Derivatives of 5-carbamoyloxymethyl-3-substituted-2-oxazolidinones, process of preparation thereof and therapeutic application

Abstract

A compound of the formula ##STR1## .[.in which R is H, halogen, alkyl having 1 to 4 carbon atoms or trifluoromethyl, and R 1 and R 2 each is H or dialkylaminoalkyl or together with N comprise methylpiperazino..]. .Iadd.in which (1) .Iadd. ##STR2##.Iaddend. is -NH 2 and R is H, m-CH 3 , o-CF 3 , m-Cl, p-Cl, m-Br, m-F, p-F, o-F, p-CH 3 or m-CH 3 , or .Iadd. ##STR3##.Iaddend. and R is H, m-CF 3 or m-F, or .Iadd. ##STR4##.Iaddend. and R is H, m-CF 3 or m-F. The compound is prepared by treating the corresponding 5-hydroxymethyl compound with ammonia or an amine in the presence of phosgene. The compounds possess anti-depressive, myorelaxing, tranquilizing, sedative, analgesic, anti-convulsive, anti-pyretic, anti-inflammatory and uricosuric activities.

What we claim is: .[.1. A compound of the formula ##STR16## in which R is hydrogen, halogen, alkyl having 1 to 4 carbon atoms and trifluoromethyl, and 
     
        and the pharmaceutically acceptable acid addition salts thereof..]. .[.2. A compound as claimed in claim 1, in which R is a chlorine, bromine or 
     
     
        fluorine atom..]. .Iadd.3.  A compound of the formula .Iadd. ##STR18##.Iaddend. in which (1)  .Iadd. ##STR19##.Iaddend. is --NH 2  and R is H, m-CF 3 , o-CF 3 , m-Cl, p-Cl, m-Br, m-F, p-F, o-F, p-CH 3  or m-CH 3 , or  .Iadd. ##STR20##.Iaddend. and R is H, m-CF 3  or m-F, or  .Iadd. ##STR21##.Iaddend. and R is H, m-CF 3  or m-F, and the pharmaceutically acceptable acid addition salts thereof.