440105-74-8Relevant academic research and scientific papers
Discovery and optimization of potent GPR40 full agonists containing tricyclic spirocycles
Wang, Yingcai,Liu, Jiwen,Dransfield, Paul J.,Zhu, Liusheng,Wang, Zhongyu,Du, Xiaohui,Jiao, Xianyun,Su, Yongli,Li, An-Rong,Brown, Sean P.,Kasparian, Annie,Vimolratana, Marc,Yu, Ming,Pattaropong, Vatee,Houze, Jonathan B.,Swaminath, Gayathri,Tran, Thanhvien,Nguyen, Khanh,Guo, Qi,Zhang, Jane,Zhuang, Run,Li, Frank,Miao, Lynn,Bartberger, Michael D.,Correll, Tiffany L.,Chow, David,Wong, Simon,Luo, Jian,Lin, Daniel C.-H.,Medina, Julio C.
supporting information, p. 551 - 555 (2013/07/25)
GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to its unique mechanism leading to little risk of hypoglycemia. We recently reported the discovery of AM-1638 (2), a potent full agonist of GPR40. In this repor
3-Aminopyrrolidinone farnesyltransferase inhibitors: Design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency
Bell, Ian M.,Gallicchio, Steven N.,Abrams, Marc,Beese, Lorena S.,Beshore, Douglas C.,Bhimnathwala, Hema,Bogusky, Michael J.,Buser, Carolyn A.,Culberson, J. Christopher,Davide, Joseph,Ellis-Hutchings, Michelle,Fernandes, Christine,Gibbs, Jackson B.,Graham, Samuel L.,Hamilton, Kelly A.,Hartman, George D.,Heimbrook, David C.,Homnick, Carl F.,Huber, Hans E.,Huff, Joel R.,Kassahun, Kelem,Koblan, Kenneth S.,Kohl, Nancy E.,Lobell, Robert B.,Lynch Jr., Joseph J.,Robinson, Ronald,Rodrigues, A. David,Taylor, Jeffrey S.,Walsh, Eileen S.,Williams, Theresa M.,Zartmant, C. Blair
, p. 2388 - 2409 (2007/10/03)
A series of macrocyclic 3-aminopyrrolidinone farnesyltransferase inhibitors (FTIs) has been synthesized. Compared with previously described linear 3-aminopyrrolidinone FTIs such as compound 1, macrocycles such as 49 combined improved pharmacokinetic prope
