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11 条记录 (耗时 0.036 秒)

    Pyrazoloquinolinone derivatives as protein kinase C inhibitors
    2.
    发明授权
    Pyrazoloquinolinone derivatives as protein kinase C inhibitors 失效
    吡唑啉酮衍生物作为蛋白激酶C抑制剂

    公开(公告)号：US06686373B2

    公开(公告)日：2004-02-03

    申请号：US10191593

    申请日：2002-07-09

    申请人： Kiyoshi Kawamura ,  Sachiko Mihara ,  Seiji Nukui ,  Chikara Uchida

    发明人： Kiyoshi Kawamura ,  Sachiko Mihara ,  Seiji Nukui ,  Chikara Uchida

    IPC分类号： A61K314745

    CPC分类号： C07D471/04

    摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein the dashed lines represent optional double bonds; C1, C2, C3 and C4 are carbon atom; R1 is C1-4 alkyl; R2 is H, amino, etc.; R3 is H, halo-CH2—, C2-8 alkyl or Q1-, wherein said C2-8 alkyl is optionally substituted with up to 3 substituents selected from halo, C1-3 alkyl, R4(R5)N, etc.; R4 is H, C1-7 alkyl, etc.; R5 is H, C1-7alkyl, etc.; R6 and R7 are independently selected from H and C1-4 alkyl; R8 is aryl or heteroaryl; Q1 is a 4-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 4 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4 alkyl, etc.; Y5, Y6, Y7 and Y8 are hydrogen; Y1, Y2, Y3 and Y4 are independently selected from hydrogen, halo, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 3 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4alkyl-, etc.; These compounds have protein kinase C inhibitory activity and thus are useful for the treatment of neuropathic pain, acute or chronic inflammatory pain, auditory deficiency (synaptic repair), or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中虚线表示任选的双键; C 1，C 2，C 3和C 4是碳原子; R 1是C 1-4烷基; R 2是H，氨基等; R 3是H，卤代-CH 2 - ，C 2-8烷基或Q 1 - ，其中所述C 2-8烷基任选被至多3个选自卤素，C 1-3烷基，R 4， （R 5）N等; R 4是H，C 1-7烷基等; R 5是H，C 1-7烷基等; R 6和R 7独立地选自H和C 1-4烷基; R 8是芳基或杂芳基; Q 1是4-12元单环或双环芳族，部分饱和或完全饱和的环，任选地含有至多4个选自O，N和S的杂原子，并且任选地被卤素，C 1-4烷基等取代; Y 5，Y 6，Y 7和Y 8是氢; Y 1，Y 2，Y 3和Y 4独立地选自氢，卤素等; Q 2是5-12元单环或双环芳族，部分饱和或完全饱和的环，任选地含有至多3个选自O，N和S的杂原子，并且任选被卤素，C 1-4烷基等取代; 这些化合物具有蛋白激酶C抑制活性，因此可用于治疗哺乳动物，特别是人类的神经性疼痛，急性或慢性炎性疼痛，听觉缺陷（突触修复）等。 本发明还提供了包含上述化合物的药物组合物。

    Indazole derivatives
    3.
    发明授权
    Indazole derivatives 失效
    吲唑衍生物

    公开(公告)号：US07906532B2

    公开(公告)日：2011-03-15

    申请号：US11995179

    申请日：2006-07-14

    申请人： Asako Ishibashi ,  Tomoki Kato ,  Kiyoshi Kawamura ,  Sachiko Mihara ,  Mikio Morita

    发明人： Asako Ishibashi ,  Tomoki Kato ,  Kiyoshi Kawamura ,  Sachiko Mihara ,  Mikio Morita

    IPC分类号： A61K31/454 ,  A61K31/416 ,  C07D211/56 ,  C07D231/56

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/14

    摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中：R1，R2，R3，A和m各自如本文所述，含有这些化合物的组合物和这些化合物在治疗中的用途 由5-HT4激动活性介导的病症，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃肠疾病 恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病和呼吸暂停综合征。

    Indazole Derivatives
    4.
    发明申请
    Indazole Derivatives 失效
    吲唑衍生物

    公开(公告)号：US20080269211A1

    公开(公告)日：2008-10-30

    申请号：US11995179

    申请日：2006-07-14

    申请人： Asako Ishibashi ,  Tomoki Kato ,  Kiyoshi Kawamura ,  Sachiko Mihara ,  Mikio Morita

    发明人： Asako Ishibashi ,  Tomoki Kato ,  Kiyoshi Kawamura ,  Sachiko Mihara ,  Mikio Morita

    IPC分类号： A61K31/416 ,  A61P1/00 ,  A61P25/00 ,  A61P9/00 ,  C07D401/12 ,  C07D405/14 ,  A61K31/5377 ,  C07D403/12 ,  C07D413/14 ,  C07D401/14 ,  A61K31/454

    CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/14

    摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中：R 1，R 2，R 3， A和m各自如本文所述，含有这些化合物的组合物和这些化合物在治疗由5-HT 4激动剂活性介导的病症中的用途，例如但不限于胃食管反流 疾病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默氏病，认知障碍，呕吐，偏头痛， 神经疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病和呼吸暂停综合征。