HETEROCYCLIC COMPOUNDS FOR TYROSINE KINASE 2 ACTIVITY MEDIATION Russian patent published in 2024 - IPC C07D487/04 C07D403/14 C07D403/04 C07D405/14 A61K31/506 A61K31/5377 A61P1/04 A61P3/10 A61P11/00 A61P17/06 A61P25/28 A61P27/02 A61P35/00 A61P37/00 

Abstract RU 2826012 C2

FIELD: chemistry; pharmaceutics.

SUBSTANCE: present invention relates to heterocyclic compounds or pharmaceutically acceptable salts thereof, suitable for controlling or inhibiting Janus kinase (JAK) activity, in particular tyrosine kinase 2 (TYK2), specifically to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a stable isotope, a stereoisomer, in which R1 is pyrazolyl, where one pyrazolyl hydrogen is optionally substituted -COORb, -C(O)Rb, -C(O)NRbRc, C1–6alkyl, CD3 or piperidinyl; R2 is H; R3 is H, halogen, cyano, C1-6 alkyl, or OC1–6alkyl; R4 and R5 are independently selected from H, or C1-6 alkyl; R6 and R7 are independently selected from H, or R6 and R7 are combined in the form of oxo; L is a bond, C1-6 alkylene, -C(O)-, -C(O)O-, -C(O)N(Ra)- or -S(O)2-; A is H, C1-6alkyl, C3-6 cycloalkyl, 4-membered heterocyclyl, in which one ring atom is N or O, or 5–6-membered heteroaryl, in which from 1 to 3 ring atoms are N or O heteroatoms, where one or more hydrogen atoms of alkyl, cycloalkyl and heteroaryl are optionally substituted with halogen, cyano or -ORd; Ra represents H; Rb and Rc are independently selected from H or C1-6alkyl, and Rd is independently selected from H, C1–6 alkyl or morpholinyl. Invention also relates to specific compounds, as well as to a pharmaceutical composition based on said compounds.

EFFECT: obtaining alternative compounds for treating TYK2-mediated diseases.

11 cl, 101 ex

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RU 2 826 012 C2

Authors

Chen, Syanyan

Pan, Yujchen

Dates

2024-09-03Published

2020-06-24Filed