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    Substituted 1,2,3,4-tetrahydronaphthalene derivatives
    1.
    发明授权
    Substituted 1,2,3,4-tetrahydronaphthalene derivatives 失效
    取代的1,2,3,4-四氢萘衍生物

    公开(公告)号：US06313118B1

    公开(公告)日：2001-11-06

    申请号：US09171577

    申请日：1998-10-21

    申请人： Stefan Berg ,  Mats Linderberg ,  Svante Ross ,  Seth-Olov Thorberg ,  Bengt Ulff

    发明人： Stefan Berg ,  Mats Linderberg ,  Svante Ross ,  Seth-Olov Thorberg ,  Bengt Ulff

    IPC分类号： A61K31495

    CPC分类号： C07D295/192 ,  C07C237/24 ,  C07C2602/10 ,  C07D295/135 ,  C07D295/155 ,  C07D295/205

    摘要： The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 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, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, 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 thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

    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-1,2,3,4-四氢萘衍生物，其中X是N或CH; Y是NR2CH2，CH2-NR2，NR2-CO，CO-NR2或NR2SO2，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，其中芳基是苯基或含有一个或两个选自N，O和S的杂原子并且可被单取代或二取代的杂芳环是 0-4; R9是C1-C6烷基，C3-C6环烷基，OCF3，OCHF2，OCH2F，卤素，CN，CF3，OH，C1-C6烷氧基，C1-C6烷氧基-C1-C6烷基，NR6R7，SO3CH3，SO3CF3 ，SO 2 NR 6 R 7，含有一个或两个选自N和O的杂原子的未取代或取代的杂环或杂芳环，其中取代基是（C 1 -C 6）烷基; 或COR8; 其中R 6，R 7和R 8如上所定义，为游离碱形式的（R） - 对映体，（S） - 对映异构体或外消旋物或其药学上可接受的盐，其制备方法，含有所述治疗活性的药物组合物 化合物和所述活性化合物在治疗中的用途。

    Substituted chroman derivatives
    2.
    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

    申请人： Stefan Berg ,  Martin Nylöf ,  Svante Ross ,  Seth-Olov Thorberg

    发明人： Stefan Berg ,  Martin Nylöf ,  Svante Ross ,  Seth-Olov Thorberg

    IPC分类号： A61K31/497 ,  C07D403/02 ,  C07D243/06

    CPC分类号： C07D405/12 ,  C07D311/58 ,  C07D407/12

    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。

    Substituted chroman derivatives
    3.
    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：US06670359B2

    公开(公告)日：2003-12-30

    申请号：US10285743

    申请日：2002-11-01

    申请人： Stefan Berg ,  Martin Nylöf ,  Svante Ross ,  Seth-Olov Thorberg

    发明人： Stefan Berg ,  Martin Nylöf ,  Svante Ross ,  Seth-Olov Thorberg

    IPC分类号： A61K31445

    CPC分类号： C07D405/12 ,  C07D311/58 ,  C07D407/12

    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 indan derivatives
    4.
    发明授权
    Substituted indan derivatives 失效
    取代的茚满衍生物

    公开(公告)号：US06548498B1

    公开(公告)日：2003-04-15

    申请号：US09171575

    申请日：1998-10-21

    申请人： Stefan Berg ,  Lennart Florvall ,  Svante Ross ,  Seth-Olov Thorberg

    发明人： Stefan Berg ,  Lennart Florvall ,  Svante Ross ,  Seth-Olov Thorberg

    IPC分类号： C07D295135

    CPC分类号： C07D295/135 ,  C07D295/155

    摘要： The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives of the formula I as (R)-enantiomers, (S)-enantiomers, or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof. The present invention further relates to a process for the preparation of the compounds, to pharmaceutical compositions containing the compounds and to methods of treatment of 5-hydroxytryptamine-mediated disorders comprising administering the compounds.

    摘要翻译： 本发明涉及式Ias（R） - 对映异构体，（S） - 对映异构体或游离碱形式的外消旋物或其药学上可接受的盐或溶剂化物的新的哌啶基或哌嗪基取代的茚满衍生物。 本发明还涉及制备所述化合物的方法，含有所述化合物的药物组合物和治疗5-羟色胺介导的病症的方法，包括给予所述化合物。

    Substituted 1,2,3,4-tetrahydronaphthalene derivatives
    5.
    发明授权
    Substituted 1,2,3,4-tetrahydronaphthalene derivatives 有权

    公开(公告)号：US06410532B1

    公开(公告)日：2002-06-25

    申请号：US09902000

    申请日：2001-07-10

    申请人： Stefan Berg ,  Mats Linderberg ,  Svante Ross ,  Seth-Olov Thorberg ,  Bengt Ulff

    发明人： Stefan Berg ,  Mats Linderberg ,  Svante Ross ,  Seth-Olov Thorberg ,  Bengt Ulff

    IPC分类号： C07D295135

    摘要： The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-6 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, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy—C1-C6 alkyl, 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 thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

    Substituted chroman derivatives
    6.
    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：US06387899B1

    公开(公告)日：2002-05-14

    申请号：US09171572

    申请日：1998-10-21

    申请人： Stefan Berg ,  Mats Linderberg ,  Svante Ross ,  Seth-Olov Thorberg ,  Bengt Ulff

    发明人： Stefan Berg ,  Mats Linderberg ,  Svante Ross ,  Seth-Olov Thorberg ,  Bengt Ulff

    IPC分类号： A61K315377

    CPC分类号： C07D311/58

    摘要： 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.

