Abstract: A process for the production of of general formula I diethylenetriaminepentacarboxylic acid monoamide derivatives ##STR1## in which E.sup.1, E.sup.2 and Z have varying meanings.

Abstract: The present invention provides an industrial method of producing N-formyl-L-aspartic anhydride from N-formyl-L-aspartic acid, formic acid and acetic anhydride with less residual formic acid than conventional methods.

Abstract: This invention relates to a method for obtaining [S,S] ethylenediamine-N,N'-disuccinic acid precipitate from an aqueous solution of the salts of such acid and L-aspartic acid.

Abstract: A compound of the following formula ##STR1## wherein m is an integer of 1 to 3, R.sub.1 and R.sub.2 are the same or different and each is hydrogen atom or lower alkyl, and R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are the same or different and each is hydroxy or a group of the formula ##STR2## (wherein n is 0 or 1, X is --NH-- or --O--, Y is alkylene, A is hydrogen atom, lower alkyl, lower alkoxy, halogen atom or trifluoromethyl, and B is alkyl or alkenyl), with the proviso that two or three of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydroxyl groups and that when two of them are hydroxyl groups, the cases where R.sub.3 and R.sub.5 are hydroxy, and R.sub.4 and R.sub.6 are hydroxy are excluded; a complex compound comprising said compound and a metallic atom; and a diagnostic agent containing said complex compound. The above compound is useful as a chelating agent and the complex compound comprising said compound and a metallic atom exhibits superior characteristics as a contrast medium for image diagnosis.

Abstract: Polycocondensates based on aspartic acid which are obtainable by condensing aspartic acid in the presence of polymers containing carboxyl groups, which contain at least 10 mol % of a monoethylenically unsaturated carboxylic acid in copolymerized form and have a molecular weight of at least 300, in the weight ratio from 1,000:1 to 2:1, processes for preparing the polycocondensates and use of the polycocondensates in the form of the free acid groups or in a form neutralized with ammonia, amines, alkali metal or alkaline earth metal bases as an additive to detergents and cleaners, as scale inhibitors or as dispersants for finely divided solids are described.

Abstract: In this method, one attaches one or more chelatant molecules to a mono- or polyamino intermediate compound I which is temporarily immobilized on a solid phase by a splittable bond. Thereafter, said bond is split to release the desired conjugate moiety, whereby a reactive site is generated at the splitting site. The conjugate can be coupled to a protein homing factor using said reactive site; the latter being single per chelatant molecule, undesirable cross-linking during conjugation is substantially avoided.

Abstract: Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject.

Abstract: A bleach prepared from an iron (III) complex of a complexing agent of the formula I ##STR1## in which L.sub.1, L.sub.2 mean an optionally substituted alkylene group with 1 to 4 C atomsL.sub.3 means an alkylene group with 1 to 4 C atoms,Z.sub.1, Z.sub.2 mean OH, NH.sub.2, NHR.sub.2,X means N, P.dbd.0, SO.sub.2 HY.sub.1 means OH, NH.sub.2, NHR.sub.3, NR.sub.3 R.sub.4, SO.sub.3 H, PO.sub.3 H.sub.2, NHCOR.sub.5,R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 mean optionally substituted alkyl or optionally substituted phenylexhibits excellent bleaching action.

Abstract: This invention relates to a process for selectively producing and recovering [S,S]-ethylenediamine-N,N'-disuccinic acid by the reaction of L-aspartic acid and 1,2-dihaloethane in an aqueous medium, wherein a stoichiometric deficiency of 1,2-dihaloethane is used and wherein the resultant aqueous solution obtained from the reaction is co-fed to water with a mineral acid to preferentially precipitate out [S,S]-ethylenediamine-N,N'-disuccinic acid from the solution.

Abstract: This invention relates to a process for the production of a solid calcium [S,S]-ethylenediamine-N,N'-disuccinate by the reaction of calcium aspartate and dihaloethane in an aqueous solvent.

Abstract: N-acyldipeptides of formula I ##STR1## wherein R represents a rest of formula ##STR2## and R.sub.4, Y, m, n and Z have the meaning as defined in the description, R.sub.1 represents hydrogen, a 1-10 C. alkyl, an optionally substituted methyl or benzyl,R.sub.2 represents a --CO--A group,wherein A has the meanings as defined in the description,R.sub.3 represents a --(CH.sub.2).sub.p --CO--W group,wherein p and W have the meaning as defined in the description.

Abstract: This invention relates to a method for converting calcium salts of [S,S]-ethylenediamine-N,N'-disuccinic acid to an easily filterable precipitate of [S,S]-ethylenediamine-N,N'-disuccinic acid.

