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 embodiment of the invention is a composition that comprises a radioactive [18F], [123I], [125I], or [131I]-N-radiohaloaryl-alkylcarboxamide molecule. The composition binds to the transient receptor potential-M8 (TRP-M8) receptor of cells. The TRP-M8 receptor is selectively expressed in sensory neurons and in malignant tissues such as prostate cancer cells. The [18F], [123I], [125I], or [131I]-N-radiohaloaryl-alkylcarboxamide ligand may be used for radioreceptor binding studies, for diagnostic studies, and for radiotherapy of cancerous tissues. Affinity of the [125I] or [131I]-N-radiohaloaryl-alkylcarboxamide ligand for the TRP-M8 receptor confers selectivity and specificity in delivering lethal radiation to the diseased cells.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: The invention relates to compounds of formula (I); wherein R1 and R2 independently selected from C1-6 alkyl; P1, P2, P3, and P4 are each independently hydrogen or a protecting group; and their use in the preparation of 18F-labelled 6-L-fluorodopa

Abstract: The invention provides a series of lipophilic phosphonium cations (PhCs) labeled with 18F for non-invasive assessment of ??m, lipophilic ammonium cation analogs of the PhCs, and methods of using same for imaging and detection of mitochondrial-related pathologies in patients using PET or SPECT.

Abstract: The invention provides imaging agents comprising a label in association with a plaque specific targeting molecule. Methods for using the imaging agents to diagnose or monitor plaque formation and growth and kits containing the cardiovascular agents or components suitable for production of the imaging agents are also provided.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.

Abstract: Tropane derivatives having a high binding affinity and selectivity for dopamine transporters bear, on the tropane backbone either a carboxylic ester or isoxazole moiety, as well as a substituted phenyl moiety. The compounds have utility both as pharmaceutical and as imaging agents, when one or more atoms are radioactive.

Abstract: New intracorporeal radiodense medicaments and certain medical uses and methods for use of such high energy phototherapeutic medicaments for treatment of human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. The halogenated xanthenes constitute a family of potent radiosensitizers that become photoactivated upon irradiation of the treatment site with ionizing radiation.

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: The present invention covers halogenated derivatives of boronated phorphyrins containing multiple carborane cages having the formula which selectively accumulate in neoplastic tissue within the irradiation volume and thus can be used in cancer therapies including, but not limited to, boron neutron-capture therapy and photodynamic therapy. The present invention also covers methods for using these halogenated derivatives of boronated porphyrins in tumor imaging and cancer treatment.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The present invention is directed to radiolabeled neuropeptide Y Y5 receptor antagonists which are useful for the labeling and diagnostic imaging of neuropeptide Y Y5 receptors in mammals.

Abstract: This relates to partially acetalized polyvinyl alcohol embolization particles suitable for implanting in the human body, to compositions containing those particles, and to methods of making and using them.

Abstract: A method of using radiolabelled and/or radiopharmaceutical small molecule inhibitors of beta-amyloid peptide production for the diagnosis of neurological and other disorders involving APP processing and beta-amyloid production. Radiolabelled small molecule inhibitors identified by the methods of the present invention would be useful in the diagnosis of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A? peptides.

Abstract: This invention is directed to the use of radiopharmaceuticals in diagnosing Alzheimer's disease. In particular the radiopharmaceuticals of the invention are able to pass through the blood-brain barrier and bind to the CCR1 receptor present in brain tissue of patients having Alzheimer's disease.

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 series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes and 4-haloethenylphenyl tropane families are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter protein with high affinity and selectivity. The invention provides methods of synthesis which incorporate radioisotopic halogens at a last step which permit high radiochemical yield and maximum usable product life. The radiolabeled compounds of the invention are useful as imaging agents for visualizing the location and density of serotonin transporter by PET and SPECT imaging.

Abstract: Compounds of formula (I) and (II): wherein groups R1, R2, RE, PG1 and PG2 have the definitions provided in the specification, methods of manufacture and methods of use.

Abstract: Use of pregnancy-associated plasma protein-A as a marker for inflammatory conditions, and in particular, for acute coronary syndromes is described.

Abstract: The present invention relates to a new method for radiolabeling chemical compounds. The new method attains the goals of simplicity, high radiochemical yields, speed, versatility, and automation. An HPLC injection loop on an HPLC injection valve is loaded with a solution of precursor and the radiolabeling reagent is passed through the loop. The contents of the loop are then quantitatively injected onto the HPLC column for purification. Radiochemical yields are equal to or superior to conventional solution methods in all cases, even though no heat need be applied. Since no vials, transfer lines, cooling, heating, or sealing valves are required, no transfer losses occur, yields are high, and clean-up is minimal. This “loop method” is ideal for the preparation of radiolabeled compounds, in particular those prepared from [11C]-iodomethane.

Abstract: Compounds of formula (I) where: X1 is OH or SH or NH2 or —L-Z; X2 and X3 are the same or different and each is H, C1-4 alkyl, benzyl a protecting group or —L-Z, X4 is H or C1-4 alkyl, L is a linker comprising a chain of 0-10 atoms, Z is a group comprising a detectable moiety which comprise at least one detectable moiety are useful in the diagnosis and prognosis and radiotherapy of metastatic bone disease.

