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NOVEL PHENYLPYRAZINONES AS KINASE INHIBITORS
专利权人:
F.KHOFFMANN-LJA ROSH AG
发明人:
D'JuDNI Nolan Dzhejms (US),ДЬЮДНИ Нолан Джеймс (US),LOU Jan' (US),ЛОУ Янь (US),ShOGREN Ehrik Brajan (US),ШОГРЕН Эрик Брайан (US),SOT Majkl (US),СОТ Майкл (US),SUINI Zakhari Kevin (US),СУИНИ Захари Кев,DJUDNI NOLAN DZHEJMS,ДЬЮДНИ Нолан Джеймс,LOU JAN,ЛОУ Янь,SHOGREN EHRIK BRAJAN,ШОГРЕН Эрик Брайан,SOT MAJKL,СОТ Майкл,SUINI ZAKHARI KEVIN,СУИНИ Захари Кевин
申请号:
RU2011103234/04
公开号:
RU0002507202C2
申请日:
2009.06.22
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry and specifically to 5-phenyl-1H-pyrazin-2-one derivatives of general formula II or pharmaceutically acceptable salts thereof, where R denotes -R1 or - R1-R2-R3; R1 denotes aryl or heteroaryl, and is optionally substituted with one or two R1'; where each R1' independently denotes C1-6alkyl, halogen or C1-6halogenalkyl; R2 denotes -C(=O), -CH2-; R3 denotes R4; where R4 denotes an amino group or heterocycloalkyl, and is optionally substituted with one or two substitutes selected from C1-6alkyl, hydroxy group, oxo group, C1-6hydroxyalkyl, C1-6alkoxy group; Q denotes CH2; Y1 denotes C1-6alkyl; Y2 denotes Y2b; where Y2b denotes C1-6alkyl, optionally substituted with one Y2b'; where Y2b' denotes a hydroxy group, n and m are equal to 0; Y4 denotes Y4c or Y4d; where Y4c denotes lower cycloalkyl, optionally substituted with halogen; and Y4d denotes an amino group, optionally substituted with one or more C1-6alkyl; where "aryl" denotes phenyl or naphthyl, "heteroaryl" denotes a monocyclic or bicyclic radical containing 5 to 9 atoms in the ring, which contains at least one aromatic ring containing 5 to 6 atoms in the ring, with one or two N or O heteroatoms, wherein the remaining atoms in the ring are carbon atoms, under the condition that the binding point of the heteroaryl radical is in the aromatic ring, "heterocycloalkyl" denotes a monovalent saturated cyclic radical consisting of one ring containing 5 to 6 atoms in the ring, with one or two ring heteroatoms selected from N, O or SO2. The invention also relates to use of the compound of formula II or a pharmaceutical composition based on the compound of formula II.EFFECT: obtaining novel compounds that are useful for modulating Btk activity and treating diseases associated with excessive activity of Btk.7 cl, 2 tbl, 53 exНастоящее изобретение относится к области органической химии, а именно к производным 5-фенил-1Н-пиразин-2-она общей формулы II и
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