主权项 |
1. A method for the therapeutic treatment of a disease in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role and wherein the disease treated is:
a solid tumour which is a tumour of the squamous epithelium, the bladder, the stomach, the kidneys, the head or neck, the oesophagus, the cervix, the thyroid, the intestine, the liver, the brain, the prostate, the uro-genital tract, the lymphatic system, the stomach, the larynx or the lung; a solid tumour selected from monocytic leukaemia, lung adenocarcinoma, small-cell lung carcinoma, pancreatic cancer, glioblastoma, colon carcinoma and breast carcinoma; a tumour of the blood or immune system; or a tumour which originates from acute myeloid leukaemia, chronic myeloid leukaemia, acute lymphatic leukaemia and/or chronic lymphatic leukaemia; the method comprising administering to a patient a compound of formula I or a pharmaceutically usable salt, solvate, tautomer or stereoisomer thereof, including mixtures thereof in all ratios: in which R1 denotes Ar or Het, R2 denotes a saturated, unsaturated or aromatic 5-membered heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by Hal, A, (CH2)nOR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, Het1, —[C(R3)2]nN(R3)2, —[C(R3)2]nHet1, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet1, S[C(R3)2]nN(R3)2, S[C(R3)2]nHet1, —NR3[C(R3)2]nN(R3)2, —NR3[C(R3)2]nHet1, —NR3Het1, NHCON(R3)2, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, CON(R3)2, ONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nHet1, COHet1, COA and/or ═O, R3 denotes H or A, R4, R5 each, independently of one another, denote H, Hal, A, OR3, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2 or S(O)mA, A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by F, Cl and/or Br, and/or in which one or two CH2 groups may be replaced by O, S, SO, SO2 and/or CH═CH groups,
orcyclic alkyl having 3-7 C atoms, Ar denotes phenyl, naphthyl or biphenyl, each of which is unsub-stituted or mono-, di- or trisubstituted by Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, Het1, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1and/or COA, Het denotes a mono-, bi- or tricyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, Het1, O[C(R3)2]n-N(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO-Het1, CHO, COA, ═S, ═NH, ═NA and/or ═O, Het1 denotes a monocyclic saturated or aromatic heterocycle having 1 to 2 N and/or O atoms, which may be mono- or disubstituted by A, OA, OH, Hal, (CH2)nN(R3)2, (CH2)nOR3, (CH2)nHet2 and/or ═O, Het2 denotes pyrrolidino, piperidino or morpholino, Hal denotes F, Cl, Br or I, m denotes 0, 1 or 2, n denotes 1, 2, 3 or 4. |