Patents by Inventor Anton Simeonov
Anton Simeonov 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: 20230079399Abstract: The disclosure provides compounds of Formula I, which may be useful as aldehyde de-hydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumorsbreast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis.Type: ApplicationFiled: February 28, 2022Publication date: March 16, 2023Inventors: Shyh Ming YANG, David J. MALONEY, Natalia MARTINEZ, Adam YASGAR, Anton SIMEONOV
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Publication number: 20230056533Abstract: Methods for generating multipotent radial glia-like cells and astrocyte-like cells from human pluripotent stem cells are provided along with the related compositions.Type: ApplicationFiled: February 19, 2021Publication date: February 23, 2023Inventors: Ilyas Singec, Vukasin Jovanovic, Anton Simeonov
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Patent number: 11505559Abstract: The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumors breast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis.Type: GrantFiled: October 30, 2018Date of Patent: November 22, 2022Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES OFFICE OF TECHNOLOGY TRANSFER, NATIONAL INSTITUTES OF HEALTH, YALE UNIVERSITYInventors: Shyh Ming Yang, David J. Maloney, Natalia Martinez, Adam Yasgar, Anton Simeonov, Vasilis Vasiliou
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Publication number: 20220228111Abstract: Methods for Generating Neural Crest-Like Cells and Nociceptor-Like Cells from Human Pluripotent Stem Cells are Provided Along with the Related Compositions.Type: ApplicationFiled: April 24, 2020Publication date: July 21, 2022Inventors: Ilyas SINGEC, Tao DENG, Anton SIMEONOV
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Publication number: 20220220078Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.Type: ApplicationFiled: January 10, 2022Publication date: July 14, 2022Inventors: David J. MALONEY, Alex Gregory WATERSON, Ganesh Rai BANTUKALLU, Kyle Ryan BRIMACOMBE, Plamen CHRISTOV, Chi V. DANG, Victor DARLEY-USMAR, Xin HU, Ajit JADHAV, Somnath JANA, Kwangho KIM, Jennifer L. KOUZNETSOVA, William J. MOORE, Bryan T. MOTT, Leonard M. NECKERS, Anton SIMEONOV, Gary Allen SULIKOWSKI, Daniel Jason URBAN, Shyh Ming YANG
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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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Patent number: 11247971Abstract: Provided is a compound of formula (I), in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.Type: GrantFiled: January 28, 2021Date of Patent: February 15, 2022Assignees: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, THE UAB RESEARCH FOUNDATION, VANDERBILT UNIVERSITY, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: David J. Maloney, Alex Gregory Waterson, Ganesh Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor Darley-Usmar, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, Jennifer L. Kouznetsova, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang
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Publication number: 20210348119Abstract: Compositions and methods useful for culturing mammalian cells, tissues and/or organs are provided. The compositions contain Chroman 1 or its derivatives, may further include Emricasan or its derivatives, and may further include one or both of trans-ISRIB and polyamines. The compositions may be formulated as media additives, media concentrates or working media. The compositions and methods may be used to culture stem cells, progenitor cells, differentiated cells, isolated primary cells, secondary cells, immortalized cells, cell line cells, germline cells, somatic cells, or modified cells, including genetically modified cells. The compositions and methods may be used to culture, preserve or maintain cells, tissues, organs parts or organs, grow embryoid bodies, embryos, organs or organ parts.Type: ApplicationFiled: October 11, 2019Publication date: November 11, 2021Applicant: The United States of America as Represented By The Secretary of The Department of Health and HumanInventors: Ilyas SINGEC, Yu CHEN, Anton SIMEONOV
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Publication number: 20210323928Abstract: Provided is a compound of formula (I)[Formula (I) should be inserted here], in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.Type: ApplicationFiled: January 28, 2021Publication date: October 21, 2021Inventors: David J. MALONEY, Alex Gregory WATERSON, Ganesh Rai BANTUKALLU, Kyle Ryan BRIMACOMBE, Plamen CHRISTOV, Chi V. DANG, Victor DARLEY-USMAR, Xin HU, Ajit JADHAV, Somnath JANA, Kwangho KIM, Jennifer L. KOUZNETSOVA, William J. MOORE, Bryan T. MOTT, Leonard M. NECKERS, Anton SIMEONOV, Gary Allen SULIKOWSKI, Daniel Jason URBAN, Shyh Ming YANG
