TW201215609A - Novel compounds and compositions for the inhibition of NAMPT - Google Patents

Abstract

The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

Description

201215609 VI. Description of the Invention: [Technical Field] The present invention relates to a compound and a composition for inhibiting nicotinamide phosphoribosyltransferase ("NAMPT"), a synthesis, an application thereof, and an antidote. PRIORITY CLAIM This application claims US Provisional Application No. 61/379,789 and No. 61/379,796, filed on Sep. 3, 2010, and U.S. Provisional Application No. 61/386,023, filed on September 24, 2010 Priority of U.S. Provisional Application No. 61/475,813, filed on Apr. 15, 2011, and U.S. Provisional Application No. 61/483,242, filed on May 6, 2011 The contents of the provisional application are fully incorporated herein by reference in its entirety. [Prior Art] The final nicotinamide adenine dinucleotide (NAD) plays an important role in cell energy metabolism and cell signaling. In energy metabolism, the chemical structure of the pyridine ring allows the NAD to readily accept and administer electrons in a hydride transfer reaction catalyzed by numerous dehydrogenases. The preparation of a compound (including several subclasses) which acts as a nicotine indoleamine adenosine nucleotide formation inhibitor and its use as an antitumor agent has been described in patent applications WO 00/50399, WO 97/48695, WO 97/48696, WO 97/48397, WO 99/31063, WO 99/31060, WO 99/31087, WO 99/31064, WO 00/50399 and WO 03/80054. 158436.doc 201215609 One of these inhibitors (E)-N-[4-(l-benzoylpiperidin-4-yl)butyl]-3-(pyridin-3-yl)-propenylamine Also known as AP0866, FK866, WK175 or WK22.175 and hereinafter referred to as FK866 [International Non-Proprietary Name], which is specifically described in the literature as an anticancer agent. FK866 can be used to treat diseases involving disorders of apoptosis, such as cancer. It has been demonstrated in the prior art that FK866 interferes with nicotine guanamine adenine dinucleotide (also known and hereinafter referred to as NAD) biosynthesis and induces apoptotic cell death without any DNA damage. In addition, FK866 ((E)-N-[4-(l-phenylhydrazinopiperidin-4-yl)butyl]-3- φ (pyridin-3-yl)propenylamine) induces cells of HepG2 cells Apoptosis has no fundamental effect on cellular energy metabolism (Hasmann M, Schemainda I. FK866, a Highly Specific Noncompetitive Inhibitor of Nicotinamide Phosphoribosyltransferase, Represents a Novel Mechanism for Induction of Tumor Cell Apoptosis. Cancer Res 2003; 63: 7436-7442. [PubMed: 14612543]). It did not cause immediate cytotoxicity, but cells that inhibited NAMPT and consumed NAD, suggesting that FK866 may be a promising agent for cancer cells that rely on nicotine amide to synthesize NAD φ. The crystal structure of the NAMPT_FK866 complex revealed that the compound binds to the nicotine indoleamine binding site of NAMPT to inhibit its activity. FK866 has been tested in a murine kidney cell carcinoma model and has been shown to exhibit anti-tumor, anti-metastatic and anti-angiogenic activities (Drevs J et al, Antiangiogenic potency of FK866/K22.175, a new inhibitor of intracellular NAD biosynthesis, In murine renal cell carcinoma. Anticancer Res 2003;23:4853-4858. [PubMed: 14981935]) ° 158436.doc 201215609 In a mouse breast cancer model, FK866 also induces tumor growth delay and enhanced tumor radiation sensitivity, accompanied by NAD content, pH and energy status decrease with dose. The chemical sensitivity of FK866 has also been observed in cell death induced by anti-neoplastic 1-methyl-3-nitro-1-nitrosoguanidine (MNNG) in THP-1 and K562 leukemia cell lines (Pogrebniak) A et al, Chemopotentiating effects of a novel NAD biosynthesis inhibitor, FK866, in combination with antineoplastic agents. Eur J Med Res 2006; 11:313-321. [PubMed: 17052966]). The efficacy of GMX1777 was evaluated in a xenograft model and the pharmacokinetic profile of GMX1778 and its response to nicotine indoleamine were measured by liquid chromatography/mass spectrometry. The effect of dinuclear acid cell content (Beauparlant P. et al., Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777. Anticancer Drugs. June 2009; 20(5): 346·54). GMX1777 is a water-soluble prodrug (LEO numbers EB1627 and CHS828, respectively) administered GMX1778 (Gemin X by LEO Pharma) administered intravenously. These compounds and other substituted cyanoguanidines have the structure of Table 1. None of the compounds of the present invention are cyanoguanidine. 158436.doc 201215609 Table 1:

Substituted cyanoguanidine with defined pharmacological effects: A cytotoxic CHS 828; B potassium channel opener pinacidil (Bl) and 12 g of compound as described in Perez-Medrano et al. (B2) And C histamine-II receptor antagonist cimemetidine (from Lovborg # A, BMC Research Notes 2009 2:114 doi:10.1186/ 1756-0500-2-114) Recently, CHS-828 has It was identified as a NAMPT inhibitor (Olesen UH et al, Anticancer agent CHS-828 inhibits cellular synthesis of NAD. Biochem Biophys Res Commun 2008; 367: 799-804. [PubMed: 18201551]). CHS-828 has been shown to effectively inhibit cell growth in a wide variety of tumor cell lines, but the detailed mechanism of this inhibition of CHS-828 has not been determined (Ravaud A et al, Phase I study and guanidine kinetics of CHS-828, a guanidine -containing compound, administered orally as a single dose every 3 weeks in solid tumors: an ECSG/EORTC study. Eur J Cancer 2005; 41: 702-707. [PubMed: 15763645]). Both FK866 and CHS-828 are currently in clinical trials for cancer treatment. 158436.doc 201215609 There are many uses for drugs that inhibit NAMPT. Lack of NAMPT expression strongly affects the development of T lymphocytes and B lymphocytes. Using a mutant form of this protein and a well characterized pharmacological inhibitor (FK866), the authors demonstrate that the ability of NAMPT to regulate cell viability during genotoxic stress requires its enzymatic activity. Collectively, these qualifications indicate that NAMPT is involved in cell resistance to genotoxic/oxidative stress and that it confers the ability of immune system cells to survive stress conditions such as inflammation (Rongvaux, A. et al., /owrwa) / 2008, 181: 4685-4695). NAMPT also has an effect on high glucose levels, oxidative stress on endothelium (EC) and on aging. It is also believed that NAMPT can make proliferative human EC resistant to aging and high glucose oxidative stress, and produce excessive use of glucose to support replication longevity and angiogenic activity. SUMMARY OF THE INVENTION One aspect of the present invention provides a compound, composition, kit, and antidote for use in a mammalian NAMPT pathway having a compound of Formula I: Ο R-1-1-NH~-(CH-(0 )q Ar—(CH2)m X—(CH2)t R4

Wherein: R is aryl, heteroaryl, (: 3-(:8-cycloalkyl, C3-C8 cycloalkenyl, heterocycloalkyl, arylalkyl-, (heteroaryl)alkyl-, (C3-C8 cycloalkyl)alkyl-, (C3-C8 cycloalkenyl)alkyl-, (heterocycloalkyl)alkyl-, (aryloxy) 158436.doc 201215609 烧基·, (杂芳Oxy)alkyl-, (c3_c8 cycloalkyloxy)alkyl-, cycloalkenyloxy)alkyl- or (heterocycloalkyloxy)alkyl-, wherein the heteroaryl group and the heterocyclic ring The alkyl group has a hetero atom number of 1, 2 or 3 and is independently selected from N, s or fluorene, and further wherein the aryl group, the heteroaryl group and the heterocycloalkyl group are each independently aryl or heteroaryl. Substituted or fused to an aryl or heteroaryl group' further wherein one of the aryl group, the heteroaryl group and the heterocycloalkyl group is unsubstituted or optionally substituted independently with one or more substituents 'The substituents may be the same or different and independently selected from the group consisting of hydrazine, halo, cyano, amine, aminoalkyl-, (amino)alkoxy-, _c〇NH2, - C(0)NH(alkyl), _C(0)N(alkyl)2, -C(〇)NH(aryl) -C(0)N(aryl)2, -CHZF3.Z, -〇CHzF3_z, -alkyl, alkenyl, alkynyl, alkoxy, hydroxy, alkyl hydroxy, hydroxy, alkyl hydroxy, or (alkoxyalkyl)amino-, -n(r3)-c(o)-alkyl, -n(r3)-c(o)-aryl, -cycloalkyl, -heterocycloalkyl, - aryl and heteroaryl' are limited to two adjacent ring heteroatoms which are s at different times or not simultaneously;

Ar is an aryl group, a heteroaryl group, a heterocycloalkyl group or a cycloalkyl group, wherein the aryl group, the heteroaryl group, the heterocycloalkyl group and the cycloalkyl group are each unsubstituted or optionally Substituted by 1, 2, 3 or 4 substituents which may be the same or different and independently selected from the group consisting of: anthracene, thiol, cyano, amine, aminoalkyl-, ( Amino)alkoxy_, -CONH2, -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(aryl), -C(0) N(aryl)2, -CHZF3.Z, -OCHzF3-z, -alkyl,-alkenyl, -alkynyl, -alkoxy,hydroxyl,-alkylhydroxy, 158436.doc 201215609 aryloxy-, (alkoxyalkyl)amino,_N(R3)-c(〇)-alkyl, -N(R3)-C(〇)-aryl, _cycloalkyl, heterocycloalkyl, - Aryl and heteroaryl; R4 is cycloalkyl, -CHZF3-Z, aryl, heterocycloalkyl, heteroaryl, alkyl, alkenyl, -alkynyl, (aryl)alkyl-, (heteroaryl)alkyl- or /R1(heterocycloalkyl)alkyl-, or -n\r2, (1) wherein the cycloalkyl group, the aryl group, the heterocycloalkyl group, the heteroaryl group, and the The bases are unsubstituted or as appropriate 1, 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of hydrazine, halo, cyano, amine, aminoalkyl-, Amino)alkoxy_, -CONH2, -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(aryl), -C(0) N(aryl)2, -CHZF3_Z, -OCHzF3-z, -alkyl, alkoxy-, -alkenyl, -alkynyl, aryloxy-, (alkoxyalkyl)amino group _, - ring Alkyl, -heterocycloalkyl, (heterocycloalkyl)alkyl-, -aryl, (aryl)alkyl-, -heteroaryl, (heteroaryl)alkyl-, -s(o) 2-alkyl, -s(0)2-aryl, -S(0)2-CF3, -C(0)N(alkyl)2, -c(0)alkyl, -N(R3)- C(0)-alkyl, -N(R3)-C(0)-aryl, -s(o2)nh2, -s(o2)nh(alkyl), -s(o2)n(alkyl) 2. -N(H)S(〇2)(alkyl), -C(0)N(H)(alkyl) and methylenedioxy, (ii) further wherein the cycloalkyl, the aryl The heterocycloalkyl group and the heteroaryl group may each optionally be fused to an independently selected aryl, heteroaryl, heterocycloalkyl or cycloalkyl group; R3 is a fluorene, alkyl or arylalkyl group. -; X is S, S(O), S(0)2 0 or C(O); 158436.doc -9- 201215609 η is 1, 2, 3 or 4; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0, 1 or 2; And z is 0, 1 or 2; and pharmaceutically acceptable salts, solvates, esters, prodrugs and isomers thereof. Another aspect of the invention is a compound wherein q = 〇, Μ, Μ, R2 A = Ar, X = Q and R4 is - ' and the structural formula is now IB:

N—(CH2)

n-A-Q-N, R2

IB wherein: R and R3 are as defined in formula I; R1 is the same as R2 or is not @, and is independently selected from H, a straight or branched bond ^ to a C7 alkyl, straight or branched CjC7 alkoxy group a direct bond or a branch bond Cl to a C4(tetra)yl group, an aryl group, a heteroaryl group, a heterocyclic alkyl group, and a ring-burned earth, and wherein the heteroaryl group and the hetero atom atom of the heterocyclic alkyl group are independently selected from the group consisting of 4 , 〇 and s 'with the proviso that two adjacent ring heteroatoms are not S at the same time or 不同 at the same time, and mR2 thereof may be unsubstituted or optionally substituted by _ or a plurality of substituents, continually substituted The groups may be the same or different and independently selected from the group consisting of: claw, dentate, cyano, amine, amine alkyl _, (amino) methoxy _ 158436.doc 201215609, _conh2, _C (0 NH(alkyl), -C(〇)N(alkyl)2, _C(0)NH(aryl), -C(0)N(aryl)2, -CHZF3.Z, -OCHzF3-z -alkyl,-alkenyl, -alkynyl, hydroxyalkyl-, alkoxy, hydroxy, alkyl-based, fluorenyl, (alkoxyalkyl)amino-, -alkylamine, amine Carbonyl-, -CHO, -n(r3)-c(o)-alkyl, -n(r3)-c(o)-aryl, -cycloalkyl, -heterocycloalkane A, an aryl group and a heteroaryl group; A is an aryl group, a heteroaryl group, a heterocycloalkyl group or a cycloalkyl group, wherein the aryl group, the heteroaryl group, the heterocycloalkyl group and the ring The alkyl groups are each unsubstituted # or, as the case may be, independently substituted with 1, 2, 3 or 4 substituents which may be the same or different and independently selected from the group consisting of: anthracene, phenyl, cyano, Amino, aminoalkyl, (amino)alkoxy~, -CONH2, -C(0)NH(alkyl), _C(0)N(alkyl)2, -C(0)NH( Aryl), ·<:(0)Ν(aryl)2, -CHzF3.z, -OCHzF3-z, -alkyl,-alkenyl, -alkynyl, -alkoxy,hydroxyl,-alkyl Hydroxy, aryloxy-, (alkoxyalkyl)amino-, -N(R3)-C(0)-alkyl, -N(R3)-C(0)-aryl, -cycloalkane , -heterocycloalkyl, -aryl and -heteroaryl; Q is C(O), S(O), s(0)2, -N(H)-C(0)-, ·3 (〇2)-ΝΗ_ or -N(H)-S(02)-; η is 0, 1, 2, 3 or 4; and ζ is 0, 1 or 2; and its pharmaceutically acceptable salts, Solvate, ester, prodrug or isomer. Another aspect of the invention provides for the provision of a compound derived from formula I using 158436.doc • 11·201215609 in the mammalian nampt pathway agent 'where q=0, m=0 and t=study acceptable salt: compound, composition, kit and detoxification 0, whereby the structural formula becomes formula II or Medicine RN-(CR2R3)n-Ar-χ-Rl

II where: R is included! a 2, 3 or 4 heteroaryl group independently selected from heteroatoms of N, s or fluorene, wherein the heteroaryl group may be substituted by one or more substituents selected from the group consisting of an amine group and a side oxygen group. a group of base and dentate groups; and = wherein the heteroaryl group may comprise - or a plurality of ruthenium-oxides formed with the heteroaryl group;

Ar is aryl or contains! , 2, 3 or 4 heteroaryl groups independently selected from heteroatoms of N, s or fluorene; 'X is s(o)2 or so; R1 is -NHR4, wherein R4 is cycloalkyl, heterocycloalkane a aryl group, an aryl group or a heteroaryl group; a cycloalkyl group; an aryl group; a heterocycloalkyl group; or a heteroaryl group; wherein: (1) the ring-based group 'the aryl group or the heteroaryl group is unsubstituted or 1, 2, 3, 4 or 5 substituents which may be 158, 436. doc -12 to 201215609 identical or different and independently selected from the group consisting of hydrazine, halo, hydroxy, hydroxyalkyl , cyano, -(CH2)mNRaRb, pendant oxy, alkyl, cyanoalkyl, alkyl, alkoxy, εδ alkoxy, alkoxyalkyl-, dilute, fast radical, fast alkyl Oxy, -CONH2, -S-alkyl, -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(cycloalkyl), -C( 0) NH(aryl), -C(0)N(aryl)2, arylalkyl-, arylalkoxy-, aryloxy-, cycloalkyl, heterocycloalkyl, aryl ,(heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, -C(O)heterocycloalkyl, heteroaryl, (heteroaryl)alkyl-, -S(0) 2-alkyl, -S(0)2-aryl, -s(o)2-ch Zf3_z, -c(o)alkyl, -n(r5)-c(o)-alkyl, -n(r5)-c(o)-aryl, -s(o2)nh2, -s(o2) Nh(alkyl), -s(o2)n(alkyl)2, -n(h)(so2)(alkyl) and a fluorenyldioxy group, wherein the cycloalkyl group, the heterocycloalkyl group, Each of the aryl or the heteroaryl group may be substituted with one or more yl, cyano, alkyl or alkoxy groups; and (ii) the cycloalkyl group, the heterocycloalkyl group, the aryl group or The heteroaryl groups may each optionally be fused to an independently selected aryl, heteroaryl, heterocycloalkyl or cycloalkyl group to form a bicyclic or tricyclic group which may be via one or more halo groups, cyanogens Substituted with an alkyl group or an alkoxy group; R2 and R3 may be independently selected from the group consisting of ruthenium and osmium; R5 is ruthenium, alkyl or arylalkyl-;

Ra and RNf, independently selected from the group consisting of hydrazine, alkyl, alkoxy, alkoxyalkyl and 158436.doc -13-201215609 halogenated groups; m is 0, 1, 2, 3, 4, 5 Or 0; and η is 0 or 1. Another aspect of the present invention is a hydrazine compound or a pharmaceutically acceptable salt thereof wherein X = S 〇 2 and the structural formula is: 〇 R 〆 R3

0II, s·II 0 •Ri

IIA wherein: R is a heteroaryl group containing 2, 3 or 4 heteroatoms independently selected from N, s or fluorene, wherein the heteroaryl group may be substituted with one or more substituents selected from the group consisting of a group of free amine groups, pendant oxy groups, and dentate groups; and wherein the heteroaryl group may comprise one or more N-oxides formed with members of the N atom of the heteroaryl group;

Ar is an aryl group or a 5- or 6-membered heteroaryl group containing 2, 3 or 4 heteroatoms independently selected from n, s or fluorene; r1 is -dir 4 and r, cycloalkyl, heterocycle m Or a heteroaryl group; a cycloalkyl group; an aryl group; or a heteroaryl group; wherein: the cycloalkyl group, the aryl group or the heteroaryl group is each unsubstituted or substituted with 5 substituents, and the substitution The groups may be the same or different and independently selected from the group consisting of: I58436.doc • 14- 201215609 氘, dentate, hydroxy, hydroxyalkyl, cyano, -(CH2)mNRaRb, pendant oxy, alkyl, cyanide Alkyl, hydryl, alkoxy, halooxy, alkoxyalkyl, alkenyl, alkynyl, alkynyloxy, -CONH2, -S-alkyl, -C(0) NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(cycloalkyl), -C(0)NH(aryl), -C(0)N(aryl 2, a arylalkyl group, an aryl alkoxy group, an aryloxy group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a (heterocycloalkyl)alkyl group, a (heterocycloalkyl) alkane Oxy-, -c(o)heterocycloalkyl, heteroaryl, (heteroaryl)alkanyl-...s(o)2-alkyl, -S(0)2-aryl, -s( o) 2-chzf3_z, -c(o)alkyl, -n(r5)-c(o)- , -N(R5)-c(o)-aryl, -s(o2)NH2, -s(o2)nh(alkyl), -s(o2)n(alkyl)2, -N(H (S〇2) (alkyl) and a methylenedioxy group, wherein the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may each pass one or more # groups, cyano groups Substituted with an alkyl group or an alkoxy group; and the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may each optionally be independently selected from an aryl group, a heteroaryl group, a heterocycloalkyl group or Rucycloalkyl is fused to form a bicyclic or tricyclic group which may be substituted by one or more halo, cyano, alkyl or alkoxy groups; R2 and R3 may be independently selected from the group consisting of ruthenium and osmium R5 is a ruthenium, a burnt base or an aryl base _;

Ra and Rb are independently selected from the group consisting of fluorene, alkyl, alkoxy, alkoxyalkyl and fluorene groups; and m is 0, 1, 2, 3, 4, 5 or 6. Another aspect of the invention is a compound of formula HA wherein Ar = phenyl, by which 158436.doc -15-201215609 structural formula becomes formula IIB:

R is a bicyclic heteroaryl group containing 1, 2, 3 or 4 heteroatoms independently selected from N, s or fluorene, wherein the heteroaryl group may be substituted by one or more substituents selected from a group consisting of an amine group, a pendant oxy group, and a dentate group; and wherein the heteroaryl group may comprise one or more N-oxides formed with members of the heteroaryl atom; R is -NHR4 and R4 is a cycloalkyl group a heterocycloalkyl, aryl or heteroaryl; cycloalkyl; aryl; or heteroaryl; wherein: the ring, the aryl or the heteroaryl are unsubstituted or 1, 2 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of: oxime, functional group, hydroxy group, hydroxyalkyl group, cyano group, -(CH2)mNRaRb, side oxygen Base, alkyl, cyanoalkyl, dentate, alkoxy, haloalkoxy, alkoxyalkyl-, alkenyl, alkynyl, alkynyloxy, -CONH2, -S-alkyl , -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(cycloalkyl), -C(0)NH(aryl), -C( 0) N(aryl) 2, arylalkyl-, arylalkoxy-, aryloxy- 158436.doc -16 · 201215609, naphthenic , heterocycloalkyl, aryl, (heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, -c(o)heterocycloalkyl, heteroaryl, (heteroaryl) Alkyl-, -S(0)2-alkyl, -S(0)2-aryl, -s(0)2-CHZF3.Z, -C(O)alkyl, -N(R5)-C (0)·Alkyl, -N(R5)-c(0)-aryl, -S(02)NH2, -S(〇2)NH(alkyl), -S(〇2)N(Hybrid 2, -N(H)(S〇2)(alkyl) and fluorenyldioxy' wherein the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group

Each of the groups may be substituted by one or more i groups, cyano groups, alkyl groups or alkoxy groups; and the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may be independently and independently selected as appropriate An aryl, heteroaryl, heterocycloalkyl or cycloalkyl group fused to form a bicyclic or tricyclic group which may be substituted by one or more halo, cyano, alkyl or alkoxy groups; R3 may be independently selected from the group consisting of η and 氘; R5 is fluorene, alkyl or arylalkyl _;

Ra and ... are independently selected from the group consisting of hydrazine, alkyl, alkoxy, alkoxyalkyl and halogen-based groups; m is 0, 1, 2, 3, 4, 5 or 6; z is 0, 1 or 2. Another aspect of the invention is to provide a method of treating a disease by inhibiting NA tolerance in an individual in need thereof, such as a human, by administering to the individual an effective amount of a compound of the invention or a pharmaceutical formulation. . String == an aspect provides a method of treating, preventing, inhibiting, or ameliorating a disease or condition in a heart by administering a therapeutically effective amount to 158436.doc • 17-201215609, a compound of the invention The inhibition is achieved by inhibiting NAMPT in the patient, wherein the disease or condition is selected from the group consisting of cancer, ovarian cancer, breast cancer, uterine cancer, colon cancer, cervical cancer, lung cancer, prostate cancer, skin cancer, bladder cancer, Pancreatic cancer, leukemia, lymphoma, Hodgkin's disease, viral infection, Human Immunodeficiency Virus, hepatitis virus, pancreatic virus, herpes simplex, inflammatory disease, colonic irritable syndrome , inflammatory bowel disease, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, osteoarthritis, osteoporosis, dermatitis, atopic dermatitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, Ankylosing spondylitis, graft versus host disease, Alzheimer's disease, cerebrovascular accident, atherosclerosis, sugar Disease, spheroid nephritis, metabolic syndrome, non-small cell lung cancer, small cell lung cancer, multiple myeloma, leukemia, lymphoma, squamous cell carcinoma, kidney cancer, ureter and bladder cancer, head and neck cancer, brain and central nervous system cancer. Another preferred embodiment is a pharmaceutical formulation comprising a pharmaceutically acceptable compound of the invention which results in a reduction in tumor burden and/or metastasis upon administration to a human. Pharmaceutical formulations can be administered by oral means or other suitable means. Another embodiment is a method of treating ovarian cancer in an individual (e.g., a human) in need thereof' by administering to the individual an effective amount of a compound of the invention or a pharmaceutical formulation. Further, the embodiment is a method of treating colon cancer in an individual (e.g., a human) in need thereof by administering to the individual an effective amount of a compound of the invention 158436.doc 201215609 or a pharmaceutical formulation. Another embodiment is a method of treating breast cancer in an individual in need thereof, such as a human, by administering to the individual an effective amount of a pharmaceutical formulation of the invention. Another embodiment is a method of treating white blood disease in an individual (e.g., a human) in need thereof' which is accomplished by administering to the individual an effective amount of a compound of the invention or a pharmaceutical formulation. Another embodiment is a method of treating colon cancer in a subject (eg, a human) in need thereof before or after surgical resection and/or radiation therapy by administering to the individual an effective amount of a compound or medicament of the invention Formulations are achieved. Another embodiment is a method of treating cancer in a subject (eg, a human) in need thereof before or after surgical resection and/or radiation therapy by administering to the individual an effective amount of a compound of the invention or a pharmaceutical formulation Achieve adjunctive therapy including nausea in the presence or absence of dexamethasone. Another embodiment is a method of treating cancer in a subject (eg, a human) in need thereof before or after surgical resection and/or radiation therapy by administering to the individual an effective amount of a compound or medicament of the invention Formulations to achieve 'including adjuvant therapy with one or more additional therapeutic agents or their pharmaceutically acceptable salts. Non-limiting examples of such additional therapeutic agents include cytotoxic agents such as, but not limited to, DNA interacting agents (such as cisplatin or cranberry (d〇x〇 rubicin)); taxanes (eg, purple) Taxotere, taxol (tax〇1)); topoisomerase η inhibitors (such as 158436.doc •19·201215609 etoposide); topoisomerase I inhibitors (such as irinotene) Irinotecan (or CPT-11), campt〇star or topotecan); tubulin interacting agents (such as paclitaxel, docetaxel or Epothilone); a hormonal agent (such as tamoxifen); a thymidylate synthase inhibitor (such as 5-fluorouracil or 5-FU); an antimetabolite (such as methotrexate ( Methoxrexate)); a burning agent (such as temozolomide, cyclophosphamide); a farnesyl protein transferase inhibitor (such as SARASARtm (4-[2-[4-[(11R)-3,10) - φ 二漠-8-gas-6,11-di-milk-511-benzo[5,-6]cycloheptazone[1,2-1)]0pyridin-11-yl-]-1 - piperidine ]-2-Sideoxyethyl]-1-piperidine-carbenamide or SCH 66336), for tipifarnib (Zarnestra® or R115777 from Janssen Pharmaceuticals), L778, 123 (farnesyl protein transferase inhibitor from Merck & Company, Whitehouse Station, NJ), BMS 214662 (Farnesyl protein transferase inhibitor from Princeton, New Jersey) Bristol-Myers Squibb φ Pharmaceuticals (Princeton, NJ·); signal transduction inhibitors (such as Iressa® (Astra Zeneca Pharmaceuticals, England), Tarceva® (EGFR kinase inhibitor), EGFR antibody (eg C225), GLEEVEC® (C-abl kinase inhibitor, from Novartis Pharmaceuticals, East Hanover, NJ); interferon, such as intron ® (from Merck & Company), Peg-Intron® 158436.doc -20- 201215609 (from Merck &Company); hormone therapy combination; Aromatase combination; ara-C, adriamycin, cytoxan, and gemcitabine.

Other anticancer agents (also known as antibiotics) include, but are not limited to, Uracil mustard, Chlormethine, Ifosfamide, Melphalan, Chlorambucil, Pipobroman, Triethylenemel amine, Triethylenethiophosphoramine, Busulfan, Carmust, Ting (Carmustine), Lomustine, Streptozocin, Dacarbazine, Floxuridine, Cytarabine, 6-mercaptopurine (6) -Mercaptopurine), 6-Thioguanine, Fludarabine phosphate, oxaliplatin, leucovirin, ELOXATIN® From Sanofi-Synthelabo Pharmaceuticals (France), Pentostatine, Vinblastine, Vincentine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin, Xiaohong, Epirubicin, Idarubicin, Mithramycin, deoxycofumycin ( Deoxycoformycin), Mitomycin-C, L-Asparaginase, Teniposide, 17α-Ethinylestradiol, 158436.doc -21 - 201215609 Diethylstilbestrol, Testosterone, Prednisone, Fluoxymesterone, Dromostanolone propionate, vinegar (Testolactone), Megestrolacetate, Methylprednisolone, Methyltestosterone, Prednisolone, Triamcinolone, Chlorotrianisene, Hydroxyprogesterone, Aminoglutethimide, Estramustine, Medroxyprogesteroneacetate, Leuprolide, Flutamide, Toremifene, goserelin, carboplatin, Hydroxyurea, Amsacrine 'Procarbazine, mitoxantan (Mitotane), Mitoxantrone, left-handed meters. Levamisole, Navelbene, Anastrazole, Letrazole, Capecitabine, Reloxafine, Droloxafine ), Hexamethylmelamine, Avastin, herceptin, Bexxar, Velcade®, Zevalin, Trisenox Xeloda, Venorelbine, Porflmer, Erbitux, Liposomal, Thiotepa, hexamine melamine Altretamine), Melphalan, Trastuzumab, Lerozole, IL Fulvestrant, Exemestane 158436.doc -22- 201215609 (Exemestane), Isocyclic Phosphate Indoleamine, Rituximab, C225' and Campath, 5-fluorouracil and leucovorin, with or without a 5_HT3 receptor inhibitor (eg, dolasetron) (dolansetron), granisetron (granisetr〇n), ondansetron (ondansetron), with or without a plug Pine. If formulated as a fixed dose', such combination products employ a compound of the invention within the dosage range described herein (or as known to those skilled in the art) and other pharmaceutically active agents or treatments within their own dosage range. For example, s ' has found that the CDC2 inhibitor 奥i〇niucine synergizes with known cytotoxic agents in inducing apoptosis (j. Cell Sci., (1995) 108, 2897). When the combined formulation is not appropriate, the compounds of the invention may also be administered sequentially with known anticancer or cytotoxic agents. The administration sequence of the present invention is not limited in any combination therapy; the compound of the disclosed formula can be administered before or after administration of a known anticancer or cytotoxic agent. For example, the cytotoxic activity of the cyclin-dependent kinase inhibitor flavopiridol is affected by the anticancer agent administration sequence. Cancer Research, (1997) 57, 3375. These techniques are within the skill of those skilled in the art and the attending physician. By administering a fluid (such as water), a Heinz ring diuretics, one or more chemotherapeutic agents or anti-neoplastic agents (such as formazan tetrahydrofolate and fluorouracil) and an auxiliary chemotherapeutic agent ( Any combination of such agents, such as filgrastim and erythropoietin, or any of the foregoing agents, enhances any of the foregoing methods. Another embodiment is a method of administering a compound of the formula 158436.doc • 23-201215609 to a subject in need thereof, such as a human. It is a method of preparing a pharmaceutical formulation of the present invention by administering to the subject another embodiment of the present invention by using at least one pharmaceutically acceptable compound of the present invention and optionally One or more pharmaceutically acceptable additives or excipients are mixed to achieve. With regard to the preparation of pharmaceutical compositions from the compounds described herein, the pharmaceutically acceptable inert carrier can be either solid or liquid. Solid form preparation packages: powders, lozenges, dispersible granules, capsules, cachets, and test agents. Powders and granules may comprise from about 5% to about 95% of the active ingredient. Suitable solid carriers are those in the art (4), such as magnesium carbonate, magnesium stearate, talc, sugar or lactose. Tablets, powders, cachets and capsules can be used as solid dosage forms suitable for oral administration. Examples of pharmaceutically acceptable carriers and methods of making various compositions can be found in A. Gennar(R) (eds.), Remingt〇n, s.

Pharmaceutical Sciences, ^ 18^, (i99〇) 5 Mack Publishing Co., Easton, Pa. Liquid form preparations include solutions, suspensions and emulsions. As an example, a water or water propylene glycol solution for parenteral injection may be mentioned, or a sweetener and an opacifier may be added for the π solution, suspension and emulsion. Liquid form preparations may also include solutions for intranasal administration. Formulations suitable for inhalation of aerosols may include solutions and solids in powder form which may be combined with a pharmaceutically acceptable carrier such as an inert compressed gas such as nitrogen. It is also intended to be converted into a solid form preparation for oral or parenteral administration of a liquid form preparation of 158436.doc • 24 · 201215609. Such liquid forms include solutions, suspensions and emulsions. The compounds of the invention may also be delivered transdermally. The transdermal compositions can be in the form of creams, lotions, aerosols and/or emulsions and can be included in a matrix or reservoir type transdermal patch which is conventionally used in the art for this purpose. The compounds of the invention may also be administered subcutaneously, preferably by oral or intravenous administration. The pharmaceutical preparation is preferably in unit dosage form. In this form, the preparation is subdivided into unit doses of suitable size containing the appropriate amount of the active ingredient, for example, an amount effective to achieve the desired purpose. The amount of active compound in a unit dosage formulation may be varied or adjusted, from about 1 mg to about 1000 mg, preferably from about 1 mg to about 5 mg, more preferably from about i mg to about 250 mg, depending on the particular application. More preferably from about i mg to about 25 mg. The actual dosage employed can vary depending on the needs of the patient and the severity of the condition being treated. The appropriate dosage regimen for determining a particular situation is within the scope of this technical february b. For convenience, the total daily dose can be divided into several parts as needed and administered in several portions over the course of a day. The amount and frequency of administration of the compound of the present invention and/or its pharmaceutically acceptable salt will be adjusted according to the judgment of the attending clinician, taking into consideration factors such as the age, condition and size of the patient and the severity of the condition being treated. A typical recommended daily dosage regimen for oral administration can be administered in divided doses of from about 2 mg per day to about 500 mg per day, preferably from 1 mg per day to 200 mg per day, in two to four divided doses. 158436.doc -25 • 201215609 Definitions Unless otherwise stated, the following terms are understood to have the following meanings as used above and throughout the present invention. If the definition is missing, it is subject to the well-known definitions known to those skilled in the art. "Patient" includes humans and animals. "Mammal" means humans and other mammals. The term "inhibitor" refers to a molecule such as a compound, drug, enzyme activator or hormone that blocks or otherwise interferes with a particular biological activity. The term "effective amount" or "therapeutically effective amount" means an amount of the agent sufficient to provide the desired biological effect. This effect may be a reduction and/or alleviation of the symptoms, symptoms or causes of the disease, or any other desired change in the biological system. For example, an "effective amount" for therapeutic use is an amount of a composition comprising a compound as disclosed herein required to provide a clinically significant reduction in disease. The appropriate "effective" amount in any individual case can be determined by a general practitioner using routine experimentation. Therefore, the expression "effective amount" generally means the amount of the active substance used for the therapeutic effect. In the case of the present invention, the active substance is an inhibitor of the formation of nicotine guanamine phosphoribosyltransferase (NAMPT). As used herein, the term "treatment" is synonymous with the term "prevention" and is intended to mean delaying the progression of the disease, preventing the progression of the disease, and/or reducing the severity of the symptoms that will or will be expected to develop. Thus, these terms include improving the symptoms of existing diseases, preventing other symptoms, ameliorating or preventing the underlying metabolic cause of the symptoms, inhibiting the condition or disease, such as preventing the progression of the condition or disease, alleviating the condition or disease, resolving the condition or disease, and alleviating the disease. Or the condition caused by the condition' or the symptoms of the disease or condition are prevented. 158436.doc •26- 201215609 “Pharmaceutically acceptable” or “pharmacologically acceptable” means a substance that is biologically or otherwise substantially desirable, that is, the substance can be administered to an individual without It can cause any substantially undesirable biological action or interaction with any component of the composition containing the substance in a substantially deleterious manner. Exemplary salts include, but are not limited to, sulfates, sulphates, acetic acid grasses, abalones, bromides, iodides, nitrates, hydrosulfite, and sulphuric acid salts. Acid salt, lactate, salicylic acid

Acidic citrate, tartrate, oleate, tannin, pantothenic acid 'hydrogenated sulphate, ascorbate, succinate, gentisate maleate, fumarate , gluconate, glucuronic acid glucaric acid salt, formate, benzoate, a face acid salt, a smoldering i (salt salt), bismuth acid salt, benzoic acid Salts, p-toluene and acid naphthenates (i.e., u, methylene-bis(tetra)yl)-carboxate pharmaceutically acceptable salts may be included to include, for example, acetate ions, succinate ions Or another molecule of other relative ions. The relative ion may be any organic or inorganic moiety that stabilizes the charge on the parent compound. Further, the pharmaceutically acceptable salt may have more than one charged atom in its structure. Where the plurality of charged atoms are part of a pharmaceutically acceptable salt, the pharmaceutically acceptable salt may have a plurality of relative ions. Thus the 'pharmaceutically acceptable salt may have - or more Charged atom and / or one or more relative ions. "Carrier substance" or "Excipients" include any convenient excipients in pharmaceutical manufacture and should be selected based on compatibility and release profile characteristics of the desired dosage form. Exemplary carrier materials include, for example, binders, suspensions, 158,436 .doc •27· 201215609 Decomposing agents, fillers, surfactants, solubilizers, stabilizers, lubricants, wetting agents, diluents and the like. “Pharmaceutically compatible carrier materials” may include, for example, Arab Gum, gelatin, colloidal cerium oxide, glycerol calcium hydride, calcium lactate, maltodextrin, glycerin, magnesium citrate, casein sodium, soy lecithin, sodium carbonate, tricalcium phosphate, dipotassium phosphate, hard Lipid-based sodium lactate, carrageenan, monoglyceride, diglyceride, pregelatinized starch and the like. See, for example, Hoover, John E, and ^

Pharmaceutical Sciences, Mack Publishing Co., Easton, Pa. 1975. ’

As used herein, the term "individual" encompasses both mammalian and non-mammalian mammals. Examples of milk animals include, but are not limited to, any member of the mammalian class, human, non-human primates, such as black, and others.猿 and farm animals: such as cattle, horses, brocade sheep, goats, pigs; livestock, various 'fine, continuous animals, including rodents, such as rats, mice and ^天包: gas is not limited to two and? Wide object. Examples of non-mammals include (but mammals are human-like animals. In the present invention - examples,

As used herein, "chain or minute, alkyl" means a saturated straight radical having from 1 to 10 carbon atoms, n-propyl. Representative saturated alkyl groups include, but are not limited to, methyl, ethyl-1-diisopropyl, 2-mercaptopropyl, 2-methyl-2-propyl, 2-yl-1-propyl Methyl-1. butyl, 2-methyl I butyl monomethyl, 2-methyl-2 yl pentyl, 3 methyl sulfhydryl, 4 methyl-1-pentyl dimethyl Di-A-pentyl, 3-indolyl-2-pentyl, 4·decyl-2-pentyl, 2,2_, 3,3·didecyl-1·butyl, 2-ethyl-b-butyl, Ding 158436.doc -28- 201215609 base, isobutyl &, tert-butyl, n-pentyl, isopentyl, neopentyl, n-hexyl and the like, and longer alkyl 'such as heptyl and Octyl and its similar groups. The alkyl group can be unsubstituted or substituted. The alkyl group having three or more carbon atoms may be a straight chain, a branched chain or a cyclic group. As used herein, "low carbon alkyl" means an alkyl group having from 1 to 6 carbon atoms. As used herein, "alkenyl" includes unbranched or branched hydrocarbon chains having one or more double bonds. The double bond of the alkenyl group may be non-conjugated or conjugated to another unsaturated group. Illustrative alkenyl groups include, but are not limited to, (C2_C8) alkenyl groups such as ethyl hexyl alkenyl, vinyl, allyl, butenyl, pentenyl, hexenyl, butadienyl, pentadienyl , hexadienyl, 2-ethylhexenyl, 2-propyl-2-butenyl, 4-(2-methyl-3-butenyl)-pentenyl and the like. The alkenyl group may be unsubstituted or substituted. The term "hydroxyalkyl" means that at least one hydrogen atom of the alkyl group in the alkyl group as defined above is replaced by a hydroxyl group. Examples of hydroxyalkyl groups include, but are not limited to, methyl, ethyl, propyl, isopropyl, isobutyl 't-butyl, tert-butyl, pentyl, wherein one or more hydrogen atoms are replaced by OH. Or n-hexyl, and • their hydroxyalkyl groups as specified in the examples below. The term "cyanoalkyl" denotes an alkyl group as defined above wherein at least one hydrogen atom of the alkyl group is replaced by a cyano group (-CN). As used herein, "alkynyl" includes one or more referenced bonds. A branched or branched hydrocarbon chain. The paraxyl bond may be non-conjugated or conjugated to another unsaturated group. Suitable alkynyl groups include, but are not limited to, (C2_C6)alkynyl groups such as ethynyl, propynyl, butynyl, pentynyl, hexynyl, methylpropynyl, 4-methyl-1-butyl Alkynyl, 4-propyl-2-pentynyl, 4-butyl-2-hexynyl and 158436.doc • 29. 201215609. An alkynyl group can be unsubstituted or substituted. The term "functional base" means that at least one hydrogen atom of the base of the hospital, as defined above, is preferably replaced by fluorine, preferably by fluorine or chlorine. Examples of haloalkyl groups include, but are not limited to, mercapto 'ethyl, propyl, isopropyl, isobutyl, t-butyl, substituted with one or more hydrogen atoms via a Cl, F, Br or I atom, The third butyl, pentyl or n-hexyl group, and the _alkyl groups specifically recited in the Examples below. Preferred alkyl is monofluoro, difluoro- or trifluoro-methyl, -ethyl or propyl, such as 3,3,3-trifluoropropyl, 2-fluoroethyl, 2,2, 2-Trifluoroethyl, fluoroindenyl, trifluoromethyl. The terms "trifluoromethyl", "sulfonyl" and "carboxy" include cf3, so2 and co2h, respectively. The term "sideoxy" means a fluorene group. The term "hydroxy" means an OH group. The term "alkoxy" as used herein includes -〇-(alkyl) wherein alkyl is as defined above. The term "aminoalkyl" as used herein means having one or more nitrogen atoms and a group having one or more alkyl groups as defined above. "Aralkyl" or "arylalkyl" means aryl-alkyl-, wherein aryl and alkyl are as previously described. Preferred aryl groups comprise a low carbon alkyl group. Non-limiting examples of suitable aralkyl groups include benzyl, 2-phenethyl and naphthylfluorenyl. The bond to the parent moiety is achieved via an alkyl group. "Heteroarylalkyl" means a heteroaryl moiety as defined herein attached to the parent core via a decyl moiety (defined above). Non-limiting examples of suitable heteroaryl groups include 2-pyridylmethyl, quinolinylmethyl and the like. 158436.doc -30·201215609. "Heterocyclyl thio" means a heterocyclyl moiety as defined herein attached to the parent core via a thiol moiety. Non-limiting examples of suitable heterocyclic base groups include. Stationary methyl 1-azinylmethyl and its = group.

The term "bicyclic heteroaryl" means a structure in which an atom is distributed in a ring in which two rings (each ring shares at least two atoms) and at least one ring is a heteroaryl group. Non-limiting examples of bicyclic heteroaryl groups include bicyclic heteroaryl groups comprising i, 2, 3 or 4 heteroatoms independently selected from N, w〇. It should also be noted that any carbon and heteroatoms in the text, procedures, examples, and tables that have an unsaturated valence state should have a sufficient number of gas atoms to saturate the valence state. When any variable (e.g., 'aryl, heterocycle, r2, etc.) occurs more than - times in any component or structure, its occurrence at each occurrence is independent of its definition in all other instances.

The N-oxide formed by the N atom member of the heteroaryl group represents an N-oxide formed by the nitrogen atom contained in the heteroaryl group. Illustrative and non-limiting examples of such ruthenium oxides are:

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As used herein, the term "composition" is intended to cover a product comprising a specified quantity of the specified ingredients, and any product that is produced directly or in combination by a specified combination of the specified ingredients. The term "氘" as used herein means a stable hydrogen isotope having a single proton and a neutron. The term "halo" as used herein means a substituent having at least one element selected from the group consisting of fluorine, gas, bromine and iodine. The term "cyano" as used herein means a substituent having a carbon atom bonded to a nitrogen atom by a bond. As used herein, "amino" means a substituent containing at least one nitrogen atom. The term "(amino)alkoxy" as used herein means a substituent having at least one amine group and at least one alkoxy group. The term "aryloxy" as used herein, means a substituent of the formula ,0, wherein Ar is aryl as defined herein. The term "methylenedioxy" as used herein means a functional group of the formula -O-CH^O- which is attached to the molecule via two chemical bonds via oxygen. As used herein, "alkoxyalkyl" means -(alkyl)-oxime-(alkyl), wherein each "alkyl group" is independently an alkyl group as defined above. 158436.doc •32· 201215609 The term "(alkoxyalkyl)amino group" as used herein, means having at least one alkoxy group as defined above and at least one amine as defined above. Substituent substituent. The term "spiroheteroalkyl" as used herein means that a spiro group (without a hetero atom) is attached to the heterocycloalkyl group in a spiro manner. Non-limiting examples will be the sections shown below:

The term "heterospirocycloalkyl" as used herein means a spiro group (containing a hetero atom such as 0, N or S) which is spiroly attached to a heterocycloalkyl group. Non-limiting examples will be the parts shown below:

"Aryl" means a monovalent aromatic hydrocarbon group having 6 to 20 carbon atoms (c^c^) obtained by removing a hydrogen atom from a single carbon atom of a parent aromatic ring system. Some aryl groups are represented in the exemplary structure as rAr"e aryl groups including

A bicyclic group containing an aromatic ring fused to a saturated, partially unsaturated ring or an aromatic carbocyclic ring. Typical aryl groups include, but are not limited to, those derived from benzene (phenyl), substituted stupid, naphthalene, onion, biphenyl, fluorenyl, fluorenyl, dinitrogen, trifluoronaphthyl, and the like. The group. The aryl group is optionally substituted independently by one of the substituents described herein. Illustrative examples of aryl groups include, but are limited to, phenyl, naphthalene, and the following: 158436.doc -33- 201215609

Illustrative substituted aryl groups include:

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F F F

F F

F

F F

F

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As used herein, the term "heteroaryl ring atom monocyclic (tetra) polycyclic, ^^ has 3 to 24

The atom and the nitrogen, oxygen and/or sulfur atom have a structure selected from the carbon language "heteroaryl" and also include 5g „ as used herein, including a 5 member, 6 member or 7 member ring group and including the right s 1 ΠΜ /5 2 DA 1 稠 力 匕 匕 稠 稠 稠 稠 稠 稠 稠 稠 稠 稠 稠 稠 稠 稠 稠 具有 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 /5 Examples of heteroaryl groups include, but are not limited to, pyridyl, imidazolyl, imidazopyridyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, tetrazolyl, furyl, thienyl, iso Oxazolyl, thiazolyl, oxazolyl, isothiazolyl, pirolidol, quinolyl, isoquinolinyl, fluorenyl, benzimidazolyl, benzophenone 158436.doc -41· 201215609 , 碎 基 , ° °. 圭 基 丨 ° ° ° Qin, Ou Qin Qin, 嗓 嗓, triazinyl, isodecyl, acridinyl, fluorenyl, oxadiazolyl, triazolyl , thiadiazolyl, furazanyl, benzofurazinyl, benzothienyl, benzothiazolyl, benzoheptyl, sulfhydryl, quinone, 啥喏琳基, 哈咬基, and η Fu The pyridyl group. The spiro moiety is also included within the scope of this definition. Heteroaryl groups may be independently substituted with one or more substituents as described herein. A 5- or 6-membered heteroaryl group may optionally be substituted as appropriate. a group consisting of pyridyl, pyrimidinyl, thiazolyl, imidazolyl, oxazolyl, isooxazolyl, pyrazolyl, pyridone, and benzimidazolyl. In a particular embodiment, a heteroaryl It is selected from the group consisting of benzothiazepine, dihydrogen peak bite, and dihydrogen η ratio. It is determined by mouth biting, dihydropyrazine and D than biting, 吱 并 ° ° ° ° ° ° ° 唾 & & 比 比 比° Sit and ° than β sitting, Mi. Sitting and β than bite, Mi Wei and ^ ° fixed, called 丨 ° sitting, ° 引 °, 喧 · 咱, 咱 、, ° ° ° ° ° ° ° bite, 》 嘻 嘻 0 、, tetrazolopyridine, tetrahydroimidazopyridine, tetrahydropyrazolopyridine, 嗓0 sit and pyridine and thienopyridine bicyclic heteroaryl. In another embodiment' The heteroaryl group is selected from the group consisting of 1Η-pyrazolo[3,4-b]ebipyridine; 1,4,6,7-tetrahydro-pyridinium[4,3-c]pyridine; 78-dihydrogen _5Η·pyrido[4,3-d]pyrimidine; 5,7-diaza ratio 11 each [3,4-b]pyridine; 7,8-two _5H-[1,6] acridine; l, 4,6,7-tetraqi-flavor. Sit and [4,5-c]pyridine; i,8a-dihydroimidazo[l,2-a]pyridine; thiophene And [3,2_c]pyridine; 1H-imidazo[l,2-b]pyrazole; 1H-biazolo[3,4-b] ratio of '°f-[2,3-c]0 ratio Bite; ΙΗ-η ratio. Sit and [3,4-b]» than bite; 1H-«• bis-[3,2-c]pyridine; thieno[2,3-b]*»bipyridine; Imidazo[l,2-a]pyrimidine bite. Nanhe [2,3-c]. Bipyridine; isoquinoline; 1H-carbazole; imidazo[l,2-a]bipyridine, thieno [2,3-c]pyridine; furo[2,3-c]pyridine; in-pyrrolo[2'3_C]pyridine; imidazo[l,2-a]pyrazine; iota, 3-benzothiazole Benzo[d] 158436.doc 201215609 Thiazole; 1H_pyrrolo[2,3-b]pyridine; [u]thiazolo[5,4_c]pyridine; [1,2,3,4]tetrasal[ l,5-a]0 than bite; l,5-habit; lH-n bow; rice saliva [4,5-c] pyridine bite; and 1,6-peak bite bicyclic heteroaryl.

By way of example and without limitation, the carbon-bonded heterocyclic and heteroaryl groups are at the 2, 3, 4, 5 or 6 position of the pyridine; the 3, 4, 5 or oxime of the oxazine Position; position 2, 4, 5 or position of pyrimidine; position 2, 3, 5 or 6 of pyrazine; 2 positions of furan, tetrahydrofuran, thiofuran, thiophene, pyrrole or tetrahydropyrrole 3, 4 or 5; 2, 4 or 5 of oxazole, imidazole or thiazole; 3, 4 or 5 of isoxazole, pyrazole or isothiazole; 2 positions of aziridine Or 3 positions; 2, 3 or 4 positions of azetidine; 2, 3, 4, 5, 6, 7 or 8 of quinoline; or 1 and 3 of isoindole 4-digit 5-, 6-, 7- or 8-bit bonding. Other examples of the carbon-bonded heterocyclic ring include 2-pyridyl, 3-pyridyl, 4·pyridyl, 5-pyridyl, heart-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 5-indole Zinyl, 6-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 6-pyrimidinyl, 2-pyrazinyl, % pyrazinyl, 5-pyrazinyl, 6-pyrazinyl , 2_thiazolyl, 4-thiazolyl or 5_ °. For example and without limitation τ, nitrogen-bonded heterocyclic rings and heteroaryl groups are in the form of acetophenone, azetidin, material, bite, 2" bilorin, 3 lin, imidazole, imidazole , 2_imidazoline, 3_imidazoline, pyrazole, pyrazoline, 2· " specific oleoline, 3-η-biazoline, Niangbita, piperazine, sputum, porphyrin, azole 1 position; 2 positions of isoindole or iso-β-roofing; 4 position of morpholine; and 9-position of (4) or β-carboline. Base, 1-azetidinyl group More generally, The nitrogen-bonded heterocyclic ring includes 丨-aziridine, 1-pyrrolyl, 1-imidazolyl, pyrazolyl and 158436.doc •43·201215609 1 - 〇 base bite. The term "bicyclic heteroaryl" means The atom is distributed in a structure in which two rings fused together, wherein each ring shares at least two atoms, and at least one ring is a heteroaryl ring. Non-limiting examples of bicyclic heteroaryl groups include, but are not limited to:

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analog. Other examples of bicyclic heteroaryl groups include, but are not limited to:

These bicyclic heteroaryl groups can be substituted as defined herein for R. As used herein, the terms "cycloalkyl" and "cycloalkenyl" refer to a saturated or partially saturated, monocyclic or fused or spiro polycyclic carbocyclic ring having from 3 to 24 ring atoms per ring. Illustrative examples of cycloalkyl and "cycloalkenyl" include (but are not limited to: 158436.doc -45 - 201215609) the following sections:

As used herein, the term "heterocycloalkyl" refers to a mono- or fused or spiro polycyclic structure of each of the selected atoms and the ring atoms of the N, fluorene and ... atoms. Illustrative examples of heterocyclic and substituted heterocyclic thio groups include, but are not limited to:

C. , 〇, on >, 158436.doc -46 - 201215609

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And its analogues. Numerical ranges as used herein are intended to include consecutive integers. For example, the range expressed as "0 to 4" should include 0, 1, 2, 3, and 4. As used herein, the term "substituted" means that the specified group or moiety bears one or more suitable substituents. The term "unsubstituted" as used herein means that the specified group has no substituent.

As used herein, the term "optionally substituted" means that the specified group is unsubstituted or substituted with one or more substituents. When a polyfunctional moiety is displayed, the point of attachment to the core is indicated by a line. By way of example, '(cycloalkyloxy)alkyl- means that the alkyl group is the point of attachment to the core and the cycloalkyl group is attached to the alkyl group via an oxy group. The expression "adjuvant chemotherapeutic agent" generally refers to an agent that can treat, alleviate, alleviate or ameliorate the side effects of a chemotherapeutic agent. Such agents include agents that modulate blood cell growth and maturation. Examples of adjunctive chemotherapeutic agents include, but are not limited to, filgrasin and erythropoietin. Other such ancillary chemotherapeutic agents include inhibition associated with administration of a chemotherapeutic agent. evil,. Agents such as 5_HT3 receptor inhibitors (eg, dolaste, granise or ondansetron), with or without dexamethasone. The term "chemotherapeutic agent" & "anti-biological agent" generally refers to an agent that can treat, prevent, cure, heal, alleviate, alleviate, alter, remedy, ameliorate, alter, or circumvent a malignant disease and its metastasis. Examples of such agents (also known as 158436.doc •53·201215609 antibiotics) include, but are not limited to, prednisone (eg, paste, a..., ratio = (bicalutannde), carboplatin, cis Platinum, chlorambucil, cisplatin, carboplatin, docetaxel, cranberry, dutamine, interferon-a, lysine, leuprolide, megestrol _, mitomycin, Orsay, Pacific yew, pUCamycin (MithracinTM), tamoxifen thiotepa, topotecan, valrubiein, vinca test, Changchun test and any description Any combination of substances. Other such agents are described later. "Nicotine guanamine phosphoribosyltransferase" (also known as NAMPT, NMPRT, NMPRT or NAmPRT) (International name: E c 2·4·2· 12 ) is a key enzyme in the biosynthesis of nicotinamide adenosine dinucleotide (NAD) from the natural precursor nicotinic guanamine. It should be noted that 'unless the context clearly dictates otherwise', otherwise the application and accompanying application The singular forms "a" and "the" are used in the <Desc/Clms Page number> The inhibitor of the formation of nicotine guanamine phosphoribosyltransferase (NAMPT) described herein can be administered with one or more physiologically acceptable excipients. Physiologically acceptable carrier or form An agent is a formulation to which a compound may be added to solubilize or otherwise facilitate its administration. The dosage form of the invention may contain a mixture of one or more compounds of the invention, and may include those known to those skilled in the art as medicinal forms. Other pharmaceutical agents include, for example, the following: Stabilizing additives can be incorporated into the transfer agent solution. With respect to some drugs, the presence of such additives promotes stability and dispersibility of the agent in the solution. Stabilizing additives The concentration used can be 158436.doc • 54· 201215609 in the range of about 0.1% to 5% (W/V), preferably about 5% (w/v). Suitable, but non-limiting, stabilization additives Examples include gum arabic, gelatin, decyl cellulose, polyethylene glycol, carboxylic acids and salts thereof, and polylysine. Preferred stabilizing additives are gum arabic, gelatin and sulfhydryl cellulose. Acetic acid, glacial acetic acid Citric acid, fumaric acid, hydrochloric acid, dilute hydrochloric acid, malic acid, nitric acid, phosphoric acid, dilute phosphoric acid, sulfuric acid, tartaric acid); aerosol propellant (butane, dichlorodifluoromethane, dioxane tetrafluoroethane) , isobutane, propane, tri-gas monofluoromethane); venting agent (carbon dioxide, • nitrogen); alcohol denaturant (denatonium benzoate, methyl isobutyl ketone, sucrose octaacetate) Ester); alkalinizing agent (concentrated ammonia / gluten solution, acid I*, monoethanolamine 'diisopropanolamine, hydrazine hydroxide, sodium carbonate, sodium sulphate, sodium carbonate, sodium hydroxide, triethanolamine); Anti-caking agent (see net 鸢漱); antifoaming agent (dioxane, polydioxane), antimicrobial preservative (gasified benzoquinone ammonium, gasified benzoic acid solution, Gasification excerpts (benzelthonium chloride), benzoic acid, sterols, butyl perbenzoate, hexadecane hexyl chloride, butyl alcohol, chlorophenol, phenol, dehydroacetic acid , p-hydroxybenzoic acid ethyl ester, p-hydroxybenzoic acid methyl ester, sodium p-hydroxybenzoate, phenol, benzene , phenylmercuric acetate, phenylmercuric nitrate, potassium benzoate, potassium sorbate, propyl p-hydroxybenzoate, sodium propyl p-hydroxybenzoate, sodium benzoate, sodium dehydroacetate, sodium propionate, sorbic acid, Thimerosal, thymol; antioxidants (ascorbic acid, ascorbyl palmitate, butylated hydroxymethoxybenzene, butylated hydroxytoluene, hypophosphorous acid, monothioglycerol, gallic acid Ester, sodium formaldehyde sulfalate, sodium metabisulfite, sodium thiosulfate Ammonium carbonate, ammonium phosphate, boric acid, citric acid, lactic acid, phosphoric acid, potassium citrate, potassium metaphosphate, potassium dihydrogen phosphate, sodium acetate, sodium citrate, sodium lactate solution, disodium hydrogen phosphate, sodium dihydrogen phosphate; Lubricant (see Ingot Hao and 缪瓛縻#/); chelating agent (disodium edetate, ethylenediaminetetraacetic acid and salt, edetic acid); coating agent (carboxymethyl fiber) Sodium, cellulose acetate, cellulose acetate Vitamins, ethyl cellulose, gelatin, medicinal glaze, hydroxypropyl cellulose,

Hydroxypropyl fluorenyl cellulose, hydroxypropyl decyl cellulose, methacrylic acid copolymer, methyl cellulose, polyethylene glycol, phthalic acid acetic acid polyethylene, shellac, sucrose, titanium dioxide, Brazilian palm Wax, microcrystalline wax, zein); colorant (sauce, red, yellow, black or blend, ferric oxide); wrong agent (ethylenediaminetetraacetic acid and salt (EDTA), lythine Acid, gentisic acid decylamine, hydroxyquinoline sulphate; desiccant (calcium chloride, calcium sulphate, cerium oxide); emulsification and / or solubilizer (arabis gum, cholesterol, diethanolamine (adjuvant), single Glyceryl stearate, lanolin alcohol, lecithin, monosuccinic acid

Oil vinegar and diglyceride, monoethanolamine (adjuvant), oleic acid (adjuvant), oil (stabilizer), poloxamer, polyoxymethylene 5 bismuth succinate, polyoxyethylene 35 Dry sesame oil, polyoxyethylene 4 〇 hydrogenated cannabis oil, polyoxyethylene oil bond, polyoxyethylene bake 2 〇 基 基 十八 趟 趟, polyoxyethylene 40 stearin, polysorbate 20, polysorbate Vinegar 4〇, polysorbate 6〇, poly-80, propylene glycol diacetate, propylene glycol monostearic acid, sodium lauryl sulfate, sodium stearate, sorbitan monolaurate, dehydrated sorbitol Monooleic acid cool, sorbitan monopalmitic acid vinegar, sorbitan 158436.doc • 56· 201215609 monostearate, stearic acid, tri-sodium cellulose, purified Shi Xi thin soil) - seasoning :Dimensional); filter aid (powder ^), flavoring and flavoring (Baixiangxiang, Benzolanline, Menthol's salicylic acid, sodium amylate, orange blossom

Secret 2, Bound Oil, Peppermint, Rose Oil 'Concentrated Rose Water, Swiss Vanilla, Tolu Balsam (10) ubalsamtincture), Vanilla, Vanilla Clove Sucrose, Sliding Agent and/or Anti-caking Agent (Shi Xi Acid, Astragalus, colloidal cerium oxide, talc) &quot;Damperant (glycerine, hexanediol, propylene glycol, sorbitol), plasticizer (! sesame oil, diacetylated monoglyceride (4) Diethyl vinegar, glycerin, monoethyl brewing and diethylene glycol monoacetate, polyethylene glycol, propylene glycol triacetin, triacetin citrate; polymer (for example, acetate)素 'alkyl cellulose, (tetra) cellulose, acrylic polymer and copolymer); solvent (acetone, alcohol, dilute alcohol, hydrated pentane, benzoic acid vinegar, butanol, carbon tetrachloride, chloroform, corn oil , cottonseed oil, ethyl acetate, glycerin, hexanediol, isopropanol, methanol, dioxin, methyl isobutyl ketone, mineral oil, peanut oil, polyethylene glycol, propylene carbonate, propylene glycol, sesame oil , water for injection, sterile water for injection, sterile irrigation water, pure water); adsorbent (powder) Cellulose, charcoal, purified diatomaceous earth · carbon dioxide adsorbent (yttrium hydroxide lime, soda lime); hardener (hydrogenated sesame oil, cetostearyl alcohol, cetyl alcohol, cetyl vinegar wax, hard Fat, paraffin, polyethylene excipient, stearyl alcohol, emulsifying wax, white wax, yellow wax suspension and / or tackifier (arabis gum, agar, alginic acid, aluminum monostearate, bentonite, purified bentonite, magmatic bentonite ' Carb〇mer 934P, carboxymethylcellulose calcium, sodium carboxymethylcellulose, sodium carboxymethylcellulose 12, carrageenan, microcrystalline and methylcellulose nanofibers •57· 158436.doc 201215609 Element, dextrin, gelatin, guar gum, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, magnesium aluminum silicate, decyl cellulose, pectin, polyoxidation Ethylene, polyvinyl alcohol, povidone, propylene glycol alginate, cerium oxide, colloidal cerium oxide, sodium alginate, tragacanth, tri-sandwich); sweetener (aspartame) , dextrate, dextrose, dextrose excipient, fructose Mannitol, saccharin 'calcium saccharin, sodium saccharin, sorbitol, sorbitol solution, sucrose, compressible sugar, confectioner's sugar, syrup); bond adhesive (arabis gum, alginic acid, carboxymethyl) Cellulose sodium, microcrystalline cellulose, dextrin, ethyl cellulose, gelatin, liquid glucose, guar gum, hydroxypropyl methylcellulose, sulfhydryl cellulose, polyethylene oxide, povidone, pre-coagulation Gelatinized starch, syrup); tablet and / or capsule diluent (calcium carbonate, calcium hydrogen phosphate, tricalcium phosphate, calcium sulfate, microcrystalline cellulose, powdered cellulose, dextrose, dextrin, dextrose Excipients, fructose 'kaolin, lactose, mannitol, sorbitol, starch, pregelatinized starch, sucrose, compressible sugar, powdered sugar); tablet disintegrant (alginic acid, microcrystalline cellulose, Cross-linked carboxycellulose sodium, corspovidone, p〇lacrilin potassium, sodium starch glycolate, starch, pregelatinized starch; lozenge and/or capsule lubricant (stearic acid, mountain glyceride, hard Acid town, light mineral oil, polyethylene glycol, sodium stearyl fumarate, stearic acid, purified stearic acid, talc, hydrogenated vegetable oil, zinc stearate); tonicity agent (dextrose, Glycerin, mannitol, potassium carbonate, sodium chloride); vehicle: flavored and / or sweet type (aromatic tincture, compound benzaldehyde tincture, etc. alcoholic tincture, mint water, sorbitol solution, syrup , Tulu balsam syrup); medium 158436.doc -58 - 201215609 agent: oily (almond oil, corn oil, cottonseed oil, ethyl oleate, isopropyl myristate, isopropyl palmitate, mineral oil , light mineral oil, tetradecyl alcohol, octyldodecanol, olive oil, peanut oil, peach oil, sesame oil, soybean oil, squalane); vehicle: solid carrier (sugar ball); vehicle: sterile (Bacteriostatic water for injection, antibacterial sodium chloride injection); tackifier (see yue float #/); water repellent (cyclomethanthan, dimethyl polyoxane, polydimethyl oxane And; wetting and / or solubilizing agent (chlorinated benzalkonium chloride, benzethonium, gasification)

Octadecyl group 0 bite, docusate sodium (d〇cusat; es〇dium), fluorenyl alcohol (n〇n〇xyn〇l) 9, nonoxynol ether, octyl phenol (〇 Ct〇xyn〇i) 9, poloxamer, polyoxyethylene 35 castor oil, polyoxyethylene 4 oxime, hydrogenated castor oil, polyoxyethylene 50 stearate, polyoxyethylene 10 oleyl ether, polyoxyethylene 20, hexadecyl 18-base riding, polyoxyethylene 4 〇 stearate, polysorbate 20, polysorbate 40, polysorbate 6 聚, polysorbate 8 〇, lauryl sulfate Sodium, sorbitan monolaurate, sorbitan monooleate, sorbitan monopalmitate, sorbitan monostearate, tetrabutylphenol (tyl〇xapo丨) ). This list is not intended to be exhaustive, but merely represents the types of excipients and specific excipients that can be used in the dosage forms of the present invention. The compounds of the disclosed formula can form salts which are also within the scope of the invention. Unless otherwise stated, reference to a compound having a structural formula herein is to be understood to include reference to a salt thereof. The term "salt" as used herein denotes an acidic salt formed with an organic acid and/or an organic acid, and an inorganic salt and/or an organically formed test salt. In addition, when a compound having the formula contains an illustrative moiety (such as but not limited to a valuable material) and an acidic moiety (such as but not limited to a tickic acid), a zwitterion ("internal salt") may be formed and included as herein The term "salt" is used in the term 158436.doc -59· 201215609. Pharmaceutically acceptable (i.e., non-toxic, physiologically acceptable) salts are preferred, but other salts are also useful. Salts of compounds having the formula can be reacted, for example, by reacting a compound having the formula with an amount (such as an equivalent amount) of an acid or base in a medium such as a medium in which the salt is precipitated or in an aqueous medium. Then formed by lyophilization. Exemplary acid addition salts include acetate, ascorbate, benzoate, besylate, hydrogen sulfate, borate, butyrate, citrate, camphorate, camphorsulfonate, fubutene Diacid salt, hydrochloride, hydrobromide, arsenate, lactate, maleate, methanesulfonate, naphthalenesulfonate, nitrate, oxalate, phosphate, C Acid salts, salicylates, succinates, sulfates, tartrates, thiocyanates, toluenes (toluenesulfonate/tosylate) and the like. In addition, acids which are generally considered to be suitable for the formation of pharmaceutically acceptable salts from alkaline pharmaceutical compounds are described, for example, in P. Stahl et al., Camille G. (ed.) Handbook of

Pharmaceutical Salts. Properties, Selection and Use. (2002) Zurich: Wiley-VCH; S. Berge et al., Journal of

Pharmaceutical Sciences (1977) 66(1) 1-19; P. Gould,

International J. of Pharmaceutics (1986) 33 201-217; Anderson et al, The Practice of Medicinal Chemistry (1996), Academic Press, New York; and The Orange Book (Food &amp; Drug Administration, MD, on its website) in. The disclosures are hereby incorporated by reference. Exemplary basic salts include ammonium salts, alkali metal salts (such as sodium salts, lithium salts, and potassium salts), alkaline earth metal salts (such as calcium salts and magnesium salts), and organic bases (for example, 158436.doc -60-201215609 machine) Salts formed from amines such as dicyclohexylamine and tert-butylamine, and salts formed with amino acids such as arginine, lysine and the like. The basic nitrogen-containing group &quot;T is quaternized by a reagent such as a low carbon alkyl group (e.g., methyl, ethyl, and butyl chloride, bromide, and alkalization), and a sulfuric acid For example, thiophene monomethyl, ethyl acetate and dibutyl ester), long-bonded dentate (such as sulfhydryl, lauryl and stearyl carbamide, bromide and iodide), aralkyl- For example, benzyl and phenethyl bromide) and the like. For the purposes of the present invention, all such acid salts and base salts are intended to be pharmaceutically acceptable salts within the scope of the present invention, and all acid salts and base salts are considered equivalent to the free form of the corresponding compound. Pharmaceutically acceptable esters of the compounds of the invention are also considered to be part of the invention. The pharmaceutically acceptable esters of the compounds of the present invention include the following groups: (1) Carboxylic esters obtained by esterification of a hydroxyl group, wherein the non-carbonyl moiety of the carboxylic acid moiety of the ester group is selected from a linear or branched chain. Alkyl (e.g., ethenyl, n-propyl, tert-butyl or n-butyl), alkoxyalkyl (e.g., decyloxymethyl), aralkyl (e.g., benzyl), aryloxyalkyl (e.g., phenoxyindenyl), aryl (e.g., phenyl optionally substituted with, for example, halogen, Cw alkyl or Cw alkoxy or amine); (2) sulfonate such as alkylsulfonyl or An aralkylsulfonyl group (for example, methanesulfonyl); (3) an amino acid ester (for example, L-guanidinium or L-iso-araminyl); (4) a phosphonate; and (5) Monophosphate, diphosphate or triphosphate. The phosphate ester can be further brewed, for example, via a Cl 2 G alcohol or a reactive derivative thereof or via 2,3-di(C6-24) brewing glycerol. Prodrugs and solvates of the compounds of the invention are also contemplated herein. A discussion of prodrugs is provided at T. Higuchi and V. Stella, Pro-drugs as Novel 158436.doc • 61 - 201215609

Delivery Systems (1987), A_C.S. Symposium Series, Volume 14; and Bioreversible Carriers in Drug Design, (1987) Ed B. Roche, American Pharmaceutical Association and Pergamon Press. The term "prodrug" means a compound (e.g., a pharmaceutical precursor) which can be converted in vivo to obtain a compound of the formula of the present invention or a pharmaceutically acceptable salt, hydrate or solvate of the compound (e.g., a pharmaceutical precursor). Transformation can occur by various mechanisms (e.g., by metabolic or chemical processes), such as via hydrolysis in blood. A discussion of the use of prodrugs is provided in T. Higuchi and W. Stella, "Pro-drugs as Novel Delivery Systems", Volume 14 of the ACS Symposium Series; and Bioreversible Carriers in Drug Design, Edward B · Roche, ed., American Pharmaceutical Association and Pergamon Press, 1987. For example, if a compound having the structural formula of the present invention or a pharmaceutically acceptable salt, hydrate or solvate of the compound contains a carboxylic acid functional group, the prodrug may comprise replacing the acid group with a group such as the following: An ester formed by a hydrogen atom: (CrC8)alkyl, ((:2_Cl2)alkylnonyloxymethyl, 1-(alkylhydrazino)ethyl having 4 to 9 carbon atoms, having 5 to 1-mercapto-1-(indolyloxy;)-ethyl group having 1 to carbon atom, alkoxycarbonyloxymethyl group having 3 to 6 carbon atoms, having 4 to 7 carbon atoms I(·alkoxycarbonyloxy)ethyl, methyl-丨-(alkoxycarbonyloxy)ethyl having 5 to 8 carbon atoms, N-(alkoxycarbonyl) having 3 to 9 carbon atoms Aminomethyl, i_(N•(alkoxycarbonyl)amino)ethyl having 4 to 10 carbon atoms, 3 fluorenyl, 4-crotonic acid vinegar, γ_butyrol _4_yl , bis-n, n_(Ci_c2) alkane 158436.doc -62 - 201215609 Aminoalkyl (C2_C3) alkyl (such as β-dimethylaminoethyl), amine indenyl (Ci-C2) alkyl , n, n_: (Ci_c2) alkylamine fluorenyl _ (Ci_c2) alkyl and pie a dentate (C2_C3) alkyl group, a pyrrolidinyl (c2-c3) alkyl group or a morpholine (c2-c3) alkyl group, and the like. Similarly, 'a compound having the structural formula of the present invention contains an alcohol functional group. , a prodrug can be formed by replacing a hydrogen atom of an alcohol group with a group such as: (Ci-C6) alkanoyloxyindenyl, alkenyloxy)ethyl, 1-methyl-l - aCrC6)alkylnonyloxy)ethyl, (Cl_C6)alkoxycarbonyloxymethyl, N^q-C6)alkoxycarbonylaminoindenyl, butyl fluorenyl, (CrC:6) alkane a mercapto group, an α-amino group (Ci_C4) alkyl group, an aryl group and an α-amino group, or an α-amino group α_amino group, wherein each 〇-amino group is a fluorenyl group Independently selected from naturally occurring L-amino acids, p(0) (0Hh, _p(〇KCKCi_)

Ce) a base or a glycosyl group (which is produced by the removal of a hydroxyl group from a semi-retracted form of a carbohydrate), and the like. If the compound of the formula of the present invention has an amine functional group, the prodrug can be formed by substituting a hydrogen atom in the amine group with a group such as the following: R-carbonyl, RO-carbonyl, NRR, -carbonyl (wherein R&amp;; R, each independently (Ci_Ci〇)alkyl, (G-C7)cycloalkyl, benzyl, or R-carbonyl is a natural cardinyl fluorenyl group or a natural a-amino fluorenyl group, 4 (〇) ΗΚ(0)0γι (where γ丨 is H, (Ci C6) alkyl or agglomerate), -C(〇Y2)Y3 (wherein Y^(Ci_C4)alkyl and Y%(Ci_Q)alkyl, carboxy (Cl-C6) alkyl, amine (Ci_C4) alkyl or monoterpene-((: 1_alkylaminoalkyl or diN,N_(Ci_C6)alkylaminoalkyl), -CO^Y5 (wherein or methyl and γ5 is mono-l(Ci-C6)alkylamino or diylamino), morpholinyl, piperidinyl or pyrrole 158436.doc • 63 · 201215609 pyridine-1-yl, Similar groups. One or more compounds of the invention may exist in unsolvated as well as solvated forms with pharmaceutically acceptable solvents such as water, ethanol, and the like, and it is contemplated that the invention encompasses solvated forms and Unsolvated form. "Solvate" means this Physical association of a compound of the invention with one or more solvent molecules. This physical association involves varying degrees of ionic bonding and covalent bonding, including hydrogen bonding. In some cases, the solvate should be capable of separation, for example When one or more solvent molecules are incorporated into the crystal lattice of a crystalline solid, "solvates" encompass solution phase solvates and isolatable solvates. Non-limiting examples of suitable solvates include ethanolate, hydrazine The alcoholate and the like. The "hydrate" is a solvate wherein the solvent molecule is h2o. One or more compounds of the present invention may be converted into a solvate as appropriate. The preparation of the solvate is generally known. M. Caira et al., [· Pharmaceutical Sci., 93(3), 601-611 (2004) describes the preparation of an antifungal fluconazole solvate in the context of acetic acid and from water. Similar preparations of compounds, hemisolvates, hydrates, and the like are described in EC van Tonder et al, AAPS PharmSciTech, 5(1), Section 12 (2004); and A. L_Bingham et al., Chem . Commun., 603-604 (2001 A typical non-limiting method comprises dissolving a compound of the invention in a desired amount of a desired solvent (organic solvent or water or a mixture thereof) at a temperature above ambient temperature and cooling at a rate sufficient to form a crystal. The solution is then separated by standard methods. Analytical techniques such as IR spectroscopy show the presence of solvent (or water) in the crystals of the solvate (or hydrate). 158436.doc -64-201215609 Compounds having various structural formulas of the present invention, and salts, solvates, vinegars and prodrugs thereof, may exist in tautomeric forms thereof (e.g., in the form of a chiral amine or an imine). All such tautomeric forms are covered herein as part of the present invention. . Asymmetry or palmarity is expected to have various formulas and mixtures thereof. Compounds having various structural formulas of the invention may contain centers and thus exist in different stereoisomeric forms. All stereoisomeric forms of the compounds of the formula (including racemic mixtures) form part of the present invention. In addition, the present invention encompasses all geometric isomers and positional isomers. For example, if you have each

Where a compound of the formula of the invention has a double bond or a fused ring, both the cis and trans forms as well as mixtures are encompassed within the scope of the invention. The mixture of diastereomers can be separated into their individual diastereoisomers by methods well known to those skilled in the art, such as by chromatography and/or fragmentation, based on their physicochemical difference I. Structure. The enantiomeric mixture can be converted to by reaction with a suitable optically active compound, such as a palmitic adjuvant, such as palmitic alcohol or Mosher's acid chlride. Diastereomeric compounds, (iv) each of the diastereomers and the individual diastereomers (for example, hydrolyzed (4) the desired pure enantiomer' to separate the enantiomers (tetra). Some of the structures of the present invention are atropisomers (e.g., substituted biaryls) and are considered to be part of the present invention. They can also be separated by using a palm-shaped column. Enantiomers. There are also oxime b, compounds having various structural formulas of the present invention may exist in different tautomeric forms, and all such forms are encompassed by the present invention 158436.doc • 65· 201215609 In addition, for example, all of the sun, alcohol and decene amine forms of the compounds are included in the present invention. The compounds of the invention (including salts, solvates, vinegars and prodrugs of such compounds, and salts of prodrugs) All stereoisomers of solvates and vinegar曰 (eg, geometric isomers, optical isomers, and the like), such as stereoisomers that may exist due to asymmetric carbons on various substituents, including enantiomeric forms (which may even be in the absence of The presence of asymmetric carbon, the isomeric forms, the isomers and the diastereomeric forms are encompassed within the scope of the invention, and positional isomers (such as 4 Å than bite and 3 _ ratio) The same applies to the bite group. (For example, if there are various compounds of the structural formula of the present invention and the double or minor ring' is used, the cis and trans forms and mixtures are encompassed within the scope of the present invention. 'All keto-enol and imine-prothalamine forms of such compounds are included in the invention.) Individual stereoisomers of the compounds of the invention may, for example, be substantially free of other isomers, or may be, for example, exogenous The spin form is mixed or mixed with all other or other selected stereoisomers. The palm center of the present invention may have an S or R configuration as defined by Ship C 1974. Sensitive (10). "Salt", "Solvate", "Vinegar", "Former The use of the drug and its analogs is equally applicable to the enantiomers, stereoisomers, rotamers, tautomers, positional isomers, racemates or prodrugs of the compounds of the invention. Salts, solvates, esters and prodrugs. The invention also encompasses isotopically labeled compounds of the invention which are identical to the compounds described herein, but in practice one or more atoms are usually in atomic mass or mass number in nature Atom substitutions with different atomic mass or mass numbers. Examples of isotopes that can be incorporated into the compounds of the present invention include hydrogen, 158436.doc • 66-201215609 Carbon oxynitride, fluorine and chlorine isotopes, respectively &amp; ,

Certain isotopically-labeled compounds having various structural formulas of the invention (eg, compounds labeled with 3H and 14c are in the compound and/or matrix distribution assay. Easy to prepare and detectable [gasification (also That is, H) and carbon _14 (i.e., 14 〇 isotopes are particularly preferred. In addition, substitution with heavier isotopes (such as ϋ 2H) may provide certain therapeutic advantages due to greater metabolic stability (eg, in vivo half-life) Increased or reduced dosage requirements are produced and may therefore be preferred in some instances. Isotopically labeled compounds having various structural formulas of the invention may be similar to those disclosed in the Schemes and/or Examples below. The preparation is carried out by substituting an isotopically labeled reagent for t. instead of an isotope-labeled reagent. Compounds having various structural formulas of the present invention and salts, solvates, brewing and prodrugs thereof having various structural formulas of the present invention The polymorphic form is intended to be included in the present invention. The benefits of the present invention include the oral administration of an optimal amount of the serotonin ribotransferase biosynthesis inhibitor. Benefits include intravenous administration of an optimal amount of a nicotine guanamine phosphoribosyltransferase biosynthesis inhibitor. Benefits of the invention include intraperitoneal administration of an optimal amount of nicotine indoleamine phosphoribosyltransferase biosynthesis inhibition The benefits of the present invention include intrathecal administration of an optimal amount of a nicotine guanamine phosphoribosyltransferase biosynthesis inhibitor. The benefits of the present invention include intramuscular administration of an optimal amount of nicotine guanamine phosphate I58436. Doc • 67-201215609 Ribotransferase Biosynthesis Inhibitors The benefits of the present invention include subcutaneous administration of an optimal amount of a nicotine indoleamine phosphoribosyltransferase biosynthesis inhibitor. The benefits of the present invention include intratumoral administration. A preferred amount of a nicotine guanamine phosphoribosyltransferase biosynthesis inhibitor. The benefits of the present invention include intrathecal administration of an optimal amount of a nicotine guanamine phosphoribosyltransferase biosynthesis inhibitor. The benefits of the present invention include hard Subcutaneous administration of an optimal amount of a nicotine guanamine phosphoribosyltransferase biosynthesis inhibitor. The benefits of the present invention include administration of an optimal amount of nicotine indoleamine phosphoribosyltransferase via the eyelid Inhibitors of synthetic synthesis. Based on these results, the present invention is disclosed or familiar to those having cancer (including leukemia and solid tumors), #inflammatory diseases, osteoporosis, atherosclerosis, colonic irritable syndrome, and others It is important to design novel therapeutic strategies for patients with conditions known to those skilled in the art. [Embodiment] One aspect of the present invention pertains to the compounds disclosed herein. The present invention relates to or as a test. A compound of the invention which forms an inhibitor of the nucleotanosome ribose transferase. The aspect of the invention relates to the preparation of a drug for the treatment, prevention, inhibition or elimination of tumors by using a final inhibitor of quinone ribosyltransferase formation. One aspect of the present invention is for the preparation of a medicament for the treatment of nicotine indole phosphoribosyltransferase to inhibit, prevent, inhibit or eliminate cancer. 158436.doc -68.201215609 Use. The invention relates to the use of a secret sugar __glycotransferase formation inhibitor for the preparation of a medicament for treating, preventing, inhibiting or eliminating cancer, wherein the cancer is selected from the group consisting of leukemia, sputum tumor, ovary Cancer, breast cancer, uterine cancer, colon cancer, cervical cancer, lung cancer, prostate cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer and Hodgkin's disease. The invention also describes one or more methods of synthesizing the compounds of the invention. The invention also describes one or more uses of the compounds of the invention.

The invention also describes the use of a compound of the invention with ancillary agents (such as with tnf, GCSF or other chemotherapeutic agents) - or multiple uses of beta. The invention also describes one or more uses of the pharmaceutical compositions of the invention. This aspect of the month is for the use of a final test for the formation of a drug for the treatment of an inflammatory disease. One aspect of the present invention relates to the use of a nicotine indoleamine phosphoribosyltransferase formation inhibitor for the manufacture of a medicament for the treatment of an inflammatory disease, such as a macrojejuntic syndrome or an inflammatory bowel disease. One aspect of the present invention relates to the use of a nicotine indoleamine phosphoribosyltransferase formation inhibitor for the preparation of a medicament for the treatment of bone diseases (the #胄胄松症). One aspect of the present invention relates to the use of a test for the formation of a guanidine moth ribotransferase for the preparation of a medicament for the treatment of a cardiovascular disease, such as atherosclerosis. One aspect of the present invention relates to the use of a nicotine indoleamine phosphoribosyltransferase formation inhibitor for the preparation of a medicament for the treatment of a disease caused by an elevated sputum content or a condition of 158436.doc-69.201215609. The disease or condition is one or more diseases or conditions selected from the group consisting of cancer, ovarian cancer, breast cancer, uterine cancer, colon cancer, uterine squamous cell carcinoma, lung cancer, prostate cancer, skin cancer, bladder cancer, pancreas Dirty cancer, leukemia, lymphoma, Hodgkin's disease, viral infection, human immunodeficiency virus, hepatitis virus, herpes virus, herpes simplex, inflammatory disease, colonic irritable syndrome, inflammatory bowel disease, rheumatoid arthritis , asthma, chronic obstructive pulmonary disease, osteoarthritis, osteoporosis, dermatitis, atopic dermatitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, graft versus host disease, Alzheimer's disease, cerebrovascular accident, atherosclerosis, diabetes, spheroid nephritis, generation S syndrome, non-small cell lung cancer, small cell lung cancer, multiple myeloma, leukemia, lymphoma, squamous cell carcinoma , kidney cancer, ureter and bladder cancer, head and neck cancer, brain and central nervous system (CNS) cancer. The compounds of the invention may be used in the treatment of proliferative diseases such as, but not limited to, cancer, autoimmune diseases, viral diseases, fungal diseases, neurological/neurodegenerative disorders, arthritis, inflammation, Anti-proliferative diseases (such as eye retinopathy), neuronal diseases, complication, and cardiovascular disease. More specifically, these compounds are useful in the treatment of a variety of cancers, including but not limited to the following: cancer, including bladder cancer, breast cancer, colon cancer, kidney cancer, liver cancer, lung cancer (including small cell lung cancer, non-small cell lung cancer) ), head and neck cancer, esophageal cancer, gallbladder cancer, ovarian cancer, pancreatic cancer, stomach cancer, cervical cancer, thyroid cancer, prostate cancer, and skin cancer (including squamous cell carcinoma); 158436.doc 70- 201215609 Hematopoietic Lymphoid neoplasms, including leukemia, acute lymphocytic leukemia, acute lymphoblastic leukemia, B-cell lymphoma, T-cell lymphoma, Hodgkins lymphoma, non-Hodgkins lymphoma ), hair cell lymphoma, mantle cell lymphoma, bone tumor, and Burkett's lymphoma; jk-based bone marrow tumors, including acute and chronic myeloid leukemia, myelodysplastic syndrome and anterior Cell leukemia; mesenchymal cell-derived tumors, including fibrosarcoma and rhabdomyosarcoma; tumors of the middle and peripheral nervous system, including astrocytoma Neuroblastoma, glioma, and schwannomas; and other tumors, including melanoma, seminoma, teratocarcinoma, osteosarcoma, xenoderoma pigmentosum, keratoacanthoma, thyroid Follicular carcinoma and Kaposi's sarcoma The compounds of the invention induce or inhibit apoptosis. The compounds of the invention may also be used in the chemoprevention of cancer. Chemoprevention is defined as inhibiting the development of invasive cancer, or inhibiting tumor recurrence, by blocking the onset of a mutation event or by blocking the progression of malignant cells that have been damaged. Another aspect of the invention is a method of inhibiting a NAMPT pathway in an animal' which comprises administering to the animal in need thereof a pharmaceutically acceptable amount of a compound of the invention. Another aspect of the invention is a pharmaceutical formulation comprising a compound of the invention. Another embodiment of the invention encompasses a pharmaceutical formulation of the invention wherein the pharmaceutical formulation reduces tumor burden after administration to a human. 158436.doc -71 201215609 Another embodiment of the invention is a pharmaceutical formulation further comprising one or more of an antibiotic, a chemotherapeutic or an adjuvant chemotherapeutic agent. The pharmaceutical formulation of the present invention may further comprise a therapeutically effective amount of an auxiliary chemical therapeutic agent. The adjuvant chemotherapeutic agent can be an agent that modulates blood cell growth and maturation. Non-limiting examples of adjunctive chemotherapeutic agents are filgrastim, pegfilgrastim, and erythropoietin. The invention also relates to a method of treating or preventing a condition associated with a rate of excessive cell growth in a mammal, the method comprising administering to the mammal an effective amount of a medicament (10) of the invention. Non-limiting examples of conditions include metastasis of cancer or malignancy. Another aspect of the invention is a method of inhibiting tumor cell growth and rate of division in a mammal having cancer or other disorder associated with aberrantly dividing cells. The method comprises administering to the mammal an effective amount of the present invention Invention of pharmaceutical formulations. Another embodiment of the invention is a method of treating bone pain caused by overgrowth or metastasis of a tumor to a bone network in a mammal in need thereof, comprising administering to the mammal an effective amount of a pharmaceutical formulation of the invention . Another embodiment of the invention is a method of administering a compound comprising a NAMPT inhibitor to a mammal in need thereof, comprising administering to the mammal a pharmaceutical formulation of the invention. In an embodiment, a mammal is a human embodiment. Another embodiment of the invention is a method of preparing a pharmaceutical formulation, comprising: at least one of the compounds of the present invention with at least one medically A combination of one or more pharmaceutically acceptable excipients or additives selected may be used as disclosed in 158436.doc -72-201215609. The invention also relates to methods of synthesizing the compounds of the invention. The present invention relates to a compound as described herein and a pharmaceutically acceptable salt, solvate, ester, prodrug or isomer thereof, and a compound comprising one or more of the compounds as described herein and A pharmaceutical composition of a pharmaceutically acceptable salt or isomer. The invention further relates to molecules useful for inhibiting the enzyme nicotine phthalamide phosphoribosyltransferase (NAMPT) and pharmaceutically acceptable salts, solvates, esters, prodrugs or isomers thereof. One aspect of the present invention provides a compound, composition, kit, and antidote for use in a mammalian NAMPT pathway having a guanidine compound: Ο R NH —(CH —(0)q—Ar—(CH2)m X —(CH2)t R1 2 3 4 5 6 7 •73· 1 2 wherein R is aryl, heteroaryl, C3_C8 cycloalkyl, C3_C8 cycloalkenyl, hetero ring alkyl, arylalkyl-, ( Heteroaryl)alkyl-, (C3-C8 cycloalkyl) 3 alkyl-, (C^-C: 8-cycloalkenyl)alkyl, (heterocycloalkyl)alkyl, (aryloxy) a pyridyl-, (heteroaryloxy)alkyl-, (c3-c8 cycloalkyloxy)alkyl-, (C^-C:8 cycloalkenyloxy)alkyl- or (heterocycloalkane) Alkoxy)alkyl-4<4> wherein the heteroaryl group and the heterocycloalkyl group each have a hetero atom number of 5 1, 2 or 3' and are independently selected from N, s or oxime, and further wherein the aryl 6 group Each of the heteroaryl group and the heterocycloalkyl group may be independently substituted by an aryl group or a hetero 7 aryl group or fused with an aryl group or a heteroaryl group, and further wherein the aryl group, 8 158436.doc 201215609 Any one of the group and the heterocycloalkyl group unsubstituted or, as the case may be, independently taken from one or more substituents The substituents may be the same or different and independently selected from the group consisting of hydrazine, halo, cyano, amine, aminoalkyl-, (amino) alkoxy, _c〇NH2 -C(〇)NH(alkyl), _c(〇)n(alkyl)2, -C(0)NH(aryl), •C(0)N(aryl)2, _CHzF3 z ' _〇 CHzF3 z, · alkyl, aryl, - alkynyl, - methoxyoxy, hydroxy, alkyl hydroxy, hydroxy, alkyl, or (alkyloxy) amine, -N(r3)_c (〇)_alkyl, -N(R3)-C(0)-aryl, -cycloalkyl, _heterocycloalkyl, aryl and heteroaryl' are limited to two adjacent ring When the atoms are not different, they are S or not at the same time;

Ar is an aryl group, a heteroaryl group, a heterocycloalkyl group or a cycloalkyl group, wherein the aryl group, the heterocyclic group, the heterocyclic alkyl group and the cycloalkyl group are each unsubstituted or, as the case may be Substituted independently by 1, 2, 3 or 4 substituents which may be the same or different and independently selected from the group consisting of: hydrazine, dentate, cyano, amine, aminoalkyl _, (Amino) alkoxy _, -CONH2, -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(aryl), -C(0 N(aryl) 2, -CHZF3_Z, -〇CHzF3.z, -alkyl, -alkenyl, -alkynyl, -alkoxy,hydroxyl,-alkylhydroxy,aryloxy-, (alkoxy) Acryl)-, -N(R3)-C(0)-homolyl, -N(R3)-c(0)-aryl, -cycloalkyl, heterocycloalkyl, aryl And _heteroaryl; R is cycloalkyl, -chzF3-z, aryl, heterocycloalkyl, heteroaryl, alkyl, -phosyl, -alkynyl, (aryl)alkyl-, (hetero Aryl)alkyl- or _/R1(heterocycloalkyl)alkyl, or _n\r2, (i) wherein the cycloalkyl group, the aryl 158436.doc-74·201215609 group, the heterocycloalkyl group , the heteroaryl group and the alkyl group are each unsubstituted or as the case may be Substituted by 1, 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of hydrazine, halo, cyano, amine, aminoalkyl-, (Amino) alkoxy-, -CONH2, -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(aryl), -C(0 N(aryl)2, -CHZF3.Z, -OCHzF3_z, -alkyl, alkoxy-, -alkenyl, -alkynyl, aryloxy-, (alkoxyalkyl)amino-- Cycloalkyl, -heterocycloalkyl, (heterocycloalkyl)alkyl-, -aryl, (aryl)alkyl-, -heteroaryl, (heteroaryl)alkyl-, -s(o ) 2-alkyl, -s(o)2-aryl, -S(0)2-CF3, -C(0)N(alkyl)2, -C(O)alkyl, -n(r3) -c(o)-alkyl, -n(r3)-c(o)-aryl, -s(o2)nh2, -s(o2)nh(alkyl), -s(o2)n(alkyl 2, -n(h)s(o2)(alkyl), -C(0)N(H)(alkyl) and fluorenyldioxy, (ii) further wherein the cycloalkyl, the aryl The heterocycloalkyl group and the heteroaryl group may each optionally be fused to an independently selected aryl, heteroaryl, heterocycloalkyl or cycloalkyl group; R3 is a fluorene, alkyl or arylalkyl group. -; X is S, S(O), S(0)2 0 or C(O); η is 1, 2, 3 or 4; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0, 1 or 2; and z is 0, 1 or 2; and its pharmaceutically acceptable salts, solvates, esters, prodrugs and isomers 158436.doc •75- 201215609

In the compound of formula i, 'each part is independently selected β. The following examples are applicable to Formula I. For any part not specifically defined, the previous definition shall prevail. Furthermore, the aryl, heteroaryl and heterocycloalkyl moieties in these embodiments can be independently unsubstituted or optionally substituted or fused as previously described. Any one or more of the following embodiments can be combined with one or more other Formula I embodiments. One embodiment of the present invention provides a compound of the formula wherein each moiety is independently selected, R is an aryl group, and n, m knives &quot;, 4 4 1 2 'Ar &gt; X, R and R are as definition. An embodiment of the present invention provides a compound of the formula nb, each part of which is independently selected, R is a heteroaryl group, and n, m, q, t, z, ', X, R4 and R3 are as definition. Fraction X, an embodiment of the invention provides a compound of the formula wherein each moiety is independently selected, Ar is an aryl group, and R, n, m, q, R4 and R3 are as defined.

One embodiment of the present invention provides a compound of formula 1 wherein each moiety is arbitrarily selected, Ar is a heteroaryl group, and the R, n, m knives X, R and R3 are as defined. One embodiment of z #明 is provided by the formula ... the 'neutral combination' is independently selected, and Ar, R, n, m, q, t, z, r/ and r3 are defined and 乂 is 8 〇 is the invention </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> s(o). One embodiment of the present invention provides for the selective selection of compounds of formula I, Ar, R, n, m, q, t, and X is S(02). One embodiment of the invention provides for the independent selection of compounds of formula I, Ar, R, n, m, q, t, and X is deuterium. An embodiment of the invention provides a compound of formula I. independently selected to be Ar, R, n, m, q, t, defined and X is C(O) » An embodiment of the invention provides a compound of formula I : Independently choose to be Ar, R, n, m, q, t, and X is C(O). An embodiment of the invention provides a compound of formula I, independently selected by force σ, defined by Ar, R, η, m, q, t, and R3 is H. An embodiment of the invention provides a compound of formula I, independently selected, Ar, R, η, m, q, t, and R3 is a hospital base. An embodiment of the invention provides a compound of formula I, independently selected, wherein Ar, R, n, m, q, t are defined and R3 is arylalkyl. An embodiment of the invention provides a compound of formula I, independently selected, Ar, R, η, m, q, t wherein each moiety Z, R4 &amp; R3 is as defined in each of the two, Han 4 and lanthanide Wherein each of the portions z, R4 and R3 are as defined, wherein each of the portions z, R4 and R3 is such that each of the portions z, R4 and X are such that each of the portions Z' R4 and X are as such Each moiety z, R4 and X is as defined in each of the z, R3 and X systems as defined by 158436.doc •77-201215609 and R4 is aryl. An embodiment of the invention provides a phantom compound that is independently selected, Ar, R, n, and # are sub-systems defined and R4 is a heteroaryl group. , Z, R are as in the month of this month - the embodiment is provided! The compounds are independently selected, and each of Ar, R, n, m, and 3 is defined and R4 is a heterocycloalkyl group. z, R and X are as described - the examples are independently selected for the provision of the phantom compound, Han is an aryl group, and the various parts of the % t, z, ArHx are as defined. Soil, and n, m, q, an embodiment of the present invention provides a lanthanide compound, which is independently selected as 'R is an aryl group, and the r4:, ® moiety is a wmx system, as defined. 'Base' and n, ^, t, an embodiment of the invention provides a phantom compound, which is independently selected, R is a heteroaryl group, hydrazine is a heteroaryl quinone, P is a sub-system q, t, z, Ar ' Rix As defined. Soil and n, m, an embodiment of the invention provides for the independent selection of a compound of formula j, R is heteroaryl 4 , a solid moiety, a heteroaryl group, R is an aryl group, and n, in b, Ar, R3 and X are as defined. q. An embodiment of the invention is independently selected for providing a phantom compound, R being a phenyl group, R, being a heteroaryl group: each. P divisions Z, Ar, R3 and X are as defined. Soil n, e.g., q, an embodiment of the invention provides a formula compound which is independently selected, R is a phenyl group, R4 is an aryl group, and n, m,.卩分系 158436.doc -78. 201215609 R1, R3, z and Ar are as defined. An embodiment of the present invention provides a phantom compound in which each part of the oxime is independently selected, R is a heteroaryl group, R4 is a phenyl group, and n, m, t, z, Ar, R3 and lanthanide are as definition. q - An embodiment of the invention provides a phantom compound in which the individual moieties are independently selected, R is a material and a (iv) group, Μ is a stupid group, and Im, q, t, Ar, z, R^x are Defined.

An embodiment of the present invention provides a phantom compound in which each is independently selected '... oxadiyl, phenyl, and ... q, t, Ar, z, R3 and X are as defined. An embodiment of the present invention provides a formula compound wherein each moiety is independently selected, R is a chelate disyl group, and is a stupid group, and n, m, q, t, z , Ar, R3 and lanthanide are as defined. An embodiment of the present invention provides a phantom compound wherein each moiety is independently selected, r is pyrazolyl, R4 is a stupid group, and η, 瓜', t, z, Ar, R3 and X are as defined. q - An embodiment of the invention provides a compound of formula i wherein each is independently selected, R is pyrazolyl (substituted by a pyridyl group for dibasic hydrazine and ^^^^" and as defined. An embodiment of the invention provides a compound of formula J wherein each moiety is independently selected, R is imidazolyl, R4 is stupid, and η, m, t'Ar, z, R3 and X are as defined β 4, an embodiment of the present invention provides a formula, μ and then each part is independently selected, R is three. Sit and β are more than bite, and anti-4 is not &quot;丞' and η, 158436. Doc-79-201215609 m, q, t, z, Ar, R^X are as defined. One embodiment of the invention provides a compound wherein each is independently selected, R is a bite-based, r4 knife system m, α t, Z, Ar, R 3 and X are as defined for the dance β 4 , an embodiment of the invention is provided; a compound of the formula wherein each part 8 is independently selected ' R is a tetrazolopyridyl group, r 4 Is a stupid base, and is defined by the lines m, q, t, z' Ar, ruler 3, and lanthanide. n. The embodiment of this month provides a compound of formula I, each of which Eight independently selected, R is an isoquinolyl group, R4 is a phenyl group, and n°, t series q, t, Ar, R3, Z, and X are as defined. m. Examples of this month are provided A compound of formula I wherein each moiety is arbitrarily selected, a quinolinyl group, R4 is a phenyl group, and η, such as t, Ar, z, R3 and X are as defined. One embodiment provides a compound of formula Z wherein each moiety is independently selected, the imidazopyridazinyl group, R4 is a phenyl group, and the m, q, t, z, Ar, R3&amp;x systems are Definitions η. An embodiment of the invention provides a compound wherein each moiety is independently selected 'R is a quinazolinyl group, R4 is a phenyl group, and n is 11, m, q, t, z, Ar, R3 and X are as defined. One embodiment of the invention provides a compound of formula j wherein each moiety is independently selected, R is a benzothiazolyl group, R4 is a phenyl group, and ', Π1, q, t, z, Ar, R3 and X are as defined. One embodiment of the invention provides a compound wherein each moiety is independently selected and R is thieno. a pyridine group, R 4 is phenyl, , and η, 158436.doc • 80 - 201215609 ni, q, t, z, Ar, R3 and X are as defined. Embodiments of the invention provide a compound of formula t, Wherein each moiety is independently selected, R is indenoindolyl, R4 is (iv)yl, and η, m, q, z, t, Ar, R3 and lanthanide are as defined. Π The present invention is an embodiment Compounds of formula 1 are provided wherein each of the Zou sub-lines are independently selected, R is oxadiazolyl, R4 is naphthyl, and η, m, q, t, z, Ar, R3 and lanthanide are as defined. m. Embodiments of the present invention provide an anthraquinone compound in which the various portions of the towel are independently selected, R is an anthracenyl (substituted by a beta-bite group), V is a porphyrin group, and n, m, q , ζ, 卜 Ar, R3 and X are as defined. An embodiment of the invention provides a compound of formula I wherein each moiety is independently selected, R is pyrazolyl, R4 is isoquinolinyl, and η, 爪, q, t, z, Ar, R3 and The oxime is as defined. One embodiment of the present invention provides a compound wherein each moiety is independently selected, the ft is azobisazolyl (substituted with a π-pyridyl group), and the oxime is stupid and - J.ri 'm.qtZNAr&gt;. An embodiment of the invention provides a compound of formula j wherein each moiety is independently selected, R is imidazolyl, R4 is morphothionyl, and η' melon, q, t, Z, Ar, R3 and x are as defined. One embodiment of the present invention provides a compound of the formula wherein each moiety is independently selected as 'R is a material and a ground wire, r4 is a phenyl group, and ^ is a phenyl group. And n, m, q, t, z, R3 and lanthanide are as defined. One embodiment of the invention provides a compound of formula j, wherein each part is 158436.doc • 81 · 201215609 independently selected 'R is evil A oxazolyl group, R 4 is a phenyl group, and is a styl group, and η, m, q, t, z, R 3 and X are as defined. An example is provided to provide a compound of formula I wherein each moiety is independently selected, R is oxadiazolyl (substituted with pyridyl), R4 is phenyl, octa 1' is phenyl, and 11, 111, 2, 9, 1, 113 and further as defined. An embodiment of the invention provides a compound of the formula wherein each moiety is independently selected, R is pyrazolyl, R4 is phenyl, Ar is phenyl, and η, m, q, t, z, R3 and X are as defined. One embodiment of the invention provides a formula: [compound wherein each moiety is independently selected, R is a specific ratio of salivation Substituting), hydrazine is phenyl, octa: phenyl, and 11, 111, 9, 2, 1, 113 and : are as defined. An embodiment of the invention provides a compound wherein each moiety is independently selected, R is imidazolyl, R4 is phenyl, Ar is stupid, and η, m, q, t, z, R3 and X are As defined. An embodiment of the invention provides a compound of formula j wherein each moiety is independently selected, R is a triazolopyridyl group, R4 is a phenyl group, the heart is a phenyl group, and η, m, q, t, z, R3 and X are as defined. One embodiment of the present invention provides a hydrazine compound wherein each moiety is independently selected, R is an acridinyl group, R4 is a phenyl group, Ar is a stupid group, and n, m, q, t, z, R3 and X is as defined. An embodiment of the present invention provides a compound wherein each moiety is independently selected, R is tetrasaphthyl (tetra), phenyl, Ar is a stupid group, and η, m, q, t, z, R3 and The lanthanide is as defined. Embodiments of the present invention provide a phantom compound wherein each moiety is 158436.doc-82-201215609 independently (4) select 'R is an iso-hydroxyl group' R4 is a phenyl group, and Ar is a phenyl group. And n' m, q, t, z, r3 and lanthanide are as defined. The present embodiment provides an oxime compound in which each part is independently selected 'R is a (tetra) group, a stupid base, Ar Is a phenyl group, and n, m, q, t, z, R^x are as defined. The present example is to provide a compound of the formula wherein each part is independently selected 'R is imidazopyridine a pyridyl group, r4 is a phenyl group, Ar is a phenyl group, and n, m, q, b, and 3 are as defined. The present invention is provided as an example [the compound wherein each part is independently Alternatively, R is (iv) linyl, phenyl, fluorene is phenyl, and η, m, q, t, z, r3 and lanthanide are as defined. Embodiments of the invention provide illusion And wherein each part is independently selected, R is a benzo(tetra)yl group, r4 is phenyl A is phenyl' and η, m, q, t, ζ, R3 and X are as defined. An example is the provision of a compound of the formula wherein each moiety is independently selected 'R is (d) and (d), r4 is phenyl A is phenyl, and n, m, q, t, z, r3 and X are as Definitions - Embodiments of the present invention provide a compound of the formula wherein each part is selected to be '... 嘻 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 ', 2 is hydrazine, R3 and X are as defined. Embodiments of the invention provide a compound of the formula wherein each moiety is independently selected, RHi-based R4 is phenyl, Ar is phenyl, η is l, m is l'q is 〇4 is 〇, 2 is 〇, 113 and lanthanide are as defined. 158436.doc -83 - 201215609 An embodiment of the invention provides a compound of formula i, wherein each part is independent Selectively, R is oxadiazolyl (substituted with pyridyl), ... is phenyl 'Ar is phenyl, n is 丨, m is 丨, q is 〇, t is 〇, 2 is 〇, Han 3 and An embodiment of the invention provides a compound of formula I wherein each moiety is independently selected, R is oxazolyl, R4 is phenyl, ^ is stupid, and ^'m is 1' q is 〇, 2 is 〇, and R3 and X are as defined. One embodiment of the invention provides a compound of formula I, wherein each moiety is

Independently selected, the ruler is pyrazolyl (substituted with pyridyl), the group Ar is phenyl, n is i, m is 1, q is 〇, t is 〇, and 〇 ' is as defined. One embodiment of the present invention provides a compound of the formula wherein each moiety independently selects a '4 (tetra) group, R 4 is a phenyl group, Ar is a phenyl group, and two 1 ' m is 1 'q is 〇, 2 is 〇, r3 and X are as defined.

= Ming - the examples are to provide a formula compound in which each = place to choose, R is a three-material (four) group, r4 is a phenyl group, and Fu ^ ^ ^ ^ ^ ^ is ^ is a meaning. 丨q κ and other systems The compound of Formula 1 is supplied to the compound of Formula 1, wherein each part is in the present invention, 2 is 0, and R3 and x are as defined. Base, ..., bis-M'R4 is phenyl 'Ar is benzene- , 〇't is 0, z is 0, and the heart is as defined 158436.doc • 84 - 201215609. One of the embodiments of the present invention provides a compound of formula I, and 1 is independently selected. Each part is Μ, _ is an iso (tetra) group, R is a stupid base, (iv) stupid base, η q Feng 〇, t is 〇, z is 〇, R3 &amp; x is as defined.独::: The 1st example of the month provides the compound of formula 1, in which each part is independently selected as a shovel _'R is 啥 基 ,, 尺 4 is phenyl, ^ is 卜 - 卜 -" ^ is defined as a phantom system. Independence - an example is to provide a compound of formula 1, wherein each part is

: Wide choice, disgusting is imidazopyrazinyl, R group, η is 1, m^ octagonal. 1, 〇 〇 〇 〇 2 2 2 2 〇 〇 〇 〇 〇 〇 〇 〇 〇 〇 R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R R m is 1, αΑη &amp; U ΛΓ is a base, η is 〇' 2 is 0, r3 and lanthanide are as defined. One embodiment of AI = aI provides a compound of formula 1, wherein each part is selected R is stupid and sulfhydryl, r4 base, η is 1, m^ 八r two original meanings. ', , q4〇'鸲〇, 2 is 〇, R3 and X are one of the specified ones. a compound in which each part is selected from the group consisting of a phenanthrene (tetra) group, R4 is a benzene = group, η is 1, or w is a virgin. '", 9 is 〇'丨 is 0, 2 is 〇, R3 and The X system is as defined by the other months. The pattern is that the formula is Ar=A'X=Q and /R, u t-〇, 4 is -%, and the structural formula is now IB: 158436.doc • 85- 201215609

R

N—(CH2)n—A—Q—NH Less 1, R2 wherein R and R3 are as defined in Formula I; R1 is the same as or different from R2, and is independently selected from Η, straight or branched bond Ci To a C7 alkyl, straight or branched chain (^ to alkoxy, straight or branched (^ to 经4 alkyl, aryl, heteroaryl, heterocycloalkyl and cycloalkyl) and wherein The heteroaryl group and the hetero atom of the heterocycloalkyl group are independently selected from one or more of N, 0 and S, with the proviso that two adjacent ring heteroatoms are not simultaneously S or not simultaneously, Wherein Ri and R2 may be unsubstituted or optionally substituted independently by one or more substituents which may be the same or different and independently selected from the group consisting of: oxime, functional group, cyano group, amine group , amine alkyl group, (amino) alkoxy _, -CONH2, -C(0)NH(alkyl), -C(0)N(alkyl) 2, -C(〇)NH(芳Base), -C(0)N(aryl)2, _CHzF3.z, -〇CHzF3_z, -alkyl, alkenyl, -alkynyl, hydroxyalkyl-, alkoxy, hydroxy, alkyl hydroxy , alkyl, (alkoxyalkyl)amino-, -homoamine, amino group _, -CHO, -N(R3)-C(0)-alkyl -N(R3)-C(0)-aryl, -cycloalkyl, -heterocycloalkyl, -aryl and heteroaryl; A is aryl, heteroaryl, heterocycloalkyl or a to Cs a cycloalkyl group wherein the aryl group, the 5 aryl group, the s-heterocyclic group, and the ring group are each unsubstituted or optionally substituted by 1, 2, 3 or 4 substituents, The substituents may be the same or different and independently selected from the group consisting of: 158436.doc -86 - 201215609 Anthracene, dentate, cyano, amino, aminoalkyl-, (amino)alkoxy-, - CONH2, -c(〇)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(aryl), _c(〇)N(aryl)2, _CHzF3 z, _〇CHzF3.z, _alkyl, alkenyl, -alkynyl, -alkoxy, hydroxy, -alkylhydroxy, aryloxy-, (alkoxyalkyl)amino-, _-N ( R3)_c(0)-alkyl, •n(r3)-c(o)-aryl, cycloalkyl, heterocycloalkyl, —aryl and —heteroaryl;

Q is C(O), S(O), s(0)2, -N(H)-C(0)-, -S(〇2)-NH- or -N(H)-S(02) - n is 0, 1, 2, 3 or 4; and z is 0, 1 or 2; and a pharmaceutically acceptable salt, solvate, ester, prodrug or isomer thereof. Another embodiment of Formula 1B is a compound of Formula 1C: IJ R1 R N-(CH2)n-A-Q-N[r2

Wherein R, A, Q, R3, 2 and !! are as defined in formula IB and R1 and R2 are joined together together with the N to which they are attached to form a CVC8 heterocyclic, C3_C8 heterocycle. a 1-bicyclic heterocyclic alkyl group, a fused 4-hetero(tetra)yl group, a spiroheterocyclic group or a heterospiroyl group, wherein the heterocyclic group, the heterocyclic group, the spirohetero ring is burnt and Heterospiroheteroaryl groups each optionally contain one or more heteroatoms selected from N, S and 0 in addition to (10) sub. 158436.doc-87-201215609 as shown in the formula. , the restriction is that two adjacent ring heteroatoms are not S at the same time or are not simultaneously 〇', wherein the heterocycloalkyl group and the heterocycloalkenyl group are each unsubstituted or optionally independently - or more Substituted for the substitution by the United States, the substituents may be (IV) or different and independently freed; group consisting of: hydrazine, south, cyano, amine, aminoalkyl-, (amino)alkoxy-, -CONH2 , -C(0)NH(alkyl), _c(〇)N(alkyl)2, -C(0)NH(aryl), _C(9)N(aryl)2, _CHzF3 —, -OCHzF3.z,- Alkenyl, ethynyl, hydroxyalkyl, alkoxy Base, hydroxy, -alkylhydroxy, carboxy, (alkoxyalkyl)amino, -alkylamine, aminocarbonyl-, -CHO, -N(R3)-C(〇)-alkyl, - N(R3)-C(0)-aryl, cycloalkyl, _heterocycloalkyl, aryl and heteroaryl; and pharmaceutically acceptable salts thereof. In the compounds of the formula IB and the formula 1C, the respective portions are independently selected. The following examples are for applicable formulas IB and 1C. For any part not specifically defined, the previous definition shall prevail. Furthermore, the aryl, heteroaryl, heterocycloalkyl, cycloalkyl, cycloalkenyl and heterocycloalkenyl moieties of these embodiments may be independently unsubstituted or optionally substituted or otherwise as previously described. The situation is fused. Any one or more of the following embodiments relating to Formula IB and Formula 1C can be combined with one or more of the other embodiments of Equations IB and 1C. An embodiment of the invention provides a compound of formula IB and formula 1C wherein each moiety is independently selected, R is aryl, and η, A, Q and R丨 and 158436.doc -88 - 201215609 r2 are as Defined. The present invention provides a compound of the formula IB and the formula 1C, wherein each of the oxime systems is independently selected, R is a heteroaryl group, and η, A, Q and R1 and R2 are as Defined. The present invention provides compounds of the formula IB and the formula 1C, each of which is independently selected, R is a C3-C8 cycloalkyl group, and η, A, Q and R and R2 are As defined. Another embodiment of the present invention provides a compound of formula IB and formula 1C wherein each of the oxime systems is independently selected, R is a C3-C8 cycloalkenyl group, and η, A, Q and R1 and R2 are as defined definition. Another embodiment of the present invention provides a compound of formula IB and formula 1C wherein each moiety is independently selected, R is heterocycloalkyl, and η, A, Q and R1 and R2 are as defined. This &amp;amp; additional embodiment provides compounds of formula IB and formula 1C wherein each moiety is independently selected, R is arylalkyl, and η, A, Q and R1 and R2 are as defined. Another embodiment of the invention provides a compound of formula IB and formula 1C wherein the various moieties are independently selected, the (heteroaryl)alkyl group, and n, A, Q and R1 and R2 are as defined . Another embodiment of the invention provides compounds of formula IB and formula 1C, each of which. The file is independently selected from cycloalkyl)alkyl groups, and 11, A, Q and Ri&amp;r2 are as defined. Another embodiment of the present invention provides a compound of formula IB and formula 1C wherein m is selected as a 'ring dilute base', and 158436.doc -89·201215609 n, A, Q and R1 and R2 are as definition. Another embodiment of the invention provides a compound of formula IB and formula IC, one of which. The P-knife is independently selected to be a (heterocyclic) group, and n, A, Q, and R1 and R2 are as defined. Another embodiment of the invention provides compounds of formula IB and formula 1C, each of which. The p-knife is independently selected to be an (aryloxy)alkyl group and n, A, Q and R1 and R2 are as defined. An example of this is to provide compounds of formula IB and formula 1C, each of which. P i is independently selected, (heteroaryloxy)alkyl, and η, A, Q and R1 and r2 are as defined. Another embodiment of the invention provides compounds of formula IB and formula 1C, each of which. The oxime is independently selected from the formula (C3-c8 cycloalkyloxy)alkyl, and η, A, (^ and ... and "as defined." Another embodiment of the present invention provides a formula a compound in which each moiety is independently selected from the group 'W(C3-C8 cycloalkenyloxy), and η, A, Q and R1 and R2 are as defined. Another embodiment of the invention is Provided are compounds of formula IB and formula 1C wherein each moiety is independently selected, the ruthenium (heterocycloalkyloxy)alkyl group, and η, A, Q, and Han 1 and 2 are as defined. Another embodiment provides a compound of Formula IB and Formula 1C wherein each moiety is independently selected, R, n, 卩 and 尺1 and R2 are synonymous and A is aryl. Another embodiment of the invention is defined To provide compounds of formula IB and formula 1C, the various moieties are independently selected, R, n, oxime and G are as defined and 1 158,436.doc 201215609 is a heteroaryl group. Another embodiment of the invention provides For the compound of the formula IC, each part is independently selected, and R, n, Q&amp; R1 &amp; R2 are as defined and A is heterozygous. Further, another embodiment of the present invention provides a compound of Formula 18 and Formula 1 (the compound, each of which is independently selected, R, n, (^ and 丨 丨 and 尺 2 are like a household, Zhongyi And Α is a C3-C8 cycloalkyl group.

