李革 研究员

文章出处: 作者: 发布时间: 2015-02-17 访问次数: 848

     

李革,Ph.D.

药明康德董事长兼首席执行官

 

 

 

教育及工作经历

 

1989年毕业于北京大学化学系,

1993年毕业于美国哥伦比亚大学,获有机化学博士。博士毕业后,与导师等人一起创立了美国新泽西州普林斯顿组合化学公司Pharmacopeia Inc.,并协助公司于1995年在纳斯达克成功上司。

2000年,回国成立药明康德新药开发有限公司,将医药研发外包这种模式引进中国。

2007年,药明康德成功在美国纽交所上市。

 

研究内容

 

组合化学和药物化学领域。李革博士曾成功地利用“组合化学技术”发现了多种药物前体化合物,其中有三个化合物进入美国不同阶段的临床试验,拥有40多项发明专著,并在业界期刊上发表了多篇学术论文。

 

发表论文及获得的国内外专利

 

1.“Podand Sulfones. EnantioselectiveReceptors for PeptidicAmmonium Ions” J. Org. Chem., 1991, 56, 6964, G. Li and W. C. Still.

2.“Dipeptidic Ammonium Ion Binding By A Synthetic Receptor” Biorganicand Medicinal Chem. Lett., 1992, 2, 731, G. Li and W. C. Still.

3.“Two-Point Binding in PodandAcetalsFavors EnantioselectiveComplexation” Tetrahedron Lett., 1992, 33, 5929, G. Li and W. C. Still.

4.“A PodandAnalog of 18-Crown-6” Tetrahedron Lett., 1993, 34, 919, G. Li and W. C. Still.

5.“An 18-Crown-6 Derivative with Only One Conformation” J. Am. Chem. Soc., 1993, 115, 3804, G. Li and W. C. Still.

6.“Peptidosteroidal Receptors for Opioid Peptides. Sequence-Selective Binding Using a Synthetic Receptor Library” J. Am. Chem. Soc., 1994, 116, 7955, R. Boyce; G. Li; P. Nestler; T. Suenagaand W. C. Still.

7.“Experimental and Theoretical Studies of Enantioselectivereceptors for Peptides” in Molecular Recognition: Chemical and Biochemical Problems, Special Publication, Royal Society of Chemistry, S. M. Roberts, Editor, pp 171-182, Cambridge, 1992, W. C. Still; S. Erickson; X. Wang; G. Li; A. Armstrong; J. Hong; S. K. Namgoongand R. Liu.

8.“A Paradigm for Drug Discovery Employing Encoded Combinatorial Libraries” Proc. Nat'l Acad. Sci. U.S.A., 1995, 92, 6027, J. Burbaum; M. Ohlmeyer; J. Reader; I. Henderson; L. W. Dillard; G. Li; T. Randle; N. Sigal; D. Chelskyand J. Baldwin.

9.“Combinatorial Libraries Encoded with ElectrophoricTags” Euro. J. Med. Chem., 1995, 30, 349, J. Baldwin; J. Burbaum; D. Chelsky; L. Dillard; I. Henderson; G. Li; M. Ohlmeyer; T. Randle; J. Reader.

10.“Binary encoded small-molecule libraries in drug discovery and optimization” Perspect. Drug Discovery Des., 1995, 2, 305, J. Chabala; J. Baldwin; J. Burbaum; D. Chelsky; L. Dillard; I. Henderson; G. Li; M. Ohlmeyer; T. Randle.

11.“Practical synthesis of an orally active renin inhibitor aliskiren” Tetrahedron Letters, 46, 2005, 6337–6340, Hua Dong, Zhi-Liu Zhang, Jia-Hui Huang, RujianMa, Shu-Hui Chen and Ge Li.

12.“A practical synthesis of (-)-kazusamycinA” Tetrahedron Letters, 46, 2005, 6341–6344, ShengfengZhou, HuaxiangChen, WenshengLiao, Shu-Hui Chen, Ge Li, Ryoichi Ando and Isao Kuwajima

13.“A novel and efficient method for the synthesis of 1,2-diazetidines” Tetrahedron Letters, 47, 2006, 6835–6837, Wei Miao, WeiliangXu, ZhiliuZhang, RujianMa, Shu-Hui Chen and Ge Li.

14.“Discovery and preliminary structure–activity relationship studiesofnovel benzotriazinebased compounds as Srcinhibitors” Bioorganic & Medicinal Chemistry Letters, 16, 2006, 5546–5550, Glenn Noronha, Kathy Barrett, JianguoCao, Elena Dneprovskaia, Richard Fine, XianchangGong, Colleen Gritzen, John Hood, XinshanKang, Boris Klebansky, G. Li, W. Liao, Dan Lohse, Chi ChingMak, Andrew McPherson.

