Novel polymorphic crystal forms of 5-(2-{ [6-(2,2-difluoro-2-phenylethoxy)hexyl]amino} -1-(r)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one, heminapadisylate as agonist of the &bgr;2 adrenergic receptor.

摘要

Provided are polymorphic forms of 5-(2-{ [6-(2,2-difluoro-2-phenylethoxy)hexyl]amino} -1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one heminapadisylate. One of the forms is a hydrate polymorph characterised by an XRPD pattern with peaks at 13.3, 16.1 and 19.2 degrees 2&thetas; (± 0.1 degrees 2&thetas;) and a DSC trace which shows a first endotherm in the range 75-120 °C (± 5 °C ) and a second endotherm with an onset at 190 °C (± 1 °C ). The other form is a type beta polymorph characterised by an XRPD pattern with a peak at 19.1 degrees 2&thetas; (±0.1 degrees 2&thetas;) and a DSC trace which shows an endotherm with an onset at 190 °C (± 1 °C). The compound is a beta2 adrenergic receptor agonist useful in the treatment of respiratory disorders.