Thioether, Sulfoxide Or Sulfone Patents (Class 514/127)
  • Patent number: 11446319
    Abstract: A composition containing one or more materials selected from the group consisting of fatty acids, proteins, peptides, amino acids, vitamins, minerals, alcohols, sweeteners, acidulants, antioxidants, thickening stabilizer, and surfactants, and a flavonoid-cyclodextrin inclusion compound, wherein the inclusion compound contains an inclusion compound obtained by treating a flavonoid having a rhamnoside structure with an enzyme having rhamnosidase activity in the presence of a cyclodextrin. According to the present invention, the bitterness and the changes in color tones originated from flavonoids can be inhibited, and foodstuff or the like having an unpleasant taste can be improved, so that the present invention can be suitably utilized in fields such as medicaments, foodstuff, health foods, foods for specified health use, and cosmetics.
    Type: Grant
    Filed: October 3, 2018
    Date of Patent: September 20, 2022
    Assignee: TAIYO KAGAKU CO., LTD.
    Inventors: Masamitsu Moriwaki, Kentaro Kumoi, Ryo Nakagawa, Miki Sagisaka, Makoto Ozeki
  • Patent number: 11352381
    Abstract: The present invention relates to an improved synthesis of malathion. The presence of an acid facilitates the reaction between O,O-dimethyldithiophosphoric acid (O,O-DMDTPA) and maleate and leads to excellent product yield in shorter reaction time with fewer impurities.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: June 7, 2022
    Assignee: CHEMINOVA A/S
    Inventors: David Huang, Bolin Fan, Kevin Luo
  • Patent number: 9857386
    Abstract: The present invention inter alia provides a method, and use thereof, of diagnosing and/or predicting atherosclerosis or CVD by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control and has identified specific lipid markers that are more specific and sensitive in detecting and predicting atherosclerosis and CVD than currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, preventing and/or treating atherosclerosis or CVD. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of atherosclerosis or CVD.
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: January 2, 2018
    Assignee: ZORA BIOSCIENCES OY
    Inventors: Reijo Laaksonen, Kim Ekroos, Reini Hurme, Riikka Katainen
  • Patent number: 9597399
    Abstract: Methods of treatment using bendamustine formulations designed for small volume intravenous administration are disclosed. The methods conveniently allow shorter administration time without the active ingredient coming out of solution as compared to presently available formulations.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: March 21, 2017
    Assignee: EAGLE PHARMACEUTICALS, INC.
    Inventor: Srikanth Sundaram
  • Patent number: 9597398
    Abstract: Methods of treatment using bendamustine formulations designed for small volume intravenous administration are disclosed. The methods conveniently allow shorter administration time without the active ingredient coming out of solution as compared to presently available formulations.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: March 21, 2017
    Assignee: EAGLE PHARMACEUTICALS, INC.
    Inventor: Srikanth Sundaram
  • Patent number: 9597397
    Abstract: Methods of treatment using bendamustine formulations designed for small volume intravenous administration are disclosed. The methods conveniently allow shorter administration time without the active ingredient coming out of solution as compared to presently available formulations.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: March 21, 2017
    Assignee: EAGLE PHARMACEUTICALS, INC.
    Inventor: Srikanth Sundaram
  • Patent number: 9572888
    Abstract: Methods of treatment using bendamustine formulations designed for small volume intravenous administration are disclosed. The methods conveniently allow shorter administration time without the active ingredient coming out of solution as compared to presently available formulations.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: February 21, 2017
    Assignee: EAGLE PHARMACEUTICALS, INC.
    Inventor: Srikanth Sundaram
  • Patent number: 9572887
    Abstract: Methods of treatment using bendamustine formulations designed for small volume intravenous administration are disclosed. The methods conveniently allow shorter administration time without the active ingredient coming out of solution as compared to presently available formulations.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: February 21, 2017
    Assignee: EAGLE PHARMACEUTICALS, INC.
    Inventor: Srikanth Sundaram
  • Publication number: 20150087510
    Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I where R1?C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, X=hydrogen or halogen, Q=direct bond, a cyclopropylene or an anellated bicyclo[2.2.
