申请人:Sankyo Company Limited
公开号:US04933355A1
公开(公告)日:1990-06-12
Compounds of formula (I): ##STR1## in which: R.sup.1 and R.sup.2 are independently hydrogen, alkyl, aliphatic hydrocarbon groups having one or two carbon-carbon double or treble bonds, cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, alkanoyl, alkenyol, cycloalkylcarbonyol, arylcarbonyl, substituted arylcarbonyl, arylalkanoyl, substituted arylalkanoyl, arylalkenoyl, substituted arylalkenoyl, alkoxycarbonyl, aryloxycarbonyl, substituted aryloxycarbonyl, aralkyloxycarbonyl, substituted aralkyloxycarbonyl, optionally substituted carbamoyl or thiocarbamoyol, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl, substituted arylsulfonyl, alkylthio, arylthio and substituted arylthio, or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group; one of R.sup.a and R.sup.b is hydrogen, alkyl or halogen, and the other of R.sup.a and R.sup.b is a group of formula (II): ##STR2## R.sup.4 is hydrogen, carboxy, protected carboxy or optionally substituted carbamoyl; R.sup.5 is hydrogen, or carboxyalkyl or protected carboxyalkyl in which the alkyl part is C.sub.1 -C.sub.6 ; n=0, 1 or 2; X is oxygen or sulfur; are useful in the treatment of the complications attendant upon diabetes and may be prepared by condensation of a thiazolidine or rhodanine compound with a compound corresponding to the remainder of the molecule of the compound of formula (I).
式(I)的化合物:##STR1## 其中:R.sup.1和R.sup.2独立地为氢、烷基、具有一个或两个碳-碳双键或三键的脂肪烃基、环烷基、芳基、取代芳基、芳基烷基、取代芳基烷基、烷酰基、烯酰基、环烷基羰基、芳基羰基、取代芳基羰基、芳基烷酰基、取代芳基烷酰基、芳基烯酰基、取代芳基烯酰基、烷氧羰基、芳氧羰基、取代芳氧羰基、芳基烷氧羰基、取代芳基烷氧羰基、可选取代的氨基甲酰基或硫脲甲酰基、烷基磺酰基、卤代烷基磺酰基、芳基磺酰基、取代芳基磺酰基、烷基硫、芳基硫和取代芳基硫,或R.sup.1和R.sup.2与它们附着的氮原子一起形成含氮杂环基团;R.sup.a和R.sup.b中的一个为氢、烷基或卤素,另一个为式(II)的基团:##STR2## R.sup.4为氢、羧基、保护羧基或可选取代的氨基甲酰基;R.sup.5为氢,或者C.sub.1-C.sub.6烷基部分为羧基烷基或保护羧基烷基;n=0、1或2;X为氧或硫;在糖尿病并发症的治疗中有用,并且可以通过将噻唑啉或罗丹明化合物与化合物的分子式(I)的其余部分相对应的化合物缩合制备。