申请人:Syntex (U.S.A.), Inc.
公开号:US04512990A1
公开(公告)日:1985-04-23
Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S; Y is halo, alkoxy, alkyl, or dialkylamino; a is 0, 1 or 2; b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is --NH.sub.2, b cannot be 2-5; and X is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR1/2, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or, in --NR1/2, both R.sup.1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; and R.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl; have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.
式为##STR1##及其药学上可接受的酸盐化合物,其中:Z为S;Y为卤素、烷氧基、烷基或二烷基氨基;a为0、1或2;b为2-12的整数,但若b为2或3,则a不能为0,并且进一步规定,若X为OH,则b不能为2-5,若X为--NH.sub.2,则b不能为2-5;而X从下列群组中选择:--OH、OR.sup.1、--NH.sub.2、--NHR.sup.1、NR1/2、##STR2##和--NHCONHR.sup.2,在其中每个R.sup.1分别独立为烷基或环烷基,或在--NR1/2中,两个R.sup.1共同为亚烷基或形成可选地在环N处被烷基或--CH.sub.2 CH.sub.2 OH取代的哌嗪环;而R.sup.2是烷基、环烷基或可选地取代的苯基;具有抗炎性能,并且可用于治疗由炎症和肿胀所特征的疾病。