Plural Oxygens Bonded Directly To The Same Sulfur (e.g., Sulfones, Etc.) Patents (Class 514/709)
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Patent number: 5614525Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control off parasites in vertebrate animals.Type: GrantFiled: May 4, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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Patent number: 5583091Abstract: A composition comprises (a) halogenated aromatic 1,2- or 1,3- dinitrile, (b) a substituted urea and (c) a halogen-containing aromatic alkyl sulphoxide or sulphone. The composition may include other materials for example inorganic diluents such as silica, alumina, titanium, dioxide, zinc oxide, etc. and may also include other anti-microbial agents such are anti-bacterial agents. The composition has anti-microbial properties, particularly anti-fungal and anti-algal properties. The composition can be incorporated into materials such as paint or plastics to provide anti-microbial properties.Type: GrantFiled: December 7, 1994Date of Patent: December 10, 1996Assignee: Zeneca LimitedInventors: Bryan S. Backhouse, Malcolm Greenhalgh
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Patent number: 5583089Abstract: This invention provides a dry blend pesticide composition which contains a fungicidal bicarbonate salt ingredient, and a spreader-sticker ingredient which is a crystalline clathrate complex of a urea constituent and a normally liquid spreader sticker constituent such as a nonionic surfactant. In a preferred embodiment all of the composition ingredients are water-soluble, and the composition is readily dispersible in an aqueous medium to form a sprayable pesticide solution.Type: GrantFiled: May 9, 1995Date of Patent: December 10, 1996Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5580570Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.Type: GrantFiled: March 16, 1995Date of Patent: December 3, 1996Assignee: Alcon Laboratories, Inc.Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
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Patent number: 5550145Abstract: An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these monoglycerides, and B) at least one chemical substance selected from the following groups: i) local anesthetics of the amide type; ii) carbamide, iii) antibacterial substances in the form of steroid antibiotics, imidazole derivatives or nitroimidazole derivatives, and iv) diols with 3-6 carbon atoms, and C) optionally, a conventional physiologically acceptable carrier and/or physiologically acceptable additives. A process for the preparation of this composition by heating (A) to the transition temperature of the lipid, adding (B), and optionally (C), and cooling the mixture to form a solid lipid crystal composition. Use of the composition for the preparation of a dermatological preparation for combatting bacteria and fungi or as a preservative additive in a cosmetic product, a food product, or a medical product.Type: GrantFiled: September 27, 1994Date of Patent: August 27, 1996Assignee: Bioglan ABInventors: Karin Olund, Lena-Karin L utz, Rickard Bryland, .ANG.ke Lindahl
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Patent number: 5547992Abstract: The oligomers of the present invention are polyureas, polycarbonates, polyesters or 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: March 21, 1995Date of Patent: August 20, 1996Assignees: The Dow Chemical Co., Merrell Pharmaceuticals Inc.Inventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
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Patent number: 5518986Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as pentachloronitrobenzene, sodium bicarbonate, sodium carbonate, potassium oleate, potassium octanoate and xanthan gum. The combination of potassium oleate, potassium octanoate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.Type: GrantFiled: April 6, 1995Date of Patent: May 21, 1996Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5518987Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as etridiazole, potassium bicarbonate, sodium carbonate, potassium oleate, potassium caprylate and xanthan gum. The combination of potassium oleate, potassium caprylate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.Type: GrantFiled: October 3, 1995Date of Patent: May 21, 1996Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5508305Abstract: 2,4-disulfonyl .alpha.-phenyl-tert-butyl nitrone and its pharmaceutically acceptable salts are disclosed. These materials are useful as pharmaceutical agents for oral or parenteral, e.g. intravenous administration to patients suffering from acute central nervous system oxidation as occurs in a stroke or from gradual central nervous system oxidation which can exhibit itself as progressive central nervous system function loss. The materials are also used to ameliorate the side effects of oxidative-damage causing antineoplastic disease treatments.Type: GrantFiled: June 6, 1995Date of Patent: April 16, 1996Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventor: John M. Carney
