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US 2003/0166655 A1Published application
Tetrahydrothiopy ranphthalazinone derivatives as PDE4 inhibitors
AssigneeAltana Pharma AG
InventorGeert Jan Sterk
Life of this patent
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Abstract
The compounds of formula (I) in which R1, R2, A and Ar have the meanings as given in the description are novel effective PDE4 inhibitors.
Claims10
Compounds of formula I
- 15
- in which
- R1 and R2 are both hydrogen or together form an additional bond,
- A represents S (sulfur), S(O) (sulfoxide) or S(O)2 (sulfone),
- Ar represents a benzene derivative of formula (a) or (b)
- 16
- wherein
- R3 is halogen, 1-4C-alkoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine,
- R4 is halogen, 1-8C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine,
- R5 is halogen, 1-4C-alkoxy, 3-5C-cycloalkoxy, 3-5C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine,
- R6 is 1-4C-alkyl and
- R7 is hydrogen or 1-4C-alkyl,
- or wherein
- R6 and R7 together and with inclusion of the two carbon atoms, to which they are bonded, form a spiro-linked 5-, 6- or 7-membered hydrocarbon ring, optionally interrupted by an oxygen or sulphur atom,
- and the salts of these compounds, with the proviso, that those compounds of formula I are excluded, in which A represents S (sulfur) and Ar represents a benzene derivative of formula (a) and both of R3 and R4 are other than halogen.
12 more elements
Dependencies are inferred from the claim text.