Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co-crystals and prodrugs thereof.

Abstract: Provided are anti-wrinkle agents having a novel scaffold that is suitable as components for external skin preparations such as cosmetics. The anti-wrinkle agents comprise compounds represented by general formula (1), stereoisomers thereof, or pharmacologically acceptable salts thereof. Said anti-wrinkle agents have excellent efficacy in improving wrinkles and sagging that are caused by skin aging with increased age or occur as a result of photoaging due to ultraviolet rays exposure. [In the formula, R1 represents a hydrogen atom or a 1 to 8 carbon straight or branched alkyl group. R2 represents —SH, —SO3H, —S—S—X1, —S—X2, —SO—X3, —SO2—X4, —SO2—NY1—X5 or —SO2—NY2—Y3. X1-X5 independently are hydrogen atoms or 1 to 8 carbon aliphatic hydrocarbon groups or 5 to 12 carbon aromatic moiety wherein carbon atoms may be substituted with heteroatoms. Y1 to Y3 independently represent hydrogen atoms or 1 to 8 carbon linear or branched alkyl groups.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Abstract: The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.

Abstract: An object of the present invention is to provide a prophylactic or ameliorating agent for pigmentation having a novel scaffold and an external preparation for skin containing the same as a component.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: Compositions, devices, systems and methods for reducing and/or preventing photo-induced damage of one or more reactants in an illuminated analytical reaction by addition of one or more photoprotective compounds to the reaction mixture and allowing the reaction to proceed for a period that is less than a photo-induced damage threshold period.

Abstract: This disclosure relates to compositions and methods including for the inhibition, prevention, and/or treatment of microbial infections, including infections from such pathogens as Staphylococcus aureus.

Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Abstract: Provided herein are organoselenium compounds and pharmaceutical compositions thereof. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders using the compounds and pharmaceutical compositions provided herein.

Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Provided are anti-wrinkle agents having a novel scaffold that is suitable as components for external skin preparations such as cosmetics. The anti-wrinkle agents comprise compounds represented by general formula (1), stereoisomers thereof, or pharmacologically acceptable salts thereof. Said anti-wrinkle agents have excellent efficacy in improving wrinkles and sagging that are caused by skin aging with increased age or occur as a result of photoaging due to ultraviolet rays exposure. [In the formula, R1 represents a hydrogen atom or a 1 to 8 carbon straight or branched alkyl group. R2 represents —SH, —SO3H, —S—S—X1, —S—X2, —SO—X3, —SO2—X4, —SO2—NY1—X5 or —SO2—NY2—Y3. X1-X5 independently are hydrogen atoms or 1 to 8 carbon aliphatic hydrocarbon groups or 5 to 12 carbon aromatic moiety wherein carbon atoms may be substituted with heteroatoms. Y1 to Y3 independently represent hydrogen atoms or 1 to 8 carbon linear or branched alkyl groups.

Abstract: There are provided a compound represented by a general formula (b1-1) shown below suitable as an acid generator for a resist composition, a compound represented by a general formula (I) shown below suitable as a precursor for the compound represented by the general formula (b1-1), an acid generator, a resist composition, and a method of forming a resist pattern. [Chemical Formula 1] X—Q1—Y1—SO3?M+??(I) X—Q1—Y1—SO3?A+??(b1-1) (wherein, Q1 represents a bivalent linking group or a single bond; Y1 represents an alkylene group which may contain a substituent group or a fluorinated alkylene group which may contain a substituent group; X represents an aromatic cyclic group of 5 to 30 carbon atoms which contains a fluorine atom and may contain a substituent group; M+ represents an alkali metal ion; and A+ represents an organic cation.).

Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.

Abstract: Wrinkles are improved by applying an oral preparation, injection preparation or external skin preparation having a substance that controls heparanase as an active ingredient thereof.

Abstract: A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection.

Abstract: There are provided a novel compound represented by a general formula (b1-1) shown below, which is useful as an acid generator for a resist composition and a manufacturing method thereof, a compound useful as a precursor of the novel compound and a manufacturing method thereof, an acid generator, a resist composition and a method of forming a resist pattern.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

Abstract: Novel fluorescent dyes are disclosed for use in analyte detection. In particular, mono- and bis-substituted HPTS dyes and methods of making them are provided.

Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.

Abstract: A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection.

Abstract: The present invention relates to an enantioselective cation-exchange material, comprising a chiral selector (1), composed of a chiral component (2) and at least one cation-exchange group (X), a spacer (3) and a carrier (4). The cation-exchange material is characterized in that the chiral component (2) has a molecular weight of less than 1,000 and the at least one cation-exchange group (X) is an acid group having a pKa<4.0.

Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.

Abstract: Substantive UV-absorbing water-soluble 2-hydroxy sulfobetaine of cinnamidoalkylamines of Formula I. Hair, skin and fabric care compositions containing the compounds of Formula I. wherein, R1 is a substituent, selected from H, halo, —OH, —NH2, —NO2, —OCH3, —N(CH3)2, alkyl groups containing from 1 to 6 carbon atoms, alkoxy groups containing from 1 to 6 carbon atoms, alkylamino or N,N-dialkylamino groups containing from 1 to 6 carbon atoms; R2 is selected from hydrogen, alkyl group containing from 1 to 12 carbon atoms; R3 and R4 are independently selected from benzyl, alkyl group containing from 1 to 12 carbon atoms, n is an integer from 1 to 6.

Abstract: A cyclic compound comprising m units of the formula Ia. and n units of the formula (Ib) joined together to form a ring, wherein Y and y2 are divalent bridging groups which may be the same or different in each unit; Ro is H or (C1-C6) alkyl or is a metal or amnmonium cation; R5 is H or (C1-C60) alkyl or OH group; j is 1 or 2; R3 is hydrogen, a hydrocarbyl or a hetero-substituted hydrocarbyl group; each of R1, R2 and R4, which may be the same or different, is hydroxyl, hydrogen, hydrocarbyl or hetero-substituted hydrocarbyl, with the provisos that i) at least one of R1, R2, R4 is hydroxyl, and m +n is 4 to 20, m is 1-8 and n is at least 3, and ii) in formula Ia at least one OH group is in the meta or para position to the COORo group and/or at least one R5 group is OH.

Abstract: Derivatives of sulphonic aminoalkane acids, corresponding to formula (I) where X is  R1, R2 and R3 are selected from hydrogen and a C1-C7 alkyl radical, and A is a group of the formula (e) where v and w are 0, 1, 2 or a group of formula (f) where R5 and R6 are selected independently of each other from hydrogen, a C1-C7 alkyl radical, an aryl radical having between 6 and 14 carbon atoms and a heteroaryl radical; t is 1-3; R4 is selected from hydrogen, a C1-C7 alkyl radical, a CF3 radical, an aryl radical having between 6 and 14 carbon atoms and a heteroaryl radical; M is a monovalent metal (Na, K, Li) or a divalent metal (Ca, Mg, Sr, Zn); m is 1 or 2; p is 1-2 and q is 1-2; and where p and q are such that the electrical neutrality of the salt is ensured. The compounds can be used for the treatment of alcohol dependence.

Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.

Abstract: A method and apparatus for purifying crude terephthalic acid from a liquid dispersion thereof also containing impurities selected from unreacted starting materials, solvents, products of side reactions and/or other undesired materials is provided. The method comprises the steps of filtering the dispersion to form a crude terephthalic acid filter cake, dissolving the filter cake in a selective crystallization solvent at an elevated temperature to form a solution, crystallizing purified terephthalic acid from the solution in the crystallization solvent by reducing the pressure and temperature of the solution, and separating the crystallized purified terephthalic acid from the solution. According to the invention, the selective crystallization solvent is non-aqueous, non-corrosive and essentially non-reactive with terephthalic acid. Preferably, the selective crystallization solvent is N-methyl pyrrolidone.

Abstract: Reactive dyes of the formula ##STR1## where n is 1 or 2,G.sup.1 is hydrogen or hydroxyl,G.sup.2 is hydrogen or hydroxysulfonyl,G.sup.3 is hydrogen or arylazo,R.sup.1 is hydrogen or hydroxysulfonylmethyl,R.sup.2 is hydrogen or hydroxysulfonylmethyl, andD is the radical of a diazo or tetraazo component having in each case at least one anchor radical of the formula SO.sub.2 --Y, where Y is vinyl or substituted ethyl,their use for dyeing or printing hydroxyl-containing or nitrogenous organic substrates, and naphthylamines as intermediates therefor.

