姓名
冯柏年
性别
男
出生年月
1962.06
党派
无


职称
太湖****
****
博士生导师
民族
汉
最高学位
博士
毕业
日本名古屋大学

联系
方式

briandfeng@163.com
研究方向
天然物化学，心血管疾病药物、抗感染药物、抗炎症药物，智能抗糖尿病药物，免疫性疾病以及抗肿瘤靶向药物

主要学习工作简历和主要学术兼职
【学习和工作经历】
l 硕博，日本名古屋大学（1985-1990年）
l 博士后，哈佛大学（哈佛大学校长特邀博士后研究员，1990-1993年）
l 1993年5月—1998年2月研究员，项目经理，Novartis， USA
l 1998年2月—2000年1月化学业务总监，RepliGen Co., Needam, USA
l 2000年1月—2002年6月高级研究员，项目经理；Cytokinetics, Inc., USA
l 2002年6月—2008年6月高级研究员，项目经理；Roche/Genentech, Inc., USA
l 2008年6月—现在董事长兼总经理；AlphaBiopharmaceuticals,Inc., USA
l 2011年1月—现在江南大学太湖****，****。工作期间，
l 在美国工作期间，有10个新药候选物进入欧美等国的临床研究； 取得临床批件40余张； 有4个新药上市（Tobi，Vismodegib，Kadcyla，TOBI Podhaler），
l 25年丰富且成功的新药物研发经验，拥有15项美国新药研发发明专利。
l 先后获批江苏省“双创”高端引进人才（2011年）；无锡市领军人物（2012年）

科学研究情况简介
【论文及专利】
1. Determination of an isonicotinylhydrazide derivative, a novel positive inotropic compound, in mouse plasma by LC-MS/MS and its application to a pharmacokinetics study
Journal of Pharmaceutical and Biomedical Analysis (2019), 165, 12-17.
2. Design, synthesis, and biological evaluation of 2-(4-(methylsulfonyl)phenyl)pyridine derivatives as GPR119 agonists
Chemical Biology & Drug Design (2019), 93(1), 67-74.
3. Synthesis and biological evaluation of novel 5,6-dihydropyrimido[4,5-f]quinazoline derivatives as potent CDK2 inhibitors
Bioorganic & Medicinal Chemistry Letters (2018), 28(20), 3385-3390.