    Type: Application
    Filed: September 29, 2014
    Publication date: March 26, 2015
    Inventors: Markus GEWEHR, Ulf GROEGER, Egon HADEN, Michael VONEND
  • Publication number: 20150038329
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 5, 2015
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Patent number: 8834848
    Abstract: A drug and device combination system used in a method for treatment of patients suffering from severe and oral corticosteroid-dependent asthma and other respiratory diseases requiring a treatment with orally administered steroids. The method for administration of the inhalable corticosteroid by a flow rate and volume regulated inhalation. The combination system of the inhalable corticosteroid and the device for regulating flow rate and volume of the inhalable corticosteroid and thus achieving delivery of said inhalable corticosteroid into the small airways of the lungs. The individually programmable device that assures safe and reproducible corticosteroid delivery compliant with treatment protocol.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: September 16, 2014
    Assignee: Activaero GmbH Research & Development
    Inventors: Bernard Muellinger, Gerhard Scheuch, Thomas Hofmann, Philipp Kroneberg
  • Patent number: 8796244
    Abstract: The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: August 5, 2014
    Assignee: Astex Therapeutics Ltd
    Inventors: Valerio Berdini, Maria Grazia Carr, Miles Stuart Congreve, Martyn Frederickson, Charlotte Mary Griffiths-Jones, Christopher Charles Frederick Hamlett, Andrew Madin, Christopher William Murray, Rajdeep Kaur Benning, Gordon Saxty, Emma Vickerstaffe, Andrew James Woodhead, Steven John Woodhead, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Patrick René Angibaud, Marian Williams
  • Patent number: 8729061
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R7 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Tanja Schulz-Gasch
  • Publication number: 20140018322
    Abstract: A synergistic antimicrobial composition comprising: (a) a hydroxymethyl-substituted phosphorus compound selected from the group consisting of tetrakis(hydroxymethyl)phoshponium salts and tris(hydroxymethyl)phosphine; and (b) tris(hydroxymethyl)nitromethane.
    Type: Application
    Filed: September 13, 2013
    Publication date: January 16, 2014
    Applicant: DOW GLOBAL TECHNOLOGIES LLC
    Inventor: Bei Yin
  • Patent number: 8609707
    Abstract: Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: December 17, 2013
    Assignee: Eagle Pharmaceuticals, Inc.
    Inventors: Nagesh R. Palepu, Philip Christopher Buxton
  • Patent number: 8536155
    Abstract: The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: September 17, 2013
    Assignee: Taro Pharmaceuticals North America, Inc.
    Inventors: Daniella Gutman, Wael Baidussi
  • Patent number: 8455431
    Abstract: The present invention is an inhibitor of the trypsin-like ?2/?2i sites of the proteasome. The inhibitor is characterized as being a peptide-based epoxyketone or vinyl sulfone that contains an arginine or 4-aminomethylene-L-phenylalanine at the C-terminus (i.e., at the P1 position). Methods for using the inhibitor to inhibit the activity of the ?2/?2i site of a proteasome and treat a proteasome-mediated disease or condition are also described.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: June 4, 2013
    Assignees: Trustees of Dartmout College, Leiden University
    Inventors: Alexei Kisselev, Dmitry V. Filippov, Herman Overkleeft
  • Publication number: 20130137571
    Abstract: The present invention relates to a novel crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: BASF SE
    Inventors: Heidi Emilia SAXELL, Peter ERK, Claude TARANTA, Thomas KROEHL, Gerhard COX, Martin SUKOPP, Stefan SCHERER, Antti OJALA, Gautam R. DESIRAJU, Rahul BANERJEE, Prashant M. BHATT
  • Publication number: 20120322654
    Abstract: The present invention relates to a mixture, comprising the succinate dehydrogenase inhibitor boscalid and at least one insecticidally active compound II selected from groups A) to D) as defined in the description in a synergistically effective amount, and to compositions comprising these mixtures.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 20, 2012
    Applicant: BASF SE
    Inventor: Markus Gewehr
  • Patent number: 8106033
    Abstract: Methods and compositions are provided for treating proliferative disorders, wherein the composition comprises at least one compound according to Formula I: wherein R1 is selected from the group consisting of —OH, —NH2, —NH—CH2—CO2H, —NH—CH(CH3)—CO2H, and —NH—C(CH3)2—CO2H, or a pharmaceutically acceptable salt of such a compound; and an anthracycline, e.g. doxorubicin, or a pharmaceutically acceptable salt thereof, or a platin, e.g. oxaliplatin, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: January 31, 2012
    Assignees: Temple University - Of The Commonwealth System of Higher Education, Mount Sinai School of Medicine
    Inventors: E. Premkumar Reddy, James F. Holland
  • Publication number: 20120021901
    Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from the class of the organophosphates or carbamates, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.
