ATROPISOMERS OF HALOGENATED TETRAPHENYLBACTERIOCHLORINS AND CHLORINS AND THEIR USE IN PHOTODYNAMIC THERAPY Russian patent published in 2020 - IPC C07D487/22 A61K31/409 A61P35/00 A61P31/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to a pharmaceutical composition containing over 70 % atropisomers of I-C and I-D formulas, a method for preparing it and a kit for photodynamic therapy. In general formula I-C and I-D is a single carbon-carbon bond or double carbon-carbon bond; bold lines indicate that bolded atoms and attached groups are sterically restricted such that they are located above the plane defined by the macrocyclic ring; X², X⁴, X⁶ and X⁸ are a halogen atom (F, Cl, Br); X¹, X³, X⁵ and X⁷ are atoms of halogen (F, Cl, Br) or hydrogen; R₁, R₂, R₃ and R₄ independently represent -OH, -OR or -SO₂R'', where each R'' is independently selected from -Cl, -OH, -amino acid, -OR, -NHR or -NR₂, where R is alkyl having from 1 to 12 carbon atoms, or R₂ is cycloalkyl having from 2 to 12 carbon atoms; R₅, R₆, R₇ and R₈ independently represent H, -OH, -OR, -Cl or -NHR, where R are alkyl having 1–12 carbon atoms.

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EFFECT: atropisomers of halogenated tetraphenylbacteriochlorins and chlorines and their use in photodynamic therapy are disclosed.

13 cl, 18 dwg, 6 tbl, 8 ex