Small molecule conjugates for intracellular delivery of biologically active compounds

US9301990B2 · kind B2 · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Philipp Hadwiger · Kulmbach, DE
• Torsten Hoffmann · Weil am Rhein, DE
• Kerstin Jahn-Hofmann · Neu-Isenburg, DE
• Eric A. Kitas · Aesch, CH
• David L. Lewis · Madison, US
• Peter Mohr · Basel, CH
• Hans Martin Mueller · Weilheim, DE
• Guenther Ott · Bayreuth, DE
• Ingo Roehl · Memmelsdorf, DE
• David B. Rozema · Madison, US

Key dates

• Filing date: Jun 13, 2013
• Grant date: Apr 5, 2016
• Expiry date: Jun 13, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12N2320/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention provides novel compounds and conjugates of these compounds useful for the delivery of biologically active substances. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to a delivery polymer to achieve in vivo mRNA knock down are disclosed therein.