发明名称 Alpha-carbolines for the treatment of cancer
摘要 The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.
申请公布号 US9428500(B2) 申请公布日期 2016.08.30
申请号 US201314399925 申请日期 2013.05.10
申请人 UNIVERSITA DEGLI STUDI DI MILANO—BICOCCA;UNIVERSITE DE GENEVE;UNIVERSITE CLAUDE BERNARD—LYON 发明人 Gambacorti-Passerini Carlo;Mologni Luca;Scapozza Leonardo;Bisson William;Ahmed Shaheen;Goekjian Peter;Tardy Sébastien;Orsato Alexandre;Gueyrard David;Benoit Joseph
分类号 C07D471/04;A61K31/44;C07F7/08 主分类号 C07D471/04
代理机构 Arent Fox LLP 代理人 Arent Fox LLP
主权项 1. Compounds of formula (I) wherein: R1 is H or C1-C3 alkyl R2 is either halogen or X is either CH or N R3 is either C1-C3 alkyl or (1-methylpiperidin-4-yl) Rx and Ry are either H or nitro Rz and Rz′ are H, OH, or oxo Rt and R′t can be the same or different and are H or C1-C3 alkoxy Ra is H or F Rb is H, C1-C3 alkoxy, trifluoromethyl, or halogen Re is H or halogen Rf is H, C1-C3 alkyl or trifluoromethyl Rg is H or F Rk is H, halogen, trifluoromethyl, C1-C3 alkoxy, C1-C3 alkylsulfonamino Rl is H or F Rm is H, C1-C3 alkoxy, F or trifluoromethyl Rn is H, C1-C3 alkyl or a 5- to 6 -membered aromatic or heteroaromatic ring Rp is either C1-C3 alkyl or 5- to 6 -membered aromatic or heteroaromatic ring Rq is either H or tri(C1-C4)alkylsilyl Rs is tri(C1-C4)alkylsilyl Rh is either H , C1-C3 alkoxy or C1-C3 alkylcarbonylamino Ru is either H or F Rv is a C1-C3 alkyl Rw and Rw′ can be the same or different and are hydroxyl or C1-C3 alkoxy L and L′ are O, S, SO or SO2; Z is either C or N and pharmaceutically acceptable salts thereof.
地址 Milan IT