Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1988-05-24
1989-11-07
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
A61K 3155
Patent
active
048792896
ABSTRACT:
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.
REFERENCES:
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Morrone William R.
Zobrist Ray H.
Friedman Stanley J.
Gillis Theresa M.
Marion Laboratories, Inc.
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