945397-18-2Relevant academic research and scientific papers
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors
Grimster, Neil P.,Anderson, Erica,Alimzhanov, Marat,Bebernitz, Geraldine,Bell, Kirsten,Chuaqui, Claudio,Deegan, Tracy,Ferguson, Andrew D.,Gero, Thomas,Harsch, Andreas,Huszar, Dennis,Kawatkar, Aarti,Kettle, Jason G.,Lyne, Paul,Read, Jon A.,Rivard Costa, Caroline,Ruston, Linette,Schroeder, Patricia,Shi, Jie,Su, Qibin,Throner, Scott,Toader, Dorin,Vasbinder, Melissa,Woessner, Richard,Wang, Haixia,Wu, Allan,Ye, Minwei,Zheng, Weijia,Zinda, Michael
, p. 5235 - 5244 (2018/06/11)
Janus kinases (JAKs) have been demonstrated to be critical in cytokine signaling and have thus been implicated in both cancer and inflammatory diseases. The JAK family consists of four highly homologous members: JAK1-3 and TYK2. The development of small-m
COMPOUND, COMPOUND FOR USE IN THE TREATMENT OF A PATHOLOGICAL CONDITION, A PHARMACEUTICAL COMPOSITION AND A METHOD FOR PREPARING SAID COMPOUND
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, (2018/11/22)
The invention concerns a compound, wherein the compound is a substance according to the following formula (I) wherein the ring A is a pyrrolidine, piperidine, morpholine, or imidazole residue or a substituted pyrrolidine, piperidine, morpholine, or imidaz
Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors
Heinzlmeir, Stephanie,Lohse, Jonas,Treiber, Tobias,Kudlinzki, Denis,Linhard, Verena,Gande, Santosh Lakshmi,Sreeramulu, Sridhar,Saxena, Krishna,Liu, Xiaofeng,Wilhelm, Mathias,Schwalbe, Harald,Kuster, Bernhard,Médard, Guillaume
, p. 999 - 1011 (2017/06/27)
The receptor tyrosine kinase EPHA2 has gained attention as a therapeutic drug target for cancer and infectious diseases. However, EPHA2 research and EPHA2-based therapies have been hampered by the lack of selective small-molecule inhibitors. Herein we rep
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors
McCoull, William,Hennessy, Edward J.,Blades, Kevin,Chuaqui, Claudio,Dowling, James E.,Ferguson, Andrew D.,Goldberg, Frederick W.,Howe, Nicholas,Jones, Christopher R.,Kemmitt, Paul D.,Lamont, Gillian,Varnes, Jeffrey G.,Ward, Richard A.,Yang, Bin
, p. 1118 - 1123 (2016/12/18)
Group I p21-activated kinase (PAK) inhibitors are indicated as important in cancer progression, but achieving high kinase selectivity has been challenging. A bis-anilino pyrimidine PAK1 inhibitor was identified and optimized through structure-based drug design to improve PAK1 potency and achieve high kinase selectivity, giving in vitro probe compound AZ13705339 (18). Reduction of lipophilicity to lower clearance afforded AZ13711265 (14) as an in vivo probe compound with oral exposure in mouse. Such probes will allow further investigation of PAK1 biology.
PYRIMIDINE DERIVATIVES
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Page/Page column 102, (2011/04/14)
The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, ring A, n, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.
INDAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
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Page/Page column 62, (2011/10/13)
Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R1, R1A, and R2 are as defined herein, and methods of making and using the same.
NOVEL PYRIMIDINE DERIVATIVES 698
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, (2008/12/07)
The invention concerns compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.
Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines
Bardelle, Catherine,Coleman, Tanya,Cross, Darren,Davenport, Sara,Kettle, Jason G.,Ko, Eun Jung,Leach, Andrew G.,Mortlock, Andrew,Read, Jon,Roberts, Nicola J.,Robins, Peter,Williams, Emma J.
scheme or table, p. 5717 - 5721 (2009/06/30)
Crystallographic studies of a range of 3-substituted anilinopyrimidine inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations and this discovery has been exploited in the design of a highly potent series of 3,5-disubstituted anilin