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Patent number: 5506267Abstract: A compound of the invention is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, an acyl group; R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are the same or different, hydrogen or an alkyl group; R.sup.5 is hydrogen, an alkyl group or a hydroxyl group which may optionally be protected, or R.sup.4 and R.sup.5 are combined to form a chemical bond; X is a carbonyl group or a sulfonyl group; Y is an amino acid sequence consisting of 1 to 7 amino acid residues which may optionally be protected and having optionally an intervening --SO.sub.2 NH--; n is an integer of 0 to 2, or a salt thereof.Type: GrantFiled: September 8, 1994Date of Patent: April 9, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Koichi Yukishige, Seiichi Tanida
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Patent number: 5496568Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as propiconazole, sodium bicarbonate, potassium bicarbonate, sodium oleate, sodium caprylate and xanthan gum. The combination of sodium oleate, sodium caprylate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.Type: GrantFiled: June 26, 1995Date of Patent: March 5, 1996Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5489612Abstract: Calixarene derivatives, their synthesis and use as chloride channel blockers are described. Preferred calixarene derivatives are of the formula: ##STR1## wherein R is an acidic group or salt thereof, such as SO.sub.3 X or R.sup.1 SO.sub.3 X where X is H or Na, and R.sup.1 is ##STR2## where m=1-2, and R.sup.3 and R.sup.4 the same or different is each H or a C.sub.1-4 alkyl, or a nitrogen-containing group of the formula ##STR3## or A, wherein R.sup.5 is a C.sub.1-4 alkyl, R.sup.6 is a C.sub.1-4 alkyl and A is ##STR4## where R.sup.7 and R.sup.8, the same or different each is H or a C.sub.1-4 alkyl, and R.sup.9 and R.sup.10, the same or different, each is H or a C.sub.1-4 alkyl; R' is H or a C.sub.1-4 alkyl; and n is an integer of 4-8, preferably 4, 6 or 8.Type: GrantFiled: January 7, 1994Date of Patent: February 6, 1996Assignee: The University of Alabama at Birmingham Research FoundationInventors: Jerry L. Atwood, Robert J. Bridges, Ravindra K. Juneja, Ashvani K. Singh
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Patent number: 5468716Abstract: The present invention provides a fungicide composition which contains ingredients which are biocompatible for purposes of agricultural applications, and which are harmless to animals and humans. An invention fungicide composition in the form of a dry blend formulation remains non-caking and free-flowing under storage conditions. Illustrative of an invention fungicide composition is a formulation which has a content of sodium bicarbonate, potassium bicarbonate, xanthan gum, dialkylsulfosuccinate salt and alkyl sulfate salt surfactants, and magnesium silicate anti-caking ingredient. The xanthan gum and surfactants function as an effective spreader-sticker and film-forming medium when the composition is diluted with water for agricultural applications.Type: GrantFiled: October 3, 1994Date of Patent: November 21, 1995Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5464805Abstract: The present invention provides a method for controlling mildew in cultivated crops. The aqueous fungicide formulation which is applied to pre-harvest and post-harvest crops contains ingredients which are biocompatible for purposes of agricultural and horticultural applications. Illustrative of a formulation which is harmless to animals and humans is an aqueous solution having a content of potassium bicarbonate, potassium carbonate, potassium oleate and xanthan gum. The combination of potassium oleate and xanthan gum functions as an effective spreader-sticker medium for forming a solid coating on plant surfaces. The solid coating exhibits both immediate and long duration fungicidal activities.Type: GrantFiled: March 23, 1995Date of Patent: November 7, 1995Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5449681Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: November 22, 1993Date of Patent: September 12, 1995Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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Patent number: 5446033Abstract: Solutions of alkylphosphocholines in glycerol alkyl ethers having enhanced storage stability containing a buffer which maintains the pH value to a range between 4 and 6.Type: GrantFiled: October 19, 1993Date of Patent: August 29, 1995Assignee: Asta Medica AGInventors: Jurgen Engel, Elisabeth Wolf-Heuss, Helmut Orth, Burkhard Wichert, Dieter Sauerbier
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Patent number: 5441983Abstract: A method for inhibiting cell infection by an enveloped virus, by administering to an infection site, a therapeutically effective amount of a calix(n)arene compound derivatized, at its ring positions meta to the bridge attachements to the ring, with polar substitutent having a terminal carboxylate, phosphate, or sulfonate groups, including esters and amides which are cleavable in vivo. The compound may be administered orally, or topically, e.g., for treatment of herpes virus.Type: GrantFiled: August 6, 1992Date of Patent: August 15, 1995Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu, William Choy, Jen Chen
