51131-55-6Relevant academic research and scientific papers
A multivalent approach to the discovery of long-acting β2- adrenoceptor agonists for the treatment of asthma and COPD
Jacobsen, John R.,Choi, Seok Ki,Combs, Jesse,Fournier, Eric J.L.,Klein, Uwe,Pfeiffer, Juergen W.,Thomas, G. Roger,Yu, Cecile,Moran, Edmund J.
scheme or table, p. 1213 - 1218 (2012/03/11)
A multivalent approach was applied to the design of long-acting inhaled β2-adrenoceptor agonists. A series of dimeric arylethanolamines based on the short acting β2-adrenoceptor agonist albuterol were prepared, varying the nature and length of the linker between the basic nitrogens. None of the C2-symmetric dimers demonstrated increased potency, however dimer 5j, derived from 4-phenethylamine, was found to have increased binding potency in vitro relative to the parent monomer. Optimization of this structure led to the identification of 22 (milveterol) which demonstrates high potency in vitro and long duration of action in a guinea pig model of bronchoprotection.
CCR10 ANTAGONISTS
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Page/Page column 79, (2009/05/28)
The invention relates to a compound of formula (I) or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.
Aryl aniline derivatives as beta2 adrenergic receptor agonists
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Page/Page column 19, (2008/06/13)
The invention provides novel β2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2 adrenergic
Carbostyril Derivatives Having Potent β-Adrenergic Agonist Properties
Milecki, Jan,Baker, Stephen P.,Standifer, Kelly M.,Ishizu, Takashi,Chida, Yasuhiro,et al.
, p. 1563 - 1566 (2007/10/02)
Derivatives carrying a substituent in the para position of the phenyl group of 8-hydroxy-5--1-hydroxyethyl>carbostyril (10) were prepared and their effects on β-adrenoceptors evaluated in vitro.Unsubstituted compound
Cu2+/BH4- REDUCTION SYSTEM: SYNTHETIC UTILITY AND MODE OF ACTION
Cowan, J. A.
, p. 1205 - 1208 (2007/10/02)
Cu2+/BH4- offers a mild, method of reduction for aromatic and aliphatic tertiary nitro groups.Its mode of action has been studied, in comparison with related reagents, by deuterium isotope experiments.
Synthesis and irreversible β-adrenergic blockade with a bromoacetamido derivative of betaxolol
Amlaiky,Leclerc
, p. 1117 - 1119 (2007/10/02)
1-[4-(2-Cyclopropylmethoxyethyl)phenoxyl]-3-[1-p-(bromoacetamidophenyl)-2 -methyl-2-propylamine]-2-propanol (8), which is a derivatve of the β1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent β-adrenergic blocking act
Synthesis and characterization of iodoazidobenzylpindolol
Rashidbaigi,Ruoho
, p. 305 - 307 (2007/10/02)
A high affinity β-adrenergic ligand, iodoazidobenzylpindolol, was synthesized and characterized. The absorption spectrum of this compound changed markedly upon photolysis consistent with decomposition of the azide group. This compound has a K(D) of 5-7 x 10-10M for the duck erythrocyte ghost β-adrenergic receptor when measured in a competitive binding assay.
Cycloaliphatic unsymmetrical diamines
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, (2008/06/13)
Novel cycloaliphatic diamines have been prepared which are consisting of two unequivalent amine groups. The diamines are prepared by reduction of aromatic dinitro compounds. The polyamides made from these diamines are useful in forming fibers and films ha
