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Fluorine

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424 - Drug, bio-affecting and body treating compositions

424100110 - RADIONUCLIDE OR INTENDED RADIONUCLIDE CONTAINING; ADJUVANT OR CARRIER COMPOSITIONS; INTERMEDIATE OR PREPARATORY COMPOSITIONS

424100650 - In an organic compound

424100810 - Nonmetal radionuclide or intended radionuclide (e.g., carbon)

424100850 - Halogen

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DocumentTitleDate
20110182812Imaging Agents for Detecting Neurological Disorders - Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.07-28-2011
20100150836RADIOLABELLED BENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING - Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 06-17-2010
20090123373AMYLOID-IMAGING AGENTS - A molecular probe for use in the detection of amyloid in a subject includes a dibenzothiazole derivative.05-14-2009
20090123372DEVELOPMENT OF MOLECULAR IMAGING PROBES FOR CARBONIC ANHYDRASE-IX USING CLICK CHEMISTRY - The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.05-14-2009
20090087379Radiofluorinated Compounds and their Preparation - The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.04-02-2009
20120244074LABELLED INTEGRIN BINDERS - The present invention provides alternative in vivo imaging agents suitable for use in the detection of α09-27-2012
20120244073ARYLOXYANILIDE IMAGING AGENTS - The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.09-27-2012
20120183474Methods and System for Detecting Soluble Amyloid-Beta - The present invention provides methods of detecting soluble amyloid β using curcumin-derived near infrared (NIR) imaging probes. Upon interacting with soluble amyloid β, these probes undergo a range of changes, qualifying them as “smart” probes. In addition, the invention provides methods of detecting soluble amyloid β by positron emission tomography (PET), magnetic resonance imaging (MRI) and multimodal imaging based on the curcumin-derived NIR imaging probes and derivatives thereof.07-19-2012
20130084245PET MONITORING OF A-BETA-DIRECTED IMMUNOTHERAPY - The present invention provides methods of monitoring Aβ-directed immunotherapy. The methods involve administering a PET ligand that binds to amyloid deposits and detecting the PET ligand in the brain to provide an indication of the level and/or distribution of amyloid deposits. Surprisingly, the data in the present application show that a statistically significant reduction in amyloid deposits occurs early and consistently among patients following initiation of treatment before statistically significant effects of most if not all other markers are detectable. In consequence, the present methods allow early detection of whether a patient is responding to the Aβ-directed immunotherapy and if necessary adjustment of the immunotherapy regime.04-04-2013
201302093622-ALKOXY-11-HYDROXYAPORPHINE DERIVATIVES AND USES THEREOF - The invention features 2-alkoxy-11-hydroxyaporphine derivatives that selectively bind D08-15-2013
201300451654-FLUORO-4-ARYLPIPERDIN-1-YL DERIVATIVES AS MU OPIOID FUNCTION MODERATORS - 4-Fluoro-4-phenylpiperidin-02-21-2013
20130045164AMYLOID IMAGING AS A SURROGATE MARKER FOR EFFICACY OF ANTI-AMYLOID THERAPIES - The present method for determining the efficacy of therapy in the treatment of amyloidosis involves administering to a patient in need thereof a compound of formula (I) or Formula (II) or structures 1-45 and imaging the patient. After said imaging, at least one anti-amyloid agent is administered to said patient. Then, an effective amount of a compound of formula (I) or Formula (II) or structures 1-45 is administered to the patient and the patient is imaged again. Finally, baseline levels of amyloid deposition in the patient before treatment with the anti-amyloid agent are compared with levels of amyloid deposition in the patient following treatment with the anti-amyloid agent.02-21-2013
20100143253COMPOUNDS AND AMYLOID PROBES THEREOF FOR THERAPEUTIC AND IMAGING USES - The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus. The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions, derivatives, prodrugs, racemic mixtures or tautomeric forms thereof.06-10-2010
20100143252IMAGING 18F OR 11C-LABELLED ALKYLTHIOPHENYL GUANIDINES - The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R06-10-2010
20130028838F18-TYROSINE DERIVATIVES FOR IMAGING BONE METASTASES - This invention relates to radioactive tyrosine derivatives for imaging bone metastases, a method for imaging or diagnosing bone metastases, compositions and kits for imaging bone metastases.01-31-2013
20130028837CONTRAST AGENTS FOR MYOCARDIAL PERFUSION IMAGING - The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.01-31-2013
20100068140MYELIN DETECTION USING BENZOFURAN DERIVATIVES - The present invention relates to methods for the detection of myelin and a quantitative measurement of its local concentration in a sample using a benzofuran compound or its radioisotope derivatives. In one embodiment a method of myelin detection comprises identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, parenterally administering to the subject the benzofuran compound, or a derivative of the compound, and determining myelination in the subject by detecting binding in the sample. In one embodiment, the invention provides a method of imaging myelinated tissue in a surgical field of mammalian tissue comprising the steps of contacting the surgical site with the benzofuran compound or a radioisotope derivative of the compound, and detecting binding in the surgical site. In yet another embodiment, a method of imaging spinal cord and spinal nerve root tissue is provided comprising the steps of parenteral administration of a radioisotope derivative of the benzofuran compound and detecting the radioisotope derivative within the spinal canal and intervertebral foramen. Methods of quantification of binding of the benzofuran compound or its derivatives are also provided.03-18-2010
20130089501SOLID-PHASE FLUORINATION OF BENZOTHIAZOLES - The invention provides a process for the production of an 04-11-2013
