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：US12173004B2

公开(公告)日：2024-12-24

申请号：US18451465

申请日：2023-08-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  A61K45/06 ,  A61P1/00 ,  A61P11/00 ,  A61P25/36 ,  A61P29/00 ,  C07D471/16

Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, 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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US12090155B2

公开(公告)日：2024-09-17

申请号：US18494754

申请日：2023-10-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Kimberly Vanover

IPC: A61K31/4985 ,  A61K9/20 ,  A61K9/48 ,  A61P25/18 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K9/20 ,  A61K9/48 ,  A61P25/18 ,  A61K45/06

Abstract: The disclosure provides methods for the treatment of Bipolar II Disorder, comprising administering to a patient in need thereof, a therapeutically effective amount of lumateperone, in free or pharmaceutically acceptable salt form, optionally in deuterated form.

公开(公告)号：US10117867B2

公开(公告)日：2018-11-06

申请号：US15467867

申请日：2017-03-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/44 ,  A61K31/4985 ,  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.

公开(公告)号：US10077267B2

公开(公告)日：2018-09-18

申请号：US15301912

申请日：2015-04-03

Applicant: Intra-Cellular Therapies, Inc.

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

IPC: C07D471/16 ,  A61K31/4985 ,  C07D471/14 ,  A61K45/06 ,  C07B59/00

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 D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

公开(公告)号：US09956227B2

公开(公告)日：2018-05-01

申请号：US15101874

申请日：2014-12-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

CPC classification number: A61K31/5383 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/5153 ,  A61K31/4985 ,  A61K45/06 ,  A61K2300/00

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：US09168258B2

公开(公告)日：2015-10-27

申请号：US14066987

申请日：2013-10-30

Applicant: INTRA-CELLULAR THERAPIES INC.

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

IPC: A61K31/535 ,  A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  A61K9/48 ,  A61K31/5383 ,  A61K31/44 ,  A61K31/4985 ,  A61K45/06 ,  C07D471/14 ,  C07D498/14

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.

Abstract translation: 公开了使用特定的取代的杂环稠合的γ-咔啉化合物作为药物和包含它们的药物组合物用于治疗涉及5-HT2A，SERT和/或多巴胺D2途径的一种或多种病症。 此外，化合物可以与其它治疗剂组合用于治疗一种或多种睡眠障碍，抑郁症，精神病，运动障碍和/或帕金森病或任何组合。

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。

公开(公告)号：US11844757B2

公开(公告)日：2023-12-19

申请号：US17015883

申请日：2020-09-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  A61P25/00 ,  A61K45/00 ,  A61K45/06 ,  C07D471/16 ,  A61K9/00 ,  A61K9/16 ,  C07D241/40 ,  A61K31/445

CPC classification number: A61K31/4985 ,  A61K9/0019 ,  A61K9/16 ,  A61K31/445 ,  A61K45/00 ,  A61K45/06 ,  A61P25/00 ,  C07D241/40 ,  C07D471/16

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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US11560382B2

公开(公告)日：2023-01-24

申请号：US17124224

申请日：2020-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/16 ,  A61P25/22 ,  A61P25/18 ,  A61P25/24 ,  A61K45/06 ,  C07D471/14 ,  C07B59/00 ,  A61K31/4985

Abstract: This 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 D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.