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1. 发明授权

US07968564B2 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US07968564B2
公开(公告)日：2011-06-28
申请号：US12760638
申请日：2010-04-15
申请人： Joseph P. Vacca , Linda S. Payne , Richard C. A. Isaacs
发明人： Joseph P. Vacca , Linda S. Payne , Richard C. A. Isaacs
IPC分类号： C07D455/00 , A01N43/42 , A61K31/44
CPC分类号： C07D471/14 , A61K31/4353 , A61K31/4375 , C07D498/14
摘要： Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset 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的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中键A，环A，R 1，R 2和R 3在本文中定义。该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。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。

2. 发明授权

US07741315B2 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US07741315B2
公开(公告)日：2010-06-22
申请号：US11920032
申请日：2006-05-05
申请人： Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaacs , Richard Pracitto
发明人： Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaacs , Richard Pracitto
IPC分类号： A01N43/00 , A61K31/33 , C07D491/00
CPC分类号： C07D471/14 , A61K31/4353 , A61K31/4375 , C07D498/14
摘要： Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset 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）的三环化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中键A，环A，R 1，R 2和R 3在本文中定义。该化合物可用于预防或治疗艾滋病毒感染以及艾滋病的预防，治疗或延迟。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. 发明授权

US5668289A Pyridinone thrombin inhibitors 失效
标题翻译：吡啶酮凝血酶抑制剂
公开(公告)号：US5668289A
公开(公告)日：1997-09-16
申请号：US669189
申请日：1996-06-24
申请人： Philip E. Sanderson , Adel M. Naylor-Olsen , Dona L. Dyer , Joseph P. Vacca , Richard C. A. Isaacs , Bruce D. Dorsey , Mark E. Fraley
发明人： Philip E. Sanderson , Adel M. Naylor-Olsen , Dona L. Dyer , Joseph P. Vacca , Richard C. A. Isaacs , Bruce D. Dorsey , Mark E. Fraley
IPC分类号： A61K38/00 , C07K5/078 , C07D211/86 , A61K31/44
CPC分类号： C07K5/06139 , A61K38/00
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##
摘要翻译：本发明的化合物可用于抑制凝血酶和相关的血栓闭塞，并具有以下结构：例如：

4. 发明授权

US5744486A Pyridinone thrombin inhibitors 失效
标题翻译：吡啶酮凝血酶抑制剂
公开(公告)号：US5744486A
公开(公告)日：1998-04-28
申请号：US829406
申请日：1997-03-31
申请人： Philip E. Sanderson , Adel M. Naylor-Olsen , Dona L. Dyer , Joseph P. Vacca , Richard C. A. Isaacs , Bruce D. Dorsey , Mark E. Fraley
发明人： Philip E. Sanderson , Adel M. Naylor-Olsen , Dona L. Dyer , Joseph P. Vacca , Richard C. A. Isaacs , Bruce D. Dorsey , Mark E. Fraley
IPC分类号： A61K38/00 , C07K5/078 , A61K31/445 , C07D211/06
CPC分类号： C07K5/06139 , A61K38/00
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##
摘要翻译：本发明的化合物可用于抑制凝血酶和相关的血栓闭塞，并具有以下结构：例如：

5. 发明申请

US20100216834A1 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：US20100216834A1
公开(公告)日：2010-08-26
申请号：US12445594
申请日：2007-10-15
申请人： Richard C. A. Isaacs , John S. Wai , Linda S. Payne , Thorsten E. Fisher
发明人： Richard C. A. Isaacs , John S. Wai , Linda S. Payne , Thorsten E. Fisher
IPC分类号： A61K31/4375 , C07D471/14 , C07D471/04 , A61P31/18
CPC分类号： C07D471/14
摘要： Stereoisomers of compounds of Formula I are disclosed: wherein V1, V2, R5a, R5b, R5c, R8 and R9b are defined herein and wherein the stereoisomer contains 2 chiral centers in the 8-membered ring and one of the chiral centers is due to the presence of a chiral ring carbon. The isomers are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression 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：公开了式I化合物的立体异构体：其中V1，V2，R5a，R5b，R5c，R8和R9b在本文中定义，其中立体异构体在8元环中含有2个手性中心，并且其中一个手性中心是由于存在手性环碳。异构体是HIV整合酶和HIV复制抑制剂的抑制剂，可用于预防或治疗艾滋病毒感染以及艾滋病的发病或进展的预防，治疗或延迟。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。

6. 发明授权

US5747540A HIV protease inhibitors useful for the treatment of AIDS 失效
标题翻译：用于治疗艾滋病的HIV蛋白酶抑制剂
公开(公告)号：US5747540A
公开(公告)日：1998-05-05
申请号：US734276
申请日：1996-10-21
申请人： Craig A. Coburn , Randall W. Hungate , Richard C. A. Isaacs , Joseph P. Vacca , Mary Beth Young
发明人： Craig A. Coburn , Randall W. Hungate , Richard C. A. Isaacs , Joseph P. Vacca , Mary Beth Young
IPC分类号： A61K45/06 , C07C235/36 , C07C271/22 , C07C311/29 , C07C317/46 , C07C323/62 , C07D209/18 , C07D263/14 , C07D311/68 , C07D333/24 , C07D333/60 , C07D335/06 , A61K31/165 , A61K31/38 , C07C203/00 , C07D333/62
CPC分类号： C07D335/06 , A61K45/06 , C07C235/36 , C07C271/22 , C07C311/29 , C07C317/46 , C07C323/62 , C07D209/18 , C07D263/14 , C07D311/68 , C07D333/24 , C07D333/60 , C07C2102/08
摘要： Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：化合物如IMAGE或其药学上可接受的盐是HIV蛋白酶抑制剂。这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

