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This report summarizes the results of our long time work in the field of 3,7- diazabicyclo[3.3.1]nonane’s (bispidine) coordination chemistry1 and points out novel directions of research for the future2-4. We will discuss the ways of the possible application of bispidines and their complexes as bioactive compounds. The radiation therapy is one of the modern and useful methods for the treatment of the oncological diseases, particularly, for the brain, head and neck tumors as well as for the tumors of some other localization. The problem of short decay time can be solved by use of new radiopharmaceuticals containing long-lived isotopes, particularly, 64Cu. To do this, the elaboration of easily modified ligand systems with high affinity to the metal cation and with wide possibilities of chemical modifications including the conjugation to the biological vectors is proposed. We will talk about two families of tri- and tetradentate bispidine-based ligands that are derived from the same commercially available starting compound, urotropine (scheme). The solubility, stability constants, spectroscopy, electrochemistry and current stage of using copper complexes, as new PET reagents, will be discussed in details. This work is supported by Russian Science Foundation (grant # 16-13-00114).