mRNA cap analogs

US8519110B2 · kind B2 · utility

Assignee

• BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY AND AGRICULTURAL AND MECHANICAL COLLEGE · US

Inventors

• Joanna Kowalska · Radom, PL
• Jacek Jemielity · Warszawa, PL
• Edward Darzynkiewicz · Białystok, PL
• Robert E. Rhoads · Shreveport, US
• Maciej Lukaszewicz · Warszawa, PL
• Joanna Zuberek · Warszawa, PL

Key dates

• Filing date: Jun 4, 2009
• Grant date: Aug 27, 2013
• Expiry date: Dec 16, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12P21/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Dinucleotide cap analogs are disclosed, modified at different phosphate positions with a boranophosphate group or a phosphoroselenoate group. The analogs are useful as reagents in the preparation of capped mRNAs and have increased stability both in vitro and in vivo. They may be used as inhibitors of cap-dependent translation. Optionally, the boranophosphate or phosphoroselenoate group has a 2′-O or 3′-O-alkyl group, preferably a methyl group, producing analogs called BH3-ARCAs or Se-ARCAs. ARCAs may be modified with α-, β-, or γ-boranophosphate or phosphoroselenoate groups.