Abstract: It has been found that certain combinations of substituted imidazoline-based amphoterics and quaternary ammonium compounds show markedly reduced irritation profile in addition to providing excellent cleaning detergency. Moreover, it has further been found that certain substituted imidazoline amphoteric surfactants in combination with didecyl dimethyl ammonium chloride (DIDAC) show unexpected synergistic irritation reduction compared to that observed when the quaternary is an ADBAC type. This allows the formulation of disinfectants and sanitizers with the favored antimicrobial agent while at the same time affording the optimum reduction in irritation potential.

Abstract: Derivatized drugs are prepared with a linker consisting of a malonate, wherein the drug is linked through a methylene to the 2-position carbon of the malonate.

Abstract: The novel compounds of the formula I ##STR1## in which n is an integer from the range from 4 to 8 and m is an integer from the range from 1 to 4,A is the aliphatic, aromatic, araliphatic or heterocyclic radical of a monobasic to tetrabasic carboxylic acid, andR.sup.1 and R.sup.1', independently of one another, are C.sub.1 -C.sub.24 alkyl or C.sub.5 -C.sub.8 cycloalkyl, are suitable for stabilizing organic material against thermal, oxidative or actinic degradation.

Abstract: Mammalian hair growth is reduced by applying to the skin an inhibitor of a cysteine synthetic pathway enzyme.

Abstract: A process for the preparation of a .alpha.,.omega.-dicarboxylic acid diester of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, C.sub.2 -C.sub.20 alkoxycarbonyl, nitro, C.sub.2 -C.sub.20 alkoxy and/or cyano andn is an integer from 1 to 12,wherein cycloalkanones of the general formula II ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the aforementioned meanings, are caused to react with dimethylcarbonate in the presence of a nitrogenous base of the general formula III ##STR3## in which R.sup.6, R.sup.7, R.sup.8 denote hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.8 cycloalkyl or C.sub.7 -C.sub.20 aralkyl or R.sup.6 and R.sup.7 together form a C.sub.2 -C.sub.7 alkylene chain optionally mono- to penta-substituted by R.sup.1,at temperatures ranging from 50.degree. to 300.degree. C.

Abstract: A homopolymer or a copolymer comprises a polymerizable compound represented by formula (I):A--X--COCOOR.sub.1 (I)wherein R.sub.1 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or an aryl group; X represents an oxygen atom, a sulfur atom, --COO-- or --NR.sub.5 -- wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group; A represents a C.sub.3 -C.sub.18 alkenyl, alkynyl, alkenylaryl or alkenylaralkyl group, or a group represented by: ##STR1## wherein R.sub.2 and R.sub.3, which may be the same or different, independently represent a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group; Y represents an oxygen atom or --NR.sub.4 -- wherein R.sub.4 represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group; n is an integer of 1 to 5; m is an integer of 1 to 10; and 1 is 0 or an integer of 1 to 20;with the proviso that if Y is present, X is not --NR.sub.5 --. Additionally, disclosed are processes of preparing the homopolymer or copolymer as well as the polymerizable compound.

Abstract: A method for preparing an amino acid ester with sulfuric acid as the catalyst in high yield, in which a mixture of amino acid, sulfuric acid and an alcohol is heated while adding the alcohol as a liquid or gas to the reaction mixture and alcohol from the reaction mixture is distilled off.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphono- and phosphinocarboxylic acids containing hydroxyl and/or mercapto groups, their use as waterproofing and/or oil-repellency agents, and a method for their preparation.

Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids containing acrylate and/or methacrylate groups, their use as waterproofing or oil-repellency agents, and a method for their preparation.

Abstract: Aminomethylene compounds of the formula ##STR1## may advantageously be prepared by reacting C--H-acidic compounds of the formula ##STR2## with formamide acetals of the formula ##STR3## in which the radicals R.sup.1 to R.sup.6 have the meaning given in the description,if the process is carried out in the presence of a secondary amine of the formula ##STR4## in which R.sup.7 and R.sup.8 have the meaning given in the description.

Abstract: A lubricating oil soluble compound suitable for use as a dispersant additive is obtainable by reacting at elevated temperature a polyacrylate with a dispersant having at least one reactive nitrogen--containing moiety.Intermediates of the general formula IV ##STR1## where Y.sup.1 is a group derived from the reaction of the polyacrylate with the reactive nitrogen-containing moieties (i.e. primary or secondary amine) are novel.The process for preparing the lubricating oil soluble compounds can be a one step or multistep process.Lubricating oil compositions comprise a major proportion of lubricating oil and a minor proportion of the lubricating oil soluble compounds.

