5-(4-(haloalkoxy)phenyl) pyrimidine-2-amine compounds and compositions as kinase inhibitors
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Abstract
The invention provides compounds of formula (1) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, AbI, BCR-AbI, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3. Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, Fms, KDR, c-rapor b-raf kinases.
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Citations
7 Claims
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1. A compound of Formula (1):
- View Dependent Claims (2, 3, 4, 5)
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2. The compound of claim 1, wherein R1 is —
- CHF2, —
CF3, —
CH2CF3, —
CF2CH3, or —
CH2CF3.
- CHF2, —
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3. The compound of claim 2, wherein R1 is —
- CHF2.
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4. The compound of claim 1, wherein R2 if present, is halo, C1-6 alkyl, C1-6 alkoxy, hydroxy or CO2R7 and R7 is H or C1-6 alkyl.
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5. The compound of claim 1, wherein said compound is selected from the group consisting of:
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N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1-methylpiperidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-azabicyclo[3.1.0]hexane-2-carboxamide; (1S,2R,5R)-N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-azabicyclo[3.1.0]hexane-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)piperidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-5-oxopyrrolidine-2-carboxamide; (R)-N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-5-oxopyrrolidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-6-oxopiperidine-3-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-6-fluoropyridine-3-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1H-imidazole-5-carboxamide; N-(2-methyl-5-(5-(4-(trifluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-5-oxopyrrolidine-2-carboxamide; (S)-N-(2-methyl-5-(5-(4-(trifluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-5-oxopyrrolidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1-cyclopropyl-5-oxopyrrolidine-3-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1-ethyl-6-oxopiperidine-3-carboxamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-N-(2-fluoroethyl)-3-hydroxypropanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-hydroxypiperidin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-hydroxypiperidin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-(2-hydroxypropyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((R)-2-hydroxypropyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((R)-2-hydroxypropyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((S)-2-hydroxypropyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((S)-2-hydroxypropyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((S)-2-hydroxypropyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-(4-hydroxycyclohexyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1r,4r)-4-hydroxycyclohexyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1r,4R)-4-hydroxycyclohexyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1r,4R)-4-hydroxycyclohexyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1s,4S)-4-hydroxycyclohexyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1s,4S)-4-hydroxycyclohexyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1s,4s)-4-hydroxycyclohexyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(3-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((S)-3-hydroxypiperidin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((S)-3-hydroxypiperidin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((S)-3-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((R)-3-hydroxypiperidin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((R)-3-hydroxypiperidin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((R)-3-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-(2-hydroxycyclopentyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1R,2R)-2-hydroxycyclopentyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2R)-2-hydroxycyclopentyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2S)-2-hydroxycyclopentyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1R,2R)-2-hydroxycyclopentyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2S)-2-hydroxycyclopentyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2R)-2-hydroxycyclopentyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2S)-2-hydroxycyclopentyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2R)-2-hydroxycyclopentyl)propanamide; 2-(4-(5-(4-(Difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-1-(4-hydroxypiperidin-1-yl)prop-2-en-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-1-(4-hydroxypiperidin-1-yl)ethanone; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-methylpiperazin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-methylpiperazin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-methylpiperazin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(3-(trifluoromethyl)piperazin-1-yl)propan-1-one; 2-(4-(5-(4-(Difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-1-(3-(trifluoromethyl)-4-methylpiperazin-1-yl)-3-hydroxypropan-1-one; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methanesulfonyl -piperazine-1-carboxamide; 1-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-(1,3-dimethyl-1H-pyrazol-5-yl)urea; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-(2-hydroxyethyl)piperazine-1-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4,7-diazaspiro[2.5]octane-7-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methyl-4,7-diazaspiro[2.59]octane-7-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-(2-hydroxyethy)-4,7-diazaspiro[2.5]octane-7-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-(trifluoromethyl)piperazine-1-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methyl-3-(trifluoromethyl)piperazine-1-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methyl-3-oxopiperazine-1-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-(2-hydroxyethyl)-3-oxopiperazine-1-carboxamide; 4-(4-(5-(4-(Difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)-1-methylpiperazin-2-one; 4-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)-1-(2-hydroxyethyl)piperazin-2-one; 4-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)piperazin-2-one; and (4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)(3-(trifluoromethyl)piperazin-1-yl)methanone.
