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    Imidazole derivatives having affinity for alpha2 receptors
    6.
    发明授权
    Imidazole derivatives having affinity for alpha2 receptors 有权
    对α2受体具有亲和力的咪唑衍生物

    公开(公告)号：US06313311B1

    公开(公告)日：2001-11-06

    申请号：US09051151

    申请日：1999-02-02

    申请人： Arto Karjalainen ,  Paavo Huhtala ,  Juha-Matti Savola ,  Siegfried Wurster ,  Maire Eloranta ,  Maarit Hillilä ,  Raimo Saxlund ,  Victor Cockcroft ,  Arja Karjalainen

    发明人： Arto Karjalainen ,  Paavo Huhtala ,  Juha-Matti Savola ,  Siegfried Wurster ,  Maire Eloranta ,  Maarit Hillilä ,  Raimo Saxlund ,  Victor Cockcroft ,  Arja Karjalainen

    IPC分类号： C07D23354

    CPC分类号： C07D233/56 ,  C07D233/64

    摘要： Imidazole derivatives of formula (I) wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.

    摘要翻译： 式（I）的咪唑衍生物，其中n为0或1，R1为氢或C1-C4-烷基，R2为氢或R2和R3一起形成双键，R3为氢或C1-C4-烷基或R2和R3 一起形成双键，R4是氢，C1-C4-烷基，羟基或C1-C4-烷氧基，R5是氢或C1-C4-烷基或R4和R5与它们所连接的碳原子一起形成羰基 基团，R 6，R 7和R 8各自相同或不同，独立地为氢，C 1 -C 4 - 烷基或C 2 -C 4 - 烯基，C 3 -C 7 - 环烷基，羟基，C 1 -C 4 - 烷氧基，C 1 -C 4羟烷基， 硫醇，C 1-4 - 烷硫基，C 1-4 - 烷基硫醇，卤素，三氟甲基，硝基或任选取代的氨基，X是-CHR 9 - （CHR 10）m - ，m是0或1，并且R 9和R 10各自相同或 独立地为氢或C 1 -C 4 - 烷基; 或其药学上可接受的酯或其盐，描述了它们的制备，用途和包含它们的药物组合物。 该化合物对α2受体具有亲和性，并且可用于例如 在治疗高血压，青光眼，慢性或急性疼痛，偏头痛，腹泻，感冒，局部缺血，化学物质成瘾，焦虑症，特别是术前焦虑和不同的神经系统，肌肉骨骼，精神和认知障碍或麻醉的辅助治疗。

    Imidazole derivatives having affinity for &agr;2 receptors
    8.
    发明授权
    Imidazole derivatives having affinity for &agr;2 receptors 有权
    对α2受体具有亲和力的咪唑衍生物

    公开(公告)号：US06479530B2

    公开(公告)日：2002-11-12

    申请号：US09904836

    申请日：2001-07-16

    申请人： Arto Karjalainen ,  Paavo Huhtala ,  Juha-Matti Savola ,  Siegfried Wurster ,  Maire Eloranta ,  Maarit Hillilä ,  Raimo Saxlund ,  Victor Cockcroft ,  Arja Karjalainen

    发明人： Arto Karjalainen ,  Paavo Huhtala ,  Juha-Matti Savola ,  Siegfried Wurster ,  Maire Eloranta ,  Maarit Hillilä ,  Raimo Saxlund ,  Victor Cockcroft ,  Arja Karjalainen

    IPC分类号： A61K314164

    CPC分类号： C07D233/56 ,  C07D233/64

    摘要： Imidazole derivatives of formula I wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.

    摘要翻译： 式I的咪唑衍生物，其中n为0或1，R 1为氢或C 1 -C 4 - 烷基，R 2为氢或R 2和R 3一起形成双键，R 3为氢或C 1 -C 4烷基或R 2和R 3一起形成 R 2是氢，C 1 -C 4 - 烷基，羟基或C 1 -C 4 - 烷氧基，R 5是氢或C 1 -C 4 - 烷基或R 4和R 5与它们所连接的碳原子一起形成羰基，R 6 ，R 7和R 8各自相同或不同，独立地为氢，C 1 -C 4 - 烷基或C 2 -C 4 - 烯基，C 3 -C 7 - 环烷基，羟基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 羟基烷基，硫醇，C 1 4-烷硫基，C 1-4 - 烷基硫醇，卤素，三氟甲基，硝基或任选取代的氨基，X是-CHR 9 - （CHR 10）m - ，m是0或1，并且R 9和R 10各自相同或不同， 独立地是氢或C 1 -C 4 - 烷基; 或其药学上可接受的酯或其盐，描述了它们的制备，用途和包含它们的药物组合物。 该化合物对α2受体具有亲和性，并且可用于例如 在治疗高血压，青光眼，慢性或急性疼痛，偏头痛，腹泻，感冒，局部缺血，化学物质成瘾，焦虑症，特别是术前焦虑和不同的神经系统，肌肉骨骼，精神和认知障碍或麻醉的辅助治疗。