Two Ring Sulfurs In The Hetero Ring Patents (Class 514/436)
  • Patent number: 11005741
    Abstract: An apparatus including at least one processing circuitry, and at least one memory for storing instructions to be executed by the processing circuitry, wherein the at least one memory and the instructions are configured to, with the at least one processing circuitry, cause the apparatus at least: to determine an abnormal operation of an external application with which at least one communication element has established a communication connection; to decide on a change of an uplink traffic to the external application; and to selectively control a communication of the at least one communication element to the external application by providing control information for the at least one communication element, the control information reflecting the decision to change the uplink traffic to the external application.
    Type: Grant
    Filed: October 31, 2014
    Date of Patent: May 11, 2021
    Assignee: NOKIA SOLUTIONS AND NETWORKS OY
    Inventor: John Juha Antero Rasanen
  • Patent number: 9994519
    Abstract: The present invention relates to synthetic organic antioxidants of small molecules. The novel dithiol-containing compounds in this invention possess strongest possible capability as both scavenger for free radicals and antioxidant. This invention is directed to novel molecules as prodrugs of the novel dithiol-containing compounds, their rational design, their feasible preparation route by means of synthetic organic chemistry, and their potential uses in application to treatment and/or prevention of major diseases associated with oxidative stress, such as Alzheimer's disease, Parkinson's disease, cancer, diabetes, HIV, acne, cardiovascular disease, renal disease, hypertension, hypercholesterolemia, hyperlipidemia, rheumatoid arthritis, inflammation, pain, aging, stroke, cataract, glaucoma, age-related macular degeneration, etc.
    Type: Grant
    Filed: April 18, 2013
    Date of Patent: June 12, 2018
    Inventor: Yansong Lu
  • Patent number: 9801905
    Abstract: Through the use of a combination of naturally occurring substances, application of mechanical energy by way of exercise, and application of a pulsed electromagnetic field (PEMF), new bone formation at lines of stress can be promoted. This bone forming activity is useful in the treatment and prevention of osteoporosis. The naturally occurring substances consist of organic sulphur, antioxidants, and amino acids. These substances are preferably administered orally. In preferred embodiments, the antioxidant is alpha-lipoic acid, and the amino acid is selected from the group consisting of lysine, glutamine, and mixtures thereof.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: October 31, 2017
    Inventors: Hossam Abdel Salam El Sayed Mohamed, Houda Abdul Rahman M. Al Mansour
  • Patent number: 9565280
    Abstract: An electronic device for rendering a display unit antifungal. The electronic device includes a body including a display unit; and an antifungal cover that is removeably attached to the body, the antifungal cover including an antifungal module on one surface thereof. If the antifungal cover covers the display unit, the display unit projects a wavelength of light that activates an antifungal property of the antifungal module.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: February 7, 2017
    Assignee: Samsung Electronics Co., Ltd
    Inventor: Jeong-Hun Seo
  • Publication number: 20150080386
    Abstract: Disclosed are compounds and pharmaceutical compositions that are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 19, 2015
    Inventors: Keizo Koya, Teresa Kowalczyk Przewloka, Shoujun Chen, Jun Jiang
  • Publication number: 20140243385
    Abstract: Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract. Also disclosed are novel mercaptan compounds, particularly those including a photolabile protecting group, as well as methods of using the compounds for the prevention and treatment of ocular damage and disease.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 28, 2014
    Applicant: Encore Health, LLC
    Inventors: William GARNER, Margaret Garner, Ronald D. Blum
  • Patent number: 8785475
    Abstract: Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: July 22, 2014
    Assignee: Cornerstone Pharmaceuticals, Inc.
    Inventors: Paul Bingham, Tom Kwok, Zuzana Zachar
  • Patent number: 8785451
    Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), wherein the variables are as defined herein, and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: July 22, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
  • Patent number: 8729118
    Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: May 20, 2014
    Assignee: Bayer CropScience AG
    Inventors: Thomas Seitz, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Publication number: 20140135217
    Abstract: The present invention relates to the use of 2,3,5,6-tetracyano-[1,4]dithiine and the N-oxides and the salts thereof for combating phytopathogenic fungi on cultivated plants, and to seeds coated with 2,3,5,6-tetracyano-[1,4]dithiine. The invention also relates to methods for combating harmful fungi, comprising treating the plants or seeds to be protected against fungal attack.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 15, 2014
    Applicant: BASF SE
    Inventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Mueller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
  • Publication number: 20140121103
    Abstract: The present invention relates to synergistic mixtures comprising at least one compound I and at least one active compound II as defined herein and to the use of these mixtures for combating phytopathogenic fungi, and to seeds coated with at least one such mixture. The invention also relates methods for combating harmful fungi using such mixtures.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: BASF SE
    Inventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
  • Publication number: 20130345268
    Abstract: The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NF1 gene such as neurofibromatosis type I, fungal infections such as those caused by Candida albicans, and proliferative disorders such as glioblastoma.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 26, 2013
    Applicants: The Trustees of Dartmouth College, Children's Hospital Medical Center
    Inventors: Nancy Ratner, Yolanda Sanchez, Gunnar Johansson, William Seibel
  • Publication number: 20130316906
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: October 28, 2011
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
  • Publication number: 20130296315
    Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.
