Abstract: Compounds, compositions and methods for the treatment of malignancy are disclosed.

Abstract: It is an object of the present invention to provide a gel-forming composition which permits on-site administration and can form a gel exhibiting prescribed strength and sustained drug release, devices for the administration thereof, and a kit for medical use. A gel-forming composition which is composed of the first composition comprising a drug, a first gelling agent represented by the general formula (I) and the like, and the first diluent and the second composition comprising the second gelling agent represented by the general formula (I) and the like and the second diluent; and application devices and kits for medical use, which can hold the gel-forming composition. X1—(OCH2CH2)n—X2 (I) wherein X1 and X2 are each —R1COONHS (wherein R1 is C1-7 alkylene), —COR1COONHS, —NOCOR1—R2 (wherein R2 is maleimido), —R1NH2, —R1SH, or —CO2PhNO2, and n is an integer of 80 to 1000.

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: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).

Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.

Abstract: The invention relates to a preservative comprising at least one isothiazolone, at least one quaternary ammonium compound, and at least one stabilizer selected from the group of sulphite salts, hydrogen sulphite salts, sulphite-releasing compounds and hydrogen-sulphite-releasing compounds, the presence of algicidal triazine being ruled out. The preservative inhibits the growth of fungi, algae and bacteria on or in alkaline coating compositions. The invention furthermore relates to a process for the preparation of the preservative, to its use in a coating composition, and to the preserved composition.

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: A method of controlling or preventing pest damage in a plant propagation material, a plant, and/or plant organs that grow at a later point in time, which comprises applying on the plant propagation material or locus thereof a compound I or II represented by formula (I) and (II) wherein R1 is represented, for example, by H; R6 is represented, for example, by H; R2 is represented, for example, by halogen; R3 to R5 is represented, for example, by H; and n is either 0 or 2; or an enantiomer, diastereomer, or salt, thereof.

Abstract: The present invention relates to 3-amino-1,2-benzisothiazole compounds of formula I wherein R1, R2, R3, R4, R5 and n are defined in the description. The present invention relates to insecticidal compounds of formula I and to their isomeric imino derivatives, as well as to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the 3-amino-1,2-benzisothiazole compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds.

Abstract: Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

Abstract: Compositions and methods for treating disorders of the outer retina with compounds with 5-HT1A agonist activity are disclosed.

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: There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s); R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); Xa and Xb are each C, N, O or S; Xc and Xd are each C or N; m is 0-2; n is 1-3; ring A is a 5-membered ring optionally having substituent(s); ring B is a 6-membered ring optionally having substituent(s); and ring C is a 3- to 5-membered ring optionally having substituent(s), provided that when Xa, Xc and Xd are each C, then Xb is N or S, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.

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: Compounds, compositions and methods for the treatment of malignancy are disclosed.

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 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: Compounds having the formula i wherein m, R1, R2, R4 and X1 are herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and synthetic intermediates used in the process.

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: A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.

Abstract: Highly concentrated, water-based dispersions of certain lipophilic and/or hydrophobic antimicrobially active materials are stabilized to a surprising degree by a surfactant combination including a nonionic acrylic graft copolymer surfactant and a alkoxylated polyarylphenol phosphate ester surfactant. The active materials may be present in dispersion concentrates of the present invention singly or in useful combinations. The active materials are selected from the group of fungicides and bactericides consisting of 1,2-benzisothiazol-3(2H)-one; 2-octyl-2H-isothiazol-3-one; 5-chloro-2-methyl-2H-isothiazol-3-one; 2-methyl-2H-isothiazol-3-one; pyrithione zinc; 3-iodo-2-propynyl butylcarbamate; 2-methylthio-4-ethylamino-6-tert-butylamino-s-triazine; and 3-(4-isopropylphenyl)-1,1-dimethylurea, and mixtures thereof. The dispersion concentrates may be efficiently shipped and stored, and subsequently diluted with water to produce less concentrated dispersions when desired.

Abstract: The present invention provides an emulsion composition comprising (A) a compound stable in an acidic range, and (B) a buffer, wherein the pH is adjusted from about 3.7 to about 5.5.