    Type: Application
    Filed: March 25, 2009
    Publication date: January 26, 2012
    Applicant: BAYER CROPsCIENCE AG
    Inventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
  • Patent number: 7977324
    Abstract: The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: July 12, 2011
    Assignee: Taro Pharmaceuticals North America, Inc.
    Inventors: Daniella Gutman, Wael Baidussi
  • Publication number: 20110098176
    Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I where R1=C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, X=hydrogen or halogen, Q=direct bond, a cyclopropylene or an anellated bicyclo[2.2.
    Type: Application
    Filed: July 2, 2009
    Publication date: April 28, 2011
    Applicant: BASF SE
    Inventors: Markus Gewehr, Ulf Groeger, Egon Haden, Michael Vonend
  • Patent number: 7932242
    Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
    Type: Grant
    Filed: March 15, 2005
    Date of Patent: April 26, 2011
    Assignees: Temple University - Of The Commonwealth System of Higher Education, Onconova Therapeutics Inc.
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
  • Publication number: 20100298145
    Abstract: The present invention relates to novel compounds of the formula (I), in which W, X, Y, Z, G, A and t have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the spiroheterocyclic tetronic acid 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 insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: May 19, 2010
    Publication date: November 25, 2010
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Reiner Fischer, Stefan Lehr, Olga Malsam, Arnd Voerste
  • Publication number: 20100261670
    Abstract: There is provided a composition comprising the reaction product of: (a) one or more phosphate derivatives of one or more hydroxylated actives; and (b) one or more complexing agents selected from the group consisting of amphoteric surfactants, cationic surfactants, amino acids having nitrogen functional groups and proteins rich in these amino acids.
    Type: Application
    Filed: April 27, 2010
    Publication date: October 14, 2010
    Inventors: Simon Michael West, Robert J. Verdicchio, David Kannar
  • Patent number: 7781488
    Abstract: The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: August 24, 2010
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventors: Paolo Botti, Matteo Villain, Sonia Manganiello, Hubert Gaertner
  • Patent number: 7560445
    Abstract: The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: July 14, 2009
    Assignee: Taro Pharmaceuticals North America, Inc.
    Inventors: Daniella Gutman, Wael Baidussi
  • Patent number: 7468360
    Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.
    Type: Grant
    Filed: August 8, 2007
    Date of Patent: December 23, 2008
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20080058290
    Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
    Type: Application
    Filed: March 15, 2005
    Publication date: March 6, 2008
    Applicants: TEMPLE UNIVERSITY - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION, ONCONOVA THERAPEUTICS INC.
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy, Stanley C. Bell
  • Patent number: 7176192
    Abstract: This invention relates to a method of treating a patient suffering from ionizing radiation exposure, or of treating a patient about to undergo ionizing radiation therapy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: February 13, 2007
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventor: Frederick H. Hausheer
  • Patent number: 7060692
    Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (43) listed in the disclosure.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: June 13, 2006
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Publication number: 20040152774
    Abstract: A method of reducing the risks of tissue extravasation injury associated with intravenous drug therapy is disclosed. The method of this invention includes administering effective amounts of specific sulfur-containing drug agents according to Formula I herein to a patient at risk of extravasation injury.
    Type: Application
    Filed: February 4, 2003
    Publication date: August 5, 2004
    Inventor: Frederick H. Hausheer
  • Patent number: 6722062
    Abstract: The present invention is directed to a method for purifying polysaccharides capable of inducing the production of high titers of opsonic antibodies that kill strains of enterococcal bacteria. In addition, the invention is directed to the antigens produced by this purification method and to vaccines which utilize such antigens.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: April 20, 2004
    Assignee: The Brigham and Women's Hospital, Inc.
    Inventors: Gerald B. Pier, Johannes Huebner, Ying Wang, Lawrence Madoff
  • Publication number: 20040019232
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Application
    Filed: November 6, 2002
    Publication date: January 29, 2004
    Inventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
  • Publication number: 20040014730
    Abstract: This invention provides for pharmaceutical formulations of compounds that are useful as protective agents when administered to patients also receiving anti-infective drugs, such as antimicrobials, antifungals, or antivirals. The invention also includes methods of reducing the toxicity of various anti-infective agents by administering an effective amount of the protective agent to a patient receiving one or more anti-infective agents. The compounds that are useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.
