Oxygen Bonded Directly To A Carbon Or Hydrogen And Wherein The Oxygen Is Not Bonded Directly To Phosphorus Patents (Class 514/129)
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Patent number: 5922404Abstract: The present invention relates to an integrated process for synthesizing dimethyl (2,2,2-trichloro-1-hydroxyethyl)-phosphonate and a process for impregnating the dimethyl (2,2,2-trichloro-1-hydroxyethyl)-phosphonate on to inert carrier granules. The process involves adding dimethyl phosphite to a reaction mixture containing chloral under anhydrous, inert conditions. The molar ratio of chloral to dimethyl phosphite used in the reaction mixture is from about 1.0:1.0 to about 1.1:1.0. The impregnation process involves transferring molten dimethyl (2,2,2-trichloro-1-hydroxyethyl)-phosphonate into a process vessel and discharging weighed aliquots into a formulation vessel to form a granular product containing dimethyl (2,2,2-trichloro-1-hydroxyethyl)-phosphonate.Type: GrantFiled: September 29, 1997Date of Patent: July 13, 1999Assignee: Bayer CorporationInventors: Vidyanatha A. Prasad, Klaus Jelich, Christopher M. Tusa, Daniel E. Terry, Stephen C. Slahck, Scott P. Hensley
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Patent number: 5863909Abstract: An adjuvant composition for agricultural chemicals comprising at least one sorbitan/fatty acid ester surfactant (A) and at least one surfactant (B) selected from the group consisting of resin acid surfactants and anionic oligomer or polymer type quaternary ammonium salt surfactants can be used for various crops in safety without causing injury thereof to the crops, and can enhance the efficacies of various agricultural chemicals.Type: GrantFiled: May 22, 1997Date of Patent: January 26, 1999Assignee: Kao CorporationInventors: Kazuhiko Kurita, Keiko Hasebe, Katsuhiko Yamaguchi, Masaharu Hayashi, Yuichi Hioki
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Patent number: 5807951Abstract: The present invention provides silicate polymers which regulate the function of a living body by restoring and normalizing the lowered cell functions due to diseases. The silicate polymers are preferably water soluble. The molecular weight of the polymers is in the range of 4,800 to 2,000,000, preferably 20,000 to 1,000,000, and they have a degree of polymerization in the range of 75 to 33,000, preferably 490 to 16,500. The monomer unit is --(SiO.sub.2)--. The polymers may be produced by dissolving a water-soluble silicate or a silicic acid containing material such as water glass in water to obtain an aqueous solution. The solution may be admixed with an acid to adjust the pH to 2-10, preferably 4-9.5. A saccharide or sugar alcohol or pharmaceutically acceptable salt may also be admixed with the solution. The aqueous solution is preferably dried to obtain a powder by heating at 150.degree. C. to 250.degree. C. or by lyophilization.Type: GrantFiled: April 30, 1997Date of Patent: September 15, 1998Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Jin-emon Konishi, Giichi Hamada
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Patent number: 5807847Abstract: Aliphatic Nitrate esters having a sulfur or phosphorus atom .beta. or .gamma. to a nitrate group having efficacy as vasodilators are described. Preferred nitrate esters may be synthesized by nitration of a 3-bromo-1,2-propanediol, and subsequent reaction to yield the desired mono, di or tetra nitrate ester.Type: GrantFiled: June 4, 1996Date of Patent: September 15, 1998Assignee: Queen's University at KingstonInventors: Gregory R. J. Thatcher, Brian M. Bennett
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Patent number: 5770587Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.Type: GrantFiled: October 21, 1996Date of Patent: June 23, 1998Assignee: Merck & Co., Inc.Inventors: Angela Basilio, Fernando Pelaez, Maria Teresa Diez, Francisca Vicente, Sandra A. Morris, James E. Curotto, Gerald F. Bills, Sarah J. Dreikorn, Otto D. Hensens, Jerrold M. Liesch, Rosalind G. Jenkins, John R. Thompson
