SUBSTITUTED PYRAZOLOAZEPINE-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS Russian patent published in 2021 - IPC C07D491/20 A61K31/55 A61P17/00 

Abstract RU 2762279 C2

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the general formula (I), in which R1 and R4 are independently selected from a group consisting of hydrogen and (C1-C4)alkyl; R2 and R3 are independently selected from a group consisting of hydrogen and (C1-C4)alkyl; or R2 and R3, together with a carbon atom, with which they are connected, form cyclopropyl or oxetanyl ring; n=0, 1 or 2; Q is selected from a group consisting of -O-C(O)-R5; R5 is selected from a group consisting of (C1-C6)alkyl, (C3-C6)cycloalkyl, phenyl; where the specified phenyl is optionally substituted with one or more substituents independently selected from R6, or where the specified R5 is optionally benzodioxol; and where the specified (C1-C6)alkyl, (C3-C6)cycloalkyl are optionally substituted with one or more substituents independently selected from R7; R6 consists of halogen, cyano, hydroxyl, (C1-C4)alkyl, halogen(C1-C4)alkyl, (C1-C4)alkyloxy, -S(O)2Rx, -S(O)2NRaRb, -C(O)Rx and -C(O)NRaRb; R7 consists of halogen, hydroxyl, (C1-C4)alkoxy, -S(O)2Rx and -SRx; Rx consists of (C1-C6)alkyl and (C3-C6)cycloalkyl; Ra and Rb are independently selected from a group consisting of hydrogen, (C1-C4)alkyl, phenyl-(C1-C4)alkyl, or Ra and Rb, together with a nitrogen atom, with which they are connected, form 5-6-element heterocycloalkyl, which may contain an additional heteroatom selected from O or N, where the specified heterocycloalkyl is optionally substituted with one (C1-C4)alkyl, -C(O)Rx; or to its pharmaceutically acceptable salt. The invention also relates to a pharmaceutical composition for the treatment or relief of a disease, disorder or condition reacting to PDE4 inhibitory activity based on the specified compounds.

EFFECT: new compound and pharmaceutical composition based on it, which can be used in medicine for the treatment of skin diseases or conditions, are obtained.

(I)

18 cl, 17 tbl, 382 ex

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RU 2 762 279 C2

Authors

Lyan, Sifu

Larsen, Jens

Nilsen, Simon Feldbek

Andersen, Peter

Dates

2021-12-17Published

2016-12-12Filed