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)

Abstract

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.

Keywords::

• asthma
• chronic obstructive pulmonary disease
• crystalline form
• glucocorticoid receptor
• inhaled therapy
• steroid
• transrepression