Epothilone analogs

US6441186B1 · kind B1 · utility

Assignee

• THE SCRIPPS RESEARCH INSTITUTE · US

Inventors

• Kyriacos C. Nicolaou · Philadelphia, US
• Yun He · San Diego, US
• Sacha Ninkovic · Village of La Jolla, US
• Joaquin Pastor · San Diego, US
• Frank Roschangar · Glen Allen, US
• Francisco Sarabia · Rincón de la Victoria, ES
• Hans Vallberg · Huddinge, SE
• Dionisios Vourloumis · San Diego, US
• Nicolas Winssinger · Village of La Jolla, US
• Zhen Yang · Lo Wu, CN
• N. Paul King · San Diego, US
• M. Ray Finlay · Killinchy, GB

Key dates

• Filing date: Sep 4, 1997
• Grant date: Aug 27, 2002
• Expiry date: Sep 4, 2017

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D493/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancer agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the anlogs are demonstrated to have a superior cytotoxic activities as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.