Abstract: Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.

Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.

Abstract: The invention relates to the use of certain chelating agents and their metal chelates and to the use of certain manganese containing compounds, in particular manganese chelates, in the manufacture of a therapeutic agent for use in reducing the cardiotoxicity of an antitumor agent. Such compounds are particularly effective in reducing the side-effects of anthracycline drugs and/or paclitaxel.

Abstract: A compound of formula (I): ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected independently from hydrogen, alkyl, and alkyl substituted with one or more --O-- atoms, or where R.sup.1, R.sup.2 and R.sup.3, R.sup.4 are ring residues. The compound is capable of functioning as a ligand and complexing with paramagnetic Fe(III) ion for use as a second-sphere contrast enhancing agent for magnetic resonance imaging of tissue, and a method of administering the second sphere contrast agent.

Abstract: A method for imaging mammalian tissue utilizing a non-ionic complex of a paramagnetic ion of lanthanide element and a macrocyclic chelating agent.

Abstract: The present invention is directed to a sterile pharmaceutical composition comprising a propofol containing oil-in-water emulsion formulation having as an antimicrobial agent, a member selected from the group consisting of benzyl alcohol and sodium ethylene diamine tetraacetate; benzethonium chloride; and benzyl alcohol and sodium benzoate.

Abstract: The present invention relates to heavy metal chelate compositions, which are used as fungicides and bactericides, and methods of using the compositions. In particular, the present invention relates to a chelate, that is an EDDHA (copper-ethylenediamine-di-o-hydroxyphenylacetic acid), combined with a heavy metal, including iron, tin, zinc, manganese, copper, and combinations thereof.

Abstract: The invention provides a method of functional imaging of a human or non-human animal body, which method comprises administering into the gastrointestinal tract of a said body an effective amount of a composition comprising (a) a first contrast agent comprising a physiologically tolerable manganese compound or a salt thereof, together with (b) a second contrast agent, and generating a functional image of the gastrointestinal tract of said body.This imaging technique has surprisingly been found to provide clear delineation of those portions of the gut wall in which manganese uptake is occurring, thereby enabling not only the detection of tumors in the gut, but also the identification of regions of the gut which may be functioning abnormally.

Abstract: The invention relates to polyrotaxanes that contain metal complexes or iodine-containing benzene derivatives as imaging components for MRT diagnosis and x-ray diagnosis.

Abstract: Compounds which can chelate paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI), the compounds having formula (I) ##STR1## wherein R is a --(CH.sub.2).sub.m --O--R.sub.2 group or hydrogen,R.sub.2 is a (C.sub.6 -C.sub.10) aryl, or an alkyl(C.sub.1 -C.sub.5)-aryl(C.sub.6 -C.sub.10) group, substituted or not by a group L corresponding to a OH group or a OR.sub.3 group, wherein R.sub.3 is a linear or branched (C.sub.1 -C.sub.5) alkyl group; or L is NH.sub.2, halogen, COOH or CONR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently hydrogen, or a linear or branched (C.sub.1 -C.sub.5) alkyl which can be substituted by 1-6 hydroxy groups and/or 1-6 alkoxy groups,R.sub.1 can have the same meanings as R, independently from it, except for hydrogen,Z is independently OH or OR.sub.6, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as previously defined, and R.sub.6 is a (C.sub.1 -C.sub.

Abstract: The invention relates to new compounds that are suitable as contrast media especially for infarction and necrosis imaging, process for their production and pharmaceutical agents that contain these compounds.

Abstract: The invention relates to new metal complex-containing or iodine-containing benzene derivatives that contain pseudopolyrotaxanes. They are valuable compounds for diagnosis. The pseudopolyrotaxane complexes have general formula (I), in which n represents the numbers 6, 7 or 8; m represents the numbers 2 to 50; X represents a direct bond or the radical --O--CO--CH(CH.sub.3)--; R.sub.1 and Y have the meaning that is indicated in the description and represent R.sub.3 --Y--R.sub.4 polyalkylene glycols.

