Abstract: The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of choice concerning inflammation and atherosclerosis progression. Thus, the present invention relates to radiolabeled Darapladib and analogs thereof and their use as imaging compounds.

Abstract: The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.

Abstract: The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.

Abstract: A main object of the invention is to provide a particle for medical use which has an excellent capability of fixing a target biologically active substance and has such chemical and physical stability that the particle is less dissolved or deteriorated in a washing step. The present invention has solved the above problem with a particle for medical use having a layer containing a polymer compound formed on a surface of a core particle, wherein the polymer compound is a polymer comprising at least repeating units derived from an ethylenically unsaturated polymerizable monomer (a) having a functional group for fixing a biologically active substance, wherein the polymer has a reactive functional group on at least one terminal side thereof.

Abstract: The present invention relates to hydrogels comprising 1,2-diol or 1,3-diol groups acetalised with a radiopaque species of one or more covalently bound radiopaque halogens which are imageable during embolization therapy. The invention further relates to methods of making radiopaque polymers and radiopaque hydrogel microspheres to provide an imageable drug delivery system.

Abstract: There is provided a composition used for contrast imaging, the composition containing an aqueous solution containing a J-aggregate of indocyanine green and at least one storage stabilizer selected from the group consisting of alkali metal ions, alkaline earth metal ions, and an ammonium ion.

Abstract: Use of benzimidazole-derived compounds of formula (I) according to the following structure, wherein x is a heteroatom selected from N, S, O, P, SO, SO2 and SO3, preferably from N, S and SO3 and most preferably from N and SO3; n may be 0 or 1, R1 is a group selected from formula (II) and formula (III) and R2 is a group selected from H and formula (IV) since the aforesaid serves for the production of a formulation used as a specific marker in the case of neurodegenerative diseases and tau pathologies.

Abstract: Novel derivatives of imidazopyridinylbenzeneamines and novel derivatives of benzothiazolylbenzeneamines are disclosed that offer improved behavior when used as imaging agents for positron emission tomography of beta-amyloids. Also disclosed is a palladium-catalyzed reaction scheme under microwave conditions for aryl thioethers in general that provides a high ratio of substitution relative to reduction and can be used for the imidazopyridinylbenzeneamine derivatives as well as other compounds of related structure.

Abstract: To encapsulate indocyanine green (ICG) at a high concentration in a liposome without causing the agglomeration of ICG so that ICG remains as a monomer in an ICG-containing particle to be used as, for example, a contrast agent for fluorescence imaging or photoacoustic imaging, provided is a method of producing an indocyanine green-containing particle, including the step of mixing indocyanine green, a particle, and a solution containing 1 mM or more and 10 M or less of a chaotropic agent.

Abstract: Compounds and a method for imaging myocardial perfusion, including administering to a patient a compound linked to an imaging moiety, wherein the compound binds MC-1, and scanning the patient using diagnostic imaging. Kits including the compound or precursor compounds linked or not linked to an imaging moiety are also described.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: The present invention provides for heptamethine cyanine dyes that possess both nuclear and near-infrared imaging capabilities. These dyes can be used for imaging, targeting and detecting tumors in patients.

Abstract: Compounds as defined herein are provided which are useful in (1) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable diluent; and (3) methods for imaging prostate cancer cells.

Abstract: There is provided a gelatin-ICG complex that can suppress leakage of ICG included therein. The complex has a gelatin derivative including at least one of a phospholipid covalently bonded to a gelatin or a cholesterol covalently bonded to a gelatin, and indocyanine green.

Abstract: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.

Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.

Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

Abstract: Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: The present invention relates to a composition and method for the detection of a detectable product formed from a compound of the present invention in the body of an individual. The detectable product may include a halide or a benzenetriol-based or benzenetetrol-based product of a dehalogenation reaction in the presence of FROS. In many embodiments, an indigo-like product formed from an indigogenic compound of the present invention may also be a detectable product for diagnostic purposes. This indigo-like product may have a higher residence time in tissues where it is formed, thus providing a detectable product localized to sites of high FROS. An indigogenic compound containing one or more radioactive isotopes is further provided for therapeutic purposes.

Abstract: The present invention relates to a composition and method for the detection of a detectable product formed from a compound of the present invention in the body of an individual. The detectable product may include a halide or a benzenetriol-based or benzenetetrol-based product of a dehalogenation reaction in the presence of FROS. In many embodiments, an indigo-like product formed from an indigogenic compound of the present invention may also be a detectable product for diagnostic purposes. This indigo-like product may have a higher residence time in tissues where it is formed, thus providing a detectable product localized to sites of high FROS. An indigogenic compound containing one or more radioactive isotopes is further provided for therapeutic purposes.

