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Items: 1 to 50 of 73

1.

Novel Inhaled Pan-JAK Inhibitor, LAS194046, Reduces Allergen-Induced Airway Inflammation, Late Asthmatic Response, and pSTAT Activation in Brown Norway Rats.

Calbet M, Ramis I, Calama E, Carreño C, Paris S, Maldonado M, Orellana A, Calaf E, Pauta M, De Alba J, Bach J, Miralpeix M.

J Pharmacol Exp Ther. 2019 Aug;370(2):137-147. doi: 10.1124/jpet.119.256263. Epub 2019 May 13.

PMID:
31085698
2.

Pharmacological Profile of AZD8871 (LAS191351), a Novel Inhaled Dual M3 Receptor Antagonist/β 2-Adrenoceptor Agonist Molecule with Long-Lasting Effects and Favorable Safety Profile.

Aparici M, Carcasona C, Ramos I, Montero JL, Otal R, Ortiz JL, Cortijo J, Puig C, Vilella D, De Alba J, Doe C, Gavaldà A, Miralpeix M.

J Pharmacol Exp Ther. 2019 Jul;370(1):127-136. doi: 10.1124/jpet.118.255620. Epub 2019 May 13.

PMID:
31085697
3.

In vitro anti-inflammatory effects of AZD8999, a novel bifunctional muscarinic acetylcholine receptor antagonist /β2-adrenoceptor agonist (MABA) compound in neutrophils from COPD patients.

Milara J, Contreras S, de Diego A, Calbet M, Aparici M, Morcillo E, Miralpeix M, Cortijo J.

PLoS One. 2019 Jan 4;14(1):e0210188. doi: 10.1371/journal.pone.0210188. eCollection 2019.

4.

Discovery of a Novel Inhaled PI3Kδ Inhibitor for the Treatment of Respiratory Diseases.

Erra M, Taltavull J, Bernal FJ, Caturla JF, Carrascal M, Pagès L, Mir M, Espinosa S, Gràcia J, Domínguez M, Sabaté M, Paris S, Maldonado M, Hernández B, Bravo M, Calama E, Miralpeix M, Lehner MD, Calbet M.

J Med Chem. 2018 Nov 8;61(21):9551-9567. doi: 10.1021/acs.jmedchem.8b00873. Epub 2018 Oct 29.

PMID:
30351000
5.

PI3K, p38 and JAK/STAT signalling in bronchial tissue from patients with asthma following allergen challenge.

Southworth T, Mason S, Bell A, Ramis I, Calbet M, Domenech A, Prats N, Miralpeix M, Singh D.

Biomark Res. 2018 Apr 11;6:14. doi: 10.1186/s40364-018-0128-9. eCollection 2018.

6.

4-Amino-7,8-dihydro-1,6-naphthyridin-5(6 H)-ones as Inhaled Phosphodiesterase Type 4 (PDE4) Inhibitors: Structural Biology and Structure-Activity Relationships.

Roberts RS, Sevilla S, Ferrer M, Taltavull J, Hernández B, Segarra V, Gràcia J, Lehner MD, Gavaldà A, Andrés M, Cabedo J, Vilella D, Eichhorn P, Calama E, Carcasona C, Miralpeix M.

J Med Chem. 2018 Mar 22;61(6):2472-2489. doi: 10.1021/acs.jmedchem.7b01751. Epub 2018 Mar 13.

PMID:
29502405
7.

Application of a phenotypic drug discovery strategy to identify biological and chemical starting points for inhibition of TSLP production in lung epithelial cells.

Orellana A, García-González V, López R, Pascual-Guiral S, Lozoya E, Díaz J, Casals D, Barrena A, Paris S, Andrés M, Segarra V, Vilella D, Malhotra R, Eastwood P, Planagumà A, Miralpeix M, Nueda A.

PLoS One. 2018 Jan 10;13(1):e0189247. doi: 10.1371/journal.pone.0189247. eCollection 2018.

8.

Abediterol (LAS100977), an inhaled long-acting β2-adrenoceptor agonist, has a fast association rate and long residence time at receptor.

Ramos I, Aparici M, Letosa M, Puig C, Gavaldà A, Huerta JM, Espinosa S, Vilella D, Miralpeix M.

