| 摘要 |
The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.;The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into a salt thereof. |
| 主权项 |
1. Compounds of formula (I) wherein R1 denotes Het1 or Ar; R2, R3, are each independently Y or OY, or together denote —O—(CH2)n—; each R4 independently denotes A or (CH2)nOA; L denotes —CR2R3—, a single bond, —(CH2)n—, —CH(Hal)-, —C(Hal)2-, —(CH2)nCH(OY)—, —(CH2)nCO—, —(CH2)nNH—, —(CH2)nCONY2—, —NYCO—, —NHCO—NH—, —NR4CO—, —NYSO2—, —C(═NR4)—, —C(═NCN)—, —CY(NY2)—, —CY(CN)—, —CY(O—(CH2)nCN)—, —CY(Het2)- or —CY(O—(CH2)nHet2)-; each Y independently denotes H or A; each A independently denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by Hal; each Cyc independently denotes cyclic alkyl having 3-7 C atoms, in which 1-4 H atoms may be replaced by Hal; each Ar independently denotes phenyl which is unsubstituted or mono- or disubstituted by Hal, (CH2)pOY, R4, (CH2)pOR4, COOY, NY2, NYCOY and/or CN; each Het1 independently denotes mono- or bicyclic heteroaryl having 2-9 C atoms and 1-4 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by Hal, (CH2)pOY, R4, (CH2)pOR4, ═O, COOY, NY2, NYCOY, CONY2, Cyc, Het2 and/or CN; each Het2 independently denotes a monocyclic saturated heterocycle having 2-7 C atoms and 1-4 N, O and/or S atoms, which may be unsubstituted or monosubstituted by A; each Hal independently denotes F, Cl, Br or I; m denotes 0, 1 or 2; and each n, p, independently denotes 0, 1, 2, 3, 4 or 5, and/or physiologically acceptable salts, tautomers and/or stereoisomers thereof, including mixtures thereof in all ratios. |
