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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
121 Super lewis acidic borate esters as 18F-labeled PET probes US14762544 2014-01-24 US09409927B2 2016-08-09 Mark Lee McLaughlin; Haibin Tian
Compounds having a 1-bora-1-fluoro-2,6,7-trioxabicyclo[2.2.2]octane moiety wherein the fluorine is 18F are described. Also described are reagents for radiolabeling a molecule having Formula I. Method for radiolabeling molecules with the disclosed reagents are also descried, as are radiolabeled molecules prepared thereby.
122 RADIOACTIVE AGENT SYNTHESIS DEVICE AND METHOD US14912423 2013-08-28 US20160200640A1 2016-07-14 Naomi MANRI; Norihito KUNO
In a reaction between a biomolecule and a radioactive agent precursor, the amount of a component of a radioactive agent precursor before the reaction and the amount of a component contained in a reaction mixture in a reaction process in which the reaction is performed at a predetermined biomolecule concentration are measured, a reaction rate constant is calculated from the information of the obtained amounts of the components, a reaction rate constant when the biomolecule concentration is changed is calculated, a reaction time, a specific radioactivity, and a radioactivity level of an objective substance at each biomolecule concentration are predicted, and synthesis is performed under a reaction condition under which the highest specific radioactivity is obtained among the reaction conditions satisfying the synthesis requirements.
123 Precursor compound of radioactive halogen-labeled organic compound US14814185 2015-08-21 US09387266B2 2016-07-12 Osamu Ito; Akio Hayashi; Fumie Kurosaki; Masahito Toyama; Toshiyuki Shinmura; Arinori Harano
It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.
124 Phenyl glyoxal probes US14405467 2013-06-04 US09347948B2 2016-05-24 Paul R. Thompson; Kevin L. Bicker; Venkataraman Subramanian
Novel phenyl-glyoxal based anti-citrulline probes and methods of synthesis are provided. Methods of use, such as, the development of methods for monitoring substrate citrullination over time; for identifying citrullinated proteins from cells are described.
125 Process for the preparation of deuterated compounds containing N-alkyl groups US14118705 2012-05-21 US09340489B2 2016-05-17 Jens Atzrodt; Volker Derdau; Wolfgang Holla; Matthias Beller; Lorenz Neubert; Dirk Michalik
The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.
126 Method of deuteration using mixed catalyst US10585629 2004-12-21 US09255070B2 2016-02-09 Nobuhiro Ito; Tsuneaki Maesawa; Kazushige Muto; Kosaku Hirota; Hironao Sajiki
The subject of the present invention is to provide a method for deuteration, which can obtain a compound having an aromatic ring and/or a heterocyclic ring at an improved deuteration ratio. The present invention relates to a method for deuteration of a compound having an aromatic ring and/or a heterocyclic ring, comprising reacting the compound having an aromatic ring and/or a heterocyclic ring with a heavy hydrogen source in the presence of an activated mixed catalyst of not less than two kinds of catalysts selected from among a palladium catalyst, a platinum catalyst, a rhodium catalyst, an iridium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst.
127 Radiolabeled amino acids for diagnostic imaging US14115471 2012-04-30 US09238631B2 2016-01-19 Mathias Berndt; Andre Muller; Heribert Schmitt-Willich; Timo Stellfeld; Georg Kettschau; Thomas Brumby; Keith Graham; Lutz Lehmann; Jorma Haβfeld; Martin Kruger
This invention relates to novel compounds suitable for labeling by 18F and to the corresponding 18F labeled compounds themselves, 19F-fluorinated analogs 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).
128 METHOD OF SYNTHESIZING FLUORINE-18 LABELED RADIOPHARMACEUTICALS IN ETHANOL AND WATER US14744627 2015-06-19 US20150367005A1 2015-12-24 Peter J. H. Scott; Megan N. Stewart; Brian Hockley
A method of preparing fluorine-18 labeled radiopharmaceuticals (18F-radiopharmaceuticals) is disclosed. More particularly, the present invention relates to a method of preparing an 18F-radiopharmaceutical by reacting a salt containing fluorine-18 (18F) with an alkyl halide or an alkyl sulfonate in the presence of water and ethanol to obtain a high yield of the 18F-radiopharmaceutical. The synthetic method eliminates the use of toxic and/or environmentally-unfriendly organic solvents.
129 SUPER LEWIS ACIDIC BORATE ESTERS AS 18F-LABELED PET PROBES US14762544 2014-01-24 US20150361110A1 2015-12-17 Mark Lee McLaughlin; Haibin Tian
Compounds having a 1-bora-1-fluoro-2,6,7-trioxabicyclo[2.2.2]octane moiety wherein the fluorine is 18F are described. Also described are reagents for radiolabeling a molecule having Formula I. Method for radiolabeling molecules with the disclosed reagents are also descried, as are radiolabeled molecules prepared thereby.
