Oligomer-calcium channel blocker conjugates

摘要

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.

主权项

1. A compound comprising a calcium channel blocker residue covalently attached via a stable linkage to a water-soluble, non-peptidic oligomer, wherein the calcium channel blocker residue is a residue of a calcium channel blocker having the formula:wherein:
R1 is a member selected from the group consisting of lower alkyl, cyclohexyl, and phenyl; each R is independently selected from the group consisting of hydrogen, chlorine, lower alkoxy and lower alkyl, wherein at least one R is selected from chlorine, lower alkoxy and lower alkyl; and (n) is an integer from 2 to 3, inclusive; andwherein the water soluble, non-peptidic oligomer is made of 2 to 30 monomers.