Alpha position heteroatom substituted gamma aryl ketobutyric acid derivative, process, pharmaceutical combination and uses thereof
Patent Information
- Authority / Receiving Office
- CN · China
- Current Assignee / Owner
- INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
- Publication Date
- 2005-01-19
- Estimated Expiration
- Not applicable · inactive patent
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Abstract
Description
technical field
[0001] The present invention relates to butyronic acid derivatives, their preparation method, their pharmaceutical composition, and their use as medicine, especially as medicine for treating osteoarthritis and tumor. Background technique
[0002] Matrix metalloproteinases (Matrix Metalloproteinases, MMPs) is a general term for a class of endopeptidases whose active sites contain zinc ions, and exist on the extracellular matrix and membrane surface. It is mainly secreted by fibroblasts, neutrophils, macrophages and tumor cells in the form of inactive zymogen, and activated by corresponding enzymes in the extracellular matrix (Extra Cellular Matrix, ECM). MMPs can hydrolyze different protein substrates, such as: collagen, gelatin, proteoglycan, fibroblast, elastin, etc. It is regulated in three ways in vivo: mediated by cytokines and growth factors; activation of zymogens; participation of endogenous inhibitors (TIMPs, Tissue Inhibitors of Matrix Metalloprotei...