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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Patent number: 6545002Abstract: The present invention provides compounds having the formula I: X is (C1-C8)alkylene, (C2-C8)alkenylene, (C2-C8)alkynylene, wherein one of the carbon atoms in the alkylene, alkenylene or alkynylene groups is optionally replaced with a group having the formula —O—, —N(R4)C(O)—, —OC(O—, S—, —S(O)—or —SO2—, or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising compounds having the formula I. The compounds of the invention are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents for treatment of diseases that are mediated by A2B adenosine receptors.Type: GrantFiled: February 17, 2000Date of Patent: April 8, 2003Assignees: University of Virginia Patent Foundation, National Institutes of HealthInventors: Joel M. Linden, Kenneth A. Jacobson, Yong-Chul Kim
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Patent number: 6528516Abstract: This invention relates to a method of decreasing intraocular pressure by administrating an A3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen.Type: GrantFiled: May 4, 2001Date of Patent: March 4, 2003Assignee: Trustees of the University of Pennsylvania, The Center for Technology TransferInventors: Mortimer M. Civan, Richard A. Stone, Claire H. Mitchell, Kenneth A. Jacobson
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Patent number: 6413736Abstract: Phaffia rhodozyma strains are described which produce greater than 3,000 ppm astaxanthin based on dry yeast solids when cultivated in a volume of nutrient medium of at least about 1,500 liters and containing in excess of 4 percent, preferably in excess of 6 percent, dry yeast solids. These and other strains are cultivated by an improved fermentation method comprising extending the maturation phase of the fermentation by one or more various techniques including exposing the yeast cells to a low-intensity light, slow feeding the cells with a rapidly metabolized energy source, e.g. glucose, and replacing the rapidly metabolized energy source with a slowly metabolized energy source, e.g. gylcerol. The cells of these strains are incorporated into animal feeds, particularly feeds for salmonid fishes, to impart or enhance the red pigmentation of these animals and products made from these animals.Type: GrantFiled: August 12, 1999Date of Patent: July 2, 2002Assignee: Archer-Daniels-Midland CompanyInventors: Gunnard Kenneth Jacobson, Setsuko Omata Jolly, Joseph James Sedmak, Thomas Joseph Skatrud, John Marion Wasileski
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Patent number: 6376521Abstract: Disclosed are pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of selectively blocking an A3 adenosine receptor of a mammal by the use of one or more of these derivatives. An example of the pyridine derivative is of the formula (I): wherein R2 is ethyl, R3 is ethylsulfanyl; R4 is ethyl, propyl, or hydroxypropyl; R5 is ethyl, propyl, fluoroethyl, or fluoropropyl; and R6 is phenyl or fluorophenyl. The derivatives of the present invention can be used for inhibiting binding of ligands to an adenosine receptor. The derivatives also can be used for characterizing an adenosine receptor.Type: GrantFiled: April 2, 2001Date of Patent: April 23, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, An-Hu Li
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Patent number: 6329349Abstract: Materials and methods for reducing or preventing ischemic damage of the heart are disclosed. A preferred embodiment of the invention comprises methods of sequential administration of a plurality of cardioprotective agents to patients suffering from ischernic damage or at risk for the same.Type: GrantFiled: April 24, 2000Date of Patent: December 11, 2001Assignees: Trustees of the University of Pennsylvania, The United States of America as represented by the Department of Health and Human ServicesInventors: Bruce T. Liang, Kenneth A. Jacobson
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Patent number: 6316423Abstract: The present invention provides a method of treating ischemic, hypoxic or anoxic brain damage in an animal comprising administering to an animal afflicted with ischemic, hypoxic, or anoxic brain damage, or an animal in imminent danger of suffering ischemic, hypoxic, or anoxic brain damage, a therapeutically effective amount of ADAC, or an analogue thereof.Type: GrantFiled: March 4, 1999Date of Patent: November 13, 2001Assignee: The United States of America as represented by the Departmant of Health and Human ServicesInventors: Dag K. J. E. Von Lubitz, Kenneth A. Jacobson
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Patent number: 6211165Abstract: Compositions and methods for reducing or preventing ischemic damage of the heart are disclosed. A preferred embodiment of the invention comprises the simultaneous administration of specific A3/A1 receptor agonists, to patients suffering from ischemic damage or at risk for the same. In yet another embodiment of the invention, a binary conjugate which acts as an agonist for the A3 receptor and an antagonist at the A2a receptor, is administered to reduce or prevent ischemic damage to the heart.Type: GrantFiled: November 5, 1999Date of Patent: April 3, 2001Assignees: The Trustees of the University of Pennsylvania, The United States of America as represented by the Department of Health and Human ServicesInventors: Bruce T. Liang, Kenneth A. Jacobson