15.“Efficient method for the synthesis of optically pure terminal olefin bearing long chain alpha-amino acids” Letters in Organic Chemistry, 3, 2006, 489-491, Miao Wei, JiaLanqi, Zhang Zhiliu, Dong Jingchao, Shi Yifeng, Ma Rujian, Tang Suhan, Chen Shu-Hui, Li Ge.

16.“A concise total synthesis of 7-substituted eudistominanalogs” Letters in Organic Chemistry, 3, 2006, 455-458, Peng Zuozhong, Song Ji, Liao Wensheng, Ma Rujian, Chen Shu-Hui, Li Ge, Ando Ryoichi.

17.“Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide(SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist” J. Med. Chem., 49, 2006, 7603-7606, Dwyer MP, Yu Y, Chao J, Aki C, Chao J, BijuP, GirijavallabhanV, RindgenD, Bond R, Mayer-EzelR, JakwayJ, HipkinRW, FossettaJ, GonsiorekW, BianH, Fan X, TerminelliC, Fine J, LundellD, Merritt JR, RokoszLL, Kaiser B, Li G, Wang W, Stauffer T, OzgurL, Baldwin J, TaverasAG.

18.“Synthesis and structure-activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists” BioorgMed ChemLett.16, 2006, 4107-4110, Merritt JR, RokoszLL, Nelson KH Jr, Kaiser B, Wang W, Stauffer TM, OzgurLE, Schilling A, Li G, Baldwin JJ, TaverasAG, Dwyer MP, Chao J.

19.“Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-amine—a potent, orally active Srckinase inhibitor with anti-tumor activity in preclinical assays” Bioorganic & Medicinal Chemistry Letters 17, 2007, 602–608, Glenn Noronha, Kathy Barrett, Antonio Boccia, Tessa Brodhag, JianguoCao, Hong Gu, Ge Li, Feng Shi, SuhanTang.

20.“Synthetic receptors, libraries and uses thereof ” U. S. Patent 5,804,563

21.“Combinatorial dihydrobenzopyranlibrary” U. S. Patent 5,688,997

22.“Preparation of heterocyclic tricyclic compounds useful for inhibition of G-Protein function and for treatment of cell proliferative diseases” U.S. Patent 5,801,175

23.“Combinatorial dihydrobenzopyranlibrary” U.S. Patent 5,821,130

24.“Carbonyl piperazinyland piperidinylcompounds” U.S. Patent 5,880,128

25.“Combinatorial dihydrobenzopyranlibrary” U.S. Patent 6,017,768

26.“An universiallinker for combinatorial synthesis” U.S. Patent 6,008,321

27.“A combinatorial piperazinelibrary” Filed on Dec., 1996.

28.“Preparation of antineoplastic carbonylpiperazinyland -piperidinylderivatives which inhibit farnesylprotein transferase” WO 9631501

30.“Preparation of benzopyransas drugs and combinatorial libraries containing them” WO 9716729

 

31.“Compounds useful for inhibition of farnesylprotein transferase” Filed in May 1997

32.“Acid cleavable linker for combinatorial synthesis” Filed in Feb., 1998

33.“Novel inhibitors of Farnesyl-Protein Transferase” Filed in Dec., 1998

34.“Preparation of 2-ketoimidazole compounds useful for inhibition of HCV protease” in preparation

35.“Combinatorial synthesis of 2-ketoimidazole library” in preparation

36.“A novel method for the preparation of tetrahydro-imidazo-pyridinylcompounds on solid phase and potential treatment of central nervous system disorders related to angiotensin-II type 2 receptors” in preparation

37.“Novel FarnesylProtein TransferaseInhibitors as Antitumor Agents” Filed in Aug. 2000

38.“Substituted Cyclobutenedione, Chemokine Receptor Antagonists” Filed in Aug. 2000

39.“Substituted Cyclobutenedione, potential anti-inflammatory agents” Filed in Aug. 2000

