Tetrahydroquinoline derivatives

Details Tetrahydroquinoline derivatives Tetrahydroquinoline derivatives

C - Chemistry, Metallurgy

07

D

C07D 413/12 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61P 5/06 (2006.01) A61P 15/08 (2006.01) C07D 215/08 (2006.01) C07D 215/20 (2006.01) C07D 215/38 (2006.01) C07D 215/48 (2006.01) C07D 401/12 (2006.01) C07D 405/14 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2452606

The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1- 4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y-X is (CO)-O, (SO)2-O, NHC(O)-O, NHC(S)-O, OC(O)-O, bond-O, C(O)-NH, S(O)2-NH, NHC(O)-NH, NHC(S)-NH, OC(O)-NH, bond-NH, NH-C(O), O-C(O), NH-S(O)2, or O-S(O)2 or Y-X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3- 9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1- 4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3- 6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8, R9- aminocarbonyl(1-4C)alkyl, R8, R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1- 4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-10C)aryl, (3- 9C)heteroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3- 6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, (1- 4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1- 4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1- 4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2- 6C)heterocycloylkyl, or R8 and R9 may be joined in a (2-6C)heterocycloalkyl ring. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to control fertility.

L'invention se rapporte à des dérivés de tétrahydroquinoline représentés par la formule (I) ou à un sel de ces derniers pharmaceutiquement acceptable. Dans cette formule, R?1¿ est formyle, (1-6C)alkylcarbonyl ou (1-6C)alkylsulfonyl; R?2¿ et R?3¿ sont H ou (1-4C)alkyl; R?4¿ est phényle; R?5¿ est (1-4C)alkyl; Y-X est (CO)-O, (SO)¿2?-O, NHC(O)-O, NHC(S)-O, OC(O)-O, une liaison O, C(O)-NH, S(O)¿2?-NH, NHC(O)-NH, NHC(S)-NH, OC(O)-NH, une liaison NH, NH-C(O), O-C(O), NH-S(O)¿2?, ou O-S(O)¿2? ou Y-X est une liaison; R?6¿ est H, trifluorométhyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkényl, (3-9C)hétéroaryl, (3-6C)cycloalkyl, (2-6C)hétérocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)hétéroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)hétérocycloalkyl(1-4C)alkyl, R?8¿, R?9¿-aminocarbonyl(1-4C)alkyl, R?8¿, R?9¿-amino(1-4C)alkyl, R?8¿-oxycarbonyl(1-4C)alkyl, R?8¿-oxy(1-4C)alkyl, R?8¿-carbonyl(1-4C)alkyl ou (6-10C)aryl; R?7¿ est H, (1-4C)alkyl, (1-4C)alkoxy, halogène, trifluorométhyl, cyano, nitro hydroxyl; et R?8¿ et/ou R?9¿ est H, (1-4C)alkyl, (2-4C)alkényl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)hétéroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)hétéroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)hétérocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)hétérocycloylkyl, ou R?8¿ et R?9¿ peuvent être joints dans un noyau (2-6C)hétérocycloalkyl. L'invention concerne aussi des compositions pharmaceutiques contenant lesdits dérivés et l'utilisation de ces dérivés dans le contrôle de la fertilité.

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