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前列腺素受体激动剂作为抗青光眼药物(专利审查 2013-2018 年)。

Prostaglandin receptor agonists as antiglaucoma agents (a patent review 2013 - 2018).

机构信息

NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, University of Florence , Florence , Italy.

出版信息

Expert Opin Ther Pat. 2019 Oct;29(10):793-803. doi: 10.1080/13543776.2019.1661992. Epub 2019 Sep 4.

DOI:10.1080/13543776.2019.1661992
PMID:31462124
Abstract

: Elevated intraocular pressure (IOP) is the most prevalent risk factor for glaucoma. Prostaglandin analogs are a first-line therapy for glaucoma due to their ability to reduce IOP, once-daily dosing, efficacy, and minimal side-effect profile. Many compounds targeting different PG receptors have been developed in the last years, some of them being in clinical use. Latanoprost, Bimatoprost, Travoprost, and Tafluprost are clinically used as antiglaucoma drugs and act as agonists of the PGF2α receptor. The inability to fully understand the mechanism of action of clinically used PGF2α analogs is thus a strong driver for additional research into the mechanism of action of ocular hypotensive drugs belonging to this class of pharmacological agents. : This review explores the last 5 years (2013-2018), where many patents describing new compounds acting on different prostaglandin receptors, and mainly targeting EP1-4 and FP receptors, were released. : To date, there has been a growing awareness over recent years of the therapeutic use of novel derivatives as new antiglaucoma pharmaceutical products. Patents involved in discovering new approaches and new molecules for the treatment of glaucoma diseases encouraged the scientific community to increase the variety of drugs available for the treatment of ocular diseases.

摘要

眼压升高(IOP)是青光眼最常见的危险因素。前列腺素类似物是治疗青光眼的一线药物,因为它们具有降低眼压、每日一次给药、疗效和最小的副作用特征。近年来,已经开发出许多针对不同 PG 受体的化合物,其中一些已在临床应用。拉坦前列素、比马前列素、曲伏前列素和他氟前列素作为青光眼药物在临床上使用,作用于 PGF2α 受体激动剂。因此,无法完全了解临床使用的 PGF2α 类似物的作用机制是对属于该类药物的眼部降压药物作用机制进行额外研究的强大动力。

本文综述了过去 5 年(2013-2018 年)发布的许多专利,这些专利描述了作用于不同前列腺素受体的新型化合物,主要针对 EP1-4 和 FP 受体。

近年来,人们越来越意识到新型衍生物在治疗青光眼等疾病方面的治疗用途。涉及发现治疗青光眼疾病的新方法和新分子的专利鼓励科学界增加可用于治疗眼部疾病的药物种类。

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Prostaglandin receptor agonists as antiglaucoma agents (a patent review 2013 - 2018).前列腺素受体激动剂作为抗青光眼药物(专利审查 2013-2018 年)。
Expert Opin Ther Pat. 2019 Oct;29(10):793-803. doi: 10.1080/13543776.2019.1661992. Epub 2019 Sep 4.
2
Investigational drugs targeting prostaglandin receptors for the treatment of glaucoma.用于治疗青光眼的靶向前列腺素受体的研究性药物。
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Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cells.眼内压降低的FP前列腺素(PG)类似物:PG受体亚型结合亲和力和选择性,以及在培养细胞中对FP和其他PG受体的激动剂效力。
J Ocul Pharmacol Ther. 2003 Dec;19(6):501-15. doi: 10.1089/108076803322660422.
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Prostanoids in the therapy of glaucoma.前列腺素类药物在青光眼治疗中的应用
Cardiovasc Drug Rev. 2006 Spring;24(1):1-10. doi: 10.1111/j.1527-3466.2006.00001.x.
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Prostaglandins in the eye: Function, expression, and roles in glaucoma.眼部的前列腺素:功能、表达及其在青光眼中的作用
Ophthalmic Genet. 2017 Mar-Apr;38(2):108-116. doi: 10.3109/13816810.2016.1164193. Epub 2016 Apr 12.
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Comparative efficacy and tolerability of topical prostaglandin analogues for primary open-angle glaucoma and ocular hypertension.局部用前列腺素类似物治疗原发性开角型青光眼和高眼压症的疗效及耐受性比较
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Prostaglandin analogues and mouse intraocular pressure: effects of tafluprost, latanoprost, travoprost, and unoprostone, considering 24-hour variation.前列腺素类似物与小鼠眼压:考虑24小时眼压变化,探讨他氟前列素、拉坦前列素、曲伏前列素和乌诺前列酮的作用
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Effects of prostaglandin analogues on aqueous humor outflow pathways.前列腺素类似物对房水流出途径的影响。
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Effects of pre-surgical administration of prostaglandin analogs on the outcome of trabeculectomy.术前给予前列腺素类似物对小梁切除术预后的影响。
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Responses of intraocular pressure and the pupil of feline eyes to prostaglandin EP1 and FP receptor agonists.猫眼中眼压和瞳孔对前列腺素EP1和FP受体激动剂的反应。
Invest Ophthalmol Vis Sci. 1999 Nov;40(12):3047-53.

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Synthesis, Characterization, and Docking Studies of 1,4-dien as a Potential Impurity in Bimatoprost Drug.比马前列素药物中潜在杂质1,4 - 二烯的合成、表征及对接研究
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Discovery of water-soluble semicarbazide-containing sulfonamide derivatives possessing favorable anti-glaucoma effect and drug-like properties.具有良好抗青光眼作用和类药物性质的含氨基脲磺酰胺衍生物的发现。
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Indian J Ophthalmol. 2023 May;71(5):1768-1776. doi: 10.4103/IJO.IJO_2706_22.
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