C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/48 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61P 5/24 (2006.01) A61P 15/00 (2006.01) C07D 215/20 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01)
Patent
CA 2606683
The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)- heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l- 4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
L'invention concerne des dérivés de 4-phényl-5-oxo-1,4,5,6,7,8-hexahydroquinoline de formule I ou un sel pharmaceutiquement acceptable de ceux-ci. Dans cette formule, R<SUP>1</SUP> désigne alkyle (C<SUB>1-6</SUB>), alcényle (C<SUB>2-6</SUB>) ou alcynyle (C<SUB>2-6</SUB>); R<SUP>2</SUP> et R<SUP>3</SUP> désignent indépendamment halogène, alcyle (C<SUB>1-4</SUB>), alcényle (C<SUB>2-4</SUB>), alcynyle (C<SUB>2-4</SUB>), alcoxy (C<SUB>1-4</SUB>), alcényloxy (C<SUB>3-4</SUB>) ou alcynyloxy (C<SUB>3-4</SUB>); R<SUP>4</SUP> désigne phényle ou hétéroaryle (C<SUB>2-5</SUB>), les deux étant substitués par R<SUP>7</SUP> et éventuellement substitués sur l'anneau (hétéro)aromatique par au moins un substituant sélectionné parmi: hydroxy, amine, halogène, nitro, trifluorométhyle, cyano, alkyle (C<SUB>1-4</SUB>), alcoxy (C<SUB>1-4</SUB>), alkylthio (C<SUB>1-4</SUB>) et (di)alkylamino (C<SUB>1-4</SUB>). L'invention concerne également des compositions pharmaceutiques comprenant les dérivés susmentionnés, ainsi que l'utilisation des dérivés de 4-phényl-5-oxo-1,4,5,6,7,8-hexahydroquinoline pour une thérapie, et en particulier pour le traitement de l'infertilité.
Grima Poveda Pedro Manuel
Karstens Willem Frederik Johan
Timmers Cornelis Marius
Fetherstonhaugh & Co.
N.v. Organon
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