2-(3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-1-(ETHYLSULFONYL)AZETIDIN-3-YL)ACETONITRILE HEMINAPHTHYLDISULFONATE AS JANUS KINASE INHIBITOR Russian patent published in 2018 - IPC C07D487/04 A61K31/519 A61P19/02 A61P17/06 A61P3/10 A61P1/04 A61P1/06 A61P25/28 A61P5/14 A61P13/12 

Abstract RU 2644155 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula 1 having properties of Janus kinase (JAK) inhibitors. Compound of formula 1 is 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile with heminaphthyldisulfonate and corresponds to the structure

.

Method for preparing said compound comprises reaction of 2 molar equivalents of a Baricitinib base with 1,5-naphthyldisulfonic acid in a suitable solvent or solvent mixture.

EFFECT: compounds can be used for treatment of diseases selected from the group consisting of multiple sclerosis, rheumatoid arthritis, juvenile arthritis, psoriatic arthritis, type I diabetes, lupus, psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, myasthenia gravis, immunoglobulin nephropathy, autoimmune thyroid disease.

6 cl, 6 dwg, 4 tbl, 8 ex

Similar patents RU2644155C1

Title Year Author Number
{3-[4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)PYRAZOLE-1-YL]-1-ETHYLSULFONYL-AZETIDINE-3-YL}-ACETONITRILE DICHLOROACETATE AS JANUS KINASE INHIBITOR 2015
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2603959C1
{3-[(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)AZOLYL]AZETIDIN-3-YL} ACETONITRILES AS JANUS KINASE INHIBITORS 2015
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2601410C1
8-(1-{4-{(5-CHLORO-4-{(2-(DIMETHYLPHOSPHORYL)PHENYL)AMINO}PYRIMIDIN-2-YL)AMINO)-3-METHOXYPHENYL}PIPERIDIN-4-YL)-1-METHYL-1,8-DIAZASPIRO(4.5)DECAN-2-ONE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS AS AN ALK AND EGER MODULATOR FOR TREATMENT OF CANCER 2017
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2654695C1
DICHLOROACETATE OF N,N-DISUBSTITUTED N-[4-(1-METHYL-1H-INDOLE-3-YL)-PYRIMIDINE-2-YL]-5-METHOXYBENZENE-1,2,4-TRIAMINE AS EGFR MODULATOR FOR TREATING CANCER 2015
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2603960C1
DERIVATIVES OF 1-(3-AMINOPHENYL)-6,8-DIMETHYL-5-(4-IODO-2-FLUORO-PHENYLAMINO)-3-CYCLOPROPYL-1H,6H-PYRIDO[4,3-d]PYRIMIDINE-2,4,7-TRIONE AS MEK1/2 INHIBITORS 2015
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2605400C1
SUBSTITUTED N-{3-[4-(1-METHYL-1H-INDOL-3-YL)PYRIMIDIN-2-YLAMINO]-4-METHOXYPHENYL}-AMIDES AS MODULATORS OF EGFR, APPLICABLE FOR TREATING CANCER 2015
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2606949C9
SUBSTITUTED METHYL(2-{4-[3-(3-METHANESULFONYLAMINO-2-FLUORO-5-CHLORO-PHENYL)-1H-PYRAZOL-4-YL]PYRIMIDIN-2-YLAMINO}ETHYL) CARBAMATES, PROCESS FOR THEIR PREPARATION AND APPLICATION 2016
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2615986C1
N-{3-[3-CYCLOPROPYL-5-(2-FLUORO-4-IODOPHENYLAMINO)-6,8-DIMETHYL-2,4,7-TRIOXO-3,4,6,7-TETRAHYDRO-2H-PYRIDO[4,3-D]PYRIMIDINE-1-IL]-PHENYL}-CYCLOPROPANECARBOXAMIDE DIMETHYLSULFOXIDE SOLVATE AS MEK1/2 INHIBITOR 2016
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2627692C1
DICHLOROACETATES OF SUBSTITUTED N4-[2-(DIMETHYLPHOSPHORYL)PHENYL]-N2-(2-METHOXY-4-PIPERIDIN-1-YLPHENYL)-5-CHLOROPYRIMIDINE-2,4-DIAMINES AS MODULATORS OF ALK AND EGFR, INTENDED FOR TREATING CANCER 2015
  • Ivashchenko Aleksandr Vasilevich
  • Ignatev Vasilij Gennadevich
  • Repik Aleksej Evgenevich
  • Shafeev Mikhail Ajratovich
RU2606951C1
NOVEL EFFICIENT INHIBITOR OF KINASE 4, ASSOCIATED WITH INTERLEUKIN-1 (IRAK4) 2015
  • Kazyulkin Denis Nikolaevich
  • Aksenova Elena Aleksandrovna
  • Skrabelinskaya Ekaterina Igorevna
  • Moskalchuk Tatyana Viktorovna
  • Boev Viktor Ivanovich
RU2613973C1

RU 2 644 155 C1

Authors

Aleksandr Vasilevich Ivashchenko

Ignatev Vasilij Gennadevich

Shafeev Mikhail Ajratovich

Repik Aleksej Evgenevich

Dates

2018-02-08Published

2016-12-12Filed