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哌马色林酒石酸盐合成路线图解 被引量:3

Graphical synthetic routes to pimavanserin tartrate
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摘要 哌马色林酒石酸盐(1)由美国Acadia制药公司研发,并于2016年4月29日经美国食品药品监督管理局(FDA)批准上市,其商品名称为Nuplazid。
出处 《中国药物化学杂志》 CAS CSCD 2017年第6期498-500,共3页 Chinese Journal of Medicinal Chemistry
基金 国家"重大新药创制"科技重大专项(2009ZX09301-012)
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  • 1陈中元,严剑峰,陈玲英.绿色的Curtius重排及其新应用的研究[J].当代化工,2006,35(5):361-365. 被引量:2
  • 2杨帆,陈立功,王东华.1-甲基-4-哌啶酮的合成[J].精细化工,2007,24(11):1142-1144. 被引量:8
  • 3Li Z, Ichikawa J, Huang M, et al. ACP-103, a 5-HT2A/2C inverse agonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens [J]. Psychopharmacology(Berl), 2005, 183(2): 144-153.
  • 4Vanover KE, Weiner DM, Makhay M, et al. Pharma-cological and behavioral profile of N-(4-fluoro-phenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-[4-(2-methyl-propyloxy)-phenylmethyl]carbamide(2R,3R)-dihydroxy-butanedioate (2 ∶ 1)(ACP-103), a novel 5-hydroxytry-ptamine2A receptor inverse agonist [J]. J Pharmacol Exp Ther, 2006, 317(2):910-918.
  • 5Dosa PI, Strah-Pleynet S, Jayakumar H, et al. Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverseagonists and their application as antiplatelet agents [J]. Bioorg Med Chem Lett, 2009, 19(18): 5486-5489.
  • 6Thygesen MB, Schlienger N, Tolf BR, et al. Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-[4-(2-methylpropyloxy)phenylmethyl]carbamide and their preparation: WO, 2006/036874A1 [P]. 2006-04-06.
  • 7Tolf BR, Schlienger N, Thygesen MB. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-[4-(2-methylpropyloxy)phenylmethyl] carbamide and its tartrate salt and crystalline forms: US, 20070260064 [P]. 2007-11-08.
  • 8Andersen VL, Hansen HD, Herth MM, et al. 11C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand [J]. Bioorg Med Chem Lett, 2015, 25(5):53-1056.
  • 9Gant TG, Sarshar S. Substituted ureas: US, 2008/0280886A1 [P]. 2008-11-13.
  • 10He Z, Zajdlik A, St Denis JD, et al. Boroalkyl group migration provides a versatile entry into α-aminoboronic acid derivatives [J]. J Am Chem Soc, 2012, 134(24): 9926-9929.

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