(1H-Ind0l-7-Yl)-(Pyrimidin-2-Ylamino)Methanone Derivatives and Related Compounds as Igf-R1 Inhibitors for the Treatment of Cancer
申请人:Heinrich Timo
公开号:US20080194605A1
公开(公告)日:2008-08-14
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, 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
and/or S(O)
9
A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CH
2
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, NH
2
, NA
2
, NHA, CH
2
, CH
3
, OH, OA, O or S, E: CH
2
, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH
2
, O or NH, Q: 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
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)的化合物,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香族同系或异系环,可以是未取代的或经过一次、两次或三次取代的,取代基为羰基氧、卤素、A、OH、OA、NH2、NHA、NA2、NO2、CN、OCN、SCN、COOH、COOA、CONH2、CONHA、CONA2、NHCOA、NHCONH2、NHSO2A、CHO、COA、SO2NH2和/或S(O)9A,A表示具有1-14个C原子的直链、支链或环烷基,其中一个或两个CH2基团可以被O或S原子和/或- CR = CH-基团取代,此外,1-7个H原子可以被F和/或Cl取代,Hal:F、Cl、Br或I,D:NH、NH2、NA2、NHA、CH2、CH3、OH、OA、O或S,E:CH2、CH、NH或N,Y:E或饱和或不饱和键,X:CH2、O或NH,Q:Hal、A、OH、OA、NH2、NHA、NA2、NO2、CN、OCN、SCN、COOH、COOA、CONH2、CONHA、CONA2、NHCOA、NHCONH2、NHSO2A、CHO、COA、SO2NH2或X-M,以及制备和使用它们制备治疗疾病的药物,特别是涉及激酶的肿瘤和/或疾病的发展或过程。