Abstract: Sulfonyl compounds have the formula ##STR1## where n is 0, 1 or 2,Y is vinyl or a radical of the formula C.sub.2 H.sub.4 Q, where Q is hydroxyl or an alkali-detachable group,E is C.sub.3 -C.sub.6 -alkylene with or without interruption by 1 or 2 oxygen atoms in ether function,Ar is the radical of benzene or naphthalene, andR.sup.1, R.sup.2 and R.sup.3 are each hydrogen, unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, halogen, nitro, amino, hydroxysulfonyl, carboxyl, carbamoyl, sulfamoyl, cyano or a radical of the formula (NH--).sub.m (CH.sub.2 --).sub.q SO.sub.2 --Y, where m is 0 or 1, q is 0, 2 or 3, and Y is as defined above.

Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.

Abstract: A composition comprising a nitrogen-containing olefinic compound and a process for using the nitrogen-containing olefinic compound to produce a water-soluble polymer which has applications in a subterranean formation are provided. The nitrogen-containing olefinic compound can be made from an amine and an alkylating agent. The polymer produced can be used in drilling fluids, workover fluids, completion fluids, permeability corrections, water or gas coning prevention, fluid loss prevention, matrix acidizing, fracture acidizing, and combinations of any two or more thereof.

Abstract: Described herein are disubstituted p-fluorobenzenesulfonamides, containing a CF.sub.3 group, of general formula I ##STR1## which are suitable as NMR diagnostic agents.

Abstract: A process for preparing p-nitroaromatic amides is provided which comprises contacting a nitrile, nitrobenzene, a suitable base and water in the presence of a suitable solvent system to form a mixture, and reacting the mixture at a suitable temperature in a confined reaction zone in the presence of a controlled amount of protic material. The p-nitroaromatic amides of the invention can be reduced to p-aminoaromatic amides. In one embodiment, the p-aminoaromatic amide is further reacted with ammonia under conditions which produce the corresponding p-aminoaromatic amine and the amide corresponding to the nitrile starting material or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-aminoaromatic amine and the acid or salt thereof corresponding to the nitrile starting material. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine.

Abstract: A process for preparing p-nitroaromatic amides is provided which comprises contacting a nitrile, nitrobenzene, a suitable base and water in the presence of a suitable solvent system to form a mixture, and reacting the mixture at a suitable temperature in a confined reaction zone in the presence of a controlled amount of protic material. The p-nitroaromatic amides of the invention can be reduced to p-aminoaromatic amides. In one embodiment, the p-aminoaromatic amide is further reacted with ammonia under conditions which produce the corresponding p-aminoaromatic amine and the amide corresponding to the nitrile starting material or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-aminoaromatic amine and the acid or salt thereof corresponding to the nitrile starting material. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine.

Abstract: New compounds corresponding to formula (I) ##STR1## and their use as emulsifiers for aqueous emulsions and, in the case of carboxylic acid derivatives, also as reactive groups for linking to biologically active substrates. New polymers synthesized from the emulsifiers and other monomers are also claimed.

Abstract: The present invention relates to compounds of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, halogen, or phenyl; Alk.sup.1 represents straight or branched chain alkylene of 2 to 10 carbon atoms which can optionally be substituted by hydroxy, provided that said hydroxy is not attached to a carbon which is adjacent to sulfur or oxygen, X represents sulfur or oxygen, and Alk.sup.2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts thereof. These compounds are specific 5-lipoxygenase inhibitors and are useful as anti-inflammatory and anti-allergy agents and in the treatment of conditions mediated by 5-lipoxygenase.

Abstract: Dyes of formula ##STR1## wherein D is the radical of a diazo component of the benzene or naphthalene series or of the heterocyclic series, R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.2 is phenyl or substituted phenyl, give dyeings of good fastness properties on nitrogen-containing or hydroxyl group containing fibre materials.

Abstract: N-(sulfomethyl)-N'-arylureas inhibit or suppress bitter and sweet tastes when mixed with sweet and/or bitter tasting compositions, such as foods, beverages and pharmaceutical preparations.

