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男, 全球健康药物研究中心, 教授/研究员/教授级高工或同等级别
学习/工作经历
PROFESSIONAL EXPERIENCE
2021-now Director, Chemistry, Global Health Drug Discovery Institute (GHDDI), Beijing, China.
2020-2021 Senior VP, Preclinical, Galixir, Beijing, China.
2018-2020 Chemistry VP, Helios Huaming BioPharma, Suzhou, China.
2014-2019 Consultant, Cardiovascular Disease, Tasly, Tianjin, China.
2013-2014 Chemistry VP, Ascepion Pharmaceuticals, Suzhou, China.
2011-2016 Taishan Scholar, Medicinal and Environmental Chemistry and Biology, Qingdao University of Technology, Qingdao, China.
2009-2011 Senior Principal Scientist, Medicinal Chemistry, Infectious Diseases, Merck Research Laboratories, Kenilworth, NJ 07033.
1990-2009 Senior Principal Scientist, Cardiovascular, Metabolic & CNS Chemistry, Schering-Plough Research Institute, Kenilworth, NJ 07033.
1982-1984 Research and Teaching Faculty; Physical and Structural Organic Chemistry Laboratory, Department of Chemistry, Nankai University, Tianjin, China.
EDUCATION
1989-1990 Postdoctoral Visiting Fellow (Advisor: Dr. J. Pitha) on a Fogarty fellowship grant; Macromolecular Chemistry Section, Laboratory of Molecular and Cellular Biology, National Institute on Aging/NIH, Baltimore, MD
1984-1989 PhD (Organic Synthesis, Advisor: Prof. A. P. Kozikowski), University of Pittsburgh, Pittsburgh, PA 15260. Received the Andrew Mellon predoctoral fellowship from 1986-1988.
1978-1982 BS (Organic Chemistry), Nankai University, Tianjin, China. Received the World Bank scholarship for graduate study.
研究领域和兴趣
新药研发、药物化学、有机化学
主要业绩
1982年南开大学化学系本科毕业,获世界银行贷款奖学金,赴美国匹兹堡大学(University of Pittsburgh)攻读有机合成博士学位。期间,获梅隆奖学金并完成天然产物石杉碱甲(Huperzine A)全合成。石杉碱甲具有治疗老年痴呆症药效。1988-1990年,在美国健康研究所(National Institutes of Health,NIH)从事环糊精衍生物在药剂应用方面的博士后研究工作。
1990-2011年,在美国大型制药公司仙灵保雅(Schering-Plough)和默克/默沙东(Merck/MSD)从事先导物优化方面的新药研发工作,任资深主任研究员。参与降血压、心血管病,糖尿病,中枢神经,肝炎等新药项目十余种。主要代表性成果有:1)抗血栓新药-凝血酶受体拮抗剂Vorapaxar,于2014年上市。2008年获爱迪生发明奖,1996、2003年二获公司科研奖。2)帕金森病新药-A2a受体拮抗剂Preladenant,完成三期临床试验。2009年获爱迪生发明奖。
代表成果
Publications:
1. Jayne, Charles L.; Andreani, Teresa; Chan, Tin-Yau; Chelliah, Mariappan V.; Clasby, Martin C.; Dwyer, Michael; Eagen, Keith A.; Fried, Steve; Greenlee, William J.; Guo, Zhuyan; Xia, Yan; et al. Discovery of hydroxy pyrimidine Factor IXa inhibitors. Bioorganic & Medicinal Chemistry Letters (2020), 30(15), 127279.
2. Neelamkavil, Santhosh F.; Stamford, Andrew W.; Kowalski, Timothy; Biswas, Dipshikha; Boyle, Craig; Chackalamannil, Samuel; Xia, Yan; Jayne, Charles; Neustadt, Bernard; Hao, Jinsong; et al. Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes. ACS Medicinal Chemistry Letters (2018), 9(5), 457-461.
3. Shi, JS; Tan, WQ; Cui, H; Feng, YZ; Xia; Y. “Recent development of thrombin antagonists as antithrombotics”, 《Chinese Medicinal Chemistry》, 2014, 24(2): 129-137.
