Abstract: Perfluoroalkyl-containing complexes with sugar radicals of general formula I 1

Abstract: Perfluoroalkyl-containing complexes with polar radicals of general formula I

Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one salicylamidyl moiety. Also provided are probes incorporating the salicylamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

Abstract: 1,4,7,10-Tetraazacyclodedecane butyltriols of general formula IA in which R1 means hydrogen or a metal ion equivalent independent of one another and R2 means a butyltriol radical as well as their salts with organic or inorganic bases or amino acids are valuable pharmaceutical agents.

Abstract: Bacteriochlorins and bacteriopurpurins useful for photodynamic therapy and methods for their manufacture are described herein. Methods for producing the claimed compounds include contacting meso-diacrylate porphyrin precursors with a solvent and a base catalyst at sufficient temperature and time to yield the desired conversion. Reduced bacteriochlorins can be produced by contacting unsaturated bacteriochlorins or bacteriopurpurins with a hydrogenation catalyst and hydrogen. These methods provide new routes for synthesizing bacteriochlorins and bacteriopurpurins from symmetrical and asymmetrical meso-diacrylate porphyrins.

Abstract: A method for the reduction in iodine content in a mixture, particularly in a mixture of carboxylic acids and/or carboxylic anhydrides with alkyl iodides and/or hydriodic acid, comprises contacting the organic medium in the vapor phase at elevated temperature with a metal salt dispersed on activated charcoal. The metal salt may be a carboxylate salt, a carbonate, an oxide, a hydroxide and any other salt, which may react with the organic medium to give a metal carboxylate salt. The metal may be a main group element, a lanthanide, an actinide, zinc and copper. This process converts alkyl iodide compounds converted to their corresponding carboxylate esters, while the iodine is bound in the purification mass as inorganic iodide.

Abstract: An aminopolycarboxylic acid compound represented by the following formula or analogous thereof: The aminopolycarboxylic acid compound of the present invention can be used as a chelating agent for various metals, which is excellent in the biodegradability and masking effect on metals.

Abstract: The present invention provides a triaminepentaacetic acid compound which can be used as a ligand to coordinate to a metal ion to form a paramagnetic metal complex. The paramagnetic metal complex of the present invention can be used as a contrast agent for magnetic resonance imaging (MRI).

Abstract: The invention relates to compounds useful as radiosensitizers in tumor therapy.

Abstract: The present invention relates to novel ligands for forming metal complexes that absorb or fluoresce in the visible or near-infrared (NIR) region of the electromagnetic spectrum, new complexes incorporating such ligands, process for preparing such complexes, and methods of imaging or therapy using such agents. More particularly, the present invention specifically pertains to novel metal complexes derived from quinoline based heterocyclic N2O3, N3O3, N3O4, N3O5 and N2OS ligands, and are useful as general imaging, diagnostic, or therapeutic agents employing optical, nuclear medicine, or magnetic resonance procedures.

Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.

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

Abstract: Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the &agr;, &ggr;, or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Abstract: A method for diagnostic imaging a site in a patient. The method involves the use of an immunoreactive group which is linked to an unsymmetrical oligo-2,6-pyrimidine complexing agent.

Abstract: Cascade polymer complexes containing a) complexing ligands of general formula I A—{X—[Y—(Z—( W—Kw)z)y]x}a  (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≦a·x·y·z·w≦64 holds true for the product of the multiplicities, b) at least 16 ions of an element of atomic numbers 20 to 29, 39, 42, 44 or 57-83 and c) optionally cations of inorganic and/or organic bases, amino acids or amino acid amides are valuab

