518990-33-5Relevant articles and documents
3-ARYLINDAZOLES AS SELECTIVE MEK4 INHIBITORS
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Paragraph 0152; 0179-0180; 0184-0185, (2021/01/22)
Disclosed are indazole compounds and derivatives thereof for use as modulators of the activity of mitogen-activated protein kinase 4 (MEK4). The disclosed compounds include 3-Arylindazoles which may be formulated in pharmaceutical composition for treating cell proliferative diseases and disorders associated with MEK4 activity, including cancer.
Synthesis and Biological Evaluation of 3-Arylindazoles as Selective MEK4 Inhibitors
Bergan, Raymond,Clutter, Matthew R.,Deibler, Kristine K.,Fowler, Graham,George, Mariam Donny,Gordon, Ryan,Mishra, Rama K.,O'Connor, Matthew,Scheidt, Karl A.,Schiltz, Gary E.,Vagadia, Purav P.
supporting information, p. 615 - 620 (2019/02/25)
Herein we report the discovery of a novel series of highly potent and selective mitogen-activated protein kinase kinase 4 (MEK4) inhibitors. MEK4 is an upstream kinase in MAPK signaling pathways that phosphorylates p38 MAPK and JNK in response to mitogenic and cellular stress queues. MEK4 is overexpressed and induces metastasis in advanced prostate cancer lesions. However, the value of MEK4 as an oncology target has not been pharmacologically validated because selective chemical probes targeting MEK4 have not been developed. Optimization of this series via structure–activity relationships and molecular modeling led to the identification of compound 6 ff (4-(6-fluoro-2H-indazol-3-yl)benzoic acid), a highly potent and selective MEK4 inhibitor. This series of inhibitors is the first of its kind in both activity and selectivity and will be useful in further defining the role of MEK4 in prostate and other cancers.
ALKYNYL ALCOHOLS AND METHODS OF USE
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, (2015/03/13)
The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over- activation of NF-kB signaling is observed.
4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
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Page/Page column 76, (2014/03/22)
The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
New CRTh2 antagonists.
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Paragraph 0187, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
NEW CRTh2 ANTAGONISTS
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Page/Page column 69, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
NOVEL ANTIVIRAL COMPOUNDS
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, (2012/05/31)
The present invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection such as HIV using the same.