4. Alkylation method of nitrogen-containing hydrogen compound and its application
Faming Zhuanli Shenqing (2018), CN A **,
5. Preparation of pyrazolo[1,5-a]pyrimidine compounds as antitumor agents
Faming Zhuanli Shenqing (2018), CN A **,
6. Pyrimido[4,5-f]quinazoline compounds as CDK inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer
Faming Zhuanli Shenqing (2018), CN A **,
7. Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors
European Journal of Medicinal Chemistry (2018), 157, 935-945.
8. Pyrazolo[4,3-h]quinazoline compound and application thereof
Faming Zhuanli Shenqing (2017), CN A **,
9. A polypeptide derivatization method and its application in maldi-tof-ms detection of medicine metabolites [Machine Translation].
Faming Zhuanli Shenqing (2017), CN A **,
10. Transition-Metal-Free Trifluoromethylation of Aldehyde Derivatives with Sodium Trifluoromethanesulfinate
Journal of Organic Chemistry (2017), 82(18), 9384-9399.
11. 1,2,5-Thiadiazole-2-oxide analogues as schistosomicides and their preparation, pharmaceutical compositions and use in the treatment of schistosomiasis
Faming Zhuanli Shenqing (2017), CN A **,
12. Method for preparing statin bulk drug intermediate with improved Julia olefination reaction as key step
Faming Zhuanli Shenqing (2017), CN A **,
13. Synthesis method for chiral secondary allyl alcohol with hydroxy ortho position substituted with halogen atom
Faming Zhuanli Shenqing (2017), CN A **,
14. Development and validation of pharmacophore of G protein-coupled receptor 40 agonists
Jisuanji Yu Yingyong Huaxue (2017), 34(2), 157-162.
15. Gold-Oxazoline Complex-Catalyzed Cross-Dehydrogenative Coupling of Glycine Derivatives and Alkenes
Advanced Synthesis & Catalysis (2017), 359(5), 824-831.
16. Synthesis of aromatic amide derivatives and their biological evaluation against protein tyrosine phosphatase 1B and protein tyrosine phosphatase SHP2
Youji Huaxue (2016), 36(9), 2142-2149.
17. Oxadiazole-2-oxides may have other functional targets, in addition to SjTGR, through which they cause mortality in Schistosoma japonicum
Parasites & Vectors (2016), 9, 26/1-26/12.
18. Lead-removing polysulfide ether composition and its application in health food
Faming Zhuanli Shenqing (2016), CN A **,
19. A sugar protein fluorescent probe molecules for continuous synthesis method
Faming Zhuanli Shenqing (2016), CN A **,
20. Gene expression profiling of H9c2 cells subjected to H2O2-induced apoptosis with/without AF-HF001
Biological & Pharmaceutical Bulletin (2016), 39(2), 207-214.
21. Interleukin 10 protects primary melanocyte by activation of Stat-3 and PI3K/Akt/NF-κB signaling pathways
Cytokine+ (2016), 83, 275-281.
22. Acyl hydrazone derivative for treating heart failure
Faming Zhuanli Shenqing (2016), CN A **,
23. A Decoquinate analogue and application
Faming Zhuanli Shenqing (2016), CN A **,
24. Iron-catalyzed direct α-arylation of α-amino carbonyl compounds with indoles
Organic & Biomolecular Chemistry (2016), 14(5), 1550-1554.
25. Establishment and application of enzymatic assay for poly(ADP-ribose) polymerase-1
Shipin Yu Shengwu Jishu Xuebao (2015), 34(3), 324-329.
26. Immobilizing of oxo-molybdenum complex on cross-linked copolymer and its catalytic activity for epoxidation reactions
Catalysis Communications (2016), 74, 1-4.
27. Continuous preparation method of 1-aminoanthraquinone
Faming Zhuanli Shenqing (2015), CN A **,
28. Spiro-isoxazoline derivatives as PTP1B inhibitor and their preparation
Faming Zhuanli Shenqing (2015), CN A **,
29. An efficient one-pot, three-component synthesis of vinyl sulfones via iodide-catalyzed radical alkenylation
Tetrahedron (2015), 71(38), 6740-6743.
30. Benzene ring-aromatic ring in-series compound and preparation method and pharmaceutical application thereof
Faming Zhuanli Shenqing (2015), CN A **,
31. Palladium(II)-Catalyzed C-H Acylation with Arylglycine Derivatives
Synlett (2015), 26(14), 2033-2036.
32. Synthesis of Novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene Derivatives and Their Biological Evaluation Against Protein Tyrosine Phosphatase 1B
Chemical Biology & Drug Design (2015), 86(5), 1161-1167.
33. TBAI-catalyzed synthesis of α-ketoamides via sp3 C-H radical/radical cross-coupling and domino aerobic oxidation
Tetrahedron Letters (2015), 56(31), 4638-4641.
34. Rh(I)-catalyzed decarbonylation synthesis of carbazoles via C-N cleavage
Tetrahedron (2015), 71(23), 4035-4038.
35. Palladium-Catalyzed Heck-Type Coupling via C-N Cleavage
Synlett (2015), 26(9), 1253-1257.
36. Asymmetric catalytic carbon-carbon coupling reactions via cross-dehydrogenative coupling reactions
Youji Huaxue (2014), 34(12), 2406-2411.
37. Iron-catalyzed oxidative phosphorylation of α-sp3-C-H bonds of N-aryl tetrahydroisoquinolines with air as oxidant
Youji Huaxue (2014), 34(11), 2249-2254.
38. Method for preparing key intermediate of canagliflozin
Faming Zhuanli Shenqing (2015), CN A **,
39. 2,3-Dihydroperimidine analogs and synthetic method, pharmaceutical composition and use thereof
Faming Zhuanli Shenqing (2015), CN A **,
40. Method for synthesis of sodium glycididazole
Faming Zhuanli Shenqing (2015), CN A **,

41. Zebrafish as a New Model for Phenotype-based Screening of Positive Inotropic Agents
Chemical Biology & Drug Design (2015), 85(3), 253-258.
42. Preparation of glucoside and amino acid eutectic crystal form for treatment of glucose related disorder
Faming Zhuanli Shenqing (2015), CN A **,
43. Method for preparing erysovine monomer from Vaccaria segetalis seeds
Faming Zhuanli Shenqing (2014), CN A **,
44. Preparation of 1,2,5-oxadiazole-2-oxide analogs and useful in the treatment of schistosomiasis
Faming Zhuanli Shenqing (2014), CN A **,
45. Preparation of praziquantel analogs as anti-schistosomiasis drugs
Faming Zhuanli Shenqing (2014), CN A **,
46. Synthesis and evaluation of the anti-schistosoma activity against S. japonicum of 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives
Youji Huaxue (2013), 33(12), 2588-2595.
47. Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors
Bioorganic & Medicinal Chemistry Letters (2014), 24(8), 1889-1894.
48. 1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors
Molecules (2014), 19(1), 102-121, 20 pp..
49. Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase
Bioorganic & Medicinal Chemistry Letters (2013), 23(21), 5896-5899.
50. Synthesis and SAR studies of praziquantel derivatives with activity against Schistosoma japonicum
Molecules (2013), 18, 9163-9178.
51. Synthesis and antiviral activity of conformational analogues of leucamide A
Molecules (2012), 17, 14522-14530.
52. Gold-catalyzed direct indolation of tetrahydroisoquinolines
Chinese Journal of Chemistry (2012), 30(12), 2741-2746.

