发明名称 SUBSTITUTED MORPHOLINE DERIVATIVES, PREPARATION METHOD THEREOF, PHARMACEUTICAL AGENT CONTAINING THEM AND THEIR USES
摘要 The present invention relates to compounds of formula (I), wherein R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, CF3, NO2, CN, SRa, SORa, SO2Ra, CO2Ra, CONRaRb, C2-6 alkenyl, C2-6 alkynyl or C1-4 alkyl substituted by C1-4 alkoxy, where Ra and Rb are hydrogen or C1-4 alkyl; R2 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy substituted by C1-4 alkoxy or CF3; R3 is hydrogen, halogen or CF3; R4 is selected from the definitions of R1; R5 is selected from the definitions of R2; R6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by =O, =S or a C1-4 alkyl group, and optionally substituted by an aminoalkyl group; R9a and R9b are hydrogen or C1-4 alkyl, or R9a and R9b are joined to form a C5-7 ring; X is C1-4 alkylene optionally substituted by oxo; and Y is a C1-4 alkyl group optionally substituted by hydroxyl; with the proviso that if Y is C1-4 alkyl, R6 is substituted at least by an aminoalkyl group; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
申请公布号 SK83996(A3) 申请公布日期 1996.11.06
申请号 SK19960000839 申请日期 1994.12.23
申请人 MERCK SHARP & DOHME LIMITED 发明人 BAKER RAYMOND;HARRISON TIMOTHY;MACLEOD ANGUS M.;OWENS ANDREW P.;SWAIN CHRISTOPHER J.;SEWARD EILEEN M.;TEALL MARTIN R.
分类号 C07D487/08;A61K31/535;A61K31/5377;A61K31/541;A61P1/08;A61P25/00;A61P25/04;A61P25/06;A61P25/28;A61P29/00;A61P43/00;C07D413/06;C07D413/14;C07D417/14;C07F9/6533;C07F9/6558;(IPC1-7):C07D413/06;C07F9/653 主分类号 C07D487/08
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