公开(公告)号：US09630971B2

公开(公告)日：2017-04-25

申请号：US14900589

申请日：2014-06-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  INTRA-CELLULAR THERAPIES, INC.

Inventor： Takashi Abe ,  Graham Buckton ,  Robert Davis ,  Mark Hooper ,  Peng Li ,  Hideaki Maruyama ,  Masahiro Takasuga ,  Lawrence P. Wennogle ,  Yuhei Yamamoto ,  Hironori Yamashita

IPC: A61K31/519 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.

公开(公告)号：US09428506B2

公开(公告)日：2016-08-30

申请号：US14394467

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Peng Li ,  Lawrence Wennogle ,  Kimberly Vanover

IPC: A61K31/4985 ,  C07D241/38 ,  C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  C07D471/16 ,  A61K31/445

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/16 ,  A61K2300/00

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, of Formula I, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems, such as disease of the central nervous system.

Abstract translation: 本发明涉及如本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式的式I的特定取代的杂环稠合的γ-咔啉，其药物组合物，以及用于治疗涉及5- HT2A受体，血清素转运蛋白（SERT）和/或涉及多巴胺D2受体信号传导系统的途径，例如中枢神经系统疾病。

公开(公告)号：US20150259353A1

公开(公告)日：2015-09-17

申请号：US14409988

申请日：2013-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Lawrence P. Wennogle ,  Robert Davis ,  Graham Buckton ,  Mark Hooper

IPC: C07D487/14 ,  C07C57/15 ,  C07C55/02 ,  C07C309/04

CPC classification number: C07D487/14 ,  C07B2200/13 ,  C07C55/02 ,  C07C57/15 ,  C07C309/04

Abstract: The present invention relates to acid addition salt and salt crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, composition comprising the same and the method of making and using such salt and crystal

Abstract translation: 本发明涉及（6aR，9aS）-5,6a，7,8,9,9a-六氢-5-甲基-3-（苯基氨基）-2 - （（4-（6 - 氟吡啶-2-基）苯基）甲基） - 环戊并[4,5]咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4（2H） - 酮，包含该组合物的组合物和方法 制作和使用这种盐和水晶

公开(公告)号：US20150080404A1

公开(公告)日：2015-03-19

申请号：US14394470

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Kimberly Vanover ,  Lawrence Wennogle

IPC: C07D471/16 ,  A61K31/4985 ,  A61K31/445

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/16 ,  A61K2300/00

Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.

Abstract translation: 本发明涉及如本文所述的特定取代的杂环稠合的γ-咔啉在游离的，药学上可接受的盐或前药形式中的用途，以及包含任选与一种或多种试剂组合的药物组合物用于预防或治疗一种 或更多与痴呆症患者相关的疾病，特别是患有痴呆患者的行为或情绪障碍（例如，激动/侵略），精神病，抑郁症和睡眠障碍。