专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06916818B2 Azaindoles having serotonin receptor affinity 失效
标题翻译：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。

2. 发明授权

US06380242B1 N-alkylamino-indoles for the treatment of migraine 失效
标题翻译： N-烷基氨基 - 吲哚用于治疗偏头痛
公开(公告)号：US06380242B1
公开(公告)日：2002-04-30
申请号：US09469327
申请日：1999-12-22
申请人： Jalaj Arora , Louise Edwards , Methvin Isaac , Anne O'Brien , Abdelmalik Slassi , Ashok Tehim , Tao Xin
发明人： Jalaj Arora , Louise Edwards , Methvin Isaac , Anne O'Brien , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC分类号： A61K31382
CPC分类号： A61K31/415
摘要： The present invention is directed to compounds useful in the treatment of migraine which have the general formula (II).
摘要翻译：本发明涉及可用于治疗具有通式（II）的偏头痛的化合物。

3. 发明授权

US06191141B1 Azaindoles having serotonin receptor affinity 有权
标题翻译：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。

4. 发明申请

US20120302596A1 AZAINDOLES HAVING SEROTONIN RECEPTOR AFFINITY 审中-公开
标题翻译：具有丝氨酸蛋白酶受体亲和力的阿糖胞苷
公开(公告)号：US20120302596A1
公开(公告)日：2012-11-29
申请号：US13409940
申请日：2012-03-01
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 , A61K31/4375 , A61P25/00 , A61P25/24 , A61P25/16 , A61P25/28 , C07D471/04 , A61P25/18
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。

5. 发明申请

US20080004307A1 Azaindoles Having Serotonin Receptor Affinity 失效
标题翻译：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。

6. 发明授权

US07268127B2 Azaindoles having serotonin receptor affinity 失效
标题翻译：阿魏醇具有5-羟色胺受体亲和力
公开(公告)号：US07268127B2
公开(公告)日：2007-09-11
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： A01N43/00 , A01N43/58 , A61K31/55 , C07D241/36 , C07D471/00
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 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。}

7. 发明授权

US6133287A Piperidine-indole compounds having 5-HT.sub.6 affinity 失效
标题翻译：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。

8. 发明申请

US20050239788A1 Azaindoles having serotonin receptor affinity 失效
标题翻译：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。

9. 发明授权

US06635639B2 Use of N-alkylamino-heterocylic compounds for the treatment of migraine 失效
标题翻译： N-烷基氨基 - 杂环化合物用于治疗偏头痛的用途
公开(公告)号：US06635639B2
公开(公告)日：2003-10-21
申请号：US10073130
申请日：2002-02-13
申请人： Jalaj Arora , Louise Edwards , Methvin Issac , Anne O'Brien , Abdelmalik Slassi , Ashok Tehim , Tao Xin
发明人： Jalaj Arora , Louise Edwards , Methvin Issac , Anne O'Brien , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC分类号： A61K315377
CPC分类号： A61K31/415
摘要： Described are compounds having formula I or II: wherein: X is N, and Ak represents a C1-3 alkylene chain; and a salt, solvate or prodrug thereof.
摘要翻译：描述的是具有式I或II的化合物：其中：X为N，Ak为C 1-3亚烷基链;及其盐，溶剂合物或前药。

10. 发明授权

US6100291A Pyrrolidine-indole compounds having 5-HT.sub.6 affinity 失效
标题翻译：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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式