Abstract: The present invention relates to a method for producing a 1,2-benzisothiazolin-3-one compound (I) by reacting a 2-halobenzonitrile compound (II) with a thiol compound (III) to form an intermediate (IV) and subsequently reacting the intermediate (IV) with a halogenation agent in the presence of water to form a reaction mixture (RM), comprising the 1,2-benzisothiazolin-3-one compound (I) and a halide compound (V).

Abstract: A method for preparation of 2-alkyl-1,2-benzisothiazolin-3-ones from 1,2-benzisothiazolin-3-one by contacting 1,2-benzisothiazolm-3-one with a dialkyl carbonate in the presence of a base.

Abstract: Sodium sulfide hydrate is at least partially dehydrated by heating with N-methyl 2-pyrrolidone. 2-Chlorobenzamide is added to the mixture which is heated further. The mixture is cooled and treated with aqueous hydrogen peroxide to give the sodium salt of 1,2-benzisothiazolin-3-one in good yield. Acidification if desired gives rise to the free 1,2-benzisothiazolin-3-one.

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: A Schiff base compound configured to detoxify a toxic chemical agent. The toxic chemical agent includes at least one leaving group and the Schiff base compound includes an imine having at least one Lewis base and an alkyl substituent or an aryl substituent having an electron acceptor. The at least one Schiff base nitrogen is spaced way from the electron acceptor by a distance that ranges from about 200 pm to about 1000 pm.

Abstract: N-alkylated 1,2-benzisothiazolin-3-ones can be prepared in good yield and good selectivity by reaction of the lithium salt of 1,2-benzisothiazolin-3-one with an electrophilic alkylating agent.

Abstract: Sodium sulfide hydrate is at least partially dehydrated by heating with N-methyl 2-pyrrolidone. 2-Chlorobenzamide is added to the mixture which is heated further. The mixture is cooled and treated with aqueous hydrogen peroxide to give the sodium salt of 1,2-benzisothiazolin-3-one in good yield. Acidification if desired gives rise to the free 1,2-benzisothiazolin-3-one.

Abstract: The present invention provides a method for producing 1,2-benzisothiazol-3-one compounds by reacting a 2-(alkylthio)benzonitrile compound with a halogenating agent in the presence of water, the method being characterized in that the reaction proceeds while the halogenating agent and water are gradually and simultaneously added to a reaction system containing the 2-(alkylthio)benzonitrile compound. The invention allows the simple and economical production of highly pure 1,2-benzisothiazol-3-one compounds, which are useful as antimicrobial agents, antifungal agents, etc.

Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

Abstract: The present invention provides a method for producing 1,2-benzisothiazol-3-one compounds by reacting a 2-(alkylthio)benzonitrile compound with a halogenating agent in the presence of water, the method being characterized in that the reaction proceeds while the halogenating agent and water are gradually and simultaneously added to a reaction system containing the 2-(alkylthio)benzonitrile compound. The invention allows the simple and economical production of highly pure 1,2-benzisothiazol-3-one compounds, which are useful as antimicrobial agents, antifungal agents, etc.

Abstract: The present invention provides a method for producing a 1,2-benzisothiazol-3-one compound by reacting a 2-(alkylthio)benzonitrile compound with a halogenating agent in the presence of water, wherein an alkyl halide that is generated as by-product is reacted with a sulfide to form an alkylthiol, which is converted into an alkali metal salt, and then the resulting alkali metal salt is reacted with a 2-halobenzonitrile compound to be converted into a 2-(alkylthio)benzonitrile compound and reused as a starting material for the production of a 1,2-benzisothiazol-3-one compound. By means of the present invention, it is possible to efficiently use the by-product that is generated during the production of a 1,2-benzisothiazol-3-one compound and economically produce a 1,2-benzisothiazol-3-one compound without placing a burden on the environment.

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: 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: Sodium sulfide hydrate is at least partially dehydrated by heating with N-methyl 2-pyrrolidone. 2-chlorobenzamide is added to the mixture which is heated further. The mixture is cooled and treated with aqueous hydrogen peroxide to give the sodium salt of 1,2-benzoisothiazoline-3-one in good yield. Acidification if desired gives rise to the free 1,2-benzoisothiazoline-3-one.

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: 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: The present invention provides novel antimicrobial immobilized 1,2-benzisothiazolin-3-one/zinc oxide (BIT/ZnO) complexes useful as antimicrobial agents because of their resistance to being leached from the substrate to which they are attached. The present invention is also directed to methods for preparing the BIT/ZnO complexes, to BIT/ZnO complexes prepared by the novel methods, to methods for using the BIT/ZnO complexes to inhibit microbial growth or reduce the level of bacteria on the surface of a substrate, and to substrates protected to from microbial attack by being treated with the BIT/ZnO complexes. The present invention is further directed to compositions comprising 1,2-benzisothiazolin-3-one which has been immobilized with zinc oxide.

Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

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: 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: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salt and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

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 present invention provides novel antimicrobial immobilized 1,2-benzisothiazolin-3-one/zinc oxide (BIT/ZnO) complexes useful as antimicrobial agents because of their resistance to being leached from the substrate to which they are attached. The present invention is also directed to methods for preparing the BIT/ZnO complexes, to BIT/ZnO complexes prepared by the novel methods, to methods for using the BIT/ZnO complexes to inhibit microbial growth or reduce the level of bacteria on the surface of a substrate, and to substrates protected from microbial attack by being treated with the BIT/ZnO complexes. The present invention is further directed to compositions comprising 1,2-benzisothiazolin-3-one which has been immobilized with zinc oxide.

Abstract: The present invention relates to biocidal mixtures containing at least one biocide that is not a polyamine and at least one polyamine, and also to the use of the abovementioned biocidal mixtures in material protection. A special aspect of the invention relates in addition to a method for decolorizing and/or preventing discolorations of pyrithione-containing industrial materials by polyamines.

Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: What is described herein is a neutral pH, VOC-free biocidal composition of 1,2-benzisothiazolin-3-one which is stable at low temperatures for an extended period of time. The compositions are particularly advantageous in use in protecting latex, paint, coating, cosmetic and personal care formulations against microbiological spoilage.

Abstract: The present invention relates to novel tetracyclic arylsulfonyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylsulfonyl indoles of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy.

Abstract: The invention relates to derivatives of benzo[d]isothiazoles as histone deacetylase inhibitors, selected from among compounds of general formula (Ia) and (Ib) or one of the salts thereof, particularly one of the pharmaceutically acceptable salts thereof, or one of the corresponding solvates thereof. These compounds are histone deacetylase enzyme inhibitors and are suitable as pharmacologically active agents in a medicament for the treatment and/or prophylaxis of disorders or diseases associated to histone deacetylases.

Abstract: A novel class of benzisothiazole-3(2H)-one compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase mediated diseases.

Abstract: The present invention provides novel antimicrobial immobilized 1,2-benzisothiazolin-3-one/zinc oxide (BIT/ZnO) complexes useful as antimicrobial agents because of their resistance to being leached from the substrate to which they are attached. The present invention is also directed to methods for preparing the BIT/ZnO complexes, to BIT/ZnO complexes prepared by the novel methods, to methods for using the BIT/ZnO complexes to inhibit microbial growth or reduce the level of bacteria on the surface of a substrate, and to substrates protected from microbial attack by being treated with the BIT/ZnO complexes. The present invention is further directed to compositions comprising 1,2-benzisothiazolin-3-one which has been immobilized with zinc oxide.

Abstract: A 1,2-benzoisothiazole derivative or a salt thereof is not harmful to a crop and is remarkably effective against agricultural or horticultural plant diseases such as Pyricularia oryzae, Septoria nodorum, Pseudoperonospora cubensis and Colletotrichum orbiculare, and an agricultural or horticultural plant disease-controlling agent containing the derivative or its salt as an active ingredient. The 1,2-benzoisothiazole derivative is represented by the general formula [I]: (wherein R1 is a hydrogen atom or a halogen atom, and R2 is a methyl group or a halogen atom), or a salt thereof.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate 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: 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 invention relates to insecticidal methods using 3-amino-1,2-benzoisothiazole compounds of the formula (I) wherein the variables n and R1 to R6 are as defined in the description. The invention relates to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, and to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects.

Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

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

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: The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to Syndrome X as well as cardiovascular diseases.

Abstract: A composition, suitable for topical application to the skin, containing at least one benzoisothiazolone of formula (I): Novel benzoisothiazolones of formula (I) and a method of caring for dry and/or mature skin.

Abstract: The invention relates to new compounds, 3-phenylpropionic acid derivatives of formula (I) wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; X represents O, S, NH, N—C1–C10-alkyl, N-aryl, NSO2—C1–C10-alkyl, N—SO2-aryl, or N—SO2-heteroaryl; R1 to R8 each independently represents hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof.

Abstract: A process for extracting from aqueous solution the alkali metal or calcium salt of a halo or haloalkyl substituted 2-hydroxypyridine, or a 2-hydroxyquinoline or 2-hydroxybenzothiazole which comprises contacting an aqueous alkaline or neutral solution of the alkali metal or calcium salt, in which is dissolved an alkali metal fluoride, chloride, bromide, hydroxide, sulphate, sulphite, cyanate, cyanide, thiocyanate, thiosulphate, sulphide, phosphate, hydrogen phosphate, carbonate, bicarbonate, borate, chlorate, hypochlorite, perchlorate, nitrite, chromate, dichromate or permanganate or calcium chloride, bromide, nitrate, nitrite, chlorate, hypochlorite, perchlorate, thiocyanate, thiosulphate, chromate, dichtromate or permanganate, with a partially water-miscible organic solvent so as to transfer aqueous solution of the alkali metal or calcium salt of the 2-hydroxypyridine, 2-hydroxyquinoline or 2-hydroxybenzothiasole into the solvent whilst retaining separate aqueous and solvent phases, and thereafter separating

Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.

Abstract: What is described herein is a neutral pH, VOC-free biocidal composition of 1,2-benzisothiazolin-3-one which is stable at low temperatures for an extended period of time. The compositions are particularly advantageous in use in protecting latex, paint, coating, cosmetic and personal care formulations against microbiological spoilage.