5-羟基烟酸置于硼烷四氢呋喃络合物体系中,用 四氢呋喃 用作溶剂,以32.2%的收率获得3-溴吡啶-5-甲醇 参考文献: Novel Fxr (Nr1H4 ) Binding And Activity Modulating Compounds[fr] Nouveaux Composés Se Liant Au Fxr (Nr1 H4) Et Modulant Son Activité 标题: Novel Fxr (Nr1H4 ) Binding And Activity Modulating Compounds[fr] Nouveaux Composés Se Liant Au Fxr (Nr1 H4) Et Modulant Son Activité 摘要:本发明涉及结合nr1 H4受体(fxr)并作为nr1 H4受体(fxr)激动剂的化合物.该发明还涉及利用这些化合物制备药物用于通过这些化合物结合所述核受体治疗疾病和/或症状,并涉及这些化合物的合成过程.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
专利号:US-2018065917-A1 优先权日:2016-09-02 标 题 :Immune checkpoint inhibitors, compositions and methods thereof 发明人:WEBBER STEPHEN E; ALMASSY ROBERT J 权利人:POLARIS PHARMACEUTICALS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. n n n n n n n n n n For Formula (I) compounds R 1 , R 2 , X 1 , Y 1 and n are as defined in the specification. The inventive Formula (I) compounds are inhibitors of the PD-1/PD-L1 protein/protein binding or functional interaction and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer and infectious diseases.
专利号:CN-114716363-A 优先权日:2022-05-07 标 题:A new type of pyridine quaternary ammonium salt compound containing hydroxyl, its synthesis method and its application in fiber antibacterial modification
专利号:CN-103626693-B 优先权日:2012-08-28 标题:A class of pleuromutilin derivatives, its pharmaceutical composition and its synthesis method and application
专利号:CN-116120226-A 优先权日:2022-12-28 标 题 :Synthesis process of 5-hydroxymethyl nicotinonitrile
参考文献:10.1055/s-0033-1340740 摘要:Breinbauer R, Trobe M, Peters M, Grimm S. The Development of a Modular Synthesis of Teraryl-Based α-Helix Mimetics as Potential Inhibitors of Protein–Protein Interactions. Synlett. 2014 Apr 02;25(09):1202–14. doi: 10.1055/s-0033-1340740.