Patents by Inventor Margaret Grapperhaus

Margaret Grapperhaus has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20200079785
    Abstract: The present invention provides MMC prodrug compounds and liposomal MMC prodrugs and compositions thereof for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid and a MMC prodrug. The present invention also provides liposomal compositions for the treatment of cancer comprising administering to a patient in need thereof a liposome, wherein the liposome comprises: a phosphatidylcholine lipid; a sterol; a PEG-lipid and a MMC prodrug or a pharmaceutically-acceptable salt thereof.
    Type: Application
    Filed: November 8, 2017
    Publication date: March 12, 2020
    Applicant: Mallinckrodt LLC
    Inventors: William McGHEE, Michelle SCHMIDT, Margaret GRAPPERHAUS, Kah Tiong KUAN
  • Publication number: 20160250177
    Abstract: The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and a taxane. The PEG-lipid constitutes from about 2 to about 8 mol % of the lipids in the liposome. The taxane is docetaxel esterified at the 2?-O position with a heterocyclyl-(C2-5 alkanoic acid). The present invention also provides liposomal compositions for the treatment of cancer comprising administering to a patient in need thereof a liposome, wherein the liposome comprises: a phosphatidylcholine lipid; a sterol; a PEG-lipid; and a taxane or a pharmaceutically acceptable salt thereof; wherein the taxane is docetaxel esterified at the 2?-O-position with a heterocyclyl-(C2-5alkanoic acid); and wherein upon administration of the liposomal composition to the patient, the plasma concentration of docetaxel remain above an efficacy threshold of 0.2 ?M for at least 5 hours.
    Type: Application
    Filed: February 17, 2016
    Publication date: September 1, 2016
    Inventors: WILLIAM McGHEE, JAMES BLACKLEDGE, MARGARET GRAPPERHAUS, LOUISE ROCHON, KRISHNA DEVARAKONDA
  • Publication number: 20140271822
    Abstract: The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and a taxane. The PEG-lipid constitutes from about 2 to about 8 mol % of the lipids in the liposome. The taxane is docetaxel esterified at the 2?-O position with a heterocyclyl-(C2-5alkanoic acid). Methods for preparation of liposomal taxanes and treatment of cancer with liposomal taxanes are also disclosed.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Mallinckrodt LLC
    Inventors: William McGhee, James Blackledge, Margaret Grapperhaus
  • Publication number: 20070219274
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Application
    Filed: March 29, 2007
    Publication date: September 20, 2007
    Inventors: James Sikorski, Richard Durley, Margaret Grapperhaus, Mark Massa, Emily Reinhard, Yvette Fobian, Michael Tollefson, Lijuan Wang, Brian Hickory, Monica Norton, William Vernier, Deborah Mischke, Michelle Promo, Ashton Hamme, Dale Spangler, Melvin Rueppel
  • Publication number: 20060229304
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Application
    Filed: March 9, 2006
    Publication date: October 12, 2006
    Inventors: James Sikorski, Richard Durley, Margaret Grapperhaus, Mark Massa, Emily Reinhard, Yvette Fobian, Michael Tollefson, Lijuan Wang, Brian Hickory, Monica Norton, William Vernier, Deborah Mischke, Michele Promo, Ashton Hamme, Dale Spangler, Melvin Rueppel
  • Publication number: 20060074243
    Abstract: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. These compounds generally correspond in structure to Formula I: wherein A1, A2, A3, E1, E2, E3, and E4 are as defined in this patent. This invention also is directed to compositions of such compounds, intermediates for the syntheses of such compounds, methods for making such compounds, and methods for treating conditions associated with MMP activity and/or aggrecanase activity, particularly pathological conditions.
    Type: Application
    Filed: November 10, 2005
    Publication date: April 6, 2006
    Inventors: Daniel Becker, Yiyuan Chen, John Freskos, Alan Gasiecki, Margaret Grapperhaus, Donald Hansen, Robert Heintz, Darren Kassab, Ish Khanna, Stephen Kolodziej, Sergio Mantegani, Mark Massa, Joseph McDonald, Deborah Mischke, Mark Nagy, Ettore Perrone, Joseph Rico, Michelle Schmidt, Dale Spangler, John Talley, Mahima Trivedi, Thomas Wynn
  • Patent number: 6951889
    Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 15, 2001
    Date of Patent: October 4, 2005
    Assignee: Pharmacia Corporation
    Inventors: Donald W. Hansen, Jr., Ronald Keith Webber, Barnett S. Pitzele, James Sikorski, Mark A. Massa, Timothy J. Hagen, Margaret Grapperhaus, Lijuan Jane Wang, Arija A. Bergmanis, Steven W. Kramer, E. Ann Hallinan
  • Publication number: 20050209278
    Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
    Type: Application
    Filed: November 3, 2003
    Publication date: September 22, 2005
    Inventors: Joseph McDonald, Darren Kassab, Mark Massa, Margaret Grapperhaus, Michelle Schmidt, Joseph Rico, Patrick Mullins, David Brown
  • Publication number: 20050113451
    Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Application
    Filed: November 1, 2004
    Publication date: May 26, 2005
    Applicant: Pharmacia Corporation
    Inventors: Donald Hansen, Ronald Webber, Barnett Pitzele, James Sikorski, Mark Massa, Timothy Hagen, Margaret Grapperhaus, Lijuan Wang, Arija Bergmanis, Steven Kramer, E. Hallinan
  • Publication number: 20050043294
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Application
    Filed: August 27, 2004
    Publication date: February 24, 2005
    Inventors: James Sikorski, Richard Durley, Margaret Grapperhaus, Mark Massa, Emily Reinhard, Yvette Fobian, Michael Tollefson, Lijuan Wang, Brian Hickory, Monica Norton, William Vernier, Deborah Mischke, Michele Promo, Ashton Hamme, Dale Spangler, Melvin Rueppel
  • Publication number: 20050009838
    Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
    Type: Application
    Filed: April 25, 2003
    Publication date: January 13, 2005
    Inventors: Thomas Barta, Daniel Becker, Louis Bedell, Terri Boehm, David Brown, Jeffery Carroll, Yiyuan Chen, Yvette Fobian, John Freskos, Alan Gasiecki, Margaret Grapperhaus, Robert Heintz, Susan Hockerman, Darren Kassab, Ish Khanna, Stephen Kolodziej, Mark Massa, Joseph McDonald, Brent Mischke, Deborah Mischke, Patrick Mullins, Mark Nagy, Monica Norton, Joseph Rico, Michelle Schmidt, Nathan Stehle, John Talley, William Vernier, Clara Villamil, Lijuan Wang, Thomas Wynn
  • Publication number: 20020132849
    Abstract: The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Application
    Filed: September 15, 2001
    Publication date: September 19, 2002
    Inventors: Donald W. Hansen, Ronald Keith Webber, Barnett S. Pitzele, James Sikorski, Mark A. Massa, Timothy J. Hagen, Margaret Grapperhaus, Lijuan Jane Wang, Arija A. Bergmanis, Steven W. Kramer, E. Ann Hallinan