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102 条记录 (耗时 0.025 秒)

    Methods, compositions and compound assays for inhibiting amyloid-beta protein production
    52.
    发明公开
    Methods, compositions and compound assays for inhibiting amyloid-beta protein production 审中-公开
    用于抑制淀粉样β蛋白产生的方法，组合物和化合物测定

    公开(公告)号：EP2270513A2

    公开(公告)日：2011-01-05

    申请号：EP10174529.7

    申请日：2005-04-20

    申请人： Galapagos N.V.

    发明人： Merchiers, Pascal Gerard ,  Spittaels, Koenraad Frederik Florentina ,  Hoffmann, Marcel

    IPC分类号： G01N33/68 ,  G01N33/566

    CPC分类号： C12Q1/37 ,  G01N33/566 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/2821

    摘要： A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide (GPR6), or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

    摘要翻译： 鉴定抑制细胞中淀粉样-β前体蛋白加工的化合物的方法，包括使测试化合物与GPCR多肽（GPR6）或其片段接触，并测量与产生淀粉样-β肽有关的化合物-GPCR特性。 该方法的细胞分析测量包括第二信使和/或淀粉状蛋白β肽水平的指标。 治疗方法和包括有效抑制淀粉样蛋白前体加工量的GPCR表达抑制剂的药物组合物可用于治疗涉及认知障碍的病症，例如阿尔茨海默病。

    NITROGEN HETEROAROMATIC COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES
    56.
    发明公开
    NITROGEN HETEROAROMATIC COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES 审中-公开
    芳杂环含氮化合物遵循蛋白激酶BIND活性中心

    公开(公告)号：EP1814856A1

    公开(公告)日：2007-08-08

    申请号：EP05809312.1

    申请日：2005-11-11

    申请人： Galapagos N.V.

    发明人： BIRAULT, Veronique, BioFocus Discovery Limited ,  BRAVO, Jose, Antonio, BioFocus Discovery Limited ,  CROSSLEY, Roger, BioFocus Discovery Limited

    IPC分类号： C07D213/74 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/497

    CPC分类号： C07D213/74 ,  C07D213/75 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14

    摘要： Compounds of Formula (I) or pharmaceutically acceptable salts, hydrates, solvates, geometrical isomers, tautomers, optical isomers, or prodrug forms thereof, wherein X, Y, Z, R1, R2, R3 and R4 are as defined herein are capable of binding to the active site of protein kinase enzymes. In particular, they are inhibitors of a serine/ threonine kinase more particularly Rho kinase (ROK, ROCK). The compounds can be used in methods of treatment and in the manufacture of medicaments for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, AIDS or an ocular condition including glaucoma, age related macular degeneration, lacrimal gland disease, or diabetic retinopathy, or suppression of neurite growth and hence a condition requiring nerve cell extension and connectivity, neuronal regeneration, inducing new axonal growth and promotion of axonal (re)wiring, repairing damage to neurons in the CNS caused by trauma (eg stroke, traumatic brain injury etc.) or neurodegeneration (eg Alzheimer's, Parkinson's etc), repair and recovery from and treatment of disorders such as spinal cord injury and in reducing the subsequent effects thereof, or pain caused by nerve cell damage such as following trauma or amputation for example in the treatment of neuropathic pain.