Abstract: A compound of the formula

Abstract: The present invention relates to a process for labeling a synthetic or natural ribonucleic acid (RNA). It also relates to RNA fragments, which have been labeled by fragmenting the RNA to free a terminal phosphate of each fragment for further reaction, and labeling each fragment at the freed terminal phosphate which is located at the 3′ end and/or the 5′ end of each fragment of the RNA, and to the use of such RNA fragments, for example, in the field of medical diagnosis.

Abstract: Cyclic bis benzimidazole ligands of the following formula are formed by contacting a (2-aminophenyl)-benzimidazole-4-carboxaldehyde ethylene acetal or a (2-nitrophenyl)-benzimidazole-4-benzaldehyde with an acid optionally in the presence of a metal or a metal salt. wherein R1 and R2 may be the same or different and are selected from H, an alkyl having 1 to 10 carbon atoms, a benzyl group, a substituted 2-ethylphenyl group, a carbonyl group, a phenyl substituent, a tosyl group, and an alkylsulfonate group; R3 and R4 may be the same or different and are selected from H, methyl, and ethyl; and R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18 may be the same or different and are selected from H, alkyl having 1 to 10 carbon atoms, fluoride, chloride, bromide, iodide, nitro, amino, a carboxylate, an ester, and a phenyl group.

Abstract: Compounds of formula (I) in which R is in which R is hydrogen, a straight or branched or cyclic C1-C6 alkyl group, unsubstituted or substituted by 1 to 10 oxygen atoms, or a C1-C20 alkyl group, optionally interrupted by a phenylene, in turn substituted by a straight or branched C1-C6 alkyl group, unsubstituted or substituted by 1 to 3 C1-C7 alkyl groups; the phenylene group being unsubstituted or substituted by alkoxy, carboxy, sulfamoyl, hydroxyalkyl, amino groups; as well as its complexes with a bi- or trivalent metal ion having an atomic number from 20 to 31, 39, 42, 43, 44, 49, or from 57 to 83, as well as its salts with anions of physiologically acceptable organic acids chelated complexes of these compounds are used as contrast agents for nuclear magnetic resonance imaging.

Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example 1

Abstract: Zinc dithiocarbamates are obtained in especially readily filterable form and high purity when zinc salts are first added, in aqueous solution, to the secondary amines underlying the zinc carbamates, so that a zinc salt complex of the amines is formed, and carbon disulfide and then sodium hydroxide solution are then introduced, with stirring, into the aqueous suspension so obtained, the temperatures being maintained in the range from room temperature to the boiling temperature of carbon disulfide until the reaction has completely finished.

Abstract: Novel compounds capable of carrying and releasing nitrogen oxide (NO) in a biological medium, their use for implementing a therapeutic treatment method or a diagnostic method applied to a human or animal body, and for making medicines useful for treating or preventing disorders affecting the human or animal cardiovascular, nervous, immune, renal or pulmonary system, specifically, an organometallic complex of nitrogen oxide, wherein the cationic part is of the formula (I) in which x=0 or 1; x′=2 or 3; y=0, 2 or 3; z=0 or 1; with the condition that, if y=0 (or z=0) then z=0 (or y=0; respectively); R is a group chosen from the group formed by: a hydrogen atom, —(CH2)2COOH and R1, R2, R3 and R4 are groups chosen from the group formed by: a hydrogen atom and alkyl groups comprising from 1 to 4 carbon atoms; and M2+ is a divalent cation Fe++ or Co++.

Abstract: Wurster's crown ligands comprise a macrocyclic ligand such as a crown ether in which a hetero atom is substituted with a 1,4-phenylenediamine group. The phenylenediamine group is covalently bound to the macrocyclic ligand by one or both of the amine nitrogens, the amine nitrogen thereby substituting for the hetero atom of the macrocyclic ligand. The resulting compounds are redox active. Methods of making and using the compounds are also disclosed.

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 process of synthesizing a carbapenem compound of formula 6: is disclosed using a compound of formula 4′: The intermediate compounds that are described herein are also included in the present invention.

Abstract: Texaphyrin/chemotherapeutic drug conjugates, optionally including a platinum(II) or platinum(IV) metal chelating site and/or complex, are useful for treating atheroma, tumors and other neoplastic tissue, neovascular-related diseases, as well as other conditions that are typically responsive to chemotherapy, radiation sensitization and photodynamic therapy.

