Abstract: The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein R1 and R2 independently denote C1-3-alkyl groups and X? denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.

Abstract: To address the problem of insufficient biodegradability of perfluorinated surfactants, the present invention provides biodegradable fluorosurfactants derived from olefins having —CHR, —CHRf, —CHF, and/or —CH2 groups, where R is an alkyl group and Rf is a perfluoro or fluroroalkyl group. Preferably, the —CHR, —CHRf, —CHF, and/or —CH2 groups are contained within partially fluorinated alkenes.

Abstract: The present invention relates to aryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors

Abstract: A flavour composition comprising a compound according to the formula (I) and edible salts thereof, wherein R1 is an alkyl residue containing 6 to 20 carbon atoms, or an alkene residue containing from 9 to 25 carbon atoms with 1 to 6 double bonds, R1 together with the carbonyl group to which it is attached is a residue of a carboxylic acid, and m is 0 or 1.

Abstract: 4-[(Haloalkyl)(dimethyl)ammonio]butanoates of formula wherein Hal is Cl or F, n=1 or 2, method for preparing thereof and use thereof for treating cardiovascular disease.

Abstract: The present invention provides a macromolecular dispersant and a synthesis method thereof, and the dispersant is synthesized by reacting polyisobutylene-g-succinic anhydride with amine compounds. In addition, the present invention also provides an oil-soluble dispersant composition with nano particle pigments and the manufacturing method thereof. The oil-soluble dispersant composition is manufactured by milling a macromolecular dispersant with a pigment and a grinding media. The oil-soluble dispersant composition is adequate for various pigments, shows the excellent immiscibility of oil/water interface, and owns the low viscosity of ?4 cps and the optical density of ink ?1.1. Therefore, the oil-soluble dispersant of the present invention for the nano particle pigment can be acted as the material of the electrowetting display.

Abstract: A process is described for preparing acylglycinates of the formula (I) wherein R1 is a linear or branched, saturated alkanoyl group having 6 to 30 carbon atoms, or is a linear or branched, singly or multiply unsaturated alkenoyl group having 6 to 30 carbon atoms, and Q+ is a cation selected from the alkali metals Na+ and K+, the process being characterized in that glycine is reacted with fatty acid chloride R1Cl, wherein R1 possesses the definition stated in formula (I), in water and in the presence of a basic alkali metal compound which yields cations Q+ selected from Na+ and K+, but in the absence of organic solvents, at 25-50° C., and the fraction of fatty acid chloride R1Cl containing unsaturated acyl groups R1 having 18 carbon atoms, based on the total amount of fatty acid chloride used, is greater than or equal to 2.

Abstract: The present invention provides a method of preparing an alkylamine derivates which hardly generates impurities and enables mass production with high purity.

Abstract: 4-[(Haloalkyl)(dimethyl)ammonio]butanoates of formula wherein Hal is Cl or F, n=1 or 2, method for preparing thereof and use thereof for treating cardiovascular disease.

Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.

Abstract: Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials, dental bonding agents or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such dental restorative materials may help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.

Abstract: The problem of the present invention is provision of a cleansing composition providing good amount and good quality of lather. Using a particular alkenoic acid or a salt thereof, the above-mentioned problem can be solved. In addition, the cleansing composition provided by the present invention is stable in various formulations and also useful for rough skin and damaged hair.

Abstract: The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.

Abstract: ?-Trifluoromethyl-?-substituted-?-amino acids can be produced by allowing ?-trifluoromethyl-?-substituted-?,?-unsaturated esters to react with hydroxylamine to convert ?-trifluoromethyl-?-substituted-?,?-unsaturated esters into dehydrogenated closed-ring body of ?-trifluoromethyl-?-substituted-?-amino acid, and by hydrogenolyzing the dehydrogenated closed-ring body. According to this production process, novel ?-trifluoromethyl-?-substituted-?-amino acids which are free amino acids whose functional groups are not protected can be produced, in which ?-position substituent is not limited to aromatic ring group or substituted aromatic ring group while the relative stereochemistry of ?-position and ?-position can be also controlled.

Abstract: Quaternary ammonium, betaine, or sulfobetaine compositions derived from fatty amines, wherein the fatty amine is made by reducing the amide reaction product of a metathesis-derived C10-C17 monounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives and a secondary amine, are disclosed. Quaternary ammonium, betaine, or sulfobetaine compositions derived from fatty amidoamines, wherein the amidoamine is made by reacting of a metathesis-derived C10-C17 monounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives and an aminoalkyl-substituted tertiary amine, are also disclosed. The quaternized compositions are advantageously sulfonated or sulfated. In one aspect, the ester derivative of the C10-C17 monoun-saturated acid or octadecene-1,18-dioic acid is a lower alkyl ester. In other aspects, the ester derivative is a modified triglyceride made by self-metathesis of a natural oil or an unsaturated triglyceride made by cross-metathesis of a natural oil with an olefin.

