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Page 1
Identification of a potent and selective non-basic cathepsin K inhibitor.
Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Léger S, Massé F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Thérien M, Truong VL, Wesolowski G, Zamboni R, Black WC. Li CS, et al. Among authors: kimmel db. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. doi: 10.1016/j.bmcl.2005.12.071. Epub 2006 Jan 18. Bioorg Med Chem Lett. 2006. PMID: 16413777
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Palmer JT, Bryant C, Wang DX, Davis DE, Setti EL, Rydzewski RM, Venkatraman S, Tian ZQ, Burrill LC, Mendonca RV, Springman E, McCarter J, Chung T, Cheung H, Janc JW, McGrath M, Somoza JR, Enriquez P, Yu ZW, Strickley RM, Liu L, Venuti MC, Percival MD, Falgueyret JP, Prasit P, Oballa R, Riendeau D, Young RN, Wesolowski G, Rodan SB, Johnson C, Kimmel DB, Rodan G. Palmer JT, et al. Among authors: kimmel db. J Med Chem. 2005 Dec 1;48(24):7520-34. doi: 10.1021/jm058198r. J Med Chem. 2005. PMID: 16302794
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. Gauthier JY, et al. Among authors: kimmel db. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15. Bioorg Med Chem Lett. 2008. PMID: 18226527
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Robichaud J, Black WC, Thérien M, Paquet J, Oballa RM, Bayly CI, McKay DJ, Wang Q, Isabel E, Léger S, Mellon C, Kimmel DB, Wesolowski G, Percival MD, Massé F, Desmarais S, Falgueyret JP, Crane SN. Robichaud J, et al. Among authors: kimmel db. J Med Chem. 2008 Oct 23;51(20):6410-20. doi: 10.1021/jm800610j. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811135
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.
Robichaud J, Oballa R, Prasit P, Falgueyret JP, Percival MD, Wesolowski G, Rodan SB, Kimmel D, Johnson C, Bryant C, Venkatraman S, Setti E, Mendonca R, Palmer JT. Robichaud J, et al. J Med Chem. 2003 Aug 14;46(17):3709-27. doi: 10.1021/jm0301078. J Med Chem. 2003. PMID: 12904076
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD, Huff JR, Kimmel DB, Leu CT, Meissner RS, Merkle K, Nagy R, Pennypacker B, Perkins JJ, Prueksaritanont T, Rodan GA, Varga SL, Wesolowski GA, Zartman AE, Rodan SB, Duggan ME. Hutchinson JH, et al. Among authors: kimmel db. J Med Chem. 2003 Oct 23;46(22):4790-8. doi: 10.1021/jm030306r. J Med Chem. 2003. PMID: 14561098
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.
Perkins JJ, Duong LT, Fernandez-Metzler C, Hartman GD, Kimmel DB, Leu CT, Lynch JJ, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME, Meissner RS. Perkins JJ, et al. Among authors: kimmel db. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4285-8. doi: 10.1016/j.bmcl.2003.09.055. Bioorg Med Chem Lett. 2003. PMID: 14643310
Nonpeptide alpha V beta 3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative.
Breslin MJ, Duggan ME, Halczenko W, Hartman GD, Duong LT, Fernandez-Metzler C, Gentile MA, Kimmel DB, Leu CT, Merkle K, Prueksaritanont T, Rodan GA, Rodan SB, Hutchinson JH. Breslin MJ, et al. Among authors: kimmel db. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4515-8. doi: 10.1016/j.bmcl.2004.06.040. Bioorg Med Chem Lett. 2004. PMID: 15357983
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Coleman PJ, Brashear KM, Askew BC, Hutchinson JH, McVean CA, Duong LT, Feuston BP, Fernandez-Metzler C, Gentile MA, Hartman GD, Kimmel DB, Leu CT, Lipfert L, Merkle K, Pennypacker B, Prueksaritanont T, Rodan GA, Wesolowski GA, Rodan SB, Duggan ME. Coleman PJ, et al. Among authors: kimmel db. J Med Chem. 2004 Sep 23;47(20):4829-37. doi: 10.1021/jm049874c. J Med Chem. 2004. PMID: 15369386
Cathepsin K inhibitors prevent bone loss in estrogen-deficient rabbits.
Pennypacker BL, Duong LT, Cusick TE, Masarachia PJ, Gentile MA, Gauthier JY, Black WC, Scott BB, Samadfam R, Smith SY, Kimmel DB. Pennypacker BL, et al. Among authors: kimmel db. J Bone Miner Res. 2011 Feb;26(2):252-62. doi: 10.1002/jbmr.223. J Bone Miner Res. 2011. PMID: 20734451 Free article.
120 results