📜4-[4-(4-氟苯基)-2-[4-(甲硫基)苯基]-1H-咪唑-5-基]吡啶置于dipotassium Peroxodisulfate,溶剂黄146体系中,化学反应 18.0H,以78%的收率获得4-(4-氟苯基)-2-(4-甲基亚磺酰基苯基)-5-(4-吡啶基)-1H-咪唑 参考文献:Regulation Of Stress-Induced Cytokine Production By Pyridinylimidazoles; Inhibition Of Csbp Kinase 标题:Regulation Of Stress-Induced Cytokine Production By Pyridinylimidazoles; Inhibition Of Csbp Kinase 摘要:Members Of Three Classes Of Pyridinylimidazoles Bind With Varying Affinities To Csbp (P38) Kinase Which Is A Member Of A Stress-Induced Signal Transduction Pathway. Based Upon Sar And Protein Homology Modeling,The Pharmacophore And Three Potential Modes Of Binding To The Enzyme Are Presented. For A Subset Of Pyridinylimidazoles,Binding Is Shown To Correlate With Inhibition Of Csbp Kinase Activity,Whereas No Significant Inhibition Of Pka,Pkc Alpha And Erk Kinase Activity Is Observed. Copyright (C) 1997 Elsevier Science Ltd. Doi:10.1016/s0968-0896(96)00212-X
专利号:US-2006246505-A1 优先权日:2003-09-02 标题:Modulation of the synthesis of insulin 发明人:WALTHER REINHARD 权利人:WALTHER REINHARD 摘要:The invention particularly relates to the use of substances, which modulate the activity of the proteins casein kinase II (CK II) and 14-3-3 epsilon and/or of the PcG protein EED or which influence the binding of the proteins casein kinase II (CK II) and 14-3-3 epsilon, of the PcG protein EED and/or of a fragment thereof with the protein pancreatic duodenal homeobox-1 (PDX-1) that plays a decisive roll in the glucose-induced biosynthesis of insulin, for influencing the synthesis of insulin or the provision of insulin.
专利号:EP-1546732-B1 优先权日:2002-09-03 标 题:Modulation of the synthesis of insulin 发明人:WALTHER REINHARD 权利人:UNIV ERNST MORITZ ARNDT 摘要:The invention particularly relates to the use of substances, which modulate the activity of the proteins casein kinase II (CK II) and 14-3-3 epsilon and/or of the PcG protein EED or which influence the binding of the proteins casein kinase II (CK II) and 14-3-3 epsilon, of the PcG protein EED and/or of a fragment thereof with the protein pancreatic duodenal homeobox-1 (PDX-1) that plays a decisive roll in the glucose-induced biosynthesis of insulin, for influencing the synthesis of insulin or the provision of insulin.
专利号:US-2024239805-A1 优先权日:2022-12-16 标 题:Aza-yang cyclization-buchner aromatic ring expansion: collective synthesis of cycloheptatriene-containing azetidine lactones 发明人:SINGH MANVENDRA PAL; BOSKOVIC ZARKO; GASKINS BRYCE 权利人:UNIV KANSAS 摘要:The present disclosure is directed to a compound of Formula I, Formula II, Formula III, Formula IV, or Formula Vor a pharmaceutically acceptable salt and/or solvate thereof.
专利号:US-2018351104-A1 优先权日:2012-11-02 标 题:3-substituted tellurophenes and related compounds 发明人:SEFEROS DWIGHT; JAHNKE ASHLEE 权利人:GOVERNING COUNCIL UNIV TORONTO 摘要:Monomeric 3-substituted tellurophene compounds, as well as their use in the synthesis of oligomeric and/or polymeric compounds consisting of two or more tellurophene-2,5-diyl groups which are covalently linked to each other are disclosed, as is the use of said oligomers and polymers in devices such as diodes and solar cells, electrodes and semiconductors.
专利号:WO-2023241717-A1 优先权日:2022-06-16 标题:Substance for promoting regeneration and repair of organs of mammals and use thereof 发明人:LI WEI; ZHOU QI; He zheng-quan; LU ZONGBAO; WANG SHUAI; WANG XIN; YUAN XUEWEI; WANG LIU 权利人:INST ZOOLOGY CAS; BEIJING INST FOR STEM CELL AND REGENERATIVE MEDICINE 摘要:Provided is use of a substance capable of up-regulating ISG gene expression in preparing a drug or reagent for promoting the regeneration and repair capacity of tissues or complex structures or organs of mammals. The substance for up-regulating ISG gene expression is selected from one or two or more of an MAPK inhibitor, a retinoic acid receptor-related orphan receptor inhibitor, a protein synthesis inhibitor, and an interferon (IFNγ, β, λ) or alarmin (S100A8/A9) protein. The regeneration and repair refer to promoting the regeneration of tissues or complex structures or organs after tissue or organ resection or damage.
