Pyrimidine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 239/52 (2006.01) A61K 31/505 (2006.01) A61K 31/55 (2006.01) C07D 239/69 (2006.01) C07D 401/14 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2207100

The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: (see formula 1) [wherein R1 represents a lower alkyl group; each of R2 and R3 represents H, alkyl, or alkoxy; each of R4 and R5 represents H or alkyl; R6 represents alkyl, -OR7, or -NR8R9; and n is a number between 0 and 3 inclusive (wherein each of R7, R8, and R9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

L'invention concerne un dérivé pyrimidinique représenté par la formule générale (1) ou un sel de celui-ci et un médicament contenant celui-ci sous forme de principe actif. Dans cette formule (1), R<1> représente alkyle inférieur; R<2> et R<3> représentent chacun hydrogène, alkyle ou alcoxy; R<4> et R<5> représentent chacun hydrogène ou alkyle; R<6> représente alkyle, -OR<7> ou NR<8>N<9>; et n vaut un entier de 0 à 3 (R<7>, R<8> et R<9> représentant chacun hydrogène, alkyle, aryle, aralkyle, amino, un hétérocyle, etc.). Ce composé présente une puissante activité inhibitrice sur l'endothéline, un puissant vasoconstricteur et agent de prolifération cellulaire, et est utile dans le traitement, entre autres, de troubles circulatoires.

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