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: A base precursor represented by the following general formula (A) or (B): ##STR1## wherein A.sub.1, A.sub.2, A.sub.5, A.sub.6, A.sub.7, and A.sub.8 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, a substituted aryl group, an acyl group, or a heterocyclic group, and A.sub.1 and A.sub.2 can combine to form a ring and two of A.sub.5, A.sub.6, A.sub.7, and A.sub.8 can combine to form a ring, A.sub.3 and A.sub.4 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, or an aralkyl group, and A.sub.3 and A.sub.4 can combine to form a ring or A.sub.3 and A.sub.4 can be a double bond forming an imino group from ##STR2## and X represents a nucleophilic group.

Abstract: A simple method for making EDTA, ED3A or DTPA analogs from amide derivatives of alpha amino acids is disclosed. These EDTA, ED3A or DTPA analogs are useful chelating agents, and preferably are useful as bifunctional chelating agents which may be attached to biological molecules and which form physiologically stable chelates with a variety of metal ions.

Abstract: Novel octopine derivatives are disclosed which are useful for the selective growth of the agriculturally useful A. tumefaciens bacterium along with a synthetic method for their preparation. Also disclosed is a method of separating octopine derivatives from their diastereoisomers along with a method of selectively growing strains of the bacterium A. tumefaciens.

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.

Abstract: An aminocarboxylic acid derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents --NH-- or --S--, provided that when Y represents --NH--, at least one of R.sub.1 and R.sub.2 represents an alkyl group which may have a substituent. These compounds have excellent inhibitory activity on dipeptidase in animals, and are useful for administration in combination with carbapenem antibiotics.

Abstract: .alpha.-(S)-amino acid..alpha.-phenylethanesulfonate compounds and methods of optical resolution of .alpha.-amino acids and .alpha.-phenylethanesulfonic acids are described.

Abstract: Hydrolytically stable hydroxyl-terminated liquid polymers that are useful in the preparation of polyurethanes prepared by reacting at least one aminoalcohol with a carboxyl-terminated liquid polymer having a carbon-carbon backbone. The hydroxyl-terminated polymers have the formula ##STR1## wherein B is a carbon-carbon backbone, X is HO-- or HO--Y-- a univalent radical obtained by removing a hydrogen atom from an amine group of aminoalcohol containing one primary or secondary hydroxyl group and one primary or secondary amine group per molecule, and the polymers contain an average of greater than 1.5 terminal hydroxyl groups per molecule.

Abstract: Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.

Abstract: Species-linked diamine triacetic acids of the formula ##STR1## wherein T is an organic species containing at least one amine, hydroxyl, or thio functional group, L is the residue of at least one of those functional groups and R is a two or more atom long covalent bridge, are disclosed. Methods for their preparation, for the preparation of metal chelates from them and for the use of the chelates are also disclosed. In a preferred embodiment, the metal ions employed in the formation of the chelates are rare earth metal ions capable of forming fluorescent chelates which can in turn be employed in fluoroassay techniques.

Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.

Abstract: A low irritating detergent composition comprises an amphoteric surface active agent of the amideamine type having the formula (1): ##STR1## wherein R.sub.1 is an alkyl or alkenyl group having 6 to 20 carbon atoms, R.sub.2 is H, or C.sub.2 H.sub.4 OH, R.sub.3 is H, C.sub.2 H.sub.4 OH or C.sub.2 H.sub.4 CO.sub.2 M, R.sub.4 is H, C.sub.2 H.sub.4 OH or C.sub.2 H.sub.4 CO.sub.2 M, and M is H, an alkali metal, ammonium or organic ammonium,and mixing the amphteric surfactant of the formula (1) with one or more of another surfactants.

