YAN XUELEI,FU JIASHENG,HUANG XIN,OLSON STEVEN HOWARD,LI ZHIHONG,GRIBBLE JR. MICHAEL WILLIAM,MIHALIC JEFFREY THOMAS,FOX BRIAN MATTHEW,GONZALEZ LOPEZ DE TURISO FELIX,GONZALEZ BUENROSTRO ANA,YU MING,ROVE
申请号:
NZ62738511
公开号:
NZ627385A
申请日:
2011.06.03
申请国别(地区):
NZ
年份:
2016
代理人:
摘要:
Disclosed is the compound AMG-232 (2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid) and compositions comprising it for the treatment of cancer (particularly for hematopoietic tumors of lymphoid lineage, soft tissue sarcoma, breast cancer, glioblastoma, acute myeleogenous leukemia and melanoma). Also disclosed are synthetic intermediates useful for the preparation of AMG-232 and which include (3S,5S,6R,8S)-8-allyl-6-(3-chlorophenyl)-5-(4-chlorophenyl)-3-isopropyl-8-methyl-2,3,5,6,7,8-hexahydrooxazolo[3,2-a]pyridin-4-ium trifluoromethanesulfonate, (3S,5R,6R)-3-allyl-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyltetrahydro-2H-pyran-2-one, (5R,6R)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyltetrahydro-2H-pyran-2-one, (4R,5R)-4-(3-chlorophenyl)-5-(4-chlorophenyl)-5-hydroxy-2-methylpentanoic acid and isopropyl 4-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-5-oxopentanoate.