NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence , Sesto Fiorentino (Florence) , Italy.
Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia.
Expert Opin Ther Pat. 2019 Oct;29(10):781-792. doi: 10.1080/13543776.2019.1679117. Epub 2019 Oct 15.
: Glaucoma affects more than 70 million people worldwide. One of the major therapeutic options for its management is based on the inhibition of the metalloenzyme carbonic anhydrases (CAs, EC 4.2.1.1). CA inhibitors (CAIs) diminish ocular hypertension in glaucomatous patients by reducing the rate of bicarbonate formation and thus, the secretion of the aqueous humor. : This review is intended to cover the major contributions in terms of patent literature reports for the treatment of ophthalmic diseases by means of CAIs in a time frame spanning from 2013 to date. : The patent literature is dominated by innovative pharmaceutical formulations including a CAI alone or in combination with other therapeutic agents. Very few novelties within drug discovery are currently present and they mainly account for new CAI moieties and classical CAIs merged into scaffolds bearing additional chemical functionalities beneficial for the pharmacological treatment of the disease. It is reasonable to expect that in the near future the so-called 'old drugs' will achieve pharmacological performances in the management of ocular hypertension beyond any expectations and thus open a new era of drug repurposing merely based on material science advancements.
青光眼影响着全球超过 7000 万人。其治疗的主要选择之一是基于金属酶碳酸酐酶（CA，EC 4.2.1.1）的抑制。CA 抑制剂（CAIs）通过降低碳酸氢盐的形成速度，从而减少房水的分泌，从而降低青光眼患者的眼内压。
本综述旨在涵盖 2013 年至今，通过 CAIs 治疗眼科疾病的专利文献报告中的主要贡献。专利文献主要由创新药物制剂主导，包括单独的 CAI 或与其他治疗剂联合使用。目前在药物发现方面几乎没有新的创新，它们主要涉及新的 CAI 部分和经典的 CAIs 融合到具有额外化学功能的支架中，这些功能有利于疾病的药理学治疗。合理的预期是，在不久的将来，所谓的“老药”在管理眼内高压方面将取得超乎想象的药理效果，从而仅仅基于材料科学的进步，开启药物再利用的新时代。
