Abstract: The invention relates to the field of antiviral agents, and more specifically to antiviral therapy.

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.

Abstract: The present invention relates to cosmetic compositions that comprise a safe and effective amount of a bonding agent comprising trans structure wherein X represents a cosmetic benefit agent, L represents an optional chemical linker between X and a remainder of the bonding agent; and R represents an activating electron withdrawing group; and a cosmetically acceptable carrier for the bonding agent wherein the composition is administered topically to mammalian proteinaceous substrates and wherein the bonding agent reacts with a protein contained in the substrate such that the bonding agent, and thus the cosmetic benefit agent, is covalently attached to the substrate. The invention further relates to methods of using the compositions described above as well as various products that include the claimed compositions.

Abstract: (Z)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1 is selected from the group consisting of hydrogen, chloro and nitro; R2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, bromo, iodo and fluoro; and R3 and R4 are independently selected from the group consisting of hydrogen, lower alkyl, nitro, chloro, bromo, iodo and fluoro; provided that at least one of R1 or R2 is hydrogen. The corresponding (Z)-styryl benzylsulfides are useful as intermediates in the preparation of the biologically active (Z)-styryl benzyl sulfones.

Abstract: Hydroxyeicosatetraenoic acid analogs and methods of their use in treating dry eye disorders are disclosed.

Abstract: Styryl sulfone compounds of the invention selectively inhibit proliferation of tumor cells, and induce apoptosis of tumor cells, while sparing normal cells.

Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the toxic side effects of ionizing radiation. Administration of a radioprotective &agr;,&bgr; unsaturated aryl sulfone compound to a patient prior to anticancer radiotherapy reduces the cytotoxic side effects of the radiation on normal cells. The radioprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increase the dosage of anticancer radiation. In some instances, amelioration of toxicity following inadvertent radiation exposure may be mitigated with administration of &agr;,&bgr; unsaturated arylsulfone.

Abstract: A two-part disinfecting systems, as well as disinfecting compositions and methods for making and using the same. The two-part disinfecting system contains a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition, wherein the first part comprises a chlorite and the second part comprises an acid and an optional oxidizable colorant, and wherein the first part, the second part, or both the first and second parts comprise an alpha olefin sulfonate.

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof:

Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.

Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

Abstract: The mastitis control teat dip composition of the invention provides rapid initial kill, a useful highly pseudoplastic rheology, a barrier/film-forming capacity, a unique antimicrobial composition that is stable over an extended period of time, and unexpected long term microbial control when compared to the prior art materials disclosed in patents and used in the marketplace. The compositions of the invention are made by combining an aqueous thickened liquid composition containing the organic components which can be combined with a simple aqueous solution of a salt of chlorous acid, preferably an alkali metal chlorite. The materials can be combined, blended into a smooth viscous material and can be immediately contacted with the target animals. The .compositions of the invention provide rapid initial kill, consistent long term kill and chemical and rheological stability.

Abstract: (Z)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1 is selected from the group consisting of hydrogen, chloro and nitro; R2 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, chloro, bromo, and fluoro; and R3 and R4 are independently selected from the group consisting of hydrogen, lower alkyl, nitro, chloro, bromo, and fluoro; provided that at least one of R1 or R2 is hydrogen. The corresponding (Z)-styryl benzylsulfides are useful as intermediates in the preparation of the biologically active (Z)-styryl benzyl sulfones.

Abstract: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (I): in which X is one of the radicals: and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Styryl sulfone compounds of the invention selectively inhibit proliferation of tumor cells, and induce apoptosis of such tumor cells, while sparing normal cells.

Abstract: The present invention discloses the use, in the manufacture of a preventive and therapeutic drug of a brain disease, of a compound represented by formula (1): CH2═CH—CH2—S(O)n—R  (1) [wherein R represents a hydrogen atom, an alkyl group, an alkenyl group, a substituted alkyl group, a substituted alkenyl group, an alkylthio group, an alkenylthio group, a phenyl group, a substituted phenyl group, a heterocyclic group, or a group derived from an amino acid or an oligopeptide by deletion of one hydrogen atom, and which group may have a protective group; and n is 0, 1, or 2], a glycoside thereof, or a salt of the compound or the glycoside. The drug of the present invention for ameliorating brain diseases, inhibiting reduction of brain neurons and promoting branching of neurites, is useful for the prevention and treatment of brain diseases such as dementia in association with degeneration and sloughing of brain neurons.

Abstract: The invention relates to the compounds of formula I: wherein one of X1 and X2 is MeSO2 and the other one is hydrogen or halogen and X3 is hydrogen or halogen. These compounds have been found to be useful in the prevention and the treatment of respiratory diseases, especially asthma, ARDS (Acute Respiratory Distress Syndrome), COPD (chronic obstructive pulmonary diseases), allergic rhinitis and related inflammatory conditions. More specifically, the invention relates to the use of said compound in the prevention and the treatment of asthma in steroid-resistant patients. The invention also relates to pharmaceutical formulations used in the treatment of said diseases.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (I): in which X is one of the radicals: ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Iodopropargylamine compound of the general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 combine with each other to form a tetramethylene group or a pentamethylene group, R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, and X and Y each independently represent a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a phenylcarbonyl group or a phenylsulfonyl group, provided that the phenyl group of a phenylcarbonyl group or a phenylsulfonyl group may be optionally substituted by halogen atoms, alkyl groups having 1 to 3 carbon atoms, alkoxy groups having 1 to 3 carbon atoms, nitro groups or trifluoromethyl groups.

