Azaindole and indolizine derivatives, processes for their production and their use as pharmaceuticals
申请人:SANDOZ AG
公开号:EP0265640A2
公开(公告)日:1988-05-04
Compounds of Formula I:
wherein:
either one Y is -N-and the remainder are -CH-X is
X1 is
with appropriate bond formation,
R, is a primary or secondary alkyl, free of asymmetric carbon atoms,
R2 is a substituted or unsubstituted phenyl, primary or secondary C1-6 alkyl, free of asymmetric carbon atoms, C3.6 cycloalkyl or phenylakyl as defined in the specification,
A is
or
b) -(CH2)n-
wherein n is 1,2 or 3 Z is
in which R8 is hydrogen, R9 or M wherein R9 is a physiologically acceptable and hydrolysable ester group, and M is a pharmaceutically acceptable cation; or: each Y is -CH-, X is -N-, X1 is
with appropriate bond formation,
R, and R2 are independently as defined under R2 above and R2 may additionally be hydrogen A and Z are as defined above
are obtained by multi-step processes and are useful as hypolipoproteinemic and anti-atherosclerotic agents.
式 I 的化合物:
其中
其中一个 Y 是-N,其余为-CH-X 是
X1 是
与适当的键形成、
R是伯或仲烷基,不含不对称碳原子、
R2 是取代或未取代的苯基、不含不对称碳原子的伯或仲 C1-6 烷基、C3.6 环烷基或说明书中定义的苯基、
A 是
或
b) -(CH2)n-
其中 n 为 1、2 或 3 Z 为
其中 R8 是氢、R9 或 M,其中 R9 是生理上可接受的可水解的酯基,而 M 是药学上可接受的阳离子;或:每个 Y 是-CH-,X 是-N-,X1 是-CH-,X2 是-CH2-,X3 是-CH2-,X4 是-CH2-,X5 是-CH2-。
与适当的键形成、
R 和 R2 独立地如上文 R2 中所定义,R2 还可以是氢 A 和 Z 如上所定义
通过多步工艺获得,可用作降脂蛋白血症和抗动脉粥样硬化药物。