CARBOXAMIDE DERIVATIVES OF ISOXAZOLINE, METHOD FOR PRODUCTION AND USE THEREOF FOR TREATING INFLAMMATORY DISEASES Russian patent published in 2019 - IPC C07D413/04 C07D413/14 A61K31/422 A61P19/02 A61P29/00 

Abstract RU 2704967 C1

FIELD: chemistry.

SUBSTANCE: invention relates to carboxamide derivatives of an isoxazoline series of general formula 1, having properties which enable to deactivate receptors PAR-2 (receptors activated by proteases), as well as to a method for decontaminating the PAR-2 receptor, as well as to an active component of formula 1, having anti-inflammatory action. In general formula 1, X represents nitrogen atom, or C-H, or C-Cl; R1 substitute is 2,6-dimethylphenyl, 4-methyl-2-chlorophenyl, mesityl, 4-methoxy-3-trifluoromethylphenyl, 3,4-dimethylphenyl, 2-methyl-6-chlorophenyl, 2-trifluoromethyl-4-chlorophenyl, 4-trifluoromethoxyphenyl, 3,4-dicyanophenyl, 4-chlorpyridin-2-yl, 4-isopropoxy-3-cyanophenyl, 3-chloro-4-cyanophenyl, 4-(trifluoromethylphenyl); R2 substitute, R3 can be selected from the following set - hydrogen, C1-C6 alkyl.

EFFECT: compounds can be used for treating inflammatory diseases, particularly rheumatoid arthritis, as well as other diseases, the treatment of which can be associated with deactivation of PAR2 receptors.

4 cl, 1 tbl, 6 ex

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RU 2 704 967 C1

Authors

Korsakov Mikhail Konstantinovich

Ivanovskij Sergej Aleksandrovich

Smirnov Aleksej Vladimirovich

Rakov Andrej Aleksandrovich

Khokhlov Aleksandr Leonidovich

Kobylinskij Dmitrij Borisovich

Semenychev Evgenij Vadimovich

Panova Valeriya Anatolevna

Zvonareva Zhanna Sergeevna

Kozlova Tatyana Mikhajlovna

Petukhova Svetlana Aleksandrovna

Yaichkov Ilya Igorevich

Belova Aleksandra Vladimirovna

Yudina Natalya Valerevna

Shetnev Anton Andreevich

Dates

2019-11-01Published

2018-06-19Filed