    Type: Application
    Filed: March 11, 2013
    Publication date: November 7, 2013
    Inventor: Bayer CropScience AG
  • Publication number: 20130251647
    Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.
    Type: Application
    Filed: September 20, 2012
    Publication date: September 26, 2013
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel, Ralf Pelzer
  • Patent number: 8476233
    Abstract: The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as ulcerative colitis. Another aspect of the subject invention concerns compositions formulated for administration as an enema. The subject invention also concerns compositions formulated for oral administration. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient. In another embodiment, compounds or compositions are orally administered.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: July 2, 2013
    Assignee: Therapeutic Research, LLC
    Inventor: Jay Pravda
  • Patent number: 8470861
    Abstract: The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.
    Type: Grant
    Filed: January 27, 2010
    Date of Patent: June 25, 2013
    Assignee: University of Rochester
    Inventors: Marion W. Anders, James L. Robotham, Shey-Shing Sheu, Paul Spencer Brookes, Jalil Shojaie, Leif Olson, Richard L. Parton
  • Publication number: 20120329731
    Abstract: In one embodiment the invention provides a method of combating cyanide poisoning, which comprises administering to a subject a compound capable of releasing 3-mercapto-pyruvate in vivo. In other embodiments the invention also provides pharmaceutical compositions comprising a compound capable of releasing 3-mercaptopyruvate in vivo, as well as novel compounds that are capable of releasing 3-mercaptopyruvate in vivo.
    Type: Application
    Filed: October 13, 2011
    Publication date: December 27, 2012
    Inventors: Herbert T. Nagasawa, David J.W. Goon, Daune L. Crankshaw, Robert Vince
  • Publication number: 20120302581
    Abstract: The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NF1 gene such as neurofibromatosis type I, fungal infections such as those caused by Candida albicans, and proliferative disorders such as glioblastoma.
    Type: Application
    Filed: August 12, 2011
    Publication date: November 29, 2012
    Inventors: Nancy Ratner, Yolanda Sanchez, Gunnar Johansson, William Seibel
  • Publication number: 20120270917
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: July 30, 2010
    Publication date: October 25, 2012
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 8288378
    Abstract: The present invention relates to the use of agents that inhibit the toxic effects of amyloid oligomers by increasing intracellular levels of phosphoinositol 4-phosphate (PI(4)P, or “PIP”) and/or phosphotidylinositol 4,5-biphosphate (PI(4,5)P2 or “PIP2”), the use of such agents for the treatment of neurodegenerative diseases, methods of treating neurodegenerative diseases by administration of agents which alter lipid metabolism, and methods of identifying agents which alter the association of presenilins with ?-secretase and lipid rafts.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: October 16, 2012
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Tae-Wan Kim, Gilbert Di Paolo, Min Suk Kang, Diego Berman, Laura Beth Johnson McIntire
  • Publication number: 20120142676
    Abstract: Novel derivatives of dihydro-1,4,2-oxathiazine and dihydro-1,4-dithiine oxides, more particularly, novel derivatives of dihydro-1,4,2-oxathiazine and dihydro-1,4-dithiine oxides that target cysteine residues of biomolecules of pharmacological importance are provided as pharmaceutically useful compounds, for example, as anticancer, antiinfectious, antigastric acid secretion, antiosteoporosic, and antiinflammatory agents.
    Type: Application
    Filed: July 27, 2011
    Publication date: June 7, 2012
    Inventors: Gaik-Lean Chee, Walter G. Brouwer, Ewa Osika, Brian B. Hasinoff, A. David Brewer
  • Publication number: 20110294662
    Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.
    Type: Application
    Filed: April 14, 2011
    Publication date: December 1, 2011
    Applicant: Bayer CropScience AG
    Inventors: Thomas SEITZ, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Publication number: 20100168198
    Abstract: The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.
