- Structure-driven HtL: Design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity
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The design and synthesis of a new series of c-Jun N-terminal kinase inhibitors are reported. The novel series of substituted amino indazoles were designed based on a combination of hits from high-throughput screening and X-ray crystal structure informatio
- Stocks, Michael J.,Barber, Simon,Ford, Rhonan,Leroux, Frederic,St-Gallay, Steve,Teague, Simon,Xue, Yafeng
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- INDAZOLE/PYRZOLO[4,3-c]PYRIDIN DERIVATIVES AS JNK INHIBITORS, COMPOSITIONS AND METHODS RELATED THERETO AS WELL AS INTERMEDIATE THEREOF
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The present invention relates to new compounds of formula (I) in which:X is CR4 or N; R1 is -OR5, -NHCOR6 or -NR6R7; R2 is hydrogen, Oar1 or -NHAr1 wherein Ar1 is aryl optionally substituted with one or more of R8, -OR8, -NR8R9, -CONR8R9, -COOR8, -NR8COR9, -SR8, -SO2NR8R9, -NR8SO2 R9, halogen, cyano, or nitro; R3 is hydrogen or -NHAr2 wherein Ar2 is benzene optionally substituted with one or more of R8, -OR8, -NR8R9, halogen or nitro, wherein R2 and R3 is not simultaneously hydrogen; a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
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