title: 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.
authors.affiliation: Norman Consulting, 18 Pink Lane, Burnham, Bucks, SL1 8JW, UK. peter.norman2@btinternet.com
authors.forename: Peter
authors.initials: P
authors.lastname: Norman
mesh_terms: D000081:Acetamides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000280:Administration, Inhalation; D000818:Animals; D001249:Asthma / Q000188:drug therapy*; D003460:Crystallization; D006801:Humans; D007191:Indazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D010330:Patents as Topic; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy*; D011965:Receptors, Glucocorticoid / Q000819:agonists*
chemical_list: C587250:2,2,2-trifluoro-N-(1-((1-(4-fluorophenyl)-1H-indazol-5-yl)oxy)-1-(3-methoxyphenyl)-2-propanyl)acetamide; D000081:Acetamides; D007191:Indazoles; D011965:Receptors, Glucocorticoid