秦俊东北计算机博士,秦 俊 教授-云南大学省部共建教育部自然资源药物化学重点实验室...

秦俊，博士

研究方向：药物化学和有机化学

学位：博士

毕业学校：The University of Vermont, USA(美国佛蒙特大学化学系)

职称：教授/博导

电子邮件:qinjun@ynu.edu.cn

职业经历

2013/07-现在:教授—云南大学化学科学与工程学院，昆明。

2009/11-2013/06:副主任科学家—Merck Research Laboratories, New Jersey

2005/01-2009/10: 副主任科学家—Schering-Plough Research Institute, New Jersey

教育背景

2003/03-2004/12: 博士后—Indiana University

1998/09-2003/02: 博士学位—University of Vermont

1996/09-1998/06: 联合培养硕士研究生—四川大学/上海有机化学研究所

1992/09-1996/06: 本科学位—四川大学

获得奖励

2012:云南省高端科技人才引进计划

2011:云南省百名海外高层次人才引进计划

2005: President’sAwardfor Discovery, Schering-PloughResearch Institute

2003: Doctoral Scholar Award, University ofVermont

1999: Graduate Research Fellowship, Vermont NSF EPSCoR, University of Vermont

1997: Graduate Scholarship for Excellence, Sichuan University

1996: Award for Top 2% Graduate Student, Sichuan University

发表文章

2．Li, H.; Qin, J.; Dhondi, P.; Zhou, W.; Vicarel, M.; Bara, T.; Cole, D.; Josien, H.; Pissarnitski, D.; Zhu, Z.; Palani, A.; Aslanian, R.; Clader, J.; Czarniecki, M.; Greenlee, W.; Cohen-Williams, M.; Hyde, L.; Song, L.; Zhang, L.; Chu, I.; Huang, X.“

The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.”

Bioorg. Med. Chem. Lett.2013,23, 466-471.

4．Huang, X.; Su, J.; Rao, A.; Tang, H.; Zhou, W.; Zhu, X.; Chen, X.; Liu, Z.; Huang, Y.; Degrado, S.; Xiao, D.; Qin, J.;Aslanian, R.; McKittrick, B.; Greenfeder, S.; Van Heek, M.; Chintala, M.; Palani, A.“SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonists.”Bioorg.Med.Chem. Lett.2012,22, 854-858.

5．Sun, Z.; Asberom, T.; Bara, T.; Bennett, C.; Burnett, D.; Chu, I.; Clader, J.; Cohen-Williams, M.; Cole, D.; Czarniecki, M.; Durkin, J.; Gallo, G.; Greenlee, W.; Josien, H.; Huang, X.; Hyde, L.; Jones, N.; Kazakevich, I.; Li, H.; Liu, X.; Lee, J.; MacCoss, M.; Mandal, M.; McCracken, T.; Nomeir, A.; Mazzola, R.; Palani, A.; Parker, E.;Pissarnitski, D.; Qin, J.; Song, L.; Terracina, G.; Vicarel, M.; Voigt, J.; Xu, R.; Zhang, L.; Zhang, Q.; Zhao, Z.; Zhu, X.; Zhu, Z.“Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.”J. Med. Chem.2012, 55,489-502.

6．Qin, J.;Dhondi, P.; Huang, X.; Aslanian, R.; Fossetta, J.; Fang, T.;Lundell, D.;Palani, A.“Discovery ofapotentdihydrooxadiazole series of non-ATP-competitive MK2 (MAPKAPK2) inhibitors.”ACS Med. Chem.Lett.2012,3, 100-105.

7．Palani, A.;Rao, A.; Chen, X.; Huang, X.; Su, J.; Tang, H.; Huang, Y.;Qin, J.; Xiao, D.; Degrado, S.;Sofolarides, M.; Zhu, X.; Liu, Z.; McKittrick, B.; Zhou, W.;Aslanian, R.; Greenlee, W.; Senior, M.;Cheewatrakoolpong, B.; Zhang, H.; Farley, C.; Cook, J.;Kurowski, S.; Li, Q.;VanHeek, M.; Wang, G.; Hsieh, Y.; Li, F.;Greenfeder, S.; Chintala, M. “Discovery of SCH 900271, a potent nicotinic acid receptor agonist for the treatment of dyslipidemia.”ACS Med. Chem. Lett.2012,3,63-68.

