4815-35-4Relevant academic research and scientific papers
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms
Haidle, Andrew M.,Zabierek, Anna A.,Childers, Kaleen K.,Rosenstein, Craig,Mathur, Anjili,Altman, Michael D.,Chan, Grace,Xu, Lin,Bachman, Eric,Mo, Jan-Rung,Bouthillette, Melaney,Rush, Thomas,Tempest, Paul,Marshall, C. Gary,Young, Jonathan R.
, p. 1968 - 1973 (2014/04/17)
A series of carboxamide-substituted thiophenes demonstrating inhibition of JAK2 is described. Development of this chemical series began with the bioisosteric replacement of a urea substituent by a pyridyl ring. Issues of chemical and metabolic stability were solved using the results of both in vitro and in vivo studies, ultimately delivering compounds such as 24 and 25 that performed well in an acute PK/PD model measuring p-STAT5 inhibition.
Microwave-assisted synthesis of 5-substituted 2-aminothiophenes starting from arylacetaldehydes
Revelant, Germain,Dunand, Sandrine,Hesse, Stephanie,Kirsch, Gilbert
, p. 2935 - 2940 (2011/11/01)
An easy three-step pathway for the synthesis of arylacet-aldehydes from the corresponding carboxylic acids in very high yields is described. Their use as precursors of 5-substituted-2-aminothiophenes is illustrated via a microwave-assisted Gewald reaction. This method allows obtaining the expected compounds in a shorter time and with better yields and purities than the classical procedures. Georg Thieme Verlag Stuttgart - New York.
Nf-kb inhibitors
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, (2008/06/13)
The present invention provides novel compounds and methods for treating diseases with aminothiophene inhibitors of IKK-β phosphorylation of IκB.
Novel Compounds
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, (2008/06/13)
The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
