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1. 发明申请

US20080139579A1 Hiv Integrase Inhibitors 失效
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20080139579A1
公开(公告)日：2008-06-12
申请号：US10591914
申请日：2005-03-04
申请人： Matthew M. Morrissette , Peter D. Williams , John S. Wai , Thorsten E. Fisher , Terry A. Lyle
发明人： Matthew M. Morrissette , Peter D. Williams , John S. Wai , Thorsten E. Fisher , Terry A. Lyle
IPC分类号： A61K31/506 , C07D471/04 , A61K31/4375 , C07D471/10 , A61P31/12 , A61K31/438 , C07D401/14
CPC分类号： C07D471/04 , C07D471/10
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and R9 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化合物是HIV整合酶和HIV复制抑制剂的抑制剂：（I）其中Z，R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8，和R 9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。

2. 发明授权

US07619086B2 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US07619086B2
公开(公告)日：2009-11-17
申请号：US10591914
申请日：2005-03-04
申请人： Matthew M. Morrissette , Peter D. Williams , John S. Wai , Thorsten E. Fisher , Terry A. Lyle
发明人： Matthew M. Morrissette , Peter D. Williams , John S. Wai , Thorsten E. Fisher , Terry A. Lyle
IPC分类号： C07D221/18 , C07D221/22 , A01N43/40 , A61K31/435
CPC分类号： C07D471/04 , C07D471/10
摘要： Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and R9 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化合物是HIV整合酶和HIV复制抑制剂的抑制剂：其中Z，R1，R2，R3，R4，R5，R6，R7，R8和R9如本文所定义。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. 发明授权

US07538112B2 HIV integrase inhibitors 有权
标题翻译： HIV整合酶抑制剂
公开(公告)号：US07538112B2
公开(公告)日：2009-05-26
申请号：US11579772
申请日：2005-05-03
申请人： John S. Wai , Joseph P. Vacca , Linghang Zhuang , Boyoung Kim , Terry A. Lyle , Catherine M. Wiscount , Melissa S. Egbertson , Lou Anne Neilson , Mark Embrey , Thorsten E. Fisher , Donnette D. Staas
发明人： John S. Wai , Joseph P. Vacca , Linghang Zhuang , Boyoung Kim , Terry A. Lyle , Catherine M. Wiscount , Melissa S. Egbertson , Lou Anne Neilson , Mark Embrey , Thorsten E. Fisher , Donnette D. Staas
IPC分类号： C07D487/14 , A61K31/5025 , A61K31/4985
CPC分类号： A61K31/5025 , C07D487/14 , Y02A50/414
摘要： Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 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：羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4，R 5，R 6和R 7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。

4. 发明申请

US20080287394A1 Hiv Integrase Inhibitors 有权
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20080287394A1
公开(公告)日：2008-11-20
申请号：US11579772
申请日：2005-05-03
申请人： John S. Wai , Joseph P. Vacca , Linghang Zhuang , Boyoung Kim , Terry A. Lyle , Catherine M. Wiscount , Melissa S. Egbertson , Lou Anne Neilson , Mark Embrey , Thorsten E. Fisher , Donnette D. Staas
发明人： John S. Wai , Joseph P. Vacca , Linghang Zhuang , Boyoung Kim , Terry A. Lyle , Catherine M. Wiscount , Melissa S. Egbertson , Lou Anne Neilson , Mark Embrey , Thorsten E. Fisher , Donnette D. Staas
IPC分类号： A61K31/69 , C07D487/14 , C07F5/02 , A61K31/541 , A61P31/18 , C07D417/14 , A61K31/5025
CPC分类号： A61K31/5025 , C07D487/14 , Y02A50/414
摘要： Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 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：羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4， / SUP，R 5，R 6和R 7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。

5. 发明授权

US07435735B2 Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors 失效
标题翻译：可用作HIV整合酶抑制剂的羟基吡啶并吡咯并吡嗪二酮化合物
公开(公告)号：US07435735B2
公开(公告)日：2008-10-14
申请号：US10576328
申请日：2004-10-18
申请人： John S. Wai , Thorsten E. Fisher , Linghang Zhuang , Donnette D. Staas , Terry A. Lyle , Boyoung Kim , Mark W. Embrey , Catherine M. Wiscount , Lekhanh O. Tran , Melissa Egbertson , Kelly L. Savage
发明人： John S. Wai , Thorsten E. Fisher , Linghang Zhuang , Donnette D. Staas , Terry A. Lyle , Boyoung Kim , Mark W. Embrey , Catherine M. Wiscount , Lekhanh O. Tran , Melissa Egbertson , Kelly L. Savage
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00 , C07D487/00 , C07D241/36
CPC分类号： C07D471/14
摘要： Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, 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：羟基取代的吡啶并吡咯并吡嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。在一个实施方案中，二酮化合物具有式（I）：（I）其中a，b，A，B，R 1，R 2， R 4，R 4，R 5，R 6，R 7和R 9，这里定义了8。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。

6. 发明申请

US20130338141A1 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：US20130338141A1
公开(公告)日：2013-12-19
申请号：US13970130
申请日：2013-08-19
申请人： Richard C. 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 Maddes , Peter E. Maligres , Michael Shevlin , Zhiguo Jake Song , Dietrich P. Steinhuebel , Neil A. Strotman , Jingjun Yin
发明人： Richard C. 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 Maddes , Peter E. Maligres , Michael Shevlin , Zhiguo Jake Song , Dietrich P. Steinhuebel , Neil A. Strotman , Jingjun Yin
IPC分类号： C07D498/04 , C07D487/04
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。

7. 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。

8. 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。

9. 发明授权

US07517532B2 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：US07517532B2
公开(公告)日：2009-04-14
申请号：US10526275
申请日：2003-09-10
申请人： John S. Wai , Boyoung Kim , Thorsten E. Fisher , Peter D. Williams , H. Marie Langford
发明人： John S. Wai , Boyoung Kim , Thorsten E. Fisher , Peter D. Williams , H. Marie Langford
IPC分类号： A61K39/21 , C07D241/00 , C07D241/02 , C07D241/36 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
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 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。

10. 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。

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