- Benzoxazine compound and its preparation methods and application
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The invention relates to a benzoxazine compound represented in the following formula 1. The benzoxazine compound can serve as a beta 2 receptor agonist. The formula can be seen from the description.
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Paragraph 0093; 0096; 0097
(2017/10/07)
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- Synthesis and structure-activity relationships of long-acting β2 adrenergic receptor agonists incorporating metabolic inactivation: An antedrug approach
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A series of saligenin β2 adrenoceptor agonist antedrugs having high clearance were prepared by reacting a protected saligenin oxazolidinone with protected hydroxyethoxyalkoxyalkyl bromides, followed by removal of the hydroxy-protecting group, alkylation, and final deprotection. The compounds were screened for β2, β1, and β3 agonist activity in CHO cells. The onset and duration of action in vitro of selected compounds were assessed on isolated superfused guinea pig trachea. Compound 13f had high potency, selectivity, fast onset, and long duration of action in vitro and was found to have long duration in vivo, low oral bioavailability in the rat, and to be rapidly metabolized. Crystalline salts of 13f (vilanterol) were identified that had suitable properties for inhaled administration. A proposed binding mode for 13f to the β2-receptor is presented.
- Procopiou, Panayiotis A.,Barrett, Victoria J.,Bevan, Nicola J.,Biggadike, Keith,Box, Philip C.,Butchers, Peter R.,Coe, Diane M.,Conroy, Richard,Emmons, Amanda,Ford, Alison J.,Holmes, Duncan S.,Horsley, Helen,Kerr, Fern,Li-Kwai-Cheung, Anne-Marie,Looker, Brian E.,Mann, Inderjit S.,McLay, Iain M.,Morrison, Valerie S.,Mutch, Peter J.,Smith, Claire E.,Tomlin, Paula
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supporting information; experimental part
p. 4522 - 4530
(2010/08/07)
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- DERIVATIVES OF 4-(2-AMINO-1-HYDROXIETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR
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This invention is directed to compounds of formula (I): to pharmaceutical compositions comprising them; to combination products comprising them; and to their use in therapy.
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Page/Page column 21
(2008/06/13)
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