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    • 2. 发明授权
    • Methane diphosphonic acid derivative, its production process and its
pharmaceutical applications
    • 甲烷二膦酸衍生物,其生产工艺及其制药应用
    • US5565440A
    • 1996-10-15
    • US256186
    • 1994-06-28
    • Keijiro TakanishiNorio KawabeTeruo Nakadate
    • Keijiro TakanishiNorio KawabeTeruo Nakadate
    • A61K31/67A61P3/00A61P29/00C07D335/06C07F9/6553A61K31/38C07D333/64C07D337/08
    • C07F9/65539C07F9/655354C07F9/655372
    • The present invention discloses a methane diphosphonate derivative, a process for producing said derivative and its pharmaceutical applications, said methane diphosphonate derivative indicated with general formula (1): ##STR1## (wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a pharmacologically acceptable cation, a hydrogen atom or a straight chain or branched alkyl group having 1-4 carbon atoms, R.sub.5 is a hydrogen atom or a trialkylsilyl group, m is an integer of 0 to 3, n is an integer of 1 to 3, R.sub.6 and R.sub.7 are independently a hydrogen atom or an alkyl group, and X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group).The compounds of the present invention are useful as an anti-inflammatory, antipyretic, analgesic, antirheumatic drug, antiarthritic or anti-osteoporosis drug as a result of having anti-inflammatory action, antipyretic and an algesic action, or action which improves bone metabolic disorders caused by rheumatism, arthritis, osteoporosis and so forth.
    • PCT No.PCT / JP93 / 01579 Sec。 371日期:1994年6月28日 102(e)日期1994年6月28日PCT提交1993年10月29日PCT公布。 WO94 / 10181 PCT出版物 日期:1994年5月11日本发明公开了一种甲烷二膦酸酯衍生物,所述衍生物及其药物应用的制备方法,所述甲基二膦酸酯衍生物用通式(1)表示:其中R1,R2,R3 R4独立地为药理学上可接受的阳离子,氢原子或具有1-4个碳原子的直链或支链烷基,R5为氢原子或三烷基甲硅烷基,m为0-3的整数,n为整数 为1〜3,R6和R7独立地为氢原子或烷基,X为氢原子,卤素原子,烷基,烷氧基或烷硫基。 本发明的化合物可用作抗炎,解热,止痛,抗风湿药物,抗关节炎或抗骨质疏松症药物,具有抗炎作用,解热和止痛作用或改善骨代谢紊乱的作用 由风湿病,关节炎,骨质疏松症等引起。