Compounds for inhibiting mitotic progression
AssigneeMillennium Pharmaceuticals, Inc.
InventorsChristopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
Claims15
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- Ra is selected from the group consisting of C1-3 aliphatic, C1-3 fluoroaliphatic, —R1, -T-R1—R2, and -T-R2;
- T is a C1-3 alkylene chain optionally substituted with fluoro;
- R1 is an optionally substituted aryl, heteroaryl, or heterocyclyl group;
- R2 is selected from the group consisting of halo, —C≡C—R3, —CH═CH—R3, —N(R4)2, and —OR;
- R3 is hydrogen or an optionally substituted aliphatic, aryl, heteroaryl, or heterocyclyl group;
- each R4 independently is hydrogen or an optionally substituted aliphatic, aryl, heteroaryl, or heterocyclyl group;
- or two R4 on the same nitrogen atom, taken together with the nitrogen atom form an optionally substituted 5- to 6-membered heteroaryl or 4- to 8-membered heterocyclyl ring having, in addition to the nitrogen atom, 0-2 ring heteroatoms selected from N, O, and S;
- R5 is hydrogen or an optionally substituted aliphatic, aryl, heteroaryl, or heterocyclyl group;
- and
- Rb is selected from the group consisting of fluoro, chloro, —CH3, —CF3, —OH, —OCH3, —OCF3, —OCH2CH3, and —OCH2CF3.
The compound 4-([9-ethynyl-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino)-2-methoxybenzoic acid or a pharmaceutically acceptable salt thereof.
The compound 4-([7-(2-fluoro-6-methoxyphenyl)-9-(1-methyl-1H-pyrrol-2-yl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino)-2-methoxybenzoic acid or a pharmaceutically acceptable salt thereof.
The compound 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoic acid or a pharmaceutically acceptable salt thereof.
The compound sodium 4-{[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino}-2-methoxybenzoate.
Dependencies are inferred from the claim text.