Another embodiment of the present invention provides a compound of the formula 汨 and formula 1 (: each of which is independently selected, R, A, Q &amp; Rl &amp; R2 is, for example, and η is 0. Another embodiment of the invention provides that the compounds of the formula and the IC of the formula are independently selected, and R, A, (^ and the ruler and the ruler 2 are, for example, and η is 1. ' Another embodiment of the present invention provides a compound of the formula C and a compound of the formula 1C, each of which is independently selected, R, Α, 卩, and ... and han 2 are η and η is 2. Another embodiment of the present invention For example, the various moieties of the compound of formula 1C are independently selected, R, A, Qar1 &amp;, medium and η are 3. Further, as defined herein, another embodiment of the invention is provided. And the respective parts of the compound of the formula 1C are independently selected, R, Α, 卩, and ... and η are 4. Another aspect of the present invention is I58436.doc 201215609 c(〇). Another embodiment of the present invention is Providing formula 10 and formula 1 (: compounds, each of which is independently selected, R, A, The ruler 1 and the R2 system, the middle sense and the Q are S(O). Another embodiment of the present invention provides a compound of the formula IB and the formula 1 (the compound, each of which is independently selected, R, A, n&amp;Ri and R2 are defined by 303, and Q is S(〇2). Another embodiment of the present invention provides a compound of formula 1]6 and formula IC, each part being independently selected, R, A And n and Ri and R2 are as defined and Q is -n(h)-s(o2). Another embodiment of the present invention provides a compound of the formula IB and the formula IC in which each part is independently selected. , R, A, 11 and scales 1 and R2 are as defined and Q is -s(〇2)_n(h)-. Another embodiment of the invention provides compounds of formula 1]3 and formula IC The parts are selected independently, R, A, Ruler 1 and R2 are as defined and Q is -N(H)-C(0)-. One embodiment of the invention provides Formula IB and Formula 1 (: a compound wherein each of the # is independently selected, R is a phenyl group, and η, A, (^ and Ri and R are as defined. One embodiment of the invention provides a compound of formula IB and formula 1C, wherein Each of the 卩 系 is independently selected, R is naphthalene And η, A, 卩 and 尺! and R2 are as defined. An embodiment of the invention provides a compound of formula IB and formula 1C, wherein each oxime is independently selected, R is pyridyl' η, A, (^ and Ri 158436.d〇c 201215609 and R2 are as defined in the invention - an embodiment of the invention provides a compound of formula IB and formula ic wherein each moiety is independently selected and R is pyrrole Pyridyl, and n, a, Q and R1 and R2 are as defined β. Embodiments of the invention provide compounds of formula IB and formula 1C, each of which. The oxime is independently selected from the thienopyridyl group, and η, a, Q and R1 and R2 are as defined. An embodiment of the invention provides a compound of formula IB and formula 1C wherein each of the * moieties are independently selected, R is a t-sitting group, and η, A, 卩 and 尺1 and R2 are as defined. An embodiment of the invention provides a compound of formula IB and formula 1C wherein each moiety is independently selected, R is pyrazolopyridinyl, and η, A, Q and R1 and R2 are as defined. A suitable embodiment is to provide a compound of formula IB and formula 1C wherein each of the files is independently selected, R is an imidazopyridyl group, and η, A, Q and R1 and R are as defined. The present invention provides a compound of the formula 汨 and formula 1 (wherein each of the knives is independently selected, R is an imidazopyrazole group, and η, A, Q and R1 and V are By definition, a compound of formula IB and formula 1C is provided, wherein each moiety is independently selected, R is a tetrazolopyridyl group, and n, A, Q, and R and R2 are as defined. </ br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br><br> 93-201215609 and R2 are as defined. One embodiment of the invention provides a compound of formula IB and formula 1C wherein each moiety is independently selected, R is a benzodiazolyl group, and η, A, Q and R1 and R2 are as defined β. An embodiment of the invention provides a compound of formula IB and formula 1C, wherein each of the oxime systems is independently selected, R is a benzothiazolyl group, and η, A, Q and R1 And R2 is as defined. One embodiment of the invention provides a compound of formula IB and formula 1C wherein each moiety is independently selected, R is Andpyrimidinyl, and η, A, Q and R1 and R2 are as defined. One embodiment of the invention provides a compound of formula IB and formula 1C, wherein each P blade is independently selected, r is ( Pyridyloxy)methyl' and η, AQ and R1 and r2 are as defined. Another embodiment of the invention provides a compound of formula IB and formula 1C, wherein the individual moieties are independently selected, Pyridyl)alkyl, and η, A, Q and R1 and r2 are as defined. Another embodiment of the invention provides a compound of formula IB and formula 1C wherein the various moieties are independently selected, &amp; Ethyl, and η, A, Q and R and R2 are as defined. Another embodiment of the invention provides a compound of formula IB and formula 1C, wherein each knife system is independently selected, &amp; is (π 并 (唆) methyl, and n, A, Q and Ri&amp;r2 are as defined. Another embodiment of the invention provides a compound of formula IB and formula 1C, wherein each moiety is Independently choose, R, n, and café are as defined 158436.doc •94· 201215609 and A is phenyl. Another embodiment of the present invention provides a compound of the formula IB and the formula 1C, each of which is independently selected, and R, n, Q and R1 &amp; R2 are as defined and A is a bite group. Each part of the compound provided by Lima and formula 1C is independently entangled. Chuan from the choice, R, A, η, R2 and Q are synonymous, and R1 is Η » ', which is determined

Another aspect of the invention is independently selected as the base bite. The example provides a compound of formula IB wherein each moiety, R, A, n, R1 and Q are as defined, and another embodiment of the invention is independently selected as a quinolinyl group. Another embodiment of the invention is independently selected and -R2 is a morpholinyl group. Another embodiment of the invention is independently selected and -R2 is piperidinyl.

The invention provides a compound of the formula IB, wherein each part, R, A, η, R1 and Q are as defined, and the Han 2 example provides a compound of the formula IB, wherein each part, Han, A, n, Ri and Q is as defined, ... is: The application is to provide a compound, in which each part, ^8^丨 and as defined by ^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^ And Q is as defined in each of the sections, R1 is Η another embodiment of the invention is independently selected and -R2 is a quinolyl group. Another embodiment of the present invention is independently selected to provide a compound of the formula ,, R, A, η, R1 and Q are as defined, and -R2 158436.doc • 95- 201215609 . Another embodiment of the present invention provides a compound of the formula IB and the formula 1C, each of which is independently selected, wherein n, Ri, R2 and 9 are, for example, A and R are both aryl groups. Another embodiment of the present invention provides a compound of the formula and formula 1 (the compound of which is independently selected, and η, R1, R2, and Q are as defined in the formula: Aryl. Another embodiment of the present invention provides a compound of the formula IB and the formula 1C, each of which is independently selected, wherein n, Ri, R2 and Q are as defined, wherein R is a heteroaryl group and A is an aryl group. In another embodiment of the present invention, a compound of the formula IB and the formula 1C is provided, and each part is independently selected, and the n, R1, the ruler 2, and the Q system are as defined. An aryl)alkyl group and A is an aryl group. Another embodiment of the present invention provides a compound of the formula IB and the formula 1C, each of which is independently selected, and n, R1, r2 &amp; The squaring is (heteroaryloxy)alkyl and A is aryl. 疋, another embodiment of the present invention provides a compound of formula IB and formula 1C, each of which is independently selected. R1, r2 &amp; Q are, for example, two aryl groups and A is a heteroaryl group. Another embodiment of the present invention provides a compound of formula IB and formula 1C, each P is selected independently, n, R1, r2 are as defined, R is aryl and Q is S (〇2). A and another embodiment of the present invention provides Formula IB and Formula 1C. The compound of the dragon, each of the P-series is independently selected, η, Ri, R2 are as defined, 茕, A and 158436.doc 201215609 R are heteroaryl and Q is S (02). One embodiment provides a compound of formula 1 wherein each moiety is independently selected, η, Ri, R2 are as defined, a is aryl 'R is heteroaryl and Q is S (〇 2) Another embodiment of the present invention provides a compound of the formula 1] 8 and formula 1 (wherein each part is independently selected, η, Ri, R2 are as defined, and a is an aryl 'R is (Heteroaryl)alkyl and (^ is 8 (〇2). Another embodiment of the present invention provides a compound of Formula IB and Formula 1 (wherein each part is independently selected, n, R1, R2 is as defined, A is aryl 'R is (heteroaryloxy)alkyl and 9 is 8 (〇2). Another aspect of the invention is derived from a compound wherein q = 〇, m = 〇 and t=0, by this structure a formula or a pharmaceutically acceptable salt thereof: 0 R -(CR2R3)n-Ar-X-^ •π 1 wherein: R is 1, 2, 3 or 4 independently selected from N, s or a heteroaryl heteroaryl group, wherein the heteroaryl group may be substituted with one or more substituents selected from the group consisting of an amine group, a pendant oxy group, and a south group; and wherein the heteroaryl group is An N-oxide comprising one or more members of the N atom of the heteroaryl group;

Ar is an aryl group or a heteroaryl group containing ruthenium, 2, 3 or 4 heterologous 159436.doc •97·201215609 independently selected from n, s or oxime; X is s(o)2 or s=o R1 is -NHR4 and R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl; cycloalkyl; aryl; heterocycloalkyl; or heteroaryl; wherein: the cycloalkyl, the aryl The base or the heteroaryl group is each unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of: hydrazine, dentate group, hydroxyl group , hydroxyalkyl, cyano, -(CH2)mNRaRb, pendant oxy, alkyl, cyanoalkyl, halogen-based, methoxy, halooxy, alkoxyalkyl-, alkenyl, alkyne , alkynyloxy, -CONH2, -S-alkyl, -C(0)NH(alkyl), -C(0)N(alkyl)2, -C(0)NH(cycloalkyl ), -C(0)NH(aryl), -C(0)N(aryl)2, arylalkyl-, arylalkoxy-, aryloxy-, cycloalkyl, heterocycloalkane , aryl, (heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, -C(O)heterocycloalkyl, heteroaryl, (heteroaryl)alkyl-, - S(0)2-alkyl, -S(0)2-aryl , -S(0)2-CHZF3.Z, -C(O)alkyl, -N(R5)-C(0)-alkyl, -N(R5)-c(o)-aryl, -s (o2) nh2, -s(o2)nh(alkyl), -s(o2)n(alkyl)2, -n(h)(so2)(alkyl) and methylenedioxy, wherein The cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may each be substituted with one or more _ groups, cyano groups, alkyl groups or alkoxy groups; and 158436.doc •98· 201215609 • a heterocyclic or a heterocyclic group, the aryl group or the heteroaryl group, optionally in combination with an independently selected aryl, heteroaryl, heterocycloalkyl or decyl group to form a bicyclic or tricyclic group. a group which may be substituted by one or more halo, cyano, alkyl or alkyl fluorenyl groups; R 2 and R 3 may be independently selected from the group consisting of ruthenium and osmium; R 5 is an anthracene, an alkyl or an aryl group - ;

Ra and Rb are independently selected from the group consisting of hydrazine, alkyl, alkoxy, alkoxyalkyl and halogen alkyl; m is 0, 1, 2, 3, 4, 5 or 6; and η is 0 Or 1. An embodiment of Formula II of the present invention provides a compound, composition, kit, and antidote for a mammalian ναΜΡΤ pathway, wherein again 8(〇)2 and η=ι, the structural formula now becomes Formula IIA:

Wherein: R is a heteroaryl group containing 1, 2, 3 or 4 heteroatoms independently selected from N, s or fluorene, wherein the heteroaryl group may be substituted with one or more substituents selected from the group consisting of a group of free amine groups, pendant oxy groups, and functional groups; and wherein the heteroaryl group may comprise - or a plurality of N-oxides formed with the heteroaryl group;

Ar is an aryl group or a 5- or 6-membered heteroaryl group containing i, 2, 3 or 4 heterologous 158436.doc-99-201215609 independently selected from n, s or hydrazine; is NHR wherein R is a ring a compound, a heterocyclic alkyl group, an aryl group or a heteroaryl group; a cycloalkyl group; a aryl group; or a heteroaryl group; wherein: the cycloalkyl group, the aryl group or the heteroaryl group is unsubstituted or substituted 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of: sir, functional, hydroxy, hydroxyalkyl, cyano, _(CH2)mNRaRb, Side oxy, alkyl, cyanoalkyl, dentate, alkoxy, haloalkoxy, alkoxyalkyl-, alkenyl, alkynyl, alkynyloxy, _CONH2, -S- Base, -C(〇)NH(alkyl)'-C(0)N(alkyl)2, -C(0)NH(cycloalkyl), _c(0)NH(aryl), -C( 0) N(aryl) 2, arylalkyl, arylalkoxy-, aryloxy-, cycloalkyl, heterocycloalkyl, aryl, (heterocycloalkyl)alkyl _, ( Heterocycloalkyl)alkoxy-, -C(fluorene)heterocycloalkyl, heteroaryl, (heteroaryl)alkyl-, -S(0)2-alkyl, -s(0)2- Aryl, -S(0)2-CHZF3.Z, -C(O) , -N(R5)-C(0)-alkyl, -N(R5)-c(0)-aryl, -S(02)NH2, -S(〇2)NH(alkyl), - s(o2)n(alkyl)2, -n(h)(so2)(alkyl) and a methylenedioxy group, wherein the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group Each of which may be substituted by one or more yl, cyano, alkyl or alkoxy groups; and 158436.doc -100 to 201215609 the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group Optionally, additionally with an independently selected aryl, heteroaryl, heterocycloalkyl or cycloalkyl group to form a bicyclic or tricyclic group which may be via one or more halo, cyano, alkyl or Alkoxy substituted; R2 and R3 may be independently selected from the group consisting of ruthenium and osmium; R5 is fluorene, alkyl or arylalkyl _; R and Rb are independently selected from alkyl, alkoxy, alkane a group consisting of an oxyalkyl group and a haloalkyl group; and Φ m is 0, 1, 2, 3, 4, 5 or 6. In the compounds of formula II and formula IIA, the various moieties are independently selected. The following examples relate to applicable formulas and formulas. For any part not specifically defined, the previous definition shall prevail. Furthermore, the aryl, heteroaryl, heterocycloalkyl, cycloalkyl, cycloalkenyl and heterocycloalkenyl moieties of these embodiments may be independently unsubstituted or optionally substituted or otherwise as previously described. The situation is slight. Any one or more of the following embodiments relating to Formula II or Formula can be combined with one or more other embodiments of Formula π or Formula. An embodiment of the invention provides a compound of formula II or formula wherein each moiety is independently selected and Ar is aryl. An embodiment of the invention provides a compound of formula II or formula wherein each moiety is independently selected and Ar is phenyl. Another embodiment of the present invention provides a compound of formula II or formula wherein each moiety is independently selected and Ar has the formula: 158436.doc 201215609 本 - 丨Ό 。. Another embodiment of the present invention provides a compound of formula II or formula wherein each moiety is independently selected as J-Ai. is a 5- or 6-membered heteroaryl. Another embodiment of the present invention provides a compound of Formula II or Formula IIA wherein each moiety is independently selected as JL AI. Another embodiment of the invention provides a compound of formula II or formula IIA, wherein each. The oxime is independently selected and r is a bicyclic heteroaryl group. Another embodiment of the invention provides a compound of Formula II or Formula IIA wherein each moiety is independently selected and R is a heteroatom containing 1, 2, 3 or 4 independently selected from N, S or hydrazine. 9 to 1 () member of the bicyclic heteroaryl. Another embodiment of the present invention provides a compound of Formula II or Formula IIA wherein each moiety is independently selected and the sizing is selected from the group consisting of benzothiazole, indomethacin, and intimate. Ding, dihydrogen. Ratio 各 各 咬 咬 咬 咬 吱 吱 吱 、 、 、 、 、 、 、 、 、 、 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑, pyrrolopyridine, four sitting and ratio, tetrahydroindolizine and η than biting, tetrahydrogen. Sitting more than β and licking and licking. Bisidine and thienopyridine. Another embodiment of the present invention provides a compound of the formula 13 [or a compound of the formula] wherein each moiety is independently selected and the r is selected from pyrazolo (3) pyridine ... 1,4,6,7-tetrahydro Pyrazolo[4,3_cpbipyridine; 7,8-dihydro-5Η-pyrido[4'3-d]pyrimidine; 5,7-dihydropyrolo[3,4_b]pyridine; 7,8· Dihydro _5Η_ Π, 6] acridine; 1,4,6,7-tetrahydro-imidazo[4,5-cp than pyridine; 18a-dihydroimimad[l,2-a]acridine; thieno [3,2_c]pyridine; ΐΗ·imidazo[l,2-b]pyr 158436.doc 201215609 0 sitting; 1 Η-D is more than saliva “3 4 ui

'~b]nbiidine; furo[2,3_c]pyridine; ih_pyrazole[3,4-b]° ratio; M-. Ratio 各[3,2-£;]pyridine; thieno[2,3-13]. Bis-pyridinium; imidazo[1,2-ensulfonyl], furan oxime [2,3-c]pyridine; isoquinoline; 1H-carbazole; imidazolium, pyridinium; thieno[2,3_c Pyridine; furo[2,3-c]pyridine; ιη·pyrazole |, p-[2,3-c]pyridine; imidazo[i,2-a]pyrazine; Benzo[d]thiazole; 1H-pyrrolo[2,3-b]pyridine; [1,3]° stopper [5,4 outer 4; [1,2,3,4] four materials (1) buliuding;

Nai 唆 'order wood' 1 Η 'Mi. Sit and [4,5-c]. Than bite; and 1,6-peak bite. Another embodiment of the invention provides a compound of formula II or formula IIA wherein R is selected from the group consisting of:

Η

Another embodiment of the present invention provides a compound of the formula or formula wherein each moiety is independently selected, &amp; is an aryl group and contains ι, 2, 3 or 4 independently selected from n, $弋^ 9 to 10 members of the hetero atom of the order N 8 or 〇 双 -3 -3 ° ° ° ° ° Another embodiment of the invention provides a compound of the formula 式 or formula IIA, wherein one of the four knives is independently selected ' Is a phenyl group and R is a 9-member to bicyclic heteroaryl containing 1, 2 ^ 4 heteroatoms independently selected from N, W. 158436.doc 201215609 Another embodiment of the present invention provides Formula II or Formula a compound of IIA wherein each moiety is independently selected, Ar is a phenyl group and R is selected from the group consisting of benzothiazole, dihydroacridine, dihydropyridinopyrimidine, dihydropyrrolopyridine, furodenidine, imidazolium Pyrazine, M. 0 sit and ° azole, imidazole and pyridine, imidazole and squirting bow 丨 0 sitting, 〇 bow 丨 0, different 啥 啥, peak 唆, 〇 〇 sit and n bite, n ratio Slightly and bite four wow and D than bite, tetrahydro beta meters. Sit and &quot; than bite, tetrahydropyrene than saliva and 比 定 、 、 、 、 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比 比Wherein each part is independently selected and Ar is a 5- or 6-membered heteroaryl group and the stalk is a 9-membered bicyclic nucleus containing 1, 2, 3 or 4 heteroatoms independently selected from N, s or hydrazine. Another embodiment of the present invention provides a compound of formula A or formula IIA, wherein each moiety is independently selected, Ar is pyridine and the smear contains i, 2, 3 or 4 independently selected from N, A 9- to 10-membered bicyclic hetero group of a hetero atom of S or oxime. Another embodiment of the invention provides a compound of the formula or a formula wherein each moiety is independently selected and R is adjacent to the nitrogen atom of the ring Substituted by this embodiment of the present invention is the provision of a compound of the formula or a compound of the formula IIA wherein each moiety is independently selected, Ar is an aryl group and the ruler is substituted at a position adjacent to the nitrogen atom of the ring. An additional example of this month is to provide a compound of formula Η or formula 其中 A in which each part is independently Alternatively, Ar is a phenyl group and the dentine is substituted at a position adjacent to the nitrogen atom of the ring. 158436.doc -104- 201215609 Another embodiment of the invention provides a compound of the formula wherein each moiety is independently Alternatively, Ar is a 5- or 6-membered heteroaryl group and the dent is substituted at a position adjacent to the nitrogen atom on its ring. Another embodiment of the invention provides a compound of the formula wherein each moiety is independently Alternatively, ^ is pyridine and R is substituted at a position adjacent to the nitrogen atom on the ring. Another embodiment of the invention provides a compound of formula IIA wherein each moiety is independently selected, R1 is _NHR4 and R4 is cycloalkyl, • heterocycloalkyl, aryl or heteroaryl. Another embodiment of the present invention provides a compound of formula (1) or formula wherein each moiety is independently selected, Arg aryl, r1 is _NHR4 and R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl base. Another embodiment of the invention provides or a compound of formula 2 wherein each moiety is independently selected, Ar is phenyl, and R1 is _NHR4i R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Another embodiment of the present invention provides a compound of the formula wherein each moiety is independently selected, wherein the group is a 5- or 6-membered heteroaryl group, R1 is -NHR4 and R4 is a cycloalkyl group or a heterocycloalkyl group. , aryl or heteroaryl. Another embodiment of the invention provides a compound of formula IIA, wherein each. The oxime is independently selected, and VIII is β 唆, Ri is _NHR4 and R 4 is a cycloalkyl group, a heterocycloalkyl group, an aryl group or a heteroaryl group. Another embodiment of the present invention provides a compound of Formula 11 or Formula 11 wherein each moiety is independently selected and has a ruthenium, 2, 3 or 4 heteroatoms independently selected from N, S or oxime. 9-member to 1-membered bicyclic heteroaryl, along 158436.doc 201215609 phenyl and R1 is -NHR4 and R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Another embodiment of the present invention provides a compound of the formula π or ΠΑ, wherein each moiety is independently selected and R is a hetero atom containing ruthenium, 2, 3 or 4 independently selected from N, S or ruthenium. 9 to 1 member of the bicyclic heteroaryl group, the heart is. Bipyridine and R1 are -NHR4 and R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Another embodiment of the invention provides a compound of formula π or formula wherein each moiety is independently selected and R1 is unsubstituted or substituted C3-C1G cycloalkyl. Another embodiment of the present invention provides a compound of the formula or a formula wherein each moiety is independently selected, Ar is an aryl group, and R1 is an unsubstituted or substituted C3-C1G cycloalkyl group. Another embodiment provides a compound of Formula II or Formula IIA wherein each moiety is independently selected, Ar is phenyl, and r1 is unsubstituted or substituted C3-C1G cycloalkyl. An embodiment provides a compound of Formula II or Formula IIA wherein each moiety is independently selected, 5 or 6 membered heteroaryl, and r1 is unsubstituted or substituted c3_Cig cycloalkyl. Another embodiment provides a compound of Formula II or Formula IIA wherein the solid knife is independently selected, Ar is a pyridyl, and R is an unsubstituted or substituted C3-C1G cycloalkyl. Another embodiment provides a compound of Formula II or Formula IIA wherein the P-knife is independently selected and Ri is unsubstituted or substituted aromatic 158436.doc • 106· 201215609. Another embodiment of this month To provide a compound of formula Π or formula IIA, wherein each moiety is independent And the ruler 1 is an unsubstituted or substituted 5-membered to 5-membered monocyclic or bicyclic heterocycloalkyl group comprising 1, 2, 3 or 4 heteroatoms selected from N, S or fluorene. Another embodiment provides a compound of the formula „ or formula A wherein each moiety is independently selected, Ar is aryl and ... is unsubstituted or substituted comprising 1, 2, 3 or 4 selected from A 5- to 11-membered monocyclic or bicyclic heterocycloalkyl group of a hetero atom of N, S or oxime. Another embodiment of the present invention provides a compound of the formula „ or ΠΑ, wherein each part _ 立地 (4), Ar The phenyl group is an unsubstituted or substituted 5- to 11-membered monocyclic or bicyclic heterocycloalkyl group containing 1, 2, 3 or 4 heteroatoms selected from N, S or fluorene. Another embodiment of the present invention provides a compound of Formula II or Formula IIA wherein each moiety is independently selected '^ is a 5- or 6-membered heteroaryl group and r丨 is unsubstituted or substituted i, 2, 3 or 4 5- to 11-membered monocyclic or bicyclic heterocycloalkyl selected from heteroatoms of N, s or hydrazine. Another embodiment of the present invention provides a compound of the formula or formula wherein each moiety is selected, (4) and R, unsubstituted or substituted comprises 1, 2, 3 or 4 selected from N, S Or a hetero atom of 5 to 11 members of a single or double ring heterocyclic. Another embodiment of the present invention provides a compound of formula η or formula IIA wherein each moiety is selected to be unsubstituted or substituted with 5 members to ν heteroatoms to 丄! A monocyclic or bicyclic heterocyclic, 158436.doc-107-201215609 heterocycloalkyl group is attached from the N heteroatom to the remainder of the compound of formula or formula. Another embodiment of the present invention provides a compound of the formula: wherein each moiety is independently selected, Ar is an aryl group and the rule 1 is unsubstituted or substituted containing at least one hetero atom 5-membered to 11M monocyclic or bicyclic heterocycloalkyl, which is attached to the remainder of the compound of the formula or from the N heteroatom. Another embodiment of the present invention provides a compound of formula II or formula wherein each moiety is independently selected, Ar is phenyl and ... is an unsubstituted or substituted monocyclic ring containing at least one Cong atom or Bicyclic heterocycloalkyl, which is attached to the remainder of the compound of formula iia from the N heteroatom. Another embodiment of the invention provides a compound of formula II or formula IIA, wherein each. P / 7 is independently selected, 5 or 6 members of heterocyclic aryl and is unsubstituted or substituted with 5 members containing at least one N hetero atom to "membered monocyclic or bicyclic heterocyclic" The ring-based group is attached to the remainder of the compound of formula II or formula from the preceding heteroatom. Another embodiment of the present invention provides a compound of formula II or formula wherein each moiety is independently selected, (iv) and R, Unsubstituted or substituted 5 贞 to 叩 monocyclic or bicyclic hetero (tetra)yl groups containing at least one atom, the heterocyclic alkyl group being attached to the remainder of the compound of formula π or formula πΑ from the former hetero atom. One of the formulas is that Ar is a phenyl group and the formula is a compound of formula IIB. 158436.doc •108- 201215609

R is a bicyclic heteroaryl group containing 1, 2, 3 or 4 heteroatoms independently selected from N, 8 or fluorene, wherein the heteroaryl group may be substituted with one or more substituents, wherein: Selecting a group consisting of an amine group, a pendant oxy group, and a dentate group;

Wherein the heteroaryl group may comprise one or more N-oxides formed with members of the heteroaryl atom; R1 is -NHR4 and R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl; An alkyl group; an aryl group; or a heteroaryl group; wherein: the % alkyl group, the aryl group or the heteroaryl group is each unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents, the substituents They may be the same or different and independently selected from the group consisting of hydrazine, dentate, hydroxy, hydroxy, cyano, -(CH2)mNRaRb, pendant oxy, alkyl, cyanoalkyl, dentate, Alkoxy, haloalkoxy, alkoxyalkyl-, alkenyl, alkynyl, alkynyloxy, -CONH2, -S-alkyl, -C(0)NH(alkyl), _c( 〇)N(alkyl)2, -C(0)NH(cycloalkyl), -C(0)NH(aryl), _C(〇)N(aryl)2, arylalkyl-, aryl Alkoxyaryloxy-, cycloalkyl, heterocycloalkyl, aryl, (heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, -C(O)heterocycloalkane Base, heteroaryl, (heteroaryl) alkane 158436.doc •109· 201215609 base-'-S(0)2-alkyl, -S(0)2-aryl, -S(0)2-CHZF3 .Z, -C(O)alkyl -N(R5)-C(0)-alkyl, -N(R5)-C(0)-aryl, -s(o2)nh2, _s(o2)nh(alkyl), _s(〇2) N(alkyl) 2, -N(H)(S〇2)(alkyl) and a methylenedioxy group, wherein the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group are each Substituting one or more of a dentate group, a cyano group, a decyl group or an alkoxy group; and the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may be independently and independently selected a heteroaryl group, a heterocycloalkyl group or a cycloalkyl group fused to form a bicyclic or tricyclic group which may be substituted by one or more halo, cyano, alkyl or alkoxy groups; R2 and R3 may Independently selected from the group consisting of hydrazine and gas; R5 is hydrazine, alkyl or arylalkyl;

Ra and Rb are independently selected from the group consisting of hydrazine, alkyl, alkoxy, alkoxyalkyl and halogen; m is 〇, 1, 2, 3, 4, 5 or 6; z is 〇, 1 or 2. One embodiment of the invention is a hydrazine compound wherein R is selected from the group consisting of 9, 2, 3 or 4 heterocyclic heteroaryls independently selected from the heteroatoms of N, S and hydrazine. Another embodiment of the invention is a hydrazone compound wherein R is selected from the group consisting of: benzo. Plug. Sit, dihydroacridine, dihydropyrido-pyrimidine, dihydropyrrolopyridine, flurane-β ratio bite, "mi-salt and η than 嗓, p-mute and 吼α sit, taste. Sit and. Than π, glutinous rice. Sit and spray to set, 吲. Sitting, squatting, intimidating, smashing, and squinting. More than the mouth. Than bite, four saliva and beta bite, tetrahydromethane and D bite, tetrahydrogen. ratio. Sit and squat than I58436.doc -110- 201215609 bite, &quot; plug ° sit and ° than 唆 and 嗟 π π bit. Another embodiment of the invention is a compound of formula IIB, wherein r is selected from the group consisting of: 1 Η-° than 嗤[3,4 七]° ratio bite; l,4,6,7-tetrahydro _» than saliva [ 4,3-c]° ratio bite; 7,8-di-argon-5Η-β ratio bite [4,3-d] pyrimidine bite; 5,7-dihydro-τ» ratio slightly [3,4_b] Pyridine; 7,8-dihydro-5H-[1,6]acridine; 1,4,6,7-tetrahydro-imidazo[4,5-c]pyridine; l,8a-dihydroimidazo[1, 2-a]pyridine; thieno[3,2_c]pyridine; 1H-imidazo[l,2-b]pyrazole; ιη·pyrazolo[3,4_b]pyridine; furo[2,3_c]° ratio Acridine; 1H-pyrazolo[3,4_b]pyridine; 1H-pyrrolo[3,2-c]pyridine; thieno[2,3-b]pyridine; imidazo[i,2-a]pyrimidine; furan 2,3_c]pyridine; isoquinoline; 1H-carbazole; imidazo[l,2-a]pyridine; thieno[2,3-cpbipyridine; furo[2,3-c]pyridine; 1H -pyrrolo[2,3-c]bite; imidazo[l,2-aP-pyrazine; 1,3-benzothiazole; benzo[d]thiazole; 1H_〇tb ox[2,3- b]. Bisidine; [1,3]thiazolo[5,4-c]. Bisidine; [ι, 2, 3, 4] tetrazolo[l,5-a]pyridine; 1,5-acridine; 1H-oxime; 1H-imidazo[4,5-^0 ratio. And; 1,6-啥α 定. Another embodiment of the invention is a compound of formula HB wherein R is substituted at a position adjacent to the nitrogen atom on the ring. Another embodiment of the invention is a hydrazone compound wherein R is selected from the group consisting of:

158436.doc .111- 201215609

Another embodiment of the invention is a compound of formula IIB, wherein is exemplified to be a cycloalkyl, heterocycloalkyl, aryl or heteroaryl group. Another embodiment of the invention is a compound of formula IIB, wherein R4 is an unsubstituted or substituted cycloalkyl group. Another embodiment of the invention is a compound of formula IIB, wherein R4 is unsubstituted or substituted heterocycloalkyl. Another embodiment of the invention is a compound of formula IIB, wherein R4 is unsubstituted or substituted aryl. Another embodiment of the invention is a compound of formula IIB, wherein R4 is unsubstituted or substituted heteroaryl. Another embodiment of the invention is a hydrazone compound wherein Ri is unsubstituted or substituted C3-C1Q cycloalkyl. Another embodiment of the invention is a compound of formula IIB, wherein R1 is unsubstituted or substituted aryl. An embodiment of the invention is a compound of formula IIB, wherein R1 is unsubstituted or substituted 5, 10 or 4 membered monocyclic or bicyclic ring containing 1, 2, 3 or 4 heteroatoms selected from N, S or hydrazine Heteroaryl. Another embodiment of the invention is a compound of formula IIB, wherein R1 or R4 is selected from the group consisting of: 6-methoxypyridine; 2-ethoxy-4-fluorophenyl; 3'4~monophenyl ; 3,4-dimethoxyphenyl; 3,4-dimethoxyphenyl; 3-a-5-IL phenyl; 3-fluoro-4-yloxyphenyl; 4_gas_2 _methylphenyl; 4_ 158436.doc • 112- 201215609 Fluorin 2 methoxyphenyl; 4-methoxy-2,5-dianonylphenyl; 4-methylphenyl, 5-nitro-2 -ethoxyphenyl; 5•fluoro-2-methoxyphenyl; __(% benzene) than hydrazine, hydrazine-fluorophenyl)-lH-0 than "sitting; 1-(c_ 2_base)-iH-. Sitting on the sale, 1,4-dimercapto-1H-mi-jun; l,5-dimercapto-iH-°m. Sit-丨 笨 并 噻 出 出 出 出 出 出 出 曱 曱 曱 曱 曱 曱 曱 ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ; ; Azole; 1-indenyl 3-(di-unanyl)-anthracene-pyrazole; 1-methyl-5-(trifluoromethyl)-1-indole-pyrazole, oxime-propyl, 1Η-pyrazole ; 2_(2,2,2_trifluoroethoxy)_4 (trifluoromethyl)phenyl; 2 f ^ ~(3-fluorophenyl)-1,3-thiazole; 2-(benzyloxy) -5-(Trifluoromethyl)phenyl ' 2 (oxy) phenyl; 2-(didecylamino)pyrimidine; 2-(dimethylaminomethyl aryl) stupyl; 2-(B Oxycarbonyl)phenyl; 2-(decylamine sulfonyl)phenyl '2-(morpholin-4-yl)pyridine; 2-(morpholin-4-yl)pyridine; 2-(morpholine) -4-ylmethyl)phenyl; 2-(&quot;birolidin-1-yl)-1,3-thiazole; 2-(trifluoromethoxy)phenyl' 2 -(trifluoromethoxy) Phenyl; 2-(trifluoromethyl)imidazo[1,2-a]. Bis; 2-(trifluoromethyl)phenyl; 2-(trifluoromethyl)pyridine; 2,3,6-trimethoxyphenyl; 2,3-difluoro-6-nonyloxybenzene 2,3-difluorophenyl; 2,3-dihydro-1,4-benzodioxan; 2,3-dihydro-1-benzofuran; 2,3-dihydro -1-benzofuranylphenyl; 2,3-dimethoxy-5-fluorenylphenyl; 2,3-dimethoxyphenyl; 2,3-dimercapto; 2,4, 5-trimethylphenyl; 2,4-bis(trifluoromethyl)phenyl; 2,4-dioxa-3-methoxyphenyl; 2,4-difluorophenyl; 2,4· Dimethoxyphenyl; 2,4-didecylphenyl; 2,5-difluorophenyl; 2,5-dimethoxyphenyl; 2,5-didecylphenyl; 2,6 -dichloro-3-indolylphenyl; 2,6-diphenyl; 2,6-dimethoxy-4-indenylphenyl; 2,6-diindenyl"bipyridine; 6-dimethylphenyl; 2·[ethyl(indenyl)amino]·1,3_thiazole; 2-ethyl 158436.doc •113· 201215609 Stuffed base · 9 π &amp;# ' 2_丁Oxy-4-fluorophenyl; 2-butoxy-5-chlorophenyl; 2-butoxy-6-oxophenyl; 2-nitrox-3-(trifluoromethyl)phenyl; 2-chloro _3 fluorophenyl; gas 4 (monofluoromethyl) phenyl; 2- gas-4-fluorophenyl; 2-chloro-4-decyloxy Phenyl 2 gas methylphenyl; 2-gas-5-(hydroxyindenyl)phenyl; 2-gas-5-(monomethoxy)phenyl; 2_gas_5·(trimethyl sulfhydryl) Phenyl; 2-a-5-fluorophenyl-chloromethoxyphenyl; 2-chloro-5-methoxyphenyl; 2-chloro-5-methyl, benzyl 2 fluorophenyl; 3_ Trifluoromethylphenyl; 2 • chloro-6 methoxybenyl, 2- phenylphenyl; 2-cyanophenyl; 2-ethoxy-4-fluorophenyl; 2-ethoxy 6-fluoro Phenyl; 2_ethoxyphenyl; 2-ethylphenyl; 2_gas_3_(prop-2-yloxy)phenyl; 2-fluoro-3-(trifluoromethoxy)phenyl; _Fluorine_3methoxyoxyl·1 soil 'gas-3·nonylphenyl; 2-fluoro-4_(1Η-pyrazol-1-yl)phenyl; 2-fluoro_4_(difluoromethyl Phenyl; 2-fluoro-4-yloxyphenyl; 2-fluoro-4-indolylphenyl 2-fluoro-5-methoxyphenyl; 2-fluoro-5-methylphenyl; 2_Fluoryl_6-methoxyphenyl '2-oxo-6-propoxyphenyl; 2-fluorophenyl; 2H-1,3-benzodioxanthene oxime' 2-曱貌醯Aminophenyl; 2-indole phenylphenyl; 2-decyloxytrifluoromethyl)phenyl; 2-methoxy-4-(1Η·.bazole-1_yl)phenyl 2-methoxy-4-(trifluoromethyl)phenyl; 2_decyloxy_5_ (prop-2-yl)phenyl '2-methoxy-5-(trifluoromethoxy)phenyl; 2-methoxy-5-methylphenyl '2-methoxy-6-( Propyl-2-yloxy)phenyl; 2-methoxyphenyl; 2-methyl-1,3. azole; 2-mercapto-2H-carbazole; 2-mercapto-4-(1Η -pyrazol-1-yl)phenyl; 2-indolyl_4_(trifluoromethyl)phenyl; 2-hydrazino-4-propoxyphenyl; 2-methylphenyl; 2-indenyl比 pyridine; 2 phenoxyphenyl; 2-phenylethane; 3-(1 Η-pyrazole-fluorenyl)phenyl; 3-(2 2 2-trifluoroethoxy)phenyl; (2_ mercaptopropoxy)phenyl; 3-(3,5-dimethyl-1Η-°bazol-1-yl)phenyl; 3- 158436.doc -114- 201215609 (4-fluorophenoxy Phenyl, 3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl; 3-(cyclopentylaminomethyl)phenyl; 3-(diethylamine曱醯5)_5_fluorophenyl; 3-(difluorodecyloxy)phenyl; 3-(dimethylaminesulfonyl)phenyl; 3•(ethanesulfonyl)phenyl; 3- (ethylamine-mercapto)phenyl; 3-(methoxymethyl)phenyl, 3-(methylamine-methyl)phenyl; 3-(morpholin-4-yl)phenyl; 3- Piperidine-1-yl)phenyl; 3-(piperidin-1-ylindenyl) 3-(piperidinyl)phenyl; 3-(propan-2-yl)phenyl; 3-(propan-2-yloxy)phenyl; 3-(propane-hydrazine-sulfonylamino)benzene 3-(pyrimidin-2-yl)phenyl; 3-(trifluorodecyloxy)phenyl; 3•(trifluoromethyl)phenyl, 3,4-dichlorophenyl; 3,4- Dimethoxyphenyl; 3,4-dimethylphenyl, 3,5-dichlorophenyl; 3,5-difluorophenyl; 3,5-dimethoxyphenyl, 3,5- Di-nonylphenyl; 3-[(2-mercaptopropyl)amine-methylmethyl]phenyl; 3-[(didecylamino)methyl]phenyl; 3-[(morpholin-4-yl) Carbonyl] stupid; 3_[(propan-2-yl)aminoindenyl]phenyl; 3·[2-(dimethylamino)ethoxy]phenyl, 3-[2-(dimethyl Amino)ethyl]phenyl; 3_[2_(molin-4-yl)ethoxy]phenyl; 3-ethylindenylphenyl; 3-butoxyphenyl; 3_gas_2_(morpholine_ 4 _ base) ° pyridine; 3-chloro-2-fluorophenyl; 3- gas-2-methoxyphenyl; 3-chloromethylphenyl; 3-chloro-4-(trifluoromethyl) benzene 3; gas_4_methoxyphenyl; % gas-4-mercaptophenyl; 3-a-4-propoxyphenyl; 3-chloro-5-(diethylamine-methyl) Phenyl; 3-a-5-(hydroxymethyl)phenyl; 3-gas-5-fluoro 3_ gas-5-methoxyphenyl; 3-chloro-5-mercaptophenyl; 3-chlorophenyl; 3-cyanophenyl; 3-ethoxy-2-fluorophenyl; -ethoxy-4-fluorophenyl; 3-ethoxyphenyl; 3-ethylphenyl; 3-fluoro-2-methoxyphenyl; 3-fluoro-2-methylphenyl; -fluoro-2-indenylphenyl; 3-fluoro-4-(1Η-pyrazol-1-yl)phenyl; 3-fluoro-4-yl (2,2,2-trifluoroethoxy)phenyl; 3_fluoro_4_(methylthio)phenyl; 3_fluoro_4·158436.doc -115- 201215609 (difluoromethoxy)phenyl; 3-fluoro-4-(trifluoromethyl)benzene 3_fluoro-4-yloxyphenyl '3-fluoro-4-methylphenyl; 3-fluoro-4-propoxyphenyl; 3-fluoro-5-(2'2'2 — Fluoroethoxy)phenyl; 3-n-5-(2-methylpropoxy)phenyl; 3-fluoro-5-(morpholin-4-yl)phenyl; 3-fluoro-5-(吼"rrolidin-1-yl)phenyl; 3-fluoro-5-(difluoro(methyl)phenyl); 3-fluoro-5-methoxyphenyl; 3-fluoro-5-methylphenyl, 3 -fluorophenyl; 3-hydroxyphenyl; 3-methanesulfonylphenyl; 3-methoxy-4-methylphenyl; 3-methoxy-5-methylphenyl; 3-methoxy Phenylphenyl; % methylphenyl; 3-phenylphenyl; 3-phenylpropane; 3-propoxyphenyl; 3-amine sulfonium Phenylphenyl; 3-tert-butylphenyl; 4-(1-cyanocyclopentyl)phenyl; 4-(1Η·isoazol-1-yl)phenyl; 4-(1H-imidazolyl) Phenyl; 4_(1Η·pyrazol-1-yl)phenyl; 4-(2-methylpropoxy)phenyl; 4-(4-ethoxyphenyl)phenyl; 4-(4- Methylpiperazin-1-yl)phenyl; 4-(difluoromethyl)-3-fluorophenyl; 4-(didecylaminomethylhydrazino)phenyl; 4-(ethoxymethyl)benzene 4-(ethylamine-mercapto)phenyl; 4-(hydroxymethyl)phenyl; 4·(morpholin-4-yl)phenyl; 4-(propan-2-yl)phenyl; 4-(propan-2-yloxy)phenyl; 4-(. Bilobidine-1-yl); 4-(pyrrolidinyl-i-yl)phenyl; 4-(trifluoromethoxy)phenyl; 4-(trifluorofyl)phenyl; 4-(trifluoro Methyl) acridine; 3,5-difluorophenyl; 4,5-difluoro-2-methoxyphenyl; 4-[(lR)-l-hydroxybutyl]phenyl; (dimethyl Amino)methylphenyl; 4-[(»pyrrolidin-1-yl)carbonyl]phenyl; 4-[2-(dimethylamino)ethyl]phenyl; 4-[2-( .Byridine-1-yl)ethoxy]phenyl; 4-ethenylphenyl; 4-butoxy-2-methylphenyl; 4-butoxy-3-phenyl; 4 -butoxy-3-fluorophenyl; 4-butoxyphenyl; 4-butylphenyl; 4-chloro-2-(trifluoromethyl)phenyl; 4-ox-2-ethoxyl Phenyl; 4-ox-2-methoxyphenyl; 4-nitro-2-mercaptophenyl; 4-ox-3-(trifluoromethyl)phenyl; 4-gas-3-fluoro 158436. Doc •116- 201215609 Phenyl; 4-chloro-3-methoxyphenyl; 4-chlorophenyl; 4-cyanophenyl; 4-cyclohexylphenyl; 4-ethoxy-2-methyl Phenyl; 4-ethoxy-3-fluorophenyl; 4-ethoxybenyl; 4-ethylphenyl, 4-fluoro-2-(propan-2-yloxy)phenyl; 4_gas- 2,5-monomethylphenyl; 4-fluoro-2-indolylphenyl; 4-fluoro-2-methylphenyl; 4-fluoro-3-(2,2,2-trifluoroethoxy)phenyl; 4-fluoro-3-(trifluoromethyl)phenyl; 4-fluoro-3-[(propan-2-yl) Aminomethyl]phenyl; 4-fluoro-3-methoxyphenyl; 4-fluoro-3-methylphenyl; 4-fluorophenyl; 4-decanesulfonylphenyl; 4-曱oxy-2-(trifluoromethyl)phenyl; 4-methoxy-2,5-dimethylphenyl; 4-decyloxy-2-methylphenyl; 4-decyloxy 3,5-dimercaptophenyl; 4-nonyloxy-3-methylphenyl; 4-nonyloxyphenyl; 4-nonylphenyl; 4-fluorenyl. Than. 4-methylthiophene; 4-phenylbutane; 4-phenylphenyl; 4-phenylphenyl; 4-propoxyphenyl; 3,5.difluorophenyl; 5-( Diethylamine-mercapto)-2_fluorophenyl; 5-(didecylamino) η ratio; 5-(.Bilo bite_1_yl) η ratio bite; 5-(difluoroantimony) Pyridyl; 5-ethenyl-2-methoxyphenyl; 5-gas-2-(2,2,2-difluoroethoxy)phenyl; 5-gas-2-(2,2 -difluoroethoxy)phenyl; 5-chloro-2-(prop-2-yn-1-yloxy)phenyl; 5-chloro-2-(prop-2-yloxy)phenyl; 5_ Chloro-2-ethoxyphenyl; 5-oxo-2-hydroxyphenyl; 5-ox-2-methoxyphenyl; 5-chloro-2-methylphenyl·, 5-gas-2- Propyloxyphenyl; 5-acridine; 5-cyano-2-methoxyphenyl; 5-fluoro-2-(hydroxymethyl)phenyl; 5-fluoro-2-methoxyphenyl , 5-fluoro-2-indolylphenyl; 5-fluoro-6-methyl" specific bite; 5-fluoro 0 ratio bite; 5H, 6H, 7H, 8H, 9H--^ [1,2-a] t, ; 5H,6H,7H,8H,9H-^oxazolo[l,2-a]azepine;5-hydroxy-(4-phenylphenyl); 5-hydroxyl-indole-yl- 1H-carbazole; 5-hydroxy_2-(trifluoromethoxy)phenyl; 5-hydroxy-3-(morpholin-4-yl)phenyl; 5-hydroxy-3-yl (piperidinyl-indole) Phenyl; 5_ Base _3·(pyrrole 158436.doc 201215609 bite 1 base) base, 5-methoxyl ratio; 5-methyl ratio bite; 5-methyl porphin; first butyl-2-oxo Base stupid; 6-(1Η-0 vs. 0 sit-1-base) 〇 ratio. 6_(3,4·monofluorophenyl)pyridine; 6 (4methylpiperazine "yl)pyridine; 6 gas dimethylamino)pyridine; 6-(morpholine-4-yl)pyridine; 6_( Trifluoromethyl)pyridine; 6-amino-(3,5-difluorophenyl); 6_gas_2_fluoro_3_nonylphenyl; 6-gas imidazopyridine; 6-azamidazo[ l,2-a]pyridine phenyl; 6-methoxynaphthalene; 6-methyl pyridine; 6-methylpyrazine; 6-methylpyridine; 8-thiatricyclo[7.4'0·0] Tridecane-1 (13), 2,4,6,9,11-hexene; 56-chloroimidazole ratio biting; cyclohexane; dimethyl_1ί3·thiazole; furan; isoquinoline; naphthalene' Naphthylphenyl; morphine; phenyl; pyridine and quinoline. Another embodiment of the invention is a hydrazine compound wherein R1 is cycloalkyl, aryl or heteroaryl, which is the cycloalkyl group, The aryl or the heteroaryl group is each unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of: a dentate group, a hydroxyl group, Hydroxyalkyl, cyano, alkyl, alkynyl, alkynyloxy, alkoxyalkyl, alkoxy, haloalkyl, haloalkoxy, _c(〇)NH(alkyl), - C(0)NH(cycloalkyl), -C(〇)N(alkyl)2, arylalkoxy, aryloxy_, cycloalkyl, heterocycloalkyl, aryl, (heterocycloalkane Alkyl-, (heterocycloalkyl) alkoxy-, (: (fluorene) heterocycloalkyl, heteroaryl, (heteroaryl)alkyl-, -s(o)2-alkyl , _s_ alkyl, _c(0) alkyl, _s(〇2)NH2, -s(〇2)nh(alkyl), _s(〇2)N(alkyl)2, _N(H)(s〇 2) (alkyl), wherein the cyclohexyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may each be substituted with one or more functional groups, a cyano group, an alkyl group or an alkoxy group; Is 〇, 丨 or 2. Another embodiment of the invention is a compound of formula IIC, wherein Ri is cycloalkane 158436.doc 118·201215609, aryl or heteroaryl, wherein the cycloalkyl, the aryl or the The heteroaryl groups are each unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of halo, haloalkyl and _alkane Another embodiment of the present invention is a compound of the formula wherein the functional group is -CHZF3.Z, -CH2CHZF3.Z, and z is 0, 1, or 2. An example is a compound of the formula „B, wherein the haloalkoxy group is -0 CHzF3-z ' and Z is oxime, 1 or 2. Another embodiment of the invention is a compound of the formula IIB, wherein the halo group is F. An example is a hydrazone compound wherein R is a 1H-pyrazolo[3,4-b]° ratio. Another embodiment of the invention is a hydrazone compound wherein R is 1,8a-dihydromethane 0 sit and [l,2-a] ° bite. Any one or more of the Formula IIB embodiments provided above may be combined with one or more of the other embodiments as provided above. In another embodiment, the invention is further illustrated by the formula shown in Table 2: Table 2 Ν-[4-(Lactinylsulfonyl)phenyl]-3-(pyridin-3-yl) Propylamine N-[4-(azetidin-1-sulfonyl)phenyl]-2-(pyridin-3-yloxy)acetamide 158436.doc -119- 201215609 Ν〇ςνχ^ρ 0 N-[4-(piperidin-1-sulfonyl)phenyl]-1Η-»bido[3,2-c]pyridin-2-decylamine N-{[4-(piperidine-1) -sulfonyl)phenyl]fluorenyl}-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0 N-{[4-(piperidin-1-sulfonyl)phenyl] Thio[],thieno[2,3-b]pyridine-2-carboxamide b N-{[4-(piperidin-1 -indenyl)phenyl]methyl}-1H-pyrrolo[2, 3-c]pyridine-2-guanamine CO^OXO N-{[4-(piperidin-1-sulfonyl)phenyl]indolyl}-1Η-吲. -5-5-Amidoxime CC^XyO N-{[4-(piperidin-1-sulfonyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]pyridine-5 - indoleamine N-{[4-(piperidin-1-ylindolyl)phenyl]indolyl}imidazo[1,2-a]pyridine-6-carboxamide cc^oao 0 eight N-{ [4-(Piperidine-1-n-decyl)phenyl]methyl}-1Η-imidazo[l,2-b]° than sal-5-cartoamine O〇^°_/ Ν-{[ 4-(π bottom bite-1-yield)phenyl]mercapto-seceno[3,2-c]pyridine-2-carboxamide k5^X^S/HN—/ CO^XuO N-{ [4-(Piperidine-1-sulfonyl)phenyl]fluorenyl}-[1,2,3,4]tetrazolo[l,5-a]«pyridin-7-decylamine CO^ OC^O N-{[4-(piperidin-1-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyridin-7-decylamine CCr^^XO 〇8 N-{ [4-(Piperidine-1-sulfonyl)phenyl]indolyl}-1,6-acridin-2-carboxamide-120-158436.doc 201215609 0 N-{[4-(piperidine- 1-sulfonyl)phenyl]fluorenyl}' than U ^s/J pyridine-3-decylamine {rO^^CuO N-{[4-(piperidin-1-sulfonyl)phenyl] Methyl}-1Η-1,3-benzobisazole-5-decylamine o/oxo octa-N-{[4-(piperidin-1-sulfonyl)phenyl]indolyl}-1,3 - stupid and thiazole-6-nonylamine N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}furo[3,2-c]pyridin-2-decylamine Ν-{1-[4-(piperidin-1-ylidene)phenyl]ethyl}-1H-pyrrolo[3,2-c]pyridin-2-decylamine OCM: 彡N-[( 4-{8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl}phenyl)indolyl]thieno[2,3-c]&quot;bipyridin-2-indole Indoleamine &lt;=^〇0^ N-[(4-{8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl}phenyl)methyl]-1Η-» Bis-[3,2-c]° ratio bit -2-amine 0 co^o^sj N-[(4-{8-oxa-3-azabicyclo[3·2·1] xin Alkan-3-yl hydrazino}phenyl)methyl]imidazo[1,2-a]° pyridine-6-nonylamine v $ N-({4-[(5-Ga-2-oxo) Phenyl)aminosulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carbamide h\N-({4-[(2-ethenylbenzene) Amine sulfonyl]phenyl} fluorenyl)-1 Η-pyrrolo[3,2-c]pyridin-2-ylamine 158436.doc -121 - 201215609 p HN O-CH. .M N-( {4-[(4-Ga-2-oxo-5-nonylphenyl)amine sulfonyl]phenyl}indenyl)-1Η-ηpyr-[3,2-c]pyridine-2 - guanamine Xu v. N-({4-[(2-propoxyphenyl)aminesulfonyl]phenyl}indenyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide H*c \ } N-({4-[(5-fluoro-2-decyloxyphenyl)amine sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indole Amine Pi.癸N-({4-[(Quinolin-8-yl)amine sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide (Qr^ p N-[(4-{[2-(piperidin-1-yl)phenyl]aminesulfonyl}phenyl)methyl]-lH-opyrho[3,2-c]&quot; -2-decylamine. 0 Ο N-[(4-{[2-(morpholin-4-yl)phenyl]amine sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2 -c]pyridine-2-carboxamide CH, —^ Hr{ jr-^^^u N-({4-[(5-methoxy-2-indolylphenyl)amine sulfonyl) }曱基)-1Η-»比比和[3,2-c]-pyridine-2-meramine 158436.doc •122· 201215609

158436.doc •123- 201215609 N-({4-[(2-methoxy-6-methylphenyl)amine sulfonyl]phenyl}methyl)-1Η-&quot;比比和[3, 2-c]»tt pyridine-2-decylamine./flank: t &gt;-&lt;〇0 N-({4-[(4-曱oxy-2-mercaptophenyl)amine sulfonyl) Phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine N-({4-[(2,3-dihydro-1,4-benzodioxanium) Cyclohexene-6-yl)amine sulfonyl]phenyl}indenyl)-1Η-»bido[3,2-c]pyridin-2-indole Ηλ«ϊ N-[(4-{ [2-(2-Hydroxyethoxy)phenyl]aminosulfonyl}phenyl)methyl]-1H-. Bis-[3,2-c]-specific bite-2-nonylamine H&gt;^〇@ N-({4-[(4-ethoxy-2-fluorophenyl)aminesulfonyl]benzene曱 曱 ) Η Η & & & & & & & & & 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 Aminosulfonyl}phenyl)methyl]-1H-&quot;bibromo[3,2-dipyridyl-2-carboxamide. Ubiquinone-({4-[(1-o-oxy-1H-isodecen-5-yl)aminesulfonyl]phenyl}indolyl)-1Η-»比咯和[3,2-c] Pyridine-2-carboxamide

158436.doc -124- 201215609 On ρ 0&quot;,. 〇cy^ NCXxr«^o^&lt;b N-[(4-Benzene phenylamino)indolyl]-lH-pyrrolo[3,2-c]pyridin-2-indoleamine-{ [1-(Benzene fluorenyl)piperidin-4-yl]fluorenyl}-1Η-pyrrolo[3,2-c]pyridin-2-carboxamide N-[(4-benzamide) Phenyl) indenyl]-1H-. Bisolo[3,2-c]pyridine-2-carboxamide FfF 0 \-[(4-{[2-(trifluoromethoxy)benzene]sulfonylamino}phenyl)methyl]- 1Η-»比比和[3,2-c]° pyridine-2-guanamine ^νϋο &gt; 1-{[4-(piperidin-1-sulfonyl)phenyl]indolyl}thiophene [2,3-c]pyridin-2-decylamine N-({4-[(2,5-dioxaoxy)phenylsulfonyl]phenyl}methyl)-1Η-pyrrolo[ 3,2-c]pyridin-2-decylamine HN O—CH, N-[(4-{[2-decyloxy-5-(trifluoromethyl)phenyl]aminesulfonyl}曱]]-1H-pyrrolo[3,2-c]pyridin-2-decylamine C,^&gt;- N-[(4-{[4-Ga-2-(trifluoromethoxy)oxy) Phenyl]amine sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 158436.doc •125- 201215609 N-({4-[(lH- Oxazol-6-yl)aminesulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine h2n 6-amino-1H-pyrrolo[3, 2-c]pyridine-2-furic acid 4-(piperidin-1-sulfonyl)-benzyl decylamine 0 nQ^nh h IA/S; nU ο/νο 1-sulfonyl)-benzyl hydrazine Amine u Λ u, H 2 1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid 4-(4-amino-cyclohexylamine sulfonyl)-benzyl decylamine O 1H-pyrrolo[3, 2-c]pyridine-2-carboxylic acid 4-(3-amino-pyrrole -1-sulfonyl)-nodal amidoxime cTN is NH 1H-pyrrolo[3,2-c]pyridine-2-decanoic acid 4-(3,8-diaza-bicyclo[3.2.1] Octane-3-sulfonyl)-nodal decylamine·α^χι^ k^NH imidazo[l,2-a]pyrimidine-6-decanoic acid 4-(piperazin-1-sulfonyl)- Benzyl decylamine θ0% k/NH sold benzo[2,3-c]0 ratio bit -2-pyruic acid 4-decalazine-1-n-decyl)-benzyl decylamine H, Oh 1H-0 ratio. Sit and [3,4-b]0 than bite-5-decanoic acid 4-(Pyphthoquinone-1-sulfonyl)-benzylamine

158436.doc -126- 201215609 Thio[2,3-c]pyridin-2-decanoic acid 4-(4-Amino-cyclohexylaminesulfonyl)-pyristylguanamine Yanfuran[2,3- c]»Bisidine-2-decanoic acid 4-(4-amino-cyclohexylamine sulfonyl)-benzyl amidoxime N / '&quot;〇1Η-° ratio. Sit and [3,4-b]° bite 5-(4-amino-cyclohexylamine sulfonyl)-benzylamine benzophenone [2,3-c]0 than bite- 2-(3-Amino-.pyrrolidin-1-sulfonyl)-benzyl decylamine co^^ap&quot;2 O7''0 imidazo[1,2-a]. Bis-pyridine-6-decanoic acid 4-(3-amino-pyrrolidin-1-sulfonyl)-benzyl decylamine furo[2,3-c]pyridin-2-indole 4-(3) -amino-pyrrolidin-1-sulfonyl)-benzyl decylamine 1H-pyrazolo[3,4-b]pyridine-5-decanoic acid 4-(3-amino-pyrrolidine-1-sulfonate Mercapto)-benzylguanamine 0 Unh Imidazo[1,2-a]pyridine-6-decanoic acid 4-(pyrazine-1 -sulfonyl)-benzylamine γ^κ^Χ. , r / '〇k/NH furan P,3-c]pyridine-2-decanoic acid 4-(piperazin-1-sulfonyl)-benzyl decylamine 158436.doc •127· 201215609 Imidazo[1 , 2-a]pyrimidine-6-carboxylic acid 4-(3-amino-pyrrolidin-1-sulfonyl)-benzylguanamine nh2. 0 imidazo[l,2-a]pyrimidine-6-carboxylic acid 4-(4-amino-cyclohexylamine sulfonyl)-benzyl decylamine 0 C〇a&quot;&quot;XXs*n&quot;〇,minH2 cT , 0 imidazo[1,2-a]pyridine-6-carboxylic acid 4-(4-amino-cyclohexylamine sulfonyl)-benzyl decylamine H 0々» 1H-pyrazolo[3,4- b] Pyridine-5-carboxylic acid 4-(4-cyano-°Chen-1-continuation)-nodal amine H ox V] k&gt;X/CN 1H-pyrazolo[3,4-b Pyridine-5-decanoic acid 4-(4-cyanomethyl-piperidine-1-sulfonyl)-benzylguanamine 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid 4- (4-Alkoxy-σ bottom bite-1-continuation base)-nodal base amine o/^xx. , h / n nh2 1 Η-pyrazolo[3,4-b]pyridine-5-decanoic acid 4-(4-amino-Nang sigma-1 - thiol) - benzylamine H o々H Mouth eight cf3 1Η-pyrazolo[3,4-b]pyridine-5-carboxylic acid 4-[4-(2,2,2-digas-ethylamino)-bottom bite-1-wall ]_基基胺胺〇N-({4-[ 1 -(3-Phenylphenyl)-1 ratio) sit-4-continuation base]phenyl}indolyl)-1Η-°biazole[3 ,4-b]»Bipyridine-5-nonylamine 158436.doc •128· 201215609 N-({4-[(4-Ga-2-ethoxyphenyl)sulfonyl]phenyl}fluorenyl) -1Η-pyrrolo[3,2-c]pyridine-2-cartoamine CH-N \A/N 0 N-{[4-(dimethyl-1,3-thiazol-5-sulfonyl) Phenyl]methyl}-1Η-oxazolo[3,4-b]acridin-5-nonylamine COCOyXr', 0 N-[(4_{[2-fluoro-4_(1H-pyrazole) -1-yl)phenyl]sulfonyl}phenyl)indenyl][piazolo[1,2-a]pyrimidine-6-nonylamine N \/〇Lc &lt; xvxr. N-({4-[(2_气_5_methylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0 ° YCH&gt; COyjO^ 0 N-({4-[(5-Ethyl-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6- Indoleamine HX) Q N-({4-[(2-oxo-4-indolyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indenyl ψτ η/ F F--FI N-[(4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene] COyjCT sulfonyl}phenyl)indenyl]°mazole And [1,2-a]pyrimidine-6-decylamine 158436.doc -129· 201215609 N-({4-[l-methyl-5-(三说曱基)-1Η-»比'• Sodium-4-phenyl]indolyl[l,2-a]pyrimidine-6-decylamine α/αχο 〇n N-{[4-(phenylsulfonyl)phenyl] Mercapto}isoquinoline-6-nonylamine F F--FN \j6 0 N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo [1,2-a]pyrimidine-6-methanamine cO^oOn, N-[(4-{[3-(piperidin-1-ylindenyl)benzene]sulfonyl}phenyl)methyl] Imidazo[l,2-a]° ratio pyridine-6-formamide ^KO / N-({4-[6-(trifluoromethyl) ° pyridine-3-sulfonyl]phenyl}曱Thio[2,3-c]pyridin-2-decylamine over N-({4-[(4-butylbenzene)) Sulfhydryl]phenyl}methyl) imidazo[l,2-a]° than bite-6-guanamine! Factory touch N-{[4-(2-mercaptoacridin-3-sulfonyl) Phenyl]fluorenyl}-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 158436.doc 130- 201215609

°HX) e·N-({4-[(4-曱-oxy-3,5-dimethylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]nbipyridine -2-carboxamide towel. 0' i N-({4-[(4-Butoxy-3-gasbenzene)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-indene amine. /? N- {[4-(2-Mercapto-2H-carbazol-6-sulfonyl)phenyl]methyl}-1Η-«Bizozolo[3,4-b]«pyridin-5 - Hyperthyroid cr. 0 醯amine ν^0Λ&quot;^^/Γτο 〇//y N-({4-[(2- 曱 醯 醯 醯 )) sulfonyl]phenyl} methyl)-1Η-pyrazolop, 4-b]pyridine-5-nonylamine 0 〇, Xl 0H N-[(4-{[3-chloro-5-(hydroxymethyl)benzene]sulfonyl} N \\A^V/0H COyjCT 0 phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-nonylamine °K〇- p N-[(4-{[3-(diethylaminoindenyl)-5- Fluorobenzene]sulfonyl}phenyl)indolyl]furan[2,3_Φ ratio bite_2·-Ό:> V meglumine 158436.doc -131 - 201215609 HC —0 w, N-({4- [(2-Chloro-6-methoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0 N-( {4-[(3- Chloro-4-propoxybenzene)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyrimidine-6-nonylamine p N-({4-[(2,3-dimethyl) Benzene)sulfonyl]phenyl}methyl)-1Η-° than 1,3-[3,2-c]° pyridine-2-guanamine CH, 0 human CH, ,v6 0 N-[(4 -{[3-(Pron-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-carboxamide N vO1. CCVvCT,. 0 N-({4-[(4-Ethylphenyl)sulfonyl]phenyl}indenyl)imidazo[l,2-a]pyrimidine-6-carboxamide\S &quot;.乂N- { [4-({3-[(2-methylpropyl))indolyl]benzene}sulfonyl)phenyl]indolyl[3,2-c]pyridine-2-carboxamide \X) ίχνσ'α 0 N-({4-[(2-chloro-6-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine-6-carboxamide

158436.doc .132- 201215609

HX) e. N-({4-[(3-fluoro-5-mercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-ylamine K〇N-({ 4-[6-(Trifluoromethylidenepyridin-2-sulfonyl)phenyl}indolyl)furo[2,3-c]. Bis-2-carbamide Μ 0 0 /=\ y/ XX ～0 0 Ν-{[4-({4-[2_(»Byrrolidin-1-yl)ethoxy]benzene}sulfonyl)phenyl]fluorenyl}-1Η-. And [3,2-c]pyridine-2-carboxamide 0 N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl]-1H-pyrrole And [3,2-c]pyridine-2-carboxamide.\々. 0 N-(H-[(4-Butoxy-2-indolylbenzene)sulfonyl]phenyl}indolyl)imidazole And [1,2-a]pyridine-6-nonylamine ND〇C COyXT 0 N-({4-[(4-fluoro-2,5-dimercaptophenyl)sulfonyl]phenyl}fluorenyl Imidazo[1,2-a]pyrimidine-6-carbamamine CCVO)^ 0 N-[(4-{[2_indolyl-4_(trifluoromethyl)benzene]sulfonyl}phenyl )methyl]imidazo[1,2-a]pyrimidine-6-nonylamine 158436.doc •133· 201215609

158436.doc -134· 201215609 H,C V. N-({4-[(2,5-Dimethylphenyl)sulfonyl]phenyl}indenyl)-1Η-pyrrolo[3,2-c Pyridine-2-carboxamide ^_HX) N-({4-[(5-fluoro-2-indolyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine -2-decylamine plant R0 N-{[4-({3-[2-(morpholin-4-yl)ethoxy]phenyl}sulfonyl)phenyl]fluorenyl}thieno[2, 3-c]pyridine-2-carboxamide HX) N-({4-[(3-Ga-5-methylphenyl)sulfonyl]phenyl} fluorenyl)furo[2,3-c] Pyridyl-2-guanamine K〇N-({4-[(4-ethoxy-3-fluorobenzene)sulfonyl]phenyl]sulfonyl]thieno[2,3-c]pyridine- 2-nonylamine HX) f N-({4-[(4-Gas phenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 158436.doc 135· 201215609 MX) f N-({4-[(4-ethylphenyl)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]pyridin-2-decylamine c. \々. «Vxr" 0 N-({4-[(4-ethoxy-2-methylbenzene) hydrazino]phenyl}indolyl)imidazo[1,2-a]pyridine-6-carboxamide α Ά 0 N-({4-[(3-Ga-5-fluorophenyl)sulfonyl]phenyl}decyl)imidazo[l,2-a]° ratio bite-6-nonylamine C〇 yJ〇&quot;,,.] 0 Ν-[(4-{[4-(1-cyanocyclopentyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine -6-carbamamine. 卩 4. i N-({4-[(3-propoxyphenyl)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]pyridine-2-methyl Indole FF F--FN Ά N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a] Pyrimidine-6-nonylamine 158436.doc 136- 201215609

, 0-0 %Γ μ. Ν-({4-[(4-Fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-decylamine\i 0 6 N-({4-[(3-fluorophenyl)sulfonyl]phenyl}methyl)-1H-0 is more than [3,4-b]° than 5--5-amidamine) i N-[(4-{8-thiatricyclo[7.4.0.02'7]tridecy-1(13),2,4,6,9,11-hexene-6-hydroxyl}benzene Thio[2,3-c]pyridin-2-carboxamide J^CO /'ί N- {[4-( 1 -mercapto-1H-carbazole-7- Phenyl]fluorenyl}furo[2,3-c]acridin-2-indole κι Ν €0 ¥, V 卜ίΤ° 0 N-{[4-(5-gas-3-methyl Pyridine-2-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carbamimidoxime) § N-{[4-(isoquinoline-4-contigmentyl) Phenyl]fluorenyl}thieno[2,3-c]pyridine-2-carboxamide 158436.doc 137- 201215609

158436.doc •138- 201215609

„ νΰ0 0 N-({4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5 -carbamamine QO N-{[4-(phenylindolyl)phenyl]fluorenyl}-1Η-indole[2,3-c]pyridine-3-carboxamide ^vfr. tC^jOr , 0 N-[(4-{[3-Fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a] Pyrimidine-6-guanamine! &lt;0 H,C 〇^/ N-({4-[(3-fluoro-2-methylphenyl)sulfonyl]phenyl}indolyl)thieno[2] ,3-c]pyridyl-2-decylamine N-({4-[(2-chloro-4-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2 -c]pyridine-2-guanamine N 'genus "TV IT. 0 N-{[4-(quino-6-yl) phenyl] methyl}-1Η-0 ratio 0 sits and [3 , 4-b]° than the bite-5-decylamine COyOT 0 N- {[4-(1-indolyl-1H-indazol-5-sulfonyl)phenyl]methyl}imidazo[l, 2-a]pyridine-6-nonylamine 158436.doc -139· 201215609 N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)furan[2 ,3-c]pyridine-2-decylamine N 0 -CHj N- {[4-(1 -propyl·1H-pyrazole-4-sulfonyl)phenyl]indolyl} -1H-&quot; Bisazo[3,4-b]acridine-5-indoleamine^HX) p N-({4-[(3,4-dioxaoxybenzene)sulfonyl]benzene Thio[2,3-c]pyridine-2-carboxamide N Ά «νοσ,,. 0 N-({4-[(3-fluoro-5-methoxybenzene)) ]]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-nonylamine^HX) t N-({4-[(4-ethylphenyl)sulfonyl] Phenyl}fluorenyl)furo[2,3-c]pyridin-2-indoleamine 2~C〇HM, C CHS N-(H-[(2,4,5-trimercaptophenyl)sulfonate (phenyl)methyl)thieno[2,3-c]pyridine-2-carboxamide „. &&lt;Χ^ΧΓ 0 —F N-({4-[2-(Trifluoromethyl) oxazolo[l,2-a].pyridin-6-sulfonyl]phenyl}methyl) -111-°bisazolo[3,4-b]pyridine-5-decylamine

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158436.doc 141 - 201215609 }^00 N-[(4-{[2-(Merlin-4-ylmethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-φ ratio Pyridyl-2-carboxamide 0 Ν-({4-[(5-fluoro-2-indolyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6- Methionamine 0 F N-[(4-{[2-(2,2,2-trifluoroethoxy)-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]- 1Η-»Birdo[3,2-c]° pyridine-2-carbamide N-({4-[(2-fluoro-3-methylphenyl)sulfonyl]phenyl} f) -1Η-pyrrolo[3,2-c]pyridine-2-carboxamide N \Χκ «νσ,,. 9 0 N-[(4-{6-Azamidazo[l,2-a]pyridin-3-sulfonyl}phenyl)methyl]°moxazolo[l,2-a]pyrimidine-6- Methionamine oo N-{2-[4-(benzothenyl)phenyl]ethyl}-1Η-indolo[3,2-c]pyridine-2-cartoamine% N-[(4 -{[3-(Trifluoromethoxy)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridin-2-ylamine 158436.doc 142- 201215609

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N. \\, ΤΙ ΤΙ η 0 ° 0 N-{[4-(2H-l,3-benzodioxol-5-sulfonyl)phenyl]fluorenyl}-1Η-°bizozolo[ 3,4-b]〇 咬-5-nonylamine CHS N-{[4-({4-[(lR)-l-hydroxybutyl]benzene}sulfonyl)phenyl]methyl}imidazole And [l,2-a]pyrimidine-6-nonylamine pf N-{[4-(5-methylthiophen-2-indenyl)phenyl]methyl}-1沁pyrrolo[3,2 -c]pyridin-2-nonylamine^KX) «/ N-({4-[(3-decyloxybenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine -2-decylamine ~jA~0 COyJT 0 N-{[4-((3-[2-(TM)-4-yl)ethoxy]phenyl}sulfonyl)phenyl]indolyl}imidazole And [1,2-a].% of pyridine-6-formamide is o N-{[4-(phenylphenyl)phenyl]indolyl}imidazo[1,2-a]pyrazine- 2-曱醯amine broad _ v〇TC〇y^&quot;° 0 N-({4-[(4-ethoxybenzene) continuation]phenyl}indolyl)imidazo[1,2-a Pyridine-6-formamide 158436.doc -147- 201215609 HX) ¢) N-{[4-(quinoline-8 anthracenyl)phenyl]fluorenyl}furo[2,3-c] Pyridine-2-decylamine 0 N 'Ά N-[(4-{ [3-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3, 4-b]pyridine-5-carbamimid „ C0 0 N-({4-[(2-fluoro-3-methylbenzene)) ]]phenyl} fluorenyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine jKO M N-({4-[(3,4-dioxabenzene)sulfonyl] Phenyl}methyl)furo[2,3-c]pyridin-2-decylamine γ N \ij ccyXP N-{[4-({4-|l-3-[(prop-2-yl)) Amidino] phenyl}sulfonyl)phenyl]fluorenyl}imidazo[l,2-a]pyrimidine-6-carboxamide C〇ynHX^'°t 0 N-[(4-{[2 ,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]»pyridin-6-decylamine

158436.doc 148· 201215609. , 0 Ν- {[4-( 1 -Mercapto-1 Η-carbazol-6- fluorenyl)phenyl]fluorenyl}thieno[2,3-c]pyroline-2·decylamine V0 /Ν-[(4-{[3_Fluoro_4_(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridin-2-indole N -({4-[(2-Fluoro-3-indolylbenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indole ο Η〆 N-[(4-{[2,4-bis(trifluoroindolyl)benzene]sulfonyl}phenyl)indolyl]-1Η-»pyrolo[3,2-c]pyridine-2- Methionine CHj CCuXr^ N-({4-[(2-indolyl-4-propoxybenzene) hydrazino]phenyl}indolyl)imidazo[1,2-a]-pyridin-6 - amidoxime s*=0 ί N-({4-[(3-phenylphenyl)sulfonyl]phenyl}indolyl)-1,3-benzothiazole-6-decylamine Φ« τ^ 158436.doc 149- 201215609

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--~~~~ amine stupid / ΚΧ) ----- Ν-[(4·{[3-fluoro-4-(2,2,2·trifluoroethyl hydrogen i _phenyl)methyl] Thiophene dry 3 Oxygen|Di-2-carboxamine Ν-{[4-(2Η-1,3-benzodioxolyl) hydrazino)]methyl} 嗔 并 [2 ,3_e]〇比 bit_2_carbamamine cOyocdy N-[(4-{[5-Gas-2-(prop-2-yn-1-yloxy)benzene]sulfonyl}phenyl)indolyl Imidazo[1,2-a]pyridine-6-carbamimidoxime) Ν-({4-[(3 phenylphenyl) fluorenyl]phenyl}methyl)furan [2,3 -c]pyridine-2-guanamine jKO, Ρ HC-0 plant __-- N-(H-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}fluorenyl) hydrazine Cyclo[2,3-c]pyridin-2-carboxamide 158436.doc • 15Bu 201215609

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158436.doc 155· 201215609 ο Ν-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl) fluorenyl] thieno[2,3-c]° pyridine- 2-carbamamine ^κο N-({4-[l -(4-fluorophenyl)-1Η--pyrazole-4-decyl]phenyl}methyl)thieno[2,3-c ]. Bipyridine-2-carbamide / N-[(4-{[4-曱oxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-lH-o [3,2-c]°pyridin-2-amine Γ Ν vOC ocvxr 0 N-({4-[(4-ethoxy-3-fluorobenzene)sulfonyl]phenyl}fluorenyl) -1Η-«Bizozolo[3,4-b]. Bisidine-5-carbamide «, °&lt; 5 N-{[4-(4-indolyl)pyridin-3-yl)phenyl]methyl}-1沁pyrrolo[3,2 -c]pyridine-2-carboximine V, JNong~0 COyJT 0 N-{[4-({3-[2-(morpholin-4-yl)ethoxy]phenyl}sulfonyl)benzene Methyl] hydrazino} imidazo[l,2-a]pyrimidine-6-carbamimid/CH, &lt;Χ\«ΧΓ. 0 N-({4-[(4-Fluoro-3 -decyloxybenzene)sulfonyl]phenyl}indenyl)imidazo[l,2-a]pyrimidin-6-decylamine

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c^' N-{[4-(phenylindole)phenyl]indolyl}-3-(°-pyridin-2-yl)-1Η-pyrazole-5-amidoxime) N-[( 4-{[3-(5-mercapto-1,2,4-oxadiazol-3-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine-2 -nonylamine KX) N-({4-[(3-fluoro-4-indolylbenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide N \XX)·&quot; cc^xr,. 0 N-{[4-(2-Mercapto-2H-indazol-5-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyrimidine-6-decylamine hCO p cT Ν -{[4-(1,3-thiazol-2-sulfonyl)phenyl]methyl} thieno[2,3-c]pyridin-2-ylamine o CO^^CXQ 〇//CV; N-(4-(2-(Trifluoromethoxy)phenylsulfonyl)benzyl)imidazo[1,2-a]pyridine-6-nonanylamine KX) p N-{ [4-( 6-mercapto"pyrazine-2-sulfonyl)phenyl]methyl}thieno[2,3-c]acridin-2-ylamine 158436.doc -157- 201215609 ◦ANN 八N-( {4-[(3-Fluoro-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-decylamine. 0 order. / N-({4-[(4,5-Difluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-. More than [3,2-φ than pyridine-2-decylamine. Π /γ, ^yVV U^xAJ °ΊΛ Ν-[(4-{[2-(methylamine sulfonyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a] Pyrimidine-6-formamide/ \h, N-[(4-{[3-fluoro-4-(fluorenylthio)benzene]sulfonyl}phenyl)indolyl]thieno[2,3- c]. Bipyridine-2-carboximine ^κο / N-( {4-[2-(3-fluorophenyl)-1,3-thiazole-4-sulfonyl]phenyl}indolyl)furan[2 , 3-c]pyridine-2-carbamide °HX). V N-[(4-{[3-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-φ-pyridyl-2-indoleamine

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/ N-({4-[5-(Trifluoromethyl)pyridin-2-sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indole 0 N- [(4- {[4-(pyrrolidin-1 ·yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]° pyridine-6-carboxamide Ν 八丫1 η fT. 0 N-({4_[(3-曱oxy-4-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-nonylamine\=/ CH3 〇^S^〇Ν·{[4-(phenylsulfonyl)phenyl]indolyl}-1-methyl-1Η-pyrrolo[3,2-c]pyridin-2-indole MX) 夂. N-({4-[(3-fluoro-4-mercaptophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indole KX) N-{[ 4-(5-chloro-3-methylpyridine-2-sulfonyl)phenyl]indolyl]furo[2,3-c]pyridin-2-indole amine jKO N-({4-[6 -(Trifluoromethyl) &quot;bipyridin-2-sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-decylamine 158436.doc -159- 201215609 π. , N-[(4-{[2-(ethoxymethyl)phenyl]sulfonyl}phenyl)indolyl]-1Η-&quot;Bildo[3,2-c]pyridine-2- Methionine m Ν-({4-[1-(3-Phenylphenyl)-1Η-.Bizozol-4- sureinyl]phenyl}methyl)imidazo[l,2-a]acridine -6-bristamine / N-({4-[(3-methoxy-4-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]&quot; Acridine-2-decylamine H,C Ν \XhS Η\ Η fr ^ w 0 N-({4-[2-(3-fluorophenyl)-1,3-thiazole-4-sulfonyl]benzene Imidazo[l,2-a]pyrimidine-6-nonylamine 〇η η (Υ1 Η ΎΧΝ〇 ΎΧΝ〇 - N-[(4-{[3-(piperidin-1-ylmethyl)benzene) Sulfhydryl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-carbamidamine N-[(4-{[3-fluoro-5-(2-methylpropane) Oxy)phenyl]sulfonyl hydrazide 'fluorenyl}phenyl)indolyl]imidazo[1,2-a]pyrimidin-6-nonylamine 0 N-({4-[5-(trifluoromethyl)) "Bistidin-3-sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 158436.doc -160- 201215609

0) vff. 0 N-({4-[(4-decyloxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide Hlw^ N- ({4-[(3-fluoro-2-methylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide, HX) 乂[ (4-{[2-(Trifluoromethyl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridyl-2-ylamine CH, \k{ i H fru ΝΝΝΝ&gt;^ 0 N-{[4-(Dimercapto-1,3-thiazol-5-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyrimidine-6-carboxamide y 0 N-({4-[(3-Gas-4-propoxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]»pyridin-6-nonylamine ^KO 1 N-({4-[(2,4-Dioxa-3-indolylbenzene)sulfonyl]phenyl}methyl)furo[2,3-c]. Bisidine-2-indoleamine 158436.doc 161 - 201215609 〇αη Ν ν \\ΛΛΡ 〈 &quot;Π η ΓΓ. 0 Ν-({4-[(2-chloro-5-fluorobenzene)sulfonyl)] benzyl} hydrazino) imidazo[l,2-a]pyrimidin-6-nonylamine ca^xx^ N- (4-(phenylsulfonyl)benzyl)benzo[d]thiazole-5-nonylamine^ΗΧ) N-{[4-(quinolin-3-sulfonyl)phenyl]fluorenyl} Furan[2,3-c].比 曱醯 曱醯 曱醯 ΗΧ) d H,C \ N-({4-[(3,4-dimercaptophenyl)sulfonyl]phenyl}indolyl)furan[2,3-c Pyridine-2-carboxamide ^κο N-({4-[(3-fluoro-4-decyloxyphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine- 2-guanamine; W 〇ν〇τ'\. 0 N-({4-[(4-Chloro-2-indolyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide Ν ΧΧ \ΧΧ ^ λ^Γ,. 0 N-({4-[(4-ethoxy-3-fluorobenzene) hydrazino]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-decylamine

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F — 〆F —F N—[(4-{[3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a] Pyrimidine-6-indoleamine-{[4-(2Η-1,3-benzodioxol-5-)-phenyl]indolyl}imidazo[l,2-a] Pyrimidine-6-formamide (3⁄4 COyjT 0 Ν-{[4-(2Η-1,3-benzodioxol-4- continued indolyl)phenyl]methyl}imidazo[l, 2-a]»bipyridin-6-decylamine; γΝΐ H 0 /vCHs \0 N-{[4-(6-methyl)pyridin-3-yl)phenyl]indolyl}-1Η -pyrazolo[3,4-b]pyridine-5-decylamine HC-0 N-({4-[(5-t-butyl-2-methoxybenzene)sulfonyl]phenyl} Mercapto)-1Η-吼嘻[3,2-φ ratio 曱醯-nonylamine/HO Ν-[(4-{[3-(ethanesulfonyl)benzene]sulfonyl}phenyl曱]]furo[2,3-c]pyridin-2-decylamine 158436.doc 163- 201215609 MX) N-({4-[(4-曱oxy-3-indolylbenzene)sulfonate) ]]phenyl}methyl)thieno[2,3-c]pyridin-2-ylamine v * hC〇\ N-({4-[5-(° ratio slightly bite-1 · base) ° ratio Bite-3-continuation base] phenyl}mercapto)furo[2,3-c]n than pyridine-2-guanamine HC-0, N-({4-[(3-gas-2) -methoxybenzene)indolyl]phenyl}indolyl)furo[2,3-c]pyridyl -2- Yue Amides r. ,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, Pyridin-6-nonylamine 0 HC-0 N-[(4-{[2-methoxy-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]thieno[2, 3-c]&quot;Bistidine_2_carbamamine N jXX CO^XP N-({4-[5-(trifluoromethyl).pyridin-2-sulfonyl]phenyl}fluorenyl) Imidazo[l,2-a]pyrimidine-6-indoleamine 158436.doc 164- 201215609

0 \ju ODyJT N-[(4-{[3-(pyrimidin-2-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-carboxamide jKO p ^jrx^ N-({4-[(6-Gas-2-fluoro-3-indolylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indole Indoleamine, MX) QF, N-({4-[(5-fluoro-2-indolyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-indole Indole i N-({4-[(3-Aminosulfonylbenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N II \X) 0 N-({4-[(5-Cyano-2-indolyl)sulfonyl]phenyl}indenyl)imidazo[l,2-a]° pyridine-6-nonylamine^ _HX) N-[(4-{ [4_fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]» Than 2-mercaptoamine c〇vjA 0 Ν-{[4-(1,3-thiazol-2-yl)phenyl]indolyl} imidazo[l,2-a]° pyridine 6-carbamide 158436.doc -165- 201215609

158436.doc •166- 201215609 COyjO^' N-{ [4-(6-Methylpyrazin-2-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-oxime Indoleamine 0 N-({4-[(2-methylphenyl)sulfonyl]phenyl}indolyl)-1H-pyrrolo[3,2-c]pyridin-2-ylamine 8y N- ({4-[(2-Ga-4-methoxyphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine c /MX) • ·◎ N-[(4-{[2-曱oxy-4·(1Η-.bazol-1-yl)benzene]sulfonyl}phenyl)indolyl]furan[2,3-c ]pyridine-2-decylamine f N-({4-[(4-ethylphenyl)sulfonyl]phenyl}indolyl)-1H-pyrrolo[3,2-c]pyridine-2- Amidoxime A CQ/K^U V'N N- {[4-( 1 -mercapto-1 Η-»引嗤-7-)-phenyl]indolyl}imidazo[1,2 -a]pyridine-6-nonylamine II 0 158436.doc 167· 201215609 °ΗΧ) b N-[(4-{[3-(cyclopentylamino)phenyl]sulfonyl}phenyl) Mercapto]furo[2,3-c]pyridine-2-carboxamide\ 5-hydroxy-N-({4-[(4-phenylphenyl)sulfonyl]phenyl}methyl)-1Η -吲哚-2-nonylamine / N-[(4-{[4-(morpholin-4-yl)benzene]sulfonyl}phenyl) fluorenyl]furo[2,3-c]pyridine -2-decylamine / ανα, N-[(4-{[4-(ethoxy oxime) Benzene] benzyl] bromo}phenyl)methyl]imidazo[1,2-a]pyrimidin-6-carboxamide 0 α . AN &amp;\k〇X N-({4-[(3-Ga-5-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-carboxamide Σσ0 N-[(4-{[4-(morpholin-4-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]. Bipyridine-6-carbamide 0 158436.doc 168- 201215609

Γ Ν \G 0 Ν-({4-[(4-ethoxy-2-mercaptophenyl)sulfonyl]phenyl}indenyl)-1Η-»biszolo[3,4-b]. Bipyridine-5-methanamine CH, Λ ίΌ^ 0 N-({4-[(4-butoxy-3-chlorophenyl)sulfonyl]phenyl}indolyl) imidazo[l,2- a]pyridine-6-formamide $ η,Λ N-({4-[(4-甲) 醯 苯 phenyl) sulfonyl]phenyl} fluorenyl)-1Η-pyrrolo[3,2- c] Pyridin-2-decylamine 0 N-[(4-{8-oxatricyclo[7.4.0.02'7] thirteen-carbon-1 (13), 2,4,6,9,11-hexyl Alkene-6-sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidin-6-nonylamine Nh^C〇Ν-{[4-(1Η-吲哚-7-continuation) Phenyl] fluorenyl} thieno[2,3-c]pyridin-2-indole Λ ko N-[(4-{[2-(ethoxy)alkyl)benzene] Furyl]furo[2,3-c]pyridin-2-ylamine 158436.doc 169- 201215609

158436.doc -170· 201215609 η \j6 0 N-[(4_{[3-(Pyridin-1-yl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3,4 -b]pyridine-5-nonylamine κο N-({4-[(3-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}indolyl)furan[2,3-c] N-pyridin-2-nonylamine °κο i N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)indenyl]thieno[2, 3-c]. Bis-pyridine-2-decylamine κ HC-0 &quot;^Sv. N-[(4-{[2-曱-oxy-5-(trifluorodecyloxy)benzene]sulfonyl}phenyl)indole -1H-pyrrolo[3,2-c]pyridine-2-carboxamide ^κο N-({4-[(4-fluoro-3-indolyl)sulfonyl]phenyl}indole Furano[2,3-c]pyridin-2-indoleamine 0)y is N-{[4-(morphothia-4-sulfonyl)phenyl]indolyl}Mine 11 sits and [ l,2-a] °^^-6-decylamine. \\j6 COy^T N-[(4-{[3-(4-Fluorophenoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyridine-6-oxime Guanamine 158436.doc -171 - 201215609 Ν \\ person / ^ &lt;χ\ατ. Ν-{[4-(quinoline-3-sulfonyl)phenyl]methyl}-1Η-0 is sitting at 0 and [3,4-b]0 is more than 5-aminoamine 0 ΗΧ) $ N-({4-[(5-chloro-2-indolylbenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indenylamine 〇(Ύ 〇ν〇 ^ N-[(4-{[4-曱-oxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-oxime Amine 0 1 &lt;Χ) λ N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine -2-Alanine ΗΧ). 0 N-[(4-{[3-(5-Mercapto-1,2,4-oxadiazol-3-yl)benzene]sulfonyl}phenyl)indolyl]furan[2,3- c]. Bisidine-2-carboxamide _^ΗΧ) &lt; M,C N-({4-[(3-ethylmercaptophenyl)sulfonyl]phenyl}fluorenyl)thieno[2,3-c Pyridine-2-decylamine/ΚΟ,Ρ 0 i N-({4-[(4-butoxy-2-methylphenyl)indolyl]phenyl}methyl)furan[2,3_C Pyridine_2_carbamamine 158436.doc •172- 201215609

158436.doc -173- 201215609

158436.doc 174- 201215609

/Ν-({4-[2-(3-Fluorophenyl)-1,3-thiazole-4-methyl]]]yl}methyl)-1Η-pyrrolo[3,2-c]pyridine- 2-Mercaptoamine 0 N-{[4-(Benzene)phenyl]methyl}-1Η-indolepyrrolo P,3-b]pyridine-5-carboxamide HX) Ν-{[ 4-(1-benzothiophene-7-sulfonyl)phenyl]fluorenyl}furo[2,3-c]pyridine-2-carboxamide N vOf 〇\〇〇&quot;. 0 N-({4-[(3-Ga-4-oxophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-decylamine λ. N -({4-[(2-decyloxybenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo-p,2-c]pyridin-2-indoleamine) „,c_/y^ N-({4-[(2·chloro-5-methylphenyl)sulfonyl]phenyl} fluorenyl)thieno[2,3-c]pyridin-2-ylamine 〇Ν^ Τγ\ fYs ^ NV〇yK\XX 0 0 N-{ [4-(6-fluorenyl)pyrazine-2-sulfonyl)phenyl]fluorenyl}-1Η-pyrazolo[3,4-b]pyridine -5-decylamine 158436.doc -175- 201215609 Μ % Ν-({4-[2-(morpholin-4-yl)&quot;bipyridin-3-yl]phenyl}methyl rice Zoxa[l,2-a]pyrimidine-6-carboxamide^κο d Ν-[(4-{[4-(1-cyanocyclopentyl)benzene]sulfonyl}phenyl)indolyl] Furano[2,3-c]&quot;bipyridyl-2-carboxamide MX) Ν··{4-[(4,5-difluoro-2-methoxybenzene)sulfonyl]phenyl }曱)))[2,3-φ-pyridin-2-ylamine CHj ΗΝ^ ν Ί CC^jO^ 0 Ν-[(4-{[4-(ethylamine fluorenyl)benzene] Sulfhydryl} phenyl)methyl]imidazo[l,2-a] «pyridyl-6- amidoxime 0 N-{[4-(isoquinolin-4-ylindolyl)phenyl] Methyl}imidazo[1,2-a]pyridine-6-nonylamine/m i N-({4-[(3) -fluorophenyl)sulfonyl]phenyl}indolyl-1H-pyrrolo[3,2-c]pyridin-2-indoleamine 158436.doc 176· 201215609

158436.doc -177- 201215609 HX) f N-({4-[4-(Trifluoromethylbutyryl-2-sulfonyl)phenyl}methyl)thieno[2,3-c]pyridine 2-carbamamine ^KO N-({4-[6-(3,4-difluorophenyl)&quot;bipyridin-2-ylindolyl]phenyl}methyl)thieno[2,3 -c].pyridin-2-nonylamine J^co C i. N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}indolyl)furan[2,3- c]»Bipyridine-2-decylamine HX) p N-({4-[(2-decyloxy-5-methylphenyl)sulfonyl]phenyl}methyl)furan [2,3 -c]pyridin-2-nonylamine\_/^ N-({4-[(2,3-didecyloxy-5-mercaptophenyl)sulfonyl]phenyl]yl)-1Η- &quot;比比和[3,2-c]. Specific bite-2-carbamide 0 \j0iF 〇V^ 0 N-[(4-{[3-fluoro-5-〇&gt;pyrrolidin-1-yl)benzene]sulfonyl}phenyl) Imidazo[1,2-a]° ratio pyridine-6-amine H3〇/〇YVCH3 ^&gt;{VH. 〆0 N-({4-[(2,6-dioxaoxy-4-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-»biszolo[3,4-b]» Bisidine-5-nonylamine 158436.doc -178- 201215609

158436.doc -179· 201215609 \众' N-[(4-{[3-(吼-rrolidin-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a] Acridine-6-formamide m N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c] Acridine-2-nonylamine N 0 N-{[4-(isoquinolin-4-sulfonyl)phenyl]methyl}imidazo[1,2-a]pyrimidine-6-nonylamine jKO u »/ \ N-(H-[(2,4,5-trimethylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]&quot; Amine „.方&lt;x\〇cr. N-({4-[(2,4-Dichloro-3-indolylbenzene)sulfonyl]phenyl}indolyl)imidazo[1,2- a]pyrimidine-6-decylamine 0 F (E)-2-cyano-3-({4-[(5-amino-2-methoxyphenyl)aminesulfonyl]phenyl}fluorenyl) )-1-(°pyridin-4-yl)胍^_KO N-[(4-{[2-fluoro-3-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl Thiophene [2,3-dibenzylidene-2-decylamine &quot;乂158436.doc -180- 201215609 CK CK Ν-({4-[(4-曱-oxy-3-mercaptobenzene) sulfonate Mercapto]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-nonylamine 0 N n . \XX/ νΝΝ/γΝχΑ/ N-({4-[6-(trifluoromethyl) &gt;Bipyridin-2-sulfonyl]phenyl}methyl 1 imidazole [1,24 Pyrimidine-6-amidoxime f. κο N-[(4-{[4-曱-oxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]pyrene [ 2,3-nabipyridin-2-ylamine, \ϋ&gt; 〇VCT., Ν-{[4-(1-mercapto-1H-carbazol-6- surey)phenyl]fluorenyl} Imidazo[l,2-a]pyrimidin-6-decylamine 0 ^κο / bucket ({4-[2-(trifluoromethyl)imidazo[1,2-a]. pyridine-6-sulfonate醯基]phenyl}methyl)&quot;cereno[2,3-c]pyridin-2-indoleamine 0^) o=is〇•ί N-[(4_{[3-(pipe bite- 1-yl)phenyl]sulfonyl}phenyl) fluorenyl]-1,3-benzothiazole-6-indoleamine 〇rt=o I N-[(4-{[3-(piperidine-1) -yl)phenyl]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidin-6-decylamine 158436.doc -181 201215609 Plant bile p °&lt; Ν-({4-[ (4-fluoro-2-methylphenyl)sulfonyl]phenyl}indenyl)-1Η-&quot;Birdo[3,2-c]°pyridin-2-carbamide plant &lt; k N -[(4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1H-&quot;比比和[3,2 -c] pyridin-2-indoleamine 0 N-{[4-(phenylindole)sulfonylphenyl]fluorenyl}-s-H/CQ 1H-pyrrolo[3,2-c]pyridine- 2-Amidoxime N-({4-[(2-Ga-5-methoxybenzene)sulfonate Mercapto]phenyl}indenyl)-1Η-ηpyrolo[3,2-c]»pyridin-2-ylamine Ν [-[(4-{[4-(1-cyanocyclopentyl) Benzene] sulfonyl} phenyl) fluorenyl]-lH-° than succinyl [3,2-decapyridin-2-indole amine JO; N-({4-[(4-ethoxy) Benzo)sulfonyl]phenyl}methyl)thieno[2,3-c]-pyridin-2-carboxamide Η^γΝ\ (Λ η j〇^ 0 N-{ [4-(2 - mercapto"pyridin-3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 158436.doc -182- 201215609

158436.doc -183- 201215609 HX) N-[(4-{[2-Mercapto-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c ]»Bistidine-2-carbamide F-F N-[(4-{[4-(trifluorodecyloxy)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3] , 4-b]. Bisidine-5-oxime amide, eve. N-({4-[(3,4-Difluorophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-ylamine^HX) η/ N-({4-[(3,5-Dimethoxyphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine. ΗΌ N-[(4-{[4-Gaxo 2_(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]. Bipyridin-2-indoleamine 0 V. rO N-{[4-(phenylsulfonyl)phenyl]indolyl}-[1,3]thiazolo[5,4-c]pyridin-2-decylamine α η ^ 0 Cf N-({ 4-[5-(indolyl-1-yl)°pyridin-3-sulfonyl]phenyl}methyl)imidazo[l,2-a]acridin-6-amine

158436.doc • 184- 201215609 ^κο HC N-[(4-{[2·曱yl-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3- c]pyridine-2-cartoamine, 4' N-[(4-{[3-(3,5-dimercapto-1H-pyrazol-1-yl)benzene]sulfonyl}phenyl)indole -1H-pyrazolo[3,4-b]pyridine-5-decylamine: N-[(4-{[3- gas-4-(trifluoromethyl)benzene]sulfonyl) } Phenyl)methyl]-1H-. Bisino[3,2-c]&quot;bipyridin-2-amine oxime 0 N-({4-[(2-carb-4-indolyl))sulfonyl]phenyl}methyl Imidazo[1,2-a]pyrimidine-6-nonylamine α Ν \AA〇/cHi 〇V〇r. 0 N-({4-[(3-chloro-5-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-amidoxime) N -{[4-(5-Galy-3-mercaptopyridine-2-sulfonyl)phenyl]methyl}thieno[2,3-c]»pyridin-2-amine ΚΧ) mu « / N-[(4-{[2-(Didecylamino)phenyl)sulfonyl}phenyl)indolyl]furo[2,3-c]&quot;bipyridin-2-indole Amine 158436.doc -185- 201215609 0 \ N-[(4-{[4-(&quot;Byrrolidin-1-yl)benzene]sulfonyl}benzene σ 6 0 yl) fluorenyl]-1H-pyridyl Zoxa[3,4-b]pyridine-6-nonylamine N-({4-[2-(°tb, i§-'^-1 -3⁄4)-1,3 decyl]phenyl}曱-1Η-吼 并[3,2-c]° pyridine-2-guanamine ^κο / N-[(4-{ [4-(morpholine-4-yl)benzene]sulfonyl) }phenyl) fluorenyl] thieno[2,3-c]pyridin-2-ylamine hc-o ^a', N-({4_[(4-Ga-2-indoxybenzene) sulfonate Thio[phenyl]indenyl)thieno[2,3-c]pyridine-2-carboxamide CCvjCA. 0 N-[(4-{[2-methoxy-5-(trifluorodecyloxy) Benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine-6-carboxamide J~C〇 team ({4-[(4-methoxy-2,5-) Dimethylbenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]. Bis-2-carbamide\h, N-[(4-{[3-fluoro-4-(trifluoromethyl)benzene]]]phenyl)methyl]imidazo[1,2- a] pyrimidine-6-nonylamine 0 158436.doc -186- 201215609

ί· ostso N-[(4-{[3-(propan-2-yloxy)benzene]sulfonyl}phenyl)indenyl]-1Η-»biszolo[3,4-b]. Bisidine-5-nonylamine ^κο of N-{[4_({4-[〇b-bito-1-yl))yl]phenyl}sulfonyl)phenyl]methyl}thiophene [2, 3-c]»Bipyridin-2-carboxamide HC 〇&gt;8, hjc 怵({4-[(2,4,6-tridecylbenzene)sulfonyl]phenyl} fluorenyl) furan [2,3-c]pyridin-2-decylamine N \X^\ COVOCT 0 N-({4-[(2-chloro-5-methylphenyl)sulfonyl]phenyl}methyl)imidazole And [1,2-a]pyrimidine-6-nonylamine F F--F 0 N-[(4-{[2-(¥oxy)-5-(trimethylhydrazinyl)benzene]sulfonyl) }phenyl)methyl]imidazo[l,2-a]pyrimidin-6-nonylamine N-human VIII) ΛN-{[4-(6-methoxy.bipyridin-2-sulfonate) Phenyl] fluorenyl} imidazo[l,2-a]pyrimidin-6-nonylamine N-[(4_{[2_methoxy-4-(1Η-&quot;bisazol-1-yl)) Benzene] sulfonyl}phenyl)indolyl]-1Η-»bido[3,2-c]pyridin-2-decylamine 158436.doc -187· 201215609 N 吟ο(Γ 0 N-[( 4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide 0 iXJH USK i丨, N-(l,3- benzothiazol-6-ylindenyl)-4-[(3- gas benzene)sulfonyl]benzamine ^KO # »/ N-({4-[(2 ,4-dichloro-3-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c] Acridine-2-carbamamine\j〇C iOyjcr 0 Ν·({4-[(4-ethane-yl-3- benzene) continuation]phenyl}methyl)imidazo[l,2- a]pyridine-6-carboxamide^HX) N-({4-[2-(trifluoromethyl)imidazo[l,2_a]» than -6-sulfonyl]phenyl}fluorenyl) Furando[2,3-c]pyridin-2-indoleamine p p,N-{[4-(Phenylthio-4-sulfonyl)phenyl]indolyl}-1H-pyrrolo[3 ,2-c]pyridine-2-carboxamide j/ N-( {4- [ 1 -(4-fluorophenyl)-1H-pyrazole-4-sulfonyl]phenyl}indolyl)-1Η ·»比比和[3,2-c]. Bis-pyridine-2-decylamine

158436.doc •188· 201215609

Where jf Ν-{[4-(1-mercapto-1Η-pyrazole-4-sulfonyl)phenyl]indolyl}-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide Served with 0 N-[(4-{[2-decyloxypyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]-indole-n-pyrazolo[3,4-b] ° Specific bite-5- amidoxime) / N-({4-[(2-gas-5-methoxybenzene)sulfonyl]phenyl}indolyl)thieno[2,3-c] Pyridin-2-decylamine 9 丫w 0 N-[(4-{[3-(cyclopentylamino)phenyl)sulfonyl}phenyl)methyl]isoxazo[1,2- a] pyrimidine-6-formamide 0 N-{[4-({3-[2-(ethyl)-4-yl)ethoxy]phenyl}sulfonyl)phenyl]fluorenyl}-1Η- . More than [3,2-c] ° pyridine-2-guanamine 〇0F cc^xr.丫0 N-[(4-{[4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyro-6 - guanamine ^κο N-[(4-{[4-fluoro-3-(trifluoromethyl)]]]sulfonyl}phenyl)indolyl]thieno[2,3-c]»pyridinium -2- anthraquinone 158436.doc -189- 201215609 ^HX) i Λ N-{[4-(1-indolyl-1H-indazol-5-sulfonyl)phenyl]indolyl}furan[ 2,3-c]pyridine-2-carboxamide N-({4-[(2-fluoro-5-decyloxyphenyl)sulfonyl]phenyl}indolyl) furan[2,3-c ]. Bisidine-2-decylamine.丫0 N-{[4-({3-[(morpholin-4-yl)carbonyl)phenyl}sulfonyl)phenyl]indolyl}-1Η-. Bisazo[3,4-b]»pyridin-5-decylamine 0 N-[(4-{[3-(pyrimidin-2-yl)benzene]sulfonyl}phenyl)indolyl]imidazole And [1,2-a]pyrimidine-6-decylamine liO N-({4-[(2-H-3-methylphenyl)sulfonyl]phenyl}indolyl)thieno[2,3 -c]pyridine-2-guanamine Λ m N-[(4-{[4-amino-2-(trifluoromethyl)benzene]]] phenyl)methyl]-1Η-° ratio And [3,2-c]. Bisidine-2-cartoamine^HX) N-({4-[(2,3-dimercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2 - guanamine 158436.doc -190- 201215609

N-{[4-(l-fluorenyl-1H-carbazol-7-carbyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-nonylamine Q νά, 0 N -({4-[(3-Ga-5-nonyloxybenzene) hydrazino]phenyl}indolyl)imidazo[1,2-a]pyridine-6-nonylamine HX) w. £h N-({4-[(2-Ga-6-decyloxybenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2-carbamide.N, Λ cOyOr. , 0 N-({4-[(3,4-Dimethoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidin-6-nonylamine^h^/ A N-({4-[(3,5-Difluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine. Ice 0 N-[(4-{[3- gas_4_(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridin-6- formazan Amine HX) H,C_0^N-({4-[(4-Ga-2-methoxyphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-A Amine amine 158436.doc -191 - 201215609

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α Λ Η© Ν-[(4-{[5-chloro-2-(2,2-difluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1Η-吼 并 [3, 2-c]«Bistidine-2-decylamine N-{[4-(quinolin-6-sulfonyl)phenyl]indolyl}thieno[2,3-c]pyridine-2-carboxamidine Amine J&lt;0 ί 0 N-[(4_{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c]pyridin-2-indole amine.丫叫Ν Χ Χ Χ 0 N N N N N N N N N N N N N N N N N N N N N N N N N N N 3 3 3 3 3 3 3 3 3 3 3 3 3 b]*&gt;bipyridine-5-carbamamine.,δ(Χ\ο(Τ 0 N-[(4-{8-thiatricyclo[7.4.0.02,7]13-carbon-1 (13 ), 2,4,6,9,11-hexene-6-sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidin-6-nonylamine jRO, ? 0 0 ] N -({4-[(4-butoxyphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide 158436.doc -193- 201215609 F F- -F CO^jCT 0 N-({4-[5-(trifluoromethyl)pyridine-3-sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridinium-6- Formamide KO corpse, N-[(4-{[4-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-曱醯amine is \ N-{ [4-(5-methoxyacridin-2-sulfonyl)phenyl]methyl}furan P,3-c]. Cough-2-carbamamine COyjCT , 0 N-({4-[(3-fluoro-4-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-carboxamide)^ζ } N-({4-[(2-Ethylphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine}^X) N-( {4-[(4-Ethylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-indole Amine 158436.doc 194- 201215609

