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1. 发明申请

US20050176718A1 Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors 审中-公开
公开(公告)号：US20050176718A1
公开(公告)日：2005-08-11
申请号：US11056412
申请日：2005-02-11
申请人： Neville Anthony , Robert Gomez , Steven Young , Melissa Egbertson , John Wai , Linghang Zhuang , Mark Embrey , Lekhanh Tran , Jeffrey Melamed , H. Langford , James Guare , Thorsten Fisher , Samson Jolly , Michelle Kuo , Debra Perlow , Jennifer Bennett , Timothy Funk
发明人： Neville Anthony , Robert Gomez , Steven Young , Melissa Egbertson , John Wai , Linghang Zhuang , Mark Embrey , Lekhanh Tran , Jeffrey Melamed , H. Langford , James Guare , Thorsten Fisher , Samson Jolly , Michelle Kuo , Debra Perlow , Jennifer Bennett , Timothy Funk
IPC分类号： A61K31/4375 , A61K31/47 , A61K31/4985 , A61K31/541 , A61K31/554 , A61P31/12 , A61P31/18 , C07D20060101 , C07D215/48 , C07D221/00 , C07D241/00 , C07D471/00 , C07D471/04 , C07D471/16 , C07D487/00 , C07D519/00 , A61K31/498 , A61K31/4745 , C07D471/02 , C07D487/02
CPC分类号： C07D471/04
摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or 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.

2. 发明申请

US20080009490A1 Hiv Integrase Inhibitors 失效
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20080009490A1
公开(公告)日：2008-01-10
申请号：US10592222
申请日：2005-03-04
申请人： Peter Williams , John Wai , Mark Embrey , Donnette Staas , Linghang Zhuang , H. Langford
发明人： Peter Williams , John Wai , Mark Embrey , Donnette Staas , Linghang Zhuang , H. Langford
IPC分类号： A61K31/5377 , A61K31/522 , A61P31/18 , C07D413/08 , C07D471/04
CPC分类号： C07D487/04 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/54 , A61K45/06 , A61K2300/00
摘要： Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R4 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：双环尿嘧啶和相关化合物是HIV整合酶和HIV复制抑制剂的抑制剂。在一个实施方案中，化合物具有式I：其中a，b，Y，R 1，R 2，R 3和R 3， SUP> 4 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。

3. 发明申请

US20060024330A1 Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors 失效
标题翻译：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：US20060024330A1
公开(公告)日：2006-02-02
申请号：US10526275
申请日：2003-09-10
申请人： John Wai , Boyoung Kim , Thorsten Fisher , Linghang Zhuang , Peter Williams , Terry Lyle , H. Langford , Kyle Robinson
发明人： John Wai , Boyoung Kim , Thorsten Fisher , Linghang Zhuang , Peter Williams , Terry Lyle , H. Langford , Kyle Robinson
IPC分类号： A61P31/18 , A61K39/21 , C07D471/00 , C07D487/00
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 3， SUP> 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。

4. 发明申请

US20080015187A1 Hiv Integrase Inhibitors 失效
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20080015187A1
公开(公告)日：2008-01-17
申请号：US11629153
申请日：2005-06-03
申请人： John Wai , Peter Williams , H. Langford
发明人： John Wai , Peter Williams , H. Langford
IPC分类号： A61K31/55 , A61P31/00 , C07D223/00
CPC分类号： C07D487/04 , A61K31/52 , A61K31/551
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（R 8）; n是等于零或1的整数; 和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。

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