Soft tertiary amine esters of bio-affecting carboxylic acids, processes for preparing and a pharmaceutical composition containing the same
申请人:Merck & Co., Inc.
公开号:EP0051278A1
公开(公告)日:1982-05-12
Derivatives of known bio-affecting carboxylic acids, their non-toxic pharmaceutically acceptable acid addition salts and N-oxides as well as processes for preparing those novel derivatives are disclosed. Those derivatives having the
wherein R-COO- is the acyloxy residue of a bio-affecting monocarboxylic acid; Y and Y' are each hydrogen or alkyl; n is zero or one; R1 and R2 are each inter alia alkyl, alkenyl, aryl, cycloalkyl, cycloalkenyl, aralkyl or alkaryl; and R3 is inter alia hydrogen; orthe structural formula
wherein -OOC-R'-COO- is the di(acyloxy) residue of a bio-affecting dicarboxylic acid.
本研究公开了已知具有生物效应的羧酸的衍生物、它们的无毒药学上可接受的酸加成盐和 N-氧化物,以及制备这些新型衍生物的工艺。这些衍生物具有
其中 R-COO- 是生物效应单羧酸的酰氧基残基;Y 和 Y'各自是氢或烷基;n 是零或一;R1 和 R2 除其他外各自是烷基、烯基、芳基、环烷基、环烯基、芳烷基或烷芳基;以及 R3 除其他外是氢;或结构式为
其中-OOC-R'-COO-是具有生物效应的二羧酸的二(酰氧基)残基。