公开(公告)号：US20230338385A1

公开(公告)日：2023-10-26

申请号：US18344406

申请日：2023-06-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David KASS ,  Toru HASHIMOTO ,  Lawrence P. WENNOGLE ,  Joseph HENDRICK ,  Robert DAVIS

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

CPC classification number: A61K31/519 ,  A61P9/04 ,  A61K31/197 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/7056 ,  A61K9/0053 ,  A61K45/06

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：US20210213018A1

公开(公告)日：2021-07-15

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

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：US20210032247A1

公开(公告)日：2021-02-04

申请号：US17072933

申请日：2020-10-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert DAVIS ,  Lawrence P. WENNOGLE

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

Abstract: The invention relates to pharmaceutical compositions comprising 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-1-(4-fluorophenyl)-butan-1-one, 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：US20190298730A1

公开(公告)日：2019-10-03

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：US20180333403A1

公开(公告)日：2018-11-22

申请号：US15986485

申请日：2018-05-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Youyi PENG ,  John TOMESCH ,  Lawrence P. WENNOGLE ,  Qiang ZHANG

IPC: A61K31/454 ,  A61P3/10 ,  A61P13/12

CPC classification number: A61K31/454 ,  A61P3/10 ,  A61P13/12

Abstract: The disclosure relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., diabetes mellitus, chronic kidney disease, acute kidney failure, and reduction of blood glucose levels.

公开(公告)号：US20180200256A1

公开(公告)日：2018-07-19

申请号：US15918955

申请日：2018-03-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Peng LI ,  Sharon MATES ,  Robert DAVIS ,  Lawrence P. WENNOGLE

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

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：US20170360792A1

公开(公告)日：2017-12-21

申请号：US15533527

申请日：2015-12-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG ,  Gretchen SNYDER ,  Lawrence P. WENNOGLE ,  Joseph HENDRICK

IPC: A61K31/519 ,  C07D231/06 ,  C07D231/54 ,  C07D487/04 ,  C07D403/14

CPC classification number: A61K31/519 ,  A61K2300/00 ,  C07D231/06 ,  C07D231/54 ,  C07D403/14 ,  C07D487/04

Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.

公开(公告)号：US20160194326A1

公开(公告)日：2016-07-07

申请号：US15066962

申请日：2016-03-10

Applicant: Intra-Cellular Therapies, Inc.

Inventor： John Charles TOMESCH ,  Peng LI ,  Wei YAO ,  Qiang ZHANG ,  James David BEARD ,  Andrew S. THOMPSON ,  Hua CHENG ,  Lawrence P. WENNOGLE

IPC: C07D471/16 ,  C07D471/04

CPC classification number: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycl fused gamma-carbolines.

Abstract translation: 本发明提供了制备取代的杂环稠合的γ-咔啉的方法，可用于制备它们的中间体和用于制备这种中间体的方法和这种杂环稠合的γ-咔啉。

公开(公告)号：US20140050783A1

公开(公告)日：2014-02-20

申请号：US14066987

申请日：2013-10-30

Applicant: INTRA-CELLULAR THERAPIES INC.

Inventor： Sharon MATES ,  Allen FIENBERG ,  Lawrence P. WENNOGLE

IPC: A61K31/5383 ,  A61K31/4985 ,  C07D471/14 ,  C07D498/14 ,  A61K45/06

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：US20230203037A1

公开(公告)日：2023-06-29

申请号：US18067387

申请日：2022-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Peng LI ,  Lawrence P. WENNOGLE ,  Robert DAVIS

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

CPC classification number: C07D471/16 ,  C07D471/14 ,  A61K45/06 ,  C07B59/002 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18 ,  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.