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    • 3. 发明申请
    • SUBSTITUTED PICOLINIC ACIDS, PROCESSES FOR THEIR PREPARATION, THEIR USE AND MEDICAMENTS CONTAINING THEM
    • 取代的皮质类药物,其制备方法,其使用和药物含有它们
    • WO1984004302A1
    • 1984-11-08
    • PCT/EP1983000115
    • 1983-04-27
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GESELLSCHAFT ...AMSCHLER, HermannSANDERS, KarlULRICH, Wolf-Rüdiger
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GESELLSCHAFT ...
    • C07D213/79
    • C07D213/79C07D213/81
    • Substituted picolinic acids of the general formula (I), wherein R denotes alkyl with 1 to 7 carbon atoms - but not butyl if R and R denote alkyl and X denotes NH -, cycloalkylalkyl with 3 to 7 carbon atoms in the cycloalkyl part and 1 to 4 carbon atoms in the alkylene part, phenyl or substituted phenyl with up to three substituents from the group comprising halogen, hydroxyl, alkyl with 1 to 4 carbon atoms and alkoxy with 1 to 4 carbon atoms, R denotes alkyl with 1 to 4 carbon atoms or alkenyl with 3 to 5 carbon atoms and R denotes alkyl with 1 to 4 carbon atoms or alkenyl with 3 to 5 carbon atoms, or R and R together, and including the nitrogen atom to which they are bonded, denote pyrrolidino, morpholino, piperidino, hexahydroazepino, or 1-piperazinyl which is substituted in the 4-position by R , R denotes hydrogen, alkyl with 1 to 4 carbon atoms, phenyl, benzyl or substituted phenyl with up to three substituents from the group comprising halogen, hydroxyl, alkyl with 1 to 4 carbon atoms and alkoxy with 1 to 4 carbon atoms, A denotes straight-chain or branched alkylene with 1 to 5 carbon atoms and X denotes O (oxygen) or NH, and the acid addition salts of these compounds, R , R and R not simultaneously denoting alkyl if X represents O (oxygen) and A represents ethylene, are new compounds with a hypotensive activity. Processes for the preparation of these compounds are described.
    • 通式(I)的取代的吡啶甲酸,其中R 1表示具有1至7个碳原子的烷基,但不是丁基,如果R 2和R 3表示烷基,X表示NH - ,环烷基烷基,具有3至 环烷基部分中的7个碳原子和亚烷基部分中的1至4个碳原子,苯基或取代苯基与最多三个来自卤素,羟基,具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基的取代基组成 R 2表示具有1至4个碳原子的烷基或具有3至5个碳原子的烯基,R 3表示具有1至4个碳原子的烷基或具有3至5个碳原子的链烯基,或R 2和R 包括与它们键合的氮原子表示吡咯烷子基,吗啉代,哌啶子基,六氢吖庚因或在4-位被R 4取代的1-哌嗪基,R 4表示氢, 具有1至4个碳原子的烷基,苯基,苄基或取代的苯基,其中最多三个取代基包括卤素,羟基, 具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基,A表示具有1至5个碳原子的直链或支链亚烷基,X表示O(氧)或NH,并且这些化合物的酸加成盐,R 如果X表示O(氧),A表示乙烯,则R 2和R 3不同时表示烷基,是具有降血压活性的新化合物。 描述了这些化合物的制备方法。
    • 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。
    • 9. 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。