1239461-71-2Relevant academic research and scientific papers
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor
Bowers, Simeon,Truong, Anh P.,Neitz, R. Jeffrey,Neitzel, Martin,Probst, Gary D.,Hom, Roy K.,Peterson, Brian,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergley,Pan, Hu,Yao, Nanhua,Artis, Dean R.,Brigham, Elizabeth F.,Quinn, Kevin P.,Sauer, John-Michael,Powell, Kyle,Ruslim, Lany,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
, p. 1838 - 1843 (2011/05/05)
The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the 4-position of the thiophene we obtained single digit nanomolar compounds, such as 47, which demonstrated an in vivo effect on JNK activity when dosed orally in our kainic acid mouse model as measured by phospho-c-jun reduction.
INHIBITORS OF JUN N-TERMINAL KINASE
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Page/Page column 129, (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.
