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    • 2. 发明授权
    • C2-C5-alkyl-imidazole-bisphosphonates
    • C2-C5-烷基 - 咪唑 - 双膦酸盐
    • US07977323B2
    • 2011-07-12
    • US12323696
    • 2008-11-26
    • Sven WeilerLeo WidlerJean Michel RondeauSimona CotestaWolfgang Jahnke
    • Sven WeilerLeo WidlerJean Michel RondeauSimona CotestaWolfgang Jahnke
    • A61K31/675C07F9/02
    • C07F9/6506
    • C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
    • C2-C5-烷基取代的[(咪唑-1-基)-1-羟基-1-膦酰基 - 乙基] - 膦酸,以及其制备方法或方法,它们在药物制剂的制备中的用途,它们 描述了用于治疗疾病,用于治疗疾病的方法,包括它们的药物制剂和/或用于治疗疾病的化合物。 该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病,例如Hutchinson-Gilford progeria综合征。 该化合物具有式I化合物,其中R 1和R 2之一是氢,另一个是支链或非支链的C 2 -C 5 - 烷基,并且可以是酯的游离形式,和/或 盐。