Abstract: A formulation and method for therapeutic treatment of in mammals using certain metals or particle-emitting radionuclides complexed with tetraazamacrocyclic ligands are described.

Abstract: Tumors expressing VPAC receptors can be imaged or treated with compounds comprising PACAP, or a biologically active PACAP fragment or analog.

Abstract: The present invention relates to a complex comprising one or more radioisotopes selected from the group consisting of 99mTc, 188Re and 186Re chelated to a glucose derivative having an intramolecular nitrogen or sulfur atom, which is very useful as tumor diagnostic agents. It also relates to a kit for the preparation thereof comprising the glucose derivative and a reducing agent.

Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.

Abstract: Catalyst precursor compounds having both (i) a polydentate ligand which comprises a cyclic moiety as well as a heteroatom and (ii) a protected hydride/hydrocarbyl ligand bonded to a metal atom, as well as olefin polymerization catalyst systems based thereupon, polymerization processes using such catalyst systems and polymers produced thereby.

Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.

Abstract: Actinium-225 (225Ac) complexes with functionalized chelants of the formula (I) wherein; each Q is independently hydrogen or ((CHR5)pCO2R; Q1 is hydrogen or (CHR5)wCO2R; each R independently is hydrogen, benzyl or C1-C4 alkyl; with the proviso that at least two of the sum of Q and Q1 must be other than hydrogen, each R5 independently is hydrogen; C1-C4 alkyl or (C1-C2 alkyl)phenyl; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon—carbon bond; n is 0 or 1; m is an integer from 0 to 10 inclusive; p is 1 or 2; r is 0 or 1; w is 0 or 1; with the proviso that n is only 1 when X and/or Y form an additional carbon to carbon bond, and the sum of r and w is 0 or 1; L is a linker/spacer group covalently bonded to, and replaces one hydrogen atom of one of the carbon atoms to which it is joined, said linker/spacer group being represented by the formula (1) wherein s is an integer of 0 or 1; t is an integer of 0 to 20 inclusive; R1 is an electrophilie or nu

Abstract: Novel therapeutic lipid constructs comprising a polymerized liposome, an anti-cell surface targeting agent, and a radiotherapeutic metal ion are disclosed.

Abstract: A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferative tissue.

Abstract: The invention concerns a ligand comprising wherein n is an integer from 1 to 5, X represents —NO2, —NH2, —NCS, —NHCOCH2-Z. NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or —NHCO(CH2)?m ?-Q where Q is an hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, Y is CO2H or PO3H2 W is —(CH2)m— m is an integer from 1 to 10. Z is chloride, bromide or iodine.

Abstract: 225Ac complexes comprising a functionalized polyazamacrocyclic chelant compound of the formula I hereinbelow: 1

Abstract: A method and apparatus are provided for automatically separating radionuclides using a chromatographic separation process. The method includes the steps of displaying a first flow diagram on a display depicting flow of the radionuclides through a first set of separation elements of the plurality of separation processing elements, but only during a first step of the chromatographic separation process and displaying a second flow diagram on the display depicting flow of the radionuclides through a second set of separation elements of the plurality of separation processing elements, but only during a second step of the chromatographic separation process.

Abstract: 1,4,7,10-Tetraazacyclodedecane butyltriols of general formula IA 1

Abstract: A metallocene compound having an indenyl ligand substituted by a heteroaromatic group, which is useful as an olefin polymerization catalyst. The metallocene compound has the following structure wherein M is a transition metal atom; each Ra is a monocyclic or polycyclic heteroaromatic group; each R1 is halogen, a hydrocarbon group of 1-20 carbons, a halogenated hydrocarbon group of 1-20 carbons, etc., or adjacent R1's may be joined together to form a ring of 6-8 carbons; p and q are each 1-7; n and l are each 0 or 1-6; and each X is halogen, a hydrocarbon group of 1-20 carbons, a halogenated hydrocarbon group of 1-20 carbons, etc.

Abstract: Single-site catalysts useful for polymerizing olefins are disclosed. The catalysts incorporate a Group 3 to 10 transition, lanthanide, or actinide metal and an anionic thiopyran dioxide ligand. Because a wide variety of thiopyran dioxides are easy to prepare from commercially available starting materials, the invention enables the preparation of a new family of single-site catalysts.

