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Page 1
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
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.
Subasinghe NL, Travins JM, Ali F, Huang H, Ballentine SK, Marugán JJ, Khalil E, Hufnagel HR, Bone RF, DesJarlais RL, Crysler CS, Ninan N, Cummings MD, Molloy CJ, Tomczuk BE. Subasinghe NL, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2200-4. doi: 10.1016/j.bmcl.2006.01.036. Epub 2006 Feb 3. Bioorg Med Chem Lett. 2006. PMID: 16460935
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
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.
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
Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.
Subasinghe NL, Khalil E, Travins JM, Ali F, Ballentine SK, Hufnagel HR, Pan W, Leonard K, Bone RF, Soll RM, Crysler CS, Ninan N, Kirkpatrick J, Kolpak MX, Diloreto KA, Eisennagel SH, Huebert ND, Molloy CJ, Tomczuk BE, Gaul MD. Subasinghe NL, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5303-7. doi: 10.1016/j.bmcl.2012.06.030. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22795627
37 results