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    • 9. 发明授权
    • Topically administrable pharmaceutical preparations
    • 主要管理药物制剂
    • US5133972A
    • 1992-07-28
    • US546345
    • 1990-06-29
    • Pier G. FerriniCarlo VoellmyPeter H. StahlJonathan Green
    • Pier G. FerriniCarlo VoellmyPeter H. StahlJonathan Green
    • A61K9/00A61K9/70A61K31/66A61K31/675A61P17/00A61P43/00C07F9/38
    • A61K9/7053A61K31/66A61K31/675A61K9/7061A61K9/7076A61K9/7084
    • The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.1 -alkyl, or that is disubstituted by optionally Ar-containing alkylene, wherein two alkylene carbon atoms mar additionally be linked to one another via alkylene and Ar and Het.sub.1 are each as defined above, with the proviso that when R.sub.2 is --A--R.sub. 3, A is ethylene and R.sub.3 is unsubstituted or C.sub.1 -C.sub.3 alkyl-substituted amino, R.sub.1 is other than hydroxy.
    • 本发明涉及含有药学上可接受的式(I)的甲二膦酸衍生物及其盐的局部给药药物制剂,其中R1和R2各自为卤素,或其中R1为氢,R2为Ar-S-或Het1- NH-,其中Ar是未取代或取代的苯基,Het1是未经取代或取代的单环,5或6元单氮杂,二氮杂 - 或噻唑基 - 芳基,其通过环碳原子键合,或其中R1是氢或 羟基和R 2是-A-R 3,其中A是亚烷基,一方面,R 3是Het 2,其是通过环碳或环氮原子键合的Het1,或者另一方面,R 3是氢,或 未被取代或被相同或不同的选自烷基,环烷基,Ar-烷基,Ar-O-烷基,Ar-S-烷基和Het1 - 烷基的取代基取代或被取代的氨基,或被任意Ar- 其中两个亚烷基碳原子另外与一个a连接 通过亚烷基,Ar和Het1各自如上所定义,条件是当R 2是-A-R 3时,A是亚乙基,R 3是未取代的或C 1 -C 3烷基取代的氨基,R 1不是羟基。