Patents Assigned to OSI Pharmaceuticals, LLC
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Publication number: 20130231306Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.Type: ApplicationFiled: January 25, 2013Publication date: September 5, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Andrew P. CREW, Dan Sherman, Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Kathryn M. Stolz, Brian Volk, Robert Zahler
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Patent number: 8513415Abstract: 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.Type: GrantFiled: April 19, 2010Date of Patent: August 20, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Yunyu Mao, Josef A. Rechka, Paula A. Tavares-Greco
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Patent number: 8481733Abstract: Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.Type: GrantFiled: May 19, 2009Date of Patent: July 9, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Andrew P. Crew, Meizhong Jin, Mridula Kadalbajoo, Andrew Kleinberg, Mark J. Mulvihill, Jing Wang
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Patent number: 8465912Abstract: 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.Type: GrantFiled: February 26, 2010Date of Patent: June 18, 2013Assignee: OSI Pharmaceuticals, LLCInventor: Julie Kan
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Publication number: 20130137975Abstract: A method for determining whether to administer a therapeutically effective amount of a receptor tyrosine kinase-inhibiting drug for tumor treatment, by determining a glucose uptake response in the tumor of a mammal. 18FDG-PET (2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography imaging) is used as a predictive, non-invasive, pharmacodynamic biomarker of response following administration of drug.Type: ApplicationFiled: February 9, 2011Publication date: May 30, 2013Applicant: OSI PHARMACEUTICALS, LLCInventors: Joseph E. Bugaj, Henry C. Manning, Eliot T. McKinley, Robert C. Wild
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Patent number: 8445510Abstract: 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 at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.Type: GrantFiled: May 16, 2011Date of Patent: May 21, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Mark J. Mulvihill, Arno G. Steinig, Andrew Philip Crew, Meizhong Jin, Andrew Kleinberg, An-Hu Li, Jing Wang
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Patent number: 8399433Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.Type: GrantFiled: June 1, 2010Date of Patent: March 19, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Dan Sherman, Kathryn M. Stolz, Brian Volk, Robert Zahler
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Patent number: 8388957Abstract: The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R 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 IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate the above methodology are also provided.Type: GrantFiled: November 11, 2011Date of Patent: March 5, 2013Assignee: OSI Pharmaceuticals, LLCInventor: John D. Haley
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Patent number: 8383357Abstract: 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.Type: GrantFiled: April 13, 2007Date of Patent: February 26, 2013Assignee: OSI Pharmaceuticals, LLCInventors: John D. Haley, Stuart Thomson, Filippo Petti
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Patent number: 8378104Abstract: Compounds of Formula 1, 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 at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.Type: GrantFiled: February 11, 2011Date of Patent: February 19, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
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Patent number: 8377636Abstract: The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase. Based on the surprising discovery that tumors cells after having undergone an EMT, while being mesenchymal-like, still express characteristics of both epithelial and mesenchymal cells, and that such cells have altered sensitivity to inhibition by receptor protein-tyrosine kinase inhibitors, in that they have become relatively insensitive to EGFR kinase inhibitors, but have frequently acquired sensitivity to inhibitors of other receptor protein-tyrosine kinases such as PDGFR or FGFR, methods have been devised for determining levels of specific epithelial and mesenchymal biomarkers that identify such “hybrid” tumor cells (e.g. determination of co-expression of vimentin and epithelial keratins), and thus predict the tumor's likely sensitivity to inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase.Type: GrantFiled: April 14, 2008Date of Patent: February 19, 2013Assignee: OSI Pharmaceuticals, LLCInventors: John D. Haley, Stuart Thompson
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Patent number: 8367826Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.Type: GrantFiled: December 1, 2011Date of Patent: February 5, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Radoslaw Laufer, An-Hu Li, Mark J. Mulvihill, Arno G. Steinig
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Publication number: 20120302572Abstract: 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.Type: ApplicationFiled: April 25, 2012Publication date: November 29, 2012Applicants: AVEO PHARMACEUTICALS, INC., OSI Pharmaceuticals, LLCInventors: Julie Kan, Stuart Thomson, Gretchen M. Argast, Matthew E. O'Connor, Murray Robinson, Bin Feng, Joerg Heyer, Maria I. Chiu, Richard Nicoletti
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Patent number: 8314111Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: GrantFiled: May 13, 2011Date of Patent: November 20, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
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Publication number: 20120128670Abstract: Cancer therapy comprising treatment with an mTOR inhibitor, such as a dual mTORC1/mTORC2 inhibitor, such as OSI-027, in combination with an angiogenesis inhibitor.Type: ApplicationFiled: July 30, 2010Publication date: May 24, 2012Applicant: OSI PHARMACEUTICALS, LLCInventors: Sharon M. Barr, Prafulla C. Gokhale, Robert C. Wild
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Patent number: 8178668Abstract: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.Type: GrantFiled: February 4, 2009Date of Patent: May 15, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Arno G. Steinig, Mark J. Mulvihill, Jing Wang, Douglas S. Werner, Qinghua Weng, Heather Coate, Xin Chen
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Patent number: 8114846Abstract: The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases.Type: GrantFiled: December 4, 2009Date of Patent: February 14, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Elizabeth A. Buck, Graeme Griffin, Sharon Barr
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Patent number: 8101613Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.Type: GrantFiled: August 12, 2009Date of Patent: January 24, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Lee D. Arnold, Cara Cesario, Heather Coate, Andrew Philip Crew, Hanqing Dong, Kenneth Foreman, Ayako Honda, Radoslaw Laufer, An-Hu Li, Kristen Michelle Mulvihill, Mark J. Mulvihill, Anthony I. Nigro, Bijoy Panicker, Amo G. Steinig, Yingchuan Sun, Qinghua Weng, Douglas S. Werner, Michael J. Wyle, Tao Zhang
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Patent number: 8062838Abstract: The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R 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 IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R 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 IGF-1R kinase inhibitors.Type: GrantFiled: September 19, 2006Date of Patent: November 22, 2011Assignee: OSI Pharmaceuticals, LLCInventor: John D. Haley
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Patent number: 8048621Abstract: The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R 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 IGF-1R kinase inhibitors. Improved methods for treating cancer patients with IGF-1R 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 IGF-1R kinase inhibitors.Type: GrantFiled: September 29, 2008Date of Patent: November 1, 2011Assignee: OSI Pharmaceuticals, LLCInventors: John D. Haley, Elizabeth A. Buck