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Page 1
Enantiomerically pure tetrahydroquinoline derivatives as in vivo potent antagonists of the glycine binding site associated to the NMDA receptor.
Di Fabio R, Tranquillini E, Bertani B, Alvaro G, Micheli F, Sabbatini F, Pizzi MD, Pentassuglia G, Pasquarello A, Messeri T, Donati D, Ratti E, Arban R, Dal Forno G, Reggiani A, Barnaby RJ. Di Fabio R, et al. Among authors: alvaro g. Bioorg Med Chem Lett. 2003 Nov 3;13(21):3863-6. doi: 10.1016/j.bmcl.2003.06.001. Bioorg Med Chem Lett. 2003. PMID: 14552796
Chiral tetrahydroquinoline derivatives as potent anti-hyperalgesic agents in animal models of sustained inflammation and chronic neuropathic pain.
Di Fabio R, Alvaro G, Bertani B, Donati D, Pizzi DM, Gentile G, Pentassuglia G, Giacobbe S, Spada S, Ratti E, Corsi M, Quartaroli M, Barnaby RJ, Vitulli G. Di Fabio R, et al. Among authors: alvaro g. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1176-80. doi: 10.1016/j.bmcl.2006.12.022. Epub 2006 Dec 12. Bioorg Med Chem Lett. 2007. PMID: 17218099
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
Di Fabio R, Griffante C, Alvaro G, Pentassuglia G, Pizzi DA, Donati D, Rossi T, Guercio G, Mattioli M, Cimarosti Z, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M. Di Fabio R, et al. Among authors: alvaro g. J Med Chem. 2009 May 28;52(10):3238-47. doi: 10.1021/jm900023b. J Med Chem. 2009. PMID: 19388677
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Sabbatini FM, Di Fabio R, Griffante C, Pentassuglia G, Zonzini L, Melotto S, Alvaro G, Capelli AM, Pippo L, Perdona' E, St Denis Y, Costa S, Corsi M. Sabbatini FM, et al. Among authors: alvaro g. Bioorg Med Chem Lett. 2010 Jan 15;20(2):623-7. doi: 10.1016/j.bmcl.2009.11.078. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 19963378
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Di Fabio R, Alvaro G, Griffante C, Pizzi DA, Donati D, Mattioli M, Cimarosti Z, Guercio G, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M. Di Fabio R, et al. Among authors: alvaro g. J Med Chem. 2011 Feb 24;54(4):1071-9. doi: 10.1021/jm1013264. Epub 2011 Jan 13. J Med Chem. 2011. PMID: 21229983
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Di Fabio R, Alvaro G, Braggio S, Carletti R, Gerrard PA, Griffante C, Marchioro C, Pozzan A, Melotto S, Poffe A, Piccoli L, Ratti E, Tranquillini E, Trower M, Spada S, Corsi M. Di Fabio R, et al. Among authors: alvaro g. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73. doi: 10.1016/j.bmc.2013.09.001. Epub 2013 Sep 11. Bioorg Med Chem. 2013. PMID: 24075145
79 results