Eur J Pharmacol. 2018 Jan 15;819:89-97. doi: 10.1016/j.ejphar.2017.11.043. Epub 2017 Nov 26.

PMID:
29183838
9.

Pharmacological preclinical characterization of LAS190792, a novel inhaled bifunctional muscarinic receptor antagonist /β2-adrenoceptor agonist (MABA) molecule.

Aparici M, Carcasona C, Ramos I, Montero JL, Ortiz JL, Cortijo J, Puig C, Vilella D, Doe C, Gavaldà A, Miralpeix M.

Pulm Pharmacol Ther. 2017 Oct;46:1-10. doi: 10.1016/j.pupt.2017.07.003. Epub 2017 Jul 17.

PMID:
28729041
10.

Control of Neurotransmission by NaV1.7 in Human, Guinea Pig, and Mouse Airway Parasympathetic Nerves.

Kocmalova M, Kollarik M, Canning BJ, Ru F, Adam Herbstsomer R, Meeker S, Fonquerna S, Aparici M, Miralpeix M, Chi XX, Li B, Wilenkin B, McDermott J, Nisenbaum E, Krajewski JL, Undem BJ.

J Pharmacol Exp Ther. 2017 Apr;361(1):172-180. doi: 10.1124/jpet.116.238469. Epub 2017 Jan 30.

11.

Discovery of a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases.

Erra M, Taltavull J, Gréco A, Bernal FJ, Caturla JF, Gràcia J, Domínguez M, Sabaté M, Paris S, Soria S, Hernández B, Armengol C, Cabedo J, Bravo M, Calama E, Miralpeix M, Lehner MD.

ACS Med Chem Lett. 2016 Nov 30;8(1):118-123. doi: 10.1021/acsmedchemlett.6b00438. eCollection 2017 Jan 12.

12.

Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS.

Calama E, Ramis I, Domènech A, Carreño C, De Alba J, Prats N, Miralpeix M.

Pulm Pharmacol Ther. 2017 Apr;43:60-67. doi: 10.1016/j.pupt.2017.01.002. Epub 2017 Jan 10.

PMID:
28087469
13.

Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships.

Gràcia J, Buil MA, Castro J, Eichhorn P, Ferrer M, Gavaldà A, Hernández B, Segarra V, Lehner MD, Moreno I, Pagès L, Roberts RS, Serrat J, Sevilla S, Taltavull J, Andrés M, Cabedo J, Vilella D, Calama E, Carcasona C, Miralpeix M.

J Med Chem. 2016 Dec 8;59(23):10479-10497. Epub 2016 Nov 17.

PMID:
27933955
14.

Non-neuronal cholinergic system contributes to corticosteroid resistance in chronic obstructive pulmonary disease patients.

Milara J, Cervera A, de Diego A, Sanz C, Juan G, Gavaldà A, Miralpeix M, Morcillo E, Cortijo J.

Respir Res. 2016 Nov 8;17(1):145.

15.

Anti-inflammatory potential of PI3Kδ and JAK inhibitors in asthma patients.

Southworth T, Plumb J, Gupta V, Pearson J, Ramis I, Lehner MD, Miralpeix M, Singh D.

Respir Res. 2016 Oct 4;17(1):124.

16.

Pharmacological characterization of CRTh2 antagonist LAS191859: Long receptor residence time translates into long-lasting in vivo efficacy.

Calbet M, Andrés M, Armengol C, Bravo M, Eichhorn P, López R, García-González V, Roberts R, Miralpeix M.

Pharmacol Res. 2016 Sep;111:208-216. doi: 10.1016/j.phrs.2016.06.014. Epub 2016 Jun 16.

PMID:
27317944
17.

Transient receptor potential cation channel, subfamily V, member 4 and airway sensory afferent activation: Role of adenosine triphosphate.

Bonvini SJ, Birrell MA, Grace MS, Maher SA, Adcock JJ, Wortley MA, Dubuis E, Ching YM, Ford AP, Shala F, Miralpeix M, Tarrason G, Smith JA, Belvisi MG.

J Allergy Clin Immunol. 2016 Jul;138(1):249-261.e12. doi: 10.1016/j.jaci.2015.10.044. Epub 2016 Jan 11.

