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INHIBITOR OF EGFR AND PRODUCTION AND USE THEREOF
专利权人:
LTD.;SHANKHAJ KHENSOKH BIOMEDIKAL KO.
发明人:
VEJ Minsun (CN),ВЭЙ Минсун (CN),SUN Guantszyun (CN),СУНЬ Гуанцзюнь (CN),TAN Sunlyan (CN),ТАНЬ Сунлян (CN),GAO Pen (CN),ГАО Пэн (CN),VAN Shaobao (CN),ВАН Шаобао (CN),SYU Venkhua (CN),СЮ Вэньхуа (CN),CH
申请号:
RU2017114687
公开号:
RU0002702631C2
申请日:
2015.09.30
申请国别(地区):
RU
年份:
2019
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to a novel derivative of 4-substituted-2- (N- (5-substituted-allylamide) phenyl) -amino) pyrimidine represented by formula (I). In formula (I)ring A is selected from a group consisting ofwhere Q is a bond; R is selected from a group consisting of hydrogen; X1, X2 and X3 each is independently selected from a group consisting of NR7 and CR8, where one or two of X1, X2 and X3 are NR7, wherein, when X2 is NR7, other groups are CR8, and a ring with said group X2 is joined by a carbon atom to a pyrimidine ring, or when two of X1, X2 and X3 are NR7, ring is joined by nitrogen atom of said group to pyrimidine ring; R1 is selected from the group consisting of:wherein three R6 in are optionally identical or different substitutes; R2 is selected from a group consisting of C1-8 alkyl, where C1-8 alkyl is optionally substituted with one or more groups selected from a group consisting of halogen; R3 is selected from a group consisting of hydrogen, halogen, trifluoromethyl, trifluoromethoxy and P(O)R11R12, where R11R12 are C1-6 alkyl; R4 are independently selected from a group consisting of hydrogen, halogen, cyano, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 4-membered saturated heterocyclyl containing an oxygen atom in the cycle, -P(O)R11R12, where R11R12 are represented by C1-6 alkyl, -S(O)rR9, -OR10, -C(O)R10, where C1-8 alkyl is optionally substituted with one or more groups selected from a group consisting of halogen, hydroxy and -OR10; R6 is selected from a group consisting of hydrogen and C1-8 alkyl; R7 is selected from a group consisting of C1-8 alkyl, C2-8 alkenyl, C3-6 cycloalkyl, -S(O)rR9, -OR10, -C(O)R10 and 4-member saturated heterocyclyl containing an oxygen atom in a cycle; where C1-8 alkyl is substituted with one or more groups selected from a group consisting of hydroxy, C2-8 alkenyl and C2-8 alkynyl; R8 is selected from a group consisting of hydrogen, C1-8 alkyl, C3-8 cycloalkyl and -OR10; R9 is selecte
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