40.螺环类模板化合物的制备,专利号:ZL03116312.2

41.2--5-氟烟酸酯及酸的制备方法,申请号:200310108336.1

42.一种提纯制备三磷酸核苷衍生物的方法,申请号:200310108337.6

43.一种光学纯反式2,3-二胺-1,2,3,4-四氢化萘的制备方法,申请号:200310109060.9

44.一种光学纯N-叔丁基氧羰基-β-二氟苯丙氨酸的制备方法,专利号:ZL200310109061.3

45.2--5-氟烟酸的工业化制备方法,申请号:200310109199.3

46.[苯并环-4'-哌啶-2'-]模板化合物的制备,申请号:200310122852.X

47.螺二氢吲哚类模板化合物及其制备方法,申请号:200410015612.4

48.一种含有钙阻滞剂的稳定药物组合物,申请号:200410067241.4

49.A Novel Process for the Preparation of NonracemicLong Chainα-Amino Acids Derivatives (PCT),申请号:PCT/CN2004/001167

50.一种制备高光学纯度匹伐他汀钙原料药的方法,申请号:200510026641.5

51.一种用于治疗慢性肝炎的丙帕者口腔崩解片及其制造方法,申请号:200510028715.9

52.一种稳定的含有匹伐他汀钙的药物组合物及其制备方法,申请号:200510110676.7

53.W. Miao, R. Ma, S-H. Chen, G. Li; “A Process for the Preparation of Optically Active Long Ethyleneicend Chain-N-80C-Amino Acid” Application No. 200510111851.4 (Dec. 22, 2005)

54.S-F. Zhou, R. Ma, S. Tang, S-H. Chen, G. Li; “An One-Pot Synthesis of N-(tert-Butoxycarbonyl)-5-aza-3-ketone-bicyclo-[2,2,1]-Heptane” Application No. 200510111852.9 (Dec. 22, 2005)

55.S-F. Zhou, Y-L. Wu, R. Ma, S. Tang, S-H. Chen, G. Li; “The ContinueousSynthesis of N-(tert-Butoxycarbonyl)-5-aza-3-ketone-bicyclo-[2,2,1]-Heptane” Application No. 200510111853.3 (Dec. 22, 2005)

56.H-X. Chen, Z-H. Wu, Z-H. Zhang, R. Ma, S-H. Chen, G. Li; “A Process for the Preparation of 4,7-Diazafluoren Indole” Application No. 200510111854.8 (Dec. 22, 2005)

57.Y-X. Yin, Z-G. Hu, Y-F. Shi, R. Ma, S. Tang, S-H. Chen, G. Li; “The preparation of Optically Active 4,4’-Difluoro-2-Aminobutyric Acid and its Ester” Application No. 200510112040.6 (Dec. 27, 2005)

58.H. Dong, H. Wu, J-C. Dong, R. Ma, S-H. Chen, G. Li; “The Process for the Preparation of 3-Amino-2,2-dimethylpropionamide” Application No. 200510112039.3 (Dec. 27, 2005)

59.一种2-腈基呋喃的制备方法,申请号:200610023302.6

60.H. Dong, Z-L. Zhang, R. Ma, S-H. Chen, G. Li; “Practical Synthesis of Orally Active Renin Inhibitor Aliskiren” Application No.200610023804.9(Feb. 9, 2006)

61.定量滴瓶,专利号:ZL200620039908.4(实用新型)

62.核磁共振数据管理系统及其管理方法,申请号:200610026721.5

63.Z-H. Zhang, M-Q. Hu, E-Y. Tang, R. Ma, S.H. Chen, G. Li “A Method of preparing the template compounds and thereof derivatives of spiro[Benzo-2-one-3-(4’-pepridine)]” Application No. 200610027067.X (May 30, 2006)

64.Z-H. Zhang, M-Q. Hu, G-Y. Xie, E-Y. Tang, Q-S. Liu, H-X. Chen, Y-F. Luo, J-C. Dong, R. Ma, S. H. Chen, G. Li “A Method of preparing the template compounds of spiro[Benzo-1-one-3-(4’-piperidine)]” Application No. 200610027068.4 (May 30, 2006)

65.E-Y. Tang, L-Q. Qu, Y. Xu, R. Ma, S. H. Chen, G. Li “Preparation of a-AzaSpiro-bicycloTemplates” Application No. 200610027069.9 (May 30, 2006)

66.Z-L. Zhang, C. Yong, R. Ma, S. H. Chen, G. Li ?One Synthetic Method of Optically Pure w-phenyl-(2S)-N-Boc-a-amino acid derivatives“ Application No. 200610027871.8 (Jun. 20, 2006)

67.一种5-甲酰基-3-噻吩甲酸酯工业化制备方法,申请号:200610027872.2

68.W. Miao, W-L. Xu, Z-L. Zhang, R. Ma, S. H. Chen, G. Li. “ An Efficient Method for the Synthesis of Optically Pure 2-Amino-heptanedioic acid 7-ethyl ester and 2-amino-heptanedioic acid diethyl ester” Application No. 200610027873.7 (Jun. 20, 2006)