20130089502PET RADIOPHARMACEUTICALS FOR DIFFERENTIAL DIAGNOSIS BETWEEN BILATERAL AND UNILATERAL CONDITIONS OF PRIMARY HYPERALDOSTERONISM - A functional PET imaging method is disclosed for differentiation between bilateral hyperplasia and unilateral adenoma comprising (1) introducing a radioactively labelled CYP11 B2 (aldosterone synthase) inhibitor which binds selectively to CYP11 B2 (aldosterone synthase) relative to CYP11 B1 (11β-hydroxylase) into a mammal with adrenal glands and (2) conducting positron emission tomography (PET) in the region of the adrenal glands to obtain a functional PET image of the adrenal glands. Also disclosed are radioactive tracer compounds suitable for use in this method, precursors for making the same, and a process for making the radioactive tracer compounds capable of being conducted as a rapid one-pot reaction.04-11-2013
20110008254RADIOPHARMACEUTICAL COMPOSITION - The present invention relates to radiopharmaceuticals and in particular to a radiopharmaceutical composition comprising a compound of Formula (I): and polysorbate as an excipient. The radiopharmaceutical composition of the invention reduces problems encountered with prior art compositions comprising the same class of compounds. Also provided by the invention is a method for the preparation of the radiopharmaceutical composition of the invention as well as particular uses of the radiopharmaceutical composition.01-13-2011
20130071327HOMOGLUTAMIC ACID DERIVATIVES - This invention relates to homoglutamic acid derivatives suitable for labeling or already labeled with 03-21-2013
20090274624RADIOTRACERS FOR IMAGING P-GLYCOPROTEIN FUNCTION - P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established or prospective chemotherapeutics (a phenomenon known as multidrug resistance). This invention concerns the preparation and use of radiotracers for imaging P-gp function in vitro and in vivo. Radiotracers of the present invention are avid substrates for P-gp and have structures based on N-Desmethyl-loperamide.11-05-2009
20090269278Radiolabeled Glycine Trasporter Inhibitors - The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.10-29-2009
20130064770RADIOLABELED COMPOUNDS AND METHODS THEREOF - The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.03-14-2013
20130064769METHODS AND APPARATUS FOR SYNTHESIZING IMAGING AGENTS, AND INTERMEDIATES THEREOF - The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comprising a radioisotope (e.g., 03-14-2013
20130164217METHOD OF DIAGNOSING, PREVENTING AND/OR TREATING DEMENTIA & RELATED DISORDERS - Described are assay methods, modules and kits useful in the detection, treatment and/or prevention of dementia and related conditions, including but not limited to Alzheimer's disease and mild cognitive disorders.06-27-2013
20090047215MN/CA IX and Breast Cancer Therapy - Herein disclosed are methods that are predictive of resistance to endocrine therapy in an estrogen receptor-positive (ER-positive) breast cancer patient. An exemplary method comprises detecting the overexpression of MN/CA9 gene expression product(s) in a sample from an affected subject, wherein if MN/CA9 is overexpressed, then the subject is considered to have a greater probability of resistance to endocrine therapy, particularly tamoxifen, and a corresponding poorer prognosis if undergoing endocrine therapy, than if MN/CA9 is not overexpressed. MN/CA9 gene expression products useful in the predictive/prognostic methods include MN/CA IX, MN proteins/polypeptides, MN nucleic acids and soluble MN/CA IX antigen (s-CA IX). The methods are useful as an aid in the selection of treatment for a patient with an ER-positive breast tumor. The methods of the invention can be used, for example, to identify those patients requiring additional/alternative therapies, preferably, but not necessarily, therapies that are not affected by acidic pH. The methods also comprise the use of diagnostic/prognostic imaging to detect MN/CA IX in a patient tumor, wherein the presence of MN/CA IX in one or more tumors is indicative of probable resistance to antiestrogen therapy, particularly to tamoxifen.02-19-2009
20090010846Nitro-Imidazole Hypoxia Imaging Agents - The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.01-08-2009
20120237446Compounds for binding and imaging amyloid plaques and their use - The present invention relates to novel compounds (3-aminopropen-1-ones) useful for binding and imaging beta amyloid deposits and their use in detecting or treating Alzheimer's disease and amyloidosis.09-20-2012
20120237445STABILIZATION OF RADIOPHARMACEUTICAL COMPOSITIONS USING ASCORBIC ACID - Radiopharmaceutical compositions, and related methods, useful for medical imaging are provided. The radiopharmaceutical compositions include one or more radiopharmaceutical compounds, together with a stabilizer comprising ascorbic acid, wherein the pH of said composition is within the range of about 3.5-5.5.09-20-2012
20130164218HYPOXIA INDUCIBLE FACTOR-1 PATHWAY INHIBITORS AND USES ASANTICANCER AND IMAGING AGENTS - This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.06-27-2013
20110280804HIGHLY SELECTIVE SIGMA RECEPTOR RADIOLIGANDS - Compounds having the general formula III′, or IV′11-17-2011
201201895482-ARYLPYRAZOLO[L,5-ALPHA]PYRIMIDIN-3-YL ACETAMIDE DERIVATIVES AS LIGANDS FOR TRANSLOCATOR PROTEIN (18 KDA) - The invention provides compounds of formula (I) radiolabelled with 07-26-2012
20120189547[18F] LABELLED ANALOGUES OF FLUMAZENIL AS IN VIVO IMAGING AGENTS - The present invention provides radiofluorinated compounds useful for in vivo imaging GABA07-26-2012
20110142758INDOLYL-PYRIDAZINYL-DIAZABICYCLONONANE DERIVATIVES IN LABELLED AND UNLABELLED FORM AND THEIR USE IN DIAGNOSTIC METHODS - The present invention relates to indolyl-pyhdazinyl-diazabicyclononane derivatives in their labelled and unlabelled 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).06-16-2011
20080305042Radiolabelling Method Using Polymers - The present invention provides a method for the preparation of radioisotopically-labelled imaging agent compositions. The method uses precursors which are bound to soluble polymers, so that the radiolabelling reaction is carried out in solution. Also described are radiopharmaceutical compositions, automated versions of the radiolabelling method and disposable cassettes for use in the automated method.12-11-2008
200900416645-Pyrrolidinylsulfonyl Isatin Derivatives - The present invention relates to novel 5-pyrrolidinylsulfonyl isatin derivatives, non-peptidyl Caspase binding Radioligands (CbRs) and CbR-transporter conjugates derived from said isatin derivatives, diagnostic compositions comprising said compounds of the invention and their use for non-invasive diagnostic imaging.02-12-2009
20100266500STILBENE DERIVATIVES AND THEIR USE FOR BINDING AND IMAGING AMYLOID PLAQUES - 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.10-21-2010