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(R1R2)═CR3—CO—Z—Z (1) and/or C(R1R2)═CR3—CO—Z—Z—Z—CO—CR3═C(R1R2) (2) in monomer, oligomer, homopolymer and copolymer forms, in which the R1, R2 and R3 represent H or saturated or unsaturated C1-10 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-aminopolycarboxylic 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: A method has been developed for the solution-based metal exchange of carboxylato-alumoxanes [Al(O)x(OH)y(O2CR)z]n with a wide range of metal cations. Metal-exchanged carboxylato-alumoxanes are new, particularly those in which about 10% to about 50% or more of the Al ions are exchanged for other metal ions. Additionally, the carboxylic acid ligands can be stripped from the boehmite core of metal-exchanged carboxylato-alumoxanes at low temperature leading to the formation of metal-exchanged boebmite particles. These new material phases can be used as intermediates for preparation of mixed metal aluminum oxide materials. Thermolysis of the metal-exchanged carboxylato-alumoxanes or metal-exchanged boehmite particles results in doped aluminas (M/Al2O3), binary (MAlOx), ternary (MM′AlOx) and even more complex metal aluminum oxide compounds, where M and M′ are metal ions other than those of aluminum and are preferably those of Lanthanide metals or transition metals.

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: In the metallation of complexing agents such as DTPA-BMA with a lanthanide using a lanthanide oxide such as the lanthanide source, oxalic acid is used as a reaction accelerator.

Abstract: A process for producing high-purity hydrotalcites by reacting alcohols or alcohol mixtures with at least one or more divalent metal(s) and at least one or more trivalent metal(s) and hydrolysing the resultant alcoholate mixture with water. The corresponding metal oxides can be produced by calcination.

Abstract: Compounds of formulae (I) and (II) wherein the R, R1, R2, R3 and R4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.

Abstract: Mixed-metal chelates represented by the following general formula CaM(III)EDTA(OH).xH2O wherein M is a trivalent transition metal and x is 0, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, or 8 and a process for their preparation are disclosed. The process comprises the steps of a) reacting calcium hydroxide or calcium oxide, ethylenediaminetetraacetic acid, and a transition metal-containing material in an aqueous medium, optionally in the presence of an oxidant to convert any transition metal present in a divalent form to its trivalent form; and b) separating the formed mixed-metal chelate by filtration or evaporation. These mixed-metal chelates are useful as catalyst precursors and dietary supplements.

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: 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,provides that at least two reproduction units are different and that for the product of the multiplicities,16.ltoreq.a.multidot.x.multidot.y.multidot.z.multidot.w.ltoreq.

Abstract: Tripodal chelating agents incorporating imine C.dbd.N bonds are disclosed for the formation of lanthanide and other metal complexes which are relatively stable in the presence of water at neutral pH.

Abstract: The present invention provides a method of contrast enhanced ultrasonic diagnostic imaging comprising administering to a subject a contrast enhancing amount of spheres or particles comprising a matrix enclosing a contrast agent which reflects sound waves, and generating an ultrasonic image of said subject wherein the matrix comprises a polymer held together by chemical bonds and wherein the polymer is selected from the group consisting of acrylates, polystyrene and derivatives thereof.

Abstract: Compounds of formulae (I) and (II) ##STR1## wherein the R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.

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: 3-,8-substituted deuteroporphyrin derivatives with various substituents in the 13- and 17-positions of the porphyrin skeleton are suitable as pharmaceutical agents for use in photodynamic therapy (PDT) and for MRI therapy monitoring.

Abstract: The invention includes hydrolyzable and polymerizable silanes, methods of making them and using them to obtain silicic acid(hetero)polycondensates and silicic acid(hetero)polymerizates. The hydrolyzable and polymerizable silanes have the formula I, ##STR1## wherein A=O, S, NH or C(O)O; wherein B=a straight chain or branched organic residue with at least one C.dbd.C double bond and from 4 to 50 carbon atoms;R is an alkyl group, alkenyl group, aryl group, alkylaryl group or an arylalkyl group;R' is a substituted or unsubstituted alkylene group, arylene group, arylenealkylene group or alkylenearylene group each having zero to ten carbon atoms, with the proviso that the substituted groups each have at least one oxygen atom, sulfur atom and/or amine group substituent;R.sup.

Abstract: .sup.99m Tc complexes of formula L.sub.n Tc.dbd.NR, L.sub.n Tc--N.dbd.NY, or L.sub.n Tc--(N.dbd.NY).sub.2 wherein each L is independently a monodentate or multidentate ligand;Y is a substituted or unsubstituted aryl group or substituted or unsubstituted alkyl group;R is Y or the grouping --NR.sup.1 R.sup.2 ;n is 1-4;where at least one of R or Y is combined with one or more of the L groups; R.sup.1 and R.sup.2 are H, substituted or unsubstituted aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and are the same or different, provided that both are not hydrogen.

