Abstract: Compounds of general formula: wherein R0A and R0B are independently selected from hydrogen and pharmaceutically acceptable cations; and RA and RB are identical and selected from amide, carbamate, sulphonamide, azido, cyano and halide. Also, a pharmaceutical composition including one of the compounds. The composition may also include another active ingredient, especially an antineoplastic agent. Further a compound or a composition for use as a medicament, especially a compound or a composition for use in the treatment of a proliferative disease such as for example cancer.

Abstract: The present invention includes compositions and methods for treating certain conditions such as dry eye or dry mouth with a comprising a choline compound; a cholinesterase inhibitor; and Acetyl-L-Carnitine, wherein the composition is provided in an amount sufficient to treat dry eye or dry mouth.

Abstract: Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one.

Abstract: Disclosed is a method of treating or preventing a disease or disorder of the central nervous system (CNS) in a patient comprising administering transcranially, for example, directly to the skull, an effective amount of an anti-inflammatory agent to the patient. Examples of the anti-inflammatory agent include glutathione and inhibitors of purinergic receptors such as P2X4,P2X7, P2Y6, and P2Y12 receptors. Examples of disease or disorder of the CNS include brain injury, particularly traumatic brain injury, inflammation, infection, degeneration of brain cells, stroke, brain edema, tumor, Alzheimer's disease, Parkinson's disease, and multiple sclerosis. Also disclosed is a kit comprising at least one anti-inflammatory agent and printed materials containing instructions for transcranially administering the anti-inflammatory agent to the patient having a disease or disorder of the CNS, disorder of the CNS.

Abstract: This invention relates to powders for reconstitution comprising the NNRTI TMC278 dispersed in certain water-soluble polymers, which can be used in the treatment of HIV infection.

Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.

Abstract: The present invention is directed to nanoparticulate active agent compositions comprising lysozyme as a surface stabilizer. Also encompassed by the invention are pharmaceutical compositions comprising a nanoparticulate active agent composition of the invention and methods of making and using such nanoparticulate and pharmaceutical compositions.

Abstract: A method of treating an effect of a chemical agent, which agent is characterized by one or more chiral centres, by administering a dilution or an ultra-high dilution or potentised preparation of a stereoisomer of said chemical agent.

Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.

Abstract: The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.

Abstract: Use of L-carnitine and/or of one or more alkanoyl L-carnitines or one of their pharmaceutically acceptable salts for the preparation of an ophthalmic physiological supplement or medicament in the form of eye-drops, for the treatment of corneal diseases.

Abstract: The present invention concerns medicaments for slowing ageing. The medicaments can include an inhibitor of microbial folate biosynthesis as well as agents capable of reducing folate uptake by an animal. Examples of such medicaments include inhibitors that reduce the activity of an enzyme in the folate biosynthesis pathway, such as sulfonamides including sulfamethoxazole. The invention also concerns a food supplement, additive, functional food, or nutraceutial comprising the inhibitor or agent or composition as discussed above, as well as methods for screening for an agent for use as a medicament for slowing ageing comprising determining whether a test agent inhibits microbial folate biosynthesis, or whether the test agent reduces folate uptake by a non-human animal.

Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with an agent that generates or induces reactive oxygen species (ROS), significantly enhances the killing of abnormal cells but does not affect normal cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against the abnormal cells.

Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.

Abstract: A novel use of anion channels, preferably Ca2+-activated anion channels (CAACs), in regulating release of neurotransmitters from neurons and/or astrocytes is provided. More specifically, CAAC activity regulators, agents for regulating neurotransmitter release comprising such CAAC activity regulators, and methods of screening agents for regulating neurotransmitter release using CAAC as a target.

Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.

Abstract: A GABA (gamma-aminobutyric acid) release-inhibiting agent in the cerebellum and a composition for treating pathological symptoms caused by over-release of GABA in the cerebellum, each comprising a Bestrophin 1(Best1) channel inhibitor as an active ingredient; a GABA release-promoting agent in the cerebellum and a composition for treating pathological symptoms caused by the deficit of GABA in the cerebellum, each comprising a Best1 channel activator as an active ingredient; and a method for screening a GABA release-regulating agent in the cerebellum, which uses Best1 channel as target, are provided.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: Use of L-carnitine or a pharmaceutically acceptable salt thereof, for the preparation of an ophthalmic physiological supplement or medicament in the form of eye-drops, for the treatment of corneal oedema.

