Ballatore Carlo, Smith Amos B, Lee Virginia M-Y, Trojanowski John Q, Brunden Kurt R
University of Pennsylvania, Perelman School of Medicine, Center for Neurodegenerative Disease Research , 3600 Spruce Street, Philadelphia, PA 19104-6323 , USA
Expert Opin Ther Pat. 2014 Mar;24(3):355-60. doi: 10.1517/13543776.2014.871526. Epub 2014 Jan 3.
Small-molecule ligands, amenable to positron emission tomography (PET) imaging of different types of neurodegenerative disease-associated amyloid deposits in the CNS of living patients, hold considerable promise for diagnostic purposes, as well as for monitoring disease progression and the effectiveness of treatments. The patent entitled 'Heterocyclic Compounds as Imaging Probes of Tau Pathology' (WO2013090497) discloses the identification of a novel class of tau imaging agents, the aminothienopyridazines. Selected compounds from this class are described that can stain selectively tau pathology in brain tissue sections. Moreover, examples of this class of compounds exhibit absorption, distribution, metabolism, excretion and pharmacokinetics (ADME-PK) properties that are appropriate for CNS PET ligands.
小分子配体适用于对活体患者中枢神经系统中不同类型神经退行性疾病相关淀粉样沉积物进行正电子发射断层扫描(PET)成像,在诊断方面以及监测疾病进展和治疗效果方面具有巨大潜力。名为“作为tau病理学成像探针的杂环化合物”的专利(WO2013090497)公开了一类新型tau成像剂——氨基噻吩并哒嗪的鉴定。描述了从该类别中选出的化合物,它们能够在脑组织切片中选择性地标记tau病理学特征。此外,这类化合物的实例展现出适合中枢神经系统PET配体的吸收、分布、代谢、排泄及药代动力学(ADME-PK)特性。