- Discovery of novel cyanamide-based inhibitors of cathepsin C
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The discovery of potent and selective cyanamide-based inhibitors of the cysteine protease cathepsin C is detailed. Optimization of the template with regard to plasma stability led to the identification of compound 17, a potent cathepsin C inhibitor with excellent selectivity over other cathepsins and potent in vivo activity in a cigarette smoke mouse model.
- Laine, Dramane,Palovich, Michael,McCleland, Brent,Petitjean, Emilie,Delhom, Isabelle,Xie, Haibo,Deng, Jianghe,Lin, Guoliang,Davis, Roderick,Jolit, Anais,Nevins, Neysa,Zhao, Baoguang,Villa, Jim,Schneck, Jessica,McDevitt, Patrick,Midgett, Robert,Kmett, Casey,Umbrecht, Sandra,Peck, Brian,Davis, Alicia Bacon,Bettoun, David
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p. 142 - 147
(2011/04/15)
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- NOVEL CATHEPSIN C INHIBITORS AND THEIR USE
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The invention is directed to compounds according to Formula (I) wherein R1, R2a, R2b, R2c, R3, and n are defined below, and to pharmaceutically-acceptable salts thereof. They are cathepsin C inhibitors and can be used in the treatment of diseases mediated
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Page/Page column 100-101
(2009/04/25)
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