SUBSTITUTED PYRAZOLOAZEPINE-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS Russian patent published in 2022 - IPC C07D491/20 A61K31/55 A61P17/00 

Abstract RU 2768746 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a compound of general formula (I), where R1 and R4 are independently selected from the group consisting of hydrogen and (C1-C4)alkyl; R2 and R3 are independently selected from the group consisting of hydrogen and (C1-C4)alkyl; n = 0, 1 or 2; and when n is 0, R4 is absent; Q is selected from the group consisting of -O-C(O)-R 5 and -O-C(O)-(C1-C6)alkyl-R5; R5 is selected from a group consisting of (5–6)-membered heteroaryl containing 1–3 heteroatoms, selected from N, O or S, benzimidazolyl and (4–6)-membered heterocycloalkyl containing 1 heteroatom selected from N, O, S or S(O)2, where said heteroaryl, benzimidazolyl and heterocycloalkyl are optionally substituted with one or more substituents independently selected from R6; R6 consists of hydroxyl, (C1-C4)alkyl, (C1-C4)alkyloxy, -ORx, -C(O)NRaRb, -C(O)ORa, -C(O)Ra, (C3-C4)cycloalkyl; Rx is (C1-C4)alkyl; Ra and Rb independently represent (C1-C4)alkyl; or a pharmaceutically acceptable salt thereof. Invention also relates to a pharmaceutical composition for inhibiting phosphodiesterase 4 (PDE4) based on said compounds.

EFFECT: obtaining novel compounds and a pharmaceutical composition based thereon, which can be used in medicine for treating or relieving inflammatory skin diseases or conditions.

19 cl, 5 tbl, 115 ex

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RU 2 768 746 C2

Authors

Lyan, Sifu

Larsen, Jens

Nilsen, Simon Feldbek

Andersen, Peter

Dates

2022-03-24Published

2017-12-12Filed