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    • 7. 发明申请
    • SUBSTITUTED DIHYDROBENZOFURANS AS PDE INHIBITORS
    • 替代二氢苯并呋喃作为PDE抑制剂
    • WO1998022453A1
    • 1998-05-28
    • PCT/EP1997006248
    • 1997-11-11
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBHMARTIN, ThomasULRICH, Wolf-Rüdiger
    • BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBHAMSCHLER, HermannBÄR, ThomasFLOCKERZI, DieterGUTTERER, BeateTHIBAUT, UlrichHATZELMANN, ArminBOSS, HildegardBEUME, RolfKLEY, Hans-PeterHÄFNER, Dietrich
    • C07D307/94
    • C07D405/04C07D307/94C07D407/04C07D409/04C07D493/10C07F9/65517
    • Compounds of formula (I) in which R1 is 1-6C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, benzyloxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R2 is 1-4C-alkyl and R3 is hydrogen or 1-4C-alkyl, or in which R2 and R3, together and including the two carbon atoms to which they are bonded, are a spiro-linked 5-, 6- or 7-membered hydrocarbon ring, if desired interrupted by an oxygen atom or an imino (-NH-) group, R4 is hydrogen, hydroxyl, nitro, cyano, carboxyl, 1-4C-alkoxy or 1-4C-alkoxycarbonyl, A is B, -CH(R5)- or > C = N-R6, where B is oxygen (-O-), imino (-NH-), sulfinyl (-S(O)-), sulfonyl, (-S(O)2-) or carbonylimino (-C(O)NH-) and R5 is carboxyl, 1-4C-alkoxycarbonyl, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, hydroxylaminocarbonyl (-C(O)NHOH), 1-4C-alkoxyaminocarbonyl or a radical of formula (a) where R51 is hydrogen, 1-4C-alkyl or aryl and R52 is hydrogen, 1-4C-alkyl or aryl, where aryl is a phenyl, pyridyl, benzyl or phenethyl radical which can be unsubstituted or mono- or disubstituted by hydroxyl, 1-4C-alkoxy, halogen, amino, cyano or nitro, R6 is hydroxy or 1-4C-alkylcarbonyloxy, and the salts of these compounds are efficacious PDE inhibitors.
    • R 1为1-6C-烷氧基,3-7C-环烷氧基,3-7C-环烷基甲氧基,苄氧基或完全或主要被氟取代的1-4C-烷氧基的式(Ⅰ)化合物,R2为1-4C- 烷基和R 3是氢或1-4C-烷基,或其中R 2和R 3一起并包括它们所键合的两个碳原子是螺连接的5-,6-或7-元烃环,如果 需要被氧原子或亚氨基(-NH-)基团中断,R4是氢,羟基,硝基,氰基,羧基,1-4C-烷氧基或1-4C-烷氧基羰基,A是B,-CH(R5) - 或 - > C = N-R6,其中B是氧(-O-),亚氨基(-NH-),亚磺酰基(-S(O) - ),磺酰基,(-S(O)2-)或羰基亚氨基( - C(O)NH-),R 5是羧基,1-4C-烷氧基羰基,氨基羰基,单或二1-4C-烷基氨基羰基,羟基氨基羰基(-C(O)NHOH),1-4C-烷氧基氨基羰基或 式(a)其中R51是氢,1-4C-烷基或芳基,R52是氢,1-4C-烷基或芳基,其中芳基是苯基,吡啶基,苄基或苯乙基 其可以是未取代的或被羟基,1-4C-烷氧基,卤素,氨基,氰基或硝基单或二取代,R6是羟基或1-4C-烷基羰氧基,并且这些化合物的盐是有效的PDE抑制剂。