Crystalline forms of 2,2,2-trifluoro-N-[(1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)-2-propanyl]acetamide (AZD-5423)

被引:4
作者
Norman, Peter [1 ]
机构
[1] Norman Consulting, Burnham SL1 8JW, Bucks, England
关键词
asthma; chronic obstructive pulmonary disease; crystalline form; glucocorticoid receptor; inhaled therapy; steroid; transrepression; GLUCOCORTICOID-RECEPTOR AGONIST; CORTICOSTEROIDS; DESIGN;
D O I
10.1517/13543776.2013.820706
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A crystalline form (form B) of the novel glucocorticoid receptor agonist 2,2,2-trifluoro-N-[(1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)-2-propanyl]acetamide (AZD-5423) and its use alone or in combination for the treatment of asthma and chronic obstructive pulmonary disease are claimed. This form of AZD-5423 is better absorbed than Form A drug after inhalation. Two effective large-scale syntheses of AZD-5423 are described.
引用
收藏
页码:1239 / 1245
页数:7
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