ANTI-INFLAMMATORY COMPOUND, PRODUCTION AND APPLICATION THEREOF Russian patent published in 2021 - IPC C07D401/04 C07D405/12 C07D409/12 C07D213/68 A61K31/4412 A61P17/00 A61P29/00 

Abstract RU 2759626 C1

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to the field of pharmaceutical chemistry, in particular, to an anti-inflammatory compound with the structure (I), wherein RA constitutes hydrogen, an alkyl containing 1 to 6 carbon atoms, and one or several hydrogen atoms in the above groups, attached to the carbon in said groups, are optionally substituted with an alkyl containing 1 to 6 carbon atoms, a cycloalkyl constituting a three-membered, four-membered, five-membered, or six-membered cycle, or a halogen; RB constitutes hydrogen, an alkyl containing 1 to 6 carbon atoms, a cycloalkyl constituting a three-membered, four-membered, five-membered, or six-membered cycle, a heterocycloalkyl constituting an oxo/thio three-membered, four-membered, five-membered, or six-membered cycle, an alkenyl containing 2 to 4 carbon atoms, or alkynyl containing 2 to 4 carbon atoms, and one or several hydrogen atoms in the above groups, attached to the carbon in said groups, are optionally substituted with an alkyl containing 1 to 6 carbon atoms, a cycloalkyl constituting a three-membered, four-membered, five-membered, or six-membered cycle, or a halogen, and one or several carbon atoms in said groups are optionally substituted with sulphur, a sulphur atom, sulphoxide, sulphone or sulphonyl; RC constitutes hydrogen; RD1 constitutes hydrogen, oxygen, hydroxy, cyano, alkyl containing 1 to 6 carbon atoms, phenyl, an ester group, carboxyl, or alkynyl containing 2 to 4 carbon atoms, and one or several hydrogen atoms in the above groups, attached to the carbon/oxygen in said groups, are optionally substituted with an alkyl containing 1 to 6 carbon atoms, a cycloalkyl constituting a three-membered, four-membered, five-membered, or six-membered cycle, an alkynyl containing 2 to 4 carbon atoms, an alkenyl containing 2 to 4 carbon atoms, or a phenyl, and one or several carbon atoms in said groups are optionally substituted with a sulphur atom; the C1-RD1 bond constitutes a single or double bond; RD2 constitutes hydrogen or a cyano; G1 constitutes a single bond, a double bond or a cyclopropane containing C1 and C2; and RE constitutes an alkyl containing 1 to 6 carbon atoms, or a halogen. Also described are methods for producing the above compounds are described, as well as an application thereof for treatment of skin diseases associated with PDE4, and a medicinal product for treatment of inflammatory skin diseases, based on compounds by the formula (I).

EFFECT: produced and described compounds with a strong inhibitory effect on PDE4, capable of easily permeating the skin and being used in treatment of inflammatory skin diseases.

20 cl, 1 tbl, 123 ex

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RU 2 759 626 C1

Authors

Shen, Wang

Liu, Pengfei

Zhu, Jinping

Luo, Qiuping

Ke, Pingbo

Liu, Yufei

Shen, Jida

Dates

2021-11-16Published

2019-03-21Filed