{3-[4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)PYRAZOLE-1-YL]-1-ETHYLSULFONYL-AZETIDINE-3-YL}-ACETONITRILE DICHLOROACETATE AS JANUS KINASE INHIBITOR Russian patent published in 2016 - IPC C07D487/04 A61K31/519 A01N35/00 A61P19/02 A01N29/00 

Abstract RU 2603959 C1

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a novel salt - dichloroacetate {3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazole-1-yl]-1-ethylsulfonyl-azetidine-3-yl}-acetonitrile, which is Janus kinase inhibitor (JAK), wherein it exhibits selective action on JAK3. Compounds can be used for treating autoimmune disease or disorder, such as rheumatoid arthritis, psoriatic arthritis or juvenile arthritis. {3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazole-1-yl]-1-ethylsulfonyl-azetidine-3-yl}-acetonitrile dichloroacetate has formula (1):

.

Compound of formula 1 can be obtained by reaction of {3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazole-1-yl]-1-ethylsulfonyl-azetidine-3-yl}-acetonitrile with dichloroacetic acid.

EFFECT: invention also relates to pharmaceutical composition effective for treating JAK-related diseases in form of tablets, capsules or injections, placed in pharmaceutically acceptable pack, and method of treating.

9 cl, 2 tbl, 6 ex

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RU 2 603 959 C1

Authors

Ivashchenko Aleksandr Vasilevich

Ignatev Vasilij Gennadevich

Repik Aleksej Evgenevich

Shafeev Mikhail Ajratovich

Dates

2016-12-10Published

2015-11-13Filed