Farmingdale, NY, United States
Farmingdale, NY, United States

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Patent
AVEO Pharmaceuticals and OSI Pharmaceuticals Inc. | Date: 2012-04-25

The present invention provides diagnostic methods for assessing the EMT status of tumor cells, and for predicting the effectiveness of treatment of a cancer patient with an EGFR or IGF-1R kinase inhibitor, utilizing an EMT gene signature index score. The present invention further provides methods for treating patients with cancer that incorporate these methods.


Patent
OSI Pharmaceuticals Inc. | Date: 2013-01-25

Compounds of Formula 1, as shown below and defined herein:


Patent
OSI Pharmaceuticals Inc. | Date: 2012-11-12

Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.


Patent
Pfizer and OSI Pharmaceuticals Inc. | Date: 2014-11-10

Processes and intermediates for the preparation of compounds of the Formula I and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R^(1), R^(2), and R^(3 )have the definitions provided herein.


The invention provides a compound comprising N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, or a pharmaceutically acceptable salt thereof in anhydrous or hydrate form for use in the treatment of NSCLC (non small cell lung cancer).


Patent
OSI Pharmaceuticals Inc. and Pfizer | Date: 2016-12-14

The invention relates to a pharmaceutical combination and a composition for use as a medicament for treating hyperproliferative diseases comprising a combination of [6,7-Bis- (2-methoxyethoxy)quinazolin-4-yl-(3-ethynylphenyl)amine], or a pharmaceutically acceptable salt thereof, and one or more additional antitumor substances.


Patent
OSI Pharmaceuticals Inc. | Date: 2013-05-23

A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.


Patent
OSI Pharmaceuticals Inc. | Date: 2013-04-30

Compounds of Formula I, as shown below and defined herein:


The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an EGFR kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an EGFR kinase inhibitor, comprising assessing whether the tumor cell has undergone an epithelial to mesenchymal transition (EMT), by determining the expression level of epithelial and/or mesenchymal biomarkers, wherein tumor cells that have undergone an EMT are substantially less sensitive to inhibition by EGFR kinase inhibitors. Improved methods for treating cancer patients with EGFR kinase inhibitors that incorporate the above methodology are also provided. Additionally, methods are provided for the identification of new biomarkers that are predictive of responsiveness of tumors to EGFR kinase inhibitors. Furthermore, methods for the identification of agents that restore the sensitivity of tumor cells that have undergone EMT to inhibition by EGFR kinase inhibitors are also provided.


The present invention provides tumor cell preparations for use as models of the EMT process for use in the identification of anti-cancer agents, wherein said tumor cell preparations comprise cells of the epithelial tumor cell line H1650, which are stimulated by receptor ligands to induce EMT, or which have been engineered to inducibly express a protein that stimulates EMT. The present invention also provides methods of identifying potential anti-cancer agents by using such tumor cell preparations to identify agents that inhibit EMT, stimulate MET, or inhibit the growth of mesenchymal-like cells. Such agents should be particularly useful when used in conjunction with other anti-cancer drugs such as EGFR and IGF-1R kinase inhibitors, which appear to be less effective at inhibiting tumor cells that have undergone an EMT.

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