101 |
Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-(trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1H)-one, a solid form thereof and methods of their use |
US15918544 |
2018-03-12 |
US10052323B2 |
2018-08-21 |
Kevin Klopfer |
Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition. |
102 |
NOVEL COMPOUND THAT SPECIFICALLY BINDS TO AMPA RECEPTOR |
US15741965 |
2016-07-05 |
US20180200391A1 |
2018-07-19 |
Takuya Takahashi; Tomoyuki Miyazaki; Tetsuya Suhara; Makoto Higuchi; Meiei Cho |
The present invention provides a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof. (In the formula, each of A and Z independently represents CO, SO or SO2; each of X and Y independently represents S or O; each of R1-R4 independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group or a halogen group; each R5 independently represents an alkyl group, an alkenyl group, an alkynyl group or a halogen group; and n represents an integer of 0-4.) This compound is capable of specifically binding to an AMPA receptor, and shows extremely high brain uptake. |
103 |
PHARMACEUTICAL COMPOSITIONS OF 7-(6-(2-HYDROXYPROPAN-2-YL)PYRIDIN-3-YL)-1-((TRANS)-4-METHOXYCYCLOHEXYL)-3,4-DIHYDROPYRAZINO [2,3-B]PYRAZIN-2(1H)-ONE, A SOLID FORM THEREOF AND METHODS OF THEIR USE |
US15918544 |
2018-03-12 |
US20180200252A1 |
2018-07-19 |
Kevin KLOPFER |
Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition. |
104 |
Precursor compound of radioactive halogen-labeled organic compound |
US14872305 |
2015-10-01 |
US10010632B2 |
2018-07-03 |
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. |
105 |
METHODS AND KITS FOR PREPARING RADIONUCLIDE COMPLEXES |
US15554573 |
2016-03-09 |
US20180092996A1 |
2018-04-05 |
Philip BLOWER; Gregory MULLEN |
A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. |
106 |
Process for the preparation of complexes of 68Ga |
US15163484 |
2016-05-24 |
US09907868B2 |
2018-03-06 |
Lorenza Fugazza; Maria Azzurra Filannino; Maurizio Franco Mariani |
A process for the preparation of complexes containing 68Ga wherein a buffer formic acid/formate in the presence of compounds capable to sequester metal cations is used in the complexation reaction. |
107 |
RADIOACTIVE IODINE LABELED PYRIDO[1,2-a]BENZOIMIDAZOLE DERIVATIVE COMPOUND |
US15543857 |
2016-02-24 |
US20180000974A1 |
2018-01-04 |
Hideo SAJI; Masahiro ONO; Masafumi IHARA; Ikuya SEKI |
The present invention relates to a radioactive iodine-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a definite general formula or a salt thereof, or a radiopharmaceutical comprising the same. |
108 |
Method for purification of 18F-labeled choline analogues |
US14895842 |
2014-06-02 |
US09839702B2 |
2017-12-12 |
Jean-Luc Morelle; Muhammad Otabashi; Gauthier Philippart; Samuel Voccia |
The present invention relates to a method for purification of 18F-labeled choline analogs in a solution injectable to a patient, prepared using non-gaseous synthesis paths, comprising a step of solid phase extraction (SPE) purification using a solid support, wherein the solid support used in the solid phase extraction purification has the characteristic to retain impurities and reagents from the solution but not the 18F-labeled choline analogs. |
109 |
Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-B]pyrazin-2(1H)-one, a solid form thereof and methods of their use |
US15427242 |
2017-02-08 |
US09795603B2 |
2017-10-24 |
Marie Georges Beauchamps; Antonio Christian Ferretti; Juan Antonio Gamboa; Kevin Klopfer; William Edward Konnecke; Matthew Michael Kreilein; Anil Menon; Amanda Nicole Miklos; John Fitzgerald Traverse |
Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition. |
110 |
IRON AND COBALT CATALYZED HYDROGEN ISOTOPE LABELING OF ORGANIC COMPOUNDS |
US15329919 |
2015-07-29 |
US20170266648A1 |
2017-09-21 |
Paul CHIRIK; Renyuan YU |
Methods of isotopic labeling are described herein. For example, a method of isotopically labeling an organic compound, in some embodiments, comprises providing a reaction mixture including the organic compound, an iron complex or a cobalt complex and a source of deuterium or tritium. The organic compound is labeled with deuterium or tritium in the presence of the iron complex or cobalt complex or derivative of the iron complex or cobalt complex. |
111 |
Method and device for marking isotopes |
US14441536 |
2013-11-07 |
US09709570B2 |
2017-07-18 |
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. |
112 |
