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Page 1
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR. Lu T, et al. Among authors: crysler cs. J Med Chem. 2010 Feb 25;53(4):1843-56. doi: 10.1021/jm901802n. J Med Chem. 2010. PMID: 20102150 Clinical Trial.
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR. Lee YK, et al. Among authors: crysler cs. J Med Chem. 2008 Jan 24;51(2):282-97. doi: 10.1021/jm701217r. Epub 2007 Dec 27. J Med Chem. 2008. PMID: 18159923
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.
Illig CR, Chen J, Wall MJ, Wilson KJ, Ballentine SK, Rudolph MJ, DesJarlais RL, Chen Y, Schubert C, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK. Illig CR, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1642-8. doi: 10.1016/j.bmcl.2008.01.059. Epub 2008 Jan 19. Bioorg Med Chem Lett. 2008. PMID: 18242992
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
Wilson KJ, Illig CR, Chen J, Wall MJ, Ballentine SK, DesJarlais RL, Chen Y, Schubert C, Donatelli R, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK. Wilson KJ, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2010 Jul 1;20(13):3925-9. doi: 10.1016/j.bmcl.2010.05.013. Epub 2010 May 12. Bioorg Med Chem Lett. 2010. PMID: 20570147
Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).
Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE. Illig CR, et al. Among authors: crysler cs. J Med Chem. 2011 Nov 24;54(22):7860-83. doi: 10.1021/jm200900q. Epub 2011 Oct 31. J Med Chem. 2011. PMID: 22039836
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.
Illig CR, Manthey CL, Meegalla SK, Wall MJ, Chen J, Wilson KJ, DesJarlais RL, Ballentine SK, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE. Illig CR, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6363-9. doi: 10.1016/j.bmcl.2013.09.061. Epub 2013 Oct 1. Bioorg Med Chem Lett. 2013. PMID: 24138939
37 results