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Human glucagon-like peptide-1 modulator and its use in the treatment of diabetes and related conditions

机译:人胰高血糖素样肽1调节剂及其在糖尿病和相关疾病中的应用

摘要

The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified compounds that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The compounds of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
机译:本发明提供了新颖的人胰高血糖素样肽-1(GLP-1)-受体调节剂,其生物学活性类似于或优于天然GLP-1肽,因此可用于治疗或预防与GLP活性有关的疾病或失调。此外,本发明提供了新颖的,化学修饰的化合物,其不仅刺激II型糖尿病患者的胰岛素分泌,而且还产生其他有益的促胰岛素反应。这些合成的肽GLP-1受体调节剂显示出对蛋白水解裂解的更高的稳定性,使其成为口服或肠胃外给药的理想治疗候选物。本发明的化合物在糖尿病功效模型中显示出所需的药代动力学性质和所需的效力。

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