N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
    4.
    发明授权
    N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors 失效
    可用作HIV整合酶抑制剂的N-(取代苄基)-8-羟基-1,6-萘啶-7-甲酰胺

    公开(公告)号:US07323460B2

    公开(公告)日:2008-01-29

    申请号:US10508094

    申请日:2003-03-12

    IPC分类号: C07D401/02 A61K31/4375

    CPC分类号: C07D471/04

    摘要: N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R2′ and R3′ are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

    摘要翻译: N-(取代的苄基)-8-羟基-1,6-萘啶-7-甲酰胺是HIV整合酶和HIV复制抑制剂的抑制剂。 萘啶甲酰胺具有式(I):其中R 1,R 2,R 3和R 3'在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防,延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。 描述了预防,治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

    Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
    5.
    发明授权
    Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors 失效
    可用作HIV整合酶抑制剂的羟基萘啶酮甲酰胺

    公开(公告)号:US07279487B2

    公开(公告)日:2007-10-09

    申请号:US10500972

    申请日:2003-01-13

    IPC分类号: A61K31/44 C07F5/02 C07D471/02

    摘要: Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b, R3, R4, and R5 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

    摘要翻译: 下式的羟基萘啶酮甲酰胺被描述为HIV整合酶的抑制剂和HIV复制抑制剂,其中L,R 1a,R 1b,R 1c, R 2a,R 2b,R 3,R 4和R 5,以及R 5, >在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防,延迟发作和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。 还描述了预防,治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

    Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors
    6.
    发明授权
    Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors 失效
    可用作HIV整合酶抑制剂的二羟基吡啶并吡嗪-1,6-二酮化合物

    公开(公告)号:US07517532B2

    公开(公告)日:2009-04-14

    申请号:US10526275

    申请日:2003-09-10

    CPC分类号: C07D471/14 C07D471/04

    摘要: 8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I), wherein R1, R2, R3, R4 and R5 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

    摘要翻译: 8,9-二氢二氢吡啶并吡嗪-1,6-二酮和8,9-二羟基吡啶并吡嗪-1,6-二酮是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中,吡啶并吡啶酮具有式(I):(I),其中R 1,R 2,R 3,R 4和R 5在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防,延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。 描述了预防,治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

    HIV integrase inhibitors
    8.
    发明授权
    HIV integrase inhibitors 失效
    HIV整合酶抑制剂

    公开(公告)号:US07476666B2

    公开(公告)日:2009-01-13

    申请号:US11629153

    申请日:2005-06-03

    摘要: Bicyclic pyrazoles of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z is O or N(R8); n is an integer equal to zero or 1; and R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

    摘要翻译: 式I的双环吡唑是HIV整合酶和HIV复制抑制剂的抑制剂:其中Z是O或N(R8); n是等于零或1的整数; 并且R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 8在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防,延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。