Abstract: A process for preparing dipeptides with N-terminal non-proteinogenous amino acids of the formula ##STR1## in which R.sup.1 to R.sup.6 have the meaning stated in the description, from compounds of the formula ##STR2## is described.

Abstract: A method of inhibiting the abnormal postnatal axial growth of the eye of a maturing animal during conditions ordinarily leading to said abnormal growth, which comprises (1) determining the neurochemical present in the retina of said eye, e.g., dopamine, the concentration of which is reduced during said conditions, and (2) administering to said eye during postnatal maturation effective amounts of said neurochemical, its agonist or its antagonist.

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 present invention provides a novel betaine compound represented by the general formula: ##STR1## wherein R.sup.1 is a straight-chain or branched alkyl, alkenyl or hydroxyalkyl group having 8 to 22 carbon atoms; X is H or a hydroxy group; R.sup.2, R.sup.3 and R.sup.4 each represent an alkyl group having 1 to 4 carbon atoms; Y is --CH.sub.2 CH(OH)CH.sub.2 SO.sub.3, --(CH.sub.2).sub.n SO.sub.3 or --(CH.sub.2).sub.m CO.sub.2 ; n is 2 to 5; m is 1 to 5; and l is 0 to 5; a process for the preparation of the same; and a detergent composition containing the same. This detergent composition exhibits excellent foaming power and detergency and is lowly irritant, thus being suitable for a base of a body or hair shampoo.

Abstract: The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy, aryloxy, or an amino acid residue bonded at the amino nitrogen; --R" is hydrogen or an amino acid residue bonded at the carbonyl carbon; --X is halogen; and --Y is hydrogen or halogen.

Abstract: Acylamino carboxylic acid derivatives corresponding to the formula I ##STR1## in which the groups R.sup.1, R.sup.2, R.sup.3, Z.sup.1 and Z.sup.2 represent functional groups specified in the claims. The acylamino carboxylic acid derivatives have valuable pharmacological properties which, in particular, favorably influence nitrogen metabolism. The compounds are useful as active ingredients in pharmaceutical and/or dietetic compositions for treatment or prevention of nitrogen metabolism disturbances in large mammals caused, for example, by liver or kidney damage.

Abstract: The invention relates to new pure D- or L-N-hydroxy-alpha-amino acids and the derivatives thereof, including optically active N-hydroxy-phenylglycine amide, which has antibiotic and antitumor activity.

Abstract: Novel N-(dialkylaminoalkyl)-substituted derivatives or N-(dialkylaminoalkyl)-N-alkyl-substituted derivatives of oxamic acid are now synthetized and found to exhibit the cerebral protective effect against cerebral anoxia in brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain.

Abstract: A process for the production of R(+)-aminocarnitine and S(-)-aminocarnitine is disclosed by resolution of the mixture of the diastereoisomers of N-(alpha-methylbenzyl) aminocarnitine benzyl ester chloride, wherein the separated diastereoisomers are subsequently debenzylated to give R(+)-aminocarnitine chloride and S(-)-aminocarnitine chloride.

Abstract: New peptide derivatives .beta.-chloro-L-(Z)-dehydroglutamic acid are described which display antibacterial activity.

Abstract: The process described makes it possible to obtain optically pure 4-amino-3-hydroxycarboxylic acids by means of a series of stereoselective steps. The starting material is an alpha-amino acid in the L or D configuration, with which Meldrum's acid is reacted. The resulting pyrrolone derivative is reduced prior to opening of the pyrrolidine ring. The invention also relates to the new products obtained by the said process and to the pyrrolone derivatives obtained as intermediates.

Abstract: Serine-N,N-diacetic acid and derivatives thereof are prepared in various ways and used in particular as complexing agents, bleaching agent stabilizers and builders in detergents.

Abstract: In solid form, copper complex salts of the formula: ##STR1## wherein "n" is from 1 to 5, and "Z" is an anion and "y" is the number required to electrostatically balance the set.

