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1. 发明授权

US06384225B1 Intermediates in the preparation of substituted chroman derivatives 失效
标题翻译：中间体制备取代的苯并二氢吡喃衍生物
公开(公告)号：US06384225B1
公开(公告)日：2002-05-07
申请号：US09653552
申请日：2000-08-31
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： C07D31158
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 the 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, C114 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的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 -C 1-6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杂原子的杂芳环选自N，O和S，并且其可以是单取代或二取代; n是0-4; R 9是C 1 -C 6烷基，C 3 -C 6环烷基，OCF 3，OCHF 2，OCH 2 F，卤素，CONR 6 R 7，CN，CF 3， OH，C114 C6烷氧基，NR6R7，SO3CH3，SO3CF3，SO2NR6R7，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，其中取代基为（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。

2. 发明授权

US06410532B1 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.

3. 发明授权

US06387899B1 Substituted chroman derivatives 失效
标题翻译：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。

4. 发明授权

US06313118B1 Substituted 1,2,3,4-tetrahydronaphthalene derivatives 失效
标题翻译：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。

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