申请人:Toray Industries, Inc.
公开号:US05527940A1
公开(公告)日:1996-06-18
The present invention relates to a methanediphosphonate derivative, its manufacturing process and pharmaceutical applications, that is represented with the following formula: ##STR1## (wherein, B is either hydrogen, an alkyl group, hydroxyl group, alkoxy group or amino group, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2 or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to 7 carbon atoms or pharmaceutically allowable cations). The compound of the present invention has excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and is useful as an antiinflammatory agent, antirheumatic, bone metabolic disease drug, autoimmune disease drug, osteoporosis drug and so forth.
本发明涉及一种
甲烷二膦酸盐衍
生物及其制备方法和药物应用,其
化学式如下:##STR1## (其中,B为氢、烷基、羟基、烷氧基或
氨基;D为
硫、氧、NH、烷基取代的N、CH.sub.2或SCH.sub.2;X表示烷基、含有杂原子的烷基、芳基或酰基;m表示1到5的整数;R.sup.1、R.sup.2、R.sup.3和R.sup.4独立地表示氢、具有1到7个碳原子的烷基或药用可允许的阳离子)。本发明的化合物具有出色的IL-1抑制作用、抗氧化作用和抑制骨吸收作用,可用作抗炎剂、抗风湿药、骨代谢疾病药、自身免疫病药、骨质疏松症药等。