Abstract: The present invention is directed to novel polymorphic crystal forms of a 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, heminapadisylate. The invention is also directed to pharmaceutical compositions comprising said polymorphic crystal forms, methods of using them to treat respiratory diseases associated with ?2 adrenergic receptor activity and a process for preparing such polymorphic crystal forms.

Abstract: The present invention is concerned with a process for preparing 5-(2{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.

Abstract: The present invention is concerned with a process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure relates to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 receptor.

Abstract: A process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, which process comprises: a) reacting, in a xylene solvent, a compound of formula (V) having P1 and P2 protecting groups, with a compound of formula (IV), to give a compound of formula (III); and b) effecting a P1 deprotection step and a P2 deprotection step to give a compound of formula (I); and optionally c) preparing a pharmaceutically acceptable salt of a compound of formula (I); wherein the compounds of formulas III, IV, and V are described in the specification.

Abstract: A process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, which process comprises: a) reacting, in a xylene solvent, a compound of formula (V) having P1 and P2 protecting groups, with a compound of formula (IV), to give a compound of formula (III); and b) effecting a P1 deprotection step and a P2 deprotection step to give a compound of formula (I); and optionally c) preparing a pharmaceutically acceptable salt of a compound of formula (I); wherein the compounds of formulas III, IV, and V are described in the specification.

Abstract: The present disclosure relates to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 receptor.

Abstract: A process for preparing 3-methyl-4-phenylisoxazolo[3,4-d]pyridazin-7(6H)-one which process comprises the steps of: (a) reacting 1-phenylbutane-1,3-dione with ethyl 2-chloro-2-(hydroxyimino)actetate; and (b) subsequently reacting the product from step (a) with hydrazine or an hydrate thereof to yield 3-methyl-4-phenylisoxazolo-[3,4-d]pyridin-7(6H)-one, wherein step (b) is carried out on the mixture resulting from step (a) without isolating ethyl 4-benzoyl-5-methylisoxazole-3-carboxylate therefrom.