0 Ν-({4-[(2-Ethylbenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-carboxamide N-[(4-{[ 3-(3,5-dimethyl-1H-pyrazol-1-yl)benzene] hydrazino}phenyl)indolyl]isoxazo[1,2-a]»pyridin-6-oxime Amine HO.Ρ N-({4-[(2-chloro-5-mercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]npyridin-2-carboxamide Ν νζΤ /γ^ Η fYUF 0 N-[(4-{[4-chloro-2-(trifluoromethyl)benzene]] phenyl)methyl]imidazo[1,2-a]pyrimidine -6-Amidoxime Ν \默, co^. 0 N-({4-[(2-methoxy-5-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidin-6-carboxamide 0 N- ({4-[(3-Phenylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidin-6-decylamine COyjCF. 0 Ν-{[4·(6-methoxynaphthalene-2-sulfonyl)phenyl]methyl}imidazo[l,2-a]° pyridine-6-nonylamine 158436.doc -195 - 201215609 „ vO° 0 N-[(4-{[4-(morpholin-4-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidin-6-oxime Amidoxime-({4-[1-(3-chlorophenyl)-1Η-»Bizozol-4-Continuo-yl]phenyl}fluorenyl)-1Η-«比咯和[3,2-c Bis-2-nonylamine ^KO N-[(4-{[3-Ga-5-(hydroxyindenyl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3- c]»Bipyridine-2-decylamine N cr COyOT. 0 N-({4-[(4-fluoro-2-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2 -a]pyrimidine-6-formamide _^HX) N-({4-[(4-ethoxy-2-mercaptophenyl)sulfonyl]phenyl}fluorenyl)thieno[2,3 -c]pyridine-2-carboximine J:KX) $ f N-[(4-{[4-(ethylaminemethylmercapto)benzene]sulfonyl}phenyl)indolyl]thieno[2] ,3-c]&quot;Bistidine-2-carboxamide JM 0 N-[(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)methyl]-1H- Pyrrolo[3,2-c]pyridine-2-carboxamide

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^_HX) H,C N-({4-[(3-Gas-4-mercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide p „〆N-[(4-{[2-(didecylaminomethyl)phenyl]sulfonyl}phenyl)indolyl]-lH-η is more than [3,2-c]» Pyridin-2-carbendazimine O^VJ〇rYb O N-{[4-(phenylsulfonyl)phenyl]indolyl}-5-(pyridin-3-yl)-1,2,4-oxo Oxazole-3-decylamine 0兮\ '-MH Nv /0H from 5-hydroxy-N-[(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)indolyl ]-1Η-吲哚-2-carbamamine 0=1=0 Ά (X^jCT, 0 N-[(4-{[3-(dioxylaminesulfonyl)benzene]sulfonyl}benzene) Base) 曱基]&quot;Mizozolo[l,2-a]pyrimidine-6-decylamine. 0 {Y\ Η ifUJ VnnA^nxA^j N-{[4-(2,3-dihydrogen) -1-benzofuran-7-sulfonyl)phenyl]methyl}imidazo[1,2-a].pyridin-6-decylamine/yCHs VNs^yN\A^ 0 N-{ [ 4-(6-fluorenyl-bipyridin-3-ylindenyl)phenyl]indolyl}imidazo[1,2-a]pyrimidine-6-nonylamine 158436.doc -197- 201215609 1^0 N -[(4-{[2-methoxy-5-(propan-2-yl)benzene]sulfonate. 0-yl}phenyl)indolyl]-lH-opyrho[3,2-φ ratio Acridine-', 2-nonylamine plant R0 Ν-({4-[6-(didecylamino)pyridin-3-sulfonyl]phenyl}fluorenyl) Furando[2,3-c]pyridin-2-decylamine H,C-Ν 〇ocf3 N-[(4-{[2-(trifluorodecyloxy)benzene]sulfinyl}phenyl)曱基]-1H-&quot;Birtho[3,2-c]° pyridine-2-methylamine 2~C〇N-({4-[(3,5cfluorophenyl)sulfonyl] Phenyl}fluorenyl) &lt;thieno[2,3-c]pyridin-2-indoleamine MX) 0 N-({4-[(4_气-3_fluorobenzene)sulfonyl]phenyl }A) thieno[2,3-c]pyridin-2-ylamine. 'N-({4-[(2,4,5-trisyl))]phenyl] 0 fluorenyl)imidazo[1,2-a]pyrimidin-6-carboxamide HX) p N-({4-[(2,4-dimercaptophenyl)sulfonyl]phenyl}曱f' H,C-based)furo[2,3-c]»pyridin-2-indole amine 158436.doc -198- 201215609 ^_HX) 1 N-[(4-{[2- gas-3-(three Fluoromethyl) phenyl] sulfonyl} phenyl) methyl] furo[2,3-c]n than pyridine-2-guanamine Η© € 0 N-[(4-{[3-( 3,5-Dimethyl-1H-pyrazol-1-yl)benzene]sulfonyl}phenyl)indenyl]-lH-η ratio 咯[3,2-c]° ratio bite-2- Indoleamine X Κ〇H,C N-({4-[(2-Ga-4-mercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indole N-({4-[(4-carb-3-indolyl)sulfonyl]phenyl}methyl)-1Η-pyrrole [3,2-c]pyridine-2-carboxamide η/ &gt; 0=t=0 Ν-({4-[1-(propan-2-yl)-1Η-η-biazole-4-sulfonate Phenyl] phenyl} indenyl) imidazo[l,2-a]° pyridine-6-formamide&gt;&lt;X).p[(4-{[3-(difluoromethoxy)) Benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridin-2-ylamine 158436.doc 199- 201215609 /=( N-[(4-{[2-methoxy) -6-(propan-2-yloxy)benzene] &quot;v 〇NP VjT° sulfonyl}phenyl)indenyl]-1Η-°pyrho[3,2-c]pyridin-2-indole Indole AoCT N-({4-[(4-chloro-3-indolyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]acridin-6-carboxamide 0 2~00 p N-({4-[(2,3-Dimercaptophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide H, C —0 5 Λ: N-({4-[(5-Tert-butyl-2-oxooxybenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2- Methionine N-({4-[(4-methoxy-2-methylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0 nMX) .P N-({4-[(2,5-dimethylphenyl)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]pyridine-2-carboxamide N &lt; Xvxr 吖N-({4-[(2-fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)-1Η- Pyrazolo [3,4-b] pyridin-5-amine Yue 0 158436.doc -200- 201215609 Dukes

158436.doc •201 · 201215609 α . \\ \\S/V, 0 N-({4-[(2-Butoxy-5-gasbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6- Methotrexate 1 N-[(4-{[2-chloro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1Η-° ratio [3,2-ten ratio Pyridyl-2-carbamimidoxime N-({4-[(2-gas-3-fluorophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indole Amine ΗΧ-[(4-{[3-(»Byrrolidin-1-yl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridinium- 2-Protonamine K3C CHS 〇 / 'Λ COyOT N-[(4-{[3-Fluoro-5-(2-methylpropoxy)benzene]sulfonyl}phenyl)methyl]imidazo[ 1,2-a]«Bistidine-6-nonylamine N-({4-[(2-fail-5-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrrolo[ 3,2-c]pyridine-2-guanamine 202- 158436.doc 201215609

°HX) 0 l N-({4-[(3-Ga-4-propoxybenzene)-decyl]phenyl}indolyl)thieno[2,3-c]pyridine-2-carboxamide N. 0 N-[(4-{ [2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-decylamine /, 0 N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-carboxamide Φ, N-({ 4-[(2-ethoxyphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide HX) op a N-({4-[(3 -Phenylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indoleamine 0 N-[(4_{[2-曱oxy-4-(1Η-) Pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-nonylamine 158436.doc 203- 201215609

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1^0 N-({4-[(2-chloro-6-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine α :^Λ 0 N-({4-[(3-Chloro-2-indolyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-carboxamide Ν^ ΝΝ\Α^ N-({4-[2-(°Bilo bite-1 -yl)-1,3-supplement sitting-5-continuation thiol]phenyl}indolyl)imidazo[l,2 -a]pyrimidine-6-formamide ΗΧ) Of N-[(4-{5H,6H,7H,8H,9H-imidazo[l,2-a]azet-3-sulfonyl}phenyl ) mercapto] furan [2,3-c]pyridin-2-decylamine °κο 0, 0 i N-({4-[(4-butoxyphenyl)sulfonyl]phenyl}methyl Furano[2,3-c]pyridin-2-indoleamine COyjO^ 0 N-({4-[(3,5-dimethylphenyl)sulfonyl]phenyl}indolyl)imidazo[ l,2-a]pyrimidine-6-nonylamine 158436.doc 205 - 201215609

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OOyjO3. N-[(4-{[4-fluoro-2·(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]acridin-6-oxime Amidoxime, N-({4-[(3-ethoxy-4-fluorophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamidine Amine ff ^ 0 N-({4-[(3-fluoro-2-indolylbenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-carboxamide ch3 . // F 0 N-({4-[(4-butoxy-3-fluorobenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-nonylamine H , C N-({4-[(3-曱oxy-4-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-ηpyr-[3,2-c]acridine-2 -曱醢amine o=ts〇ί (# Ν-({4·[5-(σ比洛 bit-1-yl) bite-3-continuation base] phenyl}fluorenyl)-1,3- Benzothiazole-6-nonylamine 158436.doc -207· 201215609 2~C〇Λ N-{[4-(5-fluoro-6-fluorenyl-2-indenyl)phenyl]methyl} Furo[2,3-c]pyridine-2-carbamimidoxime N-{[4_(morphothio-4-methyl)phenyl]methyl}furo[2,3-c]pyridine- 2-Anthranamine 0 ({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-carboxamide N N -[(4-{[2-methyl-4-(1Η-«bazol-1-yl)benzene]sulfonyl}phenyl)methyl]-1Η-° ratio [3,2-φ Bis-pyridine-2-decylamine α °\ ^ &lt;χνσ', 0 Ν-({4-[(3-chloro-5-methoxybenzene)sulfonyl]phenyl}methyl)- 1Η-pyrazolo[3,4-b]»pyridin-5-decylamine 0 \ m Ν-[(4·{[2_(methylaminesulfonyl)benzene]sulfonyl}phenyl) Methyl]-1Η-吼 并[3,2-c].Bipyridine-2-carbamide 158436.doc 208· 201215 609

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Λ 0 Ν-{[4-({4-[2-(Dimethylamino)ethyl)phenyl}sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyridine-6- Methionamine 0 N-({4-[(5-amino-2-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-decylamine /αχο 〇η N-{[4-(phenylphenanthryl)phenyl]fluorenyl}quinazoline-6-indoleamine 屮f N-[(4-{[4-fluoro-3-(2, 2,2-Trifluoroethoxy)benzene]sulfonyl}phenyl)indenyl]-lH-ηpyr-[3,2-c]pyridine-2-carboxamide ζΤ0 〇=:!=〇 N-[(4-{[3-〇&gt;Byrrolidin-1-yl)benzene]sulfonyl}phenyl)indenyl]-1,3-benzothiazole-6-amidoxime ν / 〇Xsr^^cH= COyjCT. 0 N-({4-[(3,5-dimercaptophenyl)sulfonyl]phenyl}indolyl)-1Η·pyrazolo[3,4-b]pyridine-5-decylamine 、, j〇C ΰΟ^. 0 N-({4-[(3-Gas-4-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 158436 .doc -211 · 201215609 N \J7° N-[(4-{[4-(lH-°Bizozol-1-yl)benzene]sulfonyl}phenyl)indolyl]-1Η-«bitazole [3,4-b]°pyridin-5-decylamine 0 jKO 4 \ N-({4-[(4-butoxy-3-benzene)sulfonyl]phenyl}methyl)furan And [2,3-中比pyridine-2-hydrazinium==:/-^ry-F N-({4-[(4-fluorophenyl)sulfonyl)phenyl}indenyl)thiophene [2,3-c]°Bitter 2-nonylamine H N-{[4-({3-[(propan-2-yl)aminoindolyl]phenyl}sulfonyl)phenyl]- Imidazo[1,2-a]npyridin-6-carboxamide 0 CH, N cr OOyOT 0 N-({4-[(2,4-dimethoxyphenyl)sulfonyl]benzene } 曱 ))-1Η-pyrazolo[3,4-b]pyridine-5-decylamine Nh^X) /vP \_ N-({4-[(2,3-dimethoxy)- 5-nonylbenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide h〆, &lt;jH, 0//^S'CH, 00 &lt; x\〇cr 0 N-[(4-{[2-Fluoro-3-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]. Bisidine·6_methylamine 158436.doc 212- 201215609

158436.doc -213- 201215609 0 N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6 -carbamamine 1^0 male. N-({4-[(2-butoxy-4-fluorobenzene)sulfonyl]phenyl}indolyl)-1Η·pyrrolo[3,2-c] Pyridine-2-decylamine °κο 0,. 0 l N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine NH4-pyrenequinone Phenyl)imidazo[1,2-a]° pyridine-6-yl 肼0 N-({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}methyl)- 1Η-pyrazolo[3,4-b]pyridine-5-formamide 0 N-{[4-(isoquinolin-4-indolyl)phenyl]methyl}-1H-pyrazolo[ 3,4-b]pyridine-5-decylamine 1^0 0-ω· N-({4-[(2,6-dimethylphenyl)sulfonyl]phenyl}fluorenyl)furan[ 2,3-c]pyridine-2-guanamine

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. Dd if Μ 0 N-{[4-(2,3-dihydrobenzobenzopyran-7- fluorenyl)phenyl]indolyl}imidazo[l,2-a]pyrimidin-6-carboxamidine Amine N, s0i; OOy^r. 0 N-({4-[6-(Dimethylamino)pyridine-3-sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-oxime Amine FN Ά cc^xr. 0 N-({4-[(3-fluorophenyl)-decyl]phenyl}indolyl) imazolo[l,2-a]pyrimidine-6-nonylamine over. 0 N-({4-[(2-Ga-5-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyro-6-carbamide HX), N-({4-[(4-ethoxy-2-mercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide N-[ (4-{[2-(Hydroxy)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide jo H,C—0 〇 ^s{. N-({4-[(5-Ethyl-2-yloxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2- Formamide 158436.doc -217- 201215609 N \X&gt;~〇N-({4-[l-(3-Phenylphenyl)-lH-»Bizozol-4-sulfonyl]phenyl}fluorenyl )&quot;Mizozolo[l,2-a]〇t bit-6-carbamamine 0 ^KO 4: N-[(4-{[4- gas-3-(trifluoromethyl)benzene]sulfonate Mercapto}phenyl)methyl]furo[2,3-φ-pyridin-2-ylamine 1^0 4 Ν-({4-[(2-butoxy-4-fluorobenzene)) (phenyl)methyl)thieno[2,3-c]pyridin-2-indoleamine X Ν-[(4-{[2-decyloxy-5-(trifluoromethoxy)benzene] Sulfosyl}phenyl)indolyl]-lH-alphabiazo[3,4-b]. Bipyridine-5-cartoamine 0 N COyjiP N-[(4-{2-[ethyl(methyl)amino]-1,3-thiazol-5-sulfonyl}phenyl)methyl]imidazole And [1,2-a]«biidine-6-branched amine 0 N, N\ / e CCi^jCT. N-({4-[(4-ethylphenyl)sulfonyl]phenyl}indenyl)imidazo[1,2-a]pyrimidine-6-nonylamine 0 ii N-({4-[( 4-ox-3-oxooxybenzene)sulfonyl]phenyl}methyl)-1Η-»Bedo[3,2-φ-pyridin-2-ylamine 158436.doc •218· 201215609

〇αη c 0 N-({4-[(2-chloro-5-decyloxybenzene) hydrazino]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0 N-({4-[5-(Trifluoromethyl)acridin-2-sulfonyl]phenyl}indolyl)imidazo[1,2-appyridyl-6-carboxamide jKO 4 N- {[4-(5-fluoro.bipyridin-3-sulfonyl)phenyl]indolyl} thieno[2,3-c]pyridin-2-ylamine r.—N 〇0 ^XrVi〇0 Ν-{[4-(Benzene fluorenyl)phenyl]fluorenyl}thieno[2,3-b]pyrrole-6-nonylamine ^KO / N-({4-[5-(trifluoro Methyl)pyridine-2-sulfonyl]phenyl}methyl)furo[2,3-c]-pyridin-2-ylamine 1^0 N-({4-[(2-butoxy) 5--5-chlorophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide N \Λ/ν COyjCT 0 N-[(4-{2-[ Ethyl (methyl)amino]-l, 3-° plug ° sit-5-sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-decylamine 158436. Doc -219· 201215609 —F N-[(4-{[2-Gas-H-trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6- Indole N \ Lin &lt; χ \ατ. 0 N-{[4-(quinoline-6-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyrimidine-6-nonylamine N-({4-[(3-B) Oxy-2-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 6 N-[(4-{[2-(? Porphyrin_4·ylmercapto)phenyl]sulfonyl}phenyl)methyl]-1H--pyrho[3,2-c].比 曱醯 曱醯 曱醯 ά N-({4-[(4-曱-oxy-3-methylphenyl)sulfonyl]phenyl}indolyl)-1Η-〇比咯和[3,2 -c] acridine-2-nonylamine vl^X) N-({4-[(3-fluoro-4-decyloxyphenyl)sulfonyl]phenyl}methyl)thiophene [2,3 -c]&quot;Bipyridine-2-cartoamine 1^0 4; N-{[4-(5-fluorenyl.pyridin-3-ylindolyl)phenyl]methyl}thiophene[2, 3-c]pyridine-2-guanamine 158436.doc -220- 201215609

Ν 0 N-{[4-(2,3-dihydro-1-benzofuran-7-sulfonyl) phenyl]methyl}-1Η-pyrazolo[3,4-b]pyridine-5 -carbamamine HX) v/ N-[(4-{6-azamidazo[l,2-a]acridin-3-sulfonyl}phenyl)methyl]furo[2,3-c ]»Bistidine-2-decylamine / V νδ N-[(4-{[3-(propane-1-ylideneamino)benzene]sulfonyl}phenyl)indolyl]imidazo[1, 2-a]pyrimidine-6-nonylamine N v6 0 N-({4-[(3-decyloxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4- b]pyridine-5-nonylamine N-({4-[(3-fluoro-4-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine -2-decylamine HX) 0,. Ν·({4-[(4-methylphenyl)indolyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indole^HX) / h/ Ν-({ 4-[(4-chloro-3-indolylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine 158436.doc -221 · 201215609 °Κ0 - i HC—^ {{4-({3-[2-(didecylamino)ethoxy]benzene}sulfonyl)phenyl]fluorenyl}furo[2,3-c]pyridine 2-carbamamine ί k N-{[4-(2-mercapto-2H-indazol-6-sulfonyl)phenyl]indolyl} -1H-. Bisino[3,2-c]&quot;bipyridine-2-decylamine F F--F v0 cCyjCT N-[(4-{[3-(2,2,2-trifluoroethoxy)) Benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]»pyridin-6-carboxamide OOy^O3,1] N-[(4-{[3-(cyclopentyl) Amidino)phenyl]sulfonyl}phenyl)methyl]-oxazolo[1,2-a]. Bipyridine-6-formamide N-[(4-{[4-lac-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-indole[3,2 -c]»Bipyridine-2-carboxamide N \jp N-({4-[(2-cyanophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine- 6-decylamine p H,C N-({4-[(2,4-dimethylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine- 2-nonylamine

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0 N-{ [4-(5-decylpyridin-3-sulfonyl)phenyl]fluorenyl}0 m 0 sit and [l,2-a]0 than bite-6-nonylamine F — Ν α 0 -F J J Ν-[(4·{[2-Gayl-H-trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]isoazolo[l,2-a]pyrimidine-6- Indoleamine 5^0 c °&lt; N-[(4-{[2-chloro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3, 2-c]pyridine-2-guanamine ΗΧ) Λ N-({4-[(3-Ga-5-fluoro))sulfonyl]phenyl}indolyl)furan[2,3-c] Pyridine-2-indenylamine ^_ΗΧ) 0^&quot; N-[(4-{[3-(°-pyrrolidin-1-yl)benzene]sulfonyl}phenyl)methyl]furan[2 ,3-c]pyridin-2-ylamine^κο f N-[(4-{[3-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]furan P,3- c]pyridin-2-decylamine N-({4-[(2-ethylmercaptophenyl)sulfonyl]phenyl}methyl)-1Η-° ratio of [3,2-c]° Acridine-2-decylamine 158436.doc -223 - 201215609 Ν-({4-[(4-Gayl-3-fluorophenyl)sulfonyl]phenyl}methyl) ° Furan[2,3- c]pyridin-2-decylamine 5-trans-yl-indole-{[4-(1-mercapto-1Η-σ 引 0 sit-4-continued)phenyl]methyl}-1Η·吲哚-2-carboxamide ^κο V Ν-{[4-(2,6-dimethoxy.bipyridine-3-sulfonyl)phenyl] Furano[2,3-c]pyridine-2-carboxamide 1^0 Ν-({4-[(2-butoxy-6-fluorobenzene)sulfonyl]phenyl}methyl) -1Η-. Bisolo[3,2-c]acridin-2-carboxamide Ν ^\XXF CQy^XT, 0 N-({4-[(3-fluoro-2-mercaptophenyl)sulfonyl] Phenyl} fluorenyl)imidazo[l,2-a]pyrimidine-6-carbamimidoxime) ρ ν N-{[4_(naphthalene-1-thenyl)phenyl]fluorenyl}furan[2 ,3-c]pyridine-2-carboxamide 4 N-({4-[(3,5-difluorophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c Pyridine-2-decylamine 158436.doc • 224· 201215609

158436.doc -225 - 201215609 α 0 Ν-[(4-{[3-chloro-5-(hydroxyindenyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]&quot ; pyridine-6-nonylamine jRO Of N-[(4-{6-azamidazo[1,2-a]»pyridin-3-sulfonyl}phenyl)indolyl]thieno[2] , 3-c] acridine-2-carbamimidoxime-({4-[1-(4-fluorophenyl)-1Η-pyrazole-4- continued indolyl]phenyl}methyl)furan[ 2,3_C]acridine_2·carbamamine^κο N-{[4-(quinolin-6-sulfonyl)phenyl]methyl}furo[2,3-c]pyridin-2-indole Indoleamine 0 N-({4-[6-(3,4-difluorophenyl)pyridin-2-sulfonyl]phenyl}indolyl) oxazolo[l,2-a]pyro-6 -carbamamine / N-({4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}indolyl)-1Η-»比咯和[3,2-c]比 pyridine-2-amidoxime-{[4-(1,5-dimethyl-1H-imidazole-2-ylidene)phenyl]methyl}imidazo[1,2-a]pyrimidine -6-decylamine 158436.doc -226- 201215609

°HX) N-[(4-{[2-(dimethylaminocarbamimidino)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine-2-carboxamide COyOCT. 0 N-({4-[(4-chloro-3-gasbenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-nonylamine N Ά &lt;Χ\ ^〇Γ. 0 N-({4-[(3-fluoro-5-decyloxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-amidoxime y~ °v/^g N-[(4-{[4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine 2-Protonamine w, a-N-({4-[(2,6-dichlorobenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine- 2-曱醯amine 0 i. N-({4-[(4-Ethylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine-2- Guanamine COyXT. 0 N-({4-[(3,5-Dioxaoxybenzene)sulfonyl]phenyl} fluorenyl)imidazo[1,2-a]° pyridine-6-decylamine 158436.doc -227· 201215609

158436.doc •228· 201215609

158436.doc 229- 201215609

158436.doc *230· 201215609 广, 0=8=0 Ν-[(4-{[3-(乙烧醯基)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2- a]°-pyridyl-6-decylamine 0 N-{[4-(phenylindoleyl)phenyl]indolyl}-3-(»pyridin-3-yl)-1,2-oxazole- 5-carbamamine °ΚΧιι ΐ〇Γ N-[(4_{[2·曱oxy-4_(1H-pyrazol-1-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2] , 3-c]. Bipyridyl-2-carbendazim CCVJT 旮0 Ν-[(4-{ρ-(1Η-oxazol-1-yl) oxa]sulfonyl}phenyl)indolyl]imidazo[1,2-a Pyridine-6-carbamide plant. Touch ^/==( N-({4-[(3-Ga-4-propoxybenzene)sulfonyl]phenyl}indolyl)-1Η-.Bisto[3,2-c]〇 Bis-pyridine-2-indoleamine y^co /~〇Ν-({4·[(5-Ga-2-propoxybenzene)sulfonyl]phenyl}indolyl) furan [2,3 -c]pyridine-2-carbamide N-[(4-{[3-|L-5-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-indole[ 3,2-c].pyridin-2-amine 〇vf\ Η Ν wsAA^n\/ch&gt; σχχτ^ N-[(4-{[3-(ethylamine fluorenyl)benzene] sulfonate Mercapto}phenyl)indolyl]imidazo[1,2-a]pyrimidine-6-carboxamide 0 158436.doc •231 - 201215609 c h3c- «3 -CHj N-({4-[(5- Tert-butyl-2-decyloxybenzene)sulfonyl]phenyl}indolyl]zozolo[l,2-a]pyrimidine-6-nonylamine i N-({4-[(3- Ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-»pyrolo[3,2-c]pyridine-2-carboxamide N-({4-[6-( 3,4-difluorophenyl)indolepyridin-2-ylidene]phenyl}methyl)-1Η-ηpyrho[3,2-c]«pyridin-2-carboxamide v〇 )~i OX*j〇r^ 0 —F N-({4-[2-(Trifluoromethyl) oxazolo[l,2-a]«比pyridine-6- fluorenyl]phenyl} Methyl)imidazo[l,2_a]pyridine-6-carboxamide^KO / N-({4-[(4-cyanobenzo)sulfonyl] Furyl [2,3-c]pyridine-2-carboxamide C〇yJ〇^ 0 N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonate醯 }} phenyl) fluorenyl] oxazolo[l,2-a]pyrimidine-6-decylamine.h^CO. N-({4-[(4-Methoxybenzo)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-ylamine 158436.doc 232· 201215609

Plant should be N-({4-[(3,5-dimercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine 0 N -({4-[(4-Ethylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine N caa COyjCT. 0 N-({4-[(5-Chloro-2-indolyl)sulfonyl]phenyl}indenyl)imidazo[l,2-a]pyrimidine-6-carboxamide FN (OyjO^ 0 N-[(4-{[3-H-5-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidin-6-decylamine h /N-({4-[(2,3-Dimethoxyphenyl)indolyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine °yc ^ N \j6 «VjCT 0 N-({4-[(3-ethylmercaptophenyl)sulfonyl]phenyl}methyl)-1Η-° ratio °[3,4-b]° bite -5-decylamine 158436.doc 233 - 201215609

Fv % % N-[(4-{ [2,4-bis(trifluoromethyl)]]] fluorenyl}phenyl)methyl]furo[2,3-c]pyridin-2-decylamine m ; K0 i Ν·[(4-{[4-(ethoxyindolyl)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridine-2-carboxamide \/ό avxr. N-{[4-(5-azetidin-3-sulfonyl)phenyl]methyl} imidazo[1,2-a]pyridine-6-carboxamide 0 NP F V. N-( {4-[(2-Fluoro-5(nonylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide d N-({4 -[(3-fluoro-5-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-indole N-({4-[(4-fluoro) Benzenesulfonyl]phenyl}methyl)-1H-pyrrolo[3,2-c]pyridine-2-carboxamide HX) f N-[(4-{[2-曱-oxy-5- (prop-2-yl)phenyl]sulfonyl}phenyl)indolyl]furo[2,3-c]. Bipyridine-2-A &gt;#, guanamine 158436.doc -234- 201215609

〇/Λ〇N-[(4-{[3-(Trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1,3-benzothiazole-6-carbamimidoxime/N Tvs 0 N-{[4-(4-decylacridin-3-sulfonyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]acridin-5-indole amine HX) 6 Ν-{[4-〇·Bistidin-3-sulfonyl)phenyl]fluorenyl}furo[2,3-c]pyridin-2-decylamine r 0, N-({4 -[(3-propoxybenzene)-indolyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-amidoxime 〇Vxr, 0 N-({4-[(2 _Fluoryl_4_mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidin-6-indoleamine § H, C V. \ N-(H-[( 2,5-dimercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-indole N-({4-[(2-chloro-5-) Nonylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-ylamine 158436.doc -235 - 201215609 ^HX) N-[(4_{[ 3_Fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-φpyridin-2-carboxamide^HX) Ν-({4-[( 3,5-dimercaptophenyl)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridin-2-indoleamine C, .C0 0 Ν-({4-[(2, 3-dimethoxybenzene)sulfonyl]phenyl}mercapto)imidazo[1,2-a]pyrimidine-6- Amine.i 0 N-({4-[(3-ethylbenzene) contigyl)phenyl}methyl) imidazo[1,2-a]pyrimidin-6-carboxamide HX) φ Ν-{ [4-(2Η-1,3-benzodioxol-5-sulfonyl)phenyl]indolyl}furo[2,3-c]»bipyridine-2_decylamine/ΚΟ §) N-[(4-{[2-Mercapto-4-(1Η-&quot;pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c] Pyridine-2-decylamine r2 o=s=o \j6 0 N-({4-[(3-Aminosulfonylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a ° ° pyridine-6-formamide 158436.doc -236- 201215609

0 N-[(4-{[3-(pyrrole-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine-6-carboxamide N-[ (4-{[4-(Trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidin-6-decylamine 0 N-{[4-( {3-[(2-Methylpropyl)amine-carbamoyl]benzene}sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidin-6-nonylamine l^X) r矣咚V η/ N-({4-[(2,3,6-trimethoxybenzene)) phenyl]methyl}methyl)thieno[2,3-c]pyridine-2-carboxamidine Amine N Ά c〇y^a " O N-({4-[(2-fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6 -carbamamine»/ N-({4-[(3-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine- 2-carbamimidoxime op N- {[4-( 1 -methyl-1H-indazole-4-sulfonyl)phenyl]methyl}furo[2,3-c]pyridin-2-indole醯amine 158436.doc -237- 201215609 ο N-{[4-(phenylsulfonyl)phenyl]indolyl}imidazo[1,2-a]0 is 0 -6-cartoamine\^CH3 d ΓΤ νΝΝ;/γΝΝ&gt;^ N-({4-[(2-chloro-4-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-oxime Guanamine &quot;CCyoO5^ N-({4-[(4-butoxy-3-benzene))] benzene (曱))-1Η-pyrazolo[3,4-b]pyridine-5-nonylamine-xxx^ N-(6-(4-(morpholinylfluorenyl)phenoxy)hexyl)- 1H-pyrrolo[3,2-c]pyridin-2-indoleamine / C0 oo^xr^ 0 N-({4-[(3-ethoxy-2-fluorophenyl)sulfonyl]phenyl }曱))imidazo[l,2-a]pyridine-6-decylamine 0 O-CH, N-[(4-{[4-(4-mercaptopiperazin-1-yl)benzene]sulfonate Mercapto}phenyl)indolyl]-lH-nt-[3,2-c].pyridin-2-decylamine&lt;X\〇T. 0 N-{[4-(quino-8 -sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-nonylamine H,-,%P N-({4-[(4-chloro-2-decyloxy) Benzenesulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 158436.doc -238- 201215609

158436.doc -239- 201215609 FF-\\F) N-({4-[4-(trifluoromethyl)"pyridin-2-sulfonyl]phenyl}methyl)-1Η-pyrazole And [3,4-b]pyridine-5-decylamine Ν-{[4-(2Η-1,3-benzodioxole-4-sulfonyl)phenyl]fluorenyl} -1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0 乂[(4-{[4-(trifluoromethyl)benzene]sulfonyl}phenyl]methyl]imidazo[ 1,2-a]pyrimidin-6-decylamine 0 N-[(4- {5H,6H, 7H,8H,9H-imidazo[1,2-a]azol-3-sulfonyl}benzene Methyl]-1Η-»Bizozolo[3,4-b]pyridine-5-carboxamide, ρ --d ◎ N-[(4-{[3-fluoro-4-(1Η-&quot ;bazol-1-yl)phenyl]sulfonyl}phenyl)indolyl]-fluorene-β-pyrolo[3,2-c]°pyridin-2-ylamine^κο / V N-{ [4-(6-decylnaphthalene-2-sulfonyl)phenyl]methyl}furo[2,3-c]pyridin-2-decylamine

158436.doc 240- 201215609 0 N- {[4-(2-Methyl-2H-carbazol-6-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyridine-6-oxime Indoleamine, hydrazine) p N-({4-[(2-methylphenyl) hydrazino]phenyl}fluorenyl) thieno[2,3-c]pyridine-2-carboxamide FN \j5 co ^ir. N-{[4-(5-fluoroindole-3-sulfonyl)phenyl]methyl} imidazo[l,2-a]pyrimidine-6-cartoamine 1 'square Ν·((4- [(2,4-dioxa-3-indolylbenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]°pyridin-6-decylamine 0 Nh^O op N -({4-[(5-fluoro-2-indolylbenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine F_^0 ^\h, l^X) N-{[4-(Naphthalene-1-sulfonyl)phenyl]indolyl}thieno[2,3-c]pyridin-2-ylamine 158436.doc 241 - 201215609

158436.doc 242- 201215609 0 , \χ0 &lt;X)y^a,,. 0 N-{[4-(5-chloro.pyridin-3-sulfonyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]acridin-5-nonylamine ΜΧ) c N-({4-[(3-methylphenyl)-decyl]phenyl}fluorenyl) thieno[2,3-c]pyridin-2-ylamine / N-CH, N-[( 4-{[4-(Didecylaminoindolyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridin-2-indole OH 0 N- [(4-{[4-(Pentyl)phenyl)sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyridine-6-amidoxime N \XX 00^. , 0 N-({4-[(3,4-Dimethoxyphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine HX) N- {[4-( 1 -mercapto-1H-吲嗤-6- continuation) phenyl]fluorenyl}furo[2,3-c]pyridine-2-carboxamide 158436.doc 243 · 201215609 ρ N-{[4-(2,3-Dihydro-1-benzofuran-7-sulfanyl)phenyl]methyl}thieno[2,3-c]pyridin-2-indole Indole ηΠ Ν W 0) yja, \. 0 N-{[4-( 1H-吲哚-7-indolyl)phenyl]methyl}-1H-pyrazolo[3,4-b]pyridine-5-carboxamide C HjC^— CCyjO ^ _〇S N-({4-[(3-Tert-butylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidin-6-nonylamine V 丫A 0 fY 0 N-[(4-{[4-(propyl-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-carboxamide jHX ) p »/ N-{[4-({3-[(propan-2-yl))aminomethane]phenyl}sulfonyl)phenyl]methyl}thieno[2,3-c]pyridine- 2-Protonamine A N-({4-[(2,3-Didecyloxy-5-methylphenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine- 2-Proline amine co^a^ 〇&lt;^ N-{[4-(phenylsulfonyl)phenyl]methyl}-1,5-acridin-2-carboxamide 158436.doc -244- 201215609

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(Into 〇0^ 0 °\/CH3 N-({4-[C4-gas-2-ethoxybenzene) fluorenyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine- 6-carbamamine r&quot; 0=8=0 Ν \j6 o' N-[(4-{[3-(乙烧醯))]]]]]]]]]]]]] ,2-a]pyrimidine-6-carbamide °ΗΧ) ί N-{[4-({3-[2-(dimethylamino)ethyl]benzene}sulfonyl)phenyl]fluorenyl }Thiopheno[2,3-φ-pyridin-2-ylamine^ΗΧ) Ί e· 怍({4-[(4-曱-oxy-3,5-didecylbenzene)) }]methyl)thieno[2,3-c]&quot;bipyridyl-2-carboxamide 0 α; Ν-({4-[(3,4-difluorophenyl)sulfonyl]phenyl} Methyl)imidazo[1,2-a]pyrimidin-6-nonylamine jKO i 讣[(4-{[3-fluoro-4-(2,2,2-trifluoroethoxy)benzene] sulfonate醯 }}phenyl) fluorenyl] furan [2,3- decan-2-amine 158436.doc 247- 201215609 ^κο H,C-W Ν-({4-[2-(二曱Amino)pyrimidine-5-benzyl]phenyl}indenyl)furo[2,3-c]acridin-2-indoleamine N-({4-[(2-ethoxybenzene) Sulfo]phenyl]indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0 N-[(4-{[2-methoxy-5-(propyl-) 2-yl)phenyl]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-formamidine 1Ν\^Υ〇^Χ α N-({4-[(2,6-dioxabenzene)sulfonyl]phenyl}methyl) °m° sit and [1,2-&amp;]° bite -6-nonylamine ^κο Λ N-({4-[(2-fluoro-5-decyloxybenzene)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]pyridine-2 - indoleamine, hydrazine) hjc^-\h, N-({4-[(2-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}indolyl)thieno[2,3- c]pyridin-2-decylamine 158436.doc 248- 201215609

4 N-({4-[(3-chloro-5-methoxyphenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indoleamine F N- ({4-[(3,5-Difluorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-amidoxime) Λ N-(H-[( 2-ethylbenzene)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridin-2-indoleamine 1 0SIS· ί N-({4-[(4-phenylbenzene)) Sulfhydryl] stupyl} fluorenyl)-1,3-benzothiazol-6-nonylamine 〇s climbing sony N-[(4-{[3-(3,5-dimethyl-1H-pyridyl) Zin-1-yl) phenyl]sulfonyl}phenyl)methyl]-1,3-benzothiazol-6-nonylamine ί N-[(4-{[4-(ethoxy fluorenyl)) Benzene] S basket base} phenyl) methyl]-1H-indolo[3,2-c]-pyridin-2-ylamine 0 0 H (fW, \nAn/CH3 0 ch3 Ν-( {4·[5-(Didecylamino)pyrazine-2-sulfonyl]phenyl}methyl)"moxazolo[1,2-a].pyridyl-6-decylamine 158436. Doc -249- 201215609

158436.doc •250· 201215609

158436.doc 251 - 201215609 N Ά〇σ,, 0 N-({4-[(2-fluoro-3-indolylbenzene))]phenyl}indolyl)-1Η-pyrazolo[3 , 4-b]pyridine-5-carboxamide # N-({4-[(4-gas-3-fluorobenzene)sulfonyl]phenyl}fluorenyl)-1Η-»比比和[3, 2-c]pyridin-2-decylamine jHX) ·&amp; N- [(4- {[2-fluoro-4-(1Η-»Bizozol-1 -yl)benzene]sulfonyl}phenyl) Methyl]furo[2,3-c]&quot;bipyridine_2·carbamamine N \0 o^xr. 0 N-{[4-(5-methoxy.bipyridin-3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-nonylamine QF\ RO N- ({4-[2-(Trifluoromethyl).pyridin-3-sulfonyl]phenyl}methyl)furo[2,3-pyridin-2-amine „frF F (Y \ . jfY^. 0 N-[(4-{[4-fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l, 2-a] pyrimidine-6-amide 158436.doc 252- 201215609

158436.doc -253 - 201215609. /s 0 N-({4-[(3,5-Dimethoxybenzene)-decyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-formamidine Amine N-[(4-{[2-(morpholin-4-ylindenyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0 N-({4-[(2,6-dioxa-3-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-carboxamide jKO N- ({4-[(2-Fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide HX) i N-({4 -[(3-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-ylamine^KO Ν·[(4-{[5-fluoro_2_(( Phenyl]sulfonyl}phenyl)methyl]thieno[2,3-φ-pyridin-2-ylamine 158436.doc -254- 201215609

158436.doc - 255 - 201215609 F F--F m H VIII, N-[(4-{[5-hydroxy-2-(trifluoromethoxy) phenyl] sulfonyl}phenyl) fluorenyl] -ΙΗ-η-Bizozolo[3,4-b]»pyridin-5-decylamine 0 , '0° Ν-[(4-{[4-(1Η-imidazol-1-yl)benzene]sulfonate Mercapto}phenyl)indolyl]imidazo[1,2-a]pyrimidine-6-carboxamide 0 N-{[4-(phenylsulfonyl)phenyl]methyl}-1Η-° 嗤And [3,4-b]pyridine-3-carboxamide o II co^h^〇lsxtf N-({4-[(4-|L phenyl)sulfonyl]phenyl} fluorenyl) And [l,2-a]° ratio bite-6-nonylamine N \XX (Yl h fTx° N-({4-[(3,4-difluorobenzene)sulfonyl]phenyl}fluorenyl) )-1Η-0 is 0 and 0[3,4-b]. Ratio-5-carbamamine s jKO i N-({4-[(4-butoxy-3-benzene) sulfonium) Thio[2,3-c]pyridine-2-carboxamide p ° &lt; HjC /=( 〇N- {[4-( 1 -methyl-1H-carbazole - 6-sulfonyl)phenyl]fluorenyl}-1Η-°pyrho[3,2-c]»pyridin-2-ylamine 158436.doc -256- 201215609

158436.doc 257- 201215609 0' \ Ν-({4-[(4-butoxy-2-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c ]»Bipyridine-2-decylamine) / N-{[4-(6-decylnaphthalene-2-sulfonyl)phenyl]indolyl} -1Η-»比咯和[3,2- c]. Bis-pyridine-2-decylamine C &gt;C0 si ί N-[(4-{[3-(propane-1-sulfonylamino)benzene]sulfonyl}phenyl)methyl]thiophene[2] ,3-c]pyridine-2-carboxamide N-[(4-{[4-gas_3_(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2- a]pyrimidine-6-carbamamine^ΗΧ). Λ Ν·[(4-{[3-fluoro-5-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)methyl]thiophene And [2,3-c]. Bis-2-carbamide V «νσ, N-[(4-{[2-mercapto-4-(1Η-« thiazol-1-yl)benzene]sulfonyl}phenyl)methyl] -1Η-'Bizozolo[3,4-b]&quot;Bipyridine-5-decylamine 0 158436.doc 258· 201215609 α Ν8 COyXT. 0 Ν-({4_[(3-chloro-5-fluorophenyl)sulfonyl]phenyl}fluorenyl)-1Η-0 ratio °[3,4-b]° ratio.定-5-Amidoxime ν〇^ 0 N-({4-[5-(Trifluoromethyl)"pyridin-2-sulfonyl]phenyl}indolyl)-1Η-pyrazolo[ 3,4-b]pyridine-5-decylamine 0 N-({4-[(3-methylphenyl))]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6 - decylamine: Ύ) 0 N-{[4-(2-indolyl)pyridin-3-sulfonyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]pyridine- 5-carbamamine 1^! ? N-({4-[(2-aminophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indoleamine 〇N-{[4-(6-fluorenyl)pyridin-2-sulfonyl)phenyl]fluorenyl}furo[2,3-c]pyridin-2-indole N-{[4- (phenyl phenyl) phenyl] fluorenyl}-1 Η-&quot; bis-[3,2-c]pyridin-2-decylamine 158436.doc 259· 201215609

158436.doc -260- 201215609

/ Ν νέ 0 N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidin-6-carboxamide F „ . Yj〇r, 0 N-({4-[(3-)-(4-aminophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5 - guanamine F F--F \j6 «ν〇σ,, 0 N-({4-[4-(trifluoromethyl)pyridine-2-sulfonyl]phenyl}indolyl) imidazo[ 1,2-a]pyridine-6-nonylamine\KX) N-[(4-{[4-Gaxo 2_(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]furan[ 2,3-φ-pyridin-2-indoleamine 1^0 y-〇N-({4-[(4-chloro-2-ethoxyphenyl)sulfonyl]phenyl}methyl)furan [2,3-c]pyridin-2-carboxamide HX) N-{[4-(2,3-dihydro-1-benzofuran-7-sulfonyl)phenyl]methyl}furan And [2,3-c] acridine-2-nonylamine 158436.doc •261 - 201215609 λν 0 N-[(4-{[3-(trifluorodecyloxy)benzene] fluorenyl}phenyl Mercapto]imidazo[l,2-a]pyrimidine-6-nonylamine N-({4-[4-(trifluoromethylhomopyridin-2-sulfonyl)phenyl}fluorenyl) Furando[2,3-c]pyridine-2-carboxamide^κο Λ N-[(4- {[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl}phenyl ) mercapto] furan [2,3-c]pyridin-2-decylamine. Ρ HC-Ο S, W, ο^° N-({4-[(2-Ga-6-decyloxybenzene)sulfonyl]phenyl}indenyl)-1Η-&quot;比比和[3,2-c Acridine-2-decylamine N-{[3-(phenylsulfonyl)phenyl]methyl}-1Η-°pyrho[3,2-c]pyridin-2-decylamine VN\ A^N\Ay 0 N-[(4-{[4-fluoro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]nbipyridine -6-decylamine N {» %jCT 0 N-({4-[(2-ethoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6- Guanamine 158436.doc •262- 201215609

, ΜΧ). , 0 Άγ Ν-[(4-{[2-methoxy-5-(propan-2-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine-2 - formamide ω V N-[(4-{[2-methyl-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2_a]. Bis-pyridine-6-carbamide, ΜΧ) Λ. N-({4-[(2-methoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2 - amidoxime) ^ ρ ¥ N-({4-[(2-phenoxy)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine_2·decylamine &lt;xi 0 [η fy \,. N-({4-[(4-Gas))sulfonyl]phenyl}indolyl) is sitting and [l,2-a]°S°^-6-decylamine 1 〇F ά. ) N-({4-[(3-Gas_5_mercaptophenyl)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide 158436.doc 263 - 201215609

158436.doc 264· 201215609

^κο Ί Ν-[(4-{[3-(ethanesulfonyl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridin-2-ylamine ^_ΗΧ Ν-({4-[(2-Fluorophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indoleamine. Γ) /γ\ Η r/u 0 N-{[4-(4-mercapto's bite:-3-continuation) phenyl]fluorenyl}imidazo[1,2-a]pyrimidine-6 - indoleamine N-({4-[(3,4-dimethoxyphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indole Amine H3C d fr, \. VN^yN\A^ 0 N- {[4-(1,4·didecyl-1H-imidazol-2-sulfonyl)phenyl]indolyl}imidazo[1,2-piperidine-6 - amidoxime ν (Γ cOy^cr. 0 N-({4-[2-(didecylamino)pyrimidin-5-sulfonyl]phenyl}indolyl)imidazo[1,2- a] pyridine-6-nonylamine 158436.doc 265- 201215609

^:N 0 N-{[4-(l-fluorenyl-1Η-»Bizozol-4-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyrimidine-6-carboxamide H3C CH, 〇/ NC〇yHJ〇^ 0 N-[(4-{[3-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a ° ° pyridine-6-decylamine 0 N-[(4-{[2- gas-4-(trifluoromethyl)benzene] hydrazino} phenyl) fluorenyl] imidazo[l,2- a] Pyrimidine-6-formamide °K〇. 4. N-({4-[(3-butoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indole MX) h3c N-({4- [(2,4-dimethylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-indoleamine / ό N-({4-[(4-A) Oxyphenyl)sulfonyl]phenyl}methyl)-1H-. Bisolo[3,2-c]-bipyridine-2-carboxamide C 158436.doc -266- 201215609 }~XX) N-[(4-{[4_(prop-2-yl)benzene]sulfonate Thio[phenyl]indenyl]thieno[2,3-c]pyridin-2-indole[(4-{[2-(trifluoromethyl)benzene]sulfonyl}phenyl)indole -1H-indolo[3,2-c]pyridin-2-decylamine i N-({4-[(3-ethylhydrazinobenzene))]phenyl}indolyl)- 1Η-° 比比和[3,2-c]° pyridine-2-meramine 1^X) p N-({4-[(2-ethoxy-4-fluorobenzene)sulfonyl] Benzoyl}hydrazino)thieno[2,3-c]° pyridine-2-guanamine: TT d ff. N-{[4-(5-chloro-3-indenyl)pyridin-2-sulfonyl)phenyl]methyl}imidazo[1,2-a]pyridine-6-carboxamide S , ' Mi νΛλΧΤ. N-({4-[2-(3-Fluorophenyl)-1,3-thiazole-4-sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]. Bipyridine-5-carbamamine ! 158436.doc 267· 201215609

158436.doc •268· 201215609

hC〇ί Λ Ν-[(4-{[4-(Tri-lmethoxy)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-carboxamide N-{[4-(quinoline-3-sulfonyl)phenyl]methyl}-1Η-pyrrolo[3,2-c]pyridin-2-ylamine / \)6 COyXP 0 N-" 4-[(3-ethoxy-2-fluorophenyl)sulfonyl]phenyl}indolyl]imidazo[1,2-a]pyrimidin-6-carboxamide 0 N-({4-[( 3-fluoro-4-propoxybenzene)sulfonyl]phenyl}indenyl)imidazo[lj-appyridyl-6-carbamide. 5) 0 Ν-{[4-(1-benzo) Thiophen-7-sulfonyl)phenyl]fluorenyl}-111-»biszolo[3,4-b]° pyridine-5-amine Ν\j〇^ α^οσ,,. 0 N -[(4-{[3-chloro-4-(trifluoromethyl)benzene]] fluorenyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine-6-carboxamide 158436.doc 269- 201215609 A η/ N-({4-[(3,5-Dimethoxybenzene))]phenyl} fluorenyl)-1Η-pyrrolo[3,2-c]pyridine-2- Formamide OX0 CCuXr^ 0 N-({4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6 -carbamamine w N COyXT. N-({4-[(2-Ga-4-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidin-6-oxime Amine 0. 丫AN Ά COyXT'. O N-({4-[(3-Ethyl phenyl) sulfonate Mercapto]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-nonylamine\j〇0 CCy^a', N-{[4-(quinoline-3-sulfonyl) Phenyl]fluorenyl}imidazo[l,2-a]pyridine-6-nonylamine V 〇co^〇avJ N-[(4-{[3-fluoro-5-(morpholin-4-yl)) Benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]&quot;pyridyl-6-decylamine 0 F Cyj〇^〇N-[(4-{[2-(morpholine) 4--4-mercapto)phenyl]sulfonyl}phenyl)indolyl]-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 158436.doc 270· 201215609 ^_HX) Bucket [ (4-{[4-(111-imidazol-1-ylindenyl)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridin-2-ylamine οα: co^ Or N-({4-[(4-decyloxy-2,5-dimercaptophenyl)sulfonyl]phenyl]mercapto)imidazo[1,2-a].pyridyl-6- Indoleamine 0 F 0_pc° N-[(4-{[4-fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indenyl]thieno[2] ,3-c]«bipyridin-2-ylamine ten r °}^D $ &lt; N-[(4-{[3-fluoro-5-(2-mercaptopropoxy)benzene]sulfonate } phenyl) fluorenyl]-1 ίί-η 比 · 和 和 [3,2-c]» than bit 曱醯 曱醯 4 4 ύ N-({4-[(2,5-dimethoxy) Benzene sulfonyl]phenyl} fluorenyl)-1 Η-pyrrolo[3,2-c]pyridine-2-carboxamidine }~€ζ) p °&lt; H,C N-({4-[(2-say_4_mercaptophenyl)sulfonyl]phenyl} fluorenyl)thieno[2,3-c]pyridine -2-decylamine 158436.doc 271 - 201215609 0 Ν-({4-[5-(»Byrrolidin-1-yl)ηpyridin-3-sulfonyl]phenyl}indenyl)-1Η -»Bizozolo[3,4-7]°pyridin-5-carbamide I Ν-({4-[(3-stupylbenzene)sulfonyl]phenyl}fluorenyl)·1Η-. Ratio of each [3,2-c]° ratio '^-2-carbamamine secret I Ν \JP \-{[4-({4-[(didecylamino)methyl)benzene} sulfonate Mercapto)phenyl]methyl}imidazo[l,2-a]pyrimidin-6-carboxamide II 0 /:Touch _ , ί vCr N-[(4-{[3-(diethylamine A)醯))-5-fluorophenyl]sulfonyl}phenyl)indolyl]-1Η-»bido[3,2-c]indolepyridin-2-ylamine \ Γ N-[(4- {2-[Ethyl(indenyl)amino]-1,3-thiazol-5-sulfonyl}phenyl)methyl]furo[2,3_C]&quot;bipyridin-2-indole N-({4-[(5-Chloro-2-indolyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide. Each, 158436.doc 272· 201215609 α ί \ά CH3 Ν-({4-[(5-Gas-2-propoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a Pyridine-6-formamide 0 ΗΧ) 0 Ν-[(4-{[4-(1Η-imidazol-1-ylmethyl)benzene]sulfonyl}phenyl)methyl]pyrene [2] , 3-c]. Bipyridine-2-carbamide 1^0 Γ°\)\ νΡ N-({4-[(4-Ga-2-ethoxyphenyl)sulfonyl]phenyl}methyl)thiophene [2 ,3-c]pyridine-2-carboxamide. 'Λ α^οοτ', N-({4-[(3-Ga-5-methylbenzene)sulfonyl]phenyl}methyl)imidazolium [1,2-a]pyrimidine-6-nonylamine S ΗΧ) N-[(4-{[4-(2-methylpropoxy)benzene]sulfonyl}phenyl)indolyl]furan [2,3-c]pyridin-2-decylamine A v, f Η,. Η N-[(4-{[4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]-1H-indole[3,2-10 bite 2-carbamimidoxime 158436.doc 273 - 201215609 ^_HX) N-({4-[(2-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine 2-nonylamine i N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridine- 2-nonylamine ^KO x/ Ν-({4-[1-(3-phenylphenyl)-1Η-°bizozol-4-ylidene]phenyl}methyl)furan[2,3 -c] Pyridin-2-carbamamine COyJT. 0 N-[(4-{5H,6H,7H,8H,9H"4^i#[l,2-a] Aziridine-3-phenyl]methyl)methyl]-oxazolo[1, 2-nonylamine ^_K0 Ν-({4·[(3-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2- Methionine) y^&gt;&lt; N-({4-[(3-Ga-5-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo-p,2-c]pyridine- 2-nonylamine 158436.doc 274· 201215609

NJJYSvXJ〇0 N-{[4-(2-Mercapto-1,3-thiazole-4-methyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]pyridine-5- Methotrexate 〇w〇0 N-({4-[6-(4-mercaptopiperazin-1-yl)pyridine-3-n-indolyl]phenyl}methyl)-1Η-»比咯和[ 3,2-c]»bipyridine-2-carboxamide/ΚΟ p N-({4-[(4-fluoro-2,5-dimethylphenyl) hydrazino]phenyl}fluorenyl) furan And [2,3-中比pyridine-2-nonylamine K〇p °&lt; if H,C 八/ N-{[4-(2-mercapto-1,3-thiazole-4- sure Base)] thiol[2,3-c]pyridin-2-carbamide. , melon; γ\ fYs\\0^ H〆. N-({4-[(2,3-dimethoxy-5-mercaptophenyl)sulfonyl]phenyl}indolyl)-oxazolo[l,2-a]pyrimidine-6-decylamine Q, Cy m N-({4-[(2-曱 醯 醯 苯 苯)))]]]]]]]]]]]]]]]] 275 - 201215609 Ν 'Ά 0 N-[(4-{[4-(propyl-2-yl)benzene)sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidin-6-oxime Indoleamine.β 0 N-{[4-(Quinolin-8- sureinyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide. /1 ;vS rCHj N0〇yjCJ. , 0 N- {[4-( 1 -Mercapto-1H-indazole-4-sulfonyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]pyridine-5-oxime Amine &gt;co / N-({4-[(4-cyclohexylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indoleamine. \ f N\, 0 Ν-{[4-(1-propyl-1Η-°-benza-4-sulfonyl)phenyl]indenyl}imidazo[1,2-a]. Bipyridine-6-nonylamine N-({4-[(2-gas-5-fluorophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine-2 -carbamamine ^_HX) N-({4-[(2-butoxy-6-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-methyl Guanamine 158436.doc -276- 201215609

158436.doc -277- 201215609 FF-- N \A 0 _p N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[ 3,4-b]pyridine-5-formamide CCv^{ 0 Γ a; N-[(4-{[3-fluoro-4-(indolylthio)benzene]sulfonyl}phenyl) Imidazo[1,2-a]pyridine-6-carboxamide / Ν-{[4-(2,3·dihydro-1,4-benzodioxan-6-sulfonate) Phenyl]methyl}furo[2,3-c]pyridine-2-carboxamide °HX). f N-({4-[(4-butylphenyl)sulfonyl]phenyl} Mercapto) furo[2,3-c]pyridine-2-carboxamide ^KO N- {[4-(1 -indolyl-1H-indole-2-sulfonyl)phenyl]methyl} Thieno[2,3-c]pyridin-2-indoleamine, 丫s ^ 0 )sXh P w Cl N-[(4-{6-azamidazo[l,2-a]pyridine-3-sulfonate Mercapto}phenyl)indenyl]-1H-. Bisazo[3,4-b]. Bisidine-5-nonylamine

158436.doc 278- 201215609

ViO- '-4 ◎ Ν-[(4-{[3- gas-4-(1Η-pyrazol-1-yl)benzene]sulfonyl}phenyl)methyl]furo[2,3_c]. Bipyridine-2-carboxamide CCuj7^ 0 Ν-({4-[(4-phenylphenoxy)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine- 5-nonylamine H,C 〇&lt; Ν-({4·[(4_ethoxy-2-methylphenyl)sulfonyl]phenyl}fluorenyl)-1Η-° ratio[3 ,2-c]indole-2-carboxamine ¥\^γα τύ\ 0 N-{[4-(5-gas-3-methyl 0 to 0-but-2-jing S disc base) phenyl ]methyl}-1Η-carbazolo[3,4-b]n than pyridine-5-carbamimidide HX) Λ Μ〆N- {[4-( 1 ·propyl-1 Η·° ratio π sit -4·Continuously based on phenyl]fluorenyl}thieno[2,3-c]pyridine-2·carbamamine j Ν Ί (Χ\〇0^ 0 N-[(4-{[4-( Ethylamino)phenyl]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-decylamine 158436.doc 279- 201215609

158436.doc 280- 201215609

^_HX) N-[(4-{[3-(Methoxymethyl)benzene)]}phenyl)indolyl]furo[2,3-c]pyridin-2-indoleamine νώ COy ^T. 0 N-{[4-(5-decyloxy-3- sulfonyl)phenyl]methyl}imidazo[1,2-a] ° than bite-6-decylamine COyXP Ν-({ 4-[1-methyl-3-(trifluoromethyl)-1Η-pyrazole-4-sulfonyl]phenyl}indolyl]imidazo[l,2-a]»pyridin-6-A Indole CHj I^CH, v〇r. 0 N-[(4-{[4-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]»pyridin-6-decylamine N-[(4-{[2-(oxy))-5-(trimethylsulfonyl)benzene]sulfonyl}phenyl)indolyl]-1Η-°pyrho[3,2-c] 〇 啶 -2- 醯 醯 醯 醯 醯 醯 醯 醯 醯 / / / / / / - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - 2-c]Pyridin-2-carboxamide 158436.doc •28b 201215609 °κ〇. % N-[(4-{8-thiatricyclo[7.4.0.02,7]13-carbon-1 ( 13), 2,4,6,9,11-hexene-6-sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridin-2-ylamine 2~C〇, . N-({4-[(3,4-dioxabenzene)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]pyridin-2-decylamine α/αχχ) 〇n N- {[4-(phenylsulfonyl)phenyl]methyl}isoquinolin-7-formamide λλ N \iV〇CC^sX^ 0 N-[(4-{[3-fluoro-4·( 2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[Ua]pyrodo-6-carboxamide a 0 N-({4-[(2-butyl) Oxy-5-chlorophenyl)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyrimidine-6-nonylamine ryf /VS N-[(4-{[4-fluoro-3) -(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-decylamine

158436.doc 282- 201215609

158436.doc 283 - 201215609 , 0: 0 Ν-({4·[(4-butoxy-3-fluorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine- 6-Metamine / 〇y COyXr^ 0 N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine -6-decylamine °K0 ^&lt;s 0 N_ [(4- {[3-气-5-(°Bilobitone-1 -yl)benzene]) phenyl] fluorenyl] thiophene [2,3-c]pyridine-2-guanamine plant (10) N-({4-[(4- gas benzene)sulfonyl]phenyl}fluorenyl)-1H-pyrrolo[3,2-c Pyridine-2-guanamine ^HX) / N-{ [4-(6-methyl.pyrazine-2-sulfonyl)phenyl]fluorenyl}furo[2,3-c]. Bis-pyridine-2-decylamine H, 0 = 1=0 N- {[4-( 1 -mercapto-1H-indazole-4-sulfonyl)phenyl]methyl}-1,3-benzene And thiazole-6-formamide 158436.doc •284- 201215609

158436.doc -285· 201215609 }-^€ζ) HC-0 V01* Ά N-({4-[(5-Tert-butyl-2-oxooxybenzene)sulfonyl]phenyl}fluorenyl) Thieno[2,3-c]« than bite_2·carbamamine N-[(4- {[3 decapyridin-1-yl)benzene]sulfonyl}phenyl)methyl]- 1 H-indolo[3,2-c]&quot;bipyridyl-2-carboximine oxime Vcr 0 N-[(4-{[3-fluoro-4-(1Η-η-pyrazol-1-yl) Benzene]sulfonyl}phenyl)methyl]-1Η-»biszolo[3,4-b]. Bipyridine-5-nonylamine jKO / N-({4-[(2-gas-4-fluorobenzene)sulfonyl]phenyl}fluorenyl)furo[2,3-c]pyridine-2- Indoleamine C0 &lt;x\sj(r. 0 Ν-({4-[(2-13-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine- 6-decylamine CH, CH, 1 1 . TIT N-{[4-(2,6-dimethoxyacridin-3-sulfonyl)phenyl]indolyl}imidazo[1,2- a] acridine-6-formamide 158436.doc 286- 201215609 /ΚΟ N-{[4-(2H-l,3-benzodioxole-4-sulfonyl)phenyl]indole Furan[2,3-c]« than bit octadecylamine F 0 N-({4-[(2,3-difluorophenyl)sulfonyl]phenyl}indolyl)-1Η -pyrazolo[3,4-b]pyridine-5-decylamine 0〆N Ά (%ar. 0 N-[(4-{[3-(2-mercaptopropoxy)benzene]) })phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-nonylamine Q \j6.F (X^oCT 0 N-[(4- {[3-fluoro-5-(pyrrole) Pyridin-1 -yl)phenyl]sulfonyl}phenyl)indolyl]oxazolo[l,2-a]pyrimidine-6-nonylamine 0 N-({4-[(3-fluoro-4-) Propoxy phenyl) sulfonyl] phenyl] decyl) imidazo[l,2-a]pyrimidin-6-nonylamine 0 N-[(4-{[4-(4-mercaptopiperazine)- 1-yl)phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridin-2-ylamine 158436.doc 287· 201215609 ^HX) N-({4-[(3-Ethoxy-2-fluorophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]«pyridin-2- Methionine ί N-({4-[(4-butylphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indole N-{[4- (phenyl) phenyl]methyl}-3-bromo-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0: rW Cl N-[(4- {6-azamidazole And [1,2-a]. than -3-sulfonyl}phenyl) fluorenyl] carbazino[l,2-a]»pyridin-6-nonylamine JX〇aw, N-( {4-[(2,6-Dichlorophenyl)sulfonyl]phenyl}indenyl)furo[2,3-c]° pyridine-2-amidoxime 广% 〇V〇^ 0 N -{[4-({3-[(didecylamino)indolyl] phenyl)sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidin-6-decylamine ω W α N-({4-[(2-Fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6-decylamine 158436.doc - 288- 201215609

158436.doc 289· 201215609 /Η〆Ν-{ [4-(1-propyl-1 Η-pyrazole-4-sulfonyl)phenyl]fluorenyl}furo[2,3-c]pyridine- 2-decylamine 0=1 SO N- {[4-(dimercapto-1,3-thiazol-5-sulfonyl)phenyl]methyl}imidazo[1,2-a]»pyridinium -6-decylamine / /1 0 N-({4-[(2-amily-4-propoxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4 -b]pyridine-5- amidoxime) SP HC —0 N-({4-[(3-fluoro-2-indolyl)sulfonyl]phenyl}methyl)thiophene [2, 3-c]pyridin-2-decylamine ° ΓΓ° {γ\ Η //η 0 N-({4-[(4-Ga-2-nonyloxybenzene)sulfonyl]phenyl}fluorenyl Imidazo[l,2-a]pyrimidine-6-nonylamine l~C〇le, Η, / N-({4-[(2,3-dioxaoxybenzene)sulfonyl]phenyl } mercapto) thieno[2,3-c]pyridin-2-ylamine 158436.doc 290- 201215609

0 η /ΥΗ 0 N-({4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidin-6-carboxamide α Ν \/ό 0 N-({4-[(5-Gas-2-ethoxybenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidin-6-carboxamidine Amine cc^cr. N-[(4-{[2-Ga-5-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]»myrazolo[1,2-a]pyrimidine-6-carboxamidine Amine 0 N-({4-[(4-phenylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidin-6-nonylamine&gt;co male N-({ 4-[(2-Butoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-indoleamine nMX) $ C0. Ν-{[4-(2Η-1,3-benzodioxol-5-thenyl)phenyl]fluorenyl}thieno[2,3-c]indole-2-ene醯amine 158436.doc 291- 201215609 F .\j6 0 N-({4-[(2,5-Difluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4- b]pyridine-5-nonylamine^C〇P '0 Ν-[(4-{[4-(1Η-.bazol-1-yl)benzene]sulfonyl}phenyl)methyl]furan [2,3-c]pyridine-2-carboxamide NhC〇/xP Η, / N-({4-[(2,5-dimethoxybenzene)sulfonyl]phenyl}methyl)thiophene And [2,3-c]pyridin-2-decylamine N νό 0 Ν-{[4·(5-decyloxy.pyridin-3-sulfonyl)phenyl]indolyl}-1Η-» More than saliva [3,4-b] ° bite -5-carbamamine F \ / 0 COyjCT. 0 N-{[4-(5-fluoroη-pyridin-3-sulfonyl)phenyl]fluorenyl} imidazo[1,2-a] ° than pyridine-6-formamide N °%jS &lt ;xVcr 0 N-[(4-{2-[ethyl(indolyl)amino]-1,3-thiazol-5-sulfonyl}phenyl)indolyl]-1H-indazolo[3, 4-b] Pyridine-5-decylamine 292- 158436.doc 201215609

/ N-[(4-{[4-p 1 fluorenyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridin-2-indole HX) N-({ 4-[(3-Gas-2-mercaptophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide NhC〇N-({4-[( 3,5-dimercaptophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indole i N-[(4-{[4-(trifluoroanthracene) Phenyl]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridin-2-indoleamine N-CH, \\ΛΛ/ 0 N-{[4-( 2-methyl-2H-indazole-5-sulfonyl)phenyl]methyl}imidazo[l,2-a]acridin-6-nonylamine^KO / N-[(4-{[ 3-chloro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]furan[2,3-φ-pyridin-2-ylamine 158436.doc 293- 201215609 l^X) N-{[4-(2-methyl-2H-indazol-5-sulfonyl)phenyl]indolyl}thieno[2,3-c]pyridine-2-carboxamide N-{[4 -(quinoline-3·sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-decylamine, κο N-[(4-{[3-(dioxylamine) Sulfo]phenyl]sulfonyl}phenyl)indolyl]furo[2,3-c]&quot;bipyridyl-2-carboxamide J^X) / N-({4-[2-( 3-fluorophenyl)-1,3-thiazol-4-indenyl]phenyl}indolyl)thieno[2,3-c]pyridyl Amides 2-o.夂5-Hydroxy-N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)indolyl]-1H-indole-2-carboxamide ^KO N- ({4-[(2-Phenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide HX) / Ν-{[4-(1-Benzene) And thiophene-7-phenyl)phenyl]indenyl}thieno[2,3-c]pyridine-2-carboxamide 158436.doc •294· 201215609

158436.doc •295 · 201215609 Ά CO^oO^ N-({4-[(3-Ga-5-indenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]&quot Bis-pyridyl-6-decylamine, inflammatory N-[(4-{[5-fluoro-2-(p-carbyl)phenyl]sulfonyl}phenyl)methyl]-1H-pyrrolo[3 ,2-c]pyridine-2-carboxamide N-{[4-(1-methyl-1H-indazole-4-sulfonyl)phenyl]indolyl}imidazo[1,2-a] Pyridine-6-formamide α οό CO^oOr, . N-({4-[(3-Gas-2-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]»pyridin-6-carboxamide 0 N-( {4-[(3,5c Benzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-indoleamine, xf CO^oa, . ο N-{ [4-(4-Mercaptothiophene-2-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyridine-6-nonylamine F p /DO^oO5^ N -({4-[(2-Fluoro-4-methoxybenzene)-decyl]phenyl}indolyl)-1Η-. Bisazo[3,4-b]° pyridine-5-decylamine O N-{[4-(phenyl sulfenyl)phenyl]fluorenyl}furo[2,3-c]pyridine-2 -carbamamine 0 \j0 CCy^C^ N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a] Pyridine-6-decylamine COvoO^W o N-({4-[2-(3-fluorophenyl)-1,3-thiazole-4-sulfonyl]phenyl}methyl)imidazo[1 , 2-a]pyridine-6-nonylamine 158436.doc 296· 201215609 . :欢ο N-({4-[(5-fluoro-2-indolyl) stupid]] phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-醢amine CHS y» \JU CCX^oCr&quot; N-[(4-{[3-(decylaminemethanyl)benzene] cross-branched}phenyl)indolyl]imidazo[l,2-a] Pyrimidine-6-nonylamine N-{[4-(2,6-dimethoxy-bipyridin-3-sulfonyl)phenyl]methyl}-1 H-°bazolo[3,4 -b]»Bipyridin-5-decylamine / HX) N-[(4-{[4-曱-oxy-2-(trifluoromethyl)benzene]] fluorenyl}phenyl)indolyl]furan And [2,3-c]»bipyridine-2-carboxamide O N-{ [4-(pyridine-3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine- 6-decylamine N 'χτ° €θγ〇(Χ, N-({4-[(4-cyclohexylbenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine- 6-decylamine / i N-({4-[(4-butoxybenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indole Amine JKX) N-( {4-[2-(03⁄4^13⁄4-,3-13⁄4 fluorenyl)phenyl}fluorenyl)thieno[2,3-c]pyridine-2-carboxamide 3C N-( {4-[(4-Phenylphenyl)sulfonyl]phenyl}methyl)-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 158436.doc -297- 201215609 ^.CH , N-[(4- {[3-(Diethylamine)methyl)-5-fluorobenzene]sulfonyl}benzene Mercapto] imidazo[l,2-a]pyrimidine-6-amidoxime, xr coy^a, jKO &lt;, V N-{[4-(5-methoxy-pyridin-2- Sulfhydryl)phenyl]methyl}imidazo[1,2-a]pyridine-6-carboxamide N-[(4-{[3-fluoro-5-(2,2,2-trifluoroethyl) Oxy)phenyl]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridin-2-indoleamine COyO^S^ N-[(4-{[2-(2,2, 2-trifluoroethoxy)-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine-6-nonylamine N-[(4 -{[3·chloro_5_(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-'pyrolo[3,2-c]»pyridin-2-decylamine N -[(4-{[4-(4-ethoxyphenyl)benzene]sulfonyl}phenyl)indolyl]-1Η-»比比和 P,2-c]. Amine amine coMcxxx, 〇8 N-({4-[(3-phenylene)sulfonyl]phenyl}methyl)-1H-pyrazolo[3,4-b]pyridine-5-decylamine cx ^^fcrc, O N-({4-[(5-Gas-2-hydroxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide F CK , N j ND〇y^CT, N-({4-[(3-fluoro_4·methoxybenzene)sulfonyl]]phenyl}indenyl)-1Η-. Bisazo[3,4-b]»pyridin-5-decylamine. Ν-({4·[(3- -4-propyloxybenzene) continuation]phenyl}methyl) Thieno[2,3-c]. Bipyridin-2-ylamine 158436.doc -298- 201215609

Preparation, N-({4-[(4-decyloxy-2-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-indole Amine 〇CC^oO&quot;, 〆Ν-{[4-(1-methyl-1H-indazole-5-thenyl)phenyl]methyl}imidazo[1,2-a]pyrimidine-6- Methionine N-{[4-(6-decylpyridin-3-sulfonyl)phenyl]indolyl}-1pyrrolo[3,2-c]pyridine-2-carboxamide _ ο N-({4-[(2-phenoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-ylamine: &gt;&lt;〇&lt;; human, N-[(4-{[3-fail-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c ](-[{4-[(3-ethoxyphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c]pyridine-2- Methotrexate Ν-[(4-{[3-(1Η-pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c]pyridine-2 - guanamine &lt;% 〇 0 ^ ° 0 thiol] phenyl} fluorenyl) -1 Η -. Bisazo-p,4-b]pyridine-5-decylamine Mc-C, N-{[4-({H(2-mercaptopropyl)aminoindolyl]benzene}sulfonyl)phenyl Thiophene thieno P,3-c]pyridine-2-carboxamide 158436.doc -299- 201215609 • N-({4-[(4-methoxyphenyl)sulfonyl]phenyl}曱Furfuro[2,3-c]pyridine-2-carbamamine α 1 . N-[(4-{[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl)} phenyl) thiol][1,2-a]pyrimidine-6-曱co^Xr.丫0 N-({4-[(2,4-dimercaptophenyl)sulfonyl]phenyl}-&lt;\Ύ1 « ΓΤΧ° base)-1Η-pyrazolo[3,4-b Pyridine-5-formamide 0 .', j〇r0 N-({4-[6-(morpholin-4-yl).pyridin-3-sulfonyl]benzene CO^oQr, 'base} Methyl)imidazo[1,2-a]pyrimidin-6-nonylamine Q Ν-[(4-{[3·(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indolyl ]-1Η-pyrrolo[3,2-c]pyridine-2-methyly' decylamine jKO 〇1^-({4-[(4-fluoro-2,5-dimercaptophenyl)sulfonic acid] Phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N-[(4-{[2- gas-5-(trifluoromethoxy)benzene]sulfonyl-P) }笨基)曱基]-1Η-°比比和[3,2-c]° pyridine 2-nonylamine: KX) 〇N-({4-[(2-decyloxybenzene)) Sulfhydryl]phenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide HX) N-[(4-{[3-(piperidin-1-yl)benzene]sulfonate Phenyl) 2n- o fluorenyl] furo[2,3-c]pyridine-2-carboxamide

158436.doc -300- 201215609

HX) ί N-({4-[(4-Phenylphenyl)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridin-2-indole N-({4-[ (2-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carboxamide COy^O3^/ ο N-({4_[(3-B) Oxy-4·fluorobenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-amidoxime-({4-[1-(3-phenylene ratio) Oxazol-4-sulfonyl]phenyl}indolyl)thieno[2,3-c].pyridin-2-carboxamide. H,C N-({4-[(2-fluoro-4) - mercapto benzene) sulfonyl] phenyl} fluorenyl)-1 Η-pyrrolo[3,2-c]pyridin-2-meramine F cc^oo^1] N-({4-[( 2-fluoro-3-methylphenyl)sulfonyl]phenyl}indolyl]imidazo[1,2-a]pyrimidine-6-nonylamine}^C〇d N-{[4-(pyridine- 2-sulfonyl)phenyl]fluorenyl}furo[2,3-c]»pyridin-2-indole '&gt;r^&gt; \ N-({4-[(3-butoxy) Benzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine COy^O^ N-({4-[(3,4-two gas) Benzenesulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-formamide 158436.doc •301 · 201215609 N-({4-[(2,4) -dimethoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-indole N-[(4-{ [2-Fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1Η-°pyrho[3,2-c]° pyridine-2-decylamine COyOT^ 0 N-[(4-{[2-(Dimethylaminoindenyl)benzene]sulfonyl}phenyl)indolyl]0-moxazolo[1,2-a]acridin-6-oxime Amine NN(N 丫, H N-({4-[(2-Ga-5-methoxybenzene)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine -5-曱O decylamine J-CO N-{[4-(4-indolyl)pyridin-3-sulfonyl)phenyl]indole-ocyl}furo[2,3-c]pyridine- 2-nonylamine tf °HX) i N-({4-[(4-butoxy-3-fluorobenzene) hydrazino]phenyl}fluorenyl)thieno[2,3-c]pyridine- 2-Protonamine N-({4-[(3-ethylphenyl)sulfonyl]phenyl}methyl)*v7 1 furo[2,3-c]pyridine-2-carboxamide &gt; C〇,_f~i N-[(4-{[3-Fluoro-5-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-φ ratio 2-indoleamine y&lt;o 6 Ν-({4-[(3-gas-4-methoxybenzene)sulfonyl]benzene V-yl}methyl)thieno[2,3-c]pyridine -2-decylamine 158436.doc -302- 201215609

158436.doc •303 · 201215609 0 0 N-({4-[(3-Fluoro-2-decyloxybenzene)sulfonyl]phenyl}indenyl)imidazo[l,2-a]npyridinium -6-carbamamine N-[(4-{[3-( 乙 醯 ))) benzene] sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2 -carbamamine N o COyOCT, N- {[4-( 1,4-dimercapto-1H-imidazol-2-sulfonyl)phenyl]methyl}imidazo[1,2-a]pyrimidine- 6-decylamine h»c^^ch, N Ά N-[(4-{[4-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]-1H-. Bisazo[3,4-b]° pyridine-5-carbamimidoxime-C^ N \j6 CO^oO^ N-({4-[(3-decyloxyphenyl)sulfonyl]benzene Imidazo[1,2-a]pyrimidin-6-carbenamide N-({4-[(4-fluoro-3-indolyl)sulfonyl]phenyl}fluorenyl) Thieno[2,3-c]pyridin-2-ylamine^3~C〇Ν-[(4·{[5-fluoro-2-(hydroxyindenyl)benzene]sulfonyl}phenyl) Mercapto]furan[2,3-φ-pyridin-2-ylamine^-^Λη 〇:χΡ Ν-{[4-(1-mercapto-1Η-吲哚-2-continuation) benzene o 曱] fluorenyl}-1Η-pyrazolo[3,4-b]pyridin-5-decylamine HX) / N-({4-[(4- gas-2-mercaptophenyl)sulfonyl) Phenyl} fluorenyl)furo[2,3-c]pyridine-2-carboxamide^HX) \ N-({4-[(2,6-dioxa-3-methylbenzene)sulfonate Thio[2,3-c]pyridin-2-ylamine 158436.doc -304- 201215609

ο N-({4-[(2,5-Dioxaoxybenzene) hydrazino]phenyl} decyl)imidazo[l,2-a]pyrimidine-6-nonylamine N-({4 -[(3-fluorophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine}~χζ) Hj=_o μ° N-({4-[ (4-fluoro-2-indolylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine\xy〇ccy^a, N-({ 4-[2-(°Byrrolidin-1 -yl)-1,3-thiazol-5-sulfonyl]phenyl}methyl)imidazo[1,2-a]. Bipyridine-6-nonylamine% N-[(4-{[3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]furan[2,3 -c] acridine-2-carboxamide °^X&gt; N-{[4-(didecyl-1,3-thiazol-5-ytyl)phenyl]indolyl}furan[2,3 -c]pyridine-2-guanamine N \-^Ci^o^CH3 CO^OT,. O N-{[4-(6-methoxyacridin-2-sulfonyl)phenyl] fluorenyl}imidazo[1,2-a]»pyridin-6-carboxamide / N-[ (4-{[3-Fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1Η-&quot;bido[3,2-c]»pyridin-2- Amidoxime P kg, N-({4-[(2,4,6-tridecylbenzene)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine- 2-Proline 158436.doc -305 - 201215609 \j(X/ €〇^〇α, Ί ο N-({4- [6-(Trifluoromethyl)pyridin-2-sulfonyl]phenyl Xanthyl)imidazo[l,2-a]«pyridin-6-nonylamine N-({4-[(4-chloro-3-indolylbenzene)sulfonyl]phenyl}fluorenyl) Furano[2,3-c]pyridin-2-decylamine N-({4-[(3-chloro-5-mercaptophenyl)sulfonyl]phenyl}indolyl)thieno[2, 3-c]&quot;Bistidine-2-decylamine N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3, 2-c]pyridin-2-decylamine&gt; €0 N-({4-[(2-cyanobenzene)sulfonyl]phenyl}fluorenyl) \°&lt;Ρ thieno[2,3 -c]pyridin-2-decylamine, N-[(4-{[2-amino-M propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l, 2-a]pyrimidine-6-form CClyUCT, indoleamine F o J^Y^F N-[(4-{[4-(two Methyl)-3-phenylene]sulfonyl} r^v\^ F phenyl)methyl]imidazo[l,2-a]pyrimidin-6-carboxamide HX) d N- {[4- (1-Methyl-1Η-»Bizozol-4-sulfonyl)benzene%r,subunit]fluorenyl}furo[2,3-c]° pyridine-2-decylamine N \J〇 Ls N-{[4-(morphothia-4-sulfonyl)phenyl]methyl}- vJ〇^K«vA^ 1H-pyrazolo[3,4-b]pyridine-5-oxime amine

158436.doc •306· 201215609

π, 〆% °fS^l N-[(4-{[2-(didecylaminoindolyl)benzene]sulfonyl}phenyl)methyl]-oxazolo[1,2-a]pyrimidine -6-曱CQ^O^X decylamine JKX) N-({4-[(3-fluoro-5-decyloxyphenyl)sulfonyl]benzene&lt;v/yl}fluorenyl)furan[2 ,3-c]pyridine-2-carboxamide JKX) N-({4-[(4-decyloxy-2-mercaptophenyl)sulfonyl]benzene 9^- \η·yl} fluorenyl) Furano[2,3-c]pyridin-2-indenylamine Οn^AnA^j Cj N-[4-(phenylsulfonyl)phenyl]pyridine-3-carboxamide °HX) N-( {4-[(2-Mercapto-4-propoxyphenyl)sulfonyl]benzene-1-yl}decyl)thieno[2,3-c]pyridine-2-carboxamide^_HX) N-( {4-[(3-Ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide N-{[4-(benzene Phenyl] phenyl]fluorenyl}-1Η-imidazo[4,5-c]pyridin-2-decylamine &amp; N-[(4-{[2,4-bis(trifluoromethyl)) Benzene]sulfonyl}benzene&gt;-coyl]mercapto]thieno[2,3-c]pyridin-2-indole N-{[4-(6-decylnaphthalene-2-sulfonate) Phenyl]fluorenyl}thieno[2,3-c]pyridine-2-carboxamide N-{[4-(phenylindolyl)phenyl]methyl}-3-(acridine- / \h iTV^〆4-base)-1Η-pyrazole-5-nonylamine 158436.doc •307- 201215609 ^_l vX^N 、, N-({4-[(2-Ethylphenyl)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridine-2-carboxamide 0 \\/ cH&gt; N \ home. &lt;χγχτ. N-({4-[(4-甲烧烧 Benzene) sulfonyl]phenyl} fluorenyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine jHX) N -{[4-(4-methylacridin-2-sulfonyl)phenyl]decyl}furo[2,3-c]pyridin-2-ylamine F CC^oO3^ N-({ 4-[(3-fluoro-4-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-[(4-{[3 -Fluoro-4-(trifluorodecyloxy)benzene]sulfonyl}phenyl)methyl]-1Η-»pyrolo[3,2-c]° pyridine-2-decylamine y-0 N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide N- [(4-{[2-(Trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-ylamine c CO^oO5^ N- ({4-[(4-Ethoxy-2-methylphenyl) hydrazino]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide z_HX). N-({4-[(6-chloro-2-fluoro-3-indolylbenzene) hydrazino]phenyl}methyl)furo[2,3-c]pyridin-2-ylamine 158436 .doc .308 · 201215609 &lt;3〇ν〇α,,. ο Ν-({4-[(5-Chloro-2-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6-carbamimid\X} o N -{[4-(furan-2-sulfonyl)phenyl]methyl}imidazo[1,2-a]-pyridin-6-nonylamine N-({4-[(2,6-) Dimethoxy-4-methylbenzene)sulfonium μ&gt;yl]phenyl}fluorenyl)furo[2,3-c]. Bis-2-carbamide N-({4-[(2-phenylethyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-methyl Indoleamine N-({4-[(4-fluoro-3-methylphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c]pyridin-2-decylamine N- { [4-(1-Methyl-1H-indazole-4-sulfonyl)benzene.Pyl]fluorenyl}-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide ^KO N -[(4-{[3-Fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c]. Bipyridine-2-carbamide N xJOO oo^a,,. u O N- {[4-(1 -Methyl-1H-indazole-6-sulfonyl)phenyl]indenyl}-1Η-. Bisazo[3,4-b]»pyridin-5-carboxamide^KXs N-[(4-{[4-(transyl)phenyl)sulfonyl}phenyl) fluorenyl] Thieno[2,3-c]pyridine-2-carboxamide N-({4-[6-(3,4-difluorophenyl)acridin-2-yl)phenyl}indenyl) Furano[2,3-c]&quot;bipyridin-2-yl,^ύ guanamine 158436.doc -309· 201215609 Q N-({4-[(3-methylphenyl)sulfonyl)phenyl }曱基)- 4. 1H-pyrrolo[3,2-c]pyridine-2-carboxamide F N-({4-[(3-fluoro·5-methylphenyl)sulfonyl]phenyl } COy^O^ 曱 ))Imidazo[1,2-a]pyridine-6-carboxamide nickname N-({4-[(3,5-dioxaoxybenzene)sulfonyl]phenyl } COyoQn, fluorenyl) imidazo[l,2-a]pyrimidin-6-nonylamine 9r° N-[(4- {[3-(morpholin-4-yl)benzene]sulfonyl) ) methyl]-1,3-benzothiazol-6-carbamamine &lt;jaDr^* N-({4-[(3-ethoxyphenyl)nonyl]phenyl}fluorenyl)- 1Η-pyrrolo[3,2-c]pyridin-2-decylamine N-({4-[(3-chloro-5-decyloxybenzene)sulfonyl]phenyl}methyl)-1Η- °Prequent p,2-c]pyridin-2-carboxamide decylamine N-({4-[(4-Ga-2-methylphenyl)sulfonyl]phenyl}methyl)- 1Η-. Bis-[3,2-c]&quot;bipyridin-2-indole^_HX) j N-{[4-({4-[(°-pyrrolidin-1-yl)carbonyl)benzene) Mercapto)phenyl]fluorenyl}furo[2,3_decabiidine_2_nonylamine N-[(4-{[3-(decyloxyindenyl)benzene]sulfonyl}benzene). , 0 base) fluorenyl]-1H-indolo[3,2-c]° pyridine-2- 2 decylamine

158436.doc .310- 201215609 N-{[4-(l-Methyl-1H-carbazol-7-sulfonyl)phenyl]indolyl}-1Η-&quot;比比和[3,2-c ]. Bis-pyridine-2-carbamimidoxime-[(4-{[3-(1Η-oxazol-1-yl)]]]]]]]]]]]]]]]]] 2-c] ° pyridine-2-decylamine N- {[4-(1-indolyl-1H-indazol-5-sulfonyl)phenyl]indolyl}-1Η-.咯和和[3,2-中比pyridine-2-曱J decylamine f N-({4-[(4-cyanobenzo)sulfonyl]phenyl}indolyl)-1H-pyrrolo[3 , 2-c]pyridine-2-carbamide p N-{[4-(2,3-dihydro-1-benzofuran-7-sulfonyl)phenyl]indolyl}-1Η-. Bis-[3,2-φ-pyridyl-2-carboxamide, p Ν-({4-[(2-cyanophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3 ,2-c]pyridin-2-decylamine A 5-N-({4-[(3,5-difluorobenzene)sulfonyl]phenyl}indolyl)pyridine-2,5-diguanamine~ /0, double ~ cCyjO^ N-({4-[(4-gas-3-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine-6-oxime Amine O./. 〇/〇N-{[4-(phenylsulfonyl)phenyl]fluorenyl}-1,6-bite-2_decylamine 158436.doc -311 - 201215609 CH. CH, ', public &lt; X\〇CP 0 N-({4-[(4-decyloxy-3-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]. Bipyridine-6-formamide VcH·COyjCT N-({4-[(4-methylsulfonylbenzene)sulfonyl]phenyl}hydrazino)imidazo[l,2-a]° pyridine -6-decylamine N \j© N-({4-[(2-cyanobenzene)sulfonyl]phenyl}methyl)-1H-pyrazolo[3,4-b]pyridine-5 - indoleamine N Ά &lt;Χ^Χγ. N-({4-[(3-曱oxy-4-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-&lt;·Bizozolo[3,4-b]acridine-5 -曱醯amine's ❹ N-[(4- {[3-fluoro-4-(1 H-pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2 -a]pyridine-6-nonylamine\麻&gt;&lt;τ〇ν〇σ&quot; 0 Ν-{[4-(2Η-1,3-benzodioxol-5-sulfonyl) Phenyl]fluorenyl}imidazo[l,2-a]&quot;pyridin-6-nonylamine N. ,: 10 OOyXH 0 N-({4-[(2-chlorophenyl)sulfonyl)phenyl}methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide N DOC : &lt;Χ\ο〇π 5 N-({4-[(4-fluoro-2,5-dimercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-carbazolo[3,4 -b]»Bipyridin-5-nonylamine N &lt;X^〇r "O N-({4-[(2,5-dimercaptophenyl)sulfonyl]phenyl}fluorenyl)-1Η -pyrazolo[3,4-b]pyridine-5-decylamine COyXT. N-({4-[(5-fluoro-2-indolylbenzene)sulfonyl]phenyl}indolyl)imidazolium [1,2-a]»Bipyridine-6-nonylamine 158436.doc -312- 201215609 N 0-F-[(4-{[2-(trifluoromethyl)benzene]sulfonyl}phenyl Mercapto]imidazo[1,2-a]pyrodo-6-nonylamine &lt;Χ\〇0^ N-({4-[(2-ethylhydrazino)sulfonyl]] Methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine CCyjO5^ N-[(4-{[2-mercapto-4-(trifluoromethyl)benzene]sulfonate }}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridine-5-decylamine Γ 0 N-({4-[(2-fluoro-6-methoxybenzene)sulfonate Mercapto]phenyl}methyl)imidazo[l,2-appyridyl-6-carboxamide: 3⁄4 N-{[4-(quinolin-8-sulfonyl)phenyl]methyl}imidazole And [l,2-a]pyridine-6-nonylamine r-FF N-[(4-{[4-chloro-2-(trifluoromethyl)benzene]sulfonate } phenyl)indenyl]-1H-.Bizozolo[3,4-b]acridin-5-formamide N _νφ N-({4-[(2,5-dimethoxybenzene)sulfonate Mercapto]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-nonylamine 吟〇0^ 0 N-({4-[(4-fluoro_2·曱Oxygen) Benzene)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]acridin-5-decylamine CO COyjCP N-({4-[(2-ethoxybenzene) Sulfo]phenyl]indolyl)imidazo[1,2-a]pyridin-6-nonylamine vi cCyjCT. N-[(4-{[3-(trifluoromethyl)benzene]sulfonate }}phenyl) fluorenyl]imidazo[l,2-a]pyrodo-6-nonylamine 158436.doc -313- 201215609 N-[(4-{8-oxatricyclo[7.4.0.02' 7]Tride-1(13),2,4,6,9,11-hexene-6-sulfonyl}phenyl)indenyl]-1H-pyrazolo[3,4-b]pyridine -5-Protonamine 6-Amino-N-({4-[(3,5-difluorobenzene)sulfonyl]]phenyl}pyridyl)pyridine-3-carboxamide Γ 〇 v〇C[ &lt;χ\〇σ, N-({4-[(3-chloro-4-propoxybenzene)sulfonyl]phenyl}fluorenyl)-1Η-pyrazolo[3,4-b]pyridine -5-methalin Γ Ν xjCt ^OyjCr^ N-[(4-{[4-methoxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)indenyl]-1Η-° Bisazo[3,4-b]° pyridine-5-nonylamine, Ν ά COyjO^ N-({4-[(4- -3-decyloxybenzene)sulfonyl]phenyl}methyl)-1Η-°Bizozolo[3,4-b]»pyridin-5-amidoxime rW N-({4-[ (4-methoxy-2-mercaptophenyl)sulfonyl]benzoquinone nDCvXP 0 yl}methyl)-1 Η-pyrazolo[3,4-b]pyridine-5-decylamine COyja, 'N -({4-[(3-ethylbenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-carboxamide 'V CC^oCr ο N-({4 -[(4-Ethyl)sulfonyl]phenyl}indenyl]imidazo[l,2-a]pyridine-6-carboxamide. , is COyXT^ N-[(4-{[4-chloro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]»pyridinyl- 6-carbamide 158436.doc -314· 201215609

N \JCT is 〇0^ O N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H--pyrazolo[3, 4-b]. Bipyridine-5-carbamamine N-[(4-{[3-(cyclopentylamino)phenyl)sulfonyl}phenyl)methyl]-1H--pyrazole[3,4 -b]. F-pyridine-5-nonylamine F [(4-{[4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolop,4-b]pyridine- 5-nonylamine N-[(4-{[2-(morphin-4-ylindenyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyridine-6- Indole ο N-({4-[(2-ethylphenyl)sulfonyl)phenyl}indolyl)-1H-pyrazolo[3,4-b]pyridine-5-decylamine H3c CH , coyor. N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a] ° pyridine-6-nonylamine CH, H , C~CM, \j0 C〇yj〇nX N-({4_[(5-Tert-butyl-2-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2- a] Pyridine-6-guanamine. , summer CCVf 0 N-({4-[(4-indolyl))sulfonyl]phenyl}indolyl) imidazo[1,2-a]pyrodo-6-amidoxime να &lt;3 〇VKj〇r&quot; 0 N-({4-[(3,4-Dioxaoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyro-6- formazan Amine N.夏^〇y〇0^ 0 N-({4_[(2-fluoro_4_methylbenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]° than pyridine-6- Indoleamine 158436.doc .315. 201215609 N-{[4-(Phenylthio-4-sulfonyl)phenyl]indolyl}Mine 0 sits and [l,2-a]0 is determined to be -6- Brewing amine N-({4-[(2-mercaptophenyl)sulfonyl]phenyl}indolyl) imidazo[1,2-a]pyro-6-carboxamide N \j© CCy j 〇t', N-({4-[(2-phenoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridin-6-nonylamine N 'IT0 &lt; Xiyja^ N-[(4-{[4-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridine-5-oxime Amidoxime-CH· CCy^CP N-({4-[(2-fluoro-3-indolylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6 - indoleamine r rW ^OyjO^ N-({4-[(4-methoxy-2,5-dimercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-carbazolo[3 ,4-b]°-pyridine-5-nonylamine „ ci &quot;DOy^O^ N-[(4-{[2-chloro-3-(trifluoromethyl)benzene]sulfonyl} phenyl曱]]-1H-pyrazolo[3,4-b]pyridine-5-decylamine N \X}, &lt;χ\〇σ,,. 0 N- {[4-( 1 -methyl) -1Η-»Bizozol-4-sulfonyl)phenyl]fluorenyl}-1Η-carbazolo[3,4-b].pyridin-5-decylamine N-({4-[(3-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine Hta : COyXr, ,. N-({4-[(4,5-Difluoro-2-indolyl)sulfonyl]phenyl}indenyl)imidazo[1,2-a]»pyridinyl- 6-decylamine 158436.doc •316· 201215609 CH. CH, 1 ^ i N-({4-[(2,4-Dioxaoxybenzene)sulfonyl]phenyl} €C\cCP 0 曱Imidazo[l,2-a]«pyridin-6-nonylamine'»F coyjcr. N-({4-[(2,4-difluorophenyl)sulfonyl]phenyl}methyl Imidazo[1,2-a]pyridine-6-nonylamine CH, NO N-{ [4-(5-methylthiophen-2-sulfonyl)phenyl]methyl}-111-pyrazole And [3,4-b]pyridine-5-decylamine OH N \XXF t〇V〇CT, O N-[(4-{[5-fluoro-2-(radiomethyl)benzene]sulfonate Phenyl) fluorenyl]-1H-pyrazolo[3,4-b]acridin-5-carbamimid N-[(4-{[4-(ethylaminoindenyl)benzene]sulfonate醯)}phenyl)methylHH-pyrazolo[3,4-b]pyridine-5-nonylamine CH, CM, 丄AK \J0C &lt;X^〇C〇' 0 N-({4- [(4-decyloxy-3,5-dimethylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 1 \· 1 V N-[(4-{[3-Fluoro-5-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indole Base]-1Η-»Bizozolo[3,4-b]. Bipyridin-5-nonylamine N-({4-[(3-propoxyphenyl)sulfonyl]phenyl} fluorenyl-1 -pyrazolo[3,4-b]pyridine-5- Formamide N. This &lt;X^XT "O N-({4-[(2,4,5-tridecylbenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b] Pyridine-5-decylamine 158436.doc -317- 201215609 Γ 0 J^T N-({4-[(2-Ga-4-methoxybenzene)sulfonyl]phenyl}indenyl)-1Η -pyrazolo[3,4-b]pyridine-5-carboxamide CH, 0-CH-.';0 〇0^ N-({4-[(2,3,6-trimethoxybenzene) Sulfhydryl]phenyl}methyl)-1Η-°biazolo[3,4-b]»pyridin-5-nonylamine N-[(4_{[2- gas_4_(trifluoroanthracene) Phenyl]sulfonyl}phenyl)indolyl]-1Η-»biazolo[3,4-b]»pyridin-5-nonylamine N-({4-[(3-fluoro-2) -mercaptophenyl)sulfonyl]phenyl} fluorenyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide CQyjO^ N-({4-[(3-mercaptobenzene) Sulfhydryl]phenyl}indolyl) M. 0 sits and [l,2-a]0 is more than bite-6-carbamate @coy^a, N-[(4-{[2-methoxy -4-(1Η-pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyridine-6-nonylamine 〇丫ch&gt; COyjO^, N- ({4-[(5-Ethyl-2-yloxybenzene)sulfonyl]phenyl}indolyl)-oxazolo[1,2-a]»pyridin-6-carboxamide H&gt;c&gt;^ra N MOOyf. N-({4-[(4-chloro-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrazole [3,4-b]pyridine-5-formamide N \X)^ O^oCP N-[(4-{[3- gas-4-(trifluoromethyl)benzene]sulfonyl} phenyl )曱基]-lH"Bizozolo[3,4-b]&quot;Bipyridin-5-carbamamine... NC〇yU〇^ 10 N-({4-[(2-phenoxybenzene)sulfonate Mercapto]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 158436.doc •318- 201215609

Ν-({4-[(4-Chlorophenyl)sulfonyl]phenyl}indolyl)-1H-pyrazolo[3,4-b]pyridine-5-carbamimid 吟〇0\α. 0 N-[(4-{[4·Fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indenyl]-1H-. Bisazo[3,4-b] ° ratio 5--5-carbamamine Ν \Χϊ/ 0 Ν-[(4-{[4-1-3-(trifluoromethyl)benzene]sulfonyl} Phenyl) indenyl]-1 Η-pyrazolo[3,4-b]pyridine-5-decylamine. The present &lt;Χ\〇〇τ " 0 N-({4-[(2,4,5-tridecyl) sulfonyl]phenyl} fluorenyl)imidazo[1,2-a]pyridine- 6-decylamine, 矣N-({4-[(2,3-ditr6-methoxyphenyl)sulfonyl]phenyl}indenyl)-1Η-pyrrolo[3,2-c]pyridine -2-carbamamine\麟CC^oOn. 0 N- {[4-(quinoline-6-jinginyl)phenyl]fluorenyl}imidazo[l,2-a]pyridine-6-oxime Amine νί ccyjcr [(4-{[3_(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[Ua]pyridine-6-nonylamine &lt;Χ\〇0^ 0 N-({4-[(2-Methoxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carbamimidoxime »F €〇 〇〇ττ,,. 0 N-({4-[(4-fluoro-2-indolylbenzene)sulfonyl]phenyl}indenyl)-1Η-pyrazolo[3,4-b]pyridine -5-methalin Ν ^Cyj〇r^¥ N-[(4-{[2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-carbazole [3,4-b]&quot;Bistidine-5-carbamide 158436.doc -319- 201215609 F CH, COyjCT 0 N-({4-[(3-Ga-4-methoxybenzene)) Imidazo[1,2-a]»pyridin-6-carboxamide (OyjCT N-({4-[(2,3-dimethylphenyl)sulfonyl)benzene) Methyl imidazo[l,2-a]pyridine-6-amidoxime N N-({4-[(2-methoxy-5-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-formamidine Amine Cl N \jilj 0 N-[(4-{[3-chloro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1Η-&quot;Bizozolo[3,4 -b]«Bistidine-5-decylamine COyjO^ N-({4-[(4-Ga-3-fluorophenyl))indolyl]phenyl}indolyl)imidazo[1,2-a] Pyridine-6-nonylamine\ into tOyjQr, N-({4-[(3,5-dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]. -6-Amidoxime N-[(4-{[4-(2-methylpropoxy)benzene]sulfonyl}phenyl)indolyl]-1H--pyrazolo[3,4-7 ° ° pyridine-5-formamide ac〇Vr^&quot; O N-({4-[(3- benzene)sulfonyl]phenyl} fluorenyl)比-6-carbamamine r.» COyXn N-({4-[(2-fluoro-4-indolyl)sulfonyl]phenyl}methyl)imidazo[l,2- a] acridine-6-formamide 158436.doc •320· 201215609

0,a N-({4-[(2,4-dioxa-3-methoxybenzene)sulfonyl]phenyl}indenyl)-1Η-°biazo[3,4-b]吼Acridine-5-amidoxime CO O N-({4-[(2-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamidine Amine CCyOT. N-[(4-{[3-Fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]-lH-η-pyrazolo[3,4 -b] Pyridine-5-nonylamine N Da €〇ν〇σ,,. 0 N-({4-[(5-Chloro-2-indolyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine CHS 0〆% 'A COyXP N-({4-[(2,3-Dioxaoxybenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a] η than pyridine-6-曱Amidoxime.身-({4-[(4-methoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]° pyridine-6-decylamine 0 N-( {4-[(2-Butoxy-4-fluorophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide νφ CCy^aC ^ N-({4-[(2,5-Dioxaoxybenzene)sulfonyl]phenyl}indenyl)imidazo[1,2-a]pyridine-6-carboxamide a 〇0^ 0 N-({4-[(3,5-dichlorobenzene)sulfonyl]phenyl}indenyl) imiline 0 and [l,2-a]° ratio bite-6-carbamide 158436.doc •321 - 201215609 COyf N-({4-[(3-methoxyphenyl)sulfonyl]phenyl}indolyl) tastes sit and [l,2-a]0 than bite-6-nonylamine ^OyjCT' N- {[4-( 1 -Mercapto-1H-indazol-5 - decyl)phenyl]indolyl}-1Η-&quot;Bizozolo[3,4-b]acridine- 5-decylamine a HC 丄N 06 &quot;DOyjCP N-({4-[(3-Ga-2-ylphenyl)sulfonyl]phenyl} fluorenyl)-1Η-pyrazolo[3, 4-b]pyridine-5-carbamide FN \;6υ &lt;χ\〇σΊ N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl) Mercapto]-1H-pyrazolo[3,4-b]pyridine-5-decylamine F \j6 COyjCP N-({4-[(3-fluorophenyl)sulfonyl]phenyl}fluorenyl)咪0 sits and [1,24]° bites -6-carbamamine / H \J〇^ CCy^a', N-[(4-{[4-(ethoxymethyl)benzene]] fluorenyl}phenyl)methyl]-1Η-»biszolo[3,4-b]° pyridine-5- Brewed amine Q^oCT. Ν·({4-[(4-Phenylbutane))]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine N ':xr N- ({4-[(2-Gas_4_mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide N nD〇VUT ,. 0 N-({4-[(4-cyanobenzene)sulfonyl]phenyl}methyl)-111-0 ratio °[3,4-1)]° than bite-5-carbamide 158436.doc -322- 201215609

NH, 0 = 8=0 N-({4-[(3-Aminosulfonylbenzene)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5- Amidoxime 0^003^ 0 N-[(4-{[2-(¥oxy)-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1Η-» ratio Zizo[3,4-b]-pyridin-5-formamide 0 N-{[4-(naphthalene-1-ylidene)phenyl]indolyl}-1Η-. Bisazo[3,4-b]pyridine-5-carbamimid 00 HN-^ 〇K^ 0 N-{[4-(phenyl fluorenyl)phenyl]fluorenyl}-1Η-. Bisucci[3,2-c]pyridine-3-carboximine Ν-{[4-(1-indolyl-1H-indol-7-thenyl)phenyl]indolyl}-1Η-. Bisazo[3,4-b]»pyridin-5-indoleamine N "Happiness &lt;i\〇cr. 0 N-({4-[(5-fluoro-2-indolyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine N &&lt;xV/r. 0 Ν-{[4-(2Η-1,3-benzodioxan-4-yl) phenyl]fluorenyl}-1Η-. Bisazo-p,4-b]»pyridin-5-nonylamine a 0 N-({4-[(5-chloro-2-propoxybenzene)sulfonyl]phenyl}indolyl)- 1Η-pyrazolo[3,4-b]pyridine-5-formamide N \J〇lf 0 N-({4-[(3-fluoro-2-decyloxybenzene)sulfonyl]phenyl }曱基)-1Η-°Bizozolo[3,4-b]«pyridin-5-nonylamine N \^〇L. , &lt;XVJ〇r,, 0 N-({4-[(2-fluoro-5-decyloxybenzene))]phenyl}methyl)-1Η-pyrazolo[3,4-b Pyridine-5-decylamine 158436.doc • 323 · 201215609 N-({4-[(4-butoxy-2-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazole And [3,4-b]pyridine-5-formamide N-[(4-{[4-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2 -a]pyridine-6-nonylamine CH, O-TM· «A N-({4-[(2,3-dimethoxybenzene)sulfonyl]phenyl] fluorenyl)-1Η-pyridyl Zoxa[3,4-b]pyridine-5-carbamimid cCyO)3^ N-({4-[(3-fluoro-4-propoxybenzene)sulfonyl]phenyl}indolyl)- 1Η-pyrazolo[3,4-b]pyridine-5-nonylamine N \JD Nt〇yJ〇^l' O N-[(4-{P-(indolyl)] continued Mercapto}phenyl)indolyl]-1Η-pyrazolo[3,4-b]pyridine-5-decylamine N-[(4-{[2-methoxy-5-(prop-2-) Benzene]sulfonyl}phenyl)methyl]-1Η-»bisazolo[3,4-b]»pyridin-5-decylamine N-[(4-{[2-methyl- 4-(1Η-pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine-6-decylamine CCyjCT N-[(4-{[2 -Fluoro-4-(1Η-°Bizozol-1-yl)benzene]sulfonyl}phenyl)indenyl]&quot;Mizozolo[1,2_a]bite-6-甲醯Amine N C© N-({4-[(2-mercaptophenyl)sulfonyl]phenyl}indenyl)-1Η-° ratio. Sit and [3,4-7]° bite-5-nonylamine^X^oO5^ N-({4_[(6-Gas_2-fluoro-3-methylphenyl)sulfonyl]phenyl} Mercapto)-1Η-pyrazolo[3,4-b]pyridine-5-indoleamine 158436.doc -324- 201215609

OX N-{[4-({4-Fluoro-3-[(propan-2-yl))aminomethyl]phenyl}sulfonyl)phenyl]indenyl}-1Η-. Bisazo[3,4-1)]0 ratio °-5-formamide N-({4-[(4-butylphenyl)sulfonyl]phenyl}fluorenyl)-1 ratio °Sit and [3,4-13]° than bite-5-decylamine 0 N-({4-[(2-ethylphenyl)sulfonyl)phenyl}indolyl) imidazo[1,2 -a] ° pyridine-6-formamide DTHS c〇V〇r O N-({4-[(2,4-dimercaptophenyl)sulfonyl]phenyl}indolyl) imidazo[1 , 2-a]pyridine-6-nonylamine is called 〇0^. , N-[(4-{[3-(indolyl) sulfonyl}phenyl)methyl]-1Η-»biszolo[3,4-bppyridin-5-oxime Amine '4 &lt;^〇〇r " O N-({4-[(2,5-dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6 -nonylamine Cl 吟〇0^ 0 N-[(4-{ [5-chloro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]-1H-. Azolo[3,4-b]° pyridine-5-carbamide a C〇V〇D^ O N-({4-[(2-butoxy-5-gasbenzene))]benzene曱 曱))-1Η-°Bizozolo[3,4-b]»pyridin-5-decylamine (OyXrK N-({4_[(4_Chloro-2-yloxybenzene)) (phenyl)methyl)imidazo[l,2-a]° pyridine-6-nonylamine 158436.doc -325- 201215609 \ N-({4-[(3-butoxybenzene) sulfonate Indenyl]phenyl}indenyl)-1Η-η-pyrazolo[3,4-b]°pyridin-5-decylamine 0 丫\j6 N-({4-[(3-ethylhydrazinobenzene) Sulfo]phenyl]indolyl]imidazo[l,2-a]pyridin-6-nonylamine^KO N-({4-[(3-phenylpropenyl)sulfonyl]phenyl }曱基)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide CCyOr^ N-({4-[(4-butoxybenzene)sulfonyl]phenyl}fluorenyl) -1Η-° ratio °[3,4-b]a ratio °-5-bristled amine N said &lt;χ^〇σ “ 0 N-({4-[(2,6- Dimercaptophenyl)sulfonyl]phenyl}indolyl)-1 H-°-pyrazolo[3,4-b] °pyridin-5-carboxamide c〇v^a (5 N-({ 4-[(2-Chloro-6-nonyloxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a].pyridyl-6-carbamide\XT COyO)^ N- ({4-[(4-Fluoro-2-methoxybenzene)-indolyl]phenyl}methyl)imidazo[1,2-a].pyridyl-6-carboxamide% \ N-[ (4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indenyl]-1H-.Bizozolo[3,4-b] Pyridine-5-methionine Γ \^ϋΐε, COyjCP 0 N-({4-[(2-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2 -a] acridine-6-nonylamine 158436.doc -326- 201215609

★ 0 N-({4-[(3-fluoro-4-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6-nonylamine C〇V〇 〇^ 0 N-({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}indolyl) azo 0 sits and [l,2-a]0 is more than bite-6-nonylamine xJ〇^F N-[(4-{[2_methoxy_4_(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]° pyridine- 6-decylamine 0 N-({4-[(2-chlorophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridin-6-nonylamine N \J〇L &lt;χ^〇σΆ O N-({4-[(3-Cyanobenzo)sulfonyl]phenyl}indolyl)-1H-pyrazolo[3,4-b]pyridin-5-曱Indoleamine N &lt;χ\〇σ" N-({4-[(2,4,6-trimethylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4- b]pyridine-5-carbamamine F+ N \j^ N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}}]yl]methyl]-1H- Bisazo[3,4-b]»pyridin-5-decylamine oa tlDyjCP 0 N-({4-[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}fluorene Imidazo[l,2-a]nt bite-6-nonylamine &lt;xAo^j6 N-(4-(3-(trifluoromethoxy)phenylsulfonyl)benzyl)-1Η -pyrazolo[3,4-b]pyridine-5-decylamine &lt;χ/αχό N-(4-(3-(trifluoromethyl)phenylsulfonyl)benzyl)-1Η-° 0 sit and [3,4-b]° bite-5-decylamine 158436.doc .327· 201215609 0 FH 〇2 N-(4-(3,5-difluorophenyl fluorenyl)benzyl -1,8a-dihydroimidazo[l,2-a]pyridin-6-decylamine (X^XlP 〇/N〇7,8-dihydro-5H-pyrido[3,4-b] Pyrazin-6-decanoic acid 4-phenylphenanthryl-benzyl decylamine cox«^asP /, 0 3,4-dihydro-1 H-[2,6] acridine-2-decanoic acid 4- Benzenesulfonyl-benzyl decylamine CO^XlP /, 0 3,4-dihydro-1 Η-[2,7] acridine-2-decanoic acid 4-benzoindolinyl-benzyl decylamine 1 αχΡ /', 〇6,7-dihydro-4H-isoxazo[4,3-c]pyridine-5-decanoic acid 4-phenylsulfonyl-benzyl decylamine C〇X«XisP /, 0 5,8-Dihydro-6H-[1,7]acridine-7-carboxylic acid 4-phenyl decyl-benzyl decylamine 0 /',. 6,7-dihydro-4H-isoxazole [4,5-c]pyridine-5-decanoic acid 4-phenylsulfonyl-benzyl decylamine fpx〇asP N=/ 〇//S^〇1,3-dihydro-pyrrolo[3,4- Pyridine-2-decanoic acid 4-phenylsulfonyl-benzyl amidoxime, 0 imidazo[1,2-a]«pyrazine-6-carboxylic acid 4-phenylsulfonyl-benzylamine Co^XiP /, 〇imidazo[l,5-a]pyridine-6-carboxylic acid 4-phenylsulfonyl-benzyl decylamine

158436.doc • 328- 201215609 co^oaP 1H-pyrazolo[3,4-c]pyridine-5-carboxylic acid 4-phenylsulfonyl-benzylguanamine CO^XL/ FF imidazo[1,2- a] Pyridin-7-decanoic acid 4-(3,5-difluoro-benzenesulfonyl)-benzylguanamine H /, '〇1H-pyrazolo[4,3-b]pyridine-5-oxime 4-Benzenesulfonyl-benzyl decylamine furo[3,2-b]pyridine-2-carboxylic acid 4-phenylsulfonyl-benzyl decylamine cP^AP O N-{[4-(benzenesulfonate) Mercapto)phenyl]methyl}thieno[3,2-b]pyridine-2-carboxamide q. C〇yXr"N-{[4-(phenylsulfonyl)phenyl]indolyl}imidazo[l,5-a]0 is more than -6-anthracene amine W VIII N-{[5-(benzene Performance basis). Bipyridin-2-yl]methyl}-1Η-pyrrolo[3,2-c]pyridin-2-decylamine CCVjO^ O N-{[4-(benzophenanthyl)phenyl] fluorenyl} Imidazo[l,2-a]pyrazine-6-nonylamine cP^AP o N-{ [4-(phenylphenyl)phenyl]fluorenyl}furo[3,2-b]pyridine- 2-nonylamine 158436.doc -329- 201215609 \=/ Eight N-{[6-([ 笨 吼 吼 吼 吼 吼 -3- -3- -3- -3- -3- } } } } } } } } } } } 比 比 比 比 比 比 比 比 比 比 比 比 比-c]° than 2-acetamide N-{[4-(piperazin-1-sulfonyl)phenyl]methyl}thieno[2,3-c]° pyridine-2-indole N-{[4-(piperazin-1-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyridine-6-decylamine πα N-{[4-( 3-Amino.pyrrolidin-1-sulfonyl)phenyl]indenyl}thieno[2,3-c]pyridin-2-indole hydrochloride HCI. N-{[4-(3-Amino.pyrrolidin-1-sulfonyl)phenyl]indolyl}furo[2,3-c]acridin-2-indanamine hydrochloride 0 F Examples of N-({4-[(3,5-difluorobenzene)sulfinyl]phenyl}indenyl)imidazo[l,2-a]pyridin-6-nonylamine are as follows Illustrative, non-limiting examples of the examples. The invention is further illustrated by the following examples, which are not to be construed as limiting the scope or spirit of the invention. Those skilled in the art will recognize that the starting materials can be varied and additional procedures can be used to prepare the compounds encompassed by the present invention, as illustrated by the following examples. In some cases, it may be necessary to protect certain reactive functional groups in order to achieve some of the above transformations. In general, those skilled in the art of organic synthesis -330-158436.doc 201215609 should be aware of such requirements for protecting groups, as well as the conditions necessary to attach and remove such groups.