Abstract: A polymeric contrast enhancing agent for magnetic resonance images having a chelating agent, which can be bound to metal ions having at least one unpaired electron, such as gadolinium. Examples of such chelating agents include DTPA-ethylenediamide-methacrylate copolymer and poly-(DTPA-ethylenediamide). These contrast enhancing agents, bound to the metal ions, are then administered to a patient, and following this the MR images are taken.

Abstract: A compound of the following formula ##STR1## wherein m is an integer of 1 to 3, R.sub.1 and R.sub.2 are the same or different and each is hydrogen atom or lower alkyl, and R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are the same or different and each is hydroxy or a ##STR2## (wherein n is 0 or 1, X is --NH-- or --O--, Y is alkylene, A is hydrogen atom, lower alkyl, lower alkoxy, halogen atom or trifluoromethyl, and B is alkyl or alkenyl), with the proviso that two or three of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are hydroxyl groups and that when two of them are hydroxyl groups, the cases where R.sub.3 and R.sub.5 are hydroxy, and R.sub.4 and R.sub.6 are hydroxy are excluded; a complex compound comprising said compound and a metallic atom; and a diagnostic agent containing said complex compound. The above compound is useful as a chelating agent and the complex compound comprising said compound and a metallic atom exhibits superior characteristics as a contrast medium for image diagnosis.

Abstract: Synthesis of ethylenediaminetriacetic acid (ED3A) or its salts is disclosed. A salt of N,N'-ethylenediaminediacetic acid (ED2AH.sub.2) is condensed with formaldehyde to form a stable 5-membered ring intermediate. The addition of cyanide across this cyclic material forms ethylenediamine N,N'-diacetic acid-N'-cyanomethyl or salts thereof (mononitrile-diacid). The nitrile in aqueous solutions may be spontaneously cyclized to form 2-oxo-1,4-piperazinediacetic acid (3KP) or salts thereof, which is the desired cyclic intermediate. In the presence of excess base, salts of ED3A are formed in excellent yield and purity. Alternatively, the starting material is ED2AH.sub.a X.sub.b, where x is a base cation, e.g., an alkali or alkaline earth metal, a is 1 to 2, and b is 0 to 1 in aqueous solutions. The reaction mixture also can be acidified to ensure complete formation of carboxymethyl-2-oxopiperazine (the lactam) prior to the reaction. Formaldehyde is added, essentially resulting in the hydroxymethyl derivative.

Abstract: The synthesis and compound of a new caged calcium which is an ortho-nitrophenyl derivative of EGTA and various intermediates. It is synthesized in ten steps and 24% overall yield. The photosensitive chelator, nitrophenyl-EGTA, has a K.sub.d for Ca.sup.2+ of 80 nM and for Mg.sup.2+ of 8.8 mM. Upon exposure to ultra-violet light (in the region of 350 nm), the chelator is cleaved, yielding iminodiacetic acid photoproducts with known low Ca-affinity (K.sub.d =1 mM). The quantum yield of photolysis of nitrophenyl-EGTA in the presence of Ca.sup.a+ is 0.23 and in the absence of Ca.sup.2+ is 0.20. In experiments with chemically skinned skeletal muscle fibers, a fully relaxed fiber equilibrated with nitrophenyl-EGTA:Ca.sup.2+ complex, in the presence of physiological [Mg.sup.2+ ] (i.e. 1.0 mM), produced maximal contraction after a single flash from a frequency doubled ruby laser (347 nm). Half-maximal tension was achieved in 18 ms at 15.degree. C.

Abstract: The present invention relates to novel technetium-99m complexes and to methods of preparing the complexes. The present invention further relates to a radiopharmaceutical compositions comprising the complexes, to the use of the compositions for examining the renal function, and to a kit for preparing such compositions.

Abstract: In this method, one attaches one or more chelatant molecules to a mono- or polyamino intermediate compound which is temporarily immobilized on a solid phase by a splittable bond. Thereafter, said bond is split to release the desired conjugate moiety, whereby a reactive site is generated at the splitting site. The conjugate can be coupled to a protein homing factor using said reactive site; the latter being single per chelatant molecule, undesirable cross-linking during conjugation is substantially avoided.

Abstract: A process is reported for the preparation of bis(amidocarboxylic acid) involving reacting an ester with an aminocarboxylate compound, the latter being formed from lactams or aminocarboxylic acids and salts thereof. The ester and aminocarboxylate compound are present in a weight ratio of about 1:1 to about 1:4, and reaction is conducted in a mono- or polyhydric alcohol solvent.

