MXPA01005829A

MXPA01005829A - Thiourea inhibitors of herpes viruses

Info

Publication number: MXPA01005829A
Application number: MXPA/A/2001/005829A
Authority: MX
Inventors: Jonathan David Bloom; Kevin Joseph Curran; Russell George Dushin; Stanley Albert Lang; Adma Antonia Ross; Hara Bryan Mark O; Emily Boucher Norton; Martin Joseph Digrandi
Original assignee: Wyeth
Priority date: 1998-12-09
Filing date: 2001-06-08
Publication date: 2001-12-13

Abstract

Compounds of formula (I), wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, -CN, -NO2, -CO2R6, -COR6, -OR6, -SR6, -SOR6, -SO2R6, -CONR7R8, -NR6N(R7R8), -N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen;or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl;R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl;R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl;R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms;provided that at least one of R9-12 is not hydrogen;W is O, NR6, or is absent;Y is -(CO)- or -(CO2)-, or is absent;Z is alkyl of 1 to 4 carbon atoms, -CN, -CO2R6, COR6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -OR6, -SR6, -SOR6, -SO2R6, SR6N(R7R8), -N(R7R8) or phenyl;G is aryl or fused bicyclic heteroaryl;and X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J;J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl;and n is an integer from 1 to 6, in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.

Description

INHIBITORS OF TIOUREA OF VIRUSES OF THE HERPES BACKGROUND OF THE INVENTION Eight viruses that are members of the Herpes vir idae family have been identified (summarized in Roizman, B. 1996. Herpes vir idae, p 2221-2230) In BN Fields, DM Knipe, and PM Howley (ed. ), Fields Virology, 3rd ed. Lippincot t-Raven Publishers, Philadelphia, PA). Each member of this family is characterized by a developed virus containing proteinaceous integuments and nucleocapsid, the latter of which hosts the genome of double-stranded DNA relative to the large entiente (ie, approximately 80-250 kilobases). Members of the human faherpes vi rus subfamily are neurotropics and include herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), and varicella zoster virus (VZV). Human herpesvirus 6 with human cytomegalovirus (HCMV), herpesvirus 6 (HHV-6) and human herpesvirus 7 (HHV-7). The gammaherpe s vi rus are 1 raft infotypes and include the Epstein-Barr virus (EBV) and the Kaposi herpesvirus (HHV-8). Each of these herpesviruses is causally related to human disease, including cold sores and genital herpes (HSV-1 and HSV-2 [Whitley, RJ 1996, REF: 129747 Herpes Simples Viruses, p.2227-2342. Fields, DM Kn: .pe, and PM Ho law (ed.), Fields Virology, 3rd ed. Lippincott-Raven Publishers, Philadelphia, PA]); chickenpox and herpes zoster (chicken pox and shingles) (VZV [Arvin, A. 1996, Varicella-Zos ter Virus, pp. 2547-2585.In BN Fields, DM Knipe, and PM Howley (ed.), Fields Virology, 3rd ed. Lippincott-Raven Publishers, Philadelphia, PA]); infectious mononucleosis (EBV [Rickinson, AB and Kieff, E. 1996. Epstein-Barr Virus, pp. 2397-2446.In BN Fields, DM Knipe, and PM Howley (ed.), Fields Virology, 3rd ed. Lippincott-Raven Publishers, Philadelphia, PA]); pneumonia and retinitis (HCMV [(Britt, J., and Alford, CA 1996. Cyto egalovirus, p 2493-2523, in BN Fields, DM Knipe, and PM Howley (ed.), Fields Virology, 3rd ed. Lippincott -Raven Publishers, Philadelphia, PA]), exanthema subitum (HHV-6 [(Pellet, PE and 31ack, JB 1996. Human Herpesvirus 6, pp. 2587-2608) In BN Fields, DM Knipe, and PM Howley (ed. ), Fields Virology, 3rd ed. Lippincott-Raven Publishers, Philadelphia, PA] and HHV-7 [Frenkel, N., and Roffman, E. 1996. Human Herpesvirus 7, p 2609-2622. In BN Fields, DM Knipe , and PM Howley (ed.), Fields Virology, 3rd ed. Lippincott-Raven Publishers, Philadelphia, PA]), and Kaposi's sarcoma (HHV-8 [Neipel, F., Albrecht, JC, and Fleckenstein, B. 1997 Genes homologous to cells in herpesvirus 8 of radinovirus associated with Kaposi's sarcoma: determinants of its pathogenicity? J. Virol. 71: 4187-92, 1997].) HCMV is considered in more detail below. the primary infection, the herpesvirus estab latency within infected individuals and remain for the rest of their lives. The periodic reactivation of the latent virus is clinically relevant. In the case of HSV, the reactivated virus can be transmitted to children or infants during birth, causing either infection in the skin or eyes, infection in the central nervous system, or disseminated infection (ie, multiple organs or systems). Herpes zoster is the clinical manifestation of VZV reactivation. The treatment of HSV and VZV is usually with antiviral drugs such as acyclovir (Glaxo Wellcome), ganciclovir (Roche) and foscarne1: (Asta) whose viral target encodes the DNA polymerase. HCMV is a ubiquitous opportunistic pathogen that infects 50-90% of the adult population (Britt, WJ, and A.Lford, CA 1996. Cytomegalovirus, p.2493-2523.In BN Fields, DM Knipe, and PM Howley (ed.), Fields Virology, 3rd ed. Lippincott-Raven Publishers, Philadelphia, PA). Primary infection with HCMV is usually asymptomatic, although heterophilic negative mononucleosis has been observed. The virus is transmitted horizontally through sexual contact, breast milk, and saliva. The intrauterine transmission of HCMV from the pregnant mother to the fetus occurs, and is frequently the cause of serious clinical consequences. The HCMV remains in a latent state within the infected person for the rest of his life. The mediated immunity of the cell plays a central role in controlling the reactivation of latency. Damaged cell immunity leads to the reactivation of latent HCMV in seropositive people. HCMV disease is associated with deficient or immature cellular immunity. There are 3 main categories of people with HCMV disease (summarized by Britt and Alford, 1996). (1) In immunocompromised patients (AIDS), HCMV is one of the two most common pathogens that cause clinical disease (the other is Pne umocys t i s). The most common manifestation of HCMV in AIDS is retinitis, although infection of other organs including the adrenal glands, lungs, gastrointestinal tract and the central nervous system are also frequently reported. 90% of AIDS patients have active HCMV infection: 25-40% (-85,000 patients in the United States) have HCMV disease that threatens life or sight. HCMV is the cause of death in 10% of people with AIDS. (2) Due to the suppression of the immune system to reduce the risk of graft rejection, the reactivation or reinfection of HCMV is common among patients with kidney, liver, heart and allogeneic bone marrow transplants. Pneumonia is the most common HCMV disease in these patients, which occurs in up to 70% of these patients with a transplant. (3) Congenital infection due to HCMV occurs in 1% of all births, approximately 40K per year. Up to 25% of these children are symptomatic for HCMV disease between ages 0-3 years. HCMV disease is progressive, causing mental retardation and neurological abnormalities: .cas, in children. Recent studies suggest that treatment with anti-HCMV drugs can reduce morbidity in these children. Several antiviral drugs are currently marketed (Bron, D., R. Snoeck, and L. Lagneaux, 1996. New insights into the pathogenesis and treatment of cytomegalovirus.) Exp. Opin. Invest. Drugs 5: 337-344; Crumpacker, C. 1996. Ganciclovir, New Eng. J. Med. 335: 721-729; Sachs, S., and F. Alrabiah, 1996. Novel herpes treatments: a summary. Exp. Opin. Invest. Drugs 5: 169-183). These include: ganciclovir (Roche), a nucleoside analogue with hemopoietic cell toxicity; foscarnet (Astra), a pyrophosphate analog with nephrotoxicity; and cidofovir (Gilead), a nucleoside phosphonate with acute nephrotoxicity. Each of these target drugs encodes the viral DNA polymerase, are typically administered intravenously due to their low bioavailability, and, as noted above, are the source of significant toxicity. The clinically resistant ganciclovir resistant mutants are often resistant to cidofovir crossing. Therefore, there is a need to ensure that orally (ie less toxic) bioavailable antiviral drugs are directed against novel viral targets. Phenyl thioureas are described for use in a variety of pharmaceutical applications. Armistead, et al., WO 97/40028, describe phenylureas and thioureas as inhibitors of the enzyme of inosine dehydrogenase monophosphate (IMPDH) which are described to play a role in the viral replication diseases of such herpes.

Widdowson, et al., WO 96/25157, describe phenylurea and thiourea copolymers of the following formula for treating diseases mediated by chemokine, interleukin-8.

Morin, Jr., et al., U.S. Patent No. 5,593,993 discloses certain phenylthiourea compounds for the treatment of AIDS and the inhibition of replication of HIV and related viruses. Therefore, it is an object of this invention to provide compounds, and pharmaceutically acceptable salts thereof, for inhibiting and / or treating diseases associated with the herpes virus including human cytomegalovirus, herpes simplex virus, Eps tein-Barr virus, varicella-zoster virus, human herpesvirus 6 and 7, and Kaposi herpesvirus.

DESCRIPTION OF THE INVENTION According to the present invention, compounds having the formula are provided: 1 of R? -R;, are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6, -COR6, -OR6, "SR6, -SOR6, -S02R6, -CONR7R8, -NR6N (R7R8), -N (R7R8) or W-Y- (CH2) n -Z with the proviso that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together form a 3-7 membered heterocycloalkyl or a 3-7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl or heteroaryl, or R7 and R8, taken together they can form a 3- to 7-membered heterocycloalkyl; R9-R: 2 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or Rg and Rio or Rn and R? 2 can be taken together to form an aryl of 5 to 7 carbon atoms; with the proviso that at least one of R9-? 2 is not hydrogen; W is O, NRe, or absent; And it is - (CO) - or - (C02) -, or it is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -C02R6, ~ COR6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -OR6, -SR6 -SOR6, -S02R6, SR6N (R7R8), -N (R7R8) or phenyl; G is aryl optionally substituted with one or more substituents selected from alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6, -COR6, -0R6, -SR6, -SOR6, -S02R6, -CONR7R8, - NR6N (R7R8), -N (R7R8) or WY- (CH2) n- Z; or G is a condensed bicyclic heteroaryl; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 atoms carbon, or (CH) J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6, or pharmaceutical salts thereof. In some preferred embodiments of the present invention, at least 1 of Rg-R? 2 is not hydrogene. Preferably Rg-R? 2 are selected from halogen, methyl, methoxy, cyano, G is preferably phenyl. In more preferred embodiments of the present invention, G is substituted phenyl. In still more preferred embodiments of the present invention G is substituted with one or two halogen substituents. Most preferably G is 2-fluorophenyl. In still other preferred embodiments of the present invention, G is a fused bicyclic heterosaryl. Preferably, when G is a fused bicyclic heteroaryl, G is quinoline, isoquinoline or benzofuran. Preferred compounds of the present invention are the following compounds which include pharmaceutical salts thereof: 2-Fluoro-N- (4-. {3, 3- [l- (4-fluoro-phenyl) -ethyl] -tioureidc.}. -2, 3, 5, 6- tet ramethyl-phenyl) -benzamide, N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureidol-2,5-dimet oxy-phenyl) -2- fluoro-benzamide, 2-Fluoro-N- (4- {3- [l- (4-fluoro-phenyl) -ethyl] -thioureidc} -2,5-dimethoxy-phenyl) -benzamide , N-. { 3, 5-Dichloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide, N-. { 3-Chloro-4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -tioureidc} phenyl) -2-fluoro-benzamide, 2,3,4,5-Tetrafluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -3 -methyl-1-phenyl) -benzamide, 2,4,5-trifluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -ticureido.} -3-methyl- phenyl) -benzamide, 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureidc.] - 3-methyl-1-phenyl) -benzamide, - Fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureidc.] -2-methoxy-5-methyl-phenyl) -benzamide, 2-Fluoro-N - (4- { 3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.} - 3-methoxy-phenyl) -benzamide, N- (2, 6-Dibromo-4. 3- [l- (4-Fluoro-phenyl) -ethyl] thioureido.} - phenyl) -2-fluoro-benzamide, 2-Fluoro-N- (4-. {3- 3 [l- (4- fluoro-phenyl) -ethyl] -thioureido.} -2- t-rifluoromethyl-1-phenyl) -benzamide, N- (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido} -2-tri-fluoromethyl-phenyl) -2-fluoro-benzamide, N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2-trifluoromethyl -phenyl) -2- fluoro-benzamide, N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2-tri-fluoromethyl-phenyl} -2-fluoro-benzamide, N- (2-Chloro-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -ioureido} -phenyl) -2-fluoro-benzamide, N - (2-Chloro-4- {3- [l- (4-cyano-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- (2-Cyano-4-) {.3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- (4-. {3- [1- (4-Bromo - phenyl) -ethyl] -thioureido.} -2-cyano-phenyl) -2-fluoro-benzamide, N- (2-cyano-4-. {3- [l- (4-cyano-phenyl) - ethyl] -thioureido.}.-phenyl) -2-fluoro-benzamide, N-. { 4- [3- [1-Benzofuran-2-yl-ethyl) -thioureido] -2-cyano-phenyl} -2-fluoro-benzamide, N- (2-Benzoyl-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -tioureid.} - phenyl) -2-fluoro-benzamide, 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureid} -2-methyl-phenyl) -benzamide, N- (4-. 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2-methyl-phenyl) -2-fluoro-benzamide, N- (4-. {3- 3 [1- (4- Cyano-phenyl) -ethyl] -thioureido} -2-methyl-phenyl) -2-fluoro-benzamide, N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2-methyl-phenyl} -2- fluoro-benzamide, N- (2-Dimethylamino-4-. {3, 3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N - (2-Benzyloxy-4- {3- [l- (4-cyano-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- (2-Benzyloxy-4-) (3- (l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2-morpholin-4-yl-ethoxy) -phenyl] -2-fluoro-benzamide, N- [4-. { 3- [1- (Bromo-phenyl) -ethyl] -thioureido} -2- (2 -mor fo? In-4-yl-ethoxy) -phenyl] -2-fluoro-benzamide, 2-Fluoro-N- [4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -2- (2-morpholin-4-yl-ethoxy) -phenyl] -benzamide, N- (2-Butoxy-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido}. -phenyl) -2-fluoro-benzamide, N- (2-Butoxy-4) -. {3- [l- (4-cyano-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2-diethylamino-ethoxy) -phenyl] -2-r-fluoro-benzamide, N- (2- (2-Diethylamino-ethoxy) -4-. {3- 3- [l- (4-fluoro- phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2-diethyl amino-ethoxy) -phenyl] -2-fluoro-benzamide, N- (2-Ethoxy-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureidc .} - phenyl) -2-fluoro-benzamide, N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2-ethoxy-phenyl) -2 -fluoro-benzamide, 2-Fluoro-N- [4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -tioureidc} -2- (2-nitrile-ethoxy) -phenyl] -benzamide, N- [4-. { 3- [1- (4-Cyano-phenyl) -ethyl] -thioureido} -2- (2-nitrile-ethoxy) -phenyl] -2-fluoro-benzamide, 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -tioureidc} -2-methoxy-phenyl) -benzamide, 2-Fluoro-N- (5-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -biphenyl-2- il) -benzamide, (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-t-trifluoromethyl-phenyl) -aminoquinoline-1-carboxylic acid amide (4- {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-trifluoromethyl-phenyl) -amide of benzofuran-2-carboxylic acid, (4-. { 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-tri-fluoro-yl-phenyl) -aminoquinoline-3-carboxylic acid amide, (2-Cyano-4-. Isoquinoline-1-carboxylic acid (2-Cyano-4-. {3- 3 [l- (4-fluoro-phenyl) -ethyl] -thioureidc.} -phenyl) -amide. - (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -amide of benzofuran-2-carboxylic acid, (2-Cyano-4-. {3- [1- (4-fluoro- phenyl) -ethyl] -thioureido.} - phenyl) -aminoquin-3-carboxylic acid amide, (4-. {3- [l- (4-Fluoro-phe nil) -ethyl] -thioureido} Isoquinoline-1-carboxylic acid-2-methyl-fer il) -amide, (4- {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-methyl-fer il) -aminoquinoline-3-carboxylic acid, 2-Fluoro-N- (4- {3- [l- (4-fluoro-phenyl) -ethyl} -thioureido} -3-tri-fluoromethyl-phenyl) -benzamide, (4-. {3 - [(lS) -l- (4-Bromo-phenyl) -ethyl] -thioureido.} -2-trifluoromethyl-phenyl) -amide of i-soquinol in-3-carboxylic acid, N- (4-. {3- [(1S)] ) -1- (4-Bromo-phenyl) -ethyl] -thioureido} -2-cyano-phenyl) -2-fluoro-benzamide, N- (4-. {3- [(IR) -1- (4-Bromo-phenyl) -ethyl] -thioureido.} -2-cyano-phenyl) -2-fluoro-benzamide, N-. { 2-Cyano-4- [( { [(SS) -1- (4-fluorophenyl) ethyl] -amino.} Carbonyl) amino] pheni 1} -2- fluorine enzamide, N-. { 4- [( { [(LS) -l- (1-Benzofuran-2-yl) ethyl] -amino.} Carbonyl) amino] -2-cyanophenyl} -2-fluorobenzamide, 2-Fluoro-N-. { 4- [( { [(IR) -l- (4-fluorophenyl) ethyl] -aminocarbonyl) amino] -3-methylphenyl} benzamide, N-. { 4 - [( { [(LS) -l- (4-Fluorophenyl) ethyl] amino.}. -carbothio: .1) amino] -2-cyanophenyl} -2-fluorobenzamide, N-. { 4- [( { [(1S) -1- (4-Chlorophenyl) ethyl] amino.} - carbothioyl) amino] -2-cyanophenyl} -2-fluorobenzamide, or pharmaceutical salts thereof. "Alkyl" as used herein refers to a lower alkyl of 1 to 6 carbon atoms straight or branched chain. Exemplary alkyl groups include methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, pentyl and hexyl. "Alkenyl" as used herein refers to lower alkyl of 2 to 6 carbon atoms straight or branched chain containing at least one carbon-carbon double bond. Alkenyl includes vinyl groups.

Alkynyl as used herein refers to straight or branched chain 2 to 6 carbon lower alkyl containing at least one carbon-carbon-carbon triple bond. The alkyl, alkenyl and alkynyl groups herein can be substituted or unsubstituted. Cycloalkyl refers to a saturated mono or bicyclic ring system of 3 to 10 carbon atoms. Exemplary cycloalkyl groups include cyclopentyl, cyclohex: .lo and cycloheptyl. The cycloalkyl groups of the present invention can be substituted or unsubstituted. "Heterocycloalkyl" refers to a saturated mono or bicyclic ring system of 3 to 10 members having from 1 to 3 heteroatoms selected from N, S and O, including, but not limited to aziridinyl, azetidinyl, imidazolidinyl, morpholinyl, t -omorpholinyl, piperazimyl, pyrazolidinyl, piperidinyl, and pyrrolidinyl. The heterocycloalkyl groups of the present invention may be substituted or unsubstituted. Aryl, as used herein, refers to an aromatic mono or bicyclic ring of 5 to 10 carbon atoms. Exemplary aryl groups include phenyl, and biphenyl. The aryl groups of the present invention can be substituted or unsubstituted.

"Heteroaryl" as used herein refers to a 5- to 10-membered aromatic mono or bicyclic ring having from 1 to 3 heteroatoms selected from N, S or O including, but not limited to thiazolyl, thiadiazolyl, oxazolyl, furyl, indolyl , benzothiazolyl, benzotriazolyl, benzodioxyl, indazolyl, and benzofuryl. Preferred heteroaryls include quinolyl, isoquinolyl, naphthalenyl, benzofuranyl, benzothienyl, indolyl, pyridyl, pyrazinyl, thienyl, furyl, pyrrolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, pyrazolyl, triazolyl, thiadiazolyl, and imidazolyl. The heteroaryl groups of the present invention can be substituted or unsubstituted. Perhaloalkyl refers to an alkyl group of 1 to 6 carbon atoms in which three or more hydrogens are substituted with halogen. Phenyl as used herein refers to a 6-membered aromatic ring. Halogen, as used herein, refers to chlorine, bromine, iodine and fluorine. Unless limited the substituents are unsubstituted and may include alkyl of 1 to 6 carbon atoms, cycloalkyl of 1 to 6 carbon atoms, heterocycloalkyl of 1 to 6 members, perhaloalkyl of 1 to 6 carbon atoms, alkylamino, dialkylamino, aryl or heteroaryl. The carbon number refers to the number of carbons in the carbon skeleton and does not include carbon atoms that occur in substituents such as alkyl or alkoxy substituents. When the terms are used in combination, the definition for each individual part of the combination applies unless it is defined otherwise. For example, alkylcycloalkyl is an alkyl-cycloalkyl group in which the alkyl and the cycloalkyl are as previously described. The pharmaceutically acceptable salts are the acid addition salts which can be formed from a compound of the above general formula and a pharmaceutically acceptable acid such as phosphoric, sulfuric, hydrochloric, hydrobromic, citric, maleic, succinic, fumaric, acetic acid. , lactic, nitric, sulfonic, p-toluenesulfonic, methanesulfonic, and the like. The compounds of this invention contain a chiral center, which provide various stereoisomeric forms of the compounds such as racemic mixtures as well as the individual optical isomers. By "substantially pure" it is meant that the composition contains more than 75% of the desired isomer may include no more than 25% of the unwanted isomer. In more preferred embodiments, the pure optical isomer is greater than 90% of the desired isomer. In some preferred embodiments, when the object is VZV, the (S) isomer is preferred. The individual isomers can be prepared directly or by asymmetric synthesis or is tereospecific or by conventional separation of the optical isomers of the racemic mixture. The compounds of the present invention can be prepared by those skilled in the art of organic synthesis using the methods described below using readily available reagents and starting agents unless otherwise described. The compounds of the present invention are prepared in this manner according to the following reaction schemes. The novel compounds of the present invention are prepared according to the following reaction schemes. With reference to Methods 31 (2 and 3, upper) and 34 (4 and 5, lower), the appropriately substituted amines 2 are reacted, wherein the substituents R1-R5, and X are described as above, with 3 appropriately substituted isothiocyanates, wherein the substituents R 9 -R 2 and G are described above, either pure or in a suitable solvent such as tetrahydrofuran, acetonitrile, ethyl acetate, dichloromethane, or N, N-dimethylformamide produce the thioureas 1 desired. Similarly, the reaction of the appropriately substituted isothiocyanates 4, wherein the substituents R1-R5, and X are described as above with appropriately substituted anilines, wherein the substituents Rg-R? 2 and G are described as above, in a convenient solvent such as those listed above produce the desired thioureas.

Methods 31 and 34 Alternatively, the appropriately substituted thioureas 1 can be prepared as described by Methods 32 and 33 by reacting the amines 2 and 5, wherein R? -R5, Rg-R? 2 and G are described as above, in the presence of either a molar equivalent of 1,1-thiocarbonyldiimidazole in an appropriate solvent such as dichloromethane and tetrahydrofuran or mixtures thereof or a molar equivalent of 1,1'-thiocarbonyl-di- (1, 2, 4) - triazole in a suitable solvent such as dichloromethane and tetrahydrofuran or mixtures thereof at room temperature.

Methods 32, 33 In certain cases, the subsequent chemical modification of the final thioureas was required. These methods, Methods 35-39, are summarized below.

P ?? aJ? pguo - The thioureas 1, wherein at least one substituent of R 1 -R 5 is 1-hydroxyethoxy or carboxy-methoxy, Rg-R 2 and G are defined as above and X is equal to a bond, can be prepared from the corresponding alkyl esters by alkaline hydrolysis with aqueous sodium or potassium hydroxide in a suitable solvent such as methanol, tetrahydrofuran or mixtures thereof at room temperature according to Methods 35 and 36. The tiorueas 1, wherein at least one substituent of R 1 -R 5 is 1-acyloxyethoxy or methanesulfonoxyethoxy, Rg-R 2 and G are defined as above and X is equal to a bond, they can be prepared from the corresponding 1-hydroxyethoxy derivative by acylation with appropriate acylating agents such as benzoic acid chloride or methanesulfonic acid chloride in the presence of a suitable tertiary amine base such as triethylamine or diisopropylethylamine in a suitable solvent such as dichloromethane or the like at room temperature according to with Methods 37 and 38. Thioureas 1, wherein at least one substituent of R 1 -R 5 is 1-aminoethoxy, Rg-R 2 and G are defined as above and X is equal to one bond, can be prepared from the corresponding 1-methansul phonoxyethoxy derivative by reaction with an appropriate secondary amine such as dimethylamine in a suitable solvent mixture such as tetrahydrofuran and water or the like at room temperature according to the M all 39. Thioureas 1, in where at least one substituent of R1-5 is 1-aminoalkyl, Rg-Ri2 and G are defined as above and X is equal to a bond, they can be prepared from the corresponding 1-azidoalkyl derivative by reaction with chloride stannous in a suitable solvent such as methanol, ethanol or the like at room temperature according to Method 40. The isothiocyanates 3 and 4 intermediates shown above in Methods 31 and 34 are prepared according to Method 41 (below) essentially of acue with the procedures of Staab, H.A. and Walter, G. Jus t us Li ebi gs Ann. Ch em. 657, 104 (1962)) by reacting the appropriately substituted amines 5 or 2, respectively, wherein R1-R5, Rg-R2 and G are described in the foregoing and X is described above, with one molar equivalent of 1,1 '-thiocarbonyldiimidazole in an appropriate solvent such as dichloromethane and tetrahydrofuran or mixtures thereof.

Method 41 Intermediates 2 and 5 can be prepared according to the following protocols: According to Methods 1A-1G, amines 2, wherein R1-R5 are defined in the foregoing and X is defined in the above Lor and the amines 5, wherein Rg-R? 2 are defined in the foregoing, they can be prepared by the reduction of appropriately substituted nitrobenzenes according to a variety of procedures known to those skilled in the art and are described in RJ Lindsay, Comprehensive Organic Chemistry (Ed. Sutherland), Volume 2, Chapter 6.3.1, Aromatic Amines, 1979. Such procedures include the reduction of nitrobenzenes to form anilines with exposure to: a) iron powder and a strong acid, such as hydrochloric acid (Methods 1A ) either pure or in an alcohol solvent such as methanol or ethanol, at temperatures ranging from room temperature to the reflux temperature of the solvent, or; b) iron powder and glacial acetic acid (Method IB), either neat or in an alcohol solvent such as methanol or ethanol, at temperatures ranging from room temperature to the reflux temperature of the solvent, or; c) iron powder and aqueous ammonium chloride (Method 1C), either neat or in an alcohol solvent such as methanol or ethanol, at temperatures ranging from room temperature to the reflux temperature of the solvent, or; d) tin and a strong mineral acid, such as hydrochloric acid (Methods ID), either neat or in an alcohol solvent such as methanol or ethanol, at temperatures ranging from room temperature to the reflux temperature of the solvent, or; e) when R? ~ R5 and Rg-R? 2 are selected from Cl, Br, I, - (OS02) -CF3, or - (OS02) -1- (4-methylphenyl), by the catalytic reduction as with hydrogen and palladium on carbon (Method 1E) in an appropriate solvent such as methanol, ethanol, or ethyl acetate, under one or more pressure atmospheres or; f) when R1-R5 and Rg-R? 2 are selected from Cl, Br, I, - (OS02) -CF3, or - (0S02) -1- (4-methylphenyl), by catalytic reduction such as with cyclohexane and palladium on carbon (Method 1F) in an appropriate solvent such as methanol or ethanol, at temperatures ranging from room temperature to the reflux temperature of the solvent, or; g) aqueous sodium hydrosulfite in an alcohol solvent at temperatures ranging from room temperature to the reflux temperature of the solvent (Method 1G). Alternatively, according to the Methods 3A-3C, the amines 2, wherein R1-R5 are defined in the above and X is defined in the above and the anilines 5, wherein Rg-R? 2 are defined in lo. above, can be prepared by separation or cleavage of the aniline nitrogen-carbon linkage of the amide and carbamate derivatives of these anilines according to a variety of procedures known to those skilled in the art and described in Greene, Protective Groups in Organic Synthesis volume 2, Chapter 7, 1991, and references in the present. Such procedures include: a) exposure of arylamino-tert-butyl-carbamates appropriately substituted to a strong acid such as trifluoroacetic acid (Method 3A) either neat or in an appropriate solvent such as dichloromethane at temperatures between 0 ° C and room temperature, or; b) exposure of appropriately substituted arylamino- (2-trimethylsilylethyl) -carbamates to a source of fluoride ion such as tetrabutylammonium fluoride or potassium fluoride (Method 3B) in aqueous acetonitrile or tetrahydrofuran or mixtures thereof at varying temperatures from room temperature to the reflux temperature of the solvent, or; c) exposure of appropriately substituted arylamino-trifluoroacetamides to a strong base such as sodium or potassium hydroxide or sodium carbonate or potassium in an alcohol solvent such as methanol or ethanol (Method 3C) at temperatures ranging from room temperature at the reflux temperature of the solvent. Alternatively, according to Method 11, the amines 2, wherein R1-R5 are defined above, and X is identical to a bond and at least one substituent of R1-R5 is defined as vinyl, can be prepared by the palladium catalyst coupling of a vinylidene reagent, such as tributylvinyl, with an appropriately substituted bromo- or iodo-aniline, for example 3-chloro-4-iodo-aniline, employing a palladium catalyst, such as tris (dibenzylidene ketone) -bipaladium, and a ligand, such as t-reilar sine, in a suitable solvent such as tetrahydrofuran or N-methylpyrrolidinone, at temperatures ranging from room temperature to the reflux temperature of the solvent, according to the procedures of V. Fariña and GP Roth in Advances in Metal-Organic Chemistry, Vol. 5, 1-53, 1996 and references herein. Alternatively, according to Method 42, the amines 2, wherein R? ~ R2 are defined in the foregoing and X is defined in the foregoing and at least one substituent of R2 or R are defined as dialkylamino, can be prepared by the catalysed amination of palladium of an appropriately substituted 3- or 5-bromo- or iodo-aniline, for example 3-amino-5-bromoben? iotifluoride, by secondary amines under conditions employing a palladium catalyst, such as bis: (dibenzylidene acetone) palladium, and a ligand, such as tri-o-tolylphosphine, and at least two molar equivalents of a strong base, such as lithium bis- (trimethylsilyl) amide in a sealed tube, in a suitable solvent such as tetrahydrofuran or toluene, at temperatures ranging from room temperature to 100 ° C, essentially according to JF procedures Hartwing and J. Loui Te t rah edron Le tt ers 36 (21), 3609 (1995). Alternatively, according to Method 43, amines 2, wherein R1-R5 are defined in the foregoing and X is defined in the foregoing and at least one substituent of R2 or R4 is defined as alkyl, can be prepared by alkylation palladium catalyzed an appropriately substituted 3- or 5-bromo- or iodo-aniline, for example 3-amino-5-bromoben-otrifluoride by alkenes under conditions employing a palladium catalyst such as a chloride complex [1, 1] 'bis (diphenylphosphino) -ferrocene' palladium (11) -dichloromethane and in the presence of 9-borabicyclo [3.3.1] nonane and a suitable base such as aqueous sodium hydroxide in a suitable solvent such as tetrahydrofuran or the like temperatures that vary from the ambient temperature to the reflux temperature of the solvent.

The acyl and carbamoyl ina derivatives used as starting materials in Methods 3A-3C can be prepared by derivatization of the corresponding amines as described in Methods 2A-2G according to a variety of procedures known to those skilled in the art. technical and described in Greene, Protective Groups in Orqanic Synthesis volume 2, Chapter 7, 1991, and references herein. Such methods include: a) the reaction of an appropriately substituted amine with di-tert-butyl dicarbonate (Method 2A) in the presence or absence of one or more molar equivalents of a tertiary amine such as triethylamine or N, N-diisopropylethylamine in a suitable solvent such as acetone, tetrahydrofuran, dimethylformamide, dichloromethane, and the like, at temperatures ranging from room temperature to the reflux temperature of the solvent to produce the corresponding acylamino tert-butyl carbamate, or; b) the reaction of an appropriately substituted aniline with 1- [2- (trimethylsilyl) ethoxycarbonyl-oxy] -benzctriazole (Method 2B) in the presence of a tertiary amine such as triethylamine or diisopropylethylamine in a suitable solvent such as dimethylformamide at room temperature for producing the arylamino- (2-trimethylsilylethyl) -carbamate, or; the reaction of an appropriately substituted aniline with a carboxylic acid chloride or acid anhydride (Method 2C) either neat or in an appropriate solvent such as tetrahydrofuran, dimethylformamide, dichloromethane, pyridine and the like, in the presence of one or more molar equivalents of a tertiary amine base such as triethylamine or N, N-diisopropylethylamine to produce the corresponding arylaminoamide, or; the reaction of an appropriately substituted nitroaniline with a carboxylic acid chloride (Method 2D) in the absence of one or more molar equivalents of a tertiary amine base such as triethylamine or N, N-diisopropylethylamine either pure or in a solvent suitable such as tetrahydrofuran, 1,4-dioxane and the like at temperatures ranging from room temperature to the reflux temperature of the solvent to produce the corresponding nitroarylaminoamide, or; the reaction of an appropriately substituted aniline with a carboxylic acid (Method 2E) in the presence of a coupling agent such as benzotriazol-1-yloxytris- (dimethylamino) -phosphonium hexa luoro-phosphate, 2- (lH) hexafluorophosphate -benzotriazol-1-yloxy) -1,3,3-tetra-methyl-yluronium, dicyolohexyl-carbodiimide and the like and in the presence of a tertiary amine such as triethylamine or diisopropylethylamine in a suitable solvent such as dichloromethane, dimethylformamide and the like, at room temperature to produce the corresponding arylaminoamide, or; f) the reaction of an appropriately protected aniline such as an arylamino-tert-butylcarbonate or the like, wherein at least one substituent of R? -R? 2 is defined as -WY- (CH2) nZ wherein W, Y and Z are defined as above, with a carboxylic acid anhydride (Method 2F) in the presence of a suitable base such as pyridine in an appropriate solvent such as dichloromethane, dimethylformamide or the like at temperatures ranging from 0 ° C to room temperature to produce the corresponding carboxylic acid ester, or; g) the reaction of an appropriately substituted aniline wherein at least one substituent of R1-R5 is defined as hydroxyl with di-tert-butyl dicarbonate (Method 2G) in the absence of one or more molar equivalents of a tertiary amine such as triethylamine or N, N-diisopropylethylamine in a suitable solvent such as acetone, tetrahydrofuran, dimethylformamide, dichloromethane, and the like, at temperatures ranging from room temperature to the reflux temperature of the solvent to produce the arylamino-ter-butyl- corresponding carbamate. The nitrobenzene intermediates which are finally converted to amines 2 and 5 by known methods; in the above in Methods 1A-1G can be prepared according to Methods 4A, 4C, 4E-4F. With reference to Methods 4A, 4C and 4E-4H, the nitrobenzene intermediates which are ultimately converted to amines 2, R2 and R4 are defined in the foregoing and Ri, R3, and / or R5 are defined as alkoxy, thioalkoxy, alkylsulfenyl, alkylsulfinyl and dialkylamino, can be prepared by the nucleophilic displacement of substituted nitrobenzenes with 2-, 4-, and / or 6-fluoro-, chloro-, bromo-, iodo-, trifluoromethyl-sulfonyl-, or (4-methylphenyl) ) -sulfonyl appropriately substituted by methods that include the following: a) reaction of alcohols with 2- or 4-halo- or sulfonate nato-esters of appropriately substituted nitrobenzenes or benzonitriles (Method 4A) either pure; or in an appropriate solvent such as tetrahydrofuran, dioxane, acetonitrile, N, N-dimethylformamide or dimethyl sulfoxide in the presence or absence of one or more molar equivalents of a base such as sodium carbonate, potassium carbonate, sodium hydroxide, hydroxide of potassium, sodium hydride, potassium hydride or the like at temperatures ranging from room temperature to the reflux temperature of the solvent; b) reactions of sodium, lithium or potassium phenoxides preformed with 2- or 4-halo- or sulfonates of nitrobenzenes or appropriately substituted benzonitriles (Method 4H) either pure or in a suitable solvent such as tetrahydrofuran, dioxane, acetonitrile, N, N-dimethylformamide or dimethyl sulfoxide, at temperatures ranging from room temperature to the reflux temperature of the solvent, or; reaction of ammonia, primary or secondary amines with 2- or 4-halo- or sulphonates of nitrobenzenes or appropriately substituted benzonitides (Methods 4C, F) either in a pure or in an appropriate solvent such as tetrahydrofuran, dioxane, acetonitrile, N, N -dimet il-formamide or dimethyl sulfoxide, at temperatures ranging from room temperature to the reflux temperature of the solvent; reaction of the preformed sodium, lithium, or potassium salts of amines with 2- or 4-halo- or sulfonates of nitrobenzenes or appropriately substituted benzonitriles (Method 4G) in a suitable solvent such as tetrahydrofuran at temperatures ranging from 0 ° C to the reflux temperature of the solvent, or; reaction of sodium sulphide with 2- or 4-halo- or sulphonates of nitrobenzenes or benzonitriles appropriately substituted either neat or in an appropriate solvent such as tetrahydrofuran, dioxane, acetonitrile, N, N-dimethylformamide or dimethyl sulfoxide, at temperatures which vary from room temperature to the reflux temperature of the solvent, followed by the addition of an alkyl halide directly to the reaction mixture (Method 4E). Alternatively, with reference to Methods 5C and 6, the nitrobenzene intermediates that are ultimately converted to amines 2, wherein at least one substituent of R1-R5 is defined as alkoxy, can be prepared from the corresponding substituted hydroxynithrobenzenes by methods which include the following: a) reaction of the hydroxy nitrobenzene with a dialkyl alkyl halide or sulfonate ester (Method 5C) in the presence of a base, such as potassium carbonate, sodium carbonate, potassium hydroxide, sodium hydroxide, hydride of potassium or sodium hydride, in a suitable solvent such as acetone, N, N-dimethyl formamide, tetrahydrofuran or dimethyl sulfoxide at temperatures ranging from room temperature to the reflux temperature of the solvent, or; b) reaction of the hydroxy nitrobenzene with an alkyl alcohol, triphenylphosphine, and a dialkylazadicarboxylate reagent (Method 6), such as diethylazodicarboxylate, in an anhydrous aprotic solvent such as diethyl ether or tetrahydrofuran at temperatures ranging from 0 ° C to temperature of reflux of the solvent, essentially according to the methods described in Mitsunobu, 0. Synthesis 1981, 1 and reference herein. Further, with reference to Method 5A and 5E, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein at least one substituent R1-R5 is defined as alkoxy can be prepared substituted hydroxyarylamino-tertiary butyl carbamate by reaction with alkyl halides, tri fluorome tan sulphonates, 4-methybenzene sulphonates, dialkyl sulfonate, ethylene carbonate and the like in the presence of a suitable base such as carbonate potassium in a suitable solvent such as acetone, toluene, or N, N-dimethyl-formamide which varies from room temperature to the reflux temperature of the solvent. Alternatively, with reference to Methods 7A-G, the nitrobenzene intermediates that are ultimately converted to amines 2, Ri and / or R3 is alkoxy, and R2 and / or R4 is a halogen, and X is equal to a bond, they can be prepared by standard halogenation reactions which include the following: a) reaction of a 2- or 4-hydroxy-nitrobenzene with an aqueous sodium hypochlorite (Methods 7A and 7B), at room temperature or; b) reaction of a 2-hydroxy-4-methoxy or 2,4-dimethoxy-nitrobenzene (Method 7C and 7D) with bromine in a suitable solvent such as chloroform, dichloromethane, glacial acetic acid or the like in the presence or absence of trifluoroacetate of silver at room temperature, or; c) reaction of a 2,4-dimethoxytrin-trobenzene (Method 7E) with benzyltrimethylammonium dichloroiodate in the presence of anhydrous zinc chloride in a suitable solvent such as glacial acetic acid, at room temperature or; d) reaction of a 2-hydroxy-4-methoxynitrobenzene (Method 7F) with benzyltrimethylammonium dichloroiodate in the presence of sodium bicarbonate in a suitable solvent mixture such as dichloromethane and methanol, at room temperature or; e) reaction of a 2,4-dimethoxyne trobenzene (Method 7G) with 3,5-dichloro-1-fluoropyridine triflate in a suitable solvent such as tetrachloroethane, at a temperature ranging from room temperature to reflux temperature of the solvent.