2011030007318F-LABELLED THREE-AND FOUR-CARBON ACIDS FOR PET IMAGING - Compositions containing three and four-carbon acids labeled with 12-08-2011
20110300072Benzimidazole-derived compounds use as markers in the case of neurodegenerative diseases - 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, SO12-08-2011
2011028692118F-LABELLED FOLATES AS PET RADIOTRACERS - The present invention is directed towards new 11-24-2011
20110286922IMAGING AND RADIOTHERAPY METHODS - The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.11-24-2011
20110293520NEW DRUG FOR INHIBITING AGGREGATION OF PROTEINS INVOLVED IN DISEASES LINKED TO PROTEIN AGGREGATION AND/OR NEURODEGENERATIVE DISEASES - The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R12-01-2011
20110002850Nitro-Imidazole Hypoxia Imaging Agent - The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.01-06-2011
20090317328TRICYCLIC OXAZEPINES AS IN VIVO IMAGING COMPOUNDS - Novel compounds of formula (I): suitable for use as in vivo imaging agents are provided as well as precursors suitable for the preparation of said compounds. The present invention also provides pharmaceuticals comprising the compounds and kits for the preparation of the pharmaceuticals. Furthermore, use of the compounds for imaging peripheral benzodiazepine receptors in a subject is provided, in particular for imaging pathological conditions in which PBR are upregulated, e.g. Parkinson's disease, multiple sclerosis, Alzheimer's disease and Huntington's disease, neuropathic pain, arthritis, asthma, atherosclerosis and cancer.12-24-2009
20100055036PET VISUALIZATION OF AMYLOID-ASSOCIATED NEUROINFLAMMATION IN THE BRAIN - The present invention relate to a method for monitoring a response to a therapy on a mammal having a neurodegenerative or neuroinflammatory disorder. According to a preferred embodiment, the method comprising the steps of:03-04-2010
20120189546Radiolabelling Method Using Cycloalkyl Groups - This invention relates to novel cyclo alkyl compounds suitable for labeling by 07-26-2012
20110217234IMAGING LIGANDS - Naphthoxazine derivatives which are selective ligands for the dopamine D2 receptor and which carry an 18F radio-label suitable for imaging with PET are described. The compounds of the present invention are thus useful for in vivo diagnostics and in vivo imaging of the dopamine D2 receptor.09-08-2011
20080292552Pet Radiotracers - The invention relates to novel 11-27-2008
2010011186318F-LABELLED FOLATES - The present invention is directed towards new 05-06-2010
20100015053RADIOLABELLED TRP M8 RECEPTOR LIGANDS - The present invention is directed to radiolabelled ligands, useful for the labeling and imaging of TRP M8 (transient receptor potential M8 channel) functionality. The present invention is further directed to pharmaceutical compositions comprising the radiolabelled ligands and methods for the preparation of the radiolabelled ligands.01-21-2010
20080247948STEREOISOMERS OF FATTY ACID ANALOGS FOR DIAGNOSTIC IMAGING - 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.10-09-2008
20100119448METHOD FOR PRODUCTION OF RADIATION DIAGNOSTIC IMAGING AGENT - A method for producing a radioactive diagnostic imaging agent which contains a radioactive halogen-labeled amino acid compound as an effective ingredient and has a composition that can inhibit radiolysis of the effective ingredient, thereby further improving stability, is provided. Disclosed is a method for producing a radioactive diagnostic imaging agent, comprising a solution preparation step of preparing a solution containing a radioactive halogen-labeled amino acid compound, and a dilution step of diluting the solution containing the radioactive fluorine-labeled organic compound in order to adjust radioactive concentration thereof, which further comprises an acid addition step of adding an acid to the solution containing the radioactive fluorine-labeled organic compound, after the solution preparation step and before the dilution step, wherein the acid is added in the acid addition step in an amount sufficient to adjust the pH of the solution resulting from the dilution step to 2.0-5.9, for example, in an amount corresponding to 0.40-2.8 mmol per 1 L of the solution resulting from the dilution step.05-13-2010
20120269727IMAGING AGENTS WITH IMPROVED PHARMACOKINETIC PROFILES - The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.10-25-2012
20100098634Imaging Agents Useful for Identifying AD Pathology - Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.04-22-2010
20090142265ALPHA-FLUOROALKYL TETRABENAZINE AND DIHYDROTETRABENAZINE IMAGING AGENTS AND PROBES - The present invention provides novel alpha-fluoroalkyl compounds having structure I and the corresponding dihydrotetrabenazine compounds IV06-04-2009
20120107240Probes and methods of melanoma imaging - Embodiments of the present disclosure provide for labeled probes such as a 3-05-03-2012
20120107239Precursor of Molecular Probe for Pancreatic Islet Imaging and Use of the Same - A precursor of a molecular probe for imaging of pancreatic islets is a compound expressed as the following formula (I):05-03-2012
20090263322OCTAHYDRO-INDOLIZINE AND QUINOLIZINE AND HEXAHYDRO-PYRROLIZINES - The invention features substituted fused bicyclic compounds, pharmaceutical compositions containing them, and methods of using them to treat or prevent histamine-mediated diseases and conditions.10-22-2009
20090169475RADIOLABELED DERIVATIVES OF POTENT CHYMASE INHIBITORS - Methods of imaging tissue of a mammal which expresses chymase include administering to the mammal an effective amount of a radiolabeled chymase inhibitor. Radiopharmaceuticals that may be used in diagnostic imaging and therapeutic treatment of disease characterized by expression of chymase have the structure of Formula I:07-02-2009
20080311038Radicicol Derivatives Useful for Position Emission Tomography - The present invention relates to novel radicicol derivatives of the formula I,12-18-2008
20080213178Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid - 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.09-04-2008
20120294803CXCR4 ANTAGONISTS FOR IMAGING OF CANCER AND INFLAMMATORY DISORDERS - The invention provides radiolabeled CXCR4 antagonists, compositions and methods of use for imaging of chemokine CXCR4 receptors and biological conditions associated with the expression of CXCR4 receptors, including cancer, metastasis, and inflammatory disorders.11-22-2012