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2. The compound of claim 1, wherein R1 is —
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6. A pharmaceutical composition comprising a therapeutically effective amount of a compound having the structure of Formula (1), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier:
- View Dependent Claims (7)
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7. The pharmaceutical composition of claim 6, wherein the compound is selected from the group consisting of:
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N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1-methylpiperidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-azabicyclol[3.1.0]hexane-2-carboxamide; (1S,2R,5R)-N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-azabicyclol[3.1.0]hexane-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)piperidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-5-oxopyrrolidine-2-carboxamide; (R)-N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-5-oxopyrrolidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-6-oxopiperidine-3-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-6-fluoropyridine-3-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1H-imidazole-5-carboxamide; N-(2-methyl-5-(5-(4-(trifluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-5-oxopyrrolidine-2-carboxamide; (S)-N-(2-methyl-5-(5-(4-(trifluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-5-oxopyrrolidine-2-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1-cyclopropyl-5-oxopyrrolidine-3-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-1-ethyl-6-oxopiperidine-3-carboxamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-N-(2-fluoroethyl)-3-hydroxypropanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-hydroxypiperidin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-hydroxypiperidin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-(2-hydroxypropyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((R)-2-hydroxypropyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((R)-2-hydroxypropyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((S)-2-hydroxypropyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((S)-2-hydroxypropyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((S)-2-hydroxypropyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-(4-hydroxycyclohexyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((lr,4r)-4-hydroxycyclohexyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1r,4R)-4-hydroxycyclohexyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1r,4R)-4-hydroxycyclohexyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1s,4S)-4-hydroxycyclohexyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1s,4S)-4-hydroxycyclohexyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1s,4s)-4-hydroxycyclohexyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(3-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((S)-3-hydroxypiperidin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((S)-3-hydroxypiperidin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((S)-3-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((R)-3-hydroxypiperidin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((R)-3-hydroxypiperidin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-((R)-3-hydroxypiperidin-1-yl)propan-1-one; 2-(4-(5 -(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-(2-hydroxycyclopentyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1R,2R)-2-hydroxycyclopentyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2R)-2-hydroxycyclopentyl)propanamide; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2S)-2-hydroxycyclopentyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1R,2R)-2-hydroxycyclopentyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2S)-2-hydroxycyclopentyl)propanamide; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2R)-2-hydroxycyclopentyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2S)-2-hydroxycyclopentyl)propanamide; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-N-((1S,2R)-2-hydroxycyclopentyl)propanamide; 2-(4-(5-(4-(Difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-1-(4-hydroxypiperidin-1-yl)prop-2-en-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-1-(4-hydroxypiperidin-1-yl)ethanone; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-methylpiperazin-1-yl)propan-1-one; (R)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-methylpiperazin-1-yl)propan-1-one; (S)-2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(4-methylpiperazin-1-yl)propan-1-one; 2-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-3-hydroxy-1-(3-(trifluoromethyl)piperazin-1-yl)propan-1-one; 2-(4-(5-(4-(Difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)-1-(3-(trifluoromethyl)-4-methylpiperazin- 1 -yl)-3 -hydroxypropan- 1 -one; N-(5-(5 -(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methanesulfonyl-piperazine-1-carboxamide; 1-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-(1,3-dimethyl-1H-pyrazol-5-yl)urea; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-(2-hydroxethyl)piperazine-1-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4,7-diazaspiro[2.5]octane-7-carboxamide; N-(5-(5-(4(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methyl-4,7-diazaspiro[2.5]octane-7-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-(2-hydroxyethy)-4,7-diazaspiro[2.5]octane-7-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-3-(trifluoromethyl)piperazine-1-carboxamide; N-(5-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methyl-3-(trifluoromethyl)piperazine-1-carboxamide; N-(5-(5 -(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-methyl-3-oxopiperazine-1-carboxamide; N-(5-(5 -(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)-2-methylphenyl)-4-(2-hydroxyethyl)-3-oxopiperazine-1-carboxamide; 4-(4-(5-(4-(Difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)-1-methylpiperazin-2-one; 4-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl)-1-(2-hydroxyethyl)piperazin-2-one; 4-(4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)benzoyl) piperazin-2-one; and (4-(5-(4-(difluoromethoxy)phenyl)pyrimidin-2-ylamino)phenyl)(3-(trifluoromethyl)piperazin-1-yl)methanone.
