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    • 4. 发明申请
    • HETEROBICYCLIC MATRIX METALLOPROTEASE INHIBITORS
    • 异源基质金属蛋白酶抑制剂
    • WO2008063670A1
    • 2008-05-29
    • PCT/US2007/024365
    • 2007-11-20
    • ALANTOS PHARMACEUTICALS HOLDING, INC.HOCHGÜRTEL, MatthiasBLUHM, HaraldESSERS, MichaelKROTH, HeikoGEGE, ChristianTAVERAS, Arthur
    • HOCHGÜRTEL, MatthiasBLUHM, HaraldESSERS, MichaelKROTH, HeikoGEGE, ChristianTAVERAS, Arthur
    • C07D487/04C07D495/04A61K31/495A61K31/53A61P35/00A61P29/00
    • C07D487/04C07D519/00
    • The present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, of Formula (I) that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors. The heterobicyclic metalloprolease inhibiting compounds of the present invention may be used in the treatment of metalloprotease mediated diseases, such as rheumatoid arthritis, osteoarthritis, abdominal aortic aneurysm, cancer, inflammation, atherosclerosis, multiple sclerosis, chronic obstructive pulmonary disease, ocular diseases, neurological diseases, psychiatric diseases, thrombosis, bacterial infection, Parkinson's disease, fatigue, tremor, diabetic retinopathy, vascular diseases of the retina, aging, dementia, cardiomyopathy, renal tubular impairment, diabetes, psychosis, dyskinesia, pigmentary abnormalities, deafness, inflammatory and fibrotic syndromes, intestinal bowel syndrome, allergies, Alzheimer's disease, arterial plaque formation, periodontal, viral infection, stroke, cardiovascular disease, reperfusion injury, trauma, chemical exposure or oxidative damage to tissues, wound healing, hemorroid, skin beautifying, pain, inflammatory pain, bone pain and joint pain.
    • 本发明提供了与目前已知的MMP-13和MMP-3抑制剂相比显示增加的效力和选择性的新一类式(I)的杂双环MMP-3和/或MMP-13抑制化合物。 本发明的杂双环金属蛋白酶抑制化合物可用于治疗金属蛋白酶介导的疾病,例如类风湿性关节炎,骨关节炎,腹主动脉瘤,癌症,炎症,动脉粥样硬化,多发性硬化,慢性阻塞性肺病,眼病,神经系统疾病 精神疾病,血栓形成,细菌感染,帕金森病,疲劳,震颤,糖尿病性视网膜病变,视网膜血管疾病,衰老,痴呆,心肌病,肾小管损伤,糖尿病,精神病,运动障碍,色素异常,耳聋,炎性和纤维化综合征 肠道综合征,过敏症,阿尔茨海默病,动脉斑块形成,牙周病,病毒感染,中风,心血管疾病,再灌注损伤,创伤,化学暴露或对组织的氧化损伤,伤口愈合,血红细胞,皮肤美化,疼痛,炎性疼痛, 骨痛和关节疼痛。