945397-20-6Relevant academic research and scientific papers
NOVEL INHIBITORS OF MAP4K1
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Page/Page column 67; 118, (2018/12/13)
The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R5, R6, R7, Z, ring Q, n, x and y are as given in the application.
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
supporting information, 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
PYRIMIDINE DERIVATIVES
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Page/Page column 102-103, (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.
NOVEL PYRIMIDINE DERIVATIVES 698
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Page/Page column 191, (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.
