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22. 发明申请

WO1995018124A1 SUBSTITUTED MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：取代的吗啉衍生物及其作为治疗剂的用途
公开(公告)号：WO1995018124A1
公开(公告)日：1995-07-06
申请号：PCT/GB1994002819
申请日：1994-12-23
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , HARRISON, Timothy , MACLEOD, Angus, Murray , OWENS, Andrew, Pate , SEWARD, Eileen, Mary , SWAIN, Christopher, John , TEALL, Martin, Richard
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D413/06
CPC分类号： C07D413/06 , C07D413/14 , C07F9/6533 , C07F9/65583
摘要： The present invention relates to compounds of formula (I), wherein R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, CF3, NO2, CN, SR , SOR , SO2R , CO2R , CONR R , C2-6 alkenyl, C2-6 alkynyl or C1-4 alkyl substituted by C1-4 alkoxy, where R and R are hydrogen or C1-4 alkyl; R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy substituted by C1-4 alkoxy or CF3; R is hydrogen, halogen or CF3; R is selected from the definitions of R ; R is selected from the definitions of R ; R 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; R and R are hydrogen or C1-4 alkyl, or R and R 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, R 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.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，NO 2，CN，SR a，SOR a，SO 2 R， α，CO 2 R a，CONR a R b，C 2-6烯基，C 2-6炔基或被C 1-4烷氧基取代的C 1-4烷基，其中R a和R b是氢或C 1-4烷基; R 2是氢，卤素，C 1-6烷基，被C 1-4烷氧基或CF 3取代的C 1-6烷氧基; R 3是氢，卤素或CF 3; R 4选自R 1的定义; R 5选自R 2的定义; R 6是含有2或3个氮原子的5元或6元杂环，其任选被= O，= S或C 1-4烷基取代，并且任选被氨基烷基取代; R 9a和R 9b是氢或C 1-4烷基，或R 9a和R 9b连接形成C5-7环; X是任选被氧代取代的C 1-4亚烷基; Y是任选被羟基取代的C 1-4烷基; 条件是如果Y是C 1-4烷基，则R 6至少被氨基烷基取代; 及其药学上可接受的盐和前药。该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

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