| abstract |
Novel biologically-active tetracyclic spirohydantoin derivatives of formulan nwhereinn X is hydrogen, fluorine, chlorine or methyl; and R is hydrogen, alkyl, alkenyl, cycloalkyl, benzy, 4-hydroxy- benzy!, pyridyl, HSCH 2 -, CH 3 SCH 2 -, CH 3 SCH 2 CH 2 -, FCH 2 -, HOCH 2 -, CH 2 CH(OH)-, CH 3 CH(OH)CH 2 -, HOOCCH 2 -, HOOCCH 2 CH 2 -, H 2 NCOCH 2 -, H 2 NCOCH 2 CH 2 -, H 2 NCH 2 CH 2 -n n COOC 2 H 5 , -CONH 2 , CONH(CH 2 ) 2 0H, -CONH cyclohexyl, -CONH-Bu, -CONH(CH 2 ) 3 N(CH 3 ) 2 , -CON(C 2 H 5 ) 2 ,n phenyl or phenyl substituted by chlorine, fluorine, bromine, hydroxy, methyl, methoxy, trifluoromethyl, -COCH 3 , -N(CH 3 ) 2 , -SCH 3 , -SOCH 3 , -SO 2 CH 3 , -COOH, -CONH 2 , -COOCH 3 or -CON Alk, are disclosed. n These derivatives are potent inhibitors of aldose reductase and useful in treating diabetic complications are disclosed. n Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed. |