Patent ID: 8188222

Claim:
The high molecular weight derivative of a nucleic acid antimetabolite represented by the following formula (1): wherein R represents a hydrogen atom or a C1-C6 alkyl group; A represents a hydrogen atom, a C1-C6 acyl group or a C1-C6 alkoxycarbonyl group; a+b represents from 3 to 200 as an average value, while a represents 75 to 100% of a+b, and b represents 0 to 25% of a+b; n represents from 5 to 2000 as an average value; X represents a hydrophobic linker represented by formula (5): wherein Q represents the side chain of a neutral amino acid; each instance of Y independently represents a group selected from the group consisting of a residue of nucleic acid antimetabolite represented by formula (2): wherein —Rf represents a group selected from the group of substituents of formula (3): A hydroxyl group, and —N(R1)CONH(R2); wherein the nucleic acid antimetabolite residue is bound by an ester or amide linkage; wherein R1 and R2 may be identical or different, and are each a C1-C6 alkyl group which may be substituted with a tertiary amino group, and wherein, assuming that a+b is 100%, the number of nucleic acid antimetabolite residue is 5 to 80%, the number of —N(R1)CONH(R2) is 0 to 70%, and the number of hydroxyl group is 0 to 70%) and the constituent units of polyglutamic acid are bound in any order.