申请人:Merrell Pharmaceuticals Inc.
公开号:US05545660A1
公开(公告)日:1996-08-13
This invention relates to novel hydrazide acyl hydrazinium derivatives of certain 3,4-dihydro-2H-1-benzopyrans of the formula ##STR1## the stereoisomers and mixtures thereof, their inner salts, and the pharmaceutically acceptable salts thereof wherein R is H or C.sub.1-6 alkyl, R.sub.1 is C.sub.1-6 alkyl, R.sub.2 is H or --C(O)R,R.sub.3 and R.sub.4 are independently C.sub.1-6 alkyl; R.sub.5 is C.sub.1-6 alkyl, or ##STR2## with R.sub.8 being H or halogeno, n is zero, 1, 2, or 3 and is a halide, --S(O).sub.3 R.sub.6, or nothing when the inner salt is formed R.sub.6 is H, C.sub.1-6 alkyl, phenyl or 4-methylphenyl, to the intermediates, processes and techniques for their preparation, to their ability to manifest the property of being free radical scavengers, and to their end-use application in the treatment of disease conditions capable of being ameliorated by free radical scavengers.
这项发明涉及某些3,4-二氢-2H-1-苯并吡喃的新型肼酰肼盐衍生物,其化学式为##STR1## 其立体异构体及其混合物,它们的内盐,及其药学上可接受的盐,其中R为H或C.sub.1-6烷基,R.sub.1为C.sub.1-6烷基,R.sub.2为H或--C(O)R,R.sub.3和R.sub.4独立地为C.sub.1-6烷基;R.sub.5为C.sub.1-6烷基,或##STR2## 其中R.sub.8为H或卤素,n为零,1,2或3且为卤化物,--S(O).sub.3R.sub.6,或当形成内盐时为空,R.sub.6为H,C.sub.1-6烷基,苯基或4-甲基苯基,以及它们的中间体,制备它们的方法和技术,它们表现为自由基清除剂的性质,以及它们在治疗能够通过自由基清除剂改善的疾病状况中的最终应用。