Back to results
US 7,442,697 B2Granted
4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity
AssigneeAstraZeneca AB
InventorsNicholas John Newcombe, Andrew Peter Thomas
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
Claims11
A compound of formula (I):
- wherein:
- R1 is halo, cyano, C1-3alkyl or C1-3alkoxy;
- p is 0-2;
- wherein the values of R1 may be the same or different;
- R2 is C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, a heterocyclyl or heterocyclylC1-3 alkyl;
- wherein R2 may be optionally substituted on carbon by one or more methyl, ethyl, methoxy, ethoxy, propoxy, trifluoromethyl, trifluoromethoxy, 2,2,2-trifluoroethoxy or cyclopropylmethoxy;
- and wherein if said heterocyclyl contains an —NH— moiety that nitrogen may be optionally substituted by one or more methyl, ethyl, acetyl, 2,2,2-trifluoroethyl or methoxyethyl;
- R3 is hydrogen, halo or cyano;
- R4 is C1-6alkyl or C1-6alkoxyC1-6alkyl;
- R5 is substituted methyl, optionally substituted C2-6alkyl, or optionally substituted C2-6alkenyl;
- wherein said substituents are selected from one or more methoxy, ethoxy, propoxy, trifluoromethyl, trifluoromethoxy, 2,2,2-trifluoroethoxy or cyclopropylmethoxy;
- or a pharmaceutically acceptable salt thereof;
- provided that the compound is not 4-(1-methyl-2-ethylimidazol-5-yl)-2-{4-[N-(tetrahydrofur-2-ylmethyl)sulphamoyl]anilino}pyrimidine;
- 4-(1-methyl-2-ethyl-imidazol-5-yl)-2-{4-[N-(2-methoxyethyl)sulphamoyl]anilino}pyrimidine;
- 4-(1-methyl-2-isopropyl-imidazol-5-yl)-2-{4-[N-(2-methoxyethyl)sulphamoyl]anilino}pyrimidine;
- 4-(1-methyl-2-isopropyl-imidazol-5-yl)-2-{4-[N-(cyclopropylmethyl) sulphamoyl]anilino}pyrimidine;
- 4-(1-methyl-2-isopropyl-imidazol-5-yl )-2-{4-[N-(tetrahydrofur-2-ylmethyl)sulphamoyl]anilino}pyrimidine;
- 4-(1-methyl-2-ethylimidazol-5-yl)-2-{4-[N-(cyclopropylmethyl) sulphamoyl]anilino}pyrimidine;
- 4-(1-methyl-2-ethyl-imidazol-5-yl)-2-[4-(N-cyclopropylsulphamoyl) anilino]pyrimidine;
- 4-(1-methyl-2-ethylimidazol-5-yl)-2-[4-(N-cyclobutyl-sulphamoyl) anilino]pyrimidine;
- or 4-(1-methyl-2-methoxymethylimidazol-5-yl)-2-{4-[N-(2-methoxyethyl) sulphamoyl]anilino}pyrimidine.
18 more elements
Dependencies are inferred from the claim text.