公开(公告)号：US20200247805A1

公开(公告)日：2020-08-06

申请号：US16649515

申请日：2018-09-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. WENNOGLE ,  Peng LI ,  Edwin ARET

IPC: C07D471/16

Abstract: The disclosure provides new, stable, pharmaceutically acceptable hydrochloride salt forms of 1-(4-fluoro-phenyl)-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)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20190292185A1

公开(公告)日：2019-09-26

申请号：US16439361

申请日：2019-06-12

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

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 heterocycle fused gamma-carbolines.

公开(公告)号：US20180280396A1

公开(公告)日：2018-10-04

申请号：US15997438

申请日：2018-06-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/519 ,  A61K31/495

CPC classification number: A61K31/519 ,  A61K31/495 ,  Y02A50/463

Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.

公开(公告)号：US20170217975A1

公开(公告)日：2017-08-03

申请号：US15502455

申请日：2015-08-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG ,  Jun ZHAO ,  Lawrence P. WENNOGLE

IPC: C07D487/14

CPC classification number: C07D487/14

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：US20160324860A1

公开(公告)日：2016-11-10

申请号：US15110640

申请日：2015-01-08

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Joseph HENDRICK ,  Jennifer O'BRIEN ,  Gretchen SNYDER ,  Peng LI ,  Lawrence P. WENNOGLE

IPC: A61K31/519 ,  A61K9/00 ,  A61K31/53

CPC classification number: A61K31/519 ,  A61K9/0048 ,  A61K31/53 ,  A61K45/06 ,  C07D487/04 ,  C07D487/14 ,  A61K2300/00

Abstract: The present invention relates to a product comprising a PDE1 inhibitor and a PDE2 inhibitor, in free or salt form, pharmaceutical compositions comprising them and their use as pharmaceuticals for the treatment of cAMP and/or cGMP related disorders.

Abstract translation: 本发明涉及包含游离或盐形式的PDE1抑制剂和PDE2抑制剂的产品，其包含它们的药物组合物及其作为治疗cAMP和/或cGMP相关疾病的药物的用途。

公开(公告)号：US20160031895A1

公开(公告)日：2016-02-04

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

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：US20140364609A1

公开(公告)日：2014-12-11

申请号：US14323545

申请日：2014-07-03

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 heterocycle 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：US20140005155A1

公开(公告)日：2014-01-02

申请号：US14020016

申请日：2013-09-06

Applicant: INTRA-CELLULAR THERAPIES, INC

Inventor： Peng LI ,  Jun ZHAO ,  Hailin ZHENG ,  Lawrence P. WENNOGLE

IPC: C07D487/14 ,  A61K45/06 ,  A61K31/5025

CPC classification number: C07D487/14 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/529 ,  A61K31/5575 ,  A61K45/06 ,  C07D487/04

Abstract: Optionally substituted 3-(thio, sulfinyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract translation: 任选取代的3-（硫代亚磺酰基或磺酰基）-7,8-二氢 - （1H或2H） - 咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4（5H） - 酮或 取代的3-（硫代亚磺酰基或磺酰基）-7,8,9-三氢 - （1H或2H） - 嘧啶并[1,2-a]吡唑并[4,3-e]嘧啶-4（5H） - 酮化合物 或式（I）的化合物，其制备方法，它们作为药物的用途以及包含它们的药物组合物。

公开(公告)号：US20240252491A1

公开(公告)日：2024-08-01

申请号：US18621067

申请日：2024-03-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen SNYDER ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: A61K31/4985 ,  A61K9/00 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/155 ,  A61K31/165 ,  A61K31/197 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/485 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/07 ,  A61P25/24

CPC classification number: A61K31/4985 ,  A61K9/006 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/155 ,  A61K31/165 ,  A61K31/197 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/485 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/07 ,  A61P25/24

Abstract: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A or 5-HT2A/D2 receptor ligand, e.g. lumateperone.

公开(公告)号：US20240041871A1

公开(公告)日：2024-02-08

申请号：US18481170

申请日：2023-10-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

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.