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US 8,044,074 B2Granted
Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them
AssigneeSanofi-Aventis
InventorsJoachim Brendel, Heinrich Christian Englert, Klaus Wirth, Michael Wagner, Jean-Marie Ruxer, Fabienne Pilorge
Life of this patent
Estimating the term…
Abstract
The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
Claims6
A compound of formula I,
- in which:
- R1 is phenyl which is unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, I, CN, alkoxy having 1, 2, 3 or 4 carbon atoms, OCF3, methylsulfonyl, CF3, alkyl having 1, 2, 3 or 4 carbon atoms, dimethylamino, sulfamoyl, acetyl, and methylsulfonylamino;
- R2 is phenyl or naphthyl,
- where each of these aryl radicals is unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, I, CN, COOMe, CONH2, alkoxy having 1, 2, 3 or 4 carbon atoms, OCF3, OH, methylsulfonyl, CF3, alkyl having 1, 2, 3 or 4 carbon atoms, dimethylamino, sulfamoyl, acetyl, and methylsulfonylamino;
- R3 is CpH2p—R7;
- p is 0, 1, 2, 3, 4or 5;
- R7 is CH3, CH2F, CHF2, CF3, cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms, C≡CH, C≡C—CH3, alkoxy having 1, 2, 3 or 4 carbon atoms, or phenyl,
- where phenyl is unsubstituted or substituted by 1, 2 or 3 substituents selected from the group consisting of F, Cl, Br, I, CF3, OCF3, CN, COOMe, CONH2, COMe, OH, alkyl having 1, 2, 3 or 4 carbon atoms, alkoxy having 1, 2, 3 or 4 carbon atoms, dimethylamino, sulfamoyl, methylsulfonyl and methylsulfonylamino;
- R4 is hydrogen or alkyl having 1, 2 or 3 carbon atoms;
- R5 is hydrogen or alkyl having 1, 2 or 3 carbon atoms;
- R6 is hydrogen, F, Cl, CF3 or alkyl having 1, 2 or 3 carbon atoms;
- X is CH;
- or a pharmaceutically acceptable salt or trifluoroacetate thereof.
10 more elements
Dependencies are inferred from the claim text.