Abstract: The invention provides metallocene catalyst systems for the controlled polymerization of alkenes to a wide variety of polyolefins and olefin coplymers. Catalyst systems are provided that specifically produce isotactic, syndiotactic and steroblock polyolefins. The type of polymer produced can be controlled by varying the catalyst system, specifically by varying the ligand substituents. Such catalyst systems are particularly useful for the polymerization of polypropylene to give elastomeric polypropylenes. The invention also provides novel elastomeric polypropylene polymers characterized by dyad (m) tacticities of about 55% to about 65%, pentad (mmmm) tacticities of about 25% to about 35%, molecular weights (Mw)in the range of about 50,000 to about 2,000,000, and have mmrm+rrmr peak is less than about 5%.

Abstract: A method for the generation of ammonia from dinitrogen is provided including reacting a three coordinate, low oxidation state transition metal complex with dinitrogen under substantially atmospheric pressures to obtain a metal-nitrido complex, whereby the oxidation state of the metal complex increases, and reducing the metal of the metal nitrido complex in the presence of a hydrogen source, so as to obtain NH3. A novel metal complex is provided which is capable of cleaving small molecules which includes a metal selected from the group consisting of molybdenum, titanium, vanadium, niobium, tungsten, uranium and chromium. The compound may have the formula M(NR1R2)3 where M is a transition metal; R1 and R2 are independently selected from the group consisting of tertiary alkyls, phenyls and substituted phenyls. The compound permits cleavage of nitrogen-nitrogen triple bonds.

Abstract: Processes for the large scale production of tetrapyrrolic compounds useful as photosensitizers in photodynamic therapy, such as meso-formyl porphyrins, meso-acrylate porphyrins, purpurins and benzochlorins. In particular, tin ethyl etiopurpurin (SnET2) and the intermediates necessary for its production without chromatography are disclosed.

Abstract: Detectably labeled macrophage scavenger receptor antagonists useful for the diagnosis and monitoring of various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque, coronary artery disease, renal disease, thrombosis, transient ischemia due to clotting, stroke, myocardial infarction, organ transplant, organ failure and hypercholesterolemia.

Abstract: A class of metallocene compounds is disclosed having the general formula (I): wherein Y is a moiety of formula (II) wherein A, B and D, same or different from each other, are selected from an element of the groups 14 to 16 of the Periodic Table of the Elements (new IUPAC version), with the exclusion of nitrogen and oxygen; R1, R2, R3, R4 and R5 are hydrogen or hydrocarbon groups, Z is selected from a moiety of formula (II) as described above and from a moiety of formula (III): wherein R6, R7, R8 and R9, are hydrogen or hydrocarbon groups; L is a divalent bridging group; M is an atom of a transition metal selected from those belonging to group 3, 4, 5, 6 or to the lanthanide or actinide groups in the Periodic Table of the Elements (new IUPAC version), X, same or different, is hydrogen, a halogen, a R10, OR10, OSO2CF3, OCOR10, SR10, NR102 or PR102 group, wherein the substituents R10 are hydrogen or alkyl groups; p is an integer of from 0 to 3, being equal to

Abstract: A new process, particularly simple, convenient and practical, for the direct synthesis of organometallic compounds of formula(I): (A)(ZR1m)n(A′)MLpL′q  (I) wherein (ZR1m)n is a divalent group bridging A and A′; A and A′ re independently —O—, —S—, or —N(R2)—, wherein R2 is hydrogen, alkyl, cycloalkyl, aryl, alkylaryl or arylalkyl; M is a transition metal belonging to group 3, 4, 5, 6 or to the lanthanide or actinide groups; L is a monoanionic sigma ligand, such as alkyl, cycloalkyl, aryl, alkylaryl or arylalkyl, optionally containing Si or Ge; L′ is halogen or —OR3, R3 being an hydrocarbon radical; m is 0, 1 or 2; n is 1-8; p is 1-3; q is 0-2. Said process comprises reacting the ligand (H—A)(ZR1m)n(A′—H) with about 1 molar equivalent of ML′s in the presence of about (2+p) molar equivalents of LjB or LMgL′, wherein B is an alkaline or alkaline-earth metal, s ranges from 3 to 6, and j is 1 or 2.

