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。

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。

公开(公告)号：US20090143356A1

公开(公告)日：2009-06-04

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： A61K31/553 ,  C07D487/04 ,  A61K31/53 ,  C07D413/06 ,  C07D498/14 ,  C07D498/12 ,  A61K31/5383 ,  A61K31/5377 ,  C07D487/14 ,  A61K31/551

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）