Abstract: The invention provides, as contrast signal generators in MR imaging of the digestive tract, paramagnetic metal chelates of novel acrylic compounds of formula C(R.sup.1 R.sup.2).dbd.CR.sup.3 --CO--Z--A (1) and/or C(R.sup.1 R.sup.2).dbd.CR.sup.3 --O--Z--A--Z--CO--CR.sup.3 .dbd.C(R.sup.1 R.sup.2) (2) in monomer, oligomer, homopolymer and copolymer forms, in which the R.sup.1, R.sup.2 and R.sup.3 represent H or saturated or unsaturated C.sub.1-10 aliphatic radicals optionally substituted by one or more OH groups; Z is a covalent bond or a linker spacer and A is a moiety capable of fixing a paramagnetic metal by chelation. Compounds of type (1) useful in the present invention are, for instance the polyalkylene-aminopolycaboxylic acids such as NTA, EDTA, DTPA, DOTA and like structures, possibly involving additional substituents; an example is the compound BOPTA which is a DTPA derivative carrying a benzyloxypropyl group.

Abstract: Cascade polymer complexes that contain a) complexing ligands of general formula (I), in which A stands for a nitrogen-containing cascade nucleus of base multiplicity a, X and Y, independently of one another, stand for a direct bond or a cascade reproduction unit of reproduction multiplicity x or y, z and W, independently of one another, stand for a cascade reproduction unit of reproduction multiplicity z or w, K stands for the radical of a complexing agent, a stands for numbers 2 to 12, x, y, z and w, independently of one another, stand for numbers 1 to 4, provided that at least two reproduction units are different, and that 16.ltoreq.a.multidot.x.multidot.y.multidot.z.multidot.w.ltoreq.

Abstract: Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.

Abstract: The invention relates to a process for the production of metal-complex carboxylic acid amides, characterized in that a metal-complex carboxylic acid mixture that consists of the metal-complex carboxylic acid and at least one solubilizing substance in dimethyl sulfoxide (DMSO) is pretreated with a dehydrating reagent, optionally with the addition of a coupling adjuvant, and is then reacted with an amine of general formula IA(NH.sub.2).sub.n (I),in whichA stands for the radical of a natural or synthetic amine, andn stands for numbers 1 to 100.

Abstract: This invention relates to improvements in and relating to magnetic resonance imaging of the human or non-human body. The invention particularly relates to a method in which positive and negative contrast agents are administered to enhance image contrast.

Abstract: A composition for use as a contrast medium being particularly suitable for imaging of the stomach, liver, bile duct and gall bladder, said composition comprising as an active ingredient a physiologically acceptable manganese compound and an uptake promoter, wherein the uptake promoter comprises a physiologically acceptable reducing compound containing a physiologically acceptable amino acid or a salt thereof, and/or vitamin D.

Abstract: Novel complexes of paramagnetic ions and compounds bearing long acyl chains have been synthesized as magnetic resonance imaging contrast agents. These novel liposoluble contrast agents may be administered alone, or with lipids, suspending agents or other additives. The lipids may be in the form of liposomes, micelles or lipid emulsions. The contrast agents of the invention have particular use in magnetic resonance imaging of the liver, blood pool and reticuloendothelial system.

Abstract: A novel chelate complex allows the formation of stable solutions of molecular chlorine dioxide. The chelate complexes are composed of the electron-deficient chlorine dioxide molecule, which can accept an electron, and a chelating agent, which can contribute its available electrons to the accepting orbital of the chlorine dioxide molecule. Both active and passive methods of releasing the chlorine dioxide from such chelates by competitive displacement with selected metal cations are presented. In this manner a stabilized solution of molecular chlorine dioxide can be stored until needed and the chlorine dioxide released at time of use for cleaning, disinfection or other uses.

Abstract: 1,4,7,10-Tetraazacyclodedecane butyltriols of general formula I.sub.A ##STR1## in which R.sup.1 means hydrogen or a metal ion equivalent independent of one another andR.sup.2 means a butyltriol radicalas well as their salts with organic or inorganic bases or amino acids are valuable pharmaceutical agents.

Abstract: A contrast medium useful for diagnostic imaging is provided. The contrast medium comprises gel particles, preferably of less than about 90.mu. in mean diameter, the gel particles comprising at least one polymer entrapping at least one contrast enhancing metal.

