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US 8,076,327 B2Granted
Condensed imidazole derivatives as aldosterone synthase inhibitors
AssigneeNovartis AG
InventorsPeter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stefan Stutz, Bibia Bennacer
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Abstract
The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
Claims18
A compound of the formula
- in which
- R is deuterium, halogen, or hydrogen;
- R1 is aryl-C0-C4-alkyl or heterocyclyl-C0-C4-alkyl, which radicals are unsubstituted or substituted by 1-4 C1-C8 alkoxy, C1-C8 alkoxycarbonyl, C1-C8 alkyl, C0-C8 alkylcarbonyl, C1-C8 alkylsulphonyl, unsubstituted or substituted aryl, aryl-C0-C4 alkoxycarbonyl, cyano, halogen, unsubstituted or substituted heterocyclyl, hydroxy, nitro, oxide, oxo, tri-C1-C4 alkylsilyl, trifluoromethoxy or trifluoromethyl;
- R2 is a) deuterium, halogen, hydroxy, cyano or hydrogen;
- or
- is b) C2-C8 alkenyl, C2-C8 alkynyl, C1-C8 alkoxy, C1-C4 alkoxycarbonyl-C1-C4 alkyl, C1-C8 alkyl, C0-C4 alkylcarbonyl, aryl-C0-C4 alkyl, carboxy-C1-C4 alkyl, C3-C8 cycloalkyl or heterocyclyl-C0-C4 alkyl, which radicals are unsubstituted or substituted by 1-4 C1-C8 alkoxy, C1-C8 alkoxycarbonyl, C1-C8 alkyl, C0-C8 alkylcarbonyl, C1-C8 alkylsulphonyl, unsubstituted or substituted aryl, aryl-C0-C4 alkoxycarbonyl, cyano, halogen, unsubstituted or substituted heterocyclyl, hydroxy, nitro, oxide, oxo, tri-C1-C4 alkylsilyl, trifluoromethoxy or trifluoromethyl;
- R3 is C1-C8 alkyl;
- Q is sulphur;
- m is a number 0, 1 or 2;
- n is a number 1;
- or a pharmaceutically acceptable salt thereof
- where
- R1 is not C1-C8 alkyl-substituted aryl if R2 is hydrogen;
- and heterocyclyl in heterocyclyl-C0-C4-alkyl stands for a saturated, partially saturated or unsaturated, 4-8 membered monocylic ring system, a saturated, partially saturated or unsaturated 7-12 membered bicyclic ring system, or a partially saturated or unsaturated 9-12 membered tricyclic ring system.
11 more elements
Dependencies are inferred from the claim text.