申请人:Burroughs Wellcome Co.
公开号:US04690933A1
公开(公告)日:1987-09-01
The invention provides compounds of the formula (I) ##STR1## or salts, esters, or amides or other protected forms thereof; wherein R.sub.1 is a C.sub.1-7 bivalent aliphatic hydrocarbon group or a single bond; R.sub.2 and R.sub.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members; X is --N.dbd. or --CH.dbd.; A and B each represent hydrogen atoms or --CA--CB-- represents --C.dbd.C--; and D is an acidic group other than a carboxylic acid group. Also provided are pharmaceutical compositions of compounds of the formula (I), methods for the preparation of the compounds and intermediates in their preparation. The compounds of the formula (I) have antihistamic activity.
该发明提供了式(I)的化合物##STR1##或其盐、酯、酰胺或其他受保护形式;其中R.sub.1是C.sub.1-7双价脂肪烃基团或单键;R.sub.2和R.sub.3相同或不同,分别是氢、C.sub.1-4烷基或与氮一起构成含氮杂环环有四到六个环成员的杂环;X为--N.dbd.或--CH.dbd.;A和B各代表氢原子或--CA--CB--代表--C.dbd.C--;D是除羧酸基以外的酸性基团。还提供了式(I)化合物的药物组合物,以及制备该化合物和制备过程中的中间体的方法。式(I)的化合物具有抗组胺活性。