Patents by Inventor Frank A. Lewandowski
Frank A. 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).
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Publication number: 20230103214Abstract: A massage system for a seat having a seat surface. At least one plane is defined for the seat, which plane is spanned by a longitudinal axis and a vertical axis of the seat. The at least one plane separates a first side and a second side of the seat from one another and intersects the seat. At least one massage element is arranged in at least one component of the seat. The at least one massage element has at least one active surface which is arranged on at least one of the two sides of the seat.Type: ApplicationFiled: December 7, 2020Publication date: March 30, 2023Applicant: AUDI AGInventors: Susanne MENTZEL, Frank THIERFELDT, Josef MEIER, Frank LEWANDOWSKI, Tobias LANDGRAF
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Patent number: 8927297Abstract: 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: GrantFiled: August 4, 2010Date of Patent: January 6, 2015Assignee: Janssen Pharmaceutica N.V.Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
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Patent number: 8883473Abstract: 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: GrantFiled: June 26, 2012Date of Patent: November 11, 2014Assignee: 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
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Patent number: 8798939Abstract: 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: GrantFiled: June 26, 2012Date of Patent: August 5, 2014Assignee: 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
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Patent number: 8753857Abstract: 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: GrantFiled: June 26, 2012Date of Patent: June 17, 2014Assignee: 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
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Publication number: 20130166268Abstract: 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: ApplicationFiled: June 26, 2012Publication date: June 27, 2013Inventors: 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
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Patent number: 8455244Abstract: 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: GrantFiled: April 30, 2012Date of Patent: June 4, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
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Publication number: 20130040360Abstract: 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: ApplicationFiled: June 26, 2012Publication date: February 14, 2013Inventors: 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
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Publication number: 20130040994Abstract: 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: ApplicationFiled: June 26, 2012Publication date: February 14, 2013Inventors: 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
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Publication number: 20120226021Abstract: 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: ApplicationFiled: April 30, 2012Publication date: September 6, 2012Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
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Patent number: 8257698Abstract: 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: GrantFiled: April 24, 2009Date of Patent: September 4, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Bruce L. Grasberger, Celine Schalk-Hihi, Diane M. Maguire, Frank A. Lewandowski, Cynthia M. Milligan, Richard S. Alexander
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Patent number: 8187871Abstract: 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: GrantFiled: August 4, 2010Date of Patent: May 29, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
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Patent number: 8080400Abstract: 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: GrantFiled: April 24, 2009Date of Patent: December 20, 2011Assignee: 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
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Patent number: 8067220Abstract: 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: GrantFiled: October 9, 2009Date of Patent: November 29, 2011Assignee: 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
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Publication number: 20110046891Abstract: 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: ApplicationFiled: August 4, 2010Publication date: February 24, 2011Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
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Publication number: 20110039352Abstract: 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: ApplicationFiled: August 4, 2010Publication date: February 17, 2011Inventors: Dionisios Rentzeperis, Marta Cristina Abad, Ludmila A. Barnakova, Frank A. Lewandowski, Cynthia M. Milligan
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Publication number: 20100093009Abstract: 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: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Carsten Schubert, Bruce L. Grasberger, Celine Schalk-Hihi, Diane M. Maguire, Frank A. Lewandowski, Cynthia M. Milligan, Richard S. Alexander
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Patent number: 7655756Abstract: 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: GrantFiled: May 26, 2006Date of Patent: February 2, 2010Assignee: Johnson & Johnson Pharmaceutical Research & Development, LLCInventors: Marta C. Abad, Dionisios Rentzeperis, John O'Neill, Hossein B. Askari, Cynthia M. Milligan, Frank A. Lewandowski
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Publication number: 20090269784Abstract: 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: ApplicationFiled: April 24, 2009Publication date: October 29, 2009Inventors: BRUCE L. GRASBERGER, CELINE SCHALK-HIHI, DIANE M. MAGUIRE, FRANK A. LEWANDOWSKI, CYNTHIA M. MILLIGAN, RICHARD S. ALEXANDER
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Publication number: 20090269785Abstract: 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: ApplicationFiled: April 24, 2009Publication date: October 29, 2009Inventors: CARSTEN SCHUBERT, BRUCE L. GRASBERGER, CELINE SCHALK-HIHI, DIANE M. MAGUIRE, FRANK A. LEWANDOWSKI, CYNTHIA M. MILLIGAN, RICHARD S. ALEXANDER