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113 条记录 (耗时 0.064 秒)

    Piperidine-indole compounds having 5-HT.sub.6 affinity
    11.
    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

    申请人： Abdelmalik Slassi ,  Louise Edwards ,  Anne O'Brien ,  Tao Xin ,  Ashok Tehim

    发明人： Abdelmalik Slassi ,  Louise Edwards ,  Anne O'Brien ,  Tao Xin ,  Ashok Tehim

    IPC分类号： A61K31/454 ,  C07D401/04 ,  A61K31/445

    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
    12.
    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

    申请人： Louise Edwards ,  Abdelmalik Slassi ,  Ashok Tehim ,  Tao Xin

    发明人： Louise Edwards ,  Abdelmalik Slassi ,  Ashok Tehim ,  Tao Xin

    IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D221/02

    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
    13.
    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

    申请人： Louise Edwards ,  Abdelmalik Slassi ,  Ashok Tehim ,  Tao Xin

    发明人： Louise Edwards ,  Abdelmalik Slassi ,  Ashok Tehim ,  Tao Xin

    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。

    Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity
    14.
    发明授权
    Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity 有权
    具有5-HT 6受体亲和力的双环哌啶和哌嗪化合物

    公开(公告)号：US06251893B1

    公开(公告)日：2001-06-26

    申请号：US09156495

    申请日：1998-09-18

    申请人： Shawn Maddaford ,  Tao Xin ,  Abdelmalik Slassi ,  Ashok Tehim ,  Qi Qiao

    发明人： Shawn Maddaford ,  Tao Xin ,  Abdelmalik Slassi ,  Ashok Tehim ,  Qi Qiao

    IPC分类号： A61K3155

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, halo, OH, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl and others; R5 is selected from the group consisting of SO2Ar, C(O)Ar, Ar and CH2Ar; R6 and R7 are independently selected from the group consisting of H, C1-6alkyl, optionally substituted phenyl and optionally substituted benzyl; ————— represents a single or double bond; n is selected from an integer of from 1-3; X is selected from the group consisting of CR17 and N; 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 aromatic group selected from the group consisting of phenyl, pyridyl, thienyl, furanyl, naphthyl, quinolyl and isoquinolyl; R16 is selected from the group consisting of H, C1-6alkyl and benzyl. 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，其具有以下通式：其中R 1，R 2，R 3和R 4独立地选自H，卤素，OH，C 1-6烷基，C 1-6烷氧基，C 2 C 1-6烷基，C 2-6炔基，C 3-7环烷基等; R 5选自SO 2 Ar，C（O）Ar，Ar和CH 2 Ar; R 6和R 7独立地选自H，C 1-6烷基， 任选取代的苯基和任选取代的苄基; -----表示单键或双键; n选自1-3的整数; X选自CR 17和N; Z选自 由C，CH和N组成，条件是当-----是双键时，Z是C，当-----是单键时，Z选自CH和N; Ar是任选取代的芳族 基团，其选自苯基，吡啶基，噻吩基，呋喃基，萘基，喹啉基和异喹啉基; R16选自H，C1-6烷基 1和苄基。还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的指征的用途，例如精神分裂症。