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391 results

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Page 1
Evaluation of a Series of β-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads.
Oehlrich D, Peschiulli A, Tresadern G, Van Gool M, Vega JA, De Lucas AI, Alonso de Diego SA, Prokopcova H, Austin N, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Rombouts FJR, Macdonald G, Moechars D, Gijsen HJM, Trabanco AA. Oehlrich D, et al. Among authors: vega ja. ACS Med Chem Lett. 2019 Jul 2;10(8):1159-1165. doi: 10.1021/acsmedchemlett.9b00181. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413800 Free PMC article.
Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors.
Tresadern G, Delgado F, Delgado O, Gijsen H, Macdonald GJ, Moechars D, Rombouts F, Alexander R, Spurlino J, Van Gool M, Vega JA, Trabanco AA. Tresadern G, et al. Among authors: vega ja. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7255-60. doi: 10.1016/j.bmcl.2011.10.050. Epub 2011 Oct 20. Bioorg Med Chem Lett. 2011. PMID: 22071305
Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.
Tresadern G, Cid JM, Macdonald GJ, Vega JA, de Lucas AI, García A, Matesanz E, Linares ML, Oehlrich D, Lavreysen H, Biesmans I, Trabanco AA. Tresadern G, et al. Among authors: vega ja. Bioorg Med Chem Lett. 2010 Jan 1;20(1):175-9. doi: 10.1016/j.bmcl.2009.11.008. Epub 2009 Nov 10. Bioorg Med Chem Lett. 2010. PMID: 19932615
Imidazo[1,2-a]pyridines: orally active positive allosteric modulators of the metabotropic glutamate 2 receptor.
Trabanco AA, Tresadern G, Macdonald GJ, Vega JA, de Lucas AI, Matesanz E, García A, Linares ML, Alonso de Diego SA, Alonso JM, Oehlrich D, Ahnaou A, Drinkenburg W, Mackie C, Andrés JI, Lavreysen H, Cid JM. Trabanco AA, et al. Among authors: vega ja. J Med Chem. 2012 Mar 22;55(6):2688-701. doi: 10.1021/jm201561r. Epub 2012 Mar 1. J Med Chem. 2012. PMID: 22352782
Discovery of 1,4-disubstituted 3-cyano-2-pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.
Cid JM, Duvey G, Tresadern G, Nhem V, Furnari R, Cluzeau P, Vega JA, de Lucas AI, Matesanz E, Alonso JM, Linares ML, Andrés JI, Poli SM, Lutjens R, Himogai H, Rocher JP, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Trabanco AA. Cid JM, et al. Among authors: vega ja. J Med Chem. 2012 Mar 8;55(5):2388-405. doi: 10.1021/jm2016864. Epub 2012 Feb 24. J Med Chem. 2012. PMID: 22364337
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. Cid JM, et al. Among authors: vega ja. J Med Chem. 2012 Oct 25;55(20):8770-89. doi: 10.1021/jm3010724. Epub 2012 Oct 16. J Med Chem. 2012. PMID: 23072213
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
Cid JM, Tresadern G, Duvey G, Lütjens R, Finn T, Rocher JP, Poli S, Vega JA, de Lucas AI, Matesanz E, Linares ML, Andrés JI, Alcazar J, Alonso JM, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA. Cid JM, et al. Among authors: vega ja. J Med Chem. 2014 Aug 14;57(15):6495-512. doi: 10.1021/jm500496m. Epub 2014 Jul 28. J Med Chem. 2014. PMID: 25032784
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
Cid JM, Tresadern G, Vega JA, de Lucas AI, Del Cerro A, Matesanz E, Linares ML, García A, Iturrino L, Pérez-Benito L, Macdonald GJ, Oehlrich D, Lavreysen H, Peeters L, Ceusters M, Ahnaou A, Drinkenburg W, Mackie C, Somers M, Trabanco AA. Cid JM, et al. Among authors: vega ja. J Med Chem. 2016 Sep 22;59(18):8495-507. doi: 10.1021/acs.jmedchem.6b00913. Epub 2016 Sep 9. J Med Chem. 2016. PMID: 27579727
391 results