NOVEL PHENYLPYRAZINONES AS KINASE INHIBITORS

FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry and specifically to 5-phenyl-1H-pyrazin-2-one derivatives of general formula IIor pharmaceutically acceptable salts thereof, where R denotes -Ror - R-R-R; Rdenotes aryl or heteroaryl, and is optionally substituted with one or...

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Hauptverfasser: SUINI ZAKHARI KEVIN, D'JUDNI NOLAN DZHEJMS, SHOGREN EHRIK BRAJAN, LOU JAN, SOT MAJKL
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry and specifically to 5-phenyl-1H-pyrazin-2-one derivatives of general formula IIor pharmaceutically acceptable salts thereof, where R denotes -Ror - R-R-R; Rdenotes aryl or heteroaryl, and is optionally substituted with one or two R; where each Rindependently denotes Calkyl, halogen or Chalogenalkyl; Rdenotes -C(=O), -CH-; Rdenotes R; where Rdenotes an amino group or heterocycloalkyl, and is optionally substituted with one or two substitutes selected from Calkyl, hydroxy group, oxo group, Chydroxyalkyl, Calkoxy group; Q denotes CH; Ydenotes Calkyl; Ydenotes Y; where Ydenotes Calkyl, optionally substituted with one Y; where Ydenotes a hydroxy group, n and m are equal to 0; Ydenotes Yor Y; where Ydenotes lower cycloalkyl, optionally substituted with halogen; and Ydenotes an amino group, optionally substituted with one or more Calkyl; 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 SO. 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 ex Настоящее изобретение относится к области органической химии, а именно к производным 5-фенил-1Н-пиразин-2-она общей формулы II или к их фармацевтически приемлемым солям, где R представляет собой -Rили -R-R-R; Rпредставляет собой арил или гетероарил, и необязательно замещен одним или двумя R; где каждый Rнезависимо представляет собой Cалкил, галоген или Cгалогеналкил; Rпредставляет собой -C(=O), -СН-; Rпредставляет собой R; где Rпредставляет собой аминогруппу или гетероциклоалкил, и необязательно замещен одним или двумя заместителями, выбранными из Cалкила, гидроксигруппы, оксогруппы, Cгидроксиалкила, Салкоксигруппы; Q представляет собой СН; Yпредставляет собой Cалкил; Yпредставляет собой Y; где Yп