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    • 2. 发明授权
    • Substituted alkanediphosphonic acids and pharmaceutical use
    • 取代的烷二膦酸和药用
    • US4939130A
    • 1990-07-03
    • US315962
    • 1989-02-27
    • Knut A. JaeggiLeo Widler
    • Knut A. JaeggiLeo Widler
    • C07F9/38A61K31/66A61K31/665A61K31/67A61K31/675A61P3/00A61P3/02A61P3/14A61P9/10A61P29/00A61P35/00A61P43/00C07F9/547C07F9/645C07F9/6503C07F9/6506C07F9/6518C07F9/653C07F9/6539
    • C07F9/65061C07F9/65032C07F9/65033C07F9/65062C07F9/65181C07F9/65182C07F9/6539
    • Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.1 is a functionally modified phosphono group and X.sub.2 is a free or functionally modified phosphono group, X.sub.1 and, if appropriate X.sub.2, into the free phosphono group.
    • 烷基膦酸,特别是式(I)的杂芳烷基亚烷基二酸,其中R 1是可与苯或环己烯核稠合的5元杂芳基,并且其含有2至4个N原子或1或4个N原子 2个N原子以及1个O-或S-原子,并且是被低级烷基,苯基或被低级烷基,低级烷氧基和/或卤素取代的苯基未被取代或C取代,或被低级烷氧基,羟基 ,二低级烷基氨基,低级烷硫基和/或卤素,和/或在能够被低级烷基,低级烷氧基和/或卤素取代的N-原子上被N-取代,并且R 2是氢,羟基,氨基, 低级烷硫基或卤素及其盐具有对钙代谢的调节作用,可用作治疗与钙代谢损伤有关的疾病的药物。 化合物例如通过在其中X 1是官能改性的膦酰基并且X 2是游离或官能改性的膦酰基的式(II)化合物中转化为X1,并且如果合适的话,X2转化成游离膦酰基 组。
    • 6. 发明授权
    • Araliphatylaminoalkanediphosphonic acids
    • 芳烷基亚氨基烷二膦酸
    • US5110807A
    • 1992-05-05
    • US500441
    • 1990-03-28
    • Knut A. Jaeggi
    • Knut A. Jaeggi
    • C07F9/38C07F9/58C07F9/6506
    • C07F9/65067C07F9/3873C07F9/588
    • Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolism disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is a carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorous trichloride and hydrolysing the primary product.
    • 式(I)的芳烷基氨基烷二膦酸,其中R 1是芳香取代的脂族基团,R 2是氢或一价脂族基团,并且alk是二价脂族基团,并且它们的盐表现出对钙代谢的显着的调节作用 用作治疗可归因于钙代谢紊乱的疾病的药物。 它们例如通过使其中X3是羧基并且R0是基团R2的式IMAMA(V)的化合物与亚磷酸和三氯化磷反应并水解初级产物来制备。