申请人:Carmot Therapeutics, Inc.
公开号:US11535660B1
公开(公告)日:2022-12-27
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor (“GLP?1R”) and/or the gastric inhibitory polypeptide receptor (“GIPR”). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is beneficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancement of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple)-arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.
本公开的化学实体(如化合物或该化合物的药学上可接受的盐和/或水合物和/或原药)可调节(如激动或部分激动或拮抗)胰高血糖素样肽1受体("GLP?1R")和/或胃抑制多肽受体("GIPR")。这些化学实体是有用的,例如,用于治疗患有疾病、失调或病症的受试者(例如人类),在这种情况下,调节(例如,激动、部分激动或拮抗)GLP?1R 和/或 GIPR 的活性有利于治疗或预防潜在的病理和/或症状和/或疾病、失调或病症的进展。在一些实施方案中,调节的结果是增强(如增加)现有水平(如正常或低于正常水平)的GLP?1R和/或GIPR活性(如信号传导)。在某些实施方案中,本文所述的化学实体可进一步调节(如减弱、解除耦合)--相对于原生配体的信号转导。本公开还包括组合物以及使用和制造所述化学实体的其他方法。