New carboxy-reduced and selectively O-sulfated chondroitin sulfate derivatives, useful for treating e.g. articular degeneration or disorders of bone metabolism, are inhibitors of matrix metalloproteases

摘要

Isolated or mixed carboxy-reduced and chemoselectively O-sulfated derivatives (A) of chondroitin sulfate (CS) and their salts are new. An independent claim is also included for three methods for preparing (A). ACTIVITY : Antiarthritic; Vulnerary; Analgesic; Osteopathic; Antiinflammatory; Muscular-Gen.; Antirheumatic. MECHANISM OF ACTION : Metalloprotease inhibitor. Carboxy-reduced, persulfated CS had IC50 for inhibition of aggrecanase of 0.004 Microg/ml; inhibited factor Xa only weakly (1.2 units/mg; contrast 100 units /mg for reference heparin) and had IC50 against human MMP 2 and 7 of 0.4 Microg/ml.