主权项 |
1. Compounds of the formula I in which R1 denotes Ar1 or Het1, R2 denotes Ar2, Het2, NH(CH2)nAr2, O(CH2)nAr2, NH(CH2)nHet2, NHCONHA, CONH2 or N3, R4 denotes H or F, Ar1 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R3)2]nCN, (CH2)nOH, (CH2)nOA, (CH2)nCOOH, (CH2)nCOOA, S(O)mA, (CH2)nHet3, CON(R3)2, CONH(CH2)nC(R3)2N(R3)2 and/or CONH(CH2)pCH[(CH2)nOR3](CH2)pOR3, Ar2 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by A, Hal, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, SO2NH2, SO2NHA, SO2NA2, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, [C(R3)2]nN(R3)2, CONH(CH2)pCH[(CH2)nN(R3)2] (CH2)pOR3, CONH(CH2)pCH[(CH2)nOR3]NHSO2A, CONH(CH2)pCH[(CH2)nOR3]OR3, CONH(CH2)p[(CH(OR)]pCH2OR3, CONHR4, CONH(CH2)pCH[(CH2)nN(R3)2]Cyc, CONH(CH2)nC(R3)2N(R3)2 and/or CONHC(R3)2(CH2)pOR3, Het1 denotes benzo-1,3-dioxolyl or indazolyl, each of which is unsubstituted or monosubstituted by A, Het2 denotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, quinolyl, isoquinolyl, benzimidazolyl, furopyridinyl or indazolyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, NH(CH2)nHet4, A, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2 and/or ═O, Het3 denotes tetrazolyl or oxadiazolyl, each of which is unsubstituted or mono- or disubstituted by A, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2 and/or ═O, Het4 denotes piperidinyl or tetrahydrofuranyl, each of which is unsubstituted or monosubstituted by A or NH2, R3 denotes H or alkyl having 1, 2, 3 or 4 C-atoms, 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 groups may be replaced by O and/or NH, or
cyclic alkyl having 3-7 C atoms, which may be unsubstituted or monosubstituted by OH, NHCOA or NH2, Cyc denotes cyclic alkyl having 3-7 C atoms, m denotes 0, 1 or 2, n denotes 0, 1, 2, 3 or 4, p denotes 1, 2, 3 or 4, and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. |