Benzoate 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 31/66 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01) C07F 9/547 (2006.01) C07F 9/655 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2095375

ABSTRACT This invention relates to a compound of formula I Image I or a pharmaceutically acceptable salt thereof, in which R2 is a radical of the formula Image or Image in which Ra and Rb are independently hydrogen or C1-6 alkyl, said C1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C1-6alkyl)amino; or NRaRb together represents a radical of the formula Image , Image , Image or Image in which y is one to three, and Ra is as defined above; Rp and Rr are independently same or different C1-6 alkyl; R1 is hydrogen or a radical Z of the formula Image or Image in which Q is -(CH2)f-, optionally substituted with one to six same or different C1-6 alkyl or C3-6 cycloalkyl, or a carbon atom of said -(CH2)f- radical may also be a part of C3-6 cycloalkylidene; R3 and R4 are independently hydrogen or C1-6 alkyl, or R3 and R4 taken together with the carbon atom to which they are attached form C3-6 cycloalkylidene; R5 is -OC(=O)R, -OP=O(OH)2 or -CH2OP=O(OH)2, in which R is C1-6 alkyl; R6, R7, R8 and R9 are independently halogen, C1-6 alkyl, C1-6 alkoxy or hydrogen, but when R5 is -OC(=O)R, one of R6, R7, R8 or R9 is -OP=O(OH)2; f is 2 to 6; n is O, and m is 1 or 0 when R5 is -CH2OP=O(OH)2; and n is 1 or O, and m is 1 when R5 is -OC(=O)R or -OP=O(OH)2. Also provided by this invention are pharmaceutical formulations and a method for treating mammalian tumors with a compound of formula I.

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