Výsledky vyhledávání - "Josep M, Huerta"

Abediterol (LAS100977), an inhaled long-acting β 2 -adrenoceptor agonist, has a fast association rate and long residence time at receptor

Autor: Josep M. Huerta, Montserrat Miralpeix, Sonia Espinosa, Dolors Vilella, Carlos Puig, Israel Ramos, Amadeu Gavaldà, Mònica Aparici, Maria Letosa

Publikováno v: European Journal of Pharmacology. 819:89-97

This study describes the association rate and residence time of abediterol, a novel long-acting β2-adrenoceptor agonist (LABA) in Phase II development for treatment of asthma and COPD, in comparison with indacaterol, olodaterol, vilanterol and salme

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a48c87c835e4e873e031a05acca8f8d6
https://doi.org/10.1016/j.ejphar.2017.11.043

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Setup and validation of shake-flask procedures for the determination of partition coefficients (logD) from low drug amounts

Autor: Elisabeth Bosch, Axel Andrés, Sonia Espinosa, Victor Segarra, Josep M. Huerta, Clara Ràfols, Martí Rosés

Publikováno v: Recercat. Dipósit de la Recerca de Catalunya
instname
Dipòsit Digital de la UB
Universidad de Barcelona

Several procedures based on the shake-flask method and designed to require a minimum amount of drug for octanol-water partition coefficient determination have been established and developed. The procedures have been validated by a 28 substance set wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73c796e662de7085999a350ed689533a
https://doi.org/10.1016/j.ejps.2015.05.008

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

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:1736-1741

Novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides have been identified as potent M3 muscarinic antagonists with a long duration of action in an in vivo model of bronchoconstriction. The synthesis, structure-activity relationships and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::430af71f81dd784dd8e3710b416eebc5
https://doi.org/10.1016/j.bmcl.2015.02.065

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Design, Synthesis, and Structure−Activity Relationships of Aminopyridine N-Oxides, a Novel Scaffold for the Potent and Selective Inhibition of p38 Mitogen Activated Protein Kinase

Autor: María Domínguez, Laura Vidal, Wenceslao Lumeras, Nuria Godessart, Adelina Orellana, Cristina Balagué, Cristina Esteve, Ramón Roca, Bernat Vidal, Francisco Caturla, Josep M. Huerta

Publikováno v: Journal of Medicinal Chemistry. 52:5531-5545

A novel series of aminopyridine N-oxides were designed, synthesized, and tested for their ability to inhibit p38alpha MAP kinase. Some of these compounds showed a significant reduction in the LPS-induced TNFalpha production in human whole blood. Stru

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b495cfd7a1b917e7dc4356e7516bb008
https://doi.org/10.1021/jm9008604

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Synthesis and Structure−Activity Relationships of Novel Histamine H1 Antagonists: Indolylpiperidinyl Benzoic Acid Derivatives

Autor: Carles Puig, Jordi Gras, Elena Calaf, Arantxa Cardús, Lluís Pagès, Jorge Beleta, Montse Miralpeix, Francisca Antón, Graham Warrellow, Hamish Ryder, José Prieto, Alvaro Cardenas, Mònica Aparici, Silvia Fonquerna, Josep M. Huerta, Dolors Vilella

Publikováno v: Journal of Medicinal Chemistry. 47:6326-6337

A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H(1) antagonists. Structure-activity relationship studies were directed toward improving in vivo activity and pharmacokinetic profile of our first

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3f2efad3e23777d79ac1bd1d2cbd9dd
https://doi.org/10.1021/jm0498203

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Solid-phase syntheses of N-substituted carbamates. Reaction monitoring by gel-phase 13C NMR using a 13C enriched BAL-linker

Autor: Manel Ferrer, Dolors Fernández-Forner, Ernest Giralt, Hamish Ryder, Fernando Albericio, Josep M. Huerta, Gaspar Casals

Publikováno v: Tetrahedron Letters. 43:3543-3546

The solid-phase synthesis of N -substituted carbamates using the tris(alkoxy)benzyl (BAL) resin is reported. The incorporation of the primary amine was carried out by reductive amination, which was followed by reaction with an alkyl succinimidyl carb

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b55d12ee488da1ee29286fb1ef09a093
https://doi.org/10.1016/s0040-4039(02)00564-6

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Synthesis and Biological Evaluation of 3,4-Diaryloxazolones: A New Class of Orally Active Cyclooxygenase-2 Inhibitors

Autor: Victor Segarra, MA López, Montserrat Miralpeix, Josep M. Huerta, Ascensión Heredia, Ignasi Cardelús, Jaume Puig, José Palacios, Hamish Ryder, Nuria Godessart, María I. Crespo, Carles Puig, Joan Feixas, Javier Ibarzo, Jordi Beleta, Juan-Miguel Jimenez, Lidia Soca

Publikováno v: Journal of Medicinal Chemistry. 43:214-223

A series of 3,4-diaryloxazolones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure-activity relationship work was carried out within this series, and a number of potent and selective COX-2 inhibito

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca626049f8539d7e9df6e5860f497ce5
https://doi.org/10.1021/jm991106b

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Strategies to improve lung absorption of intratracheally administered compounds in Drug Discovery

Autor: Isabel Ramis, Sonia Espinosa, Peter Eichhorn, Josep M. Huerta, Elena Calama, Jorge De Alba, Montserrat Vives, Juan Pérez

Publikováno v: Journal of Inflammation (London, England)

The key factors governing the absorption of drugs from the lungs are deposition pattern, dissolution rate, solubility and permeability. Whereas the thin epithelium in the respiratory airways is generally considered to constitute a minor barrier in th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83b7b54c9042244e26f1a371708c6c4f
https://doi.org/10.1186/1476-9255-10-s1-p35

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