Abstract: &pgr;-complex compounds and in particular metallocene compounds of formula (Ia)(Ib), in which &pgr;I and &pgr;II represent &pgr;-systems, D designates a donor atom and A designates an acceptor atom, D and A being linked by a reversible coordinative bond such that the donor group assumes a positive (partial) charge and the acceptor group assumes a negative (partial) charge, at least one of D and A being part of the associated &pgr;-system in each case, M stands for a transition metal of the 3rd, 4th, 5th or 6th subgroup of the (Mendelian) periodic system of elements, X designates an anion equivalent and n designates the number zero, one, two three or four depending on the charges of M and those of &pgr;I and &pgr;II, are novel and can be used as catalysts for the (co)polymerization of olefins, i-olefins, alkines and/or diolefins or for ring-opening polyaddition.

Abstract: The present invention relates to the field of site directed therapy. More specifically the invention relates to site directed radio therapy, and provides a method for production of radioconjugates and an apparatus for radioimmunotherapy. The method, conjugates and apparatus can be practicalized without the need for radioactive shielding and/or airtight facilities. Without these restrictions the invention provides a simple and efficient means of therapy at the bed-side of the patient.

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: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.

Abstract: A family of trimetallic nitride endohedral metallofullerenes and their preparation are described. The trimetallic nitride endohedral metallofullerenes have the general formula A3-nXn@Cm where n ranges from 0 to 3, A and X may be trivalent metals and may be either rare earth metal or group IIIB metals, and m is between about 60 and about 200. Further, the A3-nXn@C68, A3-nXn@C78, A3-nXn@C80 families of endohedral fullerenes are described. The trimetallic nitride endohedral metallofullerenes are produced by charging a reactor with a cored graphite rod that has been filled with a metal oxide graphite mixture. The metal oxides correspond to the metals for A and X. The graphite rod is arc discharged in a helium and nitrogen atmosphere to produce the desired trimetallic nitride endohedral metallofullerenes.

Abstract: In binuclear metal hydride complexes of the formuula (I) the substituents and indices have the following meanings: M is scandium, yttrium, lanthanum or a lanthanide metal, R is hydrogen, halogen, C1-C20-alkyl, C3-C1-cycloalkyl, C6-C15-aryl or C3-C30-organosilyl, where two adjacent radicals R can also form a saturated or unsaturated, cyclic or heterocyclic group having from 4 to 18 carbon atoms, Z is —SiR′2—, —CR′2—, —GeR′2—, —SnR′2—, —BR′— or —O—, R′ is C1-C20-alkyl, C3-C10-cycloalkyl, C6-C15-aryl or alkylaryl having from 1 to 10 carbon atoms in the alkyl part and from 6 to 10 carbon atoms in the aryl part, m is 1 or 2, X is —O—, —S—, —NR″—, —PR″—, —OR″, —SR″, —NR″2 or —PR″2, R″ is hydrogen, C1-C20-alkyl, C3-C10-cycloalkyl, C6-C15-aryl, alkylaryl having from 1 to 10

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

Abstract: Chiral metallocenes are prepared by reacting a salt of an asymmetric bis(cyclopentadienyl)-moiety-containing ligand with a tertiary heteroaromiatic amine adduct of a transition, lanthanide, or actinide metal halide in an organic solvent or diluent so as to produce said chiral metallocene.

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: Pharmaceuticals and Apparatus used in combination for diagnosis and tissue necrosis applicable to provide effective and selective therapy using the Mossbauer absorption phenomenon. Selected pharmaceutical compounds containing a radiation absorber isotope are administered to a tissue and excited by a radiation source which provides energy at the corresponding resonant Mossbauer absorption frequency of isotope containing pharmaceutical, where excitation effects nuclear transitions to cause highly selective energy absorption in the selected target tissue. For diagnostic purposes, de-excitation fluorescence of the isotope is monitored. For therapeutic purposes, the energy is converted to particle radiation by the isotope at the target tissue by internal conversion followed by an Auger electron cascade which results in radiolysis of DNA resulting in lethal double strand breaks in the DNA molecules of the target tissue.

