📜4-Amino-N,N-Dicyclopropyl-6-Ethyl-1-Methyl-1,6-Dihydroimidazo[4,5-D]Pyrrolo[2,3-B]Pyridine-7-Carboxamide置于tris-(Dibenzylideneacetone)Dipalladium(0) 二碘甲烷,Caesium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽,亚硝酸异戊酯体系中,用 乙二醇二甲醚 用作溶剂,化学反应 6.0H,反应生成N,N-二环丙基-4-[(1,5-二甲基-1H-吡唑-3-基)氨基]-6-乙基-1,6-二氢-1-甲基-咪唑并[4,5-D]吡咯并[2,3-B]吡啶-7-甲酰胺 参考文献: Jak2 Inhibitors And Their Use For The Treatment Of Myeloproliferative Diseases And Cancer[fr] Inhibiteurs De Jak2 Et Leur Utilisation Pour Le Traitement De Maladies Myéloprolifératives Et Du Cancer 标题: Jak2 Inhibitors And Their Use For The Treatment Of Myeloproliferative Diseases And Cancer[fr] Inhibiteurs De Jak2 Et Leur Utilisation Pour Le Traitement De Maladies Myéloprolifératives Et Du Cancer 摘要:本发明提供了式(i)的化合物及其药学上可接受的盐.式(i)的化合物抑制jak2的酪氨酸激酶活性,因此使它们在作为抗增殖剂治疗癌症和其他疾病时具有用途.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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-2022411407-A1 优先权日:2019-11-15 标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof 发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN 权利人:UNIV NORTH CAROLINA CHAPEL HILL 摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.
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: Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21.
合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749