摘要 |
The present invention relates to compounds of formula (I), wherein R<1> represents halogen, hydroxy, C1-6alkyl group optionally substituted by one to three fluorine atoms, C1-6alkoxy group optionally substituted by one to three fluorine atoms, or C1-6alkylthio optionally substituted by one to three fluorine atoms; R<2> represents hydrogen, halogen, C1-6alkyl or C1-6alkoxy; or when R<2> is adjacent to R<1>, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R<3> represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; R<4>, R<5>, R<9> and R<10> are a variety of substituents; R<6> represents hydrogen, COR<a>, CO2R<a>, COCONR<a>R<b>, COCO2R<a>, C1-6alkyl optionally substituted by a group selected from (CO2R<a>, CONR<a>R<b>, hydroxy, CN, COR<a>, NR<a>R<b>, C(NOH)NR<a>R<b>, CONHphenyl(C1-4alkyl), COCO2R<a>, CONHNR<a>R<b>, C(S)NR<a>R<b>, CONR<a>C1-6alkylR<12>, CONR<13>C2-6alkenyl, CONR<13>C2-6alkynyl, COCONR<a>R<b>, CONR<a>C(NR<b>)NR<a>R<b>, CONR<a>heteroaryl, and optionally substituted phenyl) or -CH2CCCH2NR<7>R<8> or C1-6alkyl, optionally substituted by oxo, substituted by an optionally substituted 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; 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.
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申请人 |
MERCK SHARP & DOHME LIMITED;BAKER, RAYMOND;HARRISON, TIMOTHY;SWAIN, CHRISTOPHER, JOHN;WILLIAMS, BRIAN, JOHN |
发明人 |
BAKER, RAYMOND;HARRISON, TIMOTHY;SWAIN, CHRISTOPHER, JOHN;WILLIAMS, BRIAN, JOHN |