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王喆
南開大學藥學院教授
1991,1 - 1993,8: 美國哈佛大學化學系有機合成化學專業, 指導教授: Elias J.Corey (1990年諾貝爾化學獎得主),博士后。
1986,9 - 1991,1: 美國田納西州大學化學系有機合成化學專業, 指導教授: George W. Kabalka,博士學位。
1982, 2 - 1985, 1: 中國蘭州大學化學系天然產物化學產物專業及及昆明植物研究所, 指導教授: 朱子清, 賈忠健,周俊,揚崇仁, 碩士學位。
1978, 2 – 1982, 1: 中國蘭州大學化學系分析化學專業, 學士學位。
藥物化學方向。
成立美國Longwood藥物研究所,開始抗丙,乙型肝炎,抗腫瘤,及心血管藥物的研究與開發。其中,一個抗癌藥已成功以1000萬元人民幣轉讓給中國維和葯業。
主持領導Enanta抗丙型肝炎病毒NS3蛋白酶抑製劑項目,該項目完成向雅培(Abbott)的技術合作轉讓(總價值3.07億美元)。
抗丙型肝炎藥物ABT/EDP-450 臨床實驗I及臨床實驗II顯示非常好的結果。臨床實驗III已開始。
抗丙型肝炎葯藥物ABT/EDP-148臨床實驗已開始。
多個類型的後續抗丙型肝炎化合物的臨床前毒理及安全性研究已展開。
主持發明Enanta新一代大環內酯類抗生素3,6 – Bicyclolide (EDP-877,臨床前實驗證明了針對甲氧西林耐葯金黃色葡萄球菌MRSA,及針對社區獲得性肺炎CAP的優異活性)。
主持CMC開發第三代大環內酯類抗生素EDP-420,臨床I,II效果優良。與日本鹽野義(Shionogi)葯業合作開發亞洲市場,鹽野義葯業付 Enanta 2500萬美元頭期臨床專利授權費)。
主持CMC開發EDP-322(針對甲氧西林耐葯金黃色葡萄球菌 MRSA,及針對社區獲得性肺炎CAP) 臨床I已完成。
主持CMC開發EDP-5xx及EDP-1xx(針對社區獲得性肺炎CAP),臨床實驗I準備工作已完成。
參與開發Sustiva(HIV NNRTI非核苷逆轉錄酶抑製劑類抗艾滋病毒藥物)化學製造工藝。
作為Enanta製藥公司項目領導參與雅培公司 (Abbott) 合作開發抗丙肝新葯。
作為Enanta製藥公司CMC(化學、製造與控制)及cGMP管理領導參與日本Shionogi公司合作開發抗生素新葯。
擁有超過100項美國發明專利。
發表文章
Xu, G. Y; Tang, D. T.; Gai, Y.; Wang, G. Q.; Kim, H.; Chen, Z.; Phan, L. T.; Or, Y. S. and Wang, Zhe; An Efficient Large-Scale Synthesis of EDP-420, a First-in-Class Bridged Bicyclic Macrolide (BBM) Antibiotic Drug Candidate. Org. Proc. Res & Dev. 2010, 14, 504–510
Gai, Y.; Tang, D.; Xu, G.; Chen, Z.; Polemeropoulos, A.; Wang, Z.; Or, Y. S. Synthesis of 3,6-bicyclolides: A novel class of macrolide antibiotics. Bioorg. Med. Chem. Lett. 2008, 18, 6315.
Tang, D.; Gai, Y.; Chen, Z.; Polemeropoulos, A.; Wang, Z.; Or, Y. S. Design, synthesis, and antibacterial activities of novel 3,6-bicyclolide oximes: Length optimization and zero carbon linker oximes. Bioorg. Med. Chem. Lett. 2008, 18, 5078.
Choudhury, A.; Jin, F.; Wang, D.; Wang, Z.; Xu, G.; Confalone, P. N.; Pierce, M. E.; Nguyen, D. "A Concise Synthesis of anti-Viral Agent F-ddA, Starting from (S)-dihydro-5-(hydroxymethyl)-2(3H)-Furanone”, Tetrahedron Lett. 2003, 247.
Yang, Y.; Wang, Z.; Pan, X.; Lignans with Anti-HIV Properties” Huaxue Jinzhan. . 2003, 327.
Jin, F.; Wang, D.; Confalone, P. N.; Pierce, M. E.; Wang, Z.; Xu, G.; Choudhury, A.; Nguyen, D. "(2R, 3S, 5S)-2-Acetoxy-3-fluoro-5-(p-touloyloxymethyl) tetrahydrofuran: A Key Intermediate for the Synthesis of 9-(2,3-Dideoxy-2-fluoro-D-threo-pentofuranolsyl)adenine (F-ddA)", Tetrahedron Lett. 2001, 4787.
Kabalka, G. W.; Yang, K.; Wang, Z.; “Synthesis of Tertiary -Hydroxy Carboxylic Acids¾Allylboration of -keto Carboxylic Aicds via Neighboring Group Control”, Syn. Commun. 2001, 31, 511.
Wang, Z.; Xu, G.; Pierce, M. E. “Synthesis of Tertiary -Hydroxy Carboxylic Acids via Hypervalent Silicate”, Tetrahedron Lett. 2000, 41, 4523.
Kabalka, G. W.; Yang, K.; Wang, Z.; “The Reaction of -Ketoacids with Allylboronates”, in Contemporary Boron Chemistry, A. K. Hughes, M. Davidson Ed.; Royal Society of Chemistry, UK; 2000, 253, 454.
