925922-24-3Relevant academic research and scientific papers
PYRIDYLPHENOL COMPOUND AND USE THEREOF
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Page/Page column 62, (2008/12/05)
The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula -X-R1 wherein X represents a bond or a spacer, and R1 represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R2 represents an optionally substituted homocyclic or heterocyclic group; and R3 and R4 independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.
Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1
Murata, Toshiki,Shimada, Mitsuyuki,Sakakibara, Sachiko,Yoshino, Takashi,Kadono, Hiroshi,Masuda, Tsutomu,Shimazaki, Makoto,Shintani, Takuya,Fuchikami, Kinji,Sakai, Katsuya,Inbe, Hisayo,Takeshita, Keisuke,Niki, Toshiro,Umeda, Masaomi,Bacon, Kevin B.,Ziegelbauer, Karl B.,Lowinger, Timothy B.
, p. 913 - 918 (2007/10/03)
IκB kinase β (IKK-β) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-κB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-β. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-β inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFα).
