abstract |
REFERS TO COMPOUNDS DERIVED FROM ISOQUINOLINE OF FORMULA (I), WHERE n, r ARE FROM 0 TO 2; m IS 0 TO 4; J IS OPTIONALLY REPLACED ONE OR TWO TIMES BY Q, J IS ARYL (C6-C14) AS PHENYL, NAPHTHYL, FLUORENYL AND PHENANTHRENYL, HETEROARYL (C4-C14) AS FURYL, PYRANIL, PYRIDYL, BETWEEN CY3-OTHERS AS CYCLOPROPYL, CYCLOPENTILO, AND CYCLOHEXYL, HETEROCICLOALKYL (C3-C8) AS PIPERIDYL, PIPERAZINYL, IMIDAZOLINYL, AMONG OTHERS; Q IS HALOGEN, LOWER ALKYL, -OR2, -SR2, AMONG OTHERS; X IS Y, -N (R), OXA, THIO, SULFONE, AMONG OTHERS; AND IS H, LOWER ALKYL, ARYL AS OPTIONALLY SUBSTITUTED PHENYL, AMONG OTHERS; Z IS AMINO, HALOGEN, RENT AMONG OTHERS. PREFERRED COMPOUNDS ARE: (4-TER-BUTYL-PHENYL) - [6-FLUORO-4- (2-MORPHOLIN-4-IL-PYRIMIDIN-4-IL) -ISOQUINOLIN-1-IL) -AMINE, [4- ( 2-MORFOLIN-4-IL-PYRIMIDIN-4-IL) -ISOQUINOLIN-1-IL] - (3-TRIFLUOROMETILOXY-PHENYL) -AMINE, (4-TER-BUTYL-PHENYL) - {4- [2- (4 -TRIFLUOROMETHYL-PIPERIDIN-4-IL) -PYRIMIDIN-4-IL] -ISOQUINOLIN-1-IL} -AMINE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS INHIBIT KINASE B-RAF (A SERINE / THREONINE KINASE) AND ARE USEFUL IN THE TREATMENT OF PROLIFERATIVE DISEASES SUCH AS CANCER |