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CHECKPOINT KINASE 1 INHIBITORS FOR POTENTIATING DNA DAMAGING AGENTS
专利权人:
ARRAY BIOPHARMA INC.
发明人:
HUMPHRIES, MICHAEL J,WINSKI, SHANNON L
申请号:
NZ59612510
公开号:
NZ596125A
申请日:
2010.04.09
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed is a Chk1 (Checkpoint kinase-1) inhibitor selected from the group consisting of (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)nicotinamide (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)isobutyramide (R)-N-(5-bromo-4-(3-(methylamino)piperidin-1-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl)nicotinamide (R)-N-(4-(3-aminopiperidin-1-yl)-5- bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-methylnicotinamide (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1Hpyrrolo[ 2,3-b]pyridin-3-yl)-3-methyl-butanamide and (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)-2- cyclopropylacetamide, for administration to a patient with cancer for potentiating a DNA damaging agent, wherein the administration of the CHK1 inhibitor follows the administration of the DNA damaging agent, wherein the CHK1 inhibitor is administered in two doses, the first dose of the CHK1 inhibitor is administered one day after the DNA damaging agent, and the second dose of the CHK1 inhibitor is administered two days after the DNA damaging agent.
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