Výsledky vyhledávání - "Gaspar, Casals"

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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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)

Publikováno v: Journal of Medicinal Chemistry. 52:5076-5092

The objective of this work was to discover a novel, long-acting muscarinic M3 antagonist for the inhaled treatment of chronic obstructive pulmonary disease (COPD), with a potentially improved risk−benefit profile compared with current antimuscarini

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::45428bc44e0992b58d50d3c5f07d6aa2
https://doi.org/10.1021/jm900132z

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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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Solid-phase synthesis of 4-aminopiperidine analogues using the Alloc protecting group: an investigation of Alloc removal from secondary amines

Autor: Gaspar Casals, Fernando Albericio, Dolors Fernández-Forner, Hamish Ryder, Eloı́sa Navarro

Publikováno v: Tetrahedron Letters. 42:4471-4474

A useful method for Alloc removal from secondary amines on solid-phase has been optimised. The use of Me2NH·BH3 (40 equiv., 40 min) as scavenger of the allyl cations in a palladium-catalysed process with Pd[PPh3]4 leads to quantitative removal of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2af620b84410abf93c68afb5e8094d67
https://doi.org/10.1016/s0040-4039(01)00755-9

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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)

Publikováno v: Journal of medicinal chemistry. 52(16)

The objective of this work was to discover a novel, long-acting muscarinic M(3) antagonist for the inhaled treatment of chronic obstructive pulmonary disease (COPD), with a potentially improved risk-benefit profile compared with current antimuscarini

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::d0fa685f586051a3b9bc091198b8f22d
https://pubmed.ncbi.nlm.nih.gov/19653626

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