69.W-L. Xu, W. Miao, Z-L. Zhang, R. Ma, S. H. Chen, G. Li. “A Method of Synthesizing 1,2-Diazetidine” Application No. 200610027874.1 (Jun. 20, 2006)

70.Z-L. Zhang, H. Dong, R. Ma, S. H. Chen, G. LiOne Synthetic Method for Optically Pure w-phenyl-(S)-N-Boc-a-Amino Acid Derivatives Application No. 200610027875.6 (Jun. 20, 2006

71.H. Dong, W. Miao, Z-L. Zhang, J-C. Dong, Y-F. Shi, R. Ma, S. H. Chen, G. Li “A Method for the Synthesis of Optically Pure 2-Amino-dec-8-Nonenoica” Application No. 200610027876.0 (Jun. 20, 2006)

73.一种一锅法制备4-甲氧基苯腈的方法,申请号:200610027878.X

74.H-X. Chen, R. Ma, S. H. Chen, G. Li. “Preparation of Spiro[1,3-2H-indene-4’-piperidin-1-Carboxylic Acids] Templates” Application No. 200610027879.4 (Jun. 20, 2006)

75.F. Tang, W-L. Xu, Z-L. Zhang, N. Jiang, C. Li, R. Ma, S. H. Chen, G. Li. “A Method for Converting the cis-4-alkyl-N-Boc-pyroglutamic acid ester to its trans-form product” Application No. 200610117598.8 (Oct. 26, 2006)

76.W. Miao, Z-L. Zhang, W. Xu, R. Ma, S. H. Chen, G. Li. “A PraticalSynthesis of Optically Pure a-Amino-subericacid mono-and di-ester” Application No. 200610117599.2 (Oct. 26, 2006)

77.4-三氟甲基苯肼盐酸盐的工业化合成方法,申请号:200610148793.7

78.Z. Bai, G. Xu, H. He, S. H. Chen, G. Li. “A Practical Synthesis of Cyclobutylbromide”. Application No. 200610148794.1 (Oct. 26, 2006)

79.R. Liu, Z. Qian, Y. Shi, S. H. Chen, S. Tang. “The Synthesis of 4-Pyrimidin carboxylic acid esters”. Application No. 200610148795.6 (Dec. 30, 2006)

80.X. Xu, R. ma, S. H. Chen, G. Li. “The Synthesis of 2-Substituted mercapto-4-pyrimidin carboxylic acid derivatives”. Application No. 200710037726.2 (Feb. 28, 2007)

81.H-X. Chen, R. ma, S. H. Chen, G. Li. “Preparation method of the 3,9-diazaspiro[5.5]undecaneanalogue template”. Application No. 200710037727.7 (Feb. 28, 2007)

82.H-X. Chen, R. ma, S. H. Chen, G. Li. “Preparation method of the 3,9-diazaspiro[5.5]undecan-2-one analogue template”. Application No. 200710037728.1 (Feb. 28, 2007)

83.H-X. Chen, R. ma, S. H. Chen, G. Li. “Preparation method of the 3,9-diazaspiro[5.5]undecane-2,4-dione analogue template”. Application No. 200710037729.6 (Feb. 28, 2007)

84.C-F. Zhong, R. ma, S. H. Chen, G. Li. “A new synthesis of 5-trifluorometyl-indan-1-one”. Application No. 200710040068.2 (Apr. 27, 2007)

85.特戊胺草酸盐工业化制备方法,申请号:200710093950.3

 

86.一种磺酰胺类化合物的合成方法,申请号:200710093949.0

87.J. Xiong, R. ma, S. H. Chen, G. Li. “A synthetic method for 3-aryl-5-vinyl-oxazolidin-2-one”. Application No. 200710094099.6 (Sep. 27, 2007)

88.J-Y. Li, H-Y.He, S. H. Chen, G. Li. “A practical way to make 3,5-disubstituted pyrazoles”. Application No. 200710094137.8 (Oct. 12, 2007)

89.H-Y.Hu, R. ma, S. H. Chen, G. Li. “A synthetic method for 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine”. Application No. 200710094138.2 (Oct. 12, 2007)

90.W-X. Yang, R. ma, S. H. Chen, G. Li. “A new resolute 1-(naphthalen-1-yl)ethanaminemethod”. Application No. 200710094139.7 (Oct. 12, 2007)

