Marion Laboratories

William R Morrone

Ray H Zobrist

Seizures are ameliorated with certain benzothiazepines.

Benzothiazepine anti-seizure method

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 ##STR1## 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; R.sub.1 is hydrogen, hydroxy or acetyloxy; R.sub.2 and R.sub.3 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, R.sub.1 is acetyloxy and R.sub.2 and R.sub.3 are each methyl. Most preferred compounds include (+)(2S,3S)-3-acetyloxy-5-(2-dimethylaminoethyl)-2,3-dihydro-2-(4-methoxyph enyl) 1,5-benzothiazepin-4-(5)-one and (+)(2S,3S)-3-acetoxy-8-chloro-5-(2-dimethylaminoethyl)-2,3-dihydro-2-(4-me thoxy phenyl)-1,5-benzothiazepin-4-(5H)-one.

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Olathe, KS, United States of America

William R Morrone