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托法替尼柠檬酸盐(Tofacitinib) 被引量：3

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摘要 2012年11月6日，由美国辉瑞公司开发的托法替尼（tofacifinib）柠檬酸盐（商品名：Xeljanz）被美国食品药品管理局批准上市，该药用于对氨甲喋呤治疗应答不充分或不耐受的中至重度活动性类风湿关节炎的成人患者，是一种新型口服JAK抑制剂。
作者 王铁英 胡春
机构地区 沈阳药科大学
出处 《中国药物化学杂志》 CAS CSCD 2013年第2期166-167,共2页 Chinese Journal of Medicinal Chemistry
关键词 柠檬酸盐 美国食品药品管理局 托法 活动性类风湿关节炎 批准上市 辉瑞公司 成人患者 治疗应答
分类号 R979.5 [医药卫生—药品]
  • 相关文献

参考文献7

  • 1US FDA. FDA approves Xeljanz for rheumatoid arthritis[ EB/ OL ]. [ 2012 -11 - 06 ]. http://www, fda. gov/NewsEvents/ N ucm327152, htm.
  • 2CAI W L, CONONY J L FROST H, et al. Investigation of practical routes for the kilogram-scale production of cis-3- methylamino-4-methylpiperidines[ J]. Org Process Res Dev, 2005,9(1) :51 -56.
  • 3RIBIN D H B. 3-Amino-piperidine derivatives and methods of manufacture: US,20040102627 [ P ]. 2004 - 05 - 27.
  • 4RUGGER/ S G, HAWKINS J M, MAKOWSKI T M, et al. Pyrrolo [ 2,3-d] pyrimidine derivatives: their intermediates and synthesis : US ,8309716 [ P]. 2012 - 11 - 13.
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  • 6莫选荣,罗心静.类风湿性关节炎发病机制的研究进展[J].医学临床研究,2007,24(2):336-340. 被引量：45
  • 7范鸣.抗类风湿性关节炎药Tofacitinib[J].药学进展,2011,35(10):480-480. 被引量：9

二级参考文献28

  • 1张义浜,刘志敏,熊凌霜.类风湿关节炎发病机制及其治疗方法研究进展[J].细胞与分子免疫学杂志,2005,21(B03):88-90. 被引量：65
  • 2Silverman GJ,Carson DA.Roles of B cells in rheumatoid arthritis[J].Arthritis Res Ther,2003,5 (suppl.4):S1-S6.
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  • 6Scheel-Toellner D,Wang K,Henriquez NV,et al.Cytokine-mediated inhibition of apoptosis in non-transformed T cells and neutrophils can be dissociated from protein kinase B activation[J].Eur J Immunol,2002,32:486-493.
  • 7Mecklenburgh KI,Walmsley SR,Cowburn AS,et al.Involvement of a ferroprotein sensor in hypoxia mediated inhibition of neutrophil apoptosis[J].Blood,2002,100:3008-3016.
  • 8Sun Y,Cheung JM,Martel-Pelletier J,et al.Wild type and mutant p53 differentially regulate the gene expression of human collagenase-3 (hMMP-13)[J].J Biol Chem,2000,275:11327-11332.
  • 9Perlman H,Bradley K,Liu H T,et al.IL-6 and Matrix Metalloproteinase-1 Are Regulated by the Cyclin-Dependent Kinase Inhibitor p21 in Synovial Fibroblasts[J].J Immun,2003,170:838-845.
  • 10Burkhardt H,Sehnert B,Bockermann R,et al.Humoral immune response to citrullinated collagen type II determinants in early rheumatoid arthritis[J].Eur J Immunol,2005,35:1643-1652.

共引文献52

同被引文献23

  • 1未本美,张智勇,戴志群,易嘉玲.4-氯吡咯[2,3-d]嘧啶的合成[J].化学试剂,2007,29(5):301-302. 被引量：3
  • 2FDA. FDA approves Xeljanz for rheumatoid arthritis[EB/OL] . 2012[2015 -03 -12]. http://www.fda.gov/newsevents/news?room/pressannouncements/ucm327152. html.
  • 3BHIRUD SB, MISHRA S, NARAYANAN SB, et at. Process for the preparation of tofacitinib and intermediates thereof: WO, 2014102826 Al[PJ. 2013 -12 - 27.
  • 4LARSEN SD, GRIECO PA. Aza Diels-Alder reactions in aque?ous solution: cyclocondensation of dienes with simple iminium salts generated under Mannich conditions[J].J Am Chem Soc, 1985, 107(6): 1768 -1769.
  • 5CAl WL, COLONYJL, FROST H, et at. Investigation of practi- cal routes for the kilogram-scale production of cis-3-methylamino- 4-methylpiperidines[J]. Org Process Res Dev, 2005, 9 ( 1 ) : 51 - 56.
  • 6WILCOX GE, KOECHER C, VRIES T, et al. Optical resolution of ( I-benzyI4-methylpiperidi-3 -yl ) -rnethylamine and thereof for the preparation of pyrrolo-2, 3 -pyrimidine derivatives as protein kinases inhibitors: W 0, 02096909 Al[P]. 2002 - 12 - 05 .
  • 7JIANGJK, GHORESCHI K, DEFLORIAN F, et al, Examining the chirality, conformation and selective kinase inhibition of 3- ( (3R ,4R) 4-methyl-3-( methyl ( 7 H-pyrrolo[2 ,3-dJ pyrimidin4- yl) amino) piperidin-l=yl ) -3-oxopropanenitrile ( CP-690, 550)[J].J Med Chern, 2008, 51(24) :8012 -8018.
  • 8HAO BY, LIUJQ, ZHANG WH, et al, A novel asymmetric syn?thesis of cis-f 3R, 4R ) -N-( tert-butoxycarbonyl ) 4-methyl-3- (methylamino) piperidine[J]. Synthesis, 2011, 2011 (8): 1208 -1212.
  • 9HAO BY, LIUJQ, ZHANG WH, et al, Chiral pool synthesis of Nvcba-cis-f 3R, 4R) -3-methylamino4-methylpiperidine from L?malic acid[J]. Bull Korean Chem Soc, 2013, 34 (5) : 1371 - 1377.
  • 10MARICAN A, SIMIRGITIS MJ, SANTOS LS. Asymmetric total synthesis of tofacitinib[J]. Tetrahedron Lett, 2013,54 ( 37 ) : 5096 - 5098.

引证文献3

二级引证文献36

中国药物化学杂志
2013年 第2期

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