Patents by Inventor Richard S. Alexander
Richard S. Alexander 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: 20230175038Abstract: The present invention provides a crystal structure of human BTK with space group space group p 2 21 21 and has unit cell parameters a=38.155±2?; b=72.394±2?; c=103.946±2?; a=90°; b=90°; g=90°; the BTK protein is complexed with N-((1R,2S)-2-Acrylamidocyclopentyl)-5-(S)-(6-isobutyl-4-methylpyridin-3-yl)-4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide.Type: ApplicationFiled: December 7, 2022Publication date: June 8, 2023Inventors: Richard S. ALEXANDER, Cynthia MILLIGAN, Mark S. TICHENOR
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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: 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: 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: 7662824Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: March 16, 2006Date of Patent: February 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristi Leonard, Tianbao Lu, Robert W. Tuman, Dana L. Johnson, Anna C. Maroney, Jan L. Sechler, Richard W. Connors, Richard S. Alexander, Maxwell D. Cummings, Robert A. Galemmo, Thomas P. Markotan
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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