Medicaments for the treatment of chronic obstructive pulmonary disease

• US 8,044,046 B2
• Filed: 05/18/2005
• Issued: 10/25/2011
• Est. Priority Date: 11/15/2002
• Status: Expired due to Term

• Current Assignee: Boehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Hoenke, Christoph, Heine, Claudia, Pestel, Sabine, Buettner, Frank, Schromm, Kurt, Schollenberger, Hermann, Lustenberger, Philipp, Konetzki, Ingo, Rudolf, Klaus, Bouyssou, Thierry, Schnapp, Andreas
• Primary Examiner(s): HABTE, KAHSAY
• Application Number:
  US11/132,075
• Publication Number:
  US 20050222144A1
• Time in Patent Office: 2,351 Days
• Field of Search: 514/230.5
• US Class Current: 514/230.5
• CPC Class Codes: A61K 31/535 having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• CPC Class Codes: A61K 31/538 ortho- or peri-condensed with carbocyclic ring systems
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: C07D 265/36 condensed with one six-membered ring

Abstract

A pharmaceutical composition comprising a compound of formula 1

wherein:

• n is 1 or 2;
• R¹ is hydrogen, C₁-C₄-alkyl, halogen, OH, or —O—C₁-C₄-alkyl;
• R² is hydrogen, C₁-C₄-alkyl, halogen, OH, or —O—C₁-C₄-alkyl;
• R³ is hydrogen, C₁-C₄-alkyl, OH, halogen, —O—C₁-C₄-alkyl, —O—C₁-C₄-alkylene-COOH, or —O—C₁-C₄-alkylene-CO—O—C₁-C₄-alkyl, or
  an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and
  a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).

Claims

1. A method for the treatment of Chronic Obstructive Pulmonary Disease (COPD) comprising administration of a therapeutically effective amount of R-6-Hydroxy-8-{1-hydroxy-2[2-(4-methoxy-phenyl)-1,1-dimethyl-ethylamino]-ethyl}-4H-benzo[1,4]oxazin-3-one, or an acid addition salt thereof with a pharmacologically acceptable acid;

and

a pharmaceutically acceptable excipient or carrier.

2. A method for the treatment of Chronic Obstructive Pulmonary Disease (COPD) comprising administration of a therapeutically effective amount of R-8-{2-[2-(2,4-difluorophenyl)-1,1-dimethyl-ethylamino]-1-hydroxy-ethyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one, or an acid addition salt thereof with a pharmacologically acceptable acid;

and

a pharmaceutically acceptable excipient or carrier.

3. A method for the treatment of Chronic Obstructive Pulmonary Disease (COPD) comprising administration of a therapeutically effective amount of R-8-{2-[2-(3,5-difluorophenyl)-1,1-dimethyl-ethylamino]-1-hydroxy-ethyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one, or an acid addition salt thereof with a pharmacologically acceptable acid;

and

a pharmaceutically acceptable excipient or carrier.

4. A method for the treatment of Chronic Obstructive Pulmonary Disease (COPD) comprising administration of a therapeutically effective amount of R-8-{2-[2-(4-Ethoxy-phenyl)-1,1-dimethyl-ethylamino]-1-hydroxy-ethyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one, or an acid addition salt thereof with a pharmacologically acceptable acid;

and

a pharmaceutically acceptable excipient or carrier.

5. A method for the treatment of Chronic Obstructive Pulmonary Disease (COPD) comprising administration of a therapeutically effective amount of R-8-{2-[2-(4-fluorophenyl)-1,1-dimethyl-ethylamino]-1-hydroxy-ethyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one, or an acid addition salt thereof with a pharmacologically acceptable acid;

and

a pharmaceutically acceptable excipient or carrier.