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1. 发明授权

US4496755A Optically active 1-(6-methoxy-2-naphthyl)-2-(alkoxycarbonyl) amino-1-propanone, its derivatives and their halo analogs and the methods for their manufacture 失效
标题翻译：光学活性1-（6-甲氧基-2-萘基）-2-（烷氧基羰基）氨基-1-丙酮及其衍生物及其卤素类似物及其制备方法
公开(公告)号：US4496755A
公开(公告)日：1985-01-29
申请号：US479768
申请日：1983-03-28
申请人： Genichi Tsuchihashi , Shuichi Mitamura , Koji Kitajima , Kumi Kobayashi
发明人： Genichi Tsuchihashi , Shuichi Mitamura , Koji Kitajima , Kumi Kobayashi
IPC分类号： A61K31/19 , A61P29/00 , C07C51/00 , C07C51/09 , C07C59/64 , C07C67/00 , C07C239/00 , C07C271/18 , C07C125/067 , C07C125/02
CPC分类号： C07C51/09
摘要： A manufacturing method is described for the preparation of optically active 1-(6-methoxy-2-naphthyl)-2-(alkoxycarbonyl)amino-1-propanone, its derivatives and their halo analogs. The optically active 1-(6-methoxy-2-naphthyl)-2-(alkoxycarbonyl)amino-1-propanone, its derivatives and their halo analogs are useful intermediates in the preparation of 2-(6-methoxy-2-naphthyl)propionic acid, which is useful as pharmaceutical, e.g. antiinflammatory, analgesic and anti-pyretic agents.
摘要翻译：描述了制备光学活性1-（6-甲氧基-2-萘基）-2-（烷氧基羰基）氨基-1-丙酮及其衍生物及其卤代类似物的制备方法。光学活性的1-（6-甲氧基-2-萘基）-2-（烷氧基羰基）氨基-1-丙酮及其衍生物及其卤素类似物是制备2-（6-甲氧基-2-萘基）丙酸，其可用作药物，例如抗炎，止痛和抗热解剂。

2. 发明申请

US20110230538A1 PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS 审中-公开
标题翻译：用于治疗尿毒症的药物
公开(公告)号：US20110230538A1
公开(公告)日：2011-09-22
申请号：US13086040
申请日：2011-04-13
申请人： Mamoru Kobayashi , Yoshitaka Tomiyama , Kumi Kobayashi
发明人： Mamoru Kobayashi , Yoshitaka Tomiyama , Kumi Kobayashi
IPC分类号： A61K31/404 , A61P13/12 , A61P25/04
CPC分类号： C07D209/08 , A61K31/4045
摘要： The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di (lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R1 represents cyano or carbamoyl; and R2 represents lower alkyl which may have as a substituent halogen, cyano or aryl.
摘要翻译：本发明提供了用于缓解由输尿管结石引起的疼痛，有助于排除输尿管结石等的药物组合物。也就是说，本发明提供了用于治疗输尿管结石的药物组合物，其包含作为活性成分的由以下通式（I）表示的二氢吲哚衍生物或其盐。在该式中，R表示可具有取代基的饱和或不饱和脂肪族酰基; 羟烷基脂肪酰氧基烷基; 羧基，低级烷氧基羰基，芳基取代的低级烷氧基羰基，氨基甲酰基，一或二（低级烷基）取代的氨基甲酰基或氰基的低级烷基; 任选取代的芳族酰基; 糠酰基或吡啶基羰基; R1表示氰基或氨基甲酰基; 并且R 2表示可以具有卤素，氰基或芳基的取代基的低级烷基。

3. 发明申请

US20090163571A1 PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS 审中-公开
标题翻译：用于治疗尿毒症的药物
公开(公告)号：US20090163571A1
公开(公告)日：2009-06-25
申请号：US12093230
申请日：2006-11-22
申请人： Mamoru Kobayashi , Yoshitaka Tomiyama , Kumi Kobayashi
发明人： Mamoru Kobayashi , Yoshitaka Tomiyama , Kumi Kobayashi
IPC分类号： A61K31/404 , A61P13/00
CPC分类号： C07D209/08 , A61K31/4045
摘要： The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di(lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R1 represents cyano or carbamoyl; and R2 represents lower alkyl which may have as a substituent halogen, cyano or aryl.
摘要翻译：本发明提供了用于缓解由输尿管结石引起的疼痛，有助于排除输尿管结石等的药物组合物。也就是说，本发明提供了用于治疗输尿管结石的药物组合物，其包含作为活性成分的由以下通式（I）表示的二氢吲哚衍生物或其盐。在该式中，R表示可具有取代基的饱和或不饱和脂肪族酰基; 羟烷基; 脂肪酰氧基烷基; 羧基，低级烷氧基羰基，芳基取代的低级烷氧基羰基，氨基甲酰基，一或二（低级烷基）取代的氨基甲酰基或氰基的低级烷基; 任选取代的芳族酰基; 糠酰基或吡啶基羰基; R1表示氰基或氨基甲酰基; 并且R 2表示可以具有卤素，氰基或芳基的取代基的低级烷基。

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