Single chemical entities and methods for delivery of oligonucleotides

US8691580B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Jeffrey Aaronson · Johnstown, US
• Stanley F. Barnett · North Wales, US
• René Bartz · Lawrenceville, US
• Steven L. Colletti · Princeton Junction, US
• Vasant Jadhav · Cambridge, US
• Aaron Momose · Johnstown, US
• Anthony W. Shaw · Johnstown, US
• David M. Tellers · Lansdale, US
• Thomas J. Tucker · North Wales, US
• Weimin Wang · Hangzhou City, CN
• Yu Yuan · Sichuan, CN

Key dates

• Filing date: Apr 4, 2011
• Grant date: Apr 8, 2014
• Expiry date: Apr 4, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K19/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at any 3′ and/or 5′ end; 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.