公开(公告)号：US11839614B2

公开(公告)日：2023-12-12

申请号：US16966818

申请日：2019-01-31

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David Kass ,  Toru Hashimoto ,  Lawrence Wennogle ,  Joseph Hendrick ,  Robert Davis

IPC: A61K31/519 ,  A61P9/04 ,  A61K31/41 ,  A61K31/7056 ,  A61K9/00 ,  A61K45/06 ,  A61K31/197 ,  A61K31/216 ,  A61K31/4178 ,  A61K31/04

CPC classification number: A61K31/519 ,  A61K9/0053 ,  A61K31/04 ,  A61K31/197 ,  A61K31/216 ,  A61K31/4178 ,  A61K31/7056 ,  A61K45/06 ,  A61P9/04

Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.

公开(公告)号：US09616061B2

公开(公告)日：2017-04-11

申请号：US14885813

申请日：2015-10-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Allen Fienberg ,  Lawrence Wennogle

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

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K31/198 ,  A61K31/44 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/14 ,  C07D498/14

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.

公开(公告)号：USRE48839E1

公开(公告)日：2021-12-07

申请号：US16784112

申请日：2020-02-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Allen Fienberg ,  Lawrence Wennogle

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

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.

公开(公告)号：US11124514B2

公开(公告)日：2021-09-21

申请号：US16585251

申请日：2019-09-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/50 ,  A61K31/13 ,  A61K31/445 ,  A61K31/44 ,  A61K31/27 ,  C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  A61P25/28 ,  C07D471/16

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.

公开(公告)号：US20150072964A1

公开(公告)日：2015-03-12

申请号：US14394469

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 ,  A61K45/06

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

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.

Abstract translation: 使用特定的取代的杂环稠合的γ-咔啉化合物作为药物用于治疗激动，侵袭行为，创伤后应激障碍或冲动控制障碍。

公开(公告)号：US10183023B2

公开(公告)日：2019-01-22

申请号：US15406346

申请日：2017-01-13

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence Wennogle

IPC: A61K31/519 ,  A61K31/527 ,  A61K31/53 ,  A61K31/517 ,  G01N33/84

Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

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：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。

公开(公告)号：US09598426B2

公开(公告)日：2017-03-21

申请号：US14777446

申请日：2014-03-13

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Jun Zhao ,  Lawrence 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 and their use as pharmaceuticals, and pharmaceutical compositions comprising them.

公开(公告)号：US20150079172A1

公开(公告)日：2015-03-19

申请号：US14394467

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Peng Li ,  Lawrence Wennogle ,  Richard A. Lerner

IPC: C07D471/14

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, their prodrugs, 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.

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特定取代的杂环稠合的γ-咔啉及其前药，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。