    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-3,4-二氢-2H-1-苯并吡喃衍生物，其中X是N或CH; Y是NR2CH2，CH2NR2，NR2CO，CONR2或NR2SO2，其中R2是H或C1-C6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的杂原子并可以被单取代或二取代的杂芳环; n为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环 一个或两个选自N和O的杂原子，其中取代基是（C 1 -C 6）烷基; 或COR8; 其中R 6，R 7和R 8如上所定义，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 治疗活性化合物和所述活性化合物在治疗中的用途。

    Substituted indan derivatives
    8.
    发明授权
    Substituted indan derivatives 失效
    取代的茚满衍生物

    公开(公告)号：US07439356B2

    公开(公告)日：2008-10-21

    申请号：US11543250

    申请日：2006-10-03

    申请人： Stefan Berg ,  Lennart Florvall ,  Svante Ross ,  Seth-Olov Thorberg

    发明人： Stefan Berg ,  Lennart Florvall ,  Svante Ross ,  Seth-Olov Thorberg

    IPC分类号： C07D265/30 ,  C07D295/135 ,  C07D211/26 ,  C07D295/155 ,  A61K31/495 ,  A61K31/445

    CPC分类号： C07D295/135 ,  C07D295/155

    摘要： The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C6 alkyl; 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, wherein R4 and R5 are as defined in the specification; and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, 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 in the specification. The invention further relates to a process for the preparation of the intermediates.

    摘要翻译： 本发明涉及可用于制备哌嗪基取代的茚满衍生物的式的中间体，其中Y是CONR 2，其中R 2是H或C 1 C 6 -C 6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，其中R 4和R 5定义如上所定义 在规范中; R 9是H，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 3 -C 6烷基， OCF 3，OCHF 2，OCH 2 F，卤素，CN，CF 3 N， OH，C 1 -C 6烷氧基，C 1 -C 6烷氧基-C 1 -C 6烷氧基，C 1 -C 6烷氧基，C 1 -C 6烷氧基， C 6 -C 6烷基，NR 6 R 7，SO 3 CH 3， SO 3，SO 3，CF 3，SO 2，NR 6，R 7， 含有一个或两个选自N和O的杂原子的未取代或取代的杂环或杂芳环，其中所述取代基是C 1 -C 6 -C 6烷基; 或COR 8; 其中R 6，R 7和R 8是如说明书中所定义的。 本发明还涉及制备中间体的方法。

    Substituted indan derivatives
    9.
    发明申请
    Substituted indan derivatives 失效
    取代的茚满衍生物

    公开(公告)号：US20070149545A1

    公开(公告)日：2007-06-28

    申请号：US11543250

    申请日：2006-10-03

    申请人： Stefan Berg ,  Lennart Florvall ,  Svante Ross ,  Seth-Olov Thorberg

    发明人： Stefan Berg ,  Lennart Florvall ,  Svante Ross ,  Seth-Olov Thorberg

    IPC分类号： A61K31/495 ,  C07D211/06 ,  A61K31/445 ,  C07D241/04

    CPC分类号： C07D295/135 ,  C07D295/155

    摘要： The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C6 alkyl; 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, wherein R4 and R5 are as defined in the specification; and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, 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 in the specification. The invention further relates to a process for the preparation of the intermediates.

    摘要翻译： 本发明涉及可用于制备哌嗪基取代的茚满衍生物的式的中间体，其中Y是CONR 2，其中R 2是H或C 1 C 6 -C 6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，其中R 4和R 5定义如上所定义 在规范中; R 9是H，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 3 -C 6烷基， OCF 3，OCHF 2，OCH 2 F，卤素，CN，CF 3 N， OH，C 1 -C 6烷氧基，C 1 -C 6烷氧基-C 1 -C 6烷氧基，C 1 -C 6烷氧基，C 1 -C 6烷氧基， C 6 -C 6烷基，NR 6 R 7，SO 3 CH 3， SO 3，SO 3，CF 3，SO 2，NR 6，R 7， 含有一个或两个选自N和O的杂原子的未取代或取代的杂环或杂芳环，其中所述取代基是C 1 -C 6 -C 6烷基; 或COR 8; 其中R 6，R 7和R 8是如说明书中所定义的。 本发明还涉及制备中间体的方法。