Neuropeptide Y5 receptor antagonists
    51.
    发明授权
    Neuropeptide Y5 receptor antagonists 失效
    神经肽Y5受体拮抗剂

    公开(公告)号:US06329395B1

    公开(公告)日:2001-12-11

    申请号:US09326575

    申请日:1999-06-07

    IPC分类号: A61K31445

    摘要: Compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; X is —O—, —S—, —SO—, —SO2—, —CH(OR8)—, —C(O)—, —C(R23)2—, optionally substituted alkenyl, alkynyl or; R1 is optionally substituted aryl, heteroaryl, substituted amino, alkyl-OC(O)R8, aryloxyalkyl,  wherein m is 1-4, or  wherein d and e are 0-2; R2, R3, R4 and R5 are H, alkyl, optionally substituted cycloalkyl, halogen, —OR8, —N(R8)2, —CO2R8 or CF3; R6 and R7 are H, alkyl, alkenyl, hydroxyalkyl, aminoalkyl, alkoxy-alkyl, cycloalkyl or cycloalkylalkyl, or R6 and R7, form a 3-7-membered carbocyclic ring, or a 4-7-membered heterocyclic ring; R8 is H, alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R9 is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R11 is H, alkyl or cycloalkyl; and R23 is R8 or halogen; are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using said novel compounds in the treatment of eating disorders and diabetes.

    摘要翻译: 式I的化合物或其药学上可接受的盐,其中a和b为0-2,条件是总和为0-3; X是-O - , - S - , - SO - , - SO 2 - , - CH(OR 8 ) - , - C(O) - , - C(R 23)2 - ,任选取代的烯基,炔基或R 1是任选取代的芳基,杂芳基,取代的氨基,烷基-C(O)R 8,芳氧基烷基,其中m是1 -4或其中d和e为0-2; R 2,R 3,R 4和R 5为H,烷基,任选取代的环烷基,卤素,-OR 8,-N(R 8)2,-CO 2 R 8或CF 3; R 6和R 7为 H,烷基,烯基,羟基烷基,氨基烷基,烷氧基 - 烷基,环烷基或环烷基烷基,或R6和R7形成3-7元碳环或4-7元杂环; R8是H,烷基,环烷基 ,任选取代的芳基或杂芳基; R 9为烷基,环烷基,任选取代的芳基或杂芳基; R 11为H,烷基或环烷基; R 23为R 8或卤素; 以及其他新型化合物; 还要求的是使用所述新型化合物治疗进食障碍和糖尿病的药物组合物和方法。