公开(公告)号：US12144808B2

公开(公告)日：2024-11-19

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：US11980617B2

公开(公告)日：2024-05-14

申请号：US16981639

申请日：2019-03-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen Snyder ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/4985 ,  A61K9/00 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/155 ,  A61K31/165 ,  A61K31/197 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/485 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/07 ,  A61P25/24

CPC classification number: A61K31/4985 ,  A61K9/006 ,  A61K31/13 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/155 ,  A61K31/165 ,  A61K31/197 ,  A61K31/343 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/42 ,  A61K31/485 ,  A61K31/55 ,  A61K31/5513 ,  A61K38/07 ,  A61P25/24

Abstract: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A or 5-HT2A/D2 receptor ligand, e.g. lumateperone.

公开(公告)号：US11958852B2

公开(公告)日：2024-04-16

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

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  A61P25/28 ,  C07D471/16 ,  A61K31/4985 ,  A61K2300/00 ,  A61K31/5383 ,  A61K2300/00

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：US11690842B2

公开(公告)日：2023-07-04

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

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/485 ,  A61K9/4825 ,  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：US11427587B2

公开(公告)日：2022-08-30

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 ,  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：US11376249B2

公开(公告)日：2022-07-05

申请号：US16634055

申请日：2018-07-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  A61P25/36 ,  A61K9/00 ,  A61K9/16 ,  A61K45/06 ,  A61P23/00 ,  A61K31/137 ,  A61K31/485

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：US11052083B2

公开(公告)日：2021-07-06

申请号：US16900746

申请日：2020-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis

IPC: A61K31/498 ,  A61P15/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61K31/4985 ,  A61K9/06 ,  A61K9/00

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：US10961245B2

公开(公告)日：2021-03-30

申请号：US16473693

申请日：2017-12-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

IPC: C07D471/14 ,  C07D471/16 ,  A61K31/4985 ,  A61K9/51 ,  A61K47/34 ,  A61K31/44 ,  A61K9/00 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P1/00 ,  A61P15/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/20 ,  A61P25/32 ,  A61P25/36 ,  A61P3/04

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.

公开(公告)号：US10960009B2

公开(公告)日：2021-03-30

申请号：US16392409

申请日：2019-04-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US10899762B2

公开(公告)日：2021-01-26

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

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.