754159-15-4Relevant academic research and scientific papers
A convergent preparation of the CHK1 inhibitor MK-8776 (SCH 900776)
Labroli, Marc A.,Dwyer, Michael P.,Poker, Cory,Keertikar, Kerry M.,Rossman, Randall,Guzi, Timothy J.
, p. 2601 - 2603 (2016)
This Letter describes the development of a convergent, efficient route to the CHK1 inhibitor MK-8776. This synthetic approach relies upon the cyclization of a bispyrazole adduct 10 with a optically pure β-keto nitrile 9 to construct the pyrazolo[1,5-a]pyrimidine scaffold in a single step.
COMPOSITIONS AND METHODS FOR TREATING CANCER
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Page/Page column 34, (2014/05/07)
The instant invention relates to methods for the treatment of neuroblastoma by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is WEE1-1 or a pharmaceutically acceptable salt thereof, or WEE1-2 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is CHK1-1 or a pharmaceutically acceptable salt thereof. In another embodiment, the invention relates to a method for treating a neuroblastoma patient, comprising administering a WEE1 inhibitor and a CHK1 inhibitor, wherein the cancer cells of said patient to be treated are characterized by amplified expression levels of MYCN.
COMPOSITIONS AND METHODS FOR TREATING CANCER
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Page/Page column 30, (2013/03/28)
The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach - Part 1
Dwyer, Michael P.,Paruch, Kamil,Labroli, Marc,Alvarez, Carmen,Keertikar, Kerry M.,Poker, Cory,Rossman, Randall,Fischmann, Thierry O.,Duca, Jose S.,Madison, Vincent,Parry, David,Davis, Nicole,Seghezzi, Wolfgang,Wiswell, Derek,Guzi, Timothy J.
scheme or table, p. 471 - 474 (2011/02/26)
The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a] pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such as compound 17r. In the Letter, the further utility of the pyrazolo[1,5-a]pyrimidine template fo
SYNTHESIS OF SUBSTITUTED-3-AMINOPYRAZOLES
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Page/Page column 30-31, (2009/01/24)
The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1'H-4,4'-bispyrazole.
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors
Frey, Robin R.,Curtin, Michael L.,Albert, Daniel H.,Glaser, Keith B.,Pease, Lori J.,Soni, Niru B.,Bouska, Jennifer J.,Reuter, David,Stewart, Kent D.,Marcotte, Patrick,Bukofzer, Gail,Li, Junling,Davidsen, Steven K.,Michaelides, Michael R.
experimental part, p. 3777 - 3787 (2009/04/07)
7-Aminopyrazolo[1,5-a]pyrimidine urea receptor tyrosine kinase inhibitors have been discovered. Investigation of structure-activity relationships of the pyrazolo[1,5-a]pyrimidine nucleus led to a series of 6-(4-N,N′-diphenyl) ureas that potently inhibited
