Abstract: The invention provides imidazo [1,2-a] pyridines of formula (1), wherein Y is selected from F, Cl, Br, I, OH, SH, NH2, CN and COOH; Z is selected from N(R3)C(O)R4 and C(O)NR3R4; R1, R2, R3, R4 can represent various radicals; m and n are independently 0, 1 or 2; and p is an integer from 1 to 4; radiolabelled derivatives and pharmaceutical compositions thereof. The compounds of the invention are useful for the diagnosis and treatment, including radiotherapy, of disorders that are characterized by an abnormal density of peripheral benzodiazepine receptors.

Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain. Intermediates to the compounds of the formula I are also claimed.

Abstract: The present invention is related to process for producing radioiodinate neuroreceptor agents with improves yields. In said process the trialkyltin group of the precursor of the neuroreceptor agent is replaced by radioiodine in the presence of an oxidation agent, preferably chloramine T in a pH adjusted by a buffering system comprising inorganic or organic acids and their salts. The end-products are subsequently separated from the by-products using chromatographic separation methods such as high performance liquid chromatography (HPLC), wherein the mobile solvent phase comprises a mixture of ethanol and water having a pH of 1-6. The improved yield are obtainable by preventing the formation of volatile radioactive by-products and by using a non-toxic solvent system in the chromatographic separation process, which simplifies the down stream processing of the end product.

Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: wherein RF is a fluorinated radical, X is a linear or branched alkylene, R1 is H or CH3, R2 is a radical having at least one OH group, R3 is a radical derived from an amino acid or a peptide, 1≦n≦50 and 0≦m≦200 with 0.2≦n/n+m≦1. These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.

Abstract: The 3&agr; isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a more rapid achievement of apparent equilibrium in the striatal-to-cerebellar ratio (compared to RTI-55) as the ratio peaks at about 30 min and is maintained for about 20 min thereafter. Such apparent equilibrium is useful in developing an approach to measuring the number of dopamine transporters present in tissues. Moreover, these results indicate that the utilization of 3&agr; isomers of a variety of 3&bgr;-(substituted phenyl)tropanes will result in greater selectivity for dopamine transporters and a more rapid of achievement of apparent equilibrium.

Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: 1

Abstract: Provided are compounds of the following formula: wherein R is C2-C6 mono- or multi-unsaturated hydrocarbon having one or more ethylene, acetylene or allene groups, A is 18 or 19, and X is H or halogen. The compounds of the invention bind to dopamine transporter with high affinity and selectivity and are thus useful as diagnostic and therapeutic agents for diseases associated with dopamine transporter dysfunction. The radiolabeled compounds are useful as imaging agents for visualizing the location and density of dopamine transporter by PET imaging.

Abstract: The nucleoside analog 2′-fluoro-5-methyl-1-&bgr;-D-arabinofuranosyluracil (FMAU) has been found to have an especially desirable combination of properties for use as an imaging agent, including in particular limited in vivo catabolism. Methods for the preparation of the [11C]-and [18F]-labeled FMAU and for the use of the labeled material are also provided.

Abstract: Methods of treating and imaging diseased tissue having the steps of administering a radiosensitizer agent proximate to or into the diseased tissue; and treating the diseased tissue with x-rays or other ionizing radiation so as to activate the radiosensitizer agent in the diseased tissue. Preferably, the radiosensitizer agent is a halogenated xanthene.

Abstract: The present invention concerns the use of a radioiodinated phenolic compound of the formula wherein: m and n are independently 0, 1, 2 or 3, X is a group that is negatively or positively charged at physiological pH, R, R1, R2 and R3 are independently hydrogen, C1-C4 alkyl, or a carboxyl group, and I* is 123I, 131I or 125I, and its pharmaceutically-acceptable salts. The compound is formulated and used in vivo in an animal in brachytherapy in an implantable catheter. In addition, due to the rapid renal clearance of these compounds, they may be used to study renal function. A process to prepare these compounds is also disclosed.

Abstract: A method for labeling &bgr;-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): with mammalian tissue.

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 instant invention utilizes the preferential uptake of iodine by mammary cells in general, and neoplastic mammary cells in particular to promote the concentration of radioactive iodine in malignant mammary cells. Radioactive iodine has utility in the instant invention as both a cancer therapeutic and a radioimaging dye. Iodine 125 and/or iodine 131 are administered in doses from 1 to 50 milliCurie per day. Subsequent doses may also be administered as clinically warranted. Administration of hormones prior to, or simultaneous with, the administration of the radio iodine is optionally utilized to stimulate iodine uptake in neoplastic mammary cells or to inhibit iodine uptake by the thyroid gland.

Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is O or S; n is 2, 3, 4 or 5; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R2 is hydrogen, C1-6alkyl, phenyl, phenylC1-6alkyl or phenylcarbonyl; R3 and R4 each independently are selected from hydrogen, halo, nitro, C1-6alkyl, C1-6alkyloxy, haloC1-6alkyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl; or R3 and R4 may also be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.

Abstract: Bifunctional aromatic compounds which are capable of linking metal ions to biologically useful molecules. The bifunctional compounds are characterized as having a hydrazine or hydrazide group and a protein reactive group. The hydrazine or hydrazide group may be protected as a lower alkyl hydrazone. Conjugates of the bifunctional compounds with macromolecules are also described and labelled macromolecules comprised of the conjugates and metal ions are provided. Additionally, a method is provided for forming a labelled macromolecule by reacting a conjugate with a metal species. The compounds and method of this invention are particularly useful in the fields of biology and medicine for imaging and/or therapy.

Abstract: Metalloporphyrin-metal complex conjugates are prepared by reacting a porphyrin-metal complex conjugate with a metal acetylacetoane in a solvent or solvent mixture at a temperature from room temperature to 150° C. in concentrations of 3-30% in the metalloporphyrin-metal complex conjugate.

Abstract: The present invention relates to tropane derivatives having particular use for the in vivo detection of dopamine transporters. These derivatives meet the formula in which R1 is I or Sn (R3)3, R2 is for example the methyl group, and X and Y are various substituents. The derivatives with X═CH3 and Y═H show strong specificity for the dopamine transporter compared with the serotonin transporter (74% inhibition when the transporter is previously saturated with GBR 12909).