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Page 1
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Cai J, Baugh M, Black D, Long C, Jonathan Bennett D, Dempster M, Fradera X, Gillespie J, Andrews F, Boucharens S, Bruin J, Cameron KS, Cumming I, Hamilton W, Jones PS, Kaptein A, Kinghorn E, Maidment M, Martin I, Mitchell A, Rankovic Z, Robinson J, Scullion P, Uitdehaag JC, Vink P, Westwood P, van Zeeland M, van Berkom L, Bastiani M, Meulemans T. Cai J, et al. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4350-4. doi: 10.1016/j.bmcl.2010.06.072. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20598883
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T. Cai J, et al. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. doi: 10.1016/j.bmcl.2010.10.012. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2010. PMID: 21030256
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Cai J, Bennett DJ, Rankovic Z, Dempster M, Fradera X, Gillespie J, Cumming I, Finlay W, Baugh M, Boucharens S, Bruin J, Cameron KS, Hamilton W, Kerr J, Kinghorn E, McGarry G, Robinson J, Scullion P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Cai J, et al. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15. Bioorg Med Chem Lett. 2010. PMID: 20594841
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Hamilton E, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Scullion P, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Bruin J, Hamilton W, Uitdehaag J, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Rankovic Z, et al. Among authors: cai j. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. doi: 10.1016/j.bmcl.2010.01.100. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20149657
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Finlay W, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Arbuckle W, Anderson M, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Jones P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Rankovic Z, et al. Among authors: cai j. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6237-41. doi: 10.1016/j.bmcl.2010.08.101. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20843687
Therapeutic dosing of an orally active, selective cathepsin S inhibitor suppresses disease in models of autoimmunity.
Baugh M, Black D, Westwood P, Kinghorn E, McGregor K, Bruin J, Hamilton W, Dempster M, Claxton C, Cai J, Bennett J, Long C, McKinnon H, Vink P, den Hoed L, Gorecka M, Vora K, Grant E, Percival MD, Boots AM, van Lierop MJ. Baugh M, et al. Among authors: cai j. J Autoimmun. 2011 May;36(3-4):201-9. doi: 10.1016/j.jaut.2011.01.003. Epub 2011 Mar 24. J Autoimmun. 2011. PMID: 21439785
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Arbuckle W, Baugh M, Belshaw S, Bennett DJ, Bruin J, Cai J, Cameron KS, Claxton C, Dempster M, Everett K, Fradera X, Hamilton W, Jones PS, Kinghorn E, Long C, Martin I, Robinson J, Westwood P. Arbuckle W, et al. Among authors: cai j. Bioorg Med Chem Lett. 2011 Feb 1;21(3):932-5. doi: 10.1016/j.bmcl.2010.12.065. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21227690
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