916143-46-9Relevant academic research and scientific papers
A New Class of Amide Ligands Enable Cu-Catalyzed Coupling of Sodium Methanesulfinate with (Hetero)aryl Chlorides
Ma, Dawei,Niu, Songtao,Zhao, Jinlong,Jiang, Xi,Jiang, Yongwen,Zhang, Xiaojing,Sun, Tiemin
supporting information, p. 1661 - 1664 (2017/10/30)
((2S,4R)-4-Hydroxy-N-(2-methylnaphthalen-1-yl)pyrrolidine-2-carboxamide (HMNPC), an amide derived from 4-hydroxy-L-proline and 2-methyl naphthalen-1-amine, is a powerful ligand for Cu-catalyzed coupling of (hetero)aryl halides with sulfinic acid salts, allowing for first time the metal-catalyzed coupling of (hetero)aryl chlorides and NaSO2Me. A considerable number of (hetero)aryl chlorides worked well, providing the pharmaceutically important (hetero)aryl methylsulfones in good to excellent yields.
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres
Cohen, Frederick,Koehler, Michael F.T.,Bergeron, Philippe,Elliott, Linda O.,Flygare, John A.,Franklin, Matthew C.,Gazzard, Lewis,Keteltas, Stephen F.,Lau, Kevin,Ly, Cuong Q.,Tsui, Vickie,Fairbrother, Wayne J.
scheme or table, p. 2229 - 2233 (2010/06/15)
A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compound
INHIBITORS OF IAP
-
Page/Page column 76, (2008/12/08)
The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1 - M - U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3', R4, R4' and R5, are as described herein.
Proline bis-amides as potent dual orexin receptor antagonists
Bergman, Jeffrey M.,Roecker, Anthony J.,Mercer, Swati P.,Bednar, Rodney A.,Reiss, Duane R.,Ransom, Richard W.,Meacham Harrell,Pettibone, Douglas J.,Lemaire, Wei,Murphy, Kathy L.,Li, Chunze,Prueksaritanont, Thomayant,Winrow, Christopher J.,Renger, John J.,Koblan, Kenneth S.,Hartman, George D.,Coleman, Paul J.
, p. 1425 - 1430 (2008/12/21)
A series of OX2R/OX1R dual orexin antagonists was prepared based on a proline bis-amide identified as a screening lead. Through a combination of classical and library synthesis, potency enhancing replacements for both amide portions
INHIBITORS OF IAP
-
Page/Page column 52, (2008/06/13)
The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3', R4, R4', R5, R6, R6' and n are as described herein.
PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS
-
Page/Page column 38, (2008/06/13)
The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
