公开(公告)号：WO2018022603A1

公开(公告)日：2018-02-01

申请号：PCT/US2017/043694

申请日：2017-07-25

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

Inventor： BASULI, Falguni ,  SWENSON, Rolf ,  JAGODA, Elaine Marie

IPC: C07K14/475 ,  C07D213/82 ,  C07B59/00

CPC classification number: A61K51/088 ,  A61K9/0019 ,  C07B59/002 ,  C07B59/008 ,  C07D213/80 ,  C07D213/803 ,  C07K14/4753

Abstract: Described herein are novel methods for the synthesis of radiolabeling synthons such as [ 18 F]fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester, and also methods of labeling a protein or peptide comprising a free amine group. A novel c-Met binding peptide, and imaging methods, are also described.

Abstract translation: 本文描述了合成放射性标记合成子的新方法，例如[18 F]氟代烟酸-2,3,5,6-四氟苯酯，以及 标记包含游离胺基团的蛋白质或肽。 还描述了一种新的c-Met结合肽和成像方法。

公开(公告)号：WO2017089492A1

公开(公告)日：2017-06-01

申请号：PCT/EP2016/078729

申请日：2016-11-24

Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITE DE NANTES ,  UNIVERSITE D'ANGERS ,  THE GOVERNMENT OF THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

Inventor： GUERARD, François ,  GESTIN, Jean-François ,  BRECHBIEL, Martin W ,  LEE, Yong-Sok

IPC: C07B59/00 ,  C07D207/46 ,  C07C17/361 ,  C07C25/24 ,  C07C67/307 ,  C07C41/18 ,  C07C201/12 ,  C07C247/10 ,  C07C247/16 ,  C07C253/30

CPC classification number: C07C25/24 ,  C07B59/001 ,  C07B59/002 ,  C07B59/008 ,  C07B2200/05 ,  C07C17/361 ,  C07C29/10 ,  C07C29/58 ,  C07C29/62 ,  C07C33/46 ,  C07C41/18 ,  C07C43/225 ,  C07C67/307 ,  C07C201/12 ,  C07C247/10 ,  C07C247/16 ,  C07C253/30 ,  C07D207/46 ,  C07C69/76 ,  C07C255/50 ,  C07C205/11

Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.

Abstract translation: 本发明涉及一种合成碘或Astatoarene的方法，其包括二芳基碘鎓化合物分别与碘化物或astatide盐反应。 本发明还涉及所述碘 - 或吗啡烷芳烃和二芳基碘鎓化合物本身。 本发明还涉及使用所述碘 - 或者astatoarene合成碘 - 或者漂白的生物分子和/或载体的方法。

公开(公告)号：WO2014052471A1

公开(公告)日：2014-04-03

申请号：PCT/US2013/061712

申请日：2013-09-25

Applicant: BIOSYNTHEMA INC.

Inventor： MAINA-NOCK, Theodosia ,  NOCK, Berthold, Artur ,  DE JONG HENDRIKS, Marion

IPC: A61K51/08 ,  A61P35/00 ,  C07B59/00

CPC classification number: A61K51/088 ,  A61K51/08 ,  C07B59/008

Abstract: The present invention relates to probes for use in the detection, imaging, diagnosis, targeting, treatment, etc. of cancers expressing the gastrin releasing peptide receptor (GRPR). For example, such probes may be molecules conjugated to detectable labels which are preferably moieties suitable for detection by gamma imaging and SPECT or by positron emission tomography (PET) or magnetic resonance imaging (MRI) or fluorescence spectroscopy or optical imaging methods.

Abstract translation: 本发明涉及用于表达胃泌素释放肽受体（GRPR）的癌症的检测，成像，诊断，靶向，治疗等的探针。 例如，这样的探针可以是缀合到可检测标记的分子，其优选适合于通过γ成像和SPECT或正电子发射断层摄影（PET）或磁共振成像（MRI）或荧光光谱学或光学成像方法进行检测的部分。

公开(公告)号：WO2012118909A1

公开(公告)日：2012-09-07

申请号：PCT/US2012/027168

申请日：2012-03-01

Applicant: GE HEALTHCARE LIMITED ,  IMPERIAL COLLEGE ,  MEDI-PHYSICS, INC. ,  LUTHRA, Sajinder Kaur ,  LEYTON, Julius ,  ABOAGYE, Eric, Ofori ,  IDDON, Lisa ,  INDREVOLL, Bard ,  GLASER, Matthias Eberhard ,  CUTHBERTSON, Alan

Inventor： LUTHRA, Sajinder Kaur ,  LEYTON, Julius ,  ABOAGYE, Eric, Ofori ,  IDDON, Lisa ,  INDREVOLL, Bard ,  GLASER, Matthias Eberhard ,  CUTHBERTSON, Alan

IPC: A61K51/08 ,  A61K101/02 ,  C07B59/00

CPC classification number: A61K51/08 ,  A61K51/083 ,  A61K51/088 ,  C07B59/002 ,  C07B59/008

