PYRAZOLE DERIVATIVES AS H4 ANTAGONIST COMPOUNDS Russian patent published in 2024 - IPC C07D401/14 C07D403/14 C07D405/14 C07D471/04 C07D487/04 A61K31/437 A61K31/4439 A61K31/506 A61P1/04 A61P11/06 A61P17/04 A61P19/02 

Abstract RU 2821516 C2

FIELD: chemistry; pharmaceutics.

SUBSTANCE: invention relates to a compound of formula (1) or a pharmaceutically acceptable salt thereof, which have H4 receptor antagonist activity. In formula (1), X is CH or N; n is equal to 2; R1 is selected from H or C1-3 alkyl; R2 is H or methyl and A is an optionally substituted pyrazole ring which is bonded to the ring containing X by a carbon-carbon bond, where (i) A is an optionally substituted pyrazole ring selected from the following, where R3 is selected from H; C1-6 non-aromatic hydrocarbon group selected from alkyl, optionally substituted with 1–6 fluorine atoms, or cycloalkyl, optionally substituted with 1–6 fluorine atoms; (CH2)mR6, where m is from 1 to 3 and R6 is selected from CN, OH, C1-C3 alkoxy and optionally substituted 4–6-membered saturated heterocyclic ring containing 1 heteroatom selected from O and N, where the optional substitute is CO2R7, where R7 is C1-3 alkyl; where R4 and R5 are independently selected from a C1-6 non-aromatic hydrocarbon group selected from alkyl, optionally substituted with 1–6 fluorine atoms, or cycloalkyl, optionally substituted with 1–6 fluorine atoms; and (CH2)pR9, where p is from 0 to 3 and R9 is selected from CN, halogen, OH, C1-C3 alkoxy and SR8, where R8 is C1-C3 alkyl; or R4 and R5 can be optionally connected to form fused 5- or 6-member ring; or R4 and R3 can be optionally connected to form fused 5-member aliphatic ring; or where (ii) A is selected from a group consisting of , and several other values given in the claims. Invention also relates to a pharmaceutical composition containing said compound.

EFFECT: compounds of the present invention can be used to treat diseases associated with H4 receptor antagonist activity.

19 cl, 1 dwg, 4 tbl, 100 ex

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RU 2 821 516 C2

Authors

Braun Dzhajls Albert

Kongriv Majls Styuart

Teobald Barri Dzhon

Fildkhaus Sharlotta

Svejn Najdzhel Alan

Pikvort Mark

Bottegoni Dzhovani

Dates

2024-06-25Published

2019-10-21Filed