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1. 发明申请

US20140288027A1 Derivative of Butylphthalide and Preparation Method and Use Thereof 有权
标题翻译：丁苯酞的衍生物及其制备方法及用途
公开(公告)号：US20140288027A1
公开(公告)日：2014-09-25
申请号：US14351424
申请日：2012-09-26
申请人： Shijiazhuang Yiling Pharmaceutical Co., Ltd
发明人： Wei Wang , Yayao Zhou , Ya'nan Liu
IPC分类号： A61K31/365 , A61K31/665
CPC分类号： C07D307/88 , A61K9/0019 , A61K9/4858 , A61K31/365 , A61K31/665 , A61K47/26 , C07F9/65517
摘要： (−)-(S)-3-(3′-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to treatment and prevention of cerebral ischemic diseases and have a sleep-improving function. The acid refers to a pharmaceutically acceptable inorganic or organic acid. The inorganic acid refers to nitric acid, sulfuric acid, or phosphoric acid. In addition to an acid radical, the organic acid at least comprises at least one of an amino group, a hydroxyl group, and a carboxyl group. None of the compound shown by Formula I and the ester thereof is water-soluble. An ester generated from the compound and the acid further react with an acid or a base to generate a salt which is water-soluble and is used to prepare injection preparation. The experiment proves that the salt does not stimulate vessels.
摘要翻译：通过实验证明（ - ） - （S）-3-（3'-羟基） - 丁基苯酞（式I所示的化合物）和由其形成的酯和酸，可用于治疗和预防脑缺血疾病并具有睡眠改善功能。酸是指药学上可接受的无机酸或有机酸。无机酸是指硝酸，硫酸或磷酸。除了酸基之外，有机酸至少包含氨基，羟基和羧基中的至少一个。式I所示的化合物及其酯不是水溶性的。由化合物和酸生成的酯进一步与酸或碱反应生成水溶性盐并用于制备注射制剂。实验证明盐不会刺激血管。

2. 发明申请

US20160244421A1 Derivative of Butylphthalide and Preparation Method and Use Thereof 审中-公开
标题翻译：丁苯酞的衍生物及其制备方法及用途
公开(公告)号：US20160244421A1
公开(公告)日：2016-08-25
申请号：US15042263
申请日：2016-02-12
申请人： Shijiazhuang Yiling Pharmaceutical Co., Ltd.
发明人： Wei Wang , Yayao Zhou , Ya'nan Liu
IPC分类号： C07D307/88 , C07F9/655
CPC分类号： C07D307/88 , A61K9/0019 , A61K9/4858 , A61K31/365 , A61K31/665 , A61K47/26 , C07F9/65517
摘要： (−)-(S)-3-(3′-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to treatment and prevention of cerebral ischemic diseases and have a sleep-improving function. The acid refers to a pharmaceutically acceptable inorganic or organic acid. The inorganic acid refers to nitric acid, sulfuric acid, or phosphoric acid. In addition to an acid radical, the organic acid at least comprises at least one of an amino group, a hydroxyl group, and a carboxyl group. None of the compound shown by Formula I and the ester thereof is water-soluble. An ester generated from the compound and the acid further react with an acid or a base to generate a salt which is water-soluble and is used to prepare injection preparation. The experiment proves that the salt does not stimulate vessels.
摘要翻译：通过实验证明（ - ） - （S）-3-（3'-羟基） - 丁基苯酞（式I所示的化合物）和由其形成的酯和酸，可用于治疗和预防脑缺血疾病并具有睡眠改善功能。酸是指药学上可接受的无机酸或有机酸。无机酸是指硝酸，硫酸或磷酸。除了酸基之外，有机酸至少包含氨基，羟基和羧基中的至少一个。式I所示的化合物及其酯不是水溶性的。由化合物和酸生成的酯进一步与酸或碱反应生成水溶性盐并用于制备注射制剂。实验证明盐不会刺激血管。

3. 发明授权

US09278087B2 Derivative of butylphthalide and preparation method and use thereof 有权
标题翻译：丁苯酞的衍生物及其制备方法及用途
公开(公告)号：US09278087B2
公开(公告)日：2016-03-08
申请号：US14351424
申请日：2012-09-26
申请人： Shijiazhuang Yiling Pharmaceutical Co., Ltd
发明人： Wei Wang , Yayao Zhou , Ya'nan Liu
IPC分类号： C07D307/88 , C07F9/655 , A61K31/365 , A61K31/665 , A61K47/26 , A61K9/00 , A61K9/48
CPC分类号： C07D307/88 , A61K9/0019 , A61K9/4858 , A61K31/365 , A61K31/665 , A61K47/26 , C07F9/65517
摘要： (−)-(S)-3-(3′-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to treatment and prevention of cerebral ischemic diseases and have a sleep-improving function. The acid refers to a pharmaceutically acceptable inorganic or organic acid. The inorganic acid refers to nitric acid, sulfuric acid, or phosphoric acid. In addition to an acid radical, the organic acid at least comprises at least one of an amino group, a hydroxyl group, and a carboxyl group. None of the compound shown by Formula I and the ester thereof is water-soluble. An ester generated from the compound and the acid further react with an acid or a base to generate a salt which is water-soluble and is used to prepare injection preparation. The experiment proves that the salt does not stimulate vessels.
摘要翻译：通过实验证明（ - ） - （S）-3-（3'-羟基） - 丁基苯酞（式I所示的化合物）和由其形成的酯和酸，可用于治疗和预防脑缺血疾病并具有睡眠改善功能。酸是指药学上可接受的无机酸或有机酸。无机酸是指硝酸，硫酸或磷酸。除了酸基之外，有机酸至少包含氨基，羟基和羧基中的至少一个。式I所示的化合物及其酯不是水溶性的。由化合物和酸生成的酯进一步与酸或碱反应生成水溶性盐并用于制备注射制剂。实验证明盐不会刺激血管。

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