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Patent number: 5763468Abstract: A quaternary-ammonium-free composition having bactericidal activity for both Gram positive and Gram negative bacteria, and including (i) at least one terpene alcohol and (ii) at least one bactericidal acidic surfactant such as an alkyl polyether carboxylic acid, an alkenyl polyether carboxylic acid, an alkylaryl polyether carboxylic acid or a phosphoric ester of an alkoxylated non-ionic surfactant, particularly a phosphoric mono- or diester, in acidic or partially neutralized form.Type: GrantFiled: September 10, 1996Date of Patent: June 9, 1998Assignee: Action PinInventors: Alain Barranx, Michel Barsacq, Ghislain Dufau, Jean-Paul Lauilhe
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Patent number: 5728731Abstract: The oligomers of the present invention are polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone with a predictable anion spacing, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of HSV and HCMV.Type: GrantFiled: June 6, 1995Date of Patent: March 17, 1998Assignees: Merrell Pharmaceuticals Inc., The Dow Chemical Co.Inventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
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Patent number: 5726166Abstract: A method of treating or preventing clinical manifestations associated with diseases caused by infectious organisms which express antigens which in the patient stimulate secretion of harmful levels of at least one cytokine, other than diseases caused by organisms which stimulate secretion of cytokines only by expression of lipopolysaccharide, which method comprises administering to a human in need thereof an effective non-toxic amount of a material selected from the group consisting of inhibitors and immunogens wherein said inhibitors are pharmacologically acceptable materials which, in vitro, reduce or abolish secretion, by at least one of human monocytes and mouse peritoneal macrophages, of tumour necrosis factor following stimulation with a phospholipid-containing; tumour necrosis factor-inducing antigen other than lipopolysaccharide, and wherein said immunogens are pharmacologically acceptable materials comprising at least one B-cell epitope and which stimulate production of antibodies which, in vitro, redType: GrantFiled: December 5, 1994Date of Patent: March 10, 1998Assignee: British Technology Group LimitedInventors: John Hugh Lyon Playfair, Janice Taverne, Clive Alan Winston Bate
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Patent number: 5712261Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.Type: GrantFiled: June 21, 1995Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5709890Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.Type: GrantFiled: March 20, 1997Date of Patent: January 20, 1998Assignee: Donlar CorporationInventor: J. Larry Sanders
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Patent number: 5698541Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.Type: GrantFiled: September 25, 1996Date of Patent: December 16, 1997Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
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Patent number: 5676742Abstract: The present invention comprises dipropylene glycol dibenzoate and diethylene glycol dibenzoate, the improvement comprising the addition of dipropylene glycol monobenzoate or diethylene glycol monobenzoate, whereby the plasticizer is resistant to fungal growth.Type: GrantFiled: October 30, 1995Date of Patent: October 14, 1997Assignee: Velsicol Chemical CorporationInventors: William D. Arendt, David Wayne Barrington
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Patent number: 5665715Abstract: The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.Type: GrantFiled: July 28, 1995Date of Patent: September 9, 1997Assignee: Merrell Pharmaceuticals Inc.Inventor: David M. Stemerick
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Patent number: 5658897Abstract: The present invention relates to cyclopentane (or cyclopentane) heptanoic or cyclopentane (or cyclopentene) heptenoic acid, 2-hydrocarbyl phosphinyloxyalkyl or phosphonamidoalkyl, 1-esters, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: April 8, 1996Date of Patent: August 19, 1997Assignee: AllerganInventor: Robert M. Burk
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Patent number: 5656616Abstract: An insecticidal composition comprising an effective amount of a biocide and an effective amount of a insecticide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: KAO CorporationInventor: Tetsuji Iwasaki