Wang, Z.; Campana, S.; Fortunak. J. “A New Method for the Synthesis of Vinyl Dihalides and Its Application to the Synthesis of Terminal Acetylenes." Tetrahedron Lett. 2000, 41, 4007.
Wang, Z.; Campana, S.; Yang, K.; Xu, G.; Pierce, M. E.; Fortunak. J. “A Practical Preparation of Terminal Acetylene from Aldehydes”, J. Org. Chem.;1999, 64, 1889.
Wang, Z.; Yin, J. G.; Campagna, S. A.; Pesti, J. A.; Fortunak, J. M. “An Alternative Approach for the Conversion of Aldehydes to Terminal Alkynes”, J. Org. Chem. 1999, 64, 6918.
Wang, Z.; Zhao, C. L.; Pierce, M. E.; Fortunak, J. M. “Enantioselective Synthesis of -Hydroxy Carboxylic Acids: Direct Conversion of -Oxocarboxylic Acids to Enantiomerically Enriched -Hydroxy Carboxylic Acids via Neighboring Group Control”, Tetrahedron Asymmetry, 1999, 10, 225.
Wang, Z.; La, B.; Fortunak, J. M.; Meng, X. J.; and Kabalka, G. W. “Enantioselective Synthesis of -Hydroxy Carboxylic Acids: Direct Conversion of -Oxocarboxylic Acids to Enantiomerically Enriched -Hydroxy Carboxylic Acids via Neighboring Group Control”, Tetrahedron Lett. 1998, 39, 5501.
Corey, E. J.; Wang, Z. "Conversion of Arachidonic Acid to the Prostaglandin Endoperoxide PGG2, A Chemical Analog of the Biosynthetic Pathway," Tetrahedron Lett. 1994, 35, 539.
Corey, E. J.; Wang, Z. "Enantioselective Conversion of Aldehydes to cyanohydrins by a Catalytic System with Separate Chiral Binding Sites for Aldehydes and Cyanide Components," Tetrahedron Lett. 1993, 34, 4001.
Wang, Z.; Chatla, N.; Wadgaonkar, P. P.; Kabalka, G. W. "Methylphenylborane, A New Hydroborating Reagent for the Syntheses of Totally Mixed Triorganoboranes," J. Organomet. Chem., 1992, 440, 243.
Kabalka, G. W.; Wang, Z.; Goodman, M. M. "Synthesis of Isomerically Pure N-13 Labeled -Aminobutyric Acid and Putrescine," Int. J. Radiat. Appl. Instrum. [A] 1992, 43, 389.
Wang, Z.; Meng, X.-J.; Kabalka, G. W. "The Stereoselective Crotylboration of -Oxocarboxylic Acids," Tetrahedron Lett. 1991, 32, 5677.
Wang, Z.; Meng, X.-J.; Kabalka, G. W. "The Addition of Allylboronates to -Oxocarboxylic Acids," Tetrahedron Lett. 1991, 32, 4619.
Wang, Z.; Meng, X.-J.; Kabalka, G. W. "The Stereoselective Allyl- and Crotylboration of -Hydroxyketones," Tetrahedron Lett. 1991, 32, 1945.
Kabalka, G. W.; Green, J. F.; Goodman, M. M.; Wang, Z.; Wadgaonkar, P. P. "Syntheses of Organoborane Polymers for Use in the Preparation of Nitrogen-13 Labeled Amines," J. Labeled Compds. & Radiopharm. 1991, 30, 409.
Kabalka, G. W.; Wang, Z. "Hydroboration / Amination of N-trimethylsilyl Protected Olefinic Amines and Diolefins: Syntheses of Isomerically Pure Diamines," Synth. Commun. 1990, 20, 2113.
Kabalka, G. W.; Wang, Z. "Preparation of Isomerically Pure Dialkylamines via the Reaction of Dimethylboranes with Chloralkylamine," Synth. Commun. 1990, 20, 231.
Kabalka, G W.; Wang, Z.; Goudgaon, N. M. "Preparation of Isomerically Pure Alkylamines via the Reaction of Dimethylboranes with Chloramine," Synth. Commun. 1989, 19, 2409.
Kabalka, G. W.; Wang, Z. "Reaction of Trialkylboranes with Alkylamines: Synthesis of Dialkylamines," Organometallics 1989, 8, 1093
Kabalka, G. W.; Green, J. F.; Wang, Z.; Goodman, M. M. "The Synthesis of Nitrogen-13 Labeled Butylamine Using Organoborane Polymers," J. Labeled Compds. & Radiopharm. 1988, 26, 90.
Yang, C. R.; Wang, Z. "Steroid Saponins from the Fresh Fruits of Dracaena Cambodiana," Acta Botanica Yunanica (Ch.) 1986, 8, 355.
Wang, Z.; Jia, Z.-j.; Zhu, T.-t.; Yang, C.-r.; Zhou, J. "Flavonoid Constituents from the Seeds of Camellia Oleifera," Acta Botanica Yunnanica (Ch.) 1986, 8, 157.
Wang, Z.; Jia, Z.-j.; Zhu, T.-t.; Yang, C.-r.; Zhou, J.; Kasai, R.; Tanaka, O. "The Triterpenoid Saponins of Rhizomes of Panax Japonicus C. A. Meyer Var. Angustifolius (Burk.) Chen et Chu," Acta Botanica Sinica (Ch.) 1985, 27, 618.
Ye, S.-b.; Wang, Z.; Chen, C.-y. "Syntheses of Chelating Resins and Their Applications in Analytical Chemistry," Journal of Suzhou Railway Teacher's University, Natural Science Edition (Ch.), 1984, 1, 60.