Treatment of glaucoma and ocular hypertension using rho kinase inhibitors: patent evaluation of US2018244666 and US2018256595. (3rd October 2019)

• Record Type: Journal Article
• Authors: Bonardi, Alessandro; Supuran, Claudiu T
• Is Part Of: Expert opinion on therapeutic patents. Volume 29:Number 10(2019)
• Page Start: 753
• Page End: 759
• Publication Date: 2019-10-03
• Subjects: Glaucoma -- ocular hypertension -- IOP -- rho kinase inhibitors -- netarsudil -- ripasudil; Drugs -- Patents -- Periodicals; 615.10272
• DOI: 10.1080/13543776.2019.1658743
• Languages: English
• ISSNs: 1354-3776

Abstract

ABSTRACT: Introduction : Glaucoma refers to a heterogeneous group of optic neuropathies characterized by an enhanced intraocular pressure (IOP). To date, there are six available different drug classes for the treatment of glaucoma and ocular hypertension: β-adrenergic antagonists, prostaglandins, carbonic anhydrase inhibitors, α2-selective adrenergic, muscarinic agonists and rho kinase inhibitors, which act by reducing the production or increasing the drainage of aqueous humor. Areas covered : This manuscript reviews patent US2018244666A1, that describes the synthesis of novel potential rho kinase and monoamine transporters inhibitors with a benzamide or isoquinoline amide scaffolds, and patent US2018256595A1 that investigates the long-term treatment of glaucoma or ocular hypertension with ripasudil, a rho kinase inhibitor. Expert opinion : A variety of netarsudil congeners were synthesized as rho kinases inhibitors in patent US2018244666A1. Results of patent US2018256595A1 showed that ripasudil is among the best candidates for glaucoma long-term treatment, as IOP continuously dropped over the course of the treatment.