I 5

wherein

(b) R2 is hydrogen;

(d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, or N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

R 1 2 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, NO2, lower alkyl of Ci C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'.

A tenth aspect of the third embodiment is directed to a compound represented by formula I 6

R10 z

N R3b R2 O_ R3 N 0

ORi R5 R6 NR1 CO2R 4 OR

Y X

1-6

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one ofC1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, CI-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, CI-6 acylamino, -NHSO2C-6 alkyl, -SO2N(R"')2, COR", and -SO2C-6

alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or CI-6 alkyl, Rl" is -OR'or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3 a and R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, CI-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl CI-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C-6 alkoxy, halogen, nitro and cyano; (ii) R3 and R3b both are C-6 alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R 3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v)R 3b is hydrogen and R3 a and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or C1-6 alkyl and R3 " is -OR' or -N(R 3 ')2); (vi) R 3 a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2 _r, 1_ indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or N(R 3')2);

(d) R4 is hydrogen, C1-10 alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy or halogen, Ci-io haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, Cl, Br,I, NH2, or N3;

(h) Y is OH, H, CI-4 alkyl, C24 alkenyl, C24 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(CI- 4 alkyl), OC(O)O(CI- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI- 4 alkyl), O(C 2-4 alkenyl), S(C- 4 acyl), S(CI- 4 alkyl), S(C 2 -4 alkynyl), S(C 2-4 alkenyl), SO(CI- 4 acyl), SO(C- 4 alkyl), SO(C 2- 4 alkynyl), SO(C 2 4 alkenyl), S0 2 (C- 4 acyl), S0 2 (C- 4 alkyl), S 2 (C 2 - 4 alkynyl), S 2 (C 2 - 4

alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(C-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(CI- 4 acyl), O(CI- 4 alkyl), O(C 2-4 alkenyl), S(CI- 4 acyl), S(C- 4 alkyl), S(C 2-4 alkynyl), S(C 2 4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2-4 alkynyl), SO(C 2-4 alkenyl), S0 2 (C 1 -4 acyl), S0 2 (C1 -4 alkyl), S0 2(C 2 -4 alkynyl), S0 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl),

OS(O) 2 (CI-4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

(i) R 10 and R 1 1 are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R 1 0 is OH and R1 is not NH2;

(j) Z is N or CR 12 ; and

An eleventh aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen or CH3;

(e) R' is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

(i) Ri and R 1 1 are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R 1 0 is OH and R1 1 is not NH2;

(j) Z is N or CR 12 ; and

A twelvth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen or CH3;

(e) R 5 is H, CN, CH2F, F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

R 12 is a H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkyl of Ci C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'.

A thirteenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen;

(e) R' is H, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(i) R 10 and R 1 1 are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', with the proviso that when R 10 is OH and R11 is not NH2; wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

(j) Z is N or CR 12 ; and

A fourteenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

R 12 is an H, halogen (including F, Cl, Br, I), OR', NH2,NHR', NR'2, NO2, lower alkyl of Ci C6, CO2R', CONH2,CONHR',CONR'2,CH=CHCO2H, or CH=CHCO2R'.

A fifteenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least oneofC1-6alkyl,C2-6alkenyl,C2-6alkynyl,C1-6alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6haloalkyl, -N(Rl')2, CI-6acylamino, -NHSO2C1-6alkyl, -SO2N(R')2,COR 1 ", and-SO2C-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to,C1-20 alkyl, Ci-io alkyl, orCI-6alkyl, R1"is -OR' or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3aand R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3')2, CI-6hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and arylC1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl,C1-6 alkoxy, halogen, nitro and cyano; (ii) R3aand R3 both areC-6alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen orC1-6alkyl and R3 " is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3,CH2CH3,CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3,CH2CO2H,CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3, CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H,CH2C(O)NH2,CH2CH2COOH,CH2CH2C(O)NH2,CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3 'is independently hydrogen or alkyl, which includes, but is not limited to,C1-20alkyl, Ci-io alkyl, orC1-6alkyl, R 3" is -OR' or N(R3')2);

(e) R' is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., (CH2)pOH, where p is 1 -6, including hydroxyl methyl (CH2OH), CH2F, N3, CH2CN, CH2NH2, CH2NHCH3, CH2N(CH3)2, alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R' is H, R5 cannot be N3 and when X is OH, R' is CH3 or CH2F and B is a purine base, R 5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, Ci-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, vinyl, N3, CN, Cl, Br, F, I, NO2, OC(O)O(CI- 4 alkyl), OC(O)O(CI- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI- 4 alkyl), O(C 2 - 4 alkenyl), S(C- 4 acyl), S(CI-4 alkyl), S(C 2 - 4 alkynyl), S(C 2 -4 alkenyl), SO(C 1-4 acyl), SO(C1 -4 alkyl), SO(C 2 -4 alkynyl), SO(C 2 -4 alkenyl), SO 2 (C- 4 acyl), SO 2 (C- 4 alkyl), SO 2 (C 2 - 4 alkynyl), SO 2 (C 2 - 4 alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(Ci-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), NO2, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(C 1-4 acyl), O(C- 4 alkyl), O(C 2 -4 alkenyl), S(C- 4 acyl), S(C- 4 alkyl), S(C 2 -4 alkynyl), S(C 2 -4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2 -4 alkynyl), SO(C 2 -4 alkenyl), SO 2 (C 1-4 acyl), SO 2 (C 1 -4 alkyl), SO 2 (C 2 -4 alkynyl), SO 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl), OS(O) 2 (CI-4 alkyl), OS(O) 2 (C 2 -4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

(j) Z is N or CR 12 ; and

R 1 2 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkyl of Ci C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'.

An sixteenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen or CH3;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

(j) Z is N or CR 12 ; and

A seventeenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen or CH3;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

An eighteenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(b) R2 is hydrogen;

(c) R3 a is H and R3b is H, CH3,CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, or lower cycloalkyl;

(e) R' is H, with the provisos that when X is OH, R6 isCH3or CH2F, R5 cannot be H;

(f) R 6 is H, CH3,CH2F, CHF2,CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2,OCH3, or OC(O)CH3;

(i) Rio is NH2and R" is H, F, Br, I, OH, OR', NH2,NHR', NR'2, CO2R', CONH2, CONHR',CONR'2,CH=CHCO2H, or CH=CHCO2R';

(j) Z is N or CR 12 ; and

R 12 is an H, halogen (including F, Cl, Br, I), OR', NH2,NHR', NR'2, N02, lower alkyl of Ci C6, CO2R', CONH2,CONHR',CONR'2,CH=CHCO2H, or CH=CHCO2R'.

A ninteenth aspect of the third embodiment is directed to a compound represented by formula 1-6

wherein

(a) R' is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(i) Rio is NH2 and R" are independently H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R';

(j) Z is N or CR 12 ; and

A fourth embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula c above, where R 1 is H and R2, R3 a, R3 bR4 ,, R , X, and Y are defined in the Summary of the Invention section above.

A first aspect of the fourth embodiment is directed to a compound represented by formula I

R10 z

R2 O N R3 b 1 o11 N R3aN 0 N

C0 2R 4 OR 1 R6

Y X

1-7

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least oneofC1-6alkyl,C2-6alkenyl,C2-6alkynyl,C1-6alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6haloalkyl, -N(Rl')2, C1-6acylamino, -NHSO2C1-6alkyl, -SO2N(R')2,COR1 ", and-SO2C-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to,C1-20 alkyl, Ci-io alkyl, orCI-6alkyl, R1"is -OR' or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3aand R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, C1-6hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and arylC1-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl,C1-6 alkoxy, halogen, nitro and cyano; (ii) R3aand R3 both areC-6alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R3b and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms (v)R3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen orC1-6alkyl and R3 " is -OR' or -N(R 3')2); (vi) R 3 a is H and R3b is H, CH3,CH2CH3,CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3,CH2CO2H, CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3, CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2,CH2CH2CH2CH2NH2, -

CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3 is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-2o alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR'or N(R 3')2);

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, CI-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(CI- 4 alkyl), OC(O)O(CI- 4 alkyl), OC(O)O(C 2 -4 alkynyl), OC(O)O(C 2 -4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI- 4 alkyl), O(C 2 - 4 alkenyl), S(C- 4 acyl), S(CI- 4 alkyl), S(C 2 - 4 alkynyl), S(C 2 -4 alkenyl), SO(CI- 4 acyl), SO(C- 4 alkyl), SO(C 2 - 4 alkynyl), SO(C 2 -4 alkenyl), S0 2 (C- 4 acyl), S0 2 (C- 4 alkyl), S0 2 (C 2 - 4 alkynyl), S0 2 (C 2 - 4 alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(Ci-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), N02, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 -4 alkynyl), C(O)O(C 2 -4 alkenyl), O(C 1-4 acyl), O(CI- 4 alkyl), O(C 2 -4 alkenyl), S(C- 4 acyl), S(C- 4 alkyl), S(C 2 -4 alkynyl), S(C 2 -4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2 -4 alkynyl), SO(C 2 -4 alkenyl), S0 2 (C 1 -4 acyl), S0 2 (C1 -4 alkyl), S0 2(C 2 -4 alkynyl), S0 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl), OS(O) 2 (CI-4 alkyl), OS(O) 2 (C 2 -4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2;

(i) R 1 0 is H, F, Cl, Br, I, OH, OR', SH, SR', NH2, NHR', NR'2, lower alkyl of C1-C6, halogenated (F, Cl, Br, I) lower alkylof C-C6, lower alkenylof C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6, lower alkynyl of C2-C6 such as CaCH, halogenated (F, Cl, Br,

I) lower alkynyl of C2-C6, lower alkoxy of C1-C6, halogenated (F, Cl, Br, I) lower alkoxy of CI-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R',

(j) Z is N or CR 12 ; and

R 12 is H, halogen (including F, Cl, Br, I), OH, OR', SH, SR', NH2, NHR', NR'2, N02 lower alkyl ofC1-C6, halogenated (F, Cl, Br, I) lower alkylofCi-C, lower alkenylofC2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C2-C6 , lower alkynyl of C2-C6, halogenated (F, Cl, Br, I) lower alkynyl of C2-C6, lower alkoxy of CI-C6, halogenated (F, Cl, Br, I) lower alkoxy ofC1-C6, CO2H, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that R 12 is not a: (i) -C-C-H, (ii) -C=CH2, or (iii) -N02.

A second aspect of the fourth embodiment is directed to a compound represented by formula 1-7

wherein

(b) R2 is hydrogen or CH3;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, halogen, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

(i) Rio is H, F, Br,I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R',

(j) Z is N or CR 12 ; and

R 12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkylof C1-C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that R 12 is not a: (i) -C-C-H, (ii) -C=CH2, or (iii) -N02.

A third aspect of the third embodiment is directed to a compound represented by formula 1-7

wherein

(b) R2 is hydrogen or CH3;

(e) R 5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 is CH3 or CH2F, R 5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(i) R 10 is H, F, Br,I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R',

(j) Z is N or CR 12 ; and

A fourth aspect of the fourth embodiment is directed to a compound represented by formula 1-7

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(i) Rio and R" H, F, Br, I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R',

(j) Z is N or CR 12 ; and

R 12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkyl of Ci C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that R 12 is not a: (i) -C-C-H, (ii) -C=CH2, or (iii) -N02.

A fifth aspect of the fourth embodiment is directed to a compound represented by formula I 7

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(i) R 10 is H, F, Br,I, OH, OR', NH2, NHR', NR'2, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R', wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

(j) Z is N or CR 12 ; and

R 12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkylof C1-C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'.

A sixth aspect of the fourth embodiment is directed to a compound represented by formula 1-8

z 0

R2 O N R3b I- * N RaN P-'* 0 0 N i--R11 R5\\\6 4 C0 2R ORR

Y X

1-8

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one ofC1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, CI-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, CI-6 acylamino, -NHSO2C1-6 alkyl, -SO2N(R"')2, COR", and -SO2C-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or CI-6 alkyl, Rl" is -OR'or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3 a and R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, CI-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl CI-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C-6 alkoxy, halogen, nitro and cyano; (ii) R3 and R3b both are C-6 alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R 3b and R2 together

_, 0o are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v) R3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3 ' is independently hydrogen or CI-6 alkyl and R3 " is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or

N(R 3')2);

(d) R4 is hydrogen, Ci-io alkyl, Ci-io alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C1-10 haloalkyl, C3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, Ci-4 alkyl, C24 alkenyl, C24 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(CI- 4 alkyl), OC(O)O(C2-4 alkynyl), OC(O)O(C2-4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(CI-4 alkyl), O(C2-4 alkenyl), S(CI-4 acyl), S(C-4 alkyl), S(C2 4 alkynyl), S(C24 alkenyl), SO(C1-4 acyl), SO(C-4 alkyl), SO(C2-4 alkynyl), SO(C2-4 alkenyl), S02(CI-4 acyl), S02(C-4 alkyl), S02(C2-4 alkynyl), S2(C2-4 alkenyl), OS(O)2(C-4 acyl), OS(O)2(C1-4 alkyl), OS(O)2(C2-4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(Ci-4 acyl), N(Ci-4 alkyl)2, N(Ci-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F, I),

N02, C(O)O(C1-4 alkyl), C(O)O(C1-4 alkyl), C(O)O(C 2 - 4 alkynyl), C(O)O(C 2 - 4 alkenyl), O(CI- 4 acyl), O(CI- 4 alkyl), O(C 2 -4 alkenyl), S(CI- 4 acyl), S(C- 4 alkyl), S(C 2 - 4 alkynyl), S(C 2 4 alkenyl), SO(C 1 -4 acyl), SO(C- 4 alkyl), SO(C 2 - 4 alkynyl), SO(C 2 - 4 alkenyl), S0 2 (C- 4 acyl), S0 2 (C 1-4 alkyl), S0 2 (C 2 -4 alkynyl), S0 2 (C 2 -4 alkenyl), OS() 2 (C- 4 acyl), OS(O) 2 (C- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(C-4 acyl)2;

(j) Z is N or CR 12 ; and

R 12 is H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkylof C1-C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that when base is represented by the structure c with R 1eing b hydrogen, R12 is not a: (i) -C--C H, (ii) -C=CH2, or (iii) -N02.

A seventh aspect of the fourth embodiment is directed to a compound represented by formula 1-8

wherein

(b) R2 is hydrogen or CH3;

'71 _

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, halogen, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

(j) Z is N or CR 12 ; and

An eighth aspect of the fourth embodiment is directed to a compound represented by formula 1-8

wherein

(b) R2 is hydrogen or CH3;

(d) R4 is hydrogen, CH3, Et, 'Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl , N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

A ninth aspect of the fourth embodiment is directed to a compound represented by formula 1-8

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

(j) Z is N or CR 12 ; and

A tenth aspect of the fourth embodiment is directed to a compound represented by formula 1-8

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

-7A- wherein R' is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR'2, each R' comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and

(j) Z is N or CR 12 ; and

R 12 is an H, halogen (including F, Cl, Br, I), OR', NH2, NHR', NR'2, N02, lower alkyl of Ci C6, CO2R', CONH2, CONHR', CONR'2, CH=CHCO2H, or CH=CHCO2R'; with the proviso that R 12 is not a: (i) -C-C-H, (ii) -C=CH2, or (iii) -N02. A fifth embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula d above, wherein R, R2, R3 a, R3b, R4, R 5 , R6, X, and Y are defined in the Summary of the Invention section above.

The first aspect of the fifth embodiment is directed to a compound represented by formula I 9

0 N

R3b R2 O NH

N P 0 0 N R3a N-- OJ

R6 NH 2 C0 2R 4 OR R5

Y X

1-9

wherein

(a) R 1 is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one ofC1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, F, Cl, Br, I, nitro, cyano, Ci 6 haloalkyl, -N(Rl')2, C1-6 acylamino, -NHSO2C1-6 alkyl, -SO2N(R"')2, COR1 ", and -SO2CI-6 alkyl; (R"'is independently hydrogen or alkyl, which includes, but is not limited to, C1-20 alkyl, Ci-io alkyl, or C1-6 alkyl, Rl" is -OR'or -N(Rl')2);

(b) R2 is hydrogen or CH3;

(c) R3a and R3 bare (i) independently selected from hydrogen, Ci-io alkyl, cycloalkyl, (CH2)c(NR 3 ')2, C1-6 hydroxyalkyl, -CH2SH, -(CH2)2S(O)dMe, -(CH2)3NHC(=NH)NH2, (1H- indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, -(CH2)eCOR 3", aryl and aryl CI-3 alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, Ci-io alkyl, C-6 alkoxy, halogen, nitro and cyano; (ii) R3 and R3b both are C-6 alkyl; (iii) R3 a and R3b together are(CH2)fso as to form a spiro ring; (iv) R3a is hydrogen and R 3b and R2 together are (CH2)n so as to form a cyclic ring that includes the adjoining N and C atoms (v)R 3b is hydrogen and R3a and R2 together are (CH2)nso as to form a cyclic ring that includes the adjoining N and C atoms, where c is to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R3' is independently hydrogen or CI-6 alkyl and R3 " is -OR' or -N(R 3')2); (vi) R3a is H and R3b is H, CH3, CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2 indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl; or (viii) R3 a is CH3, -CH2CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H, where R3'is independently hydrogen or alkyl, which includes, but is not limited to, C-20 alkyl, Ci-io alkyl, or CI-6 alkyl, R3 " is -OR' or

N(R 3')2);

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OMe, halogen, NH2, or N3;

(h) Y is OH, H, CI-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, vinyl, N3, CN, Cl, Br, F, I, N02, OC(O)O(C1-4 alkyl), OC(O)O(C1-4 alkyl), OC(O)O(C2-4 alkynyl), OC(O)O(C2-4 alkenyl), OCi-io haloalkyl, O(aminoacyl), O(Ci-io acyl), O(C-4 alkyl), O(C2-4 alkenyl), S(C-4 acyl), S(C1-4 alkyl), S(C2-4 alkynyl), S(C2-4 alkenyl), SO(C1-4 acyl), SO(C-4 alkyl), SO(C2-4 alkynyl), SO(C 2 -4 alkenyl), SO 2 (C1 -4 acyl), SO 2 (C-4 alkyl), SO 2 (C 2 - 4 alkynyl), SO 2 (C 2 - 4 alkenyl), OS(O) 2 (C 1-4acyl), OS(O) 2 (CI- 4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(C-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(Ci-is acyl)2, wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N3, CN, one to three halogen (Cl, Br, F,I), NO2, C(O)O(C1- 4 alkyl), C(O)O(C1- 4 alkyl), C(O)O(C 2 - 4 alkynyl), C(O)O(C 2 - 4 alkenyl), O(C 1-4 acyl), O(C- 4 alkyl), O(C 2 - 4 alkenyl), S(C- 4 acyl), S(C- 4 alkyl), S(C 2 - 4 alkynyl), S(C 2 -4 alkenyl), SO(C- 4 acyl), SO(C- 4 alkyl), SO(C 2 - 4 alkynyl), SO(C 2 - 4 alkenyl), SO 2 (C 1-4 acyl), SO 2 (C 1 -4 alkyl), SO 2 (C 2 -4 alkynyl), SO 2 (C 2 -4 alkenyl), OS(O) 2 (CI- 4 acyl), OS(O) 2 (CI-4 alkyl), OS(O) 2 (C 2 - 4 alkenyl), NH2, NH(CI-4 alkyl), NH(C2-4 alkenyl), NH(C2-4 alkynyl), NH(CI-4 acyl), N(CI-4 alkyl)2, N(CI-4 acyl)2.

A second aspect of the fifth embodiment is directed to a compound represented by formula 1-9

wherein

(b) R2 is hydrogen or CH3;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R' is CH3 or CH2F, R5 cannot be H.

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, halogen, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F,I, OC(O)CH3, OCH3;

A third aspect of the fifth embodiment is directed to a compound represented by formula1-9

'7'7 wherein

(b) R 2 is hydrogen or CH3;

(e) R 5 is H, CN, CH2F, F, Cl, Br, or I; with the proviso that X is OH, R6 isCH3or CH2F, R 5 cannot be H;

(f) R 6 is H, CH3,CH2F, CHF2,CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 N3, OCH3, or OC(O)CH3;

A fourth aspect of the fifth embodiment is directed to a compound represented by formula I 9

wherein

(b) R2 is hydrogen;

'7Q-

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

A fifth aspect of the fifth embodiment is directed to a compound represented by formula 1-9

wherein

(b) R2 is hydrogen;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

A sixth aspect of the fifth embodiment is directed to a compound represented by formula I 10

0 N

R3b R2 0 NH

RI N-- * O O N R50R6 CO2 R4 OR 1 NH 2

Y X

'70_

1-10

wherein

(a) R 1 is hydrogen, methyl, ethyl, n-propyl, i-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH3,OCH3, F, Cl, Br, I, nitro, cyano, and a CH3-qXq,where X is F, Cl, Br, or I, and q is 1-3;

(b) R2 is hydrogen or CH3;

(c) R3 a is H and R3b is H, CH3,CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3,CH2CO2H, CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2,CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl or R3a is CH3, CH(CH3)2,CH2CH(CH3)2,CH(CH3)CH2CH3,CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2,CH2CH2COOH, CH2CH2C(O)NH2,CH2CH2CH2CH2NH2, CH2CH2CH2NHC(NH)NH2,CH2-imidazol-4-yl, CH2OH, CH(OH)CH3,CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H;

(e) R 5 is H, CN, CH3,OCH3,CH2OH, CH2F, N3, CH2CN, CH2N3, CH2NH2, CH2NHCH3,CH2N(CH3)2, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R6 is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3,CH2F, CHF2,CF3, F, or CN;

(g) X is H, OH, F, OCH3,Cl, Br, I, NH2, or N3;

(h) Y is OH, H, CH3, vinyl, N3, CN, Cl, Br, F, I, OC(O)CH3,OCH3,NH2,NHCH3, NH(vinyl), NH(acetyl), NH(C(O)CH3),N(CH3)2,N(C(O)CH3)2;

A seventh aspect of the fifth embodiment is directed to a compound represented by formula 1-10

wherein

(b) R 2 is hydrogen or CH3;

(e) R 5 is H, CN, CH3, OCH3, CH2OH, CH2F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R' is CH3 or CH2F, R5 cannot be H;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, F, or CN;

(g) X is H, OH, F, OCH3, Cl, Br, I, NH2, or N3; and

(h) Y is OH, H, CH3, vinyl, NH2, N3, CN, Cl, Br, F, I, OC(O)CH3, OCH3.

An eighth aspect of the fifth embodiment is directed to a compound represented by formula 1-10

wherein

(b) R2 is hydrogen or CH3;

_ 1 _

(e) R 5 is H, CN, CH2F, F, Cl, Br, or I, with the provisos that when X is OH, R is CH3 or CH2F, R5 cannot be H;

(f) R is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, F, OCH3, F, Cl, Br, I, NH2 or N3;

(h) Y is H, OH, CH3, F, Cl, Br,I, NH2 or N3, OCH3, or OC(O)CH3;

A ninth aspect of the fifth embodiment is directed to a compound represented by formula I 10

wherein

(b) R2 is hydrogen;

(f) R is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3;

A tenth aspect of the fifth embodiment is directed to a compound represented by formula I 10

wherein

(b) R2 is hydrogen;

S2)-

(c) R3 is H and R3bis H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl;

(f) R 6 is H, CH3, CH2F, CHF2, CF3, or F;

(g) X is H, OH, OCH3, F, NH2 or N3;

(h) Y is OH, NH2, OCH3, or OC(O)CH3.

The following tables contain numeric identifiers associated with various substituent designators that should be viewed in light of the accompanying structure. These structures are contemplated species of the various aspects of the disclosed embodiments and are not intended to be limiting on full breadth of the contemplated compound represented by the structure of formula I. However, it is contemplated that any one of the exemplified nucleoside bases can be used in combination with any one of contemplated species that specify a particular combination of R', R2, R3 a, R 3 , R4 , R 5, R 6, X, and Y. In each of the presented tables, the phosphoramidate substituent containing the substituents R3a and R3b are depicted without reference to stereochemical structure (cf structures I-1, 1-3, 1-5, 1-7, and I 9 above). It is contemplated that the compounds recited below embody compounds in which R3 a projects toward the viewer while R3 bprojects away from the viewer (cf. structures 1-2, I 4, 1-6, 1-8, and 1-10). Moreover, it is contemplated that the compounds recited below also embody compounds in which R3a projects away from the viewer while R 3b projects towards the viewer. Not meant to be limiting, however, it is contemplated that preferred compounds are those in which R3a projects towards the viewer and R3b projects away from the viewer such that the natural L-amino acid (S)-configuration is presented. Additionally, the inventors recognize that the phosphorus atom of the phosphoramidate moiety is another source of chirality. Although the structures below do not specifically depict chirality at phosphorus, the inventors recognize that stereochemical configurations are possible such that in a staggered (or zig-zag) line structure the oxo-substitutent projects towards the viewer while the OR' substitutent projects away from the viewer, and vice versa, i.e., where the Cahn-Ingold-Prelog stereochemical designation of phosphorous is either R or S. Therefore, the structures below include all possible stereochemical configurations possible for phosphorus.

R9

8 R

IN R2 O R3b P R7 N 0 R3a N-P--O

C0 2 R 4 OR 1 R6

Y X II

Table II-1. No R1 R 2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 II-1-1 CH 3 H H H CH 3 H CH 3 OH OH H H NH 2 11-1-2 CH 3 H H CH3 CH 3 H CH 3 OH OH H H NH 2 11-1-3 CH 3 H H CH(CH 3)2 CH 3 H CH 3 OH OH H H NH 2 11-1-4 CH 3 H H CH2CH(CH 3)2 CH 3 H CH 3 OH OH H H NH 2 11-1-5 CH 3 H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-1-7 CH 3 H H CH2 CH 2 SCH 3 CH 3 H CH 3 OH OH H H NH 2 II-1-8 CH 3 * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 11-2. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 11-2-1 Et H H H CH 3 H CH 3 OH OH H H NH 2 11-2-2 Et H H CH3 CH3 H CH 3 OH OH H H NH 2 11-2-3 Et H H CH(CH 3)2 CH3 H CH 3 OH OH H H NH 2 11-2-4 Et H H CH2CH(CH 3) 2 CH 3 H CH 3 OH OH H H NH 2 11-2-5 Et H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-2-6 Et H H CH 2-indol-3-yl CH3 H CH 3 OH OH H H NH 2 11-2-7 Et H H CH2CH2SCH 3 CH 3 H CH 3 OH OH H H NH 2 II-2-8 Et * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 11-3. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9

-QA-

No R1 R2 R 3a R3 b R4 R 5 R' X Y R7 R' R9 II-3-1 tPr H H H CH 3 H CH 3 OH OH H H NH 2 11-3-2 'Pr H H CH 3 CH 3 H CH 3 OH OH H H NH 2 11-3-3 'Pr H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-3-4 'Pr H H CH 2CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-3-5 'Pr H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-3-6 'Pr H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-3-7 'Pr H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H NH 2 II-3-8 iPr * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-4. N9 R1 R2 R3 a R 3b R4 R 5 R6 X Y R7 R' R9 II-4-1 'Bu H H H CH 3 H CH 3 OH OH H H NH 2 11-4-2 'Bu H H CH 3 CH 3 H CH 3 OH OH H H NH 2 11-4-3 'Bu H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-4-4 'Bu H H CH 2CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-4-5 'Bu H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-4-6 'Bu H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-4-7 'Bu H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H NH 2 II-4-8 'Bu * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-5. N9 Rl R 2 R 3 a R3 b R4 R 5 R6 X Y R7 R' R9 II-5-1 Ph H H H CH 3 H CH 3 OH OH H H NH 2 11-5-2 Ph H H CH 3 CH 3 H CH 3 OH OH H H NH 2 11-5-3 Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-5-4 Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-5-5 Ph H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-5-6 Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-5-7 Ph H H CH 2CH2SCH 3 CH 3 H CH 3 OH OH H H NH 2 II-5-8 Ph * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-6.

N9 R1 R 2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 11-6-1 p-Me-Ph H H H CH 3 H CH 3 OH OH H H NH 2 11-6-2 p-Me-Ph H H CH 3 CH 3 H CH 3 OH OH H H NH 2

S2r-

R' N9 Rl R 2 R3 a Rb R4 R' X Y R7 R' R9 11-6-3 p-Me-Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-6-4 p-Me-Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-6-5 p-Me-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-6-7 p-Me-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H NH 2 11-6-8 p-Me-Ph * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-7. N9 Rl R 2 R 3a R 3b R4 R R6 X Y R7 R' R9 11-7-1 p-F-Ph H H H CH 3 H CH 3 OH OH H H NH 2 11-7-2 p-F-Ph H H CH 3 CH 3 H CH 3 OH OH H H NH 2 11-7-3 p-F-Ph H H CH(CH3) 2 CH3 H CH 3 OH OH H H NH 2 11-7-4 p-F-Ph H H CH 2CH(CH3) 2 CH3 H CH 3 OH OH H H NH 2 11-7-6 p-F-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H CH 3 OH OH H H NH 2 11-7-8 p-F-Ph H H CH 2CH 2SCH 3 CH3 H CH 3 OH OH H H NH 2 11-7-20 p-F-Ph * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-8. N9 Rl R 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 11-8-1 p-Cl-Ph H H H CH 3 H CH 3 OH OH H H NH 2 11-8-2 p-Cl-Ph H H CH3 CH 3 H CH 3 OH OH H H NH 2 11-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-8-5 p-Cl-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-8-7 p-Cl-Ph H H CH2CH 2SCH 3 CH 3 H CH 3 OH OH H H NH 2 11-8-8 p-Cl-Ph * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 11-9. N9 Rl R2 R 3a R 3b R4 R 5 R6 X Y R7 R' R9 11-9-1 p-Br-Ph H H H CH 3 H CH 3 OH OH H H NH 2 11-9-2 p-Br-Ph H H CH 3 CH 3 H CH 3 OH OH H H NH 2 11-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-9-4 p-Br-Ph H H CH 2CH(CH 3) 2 CH 3 H CH 3 OH OH H H NH 2 11-9-6 p-Br-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2

S2 r-

N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 11-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-9-8 p-Br-Ph H H CH 2CH 2 SCH3 CH 3 H CH 3 OH OH H H NH 2 11-9-20 p-Br-Ph * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-10. R N9 Rl R 2 R 3 a R3 b R4 R X Y R7 R' R9 11-10-1 p-I-Ph H H H CH 3 H CH 3 OH OH H H NH 2 11-10-2 p-I-Ph H H CH 3 CH 3 H CH 3 OH OH H H NH 2 11-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-10-4 p-I-Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 OH OH H H NH 2 11-10-5 p-I-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H NH 2 11-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H NH 2 11-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H NH 2 11-10-8 p-I-Ph * H * CH 3 H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-11. N9 R R2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 II-11-1 CH3 H H H Et H CH 3 OH OH H H NH 2 11-11-2 CH3 H H CH 3 Et H CH 3 OH OH H H NH 2 11-11-3 CH3 H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-11-4 CH3 H H CH 2CH(CH 3) 2 Et H CH 3 OH OH H H NH 2 11-11-5 CH3 H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-11-6 CH3 H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-11-7 CH3 H H CH 2CH 2SCH3 Et H CH 3 OH OH H H NH 2 II-11-8 CH3 * H * FtH CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-12. N9 Rl R 2 R 3a R3 b R4 R R6 X Y R7 R' R9 II-12-1 Et H H H Et H CH 3 OH OH H H NH 2 11-12-2 Et H H CH3 Et H CH 3 OH OH H H NH 2 11-12-3 Et H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-12-4 Et H H CH2CH(CH 3) 2 Et H CH 3 OH OH H H NH 2 11-12-5 Et H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-12-6 Et H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-12-7 Et H H CH2CH 2SCH 3 Et H CH 3 OH OH H H NH 2 II-12-8 Et * H * EtH CH 3 OH OH H H NH 2 *R2 and R3b joined together by (CH2)3 to formfive-membered ring.

S2'7-

Table 11-13. N9 R1 R2 R 3 a R 3b R4 R5 R6 X Y R7 R' R9 II-13-1 'Pr H H H Et H CH 3 OH OH H H NH 2 11-13-2 'Pr H H CH 3 Et H CH 3 OH OH H H NH 2 11-13-3 'Pr H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-13-4 Pr H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-13-5 Pr H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-13-6 Pr H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-13-7 Pr H H CH 2CH 2SCH3 Et H CH 3 OH OH H H NH 2 II-13-8 Pr * H * EtH CH 3 OH OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 11-14. No R1 R2 R R3b R4 R5 R6 X Y R7 R' R9 3a

II-14-1 'Bu H H H Et H CH 3 OH OH H H NH 2 11-14-2 'Bu H H CH 3 Et H CH 3 OH OH H H NH 2 11-14-3 'Bu H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-14-4 'Bu H H CH 2CH(CH 3) 2 Et H CH 3 OH OH H H NH 2 11-14-5 'Bu H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-14-6 'Bu H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-14-7 'Bu H H CH 2CH2SCH 3 Et H CH 3 OH OH H H NH 2 II-14-8 'Bu * H * Et H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-15. N9 R R2 R 3 a R 3b R 5 RR X Y R7 R' R9 II-15-1 Ph H H H Et H CH 3 OH OH H H NH 2 11-15-2 Ph H H CH 3 Et H CH 3 OH OH H H NH 2 11-15-3 Ph H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-15-4 Ph H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-15-5 Ph H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-15-6 Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-15-7 Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H NH 2 II-15-8 Ph * H * FtH CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-16. N9 R1 R 2 R 3 a R3 b R 5 RR X Y R7 R' R9 11-16-1 p-Me-Ph H H H Et H CH 3 OH OH H H NH 2 11-16-2 p-Me-Ph H H CH 3 Et H CH 3 OH OH H H NH 2

R' N9 Rl R 2 R 3 a Rb R4 R X Y R7 R' R9 11-16-3 p-Me-Ph H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-16-4 p-Me-Ph H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-16-5 p-Me-Ph H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H NH 2 11-16-8 p-Me-Ph * H * Et H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-17. N9 Rl R 2 R 3a R 3b R4 R R6 X Y R7 R' R9 11-17-1 p-F-Ph H H H Et H CH 3 OH OH H H NH 2 11-17-2 p-F-Ph H H CH 3 Et H CH 3 OH OH H H NH 2 11-17-3 p-F-Ph H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-17-4 p-F-Ph H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-17-5 p-F-Ph H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-17-6 p-F-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H NH 2 11-17-8 p-F-Ph * H * Et H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-18. N9 Rl R 2 R 3 a R3 b R4 R5 R6 X Y R7 R' R9 11-18-1 p-Cl-Ph H H H Et H CH3 OH OH H H NH 2 11-18-2 p-Cl-Ph H H CH3 Et H CH3 OH OH H H NH 2 11-18-3 p-Cl-Ph H H CH(CH 3) 2 Et H CH3 OH OH H H NH 2 11-18-4 p-Cl-Ph H H CH2CH(CH3) 2 Et H CH3 OH OH H H NH 2 11-18-5 p-Cl-Ph H H CH 2Ph Et H CH3 OH OH H H NH 2 11-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H CH3 OH OH H H NH 2 11-18-7 p-Cl-Ph H H CH2CH 2SCH 3 Et H CH3 OH OH H H NH 2 11-18-8 p-Cl-Ph * H * Et H CH3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 11-19. N9 Rl R2 R3a R 3b R4 R5 R6 X Y R7 R' R9 11-19-1 p-Br-Ph H H H Et H CH 3 OH OH H H NH 2 11-19-2 p-Br-Ph H H CH 3 Et H CH 3 OH OH H H NH 2 11-19-3 p-Br-Ph H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-19-4 p-Br-Ph H H CH 2CH(CH 3) 2 Et H CH 3 OH OH H H NH 2 11-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 OH OH H H NH 2

N9 Rl R2 R3 a R3 b R4 R' R' X Y R7 R' R9 11-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-19-7 p-Br-Ph H H CH 2CH 2 SCH3 Et H CH 3 OH OH H H NH 2 11-19-8 p-Br-Ph * H * Et H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-20. N9 Rl R 2 R 3 a R3 b R4 R R6 X Y R7 R' R9 11-20-1 p-I-Ph H H H Et H CH 3 OH OH H H NH 2 11-20-2 p-I-Ph H H CH 3 Et H CH 3 OH OH H H NH 2 11-20-3 p-I-Ph H H CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-20-4 p-I-Ph H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H NH 2 11-20-5 p-I-Ph H H CH 2Ph Et H CH 3 OH OH H H NH 2 11-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H NH 2 11-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H NH 2 11-20-8 p-I-Ph * H * Et H CH 3 OH OH H H NH 2 *R2 and R 3b joined together by (CH 2 ) 3 to formfive-membered ring.

Table 11-21. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 11-21-1 CH3 H H H 'Pr H CH 3 OH OH H H NH 2 11-21-2 CH3 H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-21-3 CH3 H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-21-4 CH3 H H CH 2CH(CH 3) 2 'Pr H CH 3 OH OH H H NH 2 11-21-5 CH3 H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-21-6 CH3 H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-21-7 CH3 H H CH 2CH 2SCH3 'Pr H CH 3 OH OH H H NH 2 11-21-8 CH3 * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-22. N9 Rl R2 R3 a R3 b R5 R R X Y R7 R' R9 II-22-1 Et H H H 'Pr H CH 3 OH OH H H NH 2 11-22-2 Et H H CH3 'Pr H CH 3 OH OH H H NH 2 11-22-3 Et H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-22-4 Et H H CH2CH(CH 3) 2 'Pr H CH 3 OH OH H H NH 2 11-22-5 Et H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-22-6 Et H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-22-7 Et H H CH2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 II-22-8 Et * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

on_

Table 11-23. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 11-23-1 'Pr H H H 'Pr H CH 3 OH OH H H NH 2 11-23-2 'Pr H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-23-3 'Pr H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-23-4 'Pr H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-23-5 'Pr H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-23-6 'Pr H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-23-7 'Pr H H CH 2CH 2SCH3 'Pr H CH 3 OH OH H H NH 2 11-23-8 'Pr * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-24. N9 R R2 R 3a R3b R4 R' R6 X Y R7 R' R9 11-24-1 'Bu H H H 'Pr H CH 3 OH OH H H NH 2 11-24-2 'Bu H H CH3 'Pr H CH 3 OH OH H H NH 2 11-24-3 'Bu H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-24-4 'Bu H H CH2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-24-5 'Bu H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-24-6 'Bu H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-24-7 'Bu H H CH2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 11-24-8 'Bu * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-25. N9 R R2 R 3 a R3 b R 5 R6 X Y R7 R' R9 II-25-1 Ph H H H 'Pr H CH 3 OH OH H H NH 2 11-25-2 Ph H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-25-3 Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-25-4 Ph H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-25-5 Ph H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-25-7 Ph H H CH 2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 II-25-8 Ph * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-26. N9 Rl R2 R 3 a R3 b R5 R6 X Y R7 R' R9

_ 01 _

N9 Rl R2 R3 a R3 b R4 R R6 X Y R7 R' R9 11-26-1 p-Me-Ph H H H 'Pr H CH 3 OH OH H H NH 2 11-26-2 p-Me-Ph H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-26-4 p-Me-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-26-7 p-Me-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 11-26-8 p-Me-Ph * H * 'Pr H CH 3 OH OH H H NH 2 2 *R and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 11-27. N9 Rl R2 R 3a R3b R4 R R6 X Y R7 R' R9 11-27-1 p-F-Ph H H H 'Pr H CH 3 OH OH H H NH 2 11-27-2 p-F-Ph H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-27-3 p-F-Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-27-4 p-F-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-27-5 p-F-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-27-7 p-F-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 11-27-8 p-F-Ph * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-28. N9 Rl R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 11-28-1 p-Cl-Ph H H H 'Pr H CH 3 OH OH H H NH 2 11-28-2 p-Cl-Ph H H CH3 'Pr H CH 3 OH OH H H NH 2 11-28-3 p-Cl-Ph H H CH(CH 3) 2 'Pr H CH 3 OH OH H H NH 2 11-28-4 p-Cl-Ph H H CH2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-28-5 p-Cl-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 11-28-8 p-Cl-Ph * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 11-29. N9 Rl R2 R3a R 3b R4 R5 R6 X Y R7 R' R9 11-29-1 p-Br-Ph H H H 'Pr H CH 3 OH OH H H NH 2 11-29-2 p-Br-Ph H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2

01_

N9 Rl R2 R3 a R3 b R4 R5 R' X Y R7 R' R9 11-29-4 p-Br-Ph H H CH 2CH(CH 3) 2 'Pr H CH 3 OH OH H H NH 2 11-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-29-7 p-Br-Ph H H CH 2CH 2 SCH3 'Pr H CH 3 OH OH H H NH 2 11-29-8 p-Br-Ph * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 11-30. N9 Rl R2 R 3 R3 b R4 R R6 X Y R7 R' R9 11-30-1 p-I-Ph H H H 'Pr H CH 3 OH OH H H NH 2 11-30-2 p-I-Ph H H CH 3 'Pr H CH 3 OH OH H H NH 2 11-30-3 p-I-Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-30-4 p-I-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H NH 2 11-30-5 p-I-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H NH 2 11-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H NH 2 11-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 OH OH H H NH 2 11-30-8 p-I-Ph * H * 'Pr H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-31. No R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 11-31-1 CH3 H H H "Bu H CH3 OH OH H H NH 2 11-31-2 CH3 H H CH 3 "Bu H CH3 OH OH H H NH 2 11-31-3 CH3 H H CH(CH3) 2 "Bu H CH3 OH OH H H NH 2 11-31-4 CH3 H H CH 2CH(CH 3) 2 "Bu H CH3 OH OH H H NH 2 11-31-5 CH3 H H CH 2Ph "Bu H CH3 OH OH H H NH 2 11-31-6 CH3 H H CH 2-indol-3-yl "Bu H CH3 OH OH H H NH 2 11-31-7 CH3 H H CH 2CH 2SCH3 "Bu H CH3 OH OH H H NH 2 11-31-8 CH3 * H * "Bu H CH3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-32. N9 Rl R 2 R3 a 3 R R4 R5 R6 X Y R7 R' R9 11-32-1 Et H H H "Bu H CH 3 OH OH H H NH 2 11-32-2 Et H H CH3 "Bu H CH 3 OH OH H H NH 2 11-32-3 Et H H CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-32-4 Et H H CH2CH(CH 3) 2 "Bu H CH 3 OH OH H H NH 2 11-32-5 Et H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-32-6 Et H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2

02_

N9 Rl R2 R3 a 3 R b R4 R' R' X Y R7 R' R9 11-32-7 Et H H CH2CH 2SCH 3 "Bu H CH 3 OH OH H H NH 2 II-32-8 Et * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-33. No R R2 R3 a R3 b R4 R 6 X Y R7 R' R9 11-33-1 'Pr H H H "Bu H CH3 OH OH H H NH 2 11-33-2 'Pr H H CH 3 "Bu H CH3 OH OH H H NH 2 11-33-3 'Pr H H CH(CH3) 2 "Bu H CH3 OH OH H H NH 2 11-33-4 'Pr H H CH 2CH(CH3) 2 "Bu H CH3 OH OH H H NH 2 11-33-5 'Pr H H CH 2Ph "Bu H CH3 OH OH H H NH 2 11-33-6 'Pr H H CH 2-indol-3-yl "Bu H CH3 OH OH H H NH 2 11-33-7 'Pr H H CH 2CH 2SCH3 "Bu H CH3 OH OH H H NH 2 11-33-8 'Pr * H * "Bu H CH3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

OA _

Table 11-34. No R1 R2 R 3a R 3b R4 R' R6 X Y R7 R' R9 11-34-1 'Bu H H H "Bu H CH 3 OH OH H H NH 2 11-34-2 'Bu H H CH3 "Bu H CH 3 OH OH H H NH 2 11-34-3 'Bu H H CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-34-4 'Bu H H CH2CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-34-5 'Bu H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-34-6 'Bu H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2 11-34-7 'Bu H H CH2CH 2SCH 3 "Bu H CH 3 OH OH H H NH 2 11-34-8 'Bu * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 11-35. No R 2 2 R 3aRb R4 R5 R6 X Y R7 R' R9 II-35-1 Ph H H H "Bu H CH 3 OH OH H H NH 2 11-35-2 Ph H H CH 3 "Bu H CH 3 OH OH H H NH 2 11-35-3 Ph H H CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-35-4 Ph H H CH 2CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-35-5 Ph H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-35-6 Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2 11-35-7 Ph H H CH 2CH 2SCH 3 "Bu H CH 3 OH OH H H NH 2 II-35-8 Ph * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 11-36. N9 R1 R 2 R 3a R 3b R4 R R X Y R7 R' R9

11-36-1 p-Me-Ph H H H "Bu H CH 3 OH OH H H NH 2 11-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 OH OH H H NH 2 11-36-3 p-Me-Ph H H CH(CH 3) 2 "Bu H CH 3 OH OH H H NH 2 11-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H CH 3 OH OH H H NH 2 11-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2 11-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 OH OH H H NH 2 11-36-8 p-Me-Ph * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3 joined together by (CH 2) 3 to form five-membered ring.

Table 11-37. N9 R1 R 2 R 3aRSb R4 R5 R6 X Y R7 R' R9 11-37-1 p-F-Ph H H H "Bu H CH 3 OH OH H H NH 2 11-37-2 p-F-Ph H H CH 3 "Bu H CH 3 OH OH H H NH 2 11-37-3 p-F-Ph H H CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2

0_r-

R' N9 Rl R2 R 3a Rb R4 R5 X Y R7 R' R9 11-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-37-5 p-F-Ph H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2 11-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 OH OH H H NH 2 11-37-8 p-F-Ph * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-38. N9 Rl R2 R 3a R 3b R4 R' R6 X Y R7 R' R9 11-38-1 p-Cl-Ph H H H "Bu H CH 3 OH OH H H NH 2 11-38-2 p-Cl-Ph H H CH3 "Bu H CH 3 OH OH H H NH 2 11-38-3 p-Cl-Ph H H CH(CH 3) 2 "Bu H CH 3 OH OH H H NH 2 11-38-4 p-Cl-Ph H H CH2 CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-38-5 p-Cl-Ph H H CH 2 Ph "Bu H CH 3 OH OH H H NH 2 11-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2 11-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 OH OH H H NH 2 11-38-8 p-Cl-Ph * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 11-39. N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 11-39-1 p-Br-Ph H H H "Bu H CH 3 OH OH H H NH 2 11-39-2 p-Br-Ph H H CH 3 "Bu H CH 3 OH OH H H NH 2 11-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-39-4 p-Br-Ph H H CH 2CH(CH 3 ) 2 "Bu H CH 3 OH OH H H NH 2 11-39-5 p-Br-Ph H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2 11-39-7 p-Br-Ph H H CH 2CH 2 SCH3 "Bu H CH 3 OH OH H H NH 2 11-39-8 p-Br-Ph * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 11-40. N9 Rl R2 R 3a R 3b R4 R R6 X Y R7 R' R9 11-40-1 p-I-Ph H H H "Bu H CH 3 OH OH H H NH 2 11-40-2 p-I-Ph H H CH 3 "Bu H CH 3 OH OH H H NH 2 11-40-3 p-I-Ph H H CH(CH 3) 2 "Bu H CH 3 OH OH H H NH 2 11-40-4 p-I-Ph H H CH 2CH(CH3) 2 "Bu H CH 3 OH OH H H NH 2 11-40-5 p-I-Ph H H CH 2Ph "Bu H CH 3 OH OH H H NH 2 11-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H NH 2

_or_

R' N9 R1 R 2 R 3 a R3 b R4 R5 X Y R7 R' R9 11-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 OH OH H H NH 2 11-40-8 p-I-Ph * H * "Bu H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-41. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 II-41-1 CH3 H H H Bz H CH 3 OH OH H H NH 2 11-41-2 CH3 H H CH 3 Bz H CH 3 OH OH H H NH 2 11-41-3 CH3 H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-41-4 CH3 H H CH 2CH(CH 3) 2 Bz H CH 3 OH OH H H NH 2 11-41-5 CH3 H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-41-6 CH3 H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-41-7 CH3 H H CH 2CH 2SCH3 Bz H CH 3 OH OH H H NH 2 II-41-8 CH3 * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-42. N9 Rl R 2 R 3a R R4 R' R6 X Y R7 R' R9 11-42-1 Et H H H Bz H CH 3 OH OH H H NH 2 11-42-2 Et H H CH3 Bz H CH 3 OH OH H H NH 2 11-42-3 Et H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-42-4 Et H H CH2CH(CH 3) 2 Bz H CH 3 OH OH H H NH 2 11-42-5 Et H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-42-6 Et H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-42-7 Et H H CH2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 II-42-8 Et * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-43. R' No R1 R2 R3a R3b R4 R5 R6 X Y R7 R9 *R 2 and 11-43-1 'Pr H H H Bz H CH 3 OH OH H H NH 2 R3 b joined 11-43-2 'Pr H H CH 3 Bz H CH 3 OH OH H H NH 2 together 11-43-3 'Pr H H CH(CH3) 2 Bz H CH 3 OH OH H H N by (CH2)3 2

11-43-4 'Pr H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 to form 11-43-5 'Pr H H CH 2Ph Bz H CH 3 OH OH H H NH 2 five 11-43-6 Pr H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 membere 11-43-7 1Pr H H CH 2CH 2SCH3 Bz H CH 3 OH OH H H NH 2 11-43-8 Pr * H * Bz H CH 3 OH OH H H NH 2 d ring.

Table 11-44.

o7

R R 3a R3 b R4 R' R' X Y R7 R' R9 N9 R2 II-44-1 'Bu H H H Bz H CH 3 OH OH H H NH 2 11-44-2 'Bu H H CH3 Bz H CH 3 OH OH H H NH 2 11-44-3 'Bu H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-44-4 'Bu H H CH2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-44-5 'Bu H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-44-6 'Bu H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-44-7 'Bu H H CH2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 II-44-8 'Bu * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-45. No R R2 R 3 a R 3b R4 R R X Y R7 R' R9 II-45-1 Ph H H H Bz H CH 3 OH OH H H NH 2 11-45-2 Ph H H CH 3 Bz H CH 3 OH OH H H NH 2 11-45-3 Ph H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-45-4 Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-45-5 Ph H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-45-6 Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-45-7 Ph H H CH 2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 II-45-8 Ph * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-46. N9 Rl R 2 R 3 a R3 b R4 R5 R6 X Y R 7 R R9 11-46-1 p-Me-Ph H H H Bz H CH 3 OH OH H H NH 2 11-46-2 p-Me-Ph H H CH 3 Bz H CH 3 OH OH H H NH 2 11-46-3 p-Me-Ph H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-46-4 p-Me-Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-46-5 p-Me-Ph H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 11-46-8 p-Me-Ph * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-47. N9 Rl R 2 R 3a R 3b R4 R R X Y R7 R' R9 11-47-1 p-F-Ph H H H Bz H CH 3 OH OH H H NH 2 11-47-2 p-F-Ph H H CH 3 Bz H CH 3 OH OH H H NH 2 11-47-3 p-F-Ph H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2

O2

N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 11-47-4 p-F-Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-47-5 p-F-Ph H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-47-7 p-F-Ph H H CH 2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 11-47-8 p-F-Ph * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 11-48. N9 Rl R 2 R 3 a R 3b R4 R 5 R6 X Y R7 R' R9 11-48-1 p-Cl-Ph H H H Bz H CH 3 OH OH H H NH 2 11-48-2 p-Cl-Ph H H CH3 Bz H CH 3 OH OH H H NH 2 11-48-3 p-Cl-Ph H H CH(CH 3) 2 Bz H CH 3 OH OH H H NH 2 11-48-4 p-Cl-Ph H H CH2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-48-5 p-Cl-Ph H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 11-48-8 p-Cl-Ph * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 11-49. N9 Rl R2 R3a R3 b R4 R5 R6 X Y R7 R' R9 11-49-1 p-Br-Ph H H H Bz H CH 3 OH OH H H NH 2 11-49-2 p-Br-Ph H H CH 3 Bz H CH 3 OH OH H H NH 2 11-49-3 p-Br-Ph H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz H CH 3 OH OH H H NH 2 11-49-5 p-Br-Ph H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2 11-49-7 p-Br-Ph H H CH 2CH 2 SCH3 Bz H CH 3 OH OH H H NH 2 11-49-8 p-Br-Ph * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 11-50. N9 Rl R 2 R 3 a R 3b R4 R R X Y R7 R' R9 11-50-1 p-I-Ph H H H Bz H CH 3 OH OH H H NH 2 11-50-2 p-I-Ph H H CH 3 Bz H CH 3 OH OH H H NH 2 11-50-3 p-I-Ph H H CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-50-4 p-I-Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H NH 2 11-50-5 p-I-Ph H H CH 2Ph Bz H CH 3 OH OH H H NH 2 11-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H NH 2

00_

N9 Rl R 2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 11-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz H CH 3 OH OH H H NH 2 11-50-8 p-I-Ph * H * Bz H CH 3 OH OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

R9

R8

R2 0 R3b R R N'l 0 N P 0 N--P--OO0 R

CO2R4 OR 1 R5 R6

Y X III

Table 111-1. N9 R R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 III-1-1 CH 3 H H H CH 3 H CH3 F OH H H NH 2 111-1-2 CH 3 H H CH 3 CH 3 H CH 3 F OH H H NH 2 111-1-3 CH 3 H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-1-4 CH 3 H H CH 2CH(CH 3)2 CH 3 H CH 3 F OH H H NH 2 111-1-5 CH 3 H H CH 2Ph CH 3 H CH 3 F OH H H NH 2 111-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-1-7 CH 3 H H CH 2CH2SCH 3 CH 3 H CH 3 F OH H H NH 2 III-1-8 CH 3 * H * CH 3 H CH3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-2. N9 Rl R2 R3a RS R4 R5 R6 X Y R7 R' R9 111-2-1 Et H H H CH 3 H CH3 F OH H H NH 2 111-2-2 Et H H CH3 CH 3 H CH 3 F OH H H NH 2 111-2-3 Et H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-2-4 Et H H CH2CH(CH 3) 2 CH 3 H CH 3 F OH H H NH 2 111-2-5 Et H H CH 2Ph CH 3 H CH 3 F OH H H NH 2 111-2-6 Et H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-2-7 Et H H CH2CH2SCH 3 CH 3 H CH 3 F OH H H NH 2 III-2-8 Et * H * CH 3 H CH3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Sn

Table 111-3. N9 R1 R2 R 3 a R 3b R4 R 5 R' X Y R7 R' R9 III-3-1 tPr H H H CH3 H CH3 F OH H H NH 2 111-3-2 'Pr H H CH 3 CH 3 H CH 3 F OH H H NH 2 111-3-3 'Pr H H CH(CH3) 2 CH3 H CH 3 F OH H H NH 2 111-3-4 Pr H H CH 2CH(CH3) 2 CH3 H CH 3 F OH H H NH 2 111-3-5 Pr H H CH 2Ph CH3 H CH 3 F OH H H NH 2 111-3-6 Pr H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-3-7 Pr H H CH 2CH 2SCH 3 CH3 H CH 3 F OH H H NH 2 III-3-8 Pr * H * CH 3 H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-4. R3a No R1 R2 R 3b R4 R 5 R6 X Y R7 R' R9 III-4-1 'Bu H H H CH3 H CH3 F OH H H NH 2 111-4-2 'Bu H H CH3 CH3 H CH 3 F OH H H NH 2 111-4-3 'Bu H H CH(CH3) 2 CH3 H CH 3 F OH H H NH 2 111-4-4 'Bu H H CH2CH(CH3) 2 CH3 H CH 3 F OH H H NH 2 111-4-5 'Bu H H CH 2Ph CH3 H CH 3 F OH H H NH 2 111-4-6 'Bu H H CH 2-indol-3-yl CH3 H CH 3 F OH H H NH 2 111-4-7 'Bu H H CH2CH 2SCH 3 CH3 H CH 3 F OH H H NH 2 III-4-8 'Bu * H * CH 3 H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-5. N9 R R2 R 3a R 3b R4 R5 R6 X Y R7 R' R9

III-5-1 Ph H H H CH3 H CH3 F OH H H NH 2 111-5-2 Ph H H CH 3 CH3 H CH 3 F OH H H NH 2 111-5-3 Ph H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-5-4 Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-5-5 Ph H H CH 2Ph CH3 H CH 3 F OH H H NH 2 111-5-6 Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-5-7 Ph H H CH 2CH2SCH 3 CH 3 H CH 3 F OH H H NH 2 III-5-8 Ph * H * CH3 H CH3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1M

Table 111-6. N9 R1 R 2 R 3a R 3b R4 R R6 X Y R7 R' R9 111-6-1 p-Me-Ph H H H CH3 H CH 3 F OH H H NH 2 111-6-2 p-Me-Ph H H CH 3 CH3 H CH 3 F OH H H NH 2 111-6-3 p-Me-Ph H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-6-4 p-Me-Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-6-5 p-Me-Ph H H CH 2Ph CH3 H CH 3 F OH H H NH 2 111-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH 3 H CH 3 F OH H H NH 2 111-6-8 p-Me-Ph * H * CH3 H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-7. R3a N9 R1 R2 R 3b R4 R R6 X Y R7 R' R9 111-7-1 p-F-Ph H H H CH3 H CH 3 F OH H H NH 2 111-7-2 p-F-Ph H H CH 3 CH3 H CH 3 F OH H H NH 2 111-7-3 p-F-Ph H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-7-4 p-F-Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-7-6 p-F-Ph H H CH 2Ph CH3 H CH 3 F OH H H NH 2 111-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-7-8 p-F-Ph H H CH 2CH2SCH 3 CH 3 H CH 3 F OH H H NH 2 111-7-20 p-F-Ph * H * CH3 H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-8. N9 R1 R 2 R 3 a R 3b R4 R5 R6 X Y R7 R' R9 111-8-1 p-Cl-Ph H H H CH3 H CH 3 F OH H H NH 2 111-8-2 p-Cl-Ph H H CH3 CH3 H CH 3 F OH H H NH 2 111-8-3 p-Cl-Ph H H CH(CH 3) 2 CH3 H CH 3 F OH H H NH 2 111-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH H H NH 2 111-8-5 p-Cl-Ph H H CH 2Ph CH3 H CH 3 F OH H H NH 2 111-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH H H NH 2 111-8-7 p-Cl-Ph H H CH2CH 2SCH3 CH3 H CH 3 F OH H H NH 2 111-8-8 p-Cl-Ph * H * CH3 H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-9. N9 R1 R 2 R3 a RS R4 R5 R6 X Y R7 R' R9 111-9-1 p-Br-Ph H H H CH 3 H CH 3 F OH H H NH 2 111-9-2 p-Br-Ph H H CH 3 CH 3 H CH3 F OH H H NH 2 111-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H CH3 F OH H H NH 2

_1CV)_

N9 Rl R2 R3 a R3 b R4 R' R' X Y R7 R' R9 111-9-4 p-Br-Ph H H CH 2CH(CH 3) 2 CH 3 H CH 3 F OH H H NH 2 111-9-6 p-Br-Ph H H CH 2Ph CH 3 H CH 3 F OH H H NH 2 111-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 F OH H H NH 2 111-9-20 p-Br-Ph * H * CH 3 H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-10. N9 Rl R2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 111-10-1 p-I-Ph H H H CH 3 H CH 3 F OH H H NH 2 111-10-2 p-I-Ph H H CH 3 CH 3 H CH 3 F OH H H NH 2 111-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-10-4 p-I-Ph H H CH 2CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 111-10-5 p-I-Ph H H CH 2Ph CH 3 H CH 3 F OH H H NH 2 111-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 111-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 F OH H H NH 2 111-10-8 p-I-Ph * H * CH 3 H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-11. No R1 R2 R3a R3 b R4 R' R6 X Y R7 R' R9 III-11-1 CH3 H H H Et H CH3 F OH H H NH 2 111-11-2 CH3 H H CH 3 Et H CH 3 F OH H H NH 2 111-11-3 CH3 H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-11-4 CH3 H H CH 2CH(CH 3) 2 Et H CH 3 F OH H H NH 2 111-11-5 CH3 H H CH 2Ph Et H CH 3 F OH H H NH 2 111-11-6 CH3 H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-11-7 CH3 H H CH 2CH2SCH 3 Et H CH 3 F OH H H NH 2 III-11-8 CH3 * H * EtH CH3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-12. N9 Rl R 2 R3 a R3b R4 R R6 X Y R7 R' R9 III-12-1 Et H H H Et H CH3 F OH H H NH 2 111-12-2 Et H H CH3 Et H CH 3 F OH H H NH 2 111-12-3 Et H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-12-4 Et H H CH2CH(CH 3) 2 Et H CH 3 F OH H H NH 2 111-12-5 Et H H CH 2Ph Et H CH 3 F OH H H NH 2 111-12-6 Et H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2

1 _),1

N9 Rl R 2 R3 a R3 b R4 R' R' X Y R7 R' R9 111-12-7 Et H H CH2CH2SCH 3 Et H CH 3 F OH H H NH 2 III-12-8 Et * H * Et H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-13. No9 R R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 III-13-1 'Pr H H H Et H CH3 F OH H H NH 2 111-13-2 'Pr H H CH3 Et H CH 3 F OH H H NH 2 111-13-3 'Pr H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-13-4 'Pr H H CH2CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-13-5 'Pr H H CH 2Ph Et H CH 3 F OH H H NH 2 111-13-6 'Pr H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-13-7 'Pr H H CH2CH 2SCH 3 Et H CH 3 F OH H H NH 2 III-13-8 'Pr * H * FtH CH3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-14. No R R2 R R3b R4 R5 R6 X Y R7 R' R9 3a

111-14- 'Bu H H H Et H CH 3 F OH H H NH 2 1 111-14- 'Bu H H CH 3 Et H CH 3 F OH H H NH 2 2 111-14- 'Bu H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 3 111-14- 'Bu H H CH 2CH(CH 3) 2 Et H CH 3 F OH H H NH 2 4 111-14- 'Bu H H CH 2Ph Et H CH 3 F OH H H NH 2 5 111-14- 'Bu H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 6 111-14- 'Bu H H CH 2CH2SCH 3 Et H CH 3 F OH H H NH 2 7 III-14- 'Bu* H * EtH CH 3 F OH H H NH 2 8 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-15. No9 R R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9

1 A

R R2 R3 a R3 b R4 R5 R' X Y R7 R' R9 No9 III-15-1 Ph H H H Et H CH 3 F OH H H NH 2 111-15-2 Ph H H CH 3 Et H CH 3 F OH H H NH 2 111-15-3 Ph H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-15-4 Ph H H CH 2CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-15-5 Ph H H CH 2Ph Et H CH 3 F OH H H NH 2 111-15-6 Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-15-7 Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH H H NH 2 III-15-8 Ph * H * FtH CH 3 F OH H H NH 2 *R and2 R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-16. N Rl R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 111-16-1 p-Me-Ph H H H Et H CH 3 F OH H H NH 2 111-16-2 p-Me-Ph H H CH 3 Et H CH 3 F OH H H NH 2 111-16-3 p-Me-Ph H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-16-4 p-Me-Ph H H CH 2CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-16-5 p-Me-Ph H H CH 2Ph Et H CH 3 F OH H H NH 2 111-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH H H NH 2 111-16-8 p-Me-Ph * H * Et H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-17. N9 Rl R2 R 3a R3 b R4 R R6 X Y R7 R' R9 111-17-1 p-F-Ph H H H Et H CH 3 F OH H H NH 2 111-17-2 p-F-Ph H H CH 3 Et H CH 3 F OH H H NH 2 111-17-3 p-F-Ph H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-17-4 p-F-Ph H H CH 2CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-17-5 p-F-Ph H H CH 2Ph Et H CH 3 F OH H H NH 2 111-17-6 p-F-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH H H NH 2 111-17-8 p-F-Ph * H * Et H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-18. N Rl R2 R 3a R3b R4 R5 R6 X Y R7 R' R9 111-18-1 p-Cl-Ph H H H Et H CH 3 F OH H H NH 2 111-18-2 p-Cl-Ph H H CH3 Et H CH 3 F OH H H NH 2 111-18-3 p-Cl-Ph H H CH(CH 3)2 Et H CH 3 F OH H H NH 2

_ () _

N Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 111-18-4 p-Cl-Ph H H CH2CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-18-5 p-Cl-Ph H H CH 2Ph Et H CH 3 F OH H H NH 2 111-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-18-7 p-Cl-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH H H NH 2 111-18-8 p-Cl-Ph * H * Et H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-19. N9 Rl R2 R3 a R3 R4 R' R6 X Y R7 R' R9 111-19-1 p-Br-Ph H H H Et H CH 3 F OH H H NH 2 111-19-2 p-Br-Ph H H CH 3 Et H CH 3 F OH H H NH 2 111-19-3 p-Br-Ph H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-19-4 p-Br-Ph H H CH 2CH(CH 3) 2 Et H CH 3 F OH H H NH 2 111-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 F OH H H NH 2 111-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH H H NH 2 111-19-8 p-Br-Ph * H * Et H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-20. N9 Rl R2 R3a R3 b R4 R5 R6 X Y R7 R' R9 111-20-1 p-I-Ph H H H Et H CH 3 F OH H H NH 2 111-20-2 p-I-Ph H H CH 3 Et H CH 3 F OH H H NH 2 111-20-3 p-I-Ph H H CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-20-4 p-I-Ph H H CH 2CH(CH3) 2 Et H CH 3 F OH H H NH 2 111-20-5 p-I-Ph H H CH 2Ph Et H CH 3 F OH H H NH 2 111-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H NH 2 111-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH H H NH 2 111-20-8 p-I-Ph * H * Et H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 111-21. No9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 111-21-1 CH3 H H H 'Pr H CH 3 F OH H H NH 2 111-21-2 CH3 H H CH 3 'Pr H CH 3 F OH H H NH 2 111-21-3 CH3 H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-21-4 CH3 H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH H H NH 2 111-21-5 CH3 H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-21-6 CH3 H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2

1( _ -r

No9 R R2 R3 a R3 b R4 R5 R' X Y R7 R' R9 111-21-7 CH3 H H CH 2CH2SCH 3 'Pr H CH 3 F OH H H NH 2 111-21-8 CH3 * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-22. N9 Rl R 2 R3 a RS R4 R R' X Y R7 R' R9 111-22-1 Et H H H 'Pr H CH 3 F OH H H NH 2 111-22-2 Et H H CH3 'Pr H CH 3 F OH H H NH 2 111-22-3 Et H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-22-4 Et H H CH2CH(CH 3) 2 'Pr H CH 3 F OH H H NH 2 111-22-5 Et H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-22-6 Et H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-22-7 Et H H CH2CH2SCH 3 'Pr H CH 3 F OH H H NH 2 III-22-8 Et * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-23. No9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 111-23-1 'Pr H H H 'Pr H CH 3 F OH H H NH 2 111-23-2 Pr H H CH3 'Pr H CH 3 F OH H H NH 2 111-23-3 'Pr H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-23-4 'Pr H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-23-5 'Pr H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-23-6 'Pr H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-23-7 'Pr H H CH2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 111-23-8 Pr * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-24. No9 R R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 111-24-1 'Bu H H H 'Pr H CH 3 F OH H H NH 2 111-24-2 'Bu H H CH3 'Pr H CH 3 F OH H H NH 2 111-24-3 'Bu H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-24-4 'Bu H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-24-5 'Bu H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-24-6 'Bu H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-24-7 'Bu H H CH2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 111-24-8 'Bu * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1(Y7_

Table 111-25. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 III-25-1 Ph H H H 'Pr H CH 3 F OH H H NH 2 111-25-2 Ph H H CH 3 'Pr H CH 3 F OH H H NH 2 111-25-3 Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-25-4 Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-25-5 Ph H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-25-7 Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 III-25-8 Ph * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 111-26. N9 R1 R 2 R 3 a R3 b R4 R5 R6 X Y R7 R' R9 111-26-1 p-Me-Ph H H H 'Pr H CH 3 F OH H H NH 2 111-26-2 p-Me-Ph H H CH 3 'Pr H CH 3 F OH H H NH 2 111-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-26-4 p-Me-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-26-7 p-Me-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 111-26-8 p-Me-Ph * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-27. N9 R1 R 2 R 3a R 3b R4 R R X Y R7 R' R9 111-27-1 p-F-Ph H H H 'Pr H CH 3 F OH H H NH 2 111-27-2 p-F-Ph H H CH 3 'Pr H CH 3 F OH H H NH 2 111-27-3 p-F-Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-27-4 p-F-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-27-5 p-F-Ph H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH H H NH 2 111-27-8 p-F-Ph * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-28. N R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 111-28-1 p-Cl-Ph H H H 'Pr H CH3 F OH H H NH 2 111-28-2 p-Cl-Ph H H CH3 'Pr H CH3 F OH H H NH 2 111-28-3 p-Cl-Ph H H CH(CH 3)2 'Pr H CH3 F OH H H NH 2

_l1l2-

R2 R 3a R3 b R4 R' R' R' R9 N9 Rl X Y R7 111-28-4 p-Cl-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-28-5 p-Cl-Ph H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 111-28-8 p-Cl-Ph * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table 111-29. N9 Rl R2 R3 a R3 R4 R5 R6 X Y R7 R' R9 111-29-1 p-Br-Ph H H H 'Pr H CH 3 F OH H H NH 2 111-29-2 p-Br-Ph H H CH 3 'Pr H CH 3 F OH H H NH 2 111-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-29-4 p-Br-Ph H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH H H NH 2 111-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 111-29-8 p-Br-Ph * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-30. N9 Rl R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 111-30-1 p-I-Ph H H H 'Pr H CH 3 F OH H H NH 2 111-30-2 p-I-Ph H H CH 3 'Pr H CH 3 F OH H H NH 2 111-30-3 p-I-Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-30-4 p-I-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH H H NH 2 111-30-5 p-I-Ph H H CH 2Ph 'Pr H CH 3 F OH H H NH 2 111-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H NH 2 111-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH H H NH 2 111-30-8 p-I-Ph * H * 'Pr H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 111-31. No R R2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 111-31-1 CH3 H H H "Bu H CH 3 F OH H H NH 2 111-31-2 CH3 H H CH 3 "Bu H CH 3 F OH H H NH 2 111-31-3 CH3 H H CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-31-4 CH3 H H CH 2CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-31-5 CH3 H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-31-6 CH3 H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2

_ O1

N9 R R2 R3 a R3 b R4 R' R' X Y R7 R' R9 111-31-7 CH3 H H CH 2CH2SCH 3 "Bu H CH 3 F OH H H NH 2 111-31-8 CH3 * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-32. N9 Rl R 2 R3 a R R4 R' R' X Y R7 R' R9 111-32-1 Et H H H "Bu H CH3 F OH H H NH 2 111-32-2 Et H H CH3 "Bu H CH 3 F OH H H NH 2 111-32-3 Et H H CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-32-4 Et H H CH2CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-32-5 Et H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-32-6 Et H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-32-7 Et H H CH2CH2SCH 3 "Bu H CH 3 F OH H H NH 2 III-32-8 Et * H * "Bu H CH3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-33. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R R9 111-33-1 'Pr H H H "Bu H CH 3 F OH H H NH 2 111-33-2 Pr H H CH3 "Bu H CH 3 F OH H H NH 2 111-33-3 'Pr H H CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-33-4 'Pr H H CH2CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-33-5 'Pr H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-33-6 'Pr H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-33-7 'Pr H H CH2CH 2SCH 3 "Bu H CH 3 F OH H H NH 2 111-33-8 Pr * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1 1t

Table 111-34. N9 R1 R2 R 3a R 3b R4 R' R6 X Y R7 R' R9 111-34-1 'Bu H H H "Bu H CH 3 F OH H H NH 2 111-34-2 'Bu H H CH3 "Bu H CH 3 F OH H H NH 2 111-34-3 'Bu H H CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-34-4 'Bu H H CH2CH(CH 3)2 "Bu H CH 3 F OH H H NH 2 111-34-5 'Bu H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-34-6 'Bu H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-34-7 'Bu H H CH2CH 2SCH 3 "Bu H CH 3 F OH H H NH 2 111-34-8 'Bu * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-35. No R1 R2 R3a R3b R4 R 5 R6 X Y R7 R' R9 III-35-1 Ph H H H "Bu H CH 3 F OH H H NH 2 111-35-2 Ph H H CH 3 "Bu H CH 3 F OH H H NH 2 111-35-3 Ph H H CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-35-4 Ph H H CH 2CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-35-5 Ph H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-35-6 Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-35-7 Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH H H NH 2 III-35-8 Ph * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-36. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 111-36-1 p-Me-Ph H H H "Bu H CH 3 F OH H H NH 2 111-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 F OH H H NH 2 111-36-3 p-Me-Ph H H CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH H H NH 2 111-36-8 p-Me-Ph * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table 111-37. N9 R1 R2 R 3aRb R4 R5 R6 X Y R7 R' R9 111-37-1 p-F-Ph H H H "Bu H CH 3 F OH H H NH 2 111-37-2 p-F-Ph H H CH 3 "Bu H CH 3 F OH H H NH 2 111-37-3 p-F-Ph H H CH(CH3) 2 "Bu H CH 3 F OH H H NH 2

N9 Rl R2 R 3 a Rb R4 R5 R' X Y R7 R' R9 111-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-37-5 p-F-Ph H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH H H NH 2 111-37-8 p-F-Ph * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-38. N9 Rl R2 R 3a R3b R4 R' R6 X Y R7 R' R9 111-38-1 p-Cl-Ph H H H "Bu H CH 3 F OH H H NH 2 111-38-2 p-Cl-Ph H H CH3 "Bu H CH 3 F OH H H NH 2 111-38-3 p-Cl-Ph H H CH(CH 3 )2 "Bu H CH 3 F OH H H NH 2 111-38-4 p-Cl-Ph H H CH2 CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-38-5 p-Cl-Ph H H CH 2 Ph "Bu H CH 3 F OH H H NH 2 111-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 F OH H H NH 2 111-38-8 p-Cl-Ph * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 111-39. N Rl R2 R 3 a R R4 R' R6 X Y R7 R' R9 111-39-1 p-Br-Ph H H H "Bu H CH 3 F OH H H NH 2 111-39-2 p-Br-Ph H H CH 3 "Bu H CH 3 F OH H H NH 2 111-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-39-4 p-Br-Ph H H CH 2 CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-39-5 p-Br-Ph H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2 111-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH H H NH 2 111-39-8 p-Br-Ph * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 111-40. N9 Rl R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 111-40-1 p-I-Ph H H H "Bu H CH 3 F OH H H NH 2 111-40-2 p-I-Ph H H CH 3 "Bu H CH 3 F OH H H NH 2 111-40-3 p-I-Ph H H CH(CH 3) 2 "Bu H CH 3 F OH H H NH 2 111-40-4 p-I-Ph H H CH 2CH(CH3) 2 "Bu H CH 3 F OH H H NH 2 111-40-5 p-I-Ph H H CH 2Ph "Bu H CH 3 F OH H H NH 2 111-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H NH 2

11)

N9 R1 R2 R3 a R3 b R4 R 5 R' X Y R7 R' R9 111-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH H H NH 2 111-40-8 p-I-Ph * H * "Bu H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-41. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 III-41-1 CH3 H H H Bz H CH3 F OH H H NH 2 111-41-2 CH3 H H CH 3 Bz H CH 3 F OH H H NH 2 111-41-3 CH3 H H CH(CH3) 2 Bz H CH 3 F OH H H NH 2 111-41-4 CH3 H H CH 2CH(CH 3) 2 Bz H CH 3 F OH H H NH 2 111-41-5 CH3 H H CH 2Ph Bz H CH 3 F OH H H NH 2 111-41-6 CH3 H H CH 2-indol-3-yl Bz H CH 3 F OH H H NH 2 111-41-7 CH3 H H CH 2CH2SCH 3 Bz H CH 3 F OH H H NH 2 III-41-8 CH3 * H * Bz H CH3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-42. N9 Rl R 2 R3 a R R4 R' R6 X Y R7 R' R9 111-42-1 Et H H H Bz H CH3 F OH H H NH 2 111-42-2 Et H H CH3 Bz H CH 3 F OH H H NH 2 111-42-3 Et H H CH(CH3) 2 Bz H CH 3 F OH H H NH 2 111-42-4 Et H H CH2CH(CH 3) 2 Bz H CH 3 F OH H H NH 2 111-42-5 Et H H CH 2Ph Bz H CH 3 F OH H H NH 2 111-42-6 Et H H CH 2-indol-3-yl Bz H CH 3 F OH H H NH 2 111-42-7 Et H H CH2CH2SCH 3 Bz H CH 3 F OH H H NH 2 III-42-8 Et * H * Bz H CH3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-43. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 *R2 and 111-43-1 'Pr H H H Bz H CH 3 F OH H H NH 2 R3 b joined 111-43-2 'Pr H H CH3 Bz H CH 3 F OH H H NH 2 together 111-43-3 'Pr H H CH(CH3) 2 Bz H CH 3 F OH H H N2 by (CH2)3 111-43-4 'Pr H H CH2CH(CH3) 2 Bz H CH 3 F OH H H NH 2 to form 111-43-5 'Pr H H CH 2Ph Bz H CH 3 F OH H H NH 2 five 111-43-6 'Pr H H CH 2-indol-3-yl Bz H CH 3 F OH H H NH 2 membered 111-43-7 'Pr H H CH2CH 2SCH 3 Bz H CH 3 F OH H H NH 2 111-43-8 Pr * H * Bz H CH 3 F OH H H NH 2 ring.

Table 111-44.

_1 1'2-

R R2 R 3a R3 b R4 R' R' X Y R7 R' R9 No9 III-44-1 'Bu H H H Bz H CH3 F OH H H NH 2 111-44-2 'Bu H H CH3 Bz H CH 3 F OH H H NH 2 111-44-3 'Bu H H CH(CH3) 2 Bz H CH 3 F OH H H NH 2 111-44-4 'Bu H H CH2CH(CH3) 2 Bz H CH 3 F OH H H NH 2 111-44-5 'Bu H H CH 2Ph Bz H CH 3 F OH H H NH 2 111-44-6 'Bu H H CH 2-indol-3-yl Bz H CH 3 F OH H H NH 2 111-44-7 'Bu H H CH2CH 2SCH 3 Bz H CH 3 F OH H H NH 2 III-44-8 'Bu * H * Bz H CH3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1 1 /

Table 111-45. R1 R2 R3 a R3b R4 R5 R' X Y R7 R' R9 N9 III-45-1 Ph H H H Bz H CH3 F OH H H NH 2 111-45-2 Ph H H CH 3 Bz H CH3 F OH H H NH 2 111-45-3 Ph H H CH(CH 3) 2 Bz H CH3 F OH H H NH 2 111-45-4 Ph H H CH 2CH(CH3) 2 Bz H CH3 F OH H H NH 2 111-45-5 Ph H H CH 2Ph Bz H CH3 F OH H H NH 2 111-45-6 Ph H H CH 2-indol-3-yl Bz H CH3 F OH H H NH 2 111-45-7 Ph H H CH 2CH 2SCH 3 Bz H CH3 F OH H H NH 2 III-45-8 Ph * H * Bz H CH3 F OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table 111-46. N9 R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 111-46-1 p-Me-Ph H H H Bz H CH3 F OH H H NH 2 111-46-2 p-Me-Ph H H CH 3 Bz H CH3 F OH H H NH 2 111-46-3 p-Me-Ph H H CH(CH3) 2 Bz H CH3 F OH H H NH 2 111-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz H CH3 F OH H H NH 2 111-46-5 p-Me-Ph H H CH 2Ph Bz H CH3 F OH H H NH 2 111-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH3 F OH H H NH 2 111-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H CH3 F OH H H NH 2 111-46-8 p-Me-Ph * H * Bz H CH3 F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table 111-47. N9 R1 R 2 R 3a R 3b R4 R 5 R6 X Y R7 R' R9 111-47-1 p-F-Ph H H H Bz H CH3 F OH H H NH 2 111-47-2 p-F-Ph H H CH 3 Bz H CH3 F OH H H NH 2 111-47-3 p-F-Ph H H CH(CH3) 2 Bz H CH3 F OH H H NH 2 111-47-4 p-F-Ph H H CH 2CH(CH3) 2 Bz H CH3 F OH H H NH 2 111-47-5 p-F-Ph H H CH 2Ph Bz H CH3 F OH H H NH 2 111-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H CH3 F OH H H NH 2 111-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz H CH3 F OH H H NH 2 111-47-8 p-F-Ph * H * Bz H CH3 F OH H H NH 2 *R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

Table 111-48. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 111-48-1 p-Cl-Ph H H H Bz H CH 3 F OH H H NH 2 111-48-2 p-Cl-Ph H H CH3 Bz H CH 3 F OH H H NH 2 111-48-3 p-Cl-Ph H H CH(CH 3)2 Bz H CH 3 F OH H H NH 2

_11;-

No Rl R2 R 3a R3 b R4 R5 R' X Y R7 R' R9 111-48-4 p-Cl-Ph H H CH2CH(CH3) 2 Bz H CH 3 F OH H H NH 2 111-48-5 p-Cl-Ph H H CH 2Ph Bz H CH 3 F OH H H NH 2 111-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H NH 2 111-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH H H NH 2 111-48-8 p-Cl-Ph * H * Bz H CH 3 F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

11 _

Table 111-49. N9 Rl R2 R3 a R3 R4 R R6 X Y R7 R' R9 111-49-1 p-Br-Ph H H H Bz H CH 3 F OH H H NH 2 111-49-2 p-Br-Ph H H CH 3 Bz H CH 3 F OH H H NH 2 111-49-3 p-Br-Ph H H CH(CH 3) 2 Bz H CH 3 F OH H H NH 2 111-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz H CH 3 F OH H H NH 2 111-49-5 p-Br-Ph H H CH 2Ph Bz H CH 3 F OH H H NH 2 111-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H NH 2 111-49-7 p-Br-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH H H NH 2 111-49-8 p-Br-Ph * H * Bz H CH 3 F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table 111-50. N9 Rl R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 111-50-1 p-I-Ph H H H Bz H CH3 F OH H H NH 2 111-50-2 p-I-Ph H H CH 3 Bz H CH3 F OH H H NH 2 111-50-3 p-I-Ph H H CH(CH 3) 2 Bz H CH3 F OH H H NH 2 111-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz H CH3 F OH H H NH 2 111-50-5 p-I-Ph H H CH 2Ph Bz H CH3 F OH H H NH 2 111-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH3 F OH H H NH 2 111-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz H CH3 F OH H H NH 2 111-50-8 p-I-Ph * H * Bz H CH3 F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

R9

R8

0N 3 R b R2 O R7 N 0 14 P1 0 0

CO2 R 4 OR' R5OR6

Y X IV

Table IV-1. No R R2 R3a R3b R4 R5 R 6 X Y R7 R' R9 IV-1-1 CH3 H H H CH3 H F F OH H H NH 2 IV-1-2 CH3 H H CH3 CH 3 H F F OH H H NH 2

S117

No9 R R2 R3 a R3 b R4 R 5 R' X Y R7 R' R9 IV-1-3 CH3 H H CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-1-4 CH3 H H CH2CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-1-5 CH3 H H CH 2Ph CH 3 H F F OH H H NH 2 IV-1-6 CH3 H H CH 2-indol-3-yl CH 3 H F F OH H H NH 2 IV-1-7 CH3 H H CH2CH 2SCH 3 CH 3 H F F OH H H NH 2 IV-1-8 CH3 * H * CH 3 H F F OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table IV-2. N9 Rl R 2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 IV-2-1 Et H H H CH 3 H F F OH H H NH 2 IV-2-2 Et H H CH 3 CH 3 H F F OH H H NH 2 IV-2-3 Et H H CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-2-4 Et H H CH 2CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-2-5 Et H H CH 2Ph CH 3 H F F OH H H NH 2 IV-2-6 Et H H CH 2-indol-3-yl CH 3 H F F OH H H NH 2 IV-2-7 Et H H CH 2CH 2SCH 3 CH 3 H F F OH H H NH 2 IV-2-8 Et * H * CH 3 H F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-3. No9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 IV-3-1 TPr H H H CH 3 H F F OH H H NH 2 IV-3-2 Pr H H CH 3 CH 3 H F F OH H H NH 2 IV-3-3 Pr H H CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-3-4 Pr H H CH 2CH(CH 3) 2 CH 3 H F F OH H H NH 2 IV-3-5 'Pr H H CH 2Ph CH 3 H F F OH H H NH 2 IV-3-6 'Pr H H CH 2-indol-3-yl CH 3 H F F OH H H NH 2 IV-3-7 'Pr H H CH 2CH2SCH 3 CH 3 H F F OH H H NH 2 IV-3-8 Pr * H * CH 3 H F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-4. N9 R R2 R 3a R3 R4 R5 R6 X Y R7 R' R9 IV-4-1 'Bu H H H CH 3 H CH 3 F OH H H NH 2 IV-4-2 'Bu H H CH 3 CH 3 H CH 3 F OH H H NH 2 IV-4-3 'Bu H H CH(CH3) 2 CH 3 H CH 3 F OH H H NH 2 IV-4-4 'Bu H H CH 2CH(CH 3)2 CH 3 H CH 3 F OH H H NH 2 IV-4-5 'Bu H H CH 2Ph CH 3 H CH 3 F OH H H NH 2

112 _

No9 R R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-4-6 'Bu H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H NH 2 IV-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H CH 3 F OH H H NH 2 IV-4-8 'Bu * H * CH 3 H CH3 F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-5. No9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 IV-5-1 Ph H H H CH 3 H F F OH H H NH 2 IV-5-2 Ph H H CH3 CH3 H F F OH H H NH 2 IV-5-3 Ph H H CH(CH 3) 2 CH3 H F F OH H H NH 2 IV-5-4 Ph H H CH2CH(CH3) 2 CH3 H F F OH H H NH 2 IV-5-5 Ph H H CH 2Ph CH 3 H F F OH H H NH 2 IV-5-6 Ph H H CH 2-indol-3-yl CH3 H F F OH H H NH 2 IV-5-7 Ph H H CH2CH 2SCH 3 CH3 H F F OH H H NH 2 IV-5-8 Ph * H * CH 3 H F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-6. N R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 IV-6-1 p-Me-Ph H H H CH 3 H F F OH H H NH 2 IV-6-2 p-Me-Ph H H CH3 CH3 H F F OH H H NH 2 IV-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 H F F OH H H NH 2 IV-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 H F F OH H H NH 2 IV-6-5 p-Me-Ph H H CH 2Ph CH 3 H F F OH H H NH 2 IV-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F F OH H H NH 2 IV-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H F F OH H H NH 2 IV-6-8 p-Me-Ph * H * CH 3 H F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-7. R2 R3 a R3b R4 5 6 X R' R9 N R1 R R Y R7 IV-7-1 p-F-Ph H H H CH 3 H F F OH H H NH 2 IV-7-2 p-F-Ph H H CH3 CH3 H F F OH H H NH 2 IV-7-3 p-F-Ph H H CH(CH 3) 2 CH3 H F F OH H H NH 2 IV-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H F F OH H H NH 2 IV-7-6 p-F-Ph H H CH 2Ph CH 3 H F F OH H H NH 2 IV-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F F OH H H NH 2 IV-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H F F OH H H NH 2 IV-7-20 p-F-Ph * H * CH 3 H F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-8. N9 R R2 R3 a R3 b R4 R R 6 X Y R7 R' R9 IV-8-1 p-Cl-Ph H H H CH 3 H F F OH H H NH 2 IV-8-2 p-Cl-Ph H H CH 3 CH 3 H F F OH H H NH 2 IV-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F F OH H H NH 2

1 _)

N9 Rl R 2 R3 a R3 b R4 R' R' X Y R7 R' R9 IV-8-4 p-Cl-Ph H H CH 2CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F F OH H H NH 2 IV-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F F OH H H NH 2 IV-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH 3 H F F OH H H NH 2 IV-8-8 p-Cl-Ph * H * CH 3 H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-9. N9 R R2 R 3a R 3b R4 R 5 R6 X Y R7 R' R9 IV-9-1 p-Br-Ph H H H CH 3 H F F OH H H NH 2 IV-9-2 p-Br-Ph H H CH3 CH 3 H F F OH H H NH 2 IV-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-9-6 p-Br-Ph H H CH 2Ph CH 3 H F F OH H H NH 2 IV-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H F F OH H H NH 2 IV-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 H F F OH H H NH 2 IV-9-20 p-Br-Ph * H * CH 3 H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-10. N9 Rl R 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-10-1 p-I-Ph H H H CH 3 H F F OH H H NH 2 IV-10-2 p-I-Ph H H CH 3 CH 3 H F F OH H H NH 2 IV-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H F F OH H H NH 2 IV-10-4 p-I-Ph H H CH 2CH(CH 3) 2 CH 3 H F F OH H H NH 2 IV-10-5 p-I-Ph H H CH 2Ph CH 3 H F F OH H H NH 2 IV-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H F F OH H H NH 2 IV-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H F F OH H H NH 2 IV-10-8 p-I-Ph * H * CH 3 H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-11. No9 R R2 R3a R 3b R4 R 5 R 6 X Y R7 R' R9 IV-11-1 CH 3 H H H Et H F F OH H H NH 2 IV-11-2 CH 3 H H CH3 Et H F F OH H H NH 2 IV-11-3 CH 3 H H CH(CH3) 2 Et H F F OH H H NH 2 IV-11-4 CH 3 H H CH2CH(CH3) 2 Et H F F OH H H NH 2 IV-11-5 CH 3 H H CH 2Ph Et H F F OH H H NH 2 IV-11-6 CH 3 H H CH 2-indol-3-yl Et H F F OH H H NH 2

_1 1

No9 R R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 IV-11-7 CH 3 H H CH2CH 2SCH 3 Et H F F OH H H NH 2 IV-11-8 CH 3 * H * Et H F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-12. N Rl RR 2 R 3a R3 b R4 R 5 R6 X Y R7 R' R9 IV-12-1 Et H H H Et H F F OH H H NH 2 IV-12-2 Et H H CH3 Et H F F OH H H NH 2 IV-12-3 Et H H CH(CH3) 2 Et H F F OH H H NH 2 IV-12-4 Et H H CH2CH(CH3) 2 Et H F F OH H H NH 2 IV-12-5 Et H H CH2Ph Et H F F OH H H NH 2 IV-12-6 Et H H CH2-indol-3-yl Et H F F OH H H NH 2 IV-12-7 Et H H CH2CH 2SCH 3 Et H F F OH H H NH 2 IV-12-8 Et * H * FtH F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-13. No9 R R2 R3a Rb R 4 R' R6 X Y R7 R' R9 IV-13-1 'Pr H H H Et H F F OH H H NH 2 IV-13-2 Pr H H CH 3 Et H F F OH H H NH 2 IV-13-3 Pr H H CH(CH3) 2 Et H F F OH H H NH 2 IV-13-4 Pr H H CH 2CH(CH 3) 2 Et H F F OH H H NH 2 IV-13-5 'Pr H H CH 2Ph Et H F F OH H H NH 2 IV-13-6 'Pr H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-13-7 'Pr H H CH 2CH2SCH 3 Et H F F OH H H NH 2 IV-13-8 Pr * H * FtH F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-14. No R R2 R R3b R4 R5 R6 X Y R7 R' R9 3a

IV-14- 'Bu H H H Et H F F OH H H NH 2 1 IV-14- 'Bu H H CH 3 Et H F F OH H H NH 2 2 IV-14- 'Bu H H CH(CH3) 2 Et H F F OH H H NH 2 3 IV-14- 'Bu H H CH 2CH(CH 3) 2 Et H F F OH H H NH 2

No R R2 R R3b R4 R' R6 X Y R7 R' R9 3a

IV-14- 'Bu H H CH 2Ph Et H F F OH H H NH 2 5 IV-14- 'Bu H H CH 2-indol-3-yl Et H F F OH H H NH 2 6 IV-14- 'Bu H H CH 2CH2SCH 3 Et H F F OH H H NH 2 7 IV-14- 'Bu* H * FtH F F OH H H NH 2 8 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-15. No R R 2 R 3 aR R4 R R6 X Y R7 R R9 IV-15-1 Ph H H H Et H F F OH H H NH 2 IV-15-2 Ph H H CH3 Et H F F OH H H NH 2 IV-15-3 Ph H H CH(CH 3)2 Et H F F OH H H NH 2 IV-15-4 Ph H H CH2CH(CH 3) 2 Et H F F OH H H NH 2 IV-15-5 Ph H H CH 2Ph Et H F F OH H H NH 2 IV-15-6 Ph H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-15-7 Ph H H CH2CH2SCH 3 Et H F F OH H H NH 2 IV-15-8 Ph * H * EtH F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-16. N9 Rl R2 R 3a R3 b R4 R 5 R6 X Y R7 R' R9 IV-16-1 p-Me-Ph H H H Et H F F OH H H NH 2 IV-16-2 p-Me-Ph H H CH 3 Et H F F OH H H NH 2 IV-16-3 p-Me-Ph H H CH(CH 3)2 Et H F F OH H H NH 2 IV-16-4 p-Me-Ph H H CH 2CH(CH 3) 2 Et H F F OH H H NH 2 IV-16-5 p-Me-Ph H H CH 2Ph Et H F F OH H H NH 2 IV-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H F F OH H H NH 2 IV-16-8 p-Me-Ph * H * Et H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-17. N9 Rl R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 IV-17-1 p-F-Ph H H H Et H F F OH H H NH 2 IV-17-2 p-F-Ph H H CH3 Et H F F OH H H NH 2

N9 Rl R2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 IV-17-3 p-F-Ph H H CH(CH 3) 2 Et H F F OH H H NH 2 IV-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H F F OH H H NH 2 IV-17-5 p-F-Ph H H CH 2Ph Et H F F OH H H NH 2 IV-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-17-7 p-F-Ph H H CH2CH 2SCH 3 Et H F F OH H H NH 2 IV-17-8 p-F-Ph * H * FtH F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-18. N9 Rl R2 R3 a R 3b R4 R R6 X Y R7 R' R9 IV-18-1 p-Cl-Ph H H H Et H F F OH H H NH 2 IV-18-2 p-Cl-Ph H H CH 3 Et H F F OH H H NH 2 IV-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F F OH H H NH 2 IV-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et H F F OH H H NH 2 IV-18-5 p-Cl-Ph H H CH 2Ph Et H F F OH H H NH 2 IV-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H F F OH H H NH 2 IV-18-8 p-Cl-Ph * H * Et H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-19. N9 Rl R2 R 3a R3 b R4 R 5 R6 X Y R7 R R9 IV-19-1 p-Br-Ph H H H Et H F F OH H H NH 2 IV-19-2 p-Br-Ph H H CH3 Et H F F OH H H NH 2 IV-19-3 p-Br-Ph H H CH(CH3) 2 Et H F F OH H H NH 2 IV-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H F F OH H H NH 2 IV-19-5 p-Br-Ph H H CH 2Ph Et H F F OH H H NH 2 IV-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H F F OH H H NH 2 IV-19-8 p-Br-Ph * H * FtH F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-20. N9 Rl R2 R 3a R3b R4 R 5 R6 X Y R7 R' R9 IV-20-1 p-I-Ph H H H Et H F F OH H H NH 2 IV-20-2 p-I-Ph H H CH 3 Et H F F OH H H NH 2 IV-20-3 p-I-Ph H H CH(CH3) 2 Et H F F OH H H NH 2 IV-20-4 p-I-Ph H H CH 2CH(CH 3) 2 Et H F F OH H H NH 2 IV-20-5 p-I-Ph H H CH 2Ph Et H F F OH H H NH 2

1 _A

N9 Rl R2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 IV-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F F OH H H NH 2 IV-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H F F OH H H NH 2 IV-20-8 p-I-Ph * H * Et H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-21. No9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 IV-21-1 CH 3 H H H 'Pr H F F OH H H NH 2 IV-21-2 CH 3 H H CH3 'Pr H F F OH H H NH 2 IV-21-3 CH 3 H H CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-21-4 CH 3 H H CH2CH(CH 3)2 'Pr H F F OH H H NH 2 IV-21-5 CH 3 H H CH 2Ph 'Pr H F F OH H H NH 2 IV-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H F F OH H H NH 2 IV-21-8 CH 3 * H * 'Pr H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-22. N Rl RR 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-22-1 Et H H H 'Pr H F F OH H H NH 2 IV-22-2 Et H H CH3 'Pr H F F OH H H NH 2 IV-22-3 Et H H CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-22-4 Et H H CH2CH(CH 3)2 'Pr H F F OH H H NH 2 IV-22-5 Et H H CH2Ph 'Pr H F F OH H H NH 2 IV-22-6 Et H H CH2-indol-3-yl 'Pr H F F OH H H NH 2 IV-22-7 Et H H CH2CH 2SCH 3 'Pr H F F OH H H NH 2 IV-22-8 Et * H * 'Pr H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-23. No9 R R2 R3a RS R4 R 5 R6 X Y R7 R' R9 IV-23-1 'Pr H H H 'Pr H F F OH H H NH 2 IV-23-2 'Pr H H CH 3 'Pr H F F OH H H NH 2 IV-23-3 'Pr H H CH(CH3) 2 'Pr H F F OH H H NH 2 IV-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-23-5 'Pr H H CH 2Ph 'Pr H F F OH H H NH 2 IV-23-6 'Pr H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-23-7 'Pr H H CH 2CH2SCH 3 'Pr H F F OH H H NH 2 IV-23-8 'Pr * H * 'Pr H F F OH H H NH2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1'M

Table IV-24. No9 R1 R2 R3 a R3 R4 R R' X Y R7 R' R9 IV-24-1 'Bu H H H 'Pr H F F OH H H NH 2 IV-24-2 'Bu H H CH 3 'Pr H F F OH H H NH 2 IV-24-3 'Bu H H CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-24-5 'Bu H H CH 2Ph 'Pr H F F OH H H NH 2 IV-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-24-7 'Bu H H CH 2CH2SCH 3 'Pr H F F OH H H NH 2 IV-24-8 'Bu * H * 'Pr H F F OH H H NH 2 *R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table IV-25. No9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 IV-25-1 Ph H H H 'Pr H F F OH H H NH 2 IV-25-2 Ph H H CH3 'Pr H F F OH H H NH 2 IV-25-3 Ph H H CH(CH 3)2 'Pr H F F OH H H NH 2 IV-25-4 Ph H H CH2CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-25-5 Ph H H CH 2Ph 'Pr H F F OH H H NH 2 IV-25-6 Ph H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-25-7 Ph H H CH2CH2SCH 3 'Pr H F F OH H H NH 2 IV-25-8 Ph * H * 'Pr H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-26. N9 R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' R9 IV-26-1 p-Me-Ph H H H 'Pr H F F OH H H NH 2 IV-26-2 p-Me-Ph H H CH 3 'Pr H F F OH H H NH 2 IV-26-3 p-Me-Ph H H CH(CH 3)2 'Pr H F F OH H H NH 2 IV-26-4 p-Me-Ph H H CH 2CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-26-5 p-Me-Ph H H CH 2Ph 'Pr H F F OH H H NH 2 IV-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H F F OH H H NH 2 IV-26-8 p-Me-Ph * H * 'Pr H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-27. N9 R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 IV-27-1 p-F-Ph H H H 'Pr H F F OH H H NH 2 IV-27-2 p-F-Ph H H CH3 'Pr H F F OH H H NH 2 IV-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H F F OH H H NH 2

1% _

N9 Rl R2 R3 a R3 b R4 R' R' X Y R7 R' R9 IV-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H F F OH H H NH 2 IV-27-5 p-F-Ph H H CH 2Ph 'Pr H F F OH H H NH 2 IV-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H F F OH H H NH 2 IV-27-8 p-F-Ph * H * 'Pr H F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-28. No9 Rl R2 R 3 R 3 b R4 R R X Y R7 R' R9 IV-28-1 p-Cl-Ph H H H 'Pr H F F OH H H NH 2 IV-28-2 p-Cl-Ph H H CH 3 'Pr H F F OH H H NH 2 IV-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F F OH H H NH 2 IV-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr H F F OH H H NH 2 IV-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F F OH H H NH 2 IV-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H F F OH H H NH 2 IV-28-8 p-Cl-Ph * H * 'Pr H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-29. No9 Rl R2 R 3 R3 b R4 R' R6 X Y R7 R' R9 IV-29-1 p-Br-Ph H H H 'Pr H F F OH H H NH 2 IV-29-2 p-Br-Ph H H CH3 'Pr H F F OH H H NH 2 IV-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F F OH H H NH 2 IV-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F F OH H H NH 2 IV-29-5 p-Br-Ph H H CH 2Ph 'Pr H F F OH H H NH 2 IV-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2 IV-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F F OH H H NH 2 IV-29-8 p-Br-Ph * H * 'Pr H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-30. N Rl R2 R 3a R 3b R4 R5 R 6 X Y R7 R' R9 IV-30-1 p-I-Ph H H H 'Pr H F F OH H H NH 2 IV-30-2 p-I-Ph H H CH 3 'Pr H F F OH H H NH 2 IV-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F F OH H H NH 2 IV-30-4 p-I-Ph H H CH 2CH(CH 3) 2 'Pr H F F OH H H NH 2 IV-30-5 p-I-Ph H H CH 2Ph 'Pr H F F OH H H NH 2 IV-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H NH 2

1T7

N9 Rl R2 R 3 a R3 b R4 R' R' X Y R7 R' R9 IV-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr H F F OH H H NH 2 IV-30-8 p-I-Ph * H * 'Pr H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-31. No9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 IV-31-1 CH 3 H H H "Bu H F F OH H H NH 2 IV-31-2 CH 3 H H CH3 "Bu H F F OH H H NH 2 IV-31-3 CH 3 H H CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-31-4 CH 3 H H CH2CH(CH 3)2 "Bu H F F OH H H NH 2 IV-31-5 CH 3 H H CH 2Ph "Bu H F F OH H H NH 2 IV-31-6 CH 3 H H CH 2-indol-3-yl "Bu H F F OH H H NH 2

IV-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H F F OH H H NH 2 IV-31-8 CH 3 * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-32. N Rl RR 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-32-1 Et H H H "Bu H F F OH H H NH 2 IV-32-2 Et H H CH3 "Bu H F F OH H H NH 2 IV-32-3 Et H H CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-32-4 Et H H CH2CH(CH 3)2 "Bu H F F OH H H NH 2 IV-32-5 Et H H CH2Ph "Bu H F F OH H H NH 2 IV-32-6 Et H H CH2-indol-3-yl "Bu H F F OH H H NH 2

IV-32-7 Et H H CH2CH 2SCH 3 "Bu H F F OH H H NH 2 IV-32-8 Et * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-33. No9 R R2 R3a RS R4 R 5 R6 X Y R7 R' R9 IV-33-1 'Pr H H H "Bu H F F OH H H NH 2 IV-33-2 'Pr H H CH 3 "Bu H F F OH H H NH 2 IV-33-3 'Pr H H CH(CH3) 2 "Bu H F F OH H H NH 2 IV-33-4 'Pr H H CH 2CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-33-5 'Pr H H CH 2Ph "Bu H F F OH H H NH 2 IV-33-6 'Pr H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-33-7 'Pr H H CH 2CH2SCH 3 "Bu H F F OH H H NH 2 IV-33-8 'Pr * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 1' _Q

Table IV-34. No9 R1 R2 R3 a R3 R4 R R X Y R7 R' R9 IV-34-1 'Bu H H H "Bu H F F OH H H NH 2 IV-34-2 'Bu H H CH 3 "Bu H F F OH H H NH 2 IV-34-3 'Bu H H CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-34-5 'Bu H H CH 2Ph "Bu H F F OH H H NH 2 IV-34-6 'Bu H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-34-7 'Bu H H CH 2CH2SCH 3 "Bu H F F OH H H NH 2 IV-34-8 'Bu * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-35. N R R 2 R 3 a RR R4 R R6 X Y R7 R R9 IV-35-1 Ph H H H "Bu H F F OH H H NH 2 IV-35-2 Ph H H CH3 "Bu H F F OH H H NH 2 IV-35-3 Ph H H CH(CH 3)2 "Bu H F F OH H H NH 2 IV-35-4 Ph H H CH2CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-35-5 Ph H H CH 2Ph "Bu H F F OH H H NH 2 IV-35-6 Ph H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-35-7 Ph H H CH2CH2SCH 3 "Bu H F F OH H H NH 2 IV-35-8 Ph * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-36. No9 R1 R2 R 3a R3b R4 R 5 R' X Y R7 R' R9 IV-36-1 p-Me-Ph H H H "Bu H F F OH H H NH 2 IV-36-2 p-Me-Ph H H CH 3 "Bu H F F OH H H NH 2 IV-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H F F OH H H NH 2 IV-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-36-5 p-Me-Ph H H CH 2Ph "Bu H F F OH H H NH 2 IV-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F F OH H H NH 2 IV-36-8 p-Me-Ph * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-37. N R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 IV-37-1 p-F-Ph H H H "Bu H F F OH H H NH 2 IV-37-2 p-F-Ph H H CH3 "Bu H F F OH H H NH 2 IV-37-3 p-F-Ph H H CH(CH 3) 2 "Bu H F F OH H H NH 2

110 _

N9 Rl R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 IV-37-4 p-F-Ph H H CH2CH(CH3) 2 "Bu H F F OH H H NH 2 IV-37-5 p-F-Ph H H CH 2Ph "Bu H F F OH H H NH 2 IV-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-37-7 p-F-Ph H H CH2CH 2SCH 3 "Bu H F F OH H H NH 2 IV-37-8 p-F-Ph * H * "Bu H F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-38. N9 Rl R2 R3 a R 3b R4 R R 6 X Y R7 R' R9 IV-38-1 p-Cl-Ph H H H "Bu H F F OH H H NH 2 IV-38-2 p-Cl-Ph H H CH 3 "Bu H F F OH H H NH 2 IV-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F F OH H H NH 2 IV-38-4 p-Cl-Ph H H CH 2CH(CH3) 2 "Bu H F F OH H H NH 2 IV-38-5 p-Cl-Ph H H CH 2Ph "Bu H F F OH H H NH 2 IV-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H F F OH H H NH 2 IV-38-8 p-Cl-Ph * H * "Bu H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-39. N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R R9 IV-39-1 p-Br-Ph H H H "Bu H F F OH H H NH 2 IV-39-2 p-Br-Ph H H CH3 "Bu H F F OH H H NH 2 IV-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H F F OH H H NH 2 IV-39-4 p-Br-Ph H H CH2 CH(CH3) 2 "Bu H F F OH H H NH 2 IV-39-5 p-Br-Ph H H CH 2 Ph "Bu H F F OH H H NH 2 IV-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F F OH H H NH 2 IV-39-7 p-Br-Ph H H CH2 CH 2 SCH 3 "Bu H F F OH H H NH 2 IV-39-8 p-Br-Ph * H * "Bu H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-40. N9 Rl R2 R 3a R3b R4 R 5 R6 X Y R7 R' R9 IV-40-1 p-I-Ph H H H "Bu H F F OH H H NH 2 IV-40-2 p-I-Ph H H CH 3 "Bu H F F OH H H NH 2 IV-40-3 p-I-Ph H H CH(CH3) 2 "Bu H F F OH H H NH 2 IV-40-4 p-I-Ph H H CH 2CH(CH 3) 2 "Bu H F F OH H H NH 2 IV-40-5 p-I-Ph H H CH 2Ph "Bu H F F OH H H NH 2 IV-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F F OH H H NH 2

1'2l

N9 R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H F F OH H H NH 2 IV-40-8 p-I-Ph * H * "Bu H F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-41. No9 R1 R2 R3 a R3 b R4 R' R' X Y R7 R' R9 IV-41-1 CH 3 H H H Bz H F F OH H H NH 2 IV-41-2 CH 3 H H CH3 Bz H F F OH H H NH 2 IV-41-3 CH 3 H H CH(CH3) 2 Bz H F F OH H H NH 2 IV-41-4 CH 3 H H CH2CH(CH3) 2 Bz H F F OH H H NH 2 IV-41-5 CH 3 H H CH 2Ph Bz H F F OH H H NH 2 IV-41-6 CH 3 H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-41-7 CH 3 H H CH2CH 2SCH 3 Bz H F F OH H H NH 2 IV-41-8 CH 3 * H * Bz H F F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-42. N R1 RR 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-42-1 Et H H H Bz H F F OH H H NH 2 IV-42-2 Et H H CH3 Bz H F F OH H H NH 2 IV-42-3 Et H H CH(CH3) 2 Bz H F F OH H H NH 2 IV-42-4 Et H H CH2CH(CH3) 2 Bz H F F OH H H NH 2 IV-42-5 Et H H CH2Ph Bz H F F OH H H NH 2 IV-42-6 Et H H CH2-indol-3-yl Bz H F F OH H H NH 2 IV-42-7 Et H H CH2CH 2SCH 3 Bz H F F OH H H NH 2 IV-42-8 Et * H * Bz H F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-43. No R1 R2 R3a R 3b R4 R5 R6 X Y R7 R' R9 *R2 and R 3b

IV-43-1 'Pr H H H Bz H F F OH H H NH 2 joined IV-43-2 'Pr H H CH 3 Bz H F F OH H H NH 2 together by IV-43-3 'Pr H H CH(CH3) 2 Bz H F F OH H H N1lJ2 (CH2) 3 to IV-43-4 'Pr H H CH 2CH(CH 3) 2 Bz H F F OH H H NH 2 form five IV-43-5 'Pr H H CH 2Ph Bz H F F OH H H NH 2 membered IV-43-6 'Pr H H CH 2-indol-3-yl Bz H F F OH H H NH 2 .

IV-43-7 'Pr H H CH 2CH2SCH 3 Bz H F F OH H H NH 2 rmg. IV-43-8 'Pr * H * Bz H F F OH H H NH 2 Table IV 15 44. 9 1 RI R2 R3aR3b4 R5 R6X Y R7 R R

121 _

No9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 IV-44-1 'Bu H H H Bz H F F OH H H NH 2 IV-44-2 'Bu H H CH 3 Bz H F F OH H H NH 2 IV-44-3 'Bu H H CH(CH 3) 2 Bz H F F OH H H NH 2 IV-44-4 'Bu H H CH 2CH(CH 3) 2 Bz H F F OH H H NH 2 IV-44-5 'Bu H H CH 2Ph Bz H F F OH H H NH 2 IV-44-6 'Bu H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-44-7 'Bu H H CH 2CH2SCH 3 Bz H F F OH H H NH 2 IV-44-8 'Bu * H * Bz H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-45. No9 R R2 R 3a R3b R4 R5 R6 X Y R7 R' R9 IV-45-1 Ph H H H Bz H F F OH H H NH 2 IV-45-2 Ph H H CH3 Bz H F F OH H H NH 2 IV-45-3 Ph H H CH(CH 3)2 Bz H F F OH H H NH 2 IV-45-4 Ph H H CH2CH(CH 3) 2 Bz H F F OH H H NH 2 IV-45-5 Ph H H CH 2Ph Bz H F F OH H H NH 2 IV-45-6 Ph H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-45-7 Ph H H CH2CH2SCH 3 Bz H F F OH H H NH 2 IV-45-8 Ph * H * Bz H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IV-46. N Rl R2 R 3a R3 b R4 R5 R 6 X Y R7 R' R9 IV-46-1 p-Me-Ph H H H Bz H F F OH H H NH 2 IV-46-2 p-Me-Ph H H CH 3 Bz H F F OH H H NH 2 IV-46-3 p-Me-Ph H H CH(CH 3)2 Bz H F F OH H H NH 2 IV-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz H F F OH H H NH 2 IV-46-5 p-Me-Ph H H CH 2Ph Bz H F F OH H H NH 2 IV-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H F F OH H H NH 2 IV-46-8 p-Me-Ph * H * Bz H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-47. N Rl R2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 IV-47-1 p-F-Ph H H H Bz H F F OH H H NH 2 IV-47-2 p-F-Ph H H CH3 Bz H F F OH H H NH 2 IV-47-3 p-F-Ph H H CH(CH 3) 2 Bz H F F OH H H NH 2

1 11)-

N9 Rl R2 R 3 a R3 b R4 R 5 R 6 X Y R7 R' R9 IV-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H F F OH H H NH 2 IV-47-5 p-F-Ph H H CH 2Ph Bz H F F OH H H NH 2 IV-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H F F OH H H NH 2 IV-47-8 p-F-Ph * H * Bz H F F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IV-48. N Rl R2 R 3 a R 3b R4 R R X Y R7 R' R9 IV-48-1 p-Cl-Ph H H H Bz H F F OH H H NH 2 IV-48-2 p-Cl-Ph H H CH 3 Bz H F F OH H H NH 2 IV-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F F OH H H NH 2 IV-48-4 p-Cl-Ph H H CH 2CH(CH3) 2 Bz H F F OH H H NH 2 IV-48-5 p-Cl-Ph H H CH 2Ph Bz H F F OH H H NH 2 IV-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H F F OH H H NH 2 IV-48-8 p-Cl-Ph * H * Bz H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-49. N Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-49-1 p-Br-Ph H H H Bz H F F OH H H NH 2 IV-49-2 p-Br-Ph H H CH3 Bz H F F OH H H NH 2 IV-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F F OH H H NH 2 IV-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H F F OH H H NH 2 IV-49-5 p-Br-Ph H H CH 2Ph Bz H F F OH H H NH 2 IV-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F F OH H H NH 2 IV-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F F OH H H NH 2 IV-49-8 p-Br-Ph * H * Bz H F F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IV-50. N Rl R2 R 3a R 3b R4 R 5 R 6 X Y R7 R' R9 IV-50-1 p-I-Ph H H H Bz H F F OH H H NH 2 IV-50-2 p-I-Ph H H CH 3 Bz H F F OH H H NH 2 IV-50-3 p-I-Ph H H CH(CH3) 2 Bz H F F OH H H NH 2 IV-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz H F F OH H H NH 2 IV-50-5 p-I-Ph H H CH 2Ph Bz H F F OH H H NH 2 IV-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F F OH H H NH 2

No Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 IV-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz H F F OH H H NH 2 IV-50-8 p-I-Ph * H * Bz H F F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R9

R8

0N R3b R2 O 7 N 0 R3a N-P--OOSR

C0 2 R 4 OR' R6

Y X V

_ 1'/

Table V-1. No9 R R2 R 3 a R 3b R4 R R X Y R7 R' R9 V-1-1 CH 3 H H H CH3 H H F OH H H NH 2 V-1-2 CH 3 H H CH 3 CH3 H H F OH H H NH 2 V-1-3 CH 3 H H CH(CH3) 2 CH 3 H H F OH H H NH 2 V-1-4 CH 3 H H CH 2CH(CH3) 2 CH 3 H H F OH H H NH 2 V-1-5 CH 3 H H CH 2Ph CH3 H H F OH H H NH 2 V-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H H F OH H H NH 2 V-1-7 CH 3 H H CH 2CH 2SCH 3 CH 3 H H F OH H H NH 2 V-1-8 CH 3 * H * CH3 H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-2. N9 Rl R 2 R 3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-2-1 Et H H H CH3 H H F OH H H NH 2 V-2-2 Et H H CH 3 CH 3 H H F OH H H NH 2 V-2-3 Et H H CH(CH3) 2 CH3 H H F OH H H NH 2 V-2-4 Et H H CH 2CH(CH3) 2 CH3 H H F OH H H NH 2 V-2-5 Et H H CH 2Ph CH3 H H F OH H H NH 2 V-2-6 Et H H CH 2-indol-3-yl CH 3 H H F OH H H NH 2 V-2-7 Et H H CH 2CH 2SCH 3 CH3 H H F OH H H NH 2 V-2-8 Et * H * CH 3 H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-3. No9 R 1 R2 R 3 a R 3b R4 R 5 R6 X Y R7 R' R9 V-3-1 'Pr H H H CH 3 H H F OH H H NH 2 V-3-2 'Pr H H CH 3 CH3 H H F OH H H NH 2 V-3-3 'Pr H H CH(CH3) 2 CH3 H H F OH H H NH 2 V-3-4 'Pr H H CH 2CH(CH 3) 2 CH 3 H H F OH H H NH 2 V-3-5 Pr H H CH 2Ph CH 3 H H F OH H H NH 2 V-3-6 Pr H H CH 2-indol-3-yl CH3 H H F OH H H NH 2 V-3-7 Pr H H CH 2CH 2SCH3 CH3 H H F OH H H NH 2 V-3-8 Pr * H * CH 3 H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

_11 r _

Table V-4. No9 R1 R2 R 3a R3b R4 R' R6 X Y R7 R' R9 V-4-1 'Bu H H H CH 3 H H F OH H H NH 2 V-4-2 'Bu H H CH 3 CH3 H H F OH H H NH 2 V-4-3 'Bu H H CH(CH 3) 2 CH3 H H F OH H H NH 2 V-4-4 'Bu H H CH 2CH(CH 3) 2 CH 3 H H F OH H H NH 2 V-4-5 'Bu H H CH 2Ph CH 3 H H F OH H H NH 2 V-4-6 'Bu H H CH 2-indol-3-yl CH3 H H F OH H H NH 2 V-4-7 'Bu H H CH 2CH2SCH 3 CH3 H H F OH H H NH 2 V-4-8 'Bu * H * CH 3 H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-5. No9 R1 R2 R 3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-5-1 Ph H H H CH 3 H H F OH H H NH 2 V-5-2 Ph H H CH 3 CH 3 H H F OH H H NH 2 V-5-3 Ph H H CH(CH 3) 2 CH3 H H F OH H H NH 2 V-5-4 Ph H H CH 2CH(CH 3)2 CH3 H H F OH H H NH 2 V-5-5 Ph H H CH 2Ph CH3 H H F OH H H NH 2 V-5-6 Ph H H CH 2-indol-3-yl CH3 H H F OH H H NH 2 V-5-7 Ph H H CH 2CH 2SCH 3 CH3 H H F OH H H NH 2 V-5-8 Ph * H * CH 3 H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-6. N9 R R2 R 3 a R 3b R4 R 5 R6 X Y R7 R' R9 V-6-1 p-Me-Ph H H H CH3 H H F OH H H NH 2 V-6-2 p-Me-Ph H H CH 3 CH3 H H F OH H H NH 2 V-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 H H F OH H H NH 2 V-6-4 p-Me-Ph H H CH 2CH(CH 3)2 CH3 H H F OH H H NH 2 V-6-5 p-Me-Ph H H CH 2Ph CH3 H H F OH H H NH 2 V-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H H F OH H H NH 2 V-6-7 p-Me-Ph H H CH 2CH 2SCH 3 CH3 H H F OH H H NH 2 V-6-8 p-Me-Ph * H * CH3 H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-7. N R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-7-1 p-F-Ph H H H CH 3 H H F OH H H NH 2 V-7-2 p-F-Ph H H CH3 CH3 H H F OH H H NH 2 V-7-3 p-F-Ph H H CH(CH 3) 2 CH3 H H F OH H H NH 2

1 11 r

N9 Rl R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9

V-7-4 p-F-Ph H H CH2CH(CH3) 2 CH 3 H H F OH H H NH 2 V-7-6 p-F-Ph H H CH 2Ph CH 3 H H F OH H H NH 2 V-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H H F OH H H NH 2 V-7-8 p-F-Ph H H CH2CH2 SCH3 CH 3 H H F OH H H NH 2 V-7-20 p-F-Ph * H * CH 3 H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-8. N9 Rl R2 R3 a R3 R4 R R6 X Y R7 R' R9 V-8-1 p-Cl-Ph H H H CH 3 H H F OH H H NH 2 V-8-2 p-Cl-Ph H H CH 3 CH 3 H H F OH H H NH 2 V-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H H F OH H H NH 2 V-8-4 p-Cl-Ph H H CH 2CH(CH 3) 2 CH 3 H H F OH H H NH 2 V-8-5 p-Cl-Ph H H CH 2Ph CH 3 H H F OH H H NH 2 V-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H H F OH H H NH 2 V-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH H H NH 2 V-8-8 p-Cl-Ph * H * CH 3 H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-9. N9 Rl R2 R3 a R3 b R4 R R6 X Y R7 R' R9 V-9-1 p-Br-Ph H H H CH 3 H H F OH H H NH 2 V-9-2 p-Br-Ph H H CH 3 CH 3 H H F OH H H NH 2 V-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H H F OH H H NH 2 V-9-4 p-Br-Ph H H CH 2CH(CH3) 2 CH 3 H H F OH H H NH 2 V-9-6 p-Br-Ph H H CH 2Ph CH 3 H H F OH H H NH 2 V-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H H F OH H H NH 2 V-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH H H NH 2 V-9-20 p-Br-Ph * H * CH 3 H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-10. N9 Rl R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 V-10-1 p-I-Ph H H H CH 3 H H F OH H H NH 2 V-10-2 p-I-Ph H H CH3 CH 3 H H F OH H H NH 2 V-10-3 p-I-Ph H H CH(CH 3) 2 CH 3 H H F OH H H NH 2 V-10-4 p-I-Ph H H CH2CH(CH3) 2 CH 3 H H F OH H H NH 2 V-10-5 p-I-Ph H H CH 2Ph CH 3 H H F OH H H NH 2 V-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H H F OH H H NH 2

N9 Rl R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-10-7 p-I-Ph H H CH2CH 2SCH 3 CH 3 H H F OH H H NH 2 V-10-8 p-I-Ph * H * CH 3 H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-11. N9 R R2 R3 a R3 b R4 R 5 R' X Y R7 R' R9 V-11-1 CH3 H H H Et H H F OH H H NH 2 V-11-2 CH3 H H CH3 Et H H F OH H H NH 2 V-11-3 CH3 H H CH(CH3) 2 Et H H F OH H H NH 2 V-11-4 CH3 H H CH2CH(CH3) 2 Et H H F OH H H NH 2 V-11-5 CH3 H H CH 2Ph Et H H F OH H H NH 2 V-11-6 CH3 H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-11-7 CH3 H H CH2CH 2SCH 3 Et H H F OH H H NH 2 V-11-8 CH3 * H * FtH H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-12. N9 Rl R 2 R 3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-12-1 Et H H H Et H H F OH H H NH 2 V-12-2 Et H H CH3 Et H H F OH H H NH 2 V-12-3 Et H H CH(CH3) 2 Et H H F OH H H NH 2 V-12-4 Et H H CH2CH(CH3) 2 Et H H F OH H H NH 2 V-12-5 Et H H CH 2Ph Et H H F OH H H NH 2 V-12-6 Et H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-12-7 Et H H CH2CH 2SCH 3 Et H H F OH H H NH 2 V-12-8 Et * H * FtH H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-13. No R R2 R 3 R R R4 R R X Y R7 R R9 V-13-1 'Pr H H H Et H H F OH H H NH 2 V-13-2 'Pr H H CH 3 Et H H F OH H H NH 2 V-13-3 'Pr H H CH(CH3) 2 Et H H F OH H H NH 2 V-13-4 'Pr H H CH 2CH(CH 3) 2 Et H H F OH H H NH 2 V-13-5 'Pr H H CH 2Ph Et H H F OH H H NH 2 V-13-6 'Pr H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-13-7 'Pr H H CH 2CH2SCH 3 Et H H F OH H H NH 2 V-13-8 iPr * H * FtH H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

12IQ

Table V-14. No R1 R2 R R3b R4 R5 R6 X Y R7 R' R9 3a

V-14-1 'Bu H H H Et H H F OH H H NH 2 V-14-2 'Bu H H CH 3 Et H H F OH H H NH 2 V-14-3 'Bu H H CH(CH3) 2 Et H H F OH H H NH 2 V-14-4 'Bu H H CH 2CH(CH 3) 2 Et H H F OH H H NH 2 V-14-5 'Bu H H CH 2Ph Et H H F OH H H NH 2 V-14-6 'Bu H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-14-7 'Bu H H CH 2CH2SCH 3 Et H H F OH H H NH 2 V-14-8 'Bu * H * Et H H F OH H H NH 2 *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table V-15. No9 R1 R 2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 V-15-1 Ph H H H Et H H F OH H H NH 2 V-15-2 Ph H H CH3 Et H H F OH H H NH 2 V-15-3 Ph H H CH(CH 3) 2 Et H H F OH H H NH 2 V-15-4 Ph H H CH2CH(CH3) 2 Et H H F OH H H NH 2 V-15-5 Ph H H CH 2Ph Et H H F OH H H NH 2 V-15-6 Ph H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-15-7 Ph H H CH2CH 2SCH 3 Et H H F OH H H NH 2 V-15-8 Ph * H * FtH H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-16. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 V-16-1 p-Me-Ph H H H Et H H F OH H H NH 2 V-16-2 p-Me-Ph H H CH3 Et H H F OH H H NH 2 V-16-3 p-Me-Ph H H CH(CH 3) 2 Et H H F OH H H NH 2 V-16-4 p-Me-Ph H H CH2CH(CH3) 2 Et H H F OH H H NH 2 V-16-5 p-Me-Ph H H CH 2Ph Et H H F OH H H NH 2 V-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H H F OH H H NH 2 V-16-8 p-Me-Ph * H * FtH H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-17. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-17-1 p-F-Ph H H H Et H H F OH H H NH 2 V-17-2 p-F-Ph H H CH3 Et H H F OH H H NH 2

1'20

9 Rl R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 V-17-3 p-F-Ph H H CH(CH 3) 2 Et H H F OH H H NH 2 V-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H H F OH H H NH 2 V-17-5 p-F-Ph H H CH 2Ph Et H H F OH H H NH 2 V-17-6 p-F-Ph H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-17-7 p-F-Ph H H CH2CH2SCH 3 Et H H F OH H H NH 2 V-17-8 p-F-Ph * H * EtH H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-18. X9 R R2 R 3a R 3b R 4 R R 6 X Y R7 R' R9 V-18-1 p-Cl-Ph H H H Et H H F OH H H NH 2 V-18-2 p-Cl-Ph H H CH 3 Et H H F OH H H NH 2 V-18-3 p-Cl-Ph H H CH(CH3) 2 Et H H F OH H H NH 2 V-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et H H F OH H H NH 2 V-18-5 p-Cl-Ph H H CH 2Ph Et H H F OH H H NH 2 V-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H H F OH H H NH 2 V-18-8 p-Cl-Ph * H * FtH H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-19. X9 R R2 R 3 a R3 b R4 R 5 R 6 X Y R7 R' R9 V-19-1 p-Br-Ph H H H Et H H F OH H H NH 2 V-19-2 p-Br-Ph H H CH 3 Et H H F OH H H NH 2 V-19-3 p-Br-Ph H H CH(CH3) 2 Et H H F OH H H NH 2 V-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et H H F OH H H NH 2 V-19-5 p-Br-Ph H H CH 2Ph Et H H F OH H H NH 2 V-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H H F OH H H NH 2 V-19-8 p-Br-Ph * H * FtH H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-20. 9 Rl R2 R 3 a R 3b R4 R5 R6 X Y R7 R' R9 V-20-1 p-I-Ph H H H Et H H F OH H H NH 2 V-20-2 p-I-Ph H H CH3 Et H H F OH H H NH 2 V-20-3 p-I-Ph H H CH(CH 3) 2 Et H H F OH H H NH 2 V-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H H F OH H H NH 2 V-20-5 p-I-Ph H H CH 2Ph Et H H F OH H H NH 2

lA -

N9 Rl R2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 V-20-6 p-I-Ph H H CH 2-indol-3-yl Et H H F OH H H NH 2 V-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H H F OH H H NH 2 V-20-8 p-I-Ph * H * Et H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-21. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 V-21-1 CH3 H H H 'Pr H H F OH H H NH 2 V-21-2 CH3 H H CH3 'Pr H H F OH H H NH 2 V-21-3 CH3 H H CH(CH 3)2 'Pr H H F OH H H NH 2 V-21-4 CH3 H H CH2CH(CH 3) 2 'Pr H H F OH H H NH 2 V-21-5 CH3 H H CH 2Ph 'Pr H H F OH H H NH 2 V-21-6 CH3 H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-21-7 CH3 H H CH2CH 2SCH 3 'Pr H H F OH H H NH 2 V-21-8 CH3 * H * 'Pr H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-22. N9 Rl R 2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 V-22-1 Et H H H 'Pr H H F OH H H NH 2 V-22-2 Et H H CH3 'Pr H H F OH H H NH 2 V-22-3 Et H H CH(CH 3)2 'Pr H H F OH H H NH 2 V-22-4 Et H H CH2CH(CH 3) 2 'Pr H H F OH H H NH 2 V-22-5 Et H H CH 2Ph 'Pr H H F OH H H NH 2 V-22-6 Et H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-22-7 Et H H CH2CH 2SCH 3 'Pr H H F OH H H NH 2 V-22-8 Et * H * 'Pr H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-23. No9 R R2 R 3a R3 b R4 R5 R6 X Y R7 R' R9 V-23-1 'Pr H H H 'Pr H H F OH H H NH 2 V-23-2 'Pr H H CH 3 'Pr H H F OH H H NH 2 V-23-3 'Pr H H CH(CH 3)2 'Pr H H F OH H H NH 2 V-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H H F OH H H NH 2 V-23-5 'Pr H H CH 2Ph 'Pr H H F OH H H NH 2 V-23-6 'Pr H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-23-7 'Pr H H CH 2CH2SCH 3 'Pr H H F OH H H NH 2 V-23-8 'Pr * H * 'Pr H H F OH H H NH2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 1A1

Table V-24. No9 R1 R2 R3 a R3 R4 R R' X Y R7 R' R9 V-24-1 'Bu H H H 'Pr H H F OH H H NH 2 V-24-2 'Bu H H CH 3 'Pr H H F OH H H NH 2 V-24-3 'Bu H H CH(CH3) 2 'Pr H H F OH H H NH 2 V-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H H F OH H H NH 2 V-24-5 'Bu H H CH 2Ph 'Pr H H F OH H H NH 2 V-24-6 'Bu H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-24-7 'Bu H H CH 2CH2SCH 3 'Pr H H F OH H H NH 2 V-24-8 'Bu * H * 'Pr H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-25. No9 R1 R 2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 V-25-1 Ph H H H 'Pr H H F OH H H NH 2 V-25-2 Ph H H CH3 'Pr H H F OH H H NH 2 V-25-3 Ph H H CH(CH 3) 2 'Pr H H F OH H H NH 2 V-25-4 Ph H H CH2CH(CH 3) 2 'Pr H H F OH H H NH 2 V-25-5 Ph H H CH 2Ph 'Pr H H F OH H H NH 2 V-25-6 Ph H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-25-7 Ph H H CH2CH 2SCH 3 'Pr H H F OH H H NH 2 V-25-8 Ph * H * 'Pr H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-26. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 V-26-1 p-Me-Ph H H H 'Pr H H F OH H H NH 2 V-26-2 p-Me-Ph H H CH3 'Pr H H F OH H H NH 2 V-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr H H F OH H H NH 2 V-26-4 p-Me-Ph H H CH2CH(CH 3) 2 'Pr H H F OH H H NH 2 V-26-5 p-Me-Ph H H CH 2Ph 'Pr H H F OH H H NH 2 V-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H H F OH H H NH 2 V-26-8 p-Me-Ph * H * 'Pr H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-27. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-27-1 p-F-Ph H H H 'Pr H H F OH H H NH 2 V-27-2 p-F-Ph H H CH3 'Pr H H F OH H H NH 2 V-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H H F OH H H NH 2

_ 1A)

N9 Rl R2 R3 a R3 b R4 R' R' X Y R7 R' R9 V-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H H F OH H H NH 2 V-27-5 p-F-Ph H H CH 2Ph 'Pr H H F OH H H NH 2 V-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-27-7 p-F-Ph H H CH2CH2 SCH3 'Pr H H F OH H H NH 2 V-27-8 p-F-Ph * H * 'Pr H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-28. N9 Rl R2 R3 R 3 b R4 R R X Y R7 R' R9 V-28-1 p-Cl-Ph H H H 'Pr H H F OH H H NH 2 V-28-2 p-Cl-Ph H H CH 3 'Pr H H F OH H H NH 2 V-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H H F OH H H NH 2 V-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr H H F OH H H NH 2 V-28-5 p-Cl-Ph H H CH 2Ph 'Pr H H F OH H H NH 2 V-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H H F OH H H NH 2 V-28-8 p-Cl-Ph * H * 'Pr H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-29. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 V-29-1 p-Br-Ph H H H 'Pr H H F OH H H NH 2 V-29-2 p-Br-Ph H H CH 3 'Pr H H F OH H H NH 2 V-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H H F OH H H NH 2 V-29-4 p-Br-Ph H H CH 2CH(CH3) 2 'Pr H H F OH H H NH 2 V-29-5 p-Br-Ph H H CH 2Ph 'Pr H H F OH H H NH 2 V-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2 V-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr H H F OH H H NH 2 V-29-8 p-Br-Ph * H * 'Pr H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-30. N Rl R2 R3 a R3b R4 R5 R6 X Y R7 R' R9 V-30-1 p-I-Ph H H H 'Pr H H F OH H H NH 2 V-30-2 p-I-Ph H H CH3 'Pr H H F OH H H NH 2 V-30-3 p-I-Ph H H CH(CH 3) 2 'Pr H H F OH H H NH 2 V-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H H F OH H H NH 2 V-30-5 p-I-Ph H H CH 2Ph 'Pr H H F OH H H NH 2 V-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H NH 2

1 /I2

No Rl R2 R 3 a R3 b R4 R' R' X Y R7 R' R9 V-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H H F OH H H NH 2 V-30-8 p-I-Ph * H * 'Pr H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1A//

Table V-31. No9 R1 R2 R3 a R3b R4 R 5 R' X Y R7 R' R9 V-31-1 CH3 H H H "Bu H H F OH H H NH 2 V-31-2 CH3 H H CH3 "Bu H H F OH H H NH 2 V-31-3 CH3 H H CH(CH3) 2 "Bu H H F OH H H NH 2 V-31-4 CH3 H H CH2CH(CH3) 2 "Bu H H F OH H H NH 2 V-31-5 CH3 H H CH 2Ph "Bu H H F OH H H NH 2 V-31-6 CH3 H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-31-7 CH3 H H CH2CH 2SCH 3 "Bu H H F OH H H NH 2 V-31-8 CH3 * H * "Bu H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-32. N9 Rl R 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 V-32-1 Et H H H "Bu H H F OH H H NH 2 V-32-2 Et H H CH3 "Bu H H F OH H H NH 2 V-32-3 Et H H CH(CH3) 2 "Bu H H F OH H H NH 2 V-32-4 Et H H CH2CH(CH3) 2 "Bu H H F OH H H NH 2 V-32-5 Et H H CH 2Ph "Bu H H F OH H H NH 2 V-32-6 Et H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-32-7 Et H H CH2CH 2SCH 3 "Bu H H F OH H H NH 2 V-32-8 Et * H * "Bu H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-33. No9 R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' R9 V-33-1 'Pr H H H "Bu H H F OH H H NH 2 V-33-2 'Pr H H CH 3 "Bu H H F OH H H NH 2 V-33-3 'Pr H H CH(CH3) 2 "Bu H H F OH H H NH 2 V-33-4 'Pr H H CH 2CH(CH 3) 2 "Bu H H F OH H H NH 2 V-33-5 Pr H H CH 2Ph "Bu H H F OH H H NH 2 V-33-6 Pr H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-33-7 Pr H H CH 2CH2SCH 3 "Bu H H F OH H H NH 2 V-33-8 Pr * H * "Bu H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1/ r,

Table V-34. N9 R1 R2 R3 a R3 R4 R R X Y R7 R' R9 V-34-1 'Bu H H H "Bu H H F OH H H NH 2 V-34-2 'Bu H H CH 3 "Bu H H F OH H H NH 2 V-34-3 tBu H H CH(CH3) 2 "Bu H H F OH H H NH 2 V-34-4 tBu H H CH 2CH(CH 3) 2 "Bu H H F OH H H NH 2 V-34-5 tBu H H CH 2Ph "Bu H H F OH H H NH 2 V-34-6 tBu H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 t V-34-7 Bu H H CH 2CH2SCH 3 "Bu H H F OH H H NH 2 t V-34-8 Bu * H * "Bu H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-35. No9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-35-1 Ph H H H "Bu H H F OH H H NH 2 V-35-2 Ph H H CH3 "Bu H H F OH H H NH 2 V-35-3 Ph H H CH(CH 3) 2 "Bu H H F OH H H NH 2 V-35-4 Ph H H CH2CH(CH 3) 2 "Bu H H F OH H H NH 2 V-35-5 Ph H H CH 2Ph "Bu H H F OH H H NH 2 V-35-6 Ph H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-35-7 Ph H H CH2CH 2SCH 3 "Bu H H F OH H H NH 2 V-35-8 Ph * H * "Bu H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-36. No9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 V-36-1 p-Me-Ph H H H "Bu H H F OH H H NH 2 V-36-2 p-Me-Ph H H CH3 "Bu H H F OH H H NH 2 V-36-3 p-Me-Ph H H CH(CH 3) 2 "Bu H H F OH H H NH 2 V-36-4 p-Me-Ph H H CH2CH(CH 3) 2 "Bu H H F OH H H NH 2 V-36-5 p-Me-Ph H H CH 2Ph "Bu H H F OH H H NH 2 V-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-36-7 p-Me-Ph H H CH2CH 2SCH 3 "Bu H H F OH H H NH 2 V-36-8 p-Me-Ph * H * "Bu H H F OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table V-37. N9 R R2 R3a R3 b R4 R 5 R6 X Y R7 R' R9 V-37-1 p-F-Ph H H H "Bu H H F OH H H NH 2 V-37-2 p-F-Ph H H CH3 "Bu H H F OH H H NH 2 V-37-3 p-F-Ph H H CH(CH 3) 2 "Bu H H F OH H H NH 2

_ 1A _

N9 Rl R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 V-37-4 p-F-Ph H H CH2CH(CH3) 2 "Bu H H F OH H H NH 2 V-37-5 p-F-Ph H H CH 2Ph "Bu H H F OH H H NH 2 V-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-37-7 p-F-Ph H H CH2CH2 SCH3 "Bu H H F OH H H NH 2 V-37-8 p-F-Ph * H * "Bu H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-38. N9 R R2 R 3a R 3b R4 R R 6 X Y R7 R' R9 V-38-1 p-Cl-Ph H H H "Bu H H F OH H H NH 2 V-38-2 p-Cl-Ph H H CH 3 "Bu H H F OH H H NH 2 V-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H H F OH H H NH 2 V-38-4 p-Cl-Ph H H CH 2 CH(CH3) 2 "Bu H H F OH H H NH 2 V-38-5 p-Cl-Ph H H CH 2 Ph "Bu H H F OH H H NH 2 V-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH H H NH 2 V-38-8 p-Cl-Ph * H * "Bu H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-39. R 3a R3 b R4 5 6 R9 N9 R R2 R R X Y R7 R' V-39-1 p-Br-Ph H H H "Bu H H F OH H H NH 2 V-39-2 p-Br-Ph H H CH 3 "Bu H H F OH H H NH 2 V-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H H F OH H H NH 2 V-39-4 p-Br-Ph H H CH 2 CH(CH3) 2 "Bu H H F OH H H NH 2 V-39-5 p-Br-Ph H H CH 2 Ph "Bu H H F OH H H NH 2 V-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H H F OH H H NH 2 V-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH H H NH 2 V-39-8 p-Br-Ph * H * "Bu H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-40. N Rl R2 R 3a R 3b R4 R 5 R6 X Y R7 R' R9 V-40-1 p-I-Ph H H H "Bu H H F OH H H NH 2 V-40-2 p-I-Ph H H CH3 "Bu H H F OH H H NH 2 V-40-3 p-I-Ph H H CH(CH 3) 2 "Bu H H F OH H H NH 2 V-40-4 p-I-Ph H H CH2CH(CH3) 2 "Bu H H F OH H H NH 2 V-40-5 p-I-Ph H H CH 2Ph "Bu H H F OH H H NH 2 V-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H H F OH H H NH 2

1 AI7

N9 R1 R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 V-40-7 p-I-Ph H H CH2CH 2SCH 3 "Bu H H F OH H H NH 2 V-40-8 p-I-Ph * H * "Bu H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-41. N9 R1 R2 R3 a R3 b R4 R' R' X Y R7 R' R9 V-41-1 CH3 H H H Bz H H F OH H H NH 2 V-41-2 CH3 H H CH3 Bz H H F OH H H NH 2 V-41-3 CH3 H H CH(CH3) 2 Bz H H F OH H H NH 2 V-41-4 CH3 H H CH2CH(CH3) 2 Bz H H F OH H H NH 2 V-41-5 CH3 H H CH 2Ph Bz H H F OH H H NH 2 V-41-6 CH3 H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-41-7 CH3 H H CH2CH 2SCH 3 Bz H H F OH H H NH 2 V-41-8 CH3 * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-42. N9 Rl R 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 V-42-1 Et H H H Bz H H F OH H H NH 2 V-42-2 Et H H CH3 Bz H H F OH H H NH 2 V-42-3 Et H H CH(CH3) 2 Bz H H F OH H H NH 2 V-42-4 Et H H CH2CH(CH3) 2 Bz H H F OH H H NH 2 V-42-5 Et H H CH 2Ph Bz H H F OH H H NH 2 V-42-6 Et H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-42-7 Et H H CH2CH 2SCH 3 Bz H H F OH H H NH 2 V-42-8 Et * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-43. No R1 R2 R3a R3b R4 R5 R6 X Y R7 R' R9 *R2 and R 3b

V-43-1 tPr H H H Bz H H F OH H H NH 2 joined V-43-2 'Pr H H CH 3 Bz H H F OH H H NH 2 together by V-43-3 'Pr H H CH(CH3) 2 Bz H H F OH H H N2 (CH 2 ) 3 to V-43-4 'Pr H H CH 2CH(CH 3) 2 Bz H H F OH H H NH 2 form five V-43-5 'Pr H H CH 2Ph Bz H H F OH H H NH 2 membered V-43-6 Pr H H CH 2-indol-3-yl Bz H H F OH H H NH 2 .

