| 主权项 |
1. Compounds of the formula Iin which
R1 denotes H, F, Cl, CN, CH3, CH2OH, CH2Cl, CH2Br, CF3, CHF2 or CH2F, R2 denotes H or A, R3 denotes H, F, Cl, CH3, CF3 or CHF2, X denotes CR3 or N, Y denotes Ar1, Carb, Het1 or Cyc, Ar1 denotes phenyl or naphthyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R2)2]pOR2, [C(R2)2]pN(R2)2, [C(R2)2]pHet2, NO2, CN, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, NR2COA, NR2SO2A, [C(R2)2]pSO2N(R2)2, S(O)nA, COHet3, O[C(R2)2]mN(R2)2, O[C(R2)2]pAr2, O[C(R2)2]pHet2, NHCOOA, NHCON(R2)2, Cyc, CHO and/or COA, Ar2 denotes phenyl, which is unsubstituted or mono- or disubstituted by Hal, A, [C(R2)2]pOR2, [C(R2)2]pN(R2)2, [C(R2)2]pHet3, NO2, CN, [C(R2)2]pCOOR, [C(R2)2]pN(R2)2, N(R2)2COA, NR2SO2A, [C(R2)2]pSO2N(R2)2, S(O)nA, COHet3, O[C(R2)2]mN(R2)2, O[C(R2)2]pHet3, NHCOOA, NHCON(R2)2, CHO and/or COA, Het1 denotes pyrrolidinyl, azetidinyl, tetrahydroimidazolyl, tetrahydrofuranyl, tetrahydropyrazolyl, tetrahydropyranyl, piperidinyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, piperazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl, quinolyl, 1,3-benzodioxolyl, benzothiophenyl, benzofuranyl, imidazopyridyl or furo[3,2-b]pyridyl, each of which is unsubstituted or mono- or disubstituted by Hal, A, [C(R2)2]pOR2, [C(R2)2]pN(R2)2, [C(R2)2]pHet2, [C(R2)2]pAr2, NO2, CN, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, NR2COA, NR2SO2A, [C(R2)2]pSO2N(R2)2, S(O)nA, COHet3, [C(R2)2]mN(R2)2, O[C(R2)2]pAr2, O[C(R2)2]pHet2, NHCOOA, NHCON(R2)2, CHO, COA, ═S, ═NR and/or ═O, Carb denotes indanyl or tetrahydronaphthyl, each of which may be unsubstituted or mono-, di-, tri- or tetrasubstituted by A, Cyc denotes cyclic alkyl with 3, 4, 5, 6 or 7 C-atoms, which may be unsubstituted or monosubstituted by A, OH, Hal, CN or Ar2 or Het2, Het2 denotes pyrrolidinyl, azetidinyl, tetrahydroimidazolyl, tetrahydrofuranyl, tetrahydropyrazolyl, tetrahydropyranyl, piperidinyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, piperazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl, quinolyl, 1,3-benzodioxolyl, benzothiophenyl, benzofuranyl, imidazopyridyl or furo[3,2-b]pyridyl, each of which is unsubstituted or mono- or disubstituted by Hal, A, [C(R2)2]pOR2, [C(R2)2]pN(R2)2, [C(R2)2]pHet3, [C(R2)2]pOHet3, [C(R2)2]pAr2, NO2, CN, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, NR2COA, NR2SO2A, [C(R2)2]pSO2N(R2)2, S(O)nA, COHet3, O[C(R2)2]mN(R2)2, O[C(R2)2]pAr2, O[C(R2)2]pHet3, NHCOOA, NHCON(R2)2, CHO, COA, ═S, ═NR and/or ═O, Het3 denotes dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, tetrahydropyranyl or piperazinyl, each of which is unsubstituted or mono- or disubstituted by Hal, CN, OR2, COOR2, CON(R2)2, S(O)nA, S(O)nAr, COA, A and/or ═O, A denotes unbranched or branched alkyl with 1-10 C-atoms, wherein two adjacent CH- and/or CH2-groups may form a double bond and wherein one or two non-adjacent CH- and/or CH2-groups may be replaced by N-, O- and/or S-atoms and wherein 1-7 H-atoms may be replaced by F or Cl, Hal denotes F, Cl, Br or I, n denotes 0, 1 or 2, m denotes 1, 2 or 3, p denotes 0, 1, 2, 3 or 4, with the proviso that, if R1 is CH2OH, then Ar1 is not 2,4-dichlorophenyl,and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. |
