MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS

摘要

The present invention relates to compounds of formula (I) wherein: R<1>, R<2>, R<3>, R<4> and R<5> are selected from a variety of suitable aromatic substituents; R<6> is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, or C2-4alkyl substituted by C1-4alkoxy or hydroxy; R<7> is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, C2-4alkyl substituted by C1-4alkoxy or hydroxy, or the group C(=NR<c>)NR<a>R<b>; or R<6> and R<7>, 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 NR<8>, S(O) or S(O)2; or R<6> and R<7>, 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; R<8> is hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R<9a> and R<9b> are each independently hydrogen or C1-4alkyl, or R<9a> and R<9b> 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.