Pyrazoloquinolines

摘要

The invention relates to compounds of the formulae (I), (II) and (III), 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 formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts

主权项

1. A compound of formula (I)in which
R1 denotes Y, -Alk-OY, -Alk-NYY or -Alk-Ar, R2 denotes Y, -Alk-OY, -Alk-NYY, —C(Y)(R6)(R7), —C(Hal)(R6)(R7), —SO2A, —SO2—Ar or —POOH—Ar, R3 denotes H, Hal, CN, -Alk-CN, -Alk-NYY, Het1 or Het2, R4 denotes Hal, Y, Cyc, CN, -Alk-CN, -Alk-COOY, -Alk-CO—NYY or Het1, R5 denotes Hal, Y, OY, NYY, —NY—COY, COOY, —CO—NYY, —CO—NY-Alk-OY, -Alk-CO—NYY, -Alk-OY, -Alk-NYY, Ar, Het1 or Het2, or R3, R5 together denote -Alk-CO—NY—, R6 denotes Hal, Y, —COOY, —CO—NYY, —CO—NY—OY, —CO—NY—C(═NH)—NYY, —CO—NY-Alk-OY, —CO—NY-Alk-NYY, —CO—NY-Alk-SO2—NYY, —CO—NY-Alk-Ar, —CO—NY-Alk-Het2 or —CO—NY—O-Alk-CN, R7 denotes Ar, Het1 or -Het1-Het1, X denotes CH2, O, S or Het1, Y denotes H or A, A denotes unbranched or branched alkyl having 1-10 C atoms, in which, independently of one another, 1-7 H atoms may be replaced by Hal, and/or in which, independently of one another, one or two adjacent CH2 groups are optionally replaced by a —CH═CH— and/or —C≡C— group, Alk denotes alkylene having 1-6 C atoms, in which, independently of one another, 1-4 H atoms are optionally replaced by Hal and/or OY, Cyc denotes cyclic alkyl having 3-7 C atoms, in which, independently of one another, 1-4 H atoms are optionally replaced by Hal and/or OY, Ar denotes phenyl which is unsubstituted or monosubstituted by Hal, A, CN, OY, NYY, —NY—COY, COOY, Het1, Het2, -Alk-OY, -Alk-NYY, -Alk-Het1 or Alk-Het2, Het1 denotes mono- or bicyclic heteroaryl having 2-9 C atoms and 1-4 N, O and/or S atoms, which is unsubstituted or monosubstituted by Hal, A, CN, OY, NYY, —NY—COY, COOY, -Alk-OY or -Alk-NYY, Het2 denotes a monocyclic saturated heterocycle having 2-7 C atoms and 1-4 N, O and/or S atoms, which is unsubstituted or monosubstituted by A, and Hal denotes F, Cl, Br or I, or a pharmaceutically acceptable salt or tautomer thereof.