Patents by Inventor Frank Lewandowski

Frank Lewandowski 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: 8927297
    Abstract: The crystal structure of the ligand binding domain of ERR-? in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-?, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-? activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-? and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: January 6, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
  • Patent number: 8883473
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Carl Crysler, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Carl Manthey, Cynthia M. Milligan, Beverley Moore, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett A. Tounge, Aihua Wang
  • Patent number: 8798939
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Cynthia M. Milligan, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett A. Tounge, Aihua Wang
  • Patent number: 8753857
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: June 17, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Cynthia M. Milligan, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett A. Tounge, Aihua Wang
  • Publication number: 20130166268
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Application
    Filed: June 26, 2012
    Publication date: June 27, 2013
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Cynthia M. Milligan, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett Andrew Tongue, Aihua Wang
  • Patent number: 8455244
    Abstract: The crystal structure of the ligand binding domain of ERR-? in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-?, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-? activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-? and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: June 4, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
  • Publication number: 20130040994
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Application
    Filed: June 26, 2012
    Publication date: February 14, 2013
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Carl Crysler, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Carl Manthey, Cynthia M. Milligan, Beverley Moore, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett Andrew Tongue, Aihua Wang
  • Publication number: 20130040360
    Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.
    Type: Application
    Filed: June 26, 2012
    Publication date: February 14, 2013
    Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Cynthia M. Milligan, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett Andrew Tongue, Aihua Wang
  • Publication number: 20120226021
    Abstract: The crystal structure of the ligand binding domain of ERR-? in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-?, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-? activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-? and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
    Type: Application
    Filed: April 30, 2012
    Publication date: September 6, 2012
    Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
  • 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: 8187871
    Abstract: The crystal structure of the ligand binding domain of ERR-? in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-?, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-? activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-? and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: May 29, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
  • 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: 20110046891
    Abstract: The crystal structure of the ligand binding domain of ERR-? in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-?, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-? activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-? and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
    Type: Application
    Filed: August 4, 2010
    Publication date: February 24, 2011
    Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
  • Publication number: 20110039352
    Abstract: The crystal structure of the ligand binding domain of ERR-? in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-?, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-? activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-? and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.
    Type: Application
    Filed: August 4, 2010
    Publication date: February 17, 2011
    Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
  • 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
  • Patent number: 7655756
    Abstract: A method for the identification of novel compounds that interact and stabilize the ligand binding domain of estrogen-related receptor gamma (ERR?), a methodology for producing diffraction quality crystal structures in the presence of antagonist and agonist ligands, including Bisphenol A, and the identification of novel biologically-active compounds that have an effect on the transcriptional-activating activity of ERR? are disclosed.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: February 2, 2010
    Assignee: Johnson & Johnson Pharmaceutical Research & Development, LLC
    Inventors: Marta C. Abad, Dionisios Rentzeperis, John O'Neill, Hossein B. Askari, Cynthia M. Milligan, Frank A. Lewandowski
  • 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
  • Patent number: 5987425
    Abstract: A variable margin pricing system and method that generates retail prices based on customer price sensitivity. Products are grouped into pools from a first pool for most price sensitive products to a last pool for least price sensitive products. A logical relationship between margins and the customer price sensitivity is determined for the products. Based on this logical relationship and each product's pool assignment, the system and method calculate each product's margin and corresponding retail price. The method is also used to generate retail price labels having retail prices based on customer price sensitivity for the products to which the labels are to be affixed or located proximate.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: November 16, 1999
    Assignee: United Hardware Distributing Company
    Inventors: David J. Hartman, Frank Lewandowski