BLOCK-COPOLYMER CONJUGATE OF A PHYSIOLOGICALLY ACTIVE SUBSTANCE Russian patent published in 2020 - IPC A61K31/4745 A61K31/4748 A61K47/50 C08G81/00 C08G65/333 A61P35/00 A61K9/51 

Abstract RU 2732612 C2

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to a macromolecular derivative of a physiologically active substance and use thereof. Disclosed are block copolymers containing a polyethylene glycol segment bound to a segment of a polyamino acid derivative, conjugated with a physiologically active substance, in which the molecular weight of the block copolymer ranges from 2 to 15 kDa, and the light-scattering intensity of 1 mg/ml of the aqueous block copolymer solution, measured using a photometer for measuring scattering of laser radiation under the following measurement conditions: measurement temperature of 25 °C, scattering angle of 90° and wave length 632.8 nm—at least twice or more than intensity of light scattering of toluene measured under the same conditions. Nanoparticles obtained from the block copolymer are suitable for delivering a physiologically active substance into the deeper parts of the affected target tissue and sensitizing the involved target tissue. Block-copolymer is used as a part of a pharmaceutical product for treating focal diseases of tissues and an anticancer agent.

EFFECT: disclosed block copolymer has improved efficacy and safety due to the penetration of the involved target tissue and the increased renal excretion properties, thereby sensitizing normal tissues with physiologically active substance.

15 cl, 7 tbl, 11 ex, 7 dwg

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RU 2 732 612 C2

Authors

Onda Takesi

Masuda Akira

Yamakava Ken

Tomiyama Tisato

Eneta Yasusi

Akatsu Yuiti

Yamamoto Keitiro

Motizuki Ayaka

Dates

2020-09-21Published

2016-02-19Filed