[EN] BIARYL AMIDE OR UREA DERIVATIVES AS TRPV1 LIGANDS<br/>[FR] DÉRIVÉS DE BIARYL AMIDE OU D'URÉE EN TANT QUE LIGANDS DE TRPV1
申请人:UNIV SIENA
公开号:WO2015162216A1
公开(公告)日:2015-10-29
The present invention relates to high affinity compounds, able to bind the transient receptor potential cation channel, subfamily Vanilloid, type 1 or TRPV1. Being this receptor involved in pain processing and neurogenic inflammatory responses and being up-regulated during chronic pain conditions, the compounds of the invention find particular application in all medical conditions involving said receptors, in particular as agents for pain therapy and/or anti-inflammatory and/or cluster headache therapy and/or anti-oxidant and/or anti-cancer therapy. Moreover, the chemical structure of these compounds provides the opportunity of developing new radiotracers for Positron Emission Tomography (PET) imaging. These radiotracers are of great relevance for mapping TRPV1 receptors in (patho)physiological conditions.
本发明涉及高亲和力化合物,能够结合瞬时受体电位阳离子通道,亚家族Vanilloid,类型1或TRPV1。由于这种受体参与疼痛处理和神经源性炎症反应,并且在慢性疼痛情况下上调,本发明的化合物在涉及该受体的所有医学状况中找到特定应用,特别是作为疼痛治疗和/或抗炎疗法和/或群集性头痛治疗和/或抗氧化剂和/或抗癌疗法的药物。此外,这些化合物的化学结构为开发新的正电子发射断层扫描(PET)成像的放射示踪剂提供了机会。这些放射示踪剂对于在(病理)生理条件下映射TRPV1受体具有重要意义。