4,5-二氯邻苯二胺置于氢氧化钾,Ammonium Hydroxide,三氟甲磺酸三甲基硅酯,氨,镍,牛血清白蛋白体系中,用 乙醇,水,乙腈 作为反应溶剂,化学反应 65.25H,反应生成 5,6-二氯-1-β-D-呋喃核糖基苯并咪唑 参考文献:Benzimidazole Ribonucleosides: Design,Synthesis,And Antiviral Activity Of Certain 2-(Alkylthio)-And 2-(Benzylthio)-5,6-Dichloro-1-(.Beta.-D-Ribofuranosyl)Benzimidazoles 标题:Benzimidazole Ribonucleosides: Design,Synthesis,And Antiviral Activity Of Certain 2-(Alkylthio)-And 2-(Benzylthio)-5,6-Dichloro-1-(.Beta.-D-Ribofuranosyl)Benzimidazoles 摘要:Several 2-Alkylthio-And 2-Benzylthio Derivatives Of 5,6-Dichloro-1-(Beta-D-Ribofuranosyl)Benzimidazole (Drb) Have Been Designed And Synthesized From 5,6-Dichloro-1-(Beta-D-Ribofuranosyl)-Benzimidazole-2-Thione. All Compounds Were Evaluated For Activity Against Human Cytomegalovirus (Hcmv) And/or Herpes Simplex Virus Type-1 (Hsv-1). Three Different Cytotoxicity Assays Were Used To Determine If The Compounds Were Toxic To Uninfected Cells. Most Of The 2-Alkylthio Compounds Were Either Inactive Against Hcmv And Hsv-1 Or Were Active Only At Concentrations At Or Near Those Which Produced Toxicity In Uninfected Cells. The Best Separation Between Activity Against Hcmv And Cytotoxicity Was Observed With The 2-Benzylthio Analog 7. This Prompted Us To Synthesize The Substituted 2-Benzylthio Analogs 11-23 Using A Topliss Tree Approach. None Of These Compounds Were More Active Than Compound 7; Most Of The Analogs Were Weakly Active Against Both Hcmv And Hsv-1,But The Activity Was Not Separated From Cytotoxicity. On The Basis Of Both Antiviral And Cytotoxicity Data,Compound 7 Was The Best Compound In The Series. It Was More Active Against Hcmv Than Drb (The 2-Unsubstituted Analog),Acyclovir,And Foscarnet,But It Was Less Active Than Ganciclovir. DOI:10.1021/jm00044A015
专利号:US-8673594-B2 优先权日:2000-05-05 标题:Methods for stimulating nervous system regeneration and repair by regulating arginase I and polyamine synthesis 发明人:FILBIN MARIE T; RATAN RAJIV R 权利人:FILBIN MARIE T; RATAN RAJIV R; RES FOUNDATION OF CITY UNIVERSITY OF NEW YORK; BETH ISRAEL DEACONNESS MEDICAL CT 摘要:This invention relates to the novel identification of arginase as an enzymatic activity which can reverse inhibition of neuronal regeneration in the central and peripheral nervous system. Assays to monitor the effects of various agents on arginase expression and thus on neuronal regeneration and repair and to identify agents which will block or promote the inhibitory effects on neuronal outgrowth are provided. This invention also relates to compositions and methods using agents that can reverse the inhibitory effects of myelin on neural regeneration by affecting arginase activity or putrescine and derivative polyamine levels in a neuron. Methods for regulating and for promoting (or repressing) neuronal growth or regeneration in the nervous system, methods for treating injuries or damage to nervous tissue or neurons, and methods for treating neural degeneration associated with conditions, disorders or diseases, comprising the step of administering at least one of the compositions according to this invention, are provided.
专利号:US-4482708-A 优先权日:1982-08-09 标题 :3', 5'-Dinucleoside phosphates of 5,6-dichloro-1-β-D-ribofuranosyl-1-benzimidazole and methods of making and using the same 发明人:NGUYEN NICOLAS C 权利人:NGUYEN NICOLAS C 摘要:A new 3',5'-dinucleoside phosphate, the pharmaceutically acceptable salts thereof and intermediates therefor. The 3',5'-dinucleoside phosphate of 5,6-dichloro-1- beta -D-ribofuranosyl-1-benzimidazole and namely 5,6-dichloro-1- beta -D-ribofuranosyl-1-benzimidazole-3'-yl-5,6-dichloro-1- beta -D-ribofuranosyl-1-benzimidazole-5'-yl-phosphate possesses potent inducing activity for the cellular synthesis of interferons and in particular beta -interferon. The compound is also markedly effective to induce antiviral levels of interferon and possesses significant interferon potentiation properties. The invention also contemplates methods for the preparation of the new compounds and for using the new 3',5'-dinucleoside phosphate.
