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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

US08188271B2 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：US08188271B2
公开(公告)日：2012-05-29
申请号：US12084128
申请日：2006-10-26
申请人： Hiroshi Yoshida , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
发明人： Hiroshi Yoshida , Takashi Kawasuji , Teruhiko Taishi , Yoshiyuki Taoda
IPC分类号： C07D487/04 , C07D471/04 , A61K31/53 , A61P31/18
CPC分类号： C07F9/6561 , C07D471/04 , C07D471/14 , C07D471/20 , C07D498/14
摘要： Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line. When B2 is NR22, R4 and R22 may be connected together to form an optionally substituted heterocycle;When B2 is CHR21, R4 and R21 may be connected together to form an optionally substituted heterocycle.Alternatively, B1 and B2 are independently C, CR23 or N and, in this case, B1 and B2 may be taken together to form a heterocycle.R20, R21, R22 and R23 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl etc.)
摘要翻译：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，以及药物组合物，特别是抗HIV剂。（其中R1为氢或低级烷基; X为低级亚烷基等; R2为任选取代的芳基; R3为氢，卤素，羟基，任选取代的低级烷基等; R4为氢，任选取代的低级烷基，任选取代的环烷基，任选取代的环烷基低级烷基，任选取代的芳基，任选取代的芳基低级烷基，任选取代的杂环基，任选取代的杂环低级烷基等;虚线表示存在或不存在键; B1和B2使得任何一个它们是CR20R21，另一个是NR22，在这种情况下没有虚线，当B2是NR22时，R4和R22可以连接在一起形成任选取代的杂环;当B2是CHR21时，R4和R21可以是连接在一起形成任选取代的杂环，或者B1和B2独立地为C，CR23或N，在这种情况下，B1和B2可以一起形成杂环R 20，R 21，R 22 和R 23独立地是氢，任选取代的低级烷基，任选取代的环烷基，任选取代的环烷基低级烷基等）

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