Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
[EN] NOVEL GLP-1 RECEPTOR STABILIZERS AND MODULATORS<br/>[FR] NOUVEAUX STABILISANTS ET MODULATEURS DU RÉCEPTEUR DE GLP-1
申请人:RECEPTOS INC
公开号:WO2012166951A9
公开(公告)日:2013-02-21
US9278910B2
申请人:——
公开号:US9278910B2
公开(公告)日:2016-03-08
US9700543B2
申请人:——
公开号:US9700543B2
公开(公告)日:2017-07-11
Functionalization of Organotrifluoroborates via Cu-Catalyzed C-N Coupling Reaction
作者:Jung-Hyun Lee、Heejin Kim、Taejung Kim、Jung Ho Song、Won-Suk Kim、Jungyeob Ham
DOI:10.5012/bkcs.2013.34.1.42
日期:2013.1.20
Potassium N-heterobiaryltrifluoroborates were successfully prepared via a selective Cu-catalyzed C-N coupling reaction. The BF3K moiety was well tolerated under the reaction conditions involving CuI and dimethylethylenediamine (DMEDA) in the presence of DMSO. The Pd-catalyzed Suzuki-Miyaura cross couplings of potassium N-heterobiaryltrifluoroborates with bromoarenes were studied to prepare the N-heterotriaryl
通过选择性Cu催化的CN偶联反应成功制备了N-杂二芳基三氟硼酸钾。在 DMSO 存在下,在涉及 CuI 和二甲基乙二胺 (DMEDA) 的反应条件下,BF3K 部分具有良好的耐受性。研究了Pd催化的N-杂二芳基三氟硼酸钾与溴代芳烃的Suzuki-Miyaura交叉偶联制备N-杂三芳基化合物。此外,N-杂二芳基三氟硼酸钾的同源偶联、碘化和羟基化以高产率提供了相应的产物。