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公开(公告)号：US08691991B2
公开(公告)日：2014-04-08
申请号：US10597902
申请日：2005-02-10
申请人： Brian Alvin Johns , Eric Eugene Boros , Takshi Kawasuji , Cecilia S. Koble , Noriyuki Kurose , Hitoshi Murai , Ronald George Sherrill , Jason Gordon Weatherhead
发明人： Brian Alvin Johns , Eric Eugene Boros , Takshi Kawasuji , Cecilia S. Koble , Noriyuki Kurose , Hitoshi Murai , Ronald George Sherrill , Jason Gordon Weatherhead
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译： 本发明的特征在于是HIV整合酶抑制剂的化合物，因此可用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC。
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2.发明授权Methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate and processes for the preparation thereof 有权3-（苄氧基）-1-（2,2-二羟乙基）-4-氧代-1,4-二氢吡啶-2-羧酸甲酯及其制备方法公开(公告)号：US08580967B2
公开(公告)日：2013-11-12
申请号：US13054847
申请日：2009-07-23
IPC分类号： C07D213/79
CPC分类号： A61K31/675 , A61K31/4985 , A61K31/5377 , C07D211/86 , C07D309/40 , C07D498/14 , C07F9/65583
摘要： The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. For example, the present invention includes methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2 -carboxylate of the formula P-8: and processes for the preparation thereof.
摘要翻译： 本发明的特征在于作为HIV整合酶抑制剂的前药的化合物，因此可用于递送用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC的化合物。 例如，本发明包括式P-8的3-（苄氧基）-1-（2,2-二羟乙基）-4-氧代-1,4-二氢吡啶-2-羧酸甲酯：及其制备方法 。
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公开(公告)号：US20110183940A1
公开(公告)日：2011-07-28
申请号：US13054847
申请日：2009-07-23
IPC分类号： A61K31/675 , C07D491/147 , A61K31/4985 , C07D413/14 , A61K31/5377 , C07D315/00 , C07D213/803 , A61P31/18
CPC分类号： A61K31/675 , A61K31/4985 , A61K31/5377 , C07D211/86 , C07D309/40 , C07D498/14 , C07F9/65583
摘要： The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译： 本发明的特征在于作为HIV整合酶抑制剂的前药的化合物，因此可用于递送用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC的化合物。
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4.发明授权Processes and intermediates for carbamoylpyridone HIV integrase inhibitors 有权氨基甲酰吡啶酮HIV整合酶抑制剂的方法和中间体公开(公告)号：US08552187B2
公开(公告)日：2013-10-08
申请号：US13128457
申请日：2009-12-09
IPC分类号： C07D213/79 , C07D213/803 , C07D498/14 , C07D211/86
CPC分类号： C07D213/82 , C07D213/79 , C07D213/803 , C07D213/807 , C07D498/14
摘要： Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1 P3, R3 and Rx are as described herein.
摘要翻译： 提供了产生醛亚甲基或连接到6元环的杂原子的水合或半缩醛亚甲基而不经过烯属基团而不需要使用锇试剂的方法。 特别地，式（I）化合物可以由（II）制备，并避免使用烯丙基胺：（式I和II）其中R，P1 P3，R3和Rx如本文所述。
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![(3S,11aR)-N-[2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide useful as anti-HIV agent](/abs-image/US/2013/04/02/US08410103B2/abs.jpg.150x150.jpg)
5.发明授权(3S,11aR)-N-[2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide useful as anti-HIV agent 有权（3S，11aR）-N- [2,4-二氟苯基）甲基] -6-羟基-3-甲基-5,7-二氧代-2,3,5,7,11,11a-六氢[1,3] 恶唑并[3,2-a]吡啶并[1,2-d]吡嗪-8-甲酰胺，用作抗HIV剂公开(公告)号：US08410103B2
公开(公告)日：2013-04-02
申请号：US13352686
申请日：2012-01-18
IPC分类号： A61K31/495
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is directed to a substituted 2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2 -a]pyrido[1,2-d]pyrazine-5,7-dione useful as an anti-HIV agent, which has the formula: as well as pharmaceutically acceptable salts thereof, compostions thereof, and methods of use thereof.
