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FGF21 derivatives having albumin binder ABCDE and their use

机译:具有白蛋白结合剂ABCDE的FGF21衍生物及其用途

摘要

The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B-C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.
机译:本发明涉及成纤维细胞生长因子21(FGF21),更特别地涉及具有共价连接的式A-B-C-D-E-的白蛋白结合物的FGF21化合物的衍生物。本发明还涉及新颖的FGF21类似物,以及这些FGF21衍生物和类似物的药物用途,特别是用于治疗糖尿病,血脂异常,肥胖,心血管疾病,代谢综合征和/或非酒精性脂肪肝疾病( NAFLD)。本发明的衍生物是持久的,例如。能够长时间维持低血糖水平,能够增加FGF21的体内半衰期,和/或导致FGF21的清除率降低。此外,本发明的衍生物优选具有改善的氧化稳定性。

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