321533-90-8Relevant articles and documents
TREATMENT OF INFLAMMATION AND RELATED DISORDERS BY ACTIVATION OF THE UNFOLDED PROTEIN RESPONSE
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Page/Page column 27, (2008/06/13)
The present invention is directed to a novel method for the treatment of diseases by activating the unfolded protein response (UPR), or of inhibiting the expression of the inducible isoform of the nitric oxide synthase (iNOS) enzyme, or both. New methylpyrazole compounds which activate the UPR, downregulate iNOS, and reduce inflammatory markers are disclose herein, as are compositions comprising said compounds and their applications as pharmaceuticals for the treatment of disease.
5-((1H-Pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
Gilbert, Adam M.,Bursavich, Matthew G.,Lombardi, Sabrina,Georgiadis, Katy E.,Reifenberg, Erica,Flannery, Carl R.,Morris, Elisabeth A.
, p. 1189 - 1192 (2007/10/03)
A series of 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5 (aggrecanase-2) is described. These compounds show μM functional inhibition of ADAMTS-5, and represent a new class of agents with the potential of inhibiting degradation of aggrecan, a major component of cartilage which is lost in osteoporosis. Compound 12 is noteworthy in that it has an ADAMTS-5 IC50: 1.1 μM and shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).