With reference to Method 8, the nitrobenzene intermediates that are finally converted to amines 2, wherein R4 = -CF3, and R? ~ R3 and R5-R8 are defined as above and X is equal to a bond, can be prepare from the corresponding substituted 4-yodoni robbencenes by the reaction with t-rimethyl (trifluoromethyl) silane in the presence of cuprous iodide and potassium fluoride in a suitable solvent such as N, N-dimethylformamide or the like at a varying temperature from room temperature to the reflux temperature of the solvent in a sealed reaction vessel. With reference to Methods 19A and 19B, the nitrobenzene intermediates that are finally converted to amines 2, wherein R4 = -HNCOCH2NR7R8 or -HNCOCH2SR6, and R? -R3 and R5-R8 are defined as above and X is equal to a bond, can be prepared from the corresponding substitute 4- (N-chloroacet-il) -nit roaniline by reaction with either a suitable secondary amine such as dimethylamine, morpholine or the like in a suitable solvent such as mixtures of tetrahydrofuran and / or water at temperatures ranging from room temperature to the reflux temperature of the solvent or by reaction with an appropriate thiol in the presence of a suitable base such as sodium or potassium carbonate or the like in a suitable solvent such as tetrahydrofuran , 1,4-dioxane or the like at temperatures ranging from room temperature to the reflux temperature of the solvent. With reference to Method 25, the nitrobenzene intermediates which are ultimately converted to amines 2, wherein at least one substituent of R1-R5 is defined as triflate and X is equal to a bond, can be prepared from the corresponding phenol by the reaction with trifluoromethanesulfonic anhydride in the presence of a tertiary amine such as triethylamine or diisopropylethylamine or the like in a suitable solvent such as dichloromethane at temperatures ranging from 0 ° C to room temperature. With reference to Methods 9, 9B, and 10, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein at least one substituent of R1-R5 is defined as any alkyl phenyl or alkylsulfinyl can be prepared by the reaction of the appropriate 4-alkylthioacylamino or carbamoylarylamino derivative with an appropriate oxidizing agent such as dimethyloxirane or sodium periodate in a suitable solvent mixture such as acetone and dichloromethane or water at room temperature. ambient. With reference to Method 12, the carbamoyl amine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein R4 is defined as 1-hydroxyethyl and R? -R3 and 5 are defined as the above and X is equal to a bond, can be prepared by reacting the corresponding 4-vinylcarbamoylaniline with sodium borohydride in the presence of mercuric acetate in a suitable solvent such as tetrahydrofuran, 1,4-dioxane or the like and water at room temperature ambient. With reference to Method 13, the carbamoyl sheet derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein R4 is defined as 2-hydroxyethyl and R? ~ R3 and Rs are defined as in the foregoing and X is equal to a bond, it can be prepared by reacting the corresponding 4-vinylcarbamoylanyl ina with sodium borohydride in the presence of glacial acetic acid in a suitable solvent such as tetrahydrofuran, 1,4-dioxane or the like and water at temperatures that vary from 0 ° C to room temperature. With reference to Method 14, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein R4 is defined as 1-azidoethyl and R ~ R3 and R5 are defined as above and X is equal to a bond, can be prepared by reacting the corresponding 4- (1-hydroxyethyl) carbamoylaniline with hydrazoic acid in the presence of a dialkylazo dicarboxylate such as diethylazodicarboxylate and triphenyl osphine in a suitable solvent mixture such as tetrahydrofuran and dichloromethane at temperatures ranging from 0 ° C to room temperature. With reference to Method 15, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2 ,. wherein R4 is defined as 3-dimethylaminoprop-1-ynyl and R? -R3 and R5 are defined as above and X is defined in the foregoing, it can be prepared by reacting the corresponding 4-vinylcarbamoylaniline with 1-dimethylamino- 2-Propene in a suitable tertiary amine solvent such as triethylamine or diisopropyl-ethylamine in the presence of bis (triphenylphosphine) palladium (II) chloride and cuprous iodide at temperatures ranging from room temperature to the reflux temperature of the solvent. With reference to Method 16, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2 ,. wherein R4 is defined as 3-dimethylamino-acryloyl and R? -R3 and R5 are defined as above and X is equal to a bond, it can be prepared by reacting 4- (3-dimethylaminoprop-1-in) 1) carbamoi 1-aniline with a suitable peracid such as 3-chloroperoxybenzoic acid in a suitable solvent mixture such as dichloromethane and methanol at temperatures ranging from 0 ° C to room temperature. With reference to Methods 17 and 18, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein R is defined as any -isoxazol-5-yl or 4 - (lH -pyrazol-3-yl) and Rj.-R3 and R4 are defined as above and X is equal to a bond, they can be prepared by reacting the corresponding 4- (3-dimethylamino-acryloyl) carbamoylaniline with either hydroxylamine hydrochloride or hydrazine hydrate in a suitable solvent such as 1,4-dioxane or ethanol and the like at room temperature. With reference to Method 20, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein R4 = -HNC02Z, and R? -R3, R5 and Z are defined as above and X is equal to a bond, can be prepared by reacting the corresponding 4-amino-carbamoylaniline with 1, 1-carbonyl-di- (1, 2, 4) -triazole and an appropriately substituted alcohol in a suitable solvent mixture such as tetrahydrofuran and dichloromethane and the like at temperatures ranging from room temperature to the reflux temperature of the solvent. With reference to Methods 26 and 30, the carbamoylamine derivatives used as starting materials in Methods 3A-3C which are ultimately converted to amines 2, wherein at least one substituent of R1-R5 is defined as dialkylamino and X is defined; in the foregoing, they may be prepared by the reaction of appropriately substituted aldehydes in the presence of either sodium cyanoborohydride or hydrogen gas and 10% palladium on carbon in a suitable solvent such as mixtures of water, methanol, tetrahydrofuran or toluene or similar to room temperature. With reference to Methods 27 and 28, amines 2, wherein at least one substituent of R1-R5 is defined as hydroxy and X is defined in the foregoing, can be prepared by the reaction of the corresponding ester such as acetate with a base Suitable such as sodium bicarbonate or sodium hydroxide in a suitable solvent mixture such as methanol-water mixtures at temperatures ranging from room temperature to the reflux temperature of the solvent. With reference to Method 29, amines 2, wherein at least one substituent of R 1 -R 5 is defined as 2-hydroxybenzamido and X is defined in the foregoing, can be prepared by the reaction of N- (4-aminophenyl) - corresponding phthalimide with lithium borohydride in an appropriate solvent such as tetrahydrofuran, diethylether, or the like at room temperature. Intermediate amines 2, where R1-R5 are defined as above and X is equal to any -CH2- or - (CH2) 2-, can be prepared by the following procedures: a) reduction of a benzo- or phenylacetyl trile appropriately substituted with a borane-dimethylsulfide complex in a suitable solvent such as ethylene glycol dimethyl ether, tetrahydrofuran or the like at temperatures ranging from room temperature to the reflux temperature of the solvent. (Method 44); b) reduction under one or more atmospheres of hydrogen in the presence of a suitable catalyst such as 5% or 10% palladium on carbon and an acid such as 4-methyl-benzenesulfonic acid, hydrochloric acid or the like in a suitable solvent such as ethylene glycol monomethyl ether, ethyl acetate, ethanol or the like at room temperature. (Method 50); c) reduction with lithium aluminum hydride in a suitable solvent such as tetrahydrofuran or diethylether at temperatures ranging from 0 ° C to room temperature. (Method 51). The unsaturated nitro precursors that are used as starting materials in Method 51 and finally converted to amines 2, wherein R1-5 are defined as above and X is equal to - (CH2) 2- can be prepared by reacting a benzaldehyde appropriately substituted with nitro-methane in the presence of ammonium acetate in a suitable solvent such as acetic acid at temperatures ranging from room temperature to the reflux temperature of the solvent. (Method 53); The benzaldehydes, used as starting materials in Method 53, can be prepared by the reduction of diisobutylaluminum hydride of an appropriately substituted benzonitrile. (Method 52) Substituted benzonitriles, used as starting materials in Method 52, can be prepared from the corresponding aryl bromide by reaction with copper cyanide in a suitable solvent such as N, N-dimethylformamide at temperatures that they vary from the ambient temperature to the reflux temperature of the solvent. (Method 59) For amines 2, wherein R1-R5 is defined as above and X is equal to any of 0 (CH2) 2NH2 or -S (CH2) 2NH2, the necessary nitrile precursors can be prepared by the reaction of a phenol or thiophenol appropriately substituted with bromoacetonitrile in the presence of a suitable base such as potassium carbonate in a suitable solvent such as acetone at room temperature according to Method 49. Alternatively, for amines 2, wherein R 1 -R 5 defined as in the above and X is equal to - (CH2) 3-, the nitrile precursors can be prepared essentially according to the procedure of Wilk, B. Syn the ti c Comm. 23, 2481 (1993), by the reaction of a phenetanol appropriately substituted with acetone cyanohydrin and triphenylphosphine in the presence of a suitable azodicarboxylate such as diethyl azodicarboxylate in an appropriate solvent such as diethyl ether or tetrahydrofuran or the like at temperatures ranging from 0 °. C at room temperature. (Method 54) alternatively, intermediary amines 2, wherein R1-R5 are defined as above and X is equal to - (CH (CH3)) - can be prepared by catalyzed hydrolysis of base or acid of the corresponding formamide using an acid catalyst Suitable such as 6N hydrochloric acid or a suitable base catalyst such as 5N sodium or potassium hydroxide in an appropriate solvent mixture such as water and methanol or water and ethanol at temperatures ranging from room temperature to the reflux temperature of the solvent . (Method 46) The formamide precursors used as starting materials in Method 46 and which are finally converted to amines 2, are prepared according to Method 45 by treatment of an acetophencna appropriately substituted with ammonium, formic acid and formamide at temperatures that vary from the ambient temperature to the reflux temperature of the solvent. Alternatively, the amines 2, wherein R1-R5 are defined as above and X is equal to - (CH (CH3)) - can be prepared by the reduction of an appropriately substituted 0-methyl oxime in the presence of sodium borohydride and zirconium tetrachloride in a suitable solvent such as tetrahydrofuran or diethylether at room temperature. Method 48 essentially in accordance with the procedure of Itsuno, S., Sakurai, Y., Ito, K. Syn thes is 1988, 995. The desired O-methylloximes can be prepared from the corresponding acetophenone by the reaction with hydrochloride of methoxylamine and pyridine in a suitable solvent such as ethanol or methanol at temperatures ranging from room temperature to the reflux temperature of the solvent. (Method 47) Amines 2 for which R1-R5 are defined as above and X is equal to -CH (J) - where J is defined as above, can be prepared by reducing. of the ketone appropriately substituted by the methods described above (Methods 45, 47, and 48). These desired ketones, when not commercially available, can be prepared by the reaction of a suitably substituted benzaldehyde with an appropriate organometallic reagent such as phenyl lithium, isopropylmagnesium bromide or ethylmagnesium bromide or the like in a suitable solvent such as diethyl ether. : ether or tetrahydrofuran at temperatures ranging from -78 ° C to 0 ° C. (Method 57) The resultant alcohols can be oxidized to the corresponding ketone with an appropriate oxidizing agent such as chromium trioxide in aqueous sulfuric acid or pyridinium chlorochromate or pyridium dichromate in an appropriate solvent such as dichloromethane or the like at room temperature. . (Method 58) The intermediate anilines 5 can be prepared as previously described in Method 3A. Treating in this way the phenylcarbamic acid ter-butylester 6, wherein G is described as above, with pure trifluoroacetic acid at room temperature followed by neutralization with aqueous sodium hydroxide yields the desired anilines. The desired carbamic acid esters, wherein R9-R12 and G are described as above, are prepared as shown in Method 2C by the reaction of substituted acid chlorides, 8, where G is described as in the above , and the ter-but-esters of 4-aminophenylcarbamics 7, wherein Rg-R? 2 are described as above, in the presence of triethylamine in an appropriate solvent such as dichloromethane, dimethyl sulfoxide or dimethyl formamide or mixtures thereof. same. The carboxylic acid chlorides 8 are either commercially available or prepared from the carboxylic acid.Lco corresponding by the reaction with oxalyl chloride in a suitable solvent such as dichloromethane at room temperature.

Method 2C, 3A Alternatively, carbamic acid esters 6, wherein Rg-R 2 and G are described as above, are prepared as shown in Method 2E by the reaction of substituted carboxylic acids 8a, in dc > nde G is described as above, and ter-butyl esters of appropriately substituted 4-aminophenylcarbamic acid 7 in the presence of a suitable coupling agent such as benzotriazol-1-yloxy-tris- (dimethylamino) phosphonium hexafluorophosphate, hexafluorophosphate 2 - (1H-benzothiazol-1-yloxy) -1,3,3-tetramethyluronium, dicyclohexylcarbodiimide or the like in the presence of a tertiary amine base such as triethylamine or diisopropylethylamine in a suitable solvent such as dichloromethane, dimethylformamide and similar, at room temperature to produce the corresponding arylaminoamide. The carboxylic acids 8a are either commercially available or are prepared according to the methods of the literature. For example, when G is a substituted thiadiazole, the acid is available from the corresponding carboxylic acid ester by reaction with an appropriate base such as sodium or potassium hydroxide in a mixture of a suitable solvent such as methanol or ethanol and water. room temperature . Similarly, when G is either substituted or unsubstituted thiazole, substituted or unsubstituted oxazole, substituted or unsubstituted isothiazole or substituted or unsubstituted isoxazole, when not commercially available, the carboxylic acid 8a is available from the corresponding ethyl or methyl ester. by reaction with an appropriate base such as sodium or potassium hydroxide in a suitable solvent mixture such as methanol or ethanol and water at room temperature. These esters are either commercially available or can be prepared according to the methods of the literature. When the carboxylic acid ester precursors that are finally converted to 8a acids are not commercially available, they can be prepared by methods known in the literature. For example, the ethers of 1, 2, 3-thiadiazole-4-carboxylic acid 5-their compounds can be prepared essentially according to the method of Caron, M. J. Org. Ch em. 51, 4075 (1986) and Taber, D.F., Ruckle, P. E. J. Amer. Ch em. Soc. 108, 7686 (1986). Thus, according to Method 21, the treatment of an ester of beta-keto carboxylic acid with 4-methylbenzenesul fonyl azide or methanesulfonyl azide or the like in the presence of a tertiary amine base such as triethylamine or diisopropylethylamine in a suitable solvent such as acetonitrile yields the diazo-beta-keto carboxylic acid ester. The treatment of this compound with 2,4-bis (4-methoxy phenyl) -l, 3-dithia-2,4-diphosphetane-2,4-disulfide in a suitable solvent such as benzene or toluene or the like at varying temperatures from the ambient temperature to the reflux temperature of the solvent, gives the 1,2-thiadiazole-4-carboxylic acid ester 5-its substituted. alternatively, the esters of 1,2,3-thiadiazole-5-carboxylic acid 4-their compounds can be prepared essentially according to the procedure of Shafiee, A., Lalezari, I., Yazdani, S., Shahbazian , FM, Partovi, TJ Pha rma ceu ti ca l Sci. 65, 304 (1976). Thus, according to Method 22 and 23, the reaction of an appropriately substituted beta-keto carboxylic acid ester in a suitable alcohol solvent such as methanol or ethanol with an aqueous solution of semicarbazide hydrochloride at temperatures varying from the ambient temperature at the reflux temperature of the solvent in the presence of a suitable base such as pyridine gives the corresponding semicarba zone derivative. Treatment of this compound with pure thionyl chloride at 0 ° C followed by treatment with an excess aqueous solution of sodium bicarbonate produces the 4-substituted 1, 2, 3-ticdiazole-5-carboxylic acid esters. The 4-carboalkoxythiazoles are prepared essentially according to the Scholkopf procedure, U., Porsch, P., Lau., H. Li ebi gs Ann. Chem. 1444 (1979). Thus, according to Method 55 and 56, the reaction of ethyl isocyanoacetate with N, N-dimethylformamide dimethylacetal in a suitable alcohol solvent such as ethanol at room temperature gives the ethyl ester of 3-dimethylamino acid Corresponding isocyano-acrylic. A solution of this compound in a suitable solvent such as tetrahydrofuran with gaseous hydrogen sulfide was treated in the presence of a suitable tertiary amine base such as triethylamine or diisopropylenetriamine or the like at room temperature to give the corresponding 4-carbethoxy-thiazole.

The additional appropriately substituted thiazoles can be prepared essentially according to the procedure of Bredenkamp, M.W., Holzafel, C.W., van Zyl, W.J. Syn the t i c Comm. 20, 2235 (1990). The appropriate unsaturated oxazoles were prepared, essentially according to the procedure of Henneke, K.H., Scholkopf, U., Neudecker, T. Li ebi gs Ann. Chem. 1979 (1979). Suitable oxazoles can be prepared, essentially in accordance with the procedures of Galeotti, N., Montagne, C., Poncet, J., Jouin, P. Te trah edron Le t t. 33, 2807, (1992) and Shin, C, Okumura, K., Ito, A., Nakamura, Y. Ch emi s t r and Le t t. 1305, (1994). The following specific examples are illustrative, but does not mean that they are limiting of the present invention.

EXAMPLE 1 (METHOD 1A) 4-Methoxy-3-trif-uorornethyl-phenylamine A suspension of 4-methoxy-3-tri fluoromet il-nitrobenzene (2.2 g) and iron powder (1.68 g) in ethanol (35 ml) was treated with a solution of concentrated hydrochloric acid (0.42 ml) in ethanol (6 ml) and water (3 ml) and the mixture was heated to reflux for about 1 hour. The mixture was then cooled, filtered, and concentrated under reduced pressure. The resulting oil was dissolved in ethyl acetate and extracted three times with 5% aqueous hydrochloric acid.

The collected acidic extracts were then cooled in an ice bath and basified with solid potassium carbonate, then extracted with ethyl acetate.

These organic extracts were washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate, concentrated under reduced pressure, then passed through a short column of silica gel. (ethyl acetate was used as the eluent) to provide the desired compound as an amber oil. Using the above procedure and appropriate starting materials, the following compounds are prepared: 2,6-Dichloro-benzene-1,4-diamine-3-chloro-4-methylsulfanyl-phenylamine 2,6-Dibromo-benzene-4. -diamine 3-Chloro-4-trifluoromethyl-phenylamine 3-Chloro-4-ethylsulfanyl-phenylamine 4-Met oxy-3-trifluoromethyl-phenylamine 3,5-Di-chloro-4-methoxy-2-methyl-1-phenylamine 5-Chloro-2-ethoxy-4-methoxy-phenylamine 5-Chloro--ethoxy-2-methoxy-phenylamine 5-iodo-2,4-dimethoxy-phenylamine 3, 5-Diioco-2,4-dimethoxy-phenyl 3, 5-Dibrcmo-2,4-dimethoxy-phenylamine 5-Chloro-2-methoxy-4-metyl-phenylamine 2-Chloro-K (l), N (1) -dimethyl-benzene-1,4-diamine 3-Chloro-4-piperidin-1-yl-phenylamine 3-Chloro-pyr ol idin-1-yl-phenyl plate (1) -Benzyl-2-chloro-benzene-l, 4-diamine 3-Chloro-4 - (4-Methyl-piperazin-1-yl) -phenylamine 2-Chloro- (1) -methyl-N (1) - (1-met i 1 -piperidin-4-yl) -benzene-1,4-diamine 2-Chloro-K (l) -methyl-N (l) - (1-met il-pyrrol idin-3-yl) -benzene-1,4-diamine 2-Chloro-K (l) -me Til-N (l) -phenyl-benzene-1, -di amine N (1) - (1-Benzyl-pyrrolidin-3-yl) -2-chloro-N (1) -methylbenzene-1, 4 - diamine 2-Chloro-IN (l) -cyclopentyl-N (l) -met-il-benzene-1,4-diamine 2- [(4-amino-2-chloro-phenyl) - (2-hydroxy-ethyl) -amino] - ethanol 2-Chloro-N (l) -hexyl-N (l) -methyl-benzene-1,4-diamine 2-Chloro-K (l) -isobutyl-N (l) -met-il-benzene - 1,4-diamine 2- [(4-amino-2-chloro-phenyl) -methyl-amino] -ethanol 2-chloro-K (l) - (3-dimethylamino-propyl) -N (1) - methyl-benzene-1,4-diamine 2-chloro-N (1) - (2-dimethylamino-ethyl) -N (1) -methyl-benzene-1,4-diamine 2-chloro- (1) - ( 2-dimethylamino-ethyl) -benzene-1,4-di-amine (1) - (1-Benzyl-piperidin-4-yl) -2-chloro-benzene, 4-di-am: na 2 -Cloro-N (l) - (2-methoxy-ethyl) -N (1) -met-il-benzene-, 4-diamine 2-Chloro-N (1) - (3-dimethylamino-propyl) -benzene 1,4-diamine N (1) - (1-ene-pyrrolidin-3-yl) -2-chloro-benzene-4-diamine 3-chloro-4- (1-methyl-piperidin-4-yloxy) phenylamine 3-chloro-4- (2-dimethylamino-ethoxy) -phenylamine 3-chloro-4- (3-dime) tilamino-propoxy) -phenylamine 3-Chloro-4- (l-methyl-pyrrolidin-3-yloxy) -phenylamine 3-Chloro-4-cyclohexyloxy-phenyl plate.

EXAMPLE 2 (METHOD IB) 4 -Bromo-2, 4-dimethoxy-phenylamine A suspension of 4-bromo-2, 4-dimethoxy-nitrobenzene (0.48 g) and iron powder (0.42 g) in acetic acid (10 ml) and ethanol (10 ml) was heated at 120 ° C for about 5 hours. The mixture was then cooled, filtered, and concentrated under reduced pressure. Water was added and the mixture was cooled in an ice bath and neutralized with solid potassium carbonate then extracted with dichloromethane. These organic extracts were washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate, concentrated under reduced pressure, then chromatographed on silica gel (20% ethyl acetate in hexanes was used as the eluent ) to provide the desired compound as an amber colored oil.

EXAMPLE 3 (METHOD 1C) Tez-Butylester of (4-amino-2,6-dichloro-enoxy) -acetic acid A solution of tert-but-lyses ter (4-nitro-2, -dichloro-phenoxy) - acetic acid (1 g) in ethanol (17 ml) and water (8.6 ml) was treated with iron powder (0.861 g) and ammonium chloride (86 mg) and the mixture was heated to reflux for about 1 hour. The mixture was then filtered and concentrated under reduced pressure. The resulting oil was partitioned between water and ethyl acetate, and the organic phase was washed with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to provide the desired compound as a pale yellow solid. .

Using the above procedure and appropriate starting materials, the following compounds were prepared: 4-Chloro-benzene-1, 2-diamine N- (4-amino-2-chlorophenyl) -acetamide (4 -Amino-2, 6 -dichloro-phenoxy) -acetonitrile (4-Amino-2,6-dichloro-phenoxy) -acetic acid (2-amino-4-chloro-5-methoxy-phenoxy) -acetonitrile (4-Amino-2,6-dichloro-phenoxy) -acetonitrile Methyl ester (4-amino) -amino-2-chloro-5-methoxy-phenoxy) -acetic acid (4-amino-2-chloro-5-methoxy-phenoxy) -acetic acid tert-butyl ester (2-amino- -chloro-5-methoxy-phenoxy) -acetic (1) -Benyl-4-chloro-5-methoxy-benzene-l, 2-diamine N- (4-Amino-2-chloro-phenyl) -2- Fluoro-benzamide N- (4-Amino-5-chloro-2-hydroxy-phenyl) -acetamide N- (4-amino-5-chloro-2-hydroxy-phenyl) -2-fluoro-benzamide (4-amino- 2-chloro-phenyl) -amide of furan-2-carb-3-oxidic acid (4-amino-2-chloro-phenyl) -carbamic acid ester N- (4-Amino-5-chloro-2-methyl-phenyl) - acetamide N- (4-amino-5-chloro-2) -met-il-phenyl) -2-fluoro-benzamide (furan-2-carboxylic acid 4-amino-5-chloro-2-methyl-phenyl) amide N- (4-Amir.o-3-chloro-phenyl) ) -2-fluoro-benzamide (4-amino-3-chloro-phenyl) -amide of furan-2-carboxylic acid N- (4-Amino-2-chloro-phenyl-2-dimethylamino-acetamide N- ( 4-Amino-2-chloro-phenyl-2-piperidin-1-yl-acetamide N- (4-Amino-2-chloro-phenyl-2-morpholin-4-yl-acetamide N- (4-Amyr? - 2-chloro-phenyl-methanesulfonamide N- (4-Amino-2-chloro-phenyl-benzamide N- (4-amino-2-chloro-phenyl-2-diethylamino-acetamide N- (4-amino-2-chloro- phenyl-2-pyrrolidin-1-yl-acetamide - (4-amino-2-chloro-phenyl-2-azepan-1-yl-acetamide N- (4-amino-2-chloro-phenyl) -2- (2- methyl 1-piperidin-1-yl) -acetamide N- (4-amino-2-chloro-phenyl) -2- (3-methyl-piperidin-1-yl) -acet amide 3-chloro-benzene-2 -diamine 4-chloro-N, N-dimethyl-benzene-l, 2-diamine.

EXAMPLE 4 (METHOD ID) 3, 5-Dichloro-4-phenoxy-phenylamine To a suspension of 3,5-dichloro-4-phenoxy-nitrobenzene (6.1 g) and tin powder (12 g) was added dropwise acid concentrated hydrochloric acid (60 ml). Ethanol (60 ml) was added and the mixture was heated to reflux for about 1 hour. The mixture was then cooled in an ice bath and basified by the addition of solid sodium hydroxide. The resulting suspension was filtered through a diatomaceous earth bearing and extracted three times with ethyl acetate. The combined organic extracts were then washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to give a product as a yellow solid. Recrystallization from ethyl acetate-hexanes gave the product as a pale yellow solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: l-Furan-2-yl-ethyl-3-chloro-4-isopropoxy-phenylamine 2 -Butoxy-5-chloro-4-methoxy-phenylalanine 3 , 5Diclo? o-2-methoxy-4-methyl-phenylamine 2-Benzyloxy-5-chloro-4-methoxy-phenyl 4-benzylcxy-5-chloro-2-methoxy-phenylamine 5-Fluoro-2,4-dimethoxy-phenylamine Ethyl ester (4-amino-2,6-dichloro-phenoxy) -acetic acid 3,5-dichloro-phenoxy-phenylamine 2- (4-amino-2-chloro-5-methoxy-phenoxy) -acetamide (4 - Ami no-2-chloro-5-methoxy-phenoxy) -acetonitrile 2- (2-Amino-4-chloro-5-methoxy-phenoxy) -ethanol 2- (4-amino-2-c-5-methoxy-methoxy) phenoxy) -ethanol 4- (4-amino-2-chloro-5-methoxy-phenoxy) -but ironit ryl -Ami non-chloro-5-methoxy-phenol 2 -Ami no-? -chloro-5-methoxy-phenol 5-chloro-methoxy-2-morpholin-4-yl-phenylamine 4-chloro-5-methoxy-N (l), N (l) -dimethyl-benzene-l, 2-diamine 5-Chloro-β-methoxy-2-piperidin-1-yl-phenylamine 5-Chloro-. -methoxy-2-pyrrol idinyl 1-pheny lamin 2 -chloro-N (1) -cyclohexyl-N (1) -methyl-benzene-1,4-diamine (2) -benzyl-4-methoxy-benzene 1,2-diamine 2- (4-amino-2-chloro-phenoxy) -ethanol 2-chloro-N (l) -cyclohexyl-N (l) -ethyl-benzene-l, 4-diamine 4 -Butoxy -3 -chloro-phenylamino (4-amino-2-chlorophenoxy) -acetonitrile 2-chloro-N (1) -cyclohexyl-benzene-1, -diamine 2-chloro-N (l), N (l) -dipropil -benzene-1, 4-diamine 3-chloro-4- (2, 2, 2-trifluoro-ethoxy) -phenylamine 3-chloro- - (octahydro-quinolin-1-yl) -phenylamine (1) -Alil-2 -chloro-N (1) -cyclohexyl-benzene-1,4-diamine N- (4-Amino.o-2-methoxy-5-methyl-yl-phenyl) -2-fluoro-benzamide (4-Amino- 2- methoxy-5-methyl-phenyl) furan-2-carboxylic acid amide N- (4-Amir.o-naphthen-1-yl) -2-fluoro-benzamide 3-Chloro-M, N-dimethyl-benzene 1,2-diamine 3-Chloro-4-propoxy-phenylamine 3 -Oodo- 4 -methoxy-phenylamine 3-Chloro-2,4-dimethoxy-aniline 3-Bromo-methoxy-phenylamine 3-Chloro-4-ethoxy- phenyl amine EXAMPLE 5 (Method 1E) 4- (Amino-phenyl) -carbamic acid isobulester It was added to a solution of N- (4-Nitro-phenyl) -isobutyral lamide (2.0 g) in 100 ml of ethylene glycol monomethyl ether (100 ml). ml) 10% palladium on carbon (275 mg). The mixture is hydrogen for 2 hours at room temperature under 30 psi of hydrogen in a Parr hydrogenation apparatus. The catalyst was then removed by filtration through diatomaceous earth and the filtrate was evaporated to dryness under reduced pressure by a three-fold azeotropic process with heptane. Trituration of the residue with heptane produces the desired product as a white solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: 2 -Meti 1-2'H-benzoimidazol-5-ylamine N- (4-Amino-phenyl) -formamide lH-Benzoimidazol-5-ylamine Isobutyl ester of (4-amino-phenyl) -carbamic acid N- (4-Amino-phenyl) -isobutyramide N- (5-Amino-pyridin-2-yl) -2-methyl-yl-benzamide (5-Amino-pyridin-2-) il) -furan-2-carboxylic acid amide N- (5-Amir.o-pyridin-2-yl) -2-fluoro-benzamide [6- (2, 2, 2- t) -butyl ester ri-fluoro-acetylamino) -pyridin-3-yl] -carbamic acid N- (5-Amyr o-pyridin-2-yl) -2,2, 2-trifluoro-acetamide Ter-butyl ester of (4-amino-benzyl) -carbamic acid 2- (3, 5-Bis-tri-fluoromet-il-phenyl) -eti-lane 1-tert-Butyl-lH-imidazol-2-ylamine 3- (3-Dimethylamino-propyl) -5-tri-fluoromethyl-phenylamine EXAMPLE 6 (METHOD 1F) N- (4-Amino-2-methylphenyl) -2-fluorobenzamide A mixture of 2-fluoro-N- (2-met il-4-nitre rofeni 1) benzamide (4.55 g) was refluxed. ), cyclohexane (30 ml), ethanol (70 ml), water (30 ml) and 10% palladium on charcoal (3 g) for 30 minutes. The mixture was filtered through diatomaceous earth and concentrated under reduced pressure. The resulting oil was dissolved in 50 ml of ethyl acetate and cooled to 4 ° C for 12 hours. Filtration produced the product as a brown solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- (4-Amir or-2-methyl-phenyl) -acetamide 2-Methyl-benzooxazol-6-ylamine N- (4-Amir or-3 -methoxy-phenyl) -acetamide 2-a-cetylamino-5-amino-benzoic acid N- (4-amir o-phenyl) -acetamide -th- (4- (3-amino-benzoylamino) -phene-L-butyl ester) ] -carbamic Ter [butyl ester of [4- (2-amino-benzoylamino) -pheni]] -carbamic acid N- (4-Amino-2-cyano-phenyl) -acetamide N- (4-Amir o-2, 5-dimethoxy-phenyl) -2-f-luoro-benzamide (4-Amino-2, 5-dimethoxy-phenyl) -amide of furan-2-carboxylic acid N- (4-Amino-2-cyano-phenyl) -2 -fluoro-benzamide (4-Amino-2-methoxy-phenyl) -amide of furan-2-carboxylic acid N- (4-Amino-2-methoxy-phenyl) -2-fluoro-benzamide N- (4 -Amino -2-methoxy-5-meth i 1- phenyl) -acetamide N- (4-Amyr o-2-benzoyl-phenyl) -acetamide N- (4-Amino-2-benzoyl-phenyl) -2-fluoro-benza ida (4-Amino-2-benzoyl-phenyl) -amide acid ran-2-carboxylic N- (4-amino-3-methylphenyl) -acetamide N- (4-Amir. o-3-methyl-phenyl) -2-fluoro-benzamide (furan-2-carboxylic acid 4-amino-3-methyl-yl-phenyl) -amide 5-Amino-2- [(2-fluorobenzoyl) amino] N- (4-Amino-naphthalen-1-yl) -acetamide (4-amino-naphthalene-1-yl) -N-phenylbenzamide (4-amino-2-phenylcarbamoyl-phenyl) amide of furan-2-carboxylic acid ) -furan-2-carboxylic acid amide N- (4-Amin or-2-tri-fluorophenyl-phenyl) -acetamide (4-amino-2-cyano-phenyl) -amide of furan-2-carboxylic acid (4-) Amino-2-trifluoromethyl-phenyl) -amide of furan-2-carboxylic acid N- (4-Amir or-2-methyl-phenyl) -2-fluoro-benzamide (4-Amino-2-methyl-yl-phenyl) ) -furan-2-carboxylic acid amide 5-amino-2- (2-fluoro-benzoylamino) -benzoic acid 5-amino-2- [(furan-2-carbonyl) -amino] -benzoic acid N- (4) -Amir or-2-cyano-phenyl) -2, 2, 2-trifluoro-acetamide N- (4 -Amin or -3-met-il-phenyl) -2,6-di-fluoro-benzamide N- (4-Amino -3-tri fluoromet-phenyl) -acetamide N- (4-amino-3-trifluoromethyl-phenyl) -2-fluorobenza Measure N- (4-Amino-2-trifluororneti 1-phenyl) -2,2,2-trifluoroacetamide N- (4-amino-2-methoxy-phenyl) -2,2,2-trifluoroacetamide N- (4-Amino-2-trifluoromethyl-phenyl) -2-fluoro-N- (2-fluoro-benzoyl) -benzamide N- (4-Amino-2-trifluoromethyl-phenyl) -2-fluoro-benzamide EXAMPLE 7 (METHOD 16) N- (4-Amino-2-chlorophenyl) -2-thiomorpholino-4-yl-acetamide A solution of N- (2-chloro-4-nitropheni.l) -2-thiomorpholino- 4-yl-acetamide (3.02 g) in ethanol (200 ml) to a solution of sodium thiosulfate (12 g) in water (60 ml). The mixture was refluxed for 12 hours, cooled and poured into water. The mixture was then extracted with ethyl acetate. The ethyl acetate solution was washed twice with saturated aqueous sodium chloride, dried over anhydrous potassium carbonate, filtered through a domaceous earth bearing and concentrated under reduced pressure to give an oil. Toluene was added and the solution was cooled to give the desired product as a light orange crystalline solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- (4-amino-2-chloro-phenyl) -2-t -omorpholin-4-yl-acetamide N- (4-Amyr-2) -chloro-phenyl) -2-dipropylamino-acetamide EXAMPLE 8 (METHOD 2A) (3-Chloro-4-iodo-phenyl) -carbamic acid tert-butylester It was added to a solution of 3-chloro-4-iodo-aniline (10 g) in tetrahydrofuran (40 ml) containing diisopropylethylamine (6.9 ml) di-tert-butyl-dicarbonate (8.6 g) and the mixture was heated to reflux. After approximately 15 hours the additional portions of diisopropylethylamine (6.9 ml) and di-tert-butyl-dicarbonate (21 g) were added and heating continued for approximately 24 hours. The solution was then cooled, concentrated under reduced pressure, diluted with ethyl acetate, and washed sequentially three times with 5% aqueous hydrochloric acid then once with saturated aqueous sodium chloride. The solution was dried over sodium sulfate. Anhydrous was then concentrated under reduced pressure to provide the desired crude product as a brown oil. Crystallization was induced by the addition of hexanes, and the collected solid material was recrystallized from hexanes to give the desired product as a white solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: N '- (4-nit ro-benzoyl) -hydrazin-carboxylic acid tert-butylester (3-Chloro-4-iodo-phenyl) -carbamic acid tert-butylester (4-Bromo-3-) acid chloro-phenyl) -carbamic Ter-buti ester of (3-chloro-4-vinyl-phenyl) -carbamic acid (3-chloro-4-methylsulfanyl-phenyl) -carbamic acid tert-butylester -amino-3-chloro-phenyl) -carbamic (4-Chloro-2-nitro-phenyl) -carbamic acid tert-butylester (3-tert-butoxycarbonylamino-5-chloro-phenyl) -carbamic acid tert-butylester Ter -butyl ester (4-nitro-benzyl) -carbamic acid (3-bromo-5-trifluoromethyl-L-carbamic acid) -carbamic acid ester (2-amino-3-chloro-5-) tri fluoromet i 1- phenyl) -carbamic EXAMPLE 9 (METHOD 2B) 2-Trimet (3-Chloro-4-vinyl-phenyl) -carbamic acid Lysilanyl-tilastoster It was added to a solution of 3-chloro-4-vinyl-phenylalan.a (3.4 g) in N, N-dimethylformamide (44 ml) containing diisopropylethylamine (5.8 ml) 1- [2- (trimethylsilyl) -et oxycarbonyl-oxy] benzotriazole (7.1 g) and the mixture was stirred at room temperature under one atmosphere of argon for three days. The solution was then diluted with water and extracted three times with diethyl ether. The combined organic extracts were washed successively with water, saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The resulting residue was chromatographed on silica gel (10% ethyl acetate in hexanes was used as the eluent) to provide the desired product as a yellow oil.

