申请人:A. H. Robins Company, Inc.
公开号:US04440785A1
公开(公告)日:1984-04-03
Novel 2-aminobiphenylacetic acids, esters and metal salts of the formula are disclosed: ##STR1## wherein R represents hydrogen, lower alkyl, sodium or potassium; R.sup.1 represents fluoro, chloro, bromo, lower-alkyl or amino; R.sup.2 represents lower-alkyl, lower-alkoxy, fluoro, chloro, bromo, amino or trifluoromethyl; and m and n are 0-2 with the proviso that when R.sup.1 or R.sup.2 are tertiary butyl or a sterically hindering lower alkyl radical, m and/or n are 1. The compounds are prepared by hydrolysis of 4-(5-, 6- and 7-)phenylindolin-2-ones to give the 2-amino-3-(4-, 5- and 6-)biphenylacetic acids. The free acids are converted to the esters and metal salts. The compounds have anti-inflammatory activity and inhibit blood platelet aggregation.
本发明揭示了式的新型2-氨基联苯乙酸、酯和金属盐:##STR1## 其中R代表氢、低碳基、钠或钾;R.sup.1代表氟、氯、溴、低碳基或氨基;R.sup.2代表低碳基、低碳氧基、氟、氯、溴、氨基或三氟甲基;m和n为0-2,但当R.sup.1或R.sup.2为叔丁基或立体阻碍的低碳基基团时,m和/或n为1。该化合物通过将4-(5-、6-和7-)苯基吲哚啉-2-酮水解制备而成,从而得到2-氨基-3-(4-、5-和6-)联苯乙酸。游离酸转化为酯和金属盐。该化合物具有抗炎活性和抑制血小板聚集作用。