Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.

Abstract: Disclosed is a method for killing spores from a surface or a material, comprising applying an effective amount of a biocidal composition which comprises one or more biguanide polymers, and one or more further active agents on said surface or material, characterised in that the or each further active agent is, when taken alone, sporicidally inactive. Compositions comprising polymeric biguanides and one or more further biocidal agents and, optionally, a polyorganosiloxane, have been found to be effective as a sporicidal agent and are particularly effective against the spores of C. difficile. The compositions may be used in industry, in domestic applications and are particularly suitable for use in hospital due to their low toxicity. Furthermore, the method may comprise impregnating a fabric to thereby provide long lasting sporicidal activity thereto.

Abstract: An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II) wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.

Abstract: This invention relates to synergistic combinations of selected isothiazolin-3-one microbicides in combination with a second microbicide or formulation ingredient or raw material. The combinations have greater efficacy than would be expected from combinations of the individual components. The combinations include mixtures of (a) Methyl-4-isothiazolin-3-one or (b) 1,2-Benzisothiazolin-3-one with one or more of a variety of other compounds.

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

Abstract: A preservative which comprises a) one or more isothiazolones and b) one or more glycerol monoalkyl ethers, and the use of the preservative for microbicidal finishing of cosmetic and pharmaceutical products.

Abstract: In a first aspect of the present invention, there is provided a composition comprising 1,2-benzisothiazolin-3-one dispersed in an aqueous medium and further comprising one or more polysaccharide; wherein either (a) said composition comprises no surface-active compound, or (b) said composition comprises one or more surface-active compounds, and the amount of said surface-active compounds in said composition is less than 0.4% by weight based on the weight of said composition.

Abstract: The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.

Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: Novel classes of viral and fungal inhibitors are disclosed. These compounds are useful in treating, preventing, and/or ameliorating viral infections such as, for example, Hepatitis C Virus, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus, and fungal infections such as, for example, candidiasis.

Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.

Abstract: The disclosure provides new compounds and compositions thereof, and methods for treating or ameliorating a disorder relating to CDG-Ia. In particular, the disclosure provides benzoisothiazolone inhibitors of PMI, which have been synthesized and their ability to drive glycosylation has been demonstrated. The disclosure provides two synthetic routes for these compounds, including a new copper-catalyzed N-arylation reaction amenable to parallel derivitization. The disclosed compounds represent potent inhibitors of PMI, and their dose-dependent efficacy in cell-based models of glycosylation have been demonstrated. In addition, the disclosed compounds are selective over PMM and therefore, are useful in treating or ameliorating a disorder relating to CDG-Ia.

Abstract: Novel classes of 1,2-benzisothiazolinone and isoindolinone compounds and compositions are disclosed. These compounds and compositions are useful in treating, preventing, and/or ameliorating viral, yeast, and fungal infections such as, for example, Hepatitis C Virus, Flavivirus infections, Aspergillus fumigatus, and candidiasis.

Abstract: The present invention relates to combinations of 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, and the biocidal compound 2-butyl-1,2-benzisothiazol-3(2H)one (butylBIT), or a salt thereof, which provide an improved protecting effect against fouling organisms. More particularly, the present invention relates to compositions comprising a combination of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, together with the biocidal compound butylBIT; in respective proportions to provide a synergistic effect against fouling organisms and the use of these compositions for protecting materials against fouling organisms.

Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.

Abstract: A compound of the formula I or where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as as pesticidal agents.

Abstract: What is described herein are antimicrobial compositions which are defined blends of a 1,2-diol and phenoxyethanol which show broad activity against bacteria, fungi and mold spores. This activity is potentiated by the addition thereto of small amounts of a co-biocide for which the blend acts as a delivery system for the otherwise water-insoluble co-biocide.

Abstract: The present technology relates to biocidal compositions and methods that contain and utilize at least one biocidal agent and at least one potentiator system wherein the resultant combination has an enhanced biocidal efficacy. The present technology also discloses a rapid screening assay for determining biocidal compositions with enhanced efficacy, e.g., a microbial contact kill time of 5 minutes or less. Further, the present technology provides a method of determining biocidally effective concentrations of biocidal compositions comprising at least one biocidal agent and at least one potentiator system.

Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.

Abstract: The present invention provides an agent for the prophylaxis or treatment of severe sepsis, which contains a compound represented by the formula (I): or, the formula (II): or a salt thereof or a prodrug thereof, a TLR signal inhibitor containing a non-peptide compound and an agent for the prophylaxis or treatment of organ dysfunction and the like, which contains a TLR signal inhibitory substance.

Abstract: The present invention relates to bitter-taste receptors and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block, bitter taste transduction, or enhance bitter taste response.

Abstract: Disclosed are a composition for inhibiting a proliferation of sulphate reducing bacteria comprising at least one of 1,2-benzisothiazol-3(2H)-one, irgasan, benzyl-2-bromoacetate, 2,2-dibromo-2-cyanoacetamide, and 2-bromo-2-nitropropan-1,3-diol as effective ingredients; a method for inhibiting the proliferation of sulphate reducing bacteria comprising the step of including a sufficient amount for inhibiting the proliferation of sulphate reducing bacteria of at least one of 1,2-benzisothiazol-3(2H)-one, irgasan, benzyl-2-bromoacetate, 2,2-dibromo-2-cyanoacetamide, and 2-bromo-2-nitropropan-1,3-diol in a corrosion sensitive material or degradation sensitive material; a sheet comprising the composition; and a steel plate to which the composition is applied.

