METHOD FOR OBTAINING AROMATIC HETEROCYCLIC COMPOUND USED AS SELECTIVE INHIBITOR OF KINASE JAK1 AND APPLICATION THEREOF Russian patent published in 2018 - IPC C07D239/48 C07D239/47 C07D401/12 A61K31/505 A61K31/506 A61P19/02 A61P3/10 A61P17/06 A61P35/00 A61P11/00 A61P25/28 A61P9/10 A61P37/08 

Abstract RU 2671195 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of general formula (I) or a pharmaceutically acceptable salt thereof. In the compound of general formula of (I)

R1 is halogen or C1-C6 alkyl; R2 represents one or more substituents selected from the group consisting of hydrogen, hydroxy, cyano, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 alkylcarbonyl and C1-C6 alkylamino; R3 is hydrogen or halogen; R4 is hydrogen or C1-C4 alkyl; X is NH, O or S; Y is CO or S(O)2; Z is a covalent bond, CH2 or (CH2)2; n is an integer from 1 to 4; and ring A is a benzene ring, a pyridine ring or a piperidine ring. Invention also relates to methods for the preparation of compounds of formula (I) comprising reacting a compound of general formula (IV) with a compound of formula (V) in an organic solvent and under the influence of a catalyst and to a process for preparing a compound of formula (IV).

,

.

EFFECT: invention can be used to treat diseases associated with abnormal activity of JAK3 and/or JAK1 kinases selected from autoimmune diseases, inflammatory diseases, cancer, myeloproliferative diseases, bone resorption diseases, or graft-versus-host disease (such diseases can be, for example, diseases selected from rheumatoid arthritis, psoriasis, Crohn's disease, systemic lupus erythematosus, multiple sclerosis, type I diabetes, allergic diseases, chronic obstructive pulmonary disease, asthma, leukemia and lymphoma).

21 cl, 1 dwg, 7 tbl, 123 ex

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RU 2 671 195 C2

Authors

Lu, Xianping

Yu, Jindi

Yang, Qianjiao

Li, Zhibin

Pan, Desi

Shan, Song

Zhu, Jiangfei

Wang, Xianghui

Liu, Xiangheng

Ning, Zhiqiang

Dates

2018-10-30Published

2015-09-14Filed