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Page 1
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
Structure-based optimization of a potent class of arylamide FMS inhibitors.
Meegalla SK, Wall MJ, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Illig CR. Meegalla SK, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3632-7. doi: 10.1016/j.bmcl.2008.04.059. Epub 2008 Apr 26. Bioorg Med Chem Lett. 2008. PMID: 18495479
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.
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR. Kreutter KD, et al. Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18420408
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Qiao L, Baumann CA, Crysler CS, Ninan NS, Abad MC, Spurlino JC, Desjarlais RL, Kervinen J, Neeper MP, Bayoumy SS, Williams R, Deckman IC, Dasgupta M, Reed RL, Huebert ND, Tomczuk BE, Moriarty KJ. Qiao L, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. doi: 10.1016/j.bmcl.2005.09.037. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236500
Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.
Travins JM, Ali F, Huang H, Ballentine SK, Khalil E, Hufnagel HR, Pan W, Gushue J, Leonard K, Bone RF, Soll RM, DesJarlais RL, Crysler CS, Ninan N, Kirkpatrick J, Cummings MD, Huebert N, Molloy CJ, Gaul M, Tomczuk BE, Subasinghe NL. Travins JM, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1603-6. doi: 10.1016/j.bmcl.2008.01.064. Epub 2008 Jan 19. Bioorg Med Chem Lett. 2008. PMID: 18242991
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
37 results