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 413/04 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 413/14 (2006.01) C07D 417/04 (2006.01) C07D 417/14 (2006.01) C07D 453/06 (2006.01) C07D 471/08 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2235855

The present invention relates to compounds of formula (I) wherein X is a 5- or 6-membered C-linked heteroaromatic ring containing 1 to 4 nitrogen atoms and optionally containing in the ring one oxygen or sulphur atom; Y is a group of the formula -(CH2)nNR6R7, or a methylene- or ethylene-linked imidazolyl group; Z is hydrogen or C1-4alkyl optionally substituted by a hydroxy group; R1, R2, R3, R4, R5, R9a and R9b are a variety of 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, or C2-4alkyl substituted by one or two substituents selected from C1-4alkoxy, hydroxy or a 4-, 5- or 6- membered heteroaliphatic ring containing one or two heteroatoms selected from N, O and S; or R6 and R7, together with the nitrogen atom to which they are attached, form a saturated or partially saturated heterocyclic ring or a non- aromatic azabicyclic ring system; and n is zero, 1 or 2; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherapeutic neuralgia.

L'invention concerne des composés de la formule (I). Dans cette formule, X est un cycle hétéroaromatique à liaison carbone de 5 à 6 éléments et contenant de 1 à 4 atomes d'azote, ainsi qu'éventuellement un atome d'oxygène ou de soufre; Y est un groupe de la formule -(CH¿2?)¿n?NR?6¿R?7¿ ou un groupe imidazolyle à liaison méthylène ou éthylène: Z est un hydrogène ou un alkyle C¿1-4?, éventuellement substitué par un groupe hydroxy; R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?9a¿ et R?9b¿ sont différents substituants; R?6¿ est un hydrogène, alkyle C¿1-6?, cycloalkyle C¿3-7?, cycloalkyl C¿3-7? alkyle C¿1-4?, phényle ou alkyle C¿2-4?, substitué par alcoxy C¿1-4? ou hydroxy; R?7¿ est un hydrogène, alkyle C¿1-6?, cycloalkyle C¿3-7?, cycloalkyl C¿3-7? alkyle C¿1-4?, phényle ou alkyle C¿2-4? substitué par un ou deux substituants choisis parmi alcoxy C¿1-4?, hydroxy ou un cycle hétéroaliphatique à 4, 5 ou 6 éléments, renfermant un ou deux hétéroatomes choisis parmi N, O et S; ou R?6¿ et R?7¿ forment ensemble et avec l'atome d'azote auquel ils sont liés, un hétérocycle saturé ou partiellement saturé, ou encore un système non aromatique azabicylique; et n est égal à zéro, 1 ou 2. L'invention concerne également les sels de ces composés acceptables sur le plan pharmaceutique. Ces composés sont particulièrement utiles dans le traitement ou la prévention de douleurs, d'inflammations, de migraines, de vomissements ou d'algies post-zostériennes.

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