Method of ameliorating epileptic seizures

C - Chemistry – Metallurgy – 07 – D

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C07D 281/10 (2006.01) A61K 31/55 (2006.01)

Patent

CA 1317593

Abstract of the Disclosure A method for ameliorating or preventing general- ized 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 ef- fective to ameliorate or prevent generalized tonic-clonic type seizures. Preferred compounds are those in which X is hydrogen or a-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-methoxyphenyl)-1,5-benzothiazepin-4-(5)-one and (+)(2S,3S)-3-acetoxy-a-chloro-5-(2-dimethylaminoethyl)-2,3- dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4-(5H)-one.

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