Abstract: A stabilized two-part disinfecting system comprising a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition. The first part contains a non-esterifying acid and an alcohol-containing humectant or antifreeze, while the second part contains a salt of an organic acid and an optional metal chlorite. Methods for making a disinfecting composition by mixing the two-part disinfecting system, as well as for disinfecting substrates by contact therewith, are also disclosed.

Abstract: An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): ##STR1## wherein X represents an oxygen atom or a group of formula (2): ##STR2## wherein n represents an integer of from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group; R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R.sub.3 represents a lower alkyl group; and R.sub.4, R.sub.5, and R.sub.6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R.sub.3 and R.sub.4 may be taken together to form a 5-membered ring; or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group; provided that R.sub.6 is nil when R.sub.3 and R.sub.4 are taken together to form benzofuran or benzo[b]thiophene.

Abstract: The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

Abstract: A method of treating a free radical-related medical condition. The method includes the step of administering to a subject in need of such treatment an effective amount of a compound of the formulaF(--X).sub.mwhereinF is a fullerene core; each X is independently OH, (CH.sub.2).sub.n --SO.sub.3 H, or a metal salt of (CH.sub.2).sub.n --SO.sub.3.sup.- in which each n is independently 2-50; and m is 2-40.

Abstract: A composition and method for treating epidermal wounds utilizes an aqueous solution of sodium sulphate, sodium carbonate, sodium bicarbonate, sodium chloride and ichthammol.

Abstract: A liquid bait for target insects and methods of attracting or controlling insects by means of its use. Sorbitol is dissolved in an amount of water sufficient to form an aqueous carrier. The dissolved sorbitol is in a concentration great enough to be effective as a humectant to retard drying of the liquid carrier. The liquid bait further includes at least one insect attractant that is dissolved, dispersed, suspended, or emulsified in the liquid carrier in an amount effective to attract the target insects. The insect attractant may include, in combination, sucrose, fructose, d-maltose, the lithium salt of saccharin, lithium chloride, and vitamins. The liquid bait also may include an effective amount of an insect control active ingredient selected from the group consisting of insecticides, insect growth regulators, chitin inhibitors, insect pathogens, insect-controlling materials derived from insect pathogens, and combinations thereof.

Abstract: This invention provides a novel aqueous pesticide formulation having a fungicidal bicarbonate-containing inorganic salt ingredient which enhances the efficacy of an insecticidal ingredient for treatment of cultivated crops. An invention pesticide formulation also contains a water-soluble organic compound which functions as a compatibility enhancing ingredient in the aqueous pesticide formulation, and improves the spreadability and adhesiveness of the composition ingredients when applied to foliage.

Abstract: Substituted indenyl sulfonyl acetic acids, esters and alcohols are useful in the treatment of psoriasis.

Abstract: This invention provides a method for controlling soilborne fungal disease in cultivated field plants such as a peanut crop. Field crop soil is treated with a free-flowing granular fungicide composition which can be applied by aerial means with minimal settling on plant foliage. The granular fungicide composition comprises ammonium bicarbonate and a solid surfactant ingredient, and is effective against soilborne fungi such as a Sclerotinia, Rhizoctonia, Pythium, Fusarium, Phytophthora or Verticillium species.

Abstract: Disclosed is a method of controlling or inhibiting the growth of microorganisms comprising introducing in, at, or on a locus an antimicrobially effective amount of an antimicrobially active nitroethene compound.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin produced by photodamage which disorders include: wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein n represents 1 or 2, Z represents --SO.sub.2 R, wherein R represents lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkoxy-lower-alkyl, lower-alkanoyl-lower-alkyl, hydroxy-lower-alkyl, halo-lower-alkyl, lower-carbalkoxy-lower-alkyl, lower-alkoxy, hydroxy, mono-lower-alkyl amino or di-lower-alkylaminoand pharmaceutically acceptable salts thereof.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: An improved process for the production of a pharmaceutical composition comprising p-hydroxyacetanilide and L-cysteine or a compound which is converted thereto in vivo comprises mixing p-hydroxyacetanilide and L-cysteine or its precursor in the solid state and then shaping the solid mixture.

Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes alkoxy substituents including a dialkylaminoalkoxy group, an unsubstituted piperazine alkoxy group, a substituted piperazine alkoxy group, an unsubstituted piperidine alkoxy group, and a substituted piperidine alkoxy group, and which may have one or two alkyl groups bonded to the cyclopropane. The compounds are useful as antiestrogens and anti-tumor agents.

Abstract: 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.

Abstract: 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.

Abstract: A method of preventing acetaminophen (APAP)-induced hepatotoxicity utilizing diallyl sulfide (DAS) and diallyl sulfone (DASO.sub.2) is disclosed. DAS and DASO.sub.2 are prepared as an oral dosage form or injected. In a preferred embodiment, diallyl sulfone is added to a dosage form of acetaminophen in an amount effective to prevent the metabolism of said unit dose of acetaminophen into its hepatotoxic metabolites. In certain preferred embodiments, the above formulations further include an effective amount of N-acetylcysteine to detoxify hepatotoxic metabolites of acetaminophen.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: Compounds of formula I ##STR1## wherein X, A, B, R.sup.1 and R.sup.2 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable ester thereof, processes for preparing the compounds and pharmaceutical compositions comprising them. The compounds are useful as potassium channel openers and as therapeutic agents in the treatment of urinary incontinence.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.

Abstract: 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.

Abstract: 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.

Abstract: Novel aluminum and aluminum-zirconium salts are produced by reacting aluminum or aluminum-zirconium halohydrate with an anionic lipophilic component. These salts are useful in antiperspirant compositions or as rheological additives. Also disclosed is a novel process of producing oil-in-water emulsions whereby the novel aluminum or aluminum-zirconium salt functions as a surfactant upon forming.

Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.

Abstract: 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.