Epothilone derivatives and their synthesis and use

US7579366B2 · kind B2 · utility

Assignee

• THE SCRIPPS RESEARCH INSTITUTE · US

Inventors

• Kyriacos C. Nicolaou · Philadelphia, US
• Nigel Paul King · Harlow, GB
• Maurice Raymond Verschoyle Finlay · Cambridge, GB
• Yun He · San Diego, US
• Frank Roschangar · Glen Allen, US
• Dionisios Vourloumis · San Diego, US
• Hans Vallberg · Huddinge, SE
• Antony Bigot · Massy, FR

Key dates

• Filing date: Mar 11, 2003
• Grant date: Aug 25, 2009
• Expiry date: Mar 20, 2024

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to epothilone analog represented by the formula Iwherein(i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.