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公开(公告)号:US20170291904A1
公开(公告)日:2017-10-12
申请号:US15512005
申请日:2015-09-17
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor: Peng LI , Hailin ZHENG , Jun ZHAO , Lawrence WENNOGLE
IPC: C07D487/14
CPC classification number: C07D487/14
Abstract: The subject matter generally relates to compounds and 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.
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公开(公告)号:US20150259329A1
公开(公告)日:2015-09-17
申请号:US14727443
申请日:2015-06-01
Applicant: Intra-Cellular Therapies, Inc.
Inventor: Peng LI
IPC: C07D405/14 , C07D239/42 , C07D403/12 , C07D401/12
CPC classification number: C07D405/14 , A61K31/4439 , A61K31/506 , A61K45/06 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12
Abstract: The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which penetrate the blood brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.
Abstract translation: 本发明涉及式(I)的化合物或其药学上可接受的盐:其渗透血脑屏障,抑制β-淀粉样蛋白的形成和积累,并且可用于治疗神经变性疾病,特别是阿尔茨海默病。 此外,本发明的化合物抑制某些激酶,因此可用于治疗中枢神经系统的癌症。
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公开(公告)号:US20250009741A1
公开(公告)日:2025-01-09
申请号:US18893190
申请日:2024-09-23
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor: Peng LI , Robert DAVIS
IPC: A61K31/4985 , A61K9/70
Abstract: The disclosure provides new transdermal 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:US20240101569A1
公开(公告)日:2024-03-28
申请号:US18263302
申请日:2022-01-27
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor: Peng LI
IPC: C07D487/14
CPC classification number: C07D487/14
Abstract: The present disclosure relates to free base and salt crystals of 2-(4-acetylbenzyl)-3-((4-fluorophenyl)amino)-5,7,7-trimethyl-7,8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one, composition comprising the same and the method of making and using such free base and salt crystals.
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公开(公告)号:US20240059687A1
公开(公告)日:2024-02-22
申请号:US18451465
申请日:2023-08-17
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:US20230372336A1
公开(公告)日:2023-11-23
申请号:US18320173
申请日:2023-05-18
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor: Sophie DUTHEIL , Gretchen SNYDER , Peng LI , Robert E. DAVIS
IPC: A61K31/4985 , A61P25/00 , A61P25/18
CPC classification number: A61K31/4985 , A61P25/00 , A61P25/18
Abstract: The disclosure provides methods the treatment of psychiatric disorders caused by viral, bacterial, or autoimmune encephalitis, and for treatment of psychiatric symptoms of viral, bacterial, and autoimmune encephalitis, and for protecting or reinforcing the blood-brain barrier, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A.
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公开(公告)号:US20230181576A9
公开(公告)日:2023-06-15
申请号:US17015883
申请日:2020-09-09
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor: Wei YAO , Peng LI , Robert DAVIS , Sharon MATES , Kimberly VANOVER , Gretchen SNYDER
IPC: A61K31/4985 , A61P25/00 , C07D471/16 , A61K9/00 , A61K9/16 , A61K45/00 , C07D241/40 , A61K31/445 , A61K45/06
CPC classification number: A61K31/4985 , A61P25/00 , C07D471/16 , A61K9/0019 , A61K9/16 , A61K45/00 , C07D241/40 , A61K31/445 , 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.
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公开(公告)号:US20230021717A1
公开(公告)日:2023-01-26
申请号:US17757212
申请日:2020-12-10
Applicant: INTRA-CELLULAR THERAPIES, INC.
Inventor: Peng LI , Robert E DAVIS , Kimberly Vanover
IPC: C07D519/00
Abstract: The invention relates to a particular substituted heterocycle fused gamma-carboline, the compound of Formula I, and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.
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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.
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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.
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