Small molecule conjugates for intracellular delivery of nucleic acids

US9198947B2 · 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: Dec 1, 2015
• Expiry date: Jul 12, 2033

Classification

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

Abstract

The invention provides use of novel compounds for delivery of nucleic acids, and conjugates of these compounds with nucleic acids. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to said compounds and co-administered with a delivery polymer to achieve mRNA knock down in vivo are disclosed therein.