V-43-7 Pr H H CH 2CH2SCH 3 Bz H H F OH H H NH 2 rmg. V-43-8 Pr * H * Bz H H F OH H H NH 2 Table V-44. 1 2 3 Rb 4 R 5 R 6 X Y R7 R' R9 No R R R a R

1/12

No9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' R9 V-44-1 'Bu H H H Bz H H F OH H H NH 2 V-44-2 'Bu H H CH 3 Bz H H F OH H H NH 2 V-44-3 'Bu H H CH(CH3) 2 Bz H H F OH H H NH 2 V-44-4 'Bu H H CH 2CH(CH 3) 2 Bz H H F OH H H NH 2 V-44-5 'Bu H H CH 2Ph Bz H H F OH H H NH 2 V-44-6 'Bu H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-44-7 'Bu H H CH 2CH2SCH 3 Bz H H F OH H H NH 2 V-44-8 'Bu * H * Bz H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-45. No9 R1 R 2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 V-45-1 Ph H H H Bz H H F OH H H NH 2 V-45-2 Ph H H CH3 Bz H H F OH H H NH 2 V-45-3 Ph H H CH(CH 3) 2 Bz H H F OH H H NH 2 V-45-4 Ph H H CH2CH(CH3) 2 Bz H H F OH H H NH 2 V-45-5 Ph H H CH 2Ph Bz H H F OH H H NH 2 V-45-6 Ph H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-45-7 Ph H H CH2CH 2SCH 3 Bz H H F OH H H NH 2 V-45-8 Ph * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-46. N Rl R2 R3 a R3 b R4 R 5 R6 X Y R7 R' R9 V-46-1 p-Me-Ph H H H Bz H H F OH H H NH 2 V-46-2 p-Me-Ph H H CH3 Bz H H F OH H H NH 2 V-46-3 p-Me-Ph H H CH(CH 3) 2 Bz H H F OH H H NH 2 V-46-4 p-Me-Ph H H CH2CH(CH3) 2 Bz H H F OH H H NH 2 V-46-5 p-Me-Ph H H CH 2Ph Bz H H F OH H H NH 2 V-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz H H F OH H H NH 2 V-46-8 p-Me-Ph * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-47. N9 R R2 R3a R 3b R4 R 5 R6 X Y R7 R' R9 V-47-1 p-F-Ph H H H Bz H H F OH H H NH 2 V-47-2 p-F-Ph H H CH3 Bz H H F OH H H NH 2 V-47-3 p-F-Ph H H CH(CH 3) 2 Bz H H F OH H H NH 2

lAO_

N Rl R2 R3 a R3 b R4 R 5 R' X Y R7 R' R9 V-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H H F OH H H NH 2 V-47-5 p-F-Ph H H CH 2Ph Bz H H F OH H H NH 2 V-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-47-7 p-F-Ph H H CH2CH2 SCH3 Bz H H F OH H H NH 2 V-47-8 p-F-Ph * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table V-48. N9 R R2 R 3a R 3b R4 R R X Y R7 R' R9 V-48-1 p-Cl-Ph H H H Bz H H F OH H H NH 2 V-48-2 p-Cl-Ph H H CH 3 Bz H H F OH H H NH 2 V-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H H F OH H H NH 2 V-48-4 p-Cl-Ph H H CH 2CH(CH3) 2 Bz H H F OH H H NH 2 V-48-5 p-Cl-Ph H H CH 2Ph Bz H H F OH H H NH 2 V-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H H F OH H H NH 2 V-48-8 p-Cl-Ph * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-49. N9 R R2 R 3 a R3 b R4 R' R6 X Y R7 R' R9 V-49-1 p-Br-Ph H H H Bz H H F OH H H NH 2 V-49-2 p-Br-Ph H H CH 3 Bz H H F OH H H NH 2 V-49-3 p-Br-Ph H H CH(CH3) 2 Bz H H F OH H H NH 2 V-49-4 p-Br-Ph H H CH 2CH(CH3) 2 Bz H H F OH H H NH 2 V-49-5 p-Br-Ph H H CH 2Ph Bz H H F OH H H NH 2 V-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H H F OH H H NH 2 V-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz H H F OH H H NH 2 V-49-8 p-Br-Ph * H * Bz H H F OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table V-50. N Rl R2 R 3 a R 3b R4 R 5 R 6 X Y R7 R' R9 V-50-1 p-I-Ph H H H Bz H H F OH H H NH 2 V-50-2 p-I-Ph H H CH3 Bz H H F OH H H NH 2 V-50-3 p-I-Ph H H CH(CH 3) 2 Bz H H F OH H H NH 2 V-50-4 p-I-Ph H H CH2CH(CH3) 2 Bz H H F OH H H NH 2 V-50-5 p-I-Ph H H CH 2Ph Bz H H F OH H H NH 2 V-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H H F OH H H NH 2

1;n_

N9 Rl R2 R3 a R3 b R4 R 5 R' X Y R7 R' R9 V-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H H F OH H H NH 2 V-50-8 p-I-Ph * H * Bz H H F OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

0

R8

NH

Rt 2 0 R3b 0 R7 N 0 R3a N--P - OO

OR 1 R5 R6 CO2R4

Y X VI

Table VI-1. N9 R R2 R3 a R3 b R4 R 5 R6 X Y R7 R' VI-1-1 CH3 H H H CH 3 H F H OH H H VI-1-2 CH3 H H CH3 CH 3 H F H OH H H VI-1-3 CH3 H H CH(CH3) 2 CH 3 H F H OH H H VI-1-4 CH3 H H CH2CH(CH3) 2 CH 3 H F H OH H H VI-1-5 CH3 H H CH 2Ph CH 3 H F H OH H H VI-1-6 CH3 H H CH 2-indol-3-yl CH 3 H F H OH H H VI-1-7 CH3 H H CH2CH 2SCH 3 CH 3 H F H OH H H VI-1-8 CH3 * H * CH 3 H F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-2. N9 Rl R 2 R3 a R3 b R4 R5 R 6 X Y R7 R' VI-2-1 Et H H H CH 3 H F H OH H H VI-2-2 Et H H CH 3 CH 3 H F H OH H H VI-2-3 Et H H CH(CH3) 2 CH 3 H F H OH H H VI-2-4 Et H H CH 2CH(CH3) 2 CH 3 H F H OH H H VI-2-5 Et H H CH 2Ph CH 3 H F H OH H H VI-2-6 Et H H CH 2-indol-3-yl CH 3 H F H OH H H VI-2-7 Et H H CH 2CH 2SCH 3 CH 3 H F H OH H H VI-2-8 Et * H * CH 3 H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1 1 _

Table VI-3. N9 R R2 R3 a R3b R4 R' R6 X Y R7 R' VI-3-1 'Pr H H H CH 3 H F H OH H H VI-3-2 'Pr H H CH 3 CH3 H F H OH H H VI-3-3 'Pr H H CH(CH 3) 2 CH3 H F H OH H H VI-3-4 Pr H H CH 2CH(CH 3) 2 CH 3 H F H OH H H VI-3-5 Pr H H CH 2Ph CH 3 H F H OH H H VI-3-6 Pr H H CH 2-indol-3-yl CH3 H F H OH H H VI-3-7 Pr H H CH 2CH2SCH 3 CH3 H F H OH H H VI-3-8 Pr * H * CH 3 H F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VI-4. N9 R R2 R 3a R R4 R R6 X Y R7 R' VI-4-1 'Bu H H H CH 3 H F H OH H H VI-4-2 'Bu H H CH 3 CH 3 H F H OH H H VI-4-3 'Bu H H CH(CH 3)2 CH 3 H F H OH H H VI-4-4 'Bu H H CH 2CH(CH 3)2 CH 3 H F H OH H H VI-4-5 'Bu H H CH 2Ph CH 3 H F H OH H H VI-4-6 'Bu H H CH 2-indol-3-yl CH 3 H F H OH H H VI-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H F H OH H H VI-4-8 'Bu * H * CH 3 H F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

_1 G _

Table VI-5. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' VI-5-1 Ph H H H CH 3 H F H OH H H VI-5-2 Ph H H CH3 CH3 H F H OH H H VI-5-3 Ph H H CH(CH3)2 CH3 H F H OH H H VI-5-4 Ph H H CH2CH(CH3) 2 CH3 H F H OH H H VI-5-5 Ph H H CH 2Ph CH 3 H F H OH H H VI-5-6 Ph H H CH 2-indol-3-yl CH3 H F H OH H H VI-5-7 Ph H H CH2CH 2SCH 3 CH3 H F H OH H H VI-5-8 Ph * H * CH 3 H F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-6. N9 R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' VI-6-1 p-Me-Ph H H H CH 3 H F H OH H H VI-6-2 p-Me-Ph H H CH3 CH3 H F H OH H H VI-6-3 p-Me-Ph H H CH(CH3)2 CH3 H F H OH H H VI-6-4 p-Me-Ph H H CH2CH(CH 3) 2 CH3 H F H OH H H VI-6-5 p-Me-Ph H H CH 2Ph CH 3 H F H OH H H VI-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F H OH H H VI-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H F H OH H H VI-6-8 p-Me-Ph * H * CH 3 H F H OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-7. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' VI-7-1 p-F-Ph H H H CH 3 H F H OH H H VI-7-2 p-F-Ph H H CH3 CH3 H F H OH H H VI-7-3 p-F-Ph H H CH(CH3)2 CH3 H F H OH H H VI-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H F H OH H H VI-7-6 p-F-Ph H H CH 2Ph CH 3 H F H OH H H VI-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F H OH H H VI-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H F H OH H H VI-7-20 p-F-Ph * H * CH 3 H F H OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1 2-_

Table VI-8. N R1 R 2 RR3 b R4 R R X Y R7 R' VI-8-1 p-Cl-Ph H H H CH 3 H F H OH H H VI-8-2 p-Cl-Ph H H CH 3 CH 3 H F H OH H H VI-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F H OH H H VI-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H F H OH H H VI-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F H OH H H VI-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F H OH H H VI-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H F H OH H H VI-8-8 p-Cl-Ph * H * CH 3 H F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-9. N9 R1 R 2 R 3a R3 b R4 R6 X Y R7 R' VI-9-1 p-Br-Ph H H H CH 3 H F H OH H H VI-9-2 p-Br-Ph H H CH3 CH 3 H F H OH H H VI-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H F H OH H H VI-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH 3 H F H OH H H VI-9-6 p-Br-Ph H H CH 2Ph CH 3 H F H OH H H VI-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H F H OH H H VI-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 H F H OH H H VI-9-20 p-Br-Ph * H * CH 3 H F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-10. N9 R1 R 2 R 3a R 3b R4 R 5 R6 X Y R7 R' VI-10-1 p-I-Ph H H H CH 3 H F H OH H H VI-10-2 p-I-Ph H H CH 3 CH3 H F H OH H H VI-10-3 p-I-Ph H H CH(CH3) 2 CH3 H F H OH H H VI-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H F H OH H H VI-10-5 p-I-Ph H H CH 2Ph CH 3 H F H OH H H VI-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H F H OH H H VI-10-7 p-I-Ph H H CH 2CH2SCH 3 CH3 H F H OH H H VI-10-8 p-I-Ph * H * CH 3 H F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 rA

Table V-11. No9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' VI-11-1 CH 3 H H H Et H F H OH H H VI-11-2 CH 3 H H CH3 Et H F H OH H H VI-11-3 CH 3 H H CH(CH3) 2 Et H F H OH H H VI-11-4 CH 3 H H CH2CH(CH3) 2 Et H F H OH H H VI-11-5 CH 3 H H CH 2Ph Et H F H OH H H VI-11-6 CH 3 H H CH 2-indol-3-yl Et H F H OH H H VI-11-7 CH 3 H H CH2CH 2SCH 3 Et H F H OH H H VI-11-8 CH 3 * H * Et H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-12. N R1 RR 2 R 3a R3 b R4 R 5 R6 X Y R7 R' VI-12-1 Et H H H Et H F H OH H H VI-12-2 Et H H CH3 Et H F H OH H H VI-12-3 Et H H CH(CH3) 2 Et H F H OH H H VI-12-4 Et H H CH2CH(CH3) 2 Et H F H OH H H VI-12-5 Et H H CH2Ph Et H F H OH H H VI-12-6 Et H H CH2-indol-3-yl Et H F H OH H H VI-12-7 Et H H CH2CH 2SCH 3 Et H F H OH H H VI-12-8 Et * H * Et H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-13. No9 R1 R2 R3a R 3b R4 R R6 X Y R7 R' VI-13-1 'Pr H H H Et H F H OH H H VI-13-2 'Pr H H CH 3 Et H F H OH H H VI-13-3 'Pr H H CH(CH3) 2 Et H F H OH H H VI-13-4 'Pr H H CH 2CH(CH3)2 Et H F H OH H H VI-13-5 'Pr H H CH 2Ph Et H F H OH H H VI-13-6 'Pr H H CH 2-indol-3-yl Et H F H OH H H VI-13-7 'Pr H H CH 2CH2SCH 3 Et H F H OH H H VI-13-8 Pr * H * Et H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-14. No R1 R2 R3 a R3b R4 R' R' X Y R7 R' VI-14-1 'Bu H H H Et H F H OH H H VI-14-2 'Bu H H CH 3 Et H F H OH H H VI-14-3 'Bu H H CH(CH 3) 2 Et H F H OH H H VI-14-4 'Bu H H CH 2CH(CH 3) 2 Et H F H OH H H VI-14-5 'Bu H H CH 2Ph Et H F H OH H H VI-14-6 'Bu H H CH 2-indol-3-yl Et H F H OH H H VI-14-7 'Bu H H CH 2CH2SCH 3 Et H F H OH H H VI-14-8 'Bu * H * Et H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-15. N R R 2 R 3 aRR R4 R R6 X Y R7 R VI-15-1 Ph H H H Et H F H OH H H VI-15-2 Ph H H CH3 Et H F H OH H H VI-15-3 Ph H H CH(CH 3)2 Et H F H OH H H VI-15-4 Ph H H CH2CH(CH 3) 2 Et H F H OH H H VI-15-5 Ph H H CH 2Ph Et H F H OH H H VI-15-6 Ph H H CH 2-indol-3-yl Et H F H OH H H VI-15-7 Ph H H CH2CH2SCH 3 Et H F H OH H H VI-15-8 Ph * H * Et H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-16. N9 R1 R2 R 3a R3b R4 R 5 R' X Y R7 R VI-16-1 p-Me-Ph H H H Et H F H OH H H VI-16-2 p-Me-Ph H H CH 3 Et H F H OH H H VI-16-3 p-Me-Ph H H CH(CH 3)2 Et H F H OH H H VI-16-4 p-Me-Ph H H CH 2CH(CH 3) 2 Et H F H OH H H VI-16-5 p-Me-Ph H H CH 2Ph Et H F H OH H H VI-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F H OH H H VI-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H F H OH H H VI-16-8 p-Me-Ph * H * Et H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-17. N R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' VI-17-1 p-F-Ph H H H Et H F H OH H H VI-17-2 p-F-Ph H H CH3 Et H F H OH H H VI-17-3 p-F-Ph H H CH(CH 3) 2 Et H F H OH H H

1% _

N9 Rl R2 R3 a R3 b R4 R' R6 X Y R7 R' VI-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H F H OH H H VI-17-5 p-F-Ph H H CH 2Ph Et H F H OH H H VI-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F H OH H H VI-17-7 p-F-Ph H H CH2CH 2SCH 3 Et H F H OH H H VI-17-8 p-F-Ph * H * Et H F H OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table VI-18. N Rl R2 R3 a R 3b R4 R R6 X Y R7 R' VI-18-1 p-Cl-Ph H H H Et H F H OH H H VI-18-2 p-Cl-Ph H H CH 3 Et H F H OH H H VI-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F H OH H H VI-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H F H OH H H VI-18-5 p-Cl-Ph H H CH 2Ph Et H F H OH H H VI-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F H OH H H VI-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H F H OH H H VI-18-8 p-Cl-Ph * H * Et H F H OH H H

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table VI-19. N Rl R2 R 3a R3 b R4 R 5 R6 X Y R7 R VI-19-1 p-Br-Ph H H H Et H F H OH H H VI-19-2 p-Br-Ph H H CH3 Et H F H OH H H VI-19-3 p-Br-Ph H H CH(CH3) 2 Et H F H OH H H VI-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H F H OH H H VI-19-5 p-Br-Ph H H CH 2Ph Et H F H OH H H VI-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F H OH H H VI-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H F H OH H H VI-19-8 p-Br-Ph * H * Et H F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VI-20. N Rl R2 R 3a R3b R4 R 5 R6 X Y R7 R' VI-20-1 p-I-Ph H H H Et H F H OH H H VI-20-2 p-I-Ph H H CH 3 Et H F H OH H H VI-20-3 p-I-Ph H H CH(CH3) 2 Et H F H OH H H VI-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H F H OH H H VI-20-5 p-I-Ph H H CH 2Ph Et H F H OH H H VI-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F H OH H H

1 _'7

N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' VI-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H F H OH H H VI-20-8 p-I-Ph * H * Et H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-21. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' VI-21-1 CH 3 H H H 'Pr H F H OH H H VI-21-2 CH 3 H H CH3 'Pr H F H OH H H VI-21-3 CH 3 H H CH(CH 3) 2 'Pr H F H OH H H VI-21-4 CH 3 H H CH2CH(CH 3)2 'Pr H F H OH H H VI-21-5 CH 3 H H CH 2Ph 'Pr H F H OH H H VI-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H F H OH H H VI-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H F H OH H H VI-21-8 CH 3 * H * 'Pr H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-22. N Rl RR 2 R 3a R3 b R4 R' R6 X Y R7 R' VI-22-1 Et H H H 'Pr H F H OH H H VI-22-2 Et H H CH3 'Pr H F H OH H H VI-22-3 Et H H CH(CH 3) 2 'Pr H F H OH H H VI-22-4 Et H H CH2CH(CH 3)2 'Pr H F H OH H H VI-22-5 Et H H CH2Ph 'Pr H F H OH H H VI-22-6 Et H H CH2-indol-3-yl 'Pr H F H OH H H VI-22-7 Et H H CH2CH 2SCH 3 'Pr H F H OH H H VI-22-8 Et * H * 'Pr H F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VI-23. No R R2 R3a RS R4 R 5 R6 X Y R7 R' VI-23-1 'Pr H H H 'Pr H F H OH H H VI-23-2 'Pr H H CH 3 'Pr H F H OH H H VI-23-3 'Pr H H CH(CH3) 2 'Pr H F H OH H H VI-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H F H OH H H VI-23-5 'Pr H H CH 2Ph 'Pr H F H OH H H VI-23-6 'Pr H H CH 2-indol-3-yl 'Pr H F H OH H H VI-23-7 'Pr H H CH 2CH2SCH 3 'Pr H F H OH H H VI-23-8 'Pr * H * 'Pr H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 Q _

Table VI-24. N9 R1 R2 R3 a R3 R4 R R' X Y R7 R' VI-24-1 'Bu H H H 'Pr H F H OH H H VI-24-2 'Bu H H CH 3 'Pr H F H OH H H VI-24-3 'Bu H H CH(CH3) 2 'Pr H F H OH H H VI-24-4 'Bu H H CH 2CH(CH3)2 'Pr H F H OH H H VI-24-5 'Bu H H CH 2Ph 'Pr H F H OH H H VI-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F H OH H H VI-24-7 'Bu H H CH 2CH2SCH 3 'Pr H F H OH H H VI-24-8 'Bu * H * 'Pr H F H OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table VI-25. No9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' VI-25-1 Ph H H H 'Pr H F H OH H H VI-25-2 Ph H H CH3 'Pr H F H OH H H VI-25-3 Ph H H CH(CH 3)2 'Pr H F H OH H H VI-25-4 Ph H H CH2CH(CH 3) 2 'Pr H F H OH H H VI-25-5 Ph H H CH 2Ph 'Pr H F H OH H H VI-25-6 Ph H H CH 2-indol-3-yl 'Pr H F H OH H H VI-25-7 Ph H H CH2CH2SCH 3 'Pr H F H OH H H VI-25-8 Ph * H * 'Pr H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-26. N R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' VI-26-1 p-Me-Ph H H H 'Pr H F H OH H H VI-26-2 p-Me-Ph H H CH 3 'Pr H F H OH H H VI-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H F H OH H H VI-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr H F H OH H H VI-26-5 p-Me-Ph H H CH 2Ph 'Pr H F H OH H H VI-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H VI-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H F H OH H H VI-26-8 p-Me-Ph * H * 'Pr H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-27. N9 R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' VI-27-1 p-F-Ph H H H 'Pr H F H OH H H VI-27-2 p-F-Ph H H CH3 'Pr H F H OH H H VI-27-3 p-F-Ph H H CH(CH3)2 'Pr H F H OH H H

1;O _

N9 Rl R2 R3 a R3 b R4 R' R' X Y R7 R' VI-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H F H OH H H VI-27-5 p-F-Ph H H CH 2Ph 'Pr H F H OH H H VI-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H VI-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H F H OH H H VI-27-8 p-F-Ph * H * 'Pr H F H OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table VI-28. N9 Rl R2 R 3 R 3 b R4 R R X Y R7 R' VI-28-1 p-Cl-Ph H H H Pr H F H OH H H VI-28-2 p-Cl-Ph H H CH 3 'Pr H F H OH H H VI-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F H OH H H VI-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr H F H OH H H VI-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F H OH H H VI-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H VI-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H F H OH H H VI-28-8 p-Cl-Ph * H * 'Pr H F H OH H H

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table VI-29. No9 Rl R2 R 3 R 3 b R4 R' R6 X Y R7 R' VI-29-1 p-Br-Ph H H H 'Pr H F H OH H H VI-29-2 p-Br-Ph H H CH3 'Pr H F H OH H H VI-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F H OH H H VI-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F H OH H H VI-29-5 p-Br-Ph H H CH 2Ph 'Pr H F H OH H H VI-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H VI-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F H OH H H VI-29-8 p-Br-Ph * H * 'Pr H F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VI-30. N9 Rl R2 R 3a R3b R4 R5 R6 X Y R7 R' VI-30-1 p-I-Ph H H H Pr H F H OH H H VI-30-2 p-I-Ph H H CH 3 'Pr H F H OH H H VI-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F H OH H H VI-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr H F H OH H H VI-30-5 p-I-Ph H H CH 2Ph 'Pr H F H OH H H VI-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H

1A _-

N9 Rl R2 R 3a R3 b R4 R' R' X Y R7 R' VI-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr H F H OH H H VI-30-8 p-I-Ph * H * 'Pr H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-31. N9 R R2 R3 a R3 b R4 R' R6 X Y R7 R' VI-31-1 CH 3 H H H "Bu H F H OH H H VI-31-2 CH 3 H H CH3 "Bu H F H OH H H VI-31-3 CH 3 H H CH(CH 3) 2 "Bu H F H OH H H VI-31-4 CH 3 H H CH2CH(CH 3)2 "Bu H F H OH H H VI-31-5 CH 3 H H CH 2Ph "Bu H F H OH H H VI-31-6 CH 3 H H CH 2-indol-3-yl "Bu H F H OH H H VI-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H F H OH H H VI-31-8 CH 3 * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-32. N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R'

VI-32-1 Et H H H "Bu H F H OH H H VI-32-2 Et H H CH3 "Bu H F H OH H H VI-32-3 Et H H CH(CH 3) 2 "Bu H F H OH H H VI-32-4 Et H H CH2CH(CH 3)2 "Bu H F H OH H H VI-32-5 Et H H CH2Ph "Bu H F H OH H H VI-32-6 Et H H CH2-indol-3-yl "Bu H F H OH H H VI-32-7 Et H H CH2CH 2SCH 3 "Bu H F H OH H H VI-32-8 Et * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-33. N9 R R2 R3a RS R4 R5 R 6 X Y R7 R' VI-33-1 'Pr H H H "Bu H F H OH H H VI-33-2 'Pr H H CH 3 "Bu H F H OH H H VI-33-3 'Pr H H CH(CH3) 2 "Bu H F H OH H H VI-33-4 'Pr H H CH 2CH(CH 3) 2 "Bu H F H OH H H VI-33-5 'Pr H H CH 2Ph "Bu H F H OH H H VI-33-6 'Pr H H CH 2-indol-3-yl "Bu H F H OH H H VI-33-7 'Pr H H CH 2CH2SCH 3 "Bu H F H OH H H VI-33-8 'Pr * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 11_

Table VI-34. N9 R1 R2 R3 a R3 R4 R R X Y R7 R' VI-34-1 'Bu H H H "Bu H F H OH H H VI-34-2 'Bu H H CH 3 "Bu H F H OH H H VI-34-3 'Bu H H CH(CH 3) 2 "Bu H F H OH H H VI-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H F H OH H H VI-34-5 'Bu H H CH 2Ph "Bu H F H OH H H VI-34-6 'Bu H H CH 2-indol-3-yl "Bu H F H OH H H VI-34-7 'Bu H H CH 2CH2SCH 3 "Bu H F H OH H H VI-34-8 'Bu * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-35. N R R 2 R 3 a RR R4 R R6 X Y R7 R VI-35-1 Ph H H H "Bu H F H OH H H VI-35-2 Ph H H CH3 "Bu H F H OH H H VI-35-3 Ph H H CH(CH 3)2 "Bu H F H OH H H VI-35-4 Ph H H CH2CH(CH 3) 2 "Bu H F H OH H H VI-35-5 Ph H H CH 2Ph "Bu H F H OH H H VI-35-6 Ph H H CH 2-indol-3-yl "Bu H F H OH H H VI-35-7 Ph H H CH2CH2SCH 3 "Bu H F H OH H H VI-35-8 Ph * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-36. N9 R1 R2 R 3a R3b R4 R 5 R' X Y R7 R' VI-36-1 p-Me-Ph H H H "Bu H F H OH H H VI-36-2 p-Me-Ph H H CH 3 "Bu H F H OH H H VI-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H F H OH H H VI-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H F H OH H H VI-36-5 p-Me-Ph H H CH 2Ph "Bu H F H OH H H VI-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F H OH H H VI-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F H OH H H VI-36-8 p-Me-Ph * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-37. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' VI-37-1 p-F-Ph H H H "Bu H F H OH H H VI-37-2 p-F-Ph H H CH3 "Bu H F H OH H H VI-37-3 p-F-Ph H H CH(CH 3) 2 "Bu H F H OH H H

1 )

No Rl R2 R3 a R3 b R4 R' R6 X Y R7 R' VI-37-4 p-F-Ph H H CH2CH(CH3) 2 "Bu H F H OH H H VI-37-5 p-F-Ph H H CH 2Ph "Bu H F H OH H H VI-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F H OH H H VI-37-7 p-F-Ph H H CH2CH 2SCH 3 "Bu H F H OH H H VI-37-8 p-F-Ph * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1A2-I

Table VI-38. N RR 2 R 3 a R3 R4 R 5 R' X Y R7 R' VI-38-1 p-Cl-Ph H H H "Bu H F H OH H H VI-38-2 p-Cl-Ph H H CH 3 "Bu H F H OH H H VI-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F H OH H H VI-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H F H OH H H VI-38-5 p-Cl-Ph H H CH 2Ph "Bu H F H OH H H VI-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F H OH H H VI-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H F H OH H H VI-38-8 p-Cl-Ph * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-39. N9 R1 R2 R 3a R3 b R4 R' R6 X Y R7 R VI-39-1 p-Br-Ph H H H "Bu H F H OH H H VI-39-2 p-Br-Ph H H CH3 "Bu H F H OH H H VI-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H F H OH H H VI-39-4 p-Br-Ph H H CH2 CH(CH3) 2 "Bu H F H OH H H VI-39-5 p-Br-Ph H H CH 2 Ph "Bu H F H OH H H VI-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F H OH H H VI-39-7 p-Br-Ph H H CH2 CH 2 SCH 3 "Bu H F H OH H H VI-39-8 p-Br-Ph * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VI-40. N9 R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' VI-40-1 p-I-Ph H H H "Bu H F H OH H H VI-40-2 p-I-Ph H H CH 3 "Bu H F H OH H H VI-40-3 p-I-Ph H H CH(CH3) 2 "Bu H F H OH H H VI-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu H F H OH H H VI-40-5 p-I-Ph H H CH 2 Ph "Bu H F H OH H H VI-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F H OH H H VI-40-7 p-I-Ph H H CH 2 CH 2 SCH 3 "Bu H F H OH H H VI-40-8 p-I-Ph * H * "Bu H F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 A/

Table VI-41. N9 R1 R2 R3 a R3b R4 R' R' X Y R7 R' VI-41-1 CH 3 H H H Bz H F H OH H H VI-41-2 CH 3 H H CH3 Bz H F H OH H H VI-41-3 CH 3 H H CH(CH3) 2 Bz H F H OH H H VI-41-4 CH 3 H H CH2CH(CH3) 2 Bz H F H OH H H VI-41-5 CH 3 H H CH 2Ph Bz H F H OH H H VI-41-6 CH 3 H H CH 2-indol-3-yl Bz H F H OH H H VI-41-7 CH 3 H H CH2CH 2SCH 3 Bz H F H OH H H VI-41-8 CH 3 * H * Bz H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-42. N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' VI-42-1 Et H H H Bz H F H OH H H VI-42-2 Et H H CH3 Bz H F H OH H H VI-42-3 Et H H CH(CH3) 2 Bz H F H OH H H VI-42-4 Et H H CH2CH(CH3) 2 Bz H F H OH H H VI-42-5 Et H H CH2Ph Bz H F H OH H H VI-42-6 Et H H CH2-indol-3-yl Bz H F H OH H H VI-42-7 Et H H CH2CH 2SCH 3 Bz H F H OH H H VI-42-8 Et * H * Bz H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-43. N9 R1 R2 R3 a Rb R4 R 5 R6 X Y R7 R' VI-43-1 'Pr H H H Bz H F H OH H H VI-43-2 Pr H H CH 3 Bz H F H OH H H VI-43-3 'Pr H H CH(CH3) 2 Bz H F H OH H H VI-43-4 'Pr H H CH 2CH(CH3)2 Bz H F H OH H H VI-43-5 'Pr H H CH 2Ph Bz H F H OH H H VI-43-6 'Pr H H CH 2-indol-3-yl Bz H F H OH H H VI-43-7 'Pr H H CH 2CH2SCH 3 Bz H F H OH H 11M VI-43-8 'Pr * H * Bz H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 1r,

Table VI-44. N9 R1 R2 R3 a R3 R4 R R6 X Y R7 R' VI-44-1 'Bu H H H Bz H F H OH H H VI-44-2 'Bu H H CH 3 Bz H F H OH H H VI-44-3 'Bu H H CH(CH3) 2 Bz H F H OH H H VI-44-4 'Bu H H CH 2CH(CH3)2 Bz H F H OH H H VI-44-5 'Bu H H CH 2Ph Bz H F H OH H H VI-44-6 'Bu H H CH 2-indol-3-yl Bz H F H OH H H VI-44-7 'Bu H H CH 2CH2SCH 3 Bz H F H OH H H VI-44-8 'Bu * H * Bz H F H OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table VI-45. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' VI-45-1 Ph H H H Bz H F H OH H H VI-45-2 Ph H H CH3 Bz H F H OH H H VI-45-3 Ph H H CH(CH3) 2 Bz H F H OH H H VI-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH H H VI-45-5 Ph H H CH 2Ph Bz H F H OH H H VI-45-6 Ph H H CH 2-indol-3-yl Bz H F H OH H H VI-45-7 Ph H H CH2CH2SCH 3 Bz H F H OH H H VI-45-8 Ph * H * Bz H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-46. N9 R1 R2 R 3a R3b R4 R5 R' X Y R7 R' VI-46-1 p-Me-Ph H H H Bz H F H OH H H VI-46-2 p-Me-Ph H H CH 3 Bz H F H OH H H VI-46-3 p-Me-Ph H H CH(CH 3)2 Bz H F H OH H H VI-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz H F H OH H H VI-46-5 p-Me-Ph H H CH 2Ph Bz H F H OH H H VI-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F H OH H H VI-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H F H OH H H VI-46-8 p-Me-Ph * H * Bz H F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1AA-

Table VI-47. N9 R1 R2 R3a R3b R4 R 5 R6 X Y R7 R' VI-47-1 p-F-Ph H H H Bz H F H OH H H VI-47-2 p-F-Ph H H CH3 Bz H F H OH H H VI-47-3 p-F-Ph H H CH(CH 3) 2 Bz H F H OH H H VI-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H F H OH H H VI-47-5 p-F-Ph H H CH 2Ph Bz H F H OH H H VI-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F H OH H H VI-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H F H OH H H VI-47-8 p-F-Ph * H * Bz H F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VI-48. N9 R1 R2 R 3 a R3 b R4 R R 6 X Y R7 R' VI-48-1 p-Cl-Ph H H H Bz H F H OH H H VI-48-2 p-Cl-Ph H H CH 3 Bz H F H OH H H VI-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F H OH H H VI-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H F H OH H H VI-48-5 p-Cl-Ph H H CH 2Ph Bz H F H OH H H VI-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F H OH H H VI-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H F H OH H H VI-48-8 p-Cl-Ph * H * Bz H F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VI-49. 5 6 N9 R1 R 2 R 3a R 3b R4 R R X Y R7 R' VI-49-1 p-Br-Ph H H H Bz H F H OH H H VI-49-2 p-Br-Ph H H CH3 Bz H F H OH H H VI-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F H OH H H VI-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H F H OH H H VI-49-5 p-Br-Ph H H CH 2Ph Bz H F H OH H H VI-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F H OH H H VI-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F H OH H H VI-49-8 p-Br-Ph * H * Bz H F H OH H H

*R2 and R 3b joined together by (CH2)3 to form five-membered ring.

1r7l_

Table VI-50. N9 Rl R2 R 3a R3b R4 R5 R6 X Y R7 R' VI-50-1 p-I-Ph H H H Bz H F H OH H H VI-50-2 p-I-Ph H H CH 3 Bz H F H OH H H VI-50-3 p-I-Ph H H CH(CH 3)2 Bz H F H OH H H VI-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz H F H OH H H VI-50-5 p-I-Ph H H CH 2Ph Bz H F H OH H H VI-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F H OH H H VI-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H F H OH H H VI-50-8 p-I-Ph * H * Bz H F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

R9

R8

Rt 2 0 R3b R 7 N 0 R3a N-P--OOSR

CO2R4 OR 1 R R6

Y X VII

Table VII-1. No9 R R2 R 3a R3 b R4 R 5 R6 X Y R7 R' R9 VII-1-1 CH 3 H H H CH3 H F H OH H H NH 2 VII-1-2 CH 3 H H CH3 CH3 H F H OH H H NH 2 VII-1-3 CH 3 H H CH(CH 3)2 CH3 H F H OH H H NH 2 VII-1-4 CH 3 H H CH2CH(CH3) 2 CH3 H F H OH H H NH 2 VII-1-5 CH 3 H H CH 2Ph CH3 H F H OH H H NH 2 VII-1-6 CH 3 H H CH 2-indol-3-yl CH3 H F H OH H H NH 2 VII-1-7 CH 3 H H CH2CH 2SCH 3 CH3 H F H OH H H NH 2 VII-1-8 CH 3 * H * CH3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-2. N9 Rl R2 R 3a R3b R4 R 5 R6 X Y R7 R' R9 VII-2-1 Et H H H CH 3 H F H OH H H NH 2

1A _Q

N9 Rl R2 R 3a R3 b R4 R' R6 X Y R7 R' R9 VII-2-2 Et H H CH3 CH 3 H F H OH H H NH 2 VII-2-3 Et H H CH(CH 3)2 CH 3 H F H OH H H NH 2 VII-2-4 Et H H CH2CH(CH 3)2 CH 3 H F H OH H H NH 2 VII-2-5 Et H H CH 2Ph CH 3 H F H OH H H NH 2 VII-2-6 Et H H CH 2-indol-3-yl CH 3 H F H OH H H NH 2 VII-2-7 Et H H CH2CH 2SCH 3 CH 3 H F H OH H H NH 2 VII-2-8 Et * H * CH 3 H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VII-3. No9 R' R2 R 3a R3b R4 R R 6 X Y R7 R' R9 VII-3-1 'Pr H H H CH 3 H F H OH H H NH 2 VII-3-2 'Pr H H CH 3 CH 3 H F H OH H H NH 2 VII-3-3 'Pr H H CH(CH 3)2 CH3 H F H OH H H NH 2 VII-3-4 'Pr H H CH 2CH(CH 3) 2 CH3 H F H OH H H NH 2 VII-3-5 Pr H H CH 2Ph CH 3 H F H OH H H NH 2 VII-3-6 Pr H H CH 2-indol-3-yl CH3 H F H OH H H NH 2 VII-3-7 Pr H H CH 2CH2SCH 3 CH3 H F H OH H H NH 2 VII-3-8 iPr * H * CH 3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VII-4. No9 R' R2 R3 a R3 b R4 R R 6 X Y R7 R' R9 VII-4-1 'Bu H H H CH 3 H F H OH H H NH 2 VII-4-2 'Bu H H CH 3 CH 3 H F H OH H H NH 2 VII-4-3 'Bu H H CH(CH 3) 2 CH 3 H F H OH H H NH 2 VII-4-4 'Bu H H CH 2CH(CH 3) 2 CH 3 H F H OH H H NH 2 VII-4-5 'Bu H H CH 2Ph CH 3 H F H OH H H NH 2 VII-4-6 'Bu H H CH 2-indol-3-yl CH 3 H F H OH H H NH 2 VII-4-7 'Bu H H CH 2CH 2SCH 3 CH 3 H F H OH H H NH 2 VII-4-8 'Bu * H * CH 3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

1 AO_

Table VII-5. M9 R1 R2 R3 a R3 R4 R 5 R' X Y R7 R' R9 VII-5-1 Ph H H H CH 3 H F H OH H H NH 2 VII-5-2 Ph H H CH3 CH 3 H F H OH H H NH 2 VII-5-3 Ph H H CH(CH3) 2 CH 3 H F H OH H H NH 2 VII-5-4 Ph H H CH2CH(CH 3) 2 CH 3 H F H OH H H NH 2 VII-5-5 Ph H H CH 2Ph CH 3 H F H OH H H NH 2 VII-5-6 Ph H H CH 2-indol-3-yl CH 3 H F H OH H H NH 2 VII-5-7 Ph H H CH2CH2SCH 3 CH 3 H F H OH H H NH 2 VII-5-8 Ph * H * CH 3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-6. 9 R1 R 2 R 3 a RS R4 R 5 R 6 X Y R7 R' R9 VII-6-1 p-Me-Ph H H H CH 3 H F H OH H H NH 2 VII-6-2 p-Me-Ph H H CH 3 CH 3 H F H OH H H NH 2 VII-6-3 p-Me-Ph H H CH(CH3) 2 CH 3 H F H OH H H NH 2 VII-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH 3 H F H OH H H NH 2 VII-6-5 p-Me-Ph H H CH 2Ph CH 3 H F H OH H H NH 2 VII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 H F H OH H H NH 2 VII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH 3 H F H OH H H NH 2 VII-6-8 p-Me-Ph * H * CH 3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-7. o R1 R2 R3 a R 3b R4 R 5 R 6 X Y R7 R' R9 VII-7-1 p-F-Ph H H H CH3 H F H OH H H NH 2 VII-7-2 p-F-Ph H H CH 3 CH3 H F H OH H H NH 2 VII-7-3 p-F-Ph H H CH(CH3) 2 CH3 H F H OH H H NH 2 VII-7-4 p-F-Ph H H CH 2CH(CH3) 2 CH3 H F H OH H H NH 2 VII-7-6 p-F-Ph H H CH 2Ph CH3 H F H OH H H NH 2 VII-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F H OH H H NH 2 VII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 H F H OH H H NH 2 VII-7-20 p-F-Ph * H * CH3 H F H OH H H NH 2 *R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

Table VII-8. 9 R1 R 2 R 3a R3 b R4 R 5 R 6 X Y R7 R' R9 VII-8-1 p-Cl-Ph H H H CH3 H F H OH H H NH 2 VII-8-2 p-Cl-Ph H H CH3 CH 3 H F H OH H H NH 2 VII-8-3 p-Cl-Ph H H CH(CH3) 2 CH3 H F H OH H H NH 2

1'70 _

N Rl R2 R 3a R3 b R4 R 5 R' X Y R7 R' R9 VII-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH 3 H F H OH H H NH 2 VII-8-5 p-Cl-Ph H H CH2Ph CH 3 H F H OH H H NH 2 VII-8-6 p-Cl-Ph H H CH2-indol-3-yl CH 3 H F H OH H H NH 2 VII-8-7 p-Cl-Ph H H CH2CH 2SCH 3 CH 3 H F H OH H H NH 2 VII-8-8 p-Cl-Ph * H * CH 3 H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VII-9. No R R2 R 3 a R 3b R4 R' R6 X Y R7 R' R9 VII-9-1 p-Br-Ph H H H CH 3 H F H OH H H NH 2 VII-9-2 p-Br-Ph H H CH3 CH 3 H F H OH H H NH 2 VII-9-3 p-Br-Ph H H CH(CH 3) 2 CH 3 H F H OH H H NH 2 VII-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH 3 H F H OH H H NH 2 VII-9-6 p-Br-Ph H H CH 2Ph CH 3 H F H OH H H NH 2 VII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H F H OH H H NH 2 VII-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 H F H OH H H NH 2 VII-9-20 p-Br-Ph * H * CH 3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VII-10. No Rl R2 R3a R3 b R4 R R 6 X Y R7 R' R9 VII-10-1 p-I-Ph H H H CH 3 H F H OH H H NH 2 VII-10-2 p-I-Ph H H CH3 CH 3 H F H OH H H NH 2 VII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H F H OH H H NH 2 VII-10-4 p-I-Ph H H CH2CH(CH3) 2 CH 3 H F H OH H H NH 2 VII-10-5 p-I-Ph H H CH2Ph CH 3 H F H OH H H NH 2 VII-10-6 p-I-Ph H H CH2-indol-3-yl CH 3 H F H OH H H NH 2 VII-10-7 p-I-Ph H H CH2CH 2SCH 3 CH 3 H F H OH H H NH 2 VII-10-8 p-I-Ph * H * CH 3 H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

1'71 _

Table VII-11. No R1 R2 R3 a R 3b R4 R' R6 X Y R7 R' R9 VII-11-1 CH3 H H H Et H F H OH H H NH 2 VII-11-2 CH3 H H CH3 Et H F H OH H H NH 2 VII-11-3 CH 3 H H CH(CH 3) 2 Et H F H OH H H NH 2 VII-11-4 CH 3 H H CH2CH(CH3) 2 Et H F H OH H H NH 2 VII-11-5 CH 3 H H CH 2Ph Et H F H OH H H NH 2 VII-11-6 CH 3 H H CH 2-indol-3-yl Et H F H OH H H NH 2 VII-11-7 CH 3 H H CH2CH2 SCH3 Et H F H OH H H NH 2 VII-11-8 CH 3 * H * EtH F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-12. N9 R1 R2 R3a R3 b R4 R' R6 X Y R7 R' R9 VII-12-1 Et H H H Et H F H OH H H NH 2 VII-12-2 Et H H CH3 Et H F H OH H H NH 2 VII-12-3 Et H H CH(CH3) 2 Et H F H OH H H NH 2 VII-12-4 Et H H CH2CH(CH 3) 2 Et H F H OH H H NH 2 VII-12-5 Et H H CH 2Ph Et H F H OH H H NH 2 VII-12-6 Et H H CH 2-indol-3-yl Et H F H OH H H NH 2 VII-12-7 Et H H CH2CH 2SCH3 Et H F H OH H H NH 2 VII-12-8 Et * H * FtH F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-13. N9 RI R 22 R3 a R3b R 4 R 5 R6 X Y R7 R' R9 VII-13-1 'Pr H H H Et H F H OH H H NH 2 VII-13-2 'Pr H H CH 3 Et H F H OH H H NH 2 VII-13-3 'Pr H H CH(CH3) 2 Et H F H OH H H NH 2 VII-13-4 'Pr H H CH 2CH(CH3) 2 Et H F H OH H H NH 2 VII-13-5 Pr H H CH 2Ph Et H F H OH H H NH 2 VII-13-6 Pr H H CH 2-indol-3-yl Et H F H OH H H NH 2 VII-13-7 Pr H H CH 2CH2SCH 3 Et H F H OH H H NH 2 VII-13-8 Pr * H * FtH F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1'7) _

Table VII-14. M R1 R2 R R3b R4 R5 R6 X Y R7 R' R9 3a

VII- 'Bu H H H Et H F H OH H H NH 2 14-1 VII- 'Bu H H CH 3 Et H F H OH H H NH 2 14-2 VII- 'Bu H H CH(CH3) 2 Et H F H OH H H NH 2 14-3 VII- 'Bu H H CH 2CH(CH 3) 2 Et H F H OH H H NH 2 14-4 VII- 'Bu H H CH 2Ph Et H F H OH H H NH 2 14-5 VII- 'Bu H H CH 2-indol-3-yl Et H F H OH H H NH 2 14-6 VII- 'Bu H H CH 2CH2SCH 3 Et H F H OH H H NH 2 14-7 VII- 'Bu* H * FtH F H OH H H NH 2 14-8 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-15. No RI R2 R 3a R 3b R 4 R 6 X Y R7 R' R9 VII-15-1 Ph H H H Et H F H OH H H NH 2 VII-15-2 Ph H H CH3 Et H F H OH H H NH 2 VII-15-3 Ph H H CH(CH3) 2 Et H F H OH H H NH 2 VII-15-4 Ph H H CH2CH(CH3) 2 Et H F H OH H H NH 2 VII-15-5 Ph H H CH2Ph Et H F H OH H H NH 2 VII-15-6 Ph H H CH2-indol-3-yl Et H F H OH H H NH 2 VII-15-7 Ph H H CH2CH2SCH 3 Et H F H OH H H NH 2 VII-15-8 Ph * H * FtH F H OH H H NH 2 *R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

Table VII-16. o R1 R2 R3 a R3 b R 4 RR6 X Y R7 R' R9

VII-16-1 p-Me-Ph H H H Et H F H OH H H NH 2 VII-16-2 p-Me-Ph H H CH3 Et H F H OH H H NH 2 VII-16-3 p-Me-Ph H H CH(CH3) 2 Et H F H OH H H NH 2 VII-16-4 p-Me-Ph H H CH2CH(CH3) 2 Et H F H OH H H NH 2 VII-16-5 p-Me-Ph H H CH2Ph Et H F H OH H H NH 2

1 '7'1

No Rl R2 R3 a R3 b R 4 R' R X Y R7 R' R9 VII-16-6 p-Me-Ph H H CH2-indol-3-yl Et H F H OH H H NH 2 VII-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H F H OH H H NH 2 VII-16-8 p-Me-Ph * H * Et H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-17. No Rl R2 R3 a R3 b R 4 R R 6 X Y R7 R' R9 VII-17-1 p-F-Ph H H H Et H F H OH H H NH 2 VII-17-2 p-F-Ph H H CH 3 Et H F H OH H H NH 2 VII-17-3 p-F-Ph H H CH(CH3) 2 Et H F H OH H H NH 2 VII-17-4 p-F-Ph H H CH 2CH(CH3) 2 Et H F H OH H H NH 2 VII-17-5 p-F-Ph H H CH 2Ph Et H F H OH H H NH 2 VII-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F H OH H H NH 2 VII-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H F H OH H H NH 2 VII-17-8 p-F-Ph * H * Et H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-18. 6 No R R2 R 3 a R3 b R4 R 5 R X Y R7 R' R9 VII-18-1 p-Cl-Ph H H H Et H F H OH H H NH 2 VII-18-2 p-Cl-Ph H H CH3 Et H F H OH H H NH 2 VII-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F H OH H H NH 2 VII-18-4 p-Cl-Ph H H CH2CH(CH3) 2 Et H F H OH H H NH 2 VII-18-5 p-Cl-Ph H H CH 2Ph Et H F H OH H H NH 2 VII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F H OH H H NH 2 VII-18-7 p-Cl-Ph H H CH2CH 2SCH 3 Et H F H OH H H NH 2 VII-18-8 p-Cl-Ph * H * Et H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VII-19. No R R2 R 3 a R3 b R4 R 5 R 6 X Y R7 R' R9 VII-19-1 p-Br-Ph H H H Et H F H OH H H NH 2 VII-19-2 p-Br-Ph H H CH3 Et H F H OH H H NH 2 VII-19-3 p-Br-Ph H H CH(CH 3) 2 Et H F H OH H H NH 2 VII-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H F H OH H H NH 2 VII-19-5 p-Br-Ph H H CH 2Ph Et H F H OH H H NH 2 VII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F H OH H H NH 2 VII-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H F H OH H H NH 2 VII-19-8 p-Br-Ph * H * Et H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1'7/A-

Table VII-20. No R RR3 R 3b R 4 R R' X Y R7 R' R9 VII-20-1 p-I-Ph H H H Et H F H OH H H NH 2 VII-20-2 p-I-Ph H H CH3 Et H F H OH H H NH 2 VII-20-3 p-I-Ph H H CH(CH3) 2 Et H F H OH H H NH 2 VII-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H F H OH H H NH 2 VII-20-5 p-I-Ph H H CH2Ph Et H F H OH H H NH 2 VII-20-6 p-I-Ph H H CH2-indol-3-yl Et H F H OH H H NH 2 VII-20-7 p-I-Ph H H CH2 CH 2 SCH 3 Et H F H OH H H NH 2 VII-20-8 p-I-Ph * H * Et H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-21. No9 R1 R2 R 3a R3 b R4 R' R 6 X Y R7 R' R9 VII-21-1 CH3 H H H 'Pr H F H OH H H NH 2 VII-21-2 CH3 H H CH3 'Pr H F H OH H H NH 2 VII-21-3 CH3 H H CH(CH 3) 2 'Pr H F H OH H H NH 2 VII-21-4 CH3 H H CH2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-21-5 CH3 H H CH 2Ph 'Pr H F H OH H H NH 2 VII-21-6 CH3 H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-21-7 CH3 H H CH2CH2 SCH3 'Pr H F H OH H H NH 2 VII-21-8 CH3 * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-22. No Rl R 2 R3 a R 3b R4 R5 R6 X Y R7 R' R9 VII-22-1 Et H H H 'Pr H F H OH H H NH 2 VII-22-2 Et H H CH3 'Pr H F H OH H H NH 2 VII-22-3 Et H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-22-4 Et H H CH2CH(CH 3) 2 'Pr H F H OH H H NH 2 VII-22-5 Et H H CH 2Ph 'Pr H F H OH H H NH 2 VII-22-6 Et H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-22-7 Et H H CH2CH 2SCH3 'Pr H F H OH H H NH 2 VII-22-8 Et * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-23. No9 R1 R2 R3 a R 3b R5 R6 X Y R7 R' R9 VII-23-1 tPr H H H 'Pr H F H OH H H NH 2 VII-23-2 'Pr H H CH 3 'Pr H F H OH H H NH 2 VII-23-3 'Pr H H CH(CH3) 2 'Pr H F H OH H H NH 2

_1'7 _

No R R2 R3 aRb R4 R 5 R6 X Y R7 R' R9 VII-23-4 'Pr H H CH 2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-23-5 'Pr H H CH 2Ph 'Pr H F H OH H H NH 2 VII-23-6 'Pr H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-23-7 'Pr H H CH 2CH2SCH 3 'Pr H F H OH H H NH 2 VII-23-8 Pr * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-24. No R R2 R3 a R3b R4 R 5 R6 X Y R7 R' R9 VII-24-1 'Bu H H H 'Pr H F H OH H H NH 2 VII-24-2 'Bu H H CH 3 'Pr H F H OH H H NH 2 VII-24-3 'Bu H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-24-5 'Bu H H CH 2Ph 'Pr H F H OH H H NH 2 VII-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H F H OH H H NH 2 VII-24-8 'Bu * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-25. No9 R R2 R3a R3 b R4 R 5 R6 X Y R7 R' R9 VII-25-1 Ph H H H 'Pr H F H OH H H NH 2 VII-25-2 Ph H H CH3 'Pr H F H OH H H NH 2 VII-25-3 Ph H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-25-4 Ph H H CH2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-25-5 Ph H H CH2Ph 'Pr H F H OH H H NH 2 VII-25-6 Ph H H CH2-indol-3-yl 'Pr H F H OH H H NH 2 VII-25-7 Ph H H CH2CH2SCH 3 'Pr H F H OH H H NH 2 VII-25-8 Ph * H * 'Pr H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1'7A _

Table VII-26. No R R2 RaR 3 b 4 R 5 R6 X Y R7 R' R9 VII-26-1 p-Me-Ph H H H 'Pr H F H OH H H NH 2 VII-26-2 p-Me-Ph H H CH3 'Pr H F H OH H H NH 2 VII-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-26-4 p-Me-Ph H H CH2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-26-5 p-Me-Ph H H CH2Ph 'Pr H F H OH H H NH 2 VII-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr H F H OH H H NH 2 VII-26-7 p-Me-Ph H H CH2CH2SCH 3 'Pr H F H OH H H NH 2 VII-26-8 p-Me-Ph * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-27. No9 R1 R2 R3 a R3 b R4 R R 6 X Y R7 R' R9 VII-27-1 p-F-Ph H H H 'Pr H F H OH H H NH 2 VII-27-2 p-F-Ph H H CH 3 'Pr H F H OH H H NH 2 VII-27-3 p-F-Ph H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-27-4 p-F-Ph H H CH 2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-27-5 p-F-Ph H H CH 2Ph 'Pr H F H OH H H NH 2 VII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H F H OH H H NH 2 VII-27-8 p-F-Ph * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-28. No R1 R2 R3a R3b R4 R 5 R6 X Y R7 R' R9 VII-28-1 p-Cl-Ph H H H 'Pr H F H OH H H NH 2 VII-28-2 p-Cl-Ph H H CH3 'Pr H F H OH H H NH 2 VII-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-28-4 p-Cl-Ph H H CH2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F H OH H H NH 2 VII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr H F H OH H H NH 2 VII-28-8 p-Cl-Ph * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VII-29. No R R2 R3a R3 b R4 R 5 R6 X Y R7 R' R9 VII-29-1 p-Br-Ph H H H 'Pr H F H OH H H NH 2 VII-29-2 p-Br-Ph H H CH3 'Pr H F H OH H H NH 2 VII-29-3 p-Br-Ph H H CH(CH 3) 2 'Pr H F H OH H H NH 2

1 '77

No R RR 3 a R3 b R4 R' R' X Y R7 R' R9 VII-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-29-5 p-Br-Ph H H CH 2Ph 'Pr H F H OH H H NH 2 VII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F H OH H H NH 2 VII-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F H OH H H NH 2 VII-29-8 p-Br-Ph * H * 'Pr H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-30. No R R2 R3 a R 3b R4 R R X Y R7 R' R9 VII-30-1 p-I-Ph H H H 'Pr H F H OH H H NH 2 VII-30-2 p-I-Ph H H CH3 'Pr H F H OH H H NH 2 VII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F H OH H H NH 2 VII-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H F H OH H H NH 2 VII-30-5 p-I-Ph H H CH2Ph 'Pr H F H OH H H NH 2 VII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr H F H OH H H NH 2 VII-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H F H OH H H NH 2 VII-30-8 p-I-Ph * H * 'Pr H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1'72 _

Table VII-31. No R1 R2 R3 a R 3b R4 R' R6 X Y R7 R' R9 VII-31-1 CH3 H H H "Bu H F H OH H H NH 2 VII-31-2 CH3 H H CH3 "Bu H F H OH H H NH 2 VII-31-3 CH3 H H CH(CH 3) 2 "Bu H F H OH H H NH 2 VII-31-4 CH3 H H CH2CH(CH3) 2 "Bu H F H OH H H NH 2 VII-31-5 CH3 H H CH 2Ph "Bu H F H OH H H NH 2 VII-31-6 CH3 H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-31-7 CH3 H H CH2CH2 SCH3 "Bu H F H OH H H NH 2 VII-31-8 CH3 * H * "Bu H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-32. No R1 R2 R3a R3 b R4 R' R6 X Y R7 R' R9 VII-32-1 Et H H H "Bu H F H OH H H NH 2 VII-32-2 Et H H CH3 "Bu H F H OH H H NH 2 VII-32-3 Et H H CH(CH3) 2 "Bu H F H OH H H NH 2 VII-32-4 Et H H CH2CH(CH 3) 2 "Bu H F H OH H H NH 2 VII-32-5 Et H H CH 2Ph "Bu H F H OH H H NH 2 VII-32-6 Et H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-32-7 Et H H CH2CH 2SCH3 "Bu H F H OH H H NH 2 VII-32-8 Et * H * "Bu H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-33. N9 RI R2 R3 a R3b R4 R R X Y R7 R' R9 VII-33-1 'Pr H H H "Bu H F H OH H H NH 2 VII-33-2 'Pr H H CH 3 "Bu H F H OH H H NH 2 VII-33-3 'Pr H H CH(CH3) 2 "Bu H F H OH H H NH 2 VII-33-4 'Pr H H CH 2CH(CH3) 2 "Bu H F H OH H H NH 2 VII-33-5 Pr H H CH 2Ph "Bu H F H OH H H NH 2 VII-33-6 Pr H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-33-7 Pr H H CH 2CH2SCH 3 "Bu H F H OH H H NH 2 VII-33-8 Pr * H * "Bu H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

170 _

Table VII-34. No R1 R2 R3 a R3b R4 R' R' X Y R7 R' R9 VII-34-1 'Bu H H H "Bu H F H OH H H NH 2 VII-34-2 'Bu H H CH 3 "Bu H F H OH H H NH 2 VII-34-3 'Bu H H CH(CH 3)2 "Bu H F H OH H H NH 2 VII-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H F H OH H H NH 2 VII-34-5 'Bu H H CH 2Ph "Bu H F H OH H H NH 2 VII-34-6 'Bu H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F H OH H H NH 2 VII-34-8 'Bu * H * "Bu H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VII-35. No R' R2 R3a R3 b R4 R R6 X Y R7 R' R9 VII-35-1 Ph H H H "Bu H F H OH H H NH 2 VII-35-2 Ph H H CH3 "Bu H F H OH H H NH 2 VII-35-3 Ph H H CH(CH3) 2 "Bu H F H OH H H NH 2 VII-35-4 Ph H H CH2CH(CH 3) 2 "Bu H F H OH H H NH 2 VII-35-5 Ph H H CH2Ph "Bu H F H OH H H NH 2 VII-35-6 Ph H H CH2-indol-3-yl "Bu H F H OH H H NH 2 VII-35-7 Ph H H CH2CH2SCH 3 "Bu H F H OH H H NH 2 VII-35-8 Ph * H * "Bu H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VII-36. o R1 R2 R 3 a R3 b R4 R 5 R 6 X Y R7 R' R9 VII-36-1 p-Me-Ph H H H "Bu H F H OH H H NH 2

VII-36-2 p-Me-Ph H H CH3 "Bu H F H OH H H NH 2 VII-36-3 p-Me-Ph H H CH(CH3) 2 "Bu H F H OH H H NH 2 VII-36-4 p-Me-Ph H H CH2CH(CH 3) 2 "Bu H F H OH H H NH 2 VII-36-5 p-Me-Ph H H CH2Ph "Bu H F H OH H H NH 2 VII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu H F H OH H H NH 2 VII-36-7 p-Me-Ph H H CH2CH 2SCH 3 "Bu H F H OH H H NH 2 VII-36-8 p-Me-Ph * H * "Bu H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VII-37. o R1 R2 R 3 a Rb R4 R 5 R6 X Y R7 R' R9 VII-37-1 p-F-Ph H H H "Bu H F H OH H H NH 2 VII-37-2 p-F-Ph H H CH 3 "Bu H F H OH H H NH 2 VII-37-3 p-F-Ph H H CH(CH 3)2 "Bu H F H OH H H NH 2

_12fl_

No R R RlaRlb R4 R' R' X Y R7 R' R9 VII-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H F H OH H H NH 2 VII-37-5 p-F-Ph H H CH 2Ph "Bu H F H OH H H NH 2 VII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F H OH H H NH 2 VII-37-8 p-F-Ph * H * "Bu H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-38. No R R 2 R 3a R 3b R4 R' R6 X Y R7 R' R9 VII-38-1 p-Cl-Ph H H H "Bu H F H OH H H NH 2 VII-38-2 p-Cl-Ph H H CH3 "Bu H F H OH H H NH 2 VII-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F H OH H H NH 2 VII-38-4 p-Cl-Ph H H CH2 CH(CH3) 2 "Bu H F H OH H H NH 2 VII-38-5 p-Cl-Ph H H CH 2 Ph "Bu H F H OH H H NH 2 VII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H F H OH H H NH 2 VII-38-8 p-Cl-Ph * H * "Bu H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VII-39. No R R 2 R 3a R3 b R4 R' R6 X Y R7 R' R9 VII-39-1 p-Br-Ph H H H "Bu H F H OH H H NH 2 VII-39-2 p-Br-Ph H H CH3 "Bu H F H OH H H NH 2 VII-39-3 p-Br-Ph H H CH(CH 3) 2 "Bu H F H OH H H NH 2 VII-39-4 p-Br-Ph H H CH2CH(CH3) 2 "Bu H F H OH H H NH 2 VII-39-5 p-Br-Ph H H CH 2Ph "Bu H F H OH H H NH 2 VII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F H OH H H NH 2 VII-39-7 p-Br-Ph H H CH2CH 2 SCH 3 "Bu H F H OH H H NH 2 VII-39-8 p-Br-Ph * H * "Bu H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VII-40. No Rl R2 R3a R 3b R4 R 5 R 6 X Y R7 R' R9 VII-40-1 p-I-Ph H H H "Bu H F H OH H H NH 2 VII-40-2 p-I-Ph H H CH3 "Bu H F H OH H H NH 2 VII-40-3 p-I-Ph H H CH(CH3) 2 "Bu H F H OH H H NH 2 VII-40-4 p-I-Ph H H CH2CH(CH3) 2 "Bu H F H OH H H NH 2 VII-40-5 p-I-Ph H H CH2Ph "Bu H F H OH H H NH 2 VII-40-6 p-I-Ph H H CH2-indol-3-yl "Bu H F H OH H H NH 2

121 _

No R R RlaRlb R4 R' R' X Y R7 R' R9 VII-40-7 p-I-Ph H H CH2CH 2SCH 3 "Bu H F H OH H H NH 2 VII-40-8 p-I-Ph * H * "Bu H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-41. No R R2 R 3a R3 b R4 R 5 R' X Y R7 R' R9 VII-41-1 CH3 H H H Bz H F H OH H H NH 2 VII-41-2 CH3 H H CH3 Bz H F H OH H H NH 2 VII-41-3 CH3 H H CH(CH 3) 2 Bz H F H OH H H NH 2 VII-41-4 CH3 H H CH2CH(CH3) 2 Bz H F H OH H H NH 2 VII-41-5 CH3 H H CH 2Ph Bz H F H OH H H NH 2 VII-41-6 CH3 H H CH 2-indol-3-yl Bz H F H OH H H NH 2 VII-41-7 CH3 H H CH2CH2 SCH3 Bz H F H OH H H NH 2 VII-41-8 CH3 * H * Bz H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1 Q')

Table VII-42. No Rl R2 R3 a R 3b R4 R' R6 X Y R7 R' R9 VII-42-1 Et H H H Bz H F H OH H H NH 2 VII-42-2 Et H H CH3 Bz H F H OH H H NH 2 VII-42-3 Et H H CH(CH3) 2 Bz H F H OH H H NH 2 VII-42-4 Et H H CH2CH(CH 3) 2 Bz H F H OH H H NH 2 VII-42-5 Et H H CH 2Ph Bz H F H OH H H NH 2 VII-42-6 Et H H CH 2-indol-3-yl Bz H F H OH H H NH 2 VII-42-7 Et H H CH2CH 2SCH3 Bz H F H OH H H NH 2 VII-42-8 Et * H * Bz H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-43. No R1 R2 R3 a Rb 3 R4 R R6 X Y R7 R' R9 *R2 and VII-43-1 'Pr H H H Bz H F H OH H H NI 2 R 3 b joined VII-43-2 'Pr H H CH 3 Bz H F H OH H H NH 2 together by VII-43-3 'Pr H H CH(CH3) 2 Bz H F H OH H H NH 2 (CH 2) 3 to VII-43-4 'Pr H H CH 2CH(CH3) 2 Bz H F H OH H H NH 2 form five VII-43-5 'Pr H H CH 2Ph Bz H F H OH H H NH 2 membered VII-43-6 'Pr H H CH 2-indol-3-yl Bz H F H OH H H NH 2 10 ring. VII-43-7 'Pr H H CH 2CH2SCH 3 Bz H F H OH H H NH 2 VII-43-8 'Pr * H * Bz H F H OH H H NH 2 Table VII 44. No RI 1 R2 R3 a R3 b R4 R R6 X Y R7 R R9 VII-44-t t Bu H H H Bz H F H OH H H NH 2 VII-44-2 'Bu H H CH 3 Bz H F H OH H H NH 2 VII-44-3 'Bu H H CH(CH3 2 Bz H F H OH H H NH 2 VII-44-4 'Bu H H CH 2CH(CH3)2 Bz H F H OH H H NH 2 VII-44-5 'Bu H H CH 2Ph Bz H F H OH H H NH 2 VII-44-6 'Bu H H CH 2-indol-3-yl Bz H F H OH H H NH 2 VII-44-7 'Bu H H CH 2CH2SCH3 Bz H F H OH H H NH 2 VII-44-8 'Bu * H CH Bz H F H OH H H NH 2 *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

122-I

Table VII-45. No RI R2 RaR 3 b R4 R R X Y R7 R' R9 VII-45-1 Ph H H H Bz H F H OH H H NH 2 VII-45-2 Ph H H CH3 Bz H F H OH H H NH 2 VII-45-3 Ph H H CH(CH3) 2 Bz H F H OH H H NH 2 VII-45-4 Ph H H CH2CH(CH3) 2 Bz H F H OH H H NH 2 VII-45-5 Ph H H CH2Ph Bz H F H OH H H NH 2 VII-45-6 Ph H H CH2-indol-3-yl Bz H F H OH H H NH 2 VII-45-7 Ph H H CH2CH2SCH 3 Bz H F H OH H H NH 2 VII-45-8 Ph * H * Bz H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-46. No R1 R2 R3 a R3 b R4 R R X Y R7 R' R9 VII-46-1 p-Me-Ph H H H Bz H F H OH H H NH 2 VII-46-2 p-Me-Ph H H CH3 Bz H F H OH H H NH 2 VII-46-3 p-Me-Ph H H CH(CH3) 2 Bz H F H OH H H NH 2 VII-46-4 p-Me-Ph H H CH2CH(CH 3) 2 Bz H F H OH H H NH 2 VII-46-5 p-Me-Ph H H CH2Ph Bz H F H OH H H NH 2 VII-46-6 p-Me-Ph H H CH2-indol-3-yl Bz H F H OH H H NH 2 VII-46-7 p-Me-Ph H H CH2CH2SCH 3 Bz H F H OH H H NH 2 VII-46-8 p-Me-Ph * H * Bz H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-47. No R1 R2 R3 a R 3b R4 R R X Y R7 R' R9 VII-47-1 p-F-Ph H H H Bz H F H OH H H NH 2 VII-47-2 p-F-Ph H H CH 3 Bz H F H OH H H NH 2 VII-47-3 p-F-Ph H H CH(CH3) 2 Bz H F H OH H H NH 2 VII-47-4 p-F-Ph H H CH 2CH(CH3) 2 Bz H F H OH H H NH 2 VII-47-5 p-F-Ph H H CH 2Ph Bz H F H OH H H NH 2 VII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F H OH H H NH 2 VII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz H F H OH H H NH 2 VII-47-8 p-F-Ph * H * Bz H F H OH H H NH 2 *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VII-48. No R R2 R 3 a R3 b R4 R 5 R6 X Y R7 R' R9 VII-48-1 p-Cl-Ph H H H Bz H F H OH H H NH 2 VII-48-2 p-Cl-Ph H H CH3 Bz H F H OH H H NH 2 VII-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F H OH H H NH 2

12/1_

No R R 2 R 3a R3 b R4 R' R' X Y R7 R' R9 VII-48-4 p-Cl-Ph H H CH2CH(CH3) 2 Bz H F H OH H H NH 2 VII-48-5 p-Cl-Ph H H CH 2Ph Bz H F H OH H H NH 2 VII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F H OH H H NH 2 VII-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz H F H OH H H NH 2 VII-48-8 p-Cl-Ph * H * Bz H F H OH H H NH 2 *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 Qr-

Table VII-49. No R RR 3 a R 3b R4 R' R6 X Y R7 R' R9 VII-49-1 p-Br-Ph H H H Bz H F H OH H H NH 2 VII-49-2 p-Br-Ph H H CH3 Bz H F H OH H H NH 2 VII-49-3 p-Br-Ph H H CH(CH 3) 2 Bz H F H OH H H NH 2 VII-49-4 p-Br-Ph H H CH2CH(CH 3) 2 Bz H F H OH H H NH 2 VII-49-5 p-Br-Ph H H CH 2Ph Bz H F H OH H H NH 2 VII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F H OH H H NH 2 VII-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F H OH H H NH 2 VII-49-8 p-Br-Ph * H * Bz H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VII-50. No R' R2 R3 a R3 b R4 R5 R6 X Y R7 R' R9 VII-50-1 p-I-Ph H H H Bz H F H OH H H NH 2 VII-50-2 p-I-Ph H H CH3 Bz H F H OH H H NH 2 VII-50-3 p-I-Ph H H CH(CH3) 2 Bz H F H OH H H NH 2 VII-50-4 p-I-Ph H H CH2CH(CH 3) 2 Bz H F H OH H H NH 2 VII-50-5 p-I-Ph H H CH2Ph Bz H F H OH H H NH 2 VII-50-6 p-I-Ph H H CH2-indol-3-yl Bz H F H OH H H NH 2 VII-50-7 p-I-Ph H H CH2CH2SCH 3 Bz H F H OH H H NH 2 VII-50-8 p-I-Ph * H * Bz H F H OH H H NH 2 *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

0

R8 NH

R R2 O R3b R N R3aN PN--P- ONO

R6 C0 2R 4 OR' R5

Y X VIII

Table VIII-1. No R1 R2 R 3a R 3b R4 R5 R6 X Y R7 R' VIII-1-1 CH3 H H H CH 3 H CH 3 OH OH H H VIII-1-2 CH3 H H CH 3 CH3 H CH 3 OH OH H H VIII-1-3 CH3 H H CH(CH 3) 2 CH3 H CH 3 OH OH H H

1Q _

No R R2 R 3a R3 b R4 R 5 R6 X Y R7 R' VIII-1-4 CH3 H H CH 2CH(CH3) 2 CH 3 H CH 3 OH OH H H VIII-1-5 CH3 H H CH 2Ph CH 3 H CH 3 OH OH H H VIII-1-6 CH3 H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H VIII-1-7 CH3 H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H VIII-1-8 CH3 * H * CH 3 H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1 27

Table VIII-2. No Rl R 2 R 3a R 3b R4 R' R6 X Y R7 R' VIII-2-1 Et H H H CH 3 H CH 3 OH OH H H VIII-2-2 Et H H CH 3 CH3 H CH 3 OH OH H H VIII-2-3 Et H H CH(CH3) 2 CH3 H CH 3 OH OH H H VIII-2-4 Et H H CH 2CH(CH3)2 CH 3 H CH 3 OH OH H H VIII-2-5 Et H H CH 2Ph CH 3 H CH 3 OH OH H H VIII-2-6 Et H H CH 2-indol-3-yl CH3 H CH 3 OH OH H H VIII-2-7 Et H H CH 2CH2SCH 3 CH3 H CH 3 OH OH H H VIII-2-8 Et * H * CH3 H CH 3 OH OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-3. No R R2 R3 a R3 b R4 R R6 X Y R7 R' VIII-3-1 'Pr H H H CH3 H CH 3 OH OH H H VIII-3-2 'Pr H H CH 3 CH3 H CH 3 OH OH H H VIII-3-3 'Pr H H CH(CH3) 2 CH 3 H CH 3 OH OH H H VIII-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H CH 3 OH OH H H VIII-3-5 'Pr H H CH 2Ph CH3 H CH 3 OH OH H H VIII-3-6 'Pr H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H VIII-3-7 'Pr H H CH 2CH2SCH 3 CH 3 H CH 3 OH OH H H VIII-3-8 'Pr * H * CH3 H CH 3 OH OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-4. No R1 R2 R3 a R 3b R4 R5 R6 X Y R7 R' VIII-4-1 'Bu H H H CH3 H CH 3 OH OH H H VIII-4-2 'Bu H H CH 3 CH 3 H CH 3 OH OH H H VIII-4-3 'Bu H H CH(CH3) 2 CH3 H CH 3 OH OH H H VIII-4-4 'Bu H H CH 2CH(CH3) 2 CH3 H CH 3 OH OH H H VIII-4-5 'Bu H H CH 2Ph CH3 H CH 3 OH OH H H VIII-4-6 'Bu H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H VIII-4-7 'Bu H H CH 2CH 2SCH 3 CH3 H CH 3 OH OH H H VIII-4-8 'Bu * H * CH3 H CH 3 OH OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

122_

Table VIII-5. RR No RI R2 RaR 3 b R4 X Y R7 R' VIII-5-1 Ph H H H CH 3 H CH 3 OH OH H H VIII-5-2 Ph H H CH 3 CH 3 H CH3 OH OH H H VIII-5-3 Ph H H CH(CH 3)2 CH 3 H CH3 OH OH H H VIII-5-4 Ph H H CH 2CH(CH 3)2 CH 3 H CH3 OH OH H H VIII-5-5 Ph H H CH 2Ph CH 3 H CH3 OH OH H H VIII-5-6 Ph H H CH 2-indol-3-yl CH 3 H CH3 OH OH H H VIII-5-7 Ph H H CH 2CH2SCH 3 CH 3 H CH3 OH OH H H VIII-5-8 Ph * H * CH 3 H CH3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-6. No R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' VIII-6-1 p-Me-Ph H H H CH 3 H CH3 OH OH H H VIII-6-2 p-Me-Ph H H CH 3 CH 3 H CH3 OH OH H H VIII-6-3 p-Me-Ph H H CH(CH 3)2 CH 3 H CH3 OH OH H H VIII-6-4 p-Me-Ph H H CH 2CH(CH 3)2 CH 3 H CH3 OH OH H H VIII-6-5 p-Me-Ph H H CH 2Ph CH 3 H CH3 OH OH H H VIII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 H CH3 OH OH H H VIII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH 3 H CH3 OH OH H H VIII-6-8 p-Me-Ph * H * CH 3 H CH 3 OH OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VIII-7. No R1 R2 R3a R 3b R4 R 5 R6 X Y R7 R' VIII-7-1 p-F-Ph H H H CH 3 H CH3 OH OH H H VIII-7-2 p-F-Ph H H CH3 CH 3 H CH3 OH OH H H VIII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 H CH3 OH OH H H VIII-7-4 p-F-Ph H H CH2CH(CH 3) 2 CH 3 H CH3 OH OH H H VIII-7-6 p-F-Ph H H CH2Ph CH 3 H CH3 OH OH H H VIII-7-7 p-F-Ph H H CH2-indol-3-yl CH 3 H CH3 OH OH H H VIII-7-8 p-F-Ph H H CH2CH2SCH 3 CH 3 H CH3 OH OH H H VIII-7-20 p-F-Ph * H * CH 3 H CH3 OH OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table VIII-8. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R' VIII-8-1 p-Cl-Ph H H H CH3 H CH 3 OH OH H H VIII-8-2 p-Cl-Ph H H CH3 CH3 H CH 3 OH OH H H VIII-8-3 p-Cl-Ph H H CH(CH 3) 2 CH3 H CH 3 OH OH H H

1QO

No R R2 R 3 a R3 b R4 R 5 R6 X Y R7 R' VIII-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH 3 H CH 3 OH OH H H VIII-8-5 p-Cl-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H VIII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H VIII-8-7 p-Cl-Ph H H CH2CH2 SCH3 CH 3 H CH 3 OH OH H H VIII-8-8 p-Cl-Ph * H * CH 3 H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-9. No R R2 R 3 a R3b R4 R' R6 X Y R7 R' VIII-9-1 p-Br-Ph H H H CH 3 H CH 3 OH OH H H VIII-9-2 p-Br-Ph H H CH 3 CH 3 H CH 3 OH OH H H VIII-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H VIII-9-4 p-Br-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 OH OH H H VIII-9-6 p-Br-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H VIII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H VIII-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H VIII-9-20 p-Br-Ph * H * CH 3 H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1o

Table VIII-10. No R R2 R 3 a R 3b R4 R R X Y R7 R' VIII-10-1 p-I-Ph H H H CH 3 H CH 3 OH OH H H VIII-10-2 p-I-Ph H H CH 3 CH 3 H CH 3 OH OH H H VIII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H CH 3 OH OH H H VIII-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 OH OH H H VIII-10-5 p-I-Ph H H CH 2Ph CH 3 H CH 3 OH OH H H VIII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H CH 3 OH OH H H VIII-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 OH OH H H VIII-10-8 p-I-Ph * H * CH 3 H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-11. No R1 R2 R3a R3 R4 R' R6 X Y R7 R' VIII-11-1 CH 3 H H H Et H CH 3 OH OH H H VIII-11-2 CH 3 H H CH3 Et H CH 3 OH OH H H VIII-11-3 CH 3 H H CH(CH3)2 Et H CH 3 OH OH H H VIII-11-4 CH 3 H H CH2CH(CH3) 2 Et H CH 3 OH OH H H VIII-11-5 CH 3 H H CH 2Ph Et H CH 3 OH OH H H VIII-11-6 CH 3 H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-11-7 CH 3 H H CH2CH 2SCH 3 Et H CH 3 OH OH H H VIII-11-8 CH 3 * H * Et H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-12. No Rl R 2 R 3 a R 3b R4 R5 R6 X Y R7 R' VIII-12-1 Et H H H Et H CH 3 OH OH H H VIII-12-2 Et H H CH3 Et H CH 3 OH OH H H VIII-12-3 Et H H CH(CH3) 2 Et H CH 3 OH OH H H VIII-12-4 Et H H CH2CH(CH3)2 Et H CH 3 OH OH H H VIII-12-5 Et H H CH 2Ph Et H CH 3 OH OH H H VIII-12-6 Et H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-12-7 Et H H CH2CH2SCH 3 Et H CH 3 OH OH H H VIII-12-8 Et * H * Et H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

101 _

Table VIII-13. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' VIII-13-1 'Pr H H H Et H CH 3 OH OH H H VIII-13-2 'Pr H H CH 3 Et H CH 3 OH OH H H VIII-13-3 'Pr H H CH(CH 3)2 Et H CH 3 OH OH H H VIII-13-4 Pr H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H VIII-13-5 Pr H H CH 2Ph Et H CH 3 OH OH H H VIII-13-6 Pr H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-13-7 Pr H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H VIII-13-8 Pr * H * Et H CH 3 OH OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-14. M R1 R2 R3a R3 b R4 R' R6 X Y R7 R VIII-14-1 'Bu H H H Et H CH 3 OH OH H H VIII-14-2 'Bu H H CH 3 Et H CH 3 OH OH H H VIII-14-3 'Bu H H CH(CH3) 2 Et H CH 3 OH OH H H VIII-14-4 'Bu H H CH 2CH(CH 3)2 Et H CH 3 OH OH H H VIII-14-5 'Bu H H CH 2Ph Et H CH 3 OH OH H H VIII-14-6 'Bu H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-14-7 'Bu H H CH 2CH2SCH 3 Et H CH 3 OH OH H H VIII-14-8 'Bu * H * Et H CH 3 OH OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-15. No RI R 2 R3 a R3b 4 R5 R6 X Y R7 R VIII-15-1 Ph H H H Et H CH 3 OH OH H H VIII-15-2 Ph H H CH 3 Et H CH 3 OH OH H H VIII-15-3 Ph H H CH(CH3) 2 Et H CH 3 OH OH H H VIII-15-4 Ph H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H VIII-15-5 Ph H H CH 2Ph Et H CH 3 OH OH H H VIII-15-6 Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-15-7 Ph H H CH 2CH2SCH 3 Et H CH 3 OH OH H H VIII-15-8 Ph * H * Et H CH 3 OH OH H H *R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

10)_

Table VIII-16. No R R2 R 3 a R 3b R4 R R6 X Y R7 R' VIII-16-1 p-Me-Ph H H H Et H CH 3 OH OH H H VIII-16-2 p-Me-Ph H H CH 3 Et H CH 3 OH OH H H VIII-16-3 p-Me-Ph H H CH(CH 3) 2 Et H CH 3 OH OH H H VIII-16-4 p-Me-Ph H H CH 2CH(CH3) 2 Et H CH 3 OH OH H H VIII-16-5 p-Me-Ph H H CH 2Ph Et H CH 3 OH OH H H VIII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H CH 3 OH OH H H VIII-16-8 p-Me-Ph * H * Et H CH 3 OH OH H H

*R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table VIII-17. 9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' VIII-17-1 p-F-Ph H H H Et H CH 3 OH OH H H VIII-17-2 p-F-Ph H H CH3 Et H CH 3 OH OH H H VIII-17-3 p-F-Ph H H CH(CH3) 2 Et H CH 3 OH OH H H VIII-17-4 p-F-Ph H H CH2CH(CH 3) 2 Et H CH 3 OH OH H H VIII-17-5 p-F-Ph H H CH2Ph Et H CH 3 OH OH H H VIII-17-6 p-F-Ph H H CH2-indol-3-yl Et H CH 3 OH OH H H VIII-17-7 p-F-Ph H H CH2CH2SCH 3 Et H CH 3 OH OH H H VIII-17-8 p-F-Ph * H * Et H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-18. No R R2 R 3 a R 3b R4 R5 R6 X Y R7 R' VIII-18-1 p-Cl-Ph H H H Et H CH 3 OH OH H H VIII-18-2 p-Cl-Ph H H CH3 Et H CH 3 OH OH H H VIII-18-3 p-Cl-Ph H H CH(CH 3)2 Et H CH 3 OH OH H H VIII-18-4 p-Cl-Ph H H CH2CH(CH 3)2 Et H CH 3 OH OH H H VIII-18-5 p-Cl-Ph H H CH 2Ph Et H CH 3 OH OH H H VIII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H VIII-18-8 p-Cl-Ph * H * Et H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-19. No R R 2 R 3a R3 b R4 R5 R6 X Y R7 R' VIII-19-1 p-Br-Ph H H H Et H CH3 OH OH H H VIII-19-2 p-Br-Ph H H CH 3 Et H CH3 OH OH H H VIII-19-3 p-Br-Ph H H CH(CH 3) 2 Et H CH3 OH OH H H

10'1

R' No R RR 3 a R3 b R4 R' X Y R7 R' VIII-19-4 p-Br-Ph H H CH 2CH(CH3)2 Et H CH 3 OH OH H H VIII-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 OH OH H H VIII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H VIII-19-8 p-Br-Ph * H * Et H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-20. No R R2 R 3 a R 3b R4 R R6 X Y R7 R' VIII-20-1 p-I-Ph H H H Et H CH 3 OH OH H H VIII-20-2 p-I-Ph H H CH 3 Et H CH 3 OH OH H H VIII-20-3 p-I-Ph H H CH(CH3) 2 Et H CH 3 OH OH H H VIII-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H CH 3 OH OH H H VIII-20-5 p-I-Ph H H CH 2Ph Et H CH 3 OH OH H H VIII-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH 3 OH OH H H VIII-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H CH 3 OH OH H H VIII-20-8 p-I-Ph * H * Et H CH 3 OH OH H H

*R2 and R3b joined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-21. No R R2 R 3 a R3 b R4 R' R6 X Y R7 R' VIII-21-1 CH 3 H H H 'Pr H CH 3 OH OH H H VIII-21-2 CH 3 H H CH3 'Pr H CH 3 OH OH H H VIII-21-3 CH3 H H CH(CH 3) 2 'Pr H CH 3 OH OH H H VIII-21-4 CH3 H H CH2CH(CH3) 2 'Pr H CH 3 OH OH H H VIII-21-5 CH3 H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-21-6 CH3 H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-21-7 CH3 H H CH2CH 2SCH 3 'Pr H CH 3 OH OH H H VIII-21-8 CH3 * H * 'Pr H CH 3 OH OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-22. No Rl R 2 R 3 a R 3b R4 R5 R6 X Y R7 R' VIII-22-1 Et H H H 'Pr H CH 3 OH OH H H VIII-22-2 Et H H CH3 'Pr H CH 3 OH OH H H VIII-22-3 Et H H CH(CH 3)2 'Pr H CH 3 OH OH H H VIII-22-4 Et H H CH2CH(CH 3) 2 'Pr H CH 3 OH OH H H VIII-22-5 Et H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-22-6 Et H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H

10/1

Rl R 2 R3 a R3 b R4 R' R' X Y R7 R' o

VIII-22-7 Et H H CH2CH2SCH 3 'Pr H CH 3 OH OH H H VIII-22-8 Et * H * 'Pr H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-23. No R1 R2 R3 a R3 b R4 R' R6 X Y R7 R' VIII-23-1 'Pr H H H 'Pr H CH3 OH OH H H VIII-23-2 'Pr H H CH 3 'Pr H CH3 OH OH H H VIII-23-3 'Pr H H CH(CH 3)2 'Pr H CH3 OH OH H H VIII-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H CH3 OH OH H H VIII-23-5 'Pr H H CH 2Ph 'Pr H CH3 OH OH H H VIII-23-6 'Pr H H CH 2-indol-3-yl 'Pr H CH3 OH OH H H VIII-23-7 'Pr H H CH 2CH 2SCH 3 'Pr H CH3 OH OH H H VIII-23-8 'Pr * H * 'Pr H CH3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-24. No R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' VIII-24-1 'Bu H H H 'Pr H CH 3 OH OH H H VIII-24-2 'Bu H H CH3 'Pr H CH 3 OH OH H H VIII-24-3 'Bu H H CH(CH3) 2 'Pr H CH 3 OH OH H H VIII-24-4 'Bu H H CH2CH(CH 3)2 'Pr H CH 3 OH OH H H VIII-24-5 'Bu H H CH2Ph 'Pr H CH 3 OH OH H H VIII-24-6 'Bu H H CH2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-24-7 'Bu H H CH2CH 2SCH 3 'Pr H CH 3 OH OH H H VIII-24-8 'Bu * H * 'Pr H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-25. M R R2 R3 a R3 b R5 R6 X Y R7 R' VIII-25-1 Ph H H H 'Pr H CH 3 OH OH H H VIII-25-2 Ph H H CH 3 'Pr H CH 3 OH OH H H VIII-25-3 Ph H H CH(CH 3) 2 'Pr H CH 3 OH OH H H VIII-25-4 Ph H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H VIII-25-5 Ph H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-25-7 Ph H H CH 2CH2SCH 3 'Pr H CH 3 OH OH H H VIII-25-8 Ph * H * 'Pr H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1o _

Table VIII-26. No R R2 R 3 a R3b R4 R R6 X Y R7 R' VIII-26-1 p-Me-Ph H H H 'Pr H CH 3 OH OH H H VIII-26-2 p-Me-Ph H H CH 3 'Pr H CH 3 OH OH H H VIII-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr H CH 3 OH OH H H VIII-26-4 p-Me-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 OH OH H H VIII-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H CH 3 OH OH H H VIII-26-8 p-Me-Ph * H * 'Pr H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-27. 9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' VIII-27-1 p-F-Ph H H H 'Pr H CH 3 OH OH H H VIII-27-2 p-F-Ph H H CH3 'Pr H CH 3 OH OH H H VIII-27-3 p-F-Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H VIII-27-4 p-F-Ph H H CH2CH(CH 3) 2 'Pr H CH 3 OH OH H H VIII-27-5 p-F-Ph H H CH2Ph 'Pr H CH 3 OH OH H H VIII-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-27-7 p-F-Ph H H CH2CH2SCH 3 'Pr H CH 3 OH OH H H VIII-27-8 p-F-Ph * H * 'Pr H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-28. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' VIII-28-1 p-Cl-Ph H H H 'Pr H CH 3 OH OH H H VIII-28-2 p-Cl-Ph H H CH3 'Pr H CH 3 OH OH H H VIII-28-3 p-Cl-Ph H H CH(CH 3)2 'Pr H CH 3 OH OH H H VIII-28-4 p-Cl-Ph H H CH2CH(CH 3)2 'Pr H CH 3 OH OH H H VIII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr H CH 3 OH OH H H VIII-28-8 p-Cl-Ph * H * 'Pr H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-29. No R R 2 R 3a R3 b R4 R5 R6 X Y R7 R' VIII-29-1 p-Br-Ph H H H 'Pr H CH 3 OH OH H H VIII-29-2 p-Br-Ph H H CH 3 'Pr H CH 3 OH OH H H VIII-29-3 p-Br-Ph H H CH(CH 3) 2 'Pr H CH 3 OH OH H H

1o _

R' No R RR 3 a R3 b R4 R' X Y R7 R' VIII-29-4 p-Br-Ph H H CH 2CH(CH3)2 'Pr H CH 3 OH OH H H VIII-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 OH OH H H VIII-29-8 p-Br-Ph * H * 'Pr H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

107_

Table VIII-30. No R R2 R 3 a R3 b R4 R R6 X Y R7 R' VIII-30-1 p-I-Ph H H H 'Pr H CH 3 OH OH H H VIII-30-2 p-I-Ph H H CH 3 'Pr H CH 3 OH OH H H VIII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H CH 3 OH OH H H VIII-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr H CH 3 OH OH H H VIII-30-5 p-I-Ph H H CH 2Ph 'Pr H CH 3 OH OH H H VIII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH 3 OH OH H H VIII-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H CH 3 OH OH H H VIII-30-8 p-I-Ph * H * 'Pr H CH 3 OH OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-31. No R1 R2 R3a R3 R4 R' R6 X Y R7 R' VIII-31-1 CH 3 H H H "Bu H CH 3 OH OH H H VIII-31-2 CH 3 H H CH3 "Bu H CH 3 OH OH H H VIII-31-3 CH 3 H H CH(CH3)2 "Bu H CH 3 OH OH H H VIII-31-4 CH 3 H H CH2CH(CH3) 2 "Bu H CH 3 OH OH H H VIII-31-5 CH 3 H H CH 2Ph "Bu H CH 3 OH OH H H VIII-31-6 CH 3 H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H CH 3 OH OH H H VIII-31-8 CH 3 * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-32. No Rl R 2 R3 a R3b R4 R 5 R6 X Y R7 R' VIII-32-1 Et H H H "Bu H CH 3 OH OH H H VIII-32-2 Et H H CH3 "Bu H CH 3 OH OH H H VIII-32-3 Et H H CH(CH3) 2 "Bu H CH 3 OH OH H H VIII-32-4 Et H H CH2CH(CH3)2 "Bu H CH 3 OH OH H H VIII-32-5 Et H H CH 2Ph "Bu H CH 3 OH OH H H VIII-32-6 Et H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-32-7 Et H H CH2CH2SCH 3 "Bu H CH 3 OH OH H H VIII-32-8 Et * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

102_

Table VIII-33. No R1 R2 R3 a R3b R4 RI R6 X Y R7 R' VIII-33-1 'Pr H H H "Bu H CH 3 OH OH H H VIII-33-2 'Pr H H CH 3 "Bu H CH 3 OH OH H H VIII-33-3 'Pr H H CH(CH 3)2 "Bu H CH 3 OH OH H H VIII-33-4 Pr H H CH 2CH(CH 3) 2 "Bu H CH 3 OH OH H H VIII-33-5 Pr H H CH 2Ph "Bu H CH 3 OH OH H H VIII-33-6 Pr H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-33-7 Pr H H CH 2 CH 2 SCH 3 "Bu H CH 3 OH OH H H VIII-33-8 Pr * H * "Bu H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-34. M R1 R2 R3a R3b R4 R' R6 X Y R7 R' VIII-34-1 'Bu H H H "Bu H CH 3 OH OH H H VIII-34-2 'Bu H H CH3 "Bu H CH 3 OH OH H H VIII-34-3 'Bu H H CH(CH3 ) 2 "Bu H CH 3 OH OH H H VIII-34-4 'Bu H H CH2 CH(CH 3 )2 "Bu H CH 3 OH OH H H VIII-34-5 'Bu H H CH2 Ph "Bu H CH 3 OH OH H H VIII-34-6 'Bu H H CH2 -indol-3-yl "Bu H CH 3 OH OH H H VIII-34-7 'Bu H H CH2 CH 2 SCH 3 "Bu H CH 3 OH OH H H VIII-34-8 'Bu * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-35. o RI R 2 R 3a R 3b R4 R5 R6 X Y R7 R' VIII-35-1 Ph H H H "Bu H CH 3 OH OH H H VIII-35-2 Ph H H CH 3 "Bu H CH 3 OH OH H H VIII-35-3 Ph H H CH(CH 3) 2 "Bu H CH 3 OH OH H H VIII-35-4 Ph H H CH 2CH(CH3) 2 "Bu H CH 3 OH OH H H VIII-35-5 Ph H H CH 2Ph "Bu H CH 3 OH OH H H VIII-35-6 Ph H H CH 2 -indol-3-yl "Bu H CH 3 OH OH H H VIII-35-7 Ph H H CH 2 CH2 SCH 3 "Bu H CH 3 OH OH H H VIII-35-8 Ph * H * "Bu H CH 3 OH OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

100_

Table VIII-36. No R R2 R 3 a R3 b R4 R R6 X Y R7 R' VIII-36-1 p-Me-Ph H H H "Bu H CH 3 OH OH H H VIII-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 OH OH H H VIII-36-3 p-Me-Ph H H CH(CH 3) 2 "Bu H CH 3 OH OH H H VIII-36-4 p-Me-Ph H H CH 2CH(CH3) 2 "Bu H CH 3 OH OH H H VIII-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 OH OH H H VIII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 OH OH H H VIII-36-8 p-Me-Ph * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-37. No R1 R2 R 3 a Rb R4 R' R6 X Y R7 R' VIII-37-1 p-F-Ph H H H "Bu H CH 3 OH OH H H VIII-37-2 p-F-Ph H H CH3 "Bu H CH 3 OH OH H H VIII-37-3 p-F-Ph H H CH(CH3 ) 2 "Bu H CH 3 OH OH H H VIII-37-4 p-F-Ph H H CH2 CH(CH 3 ) 2 "Bu H CH 3 OH OH H H VIII-37-5 p-F-Ph H H CH2 Ph "Bu H CH 3 OH OH H H VIII-37-6 p-F-Ph H H CH2-indol-3-yl "Bu H CH 3 OH OH H H VIII-37-7 p-F-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 OH OH H H VIII-37-8 p-F-Ph * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-38. No R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' VIII-38-1 p-Cl-Ph H H H "Bu H CH 3 OH OH H H VIII-38-2 p-Cl-Ph H H CH 3 "Bu H CH 3 OH OH H H VIII-38-3 p-Cl-Ph H H CH(CH 3 )2 "Bu H CH 3 OH OH H H VIII-38-4 p-Cl-Ph H H CH 2 CH(CH 3 )2 "Bu H CH 3 OH OH H H VIII-38-5 p-Cl-Ph H H CH 2 Ph "Bu H CH 3 OH OH H H VIII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 OH OH H H VIII-38-8 p-Cl-Ph * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-39. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R' VIII-39-1 p-Br-Ph H H H "Bu H CH 3 OH OH H H VIII-39-2 p-Br-Ph H H CH 3 "Bu H CH 3 OH OH H H VIII-39-3 p-Br-Ph H H CH(CH 3) 2 "Bu H CH 3 OH OH H H

R' No R RR 3 a R3 b R4 R' X Y R7 R' VIII-39-4 p-Br-Ph H H CH 2CH(CH3)2 "Bu H CH 3 OH OH H H VIII-39-5 p-Br-Ph H H CH 2Ph "Bu H CH 3 OH OH H H VIII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 OH OH H H VIII-39-8 p-Br-Ph * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'IM1 _

Table VIII-40. No R R2 R 3 a R 3b R4 R R X Y R7 R' VIII-40-1 p-I-Ph H H H "Bu H CH 3 OH OH H H VIII-40-2 p-I-Ph H H CH 3 "Bu H CH 3 OH OH H H VIII-40-3 p-I-Ph H H CH(CH3) 2 "Bu H CH 3 OH OH H H VIII-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu H CH 3 OH OH H H VIII-40-5 p-I-Ph H H CH 2Ph "Bu H CH 3 OH OH H H VIII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 OH OH H H VIII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 OH OH H H VIII-40-8 p-I-Ph * H * "Bu H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-41. No R1 R2 R3a R3 R4 R5 R6 X Y R7 R' VIII-41-1 CH 3 H H H Bz H CH 3 OH OH H H VIII-41-2 CH 3 H H CH3 Bz H CH 3 OH OH H H VIII-41-3 CH 3 H H CH(CH3)2 Bz H CH 3 OH OH H H VIII-41-4 CH 3 H H CH2CH(CH3) 2 Bz H CH 3 OH OH H H VIII-41-5 CH 3 H H CH 2Ph Bz H CH 3 OH OH H H VIII-41-6 CH 3 H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-41-7 CH 3 H H CH2CH 2SCH 3 Bz H CH 3 OH OH H H VIII-41-8 CH 3 * H * Bz H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-42. R' No Rl R 2 R 3a R 3b R4 R5 X Y R7 R' VIII-42-1 Et H H H Bz H CH 3 OH OH H H VIII-42-2 Et H H CH3 Bz H CH 3 OH OH H H VIII-42-3 Et H H CH(CH3) 2 Bz H CH 3 OH OH H H VIII-42-4 Et H H CH2CH(CH3)2 Bz H CH 3 OH OH H H VIII-42-5 Et H H CH 2Ph Bz H CH 3 OH OH H H VIII-42-6 Et H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-42-7 Et H H CH2CH2SCH 3 Bz H CH 3 OH OH H H VIII-42-8 Et * H * Bz H CH 3 OH OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table VIII-43. No R1 R2 R3a R3 R4 R' R' X Y R7 R' *R 2 and R 3

' VIII-43-1 Pr H H H Bz H CH3 OH OH H H joined VIII-43-2 Pr H H CH 3 Bz H CH3 OH OH H H together by VIII-43-3 Pr H H CH(CH 3)2 Bz H CH3 OH OH H 4 (CH2)3 to VIII-43-4 Pr H H CH 2CH(CH 3) 2 Bz H CH3 OH OH H H form five VIII-43-5 'Pr H H CH 2Ph Bz H CH3 OH OH H H membered VIII-43-6 'Pr H H CH 2-indol-3-yl Bz H CH3 OH OH H H VIII-43-7 'Pr H H CH 2CH 2SCH 3 Bz H CH3 OH OH H H ring. VIII-43-8 'Pr * H * Bz H CH3 OH OH H H Table VIII 10 44. No R1 R2 R 3a R3 b R4 R' R6 X Y R7 R VIII-44-1 'Bu H H H Bz H CH 3 OH OH H H VIII-44-2 'Bu H H CH3 Bz H CH 3 OH OH H H VIII-44-3 'Bu H H CH(CH3) 2 Bz H CH 3 OH OH H H VIII-44-4 'Bu H H CH2CH(CH 3)2 Bz H CH 3 OH OH H H VIII-44-5 'Bu H H CH2Ph Bz H CH 3 OH OH H H VIII-44-6 'Bu H H CH2-indol-3-yl Bz H CH 3 OH OH H H VIII-44-7 'Bu H H CH2CH 2SCH 3 Bz H CH 3 OH OH H H VIII-44-8 'Bu * H * Bz H CH 3 OH OH H H *R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table VIII-45. No R' R2 R3 a R3 b R4 R5 R6 X Y R7 R' VIII-45-1 Ph H H H Bz H CH 3 OH OH H H VIII-45-2 Ph H H CH 3 Bz H CH 3 OH OH H H VIII-45-3 Ph H H CH(CH 3) 2 Bz H CH 3 OH OH H H VIII-45-4 Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H VIII-45-5 Ph H H CH 2Ph Bz H CH 3 OH OH H H VIII-45-6 Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-45-7 Ph H H CH 2CH2SCH 3 Bz H CH 3 OH OH H H VIII-45-8 Ph * H * Bz H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-46. No R R2 R 3 a R3b R4 R R X Y R7 R' VIII-46-1 p-Me-Ph H H H Bz H CH 3 OH OH H H VIII-46-2 p-Me-Ph H H CH 3 Bz H CH 3 OH OH H H VIII-46-3 p-Me-Ph H H CH(CH 3) 2 Bz H CH 3 OH OH H H VIII-46-4 p-Me-Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H VIII-46-5 p-Me-Ph H H CH 2Ph Bz H CH 3 OH OH H H VIII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H CH 3 OH OH H H VIII-46-8 p-Me-Ph * H * Bz H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-47. No R1 R2 R3 a R3 b R4 R R6 X Y R7 R' VIII-47-1 p-F-Ph H H H Bz H CH 3 OH OH H H VIII-47-2 p-F-Ph H H CH3 Bz H CH 3 OH OH H H VIII-47-3 p-F-Ph H H CH(CH3) 2 Bz H CH 3 OH OH H H VIII-47-4 p-F-Ph H H CH2CH(CH 3) 2 Bz H CH 3 OH OH H H VIII-47-5 p-F-Ph H H CH2Ph Bz H CH 3 OH OH H H VIII-47-6 p-F-Ph H H CH2-indol-3-yl Bz H CH 3 OH OH H H VIII-47-7 p-F-Ph H H CH2CH2SCH 3 Bz H CH 3 OH OH H H VIII-47-8 p-F-Ph * H * Bz H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-48. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' VIII-48-1 p-Cl-Ph H H H Bz H CH 3 OH OH H H VIII-48-2 p-Cl-Ph H H CH3 Bz H CH 3 OH OH H H VIII-48-3 p-Cl-Ph H H CH(CH 3)2 Bz H CH 3 OH OH H H VIII-48-4 p-Cl-Ph H H CH2CH(CH 3)2 Bz H CH 3 OH OH H H VIII-48-5 p-Cl-Ph H H CH 2Ph Bz H CH 3 OH OH H H VIII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz H CH 3 OH OH H H VIII-48-8 p-Cl-Ph * H * Bz H CH 3 OH OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-49. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R' VIII-49-1 p-Br-Ph H H H Bz H CH 3 OH OH H H VIII-49-2 p-Br-Ph H H CH 3 Bz H CH 3 OH OH H H VIII-49-3 p-Br-Ph H H CH(CH 3) 2 Bz H CH 3 OH OH H H

- fA-

No R RR 3 a R3 b R4 R' R6 X Y R7 R' VIII-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz H CH 3 OH OH H H VIII-49-5 p-Br-Ph H H CH 2Ph Bz H CH 3 OH OH H H VIII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz H CH 3 OH OH H H VIII-49-8 p-Br-Ph * H * Bz H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table VIII-50. R No R' R2 R3 a R3b R4 R X Y R7 R' VIII-50-1 p-I-Ph H H H Bz H CH 3 OH OH H H VIII-50-2 p-I-Ph H H CH 3 Bz H CH 3 OH OH H H VIII-50-3 p-I-Ph H H CH(CH 3) 2 Bz H CH 3 OH OH H H VIII-50-4 p-I-Ph H H CH 2CH(CH3) 2 Bz H CH 3 OH OH H H VIII-50-5 p-I-Ph H H CH 2Ph Bz H CH 3 OH OH H H VIII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH 3 OH OH H H VIII-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz H CH 3 OH OH H H VIII-50-8 p-I-Ph * H * Bz H CH 3 OH OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

0

R8 NH

R2 0 R3b R7 N O R3aN PNN--P- OO

R6 C0 2R 4 OR' R5

Y X IX

Table IX-1. No R R2 R3 a R3 b R4 R5 R6 X Y R7 R' IX-1-1 CH3 H H H CH 3 H CH 3 F OH H H IX-1-2 CH3 H H CH3 CH 3 H CH 3 F OH H H IX-1-3 CH3 H H CH(CH 3) 2 CH 3 H CH 3 F OH H H IX-1-4 CH3 H H CH2CH(CH 3) 2 CH 3 H CH 3 F OH H H IX-1-5 CH3 H H CH 2Ph CH 3 H CH 3 F OH H H

No R R2 R3 a R3 b R4 R 5 R' X Y R7 R' IX-1-6 CH3 H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H IX-1-7 CH3 H H CH2CH 2SCH 3 CH 3 H CH 3 F OH H H IX-1-8 CH3 * H * CH 3 H CH 3 F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table IX-2. N9 Rl R 2 R3 a R3 b R4 R 5 R6 X Y R7 R' IX-2-1 Et H H H CH 3 H CH 3 F OH H H IX-2-2 Et H H CH 3 CH 3 H CH 3 F OH H H IX-2-3 Et H H CH(CH3) 2 CH 3 H CH 3 F OH H H IX-2-4 Et H H CH 2CH(CH3) 2 CH 3 H CH 3 F OH H H IX-2-5 Et H H CH 2Ph CH 3 H CH 3 F OH H H IX-2-6 Et H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H IX-2-7 Et H H CH 2CH 2SCH 3 CH 3 H CH 3 F OH H H IX-2-8 Et * H * CH 3 H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Int;-

Table IX-3. No R1 R 2 R3 a R3b R4 R' R6 X Y R7 R' IX-3-1 'Pr H H H CH 3 H CH 3 F OH H H IX-3-2 'Pr H H CH 3 CH3 H CH 3 F OH H H IX-3-3 'Pr H H CH(CH3) 2 CH3 H CH 3 F OH H H IX-3-4 Pr H H CH 2CH(CH 3) 2 CH 3 H CH 3 F OH H H IX-3-5 Pr H H CH 2Ph CH 3 H CH 3 F OH H H IX-3-6 Pr H H CH 2-indol-3-yl CH3 H CH 3 F OH H H IX-3-7 Pr H H CH 2CH2SCH 3 CH3 H CH 3 F OH H H IX-3-8 Pr * H * CH 3 H CH 3 F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table IX-4. No R1 R2 R 3a Rb R4 R R6 X Y R7 R' IX-4-1 'Bu H H H CH 3 H CH 3 F OH H H IX-4-2 'Bu H H CH 3 CH 3 H CH 3 F OH H H IX-4-3 'Bu H H CH(CH3) 2 CH 3 H CH 3 F OH H H IX-4-4 'Bu H H CH 2CH(CH 3)2 CH 3 H CH 3 F OH H H IX-4-5 'Bu H H CH 2Ph CH 3 H CH 3 F OH H H IX-4-6 'Bu H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H IX-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H CH 3 F OH H H IX-4-8 'Bu * H * CH 3 H CH 3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-5. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' IX-5-1 Ph H H H CH 3 H CH 3 F OH H H IX-5-2 Ph H H CH3 CH3 H CH 3 F OH H H IX-5-3 Ph H H CH(CH3)2 CH3 H CH 3 F OH H H IX-5-4 Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH H H IX-5-5 Ph H H CH 2Ph CH 3 H CH 3 F OH H H IX-5-6 Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH H H IX-5-7 Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH H H IX-5-8 Ph * H * CH 3 H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

IWr7-

Table IX-6. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' IX-6-1 p-Me-Ph H H H CH 3 H CH 3 F OH H H IX-6-2 p-Me-Ph H H CH3 CH3 H CH 3 F OH H H IX-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 H CH 3 F OH H H IX-6-4 p-Me-Ph H H CH2CH(CH 3)2 CH3 H CH 3 F OH H H IX-6-5 p-Me-Ph H H CH 2Ph CH 3 H CH 3 F OH H H IX-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH H H IX-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH H H IX-6-8 p-Me-Ph * H * CH 3 H CH 3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-7. N R1 R2 R3a R3 R4 R' R6 X Y R7 R' IX-7-1 p-F-Ph H H H CH 3 H CH3 F OH H H IX-7-2 p-F-Ph H H CH3 CH3 H CH3 F OH H H IX-7-3 p-F-Ph H H CH(CH3)2 CH3 H CH3 F OH H H IX-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H CH3 F OH H H IX-7-6 p-F-Ph H H CH 2Ph CH 3 H CH3 F OH H H IX-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H CH3 F OH H H IX-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H CH3 F OH H H IX-7-20 p-F-Ph * H * CH 3 H CH3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-8. N9 R1 R 2 R 3 a R 3b R4 R5 R6 X Y R7 R' IX-8-1 p-Cl-Ph H H H CH 3 H CH3 F OH H H IX-8-2 p-Cl-Ph H H CH 3 CH 3 H CH3 F OH H H IX-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H CH3 F OH H H IX-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H CH3 F OH H H IX-8-5 p-Cl-Ph H H CH 2Ph CH 3 H CH3 F OH H H IX-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H CH3 F OH H H IX-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H CH3 F OH H H IX-8-8 p-Cl-Ph * H * CH 3 H CH 3 F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

IMnQ

Table IX-9. N9 R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' IX-9-1 p-Br-Ph H H H CH 3 H CH 3 F OH H H IX-9-2 p-Br-Ph H H CH3 CH 3 H CH 3 F OH H H IX-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H CH 3 F OH H H IX-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH 3 H CH 3 F OH H H IX-9-6 p-Br-Ph H H CH 2Ph CH 3 H CH 3 F OH H H IX-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH H H IX-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 H CH 3 F OH H H IX-9-20 p-Br-Ph * H * CH 3 H CH 3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-10. N R1 R2 R3a R3b R4 R' R6 X Y R7 R' IX-10-1 p-I-Ph H H H CH 3 H CH 3 F OH H H IX-10-2 p-I-Ph H H CH 3 CH3 H CH 3 F OH H H IX-10-3 p-I-Ph H H CH(CH3) 2 CH3 H CH 3 F OH H H IX-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 F OH H H IX-10-5 p-I-Ph H H CH 2Ph CH 3 H CH 3 F OH H H IX-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH H H IX-10-7 p-I-Ph H H CH 2CH2SCH 3 CH3 H CH 3 F OH H H IX-10-8 p-I-Ph * H * CH 3 H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-11. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' IX-11-1 CH 3 H H H Et H CH 3 F OH H H IX-11-2 CH 3 H H CH3 Et H CH 3 F OH H H IX-11-3 CH 3 H H CH(CH3) 2 Et H CH 3 F OH H H IX-11-4 CH 3 H H CH2CH(CH3) 2 Et H CH 3 F OH H H IX-11-5 CH 3 H H CH 2Ph Et H CH 3 F OH H H IX-11-6 CH 3 H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-11-7 CH 3 H H CH2CH 2SCH 3 Et H CH 3 F OH H H IX-11-8 CH 3 * H * Et H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Ino_

Table IX-12. N9 Rl R2 R 3 a R 3b R 4 R5 R6 X Y R7 R' IX-12-1 Et H H H Et H CH 3 F OH H H IX-12-2 Et H H CH3 Et H CH 3 F OH H H IX-12-3 Et H H CH(CH3) 2 Et H CH 3 F OH H H IX-12-4 Et H H CH2CH(CH3) 2 Et H CH 3 F OH H H IX-12-5 Et H H CH2Ph Et H CH 3 F OH H H IX-12-6 Et H H CH2-indol-3-yl Et H CH 3 F OH H H IX-12-7 Et H H CH2CH 2SCH 3 Et H CH 3 F OH H H IX-12-8 Et * H * Et H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-13. No R1 R2 R3 a Rb R 4 R' R6 X Y R7 R' IX-13-1 'Pr H H H Et H CH3 F OH H H IX-13-2 'Pr H H CH 3 Et H CH3 F OH H H IX-13-3 'Pr H H CH(CH3) 2 Et H CH3 F OH H H IX-13-4 'Pr H H CH 2CH(CH3)2 Et H CH3 F OH H H IX-13-5 'Pr H H CH 2Ph Et H CH3 F OH H H IX-13-6 'Pr H H CH 2-indol-3-yl Et H CH3 F OH H H IX-13-7 'Pr H H CH 2CH2SCH 3 Et H CH3 F OH H H IX-13-8 'Pr * H * Et H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-14. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R IX-14-1 'Bu H H H Et H CH 3 F OH H H IX-14-2 'Bu H H CH 3 Et H CH 3 F OH H H IX-14-3 'Bu H H CH(CH3) 2 Et H CH 3 F OH H H IX-14-4 'Bu H H CH 2CH(CH3)2 Et H CH 3 F OH H H IX-14-5 'Bu H H CH 2Ph Et H CH 3 F OH H H IX-14-6 'Bu H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-14-7 'Bu H H CH 2CH2SCH 3 Et H CH 3 F OH H H IX-14-8 'Bu * H * Et H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_1 f _

Table IX-15. No R1 R2 R 3a R3b R 4 R5 R X Y R7 R' IX-15-1 Ph H H H Et H CH 3 F OH H H IX-15-2 Ph H H CH3 Et H CH 3 F OH H H IX-15-3 Ph H H CH(CH3) 2 Et H CH 3 F OH H H IX-15-4 Ph H H CH2CH(CH3)2 Et H CH 3 F OH H H IX-15-5 Ph H H CH 2Ph Et H CH 3 F OH H H IX-15-6 Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-15-7 Ph H H CH2CH2SCH 3 Et H CH 3 F OH H H IX-15-8 Ph * H * Et H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-16. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R IX-16-1 p-Me-Ph H H H Et H CH 3 F OH H H IX-16-2 p-Me-Ph H H CH 3 Et H CH 3 F OH H H IX-16-3 p-Me-Ph H H CH(CH3) 2 Et H CH 3 F OH H H IX-16-4 p-Me-Ph H H CH 2CH(CH3)2 Et H CH 3 F OH H H IX-16-5 p-Me-Ph H H CH 2Ph Et H CH 3 F OH H H IX-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H CH 3 F OH H H IX-16-8 p-Me-Ph * H * Et H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-17. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' IX-17-1 p-F-Ph H H H Et H CH 3 F OH H H IX-17-2 p-F-Ph H H CH3 Et H CH 3 F OH H H IX-17-3 p-F-Ph H H CH(CH3)2 Et H CH 3 F OH H H IX-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H CH 3 F OH H H IX-17-5 p-F-Ph H H CH 2Ph Et H CH 3 F OH H H IX-17-6 p-F-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-17-7 p-F-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH H H IX-17-8 p-F-Ph * H * Et H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

_ ,11 _

Table IX-18. N9 R1 R2 R 3 a R 3b R4 R R X Y R7 R' IX-18-1 p-Cl-Ph H H H Et H CH 3 F OH H H IX-18-2 p-Cl-Ph H H CH 3 Et H CH 3 F OH H H IX-18-3 p-Cl-Ph H H CH(CH3) 2 Et H CH 3 F OH H H IX-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H CH 3 F OH H H IX-18-5 p-Cl-Ph H H CH 2Ph Et H CH 3 F OH H H IX-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH H H IX-18-8 p-Cl-Ph * H * Et H CH 3 F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IX-19. Nt R R2 R3aR3b 6 R4 R5R X Y R7 R' IX-19-1 p-Br-Ph H H H Et H CH 3 F OH H H IX-19-2 p-Br-Ph H H CH3 Et H CH 3 F OH H H IX-19-3 p-Br-Ph H H CH(CH3) 2 Et H CH 3 F OH H H IX-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H CH 3 F OH H H IX-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 F OH H H IX-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH H H IX-19-8 p-Br-Ph * H * Et H CH 3 F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IX-20. N R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R IX-20-1 p-I-Ph H H H Et H CH 3 F OH H H IX-20-2 p-I-Ph H H CH 3 Et H CH 3 F OH H H IX-20-3 p-I-Ph H H CH(CH3) 2 Et H CH 3 F OH H H IX-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H CH 3 F OH H H IX-20-5 p-I-Ph H H CH 2Ph Et H CH 3 F OH H H IX-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH 3 F OH H H IX-20-7 p-I-Ph H H CH 2CH2SCH 3 Et H CH 3 F OH H H IX-20-8 p-I-Ph * H * Et H CH 3 F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

111l)-

Table IX-21. N9 R1 R2 R3 a R3b R4 R' R6 X Y R7 R' IX-21-1 CH 3 H H H 'Pr H CH 3 F OH H H IX-21-2 CH 3 H H CH3 'Pr H CH 3 F OH H H IX-21-3 CH 3 H H CH(CH3) 2 'Pr H CH 3 F OH H H IX-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H IX-21-5 CH 3 H H CH 2Ph 'Pr H CH 3 F OH H H IX-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H IX-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H CH 3 F OH H H IX-21-8 CH 3 * H * 'Pr H CH 3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-22. N9 Rl R2 R 3 a R3 b R4 R' R6 X Y R7 R' IX-22-1 Et H H H 'Pr H CH 3 F OH H H IX-22-2 Et H H CH3 'Pr H CH 3 F OH H H IX-22-3 Et H H CH(CH 3)2 'Pr H CH 3 F OH H H IX-22-4 Et H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H IX-22-5 Et H H CH2Ph 'Pr H CH 3 F OH H H IX-22-6 Et H H CH2-indol-3-yl 'Pr H CH 3 F OH H H IX-22-7 Et H H CH2CH 2SCH 3 'Pr H CH 3 F OH H H IX-22-8 Et * H * 'Pr H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-23. No R1 R2 R3a R3 R4 R5 R6 X Y R7 R' IX-23-1 'Pr H H H 'Pr H CH 3 F OH H H IX-23-2 'Pr H H CH 3 'Pr H CH 3 F OH H H IX-23-3 'Pr H H CH(CH3) 2 'Pr H CH 3 F OH H H IX-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH H H IX-23-5 'Pr H H CH 2Ph 'Pr H CH 3 F OH H H IX-23-6 'Pr H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H IX-23-7 Pr H H CH 2CH2SCH 3 'Pr H CH 3 F OH H H IX-23-8 Pr * H * 'Pr H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

t12-1

Table IX-24. R1 R2 R3 a R3 R4 R R' X Y R7 R' No IX-24-1 'Bu H H H 'Pr H CH 3 F OH H H IX-24-2 'Bu H H CH 3 'Pr H CH 3 F OH H H IX-24-3 'Bu H H CH(CH3) 2 'Pr H CH 3 F OH H H IX-24-4 'Bu H H CH 2CH(CH3)2 'Pr H CH 3 F OH H H IX-24-5 'Bu H H CH 2Ph 'Pr H CH 3 F OH H H IX-24-6 'Bu H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H IX-24-7 'Bu H H CH 2CH2SCH 3 'Pr H CH 3 F OH H H IX-24-8 'Bu * H * 'Pr H CH 3 F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table IX-25. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' IX-25-1 Ph H H H 'Pr H CH3 F OH H H IX-25-2 Ph H H CH3 'Pr H CH3 F OH H H IX-25-3 Ph H H CH(CH 3)2 'Pr H CH3 F OH H H IX-25-4 Ph H H CH2CH(CH 3) 2 'Pr H CH3 F OH H H IX-25-5 Ph H H CH 2Ph 'Pr H CH3 F OH H H IX-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH H H IX-25-7 Ph H H CH2CH2SCH 3 'Pr H CH3 F OH H H IX-25-8 Ph * H * 'Pr H CH3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-26. N9 R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' IX-26-1 p-Me-Ph H H H 'Pr H CH3 F OH H H IX-26-2 p-Me-Ph H H CH 3 'Pr H CH3 F OH H H IX-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H CH3 F OH H H IX-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr H CH3 F OH H H IX-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH3 F OH H H IX-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH H H IX-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H CH3 F OH H H IX-26-8 p-Me-Ph * H * 'Pr H CH3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_11 A

Table IX-27. N9 R1 R2 R3 a R3b R4 R' R' X Y R7 R' IX-27-1 p-F-Ph H H H 'Pr H CH 3 F OH H H IX-27-2 p-F-Ph H H CH3 'Pr H CH 3 F OH H H IX-27-3 p-F-Ph H H CH(CH3)2 'Pr H CH 3 F OH H H IX-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H IX-27-5 p-F-Ph H H CH 2Ph 'Pr H CH 3 F OH H H IX-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH H H IX-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H CH3 F OH H H IX-27-8 p-F-Ph * H * 'Pr H CH3 F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table IX-28. N9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' IX-28-1 p-Cl-Ph H H H 'Pr H CH 3 F OH H H IX-28-2 p-Cl-Ph H H CH 3 'Pr H CH 3 F OH H H IX-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H IX-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr H CH 3 F OH H H IX-28-5 p-Cl-Ph H H CH 2Ph 'Pr H CH 3 F OH H H IX-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H IX-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH H H IX-28-8 p-Cl-Ph * H * 'Pr H CH 3 F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IX-29. N9 R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' IX-29-1 p-Br-Ph H H H 'Pr H CH 3 F OH H H IX-29-2 p-Br-Ph H H CH3 'Pr H CH 3 F OH H H IX-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H CH 3 F OH H H IX-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH H H IX-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 F OH H H IX-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH H H IX-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H CH 3 F OH H H IX-29-8 p-Br-Ph * H * 'Pr H CH 3 F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IX-30. R1 R 2 R 3a R3b R4 R' R' X Y R7 R' N9 IX-30-1 p-I-Ph H H H 'Pr H CH3 F OH H H IX-30-2 p-I-Ph H H CH 3 'Pr H CH3 F OH H H IX-30-3 p-I-Ph H H CH(CH3) 2 'Pr H CH3 F OH H H IX-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr H CH3 F OH H H IX-30-5 p-I-Ph H H CH 2Ph 'Pr H CH3 F OH H H IX-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH H H IX-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H CH3 F OH H H IX-30-8 p-I-Ph * H * 'Pr H CH3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-31. No R1 R2 R3a R3b R4 R 5 R6 X Y R7 R' IX-31-1 CH 3 H H H "Bu H CH 3 F OH H H IX-31-2 CH 3 H H CH3 "Bu H CH 3 F OH H H IX-31-3 CH 3 H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-31-4 CH 3 H H CH2CH(CH3) 2 "Bu H CH 3 F OH H H IX-31-5 CH 3 H H CH 2Ph "Bu H CH 3 F OH H H IX-31-6 CH 3 H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H CH 3 F OH H H IX-31-8 CH 3 * H * "Bu H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-32. No R1 R2 R 3a R 3b R4 R5 R6 X Y R7 R'

IX-32-1 Et H H H "Bu H CH 3 F OH H H IX-32-2 Et H H CH3 "Bu H CH 3 F OH H H IX-32-3 Et H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-32-4 Et H H CH2CH(CH3) 2 "Bu H CH 3 F OH H H IX-32-5 Et H H CH2Ph "Bu H CH 3 F OH H H IX-32-6 Et H H CH2-indol-3-yl "Bu H CH 3 F OH H H IX-32-7 Et H H CH2CH 2SCH 3 "Bu H CH 3 F OH H H IX-32-8 Et * H * "Bu H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-33. R1 R2 R3 a R3 R4 R' R X Y R7 R' No IX-33-1 'Pr H H H "Bu H CH3 F OH H H IX-33-2 'Pr H H CH 3 "Bu H CH3 F OH H H IX-33-3 'Pr H H CH(CH3) 2 "Bu H CH3 F OH H H IX-33-4 'Pr H H CH 2CH(CH3)2 "Bu H CH3 F OH H H IX-33-5 'Pr H H CH 2Ph "Bu H CH3 F OH H H IX-33-6 'Pr H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-33-7 'Pr H H CH 2CH2 SCH 3 "Bu H CH 3 F OH H H IX-33-8 'Pr * H * "Bu H CH 3 F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table IX-34. No R1 R2 R3 a Rb R4 R' R6 X Y R7 R IX-34-1 'Bu H H H "Bu H CH 3 F OH H H IX-34-2 'Bu H H CH 3 "Bu H CH 3 F OH H H IX-34-3 'Bu H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-34-4 'Bu H H CH 2CH(CH 3)2 "Bu H CH 3 F OH H H IX-34-5 'Bu H H CH 2Ph "Bu H CH 3 F OH H H IX-34-6 'Bu H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-34-7 'Bu H H CH 2CH2SCH 3 "Bu H CH 3 F OH H H IX-34-8 'Bu * H * "Bu H CH 3 F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-35. R1 N R2 R 3a R3b R4 R5 R6 X Y R7 R'

IX-35-1 Ph H H H "Bu H CH 3 F OH H H IX-35-2 Ph H H CH3 "Bu H CH 3 F OH H H IX-35-3 Ph H H CH(CH 3 )2 "Bu H CH 3 F OH H H IX-35-4 Ph H H CH2CH(CH3)2 "Bu H CH 3 F OH H H IX-35-5 Ph H H CH 2 Ph "Bu H CH 3 F OH H H IX-35-6 Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-35-7 Ph H H CH2 CH2 SCH 3 "Bu H CH 3 F OH H H IX-35-8 Ph * H * "Bu H CH 3 F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

'1 '7 _

Table IX-36. N9 R1 R 2 R 3a R 3b R4 R' R6 X Y R7 R' IX-36-1 p-Me-Ph H H H "Bu H CH 3 F OH H H IX-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 F OH H H IX-36-3 p-Me-Ph H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-36-4 p-Me-Ph H H CH 2CH(CH3)2 "Bu H CH 3 F OH H H IX-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 F OH H H IX-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH H H IX-36-8 p-Me-Ph * H * "Bu H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-37. N R1 R2 R3a R3 R4 R' R6 X Y R7 R' IX-37-1 p-F-Ph H H H "Bu H CH 3 F OH H H IX-37-2 p-F-Ph H H CH3 "Bu H CH 3 F OH H H IX-37-3 p-F-Ph H H CH(CH3)2 "Bu H CH 3 F OH H H IX-37-4 p-F-Ph H H CH2 CH(CH3) 2 "Bu H CH 3 F OH H H IX-37-5 p-F-Ph H H CH 2 Ph "Bu H CH 3 F OH H H IX-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-37-7 p-F-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 F OH H H IX-37-8 p-F-Ph * H * "Bu H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-38. R N9 R1 R2 R3 a R 3b R4 R X Y R7 R' IX-38-1 p-Cl-Ph H H H "Bu H CH 3 F OH H H IX-38-2 p-Cl-Ph H H CH 3 "Bu H CH 3 F OH H H IX-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H CH 3 F OH H H IX-38-5 p-Cl-Ph H H CH 2Ph "Bu H CH 3 F OH H H IX-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH H H IX-38-8 p-Cl-Ph * H * "Bu H CH 3 F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 1Q

Table IX-39. N9 R1 R2 R 3a R 3 b R4 R' R6 X Y R7 R' IX-39-1 p-Br-Ph H H H "Bu H CH 3 F OH H H IX-39-2 p-Br-Ph H H CH3 "Bu H CH 3 F OH H H IX-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-39-4 p-Br-Ph H H CH2CH(CH3) 2 "Bu H CH 3 F OH H H IX-39-5 p-Br-Ph H H CH 2Ph "Bu H CH 3 F OH H H IX-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-39-7 p-Br-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 F OH H H IX-39-8 p-Br-Ph * H * "Bu H CH 3 F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-40. N R1 R2 R3a R3b R4 R' R6 X Y R7 R' IX-40-1 p-I-Ph H H H "Bu H CH 3 F OH H H IX-40-2 p-I-Ph H H CH 3 "Bu H CH 3 F OH H H IX-40-3 p-I-Ph H H CH(CH3) 2 "Bu H CH 3 F OH H H IX-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu H CH 3 F OH H H IX-40-5 p-I-Ph H H CH 2Ph "Bu H CH 3 F OH H H IX-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH H H IX-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH H H IX-40-8 p-I-Ph * H * "Bu H CH 3 F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-41. N9 R1 R2 R3a R3b R4 R5 R6 X Y R7 R' IX-41-1 CH 3 H H H Bz H CH 3 F OH H H IX-41-2 CH 3 H H CH3 Bz H CH 3 F OH H H IX-41-3 CH 3 H H CH(CH3) 2 Bz H CH 3 F OH H H IX-41-4 CH 3 H H CH2 CH(CH3) 2 Bz H CH 3 F OH H H IX-41-5 CH 3 H H CH 2Ph Bz H CH 3 F OH H H IX-41-6 CH 3 H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-41-7 CH 3 H H CH2CH 2SCH 3 Bz H CH 3 F OH H H IX-41-8 CH 3 * H * Bz H CH 3 F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 1Q _

Table IX-42. Rl R2 R 3 a R 3b R4 R' R' X Y R7 R' N9 IX-42-1 Et H H H Bz H CH 3 F OH H H IX-42-2 Et H H CH3 Bz H CH 3 F OH H H IX-42-3 Et H H CH(CH3) 2 Bz H CH 3 F OH H H IX-42-4 Et H H CH2CH(CH3) 2 Bz H CH 3 F OH H H IX-42-5 Et H H CH2Ph Bz H CH 3 F OH H H IX-42-6 Et H H CH2-indol-3-yl Bz H CH 3 F OH H H IX-42-7 Et H H CH2CH 2SCH 3 Bz H CH 3 F OH H H IX-42-8 Et * H * Bz H CH 3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-43. No R R2 R3 a Rb R4 R R6 X Y R7 R' IX-43-1 'Pr H H H Bz H CH 3 F OH H H IX-43-2 'Pr H H CH 3 Bz H CH 3 F OH H IA IX-43-3 'Pr H H CH(CH3) 2 Bz H CH 3 F OH H H IX-43-4 'Pr H H CH 2CH(CH3)2 Bz H CH 3 F OH H H IX-43-5 'Pr H H CH 2Ph Bz H CH 3 F OH H H IX-43-6 'Pr H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-43-7 'Pr H H CH 2CH2SCH 3 Bz H CH 3 F OH H H IX-43-8 'Pr * H * Bz H CH 3 F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-44. No R R2 R3 a Rb R4 R R6 X Y R7 R' IX-44-1 'Bu H H H Bz H CH 3 F OH H H IX-44-2 'Bu H H CH 3 Bz H CH 3 F OH H H IX-44-3 'Bu H H CH(CH3) 2 Bz H CH 3 F OH H H IX-44-4 'Bu H H CH 2CH(CH3)2 Bz H CH 3 F OH H H IX-44-5 'Bu H H CH 2Ph Bz H CH 3 F OH H H IX-44-6 'Bu H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-44-7 'Bu H H CH 2CH2SCH 3 Bz H CH 3 F OH H H IX-44-8 'Bu * H * Bz H CH 3 F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-45. No R1 R2 R 3a R3b R4 R5 R X Y R7 R' IX-45-1 Ph H H H Bz H CH 3 F OH H H IX-45-2 Ph H H CH3 Bz H CH 3 F OH H H IX-45-3 Ph H H CH(CH 3)2 Bz H CH 3 F OH H H IX-45-4 Ph H H CH2CH(CH 3) 2 Bz H CH 3 F OH H H IX-45-5 Ph H H CH 2Ph Bz H CH 3 F OH H H IX-45-6 Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-45-7 Ph H H CH2CH2SCH 3 Bz H CH 3 F OH H H IX-45-8 Ph * H * Bz H CH 3 F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-46. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' IX-46-1 p-Me-Ph H H H Bz H CH 3 F OH H H IX-46-2 p-Me-Ph H H CH 3 Bz H CH 3 F OH H H IX-46-3 p-Me-Ph H H CH(CH 3)2 Bz H CH 3 F OH H H IX-46-4 p-Me-Ph H H CH 2CH(CH3)2 Bz H CH 3 F OH H H IX-46-5 p-Me-Ph H H CH 2Ph Bz H CH 3 F OH H H IX-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH H H IX-46-8 p-Me-Ph * H * Bz H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-47. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' IX-47-1 p-F-Ph H H H Bz H CH 3 F OH H H IX-47-2 p-F-Ph H H CH3 Bz H CH 3 F OH H H IX-47-3 p-F-Ph H H CH(CH3)2 Bz H CH 3 F OH H H IX-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H CH 3 F OH H H IX-47-5 p-F-Ph H H CH 2Ph Bz H CH 3 F OH H H IX-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH H H IX-47-8 p-F-Ph * H * Bz H CH 3 F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table IX-48. N9 R1 R2 R 3 a R 3b R4 R5 R X Y R7 R' IX-48-1 p-Cl-Ph H H H Bz H CH 3 F OH H H IX-48-2 p-Cl-Ph H H CH 3 Bz H CH 3 F OH H H IX-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H CH 3 F OH H H IX-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H CH 3 F OH H H IX-48-5 p-Cl-Ph H H CH 2Ph Bz H CH 3 F OH H H IX-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H CH 3 F OH H H IX-48-8 p-Cl-Ph * H * Bz H CH 3 F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table IX-49. 2 R3a3b 6 Nt R R R R4 R' R XY R7 R'

IX-49-1 p-Br-Ph H H H Bz H CH3 F OH H H IX-49-2 p-Br-Ph H H CH3 Bz H CH3 F OH H H IX-49-3 p-Br-Ph H H CH(CH3) 2 Bz H CH3 F OH H H IX-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H CH3 F OH H H IX-49-5 p-Br-Ph H H CH 2Ph Bz H CH3 F OH H H IX-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH3 F OH H H IX-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H CH3 F OH H H IX-49-8 p-Br-Ph * H * Bz H CH3 F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table IX-50. N R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' IX-50-1 p-I-Ph H H H Bz H CH 3 F OH H H IX-50-2 p-I-Ph H H CH 3 Bz H CH 3 F OH H H IX-50-3 p-I-Ph H H CH(CH3) 2 Bz H CH 3 F OH H H IX-50-4 p-I-Ph H H CH 2CH(CH3)2 Bz H CH 3 F OH H H IX-50-5 p-I-Ph H H CH 2Ph Bz H CH 3 F OH H H IX-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH H H IX-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH H H IX-50-8 p-I-Ph * H * Bz H CH 3 F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

R8 NH

R3 b R2 N O R3N-P -- 0 ON 0

C0 2R 4 OR' R5 R6

Y X

x Table X-1. 6 No R R2 R 3 a R3 b R4 R R X Y R7 R' X-1-1 CH 3 H H H CH 3 H F F OH H H X-1-2 CH 3 H H CH 3 CH 3 H F F OH H H X-1-3 CH 3 H H CH(CH 3) 2 CH 3 H F F OH H H X-1-4 CH 3 H H CH 2CH(CH 3) 2 CH 3 H F F OH H H X-1-5 CH 3 H H CH 2Ph CH 3 H F F OH H H X-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H F F OH H H X-1-7 CH 3 H H CH 2CH 2SCH 3 CH 3 H F F OH H H X-1-8 CH 3 * H * CH 3 H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-2. N9 Rl R2 R3 a R 3b R4 R5 R6 X Y R7 R' X-2-1 Et H H H CH 3 H F F OH H H X-2-2 Et H H CH 3 CH 3 H F F OH H H X-2-3 Et H H CH(CH 3) 2 CH 3 H F F OH H H X-2-4 Et H H CH 2CH(CH 3) 2 CH 3 H F F OH H H X-2-5 Et H H CH 2Ph CH 3 H F F OH H H X-2-6 Et H H CH 2-indol-3-yl CH 3 H F F OH H H X-2-7 Et H H CH 2CH 2SCH 3 CH 3 H F F OH H H X-2-8 Et * H * CH 3 H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-3. No R1 R2 R3 a R 3b R4 R' R6 X Y R7 R' X-3-1 'Pr H H H CH 3 H F F OH H H X-3-2 'Pr H H CH 3 CH3 H F F OH H H X-3-3 'Pr H H CH(CH 3)2 CH3 H F F OH H H X-3-4 Pr H H CH 2CH(CH 3) 2 CH 3 H F F OH H H X-3-5 Pr H H CH 2Ph CH 3 H F F OH H H X-3-6 Pr H H CH 2-indol-3-yl CH3 H F F OH H H X-3-7 Pr H H CH 2CH 2SCH3 CH3 H F F OH H H X-3-8 Pr * H * CH 3 H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-4. N9 R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' X-4-1 'Bu H H H CH 3 H F F OH H H X-4-2 'Bu H H CH 3 CH3 H F F OH H H X-4-3 'Bu H H CH(CH3) 2 CH3 H F F OH H H X-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H F F OH H H X-4-5 'Bu H H CH 2Ph CH 3 H F F OH H H X-4-6 'Bu H H CH 2-indol-3-yl CH3 H F F OH H H X-4-7 'Bu H H CH 2CH2SCH 3 CH3 H F F OH H H X-4-8 'Bu * H * CH 3 H F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-5. N9 R1 R2 R 3 a R 3b R4 R 5 R6 X Y R7 R' X-5-1 Ph H H H CH3 H F F OH H H X-5-2 Ph H H CH 3 CH3 H F F OH H H X-5-3 Ph H H CH(CH3)2 CH3 H F F OH H H X-5-4 Ph H H CH 2CH(CH3) 2 CH3 H F F OH H H X-5-5 Ph H H CH 2Ph CH3 H F F OH H H X-5-6 Ph H H CH 2-indol-3-yl CH3 H F F OH H H X-5-7 Ph H H CH 2CH 2SCH 3 CH3 H F F OH H H X-5-8 Ph * H * CH 3 H F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

'))A-

Table X-6. N9 R1 R2 R 3a R 3b R4 R' R6 X Y R7 R' X-6-1 p-Me-Ph H H H CH3 H F F OH H H X-6-2 p-Me-Ph H H CH 3 CH3 H F F OH H H X-6-3 p-Me-Ph H H CH(CH3)2 CH3 H F F OH H H X-6-4 p-Me-Ph H H CH 2CH(CH3) 2 CH3 H F F OH H H X-6-5 p-Me-Ph H H CH 2Ph CH3 H F F OH H H X-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F F OH H H X-6-7 p-Me-Ph H H CH 2CH 2SCH 3 CH3 H F F OH H H X-6-8 p-Me-Ph * H * CH3 H F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-7. N9 R1 R2 R3a R3 b R4 R 5 R6 X Y R7 R' X-7-1 p-F-Ph H H H CH 3 H F F OH H H X-7-2 p-F-Ph H H CH3 CH3 H F F OH H H X-7-3 p-F-Ph H H CH(CH3)2 CH3 H F F OH H H X-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H F F OH H H X-7-6 p-F-Ph H H CH 2Ph CH 3 H F F OH H H X-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F F OH H H X-7-8 p-F-Ph H H CH2CH2 SCH3 CH3 H F F OH H H X-7-20 p-F-Ph * H * CH3 H F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-8. 9 RI 1 R2 R3 a R3 R4 R 5 R6 X Y R7 R' X-8-1 p-Cl-Ph H H H CH 3 H F F OH H H X-8-2 p-Cl-Ph H H CH 3 CH 3 H F F OH H H X-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F F OH H H X-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H F F OH H H X-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F F OH H H X-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F F OH H H X-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H F F OH H H X-8-8 p-Cl-Ph * H * CH 3 H F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-9. 5 N9 R1 R2 R3a R3b R4 R R' X Y R7 R' X-9-1 p-Br-Ph H H H CH3 H F F OH H H X-9-2 p-Br-Ph H H CH 3 CH 3 H F F OH H H X-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H F F OH H H X-9-4 p-Br-Ph H H CH 2CH(CH3) 2 CH3 H F F OH H H X-9-6 p-Br-Ph H H CH 2Ph CH3 H F F OH H H X-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H F F OH H H X-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH3 H F F OH H H X-9-20 p-Br-Ph * H * CH3 H F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-10. N R1 R2 R3a R3 R4 R 5 R6 X Y R7 R' X-10-1 p-I-Ph H H H CH 3 H F F OH H H X-10-2 p-I-Ph H H CH3 CH3 H F F OH H H X-10-3 p-I-Ph H H CH(CH3)2 CH3 H F F OH H H X-10-4 p-I-Ph H H CH2CH(CH3) 2 CH3 H F F OH H H X-10-5 p-I-Ph H H CH 2Ph CH 3 H F F OH H H X-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H F F OH H H X-10-7 p-I-Ph H H CH2CH 2SCH 3 CH3 H F F OH H H X-10-8 p-I-Ph * H * CH 3 H F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-11. No9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' X-11-1 CH3 H H H Et H F F OH H H X-11-2 CH3 H H CH3 Et H F F OH H H X-11-3 CH3 H H CH(CH3) 2 Et H F F OH H H X-11-4 CH3 H H CH2CH(CH3) 2 Et H F F OH H H X-11-5 CH3 H H CH 2Ph Et H F F OH H H X-11-6 CH3 H H CH 2-indol-3-yl Et H F F OH H H X-11-7 CH3 H H CH2CH 2SCH 3 Et H F F OH H H X-11-8 CH3 * H * Et H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

IMg-

Table X-12. N9 Rl R 2 R 3 a R3b R4 R 5 R6 X Y R7 R' X-12-1 Et H H H Et H F F OH H H X-12-2 Et H H CH 3 Et H F F OH H H X-12-3 Et H H CH(CH3) 2 Et H F F OH H H X-12-4 Et H H CH 2CH(CH3) 2 Et H F F OH H H X-12-5 Et H H CH 2Ph Et H F F OH H H X-12-6 Et H H CH 2-indol-3-yl Et H F F OH H H X-12-7 Et H H CH 2CH 2SCH 3 Et H F F OH H H X-12-8 Et * H * FtH F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-13. N R R 2 R3 a RR R4 R' R X Y R7 R X-13-1 'Pr H H H Et H F F OH H H X-13-2 'Pr H H CH 3 Et H F F OH H H X-13-3 'Pr H H CH(CH3) 2 Et H F F OH H H X-13-4 'Pr H H CH 2CH(CH3)2 Et H F F OH H H X-13-5 'Pr H H CH 2Ph Et H F F OH H H X-13-6 'Pr H H CH 2-indol-3-yl Et H F F OH H H X-13-7 'Pr H H CH 2CH2SCH 3 Et H F F OH H H X-13-8 'Pr * H * Et H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-14. No R1 R2 R R3b R4 R5 R6 X Y R7 R' 3a

X-14-1 'Bu H H H Et H F F OH H H X-14-2 'Bu H H CH 3 Et H F F OH H H X-14-3 'Bu H H CH(CH3) 2 Et H F F OH H H X-14-4 'Bu H H CH 2CH(CH3)2 Et H F F OH H H X-14-5 'Bu H H CH 2Ph Et H F F OH H H X-14-6 'Bu H H CH 2-indol-3-yl Et H F F OH H H X-14-7 'Bu H H CH 2CH2SCH 3 Et H F F OH H H X-14-8 'Bu * H * Et H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'))7-

Table X-15. No9 R1 R 2 R3 a R3b R4 R5 R6 X Y R7 R' X-15-1 Ph H H H Et H F F OH H H X-15-2 Ph H H CH3 Et H F F OH H H X-15-3 Ph H H CH(CH3)2 Et H F F OH H H X-15-4 Ph H H CH2CH(CH3) 2 Et H F F OH H H X-15-5 Ph H H CH 2Ph Et H F F OH H H X-15-6 Ph H H CH 2-indol-3-yl Et H F F OH H H X-15-7 Ph H H CH2CH 2SCH 3 Et H F F OH H H X-15-8 Ph * H * Et H F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table X-16. N R1 R2 R3a R3 b R4 R5 R6 X Y R7 R X-16-1 p-Me-Ph H H H Et H F F OH H H X-16-2 p-Me-Ph H H CH3 Et H F F OH H H X-16-3 p-Me-Ph H H CH(CH3)2 Et H F F OH H H X-16-4 p-Me-Ph H H CH2CH(CH3) 2 Et H F F OH H H X-16-5 p-Me-Ph H H CH 2Ph Et H F F OH H H X-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F F OH H H X-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H F F OH H H X-16-8 p-Me-Ph * H * Et H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-17. N R1 R2 R3 a R 3b R4 R 5 R6 X Y R7 R' X-17-1 p-F-Ph H H H Et H F F OH H H X-17-2 p-F-Ph H H CH3 Et H F F OH H H X-17-3 p-F-Ph H H CH(CH3)2 Et H F F OH H H X-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H F F OH H H X-17-5 p-F-Ph H H CH 2Ph Et H F F OH H H X-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F F OH H H X-17-7 p-F-Ph H H CH2CH2 SCH3 Et H F F OH H H X-17-8 p-F-Ph * H * Et H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

)Q-s

Table X-18. N R1 R 2 RaR3 b R 4 R R X Y R7 R' X-18-1 p-Cl-Ph H H H Et H F F OH H H X-18-2 p-Cl-Ph H H CH 3 Et H F F OH H H X-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F F OH H H X-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H F F OH H H X-18-5 p-Cl-Ph H H CH 2Ph Et H F F OH H H X-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F F OH H H X-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et H F F OH H H X-18-8 p-Cl-Ph * H * Et H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-19. N9 R1 R2 R3a R3 b R4 R 5 R6 X Y R7 R' X-19-1 p-Br-Ph H H H Et H F F OH H H X-19-2 p-Br-Ph H H CH 3 Et H F F OH H H X-19-3 p-Br-Ph H H CH(CH3) 2 Et H F F OH H H X-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et H F F OH H H X-19-5 p-Br-Ph H H CH 2Ph Et H F F OH H H X-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F F OH H H X-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H F F OH H H X-19-8 p-Br-Ph * H * Et H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-20. R1 R2 R 3 a R3 b R4 R5 R 6 X Y R7 N X-20-1 p-I-Ph H H H Et H F F OH H X-20-2 p-I-Ph H H CH3 Et H F F OH H X-20-3 p-I-Ph H H CH(CH3)2 Et H F F OH H X-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H F F OH H X-20-5 p-I-Ph H H CH 2Ph Et H F F OH H X-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F F OH H X-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H F F OH H X-20-8 p-I-Ph * H * Et H F F OH H

*R2 and R 3b joined together by (CH2)3 to form five-membered ring.

