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博士生导师

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冯柏年

编辑: 吴新    发布日期: 2016-12-15   来源:  

姓名

冯柏年

性别

出生年月

1962.06

党派

职称

太湖学者

特聘教授

博士生导师

民族

最高学位

博士

毕业

日本名古屋大学

联系

方式

0510-85197052

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 19935—19982月研究员,项目经理,Novartis,   USA

l 19982—20001月化学业务总监,RepliGen   Co., Needam, USA

l 20001—20026月高级研究员,项目经理;Cytokinetics, Inc., USA

l 20026—20086月高级研究员,项目经理;Roche/Genentech, Inc., USA

l 20086现在董事长兼总经理;AlphaBiopharmaceuticals,Inc., USA

l 20111现在江南大学太湖学者,特聘教授。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(TobiVismodegibKadcylaTOBI 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 108503583 A 20180907,

 

5. Preparation of   pyrazolo[1,5-a]pyrimidine compounds as antitumor agents

Faming Zhuanli Shenqing (2018),   CN 108484613 A 20180904,

 

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 108484606 A 20180904,

 

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 107383019 A 20171124,

 

9. A polypeptide derivatization   method and its application in maldi-tof-ms detection of medicine metabolites   [Machine Translation].

Faming Zhuanli Shenqing (2017),   CN 107085032 A 20170822,

 

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 106632142 A 20170510,

 

12. Method for preparing statin   bulk drug intermediate with improved Julia olefination reaction as key step

Faming Zhuanli Shenqing (2017),   CN 106588763 A 20170426,

 

13. Synthesis method for chiral   secondary allyl alcohol with hydroxy ortho position substituted with halogen   atom

Faming Zhuanli Shenqing (2017),   CN 106588565 A 20170426,

 

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 105815781 A 20160803,

 

19. A sugar protein fluorescent   probe molecules for continuous synthesis method

Faming Zhuanli Shenqing (2016),   CN 105806820 A 20160727,

 

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 105481765 A 20160413,

 

23. A Decoquinate analogue and   application

Faming Zhuanli Shenqing (2016),   CN 105330602 A 20160217,

 

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 105017039 A 20151104,

 

28. Spiro-isoxazoline derivatives   as PTP1B inhibitor and their preparation

Faming Zhuanli Shenqing (2015),   CN 104945416 A 20150930,

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 104788410 A 20150722,

 

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 104447678 A 20150325,

 

39. 2,3-Dihydroperimidine analogs   and synthetic method, pharmaceutical composition and use thereof

Faming Zhuanli Shenqing (2015),   CN 104418811 A 20150318,

 

40. Method for synthesis of   sodium glycididazole

Faming Zhuanli Shenqing (2015),   CN 104356070 A 20150218,

 

 

 

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 104292221 A 20150121,

 

43. Method for preparing   erysovine monomer from Vaccaria segetalis seeds

Faming Zhuanli Shenqing (2014),   CN 104030965 A 20140910,

 

44. Preparation of   1,2,5-oxadiazole-2-oxide analogs and useful in the treatment of   schistosomiasis

Faming Zhuanli Shenqing (2014),   CN 104003954 A 20140827,

 

45. Preparation of praziquantel   analogs as anti-schistosomiasis drugs

Faming Zhuanli Shenqing (2014),   CN 103910725 A 20140709,

 

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 2009111278   A2 20090911,

 

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   2009111279 A1 20090911,

 

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   2009111280 A1 20090911,

 

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   2009111277 A1 20090911,

 

61. Methods and compositions   utilizing quinazolinones as KSP kinesin inhibitors and their preparation

U.S. Pat. Appl. Publ. (2008), US   20080182864 A1 20080731,

 

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   20060014700 A1 20060119,

 

64. Heterocyclic   self-immobilative linkers and conjugates

PCT Int. Appl. (2005), WO   2005082023 A2 20050909,

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   2003097053 A1 20031127,

 

66. Preparation of chromones as   KSP kinesin inhibitors

PCT Int. Appl. (2003), WO   2003088903 A2 20031030,

 

67. Compositions and methods   using cardiac sarcomere-modulating benzenesulfonamide derivatives for   treating heart failure, and preparation thereof

PCT Int. Appl. (2003), WO   2003059265 A2 20030724,

 

68. Compositions and methods   using arylamide compounds for treating heart failure

PCT Int. Appl. (2003), WO   2003059258 A2 20030724,

 

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   2001098278 A1 20011227,

 

71. Methods and compositions   utilizing quinazolinones as KSP kinesin modulators

PCT Int. Appl. (2001), WO   2001030768 A1 20010503,

 

72. Preparation of   isoquinolonecarboxylates and related compounds as immunosuppressive agents.

PCT Int. Appl. (1999), WO 9938846   A1 19990805,

 

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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