Pharmaceutical compositions containing benzoylurea compounds

A - Human Necessities – 61 – K

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A61K 31/17 (2006.01)

Patent

CA 1208561

ABSTRACT OF THE DISCLOSURE Pharmaceutical compositions including as an active ingredient a benzoylurea of formula (I): Image I R11 represents hydrogen, or 1 or 2 substituents chosen from halogen, and alkyl and haloalkyl having 1-4 carbon atoms; R12 represents hydrogen or halogen; R13 represents hydrogen or 1 or 2 substituents which are selected from the group consisting of chlorine, methyl, and tri- fluoromethyl; R14 is a hydrogen atom, an alkyl group having 1-6 carbon atoms, an alkenyl group having 2-6 carbon atoms; a cycloalkyl group having 3-6 carbon atoms provided that (i) when X is O, R14 is absent; and (ii) when n is zero and R14 is hydrogen, R13 is also hydrogen; R15 represents either a phenyl group, a substituted phenyl group having 1-3 substituents selected from halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy having 1-4 carbon atoms, or R15 represents a bi-or polycyclic hydrocarbyl group having 8-14 carbon atoms, a cyclohexyl group, or a cyclohexyl group sub- stituted with 1-3 alkyl or alkenyl groups each having 1-6 carbon atoms; X represents N, CH, or O and n represents O or 1, provided that (a) when X is N or CH, R11 is halogen in the 2-position, R12 represents hydrogen or halogen in the 6-position R15 represents a phenyl group, or a substituted phenyl group having 1-3 substituents chosen from halogen and alkyl, alkoxy, haloalkyl, or haloalkoxy having 1-4 carbon atoms. (b) when X is 0, then n is zero, R12 is hydrogen, and R15 represents a bi- or polycyclic hydrocarbyl group having 8-14 carbon atoms, a cyclohexyl group, or a cyclohexyl group substituted with 1-3 alkyl or alkenyl groups each having 1-6 carbon atoms. These compositions find use in the treatment of cancer.

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