CAS: 1234490-83-5; Inx-08189

该化合物是一种合成化合物,属于以其潜在生物活动而闻名的分子类别,特别是在信号路径方面;该化合物的特征是:一个经常参与细胞信号的guanylyl群体,以及一种可能助长其疏水特性和与生物膜潜在相互作用的环烷基酸;L-alain残留物的存在表明,它可能以类似于氨基酸的方式与生物系统相互作用,可能影响蛋白相互作用或酶活动;2-2二甲基丙基酯群体表明,该化合物可能具有脂体特性,可能影响其在生物环境中的溶性及渗透性;总体而言,该复合物的独特结构特征表明,可能具有药用化学或生物化学用途,尽管具体的生物活动和机制需要进一步研究.

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物理性质

MSDS等安全信息

    上下游产品

    (S)-2-[chloro-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid 2,2-dimethyl propyl ester (2R,3R,4R,5R)-2-(2-amino-6-methoxy-9H-purin-9-yl)-5-(hydroxymethyl)-3-methyltetrahydrofuran-3,4-diol 2-Amino-6-chloropurin 1,2,3,5-tetra-O-benzoyl-2-C-methyl-β-D-ribofuranose

    合成工艺路线路线简述

      📜1,2,3,5-四苯甲酰氧基-2-C-甲基-Beta-D-呋喃核糖置于三氟甲磺酸三甲基硅酯,叔丁基氯化镁,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 四氢呋喃,甲醇,乙腈 用作溶剂,化学反应 24.0H,反应生成N-(2'-C-甲基-6-O-甲基-P-1-萘基-5'-鸟苷酰基)-L-丙氨酸 2,2-二甲基丙酯
      参考文献: Crystalline Solvates Of Nucleoside Phosphoroamidates,Their Stereoselective Preparation,Novel Intermediates Thereof,And Their Use In The Treatment Of Viral Disease[fr] Solvates Cristallins De Nucléoside Phosphoroamidates,Leur Préparation Stéréosélective,Nouveaux Intermédiaires De Ceux-Ci Et Leur Utilisation Dans Le Traitement D'Une Maladie Virale
      标题: Crystalline Solvates Of Nucleoside Phosphoroamidates,Their Stereoselective Preparation,Novel Intermediates Thereof,And Their Use In The Treatment Of Viral Disease[fr] Solvates Cristallins De Nucléoside Phosphoroamidates,Leur Préparation Stéréosélective,Nouveaux Intermédiaires De Ceux-Ci Et Leur Utilisation Dans Le Traitement D'Une Maladie Virale
      摘要:该发明涉及抗hcv核苷磷酸酰胺的(S)-P对映体的新型晶体溶剂化合物,(2S)-新戊基2-((((2R,3R,4R,5R)-5-(2-氨基-6-甲氧基-9H-嘌呤-9-基)-3,4-二羟基-4-甲基四氢呋喃-2-基)甲氧基)(萘基氧基)磷酰胺)丙酸酯(也称为inx-08189或inx-189),以及用于分离inx-08189两个对映体的重结晶方法.此外,该申请涉及一种新颖的立体选择性制备两个对映体的方法,以及用于这种立体选择性合成的新型合成中间体.该发明还涉及利用晶体溶剂化合物提高2'-C-甲基鸟苷三磷酸酯从口服剂量中的肝脏暴露.

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      专利信息


      专利号:US-12383499-B2
      优先权日:2018-01-01
      标题:Scale up synthesis of silicasome nanocarriers
      发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
      权利人:UNIV CALIFORNIA
      摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

      专利号:US-9573939-B2
      优先权日:2011-09-08
      标题:Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
      发明人：MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN
      权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN; MERCK SHARP & DOHME; MSD ITALIA SRL
      摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

      专利号:US-2016130259-A1
      优先权日:2013-06-24
      标题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
      发明人：LIU HONG; DAI XING; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; DANG QUN; PENG XUANJIA; LI PENG
      权利人:MERCK SHARP & DOHME
      摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

      专利号:US-9364482-B2
      优先权日:2013-06-24
      标 题 :Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
      发明人：DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; NARGUND RAVI; XIAO DONG; ZORN NICOLAS; DANG QUN; MCCOMAS CASEY C; PENG XUANJIA; LI PENG; SOLL RICHARD
      权利人:MERCK SHARP & DOHME
      摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. (I)

      专利号:US-9265773-B2
      优先权日:2011-09-08
      标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
      发明人：MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI
      权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI; MERCK SHARP & DOHME; MSD ITALIA SRL
      摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

      专利号:US-9549917-B2
      优先权日:2011-09-08
      标 题 :Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
      发明人：MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS
      权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS; MERCK SHARP & DOHME
      摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

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      主要参考文献


      1: McGuigan C, Madela K, Aljarah M, Gilles A, Brancale A, Zonta N, Chamberlain S, Vernachio J, Hutchins J, Hall A, Ames B, Gorovits E, Ganguly B, Kolykhalov A, Wang J, Muhammad J, Patti JM, Henson G. Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4850-4. doi: 10.1016/j.bmcl.2010.06.094. doi: 10.1128/AAC.01335-10.
      3: Yeo KL, Chen YL, Xu HY, Dong H, Wang QY, Yokokawa F, Shi PY. Synergistic suppression of dengue virus replication using a combination of nucleoside analogs and nucleoside synthesis inhibitors. Antimicrob Agents Chemother. 2015 Apr;59(4):2086-93. doi: 10.1128/AAC.04779-14.
      4: Gentile I, Buonomo AR, Zappulo E, Borgia G. Discontinued drugs in 2012 -

      合成参考文献


      参考文献:10.1007/7653_2020_51
      摘要:Kumar V, Roy K. Computational Modeling of RdRp Inhibitors for the Development of Drugs against Novel Coronavirus (nCoV). 2021. In: Methods in Pharmacology and Toxicology.
      参考文献:10.1007/s11172-025-4746-8
      摘要:Ulomsky EN, Aminov SV, Neymash AO, Lyapustin DN, Fedotov VV, Ishimnikov VA, Rusinov VL. Aminopurines: synthesis, modifications, and applications. Russ Chem Bull. 2025 Sep;74(9):2629–67. doi: 10.1007/s11172-025-4746-8.
      参考文献:10.1007/s00705-013-1803-7
      摘要:Imran M, Manzoor S, Khattak NM, Khalid M, Ahmed QL, Parvaiz F, Tariq M, Ashraf J, Ashraf W, Azam S, Ashraf M. Current and future therapies for hepatitis C virus infection: from viral proteins to host targets. Arch Virol. 2014 May;159(5):831–46. doi: 10.1007/s00705-013-1803-7.
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