发明名称 Morpholine derivatives and their use as therapeutic agents
摘要 PCT No. PCT/GB96/02766 Sec. 371 Date May 14, 1998 Sec. 102(e) Date May 14, 1998 PCT Filed Nov. 13, 1996 PCT Pub. No. WO97/18206 PCT Pub. Date May 22, 1997The 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, R9aand R9b are a variety of substituents; R6 is hydrogen, C1-6akyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, or C2-4akyl 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.
申请公布号 US5968934(A) 申请公布日期 1999.10.19
申请号 US19980068818 申请日期 1998.05.14
申请人 MERCK SHARP & DOHME LTD. 发明人 SWAIN, CHRISTOPHER JOHN;TEALL, MARTIN RICHARD;WILLIAMS, BRIAN JOHN
分类号 A61K31/00;A61K31/535;A61K31/5375;A61K31/5377;A61P25/06;A61P29/00;A61P43/00;C07D413/04;C07D417/04;(IPC1-7):C07D413/04 主分类号 A61K31/00
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