53. Au(III)-catalyzed intermolecular amidation of benzylic C-H bonds
Organic & Biomolecular Chemistry (2012), 10(46), 9137-9141.
54. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152)
Journal of Medicinal Chemistry (2012), 55(9), 4101-4113.
55. Pyrazolopyridine inhibitors of B-RafV600E. Part 2: Structure-activity relationships
Bioorganic & Medicinal Chemistry Letters (2011), 21(18), 5533-5537.
56. Pyrazolopyridine Inhibitors of B-RafV600E. Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors
ACS Medicinal Chemistry Letters (2011), 2(5), 342-347.
57. N-Pyrrolo[2,3-b]pyridinyl benzamide derivatives as Raf inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases
PCT Int. Appl. (2009), WO A2 **,
58. N-Pyrazolo[3,4-b]pyridinyl benzamide derivatives as Raf inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases
PCT Int. Appl. (2009), WO A1 **,
59. N-(6-Aminopyridin-3-yl)-3-(sulfonamido)benzamide derivatives as b-Raf inhibitors for the treatment of cancer and their preparation
PCT Int. Appl. (2009), WO A1 **,
60. Imidazo[4,5-b]pyridine derivatives used as Raf inhibitors and their preparation and use in the treatment of diseases
PCT Int. Appl. (2009), WO A1 **,
61. Methods and compositions utilizing quinazolinones as KSP kinesin inhibitors and their preparation
U.S. Pat. Appl. Publ. (2008), US A1 **,
62. Evaluation of Assay Technologies for the Identification of Protein-Peptide Interaction Antagonists
Assay and Drug Development Technologies (2007), 5(4), 501-514.
63. Preparation of peptides as inhibitors of IAP proteins
U.S. Pat. Appl. Publ. (2006), US A1 **,
64. Heterocyclic self-immobilative linkers and conjugates
PCT Int. Appl. (2005), WO A2 **,
65. 2-[1-(Imidazol-1-yl)alkyl]-3H-quinazolin-4-one derivatives, pharmaceutical compositions containing them, and methods of their use as KSP kinesin inhibitors for the treatment of cellular proliferative diseases
PCT Int. Appl. (2003), WO A1 **,
66. Preparation of chromones as KSP kinesin inhibitors
PCT Int. Appl. (2003), WO A2 **,
67. Compositions and methods using cardiac sarcomere-modulating benzenesulfonamide derivatives for treating heart failure, and preparation thereof
PCT Int. Appl. (2003), WO A2 **,
68. Compositions and methods using arylamide compounds for treating heart failure
PCT Int. Appl. (2003), WO A2 **,
69. Mitotic kinesin-targeted antitumor agents: Discovery, lead optimization and anti-tumor activity of a series of novel quinazolinones as inhibitors of kinesin spindle protein (KSP)
Abstracts of Papers, 223rd ACS National Meeting, Orlando, FL, United States, April 7-11, 2002 (2002), MEDI-249.
70. Preparation of N-acylquinazolinonealkylamines as KSP kinesin inhibitors
PCT Int. Appl. (2001), WO A1 **,
71. Methods and compositions utilizing quinazolinones as KSP kinesin modulators
PCT Int. Appl. (2001), WO A1 **,
72. Preparation of isoquinolonecarboxylates and related compounds as immunosuppressive agents.
PCT Int. Appl. (1999), WO ** A1 **,
73. Combinatorial methods for developing complex molecular scaffolds: Application to the design of carbohydrate mimetic libraries as potential chemotherapeutics
Book of Abstracts, 216th ACS National Meeting, Boston, August 23-27 (1998), MEDI-197.
74. Total synthesis of rhizoxin D
Tetrahedron Letters (1997), 38(39), 6825-6828.
75. Biosyntheses of host-selective toxins produced by Alternaria alternata pathogens. I: (8R,9S)-9,10-epoxy-8-hydroxy-9-methyl-deca-(2E,4Z,6E)-trienoic acid as a biological precursor of AK-toxins
Agricultural and Biological Chemistry (1990), 54(3), 845-8.
76. Structures of flazin and YS, highly fluorescent compounds isolated from Japanese soy sauce
Tetrahedron Letters (1986), 27(29), 3399-402.
77. Determination of the average molecular weight of linear alkylbenzenesulfonates by ion-pair reversed-phase high-performance liquid chromatography
Fenxi Huaxue (1985), 13(5), 368-70.
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工程背景

教学 情况简介