申请人:Roussel-UCLAF
公开号:US03931302A1
公开(公告)日:1976-01-06
Novel butyric acid derivatives of the formula ##SPC1## Wherein X, X.sub.1, X.sub.2 and X.sub.3 are individually selected from the group consisting of hydrogen, halogen, lower alkyl of 1 to 5 carbon atoms, lower alkoxy of 1 to 5 carbon atoms, lower alkylthio of 1 to 5 carbon atoms, trifluoromethoxy, trifluoromethylthio, trifluoromethyl, OH and dilower alkylamino of 1 to 5 carbon atoms for each alkyl, R is selected from the group consisting of hydrogen, lower alkyl of 1 to 5 carbon atoms, o-carboxyphenyl, 2,3-dihydroxypropyl and -CH.sub.2 -CH - CH.sub.2 ##EQU1## wherein P and Q are individually lower alkyl of 1 to 5 carbon atoms, Z and X.sub.4 are individually selected from the group consisting of hydrogen and lower alkyl of 1 to 5 carbon atoms and Y is selected from the group consisting of hydrogen and --OH and the dotted line indicates the optional presence of a double bond when Y is hydrogen and when R is hydrogen or o-carboxyphenyl, the salts thereof with a non-toxic pharmaceutically acceptable mineral or organic base, which compounds have anti-inflammatory and analgesic activity and are substantially devoid of ulcerigenic activity and their preparation and novel intermediates formed therein.
化合物的式子为##SPC1##,其中X、X.sub.1、X.sub.2和X.sub.3分别选自氢、卤素、1-5个碳原子的低级烷基、1-5个碳原子的低级烷氧基、1-5个碳原子的低级烷基硫基、三氟甲氧基、三氟甲基硫基、三氟甲基、羟基和每个烷基的1-5个碳原子的双低级烷基氨基;R选自氢、1-5个碳原子的低级烷基、o-羧基苯基、2,3-二羟基丙基和-CH.sub.2-CH-CH.sub.2 ##EQU1##其中P和Q分别为1-5个碳原子的低级烷基,Z和X.sub.4分别选自氢和1-5个碳原子的低级烷基,Y选自氢和-OH,虚线表示当Y为氢时,R为氢或o-羧基苯基时,存在一个可选的双键。该化合物与非毒性药用可接受的矿物质或有机碱的盐具有抗炎和镇痛活性,并且基本上没有溃疡原性活性。该化合物的制备以及在其中形成的新中间体。