EXAMPLE 10 (METHOD 2C) [4- (2-Luoro-benzoylamino) -phenyl] -carbamic acid tert-butyl ester Added to a solution of mono-N- (t-butoxy-carbonyl) -1, 4 - phenylenediamine (1.58 g) and triethylamine (1.50 ml) in 25 ml of dichloromethane o-fluorobenzoyl chloride (1.20 g). A formed solid is immediately formed and filtered and washed with fresh solvent to produce a white solid, 190 g. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- (3-Methoxy-4-n-t-phenyl) -acetamide N- (4-Amino-phenyl) -isobutyrylamide 2.2.2- Trifluoro-N- (2-methoxy-4-nitrophenyl) -acetamide [4- (2-methyl-t-benzoylamino) -pheni-L] -carbamic acid-tert-butylester 2- (4-tert-Butoxycarbonylamino-phenylcarbamoyl) -phenyl-ester of acetic acid Tert-butylester of acid [4- (4-Fluoro-benzoylamino) -pheni.L] -carbamic acid [4- (3-fluoro-benzoylamino) -phenyL] -carbamic acid [4 - (2-fluoro-benzoylamino]] -butylester. ) - Pheni L] -carbamic [4- (2-methoxy-benzoylamino) -pheni-L] -carbamic acid tert-butylester [4- (3-methoxy-benzoylamino) -pheni] -carbamic acid tert-butylester Ter-buti ester of [4 - (4-methoxy-benzoylamino) -pheni L] -carbamic acid [4- (2, 2-dimethyl-l-propionylamino) -phenyl] -carbamic acid tert-butylester [4- (2-bromo-acetyl-amino) -pheni] -carbamic acid [4- (2, 2, 2-trifluoroacet-ylamino) -phenyl] -carbamic acid acid tert-butylester -benzoylamino-phenyl) -carbamic acid tert-butylester (-metan sulfonylamino-phenyl) -carbamic acid (4-phenylacetylamino-phenyl) -carbamic acid tert-butylester Ter-butylester of acid. { 4 - [(thiophene-2-carbonyl) -amino] -phenyl} -carbamic [4 - (3-nit ro-benzoylamino) -phenyl] -carbamic acid tert-butylester [4- (3-Acetylamino-benzoylamino) -phenyl] -carbamic acid tert-butylester Tert-butylester of acid [4- (3-methylsulfonylamino-benzylamino) -phenyl] -carbamic acid [3- [[[4-; [(1, 1-Dimethylethoxy) carbonyl] amino] phenyl] -amino] carbonyl] phenyl] -carbamic acid ethyl ester Ter-but üiés ter [4- (2-tri fluoromet-il-benzoylamino) -phenyl] -carbamic acid Ter - [4- (2,6-difluoro-benzoylamino) -phenyl] -carbamic acid butyl ester [4- (2-Chloro-benzoylamino) -phenyl] -carbamic acid butyl ester Ter-butyl ester of acid [4 - (2-bromo-benzoylamino) -phenyl] -carbamic Ter-buti. [4- (2-nit ro-benzoylamino) -phenyl] -carbamic acid ester Ter-but i Les ter de ácido. { 4 - [(benzo [b] thiophen-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(pyridine-4-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(naphthalene-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4 - [(naphthalen-1 -carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(3-bromo-thiophene-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(biphenyl-2-carbonyl) -amin] -phenyl} -carbamic N- (4-tert-butoxycarbonyl amino-phenyl) -phthalamic acid [4- (2,3-difluoro-benzoylamino) -phenyl] -carbamic acid tert-butylester [4- (2, 5-difluoro-benzoylamino) -phenyl] -carbamic acid tert-butylester [Tert-butylester] [ 4- (2,4-difluoro-benzoylamino) -phenyl] -carbamic acid [4- (2-acetylaminobenz or ylamino) -phenyl] -carbamic acid tert-butylester [4- (2-methanesulfonylamino]] -butylester benzoylamino) -phenyl] -carbamic acid [4- (2,3-, 4-trifluorobenzoylamino) -phenyl] -carbamic acid tert-butylester [4- (2, 3, 4, 5, 6-pentafluorobenzoylamino) -phenyl] -carbamic N- (tert-butoxycarbonylamino-phenyl) L-isophthalamic acid methyl ester 2-Methyls l-nyl-N- [4- (2,2, 2-trifluoroacetylamino ) - feni.L] -benzamide [4- (3-Benzyloxy-benzoylamino) -pheni.L] -carbamic acid tert-butyl ester [4- (3-butoxy-benzoylamino) -pheni acid] butyl ester. ] -carbamic Ter-buti acid ester. { 4- [(5-difluoromethyl-furan-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4 - [(t-iofen-3-carbonyl) -amino] -phenyl} -carbamic Ter-buti acid ester. { 4- [(5-methyl-furan-2-carb nyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(5-bromo-furan-2-carbonyl) -amino] -phenyl} -carbamic Ter-butylester of (4-hexanoylamino-phenyl) -carbamic acid [4- (2-T-pheno-2-yl-acetylamino) -phenyl] -carbamic acid tert-butylester Acid tert-butylester. { 4- [(Pyridine-3-carbonyl) -amine or] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(4-bromo-furanedicarbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(furan-3-carbonyl) -amino] -pheni 1} -carbamic Ter-butylester (4-phenoxycarbonylamino-phenyl) carbamic acid tert-butylester. { 4 - [(benzo [1, 3] dioxol-4 • carbonyl) -amino] -phenyl} -carbamic acid [4- (3-trifluoromethoxy-benzoyl-amino) -phenyl] -carbamic acid tert-butylester N- (2,5-dimethoxy-4-nitro-phenyl) -2-fluoro-benzamide acid tert-butylester . { 4- [(furan-2-carbonyl) -amino] -phenyl} -carbamic acid [4- (2-phenoxy-acetylamino) -phenyl] -carbamic acid tert-butylester. { 4- [(5-ni tro-furan-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(5-chloro-furan-2-carboni 1) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(3-met il-furan-2-carbonyl) -amino] -phenyl} -carbamic acid [4- (2-methoxy-acetylamino) -phenyl] -carbamic acid tert-butylester. { 4- [(4-furan-3-yl- [1, 2, 3] -tiad azole-5-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(5-Butyl-furan-2-carbonyl) -amino] -phenyl} -carbamic N- [3-Cyano-4- (2, 2, 2-trifluoro-acetylamino) -phenyl] -2-fluoro-benzamide [3-Cyano-4- (2,2,2-trifluoro) Furan-2-carboxylic acid N- (4-Acetylamino-2-cyano-phenyl) -2,2,2-trifluoroacetamide 2,2,2-Trifluoro-N- (4-acetylamino) -phenyl] amide of furan-2-carboxylic acid -not r-2-trifluoromethyl-phenyl) -acetamide N- (4-Acetyl-lamino-2-trifluoromethyl-phenyl) -2, 2, 2-trifluoro-acetamide 2-Fluoro-N- [4- ( 2,2,2-trifluoroacetylamino) -3-trifluoromethyl-phenyl] benzamide [4- (2, 2, -trifluoro-acetylamino) -3-trifluoromethyl-phenol] furan-2-carboxylic acid-2-carboxylic acid -Fluoro-N- (2-met il-benzooxa-lol-6-yl) -benzamide 4- (2-Fluoro-benzoylamino) -2- hydroxy-dibutylbenzoic acid acid tert-butylester. { 4- [(I-Soxazol-5-carboni 1) -amino] -phenyl} -carbamic N- (4-Acetylamino-2-methoxy-phenyl) -2,2, 2-trifluoroacetylamide 2-Fluoro-N- [3-methoxy-4- (2, 2, 2-tri-fluorine) acetylamino) -phenyl] benzamide 2-Fluoro-N- (2-fluoro-benzoyl) -N- (4-nitro-2-trifluoromethyl-phenyl) benzamide Acid ter-butylester. { 4- [(1H-pyrazol-4-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(lH-imidazole-4-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(5-met il- [1, 2, 3] thiadiazole-4-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(5-furan- [1, 2, 3] thiadiazole-4-carbonyl) -amino] -phenyl} -carbámico 2, 2, 2-Tri. Fluoro-N- (5-nitro-pyridin-2-yl) -acetamide acid tert-butylester. { 4- [(1-methyl-1H-pyrazole-4-carbonyl) -amino] -phenyl} -carbamic 4- (2-Fluoro-benzoylamino) -2-hydroxy-benzoic acid methyl ester N- 5-chloro-2,4-dimethoxy-phenyl) -oxamic acid (4-amino-phenyl) -amide of isoxazole acid -5-carboxylic acid 2-Fluoro-N- (4-nitro-benzyl) -benzamide 4-nitro-benzylamide of furan-2-carboxylic acid N- [3-Chloro-5- (2,2,2- trifluoroacetylamino) -phenyl] -2,2,2-trifluoroacetamide N- (3-amino-5-chloro-phenyl) -2,2,2-trifluoroacetamide, tert-butylester of acid [4 - ( 2-Fluoro-benzoi lamino) -benzyl] -carbamic Ter-buti [4- (2,6-difluoro-benzoylamino) -benzyl] -carbamic acid ester 2,6-Difluoro-N- (4-nitro-benzyl) -benzamide Ter-but i Lester acid. { - [(furan-2-carbonyl) -amino] -benzyl} -carbamic N- (3-Amino-5-chloro-phenyl) -acetamide [4- (3-Chloro-benzoylamino) -phenyl] -carbamic acid tert-butylester [4- (4-chloro- benzoylamino) -phenyl] -carbamic [4 - (-Dimethylamino-benzoyl-amino) -phenyl] -carbamic acid tert-butylester (4-Benzenesulphilamino-phenyl) -carbamic acid tert-butylester [] 4- (3-tr i fluoromet-il-benzoyl-amin) -phenyl] -carbamic acid 2, 2, 2-trifluoro-N- (5-nitro-pyrimidin-2-yl) -acetamide EXAMPLE 11 (2D METHOD) 2-Chloro-N- (2-chloro-4-nitrophenyl) ace-amide A solution of 2-chloro-4-nit roanil ina (19.0 g) and chloroacetyl chloride (30 ml) in tetrahydrofuran ( 150 ml) is heated at reflux for 1 hour. The solution was cooled and concentrated under reduced pressure, giving a wet yellow solid. Ether (250 ml) was added and the yellow solid was collected. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- (4-Nitro-3-trifluoromethyl-phenyl) -acetamide Ethyl ester (2-chloro-4-nitro-phenyl) -carbamic acid 2- Acid acetylamino-5-nitro-benzoic acid (5-chloro-2-hydroxy-4-nitro-phenyl) -amide of furan-2-carboxylic acid (2-methyl-4-nitro-phenyl) -amide of furan-2- acid carboxylic (2-methoxy-4-nitro-phenyl) -amide of furan-2-carboxylic acid N- (2-Chloro-4-nitro-phenyl) -benzamide 2-methoxy-N- (4-nitro-phenyl) - acetamide N- (4-Nitro-phenyl) -acrylamide N- (4-Nitro-phenyl) -isobutyrylamide [4- (acryloylamino) -phenyl] -carbamic acid tert-butylester I butyl ester of acid (4-nitrate) ro-phenyl) -carbamone co (5-nitro-pyridin-2-yl) -amide [1,2,3] -thiad The zol-4-carboxylic acid (5-nitro-pyridin-2-yl) -furan-2-carboxylic acid amide 2-Fluoro-N- (5-nitro-pyridin-2-yl) -benzamide N- (2-C lo or 4-nitrophenyl) -2-fluoro-benzamide (2 , 5-dimethoxy-4-nitro-phenyl) -amide of furan-2-carboxylic acid N- (2-Cyano-4-nitro-phenyl) -2-fluoro-benzamide 2-Fluoro-N- (2- methoxy-4-ni t-phenyl-benzamide 2-Methyl-N- (5-nitro-pyridin-2-yl) -benzamide (2-methoxy-5-methyl-4-nitro-phenyl) -amide of acid furan-2-carboxylic 2-Fluoro-N- (2-methoxy-5-methyl-4-nitro-phenyl) -benzamide N- (2-Benzyl-4-nitrophenyl) -acetamide N- ( 2-Benzoyl-4-nitro-phenyl) -2-fluoro-benzamide (2-benzoyl-4-nitro-phenyl) -amide of furan-2-carboxylic acid N- (3-Methyl-4-nitro-phenyl) - acetamide 2-Fluoro-N- (3-methyl-4-nitro-phenyl) -benzamide (3-Met-il-4-nitro-phenyl) -amide of furan-2-carboxylic acid 2-Acetylamino-5-nitro-N phenyl-benzamide 2- [(2-Fl? orobenzoyl) amino] -5-nitro-N-phenylbenzamide (4-Nitro-2-phenylcarbamoyl-phenyl) -amide of furan-2-ca boxyl 2-Fluoro-N - (4-nitro-naphthalen-1-yl) -benzamide (4-Nitro-naphthalen-1-yl) -amide of furan-2-carboxylic acid N- (5-Clo or-2-hydroxy-4-nitro) -phenyl) -acetami N- (5-Chloro-2-hydroxy-4-nitro-phenyl) -2-fluoro-benzamide (2-chloro-4-nitro-phenyl) -amide of furan-2-carboxylic acid N- (4 - Ni tro- 2 -tri fluoromet il-phenyl) -acetamide (2-cyano-4-nitro-phenyl) -amide of furan-2-carboxylic acid 2-Fluoro-N- (4-nit ro-2-tri fluoromet il-phenyl) -benzamide (furan-2-carboxylic acid 2-fluoro-N- (2-methyl-4-nitro-phenyl) -benzamide N- (5-nitro-2-trifluoromethyl-phenyl) -amide) Chloro-2-methyl-4-nitro-phenyl) -2-f-luoro-benzamide (5-chloro-2-methyl-4-nitro-phenyl) -amide of furan-2-carboxylic acid 2- (2- fluoro-benzoylamino) -5-nitro-benzoic acid 2- [(f-2-carbonyl) -amino] -5-nitro-benzoic acid N- (3-Chloro-4-nitrophenyl) -2-fluoro- Furan-2-carboxylic acid benzamide (3-chloro-4-nitro-phenyl) -amide 2,6-Difluoro-N- (3-methyl-4-nitro-phenyl) -benzamide 2-Fluoro-N- (4 -nitro-3-tri fluoromethyl-phenyl) -benzamide (furan-2-carboxylic acid 2-chloro-N- (2-chloro-2-chloro-N- (4-nitro-3-trifluoromethyl-phenyl) -amide) ro-4-nitro-phenyl) -acetamide N- (2-Clor o-4-nitrophenyl) methansul fonamide [3-Methoxy-4- (2,2,2-trifluoro-acetylamino) -phenyl] -amide of furan-2-carboxylic acid N- (2-Chloro-4-nitro-phenyl) -2,2,2-trifluoroacetamide EXAMPLE 12 Ter-butyl ester of acid. { 4- [(4-phenyl- [1, 2, 3] thiadiazole-5-carbonyl) -amino] -phenyl} -carbamic A solution of 1- (N-tert-butoxycarbonyl) -1,4-phenylenendi amine (0.8 g) and 4-phenyl- [1,2,3] thiadiazole-5-carboxylic acid (0.7 g) in dichloromethane (10 ml) was treated with triethylamine (1.3 ml) and hexa-f luorofos, benzotriazol-1-yloxy-tris (dimethylamino) phosphonium fato (1.6 g). After stirring at room temperature, the reaction was diluted with water and extracted with dichloromethane. The organic layer was washed with hydrochloric acid 0.5 N, saturated sodium bicarbonate, and water, then dried over magnesium sulfate, and concentrated under reduced pressure to give the desired product. Using the above procedure and appropriate starting materials, the following compounds were prepared: acid Ter-butylester. { 4- [(lH-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { - [(pyrazine-2-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(5-methyl-thiophene-2-carbonyl] -amino] -phenyl} -carbamic acid tert -butylester. {4- [(l-methyl-lH-pyrrol-2-carbonyl)] -amino] -phenyl.}. -carbamic acid tert.-butyl ester {4-quinoline-8-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(benzofuran-2 -carboni 1) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(i soquinolin-1-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(quinolin-2-carbonyl) -amino] -phenyl} -carbamic Ter-butylester. { 4- [(pyridine-2-carbonyl) -amino] -phenyl} - Carbamic Ter-but i.Lés ter of acid. { 4 - [(isoquinolin-4-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4 - [([1, 2, 3] thiadiazole-4-carbonyl) -amino] -phenyl} -carbatic Ter-butiLester of acid. { 4- [(1H- [1, 2, 3] triazole-4-carbonyl) -amino] -phenyl} -carbamic acid [4- (2-Methylsufanyl-benzoylamino) -phenyl] -carbamic acid tert-butylester. { 4- [quinolin-4-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(4-methyl [1,2,3] thiadiazole-5-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(4-phenyl- [1, 2, 3] thiadiazole-5-carbonyl) -amino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [(lH-indol-2-carbonyl) -amino] -phenyl} -carbamic acid [1, 2, 3] thiadiazole-4-carboxylic acid tert-butylester 4-Nitro-benzylamide. { 4- [([1, 2, 3] thiadiazole-4-carbonyl) -amino] -benzyl} -carbamic 4- (4-tert-butoxycarboni-lamino-phenylcarbamoyl) -phenyl-estai: of acetic acid Ter-butylester of acid. { 4- [(quinolin-6-carbonyl) -amin or] -phenyl} -carbamic EXAMPLE 13 (METHOD 2F) 2- (4-T rr-butoxycarbonylamino-2,6-dichloro-phenoxy) -acetic acid ethyl ester A solution of tert-butylester of [3, 5-dichloro-4- (2- hydroxy-ethoxy) -phenyl] -carbamic acid (0.85 g) in pyridine (14 ml) with acetic anhydride (1.24 ml) and the mixture was stirred at room temperature for 15 hours.The solvent was removed under reduced pressure and the residue was dissolved This solution was then washed twice with 5% aqueous hydrochloric acid, once with saturated aqueous sodium bicarbonate, and then with saturated aqueous sodium chloride.The solution was dried over anhydrous magnesium sulfate. and the solvent was removed under reduced pressure to provide the desired product as a colorless oil.Using the above procedure and appropriate starting materials, the following compounds were prepared: Phenylsulfanyl-acetonitrile 2- (4-tert-butoxycarbonylamino-2-6- dichloro-phenoxy) - ethyl ester of ac acid tico EXAMPLE 14 (METHOD 2G) (3,5-Dichloro-4-hydroxy-phenyl) -carbamic acid tert-butylester It was added to a solution of 2,6-dichloro-4-aminophen (9.5 g) in tetrahydrofuran (130 ml. di-tert-butyl-dicarbonate (11.7 g) and the mixture was heated to reflux for about 15 hours. The solution was then cooled, concentrated under reduced pressure, diluted with ethyl acetate, and washed successively three times with 5% aqueous hydrochloric acid, then once with saturated aqueous sodium chloride. The solution was dried to provide the desired crude product. This material was then triturated with cold dichloromethane to provide the product as a white solid.

Using the above procedure and appropriate starting materials, the following compounds were prepared: (3-amino-5-chloro-phenyl) -carbamic acid tert-butylester EXAMPLE 15 (METHOD 3a 3, 5-Dichloro-4-ethoxy-phenylamine Trifluoroacetic acid (5 ml) was added to (3,5-dichloro-4-ethoxy-phenyl) -carbamic acid tert-butylester (0.97 g) and the mixture was stirred for about 45 minutes at room temperature, then water was added, and the mixture was cooled in an ice bath and basified with solid potassium carbonate.The solution was extracted three times with ethyl acetate and the organic phases The combined extracts were washed with saturated aqueous sodium chloride, then dried over anhydrous sodium sulfate, concentration under reduced pressure and recrystallization from hexanes afforded the desired product as a pale yellow crystalline solid. Starting with the appropriate starting materials, the following compounds were prepared: 5-Bromo-pyridine-3-ylamine 3-Chloro-4-methanesulfonyl-phenyl-amine N- (4-amino-phenyl) -2-methyl-benzamide 2- (4- Amino-phenylcarbamoyl) -phenyl acid acyl ester ico N- (4-amino-phenyl-4-fluoro-benzamide N- (4-amir.o-phenyl-3-fluoro-benzamide N- (4-amyr or phenyl-2-fluoro-benzamide N- (4 -Amir.o-phenyl-2-methoxy-benzamide N- (4-Amir.o-phenyl-3-methoxy-benzamide N- (4-Amir.o-phenyl-4-methoxy-benzamide N- (4-Amino -phenyl -2-phenyl-acetamide N- (4-Amir.o-phenyl) -2, 2-dimethyl-propionamide N- (4-Amir.o-phenyl-2,2,2,2-trifluoroacetamide (4-Amino -phenyl) -thiophene-2-carboxylic acid (4-amino-phenyl) -amide of lH-pyrrole-2-carboxylic acid N- (4-Amino-phenyl) -3-nitro-benzamide 3-Acetyl mino-N- (4-amino-phenyl) -benzamide N- (4-Amyr? o-phenyl) -3-dimethylamino-benzamide N- (4-Amyr? o-phenyl) -3-methanesulfonylamino-benzamide N- (4-Amino-phenyl) -2- tri fluoromethyl-benzamide N- (4-Amino-phenyl) -2,6-difluoro-benzamide N- (4-amino-phenyl) -2-chloro-benza-ida N- ( 4-Amyr? O-phenyl) -2-bromo-benzamide N- (4-amino-phenyl) -2-nitro-benzamide (4-amino-phenyl) -amide of pyrazine-2-carboxylic acid (4- Amino-phenyl) -am of 5-methylo-thiophen-2-carboxylic acid (4-Amino-phenyl) -amide of quinoline-8-carboxylic acid (4-Amino-phenyl) -amide of l-methyl-lH-pyrrol- 2- benzo [b] thiophene-2-carboxylic acid (4-amino-phenyl) -amide of benzofuran-2-carboxylic acid N- (4-Amyr. phenyl) -isonicot-naphthalene-2-carboxylic acid (4-Amino-phenyl) -amide (4-Amino-phenyl) -amide of naphthalene-1-carboxylic acid (4-Amino-phenyl) -amide 1-acetonin-1-carboxylic acid (4-amino-phenyl) -amide of quinoline-2-carboxylic acid li 3, 5-Dicyl ro-4-ethoxy-phenyl lamin 4 -Butoxy-3, 5-dichloro-phenyl (4-Amino-phenyl) -amide of sochiolin-4-carboxylic acid (4-Amino-phenyl) [1, 2, 3] thiadiazole-4-carboxylic acid (4-amino-phenyl) -amide of 1H- [1,2,3] triazole-4-carboxylic acid (4-Amino-phenyl) ) 3-bromo-t-iofen-2-carboxylic acid amide 4-Benzyloxy-3,5-dichloro-phenylamine 2- (4-amino-2,6-dichloro-phenoxy) -acetamide (4-amino) acid methyl ester -2,6-dichloro-phenoxy) -acetic acid [3- (4-Amino-phenylcarbamoyl) -phenyl] -carbamic acid ester] 2-Amino-N- (-amino-phenyl) -benzamide (4-Amino-phenyl) -Biphenyl-2-carboxylic acid amide N- (4-Amino-phenyl) -2, 3-di-fluoro-benzamide N- (4-Amino-phenyl) -2,5-difluoro-benzamide N- (4 - Amino-phenyl) -2,4-di-fluoro-benzamide 2-Acetylamino-N- (4-amino-phenyl) -benzamide N- (-Amino-phenyl) -2-methansul-fonyl-amino-benzamide N- (4-Amino - phenyl) -2, 3, 4- trifluoro-benzamide N- (4-Amine non-phenyl ) -2, 3, 4, 5, 6-pentafluoro-benzamide N- (4-Ami-phenyl) -2-methyl-sulfanyl-benzamide (4-Amino-2,6-dichloro-phenoxy) -acetic acid ethyl ester Methyl ester of N- (4-amino-phenyl) -isophthalamic acid N- (4-Ami o-phenyl) -3-benzyloxy-benzamide N- (4-amino-phenyl) -3-butoxy-benzamide acid ethyl ester [3 - (4-amino-phenylacarbamoyl) -phenoxy] -acetic (4-amino-phenyl) -amino of pyridin-2-carboxylic acid (amino-phenyl) -amide of quinoline-4-carboxylic acid (4-Amino) 5-Methyl-furan-2-carboxylic acid (4-amino-phenyl) -amide of 5-dichloromethyl-furan-2-carboxylic acid (4-amino-phenyl) -amide of lH-indole -2-carboxylic acid (4-amino-phenyl) -amide 4-methyl- [1, 2, 3] • thiadiazole-5-carboxylic acid (4-amino-phenyl) -amide of thiophene-3-carboxylic acid (5-chloro-furan-2-carboxylic acid (4-amino-phenyl) -amide of 5-nitro-furan-2-carboxylic acid N- (4-Amyr) .o-feni 1) -2 5-bromo-furan-2-carboxylic acid (3-methyl-2-furan-2-carboxylic acid (4-amino-phenyl) -amide) -thiophen-2-yl-acetamide (4-amino-phenyl) -amide ( 4-Amino-phenyl) -amide of 4-bromo-furan-2-carboxylic acid N- (4-Amino-phenyl) -nicotinamide N- (4-Aminophenyl) -3-furancarboxamide (4-Amino-phenyl) -amide of 4-phenyl- [1, 2, 3] -thiadiazole-5-carboxylic acid 3- (4-Amino-phenylcarbamoyl) -phenylester of acetic acid (4-amino-phenyl) -amide of benzoic acid [1, 3] dioxol-4'-carboxylic acid N- (4-amino-phenyl) -3- (2-dimethyl-lamino-ethoxy) -benzamide N- (4-amino-phenyl) -3-tri fluoromethoxy-benzamide N- (4-Amyr) o-phenyl) -3- (2-mor-folin-4-yl-ethoxy) -benzamide Hexyl ester of (4-amino-phenyl) -carbamic acid (4-amino-phenyl) -amide of furan-2-carboxylic acid (4-Amino-phenyl) -carbamic acid (4-Amino-phenyl) -amide of hexanoic acid N- (4-Amir.o-phenyl) -acrylamide N- (4-Amir or -phenyl) -2- methoxy acetamide (4-Aminoph enyl) -amide of 4-furan-3-yl- [1, 2, 3] -thiazol-5-carboxylic acid (4-amino-phenyl) -amide of 5-tert-butyl-furan-2-carboxylic acid 3-Chloro-methansulfinyl-phenylamine (4-Amino-phenyl) -amide of 5-methyl- [1, 2, 3] -thiadiazole-4-carboxylic acid 2- (-Amino-2-chlorophenyl) -ethanol 2-Piperidin-l-yl-ethyl ester of (4-amino-2-chlorophenyl) -carbamic acid 5-Chloro-II, N-dimethyl-benzene-1,3-diamine 3- (2-Met: .1 -butyl) -5- trifluoromet il-phenylamine 3- (Isobu il-5-trifluoromethyl-phenylamine (4-Aminomethyl-phenyl) -amide of furan-2-carboxylic acid N- (4-Aminomethyl-phenyl) -2- Fluoro-benzamide (4-Aminomethyl-phenyl) -amide of [1,2,3] thiadiazole-4-carboxylic acid N- (4-Aminomethyl-phenyl) -2,6-difluoro-benzamide (4-Amino- -phenyl) -oxazole-4-carboxylic acid amide N- (-Amino-phenyl) -3-chloro-benzamide N- (4-amino-phenyl) -4-chloro-benzamide 4- (4-amino-phenylcarbamoyl) ) - acetic acid phenylester N- (4-Amino-phenyl) -4 -dimet Ilamide-benzamide 1- (4-Amino-phenyl) -3- (3,5-bis-tri-fluoromet-il-phenyl) -thiourea N- (4-Amino-phenyl) -2-iodo-benzamide N- (4 - Amino-phenyl) -3-trifluororneti-1-benzamide EXAMPLE 16 (METHOD 3B) 1- (4-Amino-2-chloro-phenyl) -ethanol A solution of 1M tetrabutylammonium fluoride in tetrahydrofuran (5.7 ml) was added to 2-trimethylsilane-ethyl ester of [3-chloro-4] - (1-hydroxy-ethyl) -phenyl] -carbamic acid (0.5 g) and the mixture was stirred at room temperature for about 3.5 hours. The solution was then concentrated under reduced pressure, dissolved in a mixture of ethyl acetate and hexanes 1: 1, washed successively with water, then saturated aqueous sodium chloride, and dried on anhydrous magnesium sulfate. Removal of the solvent under reduced pressure followed by chromatography on silica gel (40% ethyl acetate in hexanes was used as the eluent) provided the product as an amber oil.

EXAMPLE 17 (METHOD 3C) N-. { 4-Amino-3-cyanophenyl) -2-fluoro-benzamide Potassium carbonate (5.0 g) was added to a solution of N- [3-cyano-4- (2, 2, 2-1 rifluoroaceti 1-amino) - phenyl] -2-fluoro-benzamide (2.5 g) in methanol (270 ml) and water (16 ml) and the mixture was refluxed overnight. After removal of the solvent under reduced pressure, the residue was suspended in water and extracted with dichloromethane. The organic extracts were poured, washed with water and then saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure to provide the desired compound as a white solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- (4-amino-phenyl) -2-methanesulfinyl-benzamide N- (4-amino-3-cyano-phenyl) -2-fluoro-benzamide (4-amino-3-cyano-phenyl) -amide of furan -2- carboxylic N- (4-amino-3-cyano-phenyl) -acetamide (4-amino-3-trifluoromethyl-phenyl) -amide of furan-2-carboxylic acid N- (4-amino-3-) methoxy-phenyl) -acetamide N- (4-amino-3-methoxy-phenyl) -2-fluoro-benzamide (4-amino-3-methoxy-phenyl) -amide of furan-2-carboxylic acid EXAMPLE 17 (METHOD 4A) 2-Chloro-1-cyclohexyloxy-nitro-benzene Cyclohexanol (2.9 g) in dimethyl sulfoxide (20 ml) was slowly added to a flask containing potassium hydride (0.90 g, pre-wash three times with hexanes) under an argon atmosphere and the solution was stirred for about 1 hour at room temperature. A solution of 3-chloro-4-fluoro-nitrobenzene (1 g) in dimethyl sulfoxide (10 ml) was added and the resulting dark red solution was then heated for three hours to about 100 degrees. The reaction mixture was then cooled, diluted with diethyl ether (300 ml), and washed successively with saturated aqueous ammonium chloride, three times with water, then with saturated aqueous sodium chloride. The organic layer was then dried over anhydrous magnesium sulfate, the solvent was removed under reduced pressure, and the resulting oil was chromatographed on silica gel (5% ethyl acetate in hexanes was used as the eluent) to provide the desired product as an orange solid.

EXAMPLE 18 (4C METHOD) 2-Chloro-4-nitro-phenyl) -methyl- (1-methyl-pyrrolidin-3-yl) -amine 3-Chloro-4-fluoronitrobenzene (1.0 g) was combined and stirred for approximately 24 hours. ) and N, N'-dimethyl-3-aminopyrrolidine (1.72 g). The mixture was then diluted with ethyl acetate, washed twice with water and once with saturated sodium chloride, and dried over anhydrous sodium sulfate. After removal of the solvent under reduced pressure, the residue was subjected to chromatography on silica gel (pure ethyl acetate was used followed by pure methanol as the eluents) to provide the desired product as a yellow oil.

Using the above procedure and appropriate starting materials, the following compounds were prepared: (2-Chloro-4-nitro-phenyl) -dipropyl-amine 1- (2-Cloi "? - 4-nitro-phenyl) -piperidine 1- (2-Chloro-4-nitro-phenyl) -pyrrolidine (2-Chloro-4-nitro-phenyl) -cyclohexy-1-meth i1-amine Benzyl- (-chloro-4-nitro-phenyl) -amine (2-Chloro-4-nitro-phenyl) -methyl- (1-methyl-piperidin-4-yl) -amine (2-Chloro-4-nitro) phenyl) -cyclohexyl-ethyl-amine (2-chloro-4-nitro-phenyl) -cyclohexyl-amine (2-chloro-4-nitro-phenyl) -methyl- (1-methyl-1-pyrrole idin-3-yl) -amine (l-Benzyl-pyrrolidin-3-yl) - (2-chloro-4-nitro-phenyl) -methyl-amine (2-chloro-4-nitro-phenyl) -cyclopent-1-methylamine 1- (2-Clo or-4-nitro-phenyl) -decahydro-quinoline Allyl- (2-chloro-4-nitro-phenyl) -cyclohexyl-amine 2- [(2-Chloro-4-nitro-phenyl) - (2-hydroxy-ethyl) -amino] -ethanol (2-Chloro-4-nitro-phenyl) -isobutyl-methyl-amine (2-Chloro-4-nitro-phenyl) -hexyl-methyl-amine 2- [ (2-Chloro-4-nitro-phenyl) -met-il-amino] -ethanol N- (2-Chloro-4-nitro-phenyl) -N, N ', N' -trimet i1-ethan-l, 2- diam Lna N- (2-Clo-o-4-nitrophenyl) -N, N ', N' -trimeti 1 -propan- 1, 3- diam Lna (l-Benzyl-piperidin-4-yl) - (2-chloro-4-nitro-phenyl) -amine N- (2-Chloro-4-nitrophenyl) -N ', N' -dimethyl -etan-1, 2- diamine N- (2-Chloro-4-nitro-phenyl) -N ', N' -dimethyl-propan-1, 3-diamine (2-Chloro-4-nitro-phenyl) - ( 2-methoxy-eti 1) -methyl-amine (l-Benzyl-pyrrolidin-3-yl) - (2-chloro-4-nitro-phenyl) -amine 4-Pipe-idin-1-yl-3-trifluoromethyl-benz onit rilo 4-Dimetylamino-3-tri fluorometyl-benzonitrile 4- (4-Methyl-piperazin-1-yl) -3- 1 rifluoromethyl-benzonitrile EXAMPLE 19 (METHOD 4E) Butyl- (2-chloro-4-nitro-phenyl) ioether A solution of 3-chloro-4-fluoro-nitrobenzene (5.0 g) and sodium sulfide (2.5 g) was stirred in N, N-dimethylformamide (30 ml) at room temperature for 1 hour and then treated with 1-iodobutane (12.6 g). The solvent was then removed under reduced pressure and the resulting residue was treated with ethyl acetate and hexanes to precipitate the inorganic salts. The solids were removed by filtration and the filtrate was reduced under reduced pressure. The resulting residue was then passed through anhydrous magnesium silicate using dichloromethane as the eluent to give the desired compound as a yellow solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: 1 -But i 1 sul fanyl-2-chloro-4-nitro-benzene 2-chloro-1-cyclohexyl sulphonyl-4-nitro-benzene 2 -Chloro- 1-ethylsulfani 1-4 -nitro-benzene EXAMPLE 20 (4F METHOD) (4-Chloro-5-netoxy-2-nitro-phenyl) -dimethyl-amine It was added to a solution of trifluoro-methanesulfuryl 4-chloro-5-methoxy-2-nitro-f-enyl ester Phonic (1.0 g) in tetrahydrofuran (2.0 ml) dimethylamine (4.0 ml of a 40% aqueous solution) and the mixture was stirred at room temperature for about 15 hours. The solution was then concentrated under reduced pressure and the residue was dissolved in ethyl acetate and then washed with water. The aqueous layer was extracted once with ethyl acetate and the combined organic layers were washed with saturated aqueous sodium chloride and dried over anhydrous sodium sulfate. The solvent was removed by evaporation under reduced pressure and the residue was triturated with hexanes to provide the desired product as a colorless solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: (4-Chloro-2-nitro-phenyl) -dimethyl-amine 4 - (4-chloro-5-methoxy-2-nitrophenyl) -morpholine (4-Chloro-5-methoxy-2-nitro-phenyl) -dimethyl-amine 1- (4-Chloro-5-methoxy-2-nitro-phenyl) -piperidine 1- (4-Clo): o- 5-met oxy-2-nit ro-phenyl) -pyrrolidine Benzyl- (-chloro-5-methoxy-2-nitrophenyl) -amine (2-chloro-6-nitro-phenyl) -dimethyl-amine EXAMPLE 21 (4G METHOD) (Chloro-4-nitro-enyl) -methyl enyl-amine n-Butyl-lithium (12.3 ml of a 2.5 M solution in hexanes) was added dropwise to a solution of N-methylane. .Line (3.0 g) in tetrahydrofuran (75 ml) a 0 ° C. The mixture was allowed to slowly warm to room temperature and then cooled again to 0 ° C and cannula was added to a solution of 3-chloro-4-fluoro-nitrobenzene (4.9 g) in tetrahydrofuran (35 ml) which was maintained at room temperature. -78 ° C. Following the addition, the reaction mixture was allowed to warm to room temperature over the course of 1 hour, and then concentrated under reduced pressure, quenched by the addition of saturated, aqueous ammonium chloride, and extracted three times with ethyl acetate. The collected organic layers were washed three times with 5% aqueous hydrochloric acid, once with water, once with saturated aqueous sodium bicarbonate, once with saturated aqueous sodium chloride, and then dried over anhydrous magnesium sulfate. Following removal of the solvent under reduced pressure the residue was subjected to chromatography on silica gel (5% diethyl ether in hexanes was used) to provide the desired product as a clear, colorless oil.

EXAMPLE 22 (4H METHOD) 2,6-Dichloro-4-nitrophenol 5e added 3,4,5-trichloronitrobenzene (14.86 g) to a solution of potassium phenoxide (8.66 g) in diethylene glycol (66 ml) and the mixture heated to 160 ° C for approximately 15 hours. The resulting dark brown solution was cooled to room temperature, poured into 100 ml of cold water, and extracted twice with diethyl ether. The collected organic extracts were washed with water, 10% aqueous sodium hydroxide, and then dried over anhydrous magnesium sulfate. Following removal of the solvent under reduced pressure, the resulting oil was distilled in a Kugeirohr apparatus to provide a yellow oil that solidified in stagnant. Recrystallization from ethanol-water produces the desired product as a pale yellow solid.

EXAMPLE 23 (METHOD 5A) Ter-but: 3,5-dichloro-4-ethoxy-phenyl-carbamic acid ester Ethyl iodide (0.36 ml) was added to a solution of tert-butylester of acid (3, 5-dichloro-4-hydroxy-phenyl) -carbamic 81.0 g) and potassium carbonate (1.0 g) and the mixture was stirred for approximately 15 hours at room temperature. The solution was then filtered, concentrated under reduced pressure, and partitioned between ethyl acetate and water. The separated aqueous layer was further extracted twice with ethyl acetate, and the collected organic extracts were washed successively with 10% aqueous sodium hydroxide, with water, and then dried over anhydrous sodium sulfate. Evaporation of the solvent under reduced pressure gave the desired product as a brown colored solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: Ter-butylester (3,5-dichloro-4-ethoxy-phenyl) -carbamic acid tert-butylester (4-butoxy-3, 5-) dichloro-phenyl) -carbamic (4-benzyloxy-3, 5-dichloro-phenyl) -carbamic acid tert-butylester (4-carbamoylmethoxy-3, 5-phenyl) -carbamic acid ter-butylester [3, 5-dicl oro-4 - (2-nitrile-ethoxy) -phenyl] -carbamic acid butylester (4-tert-butoxycarbonylamino-2, 6-dicl-phenoxy) -acetic acid methyl ester Acid methyl ester -butoxy-benzoic acid 3-tert-butoxycarbonylmethoxy-benzoic acid methyl ester 3-carbamoylmethoxy-benzoic acid methyl ester [4- (3-carbamoylmethoxy-benzoylamino) -phenyl] -carbamic acid tert-butylester Tert-butylester of acid. { 4- [3- (2-chloro-ethoxy) -benzoylamino] -phenyl} -carbamic EXAMPLE 24 (METHOD 5C) (2, 6-Dichloro-4-nitro-enoxy) -acetic acid tert-butylester Tert-butyl-bromoacetate (10 ml) was added to a solution of 2,6-dichloro-4 -nitrophenol (2.5 g) and potassium carbonate (3.3 g) in dimethylformamide (50 ml) and the mixture was stirred at room temperature for two cycles. The solution was then poured into 500 ml of water, extracted three times with hexanes, and the collected organic extracts were washed with saturated aqueous ammonium chloride and then dried over anhydrous magnesium sulfate. Evaporation of the solvent under reduced pressure followed by trituration of the resulting oil with hexanes afforded the desired product as a white solid. Using the above procedure and starting materials, the following compounds were prepared: 3-Dimeti-1-amino-1- (4-nitro-phenyl) -propenyone 2-Chloro-1-isopropoxy-4-nitro-benzene 1,3-Dichloro- 2-methoxy-4-methyl-5-nitro-benzene l-Chloro-4-ethoxy-2-methoxy-5-nitro-benzene-l-Butoxy-4-chloro-5-methoxy-2-nitro-benzene Chloro-2-methoxy-5-nitro-4- (phenylmethoxy) benzene (CA name) l-Chloro-4-methoxy-5-nitro-2- (phenylmethoxy) benzene (CA name) Ter-butyl ester of acid (2, 6-dichloro-4-nitro-phenoxy) - acetic acid (2,6-dichloro-4-nitro-phenoxy) -acetonitrile l-Chloro-4-methoxy-2-methyl-5-nitro-benzene 2- (4-chloro -5-methoxy-2-nitro-phenoxy) -acetamide 2- (2-Chloro-5-methoxy-4-nitro-phenoxy) -acetamide (4-chloro-5-methoxy-2-nitro-phenoxy) -acetonitrile ( 2-Chloro-5-methoxy-4-nitro-phenoxy) -acetonitrile 4- (2-Chloro-5-methoxy-4-nitro-phenoxy) -butyronitrile 2- (4-chloro-5-methoxy-2-nitro- phenoxy) -ethanol 2- (2-Chloro-5-methoxy-4-nitro-phenoxy) -ethanol Ter-bu-acid ester (2-chloro-5-me toxi-4-ni tr o-phenoxy) -acetic acid (2-chloro-5-methoxy-4-nit-phenoxy) -acetic acid methyl ester (4-chloro-5-methoxy-2-nitro-phenoxy) -acetic acid methyl ester. co-Butyl ester of (4-chloro-5-methoxy-2-nit-phenoxy) -acetic acid (2-chloro-4-nitro-phenoxy) -acetonitrile l-Butoxy-2-chloro-4-nitro- benzene 2-Chloro-4-nitro-l- (2, 2, 2-trifluoro-ethoxy) -benzene 2-chloro-4-nitro-1-propoxy-benzene 2-chloro-l-ethoxy-4-nitro Benzene 1,3-Diiodo-2,4-dimethoxy-5-nitrobenzene 1,3-Dibro-2,4-dimethoxy-5-nitro-benzene 3-chloro-2,4-dimethoxy-nitrobenzene EXAMPLE 25 (METHOD 5E) [3,5-Dichloro-4- (2-hydroxy-ethoxy) -phenyl] -carbamic acid tert-butylester Ethylene carbonate (1.6 g) was added to a solution of tert-butylester of acid (3, 5-dichloro-4-hydroxy-phenyl) -carbamic acid (1.0 g) and potassium carbonate [0.55 g) in toluene (20 ml) and the mixture was refluxed for 3 hours. To the cooled reaction mixture was added 2.5 M aqueous sodium hydroxide (50 ml), and the separated organic layer was then washed successively with water, then saturated aqueous sodium chloride, and then dried over anhydrous sodium sulfate. The solvent was then removed by evaporation under reduced pressure and the resulting residue was subjected to chromatography on silica gel (30% ethyl acetate in hexanes was used as the eluent) to provide the desired product as a white foam.

EXAMPLE 26 (METHOD 6) 3- (2-Chloro-4-nitro-phenoxy) -1-methyl-pyrrolidine To a solution of 2-chloro-4-nitrophenol (2.0 g) in tetrahydrofuran (60 ml) was added l- methyl-3-pyrrolidinol (2.3 g), triphenylphosphine (6.0 g), and ethylazodicarboxylate (3.6 ml) and the mixture was stirred at room temperature under an argon atmosphere for 1.5 hours. The solution was then concentrated under reduced pressure, diluted with ethyl acetate, washed successively with 10% aqueous sodium hydroxide, water, saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate. The solvent was removed by evaporation under reduced pressure and the residue was chromatographed on silica gel (ethyl acetate, then 10% methanol in dichloromethane as the eluent). The fractions of the harvested product were then recrystallized from hexanes to produce the desired product as a yellow solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: 4- (2-Chloro-4-nitro-phenoxy) -1-meth i 1 -piperidine 3- (2-Chloro-4-nitro-phenoxy) -1-met il-pyrrolidine [2- (2-Clcro-4-nitro-phenoxy) -ethyl] -dimethyl-amine [3- (2-Clcro-4-nitro-phenoxy) -propyl] -dimethyl-amine EXAMPLE 27 (METHOD 7?) 2-Chloro-3-me oxy-6-n-ro-phenol and 2,4-dichloro-3-methoxy-6-nitro-phenol was added to a flask containing 3-methoxy-6- nitro-phenol (0.5 g) aqueous sodium hypochloride (5.25% aqueous solution, 21 ml) and the mixture was stirred at room temperature for approximately 24 hours. The mixture was then cooled in an ice bath, acidified by the addition of concentrated hydrochloric acid, then extracted twice with ethyl acetate. These organic extracts were dried over anhydrous magnesium sulfate, the solvent was removed by evaporation under reduced pressure, and the residue was subjected to chromatography on silica gel (15% acetone in hexanes was used as the eluent) to provide both the products mono- as dichlorinated as yellow solids. Using the above procedure and appropriate starting materials, the following compounds were prepared: 3-Chloro-2-hydroxy-4-methoxy-nitrobenzene 3,5-Dicyl-2-hydroxy-4-methoxy-nitrobenzene EXAMPLE 28 (METHOD 7B 2, 4-Dichloro-3-methyl-6-nitro-phenol Aqueous sodium hypochlorite (5.25% aqueous solution, 230 ml) was added to a solution of 3-methyl-4-nitrophenol (5.0 g) in water (150 ml) and the mixture was stirred at room temperature for approximately 15 hours. Additional aqueous sodium hypochlorite (5.25% aqueous solution, 230 ml) was added and the mixture allowed to stir at room temperature for 2.5 days. The mixture was then cooled in an ice bath, acidified by the addition of concentrated hydrochloric acid, then extracted twice with ethyl acetate. These organic extracts were dried over anhydrous magnesium sulfate, the solvent was removed by evaporation under reduced pressure, and the residue was chromatographed on silica gel (ethyl acetate was used as the eluent) to provide the desired product as a solid. yellow. An analytically pure sample was obtained by a simple recrystallization of chloroform.