8．Qin, J.;Zhou, W.; Huang, X.; Dhondi, P.; Palani, A.; Aslanian, R.; Zhu, Z.; Greenlee, W.; Cohen-Williams, M.; Jones, N.; Hyde, L.; Zhang, L. “Discovery of a potent pyrazolopyridine series of γ-secretase modulators.”ACSMed. Chem.Lett.2011,2, 471-476.

9．Qin, J.;Dhondi, P.; Huang, X.;Mandal, M.; Zhao, Z.;Pissarnitski, D.; Zhou, W.;Aslanian, R.; Zhu, Z.; Greenlee, W.;Clader, J.; Zhang, L.; Cohen-Williams, M.; Jones, N.; Hyde, L.;Palani, A.“Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.”Bioorg. Med. Chem. Lett.2011,21, 664-669.

10．Qin, J.;Rao, A.; Chen, X.; Zhu, X.; Liu, Z.; Huang, X.;Degrado, S.; Huang, Y.; Xiao, D.; Aslanian, R.; Cheewatrakoolpong, B.; Zhang, H.; Greenfeder, S.; Farley, C.; Cook, J.; Kurowski, S.; Li, Q.;Van Heek, M.; Chintala, M.; Wang, G.; Hsieh, Y.; Li, F.; Palani, A.“Discovery of a potent nicotinic acid receptor agonist for the treatment of dyslipidemia.”ACS Med. Chem. Lett.2011,2, 171-176.

11．Friestad, G. K.; Ji, A.; Korapala, C. S.; Qin, J.“Intermolecular radical addition toN-acylhydrazones as a stereocontrol strategy for alkaloid synthesis: formal synthesis of quinine.”Org.

Biomol.Chem.2011,9,4039-4043.

12．Huang, X.; Aslanian, R.; Zhou, W.; Zhu, X.; Qin, J.; Greenlee, W.; Zhu, Z.; Zhang, L.; Hyde, L.; Chu, I.; Cohen-Williams, M.; Palani, A. “The discovery of pyridone and pyridazoneheterocycles as γ-secretase modulators.”ACS Med.Chem.Lett.2010,1, 184-187.

13．Evans, P.A.; Qin, J.;Robinson, J.E.; Bazin, B.“Enantioselective total synthesis of the polycyclic guanidine containing marine alkaloid, (-)-Batzelladine D.”Angew.Chem.Int.Ed.2007,46, 7417-7419.

14．Korapala, C.S.; Qin, J.;Friestad, G. K.“Quinine synthesis studies: a radical-ionic annulation via Mn-mediated addition to chiralN-acylhydrazones.”Org.Lett.2007,9,4243-4246.

15．Friestad, G.K.; Marie, J.-C.; Suh, Y.; Qin, J. “Mn-mediated coupling of alkyl iodides andN-acylhydrazones: optimization, scope and evidence of radical mechanism.”J. Org. Chem.2006,71, 7016-7027.

16．Friestad, G.K.; Draghici, C.; Soukri, M.; Qin, J.“Radical addition approach to asymmetric amine synthesis: design, implementation, and comparison of new chiralN-acylhydrazones.”J. Org. Chem.2005,70, 6330-6338.

17．Qin, J.;Friestad, G.K.“Stereocontrol in hydride addition to ketone-derived chiralN-acylhydrazones.”Tetrahedron,2003,59, 6393-6402.

18．Friestad,G.K.; Qin,J. “Intermolecular alkyl radical addition to chiralN-acylhydrazones mediated by manganese carbonyl.”J.Am.Chem.Soc.2001,123,9922-9923.

19．Friestad, G.K.; Qin, J. “Highly stereoselective intermolecular radical addition to aldehyde hydrazones from chiral 3-amino-2-oxazolidinone.”J.Am. Chem. Soc.2000,122, 8329-8330.

20．Li, X.-S.; Qin, J.; Zhang, X.-L.; Xie, R.-G.“A convenient synthesis of chiral sulfur-containingmacrocyclic ligands.”Synth.Commun.1997,27,3079-3085.