Abstract: Disclosed are linear and cross-linked polymers suitable for use as a contrast agent for magnetic resonance imaging containing units comprising the residue of a poly(amine) moiety linked to a chelating agent and to one or more pendant (poly)alkylene oxides.

Abstract: The present invention provides a polychelant compound of formula (VII), (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ; B is (CR.sup.1 Y) or --N(CR.sup.1.sub.2 Y)--; each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z being a group CR.sup.1.sub.2 Y; each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2 ; m is 0 or 1 or 2; each n is 2 or 3; q is 0 or 1 when B is (CR.sup.1 Y) and 2 when B is N(CR.sup.1.sub.2 Y); p is an integer having a value of at least 2; each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl, aryl or aralkyl group optionally substituted by one or more hydroxy or alkoxy groups, or two R.sup.1 groups on ring atoms or in Z groups together represent a linker group L; each L which may be the same or different represents a bond or an organic linker group having a molecular weight of less than 1000 and salts and chelates thereof.

Abstract: An x-ray contrast medium containing a multinuclear complex of the formula (M.sub.6 (.mu..sub.3 B).sub.8 A.sub.v).sub.x L.sub.w, wherein M is Mo, W, Re Tc, V, Nb, Ta, Ru, or Fe; .mu..sub.3 B represent a tridentate bridging atom; A is a non-bridging atom; L is a ligand coordinately bonded to at least one M atom; x is a positive integer; and v and w are independently zero or positive integers.

Abstract: The invention relates to new macrocyclic metal complex carboxylic acids of formula II ##STR1## whereby Z.sup.o stands for a metal ion equivalent of atomic numbers 58-71 andR stands for a CHX.sup.1 --CO--NH--CHY.sup.1 --(CH.sub.2).sub.f --COOH group, in which X.sup.1 and Y.sup.1, independently of one another, mean a hydrogen atom, a straight-chain or branched C.sub.1 -C.sub.7 alkyl radical, a phenyl or benzyl group and f means numbers 0 to 9.They can be used as intermediate stages for synthesis of cascade polymer complexes that are suitable as diagnostic agents.

Abstract: The invention relates to new 1,4,7,10-tetraazacyclododecane derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, X and V have various meanings, their metal complexes, pharmaceutical agents containing these compounds, their use in diagnosis and treatment as well as process for the production of these compounds and agents.

Abstract: The present invention relates to the preparation of amino-acyl-type and catecholamine-type compounds having multiple carboxylic acid functional groups. Paramagnetic metal (II) or (III) ion chelate complexes are formed using these compounds for use as intravenous contrast agents to produce enhanced contrast magnetic resonance images of the heart, liver, biliary tree or upper small intestine. The mono- and di-amino acids, their esters and amides, and catecholamine-like derivatives, of EDTA, DTPA, and the like are prepared. The paramagnetic metal (II) or (III) ion complexes are formed and produce T1-related contrast effects in MR images. The compounds and complexes also appear to have low toxicities and to be relatively rapidly and completely cleared from the tissue of a living mammal, e.g. a human being.

Abstract: There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g. DOTA residues, conjugated to a dendritic polyamine backbone molecule, e.g. a starburst dendrimer. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein.

Abstract: Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.

Abstract: The in vivo catalytic dismutation of hydrogen peroxide by pseudocatalase such as a transition metal bicarbonate complex is increased by the addition of a chelating agent, preferably ethylenediaminetetraacetic acid (EDTA), citic acid, 2,6-pyridinedicarboxylic acid, or a salt thereof Further, the stability of a topical composition comprising a transition metal bicarbonate complex is improved by storing the composition under carbon dioxide, preferably under pressure in aerosol form.

Abstract: Methods of providing an image of the gastrointestinal region of a patient and diagnosing the presence of any tumorous tissue in that region using contrast media comprising a combination of at least one polyphosphorylated aliphatic or polyphosphorylated alicyclic compound and at least one paramagnetic ion, wherein the aliphatic and alicyclic compounds comprise at least five carbon atoms, is described. Also described are diagnostic kits for gastrointestinal imaging which include the subject contrast media.

