Morpholine derivatives, compositions containing them and...

C - Chemistry – Metallurgy – 07 – D

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C07D 413/06 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/695 (2006.01) C07D 413/14 (2006.01) C07D 417/06 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2215699

The present invention relates to compounds of formula (I), wherein R1 and R4 represent hydrogen, halogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3- 7cycloalkyl, C3-7cycloalkylC1-4alkyl, C1-6alkoxy, C1-4alkyl substituted by a hydroxy or C1-4alkoxy group, OCF3, hydroxy, trifluoromethyl, trimethylsilyl, nitro, CN, SRa, SORa, SO2Ra, CORa, CO2Ra or CONRaRb, where Ra and Rb are each independently hydrogen or C1-4alkyl; R2, R3 and R5 represent hydrogen, halogen, C1-6alkyl, C1-6alkoxy substituted by a C1-4alkoxy group, or trifluoromethyl; R6 represents C1-6alkyl, optionally substituted by oxo, substituted by a 5-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, oxadiazole and thiadiazole, wherein each heteroaromatic ring is substituted at the available carbon atom by a group of the formula: ZNR7R8. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.

La présente invention concerne des composés ayant la formule (I). Dans cette formule, R?1¿ et R?4¿ représentent un hydrogène, un halogène, un C¿1-6? alkyle, un C¿2-6? alcényle, un C¿2-6? alcynyle, un C¿3-7? cycloalkyle, un C¿3-7? cycloalkyleC¿1-4?alkyle, un C¿1-6?alcoxy, un C¿1-4? alkyle substitué par un hydroxy ou par un groupe C¿1-4? alcoxy, OCF¿3?, hydroxy, trifluorométhyle, triméthylsilyle, nitro, CN, SR?a¿, SOR?a¿, SO¿2?R?a¿, COR?a¿, CO¿2?R?a¿ ou CONR?a¿R?b¿, où R?a¿ et R?b¿ sont chacun indépendamment un hydrogène, un C¿1-4? alkyle; R?2¿, R?3¿ et R?5¿ représentent un hydrogène, un halogène, un C¿1-6? alkyle, un C¿1-6? alcoxy substitué par un groupe C¿1-4? alcoxy ou un groupe trifluorométhyle; R?6¿ représente un C¿1-6? alkyle, éventuellement substitué par oxo, et substitué par un hétérocycle aromatique à 5 éléments choisi parmi l'oxazole, le thiazole, l'isoxazole, l'isothiazole, l'oxadiazole et le thiadiazole, où chaque hétérocycle aromatique est substitué sur l'atome de carbone disponible par un groupe de la formule: ZNR?7¿R?8¿. Ces composés sont particulièrement utiles pour le traitement des douleurs, de l'inflammation, de la migraine et des vomissements.

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