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    • 10. 发明授权
    • SUBSTITUTED CHROMAN DERIVATIVES
    • 取代的色素衍生物
    • EP1025095B1
    • 2003-11-26
    • EP98944377.5
    • 1998-09-09
    • AstraZeneca AB
    • BERG, StefanNYLÖF, MartinROSS, SvanteTHORBERG, Seth-Olov
    • C07D311/58A61K31/495A61K31/535
    • C07D405/12C07D311/58C07D407/12
    • The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compounds having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 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 with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
    • 本发明涉及具有式(I)的新的哌啶基或哌嗪基取代的二氢-2H-1-苯并吡喃衍生物化合物,其中X是N或CH; Y是NR 2 CH 2,CH 2 NR 2,NR 2 CO,CONR 2,NR 2 SO 2或NR 2 CONR 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的杂原子的杂芳族环,并且其可以单 - 或二 - 取代 R4和/或R5; 并且n是0-4; 作为(R) - 对映异构体,(S) - 对映异构体或游离碱形式的外消旋体或其药学上可接受的盐或溶剂合物,其制备方法,含有所述治疗活性化合物的药物组合物以及所述 活性化合物。