C - Chemistry – Metallurgy – 07 – D
Patent
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 409/12 (2006.01)
Patent
CA 2508923
The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein Rl and R2 are H, Me; R3 is (2-6C)heterocycloalkyl(1-~4C)alkyl, (2-5C)heteroaryl(1- 4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-~6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R5-(2-4C)alkyl or R5- carbonyl(1-4C)alkyl; R4 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2- 6C)heterocycloalkyl or (1-6C) alkyl and R5 is (di)(1-4C)alkylamino, (1- 4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2- 5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1~-4C)alkoxy(2- 4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2- 4C)alkyl]amino or (di)[hydroxy(2~-4C)alkyl]amino. 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, Me; R?3¿ représente (2-6C)hétérocycloalkyl(1--4C)alkyle, (2-5C)hétéroaryl(1-4C)alkyle, (6C)aryle (1-4C)alkyle, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyle, (2--6C) hétérocycloalkylcarbonylamino(2-4C)alkyle, R?5¿-(2-4C)alkyle ou R?5¿-carbonyl(1-4C)alkyle; R?4¿ représente (2-5C)hétéroaryle, (6C)aryle, (3-8C)cycloalkyle, (2-6C)hétérocycloalkyle ou (1-6C) alkyle et R?5¿ représente (di)(1-4C)alkylamino, (1-4C)alcoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alcénylamino, (2-5C)hétéroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1--4C)alcoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino ou (di)[hydroxy(2--4C)alkyl]amino. La présente invention porte également sur des compositions pharmaceutiques comprenant ces dérivés et sur leur utilisation afin de réguler la fécondité.
Karstens Willem Frederik Johan
Timmers Cornelis Marius
Akzo Nobel N.v.
Fetherstonhaugh & Co.
N.v. Organon
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