公开(公告)号：US20230181576A9

公开(公告)日：2023-06-15

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 ,  C07D471/16 ,  A61K9/00 ,  A61K9/16 ,  A61K45/00 ,  C07D241/40 ,  A61K31/445 ,  A61K45/06

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

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：US20230021717A1

公开(公告)日：2023-01-26

申请号：US17757212

申请日：2020-12-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert E DAVIS ,  Kimberly Vanover

IPC: C07D519/00

Abstract: The invention relates to a particular substituted heterocycle fused gamma-carboline, the compound of Formula I, and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.

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.

公开(公告)号：US11491150B2

公开(公告)日：2022-11-08

申请号：US15986485

申请日：2018-05-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Youyi Peng ,  Lawrence P. Wennogle ,  Qiang Zhang

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

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：US11407751B2

公开(公告)日：2022-08-09

申请号：US16594603

申请日：2019-10-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Charles Tomesch ,  Peng Li ,  Qiang Zhang ,  Andrew S. Thompson

IPC: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, such as Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, and as further defined herein:

公开(公告)号：US20220202813A1

公开(公告)日：2022-06-30

申请号：US17655143

申请日：2022-03-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

IPC: A61K31/4985 ,  A61K9/20 ,  A61K9/16 ,  A61K9/00 ,  A61K47/38 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/06 ,  A61K9/48

Abstract: The disclosure provides new, stable, pharmaceutically acceptable amorphous solid dispersions 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：US20220142932A1

公开(公告)日：2022-05-12

申请号：US17582516

申请日：2022-01-24

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K9/48 ,  A61K31/4985 ,  A61K45/06

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

公开(公告)号：US20220064169A1

公开(公告)日：2022-03-03

申请号：US17288225

申请日：2019-10-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG

IPC: C07D487/04

Abstract: The present disclosure relates to novel PDE2 inhibitory compounds of Formula I as described herein, their use as pharmaceuticals and pharmaceutical compositions comprising them.

公开(公告)号：USRE48839E1

公开(公告)日：2021-12-07

申请号：US16784112

申请日：2020-02-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Allen Fienberg ,  Lawrence Wennogle

IPC: A61K31/4985 ,  A61K9/00 ,  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.

公开(公告)号：US20210369715A1

公开(公告)日：2021-12-02

申请号：US17336798

申请日：2021-06-02

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert E. Davis

IPC: A61K31/519 ,  A61K45/06

Abstract: The disclosure provides the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment and prophylaxis of diseases or disorders characterized by inflammation, including methods of treatment and pharmaceutical compositions for use therein.