Nippon Kayaku Kabushiki Kaisha

Chieko Seno

Masayuki Kitagawa

Hisao Ekimoto

Masaharu Nakamura

Keiichirou Yamamoto

Masao Onishi

Kazutoshi Takashio

Kazuhisa Hara

Takeshi Nakanishi

Teruyuki Sakai

Keiko Ebara

Disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein an amide bond is not used. The compound has chemical stability and adequate drug release rate in the living organism. Specifically disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein a substituent represented by formula (I) is bonded to a carboxy group of a block copolymer which is composed of a polyethylene glycol and a polymer having a carboxy group in a side chain, or a pharmacologically acceptable salt thereof. 

Polymer conjugate of folic acid or folic acid derivative

Disclosed is a water-soluble high-molecular weight conjugate of physiologically active substances which enable medicament to release without depending on the enzymes in a living body and which is expected to have a useful therapeutic effect. A high-molecular weight conjugate of a physiologically active substance has a substituent group represented by a general formula (1) bonded to a side-chain carboxy group of a block copolymer which has a polyethylene glycol moiety and either a polyaspartic acid moiety or a polyglutamic acid moiety. Formula (1): &#x2014;Ar&#x2014;CR15R16-O&#x2014;C(&#x2550;O)-A [In the formula: Ar represents an aromatic hydrocarbon group optionally a substituent group, or an aromatic heterocyclic group optionally having a substituent group; R15 and R16 independently represent a hydrogen atom or a (C1-C6) alkyl group optionally having a substituent group; and A represents a residual group of a physiologically active substance that has an carboxy group, or a residual group of a physiologically active substance that has an amino group].

High-molecular weight conjugate of physiologically active substances

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

Effective treatment of tumors, especially carcinomas, can be achieved by administering to man a photochemotherapeutic agent containing as an active ingredient a compound showing maximum absorption in the wavelength region of 800 to 1,200 nm, and then applying light rays of a wavelength of 800 to 1,200 nm.

Remedies for photochemotherapy

Growing community of inventors

Tokyo, Japan

Chieko Seno