Substituted taxanes and pharmaceutical compositions...

Details Substituted taxanes and pharmaceutical compositions... Substituted taxanes and pharmaceutical compositions...

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/395 (2006.01) A61K 31/695 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07F 7/00 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2077394

A taxane derivative of the formula (see fig. I) wherein R1 and R3 are independently selected from the group comprising phenyl, naphthalene, C6H5CHCH-, (see fig. II) , (see fig. III) and (see fig. IV), provided, however, R1 and R3 are not both phenyl; Q is CH3-, (CH3)3C-, CH3O-, Cl, Br, F, or NO2; Z is -OT1; T1 is hydrogen, hydroxyl protecting group, or -COT2; T2 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or monocylic aryl; A c is acetyl; and E1 and E2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.

Dérivé de taxane, de formule (voir fig. I), où R1 et R3 sont choisis indépendamment parmi un phényle, un naphtalène, C6H5CHCH- (voir fig. II), (voir fig.III) et (voir fig. IV), à la condition, cependant, que R1 et R3 ne soient pas tous deux un phényle; Q est CH3-, (CH3)3C-, CH3O-, Cl, Br, F ou NO2; Z est -OT1; T1 est de l'hydrogène, un groupe protecteur hydroxyle, ou -COT2; T2 est H, un alkyle C1-C6, un alcényle C2-C6, un alcynyle C2-C6 ou un aryle monocylique; Ac est un acétyle; enfin, E1 et E2 sont choisis indépendamment parmi de l'hydrogène et des groupes fonctionnels qui augmentent l'hydrosolubilité du dérivé de taxane. Ce type de dérivé est utile comme agent antitumoral.

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