夏岩

青島理工大學教授

夏岩,博士,1957年出生,青島理工大學教授,山東省“泰山學者海外特聘專家”。

人物經歷


1982年畢業於南開大學有機化學專業,獲學士學位;1989年於美國匹茲堡大學有機合成專業,獲博士學位。攻讀博士學位期間,在世界上首次完成了天然產物石杉鹼的全合成。1989-1990年在美國健康研究所從事博士后研究工作。1990年到2011年,在美國仙靈保雅製藥公司(與默克公司合併)工作,先後擔任資深研究員、副骨幹研究員、骨幹研究員、2000年開始擔任資深骨幹研究員(Senior Principal Scientist),學術兼職為美中醫藥開發協會秘書長

研究方向


心血管新葯的研發。

主要貢獻


從事新葯開發工作,參與研發降血壓、抗心血管病,糖尿病中樞神經肝炎等新葯十餘種。主要代表性成果有:1) 抗血凝新葯-凝血酶受體拮抗劑,現在三期臨床測試。 2) 帕金森病新葯-A2a受體拮抗劑,現在二期臨床測試, 2009年獲愛迪生(Thomas Alva Edison) 發明獎。目前申請專利29項,發表學術論文28篇。
代表論文
1. Discovery of nor-seco himbacine analogs as thrombin receptor antagonists. Bioorganic & Medicinal Chemistry Letters, Available online 16 February 2012.
2. Discovery of a Nortropanol Derivative as a Potent and Orally Active GPR119 Agonist for Type 2 Diabetes. Bioorganic & Medicinal Chemistry Letters 2011, 21, 3290-3296.
3. Discovery of a vorapaxar analog with increased aqueous solubility. Bioorganic & Medicinal Chemistry Letters 2010, 20, 6676-6679.
4. The role of exploratory drug metabolism and pharmacokinetics in new drug research: case study-selection of a Thrombin Receptor Antagonist for development . Current Pharmaceutical Design, 2009, 15, 2262-2269.
5. Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity. Journal of Medicinal Chemistry; 2008, 51, 3061-3064.
6. Heterotricyclic Himbacine Analogs as Potent, Orally Active Thrombin Receptor (Protease Activated Receptor-1) Antagonists. Journal of Medicinal Chemistry, 2007, 50, 5147-5160.
7. Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring. Bioorganic & Medicinal Chemistry Letters 2007, 17, 4509-4513.
8. Himbacine derived thrombin receptor antagonists: Discovery of a new tricyclic core. Bioorganic & Medicinal Chemistry Letters 2007, 17, 3647-3651.
9. Metabolism-Based Identification of a Potent Thrombin Receptor Antagonis. Journal of Medicinal Chemistry 2007, 50, 129-138.
10. Himbacine derived thrombin receptor (PAR-1) antagonists: Structure-activity relationship of the lactone ring. Bioorganic & medicinal chemistry letters 2006, 16, 4969-4972.
11. Thrombin receptor (PAR-1) antagonists as novel antithrombotic agents. Expert Opinion on Therapeutic Patents 2006, 16, 493-505.
12. Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists. Bioorganic & Medicinal Chemistry Letters 2006, 16, 1544
13. Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents. Journal of Medicinal Chemistry 2005, 48, 5884-5887.
專利
1. Bicyclic heterocycle derivatives and their use as gpcr modulators. WO 20100092072.
2. Preparation of heterocyclic compounds as factor IXa inhibitors. WO 2009143039
3. Combination therapies comprising PAR1 antagonists with PAR4 antagonists for treatment of diseases assocd. with thrombosis. WO 2009124103
4. Bicyclic heterocycle derivatives and methods of use thereof. WO 2009055331
5. Preparation of bicyclic and tricyclic himbacine derivatives as thrombin receptor antagonists. WO 2008042422
6. Preparation of bicyclic and tricyclic himbacine derivatives as thrombin receptor antagonists. US 2008004318
7. Fused ring thrombin receptor antagonists. US 2007244163
8. Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists. US 2007232635
9. Diaryl piperidines as CB1 modulators and their preparation, pharmaceutical compositions and use in the treatment of diseases. WO 2007084319
10. Spiroheterocyclic-decalin compounds as thrombin receptor antagonists and their preparation and pharmaceutical compostions. WO 2006105217
11. Preparation of himbacine analogs for use in pharmaceutical compositions as thrombin receptor antagonists. US 2006079684
12. Preparation of constrained himbacine analogs as thrombin receptor antagonists. US 2005267155
13. Preparation of aminohydroxyalkyl cyclic amine BACE-1 inhibitors having a benzamide substituent. WO 2005016876
14. Tricyclic thrombin receptor antagonists. WO 2003089428
14. Adenosine A2a receptor antagonists. WO20010192264

獲獎記錄


2008年榮獲愛迪生(Thomas Alva Edison) 發明獎;1996、2003年二獲科研所長獎(President’s Award)。