Abstract: The invention relates to sulphur- and/or selenium-containing compounds that can inhibit the enzyme inositol mono-phosphatase (IMPase), and which can be used in treating conditions that are treatable through inhibition of this enzyme, such as bi-polar disorder, the compounds having a structure of Formula (I), or is a pharmaceutically acceptable salt thereof; Formula (I); in which: E is S or Se and each of phenyl rings A and B is optionally substituted with one or more substituents, in which each substituent is selected independently from: (1) a halogen, which is preferably selected from F, Cl and Br; (2) C1-C4 alkyl, such as C1-C2 alkyl or C1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and (3) C1-C4 alkoxy, such as C1-C2 alkoxy or C1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br.

Abstract: A synergistic antimicrobial composition containing 1,2-benzisothiazolin-3-one and tris(hydroxymethyl)nitromethane.

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

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 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: The present invention identifies the cholesterol biosynthetic pathway, including the enzyme oxidosqualene cyclase, as new protein targets for anti-tumor therapeutics. The present invention further provides a class of oxidosqualene cyclase inhibitors containing a tertiary amine linked with aromatic ring structures, as a new class of anticancer agents. Compounds disclosed herein have been tested in 19 cell lines including breast cancer, prostate cancer, lung cancer (including drug-resistant lung cancer H69AR), colon cancer, ovarian cancer (including drug-resistant OVCAR-3), and pancreatic cancer cells, as wells as in human breast and prostate xenograft tumor growth in nude mice, and have been shown to be active.

Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

Abstract: The present invention comprises 2-cyanobenzenesulfonic acid amides of the formula (I) and isomeric forms thereof (I-A) and (I-B) wherein R1, R2, R3, R4, R5 and A have the aforesaid meaning for the control of animal pests with the use of penetration enhancers and/or ammonium or phosphonium salts.

Abstract: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.

Abstract: The mechanism of action of Ebselen differentiates between bacterial and mammalian thioredoxin reductase (TrxR). It displays fast oxidation of mammalian Trx and via the NADPH-TrxR catalyzed turnover of ebselen selenol with hydrogen peroxide, and therefore are mammalian antioxidants. Ebselen, and its diselenide, are strong competitive inhibitors of E. coli TrxR with Ki of 0.14 ?M and 0.46 ?M, respectively. E. coli mutants lacking glutathione reductase or glutathione were much more sensitive to inhibition by ebselen. Since either glutaredoxin or thioredoxin systems are electron donors to ribonucleotide reductase, ebselen targets primarily glutathione and glutaredoxin-negative bacteria, a class which includes major pathogens. Ebselen, and similar compounds are therefore useful as antibacterial agents, even for multiresistant strains.

Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

Abstract: Compositions and methods for inhibiting BoNT protease activity are presented. In most preferred aspects, inhibitors comprise a thiol reactive group, a zinc binding group, a redox active group, an alkylating group, and/or an electrophilic Michael addition acceptor group. Particularly preferred inhibitors include an isothiazolone ring, a thiadiazolidine dione ring, a (hydro)quinone ring, an iminophenol group, and/or a hydrazonophenol group, and inhibit BoNT/A at ?M and sub-?M concentrations.

Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.

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: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R1 and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.

Abstract: The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.

Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: The present invention relates to novel benzisothiazol-3(1H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: The present disclosure provides DDAH modulators. Thus, the present disclosure provides a method of treating a patient suffering from a disorder characterized by excessive NO production and/or elevated DDAH activity, the method comprising administering to said patient an effective amount of a compound of one of formulae I-X. The present disclosure also provides a pharmaceutical composition comprising a compound of one of formulae I-X.

Abstract: A phosphate-free, highly-concentrated aqueous dispersion composition comprising at least one biocide, sulfosuccinate based surfactant, block copolymer, suspending agent, and optionally an antifoaming agent and desired additives if any. The composition of the present application is significantly stable against heat, cold, transit, storage and dilution for at least 18 months. The preferred biocides of the dispersion composition are 2-meth-4-isothiazolin-3-one (MIT), 1,2-Benzisothiazolin-3-one (BIT), 5-Chloro-2-methyl-4-isothiazolin-3-one (CMIT), 2-Octyl-4-isothiazolin-3-one (Off) 3-Iodo-2-propynylbutyl carbamate (IPBC), oxyfluorfen, thiabendazole, terbutryn, zinc pyrithione (ZnPy), bronopol, folpet, diiiron, dehydroacetic acid (DHA), dazomet and carbendazim alone or in combination. Also disclosed is a process for preparing the dispersion composition and appropriate applications 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 for treating conditions and disorders using such compounds and compositions.

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: Aqueous solutions of the tetramethylammonium salt of 1,2-benzothiazolone stable below 0° C.

Abstract: Disclosed herein is an aqueous-miscible or aqueous-dispersible biocidal composition of BIT capable of exhibiting substantially enhanced biocidal activity with lesser minimum inhibitory concentration (MIC) level at faster kill rate of gram-negative bacterial strains. The biocidal composition of the present application comprises (i) BIT, (ii) at least one cationic polymer and/or at least one cationic amine surfactant, (iii) optionally one or more sequestering agents, (iv) optionally one or more aromatic aldehydes, and (v) optionally, at least one additive. The composition is volatile organic compounds (VOC) free, heat and cold stable, and has a pH of about 3.0 to about 8.5. Also, disclosed is a process for preparing the aqueous-miscible and aqueous-dispersible compositions and their applications in various fields.

