Patents by Inventor Kenneth Jacobson
Kenneth Jacobson 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: 20230365568Abstract: Provided is a method of treating cancer, particularly cancers associated with an overexpression of polo-like kinase (Plk1), comprising administering a compound of formula (I) or a pharmaceutically acceptable salt thereof in which ring A, X1, X2, X3, X4, X5, R2, R3, R4, n, bond a, and bond b are described herein. Exemplary compounds of formula (I) and pharmaceutically acceptable salts thereof, especially those that selectively inhibit the polo box domain of Plk1, also are provided.Type: ApplicationFiled: September 24, 2021Publication date: November 16, 2023Applicant: The United States of America,as represented by the Secretary,Department of Health and Human ServicesInventors: Kyung S. Lee, Kenneth A. Jacobson, Celeste N. Alverez, Jung-Eun Park, Paola Oliva, Hobin Lee, Klara Pongorne Kirsch
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Patent number: 11584736Abstract: Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, wherein R1-R8, X, Y, Z, X?, Y?, Z?, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.Type: GrantFiled: February 11, 2019Date of Patent: February 21, 2023Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Jinha Yu, Antonella Ciancetta, Zhiwei Wen, Young-Hwan Jung
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Publication number: 20220305044Abstract: The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.Type: ApplicationFiled: April 21, 2017Publication date: September 29, 2022Inventors: William S. Korinek, James D. Lechleiter, Theodore E. Liston, Kenneth A. Jacobson
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Publication number: 20220024926Abstract: Disclosed are compounds of the formulas (I), (II), and (II): which are A1 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein Y, R1-R6, R10-R15, and R20-R22 are as defined in the specification. These compounds are selective to the A1 adenosine receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, for inducing and/or maintaining a hypothermic and/or hypometabolic state for treatment of a mammal.Type: ApplicationFiled: December 6, 2019Publication date: January 27, 2022Applicant: The United States of America,as represented by the Secretary,Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Dilip K. Tosh, Marc L. Reitman, Oksana Gavrilova
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Publication number: 20210169911Abstract: Disclosed is a compound of formula (I), wherein Q, U, T, A, a, b, c, and n are as defined herein. Also disclosed are methods of inhibiting ecto-5?-nucleotidase, inhibiting suppression of an antitumor immune response, inhibiting tumor growth of a cancerous tumor, inhibiting metastasis of cancer in a mammal afflicted with cancer, synergistically enhancing a response of a mammal afflicted with cancer undergoing treatment with an immunotherapeutic anti-cancer agent, potentiating an activity of an inhibitor of nicotinamide phosphoribosyltransferase in a mammal undergoing treatment of a mammal with the inhibitor, and treating preeclampsia in a mammal in need thereof, comprising administering to an animal an effective amount of a compound of formula (I).Type: ApplicationFiled: August 16, 2019Publication date: June 10, 2021Applicants: The United States of America,as represented by the Secretary,Department of Health and Human Services, University of Bonn, University of MünsterInventors: Kenneth A. Jacobson, Anna Junker, Mirko Scortichini, Clemens Dobelmann, Christian P. Renn, Vigneshwaran Namasivayam, Riham Mohammed Idris, Christa E. Müller
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Publication number: 20210047293Abstract: Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, wherein R1-R8, X, Y, Z, X?, Y?, Z?, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.Type: ApplicationFiled: February 11, 2019Publication date: February 18, 2021Applicant: The United States of America,as represented by the Secretary,Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Jinha Yu, Antonella Ciancetta, Zhiwei Wen, Young-Hwan Jung
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Patent number: 10695355Abstract: Described herein are methods for the treatment of a human subject who has had a stroke by administering to the subject a pharmaceutical composition including an antagonist of the P2X4 receptor. The antagonist of the P2X4 receptor can be administered in the acute phase of stroke, optionally in combination with a thrombolytic therapeutic or a procedure on the subject involving a clot-removal device.Type: GrantFiled: March 23, 2018Date of Patent: June 30, 2020Assignees: UNIVERSITY OF CONNECTICUT, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Bruce Liang, Rajkumar Verma, Kenneth A. Jacobson
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Patent number: 10683277Abstract: Described are compounds, which are antagonists of the P2Y14 receptor, for example, a compound of formula (I) in which ring A, R1, R2, R3, and n are as described herein. Also provided are dendron conjugates comprising the compounds, and methods of using the compounds, including a method of treating a disorder, such as inflammation, diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, a condition associated with metabolic syndrome, and asthma, and a method of antagonizing P214 receptor activity in a cell.Type: GrantFiled: September 23, 2016Date of Patent: June 16, 2020Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Anna Junker, Elisa Uliassi, Evgeny Kiselev
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Patent number: 10577368Abstract: Disclosed are compounds of the formula (I) and (II): which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.Type: GrantFiled: April 10, 2018Date of Patent: March 3, 2020Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Saint Louis UniversityInventors: Kenneth A. Jacobson, Dilip K. Tosh, Daniela Salvemini
