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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: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: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:US20100216834A1
公开(公告)日:2010-08-26
申请号:US12445594
申请日:2007-10-15
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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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: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: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: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:US5665720A
公开(公告)日:1997-09-09
申请号:US458529
申请日:1995-06-02
IPC分类号: A61K31/535 , A61K31/536 , A61K45/06 , C07D265/18
CPC分类号: C07D265/18 , A61K31/535 , A61K31/536 , A61K31/70 , A61K45/06 , Y10S514/934
摘要: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), 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: 某些苯并恶嗪酮可用于抑制HIV逆转录酶(包括其抗性品种),预防或治疗艾滋病毒感染和艾滋病治疗,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 其他抗病毒药物,免疫调节剂,抗生素或疫苗。 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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