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Patent number: 5434144Abstract: The subject invention relates to methods of regulating skin wrinkles and/or atrophy in mammalian skin comprising topically applying to the skin of a mammal in need of treatment a composition comprising a safe and effective amount of a cyclic polyanionic polyol derivative having the structure: ##STR1## wherein n is an integer from 1 to 3; and each X is, independently, selected from the group consisting of OSO.sub.3.sup.-, OPO.sub.3.sup..dbd., SO.sub.3.sup.--, PO.sub.3.sup..dbd., CO.sub.2.sup.--, and OH; with at least 3 X's being other than OH.Type: GrantFiled: March 4, 1994Date of Patent: July 18, 1995Assignee: The Procter & Gamble CompanyInventors: Gerald B. Kasting, John M. Gardlik
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Patent number: 5432184Abstract: A biocidal composition and method for inhibiting and controlling the growth of the fungus, Trichoderma viride, are disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and an additional biocidal component. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: September 6, 1994Date of Patent: July 11, 1995Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
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Patent number: 5432148Abstract: This invention provides a fungicide composition which is capable of in situ generation of ammonium bicarbonate when applied to plant foliage in the form of an aqueous dispersion. The constituents include (1) an ingredient such as urea which slow-releases ammonia under aqueous alkaline pH conditions; and (2) an alkali metal bicarbonate ingredient which imparts alkalinity to the aqueous dispersion, and provides bicarbonate ions for combination with the released ammonium ions. A spreader-sticker ingredient is included to maintain the ingredients in contact with plant foliage over an extended period after application.Type: GrantFiled: December 7, 1994Date of Patent: July 11, 1995Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5425952Abstract: This invention provides a fungicide composition which is capable of in situ generation of ammonium bicarbonate when applied to plant foliage in the form of an aqueous dispersion. The constituents include (1) an ingredient such as urea which slow-releases ammonia under aqueous alkaline pH conditions; and (2) an alkali metal bicarbonate ingredient which imparts alkalinity to the aqueous dispersion, and provides bicarbonate ions for combination with the released ammonium ions. A spreader-sticker ingredient is included to maintain the ingredients in contact with plant foliage over an extended period after application.Type: GrantFiled: October 13, 1993Date of Patent: June 20, 1995Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5420160Abstract: There are described new 1-alkoxyhexatriene-2-carboxylates of the formula (I) ##STR1## in which R represents substituted phenyl,and a plurality of processes for their preparation.The new 1-alkoxyhexytriene-2-carboxylates are used as pesticides.Type: GrantFiled: January 21, 1994Date of Patent: May 30, 1995Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Heinz-Wilhelm Dehne, Stefan Dutzmann
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Patent number: 5418254Abstract: A class of 2,3-substituted cyclopenta-2,4-dienyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, lower alkyl, lower hydroxyalkyl, halo, lower haloalkyl, lower alkoxycarbonyl and carboxyl; and wherein each of R.sup.3 through R.sup.12 is independently selected from hydrido, halo, lower alkyl, lower alkylthio, cyano, hydroxyl, mercapto, lower haloalkyl, lower haloalkoxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkylsulfonyl, lower haloalkylsulfonyl and sulfamyl; provided R.sup.5 and R.sup.10 are not both hydrido or methoxy; or a pharmaceutically suitable salt or prodrug thereof.Type: GrantFiled: May 4, 1994Date of Patent: May 23, 1995Assignee: G. D. Searle & Co.Inventors: Horng-Chih Huang, David R. Reitz
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Patent number: 5416121Abstract: A microbial inhibiting composition and method is disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and B-bromo-B-nitrostyrene. The method comprises administering an amount of this combined treatment to the particular water containing system for which treatment is desired.Type: GrantFiled: January 19, 1994Date of Patent: May 16, 1995Assignee: Betz Laboratories, Inc.Inventors: Wilson K. Whitekettle, Deborah K. Donofrio
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Patent number: 5415877Abstract: The present invention provides a fungicide composition which contains ingredients which are biocompatible for purposes of agricultural applications, and which are harmless to animals and humans. An invention fungicide composition in the form of a dry blend formulation remains non-caking and free-flowing under storage conditions. Illustrative of an invention fungicide composition is a formulation which has a content of sodium bicarbonate, potassium bicarbonate, xanthan gum, dialkylsulfosuccinate salt and alkyl sulfate salt surfactants, and magnesium silicate anti-caking ingredient. The xanthan gum and surfactants function as an effective spreader-sticker and film-forming medium when the composition is diluted with water for agricultural applications.Type: GrantFiled: December 22, 1993Date of Patent: May 16, 1995Assignee: Church & Dwight Co., Inc.Inventor: Anthony E. Winston
