Patents by Inventor Diane K. Luci
Diane K. Luci 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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Patent number: 9802904Abstract: Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.Type: GrantFiled: December 26, 2013Date of Patent: October 31, 2017Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of DelawareInventors: David J. Maloney, Andrew S. Rosenthal, Ajit Jadhav, Thomas S. Dexheimer, Anton Simeonov, Zhihao Zhuang, Qin Liang, Diane K. Luci
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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: 20150344443Abstract: Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.Type: ApplicationFiled: December 26, 2013Publication date: December 3, 2015Applicants: The United States of America, as represented by the Secretary, Department of Health and Human, University of DelawareInventors: David J. Maloney, Andrew S. Rosenthal, Ajit Jadhav, Thomas S. Dexheimer, Anton Simeonov, Zhihao Zhuang, Qin Liang, Diane K. Luci
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Patent number: 9079896Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters and prodrugs thereof, pharmaceutical compositions containing compounds of formula (I) and the use of said compounds and compositions as urotensin II receptor antagonists.Type: GrantFiled: July 31, 2009Date of Patent: July 14, 2015Assignee: Janssen Pharmaceutica NVInventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff, Shyamali Ghosh, Edward C. Lawson
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Benzo[1,4]oxazin-3-one, benzo[1,4]thiazin-3-one and quinolin-2-one urotensin II receptor antagonists
Patent number: 8759342Abstract: The invention is directed to benzo[1,4]oxazin-3-one, benzo[1,4]thiazin-3-one and quinolin-2-one Urotensin II receptor antagonists useful in treating or ameliorating a Urotensin-II mediated disorder. More specifically, the present invention relates to certain novel benzo[1,4]oxazin-3-one, benzo[1,4]thiazin-3-one and quinolin-2-one compounds and methods for preparing compounds, compositions, intermediates and derivatives thereof. Pharmaceutical compositions and methods for treating or ameliorating a Urotensin-II mediated disorder using compounds of the invention are also described.Type: GrantFiled: July 26, 2007Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Ghosh Shyamali, William A Kinney, Edward C Lawson, Diane K Luci, Bruce E Maryanoff, Francois Maria Sommen -
Patent number: 8536174Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: April 30, 2012Date of Patent: September 17, 2013Assignee: Janssen Pharmaceutica NVInventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Shyamali Ghosh
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Patent number: 8445514Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: July 14, 2011Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20120214817Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Inventors: Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Patent number: 8193191Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: February 14, 2011Date of Patent: June 5, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Shyamali Ghosh
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Publication number: 20110269768Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20110136824Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: February 14, 2011Publication date: June 9, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20100029616Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters and prodrugs thereof, pharmaceutical compositions containing compounds of formula (I) and the use of said compounds and compositions as urotensin II receptor antagonists.Type: ApplicationFiled: July 31, 2009Publication date: February 4, 2010Inventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff, Shyamali Ghosh, Edward C. Lawson
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Publication number: 20080318973Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: ApplicationFiled: June 5, 2008Publication date: December 25, 2008Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey