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Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide).
Prat M, Fernández D, Buil MA, Crespo MI, Casals G, Ferrer M, Tort L, Castro J, Monleón JM, Gavaldà A, Miralpeix M, Ramos I, Doménech T, Vilella D, Antón F, Huerta JM, Espinosa S, López M, Sentellas S, González M, Albertí J, Segarra V, Cárdenas A, Beleta J, Ryder H. Prat M, et al. Among authors: beleta j. J Med Chem. 2009 Aug 27;52(16):5076-92. doi: 10.1021/jm900132z. J Med Chem. 2009. PMID: 19653626
Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
Vidal B, Nueda A, Esteve C, Domenech T, Benito S, Reinoso RF, Pont M, Calbet M, López R, Cadavid MI, Loza MI, Cárdenas A, Godessart N, Beleta J, Warrellow G, Ryder H. Vidal B, et al. Among authors: beleta j. J Med Chem. 2007 May 31;50(11):2732-6. doi: 10.1021/jm061333v. Epub 2007 May 1. J Med Chem. 2007. PMID: 17469811
Characterization of aclidinium bromide, a novel inhaled muscarinic antagonist, with long duration of action and a favorable pharmacological profile.
Gavaldà A, Miralpeix M, Ramos I, Otal R, Carreño C, Viñals M, Doménech T, Carcasona C, Reyes B, Vilella D, Gras J, Cortijo J, Morcillo E, Llenas J, Ryder H, Beleta J. Gavaldà A, et al. Among authors: beleta j. J Pharmacol Exp Ther. 2009 Nov;331(2):740-51. doi: 10.1124/jpet.109.151639. Epub 2009 Aug 26. J Pharmacol Exp Ther. 2009. PMID: 19710368 Free article.
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.
Prat M, Buil MA, Fernández MD, Castro J, Monleón JM, Tort L, Casals G, Ferrer M, Huerta JM, Espinosa S, López M, Segarra V, Gavaldà A, Miralpeix M, Ramos I, Vilella D, González M, Córdoba M, Cárdenas A, Antón F, Beleta J, Ryder H. Prat M, et al. Among authors: beleta j. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3457-61. doi: 10.1016/j.bmcl.2011.03.096. Epub 2011 Apr 3. Bioorg Med Chem Lett. 2011. PMID: 21524581
Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.
Taltavull J, Serrat J, Gràcia J, Gavaldà A, Córdoba M, Calama E, Montero JL, Andrés M, Miralpeix M, Vilella D, Hernández B, Beleta J, Ryder H, Pagès L. Taltavull J, et al. Among authors: beleta j. Eur J Med Chem. 2011 Oct;46(10):4946-56. doi: 10.1016/j.ejmech.2011.07.054. Epub 2011 Aug 5. Eur J Med Chem. 2011. PMID: 21871695
57 results