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US 2006/0189645 A1Published application
Novel 6-phenylphenantridines
AssigneeAltana Pharma AG
InventorBeate Schmidt
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R7 and R8 have the meanings indicated in the description, are novel effective PDE4 inhibitors.
Claims11
Compounds of the formula I,
- in which
- R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy,
- R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy,
- or in which R1 and R2 together are a 1-2C-alkylenedioxy group,
- R3 is hydrogen or 1-4C-alkyl,
- R31 is hydrogen or 1-4C-alkyl,
- or in which R3 and R31 together are a 1-4C alkylene group,
- R4 is hydrogen or 1-4C-alkyl,
- R5 is hydrogen,
- R51 is hydrogen,
- or in which R5 and R51 together represent an additional bond,
- R6 is hydrogen, halogen, nitro, 1-4C-alkyl, trifluoromethyl or 1-4-C-alkoxy,
- R7 is 1-4C-alkyl, 3-7C-cycloalkyl, 3-7C-cycloalkylmethyl, pyridinyl, phenyl or R71- and/or R72-substituted phenyl, wherein
- R71 is halogen, hydroxyl, cyano, trifluoromethyl, carboxyl, nitro, 1-4C-alkyl or 1-4C-alkoxy,
- R72 is 1-4C-alkoxy,
- R8 is 1-4C-alkyl, hydroxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, amino, C(O)N(H)R9, phenyl, HetA, aryl-1-4C-alkyl, HetB-1-4C-alkyl, cyano-1-4C-alkyl, 1-4C-alkoxycarbonyl-1-4C-alkyl or R14- and/or R15- and/or R16-substituted phenyl, wherein
- R9 is hydrogen, phenyl or R91- and/or R92-substituted phenyl, wherein
- R91 is halogen, 1-4C-alkyl, 1-4C-alkoxy, nitro, trifluoromethyl or completely or predominantly fluorine-substituted 1-4C-alkoxy,
- R92 is halogen or 1-4C-alkoxy,
- HetA is an unsubstituted or R10- and/or R11-substituted heteroaryl radical which is selected from the group consisting of pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl and pyridazinyl, wherein
- R10 is 1-4C-alkyl, phenyl, halogen or trifluoromethyl,
- R11 is 1-4C-alkyl,
- aryl is phenyl or R12- and/or R13-substituted phenyl, wherein
- R12 is 1-4C-alkyl, 1-4C-alkoxy, halogen, nitro or hydroxyl,
- R13 is 1-4C-alkoxy or halogen,
- HetB is an unsubstituted or R12- and/or R13-substituted indolyl radical,
- R14 is 1-4C-alkyl, trifluoromethyl, 1-4C-alkoxy, halogen, nitro, hydroxyl, amino, mono- or di-1-4C-alkylamino or completely or predominantly fluorine-substituted 1-4C-alkoxy,
- R15 is 1-4C-alkyl, 1-4C-alkoxy, halogen or completely or predominantly fluorine-substituted 1-4C-alkoxy,
- R16 is 1-4C-alkoxy,
- and the salts and the E/Z isomers of these compounds.
27 more elements
Dependencies are inferred from the claim text.