公开(公告)号：EP2178823A1

公开(公告)日：2010-04-28

申请号：EP08786374.2

申请日：2008-07-24

申请人： Glaxo Group Limited

发明人： CASTIGLIONI, Emiliano ,  DI FABIO, Romano ,  GIANOTTI, Massimo ,  MESIC, Milan ,  PAVONE, Francesca ,  RAST, Slavko ,  STASI, Luigi, Piero

IPC分类号： C07C211/38 ,  A61K31/131 ,  A61P25/00

CPC分类号： C07C211/38 ,  C07C2603/94

摘要： This invention relates to novel spiro cyclopentane derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.

摘要翻译： 本发明涉及式（I）的新型螺环戊烷衍生物或其药学上可接受的盐，用于治疗中枢神经系统（CNS）的疾病和病症，特别是睡眠障碍。

公开(公告)号：EP2094686A1

公开(公告)日：2009-09-02

申请号：EP07820489.8

申请日：2007-09-24

申请人： Glaxo Group Limited

发明人： BERTANI, Barbara ,  BROMIDGE, Steven, Mark ,  GIANOTTI, Massimo ,  PASQUARELLO, Alessandra ,  ZUCCHELLI, Valeria

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D487/08 ,  A61K31/496

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D487/08

摘要： The invention provides compounds of formula (I) wherein R1 is C1-6alkyl, halo or haloC1-6alkyl; R2 is hydrogen or C1-6alkyl; ===== is a single or double bond; each R3 and R4, which may be the same or different, are hydrogen, C1-6alkyl or haloC1-6alkyl; wherein i) when ===== is a double bond p and q are 1, and ii) when ===== is a single bond, p and q are 2, and one of R3 and one of R4 together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R5, which may be the same or different, is C1-6alkyl or halo; or two R5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R6 which may be the same or different, is C1-6alkyl or halo; and m is 0, 1, 2 or 3.

公开(公告)号：EP2421850A1

公开(公告)日：2012-02-29

申请号：EP10715239.9

申请日：2010-04-23

申请人： Glaxo Group Limited

发明人： AMANTINI, David ,  FERRONI, Francesco ,  GIANOTTI, Massimo ,  PAVONE, Francesca ,  DI FABIO, Romano

IPC分类号： C07D401/12 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/44 ,  A61K31/501 ,  A61K31/506 ,  A61P3/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30

CPC分类号： C07D401/12 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

摘要： This invention relates to 3-azabicyclo[4.1.0] heptane derivatives (I) and their use as orexin receptor antagonists.

公开(公告)号：EP2164837A1

公开(公告)日：2010-03-24

申请号：EP08760915.2

申请日：2008-06-12

申请人： Glaxo Group Limited

发明人： GIANOTTI, Massimo ,  LOVELL, Peter, John ,  SERI, Catia ,  TEHAN, Benjamin, Gerald ,  HEER, Jag, Paul

IPC分类号： C07D295/185 ,  A61K31/496 ,  A61P25/18

CPC分类号： C07D295/185

摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof for treating diseases and conditions mediated by positive allosteric modulation of the G- protein coupled metabotropic subtype 5 receptor (mGluR5), such as neurological and psychiatric disorders, for example schizophrenia. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.

摘要翻译： 本发明提供了式（I）化合物或其药学上可接受的盐，用于治疗由G-蛋白偶联的代谢型亚型5受体（mGluR5）的正变构调节介导的疾病和病症，例如神经病学和精神病学疾病，例如精神分裂症 。 此外，本发明涉及含有该衍生物的组合物及其制备方法。