FLUORINATED LIGANDS FOR TARGETING PERIPHERAL BENZODIAZEPINE RECEPTORS Russian patent published in 2012 - IPC C07D241/38 C07D487/04 C07D471/04 A61K31/437 A61K31/498 A61K31/4985 A61K31/5025 A61K31/519 A61K31/53 A61P25/00 A61P25/28 A61P35/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to fluorinated compounds of formula , where: D, G and L are independently selected from a group consisting of: CH, C and N, and J and M are independently selected from a group consisting of C and N, under the condition that one of J and M denotes C and the other denotes N, wherein at least two of D, G, M, J and L denote N; X denotes CH₂; Y is absent; Z denotes NR₁R₂; R₁ and R₂ are independently selected from a group consisting of: hydrogen, C₁-C₁₀ alkyl, aryl and heteroaryl, which is associated with aromatic radicals having 6 ring atoms, where 1-2 of these ring atoms are N; each of which can be substituted with one or more halogen atoms; or R₁ and R₂, together with nitrogen to which they are bonded, form a heterocyclic ring having 5 ring members; R₃ is selected from a group consisting of: halogen, C₁-C₁₀ alkyl; E denotes aryl which can be substituted with one or more fluoro-substitutes or one or more of the following substitutes: C₁-C₆ alkyl, QC₁-C₁₀ alkyl, QC₂-C₁₀ alkenyl, each of which can be substituted with one or more fluoro-substitutes, and where Q denotes O; m denotes a number from 1 to 2; under the condition that: R₃ is a fluoro-substitute, or group E includes a fluoro-substitute, or group Z includes a fluoro-substitute, with the condition that E does not denote 4-fluorophenyl or a compound of formula , where D, G and L are independently selected from a group consisting of: CH, C and N, and J and M are independently selected from a group consisting of C and N, under the condition that one of J and M denotes C and the other denotes N, wherein at least two of D, G, M, J and L denote N; X denotes CH₂; Y is absent; Z denotes NR₁R₂; R₁ and R₂ are independently selected from a group consisting of: hydrogen, C₁-C₁₀ alkyl, aryl and heteroaryl, which is associated with aromatic radicals having 6 ring atoms, where 1-2 of these ring atoms are N; each of which can be substituted with one or more of the following substitutes: chlorine, bromine, iodine; or R₁ and R₂, together with nitrogen to which they are bonded, form a heterocyclic ring having 5 ring members; R₃ is selected from a group consisting of: chlorine, bromine, iodine, C₁-C₁₀ alkyl; E denotes aryl which can be substituted with one or more chlorine, bromine or iodine atoms, and/or one or more of the following substitutes: C₁-C₆ alkyl, QC₁-C₁₀ alkyl, QC₂-C₁₀ alkenyl, each of which can be substituted with one or more substitutes selected from chlorine, bromine, iodine or hydroxy, where Q denotes O, wherein when E denotes phenyl, E does not contain, as a substitute, iodine which is directly bonded to it at position 4; m denotes a number from 1 to 2; wherein at least one of Z, E and R₃ includes iodine; under the condition that E does not denote 4-iodophenyl and under the condition that said compound is not a compound of formula (Ia), defined in the following table:

The invention also relates to a pharmaceutical composition based on the compound of formula (I) or (Ia), a diagnosis method, a method of treating said disorders, based on use of the compound of formula (I) or (Ia), and use of the compound of formula (I) or (Ia).

EFFECT: obtaining novel compounds useful in treating disorders in mammals, characterised by anomalous density of peripheral benzodiazepine receptors.

24 cl, 13 dwg, 9 tbl, 23 ex