Table X-21. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' X-21-1 CH3 H H H 'Pr H F F OH H H X-21-2 CH3 H H CH3 'Pr H F F OH H H X-21-3 CH3 H H CH(CH3) 2 'Pr H F F OH H H X-21-4 CH3 H H CH2CH(CH3) 2 'Pr H F F OH H H X-21-5 CH3 H H CH 2Ph 'Pr H F F OH H H X-21-6 CH3 H H CH 2-indol-3-yl 'Pr H F F OH H H X-21-7 CH3 H H CH2CH 2SCH 3 'Pr H F F OH H H X-21-8 CH3 * H * 'Pr H F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table X-22. N9 Rl R 2 R 3 a R3 b R4 R' R6 X Y R7 R' X-22-1 Et H H H 'Pr H F F OH H H X-22-2 Et H H CH 3 'Pr H F F OH H H X-22-3 Et H H CH(CH 3)2 'Pr H F F OH H H X-22-4 Et H H CH 2CH(CH3) 2 'Pr H F F OH H H X-22-5 Et H H CH 2Ph 'Pr H F F OH H H X-22-6 Et H H CH 2-indol-3-yl 'Pr H F F OH H H X-22-7 Et H H CH 2CH 2SCH 3 'Pr H F F OH H H X-22-8 Et * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-23. No9 R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' X-23-1 'Pr H H H 'Pr H F F OH H H X-23-2 'Pr H H CH 3 'Pr H F F OH H H X-23-3 'Pr H H CH(CH 3)2 'Pr H F F OH H H X-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H F F OH H H X-23-5 Pr H H CH 2Ph 'Pr H F F OH H H X-23-6 Pr H H CH 2-indol-3-yl 'Pr H F F OH H H X-23-7 Pr H H CH 2CH2SCH 3 'Pr H F F OH H H X-23-8 Pr * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-24. N9 R1 R2 R3 a R3 R4 R R' X Y R7 R' X-24-1 'Bu H H H 'Pr H F F OH H H X-24-2 'Bu H H CH 3 'Pr H F F OH H H X-24-3 'Bu H H CH(CH3) 2 'Pr H F F OH H H X-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H F F OH H H X-24-5 'Bu H H CH 2Ph 'Pr H F F OH H H X-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F F OH H H X-24-7 'Bu H H CH 2CH2SCH 3 'Pr H F F OH H H X-24-8 'Bu * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-25. N9 R1 R 2 R3 a R3 b R4 R5 R6 X Y R7 R' X-25-1 Ph H H H 'Pr H F F OH H H X-25-2 Ph H H CH3 'Pr H F F OH H H X-25-3 Ph H H CH(CH 3) 2 'Pr H F F OH H H X-25-4 Ph H H CH2CH(CH 3) 2 'Pr H F F OH H H X-25-5 Ph H H CH 2Ph 'Pr H F F OH H H X-25-6 Ph H H CH 2-indol-3-yl 'Pr H F F OH H H X-25-7 Ph H H CH2CH 2SCH 3 'Pr H F F OH H H X-25-8 Ph * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-26. N R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' X-26-1 p-Me-Ph H H H 'Pr H F F OH H H X-26-2 p-Me-Ph H H CH3 'Pr H F F OH H H X-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr H F F OH H H X-26-4 p-Me-Ph H H CH2CH(CH 3) 2 'Pr H F F OH H H X-26-5 p-Me-Ph H H CH 2Ph 'Pr H F F OH H H X-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H X-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H F F OH H H X-26-8 p-Me-Ph * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-27. N R1 R2 R3 a R 3b R4 R' R' X Y R7 R' X-27-1 p-F-Ph H H H 'Pr H F F OH H H X-27-2 p-F-Ph H H CH3 'Pr H F F OH H H X-27-3 p-F-Ph H H CH(CH3)2 'Pr H F F OH H H X-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H F F OH H H X-27-5 p-F-Ph H H CH 2Ph 'Pr H F F OH H H X-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H X-27-7 p-F-Ph H H CH2CH2 SCH3 'Pr H F F OH H H X-27-8 p-F-Ph * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-28. N9 R1 R2 R 3a R3 b R4 R R6 X Y R7 R' X-28-1 p-Cl-Ph H H H 'Pr H F F OH H H X-28-2 p-Cl-Ph H H CH 3 'Pr H F F OH H H X-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F F OH H H X-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr H F F OH H H X-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F F OH H H X-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H X-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr H F F OH H H X-28-8 p-Cl-Ph * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-29. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' X-29-1 p-Br-Ph H H H Pr H F F OH H H X-29-2 p-Br-Ph H H CH 3 'Pr H F F OH H H X-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F F OH H H X-29-4 p-Br-Ph H H CH 2CH(CH3) 2 'Pr H F F OH H H X-29-5 p-Br-Ph H H CH 2Ph 'Pr H F F OH H H X-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H X-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr H F F OH H H X-29-8 p-Br-Ph * H * Pr H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-30. N9 R1 R2 R3 a R3b R4 R' R' X Y R7 R' X-30-1 p-I-Ph H H H 'Pr H F F OH H H X-30-2 p-I-Ph H H CH3 'Pr H F F OH H H X-30-3 p-I-Ph H H CH(CH3)2 'Pr H F F OH H H X-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H F F OH H H X-30-5 p-I-Ph H H CH 2Ph 'Pr H F F OH H H X-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F F OH H H X-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H F F OH H H X-30-8 p-I-Ph * H * 'Pr H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-31. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' X-31-1 CH3 H H H "Bu H F F OH H H X-31-2 CH3 H H CH3 "Bu H F F OH H H X-31-3 CH3 H H CH(CH3) 2 "Bu H F F OH H H X-31-4 CH3 H H CH2CH(CH3) 2 "Bu H F F OH H H X-31-5 CH3 H H CH 2Ph "Bu H F F OH H H X-31-6 CH3 H H CH 2-indol-3-yl "Bu H F F OH H H X-31-7 CH3 H H CH2CH 2SCH 3 "Bu H F F OH H H X-31-8 CH3 * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-32. No R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R'

X-32-1 Et H H H "Bu H F F OH H H X-32-2 Et H H CH 3 "Bu H F F OH H H X-32-3 Et H H CH(CH3) 2 "Bu H F F OH H H X-32-4 Et H H CH 2CH(CH3) 2 "Bu H F F OH H H X-32-5 Et H H CH 2Ph "Bu H F F OH H H X-32-6 Et H H CH 2-indol-3-yl "Bu H F F OH H H X-32-7 Et H H CH 2CH 2SCH 3 "Bu H F F OH H H X-32-8 Et * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-33. No R1 R2 R 3a R3b R4 R' R' X Y R7 R' X-33-1 'Pr H H H "Bu H F F OH H H X-33-2 'Pr H H CH 3 "Bu H F F OH H H X-33-3 'Pr H H CH(CH 3)2 "Bu H F F OH H H X-33-4 Pr H H CH 2CH(CH 3) 2 "Bu H F F OH H H X-33-5 Pr H H CH 2Ph "Bu H F F OH H H X-33-6 Pr H H CH 2-indol-3-yl "Bu H F F OH H H X-33-7 Pr H H CH 2 CH2 SCH 3 "Bu H F F OH H H X-33-8 Pr * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-34. No R1 R2 R3a Rb R4 R R6 X Y R7 R' X-34-1 'Bu H H H "Bu H F F OH H H X-34-2 'Bu H H CH 3 "Bu H F F OH H H X-34-3 'Bu H H CH(CH3) 2 "Bu H F F OH H H X-34-4 'Bu H H CH 2CH(CH3)2 "Bu H F F OH H H X-34-5 'Bu H H CH 2Ph "Bu H F F OH H H X-34-6 'Bu H H CH 2-indol-3-yl "Bu H F F OH H H X-34-7 'Bu H H CH 2CH2SCH 3 "Bu H F F OH H H X-34-8 'Bu * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-35. R 3 N R 2 R3 a R R4 R R6 X Y R7 R

X-35-1 Ph H H H "Bu H F F OH H H X-35-2 Ph H H CH3 "Bu H F F OH H H X-35-3 Ph H H CH(CH3)2 "Bu H F F OH H H X-35-4 Ph H H CH2CH(CH3) 2 "Bu H F F OH H H X-35-5 Ph H H CH 2 Ph "Bu H F F OH H H X-35-6 Ph H H CH 2-indol-3-yl "Bu H F F OH H H X-35-7 Ph H H CH2 CH 2 SCH 3 "Bu H F F OH H H X-35-8 Ph * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-36. N9 R1 R2 R3a R3b R4 R' R6 X Y R7 R' X-36-1 p-Me-Ph H H H "Bu H F F OH H H X-36-2 p-Me-Ph H H CH3 "Bu H F F OH H H X-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F F OH H H X-36-4 p-Me-Ph H H CH2CH(CH3) 2 "Bu H F F OH H H X-36-5 p-Me-Ph H H CH 2Ph "Bu H F F OH H H X-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F F OH H H X-36-7 p-Me-Ph H H CH2 CH 2 SCH 3 "Bu H F F OH H H X-36-8 p-Me-Ph * H * "Bu H F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table X-37. 6 N9 R1 R2 R 3a R3 b R4 R' R X Y R7 R' X-37-1 p-F-Ph H H H "Bu H F F OH H H X-37-2 p-F-Ph H H CH3 "Bu H F F OH H H X-37-3 p-F-Ph H H CH(CH3)2 "Bu H F F OH H H X-37-4 p-F-Ph H H CH2 CH(CH3) 2 "Bu H F F OH H H X-37-5 p-F-Ph H H CH 2Ph "Bu H F F OH H H X-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F F OH H H X-37-7 p-F-Ph H H CH2 CH2 SCH3 "Bu H F F OH H H X-37-8 p-F-Ph * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-38. N9 R1 R 2 R 3a R 3b R4 R R X Y R7 R' X-38-1 p-Cl-Ph H H H "Bu H F F OH H H X-38-2 p-Cl-Ph H H CH 3 "Bu H F F OH H H X-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F F OH H H X-38-4 p-Cl-Ph H H CH 2 CH(CH3)2 "Bu H F F OH H H X-38-5 p-Cl-Ph H H CH 2 Ph "Bu H F F OH H H X-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F F OH H H X-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH H H X-38-8 p-Cl-Ph * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-39. N9 R1 R2 R3a R3b R4 R 5 R6 X Y R7 R' X-39-1 p-Br-Ph H H H "Bu H F F OH H H X-39-2 p-Br-Ph H H CH 3 "Bu H F F OH H H X-39-3 p-Br-Ph H H CH(CH 3)2 "Bu H F F OH H H X-39-4 p-Br-Ph H H CH 2CH(CH3) 2 "Bu H F F OH H H X-39-5 p-Br-Ph H H CH 2Ph "Bu H F F OH H H X-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F F OH H H X-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH H H X-39-8 p-Br-Ph * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-40. N R1 R 2 R3 a R3 R4 R' R6 X Y R7 R' X-40-1 p-I-Ph H H H "Bu H F F OH H H X-40-2 p-I-Ph H H CH3 "Bu H F F OH H H X-40-3 p-I-Ph H H CH(CH3)2 "Bu H F F OH H H X-40-4 p-I-Ph H H CH2CH(CH3) 2 "Bu H F F OH H H X-40-5 p-I-Ph H H CH 2Ph "Bu H F F OH H H X-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F F OH H H X-40-7 p-I-Ph H H CH2CH 2SCH 3 "Bu H F F OH H H X-40-8 p-I-Ph * H * "Bu H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-41. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' X-41-1 CH3 H H H Bz H F F OH H H X-41-2 CH3 H H CH3 Bz H F F OH H H X-41-3 CH3 H H CH(CH3) 2 Bz H F F OH H H X-41-4 CH3 H H CH2CH(CH3) 2 Bz H F F OH H H X-41-5 CH3 H H CH 2Ph Bz H F F OH H H X-41-6 CH3 H H CH 2-indol-3-yl Bz H F F OH H H X-41-7 CH3 H H CH2CH 2SCH 3 Bz H F F OH H H X-41-8 CH3 * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-42. N9 Rl R 2 R 3 a R3b R4 R' R' X Y R7 R' X-42-1 Et H H H Bz H F F OH H H X-42-2 Et H H CH 3 Bz H F F OH H H X-42-3 Et H H CH(CH3) 2 Bz H F F OH H H X-42-4 Et H H CH 2CH(CH3) 2 Bz H F F OH H H X-42-5 Et H H CH 2Ph Bz H F F OH H H X-42-6 Et H H CH 2-indol-3-yl Bz H F F OH H H X-42-7 Et H H CH 2CH 2SCH 3 Bz H F F OH H H X-42-8 Et * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-43. No R R2 R 3a R3 b R4 R 5 R6 X Y R7 R' X-43-1 'Pr H H H Bz H F F OH H H X-43-2 'Pr H H CH 3 Bz H F F OH H A X-43-3 'Pr H H CH(CH3) 2 Bz H F F OH H H X-43-4 'Pr H H CH 2CH(CH3)2 Bz H F F OH H H X-43-5 'Pr H H CH 2Ph Bz H F F OH H H X-43-6 'Pr H H CH 2-indol-3-yl Bz H F F OH H H X-43-7 'Pr H H CH 2CH2SCH 3 Bz H F F OH H H X-43-8 'Pr * H * Bz H F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-44. No R R2 R3 a Rb R4 R R6 X Y R7 R' X-44-1 'Bu H H H Bz H F F OH H H X-44-2 'Bu H H CH 3 Bz H F F OH H H X-44-3 'Bu H H CH(CH3) 2 Bz H F F OH H H X-44-4 'Bu H H CH 2CH(CH3)2 Bz H F F OH H H X-44-5 'Bu H H CH 2Ph Bz H F F OH H H X-44-6 'Bu H H CH 2-indol-3-yl Bz H F F OH H H X-44-7 'Bu H H CH 2CH2SCH 3 Bz H F F OH H H X-44-8 'Bu * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-45. No R1 R 2 R3 a R3b R4 R 5 R' X Y R7 R' X-45-1 Ph H H H Bz H F F OH H H X-45-2 Ph H H CH3 Bz H F F OH H H X-45-3 Ph H H CH(CH3)2 Bz H F F OH H H X-45-4 Ph H H CH2CH(CH3) 2 Bz H F F OH H H X-45-5 Ph H H CH 2Ph Bz H F F OH H H X-45-6 Ph H H CH 2-indol-3-yl Bz H F F OH H H X-45-7 Ph H H CH2CH 2SCH 3 Bz H F F OH H H X-45-8 Ph * H * Bz H F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table X-46. R3a 5 N R1 R2 R3 b R4 R R6 X Y R7 R' X-46-1 p-Me-Ph H H H Bz H F F OH H H X-46-2 p-Me-Ph H H CH3 Bz H F F OH H H X-46-3 p-Me-Ph H H CH(CH3)2 Bz H F F OH H H X-46-4 p-Me-Ph H H CH2CH(CH3) 2 Bz H F F OH H H X-46-5 p-Me-Ph H H CH 2Ph Bz H F F OH H H X-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F F OH H H X-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz H F F OH H H X-46-8 p-Me-Ph * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-47. N9 R1 R2 R3 a R 3b R4 R 5 R6 X Y R7 R' X-47-1 p-F-Ph H H H Bz H F F OH H H X-47-2 p-F-Ph H H CH3 Bz H F F OH H H X-47-3 p-F-Ph H H CH(CH3)2 Bz H F F OH H H X-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H F F OH H H X-47-5 p-F-Ph H H CH 2Ph Bz H F F OH H H X-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F F OH H H X-47-7 p-F-Ph H H CH2CH2 SCH3 Bz H F F OH H H X-47-8 p-F-Ph * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table X-48. 6 N9 R1 R 2 R 3a R3 b R4 R 5 R X Y R7 R' X-48-1 p-Cl-Ph H H H Bz H F F OH H H X-48-2 p-Cl-Ph H H CH 3 Bz H F F OH H H X-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F F OH H H

ItI2

N9 Rl R2 R 3a R3 b R4 R' R X Y R7 R' X-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H F F OH H H X-48-5 p-Cl-Ph H H CH 2Ph Bz H F F OH H H X-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F F OH H H X-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H F F OH H H X-48-8 p-Cl-Ph * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-49. N9 Rl R 2 R 3 a R 3b R4 R' R6 X Y R7 R' X-49-1 p-Br-Ph H H H Bz H F F OH H H X-49-2 p-Br-Ph H H CH 3 Bz H F F OH H H X-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F F OH H H X-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz H F F OH H H X-49-5 p-Br-Ph H H CH 2Ph Bz H F F OH H H X-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F F OH H H X-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz H F F OH H H X-49-8 p-Br-Ph * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table X-50. N9 Rl R 2 R 3 a R3 b R4 R 5 R6 X Y R7 R' X-50-1 p-I-Ph H H H Bz H F F OH H H X-50-2 p-I-Ph H H CH3 Bz H F F OH H H X-50-3 p-I-Ph H H CH(CH3)2 Bz H F F OH H H X-50-4 p-I-Ph H H CH2CH(CH3) 2 Bz H F F OH H H X-50-5 p-I-Ph H H CH 2Ph Bz H F F OH H H X-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F F OH H H X-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H F F OH H H X-50-8 p-I-Ph * H * Bz H F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 o _

R8 NH

Rt 2 0 R3 b R2 N O R3N-P -- 0 ON 0

CO2R4 OR 1 R5 R6

Y X XI

Table XI-1. No R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' XI-1-1 CH3 H H H CH 3 H H F OH H H XI-1-2 CH3 H H CH3 CH 3 H H F OH H H XI-1-3 CH3 H H CH(CH3) 2 CH 3 H H F OH H H XI-1-4 CH3 H H CH2CH(CH3) 2 CH 3 H H F OH H H XI-1-5 CH3 H H CH 2Ph CH 3 H H F OH H H XI-1-6 CH3 H H CH 2-indol-3-yl CH 3 H H F OH H H XI-1-7 CH3 H H CH2CH 2SCH 3 CH 3 H H F OH H H XI-1-8 CH3 * H * CH 3 H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-2. No R1 R 2 R3 a R3b R4 R5 R6 X Y R7 R' XI-2-1 Et H H H CH 3 H H F OH H H XI-2-2 Et H H CH 3 CH 3 H H F OH H H XI-2-3 Et H H CH(CH3) 2 CH 3 H H F OH H H XI-2-4 Et H H CH 2CH(CH3) 2 CH 3 H H F OH H H XI-2-5 Et H H CH 2Ph CH 3 H H F OH H H XI-2-6 Et H H CH 2-indol-3-yl CH 3 H H F OH H H XI-2-7 Et H H CH 2CH 2SCH 3 CH 3 H H F OH H H XI-2-8 Et * H * CH 3 H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

')Al-

Table XI-3. N9 R1 R2 R3 a R3b R4 R' R6 X Y R7 R' XI-3-1 'Pr H H H CH 3 H H F OH H H XI-3-2 'Pr H H CH 3 CH3 H H F OH H H XI-3-3 'Pr H H CH(CH3) 2 CH3 H H F OH H H XI-3-4 Pr H H CH 2CH(CH 3) 2 CH 3 H H F OH H H XI-3-5 Pr H H CH 2Ph CH 3 H H F OH H H XI-3-6 Pr H H CH 2-indol-3-yl CH3 H H F OH H H XI-3-7 Pr H H CH 2CH2SCH 3 CH3 H H F OH H H XI-3-8 Pr * H * CH 3 H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-4. N9 R1 R2 R 3a Rb R4 R R6 X Y R7 R' XI-4-1 'Bu H H H CH 3 H H F OH H H XI-4-2 'Bu H H CH 3 CH 3 H H F OH H H XI-4-3 'Bu H H CH(CH3) 2 CH 3 H H F OH H H XI-4-4 'Bu H H CH 2CH(CH 3)2 CH 3 H H F OH H H XI-4-5 'Bu H H CH 2Ph CH 3 H H F OH H H XI-4-6 'Bu H H CH 2-indol-3-yl CH 3 H H F OH H H XI-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H H F OH H H XI-4-8 'Bu * H * CH 3 H H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-5. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' XI-5-1 Ph H H H CH 3 H H F OH H H XI-5-2 Ph H H CH3 CH3 H H F OH H H XI-5-3 Ph H H CH(CH3)2 CH3 H H F OH H H XI-5-4 Ph H H CH2CH(CH3) 2 CH3 H H F OH H H XI-5-5 Ph H H CH 2Ph CH 3 H H F OH H H XI-5-6 Ph H H CH 2-indol-3-yl CH3 H H F OH H H XI-5-7 Ph H H CH2CH 2SCH 3 CH3 H H F OH H H XI-5-8 Ph * H * CH 3 H H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

_/)A1 _

Table XI-6. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' XI-6-1 p-Me-Ph H H H CH 3 H H F OH H H XI-6-2 p-Me-Ph H H CH3 CH3 H H F OH H H XI-6-3 p-Me-Ph H H CH(CH3)2 CH3 H H F OH H H XI-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 H H F OH H H XI-6-5 p-Me-Ph H H CH 2Ph CH 3 H H F OH H H XI-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H H F OH H H XI-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H H F OH H H XI-6-8 p-Me-Ph * H * CH 3 H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-7. R3a 6 N R1 R2 R3 b R4 R' R X Y R7 R' XI-7-1 p-F-Ph H H H CH 3 H H F OH H H XI-7-2 p-F-Ph H H CH3 CH3 H H F OH H H XI-7-3 p-F-Ph H H CH(CH3)2 CH3 H H F OH H H XI-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H H F OH H H XI-7-6 p-F-Ph H H CH 2Ph CH 3 H H F OH H H XI-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H H F OH H H XI-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H H F OH H H XI-7-20 p-F-Ph * H * CH 3 H H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-8. 5 6 N9 R1 R 2 R 3 a R 3b R4 R R X Y R7 R' XI-8-1 p-Cl-Ph H H H CH 3 H H F OH H H XI-8-2 p-Cl-Ph H H CH 3 CH 3 H H F OH H H XI-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H H F OH H H XI-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H H F OH H H XI-8-5 p-Cl-Ph H H CH 2Ph CH 3 H H F OH H H XI-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H H F OH H H XI-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H H F OH H H XI-8-8 p-Cl-Ph * H * CH 3 H H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

')A I

Table XI-9. N9 R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' XI-9-1 p-Br-Ph H H H CH 3 H H F OH H H XI-9-2 p-Br-Ph H H CH3 CH 3 H H F OH H H XI-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H H F OH H H XI-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH 3 H H F OH H H XI-9-6 p-Br-Ph H H CH2Ph CH 3 H H F OH H H XI-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H H F OH H H XI-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 H H F OH H H XI-9-20 p-Br-Ph * H * CH 3 H H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-10. N R1 R2 R3a R3 b R4 R' R6 X Y R7 R' XI-10-1 p-I-Ph H H H CH 3 H H F OH H H XI-10-2 p-I-Ph H H CH 3 CH3 H H F OH H H XI-10-3 p-I-Ph H H CH(CH3) 2 CH3 H H F OH H H XI-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H H F OH H H XI-10-5 p-I-Ph H H CH 2Ph CH 3 H H F OH H H XI-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H H F OH H H XI-10-7 p-I-Ph H H CH 2CH2SCH 3 CH3 H H F OH H H XI-10-8 p-I-Ph * H * CH 3 H H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-11. No9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' XI-11-1 CH 3 H H H Et H H F OH H H XI-11-2 CH 3 H H CH3 Et H H F OH H H XI-11-3 CH 3 H H CH(CH3) 2 Et H H F OH H H XI-11-4 CH 3 H H CH2CH(CH3) 2 Et H H F OH H H XI-11-5 CH 3 H H CH 2Ph Et H H F OH H H XI-11-6 CH 3 H H CH 2-indol-3-yl Et H H F OH H H XI-11-7 CH 3 H H CH2CH 2SCH 3 Et H H F OH H H XI-11-8 CH 3 * H * Et H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

')A2'

Table XI-12. N R1 RR 2 R 3a R 3b R4 R 5 R6 X Y R7 R' XI-12-1 Et H H H Et H H F OH H H XI-12-2 Et H H CH3 Et H H F OH H H XI-12-3 Et H H CH(CH3) 2 Et H H F OH H H XI-12-4 Et H H CH2CH(CH3) 2 Et H H F OH H H XI-12-5 Et H H CH2Ph Et H H F OH H H XI-12-6 Et H H CH2-indol-3-yl Et H H F OH H H XI-12-7 Et H H CH2CH 2SCH 3 Et H H F OH H H XI-12-8 Et * H * FtH H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-13. No9 R1 R2 R3a Rb R 4 R' R6 X Y R7 R' XI-13-1 'Pr H H H Et H H F OH H H XI-13-2 'Pr H H CH 3 Et H H F OH H H XI-13-3 'Pr H H CH(CH3) 2 Et H H F OH H H XI-13-4 'Pr H H CH 2CH(CH 3) 2 Et H H F OH H H XI-13-5 'Pr H H CH 2Ph Et H H F OH H H XI-13-6 'Pr H H CH 2-indol-3-yl Et H H F OH H H XI-13-7 'Pr H H CH 2CH2SCH 3 Et H H F OH H H XI-13-8 'Pr * H * Et H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-14. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R XI-14-1 'Bu H H H Et H H F OH H H XI-14-2 'Bu H H CH 3 Et H H F OH H H XI-14-3 'Bu H H CH(CH3) 2 Et H H F OH H H XI-14-4 'Bu H H CH 2CH(CH3)2 Et H H F OH H H XI-14-5 'Bu H H CH 2Ph Et H H F OH H H XI-14-6 'Bu H H CH 2-indol-3-yl Et H H F OH H H XI-14-7 'Bu H H CH 2CH2SCH 3 Et H H F OH H H XI-14-8 'Bu * H * Et H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

')A-

Table XI-15. No9 R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' XI-15-1 Ph H H H Et H H F OH H H XI-15-2 Ph H H CH3 Et H H F OH H H XI-15-3 Ph H H CH(CH3) 2 Et H H F OH H H XI-15-4 Ph H H CH2CH(CH3)2 Et H H F OH H H XI-15-5 Ph H H CH 2Ph Et H H F OH H H XI-15-6 Ph H H CH 2-indol-3-yl Et H H F OH H H XI-15-7 Ph H H CH2CH2SCH 3 Et H H F OH H H XI-15-8 Ph * H * EtH H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-16. N R1 R2 R 3a R3 b R4 R 5 R6 X Y R7 R' XI-16-1 p-Me-Ph H H H Et H H F OH H H XI-16-2 p-Me-Ph H H CH 3 Et H H F OH H H XI-16-3 p-Me-Ph H H CH(CH3) 2 Et H H F OH H H XI-16-4 p-Me-Ph H H CH 2CH(CH 3) 2 Et H H F OH H H XI-16-5 p-Me-Ph H H CH 2Ph Et H H F OH H H XI-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H H F OH H H XI-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H H F OH H H XI-16-8 p-Me-Ph * H * Et H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-17. N R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' XI-17-1 p-F-Ph H H H Et H H F OH H H XI-17-2 p-F-Ph H H CH3 Et H H F OH H H XI-17-3 p-F-Ph H H CH(CH3)2 Et H H F OH H H XI-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H H F OH H H XI-17-5 p-F-Ph H H CH 2Ph Et H H F OH H H XI-17-6 p-F-Ph H H CH 2-indol-3-yl Et H H F OH H H XI-17-7 p-F-Ph H H CH2CH 2SCH 3 Et H H F OH H H XI-17-8 p-F-Ph * H * Et H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-18. N9 R1 R2 R3 a R 3b R4 R R X Y R7 R' XI-18-1 p-Cl-Ph H H H Et H H F OH H H XI-18-2 p-Cl-Ph H H CH 3 Et H H F OH H H XI-18-3 p-Cl-Ph H H CH(CH3) 2 Et H H F OH H H XI-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H H F OH H H XI-18-5 p-Cl-Ph H H CH 2Ph Et H H F OH H H XI-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H H F OH H H XI-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H H F OH H H XI-18-8 p-Cl-Ph * H * Et H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XI-19. N9 R1 R2 R3a R3 b R4 R 5 R6 X Y R7 R' XI-19-1 p-Br-Ph H H H Et H H F OH H H XI-19-2 p-Br-Ph H H CH3 Et H H F OH H H XI-19-3 p-Br-Ph H H CH(CH3) 2 Et H H F OH H H XI-19-4 p-Br-Ph H H CH2CH(CH 3)2 Et H H F OH H H XI-19-5 p-Br-Ph H H CH 2Ph Et H H F OH H H XI-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H H F OH H H XI-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H H F OH H H XI-19-8 p-Br-Ph * H * Et H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XI-20. N R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XI-20-1 p-I-Ph H H H Et H H F OH H H XI-20-2 p-I-Ph H H CH 3 Et H H F OH H H XI-20-3 p-I-Ph H H CH(CH3) 2 Et H H F OH H H XI-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H H F OH H H XI-20-5 p-I-Ph H H CH 2Ph Et H H F OH H H XI-20-6 p-I-Ph H H CH 2-indol-3-yl Et H H F OH H H XI-20-7 p-I-Ph H H CH 2CH2SCH 3 Et H H F OH H H XI-20-8 p-I-Ph * H * Et H H F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XI-21. No9 R1 R2 R3 a R3b R4 R' R6 X Y R7 R' XI-21-1 CH 3 H H H 'Pr H H F OH H H XI-21-2 CH 3 H H CH3 'Pr H H F OH H H XI-21-3 CH 3 H H CH(CH3) 2 'Pr H H F OH H H XI-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H H F OH H H XI-21-5 CH 3 H H CH 2Ph 'Pr H H F OH H H XI-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H H F OH H H XI-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H H F OH H H XI-21-8 CH 3 * H * 'Pr H H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-22. N R1 RR 2 R 3a R3 b R4 R' R6 X Y R7 R' XI-22-1 Et H H H 'Pr H H F OH H H XI-22-2 Et H H CH3 'Pr H H F OH H H XI-22-3 Et H H CH(CH3) 2 'Pr H H F OH H H XI-22-4 Et H H CH2CH(CH3) 2 'Pr H H F OH H H XI-22-5 Et H H CH2Ph 'Pr H H F OH H H XI-22-6 Et H H CH2-indol-3-yl 'Pr H H F OH H H XI-22-7 Et H H CH2CH 2SCH 3 'Pr H H F OH H H XI-22-8 Et * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-23. N9 R1 R2 R3 a R3 R4 R 5 R6 X Y R7 R' XI-23-1 'Pr H H H 'Pr H H F OH H H XI-23-2 'Pr H H CH 3 'Pr H H F OH H H XI-23-3 'Pr H H CH(CH3) 2 'Pr H H F OH H H XI-23-4 'Pr H H CH 2CH(CH3)2 'Pr H H F OH H H XI-23-5 Pr H H CH 2Ph 'Pr H H F OH H H XI-23-6 Pr H H CH 2-indol-3-yl 'Pr H H F OH H H XI-23-7 Pr H H CH 2CH2SCH 3 'Pr H H F OH H H XI-23-8 Pr * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

')A'7-

Table XI-24. N9 R1 R2 R3 a R3 R4 R R' X Y R7 R' XI-24-1 'Bu H H H 'Pr H H F OH H H XI-24-2 'Bu H H CH 3 'Pr H H F OH H H XI-24-3 'Bu H H CH(CH3) 2 'Pr H H F OH H H XI-24-4 'Bu H H CH 2CH(CH3)2 'Pr H H F OH H H XI-24-5 'Bu H H CH 2Ph 'Pr H H F OH H H XI-24-6 'Bu H H CH 2-indol-3-yl 'Pr H H F OH H H XI-24-7 'Bu H H CH 2CH2SCH 3 'Pr H H F OH H H XI-24-8 'Bu * H * 'Pr H H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XI-25. No9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' XI-25-1 Ph H H H 'Pr H H F OH H H XI-25-2 Ph H H CH3 'Pr H H F OH H H XI-25-3 Ph H H CH(CH3) 2 'Pr H H F OH H H XI-25-4 Ph H H CH2CH(CH 3) 2 'Pr H H F OH H H XI-25-5 Ph H H CH 2Ph 'Pr H H F OH H H XI-25-6 Ph H H CH 2-indol-3-yl 'Pr H H F OH H H XI-25-7 Ph H H CH2CH2SCH 3 'Pr H H F OH H H XI-25-8 Ph * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-26. N R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' XI-26-1 p-Me-Ph H H H Pr H H F OH H H XI-26-2 p-Me-Ph H H CH 3 'Pr H H F OH H H XI-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H H F OH H H XI-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr H H F OH H H XI-26-5 p-Me-Ph H H CH 2Ph 'Pr H H F OH H H XI-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H XI-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H H F OH H H XI-26-8 p-Me-Ph * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

')AQ-

Table XI-27. N9 R1 R 2 R 3 a R 3b R4 R' R' X Y R7 R' XI-27-1 p-F-Ph H H H 'Pr H H F OH H H XI-27-2 p-F-Ph H H CH3 'Pr H H F OH H H XI-27-3 p-F-Ph H H CH(CH3)2 'Pr H H F OH H H XI-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H H F OH H H XI-27-5 p-F-Ph H H CH 2Ph 'Pr H H F OH H H XI-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H XI-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H H F OH H H XI-27-8 p-F-Ph * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-28. N9 R1 R2 R 3 a R3 b R4 R R 6 X Y R7 R' XI-28-1 p-Cl-Ph H H H 'Pr H H F OH H H XI-28-2 p-Cl-Ph H H CH 3 'Pr H H F OH H H XI-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H H F OH H H XI-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr H H F OH H H XI-28-5 p-Cl-Ph H H CH 2Ph 'Pr H H F OH H H XI-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H XI-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H H F OH H H XI-28-8 p-Cl-Ph * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XI-29. 6 N R1 R2 R 3a R 3b R4 R5 R X Y R7 R' XI-29-1 p-Br-Ph H H H 'Pr H H F OH H H XI-29-2 p-Br-Ph H H CH3 'Pr H H F OH H H XI-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H H F OH H H XI-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H H F OH H H XI-29-5 p-Br-Ph H H CH 2Ph 'Pr H H F OH H H XI-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H XI-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H H F OH H H XI-29-8 p-Br-Ph * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

To_ _

Table XI-30. N9 R1 R 2 R 3a R3b R4 R' R' X Y R7 R' XI-30-1 p-I-Ph H H H 'Pr H H F OH H H XI-30-2 p-I-Ph H H CH 3 'Pr H H F OH H H XI-30-3 p-I-Ph H H CH(CH3) 2 'Pr H H F OH H H XI-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr H H F OH H H XI-30-5 p-I-Ph H H CH 2Ph 'Pr H H F OH H H XI-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H H F OH H H XI-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H H F OH H H XI-30-8 p-I-Ph * H * 'Pr H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-31. No R1 R2 R3a R3b R4 R 5 R6 X Y R7 R' XI-31-1 CH 3 H H H "Bu H H F OH H H XI-31-2 CH 3 H H CH3 "Bu H H F OH H H XI-31-3 CH 3 H H CH(CH3) 2 "Bu H H F OH H H XI-31-4 CH 3 H H CH2CH(CH3) 2 "Bu H H F OH H H XI-31-5 CH 3 H H CH 2Ph "Bu H H F OH H H XI-31-6 CH 3 H H CH 2-indol-3-yl "Bu H H F OH H H XI-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H H F OH H H XI-31-8 CH 3 * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-32. No R1 R2 R 3a R 3b R4 R 5 R6 X Y R7 R'

XI-32-1 Et H H H "Bu H H F OH H H XI-32-2 Et H H CH3 "Bu H H F OH H H XI-32-3 Et H H CH(CH3) 2 "Bu H H F OH H H XI-32-4 Et H H CH2CH(CH3) 2 "Bu H H F OH H H XI-32-5 Et H H CH2Ph "Bu H H F OH H H XI-32-6 Et H H CH2-indol-3-yl "Bu H H F OH H H XI-32-7 Et H H CH2CH 2SCH 3 "Bu H H F OH H H XI-32-8 Et * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-33. No R1 R2 R3 a R3 R4 R R X Y R7 R' XI-33-1 'Pr H H H "Bu H H F OH H H XI-33-2 'Pr H H CH 3 "Bu H H F OH H H XI-33-3 'Pr H H CH(CH3) 2 "Bu H H F OH H H XI-33-4 'Pr H H CH 2CH(CH3)2 "Bu H H F OH H H XI-33-5 'Pr H H CH 2Ph "Bu H H F OH H H XI-33-6 'Pr H H CH 2-indol-3-yl "Bu H H F OH H H XI-33-7 'Pr H H CH 2CH2 SCH 3 "Bu H H F OH H H XI-33-8 'Pr * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-34. No R1 R2 R3a Rb R4 R R6 X Y R7 R' XI-34-1 'Bu H H H "Bu H H F OH H H XI-34-2 'Bu H H CH 3 "Bu H H F OH H H XI-34-3 'Bu H H CH(CH 3) 2 "Bu H H F OH H H XI-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H H F OH H H XI-34-5 'Bu H H CH 2Ph "Bu H H F OH H H XI-34-6 'Bu H H CH 2-indol-3-yl "Bu H H F OH H H XI-34-7 'Bu H H CH 2CH2SCH 3 "Bu H H F OH H H XI-34-8 'Bu * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-35. N R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R'

XI-35-1 Ph H H H "Bu H H F OH H H XI-35-2 Ph H H CH3 "Bu H H F OH H H XI-35-3 Ph H H CH(CH3) 2 "Bu H H F OH H H XI-35-4 Ph H H CH2CH(CH3)2 "Bu H H F OH H H XI-35-5 Ph H H CH 2 Ph "Bu H H F OH H H XI-35-6 Ph H H CH 2-indol-3-yl "Bu H H F OH H H XI-35-7 Ph H H CH2 CH2 SCH 3 "Bu H H F OH H H XI-35-8 Ph * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'M1 _

Table XI-36. N9 R1 R 2 R 3a R3b R4 R' R6 X Y R7 R' XI-36-1 p-Me-Ph H H H "Bu H H F OH H H XI-36-2 p-Me-Ph H H CH 3 "Bu H H F OH H H XI-36-3 p-Me-Ph H H CH(CH3) 2 "Bu H H F OH H H XI-36-4 p-Me-Ph H H CH 2CH(CH3)2 "Bu H H F OH H H XI-36-5 p-Me-Ph H H CH 2Ph "Bu H H F OH H H XI-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H H F OH H H XI-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH H H XI-36-8 p-Me-Ph * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-37. N R1 R2 R3a R3b R4 R' R6 X Y R7 R' XI-37-1 p-F-Ph H H H "Bu H H F OH H H XI-37-2 p-F-Ph H H CH3 "Bu H H F OH H H XI-37-3 p-F-Ph H H CH(CH3)2 "Bu H H F OH H H XI-37-4 p-F-Ph H H CH2CH(CH3) 2 "Bu H H F OH H H XI-37-5 p-F-Ph H H CH 2 Ph "Bu H H F OH H H XI-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H H F OH H H XI-37-7 p-F-Ph H H CH2 CH 2 SCH 3 "Bu H H F OH H H XI-37-8 p-F-Ph * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-38. N9 R1 R2 R3 a R3 b R4 R5 R 6 X Y R7 R' XI-38-1 p-Cl-Ph H H H "Bu H H F OH H H XI-38-2 p-Cl-Ph H H CH 3 "Bu H H F OH H H XI-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H H F OH H H XI-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H H F OH H H XI-38-5 p-Cl-Ph H H CH 2Ph "Bu H H F OH H H XI-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H H F OH H H XI-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H H F OH H H XI-38-8 p-Cl-Ph * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XI-39. N9 R1 R2 R 3a R 3 b R4 R' R6 X Y R7 R' XI-39-1 p-Br-Ph H H H "Bu H H F OH H H XI-39-2 p-Br-Ph H H CH3 "Bu H H F OH H H XI-39-3 p-Br-Ph H H CH(CH 3)2 "Bu H H F OH H H XI-39-4 p-Br-Ph H H CH2CH(CH3) 2 "Bu H H F OH H H XI-39-5 p-Br-Ph H H CH 2Ph "Bu H H F OH H H XI-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H H F OH H H XI-39-7 p-Br-Ph H H CH2 CH 2 SCH 3 "Bu H H F OH H H XI-39-8 p-Br-Ph * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-40. N R1 R2 R3a R3b R4 R' R6 X Y R7 R' XI-40-1 p-I-Ph H H H "Bu H H F OH H H XI-40-2 p-I-Ph H H CH 3 "Bu H H F OH H H XI-40-3 p-I-Ph H H CH(CH3) 2 "Bu H H F OH H H XI-40-4 p-I-Ph H H CH 2CH(CH 3) 2 "Bu H H F OH H H XI-40-5 p-I-Ph H H CH 2Ph "Bu H H F OH H H XI-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H H F OH H H XI-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H H F OH H H XI-40-8 p-I-Ph * H * "Bu H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-41. No R1 R2 R3a R3b R4 R5 R6 X Y R7 R' XI-41-1 CH 3 H H H Bz H H F OH H H XI-41-2 CH 3 H H CH3 Bz H H F OH H H XI-41-3 CH 3 H H CH(CH3) 2 Bz H H F OH H H XI-41-4 CH 3 H H CH2CH(CH3) 2 Bz H H F OH H H XI-41-5 CH 3 H H CH 2Ph Bz H H F OH H H XI-41-6 CH 3 H H CH 2-indol-3-yl Bz H H F OH H H XI-41-7 CH 3 H H CH2CH 2SCH 3 Bz H H F OH H H XI-41-8 CH 3 * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-42. N9 Rl R2 R 3 a R 3b R4 R' R' X Y R7 R' XI-42-1 Et H H H Bz H H F OH H H XI-42-2 Et H H CH3 Bz H H F OH H H XI-42-3 Et H H CH(CH3) 2 Bz H H F OH H H XI-42-4 Et H H CH2CH(CH3) 2 Bz H H F OH H H XI-42-5 Et H H CH2Ph Bz H H F OH H H XI-42-6 Et H H CH2-indol-3-yl Bz H H F OH H H XI-42-7 Et H H CH2CH 2SCH 3 Bz H H F OH H H XI-42-8 Et * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-43. N9 R R2 R3 a Rb R4 R R6 X Y R7 R' XI-43-1 'Pr H H H Bz H H F OH H H XI-43-2 'Pr H H CH 3 Bz H H F OH H A XI-43-3 'Pr H H CH(CH3) 2 Bz H H F OH H H XI-43-4 'Pr H H CH 2CH(CH 3) 2 Bz H H F OH H H XI-43-5 'Pr H H CH 2Ph Bz H H F OH H H XI-43-6 'Pr H H CH 2-indol-3-yl Bz H H F OH H H XI-43-7 'Pr H H CH 2CH2SCH 3 Bz H H F OH H H XI-43-8 'Pr * H * Bz H H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-44. N9 R R2 R3 a Rb R4 R R6 X Y R7 R' XI-44-1 'Bu H H H Bz H H F OH H H XI-44-2 'Bu H H CH 3 Bz H H F OH H H XI-44-3 'Bu H H CH(CH 3) 2 Bz H H F OH H H XI-44-4 'Bu H H CH 2CH(CH 3) 2 Bz H H F OH H H XI-44-5 'Bu H H CH 2Ph Bz H H F OH H H XI-44-6 'Bu H H CH 2-indol-3-yl Bz H H F OH H H XI-44-7 'Bu H H CH 2CH2SCH 3 Bz H H F OH H H XI-44-8 'Bu * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

IrA-

Table XI-45. N9 R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' XI-45-1 Ph H H H Bz H H F OH H H XI-45-2 Ph H H CH3 Bz H H F OH H H XI-45-3 Ph H H CH(CH3) 2 Bz H H F OH H H XI-45-4 Ph H H CH2CH(CH3)2 Bz H H F OH H H XI-45-5 Ph H H CH 2Ph Bz H H F OH H H XI-45-6 Ph H H CH 2-indol-3-yl Bz H H F OH H H XI-45-7 Ph H H CH2CH2SCH 3 Bz H H F OH H H XI-45-8 Ph * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-46. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' XI-46-1 p-Me-Ph H H H Bz H H F OH H H XI-46-2 p-Me-Ph H H CH 3 Bz H H F OH H H XI-46-3 p-Me-Ph H H CH(CH3) 2 Bz H H F OH H H XI-46-4 p-Me-Ph H H CH 2CH(CH3)2 Bz H H F OH H H XI-46-5 p-Me-Ph H H CH 2Ph Bz H H F OH H H XI-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H H F OH H H XI-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H H F OH H H XI-46-8 p-Me-Ph * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XI-47. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' XI-47-1 p-F-Ph H H H Bz H H F OH H H XI-47-2 p-F-Ph H H CH3 Bz H H F OH H H XI-47-3 p-F-Ph H H CH(CH3)2 Bz H H F OH H H XI-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H H F OH H H XI-47-5 p-F-Ph H H CH 2Ph Bz H H F OH H H XI-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H H F OH H H XI-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H H F OH H H XI-47-8 p-F-Ph * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1); r-r

Table XI-48. N9 R1 R2 R 3 a R 3b R4 R R X Y R7 R' XI-48-1 p-Cl-Ph H H H Bz H H F OH H H XI-48-2 p-Cl-Ph H H CH 3 Bz H H F OH H H XI-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H H F OH H H XI-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H H F OH H H XI-48-5 p-Cl-Ph H H CH 2Ph Bz H H F OH H H XI-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H H F OH H H XI-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H H F OH H H XI-48-8 p-Cl-Ph * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XI-49. 2 R3a3b 6 NI R R R R4 R' R XY R7 R' XI-49-1 p-Br-Ph H H H Bz H H F OH H H XI-49-2 p-Br-Ph H H CH3 Bz H H F OH H H XI-49-3 p-Br-Ph H H CH(CH3) 2 Bz H H F OH H H XI-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H H F OH H H XI-49-5 p-Br-Ph H H CH 2Ph Bz H H F OH H H XI-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H H F OH H H XI-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H H F OH H H XI-49-8 p-Br-Ph * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XI-50. N R1 R2 R 3a R3 b R4 R5 R 6 X Y R7 R' XI-50-1 p-I-Ph H H H Bz H H F OH H H XI-50-2 p-I-Ph H H CH 3 Bz H H F OH H H XI-50-3 p-I-Ph H H CH(CH3) 2 Bz H H F OH H H XI-50-4 p-I-Ph H H CH 2CH(CH3)2 Bz H H F OH H H XI-50-5 p-I-Ph H H CH 2Ph Bz H H F OH H H XI-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H H F OH H H XI-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H H F OH H H XI-50-8 p-I-Ph * H * Bz H H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R8 NH

Rt 2 0 R3 b R2 N O R3aN- -P 0 0

CO2R4 OR 1 R5 R6

Y X XII

Table XII-1. No R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' XII-1-1 CH 3 H H H CH 3 N3 F F OH H H XII-1-2 CH 3 H H CH3 CH 3 N3 F F OH H H XII-1-3 CH 3 H H CH(CH 3)2 CH 3 N3 F F OH H H XII-1-4 CH 3 H H CH2CH(CH 3) 2 CH 3 N3 F F OH H H XII-1-5 CH 3 H H CH 2Ph CH 3 N3 F F OH H H XII-1-6 CH 3 H H CH 2-indol-3-yl CH 3 N3 F F OH H H XII-1-7 CH 3 H H CH2CH 2SCH 3 CH 3 N3 F F OH H H XII-1-8 CH 3 * H * CH 3 N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-2. N R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XII-2-1 Et H H H CH 3 N3 F F OH H H XII-2-2 Et H H CH3 CH 3 N3 F F OH H H XII-2-3 Et H H CH(CH 3)2 CH 3 N3 F F OH H H XII-2-4 Et H H CH2CH(CH 3)2 CH 3 N3 F F OH H H XII-2-5 Et H H CH 2Ph CH 3 N3 F F OH H H XII-2-6 Et H H CH 2-indol-3-yl CH 3 N3 F F OH H H XII-2-7 Et H H CH2CH 2SCH 3 CH 3 N3 F F OH H H XII-2-8 Et * H * CH 3 N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-3. No R1 R2 R 3a R3b R4 R R6 X Y R7 R' XII-3-1 'Pr H H H CH3 N 3 F F OH H H XII-3-2 'Pr H H CH 3 CH3 N 3 F F OH H H XII-3-3 'Pr H H CH(CH 3)2 CH3 N 3 F F OH H H XII-3-4 Pr H H CH 2CH(CH 3) 2 CH3 N 3 F F OH H H XII-3-5 Pr H H CH 2Ph CH3 N 3 F F OH H H XII-3-6 Pr H H CH 2-indol-3-yl CH3 N 3 F F OH H H XII-3-7 Pr H H CH 2CH2SCH 3 CH3 N 3 F F OH H H XII-3-8 Pr * H * CH 3 N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-4. No R1 R2 R3 a R3b R4 RR X Y R7 R XII-4-1 'Bu H H H CH3 N 3 F F OH H H XII-4-2 'Bu H H CH 3 CH3 N 3 F F OH H H XII-4-3 'Bu H H CH(CH 3) 2 CH 3 N 3 F F OH H H XII-4-4 'Bu H H CH 2CH(CH 3)2 CH 3 N 3 F F OH H H XII-4-5 'Bu H H CH 2Ph CH3 N 3 F F OH H H XII-4-6 'Bu H H CH 2-indol-3-yl CH 3 N 3 F F OH H H XII-4-7 'Bu H H CH 2CH 2SCH 3 CH 3 N 3 F F OH H H XII-4-8 'Bu * H * CH 3 N3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-5. N R1 R2 R3 a R3b 4 R5 R6 X Y R7 R XII-5-1 Ph H H H CH 3 N 3 F F OH H H XII-5-2 Ph H H CH3 CH 3 N 3 F F OH H H XII-5-3 Ph H H CH(CH 3)2 CH 3 N 3 F F OH H H XII-5-4 Ph H H CH2CH(CH 3) 2 CH 3 N 3 F F OH H H XII-5-5 Ph H H CH 2Ph CH 3 N 3 F F OH H H XII-5-6 Ph H H CH 2-indol-3-yl CH 3 N 3 F F OH H H XII-5-7 Ph H H CH2CH2SCH 3 CH 3 N 3 F F OH H H XII-5-8 Ph * H * CH 3 N3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Ir;Q-

Table XII-6. R1 R2 R3 a R3 R4 R' R6 X Y R7 R' N9 XII-6-1 p-Me-Ph H H H CH 3 N 3 F F OH H H XII-6-2 p-Me-Ph H H CH 3 CH 3 N 3 F F OH H H XII-6-3 p-Me-Ph H H CH(CH 3)2 CH 3 N 3 F F OH H H XII-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH 3 N 3 F F OH H H XII-6-5 p-Me-Ph H H CH 2Ph CH 3 N 3 F F OH H H XII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 N 3 F F OH H H XII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH 3 N 3 F F OH H H XII-6-8 p-Me-Ph * H * CH 3 N 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-7. N R IR2 R3a R3 b R4 R' R6 X Y R7 R' XII-7-1 p-F-Ph H H H CH3 N 3 F F OH H H XII-7-2 p-F-Ph H H CH 3 CH3 N 3 F F OH H H XII-7-3 p-F-Ph H H CH(CH 3)2 CH3 N 3 F F OH H H XII-7-4 p-F-Ph H H CH 2CH(CH 3)2 CH3 N 3 F F OH H H XII-7-6 p-F-Ph H H CH 2Ph CH3 N 3 F F OH H H XII-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 N 3 F F OH H H XII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 N 3 F F OH H H XII-7-20 p-F-Ph * H * CH3 N 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-8. N R R2 R 3 a R3b R4 R5 R6 X Y R7 R XII-8-1 p-Cl-Ph H H H CH3 N 3 F F OH H H XII-8-2 p-Cl-Ph H H CH3 CH 3 N 3 F F OH H H XII-8-3 p-Cl-Ph H H CH(CH3) 2 CH3 N 3 F F OH H H XII-8-4 p-Cl-Ph H H CH2CH(CH 3)2 CH3 N 3 F F OH H H XII-8-5 p-Cl-Ph H H CH2Ph CH3 N 3 F F OH H H XII-8-6 p-Cl-Ph H H CH2-indol-3-yl CH 3 N 3 F F OH H H XII-8-7 p-Cl-Ph H H CH2CH 2SCH 3 CH3 N 3 F F OH H H XII-8-8 p-Cl-Ph * H * CH3 N 3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_; o_

Table XII-9. R RR 3 R 3b R4 R' R' X Y R7 R' No a

XII-9-1 p-Br-Ph H H H CH 3 N 3 F F OH H H XII-9-2 p-Br-Ph H H CH3 CH3 N 3 F F OH H H XII-9-3 p-Br-Ph H H CH(CH 3) 2 CH3 N 3 F F OH H H XII-9-4 p-Br-Ph H H CH2CH(CH 3) 2 CH3 N 3 F F OH H H XII-9-6 p-Br-Ph H H CH 2Ph CH 3 N 3 F F OH H H XII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 N 3 F F OH H H XII-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 N 3 F F OH H H XII-9-20 p-Br-Ph * H * CH 3 N 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-10. N R IR2 R3a R3 b R4 R' R6 X Y R7 R' XII-10-1 p-I-Ph H H H CH 3 N 3 F F OH H H XII-10-2 p-I-Ph H H CH3 CH 3 N 3 F F OH H H XII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 N 3 F F OH H H XII-10-4 p-I-Ph H H CH2CH(CH 3)2 CH 3 N 3 F F OH H H XII-10-5 p-I-Ph H H CH2Ph CH 3 N 3 F F OH H H XII-10-6 p-I-Ph H H CH2-indol-3-yl CH 3 N 3 F F OH H H XII-10-7 p-I-Ph H H CH2CH2SCH 3 CH 3 N 3 F F OH H H XII-10-8 p-I-Ph * H * CH 3 N 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-11. No RI 1 R2 R3 a R 3b R4 R5 R6 X Y R7 R XII-11-1 CH3 H H H Et N3 F F OH H H XII-11-2 CH3 H H CH3 Et N3 F F OH H H XII-11-3 CH3 H H CH(CH 3) 2 Et N3 F F OH H H XII-11-4 CH3 H H CH2CH(CH3) 2 Et N3 F F OH H H XII-11-5 CH3 H H CH 2Ph Et N3 F F OH H H XII-11-6 CH3 H H CH 2-indol-3-yl Et N3 F F OH H H XII-11-7 CH3 H H CH2CH2 SCH3 Et N3 F F OH H H XII-11-8 CH3 * H * Et N3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-12. R1 R2 R3 a R 3b R4 R' R' X Y R7 R' No XII-12-1 Et H H H Et N3 F F OH H H XII-12-2 Et H H CH3 Et N3 F F OH H H XII-12-3 Et H H CH(CH 3) 2 Et N3 F F OH H H XII-12-4 Et H H CH2CH(CH 3) 2 Et N3 F F OH H H XII-12-5 Et H H CH 2Ph Et N3 F F OH H H XII-12-6 Et H H CH 2-indol-3-yl Et N3 F F OH H H XII-12-7 Et H H CH2CH 2SCH3 Et N3 F F OH H H XII-12-8 Et * H * Et N3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-13. R N9 R R2 R3 a R3 b R4 R 6 X Y R7 R' XII-13-1 'Pr H H H Et N3 F F OH H H XII-13-2 'Pr H H CH 3 Et N3 F F OH H H XII-13-3 'Pr H H CH(CH 3) 2 Et N3 F F OH H H XII-13-4 'Pr H H CH 2CH(CH 3) 2 Et N3 F F OH H H XII-13-5 'Pr H H CH 2Ph Et N3 F F OH H H XII-13-6 'Pr H H CH 2-indol-3-yl Et N3 F F OH H H XII-13-7 'Pr H H CH 2CH2SCH 3 Et N3 F F OH H H XII-13-8 'Pr * H * Et N3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-14. No R 1 R2 R R3b R4 R5 R6 X Y R7 R' 3a

XII- 'Bu H H H Et N F F OH H H 14-1 3

XII- 'Bu H H CH 3 Et N F F OH H H 14-2 3

XII- 'Bu H H CH(CH 3) 2 Et N F F OH H H 14-3 3

XII- 'Bu H H CH 2CH(CH 3) 2 Et N F F OH H H 14-4 3

XII- 'Bu H H CH 2Ph Et N F F OH H H 14-5 3

XII- 'Bu H H CH 2-indol-3-yl Et N F F OH H H 14-6 3

XII- 'Bu H H CH 2CH2SCH 3 Et N F F OH H H

Il1 _

No R R2 R R3b R4 R5 R6 X Y R7 R' 3a

14-7 3

XII- 'Bu * H * Et N F F OH H H 14-8 3

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-15. No R R2 R3a R3b R 4 R6 X Y R7 R' XII-15-1 Ph H H H Et N3 F F OH H H XII-15-2 Ph H H CH3 Et N3 F F OH H H XII-15-3 Ph H H CH(CH3) 2 Et N3 F F OH H H XII-15-4 Ph H H CH2CH(CH 3) 2 Et N3 F F OH H H XII-15-5 Ph H H CH2Ph Et N3 F F OH H H XII-15-6 Ph H H CH2-indol-3-yl Et N3 F F OH H H XII-15-7 Ph H H CH2CH2SCH 3 Et N3 F F OH H H XII-15-8 Ph * H * Et N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-16. No RI R2 R3 a R3 b R4 R 5 R' X Y R7 R XII-16-1 p-Me-Ph H H H Et N3 F F OH H H XII-16-2 p-Me-Ph H H CH3 Et N3 F F OH H H XII-16-3 p-Me-Ph H H CH(CH3) 2 Et N3 F F OH H H XII-16-4 p-Me-Ph H H CH2CH(CH 3) 2 Et N3 F F OH H H XII-16-5 p-Me-Ph H H CH2Ph Et N3 F F OH H H XII-16-6 p-Me-Ph H H CH2-indol-3-yl Et N3 F F OH H H XII-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et N3 F F OH H H XII-16-8 p-Me-Ph * H * Et N3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-17. 6 No RI R2 R3 a R3 b R 4 R5 R X Y R7 R' XII-17-1 p-F-Ph H H H Et N3 F F OH H H XII-17-2 p-F-Ph H H CH 3 Et N3 F F OH H H XII-17-3 p-F-Ph H H CH(CH 3)2 Et N3 F F OH H H XII-17-4 p-F-Ph H H CH 2CH(CH 3) 2 Et N3 F F OH H H XII-17-5 p-F-Ph H H CH 2Ph Et N3 F F OH H H XII-17-6 p-F-Ph H H CH 2-indol-3-yl Et N3 F F OH H H XII-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et N3 F F OH H H

R RR SaREb R4 R' R 6 X Y R7 R' No XII-17-8 p-F-Ph * H * Et N3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-18. R2 R R3 b R4 R R' X Y R7 R' No R 3 a

XII-18-1 p-Cl-Ph H H H Et N3 F F OH H H XII-18-2 p-Cl-Ph H H CH3 Et N3 F F OH H H XII-18-3 p-Cl-Ph H H CH(CH 3) 2 Et N3 F F OH H H XII-18-4 p-Cl-Ph H H CH2CH(CH 3) 2 Et N3 F F OH H H XII-18-5 p-Cl-Ph H H CH 2Ph Et N3 F F OH H H XII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et N3 F F OH H H XII-18-7 p-Cl-Ph H H CH2CH 2SCH 3 Et N3 F F OH H H XII-18-8 p-Cl-Ph * H * Et N3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-19. R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' N9 XII-19-1 p-Br-Ph H H H Et N3 F F OH H H XII-19-2 p-Br-Ph H H CH3 Et N3 F F OH H H XII-19-3 p-Br-Ph H H CH(CH 3) 2 Et N3 F F OH H H XII-19-4 p-Br-Ph H H CH2CH(CH 3) 2 Et N3 F F OH H H XII-19-5 p-Br-Ph H H CH 2Ph Et N3 F F OH H H XII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et N3 F F OH H H XII-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et N3 F F OH H H XII-19-8 p-Br-Ph * H * Et N3 F F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XII-20. No R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 XII-20-1 p-I-Ph H H H Et N3 F F OH H XII-20-2 p-I-Ph H H CH3 Et N3 F F OH H XII-20-3 p-I-Ph H H CH(CH3) 2 Et N3 F F OH H XII-20-4 p-I-Ph H H CH2CH(CH 3)2 Et N3 F F OH H XII-20-5 p-I-Ph H H CH2Ph Et N3 F F OH H XII-20-6 p-I-Ph H H CH2-indol-3-yl Et N3 F F OH H XII-20-7 p-I-Ph H H CH2CH 2SCH 3 Et N3 F F OH H XII-20-8 p-I-Ph * H * Et N3 F F OH H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-21.

R' No R R2 R3 a R3 b R4 R6 X Y R7 R' XII-21-1 CH3 H H H 'Pr N3 F F OH H H XII-21-2 CH3 H H CH3 'Pr N3 F F OH H H XII-21-3 CH3 H H CH(CH 3) 2 'Pr N3 F F OH H H XII-21-4 CH3 H H CH2CH(CH3) 2 'Pr N3 F F OH H H XII-21-5 CH3 H H CH 2Ph 'Pr N3 F F OH H H XII-21-6 CH3 H H CH 2-indol-3-yl 'Pr N3 F F OH H H XII-21-7 CH3 H H CH2 CH2 SCH3 'Pr N3 F F OH H H XII-21-8 CH3 * H * 'Pr N3 F F OH H H

*R2 and R3b joined together by (CH 2 ) 3 to form five-membered ring.

Table XII-22. No R R2 R3 a R 3b R4 R' R6 X Y R7 R' XII-22-1 Et H H H 'Pr N3 F F OH H H XII-22-2 Et H H CH3 'Pr N 3 F F OH H H XII-22-3 Et H H CH(CH 3) 2 'Pr N3 F F OH H H XII-22-4 Et H H CH2CH(CH 3) 2 'Pr N3 F F OH H H XII-22-5 Et H H CH 2Ph 'Pr N3 F F OH H H XII-22-6 Et H H CH 2-indol-3-yl 'Pr N3 F F OH H H XII-22-7 Et H H CH2CH 2SCH3 'Pr N3 F F OH H H XII-22-8 Et * H * 'Pr N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-23. R 6 No R R2 R3 a R3 b R4 R X Y R7 R' XII-23-1 'Pr H H H 'Pr N3 F F OH H H XII-23-2 'Pr H H CH 3 'Pr N3 F F OH H H XII-23-3 'Pr H H CH(CH 3) 2 'Pr N3 F F OH H H XII-23-4 'Pr H H CH 2CH(CH3) 2 'Pr N3 F F OH H H XII-23-5 'Pr H H CH 2Ph 'Pr N3 F F OH H H XII-23-6 'Pr H H CH 2-indol-3-yl 'Pr N3 F F OH H H XII-23-7 'Pr H H CH 2CH2SCH 3 'Pr N3 F F OH H H XII-23-8 'Pr * H * 'Pr N3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-24. No R R2 R3 a R3b R4 R5 R6 X Y R7 R' XII-24-1 'Bu H H H 'Pr N3 F F OH H H XII-24-2 'Bu H H CH 3 'Pr N 3 F F OH H H XII-24-3 'Bu H H CH(CH 3)2 'Pr N3 F F OH H H

R R2 R3 a R3 b R4 R R' X Y R7 R' No

XII-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr N3 F F OH H H XII-24-5 'Bu H H CH 2Ph 'Pr N3 F F OH H H XII-24-6 'Bu H H CH 2-indol-3-yl 'Pr N3 F F OH H H XII-24-7 'Bu H H CH 2CH 2SCH 3 'Pr N3 F F OH H H XII-24-8 'Bu * H * 'Pr N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-25. No R R2 R 3a R 3b R4 R5 R 6 X Y R7 R' XII-25-1 Ph H H H 'Pr N3 F F OH H H XII-25-2 Ph H H CH3 'Pr N3 F F OH H H XII-25-3 Ph H H CH(CH3) 2 'Pr N3 F F OH H H XII-25-4 Ph H H CH2CH(CH 3) 2 'Pr N3 F F OH H H XII-25-5 Ph H H CH2Ph 'Pr N3 F F OH H H XII-25-6 Ph H H CH2-indol-3-yl 'Pr N3 F F OH H H XII-25-7 Ph H H CH2CH2SCH 3 'Pr N3 F F OH H H XII-25-8 Ph * H * 'Pr N3 F F OH H H

*R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

Table XII-26. R R2 R3 a RIt 4 R5 R6 X Y R7 R XII-26-1 p-Me-Ph H H H 'Pr N3 F F OH H H XII-26-2 p-Me-Ph H H CH3 'Pr N3 F F OH H H XII-26-3 p-Me-Ph H H CH(CH3) 2 'Pr N3 F F OH H H XII-26-4 p-Me-Ph H H CH2CH(CH 3) 2 'Pr N3 F F OH H H XII-26-5 p-Me-Ph H H CH2Ph 'Pr N3 F F OH H H XII-26-6 p-Me-Ph H H CH2-indol-3-yl 'Pr N3 F F OH H H XII-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr N3 F F OH H H XII-26-8 p-Me-Ph * H * 'Pr N 3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-27. IRI R2R 3 aR3b R4 t R6 X Y R 7 R XII-27-1 p-F-Ph H H H 'Pr N3 F F OH H H XII-27-2 p-F-Ph H H CH 3 'Pr N3 F F OH H H XII-27-3 p-F-Ph H H CH(CH 3)2 'Pr N3 F F OH H H XII-27-4 p-F-Ph H H CH 2CH(CH 3) 2 'Pr N3 F F OH H H XII-27-5 p-F-Ph H H CH 2Ph 'Pr N3 F F OH H H XII-27-6 p-F-Ph H H CH 2 -indol-3-yl 'Pr N3 F F OH H H

No R R RlaRlb R4 R5 R' X Y R7 R' XII-27-7 p-F-Ph H H CH 2CH 2SCH 3 'Pr N3 F F OH H H XII-27-8 p-F-Ph * H * 'Pr N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-28. RI R2 R 3 a R3 b R4 R' R' X Y R7 R o

XII-28-1 p-Cl-Ph H H H 'Pr N3 F F OH H H XII-28-2 p-Cl-Ph H H CH3 'Pr N3 F F OH H H XII-28-3 p-Cl-Ph H H CH(CH 3) 2 'Pr N3 F F OH H H XII-28-4 p-Cl-Ph H H CH2CH(CH 3) 2 'Pr N3 F F OH H H XII-28-5 p-Cl-Ph H H CH 2Ph 'Pr N3 F F OH H H XII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr N3 F F OH H H XII-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr N3 F F OH H H XII-28-8 p-Cl-Ph * H * 'Pr N3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-29. 4 R 6 No 3 3 IRI R2 RaRb R R X Y R7 R XII-29-1 p-Br-Ph H H H 'Pr N3 F F OH H H XII-29-2 p-Br-Ph H H CH3 'Pr N3 F F OH H H XII-29-3 p-Br-Ph H H CH(CH 3) 2 'Pr N3 F F OH H H XII-29-4 p-Br-Ph H H CH2CH(CH 3) 2 'Pr N3 F F OH H H XII-29-5 p-Br-Ph H H CH 2Ph 'Pr N3 F F OH H H XII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr N3 F F OH H H XII-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr N3 F F OH H H XII-29-8 p-Br-Ph * H * 'Pr N3 F F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XII-30. 456 aRIt RRX 3 'R R2 R Y R7 R XII-30-1 p-I-Ph H H H Pr N3 F F OH H H XII-30-2 p-I-Ph H H CH3 'Pr N3 F F OH H H XII-30-3 p-I-Ph H H CH(CH3) 2 'Pr N3 F F OH H H XII-30-4 p-I-Ph H H CH2CH(CH 3)2 'Pr N3 F F OH H H XII-30-5 p-I-Ph H H CH2Ph 'Pr N3 F F OH H H XII-30-6 p-I-Ph H H CH2-indol-3-yl 'Pr N3 F F OH H H XII-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr N3 F F OH H H XII-30-8 p-I-Ph * H * 'Pr N3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-31. R1 R2 R 3a R 3b R4 R' R' X Y R7 R' No XII-31-1 CH3 H H H "Bu N 3 F F OH H H XII-31-2 CH3 H H CH3 "Bu N 3 F F OH H H XII-31-3 CH3 H H CH(CH 3) 2 "Bu N 3 F F OH H H XII-31-4 CH3 H H CH2CH(CH3) 2 "Bu N 3 F F OH H H XII-31-5 CH3 H H CH 2Ph "Bu N 3 F F OH H H XII-31-6 CH3 H H CH 2-indol-3-yl "Bu N 3 F F OH H H XII-31-7 CH3 H H CH2CH2 SCH3 "Bu N3 F F OH H H XII-31-8 CH3 * H * "Bu N 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-32. N RI R 2 R3a R3b R4 R' R6 X Y R7 R' XII-32-1 Et H H H "Bu N3 F F OH H H XII-32-2 Et H H CH3 "Bu N 3 F F OH H H XII-32-3 Et H H CH(CH 3) 2 "Bu N 3 F F OH H H XII-32-4 Et H H CH2CH(CH 3)2 "Bu N3 F F OH H H XII-32-5 Et H H CH 2Ph "Bu N3 F F OH H H XII-32-6 Et H H CH 2-indol-3-yl "Bu N3 F F OH H H XII-32-7 Et H H CH2CH 2SCH3 "Bu N3 F F OH H H XII-32-8 Et * H * "Bu N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-33. 6 No RI R2 R3 a R3b R4 R5 R X Y R7 R XII-33-1 'Pr H H H "Bu N 3 F F OH H H XII-33-2 'Pr H H CH 3 "Bu N 3 F F OH H H XII-33-3 'Pr H H CH(CH 3) 2 "Bu N 3 F F OH H H XII-33-4 'Pr H H CH 2CH(CH3) 2 "Bu N 3 F F OH H H XII-33-5 Pr H H CH 2Ph "Bu N 3 F F OH H H XII-33-6 Pr H H CH 2-indol-3-yl "Bu N 3 F F OH H H XII-33-7 Pr H H CH 2CH2SCH 3 "Bu N 3 F F OH H H XII-33-8 Pr * H * "Bu N 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-34. No RI 1 R 2 R3 a R3 b R4 R5 R6 X Y R7 R XII-34-1 'Bu H H H "Bu N3 F F OH H H XII-34-2 'Bu H H CH 3 "Bu N3 F F OH H H XII-34-3 'Bu H H CH(CH 3)2 "Bu N3 F F OH H H

R R2 R3 a R3 b R4 R R6 X Y R7 R' No XII-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu N3 F F OH H H XII-34-5 'Bu H H CH 2Ph "Bu N3 F F OH H H XII-34-6 'Bu H H CH 2-indol-3-yl "Bu N3 F F OH H H XII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu N3 F F OH H H XII-34-8 'Bu * H * "Bu N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-35. No RI R2 R3a R 3b R4 R5 R6 X Y R7 R XII-35-1 Ph H H H "Bu N3 F F OH H H XII-35-2 Ph H H CH3 "Bu N 3 F F OH H H XII-35-3 Ph H H CH(CH3 ) 2 "Bu N 3 F F OH H H

XII-35-4 Ph H H CH2CH(CH 3) 2 "Bu N3 F F OH H H XII-35-5 Ph H H CH2Ph "Bu N3 F F OH H H XII-35-6 Ph H H CH2-indol-3-yl "Bu N 3 F F OH H H XII-35-7 Ph H H CH2CH2SCH 3 "Bu N3 F F OH H H XII-35-8 Ph * H * "Bu N3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-36. 'R R2R3aR3b It4 RItRX Y R7 R XII-36-1 p-Me-Ph H H H "Bu N 3 F F OH H H XII-36-2 p-Me-Ph H H CH3 "Bu N 3 F F OH H H XII-36-3 p-Me-Ph H H CH(CH3 ) 2 "Bu N 3 F F OH H H XII-36-4 p-Me-Ph H H CH2 CH(CH 3 ) 2 "Bu N 3 F F OH H H

XII-36-5 p-Me-Ph H H CH2 Ph "Bu N3 F F OH H H XII-36-6 p-Me-Ph H H CH2-indol-3-yl "Bu N 3 F F OH H H

XII-36-7 p-Me-Ph H H CH2 CH 2 SCH 3 "Bu N3 F F OH H H XII-36-8 p-Me-Ph * H * "Bu N 3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-37. No RI R2 R3 a R3b R4 R5 R 6 X Y R7 R XII-37-1 p-F-Ph H H H "Bu N3 F F OH H H

XII-37-2 p-F-Ph H H CH 3 "Bu N3 F F OH H H

XII-37-3 p-F-Ph H H CH(CH 3 )2 "Bu N3 F F OH H H

XII-37-4 p-F-Ph H H CH 2 CH(CH 3) 2 "Bu N3 F F OH H H

XII-37-5 p-F-Ph H H CH 2 Ph "Bu N3 F F OH H H XII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu N3 F F OH H H

R R R4 R' R 6 X Y R7 R' No RlaRlb

XII-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu N3 F F OH H H XII-37-8 p-F-Ph * H * "Bu N3 F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XII-38. o RI R2 R 3 a R3 b R4 R' R' X Y R7 R XII-38-1 p-Cl-Ph H H H "Bu N3 F F OH H H XII-38-2 p-Cl-Ph H H CH3 "Bu N3 F F OH H H XII-38-3 p-Cl-Ph H H CH(CH 3) 2 "Bu N3 F F OH H H XII-38-4 p-Cl-Ph H H CH2CH(CH 3) 2 "Bu N3 F F OH H H XII-38-5 p-Cl-Ph H H CH 2Ph "Bu N3 F F OH H H XII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu N3 F F OH H H XII-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu N3 F F OH H H XII-38-8 p-Cl-Ph * H * "Bu N3 F F OH H H

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XII-39. No RI R2 R 3a R3 b R4 R R6 X Y R7 R XII-39-1 p-Br-Ph H H H "Bu N 3 F F OH H H

XII-39-2 p-Br-Ph H H CH3 "Bu N 3 F F OH H H XII-39-3 p-Br-Ph H H CH(CH 3) 2 "Bu N 3 F F OH H H XII-39-4 p-Br-Ph H H CH2CH(CH 3 ) 2 "Bu N 3 F F OH H H XII-39-5 p-Br-Ph H H CH 2Ph "Bu N3 F F OH H H XII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu N 3 F F OH H H XII-39-7 p-Br-Ph H H CH2CH 2 SCH 3 "Bu N3 F F OH H H XII-39-8 p-Br-Ph * H * "Bu N3 F F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XII-40. R I R2 R3a R3 b R4 R5 R6 X Y R7 R XII-40-1 p-I-Ph H H H "Bu N 3 F F OH H H XII-40-2 p-I-Ph H H CH3 "Bu N 3 F F OH H H XII-40-3 p-I-Ph H H CH(CH3)2 "Bu N 3 F F OH H H XII-40-4 p-I-Ph H H CH2CH(CH 3) 2 "Bu N3 F F OH H H XII-40-5 p-I-Ph H H CH2Ph "Bu N3 F F OH H H XII-40-6 p-I-Ph H H CH2-indol-3-yl "Bu N 3 F F OH H H XII-40-7 p-I-Ph H H CH2CH 2SCH 3 "Bu N3 F F OH H H XII-40-8 p-I-Ph * H * "Bu N3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ wo_

Table XII-41. No R R2 R3 a R 3b R4 R 5 R6 X Y R7 R' XII-41-1 CH3 H H H Bz N3 F F OH H H XII-41-2 CH3 H H CH3 Bz N3 F F OH H H XII-41-3 CH3 H H CH(CH3)2 Bz N3 F F OH H H XII-41-4 CH3 H H CH2CH(CH3) 2 Bz N3 F F OH H H XII-41-5 CH3 H H CH 2Ph Bz N3 F F OH H H XII-41-6 CH3 H H CH 2-indol-3-yl Bz N3 F F OH H H XII-41-7 CH3 H H CH2CH2 SCH3 Bz N3 F F OH H H XII-41-8 CH3 * H * Bz N3 F F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XII-42. R R2 R3 a R 3b R4 R' R' X Y R7 R' No XII-42-1 Et H H H Bz N3 F F OH H H XII-42-2 Et H H CH3 Bz N3 F F OH H H XII-42-3 Et H H CH(CH 3) 2 Bz N3 F F OH H H XII-42-4 Et H H CH2CH(CH 3) 2 Bz N3 F F OH H H XII-42-5 Et H H CH 2Ph Bz N3 F F OH H H XII-42-6 Et H H CH 2-indol-3-yl Bz N3 F F OH H H XII-42-7 Et H H CH2CH 2SCH3 Bz N3 F F OH H H XII-42-8 Et * H * Bz N3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-43. N Rl R2 R3 a R3 b 4 R' R6 X Y R7 R XII-43-1 'Pr H H H Bz N3 F F OH H H XII-43-2 'Pr H H CH 3 Bz N3 F F OH H A XII-43-3 'Pr H H CH(CH 3) 2 Bz N3 F F OH H H XII-43-4 'Pr H H CH 2CH(CH3) 2 Bz N3 F F OH H H XII-43-5 'Pr H H CH 2Ph Bz N3 F F OH H H XII-43-6 'Pr H H CH 2-indol-3-yl Bz N3 F F OH H H XII-43-7 'Pr H H CH 2CH2SCH 3 Bz N3 F F OH H H XII-43-8 'Pr * H * Bz N3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-44. RI R2 R3 a R3 b R4 R R6 X Y R7 R No XII-44-1 'Bu H H H Bz N3 F F OH H H XII-44-2 'Bu H H CH 3 Bz N3 F F OH H H XII-44-3 'Bu H H CH(CH 3)2 Bz N3 F F OH H H XII-44-4 'Bu H H CH 2CH(CH 3) 2 Bz N3 F F OH H H XII-44-5 'Bu H H CH 2Ph Bz N3 F F OH H H XII-44-6 'Bu H H CH 2-indol-3-yl Bz N3 F F OH H H XII-44-7 'Bu H H CH 2CH 2SCH 3 Bz N3 F F OH H H XII-44-8 'Bu * H * Bz N3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 771 _

Table XII-45. RI No R2 RaR 3 b R4 R5 R' X Y R7 R' XII-45-1 Ph H H H Bz N 3 F F OH H H XII-45-2 Ph H H CH3 Bz N 3 F F OH H H XII-45-3 Ph H H CH(CH3) 2 Bz N 3 F F OH H H XII-45-4 Ph H H CH2CH(CH 3) 2 Bz N 3 F F OH H H XII-45-5 Ph H H CH2Ph Bz N 3 F F OH H H XII-45-6 Ph H H CH2-indol-3-yl Bz N 3 F F OH H H XII-45-7 Ph H H CH2CH2SCH 3 Bz N 3 F F OH H H XII-45-8 Ph * H * Bz N 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-46. N R1 R2 R3 a R3 b 4 R5 R6 X Y R7 R XII-46-1 p-Me-Ph H H H Bz N 3 F F OH H H XII-46-2 p-Me-Ph H H CH3 Bz N 3 F F OH H H XII-46-3 p-Me-Ph H H CH(CH3) 2 Bz N 3 F F OH H H XII-46-4 p-Me-Ph H H CH2CH(CH 3)2 Bz N 3 F F OH H H XII-46-5 p-Me-Ph H H CH2Ph Bz N 3 F F OH H H XII-46-6 p-Me-Ph H H CH2-indol-3-yl Bz N 3 F F OH H H XII-46-7 p-Me-Ph H H CH2CH2SCH 3 Bz N 3 F F OH H H XII-46-8 p-Me-Ph * H * Bz N 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XII-47. RI 1 R3 a 4 R R R R7 R No R2 R3b X Y

XII-47-1 p-F-Ph H H H Bz N3 F F OH H H XII-47-2 p-F-Ph H H CH 3 Bz N3 F F OH H H XII-47-3 p-F-Ph H H CH(CH 3)2 Bz N3 F F OH H H XII-47-4 p-F-Ph H H CH 2CH(CH 3) 2 Bz N3 F F OH H H XII-47-5 p-F-Ph H H CH 2Ph Bz N3 F F OH H H XII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz N3 F F OH H H XII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz N3 F F OH H H XII-47-8 p-F-Ph * H * Bz N3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

t 17 )-

Table XII-48. No R R2 R 3 a R3b R4 R' R6 X Y R7 R' XII-48-1 p-Cl-Ph H H H Bz N3 F F OH H H XII-48-2 p-Cl-Ph H H CH3 Bz N3 F F OH H H XII-48-3 p-Cl-Ph H H CH(CH 3) 2 Bz N3 F F OH H H XII-48-4 p-Cl-Ph H H CH2CH(CH 3) 2 Bz N3 F F OH H H XII-48-5 p-Cl-Ph H H CH 2Ph Bz N3 F F OH H H XII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz N3 F F OH H H XII-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz N3 F F OH H H XII-48-8 p-Cl-Ph * H * Bz N3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-49. N9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' XII-49-1 p-Br-Ph H H H Bz N3 F F OH H H XII-49-2 p-Br-Ph H H CH3 Bz N3 F F OH H H XII-49-3 p-Br-Ph H H CH(CH 3) 2 Bz N3 F F OH H H XII-49-4 p-Br-Ph H H CH2CH(CH 3) 2 Bz N3 F F OH H H XII-49-5 p-Br-Ph H H CH 2Ph Bz N3 F F OH H H XII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz N3 F F OH H H XII-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz N3 F F OH H H XII-49-8 p-Br-Ph * H * Bz N3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XII-50. No RI 1 R2 R3 a R 3b 4 R5 R6 X Y R7 R XII-50-1 p-I-Ph H H H Bz N 3 F F OH H H XII-50-2 p-I-Ph H H CH3 Bz N 3 F F OH H H XII-50-3 p-I-Ph H H CH(CH3) 2 Bz N 3 F F OH H H XII-50-4 p-I-Ph H H CH2CH(CH 3) 2 Bz N 3 F F OH H H XII-50-5 p-I-Ph H H CH2Ph Bz N 3 F F OH H H XII-50-6 p-I-Ph H H CH2-indol-3-yl Bz N 3 F F OH H H XII-50-7 p-I-Ph H H CH2CH2SCH 3 Bz N 3 F F OH H H XII-50-8 p-I-Ph * H * Bz N3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 72-

R8 NH

Rt 2 0 R3 b R2 N O R3aN- -P 0 0

CO2R4 OR 1 R5 R6

Y X XIII

Table XIII-1. R No R1 R2 R 3a R3 b R4 R6 X Y R7 R' XIII-1-1 CH3 H H H CH 3 N3 H F OH H H XIII-1-2 CH3 H H CH 3 CH 3 N3 H F OH H H XIII-1-3 CH3 H H CH(CH 3) 2 CH 3 N3 H F OH H H XIII-1-4 CH3 H H CH 2CH(CH 3)2 CH 3 N3 H F OH H H XIII-1-5 CH3 H H CH 2Ph CH 3 N3 H F OH H H XIII-1-6 CH3 H H CH 2-indol-3-yl CH 3 N3 H F OH H H XIII-1-7 CH3 H H CH 2CH 2 SCH 3 CH 3 N3 H F OH H H XIII-1-8 CH3 * H * CH 3 N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-2. N RI R2 R3a R 3b R4 R5 R6 X Y R7 R' XIII-2-1 Et H H H CH 3 N3 H F OH H H XIII-2-2 Et H H CH 3 CH 3 N3 H F OH H H XIII-2-3 Et H H CH(CH 3) 2 CH 3 N3 H F OH H H XIII-2-4 Et H H CH 2CH(CH 3)2 CH 3 N3 H F OH H H XIII-2-5 Et H H CH 2Ph CH 3 N3 H F OH H H XIII-2-6 Et H H CH 2-indol-3-yl CH 3 N3 H F OH H H XIII-2-7 Et H H CH 2CH2SCH 3 CH 3 N3 H F OH H H XIII-2-8 Et * H * CH 3 N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

17A-

Table XIII-3. No RI R2 R3 a R 3 b R4 R R X Y R7 R' XIII-3-1 'Pr H H H CH3 N 3 H F OH H H XIII-3-2 'Pr H H CH 3 CH3 N 3 H F OH H H XIII-3-3 'Pr H H CH(CH3) 2 CH 3 N 3 H F OH H H XIII-3-4 'Pr H H CH 2CH(CH 3) 2 CH 3 N 3 H F OH H H XIII-3-5 'Pr H H CH 2Ph CH3 N 3 H F OH H H XIII-3-6 'Pr H H CH 2-indol-3-yl CH 3 N 3 H F OH H H XIII-3-7 'Pr H H CH 2CH2SCH 3 CH 3 N 3 H F OH H H XIII-3-8 'Pr * H * CH3 N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-4. No R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R XIII-4-1 'Bu H H H CH3 N 3 H F OH H H XIII-4-2 'Bu H H CH 3 CH 3 N 3 H F OH H H XIII-4-3 'Bu H H CH(CH 3) 2 CH3 N 3 H F OH H H XIII-4-4 'Bu H H CH 2CH(CH 3) 2 CH3 N 3 H F OH H H XIII-4-5 'Bu H H CH 2Ph CH3 N 3 H F OH H H XIII-4-6 'Bu H H CH 2-indol-3-yl CH 3 N 3 H F OH H H XIII-4-7 'Bu H H CH 2CH 2SCH 3 CH3 N 3 H F OH H H XIII-4-8 'Bu * H * CH3 N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-5. No RI R2 R 3a R 3b 4 R5 R 6 X Y R7 R XIII-5-1 Ph H H H CH 3 N 3 H F OH H H XIII-5-2 Ph H H CH 3 CH 3 N 3 H F OH H H XIII-5-3 Ph H H CH(CH 3)2 CH 3 N 3 H F OH H H XIII-5-4 Ph H H CH 2CH(CH 3)2 CH 3 N 3 H F OH H H XIII-5-5 Ph H H CH 2Ph CH 3 N 3 H F OH H H XIII-5-6 Ph H H CH 2-indol-3-yl CH 3 N 3 H F OH H H XIII-5-7 Ph H H CH 2CH2SCH 3 CH 3 N 3 H F OH H H XIII-5-8 Ph * H * CH 3 N 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

1 77 r

Table XIII-6. R R 2 R 3 a R 3b R4 R R 6 X Y R7 R' No XIII-6-1 p-Me-Ph H H H CH 3 N 3 H F OH H H XIII-6-2 p-Me-Ph H H CH 3 CH 3 N 3 H F OH H H XIII-6-3 p-Me-Ph H H CH(CH 3)2 CH 3 N 3 H F OH H H XIII-6-4 p-Me-Ph H H CH 2CH(CH 3)2 CH 3 N 3 H F OH H H XIII-6-5 p-Me-Ph H H CH 2Ph CH 3 N 3 H F OH H H XIII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 N 3 H F OH H H XIII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH 3 N 3 H F OH H H XIII-6-8 p-Me-Ph * H * CH 3 N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-7. N R1 R2 R3 a R3 b 4 R' R 6 X Y R7 R' XIII-7-1 p-F-Ph H H H CH 3 N 3 H F OH H H XIII-7-2 p-F-Ph H H CH3 CH 3 N 3 H F OH H H XIII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 N 3 H F OH H H XIII-7-4 p-F-Ph H H CH2CH(CH 3) 2 CH 3 N 3 H F OH H H XIII-7-6 p-F-Ph H H CH2Ph CH 3 N 3 H F OH H H XIII-7-7 p-F-Ph H H CH2-indol-3-yl CH 3 N 3 H F OH H H XIII-7-8 p-F-Ph H H CH2CH2SCH 3 CH 3 N 3 H F OH H H XIII-7-20 p-F-Ph * H * CH 3 N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-8. No RI 1 R2 R 3 a R3b R4 R5 R 6 X Y R7 R XIII-8-1 p-Cl-Ph H H H CH3 N 3 H F OH H H XIII-8-2 p-Cl-Ph H H CH3 CH3 N 3 H F OH H H XIII-8-3 p-Cl-Ph H H CH(CH 3) 2 CH3 N 3 H F OH H H XIII-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH3 N 3 H F OH H H XIII-8-5 p-Cl-Ph H H CH 2Ph CH3 N 3 H F OH H H XIII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 N 3 H F OH H H XIII-8-7 p-Cl-Ph H H CH2CH2 SCH3 CH3 N 3 H F OH H H XIII-8-8 p-Cl-Ph * H * CH3 N 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1 7 r,

Table XIII-9. R RR 3 R3b R4 R' R' X Y R7 R' No a

XIII-9-1 p-Br-Ph H H H CH 3 N 3 H F OH H H XIII-9-2 p-Br-Ph H H CH 3 CH3 N 3 H F OH H H XIII-9-3 p-Br-Ph H H CH(CH 3) 2 CH3 N 3 H F OH H H XIII-9-4 p-Br-Ph H H CH 2CH(CH 3) 2 CH 3 N 3 H F OH H H XIII-9-6 p-Br-Ph H H CH 2Ph CH 3 N 3 H F OH H H XIII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 N 3 H F OH H H XIII-9-8 p-Br-Ph H H CH 2CH2SCH 3 CH3 N 3 H F OH H H XIII-9-20 p-Br-Ph * H * CH 3 N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-10. N R R2 R3a R3 b R4 R' R X Y R7 R' XIII-10-1 p-I-Ph H H H CH3 N 3 H F OH H H XIII-10-2 p-I-Ph H H CH 3 CH3 N 3 H F OH H H XIII-10-3 p-I-Ph H H CH(CH 3) 2 CH 3 N 3 H F OH H H XIII-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 N 3 H F OH H H XIII-10-5 p-I-Ph H H CH 2Ph CH3 N 3 H F OH H H XIII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 N 3 H F OH H H XIII-10-7 p-I-Ph H H CH 2CH2SCH 3 CH 3 N 3 H F OH H H XIII-10-8 p-I-Ph * H * CH 3 N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-11. No RI1 R2 R3 a R3b R4 R5 R6 X Y R7 R XIII-11-1 CH 3 H H H Et N3 H F OH H H XIII-11-2 CH 3 H H CH3 Et N3 H F OH H H XIII-11-3 CH3 H H CH(CH 3) 2 Et N3 H F OH H H XIII-11-4 CH3 H H CH2CH(CH 3) 2 Et N3 H F OH H H XIII-11-5 CH3 H H CH 2Ph Et N3 H F OH H H XIII-11-6 CH3 H H CH 2-indol-3-yl Et N3 H F OH H H XIII-11-7 CH3 H H CH2CH 2SCH 3 Et N3 H F OH H H XIII-11-8 CH3 * H * Et N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1'77-

Table XIII-12. R1 R2 R3 a R3b R4 R' R6 X Y R7 R' No XIII-12-1 Et H H H Et N3 H F OH H H XIII-12-2 Et H H CH3 Et N3 H F OH H H XIII-12-3 Et H H CH(CH 3) 2 Et N3 H F OH H H XIII-12-4 Et H H CH2CH(CH 3) 2 Et N3 H F OH H H XIII-12-5 Et H H CH 2Ph Et N3 H F OH H H XIII-12-6 Et H H CH 2-indol-3-yl Et N3 H F OH H H XIII-12-7 Et H H CH2CH2SCH 3 Et N3 H F OH H H XIII-12-8 Et * H * Et N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-13. N9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' XIII-13-1 'Pr H H H Et N3 H F OH H H XIII-13-2 'Pr H H CH 3 Et N3 H F OH H H XIII-13-3 'Pr H H CH(CH 3)2 Et N3 H F OH H H XIII-13-4 'Pr H H CH 2CH(CH 3) 2 Et N3 H F OH H H XIII-13-5 'Pr H H CH 2Ph Et N3 H F OH H H XIII-13-6 'Pr H H CH 2-indol-3-yl Et N3 H F OH H H XIII-13-7 'Pr H H CH 2CH 2SCH 3 Et N3 H F OH H H XIII-13-8 'Pr * H * Et N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-14. No R IR2 R3a R3b R4 R5 R6 X Y R7 R XIII-14-1 'Bu H H H Et N3 H F OH H H XIII-14-2 'Bu H H CH3 Et N3 H F OH H H XIII-14-3 'Bu H H CH(CH 3) 2 Et N3 H F OH H H XIII-14-4 'Bu H H CH2CH(CH 3) 2 Et N3 H F OH H H XIII-14-5 'Bu H H CH 2Ph Et N3 H F OH H H XIII-14-6 'Bu H H CH 2-indol-3-yl Et N3 H F OH H H XIII-14-7 'Bu H H CH2CH 2SCH 3 Et N3 H F OH H H XIII-14-8 'Bu * H * Et N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

1 7S2-

Table XIII-15. No RI R2 RaR3 b R 5 R6 X Y R7 R' XIII-15-1 Ph H H H Et N3 H F OH H H XIII-15-2 Ph H H CH 3 Et N3 H F OH H H XIII-15-3 Ph H H CH(CH 3) 2 Et N3 H F OH H H XIII-15-4 Ph H H CH 2CH(CH3) 2 Et N3 H F OH H H XIII-15-5 Ph H H CH 2Ph Et N3 H F OH H H XIII-15-6 Ph H H CH 2-indol-3-yl Et N3 H F OH H H XIII-15-7 Ph H H CH 2CH2SCH 3 Et N3 H F OH H H XIII-15-8 Ph * H * Et N3 H F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-16. N9 R1 R 2 R 3 a R3 b R 4 R 5 R 6 X Y R7 R' XIII-16-1 p-Me-Ph H H H Et N3 H F OH H H XIII-16-2 p-Me-Ph H H CH 3 Et N3 H F OH H H XIII-16-3 p-Me-Ph H H CH(CH 3) 2 Et N3 H F OH H H XIII-16-4 p-Me-Ph H H CH 2CH(CH3)2 Et N3 H F OH H H XIII-16-5 p-Me-Ph H H CH 2Ph Et N3 H F OH H H XIII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et N3 H F OH H H XIII-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et N3 H F OH H H XIII-16-8 p-Me-Ph * H * Et N3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-17. 6 No R1 R2 R3 a R 3b R 5 R X Y R7 R' XIII-17-1 p-F-Ph H H H Et N3 H F OH H H XIII-17-2 p-F-Ph H H CH3 Et N3 H F OH H H XIII-17-3 p-F-Ph H H CH(CH3) 2 Et N3 H F OH H H XIII-17-4 p-F-Ph H H CH2CH(CH 3) 2 Et N3 H F OH H H XIII-17-5 p-F-Ph H H CH2Ph Et N3 H F OH H H XIII-17-6 p-F-Ph H H CH2-indol-3-yl Et N3 H F OH H H XIII-17-7 p-F-Ph H H CH2CH2SCH 3 Et N3 H F OH H H XIII-17-8 p-F-Ph * H * Et N3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 70 _

Table XIII-18. R R2 R 3 R 3b R4 R R' X Y R7 R' No a

XIII-18-1 p-Cl-Ph H H H Et N3 H F OH H H XIII-18-2 p-Cl-Ph H H CH3 Et N3 H F OH H H XIII-18-3 p-Cl-Ph H H CH(CH 3)2 Et N3 H F OH H H XIII-18-4 p-Cl-Ph H H CH2CH(CH 3)2 Et N3 H F OH H H XIII-18-5 p-Cl-Ph H H CH 2Ph Et N3 H F OH H H XIII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et N3 H F OH H H XIII-18-7 p-Cl-Ph H H CH2CH 2SCH 3 Et N3 H F OH H H XIII-18-8 p-Cl-Ph * H * Et N3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIII-19. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y R7 R' XIII-19-1 p-Br-Ph H H H Et N3 H F OH H H XIII-19-2 p-Br-Ph H H CH 3 Et N3 H F OH H H XIII-19-3 p-Br-Ph H H CH(CH 3) 2 Et N3 H F OH H H XIII-19-4 p-Br-Ph H H CH 2CH(CH 3)2 Et N3 H F OH H H XIII-19-5 p-Br-Ph H H CH 2Ph Et N3 H F OH H H XIII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et N3 H F OH H H XIII-19-7 p-Br-Ph H H CH 2CH2SCH 3 Et N3 H F OH H H XIII-19-8 p-Br-Ph * H * Et N3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIII-20. No R R2 R 3 a R 3b R 4 R 5 R 6 X Y R7 R' XIII-20-1 p-I-Ph H H H Et N3 H F OH H H XIII-20-2 p-I-Ph H H CH 3 Et N3 H F OH H H XIII-20-3 p-I-Ph H H CH(CH 3) 2 Et N3 H F OH H H XIII-20-4 p-I-Ph H H CH 2CH(CH3) 2 Et N3 H F OH H H XIII-20-5 p-I-Ph H H CH 2Ph Et N3 H F OH H H XIII-20-6 p-I-Ph H H CH 2-indol-3-yl Et N3 H F OH H H XIII-20-7 p-I-Ph H H CH 2CH2SCH 3 Et N3 H F OH H H XIII-20-8 p-I-Ph * H * Et N3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

ISMn

Table XIII-21. No R1 R 2 R3 a R3b R4 R' R6 X Y R7 R' XIII-21-1 CH 3 H H H 'Pr N 3 H F OH H H XIII-21-2 CH 3 H H CH3 'Pr N 3 H F OH H H XIII-21-3 CH 3 H H CH(CH 3) 2 'Pr N 3 H F OH H H XIII-21-4 CH 3 H H CH2CH(CH 3) 2 'Pr N 3 H F OH H H XIII-21-5 CH 3 H H CH 2Ph 'Pr N 3 H F OH H H XIII-21-6 CH 3 H H CH 2-indol-3-yl 'Pr N 3 H F OH H H XIII-21-7 CH 3 H H CH2CH 2SCH 3 'Pr N 3 H F OH H H XIII-21-8 CH 3 * H * 'Pr N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-22. N9 Rl R 2 R3 a R3 b R4 R R6 X Y R7 R' XIII-22-1 Et H H H 'Pr N 3 H F OH H H XIII-22-2 Et H H CH3 'Pr N 3 H F OH H H XIII-22-3 Et H H CH(CH 3) 2 'Pr N 3 H F OH H H XIII-22-4 Et H H CH2CH(CH 3) 2 'Pr N 3 H F OH H H XIII-22-5 Et H H CH 2Ph 'Pr N 3 H F OH H H XIII-22-6 Et H H CH 2-indol-3-yl 'Pr N 3 H F OH H H XIII-22-7 Et H H CH2CH2SCH 3 'Pr N 3 H F OH H H XIII-22-8 Et * H * 'Pr N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-23. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' XIII-23-1 'Pr H H H 'Pr N 3 H F OH H H XIII-23-2 'Pr H H CH 3 'Pr N 3 H F OH H H XIII-23-3 'Pr H H CH(CH 3)2 'Pr N 3 H F OH H H XIII-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr N 3 H F OH H H XIII-23-5 Pr H H CH 2Ph 'Pr N 3 H F OH H H XIII-23-6 Pr H H CH 2-indol-3-yl 'Pr N 3 H F OH H H XIII-23-7 Pr H H CH 2CH 2SCH 3 'Pr N 3 H F OH H H XIII-23-8 Pr * H * 'Pr N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-24. No R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' XIII-24-1 'Bu H H H 'Pr N 3 H F OH H H XIII-24-2 'Bu H H CH3 'Pr N 3 H F OH H H XIII-24-3 'Bu H H CH(CH3) 2 'Pr N 3 H F OH H H

_2)Q1 _

R R2 R 3a R3 b R4 R' R' X Y R7 R' No XIII-24-4 'Bu H H CH2 CH(CH 3 )2 'Pr N3 H F OH H H XIII-24-5 'Bu H H CH2Ph 'Pr N3 H F OH H H XIII-24-6 'Bu H H CH2-indol-3-yl 'Pr N3 H F OH H H XIII-24-7 'Bu H H CH2CH 2SCH 3 'Pr N3 H F OH H H XIII-24-8 'Bu * H * 'Pr N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-25. R No R2 R 3 a R 3b R4 R5 R 6 X Y R7 R' XIII-25-1 Ph H H H 'Pr N3 H F OH H H XIII-25-2 Ph H H CH 3 'Pr N3 H F OH H H XIII-25-3 Ph H H CH(CH 3) 2 'Pr N3 H F OH H H XIII-25-4 Ph H H CH 2CH(CH3) 2 'Pr N3 H F OH H H XIII-25-5 Ph H H CH 2Ph 'Pr N3 H F OH H H XIII-25-6 Ph H H CH 2-indol-3-yl 'Pr N3 H F OH H H XIII-25-7 Ph H H CH 2CH2SCH 3 'Pr N3 H F OH H H XIII-25-8 Ph * H * 'Pr N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-26. I' R R2 R3aRIt 4R5R6XY R7 R XIII-26-1 p-Me-Ph H H H 'Pr N3 H F OH H H XIII-26-2 p-Me-Ph H H CH 3 'Pr N3 H F OH H H XIII-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr N3 H F OH H H XIII-26-4 p-Me-Ph H H CH 2CH(CH3) 2 'Pr N3 H F OH H H XIII-26-5 p-Me-Ph H H CH 2Ph 'Pr N3 H F OH H H XIII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr N3 H F OH H H XIII-26-7 p-Me-Ph H H CH 2CH 2SCH 3 'Pr N3 H F OH H H XIII-26-8 p-Me-Ph * H * 'Pr N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-27. RR No R1 R2 R3 a R3 b R' X Y R7 R' XIII-27-1 p-F-Ph H H H 'Pr N 3 H F OH H H XIII-27-2 p-F-Ph H H CH3 'Pr N 3 H F OH H H XIII-27-3 p-F-Ph H H CH(CH3) 2 'Pr N 3 H F OH H H XIII-27-4 p-F-Ph H H CH2CH(CH 3) 2 'Pr N 3 H F OH H H XIII-27-5 p-F-Ph H H CH2Ph 'Pr N 3 H F OH H H XIII-27-6 p-F-Ph H H CH2-indol-3-yl 'Pr N 3 H F OH H H XIII-27-7 p-F-Ph H H CH2 CH 2 SCH 3 'Pr N3 H F OH H H XIII-27-8 p-F-Ph * H * 'Pr N 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-28. N R1 R2 R 3a R3 b R4 R' R6 X Y R7 R XIII-28-1 p-Cl-Ph H H H 'Pr N 3 H F OH H H XIII-28-2 p-Cl-Ph H H CH3 'Pr N 3 H F OH H H XIII-28-3 p-Cl-Ph H H CH(CH 3)2 'Pr N 3 H F OH H H XIII-28-4 p-Cl-Ph H H CH2CH(CH 3)2 'Pr N 3 H F OH H H XIII-28-5 p-Cl-Ph H H CH 2Ph 'Pr N 3 H F OH H H XIII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr N 3 H F OH H H XIII-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr N 3 H F OH H H XIII-28-8 p-Cl-Ph * H * 'Pr N 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIII-29. No RI 1 R2 R3 a R3b R4 R5 R6 X Y R7 R XIII-29-1 p-Br-Ph H H H 'Pr N 3 H F OH H H XIII-29-2 p-Br-Ph H H CH 3 'Pr N 3 H F OH H H XIII-29-3 p-Br-Ph H H CH(CH 3) 2 'Pr N 3 H F OH H H XIII-29-4 p-Br-Ph H H CH 2CH(CH 3) 2 'Pr N 3 H F OH H H XIII-29-5 p-Br-Ph H H CH 2Ph 'Pr N 3 H F OH H H XIII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr N 3 H F OH H H XIII-29-7 p-Br-Ph H H CH 2CH2SCH 3 'Pr N 3 H F OH H H XIII-29-8 p-Br-Ph * H * 'Pr N 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIII-30. 4 No RI R2 R3 a RIt R5 R 6 X Y R7 R XIII-30-1 p-I-Ph H H H 'Pr N 3 H F OH H H XIII-30-2 p-I-Ph H H CH 3 'Pr N 3 H F OH H H XIII-30-3 p-I-Ph H H CH(CH 3) 2 'Pr N 3 H F OH H H

IS22 -

R R2 R 3 Rb R4 R R' X Y R7 R' No a

XIII-30-4 p-I-Ph H H CH 2CH(CH3) 2 'Pr N3 H F OH H H XIII-30-5 p-I-Ph H H CH 2Ph 'Pr N3 H F OH H H XIII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr N3 H F OH H H XIII-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr N3 H F OH H H XIII-30-8 p-I-Ph * H * 'Pr N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-31. No RI R2 R 3 a R3 b R4 R' R6 X Y R7 R XIII-31-1 CH 3 H H H "Bu N3 H F OH H H XIII-31-2 CH 3 H H CH3 "Bu N3 H F OH H H XIII-31-3 CH 3 H H CH(CH 3) 2 "Bu N3 H F OH H H XIII-31-4 CH 3 H H CH2CH(CH 3) 2 "Bu N3 H F OH H H XIII-31-5 CH 3 H H CH 2Ph "Bu N3 H F OH H H XIII-31-6 CH 3 H H CH 2-indol-3-yl "Bu N3 H F OH H H XIII-31-7 CH 3 H H CH2CH 2SCH 3 "Bu N3 H F OH H H XIII-31-8 CH 3 * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-32. I1R R2 R3a R3b R4 R R6X Y R7 R

XIII-32-1 Et H H H "Bu N3 H F OH H H XIII-32-2 Et H H CH3 "Bu N3 H F OH H H XIII-32-3 Et H H CH(CH 3) 2 "Bu N3 H F OH H H XIII-32-4 Et H H CH2CH(CH 3) 2 "Bu N3 H F OH H H XIII-32-5 Et H H CH 2Ph "Bu N3 H F OH H H XIII-32-6 Et H H CH 2-indol-3-yl "Bu N3 H F OH H H XIII-32-7 Et H H CH2CH2SCH 3 "Bu N3 H F OH H H XIII-32-8 Et * H * "Bu N3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-33. 1 R R2R3aR3b R4 R5 R6 X Y R7 R XIII-33-1 'Pr H H H "Bu N3 H F OH H H XIII-33-2 'Pr H H CH 3 "Bu N3 H F OH H H XIII-33-3 'Pr H H CH(CH 3)2 "Bu N3 H F OH H H XIII-33-4 'Pr H H CH 2CH(CH 3) 2 "Bu N3 H F OH H H XIII-33-5 'Pr H H CH 2Ph "Bu N3 H F OH H H XIII-33-6 'Pr H H CH 2-indol-3-yl "Bu N3 H F OH H H

R1 R2 R3 a R3 b R4 R R' X Y R7 R' No XIII-33-7 'Pr H H CH 2CH 2SCH 3 "Bu N3 H F OH H H XIII-33-8 'Pr * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-34. No RI R2 R 3a R3 b R4 R' R' X Y R7 R' XIII-34-1 'Bu H H H "Bu N 3 H F OH H H XIII-34-2 'Bu H H CH3 "Bu N 3 H F OH H H XIII-34-3 'Bu H H CH(CH3) 2 "Bu N 3 H F OH H H XIII-34-4 'Bu H H CH2CH(CH 3)2 "Bu N 3 H F OH H H XIII-34-5 'Bu H H CH2Ph "Bu N 3 H F OH H H XIII-34-6 'Bu H H CH2-indol-3-yl "Bu N 3 H F OH H H

XIII-34-7 'Bu H H CH2CH 2SCH 3 "Bu N 3 H F OH H H XIII-34-8 'Bu * H * "Bu N 3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-35. 1 R R2 R3a R3b R4 R5R6X Y R7 R XIII-35-1 Ph H H H "Bu N3 H F OH H H XIII-35-2 Ph H H CH 3 "Bu N3 H F OH H H XIII-35-3 Ph H H CH(CH 3) 2 "Bu N3 H F OH H H

XIII-35-4 Ph H H CH 2CH(CH3) 2 "Bu N3 H F OH H H XIII-35-5 Ph H H CH 2Ph "Bu N3 H F OH H H XIII-35-6 Ph H H CH 2-indol-3-yl "Bu N3 H F OH H H

XIII-35-7 Ph H H CH 2 CH2 SCH 3 "Bu N3 H F OH H H

XIII-35-8 Ph * H * "Bu N3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-36. No RI R2 R 3a RIt 4 R5 R 6 X Y R7 R XIII-36-1 p-Me-Ph H H H "Bu N3 H F OH H H

XIII-36-2 p-Me-Ph H H CH 3 "Bu N3 H F OH H H

XIII-36-3 p-Me-Ph H H CH(CH 3)2 "Bu N3 H F OH H H

XIII-36-4 p-Me-Ph H H CH 2 CH(CH3 ) 2 "Bu N3 H F OH H H

XIII-36-5 p-Me-Ph H H CH 2Ph "Bu N3 H F OH H H

XIII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu N3 H F OH H H

XIII-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu N3 H F OH H H

XIII-36-8 p-Me-Ph * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

IsQ;-

Table XIII-37. R No R1 R2 R3 a R3 b RR X Y R7 R' XIII-37-1 p-F-Ph H H H "Bu N 3 H F OH H H XIII-37-2 p-F-Ph H H CH3 "Bu N 3 H F OH H H XIII-37-3 p-F-Ph H H CH(CH3) 2 "Bu N 3 H F OH H H XIII-37-4 p-F-Ph H H CH2CH(CH 3) 2 "Bu N 3 H F OH H H XIII-37-5 p-F-Ph H H CH2Ph "Bu N 3 H F OH H H XIII-37-6 p-F-Ph H H CH2-indol-3-yl "Bu N 3 H F OH H H XIII-37-7 p-F-Ph H H CH2CH 2SCH 3 "Bu N3 H F OH H H XIII-37-8 p-F-Ph * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-38. R' No R1 R 2 R 3a R3 b R4 R6 X Y R7 R' XIII-38-1 p-Cl-Ph H H H "Bu N3 H F OH H H XIII-38-2 p-Cl-Ph H H CH 3 "Bu N3 H F OH H H XIII-38-3 p-Cl-Ph H H CH(CH 3)2 "Bu N3 H F OH H H XIII-38-4 p-Cl-Ph H H CH 2CH(CH 3)2 "Bu N3 H F OH H H XIII-38-5 p-Cl-Ph H H CH 2Ph "Bu N3 H F OH H H XIII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu N3 H F OH H H XIII-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu N3 H F OH H H XIII-38-8 p-Cl-Ph * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIII-39. No RI1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XIII-39-1 p-Br-Ph H H H "Bu N 3 H F OH H H XIII-39-2 p-Br-Ph H H CH 3 "Bu N 3 H F OH H H XIII-39-3 p-Br-Ph H H CH(CH 3) 2 "Bu N 3 H F OH H H XIII-39-4 p-Br-Ph H H CH 2 CH(CH 3) 2 "Bu N 3 H F OH H H XIII-39-5 p-Br-Ph H H CH 2Ph "Bu N3 H F OH H H XIII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu N3 H F OH H H XIII-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu N 3 H F OH H H XIII-39-8 p-Br-Ph * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIII-40. 6 No RI R2 R 3a RIt 4 R5 R X Y R7 R XIII-40-1 p-I-Ph H H H "Bu N3 H F OH H H XIII-40-2 p-I-Ph H H CH 3 "Bu N3 H F OH H H XIII-40-3 p-I-Ph H H CH(CH 3) 2 "Bu N3 H F OH H H

No R R2 R 3 a R3 b R4 R R X Y R7 R' XIII-40-4 p-I-Ph H H CH 2CH(CH3) 2 "Bu N3 H F OH H H XIII-40-5 p-I-Ph H H CH 2Ph "Bu N3 H F OH H H XIII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu N3 H F OH H H

XIII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu N3 H F OH H H XIII-40-8 p-I-Ph * H * "Bu N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-41. No R R2 R 3a R 3b R4 R R6 X Y R7 R' XIII-41-1 CH 3 H H H Bz N3 H F OH H H XIII-41-2 CH 3 H H CH3 Bz N3 H F OH H H XIII-41-3 CH 3 H H CH(CH 3) 2 Bz N3 H F OH H H XIII-41-4 CH 3 H H CH2CH(CH 3) 2 Bz N3 H F OH H H XIII-41-5 CH 3 H H CH 2Ph Bz N3 H F OH H H XIII-41-6 CH 3 H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-41-7 CH 3 H H CH2CH 2SCH 3 Bz N3 H F OH H H XIII-41-8 CH 3 * H * Bz N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-42. No Rl R2 R3a R3b R4 R 5 R 6 X Y R7 R' XIII-42-1 Et H H H Bz N3 H F OH H H XIII-42-2 Et H H CH3 Bz N3 H F OH H H XIII-42-3 Et H H CH(CH 3) 2 Bz N3 H F OH H H XIII-42-4 Et H H CH2CH(CH 3) 2 Bz N3 H F OH H H XIII-42-5 Et H H CH 2Ph Bz N3 H F OH H H XIII-42-6 Et H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-42-7 Et H H CH2CH2SCH 3 Bz N3 H F OH H H XIII-42-8 Et * H * Bz N3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-43. No R R2 R3 a R 3b R4 R5 R6 X Y R7 R' XIII-43-1 'Pr H H H Bz N3 H F OH H H XIII-43-2 'Pr H H CH 3 Bz N3 H F OH H H XIII-43-3 'Pr H H CH(CH 3)2 Bz N3 H F OH H H XIII-43-4 Pr H H CH 2CH(CH 3) 2 Bz N3 H F OH H H XIII-43-5 Pr H H CH 2Ph Bz N3 H F OH H H XIII-43-6 Pr H H CH 2-indol-3-yl Bz N3 H F OH H H

XIII-43-7 Pr H H CH 2CH 2SCH 3 Bz N3 H F OH H H XIII-43-8 'Pr * H * Bz N3 H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-44. No R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XIII-44-1 'Bu H H H Bz N3 H F OH H H XIII-44-2 'Bu H H CH3 Bz N3 H F OH H H XIII-44-3 'Bu H H CH(CH3) 2 Bz N3 H F OH H H XIII-44-4 'Bu H H CH2CH(CH 3)2 Bz N3 H F OH H H XIII-44-5 'Bu H H CH2Ph Bz N3 H F OH H H XIII-44-6 'Bu H H CH2-indol-3-yl Bz N3 H F OH H H XIII-44-7 'Bu H H CH2CH 2SCH 3 Bz N3 H F OH H H XIII-44-8 'Bu * H * Bz N3 H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-45. 5 N RI R 2 R3 a R3 b R4 R6 X Y R7 R' XIII-45-1 Ph H H H Bz N3 H F OH H H XIII-45-2 Ph H H CH 3 Bz N3 H F OH H H XIII-45-3 Ph H H CH(CH 3) 2 Bz N3 H F OH H H XIII-45-4 Ph H H CH 2CH(CH3) 2 Bz N3 H F OH H H XIII-45-5 Ph H H CH 2Ph Bz N3 H F OH H H XIII-45-6 Ph H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-45-7 Ph H H CH 2CH2SCH 3 Bz N3 H F OH H H XIII-45-8 Ph * H * Bz N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-46. No RI1 R2 R3 a R3 b 4 R RIt R X Y R7 R XIII-46-1 p-Me-Ph H H H Bz N3 H F OH H H XIII-46-2 p-Me-Ph H H CH 3 Bz N3 H F OH H H

ISQQ

R No R R2 R 3 a R3 b R4 R X Y R7 R' XIII-46-3 p-Me-Ph H H CH(CH 3) 2 Bz N3 H F OH H H XIII-46-4 p-Me-Ph H H CH 2CH(CH3) 2 Bz N3 H F OH H H XIII-46-5 p-Me-Ph H H CH 2Ph Bz N3 H F OH H H XIII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz N3 H F OH H H XIII-46-8 p-Me-Ph * H * Bz N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-47. RI R2 R3a R 3b 4 R' R6 X Y R7 R No XIII-47-1 p-F-Ph H H H Bz N3 H F OH H H XIII-47-2 p-F-Ph H H CH3 Bz N3 H F OH H H XIII-47-3 p-F-Ph H H CH(CH3) 2 Bz N3 H F OH H H XIII-47-4 p-F-Ph H H CH2CH(CH 3) 2 Bz N3 H F OH H H XIII-47-5 p-F-Ph H H CH2Ph Bz N3 H F OH H H XIII-47-6 p-F-Ph H H CH2-indol-3-yl Bz N3 H F OH H H XIII-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz N3 H F OH H H XIII-47-8 p-F-Ph * H * Bz N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-48. RI R2 R 3 a R3 b R4 R R6 X Y R7 R' No XIII-48-1 p-Cl-Ph H H H Bz N3 H F OH H H XIII-48-2 p-Cl-Ph H H CH 3 Bz N3 H F OH H H XIII-48-3 p-Cl-Ph H H CH(CH 3)2 Bz N3 H F OH H H XIII-48-4 p-Cl-Ph H H CH 2CH(CH 3)2 Bz N3 H F OH H H XIII-48-5 p-Cl-Ph H H CH 2Ph Bz N3 H F OH H H XIII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz N3 H F OH H H XIII-48-8 p-Cl-Ph * H * Bz N3 H F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XIII-49. IR R2 R3 a R3b R4 R5 R6 X Y R7 R XIII-49-1 p-Br-Ph H H H Bz N3 H F OH H H XIII-49-2 p-Br-Ph H H CH 3 Bz N3 H F OH H H XIII-49-3 p-Br-Ph H H CH(CH 3) 2 Bz N3 H F OH H H XIII-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz N3 H F OH H H XIII-49-5 p-Br-Ph H H CH 2Ph Bz N3 H F OH H H

_So_

R RR 3 a R3 b R4 R' R' X Y R7 R' No XIII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz N3 H F OH H H XIII-49-8 p-Br-Ph * H * Bz N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIII-50. No RI R2 R3 a R3 b 4 R RIt R X Y R7 R XIII-50-1 p-I-Ph H H H Bz N3 H F OH H H XIII-50-2 p-I-Ph H H CH 3 Bz N3 H F OH H H XIII-50-3 p-I-Ph H H CH(CH 3)2 Bz N3 H F OH H H XIII-50-4 p-I-Ph H H CH 2CH(CH3) 2 Bz N3 H F OH H H XIII-50-5 p-I-Ph H H CH 2Ph Bz N3 H F OH H H XIII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz N3 H F OH H H XIII-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz N3 H F OH H H XIII-50-8 p-I-Ph * H * Bz N3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

0

R8

NH

R2 0 R3b R7 N O R3aN PNN--P- OO

OR 1 R5 R6 CO2R4

Y X

xIV

Table XIV-1. No RI R2 R3 a R3 b R4 R5 R6 X Y R7 R XIV-1-1 CH 3 H H H CH 3 N3 F H OH H H XIV-1-2 CH 3 H H CH3 CH 3 N3 F H OH H H XIV-1-3 CH 3 H H CH(CH 3) 2 CH 3 N3 F H OH H H XIV-1-4 CH 3 H H CH2CH(CH3) 2 CH 3 N3 F H OH H H XIV-1-5 CH 3 H H CH 2Ph CH 3 N3 F H OH H H XIV-1-6 CH 3 H H CH 2-indol-3-yl CH 3 N3 F H OH H H XIV-1-7 CH 3 H H CH2CH 2SCH3 CH 3 N3 F H OH H H

_ on_

R R2 R3 a R3 b R4 R R6 X Y R7 R' No XIV-1-8 CH 3 * H * CH 3 N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-2. RI R3 a R3 b R4 R' R' X Y R7 R No R2 XIV-2-1 Et H H H CH 3 N3 F H OH H H XIV-2-2 Et H H CH 3 CH 3 N3 F H OH H H XIV-2-3 Et H H CH(CH 3) 2 CH 3 N3 F H OH H H XIV-2-4 Et H H CH 2CH(CH3) 2 CH 3 N3 F H OH H H XIV-2-5 Et H H CH 2Ph CH 3 N3 F H OH H H XIV-2-6 Et H H CH 2-indol-3-yl CH 3 N3 F H OH H H XIV-2-7 Et H H CH 2CH 2SCH 3 CH 3 N3 F H OH H H XIV-2-8 Et * H * CH 3 N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'201 _

Table XIV-3. No R1 R2 R3 a R3b R4 R R6 X Y R7 R' XIV-3-1 'Pr H H H CH 3 N 3 F H OH H H XIV-3-2 'Pr H H CH 3 CH 3 N 3 F H OH H H XIV-3-3 'Pr H H CH(CH 3) 2 CH 3 N 3 F H OH H H XIV-3-4 'Pr H H CH 2CH(CH 3) 2 CH 3 N 3 F H OH H H XIV-3-5 'Pr H H CH 2Ph CH 3 N 3 F H OH H H XIV-3-6 'Pr H H CH 2-indol-3-yl CH 3 N 3 F H OH H H XIV-3-7 'Pr H H CH 2CH2SCH 3 CH 3 N 3 F H OH H H XIV-3-8 'Pr * H * CH 3 N 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-4. No R1 R2 R 3a R R4 R R6 X Y R7 R t XIV-4-1 Bu H H H CH3 N 3 F H OH H H t XIV-4-2 Bu H H CH 3 CH3 N 3 F H OH H H t XIV-4-3 Bu H H CH(CH 3)2 CH3 N 3 F H OH H H t XIV-4-4 Bu H H CH 2CH(CH 3)2 CH3 N 3 F H OH H H t XIV-4-5 Bu H H CH 2Ph CH3 N 3 F H OH H H t XIV-4-6 Bu H H CH 2-indol-3-yl CH3 N 3 F H OH H H t XIV-4-7 Bu H H CH 2CH2SCH 3 CH3 N 3 F H OH H H t XIV-4-8 Bu * H * CH3 N 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-5. No RI1 R2 R3 a R3 b R4 R5 R6 X Y R7 R XIV-5-1 Ph H H H CH 3 N 3 F H OH H H XIV-5-2 Ph H H CH3 CH3 N 3 F H OH H H XIV-5-3 Ph H H CH(CH 3) 2 CH3 N 3 F H OH H H XIV-5-4 Ph H H CH2CH(CH 3) 2 CH 3 N 3 F H OH H H XIV-5-5 Ph H H CH 2Ph CH 3 N 3 F H OH H H XIV-5-6 Ph H H CH 2-indol-3-yl CH3 N 3 F H OH H H XIV-5-7 Ph H H CH2CH 2SCH3 CH3 N 3 F H OH H H XIV-5-8 Ph * H * CH 3 N 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

