Polymer conjugates of K-252A and derivatives thereof

摘要

Disclosed is a polymer conjugate of an indolocarbazole compound of the general formula (I) wherein Ra and Rb are independently a hydrogen or an organic residue selected from the group consisting of alkyl, alkenyl, alkynyl, hydroxy, alkoxy, carboxy or alcoxycarbonyl; or Ra and Rb together form a 5-7 member cyclic structure fused directly to the indolo[2,3-a]carbazole nucleus structure, containing 0, 1 or 2 heteroatoms; and wherein Rc and Rd and R1 and R2 are defined in the specification or a pharmaceutically acceptable salt thereof, characterized in that the compound of formula (I) has at least one functional group to which a polymeric moiety is conjugated. Also disclosed is a composition comprising said conjugate, the use of said conjugate for the manufacture of a medicament for the treatment of HMGB1-associated pathologies e.g. stenosis or arthritis and the use of said conjugate for the manufacture of a medicament for the treatment of NGF-related pain and hyperalgesia.