Abstract: A new process is disclosed, particularly simple, convenient and practical, for the direct synthesis of metallocenes of formula (I): (CP)(ZR1m)n(A)rMLpL′q wherein (ZR1m)n is a divalent group bridging Cp and A; Cp is a substituted or unsubstituted cyclopentadieryl group; A is —O—, —S—, —N(R2)—, wherein R2 is hydrogen, alkyl, cycloalkyl aryl, alkylaryl or arylalkyl, or A has the same meaning of Cp; M is a transition metal belonging to group 3, 4, 5, 6 or to the lanthanide or actinide groups; L is a monoanionic sigma ligand, such as alkyl, cycloalkyl, aryl, alkylaryl or arylalkyl, optionally containing Si or Ge; L′ is halogen or —OR5, R5 being a hydrocarbon radical; m is 1 or 2; n is 0-4; r is 0 or 1; p is 1-3; q is 0-2.

Abstract: A method for separating a desired metal or metalloi from impurities using a supercritical extraction process based on solubility differences between the components, as well as the ability to vary the solvent power of the supercritical fluid, is described. The use of adduct-forming agents, such as phosphorous-containing ligands, to separate metal or metalloid chelates in such processes is further disclosed. In preferred embodiments, the extraction solvent is supercritical carbon dioxide and the chelating agent is selected from the group consisting of &bgr;-diketones; phosphine oxides, such as trialkylphosphine oxides, triarylphosphine oxides and alkylarylphosphine oxides; phosphinic acids; carboxylic acids; phosphates, such as trialkylphosphates, triarylphosphates and alkylarylphosphates; crown ethers; dithiocarbamates; phosphine sulfides; phosphorothioic acids; thiophosphinic acids; halogenated analogs of these chelating agents; and mixtures of these chelating agents.

Abstract: Salts of (polyfluoroaryl)fluoroanions of aluminum, gallium, and indium are described. The (polyfluoroaryl)fluoroanions have the formula [ER'R"R'"F].sup..crclbar. wherein E is aluminum, gallium, or indium, wherein F is fluorine, and wherein R', R", and R'" is each a fluorinated phenyl, fluorinated biphenyl, or fluorinated polycyclic group.

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: Novel metallocene compounds are provided which are useful as polymerization catalysts, particularly in the polymerization of addition polymerizable monomers such as olefinic or vinyl monomers. Preferred polymer compositions prepared using the novel catalysts are bimodal or multimodal in nature, typically having a bimodal or multimodal molecular weight distribution. The metallocenes are binuclear or multinuclear, and contain two or more chemically distinct active sites. Methods for synthesizing the novel catalysts are also provided, as are methods for using the novel compounds as homogeneous or heterogeneous polymerization catalysts.

Abstract: The present invention has identified compounds with extended aromatic chromophores that bind the G-quadruplex formed by the folding of single-stranded human telomeric DNA. These compounds have been shown to be effective telomerase inhibitors and are contemplated to be useful in developing cancer treatments. A model of cationic porphyrin interaction with quadruplex DNA by intercalation has been established and in combination with structure activity relations has provided novel porphyrin compounds that exhibit discrimination between binding duplex and quadruplex DNA and show improved activity against telomerase.

Abstract: The invention pertains to compounds for binding lanthanide ions and actinide ions. The invention further pertains to compounds for binding radionuclides, and to methods of making radionuclide complexes. Also, the invention pertains to methods of extracting radionuclides. Additionally, the invention pertains to methods of delivering radionuclides to target locations. In one aspect, the invention includes a compound comprising: a) a calix[n]arene group, wherein n is an integer greater than 3, the calix[n]arene group comprising an upper rim and a lower rim; b) at least one ionizable group attached to the lower rim; and c) an ion selected from the group consisting of lanthanide and actinide elements bound to the ionizable group.

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: A method for the generation of ammonia from dinitrogen is provided including reacting a three coordinate, low oxidation state transition metal complex with dinitrogen under substantially atmospheric pressures to obtain a metal-nitrido complex, whereby the oxidation state of the metal complex increases, and reducing the metal of the metal nitrido complex in the presence of a hydrogen source, so as to obtain NH.sub.3. A novel metal complex is provided which is capable of cleaving small molecules which includes a metal selected from the group consisting of molybdenum, titanium, vanadium, niobium, tungsten, uranium and chromium. The compound may have the formula M(NR.sub.1 R.sub.2).sub.3 where M is a transition metal; R.sub.1 and R.sub.2 are independently selected from the group consisting of tertiary alkyls, phenyls and substituted phenyls. The compound permits cleavage of nitrogen--nitrogen triple bonds.

