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    • 5. 发明申请
    • 7H-8,9-DIHYDRO-PYRANO (2,3-C) IMIDAZO (1,2A) PYRIDINE DERIVATIVES AND THEIR USE AS GASTRIC ACID SECRETION INHIBITORS
    • 7H-8,9-二氢吡喃(2,3-C)咪唑(1,2A)吡啶衍生物及其作为胃酸分泌抑制剂的用途
    • WO2005090358A3
    • 2006-01-26
    • PCT/EP2005051211
    • 2005-03-16
    • ALTANA PHARMA AGPALMER ANDREASBUHR WILM
    • PALMER ANDREASBUHR WILMCHIESA M VITTORIAZIMMERMANN PETER JANBREHM CHRISTOFSIMON WOLFGANG-ALEXANDERKROMER WOLFGANGPOSTIUS STEFAN
    • C07D491/14A61K31/437C07D221C07D235C07D311
    • C07D491/14
    • The invention provides compounds of the formula (1), in which R1 is hydrogen, 1-4C-alkyl, 3-7C-cydoalkyl, 3-7C-cycloalkyl-1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxy-1-­4C-alkyl, 1-4C-alkoxycarbonyl, 2-4C-alkenyl, 2-4C-alkynyl, fluoro-l-4C-alkyl or hydroxy-1-4C­alkyl, R2 is hydrogen, 1-4C-alkyl, 3-7C-cydoalkyl, 3-7C-cycloalkyl.-1-4C-alkyl, 1-4C-alkoxycarbonyl, hy­droxy-1-4C-alkyl, hydroxy-3-4-C-alkenyl, hydroxy-3-4C-alkinyl, halogen, 2-4C-alkenyl, 2-4C­alkynyl, fluoro-1-4C-alkyl, cyanomethyl, hydroxy, 1-4C-alkoxy, amino, mono- or di-1-4C­alkylamino, 1-4C-alkylcarbonylamino, 1-4C-alkoxycarbonylamino, 1-4C-alkoxy-1-4C­alkoxycarbonylamino, carboxyl, mono- or di-1-4C-alkylamino-1-4C-alkyl, 1-4C-alkylcarbonyl, 2­4C-alkenylcarbonyl, 2-4C-alkinylcarbonyl or the radical -CO-NR21R22, R3 is 1-4C-alkylcarbonyl, hydroxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkoxy-l­4C-alkyl, 1-4C-alkoxycarbonyl, fluoro-1-4C-alkoxy-1-4C-alkyl, cyano, the radical -CO-NR31R32, the radical -S0 2 -NR31 R32, the radical -CS-NR31 R32, the radical -C=N(OH)-NR1 R32 or the group Het. Arom is a R4-, R5-, R6- and R7-substituted mono- or bicyclic aromatic radical selected from the group consisting of phenyl, naphthyl, pyrrolyl, pyrazolyl, imidazolyl, 1,2,3-triazolyl, indolyl, benzimida­zolyl, furanyl (furyl), benzofuranyl (benzofuryl), thiophenyl (thienyl), benzothiophenyl (ben­zothienyl), thiazolyl, isoxazolyl, pyridinyl, pyrimidinyi, quinolinyl and isoquinolinyl. The compounds inhibit the secretion of gastric acid.
    • 本发明提供式(1)化合物,其中R 1是氢,1-4C-烷基,3-7C-环烷基,3-7C-环烷基1-4C-烷基,1-4C-烷氧基,1-4C - 烷氧基-14C-烷基,1-4C-烷氧基羰基,2-4C-烯基,2-4C-炔基,氟-141-烷基或羟基-14C烷基,R2是氢,1-4C-烷基 ,3-7C-环烷基,3-7C-环烷基,1-4C-烷基,1-4C-烷氧基羰基,羟基-14C-烷基,羟基-34-C-烯基,羟基-3-4c- 链烯基,卤素,2-4C-烯基,2-4C炔基,氟-1-4C-烷基,氰基甲基,羟基,1-4C-烷氧基,氨基,单或二1-4C烷基氨基,1-4C-烷基羰基氨基,1 1-4C-烷氧基羰基氨基,1-4C-烷氧基-14C烷氧基羰基氨基,羧基,单或二1-4C-烷基氨基1-4C-烷基,1-4C-烷基羰基,24C-链烯基羰基,2-4C-链烯基羰基 或基团-CO-NR 21 R 22,R 3是1-4C-烷基羰基,羟基-4- C 1-4 - 烷基,1-4C-烷氧基 - 1-4C-烷基,1-4C-烷氧基-1-4C-烷氧基-14C- 烷基,1-4C-烷氧基羰基,氟-1-4C-烷氧基-1-4C-烷基,氰基,基团-CO-NR31R32,基团-S0 < 基团-NR 31 R 32,基团-CS-NR 31 R 32,基团C = N(OH)-NR 1 R 32或基团Het。 Arom是选自苯基,萘基,吡咯基,吡唑基,咪唑基,1,2,3-三唑基,吲哚基,苯并咪唑基,呋喃基的呋喃基的R4-,R5-,R6-和R7取代的单环或二环芳基 (呋喃基),苯并呋喃基(苯并呋喃基),噻吩基(噻吩基),苯并噻吩基(苯并噻吩基),噻唑基,异恶唑基,吡啶基,嘧啶基,喹啉基和异喹啉基。 这些化合物抑制胃酸的分泌。