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    • 16. 发明申请
    • NEUROPEPTIDE RECEPTOR MODULATORS
    • 神经肽受体调节剂
    • WO2005111031A3
    • 2005-12-22
    • PCT/US2005014518
    • 2005-04-28
    • SCHERING CORPZHU ZHAONINGSUN ZHONG-YUEYE YUANZANMULLINS DEBORRA EMCKITTRICK BRIANSTAMFORD ANDREWGREENLEE WILLIAM J
    • ZHU ZHAONINGSUN ZHONG-YUEYE YUANZANMULLINS DEBORRA EMCKITTRICK BRIANSTAMFORD ANDREWGREENLEE WILLIAM J
    • A61K31/428A61K31/541C07D417/00C07D417/12C07D487/04C07D513/04
    • C07D487/04C07D417/12C07D513/04
    • 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, Chemical formula should be inderted here as it appears on the abstract in paper form. 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.
    • 本发明公开了作为NPY Y1的新受体拮抗剂的化合物以及制备这些化合物的方法。 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症,代谢紊乱,进食障碍如食欲过盛和糖尿病的方法。 这些化合物由结构式1表示,化学式在此以摘要形式出现在本文中应该没有改变。 其中R 1为杂芳基,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的化合物或所述前药的任何药学上可接受的盐,溶剂化物,异构体或外消旋混合物; R15存在或不存在并且如果存在则为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,环亚烷基,亚杂环烷基或杂环烷基,其中所述芳基,杂芳基,环烷基,亚环烷基,亚杂环烷基和杂环烷基部分可以被取代或未被取代; 并且B,L,X和R 18如本文所定义。