Shanghai Institute of Material Medical Chinese Academy of Sciences

Biography

Doctor YANG Yushe received his Ph. D. degree from shanghai Institute of Materia Medica, Chinese Academy of Sciences in 1996 and at present he is the principal instructor, Ph.D. supervisor and researcher at shanghai Institute of Materia Medica, Chinese Academy of Sciences.

The major research field of Prof. YANG’s group covers antibacterial agent, antineoplastic and antithrombotic drug discovery and developments. In 2009, the first new fluoroquinolone antibacterial agent with independent intellectual property―antofloxacin hydrochloride (NCE) was successfully developed by YANG’s group. It is recognized as the landmark achievement of the “Key New Drug Creation and Manufacturing Program” of the “Eleventh Five-year Plan” in China, filling up the innovation gap in this field of China in more than 40 years . Antofloxacin hydrochloride has a better safety profile and pharmacokinetic property than that of Levofloxacin and Moxifloxacin and its successful marketing is of great importance to the promotion of national innovative drug research and self-innovative ability in China.

In recent years, Prof. YANG has completed preclinical studies of two Candidate drugs, a FXa inhibitor YG-001 and oxazolidinone derivatives YG-056SP, which was licensed to pharmaceutical companys. A total of over 64 papers have been published in core periodicals at home and abroad including J. Med. Chem., J. Org. Chem., Eur. J. Med. Chem., etc. 50 China or international patent applications were submitted.

EDUCATION

09/01/1983-08/01/1987, Sichuan University Bachelor’s Degree in Chemistry

09/01/1987-08/01/1990, Sichuan University Master’s Degree in Organic Chemistry

09/01/1993-08/01/1996, Shanghai Institute of Materia Medica, Chinese Academy of Sciencess Ph.D. in Organic Chemistry/Medicinal Chemistry

09/01/1996-08/01/1998, Shanghai Institute of Materia Medica, Chinese Academy of Sciencess Postdoctoral Research

WORK EXPERIENCE

09/01/1990-08/01/1993, Xi’an Modern Chemistry Research Institute

09/01/1998-Present, Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Research Directions

Knowledge based innovative drug discovery and development, mainly focused on antibacterial agents against multidrug resistant bacteria, anticoagulant drugs and Anticancer drug

Grants & Research Projects

1. National Natural Science Foundation of China, Y901601011, Yushe Yang, 2019.01-2022.12

2. National Natural Science Foundation of China, 82073684, Yushe Yang, 2021.01-2024.12

Achievements

1. Class 1.1 Chemical New Drug Antofloxacin Hydrochloride

2. Antibacterial Agents against Multidrug Resistant Bacteria- YG-056SP

3. FXa inhibitor YG-001

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Social Titles

1.Member of academic committee of Shanghai Institute of Materia Medica, Chinese Academy of Sciences

2.Member of the editorial advisory board of Zhongguo Yiyao Gongye Zazhi

3.Member of professional committee on medicinal chemistry, Chinese Pharmaceutical Association

4.Member of professional committee on medicinal chemistry, Shanghai Pharmaceutical Association

5.Member of professional committee on antibiotics, Shanghai Pharmaceutical Association

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Awards & Honors

1.The 2017 Second prize of national technical invention

2.The 2015 first prize of Shanghai technical invention

3.The 2013 China Pharmacy Development Award-Innovative Drugs Award-Outstanding Achievement Award.

4.In 2010, he won the title of “2007-2009 Advanced Worker in Shanghai (Model Worker)”

5.The 2013 China Pharmacy Development Award-Innovative Drugs Award-Outstanding Achievement Award, Chinese Pharmaceutical Association

6.The 2013 Special Government Allowances of the State Council, State Council

7.The 2009 Creation Prize of China International Industry Fair (Antofloxacin Hydrochloride), China International Industry Fair

8.The Second Prize of 2007 WuXi AppTec Life Science and Chemistry Award, WuXi AppTec Company

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Pubilcations

Full Publication List

Selected Publications

1.Chenghui Shi, Yinyong Zhang, Ting Wang, Wenchao Lu, Shuhua Zhang, Bin Guo, Qian Chen, Cheng Luo, Xianli Zhou,* and Yushe Yang*, Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria，J. Med. Chem. 2019, 62（6）, 2950-2973

2.Deyu Kong, Tao Xue, Bin Guo, Jianjun Cheng, Shunyin Liu, Jianhai Wei, Zhengyu Lu, Haoran Liu, Guoqing Gong, Tian Lan, Wenhao Hu, and Yushe Yang*，Optimization of P2Y12 Antagonist Ethyl 6？(4-((Benzylsulfonyl) carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties，J. Med. Chem. 2019, 62（6）, 3088-3106

3.Liang Tan, Yunliang Tao, Ting Wang, Feng Zou, Shuhua Zhang, Qun huan Kou, Ao Niu, Qian Chen, Wenjing Chu,Xiaoyan Chen, Haidong Wang, and Yushe Yang*.Discovery of Novel Pyridone-Conjugated Monosulfactams as Potent and Broad-Spectrum Antibiotics for Multidrug-Resistant Gram-Negative Infections. J. Med. Chem. 2017, 60, 2669–2684

4.Xue, T.; Ding, S.; Guo, B.; Zhou, Y.; Sun, P.; Wang, H.; Chu, W.; Gong, G.; Wang, Y.; Chen, X.; Yushe Yang*. Design, Synthesis, and Structure-Activity and Structure-Pharmacokinetic Relationship Studies of Novel [6,6,5] Tricyclic Fused Oxazolidinones Leading to the Discovery of a Potent, Selective, and Orally Bioavailable FXa Inhibitor. J. Med. Chem. 2014, 57, 7770-7791

5.Chenyu Ling, Liqiang Fu, Suo Gao, Hui Wang, Yanqin Huang, Xiaoyan Chen and Yushe Yang*, Design, Synthesis, and Structure-Activity Relationship Studies of Novel Thioether Pleuromutilin Derivatives as Potent Antibacterial Agents. J. Med.Chem.2014,57，4772-4795

6.Xufeng Cao, , Zhaoshuan Sun, ,Yongbing Cao, Ruilian Wang, Wenjing Chu Wenhao Hu, Yushe Yang,* Design, synthesis, and structure–activity relationship studies of novel fused – heterocycle - linked triazoles with high activity and water solubility. J. Med.Chem. 2014,57,3687-3760

7.Bin Guo, Houxing Fan, Qisheng Xin, Wenjing Chu, Hui Wang, Yanqin Huang, Xiaoyan Chen, and Yushe Yang* Solubility-Driven Optimization of (Pyridin-3-yl) Benzoxaziny l-Oxazolidinones Leading to a Promising Antibacterial Agent. J. Med.Chem.2013,56, 2642-2650

8.Qisheng Xin, Houxing Fan, Bin Guo, Huili He, Suo Gao, Hui Wang, Yanqin Huang, Weiliang Zhu, Yushe Yang* Design, Synthesis and Structure-Activity Relationship Studies of Highly Potent Novel Benzoxazinyl - Oxazolidinone Antibacterials. J. Med.Chem.2011,54, 7493-7502

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