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Patent number: 6083954Abstract: The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl.sup.- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which constitutes a portion of the CFTR protein. The present invention also provides a method of treating CF cells by contacting cells having a reduced apical Cl.sup.- conductance with a therapeutically effective quantity of a compound selected by the present inventive identification method. Preferred compounds for such treatment have little or no affinity for adenosine cell receptors. The present invention provides novel compounds useful in practicing the present inventive method, as well as pharmaceutical compositions containing such compounds.Type: GrantFiled: July 13, 1998Date of Patent: July 4, 2000Inventors: Harvey B. Pollard, Kenneth A. Jacobson
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Patent number: 6066642Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.Type: GrantFiled: December 7, 1998Date of Patent: May 23, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
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Patent number: 6015684Abstract: Phaffia rhodozyma strains are described which produce greater than 3,000 ppm astaxanthin based on dry yeast solids when cultivated in a volume of nutrient medium of at least about 1,500 liters and containing in excess of 4 percent, preferably in excess of 6 percent, dry yeast solids. These and other strains are cultivated by an improved fermentation method comprising extending the maturation phase of the fermentation by one or more various techniques including exposing the yeast cells to a low-intensity light, slow feeding the cells with a rapidly metabolized energy source, e.g. glucose, and replacing the rapidly metabolized energy source with a slowly metabolized energy source, e.g. gylcerol. The cells of these strains are incorporated into animal feeds, particularly feeds for salmonid fishes, to impart or enhance the red pigmentation of these animals and products made from these animals.Type: GrantFiled: November 10, 1997Date of Patent: January 18, 2000Assignee: Archer-Daniels-Midland CompanyInventors: Gunnard Kenneth Jacobson, Setsuko Omata Jolly, Joseph James Sedmak, Thomas Joseph Skatrud, John Marion Wasileski
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Patent number: 5922560Abstract: Phaffia rhodozyma strains are described which produce greater than 3,000 ppm astaxanthin based on dry yeast solids when cultivated in a volume of nutrient medium of at least about 1,500 liters and containing in excess of 4 percent, preferably in excess of 6 percent, dry yeast solids. These and other strains are cultivated by an improved fermentation method comprising extending the maturation phase of the fermentation by one or more various techniques including exposing the yeast cells to a low-intensity light, slow feeding the cells with a rapidly metabolized energy source e.g. glucose, and replacing the rapidly metabolized energy source with a slowly metabolized energy source, e.g. gylcerol. The cells of these strains are incorporated into animal feeds, particularly feeds for salmonid fishes, to impart or enhance the red pigmentation of these animals and products made from these animals.Type: GrantFiled: November 13, 1995Date of Patent: July 13, 1999Assignee: Archer Daniels Midland CompanyInventors: Gunnard Kenneth Jacobson, Setsuko Omata Jolly, Joseph James Sedmak, Thomas Joseph Skatrud, John Marion Wasileski
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Patent number: 5877179Abstract: The present invention provides novel compounds and pharmaceutical compositions comprising such compounds useful for treating cystic fibrosis cells, wherein such compounds have the formula ##STR1## wherein (a) R.sub.1 and R.sub.3 are methyl, R.sub.7 is ethyl or cyclopropylmethyl, and R.sub.8 is cyclohexyl; (b) R.sub.1 and R.sub.3 are allyl, R.sub.7 is hydrogen and R.sub.8 is cyclohexyl, cyclohexylmethyl, or cycloheptyl; (c) R.sub.1 is allyl and R.sub.3 is methyl, R.sub.7 is hydrogen, and R.sub.8 is cyclohexyl; or (d) R.sub.1 is methyl, R.sub.3 is allyl, R.sub.7 is cyclopropylmethyl or ethyl, and R.sub.8 is cyclohexyl.Type: GrantFiled: November 22, 1994Date of Patent: March 2, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Harvey B. Pollard, Kenneth A. Jacobson
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Patent number: 5861405Abstract: The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A.sub.2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1## In compound (a), R.sub.1, R.sub.3, and R.sub.7 are methyl and X is one to three substituents, which may be the same or different and selected from the group consisting of amino, C.sub.1 -C.sub.4 alkylcarbonylamino, carboxy C.sub.2 -C.sub.4 alkylcarbonylamino, halo, C.sub.1 -C.sub.3 alkyloxy, amino C.sub.1 -C.sub.4 alkyloxy, C.sub.1 -C.sub.4 alkyloxy carbonylamino, amino C.sub.1 -C.sub.4 alkenyloxy, isothiocyanato, and diazonium tetrafluoroborate. In compound (b), R.sub.1, R.sub.3, and R.sub.7 are methyl, R.sub..beta. is hydrogen or methyl, and X is selected from the group consisting of R, C(.dbd.O)OR, and C(.dbd.O)NH--R, wherein R is a C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: November 7, 1994Date of Patent: January 19, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Yishai Karton, Carola Gallo-Rodriguez, Bilha Fischer, Philip J. M. van Galen, Michel Maillard
