13-alkyl epothilone derivatives

Details 13-alkyl epothilone derivatives 13-alkyl epothilone derivatives

C - Chemistry, Metallurgy

12

P

C12P 17/16 (2006.01) A61K 31/427 (2006.01) A61P 35/00 (2006.01) C07D 277/00 (2006.01) C07D 277/24 (2006.01) C07D 277/34 (2006.01) C07D 277/36 (2006.01) C07D 313/00 (2006.01) C07D 417/06 (2006.01) C07D 493/04 (2006.01) C07K 16/44 (2006.01) C12N 9/00 (2006.01) C12P 17/18 (2006.01) C12P 41/00 (2006.01)

Patent

CA 2425620

The invention relates to novel 13-lower alkyl epothilones of formula (IA); wherein R1 is methyl, hydroxymethyl, halomethyl, methylthio or methoxy; R2 is hydrogen or methyl, R3 is lower alkyl, and Z is O or a bond; intermediates and a process for the preparation of such 13-lower alkyl epothilones and epothilones in general; a pharmaceutical composition comprising such 13-lower alkyl epothilones and the use of such compounds for the treatment of tumor diseases; a method of treatment of warm-blooded animals; catalytic antibodies having aldolase activity and a process for enantioselectively resolving a racemic mixture of aldol synthons by means of antibody catalyzed retro-aldol reaction.

Cette invention a trait à de nouvelles épothilones d'alkyle - 13 inférieur correspondant à la formule (IA). Dans cette formule, R¿1? représente un méthyle, un hydroxyméthyle, un halométhyle, un méthylthio ou un méthoxy, R¿2? représente un hydrogène ou un méthyle, R¿3? représente un alkyle inférieur et Z représente un oxygène ou une liaison. L'invention concerne également des intermédiaires et un procédé de préparation de ces épothilones d'alkyle - 13 inférieur ainsi que de préparation d'épothilones en général. Elle porte, de surcroît, sur une composition pharmaceutique renfermant ces épothilones d'alkyle - 13 inférieur ainsi que sur l'utilisatio

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