Filipski Kevin J
Cardiovascular, Metabolic and Endocrine Diseases Chemistry, Pfizer Worldwide Research and Development , 610 Main St, Cambridge, MA 02139 , USA +1 617 551 3267 ;
Expert Opin Ther Pat. 2015 Jul;25(7):819-30. doi: 10.1517/13543776.2015.1032250. Epub 2015 Mar 31.
Glucagon receptor antagonists (GCGRAs) have been an area of ongoing research in the pharmaceutical industry for more than two decades. Blocking the action of the glucagon peptide leads to repression of hepatic glucose production and reduced blood glucose. Small molecule GCGRAs continue to be pursued as a potential new treatment for diabetes.
The current review summarizes small molecule GCGRA patents and patent applications that first appeared during 2011 - 2014. The search term 'glucagon receptor' was used to find patents of the desired type.
Several companies have brought forward GCGRAs into human clinical trials with the most advanced to date being in Phase II. This field is mature and the number of patents has been decreasing in the last few years.
二十多年来，胰高血糖素受体拮抗剂（GCGRAs）一直是制药行业持续研究的领域。阻断胰高血糖素肽的作用会导致肝葡萄糖生成受到抑制，血糖降低。小分子GCGRAs仍在作为糖尿病的一种潜在新疗法进行研发。
本综述总结了2011年至2014年期间首次出现的小分子GCGRA专利和专利申请。使用搜索词“胰高血糖素受体”来查找所需类型的专利。
几家公司已将GCGRAs推进到人体临床试验阶段，目前最先进的处于II期。该领域已成熟，在过去几年中专利数量一直在减少。