18.

In vitro and in vivo preclinical profile of abediterol (LAS100977), an inhaled long-acting β2-adrenoceptor agonist, compared with indacaterol, olodaterol and vilanterol.

Aparici M, Gavaldà A, Ramos I, Carcasona C, Otal R, Fernández-Blanco JA, Montero JL, García VM, López R, De Alba J, Doe C, Puig C, Vilella D, Miralpeix M.

Eur J Pharmacol. 2016 Jan 5;770:61-9. doi: 10.1016/j.ejphar.2015.11.053. Epub 2015 Dec 4.

PMID:
26656755
19.

Enhanced cough reflex in a model of bleomycin-induced lung fibrosis in guinea pigs.

Fernández-Blanco JA, Aguilera M, Domènech A, Tarrasón G, Prats N, Miralpeix M, De Alba J.

Clin Sci (Lond). 2015 Dec;129(12):1001-10. doi: 10.1042/CS20150302. Epub 2015 Aug 14.

PMID:
26275723
20.

Combined anti CXC receptors 1 and 2 therapy is a promising anti-inflammatory treatment for respiratory diseases by reducing neutrophil migration and activation.

Planagumà A, Domènech T, Pont M, Calama E, García-González V, López R, Aulí M, López M, Fonquerna S, Ramos I, de Alba J, Nueda A, Prats N, Segarra V, Miralpeix M, Lehner MD.

Pulm Pharmacol Ther. 2015 Oct;34:37-45. doi: 10.1016/j.pupt.2015.08.002. Epub 2015 Aug 10. Review.

PMID:
26271598
21.

Double-stranded RNA evokes exacerbation in a mouse model of corticosteroid refractory asthma.

De Alba J, Otal R, Calama E, Domenech A, Prats N, Gozzard N, Miralpeix M; U-BIOPRED consortium.

Clin Sci (Lond). 2015 Dec;129(11):973-87. doi: 10.1042/CS20150292. Epub 2015 Aug 5.

PMID:
26245201
22.

A novel inhaled Syk inhibitor blocks mast cell degranulation and early asthmatic response.

Ramis I, Otal R, Carreño C, Domènech A, Eichhorn P, Orellana A, Maldonado M, De Alba J, Prats N, Fernández JC, Vidal B, Miralpeix M.

Pharmacol Res. 2015 Sep;99:116-24. doi: 10.1016/j.phrs.2015.05.011. Epub 2015 Jun 4.

PMID:
26051661
23.

Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.

Prat M, Buil MA, Fernández MD, Tort L, Monleón JM, Casals G, Ferrer M, Castro J, Gavaldà A, Miralpeix M, Ramos I, Vilella D, Huerta JM, Espinosa S, Hernández B, Segarra V, Córdoba M.

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1736-1741. doi: 10.1016/j.bmcl.2015.02.065. Epub 2015 Mar 5.

PMID:
25800115
24.

Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.

Esteve C, González J, Gual S, Vidal L, Alzina S, Sentellas S, Jover I, Horrillo R, De Alba J, Miralpeix M, Tarrasón G, Vidal B.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1217-22. doi: 10.1016/j.bmcl.2015.01.063. Epub 2015 Feb 4.

PMID:
25690784
25.

The in vitro and in vivo profile of aclidinium bromide in comparison with glycopyrronium bromide.

Gavaldà A, Ramos I, Carcasona C, Calama E, Otal R, Montero JL, Sentellas S, Aparici M, Vilella D, Alberti J, Beleta J, Miralpeix M.

Pulm Pharmacol Ther. 2014 Aug;28(2):114-21. doi: 10.1016/j.pupt.2014.05.005. Epub 2014 Jun 10.

26.

Effects of aclidinium bromide in a cigarette smoke-exposed Guinea pig model of chronic obstructive pulmonary disease.

Domínguez-Fandos D, Ferrer E, Puig-Pey R, Carreño C, Prats N, Aparici M, Musri MM, Gavaldà A, Peinado VI, Miralpeix M, Barberà JA.

Am J Respir Cell Mol Biol. 2014 Feb;50(2):337-46. doi: 10.1165/rcmb.2013-0117OC.

