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Abstract：
UNASSIGNED: Group II metabotropic glutamate (mGlu) receptors have emerged as an attractive potential target for the development of novel CNS therapeutics in areas such as Alzheimer\'s disease (AD), anxiety, cognitive disorders, depression, and others. Several small molecules that act as negative allosteric modulators (NAMs) on these receptors have demonstrated efficacy and/or target engagement in animal models, and one molecule (decoglurant) has been advanced into clinical trials.
UNASSIGNED: This review summarizes patent applications published between January 2015 and November 2020. It is divided into three sections: (1) small molecule nonselective mGlu2/3 NAMs, (2) small molecule selective mGlu2 NAMs, and (3) small molecule selective mGlu3 NAMs.
UNASSIGNED: Much progress has been made in the discovery of novel small molecule mGlu2 NAMs. Still, chemical diversity remains somewhat limited and room for expansion remains. Progress with mGlu3 NAMs has been more limited; however, some promising molecules have been disclosed. The process of elucidating the precise role of each receptor in the diseases associated with group II receptors has begun. Continued studies in animals with selective NAMs for both receptors will be critical in the coming years to inform researchers on the right compound profile and patient population for clinical development.
UNASSIGNED: This review summarizes patent applications published between January 2015 and November 2020. It is divided into three sections: (1) small molecule nonselective mGlu2/3 NAMs, (2) small molecule selective mGlu2 NAMs, and (3) small molecule selective mGlu3 NAMs.
UNASSIGNED: Much progress has been made in the discovery of novel small molecule mGlu2 NAMs. Still, chemical diversity remains somewhat limited and room for expansion remains. Progress with mGlu3 NAMs has been more limited; however, some promising molecules have been disclosed. The process of elucidating the precise role of each receptor in the diseases associated with group II receptors has begun. Continued studies in animals with selective NAMs for both receptors will be critical in the coming years to inform researchers on the right compound profile and patient population for clinical development.
摘要：
■II组代谢型谷氨酸（mGlu）受体已成为在阿尔茨海默病（AD）等领域开发新的CNS疗法的有吸引力的潜在靶标，焦虑,认知障碍,抑郁症,和其他人。在这些受体上充当负变构调节剂（NAMs）的几种小分子已在动物模型中证明了功效和/或靶标参与，一个分子（脱胶剂）已经进入临床试验。
■本综述总结了2015年1月至2020年11月期间公布的专利申请。它分为三个部分：（1）小分子非选择性mGlu2/3NAMs，（2）小分子选择性mGlu2NAMs，和（3）小分子选择性mGlu3NAMs。
■在发现新型小分子mGlu2NAMs方面取得了很大进展。尽管如此，化学多样性仍然有限，扩张空间仍然存在。mGlu3NAM的进展较为有限；然而，一些有前途的分子已经被公开。阐明每种受体在与II组受体相关的疾病中的精确作用的过程已经开始。在未来几年中，对两种受体具有选择性NAM的动物进行持续研究将是至关重要的，以告知研究人员正确的化合物概况和患者群体以进行临床开发。
■本综述总结了2015年1月至2020年11月期间公布的专利申请。它分为三个部分：（1）小分子非选择性mGlu2/3NAMs，（2）小分子选择性mGlu2NAMs，和（3）小分子选择性mGlu3NAMs。
■在发现新型小分子mGlu2NAMs方面取得了很大进展。尽管如此，化学多样性仍然有限，扩张空间仍然存在。mGlu3NAM的进展较为有限；然而，一些有前途的分子已经被公开。阐明每种受体在与II组受体相关的疾病中的精确作用的过程已经开始。在未来几年中，对两种受体具有选择性NAM的动物进行持续研究将是至关重要的，以告知研究人员正确的化合物概况和患者群体以进行临床开发。