201002787321H-[1, 2, 3] TRIAZOLE SUBSTITUTED AMINO ACIDS AND USES THEREOF - Tracers for cationic amino acid transport systems and methods of synthesis are disclosed, including compounds comprising a 1H-[1,2,3]triazole moiety. Further disclosed are uses of the analogues, including in vivo imaging of tumors by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).11-04-2010
20090311179Selective Targeting of Apoptotic Cells - The invention relates to a method of selectively targeting an active agent (or agent capable of becoming an active agent) to apoptotic cells in a vertebrate, comprising administering to said vertebrate a system comprising an arsenoxide (or arsenoxide equivalent) compound and said agent, wherein said system selectively targets apoptotic cells.12-17-2009
20090162283DIAGNOSTIC AND REMEDY FOR DISEASE CAUSED BY AMYLOID AGGREGATION AND/OR DEPOSITION - To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition.06-25-2009
20110142760PSMA-BINDING AGENTS AND USES THEREOF - Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.06-16-2011
20110142759AGENTS AND METHODS FOR THE IMAGING OF MYELIN BASIC PROTEIN - The present invention relates to agents capable of binding to myelin basic protein in a subject. Also provided are methods for the detection of myelin-associated neuropathy comprising identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, administering to a subject an agent that binds specifically to myelin basic protein, and determining myelination in the subject by detecting the agent present in the subject. A kit containing the agent or its derivatives for use in detecting myelin basic protein is also provided.06-16-2011
20080299041HETEROCYCLIC INDENE DERIVATIVES AND THEIR RADIOISOTOPE LABELED COMPOUNDS FOR IMAGING BETA-AMYLOID DEPOSITION - The invention is directed to heterocyclic indene derivatives useful for β-amyloid plaque imaging, their radiolabeled compounds and their preparation methods. The compounds of the invention are easily labeled with radioisotopes and have high affinities to β-amyloid depositions, thus they facilitate diagnosis of Alzheimer's disease by imaging the distribution of β-amyloid depositions.12-04-2008
20090004107BETA-AMYLOID AND NEUROFIBRILLARY TANGLE IMAGING AGENTS - Compounds, compositions and methods are contemplated in which senile plaques and/or neurofibrillary tangles are labeled using compounds with improved permeability across the blood brain barrier and improved selective binding to senile plaques and/or neurofibrillary tangles. Contemplated compounds are derivatives of FDDNP or curcumin, which most preferably have improved solubility in aqueous solvents. Labeling is typically performed using a PET detectable label, and especially 01-01-2009
20090220420TETRACYCLIC INDOLE DERIVATIVES AS IN VIVO IMAGING AGENTS AND HAVING PERIPHERALBENZODIAZEPINE RECEPTOR AFFINITY (PBR) - The present invention provides novel tetracyclic indole compounds of Formula (I) either as in vivo imaging agents or as therapeutic agents. A method for the preparation of the in vivo imaging agent compound is also provided by the invention, as well as a precursor for use in said method. Pharmaceutical compositions comprising the compounds of the invention are additionally provided. Where the pharmaceutical composition comprises a compound suitable for in vivo imaging, a kit is provided for the preparation of the pharmaceutical composition. In a further aspect, use of the compound for in vivo imaging or treatment of conditions associated with PBR is provided.09-03-2009
20090252680NOVEL COMPOUND WITH AFFINITY FOR AMYLOID - A compound represented by the following formula or a salt thereof:10-08-2009
20090252679Novel Compound Having Affinity for Amyloid - The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof:10-08-2009
20100178248USE OF PHENYLOXYANILINE DERIVATIVES FOR IMAGING CARDIOVASCULAR DISEASES - The present invention relates to the use of a specific compound, as described in detail below, having a high affinity to the peripheral benzodiazepine receptor for imaging cardiac and cardiovascular diseases for which inflammation and/or mitochondrial dysfunction and any other pathophysiological process leading to PBR activation are major contributing factor.07-15-2010
20090117042Imaging agents and methods of imaging NAALADase or PSMA - 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.05-07-2009
20100260674QUINAZOLINE DERIVATIVES AND METHODS OF TREATMENT - This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.10-14-2010
20100254903Substituted Aryl-Fluoroborates as Imaging Agents - Substituted aryl-boron compounds comprising at least one 10-07-2010
20120034165IMAGING THE CENTRAL NERVOUS SYSTEM WITH PURINERGIC P2X7 RECEPTOR BINDING AGENTS - The present invention provides novel compounds which may be used as in vivo imaging agents. The compounds of the invention are useful in a method to image the expression of P2X7 receptors in a subject, as a means to facilitate the diagnosis of a range of disease states.02-09-2012
20100034741Imaging agents and methods of imaging alpha7-nicotinic cholinergic receptor - The present invention relates to radiolabelled compounds particularly 1-azabicyclo[2.2.2]octane compounds (i.e., quinuclidine 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 the α7-nicotinic cholinergic receptor. 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 α7-nicotinic cholinergic receptor to which the compounds of the invention have an affinity.02-11-2010
20090110636FLUORINATED DIHYDROTETRABENAZINE ETHER IMAGING AGENTS AND PROBES - The present invention provides novel fluorinated ether compounds having structure I04-30-2009
20130129625IN VIVO IMAGING AGENTS - The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.05-23-2013
20130129626IN VIVO IMAGING AGENTS - The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.05-23-2013
20110044899LABELLED ANALOGUES OF HALOBENZAMIDES AS MULTIMODAL RADIOPHARMACEUTICALS AND THEIR PRECURSORS - A compound of formula (I): in which R02-24-2011
20110044898TRANSLOCATOR PROTEIN LIGANDS - The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.02-24-2011
20110091383FENRETINIDE DERIVATIVES AND USES THEREOF AS THERAPEUTIC, DIAGNOSTIC AND IMAGING AGENTS - Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.04-21-2011
20090028791Dichloroacetate Analogs as Imaging Agents - A compound having structure I:01-29-2009
20110097269PHENYLOXYANILINE DERIVATIVES - The present invention relates to phenyloxyaniline derivatives, to methods of their production and to uses thereof.04-28-2011
20110250137RADIOISOTOPE-LABELED LYSINE AND ORNITHINE DERIVATIVES, THEIR USE AND PROCESSES FOR THEIR PREPARATION - The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I.10-13-2011
