Napadisylate salt of 5-(2--1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as agonist of the beta 2 adrenergic receptor

a technology of napadisylate salt and beta 2 adrenergic receptor, which is applied in the field of crystalline naphthalene1 and 5disulfonic acid salts, can solve problems such as difficult to obtain, and achieve the effect of high melting poin
US20100093681A1Active Publication Date: 2010-04-15ALMIRALL
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Patent Information

Authority / Receiving Office
US ยท United States
Patent Type
Applications(United States)
Current Assignee / Owner
ALMIRALL
Publication Date
2010-04-15

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Abstract

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.
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Description

FIELD OF THE INVENTION

[0001] The present invention is directed to novel crystalline naphthalene-1,5-disulfonic acid salts (napadisylates) of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, its enantiomers and solvates thereof. The invention is also directed to pharmaceutical compositions comprising the crystalline salts, methods of using them to treat respiratory diseases associated with ฮฒ2 adrenergic receptor activity, and processes and intermediates useful for preparing such salts.BACKGROUND OF THE INVENTION

[0002] ฮฒ2 adrenergic receptor agonists are advantageously administered directly into the respiratory tract by inhalation when used for treating pulmonary or respiratory disorders. Several types of pharmaceutical inhalation devices have been developed for administering therapeutic agents by inhalation including dry powder inhalers (DPI), metered-dose inhalers (MDI) and nebulizer inhalers. It is highly desirable to have a crystalline ...

Claims

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