Abstract: The present invention relates to a contrast agent for NMR imaging constituted by a complex between a chelating agent and paramagnetic metal cations, wherein said complex corresponds to the formula I: ##STR1## or a physiologically acceptable salt of this complex, in which formula: n and n' are whole numbers from 1 to 4R.sub.1 -R.sub.7 are selected from among H, a halogen, alkyl, alkoxy, aryl, alkenyl, and cycloalkyl groups; with the alkyl groups being optionally substituted by halogen, alkoxy, alkyl, nitrile, nitro or amino; >C(R.sub.6, R.sub.7) can in addition represent >C=O;the three substituents Y are identical or different and represent H or an ionic equivalent of a divalent or trivalent paramagnetic metal cation or of a physiologically acceptable cation derived from an inorganic or organic base,with the condition that at least two of the substituents Y represent ionic equivalents of paramagnetic metal cations.

Abstract: A process for preparing carboxylates of polyoxyalkylene siloxanes and -amines, alkylpolyoxyalkylenes, polyoxyalkylene block polymers, alkylamidepolyoxyalkylenes and alkylpolyglucosides comprising subjecting a primary hydroxyl group-containing polyoxyalkylene compound or alkylpolyglucoside to mild oxidiation. The invention also relates to the novel polyoxyalkylene amine and alkylamidepolyoxyalkylene carboxylates prepared by the process.

Abstract: The present invention is directed to a new class of beta-ketone, beta oxime and beta hydrazine phosphonate NMDA antagonists.

Abstract: 3-Hydroxy-2,2'-iminodisuccinic acid, water soluble salts thereof, a process for their preparation, and their use as biodegradable complexing agents in detergents.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines indicate an optionally endo or exo double bond, Y is selected from the group consisting of alkyl, alkenyl and alkynyl of 2 to 18 carbon atoms and alkyl of 1 to 18 carbon atoms substituted with at least one halogen, X, X' and X.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms, acyl of a fatty acid and acyl of an .alpha. or .omega.-amino acid, n and/or n.sub.1 is 1 and R and/or R.sub.1 is the remainder of an amine or an .alpha. or .omega.-amino acid or n and/or n.sub.1 is 2 and R and R.sub.1 are selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R.sub.

Abstract: Novel N-acyl derivatives of ethylenediaminetriacetic acid are disclosed, as well as a process for preparing the same.

Abstract: A compound of the formula II: ##STR1## wherein n is an integer of 2 to 10,A' is a bivalent linking group formed by reacting both the reactive groups of a cross linking reagent, andB is a residue of a polypeptide compound,and physiologically acceptable salts thereof are disclosed. Such compound is useful as a non-radioactive carrier for radioactive metal elements.

Abstract: Synthesis of ethylenediaminetriacetic acid (ED3A) or its salts is disclosed. A salt of N,N'-ethylenediaminediacetic acid (ED2AH.sub.2) is condensed with formaldehyde to form a stable 5-membered ring intermediate. The addition of cyanide across this cyclic material forms ethylenediamine N,N'-diacetic acid-N'-cyanomethyl or salts thereof (mononitrile-diacid). The nitrile in aqueous solutions may be spontaneously cyclized to form 2-oxo-1,4-piperazinediacetic acid (3KP) or salts thereof, which is the desired cyclic intermediate. In the presence of excess base, salts of ED3A are formed in excellent yield and purity. Alternatively, the starting material is ED2AH.sub.a X.sub.b, where x is a base cation, e.g., an alkali or alkaline earth metal, a is 1 to 2, and b is 0 to 1 in aqueous solutions. The reaction mixture also can be acidified to ensure complete formation of carboxymethyl-2-oxopiperazine (the lactam) prior to the reaction. Formaldehyde is added, essentially resulting in the hydroxymethyl derivative.

Abstract: There are provided chelating agents particularly useful for the preparations of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula X--CHR.sub.1 --NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X wherein (each of the groups Z is a group --CHR.sub.1 X or the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, where A' is an oxygen or sulphur atom or a group --N--Y; A is a group --N--Y or A--(CHR.sub.1).sub.m -- represents a carbon-nitrogen bond or, when the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, A may also represent an oxygen or sulphur atom; each Y, which may be the same or different, is a group --(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2 or a group --CHR.sub.1 X; each X, which may be the same or different, is a carboxyl group or a derivative thereof or a group R.sub.1 ; each R.sub.

