C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/207, 260/368
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
Deutsch Howard M.
Glinski Jan A.
Haugwitz Rudiger D.
Narayanan Venkatachala L.
Suffness Matthew
Borden Ladner Gervais Llp
U.s. Departm Ent Of Commerce The United States Of America Represented By The Secretary
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