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Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
Bartolomé-Nebreda JM, Delgado F, Martín-Martín ML, Martínez-Viturro CM, Pastor J, Tong HM, Iturrino L, Macdonald GJ, Sanderson W, Megens A, Langlois X, Somers M, Vanhoof G, Conde-Ceide S. Bartolomé-Nebreda JM, et al. J Med Chem. 2014 May 22;57(10):4196-212. doi: 10.1021/jm500073h. Epub 2014 May 9. J Med Chem. 2014. PMID: 24758746
Identification of a novel orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor with efficacy in animal models of schizophrenia.
Bartolomé-Nebreda JM, Alonso de Diego SA, Artola M, Delgado F, Delgado Ó, Martín-Martín ML, Martínez-Viturro CM, Pena MÁ, Tong HM, Van Gool M, Alonso JM, Fontana A, Macdonald GJ, Megens A, Langlois X, Somers M, Vanhoof G, Conde-Ceide S. Bartolomé-Nebreda JM, et al. J Med Chem. 2015 Jan 22;58(2):978-93. doi: 10.1021/jm501651a. Epub 2015 Jan 12. J Med Chem. 2015. PMID: 25495129
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. 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
Diazaspirononane Nonsaccharide Inhibitors of O-GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders.
Martínez-Viturro CM, Trabanco AA, Royes J, Fernández E, Tresadern G, Vega JA, Del Cerro A, Delgado F, García Molina A, Tovar F, Shaffer P, Ebneth A, Bretteville A, Mertens L, Somers M, Alonso JM, Bartolomé-Nebreda JM. Martínez-Viturro CM, et al. J Med Chem. 2020 Nov 25;63(22):14017-14044. doi: 10.1021/acs.jmedchem.0c01479. Epub 2020 Nov 16. J Med Chem. 2020. PMID: 33197187
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
Andrés JI, Alonso JM, Díaz A, Fernández J, Iturrino L, Martínez P, Matesanz E, Freyne EJ, Deroose F, Boeckx G, Petit D, Diels G, Megens A, Somers M, Van Wauwe J, Stoppie P, Cools M, De Clerck F, Peeters D, de Chaffoy D. Andrés JI, et al. Bioorg Med Chem Lett. 2002 Feb 25;12(4):653-8. doi: 10.1016/s0960-894x(01)00817-4. Bioorg Med Chem Lett. 2002. PMID: 11844693
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