10Qt)-

Table XIV-6. R' No R RR 3 a R 3b R4 R6 X Y R7 R' XIV-6-1 p-Me-Ph H H H CH 3 N 3 F H OH H H XIV-6-2 p-Me-Ph H H CH 3 CH3 N 3 F H OH H H XIV-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 N 3 F H OH H H XIV-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH 3 N 3 F H OH H H XIV-6-5 p-Me-Ph H H CH 2Ph CH 3 N 3 F H OH H H XIV-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 N 3 F H OH H H XIV-6-7 p-Me-Ph H H CH 2CH 2SCH3 CH3 N 3 F H OH H H XIV-6-8 p-Me-Ph * H * CH 3 N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-7. R' No R R2 R 3 a R3 b R4 R6 X Y R7 R' XIV-7-1 p-F-Ph H H H CH 3 N 3 F H OH H H XIV-7-2 p-F-Ph H H CH 3 CH3 N 3 F H OH H H XIV-7-3 p-F-Ph H H CH(CH 3) 2 CH3 N 3 F H OH H H XIV-7-4 p-F-Ph H H CH 2CH(CH 3) 2 CH 3 N 3 F H OH H H XIV-7-6 p-F-Ph H H CH 2Ph CH 3 N 3 F H OH H H XIV-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 N 3 F H OH H H XIV-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 N 3 F H OH H H XIV-7-20 p-F-Ph * H * CH 3 N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-8. No R R2 R 3 a R3b R4 RR X Y R7 R' XIV-8-1 p-Cl-Ph H H H CH3 N 3 F H OH H H XIV-8-2 p-Cl-Ph H H CH 3 CH3 N 3 F H OH H H XIV-8-3 p-Cl-Ph H H CH(CH 3)2 CH 3 N 3 F H OH H H XIV-8-4 p-Cl-Ph H H CH 2CH(CH 3) 2 CH 3 N 3 F H OH H H XIV-8-5 p-Cl-Ph H H CH 2Ph CH3 N 3 F H OH H H XIV-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 N 3 F H OH H H XIV-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 N 3 F H OH H H XIV-8-8 p-Cl-Ph * H * CH 3 N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

102 _

Table XIV-9. R R2 R3a R3b R4 R' R' X Y R7 R' No XIV-9-1 p-Br-Ph H H H CH 3 N 3 F H OH H H XIV-9-2 p-Br-Ph H H CH3 CH 3 N 3 F H OH H H XIV-9-3 p-Br-Ph H H CH(CH 3)2 CH 3 N 3 F H OH H H XIV-9-4 p-Br-Ph H H CH2CH(CH 3)2 CH 3 N 3 F H OH H H XIV-9-6 p-Br-Ph H H CH 2Ph CH 3 N 3 F H OH H H XIV-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 N 3 F H OH H H XIV-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 N 3 F H OH H H XIV-9-20 p-Br-Ph * H * CH 3 N 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-10. N R I R2 R3a R3b R4 R'R6 X Y R7 R' XIV-10-1 p-I-Ph H H H CH 3 N 3 F H OH H H XIV-10-2 p-I-Ph H H CH 3 CH 3 N 3 F H OH H H XIV-10-3 p-I-Ph H H CH(CH 3)2 CH 3 N 3 F H OH H H XIV-10-4 p-I-Ph H H CH 2CH(CH 3)2 CH 3 N 3 F H OH H H XIV-10-5 p-I-Ph H H CH 2Ph CH 3 N 3 F H OH H H XIV-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 N 3 F H OH H H XIV-10-7 p-I-Ph H H CH 2CH2SCH 3 CH 3 N 3 F H OH H H XIV-10-8 p-I-Ph * H * CH 3 N 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-11. No RI 1 R2 R 3a R3b R4 R5 R6 X Y R7 R XIV-11-1 CH 3 H H H Et N3 F H OH H H XIV-11-2 CH 3 H H CH3 Et N3 F H OH H H XIV-11-3 CH 3 H H CH(CH 3)2 Et N3 F H OH H H XIV-11-4 CH 3 H H CH2CH(CH 3)2 Et N3 F H OH H H XIV-11-5 CH 3 H H CH 2Ph Et N3 F H OH H H XIV-11-6 CH 3 H H CH 2-indol-3-yl Et N3 F H OH H H XIV-11-7 CH 3 H H CH2CH 2SCH 3 Et N3 F H OH H H XIV-11-8 CH 3 * H * Et N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Io _A

Table XIV-12. R1 R2 R 3a R3b R4 R R' X Y R7 R' No XIV-12-1 Et H H H Et N3 F H OH H H XIV-12-2 Et H H CH3 Et N3 F H OH H H XIV-12-3 Et H H CH(CH 3) 2 Et N3 F H OH H H XIV-12-4 Et H H CH2CH(CH 3)2 Et N3 F H OH H H XIV-12-5 Et H H CH 2Ph Et N3 F H OH H H XIV-12-6 Et H H CH 2-indol-3-yl Et N3 F H OH H H XIV-12-7 Et H H CH2CH 2SCH 3 Et N3 F H OH H H XIV-12-8 Et * H * Et N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-13. No R' R2 R 3a R3 b R4 R R6 X Y R7 R' XIV-13-1 'Pr H H H Et N3 F H OH H H XIV-13-2 'Pr H H CH 3 Et N3 F H OH H H XIV-13-3 'Pr H H CH(CH 3)2 Et N3 F H OH H H XIV-13-4 'Pr H H CH 2CH(CH 3)2 Et N3 F H OH H H XIV-13-5 'Pr H H CH 2Ph Et N3 F H OH H H XIV-13-6 'Pr H H CH 2-indol-3-yl Et N3 F H OH H H XIV-13-7 'Pr H H CH 2CH2SCH 3 Et N3 F H OH H H XIV-13-8 'Pr * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-14. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R t XIV-14-1 Bu H H H Et N3 F H OH H H t XIV-14-2 Bu H H CH 3 Et N3 F H OH H H t XIV-14-3 Bu H H CH(CH 3) 2 Et N3 F H OH H H t XIV-14-4 Bu H H CH 2CH(CH 3) 2 Et N3 F H OH H H t XIV-14-5 Bu H H CH 2Ph Et N3 F H OH H H t XIV-14-6 Bu H H CH 2-indol-3-yl Et N3 F H OH H H t XIV-14-7 Bu H H CH 2CH2SCH 3 Et N3 F H OH H H t XIV-14-8 Bu * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

,)Or,-

Table XIV-15. No R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' XIV-15-1 Ph H H H Et N3 F H OH H H XIV-15-2 Ph H H CH3 Et N3 F H OH H H XIV-15-3 Ph H H CH(CH 3)2 Et N3 F H OH H H XIV-15-4 Ph H H CH2CH(CH 3) 2 Et N3 F H OH H H XIV-15-5 Ph H H CH 2Ph Et N3 F H OH H H XIV-15-6 Ph H H CH 2-indol-3-yl Et N3 F H OH H H XIV-15-7 Ph H H CH2CH2SCH 3 Et N3 F H OH H H XIV-15-8 Ph * H * Et N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-16. N9 R1 R2 R 3a R3 b R4 R5 R' X Y R7 R XIV-16-1 p-Me-Ph H H H Et N3 F H OH H H XIV-16-2 p-Me-Ph H H CH 3 Et N3 F H OH H H XIV-16-3 p-Me-Ph H H CH(CH 3)2 Et N3 F H OH H H XIV-16-4 p-Me-Ph H H CH 2CH(CH 3)2 Et N3 F H OH H H XIV-16-5 p-Me-Ph H H CH 2Ph Et N3 F H OH H H XIV-16-6 p-Me-Ph H H CH 2-indol-3-yl Et N3 F H OH H H XIV-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et N3 F H OH H H XIV-16-8 p-Me-Ph * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-17. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' XIV-17-1 p-F-Ph H H H Et N3 F H OH H H XIV-17-2 p-F-Ph H H CH 3 Et N3 F H OH H H XIV-17-3 p-F-Ph H H CH(CH 3) 2 Et N3 F H OH H H XIV-17-4 p-F-Ph H H CH 2CH(CH 3) 2 Et N3 F H OH H H XIV-17-5 p-F-Ph H H CH 2Ph Et N3 F H OH H H XIV-17-6 p-F-Ph H H CH 2-indol-3-yl Et N3 F H OH H H XIV-17-7 p-F-Ph H H CH 2CH2SCH 3 Et N3 F H OH H H XIV-17-8 p-F-Ph * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

,)Or,-

Table XIV-18. No R R2 R 3 a R 3b R 4 R R X Y R7 R' XIV-18-1 p-Cl-Ph H H H Et N3 F H OH H H XIV-18-2 p-Cl-Ph H H CH 3 Et N3 F H OH H H XIV-18-3 p-Cl-Ph H H CH(CH3) 2 Et N3 F H OH H H XIV-18-4 p-Cl-Ph H H CH 2CH(CH 3) 2 Et N3 F H OH H H XIV-18-5 p-Cl-Ph H H CH 2Ph Et N3 F H OH H H XIV-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et N3 F H OH H H XIV-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et N3 F H OH H H XIV-18-8 p-Cl-Ph * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-19. N9 R1 R 2 R 3a R3 b R4 R R6 X Y R7 R' XIV-19-1 p-Br-Ph H H H Et N3 F H OH H H XIV-19-2 p-Br-Ph H H CH3 Et N3 F H OH H H XIV-19-3 p-Br-Ph H H CH(CH 3)2 Et N3 F H OH H H XIV-19-4 p-Br-Ph H H CH2CH(CH 3)2 Et N3 F H OH H H XIV-19-5 p-Br-Ph H H CH 2Ph Et N3 F H OH H H XIV-19-6 p-Br-Ph H H CH 2-indol-3-yl Et N3 F H OH H H XIV-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et N3 F H OH H H XIV-19-8 p-Br-Ph * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-20. No R R2 R 3 a R 3b R4 R5 R6 X Y R7 R' XIV-20-1 p-I-Ph H H H Et N3 F H OH H H XIV-20-2 p-I-Ph H H CH 3 Et N3 F H OH H H XIV-20-3 p-I-Ph H H CH(CH 3)2 Et N3 F H OH H H XIV-20-4 p-I-Ph H H CH 2CH(CH 3) 2 Et N3 F H OH H H XIV-20-5 p-I-Ph H H CH 2Ph Et N3 F H OH H H XIV-20-6 p-I-Ph H H CH 2-indol-3-yl Et N3 F H OH H H XIV-20-7 p-I-Ph H H CH 2CH2SCH 3 Et N3 F H OH H H XIV-20-8 p-I-Ph * H * Et N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

')o,

Table XIV-21. R1 R2 R 3a R3b R4 R' R' X Y R7 R' No XIV-21-1 CH 3 H H H 1Pr N3 F H OH H H XIV-21-2 CH 3 H H CH3 1Pr N3 F H OH H H XIV-21-3 CH 3 H H CH(CH 3)2 1Pr N3 F H OH H H XIV-21-4 CH 3 H H CH2CH(CH 3)2 1Pr N3 F H OH H H XIV-21-5 CH 3 H H CH 2Ph 1Pr N3 F H OH H H XIV-21-6 CH 3 H H CH 2-indol-3-yl 1Pr N3 F H OH H H XIV-21-7 CH 3 H H CH2CH 2SCH 3 1Pr N3 F H OH H H XIV-21-8 CH 3 * H * 1Pr N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-22. N R1 R2 R 3a R3 b R4 R' R6 X Y R7 R XIV-22-1 Et H H H 1Pr N3 F H OH H H XIV-22-2 Et H H CH3 1Pr N3 F H OH H H XIV-22-3 Et H H CH(CH 3) 2 1Pr N3 F H OH H H XIV-22-4 Et H H CH2CH(CH 3)2 1Pr N3 F H OH H H XIV-22-5 Et H H CH 2Ph 1Pr N3 F H OH H H Et H H CH 2-indol-3-yl 1Pr F H OH H H XIV-22-6 N3 XIV-22-7 Et H H CH2CH 2SCH 3 1Pr N3 F H OH H H XIV-22-8 Et * H * 1Pr N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-23. RI' R 2 R 3 a 4 R5 R 6 X Y R7 R No R3b

XIV-23-1 'Pr H H H 'Pr N3 F H OH H H XIV-23-2 'Pr H H CH 3 1Pr N3 F H OH H H XIV-23-3 'Pr H H CH(CH 3)2 1Pr N3 F H OH H H XIV-23-4 'Pr H H CH 2CH(CH 3)2 1Pr N3 F H OH H H XIV-23-5 'Pr H H CH 2Ph 1Pr N3 F H OH H H XIV-23-6 'Pr H H CH 2-indol-3-yl 1Pr N3 F H OH H H XIV-23-7 'Pr H H CH 2CH2SCH 3 1Pr N3 F H OH H H XIV-23-8 'Pr * H * 1Pr N3 F H OH H H *R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

IOoQ_

Table XIV-24. No RI R2 RaR 3 b R4 R R X Y R7 R' t XIV-24-1 Bu H H H 'Pr N 3 F H OH H H t XIV-24-2 Bu H H CH 3 'Pr N 3 F H OH H H t XIV-24-3 Bu H H CH(CH 3) 2 'Pr N 3 F H OH H H t XIV-24-4 Bu H H CH 2CH(CH3) 2 'Pr N 3 F H OH H H t XIV-24-5 Bu H H CH 2Ph 'Pr N 3 F H OH H H t XIV-24-6 Bu H H CH 2-indol-3-yl 'Pr N 3 F H OH H H t XIV-24-7 Bu H H CH 2CH2SCH 3 'Pr N 3 F H OH H H t XIV-24-8 Bu * H * 'Pr N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-25. No R1 R2 R 3a R3 b R4 R5 R 6 X Y R7 R' XIV-25-1 Ph H H H 'Pr N3 F H OH H H XIV-25-2 Ph H H CH3 'Pr N3 F H OH H H XIV-25-3 Ph H H CH(CH 3)2 'Pr N3 F H OH H H XIV-25-4 Ph H H CH2CH(CH 3) 2 'Pr N3 F H OH H H XIV-25-5 Ph H H CH 2Ph 'Pr N3 F H OH H H XIV-25-6 Ph H H CH 2-indol-3-yl 'Pr N3 F H OH H H XIV-25-7 Ph H H CH2CH2SCH 3 'Pr N3 F H OH H H XIV-25-8 Ph * H * 'Pr N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-26. N9 R1 R 2 R 3a R 3b R4 R5 R 6 X Y R7 R' XIV-26-1 p-Me-Ph H H H 'Pr N3 F H OH H H XIV-26-2 p-Me-Ph H H CH 3 'Pr N3 F H OH H H XIV-26-3 p-Me-Ph H H CH(CH 3)2 'Pr N3 F H OH H H XIV-26-4 p-Me-Ph H H CH 2CH(CH 3) 2 'Pr N3 F H OH H H XIV-26-5 p-Me-Ph H H CH 2Ph 'Pr N3 F H OH H H XIV-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr N3 F H OH H H XIV-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr N3 F H OH H H XIV-26-8 p-Me-Ph * H * 'Pr N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

1oo

Table XIV-27. R RR 3 R3b R4 R' R6 X Y R7 R' No a

XIV-27-1 p-F-Ph H H H 1Pr N3 F H OH H H XIV-27-2 p-F-Ph H H CH 3 1Pr N3 F H OH H H XIV-27-3 p-F-Ph H H CH(CH 3) 2 1Pr N3 F H OH H H XIV-27-4 p-F-Ph H H CH 2CH(CH 3) 2 1Pr N3 F H OH H H XIV-27-5 p-F-Ph H H CH 2Ph 1Pr N3 F H OH H H XIV-27-6 p-F-Ph H H CH 2-indol-3-yl 1Pr N3 F H OH H H XIV-27-7 p-F-Ph H H CH 2CH2SCH 3 1Pr N3 F H OH H H XIV-27-8 p-F-Ph * H * 1Pr N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-28. No RI R2 R 3a R3 b 4 R R 6 X Y R7 R' XIV-28-1 p-Cl-Ph H H H 'Pr N 3 F H OH H H XIV-28-2 p-Cl-Ph H H CH 3 1Pr N3 F H OH H H XIV-28-3 p-Cl-Ph H H CH(CH3) 2 1Pr N3 F H OH H H p-Cl-Ph H H CH 2CH(CH 3)2 1Pr F H OH H H XIV-28-4 N3 XIV-28-5 p-Cl-Ph H H CH 2Ph 1Pr N3 F H OH H H p-Cl-Ph H H CH 2-indol-3-yl 1Pr F H OH H H XIV-28-6 N3 XIV-28-7 p-Cl-Ph H H CH 2CH2SCH 3 1Pr N3 F H OH H H XIV-28-8 p-Cl-Ph * H * Pr N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-29. N R R2 R 3 a R3b R4 R5 R6 X Y R7 R XIV-29-1 p-Br-Ph H H H 1Pr N3 F H OH H H XIV-29-2 p-Br-Ph H H CH3 1Pr N3 F H OH H H XIV-29-3 p-Br-Ph H H CH(CH 3)2 1Pr N3 F H OH H H XIV-29-4 p-Br-Ph H H CH2CH(CH 3)2 1Pr N3 F H OH H H XIV-29-5 p-Br-Ph H H CH 2Ph 1Pr N3 F H OH H H XIV-29-6 p-Br-Ph H H CH 2-indol-3-yl 1Pr N3 F H OH H H XIV-29-7 p-Br-Ph H H CH2CH 2SCH 3 1Pr N3 F H OH H H XIV-29-8 p-Br-Ph * H * 'Pr N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-30. R RR 3 R3b R4 R R6 X Y R7 R' No a

XIV-30-1 p-I-Ph H H H 'Pr N3 F H OH H H XIV-30-2 p-I-Ph H H CH 3 'Pr N3 F H OH H H XIV-30-3 p-I-Ph H H CH(CH 3)2 'Pr N3 F H OH H H XIV-30-4 p-I-Ph H H CH 2CH(CH 3) 2 'Pr N3 F H OH H H XIV-30-5 p-I-Ph H H CH 2Ph 'Pr N3 F H OH H H XIV-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr N3 F H OH H H XIV-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr N3 F H OH H H XIV-30-8 p-I-Ph * H * 'Pr N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-31. No R1 R2 R3a 3 Rb R4 R' R6 X Y R7 R' XIV-31-1 CH 3 H H H "Bu N3 F H OH H H XIV-31-2 CH 3 H H CH3 "Bu N 3 F H OH H H XIV-31-3 CH 3 H H CH(CH 3)2 "Bu N 3 F H OH H H XIV-31-4 CH 3 H H CH2CH(CH 3)2 "Bu N3 F H OH H H XIV-31-5 CH 3 H H CH 2Ph "Bu N3 F H OH H H XIV-31-6 CH 3 H H CH 2-indol-3-yl "Bu N3 F H OH H H XIV-31-7 CH 3 H H CH2CH 2SCH 3 "Bu N3 F H OH H H XIV-31-8 CH 3 * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-32. No RI 1 R2 R 3a R3b R4 R5 R6 X Y R7 R

XIV-32-1 Et H H H "Bu N3 F H OH H H XIV-32-2 Et H H CH3 "Bu N3 F H OH H H XIV-32-3 Et H H CH(CH 3) 2 "Bu N3 F H OH H H XIV-32-4 Et H H CH2CH(CH 3)2 "Bu N3 F H OH H H XIV-32-5 Et H H CH 2Ph "Bu N3 F H OH H H XIV-32-6 Et H H CH 2-indol-3-yl "Bu N3 F H OH H H

XIV-32-7 Et H H CH2CH 2SCH 3 "Bu N3 F H OH H H XIV-32-8 Et * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'2l _

Table XIV-33. 3 R' 6 No R' R2 R3 aR R4 R X Y R7 R' XIV-33-1 'Pr H H H "Bu N3 F H OH H H XIV-33-2 'Pr H H CH 3 "Bu N 3 F H OH H H XIV-33-3 'Pr H H CH(CH 3)2 "Bu N 3 F H OH H H XIV-33-4 'Pr H H CH 2CH(CH 3)2 "Bu N3 F H OH H H XIV-33-5 'Pr H H CH 2Ph "Bu N3 F H OH H H XIV-33-6 'Pr H H CH 2-indol-3-yl "Bu N3 F H OH H H XIV-33-7 'Pr H H CH 2 CH2 SCH 3 "Bu N3 F H OH H H XIV-33-8 'Pr * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-34. No R1 R2 R3 a 3 Rb R4 R R X Y R7 R t XIV-34-1 Bu H H H "Bu N3 F H OH H H t XIV-34-2 Bu H H CH 3 "Bu N 3 F H OH H H t XIV-34-3 Bu H H CH(CH 3) 2 "Bu N 3 F H OH H H t XIV-34-4 Bu H H CH 2 CH(CH3 )2 "Bu N3 F H OH H H t XIV-34-5 Bu H H CH 2Ph "Bu N3 F H OH H H t XIV-34-6 Bu H H CH 2-indol-3-yl "Bu N3 F H OH H H t XIV-34-7 Bu H H CH 2 CH2SCH 3 "Bu N3 F H OH H H t XIV-34-8 Bu * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-35. No RI 1 R2 R 3a R3 b R4 R5 R6 X Y R7 R

XIV-35-1 Ph H H H "Bu N3 F H OH H H XIV-35-2 Ph H H CH3 "Bu N3 F H OH H H XIV-35-3 Ph H H CH(CH 3 )2 "Bu N3 F H OH H H XIV-35-4 Ph H H CH2 CH(CH 3) 2 "Bu N3 F H OH H H XIV-35-5 Ph H H CH 2 Ph "Bu N3 F H OH H H XIV-35-6 Ph H H CH 2-indol-3-yl "Bu N3 F H OH H H XIV-35-7 Ph H H CH2 CH2 SCH 3 "Bu N3 F H OH H H XIV-35-8 Ph * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

In')-

Table XIV-36. No R RR 3 a R3b R4 R' R6 X Y R7 R' XIV-36-1 p-Me-Ph H H H "Bu N 3 F H OH H H XIV-36-2 p-Me-Ph H H CH 3 "Bu N 3 F H OH H H XIV-36-3 p-Me-Ph H H CH(CH 3)2 "Bu N 3 F H OH H H XIV-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu N 3 F H OH H H XIV-36-5 p-Me-Ph H H CH 2Ph "Bu N3 F H OH H H XIV-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu N3 F H OH H H XIV-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu N3 F H OH H H XIV-36-8 p-Me-Ph * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-37. No R R 2 R 3a R3 b R4 R' R6 X Y R7 R' XIV-37-1 p-F-Ph H H H "Bu N3 F H OH H H XIV-37-2 p-F-Ph H H CH 3 "Bu N 3 F H OH H H XIV-37-3 p-F-Ph H H CH(CH 3) 2 "Bu N 3 F H OH H H XIV-37-4 p-F-Ph H H CH 2 CH(CH 3) 2 "Bu N3 F H OH H H

XIV-37-5 p-F-Ph H H CH 2Ph "Bu N3 F H OH H H

XIV-37-6 p-F-Ph H H CH 2 -indol-3-yl "Bu N3 F H OH H H

XIV-37-7 p-F-Ph H H CH 2 CH 2 SCH 3 "Bu N3 F H OH H H

XIV-37-8 p-F-Ph * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-38. No R1 R2 R 3a R 3b R4 R R X Y R7 R' XIV-38-1 p-Cl-Ph H H H "Bu N 3 F H OH H H XIV-38-2 p-Cl-Ph H H CH 3 "Bu N 3 F H OH H H

XIV-38-3 p-Cl-Ph H H CH(CH3 ) 2 "Bu N 3 F H OH H H

XIV-38-4 p-Cl-Ph H H CH 2CH(CH 3 ) 2 "Bu N 3 F H OH H H

XIV-38-5 p-Cl-Ph H H CH 2Ph "Bu N 3 F H OH H H

XIV-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu N 3 F H OH H H XIV-38-7 p-Cl-Ph H H CH 2CH 2 SCH 3 "Bu N 3 F H OH H H

XIV-38-8 p-Cl-Ph * H * "Bu N 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-39. No R R2 R 3a R3 b R4 R5 R6 X Y R7 R' XIV-39-1 p-Br-Ph H H H "Bu N3 F H OH H H XIV-39-2 p-Br-Ph H H CH 3 "Bu N3 F H OH H H XIV-39-3 p-Br-Ph H H CH(CH 3 )2 "Bu N3 F H OH H H

'In'-

R R2 R 3 R3 b R4 R' R' X Y R7 R' No a

XIV-39-4 p-Br-Ph H H CH 2CH(CH 3)2 "Bu N3 F H OH H H XIV-39-5 p-Br-Ph H H CH 2Ph "Bu N3 F H OH H H XIV-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu N3 F H OH H H

XIV-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu N3 F H OH H H

XIV-39-8 p-Br-Ph * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-40. No RI R2 R 3a R3 b R4 R' R6 X Y R7 R

XIV-40-1 p-I-Ph H H H "Bu N3 F H OH H H XIV-40-2 p-I-Ph H H CH 3 "Bu N3 F H OH H H XIV-40-3 p-I-Ph H H CH(CH 3)2 "Bu N3 F H OH H H XIV-40-4 p-I-Ph H H CH 2CH(CH 3) 2 "Bu N3 F H OH H H XIV-40-5 p-I-Ph H H CH 2Ph "Bu N3 F H OH H H XIV-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu N3 F H OH H H XIV-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu N3 F H OH H H XIV-40-8 p-I-Ph * H * "Bu N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-41. 1 R R 2 R3a R3b R4 R R6X Y R7 R'

XIV-41-1 CH 3 H H H Bz N3 F H OH H H XIV-41-2 CH 3 H H CH3 Bz N3 F H OH H H XIV-41-3 CH 3 H H CH(CH 3)2 Bz N3 F H OH H H XIV-41-4 CH 3 H H CH2CH(CH 3)2 Bz N3 F H OH H H XIV-41-5 CH 3 H H CH 2Ph Bz N3 F H OH H H XIV-41-6 CH 3 H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-41-7 CH 3 H H CH2CH 2SCH 3 Bz N3 F H OH H H XIV-41-8 CH 3 * H * Bz N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

210A-

Table XIV-42. No R R2 R 3a R3b R4 R R6 X Y R7 R' XIV-42-1 Et H H H Bz N3 F H OH H H XIV-42-2 Et H H CH3 Bz N3 F H OH H H XIV-42-3 Et H H CH(CH 3) 2 Bz N3 F H OH H H XIV-42-4 Et H H CH2CH(CH 3)2 Bz N3 F H OH H H XIV-42-5 Et H H CH 2Ph Bz N3 F H OH H H XIV-42-6 Et H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-42-7 Et H H CH2CH 2SCH 3 Bz N3 F H OH H H XIV-42-8 Et * H * Bz N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-43. M R' R2 R 3a R3 b R4 R6 X Y R7 R' XIV-43-1 'Pr H H H Bz N3 F H OH H H XIV-43-2 'Pr H H CH 3 Bz N3 F H OH H A XIV-43-3 'Pr H H CH(CH 3)2 Bz N3 F H OH H H XIV-43-4 'Pr H H CH 2CH(CH 3)2 Bz N3 F H OH H H XIV-43-5 'Pr H H CH 2Ph Bz N3 F H OH H H XIV-43-6 'Pr H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-43-7 'Pr H H CH 2CH2SCH 3 Bz N3 F H OH H H XIV-43-8 'Pr * H * Bz N3 F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-44. RI R2 R3 a R3 b 4 R' R6 X Y R7 R NoI t XIV-44-1 Bu H H H Bz N3 F H OH H H t XIV-44-2 Bu H H CH 3 Bz N3 F H OH H H t F H OH H H XIV-44-3 Bu H H CH(CH 3) 2 Bz N3 t OH H H XIV-44-4 Bu H H CH 2CH(CH3)2 Bz N3 F H t F H OH H H XIV-44-5 Bu H H CH 2Ph Bz N3 t XIV-44-6 Bu H H CH 2-indol-3-yl Bz N3 F H OH H H t XIV-44-7 Bu H H CH 2CH2SCH 3 Bz N3 F H OH H H t XIV-44-8 Bu * H * Bz N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-45. No R1 R2 R 3a R3b R4 R5 R' X Y R7 R' XIV-45-1 Ph H H H Bz N3 F H OH H H XIV-45-2 Ph H H CH3 Bz N3 F H OH H H XIV-45-3 Ph H H CH(CH 3)2 Bz N3 F H OH H H XIV-45-4 Ph H H CH2CH(CH 3) 2 Bz N3 F H OH H H XIV-45-5 Ph H H CH 2Ph Bz N3 F H OH H H XIV-45-6 Ph H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-45-7 Ph H H CH2CH2SCH 3 Bz N3 F H OH H H XIV-45-8 Ph * H * Bz N3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-46. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' XIV-46-1 p-Me-Ph H H H Bz N3 F H OH H H XIV-46-2 p-Me-Ph H H CH 3 Bz N3 F H OH H H XIV-46-3 p-Me-Ph H H CH(CH 3)2 Bz N3 F H OH H H XIV-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz N3 F H OH H H XIV-46-5 p-Me-Ph H H CH 2Ph Bz N3 F H OH H H XIV-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz N3 F H OH H H XIV-46-8 p-Me-Ph * H * Bz N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIV-47. No RI 1 R2 R3 a R3 b R4 R5 R6 X Y R7 R XIV-47-1 p-F-Ph H H H Bz N3 F H OH H H XIV-47-2 p-F-Ph H H CH 3 Bz N3 F H OH H H XIV-47-3 p-F-Ph H H CH(CH 3) 2 Bz N3 F H OH H H XIV-47-4 p-F-Ph H H CH 2CH(CH 3) 2 Bz N3 F H OH H H XIV-47-5 p-F-Ph H H CH 2Ph Bz N3 F H OH H H XIV-47-6 p-F-Ph H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz N3 F H OH H H XIV-47-8 p-F-Ph * H * Bz N3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2C1A-

Table XIV-48. No R R2 R 3 a R 3b R4 R6 X Y R7 R' XIV-48-1 p-Cl-Ph H H H Bz N 3 F H OH H H XIV-48-2 p-Cl-Ph H H CH 3 Bz N 3 F H OH H H XIV-48-3 p-Cl-Ph H H CH(CH3)2 Bz N 3 F H OH H H XIV-48-4 p-Cl-Ph H H CH 2CH(CH 3) 2 Bz N 3 F H OH H H XIV-48-5 p-Cl-Ph H H CH 2Ph Bz N 3 F H OH H H XIV-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz N 3 F H OH H H XIV-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz N 3 F H OH H H XIV-48-8 p-Cl-Ph * H * Bz N3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-49. N R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' XIV-49-1 p-Br-Ph H H H Bz N3 F H OH H H XIV-49-2 p-Br-Ph H H CH3 Bz N3 F H OH H H XIV-49-3 p-Br-Ph H H CH(CH 3)2 Bz N3 F H OH H H XIV-49-4 p-Br-Ph H H CH2CH(CH 3)2 Bz N3 F H OH H H XIV-49-5 p-Br-Ph H H CH 2Ph Bz N3 F H OH H H XIV-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz N3 F H OH H H XIV-49-8 p-Br-Ph * H * Bz N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIV-50. No RI 1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XIV-50-1 p-I-Ph H H H Bz N3 F H OH H H XIV-50-2 p-I-Ph H H CH 3 Bz N3 F H OH H H XIV-50-3 p-I-Ph H H CH(CH 3)2 Bz N3 F H OH H H XIV-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz N3 F H OH H H XIV-50-5 p-I-Ph H H CH 2Ph Bz N3 F H OH H H XIV-50-6 p-I-Ph H H CH 2-indol-3-yl Bz N3 F H OH H H XIV-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz N3 F H OH H H XIV-50-8 p-I-Ph * H * Bz N3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'IW7-

R8 NH

R2 0 R3b R R 0 3a 0 N

C0 2R 4 ORR6

Y X

xv Table XV-1. No R1 R2 R3a R 3b R4 R R6 X Y R7 R' XV-1-1 CH3 H H H CH 3 F F H OH H H XV-1-2 CH3 H H CH3 CH 3 F F H OH H H XV-1-3 CH3 H H CH(CH3) 2 CH 3 F F H OH H H XV-1-4 CH3 H H CH2CH(CH 3) 2 CH 3 F F H OH H H XV-1-5 CH3 H H CH2Ph CH 3 F F H OH H H XV-1-6 CH3 H H CH2-indol-3-yl CH 3 F F H OH H H XV-1-7 CH3 H H CH2CH2SCH 3 CH 3 F F H OH H H XV-1-8 CH3 * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-2. N9 R1 R2 R 3 a R3 b R4 R R6 X Y R7 R' XV-2-1 Et H H H CH 3 F F H OH H H XV-2-2 Et H H CH 3 CH 3 F F H OH H H XV-2-3 Et H H CH(CH 3) 2 CH 3 F F H OH H H XV-2-4 Et H H CH 2CH(CH 3) 2 CH 3 F F H OH H H XV-2-5 Et H H CH 2Ph CH 3 F F H OH H H XV-2-6 Et H H CH 2-indol-3-yl CH 3 F F H OH H H XV-2-7 Et H H CH 2CH 2SCH 3 CH 3 F F H OH H H XV-2-8 Et * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-3. N9 R1 R2 R3 a R 3b R4 R 5 R6 X Y R7 R' XV-3-1 'Pr H H H CH 3 F F H OH H H XV-3-2 'Pr H H CH3 CH3 F F H OH H H XV-3-3 'Pr H H CH(CH3)2 CH3 F F H OH H H XV-3-4 Pr H H CH2CH(CH3) 2 CH3 F F H OH H H XV-3-5 Pr H H CH 2Ph CH 3 F F H OH H H XV-3-6 Pr H H CH 2-indol-3-yl CH3 F F H OH H H XV-3-7 Pr H H CH2CH2 SCH3 CH3 F F H OH H H XV-3-8 Pr * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-4. N9 R1 R2 R3a R3 R4 R6 X Y R7 R' XV-4-1 'Bu H H H CH 3 F F H OH H H XV-4-2 'Bu H H CH3 CH3 F F H OH H H XV-4-3 'Bu H H CH(CH3)2 CH3 F F H OH H H XV-4-4 'Bu H H CH2CH(CH3) 2 CH3 F F H OH H H XV-4-5 'Bu H H CH 2Ph CH 3 F F H OH H H XV-4-6 'Bu H H CH 2-indol-3-yl CH3 F F H OH H H XV-4-7 'Bu H H CH2CH 2SCH 3 CH3 F F H OH H H XV-4-8 'Bu * H * CH 3 F F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-5. N9 R1 R2 R 3 a R 3b R4 R 5 R6 X Y R7 R' XV-5-1 Ph H H H CH3 F F H OH H H XV-5-2 Ph H H CH3 CH3 F F H OH H H XV-5-3 Ph H H CH(CH3) 2 CH3 F F H OH H H XV-5-4 Ph H H CH2CH(CH3) 2 CH3 F F H OH H H XV-5-5 Ph H H CH2Ph CH3 F F H OH H H XV-5-6 Ph H H CH2-indol-3-yl CH3 F F H OH H H XV-5-7 Ph H H CH2CH 2SCH 3 CH3 F F H OH H H XV-5-8 Ph * H * CH 3 F F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

_2ano-

Table XV-6. N9 R1 R2 R 3 R3 b R4 R' R6 X Y R7 R' XV-6-1 p-Me-Ph H H H CH3 F F H OH H H XV-6-2 p-Me-Ph H H CH3 CH3 F F H OH H H XV-6-3 p-Me-Ph H H CH(CH3) 2 CH3 F F H OH H H XV-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 F F H OH H H XV-6-5 p-Me-Ph H H CH 2Ph CH3 F F H OH H H XV-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 F F H OH H H XV-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 F F H OH H H XV-6-8 p-Me-Ph * H * CH3 F F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-7. No R R2 R 3 a R3 b R4 R' R6 X Y R7 R' XV-7-1 p-F-Ph H H H CH3 F F H OH H H XV-7-2 p-F-Ph H H CH3 CH3 F F H OH H H XV-7-3 p-F-Ph H H CH(CH3)2 CH3 F F H OH H H XV-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 F F H OH H H XV-7-6 p-F-Ph H H CH 2Ph CH3 F F H OH H H XV-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 F F H OH H H XV-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 F F H OH H H XV-7-20 p-F-Ph * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-8. N9 R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' XV-8-1 p-Cl-Ph H H H CH 3 F F H OH H H XV-8-2 p-Cl-Ph H H CH 3 CH3 F F H OH H H XV-8-3 p-Cl-Ph H H CH(CH3) 2 CH3 F F H OH H H XV-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 F F H OH H H XV-8-5 p-Cl-Ph H H CH 2Ph CH 3 F F H OH H H XV-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 F F H OH H H XV-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH3 F F H OH H H XV-8-8 p-Cl-Ph * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'21fl-_

Table XV-9. No R R2 R3a R3b R4 R R X Y R7 R' XV-9-1 p-Br-Ph H H H CH3 F F H OH H H XV-9-2 p-Br-Ph H H CH 3 CH3 F F H OH H H XV-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 F F H OH H H XV-9-4 p-Br-Ph H H CH 2CH(CH 3) 2 CH 3 F F H OH H H XV-9-6 p-Br-Ph H H CH 2Ph CH3 F F H OH H H XV-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 F F H OH H H XV-9-8 p-Br-Ph H H CH 2CH2SCH 3 CH 3 F F H OH H H XV-9-20 p-Br-Ph * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-10. No R R2 R 3 a R3 b R4 R' R6 X Y R7 R' XV-10-1 p-I-Ph H H H CH3 F F H OH H H XV-10-2 p-I-Ph H H CH3 CH3 F F H OH H H XV-10-3 p-I-Ph H H CH(CH3)2 CH3 F F H OH H H XV-10-4 p-I-Ph H H CH2CH(CH3) 2 CH3 F F H OH H H XV-10-5 p-I-Ph H H CH 2Ph CH3 F F H OH H H XV-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 F F H OH H H XV-10-7 p-I-Ph H H CH2CH 2SCH 3 CH3 F F H OH H H XV-10-8 p-I-Ph * H * CH 3 F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-11. No R1 R2 R3 a R3b R 4 R5 R6 X Y R7 R' XV-11-1 CH3 H H H Et F F H OH H H XV-11-2 CH3 H H CH 3 Et F F H OH H H XV-11-3 CH3 H H CH(CH3) 2 Et F F H OH H H XV-11-4 CH3 H H CH 2CH(CH3)2 Et F F H OH H H XV-11-5 CH3 H H CH 2Ph Et F F H OH H H XV-11-6 CH3 H H CH 2-indol-3-yl Et F F H OH H H XV-11-7 CH3 H H CH 2CH2SCH 3 Et F F H OH H H XV-11-8 CH3 * H * Et F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Ill

Table XV-12. No Rl R 2 R3 a R3b R4 R 5 R' X Y R7 R' XV-12-1 Et H H H Et F F H OH H H XV-12-2 Et H H CH 3 Et F F H OH H H XV-12-3 Et H H CH(CH3) 2 Et F F H OH H H XV-12-4 Et H H CH 2CH(CH3) 2 Et F F H OH H H XV-12-5 Et H H CH 2Ph Et F F H OH H H XV-12-6 Et H H CH 2-indol-3-yl Et F F H OH H H XV-12-7 Et H H CH 2CH 2SCH 3 Et F F H OH H H XV-12-8 Et * H * Et F F H OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XV-13. No R1 R2 R 3a R3 b R4 R' R6 X Y R7 R' XV-13-1 'Pr H H H Et F F H OH H H XV-13-2 'Pr H H CH3 Et F F H OH H H XV-13-3 'Pr H H CH(CH3)2 Et F F H OH H H XV-13-4 'Pr H H CH2CH(CH3) 2 Et F F H OH H H XV-13-5 'Pr H H CH 2Ph Et F F H OH H H XV-13-6 'Pr H H CH 2-indol-3-yl Et F F H OH H H XV-13-7 'Pr H H CH2CH 2SCH 3 Et F F H OH H H XV-13-8 'Pr * H * Et F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-14. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R XV-14-1 'Bu H H H Et F F H OH H H XV-14-2 'Bu H H CH 3 Et F F H OH H H XV-14-3 'Bu H H CH(CH3) 2 Et F F H OH H H XV-14-4 'Bu H H CH 2CH(CH3)2 Et F F H OH H H XV-14-5 'Bu H H CH 2Ph Et F F H OH H H XV-14-6 'Bu H H CH 2-indol-3-yl Et F F H OH H H XV-14-7 'Bu H H CH 2CH2SCH 3 Et F F H OH H H XV-14-8 'Bu * H * Et F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-15. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' XV-15-1 Ph H H H Et F F H OH H H XV-15-2 Ph H H CH3 Et F F H OH H H XV-15-3 Ph H H CH(CH3)2 Et F F H OH H H XV-15-4 Ph H H CH2CH(CH3) 2 Et F F H OH H H XV-15-5 Ph H H CH 2Ph Et F F H OH H H XV-15-6 Ph H H CH 2-indol-3-yl Et F F H OH H H XV-15-7 Ph H H CH2CH 2SCH 3 Et F F H OH H H XV-15-8 Ph * H * Et F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-16. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R' XV-16-1 p-Me-Ph H H H Et F F H OH H H XV-16-2 p-Me-Ph H H CH3 Et F F H OH H H XV-16-3 p-Me-Ph H H CH(CH3)2 Et F F H OH H H XV-16-4 p-Me-Ph H H CH2CH(CH3) 2 Et F F H OH H H XV-16-5 p-Me-Ph H H CH 2Ph Et F F H OH H H XV-16-6 p-Me-Ph H H CH 2-indol-3-yl Et F F H OH H H XV-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et F F H OH H H XV-16-8 p-Me-Ph * H * Et F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-17. No R R2 R 3 a R 3b R4 R 5 R6 X Y R7 R' XV-17-1 p-F-Ph H H H Et F F H OH H H XV-17-2 p-F-Ph H H CH3 Et F F H OH H H XV-17-3 p-F-Ph H H CH(CH3)2 Et F F H OH H H XV-17-4 p-F-Ph H H CH2CH(CH3) 2 Et F F H OH H H XV-17-5 p-F-Ph H H CH 2Ph Et F F H OH H H XV-17-6 p-F-Ph H H CH 2-indol-3-yl Et F F H OH H H XV-17-7 p-F-Ph H H CH2CH 2SCH 3 Et F F H OH H H XV-17-8 p-F-Ph * H * Et F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-18. No R1 R2 R 3a R 3b R4 R X Y R7 R' XV-18-1 p-Cl-Ph H H H Et F F H OH H H XV-18-2 p-Cl-Ph H H CH 3 Et F F H OH H H XV-18-3 p-Cl-Ph H H CH(CH3) 2 Et F F H OH H H XV-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et F F H OH H H XV-18-5 p-Cl-Ph H H CH 2Ph Et F F H OH H H XV-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et F F H OH H H XV-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et F F H OH H H XV-18-8 p-Cl-Ph * H * Et F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-19. No R R2 R 3 a R3 b R 4 R R 6 X Y R7 R' XV-19-1 p-Br-Ph H H H Et F F H OH H H XV-19-2 p-Br-Ph H H CH 3 Et F F H OH H H XV-19-3 p-Br-Ph H H CH(CH3) 2 Et F F H OH H H XV-19-4 p-Br-Ph H H CH 2CH(CH3)2 Et F F H OH H H XV-19-5 p-Br-Ph H H CH 2Ph Et F F H OH H H XV-19-6 p-Br-Ph H H CH 2-indol-3-yl Et F F H OH H H XV-19-7 p-Br-Ph H H CH 2CH2SCH 3 Et F F H OH H H XV-19-8 p-Br-Ph * H * Et F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-20. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' XV-20-1 p-I-Ph H H H Et F F H OH H H XV-20-2 p-I-Ph H H CH3 Et F F H OH H H XV-20-3 p-I-Ph H H CH(CH3)2 Et F F H OH H H XV-20-4 p-I-Ph H H CH2CH(CH3) 2 Et F F H OH H H XV-20-5 p-I-Ph H H CH 2Ph Et F F H OH H H XV-20-6 p-I-Ph H H CH 2-indol-3-yl Et F F H OH H H XV-20-7 p-I-Ph H H CH2CH 2SCH 3 Et F F H OH H H XV-20-8 p-I-Ph * H * Et F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'11 A

Table XV-21. No R1 R 2 R3 a R3b R4 R R X Y R7 R' XV-21-1 CH3 H H H 'Pr F F H OH H H XV-21-2 CH3 H H CH 3 'Pr F F H OH H H XV-21-3 CH3 H H CH(CH3) 2 'Pr F F H OH H H XV-21-4 CH3 H H CH 2CH(CH3) 2 'Pr F F H OH H H XV-21-5 CH3 H H CH 2Ph 'Pr F F H OH H H XV-21-6 CH3 H H CH 2-indol-3-yl 'Pr F F H OH H H XV-21-7 CH3 H H CH 2CH2SCH 3 'Pr F F H OH H H XV-21-8 CH3 * H * 'Pr F F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-22. N9 Rl R 2 R3 a R3 b R4 R 5 R6 X Y R7 R' XV-22-1 Et H H H 'Pr F F H OH H H XV-22-2 Et H H CH 3 'Pr F F H OH H H XV-22-3 Et H H CH(CH 3)2 'Pr F F H OH H H XV-22-4 Et H H CH 2CH(CH3) 2 'Pr F F H OH H H XV-22-5 Et H H CH 2Ph 'Pr F F H OH H H XV-22-6 Et H H CH 2-indol-3-yl 'Pr F F H OH H H XV-22-7 Et H H CH 2CH 2SCH 3 'Pr F F H OH H H XV-22-8 Et * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-23. No R1 R2 R 3a R3b R4 R5 R6 X Y R7 R' XV-23-1 'Pr H H H 'Pr F F H OH H H XV-23-2 'Pr H H CH3 'Pr F F H OH H H XV-23-3 'Pr H H CH(CH 3)2 'Pr F F H OH H H XV-23-4 'Pr H H CH2CH(CH3) 2 'Pr F F H OH H H XV-23-5 Pr H H CH 2Ph 'Pr F F H OH H H XV-23-6 Pr H H CH 2-indol-3-yl 'Pr F F H OH H H XV-23-7 Pr H H CH2CH 2SCH 3 'Pr F F H OH H H XV-23-8 Pr * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

211 r-

Table XV-24. No R1 R2 R3 a R 3b R4 R' R' X Y R7 R' XV-24-1 'Bu H H H 'Pr F F H OH H H XV-24-2 'Bu H H CH 3 'Pr F F H OH H H XV-24-3 'Bu H H CH(CH 3) 2 'Pr F F H OH H H XV-24-4 'Bu H H CH 2CH(CH 3)2 'Pr F F H OH H H XV-24-5 'Bu H H CH 2Ph 'Pr F F H OH H H XV-24-6 'Bu H H CH 2-indol-3-yl 'Pr F F H OH H H XV-24-7 'Bu H H CH 2CH2SCH 3 'Pr F F H OH H H XV-24-8 'Bu * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-25. No R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' XV-25-1 Ph H H H 'Pr F F H OH H H XV-25-2 Ph H H CH3 'Pr F F H OH H H XV-25-3 Ph H H CH(CH 3) 2 'Pr F F H OH H H XV-25-4 Ph H H CH2CH(CH 3) 2 'Pr F F H OH H H XV-25-5 Ph H H CH 2Ph 'Pr F F H OH H H XV-25-6 Ph H H CH 2-indol-3-yl 'Pr F F H OH H H XV-25-7 Ph H H CH2CH 2SCH 3 'Pr F F H OH H H XV-25-8 Ph * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-26. N R1 R2 R3 a R3b R4 R 5 R6 X Y R7 R' XV-26-1 p-Me-Ph H H H 'Pr F F H OH H H XV-26-2 p-Me-Ph H H CH3 'Pr F F H OH H H XV-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr F F H OH H H XV-26-4 p-Me-Ph H H CH2CH(CH 3) 2 'Pr F F H OH H H XV-26-5 p-Me-Ph H H CH 2Ph 'Pr F F H OH H H XV-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr F F H OH H H XV-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr F F H OH H H XV-26-8 p-Me-Ph * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-27. No R R2 R 3 a R 3b R4 R' R6 X Y R7 R' XV-27-1 p-F-Ph H H H 'Pr F F H OH H H XV-27-2 p-F-Ph H H CH3 'Pr F F H OH H H XV-27-3 p-F-Ph H H CH(CH3)2 'Pr F F H OH H H XV-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr F F H OH H H XV-27-5 p-F-Ph H H CH 2Ph 'Pr F F H OH H H XV-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr F F H OH H H XV-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr F F H OH H H XV-27-8 p-F-Ph * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-28. No R1 R2 R 3a R3 b R4 R R 6 X Y R7 R' XV-28-1 p-Cl-Ph H H H 'Pr F F H OH H H XV-28-2 p-Cl-Ph H H CH 3 'Pr F F H OH H H XV-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr F F H OH H H XV-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr F F H OH H H XV-28-5 p-Cl-Ph H H CH 2Ph 'Pr F F H OH H H XV-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr F F H OH H H XV-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr F F H OH H H XV-28-8 p-Cl-Ph * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-29. N9 R1 R 2 R 3aR3 b R4 R R X Y R7 R' XV-29-1 p-Br-Ph H H H 'Pr F F H OH H H XV-29-2 p-Br-Ph H H CH 3 'Pr F F H OH H H XV-29-3 p-Br-Ph H H CH(CH3) 2 'Pr F F H OH H H XV-29-4 p-Br-Ph H H CH 2CH(CH3)2 'Pr F F H OH H H XV-29-5 p-Br-Ph H H CH 2Ph 'Pr F F H OH H H XV-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr F F H OH H H XV-29-7 p-Br-Ph H H CH 2CH2SCH 3 'Pr F F H OH H H XV-29-8 p-Br-Ph * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'21'7_

Table XV-30. No R R2 R 3 a R3b R4 R' R' X Y R7 R' XV-30-1 p-I-Ph H H H 'Pr F F H OH H H XV-30-2 p-I-Ph H H CH3 'Pr F F H OH H H XV-30-3 p-I-Ph H H CH(CH3)2 'Pr F F H OH H H XV-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr F F H OH H H XV-30-5 p-I-Ph H H CH 2Ph 'Pr F F H OH H H XV-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr F F H OH H H XV-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr F F H OH H H XV-30-8 p-I-Ph * H * 'Pr F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-31. No R1 R2 RaR 3 b R4 R 5 R6 X Y R7 R' XV-31-1 CH3 H H H "Bu F F H OH H H XV-31-2 CH3 H H CH 3 "Bu F F H OH H H XV-31-3 CH3 H H CH(CH3) 2 "Bu F F H OH H H XV-31-4 CH3 H H CH 2CH(CH3)2 "Bu F F H OH H H XV-31-5 CH3 H H CH 2Ph "Bu F F H OH H H XV-31-6 CH3 H H CH 2-indol-3-yl "Bu F F H OH H H XV-31-7 CH3 H H CH 2CH2SCH 3 "Bu F F H OH H H XV-31-8 CH3 * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-32. No Rl R 2 R3 a R3b R4 R 5 R6 X Y R7 R'

XV-32-1 Et H H H "Bu F F H OH H H XV-32-2 Et H H CH 3 "Bu F F H OH H H XV-32-3 Et H H CH(CH3) 2 "Bu F F H OH H H XV-32-4 Et H H CH 2CH(CH3) 2 "Bu F F H OH H H XV-32-5 Et H H CH 2Ph "Bu F F H OH H H XV-32-6 Et H H CH 2-indol-3-yl "Bu F F H OH H H XV-32-7 Et H H CH 2CH 2SCH 3 "Bu F F H OH H H XV-32-8 Et * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-33. No R1 R2 R 3a R3b R4 R' R6 X Y R7 R' XV-33-1 'Pr H H H "Bu F F H OH H H XV-33-2 'Pr H H CH3 "Bu F F H OH H H XV-33-3 'Pr H H CH(CH 3)2 "Bu F F H OH H H XV-33-4 Pr H H CH2CH(CH3) 2 "Bu F F H OH H H XV-33-5 Pr H H CH 2Ph "Bu F F H OH H H XV-33-6 Pr H H CH 2-indol-3-yl "Bu F F H OH H H XV-33-7 Pr H H CH2 CH 2 SCH 3 "Bu F F H OH H H XV-33-8 Pr * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-34. No R1 R2 R3a R3 b R4 R' R6 X Y R7 R XV-34-1 'Bu H H H "Bu F F H OH H H XV-34-2 'Bu H H CH 3 "Bu F F H OH H H XV-34-3 'Bu H H CH(CH3) 2 "Bu F F H OH H H XV-34-4 'Bu H H CH 2CH(CH3)2 "Bu F F H OH H H XV-34-5 'Bu H H CH 2Ph "Bu F F H OH H H XV-34-6 'Bu H H CH 2-indol-3-yl "Bu F F H OH H H XV-34-7 'Bu H H CH 2CH2 SCH 3 "Bu F F H OH H H XV-34-8 'Bu * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-35. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R'

XV-35-1 Ph H H H "Bu F F H OH H H XV-35-2 Ph H H CH3 "Bu F F H OH H H XV-35-3 Ph H H CH(CH3)2 "Bu F F H OH H H XV-35-4 Ph H H CH2CH(CH3) 2 "Bu F F H OH H H XV-35-5 Ph H H CH 2 Ph "Bu F F H OH H H XV-35-6 Ph H H CH 2-indol-3-yl "Bu F F H OH H H XV-35-7 Ph H H CH2 CH 2 SCH 3 "Bu F F H OH H H XV-35-8 Ph * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'210-

Table XV-36. No R R2 R3a R3b R4 R' R6 X Y R7 R' XV-36-1 p-Me-Ph H H H "Bu F F H OH H H XV-36-2 p-Me-Ph H H CH3 "Bu F F H OH H H XV-36-3 p-Me-Ph H H CH(CH3)2 "Bu F F H OH H H XV-36-4 p-Me-Ph H H CH2CH(CH3) 2 "Bu F F H OH H H XV-36-5 p-Me-Ph H H CH 2Ph "Bu F F H OH H H XV-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu F F H OH H H XV-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu F F H OH H H XV-36-8 p-Me-Ph * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-37. No R R 2 R 3 a R3 b R4 R' R6 X Y R7 R' XV-37-1 p-F-Ph H H H "Bu F F H OH H H XV-37-2 p-F-Ph H H CH3 "Bu F F H OH H H XV-37-3 p-F-Ph H H CH(CH3)2 "Bu F F H OH H H XV-37-4 p-F-Ph H H CH2CH(CH3) 2 "Bu F F H OH H H XV-37-5 p-F-Ph H H CH 2Ph "Bu F F H OH H H XV-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu F F H OH H H XV-37-7 p-F-Ph H H CH2CH 2 SCH 3 "Bu F F H OH H H XV-37-8 p-F-Ph * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-38. No R1 R2 R 3a R 3b R4 RR X Y R7 R' XV-38-1 p-Cl-Ph H H H "Bu F F H OH H H XV-38-2 p-Cl-Ph H H CH 3 "Bu F F H OH H H XV-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu F F H OH H H XV-38-4 p-Cl-Ph H H CH 2 CH(CH3)2 "Bu F F H OH H H XV-38-5 p-Cl-Ph H H CH 2 Ph "Bu F F H OH H H XV-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu F F H OH H H XV-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu F F H OH H H XV-38-8 p-Cl-Ph * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-39. 5 No R R 2 R3 a 3 R4 R R' X Y R7 R' XV-39-1 p-Br-Ph H H H "Bu F F H OH H H XV-39-2 p-Br-Ph H H CH 3 "Bu F F H OH H H XV-39-3 p-Br-Ph H H CH(CH 3)2 "Bu F F H OH H H XV-39-4 p-Br-Ph H H CH 2CH(CH3)2 "Bu F F H OH H H XV-39-5 p-Br-Ph H H CH 2Ph "Bu F F H OH H H XV-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu F F H OH H H XV-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu F F H OH H H XV-39-8 p-Br-Ph * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-40. No R R 2 R 3a R3 b R4 R' R6 X Y R7 R' XV-40-1 p-I-Ph H H H "Bu F F H OH H H XV-40-2 p-I-Ph H H CH3 "Bu F F H OH H H XV-40-3 p-I-Ph H H CH(CH3)2 "Bu F F H OH H H XV-40-4 p-I-Ph H H CH2CH(CH3) 2 "Bu F F H OH H H XV-40-5 p-I-Ph H H CH 2Ph "Bu F F H OH H H XV-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu F F H OH H H XV-40-7 p-I-Ph H H CH2CH 2SCH 3 "Bu F F H OH H H XV-40-8 p-I-Ph * H * "Bu F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-41. 6 No R R2 R3 a R 3b R4 R 5 R X Y R7 R' XV-41-1 CH3 H H H Bz F F H OH H H XV-41-2 CH3 H H CH 3 Bz F F H OH H H XV-41-3 CH3 H H CH(CH3) 2 Bz F F H OH H H XV-41-4 CH3 H H CH 2CH(CH3)2 Bz F F H OH H H XV-41-5 CH3 H H CH 2Ph Bz F F H OH H H XV-41-6 CH3 H H CH 2-indol-3-yl Bz F F H OH H H XV-41-7 CH3 H H CH 2CH2SCH 3 Bz F F H OH H H XV-41-8 CH3 * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-42. No Rl R 2 R3 a R3b R4 R' R' X Y R7 R' XV-42-1 Et H H H Bz F F H OH H H XV-42-2 Et H H CH 3 Bz F F H OH H H XV-42-3 Et H H CH(CH3) 2 Bz F F H OH H H XV-42-4 Et H H CH 2CH(CH3) 2 Bz F F H OH H H XV-42-5 Et H H CH 2Ph Bz F F H OH H H XV-42-6 Et H H CH 2-indol-3-yl Bz F F H OH H H XV-42-7 Et H H CH 2CH 2SCH 3 Bz F F H OH H H XV-42-8 Et * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-43. No R1 R2 R 3a R3 b R4 R 5 R6 X Y R7 R' XV-43-1 'Pr H H H Bz F F H OH H H XV-43-2 'Pr H H CH3 Bz F F H OH H A XV-43-3 'Pr H H CH(CH3)2 Bz F F H OH H H XV-43-4 'Pr H H CH2CH(CH3) 2 Bz F F H OH H H XV-43-5 'Pr H H CH 2Ph Bz F F H OH H H XV-43-6 'Pr H H CH 2-indol-3-yl Bz F F H OH H H XV-43-7 'Pr H H CH2CH 2SCH 3 Bz F F H OH H H XV-43-8 'Pr * H * Bz F F H OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-44. No R R2 R3 a R3 b R4 R 5 R6 X Y R7 R' XV-44-1 'Bu H H H Bz F F H OH H H XV-44-2 'Bu H H CH 3 Bz F F H OH H H XV-44-3 'Bu H H CH(CH 3) 2 Bz F F H OH H H XV-44-4 'Bu H H CH 2CH(CH3)2 Bz F F H OH H H XV-44-5 'Bu H H CH 2Ph Bz F F H OH H H XV-44-6 'Bu H H CH 2-indol-3-yl Bz F F H OH H H XV-44-7 'Bu H H CH 2CH2SCH 3 Bz F F H OH H H XV-44-8 'Bu * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-45. No R1 R2 R3 a R3b R4 R 5 R' X Y R7 R' XV-45-1 Ph H H H Bz F F H OH H H XV-45-2 Ph H H CH3 Bz F F H OH H H XV-45-3 Ph H H CH(CH3)2 Bz F F H OH H H XV-45-4 Ph H H CH2CH(CH3) 2 Bz F F H OH H H XV-45-5 Ph H H CH 2Ph Bz F F H OH H H XV-45-6 Ph H H CH 2-indol-3-yl Bz F F H OH H H XV-45-7 Ph H H CH2CH 2SCH 3 Bz F F H OH H H XV-45-8 Ph * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-46. No R R2 R 3 a R3 b R4 R 5 R6 X Y R7 R' XV-46-1 p-Me-Ph H H H Bz F F H OH H H XV-46-2 p-Me-Ph H H CH3 Bz F F H OH H H XV-46-3 p-Me-Ph H H CH(CH3)2 Bz F F H OH H H XV-46-4 p-Me-Ph H H CH2CH(CH 3) 2 Bz F F H OH H H XV-46-5 p-Me-Ph H H CH 2Ph Bz F F H OH H H XV-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz F F H OH H H XV-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz F F H OH H H XV-46-8 p-Me-Ph * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-47. No R R 2 R 3 a R 3b R4 R 5 R6 X Y R7 R' XV-47-1 p-F-Ph H H H Bz F F H OH H H XV-47-2 p-F-Ph H H CH3 Bz F F H OH H H XV-47-3 p-F-Ph H H CH(CH3)2 Bz F F H OH H H XV-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz F F H OH H H XV-47-5 p-F-Ph H H CH 2Ph Bz F F H OH H H XV-47-6 p-F-Ph H H CH 2-indol-3-yl Bz F F H OH H H XV-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz F F H OH H H XV-47-8 p-F-Ph * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XV-48. No R R 2 R3a R 3b R4 R R X Y R7 R' XV-48-1 p-Cl-Ph H H H Bz F F H OH H H XV-48-2 p-Cl-Ph H H CH 3 Bz F F H OH H H XV-48-3 p-Cl-Ph H H CH(CH3) 2 Bz F F H OH H H XV-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz F F H OH H H XV-48-5 p-Cl-Ph H H CH 2Ph Bz F F H OH H H XV-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz F F H OH H H XV-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz F F H OH H H XV-48-8 p-Cl-Ph * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-49. No R R2 R 3 a R3 b R4 R R 6 X Y R7 R' XV-49-1 p-Br-Ph H H H Bz F F H OH H H XV-49-2 p-Br-Ph H H CH 3 Bz F F H OH H H XV-49-3 p-Br-Ph H H CH(CH3) 2 Bz F F H OH H H XV-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz F F H OH H H XV-49-5 p-Br-Ph H H CH 2Ph Bz F F H OH H H XV-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz F F H OH H H XV-49-7 p-Br-Ph H H CH 2CH2SCH 3 Bz F F H OH H H XV-49-8 p-Br-Ph * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XV-50. No R R2 R 3 a R 3b R4 R 5 R 6 X Y R7 R' XV-50-1 p-I-Ph H H H Bz F F H OH H H XV-50-2 p-I-Ph H H CH3 Bz F F H OH H H XV-50-3 p-I-Ph H H CH(CH3)2 Bz F F H OH H H XV-50-4 p-I-Ph H H CH2CH(CH3) 2 Bz F F H OH H H XV-50-5 p-I-Ph H H CH 2Ph Bz F F H OH H H XV-50-6 p-I-Ph H H CH 2-indol-3-yl Bz F F H OH H H XV-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz F F H OH H H XV-50-8 p-I-Ph * H * Bz F F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R8 NH

R2 0 R3b R 3a 0NR- N 0

C0 2R 4 ORR6

Y X XVI

Table XVI-1. No R1 R2 R3 a R 3b R4 R' R6 X Y R7 R XVI-1-1 CH 3 H H H CH 3 F F F OH H H XVI-1-2 CH 3 H H CH3 CH 3 F F F OH H H XVI-1-3 CH 3 H H CH(CH 3) 2 CH 3 F F F OH H H XVI-1-4 CH 3 H H CH2CH(CH3) 2 CH 3 F F F OH H H XVI-1-5 CH 3 H H CH 2Ph CH 3 F F F OH H H XVI-1-6 CH 3 H H CH 2-indol-3-yl CH 3 F F F OH H H XVI-1-7 CH 3 H H CH2CH 2SCH3 CH 3 F F F OH H H XVI-1-8 CH 3 * H * CH 3 F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-2. No R1 R2 R3a R3 b R4 R 5 R6 X Y R7 R' XVI-2-1 Et H H H CH 3 F F F OH H H XVI-2-2 Et H H CH 3 CH 3 F F F OH H H XVI-2-3 Et H H CH(CH 3) 2 CH 3 F F F OH H H XVI-2-4 Et H H CH 2CH(CH 3) 2 CH 3 F F F OH H H XVI-2-5 Et H H CH 2Ph CH 3 F F F OH H H XVI-2-6 Et H H CH 2-indol-3-yl CH 3 F F F OH H H XVI-2-7 Et H H CH 2CH 2SCH 3 CH 3 F F F OH H H XVI-2-8 Et * H * CH 3 F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-3. No R1 R 2 R3 a R3 R4 R' R' X Y R7 R' XVI-3-1 'Pr H H H CH 3 F F F OH H H XVI-3-2 'Pr H H CH 3 CH 3 F F F OH H H XVI-3-3 'Pr H H CH(CH3) 2 CH 3 F F F OH H H XVI-3-4 'Pr H H CH 2CH(CH3)2 CH 3 F F F OH H H XVI-3-5 'Pr H H CH 2Ph CH 3 F F F OH H H XVI-3-6 'Pr H H CH 2-indol-3-yl CH 3 F F F OH H H XVI-3-7 'Pr H H CH 2CH2SCH 3 CH 3 F F F OH H H XVI-3-8 Pr * H * CH 3 F F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-4. N9 R1 R2 R 3a Rb R4 R R6 X Y R7 R XVI-4-1 'Bu H H H CH3 F F F OH H H XVI-4-2 'Bu H H CH 3 CH3 F F F OH H H XVI-4-3 'Bu H H CH(CH3) 2 CH3 F F F OH H H XVI-4-4 'Bu H H CH 2CH(CH3)2 CH3 F F F OH H H XVI-4-5 'Bu H H CH 2Ph CH3 F F F OH H H XVI-4-6 'Bu H H CH 2-indol-3-yl CH3 F F F OH H H XVI-4-7 'Bu H H CH 2CH2SCH 3 CH3 F F F OH H H XVI-4-8 'Bu * H * CH3 F F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-5. No I R 2 R3 a R 3 R4 R R6 X Y R7 R XVI-5-1 Ph H H H CH 3 F F F OH H H XVI-5-2 Ph H H CH3 CH3 F F F OH H H XVI-5-3 Ph H H CH(CH3) 2 CH3 F F F OH H H XVI-5-4 Ph H H CH2CH(CH3)2 CH 3 F F F OH H H XVI-5-5 Ph H H CH 2Ph CH 3 F F F OH H H XVI-5-6 Ph H H CH 2-indol-3-yl CH3 F F F OH H H XVI-5-7 Ph H H CH2CH 2SCH3 CH3 F F F OH H H XVI-5-8 Ph * H * CH 3 F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-6. No R RR 3 a R 3b R4 R' R6 X Y R7 R' XVI-6-1 p-Me-Ph H H H CH 3 F F F OH H H XVI-6-2 p-Me-Ph H H CH 3 CH3 F F F OH H H XVI-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 F F F OH H H XVI-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH 3 F F F OH H H XVI-6-5 p-Me-Ph H H CH 2Ph CH 3 F F F OH H H XVI-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 F F F OH H H XVI-6-7 p-Me-Ph H H CH 2CH 2SCH3 CH3 F F F OH H H XVI-6-8 p-Me-Ph * H * CH 3 F F F OH H H *R2 and R3b joined together by (CH2)3 to form five-membered ring.

Table XVI-7. No R R2 R 3 a R3 b R4 R' R6 X Y R7 R' XVI-7-1 p-F-Ph H H H CH 3 F F F OH H H XVI-7-2 p-F-Ph H H CH 3 CH3 F F F OH H H XVI-7-3 p-F-Ph H H CH(CH 3) 2 CH3 F F F OH H H XVI-7-4 p-F-Ph H H CH 2CH(CH 3) 2 CH 3 F F F OH H H XVI-7-6 p-F-Ph H H CH 2Ph CH 3 F F F OH H H XVI-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 F F F OH H H XVI-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 F F F OH H H XVI-7-20 p-F-Ph * H * CH 3 F F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-8. No R R2 R 3 a R 3b R4 R 5 R 6 X Y R7 R' XVI-8-1 p-Cl-Ph H H H CH3 F F F OH H H XVI-8-2 p-Cl-Ph H H CH 3 CH3 F F F OH H H XVI-8-3 p-Cl-Ph H H CH(CH 3)2 CH 3 F F F OH H H XVI-8-4 p-Cl-Ph H H CH 2CH(CH 3) 2 CH 3 F F F OH H H XVI-8-5 p-Cl-Ph H H CH 2Ph CH3 F F F OH H H XVI-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 F F F OH H H XVI-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 F F F OH H H XVI-8-8 p-Cl-Ph * H * CH3 F F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'I1 7-

Table XVI-9. No R R2 R3a R3b R4 R' R6 X Y R7 R' XVI-9-1 p-Br-Ph H H H CH 3 F F F OH H H XVI-9-2 p-Br-Ph H H CH3 CH 3 F F F OH H H XVI-9-3 p-Br-Ph H H CH(CH3)2 CH 3 F F F OH H H XVI-9-4 p-Br-Ph H H CH2CH(CH 3)2 CH 3 F F F OH H H XVI-9-6 p-Br-Ph H H CH 2Ph CH 3 F F F OH H H XVI-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 F F F OH H H XVI-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 F F F OH H H XVI-9-20 p-Br-Ph * H * CH 3 F F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-10. N R1 R2 R3a R3 b R4 R' R6 X Y R7 R' XVI-10-1 p-I-Ph H H H CH 3 F F F OH H H XVI-10-2 p-I-Ph H H CH 3 CH 3 F F F OH H H XVI-10-3 p-I-Ph H H CH(CH3) 2 CH 3 F F F OH H H XVI-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 F F F OH H H XVI-10-5 p-I-Ph H H CH 2Ph CH 3 F F F OH H H XVI-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 F F F OH H H XVI-10-7 p-I-Ph H H CH 2CH2SCH 3 CH 3 F F F OH H H XVI-10-8 p-I-Ph * H * CH 3 F F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-11. No R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' XVI-11-1 CH 3 H H H Et F F F OH H H XVI-11-2 CH 3 H H CH3 Et F F F OH H H XVI-11-3 CH 3 H H CH(CH3) 2 Et F F F OH H H XVI-11-4 CH 3 H H CH2CH(CH3) 2 Et F F F OH H H XVI-11-5 CH 3 H H CH 2Ph Et F F F OH H H XVI-11-6 CH 3 H H CH 2-indol-3-yl Et F F F OH H H XVI-11-7 CH 3 H H CH2CH 2SCH 3 Et F F F OH H H XVI-11-8 CH 3 * H * Et F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-12. Rl R 2 R 3a R 3b R4 R 5 R 6 X Y R7 R' No XVI-12-1 Et H H H Et F F F OH H H XVI-12-2 Et H H CH3 Et F F F OH H H XVI-12-3 Et H H CH(CH3)2 Et F F F OH H H XVI-12-4 Et H H CH2CH(CH3) 2 Et F F F OH H H XVI-12-5 Et H H CH 2Ph Et F F F OH H H XVI-12-6 Et H H CH 2-indol-3-yl Et F F F OH H H XVI-12-7 Et H H CH2CH 2SCH 3 Et F F F OH H H XVI-12-8 Et * H * Et F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-13. 6 M9 R' R2 R 3a R3 b R 4 R R X Y R7 R' XVI-13-1 'Pr H H H Et F F F OH H H XVI-13-2 'Pr H H CH 3 Et F F F OH H H XVI-13-3 'Pr H H CH(CH3) 2 Et F F F OH H H XVI-13-4 'Pr H H CH 2 CH(CH3)2 Et F F F OH H H XVI-13-5 'Pr H H CH 2Ph Et F F F OH H H XVI-13-6 'Pr H H CH 2-indol-3-yl Et F F F OH H H XVI-13-7 'Pr H H CH 2CH2SCH 3 Et F F F OH H H XVI-13-8 'Pr * H * Et F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-14. No R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XVI-14-1 'Bu H H H Et F F F OH H H XVI-14-2 'Bu H H CH 3 Et F F F OH H H XVI-14-3 'Bu H H CH(CH3) 2 Et F F F OH H H XVI-14-4 'Bu H H CH 2CH(CH3)2 Et F F F OH H H XVI-14-5 'Bu H H CH 2Ph Et F F F OH H H XVI-14-6 'Bu H H CH 2-indol-3-yl Et F F F OH H H XVI-14-7 'Bu H H CH 2CH2SCH 3 Et F F F OH H H XVI-14-8 'Bu * H * Et F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_no-_

Table XVI-15. No R1 R2 R 3a R3b R4 R 5 R' X Y R7 R' XVI-15-1 Ph H H H Et F F F OH H H XVI-15-2 Ph H H CH3 Et F F F OH H H XVI-15-3 Ph H H CH(CH3) 2 Et F F F OH H H XVI-15-4 Ph H H CH2CH(CH3)2 Et F F F OH H H XVI-15-5 Ph H H CH 2Ph Et F F F OH H H XVI-15-6 Ph H H CH 2-indol-3-yl Et F F F OH H H XVI-15-7 Ph H H CH2CH2SCH 3 Et F F F OH H H XVI-15-8 Ph * H * Et F F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-16. N9 R1 R2 R 3a R3 b R4 R 5 R6 X Y R7 R' XVI-16-1 p-Me-Ph H H H Et F F F OH H H XVI-16-2 p-Me-Ph H H CH 3 Et F F F OH H H XVI-16-3 p-Me-Ph H H CH(CH3) 2 Et F F F OH H H XVI-16-4 p-Me-Ph H H CH 2CH(CH3)2 Et F F F OH H H XVI-16-5 p-Me-Ph H H CH 2Ph Et F F F OH H H XVI-16-6 p-Me-Ph H H CH 2-indol-3-yl Et F F F OH H H XVI-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et F F F OH H H XVI-16-8 p-Me-Ph * H * Et F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-17. No R R2 R 3 a R3b R4 R 5 R6 X Y R7 R' XVI-17-1 p-F-Ph H H H Et F F F OH H H XVI-17-2 p-F-Ph H H CH 3 Et F F F OH H H XVI-17-3 p-F-Ph H H CH(CH3) 2 Et F F F OH H H XVI-17-4 p-F-Ph H H CH 2CH(CH3)2 Et F F F OH H H XVI-17-5 p-F-Ph H H CH 2Ph Et F F F OH H H XVI-17-6 p-F-Ph H H CH 2-indol-3-yl Et F F F OH H H XVI-17-7 p-F-Ph H H CH 2CH2SCH 3 Et F F F OH H H XVI-17-8 p-F-Ph * H * Et F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-18. No R R2 R 3 a R 3b R4 R R X Y R7 R' XVI-18-1 p-Cl-Ph H H H Et F F F OH H H XVI-18-2 p-Cl-Ph H H CH 3 Et F F F OH H H XVI-18-3 p-Cl-Ph H H CH(CH3) 2 Et F F F OH H H XVI-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et F F F OH H H XVI-18-5 p-Cl-Ph H H CH 2Ph Et F F F OH H H XVI-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et F F F OH H H XVI-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et F F F OH H H XVI-18-8 p-Cl-Ph * H * Et F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-19. N9 R1 R2 R 3a R3 b R4 R 5 R6 X Y R7 R XVI-19-1 p-Br-Ph H H H Et F F F OH H H XVI-19-2 p-Br-Ph H H CH3 Et F F F OH H H XVI-19-3 p-Br-Ph H H CH(CH3)2 Et F F F OH H H XVI-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et F F F OH H H XVI-19-5 p-Br-Ph H H CH 2Ph Et F F F OH H H XVI-19-6 p-Br-Ph H H CH 2-indol-3-yl Et F F F OH H H XVI-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et F F F OH H H XVI-19-8 p-Br-Ph * H * Et F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-20. No R R2 R 3 a R3b R4 R5 R6 X Y R7 XVI-20-1 p-I-Ph H H H Et F F F OH H XVI-20-2 p-I-Ph H H CH 3 Et F F F OH H XVI-20-3 p-I-Ph H H CH(CH3) 2 Et F F F OH H XVI-20-4 p-I-Ph H H CH 2CH(CH3)2 Et F F F OH H XVI-20-5 p-I-Ph H H CH 2Ph Et F F F OH H XVI-20-6 p-I-Ph H H CH 2-indol-3-yl Et F F F OH H XVI-20-7 p-I-Ph H H CH 2CH2SCH 3 Et F F F OH H XVI-20-8 p-I-Ph * H * Et F F F OH H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-21. No R1 R2 R 3a R3b R4 R' R6 X Y R7 R' XVI-21-1 CH 3 H H H 'Pr F F F OH H H XVI-21-2 CH 3 H H CH3 'Pr F F F OH H H XVI-21-3 CH 3 H H CH(CH 3)2 'Pr F F F OH H H XVI-21-4 CH 3 H H CH2CH(CH3) 2 'Pr F F F OH H H XVI-21-5 CH 3 H H CH 2Ph 'Pr F F F OH H H XVI-21-6 CH 3 H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-21-7 CH 3 H H CH2CH 2SCH 3 'Pr F F F OH H H XVI-21-8 CH 3 * H * 'Pr F F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-22. N R1 RR 2 R 3a R3 b R4 R' R6 X Y R7 R' XVI-22-1 Et H H H 'Pr F F F OH H H XVI-22-2 Et H H CH3 'Pr F F F OH H H XVI-22-3 Et H H CH(CH 3) 2 'Pr F F F OH H H XVI-22-4 Et H H CH2CH(CH3) 2 'Pr F F F OH H H XVI-22-5 Et H H CH 2Ph 'Pr F F F OH H H XVI-22-6 Et H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-22-7 Et H H CH2CH 2SCH 3 'Pr F F F OH H H XVI-22-8 Et * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-23. R' 6 No R2 R 3a R3b R4 R R X Y R7 R' XVI-23-1 'Pr H H H 'Pr F F F OH H H XVI-23-2 'Pr H H CH 3 'Pr F F F OH H H XVI-23-3 'Pr H H CH(CH 3)2 'Pr F F F OH H H XVI-23-4 'Pr H H CH 2CH(CH3) 2 'Pr F F F OH H H XVI-23-5 Pr H H CH 2Ph 'Pr F F F OH H H XVI-23-6 Pr H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-23-7 Pr H H CH 2CH2SCH 3 'Pr F F F OH H H XVI-23-8 Pr * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-24. No RI R2 RaR 3 b R4 R R X Y R7 R' XVI-24-1 'Bu H H H 'Pr F F F OH H H XVI-24-2 'Bu H H CH 3 'Pr F F F OH H H XVI-24-3 'Bu H H CH(CH 3) 2 'Pr F F F OH H H XVI-24-4 'Bu H H CH 2CH(CH3) 2 'Pr F F F OH H H XVI-24-5 'Bu H H CH 2Ph 'Pr F F F OH H H XVI-24-6 'Bu H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-24-7 'Bu H H CH 2CH2SCH 3 'Pr F F F OH H H XVI-24-8 'Bu * H * 'Pr F F F OH H H

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XVI-25. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y R7 R' XVI-25-1 Ph H H H 'Pr F F F OH H H XVI-25-2 Ph H H CH3 'Pr F F F OH H H XVI-25-3 Ph H H CH(CH 3)2 'Pr F F F OH H H XVI-25-4 Ph H H CH2CH(CH 3) 2 'Pr F F F OH H H XVI-25-5 Ph H H CH 2Ph 'Pr F F F OH H H XVI-25-6 Ph H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-25-7 Ph H H CH2CH2SCH 3 'Pr F F F OH H H XVI-25-8 Ph * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-26. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' XVI-26-1 p-Me-Ph H H H 'Pr F F F OH H H XVI-26-2 p-Me-Ph H H CH 3 'Pr F F F OH H H XVI-26-3 p-Me-Ph H H CH(CH 3)2 'Pr F F F OH H H XVI-26-4 p-Me-Ph H H CH 2CH(CH 3) 2 'Pr F F F OH H H XVI-26-5 p-Me-Ph H H CH 2Ph 'Pr F F F OH H H XVI-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr F F F OH H H XVI-26-8 p-Me-Ph * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-27. No R RR 3 a R 3b R4 R' R' X Y R7 R' XVI-27-1 p-F-Ph H H H Pr F F F OH H H XVI-27-2 p-F-Ph H H CH 3 'Pr F F F OH H H XVI-27-3 p-F-Ph H H CH(CH3) 2 'Pr F F F OH H H XVI-27-4 p-F-Ph H H CH 2CH(CH3)2 'Pr F F F OH H H XVI-27-5 p-F-Ph H H CH 2Ph 'Pr F F F OH H H XVI-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr F F F OH H H XVI-27-8 p-F-Ph * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-28. N9 R1 R 2 R 3a R3 b R4 R R 6 X Y R7 R' XVI-28-1 p-Cl-Ph H H H 'Pr F F F OH H H XVI-28-2 p-Cl-Ph H H CH 3 'Pr F F F OH H H XVI-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr F F F OH H H XVI-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr F F F OH H H XVI-28-5 p-Cl-Ph H H CH 2Ph 'Pr F F F OH H H XVI-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr F F F OH H H XVI-28-8 p-Cl-Ph * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-29. 6 No R R 2 R3a R 3b R4 R5 R X Y R7 R' XVI-29-1 p-Br-Ph H H H 'Pr F F F OH H H XVI-29-2 p-Br-Ph H H CH3 'Pr F F F OH H H XVI-29-3 p-Br-Ph H H CH(CH3)2 'Pr F F F OH H H XVI-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr F F F OH H H XVI-29-5 p-Br-Ph H H CH 2Ph 'Pr F F F OH H H XVI-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr F F F OH H H XVI-29-8 p-Br-Ph * H * Pr F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

22,1-

Table XVI-30. 5 No R RR 3 a R3b R4 R R' X Y R7 R' XVI-30-1 p-I-Ph H H H 'Pr F F F OH H H XVI-30-2 p-I-Ph H H CH 3 'Pr F F F OH H H XVI-30-3 p-I-Ph H H CH(CH3) 2 'Pr F F F OH H H XVI-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr F F F OH H H XVI-30-5 p-I-Ph H H CH 2Ph 'Pr F F F OH H H XVI-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr F F F OH H H XVI-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr F F F OH H H XVI-30-8 p-I-Ph * H * 'Pr F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-31. No R1 R2 R3a R3b R4 R' R6 X Y R7 R' XVI-31-1 CH 3 H H H "Bu F F F OH H H XVI-31-2 CH 3 H H CH3 "Bu F F F OH H H XVI-31-3 CH 3 H H CH(CH3) 2 "Bu F F F OH H H XVI-31-4 CH 3 H H CH2CH(CH3) 2 "Bu F F F OH H H XVI-31-5 CH 3 H H CH 2Ph "Bu F F F OH H H XVI-31-6 CH 3 H H CH 2-indol-3-yl "Bu F F F OH H H XVI-31-7 CH 3 H H CH2CH 2SCH 3 "Bu F F F OH H H XVI-31-8 CH 3 * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-32. No Rl R2 R 3a R3b R4 R 5 R6 X Y R7 R'

XVI-32-1 Et H H H "Bu F F F OH H H XVI-32-2 Et H H CH3 "Bu F F F OH H H XVI-32-3 Et H H CH(CH3)2 "Bu F F F OH H H XVI-32-4 Et H H CH2CH(CH3) 2 "Bu F F F OH H H XVI-32-5 Et H H CH 2Ph "Bu F F F OH H H XVI-32-6 Et H H CH 2-indol-3-yl "Bu F F F OH H H XVI-32-7 Et H H CH2CH 2SCH 3 "Bu F F F OH H H XVI-32-8 Et * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-33. 3 No R' R2 R3 aR R4 R' R X Y R7 R' XVI-33-1 'Pr H H H "Bu F F F OH H H XVI-33-2 'Pr H H CH 3 "Bu F F F OH H H XVI-33-3 'Pr H H CH(CH 3)2 "Bu F F F OH H H XVI-33-4 Pr H H CH 2CH(CH3) 2 "Bu F F F OH H H XVI-33-5 Pr H H CH 2Ph "Bu F F F OH H H XVI-33-6 Pr H H CH 2-indol-3-yl "Bu F F F OH H H XVI-33-7 Pr H H CH 2 CH2 SCH 3 "Bu F F F OH H H XVI-33-8 Pr * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-34. No R1 R2 R3 a R3b R4 R R6 X Y R7 R' XVI-34-1 'Bu H H H "Bu F F F OH H H XVI-34-2 'Bu H H CH 3 "Bu F F F OH H H XVI-34-3 'Bu H H CH(CH3) 2 "Bu F F F OH H H XVI-34-4 'Bu H H CH 2 CH(CH3)2 "Bu F F F OH H H XVI-34-5 'Bu H H CH 2Ph "Bu F F F OH H H XVI-34-6 'Bu H H CH 2-indol-3-yl "Bu F F F OH H H XVI-34-7 'Bu H H CH 2 CH2SCH 3 "Bu F F F OH H H XVI-34-8 'Bu * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-35. No RI 1 R2 R 3a R3 b R4 R 5 R6 X Y R7 R'

XVI-35-1 Ph H H H "Bu F F F OH H H XVI-35-2 Ph H H CH3 "Bu F F F OH H H XVI-35-3 Ph H H CH(CH3) 2 "Bu F F F OH H H XVI-35-4 Ph H H CH2 CH(CH3)2 "Bu F F F OH H H XVI-35-5 Ph H H CH 2 Ph "Bu F F F OH H H XVI-35-6 Ph H H CH 2-indol-3-yl "Bu F F F OH H H XVI-35-7 Ph H H CH2 CH2 SCH 3 "Bu F F F OH H H XVI-35-8 Ph * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-36. No R RR 3 a R3b R4 R' R6 X Y R7 R' XVI-36-1 p-Me-Ph H H H "Bu F F F OH H H XVI-36-2 p-Me-Ph H H CH 3 "Bu F F F OH H H XVI-36-3 p-Me-Ph H H CH(CH 3)2 "Bu F F F OH H H XVI-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu F F F OH H H XVI-36-5 p-Me-Ph H H CH 2Ph "Bu F F F OH H H XVI-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu F F F OH H H XVI-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu F F F OH H H XVI-36-8 p-Me-Ph * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-37. No R R2 R 3 a R3 b R4 R' R6 X Y R7 R' XVI-37-1 p-F-Ph H H H "Bu F F F OH H H XVI-37-2 p-F-Ph H H CH 3 "Bu F F F OH H H XVI-37-3 p-F-Ph H H CH(CH 3) 2 "Bu F F F OH H H XVI-37-4 p-F-Ph H H CH 2 CH(CH 3) 2 "Bu F F F OH H H XVI-37-5 p-F-Ph H H CH 2Ph "Bu F F F OH H H XVI-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu F F F OH H H XVI-37-7 p-F-Ph H H CH 2 CH 2 SCH 3 "Bu F F F OH H H XVI-37-8 p-F-Ph * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-38. No R1 R2 R 3a R 3b R4 R R X Y R7 R' XVI-38-1 p-Cl-Ph H H H "Bu F F F OH H H XVI-38-2 p-Cl-Ph H H CH 3 "Bu F F F OH H H XVI-38-3 p-Cl-Ph H H CH(CH3 ) 2 "Bu F F F OH H H XVI-38-4 p-Cl-Ph H H CH 2CH(CH 3 ) 2 "Bu F F F OH H H XVI-38-5 p-Cl-Ph H H CH 2Ph "Bu F F F OH H H XVI-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu F F F OH H H XVI-38-7 p-Cl-Ph H H CH 2CH 2 SCH 3 "Bu F F F OH H H XVI-38-8 p-Cl-Ph * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'117-

Table XVI-39. No R R2 R3a R3b R4 R' R6 X Y R7 R' XVI-39-1 p-Br-Ph H H H "Bu F F F OH H H XVI-39-2 p-Br-Ph H H CH3 "Bu F F F OH H H XVI-39-3 p-Br-Ph H H CH(CH 3)2 "Bu F F F OH H H XVI-39-4 p-Br-Ph H H CH2CH(CH3) 2 "Bu F F F OH H H XVI-39-5 p-Br-Ph H H CH 2Ph "Bu F F F OH H H XVI-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu F F F OH H H XVI-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu F F F OH H H XVI-39-8 p-Br-Ph * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-40. N R1 R2 R3a R3b R4 R' R6 X Y R7 R' XVI-40-1 p-I-Ph H H H "Bu F F F OH H H XVI-40-2 p-I-Ph H H CH 3 "Bu F F F OH H H XVI-40-3 p-I-Ph H H CH(CH3) 2 "Bu F F F OH H H XVI-40-4 p-I-Ph H H CH 2CH(CH 3) 2 "Bu F F F OH H H XVI-40-5 p-I-Ph H H CH 2Ph "Bu F F F OH H H XVI-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu F F F OH H H XVI-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu F F F OH H H XVI-40-8 p-I-Ph * H * "Bu F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-41. No R1 R2 R 3a R3b R4 R 5 R6 X Y R7 R' XVI-41-1 CH 3 H H H Bz F F F OH H H XVI-41-2 CH 3 H H CH3 Bz F F F OH H H XVI-41-3 CH 3 H H CH(CH3) 2 Bz F F F OH H H XVI-41-4 CH 3 H H CH2CH(CH3) 2 Bz F F F OH H H XVI-41-5 CH 3 H H CH 2Ph Bz F F F OH H H XVI-41-6 CH 3 H H CH 2-indol-3-yl Bz F F F OH H H XVI-41-7 CH 3 H H CH2CH 2SCH 3 Bz F F F OH H H XVI-41-8 CH 3 * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-42. 5 No Rl R 2 R 3a R 3b R4 R R' X Y R7 R' XVI-42-1 Et H H H Bz F F F OH H H XVI-42-2 Et H H CH3 Bz F F F OH H H XVI-42-3 Et H H CH(CH3)2 Bz F F F OH H H XVI-42-4 Et H H CH2CH(CH3) 2 Bz F F F OH H H XVI-42-5 Et H H CH 2Ph Bz F F F OH H H XVI-42-6 Et H H CH 2-indol-3-yl Bz F F F OH H H XVI-42-7 Et H H CH2CH 2SCH 3 Bz F F F OH H H XVI-42-8 Et * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-43. 6 No R' R2 R 3a R3 b R4 R R X Y R7 R' XVI-43-1 'Pr H H H Bz F F F OH H H XVI-43-2 'Pr H H CH 3 Bz F F F OH H A XVI-43-3 'Pr H H CH(CH3) 2 Bz F F F OH H H XVI-43-4 'Pr H H CH 2CH(CH3)2 Bz F F F OH H H XVI-43-5 'Pr H H CH 2Ph Bz F F F OH H H XVI-43-6 'Pr H H CH 2-indol-3-yl Bz F F F OH H H XVI-43-7 'Pr H H CH 2CH2SCH 3 Bz F F F OH H H XVI-43-8 'Pr * H * Bz F F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-44. R R2 R3 a R3 b R4 R R 6 X Y R7 R' No XVI-44-1 'Bu H H H Bz F F F OH H H XVI-44-2 'Bu H H CH 3 Bz F F F OH H H XVI-44-3 'Bu H H CH(CH3) 2 Bz F F F OH H H XVI-44-4 'Bu H H CH 2CH(CH3)2 Bz F F F OH H H XVI-44-5 'Bu H H CH 2Ph Bz F F F OH H H XVI-44-6 'Bu H H CH 2-indol-3-yl Bz F F F OH H H XVI-44-7 'Bu H H CH 2CH2SCH 3 Bz F F F OH H H XVI-44-8 'Bu * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_no-_

Table XVI-45. No R1 R2 R3 a R3b R4 R 5 R' X Y R7 R' XVII-45-1 Ph H H H Bz F F F OH H H XVII-45-2 Ph H H CH 3 Bz F F F OH H H XVII-45-3 Ph H H CH(CH3) 2 Bz F F F OH H H XVII-45-4 Ph H H CH 2CH(CH3) 2 Bz F F F OH H H XVII-45-5 Ph H H CH 2Ph Bz F F F OH H H XVII-45-6 Ph H H CH 2-indol-3-yl Bz F F F OH H H XVII-45-7 Ph H H CH 2CH 2SCH 3 Bz F F F OH H H XVII-45-8 Ph * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-46. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' XVII-46-1 p-Me-Ph H H H Bz F F F OH H H XVII-46-2 p-Me-Ph H H CH3 Bz F F F OH H H XVII-46-3 p-Me-Ph H H CH(CH3) 2 Bz F F F OH H H XVII-46-4 p-Me-Ph H H CH2CH(CH3) 2 Bz F F F OH H H XVII-46-5 p-Me-Ph H H CH 2Ph Bz F F F OH H H XVII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz F F F OH H H XVII-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz F F F OH H H XVII-46-8 p-Me-Ph * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVI-47. 5 No R R2 R 3 a R 3b R4 R R6 X Y R7 R' XVII-47-1 p-F-Ph H H H Bz F F F OH H H XVII-47-2 p-F-Ph H H CH 3 Bz F F F OH H H XVII-47-3 p-F-Ph H H CH(CH 3) 2 Bz F F F OH H H XVII-47-4 p-F-Ph H H CH 2CH(CH 3)2 Bz F F F OH H H XVII-47-5 p-F-Ph H H CH 2Ph Bz F F F OH H H XVII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz F F F OH H H XVII-47-7 p-F-Ph H H CH 2CH 2SCH 3 Bz F F F OH H H XVII-47-8 p-F-Ph * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'IA -

Table XVI-48. R RR 3 R 3b R4 R' R 6 X Y R7 R' No a

XVII-48-1 p-Cl-Ph H H H Bz F F F OH H H XVII-48-2 p-Cl-Ph H H CH 3 Bz F F F OH H H XVII-48-3 p-Cl-Ph H H CH(CH3) 2 Bz F F F OH H H XVII-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz F F F OH H H XVII-48-5 p-Cl-Ph H H CH 2Ph Bz F F F OH H H XVII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz F F F OH H H XVII-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz F F F OH H H XVII-48-8 p-Cl-Ph * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-49. N9 R1 R 2 R3 a R3 b R4 R R 6 X Y R7 R' XVII-49-1 p-Br-Ph H H H Bz F F F OH H H XVII-49-2 p-Br-Ph H H CH 3 Bz F F F OH H H XVII-49-3 p-Br-Ph H H CH(CH3) 2 Bz F F F OH H H XVII-49-4 p-Br-Ph H H CH 2CH(CH3)2 Bz F F F OH H H XVII-49-5 p-Br-Ph H H CH 2Ph Bz F F F OH H H XVII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz F F F OH H H XVII-49-7 p-Br-Ph H H CH 2CH2SCH 3 Bz F F F OH H H XVII-49-8 p-Br-Ph * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVI-50. 5 6 No R R2 R 3 a R 3b R4 R R X Y R7 R' XVII-50-1 p-I-Ph H H H Bz F F F OH H H XVII-50-2 p-I-Ph H H CH3 Bz F F F OH H H XVII-50-3 p-I-Ph H H CH(CH3) 2 Bz F F F OH H H XVII-50-4 p-I-Ph H H CH2CH(CH3) 2 Bz F F F OH H H XVII-50-5 p-I-Ph H H CH 2Ph Bz F F F OH H H XVII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz F F F OH H H XVII-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz F F F OH H H XVII-50-8 p-I-Ph * H * Bz F F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'IA _

R8 NH

R2 0 R3b R R N P- 0 N 0

C0 2R 4 ORR6

Y X

XVII Table XVII-1. No R R2 R3 a R3 b R4 R' R6 X Y R7 R' XVII-1-1 CH 3 H H H CH 3 F H F OH H H XVII-1-2 CH 3 H H CH3 CH 3 F H F OH H H XVII-1-3 CH 3 H H CH(CH 3)2 CH 3 F H F OH H H XVII-1-4 CH 3 H H CH2CH(CH 3) 2 CH 3 F H F OH H H XVII-1-5 CH 3 H H CH 2Ph CH 3 F H F OH H H XVII-1-6 CH 3 H H CH 2-indol-3-yl CH 3 F H F OH H H XVII-1-7 CH 3 H H CH2 CH 2 SCH 3 CH 3 F H F OH H H XVII-1-8 CH 3 * H * CH 3 F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-2. No R R2 R3a R3b R4 R' R6 X Y R7 R' XVII-2-1 Et H H H CH 3 F H F OH H H XVII-2-2 Et H H CH3 CH 3 F H F OH H H XVII-2-3 Et H H CH(CH 3)2 CH 3 F H F OH H H XVII-2-4 Et H H CH2CH(CH 3) 2 CH 3 F H F OH H H XVII-2-5 Et H H CH 2Ph CH 3 F H F OH H H XVII-2-6 Et H H CH 2-indol-3-yl CH 3 F H F OH H H XVII-2-7 Et H H CH2CH 2SCH 3 CH 3 F H F OH H H XVII-2-8 Et * H * CH 3 F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

SIA')-

Table XVII-3. 3 No R' R2 R3 aR R4 R' R X Y R7 R' XVII-3-1 'Pr H H H CH3 F H F OH H H XVII-3-2 'Pr H H CH 3 CH3 F H F OH H H XVII-3-3 'Pr H H CH(CH3) 2 CH3 F H F OH H H XVII-3-4 Pr H H CH 2CH(CH3) 2 CH3 F H F OH H H XVII-3-5 Pr H H CH 2Ph CH3 F H F OH H H XVII-3-6 Pr H H CH 2-indol-3-yl CH3 F H F OH H H XVII-3-7 Pr H H CH 2 CH2 SCH 3 CH3 F H F OH H H XVII-3-8 Pr * H * CH3 F H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-4. No R1 R2 R3a Rb 3 R4 R R6 X Y R7 R' XVII-4-1 'Bu H H H CH 3 F H F OH H H XVII-4-2 'Bu H H CH3 CH 3 F H F OH H H XVII-4-3 'Bu H H CH(CH3) 2 CH 3 F H F OH H H XVII-4-4 'Bu H H CH2 CH(CH3)2 CH 3 F H F OH H H XVII-4-5 'Bu H H CH2Ph CH 3 F H F OH H H XVII-4-6 'Bu H H CH2-indol-3-yl CH 3 F H F OH H H XVII-4-7 'Bu H H CH2 CH2 SCH 3 CH 3 F H F OH H H XVII-4-8 'Bu * H * CH 3 F H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-5. RI 1 R 2 R 3 a R3 b R4 R 5 R 6 X Y R7 R' No XVII-5-1 Ph H H H CH 3 F H F OH H H XVII-5-2 Ph H H CH3 CH3 F H F OH H H XVII-5-3 Ph H H CH(CH3) 2 CH3 F H F OH H H XVII-5-4 Ph H H CH2CH(CH3)2 CH 3 F H F OH H H XVII-5-5 Ph H H CH 2Ph CH 3 F H F OH H H XVII-5-6 Ph H H CH 2-indol-3-yl CH3 F H F OH H H XVII-5-7 Ph H H CH2CH2SCH 3 CH3 F H F OH H H XVII-5-8 Ph * H * CH 3 F H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2,12-

Table XVII-6. No R RR 3 a R3b R4 R' R6 X Y R7 R' XVII-6-1 p-Me-Ph H H H CH 3 F H F OH H H XVII-6-2 p-Me-Ph H H CH 3 CH3 F H F OH H H XVII-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 F H F OH H H XVII-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH 3 F H F OH H H XVII-6-5 p-Me-Ph H H CH 2Ph CH 3 F H F OH H H XVII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 F H F OH H H XVII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH3 F H F OH H H XVII-6-8 p-Me-Ph * H * CH 3 F H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-7. N9 R1 R2 R3 a R R4 R R6 X Y R7 R' XVII-7-1 p-F-Ph H H H CH 3 F H F OH H H XVII-7-2 p-F-Ph H H CH 3 CH 3 F H F OH H H XVII-7-3 p-F-Ph H H CH(CH 3)2 CH 3 F H F OH H H XVII-7-4 p-F-Ph H H CH 2CH(CH 3) 2 CH 3 F H F OH H H XVII-7-6 p-F-Ph H H CH 2Ph CH 3 F H F OH H H XVII-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 F H F OH H H XVII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH 3 F H F OH H H XVII-7-20 p-F-Ph * H * CH 3 F H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-8. 6 No R R2 R 3 a R3b R4 R R X Y R7 R' XVII-8-1 p-Cl-Ph H H H CH 3 F H F OH H H XVII-8-2 p-Cl-Ph H H CH 3 CH 3 F H F OH H H XVII-8-3 p-Cl-Ph H H CH(CH 3)2 CH 3 F H F OH H H XVII-8-4 p-Cl-Ph H H CH 2CH(CH 3)2 CH 3 F H F OH H H XVII-8-5 p-Cl-Ph H H CH 2Ph CH 3 F H F OH H H XVII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 F H F OH H H XVII-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 F H F OH H H XVII-8-8 p-Cl-Ph * H * CH 3 F H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'I ~AA

Table XVII-9. No R R2 R 3 a R 3b R4 R' R6 X Y R7 R' XVII-9-1 p-Br-Ph H H H CH3 F H F OH H H XVII-9-2 p-Br-Ph H H CH 3 CH3 F H F OH H H XVII-9-3 p-Br-Ph H H CH(CH3)2 CH3 F H F OH H H XVII-9-4 p-Br-Ph H H CH 2CH(CH 3)2 CH3 F H F OH H H XVII-9-6 p-Br-Ph H H CH 2Ph CH3 F H F OH H H XVII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 F H F OH H H XVII-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH3 F H F OH H H XVII-9-20 p-Br-Ph * H * CH 3 F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-10. N9 R1 R2 R3 a RS R4 R R6 X Y R7 R' XVII-10-1 p-I-Ph H H H CH 3 F H F OH H H XVII-10-2 p-I-Ph H H CH 3 CH 3 F H F OH H H XVII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 F H F OH H H XVII-10-4 p-I-Ph H H CH 2CH(CH 3) 2 CH 3 F H F OH H H XVII-10-5 p-I-Ph H H CH 2Ph CH 3 F H F OH H H XVII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 F H F OH H H XVII-10-7 p-I-Ph H H CH 2CH2SCH 3 CH 3 F H F OH H H XVII-10-8 p-I-Ph * H * CH 3 F H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-11. No R1 R2 R3 a R 3b R4 R 5 R6 X Y R7 R' XVII-11-1 CH 3 H H H Et F H F OH H H XVII-11-2 CH 3 H H CH3 Et F H F OH H H XVII-11-3 CH 3 H H CH(CH3)2 Et F H F OH H H XVII-11-4 CH 3 H H CH2CH(CH3) 2 Et F H F OH H H XVII-11-5 CH 3 H H CH 2Ph Et F H F OH H H XVII-11-6 CH 3 H H CH 2-indol-3-yl Et F H F OH H H XVII-11-7 CH 3 H H CH2CH 2SCH 3 Et F H F OH H H XVII-11-8 CH 3 * H * Et F H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2IA r,

Table XVII-12. No Rl R2 R3 a R 3b R4 R' R6 X Y R7 R' XVII-12-1 Et H H H Et F H F OH H H XVII-12-2 Et H H CH3 Et F H F OH H H XVII-12-3 Et H H CH(CH3)2 Et F H F OH H H XVII-12-4 Et H H CH2CH(CH3) 2 Et F H F OH H H XVII-12-5 Et H H CH 2Ph Et F H F OH H H XVII-12-6 Et H H CH 2-indol-3-yl Et F H F OH H H XVII-12-7 Et H H CH2CH2 SCH3 Et F H F OH H H XVII-12-8 Et * H * Et F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-13. N9 R' R2 R3 a R3 b R4 R R 6 X Y R7 R' XVII-13-1 'Pr H H H Et F H F OH H H XVII-13-2 'Pr H H CH 3 Et F H F OH H H XVII-13-3 'Pr H H CH(CH3) 2 Et F H F OH H H XVII-13-4 'Pr H H CH 2CH(CH3)2 Et F H F OH H H XVII-13-5 'Pr H H CH 2Ph Et F H F OH H H XVII-13-6 'Pr H H CH 2-indol-3-yl Et F H F OH H H XVII-13-7 'Pr H H CH 2CH 2SCH 3 Et F H F OH H H XVII-13-8 'Pr * H * Et F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-14. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R XVII-14-1 'Bu H H H Et F H F OH H H XVII-14-2 'Bu H H CH 3 Et F H F OH H H XVII-14-3 'Bu H H CH(CH3) 2 Et F H F OH H H XVII-14-4 'Bu H H CH 2CH(CH3)2 Et F H F OH H H XVII-14-5 'Bu H H CH 2Ph Et F H F OH H H XVII-14-6 'Bu H H CH 2-indol-3-yl Et F H F OH H H XVII-14-7 'Bu H H CH 2CH2SCH 3 Et F H F OH H H XVII-14-8 'Bu * H * Et F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'IAA-,

Table XVII-15. No R1 R2 R3 a R3 R4 R 5 R' X Y R7 R' XVII-15-1 Ph H H H Et F H F OH H H XVII-15-2 Ph H H CH3 Et F H F OH H H XVII-15-3 Ph H H CH(CH3) 2 Et F H F OH H H XVII-15-4 Ph H H CH2CH(CH3)2 Et F H F OH H H XVII-15-5 Ph H H CH 2Ph Et F H F OH H H XVII-15-6 Ph H H CH 2-indol-3-yl Et F H F OH H H XVII-15-7 Ph H H CH2CH2SCH 3 Et F H F OH H H XVII-15-8 Ph * H * Et F H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-16. N9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' XVII-16-1 p-Me-Ph H H H Et F H F OH H H XVII-16-2 p-Me-Ph H H CH 3 Et F H F OH H H XVII-16-3 p-Me-Ph H H CH(CH3) 2 Et F H F OH H H XVII-16-4 p-Me-Ph H H CH 2CH(CH 3) 2 Et F H F OH H H XVII-16-5 p-Me-Ph H H CH 2Ph Et F H F OH H H XVII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et F H F OH H H XVII-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et F H F OH H H XVII-16-8 p-Me-Ph * H * Et F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-17. No R R2 R 3 a R3b R4 R6 X Y R7 R' XVII-17-1 p-F-Ph H H H Et F H F OH H H XVII-17-2 p-F-Ph H H CH 3 Et F H F OH H H XVII-17-3 p-F-Ph H H CH(CH3) 2 Et F H F OH H H XVII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et F H F OH H H XVII-17-5 p-F-Ph H H CH 2Ph Et F H F OH H H XVII-17-6 p-F-Ph H H CH 2-indol-3-yl Et F H F OH H H XVII-17-7 p-F-Ph H H CH 2CH2SCH 3 Et F H F OH H H XVII-17-8 p-F-Ph * H * Et F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'IA17-

Table XVII-18. No R R2 R 3 a R 3b R4 R 5 R6 X Y R7 R' XVII-18-1 p-Cl-Ph H H H Et F H F OH H H XVII-18-2 p-Cl-Ph H H CH 3 Et F H F OH H H XVII-18-3 p-Cl-Ph H H CH(CH3) 2 Et F H F OH H H XVII-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et F H F OH H H XVII-18-5 p-Cl-Ph H H CH 2Ph Et F H F OH H H XVII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et F H F OH H H XVII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et F H F OH H H XVII-18-8 p-Cl-Ph * H * Et F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-19. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y R7 R' XVII-19-1 p-Br-Ph H H H Et F H F OH H H XVII-19-2 p-Br-Ph H H CH 3 Et F H F OH H H XVII-19-3 p-Br-Ph H H CH(CH3)2 Et F H F OH H H XVII-19-4 p-Br-Ph H H CH 2CH(CH 3)2 Et F H F OH H H XVII-19-5 p-Br-Ph H H CH 2Ph Et F H F OH H H XVII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et F H F OH H H XVII-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et F H F OH H H XVII-19-8 p-Br-Ph * H * Et F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-20. No R R2 R 3 a R 3b R4 R6 X Y R7 R' XVII-20-1 p-I-Ph H H H Et F H F OH H H XVII-20-2 p-I-Ph H H CH 3 Et F H F OH H H XVII-20-3 p-I-Ph H H CH(CH3) 2 Et F H F OH H H XVII-20-4 p-I-Ph H H CH 2CH(CH3)2 Et F H F OH H H XVII-20-5 p-I-Ph H H CH 2Ph Et F H F OH H H XVII-20-6 p-I-Ph H H CH 2-indol-3-yl Et F H F OH H H XVII-20-7 p-I-Ph H H CH 2CH2SCH 3 Et F H F OH H H XVII-20-8 p-I-Ph * H * Et F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'IA Q

Table XVII-21. No R1 R2 R3 a R 3b R4 R' R6 X Y R7 R' XVII-21-1 CH 3 H H H 'Pr F H F OH H H XVII-21-2 CH 3 H H CH3 'Pr F H F OH H H XVII-21-3 CH 3 H H CH(CH 3) 2 'Pr F H F OH H H XVII-21-4 CH 3 H H CH2CH(CH3) 2 'Pr F H F OH H H XVII-21-5 CH 3 H H CH 2Ph 'Pr F H F OH H H XVII-21-6 CH 3 H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-21-7 CH 3 H H CH2CH 2SCH 3 'Pr F H F OH H H XVII-21-8 CH 3 * H * 'Pr F H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-22. N R1 RR 2 R3 a R3 b R4 R' R6 X Y R7 R' XVII-22-1 Et H H H 'Pr F H F OH H H XVII-22-2 Et H H CH3 'Pr F H F OH H H XVII-22-3 Et H H CH(CH 3) 2 'Pr F H F OH H H XVII-22-4 Et H H CH2CH(CH3) 2 'Pr F H F OH H H XVII-22-5 Et H H CH 2Ph 'Pr F H F OH H H XVII-22-6 Et H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-22-7 Et H H CH2CH2 SCH3 'Pr F H F OH H H XVII-22-8 Et * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-23. R2 R3 a R 3b 4 R 6 X Y R7 R' No R' R XVII-23-1 'Pr H H H 'Pr F H F OH H H XVII-23-2 'Pr H H CH 3 'Pr F H F OH H H XVII-23-3 'Pr H H CH(CH 3)2 'Pr F H F OH H H XVII-23-4 'Pr H H CH 2CH(CH3) 2 'Pr F H F OH H H XVII-23-5 Pr H H CH 2Ph 'Pr F H F OH H H XVII-23-6 Pr H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-23-7 Pr H H CH 2CH 2SCH 3 'Pr F H F OH H H XVII-23-8 Pr * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_u0

Table XVII-24. No R' R2 R3 a R3b R4 R R X Y R7 R' XVII-24-1 'Bu H H H 'Pr F H F OH H H XVII-24-2 'Bu H H CH 3 'Pr F H F OH H H XVII-24-3 'Bu H H CH(CH 3)2 'Pr F H F OH H H XVII-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr F H F OH H H XVII-24-5 'Bu H H CH 2Ph 'Pr F H F OH H H XVII-24-6 'Bu H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-24-7 'Bu H H CH 2CH2SCH 3 'Pr F H F OH H H XVII-24-8 'Bu * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-25. No R1 R2 R3 a RS R4 R 5 R6 X Y R7 R' XVII-25-1 Ph H H H 'Pr F H F OH H H XVII-25-2 Ph H H CH3 'Pr F H F OH H H XVII-25-3 Ph H H CH(CH3) 2 'Pr F H F OH H H XVII-25-4 Ph H H CH2CH(CH 3) 2 'Pr F H F OH H H XVII-25-5 Ph H H CH 2Ph 'Pr F H F OH H H XVII-25-6 Ph H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-25-7 Ph H H CH2CH2SCH 3 'Pr F H F OH H H XVII-25-8 Ph * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-26. No R R2 R 3 a R3 R4 R 5 R6 X Y R7 R' XVII-26-1 p-Me-Ph H H H 'Pr F H F OH H H XVII-26-2 p-Me-Ph H H CH 3 'Pr F H F OH H H XVII-26-3 p-Me-Ph H H CH(CH3) 2 'Pr F H F OH H H XVII-26-4 p-Me-Ph H H CH 2CH(CH 3) 2 'Pr F H F OH H H XVII-26-5 p-Me-Ph H H CH 2Ph 'Pr F H F OH H H XVII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr F H F OH H H XVII-26-8 p-Me-Ph * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-27. No R R2 R 3 a R3 R4 R R' X Y R7 R' XVII-27-1 p-F-Ph H H H 'Pr F H F OH H H XVII-27-2 p-F-Ph H H CH 3 'Pr F H F OH H H XVII-27-3 p-F-Ph H H CH(CH3) 2 'Pr F H F OH H H XVII-27-4 p-F-Ph H H CH 2CH(CH3)2 'Pr F H F OH H H XVII-27-5 p-F-Ph H H CH 2Ph 'Pr F H F OH H H XVII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr F H F OH H H XVII-27-8 p-F-Ph * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-28. N9 R1 R2 R3 a R3 b R4 R 5 R6 X Y R7 R' XVII-28-1 p-Cl-Ph H H H 'Pr F H F OH H H XVII-28-2 p-Cl-Ph H H CH 3 'Pr F H F OH H H XVII-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr F H F OH H H XVII-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr F H F OH H H XVII-28-5 p-Cl-Ph H H CH 2Ph 'Pr F H F OH H H XVII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr F H F OH H H XVII-28-8 p-Cl-Ph * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-29. No R R2 R 3 a R 3b R4 R5 R6 X Y R7 R' XVII-29-1 p-Br-Ph H H H 'Pr F H F OH H H XVII-29-2 p-Br-Ph H H CH 3 'Pr F H F OH H H XVII-29-3 p-Br-Ph H H CH(CH3)2 'Pr F H F OH H H XVII-29-4 p-Br-Ph H H CH 2CH(CH3) 2 'Pr F H F OH H H XVII-29-5 p-Br-Ph H H CH 2Ph 'Pr F H F OH H H XVII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr F H F OH H H XVII-29-8 p-Br-Ph * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

2;1 -

Table XVII-30. No R1 R 2 R3 a R 3b R4 RR X Y R7 R' XVII-30-1 p-I-Ph H H H 'Pr F H F OH H H XVII-30-2 p-I-Ph H H CH 3 'Pr F H F OH H H XVII-30-3 p-I-Ph H H CH(CH3) 2 'Pr F H F OH H H XVII-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr F H F OH H H XVII-30-5 p-I-Ph H H CH 2Ph 'Pr F H F OH H H XVII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr F H F OH H H XVII-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr F H F OH H H XVII-30-8 p-I-Ph * H * 'Pr F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-31. No R1 R2 R3a R3 b R4 R' R6 X Y R7 R' XVII-31-1 CH 3 H H H "Bu F H F OH H H XVII-31-2 CH 3 H H CH3 "Bu F H F OH H H XVII-31-3 CH 3 H H CH(CH3)2 "Bu F H F OH H H XVII-31-4 CH 3 H H CH2CH(CH3) 2 "Bu F H F OH H H XVII-31-5 CH 3 H H CH 2Ph "Bu F H F OH H H XVII-31-6 CH 3 H H CH 2-indol-3-yl "Bu F H F OH H H XVII-31-7 CH 3 H H CH2CH 2SCH 3 "Bu F H F OH H H XVII-31-8 CH 3 * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-32. No Rl R2 R3a R3 b R4 R 5 R6 X Y R7 R' XVII-32-1 Et H H H "Bu F H F OH H H XVII-32-2 Et H H CH3 "Bu F H F OH H H XVII-32-3 Et H H CH(CH3)2 "Bu F H F OH H H XVII-32-4 Et H H CH2CH(CH3) 2 "Bu F H F OH H H XVII-32-5 Et H H CH 2Ph "Bu F H F OH H H XVII-32-6 Et H H CH 2-indol-3-yl "Bu F H F OH H H XVII-32-7 Et H H CH2CH2 SCH3 "Bu F H F OH H H XVII-32-8 Et * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2Vr)-

Table XVII-33. R' 3 No R2 R3 aR R4 R R' X Y R7 R' XVII-33-1 'Pr H H H "Bu F H F OH H H XVII-33-2 'Pr H H CH 3 "Bu F H F OH H H XVII-33-3 'Pr H H CH(CH3) 2 "Bu F H F OH H H XVII-33-4 Pr H H CH 2CH(CH3) 2 "Bu F H F OH H H XVII-33-5 Pr H H CH 2Ph "Bu F H F OH H H XVII-33-6 Pr H H CH 2-indol-3-yl "Bu F H F OH H H XVII-33-7 Pr H H CH 2CH 2SCH 3 "Bu F H F OH H H XVII-33-8 Pr * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-34. No R1 R2 R3a R3b R4 R R6 X Y R7 R' XVII-34-1 'Bu H H H "Bu F H F OH H H XVII-34-2 'Bu H H CH 3 "Bu F H F OH H H XVII-34-3 'Bu H H CH(CH 3 )2 "Bu F H F OH H H XVII-34-4 'Bu H H CH 2 CH(CH3)2 "Bu F H F OH H H XVII-34-5 'Bu H H CH 2 Ph "Bu F H F OH H H XVII-34-6 'Bu H H CH 2-indol-3-yl "Bu F H F OH H H XVII-34-7 'Bu H H CH 2 CH 2 SCH 3 "Bu F H F OH H H XVII-34-8 'Bu * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-35. No RI 1 R2 R3a R3b R4 R 5 R6 X Y R7 R' XVII-35-1 Ph H H H "Bu F H F OH H H XVII-35-2 Ph H H CH3 "Bu F H F OH H H XVII-35-3 Ph H H CH(CH3) 2 "Bu F H F OH H H XVII-35-4 Ph H H CH2CH(CH3)2 "Bu F H F OH H H XVII-35-5 Ph H H CH 2Ph "Bu F H F OH H H XVII-35-6 Ph H H CH 2-indol-3-yl "Bu F H F OH H H XVII-35-7 Ph H H CH2CH2 SCH 3 "Bu F H F OH H H XVII-35-8 Ph * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-36. No R R 2 R3 a R 3b R4 R' R6 X Y R7 R' XVII-36-1 p-Me-Ph H H H "Bu F H F OH H H XVII-36-2 p-Me-Ph H H CH 3 "Bu F H F OH H H XVII-36-3 p-Me-Ph H H CH(CH3) 2 "Bu F H F OH H H XVII-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu F H F OH H H XVII-36-5 p-Me-Ph H H CH 2Ph "Bu F H F OH H H XVII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu F H F OH H H XVII-36-7 p-Me-Ph H H CH 2CH 2 SCH 3 "Bu F H F OH H H XVII-36-8 p-Me-Ph * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-37. No R1 R2 RaR 3 b R4 R' R6 X Y R7 R'

XVII-37-1 p-F-Ph H H H "Bu F H F OH H H XVII-37-2 p-F-Ph H H CH 3 "Bu F H F OH H H XVII-37-3 p-F-Ph H H CH(CH 3 )2 "Bu F H F OH H H XVII-37-4 p-F-Ph H H CH 2 CH(CH 3) 2 "Bu F H F OH H H XVII-37-5 p-F-Ph H H CH 2 Ph "Bu F H F OH H H XVII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu F H F OH H H XVII-37-7 p-F-Ph H H CH 2 CH 2 SCH 3 "Bu F H F OH H H XVII-37-8 p-F-Ph * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-38. No R R 2 R 3 a R 3b R4 R5 R 6 X Y R7 R' XVII-38-1 p-Cl-Ph H H H "Bu F H F OH H H XVII-38-2 p-Cl-Ph H H CH 3 "Bu F H F OH H H XVII-38-3 p-Cl-Ph H H CH(CH 3) 2 "Bu F H F OH H H XVII-38-4 p-Cl-Ph H H CH 2 CH(CH 3) 2 "Bu F H F OH H H XVII-38-5 p-Cl-Ph H H CH 2Ph "Bu F H F OH H H XVII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu F H F OH H H XVII-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu F H F OH H H XVII-38-8 p-Cl-Ph * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-39. No R R2 R3a R 3b R4 R' R6 X Y R7 R' XVII-39-1 p-Br-Ph H H H "Bu F H F OH H H XVII-39-2 p-Br-Ph H H CH 3 "Bu F H F OH H H XVII-39-3 p-Br-Ph H H CH(CH 3) 2 "Bu F H F OH H H XVII-39-4 p-Br-Ph H H CH 2CH(CH3) 2 "Bu F H F OH H H XVII-39-5 p-Br-Ph H H CH 2Ph "Bu F H F OH H H XVII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu F H F OH H H XVII-39-7 p-Br-Ph H H CH 2CH 2 SCH 3 "Bu F H F OH H H XVII-39-8 p-Br-Ph * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-40. N9 R1 R2 R3a RS R4 R R6 X Y R7 R' XVII-40-1 p-I-Ph H H H "Bu F H F OH H H XVII-40-2 p-I-Ph H H CH 3 "Bu F H F OH H H XVII-40-3 p-I-Ph H H CH(CH3) 2 "Bu F H F OH H H XVII-40-4 p-I-Ph H H CH 2CH(CH 3) 2 "Bu F H F OH H H XVII-40-5 p-I-Ph H H CH 2Ph "Bu F H F OH H H XVII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu F H F OH H H XVII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu F H F OH H H XVII-40-8 p-I-Ph * H * "Bu F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-41. No R1 R2 R3 a R 3b R4 R 5 R6 X Y R7 R' XVII-41-1 CH 3 H H H Bz F H F OH H H XVII-41-2 CH 3 H H CH3 Bz F H F OH H H XVII-41-3 CH 3 H H CH(CH3)2 Bz F H F OH H H XVII-41-4 CH 3 H H CH2CH(CH3) 2 Bz F H F OH H H XVII-41-5 CH 3 H H CH 2Ph Bz F H F OH H H XVII-41-6 CH 3 H H CH 2-indol-3-yl Bz F H F OH H H XVII-41-7 CH 3 H H CH2CH 2SCH 3 Bz F H F OH H H XVII-41-8 CH 3 * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

11 , r

Table XVII-42. 5 No Rl R 2 R 3a R 3b R4 R R' X Y R7 R' XVII-42-1 Et H H H Bz F H F OH H H XVII-42-2 Et H H CH3 Bz F H F OH H H XVII-42-3 Et H H CH(CH3)2 Bz F H F OH H H XVII-42-4 Et H H CH2CH(CH3) 2 Bz F H F OH H H XVII-42-5 Et H H CH 2Ph Bz F H F OH H H XVII-42-6 Et H H CH 2-indol-3-yl Bz F H F OH H H XVII-42-7 Et H H CH2CH2 SCH3 Bz F H F OH H H XVII-42-8 Et * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-43. 6 No R' R2 R3 a R3 b R4 R R X Y R7 R' XVII-43-1 'Pr H H H Bz F H F OH H H XVII-43-2 'Pr H H CH 3 Bz F H F OH H A XVII-43-3 'Pr H H CH(CH3) 2 Bz F H F OH H H XVII-43-4 'Pr H H CH 2CH(CH 3) 2 Bz F H F OH H H XVII-43-5 'Pr H H CH 2Ph Bz F H F OH H H XVII-43-6 'Pr H H CH 2-indol-3-yl Bz F H F OH H H XVII-43-7 'Pr H H CH 2CH 2SCH 3 Bz F H F OH H H XVII-43-8 'Pr * H * Bz F H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-44. R R2 R 3 a R3 b R4 R R 6 X Y R7 R' No XVII-44-1 'Bu H H H Bz F H F OH H H XVII-44-2 'Bu H H CH 3 Bz F H F OH H H XVII-44-3 'Bu H H CH(CH3) 2 Bz F H F OH H H XVII-44-4 'Bu H H CH 2CH(CH3)2 Bz F H F OH H H XVII-44-5 'Bu H H CH 2Ph Bz F H F OH H H XVII-44-6 'Bu H H CH 2-indol-3-yl Bz F H F OH H H XVII-44-7 'Bu H H CH 2CH2SCH 3 Bz F H F OH H H XVII-44-8 'Bu * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-45. No R1 R2 R3 a R3 R4 R5 R 6 X Y R7 R' XVII-45-1 Ph H H H Bz F H F OH H H XVII-45-2 Ph H H CH3 Bz F H F OH H H XVII-45-3 Ph H H CH(CH3) 2 Bz F H F OH H H XVII-45-4 Ph H H CH2CH(CH3)2 Bz F H F OH H H XVII-45-5 Ph H H CH 2Ph Bz F H F OH H H XVII-45-6 Ph H H CH 2-indol-3-yl Bz F H F OH H H XVII-45-7 Ph H H CH2CH2SCH 3 Bz F H F OH H H XVII-45-8 Ph * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-46. N9 R1 R2 R3 a R3 b R4 R R X Y R7 R' XVII-46-1 p-Me-Ph H H H Bz F H F OH H H XVII-46-2 p-Me-Ph H H CH 3 Bz F H F OH H H XVII-46-3 p-Me-Ph H H CH(CH3) 2 Bz F H F OH H H XVII-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz F H F OH H H XVII-46-5 p-Me-Ph H H CH 2Ph Bz F H F OH H H XVII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz F H F OH H H XVII-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz F H F OH H H XVII-46-8 p-Me-Ph * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-47. No R R2 R 3 a R3 R4 R5 R 6 X Y R7 R' XVII-47-1 p-F-Ph H H H Bz F H F OH H H XVII-47-2 p-F-Ph H H CH 3 Bz F H F OH H H XVII-47-3 p-F-Ph H H CH(CH3) 2 Bz F H F OH H H XVII-47-4 p-F-Ph H H CH 2CH(CH3)2 Bz F H F OH H H XVII-47-5 p-F-Ph H H CH 2Ph Bz F H F OH H H XVII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz F H F OH H H XVII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz F H F OH H H XVII-47-8 p-F-Ph * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVII-48. No R R2 R 3 a R 3b R4 R' R' X Y R7 R' XVII-48-1 p-Cl-Ph H H H Bz F H F OH H H XVII-48-2 p-Cl-Ph H H CH 3 Bz F H F OH H H XVII-48-3 p-Cl-Ph H H CH(CH3) 2 Bz F H F OH H H XVII-48-4 p-Cl-Ph H H CH 2CH(CH3) 2 Bz F H F OH H H XVII-48-5 p-Cl-Ph H H CH 2Ph Bz F H F OH H H XVII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz F H F OH H H XVII-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz F H F OH H H XVII-48-8 p-Cl-Ph * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-49. 5 N9 R1 R2 R 3 a R3 b R4 R R6 X Y R7 R' XVII-49-1 p-Br-Ph H H H Bz F H F OH H H XVII-49-2 p-Br-Ph H H CH 3 Bz F H F OH H H XVII-49-3 p-Br-Ph H H CH(CH3)2 Bz F H F OH H H XVII-49-4 p-Br-Ph H H CH 2CH(CH 3)2 Bz F H F OH H H XVII-49-5 p-Br-Ph H H CH 2Ph Bz F H F OH H H XVII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz F H F OH H H XVII-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz F H F OH H H XVII-49-8 p-Br-Ph * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVII-50. No R R2 R 3 a R3 R4 R5 R 6 X Y R7 R' XVII-50-1 p-I-Ph H H H Bz F H F OH H H XVII-50-2 p-I-Ph H H CH 3 Bz F H F OH H H XVII-50-3 p-I-Ph H H CH(CH3) 2 Bz F H F OH H H XVII-50-4 p-I-Ph H H CH 2CH(CH3)2 Bz F H F OH H H XVII-50-5 p-I-Ph H H CH 2Ph Bz F H F OH H H XVII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz F H F OH H H XVII-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz F H F OH H H XVII-50-8 p-I-Ph * H * Bz F H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R8 NH

R2 0 R3b R R 0 3a 0 N O1 0 t

CO2R4 OR 5R6

Y X XVIII

Table XVIII-1. No R1 R2 R 3a R 3b R4 R' R6 X Y R7 R8 XVIII-1-1 CH 3 H H H CH 3 OCH 3 F H OH H H XVIII-1-2 CH 3 H H CH3 CH 3 OCH 3 F H OH H H XVIII-1-3 CH 3 H H CH(CH3)2 CH 3 OCH 3 F H OH H H XVIII-1-4 CH 3 H H CH2CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-1-5 CH 3 H H CH 2Ph CH 3 OCH 3 F H OH H H XVIII-1-6 CH 3 H H CH 2-indol-3-yl CH 3 OCH 3 F H OH H H XVIII-1-7 CH 3 H H CH2 CH 2 SCH 3 CH 3 OCH 3 F H OH H H XVIII-1-8 CH 3 * H * CH 3 OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-2. 8 1 RI R2 R3a R3b R4 R5 R6 X Y R7 R XVIII-2-1 Et H H H CH 3 OCH 3 F H OH H H XVIII-2-2 Et H H CH 3 CH 3 OCH 3 F H OH H H XVIII-2-3 Et H H CH(CH3)2 CH 3 OCH 3 F H OH H H XVIII-2-4 Et H H CH 2CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-2-5 Et H H CH 2Ph CH 3 OCH 3 F H OH H H XVIII-2-6 Et H H CH 2-indol-3-yl CH 3 OCH 3 F H OH H H XVIII-2-7 Et H H CH 2CH 2SCH 3 CH 3 OCH 3 F H OH H H XVIII-2-8 Et * H * CH 3 OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2;Q-o

Table XVIII-3. R' R2 R3 3 R4 R R 6 X Y R7 R' No aR

XVIII-3-1 'Pr H H H CH 3 OCH 3 F H OH H H XVIII-3-2 'Pr H H CH3 CH 3 OCH 3 F H OH H H XVIII-3-3 'Pr H H CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-3-4 Pr H H CH2CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-3-5 Pr H H CH2Ph CH 3 OCH 3 F H OH H H XVIII-3-6 Pr H H CH2-indol-3-yl CH 3 OCH 3 F H OH H H XVIII-3-7 Pr H H CH2 CH2 SCH 3 CH 3 OCH 3 F H OH H H XVIII-3-8 Pr * H * CH 3 OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-4. N RI R 2 R3a R R4 R' R6 X Y R7 R XVIII-4-1 'Bu H H H CH3 OCH 3 F H OH H H XVIII-4-2 'Bu H H CH 3 CH3 OCH 3 F H OH H H XVIII-4-3 'Bu H H CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-4-4 'Bu H H CH 2CH(CH3)2 CH 3 OCH 3 F H OH H H XVIII-4-5 'Bu H H CH 2Ph CH3 OCH 3 F H OH H H XVIII-4-6 'Bu H H CH 2-indol-3-yl CH 3 OCH 3 F H OH H H XVIII-4-7 'Bu H H CH 2 CH 2 SCH 3 CH 3 OCH 3 F H OH H H XVIII-4-8 'Bu * H * CH3 OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-5. No RI 1 R2 R 3a R 3b R4 R5 RX Y R7 R 8 XVIII-5-1 Ph H H H CH3 OCH 3 F H OH H H XVIII-5-2 Ph H H CH3 CH3 OCH 3 F H OH H H XVIII-5-3 Ph H H CH(CH3) 2 CH3 OCH 3 F H OH H H XVIII-5-4 Ph H H CH2CH(CH3)2 CH3 OCH 3 F H OH H H XVIII-5-5 Ph H H CH 2Ph CH3 OCH 3 F H OH H H XVIII-5-6 Ph H H CH 2-indol-3-yl CH3 OCH 3 F H OH H H XVIII-5-7 Ph H H CH2CH2SCH 3 CH3 OCH 3 F H OH H H XVIII-5-8 Ph * H * CH3 OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-6. R RR 3 R 3b R4 R R6 X Y R7 R8 No a

XVIII-6-1 p-Me-Ph H H H CH3 OCH 3 F H OH H H XVIII-6-2 p-Me-Ph H H CH 3 CH3 OCH 3 F H OH H H XVIII-6-3 p-Me-Ph H H CH(CH3) 2 CH3 OCH 3 F H OH H H XVIII-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH3 OCH 3 F H OH H H XVIII-6-5 p-Me-Ph H H CH 2Ph CH3 OCH 3 F H OH H H XVIII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 OCH 3 F H OH H H XVIII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH3 OCH 3 F H OH H H XVIII-6-8 p-Me-Ph * H * CH3 OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-7. N Rl R2 R3 a R3 bR 4 R' R6 X Y R7 R8

XVIII-7-1 p-F-Ph H H H CH 3 OCH 3 F H OH H H XVIII-7-2 p-F-Ph H H CH 3 CH 3 OCH 3 F H OH H H XVIII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-7-4 p-F-Ph H H CH 2CH(CH 3)2 CH 3 OCH 3 F H OH H H XVIII-7-6 p-F-Ph H H CH 2Ph CH 3 OCH 3 F H OH H H XVIII-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 OCH 3 F H OH H H XVIII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH 3 OCH 3 F H OH H H XVIII-7-20 p-F-Ph * H * CH 3 OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2A1 -

Table XVIII-8. R' No R R2 R 3 a R 3b R4 R' X Y R7 R' XVIII-8-1 p-Cl-Ph H H H CH3 OCH3 F H OH H H XVIII-8-2 p-Cl-Ph H H CH 3 CH 3 OCH3 F H OH H H XVIII-8-3 p-Cl-Ph H H CH(CH 3) 2 CH3 OCH3 F H OH H H XVIII-8-4 p-Cl-Ph H H CH 2CH(CH 3) 2 CH3 OCH3 F H OH H H XVIII-8-5 p-Cl-Ph H H CH 2Ph CH3 OCH3 F H OH H H XVIII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 OCH3 F H OH H H XVIII-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH3 OCH3 F H OH H H XVIII-8-8 p-Cl-Ph * H * CH3 OCH3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-9. No R1 R2 R3 a R3 b R4 R' R6 X Y R7 R' XVIII-9-1 p-Br-Ph H H H CH 3 OCH 3 F H OH H H XVIII-9-2 p-Br-Ph H H CH3 CH3 OCH 3 F H OH H H XVIII-9-3 p-Br-Ph H H CH(CH 3) 2 CH3 OCH 3 F H OH H H XVIII-9-4 p-Br-Ph H H CH2CH(CH 3) 2 CH3 OCH 3 F H OH H H XVIII-9-6 p-Br-Ph H H CH 2Ph CH 3 OCH 3 F H OH H H XVIII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 OCH 3 F H OH H H XVIII-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 OCH 3 F H OH H H XVIII-9-20 p-Br-Ph * H * CH 3 OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-10. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' XVIII-10-1 p-I-Ph H H H CH 3 OCH 3 F H OH H H XVIII-10-2 p-I-Ph H H CH 3 CH 3 OCH 3 F H OH H H XVIII-10-3 p-I-Ph H H CH(CH 3) 2 CH 3 OCH 3 F H OH H H XVIII-10-4 p-I-Ph H H CH 2CH(CH3) 2 CH 3 OCH 3 F H OH H H XVIII-10-5 p-I-Ph H H CH 2Ph CH 3 OCH 3 F H OH H H XVIII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 OCH 3 F H OH H H XVIII-10-7 p-I-Ph H H CH 2CH2SCH 3 CH 3 OCH 3 F H OH H H XVIII-10-8 p-I-Ph * H * CH 3 OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-11. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' XVIII-11-1 CH 3 H H H Et OCH 3 F H OH H H XVIII-11-2 CH 3 H H CH3 Et OCH 3 F H OH H H XVIII-11-3 CH 3 H H CH(CH 3) 2 Et OCH 3 F H OH H H

R' No R R2 R3 a R3 b R4 R6 X Y R7 R' XVIII-11-4 CH 3 H H CH2CH(CH3) 2 Et OCH 3 F H OH H H XVIII-11-5 CH 3 H H CH 2Ph Et OCH 3 F H OH H H XVIII-11-6 CH 3 H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-11-7 CH 3 H H CH2CH 2SCH 3 Et OCH 3 F H OH H H XVIII-11-8 CH 3 * H * Et OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2A2-I

Table XVIII-12. Rl R 2 R3 a R3b R4 R' R6 X Y R7 R' No XVIII-12-1 Et H H H Et OCH 3 F H OH H H XVIII-12-2 Et H H CH3 Et OCH 3 F H OH H H XVIII-12-3 Et H H CH(CH3)2 Et OCH 3 F H OH H H XVIII-12-4 Et H H CH2CH(CH3) 2 Et OCH 3 F H OH H H XVIII-12-5 Et H H CH 2Ph Et OCH 3 F H OH H H XVIII-12-6 Et H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-12-7 Et H H CH2CH 2SCH 3 Et OCH 3 F H OH H H XVIII-12-8 Et * H * Et OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-13. R No R R2 R 3 a R3 b R4 R 6 X Y R7 R' XVIII-13-1 'Pr H H H Et OCH 3 F H OH H H XVIII-13-2 'Pr H H CH 3 Et OCH 3 F H OH H H XVIII-13-3 'Pr H H CH(CH3) 2 Et OCH 3 F H OH H H XVIII-13-4 'Pr H H CH 2CH(CH3)2 Et OCH 3 F H OH H H XVIII-13-5 'Pr H H CH 2Ph Et OCH 3 F H OH H H XVIII-13-6 'Pr H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-13-7 'Pr H H CH 2CH2SCH 3 Et OCH 3 F H OH H H XVIII-13-8 'Pr * H * Et OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-14. No R1 R R3 a R 3b R4 R5 R6 X Y R7 R' 2

