Patent ID: 6030997
Filing Date: 2000-02-29
Classification: A61K,C07H

Abstract:
A pharmaceutically acceptable prodrug that is a covalent conjugate of a pharmacologically active compound and at least one blocking group, wherein the covalent bond is reactively labile at a pH value between pH 4.0 and 7.0, having the general formula: ##STR11## wherein, RX-denotes a pharmacologically active agent;X is selected from the group consisting of O and NH;R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of branched or straight chain alkyl groups comprising 1-18 carbon atoms, aryl groups; andR.sub.2 and R.sub.3 may be combined to form a cyclic structure;Z is selected from the group consisting of OH, NHY, and SH; andY is selected from the group consisting of H, R.sub.4, or NH.sub.2, wherein R.sub.4 is selected from the group of lower alkyl and aryl groups.