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: Chelates of the compounds of formula I in which R is a hydrophilic group containing 3 or 4 successive phenyl rings and m is 1 or 2, with metal ions, for use in diagnostic imaging.

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: Compounds and methods of preparing compounds represented by structural formula (I): wherein X represents any suitable counter-anion; R1 and R2 independently represent hydrogen, C1-6 alkoxy or nitro; R3, R4, R5 and R6 each independently represents hydrogen, hydroxy, halo, C1-6 alkyl, C2-6 alkenyl or C1-6 alkoxy; and R7, R8, R9 and R10 each independently represents hydrogen, hydroxy, halo, C1-6 alkyl, C2-6 alkenyl or C1-6 alkoxy. Compounds represented by structural formula (I) are useful in treating or preventing free radical-associated diseases or conditions in mammals.

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: The invention relates to polyazacycloalkanes having 3, 4 or 5 nitrogen atoms, tri-, tetra- or penta-azamacrocyclic transition metal complexes and processes for the production of said polyazacycloalkanes. The object of the invention is to form polyazacycloalkanes able to trap metal cations and in particular U, Pu, Am, Ce, Eu, Al, Gd, Cr, Mn, Fe, Co, Ni, Cu, Zn, Ag, Cd, Sn, Au, Mg or Pb or complexes able to trap in particular oxygen in a gaseous mixture. The invention more particularly applies to the treatment of liquid effluents from nuclear power stations.

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: 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: Method for recovering oxygen from a medium containing O.sub.2 using polynitrogenated compounds that have five coordinating functions which are capable of binding a metal atom, particularly a cobalt atom. In the recovery method, oxygen is first absorbed by the metal complex and then desorbed from the complex and recovered in an appropriate vessel.

Abstract: The invention provides a novel composition and method for removing or reducing levels of recalcitrant constituents from an effluent, such as lignin chromophores, AOX species, such as chlorinated phenols, dioxins, dibenzofurans, biphenyls, and high molecular weight material produced in the pulp and paper bleaching operations which includes using a composition comprised of (a) an amount of a source of an oxidant effective for oxidizing and thereby reducing the levels of such constituents and (b) an oxidatively stable oxidant activator having the structure ##STR1## wherein Y.sub.1, Y.sub.3 and Y.sub.4 each represent a bridging group having zero, one, two or three carbon containing nodes for substitution, and Y.sub.2 is a bridging group having at least one carbon containing node for substitution, each said node containing a C(R), C(R.sub.1)(R.sub.2), or a C(R).sub.

Abstract: An improved synthesis for preparing a tetraamido-macrocyclic ligand, such as 5,6-Benzo-3,8,11,13-tetraoxo-2,2,9,9-tetramethyl-12,12-diethyl-1,4,7,10 -tetraazacyclotridecane, H.sub.4, in greatly improved yield and in a commercially viable manner, comprising the steps of dissolving a quantity of a 1,2-bis(2-aminoalkanamido)benzene in a solution comprised of ethyl acetate and methylene chloride to yield a first reaction solution; dissolving a quantity of a malonyl dihalide in an ethyl acetate solution to yield a second reaction solution; adding the first reaction solution and the second reaction solution to a reaction vessel containing a third reaction solution comprised of refluxing ethyl acetate solution and an acid scavenger to form a reaction mixture; and isolating a solid product comprised of the tetraamido-macrocycle directly from the reaction mixture by filtration.

Abstract: The invention relates to new porphyrin complex compounds, pharmaceutical agents that contain the latter, and the use of porphyrin complexes for the production of agents for photodynamic therapy and MRI diagnosis.

Abstract: Disclosed herein is a process for the polymerization of ethylene, norbornenes and styrenes, by contacting in solution a selected nickel compound and a selected compound which is or can coordinated to the nickel with the olefin(s). The polymers produced are useful for films and molding resins.

Abstract: A robust chelate complex is provided having the formula: ##STR1## wherein: M is a metal, preferably a transition metal; Z is an anionic donor atom, three of which are nitrogen, and the other is oxygen; L.sub.1 is a labile ligand;Ch.sub.1, Ch.sub.2 and Ch.sub.3 are oxidation resistant chelate groups which are the same or different and which form 5 or 6 membered rings with the metal, and Ch.sub.4 is a chelate group having the structure ##STR2## wherein R.sub.1 and R.sub.2 are the same or different and are preferably selected from the group consisting of hydrogen, halogen, methyl, and CF.sub.3 or when linked, a five or six membered ring cyclo substituent. The complex provides a stable, long-lived oxidation catalyst or catalyst activator.

