a Amakem Therapeutics NV , Agoralaan A Bis , Diepenbeek , Belgium.
b Cistim , Gaston Geenslaan 2 , Leuven , Belgium.
Expert Opin Ther Pat. 2017 Apr;27(4):507-515. doi: 10.1080/13543776.2017.1272579. Epub 2017 Jan 16.
The Rho-kinases (ROCK), ROCK1 and ROCK2, are potent, widespread biochemical modulators which have been extensively studied. Due to the involvement of ROCKs in multiple biological processes, ROCK inhibitors have pleiotropic actions and may be of relevance for a number of therapeutic applications. The drawback is however that their use might be limited by occurrence of side effects. Areas covered: Since the publication of the latest review in 2014, there have been significant advances in the field of ROCK inhibitors. In this paper we reviewed the patents published between September 2013 and September 2016. Recent novel molecules will be described. and progress from the compounds series described in the previous review as well as any new expected therapeutic uses for ROCK inhibitors that popped up in the last three years will be examined. Expert opinion: While a number of potential applications in human for ROCK inhibitors have been reported, very few molecules are currently available to patients. In addition to fasudil, ripasudil (K-115, Kowa) was only recently approved in Japan for the treatment of glaucoma (2014). Notwithstanding some failures and subsequent discontinuation, the Pipeline of preclinical and clinical ROCK inhibitors remains significant.
Rho 激酶（ROCK）、ROCK1 和 ROCK2 是强效、广泛存在的生化调节剂，已经得到了广泛的研究。由于 ROCK 参与了多种生物学过程，ROCK 抑制剂具有多种作用，可能与许多治疗应用有关。但缺点是，由于可能出现副作用，其使用可能会受到限制。
自 2014 年发表最新综述以来，ROCK 抑制剂领域取得了重大进展。本文综述了 2013 年 9 月至 2016 年 9 月期间公布的专利。将描述最近的新型分子，并对前一篇综述中描述的化合物系列的进展以及过去三年中出现的 ROCK 抑制剂的任何新的预期治疗用途进行检查。
虽然已经报道了 ROCK 抑制剂在人类中的许多潜在应用，但目前只有少数几种药物可供患者使用。除了法舒地尔，利帕舒地尔（K-115，高华）最近才在日本获得批准用于治疗青光眼（2014 年）。尽管有一些失败和随后的停药，但临床前和临床 ROCK 抑制剂的研发仍然具有重要意义。