7. 发明授权

US08030332B2 Potassium channel inhibitors 失效
标题翻译：钾通道抑制剂
公开(公告)号：US08030332B2
公开(公告)日：2011-10-04
申请号：US12223353
申请日：2007-01-29
申请人： B. Wesley Trotter , Richard C. A. Isaacs , Zhicai Wu , Jacob M. Hoffman , Mark T. Bilodeau , Ahren Iver Green
发明人： B. Wesley Trotter , Richard C. A. Isaacs , Zhicai Wu , Jacob M. Hoffman , Mark T. Bilodeau , Ahren Iver Green
IPC分类号： C07D401/14 , A61K31/506
CPC分类号： C07D413/14
摘要： The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
摘要翻译：本发明涉及具有用作治疗心律失常的钾通道抑制剂的结构I的二吡啶-3-基甲氧基化合物及其衍生物等。

8. 发明授权

US5932606A Pyrazinone, pyridinone, piperidine and pyrrolidine thrombin inhibitors 失效
标题翻译：吡嗪酮，吡啶酮，哌啶和吡咯烷凝血酶抑制剂
公开(公告)号：US5932606A
公开(公告)日：1999-08-03
申请号：US49639
申请日：1998-03-20
申请人： Richard C. A. Isaacs , Adel M. Naylor-Olsen , Bruce D. Dorsey , Christina L. Newton
发明人： Richard C. A. Isaacs , Adel M. Naylor-Olsen , Bruce D. Dorsey , Christina L. Newton
IPC分类号： A61K38/00 , C07K5/02 , C07K5/065 , C07K5/078 , A61K31/415 , A61K31/495 , C07D403/12
CPC分类号： C07K5/06078 , C07K5/0207 , C07K5/06139 , A61K38/00
摘要： A compound which inhibits human thrombin and where has the structure and pharmaceutically acceptable salts thereof, wherein such as ##STR1## which are useful for inhibiting formation of blood platelet aggregates in blood in a mammal.
摘要翻译：抑制人凝血酶的化合物，其具有其结构和药学上可接受的盐，其可用于抑制哺乳动物血液中血小板聚集体的形成。

9. 发明授权

US08513234B2 HIV integrase inhibitors 有权
标题翻译： HIV整合酶抑制剂
公开(公告)号：US08513234B2
公开(公告)日：2013-08-20
申请号：US12572341
申请日：2009-10-02
申请人： Richard C. A. Isaacs , Wayne J. Thompson , Peter D. Williams , Dai-Shi Su , Shankar Venkatraman , Mark W. Embrey , Thorsten E. Fisher , John S. Wai , David C. Dubost , Richard G. Ball , Eric J. Choi , Tao Pei , Sarah L. Trice , Neil Campbell , Matthew Maddess , Peter E. Maligres , Michael Shevlin , Zhiguo Jake Song , Dietrich P. Steinhuebel , Neil A. Strotman , Jingjun Yin
发明人： Richard C. A. Isaacs , Wayne J. Thompson , Peter D. Williams , Dai-Shi Su , Shankar Venkatraman , Mark W. Embrey , Thorsten E. Fisher , John S. Wai , David C. Dubost , Richard G. Ball , Eric J. Choi , Tao Pei , Sarah L. Trice , Neil Campbell , Matthew Maddess , Peter E. Maligres , Michael Shevlin , Zhiguo Jake Song , Dietrich P. Steinhuebel , Neil A. Strotman , Jingjun Yin
IPC分类号： C07D487/12
CPC分类号： C07D498/04 , C07D487/04 , H01L2924/0002 , H01L2924/00
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) 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. Processes for making compounds of Formula I and intermediates thereof are also described.
摘要翻译：式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。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。还描述了制备式I化合物的方法及其中间体。

10. 发明申请

US20100087419A1 HIV INTEGRASE INHIBITORS 有权
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：US20100087419A1
公开(公告)日：2010-04-08
申请号：US12572341
申请日：2009-10-02
申请人： Richard C. A. Isaacs , Wayne J. Thompson , Peter D. Williams , Dai-Shi Su , Shankar Venkatraman , Mark W. Embrey , Thorsten E. Fisher , John S. Wai , David C. Dubost , Richard G. Ball , Eric J. Choi , Tao Pei , Sarah L. Trice , Neil Campbell , Matthew Maddess , Peter E. Maligres , Michael Shevlin , Zhiguo Jake Song , Dietrich P. Steinhuebel , Neil A. Strotman , Jingjun Yin
发明人： Richard C. A. Isaacs , Wayne J. Thompson , Peter D. Williams , Dai-Shi Su , Shankar Venkatraman , Mark W. Embrey , Thorsten E. Fisher , John S. Wai , David C. Dubost , Richard G. Ball , Eric J. Choi , Tao Pei , Sarah L. Trice , Neil Campbell , Matthew Maddess , Peter E. Maligres , Michael Shevlin , Zhiguo Jake Song , Dietrich P. Steinhuebel , Neil A. Strotman , Jingjun Yin
IPC分类号： A61K31/553 , C07D487/04 , C07D281/10 , A61K31/55 , A61P31/18
CPC分类号： C07D498/04 , C07D487/04 , H01L2924/0002 , H01L2924/00
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) 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. Processes for making compounds of Formula I and intermediates thereof are also described.
摘要翻译：式I化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中X1，X2，Y，R1A，R1B，R2和R3如本文所定义。该化合物可用于预防或治疗艾滋病毒感染，并预防，治疗或延迟艾滋病的发病或进展。该化合物用作抗体作为化合物本身（或其水合物或溶剂化物）或以药学上可接受的盐形式的HIV感染和AIDS。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。还描述了制备式I化合物的方法及其中间体。

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