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公开(公告)号：US20210186962A1
公开(公告)日：2021-06-24
申请号：US17127867
申请日：2020-12-18
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor： Robert E. DAVIS , Kimberly VANOVER
IPC: A61K31/4985 , A61P25/18 , A61K45/06
Abstract: The present disclosure relates to the treatment of schizophrenia in adults, comprising the administration of pharmaceutical capsules comprising 42 mg of lumateperone (60 mg of lumateperone tosylate).
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公开(公告)号：US20210163481A1
公开(公告)日：2021-06-03
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
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.
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公开(公告)号：US10716786B2
公开(公告)日：2020-07-21
申请号：US15934860
申请日：2018-03-23
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor： Peng Li , Wei Yao , Robert Davis
IPC: A61K31/498 , 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.
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公开(公告)号：US10695345B2
公开(公告)日：2020-06-30
申请号：US16557083
申请日：2019-08-30
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.
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公开(公告)号：US20200022981A9
公开(公告)日：2020-01-23
申请号：US16090142
申请日：2017-03-28
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor： Lawrence P. WENNOGLE
IPC: A61K31/519 , A61K31/4985
Abstract: The invention provides methods for the prophylaxis or treatment of one or more disorders associated with dementia comprising administering to a patient in need thereof, a therapeutically effective amount of (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor, and pharmaceutical compositions comprising (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor.
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Patent Agency Ranking
公开(公告)号：US20200017500A9
公开(公告)日：2020-01-16
申请号：US16090152
申请日：2017-03-28
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor： Peng LI , Edwin ARET
IPC: C07D471/16 , C07D213/82
Abstract: The disclosure provides new, stable, pharmaceutically acceptable co-crystal 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.
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公开(公告)号：US20200017499A1
公开(公告)日：2020-01-16
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: C07D471/14 , A61K45/06 , A61K31/5383 , A61K31/4985 , C07D471/16 , A61K31/445
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.
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公开(公告)号：US20190328745A1
公开(公告)日：2019-10-31
申请号：US16507956
申请日：2019-07-10
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor： Kimberly VANOVER , Peng LI , Sharon MATES , Robert DAVIS , Lawrence P. WENNOGLE
IPC: A61K31/5383 , A61K9/00 , A61K9/51 , A61K31/4985 , A61K45/06
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.
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公开(公告)号：US10398698B2
公开(公告)日：2019-09-03
申请号：US15709258
申请日：2017-09-19
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor： Lawrence P. Wennogle , Robert Davis
IPC: A61K31/519 , A61K45/06
Abstract: The invention relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways. In one embodiment the invention relates to inhibitors of phosphodiesterase 1 (PDE1) for treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
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公开(公告)号：US20190218219A1
公开(公告)日：2019-07-18
申请号：US16244796
申请日：2019-01-10
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: C07D471/16 , C07D471/04
Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines
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