BIARYL DERIVATIVES AS INHIBITORS OF PROTEIN-PROTEIN INTERACTION YAP/TAZ-TEAD Russian patent published in 2024 - IPC C07D307/81 C07D401/14 C07D403/04 C07D405/04 C07D405/10 C07D405/12 C07D405/14 C07D407/12 C07D413/04 C07D417/04 C07D491/04 A61K31/343 A61K31/443 A61P35/00 

Abstract RU 2830596 C1

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof,

where X is selected from CH; and N; A is phenyl; Rw is selected from (i) hydrogen; and (ii) C1-C3 alkyl; Q is selected from (i) -C(R7)2-NH-R1; and (ii) 4-, 5- or 6-membered saturated heterocyclic ring containing one or two heteroatoms independently selected from N and O, provided that at least one N heteroatom is present and it is in the α-position with respect to the carbon atom binding Q to the rest of the molecule, where the heterocyclic ring is unsubstituted or substituted with one or more substituents independently selected from hydroxy, C1-C3alkyl and halogen; R1 is selected from (i) C1-C6alkyl and (ii) R1a; where R1a is C3-C6cycloalkyl, optionally independently substituted once or more than once with hydroxy, C1-C6alkyl or halogen; R2 is halogen; R3 is halogen; R4 is halogen; R5 is selected from C1-C6alkoxy and hydroxyC1-C6alkoxy; R6 is C(O)NHR6a; R6a is selected from (i) hydrogen and (ii) C1-C3alkyl; and each R7 is hydrogen, as well as pharmaceutical compositions based thereon.

EFFECT: obtaining novel compounds which have YAP/TAZ-TEAD protein-protein interaction (PPI) inhibitory activity and can be used to treat diseases mediated by said activity, for example, cancer or tumor.

18 cl, 176 ex, 2 tbl

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RU 2 830 596 C1

Authors

Bordas, Vincent

Brocklehurst, Cara

Chene, Patrick

Fei, Zhongbo

Furet, Pascal

Guagnano, Vito

Imbach-Weese, Patricia

Kallen, Joerg

Le Douget, Mickael

Li, Jialiang

Li, Wei

Lorthiois, Edwige Liliane Jeanne

Mckenna, Joseph

Salem, Bahaa

Schmelzle, Tobias

Sellner, Holger

Soldermann, Nicolas

Voegtle, Markus

Wartmann, Markus

Dates

2024-11-22Published

2021-03-15Filed