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    • 1. 发明申请
    • AMINOALKYLIMIDAZOLE DERIVATIVES AND THEIR USE IN MEDICINE
    • 氨基甲酰咪唑衍生物及其在医学中的应用
    • WO2003045381A1
    • 2003-06-05
    • PCT/GB2002/005329
    • 2002-11-27
    • MOLECULAR SKINCARE LIMITEDTAZI-AHNINI, RachidWARD, SimonCORK, MichaelDUFF, GordonHARRITY, JoeBAVIK, Claes
    • TAZI-AHNINI, RachidWARD, SimonCORK, MichaelDUFF, GordonHARRITY, JoeBAVIK, Claes
    • A61K31/4174
    • C07D403/06C07D233/54
    • The present invention provides compounds of formula (I) wherein R 1 is selected from phenyl, quinoline, isoquinoline and anthracene whereby each of these substituents may be optionally substituted by a group selected from halogen, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 dialkylamino and cyano; R 2 is selected from hydrogen and phenyl optionally substituted by a group selected from halogen, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 dialkylamino and cyano; R 3 is selected from halogen, C 1-12 hydrocarbyl, phenyl optionally substituted by a group selected from halogen, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 dialkylamino and cyano, and N-acyl piperazinyl; and X is selected from CO and SO 2 , with the proviso that when X is CO and R 1 and R 3 are both optionally substituted phenyl, R 2 is not hydrogen or when X is CO and R 2 and R 3 are both optionally substituted phenyl, R 1 is not hydrogen; and pharmaceutically acceptable derivatives and solvates thereof, pharmaceutical formulations containing them and their use in therapy particularly as CYP24 inhibitors.
    • 本发明提供式(I)化合物,其中R 1选自苯基,喹啉,异喹啉和蒽,其中这些取代基各自可以任选地被选自卤素,C 1-4烷氧基,C 1-4烷基 ,C 1-4二烷基氨基和氰基; R 2选自氢和任选被选自卤素,C 1-4烷氧基,C 1-4烷基,C 1-4二烷基氨基和氰基的基团取代的苯基; R 3选自卤素,C 1-12烃基,任选被选自卤素,C 1-4烷氧基,C 1-4烷基,C 1-4二烷基氨基和氰基的基团取代的苯基和N-酰基哌嗪基; 并且X选自CO和SO 2,条件是当X是CO且R 1和R 3都是任选取代的苯基时,R 2不是氢或当X是CO和R 2时, 和R 3都是任选取代的苯基,R 1不是氢; 及其药学上可接受的衍生物和溶剂合物,含有它们的药物制剂及其在治疗中的用途,特别是作为CYP24抑制剂。