XVIII-14-1 'Bu H H H Et OCH 3 F H OH H H XVIII-14-2 'Bu H H CH 3 Et OCH 3 F H OH H H XVIII-14-3 'Bu H H CH(CH3) 2 Et OCH 3 F H OH H H XVIII-14-4 'Bu H H CH 2CH(CH3)2 Et OCH 3 F H OH H H XVIII-14-5 'Bu H H CH 2Ph Et OCH 3 F H OH H H XVIII-14-6 'Bu H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-14-7 'Bu H H CH 2CH2SCH 3 Et OCH 3 F H OH H H XVIII-14-8 'Bu * H * Et OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2AA-A

Table XVIII-15. No RI R2 RaR 3 b R4 R 5 R 6 X Y R7 R' XVIII-15-1 Ph H H H Et OCH 3 F H OH H H XVIII-15-2 Ph H H CH 3 Et OCH 3 F H OH H H XVIII-15-3 Ph H H CH(CH3) 2 Et OCH 3 F H OH H H XVIII-15-4 Ph H H CH 2CH(CH3)2 Et OCH 3 F H OH H H XVIII-15-5 Ph H H CH 2Ph Et OCH 3 F H OH H H XVIII-15-6 Ph H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-15-7 Ph H H CH 2CH2SCH 3 Et OCH 3 F H OH H H XVIII-15-8 Ph * H * Et OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-16. Nt R R2 R3a R3 R4 R5 R' X Y R7 R XVIII-16-1 p-Me-Ph H H H Et OCH 3 F H OH H H XVIII-16-2 p-Me-Ph H H CH 3 Et OCH 3 F H OH H H XVIII-16-3 p-Me-Ph H H CH(CH 3) 2 Et OCH 3 F H OH H H XVIII-16-4 p-Me-Ph H H CH 2CH(CH3) 2 Et OCH 3 F H OH H H XVIII-16-5 p-Me-Ph H H CH 2Ph Et OCH 3 F H OH H H XVIII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et OCH 3 F H OH H H XVIII-16-8 p-Me-Ph * H * Et OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-17. No RI 1 R2 R 3a R3 R4 R5 R6 X Y R7 R' XVIII-17-1 p-F-Ph H H H Et OCH 3 F H OH H H XVIII-17-2 p-F-Ph H H CH 3 Et OCH 3 F H OH H H XVIII-17-3 p-F-Ph H H CH(CH3) 2 Et OCH 3 F H OH H H XVIII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et OCH 3 F H OH H H XVIII-17-5 p-F-Ph H H CH 2Ph Et OCH 3 F H OH H H XVIII-17-6 p-F-Ph H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-17-7 p-F-Ph H H CH 2CH2SCH 3 Et OCH 3 F H OH H H XVIII-17-8 p-F-Ph * H * Et OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-18. No RI 1 R2 R 3a R3 b R4 R5 R6 X Y R7 R8

XVIII-18-1 p-Cl-Ph H H H Et OCH 3 F H OH H H XVIII-18-2 p-Cl-Ph H H CH3 Et OCH 3 F H OH H H XVIII-18-3 p-Cl-Ph H H CH(CH 3)2 Et OCH 3 F H OH H H

R No R R2 R 3 a R3 b R4 R X Y R7 R8

XVIII-18-4 p-Cl-Ph H H CH 2CH(CH 3) 2 Et OCH 3 F H OH H H XVIII-18-5 p-Cl-Ph H H CH 2Ph Et OCH 3 F H OH H H XVIII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et OCH 3 F H OH H H XVIII-18-8 p-Cl-Ph * H * Et OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-19. No R R2 R 3 a R3b R4 R' R6 X Y R7 R8

XVIII-19-1 p-Br-Ph H H H Et OCH 3 F H OH H H XVIII-19-2 p-Br-Ph H H CH 3 Et OCH 3 F H OH H H XVIII-19-3 p-Br-Ph H H CH(CH3)2 Et OCH 3 F H OH H H XVIII-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et OCH 3 F H OH H H XVIII-19-5 p-Br-Ph H H CH 2Ph Et OCH 3 F H OH H H XVIII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et OCH 3 F H OH H H XVIII-19-8 p-Br-Ph * H * Et OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-20. R 6 N9 Rl R2 R3 a R3 b R4 R X Y R7 R8

XVIII-20-1 p-I-Ph H H H Et OCH 3 F H OH H H XVIII-20-2 p-I-Ph H H CH 3 Et OCH 3 F H OH H H XVIII-20-3 p-I-Ph H H CH(CH 3) 2 Et OCH 3 F H OH H H XVIII-20-4 p-I-Ph H H CH 2CH(CH3) 2 Et OCH 3 F H OH H H XVIII-20-5 p-I-Ph H H CH 2Ph Et OCH 3 F H OH H H XVIII-20-6 p-I-Ph H H CH 2-indol-3-yl Et OCH 3 F H OH H H XVIII-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et OCH 3 F H OH H H XVIII-20-8 p-I-Ph * H * Et OCH 3 F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-21. No R R2 R 3 a R 3b R4 R5 R 6 X Y R7 R8

XVIII-21-1 CH 3 H H H 'Pr OCH 3 F H OH H H XVIII-21-2 CH 3 H H CH3 'Pr OCH 3 F H OH H H XVIII-21-3 CH3 H H CH(CH 3) 2 'Pr OCH 3 F H OH H H XVIII-21-4 CH3 H H CH2CH(CH3) 2 'Pr OCH 3 F H OH H H XVIII-21-5 CH3 H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-21-6 CH3 H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H

R' No R R2 R3 a R3 b R4 R6 X Y R7 R' XVIII-21-7 CH 3 H H CH2CH 2SCH 3 'Pr OCH 3 F H OH H H XVIII-21-8 CH 3 * H * 'Pr OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

2'Ir7-

Table XVIII-22. R2 R3 a R3b R4 R' R6 X R' No R1 Y R7 XVIII-22-1 Et H H H 'Pr OCH 3 F H OH H H XVIII-22-2 Et H H CH3 'Pr OCH 3 F H OH H H XVIII-22-3 Et H H CH(CH 3) 2 'Pr OCH 3 F H OH H H XVIII-22-4 Et H H CH2CH(CH 3) 2 'Pr OCH 3 F H OH H H XVIII-22-5 Et H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-22-6 Et H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H XVIII-22-7 Et H H CH2CH 2SCH 3 'Pr OCH 3 F H OH H H XVIII-22-8 Et * H * 'Pr OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-23. No R1 R2 R3 a R3 b R4 R R6 X Y R7 R8

XVIII-23-1 'Pr H H H 'Pr OCH 3 F H OH H H XVIII-23-2 'Pr H H CH 3 'Pr OCH 3 F H OH H H XVIII-23-3 'Pr H H CH(CH 3)2 'Pr OCH 3 F H OH H H XVIII-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr OCH 3 F H OH H H XVIII-23-5 'Pr H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-23-6 'Pr H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H XVIII-23-7 'Pr H H CH 2CH2SCH 3 'Pr OCH 3 F H OH H H XVIII-23-8 'Pr * H * 'Pr OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-24. No R1 R2 R 3a R3b R4 R5 R6 X Y R7 R8

XVIII-24-1 'Bu H H H 'Pr OCH 3 F H OH H H XVIII-24-2 'Bu H H CH 3 'Pr OCH 3 F H OH H H XVIII-24-3 'Bu H H CH(CH 3)2 'Pr OCH 3 F H OH H H XVIII-24-4 'Bu H H CH 2CH(CH 3)2 'Pr OCH 3 F H OH H H XVIII-24-5 'Bu H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-24-6 'Bu H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H XVIII-24-7 'Bu H H CH 2CH2SCH 3 'Pr OCH 3 F H OH H H XVIII-24-8 'Bu * H * 'Pr OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'Ir;S-

Table XVIII-25. No RI R2 RaR 3 b R4 R5 R' X Y R7 R' XVIII-25-1 Ph H H H 'Pr OCH3 F H OH H H XVIII-25-2 Ph H H CH 3 'Pr OCH3 F H OH H H XVIII-25-3 Ph H H CH(CH3) 2 'Pr OCH3 F H OH H H XVIII-25-4 Ph H H CH 2CH(CH3) 2 'Pr OCH3 F H OH H H XVIII-25-5 Ph H H CH 2Ph 'Pr OCH3 F H OH H H XVIII-25-6 Ph H H CH 2-indol-3-yl 'Pr OCH3 F H OH H H XVIII-25-7 Ph H H CH 2CH2SCH 3 'Pr OCH3 F H OH H H XVIII-25-8 Ph * H * 'Pr OCH3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-26. M R1 R2 R3 a R3 b R4 R5 R 6 X Y R7 R' XVIII-26-1 p-Me-Ph H H H 'Pr OCH3 F H OH H H XVIII-26-2 p-Me-Ph H H CH 3 'Pr OCH3 F H OH H H XVIII-26-3 p-Me-Ph H H CH(CH3) 2 'Pr OCH3 F H OH H H XVIII-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr OCH3 F H OH H H XVIII-26-5 p-Me-Ph H H CH 2Ph 'Pr OCH3 F H OH H H XVIII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr OCH3 F H OH H H XVIII-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr OCH3 F H OH H H XVIII-26-8 p-Me-Ph * H * 'Pr OCH3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-27. No RI 1 R2 R 3a R 3b R4 R5 R 6 X Y R7 R XVIII-27-1 p-F-Ph H H H 'Pr OCH 3 F H OH H H XVIII-27-2 p-F-Ph H H CH 3 'Pr OCH 3 F H OH H H XVIII-27-3 p-F-Ph H H CH(CH3) 2 'Pr OCH 3 F H OH H H XVIII-27-4 p-F-Ph H H CH 2CH(CH3)2 'Pr OCH 3 F H OH H H XVIII-27-5 p-F-Ph H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H XVIII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr OCH 3 F H OH H H XVIII-27-8 p-F-Ph * H * 'Pr OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-28. N RI1 R2 R 3a R3 b R4 R5 R6 X Y R7 R XVIII-28-1 p-Cl-Ph H H H 'Pr OCH 3 F H OH H H XVIII-28-2 p-Cl-Ph H H CH3 'Pr OCH 3 F H OH H H XVIII-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr OCH 3 F H OH H H

_0o_

R R2 R 3 R3 b R4 R' R6 X Y R7 R' No a

XVIII-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr OCH 3 F H OH H H XVIII-28-5 p-Cl-Ph H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H XVIII-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr OCH 3 F H OH H H XVIII-28-8 p-Cl-Ph * H * 'Pr OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

'I 'M

Table XVIII-29. R 3 R3b R4 R' R6 X R' No RR a Y R7 XVIII-29-1 p-Br-Ph H H H 'Pr OCH 3 F H OH H H XVIII-29-2 p-Br-Ph H H CH3 'Pr OCH 3 F H OH H H XVIII-29-3 p-Br-Ph H H CH(CH 3) 2 'Pr OCH 3 F H OH H H XVIII-29-4 p-Br-Ph H H CH2CH(CH 3) 2 'Pr OCH 3 F H OH H H XVIII-29-5 p-Br-Ph H H CH 2Ph 'Pr OCH 3 F H OH H H XVIII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F H OH H H XVIII-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr OCH 3 F H OH H H XVIII-29-8 p-Br-Ph * H * 'Pr OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-30. R V R1 R2 R3 a R3 b R4 R6 X Y R7 R' XVIII-30-1 p-I-Ph H H H 'Pr OCH3 F H OH H H XVIII-30-2 p-I-Ph H H CH 3 'Pr OCH3 F H OH H H XVIII-30-3 p-I-Ph H H CH(CH 3) 2 'Pr OCH3 F H OH H H XVIII-30-4 p-I-Ph H H CH 2CH(CH3) 2 'Pr OCH3 F H OH H H XVIII-30-5 p-I-Ph H H CH 2Ph 'Pr OCH3 F H OH H H XVIII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr OCH3 F H OH H H XVIII-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr OCH3 F H OH H H XVIII-30-8 p-I-Ph * H * 'Pr OCH3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-31. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' XVIII-31-1 CH 3 H H H "Bu OCH 3 F H OH H H XVIII-31-2 CH 3 H H CH3 "Bu OCH 3 F H OH H H XVIII-31-3 CH3 H H CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-31-4 CH3 H H CH2CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-31-5 CH3 H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-31-6 CH3 H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-31-7 CH3 H H CH2CH 2SCH 3 "Bu OCH 3 F H OH H H XVIII-31-8 CH3 * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-32. o R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' XVIII-32-1 Et H H H "Bu OCH 3 F H OH H H XVIII-32-2 Et H H CH3 "Bu OCH 3 F H OH H H XVIII-32-3 Et H H CH(CH 3) 2 "Bu OCH 3 F H OH H H

_171 _

R' No Rl R 2 R3 a R3 b R4 R6 X Y R7 R' XVIII-32-4 Et H H CH2CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-32-5 Et H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-32-6 Et H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-32-7 Et H H CH2CH 2SCH 3 "Bu OCH 3 F H OH H H XVIII-32-8 Et * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-33. R No R' R2 R3 a R3b R4 R6 X Y R7 R' XVIII-33-1 'Pr H H H "Bu OCH 3 F H OH H H XVIII-33-2 'Pr H H CH 3 "Bu OCH 3 F H OH H H XVIII-33-3 'Pr H H CH(CH 3)2 "Bu OCH 3 F H OH H H XVIII-33-4 'Pr H H CH 2CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-33-5 'Pr H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-33-6 'Pr H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-33-7 Pr H H CH 2CH 2SCH 3 "Bu OCH 3 F H OH H H XVIII-33-8 Pr * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-34. No R R2 R3a R3b R4 R' R6 X Y R7 R' XVIII-34-1 'Bu H H H "Bu OCH3 F H OH H H XVIII-34-2 'Bu H H CH 3 "Bu OCH3 F H OH H H XVIII-34-3 'Bu H H CH(CH 3)2 "Bu OCH3 F H OH H H XVIII-34-4 'Bu H H CH 2CH(CH 3)2 "Bu OCH3 F H OH H H XVIII-34-5 'Bu H H CH 2Ph "Bu OCH3 F H OH H H XVIII-34-6 'Bu H H CH 2-indol-3-yl "Bu OCH3 F H OH H H XVIII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu OCH3 F H OH H H XVIII-34-8 'Bu * H * "Bu OCH3 F H OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-35. No RI R2 R3 a R3b R4 R5 R6 X Y R7 R' XVIII-35-1 Ph H H H "Bu OCH 3 F H OH H H XVIII-35-2 Ph H H CH 3 "Bu OCH 3 F H OH H H XVIII-35-3 Ph H H CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-35-4 Ph H H CH 2CH(CH3) 2 "Bu OCH 3 F H OH H H XVIII-35-5 Ph H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-35-6 Ph H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H

R' 6 No R R2 R 3 aRb R4 R X Y R7 R' XVIII-35-7 Ph H H CH 2CH 2SCH 3 "Bu OCH 3 F H OH H H XVIII-35-8 Ph * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-36. R' No R R2 RWaRb R4 R' X Y R7 R' XVIII-36-1 p-Me-Ph H H H "Bu OCH 3 F H OH H H XVIII-36-2 p-Me-Ph H H CH 3 "Bu OCH 3 F H OH H H XVIII-36-3 p-Me-Ph H H CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-36-4 p-Me-Ph H H CH 2CH(CH3) 2 "Bu OCH 3 F H OH H H XVIII-36-5 p-Me-Ph H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 F H OH H H XVIII-36-8 p-Me-Ph * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-37. N RI R2 R 3 a Rb R4 R' R6 X Y R7 R'

XVIII-37-1 p-F-Ph H H H "Bu OCH 3 F H OH H H XVIII-37-2 p-F-Ph H H CH 3 "Bu OCH 3 F H OH H H XVIII-37-3 p-F-Ph H H CH(CH 3 ) 2 "Bu OCH 3 F H OH H H XVIII-37-4 p-F-Ph H H CH 2CH(CH 3 ) 2 "Bu OCH 3 F H OH H H XVIII-37-5 p-F-Ph H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-37-7 p-F-Ph H H CH 2CH 2 SCH 3 "Bu OCH 3 F H OH H H XVIII-37-8 p-F-Ph * H * "Bu OCH 3 F H OH H H

*R 2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-38. No R R 2 R 3a Rb R4 R5 R6 X Y R7 R8 XVIII-38-1 p-Cl-Ph H H H "Bu OCH 3 F H OH H H XVIII-38-2 p-Cl-Ph H H CH 3 "Bu OCH 3 F H OH H H XVIII-38-3 p-Cl-Ph H H CH(CH 3 ) 2 "Bu OCH 3 F H OH H H XVIII-38-4 p-Cl-Ph H H CH 2 CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-38-5 p-Cl-Ph H H CH 2 Ph "Bu OCH 3 F H OH H H XVIII-38-6 p-Cl-Ph H H CH 2 -indol-3-yl "Bu OCH 3 F H OH H H

XVIII-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 F H OH H H XVIII-38-8 p-Cl-Ph * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-39. No R RR 3 a R3b R4 R' R6 X Y R7 R' XVIII-39-1 p-Br-Ph H H H "Bu OCH 3 F H OH H H XVIII-39-2 p-Br-Ph H H CH3 "Bu OCH 3 F H OH H H XVIII-39-3 p-Br-Ph H H CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-39-4 p-Br-Ph H H CH2CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-39-5 p-Br-Ph H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 F H OH H H XVIII-39-8 p-Br-Ph * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-40. N9 R1 R2 R3 a R3 b R4 R R6 X Y R7 R' XVIII-40-1 p-I-Ph H H H "Bu OCH 3 F H OH H H XVIII-40-2 p-I-Ph H H CH 3 "Bu OCH 3 F H OH H H XVIII-40-3 p-I-Ph H H CH(CH 3) 2 "Bu OCH 3 F H OH H H XVIII-40-4 p-I-Ph H H CH 2CH(CH3) 2 "Bu OCH 3 F H OH H H XVIII-40-5 p-I-Ph H H CH 2Ph "Bu OCH 3 F H OH H H XVIII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu OCH 3 F H OH H H XVIII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu OCH 3 F H OH H H XVIII-40-8 p-I-Ph * H * "Bu OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-41. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R' XVIII-41-1 CH 3 H H H Bz OCH 3 F H OH H H XVIII-41-2 CH 3 H H CH3 Bz OCH 3 F H OH H H XVIII-41-3 CH 3 H H CH(CH 3) 2 Bz OCH 3 F H OH H H XVIII-41-4 CH 3 H H CH2CH(CH 3) 2 Bz OCH 3 F H OH H H XVIII-41-5 CH 3 H H CH 2Ph Bz OCH 3 F H OH H H XVIII-41-6 CH 3 H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-41-7 CH 3 H H CH2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-41-8 CH 3 * H * Bz OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-42. No R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R' XVIII-42-1 Et H H H Bz OCH 3 F H OH H H XVIII-42-2 Et H H CH3 Bz OCH 3 F H OH H H XVIII-42-3 Et H H CH(CH 3) 2 Bz OCH 3 F H OH H H

- 17A-

Rl R 2 R3 a R3 b R4 R R' X Y R7 R' No

XVIII-42-4 Et H H CH2CH(CH3) 2 Bz OCH 3 F H OH H H XVIII-42-5 Et H H CH 2Ph Bz OCH 3 F H OH H H XVIII-42-6 Et H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-42-7 Et H H CH2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-42-8 Et * H * Bz OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-43. No RI1 R 2 R3a R3 b R4 R R6 X Y R7 R *R2 and R 3b XVIII-43-1 'Pr H H H Bz OCH 3 F H OH H H joined XVIII-43-2 'Pr H H CH 3 Bz OCH 3 F H OH H I§ together by XVIII-43-3 Pr H H CH(CH3) 2 Bz OCH 3 F H OH H H (CH2) 3 to XVIII-43-4 Pr H H CH 2CH(CH3) 2 Bz OCH 3 F H OH H H form five XVIII-43-5 Pr H H CH 2Ph Bz OCH 3 F H OH H H membered XVIII-43-6 'Pr H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-43-7 iPr H H CH2 CH2SCH 3 Bz OCH 3 F H OH H H ring. XVIII-43-8 'Pr * H * Bz OCH 3 F H OH H 1M Table XVIII-44. R' 6 No RI R2 R 3a R3 b 4 R X Y R7 R8

XVIII-44-1 'Bu H H H Bz OCH 3 F H OH H H XVIII-44-2 'Bu H H CH 3 Bz OCH 3 F H OH H H XVIII-44-3 'Bu H H CH(CH3) 2 Bz OCH 3 F H OH H H XVIII-44-4 'Bu H H CH 2CH(CH3)2 Bz OCH 3 F H OH H H XVIII-44-5 'Bu H H CH 2Ph Bz OCH 3 F H OH H H XVIII-44-6 'Bu H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-44-7 'Bu H H CH 2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-44-8 'Bu * H * Bz OCH 3 F H OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-45. N RI R 2 R 3a R3b R4 R5 R6 X Y R7 R8

XVIII-45-1 Ph H H H Bz OCH 3 F H OH H H XVIII-45-2 Ph H H CH 3 Bz OCH 3 F H OH H H XVIII-45-3 Ph H H CH(CH3) 2 Bz OCH 3 F H OH H H XVIII-45-4 Ph H H CH 2CH(CH3)2 Bz OCH 3 F H OH H H XVIII-45-5 Ph H H CH 2Ph Bz OCH 3 F H OH H H XVIII-45-6 Ph H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-45-7 Ph H H CH 2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-45-8 Ph * H * Bz OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring. '1'7r,

Table XVIII-46. No R R 2 R 3 a R 3b R4 R6 X Y R7 R' XVIII-46-1 p-Me-Ph H H H Bz OCH 3 F H OH H H XVIII-46-2 p-Me-Ph H H CH 3 Bz OCH 3 F H OH H H XVIII-46-3 p-Me-Ph H H CH(CH 3)2 Bz OCH 3 F H OH H H XVIII-46-4 p-Me-Ph H H CH 2CH(CH3) 2 Bz OCH 3 F H OH H H XVIII-46-5 p-Me-Ph H H CH 2Ph Bz OCH 3 F H OH H H XVIII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz OCH 3 F H OH H H XVIII-46-8 p-Me-Ph * H * Bz OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-47. N R1 R2 R 3a R3 bR 4 R' R6 X Y R7 R XVIII-47-1 p-F-Ph H H H Bz OCH 3 F H OH H H XVIII-47-2 p-F-Ph H H CH 3 Bz OCH 3 F H OH H H XVIII-47-3 p-F-Ph H H CH(CH3) 2 Bz OCH 3 F H OH H H XVIII-47-4 p-F-Ph H H CH 2CH(CH3)2 Bz OCH 3 F H OH H H XVIII-47-5 p-F-Ph H H CH 2Ph Bz OCH 3 F H OH H H XVIII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz OCH 3 F H OH H H XVIII-47-8 p-F-Ph * H * Bz OCH 3 F H OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XVIII-48. 6 No RI 1 R2 R 3a R3b R4 R5 R X Y R7 R' XVIII-48-1 p-Cl-Ph H H H Bz OCH 3 F H OH H H XVIII-48-2 p-Cl-Ph H H CH3 Bz OCH 3 F H OH H H XVIII-48-3 p-Cl-Ph H H CH(CH 3)2 Bz OCH 3 F H OH H H XVIII-48-4 p-Cl-Ph H H CH2CH(CH 3) 2 Bz OCH 3 F H OH H H XVIII-48-5 p-Cl-Ph H H CH 2Ph Bz OCH 3 F H OH H H XVIII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-48-8 p-Cl-Ph * H * Bz OCH 3 F H OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-49. No RI 1 R2 R 3 a R3 b R4 R5 R6 X Y R7 R XVIII-49-1 p-Br-Ph H H H Bz OCH 3 F H OH H H XVIII-49-2 p-Br-Ph H H CH3 Bz OCH 3 F H OH H H XVIII-49-3 p-Br-Ph H H CH(CH3)2 Bz OCH 3 F H OH H H

'1'7r,

R' No R RR 3 a R3 b R4 R' X Y R7 R' XVIII-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz OCH 3 F H OH H H XVIII-49-5 p-Br-Ph H H CH 2Ph Bz OCH 3 F H OH H H XVIII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-49-8 p-Br-Ph * H * Bz OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XVIII-50. No R' R2 R3 a R3b R4 R5 R6 X Y R7 R' XVIII-50-1 p-I-Ph H H H Bz OCH 3 F H OH H H XVIII-50-2 p-I-Ph H H CH 3 Bz OCH 3 F H OH H H XVIII-50-3 p-I-Ph H H CH(CH 3) 2 Bz OCH 3 F H OH H H XVIII-50-4 p-I-Ph H H CH 2CH(CH3) 2 Bz OCH 3 F H OH H H XVIII-50-5 p-I-Ph H H CH 2Ph Bz OCH 3 F H OH H H XVIII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz OCH 3 F H OH H H XVIII-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz OCH 3 F H OH H H XVIII-50-8 p-I-Ph * H * Bz OCH 3 F H OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

0

R8 NH

R2 0 R3b R7 N O R3a P- P O 00N-

R6 C0 2R 4 OR' R5

Y X

XIX Table XIX-1. No R1 R2 R3 a R3 b R4 R5 R 6 X Y R7 R' XIX-1-1 CH 3 H H H CH 3 OCH 3 F F OH H H XIX-1-2 CH 3 H H CH3 CH 3 OCH 3 F F OH H H XIX-1-3 CH 3 H H CH(CH 3) 2 CH 3 OCH 3 F F OH H H XIX-1-4 CH 3 H H CH2CH(CH3) 2 CH 3 OCH 3 F F OH H H XIX-1-5 CH 3 H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-1-6 CH 3 H H CH 2-indol-3-yl CH 3 OCH 3 F F OH H H XIX-1-7 CH 3 H H CH2CH 2SCH3 CH 3 OCH 3 F F OH H H

R R2 R3 a R3 b R4 R R' X Y R7 R' No XIX-1-8 CH 3 * H * CH 3 OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-2. No Rl R 2 R3 a R3 b R4 R R' X Y R7 R' XIX-2-1 Et H H H CH 3 OCH 3 F F OH H H XIX-2-2 Et H H CH 3 CH 3 OCH 3 F F OH H H XIX-2-3 Et H H CH(CH3) 2 CH 3 OCH 3 F F OH H H XIX-2-4 Et H H CH 2CH(CH3) 2 CH 3 OCH 3 F F OH H H XIX-2-5 Et H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-2-6 Et H H CH 2-indol-3-yl CH 3 OCH 3 F F OH H H XIX-2-7 Et H H CH 2CH 2SCH 3 CH 3 OCH 3 F F OH H H XIX-2-8 Et * H * CH 3 OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-3. No RI R2 R3 a R3 b It 4 I5 RX Y R7 R8

XIX-3-1 'Pr H H H CH 3 OCH 3 F F OH H H XIX-3-2 'Pr H H CH 3 CH 3 OCH 3 F F OH H H XIX-3-3 'Pr H H CH(CH3) 2 CH 3 OCH 3 F F OH H H XIX-3-4 Pr H H CH 2CH(CH3)2 CH 3 OCH 3 F F OH H H XIX-3-5 Pr H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-3-6 'Pr H H CH 2-indol-3-yl CH 3 OCH 3 F F OH H H XIX-3-7 'Pr H H CH 2CH2SCH 3 CH 3 OCH 3 F F OH H H XIX-3-8 'Pr * H * CH 3 OCH 3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-4. No RI R2 R 3a R3 bR 4 R5 R6 X Y R7 R8

XIX-4-1 'Bu H H H CH3 OCH 3 F F OH H H XIX-4-2 'Bu H H CH 3 CH3 OCH 3 F F OH H H XIX-4-3 'Bu H H CH(CH3) 2 CH3 OCH 3 F F OH H H XIX-4-4 'Bu H H CH 2CH(CH3)2 CH3 OCH 3 F F OH H H XIX-4-5 'Bu H H CH 2Ph CH3 OCH 3 F F OH H H XIX-4-6 'Bu H H CH 2-indol-3-yl CH3 OCH 3 F F OH H H XIX-4-7 'Bu H H CH 2CH2SCH 3 CH3 OCH 3 F F OH H H XIX-4-8 'Bu * H * CH3 OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'17S2

Table XIX-5. No R1 R2 R3 a R 3b R4 R5 R6 X Y R7 R' XIX-5-1 Ph H H H CH 3 OCH 3 F F OH H H XIX-5-2 Ph H H CH3 CH3 OCH 3 F F OH H H XIX-5-3 Ph H H CH(CH3) 2 CH3 OCH 3 F F OH H H XIX-5-4 Ph H H CH2CH(CH3)2 CH 3 OCH 3 F F OH H H XIX-5-5 Ph H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-5-6 Ph H H CH 2-indol-3-yl CH3 OCH 3 F F OH H H XIX-5-7 Ph H H CH2CH 2SCH3 CH3 OCH 3 F F OH H H XIX-5-8 Ph * H * CH 3 OCH 3 F F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-6. N R1 R2 R3 a R3 b R4 R5 R6 X Y R7 R XIX-6-1 p-Me-Ph H H H CH 3 OCH 3 F F OH H H XIX-6-2 p-Me-Ph H H CH 3 CH3 OCH 3 F F OH H H XIX-6-3 p-Me-Ph H H CH(CH3) 2 CH3 OCH 3 F F OH H H XIX-6-4 p-Me-Ph H H CH 2CH(CH 3)2 CH 3 OCH 3 F F OH H H XIX-6-5 p-Me-Ph H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 OCH 3 F F OH H H XIX-6-7 p-Me-Ph H H CH 2CH 2SCH3 CH3 OCH 3 F F OH H H XIX-6-8 p-Me-Ph * H * CH 3 OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-7. No RI 1 R2 R3 a R3b R4 R5 R6 X Y R7 R XIX-7-1 p-F-Ph H H H CH 3 OCH 3 F F OH H H XIX-7-2 p-F-Ph H H CH 3 CH3 OCH 3 F F OH H H XIX-7-3 p-F-Ph H H CH(CH3) 2 CH3 OCH 3 F F OH H H XIX-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 OCH 3 F F OH H H XIX-7-6 p-F-Ph H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 OCH 3 F F OH H H XIX-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 OCH 3 F F OH H H XIX-7-20 p-F-Ph * H * CH 3 OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-8. 4 6 No RI R2 R 3 a RIt R5 R X Y R7 R' XIX-8-1 p-Cl-Ph H H H CH3 OCH 3 F F OH H H XIX-8-2 p-Cl-Ph H H CH 3 CH3 OCH 3 F F OH H H XIX-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 OCH 3 F F OH H H

_170 _

R 6 No R RR 3 a R3 b R4 R X Y R7 R' XIX-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 OCH 3 F F OH H H XIX-8-5 p-Cl-Ph H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 OCH 3 F F OH H H XIX-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH 3 OCH 3 F F OH H H XIX-8-8 p-Cl-Ph * H * CH 3 OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-9. No RI R2 R 3a R3 b R4 R' R6 X Y R7 R8

XIX-9-1 p-Br-Ph H H H CH 3 OCH 3 F F OH H H XIX-9-2 p-Br-Ph H H CH 3 CH 3 OCH 3 F F OH H H XIX-9-3 p-Br-Ph H H CH(CH3)2 CH 3 OCH 3 F F OH H H XIX-9-4 p-Br-Ph H H CH 2CH(CH3) 2 CH 3 OCH 3 F F OH H H XIX-9-6 p-Br-Ph H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 OCH 3 F F OH H H XIX-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH 3 OCH 3 F F OH H H XIX-9-20 p-Br-Ph * H * CH 3 OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-10. R' No R RR 3 a R3b R4 R6 X Y R7 R' XIX-10-1 p-I-Ph H H H CH 3 OCH 3 F F OH H H XIX-10-2 p-I-Ph H H CH 3 CH 3 OCH 3 F F OH H H XIX-10-3 p-I-Ph H H CH(CH3) 2 CH 3 OCH 3 F F OH H H XIX-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 OCH 3 F F OH H H XIX-10-5 p-I-Ph H H CH 2Ph CH 3 OCH 3 F F OH H H XIX-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 OCH 3 F F OH H H XIX-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 OCH 3 F F OH H H XIX-10-8 p-I-Ph * H * CH 3 OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-11. N RI R2 R3a R3b R4 R' R6 X Y R7 R8

XIX-11-1 CH 3 H H H Et OCH 3 F F OH H H XIX-11-2 CH 3 H H CH3 Et OCH 3 F F OH H H XIX-11-3 CH 3 H H CH(CH3) 2 Et OCH 3 F F OH H H XIX-11-4 CH 3 H H CH2CH(CH3) 2 Et OCH 3 F F OH H H XIX-11-5 CH 3 H H CH 2Ph Et OCH 3 F F OH H H XIX-11-6 CH 3 H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-11-7 CH 3 H H CH2CH 2SCH 3 Et OCH 3 F F OH H H XIX-11-8 CH 3 * H * Et OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-12. No R 1 R2 R 3a R3b R4 R5 R6 X Y R7 R8

XIX-12-1 Et H H H Et OCH 3 F F OH H H XIX-12-2 Et H H CH3 Et OCH 3 F F OH H H XIX-12-3 Et H H CH(CH3)2 Et OCH 3 F F OH H H XIX-12-4 Et H H CH2CH(CH3) 2 Et OCH 3 F F OH H H XIX-12-5 Et H H CH 2Ph Et OCH 3 F F OH H H XIX-12-6 Et H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-12-7 Et H H CH2CH 2SCH 3 Et OCH 3 F F OH H H XIX-12-8 Et * H * Et OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-13. R 6 No R' R2 R3 a R3 b R4 R X Y R7 R' XIX-13-1 'Pr H H H Et OCH 3 F F OH H H XIX-13-2 'Pr H H CH 3 Et OCH 3 F F OH H H XIX-13-3 'Pr H H CH(CH 3)2 Et OCH 3 F F OH H H XIX-13-4 Pr H H CH 2CH(CH3) 2 Et OCH 3 F F OH H H XIX-13-5 'Pr H H CH 2Ph Et OCH 3 F F OH H H XIX-13-6 'Pr H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-13-7 'Pr H H CH 2 CH2 SCH 3 Et OCH 3 F F OH H H XIX-13-8 'Pr * H * Et OCH 3 F F OH H H *R2 and R3 joined together by (CH 2 ) 3 toform five-membered ring.

Table XIX-14. R No R1 R2 R3 a Rb 3 R4 R6 X Y R7 R8

XIX-14-1 'Bu H H H Et OCH 3 F F OH H H XIX-14-2 'Bu H H CH 3 Et OCH 3 F F OH H H XIX-14-3 'Bu H H CH(CH3) 2 Et OCH 3 F F OH H H XIX-14-4 'Bu H H CH 2CH(CH3)2 Et OCH 3 F F OH H H XIX-14-5 'Bu H H CH 2Ph Et OCH 3 F F OH H H XIX-14-6 'Bu H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-14-7 'Bu H H CH 2 CH2 SCH 3 Et OCH 3 F F OH H H XIX-14-8 'Bu * H * Et OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-15. No RI 1 R2 R 3a R 3b R4 R5 R6 X Y R7 R8

XIX-15-1 Ph H H H Et OCH 3 F F OH H H XIX-15-2 Ph H H CH3 Et OCH 3 F F OH H H XIX-15-3 Ph H H CH(CH3) 2 Et OCH 3 F F OH H H XIX-15-4 Ph H H CH2CH(CH3)2 Et OCH 3 F F OH H H XIX-15-5 Ph H H CH 2Ph Et OCH 3 F F OH H H XIX-15-6 Ph H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-15-7 Ph H H CH2CH2SCH 3 Et OCH 3 F F OH H H XIX-15-8 Ph * H * Et OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-16. R RR 3 R 3b R4 R' R6 X Y R7 R' No a

XIX-16-1 p-Me-Ph H H H Et OCH 3 F F OH H H XIX-16-2 p-Me-Ph H H CH 3 Et OCH 3 F F OH H H XIX-16-3 p-Me-Ph H H CH(CH3) 2 Et OCH 3 F F OH H H XIX-16-4 p-Me-Ph H H CH 2CH(CH3)2 Et OCH 3 F F OH H H XIX-16-5 p-Me-Ph H H CH 2Ph Et OCH 3 F F OH H H XIX-16-6 p-Me-Ph H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et OCH 3 F F OH H H XIX-16-8 p-Me-Ph * H * Et OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-17. N9 R R2 R3a R3b R4 R' R 6 X Y R7 R8

XIX-17-1 p-F-Ph H H H Et OCH 3 F F OH H H XIX-17-2 p-F-Ph H H CH 3 Et OCH 3 F F OH H H XIX-17-3 p-F-Ph H H CH(CH3) 2 Et OCH 3 F F OH H H XIX-17-4 p-F-Ph H H CH 2CH(CH 3) 2 Et OCH 3 F F OH H H XIX-17-5 p-F-Ph H H CH 2Ph Et OCH 3 F F OH H H XIX-17-6 p-F-Ph H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-17-7 p-F-Ph H H CH 2CH2SCH 3 Et OCH 3 F F OH H H XIX-17-8 p-F-Ph * H * Et OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-18. No R R2 R 3 a R 3b R4 R 5 R 6 X Y R7 R8

XIX-18-1 p-Cl-Ph H H H Et OCH3 F F OH H H XIX-18-2 p-Cl-Ph H H CH 3 Et OCH3 F F OH H H XIX-18-3 p-Cl-Ph H H CH(CH3) 2 Et OCH3 F F OH H H XIX-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et OCH3 F F OH H H XIX-18-5 p-Cl-Ph H H CH 2Ph Et OCH3 F F OH H H XIX-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et OCH3 F F OH H H XIX-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et OCH3 F F OH H H XIX-18-8 p-Cl-Ph * H * Et OCH3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-19. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R8

XIX-19-1 p-Br-Ph H H H Et OCH 3 F F OH H H XIX-19-2 p-Br-Ph H H CH3 Et OCH 3 F F OH H H XIX-19-3 p-Br-Ph H H CH(CH3)2 Et OCH 3 F F OH H H

R R2 R 3 R3 b R4 R R X Y R7 R8 No a

XIX-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et OCH 3 F F OH H H XIX-19-5 p-Br-Ph H H CH 2Ph Et OCH 3 F F OH H H XIX-19-6 p-Br-Ph H H CH 2-indol-3-yl Et OCH 3 F F OH H H XIX-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et OCH 3 F F OH H H XIX-19-8 p-Br-Ph * H * Et OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-20. No R R2 R 3 a R3b R4 R' R6 X Y R7 XIX-20-1 p-I-Ph H H H Et OCH 3 F F OH H XIX-20-2 p-I-Ph H H CH 3 Et OCH 3 F F OH H XIX-20-3 p-I-Ph H H CH(CH3) 2 Et OCH 3 F F OH H XIX-20-4 p-I-Ph H H CH 2CH(CH3)2 Et OCH 3 F F OH H XIX-20-5 p-I-Ph H H CH 2Ph Et OCH 3 F F OH H XIX-20-6 p-I-Ph H H CH 2-indol-3-yl Et OCH 3 F F OH H XIX-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et OCH 3 F F OH H XIX-20-8 p-I-Ph * H * Et OCH 3 F F OH H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-21. N Rl R2 R 3a R3 b R4 R' R6 X Y R7 R8

XIX-21-1 CH 3 H H H 'Pr OCH 3 F F OH H H XIX-21-2 CH 3 H H CH3 'Pr OCH 3 F F OH H H XIX-21-3 CH 3 H H CH(CH 3)2 'Pr OCH 3 F F OH H H XIX-21-4 CH 3 H H CH2CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-21-5 CH 3 H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-21-6 CH 3 H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-21-7 CH 3 H H CH2CH 2SCH 3 'Pr OCH 3 F F OH H H XIX-21-8 CH 3 * H * 'Pr OCH 3 F F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-22. No Rl R2 R 3a R3b R4 R5 R6 X Y R7 R8

XIX-22-1 Et H H H 'Pr OCH 3 F F OH H H XIX-22-2 Et H H CH3 'Pr OCH 3 F F OH H H XIX-22-3 Et H H CH(CH3)2 'Pr OCH 3 F F OH H H XIX-22-4 Et H H CH2CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-22-5 Et H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-22-6 Et H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H

'IQA-

Rl R2 R 3a R3 b R4 R' R' X Y R7 R8 No XIX-22-7 Et H H CH2 CH 2 SCH 3 'Pr OCH 3 F F OH H H XIX-22-8 Et * H * 'Pr OCH 3 F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-23. R No R' R2 R 3a R3 b R4 R' X Y R7 R8

XIX-23-1 'Pr H H H 'Pr OCH 3 F F OH H H XIX-23-2 'Pr H H CH 3 'Pr OCH 3 F F OH H H XIX-23-3 'Pr H H CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-23-4 'Pr H H CH 2CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-23-5 'Pr H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-23-6 'Pr H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-23-7 'Pr H H CH 2CH2SCH 3 'Pr OCH 3 F F OH H H XIX-23-8 'Pr * H * 'Pr OCH 3 F F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to formfive-membered ring.

Table XIX-24. R No R R2 R3 a R3 b R4 R 6 X Y R7 R8

XIX-24-1 'Bu H H H 'Pr OCH3 F F OH H H XIX-24-2 'Bu H H CH 3 'Pr OCH3 F F OH H H XIX-24-3 'Bu H H CH(CH3) 2 'Pr OCH3 F F OH H H XIX-24-4 'Bu H H CH 2CH(CH3) 2 'Pr OCH3 F F OH H H XIX-24-5 'Bu H H CH 2Ph 'Pr OCH3 F F OH H H XIX-24-6 'Bu H H CH 2-indol-3-yl 'Pr OCH3 F F OH H H XIX-24-7 'Bu H H CH 2CH2SCH 3 'Pr OCH3 F F OH H H XIX-24-8 'Bu * H * 'Pr OCH3 F F OH H H

*R2 and R 3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-25. No R R2 R 3a R3 b R4 R5 R 6 X Y R7 R8

XIX-25-1 Ph H H H 'Pr OCH 3 F F OH H H XIX-25-2 Ph H H CH3 'Pr OCH 3 F F OH H H XIX-25-3 Ph H H CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-25-4 Ph H H CH2CH(CH 3) 2 'Pr OCH 3 F F OH H H XIX-25-5 Ph H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-25-6 Ph H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-25-7 Ph H H CH2CH2SCH 3 'Pr OCH 3 F F OH H H XIX-25-8 Ph * H * 'Pr OCH 3 F F OH H H

*R2 and R 3b joined together by (CH2)3 to formfive-membered ring.

Table XIX-26. R RR 3 R3b R4 R R6 X Y R7 R8 No a

XIX-26-1 p-Me-Ph H H H 'Pr OCH 3 F F OH H H XIX-26-2 p-Me-Ph H H CH 3 'Pr OCH 3 F F OH H H XIX-26-3 p-Me-Ph H H CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr OCH 3 F F OH H H XIX-26-5 p-Me-Ph H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr OCH 3 F F OH H H XIX-26-8 p-Me-Ph * H * 'Pr OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-27. N9 R1 R2 R3 a R3 b R4 R' R6 X Y R7 R8

XIX-27-1 p-F-Ph H H H 'Pr OCH 3 F F OH H H XIX-27-2 p-F-Ph H H CH 3 'Pr OCH 3 F F OH H H XIX-27-3 p-F-Ph H H CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-27-4 p-F-Ph H H CH 2CH(CH3)2 'Pr OCH 3 F F OH H H XIX-27-5 p-F-Ph H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr OCH 3 F F OH H H XIX-27-8 p-F-Ph * H * 'Pr OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-28. No R R2 R 3 a R 3b R4 R6 X Y R7 R8

XIX-28-1 p-Cl-Ph H H H 'Pr OCH 3 F F OH H H XIX-28-2 p-Cl-Ph H H CH 3 'Pr OCH 3 F F OH H H XIX-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr OCH 3 F F OH H H XIX-28-5 p-Cl-Ph H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr OCH 3 F F OH H H XIX-28-8 p-Cl-Ph * H * 'Pr OCH 3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-29. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R8

XIX-29-1 p-Br-Ph H H H 'Pr OCH 3 F F OH H H XIX-29-2 p-Br-Ph H H CH3 'Pr OCH 3 F F OH H H XIX-29-3 p-Br-Ph H H CH(CH3)2 'Pr OCH 3 F F OH H H

I2A-

R' No R R2 R 3 a R3 b R4 R6 X Y R7 R' XIX-29-4 p-Br-Ph H H CH 2CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-29-5 p-Br-Ph H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr OCH 3 F F OH H H XIX-29-8 p-Br-Ph * H * 'Pr OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'2'7-

Table XIX-30. R RR 3 R3b R4 R R' X Y R7 R8 No a

XIX-30-1 p-I-Ph H H H 'Pr OCH 3 F F OH H H XIX-30-2 p-I-Ph H H CH 3 'Pr OCH 3 F F OH H H XIX-30-3 p-I-Ph H H CH(CH3) 2 'Pr OCH 3 F F OH H H XIX-30-4 p-I-Ph H H CH 2CH(CH3)2 'Pr OCH 3 F F OH H H XIX-30-5 p-I-Ph H H CH 2Ph 'Pr OCH 3 F F OH H H XIX-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr OCH 3 F F OH H H XIX-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr OCH 3 F F OH H H XIX-30-8 p-I-Ph * H * 'Pr OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-31. N RI R2 R3a R3b R4 R' R6 X Y R7 R8

XIX-31-1 CH 3 H H H "Bu OCH3 F F OH H H XIX-31-2 CH 3 H H CH3 "Bu OCH3 F F OH H H XIX-31-3 CH 3 H H CH(CH3) 2 "Bu OCH3 F F OH H H XIX-31-4 CH 3 H H CH2CH(CH3) 2 "Bu OCH3 F F OH H H XIX-31-5 CH 3 H H CH 2Ph "Bu OCH3 F F OH H H XIX-31-6 CH 3 H H CH 2-indol-3-yl "Bu OCH3 F F OH H H XIX-31-7 CH 3 H H CH2CH 2SCH 3 "Bu OCH3 F F OH H H XIX-31-8 CH 3 * H * "Bu OCH3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-32. No R 1 R2 R 3a R3b R4 R5 R6 X Y R7 R8

XIX-32-1 Et H H H "Bu OCH3 F F OH H H XIX-32-2 Et H H CH3 "Bu OCH3 F F OH H H XIX-32-3 Et H H CH(CH3)2 "Bu OCH3 F F OH H H XIX-32-4 Et H H CH2CH(CH3) 2 "Bu OCH3 F F OH H H XIX-32-5 Et H H CH 2Ph "Bu OCH3 F F OH H H XIX-32-6 Et H H CH 2-indol-3-yl "Bu OCH3 F F OH H H XIX-32-7 Et H H CH2CH 2SCH 3 "Bu OCH3 F F OH H H XIX-32-8 Et * H * "Bu OCH3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-33. 3 R' 6 No R' R2 R3 aR R4 R X Y R7 R' XIX-33-1 'Pr H H H "Bu OCH 3 F F OH H H XIX-33-2 'Pr H H CH 3 "Bu OCH 3 F F OH H H XIX-33-3 'Pr H H CH(CH3) 2 "Bu OCH 3 F F OH H H XIX-33-4 Pr H H CH 2CH(CH3) 2 "Bu OCH 3 F F OH H H XIX-33-5 Pr H H CH 2Ph "Bu OCH 3 F F OH H H XIX-33-6 Pr H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-33-7 Pr H H CH 2 CH2 SCH 3 "Bu OCH 3 F F OH H H XIX-33-8 Pr * H * "Bu OCH 3 F F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-34. N RI R2 R3 a R3b R4 R R6 X Y R7 R8 XIX-34-1 'Bu H H H "Bu OCH 3 F F OH H H XIX-34-2 'Bu H H CH 3 "Bu OCH 3 F F OH H H XIX-34-3 'Bu H H CH(CH3) 2 "Bu OCH 3 F F OH H H XIX-34-4 'Bu H H CH 2 CH(CH3)2 "Bu OCH 3 F F OH H H XIX-34-5 'Bu H H CH 2Ph "Bu OCH 3 F F OH H H XIX-34-6 'Bu H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-34-7 'Bu H H CH 2 CH2SCH 3 "Bu OCH 3 F F OH H H XIX-34-8 'Bu * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-35. No RI 1 R 2 R 3a R3b R4 R5 R6 X Y R7 R8

XIX-35-1 Ph H H H "Bu OCH 3 F F OH H H XIX-35-2 Ph H H CH3 "Bu OCH 3 F F OH H H XIX-35-3 Ph H H CH(CH3) 2 "Bu OCH 3 F F OH H H XIX-35-4 Ph H H CH2CH(CH3)2 "Bu OCH 3 F F OH H H XIX-35-5 Ph H H CH 2 Ph "Bu OCH 3 F F OH H H XIX-35-6 Ph H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-35-7 Ph H H CH2 CH2 SCH 3 "Bu OCH 3 F F OH H H XIX-35-8 Ph * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_22o-

Table XIX-36. No R RR 3 a R3b R4 R' R6 X Y R7 R' XIX-36-1 p-Me-Ph H H H "Bu OCH 3 F F OH H H XIX-36-2 p-Me-Ph H H CH 3 "Bu OCH 3 F F OH H H XIX-36-3 p-Me-Ph H H CH(CH 3)2 "Bu OCH 3 F F OH H H XIX-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu OCH 3 F F OH H H XIX-36-5 p-Me-Ph H H CH 2Ph "Bu OCH 3 F F OH H H XIX-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 F F OH H H XIX-36-8 p-Me-Ph * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-37. No R1 R2 R3a R3b R4 R' R6 X Y R7 R8 XIX-37-1 p-F-Ph H H H "Bu OCH 3 F F OH H H XIX-37-2 p-F-Ph H H CH 3 "Bu OCH 3 F F OH H H XIX-37-3 p-F-Ph H H CH(CH 3) 2 "Bu OCH 3 F F OH H H XIX-37-4 p-F-Ph H H CH 2 CH(CH 3) 2 "Bu OCH 3 F F OH H H XIX-37-5 p-F-Ph H H CH 2Ph "Bu OCH 3 F F OH H H XIX-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-37-7 p-F-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 F F OH H H XIX-37-8 p-F-Ph * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-38. No R1 R2 R 3a R 3 b R4 R5 R 6 X Y R7 R8 XIX-38-1 p-Cl-Ph H H H "Bu OCH 3 F F OH H H XIX-38-2 p-Cl-Ph H H CH 3 "Bu OCH 3 F F OH H H XIX-38-3 p-Cl-Ph H H CH(CH3 ) 2 "Bu OCH 3 F F OH H H XIX-38-4 p-Cl-Ph H H CH 2CH(CH 3 ) 2 "Bu OCH 3 F F OH H H XIX-38-5 p-Cl-Ph H H CH 2Ph "Bu OCH 3 F F OH H H XIX-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-38-7 p-Cl-Ph H H CH 2CH 2 SCH 3 "Bu OCH 3 F F OH H H XIX-38-8 p-Cl-Ph * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-39. No R R2 R 3a R3 b R4 R5 R6 X Y R7 R8 XIX-39-1 p-Br-Ph H H H "Bu OCH 3 F F OH H H XIX-39-2 p-Br-Ph H H CH 3 "Bu OCH 3 F F OH H H XIX-39-3 p-Br-Ph H H CH(CH 3 )2 "Bu OCH 3 F F OH H H

R R2 R 3 R3 b R4 R' R' X Y R7 R8 No a

XIX-39-4 p-Br-Ph H H CH 2CH(CH3) 2 "Bu OCH 3 F F OH H H XIX-39-5 p-Br-Ph H H CH 2Ph "Bu OCH 3 F F OH H H XIX-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 F F OH H H XIX-39-8 p-Br-Ph * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

'201 _

Table XIX-40. R RR 3 R3b R4 R' R6 X Y R7 R' No a

XIX-40-1 p-I-Ph H H H "Bu OCH 3 F F OH H H XIX-40-2 p-I-Ph H H CH 3 "Bu OCH 3 F F OH H H XIX-40-3 p-I-Ph H H CH(CH3) 2 "Bu OCH 3 F F OH H H XIX-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu OCH 3 F F OH H H XIX-40-5 p-I-Ph H H CH 2Ph "Bu OCH 3 F F OH H H XIX-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu OCH 3 F F OH H H XIX-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu OCH 3 F F OH H H XIX-40-8 p-I-Ph * H * "Bu OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-41. N RI R2 R3a R3b R4 R' R6 X Y R7 R' XIX-41-1 CH 3 H H H Bz OCH 3 F F OH H H XIX-41-2 CH 3 H H CH3 Bz OCH 3 F F OH H H XIX-41-3 CH 3 H H CH(CH3) 2 Bz OCH 3 F F OH H H XIX-41-4 CH 3 H H CH2CH(CH3) 2 Bz OCH 3 F F OH H H XIX-41-5 CH 3 H H CH 2Ph Bz OCH 3 F F OH H H XIX-41-6 CH 3 H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-41-7 CH 3 H H CH2CH 2SCH 3 Bz OCH 3 F F OH H H XIX-41-8 CH 3 * H * Bz OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-42. No R 1 R2 R 3a R3b R4 R5 R6 X Y R7 R XIX-42-1 Et H H H Bz OCH 3 F F OH H H XIX-42-2 Et H H CH3 Bz OCH 3 F F OH H H XIX-42-3 Et H H CH(CH3)2 Bz OCH 3 F F OH H H XIX-42-4 Et H H CH2CH(CH3) 2 Bz OCH 3 F F OH H H XIX-42-5 Et H H CH 2Ph Bz OCH 3 F F OH H H XIX-42-6 Et H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-42-7 Et H H CH2CH 2SCH 3 Bz OCH 3 F F OH H H XIX-42-8 Et * H * Bz OCH 3 F F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_20,)

Table XIX-43. No R' R2 R~a RS R4 R' R6 X Y R7 R' *R2 and R3 XIX-43-1 'Pr H H H Bz OCH 3 F F OH H H joined XIX-43-2 'Pr H H CH 3 Bz OCH 3 F F OH H H together by XIX-43-3 'Pr H H CH(CH3) 2 Bz OCH 3 F F OH H M (CH 2)3 to XIX-43-4 Pr H H CH 2CH(CH3) 2 Bz OCH 3 F F OH H H form five XIX-43-5 'Pr H H CH 2Ph Bz OCH 3 F F OH H H membered XIX-43-6 'Pr H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-43-7 'Pr H H CH 2 CH2 SCH 3 Bz OCH 3 F F OH H H ring. XIX-43-8 'Pr * H * Bz OCH 3 F F OH H H Table XIX 10 44. 6 No R R2 R3 a R3 b R4 R X Y R7 R' XIX-44-1 'Bu H H H Bz OCH 3 F F OH H H XIX-44-2 'Bu H H CH 3 Bz OCH 3 F F OH H H XIX-44-3 'Bu H H CH(CH3) 2 Bz OCH 3 F F OH H H XIX-44-4 'Bu H H CH 2CH(CH3)2 Bz OCH 3 F F OH H H XIX-44-5 'Bu H H CH 2Ph Bz OCH 3 F F OH H H XIX-44-6 'Bu H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-44-7 'Bu H H CH 2 CH2 SCH 3 Bz OCH 3 F F OH H H XIX-44-8 'Bu * H * Bz OCH 3 F F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XIX-45. No RI 1 R2 R 3a R3 b R4 R5 R 6 X Y R7 R8

XIX-45-1 Ph H H H Bz OCH 3 F F OH H H XIX-45-2 Ph H H CH3 Bz OCH 3 F F OH H H XIX-45-3 Ph H H CH(CH3) 2 Bz OCH 3 F F OH H H XIX-45-4 Ph H H CH2CH(CH3)2 Bz OCH 3 F F OH H H XIX-45-5 Ph H H CH 2Ph Bz OCH 3 F F OH H H XIX-45-6 Ph H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-45-7 Ph H H CH2CH2SCH 3 Bz OCH 3 F F OH H H XIX-45-8 Ph * H * Bz OCH 3 F F OH H H

*R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

loll

Table XIX-46. R' No R RR 3 a R3b R4 R6 X Y R7 R8

XIX-46-1 p-Me-Ph H H H Bz OCH 3 F F OH H H XIX-46-2 p-Me-Ph H H CH 3 Bz OCH 3 F F OH H H XIX-46-3 p-Me-Ph H H CH(CH 3)2 Bz OCH 3 F F OH H H XIX-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz OCH 3 F F OH H H XIX-46-5 p-Me-Ph H H CH 2Ph Bz OCH 3 F F OH H H XIX-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz OCH 3 F F OH H H XIX-46-8 p-Me-Ph * H * Bz OCH 3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-47. R3a R' No R1 R2 R3b R4 R6 X Y R7 R8

XIX-47-1 p-F-Ph H H H Bz OCH 3 F F OH H H XIX-47-2 p-F-Ph H H CH 3 Bz OCH 3 F F OH H H XIX-47-3 p-F-Ph H H CH(CH 3) 2 Bz OCH 3 F F OH H H XIX-47-4 p-F-Ph H H CH 2CH(CH 3) 2 Bz OCH 3 F F OH H H XIX-47-5 p-F-Ph H H CH 2Ph Bz OCH 3 F F OH H H XIX-47-6 p-F-Ph H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz OCH 3 F F OH H H XIX-47-8 p-F-Ph * H * Bz OCH 3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-48. No R R2 R 3 a R 3b R 4 R5 R6 X Y R7 R8

XIX-48-1 p-Cl-Ph H H H Bz OCH 3 F F OH H H XIX-48-2 p-Cl-Ph H H CH 3 Bz OCH 3 F F OH H H XIX-48-3 p-Cl-Ph H H CH(CH3) 2 Bz OCH 3 F F OH H H XIX-48-4 p-Cl-Ph H H CH 2CH(CH 3) 2 Bz OCH 3 F F OH H H XIX-48-5 p-Cl-Ph H H CH 2Ph Bz OCH 3 F F OH H H XIX-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz OCH 3 F F OH H H XIX-48-8 p-Cl-Ph * H * Bz OCH 3 F F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-49. No R R2 R 3 a R3 b R4 R5 R6 X Y R7 R8

XIX-49-1 p-Br-Ph H H H Bz OCH3 F F OH H H XIX-49-2 p-Br-Ph H H CH3 Bz OCH3 F F OH H H XIX-49-3 p-Br-Ph H H CH(CH 3)2 Bz OCH3 F F OH H H

_ 20A_

R R2 R 3 R3 b R X R8 No a R4 R Y R7 XIX-49-4 p-Br-Ph H H CH 2CH(CH 3)2 Bz OCH3 F F OH H H XIX-49-5 p-Br-Ph H H CH 2Ph Bz OCH3 F F OH H H XIX-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz OCH3 F F OH H H XIX-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz OCH3 F F OH H H XIX-49-8 p-Br-Ph * H * Bz OCH3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XIX-50. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R8

XIX-50-1 p-I-Ph H H H Bz OCH 3 F F OH H H XIX-50-2 p-I-Ph H H CH 3 Bz OCH 3 F F OH H H XIX-50-3 p-I-Ph H H CH(CH 3)2 Bz OCH 3 F F OH H H XIX-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz OCH 3 F F OH H H XIX-50-5 p-I-Ph H H CH 2Ph Bz OCH 3 F F OH H H XIX-50-6 p-I-Ph H H CH 2-indol-3-yl Bz OCH 3 F F OH H H XIX-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz OCH 3 F F OH H H XIX-50-8 p-I-Ph * H * Bz OCH 3 F F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

0

R8 NH

R2 0 R3b R7 N O R3a P- P O 0NN-

R6 C0 2R 4 OR' R5

Y X

xx

Table XX-1. No R' R2 R3 a R3 b R4 R5 R6 X Y R7 R8

XX-1-1 CH3 H H H CH 3 OCH 3 H F OH H H XX-1-2 CH3 H H CH3 CH 3 OCH 3 H F OH H H XX-1-3 CH3 H H CH(CH3) 2 CH 3 OCH 3 H F OH H H XX-1-4 CH3 H H CH2CH(CH 3) 2 CH 3 OCH 3 H F OH H H XX-1-5 CH3 H H CH2Ph CH 3 OCH 3 H F OH H H

R3 a R3 b R4 R' 6 X Y R7 R' No R R2 R XX-1-6 CH3 H H CH2-indol-3-yl CH 3 OCH 3 H F OH H H XX-1-7 CH3 H H CH2CH2SCH 3 CH 3 OCH 3 H F OH H H XX-1-8 CH3 * H * CH 3 OCH 3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-2. No Rl R 2 R 3 a R3 b 4 R' R 6 X Y R7 R8

XX-2-1 Et H H H CH 3 OCH 3 H F OH H H XX-2-2 Et H H CH 3 CH 3 OCH 3 H F OH H H XX-2-3 Et H H CH(CH3) 2 CH 3 OCH 3 H F OH H H XX-2-4 Et H H CH 2CH(CH3)2 CH 3 OCH 3 H F OH H H XX-2-5 Et H H CH 2Ph CH 3 OCH 3 H F OH H H XX-2-6 Et H H CH 2-indol-3-yl CH 3 OCH 3 H F OH H H XX-2-7 Et H H CH 2CH 2SCH 3 CH 3 OCH 3 H F OH H H XX-2-8 Et * H * CH 3 OCH 3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-3. No R1 R2 R3 a R 3b R4 R R' X Y R7 R8

XX-3-1 'Pr H H H CH 3 OCH3 H F OH H H XX-3-2 'Pr H H CH3 CH3 OCH3 H F OH H H XX-3-3 'Pr H H CH(CH3)2 CH3 OCH3 H F OH H H XX-3-4 Pr H H CH2CH(CH3)2 CH3 OCH3 H F OH H H XX-3-5 Pr H H CH 2Ph CH 3 OCH3 H F OH H H XX-3-6 Pr H H CH 2-indol-3-yl CH3 OCH3 H F OH H H XX-3-7 Pr H H CH2CH2 SCH3 CH3 OCH3 H F OH H H XX-3-8 Pr * H * CH3 OCH3 H F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-4. 9 R1 R2 R3 a RSb R4 R R6 X Y R7 R8 XX-4-1 'Bu H H H CH 3 OCH 3 H F OH H H XX-4-2 'Bu H H CH3 CH3 OCH 3 H F OH H H XX-4-3 'Bu H H CH(CH3)2 CH3 OCH 3 H F OH H H XX-4-4 'Bu H H CH2CH(CH3) 2 CH3 OCH 3 H F OH H H XX-4-5 'Bu H H CH 2Ph CH 3 OCH 3 H F OH H H XX-4-6 'Bu H H CH 2-indol-3-yl CH3 OCH 3 H F OH H H XX-4-7 'Bu H H CH2CH 2SCH 3 CH3 OCH 3 H F OH H H XX-4-8 'Bu * H * CH 3 OCH 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-5. N9 RI R2 R 3a R3b R4 R5 R6 X Y R7 R8

XX-5-1 Ph H H H CH3 OCH 3 H F OH H H XX-5-2 Ph H H CH3 CH3 OCH 3 H F OH H H XX-5-3 Ph H H CH(CH3) 2 CH3 OCH 3 H F OH H H XX-5-4 Ph H H CH2CH(CH3) 2 CH3 OCH 3 H F OH H H XX-5-5 Ph H H CH2Ph CH3 OCH 3 H F OH H H XX-5-6 Ph H H CH2-indol-3-yl CH3 OCH 3 H F OH H H XX-5-7 Ph H H CH2CH 2SCH 3 CH3 OCH 3 H F OH H H XX-5-8 Ph * H * CH 3 OCH 3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-6. R' N9 R1 R2 R 3a R 3b R4 R6 X Y R7 R' XX-6-1 p-Me-Ph H H H CH 3 OCH 3 H F OH H H XX-6-2 p-Me-Ph H H CH3 CH3 OCH 3 H F OH H H XX-6-3 p-Me-Ph H H CH(CH3) 2 CH3 OCH 3 H F OH H H XX-6-4 p-Me-Ph H H CH2CH(CH 3)2 CH3 OCH 3 H F OH H H XX-6-5 p-Me-Ph H H CH 2Ph CH3 OCH 3 H F OH H H XX-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 OCH 3 H F OH H H XX-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 OCH 3 H F OH H H XX-6-8 p-Me-Ph * H * CH 3 OCH 3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-7. R3a R' No R1 R2 R3b R4 R6 X Y R7 R8

XX-7-1 p-F-Ph H H H CH3 OCH3 H F OH H H XX-7-2 p-F-Ph H H CH3 CH3 OCH3 H F OH H H XX-7-3 p-F-Ph H H CH(CH 3) 2 CH3 OCH3 H F OH H H XX-7-4 p-F-Ph H H CH2CH(CH 3) 2 CH3 OCH3 H F OH H H XX-7-6 p-F-Ph H H CH 2Ph CH3 OCH3 H F OH H H XX-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 OCH3 H F OH H H XX-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 OCH3 H F OH H H XX-7-20 p-F-Ph * H * CH 3 OCH3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-8. N9 R1 R2 R3 a R3b R4 R5 R6 X Y R7 R8

XX-8-1 p-Cl-Ph H H H CH 3 OCH 3 H F OH H H XX-8-2 p-Cl-Ph H H CH 3 CH3 OCH 3 H F OH H H XX-8-3 p-Cl-Ph H H CH(CH 3) 2 CH3 OCH 3 H F OH H H XX-8-4 p-Cl-Ph H H CH 2CH(CH 3) 2 CH 3 OCH 3 H F OH H H XX-8-5 p-Cl-Ph H H CH 2Ph CH 3 OCH 3 H F OH H H XX-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 OCH 3 H F OH H H XX-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH3 OCH 3 H F OH H H XX-8-8 p-Cl-Ph * H * CH 3 OCH 3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-9. No R R2 R 3 a R 3b R4 R R X Y R7 R8

XX-9-1 p-Br-Ph H H H CH3 OCH 3 H F OH H H XX-9-2 p-Br-Ph H H CH 3 CH3 OCH 3 H F OH H H XX-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 OCH 3 H F OH H H XX-9-4 p-Br-Ph H H CH 2CH(CH3)2 CH 3 OCH 3 H F OH H H XX-9-6 p-Br-Ph H H CH 2Ph CH3 OCH 3 H F OH H H XX-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 OCH 3 H F OH H H XX-9-8 p-Br-Ph H H CH 2CH2SCH 3 CH 3 OCH 3 H F OH H H XX-9-20 p-Br-Ph * H * CH3 OCH 3 H F OH H H *R2 and R 3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-10. N9 R R2 R3a R3 b R4 R' R 6 X Y R7 R8

XX-10-1 p-I-Ph H H H CH3 OCH 3 H F OH H H XX-10-2 p-I-Ph H H CH3 CH3 OCH 3 H F OH H H XX-10-3 p-I-Ph H H CH(CH3)2 CH3 OCH 3 H F OH H H XX-10-4 p-I-Ph H H CH2CH(CH3) 2 CH3 OCH 3 H F OH H H XX-10-5 p-I-Ph H H CH 2Ph CH3 OCH 3 H F OH H H XX-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 OCH 3 H F OH H H XX-10-7 p-I-Ph H H CH2CH 2SCH 3 CH3 OCH 3 H F OH H H XX-10-8 p-I-Ph * H * CH3 OCH 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-11. No RI R2 R3 a R 3b R4 R5 R 6 X Y R7 R8

XX-11-1 CH3 H H H Et OCH 3 H F OH H H XX-11-2 CH3 H H CH 3 Et OCH 3 H F OH H H XX-11-3 CH3 H H CH(CH3) 2 Et OCH 3 H F OH H H XX-11-4 CH3 H H CH 2CH(CH3)2 Et OCH 3 H F OH H H XX-11-5 CH3 H H CH 2Ph Et OCH 3 H F OH H H XX-11-6 CH3 H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-11-7 CH3 H H CH 2CH2SCH 3 Et OCH 3 H F OH H H XX-11-8 CH3 * H * Et OCH 3 H F OH H H

*R2 and R3b joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-12. No RI 1 R2 R 3a R3 b R4 R5 R 6 X Y R7 R8

XX-12-1 Et H H H Et OCH 3 H F OH H H XX-12-2 Et H H CH 3 Et OCH 3 H F OH H H XX-12-3 Et H H CH(CH3) 2 Et OCH 3 H F OH H H

_200-_

Rl R 2 R3 a R3 b R4 R R' X Y R7 R' No XX-12-4 Et H H CH 2CH(CH3) 2 Et OCH 3 H F OH H H XX-12-5 Et H H CH 2Ph Et OCH 3 H F OH H H XX-12-6 Et H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-12-7 Et H H CH 2CH 2SCH 3 Et OCH 3 H F OH H H XX-12-8 Et * H * Et OCH 3 H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-13. No R R2 R 3a R3b R4 R' R6 X Y R7 R' XX-13-1 'Pr H H H Et OCH 3 H F OH H H XX-13-2 'Pr H H CH3 Et OCH 3 H F OH H H XX-13-3 'Pr H H CH(CH3)2 Et OCH 3 H F OH H H XX-13-4 'Pr H H CH2CH(CH3) 2 Et OCH 3 H F OH H H XX-13-5 'Pr H H CH 2Ph Et OCH 3 H F OH H H XX-13-6 'Pr H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-13-7 Pr H H CH2CH 2SCH 3 Et OCH 3 H F OH H H XX-13-8 Pr * H * Et OCH 3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

AIffl

Table XX-14. No R1 R2 R3 a R3b R4 R' R6 X Y R7 R' XX-14-1 'Bu H H H Et OCH 3 H F OH H H XX-14-2 'Bu H H CH 3 Et OCH 3 H F OH H H XX-14-3 'Bu H H CH(CH 3) 2 Et OCH 3 H F OH H H XX-14-4 'Bu H H CH 2CH(CH 3) 2 Et OCH 3 H F OH H H XX-14-5 'Bu H H CH 2Ph Et OCH 3 H F OH H H XX-14-6 'Bu H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-14-7 'Bu H H CH 2CH2SCH 3 Et OCH 3 H F OH H H XX-14-8 'Bu * H * Et OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-15. N9 R1 R 2 R3a R3 b R4 R5 R6 X Y R7 R' XX-15-1 Ph H H H Et OCH 3 H F OH H H XX-15-2 Ph H H CH3 Et OCH 3 H F OH H H XX-15-3 Ph H H CH(CH 3) 2 Et OCH 3 H F OH H H XX-15-4 Ph H H CH2CH(CH 3) 2 Et OCH 3 H F OH H H XX-15-5 Ph H H CH 2Ph Et OCH 3 H F OH H H XX-15-6 Ph H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-15-7 Ph H H CH2CH 2SCH 3 Et OCH 3 H F OH H H XX-15-8 Ph * H * Et OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-16. No R R2 R 3 a R3b R4 R5 R6 X Y R7 R' XX-16-1 p-Me-Ph H H H Et OCH 3 H F OH H H XX-16-2 p-Me-Ph H H CH3 Et OCH 3 H F OH H H XX-16-3 p-Me-Ph H H CH(CH 3) 2 Et OCH 3 H F OH H H XX-16-4 p-Me-Ph H H CH2CH(CH 3) 2 Et OCH 3 H F OH H H XX-16-5 p-Me-Ph H H CH 2Ph Et OCH 3 H F OH H H XX-16-6 p-Me-Ph H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et OCH 3 H F OH H H XX-16-8 p-Me-Ph * H * Et OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A11 _

Table XX-17. R R2 R 3 R 3b R4 R R X Y R7 R8 No a

XX-17-1 p-F-Ph H H H Et OCH3 H F OH H H XX-17-2 p-F-Ph H H CH3 Et OCH3 H F OH H H XX-17-3 p-F-Ph H H CH(CH3)2 Et OCH3 H F OH H H XX-17-4 p-F-Ph H H CH2CH(CH3) 2 Et OCH 3 H F OH H H XX-17-5 p-F-Ph H H CH 2Ph Et OCH3 H F OH H H XX-17-6 p-F-Ph H H CH 2-indol-3-yl Et OCH3 H F OH H H XX-17-7 p-F-Ph H H CH2CH 2SCH 3 Et OCH 3 H F OH H H XX-17-8 p-F-Ph * H * Et OCH3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-18. R 6 N9 R R2 R 3a R3 b R4 R X Y R7 R8

XX-18-1 p-Cl-Ph H H H Et OCH 3 H F OH H H XX-18-2 p-Cl-Ph H H CH 3 Et OCH 3 H F OH H H XX-18-3 p-Cl-Ph H H CH(CH3) 2 Et OCH 3 H F OH H H XX-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et OCH 3 H F OH H H XX-18-5 p-Cl-Ph H H CH 2Ph Et OCH 3 H F OH H H XX-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et OCH 3 H F OH H H XX-18-8 p-Cl-Ph * H * Et OCH 3 H F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XX-19. No RI R2 R 3 a R 3b R 4 R5 R 6 X Y R7 R8

XX-19-1 p-Br-Ph H H H Et OCH 3 H F OH H H XX-19-2 p-Br-Ph H H CH 3 Et OCH 3 H F OH H H XX-19-3 p-Br-Ph H H CH(CH3) 2 Et OCH 3 H F OH H H XX-19-4 p-Br-Ph H H CH 2CH(CH3)2 Et OCH 3 H F OH H H XX-19-5 p-Br-Ph H H CH 2Ph Et OCH 3 H F OH H H XX-19-6 p-Br-Ph H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et OCH 3 H F OH H H XX-19-8 p-Br-Ph * H * Et OCH 3 H F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

A0')-

Table XX-20. R R2 R 3 a R3b R4 R R6 X Y R7 R' No

XX-20-1 p-I-Ph H H H Et OCH 3 H F OH H H XX-20-2 p-I-Ph H H CH3 Et OCH 3 H F OH H H XX-20-3 p-I-Ph H H CH(CH3)2 Et OCH 3 H F OH H H XX-20-4 p-I-Ph H H CH2CH(CH3) 2 Et OCH 3 H F OH H H XX-20-5 p-I-Ph H H CH 2Ph Et OCH 3 H F OH H H XX-20-6 p-I-Ph H H CH 2-indol-3-yl Et OCH 3 H F OH H H XX-20-7 p-I-Ph H H CH2CH 2SCH 3 Et OCH 3 H F OH H H XX-20-8 p-I-Ph * H * Et OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-21. M R1 R2 R3 a R3 b R4 R R6 X Y R7 R8

XX-21-1 CH3 H H H 'Pr OCH 3 H F OH H H XX-21-2 CH3 H H CH 3 'Pr OCH 3 H F OH H H XX-21-3 CH3 H H CH(CH3) 2 'Pr OCH 3 H F OH H H XX-21-4 CH3 H H CH 2CH(CH3) 2 'Pr OCH 3 H F OH H H XX-21-5 CH3 H H CH 2Ph 'Pr OCH 3 H F OH H H XX-21-6 CH3 H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-21-7 CH3 H H CH 2CH2SCH 3 'Pr OCH 3 H F OH H H XX-21-8 CH3 * H * 'Pr OCH 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-22. No R R2 R3 a R3b R4 R5 R6 X Y R7 R8

XX-22-1 Et H H H 'Pr OCH 3 H F OH H H XX-22-2 Et H H CH 3 'Pr OCH 3 H F OH H H XX-22-3 Et H H CH(CH3) 2 'Pr OCH 3 H F OH H H XX-22-4 Et H H CH 2CH(CH3) 2 'Pr OCH 3 H F OH H H XX-22-5 Et H H CH 2Ph 'Pr OCH 3 H F OH H H XX-22-6 Et H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-22-7 Et H H CH 2CH 2SCH 3 'Pr OCH 3 H F OH H H XX-22-8 Et * H * 'Pr OCH 3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A 1-

Table XX-23. R1 R2 R 3a R3b R4 R' R6 X Y R7 R' No XX-23-1 'Pr H H H 'Pr OCH 3 H F OH H H XX-23-2 'Pr H H CH3 'Pr OCH 3 H F OH H H XX-23-3 'Pr H H CH(CH 3)2 'Pr OCH 3 H F OH H H XX-23-4 Pr H H CH2CH(CH3) 2 'Pr OCH 3 H F OH H H XX-23-5 Pr H H CH 2Ph 'Pr OCH 3 H F OH H H XX-23-6 Pr H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-23-7 Pr H H CH2CH 2SCH 3 'Pr OCH 3 H F OH H H XX-23-8 Pr * H * 'Pr OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-24. No R1 R2 R3 a R3 b R4 R' R6 X Y R7 R' XX-24-1 'Bu H H H 'Pr OCH 3 H F OH H H XX-24-2 'Bu H H CH 3 'Pr OCH 3 H F OH H H XX-24-3 'Bu H H CH(CH3) 2 'Pr OCH 3 H F OH H H XX-24-4 'Bu H H CH 2CH(CH 3)2 'Pr OCH 3 H F OH H H XX-24-5 'Bu H H CH 2Ph 'Pr OCH 3 H F OH H H XX-24-6 'Bu H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-24-7 'Bu H H CH 2CH2SCH 3 'Pr OCH 3 H F OH H H XX-24-8 'Bu * H * 'Pr OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-25. No R1 R2 R3 a R3b R4 R5 R6 X Y R7 R8

XX-25-1 Ph H H H 'Pr OCH 3 H F OH H H XX-25-2 Ph H H CH3 'Pr OCH 3 H F OH H H XX-25-3 Ph H H CH(CH3)2 'Pr OCH 3 H F OH H H XX-25-4 Ph H H CH2CH(CH3) 2 'Pr OCH 3 H F OH H H XX-25-5 Ph H H CH 2Ph 'Pr OCH 3 H F OH H H XX-25-6 Ph H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-25-7 Ph H H CH2CH 2SCH 3 'Pr OCH 3 H F OH H H XX-25-8 Ph * H * 'Pr OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_IA-_

Table XX-26. R R2 R 3 a R3b R4 R' R6 X Y R8 No R7 XX-26-1 p-Me-Ph H H H 'Pr OCH 3 H F OH H H XX-26-2 p-Me-Ph H H CH3 'Pr OCH 3 H F OH H H XX-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr OCH 3 H F OH H H XX-26-4 p-Me-Ph H H CH2CH(CH 3) 2 'Pr OCH 3 H F OH H H XX-26-5 p-Me-Ph H H CH 2Ph 'Pr OCH 3 H F OH H H XX-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr OCH 3 H F OH H H XX-26-8 p-Me-Ph * H * 'Pr OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-27. N9 R1 R2 R3 a R3 b R4 R' R6 X Y R7 R8 XX-27-1 p-F-Ph H H H 'Pr OCH 3 H F OH H H XX-27-2 p-F-Ph H H CH3 'Pr OCH 3 H F OH H H XX-27-3 p-F-Ph H H CH(CH 3) 2 'Pr OCH 3 H F OH H H XX-27-4 p-F-Ph H H CH2CH(CH 3) 2 'Pr OCH 3 H F OH H H XX-27-5 p-F-Ph H H CH 2Ph 'Pr OCH 3 H F OH H H XX-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr OCH 3 H F OH H H XX-27-8 p-F-Ph * H * 'Pr OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-28. No R1 R2 R 3a R3 R4 R5 R6 X Y R7 R8

XX-28-1 p-Cl-Ph H H H 'Pr OCH 3 H F OH H H XX-28-2 p-Cl-Ph H H CH 3 'Pr OCH 3 H F OH H H XX-28-3 p-Cl-Ph H H CH(CH 3)2 'Pr OCH 3 H F OH H H XX-28-4 p-Cl-Ph H H CH 2CH(CH 3) 2 'Pr OCH 3 H F OH H H XX-28-5 p-Cl-Ph H H CH 2Ph 'Pr OCH 3 H F OH H H XX-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr OCH 3 H F OH H H XX-28-8 p-Cl-Ph * H * 'Pr OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-29. No R R 2 R 3a R3b R4 R RX Y R7 R8

XX-29-1 p-Br-Ph H H H 'Pr OCH 3 H F OH H H XX-29-2 p-Br-Ph H H CH 3 'Pr OCH 3 H F OH H H XX-29-3 p-Br-Ph H H CH(CH3) 2 'Pr OCH 3 H F OH H H XX-29-4 p-Br-Ph H H CH 2CH(CH3)2 'Pr OCH 3 H F OH H H XX-29-5 p-Br-Ph H H CH 2Ph 'Pr OCH 3 H F OH H H XX-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-29-7 p-Br-Ph H H CH 2CH2SCH 3 'Pr OCH 3 H F OH H H XX-29-8 p-Br-Ph * H * 'Pr OCH 3 H F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-30. X9 R R2 R3 a R3 b R4 R' R6 X Y R7 R8

XX-30-1 p-I-Ph H H H 'Pr OCH 3 H F OH H H XX-30-2 p-I-Ph H H CH3 'Pr OCH 3 H F OH H H XX-30-3 p-I-Ph H H CH(CH3)2 'Pr OCH 3 H F OH H H XX-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr OCH 3 H F OH H H XX-30-5 p-I-Ph H H CH 2Ph 'Pr OCH 3 H F OH H H XX-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr OCH 3 H F OH H H XX-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr OCH 3 H F OH H H XX-30-8 p-I-Ph * H * 'Pr OCH 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-31. No R R2 R3 a R 3b R4 R R 6 X Y R7 R8

XX-31-1 CH3 H H H "Bu OCH 3 H F OH H H XX-31-2 CH3 H H CH 3 "Bu OCH 3 H F OH H H XX-31-3 CH 3 H H CH(CH3) 2 "Bu OCH 3 H F OH H H XX-31-4 CH 3 H H CH 2CH(CH3)2 "Bu OCH 3 H F OH H H XX-31-5 CH 3 H H CH 2Ph "Bu OCH 3 H F OH H H XX-31-6 CH 3 H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-31-7 CH 3 H H CH 2CH2SCH 3 "Bu OCH 3 H F OH H H XX-31-8 CH 3 * H * "Bu OCH 3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

AIfOr-

Table XX-32. No Rl R 2 R3 a R3b R4 R R' X Y R7 R' XX-32-1 Et H H H "Bu OCH 3 H F OH H H XX-32-2 Et H H CH 3 "Bu OCH 3 H F OH H H XX-32-3 Et H H CH(CH 3)2 "Bu OCH 3 H F OH H H XX-32-4 Et H H CH 2CH(CH3) 2 "Bu OCH 3 H F OH H H XX-32-5 Et H H CH 2Ph "Bu OCH 3 H F OH H H XX-32-6 Et H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-32-7 Et H H CH 2CH 2SCH 3 "Bu OCH 3 H F OH H H XX-32-8 Et * H * "Bu OCH 3 H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-33. R' No R1 R2 R 3a R3 b R4 R6 X Y R7 R' XX-33-1 'Pr H H H "Bu OCH 3 H F OH H H XX-33-2 'Pr H H CH3 "Bu OCH 3 H F OH H H XX-33-3 'Pr H H CH(CH3)2 "Bu OCH 3 H F OH H H XX-33-4 'Pr H H CH2CH(CH3) 2 "Bu OCH 3 H F OH H H XX-33-5 'Pr H H CH 2Ph "Bu OCH 3 H F OH H H XX-33-6 'Pr H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-33-7 'Pr H H CH2CH 2SCH 3 "Bu OCH 3 H F OH H H XX-33-8 'Pr * H * "Bu OCH 3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-34. No RI 1 R2 R3a R 3b R4 R5 R6 X Y R7 R XX-34-1 'Bu H H H "Bu OCH 3 H F OH H H XX-34-2 'Bu H H CH 3 "Bu OCH 3 H F OH H H XX-34-3 'Bu H H CH(CH3) 2 "Bu OCH 3 H F OH H H XX-34-4 'Bu H H CH 2CH(CH3)2 "Bu OCH 3 H F OH H H XX-34-5 'Bu H H CH 2Ph "Bu OCH 3 H F OH H H XX-34-6 'Bu H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-34-7 'Bu H H CH 2CH2SCH 3 "Bu OCH 3 H F OH H H XX-34-8 'Bu * H * "Bu OCH 3 H F OH H H

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-35. N RI R 2 R3a R3 b R4 R5 R6 X Y R7 R XX-35-1 Ph H H H "Bu OCH 3 H F OH H H XX-35-2 Ph H H CH3 "Bu OCH 3 H F OH H H XX-35-3 Ph H H CH(CH3)2 "Bu OCH 3 H F OH H H

A1f'7-

R R2 R3 a R3 b R4 R' R6 X Y R7 R' No XX-35-4 Ph H H CH2CH(CH 3) 2 "Bu OCH 3 H F OH H H XX-35-5 Ph H H CH 2Ph "Bu OCH 3 H F OH H H XX-35-6 Ph H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-35-7 Ph H H CH2CH 2SCH 3 "Bu OCH 3 H F OH H H XX-35-8 Ph * H * "Bu OCH 3 H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-36. No RI R2 R3 a R3 b R4 R' R6 X Y R7 R

XX-36-1 p-Me-Ph H H H "Bu OCH 3 H F OH H H XX-36-2 p-Me-Ph H H CH 3 "Bu OCH 3 H F OH H H XX-36-3 p-Me-Ph H H CH(CH 3) 2 "Bu OCH 3 H F OH H H XX-36-4 p-Me-Ph H H CH 2 CH(CH3) 2 "Bu OCH 3 H F OH H H XX-36-5 p-Me-Ph H H CH 2 Ph "Bu OCH 3 H F OH H H XX-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-36-7 p-Me-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 H F OH H H XX-36-8 p-Me-Ph * H * "Bu OCH 3 H F OH H H *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XX-37. R 6 8 IR R2 R3a R3b R4 R X Y R7 R XX-37-1 p-F-Ph H H H "Bu OCH 3 H F OH H H XX-37-2 p-F-Ph H H CH3 "Bu OCH 3 H F OH H H XX-37-3 p-F-Ph H H CH(CH3)2 "Bu OCH 3 H F OH H H XX-37-4 p-F-Ph H H CH2CH(CH3) 2 "Bu OCH 3 H F OH H H XX-37-5 p-F-Ph H H CH 2Ph "Bu OCH 3 H F OH H H XX-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-37-7 p-F-Ph H H CH2CH 2 SCH 3 "Bu OCH 3 H F OH H H XX-37-8 p-F-Ph * H * "Bu OCH 3 H F OH H H

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-38. No RI R2 R 3a R3 b 4 R5 R6 X Y R7 R8 XX-38-1 p-Cl-Ph H H H "Bu OCH 3 H F OH H H XX-38-2 p-Cl-Ph H H CH 3 "Bu OCH 3 H F OH H H XX-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu OCH 3 H F OH H H XX-38-4 p-Cl-Ph H H CH 2 CH(CH3)2 "Bu OCH 3 H F OH H H XX-38-5 p-Cl-Ph H H CH 2 Ph "Bu OCH 3 H F OH H H XX-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H

AIfQ-

R' No R R2 3 a R R4 R6 X Y R7 R' XX-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu OCH 3 H F OH H H XX-38-8 p-Cl-Ph * H * "Bu OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-39. R R2 R 3 R3 b 4 R R' X Y R7 R' No a

XX-39-1 p-Br-Ph H H H "Bu OCH 3 H F OH H H XX-39-2 p-Br-Ph H H CH 3 "Bu OCH 3 H F OH H H XX-39-3 p-Br-Ph H H CH(CH 3)2 "Bu OCH 3 H F OH H H XX-39-4 p-Br-Ph H H CH 2CH(CH 3) 2 "Bu OCH 3 H F OH H H XX-39-5 p-Br-Ph H H CH 2Ph "Bu OCH 3 H F OH H H XX-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu OCH 3 H F OH H H XX-39-8 p-Br-Ph * H * "Bu OCH 3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XX-40. No RI R2 R3 a R3 b R4 R R6 X Y R7 R

XX-40-1 p-I-Ph H H H "Bu OCH 3 H F OH H H XX-40-2 p-I-Ph H H CH3 "Bu OCH 3 H F OH H H XX-40-3 p-I-Ph H H CH(CH3)2 "Bu OCH 3 H F OH H H XX-40-4 p-I-Ph H H CH2CH(CH3) 2 "Bu OCH 3 H F OH H H XX-40-5 p-I-Ph H H CH 2Ph "Bu OCH 3 H F OH H H XX-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu OCH 3 H F OH H H XX-40-7 p-I-Ph H H CH2CH 2SCH 3 "Bu OCH 3 H F OH H H XX-40-8 p-I-Ph * H * "Bu OCH 3 H F OH H H

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XX-41. I1 R R2 R3a R3b R R6XY R 4 5 7 R XX-41-1 CH3 H H H Bz OCH 3 H F OH H H XX-41-2 CH3 H H CH 3 Bz OCH 3 H F OH H H XX-41-3 CH3 H H CH(CH3) 2 Bz OCH 3 H F OH H H XX-41-4 CH3 H H CH 2CH(CH3)2 Bz OCH 3 H F OH H H XX-41-5 CH3 H H CH 2Ph Bz OCH 3 H F OH H H XX-41-6 CH3 H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-41-7 CH3 H H CH 2CH2SCH 3 Bz OCH 3 H F OH H H XX-41-8 CH3 * H * Bz OCH 3 H F OH H H

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Anol_

Table XX-42. No Rl R 2 R3 a R3b R4 R' R6 X Y R7 R' XX-42-1 Et H H H Bz OCH 3 H F OH H H XX-42-2 Et H H CH 3 Bz OCH 3 H F OH H H XX-42-3 Et H H CH(CH3) 2 Bz OCH 3 H F OH H H XX-42-4 Et H H CH 2CH(CH3) 2 Bz OCH 3 H F OH H H XX-42-5 Et H H CH 2Ph Bz OCH 3 H F OH H H XX-42-6 Et H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-42-7 Et H H CH 2CH 2SCH 3 Bz OCH 3 H F OH H H XX-42-8 Et * H * Bz OCH 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-43. R *R2 and R 3 No RI 1 R2 R3a R3b R4 R R6 X Y R7

XX-43-1 'Pr H H H Bz OCH3 H F OH H I joined XX-43-2 'Pr H H CH3 Bz OCH3 H F OH H H together by XX-43-3 'Pr H H CH(CH3)2 Bz OCH3 H F OH H H (CH 2) 3 to form XX-43-4 'Pr H H CH2CH(CH3) 2 Bz OCH3 H F OH H H five XX-43-5 'Pr H H CH 2Ph Bz OCH3 H F OH H H membered XX-43-6 'Pr H H CH 2-indol-3-yl Bz OCH3 H F OH H H 10 ring. XX-43-7 'Pr H H CH2CH 2SCH 3 Bz OCH3 H F OH H H XX-43-8 'Pr * H * Bz OCH3 H F OH H H Table XX-44. RI 1 2 Ra 3 Rb 3 R 4 R R 6 X Y 7 R No R R

XX-44-1 'Bu H H H Bz OCH 3 H F OH H H XX-44-2 'Bu H H CH 3 Bz OCH 3 H F OH H H XX-44-3 'Bu H H CH(CH3) 2 Bz OCH 3 H F OH H H XX-44-4 'Bu H H CH 2CH(CH3)2 Bz OCH 3 H F OH H H XX-44-5 'Bu H H CH 2Ph Bz OCH 3 H F OH H H XX-44-6 'Bu H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-44-7 'Bu H H CH 2CH2SCH 3 Bz OCH 3 H F OH H H XX-44-8 'Bu * H * Bz OCH 3 H F OH H H *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-45. N RI R 2 R3a R3 b R4 R5 R6 X Y R7 R XX-45-1 Ph H H H Bz OCH 3 H F OH H H XX-45-2 Ph H H CH3 Bz OCH 3 H F OH H H XX-45-3 Ph H H CH(CH 3) 2 Bz OCH 3 H F OH H H XX-45-4 Ph H H CH2CH(CH3) 2 Bz OCH 3 H F OH H H XX-45-5 Ph H H CH 2Ph Bz OCH 3 H F OH H H

A1

R No R1 R2 R3 a R3 b R4 R' X Y R7 R' XX-45-6 Ph H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-45-7 Ph H H CH2CH 2SCH 3 Bz OCH 3 H F OH H H XX-45-8 Ph * H * Bz OCH 3 H F OH H H

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

A11 1

Table XX-46. No R R2 R 3 a R3b R4 R R6 X Y R7 R' XX-46-1 p-Me-Ph H H H Bz OCH 3 H F OH H H XX-46-2 p-Me-Ph H H CH3 Bz OCH 3 H F OH H H XX-46-3 p-Me-Ph H H CH(CH 3) 2 Bz OCH 3 H F OH H H XX-46-4 p-Me-Ph H H CH2CH(CH 3) 2 Bz OCH 3 H F OH H H XX-46-5 p-Me-Ph H H CH 2Ph Bz OCH 3 H F OH H H XX-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz OCH 3 H F OH H H XX-46-8 p-Me-Ph * H * Bz OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-47. N9 R IR2 R3a R3 b R4 R R6 X Y R7 R8

XX-47-1 p-F-Ph H H H Bz OCH 3 H F OH H H XX-47-2 p-F-Ph H H CH3 Bz OCH 3 H F OH H H XX-47-3 p-F-Ph H H CH(CH3)2 Bz OCH 3 H F OH H H XX-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz OCH 3 H F OH H H XX-47-5 p-F-Ph H H CH 2Ph Bz OCH 3 H F OH H H XX-47-6 p-F-Ph H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz OCH 3 H F OH H H XX-47-8 p-F-Ph * H * Bz OCH 3 H F OH H H *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XX-48. No RI 1 R2 R 3a R 3b R4 R5 R6 X Y R7 R8

XX-48-1 p-Cl-Ph H H H Bz OCH 3 H F OH H H XX-48-2 p-Cl-Ph H H CH 3 Bz OCH 3 H F OH H H XX-48-3 p-Cl-Ph H H CH(CH3) 2 Bz OCH 3 H F OH H H XX-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz OCH 3 H F OH H H XX-48-5 p-Cl-Ph H H CH 2Ph Bz OCH 3 H F OH H H XX-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz OCH 3 H F OH H H XX-48-8 p-Cl-Ph * H * Bz OCH 3 H F OH H H *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A11 _

Table XX-49. R No R' R2 R3 a R3b R4 R' X Y R7 R8

XX-49-1 p-Br-Ph H H H Bz OCH 3 H F OH H H XX-49-2 p-Br-Ph H H CH 3 Bz OCH 3 H F OH H H XX-49-3 p-Br-Ph H H CH(CH 3) 2 Bz OCH 3 H F OH H H XX-49-4 p-Br-Ph H H CH 2CH(CH 3) 2 Bz OCH 3 H F OH H H XX-49-5 p-Br-Ph H H CH 2Ph Bz OCH 3 H F OH H H XX-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-49-7 p-Br-Ph H H CH 2CH2SCH 3 Bz OCH 3 H F OH H H XX-49-8 p-Br-Ph * H * Bz OCH 3 H F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XX-50. R3a N9 Rl R2 R3 b R4 R5 R6 X Y R7 R8

XX-50-1 p-I-Ph H H H Bz OCH 3 H F OH H H XX-50-2 p-I-Ph H H CH3 Bz OCH 3 H F OH H H XX-50-3 p-I-Ph H H CH(CH 3) 2 Bz OCH 3 H F OH H H XX-50-4 p-I-Ph H H CH2CH(CH 3) 2 Bz OCH 3 H F OH H H XX-50-5 p-I-Ph H H CH 2Ph Bz OCH 3 H F OH H H XX-50-6 p-I-Ph H H CH 2-indol-3-yl Bz OCH 3 H F OH H H XX-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz OCH 3 H F OH H H XX-50-8 p-I-Ph * H * Bz OCH 3 H F OH H H *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

N

R 3b R2 0(I R3a P R2 0 O N N -- -- O O N N

C0 2 R 4 OR Rs R6 NH 2

Y X XM

A11

Table XXI-1. No R1 R2 R3 a R 3b R4 R 5 R' X Y XXI-1-1 CH 3 H H H CH3 H CH 3 F OH XXI-1-2 CH 3 H H CH3 CH 3 H CH 3 F OH XXI-1-3 CH 3 H H CH(CH 3) 2 CH3 H CH 3 F OH XXI-1-4 CH 3 H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXI-1-5 CH 3 H H CH 2Ph CH3 H CH 3 F OH XXI-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXI-1-7 CH 3 H H CH2CH 2SCH3 CH3 H CH 3 F OH XXI-1-8 CH 3 * H * CH 3 H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-2. N9 R1 R 2 R3a R3 b R4 R' R6 X Y XXI-2-1 Et H H H CH 3 H CH 3 F OH XXI-2-2 Et H H CH 3 CH 3 H CH 3 F OH XXI-2-3 Et H H CH(CH 3) 2 CH 3 H CH 3 F OH XXI-2-4 Et H H CH 2CH(CH 3) 2 CH 3 H CH 3 F OH XXI-2-5 Et H H CH 2Ph CH 3 H CH 3 F OH XXI-2-6 Et H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXI-2-7 Et H H CH 2CH 2SCH 3 CH 3 H CH 3 F OH XXI-2-8 Et * H * CH 3 H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-3. No RI1 R 2 R3 a R3b R4 R 5 R6 X Y

XXI-3-1 'Pr H H H CH 3 H CH3 F OH XXI-3-2 'Pr H H CH 3 CH 3 H CH3 F OH XXI-3-3 'Pr H H CH(CH 3) 2 CH 3 H CH3 F OH XXI-3-4 'Pr H H CH 2CH(CH 3) 2 CH 3 H CH3 F OH XXI-3-5 'Pr H H CH 2Ph CH 3 H CH3 F OH XXI-3-6 'Pr H H CH 2-indol-3-yl CH 3 H CH3 F OH XXI-3-7 'Pr H H CH 2CH2SCH 3 CH 3 H CH3 F OH XXI-3-8 Pr * H * CH 3 H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A1A

Table XXI-4. R3 R No R1 R2 R 3a R4 R' X Y XXI-4-1 'Bu H H H CH3 H CH3 F OH XXI-4-2 'Bu H H CH 3 CH3 H CH3 F OH XXI-4-3 'Bu H H CH(CH3) 2 CH3 H CH3 F OH XXI-4-4 'Bu H H CH 2CH(CH3)2 CH3 H CH3 F OH XXI-4-5 'Bu H H CH 2Ph CH3 H CH3 F OH XXI-4-6 'Bu H H CH 2-indol-3-yl CH3 H CH3 F OH XXI-4-7 'Bu H H CH 2CH2SCH 3 CH3 H CH3 F OH XXI-4-8 'Bu * H * CH3 H CH3 F OH *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-5. R3a No R1 R2 R3b R4 R 5 R6 X y

XXI-5-1 Ph H H H CH 3 H CH 3 F OH XXI-5-2 Ph H H CH3 CH3 H CH 3 F OH XXI-5-3 Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXI-5-4 Ph H H CH2CH(CH 3) 2 CH 3 H CH 3 F OH XXI-5-5 Ph H H CH 2Ph CH 3 H CH 3 F OH XXI-5-6 Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXI-5-7 Ph H H CH2CH 2SCH3 CH3 H CH 3 F OH XXI-5-8 Ph * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-6. No R R2 R 3 a R 3b R4 R5 R6 X Y

XXI-6-1 p-Me-Ph H H H CH 3 H CH 3 F OH XXI-6-2 p-Me-Ph H H CH 3 CH3 H CH 3 F OH XXI-6-3 p-Me-Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXI-6-4 p-Me-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 F OH XXI-6-5 p-Me-Ph H H CH 2Ph CH 3 H CH 3 F OH XXI-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXI-6-7 p-Me-Ph H H CH 2CH 2SCH3 CH3 H CH 3 F OH XXI-6-8 p-Me-Ph * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A1 r,

Table XXI-7. No R RR 3 a R 3b R4 R' R6 X Y XXI-7-1 p-F-Ph H H H CH 3 H CH 3 F OH XXI-7-2 p-F-Ph H H CH 3 CH3 H CH 3 F OH XXI-7-3 p-F-Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXI-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 F OH XXI-7-6 p-F-Ph H H CH 2Ph CH 3 H CH 3 F OH XXI-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXI-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 H CH 3 F OH XXI-7-20 p-F-Ph * H * CH 3 H CH 3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-8. N9 R R2 R3a RSh R4 R R6 X y

XXI-8-1 p-Cl-Ph H H H CH3 H CH3 F OH XXI-8-2 p-Cl-Ph H H CH 3 CH3 H CH3 F OH XXI-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H CH3 F OH XXI-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H CH3 F OH XXI-8-5 p-Cl-Ph H H CH 2Ph CH3 H CH3 F OH XXI-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H CH3 F OH XXI-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H CH3 F OH XXI-8-8 p-Cl-Ph * H * CH3 H CH3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXI-9. No R R2 R 3 a R 3b R4 R5 R6 X Y

XXI-9-1 p-Br-Ph H H H CH 3 H CH 3 F OH XXI-9-2 p-Br-Ph H H CH3 CH 3 H CH 3 F OH XXI-9-3 p-Br-Ph H H CH(CH3)2 CH 3 H CH 3 F OH XXI-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH 3 H CH 3 F OH XXI-9-6 p-Br-Ph H H CH 2Ph CH 3 H CH 3 F OH XXI-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXI-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH 3 H CH 3 F OH XXI-9-20 p-Br-Ph * H * CH 3 H CH 3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

A1 A

Table XXI-10. No R RR 3 a R3b R4 R' R6 X Y XXI-10-1 p-I-Ph H H H CH 3 H CH 3 F OH XXI-10-2 p-I-Ph H H CH 3 CH 3 H CH 3 F OH XXI-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H CH 3 F OH XXI-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 F OH XXI-10-5 p-I-Ph H H CH 2Ph CH 3 H CH 3 F OH XXI-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXI-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H CH 3 F OH XXI-10-8 p-I-Ph * H * CH 3 H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-11. No R1 R2 R3a R3b R4 R5 R6 X Y XXI-11-1 CH 3 H H H Et H CH 3 F OH XXI-11-2 CH 3 H H CH3 Et H CH 3 F OH XXI-11-3 CH 3 H H CH(CH3) 2 Et H CH 3 F OH XXI-11-4 CH 3 H H CH2CH(CH3) 2 Et H CH 3 F OH XXI-11-5 CH 3 H H CH 2Ph Et H CH 3 F OH XXI-11-6 CH 3 H H CH 2-indol-3-yl Et H CH 3 F OH XXI-11-7 CH 3 H H CH2CH 2SCH 3 Et H CH 3 F OH XXI-11-8 CH 3 * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-12. No R R2 R 3a R3b R4 R5 R6 X Y XXI-12-1 Et H H H Et H CH 3 F OH XXI-12-2 Et H H CH3 Et H CH 3 F OH XXI-12-3 Et H H CH(CH3)2 Et H CH 3 F OH XXI-12-4 Et H H CH2CH(CH3) 2 Et H CH 3 F OH XXI-12-5 Et H H CH 2Ph Et H CH 3 F OH XXI-12-6 Et H H CH 2-indol-3-yl Et H CH 3 F OH XXI-12-7 Et H H CH2CH 2SCH 3 Et H CH 3 F OH XXI-12-8 Et * H * Et H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A1'7_

Table XXI-13. R' R2 R3 a R3 b R4 R R X Y No XXI-13-1 'Pr H H H Et H CH3 F OH XXI-13-2 'Pr H H CH 3 Et H CH3 F OH XXI-13-3 'Pr H H CH(CH 3)2 Et H CH3 F OH XXI-13-4 Pr H H CH 2CH(CH3) 2 Et H CH3 F OH XXI-13-5 'Pr H H CH 2Ph Et H CH3 F OH XXI-13-6 'Pr H H CH 2-indol-3-yl Et H CH3 F OH XXI-13-7 Pr H H CH 2 CH2 SCH 3 Et H CH 3 F OH XXI-13-8 'Pr * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-14. No R1 R2 R3 a R3 b R4 R' R6 X Y

XXI-14-1 'Bu H H H Et H CH 3 F OH XXI-14-2 'Bu H H CH 3 Et H CH 3 F OH XXI-14-3 'Bu H H CH(CH3) 2 Et H CH 3 F OH XXI-14-4 'Bu H H CH 2CH(CH 3) 2 Et H CH 3 F OH XXI-14-5 'Bu H H CH 2Ph Et H CH 3 F OH XXI-14-6 'Bu H H CH 2-indol-3-yl Et H CH 3 F OH XXI-14-7 'Bu H H CH 2CH2SCH 3 Et H CH 3 F OH XXI-14-8 'Bu * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-15. No RI 1 R2 R 3a R3b R4 R5 R6 X Y

XXI-15-1 Ph H H H Et H CH 3 F OH XXI-15-2 Ph H H CH3 Et H CH 3 F OH XXI-15-3 Ph H H CH(CH3) 2 Et H CH 3 F OH XXI-15-4 Ph H H CH2CH(CH3)2 Et H CH 3 F OH XXI-15-5 Ph H H CH 2Ph Et H CH3 F OH XXI-15-6 Ph H H CH 2-indol-3-yl Et H CH3 F OH XXI-15-7 Ph H H CH2CH2SCH 3 Et H CH3 F OH XXI-15-8 Ph * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A1 2

Table XXI-16. No R RR 3 a R3b R4 R' R6 X Y

XXI-16-1 p-Me-Ph H H H Et H CH3 F OH XXI-16-2 p-Me-Ph H H CH 3 Et H CH3 F OH XXI-16-3 p-Me-Ph H H CH(CH3) 2 Et H CH3 F OH XXI-16-4 p-Me-Ph H H CH 2CH(CH3)2 Et H CH3 F OH XXI-16-5 p-Me-Ph H H CH 2Ph Et H CH3 F OH XXI-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH3 F OH XXI-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H CH3 F OH XXI-16-8 p-Me-Ph * H * Et H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-17. R3a N9 R R2 R3 b R4 R' R6 X y

XXI-17-1 p-F-Ph H H H Et H CH3 F OH XXI-17-2 p-F-Ph H H CH 3 Et H CH3 F OH XXI-17-3 p-F-Ph H H CH(CH3) 2 Et H CH3 F OH XXI-17-4 p-F-Ph H H CH 2CH(CH 3) 2 Et H CH3 F OH XXI-17-5 p-F-Ph H H CH 2Ph Et H CH3 F OH XXI-17-6 p-F-Ph H H CH 2-indol-3-yl Et H CH3 F OH XXI-17-7 p-F-Ph H H CH 2CH2SCH 3 Et H CH3 F OH XXI-17-8 p-F-Ph * H * Et H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-18. No R R2 R 3 a R 3b R 5 RR X Y

XXI-18-1 p-Cl-Ph H H H Et H CH 3 F OH XXI-18-2 p-Cl-Ph H H CH 3 Et H CH 3 F OH XXI-18-3 p-Cl-Ph H H CH(CH3) 2 Et H CH 3 F OH XXI-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H CH 3 F OH XXI-18-5 p-Cl-Ph H H CH 2Ph Et H CH 3 F OH XXI-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXI-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et H CH 3 F OH XXI-18-8 p-Cl-Ph * H * Et H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A10

Table XXI-19. No R R2 R 3 a R3b R4 R R6 X Y XXI-19-1 p-Br-Ph H H H Et H CH 3 F OH XXI-19-2 p-Br-Ph H H CH3 Et H CH 3 F OH XXI-19-3 p-Br-Ph H H CH(CH3)2 Et H CH 3 F OH XXI-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H CH 3 F OH XXI-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 F OH XXI-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXI-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH XXI-19-8 p-Br-Ph * H * Et H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-20. R3a N9 R R2 R3 b R4 R' R6 X y

XXI-20-1 p-I-Ph H H H Et H CH3 F OH XXI-20-2 p-I-Ph H H CH 3 Et H CH3 F OH XXI-20-3 p-I-Ph H H CH(CH3) 2 Et H CH3 F OH XXI-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H CH3 F OH XXI-20-5 p-I-Ph H H CH 2Ph Et H CH3 F OH XXI-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH3 F OH XXI-20-7 p-I-Ph H H CH 2CH2SCH 3 Et H CH3 F OH XXI-20-8 p-I-Ph * H * Et H CH3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-21. No R1 R2 R 3a R3b R4 R5 R6 X Y

XXI-21-1 CH 3 H H H 'Pr H CH3 F OH XXI-21-2 CH 3 H H CH3 'Pr H CH 3 F OH XXI-21-3 CH 3 H H CH(CH3) 2 'Pr H CH 3 F OH XXI-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXI-21-5 CH 3 H H CH 2Ph 'Pr H CH 3 F OH XXI-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXI-21-8 CH 3 * H * 'Pr H CH 3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

,1')fl

Table XXI-22. Rl R2 R 3a R3b R4 R' R' X Y No

XXI-22-1 Et H H H 'Pr H CH3 F OH XXI-22-2 Et H H CH3 'Pr H CH3 F OH XXI-22-3 Et H H CH(CH3)2 'Pr H CH3 F OH XXI-22-4 Et H H CH2CH(CH3) 2 'Pr H CH3 F OH XXI-22-5 Et H H CH 2Ph 'Pr H CH3 F OH XXI-22-6 Et H H CH 2-indol-3-yl 'Pr H CH3 F OH XXI-22-7 Et H H CH2CH 2SCH 3 'Pr H CH3 F OH XXI-22-8 Et * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-23. No R' R2 R 3aRb R4 R R6 X Y XXI-23-1 'Pr H H H 'Pr H CH 3 F OH XXI-23-2 'Pr H H CH 3 'Pr H CH 3 F OH XXI-23-3 'Pr H H CH(CH3) 2 'Pr H CH 3 F OH XXI-23-4 'Pr H H CH 2CH(CH3) 2 'Pr H CH 3 F OH XXI-23-5 'Pr H H CH 2Ph 'Pr H CH 3 F OH XXI-23-6 'Pr H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-23-7 'Pr H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXI-23-8 'Pr * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-24. No RI R2 R3 a R3b R4 R R X Y XXI-24-1 'Bu H H H 'Pr H CH 3 F OH XXI-24-2 'Bu H H CH 3 'Pr H CH 3 F OH XXI-24-3 'Bu H H CH(CH3) 2 'Pr H CH 3 F OH XXI-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H CH 3 F OH XXI-24-5 'Bu H H CH 2Ph 'Pr H CH 3 F OH XXI-24-6 'Bu H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-24-7 'Bu H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXI-24-8 'Bu * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

/1'1 _

Table XXI-25. R1 R2 R 3a R3b R4 R5 R' X Y No

XXI-25-1 Ph H H H 'Pr H CH 3 F OH XXI-25-2 Ph H H CH3 'Pr H CH 3 F OH XXI-25-3 Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXI-25-4 Ph H H CH2CH(CH 3) 2 'Pr H CH 3 F OH XXI-25-5 Ph H H CH 2Ph 'Pr H CH 3 F OH XXI-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-25-7 Ph H H CH2CH2SCH 3 'Pr H CH 3 F OH XXI-25-8 Ph * H * 'Pr H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-26. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y

XXI-26-1 p-Me-Ph H H H 'Pr H CH 3 F OH XXI-26-2 p-Me-Ph H H CH 3 'Pr H CH 3 F OH XXI-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXI-26-4 p-Me-Ph H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH XXI-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH 3 F OH XXI-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXI-26-8 p-Me-Ph * H * 'Pr H CH 3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-27. No R R2 R 3 a R3b R4 R5 R6 X Y

XXI-27-1 p-F-Ph H H H 'Pr H CH 3 F OH XXI-27-2 p-F-Ph H H CH 3 'Pr H CH 3 F OH XXI-27-3 p-F-Ph H H CH(CH 3)2 'Pr H CH 3 F OH XXI-27-4 p-F-Ph H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH XXI-27-5 p-F-Ph H H CH 2Ph 'Pr H CH 3 F OH XXI-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXI-27-8 p-F-Ph * H * 'Pr H CH 3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A')

Table XXI-28. R No R R2 R 3 a R 3b R4 R X Y XXI-28-1 p-Cl-Ph H H H 'Pr H CH 3 F OH XXI-28-2 p-Cl-Ph H H CH 3 'Pr H CH 3 F OH XXI-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXI-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH XXI-28-5 p-Cl-Ph H H CH 2Ph 'Pr H CH 3 F OH XXI-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXI-28-8 p-Cl-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXI-29. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXI-29-1 p-Br-Ph H H H 'Pr H CH 3 F OH XXI-29-2 p-Br-Ph H H CH3 'Pr H CH 3 F OH XXI-29-3 p-Br-Ph H H CH(CH 3)2 'Pr H CH 3 F OH XXI-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXI-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 F OH XXI-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXI-29-8 p-Br-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXI-30. No R R2 R 3 a R3b R4 R5 R6 X Y XXI-30-1 p-I-Ph H H H 'Pr H CH 3 F OH XXI-30-2 p-I-Ph H H CH 3 'Pr H CH 3 F OH XXI-30-3 p-I-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXI-30-4 p-I-Ph H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH XXI-30-5 p-I-Ph H H CH 2Ph 'Pr H CH 3 F OH XXI-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXI-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXI-30-8 p-I-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXI-31. No R1 R2 R 3a R3b R4 R' R6 X Y XXI-31-1 CH 3 H H H "Bu H CH 3 F OH XXI-31-2 CH 3 H H CH3 "Bu H CH 3 F OH XXI-31-3 CH 3 H H CH(CH3) 2 "Bu H CH 3 F OH XXI-31-4 CH 3 H H CH2CH(CH3) 2 "Bu H CH 3 F OH XXI-31-5 CH 3 H H CH 2Ph "Bu H CH 3 F OH XXI-31-6 CH 3 H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H CH 3 F OH XXI-31-8 CH 3 * H * "Bu H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-32. No R1 R2 R3a R3b R4 R' R6 X Y XXI-32-1 Et H H H "Bu H CH 3 F OH XXI-32-2 Et H H CH3 "Bu H CH 3 F OH XXI-32-3 Et H H CH(CH3)2 "Bu H CH 3 F OH XXI-32-4 Et H H CH2CH(CH3) 2 "Bu H CH 3 F OH XXI-32-5 Et H H CH 2Ph "Bu H CH 3 F OH XXI-32-6 Et H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-32-7 Et H H CH2CH 2SCH 3 "Bu H CH 3 F OH XXI-32-8 Et * H * "Bu H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-33. R' R N R2 R 3a R3b Rt 4 R X Y XXI-33-1 'Pr H H H "Bu H CH 3 F OH XXI-33-2 'Pr H H CH 3 "Bu H CH 3 F OH XXI-33-3 'Pr H H CH(CH3) 2 "Bu H CH 3 F OH XXI-33-4 'Pr H H CH 2CH(CH3) 2 "Bu H CH 3 F OH XXI-33-5 Pr H H CH 2Ph "Bu H CH 3 F OH XXI-33-6 Pr H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-33-7 Pr H H CH 2CH2SCH 3 "Bu H CH 3 F OH XXI-33-8 Pr * H * "Bu H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

AIAI

Table XXI-34. No RI R2 RaR3 b R4 R R X Y XXI-34-1 'Bu H H H "Bu H CH 3 F OH XXI-34-2 'Bu H H CH 3 "Bu H CH 3 F OH XXI-34-3 'Bu H H CH(CH3) 2 "Bu H CH 3 F OH XXI-34-4 'Bu H H CH 2CH(CH3)2 "Bu H CH 3 F OH XXI-34-5 'Bu H H CH 2Ph "Bu H CH 3 F OH XXI-34-6 'Bu H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-34-7 'Bu H H CH 2CH2SCH 3 "Bu H CH 3 F OH XXI-34-8 'Bu * H * "Bu H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-35. No R1 R2 R3a R3b R4 R5 R6 X y XXI-35-1 Ph H H H "Bu H CH 3 F OH XXI-35-2 Ph H H CH3 "Bu H CH 3 F OH XXI-35-3 Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXI-35-4 Ph H H CH2CH(CH3)2 "Bu H CH 3 F OH XXI-35-5 Ph H H CH 2Ph "Bu H CH 3 F OH XXI-35-6 Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-35-7 Ph H H CH2CH2SCH 3 "Bu H CH 3 F OH XXI-35-8 Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-36. No R1 R2 R 3a R3b R4 R5 R6 X Y XXI-36-1 p-Me-Ph H H H "Bu H CH 3 F OH XXI-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 F OH XXI-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H CH 3 F OH XXI-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H CH 3 F OH XXI-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 F OH XXI-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH3 F OH XXI-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXI-36-8 p-Me-Ph * H * "Bu H CH3 F OH *R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

A1Tr-

Table XXI-37. R RR 3 a R3b R4 R' R' X Y No XXI-37-1 p-F-Ph H H H "Bu H CH3 F OH XXI-37-2 p-F-Ph H H CH 3 "Bu H CH3 F OH XXI-37-3 p-F-Ph H H CH(CH3) 2 "Bu H CH3 F OH XXI-37-4 p-F-Ph H H CH 2CH(CH3)2 "Bu H CH3 F OH XXI-37-5 p-F-Ph H H CH 2Ph "Bu H CH3 F OH XXI-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXI-37-8 p-F-Ph * H * "Bu H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-38. N9 R1 R2 R 3a Rb R4 R5 R6 X Y

XXI-38-1 p-Cl-Ph H H H "Bu H CH 3 F OH XXI-38-2 p-Cl-Ph H H CH 3 "Bu H CH 3 F OH XXI-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXI-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H CH 3 F OH XXI-38-5 p-Cl-Ph H H CH 2Ph "Bu H CH 3 F OH XXI-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXI-38-8 p-Cl-Ph * H * "Bu H CH 3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXI-39. No R1 R2 R 3a R3b R4 R5 R6 X Y XXI-39-1 p-Br-Ph H H H "Bu H CH 3 F OH XXI-39-2 p-Br-Ph H H CH 3 "Bu H CH 3 F OH XXI-39-3 p-Br-Ph H H CH(CH3)2 "Bu H CH 3 F OH XXI-39-4 p-Br-Ph H H CH 2 CH(CH3) 2 "Bu H CH 3 F OH XXI-39-5 p-Br-Ph H H CH 2 Ph "Bu H CH 3 F OH XXI-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH XXI-39-8 p-Br-Ph * H * "Bu H CH 3 F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXI-40. R RR 3 R3b R4 R' R' X Y No a

XXI-40-1 p-I-Ph H H H "Bu H CH3 F OH XXI-40-2 p-I-Ph H H CH 3 "Bu H CH3 F OH XXI-40-3 p-I-Ph H H CH(CH3) 2 "Bu H CH3 F OH XXI-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu H CH3 F OH XXI-40-5 p-I-Ph H H CH 2Ph "Bu H CH3 F OH XXI-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXI-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXI-40-8 p-I-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-41. No R1 R2 R3a R3b R4 R' R6 X y XXI-41-1 CH 3 H H H Bz H CH 3 F OH XXI-41-2 CH 3 H H CH3 Bz H CH 3 F OH XXI-41-3 CH 3 H H CH(CH3) 2 Bz H CH 3 F OH XXI-41-4 CH 3 H H CH2CH(CH3) 2 Bz H CH 3 F OH XXI-41-5 CH 3 H H CH 2Ph Bz H CH 3 F OH XXI-41-6 CH 3 H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-41-7 CH 3 H H CH2CH 2SCH 3 Bz H CH 3 F OH XXI-41-8 CH 3 * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-42. No Rl R2 R 3a R3b R4 R5 R6 X Y XXI-42-1 Et H H H Bz H CH 3 F OH XXI-42-2 Et H H CH3 Bz H CH 3 F OH XXI-42-3 Et H H CH(CH3)2 Bz H CH 3 F OH XXI-42-4 Et H H CH2CH(CH3) 2 Bz H CH 3 F OH XXI-42-5 Et H H CH 2Ph Bz H CH 3 F OH XXI-42-6 Et H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-42-7 Et H H CH2CH 2SCH 3 Bz H CH 3 F OH XXI-42-8 Et * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-43. No R' R2 R3 aRb R4 R R6 X Y XXI-43-1 Pr H H H Bz H CH3 F OH XXI-43-2 Pr H H CH 3 Bz H CH3 F OH XXI-43-3 Pr H H CH(CH3) 2 Bz H CH3 F OH XXI-43-4 Pr H H CH 2CH(CH3) 2 Bz H CH3 F OH XXI-43-5 'Pr H H CH 2Ph Bz H CH3 F OI XXI-43-6 'Pr H H CH 2-indol-3-yl Bz H CH3 F OH XXI-43-7 'Pr H H CH 2 CH2 SCH 3 Bz H CH3 F OH XXI-43-8 'Pr * H * Bz H CH3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-44. No R R2 R3 a R3 b R4 R R6 X Y XXI-44-1 'Bu H H H Bz H CH 3 F OH XXI-44-2 'Bu H H CH 3 Bz H CH 3 F OH XXI-44-3 'Bu H H CH(CH3) 2 Bz H CH 3 F OH XXI-44-4 'Bu H H CH 2CH(CH3)2 Bz H CH 3 F OH XXI-44-5 'Bu H H CH 2Ph Bz H CH 3 F OH XXI-44-6 'Bu H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-44-7 'Bu H H CH 2 CH2 SCH 3 Bz H CH 3 F OH XXI-44-8 'Bu * H * Bz H CH 3 F OH

*R2and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-45. No Rl R2 R3a R3b R4 R5 R6 X Y XXI-45-1 Ph H H H Bz H CH 3 F OH XXI-45-2 Ph H H CH3 Bz H CH 3 F OH XXI-45-3 Ph H H CH(CH3) 2 Bz H CH 3 F OH XXI-45-4 Ph H H CH2CH(CH3)2 Bz H CH 3 F OH XXI-45-5 Ph H H CH 2Ph Bz H CH 3 F OH XXI-45-6 Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-45-7 Ph H H CH2CH2SCH 3 Bz H CH 3 F OH XXI-45-8 Ph * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-46. No R RR 3 a R3b R4 R 5 R6 X Y XXI-46-1 p-Me-Ph H H H Bz H CH 3 F OH XXI-46-2 p-Me-Ph H H CH 3 Bz H CH 3 F OH XXI-46-3 p-Me-Ph H H CH(CH 3)2 Bz H CH 3 F OH XXI-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz H CH 3 F OH XXI-46-5 p-Me-Ph H H CH 2Ph Bz H CH 3 F OH XXI-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH XXI-46-8 p-Me-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-47. N R1 R2 R3a R3b R4 R5 R6 X Y XXI-47-1 p-F-Ph H H H Bz H CH 3 F OH XXI-47-2 p-F-Ph H H CH 3 Bz H CH 3 F OH XXI-47-3 p-F-Ph H H CH(CH3) 2 Bz H CH 3 F OH XXI-47-4 p-F-Ph H H CH 2CH(CH3)2 Bz H CH 3 F OH XXI-47-5 p-F-Ph H H CH 2Ph Bz H CH 3 F OH XXI-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH XXI-47-8 p-F-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXI-48. No R R2 R 3 a R 3b R4 R5 R6 X Y

XXI-48-1 p-Cl-Ph H H H Bz H CH3 F OH XXI-48-2 p-Cl-Ph H H CH 3 Bz H CH3 F OH XXI-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H CH3 F OH XXI-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H CH3 F OH XXI-48-5 p-Cl-Ph H H CH 2Ph Bz H CH3 F OH XXI-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H CH3 F OH XXI-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz H CH3 F OH XXI-48-8 p-Cl-Ph * H * Bz H CH3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 1o0

Table XXI-49. R3b R' No R R2 R 3 a R4 R' X Y XXI-49-1 p-Br-Ph H H H Bz H CH 3 F OH XXI-49-2 p-Br-Ph H H CH3 Bz H CH 3 F OH XXI-49-3 p-Br-Ph H H CH(CH 3)2 Bz H CH 3 F OH XXI-49-4 p-Br-Ph H H CH2CH(CH 3)2 Bz H CH 3 F OH XXI-49-5 p-Br-Ph H H CH 2Ph Bz H CH 3 F OH XXI-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH XXI-49-8 p-Br-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXI-50. N9 Rl R2 R3a R3 b R4 R5 R6 X Y XXI-50-1 p-I-Ph H H H Bz H CH 3 F OH XXI-50-2 p-I-Ph H H CH 3 Bz H CH 3 F OH XXI-50-3 p-I-Ph H H CH(CH 3)2 Bz H CH 3 F OH XXI-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz H CH 3 F OH XXI-50-5 p-I-Ph H H CH 2Ph Bz H CH 3 F OH XXI-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXI-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH XXI-50-8 p-I-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

N

R3b R2 O N N P 0 N R3a N- - O \

4 C0 2 R OR' Rs R6 NH 2

Y X XXII

AA'.fl

Table XXII-1. No R1 R2 R3 a R3b R4 RR 6 X Y

XXII-1-1 CH 3 H H H CH 3 H F H OH XXII-1-2 CH 3 H H CH3 CH 3 H F H OH XXII-1-3 CH 3 H H CH(CH3) 2 CH 3 H F H OH XXII-1-4 CH 3 H H CH2CH(CH3) 2 CH 3 H F H OH XXII-1-5 CH 3 H H CH 2Ph CH 3 H F H OH XXII-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H F H OH XXII-1-7 CH 3 H H CH2CH 2SCH 3 CH 3 H F H OH XXII-1-8 CH 3 * H * CH 3 H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-2. No R1 R2 R3a R3 b R4 R' R6 X Y XXII-2-1 Et H H H CH 3 H F H OH XXII-2-2 Et H H CH3 CH 3 H F H OH XXII-2-3 Et H H CH(CH3)2 CH 3 H F H OH XXII-2-4 Et H H CH2CH(CH3) 2 CH 3 H F H OH XXII-2-5 Et H H CH 2Ph CH 3 H F H OH XXII-2-6 Et H H CH 2-indol-3-yl CH 3 H F H OH XXII-2-7 Et H H CH2CH 2SCH 3 CH 3 H F H OH XXII-2-8 Et * H * CH 3 H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-3. N R' R2 R3 a R3b R4 R R 6 X Y

XXII-3-1 'Pr H H H CH3 H F H OH XXII-3-2 'Pr H H CH 3 CH3 H F H OH XXII-3-3 'Pr H H CH(CH3) 2 CH3 H F H OH XXII-3-4 'Pr H H CH 2CH(CH3)2 CH3 H F H OH XXII-3-5 Pr H H CH 2Ph CH3 H F H OH XXII-3-6 Pr H H CH 2-indol-3-yl CH3 H F H OH XXII-3-7 Pr H H CH 2CH2SCH 3 CH3 H F H OH XXII-3-8 Pr * H * CH3 H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A21

Table XXII-4. No RI R2 RaR 3 b R4 RR X Y XXII-4-1 'Bu H H H CH 3 H F H OH XXII-4-2 'Bu H H CH3 CH 3 H F H OH XXII-4-3 'Bu H H CH(CH3) 2 CH 3 H F H OH XXII-4-4 'Bu H H CH2CH(CH3)2 CH 3 H F H OH XXII-4-5 'Bu H H CH2Ph CH 3 H F H OH XXII-4-6 'Bu H H CH2-indol-3-yl CH 3 H F H OH XXII-4-7 'Bu H H CH2CH2SCH 3 CH 3 H F H OH XXII-4-8 'Bu * H * CH 3 H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-5. R3a No R1 R2 R3 b R4 R5 R6 X Y XXII-5-1 Ph H H H CH 3 H F H OH XXII-5-2 Ph H H CH3 CH3 H F H OH XXII-5-3 Ph H H CH(CH3) 2 CH3 H F H OH XXII-5-4 Ph H H CH2CH(CH3)2 CH 3 H F H OH XXII-5-5 Ph H H CH 2Ph CH 3 H F H OH XXII-5-6 Ph H H CH 2-indol-3-yl CH3 H F H OH XXII-5-7 Ph H H CH2CH2SCH 3 CH3 H F H OH XXII-5-8 Ph * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-6. No R R2 R 3 a R3b R4 R5 R6 X Y XXII-6-1 p-Me-Ph H H H CH 3 H F H OH XXII-6-2 p-Me-Ph H H CH3 CH3 H F H OH XXII-6-3 p-Me-Ph H H CH(CH3) 2 CH3 H F H OH XXII-6-4 p-Me-Ph H H CH2CH(CH 3) 2 CH 3 H F H OH XXII-6-5 p-Me-Ph H H CH 2Ph CH 3 H F H OH XXII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F H OH XXII-6-7 p-Me-Ph H H CH2CH2SCH 3 CH3 H F H OH XXII-6-8 p-Me-Ph * H * CH 3 H F H OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

All-

Table XXII-7. 6 No R R2 R 3 a R3 R4 R R X Y XXII-7-1 p-F-Ph H H H CH 3 H F H OH XXII-7-2 p-F-Ph H H CH 3 CH 3 H F H OH XXII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 H F H OH XXII-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 H F H OH XXII-7-6 p-F-Ph H H CH 2Ph CH 3 H F H OH XXII-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H F H OH XXII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH 3 H F H OH XXII-7-20 p-F-Ph * H * CH 3 H F H OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-8. N9 R1 R 2 R 3a R3 b R4 R R6 X Y XXII-8-1 p-Cl-Ph H H H CH 3 H F H OH XXII-8-2 p-Cl-Ph H H CH 3 CH 3 H F H OH XXII-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F H OH XXII-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H F H OH XXII-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F H OH XXII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F H OH XXII-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H F H OH XXII-8-8 p-Cl-Ph * H * CH 3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXII-9. No R R2 R 3 a R 3b R4 R 5 R 6 X Y

XXII-9-1 p-Br-Ph H H H CH3 H F H OH XXII-9-2 p-Br-Ph H H CH 3 CH3 H F H OH XXII-9-3 p-Br-Ph H H CH(CH3)2 CH3 H F H OH XXII-9-4 p-Br-Ph H H CH 2CH(CH3) 2 CH3 H F H OH XXII-9-6 p-Br-Ph H H CH 2Ph CH3 H F H OH XXII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H F H OH XXII-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH3 H F H OH XXII-9-20 p-Br-Ph * H * CH3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

All2

Table XXII-10. No R R2 R 3a R3 R4 R R X Y XXII-10-1 p-I-Ph H H H CH 3 H F H OH XXII-10-2 p-I-Ph H H CH 3 CH 3 H F H OH XXII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H F H OH XXII-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H F H OH XXII-10-5 p-I-Ph H H CH 2Ph CH 3 H F H OH XXII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H F H OH XXII-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H F H OH XXII-10-8 p-I-Ph * H * CH 3 H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-11. No R1 R2 R3a R3 b R4 R R X Y

XXII-11-1 CH 3 H H H Et H F H OH XXII-11-2 CH 3 H H CH3 Et H F H OH XXII-11-3 CH 3 H H CH(CH3)2 Et H F H OH XXII-11-4 CH 3 H H CH2CH(CH3) 2 Et H F H OH XXII-11-5 CH 3 H H CH 2Ph Et H F H OH XXII-11-6 CH 3 H H CH 2-indol-3-yl Et H F H OH XXII-11-7 CH 3 H H CH2CH 2SCH 3 Et H F H OH XXII-11-8 CH 3 * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-12. 5 6 No Rl R2 R3a R 3b R4 R R X Y

XXII-12-1 Et H H H Et H F H OH XXII-12-2 Et H H CH3 Et H F H OH XXII-12-3 Et H H CH(CH3)2 Et H F H OH XXII-12-4 Et H H CH2CH(CH3) 2 Et H F H OH XXII-12-5 Et H H CH 2Ph Et H F H OH XXII-12-6 Et H H CH 2-indol-3-yl Et H F H OH XXII-12-7 Et H H CH2CH2 SCH3 Et H F H OH XXII-12-8 Et * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

IA-

Table XXII-13. R' No R2 R3 a R3 b R4 R R X Y XXII-13-1 'Pr H H H Et H F H OH XXII-13-2 'Pr H H CH 3 Et H F H OH XXII-13-3 'Pr H H CH(CH 3)2 Et H F H OH XXII-13-4 Pr H H CH 2CH(CH3) 2 Et H F H OH XXII-13-5 'Pr H H CH 2Ph Et H F H OH XXII-13-6 Pr H H CH 2-indol-3-yl Et H F H OH XXII-13-7 Pr H H CH 2 CH 2 SCH 3 Et H F H OH XXII-13-8 Pr * H * Et H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-14. N R I R2 R3a R3 b R4 R' R6 X Y XXII-14-1 'Bu H H H Et H F H OH XXII-14-2 'Bu H H CH 3 Et H F H OH XXII-14-3 'Bu H H CH(CH3) 2 Et H F H OH XXII-14-4 'Bu H H CH 2CH(CH 3) 2 Et H F H OH XXII-14-5 'Bu H H CH 2Ph Et H F H OH XXII-14-6 'Bu H H CH 2-indol-3-yl Et H F H OH XXII-14-7 'Bu H H CH 2CH2SCH 3 Et H F H OH XXII-14-8 'Bu * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-15. No RI 1 R2 R3 a R 3b 4 R tR R X Y

XXII-15-1 Ph H H H Et H F H OH XXII-15-2 Ph H H CH3 Et H F H OH XXII-15-3 Ph H H CH(CH3) 2 Et H F H OH XXII-15-4 Ph H H CH2CH(CH3)2 Et H F H OH XXII-15-5 Ph H H CH 2Ph Et H F H OH XXII-15-6 Ph H H CH 2-indol-3-yl Et H F H OH XXII-15-7 Ph H H CH2CH2SCH 3 Et H F H OH XXII-15-8 Ph * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-16. No R RR 3 a R3 R 4 R' R6 X Y XXII-16-1 p-Me-Ph H H H Et H F H OH XXII-16-2 p-Me-Ph H H CH 3 Et H F H OH XXII-16-3 p-Me-Ph H H CH(CH3) 2 Et H F H OH XXII-16-4 p-Me-Ph H H CH 2CH(CH3)2 Et H F H OH XXII-16-5 p-Me-Ph H H CH 2Ph Et H F H OH XXII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F H OH XXII-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H F H OH XXII-16-8 p-Me-Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-17. N9 R1 R2 R3 a RS R 4 R' R6 X Y XXII-17-1 p-F-Ph H H H Et H F H OH XXII-17-2 p-F-Ph H H CH 3 Et H F H OH XXII-17-3 p-F-Ph H H CH(CH3) 2 Et H F H OH XXII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et H F H OH XXII-17-5 p-F-Ph H H CH 2Ph Et H F H OH XXII-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F H OH XXII-17-7 p-F-Ph H H CH 2CH2SCH 3 Et H F H OH XXII-17-8 p-F-Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-18. No R R2 R 3 a R 3b R4 R5 R6 X Y XXII-18-1 p-Cl-Ph H H H Et H F H OH XXII-18-2 p-Cl-Ph H H CH 3 Et H F H OH XXII-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F H OH XXII-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et H F H OH XXII-18-5 p-Cl-Ph H H CH 2Ph Et H F H OH XXII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F H OH XXII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H F H OH XXII-18-8 p-Cl-Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A2A-,

Table XXII-19. No R R2 R 3 a R 3b R4 R' R6 X Y XXII-19-1 p-Br-Ph H H H Et H F H OH XXII-19-2 p-Br-Ph H H CH 3 Et H F H OH XXII-19-3 p-Br-Ph H H CH(CH3)2 Et H F H OH XXII-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et H F H OH XXII-19-5 p-Br-Ph H H CH 2Ph Et H F H OH XXII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F H OH XXII-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H F H OH XXII-19-8 p-Br-Ph * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-20. N9 R1 R2 R3 a RS R4 R' R6 X Y XXII-20-1 p-I-Ph H H H Et H F H OH XXII-20-2 p-I-Ph H H CH 3 Et H F H OH XXII-20-3 p-I-Ph H H CH(CH3) 2 Et H F H OH XXII-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H F H OH XXII-20-5 p-I-Ph H H CH 2Ph Et H F H OH XXII-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F H OH XXII-20-7 p-I-Ph H H CH 2CH2SCH 3 Et H F H OH XXII-20-8 p-I-Ph * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-21. N9 R1 R2 R3 a R 3b R4 R 5 R6 X Y

