Polycyclic compounds as soluble epoxide hydrolase inhibitors

S. Codony , E. Valverde , C. Galdeano , A.L. Turcu , R. Leiva , S. Vázquez
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Abstract

In this invention, a novel family of benzohomoadamantane-based soluble epoxide hydrolase inhibitors is disclosed. The benzohomoadamantane scaffold is a polycyclic, readily accessible, system that features a homoadamantane unit fused with an aromatic ring. Although it has been scarcely used in medicinal chemistry, it is very versatile and permits several chemical derivatizations in its structure in order to improve the inhibitory activity and/or the DMPK properties of the compounds. This invention encompasses ureas, amides, carbamates and thioureas. The compounds are of interest for the broad range of therapeutic indications related to the inhibition of soluble epoxide hydrolase, including inflammatory diseases, pain and neurodegeneration. This invention has been licensed to a US-based start-up that is actively recruiting investors and strategic partners for advancing a selected candidate to regulatory studies.
多环化合物作为可溶性环氧化物水解酶抑制剂
在本发明中,公开了一种新的苯并同源金刚烷基可溶性环氧化物水解酶抑制剂家族。苯并精金刚烷支架是一种多环、易于获取的体系,其特征是精金刚烷单元与芳香环融合。虽然它在药物化学中很少使用,但它是非常通用的,并且允许在其结构中进行几种化学衍生,以提高化合物的抑制活性和/或DMPK性质。本发明包括脲类、酰胺类、氨基甲酸酯类和硫脲类。这些化合物对与可溶性环氧化物水解酶抑制相关的广泛治疗指征感兴趣,包括炎症性疾病、疼痛和神经变性。这项发明已被授权给一家美国初创公司,该公司正在积极招募投资者和战略合作伙伴,以推进选定的候选药物进行监管研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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