4. Yan Xia, Samuel Chackalamannil, William J. Greenlee, Charles Jayne, Bernard Neustadt, Andrew Stamford, Henry Vaccaro, Xiaoying (Lucy) Xu, Hana Baker, Kim O’Neill, Morgan Woods, Brian Hawes, and Tim Kowalski. Discovery of a Nortropanol Derivative as a Potent and Orally Active GPR119 Agonist for Type 2 Diabetes. Bioorganic & Medicinal Chemistry Letters (2011), 21(11), 3290-3296.
5. Xia, Yan; Chackalamannil, Samuel; Greenlee, William J.; Wang, Yuguang; Hu, Zhiyong; Root, Yuriko; Wong, Jesse; Kong, Jianshe; Ahn, Ho-Sam; Boykow, George; Hsieh, Yunsheng; Kurowski, Stan; Chintala, Madhu. Discovery of a vorapaxar analog with increased aqueous solubility. Bioorganic & Medicinal Chemistry Letters (2010), 20(22), 6676-6679.
Patents:
1. Xia, Yan; McIver, Edward Giles; Song, Yang; Xu, Yuanyuan; Zhu, Lin; Chu, Chunjun; Wu, Ling; Liu, Miao; Bryans, Justin Stephen. Preparation of substituted tricyclic heterocyclic compounds as selective LRRK2 inhibitors for the treatment of cancer and neurodegenerative diseases. PCT Int. Appl. (2017), WO 2017215600
2. Xia, Yan; Han, Min; Li, Wei; Chu, Yang; Bai, Guirong; Tian, Wenli; Li, Ju; Zhou, Wei; Wang, Guocheng; He, Yi; et al. Preparation of himbacine analogues and pharmaceutical compns. thereof. PCT Int. Appl. (2017), WO 2017181994.
3. Xia, Yan; Han, Min; Li, Wei; Chu, Yang; Bai, Guirong; Tian, Wenli; Li, Ju; Zhou, Wei; Wang, Guocheng; He, Yi; et al. New Himbacine analogue and application in medicines. PCT Int. Appl. (2017), WO 2017181993.
4. Xia, Yan; Chackalamannil, Samuel. Combination therapies comprising PAR1 antagonists with PAR4 antagonists for treatment of diseases assocd. with thrombosis. PCT Int. Appl. (2009), WO 2009124103
5. Xia, Yan; Boyle, Craig D.; Greenlee, William J.; Chackalamannil, Samuel; Jayne, Charles Lee; Stamford, Andrew W.; Dai, Xing; Harris, Joel M.; Neustadt, Bernard R.; Neelamkavil, Santhosh Francis; Shah, Unmesh G.; Lankin, Claire M.; Liu, Hong. Bicyclic heterocycle derivatives and methods of use thereof. PCT Int. Appl. (2009), WO 2009055331
MEETING PRESENTATIONS:
1. Xia, Y. et al “Synthesis of F16618analogs and their antithrombotic activities”, Chinese Chemical Society Annual Meeting, Beijing, China, 2014-08-04.
2. Yan Xia,* Samuel Chackalamannil, William J. Greenlee, Yuguang Wang, Zhiyong Hu, Yuriko Root, Michael Czarniecki,Ho-Sam Ahn, George Boykow, Yunsheng Hsieh, Stan Kurowski, and Madhu Chintala. Discovery of a Vorapaxar Analog with Increased Aqueous Solubility, 10th Winter Conference on Medicinal & Bioorganic Chemistry, Steamboat Springs, Colorado, 23rd – 27th January 2011, poster.
3. Speaker: “Himbacine-Derived Thrombin Receptor Antagonist (TRA) – A Case Study", SAPA China Pharmaceutical & Biotechnology Conference/Bio-Forum 2007, July 3-5, 2007, Shanghai, China
4. Speaker: “New Approach to Cardiovascular Disease", China 2006 International Pharmaceutical and Biotech Symposium Co-sponsored by SAPA in Zhengzhou, China, 6/22/06.
5. Speaker: "Himbacine-based Thrombin Receptor (PAR-1) Antagonists", The 26th Gulf Coast Chemistry Conference, Pensacola Beach, Florida, September 10, 2004.
*以上信息由高级会员个人更新和维护。