METHANEDIPHOSPHONIC ACID DERIVATIVE, PRODUCTION THEREOF AND MEDICINAL USE THEREOF
申请人:TORAY INDUSTRIES, INC.
公开号:EP0594857A1
公开(公告)日:1994-05-04
A methanediphosphonic acid derivative represented by formulae (I) or (II), a process for producting the same, and a medicinal use thereof, wherein B represents hydrogen, alkyl, hydroxy, alkoxy or amino; D represents sulfur, oxygen, NH, alkyl-substituted nitrogen, CH₂ or SCH₂; X represents alkyl which may be substituted by a heteroatom, aryl or acyl; m represents an integer of 1 to 5; and R¹, R², R³ and R⁴ represent each independently hydrogen, C₁ to C₇, alkyl or a pharmacologically acceptable cation. The compound is excellent in IL-1 inhibition, antioxidant activity and bone resorption inhibition and useful for treating inflammation, rheumatism, bone metabolism disorder, autoimmune disease, osteoporosis, and so forth.
一种由式(I)或(II)代表的甲烷二膦酸衍生物、制备该衍生物的工艺及其医药用途,其中 B 代表氢、烷基、羟基、烷氧基或氨基;D 代表硫、氧、NH、烷基取代的氮、CH₂或 SCH₂;X 代表可被杂原子、芳基或酰基取代的烷基;m 代表 1 至 5 的整数;以及 R¹、R²、R³ 和 R⁴ 各自独立地代表氢、C₁ 至 C₇、烷基或药理学上可接受的阳离子。该化合物具有优异的抑制 IL-1、抗氧化活性和抑制骨吸收的作用,可用于治疗炎症、风湿病、骨代谢紊乱、自身免疫性疾病、骨质疏松症等。