■目前正在寻找针对过氧化物酶体增殖物激活受体(PPAR)的新型化合物,从以前成功识别的选择性开始,双重或泛激动剂。在过去的几年里,研究人员的努力主要是发现PPARγ和δ调节剂,激动剂和拮抗剂,选择性或具有双重多目标轮廓。其中一些化合物目前正在临床试验中,用于治疗原发性胆汁性肝硬化,非酒精性脂肪性肝病,肝,和肾脏疾病。
■对在2020-2023年范围内沉积的专利进行了批判性分析。发现的新化合物被归类为选择性PPAR调节剂,双靶点和多靶点PPAR受体激动剂。还讨论了PPAR配体与其他药物的联合使用,以及为他们提出的新的治疗适应症。
■从专利文献的分析来看,当前新兴的景观认为有必要获得PPAR多目标化合物,具有对三种亚型的平衡效力和调节不同靶标的能力。这种多目标行动作为一种治疗复杂疾病的新方法,具有很大的前景。作为新陈代谢,炎症性疾病,和癌症。PPAR配体在免疫治疗领域的应用也开启了一个创新的场景,这可能值得进一步应用。
UNASSIGNED: The search for novel compounds targeting Peroxisome Proliferator-Activated Receptors (PPARs) is currently ongoing, starting from the previous successfully identification of selective, dual or pan agonists. In last years, researchers\' efforts are mainly paid to the discovery of PPARγ and δ modulators, both agonists and antagonists, selective or with a dual-multitarget profile. Some of these compounds are currently under clinical trials for the treatment of primary biliary cirrhosis, nonalcoholic fatty liver disease, hepatic, and renal diseases.
UNASSIGNED: A critical analysis of patents deposited in the range 2020-2023 was carried out. The novel compounds discovered were classified as selective PPAR modulators, dual and multitarget PPAR agonists. The use of PPAR ligands in combination with other drugs was also discussed, together with novel therapeutic indications proposed for them.
UNASSIGNED: From the analysis of the patent literature, the current emerging landscape sees the necessity to obtain PPAR multitarget compounds, with a balanced potency on three subtypes and the ability to modulate different targets. This multitarget action holds great promise as a novel approach to complex disorders, as metabolic, inflammatory diseases, and cancer. The utility of PPAR ligands in the immunotherapy field also opens an innovative scenario, that could deserve further applications.