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Publication number: 20180297981Abstract: Described are compounds, which are antagonists of the P2Y14 receptor, for example, a compound of formula (I) in which ring A, R1, R2, R3, and n are as described herein. Also provided are dendron conjugates comprising the compounds, and methods of using the compounds, including a method of treating a disorder, such as inflammation, diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, a condition associated with metabolic syndrome, and asthma, and a method of antagonizing P214 receptor activity in a cell.Type: ApplicationFiled: September 23, 2016Publication date: October 18, 2018Applicant: The United States of America,as represented by the Secretary,Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Anna Junker, Elisa Uliassi, Evgeny Kiselev
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Publication number: 20180280409Abstract: Described herein are methods for the treatment of a human subject who has had a stroke by administering to the subject a pharmaceutical composition including an antagonist of the P2X4 receptor. The antagonist of the P2X4 receptor can be administered in the acute phase of stroke, optionally in combination with a thrombolytic therapeutic or a procedure on the subject involving a clot-removal device.Type: ApplicationFiled: March 23, 2018Publication date: October 4, 2018Inventors: Bruce Liang, Rajkumar Verma, Kenneth A. Jacobson
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Publication number: 20180230150Abstract: Disclosed are compounds of the formula (I) and (II): which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.Type: ApplicationFiled: April 10, 2018Publication date: August 16, 2018Applicants: The United States of America, as represented by the Secretary, Department of Health and Human Serv, Saint Louis UniversityInventors: Kenneth A. Jacobson, Dilip K. Tosh, Daniela Salvemini
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Patent number: 9963450Abstract: Disclosed are compounds of the formula (I) and (II) which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.Type: GrantFiled: November 20, 2014Date of Patent: May 8, 2018Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Saint Louis UniversityInventors: Kenneth A. Jacobson, Dilip K. Tosh, Daniela Salvemini
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Publication number: 20170002007Abstract: Disclosed are compounds of the formula (I) and (II) which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.Type: ApplicationFiled: November 20, 2014Publication date: January 5, 2017Inventors: Kenneth A. Jacobson, Dilip K. Tosh, Daniela Salvemini
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Patent number: 9526739Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.Type: GrantFiled: February 18, 2016Date of Patent: December 27, 2016Assignees: UNIVERSITY OF CONNECTICUT, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Bruce Liang, Kenneth A. Jacobson
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Publication number: 20160166591Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.Type: ApplicationFiled: February 18, 2016Publication date: June 16, 2016Inventors: Bruce Liang, Kenneth A. Jacobson
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Patent number: 9326978Abstract: The claimed subject matter relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.Type: GrantFiled: March 13, 2013Date of Patent: May 3, 2016Assignees: The United States of America, Represented by the Secretary, Dept. of Health and Human Services, Universiteit LeidenInventors: Anikó Göblyös, Johannes Brussee, Adriaan P. Ijzerman, Zhan-Guo Gao, Kenneth Jacobson
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Patent number: 9303053Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba(bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.Type: GrantFiled: July 23, 2014Date of Patent: April 5, 2016Assignee: UNIVERSITY OF CONNECTICUTInventors: Bruce Liang, Kenneth A. Jacobson
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Patent number: 9227979Abstract: Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A3 adenosine receptor: wherein A, R1, R2, and Y are as described herein. Also disclosed are diagnostic compositions and a method of diagnosis of a patient for a possible treatment by an antagonist of the A3 adenosine receptor, involving the use of one or more of these compounds as diagnostic agents.Type: GrantFiled: January 24, 2013Date of Patent: January 5, 2016Assignees: The United States of America, as represented by The Secretary, Department of Health and Human Services, Universita Degli Studi Di Trieste, Universita Degli Studi Di PadovaInventors: Kenneth A. Jacobson, Santhosh Kumar Thatikonda, Eszter Erika Kozma, Giampiero Spalluto, Stefano Moro, Stephanie Federico
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Patent number: 9181253Abstract: Disclosed are A3 adenosine receptor antagonists and/or partial agonists and A1 adenosine receptor agonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The A3 AR antagonists or partial agonists find use in treating a number of diseases such as cancer, glaucoma, and inflammatory diseases, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs. The A1 AR agonists and partial agonists find use in treating diseases such as seizures, convulsion, stroke, diabetes, pain, arrhythmias, depression, and anxiety and in cardioprotection or neuroprotection.Type: GrantFiled: May 24, 2012Date of Patent: November 10, 2015Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Dilip K. Tosh