477585-36-7Relevant academic research and scientific papers
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-α Converting Enzyme (TACE): Novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1′ substituents
Ott, Gregory R.,Asakawa, Naoyuki,Lu, Zhonghui,Anand, Rajan,Liu, Rui-Qin,Covington, Maryanne B.,Vaddi, Krishna,Qian, Mingxin,Newton, Robert C.,Christ, David D.,Trzaskos, James M.,Duan, James J.-W.
, p. 1577 - 1582 (2008/12/21)
Novel ((2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamides were found to be excellent P1′ substituents in conjunction with unique constrained β-amino hydroxamic acid scaffolds for the discovery of potent selective inhibitors of TNF-α Converting Enzyme (TACE). Optimized examples proved potent for TACE, exceptionally selective over a wide panel of MMP and ADAM proteases, potent in the suppression of LPS-induced TNF-α in human whole blood and orally bioavailable.
Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-alpha converting enzyme (TACE)
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, (2008/06/13)
The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
