发明名称 Substituted oxobutyric acids as matrix metalloprotease inhibitors
摘要 The present invention provides pharmaceutical compositions and methods for treating certain conditions comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metalloprotease, resulting in achievement of the desired effect. The compounds of the present invention are either of generalized formula (I) wherein y is 0, 2, or 3, r is 0-6, Z is (CH2)7 or (CH2)e-C6H4-(CH2)f, wherein e is 0-1 and f is 1-6, and R<15> is -H, -Cl, -OMe or (a), (b) wherein n is 0-4, R<17> is C2H5, allyl, benzyl, and R<16> is (c) wherein t is 0-1, x is 0-4, and R<4> is one of the following: halide, alkyl of 1-6 carbons, OR, NR2, NO2 (R = H or alkyl of 1-6 carbons). 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 atherosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
申请公布号 AU3121997(A) 申请公布日期 1997.12.05
申请号 AU19970031219 申请日期 1997.05.12
申请人 BAYER CORPORATION 发明人 BRIAN R. DIXON;JINSHAN CHEN;MICHAEL VAN ZANDT;DAVID R. BRITTELLI
分类号 A61K31/40;A61K31/00;A61K31/19;A61K31/403;A61K31/4035;A61P1/00;A61P1/02;A61P7/00;A61P7/02;A61P13/00;A61P13/02;A61P15/00;A61P19/00;A61P19/02;A61P21/00;A61P27/00;A61P27/02;A61P29/00;A61P35/00;A61P35/04;A61P43/00;C07C59/90;C07D209/48;C07D253/08 主分类号 A61K31/40
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