Patents by Inventor David B. Rozema

David B. Rozema 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).

  • Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA
    Patent number: 9249179
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinetic modulator targeting moiety targeted RNAi polynucleotides can be administered in vivo alone or together with co-targeted delivery polymers.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: February 2, 2016
    Assignee: Arrowhead Madison Inc.
    Inventors: Philipp Hadwiger, Torsten Hoffmann, Eric A. Kitas, Peter Mohr, Ingo Roehl, Linda Valis, David B. Rozema, David L. Lewis, Darren H. Wakefield
  • Peptide-Based In Vivo siRNA Delivery System
    Publication number: 20150352221
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
    Type: Application
    Filed: July 1, 2015
    Publication date: December 10, 2015
    Inventors: David B Rozema, Darren H Wakefield
  • Small molecule conjugates for intracellular delivery of nucleic acids
    Patent number: 9198947
    Abstract: The invention provides use of novel compounds for delivery of nucleic acids, and conjugates of these compounds with nucleic acids. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to said compounds and co-administered with a delivery polymer to achieve mRNA knock down in vivo are disclosed therein.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: December 1, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Philipp Hadwiger, Torsten Hoffmann, Kerstin Jahn-Hofmann, Eric A. Kitas, David L. Lewis, Peter Mohr, Hans Martin Mueller, Guenther Ott, Ingo Roehl, David B. Rozema
  • Reversibly Masked Polymers
    Publication number: 20150273081
    Abstract: The present invention is directed to reversibly inactivated membrane active polymers useful for cellular delivery of compounds. Described are polyconjugate systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery conjugates. The use of multiple reversible linkages connecting component parts provides for physiologically responsive activity modulation.
    Type: Application
    Filed: January 12, 2015
    Publication date: October 1, 2015
    Inventors: David B Rozema, Jon A Wolff, James E Hagstrom, Kirk Ekena
  • Peptide-based in vivo siRNA delivery system
    Patent number: 9107957
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
    Type: Grant
    Filed: June 25, 2013
    Date of Patent: August 18, 2015
    Assignee: Arrowhead Madison Inc.
    Inventors: David B Rozema, David L Lewis, Darren Wakefield, Eric Kitas, Philipp Hadwiger, Jon Wolff, Ingo Röhl, Peter Mohr, Torsten Hoffmann, Kerstin Jahn-Hofmann, Hans Martin Mueller, Günther Ott, Andrei V Blokhin, Jonathan D Benson, Jeffrey C Carlson
  • Compositions for Targeted Delivery of siRNA
    Publication number: 20150202298
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.
    Type: Application
    Filed: March 18, 2015
    Publication date: July 23, 2015
    Inventors: David L. Lewis, David B. Rozema, Darren H. Wakefield
  • Compositions for targeted delivery of siRNA
    Patent number: 9011919
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 21, 2015
    Assignee: Arrowhead Madison Inc.
    Inventors: David B. Rozema, David L. Lewis, Darren H. Wakefield, Torsten Hoffmann, Eric Kitas, Peter Mohr, Philipp Hadwiger, Wilma Thuer, Linda Valis
  • Poly(acrylate) Polymers for In Vivo Nucleic Acid Delivery
    Publication number: 20150104408
    Abstract: The present invention is directed membrane active poly(acrylate) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides cells in vivo. RNAi polynucleotides are conjugated to the poly(acrylate) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(acrylate) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.
    Type: Application
    Filed: November 25, 2014
    Publication date: April 16, 2015
    Applicant: ARROWHEAD MADISON INC.
    Inventors: Darren H. Wakefield, Nicholas A. Rossi, David B. Rozema, Lauren J. Almeida, Anthony L. Perillo-Nicholas
  • Polyconjugates for Delivery of RNAi triggers to Tumor Cells In Vivo
    Publication number: 20150045573
    Abstract: The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand-targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.
    Type: Application
    Filed: August 6, 2014
    Publication date: February 12, 2015
    Inventors: Weijun Cheng, So Wong, Aaron M. Almeida, David B. Rozema, Andrei V. Blokhin, Jeffrey C. Carlson
  • Poly(acrylate) polymers for in vivo nucleic acid delivery
    Patent number: 8933047
    Abstract: The present invention is directed membrane active poly(acrylate) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides cells in vivo. RNAi polynucleotides are conjugated to the poly(acrylate) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(acrylate) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: January 13, 2015
    Assignee: Arrowhead Madison Inc.
    Inventors: Darren H. Wakefield, David B. Rozema, Nicholas Rossi, Lauren Almeida, Anthony L. Perillo-Nicholas
  • In vivo polynucleotide delivery conjugates having enzyme sensitive linkages
    Patent number: 8802773
    Abstract: The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: August 12, 2014
    Assignee: Arrowhead Madison Inc.
