Pyrimidine derivatives

Details Pyrimidine derivatives Pyrimidine derivatives

C - Chemistry, Metallurgy

07

D

C07D 239/48 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07D 239/52 (2006.01) C07D 401/12 (2006.01) C07D 403/00 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/00 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2230516

The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: Image [wherein R1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or -NR2R3; X represents an oxygen atom or N-R4; m is 2 or 3; and n is 1 or 2 (wherein each of R2 and R3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)], as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

L'invention porte sur des dérivés de la pyrimidine de formule générale (1) ou leurs sels, ou un médicament dont ils constituent le principe actif. Dans ladite formule: R<1> représente hydroxy, alcoxy inférieur, phényloxy, aralkyloxy ou -NR<2>R<3>, R<2> et R<3> représentant chacun hydrogène, hydroxy, alkyle inférieur, phényle, aralkyle, ou un groupe hétérocyclique; X représente oxygène ou N-R<4>, R<4> représentant alkyle inférieur, phényle, formyle ou alcoxycarbonyle inférieur; m vaut 2 ou 3; et n vaut 1 ou 2. Ces composés, qui présentent une action inhibitrice puissante sur les endothélines ayant une action vasoconstrictrice puissante, s'avèrent utiles dans le traitement des troubles circulatoires, etc.

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