公开(公告)号：EP2065383A1

公开(公告)日：2009-06-03

申请号：EP08022584.0

申请日：2004-11-19

申请人： SIGNAL PHARMACEUTICALS, INC.

发明人： Bhagwat, Shripad, S. ,  Satoh, Yoshitaka ,  Sakata, Steven, T. ,  Buhr, Chris, A. ,  Albers, Ronald ,  Sapienza, John ,  Plantevin, Veronique ,  Chao, Qi ,  Sahasrabudhe, Kiran ,  Stengone, Rachel ,  Narla, Rama, K.

IPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  A61K31/416 ,  A61K31/4196

CPC分类号： C07D403/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseses or disorders associated with protein kinase signal transduction.

摘要翻译： 本发明涉及吲唑化合物或其药学上可接受的盐，溶剂化物和水合物。 吲唑化合物可用于治疗或预防对抑制，调节或调节激酶（例如炎症性疾病，异常血管生成及其相关疾病，癌症，动脉粥样硬化，心血管疾病）的各种疾病和病症 肾脏疾病，自身免疫性疾病，黄斑变性，疾病相关性消耗，石棉相关病症，肺动脉高压，糖尿病，肥胖症，疼痛等。 因此，还公开了治疗或预防这些疾病和病症的方法，以及包含一种或多种吲唑化合物的药物组合物。 本发明部分地基于发现关于蛋白激酶调节具有强力活性的新一类5-三唑基取代的吲唑分子。 因此，本发明包括口服活性分子以及肠胃外活性分子，其可以以较低剂量或血清浓度使用，用于治疗与蛋白激酶信号转导相关的疾病或障碍。