544669-76-3Relevant academic research and scientific papers
INHIBITORS OF JUN N-TERMINAL KINASE
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Page/Page column 96; 107, (2010/08/18)
The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula (I): or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK
Hom, Roy K.,Bowers, Simeon,Sealy, Jennifer M.,Truong, Anh P.,Probst, Gary D.,Neitzel, Martin L.,Neitz, R. Jeffrey,Fang, Larry,Brogley, Louis,Wu, Jing,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergely,Pan, Hu,Yao, Nanhua,Artis, Dean R.,Quinn, Kevin,Sauer, John-Michael,Powell, Kyle,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
scheme or table, p. 7303 - 7307 (2011/02/22)
From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards closely related MAP kinases p38 and Erk2. Herein we describe the evolution of these compounds to a novel class of thiophene and thiazole JNK inhibitors that retain favorable solubility, permeability, and P-gp properties for development as CNS agents for treatment of neurodegeneration. Compound 61 demonstrated JNK3 IC50 = 77 nM and retained the excellent broad kinase selectivity observed for the series.