Abstract: This invention relates to improvements in and relating to magnetic resonance imaging of the human or non-human body. The invention particularly relates to a method in which positive and negative contrast agents are administered to enhance image contrast.

Abstract: A skin treatment system comprises preparations for the topical application to the skin of histidine acting as a divalent cation chelator and exfoliant, pyridoxine and pantothenic acid and N-acetyl-D-glucosamine for increasing production of hyaluronic acid, superoxide dismutase and cysteine and vitamin E for decreasing the oxidative degradation of the hyaluronic acid, and pyroll carboxylic acid, or chemical salts thereof, and hyaluronic acid, or chemical salts thereof for providing increased hydration of the skin.

Abstract: The present invention relates to a medicated chewing gum comprising a pharmaceutically active agent incorporated therein. The medicated gum is used as a means for administering the active agent to a subject. The invention also relates to a method of preparing the medicated chewing gum. The process involves the formation of a cyclodextrin-active agent inclusion complex, which is dried and mixed with a granulated gum base without adding water or other solvents. The process is carried out under controlled temperature and humidity and the blended components are cold-pressed to produce a final gum product.

Abstract: Compounds of general formula I ##STR1## wherein Z.sup.1, Z.sup.2, X, R.sup.2 and R.sup.3 are as herein defined, are valuable pharmaceutical agents. In particular, the compounds are useful as contrast agents in NMR diagnosis.

Abstract: The disclosed metal complexes are suitable as contrast media for computer tomography of the liver and the biliary tracts.

Abstract: A method for imaging mammalian tissue utilizing a non-ionic complex of a paramagnetic ion of lanthanide element and a macrocyclic chelating agent.

Abstract: Chelate compounds of general formula I ##STR1## wherein X is a hydrogen atom and/or a metal ion equivalent of an element of atomic numbers 21-29, 31, 32, 37-40, 42-44, 49 or 57-83, andZ.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, as well as their salts with inorganic and/or organic bases, amino acids or amino acid amides, are valuable pharmaceutical agents, e.g., for NMR imaging.

Abstract: The invention concerns NMR imaging contrast compositions comprising magnetically responsive species coupled to physiologically acceptable amphipatic organic substrate materials in the form of mixed micelles suspended or dispersed in a physiologically acceptable aqueous liquid carrier. The compositions are particularly useful for diagnostic investigations of the blood-pool. The invention also concerns the preparation of the mixed micelles, as well as of injectable compositions containing the mixed micelles as contrast agents for MRI purpose.Once injected, the mixed micelles of the compositions behave as imaging contrast enhancers, e.g. they will improve the quality and resolution of the electronically processed images obtained during MRI examinations of the circulation and/or circulation targeted organs.

Abstract: The invention provides a method of monitoring the vasodilatory or vasoconstrictive effects of a physiologically active substance administered to a human or non-human animal body, said method comprising the steps of: administering said substance into said body; administering into the systemic vasculature of said body a contrast enhancing amount of an intravascular paramagnetic metal containing magnetic resonance imaging contrast agent; subjecting said body to a magnetic resonance imaging procedure capable of generating from magnetic resonance signals from said body a series of temporally spaced images of at least a part of said body into which said agent passes, said procedure being a fast imaging procedure having an image acquisition time of less than five seconds; and detecting temporal variations in said signals or images whereby to monitor the vasoconstriction or vasodilation induced by said substance.

Abstract: The present invention provides a method of improving the sensitivity and accuracy of a lead assay. The method enhances the recovery of lead during isolation of the lead from interfering compounds by maintaining the lead in a sample solution and making the recovered lead available for detection by the assay. An enhancing reagent complexes with the lead isolated in the sample solution. The enhancer includes a chelator having a lead equilibrium binding constant in the range of about 4 log K to about 13 log K. A kit for performing such a lead assay is also provided.