The compounds of the present invention can be synthesized by synthetic routes including those analogous to those well known in the chemical arts, especially in view of the description contained herein, and the methods described in the following references for other heterocycles: Comprehensive Heterocyclic Chemistry II, Edited by Katritzky and Rees, Elsevier, 1997, eg Volume 3; Liebigs Annalen der Chemie, (9): 1910-16, (1985); Helvetica Chimica Acta, 41: 1052-60, (1958); Arzneimittel-Forschung, 40(12): 1328-31, (1990), each of which is expressly incorporated herein by reference. The starting materials are typically obtained from commercial sources (such as Aldrich Chemicals (Milwaukee, WI)) or can be readily prepared by methods well known to those skilled in the art (e.g., by Louis F. Fieser and Mary Fieser, Reagents for Organic Synthesis, Volumes 1-23, Wiley, NY (1967-2006) or Beilsteins Handbuch der organischen Chemie, 4, Aufl. ed. Springer-Verlag, Berlin (including supplements) generally described (also via Beilstein online data) Prepared by the method of the library). Synthetic chemical transformation and protecting group methods (protection and protecting group removal) useful for the synthesis of the compounds of the invention and the necessary reagents and intermediates are known in the art and include, for example, those described in the following literature: R. Larock, Comprehensive Organic Transformations, VCH Publishers (1989); TW Greene and P. G. M. Wuts, Protective Groups in Organic Synthesis, 3rd edition, John Wiley and Sons (1999); and L. Paquette, Encyclopedia of Reagents for Organic 158436.doc -331- 201215609

Synthesis, John Wiley and Sons (1995) and subsequent versions. The compounds of the invention may be prepared separately or as a library of compounds comprising at least 2, for example 5 to 1,000, or 10 to 100 compounds. The library of formula I can be prepared by a procedure known to those skilled in the art, by a combination of "split and mix" methods or by multiple parallel synthesis using solution phase or solid phase chemistry. Thus, according to another aspect of the invention, a library of compounds comprising at least two compounds or a pharmaceutically acceptable salt thereof is provided. General procedures and examples provide exemplary methods for preparing the compounds of the invention. Those skilled in the art will appreciate that other synthetic routes can be used to synthesize the compounds of the invention. Although specific starting materials and reagents are described and discussed in the schemes, general procedures, and examples, other starting materials and reagents can be readily substituted to provide various derivatives and/or reaction conditions. In addition, many of the illustrative compounds prepared by the methods can be further modified in accordance with the present invention using conventional chemistry well known to those skilled in the art. In the preparation of the compounds of the invention, protection of the distal functional groups of the intermediate (e.g., primary or primary amines) may be necessary. The need for this protection will vary depending on the nature of the functional group and the conditions of the preparation process. Suitable amine protecting groups include ethenyl, trifluoroethenyl, tert-butoxy (B0C), benzyloxycarbonyl (CBz) and 9-decyloxycarbonyl (Fmoc). The need for this protection can be readily determined by those skilled in the art. For a general description of the protecting groups and their use, see τ. w Greene,

Protective Groups in Organic Synthesis, John Wiley &amp; Sons, New York, 1991. 158436.doc -332-201215609 In the process for preparing the compounds of the present invention, it is preferred to separate the reaction products from each other and/or from the starting materials. The desired product of each step or series of steps is separated and/or purified to the desired degree of homogeneity by techniques commonly employed in the art. Typically such separations include multiphase extraction, crystallization from a solvent or solvent mixture, distillation, sublimation or chromatography. Chromatography can include a number of methods including, for example, reverse phase and normal phase chromatography; size exclusion chromatography; ion exchange chromatography; high pressure, medium pressure and low pressure liquid chromatography methods and apparatus; small scale analytical chromatography, Simulated moving bed (SMB) and preparative thin layer or thick layer chromatography; and small-scale thin layer chromatography and flash chromatography techniques. Another type of separation process involves treating the mixture with the selected reagents to bind to the following materials or otherwise separating them: the desired product, the unreacted starting material, the reaction by-product, or the like. Such agents include adsorbents or absorbents such as activated carbon, molecular sieves, ion exchange media or the like. Alternatively, the reagent may be an acid (in the case of a basic substance), a base (in the case of an acidic substance), a binding reagent (such as an antibody, a binding protein), a selective chelating agent (such as a crown ether), a liquid/liquid ion Extraction reagent (LIX) or an analog thereof. The choice of the appropriate separation method depends on the nature of the material involved (such as boiling point and molecular weight K in distillation and sublimation), the presence or absence of polar functional groups (in chromatography), the stability of the material in acidic and basic media. (in multiphase extraction) and similar properties. The mixture of diastereomers can be separated into its individual diastereomers on the basis of their physicochemical differences by methods well known to those skilled in the art, such as by chromatography and/or fractional crystallization. It can be utilized by using appropriate optically active compounds (for example, for palm auxiliaries such as palmitic alcohol or moxil 158436.doc-333)

Reaction of 201215609 J chloride) Conversion of the enantiomeric mixture to a mixture of diastereomers, separation of the individual diastereomers and conversion (eg hydrolysis) of the individual diastereomers to the corresponding pure Enantiomers to separate the enantiomers. Furthermore, some of the compounds of the invention may be atropisomers (e.g., substituted aryl) and are considered as part of this invention. Enantiomers can also be separated by the use of a palmitic hplc column. A single stereoisomer (e.g., an enantiomer substantially free of its stereoisomer) can be obtained by resolution of the racemic mixture using methods such as the use of optically active resolving agents to form the diastereomers ( Eliel, E. and wiien, S. "Stereochemistry of Organic Comp〇unds", J〇hn Sis &amp; Sons, Inc., New York, 1994; Lochmuller, CH, (1975) J. Chromatogr., 1 13 ( 3): 283_302). The racemic mixture of the palmitic compound of the present invention can be isolated by any suitable method, including: (1) formation of an ionic diastereomeric salt with a palmitic compound and by stepwise crystallization or other methods. Separating, (2) forming a diastereomeric compound with a palmitic derivatizing reagent, separating the diastereomers, and converting into pure stereoisomers; and (3) directly separating under palmar conditions substantially Pure or concentrated stereoisomers. See: "Drug Stereochemistry, Analytical Methods and

Pharmacology, edited by Irving W. Wainer, Marcel Dekker, Inc.,

New York (1993). Under method (1) ' can be achieved by enantiomeric pure palmitic base (such as brucine, qUinine, ephedrine, strychnine) , a-fluorenyl _b-phenylethylamine (amphetamine) and its analogs) are reacted with an asymmetric 158436.doc • 334-201215609 compound (such as formic acid and sulfonic acid) with acidic functional groups. To form diastereomeric salts. Separation of the diastereomeric salts can be facilitated by fractional crystallization or ion chromatography. In order to separate the optical isomer of the amine compound, the addition of a palmitic carboxylic acid or a reductive acid such as camphor, tartaric acid, mandelic acid or lactic acid may result in the formation of diastereomeric salts. Alternatively, by the method (2), the substrate to be resolved is reacted with an enantiomer of the palm compound to form a diastereomeric pair (Ε. and Wilen, S. "Stereochemistry of Organic Compounds" John Wiley

&amp; Sons, Inc., 1994, p. 322) "Diastereomeric compounds can be formed by reacting an asymmetric compound with an enantiomerically pure palmitic derivatizing reagent such as a menthyl derivative. 'Subsequent separation of diastereomers and hydrolysis to give pure or enriched enantiomers. The method for determining optical purity comprises: preparing a palmitic ester of a racemic mixture, such as menthyl ester, for example (-) Menthyl chloroformate (in the presence of the test), or M〇sher ester ', ie, a_methoxy-a•(trifluorodecyl)phenyl acetate; and Analysis of NMR spectra by the presence of enantiomers or diastereomers (Jacob III. j. 〇rg. Chem. (1982) 47: 4165). The stable diastereomers of the stagnation of the isomers can be separated by normal phase and reverse phase chromatography following the method of isolating the isomerized naphthyl-isoquinoline (W〇 96/15111). By method (3), a mixture of two enantiomers can be separated by chromatography using a palm-shaped stationary phase ("Chiral Liquid Chromatography" (1989) W. J. Lough, edited by Chapman And Hall, New Y〇rk; 〇kainoto' J. Chromatogr., (1990) 513:375-378). The enriched or purified enantiomer can be distinguished by a method for distinguishing other palmitic molecules having asymmetric carbon atoms, such as 158436.doc-335 · 201215609 optical rotation and circular dichroism. The following schemes and the definitions used elsewhere in this paper are: BOP 4-(3-(acridin-3-yl)ureido) benzalkonium sulfonate CDC13 Deuterated gas imitation δ Chemical shift (ppm) DCM Digas methane DIEA N,N-diisopropylethylamine DMA N,N-dimethylacetamide DMF N,N-dimethyl decylamine DMSO dimethyl sulfoxide DMSO-d6 dimethyl sulfoxide EDCI Nl-( (ethylimido)methylene)-N3,N3-dimercaptopropane-1,3-diamine hydrochloride EtOAc ethyl acetate EtOH ethanol GF/F glass microfiber filter*H NMR proton NMR HOAc acetic acid HATU hexafluorophosphate 2-(3Η-[1,2,3]triazolo[4,5-b]pyridin-3-yl)-1,1,3,3-tetradecylisoindole HOBT 1H -Benzo[d][l,2,3]triazol-1-ol hydrate HPLC high pressure liquid chromatography MHz 158436.doc -336- 201215609 KOAc potassium acetate i-PrOH isopropanol LC-MS liquid layer Analysis/mass spectrometry (M+l) Mass +1 m-CPBA methane perbenzoic acid MeOH sterol n2 nitrogen NaHC03 sodium bicarbonate MgS〇4 magnesium sulfate PTLC preparative thin layer chromatography TEA triethylamine THF tetrahydrofuran TLC thin Layer chromatography of amine-sulfonamide: Process 1

+ H2N-(CH2)n-A-Q-N

Ri η = 0=4 G=OH or OR Q = S(0), S(0)2, or C(O)

HN~(CH2)n-A-Q-N

R2 I II m In Scheme 1, it can be at a temperature in the range of -78 ° C to 200 ° C, such as dioxane, N,N-dialkylguanamine, N,N- a coupling reagent such as EDCI, HATU or HOBt and a base in an inert solvent such as dialkylacetamide, dialkyl ether, cyclic ether, DMSO or N-mercapto-2-pyrrolidone (for example: K2C03, Cs2C03) , Nm, NaOR, KOR), with 158436.doc -337- 201215609

I(G-〇H) treatment II to obtain the compound πΐ. Alternatively, I(G=OR) can be used to treat compound I» in an inert solvent (such as toluene) in an inert solvent (such as toluene) at the temperature of _78 ° C to 200 ° C. Those skilled in the art will recognize that the starting materials can be varied and additional steps can be used to prepare the compounds encompassed by the present invention, as illustrated by the examples below. All reagents and solvents were standard commercial grade and were used without further purification unless otherwise stated. Brewing amine · wind: Process 2

rX 〇HN-iCH^-AQ-N7 II i ,Ri + (CH2)n—AQ-:N, η = 0=4 G= OH or OR Q = S(0), S(0)z, or C (0&gt; 1 Π ΙΠ can be at a temperature in the range of -78 ° C to 200 ° C, such as a gas-burning, N,N-dialkylguanamine, N,N-dialkyl a coupling reagent such as EDCI, HATU, BOP or HOBt and a base (for example: K2C03, Cs2C03, NRjRsR^, in an inert solvent of acetamide, dicalcin, DMSO or N-methyl-2-pyrrolidone, In the presence of NaOR, KOR), π is treated with I(G=OH) to obtain the hydrazine of the compound of Scheme 2. Alternatively, it may be in an inert solvent (such as toluene) at a temperature ranging from -78 ° C to 200 ° C. 'Processing 1 with I and trimethylaluminum to obtain the compound ΙΠβ. It will be appreciated by those skilled in the art that the starting materials can be altered and additional steps can be used to prepare the compounds encompassed by the present invention, such as The following examples are given. Unless otherwise stated, all reagents and solvents were used at standard commercial grade 158436.doc -338-201215609 and were used without further purification.

Ar3-Z

B(0R)2, Br, or J[ Q _ 如广(CH^/ 〇χ

NHiC^^^Arj-S-ONa

VI

Test

Γ3 In Scheme 3, Compound III of the invention can also be combined by following the procedures outlined in Scheme IV. At temperatures ranging from -78 ° C to 200 ° C, such as dioxane, N,N-dialkylformamide, hydrazine, hydrazine-dialkylacetamide, dialkyl ether, In an inert solvent such as DMSO or hydrazine-hydrazino-2-pyrrolidone, in the presence of a coupling reagent such as EDCI, HATU, hydrazine or HOBt and a base (for example: K2C03, Cs2C03, NRiR^R^, NaOR, KOR), Treatment of II with IV gave compound V. Compound V can be treated with a base such as sodium ethoxide in the presence of a protonating solvent such as ethanol to give compound VI. Compound VI is treated with an aryl sulfonic acid or an aryl halide under the promotion of palladium or copper to give the target compound III. EXAMPLE 1 Preparation of Representative Indoleamine-Sulphonamide Analogs These examples illustrate the preparation of representative substituted indoleamine-sulfonamide analogs.

Example 1A 158436.doc -339- 201215609 N-(4-(N-(2-(Trifluoromethoxy)phenyl)aminesulfonyl)benzyl benzo[3,2-c]pyridine-2- Formamide

A: 4-cyano-indole-(2.(trifluoromethoxy)phenyl)benzenesulfonamide:

2-(Tris-methoxy)aniline (10.902 g, 58.5 mmol) was dissolved in 0 pyridine (100 mL) and cooled to EtOAc. A solution of 4-cyanobenzene-1-amine-brewed chlorine (11.573 g, 55.7 mmol) in 0-bit (100 mL) was added via an addition funnel over 10 min. The mixture was heated to 85 ° C for 16 hours and the pyridine was removed under reduced pressure. The residue was diluted with DCM and washed with 1 M EtOAc (x2), water (xl), brine (X) and saturated NaHC03 (xl). The organic layer was dried with EtOAc EtOAc EtOAc. *H NMR (300 HMz; DMSO-d6): δ 10.58 (s, 1 Η), 8.06 (d, 2H), 7.89 (d, 2H), 7.30 (s, 4 H). B : 4-(Aminomethyl)-N-(2-(trifluoromethoxy)phenyl)benzenesulfonamide:

158436.doc -340· 201215609 4-cyano-N-(2-(trifluoromethoxy)phenyl)benzenesulfonamide (2.0 g, 5.84 mmol) was dissolved in THF (30 mL) Burning - tetrahydrogen. Furan complex (14.61 mL of 1 M THF solution). The mixture was heated to 70 °C for 2 hours, then cooled to room temperature then MeOH (10 mL). The mixture was briefly warmed to 70 &lt;0&gt;C for 15 min then the volatiles were removed in vacuo and EtOAc (EtOAc &lt The layers were separated and the organic layer was washed with water and brine. The combined aqueous washes were extracted with EtOAc, combined with previous organic extracts and dried over EtOAc. The residue was purified by EtOAc EtOAc (EtOAc) *H NMR (300 HMz; DMSO-d6): δ 7.70 (d, 2Η), 7.41 (d, 2H), 7.19 (d, 1H), 7.00 (d, 1H), 6.89 (t, 1H), 6.58 ( t, 1H), 3.84 (s, 2H). C : N-(4-(N-(2-(trifluoromethoxy)phenyl)aminesulfonyl)benzyl)-1Η-吼luo[3,2-c]pyridine-2-carboxamidine Amine: Ο

1H-pyrrolo[3,2-c]pyridine-2-furic acid (478 mg, 2.95 mmol), 4-(aminomethyl)-N-(2-(trifluoromethoxy) at 25 °C A mixture of phenyl)phenyl hydrazine (973 mg, 2.81 mmol), HATU (1.122 g, 2.95 mmol), DIEA (1.082 mL, 6.20 mmol) and DMF (15 mL) was stirred at ambient temperature for 16 h. Dilute the mixture with EtO Ac and saturate 158436.doc -341 - 201215609

NaHCCh and saline were washed sequentially. The organic extracts were separated and dried <RTI ID=0.0></RTI> to <RTI ID=0.0></RTI> <RTI ID=0.0> The combined fractions were wet-milled with EtsO to give a white solid. !H NMR (300 HMz; DMSO-de): δ 12.10 (br s, 1H), 9.23 (t, 1 H), 8.98 (s, 1H), 8.21 (d, 1H), 7.78 (d, 2H), 7.47 (d, 2H), 7.38 (d, 1H), 7.31-7.19 (m, 6H), 4.58 (d, 2H) » LC-MS: 491.11 (M+l).

Example IB Ν-(4·(piperidin-1-ylsulfonyl)benzyl)thieno[3 2_c]pyridine 2-carboxamide

Combine (4-(Butidine-1-ylsulfonyl)phenyl)methanamine (155 mg, 〇6〇9 mm〇1) with tridecyl aluminum (0.30 mL, 0.600 mmol) in 曱 (2 Mix in mL) and mix for 30 minutes at ambient temperature. Then pheno[3,2-c] was added. A solution of benzoic acid decyl ester (100 mg, 0.518 mmo according to WO 2004/064836) in toluene (2 mL) was added and the mixture was heated to u 〇〇 c for 16 h. After cooling, a sodium potassium tartrate solution and a saturated solution of Et?Aci were added and the mixture was vigorously stirred for 30 minutes and then filtered. The layers were separated, dried EtOAc EtOAcjjjjjj !H NMR (300 HMz; CDC13): δ 9.13 (s, 1H), 8.50 (d, 1H), 7.93 (s, 1H), 7.79 (t, 1H), 7.67 (d, 1H), 7.48 (d, (2, H) . LC-MS: 416.11 (M+l).

EXAMPLE 1C N-(4-(N-(2,5-Dimethoxyphenyl)aminesulfonyl)benzyl)_1H_npyr-[3,2-c]pyridine-2-carboxamide Ο

Into: 1^-(4-(1^-(2,5-dimethoxyphenyl)amine continuation base} base group)

4-(Acetylaminomethyl)benzene-1-sulfonium (25 mg, (U mmol), 2,5-dimethoxyaniline (15.3 mg, 0.1 mmol) and 0 bite (0.25 mL) The mixture was stirred in EtOAc (1 mL) EtOAc (EtOAc) (HHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHH HMz; CDC13): δ 7.73 (d, J=8 Hz, 2H), 7.30 (d, J=8 Hz, 2H), 7.14 (d, J=3.2 Hz, 1H), 7.05 (s, 1H), 6.66 (d, J=8.8 Hz, 1H), 6.54 (dd, J=8.8 Hz, J' = 3.2 Hz, 1H), 5.95 (br s, 1H), 4.46 (d, J=6 Hz, 2H), 3.74 (s, 3H), 3.61 (s, 3H), 158436.doc -343- 201215609 2.07 (s, 3H). LC-MS: 364.99 (Μ+l). B: gasification (4-(N-(2) ,5-dimethoxyphenyl)amine sulfonyl)phenyl)methylammonium:

N-(4-(N-(2,5-Dimethoxyphenyl)aminesulfonyl)benzyl)acetamide (28 mg, 0.077 mmol) and 3 N HCl (0.5 mL, 1.5 mmol) The mixture in 70% i-PrOH (0.5 mL) was heated at 100 ° C for 5 hours. The title compound was obtained as a white solid. *H NMR (400 HMz; CDC13): δ 7.84 (d, J = 8.4 Hz, 2H), 7.56 (d, J = 8.8 Hz, 2H), 7.04 (d, J = 2.8 Hz, 1H), 6.74 (d , J=9.2 Hz, 1H), 6.60 (dd, J=9.2 Hz, J'=3.2 Hz, 1H), 5.95 (br s, 1H), 4.16 (s, 2H), 3.70 (s, 3H), 3.54 (s, 3H). LC-MS: 323.03 (M+l). C : N-(4-(N-(2,5-dimethoxyphenyl)aminesulfonyl)benzyl)-1Η-«Bilozeto 13,2-c]pyridine-2-carboxamide ··

Following Example 1C, replacing HATU with BOP and replacing 4-(aminomercapto)-N- with 4-(aminomercapto)-N-(2,5-dimethoxyphenyl)benzenesulfonamide (2-(Trifluoromethoxy)phenyl)benzenesulfonamide to prepare the title compound. Purification by PTLC 158436.doc • 344· 201215609 product. !H NMR (400 HMz; CD3OD): δ 8.90 (d, J=〇.8 Hz, 1H)' 8.22 (d, J=5.6 Hz, 1H), 7.71 (d, J=8.4 Hz, 2H), 7.51 (d, J=6 Hz, 1H), 7.45 (d, J=8.8 Hz, 2H), 7.28 (d, J=〇-8 Hz, 1H), 7.02 (d, J=3.2 Hz, 1H), 6.70 (d, J=9.2 Hz, 1H), 6.59 (dd, J=8.8 Hz, J'=3.2 Hz, 1H), 4.62 (s, 2H), 3.69 (s, 3H), 3.46 (s, 3H). LC-MS: 466.98 (M+l). Example 2: Preparation of Representative Indoleamine-Base Analogs These examples illustrate the preparation of representative substituted indoleamine-sulfonamide analogs.

Example 2A N-(4-(phenylsulfonyl)benzyl)-1 Η-pyrrolo[3,2-c]pyridine-2-carboxamide

a : 4-(phenylsulfonyl)benzonitrile:

A mixture of 4-fluorobenzonitrile (5 g, 41.3 mmol) and sodium benzenesulfinate (7.45 g &apos; 45.4 mmol) in DMSO (30 mL) was heated at 130 &lt;0&gt;C for 16 h. The mixture was cooled to room temperature and poured onto 3 g of ice. The precipitate was collected, washed with water and dried to give the title compound. !Η NMR (300 MHz, CDC13): δ 8.03-8.07 (m, 2Η), 7.93- 158436.doc -345- 201215609 7.97 (m, 2H), 7.78-7.82 (m, 2H), 7.60 (m7.65 , 1H), 7.26-7.58 (m, 2H). b: (4-[phenylsulfonyl]phenyl)methylamine:

A mixture of 4-(phenylindolyl)benzonitrile (9.4 g, 38.64 mmol) and Raney Ni (500 mg) in 2 N NH3-MeOH (150 mL) was hydrogenated at 50 psi 16 hours. Nitrogen gas was bubbled through the mixture, which was then filtered through a pad of celite and washed with methanol. The filtrate was concentrated and triturated with diethyl ether to give the title compound. *H NMR (300 MHz, DMSO-d6): δ 7.85-7.95 (m, 4 Η), 7.53-7.68 (m, 5 Η), 3.74 (s, 2 Η), 1.83 (br s, 2 Η). c : N-(4-(phenylsulfonyl)benzyl)-1Η^pyrho[3,2-c]acridin-2-carboxamide:

1H-0 piroxime [3,2-2]0 ratio bite-2-carboxylic acid (1·0 g, 6.17 mmol), HATU (3.52 g, 9.25 mmol), diisopropylethylamine (2.69 mL, A mixture of 15.42 mmol) and (4-(phenylsulfonyl)phenyl)decylamine (1.754 g, 7.09 mmol) in EtOAc m. The solvent was removed under reduced pressure, water (2 mL) was then evaporated andEtOAc. The combined 158436.doc-346·201215609 organic layer was washed sequentially with water, saturated sodium bicarbonate and brine. The extract was dried <RTI ID=0.0>: </RTI> EtOAc (EtOAc) lK NMR (300 MHz, DMSO-d6) δ 4.56 (d, J = 5.57 Hz, 2H), 7.29 (s, 1H), 7.34 (d, J = 5.57 Hz, 1H), 7.56-7.66 (m, 5H) , 7.91-7.94 (m, 4H), 8.20 (d, J = 5.87 Hz, 1H), 8.91 (s, 1H), 9.245-9.28 (m, 1H), 12.03 (s, 1H). LC-MS: 392.13 (M+l) 〇

Example 2B 3-bromo-7V-(4-(phenylsulfonyl)benzyl)-1 Η-tono-acridol-2-carboxamide

N-(4-(phenylsulfonyl)benzyl)-1H-&quot; bis-[3,2-cp-pyridyl-2-carboxamide (from Example 1; 200 mg, 0.511 mmol) and A mixture of 1-bromopyrrolidine-2,5-dione (91 mg, 0.511 mmol) in DMF (10 mL) To the mixture was added EtOAc (100 mL). The organic layer was washed with water and brine, dried over sodium sulfate The crude material was purified by Biotage using MeOH / DCM (0% - 10%) to afford title compound. *Η NMR (300 MHz, DMSO-d6): δ 12.42 (br s, 1H), 8.78 (m, 2H), 8.30 (d, 1H), 7.93 (d, 4H), 7.59-7.69 (m, 5H) , 7.38 (dd, 1H), 4.59 (d, 2H). LC-MS: 470.06 (M+l). 158436.doc •347· 201215609

Example 2C N-({4-[(4-fluorophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]bite-2-carboxamide Ο

a : 4-(4-fluorophenylsulfonyl)benzonitrile:

Following title 1A, the title compound was prepared using sodium 4-fluorobenzenesulfinate instead of sodium benzenesulfinate. 'H NMR (300 MHz, DMSO-D6) δ: 8.10-8.18 (m, 6H), 7.42-7.12 (t, 2H). b: (4-[4-Fluorophenyl]indolyl]phenyl)methylamine:

Following the procedure of Example 1B, 4-(4-fluorophenylsulfonyl)benzonitrile was used instead of 4-(phenylsulfonyl)benzonitrile to give the title compound. *H NMR (300 MHz, DMSO-d6): δ 7 s 7 ,, , ° /-8-7.96 (m, 4H), 3.74 (s, 2H), 7.42-7.64 (m, 4H), 3.64 (m , 2H). c: N-({4-[(4-fluorophenyl)]]phenyl}methyl) stimulate [2,3c] bite-2-cartoamine: 158436.doc -348· 201215609 ο

(4-(4-Fluorophenylsulfonyl)phenyl)methanamine hydrochloride (ΐ4〇9, 4.67 mmol) was combined with toluene (20 mL) and cooled to hydr. Hey. Tridecyl aluminum (7.00 mL of a 2 Torr solution in toluene) was added and the mixture was stirred at ambient temperature for 4 Torr. A solution of thieno[2,3_e]pyridine·2-methyl decanoate (82 〇 mg, 4.24 mmol, prepared according to WO 2004/064836) in toluene (10 mL) was added via a syringe and the mixture was heated to 8 Hey. 〇 lasts 4 hours. The mixture was diluted with saturated sodium potassium tartrate (25 mL) and EtOAc (25 mL) and stirred vigorously for one hour&apos; and then filtered through GF/F paper. The organic layer was separated, dried <RTI ID=0.0>(M. The residue was triturated with dcm and the title compound was collected by vacuum filtration. !H NMR (300 MHz, DMSO-d6) δ 9.59 (t, 1 Η), 9.30 (Sj 1H), 9.50 (d, 1H), 8.15 (s, 1H), 8.04-7.98 (m, 2H), 7.96- 7.90 (m, 3H), 7.56 (d, 2H), 7.47-7.40 (m, 2H), 4.55 (d, 2H).

LC-MS: 427.03 (M+l) 〇 Example 2D N-(4-(phenylsulfonyl)benzyl)-1H-pyrrolo[3,2-c] acridine-2-carboxamide Ο

a: 4-(Ethylaminomethyl) benzenesulfinate sodium: 158436.doc •349- 201215609

Add 4-(ethylaminomethyl)benzene-1-sulfonium (124 g, 5 mm 〇1) to water-cooled Na2S〇3 (1.89 g '15 mmol) in water (3.75 mL) In the solution in the solution, 'solid NaHCO3 (850 mg, ι〇mmol) was added in several small portions to keep the pH slightly. The mixture was spoiled at ambient temperature for 2 hours to give a thick white suspension. Brine (2 ml) was added and the mixture was stirred at ambient temperature for 15 minutes. The precipitate was collected by filtration and dried under vacuum overnight. The solid was triturated and stirred with 125 mL MeOH for 3 min then filtered and washed with EtOAc (20 <RTI ID=0.0> The title compound was obtained as a white solid. !H NMR (400 MHz, CD3〇D): δ 7.61 (d, J=8.4 Hz, 2H), 7.34 (d, J=8.4 Hz, 2H), 4.38 (s, 2H), 1.98 (s, 3H) . b : N-(4-(benzo[dHl,3]dioxol-5-ylsulfenyl)benzyl)acetamide:

4-(Ethylaminomethyl)benzene ylide (23.5 mg, 0.1 mmol;), benzo[d][l,3]dioxol-5-yl-acid (20.7 mg , 〇. 125 mmol), a mixture of copper acetate (11) (22.7 mg, 0.125 mmol) and TEA (〇.063 mL, 0.45 mmol) in DMSO (1.5 mL). The mixture was cooled to room temperature and partitioned between EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc NMR (400 MHz, CDC13): δ 7.85 (d, J=8 Hz, 2H), 7.52 (dd, J=8 Hz, J'=1.6 Hz, 1H), 7.39 (d, J=8.4 Hz , 2H), 7.29 (d, J-2 Hz, 1H), 6.87 (d, J=8 Hz, 1H), 6.05 (s, 2H), 5.87 (br s,1H), 4.47 (d, J=6.4 Hz, 2H), 2.04 (s, 3H) LC-MS: 333.97 (M+l). c: (4-(benzo[d][1,3]dioxol-5-ylsulfonate Mercapto)phenyl)methamine hydrochloride:

N-(4-(benzo[d][l,3]dioxol-5-yl)-based)

A mixture of CIH*H2N decylamine (10 mg '0.03 mmol) and 3 N HCl (0.36 mL, 1.08 mmol) in 701⁄4 i_PrOH (0.2 mL) was heated at 100 ° C for 5 hours. The mixture was concentrated to dryness. The title compound is obtained as an off-white solid: H NMR (400 MHz, CD3OD): δ 8.00 (d, J = 8.4 Hz, 2H), 7.64 (d, J - 8.4 Hz, 2H), 7.55 (dd, J = 8.4 Hz , J'=2 Hz 1H) 7.34 (d, J-2.4 Hz, 1H), 6.98 (d, J=8 Hz, 1H), 6.08 (s, 2H), 4.19 (s, 2H). LC-MS: 219.99 (M+l). d : N-(4_(phenylsulfonyl) nodal group)-1Η-π*rrolo[3,2_c]pyridine j-carboxamide Amine: 158436.doc •351 - 201215609

Following the procedure of Example 1C, substituting (4-(benzo[d][l,3]dioxol-5-ylsulfonyl)phenyl)methanamine hydrochloride (4-(phenylsulfonate) The title compound was prepared by substituting BOP for HATU. The title compound was purified by PTLC. 4 NMR (400 MHz, CD3OD): δ 9.05 (s, 1Η), 8.29 (d, J=6

Hz, 1H), 7.90 (d, J = 8.4 Hz, 2H), 7.68 (d, J=6 Hz, 1H), 7.57 (d, J=8 Hz, 2H), 7.52 (dd, J=8Hz, J '=2 Hz, 1H), 7.42 (s, 1H), 7.31 (d, J=2 Hz, 1H), 6.95 (d, J=8.4 Hz, 1H), 6.06 (s, 2H), 4.66 (s, 2H) » LC-MS: 435.97 (M+l). Example 2E 1-Methyl-N-(4-(phenylsulfonyl)benzylazolo[3,4-b]pyridine-5-carboxamide

Iodine oxime (33.5 pL, 0.535 mmol) was added to N-(4-(phenyltrial)benzyl)-1 oxime- to saliva[3,4-b] at ambient temperature. More than a mixture of 5-5-mercaptoamine (Example 12; 100 mg '0.255 mmol) and potassium carbonate (1 〇 6 mg, 0.764 mmol) in DMF (1 mL). The reaction mixture was heated to continue for 16 h. then the mixture was diluted with EtOAc and washed with brine (x3). The organic layer was dried over Na.sub.2.sub.4 and concentrated in vacuo. The residue was dissolved in 158436. EtOAc - EtOAc (EtOAc) !H NMR (DMSO-d6): δ 9.31 (t, 1H)} 9.02 (d, 1H), 8.72 (d, 1H), 8.28 (s, 1H), 7.94-7.90 (m, 4H), 7.66-7.55 (m, 5H), 4.56 (d, 2H), 4.07 (s, 3H). LC-MS: 407.07 (M+l).

Example 2F 1-Methyl-N-(4-(phenylsulfonyl)benzyl)-1Η-tondro[3,2_c]e than pyridine-2-carboxamide

Ο

Sodium hydride (48 mg (60%), 1.226 mmol) was added to ice-cooled ΙΗ-吼 &quot; each [3,2-c]pyridine-2-carboxylate (180 mg, 1.022 mmol) in THF In a solution (3 mL). The mixture was then warmed to room temperature over 1 minute. Methyl iodide (0.070 mL, 1.124 mmol) was added and the mixture was stirred 16 hr. The mixture was partitioned between EtOAc and water. The combined organic layers were dried over MgSO4, filtered and concentrated to dry. The residue was purified by EtOAc to give the title compound. H NMR (CDC13): δ 8.90 (s, 1H), 8.35 (d, 1H), 7.92 (s, 1H), 7.20 (d, 1H), 3.95 (s, 3H), 3.82 (s, 3H). 158436.doc - 353 - 201215609 b : 1-Methyl-indole-(4.(phenylsulfonyl)benzyl)-1Η-indolo[3,2-c]% pyridine-2-carboxamide :

Following Example 3C, substituting methyl chloro-1H-pyrrolo[3,2-c]picolinate and (4-(phenylsulfonyl)phenyl)methylamine for thieno[2,3-cj% pyridine, respectively The title compound was prepared from methyl 2-nonanoate and (4-(4-fluorophenylsulfonyl)phenyl)guanamine. The title compound was purified by PTLC. H NMR (DMSO-D6): δ 9.27 (t, 1H), 8.91 (s, 1H), 8.28 (d, 1H), 7.92-7.95 (m, 4H). 7.53-7.67 (m, 6H), 7.27 (s, 1H) 4.52 (d, 2H), 3.95 (s, 3H). LC-MS: 406.01 (M+l).

Example 2G]\-(4_(phenyl fluorenyl)benzyl)-111-flavored [4,5-(;]&quot; than bite-2-methamine

u u a: 1H-imidazo[4,5-c]pyridine-2-carboxylic acid methyl ester:

Methyl 2,2-dichloro-2-methoxyacetate (1 585 g, 9 16 mm 〇i) was added to the pyridine-3,4-diamine (0.5 g, 4.58 mmol) and DIEA (4.8 〇, 27 / · 5 _ol) in a solution in DCM (20 mL). The mixture was stirred at room temperature m 158436.doc • 354·201215609 h, then EtOAc was added and the mixture was washed with saturated sodium hydrogen carbonate and brine. The organic layer was dried with EtOAc EtOAc (mjjHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHHH 1H), 4.09 (s, 3H). b : N-(4-(phenylsulfonyl) nodal)_ih-isoxazo[4,5_c]pyridine-2-carbamamine

Following Example 3C, thiophene [2,3-c] was replaced with 1H-imidazo[4,5-c]pyridine-2-carboxylic acid methyl ester and (4-(phenylsulfonyl)phenyl)decylamine, respectively. The title compound was prepared as the oxime-2-carboxylate and (4-(4-fluorophenylsulfonyl)phenyl)methylamine. The title compound was purified by PTLC. 1H NMR (CD3OD): δ 8.32 (s, 1H), 8.16 (d, 1H), 7.89-7.93 (m, 4H), 7.51-7.64 (m, 5H), 7.30 (d,1H), 4.81 (s, 2H). LC-MS: 393.02 (M+l).

Example 2H #N-(4-((3-Ga-5-fluorophenyl)sulfonyl)benzyl)furo[2,3-c]pyridine-2-carbamide

F a : ethyl furo[2,3-c]pyridine-2-carboxylate:

C02Et 158436.doc •355· 201215609 to ethyl 3-(trifluoromethylsulfonyloxy)furo[2,3-c]pyridine-2-carboxylate (524 mg, 1.545 mmo b according to US 20070049603) 1 〇〇 / 0 Pd / C (50 mg) and triethylamine (0.5 mL, 3 - 59 mmol) were added to a solution in ethanol (15 mL). The mixture was placed under a hydrogen (balloon) atmosphere and stirred for 16 hours. The mixture was filtered, EtOAc (EtOAc m. !H NMR (CDC13): δ 9.03 (s, 1H), 8.51 (d, 1H), 7.63 (dd, 1H)' 7.52 (d, 1H), 4.48 (q, 2H), 1.45 (t, 3H). MS (ESI): 192.01 (M+H). b : furo[2,3-c]pyridine-2-carboxylic acid:

To a solution of furo[2,3_c]pyridine-2-carboxylic acid ethyl ester (3.82 g, 19.98 mm Ql) in water: THF.MeOH (1:11:1 '60 mL) 59.9 mmol) and the resulting mixture was allowed to fall for 16 hours at ambient temperature. The solvent volume is then reduced to approximately 20 mL and acetic acid is added until? 11 is about 4. The solid was collected by vacuum filtration, washed twice with EtOAc (EtOAc)jjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjj , 1H), 7 81 (dd, 1H), 7.71 (d, 1H), 3.36 (br s, 1H) » c : N-(4-((3-)-5-fluorophenyl) sulfhydryl) Benzyl) cough and 2-carbamide: 158436.doc -356- 201215609

To 0f 0 South and [2,3-c] ° bite 2-decanoic acid (243 mg, 1.487 mmol), (4-(3-a-5-fluorophenylsulfonyl)phenyl) Amine hydrochloride (500 mg, 1.487 mmol) and hexafluorophosphate (benzotriazol-1-yloxy) ginseng (didecylamino) scale (724 mg, 1.636 mmol) in DMF (8 mL) N,N-Diisopropylethylamine (0.571 mL, 3.27 mmol) was added to the mixture. The homogenous reaction mixture was stirred at ambient temperature for 16 hours then the DMF was removed under reduced pressure. &lt;EMI ID=9.1&gt;&gt; The title compound (440 mg, 67%) was obtained. NMR NMR (DMSO-d6): δ 9.62 (t, 1H), 9.03 (s, 1H), 8.46 (d, 1H), 8.02 (dt, 2H), 7.87-7.80 (m5 4H), 7.62 (d, 1H) ), 7.58 (d, 2H), 4.56 (d, 2H). MS (ESI): 444.82 (M+H). Example 21 N-(4-(4-(ethylamine-methane)phenylsulfonyl)benzyl)imidazopyridine-6-carboxamide

V

a· 4-((4-cyanophenylthio)benzoic acid: 158436.doc •357- 201215609

Add 4-fluorobenzonitrile (2.121 g, 17.51 mmol), 4-M benzoquinone (3 g, 17·51 mmol) and potassium carbonate (7.26 g, 52.5 mmol) to DMF in a 250 mL round bottom flask. Solution in (volume: 50 mL). The reaction was heated to 100 &lt;0&gt;C overnight and was monitored by LCMS. When complete, the slurry was treated with 100 mL of water to give a clear solution. The solution was then slowly treated with a 6 M HCl aqueous solution until ρ Η &lt; 4, then a precipitate formed. The slurry was filtered and washed with water and dried on a filter to give 14.8 g of crude material. NMR showed the presence of product, impurities and water. Drying overnight in a vacuum oven gave 4.41 g of material, which was taken on 50 g of EtOAc and then filtered with 10% MeOH / CH.sub.2Cl2 to afford 3.45 g of material which was used without further purification. *H NMR (300 MHz, DMSO-d6): δ 13.18 (br s, 1H), 7.96 (d, 2H), 7.80 (d, 2H), 7.52 (d, 2H), 7.42 (d, 2H). b. 4-(4-Cyanophenylthio)-N-ethylbenzamide:

Add 4-(4-cyanophenylthio)benzoic acid (3.45 g, 13.51 mmol), HBTU (5.13 g, 13.51 mmol) and HOBT (2.070 g, 13.51 mmol) to DMF in a 500 mL round bottom flask. A solution of the volume: 100 mL) followed by the addition of ethylamine (2M in THF, 20.27 mL, 40.5 mmol). The reaction was stirred overnight and then concentrated under reduced pressure. The residue was dissolved in EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc. The organic layer was separated, dried over anhydrous sodium sulfate, and then concentrated and evaporated. This material was used without further purification. !H NMR (300 MHz, DMSO-d6): δ 8.57 (t, 1 Η), 7.89 (d, 2H), 7.75 (d, 2H), 7.55 (d, 2H), 7.31 (d, 2H), 3· 30 (m,2H), 1.10 (t,3H) 〇c· 4-(4-cyanophenylsulfonyl)_N_ethylbenzoquinone:

Ο Add a solution of 4-(4-cyanophenylthio)-hydrazine-ethyl carbamide (2.81 g, 9.95 mmol) in chloroform (volume: 50 mL) in a 500 mL round bottom flask. It was cooled to 0 ° C and then mCPBA (6.87 g, 29.9 mmol) was added. The reaction was spoiled for 1 hour at 〇 ° C and then warmed to room temperature overnight. The reaction was diluted with a gas sample and poured into a separatory funnel. The organic layer was washed with a 10% aqueous sodium thiosulfate solution, 2 M NaOH and a saturated aqueous sodium sulfate. The separated substrate was dried over anhydrous sodium sulfate, filtered and evaporated, evaporated The material was purified using Biotage to give 2.42 g of pure product (70% yield). *H NMR (300 MHz, DMSO-d6): δ 8.68 (t, 1H), 8.15 (d, 2H), 8.09 (m, 4H), 7.95 (d, 2H), 3.28 (m, 2H), 1.02 ( t, 3H). LC-MS (ESI): 314.92 (M+l). d. 4-(4-(Aminoguanidino)phenylindolyl)·Ν-ethylbenzamide: 158436.doc -359- 201215609

RwP

The monazepole (0.660 g, 7.70 mmol) was added to a Paar flask and washed with methanol. The MeOH was removed by pipette and the process was repeated twice more. Then a solution of 4-(4-cyanophenylsulfonyl)-N-ethylbenzamide (2.42 g, 7.70 mmol) in MeOH (vol.: 50 mL) was added followed by potassium hydroxide (0.043) g, 0·770 mmol) and ammonia (7 Μ, 11.00 mL, 77 mmol) in MeOH. The liquid was placed on a Paar shaker and hydrogenated overnight at 35 psi. The reaction was monitored by LCMS. The solution was then filtered through celite and washed with MeOH. The solution was then concentrated under reduced pressure to give 2.56 g of product. Using Biotage purification material, 2.03 g of product (83% yield) was obtained. !H NMR (300 MHz, DMSO-d6): δ 8.65 (t, 1 Η), 7.98 (m, 4H), 7.88 (d, 2H), 7.55 (d, 2H), 3.76 (d, 2H), 3.24 ( m, 2H), 2.10 (br s, 2H), 1.15 (t, 3H). LC-MS (ESI): 318.95 (M+l). e. N-(4-(4-(ethylamine)-phenyl)sulfonyl)benzyl)imidazo[l,2-a]pyridin-6-carboxamide:

Add 4-(4-(Aminomethyl)phenylsulfonyl) to a 250 mL round bottom flask - 158436.doc -360- 201215609 N-ethylbenzamide (1 g, 3.14 mmol) The solution of [l,2-a]0 is more than [l,2-a]0 than bite-6-formic acid (0.509 g, 3.14 mmol) and HATU (1.314 g, 3.45 mmol) in DMF (volume: 50 mL), followed by DIEA (1.207 mL, 6.91 mmol). The reaction was stirred overnight and then concentrated under reduced pressure. The reaction was diluted with dioxane and poured into a sep. funnel. The organic layer was washed with 1 M NaOH and water. The substrate was separated and concentrated and purified directly using Biotage to yield 514 g of clean product (35% yield). 4 NMR (300 MHz, DMSO-d6): δ 9.19 (t, 1H), 9.11 (t, 1H), 8.64 (t, 1H), 8.04-9.92 (m, 7H), 6.63 (m, 3H), 7.55 (d, 2H), 4.53 (d, 2H), 3.25 (m, 2H), 1.08 (t, 3H). LC-MS (ESI): 463.05 (M+l).

Example 2J N-(4-((3-methoxyphenyl)-decyl)benzyl)-salt and bite _6-carboxamide Ο

The title compound was prepared by following Example 4D in a yield of EtOAc. !H NMR δ (d6-dmso) 9.47 (1H, d); 9.34 (1H, t); 8.92 (lH, d); 8.01 (1H, d); 7.95 (2H, d); 7.80 (1H, d) 7.58 (2H, d); 7.54-7.47 (2H, m); 7.42-7.41 (1H, m); 7.23 (1H, dt); 4.57 (2H, d) and 3.81 (3H, s). LC-MS (ESI): 422.9 (M+l).

Example 2K 158436.doc -361 - 201215609 N-(4-(l-isopropyl-1 ugly-oxazolyl-4-ylsulfonyl)benzyl)imidazo[l,2-a]pyridine-6- Formamide

a. iV-(4-((l-isopropyl-1 ugly-pyrazol-4-yl)sulfonyl)) benzylamine:

Add sodium 4-(acetamidomethyl)benzenesulfinate (3.97 g, 16.89 mmol, 1.3 eq), 1-isopropyl-1H-pyrazole-4-yl-acid (1 liter) in a 1 L round bottom flask 2 g, 12.99 mmol) and a solution of steel (II) acetate (2.6 g, 14.29 mmol), carbonic acid (3.95 g, 28.6 mmol) in DMSO (50 ml), followed by 10 g of 4A molecular sieve. The reaction was mixed overnight. Water and Et〇Ac were added, filtered through a pad of celite, and Et0Ac was added, washed twice with water, dried and concentrated. Purification by biotage column gave ι·9 g #-(4-((1-isopropyl-1/f_°bazol-4-yl)sulfonyl)benzyl)acetamide (45%). !H NMR (DMSO-D6): δ 8.50 (s, 1H), 8.42 (t, iH), 7.91 (s, 1H), 7.86 (d, 2H)} 7.43 (d, 2H), 4.52 (m, iH) )} 4.28(d, 2H), 1.36(d,6H). b. (4-(l-Isopropyl-1 ugly-pyrazole-4-ylsulfonyl)phenyl)methanamine hydrochloride: 158436.doc •362· 201215609

3 M HC1 solution (80 1111) and team (4-(1-isopropyl-1//-0) than sylylene-4-ylsulfonyl) benzyl) acetamide (1.9 g, 5·9 ΐ mm 〇i) A mixture of solutions in 2-propanol (1 〇〇ml) is refluxed over the weekend, the solvent is removed, the test is added, filtered and dried to give 1.4 g (4-(1_isopropyl) 丨 ugly Pyrazole-4-ylsulfonyl)phenyl)methanamine hydrochloride (75%). 4 NMR (DMSO-d6): δ 8.50 (s, 1H), 7.94-7.98 (m, 3H), 7.85 (dd, 1H), 7.69 (d, 2H), 4.52 (m, 1H), 4.08 (d, 2H), 1.37 (d, 6H). c· N-(4_(l-Isopropylazole-4-ylsulfonyl)benzyl)imidazo[12_a]pyridine·6-formamide: Ο

Add imidazo[i,2-a]pyridine-6-decanoic acid (0.719 g, 4.43 mmol), (4-(1-isopropyl-1 ugly-pyrazole-4-yl) in a 250 mL round bottom flask Sulfhydryl) phenyl)methylamine hydrochloride (1.4 g, 4.43 mmol) and HBTU (1.849 g, 4.88 mmol), HOBT (0.747 g, 4.88 mmol) and DIEA (3.87 mL ' 22.16 mmol) in DMF (volume : 50 mL) solution. The reaction was turbulent overnight and then concentrated under reduced pressure. The residue was diluted with dioxane and washed with 1 M aqueous NaOH. The organic layer was separated and concentrated and purified directly in EtOAc to afford 1.24 g of N-(4-(l-isopropyl-1//-pyrazol-4-ylsulfonyl) 15S436.doc • 363-201215609 benzyl Imidazo[l,2-a]pyridine-6-formamide. </ RTI> <RTIgt; m, 4H), 4.42-4.55 (m, 3H), 1.37 (d, 6H). LC-MS: 424.01 (M+l).

Example 2L N-(4-(phenylsulfonyl)benzyl)-lH-pyrazolo[3,4-b]pyridin-5-carboxamide 0

1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid (0.8 g, 4.90 mmol), HATU (1.87 g, 4.90 mmol), diisopropylethylamine (1.2 mL, 6.69 mmol) A mixture of (4-(the present fluorenyl)phenyl) decylamine (m.p.p., 4.46 mmol) in DMF (50 mL) Remove DMF under reduced pressure. 15 mL of water was added to the residue and extracted with EtOAc (3×100 mL). The combined organic layers were washed with EtOAcq. The crude material was purified by Biotage using Me 〇 H / DCM ( 〇 % 1 〇 %) to give the title compound. ]H NMR (DMSO-d6): δ 9.27 (t, 1Η), 8.98 (d, 1H), 8.72 (d' 1H), 8.27 (s, 1H), 7.94-7.90 (m, 4H), 7.66-7.55 (m, 5H), 4.56 (d, 2H). ’

LC-MS: 393.01 (M+l) 〇 Example 2M N-(4-(2,4-dimethylthiazole_S-ylsulfonyl)benzyl)imidazolyl Qja]pyr 158436.doc • 364 - 201215609 Pyridin-6-formamide

Copper iodide (0.2 M DMSO, 1 〇〇pL, 20 μιηοΐ), (S)-pyrrolidine-2-furic acid (0·2 M DMSO w/14% MeOH (v/v) '200 pL, 40 μιηοΐ), 4-(ethylammonium decyl) sodium benzenesulfinate (0.2 M DMSO, 200 μί, 40 μπιοί) and 5-bromo-2,4-dimethylthiazole (0.2 M DMSO, 240 pL A mixture of 48 μηιοί) was heated overnight at 90 ° C with shaking. The reaction was treated with aqueous ammonia and extracted with EtOAc. EtOAc was evaporated and evaporated and evaporated. Et. Heat at ° C for 4 hours and then concentrate to dryness. Using triethylamine (5%, 200 pL in ACN (v/v)) and imidazo[l,2-a]pyridine-6-decanoic acid (0_2 Μ in DMA w/ 10% ΤΕΑ (ν/ The residue was treated with ν), 240 pL, 48 μηιοί) and BOP (0.2 M DCE, 260 pL, 52 μιηοΐ). The solution was heated to 40 °C for 4 hours, then cooled to room temperature and partitioned between EtOAc and EtOAc. The organic layer was separated and concentrated in the air. The title compound was obtained as a white solid. lH NMR (400 MHz, CDC13): δ 8.87 (dd, J=1.6 Hz, J' = 0.8 Hz 1H), 7.89 (dt, J=8.4 Hz, J*=2 Hz, 2H), 7.71 (d, J =1.6 Hz, 1H), 7.67 (s, 1H), 7.60 (d, J=9.2 Hz, 1H), 7.50 (d, J=8.4 Hz 2H), 7.43 (dd, J=9.2 Hz, J'=2 Hz, 1H), 6.84 (bs, 1H), 4.73 (d, J=6 Hz, 2H), 2_65 (s, 3H), 2.57 (s, 3H). 158436.doc -365- 201215609 LC-MS: 427.10 (M+l)»

Example 2N N-(3-(naphthalen-2-ylsulfonyl)benzyl)imidazo[1,2-a]pyridin-6-carboxamide

Add cesium carbonate (1.43) to a mixture of sodium 4-(ethylammonium decyl) benzene sulfinate (0.2 M MeOH, 100 pL, 20 μπιοί) and zinc chloride (0.5 M THF, 40 μί, 20 μηιοί) M MeOH, 25 μιη, 35 μιηοΐ), followed by the addition of 2, naphthalene (0.2 Μ toluene, 11 0, 22. μm ιοί). A solution of XantPhos and Pd2dba3 (0.01 M XantPhos/0.005 M Pd2dba3, 50 pL, 2.5 mol%) in benzene was added, and the reaction was heated at 95 ° C for 4 hours under nitrogen. The reaction was cooled to room temperature and 70% i-PrOH (0.35 mL) and &lt;RTI ID=0.0&gt;&gt; Using triethylamine (5% in ACN (v/v), 100 μM) and imidazo[l,2-a]pyridine-6-carboxylic acid (0.2 Μ in DMA w/ 10% TEA (v/v) The residue was treated with 120 pL, 24 μπιοί) and BOP (0.2 M DCE, 130 pL, 26 μιηοΐ). The solution was heated to 40 °C for 4 hours, then cooled to room temperature and partitioned between EtOAc and EtOAc. The organic layer was separated and deposited on an SCX-SPE cartridge and dissolved in two fractions: 1% with MeOH/EtOAc (v/v) and the second with Et3N/MeOH/EtOAc (1:1:10) v/v/v). The second fractions were concentrated to dryness and purified to purified crystals !H NMR (400 MHz, CDC13): δ 8.85 (s, 1Η), 8.55 (s, 1H), 7.93 (m, 4H), 7.87 (d, J=8 Hz, 1H), 7.81 (dd, J= 8.8 Hz, 158436.doc -366- 201215609 Γ=1·6 Hz, 1H), 7.63 (m,5H), 7.47 (d, J=8.4 Hz, 2H), 7.34 (m,1H), 6.81 (m, 1H), 4.70 (d, J = 5.6 Hz, 2H). LC-MS: 442_13 (M+l). Example 20 N-(4-(Naphthalen-2-ylsulfonyl)benzyl)furo[2,3-C]pyridine-2-carboxamide

a. 4-Bromobenzylaminocarbamic acid tert-butyl ester:

BocHN^Nf^· A 200 mL round bottom flask equipped with a magnetic stir bar was charged with (4y odorant) guanamine hydrochloride (5.23 g, 23.50 mmol), K2CO3 (3.90 g, 28 2 mmol), MeTHF (ratio: 4·00, volume: 50 ml) and water (ratio: 1.000, volume: 12.5 ml). BOC2O (6.00 ml, 25.9 mmol) was added portionwise to the resulting mixture with stirring at room temperature. LCMS after 1 hour indicated complete conversion. The mixture was diluted with additional MeTHF (50 mL) and water (10 mL) and layers were separated. The organic layer was washed with EtOAc (EtOAc m. The crude product was used in the next step without further purification. NMR (400 MHz, CDC13): δ 7.44 (d, J = 8.4 Hz, 2H), 7.15 (d, J = 8.3 Hz, 2H), 4.85 (br s, 1H), 4.26 (d, J = 5.8 Hz, 2H), 1.45 (s, 9H) ppm. -367- 158436.doc 201215609 b. 3-(4-((Tertidinoxy)-phenyl)methyl)phenylthio)propanoate:

BocHN was charged to a 200 mL round bottom flask equipped with a magnetic stir bar containing crude 3-bromobenzylaminocarbamic acid tert-butyl ester (6.72 g '23.5 mmol) in toluene (volume: 50 ml), Hsu's base. (Hunig's Base) (8.21 m Bu 47.0 mmol), XANTPHOS (0.680 g, 1.175 mmol), Pd2 (dba) 3 (0.538 g, 0.5 88 mmol) and finally charged with methyl 3-pyridyl propionate (2.60 guabl) 23 5〇mmol). The mixture force σ is then heated to 10 °C. LCMS after 1 hour indicated significant conversion&apos; but the starting bromide was still apparent at 220 nm. After 2 hours, the LCMS was slightly better after 2.5 hours, and the heating was stopped. After cooling, the mixture was loaded directly onto a short dream rubber tube column. Dissolve with 5:1 hexane-EtO Ac, 4:1 hexane-EtO Ac and finally 3:1 hexane-EtO Ac to give 3-(4-((t-butoxy)) as a colorless oil. Carbonylamino)methyl)phenylthio)propionic acid methyl vinegar (7.19 g, 22.09 mmol, 94 〇/〇 yield). NMR (400 MHz, CDC13): δ 7.32 (d, J = 8.3 Hz, 2H), 7.21 (d, J = 8.2 Hz, 2H), 4.84 (br s, 1H), 4.28 (d, J = 5.8 Hz, 2H), 3.67 (s, 3H), 3.14 (t, J = 7.4 Hz, 2H), 2.61 (t, J = 7.5 Hz, 2H), 1.45 (s, 9H) ppm. ESMS: 348.15 (M+Na). c. 3-(4-((Tertidinoxycarbonylamino)methyl)phenylsulfonyl)propionic acid A 158436.doc •368- 201215609

BocHN O 0,,0 A oxone (23.61 g, 38.4 mmol) and water (ratio: 1.822, volume: 82 ml) were placed in a 500 mL round bottom flask equipped with a magnetic stirrer: stir bar.

The mixture was stirred at room temperature for 5 minutes to dissolve Oxone. Next, 3-(4-((t-butoxy)- ethylamino)indolyl)phenylthio)propanoate (5.0 g, 15-36 mmol) was added to acetonitrile under stirring at room temperature. Ratio: 1. 〇〇〇, volume: 45 ml) of the solution. The mixture was stirred at room temperature. After 2 5 hours, an aliquot was removed, processed and analyzed by 4 NMR to demonstrate complete conversion to sulfone. LCMS also looks good. The reaction mixture was then extracted with Et 〇Ac (l 〇〇 mL). The extract was concentrated under reduced pressure. The aqueous layer was re-extracted with fresh Et〇Ac. This extract is combined with the first concentrated extract. The combined solution was washed twice with aq. EtOAc (EtOAc (EtOAc) Methyl propionate (5.17 g, 14.46 mmol, 94% yield). lH NMR (400 MHz, CDC13): δ 7.86 (d, J = 8.4 Hz, 2H), 7.48 (d, J = 8.6 Hz, 2H ), 5.03 (br s, 1H), 4.41 (d, J = 6.2 Hz, 2H), 3.64 (s, 3H), 3.41 (t, J = 7.7 Hz, 2H), 2.74 (t, J = 7.8 Hz, 2H), 1.46 (s, 9H) ppm. ESMS: 380.07 (M+Na). d. 3-(4-(Aminomethyl)phenylsulfonyl)propionic acid methyl ester hydrochloride

H2N HCI

158436.doc -369· 201215609 A methyl stirrer is equipped with methyl 3-(4-((t-butoxycarbonylamino)methyl)phenylsulfonyl) propionate (5 16 g,! 4.44 mmol) of a 200 mL round bottom flask was charged with MeOH (volume: 50 ml) and concentrated hydrochloric acid (1.323 ml '15·88 mmol). The solution was then heated to 50 °C. LCMS after overnight indicated complete conversion. Stop heating. After cooling, the slurry was partially concentrated under reduced pressure and 32 mL of MeOH was removed. The resulting thick slurry was diluted with MTBE (50 mL). The slurry was stirred at room temperature for 30 minutes and then filtered through a 60 mL mesoporous Buchner funnel. The filter cake was washed with MTBE and dried under suction and under a pressure of nitrogen to give methyl 3-(4-(aminomercapto)phenylsulfonyl)propanoate hydrochloride as a free-flowing, white-white crystalline solid. (4.10 g, 13.96 mmo, 97% yield). NMR (400 MHz, DMSO-d6): δ 8.62 (br s, 2H), 7.92 (d, J = 8.5 Hz, 2H), 7.77 (d, J = 8.4 Hz, 2H), 4.14 (s, 2H), 3.58 (t, J = 7.3 Hz, 2H), 3.52 (s, 3H), 2.59 (t, J = 7.3 Hz, 2H) ppm. ESMS: 258.10 (M+l) 〇 e. 3-(4-((furo[2,3-c]pyridine-2-carboxamido)methyl)phenylsulfonyl) methyl propionate:

A 25 mL round bottom flask equipped with a magnetic stir bar was charged with furan [2,3-c]0 than bite-2-carboxylic acid (135 mg, 0.828 mmol), 3-(4-(aminomethyl) Phenyl sulfonyl) methyl propionate hydrochloride (243 mg, 0.828 mmol) ' EtOH (volume · 2·7 ml), N-methyl-line (〇_218 ml, 1.986 mmol) 158436.doc - 370- 201215609 and finally EDC (190 mg '0.993 mmol). The reaction mixture was stirred at room temperature. LCMS after 75 minutes showed some conversion, which also formed by-products that remained for a longer period of time. LCMS after 3 hours showed more conversion, but not significant. After 3.5 hours, HOBT (6.34 mg, 0.041 mmol) was added. There was no significant difference in LCMS 75 minutes after the addition of HOBT. There was no significant difference in LCMS after overnight. The reaction mixture was slowly diluted with water (8.1 mL). The resulting slurry was stirred at room temperature for 1 hour and then filtered through a 3 〇 mL mesoporous glass Buchner funnel. The solid was washed with water and dried under suction and under a positive pressure of nitrogen to give 3-(4-((furo[2,3-c].pyridin-2-ylamino)methyl) as a white, off-white powder. Phenyl hydrazino) methyl propionate (0.12 § '0.298 〇1111 〇 1,3 6.0% yield). H NMR (400 MHz, DMSO-d6): δ 9.67 (t, J = 6.1 Hz, 1H), 9.05 (s, 1H), 8.47 (d, J = 5.2 Hz, 1H), 7.85 (d, J = 8.4 Hz, 2H), 7.82 (dd, J=5.3, 1.1 Hz, 1H), 7.65 (d, J=0.8 Hz, 1H), 7.60 (d, J=8.4 Hz, 2H), 4.59 (d, J=6.1 Hz, 2H), 3.53 (t, J = 7.2 Hz, 2H), 3.49 (s, 3H), 2.59 (t, J = 7.2 Hz, 2H) ppm. ESMS: 403.03 (M+l). f. 4-((furo[2,3-c]pyridin-2-carboxamido)methyl)benzene sulfinate sodium:

A 25 mL round bottom flask equipped with a magnetic stir bar was charged with 3·(4-((furo[2,3-c]pyridine-2-carboxamido)indolyl)phenylsulfonyl)propionic acid Methyl ester (113 mg, 0.281 mmol) followed by sodium ethoxide (21% by weight at 158436.doc -371 - 201215609

EtOH) (91 mg, 0.281 mm 〇1) was dissolved in Me〇H (volume: 2 in solution). The mixture was stirred at room temperature. The solid dissolved over time. LCMS after 30 minutes showed about 8 〇 85% conversion. After i hours... (10) shows substantially complete conversion. Note · As in the case of a similar aza (4) experiment, no temporary intermediate/byproduct isomerization of SM was observed. After 2 hours LCMS showed complete conversion. After 5 h, the solution was concentrated under reduced nitrogen flow overnight to afford 4-[(((())). ) phenyl) phthalic acid sodium (〇 〇 2 g, 0.301 mmol, 107% yield) NMR (400 MHz, DMSO-d6): S 8.99 (s, 1H), 8 42 (d, J = 5.2 Hz, 1H), 7.76 (dd, J=5.2, 1.1 Hz, 1H), 7·55 (d, J=0.6

Hz, 1H), 7.38 (d, J=8.0 Hz, 2H), 7.25 (d, J=8.1 Hz, 2H), 4.44 (s, 2H) ppm. ESMS: 317.04 (M+l). g. N-(4-(naphthalen-2-ylsulfonyl) nodal)furo[2,3_c]acridine_2_formamide:

To naphthalene-2-carboxylic acid (0·2 Μdioxane, 15 〇, 30 μιηοΐ) and diethyl bismuth oxychloride (0.2 M DMSO, 150 kL, 3 〇μιη〇1) and triethylamine (pure Add 4-((pyrano[2,3-c]pyridine-2-cartoamino)indolyl) phenyl phthalate (混合物.2 M DMSO, 50) to a mixture of '9.3 μί, 67 μιηοΐ) Μί, 10 μιηοΐ) and the reaction was heated overnight at 4 °C. The reaction was cooled to room temperature and partitioned between aqueous EtOAc and EtOAc. The organic layer was separated and deposited on an SCX-SPE cartridge and dissolved in two fractions: the first one was 25% MeOH/EtOAc (v/v) and the second was used in ammonia sterol solution (2 N). The second fractions were concentrated to dryness afforded title title titled *H NMR (400 MHz, CDC13): δ 8.89 (s, 1 Η), 8.56 (d, J=2 Hz, 1H), 8.50 (d, J=5.2 Hz, 1H), 7.99 (m, 3H), 7.92 (d, J=8.8 Hz, 1H), 7.87 (m, 2H), 7.62 (m, 3H), 7.51 (m, 3H), 7.08 (m, 1H), 4.72 (d, J=6.4 Hz, 2H) . LC-MS: 443.22 (M+l).

Example 2P N-(4-(5-(Dimethylamino)pyridazin-2-ylsulfonyl)benzyl)imidazolium hydrazone, 2-a] 0 ratio bite-6-carboxamide

XANTPHOS (0.573 g, 0.990 mmol), Cs2C03 (6.45 g, 19.80 mmol), Pd2 (dba) 3 (0.453 g, 0.495 mmol), 4-(ethylamino-indenyl) benzenesulfinate sodium salt (3.51) g, 14.85 mmol), 5-bromo-N, N-di 158436.doc • 373 · 201215609 Methyl. The mixture of the pyrazin-2-amine (2 g ' 9.90 mmol) in toluene (5 〇 mi) was degassed and heated to 12 Torr. (: </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; 8.03 (s, 1H), 7.87 (d, 2H), 7.38 (d, 2H), 6.11 (b, 1H), 4.45 (d, 2H), 3.21 (s, 6H), 2.16 (s, 3H). · 5-((4-(Aminomethyl)phenyl)sulfonyl)_N,N-dimethyl "pyridazine-2-amine hydrochloride:

3 M HC1 solution (80 ml) with Ν-(4-(5-(dimethylamino)D) than 嗓-2_ sylvestre) benzyl) acetamide (1.6 g) in 2-propane The mixture of the solution in the alcohol (1 ml) was refluxed over the weekend, the solvent was removed, diethyl ether was added, filtered and dried to give the title compound (76%). NMR (DMSO-D6): δ 8.71 (s, 1 Η), 8.H (s, 1H), 7.92 (d, 2H), 7.45 (d, 2H), 4.08 (d, 2H), 3.13 (s, 6H) ). c· N-(4-(5-(Dimethylamino))pyrazine-2-ylsulfonyl)benzyl)imidazo[l,2-a]pyridine-6-cartoamine:

158436.doc • 374 201215609 Adding imidazole to a 250 mL round bottom flask, 1^, 2·^, pyridine (0.592 g, 3.65 mmol), 5-(4-(aminomethyl)phenyl Sulfhydryl)_N,N_didecyl ° 0-0-2-amine hydrochloride (1.2 g, 3.65 mmol) and HBTU (1.522 g, 4.01 mmol), HOBT (0.615 g, 4.01 mmol) and DIEA (3.19)

A solution of mL, 18.25 mmol) in DMF (50 mL). The reaction was stirred overnight and then concentrated under reduced pressure. The residue was diluted with dioxins and washed with a 1 NaOH NaOH 7jc solution. The organic layer was separated and concentrated and purified directly in Biotage to yield 235 mg of N-(4-(5-(dimethylamino)pyrazinylsulfonyl)benzyl)imidazo[1,2-a]pyridine -6-carbamamine (15%). 'H NMR (DMSO-d6): δ 9.21 (t, 1H), 9.13 (s, 1H), 8.67 (s, 1H), 8.12 (s, 1H), 8.95 (s, 1H), 7.86 (d, 2H ), 7.63 (d, 2H), 7.54 (d., 2H), 4.53 (d, 2H), 3.11 (s, 6H). LC-MS: 437.0 (M+l).

Example 2Q N_(4-((3-(Trifluoromethoxy)phenyl)sulfonyl)benzyl)imidazopyridinium-6-carboxamide

NC

K2C03 (4.21 g, 30.4 mmol) was added to a colorless solution of 3-(trifluoromethoxy) thiophenol (5.0 g, 25.8 mmol) in DMF (80 mL) to form 158436.doc - 375 - 201215609 yellow mixture. To this mixture was added 4-fluorobenzonitrile (2 84 g, 23 4 mmol). The mixture was heated to 120 for 16 hours, cooled to room temperature and diluted with 1 N NaOH and EtOAc. Separate the layers. The organic layer was washed sequentially with EtOAc (br.) and brine and dried over Nat. The residue was purified by EtOAc EtOAc (EtOAc) !H NMR (300 MHz, CDC13): δ 8.8-8.06 (m, 2Η), 7.89- 7.80 (m, 2H), 7.78-7.82 (m, 2H), 7.61 (t, 1H), 7.47 (d, 2H ). LC-MS: 295.93 (M+H). b: 4-((3-(Trifluoromethoxy)phenyl)sulfonyl)benzonitrile: 〇 from 〇

Add mCPBA (20.88 g, 91) to a solution of 4-(3-(trifluoromethoxy)phenylthio)benzonitrile (6.09 g, 20.6 mmol) in CH.sub.3 (110 mL). · 0 mmol). The mixture was stirred and slowly warmed to room temperature overnight. The solid was removed by vacuum filtration and rinsed with CHC13. The filtrate was washed with 1 N NaOH (x2). The separated organic layer was washed with w~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~ </ RTI> <RTIgt; LC-MS: 349.90 (M+Na). 158436.doc -376- 201215609 C : (4-((3_(Tri-I)oxy)phenyl)]phenyl)methylamine:

To the vial was added 3 tubes of a pipette of the Mooney Nickel in water and then methanol (2 mL) was added. The washing solvent (Me〇H) was removed via a pipette. The washing was repeated twice more to obtain about 7 equivalents of nickel. To a 5 〇〇 mL Parr reaction cylinder was added 4-(3-(trifluoromethoxy)phenylsulfonyl)benzonitrile (6.00 g, 18.3 mmol) in MeOH (120 mL) The solution was then added with pre-washed nickel, 7 N ammonia (37.2 ml, 26.0 mm 〇i) in MeOH and potassium argon (0.329 g, 5.9 mmol). The mixture was evacuated and purified three times with H2 then hydrogenated overnight at 50 pSi. LC_MS analysis indicated complete hydrogenation of the nitrile. The mixture was filtered through diatomaceous earth. The filtrate was concentrated and purified by EtOAc EtOAc (EtOAc) H NMR (300 MHz, DMSO-d6): δ 7.99-7.91 (m, 4 Η), 7.75-7.73 (m, 3 Η), 7·58 (d, 2 Η), 3·76 (s, 2 Η). LC-MS: 331.97 (M+H). d : N-(4-((3-(tris)methoxy)phenyl)) hydrazino)]] oxazole and u, 2_a] pyrimidine -6-carbamamine:

Imidazo[l,2-a]pyrimidine_6_carboxylic acid (0.739 g, 4.53 mmol), (4-(3-(trifluorodecyloxy)phenylsulfonyl)phenyl)methanamine (1.5 g, 4 S3 158436.doc • 377·201215609 mmol), a mixture of BOP (2.203 g, 4.98 mmol) and DIEA (0.949 mL, 5.43 mmol) in DMF (25 mL) was stirred overnight at room temperature. The reaction mixture was concentrated in the air to remove DMF. The residue was diluted with EtOAc and then washed with 1 N EtOAc. The separated aqueous layer was back extracted with EtOAc. The combined organic extracts were washed with EtOAc EtOAc EtOAc. The title compound (980 mg, 45% yield). </ RTI> <RTIgt; , 7.60 (d, 2H), 4.57 (d, 2H) ° LC-MS: 476.87 (M+l).

Example 2R N-(4-(Benzylsulfonyl)benzylpyroloindole 3,2-(:] acridine-2-indoleamine

:N-(4-(benzylsulfonyl)benzyl)acetamide

Add TBAI (0.157 g, 0.425 mmol) and (methanol) to a solution of sodium 4-(ethylammonium decyl) benzene sulfinate (1 g, 4.25 mmol) in water (12 mL). Benzene (0.742 g, 4.34 mmol). The reaction mixture 158436.doc -378 - 201215609 was heated to 70 ° C for 2 hours. A white solid precipitated. LC-MS analysis showed the main peak to be the desired product. The white solid was filtered and washed with water and diethyl ether to remove TBAI, and then dried under reduced pressure to give 696 mg (yield: The collected solid was used in the next step without further purification. !H NMR (300 MHz, CDC13): δ 7.55 (d, 2Η), 7.33-7.23 (m, 5H), 7.08 (d, 2H), 5.94 (brs, 1H), 4.50 (d, 2H), 4.29 ( s, 2H), 2.07 (s, 3H). LC-MS: 304.12 (M+H). b: (4-(Benzylsulfonyl)phenyl)methanamine hydrochloride

Heat a mixture of N-(4-(benzylsulfonyl)benzyl)acetamide (300 mg, 0.989 mmol) and 3 N HC1 (11.87 ml, 35.6 mmol) in iprOH (ll mL) to 100 ° C. As the temperature increases, the turbid mixture becomes a clear solution. The reaction mixture was stirred at 100 ° C for 16 hours. LC-MS analysis indicated complete hydrolysis. The reaction mixture was allowed to cool to room temperature. White crystals were precipitated and filtered, washed with EtOAc EtOAc (EtOAc) !H NMR (300 MHz, DMSO-d6): δ 8.44 (brs, 3H), 7.75, 7.65 (dd, 4H), 7.29-7.27 (m, 3H), 7.16-7.13 (m, 2H), 4.69 (s , 2H), 4.12 (s, 2H). LC-MS: 262.1 1 (M+H). c : N-(4-(benzylsulfonyl)benzyl)-111-&quot;bibromo[3,2-c]&quot;bipyridin-2-carbamide 158436.doc -379- 201215609

1H-pyrrolo[3,2-c]&quot;bipyridine-2-carboxylic acid (57 2 mg, 〇353 mmol), 1 Η-benzo[d][l,2,3]triazole-1·ol (59 〇mg, 〇437 mmol) and EDC (86 mg, 0.450 mmol) were dissolved in anhydrous thf (4 mL) and then added to the test (0.12 mL '0.7 mmol). The mixture forms a slurry solution. Add DMF (1 mL). After 15 minutes of disruption, add (4_(sodium sulfonyl)phenyl)methanamine hydrochloride (100 mg, 〇.336 melon and Xu's test (0.12 mL, 0.7 mmol) in THF (1 Solution in mL). Heat the reaction mixture and discriminate at 65 C. Then dilute with ethyl acetate (x2). Use 5% aqueous acetic acid (X 1 ), saturated aqueous sodium bicarbonate (χ2) and brine (X 1) Washing the combined organic layers sequentially. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo to give the crude product (65 mg). The crude material was dissolved in DCM and a few drops of MeOH with Biotage Purification to give the desired product (34 mg, EtOAc, EtOAc: EtOAc: EtOAc: EtOAc: , 8.21 (d, 1H), 7.68 (d, 2H), 7.51(d, 2H)} 7.36-7.26 (m, 5H), 7.16-7.13 (m, 2H), 4.63 (s, 2H), 4.59 (d , 2H).

LC-MS: 406·11 (Μ+Η) 〇 Example 2S N-(4-(cyclohexylsulfonyl)benzyl)-lH-&quot;bibromo[3,2-c] acridine-2- Formamide 158436.doc • 380 - 201215609

a : N-(4-(cyclohexylsulfonyl)benzyl)acetamide

To a solution of sodium 4-(ethylguanidinoguanidino)benzenesulfinate (500 mg, 2.126 mmol) in DMSO (8 mL) was added iodocyclohexane (670 mg, 3.19 mmol). The reaction was heated to 100 °C for 48 hours. The reaction mixture was diluted with EtOAc and washed with EtOAc EtOAc. The organics were dried over Na 2 S 4 and concentrated. The crude material was purified by EtOAc to give the desired product (52 mg, 8% yield). lH NMR (300 MHz, CDC13): δ 7.66 (d5 2Η), 7.36 (d, 2H), 6.72 (m, 1H), 4.46 (d, 2H), 2.83 (tt, 1H), 2.04 (s, 3H) , 2.01-2.00 (m, 2H), 1.83-1.76 (m, 3H), 1.65 (d, 1H), 1.93-1.12 (m, 4H). LC-MS: 296.06 (M+H). b: (4-(cyclohexylsulfonyl)phenyl) decylamine

H2N

Heating a mixture of N-(4-(cyclohexylsulfonyl)benzyl)acetamide (52 mg, 0.6 mmol) and 3N HCl (2.11 mL, 6.34 mmol) in 1PrOH (2.5 mL) 1 oo°c. As the temperature increases, the turbid mixture becomes a 158436.doc •381- 201215609 clear solution. The reaction mixture was stirred and refluxed at 1 ° C for 16 h. LC-MS analysis indicated the absence of starting material and some other by-products (the desired product was found to be 22% in HPLC). The mixture was cooled to room temperature and the solvent was concentrated. The resulting slurry was treated with 1 N NaOH and EtOAc. The combined organic extracts were washed with brine, dried and dried then evaporated The crude material was purified by Biotage to give free amine (25 mg, 56% yield). LC-MS: 254.08 (M+H). c : N-(4-(cyclohexylsulfonyl)benzyl)_1Η_β is more than [3,2_c]pyridine 2 indoleamine

Will be 1H-. Bisolo[3,2-c]pyridin-2-decanoic acid (16.80 mg ' 0.104 111111〇1), 11^benzo[[1][1,2,3]triazol-1-ol (17.33 11 ^, 〇.128 mmol) and EDC (25.3 mg, 0.132 mmol) dissolved in dry THF (3 mL). Then added a test (0.7 mL, 0.7 mmol). The mixture formed a slurry. Add DMF (0.5 mL) (6: After stirring for 15 minutes, add (4-(cyclohexylnonyl)phenyl)methylamine (25 mg, 0.099 mmol) in THF / DMF (1. 〇 / 0.3 mL) The solution was stirred at 651 overnight, then diluted with ethyl acetate. The organic layer was washed sequentially with 5% aqueous acetic acid (2), saturated aqueous sodium hydrogen carbonate (2) and brine (s). The title compound (12·4 mg) was obtained from EtOAc EtOAc EtOAc. , 320 / 〇 yield). *H NMR (300 MHz, DMSO-d6): δ 12.05 (brs, 1 Η), 9.30 (t, 1H), 8.88 (s, 1H), 8.16 (d, 1H), 7.76 (d, 2H), 7.54(d, 2H), 7.32 (d, 1H), 7.27 (s, 1H), 4. 57 (d, 2H), 3.08 (m, 1H), 1.78-1.66 (m, 4H), 1.51 (d, 1H), 1.20-0.96 (m, 5H) LC-MS: 398.0 (M+H). It will be appreciated that those skilled in the art will be able to prepare compounds of the invention using methods known in the art, as well as the general synthetic methods described herein. Assay = assay Example 1 Biochemical inhibition assay NAMPT protein purification in E. coli (5. Co/ί) Recombinant His-tagged NAMPT was produced in cells, purified via a Ni column, and further purified via size exclusion column (XTAL Biostructures). NAMPT enzymatic reaction in a 96-well V-shaped chassis in buffer a The NAMPT enzymatic reaction was carried out in (50 mM Hepes pH 7.5, 50 mM NaC 5 mM MgCl 2 and 1 mM THP). Compound titration was carried out in another dilution dish by serial dilution of the compound in DMSO to make a 100 χ stock solution. A buffer containing 33 nM NAMPT protein (89 μM was added to a 1 l〇〇x compound dish containing a control (eg DMSO or blank). Incubate the compound and enzyme mixture for 15 minutes at room temperature, then add 1 〇pL 1 〇χ substrate and cofactor in buffer A to the test well to a final concentration of 1 158436.doc 201215609 NAM, 100 μΜ 5-linoic acid-D-ribose l.dicarboxylate (pRpp) and 2.5 mM adenosine triolate (ATP). The reaction was allowed to proceed at room temperature for 3 minutes, and then quenched by adding 11 pL of a solution of citric acid and L-cystathionine to give a final concentration of 1% decanoic acid and 10 μL of L-cystathion. Quantitative determination of background and signal intensity by adding (or without adding) serial dilutions of hydrazine to pre-quenched enzyme and cofactor mixtures. Quantitative determination of ruthenium reaction products using mass spectrometry-based assays And internal control (L-cystathion). Biocius Lifesciences is used to detect sputum and L-cystathion using the services of the RapidFire system. Briefly, hydrazine and L. cystathionine were combined in a graphite carbon cartridge in 〇·1% citric acid, dissolved in 3 〇% acetonitrile buffer, and injected into a Sciex 4000 mass spectrometer. The components of the sample were ionized by electrospray ionization and the masses of q丨 (mother ion) and Q3 (fragment ion) of positive ions β NMN were detected to be 334 2 and 123_2, respectively. Q1 and Q3 of 匕_cystathion were 223.1 and 134.1, respectively. The fragments were quantified and analyzed by the following methods. Use this method to determine inhibition 〇/〇. The NMN(R) 5 was first corrected to the l-cystathionine signal by dividing the NMN signal of each well by the L-cystathionine signal. The signal from the background hole is averaged and subtracted from the test disk. The inhibition 〇/〇 of the compound-treated cells was then determined by using the following formula. Inhibition % = l〇〇-l〇〇XX/y where X is the average signal of the pores without compound treatment and y is the average signal of the treated wells. 158436.doc 201215609 Use Excel and the following formula to determine IC5Q. IC50=1〇a(LOG10(X)+(((50-% inhibition at compound concentration 1)/(XX-YY)x(LOG10(X)-LOG10(Y))))) where X represents the concentration of the compound 1, Y represents the compound concentration 2, XX represents the % inhibition at the compound concentration 1 (X), and YY represents the % inhibition at the compound concentration 2 (Y). The oxime inhibitor compound of the present invention preferably has less than 1 The IC50 value of μΜ, more preferably less than 0.1 μΜ and optimally less than 0.01 μΜ. The results of the compounds are provided in Table 3. Test Example 2 In vitro cell proliferation assay Α2780 cells were added with and without β-nicotine 醯1 x 103 cells per well in an amine mononucleotide (ΝΜΝ) or nicotinamide (ΝΑΜ) in 180 μL medium (10% FBS, 1% penicillin/streptomycin amphotericin Β, RPMI-1640) The density was inoculated in a 96-well dish. After overnight incubation at 37 ° C and 5% CO 2 , compound titration was performed in a separate dilution dish by serial dilution of the compound in DMSO to make a sputum stock solution. The compound was further diluted to a final concentration of 10 μL, followed by addition of 20 pL of each dilution to the control containing control (eg DMSO and blank) The cells were seeded to a final volume of 200 pL » the final DMSO concentration in each well was 0.1%. The plates were then incubated in a 5% C〇2 incubator at 37 ° C for 72 hours. Subsequent use of sulforaphane B (SRB) assay assesses the number of viable cells. The cells were fixed for 1 hour at 4 ° C by adding 50 30% tri-glycolic acid (TCA) to a final concentration of 6% TCA. The plate was washed four times with H2〇 and Allow to dry for at least 1 hour, after 158436.doc -385-201215609, add 100 pL of 4% SRB in 1% acetic acid solution to each well and incubate for at least 30 minutes at room temperature. Then wash the dish with 1% acetic acid Three times, dried, and treated with 100 pL of 10 mM Tris-alkali solution. The plate was then read at 570 nm absorbance using a micro-dot disc reader. Background was generated on another disk containing only medium. First, the signal from the background disk is averaged, and then the background is subtracted from the test disk. Then, the % inhibition of the compound-treated cells is determined by using the following formula: % inhibition = 100-100xx/y where X represents The average signal of the compound treated cells and y represents the fines treated with DMSO Average signal of the cell. Formula for determining the ICso value of the dish: IC50=10A(LOG10(X) + (((50-% inhibition at compound concentration 1)/(XX-YY)x(LOG10(X)- LOG10(Y)))) wherein X represents the compound concentration 1, Y represents the compound concentration 2, XX represents the % inhibition at the compound concentration 1 (X), and YY represents the % inhibition at the compound concentration 2 (Y). Specificity of cytotoxicity The inhibition of sputum can be reversed by the addition of strontium or barium. The specificity of the compound is determined in the presence of the compound and hydrazine or hydrazine via a cell viability assay. The method of the above is used to determine the percent inhibition. The oxime inhibitor compound of the present invention has an IC50 value of preferably less than 1 μΜ, more preferably less than 0.1 μΜ, and most preferably less than 0.01 μΜ. The most 158436.doc of the present invention •386-201215609 The best compound is that the enzymatic IC5 0 value and the A2780 IC5 0 value are both less than 1 μΜ, and both of the two values are less than 0.1 μΜ and the best two values are less than 0.01 μΜ. Compound. The results of the compounds are provided in Table 3. Table 3 IUPAC name biochemistry IC50~M) A2780 ΙΟ50(μΜ) (Ε)-2-cyano-3-({4-[(5-fluoro-2-decyloxyphenyl)amine sulfonyl]benzene }}methyl)-1-(bite-4-yl) vein 0.0011 0.0030 5-hydroxy-indole-({4-[(4-phenylphenyl)sulfonyl]phenyl}methyl)-1Η-吲哚-2-carbamamine 0.1-1 1-10 5-hydroxy-indole-[(4-{[3-(TM#-4-yl)benzene]sulfonyl}phenyl)methyl]-1Η -吲哚-2-carbamamine 0.1-1 1-10 5-hydroxy-indole-indole (4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)indenyl]- 1Η-吲哚-2-carboamine 0.1-1 1-10 5-hydroxy-indole-[(4-{[3-(pyrrole-1-yl)benzene]sulfonyl}phenyl)methyl] -1Η-吲哚-2-nonylamine 0.1442 0.1-1 5-hydroxy-indole-{[4-(1-indolyl-1Η-carbazole-4-ylindolyl)phenyl]methyl}-1Η -吲哚-2-carboamine 0.1-1 &gt;1.0 5-Ν-({4-[(3,5-difluorophenyl)sulfonyl)phenyl}indenyl)pyridine-2,5-di Indoleamine 1-10 0.661 6-Amino-indole-({4-[(3,5-difluorophenyl)sulfonyl]phenyl}methyl)-l-pyridyl-3-caraamine 0.0142 0.275 Ν-( {4-[(2,3,6-Trimethoxybenzene) continuation]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridin-5-decylamine 0.0797 0.0663 N -({4-[(2,3,6-trimethoxybenzene)) Phenyl}methyl)furan p,3-c]pyridin-2-indoleamine 0.0399 0.0667 N-({4-[(2,3-difluoro-6-decyloxybenzene)sulfonyl]benzene }}methyl)-1Η-pyrrolo[3,2-c]pyrodo-2-cartoamine 0.204 0.0849 N-({4-[(2,3-difluorobenzene) continuation)]phenyl} Mercapto)-1Η-&lt;oxazolo[3,4-b] ° ratio biting-5-anthracene amine 0.0820 0.2786 N-({4-[(2,3-dimethoxy-5-methylbenzene) Sulfo]phenyl]methyl)-1Η-pyrazolo[3,4-b]pyridin-5-carboxamide 0.1462 0.0586 N-({4-[(2,3-dimethoxy) -5-mercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.0152 0.007 N-«4-[(2,3-dimethoxy) Base _5_mercaptobenzene) 醯 】 】 phenyl}methyl) imidazo[l,2-a] pyridine-6-carbenamide 0.0042 0.0156 N-(H-[(2,3-dioxin) Oxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 0.123 0.0833 N-({4-[(2,3-)曱oxyphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0117 0.0049 158436.doc •387. 201215609 N-({4-[ (2,3-dimethoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0093 0.0136 N-({4-[(2,3) -dimethyl Benzene)sulfonyl]phenyl}methyl)imidazo[1,2-a] pyridine-6-cartoamine 0.0687 0.0249 N-({4-[(2,3-dimethoxybenzene)) Sulfhydryl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-formamide 0.0176 0.0776 N-({4-[(2,3-dimethylphenyl)sulfonyl]benzene })methyl)furo[2,3-c]pyridine-2-carboxamide 0.0516 0.008 N-({4-[(2,3-dimethylphenyl)sulfonyl]phenyl}methyl) Imidazo[1,2-a]pyridine-6-carboxamide 0.0433 0.00985 N-({4-[(2,3-dimethylphenyl) hydrazino]phenyl}methyl)imidazo[1, 2-a]pyrimidin-6-nonylamine 0.0041 0.0469 N-({4-[(2,4,5-trimethylbenzene) continuation]phenyl}indenyl)-1Η-&quot; [3,4-b]pyridin-5-decylamine 0.0313 0.0193 N-({4-[(2,4,5-tridecylbenzene) hydrazino]phenyl}indolyl)furan[2, 3-c]Pyridin-2-carboxamide 0.0091 0.0141 N-({4-[(2,4,5-trimethylbenzene))]phenyl}indolyl) odor and spit [l, 2 -a]&quot;Bite-6-carbamamine 0.00934 0.0141 N-({4-[(2,4,5-trimethylbenzene))]phenyl}indolyl)imidazo[l,2 -a]pyrazine-6-carbamide 0.0069 0.0240 N-({4-[(2,4,6-trimethylbenzene)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3 ,4-b] Pyridin-5-formamide 0.136 0.1-1 N-({4-[(2,4,6-trimethylbenzene))]phenyl}indolyl)furan[2,3-c]nt Pyridyl-2-carboxamide 0.0592 0.1-1 N-({4-[(2,4,6-trimethylphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine Bite-6-carbamamine 0.0288 0.1-1 N-({4-[(2,4-Dichloro-3-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-&quot;Biazole And [3,4-b]pyrodo-5-carbamide 0.02 0.0147 N-({4-[(2,4-dioxa-3-methoxybenzene)sulfonyl]phenyl}fluorenyl) Furano[2,3-c]pyrodo-2·carbamamine 0.0177 0.0162 N-({4-[(2,4-dioxa-3-methoxybenzene)sulfonyl]phenyl}methyl Imidazo[l,2-a]pyridine-6-formamide 0.0311 0.013 N-({4-[(2,4-dioxa-3-methoxybenzene)nonyl]phenyl}fluorenyl) Imidazo[l,2-a]pyrimidine-6-carbenamide 0.0066 0.0255 N-({4-[(2,4-dioxa-3-methoxybenzene)sulfonyl]phenyl}- Thio[2,3-c]pyridine-2-carboxamide 0.0051 0.0067 N-({4-[(2,4-difluorobenzene))]phenyl}methyl)imidazo[l ,2-a]&quot;Bite- 6-Protonamine 0.0283 0.0281 N-({4-[(2,4-Dioxaoxybenzene)sulfonyl]phenyl}methyl)-lH-nfcazole And [3,4-b]pyrodo-5-carbamamine 0.1744 0.0447 N-({4-[(2,4-Dioxaoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] pyridyl-6-carboxamide 0.0582 0.0151 N- ({4-[(2,4-Dimethoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-decylamine 0.0045 0.0016 158436.doc -388· 201215609

N-({4-[(2,4-Dimercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4_ b]pyridine-5-decylamine 0.0612 0.0716 N -({4-[(2,4-Dimercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-decylamine 0.0218 0.024 N-({4- [(2,4-Dimercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]» than bite-6-formamide 0.0216 0.0321 N-({4-[(2 ,4-dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0021 0.0492 N-({4-[(2,5-difluoro) Benzenesulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.1-1 0.3921 N-«4-[(2,5-dimethoxy Alkyl) phenyl]methyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-nonylamine 0.0398 0.0248 N-({4-[(2,5-dioxin) Oxylbenzene) hydrazino-l-phenyl}methyl)furo[2,3-c]pyridin-2-decylamine 0.0114 0.0063 N-({4-[(2,5-dimethoxybenzene)) Sulfhydryl 1 phenyl}methyl)imidazo[l,2-a] Π比 bit-6-cartoamine 0.0202 0.0128 Ν_({4_[(2,5-dimethoxybenzene)sulfonyl] Phenyl}methyl)isoxazo[l,2-a] bite-6-cartoamine 0.0069 0.0457 N-({4-[(2,5-dimercaptophenyl)sulfonyl]phenyl} Methyl)-1Η-咕And [3,4-b]pyrodo-5-decylamine 0.0209 0.0172 N-({4-[(2,5-dimercaptophenyl)sulfonyl]phenyl}methyl)furan[2, 3-c]&quot;Bistidine-2-decylamine 0.0181 0.0239 N-({4-[(2,5-Dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2- a] lysyl-6-carbamamine 0.0293 0.0154 1^-({4-[(2,6-dichloro-3-indolylbenzene)) phenyl] fluorenyl) ,3-c]pyrazole-2-carboxamide 0.0108 0.0162 N-({4-[(2,6-dichloro-3-methylphenyl)sulfonyl]phenyl}indolyl) 1,2-a]pyrimidine-6-methanamine 0.0073 0.0560 N-({4-[(2,6-Dichloro-3-methylphenyl)sulfonyl]phenyl}indolyl)thieno-p, 3-c]Pyridin-2-indole amine 0.0044 0.0082 N-({4-[(2,6-dioxabenzene)sulfonyl]phenyl}indolyl)-1Η-carbazolo[3, 4-b] Pyridin-5-decylamine 0.1795 1-10 N-({4-[(2,6-dioxabenzene)sulfonyl]phenyl}methyl)-1Η-"pyrylene[3 ,2-c]p-pyridin-2-carboxamide 0.0447 0.0135 Bucket ({4-[(2,6-two gas stupid))] phenyl} fluorenyl) furan oxime, 3-(:] Acridine-2-carbamide 0.0124 0.0601 N-({H(2,6-dichlorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyro- 6- formazan Amine 0.0012 0.0188 N-({4- [(2,6-di-benzene) continued thiol-phenyl}indolyl)imidazo[1,2-a]pyrimidine- 6-carboxamide 0.0134 0.1-1 N-({4-[(2 ,6-dichlorobenzene) continued fluorenyl]phenyl}methyl)thieno[2,3-c]pyridyl-2-carbamide 0.0076 0.0182 N-({4-[(2,6-dioxin) Oxy-4-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-blpyridine-5-carboxamide 0.1-1 0.1-1 158436.doc -389 - 201215609 N-({4-[(2,6-Dimethoxy-4-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0050 0.0230 N-({4-[(2,6-Dimethylbenzene) fluorenyl]phenyl}indolyl)-1Η-oxazolo[3,4-b]pyridin-5-carboxamide 0.159 0.1-1 N-({4-[(2,6-dimethylphenyl)cannonyl]phenyl}methyl)furo[2,3-cI acridine-2-cartoamine 0.0323 0.1-1 N-({4-[(2-Ethylbenzene))]phenyl}methyl)-1Η-η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0036 0.0114 N- ({4-[(2-Ethylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]acridine-2-ylguanamine 0.0057 0.0065 N-({4-[( 2-Ethyl phenyl) sulfonyl phenyl] phenyl}methyl) imidazo[l,2-a] pyrimidine- 6-formamide 0.0025 0.0082 N-({4-[(2-butoxy-) 4-fluorobenzene)sulfonate Phenyl}methyl}methyl)-1Η-indolezolo[3,4-b]pyridine_5-formamide 0.176 0.1-1 N-({4-[(2-butoxy-4-fluoro) Benzenesulfonyl]phenyl}methyl)-1Η·-pyrolo[3,2-c]pyridine-2-carboxamide 0.0311 0.0055 N-({4-[(2-butoxy-4) -fluorobenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0335 0.0665 N-({4-[(2-butoxy-4-fluorobenzene) Sulfhydryl]phenyl}indolyl)imidazo[1,2-a] pyridyl-6-carboxamide 0.0512 0.0062 N-({4-[(2-butoxy-4-fluorobenzene)sulfonate Thio[phenyl]indenyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0073 0.0738 N-({4-[(2-butoxy-4-fluorobenzene)sulfonyl] Phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0070 0.0063 N-({4-[(2-butoxy-5- gasbenzene)sulfonyl]phenyl} Methyl)-1Η-indolozolo[3,4-b]pyridine-5-carboxamide 0.117 0.0737 N-({4-[(2-butoxy-5-gasbenzene)sulfonyl]benzene }}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0156 0.0083 N-({4-[(2-butoxy-5- benzene)sulfonyl] Phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0243 0.0663 Ν-({4·[(2·butoxy·5_chlorobenzene)sulfonyl]phenyl}曱基) Isozo[1,2-a] 11 is more than -6-carbamamine 0.0110 0.0080 N-({4-[(2-butoxy-5-chlorophenyl)sulfonyl]phenyl}methyl) Imidazo[1,2-a]pyrimidine-6-carboxamide 0.0037 0.0628 N-({4-[(2-Butoxy-5-chlorophenyl)sulfonyl]phenyl}methyl)thiophene [ 2,3-c] Pyridin-2-carbamide 0.0073 0.0100 N-({4-[(2-Butoxy-6-fluorobenzene)sulfonyl]phenyl}methyl)-1Η-« And [3,2-c]"pyridin-2-carboxamide 0.0088 0.0056 N-({4-[(2-butoxy-6-fluorobenzene)sulfonyl]phenyl}methyl)furan [2,3-c]pyridine-2-carboxamide 0.0256 0.0698 N-({4-[(2-butoxy-6-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[l, 2-a] Pyridine-6-formamide 0.0053 0.0069 Ν-({4·[(2_气-3-fluorobenzene)sulfonyl]phenyl}methyl)-1Η-&quot;Bizozolo[3 ,4-b]pyridine-5-carboxamide 0.0736 0.1-1 •390- 158436.doc 201215609

N-({4-[(2-chloro-3-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]»ifc bite 2-formylamine 0.0170 0.0611 N-( {4-[(2-Ga-4-fluorophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]»tt^- 2-carboxamide 0.0178 0.0634 N-({4- [(2-Chloro-4-fluorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0144 0.1-1 N-({4-[(2 - gas-4-decyloxybenzene)sulfonyl]phenyl}indolyl)-1Η-carbazolo[3,4-b]» than bite-5-carbamide 0.0516 0.0877 N-({4- [(2-Ga-4-oxooxybenzene)sulfonyl]phenyl}methyl)-lH-«th-[3,2-c]pyridin-2-carboxamide 0.0093 0.0145 N-( {4_[(2-chloro-4-inoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a] ° ratio biting-6-formamide 0.0167 0.0114 N-({4 -[(2-chloro-4-indolylbenzene)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0065 0.0669 N-({4-[( 2-Chloro-4-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-cartoamine 0.0027 0.0055 N-({4-[(2-gas) -4-mercaptobenzene) continued fluorenyl]phenyl}methyl)-m-&quot; 嗤[[,4-b]pyridine-5-decylamine 0.005 0.00278 N-({4-[(2 -chloro-4-methylbenzene)sulfonyl 1phenyl} )_1H-pyrrolo[3,2·c]0 ratio bite-2_nonylamine 0.0080 0.0027 N-({4-[(2-Ga-4-methylphenyl)sulfonyl]phenyl}fluorenyl) Furan[2,3-c]nfc pyridine-2-carboxamide 0.0141 0.0142 N-({4-[(2-Ga-4-methylphenyl)sulfonyl]phenyl}methyl)imidazolium [l,2-a]nb bite-6-formamide 0.11 0.0009 N-({4-[(2- gas-4-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l, 2-a] pyrimidine-6-formamide 0.0015 0.0007 N-({4-[(2-Ga-4-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-small Bipyridine-2-carboxamide 0.0249 0.0016 N-({4-[(2-Gas-S-fluorobenzene))indolyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine -2-carboxamide 0.0281 0.0121 N-({4-[(2-Ga-5-fluorobenzene)sulfonyl]phenyl}methyl)furo[2,3-cInb bite-2-formamide 0.0163 0.0248 Ν-({4-[(2·Ga-5-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[1,2-small ratio bite- 6-carbenamide 0.0210 0.0063 Ν-( {4-[(2-Ga-5-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0105 0.0530 N-({4-[ (2-Ga-5-fluorobenzene)sulfonyl-1phenyl}methyl)thieno[2,3-small-bite-2-carbamide 0.0042 0.0057 N-({4-[(2-gas-) 5-oxo oxygen Benzenesulfonyl]phenyl}methyl)-1Η-carbazolo[3,4-b]pyridin-5-formamide 0.0247 0.0668 N-({4-[(2-gas-5-oxime) Alkyl)phenyl]mercapto)-1H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0110 0.0097 N-({4-[(2-chloro-5-) Oxybenzene)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridine-2-carboxamide 0.0026 0.0206 158436.doc -391 - 201215609 N-((4-[(2-) -5-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] 咬"bit-6-carbamamine 0.0056 0.0027 N-({4-[(2-气- 5-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0061 0.0515 N-({4-[(2-gas-5-曱) Oxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0049 0.0053 N-({4-[(2-Ga-5-methylbenzene)) Sulfomethyl Iphenyl}methyl)-1Η-oxazolo[3,4-blpyridine-5-cartoamine 0.0602 0.0659 N-({4-[(2-Ga-5-methylbenzene)) Mercapto]phenyl}methyl)-1Η-»Λ[3,2-c]pyridine-2-cartoamine 0.0188 0.0091 Ν-({4-[(2-gas-5-mercaptobenzene)) Sulfhydryl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0178 0.0149 N-({4-[(2-chloro-5-methylphenyl))sulfonate Phenyl}methyl)imidazo[l,2-a]&quot;Bite-6-carbamamine 0.0056 0.0046 N-({4-[(2-chloro-5-methylphenyl))sulfonyl) Phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0057 0.0225 N-«4-[(2·5-nonylbenzene)sulfonyl]phenyl} Thio[2,3-c]^b pyridine-2-decylamine 0.0022 0.0049 N-({4-[(2-gas-6-fluorobenzene)sulfonyl]phenyl}methyl)- 1Η-〇比比和[3,2-c]pyridine-2-carboxamide 0.1142 0.0371 Ν-({4-[(2·chloro-6-fluorobenzene)sulfonyl]phenyl}indolyl)imidazole And [l,2-a]&quot;Bite- 6-carbamide 0.1722 0.0766 N-({4-[(2-Ga-6-methoxybenzene)sulfonyl]phenyl}methyl)furan And [2,3-c]pyridine-2-carboxamide 0.0167 0.0214 N-({4-[(2-gas-6-methoxybenzene))]phenyl}methyl)imidazo[l ,2-al σ ratio bite-6-decylamine 0.0202 0.0258 Ν-({4-[(2-gas-6-methoxyphenyl)sulfonyl]phenyl}methyl)thiophene p,3- c] pyridine-2-carbamide 0.0027 0.0029 N-({4-[(2-chlorophenyl)sulfonyl]phenyl}methyl)-1Η-»biszolo[3,4-b]« Acridine-5-carbamamine 0.0925 1-0.1 Ν-({4·[(2·Gas Benzene) fluorenyl]phenyl}methyl)imidazo[l,2-a] pyridine- 6-carbamide 0.0241 0.0567 沁({4-[(2-chlorophenyl)sulfonyl]phenyl}methyl)thiophene [2,3-decene-2-carbamide 0.0024 0.0066 N-( {4-[(2-Cyanophenyl) fluorenyl]phenyl}methyl)-1Η-»Bizozolo[3,4-b] «Bistidine-5-cartoamine 0.131 0.1-1 N- ({4-[(2-Cyanophenyl)sulfonyl]phenyl}methyl)-1Η-. Bisolo[3,2-c]»tb pyridine-2-meramine 0.0253 0.0629 N-({4-[(2-cyanobenzene) hydrazino]phenyl}methyl)furan[2, 3-c]nb-pyridine-2-carbamide 0.0246 0.0635 N-({4-[(2-cyanobenzene))]phenyl}methyl)imidazo[l,2-a]»tb bite -6-carbamamine 0.0156 0.0613 N-({4-[(2-cyanobenzene) fluorenyl]phenyl}fluorenyl)thieno[2,3-c]nt-2-ylcarboxamide 0.0676 158436.doc .392. 201215609

N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0863 0.0670 N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-«bido[3,2-c]&quot;bipyridine-2 -carbamamine 0.0034 0.0018 N-({4-[(2-ethoxy-4-1benzene)sulfonyl]phenyl}indolyl)furan p,3-c]pyridine-2-carboxamide 0.0077 0.0069 N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a] pyridine-6-carboxamide 0.0314 0.0015 N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-cartoamine 0.0071 0.0143 N-( {4-[(2-Ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)thienoindole 2,3-c]pyridin-2-decylamine 0.0038 0.0009 N-({4- [(2-Ethoxy-6-fluorophenyl)sulfonyl]phenyl}methyl)furan p,3-cl Pyridine-2-carboxamide 0.0170 0.0283 N-({4-[(2-B) Oxybenzene)sulfonyl]phenyl}indolyl)-1Η-oxazolo[3,4-b] octa-5-carbamamine 0.0493 0.0269 Ν-({4-[(2-ethoxybenzene) Sulfhydryl]phenyl}indolyl)furo[2,3-c-pyridyl-2-mercaptoamine 0.0659 0.006 N-({4-[(2-ethoxyphenyl)indolyl]phenyl } Mercapto) imidazo[l,2-a] bite- 6-formamide 0.0203 0.00339 N-({4-[(2-ethoxyphenyl) hydrazino]phenyl}methyl)imidazo[ l,2-a]pyrimidine- 6-formamide 0.0010 0.0071 N-({4-[(2-ethylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4 -b]pyridine-5-formamide 0.0084 0.013 N-({4-[(2-ethylbenzene) hydrazino]phenyl}indolyl) furan [2,3-ten ratio bite-2-A Indoleamine 0.0054 0.0129 N-({4-[(2-ethylbenzene) hydrazino]phenyl}methyl)imidazo[l,2-a]pyro-6-carbamamine 0.0302 0.0129 N-( {4-[(2-ethylbenzene) decyl]phenyl}methyl)carbazolo[1,2-a]pyrimidine-6-carbamamine 0.0025 0.0249 N-({4-[(2 -Fluoro-3-methoxybenzene)sulfonyl]phenyl}indolyl)-1Η-oxazolo[3,4-b]pyridine-5-carboxamide 0.0086 0.0563 N-({4-[( 2-fluoro-3-indolyl benzene) sulfonyl]phenyl}methyl)imidazo[l,2-a] pyridine-6-decylamine 0.033 0.0135 N-({4-[(2- Fluoro-3-methylbenzene)sulfonyl]phenyl}indenyl)-1Η-°biazo[3,4-b]pyrodo-5-cartoamine 0.0197 0.0239 N-({4-[( 2-fluoro-3-methylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0758 0.0070 乂({4-[(2- -3-mercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-decapyridin-2-ylamine 0.0063 0.0079 N-({4-[(2-fluoro_3_A) Benzo)sulfonyl]phenyl}indolyl]imidazo[1,2-a]pyridin-6-carboxamide 0.0075 0.0033 N-({4-[(2-fluoro-3-indolylbenzene)sulfonate Mercapto]phenyl}methyl)imidazo[1,2-alpyrimidine-6-nonylamine 0.0032 0.0215 158436.doc -393· 201215609 N-({4-[(2-fluoro-3-methylbenzene) Continuation of thiol]phenyl}indenyl)thieno[2,3-c]acridin-2-carboxamide 0.0107 0.0033 N-({4-[(2-fluoro-4-methoxybenzene)) Mercapto]phenyl}methyl)-lH-nboxazolo[3,4-b]pyridine-5-decylamine 0.1203 0.2067 N-({4-[(2-fluoro-4-methoxybenzene)) Sulfonic acid]phenyl}methyl)imidazo[l,2-a]pyridin-6-carboxamide 0.0413 0.0229 N-({4-[(2-fluoro-4-mercaptophenyl))] Phenyl} fluorenyl) benzoate and [2,3-decapyridin-2-carboxamide 0.0123 0.0253 N-({4-[(2-)-methylphenyl)sulfonyl]phenyl} Mercapto) imidazo[l,2-a]&quot;pyridin-6-cartoamine 0.0214 0.0247 N-({4-[(2-Ga-4-methylphenyl)sulfonyl 1phenyl}曱) Imidazo[l,2-a]pyrimidine-6-formamide 0.0063 0.0614 N-({4-[(2-fluoro-5-methoxybenzene)sulfonyl]benzene } Methyl) -1Η-. Bisazo[3,4-b]pyridine-5-carboxamide 0.139 0.1-1 N-({4-[(2-fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl) -lH-nt-[3,2-c]pyridine-2-carboxamide 0.0778 0.0144 N-({4-[(2-fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl Furano[2,3-c]pyridine-2-carboxamide 0.0268 0.0637 N-({4-[(2-fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl)imidazolium [l,2-a]pyridine-6-formamide 0.0047 0.0128 N-({4-[(2-fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[1, 2-a] 咬--6-carbamamine 0.0104 0.0629 N-({4-[(2-fluoro-5-methoxyphenyl)wall ]]phenyl}methyl)thiophene P,3-c Pyridine-2-cartoamine 0.0023 0.0128 N-({4-[(2-Fluoro-5-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-carbazolo[3,4-b Pyridine-5-formamide 0.0241 0.0716 N-({4-[(2-fluoro-5-methylphenyl)sulfonyl]phenyl}indolyl) furan [2,3-c]nt a 2-carbamide 0.0059 0.0134 N-({4-[(2-fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-A Indoleamine 0.0068 0.0275 N-({4-[(2-Fluoro-6-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide 0.0541 0.0264 N -({4-[(2-fluoro-6-propoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0133 0.0142 N-({ 4-[(2-Fluoro-6-propoxybenzene) hydrazino]phenyl}methyl) oxazole [l,2-al σ ratio bite-6-formamide 0.0914 0.0010 Ν-({4 -[(2-fluoro-6-propoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-carboxamide 0.0115 0.0293 N-({4-[ (2-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-indolyl-2-carbamamine 0.0418 0.1-1 N-({4-[(2-甲烧醢) Benzo)sulfonyl]phenyl}methyl)-lH-nboxazol[3,4-b]pyrodo-5-carboxamide 0.2022 0.1-1 N-({4-[(2-A Continuation of mercaptobenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0542 0.1-1 158436.doc -394- 201215609

