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US 8,263,590 B2Granted
Pyrimidine derivatives
OwnerCarlos Garcia-Echeverria, Takanori Kanazawa +6inventors
InventorsCarlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
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Abstract
Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
Claims13
A compound of formula I
- wherein
- each of R0, R1, and R2, independently is hydrogen, C1-C8alkyl, C2-C8alkenyl, C2-C8alkinyl, C3-C8cycloalkyl, C3-C8cycloalkylC1-C8alkyl, C5-C10arylC1-C8alkyl, hydroxyC1-C8alkyl, C1-C8alkoxyC1-C8alkyl, aminoC1-C8alkyl, haloC1-C8alkyl, unsubstituted or substituted C5-C10aryl, unsubstituted or substituted 5 or 6 membered heterocyclyl comprising 1, 2 or 3 hetero atoms selected from N, O and S, hydroxy, C1-C8alkoxy, hydroxyC1-C8alkoxy, C1-C8alkoxyC1-C8alkoxy, haloC1-C8alkoxy, unsubstituted or substituted C5-C10arylC1-C8alkoxy, unsubstituted or substituted heterocyclyloxy, or unsubstituted or substituted heterocyclylC1-C8alkoxy, unsubstituted or substituted amino, C1-C8alkylthio, C1-C8alkylsulfinyl, C1-C8alkylsulfonyl, C5-C10arylsulfonyl, halogen, carboxy, C1-C8alkoxycarbonyl, unsubstituted or substituted carbamoyl, unsubstituted or substituted sulfamoyl, cyano or nitro;
- R3 is unsubstituted or substituted sulfamoyl;
- Or the pair of adjacent substituents R2 and R3 forms —CH2—NH—CO— or —CH2—NH—SO2— or such pairs wherein NH is substituted by C1-C8-alkyl;
- R4 is hydrogen or C1-C8alkyl;
- R5 is halogen;
- R6 is hydrogen;
- each of R7, R8, R9, and R10 independently is C1-C8alkyl, C2-C8alkenyl, C2-C8alkinyl, C3-C8cycloalkyl, C3-C8cycloalkylC1-C8alkyl, C5-C10arylC1-C8alkyl, hydroxyC1-C8alkyl, C1-C8alkoxyC1-C8alkyl, aminoC1-C8alkyl, haloC1-C8alkyl, unsubstituted or substituted C5-C10aryl, unsubstituted or substituted 5 or 6 membered heterocyclyl comprising 1, 2 or 3 hetero atoms selected from N, O and S, hydroxy, C1-C8alkoxy, hydroxyC1-C8alkoxy, C1-C8alkoxyC1-C8alkoxy, haloC1-C8alkoxy, unsubstituted or substituted C5-C10arylC1-C8alkoxy, unsubstituted or substituted heterocyclyloxy, or unsubstituted or substituted heterocyclylC1-C8alkoxy, unsubstituted or substituted amino, C1-C8alkylthio, C1-C8alkylsulfinyl, C1-C8alkylsulfonyl, C5-C10arylsulfonyl, halogen, carboxy, C1-C8alkoxycarbonyl, unsubstituted or substituted carbamoyl, unsubstituted or substituted sulfamoyl, cyano or nitro;
- wherein R7, R8 and R9 independently of each other can also be hydrogen;
- or R7 and R8, R8 and R9, and/or R9 and R10 form together with the carbon atoms to which they are attached, a 5 or 6 membered carbocyclic or heterocyclic ring comprising 0, 1, 2 or 3 heteroatoms selected from N, O and S that is unsubstituted or substituted by C1-C8-alkyl, C1-C8-alkoxy, halo-C1-C8-alkyl, hydroxyl, amino, substituted amino, halogen, carboxy, C1-C8alkoxycarbonyl, carbamoyl, cyano, or oxo;
- A is C;
- and salts thereof.
9 more elements
The compound 2-{5-Chloro-2-[4-(3-methylamino-pyrrolidin-1-yl)-phenylamino]-pyrimidin-4-ylamino}-N-isopropyl-benzenesulfonamide.
Dependencies are inferred from the claim text.