【近年来获得的学术科研成果】
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)。10个新药候选物进入欧美等国的临床,3个新药上市(Tobi及Vismodegib),拥有15项美国及世界授权新药研发专利。主要授权和公开专利16项。
【近年来科研项目】
天然物化学(天然物分离、结构鉴定、全合成、生物合成)。
心血管疾病药物、抗感染药物、抗炎症药物,免疫性疾病以及抗肿瘤靶向性药物的研发。
【近年来主要论文代表作】
1. 1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors,Molecules (2014), 19, 102-121,
2. Imidazo[4,5-b]pyridine inhibitors of B-Raf kinaseBioorganic & Medicinal Chemistry Letters (2013), 23, 5896-5899
3. Synthesis and SAR studies of praziquantel derivatives with activity against Schistosoma japonicum
Molecules (2013), 18, 9163-9178.
4. Synthesis and Antiviral Activity of Conformational Analogues of Leucamide A.
Molecules 2012, 17, 14522-14530.
5. 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, 4101-4113.
6. Au(III)-catalyzed intermolecular amidation of benzylic C-H bonds.
Org. Biomol. Chem., 10, 9137-9141, 2012.
7. Gold-catalyzed direct indolation of tetrahydroisoquinolines.
Chin. J. Chem. 30, 2741-2746, 2012.
8. Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships.
Bioorg Med Chem Lett 2011, 21, 5533-7.
9. Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
ACS Medicinal Chemistry Letters 2011, 2, 342-347.
10. Pyrazolopyridine inhibitors of B-RafV600E. Part 2: Structure-activity relationships
Bioorganic & Medicinal Chemistry Letters (2011), 21(18), 5533-5537
11. 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 A
1 20090911
12. 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 A
1 20090911,
13. 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 A
1 20090911
14. N-Pyrrolo[2,3-b]pyridinyl benzamide derivatives as Raf inhibitors and their preparation, pharmaceuticalcompositions and use in the treatment of diseases
PCT Int. Appl. (2009), WO
2009111278 A
2 20090911
15. Methods and compositions utilizing quinazolinones as KSP kinesin inhibitors and their preparation
U.S.
Pat. Appl. Publ. (2008), US
20080182864 A
1 20080731,
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