COORDINATION COMPLEX OF PLATINUM (II) DIAMINOCYCLOHEXANE WITH BLOCK COPOLYMER CONTAINING POLYCARBOXYLIC ACID SEGMENT AND INCLUDING ANTICANCER AGENT Russian patent published in 2008 - IPC C08G81/00 C07F15/00 A61K31/282 A61K47/48 A61P35/00 A61K9/08 A61K47/34 

Abstract RU 2335512 C2

FIELD: chemistry.

SUBSTANCE: invention concerns coordination complex of platinum (II) diaminocyclohexane with block copolymer containing structure of the general formula PEG-block-poly(carbo), where PEG is a poly(ethyleneglycol) segment, and carbo is a repeating chain containing carboxylic group in the side chain, and platinum (II) diaminocyclohexane is immobilised by block copolymer due to linkage between carboxylic carbo residue anion and platinum; as well as method of obtaining the complex and anticancer composition including effective anticancer quantity of coordination complex and pharmaceutically acceptable carrier. In addition, invention concerns coordination complex of platinum (II) diaminocyclohexane and block copolymer with structure of the general formula (1-a) or (2-a) , where R1 is a hydrogen atom or unsubstituted or substituted serial or furcated C1-C12 alkyl group, L1 and L2 are linkage group, R3 is a hydrogen atom, protective group of aminogroup, hydrophobic group or polymerisation-capable group, R4 is hydroxylic group or initiator residue, each of R5 radicals is independently a hydrogen atom, alkali metal ion or protective group of carboxylic group, m is an integer from 5 to 20000, n is an integer from 2 to 5000 if alkali metal ion comprises 50% or more of the number of R5 groups which is n, with platinum (II) diaminocyclohexane immobilised by the said block copolymer due to linkage between carboxylic carbo residue anion and platinum, and equivalent ratio of diaminocyclohexane platinum (Pt) to carboxylic groups of the said block copolymer (Pt/COO-) is 0.3-1. The invention also concerns the method of obtaining this coordination complex and method of tumour treatment involving introduction of effective quantity of combined coordination complex of platinum (II) diaminocyclohexane and coordination complex of cis-platinum to a patient.

EFFECT: increased composition efficiency.

20 cl, 2 ex, 1 tbl

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RU 2 335 512 C2

Authors

Kataoka Kazunori

Nisijama Nobukhiro

Kabral Khorakio

Okazaki Soitiro

Dates

2008-10-10Published

2004-12-08Filed