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Patent number: 5654291Abstract: A biocide composition comprises an effective amount of a biocide and an effective amount of a biocide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.Type: GrantFiled: May 26, 1995Date of Patent: August 5, 1997Assignee: Kao CorporationInventor: Tetsuji Iwasaki
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Patent number: 5646133Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.Type: GrantFiled: March 14, 1996Date of Patent: July 8, 1997Assignee: Donlar CorporationInventor: J. Larry Sanders
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Patent number: 5629300Abstract: A metrifonate-containing medicament is disclosed that contains the (-) -enantiomeric metrifonate as the sole active compound providing better cholinesterase-inhibition than the racemate.Type: GrantFiled: November 10, 1994Date of Patent: May 13, 1997Assignee: Bayer AktiengesellschaftInventors: Michael Boberg, Wolfgang Kanhai, Armin Kern, Volker Muschalek, Ulrich Pleiss
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Patent number: 5574025Abstract: The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained in this invention are chemotherapeutic compositions containing these prenyl-transferase inhibitors and methods for their production.Type: GrantFiled: October 26, 1994Date of Patent: November 12, 1996Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Charles A. Omer
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Patent number: 5556842Abstract: This invention provides a lung graft preservative composition comprising a phosphoric acid diester compound of the formula: ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group) or a pharmaceutically acceptable salt thereof and a method for the preservation of the lung graft using the compound.Type: GrantFiled: January 23, 1995Date of Patent: September 17, 1996Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Nobuyoshi Shimizu, Kouzi Uno, Motoi Aoe, Kenichi Yoshida
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Patent number: 5547946Abstract: A method and topical pharmaceutical composition for treating respiratory allergies, allergic rhinitis, allergic conjunctivitis, allergic asthma, and allergy to fur and dust, in which free ion calcium plays a role in a subject. The composition is in the form of oral local and/or nasal liquid solution or suspension for instillation, inhalation or insufflation and includes as active agent, at least one compound selected from the group consisting of: DL-.alpha.-glycerophosphoric acid, glutaric acid and their sodium or potassium salts as the essential active agent. The active agent, when supplied in a sufficient amount, being effective to enable by a reduction in free ion calcium concentration the removal or improvement in symptoms of allergy amenable to said free calcium ion concentration reduction.Type: GrantFiled: November 15, 1993Date of Patent: August 20, 1996Assignee: Farmin S.r.l.Inventor: Giuliano Molinari
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Patent number: 5525480Abstract: The present invention provides N- and O-substituted aminophenol derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, G and L are as hereinbefore defined. The present invention also provides intermediates for the preparation of these aminophenol derivatives of general formula (I), as well as the use of the aminophenol derivatives of general formula (I) for the determination of hydrolases, as well as for the preparation of agents for carrying out determinations of hydrolysis.Type: GrantFiled: June 9, 1994Date of Patent: June 11, 1996Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Dieter Mangold
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Patent number: 5525326Abstract: Methods of providing an image of the gastrointestinal region of a patient and diagnosing the presence of any tumorous tissue in that region using contrast media comprising a combination of at least one polyphosphorylated aliphatic or polyphosphorylated alicyclic compound and at least one paramagnetic ion, wherein the aliphatic and alicyclic compounds comprise at least five carbon atoms, is described. Also described are diagnostic kits for gastrointestinal imaging which include the subject contrast media.Type: GrantFiled: May 5, 1995Date of Patent: June 11, 1996Assignee: Imarx Pharmaceutical Corp.Inventor: Evan C. Unger
