6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations

US7125893B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Ulrich Klar · Berlin, DE
• Wolfgang Schwede · Berlin, DE
• Werner Skuballa · Berlin, DE
• Bernd Buchmann · Hohen Neuendorf, DE
• Jens Hoffmann · Mühlenbeck, DE
• Rosemarie Lichtner · Berlin, DE

Key dates

• Filing date: May 1, 2000
• Grant date: Oct 24, 2006
• Expiry date: May 1, 2020

Classification

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

Abstract

This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula Iin which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.