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Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt.

Gauld S, Jacquet S, Gauvin D, Wallace C, Wang Y, McCarthy R, Goess C, Leys L, Huang S, Su Z, Edelmayer R, Wetter J, Salte K, McGaraughty S, Argiriadi M, Honore P, Luccarini JM, Bressac D, Desino K, Breinlinger E, Cusack K, Potin D, Kort M, Masson P.

J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046. doi: 10.1124/jpet.119.258046. [Epub ahead of print]


Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists.

Amaudrut J, Argiriadi MA, Barth M, Breinlinger EC, Bressac D, Broqua P, Calderwood DJ, Chatar M, Cusack KP, Gauld SB, Jacquet S, Kamath RV, Kort ME, Lepais V, Luccarini JM, Masson P, Montalbetti C, Mounier L, Potin D, Poupardin O, Rouaud S, Spitzer L, Wallace CD.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1799-1806. doi: 10.1016/j.bmcl.2019.05.015. Epub 2019 May 9.


Room-Temperature and Selective Triggering of Supramolecular DNA Assembly/Disassembly by Nonionizing Radiation.

Greschner AA, Ropagnol X, Kort M, Zuberi N, Perreault J, Razzari L, Ozaki T, Gauthier MA.

J Am Chem Soc. 2019 Feb 27;141(8):3456-3469. doi: 10.1021/jacs.8b10355. Epub 2019 Feb 14.


In Search of System-Wide Productivity Gains - The Role of Global Collaborations in Preclinical Translation.

Ussi AE, de Kort M, Coussens NP, Aittokallio T, Hajduch M.

Clin Transl Sci. 2017 Nov;10(6):423-425. doi: 10.1111/cts.12498. Epub 2017 Sep 19. No abstract available.


TRPV1 ligands with hyperthermic, hypothermic and no temperature effects in rats.

Gomtsyan A, McDonald HA, Schmidt RG, Daanen JF, Voight EA, Segreti JA, Puttfarcken PS, Reilly RM, Kort ME, Dart MJ, Kym PR.

Temperature (Austin). 2015 May 22;2(2):297-301. doi: 10.1080/23328940.2015.1046013. eCollection 2015 Apr-Jun.


Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR.

J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2.


Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.

Frost JM, DeGoey DA, Shi L, Gum RJ, Fricano MM, Lundgaard GL, El-Kouhen OF, Hsieh GC, Neelands T, Matulenko MA, Daanen JF, Pai M, Ghoreishi-Haack N, Zhan C, Zhang XF, Kort ME.

J Med Chem. 2016 Apr 14;59(7):3373-91. doi: 10.1021/acs.jmedchem.6b00063. Epub 2016 Apr 5.


Synthesis and Evaluation of a Series of Long-Acting Glucagon-Like Peptide-1 (GLP-1) Pentasaccharide Conjugates for the Treatment of Type 2 Diabetes.

Irwin N, Patterson S, de Kort M, Moffett RC, Wisse JA, Dokter WH, Bos ES, Miltenburg AM, Flatt PR.

ChemMedChem. 2015 Aug;10(8):1424-34. doi: 10.1002/cmdc.201500140. Epub 2015 Jun 9.


Pharmacological characterization and antidiabetic activity of a long-acting glucagon-like peptide-1 analogue conjugated to an antithrombin III-binding pentasaccharide.

Patterson S, de Kort M, Irwin N, Moffett RC, Dokter WH, Bos ES, Miltenburg AM, Flatt PR.

Diabetes Obes Metab. 2015 Aug;17(8):760-70. doi: 10.1111/dom.12483. Epub 2015 Jun 16.


Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.

Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME.

J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21.


Transient receptor potential channel ankyrin-1 is not a cold sensor for autonomic thermoregulation in rodents.

de Oliveira C, Garami A, Lehto SG, Pakai E, Tekus V, Pohoczky K, Youngblood BD, Wang W, Kort ME, Kym PR, Pinter E, Gavva NR, Romanovsky AA.

J Neurosci. 2014 Mar 26;34(13):4445-52. doi: 10.1523/JNEUROSCI.5387-13.2014.