Abstract: The invention relates to a novel injectable liquid formulation of paracetamol, comprising an aqueous solvent, a buffer agent with a pKa between 4.5 and 6.5, an isotonic agent and the dimer of paracetamol of formula (I), a method for preparation of said formulation and the use of said dimer for the stabilisation of a liquid paracetamol pharmaceutical formulation.

Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.

Abstract: A process has been found which increases the efficiency and effectiveness of introducing antimicrobial compounds into complex biofilm matrices through the use of liposome carriers, thereby removing the biofouling in industrial water bearing systems, including piping, heat exchanges, condensers, filtration systems and fluid storage tanks. According to one embodiment of the invention, antimicrobial compound containing liposomes are added to water systems prone to biofouling and biofilm formation. The liposomes, being similar in composition to microbial membranes or cells, are readily incorporated into the existing biofilm. Once the antimicrobial compound containing liposomes become entrained with the biofilm matrix, the decomposition or programmed disintegration of the liposome proceeds. Thereafter, the biocidal aqueous core is released to react directly with the biofilm encased microorganisms.

Abstract: Use of L-carnitine and/or of one or more alkanoyl L-carnitines or one of their pharmaceutically acceptable salts for the preparation of an ophthalmic physiological supplement or medicament in the form of eye-drops, for the treatment of corneal diseases.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Abstract: The selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A response to serotonin (5-HT) is achieved using analogs of oleamide. Selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A leads to a modulation of serotonergic signal transduction of cells having various receptor subtypes. A subset of analogs is identified that inhibits rather than potentiates the 5-HT2A, but not the 5-HT1A, receptor response. These analogs enable the selective modulation of serotonin receptor subtypes and even have opposing effects on the different subtypes. An analysis of the activity of the oleamide analogs discloses that the structural features required for activity are highly selective. In particular, the presence, position, and stereochemistry of the 9-cis double bond is required and even subtle structural variations reduce or eliminate activity.

Abstract: Novel sulfate ester agents and the use of those agents for treating gastroesophageal reflux disease (GERD) are described, exemplary agents being of the formula: wherein X is —OCH2— or —CH2O—; Y is a group pendant from X comprising at least one —OSO3R4 moiety, wherein R4 is H or a pharmaceutically acceptable cation; n is an integer from 1-3; and R1 and R2 are each independently selected from the group consisting of —H, a halogen with an atomic number from 9 to 53, —SO3R4, —NCS, —NCO, —NH(CO)—OR3, —NH(CS)SR3, —NH(C═NH)OR3, —NHCOCH2Cl, —NHCOCH2Br, —NHCO—CH═CH2, —NHC(O)—CF3, wherein R4 is H or a pharmaceutically acceptable cation.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: Carboxylic acid fluorides having a boiling point of preferably less than 100° C. are suitable for use as pesticides. Acetyl fluoride is highly suitable, and Chlorodifluoroacetyl fluoride and trifluoroacetyl fluoride are also very useful. Mixtures of carboxylic acid fluoride pesticides and other pesticides are also disclosed.

Abstract: A synergistic combination of an IL-2 transcription inhibitor (e.g., cyclosporin A or FK506) and 40-O-(2-hydroxyethyl)-rapamycin is provided, which is useful in the treatment and prevention of transplant rejection and also certain autoimmune and inflammatory diseases, together with novel pharmaceutical compositions comprising an IL-2 transcription inhibitor in combination with a rapamycin, e.g., 40-O-(2-hydroxyethyl)-rapamycin.

Abstract: Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Y is O, S or NR6; A is independently hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1 and R6 is independently hydrogen or (C1-C4)alkyl; R2 is independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic(C1-C4)alkyl; R3 is independently hydrogen or (C1-C4)alkyl; R4 and R5 is independently hydrogen, (C1-C4)alkyl, aryl, aralkyl, aryl(C2-C8)alkenyl, aryl(C2-C8)alkynyl, heterocyclic, or heterocyclic(C1-C4)alkyl wherein if one of R4 and R5 is hydrogen or (C1-C4)alkyl than the other of R4 and R5 is other than hydrogen or (C1-C4)alkyl, and its enantiomers and stereoisomers and agronomically acceptable salts.

