Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.

Abstract: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.

Abstract: A process for the resolution of two enantiomers which involves inducing the preferential crystallization of one enantiomer by adjusting the composition of a suspension or solution including a racemic mixture of the two enantiomers and a solvent, by evaporation of the latter.

Abstract: There is provided a copolymer having the general structure below, wherein a, b, and d are molar ratios varying between about 0.01 and about 0.90 and c is a molar ratio varying between about 0.01 and about 0.90; A1 represents monomer units comprising a cyano-containing pendant group in which the cyano is not directly attached to the backbone of the copolymer; A2 represents monomer units comprising two or more hydrogen bonding sites; A3 represents monomer units that increase solubility in organic solvents; and A4 represents monomer units that increase solubility in aqueous alkaline solutions. There is also provided a near-infrared radiation-sensitive coating composition comprising this copolymer as well as a positive-working thermal lithographic printing plate comprising a near-infrared radiation-sensitive coating comprising this copolymer, a method of producing such a printing plate, and finally a method of printing using such a printing plate. Formula (I).

Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more hydantoin derivatives represented by the following formula (1): wherein R1 and R2, which may be identical to or different from each other, represent a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4, to R8, which may be identical to or different from each other, represent a hydrogen atom, a chlorine atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc.; R3, to R8 may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of V, W, X, Y and Z are nitrogen atoms which have no substituent of R4 to R8.

Abstract: Dicationic azo dyes of the formula (I), which are suitable for coloring keratin fibers, in particular human hair, and are in part themselves still not described in the prior art are provided. In colorations, particularly brilliant and luminous red shades are obtained. Agents for dyeing and optionally simultaneously lightening keratin fibers and methods for dyeing and optionally simultaneously lightening keratinic fibers also are provided.

Abstract: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.

Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.

Abstract: The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched ?-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.

Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.

Abstract: The present invention is related to a new series of chemical compounds, namely 3-benzyl-imidazolidine-2,4-dione substituted in the position 2 and/or 6 of benzyl ring by halogens as presented to the molecule named LPSF-PT-31, GIRSUPAN and its therapeutic use as drug with analgesic, sedative and adjuvant of anesthetics activities. The invention is also related to a process for production of said compounds as well as pharmaceutical compositions comprising them.

Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or

Abstract: The invention relates to new alkoxyalkyl-substituted cyclic ketoenols of the formula (I) in which A, B, D, G, W, X and Y have the definitions indicated above, to processes and intermediates for their preparation, and to their use as pesticides and/or microbicides and/or herbicides. The invention further provides selectively herbicidal compositions which comprise alkoxyalkyl-substituted cyclic ketoenols on the one hand and a crop plant tolerance promoter compound on the other. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetration promoters.

Abstract: An ester compound represented by the formula (I): (wherein, R1 represents a C1-C3 alkyl group, a 2-propenyl group or a 2-propynyl group.) has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.

Abstract: An object of the present invention is to provide an industrially suitable process for preparing an imidazolidin-2,4-dione compound which is safe, simple and easy to prepare the imidazolidin-2,4-dione compound with high yield, which is a useful compound, for example, as a material for decomposing a harmful halogenated aromatic hydrocarbon compound such as dioxin, etc., an electroless silver plating solution for electronic parts, or a diazo copying material, etc. This object can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises subjecting a 4,5-dihydroxy-2-imidazolidinone compound, (1) to dehydration reaction in the presence of an acid catalyst(s); or (2) to reaction at 100 to 300° C. Or, it can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises reacting a mixed solution of a urea compound, glyoxal, and a base at 20 to 300° C.

Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.

Abstract: The present invention provides a compound represented by formula (I): wherein n is an integer selected from 1 to 20, Q is A is cyano or the like; B is hydrogen, halogen, or the like; X1 and X2 are each independently selected from O and S; E is a C1-4 alkyl group; and R1, R2, R3 and R4 are each independently selected from a hydrogen atom and a C1-C6 alkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.

Abstract: Imidazolone derivatives, as medicaments, of formula wherein: R1?H, C1 to C5 alkyl, aryl or a 5- or 6-membered heterocyclic group; Ar1=optionally substituted aryl or an aromatic heterocycle; R?R2—S—, R3—HN—, R4COHN or Ar2, with R2=a C1-C5 alkyl, vinyl or vinyl(C1-C5)alkyl, nitrile or nitrile(C1-C5)alkyl, aryl or benzyl radical, which are optionally substituted; R3=the meanings given above and H; Ar2=substituted or unsubstituted aryl.

Abstract: A novel process for the preparation of hydantoin sulfonyl chlorides of general formula (I) wherein R and n are as specified in the description, and certain novel intermediates thereto, are disclosed.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched ?-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.