Abstract: The present invention relates to novel benzisothiazol-3(1H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: A preservative composition comprising: (a) 1,2-Benzisothiazolin-3-one (BIT); (b) 3-Iodo-2-propynyl carbamate (IPBC); and (c) a mixture of 5-Chloro-2-methyl-4-isothiazolin-3-one (CMIT) and 2-Methyl-4-isothiazolm-3-one (MIT).

Abstract: Described herein are methods for enhancing airway dilation and/or relieving bronchoconstriction, e.g., to treat obstructive lung diseases such as asthma and COPD, by administering bitter tastants to subjects in need thereof. Also described herein are methods for identifying compounds that modulate function of bitter tastant receptors.

Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: Aqueous solutions of the tetramethylammonium salt of 1,2-benzisothiazolin-3-one and 2-methylisothiazolin-3-one which are stable even at low temperatures and high concentrations.

Abstract: Aqueous solutions of the tetramethylammonium salt of 1,2-benzothiazolone stable below 0° C.

Abstract: The present invention relates to storage-stable biocidal compositions comprising at least one halogen-free isothiazolinone such as in particular 2-methyl-2H-isothiazol-3-one (MIT) and/or 1,2-benzisothiazolin-3-one (BIT) and/or salts thereof, and also stabilizing amounts of copper(II) ions, to a method for preserving technical materials by means of the aforementioned biocidal compositions, and to the technical materials treated therewith.

Abstract: An ecologically compatible anti-microbial-adhesion agent is described, which is particularly suitable for use in anti-fouling paints, preferably for boats, characterized in that it comprises a compound selected from eugenol, vanillin, benzaldehyde substituted with one or two substituents selected from the groups —OH (hydroxy) and —OCH3 (methoxy), or any combination thereof. An anti-fouling paint is also described, particularly for boats, comprising the anti-microbial-adhesion agent mentioned above and other components selected from conventional biocides, solvents, resins, pigments, charges and fillings, and combinations thereof.

Abstract: The present invention provides a medicament that suppresses (or mitigates) various neurological symptoms caused by a peripheral nerve disorder induced by an anti-cancer agent.

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: There is provided a method of making an aqueous dispersion wherein said dispersion comprises (A) one or more thickener and (B) solid particles of 1,2-benzisothiazolin-3-one, wherein said method comprises the steps of (a) forming an aqueous mixture (I) comprising water, a dissolved salt of 1,2-benzisothiazolin-3-one, and optionally one or more thickener, wherein the pH of said aqueous mixture (I) is 8.5 or higher, and (b) subsequently forming said aqueous dispersion by mixing together, in any order, components, wherein said components comprise an acid, said aqueous mixture (I), and optionally one or more thickener, wherein the pH of said dispersion is 1.5 to 7.5. Also provided is an aqueous dispersion made by that method.

Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more heterocyclic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.

Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.

Abstract: This invention relates to synergistic combinations of selected 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) 5-Chloro-2-methyl-4-isothiazolin-3-one+2-Methyl-4-isothiazolin-3-one, (b) Methyl-4-isothiazolin-3-one, or (c) 1,2-Benzisothiazolin-3-one with one or more of a variety of other compounds.

Abstract: Bcl-xL/Bcl-2 binding inhibitors useful in the treatment of unwanted proliferating cells, including cancers and precancers, in subjects in need of such treatment. Also provided are methods of treating a subject having unwanted proliferating cells comprising administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject in need of such treatment. Also provided are methods of preventing the proliferation of unwanted proliferating cells, such as cancers and precancers, in a subject comprising the step of administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject at risk of developing a condition characterized by unwanted proliferating cells.

Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

Abstract: The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent “chemoattractant receptor-homologous molecule expressed on Th2 cells” antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.

Abstract: A low-melting biocidal composition comprising 4,5-dichloro-2-octyl-3(2H)-isothiazolone, 3-iodopropargyl-N-butyl carbamate and at least one C1-C4 alkyl 4-hydroxybenzoate. The composition is stable with regard to agglomeration and crystallization at room temperature.

Abstract: A microbicidal composition in the form of a concentrate includes a) one or more isothiazolin-3-ones, b) one or more organic amines with an alkyl group having at least 8 carbon atoms and c) one or more oxidizing agents. The concentrate is storage-stable and is used for the preservation of technical and domestic products.

Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an isothiazolinone-based biocide, and its use for the control of microorganisms in aqueous and water-containing systems.

Abstract: The invention relates to a microbicidal use solution which comprises a) one or more isothiazolin-3-ones and b) one or two organic amines selected from N-dodecylpropane-1,3-diamine and bis(aminopropyl)-dodecylamine and optionally c) one or more oxidizing agents. The use solution is preferably in the form of technical and domestic products.

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

Abstract: A synergistic antimicrobial composition containing 1,2-benzisothiazolin-3-one and tris(hydroxymethyl)nitromethane.

Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.

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: The present invention relates to biocidal compositions comprising at least one biocidal active substance and at least one solvent from the group of polyglycol monobutyl ethers, and to their use as preservatives and disinfectants. More specifically, the invention provides compositions comprising a) at least one biocidal active substance b) at least one solvent according to the formula I R—(O—CH2—CH2)x—O—H??(I) in which R is a linear or branched butyl group and x is a number from 3 to 10.