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1. 发明申请

US20110166135A1 AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE 审中-公开
标题翻译：含有硝酸的六元环化合物及其用途
公开(公告)号：US20110166135A1
公开(公告)日：2011-07-07
申请号：US13062841
申请日：2009-09-09
申请人： Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
发明人： Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
IPC分类号： A61K31/5377 , C07D401/14 , C07D487/04 , C07D413/14 , A61K31/517 , A61K31/506 , A61K31/497 , A61K31/519 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/28
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12
摘要： The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I0] wherein: X1, X2 and X3 each independently are N or CH, and at least two of X1, X2 and X3 are N; A is *—CH═CH—, *—C(Alk)=CH—, *—CH2—CH2— or *—O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) —O—R2 wherein R2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R1 is not quinoxalinyl or quinolyl.
摘要翻译：本发明提供具有优异的PDE10抑制活性的芳香族含氮6元环化合物。本发明涉及由下式[I0]表示的含芳族含氮的6元环化合物或其药学上可接受的盐，其制备方法以及所述化合物用于PDE10抑制剂的用途和药物组合物包括所述化合物作为活性成分：式[I0]其中：X1，X2和X3各自独立地为N或CH，X1，X2和X3中的至少两个为N; A是* -CH = CH-，* -C（Alk）= CH-，* -CH2-CH2-或* -O-CH2-（*是与R1的键）; Alk是低级烷基; 环B是任选取代的含氮脂族杂环基; R1是任选取代的含氮杂环基团，其含氮杂环部分是选自喹喔啉基，喹啉基，异喹啉基，喹唑啉基，吡嗪基，嘧啶基及其部分与5至6位稠合的部分，元环脂族环; Y0是选自下列（1）至（5）的基团：（1）任选取代的苯基或任选取代的芳族单环5至6元杂环基; （2）任选取代的氨基羰基; （3）任选取代的氨基低级烷基; （4）-O-R2，其中R2是氢，任选取代的低级烷基，低级环烷基，脂族单环5至6元杂环基或式[AA]; （5）单取代或二取代氨基; 条件是当Y 0是单取代或二取代的氨基时，R 1的含氮杂环部分不是喹喔啉基或喹啉基。

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