Diaminopyridine-containing thiourea inhibitors of herpes viruses
    2.
    发明授权
    Diaminopyridine-containing thiourea inhibitors of herpes viruses 失效
    含二氨基吡啶的疱疹病毒的硫脲抑制剂

    公开(公告)号:US06407123B1

    公开(公告)日:2002-06-18

    申请号:US09670180

    申请日:2000-09-26

    IPC分类号: A61K31443

    摘要: Compounds of the formula 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 ; 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; A is heteroaryl.

    摘要翻译: 式R 1 -R 5的化合物独立地选自氢,1至6个碳原子的烷基,2至6个碳原子的链烯基,2至6个碳原子的炔基,1至6个碳原子的全卤代烷基,3至10个碳原子的环烷基 原子,3至10个碳成员的杂环烷基,芳基,杂芳基,卤素,-CN,-NO 2,-CO 2 R 6,-COR 6,-OR 6,-SR 6,-SOR 6,-SO 2 R 6,-CONR 7 R 8,-NR 6 N(R 7 R 8) N(R 7 R 8)或WY-(CH 2)n Z; 或R2和R3或R3和R4一起形成3至7元杂环烷基或3至7元杂芳基; R6和R7独立地为氢,1至6个碳原子的烷基,1至6个碳原子的全卤代烷基或芳基 ; R 8为氢,1至6个碳原子的烷基,1至6个碳原子的全卤烷基,3至10个碳原子的环烷基,3至10个成员的杂环烷基,芳基或杂芳基,或R 7和R 8一起可以形成3 至7元杂环烷基; A为杂芳基。

    Diaminopyridine-containing thiourea inhibitors of herpes virus
    3.
    发明授权
    Diaminopyridine-containing thiourea inhibitors of herpes virus 失效
    含二氨基吡啶的疱疹病毒的硫脲抑制剂

    公开(公告)号:US06271236B1

    公开(公告)日:2001-08-07

    申请号:US09669943

    申请日:2000-09-26

    IPC分类号: C07D40102

    摘要: Compounds of the formula 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; 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; A is heteroaryl.

    摘要翻译: 式R 1 -R 5的化合物独立地选自氢,1至6个碳原子的烷基,2至6个碳原子的链烯基,2至6个碳原子的炔基,1至6个碳原子的全卤代烷基,3至10个碳原子的环烷基 原子,3至10个碳成员的杂环烷基,芳基,杂芳基,卤素,-CN,-NO 2,-CO 2 R 6,-COR 6,-OR 6,-SR 6,-SOR 6,-SO 2 R 6,-CONR 7 R 8,-NR 6 N(R 7 R 8) N(R 7 R 8)或WY-(CH 2)n Z; 或R2和R3或R3和R4一起形成3至7元杂环烷基或3至7元杂芳基; R6和R7独立地为氢,1至6个碳原子的烷基,1至6个碳原子的全卤代烷基或芳基 ; R 8为氢,1至6个碳原子的烷基,1至6个碳原子的全卤烷基,3至10个碳原子的环烷基,3至10个成员的杂环烷基,芳基或杂芳基,或R 7和R 8一起可以形成3 至7元杂环烷基; A为杂芳基。

    Diaminopyridine-containing thiourea inhibitors of herpes viruses
    4.
    发明授权
    Diaminopyridine-containing thiourea inhibitors of herpes viruses 失效
    含二氨基吡啶的疱疹病毒的硫脲抑制剂

    公开(公告)号:US06262082B1

    公开(公告)日:2001-07-17

    申请号:US09669483

    申请日:2000-09-25

    IPC分类号: C07D40112

    摘要: Compounds of the formula 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; 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; A is heteroaryl.

    摘要翻译: 式R 1 -R 5的化合物独立地选自氢,1至6个碳原子的烷基,2至6个碳原子的链烯基,2至6个碳原子的炔基,1至6个碳原子的全卤代烷基,3至10个碳原子的环烷基 原子,3至10个碳成员的杂环烷基,芳基,杂芳基,卤素,-CN,-NO 2,-CO 2 R 6,-COR 6,-OR 6,-SR 6,-SOR 6,-SO 2 R 6,-CONR 7 R 8,-NR 6 N(R 7 R 8) N(R 7 R 8)或WY-(CH 2)n Z; 或R2和R3或R3和R4一起形成3至7元杂环烷基或3至7元杂芳基; R6和R7独立地为氢,1至6个碳原子的烷基,1至6个碳原子的全卤代烷基或芳基 ; R 8为氢,1至6个碳原子的烷基,1至6个碳原子的全卤烷基,3至10个碳原子的环烷基,3至10个成员的杂环烷基,芳基或杂芳基,或R 7和R 8一起可以形成3 至7元杂环烷基; A为杂芳基。

    Alph-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group

    公开(公告)号:US06255349B1

    公开(公告)日:2001-07-03

    申请号:US09444734

    申请日:1999-11-22

    IPC分类号: A61K3117

    CPC分类号: C07D211/96 C07C335/20

    摘要: Compounds having the formula:  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 R3or 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;  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;  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; or a pharmaceutically acceptable salt thereof, useful 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 herpesvirus.

    Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing a substituted phenylenediamine group

    公开(公告)号:US06407249B1

    公开(公告)日:2002-06-18

    申请号:US09684011

    申请日:2000-12-29

    IPC分类号: A61K31341

    摘要: Compounds of the formula: 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(R7R3R) or phenyl; G is a monocyclic 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, or 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 useful 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 herpesvirus.

    Aminopyridine-containing thiourea inhibitors of herpes viruses
    10.
    发明授权
    Aminopyridine-containing thiourea inhibitors of herpes viruses 失效
    含有氨基吡啶的疱疹病毒的硫脲抑制剂

    公开(公告)号:US06262090B1

    公开(公告)日:2001-07-17

    申请号:US09444896

    申请日:1999-11-22

    IPC分类号: A61K3144

    摘要: Compounds of the formula wherein A is heteroaryl; 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; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond 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; and 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 acceptable salt thereof, useful 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 herpesvirus.

    摘要翻译: 式Ⅳa的化合物是杂芳基; R 9 -R 12独立地是氢,1至4个碳原子的烷基,1至4个碳原子的全卤代烷基,卤素,1至4个碳原子的烷氧基或氰基,或R 9和R 10或R 11和 R 12可以一起形成5至7个碳原子的芳基; W是O,NR 6或不存在; G是芳基或杂芳基; X为键,X为碳原子数为1〜6的烷基,碳原子数为1〜6的烯基,碳原子数为1〜6的烷氧基,碳原子数为1〜6的硫代烷基,碳原子数为1〜6的烷基氨基 原子或(CH)J; 且J为1至6个碳原子的烷基,3至7个碳原子的环烷基,苯基或苄基; andn是1〜6的整数; 或其药学上可接受的盐,其可用于治疗与疱疹病毒相关的疾病,包括人巨细胞病毒,单纯疱疹病毒,爱泼斯坦 - 巴尔病毒,水痘带状疱疹病毒,人疱疹病毒-6和-7以及卡波西疱疹病毒。