XXII-21-1 CH 3 H H H Pr H F H OH XXII-21-2 CH 3 H H CH3 'Pr H F H OH XXII-21-3 CH 3 H H CH(CH3)2 'Pr H F H OH XXII-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H F H OH XXII-21-5 CH 3 H H CH 2Ph 'Pr H F H OH XXII-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H F H OH XXII-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H F H OH XXII-21-8 CH 3 * H * 'Pr H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A'7-

Table XXII-22. No Rl R2 R3 a R 3b R4 R' R' X Y XXII-22-1 Et H H H 'Pr H F H OH XXII-22-2 Et H H CH3 'Pr H F H OH XXII-22-3 Et H H CH(CH 3) 2 'Pr H F H OH XXII-22-4 Et H H CH2CH(CH3) 2 'Pr H F H OH XXII-22-5 Et H H CH 2Ph 'Pr H F H OH XXII-22-6 Et H H CH 2-indol-3-yl 'Pr H F H OH XXII-22-7 Et H H CH2CH2 SCH3 'Pr H F H OH XXII-22-8 Et * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-23. 6 No R' R2 R3 a R3 b R 4 R R X Y XXII-23-1 'Pr H H H 'Pr H F H OH XXII-23-2 'Pr H H CH 3 'Pr H F H OH XXII-23-3 'Pr H H CH(CH3) 2 'Pr H F H OH XXII-23-4 'Pr H H CH 2CH(CH3) 2 'Pr H F H OH XXII-23-5 'Pr H H CH 2Ph 'Pr H F H OH XXII-23-6 'Pr H H CH 2-indol-3-yl 'Pr H F H OH XXII-23-7 'Pr H H CH 2CH 2SCH 3 'Pr H F H OH XXII-23-8 'Pr * H * 'Pr H F H OH

*R2 and R 3b joined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-24. No R1 R2 R3 a R3b R4 R R X Y XXII-24-1 'Bu H H H Pr H F H OH XXII-24-2 'Bu H H CH 3 'Pr H F H OH XXII-24-3 'Bu H H CH(CH3) 2 'Pr H F H OH XXII-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H F H OH XXII-24-5 'Bu H H CH 2Ph 'Pr H F H OH XXII-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F H OH XXII-24-7 'Bu H H CH 2CH2SCH 3 'Pr H F H OH XXII-24-8 'Bu * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A 'IQ

Table XXII-25. No R1 R2 R3 a R3 R4 R 5 R' X Y XXII-25-1 Ph H H H 'Pr H F H OH XXII-25-2 Ph H H CH3 'Pr H F H OH XXII-25-3 Ph H H CH(CH3) 2 'Pr H F H OH XXII-25-4 Ph H H CH2CH(CH 3) 2 'Pr H F H OH XXII-25-5 Ph H H CH 2Ph 'Pr H F H OH XXII-25-6 Ph H H CH 2-indol-3-yl 'Pr H F H OH XXII-25-7 Ph H H CH2CH2SCH 3 'Pr H F H OH XXII-25-8 Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-26. N9 R1 R2 R3 a RS R4 R 5 R6 X Y XXII-26-1 p-Me-Ph H H H 'Pr H F H OH XXII-26-2 p-Me-Ph H H CH 3 'Pr H F H OH XXII-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H F H OH XXII-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr H F H OH XXII-26-5 p-Me-Ph H H CH 2Ph 'Pr H F H OH XXII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXII-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H F H OH XXII-26-8 p-Me-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-27. No R R2 R 3 a R3 R4 R5 R6 X Y XXII-27-1 p-F-Ph H H H 'Pr H F H OH XXII-27-2 p-F-Ph H H CH 3 'Pr H F H OH XXII-27-3 p-F-Ph H H CH(CH 3)2 'Pr H F H OH XXII-27-4 p-F-Ph H H CH 2CH(CH 3) 2 'Pr H F H OH XXII-27-5 p-F-Ph H H CH 2Ph 'Pr H F H OH XXII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H F H OH XXII-27-8 p-F-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A0

Table XXII-28. No R R2 R 3 a R 3b R4 R 5 R6 X Y XXII-28-1 p-Cl-Ph H H H 'Pr H F H OH XXII-28-2 p-Cl-Ph H H CH 3 'Pr H F H OH XXII-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F H OH XXII-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr H F H OH XXII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F H OH XXII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXII-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H F H OH XXII-28-8 p-Cl-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXII-29. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y XXII-29-1 p-Br-Ph H H H 'Pr H F H OH XXII-29-2 p-Br-Ph H H CH 3 'Pr H F H OH XXII-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F H OH XXII-29-4 p-Br-Ph H H CH 2CH(CH3) 2 'Pr H F H OH XXII-29-5 p-Br-Ph H H CH 2Ph 'Pr H F H OH XXII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXII-29-7 p-Br-Ph H H CH 2CH 2SCH 3 'Pr H F H OH XXII-29-8 p-Br-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXII-30. No R R2 R 3 a R3 R4 R 5 R6 X Y XXII-30-1 p-I-Ph H H H 'Pr H F H OH XXII-30-2 p-I-Ph H H CH 3 'Pr H F H OH XXII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F H OH XXII-30-4 p-I-Ph H H CH 2CH(CH 3) 2 'Pr H F H OH XXII-30-5 p-I-Ph H H CH 2Ph 'Pr H F H OH XXII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXII-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H F H OH XXII-30-8 p-I-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AAnl_

Table XXII-31. No R1 R2 R3 a R 3b R4 R' R6 X Y XXII-31-1 CH 3 H H H "Bu H F H OH XXII-31-2 CH 3 H H CH3 "Bu H F H OH XXII-31-3 CH 3 H H CH(CH3)2 "Bu H F H OH XXII-31-4 CH 3 H H CH2CH(CH3) 2 "Bu H F H OH XXII-31-5 CH 3 H H CH 2Ph "Bu H F H OH XXII-31-6 CH 3 H H CH 2-indol-3-yl "Bu H F H OH XXII-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H F H OH XXII-31-8 CH 3 * H * "Bu H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-32. No R1 R2 R3a R3 b R4 R' R6 X Y XXII-32-1 Et H H H "Bu H F H OH XXII-32-2 Et H H CH3 "Bu H F H OH XXII-32-3 Et H H CH(CH3)2 "Bu H F H OH XXII-32-4 Et H H CH2CH(CH3) 2 "Bu H F H OH XXII-32-5 Et H H CH 2Ph "Bu H F H OH XXII-32-6 Et H H CH 2-indol-3-yl "Bu H F H OH XXII-32-7 Et H H CH2CH2 SCH3 "Bu H F H OH XXII-32-8 Et * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-33. R' N R2 R3 a R3b R4 R5 R X Y XXII-33-1 'Pr H H H "Bu H F H OH XXII-33-2 'Pr H H CH 3 "Bu H F H OH XXII-33-3 'Pr H H CH(CH3) 2 "Bu H F H OH XXII-33-4 'Pr H H CH 2CH(CH3)2 "Bu H F H OH XXII-33-5 Pr H H CH 2Ph "Bu H F H OH XXII-33-6 Pr H H CH 2-indol-3-yl "Bu H F H OH XXII-33-7 Pr H H CH 2CH 2SCH 3 "Bu H F H OH XXII-33-8 Pr * H * "Bu H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

AA1 _

Table XXII-34. No R1 R2 R3 a R3b R4 R R X Y XXII-34-1 'Bu H H H "Bu H F H OH XXII-34-2 'Bu H H CH 3 "Bu H F H OH XXII-34-3 'Bu H H CH(CH 3)2 "Bu H F H OH XXII-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H F H OH XXII-34-5 'Bu H H CH 2Ph "Bu H F H OH XXII-34-6 'Bu H H CH 2-indol-3-yl "Bu H F H OH XXII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F H OH XXII-34-8 'Bu * H * "Bu H F H OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXII-35. No R1 R2 R3a R3b R4 R5 R 6 X Y XXII-35-1 Ph H H H "Bu H F H OH XXII-35-2 Ph H H CH3 "Bu H F H OH XXII-35-3 Ph H H CH(CH3) 2 "Bu H F H OH XXII-35-4 Ph H H CH2CH(CH 3) 2 "Bu H F H OH XXII-35-5 Ph H H CH 2Ph "Bu H F H OH XXII-35-6 Ph H H CH 2-indol-3-yl "Bu H F H OH XXII-35-7 Ph H H CH2CH2SCH 3 "Bu H F H OH XXII-35-8 Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXII-36. No R1 R2 R3a R 3b R4 R R X Y XXII-36-1 p-Me-Ph H H H "Bu H F H OH XXII-36-2 p-Me-Ph H H CH 3 "Bu H F H OH XXII-36-3 p-Me-Ph H H CH(CH3) 2 "Bu H F H OH XXII-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H F H OH XXII-36-5 p-Me-Ph H H CH 2Ph "Bu H F H OH XXII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F H OH XXII-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXII-36-8 p-Me-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

-AA')-

Table XXII-37. No R R2 R 3 a R3 R4 R R X Y XXII-37-1 p-F-Ph H H H "Bu H F H OH XXII-37-2 p-F-Ph H H CH 3 "Bu H F H OH XXII-37-3 p-F-Ph H H CH(CH 3)2 "Bu H F H OH XXII-37-4 p-F-Ph H H CH 2CH(CH3)2 "Bu H F H OH XXII-37-5 p-F-Ph H H CH 2Ph "Bu H F H OH XXII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F H OH XXII-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXII-37-8 p-F-Ph * H * "Bu H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-38. 6 N9 R1 R2 R3 a R3 b R4 RR X Y XXII-38-1 p-Cl-Ph H H H "Bu H F H OH XXII-38-2 p-Cl-Ph H H CH 3 "Bu H F H OH XXII-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F H OH XXII-38-4 p-Cl-Ph H H CH 2CH(CH3) 2 "Bu H F H OH XXII-38-5 p-Cl-Ph H H CH 2Ph "Bu H F H OH XXII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F H OH XXII-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXII-38-8 p-Cl-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXII-39. No R1 R2 R 3 a R 3b R4 R 5 R6 X Y XXII-39-1 p-Br-Ph H H H "Bu H F H OH XXII-39-2 p-Br-Ph H H CH 3 "Bu H F H OH XXII-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F H OH XXII-39-4 p-Br-Ph H H CH 2CH(CH3) 2 "Bu H F H OH XXII-39-5 p-Br-Ph H H CH 2Ph "Bu H F H OH XXII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F H OH XXII-39-7 p-Br-Ph H H CH 2CH 2 SCH 3 "Bu H F H OH XXII-39-8 p-Br-Ph * H * "Bu H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

AA2-

Table XXII-40. No R R2 R 3a R3 R4 R R X Y XXII-40-1 p-I-Ph H H H "Bu H F H OH XXII-40-2 p-I-Ph H H CH 3 "Bu H F H OH XXII-40-3 p-I-Ph H H CH(CH3) 2 "Bu H F H OH XXII-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu H F H OH XXII-40-5 p-I-Ph H H CH 2Ph "Bu H F H OH XXII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F H OH XXII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXII-40-8 p-I-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-41. 5 No R1 R2 R3a R3 b R4 R R6 X Y XXII-41-1 CH 3 H H H Bz H F H OH XXII-41-2 CH 3 H H CH3 Bz H F H OH XXII-41-3 CH 3 H H CH(CH3)2 Bz H F H OH XXII-41-4 CH 3 H H CH2CH(CH3) 2 Bz H F H OH XXII-41-5 CH 3 H H CH 2Ph Bz H F H OH XXII-41-6 CH 3 H H CH 2-indol-3-yl Bz H F H OH XXII-41-7 CH 3 H H CH2CH 2SCH 3 Bz H F H OH XXII-41-8 CH 3 * H * Bz H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-42. No Rl R2 R3a R 3b R4 R 5 R6 X Y XXII-42-1 Et H H H Bz H F H OH XXII-42-2 Et H H CH3 Bz H F H OH XXII-42-3 Et H H CH(CH3)2 Bz H F H OH XXII-42-4 Et H H CH2CH(CH3) 2 Bz H F H OH XXII-42-5 Et H H CH 2Ph Bz H F H OH XXII-42-6 Et H H CH 2-indol-3-yl Bz H F H OH XXII-42-7 Et H H CH2CH2 SCH3 Bz H F H OH XXII-42-8 Et * H * Bz H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

-AAA-

Table XXII-43. No R' R2 R3 aRb R4 R R6 X Y XXII-43-1 Pr H H H Bz H F H OH XXII-43-2 Pr H H CH 3 Bz H F H OH XXII-43-3 Pr H H CH(CH3) 2 Bz H F H OH XXII-43-4 Pr H H CH 2CH(CH3) 2 Bz H F H OH XXII-43-5 'Pr H H CH 2Ph Bz H F H OYI XXII-43-6 'Pr H H CH 2-indol-3-yl Bz H F H OH XXII-43-7 'Pr H H CH 2 CH 2 SCH 3 Bz H F H OH XXII-43-8 'Pr * H * Bz H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-44. No R R2 R3 a R3 b R4 R R6 X Y XXII-44-1 'Bu H H H Bz H F H OH XXII-44-2 'Bu H H CH 3 Bz H F H OH XXII-44-3 'Bu H H CH(CH3) 2 Bz H F H OH XXII-44-4 'Bu H H CH 2CH(CH3)2 Bz H F H OH XXII-44-5 'Bu H H CH 2Ph Bz H F H OH XXII-44-6 'Bu H H CH 2-indol-3-yl Bz H F H OH XXII-44-7 'Bu H H CH 2 CH 2 SCH 3 Bz H F H OH XXII-44-8 'Bu * H * Bz H F H OH

*R2and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-45. N Rl R2 R3a Rb R4 R5 R6 X Y XXII-45-1 Ph H H H Bz H F H OH XXII-45-2 Ph H H CH3 Bz H F H OH XXII-45-3 Ph H H CH(CH3) 2 Bz H F H OH XXII-45-4 Ph H H CH2CH(CH3)2 Bz H F H OH XXII-45-5 Ph H H CH 2Ph Bz H F H OH XXII-45-6 Ph H H CH 2-indol-3-yl Bz H F H OH XXII-45-7 Ph H H CH2CH2SCH 3 Bz H F H OH XXII-45-8 Ph * H * Bz H F H OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A A r,

Table XXII-46. R3 6 No R R2 R 3 a R4 R R X Y XXII-46-1 p-Me-Ph H H H Bz H F H OH XXII-46-2 p-Me-Ph H H CH 3 Bz H F H OH XXII-46-3 p-Me-Ph H H CH(CH3)2 Bz H F H OH XXII-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz H F H OH XXII-46-5 p-Me-Ph H H CH 2Ph Bz H F H OH XXII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F H OH XXII-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H F H OH XXII-46-8 p-Me-Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-47. 6 N9 R1 R 2 R3 a R R4 R R X Y XXII-47-1 p-F-Ph H H H Bz H F H OH XXII-47-2 p-F-Ph H H CH 3 Bz H F H OH XXII-47-3 p-F-Ph H H CH(CH 3)2 Bz H F H OH XXII-47-4 p-F-Ph H H CH 2CH(CH 3) 2 Bz H F H OH XXII-47-5 p-F-Ph H H CH 2Ph Bz H F H OH XXII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F H OH XXII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz H F H OH XXII-47-8 p-F-Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-48. No R R2 R 3 a R 3b R4 R 5 R 6 X Y

XXII-48-1 p-Cl-Ph H H H Bz H F H OH XXII-48-2 p-Cl-Ph H H CH 3 Bz H F H OH XXII-48-3 p-Cl-Ph H H CH(CH 3)2 Bz H F H OH XXII-48-4 p-Cl-Ph H H CH 2CH(CH3) 2 Bz H F H OH XXII-48-5 p-Cl-Ph H H CH 2Ph Bz H F H OH XXII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F H OH XXII-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H F H OH XXII-48-8 p-Cl-Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AAAr,

Table XXII-49. 5 No R R2 R 3 a R 3b R4 R R' X Y XXII-49-1 p-Br-Ph H H H Bz H F H OH XXII-49-2 p-Br-Ph H H CH 3 Bz H F H OH XXII-49-3 p-Br-Ph H H CH(CH3)2 Bz H F H OH XXII-49-4 p-Br-Ph H H CH 2CH(CH3) 2 Bz H F H OH XXII-49-5 p-Br-Ph H H CH 2Ph Bz H F H OH XXII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F H OH XXII-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz H F H OH XXII-49-8 p-Br-Ph * H * Bz H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXII-50. N9 Rl R2 R 3a RS R4 R 5 R 6 X Y

XXII-50-1 p-I-Ph H H H Bz H F H OH XXII-50-2 p-I-Ph H H CH 3 Bz H F H OH XXII-50-3 p-I-Ph H H CH(CH3) 2 Bz H F H OH XXII-50-4 p-I-Ph H H CH 2CH(CH3)2 Bz H F H OH XXII-50-5 p-I-Ph H H CH 2Ph Bz H F H OH XXII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F H OH XXII-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H F H OH XXII-50-8 p-I-Ph * H * Bz H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

N

R3b R2 O N N P 0 0 N R3a N- ---- 0 I N

C0 2 R4 OR1 R5 R6 NH 2

Y X XXIII

Table XXIII-1. R 5 6 No R2 R 3a R3 b R4 R R X Y

XXIII-1-1 CH 3 H H H CH 3 H F F OH XXIII-1-2 CH 3 H H CH3 CH3 H F F OH XXIII-1-3 CH 3 H H CH(CH3)2 CH3 H F F OH

AA'7-

No R R2 R 3a R3 b R4 R' R6 X Y XXIII-1-4 CH 3 H H CH2CH(CH3) 2 CH 3 H F F OH XXIII-1-5 CH 3 H H CH 2Ph CH 3 H F F OH XXIII-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H F F OH XXIII-1-7 CH 3 H H CH2CH 2SCH 3 CH 3 H F F OH XXIII-1-8 CH 3 * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-2. 6 X No Rl R2 R 3a R 3b R4 RR Y XXIII-2-1 Et H H H CH 3 H F F OH XXIII-2-2 Et H H CH 3 CH 3 H F F OH XXIII-2-3 Et H H CH(CH3)2 CH 3 H F F OH XXIII-2-4 Et H H CH 2CH(CH3) 2 CH 3 H F F OH XXIII-2-5 Et H H CH 2Ph CH 3 H F F OH XXIII-2-6 Et H H CH 2-indol-3-yl CH 3 H F F OH XXIII-2-7 Et H H CH 2CH 2SCH 3 CH 3 H F F OH XXIII-2-8 Et * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-3. No R' R2 R3a R3 b R4 R R6 X Y XXIII-3-1 Pr H H H CH 3 H F F OH XXIII-3-2 Pr H H CH3 CH 3 H F F OH XXIII-3-3 'Pr H H CH(CH3) 2 CH 3 H F F OH XXIII-3-4 'Pr H H CH2CH(CH3)2 CH 3 H F F OH XXIII-3-5 'Pr H H CH2Ph CH 3 H F F OH XXIII-3-6 'Pr H H CH2-indol-3-yl CH 3 H F F OH XXIII-3-7 'Pr H H CH2CH2SCH 3 CH 3 H F F OH XXIII-3-8 'Pr * H * CH 3 H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-4. R No R2 R3 a R3b R4 R5 R6 X Y

XXIII-4-1 'Bu H H H CH 3 H F F OH XXIII-4-2 'Bu H H CH 3 CH 3 H F F OH XXIII-4-3 'Bu H H CH(CH3) 2 CH 3 H F F OH XXIII-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H F F OH XXIII-4-5 'Bu H H CH 2Ph CH 3 H F F OH XXIII-4-6 'Bu H H CH 2-indol-3-yl CH 3 H F F OH

AAQ-

R No R2 R3 a R3 b R4 R' R' X Y XXIII-4-7 'Bu H H CH 2CH 2SCH 3 CH 3 H F F OH XXIII-4-8 'Bu * H * CH 3 H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-5. R 5 No R2 R 3a Rb R4 R R' X Y XXIII-5-1 Ph H H H CH3 H F F OH XXIII-5-2 Ph H H CH 3 CH3 H F F OH XXIII-5-3 Ph H H CH(CH3) 2 CH3 H F F OH XXIII-5-4 Ph H H CH 2CH(CH3)2 CH3 H F F OH XXIII-5-5 Ph H H CH 2Ph CH3 H F F OH XXIII-5-6 Ph H H CH 2-indol-3-yl CH3 H F F OH XXIII-5-7 Ph H H CH 2CH2SCH 3 CH3 H F F OH XXIII-5-8 Ph * H * CH3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-6. N9 Rl R2 R 3a RS R4 R5 R 6 X Y XXIII-6-1 p-Me-Ph H H H CH3 H F F OH XXIII-6-2 p-Me-Ph H H CH 3 CH3 H F F OH XXIII-6-3 p-Me-Ph H H CH(CH3) 2 CH3 H F F OH XXIII-6-4 p-Me-Ph H H CH 2CH(CH3)2 CH3 H F F OH XXIII-6-5 p-Me-Ph H H CH 2Ph CH3 H F F OH XXIII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F F OH XXIII-6-7 p-Me-Ph H H CH 2CH 2SCH 3 CH3 H F F OH XXIII-6-8 p-Me-Ph * H * CH3 H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-7. No R R2 R 3a R R4 R5 R 6 X Y XXIII-7-1 p-F-Ph H H H CH 3 H F F OH XXIII-7-2 p-F-Ph H H CH 3 CH 3 H F F OH XXIII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 H F F OH XXIII-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 H F F OH XXIII-7-6 p-F-Ph H H CH 2Ph CH 3 H F F OH XXIII-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H F F OH XXIII-7-8 p-F-Ph H H CH 2CH 2SCH 3 CH 3 H F F OH XXIII-7-20 p-F-Ph * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AAO_

Table XXIII-8. No R R2 R 3 a R 3b R4 R 5 R' X Y XXIII-8-1 p-Cl-Ph H H H CH3 H F F OH XXIII-8-2 p-Cl-Ph H H CH 3 CH 3 H F F OH XXIII-8-3 p-Cl-Ph H H CH(CH3) 2 CH3 H F F OH XXIII-8-4 p-Cl-Ph H H CH 2CH(CH3) 2 CH3 H F F OH XXIII-8-5 p-Cl-Ph H H CH 2Ph CH3 H F F OH XXIII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F F OH XXIII-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH3 H F F OH XXIII-8-8 p-Cl-Ph * H * CH3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-9. 6 N9 R1 R2 R3 a R3 b R4 RR X Y

XXIII-9-1 p-Br-Ph H H H CH 3 H F F OH XXIII-9-2 p-Br-Ph H H CH3 CH3 H F F OH XXIII-9-3 p-Br-Ph H H CH(CH3)2 CH3 H F F OH XXIII-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH3 H F F OH XXIII-9-6 p-Br-Ph H H CH 2Ph CH 3 H F F OH XXIII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H F F OH XXIII-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 H F F OH XXIII-9-20 p-Br-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-10. No R R2 R 3 a R3b R4 R5 R 6 X Y XXIII-10-1 p-I-Ph H H H CH 3 H F F OH XXIII-10-2 p-I-Ph H H CH 3 CH 3 H F F OH XXIII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H F F OH XXIII-10-4 p-I-Ph H H CH 2CH(CH3) 2 CH 3 H F F OH XXIII-10-5 p-I-Ph H H CH 2Ph CH 3 H F F OH XXIII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H F F OH XXIII-10-7 p-I-Ph H H CH 2CH2SCH 3 CH 3 H F F OH XXIII-10-8 p-I-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-11. No R1 R2 R3 a R3 b R4 R5 R6 X Y XXIII-11-1 CH 3 H H H Et H F F OH XXIII-11-2 CH 3 H H CH3 Et H F F OH XXIII-11-3 CH3 H H CH(CH3)2 Et H F F OH

No R R2 R3 a R3 b R4 R' R6 X Y XXIII-11-4 CH 3 H H CH2CH(CH3) 2 Et H F F OH XXIII-11-5 CH 3 H H CH 2Ph Et H F F OH XXIII-11-6 CH3 H H CH 2-indol-3-yl Et H F F OH XXIII-11-7 CH3 H H CH2CH 2SCH 3 Et H F F OH XXIII-11-8 CH3 * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-12. No Rl R 2 R3 a R3b R4 R' R6 X Y XXIII-12-1 Et H H H Et H F F OH XXIII-12-2 Et H H CH3 Et H F F OH XXIII-12-3 Et H H CH(CH3)2 Et H F F OH XXIII-12-4 Et H H CH2CH(CH3) 2 Et H F F OH XXIII-12-5 Et H H CH 2Ph Et H F F OH XXIII-12-6 Et H H CH 2-indol-3-yl Et H F F OH XXIII-12-7 Et H H CH2CH 2SCH 3 Et H F F OH XXIII-12-8 Et * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-13. N9 R R2 R3 a R3 b R 4 R R6 X Y XXIII-13-1 Pr H H H Et H F F OH XXIII-13-2 Pr H H CH 3 Et H F F OH XXIII-13-3 'Pr H H CH(CH3) 2 Et H F F OH XXIII-13-4 'Pr H H CH 2CH(CH3)2 Et H F F OH XXIII-13-5 'Pr H H CH 2Ph Et H F F OH XXIII-13-6 'Pr H H CH 2-indol-3-yl Et H F F OH XXIII-13-7 'Pr H H CH 2CH 2SCH 3 Et H F F OH XXIII-13-8 'Pr * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-14. No R R2 R3a R3b R4 R5 R6 X Y

XXIII-14-1 'Bu H H H Et H F F OH XXIII-14-2 'Bu H H CH 3 Et H F F OH XXIII-14-3 'Bu H H CH(CH3) 2 Et H F F OH XXIII-14-4 'Bu H H CH 2CH(CH3) 2 Et H F F OH XXIII-14-5 'Bu H H CH 2Ph Et H F F OH XXIII-14-6 'Bu H H CH 2-indol-3-yl Et H F F OH

A1 _

R R2 R3a R3 b R4 R' R' X Y No XXIII-14-7 'Bu H H CH 2CH 2SCH 3 Et H F F OH XXIII-14-8 'Bu * H * Et H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-15. No RI R2 R3 a RIR 4 R5 R' X Y XXIII-15-1 Ph H H H Et H F F OH XXIII-15-2 Ph H H CH 3 Et H F F OH XXIII-15-3 Ph H H CH(CH3) 2 Et H F F OH XXIII-15-4 Ph H H CH 2CH(CH3)2 Et H F F OH XXIII-15-5 Ph H H CH 2Ph Et H F F OH XXIII-15-6 Ph H H CH 2-indol-3-yl Et H F F OH XXIII-15-7 Ph H H CH 2CH 2SCH 3 Et H F F OH XXIII-15-8 Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-16. R3 a R3 b 4 R RIt R No RI R2 X Y

XXIII-16-1 p-Me-Ph H H H Et H F F OH XXIII-16-2 p-Me-Ph H H CH 3 Et H F F OH XXIII-16-3 p-Me-Ph H H CH(CH3) 2 Et H F F OH XXIII-16-4 p-Me-Ph H H CH 2CH(CH3) 2 Et H F F OH XXIII-16-5 p-Me-Ph H H CH 2Ph Et H F F OH XXIII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F F OH XXIII-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H F F OH XXIII-16-8 p-Me-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-17. I1 R R2 R 3a R 3bR 4 R 5 R6 X Y

XXIII-17-1 p-F-Ph H H H Et H F F OH XXIII-17-2 p-F-Ph H H CH 3 Et H F F OH XXIII-17-3 p-F-Ph H H CH(CH3) 2 Et H F F OH XXIII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et H F F OH XXIII-17-5 p-F-Ph H H CH 2Ph Et H F F OH XXIII-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F F OH XXIII-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H F F OH XXIII-17-8 p-F-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Ar,)-

Table XXIII-18. No R R2 R 3 a R3b R4 R R X Y

XXIII-18-1 p-Cl-Ph H H H Et H F F OH XXIII-18-2 p-Cl-Ph H H CH 3 Et H F F OH XXIII-18-3 p-Cl-Ph H H CH(CH 3)2 Et H F F OH XXIII-18-4 p-Cl-Ph H H CH 2CH(CH 3) 2 Et H F F OH XXIII-18-5 p-Cl-Ph H H CH 2Ph Et H F F OH XXIII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F F OH XXIII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H F F OH XXIII-18-8 p-Cl-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-19. No R RR 3 a R3b R4 R' R6 X Y XXIII-19-1 p-Br-Ph H H H Et H F F OH XXIII-19-2 p-Br-Ph H H CH 3 Et H F F OH XXIII-19-3 p-Br-Ph H H CH(CH3)2 Et H F F OH XXIII-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et H F F OH XXIII-19-5 p-Br-Ph H H CH 2Ph Et H F F OH XXIII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F F OH XXIII-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H F F OH XXIII-19-8 p-Br-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-20. 9 R1 R2 R3 a R3 b R4 R R6 X Y XXIII-20-1 p-I-Ph H H H Et H F F OH XXIII-20-2 p-I-Ph H H CH 3 Et H F F OH XXIII-20-3 p-I-Ph H H CH(CH3) 2 Et H F F OH XXIII-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H F F OH XXIII-20-5 p-I-Ph H H CH 2Ph Et H F F OH XXIII-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F F OH XXIII-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H F F OH XXIII-20-8 p-I-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-21. V R1 R2 R3 a R3b R4 R 5 R6 X Y XXIII-21-1 CH 3 H H H 'Pr H F F OH XXIII-21-2 CH 3 H H CH3 'Pr H F F OH XXIII-21-3 CH 3 H H CH(CH 3) 2 'Pr H F F OH XXIII-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H F F OH XXIII-21-5 CH 3 H H CH 2Ph 'Pr H F F OH XXIII-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H F F OH XXIII-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H F F OH XXIII-21-8 CH 3 * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A rAA

Table XXIII-22. No Rl R 2 R3 a R3b R4 R' R' X Y XXIII-22-1 Et H H H 'Pr H F F OH XXIII-22-2 Et H H CH3 'Pr H F F OH XXIII-22-3 Et H H CH(CH 3) 2 'Pr H F F OH XXIII-22-4 Et H H CH2CH(CH3) 2 'Pr H F F OH XXIII-22-5 Et H H CH 2Ph 'Pr H F F OH XXIII-22-6 Et H H CH 2-indol-3-yl 'Pr H F F OH XXIII-22-7 Et H H CH2CH 2SCH 3 'Pr H F F OH XXIII-22-8 Et * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-23. No R1 R2 R3 aRb R4 R R 6 X Y XXIII-23-1 'Pr H H H 'Pr H F F OH XXIII-23-2 'Pr H H CH 3 'Pr H F F OH XXIII-23-3 'Pr H H CH(CH3) 2 'Pr H F F OH XXIII-23-4 'Pr H H CH 2CH(CH3) 2 'Pr H F F OH XXIII-23-5 'Pr H H CH 2Ph 'Pr H F F OH XXIII-23-6 'Pr H H CH 2-indol-3-yl 'Pr H F F OH XXIII-23-7 'Pr H H CH 2CH2SCH 3 'Pr H F F OH XXIII-23-8 'Pr * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-24. No R1 R2 R 3a R3b R4 R R XY XXIII-24-1 'Bu H H H 'Pr H F F OH XXIII-24-2 'Bu H H CH 3 'Pr H F F OH XXIII-24-3 'Bu H H CH(CH3) 2 'Pr H F F OH XXIII-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H F F OH XXIII-24-5 'Bu H H CH 2Ph 'Pr H F F OH XXIII-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F F OH XXIII-24-7 'Bu H H CH 2CH2SCH 3 'Pr H F F OH XXIII-24-8 'Bu * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-25. RI No R2 R3 aR3 b R4 RR X Y XXIII-25-1 Ph H H H 'Pr H F F OH XXIII-25-2 Ph H H CH 3 'Pr H F F OH XXIII-25-3 Ph H H CH(CH3) 2 'Pr H F F OH XXIII-25-4 Ph H H CH 2CH(CH3) 2 'Pr H F F OH XXIII-25-5 Ph H H CH 2Ph 'Pr H F F OH XXIII-25-6 Ph H H CH 2-indol-3-yl 'Pr H F F OH XXIII-25-7 Ph H H CH 2CH2SCH 3 'Pr H F F OH XXIII-25-8 Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-26. 5 N9 R1 R2 R3 aRSb R4 R R6 X Y XXIII-26-1 p-Me-Ph H H H 'Pr H F F OH XXIII-26-2 p-Me-Ph H H CH 3 'Pr H F F OH XXIII-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H F F OH XXIII-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr H F F OH XXIII-26-5 p-Me-Ph H H CH 2Ph 'Pr H F F OH XXIII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXIII-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXIII-26-8 p-Me-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-27. No R R2 R 3 a R3 R4 R 5 R6 X Y XXIII-27-1 p-F-Ph H H H 'Pr H F F OH XXIII-27-2 p-F-Ph H H CH 3 'Pr H F F OH XXIII-27-3 p-F-Ph H H CH(CH 3)2 'Pr H F F OH XXIII-27-4 p-F-Ph H H CH 2CH(CH 3)2 'Pr H F F OH XXIII-27-5 p-F-Ph H H CH 2Ph 'Pr H F F OH XXIII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXIII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXIII-27-8 p-F-Ph * H * Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-28. No R R2 R 3 a R3b R4 R' R6 X Y XXIII-28-1 p-Cl-Ph H H H 'Pr H F F OH XXIII-28-2 p-Cl-Ph H H CH3 'Pr H F F OH XXIII-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F F OH XXIII-28-4 p-Cl-Ph H H CH2CH(CH3) 2 'Pr H F F OH XXIII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F F OH XXIII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXIII-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXIII-28-8 p-Cl-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-29. 9 R1 R2 R3 a R3 b R4 R' R6 X Y XXIII-29-1 p-Br-Ph H H H 'Pr H F F OH XXIII-29-2 p-Br-Ph H H CH3 'Pr H F F OH XXIII-29-3 p-Br-Ph H H CH(CH3)2 'Pr H F F OH XXIII-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F F OH XXIII-29-5 p-Br-Ph H H CH 2Ph 'Pr H F F OH XXIII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXIII-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXIII-29-8 p-Br-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-30. 6 No R R 2 R 3a R3b R4 R R X Y

XXIII-30-1 p-I-Ph H H H 'Pr H F F OH XXIII-30-2 p-I-Ph H H CH 3 'Pr H F F OH XXIII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F F OH XXIII-30-4 p-I-Ph H H CH 2CH(CH3) 2 'Pr H F F OH XXIII-30-5 p-I-Ph H H CH 2Ph 'Pr H F F OH XXIII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXIII-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXIII-30-8 p-I-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A r7-

Table XXIII-31. No R1 R2 R3 a R3b R4 R' R6 X Y XXIII-31-1 CH 3 H H H "Bu H F F OH XXIII-31-2 CH 3 H H CH3 "Bu H F F OH XXIII-31-3 CH3 H H CH(CH3)2 "Bu H F F OH XXIII-31-4 CH3 H H CH2CH(CH3) 2 "Bu H F F OH XXIII-31-5 CH3 H H CH 2Ph "Bu H F F OH XXIII-31-6 CH3 H H CH 2-indol-3-yl "Bu H F F OH XXIII-31-7 CH3 H H CH2CH 2SCH 3 "Bu H F F OH XXIII-31-8 CH3 * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-32. No R1 R2 R3a R3 R4 R' R6 X Y XXIII-32-1 Et H H H "Bu H F F OH XXIII-32-2 Et H H CH3 "Bu H F F OH XXIII-32-3 Et H H CH(CH3)2 "Bu H F F OH XXIII-32-4 Et H H CH2CH(CH3) 2 "Bu H F F OH XXIII-32-5 Et H H CH 2Ph "Bu H F F OH XXIII-32-6 Et H H CH 2-indol-3-yl "Bu H F F OH XXIII-32-7 Et H H CH2CH 2SCH 3 "Bu H F F OH XXIII-32-8 Et * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-33. No R1 22 R3 a R3b R4 R R 6 X Y XXIII-33-1 'Pr H H H "Bu H F F OH XXIII-33-2 'Pr H H CH 3 "Bu H F F OH XXIII-33-3 'Pr H H CH(CH3) 2 "Bu H F F OH XXIII-33-4 'Pr H H CH 2CH(CH3)2 "Bu H F F OH XXIII-33-5 Pr H H CH 2Ph "Bu H F F OH XXIII-33-6 Pr H H CH 2-indol-3-yl "Bu H F F OH XXIII-33-7 Pr H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-33-8 Pr * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-34. No R1 R2 R 3a R3b R4 RR X Y XXIII-34-1 'Bu H H H "Bu H F F OH XXIII-34-2 'Bu H H CH 3 "Bu H F F OH XXIII-34-3 'Bu H H CH(CH3) 2 "Bu H F F OH XXIII-34-4 'Bu H H CH 2CH(CH3)2 "Bu H F F OH XXIII-34-5 'Bu H H CH 2Ph "Bu H F F OH XXIII-34-6 'Bu H H CH 2-indol-3-yl "Bu H F F OH XXIII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-34-8 'Bu * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-35. M R1 R2 R3 a R3b R4 R5 R 6 X Y XXIII-35-1 Ph H H H "Bu H F F OH XXIII-35-2 Ph H H CH 3 "Bu H F F OH XXIII-35-3 Ph H H CH(CH3) 2 "Bu H F F OH XXIII-35-4 Ph H H CH 2CH(CH3)2 "Bu H F F OH XXIII-35-5 Ph H H CH 2Ph "Bu H F F OH XXIII-35-6 Ph H H CH 2-indol-3-yl "Bu H F F OH XXIII-35-7 Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-35-8 Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-36. No RI1 R2 R3 a R3b 4 R5 R6 X Y XXIII-36-1 p-Me-Ph H H H "Bu H F F OH XXIII-36-2 p-Me-Ph H H CH 3 "Bu H F F OH XXIII-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H F F OH XXIII-36-4 p-Me-Ph H H CH 2CH(CH3) 2 "Bu H F F OH XXIII-36-5 p-Me-Ph H H CH 2Ph "Bu H F F OH XXIII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F F OH XXIII-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-36-8 p-Me-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

_ ro _

Table XXIII-37. No R R2 R 3a R3 R4 R R X Y XXIII-37-1 p-F-Ph H H H "Bu H F F OH XXIII-37-2 p-F-Ph H H CH 3 "Bu H F F OH XXIII-37-3 p-F-Ph H H CH(CH 3) 2 "Bu H F F OH XXIII-37-4 p-F-Ph H H CH 2CH(CH3)2 "Bu H F F OH XXIII-37-5 p-F-Ph H H CH 2Ph "Bu H F F OH XXIII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F F OH XXIII-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-37-8 p-F-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-38. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXIII-38-1 p-Cl-Ph H H H "Bu H F F OH XXIII-38-2 p-Cl-Ph H H CH 3 "Bu H F F OH XXIII-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F F OH XXIII-38-4 p-Cl-Ph H H CH 2CH(CH 3)2 "Bu H F F OH XXIII-38-5 p-Cl-Ph H H CH 2Ph "Bu H F F OH XXIII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F F OH XXIII-38-7 p-Cl-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-38-8 p-Cl-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIII-39. No R1 R2 R3 a R3b R4 R5 R6 X Y XXIII-39-1 p-Br-Ph H H H "Bu H F F OH XXIII-39-2 p-Br-Ph H H CH 3 "Bu H F F OH XXIII-39-3 p-Br-Ph H H CH(CH3)2 "Bu H F F OH XXIII-39-4 p-Br-Ph H H CH 2 CH(CH3) 2 "Bu H F F OH XXIII-39-5 p-Br-Ph H H CH 2Ph "Bu H F F OH XXIII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F F OH XXIII-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH XXIII-39-8 p-Br-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AI rl-

Table XXIII-40. No R R2 R3 a R3b R4 R R X Y XXIII-40-1 p-I-Ph H H H "Bu H F F OH XXIII-40-2 p-I-Ph H H CH 3 "Bu H F F OH XXIII-40-3 p-I-Ph H H CH(CH 3) 2 "Bu H F F OH XXIII-40-4 p-I-Ph H H CH 2CH(CH3)2 "Bu H F F OH XXIII-40-5 p-I-Ph H H CH 2Ph "Bu H F F OH XXIII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F F OH XXIII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXIII-40-8 p-I-Ph * H * "Bu H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-41. 5 No R1 R2 R3a R3 b R4 R R6 X Y XXIII-41-1 CH 3 H H H Bz H F F OH XXIII-41-2 CH 3 H H CH3 Bz H F F OH XXIII-41-3 CH3 H H CH(CH3)2 Bz H F F OH XXIII-41-4 CH3 H H CH2CH(CH3) 2 Bz H F F OH XXIII-41-5 CH3 H H CH 2Ph Bz H F F OH XXIII-41-6 CH3 H H CH 2-indol-3-yl Bz H F F OH XXIII-41-7 CH3 H H CH2CH 2SCH 3 Bz H F F OH XXIII-41-8 CH3 * H * Bz H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-42. No Rl R 2 R3 a R3b R4 R 5 R6 X Y XXIII-42-1 Et H H H Bz H F F OH XXIII-42-2 Et H H CH3 Bz H F F OH XXIII-42-3 Et H H CH(CH3)2 Bz H F F OH XXIII-42-4 Et H H CH2CH(CH3) 2 Bz H F F OH XXIII-42-5 Et H H CH 2Ph Bz H F F OH XXIII-42-6 Et H H CH 2-indol-3-yl Bz H F F OH XXIII-42-7 Et H H CH2CH 2SCH 3 Bz H F F OH XXIII-42-8 Et * H * Bz H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

AA1 _

Table XXIII-43. No R1 R2 R3 a R3 b R4 R R6 X Y XXIII-43-1 Pr H H H Bz H F F OH XXIII-43-2 Pr H H CH 3 Bz H F F OH XXIII-43-3 Pr H H CH(CH3) 2 Bz H F F OH XXIII-43-4 Pr H H CH 2CH(CH3) 2 Bz H F F OH XXIII-43-5 'Pr H H CH 2Ph Bz H F F OYI XXIII-43-6 'Pr H H CH 2-indol-3-yl Bz H F F OH XXIII-43-7 'Pr H H CH 2CH2SCH 3 Bz H F F OH XXIII-43-8 'Pr * H * Bz H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-44. R No R2 R 3a R3 b R4 R R 6 X Y

XXIII-44-1 'Bu H H H Bz H F F OH XXIII-44-2 'Bu H H CH 3 Bz H F F OH XXIII-44-3 'Bu H H CH(CH3) 2 Bz H F F OH XXIII-44-4 'Bu H H CH 2CH(CH3)2 Bz H F F OH XXIII-44-5 'Bu H H CH 2Ph Bz H F F OH XXIII-44-6 'Bu H H CH 2-indol-3-yl Bz H F F OH XXIII-44-7 'Bu H H CH 2CH2SCH 3 Bz H F F OH XXIII-44-8 'Bu * H * Bz H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-45. N Rl R2 R3 a R3b R4 R5 R 6 X Y XXIII-45-1 Ph H H H Bz H F F OH XXIII-45-2 Ph H H CH 3 Bz H F F OH XXIII-45-3 Ph H H CH(CH3) 2 Bz H F F OH XXIII-45-4 Ph H H CH 2CH(CH3)2 Bz H F F OH XXIII-45-5 Ph H H CH 2Ph Bz H F F OH XXIII-45-6 Ph H H CH 2-indol-3-yl Bz H F F OH XXIII-45-7 Ph H H CH 2CH2SCH 3 Bz H F F OH XXIII-45-8 Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Ar,

Table XXIII-46. No R R2 RaR 3 b 4 R' R6 X Y XXIII-46-1 p-Me-Ph H H H Bz H F F OH XXIII-46-2 p-Me-Ph H H CH 3 Bz H F F OH XXIII-46-3 p-Me-Ph H H CH(CH 3)2 Bz H F F OH XXIII-46-4 p-Me-Ph H H CH 2CH(CH3) 2 Bz H F F OH XXIII-46-5 p-Me-Ph H H CH 2Ph Bz H F F OH XXIII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F F OH XXIII-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H F F OH XXIII-46-8 p-Me-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-47. N9 R1 R2 R3 a R R4 R R6 X Y XXIII-47-1 p-F-Ph H H H Bz H F F OH XXIII-47-2 p-F-Ph H H CH 3 Bz H F F OH XXIII-47-3 p-F-Ph H H CH(CH3) 2 Bz H F F OH XXIII-47-4 p-F-Ph H H CH 2CH(CH3)2 Bz H F F OH XXIII-47-5 p-F-Ph H H CH 2Ph Bz H F F OH XXIII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F F OH XXIII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz H F F OH XXIII-47-8 p-F-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-48. 5 No R R2 R 3 a R3b R4 R R6 X Y XXIII-48-1 p-Cl-Ph H H H Bz H F F OH XXIII-48-2 p-Cl-Ph H H CH3 Bz H F F OH XXIII-48-3 p-Cl-Ph H H CH(CH 3)2 Bz H F F OH XXIII-48-4 p-Cl-Ph H H CH2CH(CH 3) 2 Bz H F F OH XXIII-48-5 p-Cl-Ph H H CH 2Ph Bz H F F OH XXIII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F F OH XXIII-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz H F F OH XXIII-48-8 p-Cl-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A1A2-

Table XXIII-49. 5 No R RR 3 a R3b R4 R R' X Y XXIII-49-1 p-Br-Ph H H H Bz H F F OH XXIII-49-2 p-Br-Ph H H CH3 Bz H F F OH XXIII-49-3 p-Br-Ph H H CH(CH3)2 Bz H F F OH XXIII-49-4 p-Br-Ph H H CH2CH(CH 3) 2 Bz H F F OH XXIII-49-5 p-Br-Ph H H CH 2Ph Bz H F F OH XXIII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F F OH XXIII-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F F OH XXIII-49-8 p-Br-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIII-50. N9 Rl R2 R3 a R3 b R4 R5 R 6 X Y XXIII-50-1 p-I-Ph H H H Bz H F F OH XXIII-50-2 p-I-Ph H H CH 3 Bz H F F OH XXIII-50-3 p-I-Ph H H CH(CH3) 2 Bz H F F OH XXIII-50-4 p-I-Ph H H CH 2CH(CH3)2 Bz H F F OH XXIII-50-5 p-I-Ph H H CH 2Ph Bz H F F OH XXIII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F F OH XXIII-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H F F OH XXIII-50-8 p-I-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

N

R3b R2 O N R3a N P 0 0 N N- -0 I N 5 6 NH 2 C0 2 R4 OR 1 R R

Y X XXIV

Table XXIV-1. 6 No R R22 R3 a R3b R4 R R X Y

XXIV-1-1 CH3 H H H CH 3 H H F OH XXIV-1-2 CH3 H H CH 3 CH3 H H F OH XXIV-1-3 CH3 H H CH(CH3) 2 CH 3 H H F OH

A A-

R 5 No R2 R3 a R3 b R4 R R' X Y XXIV-1-4 CH3 H H CH 2CH(CH3)2 CH 3 H H F OH XXIV-1-5 CH3 H H CH 2Ph CH 3 H H F OH XXIV-1-6 CH3 H H CH 2-indol-3-yl CH 3 H H F OH XXIV-1-7 CH3 H H CH 2CH 2SCH 3 CH 3 H H F OH XXIV-1-8 CH3 * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-2. 5 No Rl R 2 R3 a R 3b R4 R R6 X Y XXIV-2-1 Et H H H CH 3 H H F OH XXIV-2-2 Et H H CH 3 CH 3 H H F OH XXIV-2-3 Et H H CH(CH3) 2 CH 3 H H F OH XXIV-2-4 Et H H CH 2CH(CH3) 2 CH 3 H H F OH XXIV-2-5 Et H H CH 2Ph CH 3 H H F OH XXIV-2-6 Et H H CH 2-indol-3-yl CH 3 H H F OH XXIV-2-7 Et H H CH 2CH 2SCH3 CH 3 H H F OH XXIV-2-8 Et * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-3. No R R2 R3 a R3 b R4 R' R6 X Y XXIV-3-1 Pr H H H CH 3 H H F OH XXIV-3-2 Pr H H CH 3 CH 3 H H F OH XXIV-3-3 Pr H H CH(CH3) 2 CH 3 H H F OH XXIV-3-4 Pr H H CH 2CH(CH3)2 CH 3 H H F OH XXIV-3-5 'Pr H H CH 2Ph CH 3 H H F OH XXIV-3-6 'Pr H H CH 2-indol-3-yl CH 3 H H F OH XXIV-3-7 'Pr H H CH 2CH2SCH 3 CH 3 H H F OH XXIV-3-8 'Pr * H * CH 3 H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-4. R No R2 R 3a R3b R4 R 5 R6 X Y

XXIV-4-1 'Bu H H H CH 3 H H F OH XXIV-4-2 'Bu H H CH 3 CH 3 H H F OH XXIV-4-3 'Bu H H CH(CH3) 2 CH 3 H H F OH XXIV-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H H F OH XXIV-4-5 'Bu H H CH 2Ph CH 3 H H F OH XXIV-4-6 'Bu H H CH 2-indol-3-yl CH 3 H H F OH

No R R2 R 3a R3 b R4 R' R6 X Y XXIV-4-7 'Bu H H CH 2CH 2SCH 3 CH 3 H H F OH XXIV-4-8 'Bu * H * CH 3 H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-5. R 6 No R2 R3a R3 b R4 R R X Y

XXIV-5-1 Ph H H H CH 3 H H F OH XXIV-5-2 Ph H H CH3 CH 3 H H F OH XXIV-5-3 Ph H H CH(CH 3) 2 CH 3 H H F OH XXIV-5-4 Ph H H CH2CH(CH3) 2 CH 3 H H F OH XXIV-5-5 Ph H H CH 2Ph CH 3 H H F OH XXIV-5-6 Ph H H CH 2-indol-3-yl CH 3 H H F OH XXIV-5-7 Ph H H CH2CH2 SCH3 CH 3 H H F OH XXIV-5-8 Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-6. N9 Rl R2 R3a R3 b R4 R R6 X Y XXIV-6-1 p-Me-Ph H H H CH 3 H H F OH XXIV-6-2 p-Me-Ph H H CH 3 CH 3 H H F OH XXIV-6-3 p-Me-Ph H H CH(CH3)2 CH 3 H H F OH XXIV-6-4 p-Me-Ph H H CH 2CH(CH3) 2 CH 3 H H F OH XXIV-6-5 p-Me-Ph H H CH 2Ph CH 3 H H F OH XXIV-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXIV-6-7 p-Me-Ph H H CH 2CH2 SCH3 CH 3 H H F OH XXIV-6-8 p-Me-Ph * H * CH 3 H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-7. No R R2 R 3 a R3 b R4 R R6 X Y XXIV-7-1 p-F-Ph H H H CH 3 H H F OH XXIV-7-2 p-F-Ph H H CH 3 CH 3 H H F OH XXIV-7-3 p-F-Ph H H CH(CH3)2 CH 3 H H F OH XXIV-7-4 p-F-Ph H H CH 2CH(CH 3) 2 CH 3 H H F OH XXIV-7-6 p-F-Ph H H CH 2Ph CH 3 H H F OH XXIV-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXIV-7-8 p-F-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXIV-7-20 p-F-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-8. No R R2 R3 a R3b R4 R R X Y XXIV-8-1 p-Cl-Ph H H H CH 3 H H F OH XXIV-8-2 p-Cl-Ph H H CH 3 CH 3 H H F OH XXIV-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H H F OH XXIV-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H H F OH XXIV-8-5 p-Cl-Ph H H CH 2Ph CH 3 H H F OH XXIV-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXIV-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H H F OH XXIV-8-8 p-Cl-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-9. 5 N9 R1 R2 R 3a R3 b R4 R R6 X Y XXIV-9-1 p-Br-Ph H H H CH3 H H F OH XXIV-9-2 p-Br-Ph H H CH3 CH3 H H F OH XXIV-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H H F OH XXIV-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH3 H H F OH XXIV-9-6 p-Br-Ph H H CH 2Ph CH3 H H F OH XXIV-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H H F OH XXIV-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 H H F OH XXIV-9-20 p-Br-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-10. No R R2 R 3 a R3b R4 R 5 R6 X Y

XXIV-10-1 p-I-Ph H H H CH 3 H H F OH XXIV-10-2 p-I-Ph H H CH3 CH 3 H H F OH XXIV-10-3 p-I-Ph H H CH(CH 3)2 CH 3 H H F OH XXIV-10-4 p-I-Ph H H CH2CH(CH 3)2 CH 3 H H F OH XXIV-10-5 p-I-Ph H H CH 2Ph CH 3 H H F OH XXIV-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXIV-10-7 p-I-Ph H H CH2CH 2SCH 3 CH 3 H H F OH XXIV-10-8 p-I-Ph * H * CH 3 H H F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-11. No R1 R2 R 3a R3 b R4 R R X Y

XXIV-11-1 CH 3 H H H Et H H F OH XXIV-11-2 CH 3 H H CH3 Et H H F OH XXIV-11-3 CH3 H H CH(CH3) 2 Et H H F OH

R No R2 R 3a R3 b R4 R R X Y

XXIV-11-4 CH 3 H H CH2CH(CH3) 2 Et H H F OH XXIV-11-5 CH 3 H H CH 2Ph Et H H F OH XXIV-11-6 CH3 H H CH 2-indol-3-yl Et H H F OH XXIV-11-7 CH3 H H CH2CH 2SCH 3 Et H H F OH XXIV-11-8 CH 3 * H * Et H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-12. No Rl R2 R 3a R3b R4 R R X Y

XXIV-12-1 Et H H H Et H H F OH XXIV-12-2 Et H H CH 3 Et H H F OH XXIV-12-3 Et H H CH(CH3) 2 Et H H F OH XXIV-12-4 Et H H CH 2CH(CH3) 2 Et H H F OH XXIV-12-5 Et H H CH 2Ph Et H H F OH XXIV-12-6 Et H H CH 2-indol-3-yl Et H H F OH XXIV-12-7 Et H H CH 2CH 2SCH 3 Et H H F OH XXIV-12-8 Et * H * Et H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-13. N9 R R2 R 3a Rb R 4 R' R6 X Y XXIV-13-1 Pr H H H Et H H F OH XXIV-13-2 Pr H H CH 3 Et H H F OH XXIV-13-3 Pr H H CH(CH3) 2 Et H H F OH XXIV-13-4 Pr H H CH 2CH(CH3)2 Et H H F OH XXIV-13-5 'Pr H H CH 2Ph Et H H F OH XXIV-13-6 'Pr H H CH 2-indol-3-yl Et H H F OH XXIV-13-7 'Pr H H CH 2CH 2SCH 3 Et H H F OH XXIV-13-8 'Pr * H * Et H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-14. No R R2 R3 a R3b R4 R5 R6 X Y

XXIV-14-1 'Bu H H H Et H H F OH XXIV-14-2 'Bu H H CH 3 Et H H F OH XXIV-14-3 'Bu H H CH(CH3) 2 Et H H F OH XXIV-14-4 'Bu H H CH 2CH(CH3)2 Et H H F OH XXIV-14-5 'Bu H H CH 2Ph Et H H F OH XXIV-14-6 'Bu H H CH 2-indol-3-yl Et H H F OH

A Q-

R R' R' No R2 R3 a R3 b R4 X Y XXIV-14-7 'Bu H H CH 2CH 2SCH 3 Et H H F OH XXIV-14-8 'Bu * H * Et H H F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXIV-15. R No R2 R 3a R3 b R4 R5 R6 X Y XXIV-15-1 Ph H H H Et H H F OH XXIV-15-2 Ph H H CH3 Et H H F OH XXIV-15-3 Ph H H CH(CH 3)2 Et H H F OH XXIV-15-4 Ph H H CH2CH(CH 3)2 Et H H F OH XXIV-15-5 Ph H H CH 2Ph Et H H F OH XXIV-15-6 Ph H H CH 2-indol-3-yl Et H H F OH XXIV-15-7 Ph H H CH2CH 2SCH 3 Et H H F OH XXIV-15-8 Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-16. No R R2 R 3 a R3 b R4 R5 R6 X Y XXIV-16-1 p-Me-Ph H H H Et H H F OH XXIV-16-2 p-Me-Ph H H CH 3 Et H H F OH XXIV-16-3 p-Me-Ph H H CH(CH 3)2 Et H H F OH XXIV-16-4 p-Me-Ph H H CH 2CH(CH 3)2 Et H H F OH XXIV-16-5 p-Me-Ph H H CH 2Ph Et H H F OH XXIV-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H H F OH XXIV-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H H F OH XXIV-16-8 p-Me-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-17. 5 6 N9 Rl R2 R3 a R3 b R4 R R X Y

XXIV-17-1 p-F-Ph H H H Et H H F OH XXIV-17-2 p-F-Ph H H CH 3 Et H H F OH XXIV-17-3 p-F-Ph H H CH(CH 3) 2 Et H H F OH XXIV-17-4 p-F-Ph H H CH 2CH(CH 3) 2 Et H H F OH XXIV-17-5 p-F-Ph H H CH 2Ph Et H H F OH XXIV-17-6 p-F-Ph H H CH 2-indol-3-yl Et H H F OH XXIV-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H H F OH XXIV-17-8 p-F-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ rO _

Table XXIV-18. No R R2 R3 a R 3b R4 R R X Y XXIV-18-1 p-Cl-Ph H H H Et H H F OH XXIV-18-2 p-Cl-Ph H H CH3 Et H H F OH XXIV-18-3 p-Cl-Ph H H CH(CH3) 2 Et H H F OH XXIV-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H H F OH XXIV-18-5 p-Cl-Ph H H CH2Ph Et H H F OH XXIV-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H H F OH XXIV-18-7 p-Cl-Ph H H CH2CH2SCH 3 Et H H F OH XXIV-18-8 p-Cl-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-19. N9 R1 R2 R 3a R3 b R4 R R X Y

XXIV-19-1 p-Br-Ph H H H Et H H F OH XXIV-19-2 p-Br-Ph H H CH3 Et H H F OH XXIV-19-3 p-Br-Ph H H CH(CH3) 2 Et H H F OH XXIV-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H H F OH XXIV-19-5 p-Br-Ph H H CH 2Ph Et H H F OH XXIV-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H H F OH XXIV-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H H F OH XXIV-19-8 p-Br-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-20. No R R2 R 3 a R3b R4 R 5 R6 X Y

XXIV-20-1 p-I-Ph H H H Et H H F OH XXIV-20-2 p-I-Ph H H CH3 Et H H F OH XXIV-20-3 p-I-Ph H H CH(CH3)2 Et H H F OH XXIV-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H H F OH XXIV-20-5 p-I-Ph H H CH 2Ph Et H H F OH XXIV-20-6 p-I-Ph H H CH 2-indol-3-yl Et H H F OH XXIV-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H H F OH XXIV-20-8 p-I-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-21. No R1 R2 R 3a R3 b R4 R 5 R6 X Y XXIV-21-1 CH 3 H H H 'Pr H H F OH XXIV-21-2 CH 3 H H CH3 'Pr H H F OH XXIV-21-3 CH 3 H H CH(CH3) 2 'Pr H H F OH

A1'Mfl

No R R2 R 3a R3 b R4 R' R6 X Y XXIV-21-4 CH 3 H H CH2 CH(CH 3 )2 'Pr H H F OH XXIV-21-5 CH 3 H H CH 2 Ph 'Pr H H F OH XXIV-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H H F OH XXIV-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H H F OH XXIV-21-8 CH 3 * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-22. No Rl R2 R 3a R3b R4 R' R6 X Y XXIV-22-1 Et H H H 'Pr H H F OH XXIV-22-2 Et H H CH 3 'Pr H H F OH XXIV-22-3 Et H H CH(CH 3)2 'Pr H H F OH XXIV-22-4 Et H H CH 2CH(CH 3)2 'Pr H H F OH XXIV-22-5 Et H H CH 2Ph 'Pr H H F OH XXIV-22-6 Et H H CH 2-indol-3-yl 'Pr H H F OH XXIV-22-7 Et H H CH 2CH 2SCH 3 'Pr H H F OH XXIV-22-8 Et * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-23. No R R2 R 3a R3 b R4 R R 6 X Y

XXIV-23-1 Pr H H H 'Pr H H F OH XXIV-23-2 Pr H H CH 3 'Pr H H F OH XXIV-23-3 Pr H H CH(CH 3)2 'Pr H H F OH XXIV-23-4 Pr H H CH 2CH(CH 3)2 'Pr H H F OH XXIV-23-5 'Pr H H CH 2 Ph 'Pr H H F OH XXIV-23-6 'Pr H H CH 2-indol-3-yl 'Pr H H F OH XXIV-23-7 'Pr H H CH 2CH 2SCH 3 'Pr H H F OH XXIV-23-8 'Pr * H * 'Pr H H F OH

*R 2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-24. No R R2 R3 a R3 R4 R5 R6 X Y XXIV-24-1 'Bu H H H 'Pr H H F OH XXIV-24-2 'Bu H H CH 3 'Pr H H F OH XXIV-24-3 'Bu H H CH(CH 3) 2 'Pr H H F OH XXIV-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H H F OH XXIV-24-5 'Bu H H CH 2Ph 'Pr H H F OH XXIV-24-6 'Bu H H CH 2-indol-3-yl 'Pr H H F OH

A'71

R No R2 R3 a R3 b R4 R' R' X Y XXIV-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H H F OH XXIV-24-8 'Bu * H * 'Pr H H F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXIV-25. R No R2 R 3a R3 b R4 R 5 R' X Y XXIV-25-1 Ph H H H 'Pr H H F OH XXIV-25-2 Ph H H CH3 'Pr H H F OH XXIV-25-3 Ph H H CH(CH 3)2 'Pr H H F OH XXIV-25-4 Ph H H CH2CH(CH 3)2 'Pr H H F OH XXIV-25-5 Ph H H CH 2Ph 'Pr H H F OH XXIV-25-6 Ph H H CH 2-indol-3-yl 'Pr H H F OH XXIV-25-7 Ph H H CH2CH 2SCH 3 'Pr H H F OH XXIV-25-8 Ph * H * 'Pr H H F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXIV-26. No R R2 R 3 a R3 b R4 R5 R6 X Y XXIV-26-1 p-Me-Ph H H H 'Pr H H F OH XXIV-26-2 p-Me-Ph H H CH 3 'Pr H H F OH XXIV-26-3 p-Me-Ph H H CH(CH 3)2 'Pr H H F OH XXIV-26-4 p-Me-Ph H H CH 2CH(CH 3)2 'Pr H H F OH XXIV-26-5 p-Me-Ph H H CH 2Ph 'Pr H H F OH XXIV-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXIV-26-7 p-Me-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXIV-26-8 p-Me-Ph * H * 'Pr H H F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-27. 5 N9 Rl R2 R3 a R3 b R4 R R6 X Y XXIV-27-1 p-F-Ph H H H 'Pr H H F OH XXIV-27-2 p-F-Ph H H CH 3 'Pr H H F OH XXIV-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H H F OH XXIV-27-4 p-F-Ph H H CH 2CH(CH 3) 2 'Pr H H F OH XXIV-27-5 p-F-Ph H H CH 2Ph 'Pr H H F OH XXIV-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXIV-27-7 p-F-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXIV-27-8 p-F-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AAT)-

Table XXIV-28. No R R 2 R3 a R 3b R 4 R R6 X Y XXIV-28-1 p-Cl-Ph H H H 'Pr H H F OH XXIV-28-2 p-Cl-Ph H H CH3 'Pr H H F OH XXIV-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H H F OH XXIV-28-4 p-Cl-Ph H H CH2CH(CH3)2 'Pr H H F OH XXIV-28-5 p-Cl-Ph H H CH2Ph 'Pr H H F OH XXIV-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H H F OH XXIV-28-7 p-Cl-Ph H H CH2CH2SCH 3 'Pr H H F OH XXIV-28-8 p-Cl-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A1721

Table XXIV-29. No R R2 R 3 a R3b R4 R' R6 X Y XXIV-29-1 p-Br-Ph H H H 'Pr H H F OH XXIV-29-2 p-Br-Ph H H CH3 'Pr H H F OH XXIV-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H H F OH XXIV-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H H F OH XXIV-29-5 p-Br-Ph H H CH 2Ph 'Pr H H F OH XXIV-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXIV-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H H F OH XXIV-29-8 p-Br-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-30. No R R2 R3a R3 b R4 R' R6 X Y XXIV-30-1 p-I-Ph H H H 'Pr H H F OH XXIV-30-2 p-I-Ph H H CH3 'Pr H H F OH XXIV-30-3 p-I-Ph H H CH(CH 3)2 'Pr H H F OH XXIV-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H H F OH XXIV-30-5 p-I-Ph H H CH 2Ph 'Pr H H F OH XXIV-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXIV-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H H F OH XXIV-30-8 p-I-Ph * H * 'Pr H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-31. No R1 R2 R 3a R3b R4 R R 6 X Y

XXIV-31-1 CH 3 H H H "Bu H H F OH XXIV-31-2 CH 3 H H CH3 "Bu H H F OH XXIV-31-3 CH3 H H CH(CH3) 2 "Bu H H F OH XXIV-31-4 CH3 H H CH2CH(CH3) 2 "Bu H H F OH XXIV-31-5 CH3 H H CH 2Ph "Bu H H F OH XXIV-31-6 CH3 H H CH 2-indol-3-yl "Bu H H F OH XXIV-31-7 CH3 H H CH2CH 2SCH 3 "Bu H H F OH XXIV-31-8 CH3 * H * "Bu H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A17A1

Table XXIV-32. No Rl R2 R 3a R3b R4 R' R6 X Y XXIV-32-1 Et H H H "Bu H H F OH XXIV-32-2 Et H H CH 3 "Bu H H F OH XXIV-32-3 Et H H CH(CH3) 2 "Bu H H F OH XXIV-32-4 Et H H CH 2CH(CH3) 2 "Bu H H F OH XXIV-32-5 Et H H CH 2Ph "Bu H H F OH XXIV-32-6 Et H H CH 2-indol-3-yl "Bu H H F OH XXIV-32-7 Et H H CH 2CH 2SCH 3 "Bu H H F OH XXIV-32-8 Et * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-33. No R1 R2 R 3a Rb R4 R R6 X Y XXIV-33-1 'Pr H H H "Bu H H F OH XXIV-33-2 'Pr H H CH 3 "Bu H H F OH XXIV-33-3 'Pr H H CH(CH 3)2 "Bu H H F OH XXIV-33-4 'Pr H H CH 2CH(CH3)2 "Bu H H F OH XXIV-33-5 'Pr H H CH 2Ph "Bu H H F OH XXIV-33-6 'Pr H H CH 2-indol-3-yl "Bu H H F OH

XXIV-33-7 'Pr H H CH 2 CH 2 SCH 3 "Bu H H F OH XXIV-33-8 'Pr * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-34. No R1 R2 R3a R 3b R4 R R X Y XXIV-34-1 'Bu H H H "Bu H H F OH XXIV-34-2 'Bu H H CH 3 "Bu H H F OH XXIV-34-3 'Bu H H CH(CH3) 2 "Bu H H F OH XXIV-34-4 'Bu H H CH 2CH(CH3)2 "Bu H H F OH XXIV-34-5 'Bu H H CH 2Ph "Bu H H F OH XXIV-34-6 'Bu H H CH 2-indol-3-yl "Bu H H F OH

XXIV-34-7 'Bu H H CH 2CH 2 SCH 3 "Bu H H F OH XXIV-34-8 'Bu * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-35. No R1 R2 R 3a R3b R4 R 5 R6 X Y

XXIV-35-1 Ph H H H "Bu H H F OH XXIV-35-2 Ph H H CH3 "Bu H H F OH XXIV-35-3 Ph H H CH(CH3)2 "Bu H H F OH XXIV-35-4 Ph H H CH2CH(CH3) 2 "Bu H H F OH XXIV-35-5 Ph H H CH 2Ph "Bu H H F OH XXIV-35-6 Ph H H CH 2-indol-3-yl "Bu H H F OH XXIV-35-7 Ph H H CH2CH 2SCH 3 "Bu H H F OH XXIV-35-8 Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-36. N9 R1 R2 R 3a R3 b R4 R 5 R6 X Y

XXIV-36-1 p-Me-Ph H H H "Bu H H F OH XXIV-36-2 p-Me-Ph H H CH 3 "Bu H H F OH XXIV-36-3 p-Me-Ph H H CH(CH3)2 "Bu H H F OH XXIV-36-4 p-Me-Ph H H CH 2CH(CH3) 2 "Bu H H F OH XXIV-36-5 p-Me-Ph H H CH 2Ph "Bu H H F OH XXIV-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H H F OH XXIV-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXIV-36-8 p-Me-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXIV-37. No R1 R2 R3 a R3b R4 R5 R6 X Y XXIV-37-1 p-F-Ph H H H "Bu H H F OH XXIV-37-2 p-F-Ph H H CH 3 "Bu H H F OH XXIV-37-3 p-F-Ph H H CH(CH3)2 "Bu H H F OH XXIV-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H H F OH XXIV-37-5 p-F-Ph H H CH 2Ph "Bu H H F OH XXIV-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H H F OH XXIV-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXIV-37-8 p-F-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXIV-38. No R R2 3 a R 3b R4 RR X Y XXIV-38-1 p-Cl-Ph H H H "Bu H H F OH XXIV-38-2 p-Cl-Ph H H CH3 "Bu H H F OH XXIV-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H H F OH XXIV-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H H F OH XXIV-38-5 p-Cl-Ph H H CH2Ph "Bu H H F OH XXIV-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H H F OH XXIV-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H H F OH XXIV-38-8 p-Cl-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-39. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXIV-39-1 p-Br-Ph H H H "Bu H H F OH XXIV-39-2 p-Br-Ph H H CH 3 "Bu H H F OH XXIV-39-3 p-Br-Ph H H CH(CH 3 )2 "Bu H H F OH XXIV-39-4 p-Br-Ph H H CH 2 CH(CH 3)2 "Bu H H F OH XXIV-39-5 p-Br-Ph H H CH 2 Ph "Bu H H F OH XXIV-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H H F OH XXIV-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH XXIV-39-8 p-Br-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-40. No R1 R2 R 3a R3b R4 R 5 R6 X Y XXIV-40-1 p-I-Ph H H H "Bu H H F OH XXIV-40-2 p-I-Ph H H CH 3 "Bu H H F OH XXIV-40-3 p-I-Ph H H CH(CH3)2 "Bu H H F OH XXIV-40-4 p-I-Ph H H CH 2 CH(CH3) 2 "Bu H H F OH XXIV-40-5 p-I-Ph H H CH 2 Ph "Bu H H F OH XXIV-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H H F OH XXIV-40-7 p-I-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH XXIV-40-8 p-I-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

A 177-

Table XXIV-41. No R1 R2 R 3a R3b R4 R' R' X Y XXIV-41-1 CH3 H H H Bz H H F OH XXIV-41-2 CH 3 H H CH3 Bz H H F OH XXIV-41-3 CH 3 H H CH(CH3) 2 Bz H H F OH XXIV-41-4 CH 3 H H CH2CH(CH3) 2 Bz H H F OH XXIV-41-5 CH 3 H H CH 2Ph Bz H H F OH XXIV-41-6 CH 3 H H CH 2-indol-3-yl Bz H H F OH XXIV-41-7 CH 3 H H CH2CH 2SCH 3 Bz H H F OH XXIV-41-8 CH 3 * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-42. No R1 R2 R3a R3b R4 R' R6 X Y XXIV-42-1 Et H H H Bz H H F OH XXIV-42-2 Et H H CH 3 Bz H H F OH XXIV-42-3 Et H H CH(CH3) 2 Bz H H F OH XXIV-42-4 Et H H CH 2CH(CH3) 2 Bz H H F OH XXIV-42-5 Et H H CH 2Ph Bz H H F OH XXIV-42-6 Et H H CH 2-indol-3-yl Bz H H F OH XXIV-42-7 Et H H CH 2CH 2SCH 3 Bz H H F OH XXIV-42-8 Et * H * Bz H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-43. N R1 R2 R 3a R3 b 4 R 5 R 6 X Y

XXIV-43-1 'Pr H H H Bz H H F OH XXIV-43-2 Pr H H CH 3 Bz H H F OH XXIV-43-3 Pr H H CH(CH3) 2 Bz H H F OH XXIV-43-4 Pr H H CH 2CH(CH 3)2 Bz H H F OH XXIV-43-5 Pr H H CH 2Ph Bz H H F OH XXIV-43-6 'Pr H H CH 2-indol-3-yl Bz H H F OH XXIV-43-7 'Pr H H CH 2CH2SCH 3 Bz H H F dAI XXIV-43-8 'Pr * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-44. 1 RI R2 R3a R3bR4 R5 R6 X Y XXIV-44-1 'Bu H H H Bz H H F OH

A17Q-

No R1 R2 R3 a R3 b R4 R' R6 X Y XXIV-44-2 'Bu H H CH 3 Bz H H F OH XXIV-44-3 'Bu H H CH(CH3) 2 Bz H H F OH XXIV-44-4 'Bu H H CH 2CH(CH3)2 Bz H H F OH XXIV-44-5 'Bu H H CH 2Ph Bz H H F OH XXIV-44-6 'Bu H H CH 2-indol-3-yl Bz H H F OH XXIV-44-7 'Bu H H CH 2CH 2SCH 3 Bz H H F OH XXIV-44-8 'Bu * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-45. No R1 R2 R 3a R3b R4 R 5 R6 X Y XXIV-45-1 Ph H H H Bz H H F OH XXIV-45-2 Ph H H CH3 Bz H H F OH XXIV-45-3 Ph H H CH(CH3)2 Bz H H F OH XXIV-45-4 Ph H H CH2CH(CH3) 2 Bz H H F OH XXIV-45-5 Ph H H CH 2Ph Bz H H F OH XXIV-45-6 Ph H H CH 2-indol-3-yl Bz H H F OH XXIV-45-7 Ph H H CH2CH 2SCH 3 Bz H H F OH XXIV-45-8 Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-46. No R R2 R 3 a R3 b R4 R 5 R6 X Y XXIV-46-1 p-Me-Ph H H H Bz H H F OH XXIV-46-2 p-Me-Ph H H CH 3 Bz H H F OH XXIV-46-3 p-Me-Ph H H CH(CH 3)2 Bz H H F OH XXIV-46-4 p-Me-Ph H H CH 2CH(CH 3)2 Bz H H F OH XXIV-46-5 p-Me-Ph H H CH 2Ph Bz H H F OH XXIV-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H H F OH XXIV-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXIV-46-8 p-Me-Ph * H * Bz H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

A17o-

Table XXIV-47. No R RR 3 a R3b R4 R 5 R' X Y XXIV-47-1 p-F-Ph H H H Bz H H F OH XXIV-47-2 p-F-Ph H H CH3 Bz H H F OH XXIV-47-3 p-F-Ph H H CH(CH 3) 2 Bz H H F OH XXIV-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H H F OH XXIV-47-5 p-F-Ph H H CH 2Ph Bz H H F OH XXIV-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H H F OH XXIV-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H H F OH XXIV-47-8 p-F-Ph * H * Bz H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIV-48. N9 R1 R2 R3 a R3 b R4 R R6 X Y XXIV-48-1 p-Cl-Ph H H H Bz H H F OH XXIV-48-2 p-Cl-Ph H H CH3 Bz H H F OH XXIV-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H H F OH XXIV-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H H F OH XXIV-48-5 p-Cl-Ph H H CH2Ph Bz H H F OH XXIV-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H H F OH XXIV-48-7 p-Cl-Ph H H CH2CH2SCH 3 Bz H H F OH XXIV-48-8 p-Cl-Ph * H * Bz H H F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXIV-49. 5 No R R2 R 3 a R3b R4 R R6 X Y XXIV-49-1 p-Br-Ph H H H Bz H H F OH XXIV-49-2 p-Br-Ph H H CH3 Bz H H F OH XXIV-49-3 p-Br-Ph H H CH(CH3) 2 Bz H H F OH XXIV-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H H F OH XXIV-49-5 p-Br-Ph H H CH 2Ph Bz H H F OH XXIV-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H H F OH XXIV-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H H F OH XXIV-49-8 p-Br-Ph * H * Bz H H F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

AQfl

Table XXIV-50. No R RR 3 a R3b R4 R 5 R6 X Y XXIV-50-1 p-I-Ph H H H Bz H H F OH XXIV-50-2 p-I-Ph H H CH3 Bz H H F OH XXIV-50-3 p-I-Ph H H CH(CH 3)2 Bz H H F OH XXIV-50-4 p-I-Ph H H CH2CH(CH 3)2 Bz H H F OH XXIV-50-5 p-I-Ph H H CH 2Ph Bz H H F OH XXIV-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H H F OH XXIV-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H H F OH XXIV-50-8 p-I-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R3b R2 0 N N P 0 0 N R3a N- ---- 0

4 Rs R6 NH 2 C0 2 R OR'

Y X XXV

Table XXV-1. No R R2 R3 a R3 R4 R5 R6 X Y

XXV-1-1 CH 3 H H H CH 3 H CH3 F OH XXV-1-2 CH 3 H H CH 3 CH 3 H CH 3 F OH XXV-1-3 CH 3 H H CH(CH3) 2 CH 3 H CH 3 F OH XXV-1-4 CH 3 H H CH 2CH(CH 3) 2 CH 3 H CH 3 F OH XXV-1-5 CH 3 H H CH 2Ph CH 3 H CH 3 F OH XXV-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H CH3 F OH XXV-1-7 CH 3 H H CH 2CH2SCH 3 CH 3 H CH3 F OH XXV-1-8 CH 3 * H * CH 3 H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AQ1 _

Table XXV-2. RI R2 RaR 3 b R4 R R X Y No XXV-2-1 Et H H H CH 3 H CH3 F OH XXV-2-2 Et H H CH3 CH 3 H CH3 F OH XXV-2-3 Et H H CH(CH3) 2 CH 3 H CH3 F OH XXV-2-4 Et H H CH2CH(CH3)2 CH 3 H CH3 F OH XXV-2-5 Et H H CH2Ph CH 3 H CH3 F OH XXV-2-6 Et H H CH2-indol-3-yl CH 3 H CH3 F OH XXV-2-7 Et H H CH2CH2SCH 3 CH 3 H CH3 F OH XXV-2-8 Et * H * CH 3 H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-3. No R1 R2 R3 a R3 b R4 R' R6 X Y XXV-3-1 'Pr H H H CH3 H CH 3 F OH XXV-3-2 'Pr H H CH3 CH3 H CH 3 F OH XXV-3-3 'Pr H H CH(CH3)2 CH3 H CH 3 F OH XXV-3-4 'Pr H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXV-3-5 'Pr H H CH 2Ph CH3 H CH 3 F OH XXV-3-6 'Pr H H CH 2-indol-3-yl CH3 H CH 3 F OH XXV-3-7 'Pr H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXV-3-8 'Pr * H * CH3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-4. No R1 R2 R3 a R3b R4 R 5 R6 X Y XXV-4-1 'Bu H H H CH3 H CH3 F OH XXV-4-2 'Bu H H CH3 CH3 H CH3 F OH XXV-4-3 'Bu H H CH(CH3)2 CH3 H CH3 F OH XXV-4-4 'Bu H H CH2CH(CH3) 2 CH3 H CH3 F OH XXV-4-5 'Bu H H CH 2Ph CH3 H CH3 F OH XXV-4-6 'Bu H H CH 2-indol-3-yl CH3 H CH3 F OH XXV-4-7 'Bu H H CH2CH 2SCH 3 CH3 H CH3 F OH XXV-4-8 'Bu * H * CH3 H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A Q)-

Table XXV-5. R1 R2 R3 a R3b R4 R5 R' X Y No

XXV-5-1 Ph H H H CH3 H CH 3 F OH XXV-5-2 Ph H H CH3 CH 3 H CH 3 F OH XXV-5-3 Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXV-5-4 Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXV-5-5 Ph H H CH2Ph CH3 H CH 3 F OH XXV-5-6 Ph H H CH2-indol-3-yl CH 3 H CH 3 F OH XXV-5-7 Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXV-5-8 Ph * H * CH3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-6. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y

XXV-6-1 p-Me-Ph H H H CH3 H CH 3 F OH XXV-6-2 p-Me-Ph H H CH3 CH 3 H CH 3 F OH XXV-6-3 p-Me-Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXV-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXV-6-5 p-Me-Ph H H CH2Ph CH3 H CH 3 F OH XXV-6-6 p-Me-Ph H H CH2-indol-3-yl CH 3 H CH 3 F OH XXV-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXV-6-8 p-Me-Ph * H * CH3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-7. No R R2 R 3 a R 3b R4 R5 R6 X Y XXV-7-1 p-F-Ph H H H CH3 H CH 3 F OH XXV-7-2 p-F-Ph H H CH 3 CH3 H CH 3 F OH XXV-7-3 p-F-Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXV-7-4 p-F-Ph H H CH 2CH(CH3) 2 CH3 H CH 3 F OH XXV-7-6 p-F-Ph H H CH 2Ph CH3 H CH 3 F OH XXV-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXV-7-8 p-F-Ph H H CH 2CH 2SCH 3 CH3 H CH 3 F OH XXV-7-20 p-F-Ph * H * CH3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A22-

Table XXV-8. No R RR 3 a R 3b R4 R' R6 X Y XXV-8-1 p-Cl-Ph H H H CH 3 H CH 3 F OH XXV-8-2 p-Cl-Ph H H CH3 CH3 H CH 3 F OH XXV-8-3 p-Cl-Ph H H CH(CH3)2 CH3 H CH 3 F OH XXV-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXV-8-5 p-Cl-Ph H H CH 2Ph CH 3 H CH 3 F OH XXV-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXV-8-7 p-Cl-Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXV-8-8 p-Cl-Ph * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXV-9. N9 R1 R2 R3 a 3 R b R4 R R6 X Y

XXV-9-1 p-Br-Ph H H H CH 3 H CH3 F OH XXV-9-2 p-Br-Ph H H CH 3 CH 3 H CH3 F OH XXV-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H CH3 F OH XXV-9-4 p-Br-Ph H H CH 2CH(CH3)2 CH 3 H CH3 F OH XXV-9-6 p-Br-Ph H H CH 2Ph CH 3 H CH3 F OH XXV-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H CH3 F OH XXV-9-8 p-Br-Ph H H CH 2CH2SCH 3 CH 3 H CH3 F OH XXV-9-20 p-Br-Ph * H * CH 3 H CH3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXV-10. No R R2 R 3 a R3b R4 RR6 X Y

XXV-10-1 p-I-Ph H H H CH3 H CH 3 F OH XXV-10-2 p-I-Ph H H CH3 CH3 H CH 3 F OH XXV-10-3 p-I-Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXV-10-4 p-I-Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXV-10-5 p-I-Ph H H CH 2Ph CH3 H CH 3 F OH XXV-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXV-10-7 p-I-Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXV-10-8 p-I-Ph * H * CH3 H CH 3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

AIQA-

Table XXV-11. R No R1 R2 RaR 3 b R4 R X Y XXV-11-1 CH3 H H H Et H CH 3 F OH XXV-11-2 CH3 H H CH 3 Et H CH 3 F OH XXV-11-3 CH3 H H CH(CH3) 2 Et H CH 3 F OH XXV-11-4 CH3 H H CH 2CH(CH3)2 Et H CH 3 F OH XXV-11-5 CH3 H H CH 2Ph Et H CH 3 F OH XXV-11-6 CH3 H H CH 2-indol-3-yl Et H CH 3 F OH XXV-11-7 CH3 H H CH 2CH 2SCH 3 Et H CH 3 F OH XXV-11-8 CH3 * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-12. N9 R1 R 2 R3 a R3 b R 4 R R6 X y

XXV-12-1 Et H H H Et H CH 3 F OH XXV-12-2 Et H H CH 3 Et H CH 3 F OH XXV-12-3 Et H H CH(CH3) 2 Et H CH 3 F OH XXV-12-4 Et H H CH 2CH(CH 3)2 Et H CH 3 F OH XXV-12-5 Et H H CH 2Ph Et H CH 3 F OH XXV-12-6 Et H H CH 2-indol-3-yl Et H CH 3 F OH XXV-12-7 Et H H CH 2CH2SCH 3 Et H CH 3 F OH XXV-12-8 Et * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-13. N R1 R2 R 3a R3 b R4 R5 R6 X Y

XXV-13-1 'Pr H H H Et H CH 3 F OH XXV-13-2 'Pr H H CH3 Et H CH 3 F OH XXV-13-3 'Pr H H CH(CH3)2 Et H CH 3 F OH XXV-13-4 'Pr H H CH2CH(CH3) 2 Et H CH 3 F OH XXV-13-5 Pr H H CH 2Ph Et H CH 3 F OH XXV-13-6 Pr H H CH 2-indol-3-yl Et H CH 3 F OH XXV-13-7 Pr H H CH2CH 2SCH 3 Et H CH 3 F OH XXV-13-8 Pr * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-14. No R1 R2 R3 a R3b R4 R' R' X Y XXV-14-1 'Bu H H H Et H CH 3 F OH XXV-14-2 'Bu H H CH 3 Et H CH 3 F OH XXV-14-3 'Bu H H CH(CH 3) 2 Et H CH 3 F OH XXV-14-4 'Bu H H CH 2CH(CH 3) 2 Et H CH 3 F OH XXV-14-5 'Bu H H CH 2Ph Et H CH 3 F OH XXV-14-6 'Bu H H CH 2-indol-3-yl Et H CH 3 F OH XXV-14-7 'Bu H H CH 2CH2SCH 3 Et H CH 3 F OH XXV-14-8 'Bu * H * Et H CH 3 F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXV-15. N9 R1 R 2 R3a R3 b R4 R5 R6 X Y XXV-15-1 Ph H H H Et H CH3 F OH XXV-15-2 Ph H H CH 3 Et H CH3 F OH XXV-15-3 Ph H H CH(CH 3) 2 Et H CH3 F OH XXV-15-4 Ph H H CH 2CH(CH 3) 2 Et H CH3 F OH XXV-15-5 Ph H H CH 2Ph Et H CH3 F OH XXV-15-6 Ph H H CH 2-indol-3-yl Et H CH3 F OH XXV-15-7 Ph H H CH 2CH 2SCH 3 Et H CH3 F OH XXV-15-8 Ph * H * Et H CH3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXV-16. No R R2 R 3 a R3b R4 R5 R6 X Y XXV-16-1 p-Me-Ph H H H Et H CH3 F OH XXV-16-2 p-Me-Ph H H CH3 Et H CH3 F OH XXV-16-3 p-Me-Ph H H CH(CH 3) 2 Et H CH3 F OH XXV-16-4 p-Me-Ph H H CH2CH(CH 3) 2 Et H CH3 F OH XXV-16-5 p-Me-Ph H H CH 2Ph Et H CH3 F OH XXV-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH3 F OH XXV-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H CH3 F OH XXV-16-8 p-Me-Ph * H * Et H CH3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

AAQ r,

Table XXV-17. No R R2 R 3 a R 3b R4 R R6 X Y XXV-17-1 p-F-Ph H H H Et H CH 3 F OH XXV-17-2 p-F-Ph H H CH 3 Et H CH 3 F OH XXV-17-3 p-F-Ph H H CH(CH3) 2 Et H CH 3 F OH XXV-17-4 p-F-Ph H H CH 2CH(CH3) 2 Et H CH 3 F OH XXV-17-5 p-F-Ph H H CH 2Ph Et H CH 3 F OH XXV-17-6 p-F-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXV-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH XXV-17-8 p-F-Ph * H * Et H CH 3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-18. N9 R1 R2 R 3a R3 b R4 R' R6 X Y

XXV-18-1 p-Cl-Ph H H H Et H CH3 F OH XXV-18-2 p-Cl-Ph H H CH 3 Et H CH3 F OH XXV-18-3 p-Cl-Ph H H CH(CH3) 2 Et H CH3 F OH XXV-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H CH3 F OH XXV-18-5 p-Cl-Ph H H CH 2Ph Et H CH3 F OH XXV-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H CH3 F OH XXV-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et H CH3 F OH XXV-18-8 p-Cl-Ph * H * Et H CH3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXV-19. No R R2 R 3 a R3b R 5 RR X Y

XXV-19-1 p-Br-Ph H H H Et H CH 3 F OH XXV-19-2 p-Br-Ph H H CH 3 Et H CH 3 F OH XXV-19-3 p-Br-Ph H H CH(CH3) 2 Et H CH 3 F OH XXV-19-4 p-Br-Ph H H CH 2CH(CH3)2 Et H CH 3 F OH XXV-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 F OH XXV-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXV-19-7 p-Br-Ph H H CH 2CH2SCH 3 Et H CH 3 F OH XXV-19-8 p-Br-Ph * H * Et H CH 3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

A Q7-

Table XXV-20. No R R2 R 3 a R3b R4 R R6 X Y XXV-20-1 p-I-Ph H H H Et H CH3 F OH XXV-20-2 p-I-Ph H H CH3 Et H CH3 F OH XXV-20-3 p-I-Ph H H CH(CH3) 2 Et H CH3 F OH XXV-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H CH3 F OH XXV-20-5 p-I-Ph H H CH 2Ph Et H CH3 F OH XXV-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH3 F OH XXV-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H CH3 F OH XXV-20-8 p-I-Ph * H * Et H CH3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-21. X R1 R2 R3 a R3 b R4 R R6 X Y

XXV-21-1 CH3 H H H 'Pr H CH 3 F OH XXV-21-2 CH3 H H CH 3 'Pr H CH 3 F OH XXV-21-3 CH3 H H CH(CH3) 2 'Pr H CH 3 F OH XXV-21-4 CH3 H H CH 2CH(CH3) 2 'Pr H CH 3 F OH XXV-21-5 CH3 H H CH 2Ph 'Pr H CH 3 F OH XXV-21-6 CH3 H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-21-7 CH3 H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXV-21-8 CH3 * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-22. R No RI R2 R3 a R3b R4 R X Y XXV-22-1 Et H H H 'Pr H CH3 F OH XXV-22-2 Et H H CH 3 'Pr H CH3 F OH XXV-22-3 Et H H CH(CH3) 2 'Pr H CH3 F OH XXV-22-4 Et H H CH 2CH(CH3) 2 'Pr H CH3 F OH XXV-22-5 Et H H CH 2Ph 'Pr H CH3 F OH XXV-22-6 Et H H CH 2-indol-3-yl 'Pr H CH3 F OH XXV-22-7 Et H H CH 2CH2SCH 3 'Pr H CH3 F OH XXV-22-8 Et * H * 'Pr H CH3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

,1QQ-

Table XXV-23. R1 R2 R 3a R3b R4 R' R' X Y No

XXV-23-1 'Pr H H H 'Pr H CH 3 F OH XXV-23-2 'Pr H H CH3 'Pr H CH 3 F OH XXV-23-3 'Pr H H CH(CH 3) 2 'Pr H CH 3 F OH XXV-23-4 Pr H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXV-23-5 'Pr H H CH 2Ph 'Pr H CH 3 F OH XXV-23-6 'Pr H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-23-7 Pr H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXV-23-8 'Pr * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-24. N9 R1 R2 R 3a R3 b R4 R' R6 X Y

XXV-24-1 'Bu H H H 'Pr H CH3 F OH XXV-24-2 'Bu H H CH 3 'Pr H CH3 F OH XXV-24-3 'Bu H H CH(CH 3) 2 'Pr H CH3 F OH XXV-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H CH3 F OH XXV-24-5 'Bu H H CH 2Ph 'Pr H CH3 F OH XXV-24-6 'Bu H H CH 2-indol-3-yl 'Pr H CH3 F OH XXV-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H CH3 F OH XXV-24-8 'Bu * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-25. No R1 R2 R3 a R3b R4 R5 R6 X Y

XXV-25-1 Ph H H H 'Pr H CH 3 F OH XXV-25-2 Ph H H CH 3 'Pr H CH 3 F OH XXV-25-3 Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXV-25-4 Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH XXV-25-5 Ph H H CH 2Ph 'Pr H CH 3 F OH XXV-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-25-7 Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH XXV-25-8 Ph * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

AQ-o

Table XXV-26. No R R2 R 3 a R3b R4 R' R6 X Y XXV-26-1 p-Me-Ph H H H 'Pr H CH 3 F OH XXV-26-2 p-Me-Ph H H CH3 'Pr H CH 3 F OH XXV-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr H CH 3 F OH XXV-26-4 p-Me-Ph H H CH2CH(CH 3) 2 'Pr H CH 3 F OH XXV-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH 3 F OH XXV-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXV-26-8 p-Me-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXV-27. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y XXV-27-1 p-F-Ph H H H 'Pr H CH 3 F OH XXV-27-2 p-F-Ph H H CH 3 'Pr H CH 3 F OH XXV-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H CH 3 F OH XXV-27-4 p-F-Ph H H CH 2CH(CH 3)2 'Pr H CH 3 F OH XXV-27-5 p-F-Ph H H CH 2Ph 'Pr H CH 3 F OH XXV-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-27-7 p-F-Ph H H CH 2CH 2SCH 3 'Pr H CH 3 F OH XXV-27-8 p-F-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXV-28. No R R2 R 3 a R3b R4 R5 R6 X Y

XXV-28-1 p-Cl-Ph H H H 'Pr H CH 3 F OH XXV-28-2 p-Cl-Ph H H CH 3 'Pr H CH 3 F OH XXV-28-3 p-Cl-Ph H H CH(CH 3)2 'Pr H CH 3 F OH XXV-28-4 p-Cl-Ph H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH XXV-28-5 p-Cl-Ph H H CH 2Ph 'Pr H CH 3 F OH XXV-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXV-28-8 p-Cl-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ AOn _

Table XXV-29. No R R2 R3 a R3b R4 R R6 X Y XXV-29-1 p-Br-Ph H H H 'Pr H CH 3 F OH XXV-29-2 p-Br-Ph H H CH 3 'Pr H CH 3 F OH XXV-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXV-29-4 p-Br-Ph H H CH 2CH(CH3) 2 'Pr H CH 3 F OH XXV-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 F OH XXV-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-29-7 p-Br-Ph H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXV-29-8 p-Br-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-30. No R1 R2 R3 a R3 b R4 R' R6 X Y XXV-30-1 p-I-Ph H H H 'Pr H CH 3 F OH XXV-30-2 p-I-Ph H H CH3 'Pr H CH 3 F OH XXV-30-3 p-I-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXV-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXV-30-5 p-I-Ph H H CH 2Ph 'Pr H CH 3 F OH XXV-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXV-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXV-30-8 p-I-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-31. No R1 R2 R3 a R3b R4 R5 R6 X Y

XXV-31-1 CH3 H H H "Bu H CH3 F OH XXV-31-2 CH3 H H CH 3 "Bu H CH3 F OH XXV-31-3 CH3 H H CH(CH3) 2 "Bu H CH3 F OH XXV-31-4 CH3 H H CH 2CH(CH3)2 "Bu H CH3 F OH XXV-31-5 CH3 H H CH 2Ph "Bu H CH3 F OH XXV-31-6 CH3 H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-31-7 CH3 H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXV-31-8 CH3 * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A01 _

Table XXV-32. RI R 2 RaR 3 b R4 R R X Y No XXV-32-1 Et H H H "Bu H CH 3 F OH XXV-32-2 Et H H CH 3 "Bu H CH 3 F OH XXV-32-3 Et H H CH(CH3) 2 "Bu H CH 3 F OH XXV-32-4 Et H H CH 2CH(CH3)2 "Bu H CH 3 F OH XXV-32-5 Et H H CH 2Ph "Bu H CH 3 F OH XXV-32-6 Et H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-32-7 Et H H CH 2CH2SCH 3 "Bu H CH 3 F OH XXV-32-8 Et * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-33. No R1 R2 R 3a R3 b R4 R' R6 X Y XXV-33-1 'Pr H H H "Bu H CH 3 F OH XXV-33-2 'Pr H H CH3 "Bu H CH 3 F OH XXV-33-3 'Pr H H CH(CH 3) 2 "Bu H CH 3 F OH XXV-33-4 'Pr H H CH2CH(CH3) 2 "Bu H CH 3 F OH XXV-33-5 'Pr H H CH 2Ph "Bu H CH 3 F OH XXV-33-6 'Pr H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-33-7 'Pr H H CH2CH 2SCH 3 "Bu H CH 3 F OH XXV-33-8 'Pr * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-34. No R1 R2 R 3a R 3b R4 R5 R6 X Y XXV-34-1 'Bu H H H "Bu H CH 3 F OH XXV-34-2 'Bu H H CH 3 "Bu H CH 3 F OH XXV-34-3 'Bu H H CH(CH3)2 "Bu H CH 3 F OH XXV-34-4 'Bu H H CH 2CH(CH3) 2 "Bu H CH 3 F OH XXV-34-5 'Bu H H CH 2Ph "Bu H CH 3 F OH XXV-34-6 'Bu H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXV-34-8 'Bu * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

AO')-

Table XXV-35. No R1 R2 R3 a R 3 b R4 R 5 R6 X Y XXV-35-1 Ph H H H "Bu H CH 3 F OH XXV-35-2 Ph H H CH 3 "Bu H CH 3 F OH XXV-35-3 Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXV-35-4 Ph H H CH 2CH(CH3) 2 "Bu H CH 3 F OH XXV-35-5 Ph H H CH 2Ph "Bu H CH 3 F OH XXV-35-6 Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-35-7 Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXV-35-8 Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-36. No R R2 R 3 a R3 b R4 R 5 R6 X Y

XXV-36-1 p-Me-Ph H H H "Bu H CH 3 F OH XXV-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 F OH XXV-36-3 p-Me-Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXV-36-4 p-Me-Ph H H CH 2CH(CH 3)2 "Bu H CH 3 F OH XXV-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 F OH XXV-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXV-36-8 p-Me-Ph * H * "Bu H CH 3 F OH *R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXV-37. No R1 R2 R 3a R 3b R4 R5 R6 X Y XXV-37-1 p-F-Ph H H H "Bu H CH 3 F OH XXV-37-2 p-F-Ph H H CH 3 "Bu H CH 3 F OH XXV-37-3 p-F-Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXV-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H CH 3 F OH XXV-37-5 p-F-Ph H H CH 2Ph "Bu H CH 3 F OH XXV-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXV-37-8 p-F-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

A02

Table XXV-38. R' No R RR3a R3b R4 R' X Y XXV-38-1 p-Cl-Ph H H H "Bu H CH3 F OH XXV-38-2 p-Cl-Ph H H CH 3 "Bu H CH3 F OH XXV-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H CH3 F OH XXV-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H CH3 F OH XXV-38-5 p-Cl-Ph H H CH 2Ph "Bu H CH3 F OH XXV-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H CH3 F OH XXV-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH XXV-38-8 p-Cl-Ph * H * "Bu H CH3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXV-39. No R R 2 RWaRb R4 R 5 R6 X Y

XXV-39-1 p-Br-Ph H H H "Bu H CH 3 F OH XXV-39-2 p-Br-Ph H H CH 3 "Bu H CH 3 F OH XXV-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXV-39-4 p-Br-Ph H H CH 2 CH(CH3)2 "Bu H CH 3 F OH XXV-39-5 p-Br-Ph H H CH 2Ph "Bu H CH 3 F OH XXV-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH XXV-39-8 p-Br-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXV-40. No R1 R2 R3 a R3b R4 R 5 R6 X Y XXV-40-1 p-I-Ph H H H "Bu H CH 3 F OH XXV-40-2 p-I-Ph H H CH3 "Bu H CH 3 F OH XXV-40-3 p-I-Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXV-40-4 p-I-Ph H H CH2 CH(CH3) 2 "Bu H CH 3 F OH XXV-40-5 p-I-Ph H H CH 2 Ph "Bu H CH 3 F OH XXV-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXV-40-7 p-I-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 F OH XXV-40-8 p-I-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_IAo _

Table XXV-41. No R1 R2 R3 a R3b R4 R R X Y XXV-41-1 CH3 H H H Bz H CH 3 F OH XXV-41-2 CH3 H H CH 3 Bz H CH 3 F OH XXV-41-3 CH3 H H CH(CH3) 2 Bz H CH 3 F OH XXV-41-4 CH3 H H CH 2CH(CH3)2 Bz H CH 3 F OH XXV-41-5 CH3 H H CH 2Ph Bz H CH 3 F OH XXV-41-6 CH3 H H CH 2-indol-3-yl Bz H CH 3 F OH XXV-41-7 CH3 H H CH 2CH2SCH 3 Bz H CH 3 F OH XXV-41-8 CH3 * H * Bz H CH 3 F OH *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-42. N9 R1 R 2 R3 a R3 b R 4 R6 X Y XXV-42-1 Et H H H Bz H CH 3 F OH XXV-42-2 Et H H CH 3 Bz H CH 3 F OH XXV-42-3 Et H H CH(CH3) 2 Bz H CH 3 F OH XXV-42-4 Et H H CH 2CH(CH3)2 Bz H CH 3 F OH XXV-42-5 Et H H CH 2Ph Bz H CH 3 F OH XXV-42-6 Et H H CH 2-indol-3-yl Bz H CH 3 F OH XXV-42-7 Et H H CH 2CH2SCH 3 Bz H CH 3 F OH XXV-42-8 Et * H * Bz H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-43. N R1 R2 R 3a R3 b R4 R5 R6 X Y

XXV-43-1 'Pr H H H Bz H CH 3 F OH XXV-43-2 Pr H H CH3 Bz H CH 3 F OH XXV-43-3 Pr H H CH(CH 3) 2 Bz H CH 3 F OH XXV-43-4 Pr H H CH2CH(CH3) 2 Bz H CH 3 F OH XXV-43-5 Pr H H CH 2Ph Bz H CH 3 F OH XXV-43-6 'Pr H H CH 2-indol-3-yl Bz H CH 3 F OH XXV-43-7 'Pr H H CH2CH 2SCH 3 Bz H CH 3 F 9I XXV-43-8 'Pr * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A -o

Table XXV-44. No R1 R2 R 3a R 3b R4 R 5 R' X Y XXV-44-1 'Bu H H H Bz H CH 3 F OH XXV-44-2 'Bu H H CH 3 Bz H CH 3 F OH XXV-44-3 'Bu H H CH(CH3)2 Bz H CH 3 F OH XXV-44-4 'Bu H H CH 2CH(CH3) 2 Bz H CH 3 F OH XXV-44-5 'Bu H H CH 2Ph Bz H CH 3 F OH XXV-44-6 'Bu H H CH 2-indol-3-yl Bz H CH 3 F OH XXV-44-7 'Bu H H CH 2CH 2SCH 3 Bz H CH 3 F OH XXV-44-8 'Bu * H * Bz H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-45. N9 R1 R 2 R3a R3 b R4 R5 R6 X y

XXV-45-1 Ph H H H Bz H CH3 F OH XXV-45-2 Ph H H CH 3 Bz H CH3 F OH XXV-45-3 Ph H H CH(CH3) 2 Bz H CH3 F OH XXV-45-4 Ph H H CH 2CH(CH3) 2 Bz H CH3 F OH XXV-45-5 Ph H H CH 2Ph Bz H CH3 F OH XXV-45-6 Ph H H CH 2-indol-3-yl Bz H CH3 F OH XXV-45-7 Ph H H CH 2CH 2SCH 3 Bz H CH3 F OH XXV-45-8 Ph * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-46. No RI1 R2 R3 a R3b R4 R5 R6 X Y

XXV-46-1 p-Me-Ph H H H Bz H CH3 F OH XXV-46-2 p-Me-Ph H H CH3 Bz H CH3 F OH XXV-46-3 p-Me-Ph H H CH(CH 3)2 Bz H CH3 F OH XXV-46-4 p-Me-Ph H H CH2CH(CH 3) 2 Bz H CH3 F OH XXV-46-5 p-Me-Ph H H CH 2Ph Bz H CH3 F OH XXV-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH3 F OH XXV-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz H CH3 F OH XXV-46-8 p-Me-Ph * H * Bz H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

A A_

Table XXV-47. R R2 R 3 a R 3b R4 R' R' X Y No XXV-47-1 p-F-Ph H H H Bz H CH3 F OH XXV-47-2 p-F-Ph H H CH 3 Bz H CH3 F OH XXV-47-3 p-F-Ph H H CH(CH3) 2 Bz H CH3 F OH XXV-47-4 p-F-Ph H H CH 2CH(CH3) 2 Bz H CH3 F OH XXV-47-5 p-F-Ph H H CH 2Ph Bz H CH3 F OH XXV-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H CH3 F OH XXV-47-7 p-F-Ph H H CH 2CH 2SCH 3 Bz H CH3 F OH XXV-47-8 p-F-Ph * H * Bz H CH3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXV-48. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXV-48-1 p-Cl-Ph H H H Bz H CH 3 F OH XXV-48-2 p-Cl-Ph H H CH 3 Bz H CH 3 F OH XXV-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H CH 3 F OH XXV-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H CH 3 F OH XXV-48-5 p-Cl-Ph H H CH 2Ph Bz H CH 3 F OH XXV-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXV-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH XXV-48-8 p-Cl-Ph * H * Bz H CH 3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXV-49. R No R R2 R 3 a R3b R4 R X Y

XXV-49-1 p-Br-Ph H H H Bz H CH 3 F OH XXV-49-2 p-Br-Ph H H CH 3 Bz H CH 3 F OH XXV-49-3 p-Br-Ph H H CH(CH3) 2 Bz H CH 3 F OH XXV-49-4 p-Br-Ph H H CH 2CH(CH3)2 Bz H CH 3 F OH XXV-49-5 p-Br-Ph H H CH 2Ph Bz H CH 3 F OH XXV-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXV-49-7 p-Br-Ph H H CH 2CH2SCH 3 Bz H CH 3 F OH XXV-49-8 p-Br-Ph * H * Bz H CH 3 F OH *R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Ao

Table XXV-50. Rl R2 R3a R4 R5 R' X Y No R3b

XXV-50-1 p-I-Ph H H H Bz H CH3 F OH XXV-50-2 p-I-Ph H H CH3 Bz H CH3 F OH XXV-50-3 p-I-Ph H H CH(CH3) 2 Bz H CH3 F OH XXV-50-4 p-I-Ph H H CH2CH(CH3) 2 Bz H CH3 F OH XXV-50-5 p-I-Ph H H CH 2Ph Bz H CH3 F OH XXV-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH3 F OH XXV-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H CH3 F OH XXV-50-8 p-I-Ph * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

R3b R2 N N P 0 0 N R3a N- -0

4 C0 2 R OR Rs R6 NH 2

Y X XXVI

Table XXVI-1. 6 No R R22 R3 a R3b R4 R R X Y

XXVI-1-1 CH3 H H H CH 3 H F H OH XXVI-1-2 CH3 H H CH 3 CH3 H F H OH XXVI-1-3 CH3 H H CH(CH3) 2 CH 3 H F H OH XXVI-1-4 CH3 H H CH 2CH(CH3)2 CH 3 H F H OH XXVI-1-5 CH3 H H CH 2Ph CH3 H F H OH XXVI-1-6 CH3 H H CH 2-indol-3-yl CH 3 H F H OH XXVI-1-7 CH3 H H CH 2CH2SCH 3 CH 3 H F H OH XXVI-1-8 CH3 * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

AoQ-

Table XXVI-2. No Rl R 2 R3 a R 3b R4 R 5 R' X Y XXVI-2-1 Et H H H CH3 H F H OH XXVI-2-2 Et H H CH 3 CH 3 H F H OH XXVI-2-3 Et H H CH(CH3) 2 CH3 H F H OH XXVI-2-4 Et H H CH 2CH(CH3) 2 CH3 H F H OH XXVI-2-5 Et H H CH 2Ph CH3 H F H OH XXVI-2-6 Et H H CH 2-indol-3-yl CH 3 H F H OH XXVI-2-7 Et H H CH 2CH 2SCH3 CH3 H F H OH XXVI-2-8 Et * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-3. No R1 R2 R3 a R3 b R4 R' R6 X Y XXVI-3-1 'Pr H H H CH 3 H F H OH XXVI-3-2 'Pr H H CH 3 CH3 H F H OH XXVI-3-3 'Pr H H CH(CH3) 2 CH3 H F H OH XXVI-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H F H OH XXVI-3-5 'Pr H H CH 2Ph CH 3 H F H OH XXVI-3-6 'Pr H H CH 2-indol-3-yl CH3 H F H OH XXVI-3-7 'Pr H H CH 2CH2SCH 3 CH3 H F H OH XXVI-3-8 'Pr * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-4. No R1 R2 R 3a R3b R4 R 5 R6 X Y

XXVI-4-1 'Bu H H H CH 3 H F H OH XXVI-4-2 'Bu H H CH 3 CH 3 H F H OH XXVI-4-3 'Bu H H CH(CH3) 2 CH 3 H F H OH XXVI-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H F H OH XXVI-4-5 'Bu H H CH 2Ph CH 3 H F H OH XXVI-4-6 'Bu H H CH 2-indol-3-yl CH 3 H F H OH XXVI-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H F H OH XXVI-4-8 'Bu * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

AOO _

Table XXVI-5. No R1 R2 R3 a R 3b R4 R R 6 X Y

XXVI-5-1 Ph H H H CH 3 H F H OH XXVI-5-2 Ph H H CH3 CH3 H F H OH XXVI-5-3 Ph H H CH(CH3)2 CH3 H F H OH XXVI-5-4 Ph H H CH2CH(CH3) 2 CH3 H F H OH XXVI-5-5 Ph H H CH 2Ph CH 3 H F H OH XXVI-5-6 Ph H H CH 2-indol-3-yl CH3 H F H OH XXVI-5-7 Ph H H CH2CH2 SCH3 CH3 H F H OH XXVI-5-8 Ph * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-6. 6 N9 R1 R2 R3 a R3 b R4 R R X Y

XXVI-6-1 p-Me-Ph H H H CH 3 H F H OH XXVI-6-2 p-Me-Ph H H CH3 CH3 H F H OH XXVI-6-3 p-Me-Ph H H CH(CH3)2 CH3 H F H OH XXVI-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 H F H OH XXVI-6-5 p-Me-Ph H H CH 2Ph CH 3 H F H OH XXVI-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F H OH XXVI-6-7 p-Me-Ph H H CH2CH2 SCH3 CH3 H F H OH XXVI-6-8 p-Me-Ph * H * CH3 H F H OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-7. No R R2 R 3 a R3b R4 R R 6 X Y

XXVI-7-1 p-F-Ph H H H CH 3 H F H OH XXVI-7-2 p-F-Ph H H CH3 CH3 H F H OH XXVI-7-3 p-F-Ph H H CH(CH3)2 CH3 H F H OH XXVI-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H F H OH XXVI-7-6 p-F-Ph H H CH 2Ph CH 3 H F H OH XXVI-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F H OH XXVI-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H F H OH XXVI-7-20 p-F-Ph * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

;nn-

Table XXVI-8. No R R2 R3 a R3b R4 R R X Y XXVI-8-1 p-Cl-Ph H H H CH 3 H F H OH XXVI-8-2 p-Cl-Ph H H CH 3 CH 3 H F H OH XXVI-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F H OH XXVI-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H F H OH XXVI-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F H OH XXVI-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F H OH XXVI-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H F H OH XXVI-8-8 p-Cl-Ph * H * CH 3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-9. 5 N9 R1 R2 R 3a R3 b R4 R R6 X Y XXVI-9-1 p-Br-Ph H H H CH3 H F H OH XXVI-9-2 p-Br-Ph H H CH3 CH3 H F H OH XXVI-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H F H OH XXVI-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH3 H F H OH XXVI-9-6 p-Br-Ph H H CH 2Ph CH3 H F H OH XXVI-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H F H OH XXVI-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 H F H OH XXVI-9-20 p-Br-Ph * H * CH3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-10. No R R2 R 3 a R3b R4 R 5 R6 X Y

XXVI-10-1 p-I-Ph H H H CH 3 H F H OH XXVI-10-2 p-I-Ph H H CH3 CH 3 H F H OH XXVI-10-3 p-I-Ph H H CH(CH3)2 CH 3 H F H OH XXVI-10-4 p-I-Ph H H CH2CH(CH 3)2 CH 3 H F H OH XXVI-10-5 p-I-Ph H H CH 2Ph CH 3 H F H OH XXVI-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H F H OH XXVI-10-7 p-I-Ph H H CH2CH 2SCH 3 CH 3 H F H OH XXVI-10-8 p-I-Ph * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_1-_

Table XXVI-11. No R1 R2 R 3a R3b R4 R R X Y

XXVI-11-1 CH 3 H H H Et H F H OH XXVI-11-2 CH 3 H H CH3 Et H F H OH XXVI-11-3 CH3 H H CH(CH3) 2 Et H F H OH XXVI-11-4 CH 3 H H CH2CH(CH3) 2 Et H F H OH XXVI-11-5 CH 3 H H CH 2Ph Et H F H OH XXVI-11-6 CH3 H H CH 2-indol-3-yl Et H F H OH XXVI-11-7 CH3 H H CH2CH 2SCH 3 Et H F H OH XXVI-11-8 CH 3 * H * Et H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-12. No R1 R2 R3a R3b R4 R R X Y

XXVI-12-1 Et H H H Et H F H OH XXVI-12-2 Et H H CH 3 Et H F H OH XXVI-12-3 Et H H CH(CH3) 2 Et H F H OH XXVI-12-4 Et H H CH 2CH(CH3) 2 Et H F H OH XXVI-12-5 Et H H CH 2Ph Et H F H OH XXVI-12-6 Et H H CH 2-indol-3-yl Et H F H OH XXVI-12-7 Et H H CH 2CH 2SCH 3 Et H F H OH XXVI-12-8 Et * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-13. N R1 R2 R 3a R 3b R4 R5 R6 X Y XXVI-13-1 'Pr H H H Et H F H OH XXVI-13-2 'Pr H H CH 3 Et H F H OH XXVI-13-3 'Pr H H CH(CH3) 2 Et H F H OH XXVI-13-4 'Pr H H CH 2CH(CH3)2 Et H F H OH XXVI-13-5 Pr H H CH 2Ph Et H F H OH XXVI-13-6 Pr H H CH 2-indol-3-yl Et H F H OH XXVI-13-7 Pr H H CH 2CH 2SCH 3 Et H F H OH XXVI-13-8 Pr * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

nt )-

Table XXVI-14. No R1 R2 R3 a R3b R4 R' R' X Y XXVI-14-1 'Bu H H H Et H F H OH XXVI-14-2 'Bu H H CH 3 Et H F H OH XXVI-14-3 'Bu H H CH(CH 3) 2 Et H F H OH XXVI-14-4 'Bu H H CH 2CH(CH 3) 2 Et H F H OH XXVI-14-5 'Bu H H CH 2Ph Et H F H OH XXVI-14-6 'Bu H H CH 2-indol-3-yl Et H F H OH XXVI-14-7 'Bu H H CH 2CH2SCH 3 Et H F H OH XXVI-14-8 'Bu * H * Et H F H OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXVI-15. No R1 R2 R3a R3 b R4 R5 R6 X Y XXVI-15-1 Ph H H H Et H F H OH XXVI-15-2 Ph H H CH3 Et H F H OH XXVI-15-3 Ph H H CH(CH 3)2 Et H F H OH XXVI-15-4 Ph H H CH2CH(CH 3)2 Et H F H OH XXVI-15-5 Ph H H CH 2Ph Et H F H OH XXVI-15-6 Ph H H CH 2-indol-3-yl Et H F H OH XXVI-15-7 Ph H H CH2CH 2SCH 3 Et H F H OH XXVI-15-8 Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-16. No R R2 R 3 a R3b R4 R5 R6 X Y XXVI-16-1 p-Me-Ph H H H Et H F H OH XXVI-16-2 p-Me-Ph H H CH3 Et H F H OH XXVI-16-3 p-Me-Ph H H CH(CH 3)2 Et H F H OH XXVI-16-4 p-Me-Ph H H CH2CH(CH 3)2 Et H F H OH XXVI-16-5 p-Me-Ph H H CH 2Ph Et H F H OH XXVI-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F H OH XXVI-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H F H OH XXVI-16-8 p-Me-Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-17. No R RR 3 a R3b R4 R' R6 X Y XXVI-17-1 p-F-Ph H H H Et H F H OH XXVI-17-2 p-F-Ph H H CH3 Et H F H OH XXVI-17-3 p-F-Ph H H CH(CH3)2 Et H F H OH XXVI-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H F H OH XXVI-17-5 p-F-Ph H H CH 2Ph Et H F H OH XXVI-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F H OH XXVI-17-7 p-F-Ph H H CH2CH 2SCH 3 Et H F H OH XXVI-17-8 p-F-Ph * H * Et H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-18. 9 R1 R2 R3 a R3 b R4 R R6 X Y XXVI-18-1 p-Cl-Ph H H H Et H F H OH XXVI-18-2 p-Cl-Ph H H CH3 Et H F H OH XXVI-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F H OH XXVI-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F H OH XXVI-18-5 p-Cl-Ph H H CH2Ph Et H F H OH XXVI-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F H OH XXVI-18-7 p-Cl-Ph H H CH2CH2SCH 3 Et H F H OH XXVI-18-8 p-Cl-Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-19. No R R2 R 3 a R3b R4 R 5 R6 X Y XXVI-19-1 p-Br-Ph H H H Et H F H OH XXVI-19-2 p-Br-Ph H H CH3 Et H F H OH XXVI-19-3 p-Br-Ph H H CH(CH 3)2 Et H F H OH XXVI-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H F H OH XXVI-19-5 p-Br-Ph H H CH 2Ph Et H F H OH XXVI-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F H OH XXVI-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H F H OH XXVI-19-8 p-Br-Ph * H * Et H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-20. No R RR 3 a R3b R4 R' R6 X Y XXVI-20-1 p-I-Ph H H H Et H F H OH XXVI-20-2 p-I-Ph H H CH3 Et H F H OH XXVI-20-3 p-I-Ph H H CH(CH3)2 Et H F H OH XXVI-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H F H OH XXVI-20-5 p-I-Ph H H CH 2Ph Et H F H OH XXVI-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F H OH XXVI-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H F H OH XXVI-20-8 p-I-Ph * H * Et H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-21. No R1 R2 R 3a R3 b R4 R 5 R6 X Y XXVI-21-1 CH 3 H H H 'Pr H F H OH XXVI-21-2 CH 3 H H CH3 'Pr H F H OH XXVI-21-3 CH 3 H H CH(CH3) 2 'Pr H F H OH XXVI-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H F H OH XXVI-21-5 CH 3 H H CH 2Ph 'Pr H F H OH XXVI-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H F H OH XXVI-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H F H OH XXVI-21-8 CH 3 * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-22. No Rl R2 R 3a R3b R4 R5 R6 X Y XXVI-22-1 Et H H H 'Pr H F H OH XXVI-22-2 Et H H CH 3 'Pr H F H OH XXVI-22-3 Et H H CH(CH3) 2 'Pr H F H OH XXVI-22-4 Et H H CH 2CH(CH3) 2 'Pr H F H OH XXVI-22-5 Et H H CH 2Ph 'Pr H F H OH XXVI-22-6 Et H H CH 2-indol-3-yl 'Pr H F H OH XXVI-22-7 Et H H CH 2CH 2SCH 3 'Pr H F H OH XXVI-22-8 Et * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-23. No R1 R2 R 3a R3 R4 R R' X Y XXVI-23-1 'Pr H H H 'Pr H F H OH XXVI-23-2 'Pr H H CH 3 'Pr H F H OH XXVI-23-3 'Pr H H CH(CH3) 2 'Pr H F H OH XXVI-23-4 Pr H H CH 2CH(CH 3)2 'Pr H F H OH XXVI-23-5 Pr H H CH 2Ph 'Pr H F H OH XXVI-23-6 Pr H H CH 2-indol-3-yl 'Pr H F H OH XXVI-23-7 Pr H H CH 2CH2SCH 3 'Pr H F H OH XXVI-23-8 Pr * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-24. No R1 R2 R3 a R3 b R4 R R6 X Y XXVI-24-1 'Bu H H H 'Pr H F H OH XXVI-24-2 'Bu H H CH 3 'Pr H F H OH XXVI-24-3 'Bu H H CH(CH3) 2 'Pr H F H OH XXVI-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H F H OH XXVI-24-5 'Bu H H CH 2Ph 'Pr H F H OH XXVI-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F H OH XXVI-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H F H OH XXVI-24-8 'Bu * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-25. No R1 R2 R 3a R3b R4 R5 R6 X Y XXVI-25-1 Ph H H H 'Pr H F H OH XXVI-25-2 Ph H H CH3 'Pr H F H OH XXVI-25-3 Ph H H CH(CH 3)2 'Pr H F H OH XXVI-25-4 Ph H H CH2CH(CH3) 2 'Pr H F H OH XXVI-25-5 Ph H H CH 2Ph 'Pr H F H OH XXVI-25-6 Ph H H CH 2-indol-3-yl 'Pr H F H OH XXVI-25-7 Ph H H CH2CH 2SCH 3 'Pr H F H OH XXVI-25-8 Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

;nt;-

Table XXVI-26. No R RR 3 a R3b R4 R' R6 X Y XXVI-26-1 p-Me-Ph H H H 'Pr H F H OH XXVI-26-2 p-Me-Ph H H CH3 'Pr H F H OH XXVI-26-3 p-Me-Ph H H CH(CH 3)2 'Pr H F H OH XXVI-26-4 p-Me-Ph H H CH2CH(CH 3)2 'Pr H F H OH XXVI-26-5 p-Me-Ph H H CH 2Ph 'Pr H F H OH XXVI-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXVI-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H F H OH XXVI-26-8 p-Me-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-27. 9 R1 R2 R3 a R3 b R4 R' R6 X Y XXVI-27-1 p-F-Ph H H H 'Pr H F H OH XXVI-27-2 p-F-Ph H H CH3 'Pr H F H OH XXVI-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H F H OH XXVI-27-4 p-F-Ph H H CH2CH(CH 3) 2 'Pr H F H OH XXVI-27-5 p-F-Ph H H CH 2Ph 'Pr H F H OH XXVI-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXVI-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H F H OH XXVI-27-8 p-F-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-28. No R R2 R 3 a R 3b R 4 R6 X Y

XXVI-28-1 p-Cl-Ph H H H 'Pr H F H OH XXVI-28-2 p-Cl-Ph H H CH3 'Pr H F H OH XXVI-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F H OH XXVI-28-4 p-Cl-Ph H H CH2CH(CH 3) 2 'Pr H F H OH XXVI-28-5 p-Cl-Ph H H CH2Ph 'Pr H F H OH XXVI-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F H OH XXVI-28-7 p-Cl-Ph H H CH2CH2SCH 3 'Pr H F H OH XXVI-28-8 p-Cl-Ph * H * Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rW7-

Table XXVI-29. No R R2 R 3 a R3b R4 R' R6 X Y XXVI-29-1 p-Br-Ph H H H 'Pr H F H OH XXVI-29-2 p-Br-Ph H H CH3 'Pr H F H OH XXVI-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F H OH XXVI-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F H OH XXVI-29-5 p-Br-Ph H H CH 2Ph 'Pr H F H OH XXVI-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXVI-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F H OH XXVI-29-8 p-Br-Ph * H * 'Pr H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-30. No R R2 R3a R3 b R4 R' R6 X Y XXVI-30-1 p-I-Ph H H H 'Pr H F H OH XXVI-30-2 p-I-Ph H H CH3 'Pr H F H OH XXVI-30-3 p-I-Ph H H CH(CH 3)2 'Pr H F H OH XXVI-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H F H OH XXVI-30-5 p-I-Ph H H CH 2Ph 'Pr H F H OH XXVI-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXVI-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H F H OH XXVI-30-8 p-I-Ph * H * 'Pr H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-31. No R1 R2 R 3a R3b R4 R R 6 X Y

XXVI-31-1 CH 3 H H H "Bu H F H OH XXVI-31-2 CH 3 H H CH3 "Bu H F H OH XXVI-31-3 CH3 H H CH(CH3) 2 "Bu H F H OH XXVI-31-4 CH3 H H CH2CH(CH3) 2 "Bu H F H OH XXVI-31-5 CH3 H H CH 2Ph "Bu H F H OH XXVI-31-6 CH3 H H CH 2-indol-3-yl "Bu H F H OH XXVI-31-7 CH3 H H CH2CH 2SCH 3 "Bu H F H OH XXVI-31-8 CH3 * H * "Bu H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

rnQ-

Table XXVI-32. No R1 R2 R 3a R3b R4 R' R6 X Y XXVI-32-1 Et H H H "Bu H F H OH XXVI-32-2 Et H H CH 3 "Bu H F H OH XXVI-32-3 Et H H CH(CH 3)2 "Bu H F H OH XXVI-32-4 Et H H CH 2CH(CH 3)2 "Bu H F H OH XXVI-32-5 Et H H CH 2Ph "Bu H F H OH XXVI-32-6 Et H H CH 2-indol-3-yl "Bu H F H OH XXVI-32-7 Et H H CH 2CH 2SCH 3 "Bu H F H OH XXVI-32-8 Et * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-33. No R1 R2 R 3a RS R4 R R6 X Y XXVI-33-1 'Pr H H H "Bu H F H OH XXVI-33-2 'Pr H H CH 3 "Bu H F H OH XXVI-33-3 'Pr H H CH(CH 3)2 "Bu H F H OH XXVI-33-4 'Pr H H CH 2CH(CH 3)2 "Bu H F H OH XXVI-33-5 'Pr H H CH 2Ph "Bu H F H OH XXVI-33-6 'Pr H H CH 2-indol-3-yl "Bu H F H OH XXVI-33-7 'Pr H H CH 2CH 2SCH 3 "Bu H F H OH XXVI-33-8 'Pr * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-34. No R1 R2 R3 a R 3b R4 R R X Y XXVI-34-1 'Bu H H H "Bu H F H OH XXVI-34-2 'Bu H H CH 3 "Bu H F H OH XXVI-34-3 'Bu H H CH(CH 3) 2 "Bu H F H OH XXVI-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H F H OH XXVI-34-5 'Bu H H CH 2Ph "Bu H F H OH XXVI-34-6 'Bu H H CH 2-indol-3-yl "Bu H F H OH XXVI-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F H OH XXVI-34-8 'Bu * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_sno_

Table XXVI-35. No R1 R2 R 3a R3b R4 R 5 R6 X Y

XXVI-35-1 Ph H H H "Bu H F H OH XXVI-35-2 Ph H H CH3 "Bu H F H OH XXVI-35-3 Ph H H CH(CH3)2 "Bu H F H OH XXVI-35-4 Ph H H CH2CH(CH3) 2 "Bu H F H OH XXVI-35-5 Ph H H CH 2Ph "Bu H F H OH XXVI-35-6 Ph H H CH 2-indol-3-yl "Bu H F H OH XXVI-35-7 Ph H H CH2CH 2SCH 3 "Bu H F H OH XXVI-35-8 Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-36. N9 R1 R2 R 3a R3 b R4 R 5 R6 X Y

XXVI-36-1 p-Me-Ph H H H "Bu H F H OH XXVI-36-2 p-Me-Ph H H CH 3 "Bu H F H OH XXVI-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F H OH XXVI-36-4 p-Me-Ph H H CH 2CH(CH3) 2 "Bu H F H OH XXVI-36-5 p-Me-Ph H H CH 2Ph "Bu H F H OH XXVI-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F H OH XXVI-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXVI-36-8 p-Me-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXVI-37. No R1 R2 R3a R3b R4 R5 R6 X Y XXVI-37-1 p-F-Ph H H H "Bu H F H OH XXVI-37-2 p-F-Ph H H CH 3 "Bu H F H OH XXVI-37-3 p-F-Ph H H CH(CH3)2 "Bu H F H OH XXVI-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H F H OH XXVI-37-5 p-F-Ph H H CH 2Ph "Bu H F H OH XXVI-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F H OH XXVI-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXVI-37-8 p-F-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

_1in-

Table XXVI-38. R R2 R3 3b R4 R 5 R' X Y No XXVI-38-1 p-Cl-Ph H H H "Bu H F H OH XXVI-38-2 p-Cl-Ph H H CH3 "Bu H F H OH XXVI-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F H OH XXVI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F H OH XXVI-38-5 p-Cl-Ph H H CH2Ph "Bu H F H OH XXVI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F H OH XXVI-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H F H OH XXVI-38-8 p-Cl-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-39. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXVI-39-1 p-Br-Ph H H H "Bu H F H OH XXVI-39-2 p-Br-Ph H H CH 3 "Bu H F H OH XXVI-39-3 p-Br-Ph H H CH(CH 3 )2 "Bu H F H OH XXVI-39-4 p-Br-Ph H H CH 2 CH(CH 3)2 "Bu H F H OH XXVI-39-5 p-Br-Ph H H CH 2 Ph "Bu H F H OH XXVI-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F H OH XXVI-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H F H OH XXVI-39-8 p-Br-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-40. No R1 R2 R 3a R3b R4 R 5 R6 X Y XXVI-40-1 p-I-Ph H H H "Bu H F H OH XXVI-40-2 p-I-Ph H H CH 3 "Bu H F H OH XXVI-40-3 p-I-Ph H H CH(CH3)2 "Bu H F H OH XXVI-40-4 p-I-Ph H H CH 2 CH(CH3) 2 "Bu H F H OH XXVI-40-5 p-I-Ph H H CH 2 Ph "Bu H F H OH XXVI-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F H OH XXVI-40-7 p-I-Ph H H CH 2 CH 2 SCH 3 "Bu H F H OH XXVI-40-8 p-I-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 1i 1_

Table XXVI-41. No R1 R2 R 3a R3b R4 R' R' X Y XXVI-41-1 CH3 H H H Bz H F H OH XXVI-41-2 CH 3 H H CH3 Bz H F H OH XXVI-41-3 CH 3 H H CH(CH3) 2 Bz H F H OH XXVI-41-4 CH 3 H H CH2CH(CH3) 2 Bz H F H OH XXVI-41-5 CH 3 H H CH 2Ph Bz H F H OH XXVI-41-6 CH 3 H H CH 2-indol-3-yl Bz H F H OH XXVI-41-7 CH 3 H H CH2CH 2SCH 3 Bz H F H OH XXVI-41-8 CH 3 * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-42. No R1 R2 R3a R3b R4 R' R6 X Y XXVI-42-1 Et H H H Bz H F H OH XXVI-42-2 Et H H CH 3 Bz H F H OH XXVI-42-3 Et H H CH(CH3) 2 Bz H F H OH XXVI-42-4 Et H H CH 2CH(CH3) 2 Bz H F H OH XXVI-42-5 Et H H CH 2Ph Bz H F H OH XXVI-42-6 Et H H CH 2-indol-3-yl Bz H F H OH XXVI-42-7 Et H H CH 2CH 2SCH 3 Bz H F H OH XXVI-42-8 Et * H * Bz H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-43. N R1 R2 R 3a R3 b 4 R 5 R 6 X Y

XXVI-43-1 'Pr H H H Bz H F H OH XXVI-43-2 Pr H H CH 3 Bz H F H OH XXVI-43-3 Pr H H CH(CH3) 2 Bz H F H OH XXVI-43-4 Pr H H CH 2CH(CH 3)2 Bz H F H OH XXVI-43-5 Pr H H CH 2Ph Bz H F H OH XXVI-43-6 'Pr H H CH 2-indol-3-yl Bz H F H OH XXVI-43-7 'Pr H H CH 2CH2SCH 3 Bz H F H dAI XXVI-43-8 'Pr * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-44. No R1 R2 R3 a R3 R4 R R6 X Y XXVI-44-1 'Bu H H H Bz H F H OH XXVI-44-2 'Bu H H CH 3 Bz H F H OH XXVI-44-3 'Bu H H CH(CH3) 2 Bz H F H OH XXVI-44-4 'Bu H H CH 2CH(CH3)2 Bz H F H OH XXVI-44-5 'Bu H H CH 2Ph Bz H F H OH XXVI-44-6 'Bu H H CH 2-indol-3-yl Bz H F H OH XXVI-44-7 'Bu H H CH 2CH 2SCH 3 Bz H F H OH XXVI-44-8 'Bu * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-45. No R1 R2 R3a R3 R4 R 5 R6 X Y XXVI-45-1 Ph H H H Bz H F H OH XXVI-45-2 Ph H H CH3 Bz H F H OH XXVI-45-3 Ph H H CH(CH3)2 Bz H F H OH XXVI-45-4 Ph H H CH2CH(CH3) 2 Bz H F H OH XXVI-45-5 Ph H H CH 2Ph Bz H F H OH XXVI-45-6 Ph H H CH 2-indol-3-yl Bz H F H OH XXVI-45-7 Ph H H CH2CH 2SCH 3 Bz H F H OH XXVI-45-8 Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-46. No R R2 R 3 a R3b R4 R 5 R6 X Y XXVI-46-1 p-Me-Ph H H H Bz H F H OH XXVI-46-2 p-Me-Ph H H CH3 Bz H F H OH XXVI-46-3 p-Me-Ph H H CH(CH 3)2 Bz H F H OH XXVI-46-4 p-Me-Ph H H CH2CH(CH 3)2 Bz H F H OH XXVI-46-5 p-Me-Ph H H CH 2Ph Bz H F H OH XXVI-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F H OH XXVI-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz H F H OH XXVI-46-8 p-Me-Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

r12-l

Table XXVI-47. 5 No R RR 3 a R3b R4 R R' X Y XXVI-47-1 p-F-Ph H H H Bz H F H OH XXVI-47-2 p-F-Ph H H CH3 Bz H F H OH XXVI-47-3 p-F-Ph H H CH(CH 3) 2 Bz H F H OH XXVI-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H F H OH XXVI-47-5 p-F-Ph H H CH 2Ph Bz H F H OH XXVI-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F H OH XXVI-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H F H OH XXVI-47-8 p-F-Ph * H * Bz H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVI-48. N9 R1 R2 R3 a R3 b R4 R R6 X Y XXVI-48-1 p-Cl-Ph H H H Bz H F H OH XXVI-48-2 p-Cl-Ph H H CH3 Bz H F H OH XXVI-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F H OH XXVI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F H OH XXVI-48-5 p-Cl-Ph H H CH2Ph Bz H F H OH XXVI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H F H OH XXVI-48-7 p-Cl-Ph H H CH2CH2SCH 3 Bz H F H OH XXVI-48-8 p-Cl-Ph * H * Bz H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXVI-49. 5 No R R2 R 3 a R3b R4 R R6 X Y XXVI-49-1 p-Br-Ph H H H Bz H F H OH XXVI-49-2 p-Br-Ph H H CH3 Bz H F H OH XXVI-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F H OH XXVI-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H F H OH XXVI-49-5 p-Br-Ph H H CH 2Ph Bz H F H OH XXVI-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F H OH XXVI-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F H OH XXVI-49-8 p-Br-Ph * H * Bz H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

r 1A

Table XXVI-50. No R RR 3 a R3b R4 R 5 R6 X Y XXVI-50-1 p-I-Ph H H H Bz H F H OH XXVI-50-2 p-I-Ph H H CH3 Bz H F H OH XXVI-50-3 p-I-Ph H H CH(CH 3)2 Bz H F H OH XXVI-50-4 p-I-Ph H H CH2CH(CH 3)2 Bz H F H OH XXVI-50-5 p-I-Ph H H CH 2Ph Bz H F H OH XXVI-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F H OH XXVI-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H F H OH XXVI-50-8 p-I-Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R3b R2 0 N N P 0 0 N R3a N- -0

