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61. 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。

62. 发明申请

US20110212957A1 INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF 失效
标题翻译：伊佐唑，苯并噻唑和苯并噻唑及其制备及用途
公开(公告)号：US20110212957A1
公开(公告)日：2011-09-01
申请号：US13103512
申请日：2011-05-09
申请人： Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
发明人： Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
IPC分类号： A61K31/5377 , C07D453/02 , A61K31/439 , A61P25/18 , A61P25/00 , A61P25/28
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本发明一般涉及烟碱乙酰胆碱受体（nAChR）的配体领域，nAChR的活化以及与缺陷或功能不良的烟碱乙酰胆碱受体，特别是脑的疾病相关的疾病状况的治疗。此外，本发明涉及作为α7nAChR亚型的配体的新化合物（吲唑和苯并噻唑），制备这些化合物的方法，含有这些化合物的组合物及其使用方法。

63. 发明授权

US07700630B2 Heterocyclic compounds, methods for the preparation thereof, and uses thereof 失效
标题翻译：杂环化合物，其制备方法及其用途
公开(公告)号：US07700630B2
公开(公告)日：2010-04-20
申请号：US11783193
申请日：2007-04-06
申请人： Brian Herbert , Wenge Xie , Truc Minh Nguyen , Allen T Hopper , Ashok Tehim
发明人： Brian Herbert , Wenge Xie , Truc Minh Nguyen , Allen T Hopper , Ashok Tehim
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/08
摘要： The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.
摘要翻译：本发明的化合物具有式I：其中A，R 3，R 4如本文所定义，可用作烟碱受体的配体。

64. 发明申请

US20100029629A1 ACYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY 审中-公开
标题翻译：具有5-HT6受体亲和力的化合物
公开(公告)号：US20100029629A1
公开(公告)日：2010-02-04
申请号：US12502147
申请日：2009-07-13
申请人： Richard Conticello , Robert Dunn , Ashok Tehim , Wenge Xie
发明人： Richard Conticello , Robert Dunn , Ashok Tehim , Wenge Xie
IPC分类号： A61K31/538 , C07D471/02 , A61K31/437 , A61P25/28 , A61P25/18 , A61P25/00
CPC分类号： C07D471/04 , C07D513/04
摘要： The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, Q, G, Ar, m, and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本公开提供对式（I）的5-HT 6受体具有亲和力的化合物：其中R 1，R 2，R 5，Q，G，Ar，m和n如本文所定义。本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。

65. 发明申请

US20090105215A1 Heterocyclic compounds, methods for the preparation thereof, and uses thereof 失效
标题翻译：杂环化合物，其制备方法及其用途
公开(公告)号：US20090105215A1
公开(公告)日：2009-04-23
申请号：US11783193
申请日：2007-04-06
申请人： Brian Herbert , Wenge Xie , Truc Minh Nguyen , Allen T. Hopper , Ashok Tehim
发明人： Brian Herbert , Wenge Xie , Truc Minh Nguyen , Allen T. Hopper , Ashok Tehim
IPC分类号： C07D401/04 , A61K31/444 , A61K31/538 , C07D265/36 , C07D279/18 , A61K31/5415 , A61K31/497 , A61K31/535 , C07D413/14 , A61K31/541 , C07D417/14 , C07D243/08 , A61K31/551 , A61K31/553 , C07D281/04 , C07D471/18 , A61K31/44 , A61P25/28 , A61P25/32 , A61P25/00 , A61P25/30 , A61P25/18 , A61P29/00
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/08
摘要： The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.
摘要翻译：本发明的化合物具有式I：其中A，R 3，R 4如本文所定义，可用作烟碱受体的配体。