EXAMPLE 29 (METHOD 7C) l-Bromo-2,4-dimethoxy-5-nitro-benzene To a solution of 2,4-dimethoxy-nitrobenzene (0.50 g) in chloroform (3 ml) was added dropwise a solution of bromine (0.23 g) in chloroform (1 ml) and the mixture was allowed to stir at room temperature for about 15 hours. Additional bromine (0.15 g) in chloroform (1 ml) was added and the reaction was stirred for an additional 4 hours. The mixture was then poured into 5% aqueous sodium bisulfite and then extracted with chloroform. The collected organic extracts were then washed successively with 5% aqueous sodium bisulfite, then saturated sodium chloride, and then dried over anhydrous sodium sulfate. Removal of the solvent under reduced pressure and recrystallization of the residue from toluene produced the desired product as a yellow solid.

EXAMPLE 30 (METHOD 7D) 2, 4-Dibromo-3-methoxy-6-nitro-phenol To a solution of 5-methoxy-2-nitrophenol (0.25 g) and silver tri-fluoroacetate (0.49 g) in acid Glacial acetic acid (3 ml) was added dropwise a solution of bromine (1.42 g) in glacial acetic acid (3 ml) and the mixture was stirred at room temperature for approximately 24 hours. The solution was then partitioned between ethyl acetate and water, and the organic layer was washed successively three times with 5% aqueous sodium bisulfite, three times with saturated aqueous sodium bicarbonate, and once with saturated aqueous sodium chloride. The organic layer was then dried over anhydrous magnesium sulfate and the solvent was removed under reduced pressure. The residue was chromatographed on silica gel (20% ethyl acetate in hexanes was used as the eluent) then recrystallized from chloroform to provide the desired dibromo product as an orange solid.

EXAMPLE 31 (METHOD 7E) l-Iodo-2,4-dimethoxy-5-nitro-benzene To a solution of 2,4-dimethoxy-nor trobenzene (1.0 g) in glacial acetic acid (30 ml). Benzyltrimeti dichloroiodate was added. lamonium (1.90 g) and anhydrous zinc chloride (1.0 g) and the mixture was stirred at room temperature under an argon atmosphere. Additional benzyltimethylammonium dichloroiodate (0.4 g) was added after 5 hours and again after 24 hours. Additional zinc chloride (0.5 g) and glacial acetic acid (15 ml) were added after 24 hours). The mixture was allowed to stir at room temperature for 3 days and then filtered, diluted with 5% aqueous sodium bisulfite, and extracted three times with ethyl acetate. These collected organic extracts were washed successively with 5% aqueous sodium bisulfite, saturated aqueous sodium chloride, then dried over anhydrous magnesium sulfate. After removal of the solvent under reduced pressure, the residue was triturated with hexanes to provide the desired product as a pale yellow solid.

EXAMPLE 32 (METHOD 7F) 2, 4-Diiodo-3-methoxy-6-nitro-phenol To a solution of 5-methoxy-2-nitrophenol (0.25 g) in dichloromethane (15 ml) and methanol (6 ml). ml) was added d.L-chloroiodate of benzyltrimethammonium (1.08 g) and sodium bicarbonate (0.85 g) and the mixture was allowed to stir at room temperature for 24 hours. The solution was then filtered, the filtrate was concentrated under reduced pressure, the residue was dissolved in ethyl acetate and then washed successively with 5% aqueous sodium bicarbonate, 5% sodium bisulfite, and saturated aqueous sodium chloride. . After drying over anhydrous magnesium sulfate, the solvent was removed by evaporation under reduced pressure and the residue was recrystallized from toluene to give the desired product as yellow needles.

EXAMPLE 33 (METHOD 76) l-Fluoro-2,4-dimethoxy-5-nitro-benzene To a solution of 2,4-dimethoxy-nitrobenzene (1.0 g) in tetrachloroethane (10 ml) was added triflate of 3,5-dichloro-1-fluoro-pyrimidinium (85%, 5.07 g) and the mixture was heated at 120 ° C for 5 hours. Additional 3, 5-dichloro-1-fluoro-pyrimine triflate was added (85%, 0.25 g) and the heating was continued for 1 hour. The solution was then cooled to room temperature and passed over a column of silica gel (hexanes were used followed by 30% ethyl acetate in hexanes as the eluent). The fractions containing the product were combined, evaporated under reduced pressure, and the residue was crystallized from hexanes to provide the desired product as a brown solid.

EXAMPLE 34 (METHOD 8) 3-Chloro-4-trifluoromethyl-nitrobenzene A solution of 3-chloro-4-iodo-nitrobenzene (2.26 g), trimethyl-1 (trifluoromethyl) silane (5.68 g), copper iodide was heated. (I) (2.28 g), and potassium fluoride? 0.56 g) in N, N-dimethylformamide (8 ml) in a sealed tube at 80 ° C for 40 hours. The solution was then cooled, diluted with diethyl ether, filtered through diatomaceous earth, and the filtrate was washed successively with water, saturated aqueous sodium chloride, and then dried over anhydrous sodium sulfate. The solvent was removed under reduced pressure and the residue was chromatographed on silica gel (1% diethyl ether in hexanes followed by 10% ethyl acetate in hexanes as the eluent) to provide the desired product as an oil. colorless.

EXAMPLE 35 (METHOD 9) (3-Chloro-4-methanesulfinylphenyl) -carbamic acid tert-butylester To a solution of (3-chloro-4-thiomethyl-phenyl) -carbamic acid tert-butylester (0.89 g) in dichloromethane (15 ml) at 0 ° C was added a solution of dimethyld :. oxirane (-0.11 M in acetone, 34 ml) and the mixture was stirred at 0 ° C for 1 hour. The solvent was removed under reduced pressure and the residue was dissolved in dichloromethane, washed with saturated aqueous sodium chloride, and then dried over anhydrous magnesium sulfate. Removal of the solvent under reduced pressure gave the desired product as an orange foam.

EXAMPLE 36 (METHOD 9B) [4- (2-Methylsulfinyl-benzoylamino) -phenyl] -carbamic acid tert-butylester To a solution of 2-methylsulfanyl-N- [4- (2, 2, 2-trifluoroacetylamino) phenyl] -benzamide (234 mg) was added a saturated solution of sodium periodate (5 ml) and the mixture was stirred for 12 hours. The purple mixture was poured into water, extracted with ethyl acetate, dried over anhydrous potassium carbonate and evaporated to yield a red solid, 101 mg. Using the above procedure and appropriate starting materials, the following compounds were prepared: [4- (2-methanesulfonyl-benzoylamino or) -phenyl] -carbamic acid tert-butyl ester-2-methansulfinyl-N- [4 - (2, 2, 2-trifluoro-acetylamino) -phenyl] -benzamide EXAMPLE 37 (METHOD 10) (3-Chloro-4-methanesulfonyl-phenyl) -carbamic acid tert-butylester To a solution of (3-chloro-4-thiomethyl-phenyl) -carbamic acid tert-butylester (0.90 g) dichloromethane (30 ml) at 0 ° C was added a solution of dimethyldioxirane (-0.11 M in acetone, 80 ml) and the mixture was stirred at 0 ° C for 1 hour. The solvent was removed under reduced pressure and the residue was dissolved in dichloromethane, washed with saturated aqueous sodium chloride, and then dried over anhydrous magnesium sulfate. Removal of the solvent under reduced pressure gave the desired product as an orange foam.

EXAMPLE 38 (METHOD 11) 3-Chloro-4-vinyl-phenylamine To a deoxygenated solution of 3-chloro-4-iodo-aniline (6.95 g), triphenylarsine (0.67 g), and tris- (dibenzylideneacetone) palladium (0) (0.50 g) in tetrahydrofuran (120 ml) at 50 ° C was added ilvinyl tin (10 g) and the mixture was stirred for about 15 hours at 50 ° C under an argon atmosphere. The reaction was then cooled, filtered through diatomaceous earth, and the filtrate was evaporated to dryness under reduced pressure. The residue was dissolved in hexanes and then extracted three times with 5% aqueous hydrochloric acid. These aqueous acidic extracts were then basified with solid potassium carbonate and extracted three times with ethyl acetate. These collected organic extracts were then washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, and the solvent was removed under reduced pressure. The resulting residue was chromatographed on silica gel (hexanes and then 10% ethyl acetate in hexanes were used as the eluent) to provide the desired product as an amber oil.

EXAMPLE 39 (METHOD 12) 2-Trimethylsilanyl-ethyl ester of [3-chloro-4- (1-hydroxy-ethyl) -phenyl] -carbamic acid 2-trimethylsilanyl-t-t heses acid was added (3-chloro-4-vinyl-phenyl) -carbamic acid (2.6 g) to a solution of mercury acetate (3.48 g) in water (7 ml) and tetrahydrofuran (5.25 ml) and the mixture was stirred for approximately 15 hours. 3N aqueous sodium hydroxide (8.7 ml) and a solution of 0.5 M sodium borohydride in aqueous sodium hydroxide 3 (8.7 ml) were then added and stirring was continued for 6 hours. The solution was then saturated with sodium chloride and extracted with ethyl acetate. These organic extracts were then washed with saturated aqueous sodium chloride and dried over anhydrous sodium sulfate. Following removal of the solvent under reduced pressure, the residue was chromatographed on silica gel (20% ethyl acetate in hexanes was used as the eluent) to provide the desired product as a white solid.

EXAMPLE 40 (METHOD 13) [3-Chloro-4- (2-hydroxy-ethyl) -phenyl] -carbamic acid tert-butylester To a stirred suspension of sodium borohydride (0.45 g) in tetrahydrofuran (13 ml) a 0 ° C glacial acetic acid (0.75 ml) is added and the mixture is stirred at 0 ° C for 1 hour. The solution was then heated to. Room temperature and 2-trimethylsilyl-ethyl ester (3-chloro-4-vinyl-phenyl) -carbamic acid (1.0 g) was added. The reaction was stirred at room temperature for about 15 hours and then heated to reflux for about 20 hours. The mixture was then cooled and the solutions of 5N aqueous sodium hydroxide (0.80 ml) and 30% aqueous hydrogen peroxide (0.56 ml) were added. After stirring for an additional 15 hours, the layers were separated, the aqueous layer was extracted three times with diethyl ether, these organic extracts were dried over anhydrous magnesium sulfate. Following removal of the solvent under reduced pressure, the residue was chromatographed on silica gel (40% ethyl acetate in hexanes was used as the eluent) to provide the desired product as an amber oil.

EXAMPLE 41 (METHOD 14) 2-Trimethylsilane-ethyl ester of [4- (l-azidoethyl) -3-chloro-phenyl] -carbamic acid To a solution of 2-trimethylsilane 1-ethyl ester of [3-chloro- 4- (1-Hydroxy-ethyl) -phenyl] -carbamic acid (1.25 g) in tetrahydrofuran (20 ml) at 0 ° C under an argon atmosphere was added triphenylphosphine (2.6 g), hydroxyacetic acid (about 2.5 molar equivalent in dichloromethane). , were prepared by the method of Fieser and Fieser, Rea gen ts for Organ ic Syn thes is, Vol. 1, p 446, Wiley, New York) and diethyl azodicarboxylate (1.72 g). After about 10 minutes, the solvent was removed under reduced pressure and the residue was chromatographed on silica gel (5% ethyl acetate in hexanes was used as the eluent) to provide the desired product as a colorless oil.

EXAMPLE 42 (METHOD 15) [3-Chloro-4- (3-dimethylaminoprop-1-ynyl) -phenyl] -carbamic acid tert-butylester To a deoxygenated solution of tert-butylester of (3-chloro-4) acid -dodo-phenyl) -carbamic acid (10.0 g) in triethylamine (120 ml) was added l-dimethylamino-2-propin (2.82 g), bis (triphenylphosphine) -palladium (II) chloride (0.4 g), and iodide cuprous (0.054 g). The mixture was stirred at room temperature under an argon atmosphere for approximately 6 hours and then briefly heated (ca. 10 minutes) to 60 ° C. The reaction mixture was then cooled, filtered through diatomaceous earth, and the solvent was removed by evaporation under reduced pressure. The residue was dissolved in ethyl acetate, washed three times with water, united. once with saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate. The solvent was removed by evaporation under reduced pressure, and the residue was subjected to chromatography on silica gel (80% ethyl acetate in hexanes was used as the eluent) to give the purified product as an amber oil which solidified in stagnant . Using the above procedure and appropriate starting materials, the following compounds were prepared: [3-Chloro-4- (3-dimethylaminoprop-1-ynyl) -phenyl] -carbamic [3- (4-methoxy-phenyl) -prop-2-ynyl] -dimethyl-amine 4-butylester. - (3-Dimethylamino-prop-1-ynyl) -benzonitrile Dimethyl- [3- (4-nitro-phenyl) -prop-2-ynyl] -amine EXAMPLE 43 (METHOD 16) [3-Chloro-4- (3-dimethylamino-acryloyl) -phenyl] -carbamic acid tert-butylester A. an ice-cooled solution of [3-chloro-4-] tert-butylester (3-dimethylamino-prop-1-ynyl) -phenyl] -carbamic acid (4.0 g) in dichloromethane (30 ml) was added in small portions of 3-chloropercxybenzoic acid (2.34 g). After the reaction was stirred at 0 ° C for 20 minutes, the mixture was passed over twenty equivalents by weight of basic alumina (Grade 1 of Broc mann, 150 mesh) and the N-oxide was eluted using a 5% methanol solution. in dichloromethane. All fractions containing the desired amine N-oxide were combined and evaporated to near dryness under reduced pressure. The residue was treated successively three times with small portions of methanol (ca. 50 ml) followed by evaporation to dryness under reduced pressure., and the volume of the solution was adjusted to 250 ml by the addition of methanol. The methanolic solution of the N-oxide was then heated to reflux for about 15 hours, then cooled, and the solvent was evaporated to dryness under reduced pressure. The residue was purified by chromatography on silica gel (80% ethyl acetate in hexanes was used as the eluent) to give the desired product as a pale yellow solid.

EXAMPLE 44 (METHOD 17) (3-Chloro-4-isoxazol-5-yl-phenyl) -carbamic acid tert-butylester solution of [3-chloro-4- (3-dimethylamino-acryloyl) tert-butylester] ) -phenyl] -carbamic acid (270 mg) in dioxane (3 ml) was treated with hydroxylamine hydrochloride (122 mg) and the mixture was stirred at room temperature for 10 days. The mixture was diluted with ethyl acetate, washed successively with water, 5% aqueous sodium bicarbonate, saturated aqueous sodium chloride, and then dried over anhydrous magnesium sulfate. The solvent was removed by evaporation under reduced pressure and the resulting residue was chromatographed on silica gel (33% ethyl acetate in hexanes or the eluent was used) to provide the desired product as a colorless solid.

EXAMPLE 45 (METHOD 18) [3-Chloro-4- (lH-pyrazol-3-yl) -phenyl] -carbamic acid tert-butyl ester Jna solution of [3-chloro-4- (3- dimethylamino-acryloyl) -phenyl] -carbamic acid (250 mg) in ethanol (1.25 ml) was treated with hydrazine hydrate (0.25 ml) and the mixture was stirred at room temperature for 3 hours. The mixture was then diluted with 30 ml of diethyl ether, washed three times with water, once with saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate. The solvent was removed by evaporation under reduced pressure and the resulting residue was subjected to chromatography on silica gel (67% ethyl acetate in hexanes was used as the eluent) to provide the desired product as an oil.

EXAMPLE 46 (METHOD 19A) N- (2-Clo: co-4-nitrophenyl) -2-thiomorpholino-4-yl-acetamide To a solution of N- (chloroacetyl) -2-chloro-4-nitroaniline (3.80 g) in tetrahydrofuran (50 ml) thiomorpholine (10 ml) was added and the solution was allowed to stand for 1 hour. This reaction mixture was poured into water, a pale yellow solid was collected and then recrystallized from hot 2-propanol to give a pale yellow crystalline solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: (4- {2- (Bis- (2-hydroxy-ethyl) -amino] -acetylamino} -phenyl) -butyl ester. -carbamic acid [4- (2-dimethylaminoacetylamino) -phenyl] -carbamic acid tert-butylester. { 4- [3- (2-Dimethylamino-ethoxy) -benzyllamino] -phenyl} -carbamic Ter-butyl ester of acid. { 4- [3- (2-morpholin-4-yl-ethoxy) -benzoylamino] -phenyl} -carbamic N- (2-chloro-4-nitro-phenyl) -2-dimet i lamino-acetamide N- (2-Clo or-4-nitro-phenyl) -2-piperidin-l-yl-acetamide N- ( 2-Chloro-4-nitro-phenyl) -2-morpholin-4-yl-acetamide N- (2-Chloro-4-nitro-phenyl) -2-dipropylamino-acetamide N- (2-Chloro-4-nitro- phenyl) -2-t iomorpholin-4-yl-acetamide N- (2-Chloro-4-nitro-phenyl) -2-diet i lamino-ace tamide N- (2-Chloro-4-nitro-phenyl) -2 -pyrrolidin-1-yl-acetamide 2-Azepan-l-yl-N- (2-chloro-4-nitro-phenyl) -acetamide N- (2-Chloro-4-nitro-phenyl) -2- (2 -met il-piperidin-1-yl) -acetamide N- (2-Chloro-4-nitro-phenyl) -2- (3-meth i 1 -piperidin-1-yl) -acetamide N- (2-Chloro- 4-nitro-phenyl) -2- (4-meth i 1-piper idin-1-yl) -acetamide EXAMPLE 47 (METHOD 19B) N- (2-Chloro-4-nitrophenyl) -2- (2-dimethylaminoethyl-sulfanyl) acetamide a solution of N- (chloroacetyl) -2-chloro-4-nitroaniline (3.01 g) in N , N-dimet ilformamide (100 ml) was added powdered sodium carbonate (6.0 g) and 2-dimethylaminoethane hydrochloride (6.0 g). The mixture was stirred for 1 hour at 25 ° C, poured into water and extracted into ethyl acetate. The ethyl acetate solution was dried over anhydrous potassium carbonate and concentrated under reduced pressure to give an oil. The oil was crystallized from toluene-hexanes (3: 1) to yield a pale yellow crystalline solid.

EXAMPLE 48 (METHOD 20) 2-Piperidin-l-yl-ethyl ester of (4-tert-butoxycarbonylamino-2-chloro-phenyl) -carbamic acid To a suspension of 1,1-carbonyl-di- (1, 2, 4 ) -triazole (4.0 g) in dichloromethane (40 ml) was added a solution of tert-butylester of (4-amino-3-chloro-phenyl) carbamic acid (5.0 g) in dichloromethane (45 ml) dropwise during 20 minutes. The reaction was stirred at room temperature for 30 minutes at which point it formed a precipitate. To this mixture was added piperidinetanol (6.6 ml) and tetrahydrofuran (20 ml) was added to maintain homogeneity. After heating to reflux overnight, the reaction was cooled and then poured into water, the organic layer was separated and then washed with saturated aqueous sodium chloride. The solution was dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure to a crude oil which was purified by chromatography on silica gel (5% methanol in dichloromethane was used as the eluent) to give the desired product as a white foam.

EXAMPLE 49 5-Phenyl- [1, 2, 3] thiadiazole-4-carboxylic acid methyl ester A solution of ethyl benzoylacetate (1.1 g) in acetonitrile (10 ml) was treated with 4-ethylbenzenesulfonyl azide (1.3 g) and triethylamine (1.6 g).

After stirring overnight at room temperature, the reaction was concentrated under reduced pressure and the resulting crude product was dissolved in ethyl acetate and washed with IN sodium hydroxide. The organic layer was then dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure to produce a yellow oil. This oil was taken up in dichloromethane and filtered through a hydrous magnesium silicate bearing, which is eluted with dichloromethane to give the partially purified diazoketone as a colorless oil. A sample of the diazoketone from the above (1.2 g) was dissolved in toluene (25 ml) and treated with 2,4-bis (4-methoxyphenyl) -1,3-dithia-2,4-diphosphetan-2 , 4-di sulfide (2.8 g) and the reaction was heated to reflux. After 3 hours, the reaction was cooled to room temperature, loaded onto a silica gel pad and eluted with dichloromethane. After removing the solvent under reduced pressure, the resulting oil was purified by chromatography on silica gel (30% diethyl ether in petroleum ether as the eluent) and then recrystallized from hexanes to give the desired product as needles. pale yellow. Using the above procedure and appropriate starting materials, the following compounds were prepared: Ethyl ester of 5-phenyl- [1,2,3] thiadiazole-4-carboxylic acid Methyl ester: r of 5-methyl- [1, 2, 3] thiadiazole-4-carboxylic acid EXAMPLE 50 Semicarbazide of ethyl benzoylacetate Ethyl benzoylacetate (5.0 g) was dissolved in methanol (10 ml) and rapidly added to a hot solution of semicarbazide hydrochloride (29 g) in water (130 ml). To this was added pyridine (4.1 g) and after heating to reflux for 5 minutes, the reaction mixture was cooled to -20 ° C overnight. The resulting solid semicarbazone was collected by filtration, washed with water and then with diethylether to give the desired product as white crystals. Using the above procedure and appropriate starting materials, the following compounds were prepared: (Z) -3- [(Methylcarbonyl) hydrazone] -4,4,4-trifluorobutanoate ethyl Ethyl ester of 3- [(Z) - acid 2- (aminocarbonyl) hydrazono] -3-phenylpropanoic acid ester 3- [(E) -2- (aminocarbonyl) hydrazono] -3- (3-furyl) propanoic acid ester EXAMPLE 51 Ethyl < 5-phenyl- [1, 2, 3] thiadiazole-5-carboxylic acid ester A solution of semicarbazone of ethyl benzoylacetate (2.5 g) in pure thionyl chloride (5 ml) was stirred at 0 ° C for 1 hour. Then dichloromethane was added (25 ml), the excess thionyl chloride was destroyed with saturated aqueous sodium bicarbonate. The precipitate forming a rapid cooling was removed by filtration and the filtrate was extracted with dichloromethane. The collected organic extracts were dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure. Chromatography on silica gel (50% hexanes in dichloromethane was used as the eluent) afforded the desired product as a colorless oil. Using the above procedure and appropriate starting materials, the following compounds were prepared: 4-met yl- [1, 2, 3] thiadiazole-5-carboxylic acid methyl ester 4-phenyl- [1, 2, 3 ] tiadiazole-5-carboxylic acid 4-furan-3-yl- [1, 2, 3] thiadiazole-5-carboxylic acid ethyl ester EXAMPLE 52 4-methyl- [1,2,3] thiadiazole-5-acid carboxylic acid 4-Methyl- [1, 2, 3] thiadiazole-5-carboxylic acid methyl ester (1.7 g) was dissolved in methanol (15 ml) and treated with IN sodium hydroxide (16 ml). After stirring at room temperature for 1 hour, the reaction was treated with concentrated hydrochloric acid (1.5 ml) and concentrated under reduced pressure. The resulting turbid aqueous layer was extracted twice with diethyl ether and the collected organic layers were dried over anhydrous magnesium sulfate., filtered and concentrated under reduced pressure to give the desired compound as a white powder. Using the above procedure and appropriate starting materials, the following compounds were prepared: 3-e-Toxocarbonyl-L-methoxy-benzoic acid 5-f-3-yl- [1, 2, 3] thiadiazole-4-carboxylic acid thia-zol- 4-carboxylic acid 4-met yl- [1, 2, 3] -thiadiazole-5-carboxylic acid 5-methyl- [1, 2, 3] -thiadiazole-4-carboxylic acid EXAMPLE 53 (METHOD 25) 4-C Trifluoro-methanesulfonic acid-5-methoxy-2-nitro-phenyl ester To a solution of 4-chloro-5-methoxy-2-nitrophenol (6.5 g) in dichloromethane ( 150 ml) at 0 ° C under an argon atmosphere was added triethylamine (10 g) and then a solution of trifluoromethanesulfonic anhydride (13.5 g) in dichloromethane (30 ml). The solution was stirred at 0 ° C for 10 minutes, and then diluted with dichloromethane and washed successively with saturated aqueous sodium bicarbonate and saturated aqueous sodium chloride. After drying over anhydrous sodium sulfate, the solvent was removed by evaporation under reduced pressure and the residue was dissolved in a solution of 20% dichloromethane in hexanes and passed through a short column of hydrous magnesium silicate ( 20% dichloromethane in hexanes as the eluent). The fractions containing the product were collected and the solvents were removed by evaporation under reduced pressure to give the desired product as a yellow oil. Using the above procedure and appropriate starting materials, the following compounds were prepared: trifluoromethanesulfonic acid 4-chloro-5-methoxy-2-nitro-phenylester 4-chloro-2-nitro-phenyl ester of trifluoromethane, sulfonic 2-chloro-6-nitro-phenylester of trifluoromethanesulfonic acid EXAMPLE 54 (METHOD 26) [4- (3-dimethylamino-benzoylamino) -phenyl] -carbamic acid t-Butylester A solution of [4- (3-amino-benzoylamino) -phenyl] -carbamic acid t-butylester ( 505 mg), sodium cyanoborohydride (250 mg), acetic acid (3 drops) and 40% aqueous formaldehyde (4 ml) in tetrahydrofuran-methanol 1: 2 (15 ml) was stirred for 15 minutes, and then poured in saturated aqueous sodium bicarbonate and extracted into ethyl acetate. The ethyl acetate solution was dried over anhydrous potassium carbonate and concentrated under reduced pressure to give a solid which was recrystallized from acetonitrile to give a pale pink crystalline solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: [4- (3-dimethylamino-benzylamino) -phenyl] -carbamic acid tert-butylester (3-Bromo-5-tri fluoromethyl-1-phenyl) -dimet il-amine N- (3-chloro-5-dimethyl-1-amino-phenyl) -acetamide EXAMPLE 55 (METHOD 27) N- (4-Aminophenyl) -2-hydroxybenzamide To a solution of 2- (4-aminophenylcarbamoyl) phenyl acetate (580 mg) in methanol (10 ml) was added saturated sodium bicarbonate (2 ml. ) and water (3 ml). The mixture was heated at 80 ° C for 30 minutes, then poured into semi-saturated aqueous sodium chloride and extracted with ethyl acetate. The ethyl acetate solution was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give an oil which was then triturated with diethylether to provide the desired product as a white solid.

EXAMPLE 56 (METHOD 28) [4- (3-hydroxybenzoylamino) phenyl] -butylester} Carbamic acid To a solution of 3- (4-aminophenylcarbamoyl) phenyl acetate (4.34 g) in methanol (75 ml) was added 0.1 N aqueous sodium hydroxide (25 ml) and tetrahydrofuran (25 ml). This solution was heated at 40 ° C for 30 minutes, then cooled, poured into 1 M hydrochloric acid and extracted with ethyl acetate. The ethyl acetate solution was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a white solid, which was further purified by trituration with diethyl ether.

EXAMPLE 57 (METHOD 29) N- (4-Aminophenyl) -2-hydroxymethylbenzamide To a solution of N- (4-aminophen-1) phthalimide (332 mg | in tetrahydrofuran (4 ml) was added lithium borohydride (1.0 g) and the mixture was stirred for 1 hour at 25 ° C. The mixture was poured into water and extracted into ethyl acetate.The ethyl acetate solution was dried over anhydrous sodium sulfate and concentrated under reduced pressure to give a white foam. , which when triturated with diethyl ether gave the desired product as a white powder.

EXAMPLE 58 (METHOD 30) (3-Chloro-5-dimethylamino-phenyl) -carbamic acid tert-butylester To a solution of (3-amino-5-oloro-phenyl) -carbamic acid tert-butylester (0.32 g) in toluene Water (10 ml) was added aqueous formaldehyde (37%, 1.5 ml) then 10% palladium on charcoal (0.50 g) and the mixture was stirred under a hydrogen atmosphere for approximately 15 hours. The solution was then filtered through diatomaceous earth and the filtrate was concentrated under reduced pressure. The residue was chromatographed on silica gel (50% dichloromethane in hexanes was used as the eluent) to provide the desired product as a white solid.

EXAMPLE 59 (METHOD 35) N- (4- [3- [3, 5-Dichloro-4- (2-hydroxy-ethoxy) -phenyl] -thioureido}. -phenyl) -acetamide To a solution of 2 -. { 4- [3- (-acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} Acetic acid ethyl ester (0.16 g) in a mixture of tetrahydrofuran and methanol 1: 1 (2.5 ml) was added IN aqueous sodium hydroxide (1 ml) and the mixture was stirred for about 2 hours at room temperature. The solution was then poured into 2 M aqueous hydrochloric acid (3 ml), extracted into ethyl acetate, and the extracts were dried over anhydrous sodium sulfate. The solvent was removed by evaporation under reduced pressure and the residue was triturated with diethylether to yield the desired product as a solid b] anco.

EXAMPLE 60 (METHOD 36) Acid. { 4- [3- (4-acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetic To a solution of acid ethyl ester. { 4- [3- (4-acetylami o-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetic (0.29 g) in a mixture of tetrahydrofuran and methanol 1: 1 (4 mL) aqueous sodium hydroxide was added (2 ml) and the mixture was stirred for about 2 hours at room temperature. The solution was then poured into 2 M aqueous hydrochloric acid (5 ml), extracted into ethyl acetate, and the extracts were dried over anhydrous sodium sulfate. The solvent was removed by evaporation under reduced pressure and the residue was triturated with diethylether to yield the desired product as a white solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: Acid. { 4- [3- (4-acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetic acid. { 2- [3- (4-acetylamino-phenyl) -thioureido] -4-chloro-5-methoxy-phenoxy} -acetic acid. { 4- [3- (4-acetylamino-phenyl) -thioureido] -2-chloro-5-met. oxyphenoxy} -acetic EXAMPLE 61 (METHOD 37) 2-. { 4- [3- (4-acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} benzoic acid ethyl ester To an ice-cold solution of N- (4- {3 - [3, 5-dichloro-4- (2-hydroxy-ethoxy) -phenyl] -thioureido} - phenyl) - acetamide (0.20 g) in pyridine (2 ml) and tetrahydrofuran (0.5 ml) was added benzoyl chloride (0.08 g) and the mixture was stirred at 0 ° C for 1.5 hours. The mixture was then diluted with ethyl acetate, washed successively twice with 2% aqueous hydrochloric acid, once with saturated aqueous sodium chloride, then dried over anhydrous sodium sulfate. After removal of the solvent under reduced pressure, the residue was subjected to chromatography on silica gel (5% methanol in dichloromethane was used as the eluent) and the product containing the fractions was combined, evaporated under reduced pressure, and the residue was recrystallized from acetone-hexanes to provide the desired product as a white powder.

EXAMPLE 62 (METHOD 38) 2-. { 4- [3- (4-acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} methanesulfonic acid ethyl ester To an ice-cold solution of N- (4- {3 - [3, 5-dichloro-4- (2-hydroxy-ethoxy) -phenyl] -thioureido} - phenyl) - acetamide (0.20 g) in pyridine (2 ml) and tetrahydrofuran (0.5 ml) was added methanesulfonyl chloride (0.11 g) and the solution was stirred at 0 ° C for 45 minutes. The reaction mixture was then diluted with ethyl acetate, washed successively twice with 2% aqueous hydrochloric acid, once with saturated aqueous sodium chloride, and then dried over anhydrous magnesium sulfate. After removal of the solvents by evaporation under reduced pressure, the resulting residue was recrystallized from acetone-hexanes to give the desired product as a white powder.

EXAMPLE 63 (METHOD 39) N- (4-. {3- [3,5-Dichloro-4- (2-dimethylamino-ethoxy) -phenyl] -thioureido} -phenyl) -acetamide To a solution of 2 -. { 4- [3- (4-acetylanyl-phenyl) -ti oureido] -2,6-dichlorophenoxy} methanesulfonic acid ethyl ester (0.33 g) in tetrahydrofuran (6 ml) was added aqueous dimethylamine (8.8 M, 0.5 ml) and the mixture was stirred at room temperature for 5 days. The reaction mixture was then diluted with ethyl acetate, then washed with saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate. After removal of the solvent under reduced pressure, the residue was subjected to chromatography on silica gel (pure methanol was used as the eluent). The fractions containing the harvested product were evaporated under reduced pressure and the residue was recrystallized from acetonitrile to provide the desired product as a white powder. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- (4 -. {3- [3, 5-Dichloro-4- (2-dimethylamino-ethoxy) -phenyl] -thiou.reido}-phenyl) -acetamide 2-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -benzoic acid ester EXAMPLE 64 (METHOD 40) (4- { 3- [4- (1-Amino-ethyl) -3-chloro-enyl] -thioureido.} - phenyl) -amide of furan-2-carboxylic acid A Tin chloride dihydrate solution (Il) (0.25 g) in methanol (2.5 ml) was added (4-. {3- [4- (1-azido-ethyl) -3-chloro-phenyl] -thioureido} - phenyl) -amide of furan-2-carboxylic acid (0.22 g) and the solution was stirred for about 15 hours at room temperature. The solution was then diluted with ethyl acetate, washed successively with saturated aqueous sodium bicarbonate then saturated aqueous sodium chloride, then dried over anhydrous sodium sulfate. After removal of the solvent by evaporation under reduced pressure the residue was chromatographed on silica gel (8% methanol in dichloromethane containing 1% triethylamine as the eluent) to provide the desired product as a yellow solid.

EXAMPLE 65 (METHOD 41) [1,2,3] -thiadiazole-4-carboxylic acid (4-isothiocyanato-phenyl) -amide an ice-cooled solution of 1,1'-thio-carbonyldiimidazole (7.28 g) in tetrahydrofuran (50 mL) [1,2,3] -thiadiazole-4-carboxylic acid (4-amino-phenyl) amide (9.0 g) in tetrahydrofuran was added (100 ml). After about one hour, the solvent was removed by evaporation and the residue was dissolved in ethyl acetate. Diethyl ether was added to precipitate the crude product, which was then collected by filtration, dissolved in dichloromethane, and passed through a plug of hydrous magnesium silicate. After removal of the solvents, the residue was recrystallized from ethyl acetate-hexanes to give the desired product as a slightly yellow solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: 2-Fluoro-N- (4-isothiocyanato-phenyl) -benzamide (4-isothiocyanato-phenyl) -amide of furan-2-carbexylic acid (4- Isothiocyanato-phenyl) -amide of [1,2,3] -thiadiazole-4-carboxylic acid (-isothiocyanato-phenyl) -amide of thiazole-4-carboxylic acid EXAMPLE 66 (METHOD 42) N, N-Dimethyl-5-trifluororne -l-benzene-1,3-diamine To a solution of 3-amino-5-bromo-benzot rifle luoride (1.0 g) in degassed tetrahydrofuran (argon) ( 2 ml) was added bis- (tri-o-tolylphosphino) palladium (0.15 g), a solution of dimethylamine in tetrahydrofuran (2M, 4.2 ml), and a solution of lithium bis (trimethylsilyl) amide in tetrahydrofuran (1M, 10.4 ml). The reaction mixture was heated in a sealed container at 100 ° C for about 2.5 hours until the reaction was complete.

The mixture was then cooled to room temperature, quenched by the addition of water, and diluted with ethyl acetate. The product was extracted three times in 5% aqueous hydrochloric acid, and the collected acid extracts were then basified with cooling by addition of 5N aqueous sodium hydroxide. This basic solution was then extracted with ethyl acetate, and these collected organic extracts were washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, and evaporated to dryness under reduced pressure. The resulting residue was chromatographed on silica gel (20-30% ethyl acetate in hexanes was used as the eluent) to provide the desired product as a lightly colored solid. Using the above procedure and appropriate starting materials, the following compounds were prepared: 3- (4-Methyl-piperazin-1-yl) -5-trifluoromethyl-phenol 3-Morpholin-4-yl-5-tri fluorometyl- phenylamine 3-Piperidin-l-yl-5-trifluoromethyl-phenyl amine 3-pyrrolidin-l-yl-5-trif luoromethyl-phenylamine N, N-Dimethyl-5-trifluoromethyl-benzene-1,3-diamine N-Isobutyl N-methyl-5-tri fluorometyl-benzene-1,3-diamine N-Butyl-N-methyl-5-trifluoromethyl-1-yl-3-diamine EXAMPLE 67 (METHOD 43) Acid tert-butylester ( 3-isobutyl-5-trifluoromethylphenyl) -carbamic acid To a sealed tube containing tetrahydrofuran (5 ml) which was capped with a rubber packing and cooled in a dry ice-acetone bath was bubbled with isobutylene for approximately 5 minutes . A solution of 9-borabicyclo [3.3.1] nonane in tetrahydrofuran (0.5 M, 11 ml) was added, the vessel was sealed with a Teflon cap, warmed slowly to room temperature and maintained at room temperature for approximately 2.5. hours. The mixture was then re-cooled in a dry-acetone ice bath, the Teflon lid was replaced by a rubber gasket, and the argon was bubbled through the vent mixture to remove the excess isobutylene. A solution of tert-butylester of (3-bromo-5-t-rifluoromethyl-phenyl) -carbamic acid was added (1.7 g) in tetrahydrofuran (12 ml), followed by a complex of [1, 1'-bis (diphenylphosphino) -ferrocen] palladium (II) chloride-dichloromethane (0.12 g) and then 3N aqueous sodium hydroxide. The container was sealed again with the Teflon cap and then heated to 65 ° C for about 15 hours. The mixture was then cooled to room temperature, diluted with hexanes, washed with water, saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate, and evaporated under reduced pressure. The resulting oil was chromatographed on silica gel (5% ethyl acetate in hexanes was used as the eluent) to provide the desired product as a white powder. Using the above procedure and appropriate starting materials, the following compounds were prepared: [3- (2-methyl-yl-butyl) -5- t-rif1-butyl-butyl-phenyl] -carbamic acid tert-butylester -isobutyl-5-tri fluoromethyl-phenyl) -carbamic EXAMPLE 68 (METHOD 44) 2- (3,5-Dichloro-phenylsulfanyl) -ethylamine To a solution of (3,5-dichlorophenylthio) -acetonitrile (1.2 g) in 3.0 ml of ethylene glycol dimethyl ether was added 0.61 ml of a complex of 10M borane-dimethene sulfide and the mixture was heated to reflux for 0.5 hours. The reaction was cooled in an ice bath and 2.0 ml of water and 2.0 ml of concentrated hydrochloric acid were added. This mixture was heated to reflux for 0.5 hours. The clear solution was then cooled and basified with 5N sodium hydroxide and extracted with ether. The ether extract was dried over potassium carbonate, filtered and concentrated to give 1.0 g of a colorless oil. Using the above procedure and appropriate starting materials, the following compounds were prepared: 2- (3-Bromo-phenylsulfanyl) -ethylamine 2- (4-Bromo-phenoxy) -ethylamine 2- (4-iodo-phenoxy) -ethylamine 2 - (3, 4-Dichloro-phenoxy) -ethylamine 2- (3-Chloro-phenyl sulphyl) -et i sheet 2- (3, -Dichlorophenyl sulphyl) -et i sheet 3- (4-Bromo- phenyl) -propi lane 2- (2-Fluoro-phenoxy) -ethylamine 2- (2-Chloro-phenoxy) -ethylamine 2- (3-Bromo-phenoxy) -ethylamine 2- (3-fluoro-phenoxy) -ethylamine 2 - (3-iodo-phenoxy) -ethylamine 2- (3,5-Dichlorophenylsulfonyl) -eti lamin 2-Phenyl-sulpyl-ethylamine 1- (2-Chloro-phenyl) -ethylamine EXAMPLE 69 (METHOD 45) N- (1-Naphthalen-2-yl-ethyl) -formamide A mixture of 2-acetylnaphthylene (3.0 g), ammonium formate (11.0 g), formic acid (3.3 ml) and formamide (3.5 ml) was heated at 190 ° C for 3 hours. The mixture was cooled, poured into water and extracted with ether. The ether extract was dried with anhydrous potassium carbonate, filtered and concentrated to give an anion oil, which was recrystallized from toluene-hexanes to give a white solid, 1.97 g. Using the above procedure and appropriate starting materials, the following compounds were prepared: N- [1- (4-Fluoro-phenyl) -2-methyl-propyl] -formamide N- (l-Naphthalen-2-yl-ethyl) -formamide EXAMPLE 70 (METHOD 46) 1- (2-Naphthyl) ethylamine A mixture of N- (1-naphthalen-2-yl-yl) -formamide (1.12 g), ethanol (10 ml) and 5 N sodium hydroxide ( 10 ml) was heated to reflux for 1 hour. The solution was cooled, poured into water and extracted with ether. The ether solution was dried with anhydrous potassium carbonate, filtered and concentrated to give the product (0.95 g) as a pale yellow oil.

