Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China; Lilly China Innovation and Partnerships (LCIP), Eli Lilly & Company, 16F, Tower1 HKRI, Taikoo Hui 288 Shimenyi Road, Shanghai 200041, PR China.
Lilly China Research and Development Center (LCRDC), Eli Lilly & Company, Building 8, 338 Jia Li Lue Road, Shanghai 201203, PR China.
Bioorg Med Chem Lett. 2020 Mar 1;30(5):126857. doi: 10.1016/j.bmcl.2019.126857. Epub 2019 Dec 27.
The discovery and optimization of a novel series of GPR142 agonists are described. These led to the identification of compound 21 (LY3325656), which demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. Compound 21 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.
本文描述了一种新型 GPR142 激动剂的发现和优化。这些研究导致了化合物 21（LY3325656）的鉴定，该化合物在临床前研究中显示出抗糖尿病益处，并且具有适合人体给药的 ADME/PK 特性。化合物 21 是第一个进入 2 型糖尿病治疗的 GPR142 激动剂分子的 1 期临床试验。
