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    • 10. 发明申请
    • (3-{3-‘(2,4-BIS-TRIFLUORMETHYL-BENZYL)-(5-ETHYL-PYRIMIDIN-2-YL)-AMINO!-PROPOXY}-PHENYL)-ACETIC ACID AND RELATED COMPOUNDS AS MODULATORS OF PPARS AND METHODS OF TREATING METABOLIC DISORDERS
    • (3- {3 - ((2,4-BIS-三氟甲基)苄基) - (5-乙基 - 嘧啶-2-基) - 氨基} - 苯基) - 甲酸和相关化合物作为PPARS的调节剂 治疗代谢障碍的方法
    • WO2004093879A1
    • 2004-11-04
    • PCT/US2004/010970
    • 2004-04-07
    • KALYPSYS, INC.LIU, KevinZHAO, Cunxiang
    • LIU, KevinZHAO, Cunxiang
    • A61K31/505
    • C07D239/42C07D213/38C07D213/74C07D263/58C07D277/82
    • Disclosed are compounds of formula I as modulators of peroxisome proliferator activated receptors (PPARs) for the treatment of metabolic diseases such as obesity: wherein Ar 1 is selected from the group consisting of a monocyclic heteroarornatic ring structure and a bicyclic heteroaromatic ring structure; Ar 2 is selected from the group consisting of a monocyclic, a bicyclic, and a tricyclic carbocyclic aryl ring structure R 1 is selected from the group consisting of alkyl, optionally substituted a five-membered or six-membered heteroarylring or a six-membered aryl ring, optionally substituted R 2 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituied cyano; nitro; an amino; an amido; perhaloalkyl; and halogen; R 3 is selected from the group consisting of hydrogen; alkyl, optionally substituted and B is a five-membered or six-membered heteroaryl ring, or -(CH 2 )j-C(O)OR 4 , wherein j is 0 or I 1 when Ar 2 is a bicyclic or tricyclic carbocyclic ring structure and j is 1 when Ar 2 is a monocyclic carbocyclic ring structure; and R 4 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituted. The obtional substituents are as defined in claim 1.
    • 公开了作为用于治疗代谢疾病如肥胖症的过氧化物酶体增殖物激活受体(PPAR)的调节剂的式I化合物:其中Ar1选自单环杂芳环结构和双环杂芳环结构; Ar 2选自单环,双环和三环碳环芳基环结构,R 1选自烷基,任选被五元或六元杂芳基环或六元芳环取代, 任选取代的R 2选自氢; 烷基,任选取代五元或六元杂芳环或六元芳环,任选取代的氰基; 硝基; 氨基; 一个amido; 全卤; 和卤素; R3选自氢; 烷基,任选取代,B是五元或六元杂芳环,或 - (CH 2)j C(O)OR 4,其中当Ar 2是双环或三环碳环结构时,j是0或I 1,并且j是1 当Ar 2是单环碳环结构时; 并且R 4选自氢; 烷基,任选被取代的任选被取代的五元或六元杂芳基环或六元芳环。 所述取代基如权利要求1所定义。