Novel Pyrimidine Imidazole Amines as Modulators of Kinase Activity

摘要

The invention provides novel imidazole amine compounds according to formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

主权项

1. A compound of formula (I):and pharmaceutically acceptable salts, solvates, solvates of salts, or prodrugs thereof, wherein:
R1 is Hal, LA, OH, O(LA), NH2 and/or NH(LA), N(LA)2, NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), NHCONH(LA), NHCONH2, NHSO2(LA), CHO, CO(LA), SO2NH2, SO2(LA), or a C5-10 aryl or C6-15 fused aryl, a 3-12 membered saturated or partially unsaturated monocyclic or bicyclic carbocyclic ring, a 3-12 membered monocyclic or bicyclic heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-12 membered monocyclic or bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally mono-, di- or trisubstituted by Hal, LA, OH, O(LA), NH2 and/or NH(LA), N(LA)2, NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), NHCONH(LA), NHCONH2, NHSO2(LA), CHO, CO(LA), SO2NH2, SO2(LA) and/or SO2H, or an unbranched or branched linear or cyclic alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 C atoms, in which one or two CH2 groups may be replaced by an O atom and/or by an —NH—, NH(LA), —CO—, —NHCO— or —CH═CH— group, and/or in which a CH group may be replaced by —N—; R3 is H, an unbranched or branched linear or mono- or bicyclic alkyl group having 1, 2, 3, 4, 5, 6, 7, 8 or 9 C atoms, in which one or two CH2 groups may be replaced by an —O—, —NH—, group, and/or in which one or two CH groups may be replaced by —N—,
and/or in which 1, 2 or 3 H atoms may be replaced by Hal or OH, R2 is C5-10 aryl or C6-15 fused aryl, a 3-12 membered saturated or partially unsaturated monocyclic or bicyclic carbocyclic ring, a 3-12 membered monocyclic or bicyclic heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-12 membered monocyclic or bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally mono-, di- or trisubstituted by Hal, LA, OH, O(LA), NH2 and/or NH(LA), N(LA)2, NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), NHCONH(LA), NHCONH2, NHSO2(LA), CHO, CO(LA), SO2NH2, SO2(LA); Hal is F, Cl, Br or I, and LA is an unbranched or branched, saturated or partially unsaturated, linear hydrocarbon chain having 1, 2, 3 or 4 C atoms, wherein 1, 2 or 3 H atoms may be replaced by Hal.