N-({4-[(2-methoxy-5-methylphenyl)sulfonyl]phenyl}methyl)-1Η-&quot;Bizozolo[3,4-b]pyridine-5-A Indoleamine 0.0563 0.0244 N-({4-[(2-methoxy-5-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-decylamine 0.0133 0.0068 N-({4-[(2-Methoxy-5-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6-decylamine 0.0431 0.0117 N-({4-[(2-methoxy-5-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-8] shouting-6-decylamine 0.0039 0.0072 N -({4-[(2-decyloxybenzene)sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 0.0683 0.0618 N-({ 4-[(2-methoxyphenyl) hydrazino 1 phenyl}methyl)furo[2,3-c]pyro- 2- decylamine 0.0189 0.0265 N-({4-[(2- Methoxybenzene) hydrazino]phenyl}mercapto)imidazo[1,2-a]pyro- 6-decylamine 0.0265 0.0153 N-({4-[(2-methoxybenzene)) Mercapto]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-decylamine 0.0039 0.0747 N-({4-[(2-methyl-4-propoxybenzene)sulfonate) ]]phenyl}methyl)-1Η-&quot;Bizozolo[3,4-b]pyrodo-5-decylamine 0.0644 0.0794 N-({4-[(2-methyl-4-propoxy) Benzo sulfonate Mercapto]phenyl}methyl)-lH-nfc-[3,2-c]pyridin-2-carboxamide 0.0305 0.0221 N-({4-[(2-methyl-4-propoxy) Benzene sulfonyl]phenyl}indenyl)furo[2,3-c]pyridin-2-decylamine 0.0225 0.0596 N-({4-[(2-methyl-4-propoxybenzene)) Sulfhydryl]phenyl}methyl)imidazo[1,2-a]pyrazine-6-nonylamine 0.0092 0.0133 N-({4-[(2-methyl-4)propoxybenzene)sulfonate醯基]phenyl}mercapto)imidazo[1,2-a] 峨-6-carbamamine 0.0100 0.0518 N-({4-[(2-mercapto-4-propoxybenzene)sulfonate) Thio[2,3-c]pyridin-2-decylamine 0.0129 0.0017 N-({4-丨(2-mercaptophenyl)sulfonyl]phenyl}methyl) -1Η-«Bizozolo[3,4-b]nb pyridine-5-carbamidamine 0.0926 1-0.1 N-({4-[(2-mercaptophenyl)sulfonyl]phenyl}fluorenyl) Furano[2,3-c]&quot;bipyridin-2-decylamine 0.0152 0.0433 N-({4-[(2-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[1, 2-a]»比比-6- 甲甲胺0.0669 0.0912 N-({4-[(2-phenoxybenzene)sulfonyl]phenyl}fluorenyl)-111- 吐 并 [3,4 -b] 0 than bite-5-decylamine 0.1-1 0.1-1 N-({4-[(2-phenoxybenzene)sulfonyl)phenyl phenylmethyl)furan[2,3- Cl&quot; than bite - 2- Guanamine 0.0204 1-10 N-({4-[(2-phenoxybenzene) hydrazino]phenyl}indolyl)imidazo[l,2-a]pyrene-bite- 6-carboxamide 0.0636 0.0607 N-({4-[(2-phenoxyphenyl) fluorenyl]phenyl}methyl)imidazo[l,2-a]pyrimidine- 6-decylamine 0.0085 0.1-1 N-( {4-[(3,4-Dichlorobenzene) continued fluorenyl]phenyl}indolyl)-1Η-tonoxazolo[3,4-b] 0 ratio biting-5-carboxamide 0.0067 0.0055 158436.doc -395 - 201215609 N-({4-[(3,4-dioxabenzene) fluorenyl]phenyl}methyl)furo[2,3-c]pyridine-2-carbamide 0.0104 0.0048 N- ({4-[(3,4-dioxabenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine- 6-formamide 0.0015 0.0017 N-({4-[ (3,4-difluorobenzene)sulfonyl]phenyl}indenyl)-1Η-&quot;Bizozolo[3,4-b] pyridine-5-carbamamine 0.0542 0.0289 N-({4- [(3,4-difluorobenzene) hydrazino]phenyl}methyl)furan [2,3-decene bite 2-formylamine 0.0168 0.013 N-({4-[(3,4- Difluorobenzene) phenyl]methyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0041 0.0363 N-({4-[(3,4-dimethoxybenzene) Continuation of hydrazino]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyrodo-5-carbamamine 0.0206 0.0056 N-({4-[(3,4-dimethoxy) benzene Continuation of fluorenyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0062 0.0038 N-({4-[(3,4-dimethoxybenzene)sulfonyl) Phenyl}methyl)imidazolium ,,2-a] pyridine-6-carboxamide 0.012 0.00251 N-({4-[(3,4-dimethoxyphenyl)sulfonyl]phenyl }曱基)imidazo[l,2-a] pyrimidine-6-nonylamine 0.0029 0.0073 N-({4-[(3,4-dimethylphenyl)indolyl]phenyl}methyl) -1Η-oxazolo[3,4-b]pyridine-5-formamide 0.0051 0.0034 N-«4-[(3,4-dimethylphenyl) decyl]phenyl}methyl)furan [2,3-c]pyridine-2-carboxamide 0.0150 0.003 N-({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2- Ap ratio pyridine-6-formamide 0.0111 0.00297 N-({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6 -carbamamine 0.0001 0.0016 N-({4-[(3,5-di-benzene) hydrazino]phenyl}methyl)·1Η_&quot;Bizozolo[3,4-b]pyridine-5-A Indoleamine 0.0067 0.0021 N-({4-[(3,5-di-benzene) 醯 醯 丨 丨 } } } } « « « « « 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 Amine 0.001 0.0004 N-({4-[(3,5-dioxabenzene) contigyl)phenyl}methyl)imidazo[1,2-a]pyridine-6-carboxamide 0.0 0549 0.00128 N-({4-[(3,5-Difluorophenyl)sulfonyl]phenyl}methyl)-1Η-indolezolo[3,4-b]pyridine-5-carboxamide 0.008 0.007 N-({4-[(3,5-Difluorobenzene)-decyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-carboxamide 0.006 0.0015 N-({4 -[(3,5-difluorophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine- 6-cartoamine 0.002 0.003 N-«4-[(3,5 -dimethoxybenzene) phenyl]methyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-cartoamine 0.0026 0.0022 N-({4-[(3,5) -dimethoxybenzene)sulfonyl 1phenyl}methyl)-1Η-&quot;Biloxa[3,2-c]pyridine-2-cartoamine 0.0044 0.0015 N-({4-[(3 ,5-dimethoxybenzene) continued fluorenyl]phenyl}methyl)furo[2,3-c]pyridin-2-decylamine 0.0027 0.0017 •396· 158436.doc 201215609

N-({4-[(3,5-Dimethoxybenzene)] fluorenyl 1 phenyl} fluorenyl) imidazo[l,2-a] pyridine-6-nonylamine 0.0032 0.0015 N-( {4-[(3,5-Dimethoxybenzene) hydrazino]phenyl}indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0024 0.0016 N-({4-[ (3,5-dimethoxybenzene) hydrazino]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0013 0.0009 N-({4-[(3,5) - 曱 曱 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) 5-dimethylbenzene) hydrazino]phenyl}fluorenyl)furo[2,3-c]pyridin-2-indoleamine 0.0167 0.0028 N-({4-[(3,5-didecyl) Benzene sulfonyl]phenyl}mercapto)imidazo[l,2-a]-specific bite-6-formamide 0.00676 0.00317 N-({4-[(3,5-dimethylbenzene) continued Mercapto]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-carbenamide 0.0017 0.0020 N-({4-[(3-ethylindenylbenzene) hydrazino]phenyl} Mercapto)-lH-carbazolo[3,4-b]pyridin-5-decylamine 0.0100 0.0129 N-({4-[(3-ethylhydrazinobenzene)-decyl]phenyl}fluorenyl) Furano[2,3-c]pyridin-2-ylamine 0.0176 0.008 N-({4-[(3-ethylmercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[ 1,2-a]pyridine- 6-decylamine 0.0125 0.00637 N-({4-[(3-ethylmercaptophenyl) hydrazino]phenyl}indolyl)imidazo[1,2-a] Pyrimidine bite - 6-decylamine 0.0018 0.0105 N-({4-[(3-butoxybenzene) hydrazino]phenyl}methyl)-1Η-indolezolo[3,4-b]pyrr Bite-5-carbamamine 0.0384 0.0675 N-({4-[(3-butoxybenzene)sulfonyl]phenyl}methyl)-1Η-&quot;比比和[3,2-c] bite -2-cartoamine 0.0115 0.0216 Ν-({4-[(3-butoxybenzene) continuation hydrazino]phenyl} fluorenyl) furo[2,3-c]pyro- 2-nonylamine 0.0123 0.0695 N-({4-[(3-Butoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a] bite- 6-decylamine 0.0047 0.0180 N-({ 4-[(3-butoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-deca-indole-2-ylamine 0.0033 0.0387 N-«4-[(3-chloro- 2_fluorobenzene)sulfonyl]phenyl}indolyl)furan [2,3-decene bite 2-formylamine 0.0109 0.0128 N-({4-[(3-chloro-2-fluorobenzene)) Sulfhydryl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carbamide 0.0024 0.0176 N-({4-[(3-chloro-2-indolyl)benzenesulfonate) Phenyl]phenyl}indolyl)pyrano p,3-c]pyridine-2-carboxamide 0.0192 0.0623 N-({4-[(3-chloro-2-methylphenyl)sulfonyl]phenyl }曱基)-1Η-»Bizozolo[3,4-b]°Bite-5-decylamine 0.0369 0.0161 N-({4-[(3-Chloro-2-mercaptophenyl)sulfonyl) Phenyl}fluorenyl)-1Η-indolo[3,2-c]pyridin-2-decylamine 0.0625 0.0120 N-({4-[(3-Ga-2-methylphenyl)sulfonyl) Phenyl}hydrazino)furo[2,3-c]pyridine-2-carboxamide 0.0026 0.0016 158436.doc -397- 201215609 N-({4-[(3-Ga-2-methylbenzene)) Sulfhydryl]phenyl}indolyl)imidazo[l,2-a]pyridin-6-carboxamide 0.0257 0.0050 N-({4-[(3-Ga-2-methylphenyl)sulfonyl) Phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carboxamide 0.0043 0.0265 N-({4-[(3-Ga-2-methylphenyl)sulfonyl]phenyl} Thiol group] thieno[2,3-decabiidine-2-carboxamide 0.0572 0.0071 N-({4-[(3-gas-4-methoxybenzene) hydrazino]phenyl}methyl) -1Η-»carbazol [3,4-b] "Bite-Bist-5-carbamamine 0.0040 0.0036 N-({4-[(3-Ga-4-methoxybenzene)sulfonyl]phenyl) }Methyl)-1Η-»Λ 并[3,2-c]pyridin-2-carboxamide 0.0107 0.0021 N-({4-[(3-Ga-4-methoxybenzene)sulfonyl) Phenyl}methyl)furo[2,3-c]pyridine-2-cartoamine 0.0073 0.0018 N-({4-[(3-Ga-4-methoxybenzene)sulfonyl]phenyl }A Imidazo[l,2-a] pyridine-6-carbamide 0.0018 0.0018 N-«4-[(3-gasomethoxyphenyl)sulfonyl]phenyl}methyl)thiophene [2] ,3-c]pyridine-2-carbamide 0.0050 0.0016 N-({4-[(3-Ga-4-methylphenyl)sulfonyl]phenyl}methyl)-1Η-indolezolo[ 3,4-b]pyridine-5-cartoamine 0.0061 0.0019 N-({4-[(3-Ga-4-methylphenyl)sulfonyl]phenyl}indolyl)-lH-nb-[ 3,2-c]pyridin-2-carboxamide 0.0083 0.0025 N-«4-[(3-Ga-4-methylphenyl)sulfonyl]phenyl}methyl)furan[2,3- c]"tb pyridine-2-carboxamide 0.0528 0.0017 N-({4-[(3-gas-4-methylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a] Pyrimidine-6-carbamamine 0.0018 0.0012 N-({4-[(3-Ga-4-methylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c] 2-carbamamine 0.0051 0.0010 N-({4-[(3-Ga-4-propoxybenzene)sulfonyl]phenyl}methyl)-lH-ntoxazolo[3,4-b] Pyridyl-5-carbamamine 0.0079 0.00958 N-({4-[(3-Ga-4-propoxybenzene)sulfonyl]phenyl}methyl)-1Η-η ratio [3,2 -c]Pyridine-2-carbamamine 0.0740 0.0078 N-({4-[(3-Ga-4-propoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c Pyridine-2- Indoleamine 0.0049 0.0119 N-({4-丨(3-Gas-4-propoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] D-pyridyl-6-formamidine Amine 0.0065 0.0060 N-({4-[(3-Ga-4-propoxybenzene) fluorenyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-cartoamine 0.0039 0.0024 N-({4-[(3-Ga-4-propoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0151 0.0174 N-( {4-[(3-Gas-5-fluorophenyl)sulfonyl]phenyl}indolyl)-1Η-&quot;Bizozolo[3,4-b]pyridine-5-carboxamide 0.0133 0.0060 N- ({4-[(3-Gas-5-fluorophenyl)sulfonyl]phenyl}methyl)-1Η-«Byrolo[3,2-c]pyridine-2-carbamide 0.0099 0.0014 N- ({4-[(3-Gas-5-fluorophenyl)sulfonyl]phenyl}indolyl)furan [2,3-&lt;:] bite- 2-carboxamide 0.0178 0.0031 158436.doc - 398- 201215609

N-({4-[(3-chloro-5-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-apyridyl- 6-carboxamide 0.0039 0.0003 N-({ 4-[(3-Gas-5-fluorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0024 0.0029 N-({4-[(3 -gas-5-fluorobenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyrene-bito-2-carbamide 0.0014 0.0006 N-({4-[(3-气_ 5·Methoxybenzene)sulfonyl]phenyl}methyl)-1Η-carbazolo[3,4-b]pyrodo-5-decylamine 0.0093 0.0025 N-({4-[(3- Gas-5-methoxybenzene) hydrazino]phenyl}methyl)-1 Η-〇Λ 并[3,2-c] pyridine bit 2 carbamide 0.170 0.0025 Ν-({4-[ (3-Ga-5-methoxybenzene)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridine-2-carboxamide 0.0265 0.0015 Ν-({4·【(3- Chloro-5-methoxybenzene)sulfonyl 1 phenyl}methyl) oxazolo[l,2-a] 0 ratio bite _6_carbamamine 0.0092 0.0015 N-({4-[(3- Gas-5-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] pyridine-6-carbamide 0.13 0.0008 N-({4-[(3-气- 5-methoxyphenyl)sulfonyl]phenyl}methyl)thienop,3-c]pyridine-2-carboxamide 0.0041 0.0011 N-({4-[(3-chloro-5·methyl) Benzene sulfonyl] Phenyl}methyl)-1Η-»biszolo[3,4-blpyridine-5-decylamine 0.0062 0.0026 N-({4-[(3-a-5-nonylphenyl)sulfonyl] Phenyl}methyl)furo[2,3-c] «Bistidine-2-carboxamide 0.0269 0.0018 N-({4-[(3-Ga-5-nonylbenzene))]phenyl }Methyl)furo[2,3-c]pyridine-2-cartoamine0.0013 0.0008 N-({4-[(3-chloro-5-methylphenyl)sulfonyl]phenyl}methyl) Imidazo[l,2-a]acridin-6-formamide 0.0064 0.002 N-({4-[(3-Ga-5-nonylbenzene)sulfonyl]phenyl}indolyl) imidazo[ l,2-a]pyrazine-6-carbamide 0.0048 0.0023 N-({4-[(3-a-5-nonylbenzene) hydrazino]phenyl}fluorenyl) 嗟 并 [2, 3-cp than pyridine-2-decylamine 0.0045 0.0016 N-({4-[(3- gas benzene) sulfonyl]phenyl}methyl)-1Η-»biszolo[3,4-b] »Bite bite - 5-carbamide 0.007 0.006 N-({4-[(3-chlorophenyl)sulfonyl]phenyl}methyl)-1H-pyrrolo[3,2-b]pyrobitone-2 - decylamine 0.0039 0.013 N-({4-[(3-Phenylbenzene)sulfonyl-1phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.0060 0.0033 N- ({4-[(3-chlorophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]» than 唆-6-decylamine 0.00908 0.00307 N-({4-[(3 -chlorobenzene)sulfonyl] Imidazo[1,2-a]pyrimidine-6-nonylamine 0.0013 0.0012 N-({4-[(3-cyanobenzene)sulfonyl]phenyl}methyl)-lH -nfcoxazolo[3,4-b]»tb pyridine-5-formamide 0.0185 0.00954 Ν-«4-[(3·cyanobenzene) fluorenyl] phenyl]methyl)-1Η-&quot; Bis-[3,2-decabiidine-2-carboxamide 0.0121 0.0113 158436.doc - 399- 201215609 N-({4-[(3-cyanobenzene) hydrazino]phenyl}fluorenyl) Furano[2,3-c]nt bite-2-carbamamine 0.0154 0.0126 N-({4-[(3-cyanobenzene) hydrazino]phenyl}indolyl)carbazole [l,2 -a]pyrimidine-6-carbamamine 0.0059 0.0192 N-({4-[(3-cyanobenzene) fluorenyl]phenyl}fluorenyl) thieno[2,3-ten ratio bite·2· Methionamine 0.0035 0.0056 Ν-({4-[(3-ethoxy-2-fluorobenzene)sulfonyl 1phenyl}methyl)-1Η-»Λ[3,2-c] pyridine 2-carbamamine 0.0312 0.0116 N-({4-[(3-ethoxy-2-fluorobenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2- Methionamine 0.0175 0.0227 N-({4-[(3-ethoxy-2-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-cartoamine 0.0050 0.0062 Ν·({4-[(3-ethoxy-2-fluorobenzene)sulfonyl]phenyl}methyl)- oxazolo[l,2-a] 峨-6-cartoamine 0.0040 0.0197 N-({4-[(3-ethoxy-2-fluorobenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2- Indoleamine 0.0037 0.0129 N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)·1Η·&quot;Bizozolo[3,4-b]pyridin Bite-5-carbamide 0.0261 0.012 N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)-1Η-&quot;比比和[3,2 -c]pyridine-2-carbamide 0.0824 0.0044 N-({4-[(3-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c] Pyridin-2-decylamine 0.0110 0.0072 N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a] ° bite -6-formamide 0.0170 0.006 N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] pyridine-6 -carbamamine 0.0003 0.0078 N-({4-[(3_ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamidine Amine 0.0033 0.0031 N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrazolo[3,4-b] pyridine-5-carbamamine 0.0146 0.0190 N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0077 0.0035 N-( {4- [(3-ethoxyphenyl)sulfonyl]phenyl}methyl)furan [2,3-decene bite 2-nonylamine 0.0068 0.0110 N-({4-[(3- Ethoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]nfc bite- 6-decylamine 0.0050 0.0031 N-({4-丨(3-ethoxybenzene) Mercapto]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-decylamine 0.0021 0.0067 N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}A Thio[2,3-c] 〇 咬 - 2- 曱 0.00 0.0032 0.0029 N-({4-[(3-ethylbenzene) phenyl]phenyl} fluorenyl)-1Η-&lt ; oxazo[3,4-b]»pyridin-5-formamide 0.0070 0.0071 N-({4-[(3-ethylbenzene) hydrazino]phenyl}methyl)furan [2, 3-c]pyridine-2-cartoamine 0.0087 0.0065 158436.doc •400- 201215609

N-({4-[(3-ethylbenzene)) fluorenyl]phenyl}methyl)imidazo[1,2-a]pyridine-6-carboxamide 0.00483 0.00323 N-({4-[( 3-ethylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carbenamide 0.0038 0.0041 Ν-({4-[(3-1-2-曱) Oxy-phenyl) phenyl} fluorenyl-1H-carbazolo[3,4-b]pyridine-5-carboxamide 0.121 0.1-1 N-({4-[(3-gas-) 2-nonyloxybenzene) continued fluorenyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0324 0.0063 N-({4-[(3-fluoro-) 2-decyloxybenzene)sulfonyl]phenyl}indolyl)furan p,3-c]pyridin-2-carboxamide 0.0166 0.0309 N-({4-[(3-fluoro-2-) Oxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide 0.0769 0.0650 N-({4-[(3-fluoro-2-methoxybenzene) Sulfo]phenyl]methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0289 0.1-1 N-({4-[(3-fluoro-2-decyloxybenzene)) Sulfhydryl]phenyl}methyl)thieno[2,3-clpyridine-2-carboxamide 0.0133 0.0125 Ν-({4·[(3_fluoro-2-methylphenyl)sulfonyl]benzene曱 曱 ) ) · 3 3 3 3 3 3 3 3 3 3 3 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 469 Phenyl}methyl) -1Η-拉咯和[3,2-&lt;:]0 than bite-2_cartoamine 0.0576 0.0132 N-({4-[(3-fluoro-2-methylphenyl)sulfonyl)phenyl }methyl)furo[2,3-decabiidine-2-carboxamide 0.0132 0.0307 N-({4-[(3-fluoro-2-methylphenyl)sulfonyl 1phenyl}methyl) Imidazo[1,2-a]»pyridin-6-formamide 0.0469 0.0132 N-({4-丨(3-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)imidazolium [l,2-a]pyrimidine-6-methanamine 0.0081 0.0656 N-({4-[(3-敦_2·methylbenzene)sulfonyl]phenyl}methyl)thieno[2,3 -c]pyridine-2-carbamide 0.0071 0.0214 N-({4-[(3-fluoro-4-indolyl)sulfonyl]phenyl}methyl)-1Η-carbazolo[3, 4-b]Pylazen-5-carbamide 0.0430 0.0060 N-({4-[(3-fluoro-4-methoxybenzene)sulfonyl]phenyl}methyl)furan[2,3- Cl pyridine-2-carbamide 0.0022 0.0068 N-({4-[(3-fluoro-4-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] pyridine -6-carbamide 0.00595 0.00289 N-({4-[(3-fluoro-4-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6- Methionamine 0.0017 0.0083 N-({4-[(3-fluoro-4-methylphenyl)sulfonyl]phenyl}methyl)-1Η-«biazo[3,4-b]pyridine-5 -甲醯0.0117 0.0056 N-({4-[(3-Fluoro-4_methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-中比pyridine-2-carboxamide 0.0140 0.0033 N- ({4-[(3-Fluoro-4-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]&quot;Biduct-6-decylamine 0.0133 0.00378 N-( {4-[(3-Fluoro-4-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-carboxamide 0.0023 0.0063 158436.doc •401- 201215609 N-({4-[(3-fluoro-4-propoxyphenyl)sulfonyl]phenyl}methyl)-1H-&quot;biazolo[3,4-b]pyridine-5-formamidine Amine 0.0116 0.0065 N-({4-[(3-fluoro-4-propoxybenzene)sulfonyl]phenyl}methyl)-lH-nt-[3,2-c]pyridine-2-yl Indoleamine 0.0309 0.0104 N-({4-[(3-fluoro-4-propoxybenzene)sulfonyl-1phenyl}methyl)furo[2,3-c]pyridine-2-cartoamine 0.0068 0.0118 N-({4-[(3-Fluoro-4-propoxybenzene)sulfonyl]phenyl}methyl)- oxazolo[l,2-a]pyridine-6-carboxamide 0.021 0.0044 N -({4-[(3-fluoro-4-propoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2_a]pyrimidine-6-carboxamide 0.0027 0.0033 N-({4- [(3-Fluoro-4-propoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c] 0 is a bit of 2-mercaptoamine 0.0037 0.0081 N-({4-[(3-Fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-carbazolo[3,4-b]pyrene than bite-5- Indoleamine 0.0044 0.0063 N-({4-[(3-Fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0174 0.0033 N-({4-[(3-Fluoro-5-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carboxamide 0.0016 0.0033 N -({4-[(3-乱-5-methylphenyl)sulfonyl]phenyl}methyl)-lH-ntoxa[3,4-b]pyridin-5-formamide 0.0095 0.0056 N -({4-[(3-fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)-1Η-»Λ[3,2-c]pyridine-2-cartoamine 0.0083 0.0018 Ν-({4-[(3-Fluoro-5-mercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carbamide 0.0034 0.0032 N- ({4-[(3-Fluoro-5-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]»pyridin-6-carboxamide 0.0027 0.0006 N-({ 4-[(3-Fluoro-5-methylphenyl) benzyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0015 0.0054 N-({4-[( 3-fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]»tb pyridine-2-carboxamide 0.0010 0.0006 N-({4-[(3- Fluorobenzene)sulfonyl]phenyl} Methyl)-1Η-»Bizozolo[3,4-b]&quot;Bistidine-5-carbamamine 0.0339 0.0253 N-({4-[(3-fluorophenyl)sulfonyl)phenyl} Furfuro[2,3-c]acridin-2-carboxamide 0.0058 0.0145 N-({4-[(3-fluorophenyl)sulfonyl]phenyl}methyl)imidazolium,1,2 -a]&quot;Bistidine-6-carbamideamine 0.0021 0.0122 N-({4-[(3-fluorophenyl)sulfonyl)phenyl}indolyl) oxazole [l,2-a]pyrimidine- 6-Proline Amine 0.0019 0.0221 N-({4-[(3-Hydroxyphenyl)]indolyl]phenyl}methyl)imidazo[l,2-a]nfcpyridine-6-carboxamide 0.005 0.0070 N -({4-[(3-曱烧醯 醯 Benzene) sulfonyl]phenyl}methyl)furan P,3_c]pyridine-2-carboxamide 0.0060 0.0068 Ν·({4·[(3 _Methanesulfonyl benzene) sulfonyl phenyl] phenyl} fluorenyl) oxazole [l, 2-al 0 ratio bite-6-formamide 0.0256 0.016 158436.doc -402- 201215609

N-({4-[(3-曱 醯 醯 醯 苯) sulfonyl]phenyl} fluorenyl) thieno[2,3-c]pyridin-2-decylamine 0.0017 0.0035 N-({4 -[(3-methoxy-4-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-oxazolo[3,4-b]pyridin-5-carboxamide 0.0036 0.0034 N-( {4-[(3-Methoxy-4-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-»Byrolo[3,2-c]pyridin-2-decylamine 0.0079 0.0030 N-({4-[(3-methoxy-4-mercaptophenyl)sulfonic acid Iphenyl}indenyl)furo[2,3-c]pyridin-2-meramine 0.0046 0.0031 N -({4-[(3-methoxy-4-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]bitite-6-cartoamine0.0013 0.0017 N- ({4-[(3-Methoxy-4-methylphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]nt bit-2-amine 0.27. (10) 15 N-({4-[(3-methoxy-5-methylphenyl)sulfonyl]phenyl}indenyl)-1Η-&quot;Bildo[3,2-c]pyridin-2-indole Indoleamine 0.0096 0.0028 N-({4-[(3-methoxy-5-methylphenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indoleamine 0.0022 0.0016 N-({4-[(3-曱-oxy-5-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridin-6-decylamine 0.0053 0.0016 N -({4-[(3-methoxy-5-mercaptophenyl)sulfonic acid]phenyl}indolyl)imidazo[1,2-a]bitite-6-nonylamine 0.0016 0.0013 N- ({4-[(3-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-cartoamine 0.0024 0.0008 N-( {4-[(3-decyloxyphenyl)sulfonyl]phenyl}indolyl)-1Η-»oxazolo[3,4-b]pyridin-5-carboxamide 0.0209 0.0100 N-({4 -[(3-decyloxyphenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]nb-pyridine-2-amine 350.0035 0.0069 N-({4-[(3-A Oxybenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]&quot;Bite- 6-decylamine 0.00497 0.00245 N-({4-[(3-decyloxybenzene)) Further thiol]phenyl}indolyl)imidazo[1,2-a]pyrimidine-6-carboxamide 0.0020 0.0124 N-({4-[(3-methylphenyl)sulfonyl]phenyl} Methyl)furo[2,3-c]»tfcpyridine-2-carbamide 0.0023 0.0053 N-({4-[(3-methylphenyl)sulfonyl]phenyl}methyl)imidazo[ l,2-a]»Bite-6-carbamamine 0.00812 0.00639 N-({4-[(3_methylphenyl) fluorenyl]phenyl}methyl)imidazo[l,2-a] Pyrimidine-6_carbamamine 0.0019 0.0091 N-({4-[(3-phenylphenyl)sulfonyl]phenyl}methyl)-1,3_benzothiazole-6- Methionamine 0.0185 1-10 N-({4-[(3-phenylphenyl)- fluorenyl)phenyl}indolyl)-1Η-ηpyr-[3,2-c]»it pyridine-2 -Metformamide 0.0023 0.0119 N-({4-[(3-Phenylphenyl)sulfonyl)phenyl}methyl)furo[2,3-c]nb bite-2-carboxamide 0.0137 0.0234 N -({4-[(3-Phenylphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]ntidine-6-carboxamide 0.0122 0.0068 158436.doc •403 - 201215609 N -({4-[(3-phenylphenyl) hydrazino]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-decylamine 0.0009 0.0033 N-({4-[( 3-phenylphenyl) hydrazino]phenyl}methyl)thienop,3-c]«pyridin-2-carbamide 0.0045 0.0100 N-({4-[(3-phenylpropan) Continuation of fluorenyl]phenyl}indenyl)-1Η-»pyrolo[3,2-c]pyridine-2-cartoamine 0.014 0.078 N-({4-[(3-propoxybenzene)sulfonate) ]]phenyl}fluorenyl)-1Η-pyrazolo[3,4-b] acridine-5-decylamine 0.0304 0.041 N-({4-[(3-propoxybenzene)) Phenyl}methyl)-1Η-indolo[3,2-c]pyridine-2-carboxamide 0.0102 0.0122 N-({4-[(3-propoxyphenyl)sulfonyl]phenyl} Methyl)furo[2,3-c]nfc pyridine-2-meronamide 0.0101 0.0252 N-({4-[(3-propoxyphenyl)sulfonyl]phenyl}曱Imidazo[1,2-a]»pyridin-6-methalamine 0.0042 0.0063 N-({4-[(3-propoxybenzene) hydrazino]phenyl}indolyl)imidazo[l ,2-a]pyrimidine-6-carboxamide 0.0048 0.0075 N-({4-[(3-propoxyphenyl)sulfonyl-1phenyl}methyl)thieno[2,3-c]acridine 2- 2-Methylamine 0.0040 0.0122 N-({4-[(3-Aminosulfonylbenzene) hydrazino]phenyl}methyl)-indole-carbazolo[3,4-blpyridine-5- Methionamine 0.0301 0.1-1 N-({4-[(3-Aminosulfonylbenzene))sulfonyl]phenyl}methyl)imidazo[l,2-a]acridin-6-carboxamide 0.0103 0.0546 Ν-({4-[(3-Aminosulfonylbenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]"* pyridine-2-carbamide 0.0020 0.0121 N- ({4-[(3-tert-butylbenzene) hydrazino]phenyl}methyl)furo[2,3-c]nfc pyridine-2-carboxamide 0.0093 0.0070 N-({4-[ (3-tert-butylbenzene)sulfonyl]phenyl}mercapto)imidazo[l,2-a]nb pyridine-6-cartoamine 0.0097 0.0032 N-({4-[(3-3) Butyl benzene) benzyl 1 phenyl}methyl)imidazo[l,2-a]pyrimidin-6-cartoamine &lt;0.00065 0.0012 N-({4-[(3-tert-butylbenzene)) Further thiol]phenyl}methyl)thieno[2,3-c]〇tfc pyridine-2-carboxamide 0.0105 0.0091 义({ 4-[(4,5-Difluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.0281 0.0259 N-( {4-[(4,5-Difluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrodo-6-carboxamide 0.0281 0.0068 N- ({4-[(4,5-Difluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0119 0.0249 N -({4-[(4-ethylphenyl) phenyl)phenyl}indolyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0289 0.0037 N-({ 4-丨(4-Ethylbenzene) fluorenyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0052 0.0065 N-({4-[(4- Butoxy-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-α-pyrazolo[3,4-b]pyridine-5-cartoamine 0.0709 0.0688 -404- 158436.doc 201215609

N-({4-[(4-butoxy-2-mercaptophenyl)sulfonyl]phenyl}indenyl)-1Η-&quot;Bildo[3,2-c]pyridine-2-A Guanamine 0.0800 0.0625 N-({4-[(4-butoxy-2-mercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carboxamidine Amine 0.0160 0.0648 N-({4-[(4-butoxy-2-indolylbenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-decylamine 0.0100 0.0224 N-({4-丨(4-butoxy-2-indolylbenzene)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]pyridin-2-decylamine 0.0033 1.0- 0.1 N-({4-[(4-Butoxy-3-oxabenzene)sulfonyl]phenyl}methyl)-1Η-»oxazolo[3,4-b]pyrodo-5-曱Indoleamine 0.0045 0.0111 N-({4-[(4-butoxy-3-oxabenzene)sulfonyl]phenyl}methyl-[3,2-c]pyridine-2-carboxamide 0.0178 0.0124 N-({4-[(4-Butoxy-3-chlorobenzene)sulfonyl 1phenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide 0.0047 0.0100 N-( {4-[(4-Butoxy-3-chlorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a] 11 than bite-6-anthracene 0.0041 0.0076 N-({ 4-[(4-butoxy-3-acetophenone)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-decylamine 0.0048 0.0125 N-({4-[ (4-butoxy-3 -fluorophenyl)sulfonyl]phenyl}methyl)-1Η-indolo[3,2-c]pyridin-2-decylamine 0.0536 0.0134 N-({4-[(4-butoxy) 3-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-indoleamine 0.0123 0.0139 N-({4-[(4-butoxy-3-) Fluorobenzene)sulfonyl]phenyl}mercapto)imidazo[1,2-a]pyridin-6-decylamine 0.0062 0.0031 N-({4-[(4-butoxy-3-fluorobenzene)) Sulfhydryl]phenyl}methyl)imidazo[l,2-a] pyrimidine-6-decylamine 0.0012 0.0031 N-({4-[(4-butoxy-3-fluorobenzene)sulfonate) (phenyl)methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0047 0.0126 N-({4-[(4-butoxybenzene)sulfonyl]phenyl}methyl )-lH-nboxazolo[3,4-b]pyridin-5-decylamine 0.0275 0.0225 N-({4-[(4-butoxybenzene) hydrazino]phenyl}methyl)-lH -nfc-[3,2-c]pyridin-2-decylamine 0.0084 0.0171 N-({4-[(4-butoxyphenyl)sulfonyl]phenyl}methyl)furan[2, 3-c] bite - 2-carbamide 0.0062 0.0130 N-({4-[(4-butoxybenzene)-decyl]phenyl}methyl)imidazo[I,2-ten-bite- 6-decylamine 0.0038 0.0028 N-({4_[(4· Butoxybenzene))]phenyl]indolyl] thieno[2,3-ten ratio bite- 2-曱醢0.0036 0.0103 N-({4-[(4-Butylphenyl)sulfonyl]phenyl}indolyl)-1Η-»Bizozolo[3,4-b]acridin-5-carboxamide 0.0712 0.0684 N-({4-[(4-butylphenyl) aryl]phenyl}indenyl)-1Η-&quot;Bildo[3,2-c]acridin-2-carboxamide 0.0146 0.0358 N -«4-[(4-butylphenyl)sulfonyl]phenyl}methyl)furo[2,3-&lt;:] acridine-2-carbamide 0.0181 0.0265 158436.doc -405- 201215609 N-({4-[(4-butylbenzene))]phenyl}indolyl]imidazo[1,2-a]pyridyl-6-carbamamine 0.0057 0.0076 N-({4-[ (4-butylbenzene) continued fluorenyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0053 0.0107 N-({4-[(4-butylbenzene)) Mercapto]phenyl}methyl)thieno[2,3-1:]acridine-2-cartoamine 0.0029 0.0260 N-({4-[(4-Ga-2-ethoxybenzene)) Base]phenyl}methyl)-lH-nb-[3,2-c]pyridin-2-carboxamide 0.0112 0.0004 N-({4-[(4-Ga-2-ethoxybenzene)) Sulfhydryl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0072 0.0051 N-({4-[(4-chloro-2-ethoxyphenyl)sulfonyl) 】Phenyl}methyl)imidazo[l,2-a]β ratio bite-6·starting amine 0.0041 0.0007 Ν-({4-[(4-chloro-2-ethoxybenzene) Sulfhydryl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-formamide 0.0020 0.0045 N-({4-[(4-Ga-2-ethoxybenzene)sulfonyl) Phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0024 &lt;0.0004 N-({4-[(4-chloro-2-methoxybenzene)sulfonyl] Phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.085 0.0248 N-({4-[(4-Ga)methoxyphenyl)sulfonyl]phenyl}methyl Oxazo[1,2-a] 0-bite-6-carbamamine 0.0187 0.0126 N-({4-[(4-Ga-2-methoxybenzene)sulfonyl]phenyl}fluorenyl) Imidazo[l,2-a] pyridine-6-carbamide 0.0033 0.0247 N-({4_[(4-Gaxo-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η- Pyrazolo[3,4-b]pyridin-5-formamide 0.0775 0.0587 N-({4-[(4-chloro-2-methylphenyl)sulfonyl]phenyl}indolyl)furan[ 2,3-(Calazine-2-carboxamide 0.0249 0.0647 N-({4-[(4-chloro-2-methylphenyl)sulfonyl)phenyl}methyl)oxazolo[l, 2-a] pyrimidine-6-carbamide 0.0066 0.0539 N-({4-[(4-gas-3-fluorobenzene)sulfonyl]phenyl}indolyl) furan [2,3-ten ratio Acridine 2-formamide 0.0185 0.0065 N-({4_[(4·Ga-3-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]-specific - 6-decylamine 0.00722 0.00724 N-({4-[(4-Ga-3-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6- formazan Amine 0.0019 0.0089 N-({4-[(4-Ga-3-methoxyphenyl)sulfonyl]phenyl}methyl)-1H-&quot;Bizozolo[3,4-b]pyridine-5 -carbamamine 0.0127 0.0130 N-({4-[(4-Ga-3-methoxybenzene) fluorenyl]phenyl}methyl)-1Η-ηpyrho[3,2-c]咣唆-2-carbamamine 0.0055 0.0036 N-({4-[(4-Ga-3-methoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2 - brewing amine 0.0059 0.0060 N-({4-[(4-gas-3-methoxybenzene)sulfonic acid]phenyl}methyl)imidazo[l,2-a]pyridine-6-formamidine Amine 0.0135 0.006 N-({4-[(4-Ga-3-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0027 0.0052 158436.doc -406- 201215609

N_({4-[(4-Gas-3-methoxybenzene)sulfonyl]phenyl}methyl) pheno[2,3-c]pyridin-2-decylamine 0.0026 0.0023 N-( {4-[(4-Gasphenyl)sulfonyl]phenyl}methyl)-1Η-°Bizozolo[3,4-b]»it bite 5- 5-amine 0.0288 0.022 N-({4 -[(4-Gaphene)sulfonyl]phenyl}indolyl)furan[2,3-decapyridin-2-ylamine 0.0049 0.0142 N-({4-[(4-Gasbenzene)) Mercapto]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-nonylamine 0.0025 0.0236 N-({4-[(4-cyanobenzene)sulfonyl]phenyl}曱Base)-1Η-»Bizozolo[3,4-b]"pyridin-5-formamide 0.0284 0.0208 N-({4-[(4-cyanobenzene) continuation]phenyl}A Base)-1Η-&quot;比比和[3,2-decabiidine-2-carboxamide 0.0111 0.0251 N-({4-[(4-cyanobenzene)sulfonyl]phenyl}methyl) Furano[2,3-c]nb bite-2-carboxamide 0.0053 0.0309 N-({4-[(4-cyanobenzene)cansyl]phenyl}methyl)imidazo[1,2- Small bite-6-carbamamine 0.0160 0.0141 N-({4-[(4-cyclohexylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]. Formamide 0.0178 0.0117 N-({4-[(4-cyclohexylbenzene))]phenyl}indolyl]imidazo[1,2-a]pyrimidine- 6-decylamine 0.0058 0.0 077 N-({4-[(4-cyclohexylbenzene))]phenyl}methyl)thieno[2,3-c]pyridyl-2-carbamide 0.0034 0.0129 N-({4- [(4-Ethoxy-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-»carbazolo[3,4-b]pyridine-5-decylamine 0.1083 0.0667 N- ({4-[(4-Ethoxy-2-methylphenyl)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0092 0.0126 N-({4-[(4-ethoxy-2-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.016 0.0274 N -({4-[(4-ethoxy-2-methylphenyl)cansyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-nonylamine 0.0066 0.0111 N-( {4-[(4-Ethoxy-2-methylphenyl)sulfonyl-1phenyl}methyl)imidazo[1,2-a]pyrimidine-6-decylamine 0.0117 0.0607 N-({4 -[(4-ethoxy-2-methylphenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-carboxamide 0.0012 0.0132 N-({4- [(4-Ethoxy-3-fluorophenyl)sulfonyl]phenyl}methyl)-1H-indazolo[3,4-b]pyrodo-5-carboxamide 0.0095 0.0052 N-({ 4-[(4-Ethoxy-3-fluorophenyl)sulfonyl]phenyl}indolyl)-lH-nb-[3,2-c]pyridyl-2-meramine 0.0205 0.0054 N- ({4-[(4-ethoxyl) 3-fluorophenyl)sulfonyl]phenyl}indolyl]imidazo[1,2-a]pyridin-6-carboxamide 0.0127 0. (10) 18 N-({4-[(4-ethoxy) -3-IL benzene)sulfonyl]phenyl}mercapto)imidazo[l,2-a] mouth bite-6-carbenamide 0.0009 0.0031 N-({4-[(4-ethoxy-3) -fluorobenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-decylamine0.0089 0.0036 158436.doc •407· 201215609 N-({4-[(4-B Oxybenzene)sulfonyl]phenyl}methylazolo[3,4-b]pyrodo-5-carboxamide 0.0151 0.0084 N-({4-[(4-ethoxyphenyl)) Phenyl}mercapto)furo[2,3-c]-p-pyridyl-2-carbamide 0.0025 0.0071 N-({4-[(4-ethoxyphenyl)sulfonyl]phenyl}methyl Imidazo[1,2刈 bite- 6-formamide 0.0045 0.0029 N-({4-[(4-ethoxyphenyl) fluorenyl]phenyl}methyl)imidazo[l,2- a]pyrimidine·6-decylamine 0.0020 0.0061 N-({4-[(4-ethoxyphenyl)sulfonyl]phenyl}methyl)thiophene[2,3-decidin-2-yl Indoleamine 0.0021 0.0040 N-({4-[(4-ethylbenzene) hydrazino]phenyl}methyl)furo[2,3-c]pyridine-2-carbamimid 0.0050 0.007 N-({ 4-[(4-ethylbenzene) hydrazino]phenyl}methyl)imidazo[1,2-a] 吼-6- 曱Indoleamine 0.0165 0.00736 N-({4-[(4-ethylphenyl)sulfonyl)phenyl}methyl)imidazo[1,2-a]pyrimidin-6-carbenamide 0.0012 0.0062 沁({ 4-[(4-fluoro-2,5-dimethylphenyl)sulfonyl]phenyl}methyl)-111--pyrazolo[3,4-b]pyridin-5-carboxamide 0.0373 0.0459 N-({4-[(4-Fluoro-2,5-dimethylphenyl)sulfonyl]phenyl}indenyl)-111_咐•咯和[3,2-c]pyroline-2 -Mesalamine 0.0514 0.0128 N-({4-[(4-H-2,5-dimercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2 -carbamamine 0.0176 0.0242 ({4-[(4-)-2,5-dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyro-6- Formamidine 0.0440 0.011 N_({4-[(4_Fluoro.2,5-dimethylphenyl)sulfonyl]phenyl}indolyl) oxazole [1,2-a] bite-6- Methionamine 0.0058 0.0294 N-({4-[(4-fluoro-2,5-dimethylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-methyl Indoleamine 0.0042 0.0136 N-({4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-»bisazolo[3,4-b]pyridine-5 -Proline 0.159 0.0742 N-({4-[(4-Fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)furan p,3-c]pyridine-2-carboxamide 0.0127 0.0160 N-({4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)- oxazolo[l,2-a] σ ratio bite-6-formamide 0.0193 0.00705 Ν-({4-[(4-fluoro-2-methoxybenzene) hydrazino]phenyl}methyl)imidazo[l,2-a]pyrimidin-6-nonylamine 0.0191 0.0736 N-( {4-[(4-Fluoro-2-methylphenyl)indolyl]phenyl}methyl)-lH-nfcoxazolo[3,4-b]pyridin-5-carboxamide 0.0788 0.0983 N-( {4-[(4-Fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-cJnt-pyridin-2-ylamine 0.0187 0.0651 N-({4-[( 4-fluoro-2-mercaptophenyl)indolyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carbenamide 0.0130 0.1-1 N-({4-丨(4 -Fluoro-3-methoxybenzene)sulfonyl]phenyl}indenyl)-1Η-»bisazolo[3,4-b]pyridin-5-carboxamide 0.0239 0.0115 158436.doc •408· 201215609

N-({4-[(4-Fluoro-3-methoxyphenyl)sulfonyl]phenyl}methyl)-lH-nb-[3,2-c]pyridin-2-carboxamide 0.0278 0.0054 N-({4-[(4-Fluoro-3-decyloxybenzene)sulfonyl 1phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0078 0.0070 N -({4-[(4-fluoro-3-indolylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridin-6-decylamine 0.0197 0,0067 N- ({4-[(4-Fluoro-3-indolylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a] shouting-6-carbamamine 0.0049 0.0108 N-({ 4-[(4-Fluoro-3-methoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0090 0.0031 N-({4-[ (4-Fluoro-3-mercaptophenyl)sulfonyl 1phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0050 0.0083 N-({4-[ (4-Fluoro-3-mercaptophenyl)sulfonyl]phenyl}indolyl)furan p,3-indolyl-2-cartoamine 0.0132 0.006 N-({4-[(4-fluoro-) 3-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrodo-6-carboxamide 0.0235 0.00714 N-({4-[(4-fluoro-3-曱) Benzo)sulfonyl-1phenyl}methyl)imidazo[l,2-alpyrimidine-6-carboxamide 0.0022 0.0096 N-({4-[(4-methyl succinyl) sulfonyl) Phenyl}A Base)-1Η-&quot;Bizozolo[3,4-b]pyrodo-5-carbamamine 0.0293 0.0238 N-({4-[(4-methylpyrene)benzenesulfonyl]phenyl }Methyl)imidazo[l,2-a]pyridine-6-carboxamide 0.105 0.0247 puff ({4-[(4-decyloxy-2,5-dimercaptophenyl)sulfonyl]phenyl) }Methyl)-111-pyrazolo[3,4-b]pyrodo-5-anthracene amine 0.0368 0.0236 N-({4-[(4-decyloxy-2,5-dimercaptobenzene) Sulfhydryl]phenyl}indolyl)furo[2,3-c]pyridin-2-carboxamide 0.0123 0.0128 义({4-[(4-曱-oxy-2,5-dimethylbenzene) Sulfhydryl]phenyl}indolyl)imidazo[1,2-a]pyrodo-6-carboxamide 0.0281 0.006 N-({4-[(4-methoxy-2,5-dioxin) Benzo)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyrimidin-6-carboxamide 0.0052 0.0130 N-({4-[(4-decyloxy-2-methyl) Benzene sulfonyl]phenyl}indolyl)-lH-ntoxazolo[3,4-b]pyrodo-5-carboxamide 0.029 0.0555 N-({4-[(4-decyloxy-2) -mercaptophenyl)sulfonyl]phenyl}indenyl)furo[2,3-c]pyridin-2-indoleamine 0.0216 0.0351 N-({4-[(4-methoxy-2-) Mercaptobenzene)sulfonyl]phenyl}indenyl)imidazo[1,2-a]biting-6-carbenamide 0.0024 0.0679 N-({4-[(4-methoxy-3,5) -dimethylbenzene)sulfonyl]曱 曱 ) ) Η Η 〇 〇 〇 〇 〇 〇 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00 Benzene sulfonyl]phenyl}indolyl)-lH-nfc oxo[3,2-c]pyridin-2-carboxamide 0.0516 0.0017 N-({4-[(4-decyloxy-3) ,5-dimethylphenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-carboxamide 0.0056 0.0018 N-({4-[(4-methoxy) -3,5-dimethylphenyl)sulfonyl]phenyl}indolyl]imidazo[l,2-a]ntidine-6-carboxamide 0.0146 0.0014 158436.doc •409_ 201215609 N-({4 -[(4-methoxy-3,5-dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-cartoamine 0.0027 0.0013 沁({ 4-[(4-Methoxy-3,5-dimethylphenyl) hydrazino]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0098 0.0009 N-( {4-[(4-曱-oxy-3-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine-6-carboxamide 0.0141 0.00532 N-({4 -[(4-methoxy-3-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carboxamide 0.0022 0.0055 N-({4- [(4-Methoxybenzene) continued fluorenyl]phenyl}indolyl)-1Η-»Bizozolo[3,4-b]pyridine-5-carboxamide 0.0209 0.0143 N-({4- [(4-methoxybenzene) hydrazino]phenyl}methyl)furo[2,3-c]pyro- 2-carbamide 0.0055 0.006 N-({4-[(4-methoxy) Alkyl) phenyl]methyl)imidazo[l,2-a]&quot;bite- 6-formamide 0.00974 0.00866 N-({4-[(4-methoxybenzene)) Mercapto]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0027 0.0207 N-({4-[(4-methylphenyl)sulfonyl]phenyl}A Furfuro[2,3-c]nfc bite_2_carbamamine 0.1208 0.006 N-({4-[(4-mercaptophenyl) hydrazino]phenyl}methyl)imidazo[1,2 -a]»Bipyridine-6-carbamidamine 0.0176 0.012 N-({4-[(4-mercaptophenyl) hydrazino]phenyl}methyl)imidazo[1,2-a]pyrimidine-6 - Methionamine 0.0043 0.0194 N-({4-[(4-Phenylphenyl) contigyl)phenyl}methyl)-1,3-benzothiazole-6-cartoamine 0.0207 0.1-1 N- ({4-[(4-Phenylphenyl)sulfonyl)phenyl}methyl)-1Η-«Bizozolo[3,4-b]pyrene than bite-5-carbamide 0.0320 0.0117 N-( {4-[(4-Phenylphenyl)sulfonyl]phenyl}fluorenylpyrrolo[3,2-decabiidine-2-carboxamide 0.0310 0.0133 Ν-({4-[(4-benzene) Benzo)sulfonyl]phenyl}methyl)furo[2,3-decapine-2-guanamine 0.0037 0.0069 Ν-({4-[(4-phenyl) Sulfhydryl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carbenamide 0.0032 0.0076 N-({4-[(4-phenylphenyl)) phenyl]phenyl }Methyl)thieno[2,3-decabiidine_2_carbamimidin 0.0030 0.0106 N-({4-[(4-phenylbutyring)) fluorenyl Iphenyl}indenyl)-1Η-η咯 并 [3,2_c] pyridine-2-carbamide 0.216 0.0715 N-({4-[(4-propoxybenzene) hydrazino]phenyl}fluorenyl)-1Η-»比咯和[ 3,2_c]pyridine-2-carboximine 0.0053 0.0067 N-({4-[(4-propoxybenzene) hydrazino]phenyl}indolyl) furan [2,3-ten ratio bite-2 -cartoamine 0.0495 0.012 N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]» than bite- 6-carbamide 0.0061 0.0019 N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide 0.0022 0.0061 158436.doc •410 - 201215609

N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]acridine-2-carbamide 0.0043 0.0081 N-({4- [(5-Ethyl-2-methoxybenzene) hydrazino]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyrodo-5-carbamide 0.0277 0.0275 N- ({4-[(5-Ethyl-2-yloxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0072 0.0038 N-( {4-[(5-Ethyl-2-yloxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridin-6-decylamine 0.0379 0.0127 N-( {4-[(5-Ethyl-2-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-decylamine 0.0172 0.0548 N-( {4-[(5-Chloro-2-ethoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a] pyridyl-6-carboxamide 0.0022 0.0005 N-({4 -[(5-Gas-2-ethoxybenzene)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0019 0.0033 N-({4-[( 5-Gas-2-ethoxybenzene)sulfonyl]phenyl}indenyl)thieno-p,3-c]pyridin-2-decylamine 0.0027 0.0005 N-({4-[(5-gas- 2-hydroxyphenyl)sulfonyl]phenyl}indolyl)carbazolo[l,2-a]&quot;Bite-6-carbamamine 0.014 0.1682 N-({4-[(5 - gas-2-methoxybenzene) benzyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyrodo-5-carboxamide 0.0492 0.0081 N-({4-[ (5-Gas-2-decyloxybenzene)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyridin-6-decylamine 0.0191 0.0032 N-({4-[(5- Gas-2-oxooxybenzene)sulfonyl]phenyl}indolyl)imidin[1,2-a] pyridine-6-carboxamide 0.0055 0.0061 N-({4-[(5-gas) -2-mercaptobenzene) benzyl]phenyl}fluorenyl)-lH-»tboxazolo[3,4-b]pyrodo-5-decylamine 0.0227 0.0139 N-({4-[(5 - gas-2-methylbenzene)sulfonyl 1phenyl}methyl)furo[2,3-c]&quot;bipyridyl-2-carbamide 0.0058 0.0078 N-({4-[(5- Gas-2-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridinium-6-carboxamide 0.0019 0.0037 N-({4-[(5-gas- 2-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidine-6-carboxamide 0.0031 0.0043 N-({4-[(5-Gas_2_曱) Benzene sulfonyl]phenyl}methyl)thieno[2,3-c]nb pyridine-2-carboxamide 0.0048 0.0066 N-({4-[(5-Ga-2-propoxybenzene)) Sulfhydryl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 0.0492 0.0251 N-({4-[(5-Ga-2-propoxybenzene) )sulfonyl]phenyl}methyl)-1Η- π 并[3,2-c] pyridine-2-meramine 0.0075 0.0012 N-({4-[(5-Ga-2-propoxybenzene)sulfonyl]phenyl}fluorenyl) furan And p,3-c]pyridine-2-carboximine 0.0080 0.0093 Ν·({4-[(5·Ga-2-propoxybenzene)sulfonyl]phenyl}methyl) oxazole [l ,2-a] bite-6-cartoamine 0.0080 0.0032 Ν-({4-[(5-Ga-2-propoxybenzene)sulfonyl]phenyl}indolyl)thieno[2,3- c] Pyridyl-2-carboxamide 0.0057 0.0012 158436.doc -411 · 201215609 N-({4-[(5-Cyano-2-oxaoxybenzene)sulfonyl]phenyl}methyl)imidazolium [1,2-a]pyridine-6-cartoamine 0.0146 0.0119 N-({4-[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-» ratio Zoxa[3,4-b]pyridin-5-formamide 0.0390 0.0151 N-({4-[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)furan[ 2,3-c] pyridine-2-carbamide 0.0022 0.0124 N-«4-[(5-fluoro_2.methoxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2- a] Pyridine-6-carbamide 0.022 0.00665 N-({4-[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine -6-carbamamine 0.0073 0.0261 N-({4-[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)thiophene And [2,3-c]pyridine-2-carbamide 0.0020 0.0008 N-({4_[(5-fluoro_2.methylbenzene)sulfonyl]phenyl}indolyl)-1Η-»bazole And [3,4-b]pyridine-5-decylamine 0.0204 0.0597 N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl}indolyl)furan [2, 3-c]&quot;Bistidine-2-carboxamide 0.0143 0.0249 N-({4-[(5-fluoro_2.methylphenyl)sulfonyl)phenyl}indolyl)imidazo[l,2 -a] indoleidine-6-carbamide 0.0126 0.0229 N-({4-[(5-fluoro-2-indolyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a Pyrimidine-6-formamide 0.0027 0.0351 N-({4-[(5-Tert-butyl-2-methoxybenzene)sulfonyl]phenyl}indolyl)-1H-pyrazolo[3] , 4-b]pyridine-5-formamide 0.055 0.0216 N-({4-[(5-t-butyl-2-methoxybenzene) fluorenyl]phenyl}fluorenyl) furan[2 ,3-c]pyridine-2-carboxamide 0.018 0.0101 N-({4-[(5-tert-butyl-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l , 2-a] pyridine-6-carbamamine 0.029 0.00677 N-({4-[(5-t-butyl-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[ l,2-a]Uridin-6-carbamide 0.0098 0.0077 Ν-({4-[(6·Ga-2-fluoro-3-methylbenzene)sulfonyl]phenyl}A )-1Η-pyrazolo[3,4-b]nt bite-5-formamide 0.112 0.1-1 N-«4-[(6-gas_2·fluoro_3·methylbenzene)sulfonyl Phenyl}methyl)-1Η-ηpyrolo[3,2-c]pyridine-2-carboxamide 0.0065 0.0071 N-({4-[(6-Gas-2-fluoro-3-methyl) Benzenesulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 0.0219 0.0293 N-({4-[(6-Gas-2-fluoro-3-methyl) Benzenesulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0077 0.0068 Ν-({4-[1-(3-Phenylphenyl)-1Η-pyridyl) Azole-4- continued sulfhydryl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyrodo-5-carbamamine 0.0282 0.0556 Ν-({4-[1-(3- gas Phenyl)-1Η-»Bizozol-4-Continuyl]Phenyl}methyl)-lH-nfc[3,2-c]pyridyl-2-carboxamide 0.0169 0.0131 Ν-({4 -[1-(3-Phenylphenyl)-lH-〇tbazole-4-sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.0116 0.0140 Ν -({4-[1-(3-Phenylphenyl)_1Η·»Bizozol-4-sulfonyl-1phenyl}methyl)imidazo[l,2-a]pyridin-6-cartoamine 0.0140 0.0064 158436.doc -412- 201215609

Ν-({4-[1-(3-chlorophenyl)-1Η-pyrazole-4- continued indolyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-formamidine Amine 0.0022 0.0115 Ν-({4-[1-(3-Phenylphenyl)-1Η-«Bizozol-4-ylidene]phenyl}methyl)thieno[2,3-c]pyridine-bit 2-Proline amine 0.0041 0.0139 Ν-({4-[1-(4-fluorophenyl)_1Η_»Bizozole-4-branched]phenyl}indenyl)-1Η-»比咯和[3, 2-c]pyridin-2-carboxamide 0.0184 0.0066 Ν-({4-[1-(4-fluorophenyl)-1Η-pyrazole-4- continued indolyl]phenyl}indolyl) furan [2,3-c]pyridin-2-carboxamide 0.0069 0.0074 Ν-({4-[1-(4-fluorophenyl)-lH-nbazole-4-sulfonyl]phenyl}methyl Thio[2,3-c]pyridin-2-meramine 0.0045 0.0062 Ν-({4-[1-(propan-2-yl)-1Η-pyrazole-4- continued fluorenyl]phenyl }Methyl)imidazo[1,2-a]pyrodo-6-carboxamide 0.008 0.0027 Ν-({4-[1-methyl-3-(trifluoromethyl)-1Η-»-Bistazole- 4-sulfonyl]phenyl}methyl) imidazo[l,2-a]pyrodo-6-carboxamide 0.0299 0.0278 Ν-({4-[1-methyl-5-(trifluoromethyl) )-1Η-pyrazole-4-sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0534 0.0434 Ν-({4-[1 -methyl-5-(trifluoromethyl)-1Η-pyrazole-4-continuation (phenyl)methyl)imidazo[1,2-a]pyrimidine-6-decylamine 0.0040 0.0679 N-({4-[2-(3-fluorophenyl)-1,3-thiazole- 4-Mexyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyrodo-5-carboxamide 0.0271 0.0609 N-({4-[2-(3-fluorophenyl) )-1,3-thiazole-4- continued indolyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0.0192 0.0232 N-({4-[2 -(3-fluorophenyl)-1,3-thiazol-4-ylidene]phenyl}indolyl)furo[2,3-c]pyridin-2-carboxamide 0.0119 0.0504 N-({ 4-[2-(3-Fluorophenyl)-1,3-thiazol-4-ylindenyl]phenyl}indolyl)imidazo[l,2-a] ton bit-6-decylamine 0.0229 0.0128 N-({4-[2-(3-fluorophenyl)-1,3-thiazol-4-ylidene]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-A Indoleamine 0.0010 0.0069 N-({4-[2-(3-fluorophenyl)-1,3-thiazol-4- continued indolyl]phenyl}methyl)thiophene P,3-c]pyrobitone- 2-Proline Amine 0.0066 0.0244 N-({4-[2-(Benzyl)ethyl]phenyl}methyl)-1Η-»Bis-[3,2-c]«Bipyridine-2 -Artemisin 0.023 0.166 N-({4-[2-(Dimethylamino)pyrimidine-5-continuation-yl 1phenyl}indenyl)-1H-«Bizozolo[3,4-b ]Pyridine-5-carbamamine 0.0079 0.0059 N-({4-[2-(dimethylamino)) Bite -5-mercapto]phenyl}methyl succinyl[3,2-c]pyridyl-2-meramine 0.0190 0.0035 N-({4-[2-(dimethylamino)pyrimidine -5-wall sulfhydryl]phenyl}indolyl)furo[2,3-c]pyridin-2-carboxamide 0.0258 0.012 N-({4-[2-(dimethylamino)pyrimidine- 5-醢醢基]phenyl}indolyl)imidazo[l,2-a]pyrodo-6-carbamidamine 0.0229 0.0036 N-({4-[2-(diodecylamino)pyrimidine- 5-wall fluorenyl]phenyl}methyl)thieno[2,3-c]pyridin-2-carboxamide 0.0080 0.0017 N-({4-[2-(morpholin-4-yl)) pyridine -3-Continuation of fluorenyl 1 phenyl}fluorenyl) furo[2,3-c]pyridin-2-indoleamine 0.0325 0.0605 158436.doc -413- 201215609 N_({4-p-(morpholin-4 -yl)acridin-3·sulfonyl]styl}methyl)imidazo[1,2-a]°^^-6·carbamamine 0.0312 0.1-1 N-({4-[2-( Pyrrrolidin-1-yl)-1,3-thiazol-5-ytyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0028 0.0009 N- ({4-[2-(pyrrole-1-yl)-1,3-thiazol-5-continudyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyroline-2 -carbamamine 0.0060 0.0005 N-({4-[2-(pyrrole-1-yl)-1,3-thiazole-5-continudyl]phenyl}indolyl)imidazo[1,2-a Pyridine-6-oxime 0.0024 0.0004 N-({4-[2-(Pyrrolidin-1-yl)-1,3-thiazol-5-yl)]phenyl}methyl)imidazo[l,2-a]pyrimidine- 6-carbamide 0.0029 0.0009 N-({4-[2-(pyrrole-l-yl)-1,3-thiazole-5-continudyl]phenyl}methyl)thieno[2,3- c] pyridine 2-carbalamine 0.0015 0.0007 N-({4-[2-(trifluoromethyl)imidazo[l,2-a]pyrodo-6-continuation]phenyl}methyl )-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0497 0.0330 N-({4-[2-(trifluoromethyl)imidazo[l,2-a]〇ih bite -6-Continued thiol]phenyl}indolyl)furo[2,3-c]pyridine-2-cartoamine 0.0212 0.0119 N-({4-[2-(trifluoromethyl)imidazo[l ,2-a]pyridine-6-continudyl]phenyl}methyl)imidazo[l,2-a]pyrodo-6-carboxamide 0.0362 0.0070 N-({4-[2-(trifluoro) Methyl)imidazo[l,2-a] is more than -6-n-decyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.0031 0.0039 N-({ 4-[2-(Trifluoromethyl)-3-ylindolyl]phenyl}methyl)furo[2,3-c]pyridin-2-indoleamine 0.0304 0.0279 Ν-({4-[3 - gas-2-(hept-4-yl)pyridine-4- continued indolyl]phenyl}methyl)thieno[2,3-c]pyridyl-2-meramine 0.0085 0.0018 N-({ 4-[4 -(trifluoromethyl)pyridin-2-sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0283 0.0118 N-({4- [4-(Trifluoromethyl)nb-bit-2-indolyl]phenyl}methyl)&quot;Fu-[2,3-c]pyridine-2-carboxamide 0.0139 0.0061 N-({ 4-[4-(Trifluoromethyl group) 2-Phenyl]phenyl}methyl)imidazo[1,2-a]11 than bite-6-carbamide 0.0197 0.0032 N-( {4-[4-(Trifluoromethyl)acridin-2-sulfonyl]phenyl}methyl)- oxazolo[1,2·a] 唆-6-carbamamine 0.0087 0.0130 N-( {4_[4_(Trifluoromethyl)pyridine-2_Continued fluorenyl]phenyl}methyl)thieno[2,3-c]pyridin-2-decylamine 0.0036 0.0030 N-({4-[5 -(didecylamino)pyrazine-2-sulfonic acid Iphenyl}methyl)imidazo[l,2-a]pyrodo-6-carboxamide 0.016 0.0036 Ν-({4-[5 -(»Byrrolidin-1-yl)acridine-3-ylyl]phenyl}methyl)-1,3-benzothiazole-6-carboxamide 0.0092 0.1-1 N-({4- [5-(nt-bitid-1-yl)pyridine-3-ylidene]phenyl}methyl)-1Η-«carbazolo[3,4-b]&quot;bipyridin-5-carboxamide 0.0179 0.0040 N-({4-[5-(Pyrrolidin-1-yl)pyridine-3-sulfonic acid]phenyl}methyl)-1Η-pyrrolo[3,2-c]»bipyridine-2 -甲醯0.0139 0.0020 N-({4-[5-(pyrrole-1-yl)pyridine-3-sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-carboxamide 0.0228 0.0049 158436.doc •414- 201215609

N-({4-[5-(Pyrrolidin-1-yl)pyridine-3-sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridin-6-carboxamide 0.004 0.0005 N -({4-[5-(Trifluoromethyl)pyridine-2-sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridin-5-carboxamide 0.1 -1 0.1-1 N-({4-[5-(Trifluoromethyl)nfc pyridine-2- continued fluorenyl]phenyl}methyl)furo[2,3-c]pyridin-2-曱Indoleamine 0.0370 0.1-1 Ν·({4-[5-(trifluoromethyl)acridine-2·sulfonyl]phenyl}methyl)imidazo[1,2·a]°tb bite-6 -carbamamine 0.0463 0.0326 N-({4-[5-(trifluoromethyl) 吼-2- 醯 ])]phenyl}methyl)imidazo[1,2-a]pyrimidine-6- Indoleamine 0.0059 0.0708 N-({4-[5-(Trifluoromethyl)pyridin-2-cannonyl]phenyl}methyl)thieno[2,3-c]pyro-2-ene Indoleamine 0.0235 0.1-1 N-({4-[5-(trifluoromethyl)nb-bit-3-indolyl]phenyl}indolyl)-1Η-indolezolo[3,4-b] Pyridyl-5-carbamide 0.11 0.004 N-({4_[5-(trifluoromethyl)pyridine-3-sulfonyl]phenyl}methyl)imidazo[1,2-a]0tt bite- 6.Metformamide 0.009 0.0013 Ν-({4-[6-(1Η-pyrazol-1-yl)pyridine-3-sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine -6-decylamine 0.004 0.0019 N-({ 4-[6-(3,4-difluorophenyl)&quot;比唆-2- 醯 醯 】 phenyl} fluorenyl)-lH-°tb oxazo[3,4-b] pyridine-5 -carbamamine 0.0178 0.0410 N-({4-[6-(3,4-difluorophenyl)pyridin-2-wall oxime]phenyl}methyl)-1Η-pyrrolo[3,2- c]pyridine-2-cartoamine 0.0160 0.0127 N-({4-[6-(3,4-difluorophenyl)pyridin-2-ylindolyl]phenyl}methyl)furan[2, 3-c]pyridin-2-decylamine 0.0050 0.0427 N-({4-[6-(3,4-difluorophenyl)indole-2-sulfonyl-1phenyl}methyl)imidazo[ l,2-a]"tb bite-6-decylamine 0.0043 0.0057 N-({4-[6-(3,4-difluorophenyl)&quot; than bite_2_yl] phenyl} Thiol-based thieno-P,3-c]pyridin-2-meramine 0.0022 0.0132 N-({4-[6-(4-methylpiperazin-1-yl)pyridine-3-sulfonyl] Phenyl}fluorenyl)-1Η-pyrrolo[3,2-c]pyridyl-2-decylamine 0.006 0.0006 N-({4-[6-(di-decylamino) aryl] benzene Methyl-[3,4-b]pyrodo-5-carboxamide 0.0305 0.0033 N-({4-[6-(dimethylamino)pyridin-3-sulfonyl]phenyl} -1Η-pyrrolo[3,2-c]pyridin-2-decylamine 0.0209 0.0034 N-({4-[6-(didecylamino)nb -3-ylindolyl]phenyl }曱基)furo[2,3-c]pyridyl -2-decylamine 0.003 0.0018 N-({4-[6-(Dimethylamino)pyridine-3-sulfonyl]phenyl}indolyl)imidazo[1,2-3] bite- 6_decylamine 0.0449 0.0027 N-({4-[6-(2-decylamino)pyridin-3-continuation]phenyl}methyl)imidazo[l,2-a]pyrimidine-6- Methionamine 0.0027 0.0059 N-({4-[6-(Dimethylamino)pyridin-3-sulfonyl]phenyl}methyl)thieno[2,3-c]«tb bite-2 - brewing amine 0.001 0.0006 N-({4-[6-(morpholin-4-yl)pyridine-3- sureinyl]phenyl}methyl)-1Η-pyrazolo[3,4-b] Bite-5-decylamine 0.0057 0.0032 158436.doc -415- 201215609 N-({4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}methyl)-1Η -pyrrolo[3,2-c]pyridin-2-carboxamide 0.0096 0.0015 N-({4-[6-(morpholin-4-yl)pyridine-3-ylindolyl]phenyl}methyl Furan oxime 2,3-c]pyridine-2-carboxamide 0.002 0.0009 N-({4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}methyl) Imidazo[1,2-a]pyridine-6-formamide 0.0090 0.0015 N-({4-[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}methyl)imidazole And [1,2-a], bite-6-cartoamine 0.0011 0.0033 N-({4-[6-(N-Phen-4-yl)pyridin-3- sureinyl]phenyl}A Thio[2,3-c]pyridine-2-carboxamide 0.0041 0.0007 Ν-({4·[6-(trifluoromethyl)pyridine-2- continued fluorenyl]phenyl}methyl)-1H -pyrazolo[3,4-b]pyrodo-5-decylamine 0.0242 0.0111 N-({4-[6-(trifluoromethyl)bite_2_continuation]phenyl}methyl Furan [Με] pyridyl-2·carbamamine 0.0050 0.0031 Ν-({4-[6-(trifluoromethyl)pyridine-2-sulfonic acid]phenyl}methyl)imidazo[1, 2-a]Pyridine-6-decylamine 0.0087 0.0015 N-«4-[6-(Trifluoromethyl)pyridine-2- continued indolyl]phenyl}methyl)imidazo[1,2-8 ] Xiaobiting-6-carbamamine 0.0114 0.0204 Ν·({4_【6·(trifluoromethylhomopyridinylsulfonyl)phenyl}methyl)thieno[2,3-c]11 than bite- 2-Proline amine 0.0021 0.0022 Ν-({4-[6-(Trifluoromethyl)pyridine-3-sulfonyl I phenyl}methyl) thieno[2,3-c]pyridin-2- Methionamine 0.0076 0.0067 N-(l,3-benzothiazol-6-ylmethyl)-4-[(3-gasbenzene) benzyl]benzamide 0.050 &gt;10 Ν-[(4- {[2-(2,2,2-Trifluoroethoxy)-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl I-1H-pyrrolo[3,2-c] Pyridine-2-carbamide 0.009 0.0010 N-[(4-{P-(2,2,2-trifluoroethoxy)-4-(trifluoromethyl)benzene]sulfonyl}benzene Methyl)methyl oxazole [l,2-a]"tt bite-6-anthracene amine 0.007 0.0012 N-[(4-{[2-(oxy))5-(trifluoromethyl) Benzene]sulfonyl}phenyl)methyl]-1Η-°Λ 并[3,4-b]°tb bite-5-carbamamine 0.1-1 0.1-1 N-[(4-{[2 -(hydroxy)-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.1303 0.0259 N -[(4-{[2-(hydroxy))-5-(trimethyl)benzene Isulfonyl}phenyl)methyl I imidazo[l,2-a]pyrimidine-6- Amine 0.0332 0.1-1 N-[(4-{[2-(Dimethylamine))benzene]sulfonyl}phenyl)methyl]-1H-laloco[3,2-c]pyridine 2-carbamamine 0.1-1 0.1-1 N-[(4-{[2-(dimethylaminocarbamimidyl)benzene]sulfonyl}phenyl)methyl]furan[2,3- c]pyridine-2-carbamide 0.1-1 1-10 N-[(4-{[2-(dimethylaminocarbamimidyl)benzene]sulfonyl}phenyl)methyl]imidazo[l ,2-a]pyridine-6-carbamidamine&gt;0.1667 0.1-1 N-[(4-{[2-(dimethylaminocarbamimidyl)benzene]sulfonyl}phenyl)methyl]imidazole And [1,2-a] pyridine-6-anthraquinone 0.1-1 1-10 N-[(4-{[2-(dimethylamine))benzene]sulfonyl}phenyl) Methyl] thieno[2,3-c]pyridin-2-carboxamide 0.1-1 0. 1-1 N-[(4-{[2-(ethoxymethyl)benzene]sulfonyl}phenyl)methyl]-1Η-oxazolo[3,4-b]pyridine-5-A Brewing amine 0.0520 0.0612 158436.doc -416- 201215609

N-[(4-{[2-(ethoxy)hydrazino)benzene]sulfonyl}phenyl)methyl]-1Η-»Λ[3,2-c]pyridin-2-carboxamidine Amine 0.0185 0.0067 N-[(4-{[2-(ethoxymethyl)benzene] fluorenyl}phenyl)methyl]indolo[2,3-c]pyridine-2-carboxamide 0.0133 0.0260 N-[(4-{[2-(ethoxycarbonyl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-decylamine 0.0037 0.0396 N -[(4-{[2-(methylaminesulfonyl)benzene]sulfonyl}phenyl)methyl]-lH-nboxazolo[3,4-b]pyridine-5-carboxamide &gt ;0.167 &gt;10 N-[(4-{[2-(decylamine sulfonyl)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyran-2-yl Guanamine 0.0513 0.0740 N-[(4-{[2-(decylamine sulfonyl)benzene] sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6- formazan Amine 0.0304 1-10 N-[(4-{[2-(morphin-4-ylindenyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3,4-b] Pyridine-5-decylamine 0.0694 0.0465 N-[(4-{[2-(TM-4-ylmethyl)benzene]sulfonyl}phenyl)indolyl] oxazolo[l,2-a ]Pyridine-6-carbamamine 0.136 0.0342 N-[(4-{[2-(TM-yl)alkyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2 -a] pyrimidine-6-formamide 0.0145 0.1-1 N-[(4-{[2-(Trifluoromethoxy)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridine-2-carboxamide 0.0086 0.0146 N-[(4-{[2-(Trifluoromethoxy)benzene Isulfonyl}phenyl)methyl]imidazo[1,2_a]Nursing·6-decylamine 0.0024 0.0115 Ν-[ (4-{[2_(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-decabiidine-2-carboxamide 0.0194 0.0593 Ν·[(4·{[ 2_(Trifluoromethyl)benzene Isulfonyl}phenyl)methyl]isoxazo[l,2-a] bite·6·cartoamine 0.0341 0.0579 Ν-[(4-{[2-(three Fluoromethyl)benzene]sulfonyl}phenyl)methyl]isoazolo[1,2-a]pyrimidine-6-carboxamide 0.0100 0.1-1 N-[(4-{[2,4-double (trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-&quot;Bizozolo[3,4-b]pyridine-5-carbenamide 0.0816 0.0562 N-[(4-{ [2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)indenyl]-lH-nfc-[3,2-c]pyridin-2-carboxamide 0.0401 0.0140 N-[ (4-{p,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]pyrano[2,3-c]pyridine-2-carboxamide 0.0530 0.0637 Ν_[(4 -{[2,4·bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2·a]° ratio bite-6-anthracene 0.2 202 0.0532 N-[(4-{p,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[1,2-&amp;] bite-6-branched Amine 0.018 0.0964 N-[(4-{[2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl] aryl-[2,3-c]pyridine-2-carboxamidine Amine 0.0215 0.0043 Ν-[(4·{[2-chloro-H-trifluoromethyl)benzene 1 sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyrodo-5 -carbamamine 0.0365 0.0384 N-[(4-{[2- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-&quot;比比和[3,2 -c]bite-2-amylamine 0.0364 0.0088 158436.doc •417- 201215609 N-[(4-{[2- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indole Furan[2,3-c]pyridin-2-carboxamide 0.0184 0.0279 N-[(4-{[2- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl) Methyl]imidazo[l,2-a]pyrimidin-6-decylamine 0.0024 0.0246 Ν-[(4-{[2- gas-4-(trifluoromethyl)benzene] sulfonyl}phenyl) Methyl]-1Η-indolozolo[3,4-b]pyridine-5-cartoamine 0.114 0.0869 N-[(4-{[2-chloro-4-(trifluoromethyl)benzene]sulfonate }}phenyl)methyl]-1H-&quot;bibromo[3,2-c]pyridine-2-carboxamide 0.1269 0.0254 N-[(4-{[2-chloro-4-(trifluoromethyl) Benzene Isulfonyl}phenyl)methyl]pyrazolo[l,2-a]pyrimidine-6-carboxamide 0.0184 0.0644 N-[(4-{[2-Ga-5-(hydroxyindole) Base) phenyl 1 sulfonyl} phenyl) methyl]-1H-&quot; bis-[3,2-c] pyridine 2-mercaptoamine 0.0083 0.0262 N-[(4-{[2- -5-(Trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]-1Η-&quot;Bildo[3,2-c]pyridine-2-carbamide 0.0531 0.0120 N-[( 4-{[2-Ga-5-(trifluorodecyloxy)benzene]sulfonyl}phenyl)methyl] oxazolo[l,2-a]pyrimidine-6-nonylamine 0.0080 0.0125 N -[(4-{[2-chloro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]furan P,3-c]pyridin-2-carboxamide 0.0139 0.0141 N -[(4-{[2-chloro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyrimidine-6-carboxamide 0.0070 0.0141 N-[(4-{[2-H-3-(propan-2-yloxy)phenyl]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyro-6- Methionamine 0.0078 0.0040 N-[(4-{[2-Fluoro-3-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]Nandrolazole [l,2-a] Pyrimidine-6-formamide 0.0018 0.0070 N-[(4-{[2-fluoro-3-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]thieno[2,3 -cI Pyridyl-2-carboxamide 0.0047 0.0066 N-[(4-{[2-Fluoro-3-(tri-l-methoxy)benzene]sulfonyl}phenyl)methyl]pyrene P,3- c] pyridine 2-mercaptoamine 0.0098 0.0133 N-[(4-{[2-fluoro-4-(1Η-»oxazol-1-yl)benzene]sulfonyl}phenyl)indolyl]- 1H-pyrazolo[3,4-b]pyrodo-5-carbamidamine 0.0389 0.0344 N-[(4-{[2-fluoro-4-(1Η-α-pyrazol-1-yl)benzene]sulfonate Mercapto}phenyl)methyl]furo[2,3-c]pyridin-2-carboxamide 0.0184 0.008 N-[(4-{[2-fluoro-4-(1Η-lazolium-1-) Benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-decylamine0.00844 0.0128 N-[(4-{[2-fluoro-4-(1Η- Pyrazol-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0022 0.0190 N-[(4-{[2-fluoro- 4-(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1Η-α-pyrolo[3,2-c]pyridin-2-ylamine 0.0802 0.0281 N-[(4- {[2-Fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyro-6-cartoamine 0.0156 0.0157 N-[(4 -{[2-fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl I sinter[2,3-c]pyridine-2-carboxamide 0.0202 0.0423 N-[( 4-{[2-methoxy-3-(trifluoromethyl)benzene]sulfonate Yl} phenyl) Yue-imidazol-I-yl and [l, 2-a] pyrazol-6-bite Amides 0.0219 0.0148 158436.doc -418 · 201215609

N-[(4-{[2-methoxy-3-(3-trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-yl Amine 0.0094 0.0128 N-[(4-{[2-methoxy-4-(1Η-»Λ嗤-1-yl)benzene]sulfonyl}phenyl)methyl]-1Η-pyrazolop, 4-b]pyridine-5-carboxamide 0.0242 0.0094 N-[(4-{[2-methoxy-4-(1Η-η-pyrazol-1-yl)benzene]sulfonyl}phenyl) Furan-[2,3-c]pyridin-2-meramine 0.0065 0.006 Ν-[(4·{[2-methoxy-4_(1H-pyrazol-1-yl)benzene]sulfonate }}phenyl)methyl] imidazo[1,2-a]pyridin-6-decylamine 0.021 0.00359 N-[(4-{[2-曱oxy-4-(lH-ntazole-1 -yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidin-6-cartoamine 0.0032 0.0087 N-[(4-{[2-methoxy-4-( Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-lH_ ° is more than 嗤[3,4-b]11 than bite-5-decylamine 0.1200 0.0281 N-[(4-{[2 -Methoxy-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[1,2-a]pyro-6-carbamide 0.0264 0.00984 N-[(4 -{[2-methoxy-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyrimidine-6-decylamine 0.0044 0.0224 N -[(4-{[2-methoxy-4-(three) Methyl)benzene]sulfonyl}phenyl)methyl]thieno-P,3-c]pyridin-2-carboxamide 0.01 0.0022 N-[(4-{[2-methoxy-5-( Prop-2-yl)phenyl]sulfonyl}phenyl)indolyl-1Ι-»Bizozolo[3,4-b]pyrodo-5-carboxamide 0.0892 0.0294 Ν-[(4·{[ 2-methoxy-5-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]furan P,3-c]nt bite-2-cartoamine 0.0154 0.0124 N-[(4 -{[2-methoxy-5-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyro-6-nonylamine 0.0352 0.0064 N-[(4-{[2-methoxy-5((trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]-1H-0 is more than [3,4-b]nb Bite-5-method cavity 0.0926 0.0246 N-[(4-{[2-曱oxy-5-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[ 3,2-c]pyridin-2-carboxamide 0.0481 0.0066 N-[(4-{[2-methoxy-5-(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl Imidazo[l,2-a]pyrodo-6-carboxamide 0.0677 0.0144 N-[(4-{[2-methoxy-5-(trifluoromethoxy)benzene]sulfonyl}benzene Methyl)imidazo[l,2-a]pyrimidine-6-carboxamide &lt;0.00065 0.0058 N-[(4-{[2-methoxy-5-(trifluoromethyl)benzene] Sulfhydryl}phenyl)methyl Oxazo[1,2-a]pyrimidine-6-carboxamide 0.0068 0.0036 N-[(4_{[2-methyl-4_(1H-pyrazol-1-yl)benzene]sulfonyl}benzene Base) thiol]-1H-pyrazolo[3,4-b]pyrodo-5-carboxamide 0.0271 0.0235 N-[(4-{[2-methyl-4-(lH-nbazole-1 -yl)phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide 0.0062 0.006 N-[(4-{[2-methyl-4-(1Η) -pyrazol-1-yl)phenyl]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrodo-6-carboxamide 0.00799 0.0036 Ν-[(4·{[2- 4-(1Η-pyrazol-1-yl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.0015 0.0031 N-[(4 -{[2-methyl-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-indazolo[3,4-b]» than bite-5-carboxamide 0.1-1 0.0746 158436.doc -419- 201215609 N-[(4-{[2-Methyl-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-ΙΗ-nt [3,2-c]pyridine-2-carboxamide 0.0305 0.0253 N-[(4-{[2-mercapto-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl] bite M-[2,3-c]pyridine-2-cartoamine 0.0345 0.0631 N-[(4-{[2-methyl-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl Imidazo[l,2-a] Pyridin-6-formamide 0.0247 0.0166 N-[(4-{[2-methyl-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]isoxazo[l,2- a] pyrimidine-6-carbamide 0.0071 0.0511 N-[(4-{[2-mercapto-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2, 3-c]Pyridin-2-carboxamide 0.0103 0.0242 Ν-[(4-{[3-(1Η-&quot;Bizozol-1-yl)benzene]sulfonyl}phenyl)methyl]-1Η -»比比和[3,2-c]pyridine-2-cartoamine 0.0097 0.0074 N-[(4-{[3-(m-&quot;Biazol-1-yl)benzene]sulfonyl}benzene Methyl)furan p,3-c]pyridine-2-carboxamide 0.0075 0.0091 Ν-[(4-{[3-(1Η-«bisazol-1-yl)benzene]sulfonyl}benzene Methyl)imidazo[1,2-a]π ratio bite-6-formamide 0.0048 0.0062 Ν-[(4-{[3-(1Η-&quot;Biazol-1-yl)benzene]sulfonate Mercapto}phenyl)methyl]thieno-p,3-c]pyridin-2-carboxamide 0.0015 0.0001 N-[(4-U3-(2,2,2-trifluoroethoxy)benzene] Sulfhydryl}phenyl)methyl]furo[2,3-c]pyridin-2-carboxamide 0.0072 0.0120 N-[(4-{[3-(2,2,2-trifluoroethoxy) Benzo]phenyl]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-formamide 0.0150 0.0059 N-[(4-{[3-(2,2,2-3) Fluoroacetoxy Benzene]sulfonyl}phenyl)indolyl]isoxazo[1,2-a]pyrimidine-6-cartoamine 0.0055 0.0114 N-[(4-{[3-(2-methylpropoxy) Benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0285 0.0342 N-[(4-{[3-(2-) Propyloxy)phenyl]sulfonyl}phenyl)methyl]-1Η-»pyrolo[3,2-c]pyridin-2-carboxamide 0.0322 0.0143 N-[(4-{[3 -(2-methylpropoxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide 0.0148 0.0677 N-[(4-{[3- (2-methylpropoxy)benzene]sulfonyl}phenyl)methyl] oxazolo[l,2-a]pyridine-6-carboxamide 0.0157 0.0106 N-[(4-{[3- (2-methylpropoxy)benzene]sulfonyl}phenyl)methyl] oxazolo[l,2-a]pyrimidine-6-carboxamide 0.0039 0.0132 N-[(4-{[3- (2-methylpropoxy)benzene]sulfonyl}phenyl)methyl 1 fluorenyl[2,3-c]pyridin-2-carboxamide 0.0032 0.0252 N-[(4-{[3 -(3,5-dimercapto-1Η-»bisazol-1-yl)benzene]sulfonyl}phenyl)methyl]-1,3-benzothiazole-6-carboxamide 0.0179 0.1-1 N-[(4-{[3-(3,5-Dimethyl-1H-pyrazol-1-yl)benzene Isulfonyl}phenyl)methyl]-1H-pyrazolo[3,4 -b] pyridine 5-amine amide 0. 0253 0.0053 N-[(4-{[3-(3,5-Dimercapto-1H-pyrazol-1-yl)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3, 2-c]Pyridine-2-decylamine 0.0132 0.0016 N-[(4-{[3-(3,5-Dimercapto-1H-pyrazol-1-yl)benzene]sulfonyl}phenyl )methyl]-5-hydroxy-1H-indole-2-carboxamide 0.1-1 0.1-1 158436.doc -420- 201215609

N-[(4-{[3-(3,5-dimethyl-1Η-»bisazol-1-yl)benzene 1sulfonyl}phenyl)methyl]furan P,3-c]pyridyl 2-acetamide 0.0071 0.0035 N-[(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)benzene]sulfonyl}phenyl)indolyl] imidazole And [l,2-a] pyridine-6-nonylamine 0.0072 0. (10) 08 N-[(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)benzene Sulfhydryl}phenyl)indolyl] imidazo[l,2-a]pyrimidine-6-nonylamine 0.0018 0.0041 N-[(4-{[3-(3,5-dimethyl-1H) -pyrazol-1-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridin-2-indoleamine 0.0031 0.0015 N-[(4-{[3-(4 -fluorophenoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridin-6-decylamine 0.0151 0.0340 N-[(4-{[3-(4-fluoro) Phenoxy)phenyl]sulfonyl}phenyl)methyl]indeno[2,3-c]pyridine-2-carboxamide 0.0026 0.0656 N-[(4-{[3-(5-fluorenyl) -1,2,4-oxadiazol-3-yl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]&quot;biter-2-meramine 0.0079 0.0032 乂[ (4-{[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzene]sulfonyl}phenyl)indenyl]imidazo[l,2-a]pyrimidine -6-decylamine 0.0028 0.0023 N-[(4-{[3-(5-mercapto-1,2,4-oxadiazole) -3-yl)phenyl]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-indole 0.0033 0.0010 N-[(4-{[3-(cyclopentyl) Aminomethyl) phenyl] sulfonyl} phenyl) fluorenyl]-1H-carbazole hydrazine 3,4-b] pyridine 5-amine amide 0.0333 0.033 N-[(4-{[3- (cyclopentylamine-mercapto)phenyl]sulfonyl}phenyl)indolyl]furan P,3-c]pyroline-2_decylamine 0.0066 0.0226 N-[(4-{[3-( Cyclopentylamine-methyl hydrazino) phenyl]sulfonyl}phenyl) fluorenyl] oxazolo[l,2-a]pyrodo-6-decylamine 0.0103 0.0162 N-[(4-{[3- (cyclopentylamine-mercapto)phenyl]sulfonyl}phenyl)indolyl]isoxazo[l,2-a]pyrimidine-6-carbenamide 0.0047 0.0483 N-[(4-{[3 -(cyclopentylaminemethylmercapto)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridyl-2-meramine 0.0048 0.0138 N-[(4-{[3 -(diethylamine-mercapto)-5-fluorobenzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0093 0.0033 N- [(4-{[3-(Diethylaminoindenyl)-5-fluorobenzene]sulfonyl}phenyl)methyl]furo[2,3-c]nb-bit-2-carboxamide 0.0103 0.0038 N-[(4-{[3-(Diethylaminoindenyl)-5-fluorophenyl]sulfonyl)] phenyl] hydrazinyl] a] mouth bite-6-formamide 0.0047 0.0168 义[(4-{[3-(difluoromethoxy)benzene]sulfonyl}phenyl)methyl] gnato and p,3-c] pyridine -2-decylamine 0.0028 0.0030 N-[(4-{[3-(difluoromethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6 -decylamine 0.0021 0.0050 N-[(4-{[3-(dimethylaminesulfonyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyroline-2 -decylamine 0.0020 0.0032 N-[(4-{[3-(dimethylaminesulfonyl)benzene]sulfonyl}phenyl)indolyl] misxa[l,2-a] mouth bite- 6-carbamide 0.0020 0.0112 N-[(4-{[3-(乙烧横) benzene] sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridine- 2-decylamine 0.0170 0.0155 158436.doc •421 - 201215609 N-[(4-{[3-(Ethylene) phenyl] sulfonyl}phenyl)indolyl]furan P,3-c Pyridine-2-carbamide 0.0027 0.0032 N-[(4-{[3-(ethanesulfonyl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]0 ratio Bite-6-carbamamine 0.0135 0.0060 N-[(4-{[3-(Ethylene) phenyl] sulfonyl}phenyl)methyl]imidazo[1,2_carbamide 0.0027 0.0645 N -[(4-{[3-(Hexyl) phenyl) sulfonyl} benzene Methyl] phenantholine P,3-cl pyridin-2-carboxamide 0.0028 0.0054 N-[(4-{[3-(ethylaminemethanyl)benzene]sulfonyl}phenyl)methyl ] furo[2,3-c]pyridin-2-carboxamide 0.0060 0.0064 N-[(4-{[3-(ethylamine-mercapto)benzene]sulfonyl}phenyl)methyl] Oxazolo[l,2-a]pyrimidine-6-carboxamide 0.0031 0.0655 N-[(4-{[3-(methoxymethyl)benzene]] phenyl}methyl)-m -» than saliva and [3,4-b] pyridyl-5-carbamamine 0.0387 0.0394 N-[(4-{[3-(methoxymethyl)benzene]sulfonyl}phenyl)methyl 】-1H-indolo[3,2-c]pyridin-2-carboxamide 0.0202 0.0128 N-[(4-{[3-(methoxymethyl)benzene]sulfonyl}phenyl)曱基]吱吱[2,3-c]pyridine-2-carboxamide 0.0185 0.0134 N-[(4-{[3-(methoxyindolyl)benzene]sulfonyl}phenyl)methyl Imidazo[1,2-a]*nfc bite-6_cartoamine 0.0067 0.0068 N-[(4-{[3-(methoxymethyl)benzene]sulfonyl}phenyl)methyl 1 Imidazo[1,2-a] chito-6-cartoamine 0.0032 0.0138 N-[(4-{[3-(methoxymethyl)benzene]sulfonyl}phenyl)indolyl] And P,3-c]pyridine-2-carboxamide 0.0026 0.0067 N-[(4-{[3-(methylamine-mercapto)benzene]sulfonyl}phenyl)methyl] M-[2,3-c]pyridin-2-carboxamide 0.0081 0.0143 N-[(4-{[3-(indolylcarbamoyl)benzene]sulfonyl}phenyl)methyl] Zoxa[1,2-a]pyrimidine-6-carboxamide 0.0037 0.1-1 N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl] -1,3-benzothiazole-6-carboxamide 0.0401 1-10 N-[(4-{[3-(Nupolin-4-yl)benzene]sulfonyl}phenyl)indolyl I-1H -pyrazolo[3,4-b]pyridine-5-formamide 0.0167 0.0130 N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)indolyl] -lH-nb-[3,2-c]pyridine-2-carboxamide 0.0207 0.0106 N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)indole Base]-1Η-η比比和[3,2-c]pyrodo-2-cartoamine 0.0084 0.0017 N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl} Phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide 0.0050 0.0056 Ν-[(4·{[3-(morpholine-4-yl)benzene]sulfonyl}phenyl )methyl]imidazo[l,2-a] 11 to bite-6-formamide 0.0077 0.0033 N-[(4-{[3-(hept-4-yl)benzene]sulfonyl}phenyl Methyl Iisoxazole [l,2-a] pyridine-6-carbamide 0.0027 0.0135 N-[(4-{[3-(N-Phen-4-yl)benzene]sulfonyl}phenyl Methyl 1 嗟 eno[2,3-c]pyridine-2-yl Amine 0.0040 0.0019 -422 · 158436.doc 201215609

N-[(4-{[3-(Nylin-4-yl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide 0.0036 0.0032 N- [(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)methyl]_1,3_stupylthiazole-6-carboxamide 0.010 0.1-1 N-[(4 -{[3-(派)-1-yl)benzene]sulfonyl}phenyl)methyl]-1Η-&lt;·Bizozolo[3,4-b]pyrodo-5-decylamine 0.0536 0.0140 N-[(4-{[3-(Big)-1-yl)benzene]sulfonyl}phenyl)methyl I-lH-nfc-[3,2-c]pyran-2-yl Indoleamine 0.0144 0.0033 N-[(4-{[3-(Sessile-1-yl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide 0.0113 0.0127 N-[(4-{[3-(Lite-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-carboxamide 0.0114 0.0034 N-[(4-{[3-(派)-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0051 0.0114 N- [(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0012 0.0057 N-[( 4-{[3-(piperidin-1-yl)benzene Isulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-indoleamine 0.0167 0.0136 N-[(4- {[3-(派 bit-1-ylmethyl)benzene 1 sulfonate }}phenyl)methyl]imidazo[l,2-a]pyrodo-6-carboxamide 0.0091 0.0035 N-[(4-{[3-(piperidin-1-ylmethyl)benzene]sulfonate Mercapto}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-nonylamine 0.0019 0.0306 N-[(4-{[3-(propan-2-yl)benzene Isulfonyl) }phenyl)methyl]-1Η-»Bizozolo[3,4-b]pyridine-5-formamide 0.0139 0.0063 N-[(4-{[3-(propan-2-yl)benzene]sulfonate Mercapto}phenyl)methyl]furan[2,3-decapyridin-2-ylamine 0.0045 0.007 N-[(4-{[3-(propan-2-yl)benzene]sulfonyl} Phenyl) indenyl] imidazo[l,2-a]acridin-6-cartoamine 0.0124 0.00349 N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl )methyl]imidazo[1,2-a]pyrimidine-6-nonylamine 0.0029 0.0053 N-[(4-{[3-(propan-2-yloxy)benzene]sulfonyl}phenyl )methyl]-1Η-»Bizozolo[3,4_b]bite-5-nonylamine 0.0461 0.0245 N-[(4-{[3-(propan-2-yloxy)benzene]sulfonyl) }phenyl)methyl]furo[2,3-c]pyridin-2-decylamine 0.0126 0.0144 N-[(4-{[3-(propan-2-yloxy)benzene]sulfonyl }phenyl)indenyl]imidazo[1,2-8]bitat-6-decylamine 0.0023 0.0105 N-[(4-{[3-(propane-1-sulfonylamino)benzene]sulfonate Phenyl phenyl group Zoxa[1,2-a]pyrimidine-6-carbamide 0.0023 0.0862 N-[(4-{[3-(propane-1-sulfonylamino)benzene]sulfonyl}phenyl)indolyl Thio[2,3-c]pyrodo-2-cartoamine 0.0015 0.0032 N-[(4-{[3-(pyridin-2-yl)benzene]sulfonyl}phenyl)indolyl] Isozo[1,2-a] pyridyl-6-formamide 0.0219 0.0038 Ν-[(4-{[3·(pyrimidin-2-yl)benzene]sulfonyl}phenyl)methyl]imidazole And [l,2-a] shout bite -6-carbamamine 0.0032 0.0130 158436.doc •423 · 201215609 N-[(4-{[3-(&quot;比咯 bit-1-yl)benzene]sulfonate }}phenyl)methyl]-1,3-benzothiazol-6-carboxamide 0.0088 1-10 N-[(4-{[3-(&quot;pyrrolidin-1-yl)benzene]sulfonate Mercapto}phenyl)methyl]-1H-carbazolo[3,4-b]pyridine-5-carboxamide 0.0171 0.0128 N-[(4-{[3 1,4-buty-1-yl)benzene Sulfhydryl}phenyl)methyl]-1H-&quot;bibromo[3,2-c]pyridin-2-meramine 0.0134 0.0028 N-[(4-{[3-(pyrrole bite- 1-yl)phenylsulfonyl}phenyl)methyl]furo[2,3-c]pyridin-2-indoleamine 0.0082 0.0074 N-[(4-{[3-("pyrrolidine- 1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[Μη]11 than bite-6-formamide 0.0136 0.0016 Ν-[(4-{[3 decahydroridine- 1-yl)phenyl]sulfonyl}phenyl)methyl]-methazolo[1,2-a]pyrimidine-6-decylamine 0.0025 0.0041 N-[(4-{[3-(pyrrole bite-1 -yl)phenyl]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-meramine 0.0019 0.0025 N-[(4-{[3-(trifluoromethoxy) Benzene]sulfonyl}phenyl)indenyl]-1Η-»Bizozolo[3,4-b]»pyridin-5-formamide 0.0204 0.0071 N-[(4-{[3-(three Fluoromethoxy)phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide 0.0034 0.0067 N-[(4-{[3-(trifluoromethoxy) Phenyl]sulfonyl}phenyl)methyl]isoxazo[1,2-a]pyridin-6-nonylamine 0.00873 0.00318 N-[(4-{[3-(trifluoromethoxy)) Benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-formamide 0.0025 0.0027 N-[(4-{[3-(trifluoromethyl)benzene]sulfonate Mercapto}phenyl)methyl]-1,3-benzothiazole-6-carboxamide 0.006 0.5481 N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl) Methyl]-lH-nfcoxazolo[3,4-b]pyridine-5-carboxamide 0.0607 0.0104 N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl) Methyl]furo[2,3-decabiidine-2-carboxamide 0.0054 0.0048 N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl] Isozo[1,2-a] than bite-6-formamide 0.00842 0·(10) 172 N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl Imidazo[l,2-a]pyrimidine-6-carboxamide 0.0027 0.0030 N-[(4-{[3-chloro-4-(trifluoromethyl) benzene]sulfonyl}phenyl) ]]-1H-&quot;Bizozolo[3,4-b]pyridine-5-carboxamide 0.0843 0.0264 N-[(4-{[3-Ga-4-(trifluoromethyl)benzene]sulfonate }}phenyl)methyl]-1Η-&quot; 比比和P,2-c] pyridine 2-carboamine 0.0133 0.0077 N-[(4-{[3-chloro-4-(trifluoromethyl) Phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridin-2-decylamine 0.0079 0.0062 N-[(4-{[3- gas-4-(trifluoromethyl) Phenyl]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyridine-6-carboxamide 0.0029 0.0012 N-[(4-{[3-chloro-4-(trifluoro) Methyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyrimidine-6-formamide 0.0028 0.00-N-[(4-{[3-气-4-( Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide 0.0030 0.0023 158436.doc -424- 201215609

N-[(4-{[3-Ga-5-(diethylaminocarbamimidyl)benzene]sulfonyl}phenyl)methyl]furan P,3-c]&quot; Methionamine 0.0084 0.0017 N-[(4-{[3-chloro-5-(diethylaminocarbamimidyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine -6-carbamide 0.0009 0.0012 N-[(4-{[3-Ga-5-(diethylaminocarbamimidyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3- c] pyridine 2-carbamide 0.0023 0.0008 N-[(4-{[3- gas-5-(hydroxyindenyl)benzene]sulfonyl}phenyl)methyl] oxazolo[l,2 -a]Pyridine-6-decylamine 0.0058 0.0014 N-[(4-{[3-Ga-5-(hydroxymethyl)benzene]sulfonyl}phenyl)methyl]- oxazolo[1, 2-a] pyrimidine-6-carbamide 0.0034 0.0114 N-[(4-{[3-Ga-5-(hydroxymethyl)benzene]sulfonyl}phenyl)indolyl]thieno[2, 3-c]Pyridine 2-carbamide 0.0033 0.0008 N-[(4-{[3-Ga-5-(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-&quot ;Bizozolo[3,4-b]indolepyridin-5-formamide 0.0078 0.00273 N-[(4-{[3-Ga-5-(trifluoromethyl)benzene]sulfonyl}phenyl )methyl]-lH-indolepyr[3,2-c]pyridin-2-meramine 0.0199 0.0027 N-[(4-{[3-Ga-5-(trifluoromethyl)benzene] Sulfhydryl}phenyl)methyl]imidazole [1,2-a] pyrimidine-6-formamide 0.0044 0.0004 N-[(4-{[3-fluoro-4-(1Η" than sal-1-yl)benzene 1 sulfonyl}phenyl) Methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0131 0.0033 Ν-[(4-{[3-1-4-(1Η-pyrazin-1-yl)benzene) Sulfhydryl}phenyl)methyl]furo[2,3-c]pyridin-2-carboxamide 0.0173 0.005 N-[(4-{[3-fluoro-4-(1Η-pyrazole- 1-yl)phenyl]sulfonyl}phenyl)indenyl]imidazo[l,2-a]pyrodo-6-carboxamide 0.00537 0.00341 N-[(4-{[3-fluoro-4-( 2,2,2-Trifluoroethoxy)phenyl]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3,4-b]pyrodo-5-carboxamide 0.0103 0.0223 N-[ (4-{[3-H-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-methyl Indoleamine 0.0069 0.0238 N-[(4-{[3-fail-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2- a]»Bite-6-carbamamine 0.0150 0.008 N-[(4-{[3-Fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl) A Imidazo[1,2-a]pyrimidine-6-carbenamide 0.0044 0.0073 N-[(4-{[3-fluoro-4-(2,2,2-trifluoroethoxy)benzene] Sulfhydryl}phenyl)indenyl]thieno[2,3-c]pyridine-2-carboxamide 0.0046 0.0235 N-[(4 -{[3-Fluoro-4-(indolylthio)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridin-2-carboxamide 0.0123 0.0112 N-[( 4-{[3-Fluoro-4-(indolylthio)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]° ratio biting-6-formamide 0.0056 0.0027 Ν -[(4·{[3-fluoro-4-(indolylthio)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.0022 0.0020 N-[(4-{[3-Fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolylzolo[3,4-b]pyridin-5-carboxamide 0.0174 0.0137 N-[(4-{[3-Fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)indenyl]-1Η-η ratio 咯[3,2-cl pyridine 2-carbamamine 0.0262 0.0205 158436.doc -425- 201215609 N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl] And P,3_c]pyridine-2-carboxamide 0.0100 0.0156 N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene Isulfonyl}phenyl)methyl] [l,2-a]pyridine-6-formamide 0.0084 0.0063 N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl] Azolo[l,2-a]pyrimidine-6-carbamide 0.0040 0.0118 N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl Thio[], thieno[2,3-c]pyridine-2-carboxamide 0.0115 0.0115 N-[(4-{[3-H-4-(trifluoromethyl)benzene]sulfonyl}phenyl )methyl]-1Η-«比咯和[3,2-cI pyridine 2-carboamine 0.0103 0.0130 N-[(4-{[3-fluoro-4-(trifluoromethyl)benzene] sulfonate Mercapto}phenyl)methyl I oxime P,3-c]pyridin-2-carboxamide 0.0092 0.0137 N-[(4-{[3-fluoro-4-(trifluoromethyl)benzene] Sulfhydryl}phenyl)methyl]imidazo[l,2-a]pyridine-6-formamide 0.0402 0.0044 N-[(4-{[3-H-4-(trifluoromethyl)benzene] Sulfosyl}phenyl)methyl]mipropa[l,2-a]pyrimidine-6-carboxamide 0.0041 0.0069 N-[(4-{[3-fluoro-4_(trifluoromethyl)benzene) Isulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.0088 0.0072 N-[(4-{[3-fluoro-5-(2,2,2 -trifluoroethoxy)phenyl]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridine-5-cartoamine0.008 0.00482 N-[(4-{[ 3-fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0056 0.0019 N-[(4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c] Indole-2-carbamide 0.0074 0.0061 N-[ (4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6- Methionamine 0.0019 0.0015 N-[(4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl J thieno[2,3 -c]bite-2-carbamamine 0.0029 0.0035 N-[(4-{[3-fluoro-5-(2-methylpropoxy)benzene]sulfonyl}phenyl)methyl]-1Η -pyrazolo[3,4-b]pyridin-5-formamide 0112 0.00949 N-[(4-{[3-fluoro-5-(2-methylpropoxy)benzene]sulfonyl}benzene Methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0132 0.0070 N-[(4-{[3-Fluoro-5-(2-methylpropoxy)benzene) Sulfhydryl}phenyl)methyl]furo[2,3-c]pyridin-2-carboxamide 0.0103 0.0129 N-[(4-{[3-fluoro-5-(2-methylpropane) Oxy)phenyl]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-carboxamide 0.0113 0.003 N-[(4-{[3-Fluoro-5-(2- Methylpropoxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0031 0.0034 N-[(4-{[3-Fluoro-5- (2-methylpropoxy)benzene Isulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide 0.0048 0.0075 N-[(4-{[3-Fluorine -5-(morpholin-4-yl)benzene]sulfonyl}phenyl )methyl ΗΗ-»比比和[3,2-(:] acridine-2-decylamine 0.004 0.0008 N-[(4-{[3-fluoro-5-(morpholin-4-yl)benzene) Sulfhydryl}phenyl)methyl]imidazo[l,2-a]nfc -6-carbamamine 0.003 0.0006 158436.doc -426- 201215609

N-[(4-{[3-Fluoro-5-()-Butyl-1-yl)benzene]sulfonyl}phenyl)indolyl]N-oxazo[l,2-a]pyridine-6- Methionamine 0.0039 0.0022 N-[(4-{[3-Fluoro-5-(pyrrole-1-yl)benzene Isulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine -6-carbamamine 0.0031 0.0020 N-[(4-{[3-fluoro-5-(&quot;Bistyl-1-yl)benzene]sulfonyl}phenyl)indolyl] ,3-c] "Bistidine-2-carbamideamine 0.0012 0.0027 N-[(4-{[3-Fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-lH -nboxazolo[3,4-b]pyrodo-5-carbamamine 0.0112 0.00345 N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl) Methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0262 0.0036 N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene]sulfonyl} Phenyl) indenyl]furo[2,3-c]pyridine-2-carboxamide 0.0074 0.0050 N-[(4-{[3-Ga-5-(trifluoromethyl)benzene]sulfonyl} Phenyl)hydrazino]imidazo[1,2-a]pyrimidine-6-carboxamide 0.0059 0.0011 N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene]sulfonyl) }Benzene;&)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.0102 0.0031 Ν-[(4-{[4-(1-cyanocyclopentyl)benzene]sulfonate Mercapto}phenyl)methyl]-1H-indole[ 3,2-decabiidine-2-carboxamide 0.0601 0.0189 Ν-[(4-{[4-(1-cyanocyclopentyl)benzene]]] phenyl)methyl] 咬 并 [ 2,3-c]pyridine-2-carbamide 0.0080 0.0060 Ν-[(4-{[4-(1-cyanocyclopentyl)benzene]sulfonyl}phenyl)indolyl] l,2-a]Pyridine-6-decylamine 0.0107 0.0030 Ν-[(4-{[4-(1-Cyanocyclopentyl)benzene]sulfonyl}phenyl)methyl]isoxazole [l,2-a]pyrimidine-6-carbamide 0.0032 0.0047 Ν-[(4-{[4-(1Η-imidazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazole [1,2-a]pyrimidine-6-methanamine &lt;0.00065 0.0122 Ν-[(4-{[4-(1Η-imidazol-1-ylmethyl)benzene]sulfonyl}phenyl)methyl ] furan [2,3-c] bite-2-decylamine 0.0190 0.0137 Ν-[(4-{[4-(1Η-imidazolylmethyl)benzene]sulfonyl}phenyl)methyl Thio[2,3-c]pyridin-2-carboxamide 0.0053 0.0122 N-[(4- {[4-(lH-nboxa-1-yl)benzene]sulfonyl}phenyl) -1H-carbazolo[3,4-b]»tb bite-5-nonylamine 0.0123 0.0075 N-[(4-{[4-(lH-ntoxazol-1-yl)benzene]sulfonate } phenyl) fluorenyl] furo[2,3-c]pyridine-2-carboxamide 0.0041 0.0073 Ν-[(4-{[4-(2·methylpropoxy)benzene]sulfonyl) }benzene Methyl]-1H-pyrazolo[3,4-b]« than bite-5-formamide 0.0263 0.0162 N-[(4-{[4-(2-methylpropoxy)benzene] Sulfhydryl}phenyl)indenyl]-1Η-ηpyrolo[3,2-c]pyridine-2-carboxamide 0.0127 0.0094 N-[(4-{[4-(2-methylpropoxy) Phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridin-2-meramine 0.0094 0.0116 N-[(4-{[4-(2-mercaptopropoxy) Benzene]sulfonyl}phenyl)methyl]isoxazolo[1,2-a]bite-6-nonylamine 0.0022 0.0027 N-[(4-{[4-(2-mercaptopropyl) Oxy)phenyl]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-carboxamide 0.0055 0.0052 158436.doc -427- 201215609 N-[(4-{[4 -(2-methylpropoxy)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.0040 0.0103 N-[(4-{[4 -(4-ethoxyphenyl)benzene]sulfonyl}phenyl)methyl]-1Η-»pyrolo[3,2-c]pyridine-2-carboxamide 0.009 0.009 N-[(4 -{[4-(4-methylpiperazin-1-yl)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-5-carboxamide 0.004 0.0013 N-[(4-{[4-(4-Methylpiperazin-1-yl)benzene]sulfonyl}phenyl)methyl]-1H-&quot;比比和[3,2-c] Pyridyl-2-carboxamide 0.003 0.000 8 N-[(4-{[4-(4-methylpiperazin-1-yl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]bite-2-A Indoleamine 0.001 0.0005 N-[(4-{[4-(4-indolylpiperazin-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]-bito- 6-Methylamine 0.001 0.0002 N-[(4-{[4-(4-methyl). Qin-1-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine-2-carboxamide 0.001 0.0003 N-[(4-{[4-(difluoromethyl) ))-3-fluorobenzene]sulfonyl}phenyl)methyl]imidazo[1,2-a]pyrimidine-6-carboxamide 0.0082 0.0279 N-[(4-{[4-(ethoxy) Methyl)phenyl]sulfonyl}phenyl)methyl I-1H-carbazolo[3,4-b]pyrodo-5-carbenamide 0.0266 0.0128 N-[(4-{[4-(B Oxymethyl)benzene] phenyl]phenyl)indenyl]-1Η-»Biloze[3,2-c]pyridin-2-carboxamide 0.0125 0.0068 N-[(4-{[4 -(ethoxymethyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-carboxamide 0.0049 0.0066 N-[(4-{[4-(B Oxymethyl)phenyl]sulfonyl}phenyl)methyl]imidazo[1,2-a] bicose-6-carbamide 0.0027 0.0052 N-[(4-{[4-(ethylamine) Mercapto)phenylsulfonyl}phenyl)methyl]-indole-carbazolo[3,4-b]"pyridin-5-carbamide 0.103 0.0968 N-[(4-{[4- (ethylamine-mercapto)benzene]sulfonyl}phenyl)methyl]-1H-&quot;pyrolo[3,2-c]pyridin-2-ylamine 0.0145 0.0141 N-[(4 -{[4-(ethylamine-mercapto)benzene]sulfonyl}phenyl)methyl 1&quot; fuca-[2,3-c]pyridylpyridyl-2-carbamide. 0045 0.0067 N-[(4-{[4-(ethylamine)methyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2_a]pyridin-6-carboxamide 0.0120 0.0063 N -[(4-{[4-(ethylamine)methyl)benzene]sulfonyl}phenyl)methylimidazo[1,2-a]pyrimidine-6-carboxamide 0.0226 0.0878 N- [(4-{[4-(ethylamine)methyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]«pyridin-2-carboxamide 0.0015 0.0033 N- [(4-{[4-(hydroxymethyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-decabiidine-2-carboxamide 0.0049 0.0062 N-[(4-{ [4-(Hydroxymethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyridine-6-carboxamide 0.0142 0.0129 NI(4-{[4-(hydroxyl) Phenyl]sulfonyl}phenyl)methyl]thieno[2,3-c]nt-2-carboxamide 0.0038 0.0066 N-[(4-{[4-(morpholin-4-yl) Benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyrodo-5-carboxamide 0.00445 0.00247 158436.doc •428· 201215609

