Abstract: A process for polymerizing 1-butene, optionally with up to 30% by mol of ethylene, propylene or an alpha olefin of formula CH2?CHT wherein T is a C3-C10 alkyl group, in the presence of a catalyst system obtainable by contacting a metallocene compound of formula (I) Wherein M is an atom of a transition metal; X, is a hydrogen atom, a halogen atoms or a hydrocarbon group; R1, R2, R5, R6, R7, R8 and R9 are hydrogen atoms or hydrocarbon groups; with the proviso that at least one of R6 or R7 is a C1-C20 alkyl group; R3 and R4 are C1-C20 alkyl groups; and an alumoxane and/or a compound capable of forming an alkyl metallocene cation.

Abstract: The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.

Abstract: The invention relates to polyoxometalates represented by the formula (An)m+[R2(H2O)6X2W20O70]m? or solvates thereof, wherein A represents a cation, n is the number of the cations, m is the charge of the polyoxoanion, and X represents a heteroatom selected from SbIII, BiIII, AsIII, SeIV and TeIV, a process for their preparation and their use for the catalytic oxidation of organic molecules.

Abstract: The present invention incorporates weakly basic substituents (pKa about 8 or greater) such as pyrrolidine, piperidine, piperazine and azapane moieties in halogenated 2-nitromidazoles as a major improvement over prior art for the non-invasive detection of cellular hypoxia in normal and malignant tissues. The invention features the use of [18F] positron emission tomography, [19F] magnetic resonance spectroscopy, and [19F] magnetic resonance imaging. Improvements over prior art compounds are six-fold. 1) Salts of weakly basic reagents are highly water-soluble which facilitates administration. 2) Unreacted reagents are rapidly cleared from systemic circulation thereby decreasing background noise. 3) Reagents with weakly basic substituents are concentrated in tissue ˜3 fold above plasma levels thereby increasing binding intensity and enhancing signal detection.

Abstract: The present invention provides an improved, economical and environmentally benign process for metal complexes of acetylacetone having the general formula, M(acac)n wherein M is a metal cation selected from the group consisting of Fe, Co, Ni, Cu, Zn, Al, Ca, Mg, Mo, Ru, Re, U, Th, Ce, Na, K, Rb, Cs, V, Cr, and Mn etc., n is an integer which corresponds to the electrovalence of M, are obtained by reacting the corresponding metal hydroxide, metal hydrated oxide or metal oxide with a stoichiometric amount of acetylacetone and separating the product.

Abstract: A process for the production of an 18F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-SO2—O-TRACER (I) with 18F— to produce the labelled tracer of formula (II)

Abstract: A new class of heterocyclic metallocenes, a catalytic system containing them and a process for polymerizing addition polymerizable monomers using said catalytic system are disclosed; the heterocyclic metallocenes correspond to the formula (I): YjR?iZjjMeQkPl wherein Y is a coordinating group containing a six ? electron central radical directly coordinating Me, to which are associated one or more radicals containing at least one non-carbon atom selected from B, N, O, Al, Si, P, S, Ga, Ge, As, Se, In, Sn, Sb and Te; R? is a divalent bridge between the Y and Z groups; Z is a coordinating group, optionally being equal to Y; Me is a transition metal; Q is halogen or hydrocarbon substituents; P is a counterion; i is 0 or 1; j is 1–3; jj is 0–2; k is 1–3; and l is 0–2.

Abstract: Radiolabeled conjugates are disclosed which have a component that is effective to target tumor cells, which cells selectively take up and degrade the conjugate, thereby delivering to the tumor cell nucleus a radioisotope capable of being incorporated into the nuclear material, so as to produce a cytotoxic effect and/or to render the cell detectable by radioimaging.

Abstract: Novel coordination polymers, their pharmaceutical formulations, useful for treating atheroma, tumors and other neoplastic tissue, as well as other conditions that are responsive to the induction of targeted oxidative stress, are disclosed.

Abstract: The present invention is directed toward a tunable dielectric device comprising: a substrate and an endohedral fullerene encapsulating trimetallic nitride template compound disposed on the substrate. The endohedral fullerene encapsulating trimetallic nitride template compound has a dipole moment that is oriented when a voltage of less than about 5 volts is applied thereto causing a change in the orientation of the dipole moment of the compound. The physical dimension of the compound is essentially unchanged.