Using the above procedure and appropriate starting materials, the following compounds were prepared: 1- (3-Trifluoromethyl-phenyl) -ethylamine 1- (4-Fluoro-phenyl) -2-methyl-propylamine [3- (1-Amino- ethyl) -phenyl] -dimethyl-amine 3- (1-Amino-ethyl) -benzonitrile EXAMPLE 71 (METHOD 47) 1- (3-Trifluoromethyl-phenyl) -ethanone o-Methyl-oxime Methoxylamine hydrochloride (2.33 g) was added to a solution of 3 '- (trifluoromethyl) -acetophenone (1.5 g) in ethanol (20 ml) and pyridine (2 ml). The solution was heated to reflux for 45 minutes. The reaction mixture was then cooled, concentrated under reduced pressure and partitioned between water and ethyl acetate. The aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give the desired product as a colorless oil (1.61 g). Using the above procedure and appropriate starting materials, the following compounds were prepared: 3, 5-Bis-trifluoromethyl-benzaldehyde O-methyl 1- (4-fluoro-phenyl) -propan-1-one oxime O-Methyl-oxime 1- (2-chloro-phenyl) -ethanone oxime O Methyl-oxime of 1- (3-bromo-phenyl) -ethanone O-Methyl-oxime of 1- (3-chloro-phenyl) -ethanone O-Methyl-oxime of 1-p-tolyl-ethanone O-Methyl- 1- (4-fluoro-phenyl) -pentan-1-one oxime O-Methyl-oxime 1- (4-fluoro-phenyl) -2-phenyl-ethanone O-Methyl-oxime of 1-o-tolyl- ethanone O-Methyl-oxime of 1-m-tolyl-ethanone O-Methyl-oxime of 1- (2-fluoro-phenyl) -ethanone 3- (1-Methoxyimino-ethyl) -benzonitrile 4- (1-Methoxyimino-) -ethyl) -benzonitrile 1- (4-methoxy-phenyl) -ethanone O-Methyl-oxime 1- (2-methoxy-phenyl) -ethanone O-Methyl-oxime 1- (4-methyl) oxime dimethylamino-phenyl) -ethanone O-Methyl-oxime of 1- (2-trifluoromet-il-phenyl) -ethanone O-methyl-oxime of 1- (3-methoxy-phenyl) -ethanone O-Methyl-oxime of 1- (3-trifluoromethyl-phenyl) -ethanone O-Methyl-1- (4-trifluoromethyl-phenyl) -ethanone oxime O-Methyl-cime of l-furan-2-yl-ethanone O-Methyl-cime L-pyridin-4-yl-ethanone O-Methyl-1-methyl (1-methyl-1H-pyrrol-2-yl) -ethanone O-Metyl-oxime of l-thiophen-3-yl-ethanone O- Methyl-cime of (4-fluoro-phenyl) -pheni-1-metona O-Methyloxime of 1- (4-methoxy-phenyl) -ethanone O-Methyl-oxime of 1- (3-chloro-4-methoxy-phenyl) - ethanone 4- (1-Methoxyimino-ethyl) -benzenesulfonami at 4- (1-Methoxyimino-ethyl) -N, N-dimet i-benzenesulfonamide O-Methyl-oxime of 1- [4- (piperidin-1-sulphonyl ) -phenyl] - ethanone 4- (1-Methoxyimino-ethyl) -N, N-dipropyl-benzenesulfonamide 2-Fluoro-N- [4- (1-methoxyimino-eti 1) -phenyl] -benzamide O-Methyl-oxime of 1- (3, 5-bis-trifluoromethyl-phenyl) -ethanone O-Methyl-oxime of 1- [4- (lH-imidazol-1-yl) phenyl] -1-ethanone O-Methyl-oxime 1- [4- (trifluoromethyl) phenyl] -1-ethanone O-Met yl ima of 1- [1, 1'-biphenyl] -4-yl-1-ylone O-Methyloxime of 1- (-methylphenyl) -1 -etanone 1- [4-Fluoro-3- (trifluoromethyl) phenyl] -ethanone O-Methyloxime 1- [3,5-bis (trifluoromethyl) phenyl] -ethanone O-methyl ester 1- [4-Chloro-3- (trifluoromethyl) phenyl] -ethanone O-Methyloxime of 1- [3-fluoro-5- (trifluoromethyl) phenyl] -ethanone O-Methyloxime of 1- [2-fluoro- 4- (trifluoromethyl) phenyl] -ethanone O-Met ilo < 1- [2-Fluoro-5- (trifluoromethyl) phenyl] -ethanone O-Methyloxime 1- (2,4-dichlorophenyl) ethanone O-Methyloxime of 1- (2,4-dimethylphenyl) -ethanone O-Methyloxime of 1- [2,4-bis (trifluoromethyl) phenyl] ethanone O-Methyloxime of 1- (3-bromopheni 1) ethanone O-Methyloxime of 1- (3-methylphenyl) ethanone O-Methyloxime of l- [4- (4-morpholinyl) phenyl] ethanone O-Methyloxime of 1- (2-chloro-4-fluorophenyl) ethanone O-Methyloxime of 1- (4-bromo-2-fluorophenyl) ethanone O-Methyloxime of 1- (3,4) -difluorophenyl) ethanone 1- [3-trifluoromethyl) phenyl] ethanone O-Methyloxime 1- [2-trifluoromethyl] phenyl] ethanone O-Methyloxime 1- (2,4-difluorophenyl) ethanone O-Methyloxime O-Met ilox ima de l- [3-fluoro-4- (trifluorometi 1) phenyl] ethanone O-Methyloxima of 1- (3,4-dichlorophenyl) ethanone O-Met ilox ima of l- [4-fluoro-2- ( trifluoromethyl) phenyl] • ethanone O-Methyloxima of 1- (3-chloro-4-fluorophenyl) ethanone O-Methyloxime of 1- (4-chloro-3-fluorophenyl) ethanone O-Metiloxime of 1- (2, 5 -d ifluorophenyl) ethanone O-Metiloxame of 1- (2-bromo-4-fluorophenyl) ethanone O-Methyloxime of 1- (3, 4-dibromophenyl) ethanone O-Metiloxime of 1- (2-bromophenyl) ethanone EXAMPLE 72 ( METHOD 48) 1- (2-Tri-luoromethyl-phenyl) -ethylamine 3e slowly added sodium borohydride (1.17 g) to a flask containing zirconium tetrachloride (1.8 g) in tetrahydrofuran (27 ml). A solution of 1- (2-trifluoromethylphenyl) -ethanone O-meth il-oxime (1.34 g) in tetrahydrofuran (7.7 ml) was added and the resulting solution was stirred at 25 ° C for 12 hours. The reaction mixture was then cooled to 0 ° C and water (16 ml) was slowly added. The excess ammonium hydroxide was added and the solution was extracted twice with ethyl acetate. The organic portion was washed twice with IN hydrochloric acid. The aqueous layer (acid) was basified with sodium hydroxide and extracted twice with ethyl acetate. The organic layer was then washed with saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate. The solvent was removed under reduced pressure to provide the desired product as a yellow oil (0.20 g). Using the above procedure and appropriate starting materials, the following compounds were prepared: 1- (3-Methoxy-phenyl) -ethylamine 1- (4-Fluoro-phenyl) -propylamine 1 -Na phthalen-2-yl-ethyl amine 4- (1-Amino-et ) -benzonitrile 1- (4-Trifluoromethyl-phenyl) -ethylamine 1- (4-methoxy-phenyl) -ethylamine l-Prop-2-ynyl-pyrrolidine 1- (2-methoxy-phenyl) -ethylamine 1-m-Tolyl -ethylamine 1- (2-Bromo-phenyl) -ethylamine 1 -o-Tol i 1-ethylamine C- (4-Fluoro-phenyl) -C-phen i 1-methylamine 1- (4-Fluoro-phenyl) -pent i lamin 1- (4-Fluoro-phenyl) -2-phenyl-ethylamine 1- (2-trifluoromethyl-phenyl) -ethylamine 1- (3-Bromo-phenyl) -ethylamine 1- (3-chloro-phenyl) -ethylamine [4- (1-Amino-ethyl) -phenyl] -dimethyl-amino 1- (l-Methyl-lH-pyrrol-2-yl) -ethylamine-1-thiophen-3-yl-y-ylamine 1- [3, 5 bis (Trifluoromethyl) phenyl] propi lamin 1- [3,5-bis (Trifluoromethyl) phenyl] -1-butanamine 1- [3,5-bis (trifluoromethyl) phenyl] butylamine 1- [3,5-bis (Trifluoromet il) phenyl] -1-pentanamine 1- (4-methylphenyl) ethanamine 1- [3- (Tri fluoromet i 1) phenyl] ethyl amine 1- [4- (Trifluoromethyl) phenyl] ethylamine 1- (3-methylphenyl) ethanamine 1- (3,4-dichlorophenyl) ethanamine 1- (2-bromo-phenyl) -ethylamine 1- (2-trifluoromethyl-phenyl) -ethylamine 1- (3-Bromo-phenyl) -ethylamine 1- (3-Chloro-4-methoxy-phenyl) -ethylamine 4- (1-Amino-ethyl) -N, N-dimethyl-il-benzene sulphonamide [4- (Piperidin-1-sulfonyl) -phenyl] -ethylamine l-Quinolin-6-yl-ethylamine 1- (3,5-Bis -tri fluoromet i 1-phenyl) -ethylamine 4- [(SS) -l -aminoethyl] benzonitrile (S) -alpha-Methyl-3,5-bis (trifluoromethyl) -benzmetanamine (S) -alpha-methyl-3, 5- bis (rifluoromet il) -benzenemethanamine l-Biphenyl-4-yl- and 1- (1- Fluoro-phenyl) -ethylamine 1- [4-flucro-3- (trifluoromethyl) phenyl] ethanamine 1- [4-chloro-3- (trifluoromethyl) phenyl] ethanamine N-. { 4- [(1 P) -1- aminoethyl] phenyl} -1,2, 3-thiadiazole-4-carboxamide N-. { 4- [(SS) -1-aminoethyl] phenyl} -l, 2,3-thiadiazole-4'-carboxamide 1- [3-fluoro-5- (trifluoromethyl) phenyl] ethylamine 1- [2-fluoro-4- (tri fluoromethyl) phenyl] ethylamine l- [2-flucro- 5- (t ri luororneti 1) phenyl] ethylamine 1- 2, 4-dichlorophenyl) ethylamine 1- 2, 4 -dimethylphenyl) ethylamine 1- 2, 4- (bis (trifluoromethyl) phenyl] ethylamine 1- 2 -chloro-4 -fluorophenyl) ethylamine 1- 3, 4-difluorophenyl) ethylamine 1-4-bromo-2-fluorophenyl) ethylamine 1- 3-fluorophenyl) ethylamine 1- 2, 4-difluorophenyl) ethylamine 1- 3-fluoro-4- (trifluoromethyl) ) phenyl] ethylamine 1-4-fluoro-2- (trifluoromethyl) phenyl] ethylamine 1- 3-chloro-4-fluorophenyl) ethylamine 1-4-chloro-3-fluorophenyl) ethylamine 1- 3, 4 -dibromophenyl) ethylamine 1 - 2-bromo-4-fluorophenyl) ethanamine 1- (2-bromo-fluorophenyl) ethylamine EXAMPLE 73 (METHOD 49) (2-Fluoro-5-trifluoromethyl-phenoxy) -acetonitrile A solution of 2-fluoro-5-tri fluoromethyl-phenol (25 g) in reactive grade acetone (0.55 1) was treated with sodium carbonate. solid potassium (7.7 g) followed by the rapid addition of pure bromoacetonitrile (10 ml) .. The heterogeneous mixture was stirred vigorously for about 20 hours after which it was poured into water and extracted into diethyl ether. The combined ether extracts were washed with saturated sodium chloride and dried over anhydrous potassium carbonate. Filtration and concentration under reduced pressure gave a pale orange solid which was then chromatographed on silica gel, eluting with dichloromethane, to give the desired product as a white solid (28.3 g). Using the above procedure and appropriate starting materials, the following compounds were prepared: (3-Bromo-phenylsulfanyl) -acetonitrile (3-chlorophenyl sulphyl) -acetonitrile (4-iodo-phenoxy) -acetonitrile (3-trifluoromethyl) phenylsulfanyl) -acetonitrile (3,5-Dichloro-phenyl sulphonyl) -acetonitrile (3,4-Dichloro-phenylsulfanyl) -acetonitrile (3,4-Dichloro-phenoxy) -acetonitrile (2-Fluoro-phenoxy) -acetonitrile (3) -Fluoro-phenoxy) -acetonitrile (2-chlorophenoxy) -acetonitrile (3-Bromo-phenoxy) -acetonitrile (2-Fluorc-5-trifluoromethyl-phenoxy) -acetonitrile (3-iodo-f-enoxy) -acetonitrile ( 4-Bromo-phenoxy) -acetonitrile EXAMPLE 74 (METHOD 50) Tosilabo of 3-fluoro-5-trifluoromethylphenethylamine A solution of 2.5 g of 3-fluoro-5-trifluoromethylphenylacetonitrile and 2.34 g (12.3 mmole) of p-toluenesulfonic acid in 75 ml of ethylene glycol monomethylester is hydrogen for 3 hours at room temperature at 40 psi, using 200 mg of a sodium catalyst. aladio on carbon at 10%. The catalyst was removed by filtration and the solvent was evaporated to half the volume. When it stagnates, the salt of p-toluenesulfonic acid of the desired 3-fluoro-5-t rifluoromethyl-phenethylamine is crystallized. White crystals, 4.26 g (91%), were collected by filtration. Using the above procedure and appropriate starting materials, the following compounds were prepared: 2- (3,5-difluoro-phenyl) -ethylamine 2- (4-trifluoromethyl-phenyl) -ethylamine 2- (3,4-difluoro-phenyl) ) -ethylamine 2- (2-Fluoro-phenyl) -ethylamine 2- (3-Fluoro-5-trifluoromethyl-phenyl) -ethylamine 2- (2-Fluoro-3-trifluoromethyl-phenyl) -ethylamine 2- (2, 4-Bis -trifluoromethyl-phenyl) -ethylamine 2- (4-Fluoro-3-trifluoromethyl-phenyl) -ethylamine EXAMPLE 75 (METHOD 51) (4-Aminomethyl-2-trifluoromethyl-enyl) -dimethyl-amine A solution of 4 -dimethylamino-3-trifluoromethylbenzonitrile (0.35 g) in tetrahydrofuran (2 ml) was slowly added to a suspension of lithium aluminum hydride (0.1 g) in tetrahydrofuran (2 ml) at 0 ° C and stirred under an atmosphere of argon for 2 hours. While water was added slowly at 0 ° C (0.1 ml) followed by 5% sodium hydroxide (0.1 ml) and water (0.3 ml). The resulting gray solid was filtered and washed with tetrahydrofuran. The filtrates were collected and concentrated under reduced pressure and the resulting oil was chromatographed on silica gel (15% methanol in methylene chloride was used as the eluent) to afford the desired product as a pale orange oil (0.164 g) . Using the above procedure and appropriate starting materials, the following compounds were prepared: 4-Piperic in 1-3-tri fluoromet i 1-benzylamine (4-Aminornetyl-2-trifluoromethyl-phenyl) -dimethyl-amine 4- ( 4-Methyl-piperazin-1-yl) -3-tri fluoromet i 1-benzylamine (3-Aminop? Ethyl-5-trifluoromethyl-phenyl) -dimethyl-amine [3- (2-Amyl-ethyl) -5- tri fluoromet il-phenyl] -dimethyl-amine [- (2-Ami non-ethyl) -2-met il-phenyl] -dimethyl-amine EXAMPLE 76 (METHOD 52) 3-Dd.methylamino-5-trifluorornethyl-benzaldehyde 3e add dropwise diisobutyl aluminum hydride (10 ml of a 1M methylene chloride solution) to a solution of 3-dimethylamino-5-trifluoromethyl-benzonitrile (1.06 g) in methylene chloride (25 ml) 0 ° C and the mixture was stirred for 2 hours. While a saturated aqueous solution of potassium sodium tartrate (8 ml) was slowly added at 0 ° C, the solution was stirred for 1.5 hours. The reaction mixture was then extracted with ethyl acetate, dried over anhydrous magnesium sulfate and concentrated under reduced pressure to provide the desired product as a yellow solid (0.97 g). Using the above procedure and appropriate starting materials, the following compounds were prepared: 3-Dimethyl-amino-5-t-rifluoromethyl-benzaldehyde -Dimethyl-amino-3-methyl-benzaldehyde EXAMPLE 77 (METHOD 53) Dimeti - [3- (2-nitro-vinyl) -5-trifluoromethyl-phenyl] -amine Nitromethane (0.473 g) was added to a solution of 3-dimethylamino-5-trifluoromethyl-benzaldehyde ( 0.885 g) and ammonium acetate (0.339 g) in acetic acid (3.4 ml) and the solution was heated at 110 ° C for 6 hours. The reaction mixture was cooled to 0 ° C and a solid form which was fi ltered and washed with water-acetic acid 1: 1. This solid was recrystallized from ethanol to provide the desired product as a red solid (0.39 g). Using the above procedure and appropriate starting materials, the following compounds were prepared: Dimethyl- [3- (2-nitro-vinyl) -5-trifluoromethyl-phenyl] -amine Dimethyl- [2-methyl-4 - (2 -nitro-vinyl) -phenyl] -amine EXAMPLE 78 (METHOD 54) 3- (4-Bromo-phenyl) -propionitrile Diethyl azodicarboxylate (5.2 g) was added dropwise to a solution of 4-bromophenetic alcohol (2.01 g), and triphenylphosphine (7.9 g) in diethyl ether ( 16 ml) at 0 ° C. I read reaction mixture was stirred for 10 minutes and a solution of acetone cyanohydrin (2.6 g) in diethyl ether (10 ml) was added. The light orange solution was stirred for 5 minutes at 0 ° C and then at 25 ° C for 12 hours. The reaction mixture was then filtered, and washed with diethyl ether. The filtrate was concentrated under reduced pressure and subjected to chromatography on silica gel (10% ethyl acetate-hexanes was used as the eluent) to provide the desired product as a pale yellow oil (2.04 g).

EXAMPLE 79 (METHOD 55) Ethyltexes of 3-dimethylamino-2-isocyano-acrylic acid To a solution of ethyl isocyanoacetate (5.0 g) in ethanol (100 ml) was added N, N-dimethylformamide dimethylacetal (6.5 g) dropwise with stirring for 10 minutes. The reaction was stirred for 24 hours and the ethanol was evaporated. The resulting oil was passed through magnesium silicate using 50% ethyl acetate-hexanes as the eluent. The solvents were removed and the resulting oil was crystallized from ethyl acetate-hexanes to give light yellow needles, 3.0 g.

EXAMPLE 80 (METHOD 56) 4-Carboethoxy iazole A solution of 3-dimethylamino-2-isocyanoacrylic acid ethyl ester (1.0 g) and triethylamine (3.0 g) in tetrahydrofuran (30 ml) was treated with sulfur (ie hydrogen gas until all the starting material was consumed.) The mixture was concentrated to an oil and purified by column chromatography using silica and 25% ethyl acetate. ethyl-hexanes as the eluent The purified material (0.61 g) was isolated as an oil.

