877060-47-4Relevant articles and documents
BICYCLIC JAK INHIBITORS AND USES THEREOF
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Paragraph 000217, (2020/10/20)
Provided herein are compounds of Formulas (I), (II), (III), and (IV) and subformulas thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), (II), (III), or (IV) and methods of using the compounds, e.g., in the treatment of immune disorders, inflammatory disorders, and cancer.
N-substituted azaindoles as potent inhibitors of Cdc7 kinase
Bryan, Marian C.,Falsey, James R.,Frohn, Mike,Reichelt, Andreas,Yao, Guomin,Bartberger, Michael D.,Bailis, Julie M.,Zalameda, Leeanne,Miguel, Tisha San,Doherty, Elizabeth M.,Allen, John G.
, p. 2056 - 2060 (2013/05/09)
Cdc7 kinase is responsible for the initiation and regulation of DNA replication and has been proposed as a target for cancer therapy. We have identified a class of Cdc7 inhibitors based on a substituted indole core. Synthesis of focused indole and azaindole analogs yielded potent and selective 5-azaindole Cdc7 inhibitors with improved intrinsic metabolic stability (ie 36). In parallel, quantum mechanical conformational analysis helped to rationalize SAR observations, led to a proposal of the preferred binding conformation in the absence of co-crystallography data, and allowed the design of 7-azaindole 37 as a second lead in this series.
[4[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL)-METHANONES AND SYNTHESIS THEREOF
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Page/Page column 45, (2011/07/09)
The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase including but not limited to for example asthma and other inflammatory diseases including age-related macular degeneration.