公开(公告)号：USRE48825E1

公开(公告)日：2021-11-23

申请号：US16294607

申请日：2019-03-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Tomesch ,  Lawrence P. Wennogle

IPC: A61K31/4985 ,  C07D471/16 ,  C07D471/22 ,  C07D309/30 ,  C07C309/30

Abstract: The present invention relates to toluenesulfonic acid addition salt crystals of 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′: 4,5]pyrrolo[1,2,3 -de]quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone, and methods of using such crystals as 5-hydroxytryptamine 2 receptor agonists and antagonists in treating disorders of the central nervous system.

公开(公告)号：US11166956B2

公开(公告)日：2021-11-09

申请号：US16358218

申请日：2019-03-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. Wennogle ,  Peng Li

IPC: A61K31/519 ,  A61K31/341 ,  A61K31/198 ,  A61K31/216 ,  A61K31/197 ,  A61K45/06

Abstract: The invention relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) and inhibitors of Neprilysin (NEP) useful for the treatment of certain cardiovascular diseases or related disorders, e.g., hypertension, congestive heart disease, and post-myocardial infarction. In another embodiment, the invention relates to the combination of inhibitors of PDE1 and inhibitors of NEP for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways in the cardiovascular system (e.g., in cardiac tissue or in arterial smooth muscle).

公开(公告)号：US11124514B2

公开(公告)日：2021-09-21

申请号：US16585251

申请日：2019-09-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Kimberly Vanover ,  Lawrence Wennogle

IPC: A61K31/50 ,  A61K31/13 ,  A61K31/445 ,  A61K31/44 ,  A61K31/27 ,  C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  A61P25/28 ,  C07D471/16

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：US20210213018A1

公开(公告)日：2021-07-15

申请号：US16332750

申请日：2017-09-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen SNYDER ,  Lawrence P. WENNOGLE ,  Jennifer O'BRIEN ,  Joseph HENDRICK

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/4015 ,  A61P37/06 ,  A61P25/28 ,  A61P27/02

Abstract: The disclosure provides the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment and prophylaxis of diseases or disorders characterized by inflammation, e.g., neuroinflammation, including methods of treatment and pharmaceutical compositions for use therein.

公开(公告)号：US20210032247A1

公开(公告)日：2021-02-04

申请号：US17072933

申请日：2020-10-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US20210009592A1

公开(公告)日：2021-01-14

申请号：US17040892

申请日：2019-03-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert DAVIS

IPC: C07D471/16 ,  A61K9/00 ,  C07B59/00

Abstract: The invention relates to particular deuterated 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：US20210008065A1

公开(公告)日：2021-01-14

申请号：US17040893

申请日：2019-03-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K45/06 ,  C07D471/16

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：US20200375988A1

公开(公告)日：2020-12-03

申请号：US16900746

申请日：2020-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

IPC: 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：US10799500B2

公开(公告)日：2020-10-13

申请号：US16276331

申请日：2019-02-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  C07D471/16 ,  C07D241/40 ,  A61K31/445 ,  A61P25/00 ,  A61K9/00 ,  A61K9/16 ,  A61K45/00 ,  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：US20200306247A1

公开(公告)日：2020-10-01

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.