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Axl inhibitors for use in combination therapy to prevent, treat or manage metastatic cancer
专利权人:
RIGEL PHARMACEUTICALS; INC.
发明人:
HITOSHI, YASUMICHI,HOLLAND, SACHA,PAYAN, DONALD
申请号:
ES10700686
公开号:
ES2528032T3
申请日:
2010.01.15
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Axl inhibitor and one or more chemotherapeutic agents, for use to prevent, treat or manage cancer, in which the Axl inhibitor is a compound of formula (I): ** Formula ** in which: R1, R4 and R5 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl, aralkyl, -C (O) R8, -C (O) N (R6) R7 and -C (>; = NR6) N (R6) R7; R2 and R3 are each independently a polycyclic heteroaryl containing more than 14 ring atoms optionally substituted with one or more substituents selected from the group consisting of oxo, thioxo, cyano, nitro, halogen, haloalkyl, alkyl, optionally substituted cycloalkyl, cycloalkylalkyl optionally substituted, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, -R9-OR8, -R9-O-R10-OR8, -R9-O-R10-O-R10-OR8, -R9-O -R10-CN, -R9-O-R10-C (O) OR8, -R9-O-R10-C (O) N (R6) R7, -R9-O-R10-S (O) pR8 (in the that p is 0, 1 or 2), -R9-O-R10-N (R6) R7, -R9-O-R10-C (NR11) N (R11) H, -R9-OC (O) -R8, -R9-N (R6) R7, -R9-C (O) R8, -R9-C (O) OR8, -R9-C (O) N (R6) R7, -R9-N (R6) C (O ) OR8, -R9-N (R6) C (O) R8, -R9-N (R6) S (O) tR8 (where t is 1 or 2), -R9-S (O) tOR8 (in the that t is 1 or 2), -R9-S (O) pR8 (where p is 0, 1 or 2) and -R9-S (O) tN (R6) R7 (where t is 1 or 2 ); or R2 is a polycyclic heteroaryl containing more than 14 ring atoms as described above and R3 is selected from the group consisting of aryl and heteroaryl, in which aryl and heteroaryl are each optionally substituted independently with one or more substituents selected from the group consisting of alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo, thioxo, cyano, nitro, optionally substituted aryl, optionally substituted aralkyl, optionally substituted aralkenyl, optionally substituted aralkynyl, optionally substituted cycloalkyl, optionally substituted, optionally substituted cycloalkylalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycl
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