Abstract: A novel intermediate useful in the synthesis of ethylenediaminetriacetic acid (ED3A) or its salts. N,N'-ethylenediaminediacetic acid (ED2AH.sub.2) or a salt containing up to one equivalent of base cation is condensed with formaldehyde to form a stable 5-membered ring intermediate. The addition of cyanide across this cyclic material forms ethylenediamine N,N'-diacetic acid-N'-cyanomethyl or salts thereof (mononitrile-diacid), which is a useful intermediate in the production or ED3A. The nitrile in aqueous solutions may be spontaneously cyclized to form 2-oxo-1,4-piperazinediacetic acid (3KP) or salts thereof. In the presence of excess base, salts of ED3A are formed in excellent yield and purity.

Abstract: A composition and method for inhibiting corrosion of ferrous metals in contact with an aqueous solution comprising adding to the system from 0.1 to 500 ppm of an aminohydroxysuccinic acid compound selected from group consisting of compounds of the generalized formulas: ##STR1## wherein R is H or C.sub.1 to C.sub.6 alkyl, optionally substituted with --OH, --CO.sub.2 H, --SO.sub.3 H or phenyl, C.sub.4 C.sub.7 cycloalkyl, or phenyl which is optionally substituted with --OH, or --CO.sub.2 H, and R' is H, C.sub.1 to C.sub.6 alkyl, optionally substituted with --OH or CO.sub.2 H; and ##STR2## wherein R' is as above, and Z is selected from the group consisting of i) --(CH.sub.2).sub.n -- wherein n is an integer from 2 to 10, ii) --(CH.sub.2).sub.2 --X--(CH.sub.2).sub.2 -- wherein X is --O--, --S--, --NR"--; wherein R" is selected from the group consisting of H, C.sub.1 to C.sub.6 alkyl, hydroxyalkyl, carboxyallkyl, acyl, --C(O)OR"' wherein R"' is C.sub.1 C.sub.

Abstract: Comounds having the formula ##STR1## wherein: a is 2 or 3; b is an integer from 0 to 4;Me.sup.(a+) is an ion of an element of atomic number from 57 to 70 or an ion of a transition metal of atomic number 21-29, 42 or 44;E.sup.(b+) is one or more physiologically biocompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units;S is the group --A--O--R wherein:A is --(CH.sub.2).sub.m --; --CH.sub.2 --C(CH.sub.3).sub.2 --; m is an integer from 1 to 5; R is H; linear or branched alkyl of 1 to 8 carbon atoms, said carbon atoms being unsubstituted or substituted by one or more hyroxy group; aralkyl of 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, amino, hydroxy or trifluoromethyl; (poly)-oxa-alkyl of 1 to 10 oxygen atoms and from 3 to 30 carbon atoms;R.sub.1 is R.sub.2 or --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; --(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.

Abstract: Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp, Val, His, Arg, Ser, Thr, Pyr, Trp, 5-HTP, Cys, Met, .tau.-Glu, .beta.-Asp; Y is a (CH.sub.2).sub.3-6 or (CH.sub.2).sub.3-6 having an hydroxy group; R is an hydroxy group or an oxygen atom with a carboxy-protecting group; are useful as neurotropic agents.

Abstract: Complex N-hydroxyimide compounds and carboxy hydroxamic acid-functional derivatives thereof are prepared from organic amines reacted with maleate esters and maleic anhydride. The compounds exhibit strong metal ion chelating properties and are useful as detergent additives to improve stain removal.

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

Abstract: Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with aminoalkylamide derivatives of diethylenetriaminepentaacetic acid ("DTPA") or ethylenediaminetetraacetic acid ("EDTA") or other polyaminocarboxylic or cyclic polyaminocarboxylic chelating agents. These novel imaging agents are characterized by excellent NMR image-contrasting properties and by high solubilities in physiological solutions.A novel method of performing an NMR diagnostic procedure involves administering to a warm-blooded animal an effective amount of a complex as described above and then exposing the warm-blooded animal to an NMR imaging procedure, thereby imaging at least a portion of the body of the warm-blooded animal.

Abstract: Energetic binders, and, more specifically, a class of nitramine-containing homopolymers and co-polymers characterized by favorable viscosity and glass transition temperature are prepared.