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Patent number: 5512534Abstract: The present invention relates to compounds of the formula I ##STR1## in which R.sup.1 is hydrogen,a substituted or unsubstituted aliphatic radicalhaving up to 30 carbon atoms,a substituted or unsubstituted alicyclic radicalhaving up to 30 carbon atoms,a substituted or unsubstituted aromatic radicalhaving up to 24 carbon atoms ora substituted or unsubstituted heteroaromaticradical having up to 20 carbon atoms,R.sup.2 is an amino acid,x'=0-80,y'=0-50,x"=0-80 andy"=0-50,with at least one of the variables x', y', x" and y" being greater than 0. The compounds of the formula I are prepared by reacting the corresponding dihydrogen phosphate with the respective amino acid or salt thereof. The compounds according to the invention can be employed, for example, as surfactants for emulsifying organic solvents in water.Type: GrantFiled: October 4, 1993Date of Patent: April 30, 1996Assignee: Hoechst AktiengesellschaftInventors: Gerhard Frisch, Thomas Maier
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Patent number: 5508273Abstract: Compounds represented by the formula I: ##STR1## are disclosed as agents for use in treating bone wasting diseases.Type: GrantFiled: December 30, 1993Date of Patent: April 16, 1996Assignee: Ortho Pharmaceutical CorporationInventors: Scott Beers, Elizabeth A. Malloy, Charles Schwender
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Patent number: 5500417Abstract: This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or phosphonic acid derivatives of Formula II ##STR2## as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1 '-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester. The invention also provides novel acids, esters, and salts of arylmethylphosphonic acid, phosphonic acid and derivatives.Type: GrantFiled: March 16, 1995Date of Patent: March 19, 1996Assignee: The Upjohn CompanyInventor: Roy A. Johnson
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Patent number: 5474992Abstract: A pharmaceutical composition for renal disorder and a dialysis solution for extracorporeal hemodialysis which comprise a phosphoric acid diester of the following formula: ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group) or a pharmacologically acceptable salt thereof.Since the composition of this invention inhibits the formation of free radicals in the body, it can be advantageously used for the prophylaxis and treatment of various renal disorders such as glomerulonephritis, acute renal failure, uremia, adriamycin nephrosis, puromycin nephrosis, gentamicin- and cisplatin-induced disorders of the kidney, renal impairment due to paraquat and other agricultural chemicals, and immune complex nephritis. Moreover, the composition of this invention is also of use as a dialysis solution for extracorporeal hemodialysis with the propylactic/therapeutic effect on dialysis amyloidosis.Type: GrantFiled: August 31, 1994Date of Patent: December 12, 1995Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Takahiro Sakaue, Noriko Saito, Sachiko Matsuura, Rie Nagao, Shinya Ogino
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Patent number: 5466682Abstract: Compounds of formula (I) ##STR1## in which A is (CH.sub.2).sub.n in which n is 1-10, preferably 3 or 5, and R is the acyl group from a known anti-inflammatory agent, exhibit high anti-inflammatory activity. The mechanism of action is novel because they do not release the anti-inflammatory agent in the body but exhibit an activity superior to the activity of the known anti-inflammatory agent. The compounds are also active in combating bone calcium loss.Type: GrantFiled: July 26, 1993Date of Patent: November 14, 1995Assignee: Istituto Gentili S.p.A.Inventors: Sergio Rosini, Maurizio Mian
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Patent number: 5464866Abstract: Substituted hydrindanes and their use in controlling angiogenesis-dependent diseases in warm blooded animals are disclosed.Type: GrantFiled: March 10, 1994Date of Patent: November 7, 1995Assignee: Alcon Laboratories, Inc.Inventors: Abbot F. Clark, Raymond E. Conrow
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Patent number: 5463181Abstract: The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.Type: GrantFiled: November 8, 1993Date of Patent: October 31, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: David M. Stemerick
