479612-36-7Relevant academic research and scientific papers
INHIBITORS OF KEAP1-Nrf2 PROTEIN-PROTEIN INTERACTION
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, (2020/03/01)
Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
PROCESS FOR PREPARING 1-ARYLSULFONYL-PYRROLIDINE-2-CARBOXAMIDE TRANSIENT RECEPTOR POTENTIAL CHANNEL ANTAGONIST COMPOUNDS AND CRYSTALLINE FORMS THEREOF
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Paragraph 0429; 0439-0443, (2019/09/12)
The invention relates generally to methods of preparing 1-arylsulfonyl-pyrrolidine-2-carboxamide Transient Receptor Potential channel antagonist compounds of the following structure (I): (I) The invention further relates to solvate and co-crystal polymorphs of crystalline formula (I), and methods of preparation thereof.
Potent N-(1,3-Thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel
Bilodeau, Mark T.,Balitza, Adrienne E.,Koester, Timothy J.,Manley, Peter J.,Rodman, Leonard D.,Buser-Doepner, Carolyn,Coll, Kathleen E.,Fernandes, Christine,Gibbs, Jackson B.,Heimbrook, David C.,Huckle, William R.,Kohl, Nancy,Lynch, Joseph J.,Mao, Xianzhi,McFall, Rosemary C.,McLoughlin, Debra,Miller-Stein, Cynthia M.,Rickert, Keith W.,Sepp-Lorenzino, Laura,Shipman, Jennifer M.,Subramanian, Raju,Thomas, Kenneth A.,Wong, Bradley K.,Yu, Sean,Hartman, George D.
, p. 6363 - 6372 (2007/10/03)
A series of N-(1,3-thiazol-2-yl)pyridin-2-amine KDR kinase inhibitors have been developed that possess optimal properties. Compounds have been discovered that exhibit excellent in vivo potency. The particular challenges of overcoming hERG binding activity and QTc increases in vivo in addition to achieving good pharmacokinetics have been acomplished by discovering a unique class of amine substituents. These compounds have a favorable kinase selectivity profile that can be accentuated with appropriate substitution.
