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Generated: June 23, 2017

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Claims for Patent: 7,056,916

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Claims for Patent: 7,056,916

Title:Medicaments for the treatment of chronic obstructive pulmonary disease
Abstract: A pharmaceutical composition comprising a compound of formula 1 ##STR00001## wherein: n is 1 or 2; R.sup.1 is hydrogen, C.sub.1 C.sub.4-alkyl, halogen, OH, or --O--C.sub.1 C.sub.4-alkyl; R.sup.2 is hydrogen, C.sub.1 C.sub.4-alkyl, halogen, OH, or --O--C.sub.1 C.sub.4-alkyl; R.sup.3 is hydrogen, C.sub.1 C.sub.4-alkyl, OH, halogen, --O--C.sub.1 C.sub.4-alkyl, --O--C.sub.1 C.sub.4-alkylene-COOH, or --O--C.sub.1 C.sub.4-alkylene-CO--O--C.sub.1 C.sub.4-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).
Inventor(s): Konetzki; Ingo (Warthausen, DE), Schromm; Kurt (Ingelheim am Rhein, DE), Schollenberger; Hermann (Ingelheim am Rhein, DE), Pestel; Sabine (Biberach, DE), Schnapp; Andreas (Biberach, DE), Bouyssou; Thierry (Mietingen, DE), Buettner; Frank (Ummendorf, DE), Heine; Claudia (Biberach, DE), Lustenberger; Philipp (Warthausen, DE), Hoenke; Christoph (Ingelheim, DE), Rudolf; Klaus (Warthausen, DE)
Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG (Ingelheim, DE)
Application Number:10/705,012
Patent Claims: 1. A compound of formula 1 ##STR00026## wherein: n is 1; R.sup.1 is hydrogen, halogen, C.sub.1 C.sub.4-alkyl, or --O--C.sub.1 C.sub.4-alkyl; R.sup.2 is hydrogen, halogen, C.sub.1 C.sub.4-alkyl or --O--C.sub.1 C.sub.4-alkyl; R.sup.3 is C.sub.1 C.sub.4-alkyl, halogen, --O--C.sub.1 C.sub.4-alkyl, --O--C.sub.1 C.sub.4-alkylene-COOH, or --O--C.sub.1 C.sub.4-alkylene-CO--O--C.sub.1 C.sub.4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

2. The compound of formula 1 according to claim 1, wherein R.sup.3 is methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH.sub.2--COOmethyl, or --O--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

3. The compound of formula 1 according to claim 1, wherein: R.sup.1 is hydrogen, fluorine, chlorine, methyl, or methoxy; R.sup.2 is hydrogen, fluorine, chlorine, methyl, or methoxy; R.sup.3 is C.sub.1 C.sub.4-alkyl, fluorine, chlorine, bromine, --O--C.sub.1 C.sub.4-alkyl, --O--C.sub.1 C.sub.4-alkylene-COOH, or --O--C.sub.1 C.sub.4-alkylene-CO--O--C.sub.1 C.sub.4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

4. The compound of formula 1 according to claim 3, wherein R.sup.3 is methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH.sub.2--COOmethyl, or --O--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

5. The compound of formula 1 according to claim 1, wherein: R.sup.1 is hydrogen or C.sub.1 C.sub.4-alkyl; R.sup.2 is hydrogen or C.sub.1 C.sub.4-alkyl; and R.sup.3 is C.sub.1 C.sub.4-alkyl, --O--C.sub.1 C.sub.4-alkyl, --O--C.sub.1 C.sub.4-alkylene-COOH, or --O--C.sub.1 C.sub.4-alkylene-CO--O--C.sub.1 C.sub.4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

6. The compound of formula 1 according to claim 5, wherein R.sup.3 is methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH.sub.2--COOmethyl, or --O--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

7. The compound of formula 1 according to claim 1, wherein: R.sup.1 is hydrogen, methyl, or ethyl; R.sup.2 is hydrogen, methyl, or ethyl; R.sup.3 is methyl, ethyl, methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH2--COOmethyl or --O--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

8. The compound of formula 1 according to claim 7, wherein R.sup.3 is methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH.sub.2--COOmethyl, or --O--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

9. The compound of formula 1 according to claim 1, wherein: R.sup.1 is halogen, C.sub.1 C.sub.4-alkyl, or --O--C.sub.1 C.sub.4-alkyl; R.sup.2 is halogen, C.sub.1 C.sub.4-alkyl, or --O--C.sub.1 C.sub.4-alkyl; and R.sup.3 is halogen, C.sub.1 C.sub.4-alkyl, or --O--C.sub.1 C.sub.4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

10. The compound of formula 1 according to claim 9, wherein: R.sup.1 is fluorine, chlorine, methyl, or methoxy; R.sup.2 is fluorine, chlorine, methyl, or methoxy; and R.sup.3 is fluorine, chlorine, methyl, or methoxy, or an acid addition salt thereof with a pharmacologically acceptable acid.

