专利号:WO-2025128985-A1 优先权日:2023-12-14 标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.
专利号:WO-2025080818-A1 优先权日:2023-10-10 标 题:Combinations of fasn inhibitors and glp-1 agonists for liver diseases 发明人:O'FARRELL ANNE-MARIE; TSAI WEN-WEI 权利人:SAGIMET BIOSCIENCES INC 摘要:Combinations of fatty acid synthesis (FASN) inhibitors and glucagon-like peptide-1 (GLP-1) agonists for treating NAFLD/MAFLD, NASH/MASH, liver fibrosis and/or liver cirrhosis.
专利号:WO-2021018023-A1 优先权日:2019-08-01 标题:Small molecule glp-1 receptor modulator 发明人:XIE FANG; YU GUANGXIA; ZHANG SHUJUAN 权利人:THE TITAN LEADING MED TECH INC 摘要:The present invention provides a new compound for modulating a Glucagon-like peptide-1 (GLP-1) receptor, and a synthesis method therefor and a pharmaceutical use thereof. This kind of compound has an obvious agonistic effect on the GLP-1 receptor, but does not have an obvious binding effect on hERG, and therefore, it is indicated that the compound has a low risk of cardiotoxicity. The compound of the present invention can be used alone as a treatment medication for type II diabetes, or be used in combination with a polypeptide GLP-1 receptor agonist such as liraglutide, or be used in combination with the treatment medication for type II diabetes of other mechanisms.
专利号:CN-116102543-A 优先权日:2022-10-21 标题 :A kind of GLP-1R agonist, synthesis method and use thereof
1: Saxena AR, Gorman DN, Esquejo RM, Bergman A, Chidsey K, Buckeridge C, Griffith DA, Kim AM. Danuglipron (PF-06882961) in type 2 diabetes: a randomized, placebo-controlled, multiple ascending-dose phase 1 trial. Nat Med. 2021 Jun;27(6):1079-1087. doi: 10.1038/s41591-021-01391-w. Epub 2021 Jun 14. 25(3):805-814. doi: 10.1111/dom.14928. Epub 2022 Dec 19. 3: Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA. A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor. J Med Chem. 2022 Jun 23;65(12):8208-8226. doi: 10.1021/acs.jmedchem.1c01856. Epub 2022 Jun 1. 4: Saxena AR, Frias JP, Brown LS, Gorman DN, Vasas S, Tsamandouras N, Birnbaum MJ. Efficacy and Safety of Oral Small Molecule Glucagon-Like Peptide 1 Receptor Agonist Danuglipron for Glycemic Control Among Patients With Type 2 Diabetes: A Randomized Clinical Trial. JAMA Netw Open. 2023 May 1;6(5):e2314493. doi: 10.1001/jamanetworkopen.2023.14493.
合成参考文献
参考文献:10.1055/s-0041-1738304 摘要:Synthesis of Danuglipron: An Orally Available GLP-1R Agonist. Synfacts. 2022 Aug 18;18(09):1025. doi: 10.1055/s-0041-1738304.