Tokyo Institute of Technology

The University of Tokyo

Nof Corporation

Nanocarrier Co., Ltd.

Osaka University

Keio University

Sbi Pharmaceuticals Co., Ltd.

Stella Pharma Corporation

Hiroyasu Takemoto

Nobuhiro Nishiyama

Takahiro Nomoto

Makoto Matsui

Keishiro Tomoda

Kazunori Kataoka

Kanjiro Miyata

Hiroki Yoshioka

Yasuki Kato

Yuji Yamamoto

Atsushi Ishii

Naoki Yamada

Shigeto Fukushima

Masaki Kamiya

Midori Hirai

Kensuke Osada

Hiroyuki Chaya

Sumiyo Watanabe

Akiko Sasaki

Kazuki Miyauchi

Masataka Nakanishi

Masaki Mori

Hideyuki Saya

HyunJin Kim

Mika Hamura

Kazuki Osakama

Osamu Nagano

Hideshi Ishii

Yuto Honda

Takanori Inaba

Xiaohang Sun

Kenji Tsuchihashi

Kana Kohmoto

Abdul-Hackam Ranneh

Kentaro Suina

Tsukasa Nishimori

Yukiya Inoue

Ying Yao

Kaito Kanamori

Masamitsu Konno

Kanjiiro Miyata

A conjugate is provided in which a deferoxamine-type compound, which is at least one compound selected from the group consisting of deferoxamine or an ion or salt thereof, and a derivative thereof, and a biocompatible polymer are conjugated, where the biocompatible polymer contains a first biocompatible polymer chain and a second biocompatible polymer chain that is different from the first biocompatible polymer chain.

Conjugate and cancer therapeutic agent

A bio-related substance bonded to a branched and degradable polyethylene glycol derivative that is degraded in the cells represented by the following formula (A): wherein each symbol is as defined in the present specification, is provided by the present invention.

Branched degradable polyethylene glycol binder

The invention provides a bio-related substance bonded to a high-molecular-weight polyethylene glycol derivative that does not cause vacuolation of cells. The bio-related substance bonded to a degradable polyethylene glycol derivative is represented by the formula (A): wherein m is 1-7, n1 and n2 are each independently 45-682, p is 1-4, R is an alkyl group having 1-4 carbon atoms, Z is an oligopeptide with 2-8 residues composed of neutral amino acids excluding cysteine, Q is a residue of a compound having 2-5 active hydrogens, D is the bio-related substance, L1, L2, L3, L4 and L5 are each independently a single bond or a divalent spacer, and y is 1-40.

Degradable polyethylene glycol conjugate

The invention provides a high-molecular-weight polyethylene glycol derivative that does not cause vacuolation of cells. The degradable polyethylene glycol derivative is represented by the following formula (1): wherein m is 1-7, n1 and n2 are each independently 45-682, p is 1-4, R is an alkyl group having 1-4 carbon atoms, Z is an oligopeptide with 2-8 residues composed of neutral amino acids excluding cysteine, Q is a residue of a compound having 2-5 active hydrogens, X is a functional group capable of reacting with a bio-related substance, and L, L, L, Land Lare each independently a single bond or a divalent spacer.

Degradable polyethylene glycol derivative

A pH-responsive polymer formed of a biocompatible polymer to which a group which is electrically neutral under pH environments of more than 7 and which changes to be cationic at pH 7 or less is bonded.

PH-responsive polymer and drug delivery system

The present invention pertains to a ligand that contains a plurality of groups represented by formula (1) and is capable of multivalently binding to a glutamine transporter expressed in excess in a cancer cell compared to a normal cell.

Ligand capable of multivalently binding to glutamine transporter, and composition comprising same

The present invention pertains to: a p-boronophenylalanine derivative that comprises a polymer to which a group represented by formula (I) is linked directly or via a linker; a composition containing same; and a kit for producing said derivative and composition.

P-boronophenylalanine derivative and composition containing same, and kit for producing said derivative and composition

The present invention is directed to provide antitumor agent including water-soluble sulfasalazine as an active ingredient. Antitumor agents were obtained with, as the water-soluble sulfasalazine, a PEG-modified sulfasalazine represented by the following formula: wherein an average value of n is 4 or larger and 1136 or smaller.

Antitumor agent

A unit structure-type pharmaceutical composition includes a single nucleic acid, such as an antisense nucleic acid, electrostatically bound to a single block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charges of the nucleic acid are counterbalanced, at least substantially, by the positive charges of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment. The block copolymer thereby improves the blood retention capability of the nucleic acids.

Unit structure-type pharmaceutical composition for nucleic acid delivery

A unit structure-type pharmaceutical composition includes at least one nucleic acid, such as siRNA, electrostatically bound to at least one block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charge(s) of the nucleic acid are counterbalanced, at least substantially, by the positive charge(s) of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment(s). The at least one block copolymer thereby improves the blood retention capability of the nucleic acid(s).

There are provided an anionic polymer, a polyion complex, and a ternary polymer composite, each of which is stable in a biological environment and is capable of realizing small RNA delivery without causing any undesired immune response. An anionic polymer according to an embodiment of the invention includes: a main chain which includes repeating units having carboxyl groups; and a side chain which is linked with part of the carboxyl groups in the main chain and is represented by the following formula:-A-B&#x2014;Xwhere: A represents a residue having one or more aminoethyl bonds; B represents an in vivo cleavable bond; and X represents a small RNA. A polyion complex according to an embodiment of the invention includes the anionic polymer as described above and a cationic polymer. A ternary polymer composite according to an embodiment of the invention includes the polyion complex as described above and a charge conversional polymer.

Anionic polymer, polyion complex and ternary polymer composite using anionic polymer, and pharmaceutical composition

The present invention relates to a block copolymer containing an uncharged hydrophilic polymer chain block and a cationic polyamino acid chain block, wherein the hydrophilic polymer chain block is covalently bound to one end of the main chain of the polyamino acid chain block, and the hydrophobic group is covalently bound to the side chains of not less than 10% and not greater than 70% of amino acid repeating units in the polyamino acid chain block. This block copolymer forms a stable aggregate with siRNA, a small-molecule nucleic acid, under a physiological condition.

Copolymer including uncharged hydrophilic block and cationic polyamino acid block having hydrophobic group in part of side chains, and use thereof

Growing community of inventors

Tokyo, Japan

Hiroyasu Takemoto