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51. 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。

52. 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。

53. 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。}

54. 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。

55. 发明授权

US08148394B2 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：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。

56. 发明授权

US06686374B1 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：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。

57. 发明授权

US06251893B1 Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity 有权
标题翻译：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。

58. 发明申请

US20090005433A1 Fluorinated Compounds 有权
标题翻译：氟化合物
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。

59. 发明授权

US07902401B2 Fluorinated compounds 有权
标题翻译：氟化合物
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。

60. 发明申请

US20090312306A1 TETRAHYDRO-5H-PYRIDO[2,3-D]AZEPINES AS 5-HT2C LIGANDS 审中-公开
标题翻译：作为5-HT2C配体的四氢-5H-吡啶并[2,3-D]
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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