Abstract: A metal bis-triflimide compound having the formula: [Mx]n+[(N(SO2CF3)2)(nx?yz)](nx?yz)?[Ly]z? where M is a metal selected from the metals in groups 5 to 10, 12 and 14 to 16 and Cu, Au, Ca, Sr, Ba, Ra, Y, La, Ac, Hf, Rf, Ga, In, Tl, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Lu and the actinides; L is a negative or neutral ligand; n is 2,3,4,5,6,7 or 8; x is greater than or equal to 1 y is 0,1,2,3,4,5,6,7 or 8; and z is 0,1,2,3 or 4.

Abstract: Polydentate substituted pyrrole based chelants, metal complexes containing the same, olefin polymerization catalyst compositions, and polymerization processes using the same.

Abstract: The present invention relates to a process for preparing a metallocene, which comprises reacting a ligand starting compound with an adduct of the formula (I), M1XnDa ??(I) where M1 is a metal of group III, IV, V or VI of the Periodic Table of the Elements or an element of the lanthanide or actinide series, preferably titanium, zirconium or hafnium, particularly preferably zirconium, X are identical or different and are each halogen, C1–C10-alkoxy, C6–C10-aryloxy, C1–C10-alkylsulfonate such as mesylate, triflate, nonaflate, C6–C10-arylsulfonate such as tosylate, benzenesulfonate, C1–C10-alkylcarboxylate such as acetate, formate, oxalate or 1,3-dicarbonylate such as acetylacetonate or fluorinated 1,3-dicarbonylate, in particular chlorine, bromine, particularly preferably chlorine, n is an integer and is 2,3,4,5 or 6 and corresponds to the oxidation number of the metal M1, a is an integer or fraction and 0<a?4 and a is preferably in the range from 0.5 to 2.5 and is in particular 1, 1.

Abstract: Novel coordination polymers, their pharmaceutical formulations, useful for treating atheroma, tumors and other neoplastic tissue, as well as other conditions that are responsive to the induction of targeted oxidative stress, are disclosed.

Abstract: Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are disclosed.

Abstract: One aspect of the present invention relates to a method of purifying radiolabelled compounds comprising a) loading onto a fluorous polymer a radiolabelled compound precursor comprising a fluoroalkyl tin moiety; b) reacting the radiolabelled compound precursor with a radiolabel delivering compound to give a radiolabelled compound, wherein the fluoroalkyl tin moiety is replaced by a radiolabel; and c) eluting the radiolabelled compound from the fluorous polymer.

Abstract: The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.

Abstract: The invention concerns a ligand comprising (I) wherein n is an integer from 1 to 5 Y is CO2H or PO3H2T represents —X or -phenyl-X, wherein X represents NO2, NH2, NCS, NHCOCH2-Z, NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or NHCO(CH2)m-Q where Q is a 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, W is —(CH2)m- m is an integer from 1 to 10 Z is chloride, bromide or iodine.

Abstract: Compounds are described which exhibit an inhibitory action towards the enzyme aromatase and which comprise at least one detectable group. Such compounds are excellently suitable for medical diagnosis and/or for therapy, particularly for tumor diseases and above all for breast cancer.

Abstract: The invention provides, in a general sense, a new labeling strategy employing compounds that are are N2S2 chelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, COX-2, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.

Abstract: A metal bis-triflimide compound having the formula: [Mx]n+[(N(SO2CF3)2)(nx-yz)](nx-yz)−[Ly]z− where M is a metal selected from the metals in groups 5 to 10, 12 and 14 to 16 and Cu, Au, Ca, Sr, Ba, Ra, Y, La, Ac, Hf, Rf, Ga, In, Tl, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Lu and the actinides; L is a negative or neutral ligand; n is 2,3,4,5,6,7 or 8; x is greater than or equal to 1 y is 0,1,2,3,4,5,6,7 or 8; and z is 0,1,2,3 or 4.

