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：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：US20250101029A1

公开(公告)日：2025-03-27

申请号：US18847121

申请日：2023-03-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert E. DAVIS ,  Gretchen SNYDER ,  Allen A. FIENBERG

IPC: C07D487/14 ,  A61K31/4985

Abstract: The invention relates to a particular enantiomer of a substituted heterocycle fused gamma-carboline, 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, and pathways involving the dopamine D1 and D2 receptor signaling system.

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：US20240279228A1

公开(公告)日：2024-08-22

申请号：US18567743

申请日：2022-06-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D471/16 ,  A61K31/4985

CPC classification number: C07D471/16 ,  A61K31/4985

Abstract: The disclosure provides new salts, crystals and co-crystal forms of particular substituted heterocycle fused gamma-carbolines, as described herein, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20240024334A1

公开(公告)日：2024-01-25

申请号：US18481168

申请日：2023-10-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

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：US20230355625A1

公开(公告)日：2023-11-09

申请号：US17780660

申请日：2020-11-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Robert DAVIS ,  Peng LI

IPC: A61K31/519 ,  A61K45/06 ,  A61P25/28

CPC classification number: A61K31/519 ,  A61K45/06 ,  A61P25/28

Abstract: The present disclosure relates to inhibitors of phosphodiesterase 1 (PDE1) useful for the engagement with the central nervous system. The disclosure further relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of a condition, disease or disorder associated with the dopamine D1 receptor intracellular pathway, e.g., a condition, disease or disorder characterized by a deficit in attention, cognition, memory and/or inhibitory processing.

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.