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: Selected lanthanum carbonate hydrates may be administered into the gastrointestinal tract, to treat hyperphosphataemia in patients with renal failure.

Abstract: Texaphyrins substituted with imidazda are provided.

Abstract: This invention relates to new bifunctional chelating agents with intermittent chalcogen atoms, pharmaceuticals containing these compounds, their use in radiodiagnostics and radiotherapy, and methods for the production of these compounds.The compound according to the invention has the general formula (I)M--Lwhere M represents a radionuclide and L a ligand of the general formula (II).It was found, surprisingly, that these new, bifunctional chelating agents with intermittent chalcogen atoms and their coupling products with compounds that accumulate specifically are excellently suited for producing radiopharmaceuticals for diagnostic and therapeutic purposes.

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: Ligands for radiopharmaceutical use are capable of chelating radiometal species and of being bound to biological targeting molecules. The ligands have the formula (a) and (b), where A, A'=--SZ or Y, B=O or S, Y=(c), Z=H or a thiol protecting group, m=2 or 3, n=2 or 3, q=0 or 1, R=H or unsubstituted or substituted hydrocarbon and pharmaceutically acceptable salts, provided that at least one CR.sub.2 group represents CO and forms, together with an adjacent N atom; a --CONR-- amide group.

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 present invention relates to cyclic terpyridine-lanthanide complexes having 8 nitrogen atoms and 10 carbon atoms in the macrocycle and containing a functional group in the terpyridine moiety. The invention also relates to a process for the preparation of cyclic terpyridine-lanthanide complexes through the condensation of terpyridine hydrazines with pyridine-2,6-dialdehydes or -ketones. The compounds can be complexed with oligonculeotides and are useful in the sequence-specific cleavage of RNA.

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: 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: 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: The invention relates to new, multiply substituted 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, their use as contrast media and antidotes, and process for the production of pharmaceutical agents.

Abstract: The invention concerns gadolinium complexes of formula: ##STR1## in which R represents a group of formula: ##STR2## in which X is Br or I; R.sub.1 is H or optionally hydroxylated alkyl;R.sub.2 is hydroxylated alkyl; oralternatively R.sub.1 is H and R.sub.2 is a group of formula: ##STR3## X being as defined above, and R'.sub.1 and R'.sub.2 being as defined for R.sub.1 and R.sub.2 excepted that they do not represent A, provided that --CO--NR.sub.1 R.sub.2 or --CO--NR'.sub.1 R'.sub.2 comprises at least 2 hydroxyl groups, and M represents H or the cation of an inorganic or organic base.

Abstract: Cascade polymer complexes that containa) complexing ligands of general formula IA--{X--?Y--(Z--(W--K.sub.w).sub.z).sub.y!.sub.x }.sub.a, (I)in whichA 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, that 16.ltoreq.a.multidot.x.multidot.y.multidot.z.multidot.w.ltoreq.

Abstract: Tetraazacyclododecane compounds of general formula I ##STR1## in which E and Q are defined herein and their salts with inorganic and/or organic bases, amino acids or amino acid amides are valuable pharmaceutical agents.

Abstract: A novel metal-encapsulated fullerene compound wherein a side chain is introduced in a metal-encapsulated fullerene is provided.A metal-encapsulated fullerene compound represented by the following structural formula (1) is synthesized by causing a disilirane derivative or digermirane derivative having the following structural formula (2) to react with a metal-encapsulation fullerene so as to add functional groups to the fullerene. ##STR1## Herein, M is an encapsulated metal atom, m is an integer from 1 to 3, n is an even number from 28 to 200, and R is a t-butyl group or an aromatic group having alkyl groups in the 2,6-positions, such as mesityl, 2,6-diethylphenyl or 2,6-dimethylphenyl groups.

Abstract: The invention relates to certain substituted derivatives of aminopolycarboxylic acids and metal chelates thereof. The compounds are particularly suitable for use as diagnostic agent. For example, the compounds can be used as radiodiagnostic agents, detoxification agents and contrast agents for diagnostic imaging processes. In particular, the high relaxivity paramagnetic metal chelates of substituted aminopolycarboxylic acids are especially suited for use as magnetic resonance imaging contrast agents.

