Patents by Inventor Barry Springer

Barry Springer 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).

  • Chemically modified quinoline and quinolone derivatives useful as CB-1 inverse agonists
    Patent number: 9815790
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the CB1 receptor. Such compounds are represented by Formula (I) wherein R1, R2, R3, L1, n, v, r, w, and g are defined herein. and further represented by Formula (II) wherein the group “X?Y”, ring A, R10, R11, R30, W, and t are defined herein.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: November 14, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark J. Macielag, Yue-Mei Zhang, Michael N. Greco, Barry A. Springer, William V. Murray
  • CHEMICALLY MODIFIED QUINOLINE AND QUINOLONE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
    Publication number: 20170057922
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the CB1 receptor. Such compounds are represented by Formula (I) wherein R1, R2, R3, L1, n, v, r, w, and g are defined herein. and further represented by Formula (II) wherein the group “X?Y”, ring A, R10, R11, R30, W, and t are defined herein.
    Type: Application
    Filed: August 17, 2016
    Publication date: March 2, 2017
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark J. Macielag, Yue-Mei Zhang, Michael N. Greco, Barry A. Springer, William V. Murray
  • Methods of treatment using allosteric processing inhibitors for matrix metalloproteinases
    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
  • Methods for designing, selecting and/or optimizing allosteric processing inhibitors for matrix metalloproteinases
    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
  • Crystal structure of the pro form of a matrix metalloproteinase and an allosteric processing inhibitor
    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
  • Crystal Structure of the Pro Form of a Matrix Metalloproteinase and an Allosteric Processing Inhibitor
    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
  • Methods of Treatment Using Allosteric Processing Inhibitors for Matrix Metalloproteinases
    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
  • Crystal Structure of the Pro Form of a Matrix Metalloproteinase and an Allosteric Processing Inhibitor
    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
  • METHODS OF INHIBITING PRO MATRIX METALLOPROTEINASE ACTIVATION
    Publication number: 20120302573
    Abstract: This invention relates to methods for preventing, treating or ameliorating an MMP9 and/or MMP13 mediated syndrome, disorder or disease comprising administering to a subject in need thereof an effective amount of a compound listed in the examples section of this specification, or a form, composition or medicament thereof. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Paul Francis JACKSON, Carl Manthey, Kenneth Rhodes, Robert Scannevin, Kristi Anne Leonard, Joseph Kent Barbay, Matthew Todd, Barry A. Springer
  • Methods of using analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, asparate 101 or leucine 137
    Patent number: 7138374
    Abstract: The present invention relates to novel muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the production of said muteins. Also disclosed are methods for stimulating cell division, treating a wound, treating ischemia, treating heart disease, treating neural injury, treating peripheral vascular disease, treating a gastric ulcer and treating a duodenal ulcer.
    Type: Grant
    Filed: February 23, 2004
    Date of Patent: November 21, 2006
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Barry A. Springer, Michael W. Pantoliano, Celia M. Sharp
  • Method for the identification of ligands
    Publication number: 20060110732
    Abstract: The present invention relates generally to a method of identifying ligands that modulate protein-protein interactions. More particularly, the present invention relates to methods of determining agonists or antagonists of a co-regulator dependent target molecule based on the ability to modify the stability of the target molecule in a tissue-selective manner.
    Type: Application
    Filed: July 23, 2003
    Publication date: May 25, 2006
    Inventors: Roger Bone, Dionisios Rentzeperis, Hossein Askari, Barry Springer
  • Crystal structure of the c-fms kinase domain: applications and use of heterologous substitutions of kinase insert domains for crystallization
    Publication number: 20060094081
    Abstract: The present invention includes a crystal structure of the kinase domain of c-fms and a methodology to produce diffraction quality crystals of the c-fms kinase domain by heterologous substitution of the kinase insert domain. Also included in the invention is the structure of the c-fms kinase domain in liganded form for use in the discovery of inhibitors of c-fms for the treatment of diseases caused by inappropriate activity of c-fms. The present invention includes descriptions of the X-ray diffraction patterns of the crystals. The diffraction patterns allow the three dimensional structure of c-fms to be determined at atomic resolution so that ligand binding sites on can be identified and the interactions of ligands with amino acid residues can be modeled.
