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2 797 343

(13)

(51)

IPC

C08F8/42(2006-01-01)

C08F16/06(2006-01-01)

C08G69/48(2006-01-01)

A61K31/69(2006-01-01)

A61K41/00(2006-01-01)

A61K47/58(2017-01-01)

A61K49/00(2006-01-01)

A61P35/00(2006-01-01)

(21) (22)

Application

2020127562, 2019-02-19

(24)

Start date

2019-02-19

(22)

Actual filing date

2019-02-19

(45)

Published

2023-06-02

(72)

Inventor

Nisiyama, NobukhiroNomoto, TakakhiroInoue, YukiyaYao, InKanamori, KaitoTakemoto, KhiroyasuMatsui, MakotoTomoda, Keisiro

(73)

Holder

Tokio Instityut Of TeknolodzhiStella Farma Korporejshn

PAIR-BORPHENYLALANINE DERIVATIVE AND A COMPOSITION CONTAINING THESE, AND A KIT FOR OBTAINING THE MENTIONED DERIVATIVE AND COMPOSITION Russian patent published in 2023 - IPC C08F8/42 C08F16/06 C08G69/48 A61K31/69 A61K41/00 A61K47/58 A61K49/00 A61P35/00

Abstract RU 2797343 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a para-borophenylalanine derivative comprising a polymer linked, either directly or via a linker, to a group represented by formula (I). In formula (I): the arrows indicate the bond to the adjacent atom, X¹-X⁴ are each independently H, ¹⁸F or ¹⁹F. The polymer is selected from the group consisting of polyvinyl alcohol, polyether and polypeptide, and the number average molecular weight of the para-borophenylalanine derivative is 1,000 Da or more. Also pharmaceutical compositions containing a para-borophenylalanine derivative and a kit for preparing pharmaceutical compositions are proposed.

EFFECT: invention makes it possible to implement selective accumulation and long-term retention of boron in tumors, while achieving an excellent ratio of boron concentrations in tumor/normal tissues and a ratio of boron concentrations in tumor/blood.

12 cl, 34 dwg, 1 tbl, 24 ex

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RU 2 797 343 C2

Authors

Nisiyama, Nobukhiro

Nomoto, Takakhiro

Inoue, Yukiya

Yao, In

Kanamori, Kaito

Takemoto, Khiroyasu

Matsui, Makoto

Tomoda, Keisiro

Dates

2023-06-02—Published

2019-02-19—Filed