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Patent number: 5447922Abstract: .alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is alkyl, arylalkyl or aryl; R.sup.4 is H or pharmaceutically acceptable cation;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts.Type: GrantFiled: August 24, 1994Date of Patent: September 5, 1995Assignee: Bristol-Myers Squibb CompanyInventors: R. Michael Lawrence, Scott A. Biller, Olga M. Fryszman
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Patent number: 5385896Abstract: Phosphonium salts such as THP and aldehydes such as formaldehyde exhibit synergistic biocidal activity.Type: GrantFiled: May 9, 1994Date of Patent: January 31, 1995Assignee: Albright & Wilson LimitedInventors: Edward Bryan, Malcolm A. Veale, Robert E. Talbot, Kenneth G. Cooper, Nigel S. Matthews
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Patent number: 5380484Abstract: The present invention relates to treatment of marine borer infestation. It has been found that wood can be effectively protected from marine borer infestation by impregnating the wood with a pesticidally effective amount of chlorothalonil. In general, the quantity of chlorothalonil employed is in the range of from about 0.3 to about 3.0 pounds per cubic foot, although higher concentrations can be employed.Type: GrantFiled: September 3, 1992Date of Patent: January 10, 1995Assignee: ISK Biotech CorporationInventors: Thomas L. Woods, Lawrence J. Cookson
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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: 5342832Abstract: A method of preventing or alleviating tissue damage, diabetes and complications thereof, bone disorders, disorders related to transplantation, disorders related to abnormal levels of lipoproteins, cardiovascular disease and inflammatory disorders by providing a mammal having one or more of the above diseases with a preventing or an alleviating effective amount of a compound having the formula C.sub.6 H.sub.6 (OH).sub.6-n (OPO.sub.3 H.sub.2).sub.n, where n is an integer of 1 or 2.Type: GrantFiled: August 21, 1992Date of Patent: August 30, 1994Assignee: Perstorp ABInventor: Matti Siren
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Patent number: 5336671Abstract: The invention provides fungicidal compositions containing benzyl-tris(aryl)-phosphonium salts of the general formula ##STR1## in which R.sup.1 represents an optionally substituted alkyl or alkoxy group; R.sup.2 represents a hydrogen atom or an optionally substituted alkyl group; R.sup.3, R.sup.4 and R.sup.5 independently represent a hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group; and A.sup.- represents an anion processes for the preparation of such compounds. Certain of the compounds of formula I are novel and the invention therefore also provides processes for the preparation of such compounds and their use as fungicides.Type: GrantFiled: October 18, 1991Date of Patent: August 9, 1994Assignee: Shell Research LimitedInventors: Heinz-Manfred Becher, Guido Albert, Jurgen Curtze
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Patent number: 5306713Abstract: A highly active antioxidant composed of a diester of phosphoric acid with tocopherol and ascorbic acid or a salt thereof used to stabilize other materials.Type: GrantFiled: August 7, 1991Date of Patent: April 26, 1994Assignees: Shiseido Company Ltd., Senju Pharmaceutical Co, Ltd.Inventors: Keiko Suetsugu, Kazumi Ogata, Kenichi Yoshida, Keiichi Uehara, Kenichi Tomita
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Patent number: 5298500Abstract: Disclosed is a phosphoric acid ester derivative represented by the general formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each lower alkyl, X.sup.1 and X.sup.2 are the same or different and are each a hydrogen atom or halogen atom, and Y is an oxygen atom or sulfur atom. The phosphoric acid ester derivatives of the present invention are usable as insecticides and miticides having excellent residual activity and low toxicity to warm blooded animals.Type: GrantFiled: March 17, 1992Date of Patent: March 29, 1994Assignee: Otsuka Kagaku Kabushiki KaishaInventor: Hisashi Takao
