Morpholine derivatives and their use as therapeutic agents

Details Morpholine derivatives and their use as therapeutic agents Morpholine derivatives and their use as therapeutic agents

C - Chemistry, Metallurgy

07

D

C07D 265/28 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 265/32 (2006.01) C07D 413/06 (2006.01) C07D 471/10 (2006.01)

Patent

CA 2198477

The present invention relates to compounds of formula (I) wherein: R1, R2, R3, R4 and R5 are selected from a variety of suitable aromatic substituents; R6 is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, or C2- 4alkyl substituted by C1-4alkoxy or hydroxy; R7 is hydrogen, C1-6alkyl, C3- 7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, C2-4alkyl substituted by C1- 4alkoxy or hydroxy, or the group C(=NRc)NRaRb; or R6 and R7, together with the nitrogen atom to which they are attached, form an optionally substituted saturated heterocyclic ring of 4 to 7 ring atoms which may optionally contain in the ring one oxygen or sulphur atom or a group selected from NR8, S(O) or S(O)2; or R6 and R7, together with the nitrogen atom to which they are attached, form a piperidino ring substituted by a spiro-fused indene or indoline group, each of which may be unsubstituted or substituted; R8 is hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R9a and R9b are each independently hydrogen or C1-4alkyl, or R9a and R9b are joined so, together with the carbon atoms to which they are attached, there is formed a C5-7 ring; X is selected from -CH2CH2-, -COCH2- or -CH2CO-; and Y is hydrogen, or C1-4alkyl optionally substituted by a hydroxyl group; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

Composés de formule (I) dans laquelle R?1¿, R?2¿, R?3¿, R?4¿ et R?5¿ sont choisis parmi une variété de substituants aromatiques appropriés; R?6¿ est hydrogène, alkyle C¿1-6?, cycloalkyle C¿3-7?, cycloalkyle C¿3-7?-alkyle C¿1-4?, phényle, ou alkyle C¿2-4? substitué par alcoxy C¿1-4? ou hydroxy; R?7¿ est hydrogène, alkyle C¿1-6?, cycloalkyle C¿3-7?, cycloalkyle C¿3-7?-alkyle C¿1-4?, phényle, alkyle C¿2-4? substitué par alcoxy C¿1-4? ou hydroxy, ou le groupe C(=NR?c¿)NR?a¿R?b¿; ou R?6¿ et R?7¿, avec l'atome d'azote auquel ils sont attachés, forment un noyau hétérocyclique saturé éventuellement substitué de 4 à 7 atomes dans le noyau qui peuvent éventuellement contenir dans le noyau un atome d'oxygène ou un atome de soufre ou un groupe choisi parmi NR?8¿, S(O) ou S(O)¿2?; ou R?6¿ et R?7¿, avec l'atome d'azote auquel ils sont attachés, forment un noyau pipéridine substitué par un indène spiro-condensé ou un groupe indoline, chacun d'entre eux pouvant être non substitué ou substitué; R?8¿ est hydrogène, alkyle C¿1-4?, hydroxy-alkyle C¿1-4? ou alcoxy C¿1-4?-alkyle C¿1-4?; R?9a¿ et R?9b¿ sont chacun indépendamment hydrogène ou alkyle C¿1-4?, ou R?9a¿ et R?9b¿ sont joints de telle manière aux atomes de carbone auxquels ils sont attachés qu'un noyau C¿5-7? est formé; X est choisi parmi -CH¿2?CH¿2?-, -COCH¿2?- ou -CH¿2?CO-; et Y est hydrogène ou alkyle C¿1-4? éventuellement substitué par un groupe hydroxyle, ou sel pharmaceutiquement acceptable desdits composés. Lesdits composés sont particulièrement utiles dans le traitement ou la prévention de la douleur, des inflammations, de la migraine, des vomissements et des algies post-zostériennes.

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