- Transition metal-free direct C–H trifluoromethyltion of (hetero)arenes with Togni's reagent
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A new transition-metal-free direct C–H trifluoromethylation reaction of (hetero)arenes with Togni's reagent was developed. This transformation proceeded smoothly under mild conditions and exhibited good tolerance of many synthetically relevant functional groups. It provided an alternative approach for the synthesis of trifluoromethylated (hetero)arenes.
- Chen, Xiaoyu,Ding, Licheng,Li, Linlin,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
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- Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
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The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds were designed based on information derived from metabolite identification studies which led to compounds such as 42 with lower clearance, greater brain exposure and longer half life compared to earlier analogs.
- Bowers, Simeon,Truong, Anh P.,Jeffrey Neitz,Hom, Roy K.,Sealy, Jennifer M.,Probst, Gary D.,Quincy, David,Peterson, Brian,Chan, Wayman,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergely,Pan, Hu,Lin, May,Yao, Nanhua,Artis, Dean R.,Zhang, Heather,Chen, Linda,Dryer, Mark,Samant, Bhushan,Zmolek, Wes,Wong, Karina,Lorentzen, Colin,Goldbach, Erich,Tonn, George,Quinn, Kevin P.,Sauer, John-Michael,Wright, Sarah,Powell, Kyle,Ruslim, Lany,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
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scheme or table
p. 5521 - 5527
(2011/10/09)
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- INHIBITORS OF JUN N-TERMINAL KINASE
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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.
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Page/Page column 101
(2010/08/18)
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