ACYLOXYALKYLCARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND APPLICATION Russian patent published in 2011 - IPC C07C271/22 C07D213/80 C07D307/46 C07D333/38 A61K31/195 A61K31/341 A61K31/381 A61K31/44 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to acyloxyalkylcarbamate prodrugs (±)4-amino-3-(4-chlorophenyl)butanoic acid, to based pharmaceutical compositions and to their application, for treating spasticity or a spasticity symptom, gastroesophageal reflux disease (GERD), drug addiction, alcohol addiction or alcohol abuse, or cough, or vomiting. Acyloxyalkylcarbamate prodrugs represent a compound of formula (V) or its pharmaceutically acceptable salt where R¹ is selected from C₁-C₆alkyl substituted by C₁-C₆alkyl, C₃-C₆cycloalkyl, phenyl, phenyl C₁-C₆alkyl substituted by phenyl C₁-C₆alkyl, phenylC₂-C₆alkenyl, C₅-C₆heteroaryl containing 1 nitrogen, oxygen or sulphur atom as a heteroatom; R² and R³ are independently selected from hydrogen, C₁-C₆alkyl and C₃-C₆cycloalkyl; R⁴ is selected from: hydrogen, phenyl, phenyl C₁-C₆alkyl and C₁-C₆alkyl and where "substituted" means a group wherein one or two hydrogen atoms are substitute by a substitute which represent C₁-C₆alkoxy. Also, the invention refers to an intermediate compound of formula (VII) and its pharmaceutically acceptable salt where X represents: fluorine, chlorine, bromine or iodine; R² and R³ are independently selected from hydrogen and C₁-C₆alkyl; R⁴ is selected from: hydrogen, C₁-C₆alkyl, phenyl and phenyl C₁-C₆alkyl.

EFFECT: preparation of the acyloxyalkylcarbamate prodrugs (±)4-amino-3-(4-chlorophenyl)butanoic acid which are applicable for the oral introduction and oral introduction with using prolonged release dosage forms.

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