ACYLOXYALKYL CARBAMATE PRODRUG, METHOD OF SYNTHESIS AND USE

摘要

PROBLEM TO BE SOLVED: To provide new prodrugs of baclofen and baclofen analogs which are well absorbed in the large intestine/colon and hence suitable for oral sustained release formulations, thus improving the convenience, efficacy and side effect profile of baclofen therapy.

SOLUTION: This invention relates to: acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof, wherein R5 is 4-fluorophenyl; methods of making prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof; and methods of using prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease.

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