申请人:A. H. Robins Company, Incorporated
公开号:US05273993A1
公开(公告)日:1993-12-28
Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula: (HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.z wherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.
本发明涉及治疗慢性关节炎和骨质疏松症的方法,利用已知和新颖化合物,这些化合物可归为以下一般式:(HO)p-A-[-OS(O).sub.2 NR.sup.1 R.sup.2].sub.z,其中A包括一系列值,包括但不限于芳基,低烷基,环烷基和碳水化合物,包括蔗糖和果糖;p等于分子中未反应的羟基数,可以为零;z是-OS(O).sub.2 NR.sup.1 R.sup.2基团的数量,始终至少为一;R.sup.1和R.sup.2从氢,低烷基,羧基等中选择;提供了一种新颖的制备该化合物的过程,其中适当的磺酸芳基酯与含有保护羧基,氨基或羟基取代基团的羟基取代A基团在无极溶剂中反应,其中含有三级胺碱。还提供了用于治疗慢性关节炎和骨质疏松症的药物组合物。