申请人:The Purdue Frederick Company
公开号:US04476311A1
公开(公告)日:1984-10-09
Analgesic and anti-inflammatory compounds are provided. These compounds possess the following general formula: ##STR1## wherein R=--COOR.sub.5, --CH.sub.2 CO.sub.2 H, ##STR2## wherein A and B=hydrogen, lower alkyl, hydroxy alkyl, lower alkyl amine, substituted lower alkyl amine, aminoalkyl, substituted aminoalkyl; R.sub.5 =lower alkyl; R.sub.1 =aryl, substituted aryl, aralkyl, alkyl, hydrogen, substituted aralkyl and heterocycle; R.sub.2 =aryl, substituted aryl, aralkyl, alkyl, substituted aralkyl, heterocycle, substituted heterocycle, biphenyl, substituted biphenyl, naphthyl, and substituted naphthyl; R.sub.3 =aryl, substituted aryl, hydrogen, aralkyl, substituted aralkyl, alkyl, heterocycle and substituted heterocycle; R.sub.2 and R.sub.3 together form a ring; R.sub.4 =hydrogen, phenyl, substituted phenyl, heterocycle; alkyl, substituted alkyl; or, R.sub.1 and R.sub.4 may form a ring; X=>C.dbd.O, --CH.sub.2 --; Y=--S--CHR.sub.4 --, --O--OHR.sub.4 --, --CHR.sub.4 --, --CR.sub.6 R.sub.7 --CHR.sub.4 --, ##STR3## wherein R.sub.6 =same as R.sub.4 ; R.sub.7 =same as R.sub.4 ; R.sub.6 and R.sub.7 may form a ring; and Z=hydrogen, halogen, alkyl, substituted alkyl, hydroxy, alkyloxy, amino, substituted amino, nitro, aryl, substituted aryl, aryloxy.
提供镇痛和抗炎化合物。这些化合物具有以下一般公式:##
STR1## 其中R=--COOR.sub.5,--CH.sub.2 CO.sub.2 H,##
STR2## 其中A和B=
氢,低级烷基,羟基烷基,低级烷基胺,取代的低级烷基胺,
氨基烷基,取代的
氨基烷基;R.sub.5=低级烷基;R.sub.1=芳基,取代芳基,芳基烷基,烷基,
氢,取代芳基烷基和杂环;R.sub.2=芳基,取代芳基,芳基烷基,烷基,取代芳基烷基,杂环,取代杂环,
联苯,取代
联苯,
萘基和取代
萘基;R.sub.3=芳基,取代芳基,
氢,芳基烷基,取代芳基烷基,烷基,杂环和取代杂环;R.sub.2和R.sub.3一起形成环;R.sub.4=
氢,
苯基,取代
苯基,杂环;烷基,取代烷基;或者,R.sub.1和R.sub.4可以形成环;X=>C.dbd.O,--CH.sub.2 --;Y=--S--CHR.sub.4 --,--O--OHR.sub.4 --,--CHR.sub.4 --,--CR.sub.6 R.sub.7 --CHR.sub.4 --,##
STR3## 其中R.sub.6=与R.sub.4相同;R.sub.7=与R.sub.4相同;R.sub.6和R.sub.7可以形成环;Z=
氢,卤素,烷基,取代烷基,羟基,烷
氧基,
氨基,取代
氨基,硝基,芳基,取代芳基,芳
氧基。