850697-75-5Relevant academic research and scientific papers
The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors
Grice, Cheryl A.,Tays, Kevin,Khatuya, Haripada,Gustin, Darin J.,Butler, Christopher R.,Wei, Jianmei,Sehon, Clark A.,Sun, Siquan,Gu, Yin,Jiang, Wen,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.
, p. 2209 - 2212 (2007/10/03)
A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group foun
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors
Gustin, Darin J.,Sehon, Clark A.,Wei, Jianmei,Cai, Hui,Meduna, Steven P.,Khatuya, Haripada,Sun, Siquan,Gu, Yin,Jiang, Wen,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.
, p. 1687 - 1691 (2007/10/03)
A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.
