Nanocarrier Co., Ltd.

Nonocarrier Co., Ltd.

Mitsunori Harada

Yasuki Kato

Takashi Shimizu

Hiroyuki Saito

Naoya Shibata

Miho Ohuchi

Iulian Bobe

Katsutoshi Kobayashi

Tatsuyuki Hayashi

Ryosuke Tanaka

IuIian Bobe

Yuko Amano

A pharmaceutical composition includes a block copolymer having a hydrophilic segment, a hydrophobic segment, and a boronic acid compound bound to a side chain of the hydrophobic segment via a linker moiety that includes a heterocyclic structure. The heterocyclic structure contains a cyclic skeleton that includes a boron atom of the boronic acid compound, one or two atom(s) X bound to the boron atom and selected from an oxygen atom and a nitrogen atom, and one or two carbon atom(s) (respectively) bound to the atom(s) X. The block copolymer further includes at least one organic group bound to the carbon atom(s). The organic group(s) contain(s) an aromatic group or cyclic alkyl group that sterically protects a boronic acid ester bond and/or a boron amide bond resulting from bonding between the boron atom and the atom(s) X.

Pharmaceutical composition containing a block copolymer bound to a boronic acid compound

A pharmaceutical composition or combination drug, which contains, as active ingredients, (a) a coordination compound composed of a block copolymer represented by the following formula I or formula II and cisplatin, and (b) gemcitabine hydrochloride. In the formulae I and II, R, A, R, R, m and n are as defined in the description.

Pharmaceutical composition or combination drug

The present invention provides an active targeting polymer micelle encapsulating a drug, preventing an inappropriate release of a drug which may damage a normal cell. A polymer micelleincludes a backbone polymer unitthat has a target binding siteand a backbone polymer unitthat has a drugand is free from the target binding site, such polymer unitsandbeing disposed in a radial arrangement in a state where the target binding siteis directed outward and the drugis directed inward, in which: i) when the micelle is bound to a targetwhile maintaining the radial arrangement, the micelle is taken up into a cellsupplying the targetthrough endocytosis, and the drugis released into the cellby collapse of the radial arrangement in the cell; and ii) when the radial arrangement collapses in bloodbefore the micelle is bound to a target, the unitis excreted through metabolism, to thereby prevent a normal cell from being damaged by the drug

Active targeting polymer micelle encapsulating drug, and pharmaceutical composition

A pharmaceutical composition containing a drug encapsulated in a polymer micelle composition containing a first block copolymer having affinity with HDL and a second block copolymer having affinity with a lipoprotein excluding HDL, each block copolymer having a hydrophobic polymer chain segment and a hydrophilic polymer chain segment such that a plurality of block copolymers arrange radially with the hydrophobic segments directed inward and the hydrophilic segments directed outward. In the composition, a detachment of the first block copolymer is induced by HDL adhesion which forms a gap and promotes the release of a drug encapsulated, while the second block copolymer excluding an affinity with HDL controls a release speed of the drug encapsulated.

Sustained-release polymer micelle disruptable by HDL

The present invention provides a block copolymer for a drug conjugate which comprises a water-soluble polymer region consisting of polyethylene glycol and a polyamino acid region having a hydrazide group and a hydrophobic group in the side chain.

Block copolymer for drug conjugates and pharmaceutical composition

A pharmaceutical composition or combination drug, which contains, as active ingredients, (a) a coordination compound composed of a block copolymer represented by the following formula I or formula II and cisplatin, and (b) gemcitabine hydrochloride.  In the formulae I and II, R, A, R, R, m and n are as defined in the description.

The invention provides a physiologically active polypeptide- or protein-encapsulating polymer micelle composition derived from a block copolymer comprising hydrophilic segments and hydrophobic segments.

Growing community of inventors

Kashiwa, Japan

Mitsunori Harada