5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin and its preparation and use for the treatment of cancer

US8080559B2 · kind B2 · utility

Assignee

• DR. REDDY'S LABORATORIES LIMITED · IN

Inventors

• Venkateswarlu Akella · Darsi, IN
• Shanavas Alikunju · Darsi, IN
• Ajaya Kumar Reka · Hyderabad, IN
• Ramesh Mullangi · Bengaluru, IN
• Raju Sirisilla · Hyderabad, IN
• Subrahmanyam Duvvuri · Hyderabad, IN
• Sriram Rajagopal · Darsi, IN

Key dates

• Filing date: Oct 12, 2009
• Grant date: Dec 20, 2011
• Expiry date: Oct 12, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D519/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.