摘要翻译： 本发明涉及取代的2,3,5,7,11,11a-六氢[1,3]恶唑并[3,2-a]吡啶并[1,2-d]吡嗪-5,7-二酮，其可用 作为抗HIV剂，其具有下式：及其药学上可接受的盐，其组合物及其使用方法。
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公开(公告)号：US08217034B2
公开(公告)日：2012-07-10
申请号：US13054633
申请日：2009-07-23
IPC分类号： A61K31/535 , C07D498/14
CPC分类号： A61K31/535 , C07D498/14
摘要： The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
摘要翻译： 本发明的特征在于作为HIIV整合酶抑制剂的前药的化合物，因此可用于抑制HIV复制，预防和/或治疗HIV感染以及治疗AIDS和/或ARC。
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7.发明申请Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity 有权具有hiv整合酶抑制活性的多环氨基甲酰吡啶酮衍生物公开(公告)号：US20090318421A1
公开(公告)日：2009-12-24
申请号：US11919386
申请日：2006-04-28
IPC分类号： A61K31/55 , C07D241/36 , A61K31/4985 , C07D471/12 , C07D498/22 , A61K31/5383 , C07D487/22 , C07D471/22 , C07D498/12 , A61K31/5365 , C07D413/14 , A61K31/5377 , C07D487/12 , A61K31/551 , A61P31/18
CPC分类号： C07D498/14 , A61K9/0053 , A61K31/4985 , A61K31/519 , A61K31/5365 , A61K31/551 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/22 , C07D498/04 , C07D498/20 , C07D498/22
摘要： The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
摘要翻译： 本发明提供下述新型化合物（I），具有抗病毒活性，特别是HIV整合酶抑制活性，以及含有该化合物（I）的药物，特别是抗HIV药物，以及方法和 中间体。 （其中Z 1为NR 4; R 1为氢或低级烷基; X为单键，选自O，S，SO，SO 2和NH的杂原子基团，或杂原子基团可插入的低级亚烷基或低级亚烯基） R2是任选取代的芳基; R 3是氢，卤素，羟基，任选取代的低级烷基等;和R 4和Z 2部分一起形成环，形成多环化合物，包括例如三环或四环化合物。
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公开(公告)号：US08609653B2
公开(公告)日：2013-12-17
申请号：US13547199
申请日：2012-07-12
申请人： Martha Alicia De La Rosa , Brian Alvin Johns , Emile Johann Velthuisen , Jason Weatherhead , Vicente Samano
发明人： Martha Alicia De La Rosa , Brian Alvin Johns , Emile Johann Velthuisen , Jason Weatherhead , Vicente Samano
IPC分类号： A61K31/437 , C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/538 , C07D491/052 , A61P31/18
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/538 , C07D471/04 , C07D491/052
摘要： Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
摘要翻译： 本发明提供了其化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于治疗由逆转录病毒病毒家族成员（例如人类免疫缺陷病毒（HIV））介导的病毒感染的用途。
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公开(公告)号：US20130289027A1
公开(公告)日：2013-10-31
申请号：US13980085
申请日：2012-01-23
IPC分类号： C07D217/24 , A61K45/06 , C07D401/12 , A61K31/4725 , A61K31/541 , A61K31/5377 , A61K31/472 , C07D405/04
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/14
摘要： Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
摘要翻译： 本发明提供了其化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于治疗由逆转录病毒病毒家族成员（例如人类免疫缺陷病毒（HIV））介导的病毒感染的用途。
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公开(公告)号：US09029391B2
公开(公告)日：2015-05-12
申请号：US13980085
申请日：2012-01-23
IPC分类号： A61K31/472 , A61K31/4725 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/12 , C07D217/24 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D405/14
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D413/14
摘要： Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
摘要翻译： 本发明提供了其化合物及其药学上可接受的盐，其药物组合物，其制备方法及其用于治疗由逆转录病毒病毒家族成员（例如人类免疫缺陷病毒（HIV））介导的病毒感染的用途。
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