主权项 |
1. A compound comprising a calcium channel blocker residue covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer, wherein the calcium channel blocker residue is a residue of a calcium channel blocker having the formulawherein:
R is hydrogen or lower alkyl; R1 and R2 are each independently selected from the group consisting of hydrogen, substituted lower alkyl, unsubstituted lower alkyl, and —YOYNR6R7, where each Y is independently lower alkylene and R6 and R7 are each independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl; R3 and R4 are each independently selected from the group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, and —YNR6R7, where Y is lower alkylene and R6 and R7 are each independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl; and each R5 is independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, chloro, fluoro and nitro,wherein the water-soluble, non-peptidic oligomer is made of 2 to 30 monomers,or pharmaceutically acceptable salts thereof. |