Px- Bonded Directly To 1,3-diazine At 2- Position (x Is Chalcogen) Patents (Class 514/87)
  • Patent number: 8940927
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 8816082
    Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: August 26, 2014
    Assignee: The Royal Institution for the Advancement of Learning/McGill University
    Inventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
  • Patent number: 8236334
    Abstract: Disclosed is a method for protecting a tree from insects by injecting the tree with a fungicide and/or an antibiotic, and applying a composition to the surface of the tree, said composition comprising water, an insect repellent, an antihistamine, and an insect poison.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: August 7, 2012
    Inventor: James S. Bass
  • Patent number: 7192905
    Abstract: Combination of a cytochrome P450 monooxygenase inducer with an organophosphate pesticide (insecticide or acaracide) provides effective control of ticks and flies, particularly against organophosphate-resistant strains of the ticks and flies. In use, a pesticidally effective amount of a composition of the cytochrome P450 monooxygenase inducer and organophosphate pesticide is applied to the locus of the targeted tick or fly.
    Type: Grant
    Filed: June 20, 2003
    Date of Patent: March 20, 2007
    Assignee: The United States of America as represented by the Secretary of Agriculture
    Inventors: Andrew Y. Li, John Allen Miller
  • Patent number: 6919322
    Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: July 19, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Publication number: 20030171335
    Abstract: The invention provides antisense antiviral compounds and methods of their use in inhibition of growth of viruses of the picornavirus, calicivirus, togavirus and flavivirus families, as in treatment of a viral infection. The antisense antiviral compounds are substantially uncharged oligomers having a targeting base sequence that is substantially complementary to a viral target sequence which spans the AUG start site of the first open reading frame of the viral genome.
    Type: Application
    Filed: October 16, 2002
    Publication date: September 11, 2003
    Inventors: David A. Stein, Douglas E. Skilling, Patrick L. Iversen, Alvin W. Smith
  • Publication number: 20030027799
    Abstract: The present invention provides a novel method for treating a patient with cancer comprising administering to the patient a therapeutically effective amount of cisplatin and a compound having the formula I: 1
    Type: Application
    Filed: March 28, 2002
    Publication date: February 6, 2003
    Applicant: Shire BioChem Inc.
    Inventor: Jacques Jolivet
  • Publication number: 20030027785
    Abstract: The present invention is directed to a method of altering the amount or composition of synovial fluids secreted from joints in a subject in need of such treatment. The method comprises administering to a subject a pharmaceutical composition comprising a P2Y purinergic receptor agonist in an amount effective to alter the amount or composition of synovial fluids. The P2Y purinergic receptor agonist is administered in an amount effective to stimulate secretion of synovial fluid, lubricin, hyaluronic acid, or surface-active phospholipids; to enhance joint lubrication; or to treat osteoarthritis. The pharmaceutical compositions useful in the present invention comprise a P2Y purinergic receptor agonist of Formula I and include, but are not limited to: uridine-, adenosine-, cytidine-5′-di- or triphosphates, dinucleoside polyphosphates, and analogs thereof. The invention is useful for treating conditions associated with reduced joint lubrication and joint stiffness, such as osteoarthritis.
    Type: Application
    Filed: June 25, 2002
    Publication date: February 6, 2003
    Inventors: Matthew S. Cowlen, Benjamin R. Yerxa, Arthur C. Jones, Edward G. Brown
  • Patent number: 6300356
    Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: October 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
  • Patent number: 6201002
    Abstract: Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. Additionally, losartan potassium has been shown to reduce the need for hospitalization of symptomatic heart failure patients.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: March 13, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Polly A. Beere, Paul I. Chang, Bertram Pitt, Eva J. Rucinska, Robert Segal, Divakar Sharma, Duane B. Snavely
  • Patent number: 6200961
    Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: March 13, 2001
    Assignee: Aquatrols Corporation of America, Inc.
    Inventors: Stanley J. Kostka, Rennan Pan
  • Patent number: 6040299
    Abstract: There is disclosed a cold storage stabilized organophosphorus insecticide formulation. The formulation comprises a solid carrier and between approximately 2% and 40% by weight of the ultimate formulation of a nominally solid organophosphorus insecticide and between approximately 0.5% and 10% by weight of the ultimate formulation of a stabilizer compound selected from cyclohexanone and N-methylpyrrolidone. A method of making the cold storage stabilized organophosphorus insecticide formulation is also disclosed.