Abstract: The invention is directed to indole amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Abstract: A method of inhibiting protein tyrosine phosphatase in a subject includes administering to the subject a therapeutically effective amount of at least one benzo-1,4-quinone, phenyl isothiazolone, or analog thereof to the subject.

Abstract: The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: A stable, aqueous suspension concentrate which includes a solid polymeric dispersant comprising one or more anionic polymeric dispersing agents, optionally a co-dispersant which preferably is a homopolymer and/or a copolymer of a heterocyclic vinyl lactam, preferably in a wt. ratio of 0.1:1 to 1:0.1, a UV-labile, water-insoluble biocide active, and a UV-blocker or UV-absorber to stabilize said active upon storage and/or exposure to sunlight or UV radiation.

Abstract: A combination product including a mixture of 3-iodpropynyl-N-n-butylcarbamate (“IPBC”) and 2-n-N-butyl-1,2-benzisothiazolin-3-one (“BBIT) for use as a fungicide and growth inhibitor in industrial applications. Combination products of the present invention are effective for inhibiting the growth of microorganisms, and exhibit a synergistic antifungal effect against fungi such as, for example, Aspergillus niger, Penicillium funiculosum, Trichoderma virens, Chaetosphaeridium globosum, Penicillium sp., and Caratocystis Pilifera. Methods for using the product in metal working fluids, dry film coatings, in-can preservatives, caulks, sealants leather, wood, rope, cordage, textiles, ink, adhesives and polymeric materials are also described.

Abstract: A compound of Formula (I) or Formula (II) where W is C—R3; X is C—R4; Y is C—R5; R1 and R6, independently of each other, is, for example, H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl or C1-C6-alkyl-C(?O); R2 is H; and R3, R4 and R5, independently of each other, are, for example, H, halogen, cyano, nitro, C1-C6-alkyl, or C1-C6-haloalkyl; provided that in formula II R1 is H and R6 is as defined above; and in formula I that (a) at least one of R1 and R3 to R6 is other than hydrogen, (b) R3 or R4 is other than C1 when in each instance the remaining five groups of R1 to R6 are hydrogen, and (c) (i) R3 is other than methyl, (ii) R4 is other than C1, (iii) R5 is other than C1 and (iv) R3 is not C1 when R5 is methoxy, when in each instance (i) to (iv) R1 is H, R6 is MeC(?O), and remaining groups of R2 to R5 are hydrogen; and/or salts thereof; and their use as as pesticidal agents.

Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.

Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.

Abstract: Biocidal compositions and their use in aqueous media, such as metalworking fluids, the compositions comprising a biocidal agent; and a non-biocidal primary amino alcohol compound of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein.

Abstract: This invention relates to synergistic combinations of selected isothiazolin-3-one microbicides in combination with a second microbicide or formulation ingredient or raw material. The combinations have greater efficacy than would be expected from combinations of the individual components. The combinations include mixtures of (a) Methyl-4-isothiazolin-3-one or (b) 1,2-Benzisothiazolin-3-one with one or more of a variety of other compounds.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.

Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.

Abstract: Biogenic sulfide production is synergistically inhibited by treating sulfate-reducing bacteria (SRB) with a biocide and a metabolic inhibitor. The biocide directly kills a first portion of the SRB. The metabolic inhibitor inhibits sulfate-reducing growth of a second portion of the SRB without directly killing the second portion of the SRB. The treatment of SRB with both a biocide and a metabolic inhibitor provides effective biogenic sulfide inhibition at significantly lower concentrations than would be required if the biocide or metabolic inhibitor was used alone.

Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: Disclosed are fused heterocyclic compounds of Formula (I): or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract: An aqueous suspension concentrate (SC) composition of a crop protection active compound is provided, the concentrate comprising: (a) 50 to 700 g/l of an active ingredient comprising at least one compound active in crop protection; and (b) a concentrate stabilising component consisting of: (i) up to 150 g/l of at least one non-ionic dispersing agent; and/or (ii) to 150 g/l of at least one anionic dispersing agent; and 10 (c) 200 to 800 g/l of water; with the proviso that in the case that the suspension concentrate comprises an active ingredient other than an azole and the concentrate stabilising component consists of an anionic dispersing agent only, the anionic dispersing agent is present in an amount of greater than 30 g/l; or in the case that the suspension concentrate comprises an azole derivative as the active ingredient and the concentrate stabilising component consists of both an anionic dispersing agent and a non-ionic dispersing agent, the anionic dispersing agent is present in an amount of greater th

Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.

Abstract: Disclosed is a pest control agent in the form of a suspension, which exhibits excellent dispersion stability for a long time without forming a hard cake due to settling and separation of solid particles or without losing fluidity due to gelation even when a cationic pest control active ingredient and/or an acid is used. Specifically disclosed is a pest control agent in the form of a suspension, which contains (a) a cationic pest control active ingredient and/or an acid, (b) a nonionic thickening agent, (c) a nonionic surface active agent, (d) a solid active ingredient and (e) water.

Abstract: The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury.

Abstract: This invention is related to the field of compositions useful in the control of pests that eat cellulose, such as, termites, where said composition is compacted and where said composition comprises alpha-cellulose, water, and a pesticide.