CATIONIC BLOCK-COPOLYMERS Russian patent published in 2006 - IPC C08G81/00 C07H21/00 C12N9/10 

FIELD: organic chemistry, chemistry of polymers.

SUBSTANCE: invention relates to cationic block-copolymers used, in particular, as a surface-active substance, and to a method for their preparing and to a composition for carrying out the transfection process based on cationic block-copolymers. Cationic block-copolymers represent compounds of the formula (I): A(-X-B)_n or (II): C(-Y-D)_m wherein A means hydrophilic, nonionic, linear or branched polymer of molecular mass from 100 to 10000000 Da comprising such residues as a linear polyethylene glycol residue, multiple branched polyethylene glycol, stellate polyethylene glycol, polysaccharides, polyvinyl alcohol; B means a linear or branched polyethyleneimine of molecular mass from 100 to 1000000 Da; X means a direct bond of blocks A and B or a bridge with the following structures and wherein C-end of bridge is bound with nitrogen atom of polyethyleneimine: -OC(O)NH(CH₂)_oNHC(O)- wherein o = 1-20; -OC(O)NH(aryl)NHC(O)- wherein aryl means an aromatic structural unit; -O(CH₂)_pC(O)- wherein p = 1-10; -OC(O)- or -O(CH₂)_q- wherein q = 1-20 and n means a whole number 1-200. C means a linear or branched polyethyleneimine of molecular mass from 100 to 1000000 DA; D means a residue of polyethylene glycol of the formula -(CH₂CH₂O)_n'-R¹ bound through oxygen atom (O) wherein n' = 3-25000, and R¹ means hydrogen atom, aliphatic residue or a group protecting hydroxyl group (-OH). Y means a direct bond of blocks C and D or a bridge with the following structures wherein C-end of bridge is bound with nitrogen atom of polyethyleneimine: -C(O)NH(aryl)NHC(O)O- wherein aryl means aromatic structural unit; -(CH₂)_tC(O)O- wherein t = 2-10; -CH₂CH(OH)CH₂O- or -(CH₂)_uO- wherein u = 1-20; m means a whole number 1-20 under condition that residue and variable values of the formula (II) have such values that compounds of the formula (I) don't fall within to this formula. Compound of the formula (I) is prepared by three methods. The first method involves interaction of compound of the general formula A-(OH)_n wherein A and n have abovementioned values with diisocyanate and formed compound is interacted with polyethyleneimine. The second method involves addition of ethyleneimine to compound of the general formula A-(NH₂)_n wherein A and n have abovementioned values followed by polymerization process. The third method involves addition of ethyleneimine to compound of the general formula A-(OS(O)₂R⁴)_n wherein A has abovementioned value; and wherein R⁴ means aliphatic or aromatic residue followed by polymerization. Method for preparing compound of the formula (II) involves interaction of compound of the general formula D-OH wherein D has abovementioned value with diisocyanate and then the prepared compound is interacted with a linear or branched polyethyleneimine. If in compound of the formula (II) Y means -C(O)NH(CH₂)_sNHC(O)O- wherein s = 1-20 then these block-copolymers can be used as a chelating compound for nucleic acid. The composition for carrying out the transfection involves at least one nucleic acid and one compound of the formula (I) or (II).

EFFECT: improved and valuable properties of block-copolymers.

11 cl, 78 ex