CONJUGATED BISPHOSPHONATES FOR DIAGNOSING AND TREATING BONE DISEASES Russian patent published in 2021 - IPC A61K51/04 A61K31/675 A61P19/08 C07F9/6558 G01N23/46 G01N24/08 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: group of inventions relates to a compound of formula II for complexing metal isotopes: where X denotes a chelating agent, selected from DOTK (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), DOTKGC (dodeca-1-glutaric acid-1,4,7,10-tetraamine triacetic acid), DOTKM (1,4,7,10-tetrakis- (carbamoylmethyl)-1,4,7,10-tetraazacyclododecane) and other derivatives of DOTK, NOTK (nona-1,4,7-triamine triacetic acid) and derivatives thereof, such as NOTKGK (1,4,7-triazacyclononane, 1-(glutaric acid), 4,7-acetic acid), AAZTK (6-amino-6-methylperhydro-1,4-diazepin-N,N,N',N'-tetraacetic acid), and R₃ denotes ; as well as to pharmaceutical agents, consisting of a compound of formula II and forming a metal isotope complex with it, to a method for producing said agent and use thereof in diagnostic methods, in methods of treating bone diseases and as additives in artificial bone substance, in bone cement or in bone implants.

EFFECT: group of inventions provides creating an agent possessing high and selective accumulation in bones and bone tumors.

25 cl, 4 tbl, 9 ex, 6 dwg