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US 6,306,869 B1Granted
N-oxides
AssigneeByk Gulden Lomberg Chemische Febrik GmbH
InventorDieter Flockerzi
Life of this patent
Estimating the term…
Abstract
N-oxides of formula 1 wherein R1, R2, R3 and R4 have the meanings given in the description, are selective inhibitors of types 3 and 4 of cyclic nucleotide phosphodiesterase (PDE3, PDE4); they are useful on the one hand as bronchial therapeutics but on the other hand especially for the treatment of disorders of inflammatory nature.
Claims10
A compound of formula 1
- in which
- R1 is 1-4C-alkyl,
- R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or 1-4C-alkoxy in which the hydrogen atoms are completely or predominantly replaced by fluorine,
- R3 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkymethoxy or 1-4C-alkoxy in which the hydrogen atoms are completely or predominantly replaced by fluorine,
- or in which
- R2 and R3 together are a 1-2C-alkanedioxy group,
- R4 is a phenyl radical which is substituted by R5 and R6, where
- R5 is hydrogen, hydroxyl, halogen, nitro, 1-4C-alkyl, trifluoromethyl or 1-4C-alkoxy,
- R6 is CO—R7 or CO—R8, where
- R7 is hydroxyl, 1-8C-alkoxy, 3-7C-cycloalkoxy or 3-7C-cycloalkylmethoxy and
- R8 is N(R81)R82, where R81 and R82 independently of one another are hydrogen, 1-7C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkylmethyl, or where R81 and R82, together and including the nitrogen atom to which both are bonded, are a 1-pyrrolidinyl, 1-piperidyl, 1-hexahydroazepinyl or 4-morpholinyl radical,
- or a salt thereof.
9 more elements
Dependencies are inferred from the claim text.