537705-06-9Relevant academic research and scientific papers
1,2-DITHIOLANE AND DITHIOL COMPOUNDS USEFUL IN TREATING MUTANT EGFR-MEDIATED DISEASES AND CONDITIONS
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, (2018/08/09)
Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.
Design, synthesis and biological evaluation of lapatinib derivatives as HER1/HER2 inhibitors
Lyu, Aifeng,Fang, Lei,Gou, Shaohua,Liu, Xia
, p. 574 - 584 (2016/03/22)
Five Lapatinib derivatives were designed by structurally modifying the side chain as well as the aniline substituent. The ELISA assay showed that the derivatives retained or even improved the inhibitory activity of Lapatinib against HER1/HER2. In vitro cy
PHOSPHORUS CONTAINING QUINAZOLINE COMPOUNDS AND METHODS OF USE
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, (2011/02/24)
Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.
NOVEL PYRIMIDINE DERIVATIVE FOR INHIBITING THE GROWTH OF CANCER CELLS
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Page/Page column 31, (2011/09/15)
The present invention provides a novel pyrimidine derivative or pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising same, which can effectively inhibit the growth of cancer cells induced by the overexpression of EGFR incl
Highly functionalised sulfur-based silica scavengers for the efficient removal of palladium species from active pharmaceutical ingredients
Galaffu, Nicola,Man, Siud Pui,Wilkes, Robin D.,Wilson, John R. H.
, p. 406 - 413 (2012/12/31)
The use of multidentate sulfur-based silica scavengers 1,2, and 3 as highly effective adsorbents for the removal of precious metals, specifically palladium residues in this paper, from highly functionalised synthetic intermediates and APIs is described. The synthesis and purification of the polar and electron-rich reaction products, containing multiple functional groups, from palladium-catalysed removals of commonly used protecting groups such as benzyl, benzyloxycarbonyl, and allyloxycarbonyl and Sonogashira, Suzuki, Heck, and Buchwald-Hartwig coupling reactions is reported. The significant levels of residual palladium species, typically associated with these reaction products, are successfully and rapidly removed to below acceptable regulatory levels, of less than 5 ppm, by simple, unoptimised treatment with the designed silica scavengers at room temperature. Performance aspects, including broad solvent compatibility, excellent stability, and high metal affinity, combined with large-scale availability, ease of handling, and minimal loss of API make these silica scavengers particularly useful to process development groups.
PYRAZOLOPYRIMIDINE COMPOUNDS AS ANTITUMOR AGENTS
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Page/Page column 100-101, (2010/11/08)
The invention concerns compounds of the formula (I) wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.
Evaluation of kilogram-scale Sonagashira, Suzuki, and Heck coupling routes to oncology candidate CP-724,714
Ripin, David H. Brown,Bourassa, Dennis E.,Brandt, Thomas,Castaldi, Michael J.,Frost, Heather N.,Hawkins, Joel,Johnson, Phillip J.,Massett, Stephen S.,Neumann, Karin,Phillips, James,Raggon, Jeffery W.,Rose, Peter R.,Rutherford, Jennifer L.,Sitter, Barbara,Stewart III, A. Morgan,Vetelino, Michael G.,Wei, Lulin
, p. 440 - 450 (2012/12/25)
The synthesis of the anti-cancer compound 2-methoxy-N-(3-{4-[3-methyl-4-(6- methyl-pyridin-3-yloxy)phenylamino]quinazolin-6-yl}-E-allyl)acetainide (CP-724,714) (1) on multikilogram scale using several different synthetic routes is described. Application of the Sonogashira, Suzuki, and Heck couplings to this synthesis was investigated to identify a safe, environmentally friendly, and robust process for the production of this drug candidate. A convergent and selective synthesis of the candidate was identified which utilizes a Heck coupling of a protected allylamine to install the critical olefin.
SUBSTITUTED TETRAHYDROBENZOTHIENOPYRIMIDINAMINE COMPOUNDS USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS
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Page/Page column 119-120, (2010/02/10)
The present invention relates to a compound of Formula (I) and its use in treating hyper-proliferative disorders.
QUINAZOLINE DERIVATIVES
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Page/Page column 235-237, (2008/06/13)
A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.
QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS
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Page/Page column 148, (2008/06/13)
A quinazoline derivative of the formula (I): (A chemical formula should be inserted here - please see paper copy enclosed) Formula I wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.
