C - Chemistry – Metallurgy – 07 – D
Patent
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) C07F 7/18 (2006.01)
Patent
CA 2077598
A taxane derivative of the formula (see fig. 3) wherein R1 is phenyl or substituted phenyl, R3 is CH3O-, or CH3CH2O-, Z is -OCOT2, T2 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or monocycllc aryl, Ac is acetyl, and E1 and E2 are independently selected from hydrogen, and functional groups which increase the water solubility of the taxane derivative, the functional groups having the formula -COGCOR1 wherein: G is ethylene, propylene, CHCH, 1,2-cyclo-hexylene, or 1,2-phenylene; R1 = OH base, NR2R3, OR3, SR3, OCH2CONR4R5, or OH; R2 = hydrogen or methyl; R3 = (CH2)nNR6R7 or (CH2)nNR+6R7R8X-; n = 1 to 3 R6 and R7 = independently selected from lower alkyl containing 1 or 2 carbons, or benzyl, or R6 and R7 together with the nitrogen atom of NR6R7 forms one of the following rings (see fig. 4) or (see fig. 5); R8 = lower alkyl containing 1 or 2 carbons or benzyl; Xe = halide; and base = NH3, (HOC2H4)3N, N(CH3)3, CH3N(C2H4OH)2, NH2(CH2)6NH2, N-methylglucamine, NaOH, or KOH, are useful as antitumor agents.
Dérivé du taxane de formule (voir fig. 3), où R1 est un phényle avec ou sans substitution, R3 est CH3O- ou CH3CH2O-, Z est -OCOT2, T2 est H, un alkyle C1-C6, un alcényle C2-C6, un alcynyle C2-C6 ou un aryle monocyclique, Ac est un acétyle, E1 et E2 sont choisis indépendamment l'un de l'autre parmi l'hydrogène et des groupes fonctionnels qui augmentent l'hydrosolubilité de ce dérivé du taxane, les groupes ayant la formule -COGCOR1 où G est de l'éthylène, du propylène, CHCH, du 1,2-cyclohexylène ou du 1,2-phénylène; R1 = base OH, NR2R3, OR3, SR3, OCH2CONR4R5 ou OH; R2 = hydrogène ou méthyle; R3 = (CH2)nNR6R7 ou (CH2)nNR+6R7R8X-; n = entier de 1 à 3; R6 et R7 sont choisis indépendamment l'un de l'autre parmi un alkyle inférieur renfermant 1 ou 2 carbones ou un benzyle, ou R6 et R7 forment ensemble avec l'atome d'azote de NR6R7 l'un des cycles suivants (voir fig. 4) ou (voir fig. 5); R8 = alkyle inférieur renfermant 1 ou 2 carbones ou un benzyle; Xe = halogénure; base = NH3, (HOC2H4)3N, N(CH3)3, CH3N(C2H4OH)2, NH2(CH2)6NH2, N-méthylglucamine, NaOH, ou KOH; ce type de composé est utile comme agent antitumeur.
Biediger Ronald J.
Holton Robert A.
Florida State University
Smart & Biggar
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