基本信息
段文虎  男  博导  中国科学院上海药物研究所
电子邮件: whduan@simm.ac.cn
通信地址: 上海市浦东新区祖冲之路555号
邮政编码: 201203

研究领域

1、 具有重要生理活性天然产物及其衍生物的合成和生物活性研究;
2、 新型抗肿瘤分子靶点药物研究。

招生信息

招收具有良好有机化学/药物化学背景,热爱本专业,勤奋踏实的研究生。
招生专业
100701-药物化学
招生方向
具有重要生理活性天然产物及其衍生物的合成和生物活性研究
新型抗肿瘤分子靶点药物研究

教育背景

1993-09--1996-06 中国科学院上海药物研究所 博士
1990-09--1993-06 华西医科大学 硕士
1982-09--1986-06 中国药科大学 学士
学历
-- 研究生
学位
-- 博士

教授课程

药物化学

专利与奖励

   
专利成果
[1] 丁健, 段文虎, 谢华, 耿美玉, 王彩霞, 詹正生, 高娜, 张阳. CSF1R激酶抑制剂及其用途. CN: CN114246864A, 2022-03-29.
[2] 段文虎, 沈旭, 王蔚, 王佳颖, 曹素芬, 吕建璐, 徐旭. 一种具有AMPK激动活性的化合物及其前药的制备和应用. CN: CN113549010A, 2021-10-26.
[3] 段文虎, 耿美玉, 詹正生, 谢作权, 赵凯燕, 郭玉婷, 王玺渊, 张燕, 周晓倩, 丁健. 五元杂环氧代羧酸类化合物及其医药用途. CN: CN112724127A, 2021-04-30.
[4] 段文虎, 丁健, 陈运, 谢华, 张惠斌, 周金培. 一类IRAK4激酶抑制剂及其制备和应用. CN: CN112480101A, 2021-03-12.
[5] 段文虎, 耿美玉, 张贺峰, 丁健, 艾菁, 彭霞, 季寅淳. 具有Axl与c-Met激酶抑制活性的化合物及其制备和应用. CN: CN112457295A, 2021-03-09.
[6] 段文虎, 丁健, 陈运, 谢华, 张惠斌, 周金培. 一类FLT3激酶抑制剂及其制备和应用. CN: CN111217816A, 2020-06-02.
[7] 段文虎, 耿美玉, 王蔚, 丁健, 艾菁, 许丹丹, 彭霞, 曹素芬, 季寅淳. 一种具有AXL抑制活性的化合物及其制备和应用. CN: CN110036014A, 2019-07-19.
[8] 段文虎, 耿美玉, 王玉明, 艾菁, 范珺, 戴阳, 丁健. 一种具有FGFR抑制活性的新型化合物及其制备和应用. CN: CN109328187A, 2019-02-12.
[9] 段文虎, 耿美玉, 王玉明, 艾菁, 范珺, 戴阳, 丁健. 一种具有FGFR抑制活性的新型化合物及其制备和应用. CN: CN109328187A, 2019-02-12.
[10] 段文虎, 耿美玉, 詹正生, 艾菁, 丁健. 氘代SGX523及其用途. CN: CN108864101A, 2018-11-23.
[11] 罗成, 段文虎, 朱孔凯, 邵敬伟, 毛瑞风, 张元元, 蒋华良. 2-取代硫基乙酰胺类化合物及其制备方法和应用. CN: CN108689946A, 2018-10-23.
[12] 段文虎, 罗成, 邵敬伟, 朱孔凯, 张元元, 丁宏, 蒋华良. 一种具有PRMT5抑制活性的化合物及其制备和应用. CN: CN108570059A, 2018-09-25.
[13] 段文虎, 耿美玉, 王蔚, 丁健, 艾菁, 许丹丹, 彭霞, 曹素芬, 季寅淳. 一种具有Axl抑制活性的化合物及其制备和应用. CN: CN108250200A, 2018-07-06.
[14] 段文虎, 沈旭, 陈静. N‑取代‑3,5‑二取代苯甲酰胺类化合物及其制备方法和应用. CN: CN107108656A, 2017-08-29.
[15] 段文虎, 耿美玉, 严伟, 丁健, 艾菁, 赵彬, 范珺, 彭霞, 陈奕. 吲唑类化合物的制备方法和用途. CN: CN106317023A, 2017-01-11.
[16] 段文虎, 耿美玉, 詹正生, 艾菁, 丁健. 氘代的3-(6-喹啉基)二氟甲基-6-(1-甲基)-4-吡唑基1,2,4三唑并4,3-b哒嗪及其应用. CN: CN106279176A, 2017-01-04.
[17] 段文虎, 耿美玉, 赵彬, 丁健, 艾菁, 范珺, 彭霞, 严伟, 陈奕. 吡唑并3,4-b吡啶类和吲唑类化合物的制备方法和用途. CN: CN106146493A, 2016-11-23.
[18] 段文虎, 沈旭, 陈静. N-取代-3,5-二取代苯甲酰胺类化合物及其制备方法和应用. CN: CN105837599A, 2016-08-10.
[19] 段文虎, 丁健, 吕永聪, 谢华. 萘酰胺类化合物、其制备方法和用途. CN: CN104860885A, 2015-08-26.
[20] 段文虎, 丁健, 吕永聪, 谢华. 苯胺嘧啶类化合物、其制备方法和医药用途. CN: CN104829542A, 2015-08-12.
[21] 万惠新, 夏广新, 沈竞康, 许志勇, 许振民, 石辰, 马珂, 段文虎, 林逸鹏, 姚珊燕. 二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用. CN: CN104341396A, 2015-02-11.
[22] 段文虎, 万惠新, 夏广新, 梅德盛, 林逸鹏, 刘学军, 沈竞康. 一类二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用. CN: CN103804358A, 2014-05-21.
[23] 朱大元, 左建平, 曲世津, 段文虎, 王桂凤. 苯并杂环类化合物及其制备方法和用途. CN: CN102219725B, 2013-10-09.
[24] 段文虎, 左建平, 李川, 陈炜, 唐炜, 左理, 孔芳园, 牛巍. 一类霉酚酸衍生物、其制备方法和用途. CN: CN102952105A, 2013-03-06.
[25] 段文虎, 耿美玉, 陈方, 艾菁, 陈奕, 詹正生, 吕永聪, 王英, 丁健. 1,2,4三唑并4,3-b1,2,4三嗪类化合物、其制备方法和用途. CN: CN102532141A, 2012-07-04.
[26] 朱大元, 左建平, 曲世津, 段文虎, 王桂凤. 苯并杂环类化合物及其制备方法和用途. CN: CN102219725A, 2011-10-19.
[27] 段文虎, 赵翠花, 蒋华良, 丁健, 陈晓蓓, 谢华. 苯胺喹唑啉衍生物、其制备方法及其用途. CN: CN101289445A, 2008-10-22.
[28] 段文虎, 赵曦, 张士磊, 丁健, 桂敏. 曲古抑菌素A衍生物及其制备方法和用途. CN: CN101239929A, 2008-08-13.
[29] 熊志奇, 段文虎, 陈迁. N-甲基-D-天冬氨酸受体在癫痫发生中的作用. CN: CN101226199A, 2008-07-23.
[30] 段文虎, 周云隆, 丁健. 藤黄酸衍生物及其制备方法和用途. CN: CN101054382A, 2007-10-17.
[31] 段文虎, 张土磊. 一种组蛋白脱乙酰酶抑制剂的手性全合成方法. CN: CN1939898A, 2007-04-04.
[32] 段文虎, 周云隆, 蒋华良, 丁健, 罗小民, 陈奕. 新藤黄酸衍生物及其制备方法和用途. CN: CN1715283A, 2006-01-04.
[33] 段文虎, 章建刚, 丁健, 陈奕, 蔡俊超. 一类5,8-二氢萘醌衍生物、其制备方法和用途. CN: CN1690044A, 2005-11-02.
[34] 陆群, 段文虎, 蔡俊超, 刘卫军, 丁健. 一类萘茜衍生物及其制备方法和用途. CN: CN1420111A, 2003-05-28.

