公开(公告)号：US11560382B2

公开(公告)日：2023-01-24

申请号：US17124224

申请日：2020-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US11491150B2

公开(公告)日：2022-11-08

申请号：US15986485

申请日：2018-05-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Youyi Peng ,  Lawrence P. Wennogle ,  Qiang Zhang

IPC: A61K31/454 ,  A61P13/12 ,  A61P3/10

Abstract: The disclosure relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., diabetes mellitus, chronic kidney disease, acute kidney failure, and reduction of blood glucose levels.

公开(公告)号：US11407751B2

公开(公告)日：2022-08-09

申请号：US16594603

申请日：2019-10-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Charles Tomesch ,  Peng Li ,  Qiang Zhang ,  Andrew S. Thompson

IPC: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, such as Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, and as further defined herein:

公开(公告)号：US20220202813A1

公开(公告)日：2022-06-30

申请号：US17655143

申请日：2022-03-16

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

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：US20210369715A1

公开(公告)日：2021-12-02

申请号：US17336798

申请日：2021-06-02

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert E. Davis

IPC: A61K31/519 ,  A61K45/06

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

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：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：US10472359B2

公开(公告)日：2019-11-12

申请号：US16056143

申请日：2018-08-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis ,  Lawrence P. Wennogle

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

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 in toluenesulfonic acid addition salt form: and methods of use in the treatment of diseases involving the 5-HT2A receptor pathway, the serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway signaling systems.

公开(公告)号：US10464938B2

公开(公告)日：2019-11-05

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: A61K31/4353 ,  C07D471/06 ,  C07D471/16 ,  C07D471/04

Abstract: The present invention provides pharmaceutical compositions comprising certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, and as further defined herein:

公开(公告)号：US10245260B2

公开(公告)日：2019-04-02

申请号：US15660615

申请日：2017-07-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K9/00 ,  A61K9/16 ,  A61K45/00 ,  A61K45/06 ,  A61K31/445 ,  C07D241/40 ,  A61K31/4985

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.