896738-16-2Relevant articles and documents
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors
Kaieda, Akira,Takahashi, Masashi,Takai, Takafumi,Goto, Masayuki,Miyazaki, Takahiro,Hori, Yuri,Unno, Satoko,Kawamoto, Tomohiro,Tanaka, Toshimasa,Itono, Sachiko,Takagi, Terufumi,Hamada, Teruki,Shirasaki, Mikio,Okada, Kengo,Snell, Gyorgy,Bragstad, Ken,Sang, Bi-Ching,Uchikawa, Osamu,Miwatashi, Seiji
, p. 647 - 660 (2018/01/03)
We identified novel potent inhibitors of p38 MAP kinase using structure-based design strategy. X-ray crystallography showed that when p38 MAP kinase is complexed with TAK-715 (1) in a co-crystal structure, Phe169 adopts two conformations, where one intera
CONDENSED IMIDAZOLE COMPOUND AND USE THEREOF
-
Page/Page column 81-82, (2010/11/28)
The present invention relates to a compound represented by the formula [I] wherein X1, X2 and X3 are each an optionally substituted CH or a nitrogen atom, and any one of X1, X2 and X3 is a nitrogen atom, X4 is an optionally substituted CH, R1 is an optionally substituted phenyl group or an optionally substituted heterocyclic group, and R2 is an optionally substituted pyridin-4-yl group, an optionally substituted pyridine-N-oxide-4-yl group or an optionally substituted pyrimidin-4-yl group, or a salt thereof. The compound has superior p38 MAP kinase inhibitory activity and MMP-13 production inhibitory activity, and is useful as an agent for the prophylaxis or treatment and the like of an inflammatory disease, an autoimmune disease, a debilitating disease, an osteoarticular degenerative disease, a neurodegenerative disease, a vascular disease, a neoplastic disease or an infectious disease.