公开(公告)号：US20060089351A1

公开(公告)日：2006-04-27

申请号：US11117584

申请日：2005-04-28

申请人： Zhaoning Zhu ,  Zhong-Yue Sun ,  Yuanzan Ye ,  Deborra Mullins ,  Brian McKitrtick ,  Andrew Stamford ,  William Greenlee

发明人： Zhaoning Zhu ,  Zhong-Yue Sun ,  Yuanzan Ye ,  Deborra Mullins ,  Brian McKitrtick ,  Andrew Stamford ,  William Greenlee

IPC分类号： A61K31/541 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/427 ,  C07D417/02

CPC分类号： C07D487/04 ,  C07D417/12 ,  C07D513/04

摘要： The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The compounds are represented by the structural Formula 1, a prodrug thereof, or any pharmaceutically acceptable salt, solvate, isomer or racemic mixture of the compound or said prodrug wherein R1 is heteroaryl, N-arylaminocarbonyl, N-heteroarylaminocarbonyl, benzimidazolyl or benzothiazolyl; R15 is present or not and if present is H, aryl, alkyl, arylalky or heteroarylalkyl; A is aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene or heterocycloalkyl wherein said aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene and heterocycloalkyl moieties may be substituted or unsubstituted; and B, L, X and R18 are defined herein.

摘要翻译： 本发明公开了作为NPY Y1的新受体拮抗剂的化合物以及这些化合物的制备方法。 在另一个实施方案中，本发明公开了包含这种NPY Y1受体拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。 化合物由结构式1表示，其前体药物或化合物或所述前体药物的任何药学上可接受的盐，溶剂合物，异构体或外消旋混合物，其中R 1是杂芳基，N-芳基氨基羰基，N - 杂芳基氨基羰基，苯并咪唑基或苯并噻唑基; R 15存在或不存在，如果存在，则为H，芳基，烷基，芳基烷基或杂芳基烷基; A是芳基，杂芳基，环烷基，环烷叉基，杂环亚烷基或杂环烷基，其中所述芳基，杂芳基，环烷基，亚环烷基，杂环亚烷基和杂环烷基部分可以是取代或未取代的; 和B，L，X和R 18在本文中定义。