20110250135Piperazine Derivatives for Binding and Imaging Amyloid Plaques and Their Use - The invention relates to compounds of formula I, their synthesis and their use, in particular for detecting amyloid deposits in a patient.10-13-2011
20110070161ACTIVE ENANTIOMER - The present invention provides a PET tracer that has improved properties for imaging the peripheral benzodiazepine receptor (PBR) as compared with known such PET tracers. The present invention also provides a precursor compound useful in the preparation of the PET tracer of the invention and methods for the preparation of said precursor compound and said PET tracer. Also provided by the present invention is a radiopharmaceutical composition comprising the PET tracer of the invention. Methods for using the PET tracer and the radiopharmaceutical composition are also provided.03-24-2011
20110070160Dose Synthesis Mosule for Biomaker Generator System - A microfluidic radiopharmaceutical production system and process for synthesizing per run approximately, but not less than, one (1) unit dose of a radiopharmaceutical biomarker for use in positron emission tomography (PET). The radiopharmaceutical production system includes a reaction vessel that receives a radioisotope from an accelerator or other radioisotope generator. Organic and aqueous reagents are introduced into the reaction vessel, and the mixture is heated to synthesize a solution of a pre-selected radiopharmaceutical. The radiopharmaceutical solution is purified by passing the solution through a solid phase extraction column and a filter. The synthesis process produces per run a quantity of radiopharmaceutical approximately equal to, but not less than, one (1) unit dose of a radiopharmaceutical, reducing waste and allowing for the production of radiopharmaceutical on an as-needed basis. The synthesis process allows for the production of biomarker radiopharmaceuticals on site and close to the location where the unit dose will be administered to the patient. On-site, as-needed production of radiopharmaceuticals in small doses reduces the time between the synthesis of the radiopharmaceutical and the administration of that radiopharmaceutical, thereby minimizing the loss of active isotopes through decay and allowing the production of lesser amounts of radioisotopes overall.03-24-2011
20110033382Imaging Agents - This invention provides amino acid derivatives useful in detecting and evaluating brain and body tumors, including (1S,2S) anti-2-[18F]FACPC and (1R,2R) anti-2-[18F]FACPC.02-10-2011
20100310457IMAGING OF MYELIN BASIC PROTEIN - The present invention relates to methods for myelin basic protein detection comprises identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, parenterally administering to the subject the agent, and determining myelination in the subject by detecting binding to myelin basic protein. Methods for the detection of myelin and a quantitative measurement of its local concentration in a sample using an agent with specific binding to myelin basic protein are also provided as is a kit containing the agent or its derivatives for use in detecting myelin basic protein12-09-2010
20120171119PEGYLATED FLUOROBENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING - Pegylated fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labeled with a positron-emitting radioisotope such as 07-05-2012
20090317327Aqueous Dispersion of Superparamagnetic Single-Domain Particles, Production and Use Thereof in Diagnosis and Therapy - The invention relates to an aqueous dispersion of superparamagnetic iron-containing particles bearing α-hydroxycarboxylic acids as stabilizer substances on their surface, said dispersion comprising N-methyl-D-glucamine (meglumine) and/or 2-amino-2-(hydroxymethyl)-1,3-propanediol (trometamol) and the content of free iron ions being lower than 1 mg of iron per liter. In a preferred embodiment the dispersion according to the invention may additionally include an iron-complexing agent. In another preferred embodiment the dispersion includes positively charged metal ions and/or compounds containing polyamino groups, which can be bound to substances having a therapeutic or diagnostic effect. The invention is also directed to a method of producing said dispersion, the use thereof as an MRT contrast medium as well as the use thereof as therapeutic agent, including the option of therapy follow-up using an imaging method.12-24-2009
20120201754PHOSPHODIESTERASE 1-TARGETING TRACERS AND METHODS - Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particulaly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.08-09-2012
20080279774Perturbed Membrane-Binding Compounds And Methods Of Using The Same - 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.11-13-2008
20110165076NOVEL [F-18]- LABELLED L-GLUTAMIC ACID AND L-GLUTAMINE DERIVATIVES (I), USE THEREOF AND METHOD FOR THEIR PRODUCTION - 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.07-07-2011
20110027178IMAGING THE CENTRAL NERVOUS SYSTEM - The present invention provides novel compounds which may be used as in vivo imaging agents. The compounds of the invention are useful in a method to image the expression of P2X02-03-2011
20110052492Radiohalogenated Benzamide Derivatives And Their Use In Tumor Diagnosis And Tumor Therapy - This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.03-03-2011
20110097268RADIOHALOIMATINIBS AND METHODS OF THEIR SYNTHESIS AND USE IN PET IMAGING OF CANCERS - We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.04-28-2011
20110189090MOLECULAR PROBES FOR IMAGING OF MYELIN - A molecular probe for labeling myelin includes a fluorescent trans-stilbene derivative.08-04-2011
20110189089RADIOFLUORINATION - The present invention relates to 08-04-2011
20100172836SYNTHESIS OF 18F-RADIOLABELED STYRYLPYRIDINES FROM TOSYLATE PRECURSORS AND STABLE PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to methods of synthesizing 07-08-2010
20110027179Radiohalogenated Benzamide Derivatives And Their Use In Tumor Diagnosis And Tumor Therapy - This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.02-03-2011
20110305637RADIOLABELLED PDE10 LIGANDS - The present invention relates to novel, selective, radiolabeled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme 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, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.12-15-2011
20110305636COMPOUNDS, COMPOSITIONS, METHODS OF SYNTHESIS, AND METHODS OF TREATMENT - Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).12-15-2011
