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公开(公告)号：US11123351B2
公开(公告)日：2021-09-21
申请号：US16797426
申请日：2020-02-21
IPC分类号： A61K31/568 , A61P1/16 , A61K9/48 , A61K47/14 , A61K31/7016 , A61K31/437
摘要： The present invention is directed to a novel pharmaceutical formulation comprising 3α-ethynyl-3β-hydroxyandrostan-17-one oxime in an amount of 0.1-10% by weight of the total weight of the composition; and a vehicle comprising (a) 45-100% of a monoester; (b) optionally up to 51% of a diester; and (c) optionally up to about 10% of a triester. Also claimed is a method for the treatment of medical conditions such as hypersomnia and hepatic encephalopathy by the use of a pharmaceutical formulation as claimed.
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2.发明申请STEROID COMPOUND FOR USE IN THE TREATMENT OF HEPATIC ENCEPHALOPATHY 有权STEROID化合物用于治疗HEPATIC ENCEPHALOPATHYY公开(公告)号：US20170056416A1
公开(公告)日：2017-03-02
申请号：US15352035
申请日：2016-11-15
IPC分类号： A61K31/568 , A61K31/4375 , A61K45/06
CPC分类号： A61K31/568 , A61K31/198 , A61K31/216 , A61K31/437 , A61K31/4375 , A61K31/7016 , A61K45/06 , A61K2300/00
摘要： The present invention provides the steroidal compound 3□-ethynyl-3□-hydroxyandrostan-17-one oxime, or a pharmaceutically acceptable salt thereof, for use in treatment of hepatic encephalopathy.
摘要翻译： 本发明提供了用于治疗肝性脑病的甾族化合物3'-乙炔基-3□ - 羟基和雄甾烷-17-酮肟或其药学上可接受的盐。
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3.发明公开公开(公告)号：US20240216394A1
公开(公告)日：2024-07-04
申请号：US18287329
申请日：2022-04-19
发明人： Magnus Doverskog , Maja Johansson , Lars Öhman , David Jones
IPC分类号： A61K31/568 , A61P1/16
CPC分类号： A61K31/568 , A61P1/16
摘要： The present invention is directed to the compound golexanolone or a pharmaceutically acceptable salt thereof for use in the treatment of fatigue or cognitive impairment, or a combination thereof, in a non-cirrhotic patient with a chronic liver disease, wherein the patient has a serum level of allopregnanolone which is 0.03 ng/ml or higher.
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公开(公告)号：US20230134958A1
公开(公告)日：2023-05-04
申请号：US17976220
申请日：2022-10-28
IPC分类号： A61K31/568 , A61P1/16 , A61K31/15 , A61K31/138 , A61K31/4178 , A61K31/167 , A61K31/575 , A61K38/13 , A61K31/485 , A61K31/165 , A61K39/395 , A61K31/7016 , A61K31/437 , A61K31/341 , A61K31/519 , A61P25/00
摘要： The present invention is directed to a method for the treatment of cognitive impairment in a cirrhotic patient with hepatic encephalopathy (HE), said patient having a CRT index (continous reaction time index) below 1.9 at baseline (prior to treatment), whereby the compound golexanolone (3α-ethynyl-3β-hydroxyandrostan-17-one oxime) of formula (I) or a pharmaceutically acceptable salt thereof, is administered to said patient.
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公开(公告)号：US10603326B2
公开(公告)日：2020-03-31
申请号：US16450620
申请日：2019-06-24
IPC分类号： A61K31/568 , A61P1/16 , A61K9/48 , A61K47/14 , A61K31/437 , A61K31/7016
摘要： The present invention is directed to a novel pharmaceutical formulation comprising 3α-ethynyl-3β-hydroxyandrostan-17-one oxime in an amount of 0.1-10% by weight of the total weight of the composition; and a vehicle comprising (a) 45-100% of a monoester; (b) optionally up to 51% of a diester; and (c) optionally up to about 10% of a triester. Also claimed is a method for the treatment of medical conditions such as hypersomnia and hepathic encephalopathy by the use of a pharmaceutical formulation as claimed.
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6.发明申请公开(公告)号：US20170369522A1
公开(公告)日：2017-12-28
申请号：US15542800
申请日：2016-01-11
CPC分类号： C07J41/005 , A61K31/57 , A61K45/06 , Y02A50/463
摘要： The invention relates to 3α-ethynyl, 3β-hydroxy, 5α-pregnan-20-oxime or a pharmaceutically acceptable salt thereof, which compounds and/or salts are useful as modulators of the mammal brain excitability via the gamma-5 aminobutyric acid receptor-chloride ionophore (GABAA-R) complex and in the treatment of disorders such as hepatic encephalopathy, Down's syndrome and Alzheimer's disease.
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公开(公告)号：US20200297737A1
公开(公告)日：2020-09-24
申请号：US16797426
申请日：2020-02-21
IPC分类号： A61K31/568 , A61P1/16 , A61K9/48 , A61K47/14
摘要： The present invention is directed to a novel pharmaceutical formulation comprising 3α-ethynyl-3β-hydroxyandrostan-17-one oxime in an amount of 0.1-10% by weight of the total weight of the composition; and a vehicle comprising (a) 45-100% of a monoester; (b) optionally up to 51% of a diester; and (c) optionally up to about 10% of a triester. Also claimed is a method for the treatment of medical conditions such as hypersomnia and hepatic encephalopathy by the use of a pharmaceutical formulation as claimed.
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公开(公告)号：US10351589B2
公开(公告)日：2019-07-16
申请号：US15542800
申请日：2016-01-11
摘要： The invention relates to 3α-ethynyl, 3β-hydroxy, 5α-pregnan-20-oxime, represented by the following structural formula: or a pharmaceutically acceptable salt thereof, which compounds and/or salts are useful as modulators of the mammal brain excitability via the gamma-aminobutyric acid receptor-chloride ionophore (GABAA-R) complex and in the treatment of disorders such as hepatic encephalopathy, Down's syndrome and Alzheimer's disease.
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公开(公告)号：US10342804B2
公开(公告)日：2019-07-09
申请号：US15716838
申请日：2017-09-27
IPC分类号： A61K45/06 , A61K31/198 , A61K31/216 , A61K31/437 , A61K31/568 , A61K31/4375 , A61K31/7016
摘要： The present invention provides the steroidal compound 3α-ethynyl-3β-hydroxyandrostan-17-one oxime, or a pharmaceutically acceptable salt thereof, for use in treatment of hepatic encephalopathy.
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10.发明申请STEROID COMPOUND FOR USE IN THE TREATMENT OF HEPATIC ENCEPHALOPATHY 审中-公开STEROID化合物用于治疗HEPATIC ENCEPHALOPATHYY公开(公告)号：US20160339040A1
公开(公告)日：2016-11-24
申请号：US15114972
申请日：2015-01-14
IPC分类号： A61K31/568 , A61K31/437 , A61K45/06
CPC分类号： A61K31/568 , A61K31/198 , A61K31/216 , A61K31/437 , A61K31/4375 , A61K31/7016 , A61K45/06 , A61K2300/00
摘要： The present invention provides the steroidal compound 3□-ethynyl-3□-hydroxyandrostan-17-one oxime, or a pharmaceutically acceptable salt thereof, for use in treatment of hepatic encephalopathy.
摘要翻译： 本发明提供了用于治疗肝性脑病的甾族化合物3'-乙炔基-3□ - 羟基和雄甾烷-17-酮肟或其药学上可接受的盐。
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