287096-72-4Relevant academic research and scientific papers
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates
Levin,Chen,Cheung,Cole,Crago,Delos Santos,Du,Khafizova,MacEwan,Niu,Salaski,Zask,Cummons,Sung,Xu,Zhang,Xu,Ayral-Kaloustian,Jin,Cowling,Barone,Mohler,Black,Skotnicki
, p. 2799 - 2803 (2007/10/03)
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors, all bearing a butynyloxy P1′ group, was explored. In particular, compound 5j has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and MMP-9, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.
Acetylenic β-sulfonamido and phosphinic acid amide hydroxamic acid TACE inhibitors
-
, (2008/06/13)
The invention discloses hydroxamide acids of the formula: STR1which are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn''s disease and degen