EXAMPLE 81 (METHOD 34) N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -ureido] -phenyl} -2- fluoro-benzamide A suspension of N- (4-amino-phenyl) -2-fluoro-benzamide. (0.43 g) in acetonitrile (4 ml) was treated with 5-chloro-2,4-dimethoxyphenylisocyanate (0.40 g). The mixture becomes a solution and is allowed to stand for 12 hours. A white solid is formed and collected by filtration (0.79 g). [M + H) 444. Using the above procedure and appropriate starting materials, the following compounds were prepared: EJ. M + H NAME OF COMPOUND NO. 81 445 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -ureido] -phenyl} -2-fluoro-benzamide 82 441 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -ureido] -f -enyl} -2-methyl-benzamide 83 435. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -ureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 84 443. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -ureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 85 453 N-. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -ureido] -phenyl} -2-fluoro-benzamide 86 409. { 4- [3- (3, 5-Dichloro-phenyl) -ureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acidamide 486 N-. { 4- [3- (3,5-Bis-trifluoromethyl-phenyl) -ureido] -f -enyl} -2-f luoro-benzamide 88 458. { 4- [3- (3,5-bis-Trifluoromethyl-phenyl) -ureido] -phenyl} -furan-2-carboxylic acid amide 89 476. { 4- [3- (3, 5-bis-trif luoromethyl-f-enyl) -ureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 90 423. { 4- [3- (3,4-Dichloro-benzyl) -ureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide EXAMPLE 91 (METHOD 31) N- (5-. {[[( { (ÍS) -l- [3,5-bis (trifluoromethyl) phenyl] ethyl} - amino) carbo thioyl] -amino} -2-pyridinyl) -1,3-thiazole-4-carboxamide A mixture of N- (5-isothiocyanato-2-pyridinyl) -1,3-thiazole-4-carboxamide (0.36 g) and (S) - alf a-methyl-3, 5-bis (t rif luoromet il) -benzenemethamine (0.36 g) was heated with acetonitrile (10 ml) until all the solids dissolved. The solution was allowed to stand for 12 hours. A white solid was formed and collected by filtration (0.40 g). [M + H] 520. Using the above procedure and appropriate starting materials, the following compounds were prepared: EJ. M + H NAME OF COMPOUND NO. 92 506 [3-Chloro-5- (3. {4- [([1, 2, 3] -thiadiazol-4-carbonyl) -amino] -phenyl] -thioureido) -butylester. phenyl] -carbamic 93 409 1- (5-Chloro-2, -dimethoxy-f-enyl) -3- (4-morpholin-4-yl-phenyl) -thiourea 94 370 1- (5-Chloro-2, 4 -dimethoxy-f-enyl) -3- (4-methylsulfonyl-phenyl) -thiourea 95 338 1- (5-Chloro-2,4-dimethoxy-f-enyl) -3-p-tolyl-thiourea 96 414 Acid. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl sulphonyl} -acetic 97 384 1- (5-Chloro-2,4-dimethoxy-phenyl) -3- [4- (2-hydroxy-ethoxy) -phenyl] -thiourea 98 340 l- (5-chloro-2,4- dimethoxy-phenyl) -3- (4-hydroxy-phenyl) -thiourea 99 395 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-f-enyl) -thioureido] -phenyl} -N-methyl-acetamide 100 381 N-. { 3- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 101 411 Ethyl ester of acid. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl] -thioureido] -phenyl] -carbamic acid 102 319 1- (2,4-dimethoxy-phenyl) -3- (4-methoxy-phenyl) ) -tiourea 103 346 N-. { 4- [3- (2, 4-Dimethoxy-phenyl) -thioureido] -phenyl} - acetamide 104 316 N-. { 4- [3- (4-Methoxy-phenyl) -thioureido] -phenyl} - acetamide 105 316 N-. { 4- [3- (2-Methoxy-phenyl) -thioureido] -phenyl} - acetamide 106 351 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - acetamide 107 351 N-. { 4- [3- (5-Chloro-2-methoxy-phenyl) -thioureido] -phenyl} - acetamide 108 371 N-. { 4- [3- (3, 5-Dichloro-4-hydroxy-phenyl) -thioureido] -phenyl} -acetamide 109 385 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 110 381 N-. { 4- [3- (4-Chloro-2,5-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 111 389 N-. { 4- [3- (2-Chloro-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -acetamide 112 389 N-. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -acetamide 113 422 4- [3- (4-Acetylamino-phenyl) -thioureido] -3-hydroxy-phenylester of benzoic acid 114 457 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-methyl-benzamide 115 501 2-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl-carbamoyl} -acetic acid phenylester 116 461 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -4-fluoro-benzamide 117 461 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-fluoro-benzamide 118 461 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 119 473 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-methoxy-benzamide 120 473 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-methoxy-benzamide 121 473 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -4-methoxy-benzamide 122 443 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 123 417 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -metansulfonamide 124 331 N-. { 4- [3- (3-Nitro-phenyl) -thioureido] -phenyl} -acetamide 125 339 1- (3-Chloro-4-methoxy-phenyl) -3- (3-nitro-phenyl) -thiourea 126 337 N-. { 4- [3- (5-Chloro-2-hydroxy-phenyl) -thioureido] -phenyl} -acetamide 127 439 ter-butyl ester of acid. { 4- [3- (5-Chloro-2, 4- dimethoxy-phenyl) -thioureido] -phenyl} -carbámico 128 351 N-. { 4- [3- (3-Chloro-4-hydroxy-5-methyl-phenyl) -thioureido] -phenyl} -acetamide 129 385 N-. { 4- [3- (3,5-Dichloro-4-hydroxy-2-methyl-phenyl) -thioureido] -phenyl} -acetamide 130 318 N-. { 4- [3- (2, 4-Dihydroxy-phenyl) -thioureido] -phenyl} - acetamide 131 414 N-. { 4- [3- (2,4-Dimethoxy-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -acetamide 132 332 N-. { 4- [3- (2-Hydroxy-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 133 465 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -4-fluoro-benzamide 134 500 3-Acetylamino-N-. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 135 488 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-nitro-benzamide 136 486 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-dimethylamino-benzamide 137 536 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-methanesulfonyl-amino-benzamide 138 511 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-trifluoro-methyl-benzamide 139 459 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-hydroxy-benzamide 140 479 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2, 6-difluoro-benzamide 141 477 2-Chloro-N-. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 142 522 2-Bromo-N-. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 143 488 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-nitro-benzamide 144 445. { 4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -phenyl} - pyrazine-2-carboxylic acid amide 145 463. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-methyl-thiophene-2-carboxylic acid amide 146 494. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -quinoline-8-carboxylic acid amide 147 446. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -l-methyl-lH-pyrrole-2-carboxylic acid amide 148 369 1- (5-Chloro-2,4-dimethoxy-phenyl) -3- (2-nitro-phenyl) -thiourea 149 369 1- (5 -Cloro-2,4-dimethoxy-phenyl) -3- (4-nitro-phenyl) -thiourea 150-425 N-. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 151 376 N-. { 4- [3- (3, 4, 5-trimethoxy-phenyl) -thioureido] -phenyl} - acetamide 152 399 N-. { 4- [3- (3,5-Dichloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -acetamide 153 499. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzo [b] thiophene-2-carboxylic acid amide 154 483. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzofuran-2-carboxylic acid amide 155 444 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -isonicotinamide 156 493. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} Naphthalene-2-carboxylic acid amide 157 493. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} Naphthalene-1-carboxylic acid amide 158 494. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -isoquinoline-1-carboxylic acid amide 159 494. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -quinoline-2-carboxylic acid amide 160 444 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -nicotinamide 161 478 Acid phenylester. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -Charmic 162 459. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-nitro-furan-2-carboxylic acid amide 163 467. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-chloro-furan-2-carboxylic acid amide 164 439 Isobutyl ester of acid. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -carbamic 165 397 Methyl ester of acid. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -Charmic 166 433. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -furan-3-carboxylic acid amide 167 447. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 3-methyl-furan-2-carboxylic acid amide 168 512. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-bromo-furan-2-carboxylic acid amide 169 512. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 4-bromo-furan-2-carboxylic acid amide 170 433. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 171 467 Hexyl ester of acid. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -carbatic 172 494. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -isoquinoline-4-carboxylic acid amide 173 451. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 174 434. { 1 H- [1,2,3] triazole-4-carboxylic acid 4- [3- (5-chloro-2, 4-dimethoxy-phenyl) -thioureido] -phenyl-amide 175 528. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 3-bromo-thiophene-2-carboxylic acid amide 176 399 N-. { 4- [3- (5-Chloro-4-ethoxy-phenyl) -thioureido] -phenyl} - acetamide 177 427 N-. { 4- [3- (4-Butoxy-3,5-dichloro-phenyl) -thioureido] -phenyl} -acetamide 178 461 N-. { 4- [3- (4-Benzyloxy-3,5-dichloro-phenyl) -thioureido] -phenyl} -acetamide 179 381 N-. { 4- [3- (3-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 180 530 (3- {4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -phenylcarbamoyl} -phenyl} -carbamic acid ethyl ester 181 458 2-Amino-N -. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 182 519. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -Biphenyl-2-carboxylic acid amide 183 469 l- (5-Chloro-2,4-dimethoxy-phenyl) -3- [4- (1,3-dioxo-l, 3-dihydro-isoindol-2-yl) ) -phenyl] -thiourea 184 487 N- acid. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -phthalmic 185 473 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-hydroxy-methyl-benzamide 186 479 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2, 3-difluoro-benzamide 187 479 N-. { 4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -phenyl} -2,5-difluoro-benzamide 188 479 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2,4-difluoro-benzamide 189 500 2-Acetylamino-N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 190 441 l- (5-Chloro-2,4-dimethoxy-phenyl) -3- (6-oxo-5,6-dihydro-phenanthridin-2-yl) -thiourea 191 536 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-methanesulfonylamino-benzamide 192 497 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2, 3, 4-trifluoro-benzamide 193 533 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2, 3,4,5, 6-pentafluoro-benzamide 194 489 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-methylsulfanyl-benzamide 195 431. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -ureido] -phenyl} 5-methyl-furan-2-carboxylic acid amide 196 467. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -ureido] -phenyl} - 5-difluoromethyl-furan-2-carboxylic acid amide 197 472 N-. { 4- [3- (5-Iodo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 198 364 N-. { 4- [3- (5-Fluoro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 199 365 N-. { 4- [3- (5-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -acetamide 200 459. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 201 455. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 202 392 N-. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} -acetamide 203 432 N- (4-. {3- [3-Chloro-4- (cyclohexyl-methyl-amino) -phenyl] -thioureido}. phenyl) -acetamide 204 506. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} l-hydroxy-naphthalene-2-carboxylic acid amide 205 406 N-. { 4- [3- (3-Chloro-4-morpholin-4-yl-phenyl) -thioureido] -phenyl} -acetamide 206 443 l- (5-Chloro-2,4-dimethoxy-phenyl) -3- (3-chloro-4-morpholin-4-yl) phenyl) -thiourea 207-372 1- (5-chloro-2, 4-dimethoxy-phenyl) -3- (5-chloro-2-methyl-phenyl) -thiourea 208 501 Methyl ester of N- acid. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -isophthalmic 209 487 N- acid. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl-isophthalamic 210 549 3-Benzyloxy-N-. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 211 434 N- (4-. {3- [5-Chloro-2-methoxy-4- (4-nitrile-butoxy) -phenyl] -thioureido}. -phenyl) -acetamide 212 406 N- ( 4- {3- [5-Chloro-2-methoxy-4- (2-nitrile-ethoxy) -phenyl] -thioureido} -phenyl) -acetamide 213 406 N- (4- {3- [5-Chloro-4-methoxy-2- (2-nitrile-ethoxy) -phenyl] -thioureido.] - phenyl) -acetamide 214 411 N- (4-. {3- [5-Chloro-2- (2-hydroxy-ethoxy) -4-methoxy-phenyl] -thioureido.} - phenyl) -acetamide 215 411 N- (4-. {3- [5-Chloro-4- (2-hydroxy-ethoxy)] -2-methoxy-phenyl] -thioureido.}. -phenyl) -acetamide 216 481 Ter-butyl ester of acid. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-5-methoxy-phenoxy} -acetic 217 439 Methyl ester of acid. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-5-methoxy-phenoxy} -acetic 218 481 Ter-butyl ester of acid. { 2- [3- (4-Acetylamino-phenyl) -thioureido] -4-chloro-5-methoxy-phenoxy} -acetic 219 515 3-Butoxy-N-. { 4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -benzamide 220 505 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-methansulfinyl-benzamide 221 545 (3- {4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenylcarbamoyl} -phenoxy) -acetic acid ethyl ester 222 517 (3- {4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] phenylcarbamoyl} - phenoxy) -acetic acid 223 367 N-. { 4- [3- (5-Chloro-4-hydroxy-2-methoxy-phenyl) -thioureido] -phenyl} -acetamide 224 444. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} pyridine-2-carboxylic acid amide 225 494. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -quinoline-4-carboxylic acid amide 226 436 N-. { 4- [3- (5-Chloro-4-methoxy-2-morpholin-4-yl-phenyl) -thioureido] -phenyl} -acetamide 227 394 N-. { 4- [3- (5-Chloro-2-dimethylamino-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 228 420 N-. { 4- [3- (5-Chloro-4-methoxy-2-pyrrolidin-1-yl-phenyl) -thioureido] -phenyl} -acetamide 229 434 N-. { 4- [3- (5-Chloro-4-methoxy-2-piperidin-1-yl-phenyl) -thioureido] -phenyl} -acetamide 230 405. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - [1, 2, 3-thiadiazole-4-carboxylic acid amide] 231 415 N-. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - 2-fluoro-benzamide 232 427 N-. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - 3-methoxy-benzamide 233 387. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 234 411 N-. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - 2-methyl-benzamide 235 433 N-. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - 2,6-difluoro-benzamide 236 398. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - pyridine-2-carboxylic acid amide 237 502 (4-. {3- [3-Chloro-4- (cyclohexyl-methyl-amino) -phenyl] -thioureido} -phenyl) -amide of acid [1 , 2, 3] -thiadiazole-4-carboxylic acid 238 512 N- (4-. {3- [3-Chloro-4- (cyclohexyl-methyl-amino) -phenyl] - thioureido} phenyl) -2-fluoro-benzamide 239 404 N-. { 4- [3- (3-Chloro-4-piperidin-1-yl-phenyl) -thioureido] -phenyl} -acetamide 240 364 N-. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} -acetamide 241 426 N-. { 4- [3- (4-Benzylamino-3-chloro-phenyl) -thioureido] -phenyl} -acetamide 242 390 N-. { 4- [3- (3-Chloro-4-pyrrolidin-1-yl-phenyl) -thioureido] -phenyl} -acetamide 243 419 N-. { 4- [3- (3-Chloro-4- (4-methyl-piperazin-1-yl) -phenyl] -thioureido.} - phenyl) -acetamide 244 469 N-. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 245 422 N-. { 4- [3- (2-Benzylamino-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 246 484. { 4- [3- (3-Chloro-4- (cyclohexyl-methyl-amino) -phenyl] -thioureido.} - phenyl) -amide of furan-2-carboxylic acid 247 508 N- (4-. {3- [3-Chloro-4- (cyclohexyl-methyl-amino) -phenyl] -thioureido} -phenyl) -2-methylbenzamide 248 530 N- (4-. { 3- [3-Chloro-4- (cyclohexyl-methyl-amino) -phenyl] -thioureido} - phenyl) -2,6-difluoro-benzamide 249 495 (4-. {3- 3-Chloro -4- (cyclohexyl-methyl-amino) -phenyl] -thioureido.} - phenyl) -amide of pyridine-2-carboxylic acid 250 524 N- (4-. {3- [3-Chloro-4- ( cyclohexyl-methyl-amino) -phenyl] -thioureido.}. -phenyl) -3-methoxy-benzamide 251 376 N- (4-. {3- [3-Chloro-4- (2-nitrile-ethoxy) - phenyl] -thioureido.}. -phenyl) -acetamide 252 393 N-. { 4- [3- (4-sec-Butoxy-3-chloro-phenyl) -thioureido] -phenyl} -acetamide 253 501 3-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl-carbamoyl} phenyl acetic acid 254 459 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-hydroxy-benzamide 255 487. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} benzo [1,3] dioxol-4-carboxylic acid amide 256 527 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3-trifluoro-methoxy-benzamide 257 530 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3- (2-dimethylamino-ethoxy) -benzamide 258 572 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -3- (2-morpholin-4-yl-ethoxy) -benzamide 259 406 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- cyano-phenyl} -3-acetamide 260 521 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2,5-dimethoxy-phenyl} -2-fluoro-benzamide 261 441 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2,5-dimethoxy-phenyl} -acetamide 262 527 2- Acid. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2- chloro-phenoxy} -5-chloro-benzenesulfonic acid 263 562 2-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2- chloro-phenoxy} -4,5-dichloro-benzenesulfonic 264 527. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 4-phenyl- [1, 2, 3] thiadiazole-5-carboxylic acid amide 265 381 N- (4-. {3- [3-Chloro-4- (2-hydroxy-ethoxy) -phenyl] - thioureido.}.-phenyl) -acetamide 266 393 N-. { 4- [3- (4-Butoxy-3-chloro-phenyl) -thioureido] -phenyl} Acetamide 267 446 N- (4-. {3- [3-Chloro-4- (cyclohexyl-ethyl-amino) -phenyl] -thioureido}. phenyl) -acetamide 268 365 N-. { 4- [3- (3-Chloro-4-ethoxy-phenyl) -thioureido] -phenyl} - acetamide 269 427 N-. { 4- [3- (4-Benzyloxy-3-chloro-phenyl) -thioureido] -phenyl} -acetamide 270 317 Ter-butyl ester of acid. { 4- [(3-Methyl-furan-2-carbonyl) -amino] -phenyl} -carbámico 271 456 N-. { 4- [3- (2-Benzylamino-5-chloro-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 272 420 N-. { 4- [3- (3-Chloro-4-dipropylamino-phenyl) -thioureido] -phenyl} -acetamide 273-458 N- (4-. {3- [4- (Allyl-cyclohexyl-amino) -3-chloro-phenyl] -thioureido}. -phenyl) -acetamide 274-411 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methoxy-phenyl} -acetamide 275 415 N-. { 2-Chloro-4- [5-chloro-2,4-dimethoxy-phenyl) -thioureido] -fe'nil} -acetamide 276 493. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2,5-dimethoxy-phenyl} -furan-2-carboxylic acid amide 277 486 N-. { 4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -2- cyano-phenyl} -2-fluoro-benzamide 278 495 N-. { 2-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 279 465. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-methyl- [1, 2, 3] thiadiazole-4-carboxylic acid amide 280 517. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-furan-3-yl- [1, 2, 3] -thiadiazole-4-carboxylic acid amide 281 527. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} 5-phenyl- [1, 2, 3] thiadiazole-4-carboxylic acid amide 282 458 N- (4-. {3- [3-Chloro-4- (octahydro-quinolin-1-yl) -phenyl] ] -thioureido.}.-phenyl) -acetamide 283 458 N- [5- [[[(5-Chloro-2,4-dimethoxyphenyl) -amino] -thioxomethyl] amino] -2-pyridinyl] -2-methylbenzamide 284 434. { 5- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-2-yl} -furan-2-carboxylic acid amide 285 425 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methoxy-5-methyl-phenyl} -acetamide 286 505 N-. { 4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -2-methoxy-5-methyl-phenyl} -2-fluoro-benzamide 287 477. { 4- [3- (5-Chloro-2, 4-dimethoxy-phenyl) -thioureido] -2-methoxy-5-methyl-phenyl} furan-2-carboxylic acid amide 288 517. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -amide of 4-furan-3-yl- [1, 2, 3] -thiadiazole-5-carboxylic acid 289 462 N-. { 5- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-2-yl} -2-fluoro-benzamide 290 384 N-. { 4- [3- (4-Methoxy-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -acetamide 291 394 N- [4- (3. {3-Chloro-4- [(2-hydroxy-ethyl) -methyl-amino] -phenyl} -thioureido) -phenyl] -acetamide 292 485 N -. { 2-Benzoyl-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 293 565 N-. { 2-Benzoyl-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 294 537. { 2-Benzoyl-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 295 475 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methyl-phenyl} -2-fluoro-benzamide 296 447. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methyl-phenyl} -furan-2-carboxylic acid amide 297 395 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methyl-phenyl} -acetamide 298 435 N- [4- (3. {3-Chloro-4- [(3-dimethylamino-propyl) -methylamino] -phenyl} -thioureido) -phenyl] -acetamide 299 418 N-. { 4- [3- (3-Chloro-4-cyclohexylamino-phenyl) -thioureido] -phenyl} -acetamide 300 421 N- [4- (3 { 3-Chloro-4- [(2-dimethylamino-methyl) -methylamino] -phenyl} -.-thioureido) -phenyl] -acetamide 301 580 5- [ [[(5-Chloro-2,4-dimethoxyphenyl) amino] thioxomethyl] -amino] -2- [(2-fluorobenzoyl) amino] -N-phenyl-benzamide 302 552. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- phenylcarbamoyl-phenyl} -furan-2-carboxylic acid amide 303 491 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methoxy-phenyl} -2-fluoro-benzamide 304 463. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methoxy-phenyl} -furan-2-carboxylic acid amide 305 449 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- trifluoromethyl-phenyl} -acetamide 306 458. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- cyano-phenyl} -furan-2-carboxylic acid amide 307 467. { 2-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 308 501 [4 - [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- trifluoromethyl-phenyl} -furan-2-carboxylic acid amide 309 395 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- methyl-phenyl} -acetamide 310 475 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- methyl-phenyl} -2-fluoro-benzamide 311 447. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- methyl-phenyl} -furan-2-carboxylic acid amide 312 378 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -acetamide 313 408 Ethyl ester. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -carbámico 314 382 N-. { 5- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-2-yl} -acetamide 315 509 N- (4-. {3- [4- (l-Benzyl-piperidin-4-ylamino) -3-chloro-phenyl] -thioureido}. -phenyl) -acetamide 316 407 N- (4- {. 3- [3-Chloro-4- (2-dimethylamino-ethylamino) -phenyl] -thioureido}.-Phenyl) -acetamide 317 408 N- [4- (3. {3-Chloro-4 - [(2-methoxy-ethyl) -methyl-amino] -phenyl] -thioureido) -phenyl] -acetamide 318 421 N- (4-. {3- [3-Chloro-4- (3-dimethylamino -propylamino) -phenyl] -thioureido.}.-phenyl) -acetamide 319 495 N- (4- { 3- [4- (l-Benzyl-pyrrolidin-3-ylamino) -3-chlorophenyl] - thioureido.}.-phenyl) -acetamide 320 483. { 5-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -2-hydroxy-phenyl} -furan-2-carboxylic acid amide 321 431 N-. { 5-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -2-hydroxy-phenyl} -acetamide 322 511 (5H, 11H-Benzo [c] pyrrolo [1, 2-a] [1,4] diazepin-10-yl) - (2-chloro-4-imidazol-1-yl-phenyl) -metanone 323 451 (4-. {3- [5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl]} - [1, 2, 3] -thiadiazole-5-carboxylic acid amide 324 483. { 4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -naphthalene-1-yl} -furan-2-carboxylic acid amide 325 511 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -naphthalen-1-yl} -2-fluoro-benzamide 326 429 N-. { 5-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methyl-phenyl} -acetamide 327 509 N-. { 5-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methyl-phenyl} -2-fluoro-benzamide 328 481. { 5-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -2-methyl-phenyl} -furan-2-carboxylic acid amide 329 431 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -naphthalen-1-yl} -acetamide 330 416. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 31 561 [4- (3. {4 - [(1-benzyl-pyrrolidin-3-yl) -methyl-amino] -3-chloro-phenyl] -thioureido ) -phenyl] -furan-2-carboxylic acid amide 32 513 N- [4- (3. {3-Chloro-4- [methyl- (1-methyl-pyrrolidin-3-yl) -amino] - phenyl.}. -thioureido) -phenyl] -2-fluoro-benzamide 33 463 N-. { 4- [3- (5-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -2, 6-difluoro-benzamide 344-4 N- (4-. {3- [3-Chloro-4- (l-methyl-pyrrolidin-3-yloxy) -phenyl] -thioureido} -phenyl) -acetamide 335 434 N- (4-. {3- [3-Chloro-4- (l-methyl-piperidin-4-yloxy) -phenyl] -thioureido} -phenyl) -acetamide 336 422 N- (4- {3- [3-Chloro-4- (3-dimethylamino-propoxy) -phenyl] -thioureido}.-Phenyl) -acetamide 337 425 2-Acetylamino-5- [3- (5-chloro-2, 4-dimethoxy-phenyl) -thioureido] -benzoic acid 338 505 5- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- (2-fluoro-benzoylamino) -benzoic acid 339 477 Acid 5- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- [(furan-2-carbonyl) -amino] -benzoic 340 545 N- [4- (3- { 3-Chloro-4- [methyl- (1-methyl-piperidin-4-yl) -amino] -phenyl] -thioureido) -phenyl] -2,6-difluoro-benzamide 341 503 [4- (3. {3-Chloro-4- [methyl- (1-methyl-pyrrolidin-3-yl) -amino] -phenyl] -tyloreido) -phenyl] -amide [ 1, 2, 3] thiadiazole-4-carboxylic acid 342 443 N-. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} -2-Rethyl-benzamide 343 408 N- (4-. {3- [3-Chloro-4- (2-dimethylamino-ethoxy) -phenyl] -thioureido}. -phenyl) -acetamide 344 499 [4- Furan-2-carboxylic acid 3- ({3-chloro-4- [methyl- (l-methyl-piperidin-4-yl) -amino] -phenyl} -thioureido) -phenyl] -amide. 419 N-. { 4- [3- (3-Chloro-4-cyclohexyloxy-phenyl) -thioureido] -phenyl} -acetamide 346 440 N-. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} -2-methyl-benzamide 347 493 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methyl-phenyl} -2,6-difluoro-benzamide 348 462 N-. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} -2,6-difluoro-benzamide 349 531 N- [4- (3. {3-Chloro-4- [methyl- (1-methyl-pyrrolidin-3-yl) -amino] -phenyl}. thioureido) -phenyl] -2,6-difluorobenzamide 350 427. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} pyridine-2-carboxylic acid amide 351 430. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} pyridine-2-carboxylic acid amide 352 428. { 4- [3- (3-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} pyridine-2-carboxylic acid amide 353 417 (4- [3- (3-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 354 496 [4- (3. {3-Chloro-4- [methyl- (1-methyl-pyrrolidin-3-yl) -amino] -phenyl] -tyl-3-phenyl] -amide of pyridine 2-carboxylic acid 355-495 N-. {3-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 356 467. { 3-Chloro-4- [3- (5-chloro-2,4-dimethoxy-phenyD-thioureido] -phenyl} -amide of furan-2-carboxylic acid 357 515 N- { 4- [3 - (3-Chloro-4-cyclohexylsulfanyl-phenyl) -thioureido] -phenyl.} -2-fluoro-benzamide 358 449 N- { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl ) -thioureido] -3- trifluoromethyl-phenyl.}. -acetamide 359 529 N- { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-trifluoromethyl-phenyl} -2-fluoro-benzamide 360 421 N- { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2-dimethyl-amino-acetamide 361 473 ( 4- { 3- [3-Chloro-4- (2-dimethylamino-a cetylamino) - phenyl] -thioureido} -phenyl} -furan-2-carboxylic acid amide 362 501 N- (4-. {3- [3-Chloro-4- (2-dimethylamino-acetylamino) -phenyl] -thioureido} -phenyl) -2-fluoro -benzamide 363 461 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-pheny1} -2-piperidin-1-yl-acetamide 364 541 N- (4-. {3- [3-Chloro-4- (2-piperidin-1-yl-acetylamino) -phenyl] -thioureido} -phenyl ) -2-fluoro-benzamide 365 513 (4-. {3- [3-Chloro-4- (2-piperidin-1-yl-acetylamino) -phenyl] -thioureido} -phenyl) -amide of acid furan-2-carboxylic 366 463 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2-morpholin-4-yl-acetamide 367 543 N- (4-. {3- [3-Chloro-4- (2-morpholin-4-yl-acetylamino) -phenyl] -thioureido} -phenyl ) -2-fluoro-benzamide 368 515 (4-. {3- [3-Chloro-4- (2-morpholin-4-yl-acetylamino) -phenyl] -thioureido}. Phenyl) -amide of acid furan-2-carboxylic 369 414 N-. { 4- [3- (3-Chloro-4-methanesulfonylamino-phenyl) -thioureido] -phenyl} -acetamide 370 494 N-. { 4- [3- (3-Chloro-4-methanesulfonylamino-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 371 466. { 4- [3- (3-Chloro-4-methanesulfonylamino-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 372 481 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2- (2-dimethylamino-ethylsulfanyl) -acetamide 373 561 N- [4- (3- { 3-Chloro-4- [2- (2-dimethylamino-ethylsulfanyl) -acetylamino] -phenyl-thioureido) -phenyl] -2-fluorobenzamide 374 585 N- [4- (3- { 4- [(l-Benzyl-pyrrolidin-3-yl) -methylamino] -3-chloro-phenyl] -thioureido) -phenyl] -2-methyl-1-benzamide 375 523 N - [4- (3- { 3-Chloro-4- [methyl- (1-methyl-piperidin-4-yl) -amino] -phenyl] -thioureido) -phenyl] -2-methyl-benzamide 376 510 [4- (3. {3-Chloro-4- [methyl- (1-methyl-piperidin-4-yl) -amino] -phenyl] -tyl-3-phenyl] -amide of pyridin -2-carboxylic 377 347 N-. { 4- [3- (3-Chloro-4-vinyl-phenyl) -thioureido] -phenyl} - acetamide 378 441. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 379 452. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -amine of pyran-2-carboxylic acid 380 487 N-. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -2, 6-difluoro-benzamide 381 486 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-cyano-phenyl} -2-fluoro-benzamide 382 458. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-cyano-phenyl} -furan-2-carboxylic acid amide 383 406 N-. { 4- [3- (5-Chloro-2, -dimethoxy-phenyl) -thioureido] -3-cyano-phenyl} -acetamide 384 395 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -2-methyl-isothioureido] -phenyl} -acetamide 385 396 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -2-methyl-isothioureido] -phenyl} -acetamide 386 461 N-. { 4- [3- (3-Chloro-4-ethylsulfanyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 387 489 N-. { 4- [3- (4-Butylsulfanyl-3-chloro-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 388 411 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methoxy-phenyl} -acetamide 389 491 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methoxy-phenyl} -2-fluoro-benzamide 390 463. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -3-methoxy-phenyl} -furan-2-carboxylic acid amide 391 531 (4-. {3- [3-Chloro-4- (2-piperidin-1-yl-acetylamino) -phenyl] -thioureido} -phenyl-acid-amide [1,2,3 ] - thiadiazole-4-carboxylic acid 392 481 N- { 4- [3- (3-Chloro-4-methanesulfinyl-phenyl) -thioureido] -phenyl} -2,6-difluoro-benzamide 393 497 N- {. 4- [3- (3-Chloro-4-methanesulfonyl-phenyl) -thioureido] -phenyl} -2,6-difluoro-benzamide 394 459 N-. {4- [3- (5- Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -2-methyl-phenyl.} -2-fluoro-benzamide 395 429 N- { 4- [3- (3-Chloro-4-methyl phenyl) -thioureido] -2-methyl-phenyl.} -2-fluoro-benzamide 396 533 [4- (3. {3-Chloro-4- [2- (2-dimethylamino-ethylsulfanyl) -acetylamino] Furan-2-carboxylic acid amide 397-458 N-. {4- [3- (4-Acetylamino-3-chloro-phenyl) -thioureido] -phenyl} -amide} -2-fluoro-benzamide 398 460 Ethyl ester [2-chloro-4- (3- {4- [(furan-2-carbonyl) -amino] -phenyl} -thioureido) -phenyl} -carbamic 399 488 Ethyl ester of (2-chloro-4-. {3- [4- (2-fluoro-benzoylamino) -phenyl] -thioureido} -phenyl) -carbamic acid ester 400 440 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -benzamide 401 520 N-. { 4- [( { [4- (Benzoylamino) -3-chloro-phenyl] -amino.} - thioxomethyl) -amino] -phenyl} -2-fluoro-benzamide 402 529 N-. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -2- trifluoromethyl-phenyl} -2-fluoro-benzamide 403 492. { 4- [3- (4-Benzoylamino-3-chloro-phenyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 404 416 N-. { 4- [3- (4-Amino-3-chloro-phenyl) -thioureido] -phenyl} - 2-fluoro-benzamide 405 479 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2-thiomorpholin-4-yl-acetamide 406 531 (4-. {3- [3-Chloro-4- (2-thiomorpholin-4-yl-acetylamino) -phenyl] -thioureido} -phenyl) - Furan-2-carboxylic acid amide 407 559 N- (4-. {3- [3-Chloro-4- (2-thiomorpholin-4-yl-acetylamino) -phenyl] -thioureido} -phenyl ) -2-fluoro-benzamide 408 461 N-. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -2-methy1-phenyl} -2-fluoro-benzamide 409 430. { 4- [3- (4-Acetylamino-3-chloro-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 410 477 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2-dipropylamino-acetamide 411 529 (4-. {3- [3-Chloro-4- (2-dipropylamino-acetylamino) -phenyl] -thioureido} -phenyl) -amide of furan-2-carboxylic acid 412 449 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2-diethyl-amino-acetamide 413 501 (4-. {3- [3-Chloro-4- (2-diethylamino-acetylamino) -phenyl] -thioureido} -phenyl) -amide of furan-2 carboxylic acid 414 529 N- (4-. {3- [3-Chloro-4- (2-diethylamino-acetylamino) -phenyl] -thioureido}. phenyl) -2-fluoro-benzamide 415 447 N-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenyl} -2-pyrrolidin-l-yl-acetamide 416 499 (4-. {3- [3-Chloro-4- (2-pyrrolidin-1-yl-acetylamino) -phenyl] -thioureido}. -phenyl) - Furan-2-carboxylic acid amide 417 -527 N- (4-. {3- [3-Chloro-4- (2-pyrrolidin-1-yl-acetylamino) -phenyl] -thioureido} -phenyl) - 2-fluoro-benzamide 418 475 N-. { 4- [3- (5-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -3-methoxy-phenyl} -2-fluoro-benzamide 419 445 N-. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -3-methoxy-phenyl} -2-fluoro-benzamide 420 477 N-. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -3-methoxy-phenyl} -2-fluoro-benzamide 421 388. { 4- [3- (4-amino-3-chloro-phenyl) -thioureido] -phenyl} - acid amide furan-2-carboxylic acid 422 527 (4- { 3- [4- (2-Azepan-1-yl-acetylamino) -3-chloro-phenyl] -thioureido}. phenyl) -amide of furan- 2- carboxylic acid 423 555 N- (4- { 3- [4- (2-Azepan-l-yl-acetylamino) -3-chlorophenyl] -thioureido}. Phenyl) -2-fluorobenzamide 424 527 [4- (3. {3-Chloro-4- [2- (2-methyl-piperidin-1-yl) -acetyl-amino] -phenyl] -tyloreido) -phenyl] -amide of furan -2-carboxylic acid 425 555 N- [4- (3. {3-Chloro-4- [2- (2-methyl-piperidin-1-yl) -acetylamino] -phenyl} -thioureido) -phenyl ] -2-Fluorobenzamide 426 339 [4- (3-pyridin-2-yl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 427 339 [4- (3-pyridin-4-yl-thioureido ) -phenyl] -furan-2-carboxylic acid amide 428 367 2-Fluoro-N- [4- (3-pyridin-3-yl-thioureido) -phenyl] -benzamide 429 339 [4- (3-pyridine- 3-ylthioureido) -phenyl] -amide of furan-2-carboxylic acid 430 353. { 4- [3- (3-Amino-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 431 406. { 4- [3- (3-trifluoromethyl-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 432 380 2-Fluoro-N- [4- (3-m-tolyl-thioureido) -phenyl] -benzamide 433 434 2-Fluoro-N-. { 4- [3- (3-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 434 381 N-. { 4- [3- (3-Amino-phenyl) -thioureido] -phenyl} -2-fluorobenzamide 435 388. { 4- [3- (3-amino-5-chloro-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 436 352 [4- (3-m-Tolyl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 437 416 N-. { 4- [3- (2-Amino-5-chloro-phenyl) -thioureido] -phenyl} 2-fluoro-benzamide 438 571 2-Chloro-4-. {3- [4- (2-fluoro-benzoylamino) -phenyl] -thioureido} -piperidin-1-yl-ethyl ester. phenyl) -carbamic acid 439 543 2-Chloro-4- (3- {4- [(furan-2-carbonyl) amino] -phenyl} -thioureido} -piperidin-1-yl-ethyl ester] phenyl] -carbamic 440 388. { 4- [3- (2-Amino-5-chloro-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 441 363. { 4- [3- (3-Cyano-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 442 416 N-. { 4- [3- (3-Amino-5-chloro-phenyl) -thioureido] -phenyl} - 2-fluoro-benzamide 443 367 2-Fluoro-N- [4- (3-pyridin-2-yl-thioureido) -phenyl] -benzamide 444 367 2-Fluoro-N- [4- (3-pyridin-4 -yl-thioureido) -phenyl] -benzamide 445 374. { 4- [3- (6-chloro-pyridin-3-yl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 446 388. { 4- [3- (2-amino-3-chloro-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 447 396. { 4- [3- (3-hydrazinocarbonyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 448 410 2-Fluoro-N- (4-. {3- [3- (l-hydroxy-ethyl) -phenyl] -thioureido} -phenyl) -benzamide 449 414 . { 4- [3- (3-hydrazinocarbonyl-phenyl) -thioureido] -phenyl} -amide of acid [1, 2, 3] thiadiazole-4-carboxylic acid 450 399. { 4- [3- (3-isopropyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 451 380. { 4- [3- (3-isopropyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 452 409 2-Fluoro-N-. { 4- [3- (3-isopropyl-phenyl) -thioureido] -phenyl} -benzamide 453 381. { 4- [3- (3-cyano-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 454 410 N-. { 4- [3- (3-Dimethylamino-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 455 381. { 4- [3- (3-dimethylamino-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 456 370 [1,2,3-thiadiazole-4-carboxylic acid 4- (3-m-tolyl-thioureido) -phenyl] -amide 457 424. { 4- [3- (3-trifluoromethyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 458 479 N-. { 3-Chloro-4- [3- (5-chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 459 449 N-. { 3-Chloro-4- [3- (3-chloro-4-methyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 460 481 N-. { 3-Chloro-4- [3- (3-chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 461 391 N-. { 4- [3- (3-Cyano-phenyl) -thioureido] -phenyl} -2-fluorobenzamide 462 395. { 4- [3- (3-acetylamino-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 463 424 2-Fluoro-N-. { 4- [3- (3-hydrazinocarbonyl-phenyl) -thioureido] -phenyl} -benzamide 464-400 (4-. {3- [3- (1-hydroxy-ethyl) -phenyl] -thioureido}. phenyl) - [1,2,3] thiadiazole-4-carboxylic acid amide 465 434 N-. { 4- [3- (2-Amino-3-chloro-phenyl) -thioureido] -phenyl} - 2,6-difluoro-benzamide 466 406. { 4- [3- (3-Amino-5-chloro-phenyl) -thioureido] -phenyl} - [1, 2, 3] -thiadiazole-4-carboxylic acid amide 467 398. { 4- [3- (3, 5-Dimethoxy-phenyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 468 416. { 4- [3- (3, 5-Dimethoxy-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 469 454 5- (3. {4- [(furan-2-carbonyl) -amino] -phenyl-thioureido) -isophthalic acid dimethyl ester 470 434. { 4- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} isoxazole-5-carboxylic acid amide 471 392. { 4- [3- (6-chloro-pyridin-3-yl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 472 382 (4-. {3- [3- (l-hydroxy-ethyl) -phenyl] -thioureido}. phenyl) -amide furan-2-carboxylic acid 473 368. { 4- [3- (3-Methoxy-phenyl) -thioureido] -phenyl] -amide of furan-2-carboxylic acid 474 354. { 4- [3- (3-Hydroxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 475 382 2-Fluoro-. { 4- [3- (3-hydroxy-phenyl) -thioureido] -phenyl} - benzamide 476 396 2-Fluoro-N-. { 4- [3- (3-hydroxymethyl-phenyl) -thioureido] -phenyl} -benzamide 477 423 N-. { 4- [3- (3-Acetylamino-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 478 413. { 4- [3- (3-Acetylamino-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 479 400. { 4- [3- (3-Dimethylamino-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 480 340 [4- (3-pyrimidin-4-yl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 481 378. { 4- [3- (lH-indazol-5-yl) -thioureido] -phenyl} Furan-2-carboxylic acid amide 482 395 [4- (3-benzothiazol-5-yl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 483 406 2-Fluoro-N-. { 4- [3- (lH-indazol-5-yl) -thioureido] -phenyl} -benzamide 484 424 N- [4- (3-Benzothiazol-5-yl-thioureido) -phenyl] -2-fluoro-benzamide 485 473 Dimethylester of 5- (3- {4- [([1, 2]} , 3] thiadiazole-4-carbonyl) -amino] -phenyl.}. -thioureido) -isophthalic acid 486 442 (4-. {3- [4- (l-Azido-ethyl) -3-chloro-phenyl] - thoureido.} - phenyl) -amide of furan-2-carboxylic acid 487 396 3-Fluoro-N-. { 4- [3- (3-methoxy-phenyl) -thioureido] -phenyl} -benzamide 488 368. { 4- [3- (3-Hydroxymethyl-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 489 416. { 4- [3- (5-Chloro-2-dimethylamino-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 490 444 N-. { 4- [3- (5-Chloro-2-dimethylamino-phenyl) -thioureido] -phenyl} -2-fluorobenzamide 491 506 [3-Chloro-5- (3- {4- [([1, 2, 3] -thiadiazole-4-carbonyl) -amino] -phenyl} -trial-butyl ester. -tioureido) phenyl] -carbamic 492-470 N- (4-. {3- [4- (l-Azido-ethyl) -3-chloro-phenyl] -thioureido}. phenyl) -2-fluoro-benzamide 493 337 [4- (1H-thiazolo [5.4-b] pyridin-2-ylidenamino) -phenyl] -amide of furan-2-carboxylic acid 494 378. { 4- [3- (lH-benzoimidazol-5-yl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 495 392. { 4- [3- (2-Methyl-lH-benzoimidazol-5-yl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 496 406 N-. { 4- [3- (lH-Benzoimidazol-5-yl) -thioureido] -phenyl} - 2-fluoro-benzamide 497 420 2-Fluoro-N-. { 4- [3- (2-methyl-lH-benzoimidazol-5-yl) -thioureido] -phenyl} -benzamide 498 452. { 5- [3- (5-Chloro-2, 4-dimethoxy-phenyl) -thioureido] -pyridin-2-yl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 499 445. { 5- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-2-yl} -pyridine-2-carboxylic acid amide 500 434. { 4- [3- (5-Chloro-2-dimethylamino-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 501 484 (4-. {3- [4- (2-Amino-pyrimidin-4-yl) -3-chloro-phenyl] -thioureido} -phenyl) -amide of acid [1, 2, 3] thiadiazole-4-carboxylic acid 502-494 N- (4-. {3- [4- (2-Amino-pyrimidin-4-yl) -3-chloro-phenyl] -thioureido} - phenyl) -2-fluoro -benzamide 03 434. { 4- [3- (3-Chloro-2-dimethylamino-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 504 462 N-. { 4- [3- (3-Chloro-2-dimethylamino-phenyl) -thioureido] -phenyl} -2,6-difluoro-benzamide 505 416. { 4- [3- (3-Chloro-2-dimethylamino-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 506 445. { 6- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-3-yl} -pyridine-2-carboxylic acid amide 507 462 N-. { 6- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-3-yl} -2-fluoro-benzamide 508 482. { 4- [3- (3-Iodo-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 509 413. { 4- [3- (3-tert-Butyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 510 387. { 4- [3- (3-Chloro-benzyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 511 415 N-. { 4- [3- (3-Chloro-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 512 434. { 6- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-3-yl} -furan-2-carboxylic acid amide 513 435. { 4- [3- (3-Bromo-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 514 452. { 6- [3- (5-Chloro-2,4-dimethoxy-phenyl) -thioureido] -pyridin-3-yl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 515 426. { 5- [3- (3,5-Dichloro-phenyl) -thioureido] -pyridin-2-yl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 516 474. { 4- [3- (3, 5-bis-Trifluoromethyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 517 502 N-. { 4- [3- (3, 5-Bis-trifluoromethyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 518 450 N-. { 4- [3- (4-Amino-3,5-dichloro-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 519 539 N-. { 4- [3- (4-Amino-3,5-dibromo-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 520 392. { 4- [3- (5-Chloro-pyridin-3-yl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 521 529. { 4- [3- (4-Amino-3,5-dibromo-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 522 434. { 4- [3- (3-Chloro-5-dimethylamino-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 523 444 N-. { 4- [3- (3-Chloro-5-dimethylamino-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 524 416. { 4- [3- (3-Chloro-5-dimethylamino-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 525 436. { 4- [3- (5-Bromo-pyridin-3-yl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 526 379. { 4- [3- (lH-Benzotriazol-5-yl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 527 425 N-. { 4- [3- (lH-Benzotriazol-5-yl) -thioureido] -phenyl} - 2,6-difluoro-benzamide 528 388 N- [4- ( { [2- (3-Chloro-phenyl) -hydrazino] -thioxomethyl] -.-amino) -phenyl] -furan-2-carboxamide 529 416 N- [4- ( { [2- (3-Chloro-phenyl) -hydrazino] -thioxomethyl] -.-amino) -phenyl] -2-fluoro-benzamide 530 456. { 4- [3- (2-Amino-3-chloro-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 531 513 N-. { 4- [3- (3-Bromo-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 532 503. { 4- [3- (3-Bromo-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 533 374 0- (3-chloro-phenyl) acid ester. { 4- [(Furan-2-carbonyl) -amino] -phenyl} -thiocarbamic 534 474. { 4- [3- (2-Amino-3-chloro-5-trifluoromethyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 535 508. { 4- [3- (3-Piperidin-1-yl-5-trifluoromethyl-phenyl) -thioureido] -phenyl} [1, 2, 3] thiadiazole-4-carboxylic acid amide 536 380 N- [4- (3-Benzyl-thioureido) -phenyl] -2-fluoro-benzamide 537 439. { 4- [3- (3,4-Dichloro-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 538 449 N-. { 4- [3- (3,4-Dichloro-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 539 370 [1,2,3] thiadiazole-4-carboxylic acid [4- (3-benzyl-thioureido) -phenyl] -amide] 540 424 N- [4- (3-Benzo [l] , 3] dioxol-5-ylmethyl-thioureido) -phenyl] -2-fluoro-benzamide 541 414 [4- (3-Benzo [l, 3] dioxol-5-ylmethyl-thioureido) -phenyl] -amide of acid [ 1, 2, 3] thiadiazole-4-carboxylic acid 542 506. { 4- [3- (3, 5-bis-trifluoromethyl-benzyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 543 516 N-. { 4- [3- (3, 5-Bis-trifluoromethyl-benzyl) -thioureido] -phenyl} -2-Fluoro-benzamide 544 352 [4- (3-Benzyl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 545 421. { 4- [3- (3,4-Dichloro-benzyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 546 396 [4- (3-Benzo [l, 3] dioxol-5-ylmethyl-thioureido) -phenyl] -furan-2-carboxylic acid amide 547 488. { 4- [3- (3, 5-Bis-trifluoromethyl-benzyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 548 503. { 4- [3- (4-Bromo-3-trifluoromethyl-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 549 529 N-. { 4- [3- (3-Bromo-4-trifluoromethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 550 519. { 4- [3- (3-Bromo-4-trifluoromethoxy-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 551 473. { 4- [3- (3-Chloro-4-trifluoromethylsulfanyl-phenyD-thioureido] -phenyl} -amide of furan-2-carboxylic acid 552 412 2-Fluoro-N- (4-. {3- [2] - (3-fluoro-phenyl) -ethyl] -thioureido.}.-Phenyl) -benzamide 553 412 2-Fluoro-N- (4- { 3- [2- (4-fluoro-phenyl) -ethyl] - thioureido.}. phenyl) -benzamide 554 402 (4-. {3- [2- (3-Fluoro-phenyl) -ethyl] -thioureido}. phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 555 402 (4-. {3- [2- (4-Fluoro-phenyl) -ethyl] -thioureido}. Phenyl) -amide [1,2,3] thiadiazole 4-carboxylic acid 556 495 (4-. {3- [3- (2-Methyl-butyl) -5-trifluoromethyl-phenyl] -thioureido}. Phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 557 481. {4- [3- (3-Isobutyl-5-trifluoromethyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-aminide. -carboxylic acid 558 523 (4-. {3- [3- (4-Methyl-piperazin-1-yl) -5-trifluoromethyl-phenyl] -thioureido} -phenyl) -amide [1] 2,3] thiadiazole-4-carboxylic acid 559 510 { 4- [3- (3-Morpholin-4-yl-5-tr ifluoromethyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 560 494. { 4- [3- (3-Pyrrolidin-1-yl-5-trifluoromethyl-phenyl) -thioureido] -phenyl} [1, 2, 3] thiadiazole-4-carboxylic acid amide 561 384 (4-. {3- [2- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -amide furan-2-carboxylic acid 562 419 (4- { 3- [2- (3-Chloro-phenyl) -ethyl] -thioureido}. phenyl) -amide [1,2,3] thiadiazole- 4-carboxylic 563 429 (4- { 3- [2- (3-Chloro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 564 401 (4-. {3- 3- 2- Furan-2-carboxylic acid (3-chloro-phenyl) -ethyl] -thioureido.} - phenyl) -amide 565-402 (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) - [1, 2, 3] thiadiazole-4-carboxylic acid amide 566 504 2-Fluoro-N-. { 4- [3- (3-pyrrolidin-1-yl-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 567 477 N-. { 4- [3- (3-Dimethylamino-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 568 520 2-Fluoro-N-. { 4- [3- (3-morpholin-4-yl-5-trifluoromethylphenyl) -thioureido] -phenyl} -benzamide 569 533 2-Fluoro-N- (4-. {3- [3- (4-methyl-piperazin-1-yl) -5- trifluoromethyl-phenyl] -thioureido} -phenyl) -benzamide 570 518 2-Fluoro-N-. { 4- [3- (3-piperidin-l-yl-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 571 468. { 4- [3- (3-Dimethylamino-5-trifluoromethyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 572 405. { 4- [3- (3-Chloro-benzyl) -thioureido] -phenyl} -amide, of [1,2,3] thiadiazole-4-carboxylic acid 573 384 (4-. {3- [2- (3-Fluoro-phenyl) -ethyl] -thioureido} -phenyl) -amide of furan-2-carboxylic acid 574 366 [4- (3-phenethyl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 575 384 [4- (3-phenethyl-thioureido) -phenyl] -amide of acid [1,2,3] thiadiazole-4-carboxylic acid 576 394 2-Fluoro-N- [4- (3-phenethyl-thioureido) -phenyl] -benzamide 577 505 2-Fluoro-N- (4-. {3 - [3- (2-methyl-butyl) -5- trifluoromethyl-phenyl] -thioureido.} - phenyl) -benzamide 578 491 2-Fluoro-N-. { 4- [3- (3-isobutyl-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 579 388. { 4- [3- (3, 5-difluoro-benzyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 580 416 N-. { 4- [3- (3,5-Difluoro-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 581 406. { 4- [3- (3, 5-Difluoro-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 582 421. { 4- [3- (3, 5-Dichloro-benzyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 583 449 N-. { 4- [3- (3, 5-Dichloro-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 584 439. { 4- [3- (3, 5-Dichloro-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 585 438. { 4- [3- (3-Fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 586 466 2-Fluoro-N-. { 4- [3- (3-fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl} -benzamide 587 456. { 4- [3- (3-Fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 588 384. { 4- [3- (1-Phenyl-ethyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acidamide 589 394 2-Fluoro-N-. { 4- [3- (1-phenyl-ethyl) -thioureido] -phenyl] -benzamide 590 366. { 4- [3- (1-Phenyl-ethyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 591 412 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido}. phenyl) -benzamide 592 384 (4- {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -phenyl) -amide of furan-2-carboxylic acid 593 413 N-. { 4- [3- (l-tert-Butyl-lH-imidazol-2-yl) -thioureido] -phenyl} -2-fluoro-benzamide 594 510 (4-. {3- [3- (Isobutyl-methyl-amino) -5-trifluoromethylphenyl] -thioureido] -phenyl} -amide [1,2,3] thiadiazole-4-carboxylic acid 595 510 (4-. {3- [3- (3-Hydroxy-pyrrolidin-1-yl) -5-trifluoromethyl-phenyl] -thioureido} -phenyl) -amide of acid [1,2,3] thiadiazole-4-carboxylic acid 596 520 2-Fluoro-N- (4-. {3- [3- (isobutyl-methyl-amino) -trifluoromethyl-phenyl] -thioureido} -phenyl ) -benzamide 597 510 (4-. {3- [3- (Butyl-methyl-amino) -5-trifluoromethylphenyl] -thioureido}. phenyl) -amide [1,2,3] thiadiazole-4-aminide -carboxylic 598 520 N- (4-. {3- [3- (Butyl-methyl-amino) -5-trifluoromethyl-phenyl] -thioureido}. phenyl) -2-fluoro-benzamide 599 520 (4- {[3- [2- (3,5-bis-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide [1,2,3] thiadiazole-4-carboxylic acid 600 442. { [L, 2,3] thiadiazole-4-carboxylic acid 4- [3- (4-fluoro-3-trifluoromethyl-phenyl) -thioureido] -phenyl] -amide; 601 522. { 4- [3- (4-Piperidin-1-yl-3-trifluoromethyl-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 602 482. { 4- [3- (4-Dimethylamino-3-trifluoromethyl-benzyl) -thioureido] -phenyl} [1, 2, 3] thiadiazole-4-carboxylic acid amide 603 381 (4-. {3- [2- (4-Amino-phenyl) -ethyl] -thioureido.} - phenyl) -amide furan-2-carboxylic acid 604 445 (4- { 3- [2- (4-Bromo-phenyl) -ethyl] -thioureido.}. phenyl) -furan-2-carboxylic acid amide 605 380. { 4- [3- (2-p-Tolyl-ethyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 606 463 (4-. {3- [2- (4-Bromo-phenyl) -ethyl] -thioureido}. phenyl) -amide [1, 2, 3] ] thiadiazole-4-carboxylic acid 607 396 (4-. {3- [2- (3-Methoxy-phenyl) -ethyl] -thioureido} -phenyl) -furan-2-carboxylic acid amide 608 403. { 4- [3- (l-tert-Butyl-lH-imidazol-2-yl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 609 384. { 4- [3- (l-tert-Butyl-lH-imidazol-2-yl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 610 492 N-. { 4- [3- (4-Dimethylamino-3-trifluoromethyl-benzyl) -thioureido] -phenyl} -2-Fluoro-benzamide 611 427 (4-. {3- [2- (3,4-Dimethoxy-phenyl) -ethyl] -thioureido} - phenyl) -amide of furan-2-carboxylic acid 612 380 . { 4- [3- (3-Phenyl-propyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 613 399 (4- [3- (3-phenyl-propyl) -thioureido] -phenyl} -amide of [1,2,3] thiadiazole-4-carboxylic acid 614 502 (4- {3- [2- (3,5-bis-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide of furan-2-carboxylic acid 615 550. { 4- [3- (4-Iodo-3-trifluoromethyl-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 616 532 2-Fluoro-N-. { 4- [3- (4-piperidin-1-yl-3-trifluoromethyl-benzyl) -thioureido] -phenyl} -benzamide 617 537 (4- {3- [4- (4-Methyl-piperazin-1-yl) -3-trifluoromethyl-benzyl] -thioureido} -phenyl) -amide [1,2,3] thiadiazole-4-carboxylic acid 618 482. { 4- [3- (3-Dimethylamino-5-trifluoromethyl-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 619 488. { 4- [3- (3, 5-bis-Trifluoromethyl-phenyl) -thioureido-methyl] -phenyl} -furan-2-carboxylic acid amide 620 421. { 4- [3- (3,5-Dichloro-phenyl) -thioureidomethyl] -phenyl} - furan-2-carboxylic acid amide 621 421. { 4- [3- (3,4-Dichloro-phenyl) -thioureidomethyl] -phenyl} - furan-2-carboxylic acid amide 622 455. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido-methyl] -phenyl} -furan-2-carboxylic acid amide 623 466 2-Fluoro-N-. { 4- [3- (4-fluoro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 624 456. { 4- [3- (4-Fluoro-3-trif "2-uoromethyl-benzyl) -thioureido] -phenyl] -amido [l, 2,3] thiadiazole-4-carboxylic acid. 625 410 2-Fluoro-N-. { 4- [3- (2-phenoxy-ethyl) -thioureido] -phenyl} - benzamide 626 382. { 4- [3- (2-Phenoxy-ethyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 627 400. { [1,2,3] thiadiazole-4-carboxylic acid [3- (2-phenoxy-ethyl) -thioureido] -phenyl] -amide of 628 409 2-Fluoro-N-. { 4- [3- (3-phenyl-propyl) -thioureido] -phenyl} -benzamide 629 425. { 4- [3- (5-Trifluoromethyl-pyridin-3-yl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 630 439. { 4- [3- (3, 4-Dichloro-phenyl) -thioureido-methyl] phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 631 473. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido-methyl] -phenyl} [1, 2, 3] thiadiazole-4-carboxylic acid amide 632 381 2-Fluoro-N- [4- (3-pyridin-3-ylmethyl-thioureido) -phenyl] -benzamide 633 353 [4- (3 Phenyl-3-ylmethyl-thioureido) -phenyl] -amide of furan-2-carboxylic acid 634 371 [4- (3-pyridin-3-ylmethyl-thioureido) -phenyl] -amide of acid [1,2,3 ] thiadiazole-4-carboxylic acid 635 439. { 4- [3- (3, 5-Dichloro-phenyl) -thioureido-methyl] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 636 492 N-. { 4- [3- (3-Dimethylamido-5-tri-loromethyl-benzyl) -thioureido] -phenyl} -2-fluoro-benzamide 637 415 (4- { 3- [2- (3-Methoxy-phenyl) ethyl] -thioureido}. Phenyl) -amide of [1, 2, 3] thiadiazole-4-amide -carboxylic 638 399. { 4- [3- (2-p-Tolyl-ethyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide 639 445 (4-. {3- [2- (3,4-Dimethoxy-phenyl) -ethyl] -thioureido} - phenyl) - acid amide [l, 2,3] thiadiazole-4-carboxylic acid 640 506. { 4- [3- (3, 5-bis-Trifluoromethyl-phenyl) -thioureido-methyl] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 641 516 N-. { 4- [3- (3, 5-Bis-trifluoromethyl-phenyl) -thioureido-methyl] -phenyl} -2-fluoro-benzamide 642 449 N-. { 4- [3- (3,5-Dichloro-phenyl) -thioureidomethyl] phenyl} - 2-fluoro-benzamide 643 449 N-. { 4- [3- (3, 4-Dichloro-phenyl) -thioureidomethyl] -phenyl} - 2-fluoro-benzamide 644 448. { 4- [3- (3-Acetylamino-5-chloro-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 645 453 (4- {3- [2- (3,4-Dichloro-phenyl) -ethyl] -thioureido} - phenyl) -amide of [1,2, 3] thiadiazole-4-carboxylic acid 646 413. { 4- [3- (1-Methyl-3-phenyl-propyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 647 463 (4-. {3- [1- (4-Bromo-phenyl) -ethyl] -thioureido.} - phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 648 413. { 4- [3- (4-Phenyl-butyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide 649 397 [1- (3-Indan-l-yl-thioureido) -phenyl] -amide [1,2,3] thiadiazole-4 -amide] carboxyl 650 400. { 4- [3- (2-Methoxy-benzyl) -thioureido] -phenyl} [1, 2, 3] thiadiazole-4-carboxylic acid amide 651 415 (4-. {3- [2- (2-Methoxy-phenyl) -ethyl] -thioureido.} - phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 652 415 (4-. {3- [2- (4-Methoxy-phenyl) -ethyl] -thioureido} -phenyl) -amide [1] , 2,3] thiadiazole-4-carboxylic acid 653 506 N- (4-. {3- [2- (3-Dimethylamino-5-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -2- fluoro-benzamide 654 510 (4-. {3- [3- (3-Dimethylamino-propyl) -5-trifluoromethyl-phenyl] -thioureido}. phenyl) -amide [1,2,3] - thiadiazole-4-carboxylic 655 417. { 4- [3- (2-Phenylsulfanyl-ethyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 656 427 2-Fluoro-N-. { 4- [3- (2-phenylsulfanyl-ethyl) -thioureido] -phenyl} -benzamide 657 399. { 4- [3- (2-Phenylsulfanyl-ethyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 658 381 2-Fluoro-N- [4- (3-pyridin-4-ylmethyl-thioureido) -phenyl] -benzamide 659 353 [4- (3-pyridin-4-ylmethyl- thoureido) -phenyl] -amide of furan-2-carboxylic acid 660 371 [4- (3-pyridin-4-ylmethyl-thioureido) -phenyl] -amide of [1,2,3] thiadiazole-4-carboxylic acid 661 506 2-Fluoro-N-. { 4- [3- (3-iodo-benzyl) -thioureido] -phenyl} - benzamide 662 478. { 4- [3- (3-Yodo-benzyl) -thioureido] -phenyl-2-furan-2-carboxylic acid 663 496. { 4- [3- (3-Iodo-benzyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide 664 479 N- (4-. {3- [2- (3,5-Dichloro-phenoxy) -ethyl] -thioureido} - phenyl ) -2-fluoro-benzamide 665 451 (4- {3- [2- (3,5-Dichloro-phenoxy) -ethyl] -thioureido} - phenyl) -amide of furan-2-carboxylic acid 666 445 N- (4- { 3- [2- (3-Chloro-phenoxy) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 667 417 (4- { 3- [2 - (3-Chloro-phenoxy) -ethyl] -thioureido.} - phenyl) - furan-2-carboxylic acid amide 668 435 (4-. {3- [2- (3-Chloro-phenoxy) -ethyl) ] -thioureido.} - phenyl) - [1,2,3] thiadiazole-4-carboxylic acid amide 669 466 2-Fluoro-N-. { 4- [3- (2-Fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl} -benzamide 670 438. { 4- [3- (2-Fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl} furan-2-carboxylic acid amide 671 456 (4- [3- (2-Fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl] -amide of [l, 2,3] thiadiazole-4 -amide. -carboxylic 672 416 N- { 4- [3- (3, 4-Difluoro-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 673 452 N- (4-. {3- 3- 2- (4-Dimethylamino-3-methyl-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 674 496 (4-. {3- [2- (3-Dimethylamino-5- [1,2,3] thiadiazole-4-carboxylic acid trifluoromethyl-phenyl) -ethyl] -thioureido.] - phenyl) -amide [6,38] 388 { 4- [3- (3,4-difluoro-benzyl)] -thioureido] -phenyl.} - furan-2-carboxylic acid amide 676 406. {4- [3- (3, 4-Difluoro-benzyl) -thioureido] -phenyl} -amide [1] 2, 3] thiadiazole-4-carboxylic acid 677 433 N-. {4- [3- (3-Chloro-4-fluoro-benzyl) -thioureido] -phenyl} -2-fluoro-benzamide 678 495 ( 4- [3- (2- (3-Bromo-phenylsulfanyl) -ethyl] -thioureido.} - phenyl) -amide of [1,2, 3] thiadiazole-4-carboxylic acid 679 477 (4- { 3- [2- (3-Bromo-phenylsulfanyl) -ethyl) ] -tioureido} phenyl) -amide of furan-2-carboxylic acid 680 505 N- (4-. {3- [2- (3-Bromo-phenylsulfanyl) -ethyl] -thioureido} -phenyl) -2-f luoro -benzamide 681 493 (4-. {3- [2- (3-Bromo-4-methoxy-phenyl) -ethyl] -thioureido.} - phenyl) -amide of [1,2, 3] thiadiazole- 4-carboxylic 682 493 (4-. {[3- [2- (5-Bromo-2-methoxy-phenyl) -ethyl] -thioureido} - phenyl) -amide of [1,2,3] thiadiazole-4 -amide carboxylic 683 419 (4- {3- [2- (2-Chloro-phenyl) -ethyl] -thioureido} -phenyl) -amide [1,2,3] thiadiazole-4-carboxylic acid 684 402 ( 4- [{3- [2- (2-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) - [1, 2,3] thiadiazole-4-carboxylic acid amide 685 419 (4-. [1, 2, 3] thiadiazole-4-carboxylic acid {4 - (4-chloro-phenyl) -ethyl] -thioureido} -phenyl) -amide 475. { 4- [3- (3, 3-Diphenyl-propyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 687 547 2-Fluoro-N- (4-. {3- [4- (4-methyl-piperazin-1-yl) -3-trifluoromethyl) -benzyl] -thioureido.}.-phenyl) -benzamide 688 469 (4- ({3- [2- (3,5-Dichloro-phenoxy) -ethyl] -thioureido} [phenyl] -amide of [1,2, 3] thiadiazole-4-carboxylic acid 689 423 { 4- [3- (3-Chloro-4-fluoro-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 690 427. { 4- [3- (4-tert-Butyl-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 691 399. { 4- [3- (3, 5-Dimethyl-benzyl) -thioureido] -phenyl} [1, 2,3] thiadiazole-4-carboxylic acid amide 692 442 (4-. {3- [2- (4-Dimethylamino-3-methyl-phenyl) -ethyl] -thioureido} -phenyl ) - [1, 2, 3] thiadiazole-4-carboxylic acid amide 693 479 (4-. {3- [2- (4-Bromo-phenoxy) -ethyl] -thioureido} -phenyl) -amide of [1, 2, 3] thiadiazole-4-carboxylic acid 694 526 (4-. {3- [2- (4-Yodo-phenoxy) -ethyl] -thioureido} -phenyl) -amide of [ 1, 2, 3] thiadiazole-4-carboxylic acid 695 489 N- (4-. {3- [2- (4-Bromo-phenoxy) -ethyl] -thioureido} - phenyl) -2-fluoro-benzamide 696 536 2-Fluoro- (4- { 3- [2- (4-Yodo-phenoxy) -ethyl] -thioureido.} - phenyl) -benzamide 697 461 (4- { 3- [2- Furan-2-carboxylic acid (4-Bromo-phenoxy) -ethyl] -thioureido.} - phenyl) -amide 2,48-508 (4-. {3- [2- (4-Yodo-phenoxy) -ethyl] -thioureido.} - phenyl) - furan-2-carboxylic acid amide 699 408. { 4- [3- (3,4-Dichloro-phenyl) -thioureido] -phenyl} oxazole-4-carboxylic acid amide 700 424. { 4- [3- (3,5-Dichloro-phenyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 701 491. { 4- [3- (3, 5-bis-Trifluoromethyl-phenyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 702 408. { 4- [3- (3, 5-Dichloro-phenyl) -thioureido] -phenyl} oxazole-4-carboxylic acidamide 703 469 (4-. {3- [2- (3,4-Dichloro-phenoxy) -ethyl] -thioureido} - phenyl) -amide [1, 2] , 3] thiadiazole-4-carboxylic acid 704 424. { 4- [3- (3,4-Dichloro-phenyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 705 458. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 706 400. { 4- [3- (2-Phenylamino-ethyl) -thioureido] -phenyl} [1, 2, 3] thiadiazole-4-carboxylic acid amide 707 453 (4-. {3- [2- (2,4-Dichloro-phenyl) -ethyl] -thioureido} - phenyl) - [1,2,3] thiadiazole-4-carboxylic acid amide 708 452 (4-. {3- [2- (3-trifluoromethyl-phenyl) -ethyl] -thioureido} - phenyl) -amide of acid [1,2,3] thiadiazole-4-carboxylic acid 709 453 (4- {3- [2- (2,6-Dichloro-phenyl) -ethyl] -thioureido} - phenyl) -amide of [1,2, 3] thiadiazole-4-carboxylic acid 710 485 (4- {3- [2- (3,4-Dichloro-phenylsulfanyl) -ethyl] -thioureido} -phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 711 503 (4-. {[3- [2- (2-Fluoro-5-trifluoromethyl-phenylsulfanyl) -ethyl] -thioureido} -phenyl) -amide of [1,2,3] -thiadiazole-4 -amide carboxylic 712 668 N- (4-. {3- [3-Chloro-5- (3- {4- [([1,2,3] thiadiazole-4-carbonyl) -amino] -phenyl} .-thioureido) -phenyl] -thioureido.}. -phenyl) - [1,2,3] thiadiazole-4-carboxamide 713 413 (4-. {3- [2- (4-Ethyl-phenyl) -ethyl] -thioureido} -phenyl) - [1, 2, 3] thiadiazole-4-carboxylic acid amide 714 442. { 4- [3- (4-Chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} oxazole-4-carboxylic acid amide 715 475. { 4- [3- (3, 5-bis-Trifluoromethyl-phenyl) -thioureido] -phenyl} Oxazole-4-carboxylic acid amide 716 420 (4-. {3- [2- (3,4-Difluoro-phenyl) -ethyl] -thioureido} - phenyl) -amide [1, 2] , 3] thiadiazole-4-carboxylic acid 717 452 (4- {3- [2- (4-Trifluoromethyl-phenyl) -ethyl] -thioureido} - phenyl) -amide of [1,2, 3] thiadiazole-4-carboxylic acid 718 435 (4- {3- [2- (3,4-Dichloro-phenyl) -ethyl] -thioureido} - phenyl) -amide of furan-2-carboxylic acid 719 463 N- (4- {3- [2- (3,4-Dichloro-phenyl) -ethyl] -thioureido} - phenyl) -2-fluoro-benzamide 720 420 (4-. {3- [2- (3.5 -Difluoro-phenyl) -ethyl] -thioureido.] [L, 2, 3] thiadiazole-4-carboxylic acid 721 412 2-fluoro-N- (4-. {3- 3 - (2-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -benzamide 722 429 (4-. {3- [2- (4-Nitro-phenyl) -ethyl] -thioureido} - phenyl) - [1, 2, 3] thiadiazole-4-carboxylic acid amide 723 399. { 4- [3- (1-Methyl-2-phenyl-ethyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 724 437 N-. { 4- [3- (4-tert-Butyl-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 725 409 N-. { 4- [3- (3,5-Dimethyl-benzyl) -thioureido] -phenyl} -2- fluoro-benzamide 726 400. { 4- [3- (2-Hydroxy-1-phenyl-ethyl) -thioureido] -phenyl} - acid amide [1, 2,3] thiadiazole-4-carboxylic acid 727 409 2-Fluoro-N-. { 4- [3- (1-methyl-l-phenyl-ethyl) -thioureido] -phenyl} -benzamide 728 399. { 4- [3- (1-Methyl-l-phenyl-ethyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 729 405. { 4- [3- (2-Chloro-benzyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 730 388. { 4- [3- (2-Fluoro-benzyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 731 438. { 4- [3- (3-Trifluoromethyl-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 732 388. { 4- [3- (3-Fluoro-benzyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide 733 435 (4-. {3- [2- (2-Chloro-phenoxy) -ethyl] -thioureido.} - phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 734 479 (4-. {3- [2- (3-Bromo-phenoxy) -ethyl] -thioureido} -phenyl) -amide [1] , 2,3] thiadiazole-4-carboxylic acid 735 418 (4-. {3- [2- (2-Fluoro-phenoxy) -ethyl] -thioureido}. Phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 736 418 (4-. {3- [2- (3-Fluoro-phenoxy) -ethyl] -thioureido}. Phenyl) -amide [1, 2, 3] thiadiazole 4-carboxylic acid 737 486 (4-. {3- [2- (2-Fluoro-5-trifluoromethyl-phenoxy) -ethyl] -thioureido} -phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 738 384 (4-. {3- [2- (2-Fluoro-phenyl) -ethyl] -thioureido}. phenyl) -furan-2-carboxylic acid amide 739 435. { [1,2,3] thiadiazole-4-carboxylic acid [3- (4-bromo-phenyl) -thioureido] -phenyl] -amide 740 374. { 4- [3- (4-Fluoro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 741 388. { 4- [3- (4-Fluoro-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 742 405. { 4- [3- (4-Chloro-benzyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 743 449. { 4- [3- (4-Bromo-benzyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 744 332 N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) - acetamide 745 438. { 4- [3- (3,4-Dichloro-benzyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 746 455. { 4- [3- (2-Fluoro-5-trifluoromethyl-benzyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 747 426. { 4- [3- (4-tert-Butyl-benzyl) -thioureido] -phenyl} thiazole-4-carboxylic acid amide 748 374. { 4- [3- (2-Fluoro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 749 374. { 4- [3- (3-Fluoro-phenyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide 750 526 (4-. {3- [2- (3-Yodo-phenoxy) -ethyl] -thioureido.} - phenyl) -amide [1, 2,3] thiadiazole-4-carboxylic acid 751 409 N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -2-phenyl -acetamide 752-425 N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -2-methoxy-benzamide 753 425 N- (4-. { 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.]. - phenyl) -3-methoxy-benzamide 754 425 N- (4-. {3- [1- (4-Fluoro- phenyl) -ethyl] -thioureido.]. - phenyl) -4-methoxy-benzamide 755 429 2-Chloro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido .}.-phenyl) -benzamide 756 429 2-Chloro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -phenyl) -benzamide 757 453 4 - (4- { 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenylcarbamoyl) -phenylester of acetic acid 758 394 N- (4-. {3- 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -benzamide 759 395 N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido}. - phenyl) -isonicotinamide to 760 410 N- (4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -4-hydroxy-benzamide 761 429 3-Chloro-N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido}. phenyl) -benzamide 762 470 (4- {3- [2- (3-Fluoro-5-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide [1, 2,3] thiadiazole-4-carboxylic acid 763 520 [4- ({3- [2- (2,4-bis-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 764 470 (4-. {[3- [2- (4-Fluoro-3-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide [1, 2, 3] thiadiazole-4- carboxylic acid 765 438 4-Dimethylamino-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} - phenyl) -benzamide 766 470 (4-. {3- [2- (2-Fluoro-3-trifluoromethyl-phenyl) -ethyl] -thioureido.]. Phenyl) -amide [1, 2], 3] thiadiazole-4-carboxylic acid 767 470 (4-. {3- [2- (2-Fluoro-5-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide [1] 2,3] thiadiazole-4-carboxylic acid 768 510 (4-. {3- [2- (3-Yodo-phenyl) -ethyl] -thioureido} -phenyl) -amide [1, 2, 3] ] thiadiazole-4-carboxylic acid 769 470 (4-. {3- [2- (4-Fluoro-2-trifluoromethyl-phenyl) -ethyl] -thioureido} -phenyl) -amide [1, 2, 3] thiadiazole-4-carboxylic acid 770- 463 (4-. {3- [2- (3-Bromo-phenyl) -ethyl] -thioureido} - phenyl) - [1, 2, 3] thiadiazole acid 4-carboxylic acid 771 427 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -propyl] -thioureido} -phenyl) -benzamide 772 475 2-Fluoro-N - (4- { 3- [(4-fluoro-phenyl) -phenyl-methyl] -thioureido.} - phenyl) -benzamide 773 455 2-Fluoro-N- (4-. {3- 3- [1 - (4-fluoro-phenyl) -pentyl] -thioureido.}.-Phenyl) -benzamide 774 489 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -2- phenyl-ethyl] -thioureido.} - phenyl) -benzamide 775 409 2-Fluoro-N-. { 4- [3- (l-o-tolyl-ethyl) -thioureido] -phenyl} -benzamide 776 409 2-Fluoro-N-. { 4- [3- (l-m-tolyl-ethyl) -thioureido] -phenyl} -benzamide 777 425 2-Fluoro-N- (4-. {3- [l- (4-methoxy-phenyl) -ethyl] -thioureido}. -phenyl) -benzamide 778 412 2-Fluoro-N- ( 4- { 3- [1- (2-fluoro-phenyl) -ethyl] -thioureido.}.-Phenyl) -benzamide 779 429 N- (4-. {3- [l- (3-chloro- phenyl) -ethyl] -thioureido.}. phenyl) -2-fluoro-benzamide 780 473 N- (4-. {3- [l- (3-Bromo-phenyl) -ethyl] -thioureido} - phenyl) -2-fluoro-benzamide 781 429 N- (4-. {3- [l- (4-Chloro-phenyl) -ethyl] -thioureido.} - phenyl) 2-fluoro-benzamide 782 409 2-Fluoro-N-. { 4- [3- (1-p-tolyl-ethyl) -thioureido] -phenyl} -benzamide 783 473 N- (4-. {3- [1- (2-Bromo-phenyl) -ethyl] -thioureido.} - phenyl) 2-fluoro-benzamide 784 429 N- (4-. 3- [l- (2-Chloro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 785 462 2-Fluoro-N- (4-. {3- 3 [l- (2 -trifluoromethyl-phenyl) -ethyl] -thioureido.}. phenyl) -benzamide 786 462 2-Fluoro-N- (4-. {3- [1- (3-trifluoromethyl-phenyl) -ethyl] -thioureido}-phenyl) -benzamide 787 462 2-Fluoro-N- (4-. {3- [1- (4-trifluoromethyl-phenyl) -ethyl] -thioureido}. phenyl) -benzamide 788 425 2- Fluoro-N- (4-. {3- [1- (2-methoxy-phenyl) -ethyl] -thioureido}. -phenyl) -benzamide 789 425 2-Fluoro-N- (4- { 3 - [l- (3-methoxy-phenyl) -ethyl] -thioureido.}.-phenyl) -benzamide 790 441 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -2-methyl-propyl] -thioureido.}.-Phenyl) -benzamide 791 419 N- (4-. {3- [l- (3-Cyano-phenyl) -ethyl] -thioureido.} - phenyl) 2-fluoro-benzamide 792 419 N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido}. Phenyl) -2-fluoro-benzamide 793 438 N- ( 4- { 3- [l- (4-Dimethyla mino-phenyl) -ethyl] -thioureido} phenyl) -2-fluoro-benzamide 794 438 N- (4-. {3- [l- (3-Dimethylamino-phenyl) -ethyl] -thioureido} - phenyl) -2-fluoro-benzamide 795 473 2-Bromo-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -phenyl) -2-fluoro-benzamide 796 446 (4- { 3 - [1- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) - quinoline-2-carboxylic acid amide 797 410 2-Fluoro-N-. { 4- [3- (2-hydroxy-l-phenyl-ethyl) -thioureido] -phenyl} -benzamide 798 332 2-Fluoro-N- [4- (3-isopropyl-thioureido) -phenyl] -benzamide 799 445 2-Fluoro-N-. { 4- [3- (l-naphthalen-2-yl-ethyl) -thioureido] -phenyl} -benzamide 800 412 3-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl-thioureido}. phenyl) -benzamide 801 412 4-Fluoro-N- (4 - { 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -benzamide 802 384 2-Fluoro-N-. { 4- [3- (l-furan-2-yl-ethyl) -thioureido] -phenyl} -benzamide 803 395 2-Fluoro-N-. { 4- [3- (l-pyridin-2-yl-ethyl) -thioureido] -phenyl} -benzamide 804 397 2-Fluoro-N- (4-. {3- [l- (l-methyl-lH-pyrrol-2-yl) -ethyl] -thioureido}. -phenyl.}. -benzamide 805 401 2-Fluoro-N- { 4- [3- (l-thiophen-3-yl-ethyl) -thioureido] -phenyl} -benzamide 806 445 N- { 4- [3- (3 Chloro-4-ethoxy-phenyl) -thioureido] -phenyl.} - 2-fluoro-benzamide 807 459 N- { 4- [3- (3-Chloro-4-propoxy-phenyl) -thioureido] - phenyl.} -2-fluoro-benzamide 808 459 N- { 4- [3- (3-Chloro-4-isopropoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 809 473 N - { 4- [3- (4-Butoxy-3-chloro-phenyl) -thioureido] -phenyl.} - 2-fluoro-benzamide 810 522 2-Fluoro-N- { 4- [3- (3-iodo-4-methoxy-phenyl) -thioureido] -phenyl.}. -benzamide 811 475 N- { 4- [3- (3-Bromo-4-methoxy-phenyl) -thioureido] -phenyl} - 2-fluoro-benzamide 812 520 N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -2-iodo-benzamide 813 346 N - (4- { 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.}. - phenyl) -propionamide 814 286 N- [4- (3-phenyl-thioureido) -phenyl] - acetamide 1102 480 2-Fluoro-N- (4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -3-trifluoromethyl-phenyl) -benzamide 1103 574 (4-. {3- [(SS) -1- (4-bromo-phenyl) -ethyl] -thioureido} -2- trifluoromethyl-phenyl) -amide of isoquinoline-3-carboxylic acid 1104-498 N- (4-. {3- [(SS) -1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- cyano-phenyl) -2 -f luoro-benzamide 1105 498 N- (4- { 3- [(IR) -1- (4-Bromo-phenyl) -ethyl] -thioureido.} -2- cyano-phenyl) -2-f luoro-benzamida 1106 421 N-. { 2-Cyano-4- [( { [(1S) -1- (4-f-lorophenyl) ethyl] amino.} - carbonyl) amino] phenyl} -2-f luorobenzamide 1107 410 2-Fluoro-N-. { 4- [( { [(IR) -1- (4-f luorofenyl) ethyl] -amino.} Carbonyl) amino] -3-methylfenyl} -benzamide 1108 437 N-. { 4- [( { [(ÍS) -1- (4-f-lorophenyl) ethyl] amino.} - carbothiol) amino] -2-cyanophenyl} -2-fluorobenzamide 1109 453 N-. { 4- [( { [(ÍS) -1- (4-chlorophenyl) ethyl] amino.} - carbothiol) amino] -2-cyanophenyl} -2-f luorobenzamide.

