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1. 发明申请

US20120209000A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：US20120209000A1
公开(公告)日：2012-08-16
申请号：US13450784
申请日：2012-04-19
申请人： Brian Alvin JOHNS , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
发明人： Brian Alvin JOHNS , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
IPC分类号： C07D471/22
CPC分类号： C07D471/14
摘要： The present invention is directed to a compound of the formula: The compound is useful as an intermediate for preparing an HIV drug.
摘要翻译：本发明涉及下式的化合物：该化合物可用作制备HIV药物的中间体。

2. 发明授权

US08183372B2 Substituted 9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydor-1H-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazines 有权
标题翻译：取代的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
公开(公告)号：US08183372B2
公开(公告)日：2012-05-22
申请号：US13055046
申请日：2009-07-23
申请人： Brian Alvin Johns , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
发明人： Brian Alvin Johns , Yasunori Aoyama , Hiroshi Yoshida , Yoshiyuki Taoda
IPC分类号： C07D241/36
CPC分类号： C07D471/14
摘要： The present invention is directed to a process for the preparation of a compound of formula 1b which compound is useful as a prodrug of HIV integrase inhibitors and therefore is 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. The process includes the steps of a) brominating a compound of formula P-7 to form a compound of formula P-8, b) treating a compound of formula P-8 with NaIO4 to form a compound of formula P-9, c) reacting a compound of formula P-9 with [(2R)-pyrrolidinylmethyl]amine of formula to form a compound of formula P-10, d) reacting a compound of formula P-10 with 2, 4-difluorobenzylamine to form a compound of formula P-11, e) treating a compound of P-11 with palladium on carbon and ammonium hydroxide to form a compound of formula 1a, and f) treating a compound of formula 1a with NaOH and ethanol to form a compound of formula 1b. The structures of the above mentioned compounds are disclosed in the specification.
摘要翻译：本发明涉及一种制备式1b化合物的方法，该化合物可用作HIV整合酶抑制剂的前药，因此可用于抑制HIV复制，预防和/或治疗HIV感染，和治疗艾滋病和/或ARC。该方法包括以下步骤：a）将式P-7化合物溴化以形成式P-8的化合物，b）用NaIO 4处理式P-8的化合物以形成式P-9的化合物，c）使式P-9的化合物与式的[（2R） - 吡咯烷基甲基]胺反应形成式P-10的化合物，d）使式P-10的化合物与2,4-二氟苄胺反应，形成化合物式P-11，e）用钯碳和氢氧化铵处理P-11化合物以形成式1a化合物，和f）用NaOH和乙醇处理式1a化合物以形成式1b化合物。上述化合物的结构在说明书中公开。

3. 发明申请

US20120115875A1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 有权
标题翻译：具有HIV整合酶抑制活性的多环碳酰胺基衍生物
公开(公告)号：US20120115875A1
公开(公告)日：2012-05-10
申请号：US13352686
申请日：2012-01-18
申请人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
发明人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
IPC分类号： A61K31/4985 , A61P31/18 , C07D498/14
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。