PMID:
24032416
27.

Lack of activity of 15-epi-lipoxin A₄ on FPR2/ALX and CysLT1 receptors in interleukin-8-driven human neutrophil function.

Planagumà A, Domenech T, Jover I, Ramos I, Sentellas S, Malhotra R, Miralpeix M.

Clin Exp Immunol. 2013 Aug;173(2):298-309. doi: 10.1111/cei.12110.

28.

Aclidinium inhibits cigarette smoke-induced lung fibroblast-to-myofibroblast transition.

Milara J, Serrano A, Peiró T, Artigues E, Gavaldà A, Miralpeix M, Morcillo EJ, Cortijo J.

Eur Respir J. 2013 Jun;41(6):1264-74. doi: 10.1183/09031936.00017712. Epub 2012 Sep 27.

29.

Highly potent aminopyridines as Syk kinase inhibitors.

Castillo M, Forns P, Erra M, Mir M, López M, Maldonado M, Orellana A, Carreño C, Ramis I, Miralpeix M, Vidal B.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5419-23. doi: 10.1016/j.bmcl.2012.07.045. Epub 2012 Jul 20.

PMID:
22877633
30.

Pharmacological characterization of abediterol, a novel inhaled β(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models.

Aparici M, Gómez-Angelats M, Vilella D, Otal R, Carcasona C, Viñals M, Ramos I, Gavaldà A, De Alba J, Gras J, Cortijo J, Morcillo E, Puig C, Ryder H, Beleta J, Miralpeix M.

J Pharmacol Exp Ther. 2012 Aug;342(2):497-509. doi: 10.1124/jpet.112.193284. Epub 2012 May 15.

PMID:
22588259
31.

Pyrazine-based Syk kinase inhibitors.

Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreño C, Ramis I, López M, Miralpeix M, Vidal B.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2784-8. doi: 10.1016/j.bmcl.2012.02.087. Epub 2012 Mar 2.

PMID:
22425453
32.

Characterization of a model of tracheal plasma extravasation in passively sensitized rats using anti-allergic and anti-inflammatory drugs by oral and intratracheal route.

Carreño C, Domènech A, Prats N, Miralpeix M, Ramis I.

Pulm Pharmacol Ther. 2012 Feb;25(1):87-93. doi: 10.1016/j.pupt.2011.12.002. Epub 2011 Dec 22.

PMID:
22207135
33.

Aclidinium inhibits human lung fibroblast to myofibroblast transition.

Milara J, Serrano A, Peiró T, Gavaldà A, Miralpeix M, Morcillo EJ, Cortijo J.

Thorax. 2012 Mar;67(3):229-37. doi: 10.1136/thoraxjnl-2011-200376. Epub 2011 Sep 28.

34.

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.

Eur J Med Chem. 2011 Oct;46(10):4946-56. doi: 10.1016/j.ejmech.2011.07.054. Epub 2011 Aug 5.

PMID:
21871695
35.

Inhaled muscarinic antagonists for respiratory diseases: a review of patents and current developments (2006 - 2010).

Prat M, Gavaldà A, Fonquerna S, Miralpeix M.

Expert Opin Ther Pat. 2011 Oct;21(10):1543-73. doi: 10.1517/13543776.2011.596528. Epub 2011 Jun 25. Review.

PMID:
21702714
36.

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.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3457-61. doi: 10.1016/j.bmcl.2011.03.096. Epub 2011 Apr 3.

PMID:
21524581
37.

Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist.

Eastwood P, Esteve C, González J, Fonquerna S, Aiguadé J, Carranco I, Doménech T, Aparici M, Miralpeix M, Albertí J, Córdoba M, Fernández R, Pont M, Godessart N, Prats N, Loza MI, Cadavid MI, Nueda A, Vidal B.

ACS Med Chem Lett. 2010 Dec 20;2(3):213-8. doi: 10.1021/ml100249e. eCollection 2011 Mar 10.

38.

Discovery of substituted phenyl urea derivatives as novel long-acting β2-adrenoreceptor agonists.

