ПРОИЗВОДНЫЕ 1-(3-АМИНОФЕНИЛ)-6,8-ДИМЕТИЛ-5-(4-ИОД-2-ФТОР-ФЕНИЛАМИНО)-3-ЦИКЛОПРОПИЛ-1H,6H-ПИРИДО[4,3-d]ПИРИМИДИН-2,4,7-ТРИОНА В КАЧЕСТВЕ ИНГИБИТОРОВ МЕК1/2
Ivashchenko Aleksandr Vasilevich,Иващенко Александр Васильевич,Ignatev Vasilij Gennadevich,Игнатьев Василий Геннадьевич,Repik Aleksej Evgenevich,Репик Алексей Евгеньевич,SHafeev Mikhail Ajratovich,Шаф
申请号：
RU2015148807/04
公开号：
RU0002605400C1
申请日:
2015.11.13
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: present invention relates to novel 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, having effect on kinase MEK1 and can be used for treating and preventing cancer, in particular malignant melanoma. Said derivatives are selected from following group of compounds: N-{3-[6,8-dimethyl-5-(4-iodo-2-fluoro-phenylamino)-3-cyclopropyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-2-dimethylaminoacetamide hydrochloride (1.1), N-{3-[6,8-dimethyl-5-(4-iodo-2-fluoro-phenylamino)-3-cyclopropyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-2-dimethylaminopropionamide hydrochloride (1.4), N-{3-[6,8-dimethyl-5-(4-iodo-2-fluoro-phenylamino)-3-cyclopropyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-2-dimethylaminobutyramide hydrochloride (1.7), (R)-{3-[6,8-dimethyl-5-(4-iodo-2-fluoro-phenylamino)-3-cyclopropyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-2-dimethylaminopropionamide hydrochloride (1.10), {3-[6,8-dimethyl-5-(4-iodo-2-fluoro-phenylamino)-3-cyclopropyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-amide(R)-1-methylpyrrolidine-2-carboxylic acid hydrochloride (1.14). Invention also relates to a method of producing said compounds.EFFECT: method consists in that compound of formula 2 or salt thereof: , where R2 is a hydrogen atom, reacts with corresponding organic acid or an activated derivative thereof, with subsequent treatment of obtained product with hydrogen chloride solution.11 cl, 1 tbl, 7 exНастоящее изобретение относится к новым производным 1-(3-аминофенил)-6,8-диметил-5-(4-иод-2-фтор-фениламино)-3-циклопропил-1H,6H-пиридо[4,3-d]пиримидин-2,4,7-триона, которые обладают активностью в отношении киназы МЕК1 и могут быть использованы для лечения и профилактики рака, в частности злокачественной меланомы. Указанные производные
