Pyrimidine derivatives and pharmaceutical composition

Details Pyrimidine derivatives and pharmaceutical composition Pyrimidine derivatives and pharmaceutical composition

C - Chemistry, Metallurgy

07

D

C07D 239/46 (2006.01) A61K 31/505 (2006.01) C07D 239/48 (2006.01) C07D 239/50 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2150609

A pyrimidine derivative of the formula (I): Image wherein R1 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, or -NHR11 group; R2 is a hydrogen or halogen atom, alkyl of 1 to 6 carbon atoms, haloalkyl of 1 to 6 carbon atoms, -(CH2)mC6H5, -NH2, -NHR12, -NH (CH2) nC6H5, -NH (CH2 ) pC6H4-OR13, -N(R14)(CH2)qC6H5, -NHC(=O)R15, -NHC(=O)(CH2)rC6H5, -NHC(=O)CH(C6H5)2, -OR16, or -O(CH2)sC6H5 group; R3 is -COOH, -COOR17, hydroxyl, -OR18, -NH2, -N(R19)2, -NHR20, azole, or sulfonic acid group; R11 is alkyl of 1 to 6 carbon atoms or haloalkyl of 1 to 6 carbon atoms; R12, R13, R14, R15, R16, R17, R18, R19, and R20 are independently alkyl of 1 to 6 carbon atoms; m is 0 or an integer of 1 to 6; n is 0 or an integer of 1 to 6; p is 0 or an integer of 1 to 6; q is 0 or an integer of 1 to 6; r is 0 or an integer of 1 to 6; and s is 0 or an integer of 1 to 6, or a salt thereof, and a pharmaceutical composition comprising said pyrimidine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier are disclosed. The compound of the formula (I) or the salt thereof according to the present invention is sufficiently effective to renal dysfunction without affecting blood pressure.

Dérivé de la pyrimidine de formule (I) Image , où R1 est un atome d'hydrogène, un alkyle de 1 à 6 atomes de carbone, un haloalkyle de 1 à 6 atomes de carbone, ou un groupe -NHR11; R2 est un atome d'hydrogène ou d'halogène, un alkyle de 1 à 6 atomes de carbone, un haloalkyle de 1 à 6 atomes de carbone, ou encore un groupe -(CH2)mC6H5, -NH2, -NHR12, -NH (CH2) nC6H5, -NH (CH2 ) pC6H4-OR13, -N(R14)(CH2)qC6H5, -NHC(=O)R15, -NHC(=O)(CH2)rC6H5, -NHC(=O)CH(C6H5)2, -OR16 ou -O(CH2)sC6H5; R3 est un groupe -COOH, -COOR17, hydroxyle, -OR18, -NH2, -N(R19)2, -NHR20, azole ou acide sulfonique; R11 est un alkyle de 1 à 6 atomes de carbone ou un haloalkyle de 1 à 6 atomes de carbone; R12, R13, R14, R15, R16, R17, R18, R19 et R20 sont indépendamment un alkyle de 1 à 6 atomes de carbone; m est 0 ou un entier de1 à 6; n est 0 ou un entier de 1 à 6; p est 0 ou un entier de 1 à 6; q est 0 ou un entier de 1 à 6; r est 0 ou un entier de 1 à 6; enfin, s est 0 ou un entier de 1 à 6. L'invention porte également sur un sel de ce dérivé et sur une composition pharmaceutique renfermant ledit dérivé de la pyrimidine ou un sel pharmacocompatible de ce dérivé, ainsi que sur un véhicule pharmacocompatible. Le composé de formule (I) de la présente invention ou le sel de ce composé permettent de soulager efficacement le dysfonctionnement rénal sans altérer la pression artérielle.

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