6-(4-(甲基磺酰基)苯基)吡啶-3-醇,(1-(3-Isopropyl-1,2,4-Oxadiazol-5-yl)Piperidin-4-yl)Methanol置于偶氮二甲酸二异丙酯,三苯基膦体系中,用 四氢呋喃 用作溶剂,化学反应 4.0H,反应生成Gsk 1292263; 5-[[[1-(3-异丙基-1,2,4-噁二唑-5-基)-4-哌啶基]甲基]氧基]-2-[4-(甲磺酰基)苯基]吡啶 参考文献:Bicyclic Compounds And Use As Antidiabetics 标题:Bicyclic Compounds And Use As Antidiabetics 摘要:本发明涉及一种新型化合物,该化合物在治疗代谢性疾病,特别是ⅱ型糖尿病及相关疾病方面具有用途,并且还涉及制备和使用这种化合物的方法.
专利号:US-2018230127-A1 优先权日:2015-08-13 标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds 发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID 权利人:PFIZER 摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.
专利号:US-10316018-B2 优先权日:2015-08-27 标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators 发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG 权利人:PFIZER 摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Yang JW, Kim HS, Im JH, Kim JW, Jun DW, Lim SC, Lee K, Choi JM, Kim SK, Kang KW. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2015 Sep 23. pii: fj.15-273771. [Epub ahead of print] doi: 10.1371/journal.pone.0092494. eCollection 2014. 3: Kang SU. GPR119 agonists: a promising approach for T2DM treatment? A SWOT analysis of GPR119. Drug Discov Today. 2013 Dec;18(23-24):1309-15. doi: 10.1016/j.drudis.2013.09.011. Epub 2013 Sep 20. Review. doi: 10.3109/00498254.2012.739719. Epub 2012 Dec 21.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749