Half-life prolongation of therapeutic proteins by conjugation to ATIII-binding pentasaccharides: a first-in-human study of CarboCarrier® insulin.

Miltenburg AM, Prohn M, van Kuijk JH, Tiessen RG, de Kort M, Berg RJ.

Br J Clin Pharmacol. 2013 May;75(5):1221-30. doi: 10.1111/j.1365-2125.2012.04460.x.


Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature.

Reilly RM, McDonald HA, Puttfarcken PS, Joshi SK, Lewis L, Pai M, Franklin PH, Segreti JA, Neelands TR, Han P, Chen J, Mantyh PW, Ghilardi JR, Turner TM, Voight EA, Daanen JF, Schmidt RG, Gomtsyan A, Kort ME, Faltynek CR, Kym PR.

J Pharmacol Exp Ther. 2012 Aug;342(2):416-28. doi: 10.1124/jpet.111.190314. Epub 2012 May 8.


TRPV1 antagonists: clinical setbacks and prospects for future development.

Kort ME, Kym PR.

Prog Med Chem. 2012;51:57-70. doi: 10.1016/B978-0-12-396493-9.00002-9. Review. No abstract available.


Capsaicin-induced inhibition of platelet aggregation is not mediated by transient receptor potential vanilloid type 1.

Mittelstadt SW, Nelson RA, Daanen JF, King AJ, Kort ME, Kym PR, Lubbers NL, Cox BF, Lynch JJ 3rd.

Blood Coagul Fibrinolysis. 2012 Jan;23(1):94-7. doi: 10.1097/MBC.0b013e32834ddf18.


Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.

Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, Segreti JA, Han P, Zhang XF, Niforatos W, Bianchi BR, Baker SJ, Zhong C, Simler GH, McDonald HA, Schmidt RG, McGaraughty SP, Chu KL, Faltynek CR, Kort ME, Reilly RM, Kym PR.

Pain. 2011 May;152(5):1165-72. doi: 10.1016/j.pain.2011.01.049. Epub 2011 Mar 12.


Synthesis of oxazolo[4,5-c]quinoline TRPV1 antagonists.

Voight EA, Daanen JF, Kort ME.

J Org Chem. 2010 Dec 17;75(24):8713-5. doi: 10.1021/jo101938b. Epub 2010 Nov 23.


Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.

Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME.

Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29.


Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.

Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. doi: 10.1016/j.bmcl.2010.08.121. Epub 2010 Sep 18.


A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model.

Puttfarcken PS, Han P, Joshi SK, Neelands TR, Gauvin DM, Baker SJ, Lewis LG, Bianchi BR, Mikusa JP, Koenig JR, Perner RJ, Kort ME, Honore P, Faltynek CR, Kym PR, Reilly RM.

Pain. 2010 Aug;150(2):319-26. doi: 10.1016/j.pain.2010.05.015. Epub 2010 Jun 19.


Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature.

Voight EA, Kort ME.

Expert Opin Ther Pat. 2010 Sep;20(9):1107-22. doi: 10.1517/13543776.2010.497756. Review.


Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

Perner RJ, Koenig JR, Didomenico S, Gomtsyan A, Schmidt RG, Lee CH, Hsu MC, McDonald HA, Gauvin DM, Joshi S, Turner TM, Reilly RM, Kym PR, Kort ME.

Bioorg Med Chem. 2010 Jul 1;18(13):4821-9. doi: 10.1016/j.bmc.2010.04.099. Epub 2010 May 10.


A-887826 is a structurally novel, potent and voltage-dependent Na(v)1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats.

Zhang XF, Shieh CC, Chapman ML, Matulenko MA, Hakeem AH, Atkinson RN, Kort ME, Marron BE, Joshi S, Honore P, Faltynek CR, Krafte DS, Jarvis MF.

Neuropharmacology. 2010 Sep;59(3):201-7. doi: 10.1016/j.neuropharm.2010.05.009. Epub 2010 Jun 1.


TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats.

McGaraughty S, Chu KL, Perner RJ, Didomenico S, Kort ME, Kym PR.