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: Stable Rare Earth carboxylate liquids having high concentrations of Rare Earths and suitable for use in forming active Ziegler Natta catalysts, are prepared with stabilizing agents such as water and/or acid. The liquids comprise from about 4.5% to about 20% Rare Earth element(s). A novel process for making is disclosed.

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 synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT.

Abstract: Rare earth carboxylates in solid form are prepared or treated with a solubilizing agent to improve the solids solubility in aliphatic solvents. Other methods, such as treatment of the aliphatic solvent, to improve the solubility of solid rare earth carboxylates in aliphatic solvents are also described. Solubilizing agents identified for use include, but are not limited to, carboxylic acids, poly-acids, glycols, alcohols and mixtures thereof. These processes and treatments are particularly useful in regard to solid rare earth versatate, rare earth neodecanoate, rare earth octanoate, rare earth 2-ethyl hexanoate and rare earth naphthenate compositions.

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 the field of radiation sensitizers and the use of texaphyrins for radiation sensitization and other conditions for which X-ray radiation has proven to be therapeutic.

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: Cascade polymer complexes having a complexing ligand with at least two different reproduction units and having a complexing agent which is a macrocyclic group having an amide grouping or a linear DTPA-type group having a linkage to the polymer through the central nitrogen.

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: A process for producing solid, powdery carboxylates of Rare Earths (RE) elements, among them mainly Nd, La, Pr and Ce, where the ligands coordinated to the metal are long-chain, branched carboxylic acids is provided. Preferably, the carboxylic acids are selected from the group consisting of: 2-ethylhexanoic, neodecanoic, versatic and naphthenic acids.

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: 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 it hydrogen atom, a C.sub.1 -C.sub.6 -alkyl residue, or a benzyl group,X means a hydrogen atom and/or a metal ion equivalent of an element of atomic number 21-29, 42, 44 or 57-83,with the provisos that at least two the 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 mean 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.

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

Abstract: Families of Diels Alder adducts and of metal complexes of Diels Alder adducts, which are useful as particularly active compounds for use in photodynamic therapy, are disclosed. The Diels Alder adducts and a preferred family of metal complexes have the structures of Formulas 3 and 4, below: ##STR1## where R1, R2, R3 and R4 can be the same or different, and each is methyl, ethyl, an amino acid moiety which is a part of an amide produced by reaction between an amine function of a naturally occurring amino acid and a carbonyl function of the adduct, or a monoclonal antibody moiety which is attached to the adduct moiety through a carbonyl which is a part of an amide produced by reaction between an amine function of a monoclonal antibody and a CO.sub.2 R', CH.sub.2 CO.sub.2 R' or CH.sub.2 CH.sub.2 CO.sub.

Abstract: Texaphyrin metal complex-oligonucleotide and -oligonucleotide analog conjugates are provided where the texaphyrin is bound to an internal linkage of the oligonucleotide or oligonucleotide analog, the conjugates having catalytic activity for the hydrolysis of ribonucleic acid. Further, conjugates demonstrating catalytic turnover are described, the conjugates being especially effective under conditions where the concentration of RNA target exceeds that of available conjugate.

Abstract: Ligands for radiopharmaceutical use are capable of chelating radiometal species and of being bound to biological targeting molecules. The ligands have formula (a) and (b), where A, A'=--SZ or Y, B.dbd.O or S, Y.dbd. (c), Z.dbd.H or a thiol protecting group, m=2 or 3, n=2 or 3, q=0 or 1, R.dbd.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: A synth .sup.99m Tc complex which contains the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2 and an organic ligand which confers biological target-seeking properties on the technetium complex, where R is an aryl group, a substituted or unsubstituted alkyl group or the group --NR.sup.1 R.sup.2 ; Y is an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are H, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and are the same or different provided that both are not hydrogen. Radiopharmaceuticals comprising this complex are also described, together with methods for the preparation of the complex.