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    • 10. 发明授权
    • Pyrazoloquinolinone derivatives as protein kinase C inhibitors
    • 吡唑啉酮衍生物作为蛋白激酶C抑制剂
    • US06686373B2
    • 2004-02-03
    • US10191593
    • 2002-07-09
    • Kiyoshi KawamuraSachiko MiharaSeiji NukuiChikara Uchida
    • Kiyoshi KawamuraSachiko MiharaSeiji NukuiChikara Uchida
    • A61K314745
    • C07D471/04
    • 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.
    • 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。