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ANTI-CANCER BENZOPYRAZINES ACTING THROUGH FGFR-KINASES INHIBITION
专利权人:
ASTEKS TERAPYUTIKS LIMITED
发明人:
VUDKHED Stiven Dzhon (US),ВУДХЭД Стивен Джон (US),MYURREJ Kristofer Uillyam (GB),МЮРРЕЙ Кристофер Уилльям (GB),BERDINI Valerio (GB),БЕРДИНИ Валерио (GB),SAKSTI Gordon (HR),САКСТИ Гордон (HR),BEZONG Gi,БЕЗОНГ Гилберт Эбай (DE),МЕРПУЛ Ливен (BE),КЕРОЛЛЬ Оливье Алексис Жорж (FR),ПОНСЕЛЕ Виржини Софи (FR)
申请号:
RU2014121389
公开号:
RU0002639863C2
申请日:
2012.10.26
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: invention relates to benzopyrazine derivatives of the general formula (I),including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof, wherein W is -N(R3)-; R2 is C1-4alkoxy; Y is -CR18=N-OR19 or -E-D; E is bond, C2-4alkynediyl, -CO-(CR22R23)s-, -NR22-(CR22R23)s-, -(CR22R23)s-CO-NR22-(CR22R23)s- or -(CR22R23)s-NR22-CO-(CR22R23)s-; D is phenyl, 3-6 membered cycloalkyl or 5-9 membered mono- or bicyclic saturated, partially saturated or aromatic heterocyclyl containing 1-4 heteroatoms selected from N, O or S, wherein the said phenyl, cycloalkyl and heterocyclyl can each optionally being substituted with 1-2 R1-groups; with the exception of the compounds indicated in the formula; R1 is halogen, cyano, C1-6alkyl, C1-6alkoxy, -C(=O)-O-C1-6alkyl, hydroxyC1-6alkyl, -NR4R5 , C1-6alkyl substituted by -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by -NR4R5, -C(=O)-NR4R5, R6, C1-6alkyl substituted by R6, -C(=O)-R6; R3 is halogenC1-6alkyl, optionally substituted by -O-C(=O)-C1-6alkyl, hydroxyC1-6alkyl, hydroxyhalogenC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group or -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by R9, C2-6alkynyl substituted with R9, C1-6alkyl substituted by -NR10R11, C1-6alkyl substituted by -O-C(=O)-NR10R11; R4 and R5 are hydrogen, C1-6alkyl, C1-6alkyl substituted by -NR14R15, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group, -C(=O)-NR14R15, -C(=O)-O-C1-6alkyl, -C(=O)-R13; R6 is a 6-membered saturated or aromatic monocyclic heterocyclyl having 1 to 2 heteroatoms selected from N or O; the said heterocyclyl is optionally substituted by 1 substituent selected from C1-6alkyl, halogen, C1-6alkyl-O-C(=O)-; R9 is C3cycloalkyl or 3-6 membered monocyclic saturated, partially saturated or aromatic heterocyclyl containing 1-2 heteroatoms selected from N or O, the said heterocyclyl is optio
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