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(19)

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2 795 146

(13)

(51)

IPC

C07D401/04(2006-01-01)

C07D401/14(2006-01-01)

C07D417/14(2006-01-01)

C07D471/10(2006-01-01)

C07D487/04(2006-01-01)

C07D495/14(2006-01-01)

A61K31/454(2006-01-01)

A61K31/4725(2006-01-01)

A61P35/00(2006-01-01)

(21) (22)

Application

2019123462, 2018-01-31

(24)

Start date

2018-01-31

(22)

Actual filing date

2018-01-31

(45)

Published

2023-04-28

(72)

Inventor

Crew, Andrew, P.Berlin, MichaelDong, HanqingHornberger, Keith, R.Qian, YiminSnyder, Lawrence, B.Wang, JingZimmermann, Kurt

(73)

Holder

Arvinas Operations, Inc.

CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM Russian patent published in 2023 - IPC C07D401/04 C07D401/14 C07D417/14 C07D471/10 C07D487/04 C07D495/14 A61K31/454 A61K31/4725 A61P35/00

Abstract RU 2795146 C2

FIELD: pharmaceutical chemistry.

SUBSTANCE: group of inventions relates to the field of pharmaceutical chemistry, namely to a compound of the formula CLM-L-PTM, its pharmaceutically acceptable salt, enantiomer, stereoisomer and specific compounds indicated in the claims, pharmaceutical compositions and applications based on them. In the formula CLM-L-PTM, PTM is an androgen receptor binding moiety and has a structure selected from (ABM-b) and (ABM-d); CLM has a chemical structure selected from (r), (e), (o), (p`), (bc), (bd), and is a Cereblon ligand; L is a chemical linker moiety covalently linking CLM and PTM; values of L and its substituents, Q₁, Q₂, Q₃, Q₄, Q₅ and substituents (ABM-b), (ABM-d), (r), (e), (o), (p`) , (bc) and (bd) are presented in the claims.

EFFECT: chimeric compounds of the formula CLM-L-PTM inducing the destruction of the target protein in the cell.

30 cl, 1 dwg, 6 tbl

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RU 2 795 146 C2

Authors

Crew, Andrew, P.

Berlin, Michael

Dong, Hanqing

Hornberger, Keith, R.

Qian, Yimin

Snyder, Lawrence, B.

Wang, Jing

Zimmermann, Kurt

Dates

2023-04-28—Published

2018-01-31—Filed