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    • 6. 发明授权
    • Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acids
    • 通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
    • US06500847B2
    • 2002-12-31
    • US09845392
    • 2001-04-30
    • Michael C. VanZandtDavid R. BrittelliBrian R. Dixon
    • Michael C. VanZandtDavid R. BrittelliBrian R. Dixon
    • A61K3144
    • C07D253/08A61K31/425A61K31/426A61K31/4706A61K31/502A61K31/513A61K31/517A61K31/53A61K31/5513C07C62/38C07D237/32
    • Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
    • 提出了基质金属蛋白酶抑制化合物,其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式:其中r为0-2,选自T,R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶,因此可用于抑制MMP的贡献 ,如骨关节炎,类风湿关节炎,脓毒性关节炎,牙周病,角膜溃疡,蛋白尿,动脉瘤主动脉疾病,疏水性表皮松解症,大疱疹,导致炎症反应的病症,MMP活性介导的骨质减少,下颌关节病,神经系统脱髓鞘疾病 系统,肿瘤转移或创伤性关节损伤后的退行性软骨损失,以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。
    • 7. 发明授权
    • Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
    • 通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
    • US06225314B1
    • 2001-05-01
    • US09343142
    • 1999-06-29
    • Michael C. VanZandtDavid R. BrittelliBrian R. Dixon
    • Michael C. VanZandtDavid R. BrittelliBrian R. Dixon
    • A61K31495
    • C07D253/08A61K31/425A61K31/426A61K31/4706A61K31/502A61K31/513A61K31/517A61K31/53A61K31/5513C07C62/38C07D237/32
    • Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from arteriosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
    • 提出了基质金属蛋白酶抑制化合物,其药物组合物和使用这些化合物的疾病治疗方法。 本发明的化合物具有以下通式:其中r为0-2,选自T,R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶,因此可用于抑制MMP的贡献 ,如骨关节炎,类风湿关节炎,脓毒性关节炎,牙周病,角膜溃疡,蛋白尿,动脉瘤主动脉疾病,疏水性表皮松解症,大疱疹,导致炎症反应的病症,MMP活性介导的骨质减少,下颌关节病,神经系统脱髓鞘疾病 系统,肿瘤转移或创伤性关节损伤后的退行性软骨损失,以及动脉硬化斑块破裂引起的冠状动脉血栓形成。 本发明还提供了用于治疗这些病症的药物组合物和方法。