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1. 发明申请

US20110183939A1 NOVEL PYROLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 失效
标题翻译：新颖的吡咯烷酮衍生物和药物组合物
公开(公告)号：US20110183939A1
公开(公告)日：2011-07-28
申请号：US13121072
申请日：2009-09-24
申请人： Hiroyuki Kai , Yoshiyuki Taoda , Takeshi Endoh , Tohru Horiguchi , Kentaro Asahi , Hiroyuki Tobinaga
发明人： Hiroyuki Kai , Yoshiyuki Taoda , Takeshi Endoh , Tohru Horiguchi , Kentaro Asahi , Hiroyuki Tobinaga
IPC分类号： A61K31/695 , A61K31/4439 , C07D487/04 , A61K31/422 , A61K31/4162 , A61K31/444 , C07F7/02 , A61K31/4245 , C07D413/14 , A61K31/5377
CPC分类号： C07D487/04 , C07D207/38 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/04
摘要： The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist.A compound represented by the formula (I); wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(═O)—, etc.; Z3a and Z3b are taken together ═O or ═S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
摘要翻译：本发明提供了一种新型的P2X3和/或P2X2 / 3受体拮抗剂。由式（I）表示的化合物; 其中Z1是任选保护的羟基等; Z2是-C（= O） - 等; Z3a和Z3b合在一起= = 0或= t为0〜4的整数; R4a和R4b各自独立地为氢或取代或未取代的低级烷基等; m和n各自独立地为0〜2的整数。 k是0或1的整数; 环A是芳族碳环或杂环等; B是芳族碳环环 - 二基或杂环环二基等; R1a和R1b各自独立地为卤素，羟基，取代或未取代的低级烷基等; R2是取代或未取代的烷基等; R3是取代或未取代的烷基，取代或未取代的芳基或取代或未取代的杂环基等; 或其药学上可接受的盐或其溶剂合物。

2. 发明授权

US08575197B2 Pyrolinone derivative and pharmaceutical composition comprising the same 失效
标题翻译：吡罗啉酮衍生物及其组合物
公开(公告)号：US08575197B2
公开(公告)日：2013-11-05
申请号：US13121072
申请日：2009-09-24
申请人： Hiroyuki Kai , Yoshiyuki Taoda , Takeshi Endoh , Kentaro Asahi , Hiroyuki Tobinaga
发明人： Hiroyuki Kai , Yoshiyuki Taoda , Takeshi Endoh , Kentaro Asahi , Hiroyuki Tobinaga
IPC分类号： A61K31/4418 , A61K31/443 , A61K31/4439 , A61K31/422 , A61K31/4245 , A61K31/402 , A61K31/4025 , C07D207/38 , C07D271/06 , C07D261/08 , C07D409/10 , C07D403/14 , C07D413/14 , C07D401/04
CPC分类号： C07D487/04 , C07D207/38 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/04
摘要： The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist.A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(═O)—, etc.; Z3a and Z3b are taken together ═O or ═S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
摘要翻译：本发明提供了一种新型的P2X3和/或P2X2 / 3受体拮抗剂。由式（I）表示的化合物：其中Z 1任选被保护的羟基等; Z2是-C（= O） - 等; Z3a和Z3b在一起= O或= S; t为0〜4的整数; R4a和R4b各自独立地为氢或取代或未取代的低级烷基等; m和n各自独立地为0〜2的整数。 k是0或1的整数; 环A是芳族碳环或杂环等; B是芳族碳环环 - 二基或杂环环二基等; R1a和R1b各自独立地为卤素，羟基，取代或未取代的低级烷基等; R2是取代或未取代的烷基等; R3是取代或未取代的烷基，取代或未取代的芳基或取代或未取代的杂环基等; 或其药学上可接受的盐或其溶剂合物。

3. 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。

4. 发明申请

US20120184734A1 SUBSTITUTED POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE 有权
标题翻译：取代的多环碳酰胺衍生物
公开(公告)号：US20120184734A1
公开(公告)日：2012-07-19
申请号：US13378334
申请日：2010-06-14
申请人： Toshiyuki Akiyama , Kenji Takaya , Makoto Kawai , Yoshiyuki Taoda , Minako Mikamiyama , Kenji Morimoto , Chika Kageyama , Kenji Tomita , Hidenori Mikamiyama , Naoyuki Suzuki
发明人： Toshiyuki Akiyama , Kenji Takaya , Makoto Kawai , Yoshiyuki Taoda , Minako Mikamiyama , Kenji Morimoto , Chika Kageyama , Kenji Tomita , Hidenori Mikamiyama , Naoyuki Suzuki
IPC分类号： C07D498/14 , C07D471/14 , C07D471/04
CPC分类号： C07D471/04 , A61K31/53 , C07D471/14 , C07D487/14 , C07D487/20 , C07D498/14
摘要： This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
摘要翻译：本发明提供具有抗病毒活性的化合物，特别是抑制流感病毒的活性，更优选提供具有cap依赖性内切核酸酶抑制活性的取代的3-羟基-4-吡啶酮衍生物。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明申请

US20100204237A1 Hydroxypyrimidinone derivatives having inhibitory activity against HIV integrase 审中-公开
公开(公告)号：US20100204237A1
公开(公告)日：2010-08-12
申请号：US12662515
申请日：2010-04-21
申请人： Hidenori Mikamiyama , Minamo Iwata , Yoshiyuki Taoda
发明人： Hidenori Mikamiyama , Minamo Iwata , Yoshiyuki Taoda
IPC分类号： A61K31/506 , A61K31/519 , C07D487/04 , C07D403/04 , C07D413/04 , C07D417/14 , C07D413/14
CPC分类号： C07D417/14 , C07D401/04 , C07D405/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D487/04
摘要： Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S(═O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.

10. 发明授权

US08846929B2 Substituted-quinoxaline-type piperidine compounds and the uses thereof 有权
标题翻译：取代的喹喔啉型哌啶化合物及其用途
公开(公告)号：US08846929B2
公开(公告)日：2014-09-30
申请号：US12712042
申请日：2010-02-24
申请人： Kouki Fuchino , R. Richard Goehring , Bin Shao , Yoshiyuki Taoda , Naoki Tsuno , John William Frank Whitehead , Jiangchao Yao
发明人： Kouki Fuchino , R. Richard Goehring , Bin Shao , Yoshiyuki Taoda , Naoki Tsuno , John William Frank Whitehead , Jiangchao Yao
IPC分类号： C07D295/00
CPC分类号： C07D451/14 , A61K31/498 , C07D401/04 , C07D401/14 , C07D451/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D498/08 , C07D519/00
摘要： The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
摘要翻译：本发明涉及取代的喹喔啉型哌啶化合物，包含有效量的取代的喹喔啉型哌啶化合物的组合物和治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的取代的喹喔啉型哌啶化合物。

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