FIELD: pharmacology.
SUBSTANCE: invention relates to a new compound, 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]pyrimidin-1-yl]-phenyl}-cyclopropanecarboxamide dimethylsulfoxide solvate of formula 1
,
which is a MEK, in particular MEK1, MEK2 and MEK1/2, inhibitor. The compound can be used to prevent and/or treat malignant melanomas. The invention also relates to a process for preparation of a compound of formula 1. The method consists in reaction of a compound of formula 2
or a salt thereof with a cyclopropanecarboxylic acid or an activated derivative thereof, followed by obtaining a crystalline solvate of the desired product while cooling the hot saturated solution in dimethylsulfoxide.
EFFECT: compound has lower toxicity with prolonged dosing.
10 cl, 7 ex, 3 tbl, 2 dwg
| Title |
Year |
Author |
Number |
| 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
|
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2016 |
- Ivashchenko Aleksandr Vasilevich
- Ignatev Vasilij Gennadevich
- Repik Aleksej Evgenevich
- Shafeev Mikhail Ajratovich
|
RU2615986C1 |
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2015 |
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|
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2015 |
- Ivashchenko Aleksandr Vasilevich
- Ignatev Vasilij Gennadevich
- Repik Aleksej Evgenevich
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|
RU2606949C9 |
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2017 |
- Ivashchenko Aleksandr Vasilevich
- Ignatev Vasilij Gennadevich
- Repik Aleksej Evgenevich
- Shafeev Mikhail Ajratovich
|
RU2654695C1 |
| METHOD FOR ADJUVANT THERAPY OF CANCER |
2013 |
- Laquerre Sylvie
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|
RU2640180C2 |
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2015 |
- Ivashchenko Aleksandr Vasilevich
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- Repik Aleksej Evgenevich
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|
RU2606951C1 |
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2015 |
- Ivashchenko Aleksandr Vasilevich
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|
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- Ivashchenko Aleksandr Vasilevich
- Ignatev Vasilij Gennadevich
- Repik Aleksej Evgenevich
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|
RU2603959C1 |
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2016 |
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|
RU2644155C1 |