66. 发明申请

US20080287484A1 Neurotrophin antagonist compositions 审中-公开
标题翻译：神经营养因子拮抗剂组合物
公开(公告)号：US20080287484A1
公开(公告)日：2008-11-20
申请号：US11905406
申请日：2007-09-28
申请人： Ashok Tehim , Xiannong Chen
发明人： Ashok Tehim , Xiannong Chen
IPC分类号： A61K31/473
CPC分类号： C07D221/14 , A61K31/473 , A61K31/4738 , C07D401/04 , C07D401/06 , C07D405/06
摘要： A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and the other is selected from carboxy, carboxy-loweralkyl and loweralkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S—, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, loweralkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described.The compositions are useful to inhibit undesirable neurotrophin-mediated activity such as the neurite outgrowth that occurs in some neurodegenerative disease states.
摘要翻译：一种药物组合物，其包含式I化合物，其中R 1选自烷基，芳基 - 低级烷基，杂环 - 低级烷基，低级烷基 - 碳酸酯; 任选取代的氨基; 苯并咪唑-2-基; 任选取代的苯基; 低级烷基 - （R 5）（R 6）其中R 5和R 6中的一个选自H 另一个选自羧基，羧基 - 低级烷基和低级烷氧基羰基; NHCH 2 CH 2 OX其中X表示体内可水解的酯; R 2和R 3独立地选自H，NO 2，卤素，二（低级烷基）氨基，氰基，C（O） OH，苯基-S-，低级烷基和Z（O）OR 7其中Z选自C和S，R 7选自H，低级烷基氨基和芳基氨基; 或其药学上可接受的盐或某些体内可水解的酯或酰胺，以有效抑制神经营养因子介导的活性的量和合适的载体。该组合物可用于抑制不期望的神经营养因子介导的活性，例如在一些神经变性疾病状态中发生的神经突生长。

67. 发明申请

US20080154037A1 INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF 审中-公开
标题翻译：伊佐唑，苯并噻唑和苯并噻唑及其制备及用途
公开(公告)号：US20080154037A1
公开(公告)日：2008-06-26
申请号：US12032068
申请日：2008-02-15
申请人： Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
发明人： Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本发明一般涉及烟碱乙酰胆碱受体（nAChR）的配体领域，nAChR的活化以及与缺陷或功能不良的烟碱乙酰胆碱受体，特别是脑的疾病相关的疾病状况的治疗。此外，本发明涉及作为α7nAChR亚型的配体的新化合物（吲唑和苯并噻唑），制备这些化合物的方法，含有这些化合物的组合物及其使用方法。

68. 发明申请

US20050234095A1 Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof 审中-公开
标题翻译：吲唑，苯并噻唑，苯并异噻唑，苯并异恶唑及其制备和用途
公开(公告)号：US20050234095A1
公开(公告)日：2005-10-20
申请号：US11089533
申请日：2005-03-25
申请人： Wenge Xie , Brian Herbert , Richard Schumacher , Truc Nguyen , Jianguo Ma , Carla Gauss , Ashok Tehim
发明人： Wenge Xie , Brian Herbert , Richard Schumacher , Truc Nguyen , Jianguo Ma , Carla Gauss , Ashok Tehim
IPC分类号： A61K31/439 , A61K31/4745 , C07D453/02
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：本发明一般涉及烟碱乙酰胆碱受体（nACh受体）的配体领域，nACh受体的活化以及与缺陷或功能异常的烟碱乙酰胆碱受体，特别是脑的疾病相关的疾病状态的治疗。此外，本发明涉及作为α7nACh受体亚型的配体的新化合物（例如吲唑和苯并噻唑），制备这些化合物的方法，含有这些化合物的组合物及其使用方法。

69. 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。

70. 发明授权

US06667336B2 GlyT-1 inhibitors 失效
标题翻译： GlyT-1抑制剂
公开(公告)号：US06667336B2
公开(公告)日：2003-12-23
申请号：US10077579
申请日：2002-02-15
申请人： Zhaoqing Wang , William Delaney , Ashok Tehim , Shawn Maddaford , Ian Egle , Richard Schumacher , Allen T. Hopper
发明人： Zhaoqing Wang , William Delaney , Ashok Tehim , Shawn Maddaford , Ian Egle , Richard Schumacher , Allen T. Hopper
IPC分类号： A61K3138
CPC分类号： C07D409/10 , C07D333/20
摘要： The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了治疗神经和神经精神障碍的药物，其包含下式化合物或其药学上可接受的盐。

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