N-[(4-{[4-(morphin-4-yl)benzene]sulfonyl}phenyl)indolyl-1furo[2,3-c]pyridine-2-carboxamide 0.0046 0.0025 N- [(4-{[4-(morpholine-4-yl)benzene] sulfonyl}phenyl)indolyl]imidazo[l,2-a] 〇bite·6-曱 胺 amine 0.0035 0.0009 Ν- [(4-{[4-(N-Phen-4-yl)benzene]sulfonyl}phenyl)methyl]-oxazolo[l,2-a]pyrimidine-6-anthracene 0.0017 0.0040 N-[ (4_{[4-(?#-4-yl)benzene 1sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-decylamine 0.0016 0.0015 N-[(4- {[4-(propan-2-yl)benzene Isulfonyl}phenyl)indolyl 1 furo[2,3-decabiidine-2-carboxamide 0.0119 0.0080 N-[(4-{[4 -(propan-2-yl)benzene]sulfonyl}phenyl)indolyl] oxazolo[l,2-a]nt pyridine-6-carboxamide 0.0146 0.00666 Ν-[(4-{[4· (propion-2-yl)phenyl]sulfonyl}phenyl)indolyl]isoxazo[l,2-a]pyrimidine-6-carboxamide 0.0017 0.0081 N-[(4-{[4-(- _2-yloxy)phenyl]sulfonyl}phenyl)indenyl]-lH-ntoxa[3,4-b]pyridin-5-decylamine 0.0080 0.0066 N-[(4-{[4 -(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]pyrano[2,3-c]pyridin-2-decylamine 0.0068 0.0057 N-[(4-{[4 -(propan-2-yloxy)benzene]sulfonate }phenyl)methyl]isoxazo[1,2-a]pyrimidin-6-decylamine 0.0043 0.0032 N-[(4-{[4-(pyrrolidin-1-yl)benzene Isulfonyl} Phenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-6-nonylamine 0.006 0.0045 N-[(4-{[4-(&quot;比咯 bit-1-yl) Benzene]sulfonyl}phenyl)methyl]isoxazo[1,2-a]pyridine-6-decylamine 0.003 0.00- 14(N-[(4_{[4-(trifluoromethoxy)benzene]sulfonate Styrene}phenyl)methyl]-1Η-»biszolo[3,4-b]pyrodo-5-decylamine 0.0346 0.0223 N-[(4-{[4-(trifluorodecyloxy)) Benzene]sulfonyl}phenyl)methyl]&quot; fumaro[2,3-c]pyridine-2-carboxamide 0.0094 0.0277 N-[(4-{[4-(trifluoromethoxy)) Benzene]sulfonyl}phenyl)indolyl 1 oxazolo[1,2-a]bitite-6-nonylamine 0.0050 0.0176 ]\-[(4-{[4-(trifluoromethyl)benzene) Sulfhydryl}phenyl)methyl]-1Η-»biszolo[3,4-b]pyridin-5-decylamine 0.0199 0.0194 N-[(4-{[4-(trifluoromethyl)) Benzene]sulfonyl}phenyl)methyl]furo[2,3-decabiidine-2-carboxamide 0.087 0.0198 N-[(4-{[4-(trifluoromethyl)benzene]sulfonate }}phenyl)indolyl]imidazo[l,2-a] pyrimidine-6-nonylamine 0.0060 0.0235 N-[(4-{[4-Ga-2-(trifluoromethyl)benzene] Sulfhydryl}phenyl)indolyl]-1Η-pyrazolo[3,4-b]pyridine-5-indoleamine 0.147 0.0783 N-[(4-{[4-气_2_(trifluoromethyl) Benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0422 0.0174 N-[(4-{[4-气-2-( Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]trimium and P,3-c]pyridyl-2-carboxamide 0.0098 0.0254 N-[(4-{[4-气-2- (trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridin-6-nonylamine 0.0198 0.0085 158436.doc -429- 201215609 N-[(4- {[4-Ga-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl 1 oxazolo[1,2-a]pyrimidine-6-cartoamine 0.0079 0.0684 N-[( 4-{[4-Ga-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.0070 0.0096 N-[ (4-{[4-Gas-3-(trifluoromethyl)benzene] hydrazino}phenyl)methyl] benzo[2,3-c]pyridine-2-carbamide 0.0060 0.0069 N- [(4-{[4-Ga-3-(trifluoromethyl)benzene]]] phenyl)methyl] miso[1,2-a]pyridine-6-carboxamide 0.00984 0.00357 N -[(4-{[4- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyrimidine-6-carboxamide 0.0028 0. 0043 N-[(4-{[4-Fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indenyl]-indole-la-l-[3,2-c]pyridin 2-mercaptoamine 0.0254 0.0033 N-[(4-{[4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl I oxime [2, 3-c] pyridine-2-carbamide 0.0156 0.0139 N-[(4-{[4-fluoro-2-(propyl-2-yloxy)benzene]sulfonyl}phenyl) fluorenyl] Zoxa[1,2-a]pyrodo-6-carbamide 0.0222 0.0021 N-[(4-{[4-fluoro-2-(prop-2-yloxy)benzene]sulfonyl}phenyl曱 ]]] oxazolo[l,2-a]pyrimidine-6-formamide 0.0035 0.0150 N-[(4-{[4-fluoro-2-(propan-2-yloxy)benzene]sulfonate } phenyl) fluorenyl] thieno P,3-c] pyridine 2-carboximine 0.0050 0.0016 N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonate } phenyl) fluorenyl]-1H-&quot;Bizozolo[3,4-b]pyrodo-5-carbamamine 0.112 0.109 N-[(4-{[4-fluoro_2_(trifluoromethyl) Benzene]sulfonyl}phenyl)methyl]-1Η-»bido[3,2-c]pyridine-2-carboxamide 0.0270 0.0141 N-[(4-{[4-fluoro-2 -(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[l,2-a]pyridine-6-carboxamide 0.0040 0.0150 N-[(4-{[4-fluoro- 2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[ l,2-a]pyrimidine-6-formamide 0.0187 0.1-1 N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]叹 并[2,3-c]pyridine-2-carbamide 0.0064 0.0143 N-[(4-{[4-fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonate }}phenyl)methyl I-1H-pyrazolo[3,4-b]pyridin-5-formamide 0.01 0.0147 N-[(4-{[4-fluoro-3-(2,2,2) -trifluoroethoxy)phenyl]sulfonyl}phenyl)indenyl]-1H-pyrrolo[3,2-c]pyridine-2-cartoamine 0.0103 0.0065 N-[(4-{[4- Fluor-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]" is a bit of 2-methylamine 0.087 0.0255 N -[(4-{[4-fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6 -carbamamine 0.0024 0.0065 N-[(4-{[4-fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]thieno-P,3 -c] pyridine 2-carbamide 0.0033 0.0118 N-[(4-{[4-fluoro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-&quot; Bisazo[3,4-b]pyridine-5-carboxamide 0.0394 0.0138 Ν-[(4·{[4-Ga-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl ]-1Η-»比比和[3,2-c]〇比pyridine-2-carboxamide 0.0164 0.0043 158436.doc •430- 201215609

N-[(4-{[4-fluoro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridin-2-ylamine 0.0082 0.0072 Ν-[(4·{[4-)-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-oxazolo[1,2-a]pyridine_6-decylamine 0.0040 0.0017 N-[(4-{[4-Fluoro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]isoxazo[1,2-a]pyrimidine-6-oxime Amine 0.0080 0.0032 N-[(4-{[4-H-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-曱Indoleamine 0.0040 0.0028 N-[(4-{[4-曱-oxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-b ]pyridine-5-decylamine 0.0868 0.0628 N-[(4-{[4-methoxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-pyrrole [3,2-c]pyridin-2-ylamine 0.0804 0.0130 N-[(4-{[4-曱oxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl ]. Furano[2,3-c]pyridin-2-indoleamine 0.0146 0.0152 N-[(4-{[4-methoxy-2-(trifluoromethyl)benzene]sulfonyl}}phenyl )methyl]thiazolo[l,2-a]pyrimidine-6-formamide 0.0070 0.0657 N-[(4-{[4-methoxy-2-(trifluoromethyl)benzene]sulfonyl) }phenyl)methyl] 叹 并 P,3-c] pyridine 2-carbamoamine 0.0217 0.0130 N-[(4-{[5-(diethylamine)methyl)-2-fluorobenzene Sulfhydryl}phenyl)indenyl]_1H-pyrrolo[3,2-c]pyridyl-2-carboxamide 0.0384 0.0262 N-[(4-{[5-gas-2-(2, 2,2-Trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridin-6-decylamine 0.001 0.0003 Ν-[(4·{[5 - gas-2-(2,2-difluoroethoxy)benzene]sulfonyl}phenyl)methyl 1-1H-pyrrolo[3,2-c]pyridyl-2-meramine 0.005 0.0005 N-[(4-{[5-Gas-2-(2,2-difluoroethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6- Indoleamine 0.002 0.0003 N-[(4-{[5-Gas-2-(prop-2-yn-1-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2 -a]pyridine-6-formamide 0.007 0.0014 N-[(4-{[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]-indole- Oxazo[3,4-b]pyrodo-5-carbamamine 0.06 78 0.0271 N-[(4-{[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyran-2 -carbamamine 0.0091 0.0121 N-[(4-{[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a] Pyrimidine-6-decylamine 0.0047 0.0146 N-[(4-{[5-fluoro-2-(hydroxymethyl)benzene]sulfonyl}phenyl)methyl I-1H-pyrazolo[3, 4-b]Pyridine 5-carbamamine 0.109 0.1-1 N-[(4-{[5-fluoro-2-(ylmethyl)benzene]sulfonyl}phenyl)methyl]-lH -nb-[3,2-c]pyridin-2-carboxamide 0.0169 0.0675 N-[(4-{[5-fluoro-2-(hydroxymethyl)benzene]sulfonyl}phenyl) A Furan[2,3-c]pyridin-2-decylamine 0.0229 0.0670 N-[(4-{[5-fluoro-2-(ylmethyl)benzene]sulfonyl}phenyl) Methyl 1 oxazolo[l,2-a]pyrodo-6-decylamine 0.0104 0.0650 N-[(4-{[5-Gas-2-(hydroxymethyl)benzene Isulfonyl}phenyl) )methyl]imidazo[1,2-a]pyrimidine-6-nonylamine 0.0129 0.1-1 158436.doc •431 - 201215609 N-[(4-{[5-fluoro-2-(hydroxymethyl) Benzene]sulfonyl}phenyl)methyl]thieno-P,3-c]pyridin-2-carboxamide 0.0077 0.0249 N-[(4-{[5-trans-base_2_(trifluoromethoxy) Benzene]sulfonyl}phenyl) Methyl]-1H-&quot; than saliva[3,4-b]0 than bite-5-carbamide 0.019 0.0679 N-[(4-{[5-hydroxy-2-(trifluoromethoxy)) Benzene]sulfonyl}phenyl)methyl]pyrano P,3-c]pyridin-2-carboxamide 0.0064 0.0115 N-[(4-{2-[ethyl(methyl)amino] -1,3-thiazole-5-hydroxyl}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-5-carboxamide 0.0036 0.0015 N-[(4-{2- [Ethyl(methyl)amino]-1,3-thiazole-5-continuation-yl}phenyl)methyl]furo[2,3-c]pyridin-2-carboxamide 0.0048 0.0009 N- [(4-{2-[Ethyl(methyl)amino]-1,3-thiazole-5-continuous}}phenyl)methyl]imidazo[l,2-a]pyro-6- Aromatic amine 0.0033 0.0004 N-[(4-{2-[ethyl(methyl)amino]-1,3-thiazol-5-sulfonyl}phenyl)methyl] imidazo[l,2- a] pyrimidine-6-carbamamine 0.0018 0.0009 N-[(4-{2-[ethyl(methyl)amino]-1,3-thiazole-5-branched}phenyl)methyl] Thieno[2,3-c]pyridine-2-carboxamide 0.0029 0.0012 ]\-[(4-{511,611,711,811,911-imidazo[1,2-3]azet-3-醯)}phenyl)methyl]-1H-pyrazolo[3,4-b]pyridine-5-cartoamine 0.0316 0.0123 N-[(4-{5H,6H,7H,8H,9H-imidazole And [l,2-a] nitrogen -3-sulfonyl}phenyl)methyl Ifuro[2,3-c]pyridin-2-carboxamide 0.0060 0.0057 沁[(4-{511,611,711,811,911-imidazo[ 1,2-3]azetin-3-contigmentyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-formamide 0.11 0.0287 Buck [[4-{511,611, 711,811,911-imidazo[1,2-3]azhen-3-indolyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide 0.0030 0.0008 N- [(4-{6-Azamidazo[l,2-a]»ttidine-3-ylidene}phenyl)indolyl-1Ι-»Bizozolo[3,4-b]pyridine-5 -carbamamine 0.0033 0.0008 N-[(4-{6-azamidazo[l,2-a]pyridine-3-sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c Pyridine-2-indoleamine 0.0132 0.0014 N-[(4-{6-azamidazo[l,2-a]pyridin-3-ylidene}phenyl)methyl]furan[2,3- c] pyridine 2-mercaptoamine 0.0012 0.0004 N-[(4-{6-chloroimidazo[1,2-a]pyridine-3-ylidene}phenyl)methyl]imidazo[l, 2-a]Pyridine-6-carbamamine 0.0053 0.0004 N-[(4-{6-Azamidazo[l,2-a]« than bite-3-continuation)}phenyl)methyl]imidazole And [l,2-a] pyrimidine-6-carbamamine 0.0016 0.0004 N-[(4-{6-gas imidazo[l,2-a] Bite-3-continuation }}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.12 0.0004 N-[(4-(8-oxatricyclo[7.4.0.02 ,7]13-carbon-1(13),2,4,6,9,11-hexene-6-sulfonyl}phenyl)methyl]-1Η-pyrazolo[3,4-b] Pyridine-5-carbamideamine 0.021 0.00752 N-[(4-{8-oxatricyclo[7.4.0.02'7]tridecy-1(13),2,4,6,9,11-hexene -6-Continuation of fluorenyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide 0.0124 0.0128 Ν-[(4·{8-oxatricyclo[7.4.0.02'7 Trideca-1(13),2,4,6,9,11-hexene-6-hydroxyl}phenyl)indolyl]isoxazo[l,2-a]pyrimidine-6- Methionamine 0.0017 0.0029 N-[(4-{8-thiatricyclo[7.4.0.02,7]tridecy-1(13),2,4,6,9,11-hexene-6-continued醯}}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0035 0.0032

158436.doc -432- 201215609

N-[(4-{8-thiatricyclo[7.4.0.02'7] thirteen-l(13), 2,4,6,9,ll-hexene-6-diazonyl}phenyl )methyl]furo[2,3-c]pyridin-2-carboxamide 0.087 0.012 N-[(4-{8-thiatricyclo[7.4.0.02'7]tridecyl-l (13 ), 2,4,6,9,ll-hexene-6-continuation fluorenyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide 0.0018 0.0020 N-[( 4-{8-thiatricyclo[7.4.0.02'7]tridecy-1(13),2,4,6,9,11-hexene-6-diazonyl}phenyl)methyl] Thio[2,3-c]pyridin-2-carboxamide 0.0014 0.0043 N-{[4-({3-[(2-methylpropyl))indolyl]benzene}sulfonyl)benzene曱 }}}H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.0193 0.0458 N-{[4-({3-[(2-methylpropyl))aminomethyl] Benzenesulfonyl)phenyl]methyl}furo[2,3-c]pyridin-2-carboxamide 0.0169 0.0263 N-{[4-({3-[(2-methylpropyl)) Aminomethyl) phenyl} sulfonyl) phenyl] methyl} imidazo[l,2-a]pyrimidine-6-carboxamide 0.0070 0.0456 N-{[4-({3-[(2- Methylpropyl)aminemethanyl]phenyl}sulfonyl)phenyl]methyl}thieno[2,3-c]pyridin-2-carboxamide 0.0052 0.0145 N-{[4-({3 -[(didecylamino)methyl]phenyl}sulfonyl) Phenyl]fluorenyl}furo[2,3-c]nfcpyridine-2-carboxamide 0.0047 0.0062 N-{[4-({3-[(dimethylamino)indolyl]benzene}sulfonate Phenyl]methyl}imidazo[1,2-a]pyrimidin-6-decylamine 0.0044 0.0660 N-{[4-({3-[(Nol-4-yl)carbonyl)benzene}sulfonate Mercapto)phenyl]methyl}-1Η-pyrazolo[3,4-b]"pyridin-5-formamide 0.1235 0.1-1 N-{[4-({3-[(propyl-2) -yl)aminomethane]phenyl}sulfonyl)phenyl]methyl}furan P,3-c]pyridin-2-carboxamide 0.0151 0.0157 N-{[4-({3-[( Prop-2-yl)amine-carbamoyl 1 phenyl sulfonyl) phenyl]methyl oxazolidine [l,2-a] pyridine-6-decylamine 0.0222 0.0504 N-{[4-({ 3-[(propan-2-yl)aminoindenyl]phenyl}sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0070 0.0658 N-{[4 -({3-[(propan-2-yl)amine-carbamoyl]phenyl}sulfonyl)phenyl]methyl}thieno[2,3-c]pyridin-2-decylamine 0.0027 0.0067 4-({3-[2-(Didecylamino)ethoxy]phenyl}sulfonyl)phenyl]methyl}furan P,3-c]pyridyl-2-carboxamide 0.0118 0.0058 N-{[4-({3-[2-(Dimethylamino)ethyl 1 phenyl)sulfonyl)phenyl]methyl}-1Η-pyrrolo[3,2-c]pyridine -2-decylamine 0.02 92 0.0223 ]\-{[4-({3-[2-(Dimethylamino)ethyl)phenyl}sulfonyl)phenyl]methyl}imidazo[1,2-a]pyrimidine- 6-carbamide 0.0035 0.1-1 Ν-{[4-({3-[2-&amp;methylamino)ethyl]benzene}sulfonyl)phenyl]methyl}thieno-P,3- c] pyridine bit-2-carbamide 0.0025 0.0016 N-{[4-({3-[2-(TM)-4-yl)ethoxy]phenyl}sulfonyl)phenyl]methyl}-1Η · Pyrrolo[3,2-c]pyridin-2-decylamine 0.0649 0.0126 N-{[4-({3-[2-(Methyl)-4-yl)ethoxy]phenyl}sulfonyl) Phenyl 1 methyl}imidazo[l,2-a]pyrodo-6-carboxamide 0.0068 0.0034 N-{[4-({3-[2-(TM--4-yl)ethoxy) Benzenesulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0031 0.0247 N-{[4-({3-[2-(morpholin-4-yl) Ethoxy]phenyl}sulfonyl)phenyl]methyl}thieno[2,3-c]pyridin-2-carboxamide 0.0030 0.0015 158436.doc •433 - 201215609 N-{[4-( {4-[(lR)-l-hydroxybutyl]phenyl}sulfonyl)phenyl]indolyl]furo[2,3-c]pyridyl-2-carboxamide 0.0285 0.0122 N-{[4 -({4-[(lR)-l-hydroxybutyl]phenyl}sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0048 0.0142 N-{ [4-({ 4-[(didecylamino)methyl I phenyl sulfonyl)phenyl]methyl} oxazolo[l,2-a]pyrimidine-6-carboxamide 0.0033 0.0246 N-{[4 -({4-[(ntrrolidin-1-yl)carbonyl]phenyl}sulfonyl)phenyl]methyl}-1Η-pyrazolo[3,4-b]pyridin-5-carboxamide 0.0158 0.0093 Ν-{[4-({4-[()-Butyl-1-yl)carbonyl]phenyl}sulfonyl)phenyl]methyl}furo[2,3-c]pyridine-2- Methionamine 0.0015 0.0014 N-{[4-({4-[(pyrrolidin-1-yl)carbonyl)phenyl}sulfonyl)phenyl]methyl}thieno[2,3-c]pyridine-bit 2-Proline Amine 0.0037 0.0017 N-{[4-({4-[2-(Dimethylamino)ethyl)benzene}]]]]]]]]]]]] a] pyridine-6-anthracene amine 0.0021 0.0008 N-{[4-({4-[2-(didecylamino)ethyl]benzene} fluorenyl) phenyl] methyl hydrazine and [ l,2-a]pyrimidine-6-carbamide 0.0020 0.0181 N-{[4-({4-[2-〇&gt;pyrrolidin-1-yl)ethoxy]phenyl}sulfonyl) Phenyl]methyl}-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.003 0.0023 N-{[4-({4-fluoro-3-[(propan-2-yl)amine) Methylidene]phenyl}sulfonyl)phenyl]methyl}-1H-pyrazolo[3,4-b]pyridine-5-carboxamide 0.0852 0.0631 N-{[4-({4-Fluoro- 3-[(propan-2-yl)aminemethanyl] }sulfonyl)phenyl]methyl} imidazo[l,2-a]pyrimidine-6-carboxamide 0.0077 0.0854 N-{[4-({4-fluoro-3-[(prop-2-) Aminomethyl]phenyl}sulfonyl)phenyl]fluorenyl} thieno[2,3-c]pyridin-2-carboxamide 0.0213 0.0068 Ν-{[4-(1,3-thiazole) -2-Continuation of fluorenyl)phenyl]fluorenyl}furan p,3-c]pyrazole-2-carbamamine 0.0198 0.0786 Ν-{[4-(1,3-thiazol-2- continued oxime) Phenyl]methyl}imidazo[l,2-a]-specific bite-6-carbamamine 0.021 0.0994 Ν-{[4-(1,3-thiazol-2-ylindolyl)phenyl]methyl }Thiophene[2,3-c]pyrazole-2-carbamamine 0.0144 0.0751 Ν-{[4-(1,4-Dimethyl-1H-imidazol-2-yl)phenyl]methyl }furo[2,3-c]pyridin-2-decylamine 0.0607 0.1-1 Ν-{[4-(1,4-dimethyl-1H-miso-2-field-branched)phenyl] Methyl}imidazo[1,2-a]pyridin-6-carboxamide 0.1-1 0.0954 Ν-{[4-(1,4-dimercapto-1H-imidazole-2-thenyl)benzene Methyl]imidazo[1,2-a]pyrimidine-6-carboxamide 0.0316 1-10 Ν-{[4-(1,5-dimethyl-1H-imidazole-2- continued fluorenyl) Phenyl]methyl}furo[2,3-c]pyridyl-2-meramine 0.0574 0.0659 Ν-{[4-(1,5-dimethyl-1H-imidazole-2-continuous base) Phenyl Methyl}imidazo[l,2-a]pyridine-6-formamide 0.0309 0.0731 Ν-{[4-(1,5-dimethyl-1H-imidazol-2-sulfonyl)phenyl] Methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0329 1-10 Ν-{[4-(1-benzothiophene-7-thenyl)phenyl]decylpyrazole [3,4-b] Pyridine-5-formamide 099 0.0128 -434- 158436.doc 201215609

Ν-{[4-(1-benzothiophene-7-thenyl)phenyl]methyl}furo[2,3-c]pyridine-2-cartoamine 0.0049 0.0139 Ν-{[4-( 1-benzothiophene-7-phenylphenyl)phenyl]methyl}thieno[2,3-c]pyridine-2-cartoamine 0.0015 0.0015 Ν-{[4-(1Η-吲哚-7- Sulfhydryl)phenyl]methyl}-1Η-&quot;Bizozolo[3,4-b]»pyridin-5-methanamine 0.0147 0.0432 Ν-{[4-(1-methyl-1H- 1,3-benzothiazol-6-ytyl)phenyl]indenyl}imidazo[l,2-a]pyrimidine-6-carbenamide 0.0040 0.0338 Ν-{[4-(1-A -1-1H-carbazole-4-sulfonyl)phenyl]decyl 1,3-benzothiazol-6-nonylamine 0.0098 1-10 Ν-{[4-(1-mercapto-1H-吲 -4- -4- 醢 )) phenyl]methyl}-1 Η-pyrazolo[3,4-b]pyridine-5-decylamine 0.0203 0.0064 Ν-{[4-(1-methyl-1H -carbazole-4- continueinyl)phenyl]methyl}-1Η-pyrrolo[3,2-c]pyridyl-2-meramine 0.0031 0.0015 Ν-{[4-(1-methyl- 1H-carbazole-4- continued indolyl)phenyl]fluorenyl}furan p,3-c]pyridin-2-decylamine 0.0092 0.0036 Ν-{[4-(1-methyl-1H-吲 吲-4-sulfonyl)phenyl]methyl}imidazo[1,2-a]pyridin-6-carboxamide 0.0125 0.0030 Ν-{[4-(1-methyl-1H-吲嗤-4- Sulfon Phenyl] fluorenyl} imidazo[l,2-a] pyrimidine-6-formamide 0.0042 0.0103 Ν-{[4-(1-methyl-1H-carbazole-4- continued fluorenyl)benzene Thio[2,3-c]pyridine-2-carboxamide 0.11 0.0008 Ν-{[4-(1-methyl-1H-indazole-5-thenyl)phenyl]indole Keb 1H-pyrazolo[3,4-b]pyrodo-5-carbamamine 0.0054 0.00273 Ν-{[4-(1-mercapto-1H-indazole-5-continuation) phenyl] Methyl}-1Η-pyrrolo[3,2_c]pyrazole-2-meramine 0.0057 0.0031 Ν-{[4-(1-indolyl-1H-indazole-5-thenyl)phenyl]indole Furan[2,3-c]pyridin-2-decylamine 0.0033 0.0035 Ν-{[4-(1-methyl-1H-indazole-5-thenyl)phenyl]methyl}imidazole And [l,2-a] &quot;bite-6-cartoamine 0.0040 0.0016 Ν-{[4-(1-mercapto-1Η-carbazol-5-ylidene)phenyl]fluorenyl} Oxazo[l,2-a] pyrimidine-6-nonylamine 0.0017 0.0049 Ν-{[4-(1-methyl-1H-oxime-5-continuation)phenyl]indolyl}thiophene p,3-c] pyridin-2-decylamine 0.0015 0.0016 Ν-{[4-(1-methyl-1H-indazole-6-thenyl)phenyl]methyl}-1Η_pupazole And [3,4-b]pyridine-5-decylamine 0.004 0.0030 Ν-{[4-(1-methyl-1H-indazole-6-ylindolyl)phenyl]fluorenyl}-1Η- Pyrrolo[3,2-c]pyridin-2-decylamine 0.0051 0.0033 Ν-{[4-(1-indolyl-1H-indazole-6-ylindolyl)phenyl]fluorenyl}furan [2,3-c] Pyridin-2-carboxamide 0.0047 0.0034 Ν-{[4-(1-indolyl-1H-indazole-6-thenyl)phenyl]indenyl}imidazo[l, 2-a] pyridine-6-carbamide 0.0050 0.0039 Ν-{[4-(1-methyl-1H-indazole-6-thenyl)phenyl]indolyl}imidazo[l,2- a] pyrimidine-6-decylamine 0.0016 0.0050 158436.doc -435 - 201215609 Ν-{[4-(1-indolyl-1H-indazol-6-sulfonyl)phenyl]methyl}thiophene [ 2,3-c]pyridine-2-carbamide 0.0023 0.0011 Ν-{[4-(1-methyl-1H-carbazole-7- continued decyl)phenyl]methyl b 1H-pyrazolo[ 3,4-b]pyrodo-5-carbamamine 0.0918 0.0869 Ν-{[4-(1-methyl-1H-carbazole-7-thenyl)phenyl]methyl b 1H-pyrrolo[ 3,2-c]pyridin-2-carboxamide 0.0371 0.0111 Ν-{[4-(1-methyl-1H-carbazole-7-thenyl)phenyl]methyl}furan[2, 3-c] Pyridin-2-carboxamide 0.0115 0.0275 Ν-{[4-(1-indolyl-1H-carbazole-7-thenyl)phenyl]methyl}imidazo[1,2-a Pyridine-6-formamide 0.0287 0.0275 Ν-{[4-(1-methyl-1H-carbazole-7-continuation)phenyl]methyl}imi And [1,2-a] pyrimidine-6-formamide 0.0233 0.1-1 Ν-{[4-(1-mercapto-1H-carbazol-7-fluorenyl)phenyl]methyl}thiophene [2,3-c] Pyridin-2-cartoamine 0.0045 0.0104 Ν-{[4-(1-methyl-1H-indol-2-indolyl)phenyl]methyl]1H-pyrazole [3,4-b]pyridine-5-methanamine 0.0140 0.0132 Ν-{[4-(1-indolyl-1H-indole-2-sulfonic acid)phenyl]methyl}thieno[2, 3-c] Pyridin-2-carboxamide 0.0052 0.0034 Ν-{[4-(1-Methyl-1H-pyrazole-4-ethyl)phenyl]methyl}-1Η-pyrazolo[3 , 4-b]pyridine-5-formamide 0.182 0.1-1 Ν-{[4-(1-indolyl-1H-pyrazole-4-ylindolyl)phenyl]methyl}furan[2, 3-c] Pyridin-2-carboxamide 0.0168 0.0654 Ν-{[4-(1-methyl-1H-indazole--4-indolyl)phenyl]indolyl}imidazolium,2- a] pyrimidine-6-formamide 0.0082 0.1-1 Ν-{[4-(1-propyl-1H-pyrazole-4-methyl)phenyl]methyl}-1Η-pyrazolo[3 ,4-b]pyridine-5-carboxamide 0.08 0.0070 Ν-{[4-(1-propyl-1H-pyrazole-4-ylidene)phenyl]methyl}-1Η-pyrrolo[3 ,2-c]pyridin-2-indoleamine 0.0149 0.0059 Ν-{[4-(1-propyl-lH-nbazole-4-thenyl)phenyl]methyl}furan[2,3 -c] pyridine-2-carbamide 0.0057 0.0064 Ν_{[4·(1·propyl-1H-&quot;Bizozol-4-sulfonyl)phenyl]methyl}imidazo[l,2-a] ° ratio biting _6-formamide 0.0049 0.0052 Ν-{[4-(1-propyl-lH-nfcazole-4-indolyl)phenyl]methyl}thieno[2,3-c]pyridine-2-cartoamine 0.0019 0.0016 N -{[4-(2,3-dihydro-1,4-benzodioxan-6-ylidene)phenyl]methyl}furo[2,3-c]&quot; Pyridyl-2-carboxamide 0.0055 0.0062 N-{[4-(2,3-dihydro-1,4-benzodioxan-6-ylindole)phenyl]methyl}imidazo [1,2-a]pyrimidine-6-carbamimidin 0.0002 0.0005 N-{[4-(2,3-dihydro-1-benzofuran-7-diphenyl)phenyl]fluorenyl}-1Η -»Bizozolo[3,4-b]pyrodo-5-carbamamine 0.0248 0.0147 N-{[4-(2,3-dihydro-1-benzofuran-7-continuenyl)phenyl ]methyl b 1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0140 0.0038 N-{[4-(2,3-dihydro-1-benzofuran-7-yl) Phenyl]methyl}furo[2,3-c]pyridin-2-meramine 0.0060 0.0071 158436.doc •436· 201215609

N-{[4-(2,3-dihydro-1-benzofuran-7-continudyl)phenyl]indenyl}imidazo[l,2-a]pyridin-6-nonylamine 0.0125 0.0064 N-{[4-(2,3-dihydro-1-benzofuran-7-didecyl)phenyl]indenyl}imidazo[l,2-a]pyrimidine-6-nonylamine 0.0021 0.0258 N-{[4-(2,3-dihydro-1-benzofuran-7-ytyl)phenyl]indenyl}thieno[2,3-c]pyroline-2_ Amine 0.0022 0.0030 N-{[4-(2,6-didecyloxy) butyl-3-sulfonyl)phenyl]methyl}-1Η-»bisazolo[3,4-b]pyridine -5-decylamine 0.0307 0.0020 N-{[4-(2,6-Dimethoxypyridin-3-sulfonyl)phenyl]indenyl}furo[2,3-c]pyrobitone- 2-decylamine 0.0066 0.011 Ν·{[4-(2,6-dimethoxy-palladium_3·sulfonyl)phenyl]fluorenyl}imidazo[1,2-a] bite-6 -cartoamine 0.0433 0.0092 Ν-{[4-(2Η-1,3-benzodioxol-4- continued indolyl)phenyl]methyl}-1H-pyrazole[3,4 -b]pyridine-5-decylamine 0.047 0.0884 Ν-{[4-(2Η-1,3-benzodioxole-4-sulfonyl)phenyl]methyl}-1H-pyrrole And [3,2-c]pyridine-2-carboxamide 0.0205 0.0118 Ν-{[4-(2Η-1,3-benzodioxole-4- continued fluorenyl)phenyl]- Furan [2,3-cI acridine-2-carboxamide 0.0258 0.0266 Ν-{[4-(2Η-1,3-benzodioxole-4-continuous) phenyl ]Methyl}imidazo[1,2-a]pyrodo-6-nonylamine 0.0071 0.0130 Ν-{[4-(2Η-1,3-benzodioxole-4- sureinyl) Phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carbenamide 0.0029 0.0933 Ν-{[4-(2Η-1,3-benzodioxole-4- Continuation of the base) Phenyl]methyl}thieno[2,3-c]pyridin-2-carboxamide 0.0033 0.0072 Ν-{[4-(2Η-1,3-benzodioxole) -5- 醯 醯) phenyl] methyl}-ΙΗ-吼嗤 and [3,4-b] 0 than bite-5-formamide 0.0482 0.0074 Ν-{[4-(2Η-1,3- Benzodioxol-5-thenyl)phenyl]methyl}furo[2,3-&lt;:] 咬2-carbylamine 0.0053 0.0087 Ν-{[4-(2Η -1,3-benzodioxol-5-thenyl)phenyl]methyl}imidazo[l,2-a]pyrodo-6-carboxamide 0.0107 0.00533 Ν-{[4 -(2Η-1,3-benzodioxol-5-ytyl)phenyl-1-methyl}imidazo[1,2-a]pyrimidine-6-carbenamide 0.0030 0.0117 N- {[4-(2-methyl-1,3-thiazol-4- continueinyl)phenyl]methyl}-1Η-pyrazolo[3,4-b]nb -5-decylamine 0.0828 0.0207 N-{[4-(2-indolyl-1,3-thiazol-4- continueinyl)phenyl]methyl}furo[2,3-c]pyridine-2 -carbamamine 0.0367 0.0690 N-{[4-(2-mercapto-1,3-thiazole-4- continued fluorenyl)phenyl]indolyl}imidazo[l,2-a] pyridine-6- Indoleamine 0.0286 1-10 N-{[4-(2-mercapto-2H-carbazole-5-sulfonyl)phenyl]fluorenyl}imidazo[l,2-a] 0 ratio bite_6 - carbamide 0.0133 0.0058 Ν-{[4-(2-mercapto-2 Η-carbazole-5-hydroxyl)phenyl]indolyl}imidazo[1,2-a] pyrimidine-6-曱Indoleamine 0.0012 0.0082 N-{[4-(2-methyl-2H-indazol-5-sulfonyl)phenyl]methyl}thieno[2,3-c]pyridin-2-decylamine 0.0055 0.0033 158436.doc •437- 201215609 N-{[4-(2-Methyl-2H-indazole-6-sulfonyl)phenyl]methyl}-1Η-pyrazolo[3,4-b] Pyridyl-5-carbamamine 0.0147 0.0070 Ν-{[4-(2·methyl-2H-indazole-6-thenyl)phenyl]methyl}-1Η-pyrrolo[3,2-c 】Pyridine 2-carbamamine 0.0025 0.0032 N-{[4-(2-methyl-2H-indazole-6-thenyl)phenyl I methyl}furo[2,3-c]pyridine 2-carbamamine 0.0034 0.0028 N-{[4-(2-methyl-2H-indazole-6-sulfonyl)phenyl]indolyl}imidazo[1,2-a]pyridine-6- Brewing 0.0019 0.0017 Ν-{[4·(2·methyl-2H-carbazol-6-sulfonyl)phenyl]methyl}imidazo[l,2-a] Mocking-6-cartoamine 0.0012 0.0061 N-{[4-(2-methyl-2H-carbazol-6-carboxyl)phenyl]methyl}thienop,3-c]pyridine-2-carboxamide 0.0014 0.0015 N-{[ 4-(2-mercapto &quot;biten-3-n-decyl)phenyl]methyl}-1Η-»biszolo[3,4-b]pyridine-5-carboxamide 0.1045 0.1356 N-{ [4-(2-Methylacridin-3-indolyl)phenyl]methyl}-1Η-»Λ[3,2-c]pyridine-2-carboxamide 0.1803 0.0240 N-{[ 4-(2-methylpyridine-3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0208 0.1-1 N-{[4-(2- Methylpyridine-3-sulfonyl)phenyl]methyl}thieno[2,3-c]pyridine-2-carboxamide 0.0154 0.0119 N-{[4-(4-methyl&quot; 2-Continuation of fluorenyl)phenyl]methyl}furo[2,3-c]acridin-2-ylamine 0.0192 0.0114 N-{[4-(4-methylpyridine-3-sulfonyl) Phenyl]methyl}-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.1-1 0.2714 N-{[4-(4-methyl)pyridin-3- continued fluorenyl Phenyl]fluorenyl}-1Η-«bido[3,2-c]pyridine-2-carbamide 0.259 0.0258 N-{[4-(4-methylpyridine-3- Mercapto)phenyl]methyl}furo[2,3-c]pyridine-2-carboxamide 0.0252 0.062 N-{[4-(4-methylpyridine-3-sulfonyl)phenyl] A Imidazo[1,2-a]»pyridin-6-decylamine 0.0665 0.0658 N-{[4-(4-methylpyridine-3-sulfonyl)phenyl]methyl}imidazo[ l,2-a]pyrimidin-6-decylamine 0.0191 0.1-1 N-{[4-(4-methyl"pyridin-3-carbenyl)phenyl]methyl}thieno[2,3 -c]«Bistidine-2-carbamide 0.0292 0.0225 N-{[4-(4-mercaptothiophene-2-ylidene)phenyl]methyl}imidazo[l,2-a]»tb Bite-6-carbamamine 0.0124 0.0125 N-{[4-(5-gas-3-methyl 吼 bit-2-canonyl)phenyl]methyl b 1Η-»Bizozolo[3,4- b]pyridine-5-carboxamide 0.0625 0.0753 N-{[4-(5-gas-3-methylpyridin-2-continuation)phenyl]methyl}furo[2,3-c] Pyridine-2-carboxamide 099 0.0165 N-{[4-(5-gas_3_methylpyridin-2-yl)phenyl]indolyl}imidazo[l,2-a]pyridine- 6-carbamide 0.0188 0.0080 N-{[4-(5-gas-3-methylpyridin-2-continuation)phenyl]indolyl}imidazo[l,2-a]pyrimidine-6- Guanamine 0.0022 0.0220 158436.doc -438 - 201215609

N-{[4-(5-Gas-3-methylpyridin-2-ylidene)phenyl]methyl}thieno[2,3-c]pyridine-2-carboxamide 0.0039 0.0072 N- {[4-(5-gas&quot;bipyridyl-3-ylidene)phenyl]methyl}-1Η-»by-azolo[3,4-bppyridin-5-carboxamide 0.0238 0.0062 N- {[4-(5-Gas) is more than -3-ylindole) phenyl] fluorenyl}-1Η-«bido[3,2-c]咐·pyridine-2-carboxamide 0.0200 0.0036 N -{[4-(5-gas. than -3-sulfonyl)phenyl]methyl}imidazo[l,2-a] "pyridyl-6-cartoamine 0.0244 0.0032 N-{[4 -(5-fluoro-6-methylpyridine-2-sulfonyl)phenyl]methyl}furo[2,3-c]pyridine-2-carboxamide 0.0062 0.0124 N-{[4-(5 -Fluoro-6-mercaptopurine-2-mercapto)phenyl]indenyl}thieno[2,3-c]pyridine-2-carboxamide 0.0083 0.0071 N-{[4-(5-fluoro ° 咬 -3- 醢 ) ) ) ) ) ) ) ) ) ) ) ) ) 苯基 苯基 苯基 〇 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 792 792 792 792 792 792 792 792 792 792 Fluorine" is a phenyl group] methyl}-1Η-pyrrolo[3,2-c]»ifc pyridine-2-cartoamine 0.0713 0.0136 N-{[4-(5-fluorine) &quot;Bit-3-Binyl)Phenyl]methyl}imidazo[l,2-a]&quot;Bite-6-carbamamine 0.0278 0.0137 N-{[4-(5-fluoro)Λ Pyridine -3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0067 0.0564 N-{[4-(5-fluoropyridin-3-ylidene) Phenyl]methyl}thieno[2,3-c]pyridin-2-carboxamide 0.0097 0.0064 N-{[4-(5-methoxypyridin-2-ylindolyl)phenyl]methyl }furo[2,3-c]pyridine-2-cartoamine 0.0079 0.0316 N-{[4-(5-methoxy acetophenone-2-contigmentyl)phenyl]methyl}imidazo[l ,2-a]»Bistidine-6-formamide 0.0229 0.0173 N-{[4-(5-methoxypyridine-2-sulfonyl)phenyl]methyl}thieno[2,3-cl Pyridine-2-carboxamide 0.0071 0.0193 N-{[4-(5-decyloxy-3-n-decyl)phenyl]methyl}-1Η-indolozolo[3,4-b]pyridin Bite-5-decylamine 0.0414 0.0167 N-{[4-(5-methoxy)pyridin-3-ylidene)phenyl]indolyl}imidazo[l,2-a]-pyridin-6 -carbamamine 0.0090 0.0034 N-{[4-(5-methoxy)pyridin-3-yl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6- Amine 0.0016 0.0258 N-{[4-(5-methoxypyridine_3·continuenyl)phenyl]methyl}thieno[2,3-decabiidine-2-carboxamide 0.0090 0.0016 N-{ [4-(5-fluorenyl) is more than -3-indolyl) phenyl I hydrazino} imidazo[1,2-a] pyridine-6- Methionamine 0.0368 0.0071 N-{[4-(5-methyl) than bitten-3-n-decyl)phenyl]indolyl}imidazo[1,2-a]pyrimidine-6-carboxamide 0.0022 0.0124 N-{[4-(5-Methylpyridine-3-indolyl)phenyl]methyl}thieno[2,3-c]pyridine-2-carboxamide 0.0060 0.0025 N-{[4- (5-Methylthiophene-2-sulfonyl)phenyl]fluorenyl}-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide 0.023 0.0347 158436.doc -439- 201215609 N- {[4-(6-Methoxynaphthalene-2-ylindenyl)phenyl]methyl b 1H-&quot;Bildo[3,2-c]pyridine-2-carbamide 0.0099 0.0051 N-{ [4-(6-Methoxynaphthalene-2-continuation)phenyl]methyl}furo[2,3-c]»tb pyridine-2-carboxamide 0.0030 0.0036 N-{[4-( 6-Methoxynaphthalene-2-methylphenyl)phenyl Imethyl}isoxazo[l,2-a]pyridine-6-carboxamide 0.0027 0.0018 N-{[4-(6-methoxy Naphthalene-2-branched)phenyl]methyl}thieno[2,3-decapyridin-2-ylamine 0.0015 0.0033 N-{[4-(6-methoxypyrene-2-wall Mercapto)phenyl]mercapto}furo[2,3-c]pyridin-2-carboxamide 0.0025 0.0032 N-{[4-(6-methoxy&quot; ratio &lt; Base) phenyl]methyl}imidazo[l,2-a]» than bite-6-nonylamine 0.0052 0.0013 ·{[4-(6-Methoxypyridine-2-ylindenyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0022 0.0059 N-{[4- (6-methyl)pyrazine-2-thinyl)phenyl]indolyl 1Η-&quot;Bizozolo[3,4-b]pyridine-5-decylamine 0.0349 0.0312 N-{[4- (6-曱基&quot;比嗓-2-Continuation) phenyl]methyl}furo[2,3-c]&quot;bipyridyl-2-decylamine 0.0209 0.0097 N-{[4-( 6-methylpyridin-2-indolyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0010 0.0525 N-{[4-(6-methyl" ratio Pyrazin-2-sulfonyl)phenyl]methyl}thieno[2,3-c]acridin-2-ylamine 0.0048 0.0051 N-{[4-(6-methylpyridine-2-brew Phenyl]methyl]methyl}furo[2,3-c]pyridin-2-carboxamide 0.0128 0.0125 N-{[4-(6-methyl 吼-3--3- phenyl) phenyl] }}-1Η-carbazolo[3,4-b]pyridine-5-carboxamide 0.0241 0.0213 N-{[4-(6-methyl'•bipyridin-3-yl)phenyl] A }}-1Η-〇bido[3,2-c]pyridin-2-decylamine 0.0557 0.0130 N-{[4-(6-fluorenyl-•pyridin-3-sulfonyl)phenyl] Methyl}imidazo[l,2-a]&quot;bipyridine-6-carbamide 0.0150.0139 N-{[4-(6-methylpyridine- 3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidin-6-nonylamine 0.0059 0.0555 N-{[4-(6-fluorenyl)pyridin-3-sulfonyl Phenyl]methyl}thieno[2,3-c]»pyridin-2-carboxamide 0.0220 0.0063 N-{[4-(phenylsulfonyl)phenyl]methyl}-[1,3 Thiazolo[5,4-c]acridin-2-carboxamide 0.220 &gt;10 N-{[4-(phenylthenyl)phenyl]methyl}-1,6-acridine_2_ Indoleamine 2.85 &gt;10 N-{[4-(phenyl decyl)phenyl 1 methyl}-1 Η-pyrrolo[3,2-c]pyridine-3-carboxamide 1.91 2.06 N-{[ 4-(Benzene fluorenyl)phenyl-1-methyl}furo[2,3-c]pyridin-2-carboxamide 0.007 0.0088 N-{[4-(Benzene)phenyl]methyl }Zimidazo[l,2-a]pyrimidine-6-carbenamide 0.002 0.057 N-{[4-(Benzene)phenyl]methyl}quinoline-6-carboxamide 0.108 &gt;10 N-{[4-(cyclohexene fluorenyl)phenyl]methyl-pyrano[3,2-c]&quot;bipyridin-2-carbamide 0.005 0.0176 -440- 158436.doc 201215609

N-{[4-(dimethyl-1,3-thiazol-5-thenyl)phenyl]methyl}-1Η-pyrazolo[3,4-b]pyridin-5-decylamine 0.0386 0.0164 N-{[4-(Dimercapto-1,3-thiazol-5-sulfonyl)phenyl]indolyl}furo[2,3-c]pyridine-2-carboxamide 0.083 0.0103 N -{[4-(Dimethyl-1,3-thiazol-5-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyridin-6-carboxamide 0.009 0.0037 N-{[ 4-(Dimethyl-1,3-thiazole-5-cross-branched)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide 0.0037 0.0495 N-{[4-( Dimethyl-1,3-thiazole-5-benzyl)phenyl]methyl}thienop,3-c]pyridine-2-carboxamide 0.0013 0.0030 N-{[4-(furan_2· N-{[4-(isoquinolin-4- sure) Methyl}-1Η-&quot;Bizozolo[3,4-b]&quot;Bistidine-5-carbamide 0.0037 0.0025 N-{[4-(isoquinolin-4-ylindolyl)phenyl ]曱基}-1Η-»比比和[3,2-c]〇比pyridine-2-carboxamide 0.0109 0.0016 N-{[4-(isoindolin-4-yl)phenyl]indole Keef drink and [2,3-c]"tt^-2_ methotrexate 0.0190 0.003 N-{[4-(isoquinoline-4-ylindolyl] phenyl]methyl}imi And [l,2-a]»Bite-6-carbamamine 0.0224 0.0041 N-{[4-(isoquino-4--4-sulfonyl)phenyl]methyl}imidazo[1,2-a ]Umidine-6-carbamamine 0.0016 0.0032 N-{[4-(isoquinolin-4-continuation)] phenyl]methyl}thieno[2,3-c]pyrodo_2· formazan Amine 0.0067 0.0008 N-{[4-(Naphthalene-1-sulfonyl)phenyl]methyl bromide-bitrazole [3,4-b]» than bite-5-carbamamine 0.0091 0.00368 N-{ [4-(naphthalene-1-thenyl)phenyl-1-indenyl]furo[2,3-indolyl-2-carboxamide 0.0049 0.0031 N-{[4-(naphthalene-1-sulfonyl) Phenyl]fluorenyl}imidazo[l,2-a]pyrimidine-6-carbenamide 0.0029 0.0036 N-{[4-(morphothia-4-indolyl)phenyl]indolyl}- 1Η-»Bizozolo[3,4-b]«pyridin-5-carboxamide 0.0148 0.0204 N-{[4-(morphine-purified-4-decyl)phenyl]methyl}furan p ,3-c]Pyridine-2-carbamamine 0.0056 0.0131 N-{[4-(Phenyloxy-4-yl)phenyl]methyl}imidazo[l,2-a]acridine- 6-Methylamine 0.00215 0.00218 N-{[4-(Phenylthio-4-ylindolyl)phenyl]methyl}imidazo[1,2-a]pyrimidine-6-carbenamide 0.0021 0.0042 N -{[4-(Pyridine-2-indolyl) phenyl] fluorenyl[2,3-c]pyridin-2-ylamine 0.0551 0.08 70 N-{[4-(pyridine-3-sulfonyl)phenyl]methyl}furo[2,3-c]pyridin-2-carboxamide 0.0090 0.0664 N-{[4 ten bite- 3-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-decylamine 0.0059 0.1-1 158436.doc -441 - 201215609 N-{〖4-quinoline- 3-sulfonyl)phenyl]methyl}-1Η-«biazolo[3,4-b]»ifcidine-5-carbamamine 0.0052 0.0044 N-{[4-(quinoline-3- continued Mercapto)phenyl]methylpyrolo[3,2-c]«•bite- 2-formamide 0.0163 0.0029 N-{[4-(Quinolin-3-continuation)phenyl] A Furano[2,3-c]pyridine-2-carboxamide 0.0042 0.0032 N-{[4-(quinoline-3-methyl)phenyl]methyl}imidazo[1,2-3 Acridine-6-formamide 0.014 0.001 N-{[4-(Quinzin-3-Continuo)phenyl-1-methyl}imidazo[l,2-alpyrimidine-6-carboxamide 0.0025 0.0036 N -{[4-(quinoline-3-indolyl)phenyl 1 methyl}thieno[2,3-c]pyridine-2-carboxamide 0.0044 0.0009 N-{[4-(Quinline-6 - Item phenyl) phenyl] methyl b 1H-pyrazolo[3,4-b] pyridine- 5-carbamide 0.0101 0.0041 N-{[4-(quinolin-6-ylindolyl)benzene Methyl}furan[2,3-c]pyridin-2-carboxamide 0.0073 0.005 N-{[4-(quinoline-6-continued Phenyl)methyl}imidazo[l,2-a]pyrene-6-carbamamine 0.00516 0.00083 N-{[4-(Quinolin-6-sulfonyl)phenyl]methyl} Imidazo[l,2-a]pyrimidine-6-carboxamide 0.0033 0.0056 N-{[4-(Quinoxa-8-sulfonyl)phenyl]methyl J-1H-&quot;Bizozolo[3 , 4-b] acridine-5-carbamamine 0.0455 0.0236 N-{[4-(quinoline-8-continuous)phenyl]methyl}furo[2,3-c]pyroline-2 -carbamamine 0.0076 0.0060 N-{[4-(quinoline-8-thenyl)phenyl]methyl}imidazo[l,2-a]"biter-6-nonylamine 0.0098 0.0055 N- {[4-(Quinolin-8-Methyl)phenyl]methyl}imidazo[1,2-a]pyrimidine-6-carboxamide 0.0030 0.0277 N-({4-[(2,4- Dimethoxyphenyl)amine sulfonyl]phenyl}methyl-[3,2-c]»pyridin-2-ylamine 0.0058 0.0069 N-[(4-{[2-(2- Hydroxyethyl)phenyl]amine sulfonyl}phenyl)methyl]-1Η-»Λ 并[3,2-c]pyridine-2-carboxamide 0.0188 0.0199 N-({4-[( 5-fluoro-2-methoxyphenyl)amine sulfonyl]phenyl}methyl)quinoline-6-carboxamide 0.0660 1-10 N-({4-[(2,3,6-three) Nonyloxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide 0.012 0.0055 N-( {4-[(2,3-Dimethoxy-5-methylphenyl)-indolyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.010 0.002 N-({4-[(2,3-Dimethoxy-5-methylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-carboxamidine Amine 0.006 0.0027 N-({4-[(2,3-Dimethoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.009 0.0034 N -({4-[(2,3-dimethylphenyl)sulfonyl]phenyl}methyl)-1Η-indole-[3,2-c]pyridine-2-carboxamide 0.014 0.007 • 442· 158436.doc 201215609

N-({4-[(2,3-Dimercaptophenyl))]phenyl}methyl)thieno[2,3-c]»pyridin-2-carboxamide 0.011 0.0044 N-( {4-[(2,4,5-trimercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]»tfc pyridine-2-carboxamide 0.0088 0.008 N-({ 4-[(2,4,6-tridecylbenzene) hydrazino]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-ylamine 0.076 0.046 N-({ 4-[(2,4-Dioxaoxybenzene)sulfonyl]phenyl}indenyl)-1Η-indolepyrrolo[3,2-c]pyridyl-2-meramine 0.027 0.007 N- ({4-[(2,4-dimethylphenyl) hydrazino]phenyl}indolyl)_lH-nb-[3,2-c]pyridine-2-carboxamide 0.021 0.012 N-({ 4-[(2,4-dimercaptophenyl)methylene]phenyl}indenyl)thieno[2,3-indolyl-2-carboxamide 0.012 0.0222 N-({4-[(2 ,5-dimethoxybenzene) continued fluorenyl Iphenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0.017 0.006 N-({4-[(2 ,5-didecyloxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-cartoamine 0.004 0.0023 N-({4-[(2,5-II) Mercaptobenzene)sulfonyl]phenyl}methyl)-1Η-lado[3,2-c]pyridin-2-decylamine 0.011 0.014 N-({4-[(2,5-dioxin) Benzosulfonyl]phenyl}indenyl)thieno[2, 3-c]pyridin-2-decylamine 0.011 0.0086 N-({4-[(2,6-Dimethoxy-4-methylphenyl)sulfonyl-1phenyl}methyl)-1Η-pyrrole And [3,2-c]pyridin-2-carboxamide 0.016 0.010 N-({4-[(2,6-dimethoxy-4-mercaptophenyl)sulfonyl]phenyl}fluorenyl) Thiophene P,3-c]pyridyl-2-decylamine 0.007 0.0030 N-({4-[(2-ethylindenylbenzene) hydrazino]phenyl}methyl)-1Η-&quot; Butyr[3,2-c]pyridin-2-decylamine 0.006 0.004 N-({4-[(2-Ethylphenyl)sulfonyl]phenyl}methyl)thieno-p,3-c ]. Specific bite - 2-decylamine 0.001 0.0010 N-({4-[(2-Ga-6-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-° ratio [3,2 -c]Pyridine-2-carbamamine 0.013 0.003 N-({4-[(2-Phenylbenzene)sulfonyl]phenyl}indenyl)-1Η-«比咯和[3,2-c] Nfc bite 2-indanamine 0.006 0.117 N-({4-[(2-ethoxyphenyl) hydrazino]phenyl}methyl)-lH-&quot;tb-[3,2-c] Pyridin-2-decylamine 0.011 0.002 N-({4-[(2-ethoxyphenyl) hydrazino]phenyl}fluorenyl) thieno[2,3-decene-diamine 0.002 0.0008 N-({4-[(2-Ethylbenzene)sulfonyl)phenyl}indenyl)-1Η·»Biloxa[3,2-c]nfc pyridine-2-indoleamine 0.005 0.003 N-({4-[(2-ethylbenzene) hydrazino] phenyl]methyl)thieno[He]pyridine-2-carbamamine 0.005 0.0029 N-({4-[(2-fluoro) -3-decyloxybenzene)sulfonyl]phenyl}methyl)-1Η-π-pyrrolo[3,2-c]pyridine-2-carboxamide 0.010 0.007 N-«4-[(2-fluoro -4-methylbenzene)sulfonyl 1phenyl}methyl)-1Η-indolo[3,2-c]pyridin-2-decylamine 0.011 0.021 158436.doc •443 - 201215609 N-({ 4-[(2-Fluoro-4-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]nfc pyridine-2-cartoamine 0.008 207 0.0207 N-({4-[ (2-fluoro -5-methylbenzene)sulfonyl 1 phenyl}methyl)-lH-nb-[3,2-c]pyridine-2-carboxamide 0.025 0.024 N-({4-[(2-曱) Alkylsulfonylaminophenyl)sulfonyl]phenyl}methyl)-1Η-»Bisto[3,2-c]pyridin-2-carboxamide 0.284 &gt;1 N-({4-[ (2-Methoxy-5-methylphenyl)sulfonyl-1phenyl}methyl)-1H-&quot;Bilodo[3,2-c]pyridine-2-carboxamide 0.012 0.003 N-( {4-[(2-Methoxy-5-methylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-cartoamine 0.006 0.0025 N-({ 4-[(2-methoxyphenyl)indolyl-1phenyl}indolyl)-111-indolo[3,2-c]pyridin-2-carboxamide 0.009 0.007 N-({4-[ (2-methoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-decene-2-carbamoamine 0.007 0.0053 N-({4-[(2-methylbenzene)) Sulfhydryl]phenyl}methyl)-1Η-&quot;Biabut[3,2-c]&quot;bipyridin-2-carbamide 0.014 0.013 N-({4-[(2-methylbenzene) Continuation of fluorenyl]phenyl}methyl)thieno[2,3-c]pyridyl-2-carbamide 0.010 0.0222 N-({4-[(2-phenoxyphenyl)sulfonyl]benzene曱 曱 ) Η & & & 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 [ [ [ [ }]methyl)thieno[2 , 3- ten bite - 2-formylamine 0.011 0.0697 N-({4-[(2-phenylethyl)) phenyl]phenyl} fluorenyl)-1Η-&quot;比比和[3, 2-c] Pyridin-2-carboxamide 0.011 0.022 N-({4-[(3,4-Difluorobenzene))]phenyl}methyl)-1Η-pyrrolo[3,2-c Pyridine-2-carboxamide 0.013 0.014 N-({4-[(3,4-difluorobenzene) contigyl 1 phenyl}methyl) thieno[2,3-c]pyridine-2-yl Hydrazine 0.009 0.0081 N-({4-[(3,4-Dimethoxybenzene))]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyran-2-yl Acrylamine 0.014 0.003 N-({4-[(3,4-Dimethoxybenzene) hydrazino]phenyl}methyl)thieno[2,3-c] pyridine-2-carbamide 0.003 0.0009 N-({4-[(3,4-Dimethylbenzene) hydrazino]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 0.006 0.0023 N-({ 4-[(3,5-di-benzene)-indenyl-1phenyl}methyl)thieno[2,3-c]pyridine-2-carbamide 0.006 0.0007 N-({4-[(3, 5-difluorobenzene) hydrazino]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.011 0.007 N-({4-[(3,5-II) Fluorobenzene) fluorenyl 1 phenyl}methyl) thieno[2,3-decapyridyl 2-carbamide 0.004 0.0027 N-({4-[(3,5-dimethylphenyl)) Phenyl} Methyl)-1Η-pyrrolo[3,2-c] nfcpyridine-2-carboxamide 0.009 0.002 N-({4-[(3,5-dimethylphenyl))]phenyl}A Thio[2,3-c]nt-2-carboxamide 0.005 0.0018 158436.doc -444- 201215609

N-({4-[(3-Ethylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-decylamine 0.012 0.006 Ν·({ 4-[(3-Ethylphenyl) hydrazino]phenyl}methyl)thienop,3-c]pyridine-2-nonanamine 0.004 0.0026 N-({4-[(3-Benzene) Sulfhydryl]phenyl}indenyl)-lH-nt-[3,2-(:]-bite- 2-bristamine 0.005 0.003 N-({4-[(3-gasbenzene)) Base]phenyl}methyl)thieno[2,3-c]&quot;biter-2-carbamide 0.005 0.003 N-({4-[(3-ethylphenyl)sulfonyl]phenyl} Methyl)thieno[2,3-c]»ibbit-2-cartoamine 0.006 0.0027 N-({4-[(3-fluoro-4-methoxybenzene) hydrazino]phenyl}A Base)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine 0.005 0.004 N-({4-[(3-fluoro-4-decyloxybenzene)sulfonyl]phenyl}A Thio[2,3-c]pyridine-2-carboxamide 0.005 0.0025 N-({4-[(3-fluoro-4-methylphenyl)sulfonyl]phenyl}methyl)-1Η - fluorenyl [3,2-c]pyridin-2-decylamine 0.008 0.006 N-«4-[(3-fluoro-4-indolylbenzene)sulfonyl-1phenyl}methyl)thiophene [ 2,3-cl nt pyridine-2-cartoamine 0.003 0.0028 N-({4-[(3-fluorophenyl)sulfonyl]phenyl}methyl][3,2-c]唆唆-2 - guanamine 0.009 0.01 N-({4-[(3-fluorophenyl)sulfonyl]phenyl}indenyl)thieno[2,3-c]»*pyridine-2-cartoamine 0.003 0.0033 N-({4-[ (3-methoxyphenyl)sulfonyl]pyridyl}methyl)-1H-&quot;bibromo[3,2-cl pyridin-2-carboxamide 0.007 0.004 N-({4-[(3) -Methoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]bite- 2-decylamine 0.005 0.0026 N-({4-[(3-methylphenyl)sulfonate Styrene]Phenyl}methyl)-1Η-&quot;比比和[3,2-c]》tb pyridine-2-carboxamide 0.009 0.004 N-({4-[(3-mercaptobenzene)) Mercapto]phenyl}indenyl)thieno[2,3-c]pyridine-2-carbamimidin 0.004 0.0023 N-({4-[(4,5-difluoro-2-indolyl)sulfonate) Indenyl]phenyl}indolyl)-lH-nb-[3,2-c]pyridyl-2-carboxamide 0.014 0.006 N-({4-[(4,5-difluoro-2-) Oxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-indole 0.005 0.0029 N-({4-[(4-ethylhydrazino)) continued Phenyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine 0.007 0.003 N-({4-[(4-Ethylphenyl)sulfonyl]phenyl }methyl)thieno[2,3-c]&quot;比唆- 2-decylamine 0.004 0.0025 N-«4-[(4-chloro-2-methoxybenzene)sulfonyl]phenyl}曱基)-1Η-»Λ And [3,2-c]pyridin-2-decylamine 0.022 0.003 N-({4-[(4-Ga-2-yloxybenzene)sulfonyl]phenyl}methyl)thiophene [ 2,3-c] Pyridin-2-carboxamide 0.010 0.0038 N-({4-[(4-Chloro-2-indolyl)sulfonyl]phenyl}indenyl)-1Η-〇比咯[3,2-c]pyridine-2-indoleamine 0.027 0.025 158436.doc 445· 201215609 N-({4-[(4-gas-3-fluorobenzene)sulfonyl]phenyl}methyl)- 1Η-&quot;比比和[3,2-c]pyridine-2-carbamide0.008 0.013 N-({4-[(4-gas-3_fluorobenzene)sulfonyl]phenyl}methyl) Thieno[2,3-c] pyridine 2-mercaptoamine 0.003 0.0071 N-({4-[(4-Phenylbenzene)sulfonyl 1phenyl}methyl)-1Η-pyrrolo[3, 2-c]pyridine-2-formamide 0.009 0.025 N-({4-[(4-ethylbenzene) contigyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine -2-carboxamide 0.08 0.012 N-({4-[(4-ethylbenzene) contigyl)phenyl}methyl)thieno[2,3-c]pyridine-2-decylamine 0.006 0.0078 N-({4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-indole-[3,2-c]pyridin-2-carboxamidine Amine 0.031 0.007 N-({4-[(4-Fluoro-2-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide 0.009 0.0065 Ν·({ 4-[(4-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-ylamine 0.019 0.027 N-({4 -[(4-fluoro-3-methylphenyl)sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.009 0.007 N-({4- [(4-Fluoro-3-methylphenyl)sulfonyl]phenyl}indenyl]thieno[2,3-c]pyridin-2-decylamine 0.007 0.0029 N-«4-[(4-Fluorine Benzene sulfonyl]phenyl}methyl)-1Η-»Biloxi[3,2-c]〇tb bite 2-formylamine 0.038 0.008 N-({4-[(4-fluorobenzene)) Sulfhydryl]phenyl}methyl)imidazo[l,2-a]acridin-6-decylamine 0.023 0.011 N-({4-[(4-fluorophenyl)sulfonyl]phenyl}A Thio[2,3-c]»pyridin-2-carbamamine 0.003 0.010 N-({4-[(4-methylpyreneto)benzenesulfonyl]phenyl}methyl)- 1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0.024 0.012 N-({4-[(4-methoxy-2-methylphenyl)sulfonyl]phenyl}methyl )-1Η-&quot;比比和[3,2-c] pyridine 2-carbamoamine 0.024 0.024 N-({4-[(4-methoxy-3-mercaptophenyl)sulfonyl] Phenyl}methyl)-1Η-&quot;Bedo[3,2-c]pyridin-2-carboxamide 0.01 0.002 N-({4-[(4-methoxy-3-mercaptobenzene) Sulfhydryl]phenyl}methyl)thieno[2, 3-c] pyridine bit-2-carbamide 0.003 0.0024 N-({4-[(4-methoxyphenyl) benzyl]phenyl}methyl)-lH-nb-[3,2- c] pyridine-2-carbamide 0.011 0.009 N-({4-[(4-methoxybenzene) hydrazinyl]phenyl}methyl)« pheno[2,3-c]-ratio 2 - decylamine 0.005 0.0027 N-({4-[(4-methylphenyl) hydrazino]phenyl}methyl piroxi[3,2-c]nb pyridine-2-carboxamide 0.006 0.009 N -({4-[(4-methylphenyl) aryl]Iphenyl}methyl)&gt;« pheno[2,3-clnt bite-2- decylamine 0.005 0.0050 N-({4-[ (5-Ethyl-2-phenyloxybenzene)sulfonyl 1phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide 0.02 0.006 158436.doc -446 - 201215609

N-({4-[(5-Gas-2-methoxybenzene)sulfonyl]phenyl}methyl)-lH-nb-[3,2-c]pyridin-2-amine 0.006 0.002 N-({4-[(5-Chloro-2-indolyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-cartoamine 0.004 0.0013 N_ ({4-[(5-Fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)-1Η-&quot;Birdo[3,2-c]pyridin-2-decylamine 0.005 0.003 N-({4-[(5-fluoro-2-indolylbenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridin-2-ylamine 0.011 0.007 N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]&quot;bipyridyl-2-carbamide 0.003 0.0094 N-({4-[(5-Tertibutyl-2-methoxybenzene) fluorenyl]phenyl}indolyl)-1H-pyrrolo[3,2-c]pyridin-2-曱Indoleamine 0.647 0.006 N-({4-[(5-Tert-butyl-2-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2- Methionamine 0.015 0.0046 Ν-(4-(2·(Tris(1)methoxy)phenyl) decyl) oxazolo[l,2-a] 〇bite- 6-decylamine 0.008 N -(4-(phenylphenyl)benzyl)-1Η-imidazo[4,5-b]pyridine-6-decylamine 5.780 &gt; 10 N-(4-(phenylhistyl)benzyl Benzo[d]thiazole-5-carboxamide 0.047 3.872 N-[(4-{[2-(Hydroxy)benzene]sulfonyl}phenyl)methyl]-lH-nb-[3,2-c]pyridine-2-carboxamide 0.018 0.033 N-[(4-{[2-(dimethylaminocarbamimidino)benzene]sulfonyl}phenyl)indolyl-1-1H-pyrrolo[3,2-c]pyridin-2-曱Indoleamine 0.951 0.484 N-[(4-{[2-(methylaminesulfonyl)benzene]sulfonyl}phenyl)indolyl]-1Η-»pyrolo[3,2-c]pyridine 2-carbamamine 0.076 0.202 Ν-[(4-{ρ-(N-methyl-4-phenyl)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c 】Pyridine 2-carbamamine 0.034 0.006 N-[(4-{[2-(N-Phen-4-ylindenyl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3- c] pyridine-2-pyramine 0.013 0.0036 N-[(4-{[2-(trifluoromethoxy)benzene 1 sulfonyl}phenyl)methyl]-1Η-»比咯和[3 ,2-c]pyridin-2-decylamine 0.016 0.003 N-[(4-{[2-(trifluorodecyloxy)benzene]sulfonyl}phenyl)methyl] 叹 并 [2,3 -c] pyridine-2-carbamide 0.004 0.0028 N-[(4-{[2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-lH-nfc[3,2 -c] pyridine-2-pyramine 0.022 0.025 N-[(4-{[2-(trifluoromethyl)benzene] sulfonyl}phenyl)methyl 1 嗔 并 [2,3-c ]nb pyridine-2-carbamide 0.013 0.0260 N-[(4-{[2-Fluoro-4-(1Η-pyrrol-1-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyroline-2 -carbamamine 0.006 0.0080 N-[(4_{[2-methoxy-4-(lH-ntoxazol-1-yl)benzene Isulfonyl}phenyl)methyl]-1H-pyrrolo[3 ,2-c]pyrazole-2-meramine 0.016 0.002 N-[(4-{[2-methoxy-4-(1Η-pyrazol-1-yl)benzene]sulfonyl}phenyl) Methyl] thieno-P,3-c]pyridine-2-carboxamide 0.005 0.0026 N-[(4-{[2-methoxy-4-(trifluoromethyl)benzene]sulfonyl}phenyl )methyl]-1H-pyrrolo[3,2-c]pyridin-2-indoleamine 0.022 0.005 158436.doc -447- 201215609 N-[(4-{[2-methoxy-4-() Trifluoromethyl)phenyl]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-carboxamide 0.009 0.0075 N-[(4-{[2-methoxy- 5-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]-indole-indolo[3,2-c]pyridin-2-decylamine 0.061 0.012 N-[(4-{ [2-methoxy-5-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]nbpyridine-2-carboxamide 0.009 0.0062 N-[ (4-{[2-decyloxy-6-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2- Formamide 0.036 0.022 N-[(4-{[2-A 4-(1Η-〇- oxazol-1_yl)benzene]sulfonyl}phenyl)indenyl]-1H-pyrrolo[3,2-c]pyridin-2-decylamine 0.004 0.004 N- [(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]-1H-&quot;bido[3,2-c]pyridine-2-carbamide 0.006 0.004 N-[(4-{[3-(Proton-2-yl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]&quot;bipyridyl-2-carbamide 0.0026 N-[(4-{[3-(Trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]-1H·-pyrho[3,2-c]pyran-2-yl Indoleamine 0.005 0.003 N-[(4-{[3-(Trifluoromethoxy)benzene]sulfonyl}phenyl)indenyl]indeno[2,3-c]pyridine-2-cartoamine 0.002 0.0024 N-[(4-{[3-(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-"pyrho[3,2-c]pyridin-2-A Hydrazine 0.009 0.003 N-[(4-{[3-(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-decabiidine-2-carboxamide 0.003 0.0010 N-[(4-{[3-Fluoro-4-(1Η-»oxazol-1-yl)benzene Isulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridyl 2-mercaptoamine 0.011 0.004 N-[(4-{[4-(dimethylaminocarbamimidyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2- c]pyridine-2-carbamide 0.027 0.014 N-[(4-{[4- (propan-2-yl)phenyl]sulfonyl}phenyl)indenyl]thieno[2,3-c]&quot;bipyridyl-2-carbamide 0.006 0.0071 N-[(4-{[4- (Trifluoromethyl) phenyl]sulfonyl}phenyl)methyl I-1H-indolo[3,2-c]pyridine-2-carboxamide 0.024 0.026 N-[(4-{[4- Gas-3-(trifluoromethyl)benzene Isulfonyl}phenyl)methyl I-lH-nb-[3,2-c]pyridin-2-carboxamide 0.008 0.005 N-[(4 -{[4- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide 0.010 0.0034 N-[4- (Benzenesulfonyl)phenyl 1pyridine-3-carboxamide 12.038 &gt;30 N-{[3-(Benzene)phenyl]methyl}-1Η-pyrrolo[3,2-c] Pyridine-2-carbamamine &gt;30 &gt;30 Ν-{[4-(1Η-吲哚-7-continuene)phenyl]fluorenyl}thieno[2,3-c]pyridine-2- Methionamine 0.003 0.0027 Ν-{[4-(1-methyl-1H"pyrazole-4-thenyl)phenyl]methyl}-1Η-吼-[3,2-c]-bito- 2-Proline Amine 0.048 0.123 N-{[4-(2,3-Dihydro-1,4-benzodioxan-6-thenyl)phenyl]methyl}thiophene[2 ,3-c]pyridine-2-carboxamide 0.004 0.0027 Ν-{[4-(2Η-1,3-benzodioxol-5-continuenyl)phenyl]fluorenyl 1H- Pyrrolo[3,2-c] Amides A-2 0.008 0.007 158436.doc -448- 201215609

Ν-{[4-(2Η-1,3·benzodioxol-5 5 fluorenyl)phenyl]methyl}thieno[2,3-c]bit-2-carboxamide 0.003 0.0025 rN-U-p- f-based per phenyl group] phenyl] methyl b 1H_nfc 洛和[3,2_cj -=~-_^^-2-nonylamine 0.007 0.013 ΓΗ14-Ρ-f-thiophene -2-sulfonyl)phenyl]methyl}thiophene[23_c]pyridyl-one:~~zhi}carbamamine 0.005 0.0077 N-U4-(stuptent base) base] methyl}.[ 1,2,3,4]tetrazolo[wa]-*biting_6_carbamamine 0.447 &gt;30 N-U4·(benzoic acid)phenyl]f Leqizhen three spit and ^bit Each of the brewing amines 0.301 &gt;10 -" 414 · (phenyl phenyl) phenyl] methyl} _1, 5 · peak bite _2 · methotrexate 0.875 &gt; 10 M-U4- (benzene sulfonyl) Stupid base] methyl HH-imidazo[4,5-c]0*bit_2--_____? decylamine 7.062 5.37 JN-U4-(phenylindenyl)phenyl]f-based 1H-pyrazole [3, 4 clocks than each of the A- ____ decylamine 1.271 &gt; 10 JN-U4- (stupid group) phenyl 1 methyl}_1H-pyrazolo[3,4-b]0 ratio bite - 5-M-decylamine 0.070 0.051 ΓΝ-U4-(Benzene)phenyl] sulfhydryl m_pyrroloindole 2,3_b]pyridine_5_decylamine 1.906 &gt;30 N-{[4- (phenyl) phenyl] fluorenyl }_1H_pyrrolo[2,3_c]pyrazine j-carbamamine&gt;10 &gt;10 N-{[4_(phenyl-phenyl)phenyl]methyl-i-yl-yl-pyrazole[3] , 4_b] pyridine «·methanamine 1.725 &gt; 30 stupid carbonyl) phenyl J &gt; f-based} small methyl-1H_pyrrolo[3,2-c]pyridine-2-carboxamide &gt; 10 &gt;30 N-U4·(Benzene fluorenyl)phenyl]fluorenyl}-3-(pyridyl-2-yl)-1Η-pyrazole-5-decylamine 7.429 23.371 JN-{[4_( Phenylsulfonate)Phenyl]V-based}_3·(pyridine·3_yl)_1,2-oxazole-5-cartoamine 0.033 &gt;30 phenyl wall fluorenyl)phenyl j 肀}}_3_(吼Bite _4 base) Η Η 吡 吡 吡 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 3.1 Methionamine 0.306 7.390 N-U4-(stupidyl) base j T-based}-5-(pyridin-3-yl)-1,2,4-oxadiazole-3-carbamimid 0.312 &gt; 30 continuation base) base j T base}-5-(»*bit-3-yl)-1Η-° than 嗤-3-cartoamine 0.023 11.825 phenyl wall ) base) stupid base T base} imidazo丨Ha]pyridin-2_metholamine benzoquinone)phenyl-1-methyl}imidazolium, 2_a丨"bite_6_carbamamine 1.491 0.021 &gt;30 _ 0 〇11 Ν-{[4 ·(Benzene base) Stupid base]Methyl}isoquine _6 _Metamine Ν-{[4_(Benzyl yl) phenyl hydrazine methyl}isoquine _7_carbamamine 16.082 0.219 ν·υχι 21.303 2d ωπω M-U4-(benzene scouring) Stupid 1 methyl} quinazoline _6_carbamamine oxime-{[4_(phenylindolyl)phenyl]fluorenyl}thienofluorene bl〇lfc^_6-carbamamine 16.082 0.052 a*t*UUU 21.303 ~~ N-U4-(Stupid wall base) Stupid base]f base} 嗟 丨 丨 2.3-cl pyridine 2-carbamoamine 0.011 0.012 138436.doc •449· 201215609 N-{[4-( Quinolin-4-continuation base) phenyl]methyl} porphin p,3-c]nb bite-2-decylamine 0.003 0.0007 N-{[4-(naphthalene-1-ylindolyl)benzene Methyl}thieno[2,3-c]pyridin-2-ylamine 0.002 0.0005 N-{[4-(Pantothin-4-yl)phenyl]methylpyrrole [3,2-c]heptin-2-carbamide 0.005 0.0009 N-{[4-(Phenylthio-4-indolyl)phenyl]methyl}thieno[2,3-c]pyridine -2-carbamamine 0.004 0.0017 N-{[4-(phenylmethyl)sulfonylphenyl]methyl}-1Η-&quot;比比和[3,2-c]&quot;比啶_2 _Metformamide 0.029 0.3015 1^-{[4 比 咬 -3- 醢 ) ) ) 苯基 苯基 } } } } 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 0.048 N-{[4-(quino-3-indolyl)benzene Thio[], thieno[2,3-c]pyridin-2-carboxamide 0.003 0.0008 N-{[4-(quino-6-anthracenyl)phenyl]fluorenyl}thieno[2, 3-c]pyridine-2-carbamide 0.003 0.0009 N-{[4-(quinoline-8-thenyl)phenyl]fluorenyl}thieno[2,3-c]&lt;·biting- 2-carbamamine 0.006 0.0025 N-{2-[4-(phenylindolyl)phenyl]ethyl}-1Η-la-l-[3,2-c]&quot; 0.410 9.1 Ν-({4-[(1Η-carbazol-6-yl)amine sulfonyl]phenyl}fluorenyl)-1Η-° ratio 咯[3,2-c] pyridine bit-2- Amine amine 0.135 5.44 Ν-({4-[(1-Sideoxy-1H-isodecen-5-yl)amine sulfonyl]phenyl}methyl)-1H-pyrrolo[3,2-c Pyridine-2-indole amine 0.008 < 2.27 N-({4-[(2,3-dihydro-1,4-benzodioxan-6-yl)aminesulfonyl]phenyl} Methyl)-1Η-pyrrolo[3,2-c]pyridin-2-carboxamide&gt;10 &gt;10 Ν-({4-[(2·ethoxyphenyl)amine sulfonyl] Phenyl}fluorenyl)-1Η-»Biraxo[3,2-c]pyridyl-2-meramine 0.005 0.005 N-({4-[(2-methoxy-6-nonylphenyl) Aminesulfonyl]phenyl}methyl)-1Η-indolo[3,2-c]pyrodo-2-cartoamine 0.006 12.4 N-({4-[(2-methoxyphenyl) Aminesulfonyl]phenyl}indenyl)-lH-o [3,2-c]pyridine-2-carboxamide 0.089 2.150 N-({4-[(2-phenoxyphenyl)aminesulfonyl]phenyl}indolyl)-lH-nb And [3,2-c]pyridine-2-carboxamide 4.019 12.000 N-({4-[(2-propoxyphenyl)aminesulfonyl]phenyl}indolyl)-1Η-tata [3,2-c]pyridine-2-meramine 0.052 0.100 N-({4-[(3-methoxy-2-mercaptophenyl)amine sulfonyl]phenyl}methyl)- 1Η-»比比和[3,2-c]pyrazole-2-carboxamide 0.030 0.006 N-({4-[(4-Ga-2-methoxy-5-methylphenyl)amine sulfonate Mercapto]phenyl}methyl)-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 7.835 18.322 N-({4-[(4-ethoxy-2-fluorophenyl)) Aminesulfonyl]phenyl}methyl)-1Η-"pyrolo[3,2-c]pyridyl-2-carbamide 0.154 1.600 Ν-({4-[(4-fluoro-2-) Oxyphenyl)aminesulfonyl]phenyl}methyl)-1Η-"pyrolo[3,2-c]pyridin-2-carboxamide 3.38 &gt;30 -450- 158436.doc 201215609

N-({4-[(4-decyloxy-2-methylphenyl)amine sulfonyl]phenyl}methyl)-1Η-»pyrolo[3,2-c]pyridin-2 -carbamamine 1.451 &gt;30 N-({4-[(5,6,7,8-tetrahydronaphthalen-1-yl)amine sulfonyl]phenyl}methyl)-1Η-&quot; And [3,2-c]pyridin-2-carboxamide&gt;30 &gt;30 Ν-({4-[(5·气-2-曱oxyphenyl)amine sulfonyl]phenyl} Methyl)-1Η-&quot;比比和[3,2-c]》tb-bit-2-carboxamide 0.197 17.984 N-({4-[(5-fluoro_2_decyloxyphenyl)amine Sulfhydryl]phenyl}methyl)-1Η-&quot;Bisto[3,2-c]pyridin-2-decylamine 0.232 &gt;30 N-({4-[(5-methoxy) -2-methylphenyl)amine sulfonyl]phenyl}methyl)-1Η-indolepyrrolo[3,2-c]"tt bit-2-meramine 0.051 13.018 N-({4- [(Quinoline-8-yl)amine sulfonyl]phenyl}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0.075 1.478 N-[(4-{[2 -(2-hydroxyethoxy)phenyl]aminosulfonyl}phenyl)indenyl]-lH-pyrrolo[3,2-c]pyridine-2-carboxamide 19.611 23.854 N-[(4- {[2-(Hydroxymethyl)phenyl]amine sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.030 0.006 N-[(4 -{[2-(morpholin-4-yl)phenyl]aminesulfonyl} Methyl]_1H-pyrrolo[3,2-c]pyridin-2-carboxamide 0.019 0.017 N-[(4_{[2-(娘丁-1-yl)phenyl]aminesulfonyl) }phenyl)methyl]-1H-'pyrolo[3,2-c]pyrodo-2-cartoamine 0.072 0.008 N-[(4-{p-(prop-2-yloxy)benzene Aminosulfonyl}phenyl)indenyl]-1H-lalocodo[3,2-c]» than bite-2-carbamide 0.003 0.001 N-[(4-{[2-(trifluoro)曱oxy)phenyl]sulfonylamino}phenyl)indolyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.003 0.001 N-[(4-{[2-(three Fluoromethoxy)phenyl]aminosulfonyl}phenyl)indenyl]-1H-&quot;bibromo[3,2-c]pyridin-2-carboxamide 0.006 0.001 N-[(4- {[2-Methoxy-5-(trifluoromethyl)phenyl]amine sulfonyl}phenyl)indenyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.0005 0.0016 N-[(4-{[4-Gas-2-(trifluoromethoxy)phenyl]aminesulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine 2-carbamamine 0.002 0.002 N-[(4-{8-oxa-3-azabicyclo[3.2.1]octyl-3-phenyl]phenyl)indolyl]-1H-pyrrole [3,2-c]pyridine-2-carboxamide 0.08 0.003 Ν-[(4-{8·oxa-3-azabicyclo[3.2.1] Xinxun-3-continuation)}phenyl) Methyl] imidazo[l,2- a] pyridyl-6-decylamine 0.004 0.003 N-[(4-{8-oxa-3-azabicyclo[3.2.1]octyl-3-phenylindol}phenyl)methyl]thiophene And [2,3-c]pyridine-2-carboxamide 0.015 0.003 N-[(4-Benzylguanidinophenyl)indolyl]-1H-pyrrolo[3,2-c]pyridine-2- Methionamine 0.019 0.004 N-[(4-Benzene decylamino)indolyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide 0.011 0.005 N-[4-(piperider Pyridin-1-sulfonyl)phenyl]-1H-»*-[3,2-c]&quot;bipyridin-2-cartoamine0.008 0.006 N-[4-(bit bite-1-continued Base) phenyl]-2·(° bite_3·yloxy)ethinamide 0.0011 0.0066 Ν-[4-(piperidin-1-sulfonyl)phenyl]-3-(pyridine-3- Acetylamine 0.003 0.007 158436.doc -451 · 201215609 phenyl fluorenyl) piperidine-4-yl]methyl}-lH-nb-[3,2-c]»pyridin-2-carboxamidine Amine 0.015 0.009 N-{[4-(piperidin-1-indolyl)phenyl]methyl}-[1,2,3,4]tetrazolo[l,5-a] -carbamamine 0.003 0.009 N-{[4-(piperidin-1-ylindolyl)phenyl]methyl 1,3-benzothiazol-6-nonylamine 0.009 0.010 N-{[4-( Acridine-1-n-decyl)phenyl]methyl}-1,6-acridin-2-carboxamide 0.012 0.010 N-{[4-(piperidone-1-ylindole) Phenyl]methyl}-1Η-1,3-benzobisazole-5-cartoamine 0.021 0.010 N-{[4-(piperidin-1-indolyl)phenyl]methyl}-1Η -imidazo[l,2-b]»biazole-5-decylamine 0.0008 0.0110 N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}-1Η-carbazole-5 -Procarbamide 0.018 0.016 N-{[4-(Piperidine-1-dedecyl)phenyl]methyl}-1Η-pyrazolo[3,4-b]pyridine-5-carbamimidamine 0.017 0.033 N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}-1Η-&quot;比比和[2,3-c]&quot;bipyridyl 2-carbamide 0.004 0.054 N -{[4-(piperidin-1-sulfonyl)phenyl]methyl}-1Η-lado[3,2-c]nb-pyridine-2-carbamide 0.003 0.200 N-{[4- (piperidone-1-sulfonyl)phenyl]methyl}furo[3,2-c]pyridin-2-carboxamide 0.017 0.286 N-{[4-(piperidin-1-sulfonyl) Phenyl Imethyl}imidazo[l,2-a]-pyridin-6-carboxamide 0.018 1.160 N-{[4-(Big bit-1-yl)phenyl]methyl}imidazole And [l,2-a]pyridine-7-anthraquinone &gt;0.1 &gt;0.5 N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}&quot;bipyridine-3- Indoleamine 0.039 0.64 N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}thieno[2,3-b]pyridin-2-carboxamide 6.146 14.000 N-{[ 4- (Pipeline-1-n-decyl)phenyl]methyl}thienoindole 3,2-c]pyridin-2-indoleamine 0.886 10 Ν-{1-[4-(piperidin-1-sulfonate) Phenyl]ethylpyrolo[3,2-cp-pyridyl-2-carboxamide 0.020 0.007 assay example 3 in vitro cell proliferation assay U25 1 cells with and without added beta-nicotine Single nucleotide (ΝΜΝ) or nicotinamide (ΝΑΜ) in 180 pL medium (10% FBS, 1% penicillin/streptomycin amphotericin B, RPMI-1640) in 1.25X 103 cells per well Density was inoculated into 96-well plates. After overnight incubation at 37 ° C and 5% CO 2 , compound titration was carried out in another dilution dish by serial dilution of the compound in DMSO to make a hydrazine stock solution. The 158436.doc • 452-201215609 compound is then further diluted to a final concentration in the medium, followed by 20 μL of each dilution to the inoculated cells containing the control (eg DMSO and blank) to finalize The volume is 200 μί. The final DMSO concentration in each well was 0.1%. The plates were then incubated for 72 hours at 37t in a 5% CO2 incubator. The number of viable cells was then assessed using the sulfonium rhodamine B (SRB) assay. The cells were fixed at 4 °C for 1 hour by adding 50 pL of 30% trichloroacetic acid (TCA) to give a final concentration of 6% TCA. The plate was washed four times with H20 and allowed to dry for at least 1 hour, after which 100 pL of a 4% SRB in 1% acetic acid solution was added to each well and incubated at room temperature for at least 30 minutes. The plate was then washed three times with 1% acetic acid, dried, and treated with 100 pL of 10 mM Tris-test solution. The disk was then read at 570 nm absorbance using a micro-quantity disc reader. A background is created on another tray containing only medium. The disc is set to suppress °/. Method First, the signals from the background disk are averaged, and then the background is subtracted from the test disk. The % inhibition of the compound-treated cells was then determined by using the following formula: Inhibition % = 100-100xx/y where X represents the average signal of the compound treated cells and y represents the average signal of the DMSO treated cells. The formula used to determine the ICsq value: IC50 = 1〇a(LOG10(X)+(((50-% inhibition at compound concentration 1) / (XXYY)x(LOG10(X)-LOG10(Y)))) Wherein X represents the compound concentration 1, Y represents the compound concentration 2, XX represents the % inhibition at the compound concentration 1 (X), and YY represents the % inhibition at the compound concentration 2 (Y) 158436.doc - 453 - 201215609. The U251 values for some compounds are shown in Table 4. Chemical name U251 ΙΟ50(μΜ) N-{[4-(Benzene fluorenyl)phenyl]fluorenyl}thieno[3,2-b]. Indoleamine &gt;2 N-{[4-(phenylsulfonyl)phenyl]methyl}imidazo[l,5-a]acridin-6-nonylamine &gt; 2 N-{[4- (Benzene fluorenyl)phenyl]fluorenyl}-1Η-° ratio [3,2-dibenzyl-2-carbamide 0.040 N-{[5-(phenyl)pyridin-2- Methyl}-1Η-pyrrolo[3,2-c]pyridin-2-indoleamine 0.035 N-{[4-(phenylsulfonyl)phenyl]indolyl}imidazo[l,2- a]»Bitazin-6-nonylamine&gt;2 N-{[4-(benzothenyl)phenyl]fluorenyl}furo[3,2-7]«pyridin-2-carboxamide 0.545 N-{[6-(phenylsulfonyl)pyridin-3-yl]indolyl}-1Η-pyrrolo[3,2-c]pyridine-2-carboxamide&gt;2 N-{[4-( Piperazine-1-sulfonyl)phenyl]fluorenyl} Benzo[2,3-c].pyridin-2-decylamine 0.405 N-{[4-(piperazin-1-sulfonyl)phenyl]indolyl}imidazo[l,2-a] »Bistidine-6-decylamine 0.556 N-{[4-(3-Aminopyrrolidin-1-sulfonyl)phenyl]indolyl}thieno[2,3-c]pyridine-2-yl Indole hydrochloride 0.31 N-{[4-(3-Aminopyrrolidin-1-sulfonyl)phenyl]methyl}furo[2,3-c]pyridine-2-carboxamide hydrochloride Salt 1.85 N-({4-[(3,5-difluorobenzene)sulfinylidene]phenyl}indolyl) oxazolo[l,2-a]»pyridin-6-nonylamine 0.0066 heterogeneous Transplantation study: 5χ106 Α2780 cells (NCI) were injected subcutaneously into the left side of the mouse (female). After 10-12 days, when the tumor size reached 100-200 mm3, the mice were randomly divided into 8 groups of mice. In the group (including the vehicle control group) and the reference standard group, the compound was formulated in 60:30:10 PEG-400:D5W:ethanol and administered orally in a dose volume of 10 ml/kg (twice daily). The duration was 5 or 10 days. The dose used for efficacy was selected according to the MTD (Maximum Tolerated Dose) study. Mice were weighed and tumors were measured every other day using a vernier caliper. The tumor volume was calculated according to the formula (length X width 2)/2. All animal operations are conducted through the institutional animal management and use committee of the Singapore Bioresources Center (Institutional Animal)

Care and Use Committee of Biological Resource Centre, -454- 158436.doc 201215609

Singapore) approved. The compound N-[(4-{[2-(difluoromethoxy)phenyl]amine] is phenylphenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamidine Amine produces tumor stagnation. The following compounds produced tumor regression: N-{[4-(phenylsulfonyl)phenyl]methyl}imidazo.比6_4-carbamamine; N-{[4-(phenylsulfonyl)phenyl]methyl}thieno[2,3_c] π-pyridyl-2-ylan; ® Ν4[4-( Phenylsulfonyl)phenyl]mercapto}-1Η-°pyrho[3,2-c]»bipyridine-2-carboxamide&gt; 1-({4-[(4-fluorophenyl)sulfonate Mercapto]phenyl}indenyl)_111_(1 pyrrolo[3,2_(:]11-pyridyl-2-nonylamine; N-({4-[(4-fluorophenyl)sulfonyl)benzene) Methyl imidazo[ihp-pyridyl-6-amine; N-({4-[(4-ethylmercaptophenyl)sulfonyl]phenyl}methyl)_1Η_β ratio [3,2 c] pyridine-2-carbamamine; ® N-[(4-{[2-(trifluoromethoxy)benzene] hydrazino}phenyl)methyl]- 嘻[3,2-c Pyridin-2-indoleamine; Ν-({4·[(3-phenylene)sulfonyl]phenyl}indenyl)_1Η_Π比比和[3,2_c]a than pyridine-2-nonylamine The following compounds delay tumor growth: N-{[4-(pyridine-3-sulfonyl)phenyl]methylpyrrolidinopyridinium-2-amine; N-[(4-{[2- Oxy-4-(1Η-»Bizozol-1·yl)benzene]sulfonyl}phenyl)indenyl]_158436.doc -455· 201215609 1H-pyrrolo[3,2-c]pyridine-2 - guanamine. Although the invention has been described in connection with the specific embodiments described above, the general practitioner Knowing apparent that many alternatives, modifications and other variations. All such alternatives, modifications and variations are intended to fall within the spirit and scope of the present invention.

158436.doc • 456·

Claims (1)

