NLRP3 INFLAMMASOME INHIBITORS Russian patent published in 2024 - IPC C07D237/14 C07D237/20 C07D401/14 C07D403/12 A61K31/501 A61P3/10 A61P9/00 A61P19/02 A61P35/00 

Abstract RU 2826735 C2

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine, namely to a compound of a certain structure or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition having inhibitory activity on the NLRP3 inflammasome signaling pathway, and to the use of said compound or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a disease or disorder, wherein signal transmission mediated by NLRP3 promotes a pathological process and/or manifestation of symptoms and/or progression of said disease or disorder. Compound of formula (I)

(I),

or a pharmaceutically acceptable salt thereof, where R1 is Cl, CH3, -OCF3 or CF3, R2 is H, halogen, C1-C4alkyl or halogen-C1-C4alkyl, R3, R4 are H, CN, C1-C4alkyl or halogen-C1-C4alkyl, Z is -O- or -NH-(CH2)n-, where n equals 0, 1 or 2, R5 is selected from the following structures:

,

where R5a is independently selected from C1-C4alkyl, hydroxy-C1-C4alkyl and H, and R5b is independently selected from -OH, C1-C4alkyl, hydroxy-C1-C4alkyl, H, halogen, oxo, halogen-C1-C4alkyl and -CO2H, and m is 0 or 1, or R5 is selected from the following structures:

,

where R5d is independently selected from H, halogen, halogen-C1-C4alkyl and C1-C4alkyl. Pharmaceutical composition having inhibitory activity on the inflammasome signaling pathway based on NOD-like receptor protein 3 (NLRP3), containing a therapeutically effective amount of the above compound or its pharmaceutically acceptable salt and one or more pharmaceutically acceptable carriers. Use of said compound or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a disease or disorder, wherein signal transmission mediated by NLRP3 promotes a pathological process and/or manifestation of symptoms and/or progression of said disease or disorder.

EFFECT: said group of inventions can be used to inhibit the NLRP3 inflammasome signaling pathway, treat or prevent diseases and/or disorders associated with NLRP3.

9 cl, 104 ex

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RU 2 826 735 C2

Authors

Gommermann, Nina

Farady, Christopher

Janser, Philipp

Mackay, Angela

Mattes, Henri

Smith, Nichola

Fooks Solovay, Catherine

Stiefl, Nikolaus Johannes

Vangrevelinghe, Eric

Velcicky, Juraj

Von Matt, Anette

Dates

2024-09-16Published

2020-05-15Filed