PALLADIUM COMPLEXES WITH HETEROCYCLIC LIGANDS

03-06-2004 дата публикации
Номер:
AU2002364756A1
Контакты:
Номер заявки: 47-36-200256
Дата заявки: 12-11-2002

[1]

(19) AUSTRALIAN PATENT OFFICE (54) Title PALLADIUM COMPLEXES WITH HETEROCYCLIC LIGANDS (51 )6 International Patent Classification(s) C07F 015/00 C07D 211/76 C07D 241/12 C07D 241/18 C07D 265/30 C07D 295/02 A6IK 031/496 A6IK 031/535 A6IP 035/00 (21) Application No: 2002364756 (22) Application Date: 2002.11.12 (87) WIPO No: WO04/043975 (43) (43) (71) (72) Publication Date : Publication Journal Date 2004.06.03 2004.07.08 Applicant(s) ZAKRYTOE AKTSIONERNOE OBSCHESTVO "ASGL-FARMATSEVTICHESKIE INNOVATSII" Inventor(s) EFIMENKO, Inessa Alexandrovna; Veniaminovich 7 IVANOVA, Nina Alexandrovna; LOKSHIN, Boris



[2]

The invention relates to novel chemical compounds, in particular palladium complexes with heterocyclic ligands of general formula I, <CHEM> wherein R1 is NH2, O or CH2; R2 is 2H or O; R3 is H, CH3, CH2-CH2-NH3 or (CO)-CH3; X is Cl or Br; when R1 is NH2 or O; R2 is 2H; R3 is H, CH3, CH2-CH2-NH3 or (CO)-CH3, then n = 1, and m = 1; when R1 is O or CH2; R2 is O or 2H; R3 is H, CH3 or (CO)-CH3, then n = 2, and m = 1; when R1 is NH2; R2 is 2H; R3 is CH2-CH2-NH3, then n = 2, and m = 3; which compounds have pharmacological activity, in particular anti-tumor activity. The compounds of the invention are a higher activity and characterized by a lower toxicity as compared with anti-tumor platinum complex preparations.



Palladium complexes with heterocyclic ligands of general formula I, wherein

R1 is NH2, O or CH2;

R2 is 2H or O;

R3 is H, CH3, CH2-CH2-NH3 or (CO)-CH3;

X is Cl or Br;

when R1 is NH2 or O; R2 is 2H; R3 is H, CH3, CH2-CH2-NH3 or (CO)-CH3, then n = 1, and m = 1; when R1 is O or CH2; R2 is O or 2H; R3 is H, CH3 or (CO)-CH3, then n = 2, and m = 1; when R1 is NH2; R2 is 2H; R3 is CH2-CH2-NH3, then n = 2, and m = 3.

Palladium complexes with heterocyclic ligands of claim 1, characterized in that they have pharmacological activity.

Palladium complexes with heterocyclic ligands of claim 1 or claim 2, characterized in that they have anti-tumor activity.