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Items: 1 to 20 of 91

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.

J Med Chem. 2004 Dec 2;47(25):6363-72.

PMID:
15566305
2.

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R Sr, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ.

J Med Chem. 2006 Jun 29;49(13):3766-9.

PMID:
16789733
3.

Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.

Friesen RW, Ducharme Y, Ball RG, Blouin M, Boulet L, Côté B, Frenette R, Girard M, Guay D, Huang Z, Jones TR, Laliberté F, Lynch JJ, Mancini J, Martins E, Masson P, Muise E, Pon DJ, Siegl PK, Styhler A, Tsou NN, Turner MJ, Young RN, Girard Y.

J Med Chem. 2003 Jun 5;46(12):2413-26.

PMID:
12773045
4.

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ.

J Med Chem. 2007 May 3;50(9):2011-29. Epub 2007 Apr 11.

PMID:
17425296
5.

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.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5.

PMID:
14698157
6.

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.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. Epub 2005 Dec 20.

PMID:
16368234
7.

Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.

Lin H, Yamashita DS, Xie R, Zeng J, Wang W, Leber J, Safonov IG, Verma S, Li M, Lafrance L, Venslavsky J, Takata D, Luengo JI, Kahana JA, Zhang S, Robell KA, Levy D, Kumar R, Choudhry AE, Schaber M, Lai Z, Brown BS, Donovan BT, Minthorn EA, Brown KK, Heerding DA.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):684-8. doi: 10.1016/j.bmcl.2009.11.061. Epub 2009 Dec 16.

PMID:
20006500
8.

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E.

J Med Chem. 2010 Jul 22;53(14):5213-28. doi: 10.1021/jm100262j.

PMID:
20565112
9.

4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.

Fletcher SR, Burkamp F, Blurton P, Cheng SK, Clarkson R, O'Connor D, Spinks D, Tudge M, van Niel MB, Patel S, Chapman K, Marwood R, Shepheard S, Bentley G, Cook GP, Bristow LJ, Castro JL, Hutson PH, MacLeod AM.

J Med Chem. 2002 Jan 17;45(2):492-503.

PMID:
11784153
10.

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.

Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.

J Med Chem. 2005 Jul 28;48(15):4892-909.

PMID:
16033269
11.

Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.

Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3.

PMID:
19297154
12.

Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.

Vacher B, Bonnaud B, Funes P, Jubault N, Koek W, Assié MB, Cosi C, Kleven M.

J Med Chem. 1999 May 6;42(9):1648-60.

PMID:
10229633
13.

Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.

Cid JM, Tresadern G, Vega JA, de Lucas AI, Matesanz E, Iturrino L, Linares ML, Garcia A, Andrés JI, Macdonald GJ, Oehlrich D, Lavreysen H, Megens A, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA.

J Med Chem. 2012 Oct 25;55(20):8770-89. doi: 10.1021/jm3010724. Epub 2012 Oct 16.

PMID:
23072213
14.

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Ruel R, Thibeault C, L'Heureux A, Martel A, Cai ZW, Wei D, Qian L, Barrish JC, Mathur A, D'Arienzo C, Hunt JT, Kamath A, Marathe P, Zhang Y, Derbin G, Wautlet B, Mortillo S, Jeyaseelan R Sr, Henley B, Tejwani R, Bhide RS, Trainor GL, Fargnoli J, Lombardo LJ.

Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. doi: 10.1016/j.bmcl.2008.03.057. Epub 2008 Mar 22.

PMID:
18395443
15.

Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease.

Plowright AT, Nilsson K, Antonsson M, Amin K, Broddefalk J, Jensen J, Lehmann A, Jin S, St-Onge S, Tomaszewski MJ, Tremblay M, Walpole C, Wei Z, Yang H, Ulander J.

J Med Chem. 2013 Jan 10;56(1):220-40. doi: 10.1021/jm301511h. Epub 2012 Dec 24.

PMID:
23227781
16.

Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.

Ioannidis S, Lamb ML, Almeida L, Guan H, Peng B, Bebernitz G, Bell K, Alimzhanov M, Zinda M.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1669-73. doi: 10.1016/j.bmcl.2010.01.091. Epub 2010 Jan 25.

PMID:
20144546
17.

Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor agonists.

Chu GH, Saeui CT, Worm K, Weaver DG, Goodman AJ, Broadrup RL, Cassel JA, DeHaven RN, LaBuda CJ, Koblish M, Brogdon B, Smith S, Le Bourdonnec B, Dolle RE.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5931-5. doi: 10.1016/j.bmcl.2009.08.063. Epub 2009 Aug 21.

PMID:
19736007
18.

1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.

Micheli F, Bonanomi G, Blaney FE, Braggio S, Capelli AM, Checchia A, Curcuruto O, Damiani F, Fabio RD, Donati D, Gentile G, Gribble A, Hamprecht D, Tedesco G, Terreni S, Tarsi L, Lightfoot A, Stemp G, Macdonald G, Smith A, Pecoraro M, Petrone M, Perini O, Piner J, Rossi T, Worby A, Pilla M, Valerio E, Griffante C, Mugnaini M, Wood M, Scott C, Andreoli M, Lacroix L, Schwarz A, Gozzi A, Bifone A, Ashby CR Jr, Hagan JJ, Heidbreder C.

J Med Chem. 2007 Oct 18;50(21):5076-89. Epub 2007 Sep 15.

PMID:
17867665
19.

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.

J Med Chem. 2002 Jun 6;45(12):2388-409.

PMID:
12036349
20.

Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.

Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH, Chen Z, Frey RR, Johnson EF, Osterling DJ, Olson AM, Bouska JJ, Luo Y, Curtin ML, Donawho CK, Michaelides MR, Tse C, Davidsen SK, Albert DH.

J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. doi: 10.1124/jpet.112.197087. Epub 2012 Aug 30.

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