申请人:Sterling Winthrop Inc.
公开号:US05187173A1
公开(公告)日:1993-02-16
4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl, 4-R.sub.4 -4-R.sub.5 -6-R.sub.6 -4,5,6,7-tetrahydro-2-saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I, II and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
4-R.sub.1 -R.sub.2 -R.sub.3 -2-糖精基甲基,4-R.sub.4 -4-R.sub.5 -6-R.sub.6 -4,5,6,7-四氢-2-糖精基甲基和4,7-C-4,5,6,7-四氢-2-糖精基甲酸酯、膦酸酯和膦酸酯,分别在此处的公式I、II和IIA中,用于治疗退行性疾病,以及含有它们的组合物,使用它们治疗退行性疾病的方法,以及通过将相应的2-卤甲基糖精与此处的公式III的磷酸酯、膦酸酯或膦酸反应在酸受体存在下制备它们的方法。