Abstract: A process for the N-.omega.-trifluoroacetylation of a saturated aliphatic monocarboxylic .alpha.,.omega.-diamino acid. A saturated aliphatic monocarboxylic .alpha.,.omega.-diamino acid of the formula: ##STR1## wherein R represents a straight-chain or branched-chain C.sub.1 -C.sub.6 alkylene radical, is contacted with a C.sub.1 -C.sub.6 straight-chain or branched-chain alkyl trifluoroacetate.

Abstract: Dispersants containing basic amine groups are passivated toward fluorohydrocarbon compositions by reaction with a passivating amount of a dicarboxylic acid or anhydride.

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: A method is provided for synthesizing oligonucleotides and peptides directly onto a membrane. The method provides a means for generating membrane affinity supports. A modified membrane for the method of direct synthesis is also provided.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.

Abstract: This invention relates to ornithine derivatives substituted at the 5 position with an R group which can be a --CH.sub.2 F, --CHF.sub.2, --CHClF, --C.tbd.CH, --CH.dbd.CH.sub.2, or --CH.dbd.C.dbd.CH.sub.2 group and the pharmaceutically acceptable acid addition salts thereof which are specific inhibitors of OAT and can be used in the treatment of conditional deficiencies of ornithine.

Abstract: In solid form copper complex salts of the formula: ##STR1## wherein "n" is from 1 to 5, and "Z" is an anion and "y" is the number required to electrostatically balance the set.

Abstract: 2-(Fluoromethyl or chloromethyl)-2,5-diaminopentanoic acid, 2-(fluoromethyl or chloromethyl)-2,6-diaminohexanoic acid, and 2-fluoromethyl-2-amino-5-guanidinopentanoic acid, and certain derivatives thereof, are inhibitors of ornithine decarboxylase. Methods of preparing the compounds and derivatives are also described.

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: Amino acid salt having at least one unblocked amino group and comprising at least one cation which has a nitrogen cationic atom is reacted with 1-(tertiary-alkoxycarbonyl)imidazole in the liquid phase and in the presence of essentially inert organic solvent having a dielectric constant at 25.degree. C. of at least about 4, to produce N-(tertiary-alkoxycarbonyl)-blocked amino acid salt.

Abstract: There is disclosed an antibiotic complex designated as BU-2231 V which is produced by fermentation of a BU-2231-producing strain of Streptoalloteichus hindustanus, ATCC 31158. Complex BU-2231 V is recovered and purified from the fermentation broth by use of ion exchange chromatography techniques. Structural analysis shows that the complex is a mixture of components which are .gamma.-homopolymers of D-.alpha.,.gamma.-diaminobutyric acid having an average molecular weight of from about 5,100 to about 5,200. BU-2231 V has been found to be effective to inhibit growth of various Gram-positive and Gram-negative bacteria and of the herpes simplex virus.

Abstract: Formylating the amino nitrogen of an alkali metal salt of an amino carboxylic acid, by reacting the salt with an alkyl formate in an alkanol solvent. In one embodiment, the alkyl formate is added to the reaction as such; in another embodiment, the alkyl formate is formed in situ by reaction of carbon monoxide with the alkanol solvent in the presence of the alkali metal salt of the amino carboxylic acid. The process provides a new class of compounds, the alkali metal salts of N-formyl-aspartic acids.

Abstract: Compounds are provided of the following general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen or methyl and A is amino, C.sub.1 -C.sub.4 monoalkylamino, C.sub.2 -C.sub.8 dialkylamino, cyclopropylamino, 1-pyrrolidinyl, 1-piperidinyl or 4-morpholinyl. They are useful for providing sedative and antiepileptic activity.

Abstract: Procainamide and N-acetylprocainamide (NAPA) immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining the respective drugs. The immunogens comprise the drugs coupled at the .alpha.-position of the amide side chain to an immunogenic carrier material. The labeled conjugates and synthetic intermediates similarly are .alpha.-position derivatives of the drugs or precursors thereof. The antibodies and labeled conjugates are particularly useful in homogeneous nonradioisotopic immunoassays for measuring the respective drugs in biological fluids such as serum.

