Patents Assigned to OSI Pharmaceuticals, LLC
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Patent number: 11833149Abstract: A novel dosing regimen for erlotinib or a pharmaceutically acceptable salt thereof is described herein. The dosing regimen demonstrates impressive control of central nervous system disease, which is better than that reported with standard dose erlotinib. The use of the novel dosing regimen for treating patients in need thereof, including for controlling formation of metastatic brain, leptomeninges, or CNS lesions in a patient with non-small cell lung cancer (NSCLC) that harbors epidermal growth factor receptor (EGFR) mutation with or without pre-existing brain metastases, is also described herein.Type: GrantFiled: January 10, 2022Date of Patent: December 5, 2023Assignee: OSI Pharmaceuticals, LLCInventors: Stanley C. Gill, Kenneth K. Iwata, Gregory J. Riely, Jun Wu, Helena Yu
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Patent number: 11253520Abstract: A novel dosing regimen for erlotinib or a pharmaceutically acceptable salt thereof is described herein. The dosing regimen demonstrates impressive control of central nervous system disease, which is better than that reported with standard dose erlotinib. The use of the novel dosing regimen for treating patients in need thereof, including for controlling formation of metastatic brain, leptomeninges, or CNS lesions in a patient with non-small cell lung cancer (NSCLC) that harbors epidermal growth factor receptor (EGFR) mutation with or without pre-existing brain metastases, is also described herein.Type: GrantFiled: January 24, 2020Date of Patent: February 22, 2022Assignee: OSI Pharmaceuticals, LLCInventors: Stanley C. Gill, Kenneth K. Iwata, Gregory J. Riely, Jun Wu, Helena Yu
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Patent number: 10583142Abstract: A novel dosing regimen for erlotinib or a pharmaceutically acceptable salt thereof is described herein. The dosing regimen demonstrates impressive control of central nervous system disease, which is better than that reported with standard dose erlotinib. The use of the novel dosing regimen for treating patients in need thereof, including for controlling formation of metastatic brain, leptomeninges, or CNS lesions in a patient with non-small cell lung cancer (NSCLC) that harbors epidermal growth factor receptor (EGFR) mutation with or without pre-existing brain metastases, is also described herein.Type: GrantFiled: March 25, 2016Date of Patent: March 10, 2020Assignee: OSI Pharmaceuticals, LLCInventors: Stanley C. Gill, Kenneth K. Iwata, Gregory J. Riely, Jun Wu, Helena Yu
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Patent number: 9896730Abstract: 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: GrantFiled: April 25, 2012Date of Patent: February 20, 2018Assignees: OSI Pharmaceuticals, LLC, AVEO PHARMACEUTICALS, INC.Inventors: 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: 9371298Abstract: Processes and intermediates for the preparation of compounds of the Formula I and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R1, R2, and R3 have the definitions provided herein.Type: GrantFiled: November 10, 2014Date of Patent: June 21, 2016Assignees: Pfizer Inc., OSI Pharmaceuticals, LLCInventors: David B. Damon, Brian P. Jones
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Patent number: 9351974Abstract: 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.Type: GrantFiled: November 12, 2012Date of Patent: May 31, 2016Assignee: OSI Pharmaceuticals, LLCInventors: Meizhong Jin, Mridula Kadalbajoo, An-Hu Li, Mark J. Mulvihill, Kam W. Siu, Arno G. Steinig, Jing Wang
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Patent number: 9244058Abstract: 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: December 12, 2011Date of Patent: January 26, 2016Assignee: OSI Pharmaceuticals, LLCInventors: John D. Haley, Graeme Griffin, Lukas A. Amler, David A. Eberhard, Robert L. Yauch
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Patent number: 9133224Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.Type: GrantFiled: November 29, 2011Date of Patent: September 15, 2015Assignee: OSI Pharmaceuticals, LLCInventors: Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Dan Sherman, Kam W. Siu
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Patent number: 9096624Abstract: 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: January 25, 2013Date of Patent: August 4, 2015Assignee: 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: 8796455Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: GrantFiled: February 15, 2013Date of Patent: August 5, 2014Assignee: 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, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
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Patent number: 8735405Abstract: 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: April 13, 2012Date of Patent: May 27, 2014Assignee: OSI Pharmaceuticals, LLCInventors: Lee D. Arnold, Cara Cesario, Heather Coate, Andrew P. Crew, Hanqing Dong, Kenneth Foreman, Ayako Honda, Radoslaw Laufer, An-Hu Li, Kristen Michelle Mulvihill, Mark J. Mulvihill, Anthony I. Nigro, Bijoy Panicker, Arno G. Steinig, Yingchuan Sun, Quinghua Weng, Douglas S. Werner, Michael J. Wyle, Tao Zhang
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Patent number: 8653268Abstract: 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: January 11, 2013Date of Patent: February 18, 2014Assignee: OSI Pharmaceuticals, LLCInventors: Mark J. Mulvihill, Radoslaw Laufer, An-Hu Li, Arno G. Steinig
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Patent number: 8642834Abstract: 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 CFPAC-1, 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: February 4, 2014Assignee: OSI Pharmaceuticals, LLCInventors: Julie Kan, Salam A. Shaaban, Joseph S. Krueger, Maryland Franklin, Robert C. Wild
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Patent number: 8592448Abstract: Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.Type: GrantFiled: November 19, 2009Date of Patent: November 26, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Xin Chen, Melzhong Jin, Andrew Kleinberg, An-Hu Li, Mark J. Mulvihill, Arno G. Steinig, Jing Wang
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Patent number: 8586546Abstract: The present invention 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. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HC1 (also known as TARCEVA®).Type: GrantFiled: February 10, 2012Date of Patent: November 19, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Elizabeth A. Buck, Graeme Griffin, Sharon M. Barr
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Patent number: 8575164Abstract: Methods and compositions for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially (a) a therapeutically effective amount of an anti-cancer agent and (b) an IGF1R inhibitor compound of Formula I, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. Suitable IGF1R inhibitor may be represented by Formula I: wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein.Type: GrantFiled: February 25, 2008Date of Patent: November 5, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Lee D. Arnold, Qun-Sheng Ji, Elizabeth Buck, John D. Haley, Mark J. Mulvihill
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Patent number: 8557814Abstract: Salt forms of mTOR inhibitors of the Formula (I): and methods of preparation, formulation, and use in treating disease.Type: GrantFiled: March 18, 2009Date of Patent: October 15, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Arlindo L. Castelhano, Kristen Michelle Mulvihill, Gary C. Visor
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Publication number: 20130261086Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.Type: ApplicationFiled: November 29, 2011Publication date: October 3, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Dan Sherman, Kam W. Siu
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Publication number: 20130261306Abstract: 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: ApplicationFiled: May 23, 2013Publication date: October 3, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Yunyu Mao, Kristen Michelle Mulvihill, Josef A. Rechka, Paula A. Tavares-Greco
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Publication number: 20130253197Abstract: 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: ApplicationFiled: April 30, 2013Publication date: September 26, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Mark J. Mulvihill, Arno G. Steinig, Andrew Philip Crew, Meizhong Jin, Andrew Kleinberg, An-Hu Li, Jing Wang