发明名称 High-Molecular Weight Conjugate Of Resorcinol Derivatives
摘要 Provided is a high-molecular weight conjugate of resorcinol derivatives which is excellent in water solubility and stability and has high antitumor activity even when used in a smaller total drug amount than the resorcinol derivatives. The high-molecular weight conjugate of resorcinol derivatives comprises a structure in which a carboxyl group of polymer moiety having a carboxyl group in the side chain and polyethylene glycol moiety is linked to a hydroxyl group of resorcinol derivatives via an ester bond.
申请公布号 US2015011715(A1) 申请公布日期 2015.01.08
申请号 US201414497703 申请日期 2014.09.26
申请人 Nippon Kayaku Kabushiki Kaisha 发明人 Nakamura Masaharu;Kitagawa Masayuki;Yamamoto Keiichirou;Seno Chieko
分类号 C08G81/00 主分类号 C08G81/00
代理机构 代理人
主权项 1. A high-molecular weight conjugate of resorcinol derivatives in which a carboxyl group in the side chain of a copolymer of a polyethylene glycol moiety and a polymer moiety having a carboxyl group in the side chain is linked to a hydroxyl group of resorcinol derivative via an ester bond, which is represented by the general formula (1): wherein R1 represents a hydrogen atom, or an alkyl group having 1 to 6 carbon atoms which may have a substituent; R2 represents a linking group; R3 represents a hydrogen atom, an acyl group having 1 to 6 carbon atoms, or an alkoxycarbonyl group having 1 to 6 carbon atoms; R4 represents the residue of the resorcinol derivative; R5 represents a group selected from the group consisting of an alkoxy group having 1 to 30 carbon atoms, an aralkyloxy group having 7 to 30 carbon atoms, an alkylamino group having 1 to 30 carbon atoms which may have a substituent, a di(C1-C30) alkylamino group which may have substituent, an amino acid with a protected carboxyl group, and —N(R6)CONH(R7) wherein R6 and R7, which may be identical or different, each represent a cyclic alkyl group having 3 to 6 carbon atoms, or an alkyl group having 1 to 5 carbon atoms which may be substituted with a tertiary amino group; t represents an integer from 5 to 11500; d represents an integer from 1 to 200, e and f each represent an integer from 0 to 200, and d+e+f represents an integer from to 200; and the respective constituent units of the polyglutamic acid are bound in any order, wherein the resorcinol derivative is the compounds of formula (5-1):
地址 Tokyo JP