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11. 发明公开

KR1020100053458A 멜라노코틴 수용체의 항진제 有权
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020100053458A
公开(公告)日：2010-05-20
申请号：KR1020090108283
申请日：2009-11-10
申请人： 주식회사 엘지생명과학
发明人： 이구 , 이상대 , 문상필 , 안인애 , 최성필 , 이현호 , 심동섭 , 정수용 , 이현민
IPC分类号： C07D403/14 , C07D401/14 , A61K31/4025 , A61P3/10
CPC分类号： C07D417/14 , A61K31/4025 , A61K31/496 , C07D207/16 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14
摘要： PURPOSE: A compound having excellent activity to melanocortin is provided to apply to functional agonist of the melanocortin receptor and to prevent and treat obesity, electrile dysfunction, diabetes, or inflammation. CONSTITUTION: A composition having excellent activity to melanocortin receptor is denoted by chemical formula 1. The compound of chemical formula 1 is obtained by amide-coupling a compound of chemical formula 2 with a compound of chemical formula 3. A method for preparing the compound of chemical formula 1 comprises: a step of deprotecting a compound of chemical formula 1' or 2'; a step of performing reductive amine reaction of oxo substituent with C1-C2 alkyl, C3-C7 cycloalkyl, or heterocycle; or a step of performing coupling reaction with arylhalide or hetero arylhalide. The composition contains pharmaceutically acceptable carrier, and the compound of chemical formula 1, pharmaceutically acceptable salt, or isomer. The composition is used for treating obesity, electrile dysfunction, diabetes, or inflammation.
摘要翻译：目的：提供对黑皮质素具有优异活性的化合物以适用于黑皮质素受体的功能性激动剂并预防和治疗肥胖症，电功能障碍，糖尿病或炎症。构成：化学式1表示对黑皮质素受体具有优异活性的组合物。化学式1的化合物通过化学式2的化合物与化学式3的化合物酰胺偶联而获得。一种制备化合物化学式1包括：使化学式1'或2'的化合物脱保护的步骤; 氧代取代基与C 1 -C 2烷基，C 3 -C 7环烷基或杂环进行还原胺反应的步骤; 或与芳基卤或异芳基卤化物进行偶联反应的步骤。组合物含有药学上可接受的载体，化学式1的化合物，药学上可接受的盐或异构体。该组合物用于治疗肥胖症，电疗功能障碍，糖尿病或炎症。

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