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: This invention relates to a detectable molecule comprising a biospecific binding reactant attached to a luminescent lanthanide chelate comprising a lanthanide ion and a chelating ligand of the formula ##STR1## wherein --A-- is a bivalent aromatic structure selected from the group consisting of ##STR2## One of the two groups G.sub.1 or G.sub.2 is used for coupling the chelate to a biospecific binding reactant. The lanthanide ion is europium(III), terbium(III), dysprosium (III) or samarium (III).

Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.

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: Cascade polymer complexes that containa) complexing ligands of general formula IA-{X-?Y-(Z-<W-K.sub.W >.sub.Z).sub.y !.sub.x }.sub.a (I),in whichA 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 for the product of the multiplicities,16<a.multidot.x.multidot.y.multidot.z.multidot.

Abstract: Described are novel, unsymmetrical oligo-2,6-pyridine complexing agents. Also described are metal chelates and targeting immunoreagents containing such completing agents as well as diagnostic and therapeutic compositions containing such immunoreagents and diagnostic and therapeutic methods of using the immunoreagents.

Abstract: This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.

Abstract: The invention provides as new compounds cis-xis-cis-tetrasubstituted cyclopentane compounds which are expected to be useful as chelating agents for alkaline earths, transition, lanthanide, and actinide metal ions. The compounds have Formula (I). Each of the groups X.sup.1, X.sup.2, X.sup.3, and X.sup.4 comprises at least one potential ligand donor group, or one of the groups X or Z may comprise a group which may permit attachment to a biological active molecule or insoluble support.

Abstract: Process for the preparation of N-alkyl substituted metal carbamate solutions characterized in that a water solution of the salt of the metal of which the corresponding carbamate is to be obtained, is reacted with an organic solution, basically consisting of an aprotic solvent and a secondary amine, saturated with carbon dioxide.The above solutions can be used as catalysts in polymerization reactions of unsaturated monomers or for supporting metals on inorganic oxides.

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: Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O.sub.2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.

Abstract: The invention provides polymeric polychelants containing polymer repeat units of formula ?L--Ch--L--B! (where Ch is a polydentate chelant moiety; L is an amide or ester linkage; B is a hydrophobic group providing a carbon chain of at least 4 carbon atoms between the L linkages it interconnects) or a salt or chelate thereof, with the proviso that where Ch is 2,5-biscarboxymethyl-2,5-diazahex-1,6-diyl, the polychelant is metallated with lanthanide or manganese ions or B provides a carbon chain of at least 10 carbon atoms between the L linkages it interconnects and their salts and chelates. The paramagnetic polychelates of the polychelants of the invention have remarkably high R.sub.1 relaxivities.

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: The invention provides amphiphilic compounds of the formula (I) Ch--(--L--Ar--(--AH).sub.n).sub.m (where Ch is a hydrophilic chelant moiety or a salt or a chelate thereof); each L is an optionally oxo substituted C.sub.2-25 -alkylene linker wherein at least one CH.sub.2 moiety is replaced by a group X.sup.1 (e.g. L may include a chain sequence, an X.sup.1 (CH.sub.2 CH.sub.2 X.sup.1).sub.u (where u is a positive integer) such as X.sup.1 (CH.sub.2 CH.sub.2 X.sup.1).sub.u, CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1, CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1, etc.), and wherein L is optionally interrupted by a metabolizable group M but with the provisos that the terminus of L adjacent Ch is CH.sub.2 and that the terminus of L adjacent Ar is X.sup.1 or a CH.sub.2 group adjacent or separated by one CH.sub.2 from a group X.sup.1 (thus, for example the L--Ar linkage may be L.sup.1 --X.sup.1 --Ar, L.sup.1 --CH.sub.2 --Ar, L.sup.1 --X.sup.

Abstract: The invention relates to the production of solid, powdery carboxylates of Rare Earth elements, particularly Nd, La, Pr, and Ce, where the ligands coordinated to the metal are preferably long chain, branched carboxylic acids, most preferably 2-ethylhexanoic, neodecanoic (versatic) and naphthenic acids. The process involves batch precipitation of the product by utilizing Rare Earth water soluble salts, preferably Rare Earth nitrates, and salts of the carboxylic acid and washing the product with water, alcohol, water and alcohol mixtures or combinations thereof.

Abstract: There is provided a method for making a monovalent inorganic anion-intercalated hydrotalcite-like material by first reacting a magnesium-containing powder and a transition alumina powder in a carboxylic acid-free, aqueous suspension to form a meixnerite intermediate. This intermediate is then contacted with a monovalent inorganic anion, in its acid or soluble salt form, to make a hydrotalcite-like material. The latter is then separated from the suspension. Representative materials include a bromide-, chloride-, nitrate- or vanadate-intercalated, hydrotalcite-like material.

