CATIONIC BACTERIOCHLOROPHYLL DERIVATIVES AND USE THEREOF Russian patent published in 2010 - IPC C07D487/22 A61K31/409 A61K41/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to cationic tetracyclic and pentacyclic derivatives of bacteriochlorophyll (Bchl) of formula , and , where M is 2H or a bivalent metal atom selected from a group comprising Pd, Ni, Cu and Zn; R₁, R'₂ and R₆ each independently denotes Y-R₈, -NR₉R'₉ or -N⁺R₉R'₉R"₉ A^-; Y is O; R₂ is H or COOCH₃; R₃ is H or COOCH₃; R₄ is -COCH₃, -CH(CH₃)=NR₉ or -CH(CH₃)=N⁺R₉R'₉A^-; R₅ is =O; R₇, R₈, R₉, R'₉ and R"₉ each independently denotes (a) H; (b) C₁alkyl; (c) C₂-C₆alkyl substituted with one or more functional groups selected from a group comprising OR or COOR; a positively charged group selected from a cation obtained from an N-containing group or onium group selected from S⁺(RR'), -P⁺(RR'R"), -As⁺(RR'R"); a basic group which is converted to a positively charged group in physiological conditions selected from NRR', PRR', -C(=NR)-NR'R" or N-containing heteroaryl radical where each of R, R' and R" independently denotes H or C₁-C₂allkyl, or two from R, R' and R" together with a nitrogen atom form a 3-7-member saturated ring which optionally contains an O or N atom and is optionally substituted on the extra N atom; (d) C₂-C₄alkyl which contains one heteroatom and/or one heterocyclic group; (e) C₂-C₆alkyl which contains one heteroatom and/or one heterocyclic group and substituted with one or two functional groups as described above in (c); (f) an amino acid or monosaccharide residue; A^- is physiologically acceptable anion; m equals 0 or 1; and its pharmaceutically acceptable salts and optical isomers; provided that when in formula I R₂ and R₃ both denote H, R₄ is not C(CH₃)=NR₉; and also provided that the bacteriochlorophyll derivative of formula I, II or III contains at least one positively charged group and/or at least one basic group which is converted to a positively charged group under physiological conditions. The invention also relates to a pharmaceutical composition based on the bacteriochlorophyll derivative of formula I, II or III for photodynamic therapy of tumours, for destroying cells or infectious agents which contain bacteria and viruses, to a method of photodynamic therapy of tumours, a method of diagnosing tumours and a method of destroying cells or infectious agents which contain bacteria and viruses.

EFFECT: obtaining novel bacteriochlorophyll derivatives useful in photodynamic therapy of tumours.

77 cl, 21 dwg, 5 tbl, 77 ex