4. 发明授权

US08129385B2 Substituted 5-hydroxy-3,4,6,9,9a, 10-hexanhydro-2h-1-oxa04a,8a-diaza-anthracene-6,10-dioness 有权
标题翻译：取代的5-羟基-3,4,6,9,9a，10-六氢-2h-1-氧杂-4a，8a-二氮杂 - 蒽-6,10-二酮
公开(公告)号：US08129385B2
公开(公告)日：2012-03-06
申请号：US11919386
申请日：2006-04-28
申请人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
发明人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
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 class of substituted 5-hydroxy-3,4,6,9,9a,10-hexahydro-2H-1-oxa-4a,8a-diaza-anthracene-6,10-diones useful as anti-HIV agents. The compounds have the formula: Z═O; R20, R21, R22, R23, R24 and R25 independently are hydrogen, C1-C8 alkyl, (C6-C14)aryl-(C1-C8)alkyl, C6-C14 aryl, or alkoxy; the stereochemistry of an asymmetric carbon represented by * shows R- or S-configuration, or a mixture thereof; RX is hydrogen; R14 is hydrogen or optionally substituted lower alkyl; R3 is hydrogen; R1 is hydrogen or lower alkyl; R is halogen; and m is 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及一类用作抗体的取代的5-羟基-3,4,6,9,9a，10-六氢-2H-1-氧杂-4a，8a-二氮杂 - 蒽-6,10-二酮 -HIV代理化合物具有下式：Z = O; R 20，R 21，R 22，R 23，R 24和R 25独立地是氢，C 1 -C 8烷基，（C 6 -C 14）芳基 - （C 1 -C 8）烷基，C 6 -C 14芳基或烷氧基; 由*表示的不对称碳的立体化学显示R-或S-构型，或其混合物; RX是氢; R 14是氢或任选取代的低级烷基; R3是氢; R1是氢或低级烷基; R是卤素; m为1,2或3; 或其药学上可接受的盐。

5. 发明授权

US08410103B2 (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
标题翻译：（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
申请人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
发明人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
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。

6. 发明申请

US20090318421A1 Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity 有权
标题翻译：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
申请人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
发明人： Brian Alvin Johns , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
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。

7. 发明申请

US20110282055A1 SYNTHESIS OF CARBAMOYLPYRIDONE HIV INTEGRASE INHIBITORS AND INTERMEDIATES 有权
标题翻译：卡巴酰亚胺艾滋病综合抑制剂和中间体的合成
公开(公告)号：US20110282055A1
公开(公告)日：2011-11-17
申请号：US13128992
申请日：2009-12-08
申请人： Hiroshi Yoshida , Yoshiyuki Taoda , Brian Johns , Takashi Kawasuji , Daiki Nagamatsu
发明人： Hiroshi Yoshida , Yoshiyuki Taoda , Brian Johns , Takashi Kawasuji , Daiki Nagamatsu
IPC分类号： C07D498/14 , C07D471/22
CPC分类号： C07D498/14 , A61K31/351 , A61K31/4412 , C07D213/803 , C07D213/81 , C07D471/22 , C07D487/22 , Y02P20/55
摘要： A synthesis approach providing an early ring attachment via a bromination to compound 1-1 yielding compound II-II whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
摘要翻译：合成方法通过溴化得到化合物1-1的早期环附着，得到化合物II-II，由此可以合成最终产物例如AA。特别地，在产生附加环Q之前附着了含2,4-二氟苯基的侧链。

8. 发明授权

US08624023B2 Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates 有权
标题翻译：氨基甲酰吡啶酮的合成及其中间体
公开(公告)号：US08624023B2
公开(公告)日：2014-01-07
申请号：US13128992
申请日：2009-12-08
申请人： Hiroshi Yoshida , Yoshiyuki Taoda , Brian Johns , Takashi Kawasuji , Daiki Nagamatsu
发明人： Hiroshi Yoshida , Yoshiyuki Taoda , Brian Johns , Takashi Kawasuji , Daiki Nagamatsu
IPC分类号： C07D498/14 , C07D471/22
CPC分类号： C07D498/14 , A61K31/351 , A61K31/4412 , C07D213/803 , C07D213/81 , C07D471/22 , C07D487/22 , Y02P20/55
摘要： A synthesis approach providing an early ring attachment via a bromination to compound I-I yielding compound II-II: whereby a final product such as AA: can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
摘要翻译：通过溴化将早期环连接提供给化合物I-1的合成方法，得到化合物II-II：由此可以合成最终产物如AA。特别地，在产生附加环Q之前附着了含2,4-二氟苯基的侧链。

