204636-94-2Relevant academic research and scientific papers
Potent and orally bioavailable GPR142 agonists as novel insulin secretagogues for the treatment of type 2 diabetes
Toda, Narihiro,Hao, Xiaolin,Ogawa, Yasuyuki,Oda, Kozo,Yu, Ming,Fu, Zice,Chen, Yi,Kim, Yongjae,Lizarzaburu, Mike,Lively, Sarah,Lawlis, Shauna,Murakoshi, Michiko,Nara, Futoshi,Watanabe, Nobuaki,Reagan, Jeff D.,Tian, Hui,Fu, Angela,Motani, Alykhan,Liu, Qingxiang,Lin, Yi-Jyun,Zhuang, Run,Xiong, Yumei,Fan, Peter,Medina, Julio,Li, Leping,Izumi, Masanori,Okuyama, Ryo,Shibuya, Satoshi
, p. 790 - 794 (2013/09/02)
GPR142 is a G protein-coupled receptor that is predominantly expressed in pancreatic β-cells. GPR142 agonists stimulate insulin secretion in the presence of high glucose concentration, so that they could be novel insulin secretagogues with reduced or no risk of hypoglycemia. We report here the optimization of HTS hit compound 1 toward a proof of concept compound 33, which showed potent glucose lowering effects during an oral glucose tolerance test in mice and monkeys.
N-ARYL PYRAZOLE COMPOUNDS FOR USE AGAINST DIABETES
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Page/Page column 24; 39, (2008/06/13)
Compounds having formula I:where A1, A2, L, V, W, R1, R2, R3, R4 and R5 are as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2 diabetes-related conditions are provided herein.
Stereoselective synthesis of 2',3'-dideoxy-nucleosides via intramolecular glycosylation of phenyl 1-seleno-glycosides. Synthesis of 2',3'-dideoxythymidine
Lluis, Jordi,Matheu, Ma. Isabel,Castillon, Sergio
, p. 1807 - 1810 (2007/10/03)
4-methoxy and 4-(2-trimethylsilylethoxy)pyrimidine bases were attached to the 5-position of the phenyl 2,3-dideoxy-1-seleno-glycero-pentofuranoside moiety. The presence of the silyl protecting group in the base is necessary to lead to neutral β-anhydro nucleosides by intramolecular glycosylation. The subsequent ring opening affords 3'-deoxythymidine with complete stereocontrol.