Abstract: The present invention provides an improved, economical and environmentally benign process for metal complexes of acetylacetone having the general formula, M(acac)n wherein M is a metal cation selected from the group consisting of Fe, Co, Ni, Cu, Zn, Al, Ca, Mg, Mo, Ru, Re, U, Th, Ce, Na, K, Rb, Cs, V, Cr, and Mn etc., n is an integer which corresponds to the electrovalence of M, are obtained by reacting the corresponding metal hydroxide, metal hydrated oxide or metal oxide with a stoichiometric amount of acetylacetone and separating the product.

Abstract: The invention concerns olefin polymerization catalyst component comprising an organometallic compound of general formula I wherein: M is a transition metal of groups 3, 4-10, lanthanide or actinide of the periodic table of the elements; each R is independently a structural bridge rigidly connecting two ligands L1, L2 and L3 and is constituted by 1 to 4 chain atoms selected from carbon, silicon, germanium, oxygen, boron; m, n and o are 0 or 1, with the proviso that m+n+o is 2 or 3; L1 is a ligand of the cyclopentadienyl type or is isolobal to cyclopentadienyl, L2 is a ligand of the cyclopentadienyl type or is isolobal to cyclopentadienyl, or a monovalent anionic ligand selected from the group consisting of N, P, B when m+n=2, it is selected from the group consisting of NR1, PR1, BR1, O and S when m+n=1; L3 is a monovalent anionic ligand selected from the group consisting of N, P, B when n+o=2, it is selected from the group consisting of NR1, PR1

Abstract: The invention provides a complex comprising a) a compound formula I: 1

Abstract: The present invention concerns new compounds comprising a branched linker and their use for producing conjugates for applications in diagnostic or therapeutic methods.

Abstract: The disclosure provides pendant fatty acid compounds for use in diagnostic imaging, (particularly the cardiovascular system), as well as kits comprised of the same. The disclosure also provides for a method administering a imaging agent with a high specificity for the myocardium.

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

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: Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new-subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention.

Abstract: Described herein are novel indicator molecules of general formula (1): 1

Abstract: A composite metal polybasic salt containing a trivalent metal and magnesium as metal components and having a novel crystal structure, and a method of preparing the same. The invention further deals with a composite metal polybasic salt which has anion-exchanging property, which by itself is useful as an anion-exchanger, capable of introducing anions suited for the use upon anion-exchange, and finds a wide range of applications, and a method of preparing the same. The composite metal polybasic salt has a particular chemical composition and X-ray diffraction peaks, and further has a degree of orientation (Io) of not smaller than 1.5.

Abstract: The invention relates to novel radiotherapeutic formulations containing 224Ra and methods for their production. The invention discloses, in particular, radiotherapeutic formulations comprising at least one salt of the isotope 224Ra, which are characterized in that the content of other radionuclides, in particular, the respective content of certain longeval radionuclides does not exceed a specific numerical value in mBq/g. The invention also relates to a method for producing radiotherapeutic formulations of this type, which is characterized by the following steps: after at least one centrifugation of an aqueous suspension of the compound 228Th(OH)4 and optionally after the resuspension of the raw sediment obtained in said centrifugation, the precipitated 228Th(OH)4 sediment is separated. The supernatant solution of a 224Ra salt that has been obtained is subsequently subjected to sterile filtration and is then made up to the required dose.

Abstract: The present invention provides functionalized chelants and a method of treating cancerous cells with alpha particles comprising the step of administering a pharmacologically effective dose of an 225Ac conjugate comprising a functionalized chelant R is independently CHQCO2X; Q is independently hydrogen; C1-C4 alkyl or (C1-C2 alkyl) phenyl; X is independently hydrogen; benzyl or C1-C4 alkyl; Z1 is (CH2)nY where n is 1-10 and Y is an electrophilic or nucleophilic moiety and Z2 is R; or, alternatively, Z1 is hydrogen and Z2 is a peptide linker composed of 1-10 amino acids; said Y or said peptide linker covalently attached to an antibody or fragment thereof, or other biologic molecule; or a pharmaceutically acceptable salt thereof, complexed with 225Ac. These biologic molecule binds to cancerous cells and 225Ac or its daughters emit alpha particles into said cancerous cells effecting treatment.