9. 发明申请

US20080161271A1 Bicyclic Carbamoylpyridone Derivative Having Hiv Integrase Inhibitory Activity 有权
标题翻译：具有Hiv整合酶抑制活性的双环氨甲酰吡哆醇衍生物
公开(公告)号：US20080161271A1
公开(公告)日：2008-07-03
申请号：US11884686
申请日：2006-02-20
申请人： Hiroshi Yoshida , Takashi Kawasuji , Yoshiyuki Taoda
发明人： Hiroshi Yoshida , Takashi Kawasuji , Yoshiyuki Taoda
IPC分类号： A61K31/675 , C07D241/36 , A61K31/4985 , A61P31/18 , C07D295/00 , A61K31/5377
CPC分类号： C07D471/04 , C07F9/6561
摘要： [Object] Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent. [Solving means] A compound represented by the formula: (wherein Z1 is NR4 (R4 is hydrogen, optionally substituted lower alkyl etc.), O or CH2; Z2 is optionally substituted lower alkylene or optionally substituted lower alkenylene, each may be intervened by a heteroatom group selected from group consisting O, S, SO, SO2, NR5 (R5 is selected independently from the same substituent group of R4)—N═ and ═N—; R1 is hydrogen or lower alkyl; X is a single bond, a heteroatom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted alkyl group etc.)
摘要翻译：本发明提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物和药剂，特别是抗HIV剂。 [解决方案]由下式表示的化合物（其中Z 1是NR 4）（R 4）是氢，任选取代的低级烷基等。），O或CH 2; Z 2是任选取代的低级亚烷基或任选取代的低级亚烯基，各自可以被选自O，S SO，SO 2，NR 5（R 5）独立地选自与R 4相同的取代基，）-N-和-N-; R 1是氢或低级烷基; X是单键，选自O，S，SO，SO 2的杂原子基团; 和NH，或低级亚烷基或低级亚烯基各自可以被杂原子基团插入; R 2是任选取代的芳基; R 3是氢，卤素，羟基，任选取代的烷基等）

10. 发明授权

US07858788B2 Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity 有权
标题翻译：具有HIV整合酶抑制活性的双环氨基甲酰吡啶酮衍生物
公开(公告)号：US07858788B2
公开(公告)日：2010-12-28
申请号：US11884686
申请日：2006-02-20
申请人： Hiroshi Yoshida , Takashi Kawasuji , Yoshiyuki Taoda
发明人： Hiroshi Yoshida , Takashi Kawasuji , Yoshiyuki Taoda
IPC分类号： C07D413/00 , C07D471/00
CPC分类号： C07D471/04 , C07F9/6561
摘要： Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and an agent, particularly an anti-HIV agent.A compound represented by the formula: (wherein Z1 is NR4 (R4 is hydrogen, optionally substituted lower alkyl etc.), O or CH2; Z2 is optionally substituted lower alkylene or optionally substituted lower alkenylene, each may be intervened by a heteroatom group selected from group consisting O, S, SO, SO2, NR5 (R5 is selected independently from the same substituent group of R4) —N═ and ═N—; R1 is hydrogen or lower alkyl; X is a single bond, a heteroatom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene each may be intervened by the heteroatom group; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted alkyl group etc.)
摘要翻译：是提供具有抗病毒活性，特别是HIV整合酶抑制活性的新型化合物和药剂，特别是抗HIV剂。由下式表示的化合物（其中Z 1为NR 4（R 4为氢，任选取代的低级烷基等），O或CH 2; Z 2为任选取代的低级亚烷基或任选取代的低级亚烯基，各自可以被选自来自由O，S，SO，SO 2，NR 5组成的基团（R 5独立地选自与R 4相同的取代基组）-N =和N - ; R 1是氢或低级烷基; X是单键， O，S，SO，SO 2和NH，或低级亚烷基或低级亚烯基各自可以被杂原子基团插入; R2是任选取代的芳基; R 3是氢，卤素，羟基，任选取代的烷基等）

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