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Patent number: 5416122Abstract: A microbial inhibiting composition and method is disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and bis trichloro methyl sulfone. The method comprises administering an amount of this combined treatment to the particular water containing system for which treatment is desired.Type: GrantFiled: January 19, 1994Date of Patent: May 16, 1995Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
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Patent number: 5411990Abstract: An industrial microbicide which comprises at least one haloglyoxime derivative of the formula (I): ##STR1## wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and Z is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; and a known industrial microbicidal ingredient selected from the group consisting of an organonitrogen-sulfur compound, an organohalogen compound, an organonitrogen compound and an organosulfur compound; and optionally a carrier or diluent.Type: GrantFiled: May 17, 1993Date of Patent: May 2, 1995Assignees: Yoshitomi Pharmaceutical Industries Ltd., Katayama Chemical Inc.Inventors: Katsuji Tsuji, Hidenori Hirashima
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Patent number: 5407673Abstract: Disclosed is a fibrinolysis and fibrinogenolysis treatment which includes parenterally introducing into the body of a human patient human plasmin in fibrinolytically and fibrinogenolytically active form at a concentration and for a time sufficient to permit fibrinolytically and fibrinogenolytically active human plasmin to reach a concentration about the site of any intravascular clot sufficient to lyse the clot and/or to reduce circulating fibrinogen levels.Type: GrantFiled: October 6, 1993Date of Patent: April 18, 1995Assignee: Orion Therapeutic Systems, Inc.Inventors: Edward Reich, Thomas G. Easton
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Patent number: 5393790Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: February 28, 1995Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
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Patent number: 5369115Abstract: A biocidal composition and method for inhibiting and controlling the growth of the fungus, Trichoderma viride, are disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and an additional biocidal component. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: October 29, 1993Date of Patent: November 29, 1994Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
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Patent number: 5352706Abstract: A microbial inhibiting composition and method is disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and alkyl dimethyl benzyl ammonium chloride. The method comprises administering an amount of this combined treatment to the particular water containing system for which treatment is desired.Type: GrantFiled: July 22, 1993Date of Patent: October 4, 1994Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
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Patent number: 5330980Abstract: A medicament for the topical treatment of burned, irritated, ulcered, chafed, or infected, skin, a method of making the medicament, and a method of use of the medicament, the medicament comprising: about 70.6% by weight of Petrolatum U.S.P.(Vaseline); about 6.8% by weight of Wool Fat U.S.P.; about 4.0% by weight of a Sulfa compounded-ingredient; about 17.4% by weight of Zinc Oxide U.S.P.; and about 1.2% by weight of Disodium Formad Dehyde Sulfoxylate Diamino Diphenyl Sulfone.Type: GrantFiled: August 24, 1992Date of Patent: July 19, 1994Inventor: Jae S. Shin
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Patent number: 5314719Abstract: HVAC systems having interior surfaces exposed to moist air are protected against fungal growth by coating the interior surfaces with an adherent flexible polymer film which includes a fungicidal composition in an amount effective to provide a zone of inhibition against multiple fungal species of at least 1 mm, and which employs active fungicidal ingredients which are substantially non-volatile and non-soluble in water.Type: GrantFiled: March 18, 1993Date of Patent: May 24, 1994Assignee: Foster Products CorporationInventors: Vernon Batdorf, William J. Brendle
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Patent number: 5310761Abstract: A microbial inhibiting composition and method is disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and dodecylguanidine hydrochloride. The method comprises administering an amount of this combined treatment to the particular water containing system for which treatment is desired.Type: GrantFiled: July 22, 1993Date of Patent: May 10, 1994Assignee: Betz Laboratories, Inc.Inventors: Wilson K. Whitekettle, Deborah K. Donofrio
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Patent number: 5302616Abstract: A fungicidal composition and method for inhibiting and controlling the growth of the capsulated, facultative bacterium, Trichoderma viride, are disclosed. The compositions comprise 2-(2-bromo-2-nitroethenyl) furan and diiodomethyl-p-tolylsulfone. The method comprises adding from 1 part to about 500 parts composition to the aqueous system for which treatment is desired.Type: GrantFiled: May 19, 1993Date of Patent: April 12, 1994Assignee: Betz Laboratories, Inc.Inventors: Wilson K. Whitekettle, Deborah K. Donofrio
