申请人:USV Pharmaceutical Corp.
公开号:US04625034A1
公开(公告)日:1986-11-25
This invention relates to novel lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic activities. The present new compounds are di- and tetra-hydroquinoline or di- and tetra-hydronapthalene derivatives, more particularly, 1,2-, 1,4-, 5,6-, or 7,8-dihydro; 1,2,3,4-tetrahydro-; 5,8-dihydro-; or 5,6,7,8-tetrahydroquinoline or napthalene derivatives of a compound of the formula: ##STR1## and oxides, quaternary ammonium salts and acid salts thereof; wherein A is CH or N; Z is an alkylene chain containing up to 10 carbon atoms in the principal chain and a total of up to 12 carbon atoms and the said alkylene chain may be attached to the phenyl group through an oxygen atom; R is the substituent OR.sub.6 attached to one of the carbon atoms of Z in which R.sub.6 is H, lower alkyl or phenyl; X is --O(CHR.sub.5).sub.m --, alkylene of up to 2 carbon atoms in the principal chain and up to a total of 4 carbon atoms or ##STR2## wherein R.sub.5 is H or CH.sub.3 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each H or OH; n'=1 or 2; and m=1 or 2.
这项发明涉及具有抗炎和抗过敏活性的新型脂氧合酶抑制剂。这些新化合物是二氢和四氢喹啉或二氢和四氢萘衍生物,更具体地说,是化合物的1,2-、1,4-、5,6-或7,8-二氢;1,2,3,4-四氢-;5,8-二氢-;或5,6,7,8-四氢喹啉或萘衍生物,其化合物的结构式如下:##STR1##和其氧化物、季铵盐和酸盐;其中A为CH或N;Z为主链中含有最多10个碳原子和总共最多12个碳原子的烷基链,该烷基链可以通过一个氧原子连接到苯基;R是连接到Z的一个碳原子上的取代基OR.sub.6,其中R.sub.6为H、低烷基或苯基;X为--O(CHR.sub.5).sub.m --、主链中最多含有2个碳原子和总共最多4个碳原子的烷基或##STR2##其中R.sub.5为H或CH.sub.3;R.sub.1、R.sub.2、R.sub.3和R.sub.4分别为H或OH;n'=1或2;m=1或2。