917882-63-4Relevant academic research and scientific papers
1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES
-
Page/Page column 232; 233, (2016/07/05)
The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
Discovery of a 5 H-benzo[4,5]cyclohepta[1,2-b ]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer
Katz, Jason D.,Jewell, James P.,Guerin, David J.,Lim, Jongwon,Dinsmore, Christopher J.,Deshmukh, Sujal V.,Pan, Bo-Sheng,Marshall, C. Gary,Lu, Wei,Altman, Michael D.,Dahlberg, William K.,Davis, Lenora,Falcone, Danielle,Gabarda, Ana E.,Hang, Gaozhen,Hatch, Harold,Holmes, Rachael,Kunii, Kaiko,Lumb, Kevin J.,Lutterbach, Bart,Mathvink, Robert,Nazef, Naim,Patel, Sangita B.,Qu, Xianlu,Reilly, John F.,Rickert, Keith W.,Rosenstein, Craig,Soisson, Stephen M.,Spencer, Kerrie B.,Szewczak, Alexander A.,Walker, Deborah,Wang, Wenxian,Young, Jonathan,Zeng, Qinwen
supporting information; experimental part, p. 4092 - 4108 (2011/08/06)
c-Met is a transmembrane tyrosine kinase that mediates activation of several signaling pathways implicated in aggressive cancer phenotypes. In recent years, research into this area has highlighted c-Met as an attractive cancer drug target, triggering a number of approaches to disrupt aberrant c-Met signaling. Screening efforts identified a unique class of 5H-benzo[4,5] cyclohepta[1,2-b]pyridin-5-one kinase inhibitors, exemplified by 1. Subsequent SAR studies led to the development of 81 (MK-2461), a potent inhibitor of c-Met that was efficacious in preclinical animal models of tumor suppression. In addition, biochemical studies and X-ray analysis have revealed that this unique class of kinase inhibitors binds preferentially to the activated (phosphorylated) form of the kinase. This report details the development of 81 and provides a description of its unique biochemical properties.
Tyrosine kinase inhibitors
-
Page/Page column 15, (2009/07/25)
This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N′-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine
