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公开(公告)号:US11052083B2
公开(公告)日:2021-07-06
申请号:US16900746
申请日:2020-06-12
发明人: Peng Li , Wei Yao , Robert Davis
IPC分类号: A61K31/498 , A61P15/00 , A61P25/06 , A61P25/18 , A61P25/24 , A61P25/28 , A61K31/4985 , A61K9/06 , A61K9/00
摘要: 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:US11014925B2
公开(公告)日:2021-05-25
申请号:US16090152
申请日:2017-03-28
发明人: Peng Li , Edwin Aret
IPC分类号: C07D471/16 , C07D213/82 , A61K31/519 , C07D213/81 , A61K9/00 , A61P25/18
摘要: 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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53.
公开(公告)号:US10961245B2
公开(公告)日:2021-03-30
申请号:US16473693
申请日:2017-12-29
发明人: Peng Li , Robert Davis
IPC分类号: C07D471/14 , C07D471/16 , A61K31/4985 , A61K9/51 , A61K47/34 , A61K31/44 , A61K9/00 , A61P25/00 , A61P25/28 , A61P25/18 , A61P25/24 , A61P25/22 , A61P1/00 , A61P15/00 , A61P25/06 , A61P25/16 , A61P25/20 , A61P25/32 , A61P25/36 , A61P3/04
摘要: The invention relates to particular substituted heterocycle fused gamma-carbolines, the compounds of Formula I: 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 central nervous system (CNS) 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:US10960009B2
公开(公告)日:2021-03-30
申请号:US16392409
申请日:2019-04-23
发明人: Kimberly Vanover , Peng Li , Sharon Mates , Robert Davis , Lawrence P. Wennogle
IPC分类号: A61K9/00 , A61K9/51 , A61K31/5383 , A61K45/06 , A61K31/4985
摘要: 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:US20210060009A1
公开(公告)日:2021-03-04
申请号:US16981639
申请日:2019-03-15
IPC分类号: A61K31/4985 , A61P25/24 , A61K31/135 , A61K31/13 , A61K31/485 , A61K31/155 , A61K38/07 , A61K31/197 , A61K31/42 , A61K9/00 , A61K31/343 , A61K31/36 , A61K31/138 , A61K31/137 , A61K31/381 , A61K31/165 , A61K31/55 , A61K31/38 , A61K31/5513
摘要: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A or 5-HT2A/D2 receptor ligand, e.g. lumateperone.
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公开(公告)号:US10899762B2
公开(公告)日:2021-01-26
申请号:US16786240
申请日:2020-02-10
发明人: Sharon Mates , Peng Li , Lawrence P. Wennogle , Robert Davis
IPC分类号: C07D471/16 , C07D471/14 , A61K45/06 , A61K31/4985 , A61P25/18 , A61P25/22 , A61P25/24 , C07B59/00
摘要: 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.
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公开(公告)号:US20210002280A1
公开(公告)日:2021-01-07
申请号:US16926552
申请日:2020-07-10
发明人: Sharon MATES , Robert DAVIS , Kimberly VANOVER
IPC分类号: C07D471/14 , A61K45/06 , A61K31/5383 , A61K31/4985 , C07D471/16 , A61K31/445
摘要: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.
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公开(公告)号:US20210000822A1
公开(公告)日:2021-01-07
申请号:US16922893
申请日:2020-07-07
发明人: Sharon MATES , Robert DAVIS , Kimberly VANOVER
IPC分类号: A61K31/4985 , A61P25/18 , A61K9/20 , A61K9/48
摘要: The disclosure provides methods for the treatment of Bipolar II Disorder, comprising administering to a patient in need thereof, a therapeutically effective amount of lumateperone, in free or pharmaceutically acceptable salt form, optionally in deuterated form.
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公开(公告)号:US20200247806A1
公开(公告)日:2020-08-06
申请号:US16786240
申请日:2020-02-10
发明人: Sharon MATES , Peng LI , Lawrence P. WENNOGLE , Robert DAVIS
IPC分类号: C07D471/16 , A61K31/4985 , C07B59/00 , A61K45/06 , C07D471/14 , A61P25/18 , A61P25/22 , A61P25/24
摘要: 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.
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公开(公告)号:US10682355B2
公开(公告)日:2020-06-16
申请号:US16219589
申请日:2018-12-13
发明人: Lawrence P. Wennogle
IPC分类号: A61K31/519 , A61P25/16 , A61P25/14 , A61P25/28 , A61P25/02 , A61K31/527 , A61K31/53 , A61K31/517 , G01N33/84
摘要: 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.
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