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US 2013/0210850 A1Published application
Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation
AssigneeBoehringer Ingelheim International GmbH
InventorsThomas TRIESELMANN, Dieter HAMPRECHT, Holger WAGNER
Life of this patent
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Abstract
The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this protein.
Claims20
A compound of formula I
- wherein
- R1 is a mono- or bicyclic 5- to 10-membered aryl or heteroaryl group, which heteroaryl contains 1 to 4 heteroatoms selected from the group consisting of N, O and S, and which aryl or heteroaryl may optionally be substituted by R9, R10 and/or R11, in which
- R9 is hydrogen, halogen, cyano, 1-4C-alkyl, 2-4C-alkenyl, 3-6C-cycloalkyl, 1-4C-alkoxy, completely or partially fluorine-substituted 1-4C-alkyl, completely or partially fluorine-substituted 1-4C-alkoxy, pentafluorosulfanyl, cyano-1-4C-alkyl, 1-2C-alkyl-3-6C-cycloalkyl, cyano-3-6C-cycloalkyl, 1-2C-alkoxy-1-4C-alkyl, hydroxy-1-4C-alkyl or 3-(1-2C-alkyl)-oxetan-3-yl,
- R10 is hydrogen, halogen, cyano, 1-4C-alkyl, 2-4C-alkenyl, 3-6C-cycloalkyl, 1-4C-alkoxy, completely or partially fluorine-substituted 1-4C-alkyl, completely or partially fluorine-substituted 1-4C-alkoxy, cyano-1-4C-alkyl, methyl-3-6C-cycloalkyl, cyano-3-6C-cycloalkyl, methoxy-1-4C-alkyl, hydroxy-1-4C-alkyl or 3-(1-2C-alkyl)-oxetan-3-yl,
- R11 is hydrogen or halogen,
- or R9 and R10 together and with inclusion of the carbon atoms, to which they are attached, form a 5-6C-cycloalkane ring wherein one methylene group may optionally be replaced by oxygen,
- which ring, for the case of 6-membered ring system, may optionally contain a double bond, and/or
- which ring may optionally be mono- or disubstituted by methyl, wherein, for the case that both methyl groups are connected to the same carbon, the methyl groups together with the carbon to which they are connected, may optionally form a cyclopropyl ring,
- R2 is 1-6C-alkyl, 1-3C-perfluoroalkyl, 1-4C-alkoxy-1-4C-alkyl, or 4-7C-cycloalkyl, which 4-7C-cycloalkyl may optionally be mono- or disubstituted by fluorine, hydroxy, methoxy and/or 1-2C-alkyl and in which, for the case of 5-7C-cycloalkyl systems, one methylene group may optionally be replaced by oxygen,
- R3 and R4 together and with inclusion of the carbon atom, to which they are attached, form a 3-7C-cycloalkane ring,
- R5 is hydrogen or 1-4C-alkyl,
- R6 is 1-4C-alkyl,
- R7 is hydrogen or 1-4C-alkyl,
- or R6 and R7 together and with inclusion of the carbon atom, to which they are attached, form a 5-7C-cycloalkane ring wherein one methylene group may optionally be replaced by oxygen,
- which ring may optionally contain one double bond, and/or
- which ring may optionally be mono- or disubstituted by fluorine, hydroxyl, 1-2C-alkoxy and/or 1-2C-alkyl,
- R8 is hydrogen, acetoxy, propionyloxy, methoxy or hydroxy,
- the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof.
15 more elements
Dependencies are inferred from the claim text.