Camptothecin analogues, preparation methods therefor, use thereof as drugs, and pharmaceutical compositions containing said analogues

US5981542A · kind A · utility

Assignee

• Société de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S) SAS · FR

Inventors

• Dennis Bigg · Gif-sur-Yvette, FR
• Olivier Lavergne · Palaiseau, FR
• Francesc Pla Rodas · Santa Coloma de Farners, ES
• Jacques Pommier · Paris, FR
• Gerard Ulibarri · Les Ulis, FR

Key dates

• Filing date: Dec 2, 1997
• Grant date: Nov 9, 1999
• Expiry date: Dec 2, 2017

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A camptothecin analog characterized in that the hydroxy lactone of the camptothecin is a .beta.-hydroxy lactone or the corresponding .beta.-hydroxyacid, resulting from the opening of said lactone, or a derivative of said .beta.-hydroxyacid, or a Pharmaceutically acceptable salt thereof, is disclosed. In particular, compounds of formulae (I) and (II) are disclosed. Methods for preparing the compounds of formulae (I) and (II), pharmaceutical compositions containing said containing said compounds, and their use, particularly as topoisomerase inhibitors and antitumoral drugs, are also disclosed.