子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 161 | METHOD FOR PRODUCING A RADIOACTIVE TRACER | US13583521 | 2011-03-07 | US20130053607A1 | 2013-02-28 | Céline Perollier; Kaynoush Naraghi; Sami Bayoudh |
| A method for preparing a radioactive tracer provided with a radioactive fluorine isotope, including providing a precursor of the radioactive tracer, comprising at least one leaving group completely or partially formed by a labelling entity, wherein said leaving group can be moved by a fluoride ion, providing a molecularly imprinted polymer dedicated to the molecular recognition of at least the aforementioned labelling entity, exposing the precursor to a radioactive fluoride ion source under conditions suitable for movement of the leaving group by a radioactive fluoride ion, placing the mixture resulting from step (iii) in contact with the molecularly imprinted polymer under conditions suitable for the recognition of the labelling entity, and obtaining a solution containing the radioactive tracer provided with a radioactive isotope of fluorine obtained at the end of step (iii). | ||||||
| 162 | Polymer precursors of radiolabeled compounds, and methods of making and using the same | US13174154 | 2011-06-30 | US08383083B2 | 2013-02-26 | 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. | ||||||
| 163 | C-11 Cyanide Production System | US13584033 | 2012-08-13 | US20130045151A1 | 2013-02-21 | Dohyun Kim; David Alexoff; Sung Won Kim; Jacob Hooker; Richard A. Ferrieri |
| A method for providing 11C-labeled cyanides from 11C labeled oxides in a target gas stream retrieved from an irradiated high pressure gaseous target containing O2, wherein 11C labeled oxides are reduced with H2 in the presence of a nickel catalyst under a pressure and a temperature sufficient to form a product stream comprising at least about 95% 11CH4, the 11CH4 is then combined with an excess of NH3 in a carrier/reaction stream flowing at an accelerated velocity and the combined 11CH4 carrier/reaction stream is then contacted with a platinum (Pt) catalyst particulate supported on a substantially-chemically-nonreactive heat-stable support at a temperature of at least about 900° C., whereby a product stream comprising at least about 60% H11CN is provided in less than 10 minutes from retrieval of the 11C labeled oxide. | ||||||
| 164 | ISOTOPICALLY LABELED CHEMICALLY STABLE REAGENTS AND PROCESS FOR THE SYNTHESIS THEREOF | US13644925 | 2012-10-04 | US20130030184A1 | 2013-01-31 | Jerry Scot Pounds |
| A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naCbH3 (I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C3H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg—and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substitute containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl. | ||||||
| 165 | DEVICES AND METHODS FOR REDUCING RADIOLYSIS OF RADIOISOTOPES | US13173978 | 2011-06-30 | US20130004414A1 | 2013-01-03 | Christian Friedrich Peter Rensch; Marko Klaus Baller; Christoph Boeld; Victor Donald Samper; Johan Urban Ingemar Ulin |
| Disclosed are microfluidic devices and kits for containing radioisotopes. The devices and kits comprises at least one confining geometry having a cross-section dimension below the beta(+) or beta(−) range of a radioisotope, when containing the radioisotope configured in such a way that that neighboring segments of the confining geometries are isolated from its nearest neighbor such that no measurable kinetic positron energy transfer occurs between the segments when containing the radioisotope. Methods of storage and synthesis of radiopharmaceuticals are also disclosed. In another aspect, the present invention relates to methods of storing radiotracers and synthesizing radiopharmaceuticals, using the aforementioned device. The radiotracers and radiopharmaceuticals comprises 18F, 11C, 14C, 99mTc, 123I, 125I, 131I, 68Ga, 67Ga, 15O, 13N, 82Rb, 62Cu, 32P, 89Sr, 153Sm, 186Re, 201Tl, 111In, or combinations thereof. | ||||||
| 166 | System, Device and Method for Preparing Tracers and Transferring Materials During Radiosynthesis | US13445147 | 2012-04-12 | US20120283490A1 | 2012-11-08 | Umesh B. Gangadharmath; Joseph C. Walsh; Hartmuth C. Kolb; Ricardo Rodriguez; Arkadij M. Elizarov; Carroll Edward Ball |
