Tetrahydroquinoline derivatives and their use as follicle...

Details Tetrahydroquinoline derivatives and their use as follicle... Tetrahydroquinoline derivatives and their use as follicle...

C - Chemistry, Metallurgy

07

D

C07D 215/38 (2006.01) A61K 31/47 (2006.01) A61P 5/08 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2508952

The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H or Me; R3 is H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2- 4C)alkoxy or (2-6)heterocycloakl(2~-4C)alkoxy; R4 is H, OH, (1-4C)alkoxy or R7; R5 is H, OH, (1-4C)alkoxy or R7,with the proviso that if R4 is H, R5 is not H, OH or (1-4C)alkoxy and that if R5 is H, R4 is not H, OH or (1- 4C)alkoxy; R6 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2~ 6C)heterocycloalkyl or (1-6C)alkyl; R7 is amino, (di)(1-4C) alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) heteroarylcarbonylamino, (2~-5C)heteroarylcarbonyloxy, R8-(2-4C)alkylamino, R8-(2-4C)alkoxy, R9- methylamino or R9-methoxy; R8 is hydroxy, amino, (1-4C)alkoxy, (di)(1- 4C)alkylamino, (2-~6C)heterocycloalkyl, (2-6C) heterocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C) alkoxycarbonylamino and R9 is aminocarbonyl, (di)(1-4C)alkylaminocarbonyl, (2-5C)heteroaryl or (6C)aryl. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.

La présente invention porte sur des dérivés de tétrahydroquinoline de formule générale (I) ou sur un sel de ceux-ci acceptable d'un point de vue pharmaceutique. Dans cette formule, R?1¿ et R?2¿ représentent H ou Me; R?3¿ représente H, hydroxy, (1-4C)alcoxy, (di)(1-4C)alkylamino(2-4C)alcoxy ou (2-6)hétérocycloalkyl(2--4C)alcoxy; R?4¿ représente H, OH, (1-4C)alcoxy ou R?7¿; R?5¿ représente H, OH, (1-4C)alcoxy ou R?7¿, à condition que, si R?4¿ représente H, R?5¿ ne représente pas H, OH ou (1-4C)alcoxy et que si R?5¿ représente H, R?4¿ ne représente pas H, OH ou (1-4C)alcoxy; R?6¿ représente (2-5C)hétéroaryle, (6C)aryle, (3-8C)cycloalkyle, (2- 6C)hétérocycloalkyle ou (1-6C)alkyle; R?7¿ représente amino, (di)(1-4C) alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) hétéroarylcarbonylamino, (2--5C)hétéroarylcarbonyloxy, R?8¿-(2-4C)alkylamino, R?8¿-(2-4C)alcoxy, R?9¿-méthylamino ou R?9¿-méthoxy; R?8¿ représente hydroxy, amino, (1-4C)alcoxy, (di)(1-4C)alkylamino, (2--6C)hétérocycloalkyle, (2-6C) hétérocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C) alcoxycarbonylamino et R?9¿ représente aminocarbonyle, (di)(1-4C)alkylaminocarbonyle, (2-5C)hétéroaryle ou (6C)aryle. La présente invention porte également sur des compositions pharmaceutiques comprenant ces dérivés et sur leur utilisation pour réguler la fécondité.

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