    Type: Grant
    Filed: October 23, 1998
    Date of Patent: March 21, 2000
    Assignee: Griffin LLC
    Inventor: Hamid Ullah
  • Patent number: 5880111
    Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 9, 1999
    Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
  • Patent number: 5543396
    Abstract: Peptidyl derivatives of diesters of .alpha.-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like, trypsin-like, elastase-like, and dipeptidyl peptidase IV specificity and their roles as anti-inflammatory agents, anticoagulants, and anti-tumor agents.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: August 6, 1996
    Assignee: Georgia Tech Research Corp.
    Inventors: James C. Powers, Bogdan Boduszek, Jozef Oleksyszyn
  • Patent number: 5356621
    Abstract: A method of attracting flies of the Muscidae or Muscinae families comprising providing in a locus where the flies exist a fly attractant composition which contains as an active ingredient a composition extracted from a bamboo with an extractive solvent such as water or C.sub.1 -C.sub.4 alcohol.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: October 18, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Yuichiro Tabaru, Akio Saito
  • Patent number: 5179084
    Abstract: The present invention relates to phosphoric acid esters of oxetanocins having an antiviral activity which are represented by general formula (I): ##STR1## wherein R.sub.1 represents a phosphoric acid ester residue, X represents hydrogen, hydroxy or hydroxymethyl group, and B represents a purine base residue, and pharmacologically acceptable salts thereof.
    Type: Grant
    Filed: April 4, 1990
    Date of Patent: January 12, 1993
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Seiichi Saito, Shigeru Hasegawa, Masayuki Kitagawa, Nobuyoshi Shimada, Katsutoshi Takahashi, Jun-ichi Seki, Hiroo Hoshino, Yukihiro Nishiyama, Kenichi Matsubara, Takemitsu Nagahata
  • Patent number: 5140019
    Abstract: Compositions which contain, as the active ingredients, a combination of heterocyclic compounds of the general formula (I) and organophosphorous compounds, in addition to one or more compounds having a polyethyleneglycol or polypropyleneglycol chain or an ethyleneglycol-propyleneglycol copolymeric chain, or a mixture of these compounds which results in a stabilization of the active ingredients without any adverse influences on the physical properties of the formulations.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: August 18, 1992
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Yuzuru Wada, Shigeharu Koyama
  • Patent number: 5133972
    Abstract: The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: July 28, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
  • Patent number: 5120349
    Abstract: The microcapsules of the invention are comprised of crystallizable polymers which are preferably side-chain crystallizable polymers or cross-linked, side-chain crystallizable polymers having a specific first order transition point or "melt" temperature. The polymers are caused to form microcapsules and thereby encapsulate one or more compounds generally referred to herein as an active ingredient such as a herbicide, insecticide, fungicide, or fertilizer. The polymer of the microcapsule surrounds the active ingredient separating it from the outside environment. Crystallizable polymers used herein have temperature-dependent permeabilities with respect to a given component such that this component is kept out of contact with the active ingredient at a temperature below a given first order transition point and (due to increased permeability) is allowed to contact the active ingredient at a temperature at or above the transition point.
    Type: Grant
    Filed: December 7, 1990
    Date of Patent: June 9, 1992
    Assignee: Landec Labs, Inc.
    Inventors: Ray F. Stewart, Lawrence C. Greene, Ravi K. Bhaskar
  • Patent number: 4971958
    Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## according to claim 1. These compounds are useful for the treatment or prophylaxis of calcium metabolism disturbance or disease.
    Type: Grant
    Filed: May 23, 1989
    Date of Patent: November 20, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Elmar Bosies, Rudi Gall
  • Patent number: 4943307
    Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: July 24, 1990
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Tamas Detre, Sandor ngyan, Laszlo Pap, Andras Szego, Zoltan Karadi, Klara Bertus nee Bende, Katalin Marmarosi nee Kellner
  • Patent number: 4753930
    Abstract: Novel insecticides and nematicides of the formula ##STR1## in which R is i-propyl or sec.-butyl, andR.sup.1 is hydrogen or halogen.
    Type: Grant
    Filed: February 12, 1987
    Date of Patent: June 28, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Benedikt Becker, Bernhard Homeyer