TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS FSH RECEPTOR MODULATORS

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)...

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Bibliographische Detailangaben
Hauptverfasser:	TIMMERS, CORNELIS MARIUS, KARSTENS, WILLEM FREDERIK JOHAN
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	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.