Abstract: The present invention relates to degradable polyacetal polymers having a C(O)—(CH2CH2O)n—R5 or a saccharide attached to amine radical of the backbone of the polymer, their polymer-active agent conjugates and their preparation processes, to compositions, and hydrogels containing them, as well as their use in therapy, diagnostic imaging and cosmetics.

Abstract: A compound that includes a quaterrylene dye moiety as core, and a dendrimeric shell. For example, the compound may comprise at least four dendronized polyamides covalently attached to a quaterrylene dye. Also disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, comprising A(G)x, wherein: A comprises a quaterrylene dye; G comprises at least one functionalized dendrimeric structure; and x is 2 to 16. The compounds may be used for in methods for monitoring a therapeutic or diagnostic agent in a subject, or for treating a subject by administering the compound to the subject.

Abstract: This invention relates generally to the discovery of novel nanoparticles for delivery of DNA double-stranded break (DSB) repair enzyme inhibitors such as wortmannin or wortmannin analogues. In one embodiment, these nanoparticles comprise a polylactide polyglycolide (PLGA) copolymer and a polyethylene glycol (PEG). In addition methods of treatment and methods of enhancing radiation treatments are also provided.

Abstract: The invention provides co-crystals and salts of contrast agents as well as methods to use and prepare the co-crystals and salts.

Abstract: This invention relates to a method of imaging vesicular monoamine transporters and to labeled compounds and pharmaceutical compositions thereof, and methods of making labeled compounds useful in imaging vesicular monoamine transporters. This invention also relates to compounds, and methods of monitoring progression of a disease related to vesicular monoamine transporters.

Abstract: This invention relates to determining the compliance of a subject receiving dietary supplementation with uridine or a uridine source. Specifically, the invention relates to the use of MRS for measuring an increase in brain compounds resulting from dietary supplementation with uridine or a uridine source.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds of the formula R—Y—X—Z—R where each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties, Y and Z are urea and urethane groups and X is a alkylene group which may be further substituted. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: A contrast agent for angiography is disclosed, in particular, for examining animal or human bodies or components thereof such as members or organs thereof, comprising an essentially oil-based apolar contrast component for X-ray examinations, the contrast component having a contrast component viscosity in the range of 30-100 mPas. The contrast agent is characterised in that the contrast component is present in a mixture with at least one further apolar component, the viscosity of which is less than or at most equal to the contrast component viscosity. Methods for angiography examination are also disclosed, in which such a contrast agent or also a polar contrast agent are used at least periodically and applications of such contrast agents.

Abstract: Novel fluorescent dye comprising metal oxide nanoparticles are prepared where the nanoparticles are as small as 3 nm or up to 7000 nm in diameter and where the dye is bound within the metal oxide matrix. In some embodiments the invention, novel dyes are covalently attached to the matrix and in other embodiments of the invention a dye is coordinate or ionic bound within the metal oxide matrix. A method for preparing the novel covalently bondable modified fluorescent dyes is presented. A method to prepare silica comprising nanoparticles that are 3 to 8 nm in diameter is presented. In some embodiments, the fluorescent dye comprising metal oxide nanoparticles are further decorated with functionality for use as multimodal in vitro or in vivo imaging agents. In other embodiments of the invention, the fluorescent dye comprising metal oxide nanoparticles provide therapeutic activity and incorporated therapeutic temperature monitoring.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: The present invention relates to a composition and method for the detection of a detectable product formed from a compound of the present invention in the body of an individual. The detectable product may include a halide or a benzenetriol-based or benzenetetrol-based product of a dehalogenation reaction in the presence of FROS. In many embodiments, an indigo-like product formed from an indigogenic compound of the present invention may also be a detectable product for diagnostic purposes. This indigo-like product may have a higher residence time in tissues where it is formed, thus providing a detectable product localized to sites of high FROS. An indigogenic compound containing one or more radioactive isotopes is further provided for therapeutic purposes.

Abstract: The present invention provides nonradioactive NIR optical imaging agents based up on the structure of retinoid acid derivatives. The nonradioactive NIR optical imaging agent has been evaluated at the cellular level by confocal microscopy, and in vivo in a whole animal using a various xenograft models. The specific uptake of this agent in human cancer cells and multiple xenograft models demonstrate that nonradioactive near infrared dye labeled retinoid metabolites and/or analogs are useful for early stage cancer studies and diagnoses. Also, the present invention provides that nonradioactive near infrared dye labeled retinoid metabolites and/or analogs are useful for visualization of drug redistribution within the body which is useful in determining the optimal biological dose. Ultimately, the visualization data can be used as an analytical tool to reduce any systemic toxicity.

