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公开(公告)号：EP3436022A1
公开(公告)日：2019-02-06
申请号：EP17776839.7
申请日：2017-03-31
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公开(公告)号：EP3498725A1
公开(公告)日：2019-06-19
申请号：EP18203320.9
申请日：2014-04-17
发明人： BOTELLA, Gabriel Martinez , HARRISON, Boyd, L. , ROBICHAUD, Albert, Jean , SALITURO, Francesco G. , BERESIS, Richard Thomas
IPC分类号： C07J43/00 , A61K31/57 , A61K31/573 , A61K31/58 , A61P25/00 , C07J3/00 , C07J7/00 , C07J15/00 , C07J1/00 , C07J5/00 , C07J13/00 , C07J21/00 , C07J31/00
摘要： Provided herein is the compound:
for use in the treatment of the following CNS-related conditions in a human subject: mood disorders (inlcuding depression), postnatal depression and positive and negative modulation of the GABA A receptor.-
公开(公告)号：EP3488852A1
公开(公告)日：2019-05-29
申请号：EP18199381.7
申请日：2014-08-22
发明人： MARTINEZ BOTELLA, Gabriel , HARRISON, Boyd, L. , ROBICHAUD, Albert, Jean , SALITURO, Francesco, Gerald , HERR, Robert, Jason , KARGBO, Robert, Borbo
摘要： Described herein are neuroactive steroids of the Formula ( I ):
or a pharmaceutically acceptable salt thereof; wherein ------ , R 1 , R 2 , R 5 , A and L 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.-
公开(公告)号：EP3021852A2
公开(公告)日：2016-05-25
申请号：EP14826212.4
申请日：2014-07-18
发明人： MARTINEZ BOTELLA, Gabriel , HARRISON, Boyd L. , ROBICHAUD, Albert, Jean , SALITURO, Francesco Gerald
CPC分类号： C07J41/0094 , A61K31/56 , A61K31/565 , A61K31/567 , A61K45/06 , C07J1/0011 , C07J1/0022 , C07J5/0053 , C07J11/00 , C07J21/008 , C07J31/006 , C07J51/00 , C07J71/001 , A61K2300/00
摘要： Described herein are neuroactive steroids of the Formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof; wherein R
1a and R
1b 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：（式（I））或其药学上可接受的盐; 其中R 1a和R 1b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：EP3728285A1
公开(公告)日：2020-10-28
申请号：EP18839992.7
申请日：2018-12-21
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公开(公告)号：EP3392260A1
公开(公告)日：2018-10-24
申请号：EP18162373.7
申请日：2013-12-18
IPC分类号： C07J1/00 , C07J7/00 , C07J9/00 , A61K31/57 , A61K31/575 , A61P25/00 , C07J5/00 , C07J21/00 , C07J41/00 , C07J51/00
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：EP3035940B1
公开(公告)日：2018-10-17
申请号：EP14837132.1
申请日：2014-08-22
发明人： MARTINEZ BOTELLA, Gabriel , HARRISON, Boyd, L. , ROBICHAUD, Albert, Jean , SALITURO, Francesco, Gerald , HERR, Robert, Jason , KARGBO, Robert, Borbo
CPC分类号： C07J43/003 , A61K31/58 , A61K45/06 , C07J1/0059 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J21/00 , C07J21/008 , A61K2300/00
摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein -------, R1, R2, R5, A and L 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：EP3310394A1
公开(公告)日：2018-04-25
申请号：EP16812564.9
申请日：2016-06-17
CPC分类号： A61K31/57 , A61K9/0019 , A61K9/08 , A61K31/573 , A61K31/724 , A61K47/6951 , C08B37/0015
摘要： Provided herein are pharmaceutically acceptable aqueous solution comprising a neuroactive steroid, a sulfobutyl ether beta cyclodextrin and a buffer; wherein: the solution is a stable solution between a pH of about 3 and about 9, e.g., at room temperature, for at least 1, 2, 3, 4 weeks; 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 months; 1, 2, 3 years or more; the buffer is present at a concentration of at least 0.1 mM; or the solution remains substantially free of impurities (e.g., the solution is substantially free of impurities at room temperature for at least 1, 2, 3, 4 weeks; 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 months; 1, 2, 3 years or more).
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公开(公告)号：EP4351588A1
公开(公告)日：2024-04-17
申请号：EP22736445.2
申请日：2022-06-10
IPC分类号： A61K31/575 , A61K39/00 , A61K45/06 , A61P25/28
CPC分类号： A61K45/06 , A61K31/575 , A61P25/28
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公开(公告)号：EP4086270A1
公开(公告)日：2022-11-09
申请号：EP22166199.4
申请日：2013-12-18
IPC分类号： C07J1/00 , C07J7/00 , A61P25/00 , C07J21/00 , C07J41/00 , A61K31/5685 , A61K31/57 , A61K31/58 , A61P9/10 , A61P23/00 , A61P23/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28
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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