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公开(公告)号:US06562809B1
公开(公告)日:2003-05-13
申请号:US09156496
申请日:1998-09-18
申请人: Abdelmalik Slassi , Tao Xin , Louise Edwards , Ashok Tehim
发明人: Abdelmalik Slassi , Tao Xin , Louise Edwards , Ashok Tehim
IPC分类号: A61K3155
CPC分类号: C07D471/04 , C07D487/04
摘要: Described herein are compounds selective for a 5-HT1D receptor, which have the general formula:
摘要翻译: 本文描述了对具有通式的5-HT1D受体选择性的化合物
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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。
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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>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。
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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>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。
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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。
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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。
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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。
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公开(公告)号:US20090005433A1
公开(公告)日:2009-01-01
申请号:US11610864
申请日:2006-12-14
申请人: Guy A Higgins , Methvin Issac , Abdelmalik Slassi , Tao Xin
发明人: Guy A Higgins , Methvin Issac , Abdelmalik Slassi , Tao Xin
IPC分类号: A61K31/381 , C07C233/00 , A61K31/16 , C07D333/22
CPC分类号: C07D333/16 , C07C237/06 , C07C237/22 , C07C271/22 , C07C311/06
摘要: Compounds of Formula I are useful in the treatment of epilepsy, neuropathic pain, acute and chronic inflammatory pain, migraine, tardive dyskinesia and other related CNS disorders. wherein: A and R1 to R8 are defined in the specification.
摘要翻译: 式I化合物可用于治疗癫痫,神经性疼痛,急性和慢性炎症性疼痛,偏头痛,迟发性运动障碍和其他相关CNS疾病。 其中:A和R1至R8在说明书中定义。
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公开(公告)号:US07902401B2
公开(公告)日:2011-03-08
申请号:US11610864
申请日:2006-12-14
申请人: Guy A. Higgins , Methvin Issac , Abdelmalik Slassi , Tao Xin
发明人: Guy A. Higgins , Methvin Issac , Abdelmalik Slassi , Tao Xin
IPC分类号: C07C233/05 , A61K31/16
CPC分类号: C07D333/16 , C07C237/06 , C07C237/22 , C07C271/22 , C07C311/06
摘要: Compounds of Formula I are useful in the treatment of epilepsy, neuropathic pain, acute and chronic inflammatory pain, migraine, tardive dyskinesia and other related CNS disorders. wherein: A and R1 to R8 are defined in the specification.
摘要翻译: 式I化合物可用于治疗癫痫,神经性疼痛,急性和慢性炎症性疼痛,偏头痛,迟发性运动障碍和其他相关CNS疾病。 其中:A和R1至R8在说明书中定义。
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60.
公开(公告)号:US20090312306A1
公开(公告)日:2009-12-17
申请号:US12309446
申请日:2007-07-20
申请人: Guangri Sun , Methvin Isaac , Tao Xin , Higgins Guy
发明人: Guangri Sun , Methvin Isaac , Tao Xin , Higgins Guy
IPC分类号: A61K31/55 , C07D471/04 , A61P25/00
CPC分类号: C07D471/04
摘要: A compound of Formula I: and a method for treating a 5-HT2C receptor-mediated disorder in a mammal using the same.
摘要翻译: 式I的化合物:和使用其的哺乳动物中治疗5-HT 2C受体介导的病症的方法。
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