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Patent number: 11110089Abstract: There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein W, X, Y, Z, R1, R2 and R3 have meanings provided in the description, which compounds are useful in the treatment of cancers.Type: GrantFiled: August 5, 2016Date of Patent: September 7, 2021Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Elias Set Jenö ArnérInventors: Elias Set Jenö Arnér, William Chester Stafford, Nathan Patrick Coussens, Diane Karen Luci, David Joseph Maloney, Anton Simeonov, Ajit Jadhav, Thomas S. Dexheimer
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Publication number: 20210179630Abstract: The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumorsbreast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis.Type: ApplicationFiled: October 30, 2018Publication date: June 17, 2021Inventors: Shyh Ming YANG, David J. MALONEY, Natalia MARTINEZ, Adam YASGAR, Anton SIMEONOV, Vasilis VASILIOU
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Patent number: 10961200Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.Type: GrantFiled: June 28, 2019Date of Patent: March 30, 2021Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, VANDERBILT UNIVERSITY, THE UAB RESEARCH FOUNDATION, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: David J. Maloney, Alex Gregory Waterson, Ganesh Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor Darley-Usmar, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, Jennifer L. Kouznetsova, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang
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Patent number: 10954228Abstract: The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred.Type: GrantFiled: June 29, 2017Date of Patent: March 23, 2021Assignees: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, THE UAB RESEARCH FOUNDATION, VANDERBILT UNIVERSITY, NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPT. OF HEALTH AND HUMAN SERVICESInventors: David J. Maloney, Alex Gregory Waterson, Ganesha Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor M. Darley-Usmar, Matthew Hall, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang
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Patent number: 10899710Abstract: There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3, R4 and n have meanings provided in the description, which compounds are useful in the treatment of cancers.Type: GrantFiled: August 5, 2016Date of Patent: January 26, 2021Assignees: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Elias Set Jenö Arnér, William Chester Stafford, Nathan Patrick Coussens, Diane Karen Luci, David Joseph Maloney, Anton Simeonov, Ajit Jadhav, Thomas S. Dexheimer
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Patent number: 10881653Abstract: There is provided compounds of formula (I), or pharmaceutically-acceptable salts thereof, wherein X, Y, Z, R1 and R2 have meanings provided in the description, which compounds are useful in the treatment of cancers.Type: GrantFiled: August 5, 2016Date of Patent: January 5, 2021Assignees: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Elias Set Jenö Arnér, William Chester Stafford, Nathan Patrick Coussens, Diane Karen Luci, David Joseph Maloney, Anton Simeonov, Ajit Jadhav, Thomas S. Dexheimer
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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: 10836759Abstract: A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; R1 and R2 are each independently a halogen, CN, CF3, CHF2, CH2F, a C1-C10alkyl group, a C1-C10alkoxy group, a di(C1-C5alkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.Type: GrantFiled: June 21, 2017Date of Patent: November 17, 2020Assignees: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Matthew Brian Boxer, Xiaodong Wang, Kyle Ryan Brimacombe, Mindy Irene Emily Davis, Yuhong Fang, Matthew Hall, Ajit Jadhav, Surendra Karavadhi, Li Liu, Natalia Martinez, Andrew Louis McIver, Rajan Pragani, Jason Matthew Rohde, Anton Simeonov, Wei Zhao, Min Shen
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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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Patent number: 10703746Abstract: Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X1, X2, R1-4 and R13-18 are disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed.Type: GrantFiled: December 22, 2015Date of Patent: July 7, 2020Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILLInventors: Matthew Brian Boxer, Jason Matthew Rohde, Rajan Pragani, Li Liu, Mindy Irene Emily Davis, Kyle Ryan Brimacombe, Min Shen, Anton Simeonov, Surendra Karavadhi, Daniel Jason Urban, Ajit Jadhav, Xiaodong Wang, Andrew Louis McIver
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Publication number: 20200113897Abstract: There is provided compounds of formula (I) or pharmaceutically-acceptable salts thereof, wherein W, X, Y, Z, R1, R2 and R3 have meanings provided in the description, which compounds are useful in the treatment of cancers.Type: ApplicationFiled: August 5, 2016Publication date: April 16, 2020Inventors: Elias Set Jenö Arnér, William Chester Stafford, Nathan Patrick Coussens, Diane Karen Luci, David Joseph Maloney, Anton Simeonov, Ajit Jadhav, Thomas S. Dexheimer