申请人:KOWA CO. LTD.
公开号:EP0801062A1
公开(公告)日:1997-10-15
The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative:
[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.
本发明涉及下式(1)的嘧啶衍生物或该衍生物的盐:
[其中 R1 代表低级烷基;R2 和 R3 各代表 H、烷基或烷氧基;R4 和 R5 各代表 H 或烷基;R6 代表烷基、-OR7 或 -NR8R9;n 为 0 至 3 之间的数字(其中 R7、R8 和 R9 各代表 H、烷基、芳基、芳烷基、氨基、杂环等)],以及含有该衍生物或盐作为活性成分的药物。本化合物对内皮素具有很强的结合抑制活性,具有很强的血管收缩效应和细胞增殖效应。因此,这些化合物可有效治疗包括循环系统疾病在内的各种疾病。