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Patent number: 5281586Abstract: Pharmaceutical compositions for the treatment of peripheral neuropathies of dysmetabolic or toxic origin and of cerebropathies of organic and functional origin, containing as the active ingredient L-.alpha.-glycerophosphoryl-D-myo-inosital, as such or as the alkali or alkali-earth metal salt thereof.Type: GrantFiled: March 2, 1992Date of Patent: January 25, 1994Assignee: Apotekna S.A.Inventors: Carlo Scolastico, Camillo M. F. G. Palazzi, Carla Procida
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Patent number: 5242908Abstract: The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.Type: GrantFiled: February 1, 1991Date of Patent: September 7, 1993Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Eugen Uhlmann, Karlheinz Budt, Jochen Knolle, Irvin Winkler, Matthias Helsberg
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Patent number: 5219845Abstract: The invention pertains to the synthesis and use as therapeutic agents of a group of substances with a glycerol backbone or aliphatic chain structure linked to a phosphorus atom and a polar head group. Depending on the polar head group, the substance has anti-cancer, anti-inflammatory, anti-allergy or anti-cardiovascular disease properties. Compounds of the formula: ##STR1## wherein n is 0 to 14 and R.sub.1 is an alkyl group of C.sub.12 -C.sub.20, R.sub.2 is a methyl group, and wherein R.sub.3 is an inositol analog head group, a (CH.sub.2).sub.m N.sup.+ (CH.sub.3).sub.3 group with m=2 to 10, a serine head group, or an ethanolamine head group, or of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as described above, n=0 or 1, and R.sub.3 is (CH.sub.2).sub.m N.sup.+ (CH.sub.3).sub.3 (m=2-10) are claimed.Type: GrantFiled: February 11, 1992Date of Patent: June 15, 1993Assignee: The University of British ColumbiaInventors: Hassan Salari, Robert Bittman
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Patent number: 5189062Abstract: ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of alphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of >13.degree., after 20 minutes of >6.degree. and it is often 120 minutes still at least 2.degree..Type: GrantFiled: January 28, 1992Date of Patent: February 23, 1993Assignee: Chinoin Gyogyszer -ES Vegyeszeti Termekek Gyara R.T.Inventors: Andras Szego, Laszlo Pap, Lajos Nagy, Eva Somfai, Gyorgy Szucsany, Istvan Szekely, Aniko D. nee Molnar, Agnes Hegedus
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Patent number: 5166144Abstract: The invention relates to new O-halogenocyclobutyl S-alkyl (di)thiophosphoric acid ester-amides of the general formula (I) ##STR1## in which A represents fluorine or chlorine,B represents hydrogen or alkyl,X represents oxygen or sulphur,R.sup.1 represents hydrogen, alkyl, --COH (formyl) or --CO-alkyl (acyl) which is optionally substituted by halogen,R.sup.2 represents hydrogen or alkyl, andR.sup.3 represents alkyl or alkoxyalkyl,which can be used as agents for combating pests.Type: GrantFiled: March 20, 1992Date of Patent: November 24, 1992Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Dietmar Bielefeldt, Karl-R. Gassen, Jurgen Hartwig, Wilhelm Stendel, Christoph Erdelen
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Patent number: 5164383Abstract: O-Halogenocyclopentyl S-alkyl (di)thiphosphoric(phosphonic) acid ester derivatives of the general formula (I) ##STR1## in which R.sup.1 represents alkyl, alkoxy or the radical ##STR2## R.sup.3 represents hydrogen or alkyl and R.sup.4 represents hydrogen, alkyl, --COH (formyl) or optionally halogen-substituted --CO-alkyl (acyl),R.sup.2 represents alkyl or alkoxyalkyl andX represents oxygen or sulphur,can be used as pesticides.Type: GrantFiled: March 20, 1992Date of Patent: November 17, 1992Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Michael Negele, Jurgen Hartwig, Christoph Erdelen, Wilhelm Stendel
