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    • 9. 发明申请
    • MMP-13 SELECTIVE INHIBITOR
    • MMP-13选择性抑制剂
    • US20090069304A1
    • 2009-03-12
    • US12281216
    • 2007-03-01
    • Mikayo HayashiFumihiko Watanabe
    • Mikayo HayashiFumihiko Watanabe
    • A61K31/5513C07D243/08C07D241/04A61K31/4965
    • C07D209/86C07D211/96C07D241/04C07D243/08C07D295/22
    • Since it is thought that if the activity of MMP-13 can be inhibited, this will largely contribute to improvement or prevention of progession of pathological states, particularly, osteoarthritis (OA), resulting from or associated with the MMP-13 activity, the development of MMP-13 inhibitors is anticipated. There are provided a compound represented by the general formula (I): wherein R1 is optionally substituted aryl etc.; Z is C1-C5 alkylene which may be substituted and may be interrupted with a substituent selected from Substituent group a etc.; A is the formula: (R6 and R7 are each independently halogen, lower alkyl etc.; m and n are each independently 0, 1, or 2); R2 is a hydrogen atom, optionally substituted lower alkyl etc.; R3 is a hydrogen atom, optionally substituted lower alkyl etc.; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxy, lower alkyloxy etc.), or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof, and a pharmaceutical composition containing it as an active ingredient, which has the MMP-13 inhibiting activity.
    • 由于认为如果可以抑制MMP-13的活性,这将大大有助于改善或预防由MMP-13活性引起或与MMP-13活性相关的病理状态,特别是骨关节炎(OA),发展 的MMP-13抑制剂。 提供由通式(I)表示的化合物:其中R 1是任选取代的芳基等; Z是可以被取代的C1-C5亚烷基,可以被选自取代基组a等的取代基中断; A是下式:(R 6和R 7各自独立地为卤素,低级烷基等; m和n各自独立地为0,1或2); R2是氢原子,任选取代的低级烷基等; R3是氢原子,任选取代的低级烷基等; R4是氢原子; 或者R 3和R 4可以与相邻的碳原子一起与环一起取代; R5是羟基,低级烷氧基等)或光学活性异构体,其药学上可接受的盐或溶剂合物,以及含有其作为活性成分的具有MMP-13抑制活性的药物组合物。