4 C0 2 R OR Rs R6 NH 2

Y X XXVII

Table XXVII-1. No R1 R2 R3 a R3 b R4 R5 R 6 X Y XXVII-1-1 CH3 H H H CH3 H F F OH XXVII-1-2 CH3 H H CH3 CH 3 H F F OH XXVII-1-3 CH3 H H CH(CH 3)2 CH3 H F F OH XXVII-1-4 CH3 H H CH2CH(CH 3) 2 CH3 H F F OH XXVII-1-5 CH3 H H CH 2Ph CH3 H F F OH XXVII-1-6 CH3 H H CH 2-indol-3-yl CH 3 H F F OH XXVII-1-7 CH3 H H CH2CH 2SCH 3 CH3 H F F OH XXVII-1-8 CH3 * H * CH3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-2. No Rl R 2 R3 a R3b R4 R 5 R6 X Y XXVII-2-1 Et H H H CH3 H F F OH XXVII-2-2 Et H H CH 3 CH3 H F F OH XXVII-2-3 Et H H CH(CH3) 2 CH3 H F F OH XXVII-2-4 Et H H CH 2CH(CH3) 2 CH3 H F F OH XXVII-2-5 Et H H CH 2Ph CH3 H F F OH XXVII-2-6 Et H H CH 2-indol-3-yl CH3 H F F OH XXVII-2-7 Et H H CH 2CH 2SCH 3 CH3 H F F OH XXVII-2-8 Et * H * CH 3 H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-3. No R1 R2 R3 a Rb R4 R R6 X Y XXVII-3-1 'Pr H H H CH 3 H F F OH XXVII-3-2 'Pr H H CH 3 CH 3 H F F OH XXVII-3-3 'Pr H H CH(CH3) 2 CH 3 H F F OH XXVII-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H F F OH XXVII-3-5 'Pr H H CH 2Ph CH 3 H F F OH XXVII-3-6 'Pr H H CH 2-indol-3-yl CH 3 H F F OH XXVII-3-7 'Pr H H CH 2CH2SCH 3 CH 3 H F F OH XXVII-3-8 'Pr * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-4. No R1 R2 R3 a R3 R4 R5 R 6 X Y XXVII-4-1 'Bu H H H CH 3 H F F OH XXVII-4-2 'Bu H H CH 3 CH 3 H F F OH XXVII-4-3 'Bu H H CH(CH3) 2 CH 3 H F F OH XXVII-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H F F OH XXVII-4-5 'Bu H H CH 2Ph CH 3 H F F OH XXVII-4-6 'Bu H H CH 2-indol-3-yl CH 3 H F F OH XXVII-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H F F OH XXVII-4-8 'Bu * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-5. No R1 R2 R3 a R3b R4 R 5 R 6 X Y

XXVII-5-1 Ph H H H CH 3 H F F OH XXVII-5-2 Ph H H CH3 CH3 H F F OH XXVII-5-3 Ph H H CH(CH3)2 CH3 H F F OH XXVII-5-4 Ph H H CH2CH(CH3) 2 CH3 H F F OH XXVII-5-5 Ph H H CH 2Ph CH 3 H F F OH XXVII-5-6 Ph H H CH 2-indol-3-yl CH3 H F F OH XXVII-5-7 Ph H H CH2CH 2SCH 3 CH3 H F F OH XXVII-5-8 Ph * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-6. 5 6 N9 R1 R2 R3 a R3 b R4 R R X Y

XXVII-6-1 p-Me-Ph H H H CH 3 H F F OH XXVII-6-2 p-Me-Ph H H CH3 CH3 H F F OH XXVII-6-3 p-Me-Ph H H CH(CH 3) 2 CH3 H F F OH XXVII-6-4 p-Me-Ph H H CH2CH(CH 3) 2 CH3 H F F OH XXVII-6-5 p-Me-Ph H H CH 2Ph CH 3 H F F OH XXVII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F F OH XXVII-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H F F OH XXVII-6-8 p-Me-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-7. No R R2 R 3 a R3b R4 R5 R6 X Y XXVII-7-1 p-F-Ph H H H CH 3 H F F OH XXVII-7-2 p-F-Ph H H CH 3 CH3 H F F OH XXVII-7-3 p-F-Ph H H CH(CH3) 2 CH3 H F F OH XXVII-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 H F F OH XXVII-7-6 p-F-Ph H H CH 2Ph CH 3 H F F OH XXVII-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F F OH XXVII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH3 H F F OH XXVII-7-20 p-F-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 1 '7 _

Table XXVII-8. No R R2 R3 a R3b R4 RR X Y XXVII-8-1 p-Cl-Ph H H H CH 3 H F F OH XXVII-8-2 p-Cl-Ph H H CH 3 CH 3 H F F OH XXVII-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F F OH XXVII-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H F F OH XXVII-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F F OH XXVII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F F OH XXVII-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H F F OH XXVII-8-8 p-Cl-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-9. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXVII-9-1 p-Br-Ph H H H CH3 H F F OH XXVII-9-2 p-Br-Ph H H CH3 CH3 H F F OH XXVII-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H F F OH XXVII-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH3 H F F OH XXVII-9-6 p-Br-Ph H H CH 2Ph CH3 H F F OH XXVII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H F F OH XXVII-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 H F F OH XXVII-9-20 p-Br-Ph * H * CH3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-10. No R R2 R 3a R 3b R4 R 5 R6 X Y

XXVII-10-1 p-I-Ph H H H CH 3 H F F OH XXVII-10-2 p-I-Ph H H CH 3 CH3 H F F OH XXVII-10-3 p-I-Ph H H CH(CH3) 2 CH3 H F F OH XXVII-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H F F OH XXVII-10-5 p-I-Ph H H CH 2Ph CH 3 H F F OH XXVII-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H F F OH XXVII-10-7 p-I-Ph H H CH 2CH2SCH 3 CH3 H F F OH XXVII-10-8 p-I-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

r12-

Table XXVII-11. No R1 R2 R 3 a R 3b R4 R R X Y

XXVII-11-1 CH3 H H H Et H F F OH XXVII-11-2 CH3 H H CH 3 Et H F F OH XXVII-11-3 CH3 H H CH(CH3) 2 Et H F F OH XXVII-11-4 CH3 H H CH 2CH(CH3) 2 Et H F F OH XXVII-11-5 CH3 H H CH 2Ph Et H F F OH XXVII-11-6 CH3 H H CH 2-indol-3-yl Et H F F OH XXVII-11-7 CH3 H H CH 2CH 2SCH 3 Et H F F OH XXVII-11-8 CH3 * H * Et H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-12. No R1 R2 R3a R3b R4 R R X Y

XXVII-12-1 Et H H H Et H F F OH XXVII-12-2 Et H H CH3 Et H F F OH XXVII-12-3 Et H H CH(CH3)2 Et H F F OH XXVII-12-4 Et H H CH2CH(CH3) 2 Et H F F OH XXVII-12-5 Et H H CH 2Ph Et H F F OH XXVII-12-6 Et H H CH 2-indol-3-yl Et H F F OH XXVII-12-7 Et H H CH2CH 2SCH 3 Et H F F OH XXVII-12-8 Et * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-13. N R1 R2 R3 a R 3b R4 R5 R6 X Y XXVII-13-1 'Pr H H H Et H F F OH XXVII-13-2 'Pr H H CH 3 Et H F F OH XXVII-13-3 'Pr H H CH(CH3) 2 Et H F F OH XXVII-13-4 'Pr H H CH 2CH(CH3)2 Et H F F OH XXVII-13-5 Pr H H CH 2Ph Et H F F OH XXVII-13-6 Pr H H CH 2-indol-3-yl Et H F F OH XXVII-13-7 Pr H H CH 2CH 2SCH3 Et H F F OH XXVII-13-8 Pr * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-14. R' R' No R1 R2 R3 a R3b R4 X Y XXVII-14-1 'Bu H H H Et H F F OH XXVII-14-2 'Bu H H CH3 Et H F F OH XXVII-14-3 'Bu H H CH(CH 3) 2 Et H F F OH XXVII-14-4 'Bu H H CH2CH(CH 3) 2 Et H F F OH XXVII-14-5 'Bu H H CH 2Ph Et H F F OH XXVII-14-6 'Bu H H CH 2-indol-3-yl Et H F F OH XXVII-14-7 'Bu H H CH2CH 2SCH 3 Et H F F OH XXVII-14-8 'Bu * H * Et H F F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXVII-15. No R1 R2 R3a R3b R4 R 5 R6 X Y XXVII-15-1 Ph H H H Et H F F OH XXVII-15-2 Ph H H CH 3 Et H F F OH XXVII-15-3 Ph H H CH(CH 3)2 Et H F F OH XXVII-15-4 Ph H H CH 2CH(CH 3)2 Et H F F OH XXVII-15-5 Ph H H CH 2Ph Et H F F OH XXVII-15-6 Ph H H CH 2-indol-3-yl Et H F F OH XXVII-15-7 Ph H H CH 2CH2SCH 3 Et H F F OH XXVII-15-8 Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-16. No R R2 R 3 a R 3b R4 R 5 R6 X Y XXVII-16-1 p-Me-Ph H H H Et H F F OH XXVII-16-2 p-Me-Ph H H CH 3 Et H F F OH XXVII-16-3 p-Me-Ph H H CH(CH 3)2 Et H F F OH XXVII-16-4 p-Me-Ph H H CH 2CH(CH 3)2 Et H F F OH XXVII-16-5 p-Me-Ph H H CH 2Ph Et H F F OH XXVII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F F OH XXVII-16-7 p-Me-Ph H H CH 2CH2SCH 3 Et H F F OH XXVII-16-8 p-Me-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-17. No R RR 3 a R3b R4 R' R6 X Y XXVII-17-1 p-F-Ph H H H Et H F F OH XXVII-17-2 p-F-Ph H H CH 3 Et H F F OH XXVII-17-3 p-F-Ph H H CH(CH3) 2 Et H F F OH XXVII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et H F F OH XXVII-17-5 p-F-Ph H H CH 2Ph Et H F F OH XXVII-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F F OH XXVII-17-7 p-F-Ph H H CH 2CH2SCH 3 Et H F F OH XXVII-17-8 p-F-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-18. N9 R1 R2 R3 a R3 b R4 R R 6 X Y XXVII-18-1 p-Cl-Ph H H H Et H F F OH XXVII-18-2 p-Cl-Ph H H CH 3 Et H F F OH XXVII-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F F OH XXVII-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et H F F OH XXVII-18-5 p-Cl-Ph H H CH 2Ph Et H F F OH XXVII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F F OH XXVII-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et H F F OH XXVII-18-8 p-Cl-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-19. No R R2 R 3 a R 3b R4 R 5 R6 X Y XXVII-19-1 p-Br-Ph H H H Et H F F OH XXVII-19-2 p-Br-Ph H H CH3 Et H F F OH XXVII-19-3 p-Br-Ph H H CH(CH3) 2 Et H F F OH XXVII-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H F F OH XXVII-19-5 p-Br-Ph H H CH 2Ph Et H F F OH XXVII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F F OH XXVII-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H F F OH XXVII-19-8 p-Br-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

_Gi _

Table XXVII-20. No R RR 3 a R 3b R4 R' R' X Y XXVII-20-1 p-I-Ph H H H Et H F F OH XXVII-20-2 p-I-Ph H H CH 3 Et H F F OH XXVII-20-3 p-I-Ph H H CH(CH 3)2 Et H F F OH XXVII-20-4 p-I-Ph H H CH 2CH(CH3)2 Et H F F OH XXVII-20-5 p-I-Ph H H CH 2Ph Et H F F OH XXVII-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F F OH XXVII-20-7 p-I-Ph H H CH 2CH2SCH 3 Et H F F OH XXVII-20-8 p-I-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-21. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y XXVII-21-1 CH3 H H H 'Pr H F F OH XXVII-21-2 CH3 H H CH 3 'Pr H F F OH XXVII-21-3 CH3 H H CH(CH3) 2 'Pr H F F OH XXVII-21-4 CH3 H H CH 2CH(CH3) 2 'Pr H F F OH XXVII-21-5 CH3 H H CH 2Ph 'Pr H F F OH XXVII-21-6 CH3 H H CH 2-indol-3-yl 'Pr H F F OH XXVII-21-7 CH3 H H CH 2CH 2SCH 3 'Pr H F F OH XXVII-21-8 CH3 * H * 'Pr H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-22. No Rl R2 R3 a R 3b R4 R 5 R6 X Y

XXVII-22-1 Et H H H 'Pr H F F OH XXVII-22-2 Et H H CH3 'Pr H F F OH XXVII-22-3 Et H H CH(CH3)2 'Pr H F F OH XXVII-22-4 Et H H CH2CH(CH3) 2 'Pr H F F OH XXVII-22-5 Et H H CH 2Ph 'Pr H F F OH XXVII-22-6 Et H H CH 2-indol-3-yl 'Pr H F F OH XXVII-22-7 Et H H CH2CH 2SCH 3 'Pr H F F OH XXVII-22-8 Et * H * 'Pr H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-23. No R1 R2 R3 a R3 R4 R R' X Y XXVII-23-1 'Pr H H H 'Pr H F F OH XXVII-23-2 'Pr H H CH 3 'Pr H F F OH XXVII-23-3 'Pr H H CH(CH3) 2 'Pr H F F OH XXVII-23-4 Pr H H CH 2CH(CH 3) 2 'Pr H F F OH XXVII-23-5 Pr H H CH 2Ph 'Pr H F F OH XXVII-23-6 Pr H H CH 2-indol-3-yl 'Pr H F F OH XXVII-23-7 Pr H H CH 2CH 2SCH3 'Pr H F F OH XXVII-23-8 Pr * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-24. M R1 R2 R3 a R3 b R4 R R6 X Y XXVII-24-1 'Bu H H H 'Pr H F F OH XXVII-24-2 'Bu H H CH 3 'Pr H F F OH XXVII-24-3 'Bu H H CH(CH3) 2 'Pr H F F OH XXVII-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H F F OH XXVII-24-5 'Bu H H CH 2Ph 'Pr H F F OH XXVII-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F F OH XXVII-24-7 'Bu H H CH 2CH2SCH 3 'Pr H F F OH XXVII-24-8 'Bu * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-25. No R1 R2 R 3a R 3b R4 R5 R6 X Y XXVII-25-1 Ph H H H Pr H F F OH XXVII-25-2 Ph H H CH 3 Pr H F F OH XXVII-25-3 Ph H H CH(CH3) 2 'Pr H F F OH XXVII-25-4 Ph H H CH 2CH(CH 3)2 'Pr H F F OH XXVII-25-5 Ph H H CH 2Ph 'Pr H F F OH XXVII-25-6 Ph H H CH 2-indol-3-yl 'Pr H F F OH XXVII-25-7 Ph H H CH 2CH2SCH 3 'Pr H F F OH XXVII-25-8 Ph * H * Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-26. No R RR 3 a R 3b R4 R' R6 X Y XXVII-26-1 p-Me-Ph H H H 'Pr H F F OH XXVII-26-2 p-Me-Ph H H CH 3 'Pr H F F OH XXVII-26-3 p-Me-Ph H H CH(CH 3)2 'Pr H F F OH XXVII-26-4 p-Me-Ph H H CH 2CH(CH 3)2 'Pr H F F OH XXVII-26-5 p-Me-Ph H H CH 2Ph 'Pr H F F OH XXVII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXVII-26-7 p-Me-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXVII-26-8 p-Me-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-27. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXVII-27-1 p-F-Ph H H H 'Pr H F F OH XXVII-27-2 p-F-Ph H H CH 3 'Pr H F F OH XXVII-27-3 p-F-Ph H H CH(CH 3)2 'Pr H F F OH XXVII-27-4 p-F-Ph H H CH 2CH(CH 3) 2 'Pr H F F OH XXVII-27-5 p-F-Ph H H CH 2Ph 'Pr H F F OH XXVII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXVII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXVII-27-8 p-F-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-28. 5 No R R2 R 3 a R3b R4 R RXY XXVII-28-1 p-Cl-Ph H H H 'Pr H F F OH XXVII-28-2 p-Cl-Ph H H CH 3 'Pr H F F OH XXVII-28-3 p-Cl-Ph H H CH(CH 3) 2 'Pr H F F OH XXVII-28-4 p-Cl-Ph H H CH 2CH(CH3) 2 'Pr H F F OH XXVII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F F OH XXVII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXVII-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXVII-28-8 p-Cl-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-29. No R R2 R 3 a R 3b R4 R' R6 X Y XXVII-29-1 p-Br-Ph H H H 'Pr H F F OH XXVII-29-2 p-Br-Ph H H CH3 'Pr H F F OH XXVII-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F F OH XXVII-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F F OH XXVII-29-5 p-Br-Ph H H CH 2Ph 'Pr H F F OH XXVII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXVII-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXVII-29-8 p-Br-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-30. No R R2 R3a R3 b R4 R' R6 X Y XXVII-30-1 p-I-Ph H H H 'Pr H F F OH XXVII-30-2 p-I-Ph H H CH 3 'Pr H F F OH XXVII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F F OH XXVII-30-4 p-I-Ph H H CH 2CH(CH 3)2 'Pr H F F OH XXVII-30-5 p-I-Ph H H CH 2Ph 'Pr H F F OH XXVII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXVII-30-7 p-I-Ph H H CH 2CH2SCH 3 'Pr H F F OH XXVII-30-8 p-I-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-31. No R1 R2 R 3 a R 3b R4 R 5 R6 X Y

XXVII-31-1 CH3 H H H "Bu H F F OH XXVII-31-2 CH3 H H CH 3 "Bu H F F OH XXVII-31-3 CH3 H H CH(CH3) 2 "Bu H F F OH XXVII-31-4 CH3 H H CH 2CH(CH3) 2 "Bu H F F OH XXVII-31-5 CH3 H H CH 2Ph "Bu H F F OH XXVII-31-6 CH3 H H CH 2-indol-3-yl "Bu H F F OH XXVII-31-7 CH3 H H CH 2CH 2SCH 3 "Bu H F F OH XXVII-31-8 CH3 * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

ry -)r

Table XXVII-32. No Rl R2 R3 a R 3b R4 R' R6 X Y XXVII-32-1 Et H H H "Bu H F F OH XXVII-32-2 Et H H CH3 "Bu H F F OH XXVII-32-3 Et H H CH(CH3)2 "Bu H F F OH XXVII-32-4 Et H H CH2CH(CH3) 2 "Bu H F F OH XXVII-32-5 Et H H CH 2Ph "Bu H F F OH XXVII-32-6 Et H H CH 2-indol-3-yl "Bu H F F OH XXVII-32-7 Et H H CH2CH 2SCH 3 "Bu H F F OH XXVII-32-8 Et * H * "Bu H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-33. No R1 R2 R3 a Rb R4 R R6 X Y XXVII-33-1 'Pr H H H "Bu H F F OH XXVII-33-2 'Pr H H CH 3 "Bu H F F OH XXVII-33-3 'Pr H H CH(CH3) 2 "Bu H F F OH XXVII-33-4 'Pr H H CH 2CH(CH3)2 "Bu H F F OH XXVII-33-5 'Pr H H CH 2Ph "Bu H F F OH XXVII-33-6 'Pr H H CH 2-indol-3-yl "Bu H F F OH XXVII-33-7 'Pr H H CH 2CH 2SCH3 "Bu H F F OH XXVII-33-8 'Pr * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-34. RI No R2 R3a R3b R4 R R X Y XXVII-34-1 'Bu H H H "Bu H F F OH XXVII-34-2 'Bu H H CH 3 "Bu H F F OH XXVII-34-3 'Bu H H CH(CH3) 2 "Bu H F F OH XXVII-34-4 'Bu H H CH 2CH(CH3)2 "Bu H F F OH XXVII-34-5 'Bu H H CH 2Ph "Bu H F F OH XXVII-34-6 'Bu H H CH 2-indol-3-yl "Bu H F F OH XXVII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F F OH XXVII-34-8 'Bu * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-35. No R1 R2 R 3a R 3b R4 R 5 R' X Y XXVII-35-1 Ph H H H "Bu H F F OH XXVII-35-2 Ph H H CH 3 "Bu H F F OH XXVII-35-3 Ph H H CH(CH3) 2 "Bu H F F OH XXVII-35-4 Ph H H CH 2CH(CH3)2 "Bu H F F OH XXVII-35-5 Ph H H CH 2Ph "Bu H F F OH XXVII-35-6 Ph H H CH 2-indol-3-yl "Bu H F F OH XXVII-35-7 Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXVII-35-8 Ph * H * "Bu H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-36. N R1 R2 R3a R3b R4 R 5 R6 X Y XXVII-36-1 p-Me-Ph H H H "Bu H F F OH XXVII-36-2 p-Me-Ph H H CH 3 "Bu H F F OH XXVII-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H F F OH XXVII-36-4 p-Me-Ph H H CH 2CH(CH 3)2 "Bu H F F OH XXVII-36-5 p-Me-Ph H H CH 2Ph "Bu H F F OH XXVII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F F OH XXVII-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXVII-36-8 p-Me-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXVII-37. No R1 R2 R 3a R3b R4 R 5 R6 X Y XXVII-37-1 p-F-Ph H H H "Bu H F F OH XXVII-37-2 p-F-Ph H H CH 3 "Bu H F F OH XXVII-37-3 p-F-Ph H H CH(CH3) 2 "Bu H F F OH XXVII-37-4 p-F-Ph H H CH 2CH(CH3)2 "Bu H F F OH XXVII-37-5 p-F-Ph H H CH 2Ph "Bu H F F OH XXVII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F F OH XXVII-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXVII-37-8 p-F-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

r7-

Table XXVII-38. No R R2 R 3 a R3b R4 RR X Y XXVII-38-1 p-Cl-Ph H H H "Bu H F F OH XXVII-38-2 p-Cl-Ph H H CH 3 "Bu H F F OH XXVII-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F F OH XXVII-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H F F OH XXVII-38-5 p-Cl-Ph H H CH 2Ph "Bu H F F OH XXVII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F F OH XXVII-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH XXVII-38-8 p-Cl-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-39. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXVII-39-1 p-Br-Ph H H H "Bu H F F OH XXVII-39-2 p-Br-Ph H H CH 3 "Bu H F F OH XXVII-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H F F OH XXVII-39-4 p-Br-Ph H H CH 2 CH(CH3) 2 "Bu H F F OH XXVII-39-5 p-Br-Ph H H CH 2 Ph "Bu H F F OH XXVII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F F OH XXVII-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH XXVII-39-8 p-Br-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-40. No R1 R2 R 3a R 3b R4 R 5 R6 X Y XXVII-40-1 p-I-Ph H H H "Bu H F F OH XXVII-40-2 p-I-Ph H H CH 3 "Bu H F F OH XXVII-40-3 p-I-Ph H H CH(CH3) 2 "Bu H F F OH XXVII-40-4 p-I-Ph H H CH 2CH(CH 3 )2 "Bu H F F OH XXVII-40-5 p-I-Ph H H CH 2Ph "Bu H F F OH XXVII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F F OH XXVII-40-7 p-I-Ph H H CH 2CH 2 SCH 3 "Bu H F F OH XXVII-40-8 p-I-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

t r; )Q-

Table XXVII-41. No R1 R2 R 3 a R 3b R4 R' R' X Y XXVII-41-1 CH3 H H H Bz H F F OH XXVII-41-2 CH3 H H CH 3 Bz H F F OH XXVII-41-3 CH3 H H CH(CH3) 2 Bz H F F OH XXVII-41-4 CH3 H H CH 2CH(CH3) 2 Bz H F F OH XXVII-41-5 CH3 H H CH 2Ph Bz H F F OH XXVII-41-6 CH3 H H CH 2-indol-3-yl Bz H F F OH XXVII-41-7 CH3 H H CH 2CH 2SCH 3 Bz H F F OH XXVII-41-8 CH3 * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-42. R3a No R 1 R2 R3 b R4 R 5 R 6 X Y

XXVII-42-1 Et H H H Bz H F F OH XXVII-42-2 Et H H CH3 Bz H F F OH XXVII-42-3 Et H H CH(CH3)2 Bz H F F OH XXVII-42-4 Et H H CH2CH(CH3) 2 Bz H F F OH XXVII-42-5 Et H H CH 2Ph Bz H F F OH XXVII-42-6 Et H H CH 2-indol-3-yl Bz H F F OH XXVII-42-7 Et H H CH2CH 2SCH 3 Bz H F F OH XXVII-42-8 Et * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-43. R I' R RaR 3b4 R5 R6 X 2 3 Y

XXVII-43-1 'Pr H H H Bz H F F OH XXVII-43-2 Pr H H CH 3 Bz H F F OH XXVII-43-3 Pr H H CH(CH3) 2 Bz H F F OH XXVII-43-4 Pr H H CH 2CH(CH 3) 2 Bz H F F OH XXVII-43-5 Pr H H CH 2Ph Bz H F F OH XXVII-43-6 'Pr H H CH 2-indol-3-yl Bz H F F OH XXVII-43-7 'Pr H H CH 2CH 2SCH3 Bz H F F dAI XXVII-43-8 'Pr * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ yo _

Table XXVII-44. No RI R2 RaR 3 b R4 R R X Y XXVII-44-1 'Bu H H H Bz H F F OH XXVII-44-2 'Bu H H CH 3 Bz H F F OH XXVII-44-3 'Bu H H CH(CH3) 2 Bz H F F OH XXVII-44-4 'Bu H H CH 2CH(CH3)2 Bz H F F OH XXVII-44-5 'Bu H H CH 2Ph Bz H F F OH XXVII-44-6 'Bu H H CH 2-indol-3-yl Bz H F F OH XXVII-44-7 'Bu H H CH 2CH2SCH 3 Bz H F F OH XXVII-44-8 'Bu * H * Bz H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-45. No R1 R2 R3a R3b R4 R5 R6 X Y XXVII-45-1 Ph H H H Bz H F F OH XXVII-45-2 Ph H H CH 3 Bz H F F OH XXVII-45-3 Ph H H CH(CH3) 2 Bz H F F OH XXVII-45-4 Ph H H CH 2CH(CH3)2 Bz H F F OH XXVII-45-5 Ph H H CH 2Ph Bz H F F OH XXVII-45-6 Ph H H CH 2-indol-3-yl Bz H F F OH XXVII-45-7 Ph H H CH 2CH2SCH 3 Bz H F F OH XXVII-45-8 Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-46. No R R2 R 3 a R 3b R4 R5 R6 X Y XXVII-46-1 p-Me-Ph H H H Bz H F F OH XXVII-46-2 p-Me-Ph H H CH 3 Bz H F F OH XXVII-46-3 p-Me-Ph H H CH(CH 3)2 Bz H F F OH XXVII-46-4 p-Me-Ph H H CH 2CH(CH 3)2 Bz H F F OH XXVII-46-5 p-Me-Ph H H CH 2Ph Bz H F F OH XXVII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F F OH XXVII-46-7 p-Me-Ph H H CH 2CH2SCH 3 Bz H F F OH XXVII-46-8 p-Me-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

;2fl-

Table XXVII-47. No R RR 3 a R3b R4 R 5 R6 X Y XXVII-47-1 p-F-Ph H H H Bz H F F OH XXVII-47-2 p-F-Ph H H CH 3 Bz H F F OH XXVII-47-3 p-F-Ph H H CH(CH 3)2 Bz H F F OH XXVII-47-4 p-F-Ph H H CH 2CH(CH3)2 Bz H F F OH XXVII-47-5 p-F-Ph H H CH 2Ph Bz H F F OH XXVII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F F OH XXVII-47-7 p-F-Ph H H CH 2CH2SCH 3 Bz H F F OH XXVII-47-8 p-F-Ph * H * Bz H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVII-48. N9 R1 R2 R3 a R3 b R4 R R6 X Y XXVII-48-1 p-Cl-Ph H H H Bz H F F OH XXVII-48-2 p-Cl-Ph H H CH 3 Bz H F F OH XXVII-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F F OH XXVII-48-4 p-Cl-Ph H H CH 2CH(CH3) 2 Bz H F F OH XXVII-48-5 p-Cl-Ph H H CH 2Ph Bz H F F OH XXVII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F F OH XXVII-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz H F F OH XXVII-48-8 p-Cl-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVII-49. 5 No R R2 R 3a R 3b R4 R R6 X Y XXVII-49-1 p-Br-Ph H H H Bz H F F OH XXVII-49-2 p-Br-Ph H H CH3 Bz H F F OH XXVII-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F F OH XXVII-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H F F OH XXVII-49-5 p-Br-Ph H H CH 2Ph Bz H F F OH XXVII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F F OH XXVII-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F F OH XXVII-49-8 p-Br-Ph * H * Bz H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

_21 _

Table XXVII-50. No R RR 3 a R 3b R4 R5 R6 X Y XXVII-50-1 p-I-Ph H H H Bz H F F OH XXVII-50-2 p-I-Ph H H CH 3 Bz H F F OH XXVII-50-3 p-I-Ph H H CH(CH 3)2 Bz H F F OH XXVII-50-4 p-I-Ph H H CH 2CH(CH 3)2 Bz H F F OH XXVII-50-5 p-I-Ph H H CH 2Ph Bz H F F OH XXVII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F F OH XXVII-50-7 p-I-Ph H H CH 2CH2SCH 3 Bz H F F OH XXVII-50-8 p-I-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

R3b R2 0 N N P 0 0 N R3a N- - OO

C0 2 R 4 OR Rs R6 NH 2

Y X XXVIII

Table XXVIII-1. R 5 No R2 R 3a R3 b R4 R R6 X Y

XXVIII-1-1 CH 3 H H H CH3 H H F OH XXVIII-1-2 CH 3 H H CH3 CH3 H H F OH XXVIII-1-3 CH 3 H H CH(CH 3) 2 CH3 H H F OH XXVIII-1-4 CH 3 H H CH2CH(CH 3)2 CH3 H H F OH XXVIII-1-5 CH 3 H H CH 2Ph CH3 H H F OH XXVIII-1-6 CH 3 H H CH 2-indol-3-yl CH3 H H F OH XXVIII-1-7 CH 3 H H CH2CH 2SCH 3 CH3 H H F OH XXVIII-1-8 CH 3 * H * CH3 H H F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

r~l)-

Table XXVIII-2. No Rl R2 R 3a R 3b R4 R' R6 X Y XXVIII-2-1 Et H H H CH 3 H H F OH XXVIII-2-2 Et H H CH3 CH3 H H F OH XXVIII-2-3 Et H H CH(CH3)2 CH3 H H F OH XXVIII-2-4 Et H H CH2CH(CH3) 2 CH3 H H F OH XXVIII-2-5 Et H H CH 2Ph CH 3 H H F OH XXVIII-2-6 Et H H CH 2-indol-3-yl CH3 H H F OH XXVIII-2-7 Et H H CH2CH 2SCH 3 CH3 H H F OH XXVIII-2-8 Et * H * CH 3 H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-3. No R1 R2 R 3a R3 b R4 R R 6 X Y

XXVIII-3-1 'Pr H H H CH3 H H F OH XXVIII-3-2 'Pr H H CH 3 CH3 H H F OH XXVIII-3-3 'Pr H H CH(CH3) 2 CH 3 H H F OH XXVIII-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H H F OH XXVIII-3-5 'Pr H H CH 2Ph CH3 H H F OH XXVIII-3-6 'Pr H H CH 2-indol-3-yl CH 3 H H F OH XXVIII-3-7 'Pr H H CH 2CH2SCH 3 CH 3 H H F OH XXVIII-3-8 'Pr * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-4. No R1 22 R3 a R3b R4 R R 6 X Y

XXVIII-4-1 'Bu H H H CH3 H H F OH XXVIII-4-2 'Bu H H CH 3 CH3 H H F OH XXVIII-4-3 'Bu H H CH(CH3) 2 CH 3 H H F OH XXVIII-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H H F OH XXVIII-4-5 'Bu H H CH 2Ph CH3 H H F OH XXVIII-4-6 'Bu H H CH 2-indol-3-yl CH 3 H H F OH XXVIII-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H H F OH XXVIII-4-8 'Bu * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

r;Il-

Table XXVIII-5. RI No R2 RaR 3 b R4 RR X Y XXVIII-5-1 Ph H H H CH3 H H F OH XXVIII-5-2 Ph H H CH 3 CH3 H H F OH XXVIII-5-3 Ph H H CH(CH3) 2 CH3 H H F OH XXVIII-5-4 Ph H H CH 2CH(CH3)2 CH3 H H F OH XXVIII-5-5 Ph H H CH 2Ph CH3 H H F OH XXVIII-5-6 Ph H H CH 2-indol-3-yl CH3 H H F OH XXVIII-5-7 Ph H H CH 2CH2SCH 3 CH3 H H F OH XXVIII-5-8 Ph * H * CH3 H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-6. 2 3a 3 Nt R RRR R4 R5 R6 X Y

XXVIII-6-1 p-Me-Ph H H H CH3 H H F OH XXVIII-6-2 p-Me-Ph H H CH 3 CH3 H H F OH XXVIII-6-3 p-Me-Ph H H CH(CH 3)2 CH3 H H F OH XXVIII-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH3 H H F OH XXVIII-6-5 p-Me-Ph H H CH 2Ph CH3 H H F OH XXVIII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H H F OH XXVIII-6-7 p-Me-Ph H H CH 2CH2SCH 3 CH3 H H F OH XXVIII-6-8 p-Me-Ph * H * CH3 H H F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-7. No RI 1 R2 R 3a R3b R4 R R6 X Y XXVIII-7-1 p-F-Ph H H H CH 3 H H F OH XXVIII-7-2 p-F-Ph H H CH 3 CH 3 H H F OH XXVIII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 H H F OH XXVIII-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 H H F OH XXVIII-7-6 p-F-Ph H H CH 2Ph CH 3 H H F OH XXVIII-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXVIII-7-8 p-F-Ph H H CH 2CH2SCH 3 CH 3 H H F OH XXVIII-7-20 p-F-Ph * H * CH 3 H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

2'A-

Table XXVIII-8. No R R2 R 3 a R 3b R4 R 5 R' X Y XXVIII-8-1 p-Cl-Ph H H H CH3 H H F OH XXVIII-8-2 p-Cl-Ph H H CH 3 CH3 H H F OH XXVIII-8-3 p-Cl-Ph H H CH(CH3) 2 CH3 H H F OH XXVIII-8-4 p-Cl-Ph H H CH 2CH(CH3) 2 CH3 H H F OH XXVIII-8-5 p-Cl-Ph H H CH 2Ph CH3 H H F OH XXVIII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 H H F OH XXVIII-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH3 H H F OH XXVIII-8-8 p-Cl-Ph * H * CH3 H H F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-9. N R1 R2 R3a R3b R4 R' R6 X Y XXVIII-9-1 p-Br-Ph H H H CH 3 H H F OH XXVIII-9-2 p-Br-Ph H H CH 3 CH3 H H F OH XXVIII-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H H F OH XXVIII-9-4 p-Br-Ph H H CH 2CH(CH 3) 2 CH 3 H H F OH XXVIII-9-6 p-Br-Ph H H CH 2Ph CH 3 H H F OH XXVIII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H H F OH XXVIII-9-8 p-Br-Ph H H CH 2CH 2SCH3 CH3 H H F OH XXVIII-9-20 p-Br-Ph * H * CH 3 H H F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-10. No R R2 R 3 a R3b R4 R5 R 6 X Y XXVIII-10-1 p-I-Ph H H H CH 3 H H F OH XXVIII-10-2 p-I-Ph H H CH 3 CH 3 H H F OH XXVIII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H H F OH XXVIII-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H H F OH XXVIII-10-5 p-I-Ph H H CH 2Ph CH 3 H H F OH XXVIII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXVIII-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXVIII-10-8 p-I-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-11. No R1 R2 R3 a R3b R4 R' R6 X Y XXVIII-11-1 CH3 H H H Et H H F OH XXVIII-11-2 CH3 H H CH3 Et H H F OH XXVIII-11-3 CH3 H H CH(CH3)2 Et H H F OH XXVIII-11-4 CH 3 H H CH2CH(CH3) 2 Et H H F OH XXVIII-11-5 CH 3 H H CH 2Ph Et H H F OH XXVIII-11-6 CH3 H H CH 2-indol-3-yl Et H H F OH XXVIII-11-7 CH3 H H CH2CH 2SCH 3 Et H H F OH XXVIII-11-8 CH 3 * H * Et H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-12. R3a No R1 R2 R3 b R4 R' R6 X Y XXVIII-12-1 Et H H H Et H H F OH XXVIII-12-2 Et H H CH3 Et H H F OH XXVIII-12-3 Et H H CH(CH3) 2 Et H H F OH XXVIII-12-4 Et H H CH2CH(CH3)2 Et H H F OH XXVIII-12-5 Et H H CH 2Ph Et H H F OH XXVIII-12-6 Et H H CH 2-indol-3-yl Et H H F OH XXVIII-12-7 Et H H CH2CH 2SCH 3 Et H H F OH XXVIII-12-8 Et * H * Et H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-13. N9 R1 R2 R3 a R3b R4 R5 R6 X Y XXVIII-13-1 'Pr H H H Et H H F OH XXVIII-13-2 'Pr H H CH 3 Et H H F OH XXVIII-13-3 'Pr H H CH(CH3) 2 Et H H F OH XXVIII-13-4 'Pr H H CH 2CH(CH3) 2 Et H H F OH XXVIII-13-5 Pr H H CH 2Ph Et H H F OH XXVIII-13-6 Pr H H CH 2-indol-3-yl Et H H F OH XXVIII-13-7 Pr H H CH 2CH 2SCH 3 Et H H F OH XXVIII-13-8 Pr * H * Et H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-14. No R1 R2 R3 a R3b R4 R' R' X Y XXVIII-14-1 'Bu H H H Et H H F OH XXVIII-14-2 'Bu H H CH 3 Et H H F OH XXVIII-14-3 'Bu H H CH(CH 3) 2 Et H H F OH XXVIII-14-4 'Bu H H CH 2CH(CH 3) 2 Et H H F OH XXVIII-14-5 'Bu H H CH 2Ph Et H H F OH XXVIII-14-6 'Bu H H CH 2-indol-3-yl Et H H F OH XXVIII-14-7 'Bu H H CH 2CH 2SCH 3 Et H H F OH XXVIII-14-8 'Bu * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-15. No R1 R2 R3 a R3 b R 5 R6 X Y XXVIII-15-1 Ph H H H Et H H F OH XXVIII-15-2 Ph H H CH 3 Et H H F OH XXVIII-15-3 Ph H H CH(CH 3) 2 Et H H F OH XXVIII-15-4 Ph H H CH 2CH(CH 3) 2 Et H H F OH XXVIII-15-5 Ph H H CH 2Ph Et H H F OH XXVIII-15-6 Ph H H CH 2-indol-3-yl Et H H F OH XXVIII-15-7 Ph H H CH 2CH 2SCH 3 Et H H F OH XXVIII-15-8 Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-16. No R R2 R 3 a R3b R4 R5 R6 X Y XXVIII-16-1 p-Me-Ph H H H Et H H F OH XXVIII-16-2 p-Me-Ph H H CH 3 Et H H F OH XXVIII-16-3 p-Me-Ph H H CH(CH 3) 2 Et H H F OH XXVIII-16-4 p-Me-Ph H H CH 2CH(CH 3) 2 Et H H F OH XXVIII-16-5 p-Me-Ph H H CH 2Ph Et H H F OH XXVIII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H H F OH XXVIII-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H H F OH XXVIII-16-8 p-Me-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-17. No R RRaR 3 b R4 R R' X Y XXVIII-17-1 p-F-Ph H H H Et H H F OH XXVIII-17-2 p-F-Ph H H CH 3 Et H H F OH XXVIII-17-3 p-F-Ph H H CH(CH3) 2 Et H H F OH XXVIII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et H H F OH XXVIII-17-5 p-F-Ph H H CH 2Ph Et H H F OH XXVIII-17-6 p-F-Ph H H CH 2-indol-3-yl Et H H F OH XXVIII-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H H F OH XXVIII-17-8 p-F-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-18. 2 R3a3b Nt R R R R4 R R X Y

XXVIII-18-1 p-Cl-Ph H H H Et H H F OH XXVIII-18-2 p-Cl-Ph H H CH 3 Et H H F OH XXVIII-18-3 p-Cl-Ph H H CH(CH3) 2 Et H H F OH XXVIII-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et H H F OH XXVIII-18-5 p-Cl-Ph H H CH 2Ph Et H H F OH XXVIII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H H F OH XXVIII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H H F OH XXVIII-18-8 p-Cl-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-19. No RI 1 R2 R3 a R3 b R4 R5 R 6 X Y

XXVIII-19-1 p-Br-Ph H H H Et H H F OH XXVIII-19-2 p-Br-Ph H H CH 3 Et H H F OH XXVIII-19-3 p-Br-Ph H H CH(CH3) 2 Et H H F OH XXVIII-19-4 p-Br-Ph H H CH 2CH(CH3)2 Et H H F OH XXVIII-19-5 p-Br-Ph H H CH 2Ph Et H H F OH XXVIII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H H F OH XXVIII-19-7 p-Br-Ph H H CH 2CH 2SCH3 Et H H F OH XXVIII-19-8 p-Br-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

22-IS

Table XXVIII-20. No R R2 R3 a R3b R4 R R X Y XXVIII-20-1 p-I-Ph H H H Et H H F OH XXVIII-20-2 p-I-Ph H H CH 3 Et H H F OH XXVIII-20-3 p-I-Ph H H CH(CH3) 2 Et H H F OH XXVIII-20-4 p-I-Ph H H CH 2CH(CH 3) 2 Et H H F OH XXVIII-20-5 p-I-Ph H H CH 2Ph Et H H F OH XXVIII-20-6 p-I-Ph H H CH 2-indol-3-yl Et H H F OH XXVIII-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H H F OH XXVIII-20-8 p-I-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-21. N9 R1 R2 R3 a R3 b R4 R' R6 X Y XXVIII-21-1 CH3 H H H 'Pr H H F OH XXVIII-21-2 CH3 H H CH3 'Pr H H F OH XXVIII-21-3 CH 3 H H CH(CH 3) 2 'Pr H H F OH XXVIII-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H H F OH XXVIII-21-5 CH 3 H H CH 2Ph 'Pr H H F OH XXVIII-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H H F OH XXVIII-21-8 CH 3 * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-22. No Rl R2 R3 a R3b R4 R 5 R6 X Y XXVIII-22-1 Et H H H 'Pr H H F OH XXVIII-22-2 Et H H CH3 'Pr H H F OH XXVIII-22-3 Et H H CH(CH3) 2 'Pr H H F OH XXVIII-22-4 Et H H CH2CH(CH 3) 2 'Pr H H F OH XXVIII-22-5 Et H H CH 2Ph 'Pr H H F OH XXVIII-22-6 Et H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-22-7 Et H H CH2CH 2SCH 3 'Pr H H F OH XXVIII-22-8 Et * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 0 _

Table XXVIII-23. No R1 R2 R3 a R3b R4 R 5 R6 X Y XXVIII-23-1 'Pr H H H 'Pr H H F OH XXVIII-23-2 'Pr H H CH 3 'Pr H H F OH XXVIII-23-3 'Pr H H CH(CH3) 2 'Pr H H F OH XXVIII-23-4 Pr H H CH 2CH(CH3) 2 'Pr H H F OH XXVIII-23-5 Pr H H CH 2Ph 'Pr H H F OH XXVIII-23-6 Pr H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-23-7 Pr H H CH 2CH 2SCH 3 'Pr H H F OH XXVIII-23-8 Pr * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-24. No R1 R2 R 3a R3 b R4 R 5 R6 X Y XXVIII-24-1 'Bu H H H 'Pr H H F OH XXVIII-24-2 'Bu H H CH 3 'Pr H H F OH XXVIII-24-3 'Bu H H CH(CH3) 2 'Pr H H F OH XXVIII-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H H F OH XXVIII-24-5 'Bu H H CH 2Ph 'Pr H H F OH XXVIII-24-6 'Bu H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H H F OH XXVIII-24-8 'Bu * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-25. RI No R2 R3 a R3b R4 R6 X Y

XXVIII-25-1 Ph H H H 'Pr H H F OH XXVIII-25-2 Ph H H CH 3 'Pr H H F OH XXVIII-25-3 Ph H H CH(CH3) 2 'Pr H H F OH XXVIII-25-4 Ph H H CH 2CH(CH3) 2 'Pr H H F OH XXVIII-25-5 Ph H H CH 2Ph 'Pr H H F OH XXVIII-25-6 Ph H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-25-7 Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXVIII-25-8 Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-26. No R R2 R3 a R3b R4 R R6 X Y XXVIII-26-1 p-Me-Ph H H H 'Pr H H F OH XXVIII-26-2 p-Me-Ph H H CH 3 'Pr H H F OH XXVIII-26-3 p-Me-Ph H H CH(CH 3) 2 'Pr H H F OH XXVIII-26-4 p-Me-Ph H H CH 2CH(CH 3) 2 'Pr H H F OH XXVIII-26-5 p-Me-Ph H H CH 2Ph 'Pr H H F OH XXVIII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-26-7 p-Me-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXVIII-26-8 p-Me-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-27. 6 No R1 R2 R 3aRSb R4 R R X Y XXVIII-27-1 p-F-Ph H H H 'Pr H H F OH XXVIII-27-2 p-F-Ph H H CH 3 'Pr H H F OH XXVIII-27-3 p-F-Ph H H CH(CH 3)2 'Pr H H F OH XXVIII-27-4 p-F-Ph H H CH 2CH(CH 3)2 'Pr H H F OH XXVIII-27-5 p-F-Ph H H CH 2Ph 'Pr H H F OH XXVIII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-27-7 p-F-Ph H H CH 2CH2SCH 3 'Pr H H F OH XXVIII-27-8 p-F-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-28. No R R 2 R 3 a R3b R4 R5 R6 X Y XXVIII-28-1 p-Cl-Ph H H H 'Pr H H F OH XXVIII-28-2 p-Cl-Ph H H CH3 'Pr H H F OH XXVIII-28-3 p-Cl-Ph H H CH(CH 3)2 'Pr H H F OH XXVIII-28-4 p-Cl-Ph H H CH2CH(CH 3) 2 'Pr H H F OH XXVIII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H H F OH XXVIII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-28-7 p-Cl-Ph H H CH2CH 2SCH 3 'Pr H H F OH XXVIII-28-8 p-Cl-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_, A/1_

Table XXVIII-29. No R RR 3 a R 3b R4 R' R' X Y XXVIII-29-1 p-Br-Ph H H H 'Pr H H F OH XXVIII-29-2 p-Br-Ph H H CH 3 'Pr H H F OH XXVIII-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H H F OH XXVIII-29-4 p-Br-Ph H H CH 2CH(CH3)2 'Pr H H F OH XXVIII-29-5 p-Br-Ph H H CH 2Ph 'Pr H H F OH XXVIII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-29-7 p-Br-Ph H H CH 2CH 2SCH3 'Pr H H F OH XXVIII-29-8 p-Br-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-30. No R1 R2 R3 a R3 b R4 R R6 X Y XXVIII-30-1 p-I-Ph H H H 'Pr H H F OH XXVIII-30-2 p-I-Ph H H CH 3 'Pr H H F OH XXVIII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H H F OH XXVIII-30-4 p-I-Ph H H CH 2CH(CH3) 2 'Pr H H F OH XXVIII-30-5 p-I-Ph H H CH 2Ph 'Pr H H F OH XXVIII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXVIII-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXVIII-30-8 p-I-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-31. No R1 R2 R3 a R3b R4 R5 R6 X Y XXVIII-31-1 CH3 H H H "Bu H H F OH XXVIII-31-2 CH3 H H CH3 "Bu H H F OH XXVIII-31-3 CH3 H H CH(CH3)2 "Bu H H F OH XXVIII-31-4 CH3 H H CH2CH(CH3) 2 "Bu H H F OH XXVIII-31-5 CH3 H H CH 2Ph "Bu H H F OH XXVIII-31-6 CH3 H H CH 2-indol-3-yl "Bu H H F OH XXVIII-31-7 CH3 H H CH2CH 2SCH 3 "Bu H H F OH XXVIII-31-8 CH3 * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-32. No Rl R2 R3 a R3b R4 R' R' X Y XXVIII-32-1 Et H H H "Bu H H F OH XXVIII-32-2 Et H H CH3 "Bu H H F OH XXVIII-32-3 Et H H CH(CH3) 2 "Bu H H F OH XXVIII-32-4 Et H H CH2CH(CH3)2 "Bu H H F OH XXVIII-32-5 Et H H CH 2Ph "Bu H H F OH XXVIII-32-6 Et H H CH 2-indol-3-yl "Bu H H F OH XXVIII-32-7 Et H H CH2CH 2SCH 3 "Bu H H F OH XXVIII-32-8 Et * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-33. 5 No R1 R2 R3 a R3 b R4 R R6 X Y XXVIII-33-1 'Pr H H H "Bu H H F OH XXVIII-33-2 'Pr H H CH 3 "Bu H H F OH XXVIII-33-3 'Pr H H CH(CH3) 2 "Bu H H F OH XXVIII-33-4 'Pr H H CH 2CH(CH3) 2 "Bu H H F OH XXVIII-33-5 'Pr H H CH 2Ph "Bu H H F OH XXVIII-33-6 'Pr H H CH 2-indol-3-yl "Bu H H F OH XXVIII-33-7 'Pr H H CH 2CH 2SCH 3 "Bu H H F OH XXVIII-33-8 'Pr * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-34. No R1 R2 R 3a R3b R4 R R 6 X Y XXVIII-34-1 'Bu H H H "Bu H H F OH XXVIII-34-2 'Bu H H CH 3 "Bu H H F OH XXVIII-34-3 'Bu H H CH(CH3) 2 "Bu H H F OH XXVIII-34-4 'Bu H H CH 2CH(CH3) 2 "Bu H H F OH XXVIII-34-5 'Bu H H CH 2Ph "Bu H H F OH XXVIII-34-6 'Bu H H CH 2-indol-3-yl "Bu H H F OH XXVIII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H H F OH XXVIII-34-8 'Bu * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

rA2-

Table XXVIII-35. RI No R2 R3 aR3 b R4 R R X Y XXVIII-35-1 Ph H H H "Bu H H F OH XXVIII-35-2 Ph H H CH 3 "Bu H H F OH XXVIII-35-3 Ph H H CH(CH3) 2 "Bu H H F OH XXVIII-35-4 Ph H H CH 2CH(CH3)2 "Bu H H F OH XXVIII-35-5 Ph H H CH 2Ph "Bu H H F OH XXVIII-35-6 Ph H H CH 2-indol-3-yl "Bu H H F OH XXVIII-35-7 Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXVIII-35-8 Ph * H * "Bu H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-36. NI R R2 R3a R3 56 R4 RR X Y XXVIII-36-1 p-Me-Ph H H H "Bu H H F OH XXVIII-36-2 p-Me-Ph H H CH 3 "Bu H H F OH XXVIII-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H H F OH XXVIII-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H H F OH XXVIII-36-5 p-Me-Ph H H CH 2Ph "Bu H H F OH XXVIII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H H F OH XXVIII-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXVIII-36-8 p-Me-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXVIII-37. No RI 1 R2 R 3a R3b 4 R 5 R6 X Y XXVIII-37-1 p-F-Ph H H H "Bu H H F OH XXVIII-37-2 p-F-Ph H H CH 3 "Bu H H F OH XXVIII-37-3 p-F-Ph H H CH(CH3) 2 "Bu H H F OH XXVIII-37-4 p-F-Ph H H CH 2CH(CH3)2 "Bu H H F OH XXVIII-37-5 p-F-Ph H H CH 2Ph "Bu H H F OH XXVIII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H H F OH XXVIII-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXVIII-37-8 p-F-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

rAA-

Table XXVIII-38. No R R2 R 3 a R3b R4 R' R6 X Y XXVIII-38-1 p-Cl-Ph H H H "Bu H H F OH XXVIII-38-2 p-Cl-Ph H H CH3 "Bu H H F OH XXVIII-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H H F OH XXVIII-38-4 p-Cl-Ph H H CH2CH(CH3) 2 "Bu H H F OH XXVIII-38-5 p-Cl-Ph H H CH 2Ph "Bu H H F OH XXVIII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H H F OH XXVIII-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH XXVIII-38-8 p-Cl-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-39. N9 R R2 R3a R3b R4 R' R6 X Y XXVIII-39-1 p-Br-Ph H H H "Bu H H F OH XXVIII-39-2 p-Br-Ph H H CH 3 "Bu H H F OH XXVIII-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H H F OH XXVIII-39-4 p-Br-Ph H H CH 2CH(CH3)2 "Bu H H F OH XXVIII-39-5 p-Br-Ph H H CH 2Ph "Bu H H F OH XXVIII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H H F OH XXVIII-39-7 p-Br-Ph H H CH 2CH 2 SCH3 "Bu H H F OH XXVIII-39-8 p-Br-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-40. No R1 R2 R3 a R3b R4 RR X Y XXVIII-40-1 p-I-Ph H H H "Bu H H F OH XXVIII-40-2 p-I-Ph H H CH 3 "Bu H H F OH XXVIII-40-3 p-I-Ph H H CH(CH3) 2 "Bu H H F OH XXVIII-40-4 p-I-Ph H H CH 2CH(CH 3) 2 "Bu H H F OH XXVIII-40-5 p-I-Ph H H CH 2Ph "Bu H H F OH XXVIII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H H F OH XXVIII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXVIII-40-8 p-I-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-41. No R1 R2 R3 a R3b R4 R 5 R' X Y XXVIII-41-1 CH3 H H H Bz H H F OH XXVIII-41-2 CH3 H H CH3 Bz H H F OH XXVIII-41-3 CH3 H H CH(CH3)2 Bz H H F OH XXVIII-41-4 CH3 H H CH2CH(CH3) 2 Bz H H F OH XXVIII-41-5 CH3 H H CH 2Ph Bz H H F OH XXVIII-41-6 CH3 H H CH 2-indol-3-yl Bz H H F OH XXVIII-41-7 CH3 H H CH2CH 2SCH 3 Bz H H F OH XXVIII-41-8 CH3 * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-42. No R1 R2 R3a R3 b R4 R 5 R6 X Y XXVIII-42-1 Et H H H Bz H H F OH XXVIII-42-2 Et H H CH3 Bz H H F OH XXVIII-42-3 Et H H CH(CH3) 2 Bz H H F OH XXVIII-42-4 Et H H CH2CH(CH3)2 Bz H H F OH XXVIII-42-5 Et H H CH 2Ph Bz H H F OH XXVIII-42-6 Et H H CH 2-indol-3-yl Bz H H F OH XXVIII-42-7 Et H H CH2CH 2SCH 3 Bz H H F OH XXVIII-42-8 Et * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-43. No R1 R2 R3 a R3 b R4 R 5 R6 X Y XXVIII-43-1 'Pr H H H Bz H H F OH XXVIII-43-2 Pr H H CH 3 Bz H H F OH XXVIII-43-3 Pr H H CH(CH3) 2 Bz H H F OH XXVIII-43-4 Pr H H CH 2CH(CH3) 2 Bz H H F OH XXVIII-43-5 Pr H H CH 2Ph Bz H H F OH XXVIII-43-6 'Pr H H CH 2-indol-3-yl Bz H H F OH XXVIII-43-7 'Pr H H CH 2CH 2SCH 3 Bz H H F dAI XXVIII-43-8 'Pr * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-44. No R1 R2 R 3a R3b R4 R' R' X Y XXVIII-44-1 'Bu H H H Bz H H F OH XXVIII-44-2 'Bu H H CH 3 Bz H H F OH XXVIII-44-3 'Bu H H CH(CH3) 2 Bz H H F OH XXVIII-44-4 'Bu H H CH 2CH(CH3) 2 Bz H H F OH XXVIII-44-5 'Bu H H CH 2Ph Bz H H F OH XXVIII-44-6 'Bu H H CH 2-indol-3-yl Bz H H F OH XXVIII-44-7 'Bu H H CH 2CH 2SCH 3 Bz H H F OH XXVIII-44-8 'Bu * H * Bz H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-45. No R1 R2 R3 a R3 b R4 R 5 R6 X Y

XXVIII-45-1 Ph H H H Bz H H F OH XXVIII-45-2 Ph H H CH 3 Bz H H F OH XXVIII-45-3 Ph H H CH(CH3) 2 Bz H H F OH XXVIII-45-4 Ph H H CH 2CH(CH3)2 Bz H H F OH XXVIII-45-5 Ph H H CH 2Ph Bz H H F OH XXVIII-45-6 Ph H H CH 2-indol-3-yl Bz H H F OH XXVIII-45-7 Ph H H CH 2CH 2SCH 3 Bz H H F OH XXVIII-45-8 Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-46. No RI 1 R2 R3 a R3b 4 R 5 R6 X Y

XXVIII-46-1 p-Me-Ph H H H Bz H H F OH XXVIII-46-2 p-Me-Ph H H CH 3 Bz H H F OH XXVIII-46-3 p-Me-Ph H H CH(CH 3)2 Bz H H F OH XXVIII-46-4 p-Me-Ph H H CH 2CH(CH 3) 2 Bz H H F OH XXVIII-46-5 p-Me-Ph H H CH 2Ph Bz H H F OH XXVIII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H H F OH XXVIII-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXVIII-46-8 p-Me-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-47. No R1 R2 R3 a R3 b R4 R R X Y XXVIII-47-1 p-F-Ph H H H Bz H H F OH XXVIII-47-2 p-F-Ph H H CH 3 Bz H H F OH XXVIII-47-3 p-F-Ph H H CH(CH3) 2 Bz H H F OH XXVIII-47-4 p-F-Ph H H CH 2CH(CH3)2 Bz H H F OH XXVIII-47-5 p-F-Ph H H CH 2Ph Bz H H F OH XXVIII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H H F OH XXVIII-47-7 p-F-Ph H H CH 2 CH 2 SCH 3 Bz H H F OH XXVIII-47-8 p-F-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXVIII-48. 2 R3a3b Nt R R R R4 R' R6 X Y

XXVIII-48-1 p-Cl-Ph H H H Bz H H F OH XXVIII-48-2 p-Cl-Ph H H CH3 Bz H H F OH XXVIII-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H H F OH XXVIII-48-4 p-Cl-Ph H H CH2CH(CH 3)2 Bz H H F OH XXVIII-48-5 p-Cl-Ph H H CH 2Ph Bz H H F OH XXVIII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H H F OH XXVIII-48-7 p-Cl-Ph H H CH2CH 2SCH 3 Bz H H F OH XXVIII-48-8 p-Cl-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXVIII-49. No RI 1 R2 R3 a R3 b R4 R5 R6 X Y

XXVIII-49-1 p-Br-Ph H H H Bz H H F OH XXVIII-49-2 p-Br-Ph H H CH 3 Bz H H F OH XXVIII-49-3 p-Br-Ph H H CH(CH3) 2 Bz H H F OH XXVIII-49-4 p-Br-Ph H H CH 2CH(CH3)2 Bz H H F OH XXVIII-49-5 p-Br-Ph H H CH 2Ph Bz H H F OH XXVIII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H H F OH XXVIII-49-7 p-Br-Ph H H CH 2CH 2SCH3 Bz H H F OH XXVIII-49-8 p-Br-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rA2-

Table XXVIII-50. No R R2 RaR 3 b 4 R5 R6 X Y XXVIII-50-1 p-I-Ph H H H Bz H H F OH XXVIII-50-2 p-I-Ph H H CH 3 Bz H H F OH XXVIII-50-3 p-I-Ph H H CH(CH 3) 2 Bz H H F OH XXVIII-50-4 p-I-Ph H H CH 2CH(CH 3) 2 Bz H H F OH XXVIII-50-5 p-I-Ph H H CH 2Ph Bz H H F OH XXVIII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H H F OH XXVIII-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXVIII-50-8 p-I-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

0 N

R3b R2 O NH

R3a N P 0 0 N N---- -O \ OJ

C0 2 R4 OR' Rs R6 NH 2

Y X XXIX

Table XXIX-1. No R1 R2 R3 aRb R4 R5 R6 X Y

XXIX-1-1 CH3 H H H CH 3 H CH 3 F OH XXIX-1-2 CH3 H H CH 3 CH 3 H CH 3 F OH XXIX-1-3 CH3 H H CH(CH 3) 2 CH 3 H CH 3 F OH XXIX-1-4 CH3 H H CH 2CH(CH3) 2 CH 3 H CH 3 F OH XXIX-1-5 CH3 H H CH 2Ph CH 3 H CH 3 F OH XXIX-1-6 CH3 H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXIX-1-7 CH3 H H CH 2CH 2SCH 3 CH 3 H CH 3 F OH XXIX-1-8 CH3 * H * CH 3 H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ A _

Table XXIX-2. No Rl R 2 R3 a R 3b R4 R 5 R' X Y XXIX-2-1 Et H H H CH3 H CH 3 F OH XXIX-2-2 Et H H CH 3 CH 3 H CH 3 F OH XXIX-2-3 Et H H CH(CH3) 2 CH3 H CH 3 F OH XXIX-2-4 Et H H CH 2CH(CH3) 2 CH3 H CH 3 F OH XXIX-2-5 Et H H CH 2Ph CH3 H CH 3 F OH XXIX-2-6 Et H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXIX-2-7 Et H H CH 2CH 2SCH3 CH3 H CH 3 F OH XXIX-2-8 Et * H * CH 3 H CH 3 F OH *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-3. No R1 R2 R3 a R3 b R4 R' R6 X Y XXIX-3-1 'Pr H H H CH 3 H CH 3 F OH XXIX-3-2 'Pr H H CH 3 CH3 H CH 3 F OH XXIX-3-3 'Pr H H CH(CH3) 2 CH3 H CH 3 F OH XXIX-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H CH 3 F OH XXIX-3-5 'Pr H H CH 2Ph CH 3 H CH 3 F OH XXIX-3-6 'Pr H H CH 2-indol-3-yl CH3 H CH 3 F OH XXIX-3-7 'Pr H H CH 2CH2SCH 3 CH3 H CH 3 F OH XXIX-3-8 'Pr * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-4. No R1 R2 R 3a R3b R4 R5 R6 X Y

XXIX-4-1 'Bu H H H CH 3 H CH 3 F OH XXIX-4-2 'Bu H H CH 3 CH 3 H CH 3 F OH XXIX-4-3 'Bu H H CH(CH3) 2 CH 3 H CH 3 F OH XXIX-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H CH 3 F OH XXIX-4-5 'Bu H H CH 2Ph CH 3 H CH 3 F OH XXIX-4-6 'Bu H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXIX-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H CH 3 F OH XXIX-4-8 'Bu * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-5. No R1 R2 R3 a R 3b R4 RR6 X Y XXIX-5-1 Ph H H H CH 3 H CH 3 F OH XXIX-5-2 Ph H H CH3 CH3 H CH 3 F OH XXIX-5-3 Ph H H CH(CH3)2 CH3 H CH 3 F OH XXIX-5-4 Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXIX-5-5 Ph H H CH 2Ph CH 3 H CH 3 F OH XXIX-5-6 Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXIX-5-7 Ph H H CH2CH2 SCH3 CH3 H CH 3 F OH XXIX-5-8 Ph * H * CH3 H CH 3 F OH *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-6. N9 R1 R2 R3 a R3 b R4 RR6 X Y XXIX-6-1 p-Me-Ph H H H CH 3 H CH 3 F OH XXIX-6-2 p-Me-Ph H H CH3 CH3 H CH 3 F OH XXIX-6-3 p-Me-Ph H H CH(CH3)2 CH3 H CH 3 F OH XXIX-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXIX-6-5 p-Me-Ph H H CH 2Ph CH 3 H CH 3 F OH XXIX-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXIX-6-7 p-Me-Ph H H CH2CH2 SCH3 CH3 H CH 3 F OH XXIX-6-8 p-Me-Ph * H * CH3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-7. No R R2 R 3 a R3b R4 RR6 X Y XXIX-7-1 p-F-Ph H H H CH 3 H CH 3 F OH XXIX-7-2 p-F-Ph H H CH3 CH3 H CH 3 F OH XXIX-7-3 p-F-Ph H H CH(CH3)2 CH3 H CH 3 F OH XXIX-7-4 p-F-Ph H H CH2CH(CH 3) 2 CH3 H CH 3 F OH XXIX-7-6 p-F-Ph H H CH 2Ph CH 3 H CH 3 F OH XXIX-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXIX-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXIX-7-20 p-F-Ph * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-8. R R2 R3 a R3b R4 R R X Y No XXIX-8-1 p-Cl-Ph H H H CH 3 H CH 3 F OH XXIX-8-2 p-Cl-Ph H H CH 3 CH 3 H CH 3 F OH XXIX-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H CH 3 F OH XXIX-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H CH 3 F OH XXIX-8-5 p-Cl-Ph H H CH 2Ph CH 3 H CH 3 F OH XXIX-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXIX-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H CH 3 F OH XXIX-8-8 p-Cl-Ph * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-9. N9 R1 R2 R 3a R3 b R4 R 5 R6 X Y

XXIX-9-1 p-Br-Ph H H H CH3 H CH 3 F OH XXIX-9-2 p-Br-Ph H H CH3 CH3 H CH 3 F OH XXIX-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H CH 3 F OH XXIX-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH3 H CH 3 F OH XXIX-9-6 p-Br-Ph H H CH 2Ph CH3 H CH 3 F OH XXIX-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H CH 3 F OH XXIX-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 H CH 3 F OH XXIX-9-20 p-Br-Ph * H * CH3 H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-10. No R R2 R 3 a R3b R4 R5 R6 X Y

XXIX-10-1 p-I-Ph H H H CH 3 H CH 3 F OH XXIX-10-2 p-I-Ph H H CH3 CH 3 H CH 3 F OH XXIX-10-3 p-I-Ph H H CH(CH3)2 CH 3 H CH 3 F OH XXIX-10-4 p-I-Ph H H CH2CH(CH3) 2 CH 3 H CH 3 F OH XXIX-10-5 p-I-Ph H H CH 2Ph CH 3 H CH 3 F OH XXIX-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H CH 3 F OH XXIX-10-7 p-I-Ph H H CH2CH 2SCH 3 CH 3 H CH 3 F OH XXIX-10-8 p-I-Ph * H * CH 3 H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-11. No R1 R2 R 3a R3b R4 R5 R6 X Y XXIX-11-1 CH 3 H H H Et H CH 3 F OH XXIX-11-2 CH 3 H H CH3 Et H CH 3 F OH XXIX-11-3 CH 3 H H CH(CH3) 2 Et H CH 3 F OH XXIX-11-4 CH 3 H H CH2CH(CH3) 2 Et H CH 3 F OH XXIX-11-5 CH 3 H H CH 2Ph Et H CH 3 F OH XXIX-11-6 CH 3 H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-11-7 CH 3 H H CH2CH 2SCH 3 Et H CH 3 F OH XXIX-11-8 CH 3 * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-12. No R1 R2 R3a R3b R4 R5 R6 X Y XXIX-12-1 Et H H H Et H CH 3 F OH XXIX-12-2 Et H H CH 3 Et H CH 3 F OH XXIX-12-3 Et H H CH(CH3) 2 Et H CH 3 F OH XXIX-12-4 Et H H CH 2CH(CH3) 2 Et H CH 3 F OH XXIX-12-5 Et H H CH 2Ph Et H CH 3 F OH XXIX-12-6 Et H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-12-7 Et H H CH 2CH 2SCH 3 Et H CH 3 F OH XXIX-12-8 Et * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-13. N R1 R2 R 3a R 3b R4 R5 R6 X Y

XXIX-13-1 'Pr H H H Et H CH 3 F OH XXIX-13-2 'Pr H H CH 3 Et H CH 3 F OH XXIX-13-3 'Pr H H CH(CH3) 2 Et H CH 3 F OH XXIX-13-4 'Pr H H CH 2CH(CH3)2 Et H CH 3 F OH XXIX-13-5 Pr H H CH 2Ph Et H CH 3 F OH XXIX-13-6 Pr H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-13-7 Pr H H CH 2CH 2SCH 3 Et H CH 3 F OH XXIX-13-8 Pr * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-14. No R1 R2 R3 a R3b R4 R' R6 X Y XXIX-14-1 'Bu H H H Et H CH 3 F OH XXIX-14-2 'Bu H H CH 3 Et H CH 3 F OH XXIX-14-3 'Bu H H CH(CH3) 2 Et H CH 3 F OH XXIX-14-4 'Bu H H CH 2CH(CH 3) Et H CH 3 F OH 2

XXIX-14-5 'Bu H H CH 2Ph Et H CH 3 F OH XXIX-14-6 'Bu H H CH 2-indol-3- Et H CH 3 F OH y1 XXIX-14-7 'Bu H H CH 2CH2SCH Et H CH 3 F OH 3

XXIX-14-8 'Bu * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-15. No RI 1 R2 R 3a R3 b R4 R5 R6 X Y XXIX-15-1 Ph H H H Et H CH 3 F OH XXIX-15-2 Ph H H CH3 Et H CH 3 F OH XXIX-15-3 Ph H H CH(CH 3)2 Et H CH 3 F OH XXIX-15-4 Ph H H CH2CH(CH3) 2 Et H CH 3 F OH XXIX-15-5 Ph H H CH 2Ph Et H CH 3 F OH XXIX-15-6 Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-15-7 Ph H H CH2CH 2SCH 3 Et H CH 3 F OH XXIX-15-8 Ph * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-16. No RI 1 R2 R 3a R3 b R4 R5 R6 X Y XXIX-16-1 p-Me-Ph H H H Et H CH 3 F OH XXIX-16-2 p-Me-Ph H H CH3 Et H CH 3 F OH XXIX-16-3 p-Me-Ph H H CH(CH3)2 Et H CH 3 F OH XXIX-16-4 p-Me-Ph H H CH2CH(CH3) 2 Et H CH 3 F OH XXIX-16-5 p-Me-Ph H H CH 2Ph Et H CH 3 F OH XXIX-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH XXIX-16-8 p-Me-Ph * H * Et H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-17. R I R2 R3 a R3 b R4 R5 R6 X Y

No R RR 3 a R3 b R4 R' R6 X Y XXIX-17-1 p-F-Ph H H H Et H CH 3 F OH XXIX-17-2 p-F-Ph H H CH 3 Et H CH 3 F OH XXIX-17-3 p-F-Ph H H CH(CH3)2 Et H CH 3 F OH XXIX-17-4 p-F-Ph H H CH 2CH(CH 3) 2 Et H CH 3 F OH XXIX-17-5 p-F-Ph H H CH 2Ph Et H CH 3 F OH XXIX-17-6 p-F-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH XXIX-17-8 p-F-Ph * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-18. N9 Rl R2 R3a R 3b R4 R R6 X Y XXIX-18-1 p-Cl-Ph H H H Et H CH 3 F OH XXIX-18-2 p-Cl-Ph H H CH3 Et H CH 3 F OH XXIX-18-3 p-Cl-Ph H H CH(CH3)2 Et H CH 3 F OH XXIX-18-4 p-Cl-Ph H H CH2CH(CH 3) 2 Et H CH 3 F OH XXIX-18-5 p-Cl-Ph H H CH2Ph Et H CH 3 F OH XXIX-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H CH 3 F OH XXIX-18-7 p-Cl-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH XXIX-18-8 p-Cl-Ph * H * Et H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-19. No R R2 R 3 a R3 b R4 R R6 X Y XXIX-19-1 p-Br-Ph H H H Et H CH 3 F OH XXIX-19-2 p-Br-Ph H H CH 3 Et H CH 3 F OH XXIX-19-3 p-Br-Ph H H CH(CH3) 2 Et H CH 3 F OH XXIX-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et H CH 3 F OH XXIX-19-5 p-Br-Ph H H CH 2Ph Et H CH 3 F OH XXIX-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H CH 3 F OH XXIX-19-8 p-Br-Ph * H * Et H CH 3 F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-20. No R RR 3 a R3b R4 R' R6 X Y XXIX-20-1 p-I-Ph H H H Et H CH 3 F OH XXIX-20-2 p-I-Ph H H CH3 Et H CH 3 F OH XXIX-20-3 p-I-Ph H H CH(CH3)2 Et H CH 3 F OH XXIX-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H CH 3 F OH XXIX-20-5 p-I-Ph H H CH 2Ph Et H CH 3 F OH XXIX-20-6 p-I-Ph H H CH 2-indol-3-yl Et H CH 3 F OH XXIX-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H CH 3 F OH XXIX-20-8 p-I-Ph * H * Et H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-21. No R1 R2 R 3a R3 b R4 R 5 R6 X Y XXIX-21-1 CH 3 H H H 'Pr H CH3 F OH XXIX-21-2 CH 3 H H CH3 'Pr H CH 3 F OH XXIX-21-3 CH3 H H CH(CH3) 2 'Pr H CH 3 F OH XXIX-21-4 CH3 H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXIX-21-5 CH3 H H CH 2Ph 'Pr H CH 3 F OH XXIX-21-6 CH3 H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXIX-21-7 CH3 H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXIX-21-8 CH3 * H * 'Pr H CH 3 F OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-22. No Rl R2 R 3a R3b R4 R5 R6 X Y

XXIX-22-1 Et H H H 'Pr H CH 3 F OH XXIX-22-2 Et H H CH 3 'Pr H CH 3 F OH XXIX-22-3 Et H H CH(CH3) 2 'Pr H CH 3 F OH XXIX-22-4 Et H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXIX-22-5 Et H H CH 2Ph 'Pr H CH 3 F OH XXIX-22-6 Et H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXIX-22-7 Et H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXIX-22-8 Et * H * 'Pr H CH 3 F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-23. R1 R2 R 3a R3 R4 R R' X Y No XXIX-23-1 'Pr H H H 'Pr H CH 3 F OH XXIX-23-2 'Pr H H CH 3 'Pr H CH 3 F OH XXIX-23-3 'Pr H H CH(CH3) 2 'Pr H CH 3 F OH XXIX-23-4 Pr H H CH 2CH(CH 3)2 'Pr H CH 3 F OH XXIX-23-5 Pr H H CH 2Ph 'Pr H CH 3 F OH XXIX-23-6 Pr H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXIX-23-7 Pr H H CH 2CH2SCH 3 'Pr H CH 3 F OH XXIX-23-8 Pr * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-24. No R1 R2 R3 a Rb R4 R 5 R6 X Y

XXIX-24-1 'Bu H H H 'Pr H CH 3 F OH XXIX-24-2 'Bu H H CH 3 'Pr H CH 3 F OH XXIX-24-3 'Bu H H CH(CH3) 2 'Pr H CH 3 F OH XXIX-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H CH 3 F OH XXIX-24-5 'Bu H H CH 2Ph 'Pr H CH 3 F OH XXIX-24-6 'Bu H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXIX-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H CH 3 F OH XXIX-24-8 'Bu * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-25. No R1 R2 R 3a R3b R4 R5 R6 X Y

XXIX-25-1 Ph H H H Pr H CH3 F OH XXIX-25-2 Ph H H CH3 'Pr H CH3 F OH XXIX-25-3 Ph H H CH(CH 3)2 'Pr H CH3 F OH XXIX-25-4 Ph H H CH2CH(CH3) 2 'Pr H CH3 F OH XXIX-25-5 Ph H H CH 2Ph 'Pr H CH3 F OH XXIX-25-6 Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH XXIX-25-7 Ph H H CH2CH 2SCH 3 'Pr H CH3 F OH XXIX-25-8 Ph * H * 'Pr H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-26. No R RR 3 a R3b R4 R' R6 X Y

XXIX-26-1 p-Me-Ph H H H 'Pr H CH3 F OH XXIX-26-2 p-Me-Ph H H CH3 'Pr H CH3 F OH XXIX-26-3 p-Me-Ph H H CH(CH3)2 'Pr H CH3 F OH XXIX-26-4 p-Me-Ph H H CH2CH(CH3) 2 'Pr H CH3 F OH XXIX-26-5 p-Me-Ph H H CH 2Ph 'Pr H CH3 F OH XXIX-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH XXIX-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H CH3 F OH XXIX-26-8 p-Me-Ph * H * 'Pr H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-27. 9 R1 R2 R3 a R3 b R4 R' R6 X Y

XXIX-27-1 p-F-Ph H H H 'Pr H CH3 F OH XXIX-27-2 p-F-Ph H H CH3 'Pr H CH3 F OH XXIX-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H CH3 F OH XXIX-27-4 p-F-Ph H H CH2CH(CH3) 2 'Pr H CH3 F OH XXIX-27-5 p-F-Ph H H CH 2Ph 'Pr H CH3 F OH XXIX-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH XXIX-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H CH3 F OH XXIX-27-8 p-F-Ph * H * 'Pr H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-28. No R R 2 R 3a R 3b R4 R6 X Y

XXIX-28-1 p-Cl-Ph H H H 'Pr H CH 3 F OH XXIX-28-2 p-Cl-Ph H H CH3 'Pr H CH 3 F OH XXIX-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXIX-28-4 p-Cl-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXIX-28-5 p-Cl-Ph H H CH2Ph 'Pr H CH 3 F OH XXIX-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H CH 3 F OH XXIX-28-7 p-Cl-Ph H H CH2CH2SCH 3 'Pr H CH 3 F OH XXIX-28-8 p-Cl-Ph * H * Pr H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-29. No R R2 R 3 a R3b R4 R' R6 X Y XXIX-29-1 p-Br-Ph H H H 'Pr H CH 3 F OH XXIX-29-2 p-Br-Ph H H CH3 'Pr H CH 3 F OH XXIX-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H CH 3 F OH XXIX-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H CH 3 F OH XXIX-29-5 p-Br-Ph H H CH 2Ph 'Pr H CH 3 F OH XXIX-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H CH 3 F OH XXIX-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H CH 3 F OH XXIX-29-8 p-Br-Ph * H * 'Pr H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-30. N9 R1 R2 R 3a R3 b R4 R' R6 X Y

XXIX-30-1 p-I-Ph H H H 'Pr H CH3 F OH XXIX-30-2 p-I-Ph H H CH3 'Pr H CH3 F OH XXIX-30-3 p-I-Ph H H CH(CH 3)2 'Pr H CH3 F OH XXIX-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H CH3 F OH XXIX-30-5 p-I-Ph H H CH 2Ph 'Pr H CH3 F OH XXIX-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H CH3 F OH XXIX-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H CH3 F OH XXIX-30-8 p-I-Ph * H * 'Pr H CH3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-31. No R1 R2 R 3a R3b R4 RR6 X Y XXIX-31-1 CH 3 H H H "Bu H CH 3 F OH XXIX-31-2 CH 3 H H CH3 "Bu H CH 3 F OH XXIX-31-3 CH 3 H H CH(CH3) 2 "Bu H CH 3 F OH XXIX-31-4 CH 3 H H CH2CH(CH3) 2 "Bu H CH 3 F OH XXIX-31-5 CH 3 H H CH 2Ph "Bu H CH 3 F OH XXIX-31-6 CH 3 H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-31-7 CH 3 H H CH2CH 2SCH 3 "Bu H CH 3 F OH XXIX-31-8 CH 3 * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-32. No Rl R2 R 3a R3b R4 R' R6 X Y XXIX-32-1 Et H H H "Bu H CH 3 F OH XXIX-32-2 Et H H CH 3 "Bu H CH 3 F OH XXIX-32-3 Et H H CH(CH3) 2 "Bu H CH 3 F OH XXIX-32-4 Et H H CH 2CH(CH3) 2 "Bu H CH 3 F OH XXIX-32-5 Et H H CH 2Ph "Bu H CH 3 F OH XXIX-32-6 Et H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-32-7 Et H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXIX-32-8 Et * H * "Bu H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-33. No R1 R2 R 3a Rb R4 R' R6 X Y XXIX-33-1 'Pr H H H "Bu H CH 3 F OH XXIX-33-2 'Pr H H CH 3 "Bu H CH 3 F OH XXIX-33-3 'Pr H H CH(CH3) 2 "Bu H CH 3 F OH XXIX-33-4 'Pr H H CH 2CH(CH 3)2 "Bu H CH 3 F OH XXIX-33-5 'Pr H H CH 2Ph "Bu H CH 3 F OH XXIX-33-6 'Pr H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-33-7 'Pr H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXIX-33-8 'Pr * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-34. R No R1 R2 R3 a R 3b R4 R X Y XXIX-34-1 'Bu H H H "Bu H CH 3 F OH XXIX-34-2 'Bu H H CH 3 "Bu H CH 3 F OH XXIX-34-3 'Bu H H CH(CH3) 2 "Bu H CH 3 F OH XXIX-34-4 'Bu H H CH 2CH(CH 3) 2 "Bu H CH 3 F OH XXIX-34-5 'Bu H H CH 2Ph "Bu H CH 3 F OH XXIX-34-6 'Bu H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXIX-34-8 'Bu * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

rAfl-

Table XXIX-35. No R1 R2 R 3a R3b R4 R5 R6 X Y XXIX-35-1 Ph H H H "Bu H CH 3 F OH XXIX-35-2 Ph H H CH3 "Bu H CH 3 F OH XXIX-35-3 Ph H H CH(CH3)2 "Bu H CH 3 F OH XXIX-35-4 Ph H H CH2CH(CH3) 2 "Bu H CH 3 F OH XXIX-35-5 Ph H H CH 2Ph "Bu H CH 3 F OH XXIX-35-6 Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-35-7 Ph H H CH2CH 2SCH 3 "Bu H CH 3 F OH XXIX-35-8 Ph * H * "Bu H CH 3 F OH *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-36. N9 R1 R2 R 3a R3 b R4 R5 R6 X Y

XXIX-36-1 p-Me-Ph H H H "Bu H CH 3 F OH XXIX-36-2 p-Me-Ph H H CH 3 "Bu H CH 3 F OH XXIX-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H CH 3 F OH XXIX-36-4 p-Me-Ph H H CH 2CH(CH 3)2 "Bu H CH 3 F OH XXIX-36-5 p-Me-Ph H H CH 2Ph "Bu H CH 3 F OH XXIX-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXIX-36-8 p-Me-Ph * H * "Bu H CH 3 F OH *R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXIX-37. No R1 R2 R3 a R3b R4 R 5 R6 X Y

XXIX-37-1 p-F-Ph H H H "Bu H CH 3 F OH XXIX-37-2 p-F-Ph H H CH 3 "Bu H CH 3 F OH XXIX-37-3 p-F-Ph H H CH(CH 3) 2 "Bu H CH 3 F OH XXIX-37-4 p-F-Ph H H CH 2CH(CH 3) 2 "Bu H CH 3 F OH XXIX-37-5 p-F-Ph H H CH 2Ph "Bu H CH 3 F OH XXIX-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H CH 3 F OH XXIX-37-8 p-F-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

_, r,1_

Table XXIX-38. R R2 R3 a R 3b R4 R R X Y No XXIX-38-1 p-Cl-Ph H H H "Bu H CH 3 F OH XXIX-38-2 p-Cl-Ph H H CH3 "Bu H CH 3 F OH XXIX-38-3 p-Cl-Ph H H CH(CH3)2 "Bu H CH 3 F OH XXIX-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H CH 3 F OH XXIX-38-5 p-Cl-Ph H H CH2Ph "Bu H CH 3 F OH XXIX-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H CH 3 F OH XXIX-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H CH 3 F OH XXIX-38-8 p-Cl-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-39. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXIX-39-1 p-Br-Ph H H H "Bu H CH 3 F OH XXIX-39-2 p-Br-Ph H H CH 3 "Bu H CH 3 F OH XXIX-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H CH 3 F OH XXIX-39-4 p-Br-Ph H H CH 2 CH(CH 3)2 "Bu H CH 3 F OH XXIX-39-5 p-Br-Ph H H CH 2 Ph "Bu H CH 3 F OH XXIX-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH XXIX-39-8 p-Br-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-40. No R1 R2 R 3a R3b R4 R5 R6 X Y XXIX-40-1 p-I-Ph H H H "Bu H CH 3 F OH XXIX-40-2 p-I-Ph H H CH 3 "Bu H CH 3 F OH XXIX-40-3 p-I-Ph H H CH(CH3)2 "Bu H CH 3 F OH XXIX-40-4 p-I-Ph H H CH 2 CH(CH 3 )2 "Bu H CH 3 F OH XXIX-40-5 p-I-Ph H H CH 2 Ph "Bu H CH 3 F OH XXIX-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H CH 3 F OH XXIX-40-7 p-I-Ph H H CH 2 CH 2 SCH 3 "Bu H CH 3 F OH XXIX-40-8 p-I-Ph * H * "Bu H CH 3 F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-41. R' No R1 R2 R 3a R3b R4 R' X Y XXIX-41-1 CH 3 H H H Bz H CH 3 F OH XXIX-41-2 CH 3 H H CH3 Bz H CH3 F OH XXIX-41-3 CH3 H H CH(CH3) 2 Bz H CH3 F OH XXIX-41-4 CH3 H H CH2CH(CH3) 2 Bz H CH3 F OH XXIX-41-5 CH3 H H CH 2Ph Bz H CH3 F OH XXIX-41-6 CH3 H H CH 2-indol-3-yl Bz H CH3 F OH XXIX-41-7 CH3 H H CH2CH 2SCH 3 Bz H CH3 F OH XXIX-41-8 CH3 * H * Bz H CH3 F OH *R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-42. No R1 R2 R3a R3b R4 R' R6 X y

XXIX-42-1 Et H H H Bz H CH3 F OH XXIX-42-2 Et H H CH 3 Bz H CH3 F OH XXIX-42-3 Et H H CH(CH3) 2 Bz H CH3 F OH XXIX-42-4 Et H H CH 2CH(CH3) 2 Bz H CH3 F OH XXIX-42-5 Et H H CH 2Ph Bz H CH3 F OH XXIX-42-6 Et H H CH 2-indol-3-yl Bz H CH3 F OH XXIX-42-7 Et H H CH 2CH 2SCH 3 Bz H CH3 F OH XXIX-42-8 Et * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-43. N R1 R2 R 3a R3 b 4 R 5 R6 X Y

XXIX-43-1 'Pr H H H Bz H CH 3 F OH XXIX-43-2 Pr H H CH 3 Bz H CH 3 F OH XXIX-43-3 Pr H H CH(CH3) 2 Bz H CH 3 F OH XXIX-43-4 Pr H H CH 2CH(CH 3)2 Bz H CH 3 F OH XXIX-43-5 Pr H H CH 2Ph Bz H CH 3 F OH XXIX-43-6 'Pr H H CH 2-indol-3-yl Bz H CH 3 F OH XXIX-43-7 'Pr H H CH 2CH2SCH 3 Bz H CH 3 F dAI XXIX-43-8 'Pr * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-44. No R1 R2 R3 a R3 R4 R R6 X Y XXIX-44-1 'Bu H H H Bz H CH 3 F OH XXIX-44-2 'Bu H H CH 3 Bz H CH 3 F OH XXIX-44-3 'Bu H H CH(CH3) 2 Bz H CH 3 F OH XXIX-44-4 'Bu H H CH 2CH(CH3)2 Bz H CH 3 F OH XXIX-44-5 'Bu H H CH 2Ph Bz H CH 3 F OH XXIX-44-6 'Bu H H CH 2-indol-3-yl Bz H CH 3 F OH XXIX-44-7 'Bu H H CH 2CH 2SCH 3 Bz H CH 3 F OH XXIX-44-8 'Bu * H * Bz H CH 3 F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-45. No R1 R2 R3a R3 R4 R5 R6 X Y XXIX-45-1 Ph H H H Bz H CH 3 F OH XXIX-45-2 Ph H H CH3 Bz H CH 3 F OH XXIX-45-3 Ph H H CH(CH3)2 Bz H CH 3 F OH XXIX-45-4 Ph H H CH2CH(CH3) 2 Bz H CH 3 F OH XXIX-45-5 Ph H H CH 2Ph Bz H CH 3 F OH XXIX-45-6 Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXIX-45-7 Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH XXIX-45-8 Ph * H * Bz H CH 3 F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-46. R R2 R 3 R3b R4 R5 R' X Y No a

XXIX-46-1 p-Me-Ph H H H Bz H CH 3 F OH XXIX-46-2 p-Me-Ph H H CH3 Bz H CH 3 F OH XXIX-46-3 p-Me-Ph H H CH(CH 3)2 Bz H CH 3 F OH XXIX-46-4 p-Me-Ph H H CH2CH(CH 3)2 Bz H CH 3 F OH XXIX-46-5 p-Me-Ph H H CH 2Ph Bz H CH 3 F OH XXIX-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXIX-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH XXIX-46-8 p-Me-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-47. No R RR 3 a R3b R4 R 5 R' X Y XXIX-47-1 p-F-Ph H H H Bz H CH 3 F OH XXIX-47-2 p-F-Ph H H CH3 Bz H CH 3 F OH XXIX-47-3 p-F-Ph H H CH(CH3)2 Bz H CH 3 F OH XXIX-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H CH 3 F OH XXIX-47-5 p-F-Ph H H CH 2Ph Bz H CH 3 F OH XXIX-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXIX-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH XXIX-47-8 p-F-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXIX-48. N9 R1 R2 R3 a R3 b R4 R R6 X Y XXIX-48-1 p-Cl-Ph H H H Bz H CH 3 F OH XXIX-48-2 p-Cl-Ph H H CH3 Bz H CH 3 F OH XXIX-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H CH 3 F OH XXIX-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H CH 3 F OH XXIX-48-5 p-Cl-Ph H H CH2Ph Bz H CH 3 F OH XXIX-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H CH 3 F OH XXIX-48-7 p-Cl-Ph H H CH2CH2SCH 3 Bz H CH 3 F OH XXIX-48-8 p-Cl-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-49. No R R2 R 3 a R3b R4 R5 R6 X Y

XXIX-49-1 p-Br-Ph H H H Bz H CH3 F OH XXIX-49-2 p-Br-Ph H H CH3 Bz H CH3 F OH XXIX-49-3 p-Br-Ph H H CH(CH 3)2 Bz H CH3 F OH XXIX-49-4 p-Br-Ph H H CH2CH(CH 3) 2 Bz H CH3 F OH XXIX-49-5 p-Br-Ph H H CH 2Ph Bz H CH3 F OH XXIX-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H CH3 F OH XXIX-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H CH3 F OH XXIX-49-8 p-Br-Ph * H * Bz H CH3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXIX-50. No R RR 3 a R3b R4 R5 R6 X Y XXIX-50-1 p-I-Ph H H H Bz H CH 3 F OH XXIX-50-2 p-I-Ph H H CH3 Bz H CH 3 F OH XXIX-50-3 p-I-Ph H H CH(CH 3)2 Bz H CH 3 F OH XXIX-50-4 p-I-Ph H H CH2CH(CH 3)2 Bz H CH 3 F OH XXIX-50-5 p-I-Ph H H CH 2Ph Bz H CH 3 F OH XXIX-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H CH 3 F OH XXIX-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H CH 3 F OH XXIX-50-8 p-I-Ph * H * Bz H CH 3 F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

0 N

R3b R 2 0 NH

R3a N P N--P--O 0 O N

| e N 6 NH 2 4 C0 2 R OR' Rs R

Y X

xxx

Table XXX-1. No R R2 R3 a R 3b R4 R R6 X Y XXX-1-1 CH 3 H H H CH 3 H F H OH XXX-1-2 CH 3 H H CH 3 CH 3 H F H OH XXX-1-3 CH 3 H H CH(CH3) 2 CH 3 H F H OH XXX-1-4 CH 3 H H CH 2CH(CH 3) 2 CH 3 H F H OH XXX-1-5 CH 3 H H CH 2Ph CH 3 H F H OH XXX-1-6 CH 3 H H CH 2-indol-3-yl CH 3 H F H OH XXX-1-7 CH 3 H H CH 2CH2SCH 3 CH 3 H F H OH XXX-1-8 CH 3 * H * CH 3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXX-2. No RI R2 RaR 3 b R4 RR X Y XXX-2-1 Et H H H CH 3 H F H OH XXX-2-2 Et H H CH3 CH 3 H F H OH XXX-2-3 Et H H CH(CH3) 2 CH 3 H F H OH XXX-2-4 Et H H CH2CH(CH3)2 CH 3 H F H OH XXX-2-5 Et H H CH2Ph CH 3 H F H OH XXX-2-6 Et H H CH2-indol-3-yl CH 3 H F H OH XXX-2-7 Et H H CH2CH2SCH 3 CH 3 H F H OH XXX-2-8 Et * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-3. No R1 R2 R3 a R3 b R4 R' R6 X Y XXX-3-1 'Pr H H H CH 3 H F H OH XXX-3-2 'Pr H H CH3 CH3 H F H OH XXX-3-3 'Pr H H CH(CH3)2 CH3 H F H OH XXX-3-4 'Pr H H CH2CH(CH3) 2 CH3 H F H OH XXX-3-5 'Pr H H CH 2Ph CH3 H F H OH XXX-3-6 'Pr H H CH 2-indol-3-yl CH3 H F H OH XXX-3-7 'Pr H H CH2CH 2SCH 3 CH3 H F H OH XXX-3-8 'Pr * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-4. No R1 R2 R3 a R3b R4 R 5 R 6 X Y

XXX-4-1 'Bu H H H CH3 H F H OH XXX-4-2 'Bu H H CH3 CH3 H F H OH XXX-4-3 'Bu H H CH(CH3)2 CH3 H F H OH XXX-4-4 'Bu H H CH2CH(CH3) 2 CH3 H F H OH XXX-4-5 'Bu H H CH 2Ph CH3 H F H OH XXX-4-6 'Bu H H CH 2-indol-3-yl CH3 H F H OH XXX-4-7 'Bu H H CH2CH 2SCH 3 CH3 H F H OH XXX-4-8 'Bu * H * CH 3 H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-5. No R1 R2 R3 a R3b R4 R 5 R' X Y XXX-5-1 Ph H H H CH3 H F H OH XXX-5-2 Ph H H CH3 CH 3 H F H OH XXX-5-3 Ph H H CH(CH3) 2 CH3 H F H OH XXX-5-4 Ph H H CH2CH(CH3) 2 CH3 H F H OH XXX-5-5 Ph H H CH2Ph CH3 H F H OH XXX-5-6 Ph H H CH2-indol-3-yl CH 3 H F H OH XXX-5-7 Ph H H CH2CH 2SCH 3 CH3 H F H OH XXX-5-8 Ph * H * CH3 H F H OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-6. 5 N9 R1 R2 R 3a R3 b R4 R R6 X Y XXX-6-1 p-Me-Ph H H H CH3 H F H OH XXX-6-2 p-Me-Ph H H CH3 CH 3 H F H OH XXX-6-3 p-Me-Ph H H CH(CH3) 2 CH3 H F H OH XXX-6-4 p-Me-Ph H H CH2CH(CH 3)2 CH3 H F H OH XXX-6-5 p-Me-Ph H H CH2Ph CH3 H F H OH XXX-6-6 p-Me-Ph H H CH2-indol-3-yl CH 3 H F H OH XXX-6-7 p-Me-Ph H H CH2CH 2SCH 3 CH3 H F H OH XXX-6-8 p-Me-Ph * H * CH3 H F H OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-7. No R R 2 R 3 a R 3b R4 R5 R6 X Y XXX-7-1 p-F-Ph H H H CH3 H F H OH XXX-7-2 p-F-Ph H H CH 3 CH3 H F H OH XXX-7-3 p-F-Ph H H CH(CH3) 2 CH3 H F H OH XXX-7-4 p-F-Ph H H CH 2CH(CH3) 2 CH3 H F H OH XXX-7-6 p-F-Ph H H CH 2Ph CH3 H F H OH XXX-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F H OH XXX-7-8 p-F-Ph H H CH 2CH 2SCH 3 CH3 H F H OH XXX-7-20 p-F-Ph * H * CH3 H F H OH *R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-8. No R RR 3 a R 3b R4 R' R6 X Y XXX-8-1 p-Cl-Ph H H H CH 3 H F H OH XXX-8-2 p-Cl-Ph H H CH3 CH3 H F H OH XXX-8-3 p-Cl-Ph H H CH(CH3)2 CH3 H F H OH XXX-8-4 p-Cl-Ph H H CH2CH(CH3) 2 CH3 H F H OH XXX-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F H OH XXX-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH3 H F H OH XXX-8-7 p-Cl-Ph H H CH2CH 2SCH 3 CH3 H F H OH XXX-8-8 p-Cl-Ph * H * CH 3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXX-9. N9 R1 R2 R3 a R3 b R4 R R6 X Y XXX-9-1 p-Br-Ph H H H CH 3 H F H OH XXX-9-2 p-Br-Ph H H CH 3 CH 3 H F H OH XXX-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H F H OH XXX-9-4 p-Br-Ph H H CH 2CH(CH3)2 CH 3 H F H OH XXX-9-6 p-Br-Ph H H CH 2Ph CH 3 H F H OH XXX-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H F H OH XXX-9-8 p-Br-Ph H H CH 2CH2SCH 3 CH 3 H F H OH XXX-9-20 p-Br-Ph * H * CH 3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXX-10. No R R2 R 3 a R3b R4 R R6 X Y XXX-10-1 p-I-Ph H H H CH3 H F H OH XXX-10-2 p-I-Ph H H CH3 CH3 H F H OH XXX-10-3 p-I-Ph H H CH(CH3) 2 CH3 H F H OH XXX-10-4 p-I-Ph H H CH2CH(CH3) 2 CH3 H F H OH XXX-10-5 p-I-Ph H H CH 2Ph CH3 H F H OH XXX-10-6 p-I-Ph H H CH 2-indol-3-yl CH3 H F H OH XXX-10-7 p-I-Ph H H CH2CH 2SCH 3 CH3 H F H OH XXX-10-8 p-I-Ph * H * CH3 H F H OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ ruo_

Table XXX-11. No R1 R2 R3 a R3b R 4 R R X Y XXX-11-1 CH3 H H H Et H F H OH XXX-11-2 CH3 H H CH 3 Et H F H OH XXX-11-3 CH3 H H CH(CH3) 2 Et H F H OH XXX-11-4 CH3 H H CH 2CH(CH3)2 Et H F H OH XXX-11-5 CH3 H H CH 2Ph Et H F H OH XXX-11-6 CH3 H H CH 2-indol-3-yl Et H F H OH XXX-11-7 CH3 H H CH 2CH 2SCH 3 Et H F H OH XXX-11-8 CH3 * H * Et H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-12. N9 R1 R 2 R3 a R3b R4 R R6 X Y XXX-12-1 Et H H H Et H F H OH XXX-12-2 Et H H CH 3 Et H F H OH XXX-12-3 Et H H CH(CH3) 2 Et H F H OH XXX-12-4 Et H H CH 2CH(CH3)2 Et H F H OH XXX-12-5 Et H H CH 2Ph Et H F H OH XXX-12-6 Et H H CH 2-indol-3-yl Et H F H OH XXX-12-7 Et H H CH 2CH2SCH 3 Et H F H OH XXX-12-8 Et * H * EtH F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-13. N R1 R2 R 3a R3 b R4 R5 R6 X Y

XXX-13-1 'Pr H H H Et H F H OH XXX-13-2 'Pr H H CH3 Et H F H OH XXX-13-3 'Pr H H CH(CH3)2 Et H F H OH XXX-13-4 'Pr H H CH2CH(CH3) 2 Et H F H OH XXX-13-5 Pr H H CH 2Ph Et H F H OH XXX-13-6 Pr H H CH 2-indol-3-yl Et H F H OH XXX-13-7 Pr H H CH2CH 2SCH 3 Et H F H OH XXX-13-8 Pr * H * Et H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

r,7fl

Table XXX-14. R1 R2 R3 a R3b R4 R R X Y No XXX-14-1 'Bu H H H Et H F H OH XXX-14-2 'Bu H H CH 3 Et H F H OH XXX-14-3 'Bu H H CH(CH3) 2 Et H F H OH XXX-14-4 'Bu H H CH 2CH(CH3)2 Et H F H OH XXX-14-5 'Bu H H CH 2Ph Et H F H OH XXX-14-6 'Bu H H CH 2-indol-3-yl Et H F H OH XXX-14-7 'Bu H H CH 2CH2SCH 3 Et H F H OH XXX-14-8 'Bu * H * Et H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-15. N RI R 2 R3a R3 b R4 R X RXY XXX-15-1 Ph H H H Et H F H OH XXX-15-2 Ph H H CH 3 Et H F H OH XXX-15-3 Ph H H CH(CH3) 2 Et H F H OH XXX-15-4 Ph H H CH 2CH(CH3) 2 Et H F H OH XXX-15-5 Ph H H CH 2Ph Et H F H OH XXX-15-6 Ph H H CH 2-indol-3-yl Et H F H OH XXX-15-7 Ph H H CH 2CH 2SCH 3 Et H F H OH XXX-15-8 Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-16. No RI1 R2 R3 a R3b R4 R X RXY XXX-16-1 p-Me-Ph H H H Et H F H OH XXX-16-2 p-Me-Ph H H CH3 Et H F H OH XXX-16-3 p-Me-Ph H H CH(CH3) 2 Et H F H OH XXX-16-4 p-Me-Ph H H CH2CH(CH3) 2 Et H F H OH XXX-16-5 p-Me-Ph H H CH 2Ph Et H F H OH XXX-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F H OH XXX-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H F H OH XXX-16-8 p-Me-Ph * H * Et H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_' 71

Table XXX-17. No R R2 R 3 a R 3b R4 R R6 X Y XXX-17-1 p-F-Ph H H H Et H F H OH XXX-17-2 p-F-Ph H H CH 3 Et H F H OH XXX-17-3 p-F-Ph H H CH(CH3) 2 Et H F H OH XXX-17-4 p-F-Ph H H CH 2CH(CH3) 2 Et H F H OH XXX-17-5 p-F-Ph H H CH 2Ph Et H F H OH XXX-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F H OH XXX-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H F H OH XXX-17-8 p-F-Ph * H * Et H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-18. 9 R1 R2 R 3a R3 b R4 R' R6 X Y XXX-18-1 p-Cl-Ph H H H Et H F H OH XXX-18-2 p-Cl-Ph H H CH 3 Et H F H OH XXX-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F H OH XXX-18-4 p-Cl-Ph H H CH 2CH(CH3)2 Et H F H OH XXX-18-5 p-Cl-Ph H H CH 2Ph Et H F H OH XXX-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H F H OH XXX-18-7 p-Cl-Ph H H CH 2CH2SCH 3 Et H F H OH XXX-18-8 p-Cl-Ph * H * Et H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXX-19. No R R 2 R 3a R3b R 4 R5 R6 X Y XXX-19-1 p-Br-Ph H H H Et H F H OH XXX-19-2 p-Br-Ph H H CH 3 Et H F H OH XXX-19-3 p-Br-Ph H H CH(CH 3)2 Et H F H OH XXX-19-4 p-Br-Ph H H CH 2CH(CH3)2 Et H F H OH XXX-19-5 p-Br-Ph H H CH 2Ph Et H F H OH XXX-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F H OH XXX-19-7 p-Br-Ph H H CH 2CH2SCH 3 Et H F H OH XXX-19-8 p-Br-Ph * H * Et H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

r,7)-

Table XXX-20. No R R 2 R 3a R3b R4 R R X Y

XXX-20-1 p-I-Ph H H H Et H F H OH XXX-20-2 p-I-Ph H H CH3 Et H F H OH XXX-20-3 p-I-Ph H H CH(CH3) 2 Et H F H OH XXX-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H F H OH XXX-20-5 p-I-Ph H H CH 2Ph Et H F H OH XXX-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F H OH XXX-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H F H OH XXX-20-8 p-I-Ph * H * Et H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-21. X R1 R2 R3 a R3 b R4 R R6 X Y XXX-21-1 CH3 H H H 'Pr H F H OH XXX-21-2 CH3 H H CH 3 'Pr H F H OH XXX-21-3 CH3 H H CH(CH3) 2 'Pr H F H OH XXX-21-4 CH3 H H CH 2CH(CH3) 2 'Pr H F H OH XXX-21-5 CH3 H H CH 2Ph 'Pr H F H OH XXX-21-6 CH3 H H CH 2-indol-3-yl 'Pr H F H OH XXX-21-7 CH3 H H CH 2CH2SCH 3 'Pr H F H OH XXX-21-8 CH3 * H * 'Pr H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-22. No RI R2 R3 a R3b R4 R R XY XXX-22-1 Et H H H 'Pr H F H OH XXX-22-2 Et H H CH 3 'Pr H F H OH XXX-22-3 Et H H CH(CH 3)2 'Pr H F H OH XXX-22-4 Et H H CH 2CH(CH3) 2 'Pr H F H OH XXX-22-5 Et H H CH 2Ph 'Pr H F H OH XXX-22-6 Et H H CH 2-indol-3-yl 'Pr H F H OH XXX-22-7 Et H H CH 2CH2SCH 3 'Pr H F H OH XXX-22-8 Et * H * 'Pr H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

r,'72-

Table XXX-23. No R1 R2 R 3a R3b R4 R' R' X Y XXX-23-1 'Pr H H H 'Pr H F H OH XXX-23-2 'Pr H H CH3 'Pr H F H OH XXX-23-3 'Pr H H CH(CH 3) 2 'Pr H F H OH XXX-23-4 Pr H H CH2CH(CH3) 2 'Pr H F H OH XXX-23-5 Pr H H CH 2Ph 'Pr H F H OH XXX-23-6 Pr H H CH 2-indol-3-yl 'Pr H F H OH XXX-23-7 'Pr H H CH2CH 2SCH 3 'Pr H F H OH XXX-23-8 'Pr * H * 'Pr H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-24. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXX-24-1 'Bu H H H 'Pr H F H OH XXX-24-2 'Bu H H CH 3 'Pr H F H OH XXX-24-3 'Bu H H CH(CH 3) 2 'Pr H F H OH XXX-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H F H OH XXX-24-5 'Bu H H CH 2Ph 'Pr H F H OH XXX-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F H OH XXX-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H F H OH XXX-24-8 'Bu * H * 'Pr H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-25. No R1 R2 R3 a R3b R4 R 5 R 6 X Y

XXX-25-1 Ph H H H Pr H F H OH XXX-25-2 Ph H H CH 3 Pr H F H OH XXX-25-3 Ph H H CH(CH 3)2 'Pr H F H OH XXX-25-4 Ph H H CH 2CH(CH3) 2 'Pr H F H OH XXX-25-5 Ph H H CH 2Ph 'Pr H F H OH XXX-25-6 Ph H H CH 2-indol-3-yl 'Pr H F H OH XXX-25-7 Ph H H CH 2CH 2SCH 3 'Pr H F H OH XXX-25-8 Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

r,7A-

Table XXX-26. No R R2 R 3 a R3b R4 R' R6 X Y XXX-26-1 p-Me-Ph H H H 'Pr H F H OH XXX-26-2 p-Me-Ph H H CH3 'Pr H F H OH XXX-26-3 p-Me-Ph H H CH(CH3) 2 'Pr H F H OH XXX-26-4 p-Me-Ph H H CH2CH(CH3) 2 'Pr H F H OH XXX-26-5 p-Me-Ph H H CH 2Ph 'Pr H F H OH XXX-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXX-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H F H OH XXX-26-8 p-Me-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-27. N9 R1 R2 R 3 a R3 b R4 R' R6 X Y XXX-27-1 p-F-Ph H H H 'Pr H F H OH XXX-27-2 p-F-Ph H H CH 3 'Pr H F H OH XXX-27-3 p-F-Ph H H CH(CH3) 2 'Pr H F H OH XXX-27-4 p-F-Ph H H CH 2CH(CH3) 2 'Pr H F H OH XXX-27-5 p-F-Ph H H CH 2Ph 'Pr H F H OH XXX-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXX-27-7 p-F-Ph H H CH 2CH 2SCH 3 'Pr H F H OH XXX-27-8 p-F-Ph * H * 'Pr H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-28. No R R2 R 3 a R3b R4 R5 R6 X Y XXX-28-1 p-Cl-Ph H H H Pr H F H OH XXX-28-2 p-Cl-Ph H H CH 3 'Pr H F H OH XXX-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F H OH XXX-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr H F H OH XXX-28-5 p-Cl-Ph H H CH 2Ph 'Pr H F H OH XXX-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXX-28-7 p-Cl-Ph H H CH 2CH2SCH 3 'Pr H F H OH XXX-28-8 p-Cl-Ph * H * Pr H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

r, 7 r

Table XXX-29. No R R2 R3 a R3b R 4 R R6 X Y XXX-29-1 p-Br-Ph H H H 'Pr H F H OH XXX-29-2 p-Br-Ph H H CH 3 'Pr H F H OH XXX-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F H OH XXX-29-4 p-Br-Ph H H CH 2CH(CH3)2 'Pr H F H OH XXX-29-5 p-Br-Ph H H CH 2Ph 'Pr H F H OH XXX-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXX-29-7 p-Br-Ph H H CH 2CH2SCH 3 'Pr H F H OH XXX-29-8 p-Br-Ph * H * 'Pr H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-30. N9 R1 R2 R3 a R3 b R4 R' R6 X Y XXX-30-1 p-I-Ph H H H 'Pr H F H OH XXX-30-2 p-I-Ph H H CH3 'Pr H F H OH XXX-30-3 p-I-Ph H H CH(CH3) 2 'Pr H F H OH XXX-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H F H OH XXX-30-5 p-I-Ph H H CH 2Ph 'Pr H F H OH XXX-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F H OH XXX-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H F H OH XXX-30-8 p-I-Ph * H * 'Pr H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-31. No R1 R2 R3 a R3b R4 R 5 R6 X Y XXX-31-1 CH3 H H H "Bu H F H OH XXX-31-2 CH3 H H CH 3 "Bu H F H OH XXX-31-3 CH3 H H CH(CH3) 2 "Bu H F H OH XXX-31-4 CH3 H H CH 2CH(CH3)2 "Bu H F H OH XXX-31-5 CH3 H H CH 2Ph "Bu H F H OH XXX-31-6 CH3 H H CH 2-indol-3-yl "Bu H F H OH XXX-31-7 CH3 H H CH 2CH 2SCH 3 "Bu H F H OH XXX-31-8 CH3 * H * "Bu H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

r,7 r,

Table XXX-32. No RI R 2 RaR 3 b R4 R R X Y XXX-32-1 Et H H H "Bu H F H OH XXX-32-2 Et H H CH 3 "Bu H F H OH XXX-32-3 Et H H CH(CH3) 2 "Bu H F H OH XXX-32-4 Et H H CH 2CH(CH3)2 "Bu H F H OH XXX-32-5 Et H H CH 2Ph "Bu H F H OH XXX-32-6 Et H H CH 2-indol-3-yl "Bu H F H OH XXX-32-7 Et H H CH 2CH2SCH 3 "Bu H F H OH XXX-32-8 Et * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-33. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXX-33-1 'Pr H H H "Bu H F H OH XXX-33-2 'Pr H H CH3 "Bu H F H OH XXX-33-3 'Pr H H CH(CH 3) 2 "Bu H F H OH XXX-33-4 'Pr H H CH2CH(CH3) 2 "Bu H F H OH XXX-33-5 'Pr H H CH 2Ph "Bu H F H OH XXX-33-6 'Pr H H CH 2-indol-3-yl "Bu H F H OH XXX-33-7 'Pr H H CH2CH 2SCH 3 "Bu H F H OH XXX-33-8 'Pr * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-34. No R1 R2 R 3a R 3b R4 R 5 R6 X Y XXX-34-1 'Bu H H H "Bu H F H OH XXX-34-2 'Bu H H CH 3 "Bu H F H OH XXX-34-3 'Bu H H CH(CH3)2 "Bu H F H OH XXX-34-4 'Bu H H CH 2CH(CH3) 2 "Bu H F H OH XXX-34-5 'Bu H H CH 2Ph "Bu H F H OH XXX-34-6 'Bu H H CH 2-indol-3-yl "Bu H F H OH XXX-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F H OH XXX-34-8 'Bu * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-35. No R1 R2 R3 a R3b R4 R5 R6 X Y XXX-35-1 Ph H H H "Bu H F H OH XXX-35-2 Ph H H CH 3 "Bu H F H OH XXX-35-3 Ph H H CH(CH 3) 2 "Bu H F H OH XXX-35-4 Ph H H CH 2CH(CH 3) 2 "Bu H F H OH XXX-35-5 Ph H H CH 2Ph "Bu H F H OH XXX-35-6 Ph H H CH 2-indol-3-yl "Bu H F H OH XXX-35-7 Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXX-35-8 Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-36. N9 R1 R2 R3 a R3 b R4 R5 R6 X Y XXX-36-1 p-Me-Ph H H H "Bu H F H OH XXX-36-2 p-Me-Ph H H CH 3 "Bu H F H OH XXX-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H F H OH XXX-36-4 p-Me-Ph H H CH 2CH(CH 3) 2 "Bu H F H OH XXX-36-5 p-Me-Ph H H CH 2Ph "Bu H F H OH XXX-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F H OH XXX-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXX-36-8 p-Me-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

Table XXX-37. No R1 R2 R 3a R 3b R4 R 5 R 6 X Y

XXX-37-1 p-F-Ph H H H "Bu H F H OH XXX-37-2 p-F-Ph H H CH 3 "Bu H F H OH XXX-37-3 p-F-Ph H H CH(CH3) 2 "Bu H F H OH XXX-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H F H OH XXX-37-5 p-F-Ph H H CH 2Ph "Bu H F H OH XXX-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F H OH XXX-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F H OH XXX-37-8 p-F-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH 2) 3 to form five-membered ring.

,7S2-

Table XXX-38. No R RR 3 a R3b R4 R' R' X Y XXX-38-1 p-Cl-Ph H H H "Bu H F H OH XXX-38-2 p-Cl-Ph H H CH 3 "Bu H F H OH XXX-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F H OH XXX-38-4 p-Cl-Ph H H CH 2CH(CH3)2 "Bu H F H OH XXX-38-5 p-Cl-Ph H H CH 2Ph "Bu H F H OH XXX-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H F H OH XXX-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H F H OH XXX-38-8 p-Cl-Ph * H * "Bu H F H OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXX-39. 6 N9 R1 R2 R3 a R3 b R4 R R X Y XXX-39-1 p-Br-Ph H H H "Bu H F H OH XXX-39-2 p-Br-Ph H H CH 3 "Bu H F H OH XXX-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H F H OH XXX-39-4 p-Br-Ph H H CH 2 CH(CH3)2 "Bu H F H OH XXX-39-5 p-Br-Ph H H CH 2Ph "Bu H F H OH XXX-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F H OH XXX-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H F H OH XXX-39-8 p-Br-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXX-40. No R1 R2 R3a R3b R4 R5 R6 X Y XXX-40-1 p-I-Ph H H H "Bu H F H OH XXX-40-2 p-I-Ph H H CH3 "Bu H F H OH XXX-40-3 p-I-Ph H H CH(CH3) 2 "Bu H F H OH XXX-40-4 p-I-Ph H H CH2 CH(CH3) 2 "Bu H F H OH XXX-40-5 p-I-Ph H H CH 2 Ph "Bu H F H OH XXX-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F H OH XXX-40-7 p-I-Ph H H CH2 CH 2 SCH 3 "Bu H F H OH XXX-40-8 p-I-Ph * H * "Bu H F H OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

_ 70_

Table XXX-41. No R1 R2 R3 a R3b R4 R R X Y XXX-41-1 CH3 H H H Bz H F H OH XXX-41-2 CH3 H H CH 3 Bz H F H OH XXX-41-3 CH3 H H CH(CH3) 2 Bz H F H OH XXX-41-4 CH3 H H CH 2CH(CH3)2 Bz H F H OH XXX-41-5 CH3 H H CH 2Ph Bz H F H OH XXX-41-6 CH3 H H CH 2-indol-3-yl Bz H F H OH XXX-41-7 CH3 H H CH 2CH2SCH 3 Bz H F H OH XXX-41-8 CH3 * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-42. N9 R1 R 2 R3 a R3 b R4 R R X Y XXX-42-1 Et H H H Bz H F H OH XXX-42-2 Et H H CH 3 Bz H F H OH XXX-42-3 Et H H CH(CH3) 2 Bz H F H OH XXX-42-4 Et H H CH 2CH(CH3)2 Bz H F H OH XXX-42-5 Et H H CH 2Ph Bz H F H OH XXX-42-6 Et H H CH 2-indol-3-yl Bz H F H OH XXX-42-7 Et H H CH 2CH2SCH 3 Bz H F H OH XXX-42-8 Et * H * Bz H F H OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-43. N R1 R2 R 3a R3 b R4 R 5 R6 X Y XXX-43-1 'Pr H H H Bz H F H OH XXX-43-2 Pr H H CH3 Bz H F H OH XXX-43-3 Pr H H CH(CH 3) 2 Bz H F H OH XXX-43-4 Pr H H CH2CH(CH3) 2 Bz H F H OH XXX-43-5 Pr H H CH 2Ph Bz H F H OH XXX-43-6 'Pr H H CH 2-indol-3-yl Bz H F H OH XXX-43-7 'Pr H H CH2CH 2SCH 3 Bz H F H N9I XXX-43-8 'Pr * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

;Qsn-

Table XXX-44. No R1 R2 R 3a R 3b R4 R 5 R' X Y XXX-44-1 'Bu H H H Bz H F H OH XXX-44-2 'Bu H H CH 3 Bz H F H OH XXX-44-3 'Bu H H CH(CH3)2 Bz H F H OH XXX-44-4 'Bu H H CH 2CH(CH3) 2 Bz H F H OH XXX-44-5 'Bu H H CH 2Ph Bz H F H OH XXX-44-6 'Bu H H CH 2-indol-3-yl Bz H F H OH XXX-44-7 'Bu H H CH 2CH 2SCH 3 Bz H F H OH XXX-44-8 'Bu * H * Bz H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-45. N9 R1 R 2 R3a R3 b R4 R 5 R6 X Y XXX-45-1 Ph H H H Bz H F H OH XXX-45-2 Ph H H CH 3 Bz H F H OH XXX-45-3 Ph H H CH(CH3) 2 Bz H F H OH XXX-45-4 Ph H H CH 2CH(CH3) 2 Bz H F H OH XXX-45-5 Ph H H CH 2Ph Bz H F H OH XXX-45-6 Ph H H CH 2-indol-3-yl Bz H F H OH XXX-45-7 Ph H H CH 2CH 2SCH 3 Bz H F H OH XXX-45-8 Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-46. No RI1 R2 R3 a R3b R4 R 5 R6 X Y XXX-46-1 p-Me-Ph H H H Bz H F H OH XXX-46-2 p-Me-Ph H H CH3 Bz H F H OH XXX-46-3 p-Me-Ph H H CH(CH3) 2 Bz H F H OH XXX-46-4 p-Me-Ph H H CH2CH(CH3) 2 Bz H F H OH XXX-46-5 p-Me-Ph H H CH 2Ph Bz H F H OH XXX-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F H OH XXX-46-7 p-Me-Ph H H CH2CH 2SCH 3 Bz H F H OH XXX-46-8 p-Me-Ph * H * Bz H F H OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_21 _

Table XXX-47. No R R2 R 3 a R 3b R4 R' R' X Y XXX-47-1 p-F-Ph H H H Bz H F H OH XXX-47-2 p-F-Ph H H CH 3 Bz H F H OH XXX-47-3 p-F-Ph H H CH(CH 3) 2 Bz H F H OH XXX-47-4 p-F-Ph H H CH 2CH(CH3) 2 Bz H F H OH XXX-47-5 p-F-Ph H H CH 2Ph Bz H F H OH XXX-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F H OH XXX-47-7 p-F-Ph H H CH 2CH 2SCH 3 Bz H F H OH XXX-47-8 p-F-Ph * H * Bz H F H OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXX-48. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXX-48-1 p-Cl-Ph H H H Bz H F H OH XXX-48-2 p-Cl-Ph H H CH 3 Bz H F H OH XXX-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F H OH XXX-48-4 p-Cl-Ph H H CH 2CH(CH3)2 Bz H F H OH XXX-48-5 p-Cl-Ph H H CH 2Ph Bz H F H OH XXX-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H F H OH XXX-48-7 p-Cl-Ph H H CH 2CH2SCH 3 Bz H F H OH XXX-48-8 p-Cl-Ph * H * Bz H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXX-49. No R R2 R 3 a R3b R4 R R X Y

XXX-49-1 p-Br-Ph H H H Bz H F H OH XXX-49-2 p-Br-Ph H H CH 3 Bz H F H OH XXX-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F H OH XXX-49-4 p-Br-Ph H H CH 2CH(CH3)2 Bz H F H OH XXX-49-5 p-Br-Ph H H CH 2Ph Bz H F H OH XXX-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F H OH XXX-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz H F H OH XXX-49-8 p-Br-Ph * H * Bz H F H OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

t r;Q )-

Table XXX-50. No R R2 R 3 a R3b R4 R 5 R' X Y XXX-50-1 p-I-Ph H H H Bz H F H OH XXX-50-2 p-I-Ph H H CH3 Bz H F H OH XXX-50-3 p-I-Ph H H CH(CH 3) 2 Bz H F H OH XXX-50-4 p-I-Ph H H CH2CH(CH 3) 2 Bz H F H OH XXX-50-5 p-I-Ph H H CH 2Ph Bz H F H OH XXX-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F H OH XXX-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H F H OH XXX-50-8 p-I-Ph * H * Bz H F H OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

0 N

R3b R 2 0 NH

R3a N-P-0 N-P-0 J | e N 4 C0 2 R OR' Rs R6 NH 2

Y X XXXI

Table XXXI-1. No R R22 R3 aRb R4 R 5 R6 X Y XXXI-1-1 CH3 H H H CH3 H F F OH XXXI-1-2 CH3 H H CH 3 CH3 H F F OH XXXI-1-3 CH3 H H CH(CH 3) 2 CH 3 H F F OH XXXI-1-4 CH3 H H CH 2CH(CH3) 2 CH 3 H F F OH XXXI-1-5 CH3 H H CH 2Ph CH3 H F F OH XXXI-1-6 CH3 H H CH 2-indol-3-yl CH 3 H F F OH XXXI-1-7 CH3 H H CH 2CH2SCH 3 CH 3 H F F OH XXXI-1-8 CH3 * H * CH 3 H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-2. No Rl R 2 R3 a R 3b R4 R 5 R' X Y XXXI-2-1 Et H H H CH 3 H F F OH XXXI-2-2 Et H H CH 3 CH 3 H F F OH XXXI-2-3 Et H H CH(CH3) 2 CH 3 H F F OH XXXI-2-4 Et H H CH 2CH(CH3) 2 CH 3 H F F OH XXXI-2-5 Et H H CH 2Ph CH 3 H F F OH XXXI-2-6 Et H H CH 2-indol-3-yl CH 3 H F F OH XXXI-2-7 Et H H CH 2CH 2SCH3 CH3 H F F OH XXXI-2-8 Et * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-3. No R1 R2 R3 a R3 b R4 R' R6 X Y XXXI-3-1 'Pr H H H CH 3 H F F OH XXXI-3-2 'Pr H H CH 3 CH3 H F F OH XXXI-3-3 'Pr H H CH(CH3) 2 CH3 H F F OH XXXI-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H F F OH XXXI-3-5 'Pr H H CH 2Ph CH 3 H F F OH XXXI-3-6 'Pr H H CH 2-indol-3-yl CH3 H F F OH XXXI-3-7 'Pr H H CH 2CH2SCH 3 CH3 H F F OH XXXI-3-8 'Pr * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-4. No R1 R2 R 3a R3b R4 R 5 R6 X Y

XXXI-4-1 'Bu H H H CH 3 H F F OH XXXI-4-2 'Bu H H CH 3 CH 3 H F F OH XXXI-4-3 'Bu H H CH(CH3) 2 CH 3 H F F OH XXXI-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H F F OH XXXI-4-5 'Bu H H CH 2Ph CH 3 H F F OH XXXI-4-6 'Bu H H CH 2-indol-3-yl CH 3 H F F OH XXXI-4-7 'Bu H H CH 2CH2SCH 3 CH 3 H F F OH XXXI-4-8 'Bu * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

rQA-

Table XXXI-5. No R1 R2 R3 a R 3b R4 RR 6 X Y

XXXI-5-1 Ph H H H CH 3 H F F OH XXXI-5-2 Ph H H CH3 CH3 H F F OH XXXI-5-3 Ph H H CH(CH3)2 CH3 H F F OH XXXI-5-4 Ph H H CH2CH(CH3) 2 CH3 H F F OH XXXI-5-5 Ph H H CH 2Ph CH 3 H F F OH XXXI-5-6 Ph H H CH 2-indol-3-yl CH3 H F F OH XXXI-5-7 Ph H H CH2CH2 SCH3 CH3 H F F OH XXXI-5-8 Ph * H * CH 3 H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-6. 6 N9 R1 R2 R3 a R3 b R4 RR X Y

XXXI-6-1 p-Me-Ph H H H CH 3 H F F OH XXXI-6-2 p-Me-Ph H H CH3 CH3 H F F OH XXXI-6-3 p-Me-Ph H H CH(CH3)2 CH3 H F F OH XXXI-6-4 p-Me-Ph H H CH2CH(CH3) 2 CH3 H F F OH XXXI-6-5 p-Me-Ph H H CH 2Ph CH 3 H F F OH XXXI-6-6 p-Me-Ph H H CH 2-indol-3-yl CH3 H F F OH XXXI-6-7 p-Me-Ph H H CH2CH2 SCH3 CH3 H F F OH XXXI-6-8 p-Me-Ph * H * CH3 H F F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-7. No R R2 R 3 a R3b R4 RR 6 X Y XXXI-7-1 p-F-Ph H H H CH 3 H F F OH XXXI-7-2 p-F-Ph H H CH3 CH3 H F F OH XXXI-7-3 p-F-Ph H H CH(CH3)2 CH3 H F F OH XXXI-7-4 p-F-Ph H H CH2CH(CH3) 2 CH3 H F F OH XXXI-7-6 p-F-Ph H H CH 2Ph CH 3 H F F OH XXXI-7-7 p-F-Ph H H CH 2-indol-3-yl CH3 H F F OH XXXI-7-8 p-F-Ph H H CH2CH 2SCH 3 CH3 H F F OH XXXI-7-20 p-F-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-8. No R R2 R3 a R3b R4 RR X Y XXXI-8-1 p-Cl-Ph H H H CH 3 H F F OH XXXI-8-2 p-Cl-Ph H H CH 3 CH 3 H F F OH XXXI-8-3 p-Cl-Ph H H CH(CH3) 2 CH 3 H F F OH XXXI-8-4 p-Cl-Ph H H CH 2CH(CH3)2 CH 3 H F F OH XXXI-8-5 p-Cl-Ph H H CH 2Ph CH 3 H F F OH XXXI-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H F F OH XXXI-8-7 p-Cl-Ph H H CH 2CH2SCH 3 CH 3 H F F OH XXXI-8-8 p-Cl-Ph * H * CH 3 H F F OH *R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXXI-9. 5 N9 R1 R2 R 3a R3 b R4 R R6 X Y XXXI-9-1 p-Br-Ph H H H CH3 H F F OH XXXI-9-2 p-Br-Ph H H CH3 CH3 H F F OH XXXI-9-3 p-Br-Ph H H CH(CH3) 2 CH3 H F F OH XXXI-9-4 p-Br-Ph H H CH2CH(CH3) 2 CH3 H F F OH XXXI-9-6 p-Br-Ph H H CH 2Ph CH3 H F F OH XXXI-9-7 p-Br-Ph H H CH 2-indol-3-yl CH3 H F F OH XXXI-9-8 p-Br-Ph H H CH2CH 2SCH 3 CH3 H F F OH XXXI-9-20 p-Br-Ph * H * CH3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-10. No R R2 R 3 a R3b R4 R5 R6 X Y XXXI-10-1 p-I-Ph H H H CH 3 H F F OH XXXI-10-2 p-I-Ph H H CH3 CH 3 H F F OH XXXI-10-3 p-I-Ph H H CH(CH3)2 CH 3 H F F OH XXXI-10-4 p-I-Ph H H CH2CH(CH 3)2 CH 3 H F F OH XXXI-10-5 p-I-Ph H H CH 2Ph CH 3 H F F OH XXXI-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H F F OH XXXI-10-7 p-I-Ph H H CH2CH 2SCH 3 CH 3 H F F OH XXXI-10-8 p-I-Ph * H * CH 3 H F F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rQS2 r

Table XXXI-11. No R1 R2 R 3a R3b R4 R R X Y

XXXI-11-1 CH 3 H H H Et H F F OH XXXI-11-2 CH 3 H H CH3 Et H F F OH XXXI-11-3 CH3 H H CH(CH3) 2 Et H F F OH XXXI-11-4 CH 3 H H CH2CH(CH3) 2 Et H F F OH XXXI-11-5 CH 3 H H CH 2Ph Et H F F OH XXXI-11-6 CH3 H H CH 2-indol-3-yl Et H F F OH XXXI-11-7 CH3 H H CH2CH 2SCH 3 Et H F F OH XXXI-11-8 CH 3 * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-12. No R1 R2 R3a R3b R4 R R X Y

XXXI-12-1 Et H H H Et H F F OH XXXI-12-2 Et H H CH 3 Et H F F OH XXXI-12-3 Et H H CH(CH3) 2 Et H F F OH XXXI-12-4 Et H H CH 2CH(CH3) 2 Et H F F OH XXXI-12-5 Et H H CH 2Ph Et H F F OH XXXI-12-6 Et H H CH 2-indol-3-yl Et H F F OH XXXI-12-7 Et H H CH 2CH 2SCH 3 Et H F F OH XXXI-12-8 Et * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-13. N R1 R2 R 3a R 3b R4 R5 R6 X Y XXXI-13-1 'Pr H H H Et H F F OH XXXI-13-2 'Pr H H CH 3 Et H F F OH XXXI-13-3 'Pr H H CH(CH3) 2 Et H F F OH XXXI-13-4 'Pr H H CH 2CH(CH3)2 Et H F F OH XXXI-13-5 Pr H H CH 2Ph Et H F F OH XXXI-13-6 Pr H H CH 2-indol-3-yl Et H F F OH XXXI-13-7 Pr H H CH 2CH 2SCH 3 Et H F F OH XXXI-13-8 Pr * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-14. R' R' No R1 R2 R3 a R3b R4 X Y XXXI-14-1 'Bu H H H Et H F F OH XXXI-14-2 'Bu H H CH3 Et H F F OH XXXI-14-3 'Bu H H CH(CH 3) 2 Et H F F OH XXXI-14-4 'Bu H H CH2CH(CH 3) 2 Et H F F OH XXXI-14-5 'Bu H H CH 2Ph Et H F F OH XXXI-14-6 'Bu H H CH 2-indol-3-yl Et H F F OH XXXI-14-7 'Bu H H CH2CH 2SCH 3 Et H F F OH XXXI-14-8 'Bu * H * Et H F F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

Table XXXI-15. No R1 R2 R3a R3 b R4 R5 R6 X Y XXXI-15-1 Ph H H H Et H F F OH XXXI-15-2 Ph H H CH3 Et H F F OH XXXI-15-3 Ph H H CH(CH 3)2 Et H F F OH XXXI-15-4 Ph H H CH2CH(CH 3)2 Et H F F OH XXXI-15-5 Ph H H CH 2Ph Et H F F OH XXXI-15-6 Ph H H CH 2-indol-3-yl Et H F F OH XXXI-15-7 Ph H H CH2CH 2SCH 3 Et H F F OH XXXI-15-8 Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-16. No R R2 R 3 a R3b R4 R5 R6 X Y XXXI-16-1 p-Me-Ph H H H Et H F F OH XXXI-16-2 p-Me-Ph H H CH3 Et H F F OH XXXI-16-3 p-Me-Ph H H CH(CH 3)2 Et H F F OH XXXI-16-4 p-Me-Ph H H CH2CH(CH 3)2 Et H F F OH XXXI-16-5 p-Me-Ph H H CH 2Ph Et H F F OH XXXI-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H F F OH XXXI-16-7 p-Me-Ph H H CH2CH 2SCH 3 Et H F F OH XXXI-16-8 p-Me-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rQQ-

Table XXXI-17. No R RR 3 a R3b R4 R' R6 X Y XXXI-17-1 p-F-Ph H H H Et H F F OH XXXI-17-2 p-F-Ph H H CH3 Et H F F OH XXXI-17-3 p-F-Ph H H CH(CH3)2 Et H F F OH XXXI-17-4 p-F-Ph H H CH2CH(CH3) 2 Et H F F OH XXXI-17-5 p-F-Ph H H CH 2Ph Et H F F OH XXXI-17-6 p-F-Ph H H CH 2-indol-3-yl Et H F F OH XXXI-17-7 p-F-Ph H H CH2CH 2SCH 3 Et H F F OH XXXI-17-8 p-F-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-18. 9 R1 R2 R3 a R3 b R4 R R6 X Y XXXI-18-1 p-Cl-Ph H H H Et H F F OH XXXI-18-2 p-Cl-Ph H H CH3 Et H F F OH XXXI-18-3 p-Cl-Ph H H CH(CH3) 2 Et H F F OH XXXI-18-4 p-Cl-Ph H H CH2CH(CH3)2 Et H F F OH XXXI-18-5 p-Cl-Ph H H CH2Ph Et H F F OH XXXI-18-6 p-Cl-Ph H H CH2-indol-3-yl Et H F F OH XXXI-18-7 p-Cl-Ph H H CH2CH2SCH 3 Et H F F OH XXXI-18-8 p-Cl-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-19. No R R2 R 3 a R3b R4 RRX Y XXXI-19-1 p-Br-Ph H H H Et H F F OH XXXI-19-2 p-Br-Ph H H CH3 Et H F F OH XXXI-19-3 p-Br-Ph H H CH(CH 3)2 Et H F F OH XXXI-19-4 p-Br-Ph H H CH2CH(CH3) 2 Et H F F OH XXXI-19-5 p-Br-Ph H H CH 2Ph Et H F F OH XXXI-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H F F OH XXXI-19-7 p-Br-Ph H H CH2CH 2SCH 3 Et H F F OH XXXI-19-8 p-Br-Ph * H * Et H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

_Qo-

Table XXXI-20. No R RR 3 a R3b R4 R' R6 X Y XXXI-20-1 p-I-Ph H H H Et H F F OH XXXI-20-2 p-I-Ph H H CH3 Et H F F OH XXXI-20-3 p-I-Ph H H CH(CH3)2 Et H F F OH XXXI-20-4 p-I-Ph H H CH2CH(CH3) 2 Et H F F OH XXXI-20-5 p-I-Ph H H CH 2Ph Et H F F OH XXXI-20-6 p-I-Ph H H CH 2-indol-3-yl Et H F F OH XXXI-20-7 p-I-Ph H H CH2CH 2SCH 3 Et H F F OH XXXI-20-8 p-I-Ph * H * Et H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-21. No R1 R2 R 3a R3 b R4 R 5 R6 X Y XXXI-21-1 CH 3 H H H 'Pr H F F OH XXXI-21-2 CH 3 H H CH3 'Pr H F F OH XXXI-21-3 CH 3 H H CH(CH3) 2 'Pr H F F OH XXXI-21-4 CH 3 H H CH2CH(CH3) 2 'Pr H F F OH XXXI-21-5 CH 3 H H CH 2Ph 'Pr H F F OH XXXI-21-6 CH 3 H H CH 2-indol-3-yl 'Pr H F F OH XXXI-21-7 CH 3 H H CH2CH 2SCH 3 'Pr H F F OH XXXI-21-8 CH 3 * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-22. No Rl R2 R 3a R3b R4 R5 R6 X Y XXXI-22-1 Et H H H 'Pr H F F OH XXXI-22-2 Et H H CH 3 'Pr H F F OH XXXI-22-3 Et H H CH(CH 3)2 'Pr H F F OH XXXI-22-4 Et H H CH 2CH(CH3) 2 'Pr H F F OH XXXI-22-5 Et H H CH 2Ph 'Pr H F F OH XXXI-22-6 Et H H CH 2-indol-3-yl 'Pr H F F OH XXXI-22-7 Et H H CH 2CH 2SCH 3 'Pr H F F OH XXXI-22-8 Et * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ on _

Table XXXI-23. 5 No R1 R2 R3 a R3 R4 R R' X Y XXXI-23-1 'Pr H H H 'Pr H F F OH XXXI-23-2 'Pr H H CH 3 'Pr H F F OH XXXI-23-3 'Pr H H CH(CH3) 2 'Pr H F F OH XXXI-23-4 Pr H H CH 2CH(CH 3)2 'Pr H F F OH XXXI-23-5 Pr H H CH 2Ph 'Pr H F F OH XXXI-23-6 Pr H H CH 2-indol-3-yl 'Pr H F F OH XXXI-23-7 Pr H H CH 2CH2SCH 3 'Pr H F F OH XXXI-23-8 Pr * H * 'Pr H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-24. No R1 R2 R3 a R3 b R4 R R6 X Y XXXI-24-1 'Bu H H H 'Pr H F F OH XXXI-24-2 'Bu H H CH 3 'Pr H F F OH XXXI-24-3 'Bu H H CH(CH3) 2 'Pr H F F OH XXXI-24-4 'Bu H H CH 2CH(CH 3) 2 'Pr H F F OH XXXI-24-5 'Bu H H CH 2Ph 'Pr H F F OH XXXI-24-6 'Bu H H CH 2-indol-3-yl 'Pr H F F OH XXXI-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H F F OH XXXI-24-8 'Bu * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-25. No R1 R2 R 3a R3b R4 R5 R6 X Y XXXI-25-1 Ph H H H 'Pr H F F OH XXXI-25-2 Ph H H CH3 'Pr H F F OH XXXI-25-3 Ph H H CH(CH 3)2 'Pr H F F OH XXXI-25-4 Ph H H CH2CH(CH3) 2 'Pr H F F OH XXXI-25-5 Ph H H CH 2Ph 'Pr H F F OH XXXI-25-6 Ph H H CH 2-indol-3-yl 'Pr H F F OH XXXI-25-7 Ph H H CH2CH 2SCH 3 'Pr H F F OH XXXI-25-8 Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ 01_

Table XXXI-26. No R RR 3 a R3b R4 R' R6 X Y XXXI-26-1 p-Me-Ph H H H 'Pr H F F OH XXXI-26-2 p-Me-Ph H H CH3 'Pr H F F OH XXXI-26-3 p-Me-Ph H H CH(CH 3)2 'Pr H F F OH XXXI-26-4 p-Me-Ph H H CH2CH(CH 3)2 'Pr H F F OH XXXI-26-5 p-Me-Ph H H CH 2Ph 'Pr H F F OH XXXI-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXXI-26-7 p-Me-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXXI-26-8 p-Me-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-27. 9 R1 R2 R3 a R3 b R4 R' R6 X Y XXXI-27-1 p-F-Ph H H H 'Pr H F F OH XXXI-27-2 p-F-Ph H H CH3 'Pr H F F OH XXXI-27-3 p-F-Ph H H CH(CH 3) 2 'Pr H F F OH XXXI-27-4 p-F-Ph H H CH2CH(CH 3) 2 'Pr H F F OH XXXI-27-5 p-F-Ph H H CH 2Ph 'Pr H F F OH XXXI-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXXI-27-7 p-F-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXXI-27-8 p-F-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-28. No R R2 R 3a R 3b R4 R6 X Y

XXXI-28-1 p-Cl-Ph H H H 'Pr H F F OH XXXI-28-2 p-Cl-Ph H H CH3 'Pr H F F OH XXXI-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H F F OH XXXI-28-4 p-Cl-Ph H H CH2CH(CH 3) 2 'Pr H F F OH XXXI-28-5 p-Cl-Ph H H CH2Ph 'Pr H F F OH XXXI-28-6 p-Cl-Ph H H CH2-indol-3-yl 'Pr H F F OH XXXI-28-7 p-Cl-Ph H H CH2CH2SCH 3 'Pr H F F OH XXXI-28-8 p-Cl-Ph * H * Pr H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-29. No R R2 R 3 a R3b R4 R' R6 X Y XXXI-29-1 p-Br-Ph H H H 'Pr H F F OH XXXI-29-2 p-Br-Ph H H CH3 'Pr H F F OH XXXI-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H F F OH XXXI-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H F F OH XXXI-29-5 p-Br-Ph H H CH 2Ph 'Pr H F F OH XXXI-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXXI-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXXI-29-8 p-Br-Ph * H * 'Pr H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-30. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXXI-30-1 p-I-Ph H H H 'Pr H F F OH XXXI-30-2 p-I-Ph H H CH3 'Pr H F F OH XXXI-30-3 p-I-Ph H H CH(CH 3)2 'Pr H F F OH XXXI-30-4 p-I-Ph H H CH2CH(CH3) 2 'Pr H F F OH XXXI-30-5 p-I-Ph H H CH 2Ph 'Pr H F F OH XXXI-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H F F OH XXXI-30-7 p-I-Ph H H CH2CH 2SCH 3 'Pr H F F OH XXXI-30-8 p-I-Ph * H * 'Pr H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-31. No R1 R2 R 3a R3b R4 R 5 R6 X Y XXXI-31-1 CH 3 H H H "Bu H F F OH XXXI-31-2 CH 3 H H CH3 "Bu H F F OH XXXI-31-3 CH3 H H CH(CH3) 2 "Bu H F F OH XXXI-31-4 CH3 H H CH2CH(CH3) 2 "Bu H F F OH XXXI-31-5 CH3 H H CH 2Ph "Bu H F F OH XXXI-31-6 CH3 H H CH 2-indol-3-yl "Bu H F F OH XXXI-31-7 CH3 H H CH2CH 2SCH 3 "Bu H F F OH XXXI-31-8 CH3 * H * "Bu H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

r;02-

Table XXXI-32. No Rl R2 R 3a R3b R4 R' R6 X Y XXXI-32-1 Et H H H "Bu H F F OH XXXI-32-2 Et H H CH 3 "Bu H F F OH XXXI-32-3 Et H H CH(CH3) 2 "Bu H F F OH XXXI-32-4 Et H H CH 2CH(CH3) 2 "Bu H F F OH XXXI-32-5 Et H H CH 2Ph "Bu H F F OH XXXI-32-6 Et H H CH 2-indol-3-yl "Bu H F F OH XXXI-32-7 Et H H CH 2CH 2SCH 3 "Bu H F F OH XXXI-32-8 Et * H * "Bu H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-33. No R1 R2 R 3a Rb R4 R R6 X Y XXXI-33-1 'Pr H H H "Bu H F F OH XXXI-33-2 'Pr H H CH 3 "Bu H F F OH XXXI-33-3 'Pr H H CH(CH 3)2 "Bu H F F OH XXXI-33-4 'Pr H H CH 2CH(CH3)2 "Bu H F F OH XXXI-33-5 'Pr H H CH 2Ph "Bu H F F OH XXXI-33-6 'Pr H H CH 2-indol-3-yl "Bu H F F OH XXXI-33-7 'Pr H H CH 2CH 2SCH 3 "Bu H F F OH XXXI-33-8 'Pr * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-34. No R1 R2 R3a R 3b R4 R R X Y XXXI-34-1 'Bu H H H "Bu H F F OH XXXI-34-2 'Bu H H CH 3 "Bu H F F OH XXXI-34-3 'Bu H H CH(CH3) 2 "Bu H F F OH XXXI-34-4 'Bu H H CH 2CH(CH3)2 "Bu H F F OH XXXI-34-5 'Bu H H CH 2Ph "Bu H F F OH XXXI-34-6 'Bu H H CH 2-indol-3-yl "Bu H F F OH XXXI-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H F F OH XXXI-34-8 'Bu * H * "Bu H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

_ OA _

Table XXXI-35. No R1 R2 R 3a R3b R4 R 5 R6 X Y

XXXI-35-1 Ph H H H "Bu H F F OH XXXI-35-2 Ph H H CH3 "Bu H F F OH XXXI-35-3 Ph H H CH(CH3)2 "Bu H F F OH XXXI-35-4 Ph H H CH2CH(CH3) 2 "Bu H F F OH XXXI-35-5 Ph H H CH 2Ph "Bu H F F OH XXXI-35-6 Ph H H CH 2-indol-3-yl "Bu H F F OH XXXI-35-7 Ph H H CH2CH 2SCH 3 "Bu H F F OH XXXI-35-8 Ph * H * "Bu H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-36. N9 R1 R2 R 3a R3 b R4 R 5 R6 X Y

XXXI-36-1 p-Me-Ph H H H "Bu H F F OH XXXI-36-2 p-Me-Ph H H CH 3 "Bu H F F OH XXXI-36-3 p-Me-Ph H H CH(CH3)2 "Bu H F F OH XXXI-36-4 p-Me-Ph H H CH 2CH(CH3) 2 "Bu H F F OH XXXI-36-5 p-Me-Ph H H CH 2Ph "Bu H F F OH XXXI-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H F F OH XXXI-36-7 p-Me-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXXI-36-8 p-Me-Ph * H * "Bu H F F OH

*R2 and R3 bjoined together by (CH 2) 3 to form five-membered ring.

