Patents by Inventor Eric A. Kitas

Eric A. Kitas 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).

  • Patent number: 10947272
    Abstract: The present invention relates to dual-site BACE1 inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: March 16, 2021
    Assignees: Hoffmann-La Roche Inc., ROCHE NIMBLEGEN, INC.
    Inventors: Jeremy Beauchamp, Per-Ola Freskgard, Eric A. Kitas, Victor Lyamichev, Jigar Patel
  • Patent number: 10683329
    Abstract: Provided herein are peptides having dual-site BACE1 inhibitory activity, useful for the treatment of, for example Alzheimer's disease and diabetes. One such peptide is a dual-site BACE1 inhibitor, or a pharmaceutically acceptable salt thereof, binding to both an enzymatic active site and an catalytic domain of the BACE enzyme, and an exosite inhibitory part is connected to an active-site inhibitory part of the dual site BACE1 inhibitor by a linker.
    Type: Grant
    Filed: November 25, 2015
    Date of Patent: June 16, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Per-Ola Freskgard, Eric A. Kitas
  • Patent number: 10428108
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: October 1, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benoit Hornsperger, Roberto Iacone, Eric A. Kitas, Hans P. Maerki, Michael Reutlinger, Peter Mohr
  • Patent number: 10208087
    Abstract: The present invention relates to dual-site BACE1 inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: November 25, 2015
    Date of Patent: February 19, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Per-Ola Freskgard, Eric A. Kitas
  • Patent number: 10137170
    Abstract: Herein is reported a fusion polypeptide comprising i) one, two, three or four incretin receptor ligand polypeptides, and ii) one human immunoglobulin Fc-region, wherein at least one of the incretin receptor ligand polypeptides comprises an amino acid that is covalently conjugated to a lipid, and wherein each of the one, two, three or four incretin receptor ligand polypeptides is covalently conjugated by a peptide bond to a terminus of the human immunoglobulin Fc-region, whereby to each terminus of the human immunoglobulin Fc-region only a single incretin receptor ligand polypeptide is conjugated.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: November 27, 2018
    Assignees: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION, HOFFMANN-LA ROCHE INC.
    Inventors: Sara Belli, Konrad Bleicher, Richard D. Dimarchi, Eike Hoffmann, Eric A. Kitas, Anish A. Konkar
  • Publication number: 20180312541
    Abstract: The present invention relates to dual-site BACE1 inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: November 25, 2015
    Publication date: November 1, 2018
    Inventors: Per-Ola Freskgard, Eric A. Kitas
  • Patent number: 9968647
    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: Grant
    Filed: April 4, 2016
    Date of Patent: May 15, 2018
    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
  • Patent number: 9868772
    Abstract: Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: January 16, 2018
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Richard D. Dimarchi, David L. Smiley, Konrad H. Bleicher, Eric A. Kitas
  • Publication number: 20170320912
    Abstract: The present invention relates to dual-site BACE1 inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: November 25, 2015
    Publication date: November 9, 2017
    Inventors: Per-Ola Freskgard, Eric A. Kitas
  • Patent number: 9796756
    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 17, 2015
    Date of Patent: October 24, 2017
    Assignee: Arrowhead Pharmaceuticals, Inc.
    Inventors: Philipp Hadwiger, Torsten Hoffmann, Eric A Kitas, Peter Mohr, Ingo Roehl, Linda Valis, David B Rozema, David L Lewis, Darren H Wakefield
  • Publication number: 20170022505
    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: April 4, 2016
    Publication date: January 26, 2017
    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
  • Publication number: 20160102120
    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: Application
    Filed: December 17, 2015
    Publication date: April 14, 2016
    Inventors: Philipp Hadwiger, Torsten Hoffmann, Eric A Kitas, Peter Mohr, Ingo Roehl, Linda Valis, David B Rozema, David L Lewis, Darren H Wakefield
  • Patent number: 9301990
    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: Grant
    Filed: June 13, 2013
    Date of Patent: April 5, 2016
    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
  • 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
  • Publication number: 20150368310
    Abstract: Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 24, 2015
    Inventors: Richard D. Dimarchi, David L. Smiley, Konrad H. Bleicher, Eric A. Kitas
  • 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
  • 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
  • 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
  • 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
  • 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