| 主权项 |
1. A method of treating or preventing cancer, comprising administering to a subject a therapeutically effective amount of a compound of formula I wherein X denotes CH or N, R1 denotes NH2, CONH2 or H, R2 denotes Hal, Ar1 or Het1, R3 denotes NR5[C(R5)2]nHet2, NR5[C(R5)2]nCyc, Het2, O[C(R5)2]nAr2, NR5[C(R5)2]nAr2, O[C(R5)2]nHet2, NR5(CH2)pNR5R6, O(CH2)pNR5R6 or NR5(CH2)pCR7R8NR5R6, R4 denotes H, CH3 or NH2, R5 denotes H or alkyl having 1, 2, 3 or 4 C atoms, R6 N(R5)2CH2CH═CHCONH, Het3CH2CH═CHCONH, CH2═CHCONH(CH2), Het4(CH2)nCOHet3-diyl-CH2CH═CHCONH, HC≡CCO, CH3C≡CCO, CH2═CH—CO, CH2═C(CH3)CONH, CH3CH═CHCONH(CH2), N≡CCR7R8CONH(CH2)n, Het4NH(CH2)pCOHet3-diyl-CH2CH═CHCONH, Het4(CH2)pCONH(CH2CH2O)p(CH2)pCOHet3-diyl-CH2CH═CHCONH, CH2═CHSO2, ACH═CHCO, CH3CH═CHCO, Het4(CH2)pCONH(CH2)pHet3-diyl-CH2CH═CHCONH, Ar3CH═CHSO2, CH2═CHSO2NH or N(R5)CH2CH═CHCO, R7, R8 denote together alkylene having 2, 3, 4, or 5 C atoms, Ar1 denotes phenyl or naphthyl, each of which is unsubstituted or mono-, di- or trisubstituted by R6, Hal, (CH2)nNH2, CONHAr3, (CH2)nNHCOA, O(CH2)nAr3, OCyc, A, COHet3, OA and/or OHet3 (CH2), Ar2 denotes phenyl, naphthyl or pyridyl each of which is unsubstituted or mono-, di- or trisubstituted by R6, Hal, OAr3, (CH2)nNH2, (CH2)nNHCOA and/or Het3, Ar3 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by OH, OA, Hal, CN and/or A, Het1 denotes a mono- or bicyclic 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 R6, O(CH2)nAr3 and/or (CH2)nAr3, Het2 denotes a mono- or bicyclic saturated heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by R6, Het3, CycSO2, OH, Hal, COOH, OA, COA, COHet3, CycCO, SO2 and/or ═O, Het3 denotes a monocyclic unsaturated, saturated 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 and/or ═O, Het4 denotes a bi- or tricyclic unsaturated, saturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di-, tri- or tetrasubstituted by A, NO2, Hal and/or ═O, Cyc denotes cyclic alkyl having 3, 4, 5 or 6 C atoms, which is unsubstituted, monosubstituted or disubstituted by R6 and/or OH and which may comprise a double bond, A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH2 and/or CH-groups may be replaced by O, NH and/or by N, Hal denotes F, Cl, Br or I, n denotes 0, 1, 2, 3 or 4, p denotes 1, 2, 3, 4, 5 or 6, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. |
