959774-49-3Relevant academic research and scientific papers
CARBAMOYLOXYMETHYL TRIAZOLE CYCLOHEXYL ACIDS AS LPA ANTAGONISTS
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Paragraph 1007-1008, (2018/01/18)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Discovery of isonicotinamide derived β-secretase inhibitors: In vivo reduction of β-amyloid
Stanton, Matthew G.,Stauffer, Shaun R.,Gregro, Alison R.,Steinbeiser, Melissa,Nantermet, Philippe,Sankaranarayanan, Sethu,Price, Eric A.,Wu, Guoxin,Crouthamel, Ming-Chih,Ellis, Joan,Lai, Ming-Tain,Espeseth, Amy S.,Shi, Xiao-Ping,Jin, Lixia,Colussi, Dennis,Pietrak, Beth,Huang, Qian,Xu, Min,Simon, Adam J.,Graham, Samuel L.,Vacca, Joseph P.,Selnick, Harold
, p. 3431 - 3433 (2008/02/11)
β-Secretase inhibition offers an exciting opportunity for therapeutic intervention in the progression of Alzheimer's disease. A series of isonicotinamides derived from traditional aspartyl protease transition state isostere inhibitors has been optimized to yield low nanomolar inhibitors with sufficient penetration across the blood-brain barrier to demonstrate β-amyloid lowering in a murine model.
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation
Stauffer, Shaun R.,Stanton, Matthew G.,Gregro, Alison R.,Steinbeiser, Melissa A.,Shaffer, Jennifer R.,Nantermet, Philippe G.,Barrow, James C.,Rittle, Kenneth E.,Collusi, Dennis,Espeseth, Amy S.,Lai, Ming-Tain,Pietrak, Beth L.,Holloway, M. Katharine,McGaughey, Georgia B.,Munshi, Sanjeev K.,Hochman, Jerome H.,Simon, Adam J.,Selnick, Harold G.,Graham, Samuel L.,Vacca, Joseph P.
, p. 1788 - 1792 (2008/02/02)
A series of low-molecular weight 2,6-diamino-isonicotinamide BACE-1 inhibitors containing an amine transition-state isostere were synthesized and shown to be highly potent in both enzymatic and cell-based assays. These inhibitors contain a trans-S,S-methyl cyclopropane P3 which bind BACE-1 in a 10s-loop down conformation giving rise to highly potent compounds with favorable molecular weight and moderate to high susceptibility to P-glycoprotein (P-gp) efflux.
