New pyridopyrazine derivatives are modulators of kinase activity, useful for the treatment of diseases associated with abnormal cellular signaling, e.g. tumors

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专利权人:

ZENTARIS GMBH

发明人:

GUENTHER ECKHARD,RAPP ULF R,CLAUS ECKHARD,SEIPELT IRENE,WIXLER LUDMILLA

申请号：

NO20056032

公开号：

NO332005B1

申请日:

2005.12.19

申请国别(地区):

NO

年份:

2012

代理人:

摘要：

Pyrido[2,3-b]pyrazine derivatives (I) their salts, derivatives, analogs, solvates, hydrates and polymorphs, as racemates and as pure or mixed enantiomers and/or diastereomers or tautomers are new. Pyrido[2,3-b]pyrazine derivatives of formula (I) their salts, derivatives, analogs, solvates, hydrates and polymorphs, as racemates and as pure or mixed enantiomers and/or diastereomers or tautomers are new. R1 and R2 : hydrogen, hydroxy, halo, 1-8C alkyl, aryl (optionally substituted by one or more Q1), heteroaryl (optionally substituted by one or more Q2), OR5, SR6, or NR7R8； one of R3 and R4 : hydrogen and the other is NR9R10； R9 : hydrogen, alkyl (A), cycloalkyl (Cy), heterocyclyl (Hc), aryl (Ar), heteroaryl (Ha) (the last 4 optionally substituted by alkyl), and all these groups may themselves be substituted； R10 : -CYNR11R12, -CY1NR13R14 or -C(NH)R16； Y : oxygen or sulfur； R11 and R12 : hydrogen, A (optionally substituted by Q4), Cy (optionally substituted by Q5), Hc (optionally substituted by hydroxy, alkoxy, aryloxy, amino(itself optionally substituted by A, Ar), A, alkyl-Ar or Ar), Ar (optionally substituted by Q6), Ha (optionally substituted by Q7), COR17, or R11 and R12 together form Cy or Hc； Y1 : NH； R13 and R14 : hydrogen, A (optionally substituted by Q8), Cy (optionally substituted by Q9), Hc (optionally substituted by hydroxy, alkoxy, aryloxy, amino (itself optionally substituted by A or Ar), A or Ar), Ar (optionally substituted by Q10), Ha (optionally substituted by Q11), or R13 and R14 together form Cy or Hc； R16 : A (optionally substituted by Q12), Cy (optionally substituted by Q13), Hc (optionally substituted by hydroxy, alkoxy, aryloxy, amino (itself optionally substituted by A or Ar), A or Ar), Ar (optionally substituted by Q14) or Ha (optionally substituted by Q15). The full definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] ACTIVITY : Cytostatic； Vasotropic； Antipsoriatic； Antiarteriosclerosis； Hepatotropic. MECHANISM OF ACTIO

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