Imidazolidinonyl aminopyrimidine compounds for the treatment...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 409/14 (2006.01) A61K 31/381 (2006.01) A61K 31/4178 (2006.01) A61K 31/4436 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/496 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2673564

The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N- ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3- trifluoropropylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2- cyanoethylaminomethyl, mopholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1- azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or a pharmaceutically acceptable salt thereof.

L'invention concerne de nouveaux composés imidazolidinonyl aminopyrimidine considérés comme ayant une utilisation clinique dans le traitement du cancer par inhibition de Plk1 représenté par la formule I dans laquelle : R1 est un groupe aminométhyle, (alkyl en C1 à C3)aminométhyle, di(alkyle en C1 à C2)aminométhyle, N-éthyl-N-méthyl-aminométhyle, 1-aminoéthyle, 1-((alkyl en C1 à C2)amino)-éthyle, 3,3,3-trifluoropropylaminométhyle, éthynyle, 2-hydroxy-éthoxy, 2-hydroxyéthylaminométhyle, 2-cyanoéthylaminométhyle, mopholin-4-ylméthyle, méthoxyméthoxyméthyle, cyclopropyle, 1-azétidinylméthyle, 1-pyrrolidinylméthyle, ou 1,3-dioxolan-2-yle ; R2 est un atome d'hydrogène ou un groupe halogéno ; R3 un atome d'hydrogène ou un groupe halogéno ; à condition qu'au moins l'un de R2 et de R3 soit un atome d'hydrogène ; R4 est un atome d'hydrogène, un groupe méthyle ou halogéno ; et est une simple liaison qui est soit présente soit absente, ou un sel pharmaceutiquement acceptable de ceux-ci.

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