公开(公告)号：US20220362241A1

公开(公告)日：2022-11-17

申请号：US17764070

申请日：2020-09-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Robert E. DAVIS ,  Gretchen SNYDER ,  Peng LI

IPC: A61K31/4985 ,  C07D471/16 ,  A61P25/08 ,  A61K45/06

Abstract: The disclosure provides methods for the for treatment of psychosis, such as schizophrenia, or depression (such as bipolar depression) and/or anxiety, comprising administering to a patient in need thereof, (i) a 5-HT2A or 5-HT2A/D2 receptor ligand, for example a substituted heterocycle fused gamma-carboline as described herein, in free, pharmaceutically acceptable salt or prodrug form, and (ii) a nitric oxide donor, separately (sequentially or simultaneously), or in combination (e.g., in a fixed dose combination).

公开(公告)号：US20220296591A1

公开(公告)日：2022-09-22

申请号：US17832282

申请日：2022-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS ,  Sharon MATES ,  Kimberly VANOVER ,  Gretchen SNYDER

IPC: A61K31/4985 ,  A61P25/36 ,  A61P23/00 ,  A61K9/00 ,  A61K9/16 ,  A61K31/137 ,  A61K31/485 ,  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：US20220073558A1

公开(公告)日：2022-03-10

申请号：US17415667

申请日：2019-12-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Peng LI ,  Robert DAVIS ,  Yupu QIAO

IPC: C07J43/00

Abstract: The invention relates to particular prodrugs and analogs of (3α,5α)-3-hydroxy-21-(1H-imidazol-1-yl)-3-methoxymethyl)-pregnan-20-one, in free or pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use as sedatives, hypnotics, anxiolytics, and/or anesthetics, and methods for treatment of depression, anxiety, insomnia, epilepsy, and other central nervous system disorders, as well as to combinations with other agents.

公开(公告)号：US20220056031A1

公开(公告)日：2022-02-24

申请号：US17416997

申请日：2019-12-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Kimberly VANOVER ,  Robert DAVIS

IPC: C07D471/16

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：US20210220280A1

公开(公告)日：2021-07-22

申请号：US17270573

申请日：2019-08-30

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS ,  William Paul FINDLAY

IPC: A61K9/20 ,  A61K31/4985 ,  A61K9/28

Abstract: The present disclosure relates to solid oral dosage forms 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：US20210163481A1

公开(公告)日：2021-06-03

申请号：US16634059

申请日：2018-07-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG ,  Robert DAVIS ,  Sharon MATES ,  Kimberly VANOVER ,  Gretchen SNYDER

IPC: C07D471/16 ,  A61K45/06 ,  A61P1/00 ,  A61P11/00 ,  A61P29/00 ,  A61P25/36

Abstract: The invention relates to particular prodrugs of 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：US20200017500A9

公开(公告)日：2020-01-16

申请号：US16090152

申请日：2017-03-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Edwin ARET

IPC: C07D471/16 ,  C07D213/82

Abstract: The disclosure provides new, stable, pharmaceutically acceptable co-crystal 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：US20190328745A1

公开(公告)日：2019-10-31

申请号：US16507956

申请日：2019-07-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：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.