Abstract: Inorganic ion exchange materials for the separation of 90Y from 90Sr include chabazite, clinoptilolite, potassium pharmacosiderite, sodium titanosilicate and sodium nonatitanate. These materials are suitable for making a 90Y generator that contains 90Sr immobilized on an ion exchange column of the materials. The materials have a very high selectivity for 90Sr, a very low selectivity for 90Y, good radiation and thermal stability, low toxicity, fast reaction kinetics, and can be readily and reproducibly synthesized. A method is thus provided for eluting 90Y from the ion exchange material with an eluant solution. The eluant solution is preferably aqueous, preferably has a pH greater than about 5, and preferably includes a chelating agent. Preferred chelating agents include gluconic acid, oxalic acid, iminodiacetic acid, nitrilotriacetic acid, citric acid, and combinations thereof.

Abstract: Actinium-225 complexes comprising functionalized polyazamacrocyclic chelant compounds are disclosed. Such complexes show improved stability and can be conjugated to a biological carrier.

Abstract: P-chiral bisphospholane ligands and methods for their preparation are described. Use of metal/P-chiral bisphospholane complexes to catalyze asymmetric transformation reactions to provide high enantiomeric excesses of formed compounds is also described.

Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

Abstract: The invention provides methods for diagnosing and treating amyloid-related conditions and compounds useful for the same. The invention provides for detecting, imaging, monitoring, diagnosing, and treating conditions characterized by the binding or aggregation of amyloid fibrils. More particularly, the invention relates to using quinolinehydrazone compounds for diagnosing and treating amyloidotic conditions and also as an antioxidant.

Abstract: This invention relates to a composition of matter comprising the catalyst compound comprising a transition metal complexed with a facially coordinating tridentate bisamide ligand. The invention is also directed to a catalyst system or a supported catalyst system comprising this compound and an activator and to a process for using the catalyst system or supported catalyst system in a process for polymerizing olefin(s).

Abstract: The present invention provides novel imaging agents for clinical diagnosis of injuries and diseases, in the form of a radionuclide in spatial proximity to a substantially pure stereoisomer of a fatty acid analog. The invention also provides methods for using the novel imaging agents, and kits containing one or more of the novel imaging agents of the invention.

Abstract: The present invention provides methods and compositions for imaging cell death in vivo, as well as methods and compositions for tumor radiotherapy.

Abstract: The present invention relates to a bi-specific antibody or antibody fragment having at least one arm that specifically binds a targeted tissue and at least one other arm that specifically binds a targetable construct. The targetable construct comprises a carrier portion which comprises or bears at least one epitope recognizable by at least one arm of said bi-specific antibody or antibody fragment. The targetable construct further comprises one or more therapeutic or diagnostic agents or enzymes. The invention provides constructs and methods for producing the bi-specific antibodies or antibody fragments, as well as methods for using them.

Abstract: There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the —PR2 containing biomolecules by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a —PR2 containing biomolecule.

Abstract: A class of metallocene compounds is disclosed having 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 1 to 3, being equal to the oxidation state of the metal M minus 2.

Abstract: The invention relates to (ethylene)-(propylene)-triaminepentaacetic acid derivatives that are substituted on both the ethylene bridge and the propylene bridge, as well as conjugates of these compounds with biomolecules. The compounds and conjugates are suitable as agents for NMR diagnosis and radiodiagnosis as well as for radiotherapy.

Abstract: A porphyrin ring-fusion polymer which consists of two or more Zn(II)-porphyrin rings fused in a single direction and in which any two porphyrin rings adjacent to each other are fused by three covalent bonds, that is, one meso-meso carbon bond (i.e., one bond between meso-position carbon atoms) and two &bgr;-&bgr; carbon bonds (i.e., two bonds between &bgr;-position carbon atoms adjacent to the meso-position carbon atoms); a process for preparing the porphyrin ring-fusion polymer regioselectively by conducing the fusion reaction in an aromatic hydrocarbon solvent in the presence of a quinoline and Lewis acid containing rare earth element under reflux; and fused-ring porphyrin compound obtained by subjecting the porphyrin ring-fusion polymer to demetallization or replacement of the Zn atoms by other metal atoms.

Abstract: The invention relates to targeting of diagnostic agents by use of lipid-based compositions. The invention is useful in the diagnosis of various disorders which are associated with or resulting from increased levels of extracellular PLA2 activity in the diseased tissue, e.g. cancer, infectious, and inflammatory conditions.

Abstract: N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

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%.