Patents by Inventor Bruce L Grasberger

Bruce L Grasberger 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: 8257698
    Abstract: A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized form of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: September 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bruce L. Grasberger, Celine Schalk-Hihi, Diane M. Maguire, Frank A. Lewandowski, Cynthia M. Milligan, Richard S. Alexander
  • Patent number: 8080400
    Abstract: A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized form of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: December 20, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Carsten Schubert, Bruce L. Grasberger, Celine Schalk-Hihi, Diane M. Maguire, Frank A. Lewandowski, Cynthia M. Milligan, Richard S. Alexander
  • Patent number: 8067220
    Abstract: A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized forms of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: November 29, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Carsten Schubert, Bruce L. Grasberger, Celine Schalk-Hihi, Diane M. Maguire, Frank A. Lewandowski, Cynthia M. Milligan, Richard S. Alexander
  • Publication number: 20100093009
    Abstract: A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized forms of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.
    Type: Application
    Filed: October 9, 2009
    Publication date: April 15, 2010
    Inventors: Carsten Schubert, Bruce L. Grasberger, Celine Schalk-Hihi, Diane M. Maguire, Frank A. Lewandowski, Cynthia M. Milligan, Richard S. Alexander
  • Publication number: 20090269784
    Abstract: A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized form of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.
    Type: Application
    Filed: April 24, 2009
    Publication date: October 29, 2009
    Inventors: BRUCE L. GRASBERGER, CELINE SCHALK-HIHI, DIANE M. MAGUIRE, FRANK A. LEWANDOWSKI, CYNTHIA M. MILLIGAN, RICHARD S. ALEXANDER
  • Publication number: 20090269785
    Abstract: A number of soluble engineered forms of MGLL that are suitable for high-throughput screening and protein crystallization, as well as a crystallized form of monoacylglycerol lipase protein (MGLL) and descriptions of the X-ray diffraction patterns are disclosed. The engineered constructs of MGLL permit the expression and purification of protein suitable for crystallography or high-throughput screening and identification of ligands, which can function as active agents to MGLL. The X-ray diffraction patterns allow the three dimensional structure of MGLL to be determined at atomic resolution so that ligand binding sites on MGLL can be identified and the interactions of ligands with MGLL amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of MGLL.
    Type: Application
    Filed: April 24, 2009
    Publication date: October 29, 2009
    Inventors: CARSTEN SCHUBERT, BRUCE L. GRASBERGER, CELINE SCHALK-HIHI, DIANE M. MAGUIRE, FRANK A. LEWANDOWSKI, CYNTHIA M. MILLIGAN, RICHARD S. ALEXANDER
  • Publication number: 20090155815
    Abstract: A crystallized human ACC2 CT protein as well as a description of the X-ray diffraction pattern of the crystal are disclosed. The diffraction pattern allows the three dimensional structure of human ACC2 CT to be determined at atomic resolution so that ligand binding sites on human ACC2 CT can be identified and the interactions of ligands with human ACC2 CT amino acid residues can be modeled. Models prepared using such maps permit the design of ligands which can function as active agents which include, but are not limited to, those that function as inhibitors of human ACC2 and human ACC1 proteins.
    Type: Application
    Filed: October 24, 2008
    Publication date: June 18, 2009
    Inventors: Bruce L. Grasberger, Cynthia Milligan, John C. Spurlino, Ruth A. Steele, Kenneth R. Singleton, Alan C. Gibbs, Francis A. Lewandowski
  • Patent number: 7067512
    Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: June 27, 2006
    Inventors: Tianbao Lu, Louis V Lafrance, III, Daniel J Parks, Karen L Milkiewicz, Raul R Calvo, Maxwell D Cummings, Alexander J Kim, Bruce L Grasberger, Theodore E Carver, Jr.
  • Publication number: 20030109518
    Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.
    Type: Application
    Filed: November 13, 2002
    Publication date: June 12, 2003
    Inventors: Tianbao Lu, Louis V. Lafrance, Daniel J. Parks, Karen L. Milkiewicz, Raul R. Calvo, Maxwell D. Cummings, Alexander J. Kim, Bruce L. Grasberger, Theodore E. Carver