Piperidine, tetrahydropyridine and piperazine derivatives, their preparation and use
    2.
    发明申请
    Piperidine, tetrahydropyridine and piperazine derivatives, their preparation and use 审中-公开
    哌啶,四氢吡啶和哌嗪衍生物,其制备和用途

    公开(公告)号:US20020173512A1

    公开(公告)日:2002-11-21

    申请号:US10147950

    申请日:2002-05-16

    申请人: H. Lundbeck A/S

    摘要: A piperidine, tetrahydropyridine or piperazine derivative having formula (I), 1 any of its enantiomers or any mixture thereof, or an acid addition salt thereof, wherein B is C1-10-alkylene, C1-10-alkenylene or C1-10-alkynylene; X is nullOnull, nullSnull, or CR4R5null; and Y is nullCR6R7, nullCR6R7nullCR8R9, or CR6nullCR7null; or X and Y together form a group nullCR4nullCR5, or nullCR4nullCR5nullCR6R7null; Z is nullOnull, or nullSnull; W is N, C, or CH, and the dotted line is an optional bond; A is a bicyclic ring selected from (Ia) or (Ib) wherein E1, E2 and E3 are selected from O, S, N, NR11, C, CR12 and CHR13, and the dotted line indicates an optional bond, provided that E2 and E1 and/or E3 may not simultaneously be O, or S. The compounds of the invention are considered useful for the treatment of affective disorders, such as depression, psychosis, anxiety disorders including general anxiety disorder, panic disorder, obsessive compulsive disorder, and eating disorders.

    摘要翻译: 具有式(I)的哌啶,四氢吡啶或哌嗪衍生物,其任何对映异构体或其任何混合物或其酸加成盐,其中B为C1-10亚烷基,C1-10亚烯基或C1-10亚炔基; X是-O-,-S-或CR 4 R 5 - ; 且Y为-CR 6 R 7,-CR 6 R 7 -CR 8 R 9或CR 6 = CR 7 - ; 或X和Y一起形成-CR4 = CR5或-CR4-CR5-CR6R7-; Z是-O-或-S-; W是N,C或CH,虚线是任选的键; A是选自(Ia)或(Ib)的双环,其中E1,E2和E3选自O,S,N,NR11,C,CR12和CHR13,虚线表示任选的键,条件是E2和 E1和/或E3可能不能同时为O或S.本发明的化合物被认为可用于治疗情感障碍,例如抑郁症,精神病,焦虑症,包括一般焦虑症,恐慌症,强迫症,和强迫症 饮食失调。

    Novel indole derivatives
    3.
    发明申请
    Novel indole derivatives 审中-公开
    新型吲哚衍生物

    公开(公告)号:US20030050307A1

    公开(公告)日:2003-03-13

    申请号:US10183961

    申请日:2002-06-25

    申请人: H. Lundbeck A/S

    CPC分类号: C07D209/08

    摘要: The invention provide compounds of the formula 1 wherein X represents O or S; n is 2, 3, 4, 5, 6, 7, 8, 9 or 10; m is 2 or 3; Y represents N, C or CH; and the dotted line represents an optional bond; R1, R1null, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the description. The compounds are ligands of the 5-HT1a-receptor.

    摘要翻译: 本发明提供下式的化合物,其中X代表O或S; n为2,3,4,5,6,7,8,9或10; m为2或3; Y表示N,C或CH; 虚线表示可选的键; R1,R1',R2,R3,R4,R5,R6,R7,R8,R9,R10,R11和R12如说明书中所定义。 这些化合物是5-HT1a受体的配体。

    Novel heteroaryl derivatives, their preparation and use
    6.
    发明申请
    Novel heteroaryl derivatives, their preparation and use 审中-公开
    新型杂芳基衍生物,其制备和用途

    公开(公告)号:US20030050306A1

    公开(公告)日:2003-03-13

    申请号:US10183957

    申请日:2002-06-25

    申请人: H. Lundbeck A/S

    摘要: A heteroaryl derivative having the formula (I) 1 any of its enantiomers or any mixture thereof, wherein X is nullOnull, nullSnull, or CR4R5null; and Y is nullCR6R7; nullCR6R7nullCR8R9null, or nullCR6nullCR7; or X and Y together form a group nullCR4nullR5null, or nullCR4nullCR5nullCR6R7null; Z is nullOnull, or nullSnull; W is N, C, or CH; n is 2, 3, 4, 5, 6, 7, 8, 9 or 10; m is 2 or 3; A is O or S wherein the doted lines mean an optional bond. The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disorders, and neurological disorders such as psychosis.

    摘要翻译: 具有式(I)的任何其对映异构体或其任何混合物的杂芳基衍生物,其中X是-O - , - S-或CR 4 R 5 - ; Y为-CR6R7; -CR6R7-CR8R9-或-CR6-CR7; 或X和Y一起形成基团-CR 4 = R 5 - 或-CR 4 = CR 5 -CR 6 R 7 - ; Z是-O-或-S-; W是N,C或CH; n为2,3,4,5,6,7,8,9或10; m为2或3; A是O或S,其中点划线表示任选的键。 认为本发明的化合物可用于治疗情绪障碍,例如一般性焦虑障碍,恐慌症,强迫症,抑郁症,社交恐惧症和进食障碍以及神经障碍如精神病。

    Indole and 2,3-dihydroindole derivatives, their preparation and use
    7.
    发明申请
    Indole and 2,3-dihydroindole derivatives, their preparation and use 失效
    吲哚和2,3-二氢吲哚衍生物,其制备和用途

    公开(公告)号:US20030018050A1

    公开(公告)日:2003-01-23

    申请号:US10223046

    申请日:2002-08-16

    申请人: H. Lundbeck A/S

    IPC分类号: A61K031/454 C07D47/14

    摘要: The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) 1 or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.

    摘要翻译: 本发明涉及具有式(I)的吲哚和2,3-二氢吲哚衍生物或其任何对映体或其任何混合物或其酸加成盐,其中A,R 1,R 2,R 3,W,X ,Y和Z如说明书所述。 该化合物是有效的5-羟色胺再摄取抑制剂,具有5-HT1A受体拮抗作用。

    Piperidine, tetrahydropyridine and piperazine derivatives, their preparation and use

    公开(公告)号:US20020035113A1

    公开(公告)日:2002-03-21

    申请号:US09901585

    申请日:2001-07-09

    申请人: H. Lundbeck A/S

    摘要: A piperidine, tetrahydropyridine or piperazine derivative having formula (I), 1 any of its enantiomers or any mixture thereof, or an acid addition salt thereof, wherein B is C1-10-alkylene, C1-10-alkenylene or C1-10-alkynylene; X is nullOnull, nullSnull, or CR4R5null; and Y is nullCR6R7, nullCR6R7nullCR8R9, or CR6nullCR7null; or X and Y together form a group nullCR4nullCR5, or nullCR4nullCR5nullCR6R7null; Z is nullOnull, or nullSnull; W is N, C, or CH, and the dotted line is an optional bond; A is a bicyclic ring selected from (Ia) or (Ib) wherein E1, E2 and E3 are selected from O, S, N, NR11, C, CR12 and CHR13, and the dotted line indicates an optional bond, provided that E2 and E1 and/or E3 may not simultaneously be O, or S. The compounds of the invention are considered useful for the treatment of affective disorders, such as depression, psychosis, anxiety disorders including general anxiety disorder, panic disorder, obsessive compulsive disorder, and eating disorders.