公开(公告)号：WO2011076778A1

公开(公告)日：2011-06-30

申请号：PCT/EP2010/070352

申请日：2010-12-21

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

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

IPC: C07D451/02

CPC classification number: C07D451/02 ,  A61K51/0448 ,  A61K51/0455

Abstract: The present invention provides novel radio iodinated tropanes incorporating triazole or isoxazole rings. Also provided are methods of preparation of said tropanes from functionalised tropane precursors, using click cycloaddition chemistry, as well as radiopharmaceutical compositions comprising such radio iodinated tropanes. The invention also provides in vivo imaging methods using the radio iodinated tropanes.

Abstract translation: 本发明提供了掺入三唑或异恶唑环的新型放射性碘化托烷。 还提供了使用点状环加成化学制备来自功能化的托烷前体的所述托烷的方法，以及包含这种放射性碘化托烷的放射性药物组合物的方法。 本发明还提供了使用放射性碘化托烷的体内成像方法。

公开(公告)号：WO2008141249A1

公开(公告)日：2008-11-20

申请号：PCT/US2008/063343

申请日：2008-05-09

Applicant: ACADIA PHARMACEUTICALS INC. ,  GE HEALTHCARE, LTD. ,  OLSSON, Roger ,  BURSTEIN, Ethan ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen ,  CASTILLO, Joel ,  NAIRNE, James ,  IVESON, Veronique, Morisson ,  ROBINS, Edward ,  GIBSON, Alex

Inventor： OLSSON, Roger ,  BURSTEIN, Ethan ,  KNAPP, Anne, Eeg ,  ESKILDSEN, Jorgen ,  CASTILLO, Joel ,  NAIRNE, James ,  IVESON, Veronique, Morisson ,  ROBINS, Edward ,  GIBSON, Alex

IPC: C07D471/04 ,  C07D487/04 ,  A61P29/00 ,  A61P25/00 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Disclosed herein are compounds of Formula (I), or a pharmaceutically acceptable salt, ester, amide,thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula I with the cannabinoid CB2 receptor. Also disclosed are methods of imaging of a tissue by positron emission tomography, the method comprising administering to the subject a compound of Formula I, wherein the compound comprises a radioisotope. Also disclosed are methods of measuring the relative concentration of cannabinoid CB2 receptors in tissue of a subject, by using a compound of Formula I which comprises a radioisotope. In addition, method of diagnosing a disorder in a subject are disclosed.

Abstract translation: 本文公开了式（I）的化合物或其药学上可接受的盐，酯，酰胺; 以及调节大麻素CB2受体的活性的方法，包括使式I化合物与大麻素CB2受体接触。 还公开了通过正电子发射断层摄影术对组织进行成像的方法，所述方法包括向受试者施用式I化合物，其中所述化合物包含放射性同位素。 还公开了通过使用包含放射性同位素的式I化合物来测量受试者组织中的大麻素CB 2受体的相对浓度的方法。 此外，公开了患者的病症诊断方法。

公开(公告)号：WO2012067863A1

公开(公告)日：2012-05-24

申请号：PCT/US2011/059495

申请日：2011-11-07

Applicant: GE HEALTHCARE LIMITED ,  MEDI-PHYSICS, INC. ,  JONES, Clare ,  EWAN, Amanda ,  WYNN, Duncan ,  GAETA, Alessandra ,  NAIRNE, James

Inventor： JONES, Clare ,  EWAN, Amanda ,  WYNN, Duncan ,  GAETA, Alessandra ,  NAIRNE, James

IPC: C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/36 ,  C07D401/04 ,  C07D401/12 ,  C07D295/067 ,  A61K31/47 ,  A61P25/00

CPC classification number: A61K51/0455 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/36 ,  C07D295/067 ,  C07D401/04 ,  C07D401/12

Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.

Abstract translation: 描述了用作阿尔茨海默氏病Tau病理学成像探针的式（I）的杂环化合物。 还描述了制备这种化合物的组合物和方法。

公开(公告)号：WO2012068072A1

公开(公告)日：2012-05-24

申请号：PCT/US2011/060737

申请日：2011-11-15

Applicant: GE HEALTHCARE LIMITED ,  MEDI-PHYSICS, INC. ,  JONES, Clare ,  NAIRNE, James

Inventor： JONES, Clare ,  NAIRNE, James

IPC: A61K51/00 ,  A61K31/428

CPC classification number: C07D417/06 ,  A61K31/428 ,  A61K51/0465

Abstract: Radiolabeled compounds useful as diagnostic imaging agents of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.

Abstract translation: 描述了可用作阿尔茨海默病Tau病理学诊断显像剂的放射性标记化合物。 还描述了制备这种化合物的组合物和方法。