申请人:Pennwalt Corporation
公开号:US04665181A1
公开(公告)日:1987-05-12
A compound useful as anti-inflammatory agents in warm-blooded animals of the formula ##STR1## wherein X is a member of the class of ethylene and ethenyl and is substituted for hydrogen in the sixth or seventh position of the 1(2H)-phthalazinone ring Y is a member of the class of hydrogen and hydroxyl R.sub.1 is a member of the class of hydrogen, alkyl, alkoxy, hydroxyl, halogen, nitro, --NR.sub.3 R.sub.4, --COR.sub.5 and --O--A wherein A is a mineral acid residue which with --O-- forms an ester or the alkali metal salt of said ester, R.sub.2 is a member of the class of hydrogen, alkyl, phenyl, substituted phenyl, heteroaryl, hydroxyalkylene, polyhydroxyalkylene, aminoalkylene, alkylaminoalkylene, and carboxyalkylene, R.sub.3, R.sub.4 are independently from the class of hydrogen, alkyl, aminoalkylene or alkylaminoalkylene, R.sub.5 is a member of the class of OR.sub.3 and ##STR2## for example hydroxyl, methoxyl, 2-dimethylaminoethoxyl or 2-dimethylaminoethylamino, and wherein by alkyl and alkylene is meant respectively a mono- or divalent saturated aliphatic radical containing up to about eight carbon atoms, wherein the nitrogen of the alkylamino or alkylaminoalkylene may form a heterocycle with the alkyl or alkylene groups, wherein substituted phenyl may be substituted by, for example, alkyl, hydroxyl, alkoxy, halogen, nitro or amino, wherein heteroaryl may be, for example, 2-pyridyl.
一种化合物可用作温血动物的抗炎剂,其化学式为##STR1##其中X是乙烯和乙烯基类的成员,并取代1(2H)-邻苯二酮环的第六或第七位置的氢原子;Y是氢和羟基类的成员;R.sub.1是氢、烷基、烷氧基、羟基、卤素、硝基、--NR.sub.3 R.sub.4、--COR.sub.5和--O--A类的成员,其中A是与--O--形成酯或所述酯的碱金属盐的矿酸残基,R.sub.2是氢、烷基、苯基、取代苯基、杂环烯基、羟基烷基、多羟基烷基、氨基烷基、烷基氨基烷基和羧基烷基类的成员,R.sub.3、R.sub.4独立地来自氢、烷基、氨基烷基或烷基氨基烷基类,R.sub.5是OR.sub.3和##STR2##类的成员,例如羟基、甲氧基、2-二甲氨基乙氧基或2-二甲基氨基乙基氨基,其中烷基和烷基烯分别指含有最多约八个碳原子的单价或二价饱和脂肪基团,其中烷基氨基或烷基氨基烷基的氮原子可以与烷基或烷基烯基形成杂环,取代苯基可以通过烷基、羟基、烷氧基、卤素、硝基或氨基等取代,取代杂环烯基可以是例如2-吡啶基。