Substituted chroman derivatives
    7.
    发明授权
    Substituted chroman derivatives 失效
    取代的苯并二氢吡喃衍生物

    公开(公告)号:US07384943B2

    公开(公告)日:2008-06-10

    申请号:US11447589

    申请日:2006-06-05

    IPC分类号: A61K31/496 C07D407/04

    摘要: The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; 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 cycoalkyl or (CH2)n-aryl, wherein aryl is a heteromatic 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 racemates 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.

    摘要翻译: 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,其中X是N; 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 1,R 2,R 2,R 2, 2是H或C 1 -C 6烷基; R 1是H,C 1 -C 6烷基或C 3 -C 6烷基或C 3 -C 6烷基, SUB>环烷基; R 3是C 1 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基, 环烷基或(CH 2)n - 芳基,其中芳基是含有一个或两个选自N,O和S的杂原子的异构环,其可以是单或二 被R 4和/或R 5取代; n为0-4; 作为(R) - 对映异构体,(S) - 对映异构体或游离碱或其药学上可接受的盐或溶剂化物形式的外消旋物,其制备方法,含有所述治疗活性化合物的药物组合物和所述活性成分 化合物。

    Substituted chroman derivatives
    8.
    发明授权
    Substituted chroman derivatives 失效
    取代的苯并二氢吡喃衍生物

    公开(公告)号:US06479497B1

    公开(公告)日:2002-11-12

    申请号:US09171570

    申请日:1998-10-21

    IPC分类号: A61K31496

    摘要: The present invention relates to new new piperidyl or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the 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.

    摘要翻译: 本发明涉及新的具有式(I)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NR2CH2,CH2NR2,NR2CO,CONR2,NR2SO2或NR2CONR2,其中R2是H 或C 1 -C 6烷基; R 1是H,C 1 -C 6烷基或C 3 -C 6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,其中芳基是苯基或杂芳环, 两个选自N,O和S的杂原子,可以被R4和/或R5单取代或二取代; n为0-4;作为(R) - 对映异构体,(S) - 对映异构体或 形式的游离碱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和所述活性化合物的用途。

    Substituted chroman derivatives
    10.
    发明授权
    Substituted chroman derivatives 失效
    取代的色原衍生物

    公开(公告)号:US07056921B2

    公开(公告)日:2006-06-06

    申请号:US10714577

    申请日:2003-11-13

    摘要: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the 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.

    摘要翻译: 本发明涉及新的具有式(I)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 1,R 2,R 2,R 2, 2是H或C 1 -C 6烷基; R 1是H,C 1 -C 6烷基或C 3 -C 6烷基或C 3 -C 6烷基, SUB>环烷基; R 3是C 1 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基, 环烷基或(CH 2 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的杂原子的杂芳环,并且其可以是单 - 或被R 4和/或R 5二取代的二价基团。 n为0-4; 作为(R) - 对映异构体,(S) - 对映异构体或游离碱或其药学上可接受的盐或溶剂合物形式的外消旋体,其制备方法,含有所述治疗活性化合物的药物组合物和所述 活性化合物。