11. The compound of formula 1 according to claim 1, wherein: R.sup.1 is hydrogen; R.sup.2 is hydrogen, fluorine, chlorine, or methyl; and R.sup.3 is methyl, ethyl, isopropyl, tert-butyl, fluorine, chlorine, bromine, methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH.sub.2--CH.sub.2--COOH, --O--CH.sub.2--CH.sub.2--CH.sub.2--COOH, --O--CH.sub.2--COOmethyl, --O--CH.sub.2--COOethyl, --O--CH.sub.2--CH.sub.2--COOmethyl, --O--CH.sub.2--CH.sub.2--COOethyl, --O--CH.sub.2--CH.sub.2--CH.sub.2--COOmethyl, or --O--CH.sub.2--CH.sub.2--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

12. The compound of formula 1 according to claim 11, wherein: R.sup.1 is hydrogen; R.sup.2 is hydrogen, fluorine, chlorine, or methyl; and R.sup.3 is fluorine, chlorine, methyl, methoxy, ethoxy, or --O--CH.sub.2--COOH, or an acid addition salt thereof with a pharmacologically acceptable acid.

13. The compound of formula 1 according to claim 1, wherein: R.sup.1 and R.sup.2 are each hydrogen; and R.sup.3 is methyl, ethyl, isopropyl, tert-butyl, fluorine, chlorine, bromine, methoxy, ethoxy, --O--CH.sub.2--COOH, --O--CH.sub.2--CH.sub.2--COOH, --O--CH.sub.2--CH.sub.2--CH.sub.2--COOH, --O--CH.sub.2--COOmethyl, --O--CH.sub.2--COOethyl, --O--CH.sub.2--CH.sub.2--COOmethyl, --O--CH.sub.2--CH.sub.2--COOethyl, --O--CH.sub.2--CH.sub.2--CH.sub.2--COOmethyl, or --O--CH.sub.2--CH.sub.2--CH.sub.2--COOethyl, or an acid addition salt thereof with a pharmacologically acceptable acid.

14. The compound of formula 1 according to claim 13, wherein R.sup.3 is OH, fluorine, chlorine, methoxy, ethoxy, or --O--CH.sub.2--COOH, or an acid addition salt thereof with a pharmacologically acceptable acid.

15. The compound of formula 1 according to claim 14, wherein R.sup.3 is fluorine, chlorine, methoxy, or ethoxy, or an acid addition salt thereof with a pharmacologically acceptable acid.

16. The compound of formula 1 according to claim 1, wherein: R.sup.1 is hydrogen, halogen, C.sub.1 C.sub.4-alkyl, or --OC1 C4-alkyl; and R.sup.2 is hydrogen, halogen, C.sub.1 C.sub.4-alkyl, or --O--C.sub.1 C.sub.4-alkyl; or an acid addition salt thereof with a pharmacologically acceptable acid.

17. The compound of formula 1 according to claim 16, wherein: R.sup.1 is hydrogen, fluorine, chlorine, methyl or methoxy; and R.sup.2 is hydrogen, fluorine, chlorine, methyl or methoxy, or an acid addition salt thereof with a pharmacologically acceptable acid.