Mol Pain. 2010 Mar 5;6:14. doi: 10.1186/1744-8069-6-14.


From heparin to EP217609: the long way to a new pentasaccharide-based neutralisable anticoagulant with an unprecedented pharmacological profile.

Petitou M, Nancy-Portebois V, Dubreucq G, Motte V, Meuleman D, de Kort M, van Boeckel CA, Vogel GM, Wisse JA.

Thromb Haemost. 2009 Nov;102(5):804-10. doi: 10.1160/TH09-01-0063. Review.


Analgesic potential of TRPV1 antagonists.

Kym PR, Kort ME, Hutchins CW.

Biochem Pharmacol. 2009 Aug 1;78(3):211-6. doi: 10.1016/j.bcp.2009.02.014. Epub 2009 Mar 5.


Voltage-gated sodium channel blockers for the treatment of chronic pain.

Matulenko MA, Scanio MJ, Kort ME.

Curr Top Med Chem. 2009;9(4):362-76. Review.


Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.

Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, Segreti JA, Banfor PN, Marsh K, Neelands T, Bayburt E, Daanen JF, Gomtsyan A, Lee CH, Kort ME, Reilly RM, Surowy CS, Kym PR, Mantyh PW, Sullivan JP, Jarvis MF, Faltynek CR.

Pain. 2009 Mar;142(1-2):27-35. doi: 10.1016/j.pain.2008.11.004. Epub 2009 Jan 9.


Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models.

Joshi SK, Honore P, Hernandez G, Schmidt R, Gomtsyan A, Scanio M, Kort M, Jarvis MF.

J Pain. 2009 Mar;10(3):306-15. doi: 10.1016/j.jpain.2008.09.007. Epub 2008 Dec 13.


Characterization of A-425619 at native TRPV1 receptors: a comparison between dorsal root ganglia and trigeminal ganglia.

McDonald HA, Neelands TR, Kort M, Han P, Vos MH, Faltynek CR, Moreland RB, Puttfarcken PS.

Eur J Pharmacol. 2008 Oct 31;596(1-3):62-9. doi: 10.1016/j.ejphar.2008.07.063. Epub 2008 Aug 5.


Block of Nav1.8 by small molecules.

Krafte DS, Chapman M, Marron B, Atkinson R, Liu Y, Ye F, Curran M, Kort M, Jarvis MF.

Channels (Austin). 2007 May-Jun;1(3):152-3. Epub 2007 Jul 18.


Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.

Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Thomas JB, Johnson MS, Carroll WA, Marron BE, Chapman ML, Liu D, Krambis MJ, Shieh CC, Zhang X, Hernandez G, Gauvin DM, Mikusa JP, Zhu CZ, Joshi S, Honore P, Marsh KC, Roeloffs R, Werness S, Krafte DS, Jarvis MF, Faltynek CR, Kort ME.

Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. doi: 10.1016/j.bmc.2008.05.003. Epub 2008 May 6.


Molecular determinants of species-specific activation or blockade of TRPA1 channels.

Chen J, Zhang XF, Kort ME, Huth JR, Sun C, Miesbauer LJ, Cassar SC, Neelands T, Scott VE, Moreland RB, Reilly RM, Hajduk PJ, Kym PR, Hutchins CW, Faltynek CR.

J Neurosci. 2008 May 7;28(19):5063-71. doi: 10.1523/JNEUROSCI.0047-08.2008.


Conjugation of ATIII-binding pentasaccharides to extend the half-life of proteins: long-acting insulin.

de Kort M, Gianotten B, Wisse JA, Bos ES, Eppink MH, Mattaar E, Vogel GM, Dokter WH, Honing M, Vonsovic S, Smit MJ, Wijkmans JC, van Boeckel CA.

ChemMedChem. 2008 Aug;3(8):1189-93. doi: 10.1002/cmdc.200800053. No abstract available.


Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.

Kort ME, Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Johnson MS, Pacofsky GJ, Thomas JB, Carroll WA, Krambis MJ, Liu D, Shieh CC, Zhang X, Hernandez G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Marsh KC, Murray BP, Liu J, Werness S, Faltynek CR, Krafte DS, Jarvis MF, Chapman ML, Marron BE.

