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US 2008/0167355 A1Published application
Benzooxazol-2-one derivatives as lipase and phospholipase inhibitors
AssigneeSanofi-Aventis
InventorsGerhard ZOLLER, Stefan PETRY, Gunter MULLER, Hubert HEUER, Norbert TENNAGELS
Life of this patent
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Abstract
The invention relates to benzooxazol-2-one derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances.
Claims24
A compound of the formula I
- wherein
- R1 is (C5-C16)-alkyl, (C1-C4)-alkylene-(C6-C10)-aryl, (C1-C4)-alkylene-(C5-C12)-heteroaryl, (C1-C4)-alkylene-(C3-C12)-cycloalkyl, (C8-C14)-bicycle, where aryl, heteroaryl, cycloalkyl or bicycle may be substituted one or more times by halogen, (C1-C6)-alkyl, (C1-C3)-alkyloxy, hydroxy, (C1-C6)-alkylmercapto, amino, (C1-C6)-alkylamino, di-(C2-C12)-alkylamino, mono-(C1-C6)-alkylaminocarbonyl, di-(C2-C8)-alkylaminocarbonyl, (C1-C6)-alkoxycarbonyl, (C1-C6)-alkylcarbonyl, cyano, trifluoromethyl, trifluoromethyloxy, (C1-C6)-alkylsulfonyl or aminosulfonyl;
- R2 is hydrogen or (C1-C6)-alkyl;
- or
- R1 and R2 form together with the nitrogen atom bearing them a monocyclic, saturated or partially unsaturated 4- to 7-membered ring system or a bicyclic saturated or partially unsaturated 8- to 14 membered ring system, of which individual members of the ring systems may be replaced by one to three atoms or atomic groups from the series —CHR8-, —CR8R8a-, —(C═R8)-, —NR9-, —C(═O)—, —O—, —S—, —SO— or —SO2—, with the proviso that two units from the series —O—, —S—, —SO—, —SO2— may not be adjacent to each other;
- R3, R4, R5, R6 independently of one another are hydrogen, halogen, (C1-C6)-alkyl, (C1-C3)-alkyloxy-(C1-C3)-alkylene, hydroxy, (C1-C6)-alkylmercapto, amino, (C1-C6)-alkylamino, di-(C2-C12)-alkylamino, (C1-C6)-alkylcarbonyl, COOR7, trifluoromethyl, (C1-C6)-alkylsulfonyl, (C1-C6)-alkylsulfinyl, aminosulfonyl, pentafluorosulfanyl, (C6-C10)-aryl, (C5-C12)-heteroaryl, CO—NR9R10, O—CO—NR9R10, O—CO—(C1-C6)-alkylene-CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, O—CO—(C1-C6)-alkylene-CO—NR9R10 or unsubstituted or mono- or poly-F-substituted (C1-C6)-alkyloxy;
- with the proviso that not more than one of the substituents R3, R4, R5 or R6 is halogen;
- and with the proviso that not more than one of the substituents R3, R4, R5 or R6 is (C1-C6)-alkyl;
- R7 is hydrogen, (C1-C6)-alkyl or benzyl;
- R8, R8a independently of one another are (C1-C6)-alkyl, halogen, trifluoromethyl, COOR7, cyclopropyl or cyclopropylene;
- and
- R9, R10 independently of one another are hydrogen, (C1-C6)-alkyl, —(C6-C10)-aryl, (C5-C12)-heteroaryl, (C3-C12)-cycloalkyl, (C1-C4)-alkylene-(C6-C10)-aryl, (C1-C4)-alkylene-(C5-C12)-heteroaryl, (C1-C4)-alkylene-(C4-C12)-cycloalkyl or (C8-C14)-bicycle;
- or
- a tautomer or a physiologically tolerated salt thereof.
11 more elements
Dependencies are inferred from the claim text.