20110305635MYELIN DETECTION USING BENZOFURAN DERIVATIVES - The present invention relates to methods for the detection of myelin and a quantitative measurement of its local concentration in a sample using a benzofuran compound or its radioisotope derivatives. In one embodiment a method of myelin detection comprises identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, parenterally administering to the subject the benzofuran compound, or a derivative of the compound, and determining myelination in the subject by detecting binding in the sample. In one embodiment, the invention provides a method of imaging myelinated tissue in a surgical field of mammalian tissue comprising the steps of contacting the surgical site with the benzofuran compound or a radioisotope derivative of the compound, and detecting binding in the surgical site. In yet another embodiment, a method of imaging spinal cord and spinal nerve root tissue is provided comprising the steps of parenteral administration of a radioisotope derivative of the benzofuran compound and detecting the radioisotope derivative within the spinal canal and intervertebral foramen. Methods of quantification of binding of the benzofuran compound or its derivatives are also provided.12-15-2011
20090130020DIAGNOSTIC AGENTS FOR POSITRON EMISSION IMAGING USING F-18 RADIO-LABELED AMINO-ALCOHOLS - This invention relates to novel compounds F-18 radio-labeled amino-alcohols suitable for labeling or already labeled by 05-21-2009
20100135906IN VIVO IMAGING OF SULFOTRANSFERASES - Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 06-03-2010
20090068105ISATIN ANALOGUES AND USES THEREFOR - Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vivo imaging of apoptosis by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).03-12-2009
20120003153NOVEL INDOLYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL AND DIAGNOSTICAL USE - This invention relates to novel indolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.01-05-2012
20120207679Novel Heteroaryl Substituted Benzothiazoles - The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below:08-16-2012
20120207678Labeled Adenosine for Use in Positron Emission Tomography - Radiolabeled adenosine or radiolabeled adenosine containing molecules for use in positron emission tomography for assessing alterations in adenylate metabolism in a patient are provided.08-16-2012
20120301399METHOD FOR PRODUCTION OF RADIATION DIAGNOSTIC IMAGING AGENT - A method for producing a radioactive diagnostic imaging agent containing a radioactive 11-29-2012
20120058049CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT - Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula (I), or formula (II); wherein X is OH, C1-C6 alkoxyl, 18F, or 19F; Y and Z are independently selected from a C1-C6 alkyl, CpC6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H, X is not OH.03-08-2012
20120207677CATALYTIC RADIOFLUORINATION - One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.08-16-2012
2010011186418F-LABELLED FOLATES - The present invention is directed towards a new method of synthesis of 05-06-2010
20120070374Compounds for Non-Invasive Measurement of Aggregates of Amyloid Peptides - The invention relates to the provision of compounds, methods for producing them, and their use for imaging and quantification of aggregates of β-amyloid peptides in vivo. In a preferred aspect of the invention, a tracer is administered to humans and displays enrichment in body parts that are containing aggregates of amyloid peptides. Tracers of the invention can be used for non-invasive depiction and quantification of aggregates of β-amyloid peptides in humans affected with diseases that are characterized in the generation of such aggregates.03-22-2012
20110091382NOVEL IMAGING AGENTS FOR DETECTING NEUROLOGICAL DYSFUNCTION - Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.04-21-2011
20110104057Novel [F-18]-labelled L-glutamic acid and L-glutamine derivatives (II), their use and processes for their preparation - 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.05-05-2011
20120121509VITAL FLUOROCHROME CONJUGATES AND METHODS OF USE - The present invention provides compositions and methods based on vital fluorochrome conjugates that are useful for imaging dying and dead cells.05-17-2012
20110129419IN VIVO IMAGING AGENTS - The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.06-02-2011
20100247435MEASUREMENT OF NEURAL ACTIVITY - The present invention provides a method for determination of neural activity in a sample. The method of the invention is useful for the determination of neural activity in both in vivo and in vitro samples and is particularly useful in providing diagnostic information in subjects suspected to have a neurological condition that leads to disturbed neurological signalling. Also provided by the invention are compounds suitable for use in the method of the invention, and a pharmaceutical composition useful for carrying out the method of the invention.09-30-2010
20120128589Perfluoro Compounds For Use In Imaging - Described is the use of perfluoro-t-butyl cyclohexane in a contrast agent for molecular imaging, notably F MRI. Particularly, the perfluoro-t-butyl cyclohexane is present in the form of an aqueous emulsion of nanoparticles comprising the perfluoro compound as a core, and an emulsifying agent, such as a phospholipid, as a shell. The shell can be functionalized with other moieties that play a role in imaging, notably ligands for targeted binding and/or contrast agents or labels with a view to other imaging modalities. The latter particularly refers to 05-24-2012
20100209345Fluorinated Ligands for Targeting Peripheral Benzodiazepine Receptors - The invention provides fluorinated compounds of formula (I): The compounds may be used in diagnosis or treatment of a disorder in a mammal characterised by an abnormal density of peripheral benzodiazepine receptors.08-19-2010
20120219500DIAGNOSTIC AGENT FOR INFECTIOUS DISEASES - A diagnostic agent for infectious diseases which is capable of distinguishing among different kinds of bacterial species and which allows simple and non-invasive measurement and/or imaging in a short period of time is provided; and a screening method for a therapeutic agent for infectious diseases caused by microorganisms are provided.08-30-2012
20120213703RADIOLABELLED PDE10 LIGANDS - The present invention relates to novel, selective, radiolabelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme 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, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.08-23-2012