出版信息

   
发表论文
[1] Zhengsheng Zhan, Yinchun Ji, Haixia Su, Chen Fang, Xia Peng, Qiufeng Liu, Yang Dai, Dongze Lin, Yechun Xu, Jing Ai, Wenhu Duan. Discovery of 10H-benzo[b]pyrido[2,3-e][1,4]oxazine AXL inhibitors via structure-based drug design targeting c-Met kinase. Journal of Medicinal Chemistry[J]. 2022, 第 11 作者  通讯作者  66(1): 220-234, http://dx.doi.org/10.1021/acs.jmedchem.2c00962.
[2] Xie, Zuoquan, Wang, Zhen, Fan, Fengying, Zhou, Jinpei, Hu, Zhaoxue, Wang, Qingxia, Wang, Xiyuan, Zeng, Qingzhong, Zhang, Yan, Qiu, Jiaxuan, Zhou, Xiaoqian, Xu, Hui, Bai, Hudagula, Zhan, Zhengsheng, Ding, Jian, Zhang, Huibin, Duan, Wenhu, Yu, Xuekui, Geng, Meiyu. Structural insights into a shared mechanism of human STING activation by a potent agonist and an autoimmune disease-associated mutation. CELL DISCOVERY[J]. 2022, 第 17 作者  通讯作者  8(1): http://dx.doi.org/10.1038/s41421-022-00481-4.
[3] Xu, Dandan, Sun, Deqiao, Wang, Wei, Peng, Xia, Zhan, Zhengsheng, Ji, Yinchun, Shen, Yanyan, Geng, Meiyu, Ai, Jing, Duan, Wenhu. Discovery of pyrrolo2,3-dpyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2021, 第 10 作者  通讯作者  220: http://dx.doi.org/10.1016/j.ejmech.2021.113497.
[4] Du, Daohai, Xu, Dandan, Zhu, Licheng, Stazi, Giulia, Zwergel, Clemens, Liu, Yanli, Luo, Zhongyuan, Li, Yuanqing, Zhang, Yuanyuan, Zhu, Kongkai, Ding, Yiluan, Liu, Jingqiu, Fan, Shijie, Zhao, Kaiyan, Zhang, Naixia, Kong, Xiangqian, Jiang, Hualiang, Chen, Kaixian, Zhao, Kehao, Valente, Sergio, Min, Jinrong, Duan, Wenhu, Luo, Cheng. Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2021, 第 22 作者  通讯作者  64(12): 8194-8207, http://dx.doi.org/10.1021/acs.jmedchem.0c02261.
[5] Chen, Yun, Bai, Gang, Li, Yan, Ning, Yi, Cao, Sufen, Zhou, Jinpei, Ding, Jian, Zhang, Huibin, Xie, Hua, Duan, Wenhu. Discovery and structure - activity relationship exploration of pyrazolo 1,5-apyrimidine derivatives as potent FLT3-ITD inhibitors. BIOORGANIC & MEDICINAL CHEMISTRY[J]. 2021, 第 10 作者  通讯作者  48: http://dx.doi.org/10.1016/j.bmc.2021.116422.
[6] Yuting Guo, Xia Peng, Yinchun Ji, Yitong Zhang, Jian Ding, Zhengsheng Zhan, Jing Ai, Wenhu Duan. Synthesis of triazolotriazine derivatives as c-Met inhibitors. Molecular Diversity[J]. 2021, 第 8 作者  通讯作者  25(2): 839-846, http://dx.doi.org/10.1007/s11030-020-10067-5.
[7] Zhang, Hefeng, Peng, Xia, Dai, Yang, Shao, Jingwei, Ji, Yinchun, Sun, Yiming, Liu, Bo, Cheng, Xu, Ai, Jing, Duan, Wenhu. Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2021, 第 10 作者  通讯作者  64(7): 3956-3975, http://dx.doi.org/10.1021/acs.jmedchem.0c02093.
[8] Lv, Jianlu, Wang, Wei, Zhu, Xialin, Xu, Xiaoju, Yan, Qiuying, Lu, Jian, Shi, Xiaofan, Wang, Zhengyu, Zhou, Jinpei, Huang, Xi, Wang, Jiaying, Duan, Wenhu, Shen, Xu. DW14006 as a direct AMPK alpha 1 activator improves pathology of AD model mice by regulating microglial phagocytosis and neuroinflammation. BRAIN BEHAVIOR AND IMMUNITY[J]. 2020, 第 12 作者  通讯作者  90: 55-69, http://dx.doi.org/10.1016/j.bbi.2020.07.041.