Abstract: The present invention relates to a new and competitive process for the preparation of 4-amino-5-hexenoic acid and intermediates thereof. The compound, and compositions containing the compound as an active ingredient, can be used for the treatment and/or prophylaxis of epilepsy and West syndrome.

Abstract: The present invention provides a method for producing modified stable polypeptides introducing at least one non-natural amino acid into the hydrophobic region of the polypeptide. The thermal and chemical stability of such polypeptides is improved compared to those properties of its corresponding wild type proteins. The invention further provides purified leucine zipper and coiled-coil proteins in which the leucine residues have been replaced with 5,5,5-trifluoroleucines, and the modified proteins so produced demonstrate increased thermal and chemical stability compared to their corresponding wild-type natural proteins.

Abstract: Compounds according to formula (I) are particularly suitable for the treatment and/or prevention of a medical condition involving hypoxic, anoxic and/or inflamed mammalian tissue. Furthermore, the invention relates to the use of said compounds for preparing a medicament and to pharmaceutical preparations comprising such compounds.

Abstract: There are provided a processing liquid for suppressing pattern collapse of a fine metal structure, containing at least one member selected from the group consisting of an ammonium halide having a fluoroalkyl group, a betaine compound having a fluoroalkyl group, and an amine oxide compound having a fluoroalkyl group, and a method for producing a fine metal structure using the same.

Abstract: The present invention relates to a method of treating or preventing a convulsive disorder in a patient in need thereof comprising administering said patient with a therapeutically effective amount of an active ingredient that induces a high level of extracellular GABA or increases GABA receptor activation once per day in the evening or at night.

Abstract: The present invention provides compounds (n-3 PUFA derivatives) of formula (I) that modulate conditions associated with cardiac damage, especially cardiac arrhythmias.

Abstract: Disclosed are ?-amino acids that are unsubstituted in the ? position; that are substituted in the ? position with an aryl group; that are substituted in the ? position with an aryl group; that bear two substituents in the ? position; and/or that are substituted in the ? and ? positions with groups which, together with the carbon atoms at the ? and ? positions, form a ring. Also disclosed are methods for making the above-mentioned ?-amino acids and other ?-amino acids which involve providing an ?,?-unsaturated imide; converting the ?,?-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a ?-amino acid.

Abstract: The present invention provides a method of preparing an alkylamine derivates which hardly generates impurities and enables mass production with high purity.

Abstract: The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.

Abstract: Embodiments of this disclosure, among others, encompass methods for generating alkenes under mild thermolytic conditions that can provide almost total conversion of a precursor compound to an alkene without isomerization or the need to chromatographically purify the final product By selectively blocking the amino and carboxy groups of the de?vatized amino acid, the methods of the disclosure provide for the synthesis of a peptide having the vinylglycine moiety at either the carboxy or the amino terminus of the peptide The mild conditions for the thermolytic removal of an o-NO2-phenyl substituted aryl group ensure that there is minimal if any damage to thermally sensitive conjugates such as a peptide bearing the vinylglycine The methods of the present disclosure have practical applications for the preparation of unsaturated compounds under mild, thermolytic conditions.

Abstract: Disclosed are ?-amino acids that are unsubstituted in the ? position; that are substituted in the ? position with an aryl group; that are substituted in the ? position with an aryl group; that bear two substituents in the ? position; and/or that are substituted in the ? and ? positions with groups which, together with the carbon atoms at the ? and ? positions, form a ring. Also disclosed are methods for making the above-mentioned ?-amino acids and other ?-amino acids which involve providing an ?,?-unsaturated imide; converting the ?,?-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a ?-amino acid.

Abstract: RF-compositions including surfactants, foam stabilizers, monomers, polymers, urethanes, intermediates, metal complexes, phosphate esters as well as telomerization methods are provided.

Abstract: ?-Trifluoromethyl-?-substituted-?-amino acids can be produced by allowing ?-trifluoromethyl-?-substituted-?,?-unsaturated esters to react with hydroxylamine to convert ?-trifluoromethyl-?-substituted-?,?-unsaturated esters into dehydrogenated closed-ring body of ?-trifluoromethyl-?-substituted-?-amino acid, and by hydrogenolyzing the dehydrogenated closed-ring body. According to this production process, novel ?-trifluoromethyl-?-substituted-?-amino acids which are free amino acids whose functional groups are not protected can be produced, in which ?-position substituent is not limited to aromatic ring group or substituted aromatic ring group while the relative stereochemistry of ?-position and ?-position can be also controlled.

