HYALURONIC ACID DERIVATIVE HAVING AMINO ACID AND STERYL GROUP INTRODUCED THEREIN Russian patent published in 2018 - IPC C08B37/08 A61K47/36 A61K47/50 

FIELD: medicine.

SUBSTANCE: present invention relates to a medicinal hyaluronic acid derivative containing a unit of formula (I):

where R¹–R⁴ are selected from H, C_1-6alkyl, formyl and C_1-6alkylcarbonyl; R⁵ is selected from H, formyl or C_1-6alkylcarbonyl; R⁶ is selected from H and C_1-6alkyl; -CHR^a-CO-X¹ is selected from groups: , , where * denotes the site of attachment to -NR⁶-; Z¹ is C_2-30alkylene or -(CH₂CH₂O)_m-CH₂CH₂- optionally containing 1–5 groups -O-, -NR^g- or -S-S-; m is 1–100; Z² selected from -NR^b-Z³ and -NR^b-COO-Z³; R^b is selected from H, C_1-20alkyl, amino-C_2-20alkyl and hydroxy-C_2-20alkyl optionally containing 1–3 groups -O- and -NR^f-; R^f is selected from H, C_1-12alkyl, amino-C_2-12alkyl and hydroxy-C_2-12alkyl optionally containing 1 to 2 groups -O- or -NH-; R^g is selected from H, C_1-20alkyl, amino-C_2-20alkyl or hydroxy-C_2-20alkyl optionally containing 1–3 groups -O- or -NH-; Z³ – cholanoyl or cholesteryl; and for X¹, other than -NR⁹-Z¹-Z², said derivative additionally contains a unit of formula (II): where R^1a–R^4a are selected from H, C_1-6alkyl, formyl and C_1-6alkylcarbonyl; R^5a is H, formyl or C_1-6alkylcarbonyl; X² is -NH-Z¹-Z², where Z¹ and Z² are defined above; and said derivative is obtained using hyaluronic acid exclusively consisting of units of formula (IIb): where R^5b is selected from H, formyl and C_1-6alkylcarbonyl; X^b is selected from OH and -O-Q⁺, where Q⁺ selected from Li⁺, Na⁺, Rb⁺, Cs⁺, Mg²⁺, Ca²⁺, N⁺R^jR^kR^lR^m, where R^j, R^k, R^l and R^m are selected from H and C_1-6alkyl having molecular weight from 3 kDa to 1,500 kDa, when R^1b–R^4b all represent H, R^5b is acetyl, and X^b represents -O-Na⁺.

EFFECT: novel compound, effective for encapsulating drugs, and a pharmaceutical composition based thereon are disclosed.

11 cl, 9 ex, 22 tbl, 119 dwg