364793-52-2Relevant academic research and scientific papers
Synthesis of Fused Pyrimidinone and Quinolone Derivatives in an Automated High-Temperature and High-Pressure Flow Reactor
Tsoung, Jennifer,Bogdan, Andrew R.,Kantor, Stanislaw,Wang, Ying,Charaschanya, Manwika,Djuric, Stevan W.
, p. 1073 - 1084 (2018/06/18)
Fused pyrimidinone and quinolone derivatives that are of potential interest to pharmaceutical research were synthesized within minutes in up to 96% yield in an automated Phoenix high-temperature and high-pressure continuous flow reactor. Heterocyclic scaffolds that are either hard to synthesize or require multisteps are readily accessible using a common set of reaction conditions. The use of low-boiling solvents along with the high conversions of these reactions allowed for facile workup and isolation. The methods reported herein are highly amenable for fast and efficient heterocycle synthesis as well as compound scale-ups.
Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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, (2016/04/26)
The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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, (2015/02/19)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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, (2014/10/04)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors
Pannala, Madhavi,Kher, Sunil,Wilson, Norma,Gaudette, John,Sircar, Ila,Zhang, Shao-Hui,Bakhirev, Alexei,Yang, Guang,Yuen, Phoebe,Gorcsan, Frank,Sakurai, Naoki,Barbosa, Miguel,Cheng, Jie-Fei
, p. 5978 - 5982 (2008/03/11)
Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.
Inhibition of Tpl2 kinase and TNFα production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis
Hu, Yonghan,Green, Neal,Gavrin, Lori K.,Janz, Kristin,Kaila, Neelu,Li, Huan-Qiu,Thomason, Jennifer R.,Cuozzo, John W.,Hall, J. Perry,Hsu, Sang,Nickerson-Nutter, Cheryl,Telliez, Jean-Baptiste,Lin, Lih-Ling,Tam, Steve
, p. 6067 - 6072 (2007/10/03)
The synthesis and structure-activity studies of a series of quinoline-3-carbonitriles as inhibitors of Tpl2 kinase are described. Potent inhibitors of Tpl2 kinase with selectivity against a panel of selected kinases in enzymatic assays and specificity in cell-based phosphorylation assays in LPS-treated human monocytes were identified. Selected inhibitors with moderate activity in human whole blood assay effectively inhibited LPS/D-Gal induced TNFα release when administered intraperitoneally in mice.
3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
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, (2008/06/13)
This invention provides compounds of Formula (I), having the structure where T, Z, X, A, R1, R2a, R2b, R2c, R3, R4, and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of osteoporosis and polycystic kidney disease.
Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles.
Boschelli, Diane H,Wang, Daniel Y,Ye, Fei,Yamashita, Ayako,Zhang, Nan,Powell, Dennis,Weber, Jennifer,Boschelli, Frank
, p. 2011 - 2014 (2007/10/03)
Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observed.
