Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.

Abstract: The present invention relates to improved chelator conjugates with biological targeting molecules, suitable for forming metal complexes with radiometals. The radiometal complexes, especially with the radiometal 99mTc, are useful as radiopharmaceuticals.

Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.

Abstract: Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.

Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Abstract: The present invention is directed to novel radiopharmaceuticals, which can be used to image myocardium. In addition, the present invention is directed to methods for risk stratification of patients who have suffered at least one myocardial infarction.

Abstract: Compositions for imaging pancreatic beta cells comprise chelator-antidiabetic agent conjugates and optionally chelated metals.

Abstract: A peptide-chelate conjugate with affinity for the ST receptor is disclosed, wherein the chelate is tetradentate. The peptide-chelate conjugate of the invention may be labelled with a radiometal to provide a metal complex. A radiopharmaceutical composition comprising the metal complex is provided. which is suitable for the diagnostic imaging of colorectal cancer. Also provided for in the invention is a kit for the preparation of the radiopharmaceutical preparation.

Abstract: The present invention relates to a compound for use as a chelator in the radioactive labeling of biomolecules with metal tricarbonyl complexes, which compound has the general Formula (I) wherein M is a monovalent cation, such as Li, Na, K, Tl, Rb, Cs or an alkyl ammonium; R1 is H, alkyl, aryl or a biomolecule; R2 is H or a pendant arm, said pendant arm optionally comprises a biomolecule, with the proviso that when R1 is H, R2 is not H or COOH, and when R1 is alkyl or aryl, R2 is not H.

Abstract: The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of ?-aminoisobutyric acid (AIB) analogs namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. In addition the compounds can be labeled with technetium and rhenium isotopes using known chelation complexes. The amino acid compounds disclosed herein have a high specificity for target sites when administered to a subject in vivo. The labeled amino acid compounds are useful as imaging agents in detecting and/or monitoring tumors in a subject by Positron Emission Tomography (PET) and Single Photon Emission Computer Tomography (SPECT).

Abstract: Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.

Abstract: 99mTc-labeled triphenylphosphonium contrasting agents that target the mitochondria and are useful for early detection of breast tumors using scintimammographic imaging. 99mTc-Mito10-MAG3 possesses advantageous radiopharmaceutical properties. The uptake in the myocardium is reduced by one to two orders of magnitude compared to 99mTc-MIBI. 99mTc-Mito10-MAG3 exhibits fast blood clearance, with a blood half-life of less than 2 minutes in rats. A diminished myocardial uptake combined with a prompt reduction of cardiovascular blood pool signal to facilitate improved signal-to-background ratios.

Abstract: The present invention provides novel tropane compounds and methods for their use.

Abstract: An object of the present invention is to provide a composition for effectively labeling ECD with 99mTc within a short period of time. The composition for producing [N,N?-ethylenedi-L-cysteinate(3-)]oxotechnetium(99mTc) diethyl ester is characterized by containing N,N?-(1,2-ethylene)bis-L-cysteine diethyl ester or a salt thereof, a reducing agent, and an acidic substance or a salt thereof.

Abstract: Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided.

Abstract: A complex, its stereoisomer or pharmaceutically acceptable salt has the formula I, where: wherein: W is a group that is A, B, or C: R1 is hydrogen, alkyl or alkoxy; R2 is a bond, hydrogen or alkyl R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl; X is a bond, C?O, O?C—O, or CH2; Y is a bond, CH2, or O; m is an integer ranging from 1 to 6; n is an integer ranging from 0 to 6; Metal represents a metallic moiety comprising a radionuclide; and Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.

Abstract: New chelating agents as well as their tricarbonyl complexes with technetium and rhenium and the use of these compounds in radiodiagnosis and radiotherapy are described. As a peculiarity of this invention, synthesis and coupling of the chelating systems to (bio)molecules is performed simultaneously. The new chelating agents are coupled to substances that accumulate in the diseased/targeted tissue.

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: A compound useful for in vivo imaging of organs and tumors is provided of formula: wherein is a cobalamin, is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1-3.

Abstract: One aspect of the invention relates to complexes of technetium (Tc) and rhenium (Re) with various heteroaromatic ligands, e.g., quinolinyl and isoquinolinyl ligands, and their use in fluorescence and radioimaging for a variety of clinical diagnostic applications, as well as radiopharmaceuticals for therapeutic applications. Another aspect of the invention relates to quinolinyl and isoquinolinyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium and rhenium complexes are also described. Another aspect of the invention relates to quinolinyl and isoquinolinyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine 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 relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.

