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公开(公告)号:US20200155576A1
公开(公告)日:2020-05-21
申请号:US16428386
申请日:2019-05-31
发明人: Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
摘要: Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
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公开(公告)号:US10426837B2
公开(公告)日:2019-10-01
申请号:US15660114
申请日:2017-07-26
IPC分类号: A61K45/06 , C07J43/00 , A61K31/00 , C07J3/00 , C07J7/00 , C07J13/00 , C07J41/00 , C07J51/00 , C07J9/00 , A61K45/00
摘要: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, and R3 are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use, e.g., for treating a subject suffering from a disease or disorder described herein.
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公开(公告)号:US20190211054A9
公开(公告)日:2019-07-11
申请号:US15143312
申请日:2016-04-29
发明人: Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
CPC分类号: C07J43/003 , C07J3/00 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J21/00 , C07J31/006
摘要: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.
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公开(公告)号:US20190177358A1
公开(公告)日:2019-06-13
申请号:US16206472
申请日:2018-11-30
IPC分类号: C07J43/00 , A61K45/06 , A61K31/575 , A61K31/58 , C07J9/00
摘要: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
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公开(公告)号:US20190127414A1
公开(公告)日:2019-05-02
申请号:US16227013
申请日:2018-12-20
IPC分类号: C07J9/00
摘要: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.
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公开(公告)号:US10172871B2
公开(公告)日:2019-01-08
申请号:US15297845
申请日:2016-10-19
发明人: Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
IPC分类号: A61K31/58 , A61K31/573 , C07J3/00 , C07J7/00 , C07J15/00 , C07J43/00 , A61K9/00 , C07J5/00 , C07J1/00 , C07J13/00 , C07J21/00 , C07J31/00
摘要: Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
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公开(公告)号:US20180311258A1
公开(公告)日:2018-11-01
申请号:US15565645
申请日:2016-04-08
发明人: Albert Jean Robichaud , Francesco G. Salituro , Boyd L. Harrison , Gabriel Martinez Botella , Jeffrey Jonas
CPC分类号: C07J7/002 , A61K31/57 , A61K45/06 , C07B2200/05
摘要: Described herein are deuterium-enriched neuroactive steroids of the Formula (II) or a pharmaceutically acceptable salt thereof; wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R11a, R11b, R12a, R12b, R16a, R16b, R17, R19, Ra, and Rb and subvariables thereof are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment.
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公开(公告)号:US20180237470A1
公开(公告)日:2018-08-23
申请号:US15917263
申请日:2018-03-09
CPC分类号: C07J9/00 , C07J9/005 , C07J13/005 , C07J13/007 , C07J21/008 , C07J41/0061
摘要: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3a, R3b, R4, R5a, R5b, R6a, and R6b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions.
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公开(公告)号:US20180194797A1
公开(公告)日:2018-07-12
申请号:US15742424
申请日:2016-07-06
CPC分类号: C07J9/00 , A61P3/00 , C07J7/002 , C07J9/005 , C07J13/005 , C07J13/007 , C07J17/00 , C07J31/006 , C07J41/0061
摘要: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, and R3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
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公开(公告)号:US20170319695A1
公开(公告)日:2017-11-09
申请号:US15660114
申请日:2017-07-26
IPC分类号: A61K45/06 , C07J43/00 , C07J41/00 , C07J13/00 , C07J7/00 , C07J3/00 , C07J51/00 , A61K31/00 , A61K45/00
CPC分类号: A61K45/06 , A61K31/00 , A61K45/00 , C07J3/00 , C07J3/005 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J7/009 , C07J9/00 , C07J13/007 , C07J41/0044 , C07J43/003 , C07J51/00
摘要: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, and R3 are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use, e.g., for treating a subject suffering from a disease or disorder described herein.
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