专利号:US-10059780-B2 优先权日:2015-06-30 标题:Method for producing rubber particles with reduced coagulation tendency, method for producing pneumatic tire, and method for producing rubber product 发明人:YAMAGUCHI HARUHIKO; INOUE Yukino; FUSHIHARA KAZUHISA; TAKAHASHI SEIJI; YAMASHITA SATOSHI; NAKAYAMA TORU 权利人:SUMITOMO RUBBER IND; UNIV TOHOKU 摘要:Provided is a method for producing rubber particles with a reduced coagulation tendency. The present invention relates to a method for producing rubber particles with a reduced coagulation tendency, the method including a step of performing protein synthesis in the presence of both rubber particles and a cell-free protein synthesis solution containing an mRNA coding for a rubber elongation factor (REF) family protein to bind the REF family protein to the rubber particles.
专利号:US-10227344-B2 优先权日:2016-06-24 标题 :CK2 inhibitors, compositions and methods thereof 发明人:WEBBER STEPHEN E; TAO XUELIANG; BRIN ELENA 权利人:POLARIS PHARMACEUTICALS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. n nFor Formula (I) compounds R 1 , R 2 , R 3 , Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
专利号:US-10907179-B2 优先权日:2015-06-30 标题:Production method for polyisoprenoid, vector, transgenic plant, production method for pneumatic tire, and production method for rubber product 发明人:YAMAGUCHI HARUHIKO; INOUE Yukino; FUSHIHARA KAZUHISA; TAKAHASHI SEIJI; YAMASHITA SATOSHI; NAKAYAMA TORU 权利人:SUMITOMO RUBBER IND; UNIV TOHOKU 摘要:The present invention provides a method for producing a polyisoprenoid with which it is possible to enhance the rubber synthesis activity of rubber particles to increase natural rubber production. The present invention relates to a method for producing a polyisoprenoid in vitro, which involves the use of a gene coding for a cis-prenyltransferase (CPT) family protein and a gene coding for a Nogo-B receptor (NgBR) family protein, and further involves the use of rubber particles bound to proteins encoded by these genes; or a method for producing a polyisoprenoid, which includes introducing into a plant a vector in which a promoter having a promoter activity that drives laticifer-specific gene expression is linked to a gene coding for a CPT family protein and a gene coding for a NgBR family protein, to express proteins encoded by the genes specifically in laticifers.
[参考文献]: Rickert P, Et Al. Cyclin C/cdk8 And Cyclin H/cdk7/p36 Are Biochemically Distinct Ctd Kinases. Oncogene. 1999 Jan 28;18(4):1093-102. [参考文献]: Schang Lm. Cyclin-Dependent Kinases As Cellular Targets For Antiviral Drugs. J Antimicrob Chemother. 2002 Dec;50(6):779-92. [参考文献]: Te Poele Rh, Et Al. Rna Synthesis Block By 5, 6-Dichloro-1-Beta-D-Ribofuranosylbenzimidazole (Drb) Triggers P53-Dependent Apoptosis In Human Colon Carcinoma Cells. Oncogene. 1999 Oct 14;18(42):5765-72. [参考文献]: Yankulov K, Et Al. The Transcriptional Elongation Inhibitor 5,6-Dichloro-1-Beta-D-Ribofuranosylbenzimidazole Inhibits Transcription Factor Iih-Associated Protein Kinase. J Biol Chem. 1995 Oct 13;270(41):23922-5. [参考文献]: Zandomeni Ro. Kinetics Of Inhibition By 5,6-Dichloro-1-Beta-D-Ribofuranosylbenzimidazole On Calf Thymus Casein Kinase Ii. Biochem J. 1989 Sep 1;262(2):469-73.
合成参考文献
参考文献:10.1016/j.bbrc.2023.08.050 摘要:Ikeda Y, Davis MI, Sumita K, Zheng Y, Kofuji S, Sasaki M, Hirota Y, Pragani R, Shen M, Boxer MB, Takeuchi K, Senda T, Simeonov A, Sasaki AT. Multimodal action of KRP203 on phosphoinositide kinases in vitro and in cells. Biochemical and Biophysical Research Communications. 2023 Oct;679():116–21. doi: 10.1016/j.bbrc.2023.08.050.