公开(公告)号：US20170226117A1

公开(公告)日：2017-08-10

申请号：US15502144

申请日：2015-08-07

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Peng LI ,  Hailin ZHENG ,  Jun Zhao ,  Lawrence P. Wennogle

IPC: C07D487/14 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

公开(公告)号：US20170190703A9

公开(公告)日：2017-07-06

申请号：US15110613

申请日：2015-01-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Qiang Zhang ,  Youyi Peng ,  Peng Li ,  J. David Beard ,  Lawrence P. Wennogle ,  John Tomesch

IPC: C07D487/04 ,  C07D277/82 ,  C07D235/30 ,  C07B59/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D235/30 ,  C07D277/82 ,  C07D401/12

Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.

公开(公告)号：US09556186B2

公开(公告)日：2017-01-31

申请号：US14731233

申请日：2015-06-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Jun Zhao ,  Lawrence P. Wennogle

IPC: C07D487/14 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5575

CPC classification number: A61K31/519 ,  A61K31/5575 ,  A61K31/57 ,  A61K45/06 ,  C07D487/14

Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract translation: 提供式I的PDE1抑制剂，其制备方法，其作为药物的用途，以及包含它们的药物组合物。

公开(公告)号：US20160326179A1

公开(公告)日：2016-11-10

申请号：US15110613

申请日：2015-01-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Qiang Zhang ,  Youyi Peng ,  Peng Li ,  J. David Beard ,  Lawrence P. Wennogle ,  John Tomesch

IPC: C07D487/04 ,  C07D277/82 ,  C07D235/30 ,  C07B59/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D235/30 ,  C07D277/82 ,  C07D401/12

Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.

Abstract translation: 本发明提供新型化合物，包含所述化合物的组合物和用于抑制CK1的方法以及治疗CK1相关病症如阿尔茨海默氏病的方法，包括向有需要的患者施用治疗有效量的CK1抑制剂。

公开(公告)号：US20160145261A1

公开(公告)日：2016-05-26

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 ,  Hinori YAMASHITA

IPC: 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.

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，以及制备和使用这种晶体的方法。

公开(公告)号：US12264160B2

公开(公告)日：2025-04-01

申请号：US18327607

申请日：2023-06-01

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/437 ,  A61K9/48 ,  A61K9/50 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22

Abstract: The invention relates to pharmaceutical compositions comprising compounds of Formula Q: wherein W is —N(CH3)—, and Y is —C(O)—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

公开(公告)号：US11291666B2

公开(公告)日：2022-04-05

申请号：US16332750

申请日：2017-09-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen Snyder ,  Lawrence P. Wennogle ,  Jennifer O'Brien ,  Joseph Hendrick

IPC: A61K31/517 ,  A61K31/519 ,  A61P27/02 ,  A61P25/28 ,  A61P37/06 ,  A61K31/4015 ,  A61K45/06

Abstract: The disclosure provides the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment and prophylaxis of diseases or disorders characterized by inflammation, e.g., neuroinflammation, including methods of treatment and pharmaceutical compositions for use therein.

公开(公告)号：US11026951B2

公开(公告)日：2021-06-08

申请号：US16507956

申请日：2019-07-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/5383 ,  A61K9/00 ,  A61K9/51 ,  A61K31/4985 ,  A61K45/06

Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.

公开(公告)号：US10960010B2

公开(公告)日：2021-03-30

申请号：US16443240

申请日：2019-06-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/5383 ,  A61K31/4985 ,  A61K9/00 ,  A61K45/06 ,  A61K9/51

Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.

公开(公告)号：US10702522B2

公开(公告)日：2020-07-07

申请号：US16165832

申请日：2018-10-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Allen Fienberg ,  Lawrence P. Wennogle

IPC: A61K31/4985 ,  A61K31/44 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/14 ,  C07D498/14 ,  A61K9/00 ,  A61K31/198

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.