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Patent number: 5292776Abstract: A biocidal composition and method for inhibiting and controlling the growth of the fungus, Trichoderma viride, are disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and an additional biocidal component. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: March 26, 1993Date of Patent: March 8, 1994Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
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Patent number: 5283264Abstract: An antimicrobial composition and method for producing a stable, antimicrobial formulation of diiodomethyl-p-tolylsulfone is disclosed.Type: GrantFiled: November 30, 1992Date of Patent: February 1, 1994Assignee: Betz Laboratories, Inc.Inventor: Deborah K. Donofrio
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Patent number: 5270058Abstract: An alkali-metal dithionite is readily transformed into an aldehyde sulfoxylate microbicide which is absorbed through plant leaves and is more stable against oxidation.Type: GrantFiled: September 25, 1992Date of Patent: December 14, 1993Assignee: Mauricio KlingInventors: Jorge Miller, Alberto Kling
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Patent number: 5214070Abstract: The invention concerns a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a (3-6C)alkylene group which defines an optionally substituted ring having 4 to 7 ring atoms.The invention also concerns processes for the manufacture of a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said cycloalkane. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: August 21, 1991Date of Patent: May 25, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Thomas G. C. Bird, Philip N. Edwards
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Patent number: 5214069Abstract: The invention concerns a compound of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; wherein R.sup.2 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; and whereinR.sup.3 is hydroxy-(1-4C)alkyl, mercapto-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, (3-4C)alkenyloxy-(1-4C)alkyl, (3-4C)alkynyloxy-(1-4C)alkyl, (1-4C)alkoxy-(2-4C)alkoxy-(1-4C)alkyl, (1-4C)alkylthio-(1-4C)alkyl, (1-4C)alkylsulphinyl-(1-4C)alkyl, (1-4C)alkylsulphonyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, (2-4C)alkanoyl-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl or cyano-(1-4C)alkyl; or R.sup.Type: GrantFiled: January 23, 1992Date of Patent: May 25, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventor: Jean-Marc M. M. Girodeau
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Patent number: 5190944Abstract: The invention relates to synergistic antimicrobial and biocidal compositions comprising 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one and one or more commercial biocides for more effective, and broader control of microorganisms in various industrial systems.Type: GrantFiled: January 26, 1992Date of Patent: March 2, 1993Assignee: Rohm and Haas CompanyInventor: Jemin C. Hsu
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Patent number: 5189056Abstract: The present invention is related to the protection of moist stratified squamous epithelia against damage from exposure to noxious luminal agents. Protection of moist stratified squamous epithelia against these noxious luminal agents is afforded by chemical compounds having one of the following reactive groups in their molecule: X--SO.sub.3.sup.-, where X represents oxygen or carbon, and XO.sub.4.sup.= or X.sub.2 O.sub.7.sup.=, where X represents an element from group VIb or sulfur of group VIa of the periodic table. Compounds that provide protection against injury to moist stratified squamous epithelia that illustrate the protective characteristic of these reactive species are the sulfonates, the sulfate esters and the tetrahedral-shaped divalent oxy-anions of the transition metals in group VIb or of sulfur.Type: GrantFiled: December 19, 1989Date of Patent: February 23, 1993Assignee: University of North Carolina at Chapel HillInventors: Roy C. Orlando, Nelia A. Tobey
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Patent number: 5188663Abstract: An aquatic antifouling composition comprising (A) at least one 4-isothiazolin-3-one compound represented by the general formula: ##STR1## where X.sub.1 and X.sub.2 respectively represent a hydrogen atom or a halogen atom, and (B) at least one insoluble dithiocarbamic acid derivatives possessing a dithiocarbamyl group ##STR2## selected from the group consisting of divalent and higher heavy metal (zinc, manganese, copper, iron, and nickel) salts of ethylenebisdithiocarbamic acid, linear or branched propylenebisdithiocarbamic acid, linear or branched butylenebisdithiocarbamic acid, N-substituted ethylenebisdithiocarbamic acid, N,N'-substituted ethylenebisdithiocarbamic acid, N-substituted propylenebisdithiocarbamic acid, N,N'-substituted propylene-bisdithiocarbamic acid, N-substituted butylenebisdithiocarbamic acid, and N,N'-substituted butylenebisdithiocarbamic acid.Type: GrantFiled: September 16, 1991Date of Patent: February 23, 1993Assignee: Rohm and Haas CompanyInventors: Hirotake Ikari, Teruyoshi Takahashi