Abstract: N-substituted .alpha.-amino acids and dipeptides are valuable intermediate products for the production of inhibitors of the angiotensin converting enzyme (ACE); representatives are e.g. enalapril and ramipril. These compounds are prepared by means of hydrogenolytic conversion of a primary amine with a ketone with the addition of an organic or inorganic base; among the inorganic bases, basic aluminum oxide is preferred. The use of chiral organic bases favors the production of a diastereomer.

Abstract: Disclosed is a method for extracting an amino acid ester from a hydrous solution which comprises adding thereto a water-insoluble organic solvent and then an amount of a base effective to liberate only a portion of the amino acid ester in free base form, and transferring the thus liberated amino acid ester in the free base form into the organic layer, and repeating the neutralization-extraction steps until all of the amino acid ester has been extracted.

Abstract: .alpha.-Aminocarboxylic acid derivatives of the formula: ##STR1## where n, X, Y and Z have the meanings stated in the description, and their preparation are described. The compounds are used in a method for improving delivery and reducing toxicity of biologically active substances by encapsulation of the biologically active substance with the above compounds.

Abstract: Amino-functional compounds are economically prepared by reacting maleic anhydride with alcohols to form a maleate or fumarate "half-ester" which is combined with certain amines, most preferably aspartate or glutamate, under conditions selected to avoid hydrolysis. At low molecular weights, the compounds herein are useful detergency builders; at progressively higher molecular weights within a specific range, combined builder/dispersant and typical dispersant properties emerge. Processes for preparing the compounds and useful detergent compositions containing them are described.

Abstract: New synthesis and analysis procedures for novel crosslinked polyamines and ampholytes. Polyamines are crosslinked with tartaric acid ester, malonic acid ester, or polycarboxylic acid esters of the citric acid cycle. The resulting crosslinked polyamine may further react with other compounds such as an .alpha.,.beta.-unsaturated or .alpha.-halo unsaturated carboxylic acids to prepare new ampholyte mixtures. The resulting novel ampholytes exhibit greater heterogeneity and complexity than presently prepared ampholytes, and can be used in analytical and preparative isoelectric focusing processes.Novel ampholyte analysis process entails analyzing chemical compounds, usually ampholytes, used in isoelectric focusing processes. The ampholyte is isoelectrically focused on an immobilized pH gradient, and then immersed in a picric acid solution to cause precipitation and visualization of amphoteric species.

Abstract: Amine derivatives which are compounds of the formula (I): ##STR1## in which R is a C.sub.6-20 hydrocarbon; Y is --CO--NH-- and n is an integer of 1 to 6; or ##STR2## in which X is an alkylene group of 2 to 6 carbon atoms and n is an integer of 0 to 6;each R.sub.1 is independently H, --(CH.sub.2).sub.1-4 COOH, a C.sub.6-20 hydrocarbon or C.sub.6-20 hydrocarbon-carbonyl;R.sub.2 is H, (CH.sub.2).sub.1-4 COOH or C.sub.6-20 hydrocarboncarbonyl;the compound containing at least one (CH.sub.2).sub.1-4 COOH group; or a salt thereof are useful in inhibiting corrosion of metals in oil- and gas-field applications, and also show low toxicity to marine organisms.

Abstract: Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I ##STR1## in which X is --S--,W is CH.dbd.CH;o is 1 to 4;n is 2 to 6;m is 0 to 2;T and Z, same or different, represent oxygen or a direct bond;R.sup.2 and R.sup.3, represent hydrogen, or fluorine;A represents carboxyl, CO.sub.2 R.sub.4.sup.4, wherein R.sup.4 is lower alkylR is ##STR2## wherein Y represents carboxyl, CO.sub.2 R.sup.4, wherein R.sup.4 is lower alkylR.sup.7 and R.sup.8, same or different, represent H or lower alkyl;R.sup.9 represents --OH, --O-alkyl, NH.sub.2 or a NHCH.sub.2 CO.sub.2 H group; andR.sup.10 R3 is H.

Abstract: Amino acids and amino acid derivatives bearing isotopic hydrogen labels at both the .alpha.- and .beta.-positions are produced when N-substituted azomethine derivatives of carboxylic acids and carboxylic acid derivatives are hydrogenated over metal catalysts in isotopically-enriched protic solvents with molecular hydrogen.

Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H-acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of simple inorganic bases, where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.8 and X.sup..crclbar. have the meanings given in the description.

Abstract: A process for preparing precursors for amido containing organic peracids is disclosed wherein a diester of a dibasic acid is reacted with an amine to provide a mono amido carboxylic acid ester. The reaction is conducted in a reaction column to provide a highly selective reaction which limits the amount of diamide produced. The selective reaction is conducted with a moderate excess of diester and may be conveniently operated on a continuous basis.

Abstract: Ester derivatives useful as fuels and lubricating oil additives are prepared by the Michael addition of an alkyl acrylate to an amine to produce an intermediate ester, followed by an ester interchange with the intermediate ester to produce the final ester derivatives, some of which are novel compounds.

Abstract: A method of preparing a compound of the formula ##STR1## in which R.sub.1 is CH.sub.3 or C.sub.2 H.sub.5,n is 0 to 4,m is 1 to 3,R.sub.2 is H, --COOR.sub.1, alkyl or aryl, andR.sub.3 and R.sub.4 each independently is H, alkyl or aryl,which comprises reacting an alkyl ester of a dicarboxylic acid of the formula R.sub.1 OOC--CR.sub.3 R.sub.4 --COOR.sub.1 with a nitrile of the formula N.tbd.C--(CH.sub.2).sub.m R.sub.2 and with hydrogen in the presence of a hydrogenation catalyst.

Abstract: An amphipathic compound, which includes a succinic acid moiety and an amino acid moiety and is designed so as to form a stable unilayer liposome, and a negatively charged liposome comprising said amphipathic compound as a membrane-component are disclosed. The amphipathic compound of the present invention gives liposomes which minimize the leakage of a drug encapsulated therein and scarcely undergo association, aggregation or precipitation.

Abstract: A method for chemically modifying an anionic metal complex, by obtaining from an anionic metal complex insoluble in a non-aqueous solvent and a clathrate compound a clathrate complex thereof with a counter cation of said metal complex, which is soluble in a non-aqueous solvent, and then reacting functional groups of the metal complex, which are not concerned with the coordination of said metal complex, with an organic reagent in the presence of a reaction assistant.The central metal from the chemically modified metal complex may then be removed.

Abstract: The invention relates to a curing component (A) containing active CH groups, which contains at least two groups of the formula (I) ##STR1## or structural units of the formula (I') or (I") ##STR2## in which: A denotes ##STR3## X and Y are identical or different and denote ##STR4## CO.sub.2 R.sup.1, CN, NO.sub.2, CONH.sub.2, CONR.sup.1 H or CONR.sup.1 R.sup.1, where the R.sup.1 radicals may be identical or different and represent a hydrocarbon radical, preferably an alkyl radical having 1 to 12 carbon atoms, which may also be interrupted by oxygen or an N-alkyl radical, with the proviso that only one of the two radicals X and Y may represent the NO.sub.2 group;A' denotes ##STR5## X' and Y' are identical or different and denote ##STR6## Curable mixtures of (A) and a Michael acceptor (B) and, if appropriate diluents and customary additivies cure rapidly even at low temperatures and are suitable, in particular for surface-coating preparations.

Abstract: Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are z-2-acylamino-3-monosubstituted propenoates.

Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.

Abstract: Unsaturated aminodicarboxylic acid derivatives of formula I ##STR1## wherein A is a divalent aliphatic hydrocarbon radical containing 2 carbon atoms and R.sub.1 and R.sub.2 are each independently of the other free or esterified carboxyl groups, and salts thereof, have a pronounced and selective antagonistic action against N-methyl-D-aspartic acid (NMDA)-sensitive excitatory amino acid receptors. These compounds are prepared, for example, by converting, in a formula of formula II ##STR2## wherein Z.sub.1 and Z.sub.2 are hydroxy or protected hydroxy and Z.sub.3 is protected amino, Z.sub.3 into amino and, if present, converting protected hydroxyl groups Z.sub.1 and/or Z.sub.2 into hydroxy and, if desired, converting a resultant compound into another compound of formula I, resolving a resultant mixture of isomers into the individual components and separating the desired preferred isomer and/or converting a resultant free compound into a salt or a resultant salt into the corresponding free compound.

