102266-59-1Relevant articles and documents
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors
Zhao, Hongyu,Serby, Michael D.,Xin, Zhili,Szczepankiewicz, Bruce G.,Liu, Mei,Kosogof, Christi,Liu, Bo,Nelson, Lissa T. J.,Johnson, Eric F.,Wang, Sanyi,Pederson, Terry,Gum, Rebecca J.,Clampit, Jill E.,Haasch, Deanna L.,Abad-Zapatero, Cele,Fry, Elizabeth H.,Rondinone, Cristina,Trevillyan, James M.,Sham, Hing L.,Liu, Gang
, p. 4455 - 4458 (2006)
C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this report, we disclose a series of potent and highly selective JNK inhibitors with good pharmacokinetic profiles.
Inhibitors of c-Jun N-terminal kinases
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Page/Page column 35; 53, (2008/06/13)
The present invention relates to compounds that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.
Syntheses with Nitriles, LXXIV. - 3-Amino-4,4-dicyano-3-butenoate, a Synthetically Useful Dimer from Malononitrile and Cyanoacetate
Mittelbach, Martin,Junek, Hans
, p. 533 - 544 (2007/10/02)
An improved synthesis of 3-amino-4,4-dicyano-3-butenoate (4) (a codimer from cyanoacetate and malononitrile) is described.The 13C NMR data and pKa value of 4 are compared with those of the isomeric codimer 3 and the dimers 1 and 2.Reaction of 4 with acids or bases leads to the 2(1H)-pyridones 8 and 9, respectively.Conversions of 4 with aldehydes, ketones, and nitroso compounds give the products 11,14, and 15 as well as the benzopyran derivatives 12 and the 2-oxochinoline derivative 13 when using 2-hydroxy- and 2-aminobenzaldehydes. 4 reacts with formamidine to yield the dihydropyrimidine derivative 17 and with sulfur to give the 3,5-diamino-4-cyano-2-thiophenecarboxylates (18).