Abstract: Disclosed are compounds comprising the structure: In one aspect, the compounds exhibit maximum symmetric branching. Also disclosed are bilayers, micelles, coatings, and nanoparticles comprising the disclosed compounds. Also disclosed are processes for the preparation of the disclosed compounds and methods of using the disclosed compounds. Also disclosed are highly fluorinated dendrons and methods for making same. Also disclosed are methods for Fluorous Mixture Synthesis and tagging. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.

Abstract: Radiolabeled cyclic polypeptides, pharmaceutical compositions comprising radiolabeled cyclic polypeptides, and methods of using the radiolabeled cyclic polypeptides. Such polypeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an alkene or alkyne dienohile.

Abstract: Use of a radiolabelled form of 7-chloro-?/,?/,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4/-/-pyridazino[4,5-b]indole-1-acetamide as a biomarker for the detection, in an individual, of PBR levels associated with normal and pathological conditions. Method for the detection of PBR levels associated with normal and pathological conditions. Diagnostic kit.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: Presented is a method for assessing dopamine transporter levels in a selected area of a subject's central nervous system by SPECT imaging comprising administering an injection of a labeled dopamine transporter ligand at approximately the time the subject is positioned for SPECT imaging and initiating a SPECT acquisition for a duration of about 30 minutes commencing at about 15 minutes after administration of labeled dopamine transporter ligand; and assessing, based on said SPECT acquisition, the amount of labeled dopamine transporter ligand that is bound to dopamine transporter.

Abstract: Use of benzimidazole-derived compounds of formula (I) according to the following structure, wherein x is a heteroatom selected from N, S, O, P, SO, SO2 and SO3, preferably from N, S and SO3 and most preferably from N and SO3; n may be 0 or 1, R1 is a group selected from formula (II) and formula (III) and R2 is a group selected from H and formula (IV) since the aforesaid serves for the production of a formulation used as a specific marker in the case of neurodegenerative diseases and tau pathologies.

Abstract: Tetrapyrollic photosensitizers and imaging agent compounds having A, B, C, and D rings and having a reduced B ring and an oxidized D ring. The compounds preferably have a purity of at least 95 percent and preferably have a fused system connected at an unsaturated carbon atom of the C ring nearest the D ring and at the unsaturated carbon atom between the C and D rings. The invention also includes a method of making the compounds at over 95 percent yield by starting with a B and D ring oxidized tetrapyrollic compound and dissolving it in a halogenated hydrocarbon solvent and treating it with sufficient nitroalkane solution of FeCl3.6H2O to oxidize the D ring and separating the resulting organic layer and drying.

Abstract: The invention relates to compounds of formula I, their synthesis and their use, in particular for detecting amyloid deposits in a patient.

Abstract: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.

Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for therapy and diagnostic imaging by positron emission tomography (PET).

Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

Abstract: A compound of formula (I) wherein, X and Y independently bind TSPO, wherein X and Y are the same or different; and L is a linker that links X to Y; or a salt or solvate thereof. For preference, X and Y may be (II) or (III). The compounds may be radiolabeled with a radioisotope. Also methods for diagnosing or treating TSPO related disorders such as neurodegenerative disorder, inflammation or anxiety, eg. Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis, multiple system atrophy, epilepsy, encephalopathy, stroke, brain tumour, anxiety, stress, emotional disturbances or cognitive impairment, glioblastoma, ischemic stroke, herpes encephalitis, HIV, amyotrophic lateral sclerosis, corticobasal degeneration, cancer, depression, an auto-immune disease and an infectious disease.

Abstract: This invention relates to new carbocyanine fluorophores comprising a biomolecule targeting moiety containing 1-6 aromatic moieties, wherein the targeting moiety is designed to attach to biocompatible molecules to form in vivo optical imaging agents.

Abstract: Overexpression of angiotensin-converting enzyme (ACE) has been associated with a number of pathophysiologies, including those associated with cancer and the cardiovascular system. Thus, targeted imaging of ACE is of crucial importance for monitoring tissue ACE activity as well as treatment efficacy. To this end, lisinopril-coated gold nanoparticles were prepared to provide a new type of probe for targeted molecular imaging of ACE by tuned K-edge computed tomography (CT) imaging.