Abstract: Novel water-soluble methylenebis(dialkylaniline) derivatives of the following general formula and salts thereof are disclosed. They are useful as dye-forming substances in quantitative determination of peroxides in the copresence of peroxidase or the like. ##STR1## In the formula, R.sub.1 is hydrogen or a substituent selected from lower alkyl and C.sub.2-3 sulfoalkyl or hydroxysulfoalkyl; R.sub.2 is C.sub.2-3 sulfoalkyl or hydroxysulfoalkyl; and R.sub.3 is lower alkyl.

Abstract: Fluorobenzenensulfonamides of Formula I ##STR1## wherein m means the number 0, 1, 2, 3, or 4,n means the number 0 or 1, andY means the residue of an aminocarboxylic or aminosulfonic acid,with the proviso that m and n are not to stand simultaneously for the number 0 and, if desired, the acid groups are present in the form of their amides or in the form of salts with organic or inorganic bases, are suitable for use as NMR diagnostic aids.

Abstract: A compound of the formula ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each C.sub.1 -C.sub.10 alkyl which is unsubstituted or substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, phenyl, sulfo, sulfato, thiosulfato, cyano or halogen, C.sub.5 -C.sub.7 cycloalkyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkoxy, or phenyl or naphthyl which both are unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkanoylamino, benzoylamino, halogen or sulfo, R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.10 alkyl which is unsubstituted or substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, phenyl, sulfo, sulfato, thiosulfato, cyano or halogen, C.sub.1 -C.sub.10 alkoxy which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkoxy, or phenoxy which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.

Abstract: A process for improving the thermal and/or photochemical stability of dyeings on polyamide fibres by applying to said fibres, from an aqueous medium, water-soluble phenolic antioxidants of formula (A--Y--).sub.n Z(--W).sub.m, wherein A, Y, Z, W, m and n are as defined in claim 1.

Abstract: N-(sulfomethyl)-N'-arylureas inhibit or suppress bitter and sweet tastes when mixed with sweet and/or bitter tasting compositions, such as foods, beverages and pharmaceutical preparations.

Abstract: Aminobenzamide derivatives of the formula (I) ##STR1## wherein: R.sub.1 and R.sub.2 each represents a lower alkoxy group,R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower acyl group, a lower alkoxycarbonyl group or --R.sub.5 --SO.sub.3 Z, wherein R.sub.5 represents a lower alkylene group and Z represents an alkali metal or an alkaline earth metal,R.sub.4 represents an amino group, a morpholino group or a lower alkylamino group which may be substituted with a hydroxyl group at the alkyl moiety thereof, with the proviso that, when R.sub.3 represents a hydrogen atom, R.sub.4 cannot be an amino group,Y represents a hydrogen atom, a halogen atom or a lower alkoxy group,n represents an integer of from 1 to 6,and salts thereof; are disclosed. These compounds have excellent anti-peptic ulcer activities, and chemical and physical stabilities.

Abstract: This invention relates to bleaching compounds and compositions that provide effective and efficient surface bleaching of textiles over a wide range of bleach solution temperatures. The bleaching compounds of the invention yield a peroxyacid with a polar amide link in the hydrophobic chain when used in the bleaching compositions. In a preferred embodiment, the bleaching compositions of the invention are also detergent compositions.

Abstract: A new class of polymers and processes used in their preparation are described. These polymers are comprised of crosslinkable aramids, especially aramids that are based on synthetic aromatic amino acids. The aromatic amino acids suggested for this application are selected from the classes of amino benzoic acids, aminodiphenyl carboxylic acids, aminodiphenyl ether carboxylic acids, aminodiphenyl sulfide carboxylic acids, amino diphenyl sulfoxide--and sulfone carboxylic acids, aminonaphtalene carboxylic acids, amino anthracene carboxylic acids as well as their sulfonic acid counterparts, aminopyrimidine carboxylic acids and their crosslinkable and potentially crosslinkable derivatives. Crosslinkable or potentially crosslinkable moieties are selected from a group comprising amino-, nitro-, cyano-, halogene, acetylene, vinyl, acrylic moieties. Crosslinking can be achieved after linear polymers of high molecular weight are produced from low molecular weight prepolymers.