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![Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides](/abs-image/US/2015/06/09/US09051337B2/abs.jpg.150x150.jpg)
1.发明授权Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides 有权取代的10-羟基-9,11-二氧代-2,3,4a，5,9,11,13,13a-八氢-1h吡啶并[1,2-a]吡咯并[1'，2'：3,4 ]咪唑并[1,2-d]吡嗪-8-甲酰胺公开(公告)号：US09051337B2
公开(公告)日：2015-06-09
申请号：US14211364
申请日：2014-03-14
IPC分类号： A61K31/4985 , C07D241/38 , C07D498/22 , C07D471/04 , C07D471/14 , C07D498/04 , C07D471/22 , C07D498/14 , C07D498/20
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），其具有抗病毒活性; 特别是HIV整合酶抑制活性，以及含有它们的药物，特别是抗HIV药物，以及其过程和中间体。 （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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![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 having HIV integrase inhibitory activity](/abs-image/US/2021/02/23/US10927129B2/abs.jpg.150x150.jpg)
公开(公告)号：US10927129B2
公开(公告)日：2021-02-23
申请号：US16400373
申请日：2019-05-01
IPC分类号： A61K31/4985 , C07D487/14 , C07D498/14 , C07D471/04 , C07D471/14 , C07D498/04 , C07D471/22 , C07D498/20 , C07D498/22 , A61K31/5365 , A61K45/06 , A61K9/00 , A61K31/519 , A61K31/551
摘要： The present invention is directed to 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 of the formula: or a pharmaceutically acceptable salt or stereoisomer thereof, and pharmaceutical compositions comprising the same. The present invention has HIV integrase inhibitory activity.
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![Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-α]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides](/abs-image/US/2014/07/15/US08778943B2/abs.jpg.150x150.jpg)
3.发明授权Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-α]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides 有权取代的10-羟基-9,11-二氧代-2,3,4a，5,9,11,13,13a-八氢-1H-吡啶并[1,2-α]吡咯并[1'，2'：3,4 ]咪唑并[1,2-d]吡嗪-8-甲酰胺公开(公告)号：US08778943B2
公开(公告)日：2014-07-15
申请号：US13763174
申请日：2013-02-08
申请人： Shionogi & Co., Ltd.
IPC分类号： A61K31/4985 , C07D241/36
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 class of substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides useful as anti-HIV agents. The compounds have the formula (I-1-1): wherein ring A is an optionally substituted hexahydro-1H-pyrrolo[1,2-c]-imidazole; R14 and RX are independently hydrogen or optionally substituted lower alkyl; R3 is selected from various groups; R1 is hydrogen or lower alkyl; R is halogen; m is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及一类取代的10-羟基-9,11-二氧代-2,3,4a，5,9,11,13,13a-八氢-1H-吡啶并[1,2-a]吡咯并[ 1'，2'：3,4]咪唑并[1,2-d]吡嗪-8-甲酰胺，其可用作抗HIV剂。 化合物具有式（I-1-1）：其中环A是任选取代的六氢-1H-吡咯并[1,2-c] - 咪唑; R 14和RX独立地为氢或任选取代的低级烷基; R3选自不同的组; R1是氢或低级烷基; R是卤素; m为0,1,2或3; 或其药学上可接受的盐。
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![Prodrugs of (4aS, 13ar)-N-[(2,4-difluorophenyl)methyl]-10-hydroxy-9-11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1′,2′:3:4]imidazo[1,2-d]pyrazine-8-carboxamide and their use in the treatment of HIV infection](/abs-image/US/2014/04/08/US08691823B2/abs.jpg.150x150.jpg)
4.发明授权Prodrugs of (4aS, 13ar)-N-[(2,4-difluorophenyl)methyl]-10-hydroxy-9-11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1′,2′:3:4]imidazo[1,2-d]pyrazine-8-carboxamide and their use in the treatment of HIV infection 有权（4aS，13ar）-N - [（2,4-二氟苯基）甲基] -10-羟基-9-11-二氧代-2,3,4a，5,9,11,13,13a-八氢-1H- - 吡咯并[1,2-a]吡咯并[1'，2'：3：4]咪唑并[1,2-d]吡嗪-8-甲酰胺及其在治疗HIV感染中的用途公开(公告)号：US08691823B2
公开(公告)日：2014-04-08
申请号：US13770336
申请日：2013-02-19
IPC分类号： A61K31/495
CPC分类号： C07D471/14
摘要： The present invention features compounds of formula (I) for the treatment or prevention of HIV infection and for the treatment of AIDS and ARC.
