This invention provides an alternative PET radiotracer using human serum albumin radio labelled with the gallium radioisotope 68Ga (68Ga-HSA) via a chelator conjugate of HSA with the chelator NOTA. The agents are useful as markers of blood volume, haemodynamic and lymphatic function and tissue inflammation in vivo. The other aspects of the invention are an automated kit-type preparation Of 68Ga-HSA at room temperature, in the range of about 19-25 ˚C, providing 68Ga-HSA on demand and an automated kit-type preparation of 68Ga- labeled HSA macroaggregates using microwave heating.
The invention provides a preparation of a ventilation/perfusion imaging agent comprising positron emitting 68Ga, produced, from a 68Ge/68Ga generator. The agent provides high quality images and quantification that make PET examinations available to improve the management of patients under critical conditions such as pulmonary embolism. Assessment of the ventilation distribution is part of the evaluation of lung function prior to lung resection and is also part of the diagnosis of pulmonary emboli.
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
The present invention relates to a method of obtaining 68Ga from a 68Ge/68Ga radioisotope generator and a method of preparing 68Ga-radiolabelled complexes using the obtained 68Ga. The method comprises elution of the generator with an aqueous chloride ion solution. The invention further relates to an apparatus for carrying out the 68Ga metal complex formation.
A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes
C01G 15/00 - Compounds of gallium, indium, or thallium
The present invention provides radioactive gallium complexes which comprise DOTA- biotin conjugates, incorporating a linker group. Also described are radiopharmaceutical compositions, and methods and uses of the complexes for in vivo imaging involving pre-targeting with avidin.
The present invention relates to the field of [18F] radiofluorination chemistry for the preparation of Positron Emission Tomography (PET) radioligands and [18F] radiofluorinating reagents. The invention further provides kits for preparation of the same.
A method and apparatus are provided for reducing motion related imaging artifacts. The method includes determining an internal motion for of two regions of the object, each region having a different level of motion, scanning the first region using a first scan protocol based on the motion, scanning a second region using a second different scan protocol based on the motion, and generating an image of the object based on the first and second regions.
The present invention relates to 18F radiochemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.
Naphthoxazine derivatives which are selective ligands for the dopamine D2 receptor and which carry an 18F radiolabel 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.
The present invention provides isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising said derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing said derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 51/00 - Preparations containing radioactive substances for use in therapy or testing in vivo
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
10.
SYSTEM FOR DISPENSING A FLUID IN NON-CONTROLLED ENVIRONMENTS
The present invention provides a dispenser cassette (110) which provides at least one product dispense vial (122) to be filled. The cassette provides a filtrate conduit (128) extending between the dispense vial and a filter unit (116) so that flowpath (120) of the filtrate conduit and the dispense vial is provided and maintained as an environmentally-controlled, or GMP-compliant, volume. The resulting product dispensed into the dispense vial is thus dispensed in a GMP-compliant environment.
B65B 3/00 - Packaging plastic material, semiliquids, liquids or mixed solids and liquids, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans or jars
B65B 3/12 - Methods of, or means for, filling the material into the containers or receptacles by application of pressure to material mechanically, e.g. by pistons or pumps
B65B 55/02 - Sterilising, e.g. of complete packages
Provided herein are methods for introducing flυorine atom onto a biomolecule comprising: (i) providing a linker comprising a thiol-reactive teminus and an azido/alkyne-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a biomolecule comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the azido/alkyne-reactive terminus of the linker with a fluorine-substituted azide or alkyne respectively. Also provided are compositions and method of synthesis of bifunctional linkers and bioconjugates as well as radio-diagnostic agents comprising fluorine-labeled biomolecules.
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.
A microscale solution for conducting [18F] fluoride phase transfer and subsequent radiosysnthesis of 2- [18F] FDG that eliminates the azeotropic drying process. [18F] fluoride phase transfer is performed using an inexpensive disposable microchip (310). Additionally, each subsequent each step may be performed on the same single microchip (310). The integrated microchip (310) provides a microchannel (312) having a first resin chamber, or reservoir, (314) for 18F transfer, a labelling reactor (316), a deprotection reactor (318), and a second resin chamber, or reservoir, (320) for purification.
The method calculates a scatter estimate for scatter correction of detection data from a subject in a positron emission tomographic scanner. The detection data represent the scattered events and unscattered events of annihilation photons emitted in the subject. The method uses the following steps: - determine an estimate of the unscattered events; - determine a simulation of the scattered events; - determine a value of a scaling factor by fitting the sum of the estimate of the unscat-tered events and a product of the scaling factor and the simulation of the scattered events to the detection data; and - determine the scatter estimate as the product of the scaling factor having said value and the simulation of the scattered events.
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.