| A system, apparatus, and method for transferring chemical solutions and synthesizing a tracer. For transferring chemical solutions, the system comprises a primary container; a secondary container; a first line in communication with the primary container and the secondary container. The first line facilitates the flow of gas and/or liquid between the primary container and the secondary container. A valve located upstream of the secondary container and downstream of the primary container regulates flow within the first line; a second line in communication with the secondary container. For synthesizing a tracer, the system includes a source of a solution having a radionuclide. A first container has a tracer precursor and is in communication with the source of solution. | ||||||
| 167 | Method of rapid methylation, kit for preparing PET tracer and method of producing PET tracer | US12438711 | 2007-08-24 | US08288604B2 | 2012-10-16 | Masaaki Suzuki; Hisashi Doi; Hideo Tsukada |
| A method of rapid methylation of an aromatic compound or an alkenyl compound, which is capable of obtaining an aromatic compound or an alkenyl compound labeled with a methyl group or a fluoromethyl group under a mild condition rapidly in high yield using an organic boron compound whose toxicity is not so high as a substrate. A kit for preparing a PET tracer and a method of producing a PET tracer can be practiced using the rapid methylation method. In an aprotic polar solvent, methyl iodide or X—CH2F (wherein X is a functional group which can be easily released as an anion), and an organic boron compound in which an aromatic ring or an alkenyl group is attached to boron are subjected to cross-coupling in the presence of a palladium(0) complex, a phosphine ligand, and a base. | ||||||
| 168 | Process for production of radioactive-fluorine-labeled organic compound | US12747726 | 2008-12-16 | US08269035B2 | 2012-09-18 | Fumie Kurosaki; Masahito Toyama; Akio Hayashi |
| A process for production of a radioactive fluorine-labeled organic compound is provided which can improve the yield of radioactive fluorination. Provided is a process in which a compound represented by the following formula (1): (wherein R1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R2 is a straight or branched haloalkylsulfonic acid substituent with 1-10 carbon atoms, a straight or branched alkylsulfonic acid substituent with 1-10 carbon atoms, a fluorosulfonic acid substituent or an aromatic sulfonic acid substituent, and R3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 18F ions and potassium ions, so as to effect labeling with a radioactive fluorine, wherein the heating temperature is 40-90° C., and the concentration of the phase transfer catalyst in the inert organic solvent is 70 mmol/L or more. Preferably, the molar ratio of the phase transfer catalyst is 0.7 or more relative to the compound of the formula (1), and the concentration of the compound of the formula (1) in the inert organic solvent is 50 mmol/L or more. | ||||||
| 169 | METHOD FOR PRODUCING A RADIOACTIVELY MARKED CARBOXYLATE | US13387921 | 2010-07-07 | US20120186988A1 | 2012-07-26 | Markus Kinzl; Oliver Lade; Christian P. Schultz; Arno Steckenborn; Frank Thalmann |
| A method produces a radioactively marked carboxylate, at least one precursor molecule of the carboxylate being prepared in a solvent including a conductive salt. Radioactively marked carbon dioxide is fed into the solvent. The precursor molecule is electrochemically reacted with the radioactively marked carbon dioxide to form the radioactively marked carboxylate. The radioactively marked carbon dioxide is completely dissolved in the solvent when the precursor molecule is reacted. The radioactively marked carbon dioxide is used for electrochemically synthesizing a radioactively marked carboxylate, the carbon dioxide being completely dissolved in a solvent during synthesis. A microstructure is used for electrochemically synthesizing the radioactively marked carboxylate, radioactively marked carbon dioxide being reacted. | ||||||
| 170 | Microfluidic chemical reaction circuits | US11792168 | 2005-12-05 | US08206593B2 | 2012-06-26 | Chung-cheng Lee; Guodong Sui; Arkadij Elizarov; Hartmuth C. Kolb; Jiang Huang; James R. Heath; Michael E. Phelps; Stephen R. Quake; Hsian-rong Tseng; Paul Wyatt; Antoine Daridon |
| New microfluidic devices, useful for carrying out chemical reactions, are provided. The devices are adapted for on-chip solvent exchange, chemical processes requiring multiple chemical reactions, and rapid concentration of reagents. | ||||||
| 171 | PET RADIOTRACERS FOR IMAGING FATTY ACID METABOLISM AND STORAGE | US13319001 | 2010-05-04 | US20120100073A1 | 2012-04-26 | Robert H. Mach; Robert John Gropler; Zhude Tu; Pilar Herrero |
| 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. | ||||||
| 172 | METHODS TO RADIOLABEL NATURAL ORGANIC MATTER BY REDUCTION WITH HYDROGEN LABELED REDUCING AGENTS | US13276156 | 2011-10-18 | US20120034700A1 | 2012-02-09 | Ruth M. Tinnacher; Bruce D. Honeyman |
