申请人:SIGNAL PHARMACEUTICALS, INC.
公开号:EP2065383A1
公开(公告)日:2009-06-03
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.
本发明涉及吲唑化合物或其药学上可接受的盐、溶液剂和水合物。吲唑化合物可用于治疗或预防对激酶的抑制、调节或调控有反应的多种疾病和失调,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、肾脏疾病、自身免疫性疾病、黄斑变性、与疾病相关的消瘦、与石棉相关的疾病、肺动脉高压、糖尿病、肥胖症、疼痛等。因此,本发明还公开了治疗或预防此类疾病和失调的方法,以及包含一种或多种吲唑化合物的药物组合物。本发明部分基于对一类新型 5-三唑取代的吲唑分子的发现,该类分子在调节蛋白激酶方面具有强效活性。因此,本发明包括口服活性分子和肠外活性分子,这些分子可以较低的剂量或血清浓度用于治疗与蛋白激酶信号转导有关的疾病或紊乱。