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    • 4. 发明申请
    • NOVEL BENZOFURAN-4-CARBOXAMIDES
    • 新型苯并呋喃-4-羧酰胺
    • WO1998007715A1
    • 1998-02-26
    • PCT/EP1997004398
    • 1997-08-13
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBHAMSCHLER, Hermann
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBHULRICH, Wolf-RüdigerFLOCKERZI, DieterGUTTERER, BeateTHIBAUT, UlrichHATZELMANN, ArminSCHUDT, ChristianBEUME, RolfHÄFNER, DietrichKLEY, Hans-Peter
    • C07D307/79
    • C07D307/79C07D405/12
    • Compounds of formula (I) in which R1 is 1-2C-alkoxy or 1-2C-alkoxy which is completely or mainly substituted by fluorine, R2 is 1-7C-alkyl, 3-7C-cycloalkyl or 3-7C-cycloalkylmethyl, Ar is phenyl, pyridyl, phenyl which is substituted by R3, R4 and R5 or pyridyl which is substituted by R6, R7, R8 and R9, where R3 is hydroxyl, halogen, cyano, carboxyl, trifluoromethyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, amino, mono- or di-1-4C-alkylamino or 1-4C-alkylcarbonylamino, R4 is hydrogen, hydroxyl, halogen, amino, trifluoromethyl, 1-4C-alkyl or 1-4C-alkoxy, R5 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy, R6 is hydroxyl, halogen, cyano, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl or amino, R7 is hydrogen, halogen, amino or 1-4C-alkyl, R8 is hydrogen or halogen and R9 is hydrogen or halogen, the salts of this compound, and the N-oxides of the pyridines and their salts are active bronchial therapeutics.
    • R1为1-2C-烷氧基或完全或主要被氟取代的1-2C-烷氧基的式(Ⅰ)化合物,R2为1-7C-烷基,3-7C-环烷基或3-7C-环烷基甲基, Ar是苯基,吡啶基,被R3,R4和R5取代的苯基或被R6,R7,R8和R9取代的吡啶基,其中R3是羟基,卤素,氰基,羧基,三氟甲基,1-4C-烷基, 1-4C-烷氧基,1-4C-烷氧基羰基,1-4C-烷基羰基,1-4C-烷基羰基氧基,氨基,单或二1-4C-烷基氨基或1-4C-烷基羰基氨基,R4是氢,羟基,卤素, 氨基,三氟甲基,1-4C-烷基或1-4C-烷氧基,R5是氢,卤素,1-4C-烷基或1-4C-烷氧基,R6是羟基,卤素,氰基,羧基,1-4C-烷基, 1-4C-烷氧基,1-4C-烷氧基羰基或氨基,R7是氢,卤素,氨基或1-4C-烷基,R8是氢或卤素,R9是氢或卤素,该化合物的盐和N- 吡啶及其盐的氧化物是活性支气管炎。
    • 5. 发明申请
    • FLUOROALKOXY-SUBSTITUTED BENZAMIDES AND THEIR USE AS CYCLIC NUCLEOTIDE PHOSPHODIESTERASE INHIBITORS
    • 氟烷氧基取代的苯甲酰胺及其作为环核苷酸磷酸二酯酶抑制剂的用途
    • WO1995001338A1
    • 1995-01-12
    • PCT/EP1994002169
    • 1994-07-02
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBHAMSCHLER, Hermann
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBHFLOCKERZI, DieterGUTTERER, BeateHATZELMANN, ArminSCHUDT, ChristianBEUME, RolfKILIAN, UlrichWOLF, Horst, P., O.
    • C07D213/75
    • C07D213/75C07C235/56
    • Compounds of formula (I), in which one of the substituents R1 or R2 stands for hydrogen, 1-6C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, benzyloxy or totally or partially fluorine-substituted 1-4C-alkoxy, and the other stands for totally or partially fluorine-substituted 1-4C-alkoxy, and R3 stands for phenyl, pyridyl, R31, R32 and R33- substituted phenyl or R34, R35, R36 and R37- substituted pyridyl, in which R31 stands for hydroxy, halogen, cyano, carboxyl, trifluoromethyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, amino, mono- or di-1-4C-alkylamino or 1-4C-alkylcarbonylamino; R32 stands for hydrogen, hydroxy, halogen, amino, trifluoromethyl, 1-4C-alkyl or 1-4C-alkoxy; R33 stands for hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy; R34 stands for hydroxy, halogen, cyano, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl or amino; R35 stands for hydrogen, halogen, amino or 1-4C-alkyl; R36 stands for hydrogen or halogen; and R37 stands for hydrogen or halogen. These compounds constitute new effective bronchotherapeutic drugs.
    • 式(I)的化合物,其中取代基R1和R2是氢,1-6C-烷氧基,3-7C-环,3-7C-环cycloalkylmethoxy,苄氧基或完全或部分氟取代的1-4C-烷氧基之一,并且 完全或部分氟取代的1-4C-烷氧基,和R 3是苯基,吡啶基等手段,由R31,R32和R33表示取代的苯基或R34,R35,R36和R37取代的吡啶基,其中R31是羟基,卤素,氰基,羧基 甲基,三氟甲基,1-4C-烷基,1-4C-烷氧基,1-4C-烷氧基羰基,1-4C-烷基羰基,1-4C-烷基羰基氧基,氨基,单或二C 1-4 - 烷基氨基或1-4C- 烷基羰基氨基,R32是氢,羟基,卤素,氨基,三氟甲基,1-4C-烷基或1-4C-烷氧基,R33是氢,卤素,1-4C-烷基或1-4C-烷氧基,R34羟基,卤素,氰基,羧基 ,1-4C-烷基,1-4C-烷氧基,1-4C-烷氧基羰基或氨基,R35是氢,卤素,氨基或1-4C-烷基,R36是氢或卤素和R 37是氢或卤素床 eutet是新的有效治疗支气管。