申请人:Merck & Co., Inc.
公开号:US05403952A1
公开(公告)日:1995-04-04
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##
式I的新型取代环化合物被发现是治疗基质金属蛋白酶介导疾病的有用抑制剂,包括骨关节炎、类风湿关节炎、败血性关节炎、某些癌症的肿瘤浸润、牙周病、角膜溃疡、蛋白尿、营养不良性表皮松解症和与动脉粥样硬化斑块破裂相关的冠状动脉血栓形成。基质金属蛋白酶是一类含锌蛋白酶家族,包括但不限于基质金属蛋白酶、胶原酶和明胶酶,能够降解关节软骨和基底膜的主要成分。本文所宣称的抑制剂也可以用于预防创伤性损伤后可能导致永久性残疾的病理性后遗症。这些化合物还可以作为新型避孕药物,通过防止排卵或着床来使用。