Abstract: Compounds suitable for NMR imaging having the formula: ##STR1## wherein a is 2 or 3;b is an integer from 0 to 4;Me.sup.(a+) is Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+), or Mn.sup.(2+) ;E.sup.(b+) is an ion of an alkali metal, alkaline earth metal, alkyl ammonium, alkanol ammonium, polyhydroxyalkyl ammonium, or basic protonated amino acid, said ions representing a total charge of b;m is an integer from 1 to 5;R is H, alkyl with from 1 to 8 carbon atoms, alkyl with from 1 to 8 carbon atoms wherein from 1 to 5 carbons are substituted with OH; aralkyl with 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, hydroxyl, carboxyl, carboxamide, ester, SO.sub.3 H, sulfonamide, lower alkyl, lower hydroxy alkyl, amino, acylamino; (poly)oxa-alkyl with 1 to 50 oxygen atoms and from 3 to 150 carbon atoms, wherein 1 to 5 hydrogen atoms may be substituted by OH; R.sub.1 is the same as R.sub.2 oris --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, CH.sub.2 CH.sub.2 --N(CH.sub.2 COOZ).sub.

Abstract: Therapeutically active pseudo-peptide characterized in that it comprises at least the sequence of the .gamma.-glutamyl-aspartic acid or one of its derivatives. Said pseudo-peptide may be used in the preparation of a pharmaceutical composition useful particularly in the treatment of epilepsy or affections of the central nervous system in general.

Abstract: Processes employing compositions comprising certain amino acids such as aspartic acid, when fully ionized at alkaline pH, effectively inhibit corrosion of ferrous metals in the presence of an aqueous medium. This effect is enhanced with increased fluid velocity.

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

Abstract: This invention produces higher homologs, i.e., differing by at least a --CH.sub.2 -unit, of carbonyloxy-containing compounds by treating the carbonyloxy-containing compounds with carbon monoxide and hydrogen in the presence of a ruthenium-containing compound, a proton donor, an iodide promoter, and optionally, a manganese-containing compound.

Abstract: Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.

Abstract: This present invention provides an improved method for producing N-L-aspartyl-D-alanine fenchyl ester or N-L-aspartyl-methylalanine fenchyl ester and new compositions of fenchol derivatives which are intermediate compositions in the preparation of the above described fenchyl esters.

Abstract: The disclosure is directed to compounds of the formula: ##STR1## wherein n=0, 1, 2, 3 or 4, and R.sub.1 and R.sub.2 may be the sam e or different and are selected from the group consisting of hydrogen and lower alkyl and hydroxy lower alkyl groups containing between 1 and 6 carbon atoms. Complexes of iron(II), iron(III), manganese(II), manganese(III), gadolinium(III), chromium(III), cobalt(II), and nickel(II) and such compounds are useful for enhancing magnetic resonance images of body organs and tissues. Illustrative complexes include (N,N"-bis[N-(2,3-dihydroxypropyl) carbamoylmethyl]diethylenetriamine-N,N',N"-triaceto)-iron(III), (N,N"-bis[N-(2,3-dihydroxypropyl)carbamoylmethyl]diethylenetriamine-N,N',N "-triaceto)manganese(II), (N,N"-bis[N-(2,3-dihydroxypropyl) )carbamoylmethyl]diethylenetriamine-N,N',N"-triaceto)gadolinium(III) and (N,N'-bis[N-(2,3-dihydroxypropyl)-carbamoylmethyl]ethylenediamine-N,N'-dia ceto)manganese(II).

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: Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C.sub.2 -C.sub.5)alkenyl; Z is H or OH, R' is (C.dbd.O)-A(B)(C) wherein A is selected from the group consisting of (C.sub.1 -C.sub.5)alkyl, (C.sub.2 -C.sub.5)alkenyl and (C.sub.2 -C.sub.6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C.sub.1 -C.sub.5)alkyl group optionally substituted with CO.sub.2 H, OH or phenyl and C is CO.sub.2 H, SO.sub.3 H, amino or guanidino; and R" is selected from the group consisting of NH-A(B)(C) or is guanidino; and the pharmaceutically-acceptable salts thereof.

Abstract: Aminosuccinic acid derivatives corresponding to the following general formula (I): ##STR1## wherein R represents an alkyl or alkenyl group having from 10 to 22 carbon atoms which may be branched and/or interupted by one or more oxygen atoms;n represents the number 2 or 3; andK represents hyrogen or a cation;a process for their preparation and their use.

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

Abstract: A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism, useful for the treatment of obesity, hyperlipidemia and maturity-onset diabetes. The active compounds have the general formula ##STR1## or in-vivo hydrolyzable functional derivatives of the carboxylic groups thereof,whereinR.sub.1 and R.sub.2 each independently represents an unsubstituted or substituted hydrocarbyl or hetercyclyl radical;X and Y each independently represents hydrogen, optionally substituted lower alkyl, halogen, cyano, carboxy, lower alkoxycarbonyl or carbamoyl; andQ represents a diradical consisting of a linear chain of 8 to 14 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteratom chain members optionally forming part of a ring structure.