公开(公告)号：US20060275209A1

公开(公告)日：2006-12-07

申请号：US10573882

申请日：2004-09-27

Applicant: Lutz Schweiger ,  Stuart Craib ,  Andrew Welch ,  Peter Sharp

Inventor： Lutz Schweiger ,  Stuart Craib ,  Andrew Welch ,  Peter Sharp

IPC: A61K51/00 ,  C07D279/18

CPC classification number: C07B59/00 ,  C07D279/20

Abstract: This invention pertains to methods of [11C]-radiolabelling “phenothiazine” and “phenothiazine-like” compounds, which have a pendant group (which is a primary amino group; a cationic primary imino group; a secondary amino group; a cationic secondary imino group; a primary imino group; or a secondary imino group), by reaction with [11C]methyl trifluoromethanesulfonate (CF3SO2O11CH3), also known as [11C]methyl triflate. This reaction converts the pendant group into a [11C]methyl-labelled pendant group. The resulting [11C]-radiolabelling product is useful, for example, as an in vivo positron emission tomography (PET) tracer, for example, for patients suffering from melanoma, the most serious form of skin cancer, and tauopathy (e.g., Alzheimer's disease). The present invention also pertains to the resulting [11C]-radiolabelling products, compositions comprising them, their use in methods of (e.g., PET) imaging, their use in methods of medical treatment and diagnosis, etc.

Abstract translation: 本发明涉及具有侧基（其为伯氨基;阳离子性亚氨基;阳离子性亚氨基）的“[ - 11 C] - 放射标记”吩噻嗪“和”吩噻嗪样“化合物的方法 仲氨基;阳离子二次亚氨基;初级亚氨基;或仲亚氨基），通过与三氟甲磺酸酯（CF 3 SO 3）与[ 另外也称为[11 C]三氟甲磺酸甲酯。 该反应将侧基转化为[11 C]甲基标记的侧基。 所得的[11 C] - 放射性标记物可用于例如体内正电子发射断层摄影（PET）示踪剂，例如对于患有黑素瘤的患者，最严重的皮肤癌形式 ，和tau病（如阿尔茨海默病）。 本发明还涉及所得的[11 C] - 放射性标记物，包含它们的组合物，它们在（例如，PET）成像方法中的应用，它们在医学治疗和诊断方法中的应用等 。