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US 9,428,500 B2Granted
Alpha-carbolines for the treatment of cancer
AssigneesUniversita Degli Studi Di Milano-Bicocca, Universite De Geneve, Universite Claude Bernard Lyon
InventorsCarlo Gambacorti-Passerini, Luca Mologni, Leonardo Scapozza, William Bisson, Shaheen Ahmed, Peter Goekjian, Sébastien Tardy, Alexandre Orsato, David Gueyrard, Joseph Benoit
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Abstract
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.
Claims13
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.
24 more elements
Dependencies are inferred from the claim text.