2,4-diaminopyrimidine compounds as anti-cancer agents

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 239/48 (2006.01) A61K 31/505 (2006.01) A61K 31/506 (2006.01) A61K 31/655 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2275566

Use of a compound of general formula (I) wherein R1 and R2 are independently selected amino groups; R3 is C1-6 alkyl or haloalkyl; R4 is selected from alkoxy, aralkoxy, haloalkyl, halogen and amino; and R5 is selected from nitro, amino, azido or a group -N=X-NR6R7 where R6 and R7 are independently C1-6 alkyl or are aralkyl or together with the nitrogen to which they are attached form a heterocyclic ring with the proviso that one or both R6 and R7 or the heterocyclic ring carries or includes or carries and includes at least one oxygen or sulphur atom, and X is N or CH or CR9; or R4 and R5 together with the benzene ring to which they are attached form a group of formula (II), wherein X is N, CH or CR9, and R8 is C1-6 alkyl or is aralkyl; or R4 and R5 together with the benzene ring to which they are attached form a group of formula (III) wherein R9 is aryl or aralkyl; or a salt or N-oxide of any such compound, for the manufacture of a medicament for the treatment of mutant-ras gene associated cancer.

L'invention concerne l'utilisation d'un composé de formule générale (I), dans laquelle R?1¿ et R?2¿ sont des groupes amines indépendamment sélectionnés, R?3¿ représente haloalkyle ou alkyle C¿1-6?, R?4¿ est choisi parmi alcoxy, aralcoxy, haloalkyle, halogène et amino, et R?5¿ est choisi parmi nitro, amino, azido ou un groupe -N=X-NR?6¿R?7¿, où R?6¿ et R?7¿ représentent, indépendamment, alkyle C¿1-6? ou représentent aralkyle, ou forment un noyau hétérocyclique avec l'azote auquel ils sont liés, à condition que R?6¿ et/ou R?7¿ ou le noyau hétérocyclique porte et/ou comprenne au moins un atome d'oxygène ou de soufre, X représentant N ou CH ou CR?9¿; ou dans laquelle R?4¿, R?5¿ et le noyau benzénique auquel ils sont liés forment, ensemble, un groupe de formule (II), où X représente N, CH ou CR?9¿ et où R?8¿ représente alkyle C¿1-6? ou aralkyle; ou dans laquelle R?4¿, R?5¿ et le noyau benzénique auquel ils sont liés forment, ensemble, un groupe de formule (III), où R?9¿ représente aryle ou aralkyle. L'invention concerne également un sel ou un N-oxyde de l'un quelconque de ces composés. L'invention est destinée à la fabrication d'un médicament permettant de traiter un cancer lié au gène mutant ras.

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