1446236-31-2Relevant academic research and scientific papers
Discovery of 8-Methyl-pyrrolo[1,2-a]pyrazin-1(2 H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors
Li, Zizhou,Xiao, Senhao,Yang, Yaxi,Chen, Chao,Lu, Tian,Chen, Zhifeng,Jiang, Hualiang,Chen, Shijie,Luo, Cheng,Zhou, Bing
, p. 3956 - 3975 (2020/05/27)
The bromodomain and extra-terminal (BET) family proteins have recently emerged as promising drug targets for cancer therapy. In this study, identification of an 8-methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one fragment (47) as a new binder to the BET bromodomains
PYRROLO[2,3-C]PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
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, (2018/08/03)
Disclosed are a pyrrolo[2,3-c]pyridine derivative, a preparation method therefor, and use thereof in medicine. Specifically, disclosed are a pyrrolo[2,3-c]pyridine derivative as represented by general formula (1), a preparation method therefor, a pharmaceutical composition comprising the derivative, as well as use thereof as a BRD4 inhibitor in the treatment of related diseases such as cancers, inflammations, chronic liver diseases, diabetes, cardiovascular diseases and AIDS, each substituent in general formula (I) being same as defined in the description.
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
McDaniel, Keith F.,Wang, Le,Soltwedel, Todd,Fidanze, Steven D.,Hasvold, Lisa A.,Liu, Dachun,Mantei, Robert A.,Pratt, John K.,Sheppard, George S.,Bui, Mai H.,Faivre, Emily J.,Huang, Xiaoli,Li, Leiming,Lin, Xiaoyu,Wang, Rongqi,Warder, Scott E.,Wilcox, Denise,Albert, Daniel H.,Magoc, Terrance J.,Rajaraman, Ganesh,Park, Chang H.,Hutchins, Charles W.,Shen, Jianwei J.,Edalji, Rohinton P.,Sun, Chaohong C.,Martin, Ruth,Gao, Wenqing,Wong, Shekman,Fang, Guowei,Elmore, Steven W.,Shen, Yu,Kati, Warren M.
, p. 8369 - 8384 (2017/11/03)
The development of bromodomain and extraterminal domain (BET) bromodomain inhibitors and their examination in clinical studies, particularly in oncology settings, has garnered substantial recent interest. An effort to generate novel BET bromodomain inhibi
BROMODOMAIN INHIBITORS
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Paragraph 1232; 1260, (2014/06/24)
The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
DIHYDRO-PYRROLOPYRIDINONE INHIBITORS
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, (2014/09/29)
The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
