| abstract |
Lipophilic, transient ester derivatives of timolol represented by general formula (I), wherein R1 represents a substituted or unsubstituted branched chain alkyl, straight or branched chain alkenyl, aryl, aralkyl or cycloalkyl group, a substituted or unsubstituted aromatic 5- or 6-membered heterocyclic ring containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, or a substituted or unsubstituted group of the formula R2-O-, wherein R2 is an alkyl, aryl, aralkyl or cycloalkyl group or of the formula R'2-CONH, wherein R'2 is an alkyl, aryl, aralkyl or cycloalkyl group, and nontoxic pharmaceutically acceptable acid addition salts thereof, are disclosed as prodrug forms of the anti-glaucoma drug timolol which are also useful in the treatment of glaucoma and increased intraocular pressure and which exhibit either improved corneal absorption and/or impeded conjunctival absorption characteristics, thus permitting the use of smaller doses of such derivatives than of timolol, thereby reducing systemic timolol concentration while achieving the same therapeutic effect. |