Table XXXI-37. No R1 R2 R3a R3b R4 R5 R6 X Y XXXI-37-1 p-F-Ph H H H "Bu H F F OH XXXI-37-2 p-F-Ph H H CH 3 "Bu H F F OH XXXI-37-3 p-F-Ph H H CH(CH3)2 "Bu H F F OH XXXI-37-4 p-F-Ph H H CH 2CH(CH3) 2 "Bu H F F OH XXXI-37-5 p-F-Ph H H CH 2Ph "Bu H F F OH XXXI-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H F F OH XXXI-37-7 p-F-Ph H H CH 2CH 2SCH 3 "Bu H F F OH XXXI-37-8 p-F-Ph * H * "Bu H F F OH

*R2 and R3 bjoined together by (CH 2) 3 to form five-membered ring.

Table XXXI-38. No R R2 Ra 3b R4 R 5 R' X Y XXXI-38-1 p-Cl-Ph H H H "Bu H F F OH XXXI-38-2 p-Cl-Ph H H CH3 "Bu H F F OH XXXI-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H F F OH XXXI-38-4 p-Cl-Ph H H CH2CH(CH3)2 "Bu H F F OH XXXI-38-5 p-Cl-Ph H H CH2Ph "Bu H F F OH XXXI-38-6 p-Cl-Ph H H CH2-indol-3-yl "Bu H F F OH XXXI-38-7 p-Cl-Ph H H CH2 CH 2 SCH 3 "Bu H F F OH XXXI-38-8 p-Cl-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-39. N9 R1 R2 R 3a Rb R4 R' R6 X Y XXXI-39-1 p-Br-Ph H H H "Bu H F F OH XXXI-39-2 p-Br-Ph H H CH 3 "Bu H F F OH XXXI-39-3 p-Br-Ph H H CH(CH 3 )2 "Bu H F F OH XXXI-39-4 p-Br-Ph H H CH 2 CH(CH 3)2 "Bu H F F OH XXXI-39-5 p-Br-Ph H H CH 2 Ph "Bu H F F OH XXXI-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H F F OH XXXI-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH XXXI-39-8 p-Br-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-40. No R1 R2 R 3a R3b R4 R 5 R6 X Y XXXI-40-1 p-I-Ph H H H "Bu H F F OH XXXI-40-2 p-I-Ph H H CH 3 "Bu H F F OH XXXI-40-3 p-I-Ph H H CH(CH3)2 "Bu H F F OH XXXI-40-4 p-I-Ph H H CH 2 CH(CH3) 2 "Bu H F F OH XXXI-40-5 p-I-Ph H H CH 2 Ph "Bu H F F OH XXXI-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H F F OH XXXI-40-7 p-I-Ph H H CH 2 CH 2 SCH 3 "Bu H F F OH XXXI-40-8 p-I-Ph * H * "Bu H F F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rQt;-

Table XXXI-41. No R1 R2 R 3a R3b R4 R' R' X Y XXXI-41-1 CH3 H H H Bz H F F OH XXXI-41-2 CH 3 H H CH3 Bz H F F OH XXXI-41-3 CH 3 H H CH(CH3) 2 Bz H F F OH XXXI-41-4 CH 3 H H CH2CH(CH3) 2 Bz H F F OH XXXI-41-5 CH 3 H H CH 2Ph Bz H F F OH XXXI-41-6 CH 3 H H CH 2-indol-3-yl Bz H F F OH XXXI-41-7 CH 3 H H CH2CH 2SCH 3 Bz H F F OH XXXI-41-8 CH 3 * H * Bz H F F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-42. No R1 R2 R3a R3b R4 R' R6 X Y XXXI-42-1 Et H H H Bz H F F OH XXXI-42-2 Et H H CH 3 Bz H F F OH XXXI-42-3 Et H H CH(CH3) 2 Bz H F F OH XXXI-42-4 Et H H CH 2CH(CH3) 2 Bz H F F OH XXXI-42-5 Et H H CH 2Ph Bz H F F OH XXXI-42-6 Et H H CH 2-indol-3-yl Bz H F F OH XXXI-42-7 Et H H CH 2CH 2SCH 3 Bz H F F OH XXXI-42-8 Et * H * Bz H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-43. N R1 R2 R 3a R3 b 4 R 5 R 6 X Y

XXXI-43-1 'Pr H H H Bz H F F OH XXXI-43-2 Pr H H CH 3 Bz H F F OH XXXI-43-3 Pr H H CH(CH3) 2 Bz H F F OH XXXI-43-4 Pr H H CH 2CH(CH 3)2 Bz H F F OH XXXI-43-5 Pr H H CH 2Ph Bz H F F OH XXXI-43-6 'Pr H H CH 2-indol-3-yl Bz H F F OH XXXI-43-7 'Pr H H CH 2CH2SCH 3 Bz H F F dAI XXXI-43-8 'Pr * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-44. 1 RI R 2 R3a R 3 bR4 R5 R6 X Y XXXI-44-1 'Bu H H H Bz H F F OH

No R R2 R3 a R3 b R4 R' R6 X Y XXXI-44-2 'Bu H H CH 3 Bz H F F OH XXXI-44-3 'Bu H H CH(CH3) 2 Bz H F F OH XXXI-44-4 'Bu H H CH 2CH(CH3)2 Bz H F F OH XXXI-44-5 'Bu H H CH 2Ph Bz H F F OH XXXI-44-6 'Bu H H CH 2-indol-3-yl Bz H F F OH XXXI-44-7 'Bu H H CH 2CH 2SCH 3 Bz H F F OH XXXI-44-8 'Bu * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-45. No R R2 R 3a R3b R4 R 5 R6 X Y XXXI-45-1 Ph H H H Bz H F F OH XXXI-45-2 Ph H H CH3 Bz H F F OH XXXI-45-3 Ph H H CH(CH3)2 Bz H F F OH XXXI-45-4 Ph H H CH2CH(CH3) 2 Bz H F F OH XXXI-45-5 Ph H H CH 2Ph Bz H F F OH XXXI-45-6 Ph H H CH 2-indol-3-yl Bz H F F OH XXXI-45-7 Ph H H CH2CH 2SCH 3 Bz H F F OH XXXI-45-8 Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-46. No R R2 R 3 a R3 b R4 R 5 R6 X Y XXXI-46-1 p-Me-Ph H H H Bz H F F OH XXXI-46-2 p-Me-Ph H H CH 3 Bz H F F OH XXXI-46-3 p-Me-Ph H H CH(CH 3)2 Bz H F F OH XXXI-46-4 p-Me-Ph H H CH 2CH(CH 3)2 Bz H F F OH XXXI-46-5 p-Me-Ph H H CH 2Ph Bz H F F OH XXXI-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H F F OH XXXI-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H F F OH XXXI-46-8 p-Me-Ph * H * Bz H F F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

r;QQ-

Table XXXI-47. 5 No R RR 3 a R3b R4 R R' X Y XXXI-47-1 p-F-Ph H H H Bz H F F OH XXXI-47-2 p-F-Ph H H CH3 Bz H F F OH XXXI-47-3 p-F-Ph H H CH(CH 3) 2 Bz H F F OH XXXI-47-4 p-F-Ph H H CH2CH(CH3) 2 Bz H F F OH XXXI-47-5 p-F-Ph H H CH 2Ph Bz H F F OH XXXI-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H F F OH XXXI-47-7 p-F-Ph H H CH2CH 2SCH 3 Bz H F F OH XXXI-47-8 p-F-Ph * H * Bz H F F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXI-48. N9 R1 R2 R3 a R3 b R4 R R6 X Y XXXI-48-1 p-Cl-Ph H H H Bz H F F OH XXXI-48-2 p-Cl-Ph H H CH3 Bz H F F OH XXXI-48-3 p-Cl-Ph H H CH(CH3) 2 Bz H F F OH XXXI-48-4 p-Cl-Ph H H CH2CH(CH3)2 Bz H F F OH XXXI-48-5 p-Cl-Ph H H CH2Ph Bz H F F OH XXXI-48-6 p-Cl-Ph H H CH2-indol-3-yl Bz H F F OH XXXI-48-7 p-Cl-Ph H H CH2CH2SCH 3 Bz H F F OH XXXI-48-8 p-Cl-Ph * H * Bz H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

Table XXXI-49. 5 No R R2 R 3 a R3b R4 R R6 X Y XXXI-49-1 p-Br-Ph H H H Bz H F F OH XXXI-49-2 p-Br-Ph H H CH3 Bz H F F OH XXXI-49-3 p-Br-Ph H H CH(CH3) 2 Bz H F F OH XXXI-49-4 p-Br-Ph H H CH2CH(CH3) 2 Bz H F F OH XXXI-49-5 p-Br-Ph H H CH 2Ph Bz H F F OH XXXI-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H F F OH XXXI-49-7 p-Br-Ph H H CH2CH 2SCH 3 Bz H F F OH XXXI-49-8 p-Br-Ph * H * Bz H F F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

_Qo -

Table XXXI-50. No R RR 3 a R3b R4 R 5 R6 X Y XXXI-50-1 p-I-Ph H H H Bz H F F OH XXXI-50-2 p-I-Ph H H CH3 Bz H F F OH XXXI-50-3 p-I-Ph H H CH(CH 3)2 Bz H F F OH XXXI-50-4 p-I-Ph H H CH2CH(CH 3)2 Bz H F F OH XXXI-50-5 p-I-Ph H H CH 2Ph Bz H F F OH XXXI-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H F F OH XXXI-50-7 p-I-Ph H H CH2CH 2SCH 3 Bz H F F OH XXXI-50-8 p-I-Ph * H * Bz H F F OH

*R2 and R3 joined together by (CH2)3 to form five-membered ring.

0 N

R3b R 2 0 NH

N P 0 0 N R3a N--P- O O | e N 6 NH 2 4 C0 2 R OR' Rs R

Y X XXXII

Table XXXII-1. No R1 R2 R3 a R3 b R4 R5 R 6 X Y XXXII-1-1 CH3 H H H CH3 H H F OH XXXII-1-2 CH3 H H CH3 CH 3 H H F OH XXXII-1-3 CH3 H H CH(CH 3)2 CH 3 H H F OH XXXII-1-4 CH3 H H CH2CH(CH 3) 2 CH 3 H H F OH XXXII-1-5 CH3 H H CH 2Ph CH 3 H H F OH XXXII-1-6 CH3 H H CH 2-indol-3-yl CH 3 H H F OH XXXII-1-7 CH3 H H CH2CH 2SCH 3 CH 3 H H F OH XXXII-1-8 CH3 * H * CH3 H H F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXII-2. No R1 R 2 R3a R 3b R4 RR 6 X Y XXXII-2-1 Et H H H CH3 H H F OH XXXII-2-2 Et H H CH 3 CH3 H H F OH XXXII-2-3 Et H H CH(CH 3)2 CH3 H H F OH XXXII-2-4 Et H H CH 2CH(CH 3) 2 CH3 H H F OH

No Rl R 2 R3 a R3 b R4 RR X Y

XXXII-2-5 Et H H CH 2Ph CH 3 H H F OH XXXII-2-6 Et H H CH 2-indol-3-yl CH 3 H H F OH XXXII-2-7 Et H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-2-8 Et * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-3. No R R2 R3 a Rb R4 R R6 X Y XXXII-3-1 'Pr H H H CH 3 H H F OH XXXII-3-2 'Pr H H CH 3 CH 3 H H F OH XXXII-3-3 'Pr H H CH(CH3) 2 CH 3 H H F OH XXXII-3-4 'Pr H H CH 2CH(CH3)2 CH 3 H H F OH XXXII-3-5 'Pr H H CH 2Ph CH 3 H H F OH XXXII-3-6 'Pr H H CH 2-indol-3-yl CH 3 H H F OH XXXII-3-7 'Pr H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-3-8 Pr * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-4. R No R2 R3a Rb R4 R R6 X Y XXXII-4-1 'Bu H H H CH 3 H H F OH XXXII-4-2 'Bu H H CH 3 CH 3 H H F OH XXXII-4-3 'Bu H H CH(CH3) 2 CH 3 H H F OH XXXII-4-4 'Bu H H CH 2CH(CH3)2 CH 3 H H F OH XXXII-4-5 'Bu H H CH 2Ph CH 3 H H F OH XXXII-4-6 'Bu H H CH 2-indol-3-yl CH 3 H H F OH XXXII-4-7 'Bu H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-4-8 'Bu * H * CH 3 H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-5. 5 6 No R1 R2 R3 a R3 b R4 R R X Y

XXXII-5-1 Ph H H H CH 3 H H F OH XXXII-5-2 Ph H H CH3 CH 3 H H F OH XXXII-5-3 Ph H H CH(CH3)2 CH 3 H H F OH XXXII-5-4 Ph H H CH2CH(CH3) 2 CH 3 H H F OH XXXII-5-5 Ph H H CH 2Ph CH 3 H H F OH XXXII-5-6 Ph H H CH 2-indol-3-yl CH 3 H H F OH XXXII-5-7 Ph H H CH2CH 2SCH 3 CH 3 H H F OH

_ n1 _

No R1 R2 R3 a R3 b R4 R' R6 X Y XXXII-5-8 Ph * H * CH 3 H H F OH *R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXII-6. No R R2 R 3 a R3 b R4 R' R6 X Y XXXII-6-1 p-Me-Ph H H H CH 3 H H F OH XXXII-6-2 p-Me-Ph H H CH 3 CH 3 H H F OH XXXII-6-3 p-Me-Ph H H CH(CH3)2 CH 3 H H F OH XXXII-6-4 p-Me-Ph H H CH 2CH(CH 3) 2 CH 3 H H F OH XXXII-6-5 p-Me-Ph H H CH 2Ph CH 3 H H F OH XXXII-6-6 p-Me-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXXII-6-7 p-Me-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-6-8 p-Me-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-7. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXXII-7-1 p-F-Ph H H H CH 3 H H F OH XXXII-7-2 p-F-Ph H H CH 3 CH 3 H H F OH XXXII-7-3 p-F-Ph H H CH(CH3) 2 CH 3 H H F OH XXXII-7-4 p-F-Ph H H CH 2CH(CH3)2 CH 3 H H F OH XXXII-7-6 p-F-Ph H H CH 2Ph CH 3 H H F OH XXXII-7-7 p-F-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXXII-7-8 p-F-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-7-20 p-F-Ph * H * CH 3 H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-8. No R1 R2 R 3a R3 b R4 R R6 X Y XXXII-8-1 p-Cl-Ph H H H CH 3 H H F OH XXXII-8-2 p-Cl-Ph H H CH 3 CH 3 H H F OH XXXII-8-3 p-Cl-Ph H H CH(CH 3)2 CH 3 H H F OH XXXII-8-4 p-Cl-Ph H H CH 2CH(CH 3)2 CH 3 H H F OH XXXII-8-5 p-Cl-Ph H H CH 2Ph CH 3 H H F OH XXXII-8-6 p-Cl-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXXII-8-7 p-Cl-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-8-8 p-Cl-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXII-9.

No R R2 R 3a R3 b R4 R' R6 X Y XXXII-9-1 p-Br-Ph H H H CH 3 H H F OH XXXII-9-2 p-Br-Ph H H CH 3 CH 3 H H F OH XXXII-9-3 p-Br-Ph H H CH(CH3) 2 CH 3 H H F OH XXXII-9-4 p-Br-Ph H H CH 2CH(CH3) 2 CH 3 H H F OH XXXII-9-6 p-Br-Ph H H CH 2Ph CH 3 H H F OH XXXII-9-7 p-Br-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXXII-9-8 p-Br-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-9-20 p-Br-Ph * H * CH 3 H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-10. N9 Rl R2 R 3a R 3b R4 R' R6 X Y XXXII-10-1 p-I-Ph H H H CH 3 H H F OH XXXII-10-2 p-I-Ph H H CH 3 CH 3 H H F OH XXXII-10-3 p-I-Ph H H CH(CH3) 2 CH 3 H H F OH XXXII-10-4 p-I-Ph H H CH 2CH(CH3)2 CH 3 H H F OH XXXII-10-5 p-I-Ph H H CH 2Ph CH 3 H H F OH XXXII-10-6 p-I-Ph H H CH 2-indol-3-yl CH 3 H H F OH XXXII-10-7 p-I-Ph H H CH 2CH 2SCH 3 CH 3 H H F OH XXXII-10-8 p-I-Ph * H * CH 3 H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-11. R No R2 R 3 a R3 b R4 R R X Y

XXXII-11-1 CH3 H H H Et H H F OH XXXII-11-2 CH3 H H CH 3 Et H H F OH XXXII-11-3 CH3 H H CH(CH3) 2 Et H H F OH XXXII-11-4 CH3 H H CH 2CH(CH3) 2 Et H H F OH XXXII-11-5 CH3 H H CH 2Ph Et H H F OH XXXII-11-6 CH3 H H CH 2-indol-3-yl Et H H F OH XXXII-11-7 CH3 H H CH 2CH 2SCH 3 Et H H F OH XXXII-11-8 CH3 * H * Et H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-12. No Rl R2 R3 a R 3b R4 R R X Y

XXXII-12-1 Et H H H Et H H F OH XXXII-12-2 Et H H CH3 Et H H F OH XXXII-12-3 Et H H CH(CH3)2 Et H H F OH

No Rl R2 R3 a R3 b R4 R R X Y

XXXII-12-4 Et H H CH2CH(CH3) 2 Et H H F OH XXXII-12-5 Et H H CH 2Ph Et H H F OH XXXII-12-6 Et H H CH 2-indol-3-yl Et H H F OH XXXII-12-7 Et H H CH2CH 2SCH 3 Et H H F OH XXXII-12-8 Et * H * Et H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-13. No R R2 R3 a R3 R4 R' R6 X Y XXXII-13-1 'Pr H H H Et H H F OH XXXII-13-2 'Pr H H CH 3 Et H H F OH XXXII-13-3 'Pr H H CH(CH3) 2 Et H H F OH XXXII-13-4 'Pr H H CH 2CH(CH3)2 Et H H F OH XXXII-13-5 'Pr H H CH 2Ph Et H H F OH XXXII-13-6 'Pr H H CH 2-indol-3-yl Et H H F OH XXXII-13-7 Pr H H CH 2CH 2SCH3 Et H H F OH XXXII-13-8 Pr * H * Et H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-14. No R R2 R3 a R3 b R4 R' R6 X Y

XXXII-14-1 'Bu H H H Et H H F OH XXXII-14-2 'Bu H H CH 3 Et H H F OH XXXII-14-3 'Bu H H CH(CH3) 2 Et H H F OH XXXII-14-4 'Bu H H CH 2CH(CH 3) 2 Et H H F OH XXXII-14-5 'Bu H H CH 2Ph Et H H F OH XXXII-14-6 'Bu H H CH 2-indol-3-yl Et H H F OH XXXII-14-7 'Bu H H CH 2CH 2SCH 3 Et H H F OH XXXII-14-8 'Bu * H * Et H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-15. No RI R2 R3a R 3b R4 R5 R6 X Y

XXXII-15-1 Ph H H H Et H H F OH XXXII-15-2 Ph H H CH 3 Et H H F OH XXXII-15-3 Ph H H CH(CH3) 2 Et H H F OH XXXII-15-4 Ph H H CH 2CH(CH3)2 Et H H F OH XXXII-15-5 Ph H H CH 2Ph Et H H F OH XXXII-15-6 Ph H H CH 2-indol-3-yl Et H H F OH

R No R2 R 3a R3 b R4 R' R' X Y XXXII-15-7 Ph H H CH 2CH 2SCH 3 Et H H F OH XXXII-15-8 Ph * H * Et H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-16. No R R2 R 3a R3 b R4 R' R6 X Y XXXII-16-1 p-Me-Ph H H H Et H H F OH XXXII-16-2 p-Me-Ph H H CH 3 Et H H F OH XXXII-16-3 p-Me-Ph H H CH(CH 3)2 Et H H F OH XXXII-16-4 p-Me-Ph H H CH 2CH(CH 3)2 Et H H F OH XXXII-16-5 p-Me-Ph H H CH 2Ph Et H H F OH XXXII-16-6 p-Me-Ph H H CH 2-indol-3-yl Et H H F OH XXXII-16-7 p-Me-Ph H H CH 2CH 2SCH 3 Et H H F OH XXXII-16-8 p-Me-Ph * H * Et H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-17. N9 Rl R2 R 3a R3 b R4 R' R6 X Y XXXII-17-1 p-F-Ph H H H Et H H F OH XXXII-17-2 p-F-Ph H H CH 3 Et H H F OH XXXII-17-3 p-F-Ph H H CH(CH3) 2 Et H H F OH XXXII-17-4 p-F-Ph H H CH 2CH(CH3)2 Et H H F OH XXXII-17-5 p-F-Ph H H CH 2Ph Et H H F OH XXXII-17-6 p-F-Ph H H CH 2-indol-3-yl Et H H F OH XXXII-17-7 p-F-Ph H H CH 2CH 2SCH 3 Et H H F OH XXXII-17-8 p-F-Ph * H * Et H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-18. No R R2 R 3 a R3 b R4 R5 R6 X Y XXXII-18-1 p-Cl-Ph H H H Et H H F OH XXXII-18-2 p-Cl-Ph H H CH 3 Et H H F OH XXXII-18-3 p-Cl-Ph H H CH(CH 3) 2 Et H H F OH XXXII-18-4 p-Cl-Ph H H CH 2CH(CH3) 2 Et H H F OH XXXII-18-5 p-Cl-Ph H H CH 2Ph Et H H F OH XXXII-18-6 p-Cl-Ph H H CH 2-indol-3-yl Et H H F OH XXXII-18-7 p-Cl-Ph H H CH 2CH 2SCH 3 Et H H F OH XXXII-18-8 p-Cl-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rAnr-

Table XXXII-19. No R R2 R 3 a R 3b R4 R R X Y

XXXII-19-1 p-Br-Ph H H H Et H H F OH XXXII-19-2 p-Br-Ph H H CH 3 Et H H F OH XXXII-19-3 p-Br-Ph H H CH(CH3) 2 Et H H F OH XXXII-19-4 p-Br-Ph H H CH 2CH(CH3) 2 Et H H F OH XXXII-19-5 p-Br-Ph H H CH 2Ph Et H H F OH XXXII-19-6 p-Br-Ph H H CH 2-indol-3-yl Et H H F OH XXXII-19-7 p-Br-Ph H H CH 2CH 2SCH 3 Et H H F OH XXXII-19-8 p-Br-Ph * H * Et H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-20. N9 R1 R2 R 3a R3 b R4 R' R6 X Y

XXXII-20-1 p-I-Ph H H H Et H H F OH XXXII-20-2 p-I-Ph H H CH 3 Et H H F OH XXXII-20-3 p-I-Ph H H CH(CH3) 2 Et H H F OH XXXII-20-4 p-I-Ph H H CH 2CH(CH 3)2 Et H H F OH XXXII-20-5 p-I-Ph H H CH 2Ph Et H H F OH XXXII-20-6 p-I-Ph H H CH 2-indol-3-yl Et H H F OH XXXII-20-7 p-I-Ph H H CH 2CH 2SCH 3 Et H H F OH XXXII-20-8 p-I-Ph * H * Et H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-21. N9 R1 R2 R 3 a R 3b R4 R 5 R6 X Y

XXXII-21-1 CH3 H H H 'Pr H H F OH XXXII-21-2 CH3 H H CH 3 'Pr H H F OH XXXII-21-3 CH3 H H CH(CH3) 2 'Pr H H F OH XXXII-21-4 CH3 H H CH 2CH(CH3) 2 'Pr H H F OH XXXII-21-5 CH3 H H CH 2Ph 'Pr H H F OH XXXII-21-6 CH3 H H CH 2-indol-3-yl 'Pr H H F OH XXXII-21-7 CH3 H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-21-8 CH3 * H * 'Pr H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-22. No Rl R2 R3 a R3 b R4 R 5 R6 X Y XXXII-22-1 Et H H H 'Pr H H F OH XXXII-22-2 Et H H CH3 'Pr H H F OH XXXII-22-3 Et H H CH(CH3)2 'Pr H H F OH

rnr-

No Rl R2 R3 a R3 b R4 R' R6 X Y XXXII-22-4 Et H H CH2CH(CH3) 2 'Pr H H F OH XXXII-22-5 Et H H CH 2Ph 'Pr H H F OH XXXII-22-6 Et H H CH 2-indol-3-yl 'Pr H H F OH XXXII-22-7 Et H H CH2CH 2SCH 3 'Pr H H F OH XXXII-22-8 Et * H * 'Pr H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-23. No R R2 R3 a R 3b R4 R R 6 X Y

XXXII-23-1 'Pr H H H 'Pr H H F OH XXXII-23-2 'Pr H H CH 3 'Pr H H F OH XXXII-23-3 'Pr H H CH(CH 3)2 'Pr H H F OH XXXII-23-4 'Pr H H CH 2CH(CH 3) 2 'Pr H H F OH XXXII-23-5 'Pr H H CH 2Ph 'Pr H H F OH XXXII-23-6 'Pr H H CH 2-indol-3-yl 'Pr H H F OH XXXII-23-7 Pr H H CH 2CH 2SCH3 'Pr H H F OH XXXII-23-8 Pr * H * 'Pr H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-24. No R R2 R3 a R3 b R4 R R 6 X Y

XXXII-24-1 'Bu H H H 'Pr H H F OH XXXII-24-2 'Bu H H CH 3 'Pr H H F OH XXXII-24-3 'Bu H H CH(CH3) 2 'Pr H H F OH XXXII-24-4 'Bu H H CH 2CH(CH3) 2 'Pr H H F OH XXXII-24-5 'Bu H H CH 2Ph 'Pr H H F OH XXXII-24-6 'Bu H H CH 2-indol-3-yl 'Pr H H F OH XXXII-24-7 'Bu H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-24-8 'Bu * H * 'Pr H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-25. No R R2 R 3a R 3b R4 R 5 R6 X Y XXXII-25-1 Ph H H H 'Pr H H F OH XXXII-25-2 Ph H H CH 3 'Pr H H F OH XXXII-25-3 Ph H H CH(CH3) 2 'Pr H H F OH XXXII-25-4 Ph H H CH 2CH(CH 3)2 'Pr H H F OH XXXII-25-5 Ph H H CH 2Ph 'Pr H H F OH XXXII-25-6 Ph H H CH 2-indol-3-yl 'Pr H H F OH

Afl'7-

R No R2 R 3a R3 b R4 R' R' X Y XXXII-25-7 Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-25-8 Ph * H * 'Pr H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-26. No R R2 R 3 a R3 b R4 R' R6 X Y XXXII-26-1 p-Me-Ph H H H 'Pr H H F OH XXXII-26-2 p-Me-Ph H H CH 3 'Pr H H F OH XXXII-26-3 p-Me-Ph H H CH(CH 3)2 'Pr H H F OH XXXII-26-4 p-Me-Ph H H CH 2CH(CH3)2 'Pr H H F OH XXXII-26-5 p-Me-Ph H H CH 2Ph 'Pr H H F OH XXXII-26-6 p-Me-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXXII-26-7 p-Me-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-26-8 p-Me-Ph * H * 'Pr H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-27. N9 Rl R2 R 3a R3 b R4 R' R6 X Y XXXII-27-1 p-F-Ph H H H 'Pr H H F OH XXXII-27-2 p-F-Ph H H CH 3 'Pr H H F OH XXXII-27-3 p-F-Ph H H CH(CH 3)2 'Pr H H F OH XXXII-27-4 p-F-Ph H H CH 2CH(CH 3) 2 'Pr H H F OH XXXII-27-5 p-F-Ph H H CH 2Ph 'Pr H H F OH XXXII-27-6 p-F-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXXII-27-7 p-F-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-27-8 p-F-Ph * H * 'Pr H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-28. 6 No R R2 R 3 aRSb R4 R R X Y XXXII-28-1 p-Cl-Ph H H H 'Pr H H F OH XXXII-28-2 p-Cl-Ph H H CH 3 'Pr H H F OH XXXII-28-3 p-Cl-Ph H H CH(CH3) 2 'Pr H H F OH XXXII-28-4 p-Cl-Ph H H CH 2CH(CH3)2 'Pr H H F OH XXXII-28-5 p-Cl-Ph H H CH 2Ph 'Pr H H F OH XXXII-28-6 p-Cl-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXXII-28-7 p-Cl-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-28-8 p-Cl-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXII-29. No R R 2 R 3a R 3b R4 R' R6 X Y XXXII-29-1 p-Br-Ph H H H 'Pr H H F OH XXXII-29-2 p-Br-Ph H H CH3 'Pr H H F OH XXXII-29-3 p-Br-Ph H H CH(CH3) 2 'Pr H H F OH XXXII-29-4 p-Br-Ph H H CH2CH(CH3) 2 'Pr H H F OH XXXII-29-5 p-Br-Ph H H CH 2Ph 'Pr H H F OH XXXII-29-6 p-Br-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXXII-29-7 p-Br-Ph H H CH2CH 2SCH 3 'Pr H H F OH XXXII-29-8 p-Br-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

rno_

Table XXXII-30. No R RR 3 a R 3b R4 R' R' X Y XXXII-30-1 p-I-Ph H H H 'Pr H H F OH XXXII-30-2 p-I-Ph H H CH 3 'Pr H H F OH XXXII-30-3 p-I-Ph H H CH(CH3) 2 'Pr H H F OH XXXII-30-4 p-I-Ph H H CH 2CH(CH 3)2 'Pr H H F OH XXXII-30-5 p-I-Ph H H CH 2Ph 'Pr H H F OH XXXII-30-6 p-I-Ph H H CH 2-indol-3-yl 'Pr H H F OH XXXII-30-7 p-I-Ph H H CH 2CH 2SCH 3 'Pr H H F OH XXXII-30-8 p-I-Ph * H * 'Pr H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-31. No R1 R2 R3a R3b R4 R' R6 X Y XXXII-31-1 CH3 H H H "Bu H H F OH XXXII-31-2 CH3 H H CH 3 "Bu H H F OH XXXII-31-3 CH3 H H CH(CH3) 2 "Bu H H F OH XXXII-31-4 CH3 H H CH 2CH(CH3) 2 "Bu H H F OH XXXII-31-5 CH3 H H CH 2Ph "Bu H H F OH XXXII-31-6 CH3 H H CH 2-indol-3-yl "Bu H H F OH

XXXII-31-7 CH3 H H CH 2CH 2SCH 3 "Bu H H F OH XXXII-31-8 CH3 * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-32. No Rl R2 R3 a R3 b R4 R 5 R6 X Y XXXII-32-1 Et H H H "Bu H H F OH XXXII-32-2 Et H H CH3 "Bu H H F OH XXXII-32-3 Et H H CH(CH3)2 "Bu H H F OH XXXII-32-4 Et H H CH2CH(CH3) 2 "Bu H H F OH XXXII-32-5 Et H H CH 2Ph "Bu H H F OH XXXII-32-6 Et H H CH 2-indol-3-yl "Bu H H F OH XXXII-32-7 Et H H CH2CH 2SCH 3 "Bu H H F OH XXXII-32-8 Et * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-33. 6 No RI 1 R2 R3 a R3 bR 4 R5 R X Y XXXII-33-1 'Pr H H H "Bu H H F OH XXXII-33-2 'Pr H H CH 3 "Bu H H F OH XXXII-33-3 'Pr H H CH(CH 3)2 "Bu H H F OH

f1l-

R No R2 R3 a R3 b R4 R' R' X Y XXXII-33-4 'Pr H H CH 2CH(CH3)2 "Bu H H F OH XXXII-33-5 'Pr H H CH 2Ph "Bu H H F OH XXXII-33-6 'Pr H H CH 2-indol-3-yl "Bu H H F OH XXXII-33-7 'Pr H H CH 2CH 2SCH3 "Bu H H F OH XXXII-33-8 'Pr * H * "Bu H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-34. 6 No RI R2 R3 a R3b R4 R R X Y XXXII-34-1 'Bu H H H "Bu H H F OH XXXII-34-2 'Bu H H CH 3 "Bu H H F OH XXXII-34-3 'Bu H H CH(CH3) 2 "Bu H H F OH XXXII-34-4 'Bu H H CH 2CH(CH3)2 "Bu H H F OH XXXII-34-5 'Bu H H CH 2Ph "Bu H H F OH XXXII-34-6 'Bu H H CH 2-indol-3-yl "Bu H H F OH XXXII-34-7 'Bu H H CH 2CH 2SCH 3 "Bu H H F OH XXXII-34-8 'Bu * H * "Bu H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-35. 5 No Rl R2 R3a R3b R4 R R6 X Y XXXII-35-1 Ph H H H "Bu H H F OH XXXII-35-2 Ph H H CH 3 "Bu H H F OH XXXII-35-3 Ph H H CH(CH 3)2 "Bu H H F OH XXXII-35-4 Ph H H CH 2CH(CH 3 )2 "Bu H H F OH XXXII-35-5 Ph H H CH 2Ph "Bu H H F OH XXXII-35-6 Ph H H CH 2-indol-3-yl "Bu H H F OH XXXII-35-7 Ph H H CH 2CH 2 SCH 3 "Bu H H F OH XXXII-35-8 Ph * H * "Bu H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

_~ A11

Table XXXII-36. No R RR 3 a R 3b R4 R' R6 X Y XXXII-36-1 p-Me-Ph H H H "Bu H H F OH XXXII-36-2 p-Me-Ph H H CH 3 "Bu H H F OH XXXII-36-3 p-Me-Ph H H CH(CH 3)2 "Bu H H F OH XXXII-36-4 p-Me-Ph H H CH 2CH(CH 3)2 "Bu H H F OH XXXII-36-5 p-Me-Ph H H CH 2Ph "Bu H H F OH XXXII-36-6 p-Me-Ph H H CH 2-indol-3-yl "Bu H H F OH XXXII-36-7 p-Me-Ph H H CH 2CH 2 SCH 3 "Bu H H F OH XXXII-36-8 p-Me-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-37. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXXII-37-1 p-F-Ph H H H "Bu H H F OH XXXII-37-2 p-F-Ph H H CH 3 "Bu H H F OH XXXII-37-3 p-F-Ph H H CH(CH 3 )2 "Bu H H F OH XXXII-37-4 p-F-Ph H H CH 2 CH(CH 3) 2 "Bu H H F OH XXXII-37-5 p-F-Ph H H CH 2 Ph "Bu H H F OH XXXII-37-6 p-F-Ph H H CH 2-indol-3-yl "Bu H H F OH XXXII-37-7 p-F-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH XXXII-37-8 p-F-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-38. No R1 R2 R3 a R3b R4 RR X Y XXXII-38-1 p-Cl-Ph H H H "Bu H H F OH XXXII-38-2 p-Cl-Ph H H CH 3 "Bu H H F OH XXXII-38-3 p-Cl-Ph H H CH(CH3) 2 "Bu H H F OH XXXII-38-4 p-Cl-Ph H H CH 2 CH(CH3)2 "Bu H H F OH XXXII-38-5 p-Cl-Ph H H CH 2Ph "Bu H H F OH XXXII-38-6 p-Cl-Ph H H CH 2-indol-3-yl "Bu H H F OH XXXII-38-7 p-Cl-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH XXXII-38-8 p-Cl-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

rAl')-

Table XXXII-39. No R R2 R 3 a R 3b R4 R' R6 X Y XXXII-39-1 p-Br-Ph H H H "Bu H H F OH XXXII-39-2 p-Br-Ph H H CH3 "Bu H H F OH XXXII-39-3 p-Br-Ph H H CH(CH3) 2 "Bu H H F OH XXXII-39-4 p-Br-Ph H H CH2CH(CH3) 2 "Bu H H F OH XXXII-39-5 p-Br-Ph H H CH 2Ph "Bu H H F OH XXXII-39-6 p-Br-Ph H H CH 2-indol-3-yl "Bu H H F OH XXXII-39-7 p-Br-Ph H H CH 2 CH 2 SCH 3 "Bu H H F OH XXXII-39-8 p-Br-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-40. N9 R1 R2 R 3a R3 b R4 R' R6 X Y XXXII-40-1 p-I-Ph H H H "Bu H H F OH XXXII-40-2 p-I-Ph H H CH 3 "Bu H H F OH XXXII-40-3 p-I-Ph H H CH(CH 3)2 "Bu H H F OH XXXII-40-4 p-I-Ph H H CH 2CH(CH 3)2 "Bu H H F OH XXXII-40-5 p-I-Ph H H CH 2Ph "Bu H H F OH XXXII-40-6 p-I-Ph H H CH 2-indol-3-yl "Bu H H F OH XXXII-40-7 p-I-Ph H H CH 2CH 2SCH 3 "Bu H H F OH XXXII-40-8 p-I-Ph * H * "Bu H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-41. No R1 R2 R 3 a R 3b R4 R 5 R6 X Y XXXII-41-1 CH3 H H H Bz H H F OH XXXII-41-2 CH3 H H CH 3 Bz H H F OH XXXII-41-3 CH3 H H CH(CH3) 2 Bz H H F OH XXXII-41-4 CH3 H H CH 2CH(CH3) 2 Bz H H F OH XXXII-41-5 CH3 H H CH 2Ph Bz H H F OH XXXII-41-6 CH3 H H CH 2-indol-3-yl Bz H H F OH XXXII-41-7 CH3 H H CH 2CH 2SCH 3 Bz H H F OH XXXII-41-8 CH3 * H * Bz H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

rAl21

Table XXXII-42. No Rl R2 R3 a R 3b R4 R 5 R' X Y XXXII-42-1 Et H H H Bz H H F OH XXXII-42-2 Et H H CH3 Bz H H F OH XXXII-42-3 Et H H CH(CH3)2 Bz H H F OH XXXII-42-4 Et H H CH2CH(CH3) 2 Bz H H F OH XXXII-42-5 Et H H CH 2Ph Bz H H F OH XXXII-42-6 Et H H CH 2-indol-3-yl Bz H H F OH XXXII-42-7 Et H H CH2CH 2SCH 3 Bz H H F OH XXXII-42-8 Et * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-43. No R R2 R3 a Rb R4 R R6 X Y XXXII-43-1 'Pr H H H Bz H H F OH XXXII-43-2 'Pr H H CH 3 Bz H H F OA XXXII-43-3 'Pr H H CH(CH 3) 2 Bz H H F OH XXXII-43-4 'Pr H H CH 2CH(CH 3) 2 Bz H H F OH XXXII-43-5 'Pr H H CH 2Ph Bz H H F OH XXXII-43-6 'Pr H H CH 2-indol-3-yl Bz H H F OH XXXII-43-7 'Pr H H CH 2CH 2SCH3 Bz H H F OH XXXII-43-8 'Pr * H * Bz H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-44. No R R2 R3 a R3 b R4 R R6 X Y XXXII-44-1 'Bu H H H Bz H H F OH XXXII-44-2 'Bu H H CH 3 Bz H H F OH XXXII-44-3 'Bu H H CH(CH3) 2 Bz H H F OH XXXII-44-4 'Bu H H CH 2CH(CH3)2 Bz H H F OH XXXII-44-5 'Bu H H CH 2Ph Bz H H F OH XXXII-44-6 'Bu H H CH 2-indol-3-yl Bz H H F OH XXXII-44-7 'Bu H H CH 2CH2SCH 3 Bz H H F OH XXXII-44-8 'Bu * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-45. No R R2 R 3a R3 b R4 R5 R6 X Y XXXII-45-1 Ph H H H Bz H H F OH

_ 11A

No R R2 R 3a R3 b R4 R R6 X Y XXXII-45-2 Ph H H CH 3 Bz H H F OH XXXII-45-3 Ph H H CH(CH3) 2 Bz H H F OH XXXII-45-4 Ph H H CH 2CH(CH3)2 Bz H H F OH XXXII-45-5 Ph H H CH 2Ph Bz H H F OH XXXII-45-6 Ph H H CH 2-indol-3-yl Bz H H F OH XXXII-45-7 Ph H H CH 2CH 2SCH 3 Bz H H F OH XXXII-45-8 Ph * H * Bz H H F OH

*R2 and R3 joined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-46. No R R2 R 3 a R 3b R4 R 5 R6 X Y XXXII-46-1 p-Me-Ph H H H Bz H H F OH XXXII-46-2 p-Me-Ph H H CH 3 Bz H H F OH XXXII-46-3 p-Me-Ph H H CH(CH 3)2 Bz H H F OH XXXII-46-4 p-Me-Ph H H CH 2CH(CH 3)2 Bz H H F OH XXXII-46-5 p-Me-Ph H H CH 2Ph Bz H H F OH XXXII-46-6 p-Me-Ph H H CH 2-indol-3-yl Bz H H F OH XXXII-46-7 p-Me-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXXII-46-8 p-Me-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-47. No R R2 R 3 a R3 b R4 R 5 R6 X Y XXXII-47-1 p-F-Ph H H H Bz H H F OH XXXII-47-2 p-F-Ph H H CH 3 Bz H H F OH XXXII-47-3 p-F-Ph H H CH(CH 3)2 Bz H H F OH XXXII-47-4 p-F-Ph H H CH 2CH(CH 3) 2 Bz H H F OH XXXII-47-5 p-F-Ph H H CH 2Ph Bz H H F OH XXXII-47-6 p-F-Ph H H CH 2-indol-3-yl Bz H H F OH XXXII-47-7 p-F-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXXII-47-8 p-F-Ph * H * Bz H H F OH

*R2 and R3 bjoined together by (CH 2 ) 3 to form five-membered ring.

Table XXXII-48. No R R2 R 3 a R3b R4 R R X Y

XXXII-48-1 p-Cl-Ph H H H Bz H H F OH XXXII-48-2 p-Cl-Ph H H CH 3 Bz H H F OH XXXII-48-3 p-Cl-Ph H H CH(CH 3)2 Bz H H F OH XXXII-48-4 p-Cl-Ph H H CH 2CH(CH3) 2 Bz H H F OH

rl' 1-r

No R R2 R 3 a R3 b R4 R R6 X Y XXXII-48-5 p-Cl-Ph H H CH 2Ph Bz H H F OH XXXII-48-6 p-Cl-Ph H H CH 2-indol-3-yl Bz H H F OH XXXII-48-7 p-Cl-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXXII-48-8 p-Cl-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXII-49. N9 Rl R2 R 3a R3 b R4 R' R6 X Y XXXII-49-1 p-Br-Ph H H H Bz H H F OH XXXII-49-2 p-Br-Ph H H CH 3 Bz H H F OH XXXII-49-3 p-Br-Ph H H CH(CH3) 2 Bz H H F OH XXXII-49-4 p-Br-Ph H H CH 2CH(CH3) 2 Bz H H F OH XXXII-49-5 p-Br-Ph H H CH 2Ph Bz H H F OH XXXII-49-6 p-Br-Ph H H CH 2-indol-3-yl Bz H H F OH XXXII-49-7 p-Br-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXXII-49-8 p-Br-Ph * H * Bz H H F OH

*R2 and R3bjoined together by (CH2)3 to form five-membered ring.

Table XXXII-50. No R R2 R 3 a R3 b R4 R5 R6 X Y XXXII-50-1 p-I-Ph H H H Bz H H F OH XXXII-50-2 p-I-Ph H H CH 3 Bz H H F OH XXXII-50-3 p-I-Ph H H CH(CH3) 2 Bz H H F OH XXXII-50-4 p-I-Ph H H CH 2CH(CH 3)2 Bz H H F OH XXXII-50-5 p-I-Ph H H CH 2Ph Bz H H F OH XXXII-50-6 p-I-Ph H H CH 2-indol-3-yl Bz H H F OH XXXII-50-7 p-I-Ph H H CH 2CH 2SCH 3 Bz H H F OH XXXII-50-8 p-I-Ph * H * Bz H H F OH

*R2 and R3 bjoined together by (CH2)3 to form five-membered ring.

rl -

DOSAGE, ADMINISTRATION, AND USE

A sixth embodiment of the present invention is directed to a composition for the treatment of any of the viral agents disclosed herein said composition comprising a pharmaceutically acceptable medium selected from among an excipient, carrier, diluent, and equivalent medium and a compound, that is intended to include its salts (acid or basic addition salts), hydrates, solvates, and crystalline forms can be obtained, represented by formula I.

It is contemplated that the formulation of the sixth embodiment can contain any of the compounds contemplated in any of the aspects of the first, second, third, fourth, and fifth embodiments or those specifically recited in the tables above or exemplified herein, either alone or in combination with another compound of the present invention.

The compounds of the present invention may be formulated in a wide variety of oral administration dosage forms and carriers. Oral administration can be in the form of tablets, coated tablets, hard and soft gelatin capsules, solutions, emulsions, syrups, or suspensions. Compounds of the present invention are efficacious when administered by suppository administration, among other routes of administration. The most convenient manner of administration is generally oral using a convenient daily dosing regimen which can be adjusted according to the severity of the disease and the patient's response to the antiviral medication.

A compound or compounds of the present invention, as well as their pharmaceutically acceptable salts, together with one or more conventional excipients, carriers, or diluents, may be placed into the form of pharmaceutical compositions and unit dosages. The pharmaceutical compositions and unit dosage forms may be comprised of conventional ingredients in conventional proportions, with or without additional active compounds and the unit dosage forms may contain any suitable effective amount of the active ingredient commensurate with the intended daily dosage range to be employed. The pharmaceutical compositions may be employed as solids, such as tablets or filled capsules, semisolids, powders, sustained release formulations, or liquids such as suspensions, emulsions, or filled capsules for oral use; or in the form of suppositories for rectal or vaginal administration. A typical preparation will contain from about 5% to about 95% active compound or compounds (w/w). The term "preparation" or "dosage form" is intended to include both solid and liquid formulations of the active compound and one skilled in the art will appreciate that an active ingredient can exist in different preparations depending on the desired dose and pharmacokinetic parameters.

S 1'7 _

The term "excipient" as used herein refers to a compound that is used to prepare a pharmaceutical composition, and is generally safe, non-toxic and neither biologically nor otherwise undesirable, and includes excipients that are acceptable for veterinary use as well as human pharmaceutical use. The compounds of this invention can be administered alone but will generally be administered in admixture with one or more suitable pharmaceutical excipients, diluents or carriers selected with regard to the intended route of administration and standard pharmaceutical practice.

A "pharmaceutically acceptable salt" form of an active ingredient may also initially confer a desirable pharmacokinetic property on the active ingredient which were absent in the non salt form, and may even positively affect the pharmacodynamics of the active ingredient with respect to its therapeutic activity in the body. The phrase "pharmaceutically acceptable salt" of a compound as used herein means a salt that is pharmaceutically acceptable and that possesses the desired pharmacological activity of the parent compound. Such salts include: (1) acid addition salts, formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like; or formed with organic acids such as glycolic acid, pyruvic acid, lactic acid, malonic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, 3-(4-hydroxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2 hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2 naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, lauryl sulfuric acid, gluconic acid, glutamic acid, salicylic acid, muconic acid, and the like or (2) basic addition salts formed with the conjugate bases of any of the inorganic acids listed above, wherein the conjugate bases comprise a cationic component selected from among Na', K, Mg2 , Ca2 +, and NHgR'4-g*, in which R is a C1-3 alkyl and g is a number selected from among 0, 1, 2, 3, or 4. It should be understood that all references to pharmaceutically acceptable salts include solvent addition forms (solvates) or crystal forms (polymorphs) as defined herein, of the same acid addition salt.

Solid form preparations include powders, tablets, pills, capsules, suppositories, and dispersible granules. A solid carrier may be one or more substances which may also act as diluents, flavoring agents, solubilizers, lubricants, suspending agents, binders, preservatives, tablet disintegrating agents, or an encapsulating material. In powders, the carrier generally is a finely divided solid which is a mixture with the finely divided active component. In tablets, the active component generally is mixed with the carrier having the necessary binding capacity in suitable proportions and compacted in the shape and size desired. Suitable carriers include but are not limited to magnesium carbonate, magnesium stearate,

2 -1 talc, sugar, lactose, pectin, dextrin, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose, a low melting wax, cocoa butter, and the like. Solid form preparations may contain, in addition to the active component, colorants, flavors, stabilizers, buffers, artificial and natural sweeteners, dispersants, thickeners, solubilizing agents, and the like.

Liquid formulations also are suitable for oral administration include liquid formulation including emulsions, syrups, elixirs and aqueous suspensions. These include solid form preparations which are intended to be converted to liquid form preparations shortly before use. Emulsions may be prepared in solutions, for example, in aqueous propylene glycol solutions or may contain emulsifying agents such as lecithin, sorbitan monooleate, or acacia. Aqueous suspensions can be prepared by dispersing the finely divided active component in water with viscous material, such as natural or synthetic gums, resins, methylcellulose, sodium carboxymethylcellulose, and other well known suspending agents.

The compounds of the present invention may be formulated for administration as suppositories. A low melting wax, such as a mixture of fatty acid glycerides or cocoa butter is first melted and the active component is dispersed homogeneously, for example, by stirring. The molten homogeneous mixture is then poured into convenient sized molds, allowed to cool, and to solidify.

The compounds of the present invention may be formulated for vaginal administration. Pessaries, tampons, creams, gels, pastes, foams or sprays containing in addition to the active ingredient such carriers as are known in the art to be appropriate.

Suitable formulations along with pharmaceutical carriers, diluents and expcipients are described in Remington: The Science and PracticeofPharmacy 1995, edited by E. W. Martin, Mack Publishing Company, 19th edition, Easton, Pennsylvania, which is hereby incorporated by reference. The compounds of the present invention can also be encapsulated in liposomes, such as those disclosed in U.S. Patent Nos. 6,180,134, 5,192,549, 5,376,380, 6,060,080, 6,132,763, each of which is incorporated by reference. A skilled formulation scientist may modify the formulations within the teachings of the specification to provide numerous formulations for a particular route of administration without rendering the compositions of the present invention unstable or compromising their therapeutic activity.

The modification of the present compounds to render them more soluble in water or other vehicle, for example, may be easily accomplished by minor modifications (e.g., salt

_, 1 O formulation), which are well within the ordinary skill in the art. It is also well within the ordinary skill of the art to modify the route of administration and dosage regimen of a particular compound in order to manage the pharmacokinetics of the present compounds for maximum beneficial effect in patients.

A seventh embodiment of the present invention is directed to a use of the compound represented by formula I in the manufacture of a medicament for the treatment of any condition the result of an infection by any one of the following viral agents: hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus and Japanese encephalitis virus.

The term "medicament" means a substance used in a method of treatment and/or prophylaxis of a subject in need thereof, wherein the substance includes, but is not limited to, a composition, a formulation, a dosage form, and the like, comprising the compound of formula I. It is contemplated that the compound of the use of the compound represented by formula I in the manufacture of a medicament for the treatment of any of the antiviral conditions disclosed herein of the seventh embodiment can be any of the compounds contemplated in any of the aspects of the first, second, third, fourth, fifth embodiments or those specifically recited in the tables above or exemplified herein, either alone or in combination with another compound of the present invention. A medicament includes, but is not limited to, any one of the compositions contemplated by the sixth embodiment of the present invention.

A eighth embodiment of the present invention is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering a therapeutically effective amount of the compound represented by formula I to the subject.

A first aspect of the eighth embodiment is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering a therapeutically effective of at least two or more different compounds falling within the scope of the compound represented by formula I to the subject.

A second aspect of the eighth embodiment is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of at least two compounds falling within the scope of the compound represented by formula I to the subject.

It is intended that a subject in need thereof is one that has any condition the result of an infection by any of the viral agents disclosed herein, which includes, but is not limited to, hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus or Japanese encephalitis virus, flaviviridae viruses or pestiviruses or hepaciviruses or a viral agent causing symptoms equivalent or comparable to any of the above-listed viruses.

The term "subject" means a mammal, which includes, but is not limited to, cattle, pigs, sheep, chicken, turkey, buffalo, llama, ostrich, dogs, cats, and humans, preferably the subject is a human. It is contemplated that in the method of treating a subject thereof of the sixth embodiment can be any of the compounds contemplated in any of the aspects of the first, second, and third embodiments or those specifically recited in the tables above, either alone or in combination with another compound of the present invention.

The term "therapeutically effective amount" as used herein means an amount required to reduce symptoms of the disease in an individual. The dose will be adjusted to the individual requirements in each particular case. That dosage can vary within wide limits depending upon numerous factors such as the severity of the disease to be treated, the age and general health condition of the patient, other medicaments with which the patient is being treated, the route and form of administration and the preferences and experience of the medical practitioner involved. For oral administration, a daily dosage of between about 0.1 and about 10 g, including all values in between, such as 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, and 9.5, per day should be appropriate in monotherapy and/or in combination therapy. A preferred daily dosage is between about 0.5 and about 7.5 g per day, more preferred 1.5 and about 6.0 g per day. Generally, treatment is initiated with a large initial "loading dose" to rapidly reduce or eliminate the virus following by a decreasing the dose to a level sufficient to prevent resurgence of the infection. One of ordinary skill in treating diseases described herein will be able, without undue experimentation and in reliance on personal knowledge, experience and the disclosures of this application, to ascertain a therapeutically effective amount of the compounds of the present invention for a given disease and patient.

Therapeutic efficacy can be ascertained from tests of liver function including, but not limited to protein levels such as serum proteins (e.g., albumin, clotting factors, alkaline phosphatase, aminotransferases (e.g., alanine transaminase, aspartate transaminase), 5' nucleosidase, y-glutaminyltranspeptidase, etc.), synthesis of bilirubin, synthesis of cholesterol, and synthesis of bile acids; a liver metabolic function, including, but not limited to, carbohydrate metabolism, amino acid and ammonia metabolism. Alternatively the

_ G) 1_ therapeutic effectiveness may be monitored by measuring HCV-RNA. The results of these tests will allow the dose to be optimized.

A third aspect of the eighth embodiment, is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering to the subject a therapeutically effective of a compound represented by formula I and a therapeutically effective amount of another antiviral agent; wherein the administration is concurrent or alternative. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours. Examples of "another antiviral agents" include, but are not limited to: HCV NS3 protease inhibitors (see WO 2008010921, WO 2008010921, EP 1881001, WO 2007015824, WO 2007014925, WO 2007014926, WO 2007014921, WO 2007014920, WO 2007014922, US 2005267018, WO 2005095403, WO 2005037214, WO 2004094452, US 2003187018, WO 200364456, WO 2005028502, and WO 2003006490); HCV NS5B Inhibitors (see US 2007275947, US20072759300, W02007095269, WO 2007092000, WO 2007076034, WO 200702602, US 2005-98125, WO 2006093801, US 2006166964, WO 2006065590, WO 2006065335, US 2006040927, US 2006040890, WO 2006020082, WO 2006012078, WO 2005123087, US 2005154056, US 2004229840, WO 2004065367, WO 2004003138, WO 2004002977, WO 2004002944, WO 2004002940, WO 2004000858, WO 2003105770, WO 2003010141, WO 2002057425, WO 2002057287, WO 2005021568, WO 2004041201, US 20060293306, US 20060194749, US 20060241064, US 6784166, WO 2007088148, WO 2007039142, WO 2005103045, WO 2007039145, WO 2004096210, and WO 2003037895); HCV NS4 Inhibitors (see WO 2007070556 and WO 2005067900); HCV NS5a Inhibitors (see US 2006276511, WO 2006120252, WO 2006120251, WO 2006100310, WO 2006035061); Toll-like receptor agonists (seeWO 2007093901); and other inhibitors (see WO 2004035571, WO 2004014852, WO 2004014313, WO 2004009020, WO 2003101993, WO 2000006529).

A fourth aspect of the eighth embodiment, is directed to a method of treatment in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of a compound represented by formula I and another antiviral agent to the subject. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours.

r11)-

A fifth aspect of the eighth embodiment, is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering to the subject a therapeutically effective of at least one compound represented by formula I and a therapeutically effective amount of another antiviral agent; wherein the administration is concurrent or alternative. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours.

A sixth aspect of the eighth embodiment, is directed to a method of treatment in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of at least one compound represented by formula I and another antiviral agent to the subject. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours.

It is contemplated that the another antiviral agent includes, but is not limited to interferon , interferon-p, pegylated interferon-c, ribavirin, levovirin, viramidine, another nucleoside HCV polymerase inhibitor, a HCV non-nucleoside polymerase inhibitor, a HCV protease inhibitor, a HCV helicase inhibitor or a HCV fusion inhibitor. When the active compound or its derivative or salt are administered in combination with another antiviral agent the activity may be increased over the parent compound. When the treatment is combination therapy, such administration may be concurrent or sequential with respect to that of the nucleoside derivatives. "Concurrent administration" as used herein thus includes administration of the agents at the same time or at different times. Administration of two or more agents at the same time can be achieved by a single formulation containing two or more active ingredients or by substantially simultaneous administration of two or more dosage forms with a single active agent.

It will be understood that references herein to treatment extend to prophylaxis as well as to the treatment of existing conditions. Furthermore, the term "treatment" of a HCV infection, as used herein, also includes treatment or prophylaxis of a disease or a condition associated with or mediated by HCV infection, or the clinical symptoms thereof.

PROCESS FOR PREPARATION

An ninth embodiment of the present invention is directed to a process for preparing the compound of formula I, which comprises reacting a suitably substituted phosphochloridate compound 4 with a nucleoside analog 5

3a 3 R R b RI

HO Base R N X' o 0

4 5

wherein the substituents R, R2, R3a, R, R4, R', X , Y, R, and base have their meanings as disclosed in the Detailed Description of the Invention and X' is a leaving group, such as Cl, Br, I, tosylate, mesylate, trifluoroacetate, trifluorosulfonate, pentafluorophenoxide, p-N02 phenoxide, or other commonly used leaving groups as disclosed in Advanced Organic Chemistry by March, Fourth Edition. Leaving groups and methods that can be used to effect the formation of a phosphoramidate nucleoside conjugate are found in US 20060142238 and WO 2007095269. Preferably, the leaving group is Cl.

This reaction is performed in an anhydrous aprotic solvent such tetrahydrofuran, dioxane, or both tetrahydrofuran and dioxane, or any functional equivalent thereof, with tetrahydrofuran being the preferred solvent. The reaction is typically initiated at a temperature range from 78°C to 40°C with the preferred reaction temperature being between 0°C and room temperature. The nucleoside is first stirred with a base (5 to 12 equivalents) such as N methylimidazole, collidine, pyridine, 2,6-lutidine, 2, 6-Bu-pyridine, etc. a tertiary amine base, such as triethylamine, diisopropylethylamine, etc., or an alkyl Grignard reagent, such as tBuMgCl, tBuMgBr, MeMgCl, MeMgBr, etc. The phosphorochloridate (3-10 equivalents) is dissolved in the reaction solvent and added to the mixture of the nucleoside and base. The reaction is then allowed to stir over a period of time at a temperature between room temperature and 40°C for a period of 30 min to 24 hr. with the preferred reaction temperature being room temperature and time being 24 hr. The solvent is removed from the reaction mixture and the product is purified by chromatography on silica gel.

A tenth embodiment of the present invention is directed to a product obtained by a process which comprises reacting a suitably substituted phosphochloridate compound 4 with a nucleoside analog 5

3a 3 R R b R H

HO Base O X 6 RY2 X R

4 5

wherein the substituents R, R2,R 3a, R, R4, R', X, Y, R, X', and base have their meanings as disclosed in the Detailed Description of the Invention.

_ ( A

This reaction can be performed in an anhydrous aprotic solvent or other suitable solvent, such as tetrahydrofuran, dioxane, or a mixture of tetrahydrofuran and dioxane, with tetrahydrofuran being the preferred solvent. The reaction is typically initiated at a temperature range from -78°C to 40°C with the preferred reaction temperature being between 0°C and room temperature. The nucleoside is first stirred with a base (5 to 12 equivalents) such as N-methylimidazole, a tertiary amine base or tButyl Magnesium Chloride. A phosphorochloridate (3-10 equivalents (or suitable "phosphoro-(leaving group) date")) is dissolved in the reaction solvent and added to the mixture of the nucleoside and base. The reaction is then allowed to stir over a period of time at a temperature between room temperature and 40°C for a period of 30 min to 24 hr. with the preferred reaction temperature being room temperature and time being 24 hr. The solvent is removed from the reaction mixture and the product is purified by chromatography on silica gel.

Compounds and Preparation

Phosphoramidate compounds of the present invention can be prepared by condensation of a

nucleoside analog 5 with a suitably substituted phosphochloridate compound 4 (Scheme 1).

The nucleoside analog is made by conventional procedures disclosed in any one of U.S.

Published Application Nos. 2005/0009737, 2006/0199783, 2006/0122146, and

2007/0197463, each of which is incorporated by reference in its entirety.

Disclosed 1H-NMR values were recorded on a Varian AS-400 instrument. Mass spectral

data were obtain using either a Micromass-Quattromicro API or a Waters Acquity.

Thus, by way of example only, a suitably substituted phenol can be reacted with phosphorus

oxychloride (1) to afford an aryloxy phosphorodichloridate 2 (see Example 1) which is

subsequently treated with a acid addition salt of an a-amino acid ester in the presence of

TEA to afford an aryloxy phosphorochloridate 4. This arylalkoxy-amino acid

phosphoramidate is reacted with the nucleoside analog to provide the product I (for

procedure see, e.g., C. McGuigan et al. Antiviral Res. 1992 17:311-321; D. Curley et al.

Antiviral Res. 1990 14:345-356; McGuigan et al. Antiviral Chem. Chemother 1990

1(2):107-113).

Scheme 1

R 3a R b 3

,R1 / NHA- 3 CI oR 4 0 I CI--CI CI-I --I O o A- = CI-or Ts 1 2

R3$3b R1 HO * X Base N1 I R3b . Bs -P-CW D 1 B 4 R10 R4 0 120 5 R 5 RR X R6

* 4

The preparation of nucleoside phosphoramidates requires reacting an appropriately substituted phosphochloridate with a nucleoside containing a free 5'-hydroxyl moiety. In cases where only one hydroxyl group is present, preparation of the phosphoramidate usually proceeds smoothly when the phosphochloridate is reacted with the desired nucleoside. In cases where the nucleoside contains more than one free hydroxyl group, preparation of the appropriately protected nucleoside might be required. Silyl, acetonide or other alcohol protecting groups known in the art might be warranted for protection of the sugar moiety. For protection of the nucleoside base, protecting a free amino group may require amidine protection strategy.

Condensation of the phosphochloridate can be carried out on the unprotected nucleoside. Since the 5'-OH group of a nucleoside is much less hindered than the3'-OH group, selective phosphoramidation is possible under carefully controlled conditions. After condensation to form a protected phosphoramidate nucleoside, deprotection to obtain the free phosphoramidate nucleoside can be carried out using standard protocols for nucleic acid chemistry. In many cases, the desired product is readily separated from the starting material using column chromatography on silica gel. The synthetic scheme is summarized in Scheme 1.

A further understanding of the disclosed embodiments will be appreciated by consideration of the following examples, which are only meant to be illustrative, and not limit the disclosed invention.

EXAMPLE

General Procedure for Preparation of phosphorodichloridates

-R1

CI-P-CI + R 1-OH CI-P-CI 0 0 1 2

A solution of the appropriate phenol R'-OH (leq) and triethylamine (1 eq.) in anhydrous

ether was added dropwise to a stirred solution of phosphoryl trichloride 1 (leq) at 0 °C over

a period of 3 hours under nitrogen. Then the temperature was warmed to room temperature,

and the reaction was stirred overnight. The triethylamine salt was quickly removed with

suction filtration and the filtrate concentrated in vacuo to dryness to afford 2 as an oil which

was used without further purification.

EXAMPLE2

General Procedure for Preparation of phosphorochloridates

1 R 3 ;3 3 - R1 R 3b R b R

CI-P-CI + NH 2 A N -CI 4 SR 0 R40

A- = C- or Ts 2 3

A solution of triethylamine (2eq) in anhydrous dichloromethane was added dropwise to a

solution of aryloxy-phosphodichloridate 2 (1 eq) and the appropriate amino ester 3 ( 1 eq) in

anhydrous dichloromethane with vigorous stirring at -78 °C over a period of 30 to 120

minutes. Then the reaction temperature was allowed to warm to room temperature and

stirred over night. Solvent was removed. The residue was washed with ethyl ether and

filtered, the filtrate was dried over reduced pressure to give 4.

EXAMPLE3

r,)7-

General Procedures for nucleoside phosphoramidate derivatives

R3a R3b .R1 H0" as e R3b -R1 b+RC HOR BaeNBase

4 5

A solution of the appropriate phosphorochloridate 4(6.5 equivalents) in anhydrous

tetrahydrofuran (THF) was added to amixture of nucleoside 5(1 equivalent) and N

methylimidazole (8 equivalents) in anhydrous THF with vigorous stirring at room

temperature and the reaction mixture was stirred overnight. The solvent was removed in

vacuo and the crude was purified by columnchromatography and/or preparative thin layer

chromatography to giveI.

EXAMPLE4

Preparation of 2'-deoxy-2'-fluoro-2'-C-methyluridine

N NH 2 N NHBz O N 0 N HO BzCI BzO 80%AcOH

HO Fe pyridine BzO F reflux

0 N NH3 /MeOH 0 N BzO HO BzO FHdF

2'-Deoxy-2'-fluoro-2'-C-methylcytidine (1.0g, 1eq ) (Clark, J., et al., J. Med. Chem., 2005,

48, 5504-5508) was dissolved in 10 ml of anhydrous pyridine and concentrated to dryness in

vacuo. The resulting syrup was dissolved in 20 ml of anhydrous pyridine under nitrogen and

cooled to 0°C with stirring. The brown solution was treated with benzoyl chloride (1.63g,

3eq) dropwise over 10 min. The ice bath was removed and stirring continued for 1.5h

whereby thin-layer chromatography (TLC) showed no remaining starting material. The

mixture was quenched by addition of water (0.5 ml) and concentrated to dryness. The

residue was dissolved in 50 mL of dichloromethane (DCM) and washed with saturated

NaHCO3 aqueous solution and H20. The organic phase was dried over NaSO4 and filtered,

concentrated to dryness to give N4,3',5'-tribenzoyl-2'-Deoxy-2'-fluoro-2'-C-methylcytidine

(2.0 g, Yield: 91%).

N 4 ,3',5'-tribenzoyl-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (2.0g, 1 eq ) was refluxed in 80%

aqueous AcOH overnight. After cooling and standing at room temperature (15 C), most of

the product precipitated and then was filtered through a sintered funnel. White precipitate

was washed with water and co-evaporated with toluene to give a white solid. The filtrate

was concentrated and co-evaporated with toluene to give additional product which was

_ lo_ washed with water to give a white solid. Combining the two batches of white solid gave

1.50g of 3',5'-dibenzoyl-2'-Deoxy-2'-fluoro-2'-C-methyluridine (Yield: 91%).

To a solution of 3',5'-dibenzoyl-2'-Deoxy-2'-fluoro-2'-C-methyluridine (1.5 g, leq) in MeOH

(10 mL) was added a solution of saturated ammonia in MeOH (20mL). The reaction

mixture was stirred at 0 °C for 30 min, and then warmed to room temperature slowly. After

the reaction mixture was stirred for another 18 hours, the reaction mixture was evaporated

under reduced pressure to give the residue, which was purified by column chromatography

to afford pure compound 2'-deoxy-2'-fluoro-2'-C-methyluridine (500 mg, Yield: 60 %).

EXAMPLE5

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methyluridine 5'-(phenyl methoxy-alanyl phosphate)

PI\ 0 00 '

OH3CO 000 N H0 , F 00 HO 0 N V. Oy-NIIO N Meo H N H F HO'

Phenyl methoxyalaninyl phosphorochloridate (1 g, 6.5 eq ) dissolved in 3 mL of THF was added to a mixture of 2'-Deoxy-2'-fluoro-2'-C-methyluridine (0.15 g,1 eq) and N methylimidazole (0.3 g, 8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (50.1 mg, 15.6%). 1H

NMR (DMSO-d) 6 1.20-1.27 (m, 6H), 3.58 (d, J= 16.0 Hz, 3H), 3.75-3.92 (m, 2H), 4.015 4.379 (m, 2H), 5.54 (t, J= 10.2 Hz, 1H), 5.83-5.91 (m, 1H), 6.00-6.16 (m, 1H), 7.18 (d, J= 8.0 Hz, 2H), 7.22 (s, 1H), 7.35 (t, J= 4.4 Hz, 2H), 7.55 (s, 1H), 11.52 (s, 1H); MS, m/e 502 (M+1)+.

EXAMPLE6

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methyluridine 5'-(phenyl methoxy-valyl phosphate)

H 3 CO P

H H O N

Hd- eFH HOF

Phenyl methoxy-valyl phosphorochloridate (0.6 g, 3.6 eq ) dissolved in 3 mL of THF was

added to a mixture of 2'-Deoxy-2'-fluoro-2'-C-methyluridine (0.15 g,1 eq) and N

methylimidazole (0.44 g, 9 eq) in 3 mL THF with vigorous stirring at room temperature,

then the reaction was stirred overnight. Solvent was removed by reduced pressure. The

resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC

25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The

acetonitrile and water were removed under reduced pressure to give the desired product (60

mg, 20%). 1 H NMR (DMSO-d) 6 0.74-0.847 (m, 6H), 1.20-1.28 (m, 3H), 1.89-1.92 (m,

1H), 3.50-3.54 (m, 1H), 3.58 (d, J= 10.4Hz, 3H), 3.72-3.95 (m, 1H), 4.03-4.05 (m, 1H),

4.23-4.43 (m, 2H), 5.56 (t, J= 16.0 Hz, 1H), 5.85-5.92 (m, 1H), 6.01-6.07 (m, 1H), 7.16

7.21 (m, 3H), 7.37 (t, J= 8 Hz, 2H), 7.55-7.60 (m, 1H), 11.52 (s, 1H); MS, m/e 530 (M+1)*.

EXAMPLE7

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methyluridine 5'-(4-bromophenyl methoxy valyl phosphate)

H - C\0 Br PO O H HC Br -No 0 H - - 0 0 H 0 N 0-F1 N1I N 0 HO N' e O C ~ ~~MeO H0

4-Bromophenyl methoxy-valyl phosphorochloridate (1 g, 3.4 eq ) dissolved in 3 mL of THF

was added to a mixture of 2'-deoxy-2'-fluoro-2'-C-methyluridine (0.2 g,1 eq) and N

methylimidazole (0.35 g, 6 eq) in 3 mL THF with vigorous stirring at room temperature,

acetonitrile and water were removed reduced pressure to give the desired product (120 mg,

26%). 'H NMR (DMSO-d) 6 0.72-0.82 (m, 6H), 1.19-1.26 (m, 3H), 1.86-1.92 (m, 1H),

3.48-3.50 (m, 1H), 3.56 (d, J= 12.0 Hz, 3H), 3.72-3.89 (m, 1H), 3.96-4.03 (m, 1H), 4.22

4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.85-5.91 (m, 1H), 5.98-6.13 (m, 1H), 7.15 (d, J= 8.0

Hz, 2H), 7.49-7.56 (m, 3H), 11.53 (s, 1H); MS, m/e 608 (M+1)*.

EXAMPLE8

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methyluridine 5'-(4-bromophenyl methoxy alanyl phosphate)

CI\

0 HH Br o CCOH

eO H H HO MeH

4-Bromophenyl methoxy-alanyl phosphorochloridate (0.6 g, 5 eq ) dissolved in 3 mL of THF was added to a mixture of 2'-deoxy-2'-fluoro-2'-C-methyluridine (0.15 g,1 eq)and N methylimidazole (0.3 g, 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (40 mg, 12 %); 1H NMR (DMSO-d) 6 1.20-1.26 (m, 6H), 3.57 (d, J= 2.8 Hz, 3H), 3.84 (s, 1H), 3.97-4.03 (m, 1H), 4.21-4.25 (m, 1H), 4.33-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.83-5.89 (m, 1H), 5.98-6.19 (m, 1H), 7.16 (t, J= 10.2 Hz, 2H), 7.52-7.57 (m, 3H), 11.52 (s, 1 H); MS, m/e 580(M+1)*.

EXAMPLE9

Preparation of N 4-(NN-dimethylformamidinyl)-2'-deoxy-2'-fluoro-2'-C-methylcytidine

N NH 2 N N 0 N DMA-DMF H N HO F HO

Hd F H F

2'-Deoxy-2'-fluoro-2'-C-methylcytidine (500 mg, 1.9 mmol) was stirred with dimethylformamide dimethyl acetal in DMF (10 mL). The resulting mixture was stirred at room temperature overnight. After solvent removal the crude product was used for next step without further purification.

EXAMPLE 10

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methylcytidine 5'-(phenyl methoxy-alanyl phosphate)

C 0 H3COy-- Np ° N H O 0 N NH 2

/ N HO N HOF HOF

Phenyl methoxyalaninyl phosphorochloridate (0.6 g, 6 eq ) dissolved in 3 mL of THF was added to a mixture of N 4 -(NN-dimethylformamidinyl)-2'-deoxy-2'-fluoro-2'-C methylcytidine (0.15 g,1 eq) and N-methylimidazole (0.3 g, 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x30X2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (62 mg, 20.6%). 'H NMR (DMSO-d) 6 1.16 (d, J= 23.2 Hz, 3H), 1.22 (d, J= 7.2 Hz, 3H), 3.56 (S, 3H), 3.69-3.75 (d, J= 25.6 Hz, 1H), 3.82 3.86 (m, 1H), 3.96-3.98 (m, 1H), 4.21-4.34 (m, 2H), 5.68 (d, J= 7.2 Hz, 1H), 5.75-5.77 (m, 1H), 6.07-6.16 (m, 1H), 7.15-7.19 (m, 3H), 7.2 (d, J= 9.2 Hz, 2H), 7.39 (t, J= 7.8 Hz, 2H), 7.48 (d, J= 9.2 Hz, 1H); MS, m/e 501(M+1)'.

r |A

EXAMPLE11

Preparation of 2'-Deoxy-2'-fluoro-2'-C-methylcytidine 5'-(4-bromophenyl methoxy valyl phosphate)

H 3CO ci, 0 N N Br Br 00 \-N

N M <NN N NH 2 HO MeO HO0 HOE HO F

4-Bromophenyl methoxy-valyl phosphorochloridate (1.0 g, 3.4 eq. ) dissolved in 3 mL of 4 THF was added to a mixture of N-(NN-dimethylformamidinyl)-2'-deoxy-2'-fluoro-2'-C methylcytidine (0.2 g,1 eq.) and N-methylimidazole (0.35 g, 6 eq.) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was

removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25x3OX2 mm column using a water / acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product as a white solid (59 mg, 13%);1 H NMR (DMSO-d) 6 0.74-0.83 (m, 6H), 1.12-1.20 (m, 3H), 1.89-1.92 (m, 1H), 3.49-3.51 (m, 1H), 3.55 (s, 3H), 3.59-3.68 (m, 1H), 3.72-.383 (m, 1H), 4.21-4.39 (m, 2H), 5.70-5.72 (m, 1H), 5.76-5.83 (m, 1H), 6.04-6.16 (m, 1H), 7.15 (d, J= 13.0 Hz, 2H), 7.26 (s, 1H), 7.33 (s,1H), 7.46-7.55 (m, 1H), 7.56 (d, J= 4.4 Hz, 2H) ; MS, m/e 607 (M+1)'.

EXAMPLE 12

Preparation of 2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-(phenyl methoxy-valyl phosphate)

/ H 3 CO PI\ 0,ii

HOe F H0 5 HO7 NMNH 2

Phenyl methoxy-valyl phosphorochloridate (0.6 g, 6 eq ) dissolved in 3 mL of THF was

added to a mixture of N 4 -(NN-dimethylformamidinyl)-2'-deoxy-2'-fluoro-2'-C

methylcytidine (0.15 g,1 eq) and N-methylimidazole (0.3 g, 7.8 eq) in 3 mL THF with

vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was

removed by reduced pressure The resulting crude product was dissolved in methanol

purified by prep-HPLC on a YMC 25x3OX2 mm column using a water / acetonitrile

gradient elution mobile phase. The acetonitrile and water were removed under reduced

pressure to give the desired product as a white solid (86 mg, 42.9 %). 1H NMR (DMSO-d6)

6 0.72-0.80 (m, 6H), 1.09-1.18 (m, 3H), 1.87-1.92 (m, 1H), 3.47-3.51 (m, 1H), 3.58 (s, 3H),

3.71-3.75 (m, 1H), 3.97 (t, J= 11.2 Hz,1H), 4.22-4.37 (m, 2H), 5.70 (d, J= 8.0 Hz,1H),

5.76-5.84 (m, 1H), 6.01-6.15 (m, 1H), 7.13-7.18 (m, 3H), 7.27 (s, 2H), 7.34 (d, J= 4.0 Hz,

2H), 7.46-7.50 (m, 1H); MS, m/e 529 (M+1)*.

EXAMPLES

Example numbers 13-54 and 56-66 are prepared using similar procedures described for examples 5-8. The example number, compound identification, and NMR/MS details are shown below: H 3h 3 N R R b O OR' 0 4 R0 P O N 0 N 2 0 R

HO F

Ex. R1 R2 R3 a R3b R4 NMR/MS 13 Ph H H Me Et 1HNMR(DMSO-d)6 )61.12-1.16(m,3H), 1.20-1.28(m,6H),3.70-3.90 (m, 2H), 4.00-4.08 (m, 3H), 4.18-4.45 (m, 2H), 5.52-5.58 (m, 1H), 5.85-5.98 (m, 1H), 6.00-6.20 (m, 2H), 7.16-7.23 (m, 3H), 7.37-7.40 (m, 2H), 7.54-7.60 (m, 1H), 11.54 (s.1H); MS, m/e 516.1 (M+1)+

14 1-Napth H H Me Bn 1H NMR (DMSO-d) 61.18-1.30 (m, 6H), 3.78-4.10 (m, 3H), 4.38 4.49 (m, 2H), 4.99-5.11 (m, 2H), 5.28-5.40 (m, 1H), 5.85-6.10 (m, 2H), 6.30-6.41 (m, 1H), 7.28-7.32 (m, 5H), 7.41-7.60 (m, 5H), 7.73

7.76(m,1H), 7.94-8.11(m,1H), 8.13-8.15(m,1H), 11.50(s.1H);

MS, m/e 628.4 (M+1)+

15 Ph H H H Me 1H NMR (DMSO-d) 6 1.22 (d, J=22.4 Hz, 3H), 3.59(s, 3H), 3.63-3.69 (m, 2H), 3.74-3.8(m, 1 H), 4.02(d, J=11.2 Hz, 1 H), 4.23-4.28(m, 1 H), 4.40-4.43 (m, 1H), 5.57-5.60 (m, 1H), 5.89(d, J=6.8 Hz, 1H), 6.00 6.06(m, 2H), 7.15-7.23 (m, 3H), 7.35-7.39 (m, 2H),7.52(d, J=8 Hz, 1H), 11.52(s, 1H); MS, m/e 487.97 (M+1)+

16 2,4-Cl- H H Me Me 1H NMR (DMSO-d) 6 1.22-1.28 (m, 6H), 3.57-3.60 (m, 3H), 3.84 Ph 3.92 (m, 2H), 4.00-4.04 (m, 1H), 4.31-4.44 (m, 2H), 5.54-5.61 (m, 1H), 5.85-6.10 (m, 2H), 6.32-6.43 (m, 1H), 7.44-7.54 (m, 3H), 7.72 7.75 (m, 1H), 11.54 (s.1H); MS, m/e 570.2 (M+1)+

17 1-Napth H H Me Me 1H NMR (DMSO-d) 6 1.15-1.27 (m, 6H), 3.51-3.55 (d, 3H), 3.85 3.96 (m, 2H), 4.00-4.10(m, 1 H), 4.30-4.46 (m, 2H), 5.31-5.39 (m, 1H), 5.89-6.05 (m, 2H), 6.22-6.34 (m, 1H), 7.44-7.60 (m, 5H), 7.73-7.77 (m, 1H), 7.93-7.96 (m, 1H), 8.12-8.14 (m, 1H),11.50(s.1H) ; MS, m/e 552.1 (M+i)+

18 Ph * H * Me 1H NMR (DMSO-d) 6 1.19 (d, J=22.8 Hz, 3H), 1.69-1.84 (m, 3H), 1.99-2.04 (m, 1H), 3.16-3.21 (m, 2H), 3.58 (s, 3H), 3.68-3.8 (m, 1H), 4.00 (m, 1H), 4.01-4.13 (m, 1H), 4.22-4.25 (m, 1 H), 4.5 (d, J= 11.2 Hz, 1H), 5.54 (d, J = 8.0 Hz, 1H), 5.86 (s, 1H), 5.6 (d, J = 19.6 Hz, 1H), 7.15-7.2 (m, 3H), 7.34 (t, J = 8.0 Hz, 2H), 7.51 (d, J = 8.0 Hz, 1H), 11.38 (s, 1H); MS, m/e 527.93(M+1)+

19 Ph H H Me n-Bu 1H NMR (DMSO-d) 6 0.80-0.90 (m, 3H), 1.20-1.35 (m, 8H), 1.48 1.55 (m, 2H), 3.78-3.88 (m, 2H), 3.95-4.08 (m, 3H), 4.22-4.45 (m, 2H), 5.55-5.57(t, 1H), 5.85-6.18 (m, 3H), 7.14-7.23 (m, 3H), 7.35-7.40 (m, 2H), 7.51-7.60 (d, 1H), 11.50 (s.1H); MS, m/e 544.2 (M+1)+

20 Ph H H Me Bn 1H NMR (DMSO-d) 6 1.20-1.30 (m, 6H), 3.72-4.05 (m, 3H), 4.23

4.27((m, 1H),4.32-4.45((m, 1H),5.07-5.10(t,2H),5.52-5.56(t, 1H),

5.86-6.10(m,2H),6.13-6.21(m,ilH),7.15-7.21(m,3H),7.29-7.40(m, 7H), 7.51-7.56 (d, 1H), 11.50 (s.1H); MS, m/e 578.2 (M+1)+

21 4-F-Ph H H Me Me 1H NMR (DMSO-d) 6 1.28-1.34 (m, 6H), 3.65(d, J= 4 Hz, 3H), 3.85

_ '17_

Ex. R1 R2 R3 . 3 R b R4 NMR/MS 3.96 (m, 2H), 4.06-4.12 (m, 1H), 4.30-4.34 (m,1H), 4.40-4.47 (m, 1H),

5.62-5.67 (m, 1H), 5.94-6.0 1(m, 1H), 6.09 (d, J=18.8 Hz, 1 H), 6.17 6.26 (m, 1H), 7.27-7.33(m, 4H), 7.62 (d, J = 7.6 Hz, 1H), 11.61 (s, 1H) ; MS, m/e 519.94(M+1)+

22 4-Cl-Ph H H Me Me 1H NMR (DMSO-d) 6 1.22-1.28 (m, 6H), 3.58 (d, 2H), 3.70

3.95(m,2H),3.95-4.08(m,1H),4.23-4.45(m,2H),5.55-5.61(t, 1H),

5.85-6.10(m,2H),6.15-6.23(m,1H),7.20-7.26(m,2H),7.43-7.46(m, 2H), 7.54-7.57 (d, 1H), 11.50 (s.1H); MS, m/e 536.1 (M+1)+

23 3,4-Cl- H H Me Me 1H NMR (DMSO-d) 6 1.13 (m, 6H), 3.49 (s, 3H), 3.61-3.85 (m, 2H), Ph 3.90-3.93 (m, 1H), 4.16-4.22 (m, 1H), 4.27-4.31 (m, 1H), 5.47-5.52

(m, 1H), 5.82 (d, J = 11.6 Hz, 1H), 5.93(d, J = 19.2 Hz, 1H), 6.15-6.25 (m, 1H), 7.13 (t, J = 9.6 Hz, 1H), 7.43 (d, J = 12Hz, 2H), 7.57 (d, J = 6.0 Hz, 1H), 11.43(s, 1H); MS, m/e 569.85 (M+1)+

24 Ph H H Me 2-Bu 1H NMR (DMSO-d) 60.83 (d, J= 6.8 Hz, 6H), 1.20-1.26 (m, 6H), 1.79-1.86 (m, 1H), 3.73-3.90 (m, 4H), 4.01 (t, J = 11.2 Hz, 1H), 4.21 4.28 (m, 1H), 4.33-4.42 (m, 1H), 5.54 (t, J = 7.6 Hz, 1H), 5.85-5.92

(m, 1H), 5.99-6.13 (m, 2H), 7.19 (t, J = 8 Hz, 3H), 7.36 (t, J = 7.6 Hz,

2H), 7.53 (d, J = 7.6 Hz, 1H), 11.52 (s, 1H); MS, m/e 544.00 (M+1)+

Ph H H Me i-Pr 1H NMR (DMSO-d) 6 1.13-1.28 (m, 12H), 3.74-3.81 (m, 2H), 3.95 4.08 (m,1H), 4.20-4.45 (m, 2H), 4.83-4.87 (m, 1H), 5.52-5.58 (m, 1H),

5.84-6.15 (m, 3H), 7.17-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.54-7.57 (m, 1H), 11.50 (s.1H); MS, m/e 530.2 (M+1)+

26 4-MeO- H H Me n-Bu 1HNMR (400MHz, DMSO-d): 6 =0.78-0.82 (m, 3H), 1.29-1.47 (m, Ph 8H), 1.49-1.54 (m, 2H), 3.66-3.87 (m, 5H), 3.96-4.02 (m, 3H), 4.21

4.39 (m, 2H), 5.57 (t, J= 12.0Hz, 1H), 5.84-6.05 (m, 3H), 6.90 (dd, Ji =8.0Hz, J2=4.OHz, 2H), 7.09-7.14 (dd, J=16.OHz, J2=4.OHz, 2H),

7.55 (d, J=8.0Hz, 1H), 11.48-11.62 (s, 1H)

27 4-F-Ph H H Me Et 1H NMR (DMSO-d) 6 1.12-1.28 (m, 9H), 3.72-3.94(m,2H),3.98-4.10 (m,3H), 4.21-4.42(m,2H), 5.55-5.61 (t, 1H), 5.85-6.20 (m, 3H), 7.18 7.25 (m,4H), 7.55-7.58 (d, 1H), 11.50 (s.1H); MS, m/e 533.90 (M+1)+

28 4-F-Ph H H Me i-Pr 1H NMR (DMSO-d) 6 1.13-1.30 (m, 12H), 3.74-3.85(m,2H),3.98 4.06 (m,1H), 4.23-4.41(m,2H), 4.83-4.87 (m, 1H), 5.55-5.61 (t, 1H), 5.85-6.12 (m, 3H), 7.18-7.24 (m,4H), 7.55-7.58 (d, 1H), 11.50 (s.1H); MS, m/e 547.91 (M+1)+

29 4-F-Ph H H Me Bn 1H NMR (DMSO-d) 6 1.10-1.23 (m, 6H), 3.65-3.89(m,3H),4.10-4.30 (m,2H), 4.96-5.00(m,2H), 5.46-5.50 (t, 1H), 5.75-5.96 (m, 2H), 6.04 6.12(m,1H), 7.05-7.11 (m,4H), 7.20-7.24 (d, 5H), 7.42-7.45(d,H), 11.50 (s.1H); MS, m/e 595.94 (M+1)+

4-MeO- H H Me i-Pr 1HNMR (400MHz, DMSO-d): 6=1.15-1.27 (m, 12H), 3.71-3.89 (m, Ph 5H), 3.98-4.02 (m, 1H), 4.22-4.25 (m, 1H), 4.33-4.39 (m, 1H), 4.84

4.87 (m, 1H), 5.57 (t, J= 12.0Hz, 1H), 5.91-6.03 (m, 3H), 6.90 (d, J= 8.0Hz, 2H), 7.09-7.14 (m, 2H), 7.55 (d, J= 8.0Hz, 1 H), 11.51 (s, 1 H)

31 2-Cl-Ph H H Me Bn 1H NMR (DMSO-d) 6 1.23 (m, 6 H), 3.93-4.00 (m, 3 H), 4.27-4.40 (m, 2H), 5.0(t, J= 7.2 Hz, 2 H), 5.53 (m,1 H), 5.80-6.0(m, 2 H), 6.30(m, 1H), 7.15 (d, J= 2.4 Hz, 1 H), 7.27 (m, 6 H), 7.51 (m, 3 H), 11.5 (s, 1 H); MS, m/e 579.87(M+1)+ / 596.78 (M+18)+

32 2,4-Cl- H H Me n-Bu 1H NMR (DMSO-d) 6=0.82 (m, 3 H),1.23 (m, 8 H), 1.47 (m, 2 H), Ph 3.86 (m, 2 H), 3.84 (m, 3 H),4.27-4.43 (m, 2H), 5.5 (m, 1 H), 6.02 (m

,2 H), 6.35(m, 1H), 7.44 (m, 3 H), 7.77 (m, 1 H), 11.5 (s, 1 H); MS, m/e 611.87(M+1)+

33 4-Me- H H Me i-Pr 1H NMR (DMSO-d) 6 1.14-1.27 (m, 12H), 2.17-2.26 (m, 3H), 3.73 Ph 3.82 (m, 1H), 3.99-4.02 (m, 1H), 4.23-4.26 (m, 1H), 4.37-4.40 (m,

Al1 2-

Ex. R1 R2 R3 . 3 R b R4 NMR/MS 1H), 4.82-4.88 (m, 1H), 5.52-5.58 (m, 1H), 5.85-6.07 (m, 3H), 7.01 7.20 (m, 4H), 7.55 (d, J= 16Hz, 1H), 11.51 (s, 1H); MS, m/e 543.98 (M+l)+; 1108.86 (2M+23)+

34 4-F-Ph H H Me n-Bu 1H NMR (DMSO-d) 6 0.82-0.89 (m,3H), 1.20-1.31 (m, 8H), 1.48 1.53 (m,2H), 3.77-3.90 (m,2H),3.95-4.10 (m,3H), 4.21-4.45(m,2H), 5.56-5.61 (t, 1H), 5.83-6.20 (m, 3H), 7.18-7.25 (m,4H), 7.55-7.58 (d, 1H), 11.50 (s.1H); MS, m/e 584.1 (M+23)+

3,4- H H Me Et 1H NMR (DMSO-d) 61.12-1.31 (m, 9H), 3.77-3.92 (m,2H), 3.95-4.08 diCl-Ph (m,3H), 4.21-4.45(m,2H), 5.56-5.62 (t, 1H), 5.80-6.11 (m, 2H), 6.18

6.33(m,1H), 7.18-7.25 (m,1H), 7.49-7.56 (d, 2H), 7.62-7.67(m, H), 11.50 (s.1H) ; MS, m/e 606.1 (M+23)+

36 2-Cl-Ph H H Me i-Pr 1HNMR (400MHz, DMSO-d): 6=1.12-1.16 (m, 6H), 1.21-1.27 (m, 6H), 3.79-3.85 (m, 2H), 4.00-4.07 (m, 1H), 4.28-4.32 (m, 1H), 4.38

4.43 (m, 1H), 4.83-4.87 (m, 1H), 5.56 (dd, J1=16.OHz, J2=8.OHz, 1 H), 5.85-6.12 (m, 2H), 6.20-6.33 (m, 1H), 7.19-7.22 (m, 1H), 7.33 (t, J=

16.0Hz, 1H), 7.48-7.55 (m, 3H), 11.55 (s, 1H)

37 4-MeO- H H Me Bn 1HNMR(400MHz, DMSO-d): 6=1.19-1.26 (m, 6H), 3.69-3.70 (s, Ph 3H), 3.87 (m, 2H), 3.99 (m, 1H), 4.20-4.21 (m, 1H), 4.35 (m, 1H),

5.07-5.09 (m, 2H), 5.54 (t, J = 16.0Hz, 1H), 5.85-5.92 (m, 1H), 6.04 6.10 (m, 2H), 6.86 (d, J= 8.0Hz, 2H), 7.09 (dd, J=16.Hz, J2=4.Hz, 2H), 7.30-7.34 (m, 5H), 7.53 (s, 1H), 11.52 (s, 1H)

38 Ph H H Me n-Pen 1H NMR (DMSO-d) 6 0.79-0.81 (m, 3H), 1.17-1.23 (m, 1OH), 3.74 3.81 (m, 2H), 3.94-3.96 (m, 3H), 4.19-4.36 (m, 2H), 5.49-5.54 (m,

1H), 5.87-6.08 (m,3H), 7.14-7.33 (m, 3H), 7.31-7.35 (m, 2H), 7.51 (d, J = 8Hz, 1H), 11.51 (s, 1H); MS, m/e 557.9 (M+1)+; 1136.88 (2M+23)+

39 4-Cl-Ph H H Me i-Pr 1H NMR (DMSO-d) 6 1.04-1.19 (m, 12H), 3.76-3.80 (m , 2H), 3.98 4.08 (m, 1H), 4.42-4.42 (m, 2H), 4.82-4.85 (m, 1H), 5.55-5.60 (m,

1H), 5.80-6.20 (m,3H),7.20-7.2 5(m, 2H), 7.43 (d, J= 8.8Hz, 1H), 7.54 (d, J= 8Hz, 1H), 11.51 (s, 1H); MS, m/e 563.88 (M+1)+; 1148.73 (2M+23)+

4-Cl-Ph H H Me n-Bu 1H NMR (DMSO-d) 60.85 (t, J = 7.2 Hz, 3H), 1.22-1.33 (m, 8H),1.45-1.53 (m, 2H), 3.80-3.87 (m, 2H), 3.96-4.04 (m, 3H), 4.24 4.27 (m, 1H), 4.35-4.39 (m, 1H), 5.56-5.61 (m, 1H), 5.82-6.11 (m,

2H), 6.15-6.18 (m, 1H), 7.20-7.56 (m, 4H), 7.51-7.57 (m.1H), 11.54 (s, 1H); MS, m/e577.95(M+1)+

41 4-Cl-Ph H H Me Et 1H NMR (DMSO-d) 6 1.14 (t, J= 7.OHz, 3H), 1.20-1.28 (m, 6H),3.77-3.88 (m, 2H), 3.99-4.07 (m, 3H), 4.24-4.28 (m, 1H), 4.34

4.43 (m, 1H), 5.56-5.61 (m, 1H), 5.86-6.13 (m, 2H), 6.15-6.24 (m,

1H), 7.20-7.26 (m, 2H), 7.44 (d, J = 7.6Hz, 2H), 7.55 (d, J= 7.6Hz, 1H), 11.55 (s, 1H); MS, m/e549.1 (M+1)+

42 4-Me- H H Me n-Bu 1H NMR (DMSO-d) 6 0.79-0.83 (m, 3H), 1.17-1.28 (m, 8H), 1.45 Ph 1.47 (m, 2H), 2.22 (d, J= 2.8Hz, 1H), 3.70-3.90 (m, 2H), 3.95-3.98

(m, 3H), 4.10-4.40 (m, 2H), 5.51 (t, 1H), 5.80-5.90 (m, 1H), 5.95-6.05

(m, 2H), 7.02-7.06 (m, 2H), 7.51 (t, J= 4.2Hz, 4H), 7.51 (d, 1H),

11.51 (s, 1H); MS, m/e 557.99(M+1)+; 1136.84(2M+23)+

43 4-Me- H H Me Bn 1H NMR (DMSO-d) 6 1.16-1.24 (m, 6H), 2.22 (s, 3H), 3.65-4.03 Phe (m,3H), 4.11-4.38 (m, 2H), 5.04-5.05 (m, 2H), 5.48-5.50 (m, 1H), 5.77-5.87 (m,1H),5.90-6.11 (m, 2H), 6.98-7.10 (m, 4H), 7.28-7.32 (m, 5H), 7.50 (t,1H), 11.48 (s, 1H); MS, m/e 592.00 (M+1)+.

44 Ph H H Et Me 1H NMR (DMSO-d) 6 0.70-0.80 (m, 3H), 1.11-1.26 (m, 3H), 1.42 1.61 (m, 2H), 3.50-3.54 (m, 3H), 3.58-3.80 (m, 2H), 3.91-4.02 (m,

1 H), 4.12-4.38 (m, 2H), 5.47-5.52 (m, H),5.90-6.03 (m, 2H), 7.08

_A0o_

Ex. R1 R2 R3 . R b 3 R4 NMR/MS 7.16 (m, 3H), 7.26-7.35 (m, 2H),7.48 (t,H),1 1.45 (s, 1H); MS, m/e 515.95 (M+1)+; 1052.82 (2M+23)+

Ph H H Me 4-F-Bn 'HNMR (400MHz, DMSO-d): 6 1.20-1.26 (m, 6H), 3.80-3.93 (m, 2H), 3.98 (s, 1H), 4.25-4.26 (m, 1H), 4.36-4.37 (m, 1H), 5.07 (s, 2H), 5.52-5.55 (m, 1H), 5.86-5.87(m, 1H), 5.98-6.04 (m, 1H), 6.14-6.17 (m,

1H), 7.15-7.20 (m, 5H), 7.36 (dd, J= 20.0,8.0 Hz, 4H), 7.54 (s, 1H), 11.55 (s, 1H)

46 4-Cl-Ph H H Me n-Bu 'HNMR (400MHz, DMSO-d): 6 1.21-1.28 (m, 6H), 3.71-3.88 (m, 1H), 3.91-3.98 (m, 1H), 4.00-4.01 (m, 1H), 4.23-4.27 (m, 1H), 4.35 4.38 (m, 1H), 5.08 (d, J= 4.0Hz, 2H), 5.57 (dd, J= 12.0,8.0 Hz, 1H), 5.91 (d, J= 8.0 Hz, 1H), 6.01 (d, J= 8.0 Hz, 1H), 6.22-6.24 (m, 1H), 7.17-7.23 (m, 2H), 7.31-7.40 (m, 7H), 7.53 (s, 1H), 11.50 (s, 1H)

47 Ph H H Me 3-Me-i- 'H NMR (DMSO-d) 6 0.80-0.82 (m, 6H), 1.18-1.40 (m, 8H), 1.50 Bu 1.58 (m, 1H), 3.71-3.82 (m, 3H), 3.97-3.4.01 (m, 3H), 4.21-4.40 (m, 2H), 5.30(t, J= 8.6 Hz, 1H), 5.81-6.10 (m, 3H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.48 (d, J=8.4 Hz, 1H), 11.38 (s, 1H); MS, m/e 557.98 (M+1)'; 1136.88 (2M+23)

48 3,4- H H Me Bn 'H NMR (DMSO-d) 6 1.05-1.37 (m, 6H), 3.71-3.82 (m, 1H), 3.87 diCl-Ph 4.02 (m, 2H), 4.28-4.29 (m, 1H),4.36-4.38 (m, 1H),5.04 (d, J= 5.2Hz, 2H), 5.55-5.64 (m, 1H), 5.85-5.94 (m, 1H), 6.00-6.05 (m, 1H), 6.29

6.40 (m, 1 H),7.17-7.24 (m, 1H), 7.30-7.41 (m, 5H), 7.45-7.58 (m, 2H),

7.61 (d, J= 4.0Hz, 1H), 11.53 (s, 1H); MS, m/e545.80(M+1)l;

49 Ph H H Me c-Hex 'H NMR (DMSO-d 6 ) 6 1.18-1.41 (m, 12H), 1.59-1.67 (m, 4H), 3.74 13.80 (m, 1H), 3.96-4.02 (m, 1H), 4.19-4.26 (m, 1H), 4.31-4.39 (m,

1H), 4.60 (s, 1H), 5.52 (t, J= 7.8 Hz, 1H), 5.80-6.09 (m, 3H), 7.15 7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.52 (d, J= 8 Hz, 1H), 11.50 (s, 1H); MS, m/e 569.98 (M+1)l; 592.14 (M+23)'

Ph H Me H n-Bu 1H NMR (DMSO-d) 60.76 (t, J= 7.2Hz, 3H), 1.10-1.22 (m, 8H), 1.38-1.43 (m, 2H), 3.72-3.75 (m, 2H), 3.87-3.93 (m, 3H), 4.14-4.21 (m, 1H), 4.23-4.33 (m, 1H), 5.46-5.54 (m, 1H), 5.84-6.11 (m, 3H),

7.09-7.14 (m, 2H), 7.27-7.32 (m, 2H), 7.34-7.51 (m, 1H), 11.47 (s,

1H); MS, m/e543.98(M+1)+

51 Ph H Me H i-Pr 1H NMR (DMSO-d) 6 1.39 (d, J = 7.2Hz, 6H), 1.19-1.29 (m, 6H), 3.65-3.75 (m, 2H), 3.95-4.05 (m, 1H), 4.20-4.22 (m, 1H), 4.31-4.33

(m, 1H), 4.79-4.82 (m, 1H), 5.48-5.57 (m, 1H), 5.84-5.91 (m, 1H),

5.96-6.07 (m, 2H), 7.12-7.35 (m, 5H), 7.44-7.54 (m.1H), 11.49(s, 1H); MS, m/e529.96 (M+1)+

52 Ph H Me H Bn ' H NMR (DMSO-d) 6 1.18-1.28 (m, 6H), 3.70-3.83 (m, 1 H), 3.87 3.94 (m, 1H), 3.99-4.01 (m, 1H), 4.23-4.26 (m, 1H), 4.33-4.37 (m,

1H), 5.03-5.12 (m, 2H), 5.51-5.59 (m, 1H), 5.87-5.90 (m, 1H), 5.95 6.07 (m, 1H), 6.10-6.27 (m, 1H), 7.15-7.23 (m, 3H), 7.31-7.38 (m,

7H), 7.47-7.56 (m, 1H), 11.50 (s, 1H); MS, m/e577.99 (M+1)+

53 2-Cl-Ph H H Me n-Bu 'HNMR (400MHz, DMSO-d): 6 0.81-0.86 (m, 3H), 1.21-1.31 (m, 8H), 1.46-1.52 (m, 2H), 3.84-3.90 (m, 2H), 3.97-4.04 (m, 3H), 4.27 4.41 (m, 2H), 5.53-5.58 (m, 1H), 5.82-5.95 (m, 1H), 5.96-6.10 (m,

1H), 6.27-6.31 (m, 1H), 7.19-7.22 (m, 1H), 7.34 (dd, J= 8.0,4.0 Hz, 1H), 7.47-7.55 (m, 3H), 11.55 (s, 1H)

54 4-Br-Ph H H Me i-Pr 'HNMR (400MHz, DMSO-d): 6 1.10-1.14 (m, 6H), 1.20-1.27 (m, 6H), 3.74-3.81 (m, 2H), 3.99-4.01 (m, 1H), 4.21-4.25 (m, 1H), 4.37

4.38 (m, 1H), 4.81-4.85 (m, 1H), 5.58 (dd, J= 8.0,4.0 Hz, 1H), 5.82 5.95 (m, 1 H), 5.96-6.09 (m, 1H), 6.10-6.13 (m, 1H), 7.18 (dd, J= 12.0, 8.0 Hz, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1 H)

4-F-Ph H H Me c-Hex 'H NMR (DMSO-d) 6 1.20-1.44 (m, 12H), 1.60-1.71 (m, 4H), 3.75

rQAn-

Ex. R1 R2 R3 . R 3b R4 NMR/MS 4.02 (m, 2H), 3.94-4.02 (m, 1H), 4.19-4.26 (m, 2H), 4.59-4.61(m, 1H), 5.57 (t, J= 8.4 Hz, 1H), 5.85-6.06 (m, 3H), 7.17-7.23 (m, 4H), 7.54 (d, J= 8.4 Hz, 1H), 11.50 (s, 1H); MS, m/e 587.92 (M+1)l

56 4-Br-Ph H H Me c-Hex 'HNMR (400MHz, DMSO-d): 6=1.18-1.46 (m, 12H), 1.61-1.69 (m, 4H), 3.75-3.82 (m, 2H), 3.95-4.08 (m, 1H), 4.25-4.28 (m, 1H), 4.38 (s, 1H), 4.60-4.62 (m, 1H), 5.56-5.60 (m, 1H), 5.82-5.95 (m, 1H), 6.02 6.20 (m, 2H), 7.09-7.20 (m, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) MS, m/e 650.0 (M+3)'

57 Ph H H Et i-Pr 'HNMR (400MHz, DMSO-d): 6 =0.75-0.82 (m, 3H), 1.12-1.26 (m, 9H), 1.52-1.59 (m, 2H), 3.55-3.68 (m, 1H), 3.72-3.85 (m, 1H), 3.95 4.08 (m, 1H), 4.18-4.28 (m, 1H), 4.32-4.41 (m, 1H), 4.83-4.86 (m,

1H), 5.55 (m, J= 7.6Hz, 1H), 5.99-6.04 (m, 2H), 6.05-6.10 (m, 1H), 7.14-7.21 (m, 3H), 7.33-7.37 (m, 2H), 7.52-7.54 (m, 1H), 11.53 (s, 1H); MS, m/e566.07(M+23)

58 Ph H H Et c-Hex 'HNMR (400MHz, DMSO-d): 6 0.75-0.88 (m, 3H), 1.26-1.46 (m, 9H), 1.52-1.69 (m, 6H), 3.60-3.63 (m, 1H), 3.72-3.90 (m, 1H), 4.02

4.03 (m, 1H), 4.24-4.27 (m, 1H), 4.37-4.38 (m, 1H), 4.63-4.65 (m,

1H), 5.55 (dd, J=8.OHz, 4.4Hz, 1H), 5.80-5.95 (m, 1H), 6.00-6.07 (m, 2H), 7.15-7.22 (m, 3H), 7.34-7.38 (m, 2H), 7.54 (d, J=8.0Hz, 1H), 11.55 (s, 1H); MS, m/e 584.01 (M+1)*, 606.17 (M+23)

59 4-F-Ph H H Et c-Hex 'H NMR (DMSO-d) 6 0.75-0.84 (m, 3H), 1.24 (d,J= 22.8Hz, 3H), 1.29-1.47 (m, 6H), 1.51-1.70 (m, 6H), 3.59-3.66 (m, 1H), 3.77-3.84

(m, 1 H), 3.98-4.04 (m, 1 H), 4.21-4.27 (m, 1 H), 4.34-4.41 (m, 1H),

4.60-4.65 (m, 1H), 5.56-5.60 (m, 1H), 5.84-5.90 (m, 1H), 6.00-6.08

(m, 2H), 7.20-7.24 (m, 4H), 7.56(d,J= 8.0Hz, 1H), 11.49 (s, 1H); MS, m/e 602.00(M+1)

Ph H H Me F-CH 2- 'H NMR (DMSO-d) 6 1.18-1.25(m, 6H), 3.71-3.89 (m, 2H), 3.92-3.99 CH 2 - (m, 1H), 4.19-4.27 (m, 4H), 4.48-4.61 (m, 2H), 3.94-3.98 (m, 2H), 4.11-4.23 (m, 4H), 5.47-5.52 (m, 1H), 6.01-6.11 (m, 1H), 5.90-6.14

(m, 2H), 7.15-7.21 (m, 3H), 7.32-7.36 (m, 2H), 7.46-7.57 (m, 1H), 11.49 (s,1H); MS, m/e 533.86 (M+1)

61 Ph H H Me F2CH- 'H NMR (DMSO-d) 6 1.17-1.24 (m, 6H), 3.67-3.81 (m, 1H), 3.89 CH2- 3.98 (m, 2H),4.21-4.36 (m, 4H), 5.48-5.53 (m, 1H), 5.82-6.05 (m,

2H), 6.18-6.22 (m, 2H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.51 (s, 1H),11.50 (s, 1H); MS, m/e 551.92 (M+1)l;

62 Ph H H Me (CF 3 ) 2 - 'H NMR (DMSO-d) 6 1.13-1.29 (m, 6H), 3.67-3.81 (m, 1H), 3.94 CH- 4.32 (m, 4H), 5.47 (t, J= 8 Hz 1H), 5.82-6.01 (m, 2H), 6.33-6.36 (m,

1H), 6.70-6.78 (m, 1H), 7.09-7.15 (m, 3H), 7.28-7.32 (m , 2H), 7.43 7.46 (m, 1H),11.44 (s, 1H) ; MS, m/e 637.90 (M+1)'

63 Ph H H Me (CH 2F) 2 'H NMR (DMSO-d) 6 1.20-1.29 (m, 6H), 3.70-3.90 (m, 1H), 3.91 -CH- 4.12 (m, 2H), 4.20-4.33 (m, 1H), 4.35-4.48 (m, 1H), 4.52-4.55 (m,

2H), 4.63-4.67 (m, 2H), 5.20-5.35 (m, 1H), 5.56 (t, J= 8.4 Hz, 1H),

5.80-5.95 (m, 1H), 5.95-6.10 (m, 1H), 6.18-6.21 (m, 1H), 7.18-7.23 (m, 3H), 7.35-7.39 (m , 2H), 7.54 (s, 1H),11.55 (s, 1H) ; MS, m/e 565.98 (M+1)l

64 Ph H H Me c-Pr- 'H NMR (DMSO-d) 6 0.20-0.24(m, 2H), 0.47-0.48(m, 2H), 0.76 CH 2- 0.84(m, 3H), 1.03-1.05(m, 1H), 1.23(dd, J= 22.4 6.8 Hz 3H), 1.55

A/1

Ex. R1 R2 R3. 3 R b R4 NMR/MS 1.60(m, 2H), 3. 61-3.68(m, 1 H), 3. 81-3.89 (m, 3H), 3.98-4.03(m, I H),

4.23-4.29(m, 1H), 4.35-4.41(m, 1H), 5.56-6.00(m, 1H), 5.88-5.91(m,

1H), 6.04-6.10(m, 2H), 7.20-7.24(m, 4H), 7.55 (d, J= 7.6 Hz 1H),11.53 (s, 1H); MS, m/e 573.17 (M+1)

65 Ph H H Et c-Pen 'H NMR (DMSO-d,) 6 0.75-0.83 (m, 3H), 1.20-1.28 (m, 3H), 1.49 1.63 (m, 8H), 1.76-1.80 (m, 2H), 3.58-3.60 (m, 1H), 3.70-3.82 (m,

1H), 3.98-4.05 (m, 1H), 4.24-4.26 (m, 1H), 4.37-4.42 (m, 1H), 5.03

(s, 1H), 5.54-5.57 (m, 1H), 5.90-6.00 (m,lH), 6.02-6.07 (m, 2H), 7.15 7.22 (m, 3H), 7.35-7.39 (m, 2H) 7.55 (d, J= 8.0 Hz, 1H), 11.55 (s, 1 H); MS, m/e 570.03 (M+1)'

*R2 and R3 1 together are -(CH 2)3- as derived from L-proline

The purification procedure by Prep-HPLC: Crude products were dissolved in methanol. Injection volumes of these solutions were 5 mL. The preparative HPLC system including 2 sets of Gilson 306 pumps, a Gilson 156 UV/Vis detector, a Gilson 215 injector & fraction collector, with Unipoint control software. A Ymc 25x30x2 mm column was used. The mobile phase was HPLC grade water (A), and HPLC grade acetonitrile (B). Fractions were collected into 100*15mm glass tubes. HPLC gradient is shown in Table 1. Once the gradient was selected, acetonitrile solution was injected into HPLC system, and then fractions collected according to UV peaks. After the separation, each glass tubes were run MS test to collect the desired compounds. The fractions with target MS were combined in a well-weighted flask. Most of acetonitrile was removed under reduce pressure and the remaining solution was freeze-dried to give desired compound.

Table 1: Preparative HPLC gradient

Time (min) Flow rate (mL/min) %A %B 0 15 90 10 30 15 60 40

Preparation of Example 66 Scheme

CI O O IN CI

a b d N <N~~I 3 NIENPh BO\

NH3/THF ON TN NH3/MeOH H N 90 BC,overnight Bznrt overnig hot H0o v BzO IF HO I

ef

CIH H2N N NHO _O C HO O CI Et3 N/DCM

9 i

NH 2 O OO N1 NH 2

0 NN - CI OH¶ 0 /~~ HO OH HO F NMI/THF HO

66

Preparation of compound (b) To a solution of compound a (1 g, 2.69 mmol) in anhydrous THF (30 mL) was added

dropwise 1 M solution of LiAl(OBu-t)3H in THF (2.69 mL, 2. 69 mmol) at -20 °C. The

reaction mixture was stirred for 2-3 h at the same temperature. EtOAc (100 mL) was added followed by saturated NH4C1 solution (10 mL) and reaction mixture was slowly brought to room temperature. Reaction mixture was extracted with EtOAc and washed with IN HCl and water. Combined organic phase was evaporated to give 0.8 g of crude compound b as

transparent oil, which was used directly for next reaction. Preparation of compound (d) To a solution of compound b (0.8 g, 2.1mmol), compound c (0.45 g, 2.5 mmol) and Ph3P (0.56 g, 2.1 mmol) in anhydrous THF (20 mL) under nitrogen atmosphere was added DEAD (1.8 mL). The reaction mixture was stirred at room temperature overnight. The reaction solution was concentrated under reduce pressure. The residue was separated by preparative layer chromatography (hexanes:EtOAc = 3:1) to give crude compound d (0.8 g). The crude compound d was used to the next step without further purification. Preparation of compound (e) Compound d (0.8 g, 1.57 mmol) was dissolved in THF (2 mL) and THF saturated with ammonia (5 mL) was then added to this solution. The reaction mixture was heated to 90°C overnight. After 18 hours, the solution was cooled to room temperature by ice water, then

_ A'l the solvent was removed under reduced pressure and the residue was purified by column to give compound e (0.75 g) for the next step. Preparation of compound (f) Compound e (0.5 g, 1.01 mmol) was dissolved in methanol (2 mL) and methanol was saturated with ammonia (5 mL) was then added to this solution. The reaction mixture was stirred at room temperature overnight. After 18 hours, the solvent was removed under reduced pressure and the residue was purified by column to give crude compound f (0.15 g) for the next step. Preparation of compound (i) A solution of triethylamine (1.07 g, 10.6 mmol) in anhydrous dichloromethane (15 mL) was added dropwise to a solution of compound g (1.16 g, 5.3 mmol) and compound h (1.31 g, 5.3 mmol) in dichloromethane (10 mL) with vigorous stirring at -78 °C over a period of 2 hours. After completion of addition, the reaction temperature was allowed to warm to room temperature gradually and stirred over night. Then the solvent was removed under vacuum and anhydrous ether 20 mL was added and the precipitated salt was filtered and the precipitate was washed with ether. The combined organic phase was concentrated to give the colorless oil of compound i (1.0 g).

Preparation of Compound 66 To a solution of compound j (0.1 g, 0.35 mmol) dissolved in 10 mL of anhydrous THF, stirred and added 0.4g NMI till the solution became clear, added compound i (0.8 g, 2.89 mmol) in 10 mL THF dropwise, stirred at r.t. overnight. Compound purity and identification was confirmed by LCMS. The solvent was evaporated and purified by Prep HPLC to afford 66. (25 mg, Yield: 13.6%). 'H NMR (DMSO-d) 6 1.08 (d, J= 22.8 Hz, 3H), 1.17-1.24 (m, 3H), 3.50-3.52 (m, 3H), 3.78-3.83 (m, 1H), 4.10-4.13 (m, 1H), 4.24-4.44 (m, 2H), 5.85-5.92 (m, 1H), 6.01-6.11 (m,1H), 6.2.-6.27 (m, 1H), 7.08-7.19 (m, 4H), 7.31 7.38 (m, 3H), 8.15 (s, 1H), 8.26 (s, 1H); MS, m/e 525 (M+1)*.

Example numbers 67-74, identified below, were prepared using similar procedures disclosed for Example 66, above.

R11_ N -0 N R10

0 0HNPO/Q N N

HO P 10 Example R" R NMR/MS

-, tA-

Example R" R 10 NMR/MS 67 OH 1 NH 2 H NMR (DMSO-d) 6 1.06-1.13 (m, 3H), 1.20-1.24 (m, 3H), 3.27-3.33(m, 3H), 3.56 (s, 1H), 3.82-3.88 (m, 1H), 4.07-4.13 (m, 1H), 4.25-4.40 (m, 2H), 5.85-5.87 (m, 1H), 5.98-6.09 (m, 2H), 6.59 (s, 32H), 7.14-7.37 (m, 3H), 7.35-7.37 (m, 2H), 7.79 (d, J=7.2 Hz, 1H), 10.69 (s, 1H);MS, m/e 541 (M+1)*; 1 68 NH 2 NH 2 H NMR (DMSO-d) 6 1.07 (d, J=22.8 Hz, 3H), 1.19 (d, J=7.2 Hz, 3H), 3.51 (s, 3H), 3.62 (s, 1H), 3.75-3.81 (m, 1H), 4.05-4.11 (m, 1H), 4.27-4.42 (m, 2H), 5.79-5.83 (m, 1H), 5.92 (s, 2H), 6.00-6.09 (m, 2H), 6.75 (s, 2H), 7.08-7.17 (m, 3H), 7.31-7.35 (m, 2H), 7.78 (s, 1H); MS, m/e 540 (M+1)*; 1 69 NH 2 c-Pentyl-NH- H NMR (DMSO-d) 6 1.05 (d, J=22.8 Hz, 3H), 1.09-1.19 (m, 3H), 1.48 (s, 4H), 1.66 (s, 1H), 1.86 (s, 1H), 3.54 (d, J=14 Hz, 3H), 3.65 (s, 1H), 4.25-4.43 (m, 4H), 5.71-5.82(m, 1H), 5.94-6.04 (m, 4H), 7.11-7.24 (m, 3H), 7.26-7.34(m, 2H), 7.77(d, J=3.6 Hz, 1H); MS, m/e 608(M+1)*

NH 2 H NMR (DMSO-d) 6 1.07 (d, J=22.4 Hz, 3H), 2.35-2.38

- N (m, 2H), 3.54 (d, J=9.2 Hz, 3H), 3.59-3.62 (m, 2H), 3.65 (s, 1H), 3.75-3.82(m, 1H), 4.01-4.13 (m,2H), 4.22-4.40(m, 6H), 5.75-5.85(m, 1H), 6.00-6.07 (m,4H), 7.15-7.21(m, 3H), 7.32-7.35 (,2H), 7.79 (d, J=4.0 Hz, 1H); MS, m/e 580 (M+1)* 1 71 NH 2 Et 2N- H NMR (DMSO-d 6) 6 1.06-1.28 (m, 12H), 3.55 (d, J=4.8 Hz, 3H), 3.79-3.87 (m, 4H), 4.07-4.12 (m, 2H), 4.29-4.42(m, 3H), 5.75-5.82 (m, 1H), 5.94 (s, 2H), 6.04-6.10 (m, 2H), 7.14-7.22 (m, 3H), 7.31-7.37 (m, 2H), 7.82 (d, J=4.4 Hz, 1H); MS, m/e 596 (M+1)*

1 72 NH 2 n-Propyl-NH- H NMR (DMSO-d) 6 0.84 (t, J=7.2 Hz, 3H), 1.01-1.01(m, 3H), 1.09-1.12 (m, 3H), 1.51-1.56 (m, 2H), 3.48 (d, J=15.2 Hz, 3H), 3.79-3.82 (m, 1H), 4.04-4.05 (m, 1H), 4.27-4.38(m, 3H), 5.72-5.79(m, 1H), 5.98-6.04 (m, 4H), 7.13-7.20 (m, 3H), 7.26-7.32 (,2H), 7.76 (d, J=5.2 Hz, 1H); MS, m/e 582 (M+1)*

1 73 NH 2 c-Butyl-NH- H NMR (DMSO-d) 6 1.02-1.08 (m, 3H), 1.18 (d, J=4.8 Hz, 3H), 1.44-1.61 (m, 2H), 2.02-2.17 (m, 4H), 3.51 (d, J=10.8

Hz, 3H), 3.78-3.83 (m, 1H), 4.03-4.06 (m, 1H), 4.27-4.38(m, 2H), 4.53-4.62(m, 1H), 5.68-5.79(m, 1H), 5.95-6.04(m, 4H), 7.11-7.18 (m,3H), 7.29-7.35 (m,2H), 7.51-7.58(m, 1H), 7.78 (d, J=5.2 Hz, 1H); MS, m/e 594 (M+1)*

Example R" R10 NMR/MS 1 74 NH 2 H NMR (DMSO-d) 6 0.97-1.20 (m, 6H), 2.18 (s, 3H), 2.19 (s, 4H), 3.43-3.47(m, 3H), 3.75 (s, 1H), 4.01-4.06 (m, 4 H), 4.22-4.35 (m, 3H), 5.69-5.75 (m, 1H), 5.98-6.05 (m, 3H), 7.09-7.15 (m, 3H), 7.25-7.29 (m, 2H), 7.77 (d, J=3.6 Hz, 1H); MS, m/e 623 (M+1)*

Example numbers 75-80 are prepared using similar procedures disclosed for Example 66, above.

N

O 0 N N

HOs HO 0 Example R" R10 75 H n-propyl-NH 76 H c-Butyl-NH 77 H c-Pentyl-NH

78 H

79 H

80 H -N

EXAMPLE 81

Certain exemplified compounds were obtained as mixture of diastereomers because of the chirality at phosphorous. The diastereomers were separated on a Chiralpak-AS-H (2 X 25 cm) column under Supercritical Fluid Chromatography (SFC) conditions using 20% methanol in carbon dioxide as solvent. The absolute stereochemistry of the P-chiral center of the diastereromers were not determined. However, chromatographic resolution of these two diastereomers provides for isomers that are characterized as fast eluting and slow eluting isomers. Some examples are shown below. eQA-

Compound EC90 (uM) Example 15 (Diastereomeric mixture) 0.86

Fast Moving isomer of Example 15 1.35

Slow Moving isomer of Example 15 0.26 Example 39 (Diastereomeric mixture) 0.47

Fast Moving isomer of Example 39 0.78

Slow Moving isomer of Example 39 0.02

Example 49 (Diastereomeric mixture) 0.126

Fast Moving isomer of Example 49 0.03

Slow Moving isomer of Example 49 5.78

EXAMPLE 82

HCV replicon assay. HCV replicon RNA-containing Huh7 cells (clone A cells; Apath, LLC, St. Louis, Mo.) were kept at exponential growth in Dulbecco's modified Eagle's medium (high glucose) containing 10% fetal bovine serum, 4 mM L-glutamine and 1 mM sodium pyruvate, 1x nonessential amino acids, and G418 (1,000 [g/ml). Antiviral assays were performed in the same medium without G418. Cells were seeded in a 96-well plate at 1,500 cells per well, and test compounds were added immediately after seeding. Incubation time 4 days. At the end of the incubation step, total cellular RNA was isolated (RNeasy 96 kit; Qiagen). Replicon RNA and an internal control (TaqMan rRNA control reagents; Applied Biosystems) were amplified in a single-step multiplex RT-PCR protocol as recommended by the manufacturer. The HCV primers and probe were designed with Primer Express software (Applied Biosystems) and covered highly conserved 5'-untranslated region (UTR) sequences (sense, 5'-AGCCATGGCGTTAGTA(T)GAGTGT-3', and antisense, 5' TTCCGCAGACCACTATGG-3'; probe, 5'-FAM-CCTCCAGGACCCCCCCTCCC TAMRA-3').

To express the antiviral effectiveness of a compound, the threshold RT-PCR cycle of the test compound was subtracted from the average threshold RT-PCR cycle of the no-drug control (ACtHCV). A ACt of 3.3 equals a 1-log 10 reduction (equal to the 90% effective concentration [EC9]) in replicon RNA levels. The cytotoxicity of the test compound could also be expressed by calculating the ACtrRNA values. The AACt specificity parameter could then be introduced (ACtHCV- ACtrRNA), in which the levels of HCV RNA are normalized for the rRNA levels and calibrated against the no-drug control.

Ex LoglO # Compound Reduction at Eg9O M(M) -1.21 3.0 o Oh

6 -0.45 ND NH

H,

7 0.31 ND HN

H

8 -1.48 2.11

HF

10 -1.25 19.15 Ph

HHF

11 -0.55 ND

HF

12 0.31 ND

\/P H H

0 /QIh 0 N Me Ph

15 N N ND 0.86

[1/1 F

Ex LoglO E9 #Compound Reduction at (I'M)

0

250 N 0 -2.22 0.39 H O F

27 -2.25 0.66

H O F /- F

28 0 NH-2.16 0.75 PI 0 N 0

0r HO F

0

360 0 0 -1.64 21.9 HH0

CI

0

09 NH1 -1.78 0.47

0

49 0 P 0 NH -2.69 0.126 H- HO F

Cl NH 0

O\EpO 0 N 0

53 H1-1.33 <0.3 HC

Ex Log10 EC90 # Compound Reduction at (I'M 5oM (pM) Br

54 0

54 -1.55 0.57 P, 0 CN 0

Hd 'F ,00

O

55H -2.38 <0.3 55 N 0 H H

69 H -2.25 < 0.3

HO F NH2

70 oN -2.25 <0.3

HO F NH2

(4-BrPh): 4-bromo-phenyl.

The entire contents of 60/909,315, filed March 30, 2007; 60/982,309, filed October 24, 2007; and 12/053,015, filed March 21, 2008 are hereby incorporated by reference in the present application so far as needed to supplement the present disclosure and/or rectify any errors. Moreover, the patent and non-patent references disclosed herein are incorporated by reference. In the event that the incorporated patent and non-patent reference contains a term that conflicts with a term disclosed in either one of the two Provisional Applications or the present application text, the meaning of the term contained in the present application text and the two Provisional Applications controls provided that the overall meaning of the incorporated subject matter is not lost.

Throughout this specification, unless the context requires otherwise, the word "comprise" or variations such as "comprises" or "comprising", will be understood to imply the inclusion of a stated integer or group of integers but not the exclusion of any other integer or group of integers.

The following discussion of the background to the invention is intended to facilitate an understanding of the present invention only. It should be appreciated that the discussion is not an acknowledgement or admission that any of the material referred to was published, known or part of the common general knowledge of the person skilled in the art in any jurisdiction as at the priority date of the invention.

_, r 1_

Claims

The claims defining the invention are as follows:

1. A compound, or a stereoisomer thereof, represented by formula (I): 0

R8 NH

R3b R2 0 - N R7 N 0 R3a N -* 0

C0 2 R4 OR' CH 3

HO F

(I)

wherein P* is a chiral phosphorous atom,

and wherein

(a) R' is hydrogen, methyl, ethyl, n-propyl, i-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH3, OCH3, F, Cl, Br, I, nitro, cyano, and a CH3-qX, where X is F, Cl, Br, or I, and q is 1-3;

(b) R2 is hydrogen or CH3;

(c-i) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl, or

(c-ii) R3a is CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl and R3b is H;

(d) R4 is hydrogen, CH3, Et, Pr, "Pr, "Bu, 2-butyl, 'Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; and

(e) R7 and R8 are independently H, F, Cl, Br,I, OH, OCH3, SH, SCH3, NH2, NHCH3, N(CH3)2, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2H, CO2CH3, CONH2, CONHCH3, or CON(CH3)2, wherein R'is a CI-2o alkyl; a C-20 cycloalkyl; a C2-C6 alkenyl, a C2-C6 alkynyl.

2. (Previously Presented): The compound according to claim 1, wherein:

(a) R 1 is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p chloro-phenyl, p-fluorophenyl; and

(c-i) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, CH2-indol-3-yl, -CH2CH2SCH3, CH2CO2H, CH2C(O)NH2, CH2CH2COOH, CH2CH2C(O)NH2, CH2CH2CH2CH2NH2, -CH2CH2CH2NHC(NH)NH2, CH2-imidazol-4-yl, CH2OH, CH(OH)CH3, CH2((4'-OH)-Ph), CH2SH, or lower cycloalkyl.

3. The compound according to claim 1, wherein:

(c-i) R3 a is H and R 3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; and

(e) R7 and R8 are independently H, F, Br, SCH3, CH3, CH3-qX, where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO2CH3, CONH2, CONHCH3, or CON(CH3)2.

4. The compound according to claim 1, wherein:

(b) R2 is hydrogen;

(c-i) R3 a is H and R3b is H, CH3, CH(CH3)2, CH2CH(CH3)2, CH(CH3)CH2CH3, CH2Ph, or lower cycloalkyl; and

5. The compound according to claim 1, wherein:

(b) R2 is hydrogen;

6. A composition comprising the compound according to any one of claims I to 5.

7. A composition comprising the compound according to any one of claims I to 5 and a pharmaceutically acceptable medium.

8. A composition comprising an effective amount of the compound according to any one of claims 1 to 5 to treat a hepatitis C virus infection and a pharmaceutically acceptable medium.

9. A method of treating a subject infected by a virus selected from among hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus or Japanese encephalitis virus, which comprises administering to the subject an effective amount of the compound according to any one of claims I to 5.

10. The method of claim 9, wherein the virus is hepatitis C virus.

11. The method of claim 10, which further comprises administering to the subject an effective amount of another antiviral agent.

12. The method of claim 10 or 11, wherein the subject is a human.

13. A process for preparing the compound according to any one of claims I to 5 comprising reacting a compound 4" with a nucleoside analog 5':

1 7 R8 RO R 3b HR R

P-'HO N 040N0

F 0 CH 3

4" 5'

wherein

X' is a leaving group.

r, (A

14. Use of a compound according to any one of claims I to 5 in the preparation of a

medicament for treating a subject infected by a virus selected from among hepatitis C virus,

West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus,

bovine viral diarrhea virus or Japanese encephalitis virus.

15. Use of a compound according to any one of claims I to 5 in the preparation of a

medicament for treating a hepatitis C infection.