Thiazolidine and oxazolidine derivatives, their preparation and their medical use
申请人:SANKYO COMPANY LIMITED
公开号:EP0678511A2
公开(公告)日:1995-10-25
Compounds of formula (I) :
[in which : R1 and R2 are each hydrogen or alkyl, or together a group of formula -(CH2)k- in which k is an integer ; R3 is hydrogen, alkyl, alkoxy, halogen or hydroxy ; A and B are each hydrogen, alkyl, aralkyl, aliphatic carboxylic acyl, aryl-substituted aliphatic carboxylic acyl, aromatic carboxylic acyl or carbamoyl, or A and B together represent >C=O, >C=S, -C(=O)-C(=O)-, -CH2C(=0)-, -CH2CH2-, -SO2- or -CH2SO2- ; X is a group of formula : W-(CH2)m-X1- in which W is aryl or heterocyclic, X1 is a single bond, oxygen, sulphur or >NR4 in which R4 is hydrogen, alkyl, aralkyl or aryl, and m is 0 or an integer ; Y is a group of formula : -(CH2)n-Y1-, in which Y1 is a single bond, oxygen or sulphur, and n is an integer ; Z is a group of formula (i), (ii), (iii), (iv), (v) or (vi) :
in which R5 is hydrogen, carboxyalkyl, alkanoyloxyalkyl, cycloalkyl-substituted alkanoyloxyalkyl, cycloalkylcarbonyloxyalkyl, alkoxycarbonyloxyalkyl, cycloalkyl-substituted alkoxycarbonyloxyalkyl or cycloalkyloxycarbonyloxyalkyl group] ; and salts, esters and solvates thereof and pro-drugs therefor are useful for the treatment and/or prophylaxis of a variety of disorders, including one or more of: hyperlipemia, hyperglycemia, obesity, glucose tolerance insufficiency, insulin resistance and diabetic complications.
式(I)化合物:
[其中 :R1 和 R2 分别为氢或烷基,或共同为式-(CH2)k-的基团,其中 k 为整数;R3 为氢、烷基、烷氧基、卤素或羟基;A 和 B 分别是氢、烷基、芳烷基、脂肪族羧酰基、芳基取代的脂肪族羧酰基、芳香族羧酰基或氨基甲酰基,或者 A 和 B 共同代表 >C=O、>C=S、-C(=O)-C(=O)-、-CH2C(=0)-、-CH2CH2-、-SO2- 或 -CH2SO2-;X 是一个式基团:W-(CH2)m-X1-,其中 W 是芳基或杂环,X1 是单键、氧、硫或 >NR4,其中 R4 是氢、烷基、芳基或芳基,m 是 0 或整数; Y 是式中的基团 :-(CH2)n-Y1-,其中 Y1 是单键、氧或硫,n 是整数; Z 是式(i)、(ii)、(iii)、(iv)、(v)或(vi)的基团:
其中 R5 是氢、羧基烷基、烷酰氧基烷基、环烷基取代的烷酰氧基烷基、环烷基羰基氧基烷基、烷氧基羰基氧基烷基、环烷基取代的烷氧基羰基氧基烷基或环烷氧基羰基氧基烷基];其盐类、酯类和溶解物及其原药可用于治疗和/或预防多种疾病,包括以下一种或多种疾病:高脂血症、高血糖、肥胖、葡萄糖耐量不足、胰岛素抵抗和糖尿病并发症。