Aminopyridine derivatives having Aurora A selective inhibitory action
The present invention relates to a compound of Formula (I): wherein R 1 is H or C 1-2 alkyl; R 2 is H or C 1-3 alkyl; R 3 and R 4 are each independently H or C 1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R 10 ; R 5 is H, hydroxy, C 1-2 alkyl, or OCH 3 ; and R 10 is F or Cl, or a pharmaceutically acceptable salt or ester thereof.
1. A compound of Formula (I):
wherein:
R 1 is H or C 1-2 alkyl;
R 2 is H or C 1-3 alkyl;
R 3 and R 4 are each independently H or C 1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R 10 ;
R 5 is H, hydroxy, C 1-2 alkyl, or OCH 3 ; and
R 10 is F or Cl,
or a pharmaceutically acceptable salt thereof.
2. The compound according to claim 1 or a pharmaceutically acceptable salt thereof; wherein R 1 is H or methyl.
3. The compound according to claim 2 or a pharmaceutically acceptable salt thereof, wherein R 2 is H or methyl.
4. The compound according to claim 3 or a pharmaceutically acceptable salt thereof, wherein R 3 and R 4 are each independently H or methyl which may be substituted with one to three of the same or different substituents selected from R 10 ; and R 10 is F.
5. The compound according to claim 4 or a pharmaceutically acceptable salt thereof, wherein R 5 is H, hydroxy, methyl, or OCH 3 .
6. A compound which is:
(a) (2S)-1,1,1-trifluoropropan-2-yl{(3S)-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(b) (2S)-1,1,1-trifluoropropan-2-yl{(3R,4R)-4-hydroxy-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(c) (2S)-1,1,1-trifluoropropan-2-yl{(3S)-1-[4-methyl-6-(5-methyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(d) 1,1,1-trifluoro-2-methylpropan-2-yl{(3S)-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(e) tert-butyl {(3S)-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(f) tert-butyl {(3S)-1-[4-methyl-6-(5-methyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(g) (2S)-1,1,1-trifluoropropan-2-yl{(3R,4R)-4-methyl-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
(h) (2S)-1,1,1-trifluoropropan-2-yl{(3R,4R)-4-methoxyl-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate, or
(l) tert-butyl {(3R,4R)-4-methyl-1-[4-methyl-6-(1H-pyrazol-3-ylamino)pyrimidin-2-yl]pyrrolidin-3-yl}carbamate,
or a pharmaceutically acceptable salt thereof.
7. A pharmaceutical composition comprising, together with pharmaceutically acceptable carrier or diluent, at least one compound according to claim 1 as active ingredient.