INSERM U648, Université Paris Descartes, 4 avenue de l'observatoire, 75006 Paris, France.
Expert Opin Ther Pat. 2010 Mar;20(3):377-404. doi: 10.1517/13543770903524284.
Abnormalities in protein phosphorylation by cyclin-dependent kinases (CDKs) have been observed in numerous major human diseases, which has strongly encouraged the search for pharmacological inhibitors. Almost 10 years after the first compounds entered clinical studies, numerous CDK inhibitors with differing selectivity profiles are now undergoing preclinical and clinical evaluation. Nevertheless, these intensive searches have not yet resulted in drug approvals.
This paper reviews patent activity associated with these efforts during the 2005 - 2008 period.
Readers will rapidly obtain an overview of the majority of CDK inhibitor scaffolds; they will discover which companies are the main players in the field and acquire information on products that have reached the clinical phases.
In most cases, applications have been claimed in the field of cancer; however, potential applications of CDK inhibitors in other therapeutic areas are regularly reported and could herald therapeutic introduction over the next few years.
异常的蛋白磷酸化周期蛋白依赖性激酶(CDKS)已被观察到在众多重大人类疾病,这强烈鼓励了对药理学抑制剂的研究。近 10 年的第一化合物进入临床研究后,许多 CDK 抑制剂具有不同的选择性谱正在进行临床前和临床评价。然而,这些密集的搜索尚未导致药物批准。
本文综述了专利活动与这些努力在 2005 - 2008 年期间。
读者将迅速获得一个概述的大多数的 CDK 抑制剂支架;他们将发现哪些公司是主要的参与者在该领域,并获得有关产品已达到的临床阶段的信息。
在大多数情况下,应用已被要求在癌症领域;然而,CDK 抑制剂在其他治疗领域的潜在应用经常报道,并预示着治疗引入在未来几年。