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    • 3. 发明公开
      EP2318368A1 1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES 失效 转让
    • 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. Organon , Pharmacopeia, LLC
    • COOKE, Andrew, John , BENNETT, David, Jonathan , EDWARDS, Andrew Stanley , ROUGHTON, Andrew Laird , NEAGU, Irina , CHAN, Jui-Hsiang , HO, Koc-Kan , ANSARI, Nasrin , MORRIS, Michelle Lee , RONG, Yajing , OHLMEYER, Michael
    • C07D213/56 , C07D263/34 , C07D307/68 , C07D333/38 , A61P9/10 , A61K31/496
    • C07D263/34 , C07D213/56 , C07D277/56 , C07D307/68 , C07D333/38
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      EP2069315B1 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 无效 转让
    • QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES
    • CHINAZOLINON-和异喹啉酮的乙酰胺衍生物
    • EP2069315B1
    • 2011-09-07
    • EP07842157.5
    • 2007-09-10
    • N.V. Organon , Pharmacopeia, LLC
    • LETOURNEAU, Jeffrey , JOKIEL, Patrick , NAPIER, Susan, Elizabeth , HO, Koc-Kan , OHLMEYER, Michael , MCARTHUR, Duncan, Robert , FIONA, Jeremiah , RATCLIFFE, Paul, David , JURGEN, Schulz
    • C07D239/70 , C07D243/08 , C07D217/24 , A61K31/519 , A61K31/5513 , A61K31/472 , A61K31/4725 , A61K31/496 , A61P25/24
    • C07D403/04 , C07D217/24 , C07D239/91 , C07D401/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/08 , C07D487/04
    • The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, C2-6alkenyl, C2-6alkynyl, said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, C1-6alkyloxy, cyano or one or more halogens; R2 is C6-10aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy and C3-6cycloalkyloxy, said C1-6alkyl, C3-6 cycloalkyl, C1-6 alkyloxy and C3-6Cycloalkyloxy being optionally substituted with one or more halogens; or R2 is a 5-10 membered heteroaryl ring system comprising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C1-6alkyloxy and halogen; or R2 is C4-7cycloalkyl; R3 is an optional substituent selected from C1-6alkyl, C1-6alkyloxy and halogen, said C1-6alkyl and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R5 together with one of R6 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R5 together with one of R7 and R8 forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R6 is independently H, halogen or C1-4alkyl optionally substituted with halogen or SO2CH3 or one of R6 together with R5 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R7 and R8 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylc1-3alkyl, cyanoC1-3alkyl, C6-10aryl, C6-10arylC1-3alkyl, C1-3alkyloxyC1-3alkyl or C1-6acyl said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, 1 or more halogens or diC1-2alkylamino; or R7 and R8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR10, said heterocyclic ring being optionally substituted with one or two substituents selected from C1-6alkyl, halogen, hydroxy, C1-6alkyloxy, cyano and COOR11; or one of R7 and R8 is Y, CH2Y or CH2CH2Y, wherein Y is a 4-6 membered saturated heterocyclic ring comprising a heterocyclic moiety selected from O, SO2 and NR10, said ring being optionally substituted with 1 -2 substituents selected from methyl or halogen; or one of R7 or R8 together with R5 forms a 6-8 membered heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or one of R7 and R8 together with R12 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroato
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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