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US 2009/0105327 A1Published application
Dibenzocycloheptane compounds and pharmaceuticals containing these compounds
AssigneeMerckle GmbH
InventorsStefan Laufer, Wolfgang Albrecht, Cornelia Greim, Hans-Guenter Striegel, Karola Tollmann
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Abstract
The present invention relates to compounds of the formula I in which R1, R2, R3, R4, X and Y have the meanings indicated in the description. These compounds have immunomodulating effects, as well as an inhibiting or regulating effect on the release of IL-1β and/or TNF-α. They can therefore be used for the treatment of diseases associated with a disturbance of the immune system.
Claims17
A dibenzocycloheptane compound of the formula I
- in which
- one of the ring atoms X and Y is CH2 and the other is CH2, O, S, SO, SO2 or NR5;
- or —X—Y— is —CH2—CH2— or —CH═CH—;
- R1 is H or C1-C6-alkyl;
- R2 is H, halogen or C1-C4-alkyl-C≡C— which is optionally substituted by an amino group;
- R3 is selected from:
- R4 is H, halogen or C1-C6-alkyl, or R3 and R4 are bonded to adjacent C atoms of the phenyl ring and form together with these C atoms a 5- or 6-membered aromatic or nonaromatic heterocycle having a nitrogen heteroatom, where the heterocycle may be substituted by one or two C1-C6-alkyl groups or may be fused to a cyclohexyl group;
- R5 is H or C1-C6-alkyl;
- R6 is H or C1-C6-alkyl;
- R7 is selected from:
- H,
- NH2,
- mono-C1-C6-alkylamino,
- di-C1-C6-alkylamino,
- C1-C6-alkyl-CONH—,
- C1-C6-alkyl-NHCONH—,
- C1-C6-alkyl-O—CO—NH—,
- C1-C6-alkyl,
- C1-C6-alkoxy,
- NO2 or
- halogen;
- R8 is H, NH2, mono-C1-C6-alkylamino, di-C1-C6-alkylamino, C1-C6-alkoxy, or halogen;
- R9 is H or NH2;
- and the physiologically tolerated salts and the solvates of the compounds and of the salts thereof.
21 more elements
Dependencies are inferred from the claim text.