141 |
Usage of low to medium-pressure liquid chromatography for the purification of radiotracers |
US13383224 |
2010-07-06 |
US08968701B2 |
2015-03-03 |
Holger Siebeneicher; Keith Graham; Mathias Berndt |
The invention relates to a process for the production of radiotracers. In particular, this invention relates the isolation of radiotracers with containers filled with a stationary phase. |
142 |
METHOD FOR PREPARING FLUORINE-18 ELUENT WITH ADJUSTED PH, AND METHOD FOR LABELLING FLUORINE-18 USING SAME |
US14375412 |
2012-12-21 |
US20150045548A1 |
2015-02-12 |
Sang Ju Lee; Seung Jun Oh; Dae Hyuk Moon; Jin Sook Ryu; Jae Seung Kim; Jong Jin Lee |
The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies. |
143 |
COMPOUNDS FOR USE IN IMAGING, DIAGNOSING AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM OR OF TUMORS |
US14336424 |
2014-07-21 |
US20150030539A1 |
2015-01-29 |
Lutz LEHMANN; Andrea THIELE; Tobias HEINRICH; Thomas BRUMBY; Christer HALLDIN; Balazs GULYAS; Sangram NAG |
This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET). |
144 |
RADIOLABELED AMINO ACIDS FOR DIAGNOSTIC IMAGING |
US14115471 |
2012-04-30 |
US20150011773A1 |
2015-01-08 |
Mathias Berndt; Andre Muller; Heribert Schmitt-Willich; Timo Stellfeld; Georg Kettschau; Thomas Brumby; Keith Graham; Lutz Lehmann; Jorma Hassfeld; Martin Kruger |
This invention relates to novel compounds suitable for labeling by 18F and to the corresponding 18F labeled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET). |
145 |
Automatic synthesizer apparatus for producing radiopharmaceutical tumor imaging agent Gallium-68-DOTATATE and method thereof |
US13916599 |
2013-06-13 |
US20140369928A1 |
2014-12-18 |
Ming-Hsin Li |
The invention provides an automatic synthesizer apparatus and method for producing radiopharmaceutical tumor imaging agent Gallium-68-DOTATATE with one button control process to effectively isolate the medication in vials from the contamination of environment and manual operations, saving the costs of investment in production with alleviation of the critical standard required for the environmental equipments to be used for production. |
146 |
Process for producing hydrogen or heavy hydrogens, and hydrogenation (protiation, deuteration or tritiation) of organic compounds using same |
US13817637 |
2011-08-16 |
US08871980B2 |
2014-10-28 |
Hironao Sajiki; Yasunari Monguchi; Yoshinari Sawama; Shinichi Kondo |
An object is to provide a process for providing hydrogen or heavy hydrogens conveniently without the necessity of large-scale equipment and a process capable of performing hydrogenation (protiation, deuteration or tritiation) reaction conveniently without the use of an expensive reagent and a special catalyst. The production process includes a process for producing hydrogen or heavy hydrogens, containing subjecting water or heavy water to mechanochemical reaction in the presence of a catalyst metal, and a process for producing a hydrogenated (protiated, deuterated or tritiated) organic compound, containing subjecting an organic compound and water or heavy water to mechanochemical reaction in the presence of a catalyst metal. |
147 |
METHODS FOR THE SYNTHESIS OF 13C LABELED IODOTRIDECANE AND USE AS A REFERENCE STANDARD |
US14359096 |
2012-11-16 |
US20140309464A1 |
2014-10-16 |
M. Amin Khan; Paul L. Wood; Dayan Goodenowe |
A method for preparing 13C labeled iodotridecane represented by Formula A. The method comprises the conversion of 13C labeled propargyl alcohol to 13C labeled iodotridecane via alkylation of propargyl alcohol with iododecane. |
148 |
CALIBRATION AND NORMALIZATION SYSTEMS AND METHODS FOR RADIOPHARMACEUTICAL SYNTHESIZERS |
US14348189 |
2012-09-28 |
US20140243500A1 |
2014-08-28 |
Torgrim Engell; Julian Grigg |
The present invention relates to calibration and normalization systems and methods for ensuring the quality of radiopharmaceuticals during the synthesis thereof, such as radiopharmaceuticals used in Positron Emission Tomography (PET) and Single-Photon Emission Computed Tomography (SPECT). |
149 |
Compounds for use in imaging, diagnosing and/or treatment of diseases of the central nervous system or of tumors |
US12256957 |
2008-10-23 |
US08784775B2 |
2014-07-22 |
Lutz Lehmann; Andrea Thiele; Tobias Heinrich; Thomas Brumby; Christer Halldin; Balazs Gulyas; Sangram Nag |
This invention relates to novel compounds suitable for labeling or already labeled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET). |
150 |
GLUTATHIONE ALKYLESTER ISOTOPOLOGUE AND METHOD FOR DETECTING REACTIVE METABOLITE |
US14117169 |
2012-05-21 |
US20140193847A1 |
2014-07-10 |
Toshikazu Yamaoka |
[Problem] To provide a novel isotope-labeled compound that can be used as a trapping agent and that is useful for picking out drug-candidate compounds that produce reactive metabolites.[Solution] Provided is a glutathione alkylester isotopologue represented by general formula (1). In formula (1), R1 represents a linear or branched alkoxy group in which at least one of carbon, oxygen, and hydrogen atoms contained therein is isotope-labeled and which has 1 to 8 carbon atoms or a cycloalkoxy group in which at least one of carbon, oxygen, and hydrogen atoms contained therein is isotope-labeled and which has 3 to 8 carbon atoms. |
151 |
Nucleophilic fluorination of aromatic compounds |
US13054458 |
2009-07-13 |
US08674101B2 |
2014-03-18 |
Nagichettiar Satyamurthy; Jorge R. Barrio |
Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa. |
152 |
Method for Preparing Formamide Compounds |
US13805899 |
2012-04-04 |
US20140018576A1 |
2014-01-16 |
Thibault Cantat; Christophe Gomes; Olivier Jacquet |
