- Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors
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Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-α release. Oral activity in the mouse LPS model of TNF-α release
- Zask, Arie,Kaplan, Joshua,Du, XueMei,MacEwan, Gloria,Sandanayaka, Vincent,Eudy, Nancy,Levin, Jeremy,Jin, Guixian,Xu, Jun,Cummons, Terri,Barone, Dauphine,Ayral-Kaloustian, Semiramis,Skotnicki, Jerauld
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p. 1641 - 1645
(2007/10/03)
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- ACETYLENIC ALPHA-AMINO ACID-BASED SULFONAMIDE HYDROXAMIC ACID TACE INHIBITORS
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Compound of the formula (B) are useful in treating disease conditions mediated by TNF- alpha , such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
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- Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors
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Compounds of the formula: 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 degenerative cartilage loss.
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