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公开(公告)号：EP3319610A1
公开(公告)日：2018-05-16
申请号：EP16821920.2
申请日：2016-07-06
IPC分类号： A61K31/567 , A61K31/566
CPC分类号： C07J9/005 , A61P1/00 , A61P25/00 , C07J9/00 , C07J31/006 , C07J41/0055 , C07J51/00 , Y02P20/582
摘要： Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R5, and R8 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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12.发明授权NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, USEFUL IN METHODS OF TREATMENT 有权神经活性19-烷氧基-17-取代的类固醇，用于治疗方法
公开(公告)号：EP2935307B1
公开(公告)日：2018-04-25
申请号：EP13865411.6
申请日：2013-12-18
CPC分类号： A61K31/58 , A61K31/56 , A61K31/565 , A61K31/566 , A61K31/573 , C07J1/0011 , C07J1/0018 , C07J1/0029 , C07J5/0015 , C07J7/002 , C07J9/005 , C07J13/007 , C07J21/00 , C07J21/006 , C07J21/008 , C07J41/0005 , C07J41/0016 , C07J41/0094 , C07J51/00
摘要： The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
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公开(公告)号：EP3258939A2
公开(公告)日：2017-12-27
申请号：EP16753177.1
申请日：2016-02-19
发明人： ROBICHAUD, Albert, Jean , SALITURO, Francesco, G. , HARRISON, Boyd, L. , MARTINEZ BOTELLA, Gabriel
IPC分类号： A61K31/56 , A61K31/58 , A61K31/565
CPC分类号： C07J43/003 , A61K31/58 , A61K45/06 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J21/008
摘要： or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.
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公开(公告)号：EP3157528A4
公开(公告)日：2017-12-27
申请号：EP15809462
申请日：2015-06-18
IPC分类号： C07J9/00 , A61K31/56 , A61K31/575
CPC分类号： C07J9/00 , A61K9/0019 , A61K9/0095 , A61K9/2063 , A61K9/4866 , C07J9/005 , C07J13/005 , C07J13/007 , C07J31/006
摘要： Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, Y, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6a, R6b, R7, and R8 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：EP3206493A1
公开(公告)日：2017-08-23
申请号：EP15851053.7
申请日：2015-10-16
发明人： MARTINEZ BOTELLA, Gabriel , SALITURO, Francesco G. , ROBICHAUD, Albert Jean , HARRISON, Boyd L.
IPC分类号： A01N51/00
CPC分类号： C07J43/003 , A61K9/0019 , A61K9/0053 , A61K31/58 , A61P25/00 , C07D231/14 , C07D249/04 , C07D249/18 , C07D295/033
摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R1, R2a, R2b, R3and A 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.
摘要翻译： 本文描述了式（I）的神经活性甾族化合物：或其药学上可接受的盐; 其中，R 1，R 2a，R 2b，R 3和A如本文所定义。 在某些实施方案中，这些化合物被设想用作GABA调节剂。 本发明还提供了包含本发明化合物的药物组合物以及使用和治疗方法，例如用于诱导镇静和/或麻醉的方法。
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公开(公告)号：EP3157528A1
公开(公告)日：2017-04-26
申请号：EP15809462.3
申请日：2015-06-18
发明人： HARRISON, Boyd, L. , MARTINEZ BOTELLA, Gabriel , ROBICHAUD, Albert, Jean , SALITURO, Francesco, G.
IPC分类号： A61K31/56 , A61K31/575 , C07J9/00
CPC分类号： C07J9/00 , A61K9/0019 , A61K9/0095 , A61K9/2063 , A61K9/4866 , C07J9/005 , C07J13/005 , C07J13/007 , C07J31/006
摘要： Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, Y, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6a, R6b, R7, and R8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
摘要翻译： 根据式（I）及其药学上可接受的盐及其药物组合物提供化合物; 其中X，Y，R1，R2a，R2b，R4a，R4b，R5a，R5b，R6a，R6b，R7和R8如本文所定义。 预期本发明化合物可用于预防和治疗多种病症。
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17.发明公开NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME 有权神经活性19 - 烷氧基 - 17-取代类固醇，其前药，和SO治疗方法
公开(公告)号：EP2935307A1
公开(公告)日：2015-10-28
申请号：EP13865411.6
申请日：2013-12-18
CPC分类号： A61K31/58 , A61K31/56 , A61K31/565 , A61K31/566 , A61K31/573 , C07J1/0011 , C07J1/0018 , C07J1/0029 , C07J5/0015 , C07J7/002 , C07J9/005 , C07J13/007 , C07J21/00 , C07J21/006 , C07J21/008 , C07J41/0005 , C07J41/0016 , C07J41/0094 , C07J51/00
摘要： The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
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公开(公告)号：EP2753632A1
公开(公告)日：2014-07-16
申请号：EP12766766.5
申请日：2012-09-07
发明人： UPASANI, Ravindra, B. , HARRISON, Boyd, L. , ASKEW, Benny, C. Jr. , DODART, Jean-Cosme , SALITURO, Francesco, G. , ROBICHAUD, Albert, J.
CPC分类号： C07J41/00 , C07J1/00 , C07J1/0029 , C07J3/00 , C07J7/007 , C07J9/00 , C07J9/005 , C07J31/003 , C07J31/006 , C07J41/0005 , C07J41/0011 , C07J41/0055 , C07J43/003
摘要： Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L
1 , L
2 , L
3 , X
1 , X
2 , Y, R
z4 , R
z5 , R
z6 , n, R
1 , R
2 , R
3a , R
3b , R
4a , R
4b , R
6a , R
6b , R
7a , R
7b , R
11a , R
11b , R
14 , R
17 , R
19 , R
20 , R
23a , R
23b , and R
24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.-
公开(公告)号：EP4442695A2
公开(公告)日：2024-10-09
申请号：EP24195188.8
申请日：2018-12-21
发明人： ROBICHAUD, Albert Jean , SALITURO, Francesco G. , BLANCO-PILLADO, Maria Jesus , LA, Daniel , HARRISON, Boyd L.
IPC分类号： C07J71/00
CPC分类号： C07J1/0011 , C07J3/005 , C07J5/0015 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J9/00 , C07J13/007 , C07J17/00 , C07J21/00 , C07J21/008 , C07J41/005 , C07J41/0066 , C07J41/0094 , C07J43/003 , C07J51/00 , C07J71/0005
摘要： Provided herein are compounds of Formula (I-I):
and pharmaceutically acceptable salts thereof; wherein p, R1, R3a, R2a, R11a, R11b, R6a , and R6b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-X) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.-
公开(公告)号：EP4406602A2
公开(公告)日：2024-07-31
申请号：EP24170063.2
申请日：2017-07-11
发明人： ROBICHAUD, Albert J. , MARTINEZ BOTELLA, Gabriel , HARRISON, Boyd L. , SALITURO, Francesco G. , GRIFFIN, Andrew , BLANCO-PILLADO, Maria Jesus
IPC分类号： A61P25/00
CPC分类号： C07J1/0029 , C07J7/002 , C07J7/003 , C07J7/006 , C07J41/005 , C07J41/0094 , C07J43/003 , A61P25/00
摘要： Described herein are neuroactive steroids of the Formula (I), Formula (V), or Formula (IX):
or a pharmaceutically acceptable salt thereof; wherein each instance of R2, R3, R4, R5, R6, R7, R11a, R11b, R12, R16, R17, R19, and - - - - - are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
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