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    • 7. 发明申请
    • PIPERIDINO DERIVATIVES WHICH PROMOTE GROWTH HORMONE RELEASE
    • 促进生长激素释放的哌啶衍生物
    • WO98051687A1
    • 1998-11-19
    • PCT/JP1998/001695
    • 1998-04-14
    • C07D211/60A61K31/438A61K31/4439A61K31/445A61P5/06C07D401/04C07D471/10C07K5/06
    • C07K5/06017Y02P20/55
    • A pharmaceutically useful compound of formula (I) wherein R is hydrogen and X is a group of formula (II) in which R is esterified carboxy and R is ar(lower) alkyl; R is cyano and R is aryl; R is hydrogen and R is 2-oxo-1-benzimidazolinyl; or R and R are linked together to form formula (III) in which R is acyl, formula (a) is piperidino, and Y is lower alkanetriyl; or R is a group of formula (IV) in which R , R and formula (a) are each as defined above and X is bond, R is 3-azetidinyl, 4-piperidyl or a group of the formula: -Z-NHR in which R is hydrogen or amino protective group, and Z is lower alkylene or cyclo (lower) alkylene, and A is -(CH2)n-, in which n is 3, 4 or 5, or -CH=CH-(CH2)m-, in which m is 1, 2 or 3, and salts thereof. The compound or a salt thereof of the present invention has excellent promotion activity of growth hormone release for animals and human bodies.
    • 式(I)的药用有用化合物,其中R 1是氢,X是式(II)的基团,其中R 3是酯化的羧基,R 4是芳(低级)烷基; R 3是氰基,R 4是芳基; R 3是氢,R 4是2-氧代-1-苯并咪唑啉基; 或R 3和R 4连接在一起形成式(III),其中R 5是酰基,式(a)是哌啶子基,Y是低级烷酰基三烷基; 或R 1是式(Ⅳ)的基团,其中R 3,R 4和式(a)各自如上所定义,X是键,R 2是3-氮杂环丁烷基,4- 哌啶基或式-Z-NHR 6的基团,其中R 6是氢或氨基保护基,Z是低级亚烷基或环(低级)亚烷基,A是 - (CH 2)n - 其中n为3,4或5,或-CH = CH-(CH 2)m - ,其中m为1,2或3,及其盐。 本发明的化合物或其盐对于动物和人体具有优异的生长激素释放的促进活性。