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    • 4. 发明申请
    • N-AROYL PIPERAZINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
    • 作为OREXIN受体拮抗剂的N-硝基苯哌酮衍生物
    • WO2003032991A1
    • 2003-04-24
    • PCT/EP2002/011316
    • 2002-10-09
    • SMITHKLINE BEECHAM PLCBRANCH, Clive, LeslieJOHSON, Christopher, NorbertNASH, David, JohnSTEMP, Geoffrey
    • BRANCH, Clive, LeslieJOHSON, Christopher, NorbertNASH, David, JohnSTEMP, Geoffrey
    • A61K31/495
    • C07D413/10C07D241/04C07D417/06
    • This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR 2 ; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C=O, SO 2 , or CH=CH-; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by R 1 and further optional substituents; or Ar 2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; R 1 represents optionally substituted (C 1-4 )alkoxy, halo, optionally substituted (C 1-6 )alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; R?2 ¿represents hydrogen, optionally substituted (C 1-4 )alkyl, optionally substituted (C 1-6 )alkanoyl, optionally subtituted (C 1-6 )alkanoxycarbonyl or optionally substituted aryl(C 1-6 )alkyloxycarbonyl; and their use as orexin receptor-antagonists.
    • 本发明涉及式(I)的N-芳酰基哌嗪衍生物,其中:Y表示NR 2; m表示1,2或3; p表示0或1; X是O,S,C = O,SO 2或CH = CH-; Ar 1是芳基或含有至多4个选自N,O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示苯基或含有1至3个选自N,O和S的杂原子的5或6元杂环基,其中苯基杂环基被R 1取代,另外任选的取代基; 或Ar 2表示含有1至4个选自N,O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示任选取代的(C 1-4)烷氧基,卤素,任选取代的(C 1-6)烷基,任选取代的苯基,或任选取代的含有1至4个选自N, O和S; 任选取代的(C 1-6)烷酰基,任选取代的(C 1-6)烷氧基羰基或任选取代的芳基(C 1-6)烷氧基羰基; 以及它们作为食欲肽受体拮抗剂的用途。