Water soluble, antineoplastic derivatives of taxol

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 1330436

ABSTRACT OF THE DISCLOSURE Antineoplastic water soluble derivatives of taxol having the following formula: Image wherein: Z = ethylene, propylene, CHCH, 1,2-cyclohexane, 1,2-phenylene R1= OK x base, NR2R3, OR3, SR3, OCH2CONR4R5, OH R2= hydrogen, methyl R3= (CH2)nNR6R7; (CH2)nN+R6R7R8X n = 1 to 3 R4= hydrogen, lower alkyl containing 1 to 4 carbons R5= hydrogen, lower alkyl containing 1 to 4 carbons, benzyl, hydroxyethyl, CH2CO2H, dimethylaminoethyl R6R7= lower alkyl containing 1 or 2 carbons, benzyl or R6 and R7 together with the nitrogen atom of NR6R7 form the following rings Image R8= lower alkyl containing 1 or 2 carbons, benzyl X = halide base= NH3, (HOC2H4)3N, N(CH3)3, CH3N(C2H4OH)2, NH2(CH2)6NH2, N-methylglucamine, NaOH, KOH. These derivatives have utility in the treatment of cancer.

592894

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