Abstract: The invention describes compounds useful for labelling molecules of interest (i.e. analytes), particularly biomolecules such as peptides, proteins, oligonucleotides and nucleic acids, and also methods for analysing, detecting and/or isolating these labelled molecules using mass spectrometry. The compound in one aspect is a mass marker for labelling of an analyte detectable by mass spectrometry such as neutral loss mass spectroscopy, in which the mass marker comprises a neutral loss mass modifier linked via a first collision cleavable linker to a reactive group having reactive functionality for attachment to the analyte. The neutral loss mass modifier upon cleavage from the analyte during mass spectroscopy is uncharged.

Abstract: Compounds represented by formula (Rf-Q-X)s—Z. Each Rf is independently a partially fluorinated or fully fluorinated group selected from Rfa-(O)r—CHF—(CF2)n—; [Rfb-(O)tC(L)H—CF2—O]m—W—; CF3CFH—O—(CF2)p—; CF3—(O—CF2)z—; and CF3—O—(CF2)3—O—CF2—. Methods of reducing surface tension of a liquid, making foams, and treating a surface using the compounds are also disclosed.

Abstract: Disclosed herein are compositions, methods, uses, and devices having antiseptic and anticoagulation properties in a mammal. The compositions, methods, uses, and devices are based on a therapeutically effective amount of one or more N-halogenated or N,N-dihalogenated amines, analogues or derivatives thereof, or pharmaceutically acceptable salts and esters. The preferred compound is N-chlorotaurine.

Abstract: The present invention relates to drugs consisting of unsaturated fatty amino-acid derivatives of the general formula (I), and to their pharmaceutically acceptable acid addition salts, in which: X is oxygen or NH, Rn are independently hydrogen or a (C1-C6)alkyl optionally substituted by halogen; R1 is hydrogen, fluorine, chlorine or bromine, or a CF3 or CHF2 or a (C1-C6)alkyl, (C1-C6)alkenyl or (C1-C6)alkynyl, optionally substituted by one or more halogen atoms; R is hydrogen or a (C1-C6)alkyl or (C3-C6)cycloalkyl optionally substituted by one or more halogen atoms; Ra and Rb are independently hydrogen (C1-C6)alkyl or (C1-C6)acyl, and Ra and Rb a hydrocarbonated cycle containing 4 to 6 carbon atoms; and n is an integer between 2 and 14.

Abstract: The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.

Abstract: A polyurethane resin is synthesized from a compound represented by the following Formula (1), a polymerizable composition includes the polyurethane resin, a planographic printing plate precursor includes a photosensitive layer including the composition, and a method produces a diol compound that can be used as a raw material of the polyurethane resin. In Formula (1), R1 and R2 each independently represent a single bond or an alkylene group optionally having a substituent, R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl group, and A represents a divalent or higher linking group, provided that R1 and R2 are not both a single bond.

Abstract: A novel compound (I) represented by the following formula (1) is provided which is suitable for a dental composition and has a polymerizable group, a carboxyl group and a phosphoric acid group. A method for producing a polymerizable amide is provided, which method can make a condensation reaction of a carboxylic acid with an amine to proceed easily and is excellent in safety: wherein R1, R2 and R3 each independently are a hydrogen atom or a hydrocarbon group having 1 to 20 carbon atoms which may have a substituent; (A) and (B) are each any constituent unit; m is an integer of from 1 to 3; n is an integer of from 1 to 3; R4 is an organic group having 1 to 40 carbon atoms which may have a substituent; R5 is a hydrocarbon group having 1 to 20 carbon atoms which may have a substituent, R6 and R7 each independently are a hydrogen atom, a hydrocarbon group having 1 to 20 carbon atoms which may have a substituent, or a metal atom.

Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.

Abstract: The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of ?-aminoisobutyric acid (AIB) analogs namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. In addition the compounds can be labeled with technetium and rhenium isotopes using known chelation complexes. The amino acid compounds disclosed herein have a high specificity for target sites when administered to a subject in vivo. The labeled amino acid compounds are useful as imaging agents in detecting and/or monitoring tumors in a subject by Positron Emission Tomography (PET) and Single Photon Emission Computer Tomography (SPECT).

Abstract: Corrosion and gas hydrate inhibitors having improved water solubility and increased biodegradability The invention thus provides the use of compounds of the formula (1) where R1, R2 are each independently C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R3 is C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C10-alkylene group, D is an ethylene group substituted by an organic radical having from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as corrosion and gas hydrate inhibitors, and also the compounds of formula 1.

Abstract: The invention provides the use of compounds of the formula (1) where R1, R2 are each independently C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R3 is C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C30-alkylene group, D is an organic radical which optionally contains heteroatoms and has from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as gas hydrate inhibitors.

Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.

Abstract: The invention provides the use of compounds of the formula (1) where R1, R2 are each independently C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, R3 is C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, —CHR5—COO? or —O?, R4 is M, hydrogen or an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, B is an optionally substituted C1- to C30-alkylene group, D is an organic radical which optionally contains heteroatoms and has from 1 to 600 carbon atoms, X, Y are each independently O or NR6, R5, R6 are each independently hydrogen, C1- to C22-alkyl, C2- to C22-alkenyl, C6- to C30-aryl or C7- to C30-alkylaryl, and M is a cation as gas hydrate inhibitors.

Abstract: Initiators for atom transfer radical polymerizations are described. The initiators have an azlactone or ring-opened azlactone moiety to provide telechelic (co)polymers.

Abstract: A process for synthesizing L and D-5,5,5,5?,5?,5?-hexafluoroleucine and protected analogs is disclosed. These compounds have utility in the preparation of fluorous peptides and proteins, which display interesting and unusual properties including strong self-association and an affinity for lipid bilayers.

Abstract: A process for producing 4-bromo-2-oxyimino butyric acid, predominantly as the (Z)-isomer of formula (I), wherein R is hydrogen; a linear or branched C1-4 alkyl group; a linear or branched C1-4 alkyl group substituted by a carboxylic acid or an aryl group; a substituted or unsubstituted cyclic alkyl group of 3-6 carbon atoms or a substituted or unsubstituted aryl group. The product is produced by reacting bromine with a 2-(oxyimino)-3-oxo butyric acid derivative of formula (II) wherein R is as defined above and R1 is a tert-butyl group in presence of an organic solvent and in presence of a C1-4 alcohol and acetyl bromide at a temperature ranging from about ?15° C. to about +15° C. Bromine is used in a proportion of about 0.90 to about 1.35 moles per mole of compound (II), preferably 0.90 to 1.10 moles. The acetyl bromide is used in molar proportions of 0.9 to 2 moles per mole of compound (II), preferably 0.9 to 1.5 moles.

Abstract: An optically active N-protected azetidine-2-carboxylic acid (5) can be produced by preparing an optically active 4-amino-2-halobutyric acid (3) by halogenating an optically active 3-hydroxy-2-pyrrolidinone (1) with inversion of configuration to prepare an optically active 3-halo-2-pyrrolidinone (2) followed by hydrolysis or by halogenating an optically active 4-amino-2-hydroxybutyric acid ester (6) with inversion of configuration to prepare an optically active 4-amino-2-halobutyric acid ester (7) followed by hydrolysis or by halogenating the compound (6) with inversion of configuration to prepare the compound (7), cyclizing the same to prepare the compound (2) followed by hydrolysis, further cyclizing the compound (3) followed by treating the reaction product with an amino group-protecting agent.

Abstract: There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula wherein R1 and R2 are each independently of the other hydrogen, C1-C20alkyl; C3-C12cycloalkyl; unsubstituted or C1-C5alkyl-, C3-C12cycloalkyl-, C1-C5alkoxy-, C3-C12cycloalkoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C12cycloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl, phenyl-C1-C5alkyl, naphthyl and naphthyl-C1-C5alkyl; and R3 is C1-C20alkyl; C3-C12cycloalkyl. The compounds exhibit a pronounced activity against gram-positive and gram-negative bacteria, and also against yeasts and moulds.

Abstract: Perfluoroalkyl-substituted amines, acids, amino acids and thioether acid compounds containing a perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkene group as well as derivatives thereof, are described. They are useful as surfactants in a variety of applications where low surface tensions are required, including coating formulations for glass, wood, metal, cement, paper, textiles, as foam control agents in polyurethane foams and especially in aqueous fire-fighting formulations.

Abstract: A composition consisting of the reaction product of a halogenated carboxylic acid, an amine, and optionally a fatty acid. The composition has biocidal properties and enhances pigment dispersibility.

Abstract: A 2- or 4-nitrobenzenesulfonamide is allowed to react with an alkali metal alkoxide to remove a nitrobenzenesulfonyl group to thereby obtain an amine corresponding to the amide. Furthermore, a method for producing an amine derivative by allowing the resulting amine without isolation to react with an activated, substituted oxycarbonyl compound or an activated acyl compound is provided. According to this method, a corresponding free amine and its substituted derivative can be produced easily and industrially advantageously from the 2- or 4-nitrobenzenesulfonamide without using a thiol compound.

Abstract: An industrially advantageous method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids is provided. Methods are also provided of producing optically active N-protected-S-phenylcysteines having high optical purity and of intermediates thereof, respectively, in which the above production method is utilized.