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Page 1
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD. Bilodeau MT, et al. Among authors: lynch jj. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB. Bell IM, et al. Among authors: lynch jj jr. J Med Chem. 2002 Jun 6;45(12):2388-409. doi: 10.1021/jm010531d. J Med Chem. 2002. PMID: 12036349
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Fraley ME, Arrington KL, Buser CA, Ciecko PA, Coll KE, Fernandes C, Hartman GD, Hoffman WF, Lynch JJ, McFall RC, Rickert K, Singh R, Smith S, Thomas KA, Wong BK. Fraley ME, et al. Among authors: lynch jj. Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5. doi: 10.1016/j.bmcl.2003.11.007. Bioorg Med Chem Lett. 2004. PMID: 14698157
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Morrissette MM, Stauffer KJ, Williams PD, Lyle TA, Vacca JP, Krueger JA, Lewis SD, Lucas BJ, Wong BK, White RB, Miller-Stein C, Lyle EA, Wallace AA, Leonard YM, Welsh DC, Lynch JJ, McMasters DR. Morrissette MM, et al. Among authors: lynch jj. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4161-4. doi: 10.1016/j.bmcl.2004.06.030. Bioorg Med Chem Lett. 2004. PMID: 15261262
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Sisko JT, Tucker TJ, Bilodeau MT, Buser CA, Ciecko PA, Coll KE, Fernandes C, Gibbs JB, Koester TJ, Kohl N, Lynch JJ, Mao X, McLoughlin D, Miller-Stein CM, Rodman LD, Rickert KW, Sepp-Lorenzino L, Shipman JM, Thomas KA, Wong BK, Hartman GD. Sisko JT, et al. Among authors: lynch jj. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. doi: 10.1016/j.bmcl.2005.11.089. Epub 2005 Dec 20. Bioorg Med Chem Lett. 2006. PMID: 16368234
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Nanda KK, Nolt MB, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Bogusky MJ, Bilodeau MT, Dinsmore CJ, Lindsley CW, Hartman GD, Wolkenberg SE, Trotter BW. Nanda KK, et al. Among authors: lynch jj. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5897-901. doi: 10.1016/j.bmcl.2006.08.054. Epub 2006 Sep 1. Bioorg Med Chem Lett. 2006. PMID: 16949818
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beshore DC, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Heimbrook DC, Homnick CF, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Miller PA, Omer CA, Rodrigues AD, Walsh ES, Williams TM. Bell IM, et al. Among authors: lynch jj jr. J Med Chem. 2001 Aug 30;44(18):2933-49. doi: 10.1021/jm010156p. J Med Chem. 2001. PMID: 11520202
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
Coleman PJ, Askew BC, Hutchinson JH, Whitman DB, Perkins JJ, Hartman GD, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Merkle KM, Lynch R, Lynch JJ, Rodan SB, Duggan ME. Coleman PJ, et al. Among authors: lynch r, lynch jj. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2463-5. doi: 10.1016/s0960-894x(02)00396-7. Bioorg Med Chem Lett. 2002. PMID: 12161158
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: lynch jj jr. J Med Chem. 2003 Feb 13;46(4):461-73. doi: 10.1021/jm020311f. J Med Chem. 2003. PMID: 12570369
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Burgey CS, Robinson KA, Lyle TA, Nantermet PG, Selnick HG, Isaacs RC, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Stranieri MT, Cook JJ, McMasters DR, Pellicore JM, Pal S, Wallace AA, Clayton FC, Bohn D, Welsh DC, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP. Burgey CS, et al. Among authors: lynch jj jr. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1353-7. doi: 10.1016/s0960-894x(03)00099-4. Bioorg Med Chem Lett. 2003. PMID: 12657281
376 results