Azaindoles Having Serotonin Receptor Affinity
    53.
    发明申请
    Azaindoles Having Serotonin Receptor Affinity 失效
    具有血清素受体亲和力的阿魏酸

    公开(公告)号:US20080004307A1

    公开(公告)日:2008-01-03

    申请号:US11835325

    申请日:2007-08-07

    CPC分类号: C07D471/04 C07D519/00

    摘要: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

    摘要翻译: 本文描述的是对5-HT 6受体具有亲和力的化合物,其具有通式I:其中A,B,D,E,R 1至R“ > 3>和n。 还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症的用途,例如精神分裂症。

    Piperidine-indole compounds having 5-HT.sub.6 affinity
    55.
    发明授权
    Piperidine-indole compounds having 5-HT.sub.6 affinity 失效
    具有5-HT 6亲和力的哌啶 - 吲哚化合物

    公开(公告)号:US6133287A

    公开(公告)日:2000-10-17

    申请号:US46669

    申请日:1998-03-24

    CPC分类号: C07D401/04 A61K31/454

    摘要: Described herein are compounds with affinity for the 5-HT.sub.6 receptor, which have the general formula: wherein:R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 is selected from the group consisting of H, C.sub.1-4 alkyl and benzyl;-- -- -- represents a single or double bond;R.sup.3 is selected from the group consisting of COR.sup.5 and SO.sub.2 R.sup.5 ;R.sup.4a is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sup.4b is selected from the group consisting of H, hydroxy, halo, C.sub.3-7 cycloalkyloxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl;R.sup.4c is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sub.4d is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sup.5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C.sub.1-4 alkoxy, C.sub.1-4 alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylS--. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT.sub.6 receptor is implicated, such as schizophrenia.

    摘要翻译: 本文描述的是对5-HT 6受体具有亲和性的化合物,其具有以下通式:其中:R 1选自H和C 1-4烷基; R 2选自H,C 1-4烷基和苄基; - - - 表示单键或双键; R3选自COR5和SO2R5; R 4a选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R4b选自H,羟基,卤素,C 3-7环烷氧基,C 1-4烷氧基,C 1-4烷基,苄氧基,苯氧基,三氟甲基,三氟甲氧基和乙烯基; R4c选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; R4d选自H,OH,卤素,C 1-4烷基和C 1-4烷氧基; 并且R 5选自苯基,吡啶基,噻吩基,喹啉基和萘基,其任选被1-4个选自C 1-4烷氧基,C 1-4烷基,卤素,硝基,三氟甲基,三氟甲氧基,1,2-亚甲二氧基 ,C 1-4烷基羰基,C 1-4烷氧基羰基和C 1-4烷基。 还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症如精神分裂症的用途。

    Azaindoles having serotonin receptor affinity
    56.
    发明授权
    Azaindoles having serotonin receptor affinity 失效
    阿魏醇具有5-羟色胺受体亲和力

    公开(公告)号:US08148394B2

    公开(公告)日:2012-04-03

    申请号:US11835325

    申请日:2007-08-07

    CPC分类号: C07D471/04 C07D519/00

    摘要: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

    摘要翻译: 本文描述的是对5-HT 6受体具有亲和力的化合物,其具有通式I:其中A,B,D,E,R 1至R 3和n如本文所述。 还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症如精神分裂症的用途。

    Azaindoles having serotonin receptor affinity
    57.
    发明授权
    Azaindoles having serotonin receptor affinity 失效
    阿魏醇具有5-羟色胺受体亲和力

    公开(公告)号:US06686374B1

    公开(公告)日:2004-02-03

    申请号:US09636592

    申请日:2000-08-10

    IPC分类号: C07D40104

    CPC分类号: C07D471/04 C07D519/00

    摘要: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein: R represents a group of Formula II or Formula III; one of A, B D or E is a N atom, the remainder being CH groups; R1 is selected from the group consisting of SO2Ar, C(O)Ar, CH2Ar and Ar; R2, R3 and R4 are independently selected from the group consisting of H and alkyl; represents a single or double bond, with the proviso that there is only one double bond in the ring at a time; n is an integer of from 1-3; Z is selected from the group consisting of C, CH and N, provided that when is a double bond, Z is C and when is a single bond, Z is selected from CH and N; Ar is an optionally substituted aryl group; with the proviso that when R is a group of Formula II, R1 is SO2Ar. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

    摘要翻译: 本文描述的是对具有通式I的5-HT 6受体具有亲和性的化合物:其中:R代表式II或式III的基团; A,BD或E之一是N原子,其余是CH基 ; R 1选自SO 2 Ar,C(O)Ar,CH 2 Ar和Ar; R 2,R 3和R 4独立地选自H和烷基;表示单键或双键,条件是 一次在环中只有一个双键; n是1-3的整数; Z选自C,CH和N,条件是当双键,Z是C并且是单一时 键,Z选自CH和N; Ar是任选取代的芳基;条件是当R是式II的基团时,R 1是SO 2 Ar。还描述了这些化合物作为药物治疗适应症的用途,其中抑制 的5-HT6受体是牵连的,如精神分裂症。