115029-22-6Relevant articles and documents
Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors
Qin, Donghui,Lin, Xiaojuan,Liu, Zhi,Chen, Yan,Zhang, Zhiliu,Wu, Chengde,Liu, Linlin,Pan, Yan,Laquerre, Sylvie,Emery, John,Fergusson, Jeff,Roland, Kimberly,Keenan, Rick,Oliff, Allen,Kumar, Sanjay,Cheung, Mui,Su, Dai-Shi
, p. 1005 - 1010 (2021)
We report herein the discovery of quinazolindiones as potent and selective tankyrase inhibitors. Elucidation of the structure-activity relationship of the lead compound 1g led to truncated analogues that have good potency in cells, pharmacokinetic (PK) properties, and excellent selectivity. Compound 21 exhibited excellent potencies in cells and proliferation studies, good selectivity, in vitro activities, and an excellent PK profile. Compound 21 also inhibited H292 xenograft tumor growth in nude mice. The synthesis, biological, pharmacokinetic, in vivo efficacy studies, and safety profiles of compounds are presented.
P2X7 MODULATORS
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Paragraph 0284; 0286, (2014/09/29)
The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
INHIBITORS OF STEAROYL-COA DESATURASE
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, (2009/06/27)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.