Dipeptide-based prodrug linkers for aliphatic amine-containing drugs

US9062094B2 · kind B2 · utility

Assignee

• ASCENDIS PHARMA A/S · DK

Inventors

• Harald Rau · Würzburg, DE
• Torben Lessmann · Neustadt an der Weinstraße, DE

Key dates

• Filing date: Jan 21, 2011
• Grant date: Jun 23, 2015
• Expiry date: Jan 21, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K1/1077
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.