公开(公告)号：EP0888319A1

公开(公告)日：1999-01-07

申请号：EP97914727.0

申请日：1997-03-20

申请人： Astra Aktiebolag

发明人： BERG, Stefan ,  FLORVALL, Lennart ,  ROSS, Svante ,  THORBERG, Seth-Olov

IPC分类号： C07D295 ,  A61K31 ,  A61P9 ,  A61P25 ,  A61P43 ,  C07D211 ,  C07D241

CPC分类号： C07D295/096 ,  A61K31/496 ,  C07C2601/16 ,  C07C2602/10 ,  C07D211/26 ,  C07D211/34 ,  C07D241/00 ,  C07D295/135 ,  C07D295/215

摘要： New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2-NR2, NR2-CO, CO-NR2 or NR2SO2; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, where 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; as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.

摘要翻译： 具有肟基X的新的哌啶基或哌嗪基 - 取代-1,2,3,4-四氢萘衍生物为N或CH; Y为NR2CH2，CH2-NR2，NR2-CO，CO-NR2或NR2SO2; R1为H，C1- C6烷基或C3-C6环烷基; R3是C1-C6烷基，C3-C6环烷基或（CH2）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， 作为（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水合物; n为0-4; 含有这些化合物的药物制剂，该化合物在治疗5-羟色胺介导的病症中的用途，制备化合物的方法和用于制备化合物的中间体。

公开(公告)号：EP1000048A1

公开(公告)日：2000-05-17

申请号：EP98934104.5

申请日：1998-07-15

申请人： Astra Aktiebolag

发明人： BERG, Stefan ,  LINDERBERG, Mats ,  ROSS, Svante ,  THORBERG, Seth-Olov ,  ULFF, Bengt

IPC分类号： C07D295/135 ,  C07D295/155 ,  C07D211/26 ,  C07D211/34 ,  C07C237/24 ,  A61K31/495 ,  A61K31/445

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 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，其中所述取代基为（C 1 -C 6）烷基; 或COR8; 其中R 6，R 7和R 8如上所定义，为游离碱形式的（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，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。