226398-62-5Relevant articles and documents
Synthesis and Characterization of N-(4-(Piperidin-4-ylsulfonyl) phenyl)5-vinylpyrimidin-2-amine
Dong, Jingjing,Feng, Baicheng,Jin, Yan,Lu, Jianqiang,Wang, Tielin
, p. 255 - 258 (2021/08/05)
Target product N-(4-(piperidin-4-ylsulfonyl)phenyl)5-vinylpyrimidin-2- amine (13) was synthesized using 6-oxopyran-3-carbaldehyde (M1) and 4-hydroxypiperidine (M2) as starting materials by a series of nucleophilic substitution and oxidation. Different aci
UREA/CARBAMATES FAAH MAGL OR DUAL FAAH/MAGL INHIBITORS AND USES THEREOF
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Paragraph 0139, (2016/02/18)
Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL.
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)
Dragovich, Peter S.,Bair, Kenneth W.,Baumeister, Timm,Ho, Yen-Ching,Liederer, Bianca M.,Liu, Xiongcai,Liu, Yongbo,O'Brien, Thomas,Oeh, Jason,Sampath, Deepak,Skelton, Nicholas,Wang, Leslie,Wang, Weiru,Wu, Hongxing,Xiao, Yang,Yuen, Po-Wai,Zak, Mark,Zhang, Lei,Zheng, Xiaozhang
, p. 4875 - 4885 (2013/09/02)
Potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors containing 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas were identified using structure-based design techniques. The new compounds displayed improved aqueous solubilities, determined using a high-throughput solubility assessment, relative to previously disclosed urea and amide-containing NAMPT inhibitors. An optimized 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived compound exhibited potent anti-NAMPT activity (18; BC NAMPT IC50 = 11 nM; PC-3 antiproliferative IC50 = 36 nM), satisfactory mouse PK properties, and was efficacious in a PC-3 mouse xenograft model. The crystal structure of another optimized compound (29; NAMPT IC50 = 10 nM; A2780 antiproliferative IC50 = 7 nM) in complex with the NAMPT protein was also determined.