Abstract: A cyclical process for producing and isolating a mineral acid salt of an amino acid methyl ester in high purity and yield from the reaction solution produced by esterifying an amino acid with methanol in methanol in the presence of a mineral acid, by cooling the resulting reaction solution to precipitate crystals of the mineral acid salt; filtering the crystals;drying the isolated wet crystals or washing with another organic solvent; and recycling the filtrate for reuse in the esterification reaction.

Abstract: A process for preparing a carboxyalkyl-substituted hydroxylamine represented by formula (I) ##STR1## where L represents an alkylene group; A represents a hydrogen atom, a sulfo group, a carboxy group, a phosphono group, a trialkylammonio group, a hydroxy group, an amino group, an acyl group, a carbamoyl group, a sulfamoyl group, an alkoxycarbonyl group, or a cyano group; and R.sub.1, R.sub.2, and R.sub.3, which may be the same or different, each represent a hydrogen atom, an alkyl group, or an aryl group; which comprises: reacting an .alpha.,.beta.-unsaturated carboxylic acid represented by formula (II) as an alkylating agent ##STR2## where R'.sub.1, R'.sub.2, and R'.sub.3, which may be the same or different, each represent the same group as defined for R.sub.1, R.sub.2, and R.sub.

Abstract: The invention relates to a process for the preparation of pyridine-2,3-dicarboxylic acid esters using novel maleic acid esters as starting materials. In the process, in a first process step, 2,3-dihalomaleic acid esters are reacted with ammonia, or ammonium salts, with the exclusion of water at a temperature of at least 50.degree.0 C. to form novel 2-amino-3-halomaleic acid esters, and these are subsequently reacted further in a second process step with .alpha.,.beta.-unsaturated aldehydes, or ketones, in the presence of an acidic catalyst and acid-binding agents at a temperature of at least 50.degree. C. with heat being supplied until the pyridine-2,3-dicarboxylic acid esters have been formed. Pyridine-2,3-dicarboxylic acid esters of this type can be used for example, as intermediates for synthesis of herbicides based on imidazoline. The present invention also relates to novel 2-amino-3-halomaleic acid esters, which are useful for producing the final product pyyridine-2,3-dicarboxylic acid esters.

Abstract: Aminomethylene compounds of the formula ##STR1## can be prepared by reaction of C-H acid compounds of the formula ##STR2## with salts of the formula ##STR3## in the presence of alkoxides of the formulaM.sup.1 OR.sup.10 (IV)where the radicals R.sup.1 to R.sup.4, R.sup.7, R.sup.10, X.sup.- and M.sup.1 have the meaning mentioned in the description.

Abstract: The present invention relates to a method of treating an inflammatory condition, and to compounds and composition suitable for use in such a method, which compounds have the Formula: ##STR1## wherein: X is methylene, ethylene, ethyleneoxy, or oxygen;Q is ##STR2## where C' is a residue of a lipophilic amino acid, and Y is --CO.sub.2 H, --CH.sub.2 OH, --CONR.sub.1 R.sub.2, or --CO.sub.2 R.sub.1 where R.sub.1 and R.sub.2 hydrogen, alkyl, or aryl;R.sub.3 and R.sub.4 are, independently, hydrogen, alkyl or aryl; andA and B are, independently, hydrogen, fused phenyl, alkyl, aryl, alkaryl, aralkyl, alkoxy, alkoxyalkyl, halogen, or nitro;or pharmaceutically acceptable salts thereof.

Abstract: A reaction system is provided for use in forming polyureas by the reaction injection molding process which employs an enamino-functional polyether resin as an isocyanate-reactive component.

Abstract: This invention relates to certain conjugates of folates and antifolates with difluoroglutamic acid which are useful in the treatment of patients suffering from certain neoplastic diseases including leukemia, melanomas, carcinomas, sarcomas and mixed neoplasias.

Abstract: The invention provides a class of compounds having two or more nonpolar components connected by a polar group and having polar groups on the termini of the compound.The invention also concerns a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises contacting the cells under suitable condition with an amount of the compound effect to selectively induce terminal differentiation.Moreover, the invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells which comprises administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells, thereby inhibiting their proliferation and suppressing oncogenicity.

Abstract: Glycerol aminocarboxylates of the formula ##STR1## where n is from 0 to 10 andR is ##STR2## where L is iminodiacetate, aspartate, glutamate, sarcosinate, glycinate, serinate, hydroxyaspartate, ethanolaminoacetate, diethanolamino, alanate or taurinate andX is hydrogen, an alkali metal, ammonium or substituted ammonium,are prepared by esterifying glycerol or polyglycerols which contain up to 10 glycerol units with maleic anhydride or itaconic anhydride and addition of compound L-H where L is as defined above to the double bonds of the esters, and are used as complexing agents.

