5912-36-7Relevant academic research and scientific papers
METHODS OF USE FOR PYRIMIDINES AS FERROPORTIN INHIBITORS
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, (2021/11/06)
The subject matter described herein is directed to ferroportin inhibitor compounds of Formula (I) and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.
Design and synthesis of a novel series of 4-heteroarylamino-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR
Iwuagwu, Christiana,King, Dalton,McDonald, Ivar M.,Cook, James,Zusi, F. Christopher,Hill, Matthew D.,Mate, Robert A.,Fang, Haiquan,Knox, Ronald,Gallagher, Lizbeth,Post-Munson Amy Easton, Debra,Miller, Regina,Benitex, Yulia,Siuciak, Judy,Lodge, Nicholas,Zaczek, Robert,Morgan, Daniel,Bristow, Linda,Macor, John E.,Olson, Richard E.
supporting information, p. 1261 - 1266 (2017/06/19)
Quinuclidine-containing spirooxazolines, as described in the previous report in this series, were demonstrated to have utility as α7 nicotinic acetylcholine receptor (α7 nAChR) partial agonists. In this work, the SAR of this chemotype was expanded to include an array of diazine heterocyclic substitutions. Many of the heterocyclic analogs were potent partial agonists of the α7 receptor, selective against other nicotinic receptors and the serotinergic 5HT3A receptor. (1′S,3′R,4′S)-N-(6-phenylpyrimidin-4-yl)-4H-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octan]-2-amine, a potent and selective α7 nAChR partial agonist, was demonstrated to improve cognition in the mouse novel object recognition (NOR) model of episodic memory.
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: Discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives
Nishimura, Nobuko,Siegmund, Aaron,Liu, Longbin,Yang, Kevin,Bryan, Marian C.,Andrews, Kristin L.,Bo, Yunxin,Booker, Shon K.,Caenepeel, Sean,Freeman, Daniel,Liao, Hongyu,McCarter, John,Mullady, Erin L.,San Miguel, Tisha,Subramanian, Raju,Tamayo, Nuria,Wang, Ling,Whittington, Douglas A.,Zalameda, Leeanne,Zhang, Nancy,Hughes, Paul E.,Norman, Mark H.
, p. 4735 - 4751 (2011/09/20)
The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3′-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival. There is abundant evidence demonstrating that PI3K signaling is dysregulated in many human cancers, suggesting that therapeutics targeting the PI3K pathway may have utility for the treatment of cancer. Our efforts to identify potent, efficacious, and orally available PI3K/mammalian target of rapamycin (mTOR) dual inhibitors resulted in the discovery of a series of substituted quinolines and quinoxalines derivatives. In this report, we describe the structure-activity relationships, selectivity, and pharmacokinetic data of this series and illustrate the in vivo pharmacodynamic and efficacy data for a representative compound.
INHIBITORS OF PI3 KINASE
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, (2010/01/12)
The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.