发表专利

1．Boyce, C.; Degrado, S.; Chen, X.; Qin, J.; Mazzola, R.; Yu, Y.; McCormick, K.; Palani, A.; Xiao, D.; Aslanian, R.; Wu, J.; Rao, A.; Siliphaivanh, P.; Methot, J.; Zhang, H.; Kelley, E.; Brown, W.; Jiang, Q.; Gauuan, J.; Leyhane, A.; Biju, P.; Dhondi, P.; Dong, L.; Fevrier, S.; Huang, X.; Vaccaro, H.“Preparation of quinoxaline derivatives for use as CRTH2 receptor modulators.”PCTInt. Appl. WO2012087861,2012.

2．Aslanian, R.; Boyce, C.; Mazzola, R.; Mckittrick, B.; Mccormick, K.; Palani, A.; Qin, J.; Tang, H.; Xiao, D.; Yu, Y.; Caldwell, J.; Kelley, E.; Zhang, H.; Siliphaivanh, P.; Maccoss, R.; Methot, J.; Gauuan, J.; Jiang, Q.; Leyhane, A.; Biju, P.; Dong, L.; Huang, X.; Shao, N.; Zhou, W.; Dhondi, P.“Preparation of quinazolinone compounds as CRTH2 antagonists.”PCTInt.Appl. WO 2012051036,2012.

3．Zhu, Z.; Greenlee, W. J.; Huang, X.; Qin, J.; Liu, X.; Li, H.; Zhou, W.; Palani, A.; Zhu, X.; Vicarel, M. L.; Mandal, M.; Sun, Z.; Bennett, C. E.; McCracken, T. M.; Gallo, G. V.“Heterocyclic compounds as gamma-secretase modulators and their preparation and use in the treatment of CNS diseases.”PCT Int.Appl.WO 2010056849,2010.

4．Zhu, Z.; Greenlee, W. J.; Li, H.; Vicarel, M. L.; Qin, J.;Dhondi, P. K.; Huang, X.; Palani, A.; Liu, X.; Sun, Z.; Josien, H. B.; Xu, R.; Cole, D. J.; Burnett, D. A.; Bennett, C. E.; Mccracken, T. M.; Maccoss, M.“Heterocyclic compounds as gamma-secretase modulators and their preparation and use in the treatment of CNS diseases.”PCT Int. Appl. WO 2010056722,2010.

5．Zhu, Z.; Greenlee, W. J.; Cole, D. J.; Pissarnitski, D. A.; Gallo, G. V.; Li, H.; Josien, H. B.; Qin, J.; Knutson, C. E.; Mandal, M.; Vicarel, M. L.; Rajagopalan, M.; Dhondi, P. K.; Xu, R.; Sun, Z.; Bara, T. A.; Huang, X.; Zhu, X.; Zhao, Z.; Clader, J. W.; Palani, A.; Asberom, T.; McCracken, T. M.; Bennett, C. E. “Heterocyclic compounds as gamma-secretase modulators and their preparation and use in the treatment of CNS diseases.”PCTInt.Appl.WO 2010054078,2010.

6．Zhu, Z.; Greenlee, W. J.; Cole, D. J.; Pissarnitski, D. A.; Gallo, G. V.; Li, H.; Josien, H. B.; Qin, J.; Knutson, C. E.; Mandal, M.; Vicarel, M. L.; Rajagopalan, M.; Dhondi, P. K.; Xu, R.; Sun, Z.; Bara, T. A.; Huang, X.; Zhu, X.; Zhao, Z.; Clader, J. W.; Palani, A.; Asberom, T.; McCracken, T.; Bennett, C.E.“Heterocyclic compounds as gamma-secretase modulators and their preparation and use in the treatment of CNS diseases.”PCT Int. Appl.WO 2010054067,2010.

7．Huang, X.; Palani, A.; Aslanian, R. G.; Zhu, Z.; Pissarnitski, D. A.; Li, H.; Greenlee, W. J.; Zhao, Z.; Mazzola, R. D., Jr.; Qin, J.;Dhondi, P.“Preparation of novel heterocyclic compounds as gamma-secretase modulators for the treatment of Alzheimer's disease.”PCT Int.Appl. WO2009108766,2009.

