benzothiazepine for the production of drugs to alleviate of epileptic seizures.

摘要

A method for ameliorating or preventing generalized tonic-clonic type epileptic seizures in mammals is provided. The method involves systemically administering to a mammal in need of such treatment a compound having the formula IMAGE I wherein X is hydrogen, a lower straight chain or branched alkyl, hydroxy, a halogen or a lower straight chain or branched alkyl halide; Y is a lower straight chain or branched alkyl; R1 is hydrogen, hydroxy or acetyloxy; R2 and R3 are each a lower straight chain or branched alkyl or a non-aromatic cycloalkyl or together are a heterocyclic, and pharmaceutically acceptable salts thereof in an amount effective to ameliorate or prevent generalized tonic-clonic type seizures. Preferred compounds are those in which X is hydrogen or 8-chloro, Y is ethyl, R1 is acetyloxy and R2 and R3 are each methyl. Most preferred compounds include (+)(2S,3S)-3-acetyloxy-5-(2-dimethylaminoethyl)-2,3-dihydro-2-(4-metho xyphenyl) 1,5-benzothiazepin-4-(5)-one and (+)(2S,3S)-3-acetoxy-8-chloro-5-(2-dimethylaminoethyl)-2,3-dihydro-2-( 4-methoxy phenyl)-1,5-benzothiazepin-4-(5H)-one.