公开(公告)号：US20220280517A1

公开(公告)日：2022-09-08

申请号：US17636645

申请日：2020-08-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Robert E. DAVIS ,  Peng LI

IPC: A61K31/519 ,  A61P13/12

Abstract: The disclosure relates to methods of administering comprising administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment and/or prophylaxis of renal disorders, such as chronic kidney disease. Related compounds and methods of making are further defined.

公开(公告)号：US20220184240A1

公开(公告)日：2022-06-16

申请号：US17594356

申请日：2020-04-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K51/04 ,  C07D487/14

Abstract: The present invention relates to novel compounds having a capacity for PDE1 inhibition which may be used as tracers for use in diagnostic techniques, biomarkers for phosphodiesterase 1 (PDE1) in vivo, methods for treating and/or developing novel therapies for PDE1-associated conditions, and to methods of detection and treatment.

公开(公告)号：US20210315891A1

公开(公告)日：2021-10-14

申请号：US17271965

申请日：2019-08-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/70

Abstract: The disclosure provides new transdermal pharmaceutical compositions comprising 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 or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-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 or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-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, in free base, co-crystal or salt form, together with methods of making and using them.

公开(公告)号：US20210299124A1

公开(公告)日：2021-09-30

申请号：US17332417

申请日：2021-05-27

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.

公开(公告)号：US20200247806A1

公开(公告)日：2020-08-06

申请号：US16786240

申请日：2020-02-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/16 ,  A61K31/4985 ,  C07B59/00 ,  A61K45/06 ,  C07D471/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24

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：US20200247805A1

公开(公告)日：2020-08-06

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：US20200069683A1

公开(公告)日：2020-03-05

申请号：US16557083

申请日：2019-08-30

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

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

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：US20190330211A1

公开(公告)日：2019-10-31

申请号：US16473693

申请日：2017-12-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: C07D471/14 ,  A61K9/51

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：US20190292185A1

公开(公告)日：2019-09-26

申请号：US16439361

申请日：2019-06-12

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：US20190112310A1

公开(公告)日：2019-04-18

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.