8．Huang, X.; Palani, A.; Qin, J.;Aslanian, R. G.; Zhu, Z.; Greenlee, W. J. “Quinazolines and related compounds as gamma-secretase modulators and their preparation and use in the treatment of Alzheimer's disease.”PCT Int.Appl.WO 2009073779,2009.

9．Huang, X.; Palani, A.; Qin, J.;Aslanian, R. G.; Zhu, Z.; Greenlee, W. J.; Josien, H.; Zhou, W.; Zhu, X.; Bennett, C. E.; Pissarnitski, D.; Mandal, M.; Dhondi, P.; McCracken, T.; Bara, T.; Zhao, Z.; Burnett, D.; Clader, J.“Pyrazolopyridines and related compounds as gamma-secretase modulators and their preparation and use in the treatment of Alzheimer's disease.”PCT Int.Appl.WO 2009073777,2009.

10．Aslanian, R.G.; Huang, X.; Palani, A.; Qin, J.; Zhou, W.; Zhu, X.; Mazzola, R. D., Jr.; Dhondi, P.; Greenlee, W.J. “Preparation of heteroarylphenylaminopyridazinonederivatives and analogs as gamma-secretase modulators.”PCT Int.Appl. WO 2009032277,2009.

11．Palani, A.; Qin, J.; Zhu, X.; Aslanian, R. G.; McBriar, M. D. “Preparation of imidazolylphenylethenesulfonamide derivatives for use as gamma-secretase modulators.”PCT Int.Appl.WO 2009020579,2009.

12．Zhu, Z.; Greenlee, W. J.; Mazzola, R. D.; Qin, J.; Huang, X.; Palani, A.“Preparation of imidazolylphenylmethylideneiminoheterocycles as gamma-secretase modulators.”PCT Int. Appl. WO2009005729,2009.

13．Zhu, Z.; Greenlee, W. J.; Sun, Z.; Gallo, G. V.; Asberom, T.; Huang, X.; Zhu, X.; McBriar, M. D.; Pissarnitski, D. A.; Zhao, Z.; Xu, R.; Li, H.; Palani, A.; Mazzola, R. D., Jr.; Clader, J.; Josien, H.; Qin, J.“Preparation of substituted alkenyloxadiazole derivatives and analogs as gamma-secretase modulators.”PCT Int. Appl. WO 2008137139,2008.

14．Palani, A.; Su, J.; Xiao, D.; Huang, X.; Rao, A.; Chen, X.; Tan, H.;Qin, J.; Huang, Y.; Aslanian, R. G.; Mckittrick, B. A.;Degrado, S. J. “Pyrano[2,3-d]pyrimidines as nicotinic acid receptor agonists for the treatment of dyslipidemia and their preparation and pharmaceutical compositions.”U.S.Pat.Appl.US 20080019978,2008.

15．Palani, A.;Qin, J.; Xiao, D.; Huang, Y.; Chen, X.; Liu, Z.; Degrado, S.; Aslanian, R. G.; Huang, X. “Preparation of heterocyclesasnicotinicacidreceptoragonistsfor the treatment of dyslipidemia.”U.S. Pat.Appl.US 20070173495,2007.

16．Palani, A.; Su, J.; Xiao, D.; Huang, X.; Rao, A.; Chen, X.; Tan, H.;Qin, J.; Huang, Y.; Aslanian, R. G.; Mckittrick, B. A.; Degrado, S. J.“Pyrano[2,3-d]pyrimidines as nicotinic acid receptor agonists for the treatment of dyslipidemia and their preparation and pharmaceutical compositions.”U.S. Pat.Appl. US 20070066630,2007.

17．Palani, A.; Su, J.; Xiao, D.; Huang, X.; Rao, A. U.; Chen, X.; Tang, H.; Qin, J.; Huang,

Y.; Aslanian, R. G.; Mckittrick, B. “Pyrano[2,3-d]pyrimidines as nicotinic acid receptor agonists for the treatment of dyslipidemia and their preparation and pharmaceutical compositions.”PCTInt.Appl.WO 2006124490,2006.