    Type: Application
    Filed: October 20, 2005
    Publication date: May 4, 2006
    Inventors: Carsten Schubert, Barry Springer, Ingrid Deckman, Raymond Patch, Geoffrey Struble, Hongchang Ma, Celine Schalk-Hihi, Benjamin Brandt, Ioanna Petrounia
  • Method for the idenification of ligands
    Publication number: 20060024844
    Abstract: The present invention relates generally to a method of identifying ligands that modulate protein-protein interactions. More particularly, the present invention relates to methods of determining agonists or antagonists of a co-regulator dependent target molecule based on the ability to modify the stability of the target molecule.
    Type: Application
    Filed: September 20, 2002
    Publication date: February 2, 2006
    Inventors: Dionisios Rentzeperis, Hossein Askari, Barry Springer, Roger Bone, Francis Salemme
  • Analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, asparate 101 or leucine 137
    Publication number: 20050159350
    Abstract: The present invention relates to novel muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the production of said muteins. Also disclosed are methods for stimulating cell division, treating a wound, treating ischemia, treating heart disease, treating neural injury, treating peripheral vascular disease, treating a gastric ulcer and treating a duodenal ulcer.
    Type: Application
    Filed: February 23, 2004
    Publication date: July 21, 2005
    Inventors: Barry Springer, Michael Pantoliano, Celia Sharp
  • Analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, Aspartate 101 or Leucine 137
    Patent number: 6767722
    Abstract: The present invention relates to muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the production of said muteins. Also disclosed is a method for stimulating cell division.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: July 27, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Barry A. Springer, Michael W. Pantoliano, Celia M. Sharp
  • Methods of using analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, aspartate 101 or leucine 137
    Patent number: 6737404
    Abstract: The present invention relates to novel muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the production of said muteins. Also disclosed are methods for stimulating cell division, treating a wound, treating ischemia, treating heart disease, treating neural injury, treating peripheral vascular disease, treating a gastric ulcer and treating a duodenal ulcer.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: May 18, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Barry A. Springer, Michael W. Pantoliano, Celia M. Sharp
  • Microplate thermal shift assay for ligand development using 5- (4"-dimethylaminophenyl) -2- (4' -phenyl) oxazole derivative fluorescent dyes
    Publication number: 20030175813
    Abstract: The present invention provides a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of unfolding due to a thermal change.
    Type: Application
    Filed: February 14, 2003
    Publication date: September 18, 2003
    Applicant: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Michael W. Pantoliano, Eugenio C. Petrella, F. Raymond Salemme, Barry A. Springer
  • Microplate thermal shift assay for ligand development using 5-(4?dimethylaminophenyl)-2-(4?-phenyl)oxazole derivative fluorescent dyes
    Patent number: 6569631
    Abstract: The present invention provides a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of unfolding due to a thermal change.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: May 27, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Michael W. Pantoliano, Eugenio C. Petrella, F. Raymond Salemme, Barry A. Springer
  • Microplate thermal shift assay for ligand development and multi-variable protein chemistry optimization
    Patent number: 6291191
    Abstract: The present invention is a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of denaturing due to a thermal change.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: September 18, 2001
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Michael W. Pantoliano, Eugenio C. Petrella, Alexander W. Rhind, Francis R. Salemme, Barry A. Springer
  • Method for identifying conditions that facilitate recombinant protein folding
    Patent number: 6291192
    Abstract: The present invention is a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of denaturing due to a thermal change.
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: September 18, 2001
    Assignee: 3-Dimensional Pharmaceuticals Inc.
    Inventors: Michael W. Pantoliano, Eugenio C. Petrella, Francis R. Salemme, Barry A. Springer