Pérez D, Crespo M, Solé L, Prat M, Carcasona C, Calama E, Otal R, Gavaldá A, Gómez-Angelats M, Miralpeix M, Puig C.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1545-8. doi: 10.1016/j.bmcl.2010.12.096. Epub 2011 Jan 6.

PMID:
21277205
39.

Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.

Taltavull J, Serrat J, Gràcia J, Gavaldà A, Andrés M, Córdoba M, Miralpeix M, Vilella D, Beleta J, Ryder H, Pagès L.

J Med Chem. 2010 Oct 14;53(19):6912-22. doi: 10.1021/jm100524j.

PMID:
20825218
40.

Aclidinium inhibits cholinergic and tobacco smoke-induced MUC5AC in human airways.

Cortijo J, Mata M, Milara J, Donet E, Gavaldà A, Miralpeix M, Morcillo EJ.

Eur Respir J. 2011 Feb;37(2):244-54. doi: 10.1183/09031936.00182009. Epub 2010 Jun 4.

41.

Aclidinium bromide, a new, long-acting, inhaled muscarinic antagonist: in vitro plasma inactivation and pharmacological activity of its main metabolites.

Sentellas S, Ramos I, Albertí J, Salvà M, Antón F, Miralpeix M, Beleta J, Gavaldà A.

Eur J Pharm Sci. 2010 Mar 18;39(5):283-90. doi: 10.1016/j.ejps.2010.01.004. Epub 2010 Jan 20. Review.

PMID:
20093184
42.

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.

J Pharmacol Exp Ther. 2009 Nov;331(2):740-51. doi: 10.1124/jpet.109.151639. Epub 2009 Aug 26.

PMID:
19710368
43.

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.

J Med Chem. 2009 Aug 27;52(16):5076-92. doi: 10.1021/jm900132z.

PMID:
19653626
44.

Synthesis and structure-activity relationships of gamma-carboline derivatives as potent and selective cysLT(1) antagonists.

Bonjoch J, Diaba F, Pagès L, Pérez D, Soca L, Miralpeix M, Vilella D, Anton P, Puig C.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4299-302. doi: 10.1016/j.bmcl.2009.05.094. Epub 2009 May 27.

PMID:
19505824
45.

A new chemical tool (C0036E08) supports the role of adenosine A(2B) receptors in mediating human mast cell activation.

Buceta M, Domínguez E, Castro M, Brea J, Alvarez D, Barcala J, Valdés L, Alvarez-Calderón P, Domínguez F, Vidal B, Díaz JL, Miralpeix M, Beleta J, Cadavid MI, Loza MI.

Biochem Pharmacol. 2008 Oct 1;76(7):912-21. doi: 10.1016/j.bcp.2008.07.011. Epub 2008 Jul 19.

PMID:
18687311
46.

Therapeutic targeting of CCR1 attenuates established chronic fungal asthma in mice.

Carpenter KJ, Ewing JL, Schuh JM, Ness TL, Kunkel SL, Aparici M, Miralpeix M, Hogaboam CM.

Br J Pharmacol. 2005 Aug;145(8):1160-72.

47.

Combinatorial approaches towards the discovery of new tryptase inhibitors.

del Fresno M, Fernández-Forner D, Miralpeix M, Segarra V, Ryder H, Royo M, Albericio F.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1659-64.

PMID:
15745817
48.

Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.

Fonquerna S, Miralpeix M, Pagès L, Puig C, Cardús A, Antón F, Vilella D, Aparici M, Prieto J, Warrellow G, Beleta J, Ryder H.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1165-7.

PMID:
15686934
49.

Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.

Fonquerna S, Miralpeix M, Pagès L, Puig C, Cardús A, Antón F, Cárdenas A, Vilella D, Aparici M, Calaf E, Prieto J, Gras J, Huerta JM, Warrellow G, Beleta J, Ryder H.

J Med Chem. 2004 Dec 2;47(25):6326-37.

PMID:
15566302
50.

Differential expression of SAP and EAT-2-binding leukocyte cell-surface molecules CD84, CD150 (SLAM), CD229 (Ly9) and CD244 (2B4).

Romero X, Benítez D, March S, Vilella R, Miralpeix M, Engel P.

Tissue Antigens. 2004 Aug;64(2):132-44.

PMID:
15245368

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