    Type: Application
    Filed: January 27, 2010
    Publication date: July 1, 2010
    Inventors: Marion W. Anders, James L. Robotham, Shey-Shing Sheu, Paul Spencer Brookes, Jalil Shojaie, Leif Olson, Richard L. Parton
  • Publication number: 20100137403
    Abstract: A method for enhancing cognition or inhibiting cognitive decline in a subject comprises selecting a Ca2+ channel blocker that is effective, when administered intravenously to an animal in a nontoxic amount, to increase NF-?B expression in the brain of the animal; and administering the selected Ca2+ channel blocker to the subject, via a systemic route that affords an adequate therapeutic window for cognition-enhancing or cognitive decline-inhibiting effectiveness of the selected Ca2+ channel blocker, in an amount within the therapeutic window. The selected Ca2+ channel blocker can be, for example, tiapamil or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: July 9, 2009
    Publication date: June 3, 2010
    Inventors: Scott Malstrom, John J. Byrnes, Michelle Wolfe
  • Patent number: 7598289
    Abstract: The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae and pharmaceutically acceptable salts, amides, esters, and ethers thereof, wherein: Ar1, Ralk, —ORO, and -Q are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds. The compounds inhibit osteoclast survival, formation, and/or activity, and inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, and are useful in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, aseptic loosening of prosthetic implants, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: October 6, 2009
    Assignee: The University Court of the University of Aberdeen
    Inventors: Stuart H. Ralston, Iain R. Greig, Aymen I. I. Mohamed, Robert J. Van 'T Hof
  • Patent number: 7592337
    Abstract: Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Chixu Chen, Nicholas D. P. Cosford, Brian W. Eastman, Dehua Huang, Steve F. Poon, Thomas S. Reger, Jeffrey R. Roppe, Nicholas D. Smith
  • Patent number: 7572825
    Abstract: The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae: (1) (2) wherein: Ar1 is independently a biphenyl, phenanthryl, fluorenyl, or carbazolyl, and is optionally substituted; Ralk is independently a C2-10alkylene group, and is optionally substituted; —ORO, if present, is independently —OH or —ORK; —ORK, if present, is independently selected from: —O—RK1; —O—C(?O)RK2; —O—C(?O)ORK3; —O—S(?O)2ORK4; Q is independently —OH or —OROT; wherein: —OROT, if present, is independently selected from: —O—RE1; —O—C(?O)—RE2; —O—C(?O)—O—RE3; —O—C(?O)—O—SO3RE4; —O—C(?O)—O—(CH2)n—COORE5; —O—C(?O)—(CH2)n—NRN1RN2; —O—C(?O)—(CH2)n—NH—C(?O)RE6; —O—C(?O)—(CH2)n—C(?O)—NRN3RN4; —O—P(?O)(ORE7)(ORE8); —O—RPA; RPA, if present, is an organic group which incorporates a phosphonic acid group; with the proviso that if —OROT is —O—RE1, then RE1 is
    Type: Grant
    Filed: May 6, 2004
    Date of Patent: August 11, 2009
    Assignee: The University Court of the University of Aberdeen
    Inventors: Stuart H. Ralston, Iain R. Greig, Aymen I. I. Mohamed, Robert J. Van 'T Hof
  • Publication number: 20090197865
    Abstract: In one embodiment the invention provides a method of combating cyanide poisoning, which comprises administering to a subject a compound capable of releasing 3-mercapto-pyruvate in vivo. In other embodiments the invention also provides pharmaceutical compositions comprising a compound capable of releasing 3-mercaptopyruvate in vivo, as well as novel compounds that are capable of releasing 3-mercaptopyruvate in vivo.
    Type: Application
    Filed: June 28, 2007
    Publication date: August 6, 2009
    Inventors: Herbert T. Nagasawa, David J.W. Goon, Daune L. Crankshaw, Robert Vince
  • Publication number: 20090192212
    Abstract: Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract.
    Type: Application
    Filed: February 23, 2009
    Publication date: July 30, 2009
    Applicant: Encore Health, LLC
    Inventors: William Garner, Margaret Garner, Ronald D. Blum
  • Publication number: 20080312186
    Abstract: The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae and pharmaceutically acceptable salts, amides, esters, and ethers thereof, wherein: Ar1, Ralk, —ORO, and -Q are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds. The compounds inhibit osteoclast survival, formation, and/or activity, and inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, and are useful in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, aseptic loosening of prosthetic implants, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.
    Type: Application
    Filed: August 19, 2008
    Publication date: December 18, 2008
    Applicant: The University Court of the University of Aberdeen
    Inventors: Stuart H. RALSTON, Iain R. GREIG, Aymen I. I. MOHAMED, Robert J. VAN 'T HOF
  • Publication number: 20080262034
    Abstract: Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.