EXAMPLE 815 (METHOD 32). { 4- [3- (2, 5 -Dichloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide To a solution of 2,5-dichloroaniline (0.16 g) in tetrahydrofuran (20 ml) was added freshly prepared 1,1'-thiocarbonyl-imidazole (0.20 g) and the mixture was stirred for about 30 minutes at room temperature. (4-amino-f-enyl) acid amide [1] was added, 2, 3] -thiadiazole-4-carboxylic acid (0.22 g) was added to the reaction flask and the mixture was stirred for approximately 6 hours. The solvent was then removed by evaporation under reduced pressure and hot acetonitrile (3 ml) was added. After 15 hours the mixture was filtered and the collected precipitate was washed with acetonitrile, then with diethyl ether, and dried with air to provide the desired product as a white powder. Using the above procedure and appropriate starting materials, the following compounds were prepared: EJ. M + H NAME OF COMPOUND NO. 816 321 N-. { 4- [3- (3-Chloro-f-enyl) -thioureido] -phenyl} -acetamide 817 413 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - benzamide 818 443 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - 2-methoxy-benzamide 819 443 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - 3-methoxy-benzamide 820 443 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - 4-methoxy-benzamide 821 431 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - 4-methoxy-benzamide 822 431 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - 3-fluoro-benzamide 823 431 N-. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} 4-fluoro-benzamide 824 437. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 825 511 Acid hexyl ester. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -carbamic 826 481. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} hexamic acid 827 505 N-. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 828 477. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 829 501 N-. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-methyl-benzamide 830 517 N-. { 4- [3- (5-Bromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -4-methoxy-benzamide 831 395 N-. { 4- [3- (5-Chloro-2-ethoxy-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 832 395 N-. { 4- [3- (5-Chloro-4-ethoxy-2-methoxy-phenyl) -thioureido] -phenyl} -acetamide 833 423 N-. { 4- [3- (2-Butoxy-5-chloro-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 834 423 N-. { 4- [3- (4-Butoxy-5-chloro-2-methoxy-phenyl) -thioureido] -phenyl} -acetamide 835 457 N-. { 4- [3- (2-Benzyloxy-5-chloro-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 836 457 N-. { 4- [3- (4-Benzyloxy-5-chloro-2-methoxy-phenyl) -thioureido] -phenyl} -acetamide 837 421. { 4- [3- (3-Chloro-4-methoxy-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 838 424 2-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-5-methoxy-phenoxy} -acetamide 839 367 N-. { 4- [3- (5-Chloro-2-hydroxy-4-methoxy-phenyl) -thioureido] -phenyl} -acetamide 840 367 N-. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} -acetamide 841 447 N-. { 4- [3- (3-Chloro-4- [methyl- (1-methyl-piperidin-4-yl) -amino] -phenyl] -thioureido) -phenyl] -acetamide 842 426 N- (4- { 3- [3-Chloro-4- (methyl-phenyl-amino) -phenyl] -thioureido}. -phenyl) -acetamide 843 509 N- [4- (3-. {4- [(1) Benzyl-pyrrolidin-3-yl) -methylamino] -3-chloro-phenyl] -thioureido) -phenyl] -acetamide 844-418 N- (4-. {3- [3-Chloro-4- (cyclopentyl-methyl-amino) -phenyl] -thioureido} -phenyl) -acetamide 845 433 N- [4- (3-. {3-Chloro-4- [methyl- (1-methyl-pyrrolidin-3-yl) -amino] -phenyl} -thioureido) -phenyl] -acetamide 846 419. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 847 447 N-. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 848 465 N-. { 4- [3- (3-Chloro-4-methylsulfanyl-phenyl) -thioureido] -phenyl} -2,6-difluoro-benzamide 849 445 N-. { 4- [3- (5-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 850 441 N-. { 4- [3- (5-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -2-methyl-benzamide 851 434. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 852 444 N-. { 4- [3- (3-Chloro-4-dimethylamino-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 853 517 [4- (3. {3-Chloro-4- [methyl- (1-methyl-piperidin-4-yl) -amino] -phenyl] -thioureido) -phenyl ] - [1,2,3] -thiadiazole-4-carboxylic acid amide 854 579 [4-. { 3-. { 4- [(1-benzyl-pyrrolidin-3-yl) -methyl-amino] -3-chloro-phenyl} -thioureido) -phenyl] -amido [1,2,3] -thiadiazole-4-carboxylic acid 855 527 N- [4- (3. {3-Chloro-4- [methyl- (1-methyl- piperidin-4-yl) -amino] -phenyl.}. -thioureido) -phenyl] -2-fluoro-benzamide 856 435. { 4- [3- (5-Chloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide 57 589 N- [4- (3-. {4- [(1-Benzyl-pyrrolidin-3-yl) -methyl-amino] -3] -chloro-phenyl.}. -thioureido) -phenyl] -2-fluoro-benzamide 858 501. { 4- [3- (5-Chloro-2, 4-dimethoxy-phenyl) -thioureido] -3-trifluoromethyl-phenyl} -furan-2-carboxylic acid amide 859 366 2-Fluoro-N- [4- (3-phenyl-thioureido) -phenyl] -benzamide 860 338 [4- (3-phenyl-thioureido) -phenyl] -amide furan-2-carboxylic acid 861 356 [1,2,3-thiadiazole-4-carboxylic acid [4- (3-phenyl-thioureido) -phenyl] -amide] 862 365 N- (4-. {3- 3- 3-Chloro-4- (l-hydroxy-ethyl) -phenyl] -thioureido.} - phenyl) -acetamide 863 435 (4-. {3- [3-Chloro-4- (l-hydroxy-ethyl)] phenyl] -thioureido.} - phenyl) -amide [l, 2,3] thiadiazole-4-carboxylic acid 864 365 N- (4-. {3- [3-Chloro-4- (2-hydroxy-ethyl) -phenyl] -thioureido}. -phenyl) -acetamide 865 445 N- (4- { 3 - [3-Chloro-4- (1-hydroxy-ethyl) -phenyl] -thioureido.} - phenyl) -2-fluoro-benzamide 866 417 (4-. {3- [3-Chloro-4- ( 1-hydroxy-ethyl) -phenyl] -thioureido.} - phenyl) -amide of furan-2-carboxylic acid 867 371. { 4- [3- (3-Amino-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 868 501. { 4- [3- (3-Bromo-4-trifluoromethoxy-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 869 423 N-. { 4- [3- (3-tert-Butyl-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 870 440. { 4- [3- (4-Chloro-3,5-dichloro-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 974 485 N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -phenyl} - 2-trifluoromethyl-benzamide 975 412 N- (4-Fluoro-phenyl) -4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -benzamide 976 446 (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido}. phenyl) -isoquinoline-1-carboxylic acid amide 977 468. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -phenyl} - isoquinoline-1-carboxylic acid amide 978 506 (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido.} - phenyl) - isoquinoline-1-carboxylic acid amide 979 453 (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido.} - phenyl) -isoquinoline-1-carboxylic acid amide 980 435 (4-. {3- 3- 1- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) - benzofuran-2-carboxylic acid amide 981 457. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -phenyl} - benzofuran-2-carboxylic acid amide 982 495 (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido.} - phenyl) - benzofuran-2-carboxylic acid amide 983 442 (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido.} - phenyl) -benzofuran-2-carboxylic acid amide 984 446 (4-. {3- [3- 1- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -isoquinoline-3-carboxylic acid amide 985 468. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -phenyl} - isoquinoline-3-carboxylic acid amide 986 453 (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido.} - phenyl) - isoquinoline-3-carboxylic acid amide 987 508 (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido.} - phenyl) - isoquinoline-3-carboxylic acid amide 988 446 (4-. {3- 3- Quinoline-3-carboxylic acid amide 989 446 (4-. {3- [l- (4-Fluoro-phenyl) - -] - (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) - quinoline-3-carboxylic acid amide ethyl] -thioureido.}. -phenyl) -quinoline-4-carboxylic acid amide 990 446 (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -phenyl) - quinoline-6-carboxylic acid amide 991 446 (4-. {3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -phenyl) -quinoline-8-carboxylic acid amide 992 462 N- (4-. {3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -2-trifluoromethyl-1-benzamide 993 419 2-Cyano-N- (4-. {3- (l- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -benzamide 994 473 N-. { 4- [3- (3-Chloro-4-isobutoxy-ethyl) -thioureido] -phenyl} -2-fluoro-benzamide 995 414 2-Fluoro-N-. { 4- [3- (3-fluoro-4-methoxy-phenyl) -thioureido] -phenyl} -benzamide 996 475 N- (4-. {3- [3-Chloro-4- (2-methoxy-ethoxy) -phenyl] -thioureido}. -phenyl) -2-fluoro-benzamide 997 398 2-Fluoro -N- { 4- [3- (3-fluoro-4-methyl-phenyl) -thioureido] -phenyl} -benzamide 998 464 2-Fluoro-N-. { 4- [3- (4-methoxy-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 999 449 N-. { 4- [3- (2-Amino-5-trifluoromethyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 1000 459 N- (4-. {3- [l- (3-Chloro-4-methoxy-phenyl) -ethyl] -thioureido}. Phenyl) -2-fluoro-benzamide 1001 417 N-. { 4- [3- (5-Chloro-2-hydroxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 1002 435 N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -phenyl} - 2-fluoro-benzamide 1003 448 2-Fluoro-N-. { 4- [3- (4-methyl-3-trifluoromethyl-phenyl) -thioureido] -phenyl} -benzamide 1004 473 (S) -N- (4-. {3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} - phenyl) -2-fluoro-benzamide 1005 473 N- ( 4- { 3- [(IR) -1- (4-Bromo-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 1006 494 2-Fluoro-N- (4-. {3- [2-methoxy-4- (2,2,2-trifluoro-ethoxy) -phenyl] -thioureido} -phenyl} -benzamide 1007 399 N-. {4- [3- ( 2-Amino-5-fluoro-phenyl) -thioureido] -phenyl.} - 2-fluoro-benzamide 1008 502 N- (4-. {3- [l- (4-Dimethylsulfamoyl-phenyl) -ethyl] - thioureido.}. phenyl) -2-fluoro-benzamide 1009 542 2-Fluoro-N- [4- (3. {l- [4-piperidin-1-sulfonyl) -phenyl] -ethyl.} - thioureido) -phenyl] -benzamide 1010 562 N- (4- { 3- [2, 4-Bis- (2,2,2-trifluoro-ethoxy) -phenyl] -thioureido} phenyl) -2-fluoro-benzamide 1011 409 2-Fluoro-N-. { 4- [3- ((SS) -1-p-tolyl-ethyl) -thioureido] -phenyl} -benzamide 1012 409 2-Fluoro-N-. { 4- [3- ((IR) -1-p-tolyl-ethyl) -thioureido] -phenyl} -benzamide 1013 394 2-Fluoro-N-. { 4- [3- ((lS) -l-phenyl-ethyl) -thioureido] -phenyl} -benzamide 1014 429 N- (4- { 3- [(IR) -1- (4-Chloro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 1015 429 N- ( 4- { 3- [(SS) -1- (4-Chloro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 1016 394 2-Fluoro-N-. { 4- [3- ((IR) -1-phenyl-phenyl) -thioureido] -phenyl} -benzamide 1017 432 N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} - phenyl) -2-methoxy-benzamide 1018 447 N-. { 4- [3- (l-Benzofuran-2-yl-ethyl) -thioureido] -phenyl) -2-methoxy-benzamide 1019 485 N- (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido.}.-phenyl) -2-methoxy-benzamide 1020 419 3-Cyano-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} phenyl) -benzamide 1021 462 N- (4-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} - phenyl) -4-trifluoromethyl-benzamide 1022 419 4-Cyan -N- (4- { 3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.}. -phenyl) -benzamide 1023 469 2-Fluoro-N- (4-. {3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2, 3, 5, 6-tetramethyl-phenyl) -benzamide 1024 480 N- (4-. {3- 3 [l - (4-Cyano-phenyl) -ethyl] -thioureido} -2,5-dimethoxy-phenyl) -2-fluoro-benzamide 1025 473 2-Fluoro-N- (4-. {3- 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -2,5-dimethoxy-phenyl) -benzamide 1026 530 N-. { 3, 5-Dichloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) thioureido] -phenyl) -2-fluoro-benzamide 1027 447 N- (3-Chloro-4-. {3 - [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide 1028 480 2, 3,4,5-Tetrafluoro-N- (4-. {3- [1- (4-Fluoro-phenyl) -ethyl] thioureido} -3-methyl-phenyl) -benzamide 1029 462 2,4,5-Trifluoro-N- (4-. {3- 3 [l- ( 4-fluoro-phenyl) -ethyl] thioureido} -3-methy1-phenyl) -benzamide 1030 427 2-Fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl) ] - thioureido-3-methy1-phenyl) benzamide 1031 457 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -2-methoxy- 5-methyl-phenyl) -benzamide 1032 443 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -3-methoxy-phenyl) benzamide 1033 570 N- (2, 6 -Dibromo-4- { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido.}. -phenyl) -2-fluoro-benzamide 1034 480 2-Fluoro-N- (4-. { 3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-trifluoromethyl-phenyl) -benzamide 1035 541 N- (4-. {3- [l- (4-Bromo- phenyl) -ethyl] -thioureido.} -2- trifluoromethyl-phenyl) -2-fluoro-benzamide 1036 487 N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2- trifluoromethyl-phenyl) -2-fluoro-benzamide 1037 503 N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2- trifluoromethyl-phenyl} -2-fluoro-benzamide 1038 447 N- (2-Chloro-4. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido}. Phenyl) -2-fluoro-benzamide 1039 454 N- (2- Chloro-4- {3- [1- (4-cyano-phenyl) -ethyl} -thioureido} -phenyl) -2-fluoro-benzamide 1040 437 N- (2-Cyano-4- { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido}.-Phenyl) -2-fluoro-benzamide 1041 498 N- (4-. {3- [l- (4-Bromo-phenyl ) -ethyl] -thioureido.} -2- cyano-phenyl) -2-fluoro-benzamide 1042 445 N- (2-Cyano-4-. {3- [l- (4-cyano-phenyl) -ethyl) ] - thioureido.}. - phenyl) -2-fluoro-benzamide 1043 460 N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2- cyano-phenyl} -2-fluoro-benzamide 1044 517 N- (2-Benzoyl-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido}. Phenyl) -2-fluoro-benzamide 1045 427 2-Fluoro-N- (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -2-methyl-phenyl) -benzamide 1046-487 N- (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido} -2-ethyl-phenyl) -2-fluoro-benzamide 1047 434 N- (4-. {3- 3- [1- (4-Cyano-phenyl) -ethyl] -thioureido.} -2- methyl-phenyl) -2-fluoro-benzamide 1048 449 N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2-methyl-phenyl} -2-fluoro-benzamide 1049 456 N- (2-Dimethylamino-4-. {3- [l- (4-fluoro-phenyl) -ethyl] • thioureido}. Phenyl) -2-fluoro-benzamide 1050 526 N- (2-Benzyloxy-4-. {3- [l- (4-cyano-phenyl) -ethyl] -thioureido}. -phenyl) -2-fluoro-benzamide 1051 519 N- (2-Benzyloxy) -4- { 3- [4-fluoro-phenyl] -ethyl] -thioureido} phenyl) -2-fluoro-benzamide 1052 603 N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2- morpholin-4-yl-ethoxy) -phenyl] -2-fluoro-benzamide 1053 603 N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2- morpholin-4-yl-ethoxy) -phenyl] -2-fluoro-benzamide 1054 542 2-Fluoro-N- [4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -2- (2-morpholin-4-yl-ethoxy) -phenyl] -benzamide 1055 485 N- (2-Butoxy-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureid .}.-phenyl) -2-fluoro-benzamide 1056 492 N- (2-Butoxy-4-. {3- [l- (4-cyano-phenyl) -ethyl] -thioureido.} - phenyl) - 2-fluoro-benzamide 1057 589 N- [4-. { 3- [l-Bromo-phenyl) -ethyl] -thioureido} -2- (2-diethylamino-ethoxy) -phenyl] -2-fluoro-benzamide 1058 528 N- (2- (2-Diethylamino-ethoxy) -4-. {3- [l- (4-fluoro-phenyl) ) -ethyl] -thioureido.}.-phenyl) -2-fluoro-benzamide 1059 589 N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2- diethylamino-ethoxy) -phenyl] -2-fluoro-benzamide 1060 457 N- (2-Ethoxy-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido .}.-phenyl) -2-fluoro-benzamide 1061 464 N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2- ethoxy-phenyl) - 2-fluoro-benzamide 1062 468 2-Fluoro-N- [4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -2- (2-nitrile-ethoxy) -phenyl] -benzamide 1063 475 N- [4-. { 3- [1- (4-Cyano-phenyl) -ethyl] -thioureido} -2- (2- nitrile-ethoxy) -phenyl] -2-fluoro-benzamide 1064 443 2-Fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido .} -2-methoxy-phenyl) -benzamide 1065 489 2-Fluoro-N- (5-. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido}. -biphenyl-2-yl ) -benzamide 1066 514 (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido} -2-trifluoromethyl-phenyl) -aminoquinoline-1-carboxylic acid 1067 503 (4). -. {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2- trifluoromethyl-phenyl) -amide of benzofuran-2-carboxylic acid 1068 514 (4-. {3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido.} -2- trifluoromethyl-phenyl) -aminoquinoline-3-carboxylic acid amide 1069 471 (2-cyano-4-. {3- 3 - Isoquinoline-1-carboxylic acid (4-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -amide 1070 460 (2-cyano-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -amide of benzofuran-2-carboxylic acid 1071 471 (2-cyano-4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -amide of Isoquinoline-3-carboxylic acid 1072 460 (4-. Isoquinoline-1-carboxylic acid (3- (l- (4-fluoro-phenyl) -ethyl] -thioureido.} -2-methyl-phenyl) -amide. 1073 449 (4-. {3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-methyl-phenyl) -amide of benzofuran-2-carboxylic acid 1074 460 (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.} -2-methyl-phenyl) -aminoquinoline-3-carboxylic acid 1075 396 (4-. {3- [l- (4-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) pyrazine-2-carboxylic acid amide 1076 401 (4-. {3- 3- l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -amido-2-carboxylic acid amide 1077 401 (4-. {3- [l- (4-fluoro-phenyl) - ethyl] -thioureido.} - phenyl) - thiophene-3-carboxylic acid amide 1078 500. { 4- [3- (4-chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} 2-Isopropyl-thiazole-4-carboxylic acid amide 1079 466. { 4- [3- (3,5-dichloro-phenyl) -thioureido] -phenyl} 2-Isopropyl-thiazole-4-carboxylic acid amide 1080 466. { 4- [3- (3,4-dichloro-phenyl) -thioureido] -phenyl} 2-Isopropyl-thiazole-4-carboxylic acid amide 1081 534. { 4- [3- (3,5-bis-trifluoromethyl-phenyl) -thioureido] -phenyl} 2-Isopropyl-thiazole-4-carboxylic acid amide 1082 480. { 4- [3- (3,4-Dichloro-phenyl) -thioureido] -phenyl} 2-Butyl-thiazole-4-carboxylic acid amide 1083 514. { 4- [3- (4-chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} 2-Butyl-thiazole-4-carboxylic acid amide 1084 480. { 4- [3- (3, 5-dichloro-phenyl) -thioureido] -phenyl} 2-Butyl-thiazole-4-carboxylic acid amide 1085 548. { 2-Butyl-thiazole-4-carboxylic acid 4- [3- (3, 5-bis-trifluoromethyl-phenyl] -tyloreido] -phenyl} -amide; 1086 438. { 4- [3- (3,5-dichloro-phenyl) -thioureido] -phenyl} 2-Methyl-thiazole-4-carboxylic acid amide 1087 438. { 4- [3- (3,4-dichloro-phenyl) -thioureido] -phenyl} 2-Methyl-thiazole-4-carboxylic acid amide 1088 505. { 4- [3- (3, 5-bis-trifluoromethyl-phenyl) -thioureido] -phenyl} 2-Methyl-thiazole-4-carboxylic acid amide 1089 534. { 4- [3- (4-chloro-3-trifluoromethyl-phenyl) -thioureido] -phenyl} 2-Phenyl-thiazole-4-carboxylic acid amide 1090 500 { 4- [3- (3,5-dichloro-phenyl) -thioureido] -phenyl} 2-Phenyl-thiazole-4-carboxylic acid amide 1091 500. { 4- [3- (3,4-dichloro-phenyl) -thioureido] -phenyl} 2-Phenyl-thiazole-4-carboxylic acid amide 1092 568. { 4- [3- (3, 5-bis-trifluoromethyl-phenyl) -thioureido] -phenyl} 2-Phenyl-thiazole-4-carboxylic acid amide 1093 401 2-Fluoro-N-. { 4- [3- (l-thiazol-2-yl-ethyl) -thioureido] -phenyl} -benzamide 1094 588 2-Fluoro-N- [4- (3. {l- [l- (toluene-4-sulfonyl) -lH-indol-2-yl] -ethyl.}. -thioureido) -phenyl ] -benzamide 1095 446 2-Fluoro-N-. { 4- [3- (1-quinolin-2-yl-ethyl) -thioureido] -phenyl} benzamide 1096 446 2-Fluoro-N-. { 4- [3- (l-quinolin-4-yl-ethyl) -thioureido] -phenyl} -benzamide 1097 446 2-Fluoro-N-. { 4- [3- (l-isoquinolin-3-yl-ethyl) -thioureido] -phenyl} -benzamide 1098 446 2-Fluoro-N-. { 4- [3- (1-isoquinolin-1-yl-ethyl) -thioureido] -phenyl} -benzamide 1099 446 2-Fluoro-N-. { 4- [3- (1-quinolin-6-yl-ethyl) -thioureido] -phenyl} -benzamide 1100 446 2-Fluoro-N-. { 4- [3- (l-quinolin-3-yl-ethyl) -thioureido] -phenyl} -benzamide 1101 413 2-methoxy-N-. { 4- [3- (l-thiophen-3-yl-ethyl) -thioureido] -phenyl} -benzamide EXAMPLE 871 (METHOD 33). { 4- [3- (3,5-Dichloro-phenyl) -thioureido] -phenyl} [1,2,3] thiadiazole-4-carboxylic acid amide To a solution of 3,5-dichloroaniline (0.16 g) in tetrahydrofuran (20 ml) was added 1,1'-thiocarbonyl-di (1, 2, 4) -triazole prepared recently (0.20 g) and the mixture was stirred for about 30 minutes at room temperature. [1, 2, 3] -thiadiazole-4-carboxylic acid (4-amino-phenyl) amide (0.22 g) was added to the reaction flask and the mixture was stirred for about 6 hours. The solvent was then removed by evaporation under reduced pressure and hot acetonitrile (3 ml) was added. After 15 hours, the mixture was filtered and the collected precipitate was washed with acetonitrile, then with diethyl ether, and dried with air to provide the desired product as a white powder. [M + H] 424. Using the above procedure and appropriate starting materials, the following compounds were prepared: EJ. M + H NAME OF COMPOUND NO. 872 465 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -3-fluoro-benzamide 873 477 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -2-methoxy-benzamide 874 465 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 875 477 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -3-methoxy-benzamide 876 399 N-. { 4- [3- (3,5-Dichloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} -acetamide 877 365 N-. { 4- [3- (3-Chloro-4-methoxy-5-methyl-phenyl) -thioureido] -phenyl} -acetamide 878 331 N-. { 4- [3- (2-Nitro-phenyl) -thioureido] -phenyl} -acetamide 879 331 N-. { 4- [3- (4-Nitro-phenyl) -thioureido] -phenyl} -acetamide 880 477 N-. { 4- [3- (3, 5-Dichloro-4-methoxy-phenyl) -thioureido] -phenyl} -4-methoxy-benzamide 881 351 N-. { 4- [3- (2-Chloro-5-methoxy-phenyl) -thioureido] -phenyl} - Acetamide 882 428 2-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetamide 883 443 Methyl ester of acid. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetic 884 457 Ethyl ester. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetic 885 447 N-. { 4- [3- (3, 5-Dichloro-4-phenoxy-phenyl) -thioureido] -phenyl} -acetamide 886 410 N- (4-. {3- [3,5-Dichloro-4- (2-nitrile-ethoxy) -phenyl] -thioureido}. -phenyl) -acetamide 887 485 Ter-butylester of acid . { 4- [3- (4-acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} -acetic 888 469. { 4- [3- (3, 5-Dichloro-2-methoxy-4-methyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] -thiadiazole-4-carboxylic acid amide 889 335 N-. { 4- [3- (3-Chloro-4-methyl-phenyl) -thioureido] -phenyl} - acetamide 890 335 N-. { 4- [3- (5-Chloro-2-methyl-phenyl) -thioureido] -phenyl} - acetamide 891 703 N-. { 4- [3- (4- { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chloro-phenylisdisulfanyl} - 3-chloro-phenyl) -thioureido] -phenyl} -acetamide 892 369 N-. { 4- [3- (3, 5-Dichloro-4-methyl-phenyl) -thioureido] -phenyl} -acetamide 893 598 N-. { 4- [3- (3,5-Diiodo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 894 504 N-. { 4- [3- (3,5-Dibromo-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -acetamide 895 317 N-. { 4- [3- (6-Methoxy-pyridin-3-yl) -thioureido] -phenyl} - acetamide 896 347 N-. { 4- [3- (2,6-Dimethoxy-pyridin-3-yl) -thioureido] -phenyl} -acetamide 897 457 2-. { 4- [3- (4-Acetylamino-phenyl) -thioureido] -2,6-dichloro-phenoxy} acetic acid ethyl ester 898 365 4- [3- (4-Acetylamino-phenyl) -thioureido] -2-chlorobenzoic acid 899 346 N-. { 4- [3- (3-Chloro-4-cyano-phenyl) -thioureido] -phenyl} acetamide 900 512 N- (4-. {3- [5-Chloro-2- (4-chloro-phenoxy) -4-pyrrol-1-yl-phenyl] -thioureido}. phenyl) -acetamide 901 355 N-. { 4- [3- (3, 5-Dichloro-phenyl) -thioureido] -phenyl} - acetamide 902 339 N-. { 4- [3- (3-Chloro-4-fluoro-phenyl) -thioureido] -phenyl} - acetamide 903 447 N-. { 4- [3- (3-Chloro-4-iodo-phenyl) -thioureido] -phenyl} - Acetamide 904 400 N-. { 4- [3- (4-Bromo-3-chloro-phenyl) -thioureido] -phenyl} - acetamide 905 424 N- [4- (3-. {4- [Bis- (2-hydroxy-ethyl) -amino] -3-chloro-phenyl] -thioureido) -phenyl] -acetamide 906 434 N - (4- { 3- [3-Chloro-4- (hexyl-methyl-amino) -phenyl] -thioureido}. -phenyl) -acetamide 907 406 N- (4-. {3- 3 -Cloro-4- (isobutyl-methyl-amino) -phenyl] -thioureido.}. -phenyl) -acetamide 908 389 N-. { 4- [3- (3-Chloro-4-trifluoromethyl-phenyl) -thioureido] -phenyl} -acetamide 909 441. { 4- [3- (3-Chloro-4-trifluoromethyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 910 459. { 4- [3- (3-Chloro-4-trifluoromethyl-phenyl) -thioureido] -phenyl} -l, 2,3] thiadiazole-4-carboxylic acid amide 911 469 N-. { 4- [3- (3-Chloro-4-trifluoromethyl-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide 912 435 N-. { 4- [3- (3,4-Dichloro-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 913 407. { 4- [3- (3,4-Dichloro-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 914 425. { 4- [3- (3,4-Dichloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 915 480 N-. { 4- [3- (4-Bromo-3-chloro-phenyl) -thioureido] -phenyl} - 2-fluoro-benzamide 916 527 N-. { 4- [3- (3-Chloro-4-iodo-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 917 452. { 4- [3- (4-Bromo-3-chloro-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 918 499. { 4- [3- (3-Chloro-4-iodo-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 919 391. { 4- [3- (3-Chloro-4-fluoro-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 920 470. { 4- [3- (4-Bromo-3-chloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 921 517. { 4- [3- (3-Chloro-4-iodo-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 922 419 N-. { 4- [3- (3-Chloro-4-fluoro-phenyl) -thioureido] -phenyl} ' 2-fluoro-benzamide 923 409. { 4- [3- (3-Chloro-4-fluoro-phenyl) -thioureido] -phenyl} - acid amide [l, 2,3] thiadiazole-4-carboxylic acid 924 388 N-. { 4- [3- (3-Chloro-4-isoxazol-5-yl-phenyl) -thioureido] -phenyl} -acetamide 925 387 N- (4-. {3- [3-Chloro-4- (lH-pyrazol-3-yl) -phenyl] -thioureido}. phenyl) -acetamide 926 355 N-. { 4- [3- (2,3-Dichloro-phenyl) -thioureido] -phenyl} - acetamide 927 435 N-. { 4- [3- (2,3-Dichloro-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 928 407. { 4- [3- (2,3-Dichloro-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 929 425. { 4- [3- (2,3-Dichloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 930 355 N-. { 4- [3- (2, 5-Dichloro-phenyl) -thioureido] -phenyl} - acetamide 931 435 N-. { 4- [3- (2, 5-Dichloro-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 932 407. { 4- [3- (2,5-Dichloro-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 933 355 N-. { 4- [3- (3,5-Dichloro-phenyl) -thioureido] -phenyl} - acetamide 934 435 N-. { 4- [3- (3,5-Dichloro-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 935 407. { 4- [3- (3, 5-Dichloro-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 936 390 N-. { 4- [3- (3,4,5-Trichloro-phenyl) -thioureido] -phenyl} - Acetamide 937 470 2-Fluoro-N-. { 4- [3- (3,4,5-trichloro-phenyl) -thioureido] -phenyl} -benzamide 938 442. { 4- [3- (3,4,5-Trichloro-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 939 460. { 4- [3- (3,4,5-Trichloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 940 458. { 4- [3- (3-Chloro-4-isoxazol-5-yl-phenyl) -thioureido] -l, 2,3] thiadiazole-4-carboxylic acid phenyl] -amide 941 457 (4- { 3 - [l, 2,3] thiadiazole-4-carboxylic acid [3-chloro-4- (lH-pyrazol-3-yl) -phenyl] -thioureido.]. Phenyl) -amide 942 391. { 4- [3- (3-Chloro-phenyl) -thioureido] -phenyl} - [1,2, 3] thiadiazole-4-carboxylic acid amide 943 373. { 4- [3- (3-Chloro-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 944 401 N-. { 4- [3- (3-Chloro-phenyl) -thioureido] -phenyl} -2-fluorobenzamide 945 373. { 4- [3- (4-Chloro-phenyl) -thioureido] -phenyl} -amide of furan-2-carboxylic acid 946 401 N-. { 4- [3- (4-Chloro-phenyl) -thioureido] -phenyl} -2-fluorobenzamide 947 391. { 4- [3- (4-Chloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 948 401 N-. { 4- [3- (2-Chloro-phenyl) -thioureido] -phenyl} -2-fluorobenzamide 949 396 3- (3. {4- [(Furan-2-carbonyl) -amino] -phenyl] -thioureido) -benzoic acid methyl ester 950 424 Methyl ester of 3- acid. { 3- [4- (2-Fluorobenzoylamino) -amino] -thioureido} -benzoic acid 951 414 3- (3 { 4- [([1,2,3] thiadiazole-4-carbonyl) -amino] -phenyl} -thioureido) -benzoic acid methyl ester 952 409 N- [ 4- [[[[3- (Aminocarbonyl) phenyl] amino] thioxomethyl] -amino] phenyl] -2-fluoro-benzamide 953 373. { 4- [3- (2-Chloro-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 954 381. { 4- [3- (3-Carbamoyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 955 399. { 4- [3- (3-Carbamoyl-phenyl) -thioureido] -phenyl} - [1, 2, 3] thiadiazole-4-carboxylic acid amide 956 391. { 4- [3- (2-Chloro-phenyl) -thioureido] -phenyl} - [1,2,3] thiadiazole-4-carboxylic acid amide 957 356. { 4- [3- (3-Fluoro-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 958 383. { 4- [3- (3-Nitro-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 959 411 2-Fluoro-N-. { 4- [3 (3-nitro-phenyl) -thioureido] -phenyl} - benzamide 960 422. { 4- [3- (3-trifluoromethoxy-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide 961 450 2-Fluoro-N-. { 4- [3- (3-trifluoromethoxy-phenyl) -thioureido] -phenyl} -benzamide 962 384 2-Fluoro-N-. { 4- [3- (3-fluoro-phenyl) -thioureido] -phenyl} -benzamide 963 410 Acid 3-. { 3- [4- (2-Fluoro-benzoylamino) -phenyl] -thioureido} -benzoic acid 964 382 3- (3- {4- [(furan-2-carbonyl) -amino] -phenyl} - thioureido) -benzoic acid 965 408 N-. { 4- [3- (3-Acetyl-phenyl) -thioureido] -phenyl} -2- fluoro-benzamide 966 502 N-. { 4- [3- (3-Butylsulfamoyl-phenyl) -thioureido] -phenyl} - 2-fluoro-benzamide 967 380. { 4- [3- (3-Acetyl-phenyl) -thioureido] -phenyl} -furan-2-carboxylic acid amide 968 447 (4-. {3- [3- (2-Hydroxy-ethanesulfonyl) -phenyl] -thioureido.} - phenyl) -amide of furan-2-carboxylic acid 969 475 2-Fluoro-N- (4-. {3- [3- (2-hydroxy-ethanesulfonyl) -phenyl] -thioureido}. Phenyl) -benzamide 970 474. { 4- [3- (3-Butylsulfamoyl-phenyl) -thioureido] -phenyl} - furan-2-carboxylic acid amide EXAMPLE 971 (METHOD 57) 1- (4-Fluoro-phenyl) -2-methyl-propan-1-ol To a solution of 4-fluorobenzaldehyde (2.0 g) in diethyl ether (40 ml) at 0 ° C was added drop to drop isopropylmagnesium bromide (2.0 M, 9.6 ml) with stirring. After 1.5 hours the reaction was quenched with aqueous ammonium chloride and extracted with diethyl ether. The diethyl ether extracts were washed with saturated sodium chloride, dried over anhydrous magnesium sulfate, filtered and evaporated to give an oil. The oil was purified by silica gel chromatography eluting with 10% dichloromethane-hexanes to give the product, a yellow oil (1.76 g).

