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：US11440911B2

公开(公告)日：2022-09-13

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：US11331316B2

公开(公告)日：2022-05-17

申请号：US16341806

申请日：2017-10-03

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 ,  C07D471/16 ,  A61K9/10

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：US20220125791A1

公开(公告)日：2022-04-28

申请号：US17426805

申请日：2020-01-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Robert DAVIS ,  Allen A. FIENBERG

IPC: A61K31/519 ,  A61K9/00

Abstract: Disclosed herein are novel drug eluting contact lenses configured to release one or more compounds that inhibit phosphodiesterase 1 (PDE1). The PDE1 inhibitors may be administered as monotherapy or in combination with additional pharmaceutical agents in the treatment of an ophthalmic disease, disorder or injury. Related methods of use and treatment are also disclosed.

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：US20210371421A1

公开(公告)日：2021-12-02

申请号：US17405736

申请日：2021-08-18

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Kimberly VANOVER ,  Lawrence WENNOGLE

IPC: C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  A61P25/28 ,  C07D471/16 ,  A61K31/445

Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.

公开(公告)号：US11096944B2

公开(公告)日：2021-08-24

申请号：US16875432

申请日：2020-05-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li

IPC: A61K31/519 ,  C07D471/14 ,  A61P25/28 ,  A61K31/4985 ,  A61K45/06 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24

Abstract: The invention relates to particular substituted deuterated 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：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：US11052084B2

公开(公告)日：2021-07-06

申请号：US16903133

申请日：2020-06-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

IPC: A61K31/4985 ,  A61K9/48 ,  A61K9/00 ,  A61K9/16

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.