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: The invention relates to new metal complexes of dendrimeric macromolecules that contain 8 to 64 ions of an element of atomic numbers 21-129, 39, 42-44, or 57-83 and a polymeric, complexing ligand of formula IA--(X).sub.b (I)in which A, X and b have different meanings, agents that contain these compounds as well as the use of the latter in diagnosis. The invention further relates to a process for the production of the complexes and agents.

Abstract: A metal chelate comprising a compound having the following formula and one or more metal ions which metal ions are a radionucleotide or a paramagnetic metal ion: ##STR1##

Abstract: The present disclosure details the preparation of hydroxamic-acid based bifunctional chelators and their use in conjugating metal ions to proteins and nucleic acids for tumor or tissue imaging or therapy purposes. Some preferred aspects of the disclosure involve the preparation of trisuccin, chemical name N-?tris(2-N- benzyloxyaminocarbonylethyl)! methylsuccinamic acid, which is a hydroxamic acid/succinate based structure that is particularly useful for binding radionuclides such as .sup.99m Tc, .sup.186 Re and .sup.67 Cu.

Abstract: A group conjugates having a functionalized polyaminocarboxylate chelant that form complexes with rare earth-type metal ions, covalently attached to an antibody or antibody fragment, can be used for therapeutic and/or diagnostic purposes.

Abstract: An amphipathic polychelating compound including a hydrophilic polymeric moiety having a main backbone and a plurality of reactive side groups, a lipid-soluble anchor linked to the N terminal of the polymeric moiety, and a plurality of chelating agents linked to the side groups of the polymeric moiety. The polychelating compounds are bound to liposomes or micelles for use as diagnostic and therapeutic agents.

Abstract: This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.

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 invention relates to the use of macrocyclic metal complexes that consist of a complexing agent of formula I and at least one metal ion of an element of atomic numbers 21-29, 42, 44 or 57-70 ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3 and A are as set forth in the specification, are useful as temperature sensors.

Abstract: A group of functionalized polyaminocarboxamide modified chelators, such as 1,4 7,10-tetraaza-1-N-(1-carboxy-3-(4-aminophenyl)propyl)-7-N-(1-carboxymethyl )bis-4,10-N,N-(carboxamidomethyl)cyclododecane and 1,4 7,10-tetraaza-1-N-(1-carboxy-3-(4-aminophenyl)propyl)bis-4,7-N,N-(1-carbox ymethyl)-10-N-(carboxamidomethyl)cyclododecane are disclosed. These modified chelators are capable of forming complexes with rare earth-type metal ions. When the complexes are covalently attached to an antibody or antibody fragment, they can be used in therapeutic and diagnostic applications.

Abstract: Bicyclopolyazamacrocyclophosphonic acid compounds are disclosed which may form inert complexes with Gd, Mn or Fe ions. The overall charge of the complex can be varied to alter the in vivo biolocalization. Such complexes can be covalently attached to an antibody, antibody fragment or other biologically active molecule to form conjugates. The complexes and conjugates are useful as contrast agents for diagnostic purposes.

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.

Abstract: The present invention relates to the use of water-soluble texaphyrin-diamagnetic metal complexes retaining lipophilicity as photosensitizers in the treatment of benign and malignant neoplastic tissue.

Abstract: A corrosion inhibited fuel mixture includes a hydrocarbon fuel, at least one vanadium composition, and a yttrium composition. The concentration of the yttrium composition in the mixture provides at least a stoichiometric amount of yttrium for a substantially complete reaction between the yttrium and V.sub.2 O.sub.5 formed from the vanadium composition when the mixture is burned. The yttrium and V.sub.2 O.sub.5 react to form YVO.sub.4. One particular yttrium composition useful as a hydrocarbon fuel soluble, water stable vanadium corrosion inhibitor incorporates a yttrium ester having at least four carbon atoms and a hydrocarbon fuel soluble chelating agent that includes 2,4-pentanedi.?.e.!..Iadd.o.Iaddend.ne. The complex has a molar ratio of 2,4-pentanedi.?.e.!..Iadd.o.Iaddend.ne to yttrium of up to 5:1.