Fluorine-containing 2-nitroimidazole derivatives and...

C - Chemistry – Metallurgy – 07 – D

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167/239, 260/305

C07D 233/91 (2006.01) A61K 31/415 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2005261

- 31 - ABSTRACT OF THE DISCLOSURE A 2-nitroimidazole derivative of the formula: Image (I) wherein Rf is a group of the following formula (II) or (III): -CH2CFXCH2OR1 (II) wherein X is a hydrogen atom or a halogen atom; R1 is a group of the formula: Image -CH(CH2OR2)2 -(CH2)?OR2 -(CH2)?COR2 or Image wherein R2 is a hydrogen atom, a hydroxyl group, a C1-C3 alkyl group, a C2-C4 acyl group, benzylidene or acetonide; R3 is a hydrogen atom or a C1-C3 alkyl group; Z is a hydrogen atom, COOY, COOR3, CONHOY, CONR4R5 (wherein R4 and R5 are hydroxyl group-containing C1-C3 alkyl groups or hydrogen atoms; Y is a hydrogen atom or a monovalent metal atom), an amino group, a hydroxyl group or OR3; ? is an integer of 1 to 3; o is an integer of 0 to 3; p is an -32- integer of 0 to 2; q is an integer of 0 to 3; m and n are integers of 0 to 4; and 1 ? m + n ? 4 or ¦ (III) Image wherein R3, X and p are the same as defined above; Z' is the same as Z or is OCOOCH3; r is an integer of 1 to 3; s is 0 or 1; t is an integer of 0 to 4 provided that when p = 0, s ? 0 and at least one X is a fluorine atom; and a radiosensitizer comprising said nitroimidaxole derivative.

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