Nippon Kayaku Kabushiki Kaisha

Kazutoshi Takashio

Masayuki Kitagawa

Keiichirou Yamamoto

Keiichiro Yamamoto

Akira Masuda

Keizou Ishikawa

Chieko Seno

Takeshi Onda

Hiroko Mashiba

Masao Shibata

Keiko Ebara

A novel podophyllotoxin derivative, which is capable of releasing a drug without depending on biological enzymes and can be expected to have an effective therapeutic effect and is soluble in water has been demanded. A polymer having a polyethyleneglycol structural unit and two or more succinic monoamide structural units, particularly a polymer conjugate of a podophyllotoxin in which a carboxylic acid group of polyethyleneglycol/polyaspartic acid copolymer and a hydroxyl group of podophyllotoxin and linked via an ester bond is provided.

High-molecular weight conjugate of podophyllotoxins

A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded. Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, Rand Reach independently are hydrogen atom or (C1-C6)alkyl which may have a substituent, Ris hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX&#x2014;CY represents CH&#x2014;CH or C&#x2550;C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups]. 

Polymer conjugate of bioactive substance having hydroxy group

[Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.

High-molecular weight derivative of nucleic acid antimetabolite

[Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.

High molecular weight derivative of nucleic acid antimetabolite

A derivative of a cytidine metabolic antagonist which can exert a high therapeutic effect at a low dose. A polymeric derivative of a cytidine metabolic antagonist which comprises a polymeric compound having a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a cytidine metabolic antagonist, which has such a structure that the carboxyl group in the side chain of the polymeric compound and an amino group in the cytidine metabolic antagonist are bound together to form an amide bond.

Growing community of inventors

Kita-ku, Japan

Kazutoshi Takashio