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Boceprevir 被引量：3

Boceprevir
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摘要 丙型肝炎蛋白酶抑制剂Boceprevir（SCH-503034）由美国先灵葆雅（Schering-Plough）公司研发（该公司于2009年11月与默克药厂合并）。2011年5月13日美国食品药品管理局（FDA）批准该药上市,用于某些成人患者慢性丙型肝炎的治疗。该药为口服制剂，商品名为Victrelis。
作者 徐芹 董金华
机构地区 沈阳药科大学
出处 《中国药物化学杂志》 CAS CSCD 2011年第5期409-410,共2页 Chinese Journal of Medicinal Chemistry
关键词 丙型肝炎蛋白酶抑制剂 BOCEPREVIR 美国先灵葆雅 慢性丙型肝炎
分类号 R978.7 [医药卫生—药品] F416.72 [经济管理—产业经济]
  • 相关文献

参考文献4

  • 1VENKATRAMAN S, BOGEN S L, ARASAPPAN A, et al. Discovery of ( 1R,5 S ) -N- [ 3 -amino-I - (cyclobutylmethyl) -2, 3-dioxopropyl ] -3- [ 2 ( S ) - [ [ [ ( 1,1 -dimethylethyl ) amino ] carbonyl ] amino ] -3,3-dimethyl-1 -oxobutyl ] -6,6-dimethyl-3- azabicyclo [ 3.1.0 ] hexan-2 ( S ) -carboxamide ( SCH503034 ), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection [ J ]. J Med Chem, 2006,49 ( 20 ) : 6074 - 6086.
  • 2CAMPAS C, RANDIAN R, BOLOS J, et al. Boceprevir [ J ]. Drugs Future,2009,34 (9) :697 - 707.
  • 3WU G,XIE J, RASHATASAKHON P, et al. Oxidation process for the preparation of N- [ 3-amino-1 - ( cyclobutylmeth- yl ) -2,3-dioxopropyl ] -3 - { N- [ ( tert-butylamino ) carbonyl ] -3 - methyl- L-valyl [ -6,6-dimethyl-3-azabicyclo [ 3.1.0 ] hexane- 2-carboxamide and related compounds: US, 20070149459 A1 [ P]. 2007 -06 -28.
  • 4屈莉红,陈良,王介非.HCV NS3蛋白酶及抑制剂的研究进展[J].肝脏,2007,12(3):203-205. 被引量：6

二级参考文献17

  • 1Tong X,Guo Z,Wright-Minogue J,et al.Impact of naturally occurring variants of HCV protease on the binding of different classes of protease inhibitors.Biochemistry,2006,45:1353-1361.
  • 2Koev G,Dekhtyar T,Han L,et al.Antiviral interactions of an HCV polymerase inhibitor with an HCV protease inhibitor or interferon in vitro.Antiviral Res,2007,73:78-83.
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  • 4Reesink HW,Zeuzem S,Weegink CJ,et al.Final results of a phase 1B,multiple-dose study of VX-950,a hepatitis C virus protease inhibitor.Hepatology,2005,42:234A.
  • 5Reesink HW,Zeuzem S,Weegink CJ,et al.Rapid decline of viral RNA in hepatitis C patients treated with VX-950:a phase Ib,placebo-controlled,randomized study.Gastroenterology.2006,131:997-1002.
  • 6Lin K,Perni RB,Kwong AD,et al.VX-950,a novel hepatitis C virus(HCV) NS3-4A protease inhibitor,exhibits potent antiviral activities in HCV replicon cells.Antimicrob Agents Chemother,2006,50:1813-1822.
  • 7Malcolm BA,Liu R,Lahser F,et al.SCH 503034,a mechanism-based inhibitor of hepatitis C virus NS3 protease,suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells.Antimicrob Agents Chemother,2006,50:1013-1020.
  • 8Zeuzem S,Sarrazin C,Rouzier R,et al.Anti-viral activity of SCH 503034,a HCV protease inhibitor,administered as monotherapy in hepatitis C genotype-1 (HCV-1) patients refractory to pegylated interferon(Peg-IFN-a).Hepatology,2005,42:233A.
  • 9Bartenschlager R.The NS3/4A proteinase of the hepatitis C virus:unravelling structure and function of an unusual enzyme and a prime target for antiviral therapy.J Viral Hepat,1999,6:165-181.
  • 10Butkiewicz N,Yao N,Zhong W,et al.Virus-specific cofactor requirement and chimeric hepatitis C virus/GB virus B nonstructural protein 3.J Virol,2000,74:4291-4301.

共引文献5

同被引文献33

  • 1先灵葆雅丙肝药SCH 503034获美国FDA快速审批[J].制药原料及中间体信息,2006(3):41-41. 被引量：1
  • 2Saksena AK,Girijavallabhan VM,Lovey RG,et al.Peptides as NS3-serine protease inhibitors of hepatitis C virus:US,7012066[P].2006-03-14.(CA 2007,146:229614).
  • 3Venkatraman S,Bogen SL,Arasappan A,et al.Discovery of(1R,SS)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl) amino]-carbonyl]amino]-3,3-dimethyl-1-oxobuty 1]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide(SCH 503034),a selective,potent,orally bioavailable hepatitis C virus NS3 protease inhibitor:a potential therapeutic agent for the treatment of hepatitis C infection[J].J Med Chem,2006,49(20):6074-6086.
  • 4Chen MZ,Green MD,Zhang FC.Process and intermediates for the preparation of 3-(amino)-3-cyclobutylmethyl-2-hydroxypropionamide or salts thereof:WO,2004113272[P].2004-12-29.(CA2004,142:93423).
  • 5Morgan A J,Nguyen S,Uttamsingh V,et al.Design and synthesis of deuterated boceprevir analogs with enhanced pharmacokinetic properties[J].J Labelled Compd Radiopharm,2011,54(9):613-624.
  • 6Dong S,Park JH,Vater EJ.Process for the synthesis of 3-amino-3-cyclobutylmethyl-2-hydroxypropionamide or salts thereof:WO,2009085858[P].2009-07-09.(CA 2009,151:123566).
  • 7Park JH,Vater EJ,Dong S,et al.Preparation of 3-amino3-(cyclobutylmethyl)-2-(hydroxy)-propionamide hydrochloride:WO,2008082486[P].2008-07-10.(CA2008,149:129089).
  • 8Park JH,Sudhakar A,Wong GS,et al.Process and intermediates for the preparation of(1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxylates or salts thereof:WO,2004113295[P].2004-12-29.(CA 2004,142:93671).
  • 9Wu G,Chen FX,Rashatasakhon P,et al.Process for the preparation of 6,6-dimethyl 3-azabicyclo-[3.1.0]-hexane compounds and enantiomeric salts thereof:WO,2007075790[P].2007-07-05.(CA 2007,147:143273).
  • 10Berranger T,Demonchaux P.Process for the preparation of 6,6-dimethyl 3-azabicyclo-[3.1.0]-hexane compounds utilizing bisulfate intermediate:WO,2008082508[P].2008-07-10.(CA2008,149:152936).

引证文献3

二级引证文献11

中国药物化学杂志
2011年 第5期

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