201215609 VII. Scope of application: 1 · A compound of formula IIB or a pharmaceutically acceptable salt thereof, Wherein: R is a package 2: 3 or 4 of which are independently selected from the group consisting of heteroatoms, wherein the heteroaryl group may be substituted with - or a plurality of substituents selected from the group consisting of silk and pendant oxy groups. a group of groups i; and wherein the heteroaryl group may comprise - or a plurality of sense oxides formed with members of the N atom of the heteroaryl group; R is -NHR4 and R4 is a cycloalkyl group, a heterocyclic aryl group Or a heteroaryl; a cycloalkyl group; a aryl group; or a heteroaryl group; t: (0) the cycloalkyl group, the aryl group or the heteroaryl group is unsubstituted or 1, 2, 3, 4 or 5 Substituted substituents which may be the same or different and independently selected from the group consisting of: hydrazine, dentate, hydroxy, hydroxyalkyl, cyano, -(CH2)mNRaRb, pendant oxy, alkyl, Cyanoalkyl, haloalkyl, alkoxy, alkoxy, alkoxyalkyl, alkenyl, alkynyl, alkynyloxy, -CONH2, -S-alkyl, -C(0 NH(alkyl), _c(〇)N(alkyl)2, -C(0)NH(cycloalkyl), _c(0)NH(aryl), 158436.doc 201215609 • C(0)N (aryl) 2, arylalkyl-, arylalkoxy-, aryloxy-, polar pit, heterocycloalkyl , aryl, (heterocyclic) alkyl-, (heterocycloalkyl)alkoxy-, -C(O)heterocycloalkyl, heteroaryl, (heteroaryl)alkyl, -S ( 0) 2· Hyun (base, -s(0)2-aryl, -s(o)2-chzf3-z, -c(0)alkyl, -N(R5)-C(0)-alkyl, _n(R5)-C( 0)-aryl, •S(〇2)NH2, -S(〇2)NH(alkyl), -S(〇2)N(alkyl)2, -N(H)(S〇2)( An alkyl group and a fluorenyldioxy group, wherein the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may each have one or more functional groups, a cyano group, an alkyl group or an alkoxy group. And (ii) the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group may each optionally be additionally fused with an independently selected aryl group, heteroaryl group, heterocycloalkyl group or cycloalkyl group. Combining to form a bicyclic or tricyclic group which may be substituted by one or more of a dentate group, a gas group, a hospital group or an alkoxy group; R and R3 may be independently selected from the group consisting of ruthenium and osmium; R5 is oxime, alkyl or arylalkyl, alkyl, alkoxy, alkoxyalkyl Ra and Rb are independently selected from ruthenium and halo. Group of alkyl groups; m is 〇,! , 2, 3, 4, 5 or 6; z is 0, 1 or 2. 2. A compound as claimed, wherein R is selected from the group consisting of 2, 3 or 4 heteroatoms selected from the group consisting of N, S or hydrazine to 9 members of the X-membered 10-membered bicyclic heteroaryl group 158436.doc - 2-201215609 3. The compound of claim 1 or 2, wherein R is selected from the group consisting of: benzothiazole, dihydrogen peak, dihydropyrene ratio bite and bite, dihydroindole 嘻 and D ratio bite, 吱喃 〇 〇 is more than 0, taste saliva and η than 嗓, 咪 sal and ^ ratio. Sit and talk. It is more than a bite, a scent, and a pyridine, oxazole, hydrazine, isoquinoline, acridine, pyrazolopyridine, pyrrole 0 bite, four saliva and η ratio. Ding, tetrahydro σ m saliva and η than bite, tetrahydro β is more than arsenic, thiazolopyridine and thienopyridine. 4_A compound of claim 1 or 2 wherein R is selected from the group consisting of: °[3 4_ b] pyridine; i, 4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine; 7,8-dihydro·5Η-0-pyrido[4,3-d]pyrimidine; , 7-di-pyrido[pyrido[3,4-b]pyridine; 7,8-dihydro-5H-[1,6]acridine; I,4,1,2-tetrahydro-imidazo[4, 5-c]pyridine; 18a-dihydroimidazo[1,2-a]pyridine; thieno[3,2-c]pyridine; 1H•imidazo-H,2-b]pyrazole; 1H-pyrazole [3,4-b]pyridine; furo[23c]pyridine; 1H-. Bisazo[3,4-b]pyridine; 1H-pyrrolo[^^pyridine; °sepeno[2,3-b]e is more than 唆;°米* sits and [l,2-a] squirts ; 吱 并 [23_c] pyridine; isoquinoline; m-carbazole; imidazolium n, 2_a] pyridine; thieno[2'3&lt;] ton bite; bite mer to [2,3-c]n ratio bite ; 1H_n ratio 咯[23c] 〇 pyridine; oxazolo [as small azine, 1,3-benzothiazole; stupid (4) thiazole; 1H-pyrrolo[2,3_b] pyridine; [U] thiazole And [5,4_c]pyridine; [1,2,3,4]tetrazolo[i,5-a]pyridine; 1,5-acridine; 1H_吲哚; imipenone [4,5- c]*» than bite; and 1,6-peak β. 5. The compound of claim 1 or 2, wherein r is substituted at a position adjacent to the nitrogen atom on 盥 y I ν . 158436.doc 1. The compound of claim 1 or 2, wherein R is selected as the group 2, and the following composition of Putian 201215609 7. The compound of claim 1 or 2, wherein RU_NHR4, R4 is cycloalkyl, heterocycloalkyl, aryl or heteroaryl. 8. A compound according to claim 7, wherein r4 is an unsubstituted or substituted ring Alkyl 9. The compound of claim 7, wherein R4 is unsubstituted or cycloalkyl. 10. The compound of claim 7, wherein R4 is unsubstituted or substituted. Substituted substituted aryl 11. The compound of claim 7 wherein 'unsubstituted or aryl. Miscellaneous 12. The compound of claim ^, wherein w is unsubstituted or substituted C3-C1G cycloalkyl. 13 = Compound of claim 1 or 2 wherein W is an unsubstituted or substituted aryl group. A compound according to claim 1 or 2, wherein W is unsubstituted or substituted, including 5, 3 or 4 heteroatoms selected from N, S or oxime, from 5 members to H), monocyclic or bicyclic Aryl. 15. The compound of claim 7, wherein r1*r4 is selected to be free of the following composition: 158436.doc 201215609 Group: 6-decyloxy. Bisidine; 2-ethoxy-4-fluorophenyl; 3,4-difluorophenyl; 3,4-dimethoxyphenyl; 3,4-dimethoxyphenyl; 3-chloro- 5-fluorophenyl; 3- gas-4-methoxyphenyl, 4-chloro-2-methylphenyl, 4-ox-2-oxooxyphenyl; 4-decyloxy-2,5 -didecylphenyl; 4-nonylphenyl; 5-chloro-2-ethoxyphenyl; 5-fluoro-2-indolylphenyl; 1-(3-chlorophenyl)-1 - Η-razole; 1-(4-fluorophenyl)-1Η-pyrazole; 1-(propan-2-yl)-1Η-pyrazole; 1,3-thiazole; 1,4-dimercapto-1H- Imidazole; 1,5-dimercapto-1H-imidazole; 1-benzothiophene; 1H-indole; 1-mercapto-1H-1,3-benzobisazole; 1-methyl-1H-carbazole ; 1-mercapto-1H-indole; 1-mercapto-1H-pyrazole; 1-mercapto-3-(trifluoromethyl)-1Η-pyrazole; 1-indolyl-5-(trifluoro Mercapto)-1Η-pyrazole; 1-propyl-1H-carbazole; 2-(2,2,2-trifluoroethoxy)-4-(trifluoromethyl)phenyl; 2-(3 -fluorophenyl)-1,3-thiazole; 2-(benzyloxy)-5-(trifluoromethyl)phenyl; 2-(dimethylamino)pyrimidine; 2-(dimethylamine A Phenyl)phenyl; 2-(ethoxymethyl)phenyl; 2-(decylaminesulfonyl)phenyl; 2-(morpholin-4-yl)pyridine; 2-(morpholine-4 -base Pyridine; 2-(morpholin-4-ylmethyl)phenyl; 2-(pyrrolidin-1-yl)-1,3-thiazole; 2-(trifluoromethoxy)phenyl; 2-(three Fluoromethoxy)phenyl; 2-(trifluoromethyl)imidazo[1,2-a]acridine; 2-(trifluoromethyl)phenyl; 2-(trifluoromethyl)acridine; 2,3,6-trimethoxyphenyl; 2,3-difluoroj-6-methoxyphenyl, 2,3-diphenyl, 2,3-di-r--1,4-benzene And dioxane; 2,3-dihydro-1-benzofuran; 2,3-dihydro-1-benzofuranyl; 2,3-dimethoxy-5-nonylbenzene 2,3-dimethoxyphenyl; 2,3-didecylphenyl; 2,4,5-trimethylphenyl; 2,4-bis(trifluoromethyl)phenyl; , 4-diqi-3-decyloxyphenyl; 2,4-difluorophenyl; 2,4-dimethoxyphenyl; 2,4-didecylphenyl; 2,5-difluoro Phenyl; 158436.doc 201215609 2,5-dimethoxyphenyl; 2,5-dimethylphenyl; 2,6-dioxa-3-methylphenyl; 2,6-diphenyl 2,6-dimethoxy-4-methylphenyl; 2,6-dimethoxypyridine; 2,6-dimethylphenyl; 2-[ethyl(methyl)amino]- 1,3-indolazole; 2-ethenylphenyl; 2-butoxy-4-fluorophenyl; 2-butoxy -5-aryl group, 2-butoxy-6-phenylphenyl; 2-chloro-3-(tri-methyl)-based, gas-3-fluorophenyl; 2-chloro-4-( Trifluoromethyl)phenyl; 2-chloro-4-fluorophenyl; 2-ox-4-methoxyphenyl; 2-chloro-4-methylphenyl; 2-gas-5-(hydroxyl) Base), 2-chloro-5-(trifluoromethoxy)phenyl; 2-chloro-5-(trifluoromethyl)phenyl; 2-a-5-fluorophenyl; 2-gas- 5-methoxyphenyl; 2-chloro-5-methoxyphenyl; 2-a-5-methylphenyl; 2-aero-6-fluorophenyl; 3-trifluoromethylphenyl; 2-chloro-6-methoxyphenyl; 2-phenylphenyl; 2-cyanophenyl; 2-ethoxy-4-fluorophenyl; 2-ethoxy-6-fluorophenyl; -ethoxyphenyl; 2-ethylcarbyl; 2-fluoro-3-(propan-2-yloxy)phenyl; 2-fluoro-3-(trifluoromethoxy)phenyl; 2-fluoro 3-methoxyphenyl; 2-fluoro-3-methylphenyl; 2~ sulphur-1 -phenyl)phenyl; 2-fluoro-4-(triponyl)phenyl; 2_fluoro_ 4·decyloxyphenyl; 2-fluoro-4-methylphenyl; 2-fluoro-5-methoxyphenyl; 2-fluoro-5-methylphenyl; 2-fluoro-6-methoxy Phenylphenyl; fluoro-6-propoxyphenyl; 2-fluorophenyl; 2H-1,3-benzodioxole; 2_甲烧横Aminophenyl; 2-methyl calcined phenyl; 2-methoxy_3_(=methyl)phenyl; 2-methoxy-4-(1Η-oxazol-1-yl)benzene 2; methoxyl_heart (trifluoromethyl)phenyl; 2-decyloxy-5-(propan-2-yl)phenyl; 2_decyloxy-5-(tris-decyloxy) Phenyl; 2-methoxy-5-fluorenylphenyl; 2-methoxy- 6-(propan-2-yloxy)phenyl; 2-methoxyphenyl; 2-methyl 3_〇塞»Sit; 2-methyl-2H-0 lead; 2-methyl-4-(1Η-°ϋ. _ι_基)Benzene.2 158436.doc -6 - 201215609 Mercapto-4-(trifluoromethyl)phenyl; 2-mercapto-4-propoxyphenyl; 2-mercaptophenyl ; 2-mercaptoacridine; 2-phenoxyphenyl; 2-phenylethane; 3-(1Η-indazol-1-yl)phenyl; 3-(2,2,2-trifluoroethyl Oxy)phenyl; 3-(2-methylpropoxy)phenyl; 3-(3,5-dimethyl-1H-indazol-1-yl)phenyl; 3-(4-fluorobenzene Oxy)phenyl; 3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl; 3-(cyclopentylaminomethane)phenyl; 3-(diethyl Aminoguanidino)-5-fluorophenyl; 3-(difluoromethoxy)phenyl; 3-(didecylaminesulfonyl)phenyl; 3-(ethanesulfonyl)phenyl 3-(ethylaminoindenyl)phenyl; 3-(methoxyindenyl)phenyl; 3-(methylaminoindenyl)phenyl; 3-(morpholin-4-yl)benzene 3-(»Bottom-1-yl)phenyl; 3-(pyridin-1-ylmethyl)phenyl; 3-(» bottom: 1,4-yl)phenyl; 3-(propyl -2-yl) phenyl; 3-(propan-2-yloxy)phenyl; 3-(propan-1-sulfonylamino)phenyl; 3-(pyrimidin-2-yl)phenyl; -(trifluorodecyloxy)phenyl; 3-(trifluoromethyl)phenyl; 3,4-diphenyl; 3,4- Dimethoxyphenyl; 3,4-dimethylphenyl; 3,5-dichlorophenyl; 3,5-difluorophenyl; 3,5-dimethoxyphenyl; 3,5- Dimethylphenyl; 3-[(2-methylpropyl)amine-carbamoyl]phenyl; 3-[(didecylamino)methyl]phenyl; 3-[[morpholin-4-yl]) Alkyl]phenyl;3_[(propan-2-yl)aminecarboxylidene]phenyl;%[2-(dimethylamino)ethoxy]phenyl;3.[2_(didecylamine) Ethyl)phenyl; 3-[2-(morpholin-4-yl)ethoxy]phenyl; 3-ethenylphenyl; 3-butoxyphenyl; 3-chloro-2- (morpholin-4-yl)pyridinium; 3-oxo-2-fluorophenyl; 3-oxo-2-methoxyphenyl; 3-chloro-2-indolylphenyl; 3-chloro- 4_( Trifluoromethyl)phenyl; 3-ox-4-methoxyphenyl; 3-chloro-4-ylphenyl; 3-chloro-4-phenyloxyphenyl; 3-a-5-( Diethylamine-mercapto)phenyl; 3·chloro-5-(hydroxyindenyl)phenyl; 3-a-5-fluorophenyl; 3-chloro-5-methoxyphenyl; 158436.doc 201215609 3-ox-5-fluorenylphenyl; 3'-oxyphenyl; 3-cyanophenyl; 3-ethoxyphenylfluorophenyl; 3-ethoxy-4-fluorophenyl; 3-ethoxy Phenylphenyl; 3-ethylphenyl, 3-fluoro-2-methoxyphenyl; 3-fluoro_2_曱Phenyl; 3_fluoro-2-indolylphenyl; 3-fluoro-4-(anthracene-«.pyrazol-1-yl)phenyl; 3-fluoro_4_(2,2,2_trifluoroethyl Oxy)phenyl; 3~fluoro-4-(methylthio)phenyl; 3-fluoro-4-(trifluoromethoxy)phenyl; 3·fluoro-4-(trifluoromethyl)benzene 3-fluoro-4-methoxyphenyl; 3-fluoro-4.methylphenyl; 3-fluoro-4-indolylphenyl; 3-fluoro-% (2'2,2·2 Fluoroethoxy)phenyl; 3-fluoro-5-(2-methylpropoxy)phenyl; 3-fluoro-5-(morpholin-4-yl)phenyl; 3-fluoro_5_(„ Bilobidine-hydrazinyl)phenyl; 3-fluoro-5-(trifluoromethyl)phenyl; 3·fluoro-5-methoxyphenyl; 3-fluoro-5-methylphenyl; 3- Fluorophenyl; 3-hydroxyphenyl; 3-methanesulfonylphenyl; 3-methoxy-4-methylphenyl; 3-methoxy-5-nonylphenyl; 3-methoxybenzene -3 -methyl-based; 3-phenylphenyl; 3-phenylpropenyl; 3-propoxyphenyl; 3-aminesulfonylphenyl; 3-tert-butylphenyl; 4_( 1 • cyanocyclopentyl) benzyl, 4-(1Η-β米嗤-1-yl)phenyl; 4-(1Η-πm-sial-1-ylindenyl)phenyl; 4-(1Η- ηBizozol-1-yl)phenyl; 4-(2-mercaptopropoxy)phenyl, 4-(4-ethoxyphenyl) Phenyl; 4-(4-methylpiperazine-1.yl)phenyl; 4-(difluoromethyl)-3-fluorophenyl; 4-(didecylaminoindenyl)phenyl; 4_ (ethoxylated)phenyl; 4-(ethylaminoindenyl)phenyl; 4-(hydroxyindenyl)phenyl; 4-(morpholin-4-yl)phenyl; 4-(propyl -2-yl)phenyl; 4·(prop-2-yloxy)phenyl; 4-(°-pyridin-1-yl); 4-(°-pyridin-1-yl)phenyl; 4-(trifluoromethoxy)phenyl; 4-(trifluoromethyl)phenyl; 4·(tri-indenyl)pyridinium; 3,5-difluorophenyl; 4,5-difluoro 2-methoxyphenyl; 4-[〇R)-l-hydroxybutyl]phenyl; (dimethylamino)methylphenyl; 4-[(. Ratio 158436.doc 201215609 rridine-1-yl)carbonyl]phenyl; 4-[2-(dimethylamino)ethyl]phenyl; 4_ [2 (Bitter bite · 1_yl) ethoxy] benzyl, ethoxyphenyl; 4 butoxy-2-methylphenyl; 4-butoxy-3-chlorophenyl; 4_ Oxy-3_fluorophenyl, 4-butoxyphenyl; 4·butylphenyl; 4·chloro-2-(trifluoromethyl)phenyl, 4-chloro-2-ethoxyphenyl; 4-chloro-2-methoxyphenyl; 4_gas_2-methylphenyl; 4-chloro-3.(trifluoromethyl)phenyl; 4_gas_3_phenyl; 4_ 3-methoxyphenyl; 4-chlorophenyl; 4-cyanophenyl; 4-cyclohexylphenylethoxy-2-indenylphenyl; 4-ethoxy-3-d-fluorobenzene 4-yloxyphenyl; 4-ethylphenyl; 4, 2, (propan-2-yloxy)phenyl; 4, gas, 2'5-dimethylphenyl, 4-fluoro _2_methoxyphenyl; 4_gas_2_methylbenzene^; 4-Dun-3-(2,2,2_three ethoxy)phenyl; heart _3_(three gas Phenyl; 4-fluoro-3-[(propan-2-yl)aminecarboxylidene]phenyl; 4,3,methoxyphenyl, 4,fluoro-3-indolylbenzene & 4_ Fluorophenyl; 4_methanesulfonylphenyl; 4·methoxy-2-[(trimethoxymethyl)phenyl; 4-methoxy-2,5-dimethyl basic 4- 4-methoxy- 2-methylphenyl; 4-methoxy-3,5-dimethylphenyl' 4-methoxy_3_ Phenyl; 4_ methoxyphenyl; 4-methylphenyl; 4-methyl-Related bite; 4_ methyl. Diphene; 4_phenylbutane; 4 phenylphenyl; 4-phenyl-phenyl; 4·propoxyphenyl; 3,5-diphenyl; 5-(diethylamine oxime Styrene) - 2 phenyl; 5-(dimethylamino).比嗓;5·(.比嘻 ·············· &lt;;5_(trifluoromethyl)pyridine; 5·ethinyl-2-methoxyphenyl, 5·chloro-2-(2,2,2-trifluoroethoxy)phenyl; 5_ Chloro-2-(2,2-difluoroethoxy)phenyl; 5-chloro-propyl--yloxy)phenyl; 5-chloro-2-(propan-2-yloxy)phenyl; ·Chloro-2-ethoxyphenyl; % gas_2·ylphenyl” 5_wind_2_foxyphenyl; 5-chloro-2-methylphenyl; 5-chloro-2-propoxy I58436.doc 201215609 phenyl; 5·gas “bipyridine; 5-cyano-2-nonyloxyphenyl; 5-fluoro-2-(hydroxyindenyl) benzyl; 5-fluoro-2-methoxy Phenylphenyl; 5-oxo-2-methylphenyl; 5-fluoro-6-methylpyridine; 5-fluoropyridine; 5H, 6H, 7H, 8H, 9H-imidazo[12-a]azep; , 611, 711, 811, 911-imidazo[1,2-&amp;]azepine;5-hydroxy-(4-phenylphenyl);5-hydroxy-1-indolyl-1H-carbazole;5-hydroxy-2-(difluorodecyloxy)phenyl;5-hydroxy--3-(morphin-4-yl)phenyl; 5-pyridyl-3-(piperidinyl-yl)benzene 5-hydroxy-3-(.pyrrolidin-1-ylphenyl; 5-methoxypyridine; 5-methylpyridine; 5-nonylthiophene; 5-tert-butyl-2-oxo Phenylphenyl; 6-(111-° than "1 sitting-1-yl"&quot; Specific bite; 6-(3,4-difluorophenyl) 0-pyridine; 6-(4-mercaptopiperazin-1-yl)pyridine; 6-(didecylamino)pyridine; 6- ( Phenyl-4-yl)pyridine; 6-(trifluoromethyl)pyridine; 6-amino-(3,5-difluoro-based); 6-chloro-2-fluoro-3-indolylphenyl; - odor" sits and [1,2-a] 0 ratio °; 6-azamidazo[l,2-a]»pyridinylphenyl; 6-decyloxynaphthalene; 6-methoxyl pyridine ; 6-methylpyrazine; 6-methylpyridine; thiatricyclo[7.4.0.02'7]tridecane_1(13), 2,4,6,9,11-hexene; Gas imidazo[1'2-&amp;]» than bite; cyclohexane, dimethyl-1,3_〇11; 1]|furan; isoindene; naphthalene; naphthylphenyl; A compound such as the compound of claim 1 or 2 wherein R1 is a cycloalkyl group, an aryl group or a heteroaryl group wherein the cycloalkyl group, the aryl group or the heterocyclic group The aryl groups are each unsubstituted or substituted by 1, 2, 3, 4 or 5 substituents which may be the same or different and independently selected from the group consisting of: a functional group, a hydroxyl group, a hydroxyalkyl group, a cyanogen group Base, alkyl, alkynyl, alkynyloxy, alkoxyalkyl, alkoxy, chiral Alkoxy, -C(〇)NH(alkyl), -C(0)NH(cycloalkyl), -C(0)N(homo)2, arylalkoxy-, aryloxy ...cycloalkane 158436.doc •10· 201215609 base, heterocycloalkyl, aryl, (heterocycloalkyl)alkyl-, (heterocycloalkyl)alkoxy-, -c(o)heterocycloalkyl , heteroaryl, (heteroaryl)alkyl-, s(0)2-alkyl, -S.alkyl, -C(o)alkyl, -s(o2)nh2, -s(o2)nh (alkyl), -s(o2)n(alkyl)2, -n(h)(so2)(alkyl), wherein the cycloalkyl group, the heterocycloalkyl group, the aryl group or the heteroaryl group Each may be substituted with one or more _ groups, cyano groups, alkyl groups or alkoxy groups; and Z is 0, 1 or 2 〇 17. As requested! a compound of 2, wherein R1 is cycloalkyl, aryl or heteroaryl, wherein the cycloalkyl, the aryl or the heteroaryl are each unsubstituted or substituted by 1, 2, 3, 4 or 5 Substituents, which may be the same or different and independently selected from the group consisting of: a functional group, an alkyl group, and a haloalkoxy group. 18. The compound of claim 1 or 2 wherein the haloalkyl group is _CHZF3_Z, -CH2CHZF3.Z, and z is 0, 1 or 2. 19. The compound of claim 1 wherein the haloalkoxy group is _〇CHzF3.z and z is 0, 1 or 2. 20. The compound of claim 1 or 2 wherein the halo group is F. 21. The compound of claim i or 2 wherein the reverse is 1H pyrazole [3, 4_b] &lt; bite. 22. The compound of claim 1 or 2 wherein r is ι, 8 &amp; dihydroisozolo[12_a] ° ratio. set. 23. A compound selected from the group consisting of: Ν [4-(π bottom base) base]_3_(0 to 唆_3_yl) acrylamide oxime-[4_(° pyridine-1 -sulfonyl)phenyl]-2-(pyridine-3-yloxy)acetamide 158436.doc -11- 201215609 N-[4-(piperidin-1-sulfonyl)phenyl]-1Η -° ratio is [3,2-c]. Bis-2-carbamide N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}-1Η-«bido[3,2-c]acridin-2-indole Indoleamine N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}thieno[2,3-b]acridin-2-indole N-{[4-(piperidine) -1-sulfonyl)phenyl]methyl}-1Η-»pyrolo[2,3-indole]pyridin-2-carboxamide N-{[4-(piperidin-1-sulfonate) Phenyl]fluorenyl}-1Η-carbazole-5-formamide φ N-{[4-(piperidin-1-sulfonyl)phenyl]methylpyrazole[3,4-b ]. Bipyridine-5-carbamamine N-{[4-(piperidin-1-sulfonyl)phenyl]indolyl}imidazo[1,2-a]acridine-6-carboxamide N-{ [4-(Piperidine-1-sulfonyl)phenyl]methyl}-1Η-imidazo[1,2-b]. Biazo-5-carbamidine N-{[4-(piperidin-1-sulfonyl)phenyl]methyl}thieno[3,2_c]acridin-2-ylamine _ N-{[ 4-(piperidin-1-sulfonyl)phenyl]methyl}-[1,2,3,4]tetrazolo[1,5-a]pyridin-7-decylamine N- { [4 -(piperidin-1-sulfonyl)phenyl]methyl}imidazo[1,2-appyridyl-7-decylamine N-{[4-(piperidin-1-sulfonyl)benzene Methyl}-1,6-acridin-2-ylamine 1^-{[4-(piperidin-1-sulfonyl)phenyl]methyl}acridin-3-carboxamide N -{[4-(piperidin-1-sulfonyl)phenyl]indolyl}-1Η-1,3-benzobisazole-5- 158436.doc -12· 201215609 Formamide N-{[4 - (piperidine_ι· 醯 )) phenyl] fluorenyl 1 &gt; 3_benzo. Septose-6-carbamamine N-{[4-(piperidin-1 sulfoindole)phenyl]indolylfuro[3,2-c]&quot;bipyridyl 2-carbamide -{1-[4-(piperidin·ι_sulfonyl)phenyl]ethyl}_1Η·吼-[3,2-c]pyridine-2-carboxamide N-[(4-{8 -oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl}phenyl)indolyl]thieno[2,3-c]pyridin-2-indole N-[(4 -{8-oxa-3-azabicyclo[3.2.1]octane-3-sulfonyl}phenyl)methyl]-1H-. More than [3,2-c]. Bis-pyridine-2-decylamine N-[(4-{8-oxa-3-azabicyclo[3.2.1]octane-3-ylindolyl}phenyl)methyl]imidazo[l, 2-a]pyridine-6-carboxamide Ν·({4-[(5-chloro-2-indolyloxyphenyl)amine sulfonyl]phenyl}indenyl)-1Η-0 ratio 咯[ 3,2-c]pyridin-2-decylamine N-({4-[(2-ethylphenyl)phenylsulfonyl]phenyl}methyl)-1Η-η ratio [3, 2-c]pyridine-2-carboxamide ν·({4-[(4-chloro-2-indolyl-5-nonylphenyl)amine sulfonyl]phenyl}indenyl)-1Η- Pyrrolo[3,2-c]pyridine-2-carboxamide N-({4-[(2-propoxyphenyl)aminesulfonyl]phenyl}methyl)-1Η-&quot; And [3,2-c]. Bis-pyridine-2-decylamine N-({4-[(5-fluoro-2-decyloxyphenyl)aminesulfonyl]phenyl}indenyl)-1Η-0 ratio [3,2 -c]pyridin-2-decylamine N-({4-[(quinolin-8-yl)aminesulfonyl]phenyl}fluorenyl)-1Η-° ratio 158436.doc -13· 201215609 [3,2-c] acridine_2_carbamamine N_[(4-{[2-(piperidin-1-yl)phenyl]amine sulfonyl}phenyl)methyl]-1H-pyrrole And [3,2-c]pyridine_2_formamide N_[(4_{[2-(morpholine-4-yl)phenyl]aminesulfonyl}phenyl)methyl]1H_pyrrolo[3 ,2-c]pyridine_2_formamide 1^({4-[(5-methoxy-2-methylphenyl)aminesulfonyl]phenyl}methyl)_ 1H-pyrrolo[ 3,2_c]pyridine_2_carbamamine Ν[[4·{[2-(propan-2-yloxy)phenyl]amine sulfonyl phenyl)methyl b 1 Η-pyrrolo[3, 2_c]pyridine_2_ amidoxime·({4-[(2-phenoxyphenyl)aminesulfonyl]phenyl}methyl)_1H_„pyrho[3,2-c]pyridine_ 2. Myramine N_({4-[(3-methoxy-2-methylphenyl)aminesulfonyl]phenylindolemethyl)_ 1Η-°Bilo[3,2-c] Specific bite _2_carbamamine N-({4-[(4-fluoro-2-decyloxyphenyl)amine sulfonyl]phenyl}methyl)_1H_ 0 ratio [3,2- c]pyridine_2-formamide N-[(4-{[2-(Trifluoromethoxy)phenyl]aminosulfonyl)phenyl)indolyl 1H-0, piroxi[3,2-c] acridine-2-indole Amidoxime·({4-[(5,6,7,8-tetrahydronaphthalen-1-yl)aminesulfonyl]phenyl}indenyl)_ 1Η-° ratio 咯[3,2-c Pyridine-2-carbamide Ν·({4-[(2-decyloxyphenyl)amine sulfonyl]phenyl}methyl)pyrolo[3,2-c]pyridine_2_A Amidoxime·({4-[(2-methoxy-6-methylphenyl)aminesulfonyl]phenyl}indenyl)_ 1Η_〇pyrolo[3,2-c]pyridine- 2-nonylamine N-({4-[(4-methoxy-2-methylphenyl)amine sulfonyl]phenyl}methyl)- 158436.doc •14· 201215609 1H-pyrrolo[ 3,2-c]pyridine_2_carbamimidoxime-({4·[(2,3-dihydro-14-benzodioxan-6-yl)aminesulfonyl]phenyl }Methyl)-1Η-pyrrolo[3,2-c]npyridin-2-ylamine N_[(4-{[2-(2-hydroxyethoxy)phenyl]aminesulfonyl} Phenyl)methyl]_lH-ηpyrolo[3,2_c]pyridine_2-carbamimidamine N-({4-[(4-ethoxy-2-phenafluoro)aminosulfonyl] Phenyl}methyl)_1H_pyrrolo[3,2-c]pyridine-2-carboxamide N-[(4-{[2-(hydroxymethyl)phenyl]amine sulfonyl)phenyl) °比比洛和[3,2-c]» ratio Amides -2- Yue ^ 1 - ({4 - [(1-oxo-iso-rattle -111- alkenyl _5- yl) amine sulfonamide acyl] Yue-yl} phenyl) -1Η-. Biluo[3,2-c]° pyridine-2-carboxamide N-[(4- oxasulfonylamino)indolyl]_1H_pyrrolo[3,2_c]pyridine_2_ Amine Ν{{1-(phenylsulfonyl)piperidin-4-yl]indolyl}-1Η-«bibromo[3,2-cp ratio °-2-cartoamine N_[(4-stupid Methionine phenyl) fluorenyl]-ih-咐·rho[3,2-c]° pyridine-2-carbamide N-[(4-{[2-(trifluorodecyloxy)) Benzene]sulfonylamino}phenyl)indolyl]_1H_pyrrolo[3,2-c]pyridin-2-indoleamine·{[4-(piperidin-1-sulfonyl)phenyl]- Thio[2,3-c]«pyridin-2-cartoamine n-({4-[(2,5-dimethoxyphenyl)amine sulfonyl]phenyl}fluorenyl) -iH-pyrrolo[3,2-c]pyridin-2-decylamine N-[(4-{[2-methoxy-5-(trifluoromethyl)phenyl]aminesulfonyl}benzene Base) 158436.doc -15- 201215609 Methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide N-[(4-{[4-chloro-2-(trifluoromethoxy) Phenyl]aminosulfonyl}phenyl)methyl]-1H-indolo[3,2-c]pyridine-2-carbamimidoxime-({4-[(1Η-carbazole-6) -amino)sulfonyl]phenyl}methyl)-1Η-°pyrho[3,2-c]pyridine-2-carboxamide 6-amino-1H-pyrrolo[3,2-c Pyridine-2-carboxylic acid 4-(piperidin-1-sulfonyl)- 1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid 4-(piperazin-1-sulfonyl)-benzylguanamine 1H-pyrrolo[3,2-c]pyridine- 2-(4-Amino-cyclohexylamine sulfonyl)-benzyl decylamine 1H-pyrrolo[3,2-c]pyridine-2-carboxylic acid 4-(3-amino-pyrrolidine- 1-sulfonyl)-nodal decylamine 1H-pyrrolo[3,2-c]picolinic acid 4-(3,8-diaza-bicyclo[3.2.1]octane_3_sulfonyl) Benzyl decylamine sinter and [1,2-a]pyrimidine-6-carboxylic acid 4-(piperazine-1 -sulfonyl)- benzyl decylamine singly [2,3-C]° ratio 4-(Piperazine-1-sulfonyl)-pyridylamine 1Η -0 ratio Φ r ^ a open M,4-b]pyridine_5_carboxylic acid 4-(piperazine-1 -sulfonyl)-benzylamine oxime [2,3-c]% pyridine 2_carboxylic acid 4_(4-amino-cyclohexylaminesulfonyl)-benzylamine oxime 2,3_c]°-pyridine-2-carboxylic acid 4-(4-amino-cyclohexylaminesulfonyl)-benzylguanamine 1H_° ratio sit[[,4吒]pyridine_5_carboxylic acid 4- (4-Amino-cyclohexylamine sulfonium 158436.doc 201215609 base)-nodal amide thieno[2,3-c]pyridine-2-decanoic acid 4-(3-amino-pyrrolidine-1- Sulfhydryl)-nodal imidazolidine [1,2-a]pyridine-6-decanoic acid 4-(3-amine -pyrrolidin-1-sulfonyl)-nodal amide amine furo[2,3-c]pyridine-2-furic acid 4-(3-amino-pyrrolidin-1-sulfonyl)-] Indole 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid 4-(3-aminopyrrolidin-1-sulfonyl)-pyristylguanidamine imidazo[l,2-a] Acridine-6-decanoic acid 4-(piperazin-1-sulfonyl)-benzyl decylamine furo[2,3-c]acridine-2-furic acid 4-(piperazin-1-sulfonate) -benzyl carbazide imidazo[1,2-a]pyrimidin-6-decanoic acid 4-(3-amino-pyrrolidin-1-sulfonyl)-benzyl decyl imidazolium [1,2 -a]pyrimidine-6-decanoic acid 4-(4-amino-cyclohexylaminesulfonyl)-benzylguanamine imidazo[1,2-a]pyridine-6-decanoic acid 4-(4-amine -cyclohexylamine sulfonyl)-benzyl decylamine 1H-pyrazolo[3,4-b]acridin-5-decanoic acid 4-(4-cyano-piperidin-1-sulfonyl) - benzylamine 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid 4-(4-cyanoguanidino-piperidin-1-sulfonyl)-pyristylamine 1H-pyrazole And [3,4-b]pyridine-5-carboxylic acid 4-(4-decyloxy-piperidin-1-sulfonyl)-pyristylguanamine 1H-pyrazolo[3,4-b]pyridine- 4-(4-Amino-piperidine-1-sulfonate 158436.doc -17- 201215609 base)------ 1H- ° ratio "sit and h U,4-b] Pyridine-5-decanoic acid 4·[4-(2,2,2-trifluoro-ethylamino)-[Bottom-biting-Κ _# _ _]-benzyl amidoxime-({4- [ΐ·(3 Preparation, gas phenyl)-1Η-indoleazole-4_sulfonyl]phenyl}fluorenyl)- 1Η-pyrazolo[3,4,b]pyridine_5_decylamine N-, gas, 2-ethoxybenzo)sulfonyl]phenyl}methyl)pyrolo[3,2-c]» than mouth methylamine N-{[4-(dimethylazolyl [3,4-b]Dtfci-1,3-1,3-thiazol-5-sulfonyl)phenyl]methyl}_ih t-5-formamide-0 than N-[(4-{[2»fe Gas, 4-(ιη-«bazol-1-yl)benzene]sulfonyl}phenyl)indenyl] Ή[l'2-a] 咬6_甲甲胺胺'5-methyl Benzene sulfonyl]phenyl}indenyl)_1H_D-pyrazolo[Mb]pyridine|decylamine (([(5~ Ethyl-2-oxooxybenzene))) Imidazo[1'2-a]. Benzomethamine (Μ[(2_fluoro-4-mercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]° than bit-2-cartoamine N [( 4-{[3-Fluoro-5-(2,2,2-trifluoroethoxy)benzene;j sulfonyl}phenyl)methyl]imidazo[l,2-a] Amine [methyl 5-(difluoromethyl)_1Η-η ratio η sit-4-indolyl]phenyl}methyl)imidazo[l,2_a]pyrimidine_6_decylamine N-{[4 -(stupyl) phenyl]methyl}isoquinoline _6_ amidoxime [[4-{[3_(trifluoromethyl)benzene] benzyl] phenyl) methyl ^ m嗤[l,2-a]pyrimidine_6_formamide 15S436.doc 201215609 N- [(4-1 r〇, Ui-(piperidin-1-ylindolyl)]]]] ) fluorenyl] imidazo[, a]. Ratio to 6-carbamamine N-({4'-'L (trifluoromethyl) D-pyridin-3-sulfonyl]phenyl}methyl)thieno[2'3-c]. Bisidine_2_carbamidine ({4[(4-butylphenyl)] hydrazino] phenyl) methyl) oxazolo[l,2_a]pyridine-6-cartoamine N-1 [ 4 - f 〇Άmethyl η-pyridin-3-sulfonyl)phenyl;] fluorenylpyrho[3'2_e]°l, 2-decylamine ({4-[(4-methoxy) 3,5-Dimethylbenzene)sulfonyl]phenyl}fluorenyl)furano[2,3'c]pyridine-2-carboxamide, ({4'[(4-butoxy-3) - gas stupid) sulfonyl]phenyl} fluorenyl)_1H-pyrrolo[3,2~C]. Bipyridine-2-carboxamide N-1 [4〇, 'methyl-2Η-carbazol-6-sulfonyl)phenyl]fluorenyl}-1Η-pyrazolo[3'4'b]° Tt bite_5_carbamamine ({4'[(2-decanesulfonylbenzene)sulfonyl]phenyl} indenyl)_1H-pyrazolo[3'4~b]° ratio bite-5 - indoleamine N- [ (4 / r〇, ~U3_chloro_5-(hydroxymethyl)benzene]sulfonyl}phenyl)methyl]imidazo[,2-a]pyrimidine_6_A Indoleamine N_[(M[3-(diethylaminofluorenyl)_5_fluorobenzene]] fluorenyl}phenyl)methyl]0furano[2,3-C]» than bite·2· Mercaptopurine-({4-[(2-chloro-6-methoxybenzene) hydrazino]phenyl}indolyl)thieno[2,3-c]pyridine-2-carboxamide N- ({4-[(3-Chloro-4-propoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a] mouth bite-6-cartoamine 158436.doc •19· 201215609 N-({4-[(2,3-dimethylphenyl)cansyl]phenyl}methylindole-pyrrolo[3,2-c]pyridine-2-carboxamide N-[(4 -{[3-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-carboxamide N-({4-[( 4-ethylmercaptophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-{[4-({3-[(2-mercaptopropyl) Aminomethyl thiol] Phenyl]methyl}-111-pyrrolo[3,2-c]pyridine-2-carboxamide N-({4-[(2-chloro-6-fluorobenzene)sulfonyl) Phenyl}methyl)imidazo[l,2-a] ° ratio biting-6-decylamine]^-({4-[(3-fluoro-5-methylphenyl)indolyl]phenyl }曱基)°夫喃和[2,3-c]° ratio biting-2-anthracene N-({4-[6-(trifluoromethyl)phosphonium ratio. Continuation of the base] phenyl} Methyl) °f-[2,3-c]pyridine-2-carboxamide N-{[4-({4-[2-(°pyrrolidin-1-yl)ethoxy]benzene} Sulfhydryl)phenyl]fluorenyl}-1Η-pyrrolo[3,2_c]° pyridine-2-decylamine N-[(4-{[3-(morpholin-4-yl)benzene]sulfonate Mercapto}phenyl)methyl]-1Η-°pyrho[3,2-c]pyridine-2-carboxamide N-({4-[(4-butoxy-2-methylbenzene)) Sulfo]yl]methyl]imidazo[l,2-a]pyridin-6-nonylamine N-({4-[(4-fluoro-2,5-dimethylphenyl)sulfonyl) Phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-[(4-{[2-methyl-4-(trifluoromethyl)]]]]] Phenyl) indenyl]imidazo[l,2-a]pyrimidin-6-decylamine 158436.doc •20· 201215609 N-({4-[(3-ethylphenyl)indolyl]phenyl} Methyl) _ih_〇 ratio. Sit and [3 4_ b] ° than 0 to 5 -carbamamine N-({4-[(3-phenylbenzene))]phenyl} fluorenyl) sodium saliva [丨^^^ ratio Pyridin-6-formamide N-({4-[(2-chloro-5-methylbenzene)cansyl]phenyl}indolyl)imidazo[12_a]pyridine-6-nonylamine N- ({4-[(2-Chloro-3-fluorobenzene) contigyl)phenyl}indenyl). Bisazo[3,4-b]pyridine-5-carbamimidamine N-[(4-{[5-Gas-2-(2,2,2-trifluoroethoxy)benzene]sulfonyl) }phenyl)methyl]imidazo[l,2-a]° ratio bit-6-amidoxime-({4-[(4·butoxybenzene)sulfonyl]phenyl}fluorenyl) Imidazo[丨,2_a]pyridine-6-carboxamide N-({4-[6-(trifluoromethyl)pyridinium-2-sulfonyl]phenyl}methyl-azolo[3, 4-b]pyridine-5-nonylamine N-({4-[(2,5-diamidino))sulfonyl]phenyl}indolyl buprolo[3,2-c]pyridine- 2-曱醯amine^ Ν-({4·[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamidine Amine^-{[4-({3-[2-(morpholin-4-yl)ethoxy)phenyl}sulfonyl)phenyl]methyl}°[2,3-〇]° N-({4-[(3-)-5-methylphenyl)sulfonyl]phenyl}indolyl) furan [2,3_c] ° than pyridine-2 Indoleamine N-({4-[(4-ethoxy-3-fluorobenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide 158436. Doc •21 - 201215609 N (d[(4-chlorophenyl) continuation]phenyl}methyl) cough and [2,3♦ than bite _ 2-cartoamine N-({H(4-B) Phenyl) phenyl]methyl) hydrazine Affinity [23 small ratio bite-2 - anthraquinone N with 4-[(4-ethoxy.2.methylphenyl)sulfonyl]phenylindolemethyl)imidazo[l,2-a] Pyridine-6 arylamine N gas M-[(3-chloro-5-fluorophenyl)sulfonyl]phenyl}methyl)imidazo[nq ° than pyridine-6-carboxamide ^ {[4-( 1-cyanocyclopentyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine-6-nonylamine N U4-[(3-propoxyphenyl)sulfonate Thio[2,3c]pyridine-2-carboxamide N [(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl )methyl]mi-[S,2-a]pyrimidine_6-carbamamine n_({4-[(4-fluoro.2-methoxyphenyl)sulfonyl]phenyl}methyl) _1H•pyrrolo[3,2-c]pyridine_2_amidoxime_“4·[(3-fluorophenyl)sulfonyl]phenyl}methyl)pyrazole[3,4_b] 0 bite -5 -decylamine 1^[(4-{8-thiatricyclo[7.4.〇.〇2,7]tridecane_1(13), 2,4,6,911_hexene-6-sulfonate Thio[phenyl]indenyl]furo[2,3_c]pyridine_2_carbamidamine·{[4-(1-methyl-iH_carbazole-7-sulfonyl)phenyl]indole Furano[2,3-c]acridine-2-carbammine N_{[4-(5-chloro-3-methyl). Bis-2-sulfonyl)phenyl]methyl}imidazo[l,2_a]pyrimidine_6·carbamamine 158436.doc -22- 201215609 N-{[4-(isoquinoline-4-sulfonate) Mercapto)phenyl]indenyl}thieno[2,3-c]. Than. N-(methylamino)N-({4-[(5-chloro-2-ethoxyphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c]pyridin-2-indole Indoleamine N-({4-[(3-fluoro-4-decyloxyphenyl)sulfonyl]phenyl}methyl)-1Η-. [r-buto[3,2-c]pyridine-2-carboxamide N-[(4-{[3-chloro-5-(diethylaminocarbamoyl)benzene]sulfonyl}phenyl)indole Imidazo[l,2-a]pyrimidin-6-formamide φ N-({4-[(3,4-difluorophenyl)sulfonyl]phenyl}indolyl)furan [2, 3-c] Pyridine. 2-carbamidine N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridin-2-indole Amine N-[(4-{[4-(4-mercaptopiperazin-1-yl)benzene]sulfonyl}phenyl)indolyl] is sitting and [1,2 - a] ° is 0 -6 - anthraquinone N-[(4-{[2-(ethoxyindolyl)benzene]sulfonyl}phenyl)indolyl]-lH-η-pyrazolo[3,4-b]pyridine -5-decylamine • N-({4-[6-(morpholin-4-ylpyridin-3-sulfonyl)phenyl}methylpyrazolo[3,4-b]pyridine-5 - indoleamine N-{[4-(phenylsulfonyl)phenyl]indolyl}-1Η-.pyrho[2,3-c].pyridin-3-carboxamide N-[(4 -{[3-Fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine-6-carboxamide N-({4-[(3-fluoro-2-indolylbenzene)sulfonyl]phenyl}indolyl)thieno[2,3-c]pyridine-2-didecylamine 158436.doc - 23· 201215609 N-({4-[(2-Chloro-4-methylphenyl)sulfonyl]phenyl}methyl)-1Η-.pyrho[3,2-c]pyridine-2-methyl Indoleamine N-{[4-(quinolin-6-sulfonyl)phenyl]methyl}-1Η-oxazolo[3,4-b]»pyridin-5-carbamimidoxime·{[ 4-(1-methyl-1H-indazole-5-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyridine-6- Indoleamine N-({4-[(5-|L-2 -nonylbenzene) continuation]phenyl}indenyl) &lt;»夫&quot;南和[2,3-c]0 ratio °-2-carbamimidoxime-{[4-(1-propyl-1Η-carbazole-4-sulfonyl)phenyl ]曱基}·1Η-. Bisazo[3,4-b]pyridine-5-nonylamine N-({4-[(3,4-dimethoxyphenyl)sulfonyl]phenyl}methyl)thiophene [2, 3-c]pyridine-2-carboxamide N-({4-[(3-a-5-methoxybenzene))]phenyl}methyl-[3,4-b]° ratio Bite-5-carbamamine N-({4-[(4-ethylphenyl)sulfonyl)]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide N-( {4-[(2,4,5-Trimethylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carbamimidoxime-({4·[2 -(Trifluoromethyl)imidazolium pj-a]indolepyridin-6-sulfonyl]phenyl}methyl)-1Η-pyrazolo[3,4-b]pyridine-5-carboxamide N -[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]thieno-p,3_c]° than 2-mercaptoamine N-({4- [(4-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3_c]DI;fc(pyridine-2-carboxamide 158436.doc •24- 201215609 N-[(4-{ [2-Fluoro-4-(1Η-°bazol-1-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridin-2-indole N_({4 -[(2-chlorophenyl)sulfonyl]phenyl}indolyl)-1Η-°pyrolo[3,2-c]pyridine-2-carboxamide N-({4-[(3-chloro) -4-propoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c] Pyridyl-2-carboxamide N-({4-[(2-fluoro-6-propoxybenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridin-2-indole Amidoxime • N-[(4-{[2-(morpholin-4-ylmethyl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c]pyridine-2-carboxamidine Amine N-({4-[(5-fluoro-2-methoxybenzene) hydrazino]phenyl}indolyl). Sodium[1,2-a]°^^-6-carboxamide N_[(4-{[2-(2,2,2-trifluoroethoxy)_4-(trifluoromethyl)benzene]] fluorenyl)phenyl)indolyl]-1H-. [3,2-c]. 唆-2-decylamine N-({4-[(2-fluoro-3-indolyl)sulfonyl]phenyl}methylpyrrolo[3,2 -c]° than bite _2-formamide N_[(4-{6-amidazopyridinium-3-ylsulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine_6 _ decylamine N (2 [4'( oxasulfonyl)phenyl]ethyl}-1 Η-η ratio 咯[3,2-c]&quot; pyridine-2-nonylamine N [(4 -{[3'(Trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridinecarboxamide N-[(4- { [4 (丁·乂Propyl)phenyl]sulfonyl}phenyl)methyl]furo[2,3_C]° ratio bitolinamide 158436.doc -25· 201215609 N-({4-[(3-chloro) Benzene sulfonyl]phenyl}indenyl)-iH-«咯[3,2-c] ° ratio bit-2-formamide N-[(4-{ [4-(2-mercaptopropoxy)benzene] hydrazino}phenyl)indolyl]_1H_咯[3,2-c]pyridine-2-carboxamide N-({4-[(3-ethylphenyl)sulfonyl]phenyl}methyl)thieno[2,3_c]pyridine- 2-Protonamine N-({4-[(3-)-phenylene)]phenyl}methyl is more than 嘻[3,2-b] ° than 2-mercaptoamine N-{[ 4-(6-methoxy"pyridyl-2(sulfonyl)phenyl]methyl}furo[2,3_c]pyridine-2-carboxamide-({4-[6-(two) Methylamino). Bisidine_3·sulfonyl]phenyl}methyl)_1Η_pyrrolo[3,2-c]pyridine-2-carbamimidoxime-({4-[(4-fluoro-3-indolylbenzene)) Sulfosyl;|phenyl}methyl)_1Η_η-pyrazolo[3,4-b]° ratio 5-amine amidoxime-[(4·{[3-(decyloxyfluorenyl)benzene] Sulfonic acid hydrazino hydrazino] imidazo[l,2-a]0 butyl-6-cartoamine N-({4-[(2-butoxy-4-fluorobenzene))sulfonyl) ]phenyl}methyl)imidazo[1,2-a]. N-({4-[(3-hydroxyphenyl)sulfonyl)phenyl}indolyl) imidazo[丨^^吼吼-6-carboxamide N-({4 -[(3-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-(:]pyridinidine-2-cartoamine (ethoxyl group) Benzene]sulfonyl}phenyl)methyl]imidazo[l,2-aj agidine·6·carbamamine I58436.doc 201215609 Ν-{[4-(1-methyl_1H_ carbazole) _4_sulfonyl)phenyl]fluorenyl}isoxazo[l,2-a]pyrimidine-6-carboxamide N-({4-[(5-Ga-2-methoxyphenyl)sulfonate) Mercapto]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide N-({4-[(3-ethoxy-2-pipefluoro)sulfonyl]phenyl }methyl)thieno[2,3-c]n ratio bite-2-cartoamine N-({4-[(2-ethylphenyl)sulfonyl)phenyl}methyl)_ih吼[3,2_c]D is more than a bit of chiral amine N-({4-[(4-fluoro_3_methoxybenzene)sulfonyl]phenyl}methyl)imidazo[1,2 -a]10 to 唆-6-cartoamine N-({4-[(4-ethoxy-3-trifluorobenzene))sulfonyl]phenyl fluorenyl. Bis-[3,2-c Acridine amidoxime-[(4-{[3ϋ(morpholine-4-yl)benzene]] fluorenyl phenyl)methyl]. pyrrolo[3,2-c]pyridine·2-carbamimidoxime -({4·[(2-Fluoro_6_- Oxyphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c]&quot;bipyridyl-2-carboxamide N-[(4-{[2-曱oxy_4_(three Fluoromethyl)benzene] continued fluorenyl}phenyl)methyl]imidazo[l,2-a]pyrimidine_6-formamide N-{[4-(2-methyl 吼 冬 冬) Phenyl]methyl} porphin η.] 0 is more than 唆-2-carbamamine N-[(4_{8-oxatricyclo[7 4 〇〇 2,7] thirteen carbon_ι(ΐ3) ,2,4,6,9 ιι· 稀6六醯基}Phenyl) fluorenyl] 吱 并 [2,3_小比咬·2_甲甲胺Ν_({4-[(4-benzene) Benzene) 醯 ] ] 笨 } } } } } 2 2 2 2 2 2 2 158 158 158 158 ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( 4-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide N-[(4-{[2-fluoro-4-(trifluoro) Methyl)benzene; 1sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide N_({4-[(5-Ga-2-propoxybenzene)) Sulfhydryl]phenyl}fluorenyl μη-ο than „[3,2-c]pyridine-2-carbamimidoxime-{[4-(2Η-1,3-benzodioxole) Alkene-5-sulfonyl)phenyl]methyl}-1Η-. Bisazo[3,4-b]° ratio 5--5-carbamamine N_{[4-({4-[(lR)-l-hydroxybutyl]benzene}sulfonyl)phenyl]fluorenyl } Imidazo[l,2-a]pyrimidine-6-nonylamine n_{[4-(5-nonylthiophen-2-sulfonyl)phenyl]methyl}_m_.比 并 [3,2-c]» than bit -2- an amine N_({4-[(3-decyloxybenzene) hydrazino]phenyl}methyl) oxime [2,3 ^ Pyridyl-2-carboxamide N-{[4-({3-[2-(morpholine-4-yl)ethoxy]phenyl)sulfonyl)phenyl]methyl}imidazo[l, 2-a]pyridine-6-formamide N-{[4-(phenylsulfonyl)phenyl]methyl)imidazo[Ha]. Bisylazine_2_decylamine ({4[(4-ethoxyphenyl))]]}}}]]]]] { [4-(啥琳·8_续醯基)phenyl]methyl}吱〒[2,3-exobiidine_ 2-cartoamine N-[(4-{[3-(么琳_ 4_yl)phenyl]nonyl}phenyl)indenyl]_ih"pyrazolo[3,4-b]pyridine·5-carbamimidoxime-({4-[(2-fluorodecylbenzene)) Continued thiol]phenyl}methyl)_ιη" than saliva and 158436.doc 201215609 [3,4-b]pyridine-5-carbamimidoxime_({4·[(3,4-dibenzene)sulfonate) Benzo]phenyl}indolyl)furo[2,3-c] ° than bite-2 -cartoamine N_{[4-({4-fluoro-3-[(propan-2-yl))amine Benzene sulfonyl)phenyl] fluorenyl}imidazo[l,2-a]pyrimidine _6_ amidoxime [[4-{[2,4-bis(trifluoromethyl)benzene) Sulfhydryl}phenyl)methyl]imidazo[l,2-a]n ratio bite-6·artichoke-{[4-(1-mercaptocarbazole-6-sulfonyl)benzene Thio[2,3-c]pyridin-2-decylamine ν-[(4·{[3·fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl) Mercapto]furo[2,3-c]pyridine-2-carboxamide N-({4-[(2-fluoro-3-methoxybenzene)sulfonyl]phenyl}methyl)-1Η -° ratio of [3,2-c]pyrr ·2·Metaguanamine-[(4-{[2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]_ΐΗ-η ratio [3,2-c] Pyridine-2-decylamine N-({4-[(2-amily-4-propoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine-6- Formamide N-({4-[(3-phenylphenyl)sulfonyl]phenyl}indolyl)-1,3-benzothiazole_6_decylamine N-[(4-{[4- (ethylamine-mercapto)phenyl]sulfonyl}phenyl)indolyl]furan-[2,3-c]pyridin-2-decylamine N-({4-[(4-oxo) Benzene)sulfonyl]phenyl}methyl)imidazo[i,2_a]pyrimidine-6-carbamimidoxime-{[4-(1-methyl-1H-carbazole-6-sulfonyl) Phenyl]methyl}imidazo 158436.doc -29- 201215609 [l,2-a]pyridine·6-formamide [(4-{[3 gas cyclopentylamine)methyl]benzene]sulfonyl Phenyl phenyl) fluorenyl] thieno[2,3-c] „ pyridine 2 — decylamine ({4 [(3- gas-4-methylbenzene) hydrazino] phenyl hydrazine methyl) . Sepheno[2 3_ c]0 is more than 2-carbalamine, [(4,5-difluoro-2-methoxybenzene)sulfonyl]phenyl}indenyl)imidazo[l,2 -a]pyrimidine_6_nonylamine N [(4-{[3_(decyloxymethyl)benzene]sulfonylhydrazinophenyl)indolyl]imidazo[l,2-a]pyrimidine_6_ Formamide N [(4 {[3-fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl phenyl)methyl]thieno[2,3-c]pyridine -2-decylamine N {[4_(2H-1,3-benzodioxolesulfonyl)phenyl]methyl}thieno[2,3-c]pyridine-2-carboxamidine Amine N-[(4-{[5-Gas-2-(propan-2-yl-1-yloxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine -6-Protonamine N-({4-[(3-phenylphenyl)sulfonyl]phenyl}methyl)furo[2 3 e]. Bis-pyridine-2-decylamine N-({4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2- Methotrexate-[(4·{[3-(propyl-2-yloxy)benzene]sulfonylhydrazino)methyl]furo[2,3-c]acridin-2-indole Amine N-({4-[(3-methylphenyl)sulfonyl]phenylindolemethyl)furo[2,3_^〇pyridin-2-carboxamide N-({4-[6- (Dimethylamino)pyridine-3-sulfonyl]phenyl}indolyl)imidazole 158436.doc 201215609 And [1,2 a]pyrimidine_6_carbamamine N-({4-Γ(^c ^ LV ^ gas-2-propoxybenzene)sulfonyl]phenylhydrazine methyl)thieno[2'3 C]pyridine·2~decylamine, methoxy-3,5-dimercaptobenzene) Continued thiol]phenyl}methyl) mersin and [l,2-a] shouted _6 methotrexate N ^4 '[(3-cyanobenzene)sulfonyl]phenyl}methyl)furan And [2,3-c]pyridin-2-cartoamine N_G4-[(3-fluoro-4-propoxyphenyl)sulfonyl]phenyl}indenyl)furan • [2,3_c]pyridine -2-Aminoxime 4{4_[(2,6-dichloro-3-indolylbenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]acridine_2_ formazan Amine N-[(4-{2-[ethyl(methyl)amino]_1,3-thiazole-5-sulfonyl}phenyl)methyl]thieno[2,3- c]pyridine-2-carboximine N-({4-[(3-propoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[ua] oxime-6-cartoamine N-( {4-[(4-Fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3·® c]pyridin-2-indoleamine-{[4-(1 -propyl-1H-pyrazole-4-sulfonyl)phenyl]indolyl}-1Η-pyrrolo[3,2-c]. Bipyridine-2-carboximine N-{[4-(2-methyl-2H-indazole-6-sulfonyl)phenyl]indolyl}thieno[2,3-c]pyridine-2- Amidoxime-({4-[(3·decanesulfonylbenzene)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide N-[( 4-{[4-chloro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thiophene 158436.doc •31 · 201215609 and [2,3-c]pyridine-2-carboxamidine Amine N-({4-[(3-fluoro-2-methylphenyl) hydrazinyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide n-({4 -[(2-Ga-4-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-nonanyl n-({4-[(2_) Methanesulfonamide phenyl) phenyl]phenyl}indenyl)·1Η_pyrrolo[3,2-c]pyridine-2-carboxamide N-{[4-(2,3-dihydro) 1,4-benzodioxine_6_sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine·6-carbamamine Ν·({4-[2- (dimethylamino)pyrimidine_5_sulfonyl]phenylindenyl)_1H_pyrrolo[3,2-c]pyridine-2-indole N-({4-[(2-methyl) _4_propoxybenzene)sulfonyl]phenyl}methyl)imidazo[l'2-a] squeezing-6-cartoamine N-({4-[(2-methoxy_5) •methylbenzene)sulfonyl] }}methyl)_iH_〇比比和[3'2-c]pyridine_2_carbamimidoxime-({4-[(2,4.dimethoxybenzene)sulfonyl]phenyl} Methyl)lH_e than succinyl[3,2-c]pyridine_2-decylamine (Μ [2_(-methylamino)pyrimidin-5-sulfonyl]phenyl}indolyl)_1H_pyrazole [3,4-b]pyridine_5_carbamamine [(4 {[3-(morpholino)benzene]sulfonyl}]phenyl)methyl]thieno[2,3-c]pyridinecarboxamide Amine ((4 Π-(4-fluorophenylpyrazole_4_sulfonyl)phenyl}methyl)thieno[2,3-c]pyridinecarboxamide N [(4 methoxy: (three) Fluoromethyl)benzene] continued fluorenyl}phenyl)methyl]- 158436.doc •32· 201215609 1H♦ each [3,2 external ratio. _2 _ carbamide ({ [(4 ethoxy) ·3_Fluoro]sulfonyl]phenyl}methyl)_1H_D than oxazolidine [3'4 handsome bite _5_carbamamine (4 methyl ketone · 3 sulfonyl) phenyl] A Base}_1Η_π is more than [3,2_C] ° ratio. Demethylamine {[({3 [2·(morpholinyl)ethoxy]phenyl)sulfonyl)phenyl]methyl bromide and Π, 2 is called (4) _6_carbamamine ({ [(4fluoro-3-methoxyphenyl) sulfonyl] phenyl) decyl) imidazo[l,2-a] shouting _6_carbamamine {[(Benzenesulfonyl)phenyl]methyl}_3-(pyridine _2·基)-ΐΗ- &lt;·Bizozol-5-methanosamine-[(4-{[3-(5·indolyl·in-noise 2嗤))]]]]]]]]]]]]]]]]]]] 2,3-c]pyridine-2-carboxamide N-({4-[(3-fluoro-4-methylphenyl)sulfonyl]phenyl)methyl)furo[2,3·c] Pyridine-2-carboxamide N-{[4-(2-methyl_2H-indazole-5-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyrimidine-6-oxime Indoleamine N-{[4-(l,3m butyl)phenyl]methyl}indeno[2,3_c]d than pyridine-2-decylamine N_(4_(2d methoxy)phenyl Sulfonic acid base) Rice spit and Π, 2-a] ° ratio. N-{[4-(6-methylηpyrazine-2_sulfonyl)phenyl]fluorenyl} is deuterated and [2,3_c] 0 is 0--2- Amine Ν-({4-[(3·Ga-2-methoxybenzene) decyl]phenyl}methyl) miso and 158436.doc •33- 201215609 [l,2-a]pyrimidine- 6-Protonamine N-({4-[(4,5-difluoro-2-indolyl)sulfonyl]phenyl)indolyl)_1H_pyrrolo[3,2-c]pyridine-2 -Amidoxime·[(4_{[2-(decylamine sulfonyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-decylamine N-[(4-{[3-Fluoro-4-(methylthio))]]sulfonylhydrazinylphenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide N- ({4-[2-(3-Fluorophenyl)-1,3-thiazole_4_sulfonyl]phenyl}indolyl)furo[2,3-c]indole-2-yl Amine N_[(4-{[3-(2-methylpropoxy)benzene]] fluorenyl}phenyl)indenyl]thieno[2,3-c]pyridin-2-indole N-( {4-[5-(Trifluoromethyl)acridine_2_sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carbamimidoxime [[4-{ [4-(η-Byryl-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-carboxamide Ν·({4-[(3) -methoxy-4-mercaptophenyl)sulfonyl] Methyl imidazo[l,2-a]pyrimidine-6-carboxamide {·{[4-(phenylsulfonyl)phenyl]methyl bupyl-lH-n ratio [3, 2-c] 0-bite-2 -cartosamine N_({4-[(3-fluoro-4-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine 2-carbamimidin·{[4-(5·gas-3-methylpyridine-2-sulfonyl)phenyl]fluorenyl}furo[2,3-c]pyridine-2-carboxamidine Amine N-({4-[6-(trifluoromethyl)indolepyridin-2-sulfonic acid]phenyl}methyl)thiophene 158436.doc • 34- 201215609 [2,3-c]pyridine, 2_nonylamine N-[(4- / Γ9 fyt=. » , U^(ethoxymethyl)benzene]sulfonyl}phenyl)methyl]-1Η-α is 〇[3, 2'e]° ratio 2-carbalamine, ((4 [1-(3-Phenylphenyl)·ιΗ_η比azole_4_sulfonyl)])))imidazo[l,2 -a]pyridine_6_formamidine ({4'[(3-decyloxy_4_mercaptophenyl)sulfonic acid]phenylindolemethyl)furo[2,3~e]% pyridine_ 2_Metamine G4~U-(3-fluorophenyl)·13_thiazole_4_sulfonyl]phenylmercapto)imidazo[l,2-a]pyrimidine_6-formamide 4'{[3-(piperidinyl)-phenyl)phenylsulfonylphenyl)indolyl]imidazo[1'2-a]pyrimidine_6_ Indoleamine N-[(4-{[3-fluoro-5.(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2_a]pyrimidine_6_A Indoleamine N-({4-[5-(trifluoromethyl). Bisidine_3_sulfonyl]phenyl)indolyl)_1Η_〇Λoxazolo[3,4-b]pyridine-5-decylamine N &lt;{4_[(4-曱-oxyphenyl)sulfonyl]phenyl}indolyl)-1Η-«biazo[3,4-b]pyridine_5_carbamimidoxime ((4·[ (3-fluoro-2-indolyl)sulfonyl]phenyl}indolyl)_1H_pyrrolo[3,2-c]pyridine-2-carbamamine N-[(4-{[2-( Trifluoromethyl)phenyl]sulfonylhydrazinophenyl)indenyl]thieno[2,3-c]pyridine-2-indole N-{[4-(dimercapto-1,3.thiazole- 5-sulfonyl)phenyl]mercapto}imidazolium U,2-a]pyrimidine_6-carbamamine N_"4-[(3-chloro-4-propoxyphenyl)sulfonyl]phenyl丨曱基)米唾和158436.doc •35- 201215609 [l,2-a]pyridine·6_methalin Ν_({4·[(2,4-dioxa-3-methoxybenzene) sulfonate Mercapto]phenyl}methyl)furo[2'3-c].pyridin-2-indoleamine-5-fluorobenzene)sulfonyl]phenyl}indenyl)imidazo[i,2 -a] pyrimidine-6-formamide N-(4.(stylsulfonyl)benzyl)benzo[d]thiazole_5_formamide Ν_Π4-(porphyrin_3_sulfonyl)benzene Methyl hydrazinofuro[2,3_c]pyridine _ 2-carboxamide ν·({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}methyl)furan[2 ,3_c]bite-2-amidoxime _({4·[(3-fluoro-4_methoxybenzene)sulfonyl]phenyl}methyl Furando[2,3-c]pyridine-2-carbammine N_G4_[(4-chloro-2-indolylbenzene)sulfonyl]phenyl}methyl)imidazo[12·a] _Metamine "4 [(4~ethoxy-3-fluorobenzene) sulfonyl] phenyl] decyl) imidazo[1'2-a] pyrimidine · 6-formamide [(U3-( 2,2,2-difluoroethoxy)phenyl]sulfonyl}phenyl]mercapto]mizozolo[l,2-a]pyrimidine_6-carbamamine {[4 (2H-1, 3. Stupid and dioxolane_5_sulfonyl)phenyl]methyl}imidazo-Ha]pyrimidine_6•carbamamine {[4 (2H-1,3-benzodioxole)乙妇_4_醯醯)phenyl]methyl}imidazo[l,2_a]pyridine_6_decylamine {[4 (6·methyl 吼 _ _ 3- 醯 )) phenyl] A Keb m "Bizozolo[3,4-b]» than bite_5_carbamamine 158436.doc * 36 - 201215609 N-({4-[(5-T-butyl-2-methoxy) Benzene sulfonyl]phenyl}methyl&gt;1Η-&quot;Birdo[3,2-c]pyridine_2-formamide N-[(4-{[3-(i-sulfonyl) Benzene] continued fluorenyl}phenyl)indolyl]furo[2,3_c]pyridin-2-decylamine N-({4-[(4-decyloxy_3_methylphenyl))sulfonyl ]phenyl}methyl)thieno[2,3-c]pyridin-2-indole N-({4_[5-(. Bilo bite) bite small 醯 ]] phenyl hydrazine methyl) 吱 并 [2,3-c] pyridine-2-carbamamine N- ({4-[(3-gas-2-) Oxyphenyl)sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide N-({4-[(3-decyloxy-5-fluorenyl) stupid) Indeed, phenyl]phenyl)indolyl)imidazo[l,2-a]° ratio biting-6-cartoamine N-[(4-{[2-曱oxy-4-(trifluoromethyl)) Benzene]sulfonyl phenyl) thiol] thieno[2,3-c]pyridin-2-decylamine N-({4-[5-(trifluoromethyl) σ-pyridyl-2_sulfonate Mercapto]phenyl}methyl)imidazo[1,2-a]^--6-carbamamine N-[(4-{[3-(pyridin-2-yl)benzene]sulfonyl)丨Phenyl)hydrazino]imidazo[l,2-a]0 is more than 0--6-cartoamine N-({4-[(6-chloro-2-fluoro-3-methylbenzene)) (phenyl) fluorenyl [2,3-c]pyridine-2-carboxamide N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl) Thienyl) thieno[2,3_c]σ 唆-2-cartoamine]^-({4-[(3-amine hydrazino) sulfhydryl]phenyl}fluorenyl) thieno[ 2,3_ c]0 ratio. Benzene-2-carbamide 158436.doc •37·201215609 N-({4-[(5-Cyano-2-methoxy))sulfonyl]phenyl)methyl)imidazo[l,2 -a]pyridine-6-carboxamide 1^-[(4-{[4-fluoro-3_(2,2,2-trifluoroethoxy)]]]]]]]]]]] And [2,3-c]pyridine-2-carboxamide N-{[4-(1,3-thiazol-2-sulfonyl)phenyl]mercapto}imidazole and bite-6-cartoamine n_ ({4-[(3-Cyanobenzene) hydrazino]] phenyl}methyl)thieno[2,3-c]n*. N-[(4-{[3-(3,5-dimercapto-1H-pyrazole-i-yl)benzene]sulfonyl}phenyl)-methyl]imidazolium [l,2_a]pyrimidine-6-nonylamine N ({4-[(3-chlorophenyl) cans] base] fluorenyl)d-seno[2,3-c]0 ratio bite_ 2 -Metamine Ν_({4·[(2,6-dichlorobenzene)sulfonyl]phenyl}methyl)imidazo[12^]pyrimidine-6-carboxamide Ν[[4'{ [2 -Fluoro-4-(trifluoromethyl) phenyl] phenyl} phenyl) fluorenyl] oxazolo[l,2-a]. Bisidine_6_carbamamine N_"4·{[3-气-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazolium[1,2-a]pyrimidine_ 6_Metformamide N_U4-[(2·phenoxybenzene)sulfonyl]phenyl}indolyl]imidazo[u-a]pyrimidine-6-carboxamide N~{[4_(6-methyl °Bitazin-2-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyrimidinecarbamamine N-({4-[(2-methylphenyl)sulfonyl]phenyl} Methylpyrolo[3,2-c]. Ratio-2-carbamide 158436.doc •38- 201215609 N-({4-[(2 -milo-4·methoxybenzene) field 醢]]phenyl}fluorenyl) piroxi[3,2-c]pyridine-2-carboxamide N-[(4-{[2.methoxy-4_(1Η-°bizozol-1-yl) Benzene] hydrazino}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide N-({4-[(4-ethylphenyl)sulfonyl]phenyl}曱 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) [l,2-a]pyridine-6-carboxamide# Ν_[(4·{[3-(cyclopentylaminocarbamimidyl)benzene]sulfonyl}}))]]] 2,3-c]pyridine-2·decylamine 5-hydroxy-N-({4-[(4-phenylphenyl)sulfonyl]phenyl}methyl)_1H_吲哚_ 2-brew N-[(4-{[4-(TM-yl)-4-phenyl)sulfonyl}phenyl)indolyl]furo[2,3-indole]0 is determined to be 2-carboximine N -[(4-{[4-(ethoxyindolyl)benzene]sulfonyl}phenyl)methyl]imipid[l,2-a]pyrimidine-6-carboxamide N-({ 4-[(3-Gas-5-fluoro) 醯 ]]]phenyl}methyl) oxazolo[l,2-a]pyrimidine-6-carboxamide N_[(4-{[4-( Morpholine_4_yl)phenyl]sulfonyl}phenyl)methyl]imidazo[l,2-a]0 is more than 0--6-cartoamine N-({4-[(4-B) Oxymethylbenzene)sulfonyl]phenyl}methyl)-1H_n-pyrazolo[3,4-b]^bidine·5·carbamamine-({4-[(4-butoxy) __3_气苯)sulfonyl]phenyl}methyl)imidazo[l,2-a]0 than bite-6-cartoamine 158436.doc 39- 201215609 N-({4-[(4- Decanesulfonylbenzene)sulfonyl]phenyl}indenyl[3,2-c]pyridine-2-carboxamide N-[(4-{8-oxatricyclo[7.4.0.02,7] 13-carbon-1(13) 2,4,6,911_hexene-6-sulfonyl}phenyl)methyl]imidazo[i,2-a]pyrimidine-amide-{[4- (1Η-吲哚-7_Continued fluorenyl)phenyl]methyl}嗟-[2,3_c]0-pyridyl-2-carboxamide N-[(4-{[2-(ethoxy) Phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridyl 2-carbamamine N-{[4-(naphthalene-1-sulfonyl)phenyl]mercapto} imidazo[12 a] mouth bite formazan N-{ [4-(quinoline-3- Sulfhydryl)phenyl]methyl}thieno[2,3-e] D than 2-mercaptoamine N-({4-[(4-chloro-3-methoxybenzene)sulfonyl] Phenyl}methyl is more than oleno[3,4-b]pyridine-5-carboxamide N-{[4-(5-gas. Bipyridin-3-sulfonyl)phenyl]indolepyrolo[3 2 c]D than bit-2-cartoamine N-({4-[(3-fluoro-5-methylphenyl)) Mercapto]phenyl}methyl)-1Η-η than salido[3,4-b]pyridine-5-formamide N-({4-[(4-butylphenyl)sulfonyl)phenyl }methyl)_lH-«比比和[3,2_ c]0 than bite-2-cartoamine N-({4-[(2,6-dioxabenzene)sulfonyl]phenyl}methyl And [3,4-b]pyridine-5-carbamimidamine N-[(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)indolyl]-iH, 0 is more than [3,4-b]pyridine-5-decylamine 158436.doc -40- 201215609 N-({4-[(3-decyloxy-5-methylphenyl)sulfonyl]benzene Furyl [2,3-c]pyridine-2-carboxamide N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl Thio[], thieno[2,3-c].pyridin-2-carboxamide N-[(4-{[2-methoxy-5-(tri-L)oxy)benzene] Phenyl) fluorenyl]-1H-pyrrolo[3,2-c]acridin-2-carboxamide N-({4-[(4-fluoro-3-methoxyphenyl)sulfonyl) Phenyl}hydrazino)furo[2,3-c]pyridin-2-decylamine φ N-{[4-(morphothia-4-sulfonyl)phenyl]indolyl}imidazo[ 1,2-a]pyrimidine-6-formamide N-[(4-{[3-(4-fluorophenoxy)benzene] Mercapto}phenyl)indolyl]imidate[l,2-a]° than bite-6-nonylamine N-{[4-(quinolin-3-sulfonyl)phenyl]methyl} -1Η-pyrazolo[3,4-b]pyridine-5-carboxamide N-({4-[(5-Ga-2-methylphenyl)sulfonyl]phenyl}fluorenyl) furan [2,3-c]° ratio. 2-carbamide® N-[(4-{[4-methoxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl)indole Base] ° m ° sit and [1,2 - a] ° dense ° -6 -carbamamine N-[(4-{ [3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl) }phenyl)indolyl]furo[2,3-c]pyridin-2-indoleamine [(4-{[3-(5-mercapto-1,2,4-oxadiazole-3- Phenyl]sulfonyl}phenyl)indolyl]furo[2,3-c].pyridin-2-nonylamine N-({4-[(3-ethylmercaptophenyl)sulfonyl) Phenyl}methyl)thieno[2,3-c] D is more than 2-mercaptoamine 158436.doc -41 - 201215609 N-({4-[(4_butoxy-2-methyl) Benzene sulfonyl]phenyl}indolyl)furo[2,3-c]pyridine-2-carbamidine n-({4-[(2-butoxy-4-fluorobenzene)sulfonyl] Phenyl}methyl)imidazo[l,2-a]pyrimidine-6-nonylamine N_{[4-({3-[(propan-2-yl)aminoindolyl]phenyl}sulfonyl) Phenyl]fluorenyl} imidazo[l,2_a]pyrimidine_6_A Amine, K-fluoro-2-indolyl benzene) decyl]phenyl}indenyl) benzophenan [2,3-c]pyridine-2-carbamamine G4 [(3,4_dibenzene) Continuation of fluorenyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine_6-carboxamide^pyrazole_mercaptopyridine_3sulfonyl]phenylindenyl)imidazolium [l,2-a]pyridine_6•carbamamine N_G4~[(夂chloro-5-fluorophenyl)sulfonyl]phenyl}methyl)thieno[2,3_c] 0 than bite-2- Amine chloro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[,2-a].比 _6_ decylamine N-({4-[(4-ethoxyphenyl)sulfonyl]phenyl}fluorenyl)furo[2 3 c] φ 0 is D Amine [(2,3-dimethylphenyl) hydrazino]phenyl hydrazine methyl) taste spit and a] ° bite-6-formamide Ν &quot;4·[(3-chloro-4-methoxy Alkyl phenyl) continued fluorenyl]phenyl}methyl)_1H-indolo[3,2-c].比 _2 曱醢 曱醢 曱醢 _2 _2 _2 _2 _2 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 · 201215609 N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}indolyl)-1Η-ηpyrolo[3,2-c]pyridine-2-carboxamide N- ({4-[(2-Fluoro-6-propoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide N-({4- [2-(3-Fluorophenyl)-1,3-thiazole-4-sulfonyl]phenyl}methyl)-1H-pyrrolo[3,2-c]pyridine-2-carboxamide N- {[4-(Benzenesulfonyl)phenyl]methyl}-1Η-. More than [2,3-b]. Bibiidine-5-decylamine • Ν-{[4-(1-benzothiophen-7-sulfonyl)phenyl]fluorenyl}furo[2,3-c] ° ratio. N-({4-[(3-chloro-4-indolyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]a -Procarbamide N-({4-[(2-methoxyphenyl)sulfonyl]phenyl}indolyl)-1Η-indolo[3,2-c]pyridine-2-carboxamide N -({4-[(2-Ga-5-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]° ratio. 2-carbamamine_N-{[4-(6-methylpyrazine-2-sulfonyl)phenyl]methyl}-1Η·carbazolo[3,4-b]pyridine-5 - indoleamine N-({4-[2-(morpholin-4-yl)&quot;bipyridin-3-sulfonyl]phenyl}methyl)imidazo[1,2-&amp;] . -6-6-Amidoxime-[(4-{[4-(1-cyanocyclopentyl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2 -Proline N-({4-[(4,5-difluoro-2-indolyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-A醯amine 158436.doc • 43- 201215609 N-[(4-{[4-(ethylaminemethanyl)benzene; Isulfonyl}phenyl)methyl]imiindole[l,2-a] Pyridylcarbendazim N-{[4-(isoquinolin-4-ylsulfonyl)phenyl]methylimidazole and bite-6-carboxamide N-({4_[(3-dendene)sulfonate) ]]phenyl}methyl)-ΐΗ-α is more than [3,2-c] 0 than bite-2 - urethane N-{[4_(1-methyl-1H-1,3-benzo) Diazol-6-sulfonyl)phenyl]methyl} imi. Sit and [l,2-a]pyrimidine_6_carbamidine N-({4-[(2-ethyl))sulfonyl]phenyl}methyl)thieno[2 3_c]ii bite- 2-carbamidine N-({4-[(2-ethoxyphenyl)sulfonyl]phenyl}methyl)furo[2,3_q D ratio σ定-2 -甲甲胺Ν-({ 4-[(4-Fluoro-2,5·didecylbenzene) hydrazino]phenyl}methyl) scented [l,2-a]n than bitten-brown amine N_({4_[5- (°bipyridin-1-yl)&quot;bipyridin-3-ylindole]phenyl}methyl)_1H_ °piro[3,2-c]pyridinium N-{[4-( Phenylsulfonyl)phenyl]mercapto}-[1,2,4]triazolo[4,3-a]tadine-6-cartoamine Ν[[4-{[3-(5· Methyl], 2 4-oxadiazole _3_yl) benzene] 醯 } } 笨 笨 ) ) ) 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 咪唑 l l l l l l l l l l l l l l l l l l l l l 4-(Trifluoromethyl)pyridinium-2-sulfonyl]phenyl}methyl)thieno[2,3_c]° pyridine-2-carbamide Ν·({4-[6-( 3,4-difluorophenyl)β is more specific than 唆_2_ 醯 ] ]]phenyl}methyl)0 pheno[2'3-c].比 曱 曱 158 158436.doc 201215609 N-({4-[(3-ethoxyphenyl) hydrazinyl]phenyl}methyl)ufu-[2,3-c]pyridin-2-indole Amidoxime-({4·[(2-methoxy-5-methylphenyl))]phenyl}methyl)pyrano[2,3-c]pyridine-2-carboxamide N -({4-[(2,3-Dimethoxy-5-methylphenyl)sulfonyl]phenyl}methyl 111-0 is more than [3,2-〇]&quot; -Procarbamide N-[(4-{[3-fluoro-5-(»birolidin-1-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine -6-decylamine # N_({4-[(2,6-dimethoxy-4.methylbenzene)sulfonyl]phenyl}methyl 1H-pyrazolo[3,4-b] Pyridine-5-formamide N-{[4-(phenylsulfonyl)phenyl]indolyl}thieno[2,3-c]npyridin-2-carboxamide N-[(4-{ [4-(Ethylaminoindenyl)benzene]sulfonyl}phenyl)indenyl]1H_pyrrolo[3,2-c]pyridine-2-carboxamide N-[(4_{[3-( Methylamine fluorenyl) phenyl] hydrazino}phenyl)methyl] benzo[2,3-c]pyridin-2-indole ruth N_{[4_(5-fluoro-6-fluorenyl) Pyridine-2-sulfonyl)phenyl]fluorenyl}thieno[2,3_c]°tb°-2 - 曱-amine Ν-({4·[(6-chloro-2-fluoro_3_甲甲Benzosulfonyl]phenyl}indenyl)_1Η ^ 并[3,2-c] acridine-2-hydrazinium-({4·[(3-chloro-4-methylphenyl)sulfonyl]phenyl}fluorenyl)_1Η_〇 ratio [3,2-c]pyridine-2-carbamimidoxime-{[4-(2Η-1,3-benzodioxole-4-sulfonyl)phenyl] sulfhydryl} Imidazo[l,2-a]pyrimidine_6-carbamimid 158436.doc • 45· 201215609 N-[(4-./ ( u (°birolidin-1-yl)benzene]sulfonyl}benzene Alkyl imidazolium, Ν [(4'{[4-fluoro-2.(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thiophene [2,3 Specific bite-2·carbamamine Ν ί Γ 4 ^ wu isoquinoline-4-sulfonyl)phenyl]methyl}imidazo[u — a]glycine-6-formamide N-({4 '[(2,4,5-Trimethylphenyl)sulfonyl]phenyl}methyl)furo[2'3_C]° than bite 2-carbamide Ν_({4~[(2,4) -dimethyl-3-decyloxybenzene)sulfonyl]phenyl}methyl)imidazo[L2^]pyrimidine-6-carboxamide (Ε)-2·cyano_3-({4- [(5-Fluoro-2·decyloxyphenyl)amine sulfonyl]phenyl)indenyl) small (° ratio -4- base) 胍^ ([2 - gas - 3- (prop-2- Benzyl)benzene] continuation base}phenyl)methyl] sinter[2,3-c]pyridine_2-decylamine N_"4-[(4-methoxy-3-methyl) Sulfhydryl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6-carbamimidamine N-({4-[6-(trifluoromethyl)"pyridinyl-2_sulfonate Methyl)imidazo[l,2-a]pyrimidine_6_carbamimidoxime-[(4·{[4-methoxy-2-(trifluoromethyl)benzene]sulfonate Thio[2,3-c]pyridine-2-carboxamide-{[4-(1·methyl-1H-indazole-6-sulfonyl)phenyl] Methyl}mi-[i,2-a]pyrimidine-6-carbamimidoxime-({4·[2-(trifluoromethyl)) is sitting and [l,2-a] ° is bite- 6-Continuous]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 158436.doc -46- 201215609 N-[(4-{[3-(piperidine-1) -yl)phenyl]glycosyl}phenyl)methyl]_13_benzothiazole-6-nonylamine N-[(4-{[3-(piperidin-1-yl)benzene]sulfonyl) Imidyl]imidazo[l,2-a]pyrimidin-6-cartoamine N-({4-[(4-fluoro-2-methylphenyl)sulfonyl]phenyl}fluorenyl) ratio [3,2-c]pyridine-2-carboxamide N-[(4-{[3-fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}benzene Methyl]-1H-0 piroxi[3,2-c]0 than bite-2-cartoamine Φ N-{[4-(phenyldecane)sulfonylphenyl]fluorenyl} -lH-°tb-[3,2-c]pyridine-2-carboxamidine Amidoxime-({4-[(2·chloro-5-methoxyphenyl)sulfonyl]phenyl}fluorenylpyrrolo[3,2-c]pyridine-2-carbamimidoxime-[( 4-{[4-(1-Cyanocyclopentyl)benzene]sulfonyl}phenyl)indenyl]-1H. Bisolo[3,2-c]pyridine-2-carboxamide N-({4-[(4-ethoxyphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c Pyridine-2-carboxamide® N-{[4-(2-mercapto&quot;bipyridin-3-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyrimidine-6- Methionamine N-[(4-{[4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2 -carbamidine N-({4-[6-(3,4-difluorophenyl).pyridin-2-sulfonyl]phenyl}methyl)-1Η-°bizozolo[3,4 -b]pyridine-5-nonylamine N-[(4-{[2-fluoro-3-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]thieno[2,3- c] ° ratio.定-2-甲含胺158436.doc -47- 201215609 1^-[(4-{[2-methoxy-4-(trifluoromethyl)benzene] hydrazino}phenyl)indenyl]_ 1H-pyrazolo[3,4-b]pyridine-5-formamide N-({4-[(4-propoxyphenyl)sulfonyl]phenyl}methyl)furan[2,3_c Pyridine-2-carboxamide N-({4-[(4-methoxy-2,5-dimethylphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a] Pyrimidine-6-carbamamine&gt; 1-({4-[(5-Gas-2-oxooxybenzene)sulfonyl]phenyl}methyl)_111_0pyrho[3,2-c]pyridine 2-carbamidine N-[(4-{[2-mercapto-4-(trifluoromethyl)benzene]]] phenyl) fluorenyl] benzo[2,3-c]pyridine 2-carbamamine N-[(4-{[4-(trifluorodecyloxy)benzene]sulfonyl}phenyl)methyl^^^biazo[3,4-b]pyridine-5 - indoleamine N-({4-[(3,4-difluorophenyl)sulfonyl]phenyl}methyl)_1Η_β is more than [3,2-c]° than 唆-2- 曱 amine N-({4-[(3,5-monomethoxybenzene) continuation]phenyl}methyl)α-seceno[2,3-c]pyridine-2-carboxamide N-[( 4-{[4-chloro-2-(trifluoromethyl)benzene] fluorenyl}phenyl)methyl] ” pheno[2,3-c]pyridine-2-carboxamide N-{[ 4-(phenylsulfonyl)phenyl]methylthiazolo[5,4_c] Specific bite 2- 2-carboxamide N-({4-[5-(indolyl-1-yl)"pyridin-3-sulfonyl]phenyl)indolyl)imidate[l,2- a]pyridine-6-formamide N-[(4_{[2-methyl_4_(trifluoromethyl)benzene]] 醯 } 笨 笨 曱 ] ] ] ] ] 2 [2,3-c Pyridine-2-decylamine 158436.doc 48· 201215609 N-[(4-{[3-(3,5-dimercapto-1H-D is 0--1 base)] stupid] Styrene) methyl]-1Η-pyrazolo[3,4-b]pyridine-5-formamide N-[(4-{[3- gas-4-(trifluoromethyl)benzene]sulfonate }}phenyl)fluorenyl μ1Η_pyrrolo[3,2-c]pyridin-2-indoleamine·({4-[(2-chloro-4-methoxyphenyl)sulfonyl]phenyl} Methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-({4-[(3-a-5-methoxybenzene)sulfonyl]phenyl}methyl)imidazolium [l,2-a]pyrimidine-6-decylamine is N-{[4-(5-aza-3-mercaptopyridine-2·sulfonyl)phenyl]methyl}thiophene [2,3 -c]pyridine-2-carbamimidoxime [[4-{[2-(didecylaminoindolyl) phenyl]sulfonyl}phenyl)indolyl]furo[2,3-c] Pyridine-2-carboxamide N-[(4-{[4-(吼(小)))]]]]]]]]]]]]]]]]] And [3,4-b]pyridine-6-carbamidamine N-({4-[2-(pyrrolidinyl)-phenylpyrazine, %thiazole-5-sulfonyl]phenyl)indolyl) -1Η-pyrrolo[3,2-c]pyridine_2_decylamine _ Ν·[(4-{[4·(?琳_4_yl)benzene)] 醯 丨 phenyl) methyl p Deseno[2,3-c]pyridine-2-carbamamine N ({4-[(4-chloro-2-methoxybenzene)sulfonyl]phenyl}methyl)thiophene [2, 3-c]pyridine_2-formamide N [(4-{[2-methoxy-5-(trifluoromethoxy)benzene]sulfonyl)phenyl)indolyl]imidazo[l,2 -a]pyrimidine·6_carbamamine Ν·({4-[(4-methoxy-2-5_--methyl), —Τ basic) sulfonyl] phenyl] fluorenyl] furan [2,3 -c]pyridine-2-amine 158436.doc •49- 201215609 N-[(4-{[3-fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazole And [l,2-a]pyrimidine-6-formamide N-[(4-{[3-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]-1Η-η Bisazo[3,4-b]° ratio 5--5-nonylamine N-{[4-({4-[(.pyrrolidin-1-yl)carbonyl)phenyl)sulfonyl)phenyl Methyl} thieno[2,3-c]pyridine-2-carboxamide N-({4-[(2,4,6-tridecylbenzene)sulfonyl]phenyl}indolyl) furan And [2,3-c]pyridine-2- Formamide N-({4-[(2-Ga-5-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]. Bite-6-carbamamine N-[(4-{[2-(benzyloxy)-5-(trifluorofyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2 -a]pyrimidine-6-nonylamine]^-{[4-(6-methoxyacridin-2-sulfonyl)phenyl]methyl}imidazo[1,2-a]pyrimidine-6 -carbamidine N-[(4-{[2-methoxy-4-(1Η-°bizozolyl-1-yl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrrolo[3 , 2-c]pyridin-2-decylamine N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]-1H-. Bisazo[3,4-b]pyridine-5-nonylamine N-(l,3-benzothiazol-6-ylmethyl)-4-[(3-phenylene)sulfonyl]phenylhydrazine Indoleamine N-({4-[(2,4-dichloro-3-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-decylamine N-({4-[(4-ethoxy-3-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]pyridine-6-carboxamide N-({4 -[2-(Trifluoromethyl)imidazo[l,2-a]acridin-6-sulfonyl]benzene 158436.doc -50· 201215609 base} fluorenyl) 11 furan[2,3- c]Northern bite-2-nonylamine N-{[4-(.N. Ethyl.set-4-sulfonyl)phenyl]methyl}_1H_npyrho[3,2_c]pyridine-2-yl Amidoxime-({4-[1-(4-fluorophenyl)·ΐΗ-η-pyrazole-4-sulfonyl]phenyl}fluorenyl)_ 1Η-»比咯和[3,2-c Pyridine-2-carbamimidoxime-{[4-(1-methyl-1H-D-biazole-4-cyclosulfonyl)phenyl]methyl b 1H_„比比和[3,2-c] Pyridin-2-decylamine N_[(4-{[2-曱oxy_4-(ιή·.pyrazol-1-yl)benzene]sulfonyl)phenyl)methyl]-1Η-pyrazole And [3,4_b]pyridine·5_methylammonium chloride-5-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carbamidine cyclopentane Base amine) Mercapto]]imidazo[l,2-a]pyrimidine_6•carbamamine ([4 ({3-[2-(morpholine-4-yl)ethoxy]benzene) Mercapto)phenyl]methyl} lH-η is more than [3,2_c]. Bipyridylamine [4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl phenyl Mercapto] imidazo[l,2-a]pyridine-6-carbamamine, [(4 fluoro_3_(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thiophene [2, 3-c]°-pyridine-2-carboxamide N- {[4 ( λ 彳, fluorenyl-1 Η-carbazole _5_sulfonyl)phenyl] fluorenyl] furan [2,3-c Pyridine_2_carbamamine ({4[(2-fluoro-5-methoxybenzene)sulfonyl]phenylindolemethyl)furo[2,3-c]pyridine-2-carbamidine {[4 ({3-[(()))]]]]]]]]]]]]]]]]]]]]] Pyridine_5·carbamidine oxime-[(4-{[3-(bitter-2-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]carcinoma-6 - f-amine N-({4-[(2-fluoro-3-methylphenyl)sulfonyl]phenylindolemethyl)thieno[2,3_c]pyridine-2-carboxamide N-[ (4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]_1Η·pyrrolo[3,2-c]pyridin-2-indole N -({4-[(2,3-dimethylphenyl)sulfonyl]phenyl}indolyl)furo[2,3_c]pyridine-2-carboxamide-{[4-(1- Methyl-1H-carbazole-7-ylidene)phenyl]methyl}imidazo[l,2-a]°^bit-6-carbamamine N-({4-[(3-gas) -5-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]0 to 0--6-carbamamine N-({4-[(2-chloro-6) -decyloxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine·2·carbamamine\-({4-[(3,4-dimethoxybenzene)) Sulfhydryl]phenyl}indolyl)imidazo[l,2-a]°t bit-6-cartoamine N-({4-[(3,5-difluorophenyl)sulfonyl]phenyl }曱基)·ΐΗ-°Bizozolo[3,4-b]pyridine-5-carboxamide N-[(4-{[3-fluoro-4-(trifluoromethyl)benzene]sulfonyl) }phenyl)methyl]imidazo[l,2-a]°*bit 6-amidoxime-({4·[(4-Ga-2-methoxyphenyl)sulfonyl]phenyl }Methyl)furo[2,3-c]pyridine-2-carboxamide N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η -吼 并 158436.doc -52- 201215609 [3,2-c]pyridine-2-carboxamide N-({4-[(2-chloro-4-decyloxybenzene)sulfonyl]phenyl }Methyl)thieno[2,3-c]pyridine-2-f decylamine N-{[4-(phenylsulfonate) Phenyl; 1 fluorenyl}-5-(acridin-3-yl)-1Η-η than 唆3-carbamamine N-({4-[(4-butylphenyl)sulfonyl]phenyl }Methyl)carbazole[12]L-pyridyl-6-carboxamide N-({4-[(3-chlorophenyl) fluorenyl)phenyl}methyl) oxazole and n,2_a]嚷6 -Procarbamide N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]furo[2 c]pyridin-2-decylamine N-[( 4-{[3-(4-Fluorophenoxy)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine-2-carboxamide N-[(4-{[ 5-Gas-2-(2,2-difluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridin-2-indoleamine· { [4-(Quinolin-6-sulfonyl)phenyl]methyl}thieno[2,3 c]pyridine_ 2-carboxamide N-[(4-{[3-(»辰咬- 1-yl)benzene] 醯 醯 } 笨 笨 ) ) ) 甲基 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 Oxylbenzene) 酼 ] ] 笨 ] 笨 笨 笨 笨 笨 笨 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 .〇2,7]trideca]hexene-6-sulfonyl}phenyl)indolyl]imidazolium n,2_a]pyrimidine-6-carbamamine N-({4-[(4-butoxy) Stupid) sulfonyl] stupid} methyl) thieno[2,3_c] 1584 36.doc •53·201215609 Pyridine-2-carboxamide N-({4-[5-(trifluoromethylpyridyl_3_sulfonyl)phenyl}methyl)imidazo[1,2- a]pyridine-6-formamide N-[(4-{[4-(propan-2-yloxy)benzene]sulfonyl phenyl)phenyl]furan[2,3-c]pyridine 2-carbamimidoxime-{[4-(5.methoxy).比 _2 _ _ _ _2 _2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 ( ( ( ( ( ( ( ( ( ( ( ( ( ( Phenyl}methyl)imidazo[a]pyrimidine-6-carboxamide N-({4-[(2-ethylmercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3_c] Roar. N-({4-[(4-ethylmercaptophenyl)sulfonyl]phenyl)indolyl)thieno[2,3e] ° ratio σ定-2 - 曱 Ν -({4-[(2-Ethylphenyl)sulfonyl]phenyl}indolyl)imidazo[12 a]pyrimidine-6-nonylamine N-[(4-{[3-(3, 5-dimethyl-1H·»bizozol-1-yl)benzene]sulfonyl hydrazino) methyl]imidazo[l,2-a]pyridine-6-carboxamide 1^-({4 -[(2_Gas_5-methylphenyl)sulfonyl]phenylindolemethyl)furo[2,3_c]. Than 2-carbamide, N_[(4-{[4-chloro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazolyl,H,2-a]pyrimidine 6_decylamine methoxy_5·methylbenzene)sulfonyl]phenyl[1,2,6·carbamamine^ &amp;«^[(3-stylbenzene)sulfonyl]benzene } 甲基 甲基 并 ” ” 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 158 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯 曱醯} imidazo[l,2-a] 0 ratio. -6-decylamine N-[(4-{[4-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl] Imidazo[1,2 - a]α dense. -6-carbamamine 1^-({4-[1-(3-phenylphenyl)-111-.pyrazole-4-sulfonyl]benzene曱 曱 ))-1Η-pyrrolo[3,2-c]pyridin-2-decylamine N-[(4-{[3- gas-5-(hydroxyindenyl)benzene]sulfonyl}benzene Methyl]thiophene φ and [2,3-c]pyridin-2-decylamine N-({4-[(4-fluoro-2-indolyl)sulfonyl]phenyl}methyl) Imidazo[1,2-a] ππ定-6-甲甲胺Ν-({4-[(4-ethoxy-2-methylphenyl)sulfonyl]phenyl}indenyl)thiophene [2,3-c]pyridine-2-carboxamide N-[(4-{[4-(ethylamine)methyl)benzene]sulfonyl}phenyl)indolyl]thieno[2,3 -c]pyridine-2-a Indoleamine N-[(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)indolyl]-1Η-° ratio 并[3,2-c]pyridine-2 -carbamidine N-({4-[(3-chloro-4-mercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]. N-[(4-{[2-(Dimethylaminoindenyl)benzene]sulfonyl}phenyl)methyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide N-{[4-(phenylsulfonyl)phenyl]indolyl}-5-indolepyridin-3-yl)-1,2,4-oxadiazole-3-carboxamide 5-hydroxy-N -[(4-{[3-(piperidin-1-yl)benzene]sulfonyl}phenyl)indolyl]- 158436.doc -55- 201215609 lH-called 卜多_2·甲牛胺Ν^ (4_{[3-(Didecylaminesulfonyl)benzene]sulfonyl}phenyl)methyl]imidazolium U,2-a]pyrimidinecarbamamine N^[4_(2,3-dihydrogen) -1-benzofuran-7-sulfonyl)phenyl]fluorenyl}imidazolium U,2-a]pyridine_6_ amidoxime {{{4·(6-methylpyridine-3-sulfonate) Phenyl]methyl}imidazo[l,2-a]pyrimidine-6-carboxamide N_[(4-{[2-methoxy-5-(propan-2-yl)benzene]sulfonyl) }phenyl)methyl]_ 1H_°pyrho[3,2-c]pyridine-2-carbamimidoxime·({4-[6-(didecylamino)pyridine_3_sulfonyl) Phenyl}methyl)furan[2,3- c]pyridine 2-indole N-[(4-{[2-(trifluoromethoxy)benzene]sulfinyl}}phenyl)indolyl]_1H_ 0 piroxi[3,2-c Acridine-2-carboxamide N ({4-[(3,5-fluorobenzene) cans]phenyl}indenyl)D-depheno[2,3_c]pyridine-2-carboxamide Ν·({4-[(4-chloro-3-fluorophenyl)sulfonyl]phenyl}methyl) thieno[2,3_c] ° than bit-2-cartoamine N-({4-[ (2,4,5-trimethylbenzene)sulfonyl]phenyl)methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-({4-[(2,4-) Dimethylbenzene)sulfonyl]phenyl}methyl)furo[2,3_c]° than pyridine-2-carboxamide Ν[[4-{[2- gas-3-(trifluoromethyl) Benzene] 醯 醯 } } 苯基 } } } } 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 [(4-{[3-(3,5- dimethyl-- Benzene] phenyl] fluorenyl} phenyl) 158436.doc 201215609 methyl]· 1 Η-.比比和[3,2 外比〇定·2·甲胺胺Ν-({4-[(2-Ga-4-methyl))sulfonyl]phenyl}methyl)furan[23_ c ]Dit bit-2-nonylamine N-({4-[(4-fluoro-3-indolyl))sulfonyl]phenyl)indolyl)_1H_indole-[3,2c] ° ratio bite-2 _ 甲甲胺Ν-({4-[1-(propan-2-yl azole-4-ylsulfonyl)phenyl}methyl)imidazo[l,2-a]pyridine-6 -Metamine Ν-[(4-{[3·(Difluoromethoxy)benzene]sulfonyl phenyl)methyl]furo[2,3-c]pyridin-2-decylamine N -[(4-{[2-decyloxy-6-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]-1Η-»比咯和[3,2-c] Pyridine-2-formamide N-({4-[(4-chloro-3-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-玨]° ratio bite-6 - indoleamine N-({4-[(2,3-dimethylphenyl)sulfonyl]phenylindolemethyl)thieno[23·c]pyridin-2-carboxamide N-( {4-[(5-Tertibutyl-2-methoxybenzene)sulfonyl;jphenyl}indolyl)furo[2,3-c]pyridine-2-carboxamide N-({ 4-[(4-methoxy-2-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyrimidin-6-carboxamide 1^-({4-[ (2,5-dimethylphenyl)sulfonyl]phenyl}methyl) Phenomenon [2,3_c]. 0-but-2-cartoamine N-({4-[(2-fluoro-5-methylphenyl)sulfonyl]phenyl}methyl)_1H^bazole And [3,4-b]pyridine-5-nonylamine N-[(4-{[2-chloro-5-(hydroxyindenyl)benzene]sulfonyl}phenyl)methyl]· 158436.doc -57- 201215609 Pyrrolo[3,2-c]pyridine-2-carboxamide N-({4-[(4-fluoro-2,5-dimercaptophenyl)sulfonyl]phenyl) ) bromo and [3,2-c]pyridine-2-carboxamide N-({4_[(4-butoxy-3-fluorobenzene) fluorenyl]phenyl}methyl) 2,3-c]pyridine-2-carboxamide N-({4-[(2-fluoro-5-foxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a Pyrimidine-6-formamide N-[(4-{[2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]furo[2,3 · c] ° ratio - 2 _cartoamine N-[(4-{[5-chloro-2-(2,2-difluoroethoxy)benzene]sulfonyl}phenyl)methyl]0 m 0 并 [1, 2-a]0 than bite-6-formamide N-({4-[(2-butoxy-5-gasbenzene)sulfonyl]phenylmercapto) imidazo[l,2-a ]n ratio bite-6-methionine [[4-{[2- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]_1{1_pyrrolo[3,2 -c]pyridine-2-carbamide N-({4-[(2-chloro-3--fluorobenzene)) Mercapto]phenyl}methyl)pyrano[2,3_c]pyridine-2-carboxamide N-[(4-{[3-(^b-habit-1-yl)benzene]-carsonyl}benzene Methyl]α-depheno[2,3-c]pyridine-2-carboxamide N-[(4-{ [3-fluoro-5-(2-methylpropoxy)benzene] 醯Benzyl)methyl]imidazo[l,2-a]pyridine-6-carboxamide N-({4-[(2-fluoro-5-methoxyphenyl)sulfonyl]phenyl} Methyl)-ex-^piro[3,2-c]pyridine-2-carboxamide N-({4-[(3-chloro-4-propoxyphenyl)sulfonyl]phenyl} Methyl)thiophene 158436.doc -58 - 201215609 [2,3-c]pyridine-2-carboxamide N-[(4-{[2,4-bis(trifluoromethyl)benzene]sulfonyl) }phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide N_({4-[(4-propoxyphenyl)sulfonyl]phenyl}methyl)imidazo[ Iha] pyrimidine-6-formamide N-({4-[(2-ethoxyphenyl)sulfonyl]phenyl}indolyl)thieno[2,3_c]pyridine-2-carboxamide N-({4-[(3-Phenylphenyl)sulfonyl]phenyl}methyl)thieno[2,3c]. Bipyridine-2-carboxamide N [(4-{[2-曱oxy·4_(1Η·β比嗤·)))]]]))))))]]]]]]]]] -a]pyrimidine_6_carbamamine N [(4 {[2-methoxy-3-(3-trifluoromethyl)benzene]]] phenyl)methyl] thieno[2,3-c] Pyridin-2-indole N-({4-[(4-fluoromethylphenyl)sulfonyl]phenyl}methyl)_ιη·π-pyrolo[3,2-c]n-pyridin-2 - indoleamine N-({4-[(2-ethane)-4-fluorobenzene)sulfonyl]phenylmercapto)imidazo[l,2-a]-pyridin-6-carboxamide Ν_{[4·(isoquinole·4_ 醯 )) phenyl]methyl}. Fusino[2,3-c]nh π定-2-甲手胺Ν_[(Μ[2-气-5_(三乱曱基)benzene] continued 醯}}))) [2,3- c] mouth bite 4 meglumine. soil] husband 0 South N-[(4-{[5-(diethylaminoindolyl)_2_fluorobenzene]sulfonyl]W each [Ο♦ The final product is a N-({4_[(2-)-fluorophenyl)sulfonyl]phenyl]methyl)-ιη- 吨 158436.doc -59· 201215609 [3,2-c ]»Bite 2-carbamide Ν·({4-[(3-chloro-2-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[^2-a]pyrimidine-6- Methionine N-({4-[2-(.pyrrolidin-1-yl)-indole, 3·thiazole_5_sulfonyl]phenylindolemethyl)imidazo[l,2_a]pyrimidine- 6-Protonamine N-[(4-{5H,6H,7H,8H,9H-flavored) sits and [12_a]azepine_3_determininyl)phenyl)methyl]°follow[2 ,3-c]〇比咬-2- anhydroamine N-({4-[(4-butoxyphenyl)sulfonyl]phenyl}indolyl)furo[2,3 c]pyridine-2 - indoleamine N-({4-[(3,5-dimercaptophenyl)sulfonyl]phenyl)methyl)imidazo[it a]pyrimidin-6-carboxamide N-({4- [(5-Gas-2-methylphenyl)sulfonyl]phenylindenyl)imidazo[a]-mouth bite-6-cartoamine-[(4·{[3-fluoro-4-(曱) Thiophenyl)benzene Sulfhydryl phenyl) fluorenyl] furo[2,3-c]pyridin-2-decylamine N-({4-[(4-fluoro-3-indolylbenzene)sulfonyl]benzene Imidazolyl[it a] mouth bite-6-cartoamine N-({4-[(3-t-butylphenyl)sulfonyl]phenyl}indolyl)furan [2, 3_c]° than 2-mercaptoamine N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl phenyl)indolyl] , 2-a]0 to 0--6-amidoxime·({4-[(5-t-butyl-2-methoxyphenyl)sulfonyl]phenyl}indenyl)·1Η- Pyrazolo[3,4-b]pyridine-5-carboxamide N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonyl phenyl)methyl]imidazole 158436.doc •60· 201215609 and [l,2-a]pyridine-6-formamide N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}methyl Thieno[2,3-c]pyridine-2-carboxamide N-({4-[(3-fluoro-2-indolyl)sulfonyl]phenyl}indolyl)imidazo[[beta]- α]'3 ratio. Ding-6- amidoxime-({4-[(4-butoxy-3-fluorobenzene)sulfonyl]phenyl}methyl)imidazo[1,2 - a] bite-6 - N-({4-[(3-methoxy-4-methylphenyl)sulfonyl]phenyl}indolyl)-111-. Bisolo[3,2-c]pyridin-2-decylamine N-({4-[5-(°-pyrrolidin-1-yl))pyridin-3-sulfonyl]phenyl}indole -1,3-benzothiazol-6-nonylamine N-{[4-(5-fluoro-6-fluorenyl)pyridin-2-sulfonyl)phenyl]fluorenyl}furan[ 2,3-c]pyridin-2-decylamine N-{[4-(morphothia-4-sulfonyl)phenyl]indolyl}furo[2,3-c]. Bisidine-2-decylamine N-({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a] sigma-6- Amidoxime-[(4-{[2-mercapto-4-(111-°bizozol-1-yl)benzene]sulfonyl}phenyl)indolyl]-1Η-吼 并[3, 2-c]pyridin-2-decylamine N-({4-[(3-chloro-5-decyloxybenzene)sulfonyl]]phenyl}indenyl)-1Η-. Bisazo[3,4-b]pyridine-5-carbamimidamine N-[(4-{[2-(nonyl)sulfonyl)benzene]sulfonyl}phenyl)methyl]-1H- Pyrrolo[3,2-c]pyridine-2-carboxamide N-({4-[(4-methylphenyl)sulfonyl]phenyl}methylpyrrolo[3,2- 158436.doc •61 - 201215609 c]pyridine-2-carboxamide N-({4-[(3-propoxyphenyl)sulfonyl]phenyl}methyl)_1Η_βpiro[3,2-c]pyridine 2-carboxamide N-[(4-{[2-(methylaminesulfonyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-methyl Indoleamine &gt; 1-({4-[4-(dimethylmethyl) 11 to 1) _2 _ 醯 ] phenyl] methyl} methyl) imixo[l,2-a]pyrimidine-6 -Procarbamide N-({4-[(4-ethoxyphenyl)sulfonyl]phenyl}indolyl)_1H_indolozolo[3,4-b]pyridine-5-carbamimidoxime- ({4·[(3-fluoro-2-methoxybenzene)sulfonyl]phenyl}indolylbi[3,2-c]pyridine-2-carboxamide-[(4-{ [4-(1-Cyanocyclopentyl)benzene]sulfonyl}phenyl)indolyl]-sodium [l,2-a]pyridine-6-nonylamine N-[(4-{[2 -methoxy-4-(trifluoromethyl)benzene]nonyl}phenyl)methyl]- 1H-pyrrolo[3,2-c]pyridin-2-indole N-{[4- (dimercapto-1,3-thiazol-5-sulfonyl) Thio[2,3-c]pyridine-2-carboxamide N-[(4-{[4-(hydroxyindenyl)benzene]sulfonyl}phenyl)indolyl]furan [2,3-c]pyridine-2-carboxamide N-({4-[(4-cyclohexyl))sulfonyl]phenyl}methyl)imidazo[i,2_a] 0 ratio bite-6 -methamidoxime-[(4-{6-azamidazo[l,2-a]&quot;bipyridin-3-sulfonyl}phenyl)indolyl]-1H-pyrrolo[3,2- c]pyridine-2·decylamine N-[(4-{[3-(piperidin-1-yl)]]sulfonyl]phenyl)indolyl]imipine 158436.doc •62· 201215609 [ 1,2-a]pyridine-6-formamide N-{[4-({4-[2-(didecylamino)ethyl]benzene}sulfonyl)phenyl]indolyl}imidazole [l,2-a]pyridine-6-formamide N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a Pyrimidine -6-carbamamine N-{[4-(phenylsulfonyl)phenyl]methyl}quinazolin-6-nonylamine N-[(4-{[4-fluoro-3-( 2,2,2-Trifluoroethoxy)benzene]sulfonyl}phenyl)methylpyrrolo[3,2-c]pyridin-2-indoleamine N-[(4-{[3- (°Byryl-1-yl)benzene]sulfonyl}phenyl)indenyl]-1,3-benzothiazol-6-carboxamide N'({4-[(3,5-dimethyl) Benzene)sulfonyl]phenyl}indenyl)-1Η-carbazole And [3,4-b]pyridine_5_formamide 1^({4-[(3- gas-4-mercaptophenyl)sulfonyl]phenyl}indolyl)-111-«-pyrazole [3'4-b]pyridine_5-carbamimidoxime [[4-{[4-(1Η-»bisazol-1-yl)benzene]sulfonyl}phenyl)indolyl]-1H- . And [3,4-b]pyridine-5-formamide N-({4-[(4-butoxy-3-oxabenzene)sulfonyl]phenyl}fluorenyl) furan [ 2,3-c]pyridine_2_ amidoxime·(Η-[(4-fluorophenyl))]phenyl}methyl-senteno[2,3-c]acridin-2-indole Amines N~{[4-({3-[(propan-2-yl))indolyl]phenyl}sulfonyl)phenyl]indolyl}imidazo-H,2-a]pyridine-6-oxime Indole N~({4-[(2,4-dioxaphenyl)sulfonyl]phenyl}indenyl)_1H_indolozolo[3,4-b]pyridine-5-f-decylamine 158436.doc -63 - 201215609 N-({4-[(2,3-Didecyloxy-5-methylphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c]0 N-[(4-{[2-fluoro-3-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2- a]pyridine-6-carbamimidoxime-({4.[6-(morpholin-4-yl)pyridine-3-sulfonyl]phenyl}indolyl)thieno[2,3-(:] 〇 ° 定 -2- 醯 醯 醯 醯 醯 -[(4-{[3-(&quot;Byrrolidin-1-yl)benzene]sulfonyl}phenyl)indolyl]-1Η-. [3,4-b]pyridine-5-formamide N-{[4-(5-foxyacridin-2-sulfonyl)phenyl]fluorenyl}thieno[2,3_c]pyridine-2 - indoleamine N-({4-[(3-chloro-2-fluorobenzene) hydrazino]benzene } 甲基 甲基 甲基 i [i, 2-a] pyrimidine-6-formamide N-[(4-{[5-hydroxy-2-(trifluoromethoxy)benzene]sulfonyl} Phenyl)methyl]furo[2,3-c]pyridin-2-decylamine n-({4-[(3,4-dimethylphenyl)sulfonyl]phenyl}methyl)thiophene [2,3_c]pyridine-2-carboxamide N-[(4-{[4-chloro-3-(trifluoromethyl)benzene]sulfonyl)phenyl)methyl]_1H_ 0 ratio [3,2-c]pyridin-2-decylamine N_[(4-{[3-(morphin-4-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2- a] pyrimidine-6-formamide N-({4-[(2-butoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)_1H_吼/[3,2-c] Acridine-2-decylamine N ({4-[(4-propoxy))phenyl}methyl)D-sentylpyridine-2-carboxamide 158436.doc 201215609 N -( 4-曱 醯 醯 醯 phenyl) imidazopyridine _6 formazan 1 ^ - ({4-[(3'4-dimercaptobenzene) hydrazino]] phenyl] fluorenyl) [3,4-b]0 than bite-5-formamide N-{[4-(isoquinolin-4-ylsulfonyl)phenyl]fluorenyl}·1Η_η-pyrazolo[3 4_b] 0 ratio Bite-5-cartoamine N_({4-[(2,6-dimethylphenyl)sulfonyl]phenyl}indolyl)furo[2,3_c]pyridine-2-carboxamide N- ({4-[( 4-decyloxy_35_dimercaptophenyl)sulfonyl]phenyl)indenyl)_ 1H-.略略和[3,2_c]pyridine_2_decylamine N_{[4-(cyclosulfonyl)phenyl]indolyl}_[1 2 3 4]tetrazolo[15_ 〇 〇 啶 - 6-Protonamine N_({4-[(4-cyanobenzo)sulfonyl]phenyl}indolyl)imidazo[J]pyridin-6-cartoamine Ν{{4-({3- [(propan-2-yl)aminoindenyl]phenyl}sulfonyl)phenyl]fluorenyl} 0 furano[2,3-c]° than bit-2-amine Ν&lt;(4· [(2,4-Dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[Ua] shoutin-6-carbamidamine·({4-[(4-butoxy-3-) Fluorobenzene)sulfonyl]phenyl}indolyl)-1Η-pyrrolo[3,2-c]pyridinium-2-carbamidine N_{[4~(4-mercapto-pyridin-3- Sulfhydryl)phenyl]fluorenyl}thieno[2,3-c] ° ratio of 2-carbamide N-[(M[2-(trifluoromethoxy)benzene]] Phenyl)methyl]_1Η_% oxo[3,2-c]pyridine_2· amidoxime·({4-[(4-ethoxyphenyl)sulfonyl]phenyl}methyl)imidazole And n,2_a] 158436.doc -65- 201215609 Pyrimidinecardamate N_[(4~U4-(2-methylpropoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2 -a]pyrimidine-6-nonylamine N_({4_[(3-chloro-2-indolyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-methyl Guanidine methyl-1H-indazole-4-sulfonyl)phenyl]methyl}thieno[2,3-c]. Bisidine, 2-carbamamine ^4~[(4-Ga-3-indolylbenzene)sulfonyl]phenyl}methyl)imidazolium '2 a]pyrimidine_6_methalamine cyanobenzene)sulfonyl]phenyl }Methyl)_1H-pyrrolo[3,2-C]pyridinium oxime-{[4-(2 ·3 _ « , V dihydro-1-benzofuran-7-sulfonyl)phenyl Imidazole, ['2 a] shouting -6-formamide N-(|4-ff: f dimethylamino)pyridine-3-sulfonyl]phenyl}methyl)- 1H- than sitting and [3,4'b]° bite 5--nonylamine N-(|4-fr-3 ^ U fluorobenzene)sulfonyl]phenyl}methyl)imidazo[1, 2-a]pyrimidine-6-decylamine n~({4-[(2 #: c U methoxyphenyl) sulfonyl]phenyl}methyl)imidazo[1'2♦ than pyridine + amide Ν' ((4-[(4) .γ ^ LV hexyloxy-2-methylbenzene)sulfonyl]phenyl}fluorenyl)furan L2,3-c]pyridinium 2·cartoamine {[2~(oxy)benzene] Sulfhydryl phenyl) fluorenyl]_m_n pyrrolo[3,2-c]pyridinium-2-carbamamine•ethyl keto-2-oxooxybenzene)sulfonyl]phenyl}methyl) Furan 158436.doc -66· 201215609 and [2,3-c]bidine·2_methalin Ν_({4-[κ(3_气phenyl)_1Η_Π比唑_4_sulfonyl] }曱基)米°[1,2-a]pyrimidine_6_ amidoxime·[(4-{[4- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl )methyl]furo[2,3-c]pyridine_2_formamide Ν_({4·[(2-butoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)thiophene [2,3-c]pyridine·2_ amidoxime [[[4-{[2-methoxy_5_(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]-1Η- η 唑 并[3,4_b]pyridine·5_ amidoxime-[(4-{2-[ethyl(indolyl)amino]-U·thiazole_5_sulfonyl}phenyl) 曱Imidazo[l,2-a]pyridin-6-nonylamine N-({4-[(4-ethylphenyl))] Base}methyl) miso and [12 a] squeak-6-cartoamine N_({4-[(4-gas-3-methoxybenzene)sulfonyl]phenyl}methyl)_1Η_η ratio [3,2-c]pyridine-2-carboxamide N_({4-[(2-a-5-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2 -a] Pyrimidine-6-nonylamine N ({4-[5-(di- gas fluorenyl) η is more than π _2 _ _ _ _ phenyl) thiol). And [l,2-a]pyridine-6-nonylamine N-{[4-(5-fluoroacridin-3-sulfonyl)phenyl]methyl}thieno[2,3_c]d ratio Pyridyl-2-carboxamide N-{[4-(phenylsulfonyl)phenyl]methyl}thieno[2,3_b]e than azine-6-carbamamine N-({4-[5- (trifluoromethyl)pyridine_2_sulfonyl]phenyl}methyl)furo[2,3-c]pyridin-2-ylamine 158436.doc -67- 201215609 N-({4-[ (2-butoxy-5-chlorobenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-f-decylamine N-[(4-{2-[ethyl (Meth)amino]4,3-thiazole·5_sulfonyl}phenyl)methylJ imidazo[l,2-a]pyrimidine-6-carboxamide N-[(4-{[2 -gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidin-6-carboxamide N_{[4-(quinoline-6 Sulfosyl)phenyl]fluorenyl}imidazo[12a]pyrimidine, 6-formamide N-({4-[(3-ethoxy-2)fluorobenzene)sulfonyl]phenyl}anthracene Base)_1H_Dtt嚷[3,2 - c ]0 than bite-2 - an amine N-[(4-{[2-(morpholin-4-ylmethyl)benzene]sulfonyl}phenyl) Methyl]_1H pyrrolo[3,2-c]pyridin-2-decylamine n-({4_[(4-methoxy benzhydrin))]phenyl}methyl)_1H^ p Each [3,2-c]n ratio 2-nonylamine N-({4-[(3-fluoro-4.methoxybenzene) hydrazino]phenyl}indolyl) fluorenyl[2,3-c]pyridin-2-indole Indole ν·{[4-(5-methyl acridine fluorenyl)phenyl]methyl}thiophene u, 3 is the ratio. -2--2-甲胺胺Ν-{[4-(2,3-dihydro-1-benzopyran-7-continuation) stupyl] fluorenyl 0-pyrazole [3,4-b] Pyridine-5-amidoxime [[4-{6-azamidazo[l,2-a]pyridin-3-sulfonyl}phenyl)methyl]furan[2,3 &lt;]° ratio π定-2-甲含胺Ν-[(4-{[3-(propyl -1- 醯 醯 )))]]] [l,2-a]pyrimidine_6-formamide 158436.doc -68 - 201215609 Ν-({4·[(3-曱 oxyphenyl) decyl]phenyl fluorenyl)_1Η_η azole [3,4-b]»Bipyridine-5-carbamidamine&gt;1-({4-[(3-fluoro-4-methylphenyl)sulfonyl)]phenyl}methyl)_1_11 Bisolo[3,2-c]pyridine-2-T decylamine N-({4-[(4-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3_c]t^ Acridine-2_carbamamine N-({4-[(4-chloro-3-methoxybenzene)sulfonyl]phenyl)phenyl)thieno[2,3-c]pyridine-2-yl Indoleamine • N-{[4-({3-[2-(didecylamino)ethoxy]phenyl}sulfonyl)phenyl]indolyl}pyrano[2,3-c]« N-{[4-(2-mercapto-2H-indole. sitting-6-continuation) phenyl] fluorenyl ih-吼〇 each [3,2-c Pyridine-2-f decylamine N-[(4-{[3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2- a]pyridine-6-formamide N-[(4-{[3-(cyclopentylaminomethyl)phenyl]sulfonyl}phenyl)indolyl]isoxazo[l,2-a] Pyridine-6-nonylamine • N-[(4-{[4-fluoro-3-(three) Fluorofluorenyl) phenyl] hydrazino}phenyl)methyl]_ih_ &quot; than 0 each and [3,2-c]0 is more than 2-mercaptoamine (·({4-[(2 -cyanide) Benzene) 醯 ]]]phenyl}methyl)imidazo[i,2_a]n than pyridine-6-formamide N-({4-[(2,4-dimethylphenyl)sulfonyl) ] stupid}methyl)·1Η_0 嘻[3,2-c]pyridin-2-decylamine N-{[4-(5-methylheptan-3-sulfonyl)phenyl]- Imidazopyridine-6-methanamine 158436.doc -69· 201215609 ,[(([2chloro-5-(difluoroindolyl)]]]]]]]]]]]]]]]]]] ,2-a]pyrimidinecarbamamine [({[2chloro~4-(difluoroindolyl)benzene]sulfonyl}phenyl)indolyl 1H_ 吼略[3,2 外比 bit|甲醯Amine [(3-chloro-5·!