摘要翻译： 本发明的特征在于式（I）化合物用于治疗或预防HIV感染和用于治疗AIDS和ARC。
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![Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1′,2′:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having HIV integrase inhibitory activity](/abs-image/US/2022/03/08/US11267823B2/abs.jpg.150x150.jpg)
公开(公告)号：US11267823B2
公开(公告)日：2022-03-08
申请号：US16924390
申请日：2020-07-09
IPC分类号： A61K31/4985 , C07D487/22 , C07D498/14 , C07D471/04 , C07D471/14 , C07D498/04 , C07D471/22 , C07D498/20 , C07D498/22 , A61K31/5365 , A61K45/06 , A61K9/00 , A61K31/519 , A61K31/551
摘要： Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1′,2′:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a pharmaceutical composition containing the same, particularly an anti-HIV pharmaceutical composition.
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![Substituted pyrido[1',2':4,5]pyrazino[1,2-a]pyrimidines as HIV integrase inhibitors](/abs-image/US/2016/03/01/US09273065B2/abs.jpg.150x150.jpg)
6.发明授权Substituted pyrido[1',2':4,5]pyrazino[1,2-a]pyrimidines as HIV integrase inhibitors 有权取代的吡啶并[1'，2'：4,5]吡嗪并[1,2-a]嘧啶作为HIV整合酶抑制剂公开(公告)号：US09273065B2
公开(公告)日：2016-03-01
申请号：US14700679
申请日：2015-04-30
IPC分类号： C07D241/38 , C07D498/14 , C07D471/04 , C07D471/14 , C07D498/04 , C07D471/22 , C07D498/20 , C07D498/22
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 class of substituted pyrido[1′2′:4,5]pyrazino[1,2-a]-pyrimidines useful as intermediates in the production of anti-HIV agents. The compounds have the formula (I-24b): wherein Re is one or two halogen; Rz is C1-8alkyl; Rz is hydrogen, C3-6cycloalkyl, heterocyclyl, or C1-8alkyl optionally substituted with hydroxy, C3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C6-14aryl, or amino, wherein said amino may be optionally substituted with —C(O)C1-8alkyl or C1-8alkyl; and P1 is C6-14arylC1-8alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及可用作生产抗HIV剂的中间体的一类取代的吡啶并[1'2'：4,5]吡嗪并[1,2-a] - 嘧啶。 这些化合物具有式（I-24b）：其中Re是一个或两个卤素; Rz为C1-8烷基; R 3是氢，C 3-6环烷基，杂环基或任选被羟基，C 3-6环烷基，烷氧基，杂环基，杂芳基，C 6-14芳基或氨基取代的C 1-8烷基，其中所述氨基可任选地被-C（O） -8-烷基或C 1-8烷基; P1为C6-14芳基C1-8烷基; 或其药学上可接受的盐。
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![1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylic acid of the formula P-6 and/or methyl 1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylate of the formula P-7](/abs-image/US/2014/07/01/US08765965B2/abs.jpg.150x150.jpg)
7.发明授权1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylic acid of the formula P-6 and/or methyl 1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylate of the formula P-7 有权具有式P-6的1-（2,3-二羟基丙基）-4-氧代-3 - [（苯基甲基）氧基] -1,4-二氢-2-吡啶羧酸和/或1-（2,3- 二羟丙基）-4-氧代-3 - [（苯基甲基）氧基] -1,4-二氢-2-吡啶甲酸酯公开(公告)号：US08765965B2
公开(公告)日：2014-07-01
申请号：US14044285
申请日：2013-10-02
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 compounds are intermediates in the preparation of therapeutic agents useful in the treatment of viral infections, particularly HIV infection. The compounds are 1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylic acid of the formula P-6 and/or methyl 1-(2,3-dihydroxypropyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylate of the formula P-7.
摘要翻译： 该化合物是制备用于治疗病毒感染，特别是HIV感染的治疗剂的中间体。 化合物是式P-6的1-（2,3-二羟基丙基）-4-氧代-3 - [（苯基甲基）氧基] -1,4-二氢-2-吡啶甲酸和/或1-（2 （3-羟基丙基）-4-氧代-3 - [（苯基甲基）氧基] -1,4-二氢-2-吡啶甲酸酯。
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