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    • 9. 发明授权
    • Substituted cyclic derivatives as novel antidegenerative agents
    • 取代的环状衍生物作为新的抗代谢剂
    • US5403952A
    • 1995-04-04
    • US133493
    • 1993-10-08
    • William HagmannCharles G. CaldwellPaul R. Gooley
    • William HagmannCharles G. CaldwellPaul R. Gooley
    • C07C237/22C07K7/100
    • C07C237/22C07C2101/08C07C2101/10C07C2101/14C07C2101/16
    • Novel substituted cyclic compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also be useful as novel birth control agents by preventing ovulation or implantation. ##STR1##
    • 发现式I的新型取代的环状化合物是基质金属蛋白酶介导的疾病的有用的抑制剂,包括骨关节炎,类风湿性关节炎,脓毒性关节炎,某些癌症中的肿瘤侵袭,牙周病,角膜溃疡,蛋白尿,营养不良的表皮松解性大疱性和冠状动脉血栓相关 动脉粥样硬化斑块破裂。 基质金属蛋白酶是含有蛋白酶的家族,包括但不限于基质溶素,胶原酶和明胶酶,其能够降解关节软骨和基底膜的主要成分。 本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。 这些化合物也可以通过防止排卵或植入而用作新的避孕药。