18. A compound of formula 1 according to claim 6 selected from: (1) 6-hydroxy-8-{1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethylethylamino]ethy- l}-4H-benzo[1,4]oxazin-3-one; (2) 6-hydroxy-8-{1-hydroxy-2-[2-(4-phenoxyethylacetate)-1,1-dimethylethylamin- o]-ethyl}-4H-benzo[1,4]oxazin-3-one; (3) 6-hydroxy-8-{1-hydroxy-2-[2-(4-phenoxyacetic acid)-1,1-dimethylethylamino]-ethyl}-4H-benzo[1,4]oxazin-3-one; (4) 8-{2-[1,1-dimethyl-2-(2,4,6-trimethylphenyl)ethylamino]-1-hydroxyethyl}-6- -hydroxy-4H-benzo[1,4]oxazin-3-one; (5) 6-hydroxy-8-{1-hydroxy-2-[2-(4-hydroxyphenyl)-1,1-dimethylethylamino]ethy- l}-4H-benzo[1,4]oxazin-3-one; (6) 6-hydroxy-8-{1-hydroxy-2-[2-(4-isopropylphenyl)-1,1 dimethylethylamino]ethyl}-4H-benzo[1,4]oxazin-3-one; (7) 8-{2-[2-(4-ethylphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hydroxy- -4H-benzo[1,4]oxazin-3-one; (8) 8-{2-[2-(4-fluoro-3-methylphenyl)-1, 1-dimethylethylamino]-1-hydroxyethyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one- ; (9) 8-{2-[2-(4-fluoro-2-methylphenyl)-1,1-dimethylethylamino]-1-hydroxye- thyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one; (10) 8-{2-[2-(2,4-difluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hy- droxy-4H-benzo[1,4]oxazin-3-one; (11) 8-{2-[2-(3,5-difluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hy- droxy-4H-benzo[1,4]oxazin-3-one; (12) 8-{2-[2-(4-ethoxyphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hydrox- y-4H-benzo[1,4]oxazin-3-one; (13) 8-{2-[2-(3,5-dimethylphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hy- droxy-4H-benzo[1,4]oxazin-3-one; (14) 4-(4-{2-[2-hydroxy-2-(6-hydroxy-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-8-y- l)-ethylamino]-2-methylpropyl}phenoxy)butyric acid; (15) 8-{2-[2-(3,4-difluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hy- droxy-4H-benzo[1,4]oxazin-3-one; (16) 8-{2-[2-(2-chloro-4-fluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}- -6-hydroxy-4H-benzo[1,4]oxazin-3-one; (17) 8-{2-[2-(4-chlorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hydrox- y-4H-benzo[1,4]oxazin-3-one; (18) 8-{2-[2-(4-bromophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hydroxy- -4H-benzo[1,4]oxazin-3-one; (19) 8-{2-[2-(4-fluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hydrox- y-4H-benzo[1,4]oxazin-3-one; (20) 8-{2-[2-(4-fluoro-3-methoxyphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl- }-6-hydroxy-4H-benzo[1,4]oxazin-3-one; (21) 8-{2-[2-(4-fluoro-2,6-dimethylphenyl)-1,1-dimethylethylamino]-1-hydroxyet- hyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one; (22) 8-{2-[2-(4-chloro-2-methylphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}- -6-hydroxy-4H-benzo[1,4]oxazin-3-one; (23) 8-{2-[2-(4-chloro-3-fluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}- -6-hydroxy-4H-benzo[1,4]oxazin-3-one; (24) 8-{2-[2-(4-chloro-2-fluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}- -6-hydroxy-4H-benzo-[1,4]oxazin-3-one; (25) 8-{2-[2-(3-chloro-4-fluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}- -6-hydroxy-4H-benzo[1,4]oxazin-3-one; (26) 8-{2-[2-(2,6-difluoro-4-methoxyphenyl)-1,1-dimethylethylamino]-1-hydroxye- thyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one; (27) 8-{2-[2-(2,5-difluoro-4-methoxyphenyl)-1,1-dimethylethylamino]-1-hydroxye- thyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one; (28) 8-{2-[2-(4-fluoro-3,5-dimethylphenyl)-1,1-dimethylethylamino]-1-hydroxyet- hyl}-6-hydroxy-4H-benzo[1,4]oxazin-3-one; (29) 8-{2-[2-(3,5-dichlorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hy- droxy-4H-benzo[1,4]oxazin-3-one; (30) 8-{2-[2-(4-chloro-3-methylphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}- -6-hydroxy-4H-benzo[1,4]oxazin-3-one; (31) 8-{2-[2-(3,4,5-trifluorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6- -hydroxy-4H-benzo[1,4]oxazin-3-one; (32) 8-{2-[2-(3-methylphenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hydrox- y-4H-benzo[1,4]oxazin-3-one; and (33) 8-{2-[2-(3,4-dichlorophenyl)-1,1-dimethylethylamino]-1-hydroxyethyl}-6-hy- droxy-4H-benzo[1,4]oxazin-3-one, or an acid addition salt thereof with a pharmacologically acceptable acid.

19. A pharmaceutical composition comprising a compound of formula 1 according to one of claims 1 to 18, or an acid addition salt thereof with a pharmacologically acceptable acid, and a pharmaceutically acceptable excipient or carrier.

20. The pharmaceutical composition according to claim 19, wherein the pharmaceutical composition is an inhalable powder, propellant-containing metered-dose aerosol, or propellant-free inhalable solution.
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