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    Compounds Which Bind to the Active Site of Protein Kinase Enzymes
    9.
    发明申请
    Compounds Which Bind to the Active Site of Protein Kinase Enzymes 审中-公开
    绑定到蛋白激酶的活性位点的化合物

    公开(公告)号：US20090163515A1

    公开(公告)日：2009-06-25

    申请号：US10561914

    申请日：2004-07-01

    申请人： Veronique Birault ,  C. John Harris

    发明人： Veronique Birault ,  C. John Harris

    IPC分类号： A61K31/4965 ,  C07D241/10 ,  C07D213/02 ,  A61K31/44 ,  C07D215/00 ,  A61K31/47 ,  A61K31/444 ,  C07D239/24 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12

    CPC分类号： C07D213/74 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14

    摘要： The present invention relates to a compound and a group of compounds which are inhibitors of Rho kinase (ROK, ROCK). In addition, the invention relates to methods of treatment and use of the compounds in the manufacture of a medicament for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, glaucoma and AIDS. The compounds can be used in screening programmes against protein kinases. The invention also provides methods for making compounds and libraries that include these compounds.

    摘要翻译： 本发明涉及作为Rho激酶（ROK，ROCK）抑制剂的化合物和一组化合物。 此外，本发明涉及治疗和使用化合物在制备用于多种治疗适应症的药物中的应用的方法，包括心血管疾病（冠状动脉血管痉挛，高血压疾病，动脉硬化），中风，癌症，勃起功能障碍，哮喘 ，骨质疏松症，青光眼和艾滋病。 该化合物可用于抗蛋白激酶的筛选方案。 本发明还提供了制备包含这些化合物的化合物和文库的方法。

    Nitrogen Heteroaromatic Compounds Which Bind To The Active Site Of Protein Kinase Enzymes
    10.
    发明申请
    Nitrogen Heteroaromatic Compounds Which Bind To The Active Site Of Protein Kinase Enzymes 审中-公开
    绑定到蛋白激酶的活性位点的氮杂芳族化合物

    公开(公告)号：US20080194584A1

    公开(公告)日：2008-08-14

    申请号：US11667697

    申请日：2005-11-11

    申请人： Veronique Birault ,  Jose Antonio Bravo ,  Roger Crossley

    发明人： Veronique Birault ,  Jose Antonio Bravo ,  Roger Crossley

    IPC分类号： A61K31/444 ,  C07D401/04 ,  A61K31/4418 ,  C07D213/36 ,  G01N33/53 ,  A61P9/00 ,  A61P35/00 ,  A61P19/00 ,  A61K31/4709 ,  C07D401/14 ,  A61K31/4545 ,  A61K31/497

    CPC分类号： C07D213/75 ,  C07D213/38 ,  C07D213/74

    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.

    摘要翻译： 式（I）化合物或其药学上可接受的盐，水合物，溶剂合物，几何异构体，互变异构体，光学异构体或前药形式，其中X，Y，Z，R 1，R 2，R 3和R 4如本文所定义， 到蛋白激酶的活性位点。 特别地，它们是丝氨酸/苏氨酸激酶更特别是Rho激酶（ROK，ROCK）的抑制剂。 该化合物可用于治疗和制备用于多种治疗适应症的药物的方法，包括心血管疾病（冠状动脉血管痉挛，高血压疾病，动脉硬化），中风，癌症，勃起功能障碍，哮喘，骨质疏松症，AIDS或 眼病包括青光眼，年龄相关性黄斑变性，泪腺疾病或糖尿病性视网膜病变，或抑制神经突生长，因此需要神经细胞延伸和连接，神经元再生，诱导新的轴突生长和促进轴突（重新）接线， 修复由外伤（例如中风，创伤性脑损伤等）或神经变性（例如阿尔茨海默氏症，帕金森氏病等）引起的CNS神经元的损伤，修复和恢复以及治疗诸如脊髓损伤等疾病，并减少随后的影响 ，或由神经细胞损伤引起的疼痛，例如以下创伤或截肢，例如在治疗中 nt的神经性疼痛。