EXAMPLE 972 (METHOD 58) 1- (4-Fluoro-phenyl) -2-methyl-propan-l-one To a solution of 1- (4-fluoro-phenyl) -2-methyl-propan-1-ol (1.6 g) in acetone (10 ml) at 0 ° C a Jones reagent (20 ml) was added with stirring. After 10 minutes, excess Jones reagent was destroyed by the addition of isopropyl alcohol. D.Letyl ether was added followed by anhydrous magnesium and the mixture was filtered and evaporated to give the product, a yellow oil (1.2 g).

EXAMPLE 973 (METHOD 59) 3-D: Lmethylamino-5-trifluoromethyl-benzonitrile To a solution of 3-dimethylamino-5-trifluoro-methylbrorbenzene (7.3 g) in N, N-dimethylformamide (20 ml) cuprous cyanide (2.7 g) was added and the reaction was heated to reflux for 12 hours. The reaction was diluted with water (40 ml) and dichloromethane was added. The dichloromethane fraction was washed with concentrated ammonium hydroxide, then with water.

The solution was dried over anhydrous magnesium sulfate, filtered and concentrated to give a yellow solid which was recrystallized from hexanes to give a yellow solid, (4.7 g). The above compounds were tested for activity as herpes virus inhibitors using the following assays.

CITOMEGALOVIRUS HUMANO Production of the trial. Monolayer cultures of human foreskin fibroblasts were infected with wild-type HCMV, typically at a multiplicity of infection equal to 0.2, in the presence of an inhibitor compound (varying in concentration). Three days after the post-infection, the total virus produced in these cultures (ie virus production) was calculated by harvesting and titrating the virus in 12 well plates of cultured human foreskin fibroblasts (used in the absence of the inhibitor) . Plates were quantified 2 weeks post-infection. An inhibitor of HCMV was identified by the reduction of a titer of virus production in the presence, compared to titer in the absence of the compound. In this test, the relative anti-HCMV activity of an inhibitor is typically determined by calculating the ICs0 or IC90 value, ie, the amount of the compound required to reduce virus production by 50% or 90%, respectively. Table I describes IC50 data for compounds tested against HCMV.

Test of microtiter plates. Ninety-six-well plates of human foreskin fibroblasts were infected in the presence of an inhibitory compound with a recombinant HCMV mutant virus whose genome cons the prokaryotic beta-glucuronidase gene (Jefferson, RA, SM Burgess, and D. Hirsh. 1936, Beta-Glucuronidase from Es cheri ch ia col i as a fusion marker of the gene Proc. Nati, Acad. Sci. USA 83: 8447-8451) whose expression is controlled by a viral promoter. An example of such a virus is RV145 (Jones, TR, VP Muzithras, and Y. Gluzman, 1991. Replacement of the mutagenesis of the human cytomegalovirus genome: products of the US10 and US11 gene are not essential J. Virol. 65: 5860 -5872). Since it is under the control of a viral promoter, the expression beta-glucuronidase is an indirect indicator of the growth and replication of HCMV in this assay. At 96 hours post-infection, the lysates of infected cells were prepared (using 50 mM sodium phosphate [pH 7.0] coning 0.1% Triton X-100 and 0.1% sarcosyl) and assayed for the activity of beta-glucuronidase using a substrate for the enzyme that when unfolded produces either a product that can be measured colorimetrically in a spectrophotometer or fluorescently in a microfluorimeter. Examples of such substrates are p-nitrophenyl-beta-D-glucuronide and metilumbelliferalglucuronide, respectively. The presence of an antiviral compound is indicated by the reduced expression of the HCMV genome residing in the beta-glucuronidase gene, compared in the absence of the inhibitor. In this way, the generation of the chromophore or fluorophore product in this test is correspondingly reduced. The data from this generated assay utilizing varying amounts of the inhibitor compound is also used to estimate the IC50 value of an inhibitor compound.

HSV antiviral assay (ELISA) Vero cells (ATCC # CCL-81) were deposited in 96-well tissue culture plates at 3.5 × 10 04 cells per 100 μl of DMEM tissue culture (Dulbecco's modified Eagle's medium) supplemented with 2% of fetal bovine serum (FBS) in each well. After incubation overnight @ 37 ° C (in 5% C02) and 30 minutes before infection with HSV-1 (multiplicity of infection equal to 0.006), the cells are either untreated or treated with the compound test (multiple concentrations) or standard reference drug control. After approximately 24 hours at the post-infection incubation @ 37 ° C (in 5% C02), the cells were fixed by the ELISA assay. The primary antibody is a monoclonal anti-HSV glycoprotein D murine antibody and the secondary antibody is a goat-anti-mouse IgG antibody bound to β-galactosidase. In this way the scope of viral replication is determined by the calculation of β-galactosidase activity by quantifying the generation of the cleavage product of fluorescent methyl-umbelliferone after the addition of the methyl-umbeliferal-β-D-galactoside substrate (Sigma # M1633) in a microfluorimeter (365 nm by excitation and 450 nm by emission). The antiviral activity (IC50) of the test compound is determined by comparing the fluorescence obtained in the absence of the compound to that obtained in the presence of the compound. The data is shown in Table I.

VZV Antiviral Assay (ELISA) For the generation of existing VZV that is used in the assay, the Ellen VZV strain (ATCC # VR-1367) was used to infect human foreskin fibroblast (HFF) cells at low multiplicity (less than 0.1) and incubated overnight at 37 ° C in 5% C02. After incubation overnight, the mixture of HFF cells infected with VZV and uninfected were then harvested and added to each well of 96-well plates (3.5 × 10 4 cells in 100 μl of DMEM supplemented with 2% FBS). ) containing the test compound or the standard control drug control (in 100 μl of DMEM supplemented with 2% FBS per well). These cells were incubated for three days at 37 ° C in 5% C02, then fixed by the ELISA assay. The primary antibody is a murine anti-VZV glycoprotein II monoclonal antibody (Applied Biosystems, Inc. # 13-145-100) and the secondary antibody is a goat-anti-mouse IgG antibody bound to β-galactosidase. In this way, the extent of viral replication is determined by calculating β-galactosidase activity by quantifying the generation of the cleavage product of fluorescent 4-methyl umbelliferone after the addition of the substrate of metilumbumbiferal-β-D-galactoside ( Sigma # M1633) in a microfluorimeter (365 nm by excitation and 450 nm per emission). The antiviral activity (IC5o) of the test compound was determined by comparing the fluorescence obtained in the absence of the compound to that obtained in the presence of the compound. The data are shown in Table I. Table I describes IC50 data for compounds tested against the herpes virus.

Example IC50 ICSO% Inhibition IC50 (ug / ml) (ugml) 10 ug / ml (ugml) HCMV HSV VZV VZV 204 8 4 41 > ! < > 26 () > 10 > 10 18 7 277 > 10 > 10 0 > 10 286 40 2 5 > I0 295 > 10 0.15 20 > 10 301 > 10 10 10 > 10 303 > 10 > 10 15 > 1() 310 > 10? 40 > 10 322 7 4 108 8 325 > 10 I 33 > 10 327 > 10 > 10 42 > 10 338 35 > 50 13 > I0 347 10 0.06 34 > 10 359 > 10 0.6 59 > 10 381 > 10 > 10 13 > 10 389 1.5 0.04 9 > 10 394 > 10 0.2 36 > 10 400 > 10 > 10 15 > 10 401 2.5 > 10 70 > fifteen 402 4 > 10 13 > 10 408 6 0.2 56 > 10 418 3 0.05 10 > 10 419 > 10 0.2 3 > 10 420 7 0.2 34 > 10 529 8.5 1 23 9 1023 9 > 10 10 1024 > 10 > 10 > 10 1025 > 10 > 10 > 10 1026 > 10 0.15 > 10 1027 1028 1029 > 10 > 10 0.53 1030 1031 > 10 > 10 0.7 1032 1033 3.8 7 0.039 1034 2.6 > 10 0.03 1035 2.3 3.1 0.032 1036 2.1 4 0.31 1037 2 3.6 0.027 1038 3.5 3 0.04 1039 1.3 7.2 0.25 1040 > 10 > 10 0.05 Example IC50 IC50% Inhibition 1C50 (ug / ml) (ug / ml) 10 ug / ml (ug / ml) HCMV HSV VZV VZV 1041 1 100..44 > > 1100 0.096 1042 2 2..11 4 4..22 0.54 1043 > > 1100 > > 1100 0.099 1044 1 1..88 > > 1100 3.3 1045 1 1..55 6 6..22 0.05 1046 2 2..88 6 6..33 0.057 1047 6 6..11 > > 1100 0.63 1048 3 3..44 > > 1100 0.061 1C49 4 4..55 8 8 0.07 1C50 > > 1100 > > 1100 > 7.5 1051 > > 11ÜÜ > > 1100 0.7 1052 1053 1054 1055 > 10 > 10 0.32 1056 2.5 > 10 0.4 1057 1058 1059 1060 > 10 > 10 0.26 1061 7.6 > 10 0.64 1062 6 > 10 0.33 1063 3.6 > 10 0.64 1064 4.5 3.9 0.04 1065 8.1 4.9 0.33 1066 1.8 1.9 0.02 1067 3.3 3.8 0.26 1068 > 10 > 10 0.04 1069 4 > 10 0.019 1070 2 4.1 0.2 1071 > 10 9 0.03 1072 > 10 > 10 0.027 1073 6.3 4.6 0.47 1074 4 5.8 0.07 1 102 5.0 > 7.5 1 103 5.0 0.12 1 104 > 10 0.09 1 105 1.1 > 7.5 1 106 > 10 0.014 1 107 > 10 0.04 1108 > 10 0.03 1 109 > 0.07 In this way, according to the present invention, the compounds of the present invention can be administered to a patient suffering from herpes virus which includes VZV, HSV and HCMV, in an amount effective to inhibit the virus. The compounds of the present invention in this manner are useful for alleviating and eliminating the symptoms of herpes virus infections in mammals including, but not limited to humans. The compounds of the invention can be administered to a patient either neat or with a pharmaceutical convention carrier. Applicable solid carriers may include one or more substances which may also act as flavoring agents, lubricants, solubilizers, suspending agents, fillers, glidants, compression aids, binders or tablet disintegrating agents or an encapsulating material. In powders, the carrier is a finely divided solid that is in admixture with the finely divided active ingredient. In tablets, the active ingredient is mixed with a carrier having the necessary compression properties in suitable and compact proportions in the desired shape and size. The powders and tablets preferably contain up to 99% of the active ingredient. Suitable solid carriers include, for example, calcium phosphate, magnesium stearate, talc, sugars, lactose, dextrin, starch, gelatin, cellulose, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidine, low melting waxes, and ion exchange resins. The liquid carriers can be used in the preparation of solutions, suspensions, emulsions, elixir syrups. The active ingredient of this invention can be dissolved or suspended in a pharmaceutically acceptable liquid carrier such as water, an organic solvent, a mixture of both, or a pharmaceutically acceptable oils or fats. The liquid carrier may contain other suitable pharmaceutical additives such as solubilizers, emulsifiers, buffers, preservatives, sweeteners, flavoring agents, suspending agents, thickening agents, colors, viscosity regulators, stabilizers or osmo-regulators. Suitable examples of liquid carriers for oral or parenteral administration include water (particularly containing additives as in the above, for example cellulose derivatives, preferably sodium carboxymethylcellulose solution), alcohols (including onhydric alcohols and polyhydric alcohols, for example glycols) and their derivatives, and oils (for example fractionated coconut oil and peanut oil). For parenteral administration, the carrier can also be an oily ester such as ethyl oleate and isopropyl myristate. Sterile liquid carriers are used in compositions in sterile liquid form for parenteral administration. Liquid pharmaceutical compositions that are sterile solutions or suspensions can be used by, for example, intramuscular, intraperitoneal or subcutaneous injection. Sterile solutions can also be administered intravenously. The oral administration can be either in the form of a liquid or solid composition. Preferably, the pharmaceutical composition is in the form of unit doses, for example tablets or capsules. In such form, the composition is sub-divided into unit doses containing appropriate amounts of the active ingredient; the unit dosage forms may be packaged compositions, for example packaged powders, vials or vials, ampoules, pre-filled syringes or sachets containing liquids. The dosage unit form can be, for example, a capsule or tablet itself, or it can be the appropriate number of any compositions in packaged form.

Therapeutically effective doses that are used in the treatment of herpes virus infection, including VZV, HSV and HCMV must be determined subjectively by the attending physician. The vbles involved include the condition, age and weight of the patient. The novel method of the invention for the treatment of herpes virus infection comprises administering to a subject, including humans, an effective amount of at least one compound of Formula 1 or a non-toxic, pharmaceutically acceptable salt thereof. The compounds can be administered orally, rectally, parenterally or topically to the skin and mucosa. The usual daily doses are depending on the specific compound, method of treatment and condition of the patient. The usual daily dose is 0.01-1000 mg / Kg for oral applications, preferably 0.5-500 mg / Kg and 0.1-100 mg / Kg for parenteral applications, preferably 0.5-50 mg / Kg. It is noted that in relation to this date, the best method known by the applicant to carry out the aforementioned invention is that which is clear from the present description of the invention.

Claims

CLAIMS Having described the invention as above, the content of the following claims is claimed as property: 1. A compound of the formula: Characterized because R? -R; are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 atoms of carbon, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6, -C0R6, -0R6, -SR6, -SOR6, -S02R6, -C0NR R8, -NR6N (R7R8) / -N (R7R8) or WY- (CH2) nZ with the proviso that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R, taken together form a 3-7 membered heterocycloalkyl 0 a heteroaryl of 3 to 7 members; Re and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl or heteroaryl, or R7 and R8, taken together they can form a 3 to 7 membered heterocycloalkyl; R9-R1? they are independently hydrogen, alkyl 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and Rio or Rp and R? 2 can be taken together to form an aryl of 5. at 7 carbon atoms; with the proviso that at least one of R9-? 2 is not hydrogen; is O, NRβ, or is absent; And it is - (CO) - or - (C02) -, or it is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -C02R6, -COR6, -CONR7R8, -OCOR6 / -NR6COR7, -OCONR6, -OR6, -SR6, -SOR6, -S02R6, SR6N (R7R8), --N (R7R8) or phenyl; G is aryl or a fused bicyclic heteroaryl; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 atoms carbon, or (CH) J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6, or a pharmaceutical salt thereof.
2. A compound according to claim 1, characterized in that at least one of R1-R5 is not hydrogen.
3. A compound according to claim 1, characterized in that R9-R12 are independently hydrogen, halogen, methyl, methoxy and cyano.
4. A compound according to claim 1, characterized in that G is phenyl.
5. A compound according to claim 1, characterized in that G is substituted with one or more substituents selected from alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl heteroaryl, halogen, -CN, -N02, -C02R6, -COR6, -0R6, -SR6, -S0R6 , -S02R6, -CONR7R8, -NR6N (R7RT), -N (R7R8) or WY- (CH2) n- Z.
6. A compound according to claim 5, characterized in that G is substituted with one or two halogen substituents.
7. A compound according to claim 1, characterized in that G is 2-fluorophenyl.
8. A compound according to claim 1, characterized in that G is a fused bicyclic heteroaryl.
9. A compound according to claim 1, characterized in that G is isoquinoline, quinoline or benzofuran. THE. A compound according to claim 1, characterized in that it is selected from: -Fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido.} -2, 3 , 5,6-tetramethyl-phenyl) -benzamide, N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2,5-dimethoxy-phenyl) - 2-Fluoro-benzamide, 2-Fluoro-N- (4- {3 - [l - (4-fluoro-phenyl) -ethyl} -thioureido} -2,5-dimethoxy-phenyl) -benzamide, N-. { 3, 5-Dichloro-4- [3- (5-chloro-2,4-dimethoxy-phenyl) -thioureido] -phenyl} -2-fluoro-benzamide, N-. { 3-Chloro-4-. { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} phenyl) -2-fluoro-benzamide, 2,3,4,5-Tetrafluoro-N- (4-. {3- [l- (4-fluorophenyl) -ethyl] -thioureido} -3-me tyl-phenyl) -benzamide, 2,4,5-Tr i fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -3-methyl- phenyl) -benzamide, 2-Fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -3-methyl-phenyl) -benzamide, 2-Fluoro -N- (4- { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -2-met oxy-5-met il-phenyl) -benzamide, -Fluoro-N- (4- {3- [1- (4-fluoro-phenyl) -ethyl} -thioureido} -3-methoxy-phenyl) -benzamide, N- (2,6-Dibromo-4- { 3- [1- (4-fluoro-phenyl) -ethyl] thioureido.} - phenyl) -2-fluoro-benzamide, 2-Fluoro-N- (4-. {3- [1- (4-fluoro) - phenyl) -ethyl] -thioureido.} -2-trifluoromethyl-phenyl) -benzamide, N- (4-. {3- [l- (4-Bromo-phenyl) -ethyl] -thioureido} - 2-trifluoromethyl-phenyl) -2-fluoro-benzamide, N- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2-trifluoromethyl-phenyl) -2 -fluoro-benzamide, N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2-trifluoromethyl-phenyl} -2-fluoro-benzamide, N- (2-Chloro-4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -phenyl) -2-fluoro-benzamide, N - (2-Chloro-4- {3- [l- (4-cyano-phenyl) -ethyl] -thioureido} - phenyl) -2-fluoro-benzamide, N- (2-cyano-4-) {.3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- (4-. {3- 3 [l- (4-Bromo - phenyl) -ethyl] -thioureido.} -2-cyano-phenyl) -2-fluoro-benzamide, N- (2-cyano-4-. {3- [l- (4-cyano-phenyl) - ethyl] -thioureido.}.-phenyl) -2-fluoro-benzamide, i-. { 4- [3- [1-Benzofuran-2-yl-ethyl) -thioureido] -2-cyano-phenyl} -2-fluoro-benzamide, N- (2-Benzoyl-4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido}. Phenyl) -2-fluoro-benzamide, -Fluoro-N- (4- { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -2-methyl-phenyl) -benzamide, - (4-. {3- [1- (4-Bromo-phenyl) -ethyl] -thioureido.} - 2-methyl-phenyl) -2-fluoro-benzamide, N- (4-. {3- 3- [1- (4-Cyano- phenyl) -ethyl] -thioureido.} -2-methyl-phenyl) -2-fluoro-benzamide, N-. { 4- [3- (1-Benzofuran-2-yl-ethyl) -thioureido] -2-methyl-phenyl} -2-fluoro-benzamide, - (2-Dimethylamino-4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -phenyl) -2-fluoro-benzamide, W- (2-Benzyloxy-4- {3- [l- (4-cyano-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, - (2-Benzyloxy-4-. { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido.] - phenyl) -2-fluoro-benzamide, S- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2-morpholin-4-yl-ethoxy) -phenyl] -2-fluoro-benzamide, SI- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2-morpholin-4-yl-ethoxy) -phenyl] -2-fluoro-benzamide, 2-Fluoro-N- [4-. { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -2- (2-morpholin-4-yl-ethoxy) -phenyl] -benzamide, S- (2-Butoxy-4- { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, - (2-Butoxy-4-) {. 3- 3- [1- (4-cyanophenyl) -ethyl] -thioureido.} - phenyl) -2-fluoro-benzamide, N- [4-. { 3- [1- (4-Bromo-phenyl) -ethyl] -thioureido} -2- (2-diethylamino-ethoxy) -phenyl] -2-fluoro-benzamide, N- (2- (2-Diethylamino-ethoxy) -4- { 3- [1- (4-fluorophenyl) - ethyl] -thioureido.}. -phenyl) -2-fluoro-benzamide, N- [4-. { 3- [1- (4-B-phenyl) -ethyl] -thioureido} -2- (2-diethylamino-ethoxy) -phenyl] -2-fluoro-benzamide, N- (2-Ethoxy-4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido}-phenyl) -2-fluoro-benzamide, H- (4-. {3- [l- (4-Cyano-phenyl) -ethyl] -thioureido} -2-ethoxy-phenyl) -2- fluoro-benzamide, -Fluoro-N- [4-. { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -2- (2-nitrile-ethoxy) -phenyl] -benzamide, N- [4-. { 3- [1- (4-Cyano-phenyl) -ethyl] -thioureido} -2- (2-nitrile-ethoxy) -phenyl] -2-fluoro-benzamide, -Fluoro-N- (4-. {3- [1- (4-f-luoro-phenyl) -ethyl] -thioureido} -2-methoxy-phenyl) -benzamide, 2-Fluoro-N- (5-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido}. -biphenyl-2-yl. ) -benzamide, isoquinoline-1-carboxylic acid (4- { 3- [1- (4-Fluoro-phenyl) -eti-1] -thioureido.} -2-trifluoromethyl-phenyl) -amide, [4 -. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-trifluoromethyl-phenyl) -amide of benzofuran-2-carboxylic acid, 4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-tri-fluoroTiet-il-phenyl) -aminoquinoline-3-carboxylic acid amide, (2-Cyano-4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido}. -phenyl) -aminoquinoline-1-carboxylic acid amide, 2-Cyano-4-. { 3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} phenyl) -amide of benzofuran-2-carboxylic acid, [2-Cyano-4-. { 3- [1- (4-Fluoro-phenyl) -ethyl] -thioureido} -phenyl) -aminoquinoline-3-carboxylic acid amide, 4- ({3- (l- (4-Fluoro-phenyl) -ethyl) -thioureido} -2-methyl-phenyl) -amide of acid isoquinolin-1-carboxylic, (4- {3- [l- (4-Fluoro-phenyl) -ethyl] -thioureido} -2-methyl-phenyl) -amide of benzofuran-2-carboxylic acid, and (4-. { 3- [l- (4-Fluoro-phenyl) -et i 1] -thioureido.} -2-methyl-phenyl) -aminoquinoline-3-carboxylic acid amide, 2-Fluoro-N- (4-. {3- [1- (4-fluoro-phenyl) -ethyl] -thioureido} -3-trifluoromethyl-phenyl) -benzamide, (4-. {3- [(1S) -1- (4-Bromo-phenyl) -ethyl] -thioureido} -2-trifluoromethyl-phenyl) -aminoquinoline-3-carboxylic acid amide, N- (4-. {3- [3- (1S) -1- (4-Bromo-phenyl) -ethyl] -thioureido.} -2-cyano-phenyl) -2-fluoro-benzamide, N- (4-. {3- (IR) - 1- (4-Bromo-phenyl) -ethyl] -thioureido.} -2-cyano-phenyl) -2-fluoro-benzamide, N-. { 2-Cyano-4- [( { [(SS) -1- (4-fluorophenyl) ethyl] -amino} carbonyl) amino] phenyl} -2-fluorobenzamide, 2-Fluoro-N-. { 4- [( { [(IR) -1- (4-fluorophenyl) ethyl] -amino.} Carbonyl) amino] -3-methylphenyl} benzamide, N-. { 4- [( { [(LS) -l- (4-Fluorophenyl) ethyl] amino.} - carbothioyl) amino] -2-cyanophenyl} -2-fluorobenzamide, N-. { 4- [( { [(1S) -1- (4-Chlorophenyl) ethyl] amino.} - carbothioyl) amino] -2-cyanophenyl} -2-fluorobenzamide, or pharmaceutical salts thereof. 11. A pharmaceutical composition comprising a compound of the formula: characterized in that R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl from 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6i -COR6, -OR6, -SR6, -SOR6, -S02R6, -CONR7R8, -NR6N (R7R8), -N (R7R8) or -Y- (CH2) n -Z with the proviso that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or a 3 to 1 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl or heteroaryl, or R7 and R8, taken together they can form a 3- to 7-membered heterocycloalkyl; R 9 -R 2 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4. carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and Rio or Rn and R? 2 can be taken together to form an aryl of 5 to 7 carbon atoms; with the proviso that at least one of Rg-? 2 is not hydrogen; is 0, NR6, or is absent; And it is - (CO) - or - (C02) -, or it is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -C02R6, -C0R6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -OR6, -SR6, -SOR6, -S02R6, SR6N (R R8), --N (R7R8) or phenyl; G is aryl or a fused bicyclic heteroaryl; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 atoms carbon, or (CH) J; C 1 -C 6 -alkyl, C 3 -C 7 -cycloalkyl, phenyl or benzyl; and n is an integer from 1 to 6, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier or diluent. 12. A method for inhibiting the replication of a herpes virus comprising contacting a compound of the formula: characterized in that R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl from 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6, -C0R6, -OR6, -SR6, -S0R6, -S02R6, - CONR7R8, -NR6N (R7R8), -N (R7R8) or WY- (CH2) nZ with the proviso that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together: orman a 3- to 7-membered heterocycloalkyl 0 a heteroaryl of 3 to 7 members; Re and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 atoms < carbon, aryl or heteroaryl, or R and R8, taken together can form a 3-7 membered heterocycloalkyl; Rg-R ?: > they are independently hydrogen, alkyl 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or Rg and Rio or Rn and R 2 can be taken together to form an aryl of 5 to 7 carbon atoms; with the proviso that at least one of RT-I2 is not hydrogen; W is O, NR6, or is absent; And it is - (CO) - or - (C02) -, or it is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -C02R6, -COR6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -OR6, -SR. { , -SOR6 / -S02R6, SR6N (R7R8), -N (R7R8) or phenyl; G is aryl or a fused bicyclic heteroaryl; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to (5) carbon atoms, or (CH) J; J is »alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl, and n is an integer of 1 to 6, or a pharmaceutically acceptable salt of them, with a herpes virus. 13. The method according to claim 12, characterized in that the herpes virus is human cytomegalovirus. 14. The method according to claim 12, characterized in that the herpes virus is herpes simplex virus. 15. The method according to claim 12, characterized in that the herpes virus is the varicella zoster virus. 16. The method according to claim 12, characterized in that the compound is a substantially pure optical isomer (S). 17. A method for the treatment of a patient suffering from a herpes virus infection comprising administering to the patient a therapeutically effective amount of a compound having the formula: characterized in that R? -R are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms , cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6, -C0R6, -OR6, -SR6, -S0R6, -S02R6 , -CONR7R8, -NR6N (R7R8), -N (R7R8) or -Y- (CH2) nZ with the proviso that at least one of R? ~ R5 is not lidrogen; or R2 and R3 or R3 and R4, taken together form a 3- to 7-membered heterocycloalkyl a 3-7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl or heteroaryl, or R7 and R8, taken together they can form a 3- to 7-membered heterocycloalkyl; 9 ~ R 2 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or Rg and Rio or Rn and Ri2 can be taken together to form an aryl of 5 to 7 carbon atoms; with the proviso that at least one of Rg-? 2 is not hydrogen; W is O, NR6, or is absent; And it is - (CO) - or - (C02) -, or it is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -C02R6, -COR6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -OR6, -SR6, -SOR6, -S02R6, SR6N (R7R8), -N (R7R8) or phenyl; G is aryl or a fused bicyclic heteroaryl; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH) J; J is alkyl of 1 to 6 carbon atoms, ? Ikalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6, or a pharmaceutical salt thereof. 18. The method according to claim 17, characterized in that the herpes virus is human cytomegalovirus. 19. The method according to claim 17, characterized in that the herpes virus is herpes simplex virus. 20. The method according to claim 19, characterized in that the compound is a substantially pure optical isomer (S). 21. The method according to claim 17, characterized in that the herpes virus is the varicella zoster virus. SUMMARY OF THE INVENTION Compounds of the formula (I), wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, per-haloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl, heteroaryl, halogen, -CN, -N02, -C02R6, -COR6, - OR6, -SR6, -SOR6, -S02R6, -CONR7R8, -NR6N (R7R8), -N (R7R8) or WY- (CH2) n-2, with the proviso that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together form a 3-7 membered heterocycloalkyl or a 3-7 membered heteroaryl; Re and R are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon atoms, aryl or heteroaryl, or R and R8, taken together they can form a 3 to 7 membered heterocycloalkyl; R9-R2 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or Rg and Rio or Rn and R? 2 can be taken together to form an aryl of 5 to 7 carbon atoms; with the proviso that at least one of Rg-? 2 is not hydrogen; W is O, NR6, or is absent; And it is - (CO) - or - (C02) -, or it is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -C02R6, -COR6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -0R6, -SR6, -SOR6, -S02R6, SR6N (R7R8), - N (R7R8) or phenyl; G is aryl or a fused bicyclic heteroaryl; X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 atoms carbon, or (CH) J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6, in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes virus: .mple, Epstein-Barr virus, varicella-zoster virus, herpesvirus 6 and 7 human , and Kaposi herpes virus.. { »>