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    • 31. 发明申请
    • (1H-Ind0l-7-Yl)-(Pyrimidin-2-Ylamino)Methanone Derivatives and Related Compounds as Igf-R1 Inhibitors for the Treatment of Cancer
    • (1H-吲哚-7-基) - (嘧啶-2-基氨基)甲酮衍生物和相关化合物作为Igf-R1抑制剂治疗癌症
    • US20080194605A1
    • 2008-08-14
    • US11911268
    • 2006-03-17
    • Timo HeinrichAndree BlaukatMaria Kordowicz
    • Timo HeinrichAndree BlaukatMaria Kordowicz
    • A61K31/497C07D401/14A61P35/04C07D401/12
    • C07D401/14C07D403/12C07D403/14C07D405/14
    • The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 and/or S(O)9A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CR═CH— groups and/or in addition 1-7 H atoms may be replaced by F and/or Cl, Hal: F, Cl, Br or I, D: NH, NH2, NA2, NHA, CH2, CH3, OH, OA, O or S, E: CH2, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH2, O or NH, Q: Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 or X-M, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.
    • 本发明涉及式(I)化合物,其中Ar表示具有1至4个N,O和/或S原子和5至10个骨架原子的单环或双环芳族均聚或杂环,其可以是未取代的或 羰基氧,Hal,A,OH,OA,NH 2,NHA,NA 2,NO 2, ,CN,OCN,SCN,COOH,COOA,CONH 2,CONHA,CONA 2,NHCOA,NHCONH 2,NHSO 2 A,CHO,COA,SO 2 NH 2和/或S(O)9 A,A表示无支链,支链 或具有1-14个C原子的环状烷基,其中一个或两个CH 2基团可以被O或S原子和/或被-CR-CH-基团和/或另外的1- 7 H原子可以被F和/或Cl,Hal:F,Cl,Br或I,D:NH,NH 2,NH 2,NH 2,CH CH 2,CH 3,OH,OA,O或S,E:CH 2,CH,NH或N,Y:E或 饱和或不饱和键,X:CH 2,O或NH,Q:Hal,A,OH,OA,NH 2,NHA,N CN 2,NO 2,CN,OCN,SCN,COOH,COOA,CONH 2,CONHA,CONA 2 ,NHCOA,NHCONH 2,NHSO 2 A,CHO,COA,SO 2 NH 2或XM, 涉及其制备和用途,用于制备用于治疗疾病,特别是涉及激酶的发展或过程中的肿瘤和/或疾病的药物。