BORON-CONTAINING PDE4 INHIBITORS Russian patent published in 2023 - IPC C07F5/02 A61K31/69 A61P29/00 A61P17/00 

Abstract RU 2793936 C2

FIELD: medicinal chemistry.

SUBSTANCE: boron-containing compound of formula (IA) or formula (IB) or a pharmaceutically acceptable salt thereof. In formula (IA) and formula (IB): B is boron; A1 and A2 are independently O or S; R1, R2 and R5 are each independently H, deuterium, (C1-C6)alkoxy, (C1-C6)alkoxy-d1-13, (C1-C6)alkyl, (C1-C6)alkyl-d1-13, cyano, halogen or halo(C1-C6)alkyl; R3 and R4 are each independently (C1-C6)alkyl, (C1-C6)alkyl-d1-13, (C3-C8)cycloalkyl, halo(C1-C6)alkyl or hydroxy(C1-C6)alkyl; R6, R7 and R9 are each independently H, deuterium, (C1-C6)alkyl, (C1-C6)alkyl-d1-13 or halo(C1-C6)alkyl; p is 0. (R)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol or a pharmaceutically acceptable salt thereof and (S)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol or a pharmaceutically acceptable salt thereof and crystalline forms thereof, pharmaceutical composition and use for the drug preparation for the treatment of atopic dermatitis in humans are also provided. The proposed compounds inhibit phosphodiesterase 4 (PDE4).

EFFECT: treating conditions or disorders mitigated by PDE4 inhibition.

20 cl, 12 dwg, 18 tbl, 470 ex

Formula (1A) Formula (1B)

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RU 2 793 936 C2

Authors

Strohbach, Joseph Walter

Blakemore, David Clive

Jones, Peter

Limburg, David Christopher

Oderinde, Martins Sunday

Torella, Rubben Federico

Yeoh, Thean Yeow

Akama, Tsutomu

Jacobs, Robert Toms

Perry, Matthew Alexander

Plattner, Jacob John

Zhou, Yasheen

Dates

2023-04-10Published

2019-10-01Filed