324795-39-3Relevant academic research and scientific papers
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S
Chatterjee, Arnab K.,Liu, Hong,Tully, David C.,Guo, Jianhua,Epple, Robert,Russo, Ross,Williams, Jennifer,Roberts, Michael,Tuntland, Tove,Chang, Jonathan,Gordon, Perry,Hollenbeck, Thomas,Tumanut, Christine,Li, Jun,Harris, Jennifer L.
, p. 2899 - 2903 (2008/12/22)
Peptidic, non-covalent inhibitors of lysosomal cysteine protease cathepsin S (1 and 2) were investigated due to low oral bioavailability, leading to an improved series of peptidomimetic inhibitors. Utilizing phenyl succinamides as the P2 residue increased the oral exposure of this lead series of compounds, while retaining selective inhibition of the cathepsin S isoform. Concurrent investigation of the P1 and P2 subsites resulted in the discovery of several potent and selective inhibitors of cathepsin S with good pharmacokinetic properties due to the elimination of saturated aliphatic P2 residues.
INHIBITORS OF CATHEPSIN S
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Page/Page column 51-52, (2008/06/13)
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
Novel succinate derivative compounds useful as cysteine protease inhibitors
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, (2008/06/13)
Disclosed are novel succinate derivative compounds of the formula (I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
Succinate derivative compounds useful as cysteine protease inhibitors
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, (2008/06/13)
Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