^) 醯 ]]]phenyl} fluorenyl) 吱 并 [2,3_e] ° ratio 0 -2- ketoamine N [(4-{[3-( ° ratio is slightly -1 · base) stupid] 醯 }}} phenyl) fluorenyl] 吱 并 [2,3-c] pyridine 2 _ carbamide N [(4_{[3-(difluoro Methoxy)phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carbamide N ({4-[(2-ethylmercaptophenyl)sulfonyl] Phenyl)hydrazino)_1Hpyrrolo[3,2-(;]° than bite_2-formamide n-({4-[(4-gas-3-fluorobenzene))] phenyl]phenyl丨Methyl)furo[2,3_c]pyridin-2-decylamine 5-hydroxy-indole-{[4-(1-methyl-1H-indazole-4-sulfonyl)phenyl]methyl }_ 1H-吲哚_2-Metamine]^-{[4-(2,6-dioxaoxyacridin-3-sulfonyl)phenyl]methyl}furan[2,3- c]pyridine-2-carboximine N-({4-[(2-butoxy-6-fluorobenzene)sulfonyl]phenyl}methyl)_1Η_Πpyrolo[3,2-c]pyridine 2-carbamamine N_({4-[(3-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)imidazolium, 2_a]pyrimidine-6-carboxamide N-{ [4-(naphthalene-1_sulfonyl)phenyl]methyl}furo[2 3_C]D than pyridine_2_carbamidamine 158436.doc •70- 201215609 N-({4-[(3,5 -difluorobenzene)sulfonyl]phenyl}indolyl)-1Η-indolo[3,2-c]pyridine-2-carboxamide N-{[4-(phenylsulfonyl)phenyl]曱基}-1-曱--1H-. Bisazo[3,4-b]pyridine-5-carboxamide N-[(4-{8-thiatricyclo[7.4.0.02,7]tridecane-1(13),2,4, 6,9,11-hexene-6-sulfonyl}phenyl)methyl]-1H-. More than [3,2-c]. Bisidine-2-amidoxime-({4-[1-mercapto-5-(trifluoromethyl)-1Η-.bazole-4-sulfonyl]phenyl}indolyl)-1Η- Pyrazolo[3,4-b]pyridine-5-nonylamine N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}methyl)-1Η-η ratio. Sodium [3,4-b]pyridin-5-nonylamine N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}methyl)m. Sit and [1,2-a] ° than 唆-6-carbamide N-({4-[2-(didecylamino)pyrimidin-5-sulfonyl]phenyl}indenyl)thiophene [2,3-c]pyridine-2-F decylamine N- { [4-(6-fluorenyl)pyridin-3-sulfonyl)phenyl]fluorenyl}thieno[2,3-c] Pyridine-2-carboxamide N-[(4-{[3-chloro-5-(hydroxyindenyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine-6 - formamide N-[(4-{6-azamidazo[1,2-a]acridin-3-sulfonyl}phenyl)indolyl]thieno[2,3-. ° ° bite-2-methylamine> gt-({4-[1-(4-fluorophenyl)-111-.pyrazole-4-sulfonyl]phenyl}fluorenyl) furan [ 2,3-c]pyridin-2-decylamine&gt;1-{[4-(quinolin-6-sulfonyl)phenyl]fluorenyl}furo[2,3-(:]'&gt; Bisidine - 158436.doc -71- 201215609 2-armenamine ({4-[6-(3,4_2 phenyl) 〇 唆 唆 绩 绩 绩 绩 绩 ] ] ] ] ] ] ] ] ] ] ] And U, 2, a] pyridine _6_carbamamine N (H'[6-(? _____)) σ ratio bite_3_cross-branched]phenyl} fluorenyl)-1Η-» ratio Each [3,2-c]pyridine-2-carbamamine N,5-diindenyl _iH-glutinous rice. Sodium -2- styrene) phenyl] fluorenyl} taste 0 sit and U, 2 -a]pyrimidinecarbamamine N_[(4-{[2-(dimethylaminocarbamoyl)benzene]sulfonyl}phenyl)methyl]thiazino[2,3-c]pyridine_2 _Metamine chloro-3-fluorobenzene) sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N &lt;&lt;4_[(3-Fluoro-5-methoxybenzene)sulfonyl]phenyl}indenyl)imidazo[l,2-a]pyrimidine·6_decylamine Ν·[(4_{[4 -fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide N-({4-[( 2,6-dichlorobenzene)sulfonyl]phenyl}methyl)_1H•indolo[3,2-c]pyridine-2-carboxamide n_({4-[(4-ethenylbenzene) Sulfo]phenyl]methyl)_1H_D than arrog[3,2-c]pyridine-2-carboxamide N-({4-[(3,5-dimethoxybenzene)sulfonyl) Phenyl-decyl)imidazo[l,2-a]pyridine-6-carboxamide N-{[4-({4-[(lR)-l-hydroxybutyl]phenyl}sulfonyl) Phenyl]methyl)furan[2,3-c]0 than bite 2-carboxamide N-({4-[(4-fluoro-3-methylphenyl)sulfonyl)phenylhydrazine Methyl)furan [2,3_ 15S436.doc •72· 201215609 c]pyridine-2-carbamimidoxime-{[4-(1-methyl-1H-carbazol-7-sulfonyl)phenyl Thio[}, thieno[2,3 - c]0 is more specific than sigma-2 -cartosamine-{[4-({3-[2-(didecylamino)ethyl)benzene}sulfonate Phenyl]fluorenyl}-1Η-pyrrolo[3,2-c]pyridine-2-cartoamine N-{[4-(2-methyl-2H-indazole-6-sulfonyl) Phenyl]fluorenyl}imidazo[l,2-a]pyrimidineN-({4-[(2-ethoxyphenyl)sulfonyl]phenyl}methyl-pyrazolo[3,4-b]pyridine-5-carboxamide N- ({4-[(2-ethylphenyl)sulfonyl]phenyl}indenyl)imidazopyridine-6-carboxamide N_({4-[(3,4-dioxaoxybenzene)sulfonyl) ]]phenyl}fluorenyl)furo[2,3-〇]° 〇定-2-甲含胺 N-{[4-(1,5-dimercapto-1H-imidazole-2-sulfonate) Phenyl]methyl}methyl}furo[2,3-c]pyridine-2-carboxamide N-[(4-{[3-(3,5-didecyl-1H-.bazole-1) -yl)phenyl]sulfonyl}phenyl) fluorenyl]-5-hydroxy-1H-indole-2-decylamine N-({4-[(5-chloro-2-methoxybenzene)sulfonate Thio[phenyl]indenyl)thieno[2,3-c]pyridin-2-indole N-({4-[(2,3-didecyloxy-5-mercaptophenyl)sulfonyl) Phenyl]phenyl}indenyl-1H-pyrazolo[3,4-b]pyridin-5-nonylamine N-({4-[(3-chloro-4-methoxyphenyl)sulfonyl) Phenyl}methyl)-1Η-η-pyrazolo[3,4-b]pyridin-5-nonylamine N-{[4-(isoquinolin-4-ylsulfonyl)phenyl]fluorenyl }-1Η-η比比和[3,2-c] 158436.doc •73- 201215609 Pyridine-2-carboxamide N-[(4-{[2-(trifluoromethyl)benzene]sulfonyl) }phenyl)indolyl]mi[i,[S,2-a]pyrimidine-6-carboxamide N-({4-[6-(diodecylamino)n) butyl-3-continuation]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide N -[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-carboxamide N-({4-[ (2-butoxy-6-1 benzene) continued fluorenyl]phenyl}indolyl)^m. Sit and [l,2-a]pyridine-6-carboxamide N-[(4-{[3 -(ethanesulfonyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine-6-carboxamide N-{[4-(phenylsulfonyl)phenyl曱 }}-3-(.bipyridin-3-yl)-l,2-喔 __ 5-decylamine N-[(4-{[2-曱-oxy- 4-(1 Hn ratio 0 -1-yl)benzene] continuation base}phenyl)methyl]thieno[2,3-c]&quot;bipyridine-2-carboxamide N-[(4_{ [3-( 1H-°嗤-1 -yl)benzene] 醯 }}}phenyl)methyl]imidin D sits and [1,2-a]° bites 6-carbamamine N-({4-[(3-chloro) -4-propoxybenzene)sulfonyl]phenyl}methyl)_1Η_%Π[3,2-c]pyridine-2-carboxamide N-({4-[(5-chloro-2) -propoxybenzene) continuation of the base] phenyl} fluorenyl) benzo[2,3-c]pyridine-2-carboxamide Ν·[(4-{[3·fluoro-5-(trifluoro) Methyl)phenyl]sulfonyl}phenyl)indolyl]-;^-pyrrolo[3,2-c]pyridine-2-carboxamidine Amine N-[(4-{[3-(ethylamine)methyl)benzene] hydrazino}phenyl)methyl] sit 158436.doc -74· 201215609 and U,2-a]pyrimidine_6_ Methionine N_({4-[(5-t-butyl-2-methoxyphenyl)sulfonyl]phenyl}methyl)-pyrano-U,2-a]-bite _6_曱醯Amine N-"4-[(3-ethoxyfluorophenyl)sulfonyl]phenyl}fluorenyl) 1H_pyrrolo[3,2~C]° pyridine-2-carboxamide.N_({ 4_[6-(3,4-difluorophenyl)"pyridinyl-2-sulfonyl]phenyl}methyl)·111-pyrolo[3,2-c]pyridine_2-decylamine N -({4-[2-(Trifluoromethyl)imidazo[na].比 _ 6 _ _ _ _ _ _ _ _ _ l l l l l l l l l l l l l l l l l l l l l l l l l l l l l l l l l l Phenyl}methyl)furo[2,3_c]pyridine·2-cartoamine N-[(4-{[4-fluoro_2_(trifluoromethyl)benzene]]] phenyl) Isozo[1,2-a]pyrimidine_6 formamide N_({4-[(4-methoxyphenyl)sulfonyl]phenyl}indolyl)thieno[2,3-c Pyridine-2-carbamimidoxime_"4_[(3,5-dimercaptophenyl) hydrazino]phenyl}indolyl)_1H_pyrrolo[3,2-c]pyridine_2-carboxamide N-(d[(4-ethylmercaptophenyl)sulfonyl]phenyl}indenyl)_1H-n-pyrazolo[3,4-b]° pyridine-5-carbamimidoxime-(4 -[(5-chloro-2-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine_6_methalin Ν·[(4'{[3- Fluoro-5-(fluorinated fluorenyl) stupid] 醯 } } 笨 笨 笨 笨 l l l l l l l l l l l l l l l l l l l 6 6 6 6 6 6 6 6 6 6 6 6 6 6 -di-f-oxyphenyl)sulfonyl]phenyl}indenyl)-1Η_° ratio 158436.doc •75· 201215609 and [3,2-c]pyridine-2-carboxamide N-({4- [(3-Ethylphenyl)sulfonyl;|phenyl}indenyl)_1Η·„Bizozolo[3,4-b]pyridine-5-carboxamide N-[(4-{[2, 4-bis(trifluoro Methyl)phenyl]sulfonyl)phenyl)]furo[2,3-c]pyridine-2-carboxamide N-[(4-{[4-(ethoxymethyl)benzene] Sulfohydrazinylphenyl)indolyl]furo[2,3-c]pyridine-2-carboxamide N-{[4-(5-chloro"pyridin-3-sulfonyl)phenyl]indole N-imidazo[12-a] bite-6-formamide N-({4-[(2-|l·5-nonylbenzene)) thiol;]phenyl}indenyl)_1Η_Π比And [3,2-c]pyridine-2-carboxamide N-({4-[(3-fluoro-5.methylphenyl)sulfonyl]phenyl}fluorenyl)thieno[2,3_c 0 咬 曱醢 曱醢 曱醢 曱醢 N-({4_[(4-fluorophenyl)sulfonyl]phenyl} fluorenyl)_1H_n pyrolo[3 2_c] pyridine-2-carboxamide N-[ (4-{[2-Methoxy-5-(propan-2-yl)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridin-2-indole N- [(4-{[3-(trimethylsulfonyl)benzene]]indolyl phenyl) decyl 13 benzothiazole-6-formamide N-{[4-(4-methyl. Bipyridin-3-sulfonyl)phenyl]mercaptobiszolo[3,4-b]&quot;bipyridin-5-nonylamine N-{[4-(bite-3-sulfonyl) Phenyl]methyl}furo[2,3_c]d is more than pyridine·2-carbamimidamine N-({4-[(3-propoxyphenyl)sulfonyl]phenyl}methyl) 158436.doc •76- 201215 609 0 than bite-6-formamide N-({4-[(2-oxo-4-methylphenyl) stellite]phenyl}methyl) „m. Sit and [1 2 a] pyrimidine-6-carbamide N-({4-[(2,5-dimercaptophenyl)sulfonyl]phenyl}methyl)furan [2,3, c Pyridine. N-(carbazylamine N-({4-[(2-)-5-methylphenyl))]]}}}}}. 2-carbamamine N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene] hydrazino] phenyl) methyl] bite. Nanhe [2,3-c]pyridine 2-nonylamine N-({4-[(3,5-dimercaptophenyl)sulfonyl]phenyl}methyl)furo[2,3_c]° ratio 2-carbamide N-({4-[(2,3-Dioxaoxybenzene)sulfonyl]phenyl}methyl)midindole[l,2-a]pyrimidine-6-carboxamide Ν·({4 -[(3-ethylphenyl)sulfonyl]phenyl}methyl)imidazo[12a]pyrimidine-6-carboxamide Ν·{[4-(2Η-1,3·benzodioxane) Pentene_5_sulfonyl)phenyl]methyl}pyrano[2,3-indene]pyridine_2-amidoxime-[(4-{[2-mercapto_4-(1Η-) Pyridin-1-yl)phenyl]sulfonyl}phenyl)methyl]°seno[2,3-c]pyridine-2-carbamamine N-({4-[(3-amine sulfonate) Nonylphenyl)sulfonyl]phenyl}methyl)imidazo[a]pyridin-6-carboxamide N-[(4-{[3 dec, each bite) phenyl] hydrazino} benzene Methyl]-salt and [l,2-a]pyrimidine-6-carboxamide N-[(4-{[4_(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl] Imidazole 158436.doc •77· 20121 5609 [l,2-a]pyrimidine_6_formammine NM[4-({3_[(2-methylpropyl)aminemethanyl]phenylsulfonyl)phenyl]methyl}° Sit and [l,2-a]pyrimidine·6· amidoxime-({4·[(2,3,6-trimethoxybenzene)sulfonyl]phenyl}methyl)thiophene[2] ,3-c].Bipyridine-2-carbamidine N_({4-[(2-fluoro-5-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[i,2-a] Pyrimidine-6·carbamamine Ν·({4-[(3-decyloxy-5-methylphenyl)sulfonyl]phenyl}methyl)_1Η·«比比和[3,2-c] Pyridin-2-decylamine N_{[4-(1-methyl"η-carbazole-4-sulfonyl)phenyl]methyl}furo[2,3-c]pyridine-2-carboxamidine Amine N-{[4-(phenylsulfonyl)phenyl]indolyl}imidazopyridinyl-6-nonylamine N-({4-[(2-chloro-4-mercaptophenyl)sulfonyl) Phenyl}hydrazino) imidazo[丨,;^ a]pyridine-6-anthracene N-({4-[(4-butenyl-3- benzene)] phenyl] fluorenyl) · 1 Η oxazolo[3,4-b]pyridine-5-nonylamine N-(6-(4-(morpholinomethyl)phenoxy)hexyl)_1Η_η ratio [32_c]. N-({4-[(3-ethoxy-2-fluorophenyl)sulfonyl]phenyl)indolyl) miso and [l,2-a]pyridine-6 -Procarbamide N-[(4-{[4-(4-indolylpiperazin-1.yl)benzene]]] phenyl)methyl) 1H_pyrrolo[3,2-c]pyridine 2-nonylamine N-{[4-(quinolin-8-sulfonyl)phenyl]indolyl}imidazo[[,? ^]pyrimidine-6-decylamine 158436.doc •78· 201215609 N-({4-[(4-Ga-2-nonyloxybenzene)sulfonyl]phenyl}indenylpyrazine [3, 2-c]pyridine-2-f decylamine N-({4-[6-(monomethylamino) η than bite _3_ **@) phenyl] phenylmethyl) sold pheno[2, 3-c]pyridine-2-carboxamide N-({4-[(5-chloro-2-methoxybenzene)sulfonyl]phenyl}indenyl)_1Η·η-pyrazolo[3,4 -b]pyridine-5-f-decylamine N [(4 {[3fluoro-4-(dimethyl)benzene]]]]phenyl)methyl] fluoren[2,3-c]pyridine 2-carbamimidoxime-{[4-(1,4-dimethyl-1H-imidazol-2-sulfonyl)phenyl]mercapto}furo[2,3-c]acridine-2 -Proline N-{[4-(phenylsulfonyl)phenyl]methyl)imidazopyridine -6-nonylamine N-({4-[(3-propoxy)] fluorenyl]benzene } 甲基 甲基 He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He He 』^] pyrimidine-6-formamide N-({4-[4-(trifluoromethyl)"pyridinyl-2-sulfonyl]phenyl}indenyl)iH npyrazole[3,4 -b]pyridine-5-carbamamine&gt;^-{[4-(211-1,3-benzodioxole-4-sulfonyl)phenyl]methyl*}-1Η-pyrrole And [3,2-c]pyridine-2- Indoleamine N-[(4-{[4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidin-6-carboxamidophenyl)anthracene ]]-ΙΗ-吼》圭和[3,4-b]pyridinium N-[(4-{[3-败-4-(lH"m_yl))]]]] Methyl 158436.doc •79· 201215609 1H-pyrrolo[3,2-c]pyridine-2-carboxamide N-{[4-(6-decylnaphthalene-2-sulfonyl)phenyl [furfuryl]furo[2,3-c]pyridine-2-carboxamide N-{[4-(2-mercapto-2H-0-conoxazol-6-sulfonyl)phenyl]fluorenyl } «Mizozolo[l,2-a]pyridine-6-formamide N-({4-[(2-methylphenyl)sulfonyl]phenyl}methyl)thieno-p,3-c Acridine-2-carboxamide N-{[4-(5-fluoro.bipyridin-3-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyrimidin-6-carboxamidine Amine N-({4-[(2,4-dioxa-3-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine-6-carboxamide N -({4-[(5-fluoro-2-indolyl)sulfonyl]phenyl}indolyl[3,2-c]pyridine-2-carboxamide N-{[4- (naphthalene-1-sulfonyl)phenyl]methyl}thieno[2,3-c]heptan-2-nonylamine N-{[4-({4-[2-(dimethylamine) Ethyl]phenyl}sulfonyl)phenyl]indenyl} And [l,2-a]pyrimidine-6-nonylamine N-[(4-{[2-methyl_4.(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]·11 €-. Bilo and [3,2-〇]. ratio. _2-decylamine N-({4-[(2,3,6-trimethoxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]npyridin-2 -Metformin N ({4 [(3 -butoxybenzene) fluorenyl]phenyl} fluorenyl) tastes saliva and [i,2_a] α ratio bite-6-carbamide Ν-({4- [(3,5-Dimethoxybenzene)sulfonyl]phenyl}fluorenyl)furan 158436.doc 201215609 [2,3-c]pyridine-2-carboxamide N-({4-[( 3-oxo-2-fluorophenyl)sulfonyl]phenyl}indolyl)furo[2,3_c]pyridine-2-carboxamide N-{[4-(5-gas. than bite_3_ continued醢))phenyl]fluorenyl} - 1H-0 than saliva[3,4_ b]° than 唆-5-formamide N-({4-[(3-mercaptophenyl)sulfonyl]benzene Methyl)thiophene [2,3 &lt;] indole-2-carboxamide Ν[[4-{[4·(dimethylaminocarbamido)benzene;]sulfonyl}phenyl)indenyl]_#1Η-pyrrolo[ 3,; 2-c]pyridine-2-carboxamide N-[(4-{[4-(hydroxyindolyl)]]]]]]]]]]]]] Pyridine-6-formamide N-({4-[(3,4-dimethoxyoxy)sulfonyl]phenyl}methyl)_1Η_π is 嗤[3,4-b]pyridine-5 - amidoxime-{[4-(1-methyl-1Η-°ββ-6-ylidene)phenyl]methyl} 0 furano[2,3-c]pyridine-2- Methionamine N-{[4-(2,3-dihydro-1-benzofuran-7-sulfonyl)phenyl]methyl thiophene • and [2,3-c]pyridine-2-methyl Amidoxime-{[4-(1Η-吲哚-7-sulfonyl)phenyl]indolyl}·1Η-. Bizolo[3,4·b]0 is 0-but-5-cartoamine N-({4-[(3-tert-butyl))]]}}}} ι,2· a] shout bite-6-曱 胺 N N-[(4-{[4-(propyl-2-yloxy)benzene] continuation base} stupid) methyl] miso and [l ,2-a]pyrimidine-6-formamide N-{[4-({3-[(propan-2-yl)amine aryl]benzene} hydrazino)phenyl]fluorenyl) 158436.doc -81 · 201215609 Thieno[2,3-c]0 is 唆-2-nonylamine N-({4-[(2,3-didecyloxy-5-mercaptophenyl)sulfonyl]benzene }}methyl)furo[2,3-c]0 than bite-2_ 曱N-{[4-(phenyl cans) phenyl]methyl 嗉 bit-2-carbamide 5- hydroxy-N-[(4-{[3-(°-r-pyridin-1-yl)benzene]sulfonyl}phenyl)methyl]-1H-indole-2-carboxamide-[(Μ [3-(ΐΗ-β is more than s-l-yl)benzene] hydrazino}phenyl)methyl]pyrano[2,3-c]pyridine-2-cartoamine N-({4-[ (2-Methyl-4-propoxybenzene)sulfonyl]phenyl}methyl)-1Η-η ratio 0 and [3,2-〇]* ratio 0 曱 胺 1 1 1 1 4-({3-[(didecylamino)indolyl]phenyl}sulfonyl)phenyl]fluorenyl}furo[2,3-c]0-pyridyl-2-carboxamide N-( {4-[(3-nitrobenzene) cans]phenyl}methyl)furan[2,3- c]°-pyridine-2-decylamine N-{[4-(5-fluoro 0-pyridine-3-sulfonyl)phenyl]methyl}_ιη·pyrrolo[3,2-c]pyridine- 2-carbamimidoxime-[(4-{[3-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)methyl]-1Η·〇Λ 并[[,4-b] 0 to bite-5-cartoamine N-{[4-(2,3-dihydro-1,4-benzodioxan-6-sulfonyl)phenyl]indenyl}thiophene [2,3-c]pyridine·2-decylamine N-({ 4-[(4-methoxy-3,5-dimethylphenyl) benzyl]phenyl}methyl) And [l,2-a]° than 唆-6-cartoamine N-[(4-{[3-(3,5-dimethyl-1H-indazol-1-yl)benzene]sulfonyl) }phenyl) fluorenyl]thieno[2,3-c]pyridine-2-carboxamide 158436.doc -82 - 201215609 Ν_({4_[(2,5-dimethoxybenzene)sulfonyl] Phenyl}methyl)furo[2,3-c]pyridinecarboxamide N_({4-[(2,4,6-tridecylbenzene)sulfonyl]phenyl}methyl)imidazo[ l,2-a]acridine_6_carbamidine N_[(4d[4-(4-mercaptopiperazin-1-yl)benzene]sulfonyl}phenyl)methyl]thiophene [2, 3-c]pyridine_2_ amidoxime·[(4-{[2-methoxy_5_(trifluoromethyl)benzene]]] phenyl)methyl] 0 m 0 sit and [ l,2-a]pyrimidine _6_decylamine • Ν_({4-[(4· _2_Ethoxybenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine_6_bristamine N-[(4-{[3-(ethanesulfonyl)) Benzene]sulfonyl}phenyl)indolyl]Miso-[l,2-a]pyrimidine-6-nonylamine {[4-({3-[2-(didecylamino)) 6 Benzo]phenylsulfonyl)phenyl]methyl}thieno[2,3-c]acridin-2-carboxamide N-({4-[(4-曱oxy-3,5-di) Nonylbenzene) 醯 醯 ]]phenyl}methyl) ° pheno[2,3-c]pyridine-2-guanamine Lu N-({4-[(3,4-difluorobenzene) sulfonate Mercapto]phenyl}methyl)imidazo[l,2-a]. Benzo-6-decylamine N-[(4-{[3-fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indolyl]furan[2] , 3-c]pyridin-2-decylamine N-({4-[2-(didecylamino)-negative-5-3⁄4)]]}}}}))) 3-c]pyridin-2-decylamine N-({4-[(2-ethoxyphenyl)sulfonyl]phenyl}methyl)-1Η-. Bisolo[3,2-c]pyridine-2-carboxamide 158436.doc -83- 201215609 N-[(4- {[2-methoxy-5-(propan-2-yl)benzene] continued Styrene}phenyl)methyl]oxazolo[l,2-a]pyridine-6-nonylamine N-({4-[(2,6-dioxabenzene)sulfonyl]phenyl}- base). Meter. Sit and [i 2 a] 0 than bite-6-formamide N-({4-[(2-|L-5-methoxybenzene))]]] 2,3-c] acridine-2-carboxamide N-({4-[(2-oxo-5-methylphenyl) hydrazino]phenylindolyl)β-phene[2] , 3-c] ° bite 2-cartoamine N-({4-[(3- gas_5_methoxybenzene) hydrazino]phenyl}methyl) bite. Nanhe [2,3-c] ° bite 2-cartoamine N-({4-[(3,5-difluorophenyl)sulfonyl]phenyl}methyl)imidazo[12a]pyrimidine -6-carbamamine N-({4-[(2-ethylphenyl)sulfonyl]phenyl}methyl)furan[2,3 &lt;] 〇 咬 -2- 醯 醯 醯 醯 醯 醯 -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- {[3-(3,5-monomethyl-1^!-. 〇 _1_1-yl) benzene] continuation base} phenyl) methyl]-1,3-benzo D 嗤曱醯Amine N-[(4-{[4-(ethoxymethyl)benzene]sulfonyl}phenyl)indolyl[3,2-c]pyridine_2·decylamine N_({4- [5-(Dimethylamino)pyridazine_2_sulfonyl]phenyl}methyl)imidazo[1,2-a]. Bisidine_6·decylamine ν·({4-[(2-gas-5-fluoro stupid))]]phenyl}indenyl). Sit and [iha] 0 to bite-6 - ugly amine 158436.doc • 84· 201215609 N-[(4-{[3-gas-5-(diethylamine)) sulfonyl} Phenyl)fluorenyl]thieno[2,3-c]pyridinecarboxamide N-[(4-{[4-(2-mercaptopropoxy)benzene]]] phenyl)methyl] Benzyl [2,3-c]pyridin-2-decylamine N_{[4_(phenylyl)phenyl]methyl}quinolin-6-carboxamide N-({4-[(3) -butoxybenzene)sulfonyl]phenyl}indolyl)furo[2,3_c]pyridine-2-carboxamide N-({4-[(4-methylphenyl)sulfonyl)phenyl Mercapto) imidazo[12^]pyrimidine-6-carbenamide N-({4-[(3-methanesulfonylbenzene)sulfonyl]phenylindolyl)imidin[l, 2-a]n ratio bite-6-formamide N-({4-[(2,6-dimethoxyoxy-4-indolylbenzene)sulfonyl]phenylindolemethyl)thieno[2] ,3-c]pyridine_2-formamide n-{[4-({4-fluoro-3-[(propan-2-yl))aminomethane]phenyl}sulfonyl)phenyl] fluorenyl }°Penteno[2,3-c]n is a bit of 2-nonylamine ({4-[(5-chloro-2-ethoxybenzene) hydrazino]phenyl}fluorenyl) And [l,2-a]° is more than 唆-6-曱 Ν Ν·({4_[(3,5-dichlorobenzene)sulfonyl]phenyl}methyl)_1Η-η-pyrazolo[3 ,4-b]pyridine-5-A Amine N-[(4-{[2-methoxy·3_(trifluoromethyl)benzene] hydrazino}phenyl)indolyl] azo 0 sits and [l,2-a]pyridine-6- Amidoxime-[(4-{[4·(4-mercaptopiperazinyl)benzene])]phenyl)methyl]_ 1Η-»Bizozolo[3,4-b]pyridine-5 -Procarbamide N-({4-[(2-fluoro-3-indolyloxy))]]]]]]]]]]]]]] -1?]» 比 疋 疋 醯 醯 N N N-({4-[(4-嘉1 &amp; '敦苯) 醯 醯)]phenyl)methyl)_1 -c]pyridine·2_f decylamine N-[(4-{[2-fluoro-4 riTT ..biazole-buyl)benzene]sulfonyl}phenyl)methyl] 咬 并 [2,3 ^2-Protonamine n-{[4-(5-methoxy A arylpyridine-3-sulfonyl)phenyl]indolyl}imidazo[1,2-a]carbanrid-6-carboxamidine Amine N-({4-[2-(三翁鼠methyl)pyridine-3-sulfonyl]phenyl}indolyl)furo[2,3-c]pyridinecarboxamide-[(4- {[4-|ί 〇2-Trifluoroethoxy)benzene]sulfonyl fluorenylphenyl) fluorenyl]mi-salt and biting winter formazan N [(4-{[3-(difluoromethoxy) Benzene]sulfonyl}phenyl)methyl]-1H-indole[3,2-c]. Specific bite 2_carbamamine N-({4-[(3-chloro-5-methylphenyl)sulfonyl]phenyl}methyl)_1H_pyrazolo[3,4-b]pyridine- 5-carboxamide N-({4-[(2-chloro-5-fluorophenyl)sulfonyl]phenyl}methyl)furo[[2,3-c]pyridine-2-carboxamide N -{[4-({3-[(2-methylpropyl))aminomethyl)benzene} hydrazino)phenyl]methyl}furo[2,3-c]pyridine-2-carboxamidine Amine N-{[4-(phenylsulfonyl)phenyl]methyl}-1Η-η-pyrazolo[3,4-b]. Bisidine-5-decylamine N-{[4-(.pyridin-3-sulfonyl)phenyl]methyl}-1Η-«bido[3,2-c]. Than.定-2 -Artemisinin-{[4-(2Η-1,3-benzodioxol-5-sulfonyl)phenyl]indole 158436.doc • 86 · 201215609 *}-1Η - tonnes of [3,2-c]pyridin-2-decylamine N-({4-[(3,5-dimethoxyphenyl)sulfonyl]phenyl}methyl)-1Η-. Bisazo[3,4-b]pyridine-5-carboxamide N-[(4-{[2-(morpholin-4-ylmethyl)benzene]sulfonyl}phenyl)methyl]imidazole And [l,2-a]pyrimidine-6-f-decylamine N-({4-[(2,6-dioxa-3-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[l ,2-a]pyrimidine-6-formamide N-({4-[(2-fluoro-5-mercaptophenyl)sulfonyl]phenyl}indolyl)furo[2,3-c] ° ratio. Benz-2-carbamide N-({4-[(3-fluorophenyl)sulfonyl]phenyl}fluorenyl)furo[2,3-c]. Bipyridine-2-carboxamide N-[(4-{ [5-fluoro-2-(hydroxyindenyl)benzene]sulfonyl}phenyl)methyl]thiophene [2,3-c]. Bipyridine-2-carbamide N-({4-[(3-methoxy-4-mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2 -Procarbamide N-({4-[(2-Ga-4-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]bitat-6-carboxamide N -{[4-(6-methyl.pyridin-3-sulfonyl)phenyl]methyl}imidazo[l,2-a] ° ratio -6-carbamamine N-[(4 -{[2-(Trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]npyridin-2-indoleamine-{[4-(1 ,5-dimercapto-1H-imidazol-2-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyridine-6-carboxamide N-[(4-{[3-chloro) -4-(Trifluoromethyl)benzene]sulfonyl}phenyl)indenyl]thiophene 158436.doc -87- 201215609 and [2,3-c]pyridine-2-carboxamide N-[(4- {[5-Hydroxy-2-(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4-bppyridin-5-amidoxime-[ (4-{[4-(1Η-imidazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]°^^-6-nonylamine N-{[ 4-(phenylsulfonyl)phenyl]mercapto}-1Η-η-pyrazolo[3,4-b]acridine-3-carboxamide N-({4-[(4-fluorophenyl)sulfonate) Mercapto]phenyl)indolyl)imidazo[1,2-a]acridine-6-indole amine $ N- ({4-[(3,4-Difluorophenyl)sulfonyl]phenyl}indolyl)-1Η-η-pyrazolo[3,4-b]pyridine-5-carboxamide N-({4 -[(4-butoxy-3-acetophenone)sulfonyl]phenyl}indolyl]thieno[2,3-c]pyridin-2-indoleamine-{[4-(1-曱-1H-carbazole-6-sulfonyl)phenyl]fluorenyl}-1Η-η-pyrolo[3,2-c]pyridin-2-decylamine N-({4-[(3-曱 cesulfonyl benzene) sulfonyl] phenyl} fluorenyl) thieno[2,3-c]pyridine-2-decylamine N-({4-[3- gas-2-(morpholine) 4-yl)acridine-4-sulfonyl]phenyl}indenyl) thieno[2,3-c]pyridin-2-indole N-({4-[(3-chloro-4-) Methylbenzene)sulfonyl]phenyl}methyl)imidazo[1,2--cartoamine &gt; 1-{[4-(1,3-thiazol-2-sulfonyl)phenyl]indole Dehydrofuran [2,3-〇]. Bipyridine-2-carboximine N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}indolyl)imidazolium 158436.doc -88- 201215609 [l,2 -a]pyridine-6-formamide N-[(4-{[4-chloro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]imidazo[1,2-a Pyridine-6-nonylamine N-({4-[(4-butoxy-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-η ratio [3,2- c]pyridin-2-decylamine N-{[4-(6-methoxynaphthalene-2-sulfonyl)phenyl]methyl}-1Η-η-pyrolo[3,2-c]pyridine 2-carbamamine N-[(4-{[3-(propane-1-sulfonylamino)benzene]sulfonyl}phenyl)indenyl]thiophene[2,3-c]pyridine -2-decylamine N-[(4-{[4- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[1,2-a]pyrimidine- 6-decylamine N-[(4-{[3-fluoro-5-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indolyl]thieno[2,3-c]pyridine 2-nonylamine N-[(4-{[2-mercapto-4-(1Η-»bisazol-1-yl)benzene]sulfonyl}phenyl)methyl]-1H-pyrazole [3,4-b]pyridine-5-nonylamine N-({4-[(3-chloro-5-fluorobenzene)sulfonyl]phenyl}methyl)-1Η-η-r-[oxazolo] [ 3,4-b]pyridine-5-formamide N-({4-[5-(trifluoromethylpyridin-2-)醯基]phenyl}fluorenyl)-1Η-° ratio. Sit and [3,4-b] °--5-nonylamine N-({4-[(3-mercaptophenyl)sulfonyl] Phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-{[4-(2-methylacridin-3-sulfonyl)phenyl]indolyl}-1Η -η-pyrazolo[3,4-b]pyridine-5-carboxamide N-({4-[(2-cyanobenzene)sulfonyl)phenyl}indolyl)furan[2,3- c]. 158436.doc -89- 201215609 pyridine-2-carboxamide N-{[4-(6-mercapto &quot;bipyridin-2-sulfonyl)phenyl]methyl}furan[2 ,3-c] pyridin-2-indoleamine N-{[4_(phenylsulfonyl)phenyl]methyl}-1Η-pyrrolo[3,2-c]pyridin-2-decylamine N- [(4-{[3-(ethylaminoindolyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-carboxamide-{[4- (1-indenyl-ih_carbazole-5-sulfonyl)phenyl]indenyl}thieno[2,3-c]pyridine-2-carboxamide N-({4-[(3-B) Nonylphenyl)sulfonyl]phenyl}methyl)furo[2 3 c]pyridine-2-carboxamide N-({4-[(2-chloro-5-decyloxy))sulfonyl) Phenyl}methyl)furo[2,3-c]e than 2-mercaptoamine N-[(4-{[4-fluoro-3-(trifluoromethyl)benzene]sulfonyl) }phenyl)indenyl]furo[2,3-c]pyridine-2 -Procarbamide N-({4-[(4-butoxy-2-indolylbenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N-({4-[(3-ethoxyphenyl)sulfonyl]phenyl}indolyl) imidazo[1,2_幻响°定-6-carbamamine N-({4-[( 3-fluoro-4-methylphenyl)sulfonyl]phenyl}methyl Mh. Bisazo[3,4-b]pyridin-5-nonylamine N-({4-[4-(trifluoromethyl)0-pyridine-2-sulfonyl]phenyl}methyl)imidazolium [l,2-a]pyridine-6-formamide N-[(4-{[4- gas-2-(trifluoromethyl)benzene]sulfonyl)phenyl)methyl]furan 158436.doc •90· 201215609 and [2,3-c]0 than bite 2-carbamide N-({4-[(4-Ga-2-ethoxyphenyl)sulfonyl]phenyl}methyl) Furo[2,3-c]pyridine-2-carboxamide N-{[4-(2,3-dihydro-1-benzofuran-7-sulfonyl)phenyl]methylfurfurfuran [2,3-c]pyridine-2-carboxamide N-[(4-{[3-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2- a] pyrimidine-6-formamide N-({4-[4-(trifluoromethyl)pyridin-2-sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2 - indoleamine N-[(4-{[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine- 2-nonylamine ({4-[(2-gas-6-methoxybenzene) hydrazino]phenyl}indolyl)-out-0 to 0 and [3,2-c]pyridine- 2-nonylamine N-{[3-(phenyl phenyl)phenyl]fluorenyl}_ΐΗ-dehydrazino[3,2-c]吼π定_2_carbamamine N-[(4- { [4-fluoro-3-(trifluoromethyl)benzene]sulfonyl} Imidyl]imidazo[1,2-a]pyridin-6-nonylamine N-({4-[(2-ethoxyphenyl)sulfonyl]phenyl}indolyl)imidazopyridine- 6-Metamine Ν·[(4-{[2-曱-oxy-5-(propan-2-yl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine -2-decylamine N-[(4-{[2-mercapto-4-(trioxinyl)benzene]] phenyl) fluorenyl] taste 0 sits and [1,2-a] 0 to bite-6-nonylamine N-({4-[(2-decyloxybenzene)sulfonyl]phenyl}fluorenyl)thieno[2,3_c] 158436.doc -91· 201215609 pyridine- 2-Protonamine N-({4-[(2-phenoxyphenyl)sulfonyl]phenyl}indolyl)furo[2,3^pyridin-2-decylamine N-({4- [(4-Phenylbenzene)sulfonyl]phenyl}methyl)imidazolyl 6-carbamimidoxime-({4-[(3·fluoro-5-methylphenyl)sulfonyl]phenyl} A Imidazo[a]pyrimidin-6-carboxamide N-({4-[(3-Ga-2-methylphenyl)sulfonyl]phenyl}methyl)_ih-indole-[3, 2-c]pyridine-2-carboxamide N-[(4-{[3-(trifluoromethoxy)benzene]sulfonyl}phenyl)methylpyrazolo[3,4-b]pyridine -5-Protonamine N-({4-[(2-butoxy-5-gasbenzene)sulfonyl]phenyl}indolyl)-iH-pyridinium[3,2-c]pyridine 2-carbamamine- ({4·[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}indenyl)-iH·.嗤 嗤 [3,4-b] ° than bite -5-armamamine N-({4-[(2-gas-5-gas benzene) continuation] phenyl} fluorenyl) [2,3_e] ° than 2-mercaptoamine N-({4-[(3-methoxy-5-mercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2 -a]pyrimidine-6-nonylamine N-[(4-{[3-(ethanesulfonyl)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine- 2-Protonamine N-({4-[(2-fluorophenyl)sulfonyl)phenyl}indolyl)furo[2,3-c]tonidine-2-indanamine·{[4 -(4-methylacridin-3-sulfonyl)phenyl]methyl}imidazo[i,2_a] 158436.doc •92· 201215609 Pyrimidine-6-carbamamine&gt;^-({4- [(3,4-Dimethoxyphenyl)sulfonyl]phenyl}methyl)_11^_. Bisolo[3,2-c]pyridine-2-carboxamide&gt;^-{[4-(1,4-dimethyl_1^1-imidazolium-2-sulfonyl)phenyl]indole Imidazo[l,2-a]pyridine-6-carboxamide N-({4-[2-(didecylamino)pyrimidin-5-sulfonyl]phenylindolemethyl)imidazolium [1,2-a]pyridine-6-carbamimidoxime-{[4-(1-methyl-1H-indazole-4-sulfonyl)phenyl]indolyl}imidazo[l,2- a] bite-6-carbamamine N-[(4-{[3-(2-mercaptopropoxy)]]]]]phenyl)indolyl p-myzazol[l,2-a Pyridine-6-formamide N-[(4-{[2-chloro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine -6-carbamamine N-({4-[(3-butoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N-( {4-[(2,4-Dimercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carbamimidoxime-({4-[(4·)曱oxyphenyl)sulfonyl]phenyl}fluorenyl)-1Η-ηpyrolo[3,2-c]pyridine-2-carboxamide N-[(4-{[4-(propyl-2) -yl)phenyl]sulfonyl}phenyl)indenyl]thieno[2,3-C]11 than bite-2-carboxamide-[(4·{[2-(trifluoromethyl))benzene Sulfhydryl}phenyl)methyl]-1Η-&quot;bi[3,2_c]acridine-2- Methionine N-({4-[(3-ethylmercaptophenyl)sulfonyl]phenyl}decylpyrrole 158436.doc •93- 201215609 [3,2-c]pyridine-2-carboxamidine Amine N-({4-[(2-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridin-2-decylamine N_{ [4 -(5-Gas-3-methylacridin-2-sulfonyl)phenyl]methyl}imidazo[l,2-a]pyridine-6-carboxamide N-({4-[2- (3-Fluorophenyl)-1,3-thiabend-4-sulfonyl]phenyl}methyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide N_({ 4-[(3,5-dioxabenzene)sulfonyl]phenyl}indolyl)_1H_npyrho[3,2-c]pyridine-2-carbamimidoxime-[(4_{[3-( 3,5·dimethyl-1H-«bazol-1-yl) stupid]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide N-{[ 4-(5-methoxy σ-pyridyl_3- continued fluorenyl)phenyl]methyl} sinter[2,3_c]pyridin-2-decylamine]^-[(4-{[2 -Fluorine_4-(11^bisazol-1-yl)benzene]sulfonyl}phenyl)methyl]- 1Η-pyrazolo[3,4-b]pyridine-5-carboxamide N-[ (4-{[4-Gas-2-(trifluoromethyl)benzene]] fluorenyl}phenyl)methyl]pyrrolo[3,2-c]pyridin-2-indenylamine·{[4 -(2-methyl-2H-, oxazol-6-sulfonyl)phenyl]indolyl}furan[2,3 -c]pyridine-2-carboxamide N-(4-(phenyl hydrazino)))-1H-imidazo[4,5-b]«pyridyl-6-carbamamine N-[(4 -{[4-(trifluorodecyloxy)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide N-{[4-(quinoline- 3-sulfonyl)phenyl]methyl}-1Η-»pyrolo[3,2-c]npyridin-2-carboxamide 158436.doc -94- 201215609 N Ethoxy-2_Fluorine Benzene sulfonyl]phenylmercapto)imidazo[l,2-a]pyrimidine-6-carbamimidamine N ({4-[(3-Ga-4-propoxybenzene)sulfonyl] Phenylhydrazine methyl)imidazo[1,2_a]° pyridine-6-nonylamine N benzothiophene-7-sulfonyl)phenyl]methyl}-1Η-η-pyrazole[3,4 -b]pyridine_5_carbamamine, (chloro-4-(di-fluorenyl)benzene] continuation base} phenyl)methyl] glutinous rice. Sit, [, 2a] 〇 ^.定_6_甲甲胺,NU buckle [(3'5-dimethoxybenzene)sulfonyl]phenyl}indenyl)_1H-pyrrolo[3'2-c]pyridine_2-carboxamide G4-[6-(morpholine-4-yl)pyridine_3-m-decyl]phenyl}methyl)imidazo[l,2-a]pyridine_6_methalin Ν·({4-[ (2-Chloro-4-fluorobenzene)sulfonyl]phenyl}methyl)imidazopyridine-6-carboxamide N ({4-[(3-ethylmercaptophenyl))]phenyl) Methyl) σ-methazolo[ua]pyrimidine-6-formamide N-{[4-(quinoline-3-sulfonyl)phenyl]indolyl}imidazo[12_a;h-pyridyl_6_ Indoleamine N-[(4-{[3-敦-5-(morpholin-4-yl)benzene] hydrazino}phenyl)indolyl]isoxazo[l,2-a]pyridine-6 -carbamidine N-[(4-{[2-(morpholine-4-yl)phenyl)sulfonyl phenyl)indolyl]_m_pyrazolo[3,4-b]pyridine_5 _ decylamine N-[(4-{[4-(lH-imidazol-1-ylmethyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-曱醯amine 158436.doc •95· 201215609 N_({4_[(4_methoxy-2,5-dimethylphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a] .比 _ _6_ amidoxime [ [[4-{[4-fluoro-3_(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl] fluoren [2] ,3-c]D than bite_2_nonylamine N_[(4-{[3- gas '5-(2-methylpropoxy)benzene] hydrazino}phenyl)indolyl]-1H -pyrrolo[3,2_c]pyridine-2carbamamine-""(2,5-dimethoxyphenyl)sulfonyl]phenyl)methylpyrolo[3,2-c]pyridine Indoleamine &gt;^({4-[(2-fluoro_4_mercaptophenyl)sulfonyl]phenyl}methyl)thieno[2,3_c]. 0-but-2-carbamide N ({4_[5-(°Byrrolidin-1-yl) ° pyridine-3-sulfonyl]phenyl}indolyl)-iH-pyrazolo[^^^.pyridinyl-carboxamide N ({4-[(3-stupyl)sulfonyl)phenyl)indolyl)_ih_d is more than s-[3,2-c]0 than 2-mercaptoamine N_{C4_({4_[ (dimethylamino)methyl]phenyl}sulfonyl)phenyl]fluorenyl} imidazo[l,2-a]pyrimidine_6_methalin Ν-[(4·{[3-(two Ethylaminemethanyl)_5_fluorobenzene]sulfonylhydrazine phenyl)methyl]-1Η-pyrrolo[3,2_c]pyridine_2_methalin Ν·[(4-{2-[B (Methyl)aminodiphenyl, 3_thiazole-5-sulfonyl)phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide N-({4-[( 5-gas-2-methylbenzene) sulfonate Thiol]phenyl hydrazine methyl)thieno[2,3_ c]σ ratio bite-2-cartoamine N-({4-[(5-chloro-2-propoxybenzene)sulfonyl]benzene Base 丨methyl)imidazo[l,2-a].Bite-6-carbamide 158436.doc -96- 201215609 N-[(4-{[4-(lH-imidazol-1-ylfluorenyl) Benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-carboxamide N-({4-[(4-chloro-2-ethoxyphenyl))sulfonate Phenyl]methyl}methyl)thieno[2,3-c]pyridine-2-carboxamide 1^-({4-[(3-chloro-5-methylphenyl)sulfonyl]phenyl} Mercapto) imidazo[1,2-a]bitat-6-cartoamine N-[(4-{[4-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)methyl Furano[2,3-c]pyridine-2-carboxamide φ N_[(4- {[4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indole -1H-pyrrolo[3,2-c]pyridine-2-carboxamide N-({4-[(2-methylphenyl)sulfonyl]phenyl}methyl)furan[2, 3-c]. Bis-2-carbamide N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)indolyl]-1H-* 3,2-c]pyridine-2-carbamimidoxime-({4-[1-(3-phenylphenyl)-1Η-°-pyrazole-4-sulfonyl]phenyl}methyl)furan [2,3-c]pyridin-2-decylamine _ N-[(4-{5H,6H,7H ,8H,9H-imidazo[l,2-a]azet-3-sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidin-6-nonylamine N-({4 -[(3-decyloxy-5-nonylbenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N-({4-[(3) -gas-5-fluorobenzene)sulfonyl]phenyl}indolyl)-1Η-°pyrho[3,2-c]pyridine-2-carboxamide N-{[4-(2-methyl) _1,3_thiazole-4-sulfonyl)phenyl]indolyl}-1Η-pyrazolo[3,4-b]pyridine-5-decylamine 158436.doc -97- 201215609 N-({ 4-[6-(4-methylpiperazine + yl) ketone _3·sulfonyl]phenyl)-1Η-pyrrolo[3,2-c]pyridine·2-carbamimidoxime-( {4-[(4-Fluoro-2,5-dimethylbenzene) continuation]Phenyl}methyl[2,3-c]pyridine-2-carbamamine N-{[4-(2 -Methyl], 3n 醯 )))phenyl]methyl}bit [2,3-c]pyridine-2-carboxamide N-({4-[(2,3_difoxy-5) _Methylbenzene) 醯 醯 ]]]]]]]]][[2,2-8]° 密-6-6甲甲甲amine-(μ·[(2-methanesulfonylbenzene) sulfonate Mercapto]phenyl}methyl)whenchuan[2,3-c]pyridine-2-carboxamide N-[(4-{[4-(propyl-2-yl)benzene]] Methyl]myrazole Μα] pyrimidine-6-carbamidamine-{[4-(quinoline) 8-(sulfonyl)phenyl]methyl}_1Η_pyrazolo[3,4_b]pyridine-5-carbamimidoxime-{[4-(1-mercapto-1H-吲嗤-4- continued Mercapto)phenyl]methyl ratio. And [3,4_b]pyridine-5-carbamidamine &gt; 1-({4-[(4-cyclohexylbenzene) hydrazino]phenyl}fluorenyl) thieno[2,3_ &lt;:] pyridine-2-carbamimidoxime-{[4-(1-propyl-1H-pyrazole-4-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyridine -6-carbamamine N-({4-[(2-chloro-5-fluorophenyl)sulfonyl]phenyl}indolyl)-1Η-«bido[3,2-c]pyridine-2 -carbamidine N-({ 4-[(2-butoxy-6-fluorobenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide 158436 .doc -98- 201215609 Ν_{[Μ5_良°比咬-3·杂基)phenyl]methyl}-1Η-« ratio. Sit and [3,4- b] pyridine-5-carbamide U4 U3 U-(dimethylamino)ethyl] phenyl} sulfonyl) phenyl] methyl bumi sit and [1, 2 -&amp;], bite-6-carbamamine (Η [(2'6·monomethoxy-4(nonylphenyl))sulfonyl]phenyl}fluorenyl)-1H- than hydrazine [3, 2-c]n ratio bite-2 carbamide N [(4 {[3-(morpholine-4-yl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]D Bisidine_2·carbamamine N-[(4-{5H,6H,7H,8H,9H-^#[1,2-a] t, -f -3-^ m 1.} phenyl)indole Thio[2,3_c]pyridine_2_decylamine N ({4[(3 - 2 butylphenyl))]phenyl)indolyl) sinter[2, c] pyridine- 2-nonylamine N-[(4-{[3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]_1H_0-pyrazolo[3,4-b]pyridine-5-carboxamidine Amine N-[(4-{[3-fluoro-4-(fluorenylthio))]]]]]]]]]]]]]]]] -{[4-(2,3-dihydro-indole-benzodioxan-6-sulfonyl)phenyl]methyl}furo[2,3-c]° pyridine-2 -Metformamide 1^-({4-[(4-butylphenyl)sulfonyl]phenyl}methyl)furo[2,3-〇]° than pyridine-2-carboxamide Ν-{ [4-(1-methyl-1H-indol-2-sulfonyl)phenyl] Thio[2,3-c]pyridine-2-carboxamide N-[(4-{6-azamidazo[l,2-a]° pyridine-3-sulfonyl}phenyl) Methyl]_ 1H-pyrazolo[3,4-b]pyridine-5-carboxamide-99· 158436.doc 201215609 N-[(4-{[3-fluoro-4-(1Η-.biazole) -1-yl)phenyl]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide N-({4-[(4-phenylphenyl))sulfonyl) ;]phenyl}methylpyrazole[3,4_b]0 than bite-5-anthracene N-({4-[(4-ethoxy-2-mercaptophenyl)sulfonyl]benzene Methyl-methyl-[3,2-c]pyridine-2-carboxamide N-{[4-(5-gas-3-methyl) butyl-2-ylphenyl) fluorenyl }-1Η-°Bizozolo[3,4-b]pyridine-5-carbamimidoxime-{[4·(1-propyl-1H-pyrazole-4-sulfonyl)phenyl]methyl }Thiopheno[2,3-c]n-pyridyl-2-carboxamide N-[(4-{[4-(ethylaminemethyl)phenyl)sulfonyl}phenyl)methyl]imidazole And [l,2-a]pyrimidine-6-nonylamine N-{[4-(4-indolyl)pyridin-3-sulfonyl)phenyl]methyl}imidazo[i,2-a ° ° pyridine-6-formamide N-[(4-{[3-(methoxymethyl)benzene]sulfonyl}})methyl]thieno[2,3-c]pyridine- 2-carbamamine N-({4-[(2-butoxy-5-gasbenzene)sulfonyl]phenyl} Furfuro[2,3-c]pyridine-2-cartoamine N-({4-[(3-Den-4-propoxybenzene)sulfonyl]phenyl}indenyl)_m_n ratio And [3,2-c]pyridine-2-carboxamide N-({4-[(2-methyl.4.propoxybenzene)sulfonyl]phenyl}indolyl)furan[2, 3-c]pyridin-2-decylamine N-[(4-{[5-fluoro-2-(hydroxyindenyl)benzene]sulfonyl fluorenylphenyl)indolyl]imidazo[1,2-a ]°密咬-6-甲甲胺158436.doc -100- 201215609 N_[(4-{[3-(methoxymethyl)benzene]sulfonyl}phenyl)methyl]furan[2, 3-c]pyridine_2_carbamamine N-{[4-(5-methoxy). Pyridin-3-sulfonyl)phenyl]methyl}imidazo[,2-a]pyridin-6-carbamimidoxime-({4-[1-methyl-3-(trifluoromethyl))iH -n-biazole-4-sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine-6-carboxamide N-[(4-{[4-(2-mercaptopropoxy) Benzene phenyl sulfonyl}phenyl)methyl] oxazolo[l,2-a]pyridine-6-carboxamide• N-[(4-{[2-(benzyloxy)-5-(three Fluoromethyl)phenyl]sulfonyl}phenyl)methyl]-1Η-° ratio p[3,2-c]° ratio biting-2-amine N-{[4-(cyclohexane) Sulfhydryl)phenyl]methyl}_1Η_πpyrolo[3,2_c]tiit pyridine-2-carboxamide 1^-[(4-{8-thiatricyclo[7.4.〇.〇2,7 Tridecyl-1(13),2,4,6,9,11-hexene-6-sulfonyl}phenyl)methyl]thieno[2,3_c]pyridine-2-carbamamine&gt; 1-({4-[(3,4-Difluorophenyl)sulfonyl]phenyl}methyl)thieno[2,3_^. Than 2-mercaptoamine • Ν-{[4-(phenylsulfonyl)phenyl]indolyl hydrazine isoquinoline _7_ amidoxime-[(4-{[3-fluoro-4- (2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyridine-6-carboxamide N-({4-[(2) -butoxy-5-chlorophenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-nonylamine N-[(4-{[4-fluoro-3- (trifluoromethyl) phenyl]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-indole amine N-{[4-(5-methylthiophene-2- Sulfhydryl)phenyl]methyl)thieno[2,3_c] 158436.doc -101· 201215609 Pyridine-2-carboxamide N-({4-[(2,6-dioxabenzene)sulfonyl) Phenyl)methyl)thieno[23c] 0 is a ratio of 2-carbamoylamine N-[(4-{[2-methyl_4-(ih-carbazole-i-yl)benzene]sulfonate } phenyl) fluorenyl] 11 futino[2,3-c]n than bite-2- 曱 Ν Ν -{[4-(μ-[(η than bite + base) Styrene) phenyl]methyl b 1 Η-pyrazolo[3,4-b]pyridine-5-formamide N- {[4-(quinoline-8-sulfonyl)phenyl]fluorenyl} Thieno[2,3_c]pyridine_2-carboxamide N-({4-[6-(morpholine-4-isocarbazin-3-yl)phenyl}indolyl) furan[2] ,3-c]pyridin-2-nonylamine N-({4 -[(4-butoxy-3-trifluorobenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide-({4-[(3·) Ethoxy-4-fluorophenyl)sulfonyl]phenyl}indolyl]imidazo[l,2-a]pyridine-6-decylamine ν·[(4-{[3-fluoro-5-( N-r-pyridyl-i-yl)phenyl]sulfonyl}phenyl)indenyl]thieno[2,3-c]&quot;bipyridine-2-carbamamine N-({4-[(4- Chlorobenzene)sulfonic acid]phenyl}indenyl)_1H·.pyrolo[3 2_c]pyridine-2-carboxamide N-{[4-(6-methylpyridazine-2-sulfonyl) Phenyl]fluorenyl}furo[2,3-c]pyridine-2-carbamimidoxime-{[4-(1-methyl-1H-carbazole-4-sulfonyl)phenyl]methyl }_l,3-Benzo-°°°--6-cartoamine-[(4-{[3·(difluoromethoxy)benzene]sulfonyl}phenyl)indolyl]imipine and 158436 .doc • 102· 201215609 [l,2-a] mouth bite-6-cartoamine N-({4-[(3-fluoro_5·甲其其·,廿Τ暴本)嶒醯基]benzene } 甲基 甲基 甲基 [ [ 3 3 3 3 3 3 3 - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - ) Η ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( 四 四 四 ( ( ( ( ( ( ( ( Ding-6-cartoamine n_({4-[(2,3·dimethylpreparate w T-milk basic) sulfomethoxy]phenyl}indolyl)furo[2,3-c]» than bite-2 -Procarbazine 2 (via fluorenyl) benzene] is based on phenyl)methyl]. Meter. Sit and [l,2-a]»bipyridine_6_carbamamine N-({4-[(5-secondbutyl-2-methoxybenzene)sulfonyl]phenyl)methyl)thiophene And [2,3-c]pyridine·2_ amidoxime-[(4-{[3-(indolyl)-yl)benzene]sulfonyl}phenyl)indolyl]·1Η_吼[3,2-c]pyridine-2-carbamimidoxime-[(4·{[3-fluoro-4-(1Η-oxazol-1-yl)benzene]]] Base]·1Η-η ratio of oxazolo[3,4-b]° to bit-5-carbamamine N-({4-[(2-chloro-4-fluorobenzene))]phenyl}吱)[2,3-c] 0 than bite-2-cartoamine N-({4-[(2-fluoro-3-methylphenyl)sulfonyl]phenyl}indolyl)imidazole And na]0 than bite-6·carbamamine N-{[4-(2,6-dimethoxy&quot;bipyridin-3-sulfonyl)phenyl]indolyl}imidazo[l,2 -a]D-precipitate-6-cartoamine-{[4-(2Η-1,3-benzodioxole-4-sulfonyl)phenyl]-methyl-103-158436.doc 201215609-based furan [2,3-cJ-pyridine-2_f amidoxime ({4·[(2,3-difluorophenyl)sulfonyl]phenyl}methyl)-1Η-η-pyrazolo[3 '4-b]pyridine carbenamide methylpropoxy)phenyl]sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine_6-formamide N_[(M[3- Fluor-5-decapyridinium + base) Continuation of phenyl] phenyl) fluorenyl] oxazolo[l,2-a]pyrimidine _6-methalamine fluoride _4_propoxy benzene) sulfonyl] phenyl hydrazino) imidazo[ 1'2-a] pyrimidine _6_nonylamine N [(4 {[4-(4-methylpiperazin-1-yl)benzene]sulfonyl}phenyl)methyl]furan[2 , 3-c] ton bite 2 - methotrexate · ({4 · [(3-ethoxy-2-phenothiphenyl) sulfonyl] phenyl) fluorenyl) furan [2, 3-c Pyridine_2_carbamid butylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-carboxamide N {[4 (stupid) benzene Methyl}-3-bromo-1Η-° ratio of [3,2-c]° to bite-2·cartosamine N [(4丨6-azamidazo[l,2-a]pyridine -3-sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine-6-nonylamine N_({4_[(2,6-dioxabenzene)sulfonyl]phenyl}- Furfuro[2,3-c] 0 ratio biting-2-cartoamine N_{[4_({3-[(dimethylamino)methyl)] phenyl) sulfonyl) phenyl]methyl }Μ和u'2-a]Blowing _6_carbamamine N_({4-[(2-fluoromethoxyphenyl)sulfonyl]phenyl}methyl)imidazolium 158436.doc 201215609 [l ,2-a]D than bite-6-cartoamine N-[(4-{[2-methoxy_5_(trifluoromethoxy)benzene] hydrazinyl)phenyl) Imidazo-Ha]pyridine-6-carbamidamine·{[4-(2-methyl-decahydrothiazylsulfonyl)phenyl]nonylbimidazo[l,2-a]pyrimidine_6_ Methotrexate N_{[4-(morphine _4_ 醯 醯 ))) phenyl]methyl} 嗟 并 [a small ratio D-di-2-carnitine, n_[(4_{[3-( 2 曱 氡 氡 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Methoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-indole N-({4-[(3-methoxyphenyl)sulfonyl] Phenyl}fluorenyl)_ih_吼[3,2-c]bite _2-armamidine-{[4-(1-propyl_1H-pyrazole-4-sulfonyl)benzene Furan[2,3-c]pyridine-2-carbammine N-{[4-(dimethyl-1&gt;3_thiazole·5_sulfonyl)phenyl]methylhydrazine Imidazo[l,2-a]pyridine·6-carbamimidamine n_({4-[(2-methyl-4-indolyl)sulfonyl]phenyl)indolyl)_1Hpyrazolo[ 3,4-b]pyridinecarboxamide Ν·({4-[(3-fluoro-2-methoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine_ 2_Metformamide N-({4-[(4.chloro-2-methoxybenzene)sulfonyl]phenyl}methyl)imidazo[1'2-a]pyrimidine_6-decylamine Ν·({4-[(2,3) -dimethoxybenzene)sulfonyl]phenyl}methyl)thiophene 158436.doc 201215609 [2'3-c]pyridine_2_formamide fluoro-2-methoxybenzene) Phenyl}methyl) oxazole and n'2-a]pyrimidine_6-formamide N_({4-[(5-chloro-2-ethoxyphenyl)sulfonyl]phenyl}methyl) Imidazo[1'2-a]pyrimidine_6-formamide N [(4-{[2_气_5·(trifluoromethoxy)benzene]sulfonyl phenyl)indolyl] Sit and [l,2-a]pyrimidine_6_methalin Ν_({4-[(4-phenylphenyl)sulfonyl]phenyl}methyl)imidazo[12a]pyrimidine-6-A N-({4-[(2-butoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamide Ν-{ [4-(2Η-1,3-benzodioxol-5-anthracene)phenyl]methyl}thieno[2,3-c]pyridine-2-carbamidine-( {4*·[(2,5 -.一气本) 靖的基]本基}曱基)-1 Η-® than 嗤[3,4-b]0 to 11 dimethylformamide N-[( 4-{[4-(lH-&quot;Bizozol-1-yl)benzene]sulfonyl}phenyl)methyl]furo[2,3-c]pyridine-2-carboxamide N-( { 4-[(2,5-dimethoxyphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-cartoamine N-{[4-(5-A oxygen ° 咬 ) ) ) ) ) ) ) ) ) ) ) ) ) ) 苯基 苯基 苯基 苯基 苯基 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 [methyl]-salt and [i,2-a]° than pyridine-6-formamide N-[(4-{2-[ethyl(indenyl)amino]-1,3.thiazole_ 5·sulfonyl}phenyl) 158436.doc -106- 201215609 methyl]-1H-pyrazolo[3,4-b]pyridine-5-formamide N-[(4-{[4-( Trifluoromethyl)benzene]sulfonyl}phenyl)indenyl]furo[2,3-c]pyridin-2-indole N-({4-[(3- gas-2-mercaptobenzene) Sulfo]phenyl]indolyl]thieno[2,3-c]pyridine-2-carboxamide N-({4-[(3,5-dimercaptophenyl)sulfonyl]phenyl }曱))thieno[2,3-c]° ratio nitramide N-[(4-{[4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl] -1H·-Birado[3,2-c]pyridine-2-carboxamide N-{[4-(2-methyl-2H-indazole-5-sulfonyl)phenyl]fluorenyl} Imidazo[1,2-a]pyridine-6-formamide N-[(4-{[3- gas-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]furan [2,3-c]pyridine-2-f decylamine N-{[4-(2-mercapto-2H-indazol-5-sulfonyl)phenyl]methyl}thiophene [2,3- c] Pyridin-2-decylamine N-{[4-(quinolin-3-sulfonyl)phenyl] Methyl}imidazo[l,2-a]pyrimidin-6-nonylamine N-[(4-{[3-(didecylaminesulfonyl)benzene]sulfonyl}phenyl)indolyl] Furan[2,3-c]. Bis-2-carbamide N-({4-[2-(3-fluorophenyl)-1,3-thiazole-4-sulfonyl]phenyl}indolyl)thieno[2,3- c]pyridine-2-carbamide 5-hydroxy-N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)indolyl]-1H-indole-2 -carbamamine N-({4-[(2-p-phenyl)sulfonyl]phenyl}indolyl)thieno[2,3-cp-pyridyl- 158436.doc -107- 201215609 2-carboxamide Ν-{[4-(1-Benzo-ephedo-7)-phenyl]indolyl}°Septo[2,3-c] n than 2-mercaptoamine N-( {4-[(3 -Ternylphenyl)] hydrazino]phenyl}indolyl)imidazo[1,2_a]0 than bite_6-anthracene N-({4-[(3- Chloro-5-methoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N-[(4-{[3-(prop-2-) Phenyl]sulfonyl}phenyl)methyl]imidazo[a]-bite-6-cartoamine N-({4-[(4-chloro-2-ethoxyphenyl)sulfonyl]benzene Methyl imidazo[l,2-a]acridin-6-formamide N-({4-[(3-methoxyphenyl)sulfonyl]phenyl}methyl)thiophene [ 2,3_c] D is more than 2-carbalamine N-({4-[(3-cyanobenzene)sulfonyl]phenyl}methyl)imidazo[12^]pyrimidine-6- formazan Amine N-({4-[2-(phenylsulfonyl)ethyl]phenyl}methyl Bisolo[3,2·c]pyridine-2-carboxamide N-({4-[(3-chloro-5-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[a]pyridine -6-carbamamine N-[(4-{[5-fluoro-2-(hydroxymethyl)benzene]sulfonyl phenyl)indolyl]_1H_pyrrolo[3,2-c]pyridine-2 - amidoxime-{[4-(1-methyl-1H.carbazole·4·sulfonyl)phenyl]methyl}imidazo[l,2_a]pyridine-6-carboxamide N-( {4-[(3-Chloro-2-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[12_ 158436.doc -108· 201215609 a]0 than bite-6-cartoamine N-( {4-[(3,5-Dichlorophenyl)sulfonyl]phenyl}indolyl)thieno[2,3_c]pyridine-2-carboxamide N-{[4-(4-methylthiophene- 2-sulfonyl)phenyl]methyl}imidazo[i,2-a]pyridin-6-carboxamide 1^-({4-[(2-fluoro-4-methoxybenzene)sulfonate)比 - ) ) ) ) ) ) 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 2,3-c]n ratio 曱醯-2-nonylamine # N-[(4-{[3-(morpholin-4-yl)benzene]sulfonyl}phenyl)methyl]imidazo[l , 2-a]pyridine-6-nonylamine N-({4-[2-(3-fluorophenyl)-1,3-indole). -4-Continuation of thiol]phenyl}indolyl] oxazolo[l,2-a]pyridine-6-nonylamine N-({4-[(5-fluoro-2-methoxybenzene)) Sulfhydryl]phenyl}methyl)_1H-oxazolo[3,4-b]pyridine-5-carboxamide N-[(4-{[3-(decylamine)methyl)benzene]sulfonate醯 }}phenyl)indolyl]imidazo[l,2-a]pyrimidine-6-carboxamide N-{[4-(2,6-dimethoxypyridine_3_sulfonyl)benzene曱 曱 比 比 并 3 [3,4-b]pyridine-5-carbamimidoxime-[(4-{[4 曱 oxy-2-(trifluoromethyl) benzene] hydrazino} benzene Furyl [2,3-c]pyridine-2-carboxamide N-{[4-(acridin-3-sulfonyl)phenyl]methyl}imidazopyridine _ 6-曱N-({4-[(4-cyclohexylbenzene)sulfonyl]phenyl}indolyl)imidazo[丨2]pyrimidine-6-carboxamide 158436.doc -109- 201215609 ν·( {4-[(4-Butoxyphenyl)sulfonyl]phenylindenyl)1Η_0pyrho[3,2_c]acridin-2-carboxamidopyrrolidin-1-yl)-1, 3-thiazole-5-sulfonyl]phenyl}methyl) thieno[2,3-c]pyridine_2-carbamimidoxime ({4-[(4-phenylphenyl)sulfonyl]] Phenyl}fluorenyl)-1Η-° ratio 咯[3,2-c]° pyridine-2-carbamimidoxime _[(4·{[3-(diethylaminecarbamyl)_5_fluoro Sulfhydryl phenyl)methyl]imidazo[l,2-a]pyrimidine·6-carbamimidoxime_{[4-(5·methoxy D-pyridyl-2-sulfonyl)phenyl ]methyl}imidazo[a]° than pyridine-6-nonylamine N-[(4-{[3_fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl} Phenyl) fluorenyl] benzo[2,3-c]n than pyridine-2-carbamimidoxime [(4-{[2·(2,2,2-trifluoroethoxy)-4-) (three-methyl) benzene] styrene} phenyl)methyl]imidazo[l,2-a]n than pyridine-6-formamide N-[(4-{[3-gas-5- (trifluoromethyl)benzene]sulfonyl}phenyl)methyl]_1H_pyrrolo[3,2-c]pyridine-2-carbamimidoxime-[(4-{[4_(4·ethoxy) Phenyl)benzene] continued fluorenyl}phenyl)methyldoxime^piro[3,2-c]pyridine_2-carbamimidamine N-({4-[(3-phenylene)sulfonyl) Phenyl}methyl)_1H_pyrazolo[3,4_b] ° ratio -5-formamide N_({4-[(5-chloro-2-alkylbenzene) hydrazino]phenyl丨曱基)咪. Sit and [1 a]. Bipyridine-6-nonylamine N_({4-[(3-fluoro-4-decyloxybenzene) hydrazino]phenyl)methyl)_1h_d-pyrazolo[3,4-b]pyridine_5 _Metamine 158436.doc 110· 201215609 N_({4-[(3-Fluoro-4-propoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine_2 _ decylamine N-({4-[(4-decyloxy-2-methylphenyl)sulfonyl]phenyl)methyl)_1Η_〇Λ lorata[3,2-c]pyridine-2 - amidoxime-{[4-(1-methyl-1H-indazol-5-sulfonyl)phenyl]indolyl}imidazo[l,2-a]pyrimidine-6-carboxamide N_ {[4-(6-Methylpyridin-3-sulfonyl)phenyl]indolyl}_ih-pyrrolo[3,2-c]pyridine-2-carbamamine • N-({4-[( 2-phenoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c] &quot;pyridin-2-decylamine N-[(4-{[3-fluoro-5- (2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)indenyl]thieno[2,3-c]pyridine-2-carboxamide N-({4-[(3) -ethoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3-c] ° than 0--2 -carbamamine Ν[[4-{[3-(1Η-η ratio spit -1-yl)phenyl]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine·2-formamide® Ν-({4-[2-(pyrrolidine_1-yl) )_ι,3_thiazole_5_sulfonyl]benzene }曱基)-1Η-°Bizozolo[3,4_b]pyridine_5_carbamimidoxime·{[4·({3-[(2-methylpropyl)aminemethanyl]benzene}sulfonate Mercapto)phenyl]methylcereno[2,3-c]pyridine-2-carboxamide N_({4-[(4-methoxyphenyl)sulfonyl]phenyl}fluorenyl) furan And [2,3-c] 0 is more than 唆-2-cartoamine chloride·2_(prop-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a] Pyrimidine _6_formamamine 158436.doc 201215609 N-({4-[(2,4-dimethylphenyl)sulfonyl]phenyl}methyl)-1Η-η-pyrazolo[3,4- b]pyridine-5-carbamamine N-({4-[6-(?) _4-yl) π ratio biting-3-3⁄4-bristyl]phenyl}•曱基米β sits and [l,2 -a]pyrimidine-6-carbamimidoxime-[(4-{[3-(2.methylpropoxy)benzene]sulfonyl}phenyl)indolyl]·1Η-吼 并[3, 2-c]pyridine-2-guanamine N-({4-[(4-fluoro-2,5-dimethylphenyl)sulfonyl]phenyl}methyl)thieno[2,3-c Pyridine-2-carboxamide N-[(4-{[2-gas-5-(trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl 1H-pyrrolo[3,2-c Pyridine-2-carboxamide N-({4-[(2-methoxyphenyl)sulfonyl]phenyl}methyl)furo[23_c]pyridine-2-carboxamide N-[(4 -{[3-(piperidin-1-yl)benzene] Mercapto}phenyl)methyl]furo[2,3-〇]° ratio 2-carbamide N-({4-[(4-phenylphenyl)sulfonyl]phenyl}methyl Furan-[2,3 c] n-pyridyl-2-carboxamide N-({4-[(2-methoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[[] Mouth bite-6-carbamamine N-({4-[(3-ethoxy.4.fluorobenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyrimidine-6- Methotrexate-({4-[1-(3-Phenylphenyl)·1Η"Biazole_4•sulfonyl]phenylindolemethylseceno[2,3-c]pyridine-2- Amidoxime-({4·[(2-gas-4.methylbenzene) hydrazino]phenyl)methyl)_1h_d than s-[3,2-c]pyridine-2-carboxamide 158436 .doc •112- 201215609 N-({4-[(2-Fluoro-3-methylphenyl)sulfonyl)phenyl}indolyl)imidazo[1,2-a] °密17定-6- Methionine N-{[4-〇bidine_2_sulfonyl)phenyl]indolyl]furan [2,3-cp than pyridine-2-decylamine N-({4-[(3) -butoxybenzene)sulfonyl]phenyl}indolyl)-1Η-°pyrho[3,2-c]pyridin-2-decylamine N-({4-[(3,4-di) Chlorobenzene)sulfonyl]phenyl}methyl)-1Η-η is more than 嗤[3,4-b]pyridine-5-formamide _ N-({4-[(2,4-dioxine) Sulfhydryl]phenyl}fluorenyl Thieno[2,3-c]pyridin-2-decylamine N-[(4-{[2-fluoro-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H -pyrrolo[3,2-c]pyridin-2-decylamine N-[(4-{[2-(dimethylaminocarbamimidino)benzene]sulfonyl}phenyl)methyl]imidazo [l,2-a]acridine-6-formamide N-({4-[(2-chloro-5-decyloxyphenyl)sulfonyl]phenyl}methylpyrazole[3,4 -b]pyridine-5-carbamamine® N-{[4-(4-methylheptan-3-sulfonyl)phenyl]decyl}furo[2,3-c]pyridine-2- Methionine N-({4-[(4-butoxy-3-fluorobenzene)sulfonyl]phenyl}methyl)thieno[2,3-c]pyridine-2-carboxamide N- ({4-[(3-ethylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]. Bipyridine-2-carboximine N-[(4-{[3-fluoro-5-(2-mercaptopropoxy)benzene]sulfonyl}phenyl)indolyl]furan[2,3- c]pyridine-2-carbamide 158436.doc -113· 201215609 N_({4_[(3-Ga-4-methoxybenzene)sulfonyl]phenyl}methyl)thieno[2,3〇 Bisidine 2-carboamine N_({4_[(3- gas-4-decyloxybenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridinecarboxamide N_[ d{[2-(Trifluoromethoxy)benzene]sulfonyl}phenyl)indolyl]imidazo[1'2 a]pyrimidinecarbamamine N_({4_[(2-ethoxy-6-) Fluorobenzene)sulfonyl]phenyl}methyl)furo[2,3-C]°pyridin-2-carbamide~({4~[(3'5-difluorophenyl)sulfonyl] Phenyl}fluorenyl)imidazo[l,2-a]. Bipyridine-6-formamide N-[(4-{f4^U4-fluoro-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)methyl]imidazo[1, 2-, pyridine-6-carbamamine (morpholine-4-yl) (1-pyridyl_3_sulfonyl)phenylhydrazinemethyl)furo[2,3-c]pyridinium N- ({4_[(2-phenoxyphenyl)sulfonyl]phenyl}methyl)_1Η_β is more than [3,2-c]» than bite_2_carbamamine N_[(4-{[3 -Chloro-5-(diethylamine-mercapto)benzene]sulfonyl}phenyl)indolyl]0-f-[2,3-c]pyridinium.曱醯-2-decylamine n-({4-[(2-fluoro-3-methylphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamidine Amine ν·({4-[(3-fluoro-2-indolylbenzene)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide N-[( 4-{[3-(ethanesulfonyl)benzene]sulfonyl}phenyl)methyl]-1H-&quot;pyrolo[3,2-c]pyridine-2-carboxamide 158436.doc •114· 201215609 Ν-{[4-(1,4-Dimethyl-1H-imidazol-2-sulfonyl)phenyl]methyl}imidazo[1,2-a]pyrimidin-6-formamidine Amine N-[(4-{[4-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl]-1H-indazolo[3,4-b]pyridine-5-A Indoleamine N-({4-[(3-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6-carboxamide N-({4-[ (4-fluoro-3-indolylbenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridine-2-carboxamide• N-[(4-{[5-fluoro -2-(hydroxyindenyl)benzene]sulfonyl}phenyl)indolyl]furo[2,3-c]pyridine-2-carbamimidoxime-{[4-(1-mercapto-1H-吲哚-2-sulfonyl)phenyl]fluorenyl}-1Η-. Bisazo[3,4-b]pyridine-5-carbamide N-({4-[(4-chloro-2-methylphenyl)sulfonyl]phenyl}methyl)furan[2, 3-c]pyridin-2-decylamine N-({4-[(2,6-dichloro-3-indolylbenzene)sulfonyl]phenyl}methyl)thieno[2,3-indole ] ° ratio. -2--2-Mercaptoamine• N-({4-[(2,5-Dioxaoxybenzene)sulfonyl]phenyl}indolyl)imidazo[1,2-a]°^°- 6-Protonamine N-({4-[(3-fluoro)sulfonyl]phenyl}fluorenyl)thieno[2,3-c]°-pyridin-2-nonylamine N-({ 4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}indenyl)thieno[2,3-c]pyridin-2-ylamine]^-({4-[2 -(°bipyridin-1-yl)-1,3-thiazol-5-sulfonyl]phenyl]methyl) imi. Sit and [1,2-a] ° than bite-6-amide 158436.doc -115 - 201215609 Ν·[^{[3·(2,2,2-trifluoroethoxy)benzene]sulfonate }}phenyl)indolyl]furo[2,3_c]pyridine-2-carboxamide N_{[4'(didecyl-1,3-thiazol-5-sulfonyl)phenyl]methyl} Furano[2,3-c]° than pyridine-2-carboxamide N_U4-(6-decyloxy D-pyridyl-2-sulfonyl)phenyl]fluorenyl}imidazo[12_a] ° -6-carbamamine N'[(4-{[3-|L-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]_1H_ 0 is 0 and each [3,2- c]. Specific bite 2_carbamamine N G4~[(2,4,6-tridecylbenzene)sulfonyl]phenyl)indolyl)_1Η_pyrrolo[3,2-c].比 _2 _ _ _ _ 醯 n n _ { { { { { { _ _ _ { { _ _ _ _ _ _ _ _ _ { _ _ _ _ _ _ _ _ _ _ _ _ _ Indoleamine N-U4-[(4-chloro-3-methoxyphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine·2·carbamamine-5-曱Benzo)sulfonyl]phenyl}indenyl)thieno[2,3_c]° ratio bit-2-amine Ν·[(4-{[3-(trifluoromethyl)benzene]sulfonate }}phenyl)methyl]_1H_0pyrho[3,2-c]»pyridinyl-2-deamine N ((M(2-cyanobenzene) fluorenyl)phenyl}methyl).塞 并 [2,3 〇 〇 〇 ° 定 -2- 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲[l,2-a] bitter winter formazan N-[(4-{[4 r - ^ , U (difluoromethyl)-3-fluorobenzene]sulfonyl}phenyl)indolyl]imidazole And t1'2 a]pyrimidine guanamine 158436.doc 201215609 Ν-{[4-(1-methyl-1H-.biazole-4-sulfonyl)phenyl]fluorenyl}furan[2,3 -c]pyridine-2-carboximine N-{[4-(morphothia-4·sulfonyl)phenyl]methyl}_1H-pyrazolo[3,4_b]pyridine-5-carboxamide Ν-[(4-{[2·(diodecylaminomethyl) phenyl) sulfonyl}phenyl)methyl]imidazo[l,2-a]pyrimidine -6-carbamamine N-({4-[(3-fluoro-5-methoxyphenyl)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine-2-carboxamidine Amine φ N-({4-[(4-methoxy-2-indolylbenzene) hydrazino]phenyl}methylf-[2,3-c]pyridine-2-carboxamide N- [4-(phenylsulfonyl)phenyl] ° pyridine-3-carbamide N-({4-[(2-methyl-4-propoxybenzene)sulfonyl]phenyl}methyl Thio[2,3-indole]. N-({4-[(3-ethoxy-4-fluorophenyl)sulfonyl]phenyl}methyl)furan [2,3-c]pyridine-2-carboxamide N-{[4-(phenylhungyl)phenyl]fluorenyl}-lH-flavored [4,5-c]0 than 唆-2 -® carbamide n-[(4-{[2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2-methyl Indoleamine N-{[4-(6-methoxynaphthalene-2-sulfonyl)phenyl]methylhydrazine thieno[2,3c]pyridine-2-carboxamide ^-{[4-(stupid Continued base) base] 曱基}_3-( &lt;3 ratio bite_4_base)_1-only&gt; 嗤·· 5-carbamide N-({4-[(2-ethylmercaptophenyl)sulfonyl]phenyl}methyl)furan And [2,3_c] 158436.doc •117- 201215609 ° ratio bite-2-formamide N-({4-[(4-methanesulfonylbenzene)sulfonyl]phenyl}indenyl)_1Η· «Bizozolo[3,4-b]pyridine-5-nonylamine N-{[4-(4-methyl&quot;pyridin-2-sulfonyl)phenyl]indolylfuran[2] 3_c] Pyridin-2-carboxamide N-({4-[(3-fluoro-4-methoxybenzene)sulfonyl]]indolyl)imidazo[l,2-a]pyrimidine-6 -Procarbamide N-[(4-{[3-fluoro-4-(trifluoromethoxy)benzene]sulfonyl fluorenylphenyl)indenyl]_ 1Η-°Bilo[3,2-c 0 to 0-butyrylamine 1^-({4-[(2-ethoxy-4-fluorobenzene)sulfonyl]phenyl}fluorenyl)-1]^_11 ratio 咯[3 ,2-c]pyridin-2-decylamine N [(4-{[2-(dimethoxymethoxy)benzene]] fluorenyl phenyl)methyl]β-senteno[2,3-c Pyridine-2-carboxamide N-({4-[(4-ethoxy-2-methylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyrimidine-6 - indoleamine N-({4-[(6-chloro-2_fluorobutyromethylphenyl)indolyl]phenyl)pyrano[2,3-c]pyridine·2-carbamimidoxime -({4-[(5-气-2_甲甲Sulfonic acid]phenyl hydrazine methyl)imidazo[12_a]pyridine-6-nonylamine N-{[4-(indolyl-2-sulfonyl)phenyl]methyl}imidazo [12_a]t^pyridine_6-carbamimidodimethoxy_4-methylbenzene)sulfonyl]phenyl}methyl)furo[2,3-c]pyridine_2-formamide N -({4-[(2-phenylethane)sulfonyl]phenyl}indolyl)_1H_吼 并 158436.doc • 118· 201215609 [3,2-c]pyridine·2-carbamide Ν-({4-[(4-Fluoro-3-methylphenyl)sulfonyl]phenyl)methyl)thieno[2,3_c].咬2-曱醯胺曱醯-{[4-(1-methyl·1Η_carbazole_4_sulfonyl)phenyl]methyl b 1Ηpyrrole[3,2-c]Dfcbn- 2-branched amine N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]thieno[2,3-c]pyridine-2- Methotrexate-{[4-(1-indolyl-1H-indazole-6-sulfonyl)phenyl]indolyl lHpyrazolo[3,4-b]° than bite-5-A Indoleamine N-[(4-{[4-(yl)methyl)benzene]sulfonyl phenyl)indolyl]thieno[2,3-c]pyridine-2-carboxamide N-({ 4-[6-(3'4-difluorophenylpyridin-2-ylsulfonyl]phenylindolemethyl)furo[2,3-c]pyridine_2-carbenamide N-({4 -[(3-mercaptophenyl)sulfonyl]phenyl)indolyl)_1Η_πpyrho[3,2·c]pyridin-2-decylamine N-({4-[(3-fluoro-5) -mercaptophenyl)sulfonyl]phenyl}indenyl)imidazolium a]pyridin-6-carboxamide N-({4-[(3,5-dioxaoxy)sulfonyl]phenyl Mercapto) imidazo[l,2-a]pyrimidin-6-carboxamide N-[(4-{[3-(morpholine-4-yl)benzene]sulfonyl phenyl)methyl] ; 13 benzo. N-({4-[(3-ethoxyphenyl))sulfonyl]phenyl}methylpyrrolo[3,2-cp than pyridine-2-decylamine ν ·(Η-[(3·Chloro-5-methoxybenzene)sulfonyl]phenyl}indenyl) 158436.doc -119- 201215609 and [3,2-c]pyridine-2-carboxamide N -({4-[(4-Ga-2-methylphenyl) hydrazino]phenyl}fluorenyl)·1Η_0 咯[3,2-c]pyridine-2-carboxamide N-{[ 4-({4-[p-pyrrolidinyl-1-yl)carbonyl]phenyl}sulfonyl)phenyl]methyl} 0-propano[2,3-c]»-pyridin-2-ylamine N-[(4-{[3-(Methoxymethyl)benzene]sulfonyl)phenyl)indolyl]_1Η_^ oxo[3,2-c]pyridine-2-carboxamide Ν-{ [4-(1-Methyl-1HH7_Continuoyl)phenyl]methyl}1H吼 并[3,2-〇]° than bite-2 - 曱 Ν Ν -[(4-{[3 -(1Η"specific than sialyl) benzene] continuation of the base} phenyl) methyl] _ _ 〇 咯 咯 [3, 2-c] pyridine -2- oxime Ν - { [4- (1 - mercapto-lH, n-mercapto) phenyl]methyl-iH_n-pyrolo[3,2-c]pyridin-2-decylamine N-({4-[(4-cyanobenzene)sulfonate) Mercapto]phenyl}methyl)_1Η_η比比和[3,2_ c] 0 is 0-but-2-carboximine·{[4_(2,3-dihydro-1-benzo-folly) 7_continued base) phenyl]methyl b-pyrrole And [3,2-c]pyridine-2-carboxamide N-({4-[(2-carbophenyl)sulfonyl]phenyl}indenyl) ΐΗββpyrho[^ c]pyridine-2 -carbamamine ' 5-N-({4-[(3,5-: fluoro)) hydrazino] phenyl) π ) · 2 2 2 2 2 ( ( ( ( ( [(4-Fluoro-3·decylbenzene) continuation of the base] phenyl} A rape rice saliva and na] 0 than bite - &lt;6-branched amine' Ν_{[4·(phenyl phenyl) phenyl] thiophene bite I amide 158436.doc • 120- 201215609 N-({4-[(4-曱-oxygen) 3-methylphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridine-6-carboxamide N-({4-[(4-decanesulfonylbenzene) Sulfo]phenyl]methyl)imidazo[l,2-a]pyridine-6-formamide N-({4-[(2-cyanophenyl)sulfonyl]phenyl}fluorenyl) )-1Η-° 嗤[3,4-b]pyridine-5-cartoamine N-({4-[(3-曱oxy-4-methylphenyl)sulfonyl]phenyl} Base)-1Η-«Bizozolo[3,4-b]pyridine-5-decylamine • N-[(4-{[3-fluoro-4-(1Η-indazol-1-yl)benzene] Sulfhydryl}phenyl)indolyl] ° rice saliva [1,2-a] ° than bite-6-decylamine]^-{[4-(211-1,3-benzodioxane) Pentene-5-sulfonyl)phenyl]methyl}imidazo[l,2-a]° pyridine-6-nonylamine N-({4-[(2-p-phenylene)sulfonyl] Phenyl}fluorenyl)-1Η-η-pyrazolo[3,4-b]pyridine-5-carboxamide N-({4-[(4-fluoro-2,5-dimethylphenyl))sulfonate Base]phenyl}indenyl)-1Η-. Sit and [3,4-b] ° than bite-5-carbamamine • N-({4-[(2,5-dimethylphenyl)sulfonyl]phenyl}methyl)-1Η -indolozolo[3,4-b]pyridin-5-nonylamine N-({4-[(5-fluoro-2-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[ 1,2-a]. Specific bite-6-carbamamine N-[(4-{[2-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]imidazo[l,2-a]pyridine-6- Indoleamine N-({4-[(2-ethylmercaptophenyl)sulfonyl]phenyl}indolylpyrazolo[3,4-b]pyridine-5-carboxamide 158436.doc • 121 · 201215609 N-[(4-{[2-Mercapto-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3,4-b]pyridine-5 -Procarbamide N-({4-[(2-fluoro-6-decyloxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine-6-carboxamide N -{[4-(quinolin-8-sulfonyl)phenyl]indolyl}imidazo[1,2-ap-pyridyl-6-carboxamide N-[(4-{[4- gas-2 -(Trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-0 ratio. Sit and [3,4-b]° ratio bite-5-nonamine N-({4-[ (2,5-dimethoxybenzene)sulfonyl]phenyl}methylpyrazole φ and [3,4-b]pyridine-5-decylamine N-({4-[(4-fluoro-) 2-nonyloxybenzene)sulfonyl]phenyl}indenyl)-1Η-&quot;Bizozolo[3,4-b]pyridine-5-decylamine N-({4-[(2-B) Oxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]pyridin-6-carboxamide N-[(4-{[3-(trifluoromethyl)benzene]sulfonate } phenyl) fluorenyl imidazo[1,2-a]. Amine N-[(4-{8-oxatricyclo[7.4.0.02,7]tridecy-1(13),2,4,6,9,11-φhexene-6-sulfonyl} Phenyl)methyl]-1Η-.biazolo[3,4-b].pyridin-5-nonylamine 6-amino-N-({4-[(3,5-difluorobenzene)) Sulfhydryl]phenyl}indenyl)&quot;bipyridyl-3-decylamine N-({4-[(3-chloro-4-propoxyphenyl)sulfonyl]phenyl}methyl)- 1Η-η-biazo[3,4-b]pyridine-5-formamide N-[(4-{[4-曱oxy-2-(trifluoromethyl)benzene]sulfonyl}phenyl曱基]- 158436.doc -122- 201215609 1H-pyrazolo[3,4-b]pyridine-5-nonylamine N-({4-[(4-fluoro-3-methoxybenzene)) Sulfhydryl]phenyl}methyl bromide-recoordinated [3,4-b]pyridine-5-formamide N-({4-[(4-methoxy-2-methylbenzene)sulfonate Mercapto]phenyl}methyl)_1H^oxazolo[3,4-b]pyridin-5-nonylamine N-({4-[(3-ethylphenyl)sulfonyl]phenyl]methyl Imidazo[l 2 pyridine-6-nonylamine N-({4-[(4-ethylphenyl)sulfonyl]phenyl}methyl)imidazolium pyridine-6-nonylamine N-[ (4-{[4-Gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indenyl]. And [1,2-a]pyridine-6-carbamimidamine N-[(4-{[4-fluoro-2-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]1H_pyridyl Zoxa[3,4:b]pyridine-5-nonylamine N-[(4-{[3-(cyclopentylaminomethyl)phenyl]sulfonyl}phenyl)methyl]_ 1H- Pyrazolo[3,4-b]pyridine-5-formamide N-[(4-{[4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl] than olfactory 3,4-b]pyridine-5-nonylamine N-[(4-U2-(morpholin-4-ylmethyl) phenyl]sulfonyl}phenyl)indolyl]imidazo[l,2- a]pyridine-6-formamide N-({4-[(2-ethylphenyl)sulfonyl)phenyl}indolyl)_1H_D than salido[3,4_b]pyridine-5-carboxamide N-[(4-{[3-(propan-2-yl)benzene]sulfonyl}phenyl)methyl]imidazo[na]0 ratio -6-cartoamine N-({4- [(5-Tertibutyl-2-decyloxybenzene)sulfonyl]phenyl}methyl)imidate 158436.doc -123- 201215609 Oxazo[l,2-a]pyridine-6-carboxamide N-({4-[(4-mercaptophenyl)sulfonyl]phenyl}indolyl) imidazo[l,2-ap ratio bite-6-formamide N-({4-[(3, 4-Dimethoxyoxybenzene)sulfonyl]phenyl}indenyl)imidazo[1,2-a]. Ratio 0 to 6-carbamamine N-({4-[(2-fluoro-4-mercaptophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a]. Ratio 0 to -6-carbamamine N-{[4-(morphothia-4-sulfonyl)phenyl]methyl}imidazo[1,2-a] 吼-6-carbamamine N -({4-[(2-methylphenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-ap than indole-6-cartoamine N-({4-[(2-benzene) Oxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridin-6-carboxamide N-[(4-{[4-(morpholin-4-yl)benzene] Sulfhydryl}phenyl)indenyl]-1Η-η ratio. And [3,4-b]pyridine-5-carbamidamine N-({4-[(2-fluoro-3-indolyl)sulfonyl]phenyl}indolyl)imidazo[1, 2-a]. Ratio of 0 to 6-carbamamine N-({4-[(4-methoxy-2,5-dimethylphenyl)sulfonyl]phenyl}methyl)-1H-pyrazolo[3 4-b]pyridine-5-nonylamine N-[(4-{[2- gas-3-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl]-1H-. ratio. Sit and [3,4-b]0 than bite-5-carbamidamine-{[4-(1-methyl-1H-.pyrazole-4-sulfonyl)phenyl]methyl}-1Η - «Bizozolo[3,4-b]pyridine-5-nonylamine N-({4-[(3-ethoxy-4-fluorobenzene)sulfonyl]phenyl}methyl)-1Η -°Bimazole 158436.doc -124- 201215609 and [3,4-b] bite-formamide N_({4_[(4'5-difluoro-2-methoxybenzene)sulfonyl]benzene Methyl imidazo[l,2-a]. N-U4_[(2'4-dioxaphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a]. Ratio of bite-6-formamide N_({4_[(2'4-difluorophenyl)sulfonyl]phenyl}indolyl)imidazo[1,2-a] 0 to bite-6-cartoamine __{[4-(5·Methylthiophene-2-sulfonyl)phenyl]indolyl m_D-pyrazolo•[3,4-b]acridin-5-carboxamide n-[(4- {[5-fluoro-2-(hydroxymethyl)benzene]sulfonyl}phenyl)methyl]·1Η_pyrazolo[3,4-b]pyridine_5-amidoxime-[(4- {[4-(ethylamine-mercapto)benzene]-carsonyl}phenyl)indenyl]_1Η_ 0-pyrazolo[3,4-b]. N-({4-[(4-methoxy-3,5-dimercaptophenyl))sulfonyl]phenyl}indolyl 1H-pyrazolo[3,4- b] Pyridin-5-formamide N-[(4·{[3-fluoro-5-(2-methylpropoxy)benzene]] fluorenyl)phenyl)indenyl]_ • lH-η ratio嗤[3,4-b]0 than bite-5-anthracene N-({4-[(3-propoxybenzene))]phenyl}indolyl)_1H_ η-pyrazolo[3 , 4-b]pyridine-5-formamide N-( { 4 - [(2,4,5 - diindole basic) continuation]phenyl}methyl)_ih_〇 is more than 〇[3, 4-b]pyridine-5-nonylamine N-({4-[(2- gas-4-decyloxybenzene) hydrazino]phenyl}methyl)H_0-pyrazolo[3,4-b Pyridine-5-decylamine ({4-[(2,3,6-trimethoxybenzene) contigyl]phenyl}fluorenyl)_111_11 azole 158436.doc -125- 201215609 and [3, 4-b]pyridine-5-carboxamide N-[(4-{[2- gas-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-0 ratio. Sit and [3,4-b]0 than bite-5-formamide N-({4-[(3-fluoro-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-η Bisazo[3,4-b]pyridine-5-formamide N-({4-[(3-mercaptophenyl)sulfonyl]phenyl}indolyl) imidazo[1,2-aP ratio定定-6-Metaguanamine [-[(4-{[2-曱-oxy-4-(1Η-.bazol-1-yl)benzene]sulfonyl}phenyl)indolyl]imidazo[ 1,2_a]pyridine-6-nonylamine N-({4-[(5-ethylinden-2-yloxyphenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a Pyridine-6-nonylamine &gt;^-({4-[(4-chloro-2-methylphenyl)sulfonyl]phenyl}methyl)-111-. Bisazo[3,4-b]pyridine-5-carbamimidoxime [(4-{[3- gas-4-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1士°°°°[3,4-1)]. ratio. N-({4-[(2-phenoxyphenyl)sulfonyl]phenyl}methyl)-1Η-η is 嗤[3,4-b]pyridine-5- Indoleamine N-({4-[(4_gasbenzene)sulfonyl]phenyl}indolyl)-1Η-η ratio of oxazolo[3,4_b] °. N--5-carbamamine N-[(4-{[4-fluoro-3-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1H-pyridyl Zoxa[3,4-b]pyridine-5-carboxamide N-[(4-{[4-fluoro-3-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H -. Sitting at 0 and [3,4-b]° than sigma-5-methalin Ν-({4-[(2,4,5-tridecylbenzene)sulfonyl]phenyl}methyl) Imidazo 158436.doc •126- 201215609 [l,2-a]pyridine-6-formamide N-({4-[(2,3-difluoro-6-decyloxybenzene)sulfonyl]benzene }}methyl)-1Η-pyrrolo[3,2-c]pyridin-2-decylamine N-{[4-(quinolin-6-sulfonyl)phenyl]indolyl}imidazo[l , 2-a] acridine-6-nonylamine N-[(4-{[3-(trifluorodecyloxy)benzene]sulfonyl}phenyl)methyl]imidazo[l,2-a Pyridine-6-formamide N-({4-[(2-decyloxyphenyl)sulfonyl]phenyl}methyl)-1Η-η is indolo[3,4-b]pyridine-5 -carbamidine N-({4-[(4-fluoro-2-mercaptophenyl)sulfonyl]phenyl}fluorenyl)-1Η-° carbazino[3,4-b]° ratio 0 -5-Protonamine N-[(4-{[2,4-bis(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1Η-° ratio. Sit and [3,4-b]0 ratio. N-({4-[(3-fluoro-4-indolyl)sulfonyl]phenyl}indolyl)-[1,2-a]pyridine-6 - indoleamine N-({4-[(2,3-dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]° ratio biting-6-formamide N -({4-[(2-decyloxy-5-mercaptophenyl)sulfonyl]phenyl}indolyl)-1Η-°-pyrazolo[3,4-b]pyridine-5-carboxamide N-[(4-{[3-chloro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]-1H-pyrazolo[3,4-b]pyridine-5-oxime Indoleamine N-({4-[(4-chloro-3-fluorophenyl)sulfonyl]phenyl}indolyl)imidazo[l,2-a] 0 to π-des-6-carboxamide- ({4-[(3,5-Dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2- 158436.doc -127- 201215609 a]0 to 0 -6 - Amine N-[(4-{[4-(2-methylpropoxy)benzene]] phenyl)methyl]-1 Η-. Sit more than 0 and [3,4-b]0 than the bite of the amine N-({4-[(3 - Benzene))]]}}}} °°Bite-6-carbamamine N-({4-[(2-fluoro-4-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[l,2-a]pyridine- 6-Protonamine N-({4-[(2,4-Dichloro-3-indolylbenzene)sulfonyl]phenyl}methyl)-1H-0 ratio. Sit and [3,4-b]0 than bite-5-formamide N-({4-[(2-decyloxybenzene)sulfonyl]phenyl}indolyl) and [l,2_a Pyridine-6-formamide N-[(4-{[3-fluoro-4-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1H- Pyrazolo[3,4-b]pyridine-5-formamide N-({4-[(5-Ga-2-methylphenyl)sulfonyl]phenyl}methyl)-1Η-° ratio Oxazo[3,4-b]pyridine-5-nonylamine N-({4-[(2,3-dimethoxyphenyl)sulfonyl]phenyl}methyl)imidazo[1,2 -a]pyridine-6-formamide N-({4-[(4-methoxyphenyl)sulfonyl]phenyl}methyl)imidazo[l,2-a] 0 to 0--6 - formamide N-({4-[(2-butoxy-4-fluorobenzene)sulfonyl]phenyl}indolyl)-1Η-. Bisazo[3,4-b]pyridine-5-carbamimidamine N-({4-[(2,5-dimethoxyphenyl)sulfonyl]phenyl}indolyl)imidazo[1, 2-a]pyridine-6-carbamimidoxime-({4.[(3,5-dichlorobenzene)sulfonyl]phenyl}indenyl)imime&quot;sitting[l,2-a] 158436 .doc •128·201215609 ° than 唆-6-carbamamine N-({4-[(3-methoxyphenyl)sulfonyl]phenyl}methyl)imidazolium ^Bist-6-cartoamine 1^-{[4-(1-methyl-111-° bow 丨° sitting-5-continuation 醯) phenyl]fluorenyl}_1|^-'» ratio 1&gt; sit and [3,4-b Pyridine-5-T decylamine N-({4-[(3-Gaxo-2-indolyl)sulfonyl]phenyl}methyl)_iH_. Bisazo[3,4-b]pyridine-5-carboxamide N-[(4-{[3-fluoro-5-(trifluoromethyl)benzene]sulfonyl}phenyl)indolyl]_1Η · • 0-pyrido[3,4-b]pyrodo-5-carbamide N-({4-[(3-fluorophenyl)sulfonyl)phenyl}indolyl)imidazo[l,2 -a]»Bistidine-6-formamide N-[(4-{[4-(ethoxymethyl)benzene]sulfonyl}phenyl)methyl]-1Η-»biszolo[3 ,4-b]pyridine-5-formamide N-({4-[(4-phenylbutane)sulfonyl]phenyl}methyl)-1Η-«比比和[3,2-c Pyridine-2-carboxamide N-({4-[(2- gas-4-mercaptophenyl)sulfonyl]phenyl}methyl)-1Η-η-pyrazolo• [3,4-b Pyridine-5-formamide N-({4-[(4-cyanobenzo)sulfonyl]phenyl}methyl)-1Η-α is more than saliva[3,4-b] ° bite- 5 -decylamine N-({4-[(3-aminosulfonylbenzene)sulfonyl]phenyl}indolyl)-1Η-carbazolo[3,4-b]° than bite-5-甲甲Ν-[(4-{[2·(Benzyloxy)-5-(trifluoromethyl)benzene] sulfonyl} phenyl) fluorenyl]-1H-pyridinium [3,4- b]° ratio _5_carbamamine N-{[4-(naphthalene-1-sulfonyl) phenyl] fluorenyl}-1 Η-° carbazolo[3,4-b]. Ratio 158436.doc -129- 201215609 bite-5 - anthraquinone N-{[4-(phenylsulfonyl)phenyl]indolylpyrino[3,2-c].比 曱醯 曱醯 曱醯 Ν -{[4-(1-methyl-1H-carbazole-7-sulfonyl)phenyl]fluorenyl}-lH-&quot;Bizozolo[3,4- b] Pyridin-5-formamide N-({4-[(5-fluoro-2.nonylbenzene)sulfonyl]phenyl}methyl)_1Η_β-pyrazolo[3,4-b]pyridine- 5-Amidoxime-{[4-(2Η-1,3-benzodioxole-4-sulfonyl)phenyl]methyl}-111-pyrazolo[3,4- b]pyridine-5-carbamamine N-({4-[(5-chloro-2-propoxybenzene)sulfonyl]phenyl}methylpyrazolo[3,4-b]pyridine-5 -Proline N-({4-[(3-fluoro-2-methoxybenzene)sulfonyl]phenyl}methyl-pyrazolo[3,4-b]pyridine-5-decylamine N -({4-[(2-Fluoro-5-methoxyphenyl)sulfonyl]phenylmerinopyrazolo[3,4-b]pyridine-5-decylamine]^-({4 -[(4-butoxy-2-methylphenyl)sulfonyl;|phenyl}methyl)_111_11 is more than [3,4-b]. Ratio -5-decylamine N- [(4-{[4-(propan-2-yl)benzene)] phenyl)methyl]- oxazolo[na]0 than bite-6-cartoamine N-({4-[( 2,3-Dimethoxybenzene)sulfonyl]phenyl}indenyl)·ΐΗ_η is more than salido[3,4-b]pyridine-5-formamide N-({4-[(3-fluoro) -4-propoxybenzene)sulfonyl]phenyl}methyl)pyrazolo[3,4-b]pyridine-5- Indoleamine N-[(4-{[2-(methylaminesulfonyl)benzene]sulfonyl}phenyl)indolyl 158436.doc -130- 201215609 Pyrazolo[3,4-b]pyridine- 5-nonylamine 1^-[(4-{[2-methoxy_5_(propan-2-yl)benzene]] phenyl}methyl)methyl]_ 1H-carbazole [3,4 -b]pyridine-5-formamide N-[(4-{[2-methyl_4_(1H carbazole small) benzene]] fluorenyl phenyl) fluorenyl] imidazo[l,2- a]pyridine-6-nonylamine benzene] hydrazino}phenyl)methyl]imidazo[l,2-a]. 唆-6-carbamamine N-({4-[(2-曱) Benzene)sulfonyl]phenyl}methyl)ih 〇 唑 并 [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ [ Benzene)sulfonyl]phenyl}indenyl)_1Η_ϋΛoxazolo[3,4-b]pyridine-5-carboxamide N-{[4-({4-fluoro-3-[(prop-2-) Aminomethyl]phenyl}sulfonyl)phenyl]methyl}-1Η-pyrazolo[3,4-b]pyridine·5·carbamamine]^-({4-[(4- Butylbenzene)sulfonyl]phenyl}methyl)_11111-pyrazolo[3,4_b]0 is 0-but-5-cartoamine N-({4-[(2-ethylbenzene))sulfonate (phenyl)methyl)imidazo[i2a]. Ratio of bite-6-cartoamine N-({4-[(2,4-dimercaptophenyl)sulfonyl]phenyl]methyl)imidazolium a]0 ratio. D--6-carbamamine N-[(4-{[3-(methoxymethyl)phenyl]sulfonyl}phenyl)indenyl]_ΐΗ_. Bisazo[3,4-b]pyridine-5-formamide N-({4-[(2,5-dimethylphenyl)sulfonyl]phenyl}methyl)imidazo[a] ° ratio 0--6-carbamamine N-[(4-{[5-Gas-2-(propan-2-yloxy)benzene]sulfonyl}phenyl)indolyl 158436.doc -131· 201215609 1H-pyrazolo[3,4-b]pyridine-5-cartoamine N-({4-[(2-butoxy-5-gasbenzene)sulfonyl]phenyl}methyl)ih_d ratio Zoxao[3,4-b]pyridine-5-carbamidamine N-({4-[(4-Ga-2-nonyloxybenzene)sulfonyl]phenyl}indolyl)imidazo[l, 2-a]0 than bite-6-cartoamine-({4·[(3-butoxyphenyl)sulfonyl]phenyl}methyl)_1H_n-pyrazolo[3,4-b]° N-({4-[(3-ethylmercaptophenyl)sulfonyl)phenyl}indolyl)imidazo[Ha] 0 than bite-6-carboxamide N-( {4_[(3-Phenylpropan)sulfonyl]phenyl}methyl)_m_„pyrho[3,2-c]pyridine-2-carboxamide N-({4-[(4-butyl) Oxyphenyl)sulfonyl]phenyl}methyl-pyrazolo[3,4-b]pyridine-5-carboxamide N-({4-[(2,6-dimethylphenyl)sulfonyl) Phenyl}methyl)_1H_D than oxazolo[3,4-b]pyridine-5-carbamidamine N-({4-[(2-gas-6-methoxyphenyl)sulfonyl)phenyl }曱基)imidazo[l,2-a]pyridine bite- 6-Protonamine N-({4-[(4-fluoro-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidate[l,2-a]pyridine-6-oxime Amine N-[(4-{[3-fluoro-5-(2,2,2-trifluoroethoxy)benzene]sulfonyl}phenyl)methyl]-1H-pyrazolo[3,4 -b]pyridine-5-formamide N-({4-[(2-decyloxy-5-methylphenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]pyridine -6-carbamamine N-({4-[(3-fluoro-4-methylphenyl)sulfonyl]phenyl}methyl)midoxime [1,2- 158436.doc •132· 201215609 a Ratio. -6-carbamamine N-({4-[(3,4-dimercaptophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]0 to 0 Ding-6-cartoamine N-[(4-{[2-曱oxy-4-(trifluoromethyl)benzene]sulfonyl}phenyl)methyl] azo 0 sits and [l,2- a]° ratio -6-decylamine N-({4-[(2-chlorophenyl)sulfonyl]phenyl}methyl)imidazo[1,2-a]. Bipyridyl-6-oxime Indoleamine N-({4-[(3-cyanobenzo)sulfonyl]phenyl}indolyl)-1Η-°-pyrazolo[3,4-φ b]pyridine-5-carboxamide N- ({4-[(2,4,6-tridecylbenzene)sulfonyl]phenyl}indolyl)-1Η-η-pyrazolo[3,4-b]pyridine-5-carboxamide N- [(4-{[3-Fluoro-4-(trifluoromethoxy)benzene]sulfonyl}phenyl)methyl]-1H-0嗤[3,4-b]° ratio to 5--5-decylamine N-({4-[(5-fluoro-2-methoxybenzene)sulfonyl]phenyl}indolyl)imidazo[ 1,2 - a] ° ratio σ -6 -methalin Ν-(4-(3-(trifluoromethoxy)phenylsulfonyl)benzyl)-1 Η-. Bisazo[3,4-b]pyridine-5-carboxamide N-(4-(3-(trifluoromethyl)phenylsulfonyl)benzylpyrazole[3,4-1) 0°°-5 -cartosamine N-(4-(3,5-difluorophenylsulfonyl)benzyl)-l,8a-dihydroimidazo[l,2-a]pyridine- 6-decylamine 7,8-dihydro-5H-pyrido[3,4-b]pyrazine-6-carboxylic acid 4-phenylsulfonyl-benzylamine 3,4-dihydro-1Η-[ 2,6] acridine-2-decanoic acid 4-phenylsulfonyl-benzyl decylamine 158436.doc -133- 201215609 3'4-dihydro-1Η-[2,7]acridine-2-carboxylic acid 4 - Benzenesulfonyl-benzyl decylamine 6.7-dihydro·4Η-isoxazo[4,3-c]pyridine_5·decanoic acid 4-phenylsulfonyl-benzylamine 5.8-dihydro- 6H-[1,7]acridine-7-carboxylic acid 4-phenylsulfonyl-benzylamine 6,7-dihydro-4H-isoxazo[4,5-c]pyridine-5-carboxylic acid 4 -Benzenesulfonyl-benzyl benzylamine 13-dihydro-pyrrolo[3,4-c]pyridin-2-furic acid 4-benzenesulfonyl-benzyl guanamine imidazo[1,2-a] Pyrazin-6-formic acid 4·benzenesulfonyl-knotylguanamine imidazo[l,5-a]pyridine-6-carboxylic acid 4-phenylsulfonyl-benzylamine 1H-pyrazolo[3, 4_c]pyridine_5_decanoic acid 4-phenylsulfonyl-benzylimidazolidinium[1,2-4〇pyridin-7-acid 4-(3,5-difluoro-benzenesulfonate) Benzyl decylamine 1H-pyrazolo[4,3_b]pyridine _5_decanoic acid 4-phenylsulfonylbenzyl decyl furan [3,2-b]pyridine-2-carboxylic acid 4-benzene Sulfhydryl-nodal decyl phenylsulfonyl)phenyl]methyl}thieno[3,2_b]acridine-2-carbamidine N_{[4-(phenylsulfonyl)phenyl]methyl }Imidazo[15 a]pyridine_6_carbamamine N-{[5-((). Bisidine_2_yl] fluorenyl}_1Η_π比洛和[3,2 &lt;] indole-2-carbamide N-{[4-(phenylsulfonyl)phenyl]methyl"imidazo[12_a]epyrazine-6 carboxamide N-{[4-( Stupid fluorenyl)phenyl]methyl)furanylamine N-{[6-(phenylsulfonyl). Bisidine_3_yl]methyl}-1H_indole-[3,2_c]indolepyridin-2-amine N-{[4-(piperazin-1-sulfonyl)phenyl] Methyl}thieno[2,3_c]acridine_ 2-carboxamide 158436.doc -134· 201215609 N-{[4-(°辰唤-1·Continuation) phenyl]methyl}M. Sit and squat, 2♦ than bite · 6-carbamid Ν _{[4_(3_Amino~Biluo-1·Continued)Phenyl]methyl}嗟-[2,3_c]pyridine 2-carbalamine hydrochloride Nm-(3-amine base) phenyl]fluorenyl} benzo[2,3·C]pyridine-2-carboxamide hydrochloride N-( {4-[(3,5-Difluorobenzene)sulfinyl]phenyl}methyl)imidazo[na]pyridine-6-carboxamide. A pharmaceutical composition comprising a compound according to any one of claims 1 to 23 and a pharmaceutically acceptable carrier. 25. The pharmaceutical composition of claim 24, further comprising a chemotherapeutic agent. 26. The pharmaceutical composition of claim 25, wherein the chemotherapeutic agent is a DNA damaging agent. 27. The pharmaceutical composition of claim 24, further comprising a cell rescue agent. 28. The pharmaceutical composition of claim 27, wherein the cell rescue agent is nicotinic acid amine, acid test or base guanamine mononucleotide (NMN). The pharmaceutical composition of claim 25, wherein the chemotherapeutic agent is selected from the group consisting of a cytotoxic agent, ciSplatin, doxorubicin, taxotere, paclitaxel (taxol), etoposide, irinotecan, camptostar, topotecan (t〇p〇tecan), paclitaxel, docetaxel, Epothilone, tamoxifen, 5-fluorourine, methoxtrexate, temozolomide, ring 158436.doc - 135- 201215609 Amine (cyclophosphamide), SCH 66336, tipifarnib (Zarnestra®), R115777, L778, 123, BMS 214662, Iressa®, Tarceva®, C225, GLEEVEC®, intron®, Peg-Intron ®, aromatase combination, ara-C, adriamycin, cytoxan, gemcitabine, urine 0 U must be mustard (Uracil mustard), nitrogen mustard (Chlormethine), different Ifosfamide, Melphalan, Chlorambucil, Pipobroman, Triethylenemelamine, Triethylenethiophosphoramine, Busulfan, Carbest; Carmustine), Lomustine, Streptozocin, Dacarbazine, Floxuridine, Cytarabine, 6-mercaptopurine (6- Mercaptopurine), 6-Thioguanine, Fludarabine phosphate, oxaliplatin, leucovirin, ELOXATIN® ), pentastatin, Vinblastine, Vincentine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin ), Xiaohong, Epirubicin, Idarubicin, MithramycinTM, Deoxycoformycin, Mitomycin- C), L-Asparaginase, Tenipal Ring Teniposide), 158436.doc -136- 201215609 17α-Ethinylestradiol, Diethylstilbestrol, Testosterone, Prednisone, I Fluoxymesterone, Dromostanolone propionate ), Testolactone, Megestrol acetate 'Methylprednisolone, Methyltestosterone, Prednisolone, Triamcinolone, olefin Chlorotrianisene, Hydroxyprogesterone, Aminoglutethimide, Estramustine, Medroxyprogesteroneacetate, Leuprolide, Flutamide Flutamide), Toremifene, goserelin, Carboplatin, Hydroxyurea, Amsacrine, Procarbazine, Mitre Mitotane, Mitoxantrone, Levamisole, Navelbene, Anastrazole, Le Quran (L) Etrazole), capecitabine, raloxifene, droxaxene, Hexamethylmelamine, Avastin, herceptin, hundred grams Bexxar, Velcade, Zevalin, Trisenox, Xeloda, Vinorelbine, Porfimer, Erbitux ( Erbitux), Liposomal, ° Thiotepa, Altretamine, Melphalan, Trastaff 158436.doc • 137· 201215609 Mab (Trastuzumab), Lerozole ), Fulvestrant, Exemestane, Isoprostol, Rituximab, C225, Campath, leucovorin 'and dexamethasone, bicalutamide, carboplatin, chlorambucil, cisplatin, lysine, megestr〇1, valrubicin And Changchun test. The pharmaceutical composition according to any one of claims 1 to 2, wherein the pharmaceutical composition according to any one of claims 24 to 29 is for inhibiting abnormal cell growth or treating a hyperproliferative disorder in a mammal. In the method. The use of a compound according to any one of items 1 to 23, which is for the manufacture of a medicament for inhibiting nicotine indole phosphoribosyltransferase ("NAMPT") in a patient. 32. — kind of request item! The use of a compound according to any one of 23, which is for the manufacture of a medicament for treating, preventing, inhibiting or eliminating a disease or condition of a patient by inhibiting ΝΑΜρτ of a patient, wherein the disease or condition is selected Free group consisting of cancer, ovarian, breast, uterine, colon, cervical, lung, prostate, skin, bladder, pancreatic, leukemia, lymphoma, Hodgkin's Disease), viral infection, human immunodeficiency virus (Human Immun〇deficiency Virus), hepatitis virus, herpes virus, herpes simplex, inflammatory disease, colonic irritable bowel syndrome, inflammatory bowel disease, rheumatoid arthritis, asthma, chronic Obstructive pulmonary disease, osteoarthritis, osteoporosis, dermatitis, atopic dermatitis, psoriasis, all 158436.doc •138- 201215609 Physical lupus erythematosus, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, graft Anti-host disease, Alzheimer's disease, brain management accident, atherosclerosis, diabetes, spheroid nephritis Metabolic syndrome, non-small cell lung cancer, small cell lung cancer, multiple myeloma, leukemia, lymphoma, squamous cell carcinoma, kidney cancer, ureter and bladder cancer, head and neck cancer, brain and central nervous system cancer β 33. The use of item 32, wherein the disease is cancer. 34. The use of claim 33, wherein the cancer is selected from the group consisting of leukemia, lymphoma, ovarian cancer, breast cancer, uterine cancer, colon cancer, cervical cancer, lung cancer, prostate cancer, skin cancer, (: &lt;&lt;&gt;&gt;&gt;&lt;&gt;&gt;&gt;&lt;&gt;&gt;&gt;&lt;&apos;&gt;&gt;&gt; Is used to treat a hyperproliferative disorder in a mammal. 36. The use of claim 35 is for the treatment of cancer. 37. A compound according to any one of claims 1 to 23 or as claimed The use of a pharmaceutical composition according to any one of claims 24 to 29, which is for use in the manufacture of a medicament for the treatment of cancer. The use of any one of claims 36 or 37, wherein the cancer is selected from the group consisting of Groups: leukemia, lymphoma, ovarian cancer, breast cancer, uterine cancer, colon cancer, cervical cancer, lung cancer, prostate cancer, skin cancer, CNS cancer, bladder cancer, pancreatic cancer, and Hodgkin's disease. 158436.doc -139· 201215609 IV. Designated representative map: ( ) :( no case designated representative graph) (ii) of the present symbol elements representative diagram of a brief description: Fifth, if the case of formula, please disclosed invention features most indicative of the formula: 158436.doc