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    Aminopyridine-containing thiourea inhibitors of herpes viruses
    5.
    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：US06380243B1

    公开(公告)日：2002-04-30

    申请号：US09804510

    申请日：2001-03-12

    申请人： Jonathan Bloom ,  Martin DiGrandi ,  Russell Dushin ,  Stanley Lang ,  Bryan O'Hara

    发明人： Jonathan Bloom ,  Martin DiGrandi ,  Russell Dushin ,  Stanley Lang ,  Bryan O'Hara

    IPC分类号： C07D30702

    CPC分类号： C07D333/02 ,  C07D207/34 ,  C07D211/72 ,  C07D213/44 ,  C07D235/26 ,  C07D307/02

    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 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; 或其药物盐，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。

    Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group
    10.
    发明授权
    Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group 失效
    含α-甲基苄基的含有苯二胺基团的疱疹病毒的硫脲抑制剂

    公开(公告)号：US06462055B2

    公开(公告)日：2002-10-08

    申请号：US09845428

    申请日：2001-04-30

    申请人： Jonathan Bloom ,  Kevin Curran ,  Martin DiGrandi ,  Russell Dushin ,  Stanley Lang ,  Emily Norton ,  Adma Ross ,  Bryan O'Hara

    发明人： Jonathan Bloom ,  Kevin Curran ,  Martin DiGrandi ,  Russell Dushin ,  Stanley Lang ,  Emily Norton ,  Adma Ross ,  Bryan O'Hara

    IPC分类号： A61K3147

    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 R1 and R2 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; 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; 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： 具有下式的化合物：其中R 1 -R 5独立地选自氢，1至6个碳原子的烷基，2至6个碳原子的烯基，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 3至10个碳原子的杂环烷基，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，条件是R 1 -R 5中的至少一个不是氢; 或R 1和R 2或R 3和R 4一起形成3至7元杂环烷基或3至7元杂芳基; R 6和R 7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; W为O，NR 6或不存在; Y为 - （CO） - 或 - （CO 2） - 或不存在; Z为1至4个碳原子的烷基，-CN，-CO 2 R 6，COR 6 ，-CONR7R8，-OCOR6，-NR6COR7，-OCONR6，-OR6，-SR6，-SOR6，-SO2R6，SR6N（R7R8），-N（R7R8）或苯基; G是芳基或稠合双环杂芳基; X是键 ，-NH，1至6个碳原子的烷基，1至6个碳原子的烯基，1至6个碳原子的烷氧基，1至6个碳原子的硫代烷基，1至6个碳原子的烷基氨基或（CH） 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; 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。