CAS: 20662-53-7; 3-Piperidin-4-Yl-1H-Benzimidazol-2-One

该化合物是一个化学化合物,其特点是其独特的结构,包括一个与管状环结合的联氨联氨核核心,该化合物通常具有诸如有机溶剂中中溶性以及潜在生物活性等特性,因此对药用化学具有兴趣;管状藻的存在可能助长其药理特性,有可能影响其与生物目标的相互作用;该化合物经常被研究其在药物开发中的潜在应用,特别是在与...

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合成工艺路线路线简述

  • 合成目标产物 4-(2-Keto-1-Benzimidazolinyl)Piperidine 主要起始原料 4-Amino-1-Boc-Piperidine
  • (文献来源)合成步骤主要原料 4-Amino-1-Boc-Piperidine
2,3-二氟硝基苯置于碳酸氢钠,Potassium Carbonate,三氟乙酸体系中,化学反应生成4-(2-酮酸-1-苯并咪唑)哌啶
参考文献:Heterocyclic Compound,Application Thereof,And Composition Containing Same
标题:Heterocyclic Compound,Application Thereof,And Composition Containing Same
摘要:由式xi表示的杂环化合物,其药用盐,溶剂合物,或其药用盐的溶剂合物,以及其用途和含有该化合物的组合物.该化合物在结构上是新颖的,并具有非常好的stat5抑制活性.

海关参考信息

专利信息


专利号:US-6906046-B2
优先权日:2000-12-22
标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes
发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY
权利人:CELLTECH R & D INC
摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.

专利号:US-7186709-B2
优先权日:2002-08-27
标 题:Dihydropyrancarboxamides and uses thereof
发明人:SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN
权利人:HARVARD COLLEGE
摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.

专利号:US-6326372-B1
优先权日:1999-09-30
标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists
发明人:EVANS BEN E; GILBERT KEVIN F
权利人:MERCK & CO INC
摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

专利号:US-7829699-B2
优先权日:2006-04-10
标题:Process for the preparation of CGRP antagonist
发明人:BELYK KEVIN; RIVERA NELO
权利人:MERCK SHARP & DOHME
摘要:An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDIâ€?) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.

专利号:US-2003069305-A1
优先权日:2000-12-22
标题:Pharmaceutical uses and synthesis of benzobicyclooctanes

专利号:US-6096763-A
优先权日:1995-02-23
标题 :α1a adrenergic receptor antagonists
发明人:HOFFMAN JACOB M; CHANG RAYMOND S L
权利人:MERCK & CO INC
摘要:This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
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合成参考文献


参考文献:10.1111/j.1476-5381.1996.tb15631.x
摘要:Candura SM, Messori E, Franceschetti GP, D'Agostino T, Vicini D, Tagliani M, Tonini M. Neural 5‐HT4receptors in the human isolated detrusor muscle: effects of indole, benzimidazolone and substituted benzamide agonists and antagonists. British J Pharmacology. 1996 Aug;118(8):1965–70. doi: 10.1111/j.1476-5381.1996.tb15631.x.
参考文献:10.1016/j.neo.2015.08.009
摘要:Bilsland AE, Pugliese A, Liu Y, Revie J, Burns S, McCormick C, Cairney CJ, Bower J, Drysdale M, Narita M, Sadaie M, Keith WN. Identification of a Selective G1-Phase Benzimidazolone Inhibitor by a Senescence-Targeted Virtual Screen Using Artificial Neural Networks. Neoplasia. 2015 Sep;17(9):704–15.
参考文献:10.1016/j.bmcl.2006.08.010
摘要:Finley DR, Bell MG, Borel AG, Bloomquist WE, Cohen ML, Heiman ML, Kriauciunas A, Matthews DP, Miles T, Neel DA, Rito CJ, Sall DJ, Shuker AJ, Stephens TW, Tinsley FC, Winter MA, Jesudason CD. Potent benzimidazolone based human beta(3)-adrenergic receptor agonists. Bioorg Med Chem Lett. 2006 Nov 01;16(21):5691–4. doi: 10.1016/j.bmcl.2006.08.010.
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