91.W-F. Zhou, R. ma, S. H. Chen, G. Li. “A synthetic method for Aryl substituted anthranilicacids and its Derivatives”. Application No. 200710094152.2 (Oct. 19, 2007)

92.L-X. Zhang, R. ma, S. H. Chen, G. Li. “A method for synthesis of N-alkyl maleimide”. Application No. 200710094202.7 (Nov. 6, 2007)

93.J. Xiong, R. ma, S. H. Chen, G. Li. “ A synthetic method for 3-aryl-4-vinyl-oxazolidin-2-one”. Application No. 200710094203.1 (Nov. 6, 2007)

94.J-F. Jiang, R. ma, S. H. Chen, G. Li. “A new route to synthesize 1-alkyl-1,2,3,4-tetrahydro-quinolin-4-ylamine”. Application No. 200710094204.6 (Nov. 6, 2007)

95.J-F. Jiang, R. ma, S. H. Chen, G. Li. “A new route to synthesize 1-alkyl-2,3-dihydro-1H-quinolin-4-one”. Application No. 200710094205 .0(Nov. 6, 2007)

96.Y. Xu, R. ma, S. H. Chen, G. Li. “A new preparation method of methyl 4-(hydroxymethyl)cyclohexanecarboxylate”. Application No. 200710094231.3 (Nov. 15, 2007)

97.H. Wu, R. ma, S. H. Chen, G. Li. “2-azabicyclo[2.2.2]octane-3-carboxylic acid derivatives and their preparation”. Application No. 200710094603.2 (Dec.21, 2007)

98.F-Y. Jiang, R. ma, S. H. Chen, G. Li. “Fluoroor difluoro-2-azabicyclo[2.2.1]heptane-3-carboxylic acid derivatives and their preparation”. Application No. 200710094604.7 (Dec.21, 2007)

99.S-T. Jiang, R. ma, S. H. Chen, G. Li. “A type of 5-amino-2-azabicyclo[2.2.1]heptane-3-carboxylic acid derivatives and their preparation”. Application No. 200710094605.1 (Dec.21, 2007)

100.M-L. Cao, R. ma, S. H. Chen, G. Li. “Fluoroor difluoro-2-azabicyclo[2.2.2]octane-3-carboxylic acid derivatives and their preparation”. Application No. 200710094606.6 (Dec.21, 2007)

101.H-Y. Liang, J-C Dong, S. H. Chen, G. Li. “A type of octahydrocyclopenta[c]pyrrole-1-carboxylic acid derivatives and their preparation”. Application No. 200710094607 .0(Dec.21, 2007)

102.Q-S. Liu, J-C Dong, S. H. Chen, G. Li. “A type of dihydroxy-2-azabicyclo[2.2.1]heptane-3-carboxylic acid derivatives and their preparation”. Application No. 200710094608.5 (Dec.21, 2007)

103.K. Zhang, R. ma, S. H. Chen, G. Li. “A hydrolizationmethod of aromatic n-amide”. Application No. 200710094626.3 (Dec.25, 2007)

104.K. Zhang, R. ma, S. H. Chen, G. Li. “A synthetic method for preparation of substituent amino acid from Ugireaction”. Application No. 200710094625.9 (Dec.25, 2007)

105.K. Zhang, R. ma, S. H. Chen, G. Li. “A method of remove tert-alkyl amino group”. Application pending.

106.Z-H. Zhang, R. ma, S. H. Chen, G. Li. “The synthesis of a spiro(1-trotrehydro-naphthalen-Irol;4.4-piperidine)derivatives”. Application pending.

107.J-Y. Li, H-Y. He, S. H. Chen, G. Li. “A practical way to synthesize aromatic bislactamspiro-templates.” Application pending.

 

 

获得荣誉

 

2012年上海市青年科技杰出贡献奖、浦东年度经济人物、波士顿生物科技CEO大会终身成就奖

2011年获“中国健康行业创新领袖”称号、中国服务外包杰出贡献人物,百华协会终身成就奖

2010年荣获“圣地亚哥生物-制药成就奖”

2009年荣膺“中国医药60年·60人”称号

2008年荣列福布斯25位最著名美籍华裔企业家榜,并与药明康德公司分别荣列“中国企业最具创新力十大领军人物”及“中国创新型企业20强”

2007年荣获“影响中国的十大企业家”称号,以及“安永企业家奖中国2007

2006年度中国十大科技英才”

2005年,李革成为《Red Herring》杂志八月刊封面人物,同年929日于人民大会堂受领由国务院侨务办公室颁发的“华人华侨杰出创业奖”