Abstract: Sulfonic acid stilbenes block the infection of cells by HIV and these compounds can be used to prevent viral infection.

Abstract: Pharmaceutical compositions and a method are disclosed for providing neuroprotective effect to the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon 20 atoms, that may be derived from a lower alkanol.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon atoms, that may be derived from a lower alkanol.

Abstract: A method for controlling phytopathogenic fungi comprises applying a selected fungicidally active N-acetonylbenzamide compound and a second fungicidally active compound selected from the group consisting of manganese-zinc ethylenebis(dithiocarbamate), manganese ethylenebis(dithiocarbamate), zinc ammoniate ethylenebis(dithiocarbamate), zinc ethylenebis(dithiocarbamate), 2-cyano-N-((ethylamino)carbonyl)-2-(methoxyimino)acetamide, and (E,Z) 4-(3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)acryloyl)morpholine to plant seed, to plant foliage or to a plant growth medium and provides higher fungicidal activity than separate use of the same compounds.

Abstract: Sulfonic acid stilbenes block the infection of cells by HSV and CMV and these compounds can be used to treat viral infection.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon atoms, that may be derived from a lower alkanol.

Abstract: Sulfonic acid stilbenes block the infection of cells by HSV, and CMV and these compounds can be used to treat viral infection.

Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.

Abstract: 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.

Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.

Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together represent a polymethylene chain having 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having 1 to 4 carbon atoms, R.sup.3 is hydrogen, hydrocarbyl or substituted hydrocarbyl and X represents cyano, a group --SO.sub.3 M or a group --S--R.sup.4 where M is hydrogen or an alkali metal such as sodium and R.sup.4 is hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 complete a cyclopentene ring, R.sup.3 is alkyl such as methyl and X is a group --SO.sub.3 Na. The compounds have microbiological activity.

Abstract: The invention relates to the use of water-soluble polymers containing chemically bonded tertiary and/or quaternary ammonium groups as auxiliaries for formulating microbicides, the microbicide formulations prepared using these water-soluble polymers and the use of these formulations for preserving industrial materials.

Abstract: Dimercapto-substituted dinitriles are prepared which correspond to the formula: ##STR1## wherein X represents: ##STR2## These compounds have been found to exhibit antimicrobial activity in industrial and commercial applications and compositions containing these compounds are so employed.

Abstract: 3-Thiocyano-2-halo-2-propenenitriles are prepared which correspond to the formula: ##STR1## wherein X is a halogen. These compounds have been found to exhibit a high degree of antimicrobial activity in industrial and commercial applications and compositions containing these compounds are so employed.

Abstract: A pharmaceutical composition and process for preparing the same is provided, wherein the active ingredient of the said composition is one or more compounds of the general formula /I/ ##STR1## In the formula R is longer aliphatic hydrocarbon radical which may contain one or more unsaturation,R.sub.1 is hydrogen or longer aliphatic acyl radical which may contain one or more unsaturation,X is oxygen and Y is hydrogen, orX and Y, when taken together, form a radical of the formula .dbd.N--CH.sub.2 --CH.sub.2 --,z is 1 to 5, andq is 1 to 4.The use of the above compounds in the therapy of tumorous diseases and for regenerating tumorous cells and tissues is also claimed.

Abstract: This invention is directed to a method for treating helminthiasis in an animal which method comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of the Formula (I): ##STR1## wherein Z is oxygen or sulfur;R.sup.1 is hydrogen or lower alkyl; andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen, halo, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, cyano, halophenoxy, haloalkylphenoxy, thiocyano or isothiocyano, provided that R.sup.2 and R.sup.3 cannot simultaneously be hydrogen and that R.sup.4 and R.sup.5 cannot simultaneously be hydrogen; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions formulated therewith. This invention is also directed to novel anthelmintically active benzenepropanamides of Formula (I) wherein Z is oxygen.

Abstract: A method of treating an aqueous or non-aqueous system, including paints and adhesives, is described which comprises adding to the system a thiolan of the formula: ##STR1## wherein each of X and Y, which may be the same or different, represents fluorine, chlorine or bromine, in combination with an alkylene bisthiocyanate and a 2-N-alkyl-4-isothiazolin-3-one.

Abstract: Benzoylaminoalkanoic acids and esters thereof are fungitoxic and useful for controlling fungi, particularly phytopathogenic fungi.