Patents by Inventor Theodore Holman
Theodore Holman 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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Patent number: 11274077Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.Type: GrantFiled: June 23, 2020Date of Patent: March 15, 2022Assignees: Eastern Virginia Medical School, The Regents of the University of California Santa, The United States of America Department of Health, Thomas Jefferson UniversityInventors: David J. Maloney, Diane K. Luci, Ajit Jadhav, Theodore Holman, Jerry L. Nadler, Michael Holinstat, David Taylor-Fishwick, Anton Simeonov, Adam Yasgar, Steven McKenzie
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Publication number: 20200392077Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.Type: ApplicationFiled: June 23, 2020Publication date: December 17, 2020Inventors: David J. MALONEY, Diane K. LUCI, Ajit JADHAV, Theodore HOLMAN, Jerry L. NADLER, Michael HOLINSTAT, David TAYLOR-FISHWICK, Anton SIMEONOV, Adam YASGAR, Steven MCKENZIE
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Patent number: 10752581Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.Type: GrantFiled: March 1, 2019Date of Patent: August 25, 2020Assignees: Eastern Virginia Medical School, The Regents of the University of California Santa, The United States of America Department of Health, Thomas Jefferson UniversityInventors: David J. Maloney, Diane K. Luci, Ajit Jadhav, Theodore Holman, Jerry L. Nadler, Michael Holinstat, David Taylor-Fishwick, Anton Simeonov, Adam Yasgar, Steven McKenzie
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Publication number: 20190276395Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.Type: ApplicationFiled: March 1, 2019Publication date: September 12, 2019Inventors: David J. MALONEY, Diane K. LUCI, Ajit JADHAV, Theodore HOLMAN, Jerry L. NADLER, Michael HOLINSTAT, David TAYLOR-FISHWICK, Anton SIMEONOV, Adam YASGAR, Steven MCKENZIE
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Patent number: 10266488Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.Type: GrantFiled: October 10, 2014Date of Patent: April 23, 2019Assignees: Eastern Virginia Medical School, The Regents of the University of California Santa Cruz, The United States of America Department of Health and Human Services, Thomas Jefferson UniversityInventors: David J. Maloney, Diane K. Luci, Ajit Jadhav, Theodore Holman, Jerry L. Nadler, Michael Holinstat, David Taylor-Fishwick, Anton Simeonov, Adam Yasgar, Steven McKenzie
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Publication number: 20170001955Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells.Type: ApplicationFiled: October 10, 2014Publication date: January 5, 2017Inventors: David J. MALONEY, Diane K. LUCI, Ajit JADHAV, Theodore HOLMAN, Jerry L. NADLER, Michael HOLINSTAT, David TAYLOR-FISHWICK, Anton SIMEONOV, Adam YASGAR
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Publication number: 20130096159Abstract: Disclosed are inhibitors of human 12-lipoxygenase of Formula (I) or (II), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating or preventing a 12-lipoxygenase mediated disease or disorder, e.g., diabetes. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.Type: ApplicationFiled: May 18, 2011Publication date: April 18, 2013Applicants: The United States of America, as represented the Secretary Department of Health & Human Service, Thomas Jefferson University, Eastern Virginia Medical School, The Regents of the University of CaliforniaInventors: David J. Maloney, Theodore Holman, Ajit Jadhav, Anton Simeonov, Ganesha Rai Bantukallu, Jerry L. Nadler, Michael Holinstat
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Patent number: 6750247Abstract: Compounds that are effective lipoxygenase inhibitors, and methods and pharmaceutical compositions for inhibiting lipoxygenases and for treatment of lipoxygenase-mediated conditions in humans and other subjects. The compounds, methods and pharmaceutical compositions utilize subersic terpenoids, jaspic terpenoids, igernellic terpenoids, hippospongic terpenoids, halicondric terpenoids, dictyodendric terpenoids, and/or heteronemic terpenoids, and synthetic derivatives or analogs thereof. Exemplary compounds include (−)-subersic acid, (+)-subersin, jaspaquinol, (−)-jaspic acid, igernellin, halisufate 7, and hipposulfate C and D, and derivatives thereof.Type: GrantFiled: May 31, 2002Date of Patent: June 15, 2004Assignee: Galileo Laboratories, Inc.Inventors: Phillip Crews, Jennifer Carroll, Theodore Holman, Guy Miller, Steve Bobzin, Lesley Brown
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Publication number: 20030065025Abstract: Compounds that are effective lipoxygenase inhibitors, and methods and pharmaceutical compositions for inhibiting lipoxygenases and for treatment of lipoxygenase-mediated conditions in humans and other subjects. The compounds, methods and pharmaceutical compositions utilize subersic terpenoids, jaspic terpenoids, igernellic terpenoids, hippospongic terpenoids, halicondric terpenoids, dictyodendric terpenoids, and/or heteronemic terpenoids, and synthetic derivatives or analogs thereof. Exemplary compounds include (−)-subersic acid, (+)-subersin, jaspaquinol, (−)-jaspic acid, igernellin, halisufate 7, and hipposulfate C and D, and derivatives thereof.Type: ApplicationFiled: May 31, 2002Publication date: April 3, 2003Inventors: Phillip Crews, Jennifer Carroll, Theodore Holman, Guy Miller, Steve Bobzin, Lesley Brown