Abstract: A stable, low VOC, low viscosity biocide formulation comprising an effective amount of at least one biocide, 1,2-benzisothiazolin-3-one (BIT), and a polyglycol liquid carrier of formula (I): R—O-(AO)n—O—R1, wherein n is 4-25, R and R? are hydrogen, C1-C3 alkyl groups, O?C—CH3 group, or O?C—C2H5 group, and AO is a) CH2CH2O, or b) CH2CH2O/CH2CHMe-O block or random copolymer; with proviso that when R and R? are both hydrogen, AO is a block or random copolymer. A method of making such a formulation.

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 provides 3-amino-1,2-benzisothiazole compounds of formula (I) wherein n, R1, R2, R3, R4 and A are defined as in the description.

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: An antiseptic preparation is provided for the production of wound dressings or bandages. The preparation includes at least one alginate and at least one antiseptically active substance selected from the group biguanide derivatives, octenidine and taurolidine. Processes for the production of the antiseptic preparations, and the use thereof, are also provided.

Abstract: The invention concerns the combination of a short-acting hypnotic agent and a compound of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The combination of this invention is useful in treating a variety of sleep disorders.

Abstract: Compounds having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein L, A, G, R1, R2 and R3 are as defined herein. These compounds are particularly useful in the treatment of pain, inflammatory hyperalgesia, and urinary dysfunctions, such as bladder overactivity and urinary incontinence.

Abstract: Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.

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

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.

Abstract: A sultam derivative of Formula (1) described below having inhibitory action for aggrecanase activity is provided. The sultam derivative of Formula (1) and a salt thereof exhibit strong inhibitory action for aggrecanase activity in a living body of a mammalian animal including human, and is useful, for example, as an active ingredient of a pharmaceutical agent for preventing and/or treating various diseases caused by degradation of aggrecan.

Abstract: The present invention provides methods and compositions for the prophylaxis of blood cell disorders such as neutropenia, thrombocytopenia, lymphocytopenia, and anaemia. The invention provides methods wherein compositions comprising at least one cytokinin compound are administered either therapeutically or prophylactically. The invention further has utility in methods of DNA repair.

Abstract: The present invention provides compounds and methods for the treatment of diabetic retinopathy. In particular, LFA-1 antagonists are described herein to be used in the treatment of diabetic retinopathy. One aspect of the invention provides for diagnosis of diabetic retinopathy and administration of a LFA-1 antagonist, after the patient is diagnosed with diabetic retinopathy.

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: The present invention provides an agent for the prophylaxis or treatment of complications after coronary-artery bypass surgery or cardiac diseases, autoimmune diseases, central nervous system diseases, inflammatory diseases, sepsis, severe sepsis or septic shock in a patient who undergoes coronary-artery bypass surgery, which comprises a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof, and an agent for the prophylaxis or treatment of sepsis and the like, as well as complications after coronary-artery bypass surgery, which is prepared for administration of ethyl (6R)-6-[(2-chloro-4-fluoroanilino)sulfonyl]-1-cyclohexene-1-carboxylate or a salt thereof or a prodrug thereof in a specific dose at a specific administration time.

Abstract: This invention relates to biocidal compositions in the form of solutions, containing a) 1,2-benzisothiazolin-3-one (formula I) and/or a salt thereof, preferably its alkali metal or ammonium salt, in particular its lithium, sodium or potassium salt; b) 1,2-dibromo-2,4-dicyanobutane (formula (II)); c) at least one solvent which is a mixture of a compound of the formula III with glycerol (formula (III)); wherein R1 and R2 are each independently hydrogen or a linear or branched, saturated or unsaturated alkyl group having 1 to 8 carbon atoms, (O-A) is an alkoxy group selected from an ethylenoxy group (EO), propylenoxy group (PO), butylenoxy group and/or phenylethoxy group, x represents a number ranging from 1 to 15 and y represents a number ranging from 0 to 10.

Abstract: Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.

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: 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: 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.