Abstract: The present invention relates to a receptor binding conjugate which consists of an antibody, a radionuclide and folate or a folate derivative, wherein or not the conjugate possesses dual binding ability. The present invention also relates to a method and a kit to prepare, as well as a method to use, such conjugates. Furthermore, the use of a conjugate according to the present invention to prepare a pharmaceutical solution is disclosed.

Abstract: Use of pregnancy-associated plasma protein-A as a marker for inflammatory conditions, and in particular, for acute coronary syndromes is described.

Abstract: The present invention relates to nanogel networks having at least one cross-linked polyionic polymer fragment and at least one nonionic water-soluble polymer fragment, and compositions thereof, having at least one suitable biological agent.

Abstract: A compound having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R3 is H or OH; wherein R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety. Optically pure enantiomers and salts of the compound are also described. Also, the synthesis of the compound, and uses of the compound, such as in a method for detecting the localization of, or identifying, receptors, enzymes or other targets, whether in a cell or in a subject.

Abstract: The present invention features biarsenical molecules. Target sequences that specifically react with the biarsenical molecules are also included. The present invention also features kits that include biarsenical molecules and target sequences. Tetraarsenical molecules are also featured in the invention.

Abstract: Detectably-labeled compounds of formula (I) wherein A,B,C,D,E,F,R,X,Y and Z have any of the meanings given in the specification, and their pharmaceutically acceptable salts, are useful in competitive assays to assay for the presence of 2 receptors. Also disclosed are pharmaceutical compositions containing such a compound of formula (I), methods for their use and intermediates useful for preparing such compounds of formula (I).

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 novel radioligands and test methods using those radioligands in screening compounds.

Abstract: The present invention relates to 8-azabicyclo[3.2.1]oct-2-ene derivatives in their labelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).

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: An apparatus and method are provided for handling a solution. The apparatus comprises a housing and a vial assembly positioned within an enclosure of the housing. The vial assembly maintains at least one vial within the enclosure of the housing. A valve manifold extends within the enclosure of the housing for connection to the vial. A rotation mechanism, also extending within the enclosure of the housing, is operatively connected to the vial assembly for rotating the vial assembly.

Abstract: The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

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: Iodinated neuroprobes for mapping monoamine reuptake sites in the brain, and particularly iodinated neuroprobes that can also serve as radiotracers for use in single-photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging of such reuptake sites, are disclosed. Precursors of radiolabeled iodinated neuroprobes, both with and without a radiotracer atom, and kits for preparing the radiolabeled iodinated neuroprobes are also disclosed.

Abstract: The invention provides a composition of matter of the formula (I): V—L—R where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body, with the provisos that where V is angiotensin or a peptidic angiotensin derivative or analog then V—L—R is other than a non-metal radionuclide substituted peptide (e.g. 125I substituted angiotensin II) and L—V is other than simply a peptide with a chelating agent amide bonded to a side chain thereof. This composition of matter may be used to image cardiovascular diseases and disorders.

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 present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); wherein R1 represents optionally fluorinated lower alkyl; R2 represents lower alkyl; and R3 represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit &ggr;-rays at an appropriate energy level.

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: 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: The present invention provides novel agents for specifically targeting and detecting or treating focal sites of infection or inflammation in a subject.

Abstract: According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in the preparation of the radiolabelled haloaromatic are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.

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: Process for the preparation of radiohalogenated radiopharmaceuticals by an electrophillic substitution, preferably halogenodestannylation reactions, by the reaction of an organometallic substituted precursor, preferably a trialkyl tin substituted precursor, with a radioactive halogen, preferably a radioactive iodine, astatine or bromine composition, in the presence of a catalytically effective amount of an anion selected from the group consisting of bromide, chloride and nitrite anion in an acid medium with an oxidizing agent.

Abstract: The present invention relates to a radiolabeled non-steroidal compound having the formula: 1

Abstract: Ligands for nAChRs are provided based on various derivatives of methyllycaconitine (MLA) such as radiolabeled MLA, and MLA containing a fluorimetric marker group and their use in imaging for detection of Alzheimer's and other CNS diseases, and combinatorial assays for detection of compounds having affinity for nAChRs, as well as injectable compositions containing the same and kits for performing the imaging studies.

Abstract: A series of compounds in the 4-fluoroalkyl-3-halophenyl nortropanes family are described as diagnostic and therapeutic agents for diseases associated with serotonin transporter dysfunction. These compounds bind to serotonin transporter protein with high affinity and selectivity. The invention provides methods of synthesis which incorporate radioisotopic halogens at a last step which permit high radiochemical yield and maximum usable product life. The radiolabeled compounds of the invention are useful as imaging agents for visualizing the location and density of serotonin transporter by PET and SPECT imaging.

Abstract: The present invention provides improved radioiodinated phospholipid ether analogs which demonstrate significant tumor avidity and longer plasma half-life than shorter-chain analogs. The radioiodinated phospholipid ether analogs of the present invention provide superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.