Topical ocular application of 3-aryloxy-2-hydroxy propylamine derivs. - for treating without systemic beta-blocker side-effects

摘要

Glaucoma or high intraocular pressure is treated by the topical ocular application of a 3-aryloxy-2-hydroxypropylamine beta-blocker of the formula (RO.CO.A)x-Ar-O-CH2CH(OH)CH2NHR1 (I) or its salts:- (where R is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl or aryl carboxymethyl, haloloweralkyl, aryl or aralkyl; A is a bond, lower alkylenyl or lower alkenyl (sic); x is 1, 2 or 3, provided that when x is 2 or 3 the groups ROCOA may be same or different; Ar is aromatic opt. substd. by lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, OH, hydroxyloweralkyl or CN; R1 is lower alkyl, hydroxyloweralkyl, lower alkenyl, lower alkynyl, or aralkyl). (I) have sustained antiglaucoma activity when in the eye, but are short lived on reaching the general circulation. Side effects are much reduced as compared with the usual beta blockers used for treating glaucoma.