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    • 6. 发明公开
    • 1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES
    • 1-(4-脲基苯甲酰基)哌嗪衍生物
    • EP2318368A1
    • 2011-05-11
    • EP09791938.5
    • 2009-08-26
    • N.V. OrganonPharmacopeia, LLC
    • COOKE, Andrew, JohnBENNETT, David, JonathanEDWARDS, Andrew StanleyROUGHTON, Andrew LairdNEAGU, IrinaCHAN, Jui-HsiangHO, Koc-KanANSARI, NasrinMORRIS, Michelle LeeRONG, YajingOHLMEYER, Michael
    • C07D213/56C07D263/34C07D307/68C07D333/38A61P9/10A61K31/496
    • C07D263/34C07D213/56C07D277/56C07D307/68C07D333/38
    • The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R
      1 is (C
      1-8 )alkyl, (C
      3-8 )cycloalkyl or (C
      3-8 )cycloalkyl(C
      1-3 )alkyl, each of which may be substituted by hydroxy, cyano or halogen; R
      2 represents 1 or 2 optional halogens; R
      3 is (C
      1-6 )alkyl, (C
      3-6 )cycloalkyl or (C
      3-6 )cycloalkyl(C
      1-3 )alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5-or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
    • 本发明涉及具有通式I的1-(4-脲基苯甲酰基)哌嗪衍生物(我们引起您的注意,在该电子版中没有提供式I,因为它在该论文摘要中提供)其中R 1 是各自可被羟基,氰基或卤素取代的(C 1-8)烷基,(C 3-8)环烷基或(C 3-8)环烷基(C 1-3)烷基; R 2代表1或2个任选的卤素; R 3是可以被一个或多个卤素取代的(C 1-6)烷基,(C 3-6)环烷基或(C 3-6)环烷基(C 1-3)烷基; A表示包含1-3个选自N,O和S的杂原子的杂芳基环系统,当X是C时,该环系统是5-或6-元,并且当X是N时是5-元; n是1或2; 或其药学上可接受的盐; 涉及包含它们的药物组合物,并涉及这些1-(4-脲基苯甲酰基)哌嗪衍生物在制备用于治疗或预防与胆固醇和胆汁酸转运和代谢相关的动脉粥样硬化和相关病症的药物中的用途。