Abstract: A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a phamaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted —CH2CH2CON(CH2CON(CH2COOH)2)2; or —N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.

Abstract: The invention relates to a conjugate PT comprising (a) a peptide P and (b) a targeting moiety T; wherein the peptide P contains from 4 to 20 amino acid residues with optionally a single thiol moiety at the C- or N-terminus replacing one of these amino acid residues, and including a complexing amino acid sequence comprising (iv) a tridentate or tetradentate planar chelator containing a ligand backbone defined by a perimeter containing a single sulfur donor atom, two or three non-sulfur donor atoms, and intervening atoms between the donor atoms; and (v) a stabilizing sidechain comprising a further donor atom, the further donor atom being covalently linked to the ligand backbone of the planar chelator through two or three intervening atoms, provided that said further donor atom is neither the nitrogen nor the oxgen atom of a peptide bond and if said further donor atom is part of a heterocyclic ring, no more than one of the intervening atoms can be part of that ring; and a radioactive metal complexed to t

Abstract: One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Abstract: Disclosed are compositions and methods related to clot binding compounds. The disclosed targeting is useful for treatment of cancer and other diseases and disorders.

Abstract: Some embodiments of the present invention may be said to be directed to metal complexes of Formula I, wherein at least one of X1, X2, X3, R1, R2, R3, R4 and R5 is what may be characterized as an antenna capable of providing (e.g., absorbing and/or emitting) an appropriate electromagnetic signal. Some embodiments of the present invention are directed to ligands corresponding to metal complexes of Formula I. Some embodiments of the invention are directed to methods of determining renal function using at least one metal complex of Formula I.

Abstract: A metal sulfide nanocrystal manufactured by a method of reacting a metal precursor and an alkyl thiol in a solvent, wherein the alkyl thiol reacts with the metal precursor to form the metal sulfide nanocrystals, wherein the alkyl thiol is present on the surface of the metal sulfide nanocrystal, wherein the alkyl thiol is bonded to the sulfur crystal lattice. A metal sulfide nanocrystal manufactured with a core-shell structure by a method of reacting a metal precursor and an alkyl thiol in a solvent to form a metal sulfide layer on the surface of a core, wherein the alkyl thiol is present on the surface of the metal sulfide nanocrystal, wherein the alkyl thiol is bonded to the sulfur crystal lattice. These metal sulfide nanocrystals can have a uniform particle size at the nanometer-scale level, selective and desired crystal structures, and various shapes.

Abstract: Disclosed relates to organic germanium nanocolloids, to which technetium-99m (99mTc), a radionuclide, is labeled, method of the same, and a spleen-imaging agent including the same. According to the invention, 99mTc-labeled organic germanium nanocolloids having high labeling efficiency and stability can be provided. Moreover, since the 99mTc-labeled organic germanium nanocolloids of the invention are accumulated in the spleen considerably higher than the conventional spleen-imaging agent, it is possible to use the 99mTc-labeled organic germanium nanocolloids of the present invention as a therapeutic radiopharmaceutical for the spleen imaging.

Abstract: The present invention relates to compounds that selectively bind to cells undergoing perturbations and alterations of their normal plasma membrane organization, such as cells undergoing apoptosis or activated platelets. The invention further provides methods for utilizing said compounds in medical practice, for diagnostic and therapeutic purposes.

Abstract: The present invention provides a novel imaging agent targeting the mannose-6-phosphate (M6P) receptor suitable for the non-invasive visualization of fibrosis. A method for the preparation of the imaging agent is also provided by the invention, as well as a precursor for use in said method. The invention also provides a pharmaceutical composition comprising the imaging agent and a kit for the preparation of the pharmaceutical composition. In a further aspect, use of the imaging agent for in vivo imaging and in the preparation of a medicament for the diagnosis of a condition in which the mannose-6-phosphate receptor is upregulated is provided.

Abstract: The aim of the invention is to provide radiolytically and metabolically stable metal complexes suitable for conjugation with biomolecules and, therefore, useful for nuclear medical diagnostics and in endoradionuclide therapy and to provide a method for their production.

Abstract: Formula (I) compounds are described: Formula (I) where the radicals are as defined in the description, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.

Abstract: Methods to image neovasculature associated with tumors using emulsions of targeted lipid/surfactant coated nanoparticles coupled to chelating agents containing radioisotopes are described.

