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US 2011/0212901 A1Published application
Hyaluronic acid derivative and pharmaceutical composition thereof
AssigneesNational University Corporation Tokyo Medical and Dental Unversity, Chugai Seiyaku Kabushiki Kaisha
InventorsKazunari Akiyoshi, Takashi Nakai, Tai Hirakura, Tsuyoshi Shimoboji
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Abstract
The present invention provides a hydrophobic group-introduced hyaluronic acid derivative comprising at least one repeating unit represented by the formula (I): wherein R1, R2, R3, R4, Z, n, Ra, Y, and X1 are as defined in the specification.
Claims18
A hyaluronic acid derivative containing a hydrophobic group, comprising at least one repeating unit represented by the formula (I):
- wherein
- R1, R2, R3, and R4 are each independently selected from a hydrogen atom, C1-6 alkyl, formyl, and C1-6 alkylcarbonyl;
- Z represents a direct bond, or a peptide linker comprising 2 to 30 arbitrary amino acid residues;
- X1 is a hydrophobic group selected from the groups represented by the following formulas:
- —NRb—R,
- —NRb—COO—R,
- —NRb—CO—R,
- —NRb—CO—NRc—R,
- —COO—R,
- —O—COO—R,
- —S—R,
- —CO—Ya—S—R,
- —O—CO—Yb—S—R,
- —NRb—CO—Yb—S—R, and
- —S—S—R;
- Ra, Rb, and Rc are each independently selected from a hydrogen atom, C1-20 alkyl, amino C2-20 alkyl, and hydroxy C2-20 alkyl, wherein 1 to 3 groups selected from —O— and —NRf— are optionally inserted in an alkyl moiety of these groups;
- Rf is selected from a hydrogen atom, C1-12 alkyl, amino C2-12 alkyl, and hydroxy C2-12 alkyl, wherein 1 or 2 groups selected from —O— and —NH— are optionally inserted in an alkyl moiety of these groups;
- R is a steryl group;
- Y is C2-30 alkylene or —(CH2CH2O)m—CH2CH2—, wherein 1 to 5 groups selected from —O—, —NR9—, and —S—S— are optionally inserted in the alkylene;
- Rg is selected from a hydrogen atom, C1-20 alkyl, amino C2-20 alkyl, and hydroxy C2-20 alkyl, wherein 1 to 3 groups selected from —O— and —NH— are optionally inserted in an alkyl moiety of these groups;
- Ya is C1-5 alkylene;
- Yb is C2-8 alkylene or C2-8 alkenylene;
- and
- m is an integer selected from 1 to 100.
21 more elements
Dependencies are inferred from the claim text.