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Page 1
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: mackie c. 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
Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.
Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Conde-Ceide S, et al. Among authors: mackie c. ACS Med Chem Lett. 2015 May 20;6(6):716-20. doi: 10.1021/acsmedchemlett.5b00181. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26157544 Free PMC article.
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Zhou Y, et al. Among authors: mackie c. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3515-9. doi: 10.1016/j.bmcl.2015.06.096. Epub 2015 Jul 4. Bioorg Med Chem Lett. 2015. PMID: 26183084 Free PMC article.
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.
Malosh C, Turlington M, Bridges TM, Rook JM, Noetzel MJ, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martínez-Viturro CM, Piedrafita M, Sánchez-Casado MR, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Malosh C, et al. Among authors: mackie c. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5115-20. doi: 10.1016/j.bmcl.2015.10.009. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26475522 Free PMC article.
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Lindsley CW, Bartolomé-Nebreda JM. Conde-Ceide S, et al. Among authors: mackie c. Bioorg Med Chem Lett. 2016 Jan 15;26(2):429-434. doi: 10.1016/j.bmcl.2015.11.098. Epub 2015 Nov 28. Bioorg Med Chem Lett. 2016. PMID: 26684851 Free PMC article.
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: mackie c. 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: mackie c. 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: mackie c. J Med Chem. 2012 Oct 25;55(20):8770-89. doi: 10.1021/jm3010724. Epub 2012 Oct 16. J Med Chem. 2012. PMID: 23072213
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.
Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, Weaver CD, Lindsley CW, Niswender CM, Jones CK, Conn PJ, Rombouts F, Lavreysen H, Macdonald GJ, Mackie C, Steckler T. Bartolomé-Nebreda JM, et al. Among authors: mackie c. J Med Chem. 2013 Sep 26;56(18):7243-59. doi: 10.1021/jm400650w. Epub 2013 Sep 4. J Med Chem. 2013. PMID: 23947773 Free PMC article.
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.
Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Among authors: mackie c. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2. Bioorg Med Chem Lett. 2014. PMID: 24961642 Free PMC article.
223 results