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) imaging are described. Novel radiotracer(s) for Positron Emission Tomography (PET) imaging of neuorendocrine tumors are described. Specifically the present invention describes novel [18F]Fluoroethyltriazol-[Tyr3]Octreotate analogs; in particular those that target somatostatin receptors found on the cell surface of gastroenteropancreatic neuorendocrine tumors. The present invention also describes intermediate(s), precursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Abstract translation: 描述了用于正电子发射断层扫描（PET）成像的新型放射性示踪剂。 描述了用于神经内分泌肿瘤的正电子发射断层扫描（PET）成像的新型放射性示踪剂。 具体地说，本发明描述了新颖的[18 F]氟乙基三唑 - [Tyr 3] Octreotate类似物; 特别是在胃肠胰腺内分泌肿瘤的细胞表面上发现的生长抑素受体的那些。 本发明还描述了新型放射性示踪剂的中间体，前体，药物组合物，制备方法和使用方法。

公开(公告)号：WO2012069535A1

公开(公告)日：2012-05-31

申请号：PCT/EP2011/070808

申请日：2011-11-23

Applicant: GE HEALTHCARE LIMITED ,  AVORY, Michelle ,  WADSWORTH, Harry, John ,  NAIRNE, Robert James Domett

Inventor： AVORY, Michelle ,  WADSWORTH, Harry, John ,  NAIRNE, Robert James Domett

IPC: A61K51/04 ,  A61K51/08 ,  C07B59/00 ,  A61K101/02

CPC classification number: C07B59/008 ,  A61K51/0453 ,  A61K51/08 ,  C07B59/002 ,  C07D249/06 ,  C07D261/08

Abstract: The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are functionalised BTMs useful in the method, as well as methods of preparing such functionalised BTMs under mild conditions.

Abstract translation: 本发明提供了用放射性碘标记生物靶向分子（BTM）的新方法。 还提供了在该方法中有用的官能化BTM，以及在温和条件下制备这种官能化BTM的方法。

公开(公告)号：WO2012027527A2

公开(公告)日：2012-03-01

申请号：PCT/US2011/049057

申请日：2011-08-25

Applicant: REICHERT, David, E. ,  KENIS, Paul J. A. ,  WHEELER, Tobias, D. ,  DESAI, Amit, V. ,  ZENG, Dexing ,  ÖNAL, Birce, C.

Inventor： REICHERT, David, E. ,  KENIS, Paul J. A. ,  WHEELER, Tobias, D. ,  DESAI, Amit, V. ,  ZENG, Dexing ,  ÖNAL, Birce, C.

IPC: C07F5/00

CPC classification number: B01J19/0093 ,  B01J2219/00833 ,  B01J2219/0086 ,  B01J2219/00862 ,  B01J2219/00889 ,  C07B59/00 ,  C07B59/008 ,  C07K1/1077 ,  C07K1/13

Abstract: A microreactor for preparing a radiolabeled complex or a biomolecule conjugate comprises a microchannel for fluid flow, where the microchannel comprises a mixing portion comprising one or more passive mixing elements, and a reservoir for incubating a mixed fluid. The reservoir is in fluid communication with the microchannel and is disposed downstream of the mixing portion. A method of preparing a radiolabeled complex includes flowing a radiometal solution comprising a metallic radionuclide through a downstream mixing portion of a microchannel, where the downstream mixing portion includes one or more passive mixing elements, and flowing a ligand solution comprising a bifunctional chelator through the downstream mixing portion. The ligand solution and the radiometal solution are passively mixed while in the downstream mixing portion to initiate a chelation reaction between the metallic radionuclide and the bifunctional chelator. The chelation reaction is completed to form a radiolabeled complex.

Abstract translation: 用于制备放射性标记的复合物或生物分子缀合物的微反应器包括用于流体流动的微通道，其中微通道包括包含一个或多个被动混合元件的混合部分和用于孵育混合流体的储存器。 储存器与微通道流体连通并且设置在混合部分的下游。 制备放射性标记的复合物的方法包括使包含金属放射性核素的放射性金属溶液流过微通道的下游混合部分，其中下游混合部分包括一个或多个被动混合元件，并使包含双功能螯合剂的配体溶液流过下游 混合部分。 配体溶液和放射性金属溶液在下游混合部分被动混合，以引发金属放射性核素和双功能螯合剂之间的螯合反应。 完成螯合反应以形成放射性标记的复合物。

公开(公告)号：WO2010008159A2

公开(公告)日：2010-01-21

申请号：PCT/KR2009/003808

申请日：2009-07-10

Applicant: POSTECH ACADEMY-INDUSTRY FOUNDATION ,  SHIN, Seung Koo ,  SEO, Jongcheol ,  SUH, Min-Soo ,  YOON, Hye-Joo

Inventor： SHIN, Seung Koo ,  SEO, Jongcheol ,  SUH, Min-Soo ,  YOON, Hye-Joo

IPC: C07C235/74 ,  G01N33/68 ,  C07K1/13

CPC classification number: G01R3/00 ,  C07B59/008 ,  C07C237/22 ,  C07K1/13 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/06069 ,  C07K5/06078 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06139 ,  C12Q2563/167 ,  C40B20/04 ,  G01N33/6851 ,  G01N2458/15 ,  Y10S930/01 ,  Y10T436/24

Abstract: The present invention provides variable mass labeling reagents, a set of the variable mass labeling reagents, and a multiplexed set of variable mass labeling reagents.