Abstract: The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: ##STR1## wherein R, R', R.sub.1, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5, R'.sub.5, R.sub.6, R'.sub.6, R.sub.7, R'.sub.7, R.sub.8, R'.sub.8, R.sub.9, and R'.sub.9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.

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: 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 robust compound is provided having the formula: ##STR1## wherein Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are oxidation resistant groups which are the same or different and which form 5- or 6-membered rings with a metal, M, when bound to D. D is a metal complexing donor atom, O or N. Each X is a position for addition of a substituent and, when D is N, each position is (i) not occupied such that a double bond is formed between D and an atom adjacent to D, or (ii) is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, alkoxy, phenoxy, halogen, halogenated alkyl, halogenated aryl, halogenated alkenyl, halogenated alkynyl, perhaloalkyl, perhaloaryl, a substituted or unsubstituted cycloalkyl ring, a substituted or unsubstituted cycloalkenyl ring, a substituted or unsubstituted saturated heterocyclic ring, a substituted or unsubstituted unsaturated heterocyclic ring, and at least one X is hydrogen, and when D is O, the position is not occupied.

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: New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an .alpha. or .beta. amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the .alpha. or .beta.

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: A process for the preparation of complexes of macrocyclic chelants with paramagnetic metal trivalent ions of formula (XII) ##STR1## wherein R.sub.1, R.sub.2 and Me.sup.3+ are as described in the following, comprising: a) reaction of 1,4,7,10-tetraazacyclododecane with triethyl orthoformate to give 5H,9bH-2a,4a,7,9a-octahydrotetraazacycloocta[cd]pentalene; b) carboxymethylation reaction in water; c) hydrolysis reaction in basic conditions; d) alkylation according to known methods with an epoxide in water; e) complexation according to known methods carried out in water by addition of a paramagnetic metal salt; f) purification by diafiltration, final desalting of the aqueous solution on ion exchange resins and g) crystallization or recovery.

Abstract: A process for the preparation of complexes of macrocyclic chelants with paramagnetic metal trivalent ions of formula (XII) ##STR1## wherein R.sub.1, R.sub.2 and Me.sup.3+ are as described in the following, comprising: a) reaction of 1,4,7,10-tetraazacyclododecane with triethyl orthoformate to give 5H,9bH-2a,4a,7,9a-octahydrotetraazacycloocta[cd]pentalene; b) carboxymethylation reaction in water; c) hydrolysis reaction in basic conditions; d) alkylation according to known methods with an epoxide in water; e) complexation according to known methods carried out in water by addition of a paramagnetic metal salt; f) purification by diafiltration, final desalting of the aqueous solution on ion exchange resins and g) crystallization or recovery.

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: A process for the preparation of macromolecular chelants characterized by a high content in chelant groups per macromolecule.

Abstract: New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an .alpha. or .beta. amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the .alpha. or .beta.

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 the process for mono- and 1,7-bis-N-.beta.-hydroxyalkylation of cyclene, the corresponding mono- and 1,7-bis-N-.beta.-hydroxyalkyl-1,4,7,10-tetraazacyclododecane-Li-salt complexes as intermediate products in the process and the use of the N-(6-hydroxy-2,3-dimethyl-1,3-dioxepan-5-yl)-1,4,7,10-tetraazacyclododecan e-LiCl complex for the production of gadobutrol [Gd ocmplex of N-(1-hydroxy-methyl-2,3-dihydroxypropyl)-1,4,7-triscarboxymethyl-1,4,7,10- tetraazacyclododecane].

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 chiral ligand system for transition or main group metal catalysts is disclosed. These ligands can be readily synthesized using inexpensive amino acids and diamines as starting materials. Several different transition or main group metals have been inserted into the ligands. The ligands have been shown to have a tetradhedral distortion that may contribute to enhanced chiral transfer from the catalyst to the substrate in chemical modifications of olefins and other reactive substrates. These catalysts have been demonstrated to be effective in catalyzing epoxidation of a variety of substrates.

Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.

Abstract: This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring 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, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.

Abstract: Texaphyrins substituted with imidazda are provided.

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.