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US 7,405,236 B2Granted
Indole derivatives comprising an acetylene group
AssigneeHoffman-La Roche Inc.
InventorsJean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer
Life of this patent
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Abstract
This invention is directed to compounds of the formula (I): wherein one of R6, R7, R8 and R9 is and X, R1 to R12, m, n and o are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention is also directed to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARδ and/or PPARα agonists.
Claims25
A compound of the formula (I):
- wherein:
- R1 is hydrogen or C1-7-alkyl;
- R2 and R3 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl and C1-7-alkyl-C1-7-alkoxy;
- R4 and R5 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halogen, C1-7-alkoxy-C1-7-alkyl, C2-7-alkenyl, C2-7-alkinyl, fluoro-C1-7-alkyl, fluoro-C1-7-alkoxy, cyano-C1-7-alkyl and cyano;
- R6, R7, R8 and R9 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halogen, C1-7-alkoxy-C1-7-alkyl, C2-7-alkenyl, C2-7-alkinyl, fluoro-C1-7-alkyl, fluoro-C1-7-alkoxy, cyano-C1-7-alkyl and cyano;
- and one of R6, R7, R8 and R9 is
- wherein:
- X is selected from the group consisting of S, O, NR13, (CH2)pNR13CO and (CH2)pCONR13,
- R13 is selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, fluoro-C1-7-alkyl, hydroxy-C2-7-alkyl and C1-7-alkoxy-C2-7-alkyl;
- R10 is selected from the group consisting of C1-7-alkyl, C3-7-cycloalkyl, fluoro-C1-7-aklyl and C1-7-alkoxy-C1-7-alkyl;
- R11 is selected from the group consisting of hydrogen, C1-7-alkyl and C1-7-alkoxy-C1-7-alkyl;
- or R10 and R11 together with the carbon atom they are attached to form a C3-6-cycloalkyl ring;
- R12 is aryl or heteroaryl;
- m, o, p is 0, 1 or 2;
- n is 0, 1, 2 or 3 and the sum of m, n and o is 1 to 5;
- and
- pharmaceutically acceptable salts and/or esters thereof.
14 more elements
Dependencies are inferred from the claim text.