发明名称 Imidazole amines as modulators of kinase activity
摘要 The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
申请公布号 US9145392(B2) 申请公布日期 2015.09.29
申请号 US201214237075 申请日期 2012.09.12
申请人 Merck Patent GmbH 发明人 Lan Ruoxi;Huck Bayard R.;Xiao Yufang;Chen Xiaoling;Deselm Lizbeth Celeste;Qiu Hui;Neagu Constantin;Bankston Donald;Jones Christopher Charles Victor
分类号 C07D401/14;A61K31/4545;A61K31/506;A61K31/5377;C07D409/14;C07D413/14;C07D417/14;C07D491/107 主分类号 C07D401/14
代理机构 EMD Serono Research and Development Institute 代理人 Kim Dwight D.;EMD Serono Research and Development Institute
主权项 1. A compound of Formula (I): and pharmaceutically acceptable salts, solvates, or solvates of salts, 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 mono- or bicyclic, aliphatic or aromatic homo- or heterocycle having 0, 1, 2, 3 or 4 N, S and/or O atoms and 4, 5 or 6, 7, 8, 9, or 10 skeleton atoms which may be unsubstituted or, independently of one another, 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 SO2Hal 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—; R2 is H, NH2, NH(LA), N(LA)2 or NHCO(LA); R3 is N or CH; R4 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, R5 is a monocyclic aromatic or aliphatic homo- or heterocycle having 0, 1 or 2 N, S and/or O atoms and 5 or 6 skeleton atoms which may be unsubstituted or, independently of one another, 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, CI, Br or I, and LA is an unbranched or branched, saturated or partially unstaturated, linear hydrocarbon chain having 1, 2, 3 or 4 C atoms, wherein 1, 2 or 3 H atoms may be replaced by Hal.
地址 Darmstadt DE