Abstract: Acylated aminocarnitines have utility as competitive inhibitors of carnitine acyl transferases and the unacylated compounds have utility as intermediates for making the acylated compounds.

Abstract: The present invention is directed to a composition and method relating to the preparation of aspartyl peptides having the general formula: ##STR1## where the radical-NHR represents an amino acid or peptide group. In the method, a .beta.-monoester of aspartic acid having the general formula: ##STR2## where R.sub.1 represents a hydrocarbon-containing radical, is reacted with a .beta.-dicarbonyl compound, preferably ethylacetoacetate to protect the aspartyl amino group and form an enamine. The enamine is then coupld to an amino acid or peptide, following which any protecting groups are removed to yield .alpha.-aspartyl peptides without any .beta.-isomer. In its composition aspects, the present invention is directed to novel enamines resulting from reaction of the .beta.-monoester of aspartic acid with a .beta.-dicarbonyl compound.

Abstract: Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharmaceutical compositions comprising such compounds; and a method of treatment comprising administering such compounds and compositions when an antihypertensive effect or radioprotective effect is indicated.

Abstract: 2-(Fluoromethyl or chloromethyl)-2,5-diaminopentanoic acid, 2-(fluoromethyl or chloromethyl)-2,6-diaminohexanoic acid, and 2-fluoromethyl-2-amino-5-guanidinopentanoic acid, and certain derivatives thereof, are inhibitors of ornithine decarboxylase. Methods of preparing the compounds and derivatives are also described.

Abstract: Novel compounds of the following formula have restorative pharmacological activities in immuno-deficient hosts, ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is hydrogen, carboxy or a protected carboxy group,R.sup.3 is hydrogen, carboxy or a protected carboxy group,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carbamoyl(lower)alkyl or protected carbamoyl(lower)alkyl,R.sup.5 is hydrogen or lower alkyl, andR.sup.6 is hydrogen, hydroxyphenyl(lower)alkyl, imidazolyl(lower)alkyl or indolyl(lower)alkyl.

Abstract: Derivatives having the general formula: ##STR1## in which the various radicals, A,B,X,R.sub.1, R.sub.2, R.sub.3 and n have indicated definitions. These compounds have in particular enkephalinase-inhibiting, antalgic, antidepressive, antidiarrhea and hypotensive activities.

Abstract: Hexapeptides with vasodilating and hypotensive activity are described corresponding to the formula: ##STR1## wherein:X is a hydrogen atom or an acyl radical R.sub.3 -CO- wherein R.sub.3 is a straight or branched (C.sub.1 -C.sub.7)alkyl group,R.sub.1 and R.sub.2, each independently, represent the side-chain residue of the amino acid glycine (--H), alanine (--CH.sub.3), valine ##STR2## leucine ##STR3## or isoleucine ##STR4## Arg is the abbreviated designation for arginine, Pro is the abbreviated designation for proline, Tyr is the abbreviated designation for tyrosine, and the pharmaceutically acceptable salts, lower alkyl esters and amides thereof, a process for their preparation and the pharmaceutical compositions containing them.

Abstract: Described are 3-halovinylglycines and their amino acid dipeptide and oligopeptide conjugates, a new class of efficient antibacterial agents, pharmaceutical compositions containing them as active ingredients, and methods of synthesis. The compounds are thought to interfere in bacterial cell wall synthesis.

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

Abstract: Compounds having relatively long shelf lives in acidic aqueous media and which are useful as sweeteners have the formula ##STR1## or are pharmaceutically acceptable salts thereof, wherein X is --OR or --NHR, or --NH.sub.2, with R being alkyl having 3-10 carbon atoms.

