Inventors:
Zheng Wang - San Antonio TX, US
Irene Kazhdan - San Antonio TX, US
Jian Gao - Helotes TX, US
Zhiqiang Han - San Antonio MO, US
Robert Marciniak - San Antonio TX, US
International Classification:
A61K 49/00, A61K 48/00, A61K 31/409, A61K 31/555
US Classification:
424009600, 514044000, 424009610, 514185000, 514410000
Abstract:
In the broadest sense an inventive conjugate includes a macrocyclic scaffold moiety incorporating at least one nitrogen atom. Through linkages to the ring, nitrogen atoms are bonded to at least one therapeutic species, or one cellular trafficking species, and preferably two or more types of trafficking species. The linkages between ring nitrogen atoms and agents are formed through N—C, N—S, N—O or N—N bonds. It is appreciated that more than one agent or agent species are coupled to a ring nitrogen atom through the inclusion of a branched carbon atom or secondary amine nitrogen within the intermediate between the agent and ring nitrogen atom. A disulfide bond intermediate between an agent and a linkage to the ring nitrogen is preferred in instances where intracellular release of the agent or trafficking species is desired. An optional metal ion is coordinated by the scaffolding moiety.