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    • 9. 发明授权
    • 4-substituted piperidine derivatives
    • 4-取代的哌啶衍生物
    • US07572913B2
    • 2009-08-11
    • US11065696
    • 2005-02-24
    • Lisa McKerracherEryk ThouinWilliam LubellRobert SnowKarine Gingras
    • Lisa McKerracherEryk ThouinWilliam LubellRobert SnowKarine Gingras
    • C07D217/22C07D215/38A61K31/47
    • C07D211/74C07D211/58C07D211/72C07D401/06C07D403/12
    • Substituted piperidine compounds represented by the structure I are provided, wherein each of R1a, R1b, R1c, R1d, R1e, R1f, R1g, R1h, R2, R2A, R3, R4, A, X, a, x and n is as defined in the specification. Substituted piperidine compounds of structure I may permeate or penetrate across a nerve cell membrane into the interior of a nerve cell, may inhibit intracellular Rho kinase enzyme found in nerve cells in mammals, and may find utility in repair of damaged nerves in the central and peripheral nervous system of such mammals. These compounds may induce the regeneration or growth of neurites in mammalian nerve cells and may thereby induce regeneration of damaged or diseased nerve tissue. These compounds also find additional utility as antagonists of the enzyme Rho kinase in treatment of disease states in which Rho kinase is implicated. Pharmaceutical compositions containing these substituted piperidine compounds may be useful to promote neurite growth and in the treatment of diseases in which Rho kinase inhibition is indicated.
    • 提供由结构I表示的取代的哌啶化合物,其中R1a,R1b,R1c,R1d,R1e,R1f,R1g,R1h,R2f,R1g,R1h,R2,R2A,R3,R4,A,X,a,x和n如 在规范中。 结构I的取代的哌啶化合物可渗透或穿过神经细胞膜进入神经细胞的内部,可以抑制哺乳动物神经细胞中发现的细胞内Rho激酶,并可用于修复中枢和外周的受损神经 这些哺乳动物的神经系统。 这些化合物可诱导哺乳动物神经细胞中神经突的再生或生长,从而诱导损伤或患病神经组织的再生。 这些化合物在治疗其中涉及Rho激酶的疾病状态中也发现作为Rho激酶的拮抗剂的附加效用。 含有这些取代的哌啶化合物的药物组合物可用于促进神经突生长和治疗其中指示Rho激酶抑制的疾病。