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    Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity
    1.
    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。

    Azaindoles having serotonin receptor affinity
    2.
    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
    4.
    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。

    Heterocyclic compounds for the treatment of migraine
    5.
    发明授权
    Heterocyclic compounds for the treatment of migraine 失效
    用于治疗偏头痛的杂环化合物

    公开(公告)号：US06716837B1

    公开(公告)日：2004-04-06

    申请号：US09709579

    申请日：2000-11-13

    申请人： Louise Edwards ,  Methvin Isaac ,  Shawn Maddaford ,  Abdelmalik Slassi ,  Tao Xin

    发明人： Louise Edwards ,  Methvin Isaac ,  Shawn Maddaford ,  Abdelmalik Slassi ,  Tao Xin

    IPC分类号： C07D40112

    CPC分类号： C07F7/0814 ,  C07D209/08 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

    摘要： Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c and d is at least 2 and the sum of e and f is at least 2; and salts and solvates thereof.

    摘要翻译： 本文描述了可用于治疗偏头痛的化合物，其具有以下通式：其中：W是CH基团或N原子; Z是N或C-R4; B和D独立地选自CH和N，条件是B和D中的至少一个是CH，进一步的条件是仅当W和Z都不是N时，B和D中的一个可以表示N; A是式II，III或IV的基团，使得A组含有至少1个N原子; NR 7是-NH-或-N =; 是单键或双键; 当是单键; 或者，当是双键时， 一个C原子; Y是NH，N-烷基，N-苄基或CH2基团; U和V各自表示N原子或CH基团，条件是两者不能为N; a和b独立地为0或1; c是0至3的整数; d为1〜3的整数; e为1〜2的整数; f为0〜3的整数; g为3〜6的整数，h为2〜3的整数， 使得c和d的和为至少2，e和f的和为至少2; 及其盐和溶剂合物。

    Azaindoles having serotonin receptor affinity
    6.
    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
    8.
    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。

    Azaindoles Having Serotonin Receptor Affinity
    10.
    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。