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US 2006/0040933 A1Published application
Nonsteroidal antiinflammatory agents
AssigneeSchering Corporation
InventorsStefan Jaroch, Manfred Lehmann, Norbert Schmees, Bernd Buchmann, Harmur Rehwinkel, Peter Droescher, Werner Skuballa, Konrad Krolikiewicz, Hartwig Hennekes, Heike Schaecke, Arndr Schottelius
Life of this patent
Estimating the term…
Abstract
are useful in the treatment of inflammation.
Claims28
1-8. (canceled)
A compound of formula I
- wherein
- R1 and R2 are the same or different and stand for a hydrogen atom, a C1-C5 alkyl group, or, together with the C-atom of the chain, stand for a ring with a total of 3-7 links;
- R3 is a straight-chain or branched C1-C5 alkyl group or a straight-chain or branched, partially or completely fluorinated C1-C5 alkyl group;
- A stands for the group
- wherein the dashed line means the interface site;
- R4 is methyl, nitro, amino, acetylamino, or mesylamino;
- R5, R6, and R8 are the same or different from one another and are each a hydrogen atom, a halogen atom, a cyano group, a nitro group, a COOR9 group, a CONR10 group, or an NHR11 group, a straight-chain or branched C1-C5 alkyl group, a straight-chain or branched C2-C5 alkenyl group, a straight-chain or branched C2-C5 alkinyl group, a straight-chain or branched C1-C5 alkyl group that is partially or completely substituted by fluorine atoms, a C1-C5 acyl group, an aryl radical or a heteroaryl radical;
- R7 is halogen;
- R9 is a hydrogen atom, a straight-chain or branched C1-C5 alkyl group or a benzyl group;
- R10 is a hydrogen atom or a straight-chain or branched C1-C5 alkyl group;
- R11 is a hydrogen atom, a straight-chain or branched C1-C5 alkyl group, a straight-chain or branched, partially or completely fluorinated C1-C5 alkyl group, a C1-C5 acyl group, an —SO2—(C1-C5) alkyl group or an —SO2-phenyl group that is optionally substituted by halogen or a C1-C5 alkyl group;
- Ar is the ring system
- X3a and X3b are the same or different and are each a hydrogen atom, a straight-chain or branched C1-C5 alkyl group, or a straight-chain or branched, partially or completely fluorinated C1-C5 alkyl group;
- and
- X4, X6, and X7 are the same or different and are each a hydrogen atom, a straight-chain or branched C1-C5 alkyl group, a straight-chain or branched, partially or completely fluorinated C1-C5 alkyl group, a halogen atom, a hydroxy group, a C1-C5 alkoxy group or a C1-C5 alkanoyloxy group;
- and
- physiologically compatible salts thereof, wherein said compound can also be in the form of a racemate or in the form of separate stereoisomers.
14 more elements
A compound selected from the following compounds:
- 5-[4-(5-fluoro-2-methylphenyl)-2-hydroxy-4-methyl-2-trifluoromethylvaleroylamino]-phthalide;
- 5-[4-(5-fluoro-2-nitrophenyl)-2-hydroxy-4-methyl-2-trifluoromethylvaleroylamino]-phthalide;
- 5-[4-(3-fluoro-4-nitrophenyl)-2-hydroxy-4-methyl-2-trifluoromethylvaleroylamino]-phthalide;
- 5-[4-(2-amino-5-fluorophenyl)-2-hydroxy-4-methyl-2-trifluoromethylvaleroyl-amino]-phthalide;
- (−) 5-[4-(2-amino-5-fluorophenyl)-2-hydroxy-4-methyl-2-trifluoromethylvaleroyl-amino]-phthalide;
- (+) 5-[4-(2-amino-5-fluorophenyl)-2-hydroxy-4-methyl-2-trifluoromethylvaleroyl-amino]-phthalide;
- 5-[4-(2-acetylamino-5-fluorophenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-valeroylamino]-phthalide;
- (−) 5-[4-(2-acetylamino-5-fluorophenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-valeroylamino]-phthalide;
- (+) 5-[4-(2-acetylamino-5-fluorophenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-valeroylamino]-phthalide;
- 5-[4-(5-fluoro-2-mesylaminophenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-valeroylamino]-phthalide;
- (−) 5-[4-(5-fluoro-2-mesylaminophenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-valeroylamino]-phthalide;
- (+) 5-[4-(5-fluoro-2-mesylaminophenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-valeroylamino]-phthalide;
- and
- physiologically compatible salts thereof.
11 more elements
Dependencies are inferred from the claim text.