Treatment of glaucoma and ocular hypertension using rho kinase inhibitors: patent evaluation of US2018244666 and US2018256595.

Treatment of glaucoma and ocular hypertension using rho kinase inhibitors: patent evaluation of US2018244666 and US2018256595.

Bonardi, Alessandro;Supuran, Claudiu T;
expert opinion on therapeutic patents 2019 pp. 1-7
260
bonardi2019treatmentexpert

Abstract

: 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. : 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. : 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.

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21137
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10.1080/13543776.2019.1658743
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