SELECTIVE KINASE JAK1 INHIBITOR Russian patent published in 2024 - IPC C07D401/14 C07D403/14 C07D405/14 C07D413/14 C07D417/14 C07D471/04 A61K31/506 A61P11/06 A61P37/00 

Abstract RU 2818002 C2

FIELD: chemistry.

SUBSTANCE: group of inventions relates to organic chemistry and includes a compound of formula (I), pharmaceutically acceptable salts thereof, a pharmaceutical composition and a combination containing it, a method of inhibiting JAK1 and a method of treating. In formula (I), ring A is selected from a group specified in the claim, R1 is hydrogen, halogen, hydroxyl, amino, cyano or C1-3alkyl; R2 is hydrogen, C1-12alkyl or C1-12alkoxy, optionally mono- or multi-substituted with halogen, hydroxyl, amino, cyano or C1-12alkoxyl; each of R3 and R4 is independently absent or represents halogen, hydroxyl, C1-6alkyl, carboxyl, C1-6alkoxyl, C1-6alkoxycarbonyl, -NRaRb, -C(O)NRaRb, 3–10-membered saturated or unsaturated carbocyclyl, 3–10-saturated or unsaturated heterocyclyl having 1, 2 or 3 heteroatoms selected from N, O or S, which can be optionally mono- or independently multi-substituted with halogen, hydroxyl, C1-6alkyl, C1-6 alkoxy, C1-6 carboxyl, C1-6 alkoxycarbonyl, -NRaRb, -C(O)NRaRb, where one or more ring-forming group-CH2-carbocyclyl or heterocyclyl, having 1, 2 or 3 heteroatoms selected from N, O or S, can be replaced by a group -C(O)-; where each of Ra and Rb is independently selected from hydrogen, C1-6alkyl, C1-6 alkylcarbonyl, which can be optionally mono- or independently multi-substituted with halogen, hydroxyl or C1-6 alkoxy.

EFFECT: compounds of formula (I) have JAK1 inhibitory activity.

18 cl, 8 tbl, 82 ex

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RU 2 818 002 C2

Authors

Qi Changhe

Tsui Honchung

Zeng Qingbei

Yang Zhenfan

Zhang Xiaolin

Dates

2024-04-23Published

2020-04-17Filed