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: 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: Novel radioactive technetium and rhenium complexes comprising tripodal ligands are provided by the present invention. In particular, Tc(I) complexes are provided by the present invention. Novel ligands suitable for the formation of the technetium and rhenium complexes of the invention are also provided, as well as radiopharmaceutical compositions comprising said complexes, kits for their preparation. The invention also relates to the us of 99mTc radiopharmaceuticals of the invention for SPECT imaging.

Abstract: Disclosed herein is a method for the preparation of radioisotope-labeled compounds using CNT. It comprises filling the carbon nanotube with a radioisotope; and labeling a physiologically active material with the radioisotope charged in the carbon nanotube. Taking advantage of CNT, the method can prepare a radioisotope-labeled compound invention at a high yield and in a simple manner. Also, the radioisotope, when remaining unreacted, can be recovered by the filtration of the CNT, thereby achieving the prevention of radioactive contamination and the reduction of radioactive waste. Further, the radioisotope-labeled compound is useful as a contrast medium for imaging the hepatobiliary system.

Abstract: Conjugates, methods and kits are described for imaging tissues and organs that express one or more peptidases. In a preferred embodiment of the invention, a series of di-(2-pyridylmethyl)amine (D) ligands, which can bind M(CO)3+ [M=Tc or Re], were coupled to lisinopril (L). Aliphatic tethers with varying number of methylene groups (3, 4, 5, and 7; D(C4)L, D(C5)L, D(C6)L, and D(C8)L, respectively) were utilized, with in vitro inhibitory activity increasing with increasing number of methylene groups. The D(C8)L conjugate was observed to be significantly more potent than D(C4)L. In vivo specificity for ACE was studied in both tissue distribution and gamma imaging studies, demonstrating localization in tissues with high ACE content. Localization was blocked by pretreatment with lisinopril.

Abstract: The invention provides a composition of matter of the formula (I): V-L-R, where V is a vector moiety having affinity for an angiogenesis-related endothelias cell receptor, L is a linker moiety or a bond and R is a detectable moiety, characterised in that V is a non-peptidic organic group, or V is peptidic and R is a macromolecular or particulate species providing a multiplicity of labels detectable in in vivo imaging.

Abstract: Nanohybrid polymer conjugates that provide a “platform” delivery system is disclosed. The delivery platform provides a multi-focused therapeutic regimen that may be tailored to combat a host of cancers, including advanced-stage, therapy-resistant tumors. The nanohybrids of the instant invention incorporate a configurable polymeric backbone, are multivalent (e.g., may incorporate several targeting ligands), and have the capacity to carry multiple classes of “payloads” (e.g., alpha-, beta-, gamma- and positron-emitting isotopes). The polymer conjugates comprise a single molecular species that can be useful not only in diagnostic assessment, but also in tailoring therapies to suit a variety of cancers.

Abstract: The present invention provides indeno[2,1a]indene and isoindolo[2,1-a]indole derivatives of the Formula I, its salts and its stereoisomers, wherein X, R1, R2, R3, R4, R6, R7, R8, R9, R11, R12, R13 and R14 are as described in the specification. The invention also provides a method to prepare the compound of formula I, pharmaceutical composition containing such compounds, and method to manufacture a medicament. These compounds are useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardio vascular diseases and cancer.

Abstract: One embodiment provides a composition comprising a) a compound of formula I: wherein R1, X and n have any of the values described in the specification, or a pharmaceutically acceptable salt thereof; b) a radionuclide; and c) a radioprotectant.

Abstract: A novel dual functioning excipient for metal chelate contrast agents is disclosed. The present excipient, Xm[X?(L?)]n, which is the calcium or zinc salt of the calcium or zinc complex of an organic ligand, enhances safety in that it is able to scavenge both free metal ions and free organic ligand.

Abstract: This invention relates to novel cationic crown-ether containing metal complexes, methods of preparing the cationic crown-ether containing metal complexes, and radiopharmaceutical compositions comprising the cationic crown-ether containing metal complexes. This invention relates particularly to cationic crown-ether containing 99mTc complex radiopharmaceuticals for diagnosis of cardiovascular disorders and cancer. This invention further relates to cationic crown-ether containing 186/188Re complex radiopharmaceuticals for radiotherapy of cardiovascular disorders and cancer.

Abstract: The present invention provides novel compounds that bind selectively to cells undergoing perturbations and alterations of the normal organization of their plasma membrane, while binding to a lesser degree to cells having membranes of normal organization, and their uses as diagnostic probes. Said compounds and methods used therein may be useful in medical practice, for applications such as diagnosis of disease and monitoring of response to therapy.

Abstract: Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.

Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.

Abstract: The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.