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1. 发明授权

US07410987B2 Method for treating pain or pruritis by administering κ-opioid receptor agonist comprising 2-phenylbenzothiazoline derivative 有权
标题翻译：通过施用包含2-苯基苯并噻唑啉衍生物的卡帕阿片受体激动剂来治疗疼痛或瘙痒的方法
公开(公告)号：US07410987B2
公开(公告)日：2008-08-12
申请号：US11434028
申请日：2006-05-15
申请人： Maki Tokai , Takahiro Honda , Masashi Niwa , Yaeko Osumi , Ken-ichi Fujimura , Shin-ichi Kohno
发明人： Maki Tokai , Takahiro Honda , Masashi Niwa , Yaeko Osumi , Ken-ichi Fujimura , Shin-ichi Kohno
IPC分类号： A61K31/428 , A61P29/00
CPC分类号： C07D417/12 , A61K31/428 , C07D277/66
摘要： A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a κ opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and R1 is acyl.
摘要翻译：一种治疗疼痛或瘙痒症的方法，包括向有需要的患者施用药学有效量的下式的κ阿片受体激动剂其中R是具有氨基作为取代基的烷基; R 1是酰基。

2. 发明申请

US20060205796A1 Method for treating pain or pruritis by administering opinoid receptor agonist comprising 2-phenylbenzothiazoling derivative 有权
标题翻译：通过施用包含2-苯基苯并噻唑啉衍生物的阿片样物质受体激动剂治疗疼痛或瘙痒的方法
公开(公告)号：US20060205796A1
公开(公告)日：2006-09-14
申请号：US11434028
申请日：2006-05-15
申请人： Maki Tokai , Takahiro Honda , Masashi Niwa , Yaeko Osumi , Ken-ichi Fujimura , Shin-ichi kohno
发明人： Maki Tokai , Takahiro Honda , Masashi Niwa , Yaeko Osumi , Ken-ichi Fujimura , Shin-ichi kohno
IPC分类号： A61K31/428
CPC分类号： C07D417/12 , A61K31/428 , C07D277/66
摘要： A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a κ opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and R1 is acyl.
摘要翻译：一种治疗疼痛或瘙痒症的方法，包括向有需要的患者施用药学有效量的下式的κ阿片受体激动剂其中R是具有氨基作为取代基的烷基; R 1是酰基。

3. 发明授权

US07112598B2 κ opioid receptor agonist comprising 2-phenylbenzothiazoline derivative 有权
标题翻译： κ阿片受体激动剂，其包含2-苯基苯并噻唑啉衍生物
公开(公告)号：US07112598B2
公开(公告)日：2006-09-26
申请号：US10509549
申请日：2003-03-28
申请人： Maki Tokai , Takahiro Honda , Masashi Niwa , Yaeko Osumi , Ken-ichi Fujimura , Shin-ichi Kohno
发明人： Maki Tokai , Takahiro Honda , Masashi Niwa , Yaeko Osumi , Ken-ichi Fujimura , Shin-ichi Kohno
IPC分类号： C07D277/66 , C07D417/12 , A61K31/428 , A61P29/00 , A61P25/04
CPC分类号： C07D417/12 , A61K31/428 , C07D277/66
摘要： A compound or a salt thereof having the following formula wherein R1 is acyl, R2 is hydrogen, halogen, unsubstituted alkyl or alkyl substituted by halogen; R3 is halogen or alkoxy; R4 is cycloalkyl, unsubstituted alkyl or alkyl substituted by cycloalkyl, aryl or hydroxyl or an ester thereof or alkoxy; R5 is hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; or R4 and R5 are bonded with each other to form a pyrrolidine ring substituted by hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; R6 is hydroxyl or an ester thereof, alkoxy, alkoxyalkoxy, alkoxyalkoxyalkoxy, mercapto or alkylthio; and A1 and A2, are the same or different, and are alkylene, provided that (i) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by hydroxyl or an ester thereof, R2 is halogen; (ii) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by alkoxyalkyl, R2 is hydrogen; (iii) when R6 is hydroxyl or an ester thereof, R4 is isopropyl.
摘要翻译：具有下式的化合物或其盐，其中R 1是酰基，R 2是氢，卤素，未取代的烷基或被卤素取代的烷基; R 3是卤素或烷氧基; R 4是环烷基，未取代的烷基或被环烷基，芳基或羟基或其酯或烷氧基取代的烷基; R 5是羟基或其酯，烷氧基或烷氧基烷基; 或R 4和R 5彼此键合以形成被羟基或其酯取代的吡咯烷环，烷氧基或烷氧基烷基; R 6是羟基或其酯，烷氧基，烷氧基烷氧基，烷氧基烷氧基烷氧基，巯基或烷硫基; 和A 1和A 2各自相同或不同，并且是亚烷基，条件是（i）当R 4和R 0 > 5个彼此键合以形成被羟基或其酯取代的吡咯烷环，R 2是卤素; （ii）当R 4和R 5彼此键合以形成被烷氧基烷基取代的吡咯烷环时，R 2是氢; （iii）当R 6为羟基或其酯时，R 4为异丙基。

4. 发明申请

US20050113430A1 Kappa-opioid receptor agonist comprising 2-phenylbenzothiazoline derivative 有权
标题翻译：卡帕阿片受体激动剂包含2-苯基苯并噻唑啉衍生物
公开(公告)号：US20050113430A1
公开(公告)日：2005-05-26
申请号：US10509549
申请日：2003-03-28
申请人： Maki Tokai , Takahiro Honda , Yaeko Osumi , Ken-ichi Fujimura
发明人： Maki Tokai , Takahiro Honda , Yaeko Osumi , Ken-ichi Fujimura
IPC分类号： A61K31/428 , A61P19/02 , A61P19/06 , A61P25/04 , A61P29/00 , A61P43/00 , C07D277/66 , C07D417/12
CPC分类号： C07D417/12 , A61K31/428 , C07D277/66
摘要： The present invention provides κ opioid receptor agonists comprising 2-phenylbenzothiazoline derivatives. The present invention relates to κ opioid receptor agonists comprising compounds or salts thereof having the chemical structure represented by the general formula [I]. Namely, it is important for exhibition of the κ opioid receptor agonist actions to have an alkyl group having an amino group at a phenyl group of 2-phenylbenzothiazoline as a substituent and to have an acyl group at a nitrogen atom of 2-phenylbenzothiazoline, wherein R is alkyl having the amino group as the substituent; and R1 is acyl.
摘要翻译：本发明提供包含2-苯基苯并噻唑啉衍生物的κ阿片受体激动剂。本发明涉及具有由通式[I]表示的化学结构的化合物或其盐的κ阿片受体激动剂。即，对于具有2-苯基苯并噻唑啉的苯基具有氨基的烷基作为取代基并且在2-苯基苯并噻唑啉的氮原子上具有酰基，对于κ阿片受体激动剂作用的展示是重要的，其中 R是具有氨基作为取代基的烷基; R 1是酰基。

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