Abstract: Amphoteric dissociating complexes which have a cationic group having the structure ##STR1## wherein: R.sub.1 is an aliphatic alkyl group having 6 to 22 carbons,R.sub.2 is a member of the group consisting of --R.sub.4 --(CH.sub.2 CH.sub.2)--COOH, --R.sub.4 --(CH.dbd.CH)COOH and --OPO.sub.3 H.sub.2, wherein R.sub.4 is --NH--, --NH--CO--, or --O--CO--, andR.sub.3 is hydrogen, --CH.sub.2 --COOH or --CH.sub.2 --CH.sub.2 --COOH; and an anionic group which is either a carboxylate having the formula.sup.- OOC--CH.sub.2 --(O--CH.sub.2 --CH.sub.2).sub.x --OC.sub.n H.sub.2n+1or a phosphate having the formula.sup.= O.sub.3 PO--CH.sub.2 --CH.sub.2 --(OCH.sub.2 --CH.sub.2).sub.x --OC.sub.n H.sub.2n+1wherein:n is 8 to 22 and x is 1 to 10; and z is 1 when the anionic radical is a carboxylate and z is 2 when the anionic radical is a phosphate are disclosed.The compositions are effective carriers for active pharmaceutical or cosmetic ingredients.

Abstract: Species-linked diamine triacetic acids of the formula ##STR1## wherein T is an organic species containing at least one amine, hydroxyl, or thiol functional group, L is the residue of at least one of those functional groups and R is a two or more atom long covalent bridge, are disclosed. Methods for their preparation, for the preparation of metal chelates from them and for the use of the chelates are also disclosed. In a preferred embodiment, the metal ions employed in the formation of the chelates are rare earth metal ions capable of forming fluorescent chelates which can in turn be employed in fluoroassay techniques.

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

Abstract: The use of amine boranes to inhibit the inflammation process is disclosed. These boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz, 10.sup.-6 M.Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.

Abstract: The reaction of an imidazoline base of the formula: ##STR1## wherein R represents an aliphatic group comprising from 6 to 22 carbon atoms and R.sub.1 represents a substituted or unsubstituted alkyl or alkenyl group comprising 1 to 4 carbon atoms, with a carbo-alkylating agent is carried out in two stages. Initially the pH is maintained in the range 7 to 11 and subsequently it is maintained in the range 9 to 12.5. These conditions encourage at least part of the imidazoline to undergo alkylation followed by hydrolysis and further alkylation. The di alkylated amidoamines thus produced are believed to be novel. The reaction products are surfactants which exhibit very low skin irritancy and have a desirably low viscosity. They find particular application in shampoo formulations.

Abstract: An improved process for the production of polymers of acrylic acid or methacrylic acid by polymerizing acrylic acid or methacrylic acid in isopropanol or in a water-isopropanol mixture containing at least 40% by weight of isopropanol in the presence of polymerization initiators at a temperature of from 120.degree. to 200.degree. C. under pressure. The polymers obtained are used as dispersing agents for inorganic pigments.

Abstract: Process for the homogeneous catalytic hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids which yields, after hydrogenation, an optically active mixture. The process comprises the hydrogenation of .beta.-substituted-.alpha.-acylamidoacrylic acids in the presence of an optically active coordinated metal complex hydrogenation catalyst, in which the metal is selected from the group consisting of rhodium, iridium, ruthenium, osmium, palladium and platinum.This process is a generalized process for any asymmetric hydrogenation of .beta.-substituted-.alpha.-acylamido-acrylic acids in which one .alpha.-amino acid enantiomorph is the desired end-product. It is especially useful for the preparation of .alpha.-amino acids found in nature which possess optical activity and which have a hydrogen attached to the asymmetric center.This invention also relates to new optically active coordinated metal complex hydrogenation catalysts.

Abstract: New carboxyalkylacylamino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.

Abstract: A carboxylic acid is prepared by contacting an aqueous solution of the alkali metal or ammonium carboxylate with a liquid cation exchange agent dissolved in an organic solvent in which the carboxylic acid is substantially water immiscible. As an example, an aqueous solution of trisodium N-(2-hydroxyethyl)ethylenediaminetriacetate is contacted with di(2-ethylhexyl)phosphoric acid in kerosene to thereby form N-(2-hydroxyethyl)ethylenediaminetriacetic acid in the aqueous solution.

Abstract: Novel vinyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; Z is R.sub.1 OCCH.dbd.CH-- or R.sub.1 OC(CH.sub.2).sub.n -- wherein n is an integer of from 1 to 3; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is R.sub.1 OC(CH.sub.2).sub.