Abstract: The present invention provides a radiation-protecting agent which protects the active ingredient of radiopharmaceuticals against the radiolysis caused by a reaction of the active ingredient with water radicals formed by radiolysis of water, without decomposing the reactive active ingredient such as readily reducible active ingredient. The radiation-protecting agent of the present invention is characterized by comprising an organic compound usable in medical drugs and having high physiological acceptability and protecting the radiolabeled active ingredient of radiopharmaceuticals against the action of radiation. The reaction rate constant of said organic compound with OH radical, H radical or hydrated electron must be in the range of from 1.times.10.sup.8 to 5.times.10.sup.10 M.sup.-1 s.sup.-1, and when added to radiopharmaceuticals, molar concentration of the organic compound must be at least 50 times as high as molar concentration of the active ingredient.

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: The present invention is directed to methods for synthesizing water soluble hydroxy-substituted texaphyrins retaining lipophilicity. The synthesis comprises condensing a diformyltripyrrole with an ortho-phenylenediamine to give a nonaromatic texaphyrin having at least one hydroxy substituent, and oxidizing the condensation product to form an aromatic texaphyrin metal complex having at least one hydroxy substituent. These expanded porphyrin-like macrocycles may be used for magnetic resonance imaging and for photodynamic therapy in the treatment of atheroma and tumors.

Abstract: Catalyst component for the polymerization of alpha-olefins of general formula (I) ##STR1## wherein: M is a transition metal of groups 3, 4-10, lanthanide or actinide of the periodic table of the elements; A is a ring with delocalized .pi. electrons, L is a neutral Lewis base; m is an integer whose value can be: 0 or 1; E is selected from the group comprising: BR.sup.II, CR.sup.II.sub.2, SiR.sup.II.sub.2, GeR.sup.II.sub.2 ; Hal is selected from the group comprising iodine, bromine or chlorine; R.sup.III has the same meaning of R.sup.II ; Si is a silicon atom; D is selected from the group comprising: O, S, NR.sup.IV, PR.sup.IV, OR.sup.IV, SR.sup.IV, NR.sup.IV.sub.2, PR.sup.IV.sub.2 ; each X group equal to or different from each other is selected from the group comprising hydrogen, halide, alkyl, cycloalkyl, aryl, alkenyl, arylallyl, arylalkenyl or alkylaryl with 1 to 20 carbon atoms, n is a number whose value can be: 0, 1, 2 or 3, in order to full the remaining valences of metal M.

Abstract: Texaphyrins substituted with imidazda are provided.

Abstract: Novel metallocene compounds are provided which are useful as polymerization catalysts, particularly in the polymerization of addition polymerizable monomers such as olefinic or vinyl monomers. Preferred polymer compositions prepared using the novel catalysts are bimodal or multimodal in nature, typically having a bimodal or multimodal molecular weight distribution. The metallocenes are binuclear or multinuclear, and contain two or more chemically distinct active sites. Methods for synthesizing the novel catalysts are also provided, as are methods for using the novel compounds as homogeneous or heterogeneous polymerization catalysts.

Abstract: A method has been developed which utilizes a metal-2,4-dicarbonyl complex as an organic solvent soluble metal ion source in the metallation of polyazamacrocycles including porphyrins, expanded porphyrins and porphyrinoid compounds. Use of a metal ion source which is soluble in the metallation reaction medium produces significantly higher yields of a measurably purer product than is achieved using an insoluble or only sparingly soluble metal salt as in the prior art. Additionally, because the metallation can be performed in relatively concentrated mixtures, the reaction times are dramatically shorter and the amount of waste produced is less than when simple metal salts serve as the metal ion source. Further, use of the soluble metal-2,4-dicarbonyl complex simplifies the purification protocol required for the metallated expanded porphyrin.

Abstract: A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises a functionalized hydroxyalkyl phosphine ligand and a metal combined with the ligand.

Abstract: A cationic metallocene complex with trisperfluorobiphenyl borate for use as a polymerization catalyst.

Abstract: A trityl perfluorophenyl alumninate such as tris(2,2',2"-nonafluorobiphenyl) fluoroaluminate (PBA.sup.-) and its role as a cocatalyst in metallocene-mediated olefin polymerization is disclosed.