Abstract: An improved process for preparing .alpha.,.omega.-diamino acids, such as D,L-homolysine, 2,8-diaminooctanoic acid, ornithine, lysine, or the like, comprising reaction of phthalic anhydride and an amino alcohol in a hydrocarbon solvent; treatment of the resulting phthalimide--N--(CH.sub.2).sub.n --OH derivative, without isolation thereof, with phosphorus tribromide or phosphorous pentachloride; alkylation of diethyl acetamidomalonate with the phthalimide--N--(CH.sub.2).sub.n --chloride or --bromide of the previous step, in the presence of, particularly, sodium hydride/dimethylformamide; standard acid hydrolysis and decarboxylation; selective protection via copper(II) chelation, N-specific acylation with benzyl chloroformate, and decomposition of the amino acid-copper(II) complex with alkaline thioacetamide; standard t-butoxycarbonyl acylation; and deprotection to obtain the desired .alpha.,.omega.-diamino acids.

Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.

Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.

Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.

Abstract: Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharmaceutical compositions comprising such compounds; and a method of treatment comprising administering such compounds and compositions when an antihypertensive effect or radioprotective effect is indicated.

Abstract: This invention relates to new novel sweeteners of the formula: ##STR1## wherein A is hydrogen, alkyl containing 1-3 carbon atoms or alkoxymethyl wherein the alkoxy contains 1-3 carbon atoms;A' is hydrogen or alkyl containing 1-3 carbon atoms;A and A' taken together with the carbon atom to which they are attached form cycloalkyl containing 3-4 carbon atoms;Y is --(CHR.sub.2).sub.n --R.sub.1, --CHR.sub.3 R.sub.4 or R.sub.5 ;R.sub.1 is cycloalkyl, cycloalkenyl, bicycloalkyl or bicycloalkenyl containing up to 7 ring carbon atoms and up to a total of 12 carbon atoms;R.sub.5 is alkyl containing up to 11 carbon atoms;R.sub.2 is H or alkyl containing 1-4 carbon atoms;R.sub.3 and R.sub.4 are each cycloalkyl containing 3-4 ring carbon atoms;n=0 or 1; andm=0 or 1;and food-acceptable salts thereof.

Abstract: Compounds which are the reaction products of a C.sub.12-14 -alkyl N-substituted 1,3-diaminopropane and glutamic acid or its 5-methyl ester, optionally alkoxylated, and optionally their salts, are useful as antimicrobial agents.

Abstract: A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.

Abstract: Fatty acid derivatives represented by the general formula ##STR1## and salts thereof. The compounds of this invention have excellent fibrinolytic action and a highly improved solubility.

Abstract: Amino acids can be easily prepared by reducing unsaturated hydantoins to the corresponding saturated hydantoins by hydrogenating the unsaturated hydantoin using either Raney Nickel catalyst in the presence of more than a stoichiometric amount of caustic or by using zinc and hydrochloric acid followed by hydrolyzing the resultant composition with at least 3 molar equivalents of an alkali metal hydroxide to produce a racemate of an alpha amino acid. The amino acid in suitable derivative form can then be resolved particularly using a two-phase solvent system. The residual isomer of the amino acid remaining after the resolution process can then be racemized using either pyridoxal-5-phosphate or an aliphatic acid in combination with an aldehyde or a ketone. By these procedures, it is possible to obtain high yields of amino acids.

Abstract: Amino-polyacetic acids such as ethylenediaminetetraacetic acid, diethylene triaminepentaacetic acid and nitrilotriacetic acid are reacted with alkanols and then with hydrazine to form the hydrazides which may be converted to carboxyhydrazides, i.e. carbazic acids. The products perform well as chelants and sequestering agents.

Abstract: An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.

Abstract: Amphoteric compounds of the formula ##STR1## and their mixtures with compounds of the formulaR.sup.2 --NH--(CH.sub.2).sub.d --NH--(CH.sub.2).sub.e --COOH . y HA (II)and, where appropriate, of the formula ##STR2## in which R.sup.1 =R.sup.2 =R.sup.3 and is an alkyl or alkenyl radical having 8 to 22 carbon atoms; A is the anion of a mineral or carboxylic acid; a and b are 2 or 3; c is 1 or 2; x is 0, 1, 2 or 3; d is 3; e is 1 or 2; y is 0, 1 or 2; f and g are 2 or 3; h and i are 1 or 2; and z is 0, 1, 2 or 3, and processes for the preparation of these compounds and mixtures are described. They have microbicidal properties and are suitable as disinfectant cleaning agents.