| 摘要 |
The invention relates to compounds of the formulae (I), (II) and (III);
in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in Claim 1, 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 sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, 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 one of their salts. |
| 主权项 |
1. Compounds of the formula (IA) in which R1 denotes H, Hal, CN, A, OY, NYY or —NH—C(NYY)═NY, R2 denotes H, Cyc, Ar, Het1 or Het2, R3 denotes Y, OH or OA, R4 denotes H or Hal, Y denotes H, A or Alk-OA, W1, denotes CR3 or N, W2 together also denotes CH2, L denotes a single bond, —CYR3-, —CO—, —CO—NY—, —NY—CO—, —NY—CO—NY—, —NY—SO2—, —C(═NR3)-, —C(═N—CN)—, -Alk-, -Alk-NY—, Alk-CO—, -Alk-CO—NY—, -AlkO—,
-Alk-OAlk-, -Alk-C(Y)(OY)—, —C(Y)(CN)—, —C(Y)(Het1)-, —C(R3)(Het1)-, —C(Y)(Het1)-NY—, —C(Y)(Het2)-, —C(Y)(OY)—, —C(Y)(OCOOY)—, —C(Y)(NYY)—, —C(Y)(NY—COY)—, —C(Y)(NY—CO—NYY)—, —C(Y)(OAlk-CN)—, —C(Y)(OAlk-Het2)-,—C(Y)(OAlk-NYY)—, —C(Y)(OAlk-CO—NYY)—, —C(Y)(OY)-Alk-, —C(Y)(OCO—NYY)—,—C(Y)(OCO—NY-Alk-COOY)-oder-C(Y)(OY)-Het1-Alk-OCO—NY—, A denotes unbranched or branched alkyl having 1-10 C atoms, where 1-7 H atoms may be replaced, independently of one another, by Hal, Alk denotes alkylene having 1-6 C atoms, where 1-4 H atoms may be replaced, independently of one another, by Hal and/or CN, Cyc denotes cyclic alkyl having 3-7 C atoms, where 1-4
H atoms may be replaced, independently of one another by A, Hal and/or OY, Ar denotes phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono, di- or trisubstituted Y, OY, Hal, CN, COOY, -Alk-OY, NYY, —NY—COY, SiY3, Cyc and/or pheny, Het1 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-, di- or trisubstituted by Y, OY, Hal, CN, COOY, -Alk-OY, NYY, —NY—COY, -Alk-Het2, -Alk-OCO-Het2, -Alk-OCO—NY-Het2, —NY—CO-Het2, —NY—CO-Alk-Het2, SiY3, Cyc and/or phenyl, where pyridyl-methoxy is excluded if R1 is NYY, Het2 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 R3 and/or COY, Hal F, Cl, Br or I, and n denotes 1, 2, 3 or 4 or physiologically acceptable salts thereof. |