C07C 235/56 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to methods of synthesising radiolabelled compounds, to the precursors useful in such methods and to the radiolabelled compounds obtainable by such methods. More particularly, the present invention relate to methods, precursors and radiolabelled compounds useful in Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) especially for imaging neuroreceptors with radiolabelled agonists.
The present invention provides a method and an apparatus for extracting an isotope from a gas. More specifically, the present invention depicts a system that has been devised which provides [18F] fluoride from a cyclotron target in non-aqueous media.
G21G 1/10 - Arrangements for converting chemical elements by electromagnetic radiation, corpuscular radiation, or particle bombardment, e.g. producing radioactive isotopes outside of nuclear reactors or particle accelerators by bombardment with electrically-charged particles
G21G 4/08 - Radioactive sources other than neutron sources characterised by constructional features specially adapted for medical applications
The invention relates to methods and apparatus for drying [18F]fluoride which comprises (i) passing a [18F]fluoride solution comprising water, a solvent, [18F]fluoride, and a cationic counterion through a narrow bore vessel at elevated temperature such that the water and solvent are vaporised forming a vaporised component, and (ii) collecting the resulting vaporised component by condensing into a collection vessel.
The invention relates to methods and apparatus for purifying a radiolabelled compound. The method comprises (i) passing a crude reaction mixture comprising the desired radiolabelled compound and one or more contaminants in a solvent through a narrow bore vessel at elevated temperature such that the organic solvent and either the radiolabelled compound or one or more contaminants is vaporised forming a vaporised component, and (ii) collecting the resulting vaporised component by condensing into a collection vessel.
The invention relates to methods and apparatus for labelling a biologically active vector such as a peptide with reporter moiety such as a radionuclide. The methods comprise reaction of a compound of formula (I) with a compound of formula (II): R*-L2 -N3 (II) or, a compound of formula (III) with a compound of formula (IV) wherein: L1, L2, L3, and L4 are each Linker groups; R* is a reporter moiety; in a narrow bore copper vessel. Microfluidic devices for performing the methods of the invention are also claimed.
The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I): with a compound of formula (II) or, a compound of formula (III): with a compound of formula (IV): in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.
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.
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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.
C07B 59/00 - Introduction of isotopes of elements into organic compounds
C07C 213/08 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C07C 215/14 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to hydrocarbon groups substituted by amino groups
C07C 331/28 - Isothiocyanates having isothiocyanate groups bound to carbon atoms of six-membered aromatic rings
C07D 205/02 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
The invention relates to novel 18F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. The 18F-labelled compounds of the invention comprise a ⏧18F]fluoroalkenyl group.
C07D 277/66 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
C07C 255/42 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
C07D 217/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
The invention relates to new processes for preparation of 18F-fluoroalkyl halides suitable for use in labelling of Positron Emission Tomography (PET) radiotracers. The process of preparation comprises the step of reacting a 18F-fluoroacylhalide with Wilkinson's catalyst.
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.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61P 25/00 - Drugs for disorders of the nervous system
The method calculates a scatter estimate for annihilation photons in a subject having a distribution of attenuation. The method can be used for scatter correction of detection data from a positron emission tomographic scanner. The method uses the following steps: - select a first scatter point S1 and a second scatter point S2, - determine a first scatter probability for scattering of a photon at scatter point S1 and a second scatter probability for scattering of a photon at scatter point S2, - determine an integral of the attenuation over a line connecting S1 and S2, - multiply the integral and the scatter probabilities and use the product in the calculation of the scatter estimate.
The invention provides a compound of formula (I); or a salt or solvate thereof, wherein: R1 is hydrogen or C1-4alkyl; R2 and R4 are each independently selected from C1-4 alkyl, ⏧11C] C1 4alkyl, and ⏧18F]-C1-4 fluoroalkyl provided that at least one of R2 and R4 is ⏧11C] C1 4alkyl or ⏧18F]-C1-4 fluoroalkyl; and R3 is halo. Such compounds having use for imaging central nervous system receptors.
C07C 279/18 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
C07C 277/08 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
C07B 59/00 - Introduction of isotopes of elements into organic compounds
30.
METHOD OF AND SOFTWARE FOR CONDUCTING MOTION CORRECTION IN TOMOGRAPHIC SCANNING AND SYSTEM FOR TOMOGRAPHIC SCANNING USING THE METHOD
During data acquisition in a tomographic scan of a subject unscattered events and scatter events are collected. The data are corrected for the scatter events and movement of the subject during the scan. A scatter estimate is derived for use in the reconstruction of an image of the subject; a first step in the derivation has a first dependence on the movement of the subject. The image of the subject is derived from the detected events using the scatter estimate; a second step in this derivation has a second dependence on the movement of the subject, the dependence being different from that of the first step.
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