专利号:US-9982006-B2 优先权日:2014-08-21 标题:2′-chloro aminopyrimidinone and pyrimidine dione nucleosides 发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN 权利人:GILEAD SCIENCES INC 摘要:Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds.
1: Hall-Jackson CA, Goedert M, Hedge P, Cohen P. Effect of SB 203580 on the activity of c-Raf in vitro and in vivo. Oncogene. 1999 Mar 25;18(12):2047-54. doi: 10.1038/sj.onc.1202603. 364(2):229-33. doi: 10.1016/0014-5793(95)00357-f. 95(6):466-71. doi: 10.1007/s003950070022. 31(11):783-97. doi: 10.1080/00498250110065621. 161(1):467-73. Erratum in: J Immunol 1999 Mar 1;162(5):3105. 351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095. 7: Kumar S, Jiang MS, Adams JL, Lee JC. Pyridinylimidazole compound SB 203580 inhibits the activity but not the activation of p38 mitogen-activated protein kinase. Biochem Biophys Res Commun. 1999 Oct 5;263(3):825-31. doi: 10.1006/bbrc.1999.1454. 279(3):1453-61. 290(2):621-8. 279(21):22738-46. doi: 10.1074/jbc.M401389200. Epub 2004 Mar 17. 42(3):142-7. doi: 10.5483/bmbrep.2009.42.3.142. 12: Börsch-Haubold AG, Pasquet S, Watson SP. Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. SB 203580 also inhibits thromboxane synthase. J Biol Chem. 1998 Oct 30;273(44):28766-72. doi: 10.1074/jbc.273.44.28766. 278(25):22237-42. doi: 10.1074/jbc.M300847200. Epub 2003 Mar 11. 15(3):243-50. doi: 10.1385/JMN:15:3:243. 259(2):465-70. doi: 10.1006/bbrc.1999.0759. 273(25):15605-10. doi: 10.1074/jbc.273.25.15605. 10(11):3063-3064. doi: 10.18632/aging.101641.
合成参考文献
参考文献:10.1007/s11596-010-0122-4 摘要:Chen R, Tu Y, Lin J, She W, Li J, Wu Z, Xu L, Chen H. The nongenomic effects of progesterone in repressing iNOS activation through P38MAPK pathways in gonococci-infected polymorphonuclear leukocytes and the clinical significance. J Huazhong Univ Sci Technolog Med Sci. 2010 Feb;30(1):119–25. doi: 10.1007/s11596-010-0122-4. 参考文献:10.1186/1471-2199-12-29 摘要:Wen X, Chao C, Ives K, Hellmich MR. Regulation of bombesin-stimulated cyclooxygenase-2 expression in prostate cancer cells. BMC Molecular and Cell Biology. 2011 Jul 11;12(1):29. doi: 10.1186/1471-2199-12-29. 参考文献:10.1111/j.1460-9568.2011.07763.x 摘要:Baxter AW, Choi SJ, Sim JA, North RA. Role of P2X4 receptors in synaptic strengthening in mouse CA1 hippocampal neurons. Eur J of Neuroscience. 2011 Jul;34(2):213–20. doi: 10.1111/j.1460-9568.2011.07763.x. 参考文献:10.1186/ar3398 摘要:Heo YJ, Oh HJ, Jung YO, Cho ML, Lee SY, Yu JG, Park MK, Kim HR, Lee SH, Park SH, Kim HY. The expression of the receptor for advanced glycation end-products (RAGE) in RA-FLS is induced by IL-17 via Act-1. Arthritis Res Ther. 2011 Jul 12;13(4):R113. 参考文献:10.1007/s10753-011-9358-9 摘要:Mou H, Li Z, Kong Y, Deng B, Qian L, Wang JM, Le Y. Proinflammatory stimulants promote the expression of a promiscuous G protein-coupled receptor, mFPR2, in microvascular endothelial cells. Inflammation. 2012 Apr;35(2):656–64. doi: 10.1007/s10753-011-9358-9.