    Inventors: David B Rozema, David L Lewis, Darren H Wakefield, Eric A Kitas, Philipp Hadwiger, Jon A Wolff, Ingo Roehl, Peter Mohr, Torsten Hoffmann, Kerstin Jahn-Hofmann, Hans Martin Mueller, Guenther Ott, Andrei V Blokhin, Jeffrey C Carlson, Jonathan D Benson
  • Small molecule conjugates for intracellular delivery of nucleic acids
    Publication number: 20140135380
    Abstract: The invention provides use of novel compounds for delivery of nucleic acids, and conjugates of these compounds with nucleic acids. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to said compounds and co-administered with a delivery polymer to achieve mRNA knock down in vivo are disclosed therein.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 15, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Philipp Hadwiger, Torsten Hoffmann, Kerstin Jahn-Hofmann, Eric A. Kitas, David L. Lewis, Peter Mohr, Hans Martin Mueller, Guenther Ott, Ingo Roehl, David B. Rozema
  • Small molecule conjugates for intracellular delivery of biologically active compounds
    Publication number: 20140135381
    Abstract: The invention provides novel compounds and conjugates of these compounds useful for the delivery of biologically active substances. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to a delivery polymer to achieve in vivo mRNA knock down are disclosed therein.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 15, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Philipp Hadwiger, Torsten Hoffmann, Kerstin Jahn-Hofmann, Eric A. Kitas, David L. Lewis, Peter Mohr, Hans Martin Mueller, Guenther Ott, Ingo Roehl, David B. Rozema
  • Disubstituted Maleic Anhydrides with Altered Kinetics of Ring Closure
    Publication number: 20140128584
    Abstract: We describe anhydride compounds suitable for physiologically labile modification of amine-containing molecules. The described anhydrides form reversible linkages having desirable kinetics for in vivo delivery of biologically active molecules. Also described are endosomolytic polymers formed by modification of membrane active polyamines with the described anhydrides.
    Type: Application
    Filed: May 31, 2012
    Publication date: May 8, 2014
    Applicant: ARROWHEAD MADISON INC.
    Inventors: Andrei V. Blokhin, David B. Rozema, Jonathan D. Benson, Jeffrey C. Carlson
  • Polyconjugates for in vivo delivery of polynucleotides
    Patent number: 8658211
    Abstract: The present invention is directed to compounds, compositions, and methods useful for delivering polynucleotides or other cell-impermeable molecules to mammalian cells. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery vehicles. The use of multiple reversible or labile linkages connecting component parts provides for physiologically responsive activity modulation.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: February 25, 2014
    Assignee: Arrowhead Madison Inc.
    Inventors: David B. Rozema, Darren H. Wakefield, David L. Lewis, Jason Klein, So Wong, Jon A. Wolff, James E. Hagstrom
  • Poly(acrylate) Polymers for In Vivo Nucleic Acid Delivery
    Publication number: 20130317079
    Abstract: The present invention is directed membrane active poly(acrylate) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides cells in vivo. RNAi polynucleotides are conjugated to the poly(acrylate) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(acrylate) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.
    Type: Application
    Filed: August 23, 2012
    Publication date: November 28, 2013
    Applicant: ARROWHEAD MADISON INC.
    Inventors: Darren H. Wakefield, David B. Rozema, Nicholas Rossi, Lauren Almeida, Anthony L. Perillo-Nicholas
  • Peptide-Based In Vivo siRNA Delivery System
    Publication number: 20130281658
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
    Type: Application
    Filed: June 25, 2013
    Publication date: October 24, 2013
    Inventors: David B Rozema, David L Lewis, Darren Wakefield, Eric Kitas, Philipp Hadwiger, Jon Wolff, Ingo Röhl, Peter Mohr, Torsten Hoffmann, Kerstin Jahn-Hofmann, Hans Martin Mueller, Günther Ott, Andrei V Blokhin, Jonathan D Benson, Jeffrey C Carlson
  • Compounds and methods for reversible modification of biologically active molecules
    Patent number: 8541548
    Abstract: The present invention is directed compounds for reversibly modification of biologically active molecules. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery conjugates. The use of reversible modification provides for physiologically responsive activity modulation.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: September 24, 2013
    Assignee: Arrowhead Madison Inc.
    Inventor: David B. Rozema
  • Compositions for Targeted Delivery of siRNA
    Publication number: 20130245091
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.
    Type: Application
    Filed: September 14, 2012
    Publication date: September 19, 2013
    Applicant: ARROWHEAD MADISON INC.
    Inventors: David B. Rozema, David L. Lewis, Darren H. Wakefield, Torsten Hoffmann, Eric A. Kitas, Peter Mohr, Philipp Hadwiger, Wilma Thuer, Linda Valis
  • Peptide-based in vivo siRNA delivery system
    Patent number: 8501930
    Abstract: The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: August 6, 2013
    Assignee: Arrowhead Madison Inc.
    Inventors: David B. Rozema, Darren H. Wakefield, David L. Lewis, Jon A. Wolff, Andrei V. Blokhin, Jonathan D. Benson, Jeffrey C. Carlson, Philipp Hadwiger, Eric A. Kitas, Torsten Hoffmann, Kerstin Jahn-Hofmann, Peter Mohr, Hans Martin Mueller, Guenther Ott, Ingo Roehl