Abstract: The present invention relates to novel methods for the preparation of quinoline-2,3-dicarboxylic acid, useful for the preparation of the highly effective 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.

Abstract: Novel N-alkenoyl enamide of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or halogen, andR.sub.3 and R.sub.4 are each independently of the other C.sub.1 -C.sub.4 alkanolyl, C.sub.1 -C.sub.18 alkoxycarbonyl, benzoyl, phenyl, cyano or carbamoyl, and R.sub.4 can also be hydrogen,are used for photocrosslinkable compositions suitable for use in photographic solutions, as UV absorbers and as textile finishing agents.

Abstract: Polymers, such as polyisobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.

Abstract: Polymers, such as polysiobutylene or ethylene-propylene copolymers, are functionalized by reaction with an activated imine to yield novel polymers.

Abstract: New aspartic acid derivatives include N-.alpha.-t-butoxycarbonyl-aspartic acid-.beta.-2-adamantyl ester-.alpha.-benzyl ester, N-.alpha.-t-butoxycarbonyl-aspartic acid-.beta.-2-adamantyl ester and benzyloxycarbonyl-aspartic acid-.beta.-2-adamantyl ester-.alpha.-benzyl ester.

Abstract: The invention relates to compounds of antitumor activity of the formula: ##STR1## ps in which R.sup.1 is hydrogen, lower allkyl, halo(lower)alkyl or aryl,R.sup.2 is hydrogen, hydroxy or protected hydroxy,R.sup.3 is hydrogen,R.sup.4 is aminocarboxy(lower)alkyl, protected amino(lower)alkyl or protected aminocarboxy(lower)alkyl, andR.sup.5 is hydrogen or lower alkyl, or its pharmaceutical acceptable salt.

Abstract: 2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1,7-dicarboxylates of the formula, ##STR1## in which each R is independently H or lower alkyl, are prepared from from di(lower alkyl) 1,3-acetone-dicarboxylates.

Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and H.sub.2 O or an organic hydroxyl compound to produce an N-acyl-.alpha.-amino acid or ester, respectively, the improvement comprising using as the .alpha.-enamide reactant, an .alpha.-enamide which has a chiral center that is essentially all L or D, thereby producing a reaction mixture containing diastereomeric N-acyl-.alpha.-amino acids or esters having two chiral centers, said mixture having essentially no enantiomeric pairs.

Abstract: Stereoselective process for the industrial synthesis of compounds of formula (I): ##STR1## where R.sub.1 is linear or branched lower alkyl with 1 to 6 carbon atoms,R.sub.2 is a linear or branched lower alkyl with 1 to 4 carbon atoms,employing inexpensive starting materials and obtaining optimum yields.Application to the synthesis of carboxyalkyl dipeptides.

Abstract: A process is described for the preparation of aspartic acid 4-(phenylmethyl) ester from aspartic acid and benzyl alcohol, characterized by utilizing a reaction mixture which contains, per mole of aspartic acid, 10-40 moles of benzyl alcohol and 1-5 moles of acetyl chloride, by conducting the reaction at a temperature of -10.degree. C. to 50.degree. C., and by separating the product of the process, after reaction has taken place, by neutralization with organic bases.

Abstract: Amino group containing curing component (A) for compounds (B) which contain epoxy or 1,3-dioxolan-2-one groups, comprising a reaction product of (a.sub.1) active CH alkyl esters of isocyanate adducts thereof with (a.sub.2) polyamines.Mixtures of (A) and (B) with or without diluents and additives give rapid curing even at low temperatures and high atmospheric humidity and are suitable in particular for paint formulations.

Abstract: A method is provided for quantitatively monitoring the deprotection and coupling reactions employed in the solid phase synthesis of peptides. The method entails synthesizing a peptide on a support matrix that has a first marker associated therewith. The amino acids employed in the peptide synthesis procedure have a second marker attached thereto, which can be the blocking group used for the amino acid. After the coupling or deprotection step a portion of the support matrix is processed to release first and second identifers from the first and second markers, respectively. The completeness of the coupling or deprotection step can be determined by comparing the relative amounts of the detected first and second identifiers. Novel compositions of matter are used in or produced during this method, including support matrixes having pyrolyzable markers attached thereto.