20120213702NOVEL DIAGNOSTIC AGENTS FOR THE NON-INVASIVE IN VIVO IMAGING OF AMINOPEPTIDASE N (APN/CD13) - The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO08-23-2012
20120177572AMYLOID IMAGING AS A SURROGATE MARKER FOR EFFICACY OF ANTI-AMYLOID THERAPIES - The present method for determining the efficacy of therapy in the treatment of amyloidosis involves administering to a patient in need thereof a compound of formula (I) or formula (II) or structures 1-45 and imaging the patient. After said imaging, at least one anti-amyloid agent is administered to said patient. Then, an effective amount of a compound of formula (I) or formula (II) or structures 1-45 is administered to the patient and the patient is imaged again. Finally, baseline levels of amyloid deposition in the patient before treatment with the anti-amyloid agent are compared with levels of amyloid deposition in the patient following treatment with the anti-amyloid agent.07-12-2012
20090060838SUBSTITUTED N-ARYL BENZAMIDES AND RELATED COMPOUNDS FOR TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES - Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable salts, their synthesis and labeling, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided. Also provided is the use of the disclosed compounds as imaging agents and methods for in vivo imaging and diagnosis of amyloid and synuclein diseases.03-05-2009
20120230914LABELING COMPOUND FOR PET - A labeling compound of the present invention includes a structure represented by formula (1)09-13-2012
20100221182LIGANDS FOR IMAGING CARDIAC INNERVATION - Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 09-02-2010
20120263646IMAGING AGENTS AND THEIR USE FOR THE DIAGNOSTIC IN VIVO OF NEURODEGENERATIVE DISEASES, NOTABLY ALZHEIMER'S DISEASE AND DERIVATIVE DISEASES - Disclosed are new imaging agents and their use for the in vivo diagnostic of neurodegenerative diseases, notably Alzheimer's disease and related diseases.10-18-2012
20120321561CANCER DIAGNOSIS AND IMAGING - The present invention provides a method for imaging a disease or condition in a mammal which includes the steps of; administering a therapeutically effective amount of a cell cycle inhibitor to effectively stop proliferation of eukaryotic cells at a cell cycle checkpoint between the G1 and S phase, stopping administration of the cell cycle inhibitor for a period of time, administering a marker to the mammal and imaging the mammal.12-20-2012
20110236312NUCLEOSIDE ANALOGUES USEFUL AS POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENTS - The invention provides compounds that comprise a 4′-thio nucleoside that is a derivative of 4′-thiothymidine or 4′-thio-2′-deoxyuridine comprising a positron or single photon emitting radioisotope or corresponding non-radioactive isotope attached via a triazole link to the N-3 position. Methods for preparing such compounds and uses of the compounds in medicine are also provided.09-29-2011
20110250136FLUORINATED BENZOTHIAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND IMAGING AGENT FOR DIAGNOSING ALTZHEIMER'S DISEASE USING THE SAME - The present invention relates to fluorinated benzothiazole derivatives, a preparation method thereof, and an imaging agent for diagnosing Alzheimer's disease using the same, and more particularly to fluorinated benzothiazole derivatives represented by Chemical Formula 1, derivatives of Chemical Formula 2 as a starting material for preparation thereof, a preparation method thereof, and an imaging agent for diagnosing Alzheimer's disease using fluorinated benzothiazole derivatives with a strong binding force to beta-amyloid plaque, which is a kind of biomarker for Alzheimer's disease. According to the present invention, fluorine-labeled benzothiazole derivatives, which have been difficult to synthesize by conventional methods, may be obtained by simple processes and the thus-obtained benzothiazole derivatives may be useful in diagnosing the presence and severity of Alzheimer's disease.10-13-2011
20120328521FORMULATIONS SUITABLE FOR PET IMAGING WITH HYDROPHOBIC PET AGENTS - The invention is directed to formulations of lipophilic Amyloid βeta ligand stilbene based derivatives and more particularly to formulations which are administrable parentally e.g. intravenously wherein the lipophilic Amyloid βeta ligand stilbene based derivative is a 12-27-2012
20100215579PHEN-NAPHTHALENE AND PHEN-QUINOLINE DERIVATIVES AND THEIR USE FOR BINDING AND IMAGING AMYLOID PLAQUES - This invention relates to methods of imaging amyloid deposits, radiolabeled compounds, and methods of making radiolabeled 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 methods of delivering therapeutic agents to amyloid deposits.08-26-2010
20120100073PET RADIOTRACERS FOR IMAGING FATTY ACID METABOLISM AND STORAGE - Fatty acid analogue (FAA) molecules comprising positron-emitting radionuclides, salts thereof, and FAA-triglycerides are disclosed. Also disclosed are methods of synthesis, and methods of imaging distribution and metabolism of fatty acids and fatty acid triglycerides.04-26-2012
20120288445RADIOLABELLING - Compounds of the formula (I) are disclosed:11-15-2012
20120288444SINGLE DIASTEREOMERS OF 4-FLUOROGLUTAMINE AND METHODS OF THEIR PREPARATION AND USE - The present invention is directed single diasteromers of 4-fluoroglutamine having a diastereomeric excess of at least 80%. Methods of preparing the single diastereomers are also described, as well as methods of using the single diastereomers of radiolabeled 4-fluoroglutamine as imaging agent is also described.11-15-2012
20130011336IMAGING AGENTS OF FIBROTIC DISEASES - Agents and methods for imaging a cell and/or a portion of tissue characterized by fibrosis, as well as to agents and methods for determining and/or diagnosing fibrotic diseases are disclosed herein. Also disclosed herein are polymer conjugates that can include a detectable label, a retinoid and a polymer. The polymer conjugates can be used to image a portion of tissue, deliver a detectable label to a portion of tissue or a cell and/or diagnosis a condition or disease.01-10-2013
20130177501IN VIVO IMAGING METHOD OF MOOD DISORDERS - The present invention provides a method useful in the diagnosis and/or monitoring of mood disorders wherein there is an abnormal expression of PBR. The method of the invention is useful in the differential diagnosis of said mood disorders and other conditions where there is no abnormal expression of PBR but where the symptoms may be similar to those of said mood disorder.07-11-2013
