5-amino-4-hydroxy-7-(1h-indolmethyl)-8-methylnonamide...

Details 5-amino-4-hydroxy-7-(1h-indolmethyl)-8-methylnonamide... 5-amino-4-hydroxy-7-(1h-indolmethyl)-8-methylnonamide...

C - Chemistry, Metallurgy

07

D

C07D 209/20 (2006.01) A61K 31/405 (2006.01) A61P 9/12 (2006.01) C07C 237/22 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2560199

The application relatés to novel alkanamides of the general formula (I) where X is -CH2- or >CH-OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2 is C1-C6-alkyl or C3-C6-cydoalkyl; R3 are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl or C1-C6-alkanoyl; R4 is C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl or unsubstituted or substituted aryl~C1-C6-alkyl; R5 is Cl-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6- alkoxy-C1-C6-alkyl, C1-C6-alkanoyloxy~ C1-C6-alkyl, C1-C6-aminoalkyl, C1-C6- alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-Cl-C6-alkyl, C1-C6-alkanoylamido-C1- C6-alkyl, HO(O)C-C1-C6-alkyl, C1-C6-alkyl-O-(O)C-C1-C6-alkyl, H2N-C(O)-C1-C6- alkyl, C1-C6-alkyl-HN-C(O)-C1-C6-alkyl, (C1,-C6-alkyl)2N-C(O)-C1-C6-alkyl, C2- C8-alkenyl, C2-C8-alkynyl, cyano-C1-C6-alkyl, halo-Cl-C6-alkyl, optionally substituted aryl-~Co-C6-alkyl, optionally substituted C3-C8-cycloalkyl-Co-C6- alkyl or optionally substituted heterocydyl-Co-C6-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.

L'invention concerne de nouveaux alcanamides représentés par la formule générale (I), dans laquelle X représente -CH¿2?- ou >CH-OH; (A) R?1¿ représente par exemple un radical hétérocyclyle éventuellement substitué ou un radical d'hydrocarbure non saturé, polycyclique éventuellement substitué dans lequel X représente un hydroxyméthylène; R?2¿ représente C¿1?-C¿6?-alkyle ou C¿3?-C¿6?-cycloalkyle; R?3¿ représentent chacun de façon indépendante H, C¿1?-C¿6?-alkyle, C¿1-6?-alcoxycarbonyle ou C¿1?-C¿6?-alkanoyle; R?4¿ représente C¿1?-C¿6?-alkyle, C¿3?-C¿6?-cycloalkyle, C¿2?-C¿6?-alcényle ou aryle-C¿1?-C¿6?-alkyle substitué ou non substitué; R?5¿ représente C¿l?-C¿6?-alkyle, C¿1?-C¿6?-hydroxyalkyle, C¿1?-C¿6?-alcoxy-C¿1?-C¿6?-alkyle, C¿1?-C¿6?-alcanoyloxy- C¿1?-C¿6?-alkyle, C¿1?-C¿6?-aminoalkyle, C¿1?-C¿6?-alkylamino-C¿1?-C¿6?-alkyle, C¿1?-C¿6?-dialkylamino-C¿l?-C¿6?-alkyle, C¿1?-C¿6?-alkanoylamido-C¿1?-C¿6?-alkyle, HO(O)C-C¿1?-C¿6?-alkyle, C¿1?-C¿6?-alkyle-O-(O)C-C¿1?-C¿6?-alkyle, H¿2?N-C(O)-C¿1?-C¿6?-alkyle, C¿1?-C¿6?-alkyle-HN-C(O)-C¿1?-C¿6?-alkyle, (C¿1?,-C¿6?-alkyl)¿2?N-C(O)-C¿1?-C¿6?-alkyle, C¿2?-C¿8?-alcényle, C¿2?-C¿8?-alkynyle, cyano-C¿1?-C¿6?-alkyle, halo-C¿l?-C¿6?-alkyle, un aryle-C¿o?-C¿6?-alkyle éventuellement substitué, un C¿3?-C¿8?-cycloalkyle-C¿o?-C¿6?-alkyle éventuellement substitué ou un hétérocyclyle-C¿o?-C¿6?-alkyle éventuellement substitué. Cette invention concerne également un procédé destiné à la préparation et à l'utilisation de ces composés en tant que médicaments, notamment en tant qu'inhibiteurs de rénine dans le traitement de l'hypertension.

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