[9] Chen, Yun, Bai, Gang, Ning, Yi, Cai, Shi, Zhang, Tao, Song, Peiran, Zhou, Jinpei, Duan, Wenhu, Ding, Jian, Xie, Hua, Zhang, Huibin. Design and synthesis of Imidazo1,2-bpyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2020, 第 8 作者190: http://dx.doi.org/10.1016/j.ejmech.2020.112092.
[10] Zhang, Hefeng, Peng, Xia, Ji, Yinchun, Dai, Yang, Shen, Yanyan, Ai, Jing, Duan, Wenhu. A potent pyrimidinone Axl inhibitor DW17401. CANCER RESEARCH[J]. 2020, 第 7 作者80(16): https://www.webofscience.com/wos/woscc/full-record/WOS:000590059305068.
[11] Xu, Xu, Wang, Wei, Wang, Zhengyu, Lv, Jianlu, Xu, Xiaoju, Xu, Jiawen, Yang, Juanzhen, Zhu, Xialin, Lu, Yin, Duan, Wenhu, Huang, Xi, Wang, Jiaying, Zhou, Jinpei, Shen, Xu. DW14006 as a Direct AMPK alpha Activator Ameliorates Diabetic Peripheral Neuropathy in Mice. DIABETES[J]. 2020, 第 10 作者69(9): 1974-1988, http://dx.doi.org/10.2337/db19-1084.
[12] Jianlu Lv, Wei Wang, Xialin Zhu, Xiaoju Xu, Qiuying Yan, Jian Lu, Xiaofan Shi, Zhengyu Wang, Jinpei Zhou, Xi Huang, Jiaying Wang, Wenhu Duan, Xu Shen. DW14006 as a direct AMPKα1 activator improves pathology of AD model mice by regulating microglial phagocytosis and neuroinflammation. BRAIN BEHAVIOR AND IMMUNITY. 2020, 第 12 作者  通讯作者  90: 55-69, http://dx.doi.org/10.1016/j.bbi.2020.07.041.
[13] Zhu, Kongkai, Shao, Jingwei, Tao, Hongrui, Yan, Xue, Luo, Cheng, Zhang, Hua, Duan, Wenhu. Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity. JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN[J]. 2019, 第 7 作者  通讯作者  33(8): 775-785, https://www.webofscience.com/wos/woscc/full-record/WOS:000488949200006.
[14] Zheng, BaiNan, Ding, ChenHong, Chen, ShiJie, Zhu, Kongkai, Shao, Jingwei, Feng, Jifeng, Xu, WenPing, Cai, LingYan, Zhu, ChangPeng, Duan, Wenhu, Ding, Jin, Zhang, Xin, Luo, Cheng, Xie, WeiFen. Targeting PRMT5 Activity Inhibits the Malignancy of Hepatocellular Carcinoma by Promoting the Transcription of HNF4α. THERANOSTICS[J]. 2019, 第 10 作者9(9): 2606-2617, http://dx.doi.org/10.7150/thno.32344.
[15] Shao, Jingwei, Zhu, Kongkai, Du, Daohai, Zhang, Yuanyuan, Tao, Hongrui, Chen, Zhifeng, Jiang, Hualiang, Chen, Kaixian, Luo, Cheng, Duan, Wenhu. Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2019, 第 10 作者  通讯作者  164: 317-333, http://dx.doi.org/10.1016/j.ejmech.2018.12.065.
[16] Zhengsheng Zhan, Xia Peng, Yiming Sun, Jing Ai, Wenhu Duan. Evaluation of deuterium-labeled JNJ38877605: pharmacokinetic, metabolic, and in vivo antitumor profiles. Chemical Research in Toxicology[J]. 2018, 第 5 作者  通讯作者  31(11): 1213-1218, https://www.webofscience.com/wos/woscc/full-record/WOS:000451245200015.
[17] Wang, Yuming, Li, Lijun, Fan, Jun, Dai, Yang, Jiang, Alan, Geng, Meiyu, Ai, Jing, Duan, Wenhu. Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors (vol 61, pg 9085, 2018). JOURNAL OF MEDICINAL CHEMISTRY. 2018, 第 8 作者61(20): 9393-9393, https://www.webofscience.com/wos/woscc/full-record/WOS:000448754900028.