    Type: Application
    Filed: July 10, 2002
    Publication date: January 22, 2004
    Inventor: Frederick Hausheer
  • Patent number: 6649646
    Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: November 18, 2003
    Assignee: BASF Aktiengesellschaft
    Inventor: Toshiki Fukuchi
  • Publication number: 20030153536
    Abstract: The use of compounds of the formula 1
    Type: Application
    Filed: October 25, 2002
    Publication date: August 14, 2003
    Inventors: Mitchell Glass, Patricia K. Somers, David B. Edwards
  • Publication number: 20030092681
    Abstract: This invention relates to a method of treating a patient suffering from radiation exposure, or of prophylactically treating a patient about to undergo radiation therapy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
    Type: Application
    Filed: October 26, 2001
    Publication date: May 15, 2003
    Inventor: Frederick H. Hausheer
  • Patent number: 6525037
    Abstract: This invention relates to a method of treating patients afflicted with atherosclerosis or to prevent the development of atherosclerosis in patients assessed to be high risk of developing the disease. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: February 25, 2003
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Seetharamulu Peddaiahgari
  • Patent number: 6498151
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: December 24, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Chun Sing Li, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Cheuk Kun Lau, Patrick Roy, Michel Therien, Zhaoyin Wang, Claude Dufresne, Rejean Fortin
  • Patent number: 6495533
    Abstract: The present invention relates to phosphoric acid derivatives represented by general formula (I), wherein each symbol is as defined in the description and nontoxic salts thereof. Because of having a TNF&agr; production inhibitory effect, the compounds represented by general formula (I) are useful as preventives and/or remedies for rheumatoid arthritis, ulcerative colitis, Crohn's disease, hepatitis, sepsis, hemorrhagic shock, multiple sclerosis, cerebral infarction, diabetes, interstitial pneumonia, uveitis, pain, glomerulonephritis, HIV-associated diseases, cachexia, myocardial infarction, chronic heart failure, oral aphtha, Hansen's disease, infection, etc.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: December 17, 2002
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Toshiaki Matsui, Nagashige Omawari
  • Patent number: 6468993
    Abstract: This invention relates to a method of treating patients afflicted with osteoporosis. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
    Type: Grant
    Filed: October 4, 1999
    Date of Patent: October 22, 2002
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventor: Frederick H. Hausheer
  • Patent number: 6468963
    Abstract: Formulations and methods for reducing the unwanted toxicity and complications associated with treatments for diabetes mellitus. The formulations include co-formulations of an anti-diabetic agent and a toxicity reducing agent of the formula described in the specification. The methods include administration of effective amounts of the anti-diabetic agent and the toxicity reducing agent to safely treat the diabetic patient.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: October 22, 2002
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Aulma Parker, Susan E. Hamilton
  • Patent number: 6465444
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: October 15, 2002
    Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd.
    Inventors: Christopher Bayly, Mitsuru Ohkubo
  • Patent number: 6444657
    Abstract: The present invention relates to methods of using NAALADase inhibitors to regulate TGF-&bgr; and to treat neurodegenerative disorders, extracellular matrix formation disorders, cell-growth related diseases, infectious diseases, immune related diseases, epithelial tissue scarring, collagen vascular diseases, fibroproliferative disorders, connective tissue disorders, inflammatory diseases, respiratory distress syndrome and infertility.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: September 3, 2002
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Barbara S. Slusher, Xi-Chun May Lu, Krystyna Wozniak
  • Publication number: 20020115643
    Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1
    Type: Application
    Filed: April 12, 2001
    Publication date: August 22, 2002
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Publication number: 20020103163
    Abstract: The present invention relates to acetylenic aryl sulfonamide thiols which act as inhibitors of TNF-&agr; converting enzyme (TACE). The compounds of the present invention are useful in disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
    Type: Application
    Filed: August 30, 2001
    Publication date: August 1, 2002
    Applicant: American Cyanamid Company
    Inventors: Jeremy I. Levin, James M. Chen
  • Publication number: 20020099035
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: January 24, 2001
    Publication date: July 25, 2002
    Inventors: Vincent P. Sandanayaka, Arie Zask, Aranapakam M. Venkatesan, Jannie L. Baker, Lalitha Krishnan, Sreenivasulu Megati, Joseph Zeldis
  • Publication number: 20020082242
    Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus.
    Type: Application
    Filed: April 27, 2001
    Publication date: June 27, 2002
    Inventors: Louis S. Kucera, Ronald A. Fleming, Khalid S. Ishaq, Gregory L. Kucera, Susan L. Morris-Natschke