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：US20210009592A1

公开(公告)日：2021-01-14

申请号：US17040892

申请日：2019-03-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert DAVIS

IPC: C07D471/16 ,  A61K9/00 ,  C07B59/00

Abstract: The invention relates to particular deuterated 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：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：US20170283417A1

公开(公告)日：2017-10-05

申请号：US15629481

申请日：2017-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

CPC classification number: C07D471/16 ,  A61K9/4825 ,  A61K9/4891 ,  A61K9/5031 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, 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.

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：US20190218219A1

公开(公告)日：2019-07-18

申请号：US16244796

申请日：2019-01-10

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

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：US20190071445A1

公开(公告)日：2019-03-07

申请号：US16056143

申请日：2018-08-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, 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.

公开(公告)号：US20250092045A1

公开(公告)日：2025-03-20

申请号：US18968542

申请日：2024-12-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert E. DAVIS

IPC: C07D471/16 ,  A61K9/16

Abstract: The invention relates to a particular substituted heterocycle fused gamma-carboline, in free, or 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), and/or pathways involving the dopamine D1 and D2 receptor signaling system.

公开(公告)号：US20240327409A1

公开(公告)日：2024-10-03

申请号：US18741740

申请日：2024-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG

IPC: C07D471/16 ,  C07D519/00

CPC classification number: C07D471/16 ,  C07D519/00

Abstract: The present invention provides improved 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：US20230271962A1

公开(公告)日：2023-08-31

申请号：US18314785

申请日：2023-05-09

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

CPC classification number: C07D471/16 ,  C07D471/14 ,  A61K9/5031 ,  A61K9/4825 ,  A61K9/4891 ,  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-ol, 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.