916489-36-6Relevant academic research and scientific papers
AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF
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Paragraph 0207-0209, (2020/01/31)
The present invention aims to provide a compound that: has an excellent cytotoxic action on cancer cells, excellent induction of BET protein degradation in cancer cells, and an excellent binding-inhibiting action on BET protein and acetylated histone; and is effective as an anti-cancer agent, a BET protein degradation-inducing agent, or a BET protein inhibiting agent. A compound indicated in general formula (I) or a pharmacologically acceptable salt thereof. {In the formula, each symbol is as outlined in the Description.}
HETEROBIFUNCTIONAL COMPOUNDS WITH IMPROVED SPECIFICITYFOR THE BROMODOMAIN OF BRD4
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Paragraph 0351-0353, (2019/05/10)
Disclosed are heterobifunctional compounds that effectuate selective degradation of a target protein, and which include a targeting ligand that binds a target protein and at least one other protein, a ligand that binds an E3 ubiquitin ligase or a component of E3 ubiquitin ligase, and a specificity modulating linker that links the first ligand and the second ligand. Pharmaceutical compositions containing the compounds, and methods of using and making the compounds are also disclosed.
A phenotypic drug discovery study on thienodiazepine derivatives as inhibitors of T cell proliferation induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor
Endo, Junichi,Hikawa, Hidemasa,Hamada, Maiko,Ishibuchi, Seigo,Fujie, Naoto,Sugiyama, Naoki,Tanaka, Minoru,Kobayashi, Haruhito,Sugahara, Kunio,Oshita, Koichi,Iwata, Kazunori,Ooike, Shinsuke,Murata, Meguru,Sumichika, Hiroshi,Chiba, Kenji,Adachi, Kunitomo
supporting information, p. 1365 - 1370 (2016/02/19)
A phenotypic screening of thienodiazepines derived from a hit compound found through a binding assay targeting co-stimulatory molecules on T cells and antigen presenting cells successfully led to the discovery of a thienotriazolodiazepine compound (7f) po
THIENOTRIAZOLODIAZEPINE COMPOUND AND A MEDICINAL USE THEREOF
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Page/Page column 28, (2010/11/30)
[Solving means] A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. [Effect]