J Med Chem. 2008 Feb 14;51(3):407-16. doi: 10.1021/jm070637u. Epub 2008 Jan 5.


A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats.

McGaraughty S, Chu KL, Scanio MJ, Kort ME, Faltynek CR, Jarvis MF.

J Pharmacol Exp Ther. 2008 Mar;324(3):1204-11. Epub 2007 Dec 18.


Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.

Perez-Medrano A, Brune ME, Buckner SA, Coghlan MJ, Fey TA, Gopalakrishnan M, Gregg RJ, Kort ME, Scott VE, Sullivan JP, Whiteaker KL, Carroll WA.

J Med Chem. 2007 Nov 29;50(24):6265-73. Epub 2007 Oct 31.


A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS.

Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. Epub 2007 May 2.


P2X7-related modulation of pathological nociception in rats.

McGaraughty S, Chu KL, Namovic MT, Donnelly-Roberts DL, Harris RR, Zhang XF, Shieh CC, Wismer CT, Zhu CZ, Gauvin DM, Fabiyi AC, Honore P, Gregg RJ, Kort ME, Nelson DW, Carroll WA, Marsh K, Faltynek CR, Jarvis MF.

Neuroscience. 2007 Jun 8;146(4):1817-28. Epub 2007 May 3.


Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.

Altenbach RJ, Brune ME, Buckner SA, Coghlan MJ, Daza AV, Fabiyi A, Gopalakrishnan M, Henry RF, Khilevich A, Kort ME, Milicic I, Scott VE, Smith JC, Whiteaker KL, Carroll WA.

J Med Chem. 2006 Nov 16;49(23):6869-87.


Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.

Nelson DW, Gregg RJ, Kort ME, Perez-Medrano A, Voight EA, Wang Y, Grayson G, Namovic MT, Donnelly-Roberts DL, Niforatos W, Honore P, Jarvis MF, Faltynek CR, Carroll WA.

J Med Chem. 2006 Jun 15;49(12):3659-66.


Synthetic heparin derivatives as new anticoagulant drugs.

de Kort M, Buijsman RC, van Boeckel CA.

Drug Discov Today. 2005 Jun 1;10(11):769-79. Review.


Synthesis and structure-activity relationships of a novel series of tricyclic dihydropyridine-based KATP openers that potently inhibit bladder contractions in vitro.

Carroll WA, Agrios KA, Altenbach RJ, Buckner SA, Chen Y, Coghlan MJ, Daza AV, Drizin I, Gopalakrishnan M, Henry RF, Kort ME, Kym PR, Milicic I, Smith JC, Tang R, Turner SC, Whiteaker KL, Zhang H, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3180-92.


Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.

Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3163-79.


Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.

Perez-Medrano A, Buckner SA, Coghlan MJ, Gregg RJ, Gopalakrishnan M, Kort ME, Lynch JK, Scott VE, Sullivan JP, Whiteaker KL, Carroll WA.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):397-400.


The pursuit of differentiated ligands for the glucocorticoid receptor.

Coghlan MJ, Elmore SW, Kym PR, Kort ME.

Curr Top Med Chem. 2003;3(14):1617-35. Review.


A versatile approach towards regioselective platinated DNA sequences.

Heetebrij RJ, de Kort M, Meeuwenoord NJ, den Dulk H, van der Marel GA, van Boom JH, Reedijk J.

Chemistry. 2003 Apr 14;9(8):1823-7.


Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC.

J Med Chem. 2003 Mar 13;46(6):1016-30.


Conformational analysis of cyclophostin and designed analogs in comparison with the potent IP3 receptor agonist adenophostin A.

Iwata Y, de Kort M, Challiss RA, van der Marel GA, van Boom JH, Miyamoto S.

Drug Des Discov. 2001;17(3):253-63.


Spirophostins: conformationally restricted analogues of adenophostin A.

de Kort M, Regenbogen AD, Valentijn AR, Challiss RA, Iwata Y, Miyamoto S, van der Marel GA, van Boom JH.

Chemistry. 2000 Aug 4;6(15):2696-704.


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