Nucleosidic and non-nucleosidic folate conjugates

US6861514B2 · kind B2 · utility

Assignee

• Isis Pharmaceuticals, Inc. · US

Inventors

• Phillip Dan Cook · Carlsbad, US
• Muthiah Manoharan · Carlsbad, US
• Balkrishen Bhat · Carlsbad, US
• Andrei P. Guzzaev · Carlsbad, US

Key dates

• Filing date: Oct 9, 2001
• Grant date: Mar 1, 2005
• Expiry date: Jun 12, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D475/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2′-, 3′-, 5′-, nucleobase and internucleotide linkage sites. The folate can be attached via the α- or γ-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are disclosed. Also disclosed are nucleosidic and non-nucleosidic linkers conjugated to folic acid and related folates.