出席学术会议

1．Qin, J.; Palani, A.;Rao, A.; Huang, X.; Xiao, D.; Huang, Y.;Degrado, S.;Aslanian, R.; Chen, X.; Zhu, X.;Sofolarides, M.; Liu, Z.;Greenfeder, S.;VanHeek, M.;Chintala, M.; Farley, C.;Kurowski, S.; Li, Q.;Cheewatrakoolpong, B.; Zhang, H. “Discovery of 5-(3-cyclopropylpropyl)-2-(difluoromethyl)-3H-pyrano[2,3-d]pyrimidine-4,7-dione, a potent nicotinic acid receptor agonist for the treatment of dyslipidemia.” Rahway-Kenilworth Symposium Seminar& Mixer, Merck Research Laboratories, Rahway, New Jersey, USA ,2011(invited poster presentation).

2．Qin, J.;Palani, A.;Rao, A.; Huang, X.; Xiao, D.; Huang, Y.;Degrado, S.;Aslanian, R.; Chen, X.; Zhu, X.;Sofolarides, M.; Liu, Z.;Greenfeder, S.;VanHeek, M.;Chintala, M.; Farley, C.;Kurowski, S.; Li, Q.;Cheewatrakoolpong, B.; Zhang, H. “Discovery of 5-(3-cyclopropylpropyl)-2-(difluoromethyl)-3H-pyrano[2,3-d]pyrimidine-4,7-dione,a potent nicotinic acid receptor agonist for the treatment of dyslipidemia.”239th ACS National Meeting,San Francisco, CA, March 21-25,2010(poster presentation).

3．Robinson, J.E.; Evans, P.A.; Qin, J.; Bazin, B. “A novel and concise approach to the synthesis of polycyclic guanidines: total synthesis of (-)-batzelladine D.” 40thNational Organic Symposium, Durhan, NC, USA, June 3-7,2007(poster presentation).

4．Korapala, C. S.; Qin, J.; Soukri, M.;Friestad, G. K. “Manganese-mediated radical-ionic annulations unlock a C2-symmetry-breaking strategy toward quinine.”233rd ACS National Meeting, Chicago, IL, March 25-29,2007(poster presentation).

5．Friestad, G. K.; Qin, J.; Marie, J.-C.; Ruggles, E. L.; Shen, Y. “Radical addition to hydrazones: versatile carbon-carbon bond constructions for asymmetric amine synthesis.” Ninth International Kyoto Conference on New Aspects of Organic Chemistry (IKCOC-9), Kyoto, Japan, November 10-14,2003(invitedshorttalk).

6．Friestad, G. K.; Qin, J.“Asymmetric radical addition toN-acylhydrazones.”37th National Organic Chemistry Symposium, Bozeman, MT, June 10-14,2001, Abstract 80 (poster presentation).

7．Friestad, G.K.; Qin,J.“Asymmetric radical addition to chiralN-acylhydrazones: new developments in organic radical chemistry.” The 2000 International Chemical Congress of Pacific Basin Societies (Pacifichem 2000), Honolulu, HI, December 14-19,2000, Abstract ORGN 156 (invited lecture).

8．Friestad, G.K.; Qin, J. “StereoselectiveMn-mediated radical addition to chiral hydrazones.”222ndAmerican Chemical Society National Meeting, Chicago, IL, August 26-30,2001, Abstract ORGN 227 (lecture).

9．Qin, J.;Friestad,G.K. “Manganese carbonyl-promoted photolytic radical addition toN-acylhydrazone.” Northeast Regional Meeting of the American Chemical Society, Durham, New Hampshire, June 24-27,2001,Abstract 128 (lecture).

10．Qin, J.; Friestad, G.K. “Enantioselective radical addition to novelN-acylhydrazone.” Northeast Regional Meeting of the American Chemical Society, Storrs, Connecticut, June 18-21,2000, Abstract 67 (poster).

11．Friestad, G.K.;Qin, J. “Radical addition reactions in asymmetric amine synthesis.” Gordon Research Conference on Free Radical Reactions, Holderness School, Plymouth, New Hampshire, July 11-16,1999(poster).