CAS: 885264-71-1; (2R,4S,5R)-1-(4-Tert-Butyl-3-Methoxybenzoyl)-4-(Methoxymethyl)-2-(Pyrazol-1-Ylmethyl)-5-(1,3-Thiazol-2-yl)Pyrrolidine-2-Carboxylic Acid

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      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-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-2010160403-A1
      优先权日:2008-12-19
      标题 :Hcv ns3 protease inhibitors
      发明人:LINK JOHN O; VIVIAN RANDALL W
      权利人:GILEAD SCIENCES INC
      摘要:The present invention relates to macrocyclic compounds of formula (Ia) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

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      主要参考文献


      1: Maynard A, Crosby RM, Ellis B, Hamatake R, Hong Z, Johns BA, Kahler KM, Koble C, Leivers A, Leivers MR, Mathis A, Peat AJ, Pouliot JJ, Roberts CD, Samano V, Schmidt RM, Smith GK, Spaltenstein A, Stewart EL, Thommes P, Turner EM, Voitenleitner C, Walker JT, Waitt G, Weatherhead J, Weaver K, Williams S, Wright L, Xiong ZZ, Haigh D, Shotwell JB. Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase. J Med Chem. 2014 Mar 13;57(5):1902-13. doi: 10.1021/jm400317w. Epub 2013 May 29.

      合成参考文献


      参考文献:10.1055/s-0031-1290969
      摘要:Malinakova H, Raikar S, Pal B. Diastereocontrol in the Synthesis of 2,3,4-Trisubstituted Pyrrolidines and Tetrahydrofurans via a Palladium(II)-Catalyzed Three-Component Coupling Reaction. Synthesis. 2012 Jun 05;44(13):1983–92. doi: 10.1055/s-0031-1290969.
      参考文献:10.1055/s-0034-1379019
      摘要:Babu S, Rajkumar V. Regio- and Diastereoselective Cycloaddition of Azomethine Ylides with Benzylidenemalononitrile: Assembly of a New Set of Multisubstituted 4,4-Dicyanopyrrolidine-2-carboxylate and Nornicotine Scaffolds. Synlett. 2014 Aug 25;25(18):2629–35. doi: 10.1055/s-0034-1379019.
      参考文献:10.1007/s00705-022-05375-0
      摘要:Meshram RJ, Kathwate GH, Gacche RN. Progress, evolving therapeutic/diagnostic approaches, and challenges in the management of hepatitis C virus infections. Archives of Virology. 2022 Jan 28;167(3):717–36. doi: 10.1007/s00705-022-05375-0.
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