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PPAR-(GAMMA) AGONISTS AS AGENTS FOR THE TREATMENT OF TYPE II DIABETES

机译:PPAR-(GAMMA)激动剂作为II型糖尿病的治疗剂

摘要

Disclosed are compounds of formula (I) or the pharmaceutically acceptable non-toxic salts thereof wherein: Z is aryl or heteroaryl; n and m are 0, 1 or 2; A is a carboxylic acid or ester; or A is formula (II) where D, F and G are hydrogen, (un)substituted amino, (un)substituted alkoxy, methylene or an (un)substituted sulfide; X is N, O, CH2, S, SO or SO2; R4 is oxo, hydrogen, hydroxy, lower alkyl, lower alkoxy, cycloalkyl, keto, acyl, or sulfonyl; Y is hydrogen, (un)substituted amino, (un)substituted alkoxy, methylene, an (un)substituted sulfide, (un)substituted sulfonyl or an (un)substituted sulfoxide; and R5, R6 and R8 are hydrogen, lower alkyl, lower alkoxy, cycloalkyl, keto, acyl, or sulfonyl; or R5 and R6 together form a ring. The compounds are highly selective agonists for the PPAR- gamma receptor or prodrugs of agonists for the PPAR- gamma receptor. Thus these compounds are useful in the treatment Type II diabetes (NIDDM).
机译:公开了其中Z为芳基或杂芳基的式(I)化合物或其药学上可接受的无毒盐。 n和m为0、1或2; A是羧酸或酯;或A为式(II),其中D,F和G为氢,(未)取代的氨基,(未)取代的烷氧基,亚甲基或(未)取代的硫化物;或X是N,O,CH 2,S,SO或SO 2; R4是氧代,氢,羟基,低级烷基,低级烷氧基,环烷基,酮基,酰基或磺酰基; Y是氢,(未)取代的氨基,(未)取代的烷氧基,亚甲基,(未)取代的硫化物,(未)取代的磺酰基或(未)取代的亚砜; R5,R6和R8是氢,低级烷基,低级烷氧基,环烷基,酮,酰基或磺酰基; R 5和R 6一起形成环。这些化合物是PPAR-γ受体的高选择性激动剂或PPAR-γ受体的激动剂的前药。因此,这些化合物可用于治疗II型糖尿病(NIDDM)。

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