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Patent number: 5183814Abstract: The invention relates to a therapeutic product comprising an oestrogen and a pure antioestrogen for simultaneous, sequential or separate use in selective oestrogen therapy of perimenopausal or postmenopausal conditions; to a process for the manufacture of said product and to a pharmaceutical composition containing said product. The invention also relates to a pharmaceutical composition comprising an oestrogen and a pure antioestrogen and to a process for the manufacture of said composition.Type: GrantFiled: June 6, 1989Date of Patent: February 2, 1993Assignee: Imperial Chemical Industries PLCInventor: Michael Dukes
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Patent number: 5153227Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.Type: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
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Patent number: 5125967Abstract: A composition comprises an isothiazolinone or an isothiazolothione and a substituted urea or a halogen-containing aromatic alkyl sulphoxide or sulphone. The isothiazolinone derivative can be 1,2-benzisothiazolin-3-one. The substituted urea may be 3-(3,4-dichlorophenyl)-1-1-dimethylurea. The sulphoxide or sulphone may be a sulphone derivative such as di-iodomethyl-4-methylphenyl sulphone. A useful composition comprises 1,2-benzisothiazolin-3-one and the specified urea or sulphone derivative. The composition may include other materials including other compounds having anti-microbial properties.Type: GrantFiled: March 29, 1990Date of Patent: June 30, 1992Assignee: Imperial Chemical Industries PLCInventors: Fraser F. Morpeth, Malcolm Greenhalgh
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Patent number: 5122541Abstract: A sprayable aqueous disinfecting composition for disinfecting hard surfaces comprising 20 to 30% by weight of a mixture of ethyl alcohol and isopropyl alcohol in a weight ratio of 1:2 to 2:1, 0.05 to 0.5% by weight of a mixture of a primary or secondary C.sub.10-18 -alkane sulfonate and/or a C.sub.10-18 -alkyl sulfate with a C.sub.10-14 -alkyl ether sulfate, a pH adjusting agent for adjusting the pH in the range of 2 to 6 or 8 to 12, and the remainder to 100% by weight water.Type: GrantFiled: February 20, 1990Date of Patent: June 16, 1992Assignee: Sterling Drug, Inc.Inventors: Heinz Eggensperger, Ute Eggers-Maass, Bernd Lower, Holger Brill, Helmut Nolte
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Patent number: 5118713Abstract: A bactericidal composition and method for inhibiting and controlling the growth of the capsulated, facultative bacterium, Klebsiella pneumoniae, are disclosed. The composition comprises an amount, effective for the intended purpose of diiodomethyl-p-tolylsulfone and 2-bromo-2-nitropropane-1,3-diol. The method comprises administering between about 0.1 to about 200 parts of this combined treatment (based on one million parts of the desired aqueous system) to the particular water containing system for which treatment is desired.Type: GrantFiled: June 21, 1991Date of Patent: June 2, 1992Assignee: Betz Laboratories, Inc.Inventors: Deborah K. Donofrio, Wilson K. Whitekettle
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Patent number: 5108733Abstract: Spontaneous aspecific coloration in so-called Trinder reagents which can alter subsequent colorimetric determinations is inhibited by adding compounds of the chelating agent class to the solution. The resultant compositions contain a peroxidase enzyme, a phenylpyrazone derivative, a compound of phenolic or aromatic amine structure and a stabilizer. Preferred stabilizers are ethylenediaminetetraacetic acid (EDTA) and diethylenetriaminepentaacetic acid (DTPA).Type: GrantFiled: August 30, 1990Date of Patent: April 28, 1992Assignees: Instrumentation Laboratory S.p.A., 501 Instrumentation Laboratory S.p.A.Inventors: Dario Frontini, Maurizio D'Alterio
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Patent number: 5096892Abstract: Anigiogenesis is controlled by administering to a mammal an effective amount of an inhibitor of arylsulfatase. Preferably, the arylsulfatase inhibitor is administered in a pharmaceutically acceptable vehicle in combination with an angiostatic steroid and (optionally) heparin (by which term we include all forms and fragments of heparin having the desired angiostatic activity). Hydrocortisone is one specifically preferred steroid. The preferred arylsulfatase inhibitor is a carboxylic acid ester or a sulfuric acid ester of a benzylic alcohol, most preferably the esters defined more particularly below. The arylsulfatase inhibitor is preferably administered locally to the tissue experiencing undesired angiogenesis. Arylsulfatase inhibitor and an angiostatic steroid are included in a pharmaceutically acceptable vehicle, preferably also with heparin, to yield an angiostatic thereapeutic composition.Type: GrantFiled: May 27, 1988Date of Patent: March 17, 1992Assignees: The Children's Medical Center Corporation, President and Fellows of Harvard CollegeInventors: Moses J. Folkman, Neil T. Chen, Elias J. Corey