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    • 8. 发明授权
    • 피리미딘유도체
    • KR100453097B1
    • 2004-12-31
    • KR1019980701163
    • 1996-09-04
    • 코와 가부시키가이샤
    • 히라타미츠테루데우시타케오타카하시요시오타무라마사히로오시마다케시오다토시아키이시가와테츠야소노키히로유키시라츠치마사미
    • C07D239/48A61K31/505
    • C07D239/52
    • The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: Äwherein R 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 -NR R ; X represents an oxygen atom or N-R ; m is 2 or 3; and n is 1 or 2 (wherein each of R and R , 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; R represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)Ü, 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.
    • 本发明涉及下式(1)的嘧啶衍生物或其衍生物的盐:< CHEM> &Aum1;其中R 1是 表示羟基,低级烷氧基,可以具有取代基的苯氧基,可以具有取代基的芳烷氧基或-NR 2 R 3。 X代表氧原子或N-R 4; m是2或3; 并且n是1或2(其中R 2和R 3中的每一个彼此相同或不同,表示氢原子,羟基,可以具有取代基的低级烷基, 可具有取代基的苯基,可具有取代基的芳烷基或可具有取代基的杂环基; R 4表示低级烷基,苯基,甲酰基或低级烷氧基羰基 )Ü以及含有该衍生物或盐作为活性成分的药物。 该化合物对具有强效血管收缩作用的内皮素具有强结合抑制活性。 因此,这些化合物作为包括循环系统疾病在内的各种疾病的治疗剂是有效的。