[18] Cao, Sufen, Zhang, Jiangang, Duan, Wenhu. Synthesis and Bioevaluation of Shikonin Derivatives. LETTERS IN DRUG DESIGN & DISCOVERY[J]. 2018, 第 3 作者  通讯作者  15(9): 945-950, https://www.webofscience.com/wos/woscc/full-record/WOS:000438897300004.
[19] Wang, Zhengyu, Shi, Xiaofan, Zhang, Huan, Yu, Liang, Cheng, Yanhua, Zhang, Hefeng, Zhang, Huibin, Zhou, Jinpei, Chen, Jing, Shen, Xu, Duan, Wenhu. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2017, 第 11 作者  通讯作者  139: 128-152, http://dx.doi.org/10.1016/j.ejmech.2017.07.051.
[20] Mao, Ruifeng, Shao, Jingwei, Zhu, Kongkai, Zhang, Yuanyuan, Ding, Hong, Zhang, Chenhua, Shi, Zhe, Jiang, Hualiang, Sun, Dequn, Duan, Wenhu, Luo, Cheng. Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2017, 第 10 作者  通讯作者  60(14): 6289-6304, http://dx.doi.org/10.1021/acs.jmedchem.7b00587.
[21] Zhengsheng Zhan, Xia Peng, Qiufeng Liu, Fang Chen, Yinchun Ji, Shanyan Yao, Yong Xi, Yipeng Lin, Tiantian Chen, Yechun Xu, Jing Ai, Meiyu Geng, Wenhu Duan. Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor. European Journal of Medicinal Chemistry[J]. 2016, 第 13 作者  通讯作者  116: 239-251, http://dx.doi.org/10.1016/j.ejmech.2016.03.076.
[22] Li, Mengyuan, Lv, Yongcong, Tong, Linjiang, Peng, Ting, Qu, Rong, Zhang, Tao, Sun, Yiming, Chen, Yi, Wei, Lixin, Geng, Meiyu, Duan, Wenhu, Xie, Hua, Ding, Jian. DW10075, a novel selective and small-molecule inhibitor of VEGFR, exhibits antitumor activities both in vitro and in vivo. ACTA PHARMACOLOGICA SINICA[J]. 2016, 第 11 作者  通讯作者  37(3): 398-407, http://lib.cqvip.com/Qikan/Article/Detail?id=668260644.
[23] Meng-yuan LI, Yong-cong LV, Lin-jiang TONG, Ting PENG, Rong QU, Tao ZHANG, Yi-ming SUN, Yi CHEN, Li-xin WEI, Mei-yu GENG, Wen-hu DUAN, Hua XIE, Jian DING. DW10075, a novel selective and small-molecule inhibitor of VEGFR, exhibits antitumor activities both in vitro and in vivo. 中国药理学报:英文版[J]. 2016, 第 11 作者398-407, http://lib.cqvip.com/Qikan/Article/Detail?id=668260644.
[24] Sufen Cao, Wenhu Duan. Microwave assisted solvent-free CsbndH amination by silica-supported manganese dioxide. TETRAHEDRON LETTERS. 2016, 第 2 作者57(22): 2390-2394, http://dx.doi.org/10.1016/j.tetlet.2016.04.061.
[25] Fan, Jun, Dai, Yang, Shao, Jingwei, Peng, Xia, Wang, Chen, Cao, Sufen, Zhao, Bin, Ai, Jing, Geng, Meiyu, Duan, Wenhu. Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2016, 第 10 作者  通讯作者  26(11): 2594-2599, http://dx.doi.org/10.1016/j.bmcl.2016.04.028.
[26] Yan, Wei, Huang, Zhaoru, Wang, Zhengyu, Cao, Sufen, Tong, Linjiang, Zhang, Tao, Wang, Chen, Zhou, Lin, Ding, Jian, Luo, Cheng, Zhou, Jinpei, Xie, Hua, Duan, Wenhu. Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation. CHEMICAL BIOLOGY & DRUG DESIGN[J]. 2016, 第 13 作者  通讯作者  87(5): 694-703, https://www.webofscience.com/wos/woscc/full-record/WOS:000374031500006.
[27] Cao, Sufen, Duan, Wenhu. Microwave assisted solvent-free C-H amination by silica-supported manganese dioxide. TETRAHEDRON LETTERS[J]. 2016, 第 2 作者  通讯作者  57(22): 2390-2394, https://www.webofscience.com/wos/woscc/full-record/WOS:000376695700012.
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指导学生