130 METHOD AND DEVICE FOR MARKING ISOTOPES US14441536 2013-11-07 US20150309038A1 2015-10-29 Regine Fuchs; Olaf Woiwode; Enrico Peter; Hardy Schön; Christoph Wittmann; Detlev Rasch; Veronique Beckers; Lisa Dersch
The present invention relates to an isotope labeling chamber for labeling metabolites in an organism, comprising a reactor chamber (1) and an air regulation chamber (2), wherein the reactor chamber (1) comprises the following components: optionally, a housing frame (3), housing walls (4), at least one injection valve (5), where at least one housing wall (4) can be opened fully and/or in part and where at least one housing wall has a lock (6), and furthermore wherein the air regulation chamber (2) comprises the following components: a temperature-regulating unit (7), an air humidification unit (8) and a gas absorption unit (9). Furthermore, the invention relates to a labeling method for plants in which the labeling chamber according to the invention is employed.
131 Use of microfabricated devices US14253049 2014-04-15 US09169284B2 2015-10-27 Frank Brady; Sajinder Kaur Luthra; James Millar Gillies; Nicholas Toby Jeffrey
This invention relates to the miniaturization of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).
132 Method and kit for preparing a radiopharmaceutical US13475759 2012-05-18 US09161998B2 2015-10-20 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.
133 NEW NUCLEOPHILE-REACTIVE SULFONATED COMPOUNDS FOR THE (RADIO)LABELLING OF (BIO) MOLECULES; PRECURSORS AND CONJUGATES THEREOF US14647144 2013-11-22 US20150284326A1 2015-10-08 Thomas Priem; Cedric Bouteiller; Davide Camporese; Anthony Romieu; Pierre-Yves Renard
Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conform to respective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.
134 Condensed-cyclic compound and organic light-emitting device including the same US13677255 2012-11-14 US09150496B2 2015-10-06 Soo-Yon Kim; Seok-Hwan Hwang; Young-Kook Kim; Hye-Jin Jung; Jin-O Lim; Sang-Hyun Han; Eun-Jae Jeong; Jun-Ha Park; Eun-Young Lee; Bo-Ra Lee; Jong-Hyuk Lee
Embodiments of the invention are directed to a condensed-cyclic compound represented by Formula 1, and to an organic light-emitting device including the condensed-cyclic compound. The organic light-emitting device may include an organic layer containing the condensed-cyclic compound.
135 IODINE(III)-MEDIATED RADIOFLUORINATION US14641094 2015-03-06 US20150252007A1 2015-09-10 Neil Vasdev; Benjamin H. Rotstein; Nickeisha A. Stephenson; Huan Liang
A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
136 POLYMER PRECURSORS OF RADIOLABELED COMPOUNDS, AND METHODS OF MAKING AND USING THE SAME US14633689 2015-02-27 US20150239797A1 2015-08-27 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.
137 C-11 Cyanide Production System US14551141 2014-11-24 US20150217249A1 2015-08-06 Dohyun Kim; David Alexoff; Sung Won Kim; Jacob M. 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% H 11CN is provided in less than 10 minutes from retrieval of the 11C labeled oxide.
138 Method for producing 18F-labeled compound and high molecular compound to be used in the method US13578569 2011-02-08 US09073802B2 2015-07-07 Takashi Takahashi; Hiroshi Tanaka; Tsutomu Nakada
The present invention aims at solving the problems of conventional methods for producing an 18F-labeled compound, that is, the problem of purification of a compound in a liquid phase synthesis method and the problem of an insufficient yield due to the reduction of reactivity in a solid phase synthesis method. There is provided a method for producing an 18F-labeled compound including: allowing a high molecular compound containing a residue of a precursor compound to be labeled and a residue of a phase transfer catalyst in the molecule thereof to react with 18F−; and removing the 18F-labeled compound from the high molecular compound.
139 SEPARATOR CARTRIDGE FOR RADIONUCLIDE US14528789 2014-10-30 US20150165341A1 2015-06-18 Glenn H. Isensee
A processing device for a radionuclide including a cartridge assembly including a cartridge and receptacle, the cartridge containing a chromatographic material that captures one of a daughter and parent radionuclide from a mixture of the parent and daughter radionuclide passing longitudinally through the cartridge, the cartridge having respective transverse flanges on opposing ends, the receptacle having a slot on each end of a space that receives the cartridge where, the slots on each end receive the transverse flanges, the receptacle further including a connection assembly on each end of the space, the connection assemblies each having a lever that is moved along a respective slot that advances a connector towards the cartridge while twisting the connector as it makes contact with the cartridge to form a liquid tight connection.
140 NOVEL PHENYL GLYOXAL PROBES US14405467 2013-06-04 US20150148259A1 2015-05-28 Paul R. Thompson; Kevin L. Bicker; Venkataraman Subramanian
Novel phenyl-glyoxal based anti-citrulline probes and methods of synthesis are provided. Methods of use, such as, the development of methods for monitoring substrate citrullination over time; for identifying citrullinated proteins from cells are described.
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