公开(公告)号：US20250144029A1

公开(公告)日：2025-05-08

申请号：US18832674

申请日：2023-01-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: A61K9/14 ,  A61K31/519

Abstract: The present disclosure relates to amorphous solid dispersions comprising (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one and an excipient, as well as related methods of making and using such dispersions.

公开(公告)号：US20250099471A1

公开(公告)日：2025-03-27

申请号：US18960359

申请日：2024-11-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei YAO ,  Peng LI

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

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：US20240383909A1

公开(公告)日：2024-11-21

申请号：US18688618

申请日：2022-09-02

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D487/14 ,  C07C39/08 ,  C07C215/12 ,  C07D209/48

Abstract: The present disclosure relates to co-crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, compositions comprising the same, as well as methods of making and using such co-crystals.

公开(公告)号：US20240245610A1

公开(公告)日：2024-07-25

申请号：US18593060

申请日：2024-03-01

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS ,  William Paul FINDLAY

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

CPC classification number: A61K9/2013 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/284 ,  A61K31/4985 ,  C07B2200/13

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：US20240091224A1

公开(公告)日：2024-03-21

申请号：US18504345

申请日：2023-11-08

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

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

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/4825 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4891

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：US20230339951A1

公开(公告)日：2023-10-26

申请号：US18327607

申请日：2023-06-01

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/14 ,  A61K47/38 ,  A61K9/48 ,  C07D471/16 ,  A61K9/50 ,  A61K47/34 ,  A61K31/4985

CPC classification number: C07D471/16 ,  A61K9/4825 ,  A61K9/4891 ,  A61K9/5031 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14

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-one, 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.

公开(公告)号：US20230009130A1

公开(公告)日：2023-01-12

申请号：US17818606

申请日：2022-08-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG

IPC: 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：US20220372035A1

公开(公告)日：2022-11-24

申请号：US17813473

申请日：2022-07-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US20220363682A1

公开(公告)日：2022-11-17

申请号：US17815843

申请日：2022-07-28

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：US20220281867A1

公开(公告)日：2022-09-08

申请号：US17652076

申请日：2022-02-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D471/16

Abstract: The disclosure provides a new, stable, pharmaceutically acceptable bis-tosylate salt form 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.