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：US20220142932A1

公开(公告)日：2022-05-12

申请号：US17582516

申请日：2022-01-24

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K9/48 ,  A61K31/4985 ,  A61K45/06

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：US20220064169A1

公开(公告)日：2022-03-03

申请号：US17288225

申请日：2019-10-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG

IPC: C07D487/04

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：USRE48839E1

公开(公告)日：2021-12-07

申请号：US16784112

申请日：2020-02-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Allen Fienberg ,  Lawrence Wennogle

IPC: A61K31/4985 ,  A61K9/00 ,  A61K31/198 ,  A61K31/44 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/14 ,  C07D498/14

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.

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：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.