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    Azaindoles having serotonin receptor affinity
    1.
    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：US06916818B2

    公开(公告)日：2005-07-12

    申请号：US10739302

    申请日：2003-12-19

    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： A61K31/498 ,  A61P25/18 ,  A61P25/24 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D401/04 ,  A61K31/496

    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： 本文描述的是具有对具有通式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，B D或E之一为N原子，其余为CH基团; 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，条件是每次只有一个双键; n为1-3的整数; Z选自C，CH和N，条件是当 - 双键，Z为C且当 - 为单键时，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。

    Azaindoles having serotonin receptor affinity
    3.
    发明授权
    Azaindoles having serotonin receptor affinity 有权
    阿魏醇具有5-羟色胺受体亲和力

    公开(公告)号：US06191141B1

    公开(公告)日：2001-02-20

    申请号：US09373212

    申请日：1999-08-12

    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： C07D47104

    CPC分类号： C07D471/04 ,  A61K31/437

    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 ; R1选自SO2Ar，C（O）Ar，CH2Ar和Ar; R2，R3和R4独立地选自H和烷基; -----表示单键或双键， 条件是每次环中只有一个双键; n是1-3的整数; Z选自C，CH和N，条件是当-----是 双键，Z是C，当-----是单键时，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 SO2Ar。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，如精神分裂症的适应症的用途。

    Azaindoles Having Serotonin Receptor Affinity
    5.
    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

    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： A61K31/437 ,  A61P25/00 ,  C07D471/04

    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＆gt;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
    7.
    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
    8.
    发明申请
    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：US20050239788A1

    公开(公告)日：2005-10-27

    申请号：US11165122

    申请日：2005-06-24

    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： A61K31/498 ,  A61P25/18 ,  A61P25/24 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

    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： 本文描述的是具有对具有通式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，B D或E之一为N原子，其余为CH基团; 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; 代表单键或双键，条件是每次只有一个双键; n为1-3的整数; Z选自C，CH和N，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。

    Pyrrolidine-indole compounds having 5-HT.sub.6 affinity
    10.
    发明授权
    Pyrrolidine-indole compounds having 5-HT.sub.6 affinity 失效
    具有5-HT 6亲和力的吡咯烷 - 吲哚化合物

    公开(公告)号：US6100291A

    公开(公告)日：2000-08-08

    申请号：US39269

    申请日：1998-03-16

    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： C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  A61K31/404

    CPC分类号： C07D403/06 ,  C07D405/14 ,  C07D409/14

    摘要： Described herein are compounds with affinity for the 5-HT.sub.6 receptor, which have the general formula: ##STR1## 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;R.sup.3 is selected from the group consisting of COR.sup.5, SO.sub.2 R.sup.5, CONHC.sub.1-4 alkyl and C(S)SR.sup.6 ;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.sup.4d is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.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--; andR.sup.6 is selected from C.sub.1-4 alkyl, allyl, propargyl and optionally substituted benzyl wherein the benzyl group is optionally substituted with 1-4 substituents selected from cyano, C.sub.1-4 alkyl and halo.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; R3选自COR5，SO2R5，CONHC1-4烷基和C（S）SR6; 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; R5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烷氧羰基和C 1-4烷基S- 并且R 6选自C 1-4烷基，烯丙基，炔丙基和任选取代的苄基，其中苄基任选被1-4个选自氰基，C 1-4烷基和卤素的取代基取代。 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。