PHARMACEUTICAL COMPOSITIONS OF 7-(6-(2-HYDROXYPROPAN-2-YL)PYRIDIN-3-YL)-1-((TRANS)-4-METHOXYCYCLOHEXYL)-3,4-DIHYDROPYRAZINO [2,3-B]PYRAZIN-2(1H)-ONE, A SOLID FORM THEREOF AND METHODS OF THEIR USE |
US15427242 |
2017-02-08 |
US20170182042A1 |
2017-06-29 |
Marie Georges BEAUCHAMPS; Antonio Christian FERRETTI; Juan Antonio GAMBOA; Kevin KLOPFER; William Edward KONNECKE; Matthew Michael KREILEIN; Anil MENON; Amanda Nicole MIKLOS; John Fitzgerald TRAVERSE |
Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition. |
113 |
Compounds for use in imaging, diagnosing and/or treatment of diseases of the central nervous system or of tumors |
US14336424 |
2014-07-21 |
US09682944B2 |
2017-06-20 |
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). |
114 |
Nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio) molecules; precursors and conjugates thereof |
US14647144 |
2013-11-22 |
US09611215B2 |
2017-04-04 |
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. |
115 |
Method for production of F-18 labeled amyloid beta ligands |
US15062604 |
2016-03-07 |
US09592308B2 |
2017-03-14 |
Mathias Berndt; Matthias Friebe; Fabrice Samson; Rainer Braun; Gunnar Garke; 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. |
116 |
Device and method for the production of radiochemical compounds |
US14990567 |
2016-01-07 |
US09556081B2 |
2017-01-31 |
Marco Mueller; Steffen Howitz |
The invention relates to a method for the preparation of radiochemical compounds using a device having at least a reaction module, a dosing module, and a storage module, wherein the reaction module has at least one reaction vessel having a closable opening through which substances needed for the preparation of a predetermined radiochemical compound can be introduced into the reaction vessel of the reaction module and through which the prepared radiochemical compound can be removed from the reaction vessel of the reaction module; the dosing module has at least one pipetting head which can be moved relative to the storage module and the reaction module and in x, y, and z directions and also has at least one dosing unit; and at least one reservoir for one of the substances needed for the preparation of the respective radiochemical compound is formed in the storage module. Substances needed for the preparation of the respective radiochemical compound are introduced into the reaction vessel of the reaction module by means of dosing units, wherein the dosing units can be moved via a pipetting head in x, y directions or in x, y, and z directions. |
117 |
Calibration and normalization systems and methods for radiopharmaceutical synthesizers |
US14348189 |
2012-09-28 |
US09523778B2 |
2016-12-20 |
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). |
118 |
A KIT FOR PREPARING A RADIOPHARMACEUTICAL |
US15117167 |
2015-02-06 |
US20160346412A1 |
2016-12-01 |
Jan Rijn Zeevaart; Zoltan Szucs; Judith Wagener |
The present invention relates to a stabilized kit for the preparation of a radiopharmaceutical. In particular, the present invention relates to the use of a non-aqueous solvent for the stabilisation of the ligand component of the kit. |
119 |
18F-labeled precursor of PET radioactive medical supplies, and preparation method thereof |
US14117271 |
2012-05-11 |
US09505799B2 |
2016-11-29 |
Dae-Yoon Chi; Byoung-Se Lee; Chansoo Park; Min-Hyung Lee; Hyojin Cha; Woojin Cho; Heewon Kang; Kyunghun Kim |
The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system. |
120 |
Biomolecule labeling reaction container, and reactor and reaction method using the same |
US14235005 |
2012-12-26 |
US09421284B2 |
2016-08-23 |
Nami Sugita; Naomi Manri; Wataru Takeuchi; Yuichi Morimoto; Hiroko Hanzawa |
A reaction container in which to mix a first chemical compound with a second chemical compound has a main body and a lid member formed oppositely on a top face side of the main body; a flow channel on the top face of the main body; and a labeling agent solidification section at an intermediate section of the flow channel to remove a solvent in a solution of the second chemical compound and solidify the second chemical compound. First and second chemical compound supply sections and a mixture discharge section are formed on the upstream and downstream sides of the labeling agent solidification section, respectively. The reactor is provided with a liquid sending unit to supply the first and second chemical compounds and reciprocally send a solution of the first chemical compound to an upper part of the second chemical compound solidified at the solidification section. |