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    5-aminoalkyl and 5-aminocarbonyl substituted indoles
    2.
    发明申请
    5-aminoalkyl and 5-aminocarbonyl substituted indoles 失效
    5-氨基烷基和5-氨基羰基取代的吲哚

    公开(公告)号：US20020169169A1

    公开(公告)日：2002-11-14

    申请号：US10097126

    申请日：2002-03-08

    Applicant: H. Lundbeck A/S

    Inventor： Kim Andersen ,  Jens Kristian Perregaard ,  Thomas Balle

    IPC: A61K031/496 ,  A61K031/454 ,  C07D417/14 ,  C07D413/14 ,  C07D43/14

    CPC classification number: C07D401/04 ,  A61K45/06 ,  C07D401/14

    Abstract: 1 The present invention relates to 5-aminoalkyl and 5-aminocarbonyl substituted indole derivatives having formula (1), wherein R1 is-(CH2)n-1-CONR10R11, -(CH2)n-CONR10R11 or (a), wherein R10 and R11 independently are selected from substituents defined herein; n is 1 to 3 and q is 2 to 5; G is N, C, or CH; Ar is phenyl optionally substituted with one or more substituents, or Ar is heterocyclic; R2, R3, R4, R5 and R6 are independently selected from substituents defined herein; m is an integer from 2-6; W is O or S; U is N or CH; Z is null(CH2)p-, p being 2 or 3, or Z is nullCHnullCHnullor 1 ,2-phenylene, or Z isnullCOCH2- or nullCSCH2-; V is O, S, CH2, or NR9; X is N, C, or CH; Y is N, C, or CH; provided at least one of X and Y is N; or a pharmaceutically acceptable acid addition salt thereof. The novel 5-substituted indoles have high affinity for null1-adrenoceptors and are considered useful for the treatment of diseases or disorders responsive to null1-adrenoceptor antagonists. Further, as the compounds are selective null1-adrenoceptor ligands they may be particularly useflul as PET or SPECT ligands.

    Abstract translation: 本发明涉及具有式（1）的5-氨基烷基和5-氨基羰基取代的吲哚衍生物，其中R1是 - （CH2）n-1-CONR10R11， - （CH2）n-CONR10R11或（a），其中R10和R11 独立地选自本文定义的取代基; n为1〜3，q为2〜5; G是N，C或CH; Ar为任选被一个或多个取代基取代的苯基，或Ar为杂环基; R2，R3，R4，R5和R6独立地选自本文定义的取代基; m是2-6的整数; W为O或S; U是N或CH; Z为 - （CH 2）p - ，p为2或3，或Z为-CH = CH-或1,2-亚苯基，或Z为-COCH2-或-CSCH2-; V是O，S，CH 2或NR 9; X是N，C或CH; Y是N，C或CH; 提供X和Y中的至少一个是N; 或其药学上可接受的酸加成盐。 新型5-取代的吲哚对α1-肾上腺素能受体具有高亲和力，并且被认为可用于治疗对α1-肾上腺素受体拮抗剂有反应的疾病或病症。 此外，由于化合物是选择性α1-肾上腺素受体配体，它们可能特别用作PET或SPECT配体

    Indole and 2,3-dihydroindole derivatives, their preparation and use
    3.
    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

    Applicant: H. Lundbeck A/S

    Inventor： Ejner Knud Moltzen ,  Jens Kristian Perregaard ,  Ivan Mikkelsen ,  Garrick Paul Smith

    IPC: A61K031/454 ,  C07D47/14

    CPC classification number: C07D405/12 ,  C07D405/14 ,  C07D409/12

    Abstract: 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.

    Abstract translation: 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。

    Serotonin 5-HT1A and dopamin D2 receptor ligands
    4.
    发明申请
    Serotonin 5-HT1A and dopamin D2 receptor ligands 审中-公开
    5-羟色胺5-HT1A和多巴胺D2受体配体

    公开(公告)号：US20030120070A1

    公开(公告)日：2003-06-26

    申请号：US10334481

    申请日：2002-12-30

    Applicant: H. Lundbeck A/S

    Inventor： Jens Kristian Perregaard ,  Ejner Kund Moltzen

    IPC: A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC classification number: C07D401/06 ,  C07D233/32 ,  C07D233/36

    Abstract: The present invention relates to a series of 4-phenylpiperazines of formula (I) 1 wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R1 is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R2-R5 are optional substituents; R9 and R10 are hydrogen, alkyl or together form an ethylene or propylene bridge, W is O or S; V is O, S, CR6R7, or NR8 wherein R6, R7, and R8 are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R6 and R7 constitute a 3-7 membered spiro ring; Z isnull(CH2)mnull; m being 2 or 3 or Z is nullCHnullCHnull; which show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders, in particular psychosis.

    Abstract translation: 本发明涉及一系列式（I）的4-苯基哌嗪，其中A是亚烷基，亚烯基，亚炔基和C 3-7亚环烷基; R 1是C 3-10烷基，烯基或炔基，环烷基（烯）基，环烷基（烯）基 - 烯（烯/炔）基，三氟甲磺酰基或烷基磺酰基，R 2 -R 5是任选的取代基; R 9和R 10是氢，烷基或一起形成乙烯或丙烯桥，W是O或S; V是O，S，CR 6 R 7或NR 8，其中R 6，R 7和R 8是氢或烷基，烯基，环烷基，环烷基烷基，任选取代的芳烷基或芳基，或R 6和R 7构成3-7元螺环; Z是 - （CH 2）m - ; m为2或3或Z为-CH = CH-; 其显示对中枢5-羟色胺5-HT1A和多巴胺D2受体的作用。 因此，新化合物可用于治疗某些精神病和神经障碍，特别是精神病。

    Indane or dihydroindole derivatives
    5.
    发明申请
    Indane or dihydroindole derivatives 失效
    茚满或二氢吲哚衍生物

    公开(公告)号：US20010051625A1

    公开(公告)日：2001-12-13

    申请号：US09915680

    申请日：2001-07-26

    Applicant: H. Lundbeck A/S

    Inventor： Jens Kristian Perregaard ,  Ivan Mikkelsen ,  Henrik Pedersen

    IPC: A61K031/496 ,  C07D413/14 ,  A61K031/454

    CPC classification number: C07D405/12 ,  C07D317/66

    Abstract: The present invention relates to substituted indane or dihydroindole compounds of 1 Formula (I), wherein A and B are independently O or S; D is an optionally substituted methylene group; X is N or optionally substituted C; and W is a spacer group. The compounds are either selective dopamine D4 ligands or they have combined effects at dopamine D4 and serotonergic receptors and/or the serotonergic transporter. These compounds are therefore useful in the treatment of certain psychiatric and neurologic disorders, including psychosis, depression and anxiety.

    Abstract translation: 本发明涉及式（I）的取代的茚满或二氢吲哚化合物，其中A和B独立地为O或S; D是任选取代的亚甲基; X为N或任选取代的C; W是间隔基。 这些化合物是选择性多巴胺D4配体，或它们在多巴胺D4和5-羟色胺能受体和/或血清素能转运体上具有组合效应。 因此，这些化合物可用于治疗某些精神和神经障碍，包括精神病，抑郁和焦虑。

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