Abstract: A contrast enhancing agent for magnetic resonance images having a chelating agent, which can be bound to metals having at least one unpaired electron. Examples of such chelating agents include 3,6,9-tris(carboxymethyl)-1, 11-bis(dimethylamine)-3,6,9-triazaundecane; 3,6,9-tris(carboxymethyl)-1, 11-bis(diethanolamino) 3,6,9-triazaundecane; 3,6,9-tris(carboxymethyl)-1, 11-bis(tris(hydroymethyl) aminomethane)-3,6,9-triazaundecane; 3,6-bis(carboxymethyl-1,8-bis(N-carboxymethylglucosamino)-3,6-diazoctane; DTPA-bis(galactosamide), DTPA-Bis(glucosamide), DTPA-Bis(pyridoxamide), and poly-(DTPA-ethylenediamide).

Abstract: The present invention relates to water-soluble, lipophilic contrast-enhancing agents, pharmaceutical compositions thereof and methods for diagnostic analysis, particularly NMR or MRI analysis using these contrast-enhancing agents. The water-soluble, lipophilic contrast-enhancing agents are chelates of a paramagnetic, ferromagnetic or diamagnetic metal ion(s) complexed with completing acids which contain at least one short-chain fatty acyl moiety having from about 0 to about 6 carbon atoms in its structure.

Abstract: Compounds of general Formula I ##STR1## wherein Z.sup.1 and Z.sup.2 in each case independently mean the residue--(CH.sub.2).sub.m --(C.sub.6 H.sub.4).sub.q --(O).sub.k --(CH.sub.2).sub.n --(C.sub.6 H.sub.4).sub.l --(O).sub.r --R,whereinm and n means the numbers 0-20,k, l, q and r means the numbers 0 and 1, andR means a hydrogen atom, an optionally OR.sup.1 -substituted C.sub.1 -C.sub.6 -alkyl residue, or a CH.sub.2 COOR.sup.1 group with R.sup.1 meaning a hydrogen atom, a C.sub.1 -C.sub.6 -alkyl residue, or a benzyl group,with the proviso that at least two substituents X stand for a metal ion equivalent; that one of the substituents Z.sup.1 and Z.sup.2 stands for a hydrogen and the other is not H; that--if n and l each means the number 0--k and r do not simultaneously mean the number 1; that --(O).sub.r --R is not --OH; and that Z.sup.1 and Z.sup.2 are not --CH.sub.2 --C.sub.6 H.sub.4 --O--CH.sub.2 --COOCH.sub.2 C.sub.6 H.sub.5 or --CH.sub.2 --C.sub.6 H.sub.4 --O--(CH.sub.2).sub.5 --COOCH.sub.2 C.sub.6 H.sub.

Abstract: Novel complexes of paramagnetic ions and compounds bearing long acyl chains have been synthesized as magnetic resonance imaging contrast agents. These novel liposoluble contrast agents may be administered alone, or with lipids, suspending agents or other additives. The lipids may be in the form of liposomes, micelles or lipid emulsions. The contrast agents of the invention have particular use in magnetic resonance imaging of the liver, blood pool and reticuloendothelial system.

Abstract: A method for measuring temperature and/or pH in vivo using paramagnetic compounds, e.g., lanthanide complexes, in conjunction with NMR has been developed. The chemical shift of the nuclear spin in these complexes can then be correlated to temperature. This non-invasive temperature measurement method is particularly useful in monitoring temperature of cancerous tissue during hyperthermic treatment to destroy the cancerous tissue or tumor.

Abstract: The invention relates to new diethylenetriaminepentaacetic acid derivatives, their complexes and complex salts, that contain an element of atomic numbers 20-32, 39-51 or 57-83, pharmaceutical agents that contain these compounds and their use as contrast media and antidotes.

Abstract: The present invention relates to the use of paramagnetic materials, such as lanthanide chelates, as contrast agents in magnetometric analysis, especially imaging. The invention is particularly directed to structural and functional diagnosis or imaging.

Abstract: The invention relates to complex compound as well as their salts consisting of at least one metal ion and one complexing agent of general formula I ##STR1## in which Z.sup.1, Z.sup.2 and s have different meanings, as well as their use for the production of agents for radiation therapy and for NMR diagnosis and diagnostic radiology, especially for contrasting the hepatobiliary system. Further, the invention relates to a process for the production of these compounds and agents.