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7. The pharmaceutical composition of claim 6, wherein the compound is selected from the group consisting of:
Specification
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Current AssigneeNovartis Ag
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Original AssigneeIRM LLC
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InventorsMolteni, Valentina, Li, Xiaolin, Liu, Xiaodong, Chianelli, Donatella, Nabakka, Juliet, Loren, Jon, You, Shuli
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Primary Examiner(s)Shameem, Golam M M
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Assistant Examiner(s)Cheng, Karen
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Application NumberUS12/674,416Publication NumberTime in Patent Office1,526 DaysField of Search514/275, 544/338US Class Current514/275CPC Class CodesA61P 1/00 Drugs for disorders of the ...A61P 1/04 for ulcers, gastritis or re...A61P 1/14 Prodigestives, e.g. acids, ...A61P 1/16 for liver or gallbladder di...A61P 11/00 Drugs for disorders of the ...A61P 11/02 Nasal agents, e.g. deconges...A61P 11/06 AntiasthmaticsA61P 13/10 of the bladderA61P 13/12 of the kidneysA61P 15/00 Drugs for genital or sexual...A61P 15/10 for impotenceA61P 15/12 for climacteric disordersA61P 17/00 Drugs for dermatological di...A61P 17/02 for treating wounds, ulcers...A61P 17/04 AntipruriticsA61P 17/06 AntipsoriaticsA61P 17/14 for baldness or alopeciaA61P 19/02 for joint disorders, e.g. a...A61P 19/06 Antigout agents, e.g. antih...A61P 19/08 for bone diseases, e.g. rac...A61P 21/00 : Drugs for disorders of the ...A61P 21/02 : Muscle relaxants, e.g. for ...A61P 25/00 : Drugs for disorders of the ...A61P 25/04 : Centrally acting analgesics...A61P 25/14 : for treating abnormal movem...A61P 25/16 : Anti-Parkinson drugsA61P 25/18 : Antipsychotics, i.e. neurol...A61P 25/22 : AnxiolyticsA61P 25/24 : AntidepressantsA61P 25/28 : for treating neurodegenerat...A61P 25/30 : for treating abuse or depen...A61P 25/36 : Opioid-abuseA61P 27/02 : Ophthalmic agentsA61P 29/00 : Non-central analgesic, anti...A61P 29/02 : without antiinflammatory ef...A61P 3/00 : Drugs for disorders of the ...A61P 3/04 : Anorexiants; Antiobesity ag...A61P 3/10 : for hyperglycaemia, e.g. an...A61P 31/04 : Antibacterial agentsA61P 31/14 : for RNA virusesA61P 31/18 : for HIVA61P 33/12 : SchistosomicidesA61P 35/00 : Antineoplastic agentsA61P 35/02 : specific for leukemiaA61P 37/02 : ImmunomodulatorsA61P 37/06 : Immunosuppressants, e.g. dr...A61P 37/08 : Antiallergic agents antiast...A61P 43/00 : Drugs for specific purposes...A61P 7/04 : Antihaemorrhagics; Procoagu...A61P 9/00 : Drugs for disorders of the ...A61P 9/10 : for treating ischaemic or a...A61P 9/12 : AntihypertensivesC07D 239/42 : One nitrogen atom nitro rad...C07D 401/12 : linked by a chain containin...C07D 403/12 : linked by a chain containin...C07D 413/12 : linked by a chain containin...