Abstract: The present invention relates to a whole cell catalytic system for the preparation of an enantiomerically enriched ?-amino acid from a corresponding hydantoin wherein hydantoinase, L-carbamoylase and hydantoin racemase are coexpressed in a recombinant micro-organism wherein the genes coding for these three enzymes are located on a single replicon. The present invention further relates to the use of such a whole cell catalytic system according in the preparation of an enantiomerically enriched L-?-amino acid from a corresponding hydantoin.

Abstract: The present invention is related to a new series of chemical compounds, namely 3-benzyl-imidazolidine-2,4-dione substituted in the position 2 and/or 6 of benzyl ring by halogens as presented to the molecule named LPSF-PT-31, GIRSUPAN and its therapeutic use as drug with analgesic, sedative and adjuvant of anesthetics activities. The invention is also related to a process for production of said compounds as well as pharmaceutical compositions comprising them.

Abstract: Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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 relates to hydantoin derivatives having RNase H, polymerase and/or HIV reverse transcriptase modulatory, and particularly, inhibitory activity. Included in the invention are the hydantoin derivatives, compositions containing the derivatives, methods of synthesis of the derivatives, screening methods to identify the derivatives, and methods of treatment using the hydantoin derivatives, including the treatment of HIV, AIDS and retrovirus-associated cancer.

Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: The present invention relates to a novel compound of the formula I: and/or all stereoisomeric forms of the compound of the formula I and/or mixtures of these forms in any ratio, and/or a physiologically tolerated salt of the compound of the formula I, in which R1 to R5 and V1, V2 have the meanings stated in the claims and specification. The inventive compounds are suitable as inhibitors of metalloproteases, especially of ADAMTS proteases and TNF-? converting enzyme (TACE), and for the treatment of disorders such as but not limited to osteoarthrosis and rheumatoid arthritis.

Abstract: Compounds corresponding to the following general formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine or else into cosmetic compositions; novel compounds of formula (II) are also thus useful:

Abstract: An object of the present invention is to provide an industrially suitable process for preparing an imidazolidin-2,4-dione compound which is safe, simple and easy to prepare the imidazolidin-2,4-dione compound with high yield, which is a useful compound, for example, as a material for decomposing a harmful halogenated aromatic hydrocarbon compound such as dioxin, etc., an electroless silver plating solution for electronic parts, or a diazo copying material, etc. This object can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises subjecting a 4,5-dihydroxy-2-imidazolidinone compound, (1) to dehydration reaction in the presence of an acid catalyst(s); or (2) to reaction at 100 to 300° C. Or, it can be solved by a process for preparing an imidazolidin-2,4-dione compound which comprises reacting a mixed solution of a urea compound, glyoxal, and a base at 20 to 300° C.

Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.

Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.

Abstract: Novel diphenyl ether derivatives are provided that exhibit activity useful for reducing glucose, cholesterol, and/or triglyceride levels in plasma, and for treatment of obesity, inflammation, immunological diseases, autoimmune diseases, diabetes and disorders associated with insulin resistance.

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an ? bonds, the solid triangle represents a ? bond, the wavy segments represent ? or ? bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.

Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.

Abstract: The present invention provides a production method of optically active hydroxymethyl-substituted phenylalanine, which includes reducing cyano-substituted benzylidene hydantoin (1) to give aminomethyl-substituted benzyl hydantoin (2) or a salt thereof, converting an amino group of the aminomethyl-substituted benzyl hydantoin (2) or a salt thereof to a hydroxyl group to give hydroxymethyl-substituted benzyl hydantoin (3), treating the hydroxymethyl-substituted benzyl hydantoin (3) with an enzyme to give D-hydroxymethyl-substituted phenylalanine (4a) or a salt thereof, or L-hydroxymethyl-substituted phenylalanine (4b) or a salt thereof. According to the present invention, a production method capable of conveniently producing optically active hydroxymethyl-substituted phenylalanine on an industrial scale can be provided.

Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.

Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease

Abstract: 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione and analogues useful as inhibitors of macrophage elastase are disclosed.

Abstract: A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide.

Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system

Abstract: Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33: where the substituents are described herein.

Abstract: The present invention provides heterocyclic vinylic compounds that can be used to form biocidal polymers. The polymers thus generated can used alone or can be grafted onto textiles, fabrics and polymers. The polymers are readily converted to N-halamine structures on exposure to a halogen source such as commercially available chlorine bleach. The N-halamine derivatives exhibit potent antibacterial properties against microorganisms and these properties are durable and regenerable.

Abstract: The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia:

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.