- Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors
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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
- 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
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supporting information
p. 5235 - 5244
(2018/06/11)
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- 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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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
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Page/Page column 36
(2018/11/22)
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- Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors
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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
- 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
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supporting information
p. 999 - 1011
(2017/06/27)
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- INDAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
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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.
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Page/Page column 61
(2011/10/13)
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- PYRAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula (I): wherein Z, n, R1, R1A, R3, R4, and R5 are as defined herein, and methods of making and using the same.
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Page/Page column 44
(2011/10/13)
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- PYRIMIDINE DERIVATIVES
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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.
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Page/Page column 99
(2011/04/14)
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- NOVEL PYRIMIDINE DERIVATIVES 698
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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.
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Page/Page column 189
(2008/12/07)
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- Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines
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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
- 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.
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scheme or table
p. 5717 - 5721
(2009/06/30)
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