公开(公告)号：US20230339951A1

公开(公告)日：2023-10-26

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

CPC classification number: C07D471/16 ,  A61K9/4825 ,  A61K9/4891 ,  A61K9/5031 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14

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：US20220363682A1

公开(公告)日：2022-11-17

申请号：US17815843

申请日：2022-07-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. WENNOGLE ,  Peng LI ,  Edwin ARET

IPC: C07D471/16

Abstract: The disclosure provides new, stable, pharmaceutically acceptable hydrochloride salt forms 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：US20210338679A1

公开(公告)日：2021-11-04

申请号：US17279518

申请日：2019-09-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/519 ,  A61P37/06

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：US20210322433A1

公开(公告)日：2021-10-21

申请号：US17245939

申请日：2021-04-30

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Peng LI ,  Sharon MATES ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: A61K31/5383 ,  A61K31/4985 ,  A61K45/06 ,  A61K9/00 ,  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：US20200375994A1

公开(公告)日：2020-12-03

申请号：US16879676

申请日：2020-05-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. WENNOGLE

IPC: A61K31/519 ,  A61P25/16 ,  A61P25/14 ,  A61P25/28 ,  A61P25/02 ,  A61K31/527 ,  A61K31/53 ,  A61K31/517 ,  G01N33/84

Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

公开(公告)号：US20190290655A1

公开(公告)日：2019-09-26

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: A61K31/5383 ,  A61K45/06 ,  A61K31/4985 ,  A61K9/00 ,  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：US20190275046A1

公开(公告)日：2019-09-12

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：US20190183888A1

公开(公告)日：2019-06-20

申请号：US16165832

申请日：2018-10-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Allen FIENBERG ,  Lawrence P. WENNOGLE

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

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：US20190062334A1

公开(公告)日：2019-02-28

申请号：US16054728

申请日：2018-08-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Peng LI ,  Lawrence P. WENNOGLE ,  Robert DAVIS

IPC: C07D471/16 ,  A61K31/4985 ,  C07B59/00 ,  A61K45/06 ,  C07D471/14

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：US20180099060A1

公开(公告)日：2018-04-12

申请号：US15560107

申请日：2016-03-18

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Jun ZHAO ,  Lawrence P. WENNOGLE

IPC: A61K51/04 ,  C07D213/69 ,  C07D213/65 ,  A61P25/24 ,  A61P25/22

CPC classification number: A61K51/0455 ,  A61P25/22 ,  A61P25/24 ,  C07D213/65 ,  C07D213/69

Abstract: The present invention relates to novel pyridinoxy phenylpropanamines, their pharmaceutical compositions and methods of use. In addition, the present invention relates to therapeutic methods that penetrate the blood-brain barrier and regulate the norepinephrine and serotonin transporters (“NET/SERT”).