公开(公告)号：US12268686B2

公开(公告)日：2025-04-08

申请号：US18319425

申请日：2023-05-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis

IPC: A61K31/498 ,  A61K9/00 ,  A61K9/06 ,  A61K31/4985

Abstract: The disclosure provides new transmucosal and subcutaneous 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：US12264160B2

公开(公告)日：2025-04-01

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: A61K31/437 ,  A61K9/48 ,  A61K9/50 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14 ,  C07D471/16 ,  C07D471/22

Abstract: The invention relates to pharmaceutical compositions comprising compounds of Formula Q: wherein W is —N(CH3)—, and Y is —C(O)—, in free base or pharmaceutically acceptable salt form, 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：US12195464B2

公开(公告)日：2025-01-14

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.

公开(公告)号：US12180210B2

公开(公告)日：2024-12-31

申请号：US17288225

申请日：2019-10-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng

IPC: C07D487/04 ,  A61P25/00

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：US12070459B2

公开(公告)日：2024-08-27

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：US11753419B2

公开(公告)日：2023-09-12

申请号：US17757212

申请日：2020-12-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert E Davis ,  Kimberly Vanover

IPC: A61K31/4985 ,  C07D471/22 ,  C07D487/22 ,  C07D519/00

CPC classification number: 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：US11311536B2

公开(公告)日：2022-04-26

申请号：US16221162

申请日：2018-12-14

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：US11026951B2

公开(公告)日：2021-06-08

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：US10960010B2

公开(公告)日：2021-03-30

申请号：US16443240

申请日：2019-06-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly Vanover ,  Peng Li ,  Sharon Mates ,  Robert Davis ,  Lawrence P. Wennogle

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

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：US10906906B2

公开(公告)日：2021-02-02

申请号：US16473691

申请日：2017-12-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

IPC: C07D487/14 ,  C07D471/14 ,  A61K47/34 ,  C07D519/00

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, the compounds of formula I: 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 central nervous system (CNS) 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.