The present invention relates to a method for preparing formamide compounds using carbon dioxide, and to the use of said method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides and fertilisers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides and fertilisers which includes a step of preparing formamide compounds by the method according to the invention. |
153 |
Method and Kit for Preparing a Radiopharmaceutical |
US13475759 |
2012-05-18 |
US20130310537A1 |
2013-11-21 |
Dirk Müller |
The invention relates to a method and a kit for preparing a radiopharmaceutical, the method comprising the steps: elution of a 68Ge/68Ga-Generator using hydrochloric acid as an eluent for obtaining a generator eluate comprising 68Gallium, feeding the generator eluate through a cation exchange cartridge, which collects the 68Gallium, separating the used eluent, eluting the 68Gallium from the cation exchange cartridge using a solution comprising sodium chloride and hydrochloric acid and feeding the resulting eluate into an aqueous precursor mixture comprising at least a labelling precursor thereby forming a reaction solution. |
154 |
POLYMER PRECURSORS OF RADIOLABELED COMPOUNDS, AND METHODS OF MAKING AND USING THE SAME |
US13776039 |
2013-02-25 |
US20130303757A1 |
2013-11-14 |
Duncan H. HUNTER; Mustafa JANABI |
One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds. |
155 |
Ionizable isotopic labeling reagents for relative quantification by mass spectrometry |
US13155682 |
2011-06-08 |
US08563777B2 |
2013-10-22 |
Lloyd M. Smith; Michael R. Shortreed; Brian L. Frey; Margaret F. Phillips; Joshua J. Coon; Shane M. Lamos; Casey J. Krusemark; Peter J. Belshaw; Madhusudan Patel; Neil L. Kelleher |
Relative quantification of metabolites by Electrospray Ionization Mass Spectrometry (ESI-MS) requiring a mechanism for simultaneous analysis of multiple analytes in two or more samples. Labeling reagents that are reactive to particular compound classes and differ only in their isotopic compositions facilitate relative quantification. Heavy and light isotopic forms of methylacetimidate were synthesized and used as labeling reagents for quantification of amine-containing molecules. Heavy and light isotopic forms of formaldehyde and cholamine were also synthesized and used independently as labeling reagents for quantification of amine-containing and carboxylic acid-containing molecules, such as found in biological samples. The labeled end-products are positively charged under normal acidic conditions involving conventional Liquid Chromatography Mass Spectrometry (LC/MS) applications. Labeled primary and secondary amine and carboxylic acid end-products generated higher signals concerning mass-spectra than pre-cursor molecules and improved sensitivity. Improved accuracy concerning relative quantification was demonstrated by mixing heavy and light labeled Arabidopsis extracts in different ratios. |
156 |
BIOTIN STANNANE FOR HPLC-FREE RADIOIODINATION |
US13435142 |
2012-03-30 |
US20130261311A1 |
2013-10-03 |
Randall Lee Carter; Bruce Fletcher Johnson; Anup Sood; Michael James Rishel; John Fitzmaurice Valliant; Karin Ann Stephenson; Tao Wu; Yang Yang |
The present teachings provide methods that enable the preparation and purification of radioiodinated vectors without the need for HPLC purification, as well as novel precursors which include biotin-like substituents useful in such methods. |
157 |
PHARMACEUTICAL COMPOSITIONS COMPRISING POH DERIVATIVES |
US13818972 |
2011-08-26 |
US20130210877A1 |
2013-08-15 |
Thomas Chen; Daniel Levin; Satish Puppali |
The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection. |
158 |
METHOD FOR PRODUCTION OF F-18 LABELED AMYLOID BETA LIGANDS |
US13701595 |
2011-05-30 |
US20130172620A1 |
2013-07-04 |
Mathias Berndt; Matthias Friebe; Christina Hultsch; Fabrice Samson; Marianne Patt; Andreas Schildan; Christoph Smuda |
This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives. |
159 |
Fluoridation of iodonium salts |
US13058338 |
2009-08-13 |
US08466313B2 |
2013-06-18 |
John Woodcraft |
The present invention provides an improved method for fluoridation of an iodonium salt wherein a solution of the iodonium salt comprising a free radical trap is stored before the reaction is carried out. The method of the invention may be automated, which is particularly convenient when the method of the invention is radiofluoridation. As such the present invention also provides a cassette comprising the iodonium salt solution suitable for carrying out the method of the invention on an automated synthesizer. |
160 |
Prosthetic groups attached to stannyl polymer in the synthesis of radiopharmaceuticals |
US10555248 |
2004-04-30 |
US08435492B2 |
2013-05-07 |
Duncan Hunter; M. Karen J. Gagnon |
The present invention relates to compositions and methods for preparing radiopharmaceutical compounds in high chemical-purity and isotopic-purity. The present invention provides polymer-bound precursors to radiopharmaceutical compounds that can be converted to radiopharmaceutical compounds in one step. In a preferred embodiment, a radiopharmaceutical precursor is bound to a polymeric support via a prosthetic group comprising an alkenyl-tin bond. The radiopharmaceutical precursor is converted to a radiopharmaceutical compound in one step involving cleavage of the alkenyl-tin bond and incorporation of a radioisotope to form the radiopharmaceutical compound. Importantly, the polymeric support containing the toxic tin by-product can be easily removed from the radiopharmaceutical compound by filtration. The present invention can be used to install a large number of different radioisotopes. In a preferred embodiment, the radioisotope is 211At, 123I or 131I. |