首页> 外国专利> NOVEL PHENYLPROPIONIC ACID DERIVATIVES AS PEROXISOME PROLIFERATOR-ACTIVATED ALPHA/GAMMA RECEPTOR AGONISTS, METHOD OF THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

NOVEL PHENYLPROPIONIC ACID DERIVATIVES AS PEROXISOME PROLIFERATOR-ACTIVATED ALPHA/GAMMA RECEPTOR AGONISTS, METHOD OF THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

机译:新型过氧苯丙酸酯衍生物作为过氧化物酶促进剂活化的α/γ受体激动剂,具有相同的方法和组成相同的药物组合物

摘要

A phenylpropionic acid derivative is provided to lower the blood sugar and lipid in blood, and improve insulin resistance by simultaneously activating gamma and alpha peroxisome proliferator-activated receptors. A phenylpropionic acid derivative is represented by the formula(1) and is prepared by the method comprising the steps of: (a) reacting a compound represented by the formula(2), (3), or (4) with a compound represented by the formula(5); (b) reacting a cyanuric chloride represented by the formula(6); (c) reacting Y; (d) reacting Z; and (e) hydrolyzing. In the formulae, R is -OCH2CH3 or -CH2CH3; X is -NCH3, -NH, -O- or methylene; each Y and X is independently lower alkyl, lower alkoxy, lower cycloalkylamine, aniline, azetine, pyrrolidine, piperidine, piperazine, morpholine, thiomorpholine, phenyl, or phenoxy, provided that each defined substituent of the Y and Z may optionally have at least one substituent selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, hydroxy, amino, nitro, trifluoromethyl, phenyl, benzyl, benzoyl, furan, thiophene, phenoxy, piperidine; n is an integer from 1 to 5; and W is methyl or ethyl. A therapeutic agent for diabetes or X-syndrome comprises the compound of the formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient.
机译:通过同时激活γ和α过氧化物酶体增殖物激活的受体,提供了一种苯丙酸衍生物,以降低血液中的血糖和脂质,并改善胰岛素抵抗。苯丙酸衍生物由式(1)表示,并通过包括以下步骤的方法制备:(a)使由式(2),(3)或(4)表示的化合物与由式(2)表示的化合物反应。公式(5); (b)使式(6)表示的氰尿酰氯反应; (c)使Y反应; (d)反应Z; (e)水解。式中,R为-OCH 2 CH 3或-CH 2 CH 3。 X为-NCH 3,-NH,-O-或亚甲基;每个Y和X独立地是低级烷基,低级烷氧基,低级环烷基胺,苯胺,a庚因,吡咯烷,哌啶,哌嗪,吗啉,硫代吗啉,苯基或苯氧基,条件是Y和Z的每个定义的取代基可任选具有至少一个选自C 1-6烷基,C 1-6烷氧基,羟基,氨基,硝基,三氟甲基,苯基,苄基,苯甲酰基,呋喃,噻吩,苯氧基,哌啶的取代基; n为1至5的整数; W是甲基或乙基。糖尿病或X综合征的治疗剂包含式(1)的化合物或其药学上可接受的盐作为有效成分。

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