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    • 7. 发明公开
    • 칼륨채널조절제로서의디페닐복소환식화합물
    • 二苯醚作为钾通道调节剂
    • KR1020000029735A
    • 2000-05-25
    • KR1019997000839
    • 1997-07-30
    • 브리스톨-마이어스스퀴브컴파니
    • 로미네,제프리,엘.마틴,스코트,더블유.휴어와샴,피야세나민웰,니콜라스,에이.그립코프,발렌틴,케이.스타렛,존,이.,쥬니어
    • C07D271/02
    • C07D263/58C07D233/64C07D233/70C07D233/76C07D235/12C07D249/12C07D249/14C07D271/113C07D413/10
    • PURPOSE: Provided is directed to novel diphenyl heterocyclic derivatives which are modulators of the large-conductance calcium activated potassium (BK) channels and, therefore, useful in the protection of neuronal cells, especially in the treatment or prevention of ischemic stroke. The present invention is also directed to a method of treatment with the novel compounds and to pharmaceutical compositions containing them. CONSTITUTION: Novel compounds of formula (1) are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels, wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R, R and R each are independently selected from hydrogen, halogen, OH, CF3, NO2, or (a); provided R is not hydrogen; and when R and R are hydrogen, R may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; R and R each are independently selected form hydrogen, halogen, CF3, NO2 or imidazol-1-yl; m, n and p each are independently selected from an integer of 0 or 1; and R and R each are independently hydrogen; C1-4 alkyl; or R and R, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone
    • 目的:提供新型二苯基杂环衍生物,其是大电导钙活化钾(BK)通道的调节剂,因此可用于保护神经元细胞,特别是用于治疗或预防缺血性中风。 本发明还涉及用新化合物和含有它们的药物组合物进行治疗的方法。 组成:新型式(1)化合物可用于治疗对大电导钙激活钾通道开放反应的病症,其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; R,R和R各自独立地选自氢,卤素,OH,CF 3,NO 2或(a); 条件是R不是氢; 当R和R为氢时,R可以是选自咪唑-1-基,吗啉代甲基,N-甲基咪唑-2-基和吡啶-2-基的杂环部分; R和R各自独立地选自氢,卤素,CF 3,NO 2或咪唑-1-基; m,n和p各自独立地选自0或1的整数; R和R各自独立地为氢; C 1-4烷基; 或R和R与它们所连接的氮原子一起是选自N-甲基哌嗪,吗啉,硫代吗啉,N-苄基哌嗪和咪唑啉酮的杂环部分