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(19)

(11)

2 721 949

(13)

(51)

IPC

C07D305/14(2006-01-01)

C07D475/08(2006-01-01)

C07D487/04(2006-01-01)

C07D491/44(2006-01-01)

C07D491/52(2006-01-01)

A61K31/337(2006-01-01)

A61K31/436(2006-01-01)

A61K31/395(2006-01-01)

A61K31/519(2006-01-01)

A61P35/00(2006-01-01)

(21) (22)

Application

2018107843, 2016-09-21

(24)

Start date

2016-09-21

(22)

Actual filing date

2016-09-21

(45)

Published

2020-05-25

(72)

Inventor

Callmann, Cassandra E.Thompson, Matthew P.Leguyader, Clare L. M.Gianneschi, Nathan C.Bertin, Paul A.

(73)

Holder

The Regents Of The University Of CaliforniaVybyl Holdings, Inc.

MODIFIED CYTOTOXINS AND THERAPEUTIC APPLICATION THEREOF Russian patent published in 2020 - IPC C07D305/14 C07D475/08 C07D487/04 C07D491/44 C07D491/52 A61K31/337 A61K31/436 A61K31/395 A61K31/519 A61P35/00

Abstract RU 2721949 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a compound of formula (I) A¹—X¹—X²—A² (I), where A² is a paclitaxel fragment; -X²-X¹-A¹ is -C(=O)-(CH₂)_n1-C(=O)-OH, where n1 is integer from 12 to 24; or -X²-X¹-A¹ is -C(=O)-(CH₂)₇-CH=CH-(CH₂)₇-C(=O)-OH. Also disclosed are pharmaceutical compositions for treating cancer.

EFFECT: invention enables delivering increased toxic amounts of cytotoxin to cancer cells (exempli gratia, a solid tumor) with reduced side effects with respect to other non-cancer cells.

18 cl, 2 dwg, 8 tbl, 18 ex

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RU 2 721 949 C2

Authors

Callmann, Cassandra E.

Thompson, Matthew P.

Leguyader, Clare L. M.

Gianneschi, Nathan C.

Bertin, Paul A.

Dates

2020-05-25—Published

2016-09-21—Filed