20100028258Radioactive Diagnostic Imaging Agent - A composition including a radioactive fluorine-labeled amino acid compound is provided, which can be prevented from radiolysis. Disclosed is a composition which includes a solution containing a radioactive fluorine-labeled amino acid compound as an effective ingredient, in which the pH value of the solution is kept at 2.0-5.9, more preferably 2.0-4.9 in order to inhibit radiolysis. Also, it is possible to further inhibit radiolysis by adding thereto a pharmaceutical additive capable of inhibiting radiolysis, such as a sugar, a sugar alcohol and a sugar lactone, whilst the pH is kept at 2.0-5.9.02-04-2010
20120093727COMPOSITIONS AND METHODS FOR IN VIVO IMAGING OF MYELIN IN THE PERIPHERAL NERVOUS SYSTEM - A method of detecting and/or labeling myelin in an animal's peripheral nervous system tissue includes administering to the animal a fluorescent stilbenzene derivative and visualizing the animal's peripheral nervous system tissue using an in vivo imaging modality.04-19-2012
20120093726Radiolabeled Fluorine Derivatives of Methionine - The invention provides compound which is an 04-19-2012
20120251449ALDH: A COMPOUND FOR CANCER STEM CELL IMAGING - The present invention claims fluoro- & iodo-containing aldehydes as ALDH substrates for use as diagnostic imaging agents or as therapeutic agents. The aldehydes are both directly and indirectly attached to an aromatic or a straight chain ring. ALDH activity was monitored either by the formation of acid-product or consumption of aldehyde substrates.10-04-2012
20120251448Compounds for Use in the Detection of Neurodegenerative Diseases - Provided are the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of pathological characteristics unique to synuclein diseases, such as Parkinson's disease.10-04-2012
20130115168Catalytic Radiofluorination - One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.05-09-2013
20130101508STABILIZATION OF RADIOPHARMACEUTICAL COMPOSITIONS USING ASCORBIC ACID - Radiopharmaceutical compositions, and related methods, useful for medical imaging are provided. The radiopharmaceutical compositions include one or more radiopharmaceutical compounds, together with a stabilizer comprising ascorbic acid, wherein the pH of said composition is within the range of about 3.5-5.5.04-25-2013
20130101510METHODS OF TREATING PARKINSON'S DISEASE USING VIRAL VECTORS - Methods of delivering viral vectors, particularly recombinant AAV virions, to the CNS are provided. Also provided are methods of treating Parkinson's Disease.04-25-2013
20110243846BENZOTHIAZOLE AMIDES FOR DETECTION OF AMYLOID BETA - This invention relates to compounds (benzothiazoles) suitable for labelling or already labelled by 10-06-2011
20130149243METHOD FOR PRODUCTION OF F-18 LABELED GLUTAMIC ACID DERIVATIVES - This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives.06-13-2013
20130149244COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS - The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 06-13-2013
20120276007IMAGING AGENTS AND METHODS OF IMAGING NAALADASE OR PSMA - 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.11-01-2012
20120276006CONTRAST AGENTS FOR MYOCARDIAL PERFUSION IMAGING - The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.11-01-2012
20130156699RADIOLABELED COMPOUNDS AND USES THEREOF - The present invention relates to Radiolabeled Compounds labeled with fluorine, bromine, iodine, carbon, or tritium isotopes and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.06-20-2013
20130156700FLUORINE-18 AND CARBON-11 LABELED RADIOLIGANDS FOR POSITRON EMISSION TOMOGRAPHY (PET) IMAGING FOR LRRK2 - A method for positron emission tomography (PET) imaging of LRRK2 in tissue of a subject, the method comprising: administering a compound of formula I, formula II or formula III, or a pharmaceutically acceptable salt thereof to the subject, wherein the compound includes at least one C06-20-2013
20130156701METHOD OF PREPARING ETHACRYNIC AMIDE DERIVATIVES AND APPLICATION THEREOF - The present invention provides a method for preparing [06-20-2013
20120282180Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof - The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.11-08-2012
20130183240IN VIVO IMAGING METHOD FOR CANCER - The present invention provides a method useful in the diagnosis and monitoring of cancer wherein there is an abnormal expression of PBR. The method of the invention is particularly useful in evaluating the severity of the cancer, e.g. PBR expression correlates with cell proliferation rates, metastatic potential, tumour aggressiveness, malignancy progression. The method of the invention can therefore be applied in the determination of likely disease progression and in making an associated prognosis. Furthermore, the method of the invention can find use in determining the likely success of certain therapeutic approaches, or in the evaluation of the efficacy of certain proposed new treatments.07-18-2013
20110311447Compounds comprising 4-benzoylpiperidine as a Sigma-1-selective ligand - Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for σ12-22-2011
20120003154ARYLOXYANILIDE DERIVATIVES - The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.01-05-2012
20120020884INDOLE DERIVATIVES - An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.01-26-2012
20130101509IMAGING AND RADIOTHERAPY METHODS - The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.04-25-2013
20130202530NOVEL RADIOTRACER - Novel radiotracer(s) for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer—primary tumor, nodal disease or metastases). The present invention also describes intermediate(s), pre-cursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).08-08-2013
20090297447SYNTHESIS AND EVALUATION OF 18F-LABELLED-ALKYL-1-[(1R)-1-PHENYLETHYL]-1H-IMIDAZOLE-5-CARBOXYLATE AS A TRACER FOR THE QUANTIFICATION OF BETA-11-HYDROXYLASE ENZYME IN THE ADRENAL GLANDS - Radioactively labeled derivatives of (R)-3-(1-phenylethyl)-3H-imidazole-4-carboxylic acid esters and one-step methods for preparing these compounds are provided. The radioactively labelled compounds, and pharmaceutical acceptable salts and solvates are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET) for the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Associated kits and method for PET studies are also provided.12-03-2009
20130209363METHOD FOR PRODUCTION OF F-18 LABELED AMYLOID BETA LIGANDS - This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.08-15-2013

Patent applications in class Fluorine