    Type: Application
    Filed: April 17, 2008
    Publication date: October 23, 2008
    Inventors: PAUL BINGHAM, TOM KWOK, ZUZANA ZACHAR
  • Patent number: 7115651
    Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein R0–R4, Z, X, A—B, D—E, G—J, and K—L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
    Type: Grant
    Filed: August 24, 2001
    Date of Patent: October 3, 2006
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Robert M. Garbaccio, Daniel K. Baeschlin, Shawn J. Stachel, David Solit, Neal Rosen
  • Patent number: 7074422
    Abstract: Fungicidal mixtures, comprising A) the compound of the formula I and B) the compound of the formula II in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compounds I and II and the use of the compounds I and II for preparing such mixtures are described.
    Type: Grant
    Filed: June 30, 2003
    Date of Patent: July 11, 2006
    Assignee: BASF Aktiengesellschaft
    Inventors: Eberhard Ammermann, Reinhard Stierl, Ulrich Schöfl, Klaus Schelberger, Maria Scherer, Michael Henningsen, Randall Even Gold
  • Patent number: 6916835
    Abstract: Compounds and methods for mitigating neurodegeneration, effecting neuroprotection and/or effecting cognition enhancement in a subject are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic compound comprising a nitrate ester, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: July 12, 2005
    Assignee: Queen's Uninversity at Kingston
    Inventors: Gregory R. J. Thatcher, Brian M. Bennett, James N. Reynolds, Roland J. Boegman, Khem Jhamandas
  • Patent number: 6900338
    Abstract: The present invention provides novel compounds having scavenging and anti-ROS properties and pharmaceutical composition comprising these compounds for treatment of conditions associated with oxidative stress or free radical injury. The compounds of the invention are of general formula (I).
    Type: Grant
    Filed: November 25, 1999
    Date of Patent: May 31, 2005
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventor: Abdullah Haj-Yehia
  • Patent number: 6664287
    Abstract: This invention comprises administering to a human or animal in need of treatment an effective amount of an antioxidant lipoic acid derivative and/or pharmaceutically acceptable salts and solvates thereof for the treatment or prevention of pathological (inflammatory, proliferative and degenerative diseases, e.g. diabetes mellitus, atherosclerosis, Alzheimer's disease and chronic viral diseases) and non-pathological (e.g. skin aging and wrinkle formation) conditions caused by oxidative damage. Methods of synthesizing novel antioxidant lipoic acid derivatives and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are described. Another aspect of this invention is the use of these antioxidant compositions for the protection of skin from damage caused by ultraviolet radiation and dessication, and to provide improved skin feel by desquamating, cleansing and clarifying the skin.
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: December 16, 2003
    Assignee: Bethesda Pharmaceuticals, Inc.
    Inventors: Mitchell Allen Avery, Harrihar A. Pershadsingh
  • Patent number: 6649639
    Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: November 18, 2003
    Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
  • Patent number: 6635650
    Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: October 21, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
  • Patent number: 6583161
    Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: June 24, 2003
    Assignee: Tularik Inc.
    Inventor: Julio C. Medina
  • Patent number: 6562861
    Abstract: Compounds I-III wherein U is CH, O, or S; Z is mono- or di-substituted carbon; R is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, CH(SCH3)3, esters; R1 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl; RR1 is O; n is 0-4; R2, R3 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkyl; R4 is (CH2)nOH, (CH2)nNH2, substituted alkyl were prepd. as neuraminidase inhibitors. Thus, (1R,3R,4R,1′S)-(−)-(1′-acetylamino-2 ′-ethyl)butyl-4-(aminoimino)methylaminocyclopentan-1-carboxylic acid was prepd. and tested in vitro as neuraminidase inhibitor (IC50<1.mu.M).
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: May 13, 2003
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, John A. Montgomery
  • Patent number: 6512003
    Abstract: Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: January 28, 2003
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Chen Mao, He Huang
  • Patent number: 6440985
    Abstract: Methods are provided for the treatment and prophylaxis of viral infection and disease associated with such infection.
    Type: Grant
    Filed: September 3, 1999
    Date of Patent: August 27, 2002
    Assignee: ViroPharma Incorporated
    Inventors: Thomas R. Bailey, Dorothy C. Young
  • Publication number: 20020110604
    Abstract: A novel formulation is provided that serves to synergistically inhibit the generation of free radicals and oxidative stress in animals. The formulation comprises as a first component a carotenoid species, and, as a second component, at least one member selected from the group consisting of lipoic acid, dihydrolipoic acid (DHLA), a stilbene species, ergothioneine, a flavone species, a triterpene species, ascorbic acid and derivatives thereof.