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Patent number: 5149695Abstract: Fumaric acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or a metallic cation, andR.sub.2 is a saturated or unsaturated aliphatic C.sub.6 -C.sub.24 alkyl group, psoralen-9-yl, retinyl, .alpha.-tocopheryl (vitamin E), calciferyl, corticosteroid-21-yl or monosaccharid-.omega.-yl; a group of fumaric acid derivatives based on glycerol, alkane diol or polyol molecules; and fumaric acid derivatives of the formula ##STR2## wherein n is an integer from to 30 to 260,R.sub.3 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group,R.sub.4 is one of the R.sub.3 groups and n is the number of molecule repetitions, processes for their production and compositions containing same are described. These compounds are useful as drugs for the treatment of cryptogenically-caused diseases and have antisporiatic as well as antimicrobial action.Type: GrantFiled: March 13, 1989Date of Patent: September 22, 1992Inventors: Peter P. Speiser, Rajendra K. Joshi
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Patent number: 5147867Abstract: Dipeptide mimics which contain phosphorus and their pharmaceutical use and preparation are disclosed. The compounds have dehydropeptidase (DHP) enzyme inhibitor activity.Type: GrantFiled: January 21, 1992Date of Patent: September 15, 1992Assignee: Merck & Co., Inc.Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
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Patent number: 5139561Abstract: A method for protecting growing plants against fungal or microbial plant pathogens which comprises applying thereto, or to the medium on which they are growing or to be grown, a composition comprising a water soluble tetrakis (hydroxymethyl) phosphonium salt.Type: GrantFiled: July 19, 1991Date of Patent: August 18, 1992Assignee: Albright & Wilson LimitedInventors: Robert E. Talbot, Kenneth G. Cooper
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Patent number: 5102874Abstract: Antimicrobial mixtures contain quaternary ammonium compounds and quaternary phosphonium compounds in a ratio by weight of from 1:9 to 9:1.Type: GrantFiled: August 20, 1990Date of Patent: April 7, 1992Assignee: Ecolab Inc.Inventors: Karl Lintner, Reinhard Orth, Rudolf Lehmann, Hans-Juergen Mueller
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Patent number: 5055459Abstract: A method for purging tumor cells from bone marrow of a host, the method comprisingextracting bone marrow cells from the host;treating extracted bone marrow cells with a therapeutic level of a compound having the structure: ##STR1## wherein R is CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, t-C.sub.4 H.sub.9 or C.sub.6 H.sub.5 ; R.sup.1 is NH.sub.2, NHCH.sub.3, NHC.sub.2 H.sub.5, NHC.sub.3 H.sub.7, NHC.sub.4 H.sub.9, NHCH.sub.2 CH.sub.2 Cl, NHC.sub.6 H.sub.5, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, N(C.sub.3 H.sub.7).sub.2, NCH.sub.3 (C.sub.2 H.sub.5), NCH.sub.3 (C.sub.3 H.sub.7), N(CH.sub.2 CH.sub.2 Cl).sub.2, NHOH, NHNHCO.sub.2 CH.sub.2 C.sub.6 H.sub.5, NHNHCO.sub.2 C(CH.sub.3).sub.3, OCH.sub.3, OC.sub.2 H.sub.5, OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, OC.sub.6 H.sub.5, OCH.sub.2 C.sub.6 H.sub.5, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, CH.sub.2 NO.sub.2 or CH.sub.2 NH.sub.2 ; and R.sup.2 is NHCH.sub.2 CH.sub.2 Cl or N(CH.sub.2 Ch.sub.2 Cl).sub.2.Type: GrantFiled: April 6, 1989Date of Patent: October 8, 1991Assignee: Board of Regents, The University of TexasInventors: Borje S. Andersson, David Farquhar
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Patent number: 5045311Abstract: The invention relates to an emulsifiable microemulsion concentrate containing a phophoric acid ester and/or thiophosphoric acid ester as active ingredient. In addition to 20 to 80% by weight of active ingredient, the composition comprises: 7 to 70% by weight of a nonionic surface active agent, preferably a block copolymer with a molecular weight of 1000 to 10000 formed from polyethylene oxide and polypropylene oxide, an alkylphenol polyglycol ether, ethoxylated fatty alcohol or a mixture of nonionic surface active agents; 2 to 50% by weight of water; if desired, 1 to 50% by weight of a co-surfactant, preferably C.sub.1-8 straight or branched chain and/or cyclic alcohol, C.sub.3-8 straight or branched chain and/or cyclic ketone, esters of C.sub.1-6 fatty acids with C.sub.1-6 alcohols or the mixture thereof; and if desired, 15 to 30% by weight of a water-immiscible organic solvent.Type: GrantFiled: May 12, 1989Date of Patent: September 3, 1991Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Janos Pinter, Josefne Pal, Eva Kiss, Erzsebet Shuszler, Sandor Angyan, Laszlo Pap, Andras Szego, Tamas Detre, Tamasne Marmarosi