페닐피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 글루카곤 수용체 활성 관련 질환의 예방 또는 치료용 약학적 조성물
申请人:Gachon University of Industry-Academic cooperation Foundation 가천대학교 산학협력단(220040376324) BRN ▼129-82-07687
公开号:KR20200021741A
公开(公告)日:2020-03-02
페닐피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 글루카곤 수용체 활성 관련 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 상기 페닐피리미딘 유도체는 cAMP 또는 글루카곤 생성 저해 효과가 우수하여 GCGR 활성 저해 효과를 나타내고, 우수한 혈당 강하 효과를 나타냄을 in vitro 뿐만 아니라 in vivo에서도 확인하였으며, 세포 독성이 낮아, 안전성이 검증된 바, GCGR 활성 관련 질환인 대사성 질환 특히, 당뇨의 치료에 유용하게 사용될 수 있다.
Synthesis of C-14 radiolabeled glucagon receptor antagonist and its use in a human mass balance study
作者:Boris A. Czeskis、Darlene K. Satonin
DOI:10.1002/jlcr.3477
日期:2017.2
The synthesis of the radiolabeled glucagon receptorantagonist 1-[14 C] was accomplished based on decarboxylative iodination of acid 2 followed by "reattachment" of 14 C carboxylic function. The method allowed a significant reduction in the number of steps in preparation of the radiolabeled compound. Iodide 4, obtained by the halodecarboxylation, was converted to cyanide 5-[14 C], which was hydrolyzed
Glucagon receptor antagonists, preparation and therapeutic uses
申请人:Conner Scott Eugene
公开号:US08609892B2
公开(公告)日:2013-12-17
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.