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    • 6. 发明公开
    • SUBSTITUTED CHROMAN DERIVATIVES
    • 取代的色素衍生物
    • EP1025096A1
    • 2000-08-09
    • EP98944378.3
    • 1998-09-09
    • AstraZeneca AB
    • BERG, StefanLINDERBERG, MatsROSS, SvanteTHORBERG, Seth-OlovULFF, Bengt
    • C07D311/58A61K31/495A61K31/535
    • C07D311/58
    • The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CONR6R7, CN, CF3, OH, C1-C6 alkoxy, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.
    • 本发明涉及具有式(I)的新的哌啶基或哌嗪基取代的-3,4-二氢-2H-1-苯并吡喃衍生物,其中X是N或CH; Y是NR 2 CH 2,CH 2 NR 2,NR 2 CO,CONR 2或NR 2 SO 2,其中R 2是H或C 1 -C 6烷基; R1是H,C1-C6烷基或C3-C6环烷基; R 3是C 1 -C 6烷基,C 3 -C 6环烷基或(CH 2)n - 芳基,其中芳基是苯基或含有一个或两个选自N,O和S的杂原子并且可以是单取代或二取代的杂芳族环; n是0-4; R9是C1-C6烷基,C3-C6环烷基,OCF3,OCHF2,OCH2F,卤素,CONR6R7,CN,CF3,OH,C1-C6烷氧基,NR6R7,SO3CH3,SO3CF3,SO2NR6R7,未取代或取代的杂环或杂芳族环 一个或两个选自N和O的杂原子,其中取代基为C 1 -C 6烷基; 或COR8; (R) - 对映异构体,(S) - 对映异构体或外消旋体或其药学上可接受的盐或溶剂合物形式,其制备方法,含有所述化合物的药物组合物,其中R 6,R 7和R 8如上所定义, 治疗活性化合物以及所述活性化合物在治疗中的用途。