PROCESS FOR THE PREPARATION OF POLYHYDROXY-BENZYLOXYPROPANOLAMINES AND PHARMACEUTICAL COMPOSITIONS THEREOF

摘要

Compounds of the present invention, are represented by the general formula wherein R1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R2, R3 and R4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents -NHCOR5, -NHCONR5R6, or -NHCOOR5 wherein R5 and R6 may be the same or different and represent hydrogen, alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, cycloalkyl of from 3 to about 8 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 6 carbon atoms, phenyl which may be unsubstituted or substituted with alkyl of 1 to 6 carbon atoms; furanyl, thiophenyl, imidazole, oxazole or indole, aralkyl wherein the alkyl group contains from 1 to about 6 carbon atoms and the aryl group represents phenyl unsubstituted or substituted with alkyl of from 1 to about 6 carbon atoms, or R5 and R6 may together with N form a pyrrolidine, piperidine, piperazine, morpholine or thiomorpholine ring and except that R5 is not hydrogen when B is -NHCOOR5; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment or prophylaxis of cardiac disorders or in the treatment of glaucoma.