Metalloproteinase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514362, 514363, 514370, 514372, 514477, 514626, 546309, 548135, 548139, 548192, 548206, 549 69, 564153, 564155, C07D21375, A61K 3144

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active

057475148

ABSTRACT:
The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.

REFERENCES:
patent: 4599361 (1986-07-01), Dickens et al.
J. Chem. Society, Perkin Transation, vol. 1, No. 9, 1975, pp. 857-860, Broughton et al.
Broughton, "Studies Concerning the Antibiotic Actinonin. Part VIII. Structure-Activity Relationships in the Actinonin Series," J. Chem. Soc., 9:857-860 (1975).
Cawston, et al., "Mammalian Collagenases, " Meth. In Enzymol., 80:711-722 (1981).
Cawston, et al., "A Rapid and Reproducible Assay for Collagenase Using
Cawston, et al., "Purification of Rabbit Bone Inhibitor of Collagenase," Biochem. J., 195:159-165 (1981).
Devlin, et al., "Studies Concerning the Antibiotic Actinonin. Part III. Synthesis of Structural Analogues of Actinonin by the Anhydride-Imide Method," J.C.S. Perkin Trans I, 830-841 (1975).
Sellers, "Separation in Latent Forms of Distinct Enzymes that When Activated Degrade Collagen, Gelatin and Proteoglycans," Biochem. J. 171:493-496 (1978).
Woessner, "Matrix Metalloproteinases and their Inhibitors in Connective Tissue Remodeling," FASEB J., 5:2145-2154. (1991).

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