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Patent number: 5859019Abstract: Methods for reducing or preventing ischemic damage of the heart are disclosed. A preferred embodiment of the invention comprises the administration of a specific A.sub.2a receptor antagonist, 8-(3-chlorostyryl) caffeine, to patients suffering from ischemic damage or at risk for the same.Type: GrantFiled: March 7, 1997Date of Patent: January 12, 1999Assignees: Trustees of the University of Pennsylvania, National Institute of HealthInventors: Bruce T. Liang, Kenneth A. Jacobson
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Patent number: 5773423Abstract: The present invention provides N.sup.6 -benzyladenosine-5'-N-uronamide and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, and modified xanthine ribosides, as well as pharmaceutical compositions containing such compounds. The present invention also provides a method of selectively activating an A.sub.3 adenosine receptor in a mammal, which method comprises acutely or chronically administering to a mammal in need of selective activation of its A.sub.3 adenosine receptor a therapeutically effective amount of a compound which binds with the A.sub.3 receptor so as to stimulate an A.sub.3 receptor-dependent response.Type: GrantFiled: July 13, 1994Date of Patent: June 30, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Carola Gallo-Rodriguez, Philip J. M. van Galen, Dag K. J. E. von Lubitz, Heaok Kim Jeong
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Patent number: 5688774Abstract: The present invention provides A.sub.3 selective agonists, particularly, adenine compounds having selected substituents at the 2, 6, and 9 positions, and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, as well as pharmaceutical compositions containing such compounds. The present invention also provides a method of selectively activating an A.sub.3 adenosine receptor in a mammal, which method comprises acutely or chronically administering to a mammal in need of selective activation of its A.sub.3 adenosine receptor a therapeutically or prophylactically effective amount of a compound which binds with the A.sub.3 receptor so as to stimulate an A.sub.3 receptor-dependent response.Type: GrantFiled: February 28, 1995Date of Patent: November 18, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Heaok Kim Jeong, Suhaib M. Siddiqi, Carl R. Johnson, John A. Secrist, III, Kamal N. Tiwari
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Patent number: 5620676Abstract: The present invention provides certain novel adenosine triphosphate (ATP) analogs, pharmaceutical compositions, and methods of using such analogs in the treatment of septic shock and other disease conditions. Examples of the ATP analogs include the mono-, di- and triphosphates of adenosines with various selected substituents at the 2, 6, 8, and 9-positions, such as alkyl, alkylphenyl, phenylalkyl, S-alkyl, S-alkenyl, S-alkylcyano, S-phenyl, S-alkylphenyl, S-alkylamino, S-alkylthioalkyl, S-alkylthiocyanato, S-alkylaminophenyl, S-alkylnitrophenyl, hydroxy, bromo, fluoro, chloro, and aminoalkylamino. The present invention also provides pharmaceutical compositions of and methods of using certain xanthine and uracil derivatives for the above disease conditions. Examples of the xanthine derivatives include xanthines having alkyl or alkyltriphosphate substituents at the 1, 3, and 7-positions. Examples of the uracil derivatives include 5-fluoro- and 5-bromo uracil triphosphates.Type: GrantFiled: March 31, 1995Date of Patent: April 15, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Bilha Fischer, Michel Maillard
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Patent number: 5545627Abstract: Irreversible ligands for adenosine receptors are derived from agonist and antagonist functionalized congeners which contain electrophilic acylating and alkylating groups for reaction at nucleophilic residues of adenosine receptors. The ligands are based on 8-aryl-substituted xanthines as antagonists and on N.sup.6 -substituted adenosine as agonists.Type: GrantFiled: March 28, 1994Date of Patent: August 13, 1996Assignees: The United States of America as represented by the Department of Health and Human Services, Duke UniversityInventors: Kenneth A. Jacobson, Gary Stiles
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Patent number: 5498605Abstract: The adenosine derivatives which contain a sulfohydrocarbon substituent, as depicted in the formula: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 is a sulfohydrocarbon radical and W is --OCH.sub.2 --, --NHCH.sub.2 --, --SCH.sub.2 --, or --NH(C.dbd.O)--. Methods of preparing such compounds, as well as methods of using such compounds to treat ischemia or hypoxia in mammals and pharmaceutical compositions containing such compounds as the active ingredients, are also described.Type: GrantFiled: July 21, 1994Date of Patent: March 12, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Michel G. Maillard
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Patent number: 5453426Abstract: The present invention provides sulfur-containing xanthine derivatives which are 1,3-disubstituted with a C.sub.1 -C.sub.12 alkyl, which may be further substituted with a hydroxy, amino, or halo group, and are 8-substituted with either a cycloalkyl, furyl, thienyl, or substituted phenyl group. These derivatives possess increased selectivity or potency at adenosine receptors.Type: GrantFiled: December 20, 1994Date of Patent: September 26, 1995Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Wolfgang Pfleidover, John W. Daly, John L. Neumeyer