Abstract translation: 本发明提供可变质量标记试剂，一组可变质量标记试剂和多组可变质量标记试剂。

公开(公告)号：WO2009027707A3

公开(公告)日：2009-04-16

申请号：PCT/GB2008002951

申请日：2008-08-29

Applicant: UNIV KENT CANTERBURY ,  BIAGINI STEFANO CARLO GIORGIO ,  BLOWER PHILLIP JOHN ,  PARRY ALISON ,  SMITH GARETH E

Inventor： BIAGINI STEFANO CARLO GIORGIO ,  BLOWER PHILLIP JOHN ,  PARRY ALISON ,  SMITH GARETH E

IPC: A61K51/08 ,  C07F5/02 ,  C07K1/04 ,  C07K1/13 ,  C07K7/06

CPC classification number: C07K1/13 ,  A61K51/08 ,  C07B59/008 ,  C07F5/025 ,  C07K5/0827 ,  C07K14/595

Abstract: The invention provides a substituted amino acid comprising an optionally protected primary or secondary amino group, a carboxylic acid group and a group capable of binding a fluoride ion; a peptide comprising the substituted amino acid; a method for the preparation of the peptide and its use in diagnosis. The substituted amino acid according to the invention permits a synthetic approach with greater flexibility and control of the site of labelling than conventional methods.

Abstract translation: 本发明提供包含任选保护的伯或仲氨基，羧酸基团和能够结合氟离子的基团的取代的氨基酸; 包含取代的氨基酸的肽; 肽的制备方法及其在诊断中的应用。 根据本发明的取代的氨基酸允许具有比常规方法更大的灵活性和对标记位点的控制的合成方法。

公开(公告)号：WO2009035959A2

公开(公告)日：2009-03-19

申请号：PCT/US2008/075684

申请日：2008-09-09

Applicant: GE HEALTHCARE LIMITED ,  MEDI-PHYSICS, INC. ,  CUTHBERTSON, Alan ,  SOLBAKKEN, Magne ,  OLBERG, Dag Erlend

Inventor： CUTHBERTSON, Alan ,  SOLBAKKEN, Magne ,  OLBERG, Dag Erlend

IPC: A61K51/08 ,  C07B59/00 ,  C07K1/13

CPC classification number: C07B59/008 ,  A61K51/088 ,  C07K1/13 ,  C07K5/0817 ,  C07K7/56 ,  C07K14/745

Abstract: The invention relates to conjugates of formula (V) or (VI), their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.

Abstract translation: 本发明涉及式（V）或（VI）的缀合物，它们作为放射性药物的用途，它们的制备方法以及用于这些方法的合成中间体。

公开(公告)号：WO2008009004A9

公开(公告)日：2008-07-31

申请号：PCT/US2007073542

申请日：2007-07-13

Applicant: CELL SIGNALING TECHNOLOGY INC ,  HORNBECK PETER ,  GOSS VALERIE ,  LEE KIMBERLY ,  GU TING-LEI ,  MORITZ ALBRECHT

Inventor： HORNBECK PETER ,  GOSS VALERIE ,  LEE KIMBERLY ,  GU TING-LEI ,  MORITZ ALBRECHT

IPC: G01N33/574

CPC classification number: G01N33/57426 ,  C07B59/008 ,  C07K14/47 ,  C07K16/44 ,  G01N33/6842 ,  G01N2458/15

Abstract: The invention discloses novel phosphorylation sites identified in signal transduction proteins and pathways, and provides phosphorylation-site specific antibodies and heavy-isotope labeled peptides (AQUA peptides) for the selective detection and quantification of these phosphorylated sites/proteins, as well as methods of using the reagents for such purpose. Among the phosphorylation sites identified are sites occurring in the following protein types: adaptor/scaffold proteins, adhesion/extracellular matrix protein, apoptosis proteins, calcium binding proteins, cell cycle regulation proteins, chaperone proteins, chromatin, DNA binding/repair/replication proteins, cytoskeletal proteins, endoplasmic reticulum or golgi proteins, enzyme proteins, G/regulator proteins, inhibitor proteins, motor/contractile proteins, phosphatase, protease, Ser/ Thr protein kinases, protein kinase (Tyr)s, receptor/channel/cell suface proteins, RNA binding proteins, transcriptional regulators, tumor suppressor proteins, ubiquitan conjugating system proteins and proteins of unknown function.