New a-aryl-a-pyridylalkanoic acid derivatives of the formula:
wherein
R1 is cyano or carbamoyl,
R2 is hydrogen or halogen,
R3 is hydrogen or lower alkyl,
one of R4 and R5 is hydrogen and another is lower alkyl,
R6 is hydrogen or lower alkyl, and
R7 is lower alkyl, or
R6 and R7 are taken together to form an N-containing saturated heterocyclic group with the adjacent nitrogen atom, in which the heterocyclic group may be substituted with lower alkyl or optionally protected hydroxy(lower)alkyl, provided that R2 is halogen or R3 is lower alkyl, when R1 is cyano and R6 and R7 are each lower alkyl, and salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.
These derivatives and salts thereof are useful as antiulcer agents and spasmolytic agents.
式中的新 a-芳基-a-
吡啶基烷酸衍
生物:
式中
R1 是
氰基或
氨基甲酰基、
R2 是氢或卤素
R3 是氢或低级烷基
R4 和 R5 中的一个是氢,另一个是低级烷基、
R6 是氢或低级烷基,以及
R7 是低级烷基,或
当 R1 是
氰基,R6 和 R7 分别是低级烷基时,R6 和 R7 与相邻的氮原子一起形成含 N 的饱和杂环基团,其中杂环基团可被低级烷基或任选保护的羟基(低级)烷基取代,条件是 R2 是卤素或 R3 是低级烷基,以及它们的盐、它们的制备工艺和包含它们的药物组合物。
这些衍
生物及其盐可用作抗溃疡剂和解痉剂。