    Type: Application
    Filed: August 9, 2001
    Publication date: August 15, 2002
    Applicant: Ashni Naturaceuticals, Inc.
    Inventors: John G. Babish, Terrence Howell
  • Patent number: 6407136
    Abstract: The invention is directed to 1,4-dithiin- and 1,4-dithiepin-1,1,4,4-tetroxide derivatives useful as galanin receptor antagonists for treating disorders of the central nervous system. Pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions such as an eating disorder, obesity, bulimia nervosa, anorexia nervosa, binge eating, diabetes, dyslipidemia, hypertension, memory loss, sleep disturbances, pain, depression, anxiety, Alzheimer's disease, senile dementia, cerebral hemorrhage, or diarrhea are also described.
    Type: Grant
    Filed: May 2, 2000
    Date of Patent: June 18, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Malcolm K. Scott, Daniel H. S. Lee, Allen B. Reitz, Tina Morgan Ross, Haou-Yan Wang
  • Patent number: 6358960
    Abstract: The novel amidino derivatives of the formula (I): wherein all the symbols are as in specification defined; have an inhibitory activity of a blood coagulation factor VIIa and are useful for treatment and/or prevention of several angiopathy caused by enhancing a coagulation activity, such as disseminated intravascular coagulation, coronary thrombosis, cerebral infarction, cerebral embolism, transient ischemic attack, cerebrovascular disorders, pulmonary vascular diseases, deep venous thrombosis, peripheral arterial obstruction, thrombosis after artificial vascular transplantation and artificial valve transplantation, post-operative thrombosis, reobstruction and restenosis after coronary artery bypass operation, reobstruction and restenosis after PTCA or PTCR, thrombosis by extracorporeal circulation and procoagulative diseases such as glomerlonephriitis.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: March 19, 2002
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuhiko Senokuchi, Koji Ogawa
  • Publication number: 20020025310
    Abstract: A dietary supplement for promoting healthy joints and joint tissues is disclosed. The dietary supplement comprises a member selected from the group consisting of niacinamide, niacin, and mixtures thereof and an antioxidant nutrient. Illustrative antioxidant nutrients include N-acetylcysteine, lipoic acid, coenzyme Q10, vitamin E, carotenoids, and zinc. The dietary supplement supports optimal function and health of joints and joint tissues by interrupting a cascade of events involving reactive oxygen species, cytokines, and poly(ADP-ribose) synthetase, which self-amplifying, positive feed-forward cycle is inversely correlated with joint tissue integrity. A method for promoting healthy joints and joint tissues is also described.
    Type: Application
    Filed: February 2, 2001
    Publication date: February 28, 2002
    Inventor: Jeffrey S. Bland
  • Patent number: 6346626
    Abstract: The invention concerns the compounds of formula I wherein R1 and R2 independently are hydrogen, acyl, alkoxycarbonyl or alkyl; either the sulfamoyloxy side chain is bound to the 6 position; R3 is alkyl; alkenyl; alkinyl; a cycloalkyl moiety optionally substituted by alkyl, alkoxy or halogen; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; or is 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; and R4 is hydrogen; alkyl; hydroxy; or alkoxy; or the sulfamoyloxy side chain is bound to the 7 position; R3 has the significance indicated above for R4; and R4 has the significance indicated above for R3; X is O or S; and the symbol - - - is a single or a double bond; in free form or salt form. They can be prepared by sulfamoylation of corresponding hydroxylated compounds, by reduction and/or by N-substitution. They are indicated for use as pharmaceuticals, particularly in the prophylactic or curative treatment of illnesses responsive to steroid sulfatase inhibition.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: February 12, 2002
    Assignee: Novartis AG
    Inventors: Andreas Billich, Peter Nussbaumer, Erwin Schreiner, Ingeborg Schuster
  • Patent number: 6342517
    Abstract: Novel thienopyran compounds are disclosed, useful as anti-hypertensive agents and for asthma treatment. One group of the compounds has a heterocyclic ring spiro-connected at the 7-position of the thienopyran ring structure. Use of thienopyran compounds in hair growth modulation is described.
    Type: Grant
    Filed: December 3, 1999
    Date of Patent: January 29, 2002
    Assignee: Cambridge Bioclinical Limited
    Inventors: Peter Esch, Franz Rovenszky, Robertson Towart, Thomas Christoph, Michael Hartmann, George Terence Evelyn Kealey
  • Patent number: 6331554
    Abstract: Picornaviral 3C protease inhibitors of formula I, obtainable by chemical synthesis, that inhibit or block the biological activity of the picornaviral 3C protease are described. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: December 18, 2001
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou