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Piperidino derivatives that stimulate growth hormone release.

机译:刺激生长激素释放的哌啶子基衍生物。

摘要

A pharmaceutically useful compound of formula (I) wherein R1 is hydrogen and X is a group of formula (II) in which R3 is esterified carboxy and R4 is ar(lower) alkyl; R3 is cyano and R4 is aryl; R3 is hydrogen and R4 is 2-oxo-1-benzimidazolinyl; or R3 and R4 are linked together to form formula (III) in which R5 is acyl, formula (a) is piperidino, and Y is lower alkanetriyl; or R1 is a group of formula (IV) in which R3, R4 and formula (a) are each as defined above and X is bond, R2 is 3-azetidinyl, 4-piperidyl or a group of the formula: -Z-NHR6 in which R6 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.
机译:式(I)的药学上有用的化合物,其中R 1是氢并且X是其中R 3是酯化的羧基并且R 4是芳(低级)烷基的式(II)的基团; R 3为氰基,R 4为芳基; R 3为氢,R 4为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为酰基,式(a)为哌啶子基,且Y为低级链烷三基;或R 1为式(IV)的基团,其中R 3,R 4和式(a)各自如上定义且X为键,R 2为3-氮杂环丁烷基,4-哌啶基或下式的基团:-Z-NHR 6,其中R 6为氢或氨基保护基,Z为低级亚烷基或环(低级)亚烷基,且A为-(CH 2)n-,其中n为3、4或5,或-CH = CH-(CH2)m-,其中m为1、2或3,及其盐。本发明的化合物或其盐对动物和人体具有优异的促进生长激素释放的促进活性。

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