Patents by Inventor Eric Kitas

Eric 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
  • Publication number: 20200230248
    Abstract: The present invention relates to a polyplex for use in the treatment of castration resistant prostate cancer (CRPC) comprising a double stranded RNA (dsRNA) and a polymeric conjugate, wherein said polymeric conjugate consists of a linear polyethyleneimine (LPEl), one or more polyethylene glycol (PEG) moieties, one or more linkers and one or more targeting moieties, wherein said LPEl is covalently bound to one or more PEG moieties and each of said one or more PEG moieties is conjugated via one of the one or more linkers to one of the one or more targeting moieties, wherein each of said one or more targeting moieties is capable of binding to a cancer antigen, and wherein said cancer antigen is prostate surface membrane antigen (PSMA). Further, the invention relates to a pharmaceutical composition for use in the treatment of CRPC.
    Type: Application
    Filed: September 27, 2018
    Publication date: July 23, 2020
    Inventors: Esteban POMBO-VILLAR, Alexander LEVITZKI, Yael LANGUT, Maya ZIGLER, Alexei SHIR, Eric KITAS
  • 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
  • Publication number: 20180179252
    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: July 21, 2016
    Publication date: June 28, 2018
    Inventors: Jeremy BEAUCHAMP, Per-Ola FRESKGARD, Eric A. KITAS, Victor LYAMICHEV, Jigar PATEL
  • 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
  • Publication number: 20180105569
    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: December 4, 2017
    Publication date: April 19, 2018
    Inventors: Richard D. DiMARCHI, David L. SMILEY, Konrad H. BLEICHER, Eric A. KITAS
  • Publication number: 20180057526
    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: Application
    Filed: November 7, 2017
    Publication date: March 1, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Benoit HORNSPERGER, Roberto IACONE, Eric A. KITAS, Hans P. MAERKI, Michael REUTLINGER, Peter MOHR
  • 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: 20160310575
    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: Application
    Filed: December 19, 2014
    Publication date: October 27, 2016
    Inventors: Sara BELLI, Konrad BLEICHER, Richard D. DIMARCHI, Eike HOFFMANN, Eric A. KITAS, Anish A. KONKAR
  • 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