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    Indole derivatives
    3.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US07655645B2

    公开(公告)日：2010-02-02

    申请号：US12031851

    申请日：2008-02-15

    申请人： Julia Adam

    发明人： Julia Adam

    IPC分类号： A61K31/551 ,  A61K31/496 ,  C07D413/14 ,  C07D417/14

    CPC分类号： C07D417/04 ,  C07D413/04

    摘要： The invention relates to indole derivative having the general Formula I wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH; Y represents CH2, O, S or SO2; R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN or halogen; R2, R2′, R3, R3′, R4, R4′, R5 and R5′ are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO—OR8; or one pair of geminal substituents R3 and R3′ or R5 and R5′ together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2 and R5 together represent a methylene or an ethylene bridge, and R2′, R3, R3′, R4, R4′ and R5′ are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO—NR9R10, CO—OR11 or 1,2,4-oxadiazol-3-yl), SO2NR12R13 or COOR14; R7 is H or halogen; R8 is (C1-4)alkyl; R9 and R10 are independently hydrogen, (C1-4)alkyl or (C3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11 is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14 is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof, as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

    摘要翻译： 本发明涉及具有通式I的吲哚衍生物，其中A代表5元芳族杂环，其中X1，X2和X3独立地选自N，O，S和CH; Y表示CH 2，O，S或SO 2; R 1是H，（C 1-4） - 烷基，（C 1-4）烷氧基，CN或卤素; R2，R2'，R3，R3'，R4，R4'，R5和R5'独立地是氢，（C1-4）烷基（任选被OH取代）或CO-OR8; 或一对偕取代基R 3和R 3'或R 5和R 5'一起代表酮基，而其它取代基全部为氢或（C 1-4）烷基; 或者R 2和R 5一起表示亚甲基或乙烯桥，R2'，R3，R3'，R4，R4'和R5'是氢; n为1或2; R 6是H，（C 1-4）烷基（任选被OH，（C 1-4）烷氧基，CO-NR 9 R 10，CO-OR 11或1,2,4-恶二唑-3-基），SO 2 NR 12 R 13或COOR 14取代; R7是H或卤素; R8是（C1-4）烷基; R 9和R 10独立地为氢，（C 1-4）烷基或（C 3-7）环烷基，所述烷基任选被OH或（C 1-4）烷氧基取代; R11为H或（C1-4）烷基; R 12和R 13独立地为H或（C 1-4）烷基; R14是（C1-6）烷基; 或其药学上可接受的盐作为大麻素CB1受体的激动剂，其可用于治疗疼痛，例如手术前疼痛，慢性疼痛，神经性疼痛，癌症疼痛和与多发性硬化相关的疼痛和痉挛状态。

    INDOLE DERIVATIVES
    4.
    发明申请
    INDOLE DERIVATIVES 失效

    公开(公告)号：US20080207598A1

    公开(公告)日：2008-08-28

    申请号：US12031851

    申请日：2008-02-15

    申请人： Julia Adam

    发明人： Julia Adam

    IPC分类号： A61K31/496 ,  C07D417/06 ,  A61K31/551 ,  A61P25/00 ,  C07D243/08

    CPC分类号： C07D417/04 ,  C07D413/04

    摘要： The invention relates to indole derivative having the general Formula I wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH; Y represents CH2, O, S or SO2; R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN or halogen; R2, R2′, R3, R3′, R4, R4′, R5 and R5′ are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO—OR8; or one pair of geminal substituents R3 and R3′ or R5 and R5′ together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2 and R5 together represent a methylene or an ethylene bridge, and R2′, R3, R3′, R4, R4′ and R5′ are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH(C1-4)alkyloxy, CO—NR9R10, CO—OR11 or 1,2,4-oxadiazol-3-yl), SO2NR12R13 or COOR14; R7 is H or halogen; R8 is (C1-4)alkyl; R9 and R10 are independently hydrogen, (C1-4)alkyl or (C3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11 is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14 is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof, as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.