Almirall, S.a.

Enrique Moyes Valls

Iolanda Marchueta Hereu

Carlos Puig Duran

Francesc Carrera Carrera

Gemma Amat Mestres

Elvira Balaguer Ardanuy

Lolanda Marchueta Hereu

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 &#x3b2;2 adrenergic receptor activity and a process for preparing such polymorphic crystal forms.

Polymorphic crystal forms of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, heminapadisytlate as agonist of the &#x3b2;2 adrenergic receptor

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. 

Process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one via a novel intermediate

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 &#x3b2;2 receptor.

Mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]jamino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as agonist of the &#x3b2;2 adrenergic receptor

A process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, 

Process for manufacturing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one

The present disclosure relates to crystalline monoapadisylate and/or heminapadisylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, and pharmaceutically acceptable solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the crystalline monoapadisylate and/or heminapadisylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, and to methods of treatment comprising these pharmaceutical compositions.

Napadisylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as agonist of the &#x3b2;2 adrenergic receptor

Growing community of inventors

Barcelona, Spain

Enrique Moyes Valls