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    • 2. 发明申请
    • GLUCOPYRANOSIDE COMPOUND
    • 葡萄糖苷化合物
    • US20110105424A1
    • 2011-05-05
    • US13005757
    • 2011-01-13
    • Sumihiro NOMURAEiji KawanishiKiichiro Ueta
    • Sumihiro NOMURAEiji KawanishiKiichiro Ueta
    • A61K31/70C07H19/00A61P3/10A61P17/02A61P7/00A61P9/00A61P3/04
    • C07H19/048A61K45/06C07D405/04C07D409/04C07D409/10C07H19/06
    • A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
    • 下式的化合物:其中环A和环B是:(1)环A是任选取代的不饱和单环杂环,环B是任选取代的不饱和单环杂环,任选取代的不饱和稠合杂双环,或 任选取代的苯环,(2)环A是任选取代的苯环,环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环,或(3)环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环,任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - (CH 2)n - (n为1或2); 或其药学上可接受的盐,或其前药。
    • 10. 发明申请
    • AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE
    • 含有硝酸的六元环化合物及其用途
    • US20110166135A1
    • 2011-07-07
    • US13062841
    • 2009-09-09
    • Hiroshi MorimotoToshiaki SakamotoToshiyuki HimiyamaEiji KawanishiTakehiko Matsumura
    • Hiroshi MorimotoToshiaki SakamotoToshiyuki HimiyamaEiji KawanishiTakehiko Matsumura
    • A61K31/5377C07D401/14C07D487/04C07D413/14A61K31/517A61K31/506A61K31/497A61K31/519A61P25/18A61P25/24A61P25/22A61P25/16A61P25/28
    • C07D401/14C07D401/12C07D403/12C07D403/14C07D405/12
    • 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.
    • 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。