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New phenyl compounds are peroxisome proliferator activated receptor activators useful to treat hyperlipidemia and atherosclerosis

机译:新的苯基化合物是过氧化物酶体增殖物激活的受体激活剂,可用于治疗高脂血症和动脉粥样硬化

摘要

Phenyl compounds (I) are new. Phenyl compounds of formula (I) are new. A : -(C?=C)- or -(CH2)m-; m : 1-3; Y1H or OH; X1, X2-(CH2)n- or =CH-; R1, R21-8C alkyl or aryl; Z : O, S or -CH2-; and R3-R5H, 1-6C alkyl (optionally substituted). Provided that X1 and X2 do not simultaneously represent =CH-. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Antilipemic; Antiarteriosclerotic. MECHANISM OF ACTION : Peroxisome proliferator activated receptor (PPAR) activator. The agonistic activity of (I) with PPAR was tested. The results showed that 2-[4-(3-hexyl-non-3-en-1-ynyl)phenoxy]-2-methyl-propanoic acid exhibited an EC50 value of 383 nM against PPAR-beta /delta .
机译:苯基化合物(I)是新的。式(I)的苯基化合物是新的。 A :-( C2 = C)-或-(CH2)m-; m:1-3; Y1H或OH; X1,X2-(CH2)n-或= CH-; R1,R21-8C烷基或芳基; Z:O,S或-CH 2-;和R3-R5H,1-6C烷基(任选取代)。假设X1和X2不同时代表= CH-。包括独立权利要求用于制备(I)。活动:抗血脂;抗动脉硬化。作用机理:过氧化物酶体增殖物激活受体(PPAR)激活剂。测试了(I)与PPAR的激动活性。结果表明,2- [4-(3-己基-非-3-烯-1-炔基)苯氧基] -2-甲基-丙酸相对于PPAR-β/δ的EC50值为383 nM。

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