| Methods to radiolabel natural organic matter by reduction with a hydrogen labeled reducing agent, and compositions, are provided. | ||||||
| 173 | IONIZABLE ISOTOPIC LABELING REAGENTS FOR RELATIVE QUANTIFICATION BY MASS SPECTROMETRY | US13155682 | 2011-06-08 | US20120022230A1 | 2012-01-26 | 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. | ||||||
| 174 | Method of rapid methylation of alkene compound and kit for PET tracer preparation using the same | US12090642 | 2006-10-06 | US08067631B2 | 2011-11-29 | Masaaki Suzuki; Takamitsu Hosoya |
| To provide a method of rapid methylation of alkenes, which is applicable to the preparation of a PET tracer and which enables alkenes to be methylated through cross coupling between SP2 (alkenyl) and SP3 (alkyl) carbon atoms rapidly and in a high yield. Methyl iodide and an alkenyltrialkylstannane are subjected to cross coupling in an aprotic polar solvent in the presence of a palladium complex having a valence of 0, a phosphine ligand, a cuprous halide, and a carbonate and/or alkali metal fluoride. | ||||||
| 175 | Methods to radiolabel natural organic matter by reduction with hydrogen labeled reducing agents | US11856594 | 2007-09-17 | US08039266B2 | 2011-10-18 | Ruth M. Tinnacher; Bruce D. Honeyman |
| Methods to radiolabel natural organic matter by reduction with a hydrogen labeled reducing agent, and compositions, are provided. | ||||||
| 176 | Isotopically tagged synons from 2 carbon precursors | US12035871 | 2008-02-22 | US08034982B2 | 2011-10-11 | Rodolfo A. Martinez |
| The use of vinyl sulfides, sulfoxides and sulfones in synthetic chemistry for the production of a wide variety of materials is well known. For example, phenyl vinyl sulfides, sulfoxides and sulfones have been used for the synthesis of important heterocycles, in combinatorial chemistry and as Diels-Alder adducts. Although these compounds have been used extensively for a variety of applications, the isotopically labeled versions have not been reported. A simple route for the isotopically labeled production of these important building blocks has been developed. | ||||||
| 177 | NUCLEOPHILIC FLUORINATION OF AROMATIC COMPOUNDS | US13054458 | 2009-07-13 | US20110178302A1 | 2011-07-21 | 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. | ||||||
| 178 | Purification Strategy for Direct Nucleophilic Procedures | US12937665 | 2009-04-09 | US20110112293A1 | 2011-05-12 | John Cyr; Ananth Srinivasan; Mathias Berndt; Keith Graham; Dae Yoon Chi; Byoung Se Lee; So Young Chu; Song-Yi Lim; Sang Ju Lee; Jin-Sook Ryu; Seung Jun Oh |
| The present invention provides novel and advantageous processes for preparing and purifying chemical compounds such as pharmaceuticals. The processes comprise a nucleophilic substitution reaction with a moiety X wherein the leaving group L of a substrate S in the reaction is covalently attached to a purification moiety M. This concept offers a convenient and lime-saving way to purity the desired product S-X from non-reacted precursors S-L-M and by-products L-M. | ||||||
| 179 | PROCESS FOR PRODUCING RADIOACTIVE FLUORINE LABELED ORGANIC COMPOUND, AND RELEVANT SYNTHETIC APPARATUS AND PROGRAM | US12439892 | 2007-08-31 | US20110003981A1 | 2011-01-06 | Keiichi Hirano; Taku Ito; Sento Ino |
| A method of producing a radioactive-fluorine-labeled compound has a step of heating in a reaction vessel a mixture containing [18F] fluoride ions, a phase transfer catalyst, potassium ions, and water to evaporate water from the mixture (S10), and in the above step has a step of measuring a temperature of an outlet tube for discharging evaporated water during the heating of the reaction vessel (S12), and the evaporation process is finished at a timing determined based on the result of temperature measurement in the step (S12) of measuring the temperature (S16). Consequently, the amount of water present in the mixture can be controlled to an appropriate range and a stable yield can be achieved in the method of producing a radioactive-fluorine-labeled organic compound. | ||||||
| 180 | Method for preparation of F-18 containing organofluoro compounds in alcohol solvents | US11720393 | 2005-12-09 | US07847092B2 | 2010-12-07 | Dae Hyuk Moon; Dae Yoon Chi; Dong Wook Kim; Seung Jun Oh; Jin-sook Ryu |
| The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of primary or secondary organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with primary or secondary alkyl halide or primary or secondary alkyl sulfonate in the presence of alcohol of Chemical Formula 1 as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds. | ||||||
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