已指导学生

章建刚  博士研究生  070303-有机化学  

赵翠花  硕士研究生  070303-有机化学  

赵曦  硕士研究生  100701-药物化学  

张士磊  博士研究生  100701-药物化学  

左理  博士研究生  100701-药物化学  

王文晶  硕士研究生  100701-药物化学  

胡珂  硕士研究生  100701-药物化学  

周琳娜  硕士研究生  100701-药物化学  

曲世津  博士研究生  100701-药物化学  

陈方  硕士研究生  100701-药物化学  

焦宇  博士研究生  100701-药物化学  

现指导学生

吴建睿  硕士研究生  077901-药物化学  

陈炜  博士研究生  100701-药物化学  

陈方  博士研究生  100701-药物化学  

叶苓  博士研究生  100701-药物化学  

赵彬  硕士研究生  077901-药物化学  

吕永聪  博士研究生  100701-药物化学  

詹正生  博士研究生  100701-药物化学  

课题组简单介绍

    我的主要研究目的是研究发现新型抗肿瘤药物,主要方向有:1、具有重要生理活性天然产物及其衍生物的合成和生物活性研究;2、 新型抗肿瘤分子靶点药物研究。 目前已在国内外重要学术期刊发表论文60余篇,参与了“天然产物化学”以及“药物化学进展”两部专著的章节编写;申请专利10多项,其中已获授权3项。

工作经历

   
工作简历
2000-11--今 中国科学院上海药物研究所 研究员
1997-01--2000-10 美国德州大学药学院 博士后
1986-07--1990-08 江苏常州第三制药厂 工程师