Patents Assigned to OSI Pharmaceuticals, Inc.
  • Publication number: 20110136764
    Abstract: 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: Application
    Filed: June 1, 2010
    Publication date: June 9, 2011
    Applicant: OSI Pharmaceuticals, Inc.
    Inventors: Rama Devi APPARI, Xin CHEN, Ramesh Chllukuri, Andrew P. CREW, Hanqing DONG, Caterina FERRARO, Kenneth FOREMAN, Ramesh C. GUPTA, An-Hu LI, Dan SHERMAN, Kathryn M. STOLZ, Brian VOLK, Robert ZAHLER
  • Patent number: 7951549
    Abstract: 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 H358, 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: Grant
    Filed: March 6, 2009
    Date of Patent: May 31, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: John D. Haley, Stuart Thomson, Julie Kan, Salam A. Shaaban
  • Patent number: 7943767
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: May 17, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: 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, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
  • Patent number: 7939272
    Abstract: 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: Grant
    Filed: September 29, 2008
    Date of Patent: May 10, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventor: Elizabeth A. Buck
  • Patent number: 7923555
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: April 12, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Hanqing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
  • Patent number: 7879566
    Abstract: This invention relates to the identification of LPA as a ligand for the G-protein coupled receptors OSGPR114 and OSGPR78. The invention is directed to new methods for screening candidate drugs for their ability to modulate the activity of OSGPR114 or OSGPR78, and new pharmaceutical agents identified by these methods. It is also directed to the use of such agents in the manufacture of medicaments for the treatment of OSGPR114 or OSGPR78 mediated diseases, and methods of treating diseases such as cancers by administering to an individual a therapeutic amount of a modulator of OSGPR114 or OSGPR78 identified by these methods.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: February 1, 2011
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Graeme Griffin, Lambertus J. Oehlen
  • Publication number: 20110015197
    Abstract: Salt forms of mTOR inhibitors of the Formula (I): and methods of preparation, formulation, and use in treating disease.
    Type: Application
    Filed: March 18, 2009
    Publication date: January 20, 2011
    Applicant: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Kristen Michelle Mulvihill, Josef A. Rechka, Gary C. Visor
  • Publication number: 20100286155
    Abstract: A method of treating adrenocortical carcinoma with OSI-906.
    Type: Application
    Filed: May 7, 2010
    Publication date: November 11, 2010
    Applicant: OSI PHARMACEUTICALS, INC.
    Inventors: Elizabeth A. BUCK, Andrew W. STEPHENS
  • Patent number: 7829717
    Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R5, m and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.
    Type: Grant
    Filed: September 15, 2005
    Date of Patent: November 9, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Andrew Crew, Hanqing Dong, An-Hu Li, Li Qiu, Alun Smith, Lawrence Tardibono, Tao Zhang
  • Patent number: 7820662
    Abstract: 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: Grant
    Filed: October 3, 2008
    Date of Patent: October 26, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: 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, Arno G. Steinig, Yingchuan Sun, Quinghua Weng, Douglas S. Werner, Michael J. Wyle, Tao Zhang
  • Patent number: 7816325
    Abstract: The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: October 19, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Kerstin Kühn-Wache, Joachim Bär, Hans-Ulrich Demuth, Torsten Hoffmann, Ulrich Heiser, Wolfgang Brandt
  • Patent number: 7790902
    Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
    Type: Grant
    Filed: July 29, 2008
    Date of Patent: September 7, 2010
    Assignees: Pfizer, Inc., OSI Pharmaceuticals, Inc.
    Inventors: Eric R. Larson, Mark C. Noe, Thomas G. Gant
  • Patent number: 7767673
    Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: August 3, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Andrew P. Crew, Han-Qing Dong, Radoslaw Laufer, An-Hu Li, Li Qiu, Colin Peter Sambrook Smith, Tao Zhang
  • Patent number: 7741324
    Abstract: Compounds of the formula and pharmaceuticaly acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: June 22, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Andrew Philip Crew, Mark Joseph Mulvihill, Douglas Scott Werner
  • Patent number: 7700594
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: April 20, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: 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, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
  • Patent number: 7696225
    Abstract: Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: April 13, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Jason Bloxham, Andrew Phillip Crew, Ayako Honda, An-Hu Li, Bijoy Panicker, Graham Michael Wynne, Lawrence Tardibono, Jr.
  • Patent number: 7662844
    Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G1, Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: February 16, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Vanessa Smith, Anthony Nigro, Mark Mulvihill, Cara Cesario, Patricia Anne Beck, Arlindo L. Castelhano
  • Patent number: 7659274
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: January 24, 2007
    Date of Patent: February 9, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Andrew Philip Crew, Douglas S. Werner, Paula A. R. Tavares
  • Patent number: 7651687
    Abstract: 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: Grant
    Filed: March 13, 2007
    Date of Patent: January 26, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Elizabeth A. Buck, Graeme Griffin, Sharon M. Barr
  • Patent number: 7648987
    Abstract: Compounds of the Formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit protein kinase enzymes 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: Grant
    Filed: December 4, 2006
    Date of Patent: January 19, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Andrew Philip Crew, Han-Qing Dong, Mark Joseph Mulvihill, Douglas S. Werner, Mridula Kadalbajoo, Radoslaw Laufer