Px- Bonded Directly To 1,3-diazine At 2- Position (x Is Chalcogen) Patents (Class 514/87)
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Patent number: 8940927Abstract: 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: GrantFiled: May 25, 2011Date of Patent: January 27, 2015Assignee: Metabasis Therapeutics, Inc.Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Patent number: 8816082Abstract: 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: GrantFiled: May 27, 2011Date of Patent: August 26, 2014Assignee: The Royal Institution for the Advancement of Learning/McGill UniversityInventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
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Patent number: 8236334Abstract: 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: GrantFiled: September 6, 2005Date of Patent: August 7, 2012Inventor: James S. Bass
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Patent number: 7192905Abstract: 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: GrantFiled: June 20, 2003Date of Patent: March 20, 2007Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Andrew Y. Li, John Allen Miller
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Patent number: 6919322Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: March 7, 2001Date of Patent: July 19, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Publication number: 20030171335Abstract: 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: ApplicationFiled: October 16, 2002Publication date: September 11, 2003Inventors: David A. Stein, Douglas E. Skilling, Patrick L. Iversen, Alvin W. Smith
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Publication number: 20030027785Abstract: 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: ApplicationFiled: June 25, 2002Publication date: February 6, 2003Inventors: Matthew S. Cowlen, Benjamin R. Yerxa, Arthur C. Jones, Edward G. Brown
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Publication number: 20030027799Abstract: 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: 1Type: ApplicationFiled: March 28, 2002Publication date: February 6, 2003Applicant: Shire BioChem Inc.Inventor: Jacques Jolivet
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Patent number: 6300356Abstract: 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: GrantFiled: August 10, 2000Date of Patent: October 9, 2001Assignee: Merck & Co., Inc.Inventors: Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
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Patent number: 6201002Abstract: 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: GrantFiled: January 6, 1998Date of Patent: March 13, 2001Assignee: Merck & Co., Inc.Inventors: Polly A. Beere, Paul I. Chang, Bertram Pitt, Eva J. Rucinska, Robert Segal, Divakar Sharma, Duane B. Snavely
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Patent number: 6200961Abstract: 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: GrantFiled: December 16, 1998Date of Patent: March 13, 2001Assignee: Aquatrols Corporation of America, Inc.Inventors: Stanley J. Kostka, Rennan Pan
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Patent number: 6040299Abstract: 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: GrantFiled: October 23, 1998Date of Patent: March 21, 2000Assignee: Griffin LLCInventor: Hamid Ullah
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Patent number: 5880111Abstract: 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: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
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Patent number: 5543396Abstract: 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: GrantFiled: April 28, 1994Date of Patent: August 6, 1996Assignee: Georgia Tech Research Corp.Inventors: James C. Powers, Bogdan Boduszek, Jozef Oleksyszyn
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Patent number: 5356621Abstract: 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: GrantFiled: February 10, 1993Date of Patent: October 18, 1994Assignee: Sankyo Company, LimitedInventors: Yuichiro Tabaru, Akio Saito
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Patent number: 5179084Abstract: 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: GrantFiled: April 4, 1990Date of Patent: January 12, 1993Assignee: Nippon Kayaku Kabushiki KaishaInventors: Seiichi Saito, Shigeru Hasegawa, Masayuki Kitagawa, Nobuyoshi Shimada, Katsutoshi Takahashi, Jun-ichi Seki, Hiroo Hoshino, Yukihiro Nishiyama, Kenichi Matsubara, Takemitsu Nagahata
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Patent number: 5140019Abstract: 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: GrantFiled: November 19, 1990Date of Patent: August 18, 1992Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Yuzuru Wada, Shigeharu Koyama
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Patent number: 5133972Abstract: 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: GrantFiled: June 29, 1990Date of Patent: July 28, 1992Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
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Patent number: 5120349Abstract: 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: GrantFiled: December 7, 1990Date of Patent: June 9, 1992Assignee: Landec Labs, Inc.Inventors: Ray F. Stewart, Lawrence C. Greene, Ravi K. Bhaskar
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Patent number: 4971958Abstract: 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: GrantFiled: May 23, 1989Date of Patent: November 20, 1990Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Rudi Gall
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Patent number: 4943307Abstract: 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: GrantFiled: July 15, 1988Date of Patent: July 24, 1990Assignee: 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
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Patent number: 4753930Abstract: 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: GrantFiled: February 12, 1987Date of Patent: June 28, 1988Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Benedikt Becker, Bernhard Homeyer