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阿哌沙班合成路线图解 被引量：11

Graphical Synthetic Routes of Apixaban
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摘要 阿哌沙班（apixaban,1）,化学名为l-（4-甲氧基苯基）-7-氧代-6-[4-（2-氧代哌啶-1-基）苯基]-4,5,6,7-四氢-1H-吡唑并[3,4-c]吡啶-3-甲酰胺,是由百时美施贵宝公司和辉瑞公司联合研制的一种新型口服直接Xa因子抑制剂。1于2011年3月在欧盟批准上市,商品名Eliquis,临床用于预防进行,
作者 王冠 郭晔堃 钟静芬 时惠麟
机构地区 浙江工业大学药学院 中国医药工业研究总院上海医药工业研究院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2012年第2期157-159,共3页 Chinese Journal of Pharmaceuticals
基金 国家"重大新药创制"科研重大专项(2009ZX09301-007)
关键词 合成路线图解 甲氧基苯基 XA因子 辉瑞公司 批准上市 化学名 甲酰胺 抑制剂
分类号 R973.2 [医药卫生—药品]
  • 相关文献

参考文献8

  • 1Lassen MR, Raskob GE, Gallus A, et al. Apixaban versus enoxaparin for thromboprophylaxis after knee replacement (ADVANCE-2) : a randomised double-blind trial [J]. Lancet, 2010, 375(9717) : 807-815.
  • 2许昕,薛晓文.开发中的新型口服抗凝血药-Xa因子抑制剂[J].药学与临床研究,2010,18(3):294-298. 被引量：9
  • 3Zhou J, Oh LM, Ma P, et al. Synthesia of 4,5-dihydro- pyrazolo[3,4-c] pyrid-2-ones: WO, 03049681 [P]. 2001-12-10.
  • 4Pinto DJ. Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors: WO, 2004083177 [P]. 2003 -03-18.
  • 5Donald J, Michael JO, Stephanie K, et al. Discovery of 1- (4-methoxyphenyl) -7-oxo-6- (4- (2-oxopiperidin- 1 - yl) phenyl) -4,5,6,7-tetrahydro-1H-pyrazolo t3,4-c] pyridine- 3-carboxamide (Apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa [J]. JMed Chem, 2007, 50 (22) : 5339-5356.
  • 6Gant TG, Shahbaz M. Pyrazole carboxamide inhibitors of factor Xa: WO, 2010030983 [P]. 2008-09-15.
  • 7冀亚飞,蒋健安,刘倩,等.一种抗血栓药物阿匹沙班的制备方法:中国,101967145[P].2010-09-09.
  • 8Brad DM, Scott BT, Shiang YC, et al. The syntheses and in vitro metabolism of [^14C] apixaban, an inhibitor of blood coagulation FXa [J]. J Label Compd Radiopharm, 2010, 53 (5-6) : 355-367.

二级参考文献28

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  • 4Perzbom E,Strassburger J,Wilmen A,et al.In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939-an oral,direct factor Xa inhibitor[J].J Thromb Haemost,2005,3(3):514-21.
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  • 10青爱国 武建卓.抗凝血的低分子量肽类似物.生命的化学,2008,28(4):395-8.

共引文献9

同被引文献43

  • 1冀亚飞, 江健安, 刘倩, 等. 一种抗血栓药物阿匹沙班的制备方法: 中国, 201010277358.0[P]. 2011-02-09.
  • 2Donald J.P. Pinto,Michael J. Orwat,Mimi L. Quan,Qi Han,Robert A. Galemmo,Eugene Amparo,Brian Wells,Christopher Ellis,Ming Y. He,Richard S. Alexander,Karen A. Rossi,Angela Smallwood,Pancras C. Wong,Joseph M. Luettgen,Alan R. Rendina,Robert M. Knabb,Lawrence Mersinger,Charles Kettner,Steven Bai,Kan He,Ruth R. Wexler,Patrick Y.S. Lam.1-[3-Aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-( R )-hydroxy- N -pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4- c ]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa[J].Bioorganic & Medicinal Chemistry Letters.2006(15)
  • 3薛吉军,李毅,王仕祥,等.一种抗血栓药物阿哌沙班的制备方法:中国,103342704A[P].2013—10—09.
  • 4赵纪山,徐强,徐卓业,等.一种阿哌沙班的合成方法:中国,102675314A[P].2012-09-19.
  • 5国家药典委员会.中国药典2010年版:二部[M].北京:中国医药科技出版社,2010:附录61-65.
  • 6Hohnloser SH, Hijazi Z, Thomas L, et al. Efficacy of apixaban when compared with warfarin in relation to renal function in patients with atrial fibrillation: insights from the ARISTOTLE trial [J]. Eur Heart J, 2012, 33 (22): 2821-- 2830.
  • 7Gant TG, Shahbaz M. Pyrazole carboxamide inhibitors of factor Xa: WO, 2010030983A2 [P]. 2010-03-18.
  • 8Zhou JC, Oh LM, Ma P, et al. pyrazolo 3,4-c pyrid-2-ones 2003-06-19. Synthesis of 4,5-dihydro- WO, 03049681A2 [P].
  • 9叶大健,刘涛,马苏旺.4一环内酰胺基苯胺的制备方法:中国,103709095A[P].2014-04-09.
  • 10Shapiro R, Rossano LT, Mudryk BM, et al. Process for preparing 4,5-dihydro-pyrazolo E 3,4-c pyrid-2-ones: US, 20060069258A1 [P]. 2006-03-30.

引证文献11

二级引证文献17

中国医药工业杂志
2012年 第2期

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