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公开(公告)号:US20130178468A1
公开(公告)日:2013-07-11
申请号:US13606929
申请日:2012-09-07
申请人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaccs , Wei Han , Melissa Egbertson , Richard Pracitto
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C. A. Isaccs , Wei Han , Melissa Egbertson , Richard Pracitto
IPC分类号: C07D471/14 , C07D498/14
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。
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公开(公告)号:US20090054399A1
公开(公告)日:2009-02-26
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 , Wei Han , Melissa Egbertson , Richard Pracitto
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne , Richard C.A. Isaacs , Wei Han , Melissa Egbertson , Richard Pracitto
IPC分类号: A61K31/5383 , C07D471/14 , A61K31/551 , A61K31/4985 , A61K31/4375 , C07D498/14
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。
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公开(公告)号:US06380249B1
公开(公告)日:2002-04-30
申请号:US09323417
申请日:1999-06-01
申请人: Steven D. Young , Melissa Egbertson , Linda S. Payne , John S. Wai , Thorsten E. Fisher , James P. Guare, Jr. , Mark W. Embrey , Lekhanh Tran , Linghang Zhuang , Joseph P. Vacca , H. Marie Langford , Jeffrey Melamed , Juan C. Jaen , David L. Clark , Julio C. Medina
发明人: Steven D. Young , Melissa Egbertson , Linda S. Payne , John S. Wai , Thorsten E. Fisher , James P. Guare, Jr. , Mark W. Embrey , Lekhanh Tran , Linghang Zhuang , Joseph P. Vacca , H. Marie Langford , Jeffrey Melamed , Juan C. Jaen , David L. Clark , Julio C. Medina
IPC分类号: A61K31215
CPC分类号: C07D213/64 , C07C59/84 , C07C59/86 , C07C59/88 , C07C59/90 , C07C69/738 , C07C217/60 , C07C229/34 , C07C229/42 , C07C233/63 , C07C235/60 , C07C255/41 , C07C271/16 , C07C271/28 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D209/12 , C07D241/12 , C07D253/08 , C07D263/58 , C07D295/088 , C07D295/155 , C07D295/192 , C07D333/22
摘要: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and 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: 某些六元芳族和杂芳族二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制的抑制剂。 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药,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。
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公开(公告)号:US07741315B2
公开(公告)日:2010-06-22
申请号:US11920032
申请日:2006-05-05
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。
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公开(公告)号:US20110275621A1
公开(公告)日:2011-11-10
申请号:US13107512
申请日:2011-05-13
申请人: Joseph P. Vacca , John S. Wai , Linda S. Payne
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne
IPC分类号: A61K31/4375 , C07D498/14 , A61P37/00 , A61K31/5383 , A61K31/5377 , A61P31/18 , C07D471/14 , A61K31/4985
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。
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公开(公告)号:US08293731B2
公开(公告)日:2012-10-23
申请号:US13107512
申请日:2011-05-13
申请人: Joseph P. Vacca , John S. Wai , Linda S. Payne
发明人: Joseph P. Vacca , John S. Wai , Linda S. Payne
IPC分类号: A01N43/62 , A61K31/55 , C07D487/00
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。
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公开(公告)号:US07968564B2
公开(公告)日:2011-06-28
申请号:US12760638
申请日:2010-04-15
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。
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公开(公告)号:US20100204201A1
公开(公告)日:2010-08-12
申请号:US12760638
申请日:2010-04-15
IPC分类号: A61K31/553 , C07D471/14 , A61K31/4375 , A61P31/18 , A61K31/551 , A61K31/4985 , A61K31/5365 , C07D498/14
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。
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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。
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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。
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