- Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors
[作者:WANG TAO; LAMB MICHELLE L; BLOCK MICHAEL H; DAVIES AUDREY MOLINA; HAN YONGXIN; HOFFMANN ETHAN; IOANNIDIS STEPHANOS; JOSEY JOHN A; LIU ZHONGYING; LYNE PAUL D; MACINTYRE TERRY; MOHR PETER J; OMER CHARLES A; SJOGREN TOVE; THRESS KENNETH; WANG BIN; WANG HAIYUN; YU DINGWEI; ZHANGT HAIJUN,期刊:ACS Medicinal Chemistry Letters, 页码:705-709 , 文章类型: Article,,卷期:2012年3-9]
- Trk receptor tyrosine kinases have been implicated in cancer and pain. A crystal structure of TrkA with AZ-23 (1a) was obtained, and scaffold hopping resulted in two 5/6-bicyclic series comprising either imidazo[4,5-b]py...
- Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist
[作者:BROWN SEAN P; DRANSFIELD PAUL J; VIMOLRATANA MARC; JIAO XIANYUN; ZHU LIUSHENG; PATTAROPONG VATEE; SUN YING; LIU JINQIAN; LUO JIAN; ZHANG JANE; WONG SIMON; ZHUANG RUN; GUO QI; LI FRANK; MEDINA JULIO C; SWAMINATH GAYATHRI; LIN DANIEL C H; HOUZE JONATHAN B,期刊:ACS Medicinal Chemistry Letters, 页码:726-730 , 文章类型: Article,,卷期:2012年3-9]
- GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activation of which elicits increased insulin secretion only in the presence of elevated glucose levels. A potent, orally bioava...
- Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease
[作者:PRIME MICHAEL E; BROOKFIELD FREDERICK A; COURTNEY STEPHEN M; GAINES SIMON; MARSTON RICHARD W; ICHIHARA OSAMU; LI MARIE; VAIDYA DARSHAN; WILLIAMS HELEN; PEDRETDUNN ANNA; REED LAURA; SCHAERTL SABINE; TOLEDOSHERMAN LETICIA; BECONI MARIA; MACDONALD DOUGLAS; MUNOZSANJUAN IGNACIO; DOMINGUEZ CELIA; WITYAK JOHN,期刊:ACS Medicinal Chemistry Letters, 页码:731-735 , 文章类型: Article,,卷期:2012年3-9]
- A new series of potent TG2 inhibitors are reported that employ a 4-aminopiperidine core bearing an acrylamide warhead. We establish the structure activity relationship of this new series and report on the transglutaminas...
|