99557-99-0Relevant academic research and scientific papers
Piperazine substituted 1, 3 - di-substituted urea compound and piperazine substituted amide compounds and a method for its preparation and use
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Paragraph 0209-0211, (2017/04/22)
The present invention relates to a class of piperazine substituted 1,3-disubstitued urea compounds and piperazine substituted amide compounds, or pharmaceutically acceptable salts of the piperazine substituted 1,3-disubstitued urea compounds and the piper
Discovery of potent and selective rhodanine type IKKβ inhibitors by hit-to-lead strategy
Song, Hyeseung,Lee, Yun Suk,Roh, Eun Joo,Seo, Jae Hong,Oh, Kwang-Seok,Lee, Byung Ho,Han, Hogyu,Shin, Kye Jung
scheme or table, p. 5668 - 5674 (2012/09/22)
Regulation of NF-κB activation through the inhibition of IKKβ has been identified as a promising target for the treatment of inflammatory and autoimmune disease such as rheumatoid arthritis. In order to develop novel IKKβ inhibitors, we performed high throughput screening toward around 8000 library compounds, and identified a hit compound containing rhodanine moiety. We modified the structure of hit compound to obtain potent and selective IKKβ inhibitors. Throughout hit-to-lead studies, we have discovered optimized compounds which possess blocking effect toward NF-κB activation and TNFα production in cell as well as inhibition activity against IKKβ. Among them, compound 3q showed the potent inhibitory activity against IKKβ, and excellent selectivity over other kinases such as p38α, p38β, JNK1, JNK2, and JNK3 as well as IKKα.
PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS
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Page/Page column 395, (2010/08/05)
The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
Incorporation of piperazino functionality into 1,3-disubstituted urea as the tertiary pharmacophore affording potent inhibitors of soluble epoxide hydrolase with improved pharmacokinetic properties
Huang, Shao-Xu,Li, Hui-Yuan,Liu, Jun-Yan,Morisseau, Christophe,Hammock, Bruce D.,Long, Ya-Qiu
supporting information; experimental part, p. 8376 - 8386 (2011/02/21)
The inhibition of the mammalian soluble epoxide hydrolase (sEH) is a promising new therapy in the treatment of hypertension, inflammation, and other disorders. However, the problems of limited water solubility, high melting point, and low metabolic stabil
11H-Isoindoloindol-11-ones: Novel Rearrangement Products from the Attempted Preparation of 2-(2-Diethylaminomethylphenyl)isatogens
Hooper, Malcolm,Imam, S. Haider
, p. 1583 - 1588 (2007/10/02)
The attempted synthesis of 2-(2-diethylaminomethylphenyl)isatogens, from appropriately substituted phenylacetylenes and aromatic iodo compounds by two different routes gave novel substituted 11H-isoindoloindol-11-ones (6a-d) as the only identifiabl
