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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
Applicant: Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
Inventor： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC: A61K31/437 , A61K31/4375 , A61P25/00 , A61P25/24 , A61P25/16 , A61P25/28 , C07D471/04 , A61P25/18
CPC classification number: C07D471/04 , C07D519/00
Abstract: 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.
Abstract translation: 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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2.发明授权Indazoles, benzothiazoles, and benzoisothiazoles, and preparation and uses thereof 失效吲唑，苯并噻唑和苯并异噻唑，及其制备和用途公开(公告)号：US08134003B2
公开(公告)日：2012-03-13
申请号：US13103512
申请日：2011-05-09
Applicant: Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
Inventor： Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
IPC: C07D211/02
CPC classification number: C07D453/02
Abstract: 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.
Abstract translation: 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。
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3.发明申请INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF 失效吲哚，1H-INDAZOLES，1,2-二苯并唑和1,2-二苯并噻唑及其制备及用途公开(公告)号：US20110312989A1
公开(公告)日：2011-12-22
申请号：US13162786
申请日：2011-06-17
Applicant: Wenge Xie , Brian Herbert , Jianguo Ma , Truc Minh Nguyen , Richard Schumacher , Carla Maria Gauss , Ashok Tehim
Inventor： Wenge Xie , Brian Herbert , Jianguo Ma , Truc Minh Nguyen , Richard Schumacher , Carla Maria Gauss , Ashok Tehim
IPC: A61K31/416 , C07D471/08 , C07D417/14 , C07D413/14 , A61K31/439 , A61K31/428 , A61K31/423 , A61K31/427 , A61K31/422 , A61P25/18 , A61P25/28 , A61P25/22 , A61P25/24 , A61P25/00 , A61P25/16 , A61P25/14 , A61P31/18 , A61P9/00 , A61P25/32 , A61P25/30 , A61P3/04 , A61P3/10 , A61P9/04 , A61P23/00 , A61P29/00 , C07D403/14
CPC classification number: C07D487/08
Abstract: 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 for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Abstract translation: 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，本发明涉及例如吲哚，1H-吲唑，1,2-苯并异恶唑和1,2-苯并异噻唑的新化合物，其作为α7nAChR亚型的配体，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。
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4.发明申请INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF 审中-公开吲哚，1H-INDAZOLES，1,2-苄基氧杂环己烷，1,2-苯并唑烷，及其制备及用途公开(公告)号：US20110178075A1
公开(公告)日：2011-07-21
申请号：US13041859
申请日：2011-03-07
Applicant: Wenge XIE , Brian Herbert , Jianguo Ma , Truc Minh Nguyen , Richard Schumacher , Carla Maria Gauss , Ashok Tehim
Inventor： Wenge XIE , Brian Herbert , Jianguo Ma , Truc Minh Nguyen , Richard Schumacher , Carla Maria Gauss , Ashok Tehim
IPC: A61K31/416 , C07D471/08 , A61K31/46 , C07D471/04 , A61K31/4985 , C07D487/04 , C07D487/08 , A61K31/4995 , A61K31/439 , C07D403/12 , C07D417/14 , A61K31/427 , C07D405/14 , C07D409/14 , C07D413/14 , A61K31/422 , A61K31/5377 , A61K31/541 , A61P3/10 , A61P29/00 , A61P7/00 , A61P25/28 , A61P25/00 , A61P25/16 , A61P25/24 , A61P9/00
CPC classification number: C07D451/04 , C07D451/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
Abstract: 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 (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.
Abstract translation: 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（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。
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公开(公告)号：US07696198B2
公开(公告)日：2010-04-13
申请号：US10825610
申请日：2004-04-16
Applicant: Ashok Tehim , Allen Hopper , Ruiping Liu , Erik Kuester , Robert F. Dunn , Thomas E. Renau
Inventor： Ashok Tehim , Allen Hopper , Ruiping Liu , Erik Kuester , Robert F. Dunn , Thomas E. Renau
IPC: A61K31/54 , A61K31/425 , C07D417/02 , C07D413/02 , C07D405/00
CPC classification number: C07D207/26 , C07D405/12 , C07D417/14
Abstract: Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.
Abstract translation: 选择性PDE4抑制由4-（取代的 - 苯基）-2-吡咯烷酮化合物实现。 与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且显示关于抑制其它类别的PDE的选择性。 本发明的化合物具有式I：其中R 1，R 2和R 3如本文所定义。
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Patent Agency Ranking
6.发明申请PYRROLIDINE-SUBSTITUTED AZAINDOLE COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY 审中-公开具有5-HT6受体亲和性的吡咯烷 - 取代的唑烷化合物公开(公告)号：US20100022581A1
公开(公告)日：2010-01-28
申请号：US12492430
申请日：2009-06-26
Applicant: Mihaela Diana Danca , Robert Dunn , Ashok Tehim , Wenge Xie
Inventor： Mihaela Diana Danca , Robert Dunn , Ashok Tehim , Wenge Xie
IPC: A61K31/437 , C07D401/14 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30 , A61P1/00 , A61P25/16 , A61P25/06 , A61P9/00
CPC classification number: C07D401/04
Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, A, B, D, E, G, Ar, 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.
Abstract translation: 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，A，B，D，E，G，Ar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。
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7.发明申请NICOTINIC ALPHA-7 RECEPTOR LIGANDS AND PREPARATION AND USES THEREOF 审中-公开NICOTINIC ALPHA-7受体配体及其制备及其用途公开(公告)号：US20100016351A1
公开(公告)日：2010-01-21
申请号：US12551020
申请日：2009-08-31
Applicant: Truc Minh Nguyen , Wenge Xie , Richard Schumacher , Brian Herbert , Ashok Tehim
Inventor： Truc Minh Nguyen , Wenge Xie , Richard Schumacher , Brian Herbert , Ashok Tehim
IPC: A61K31/4375 , C07D453/02
CPC classification number: C07D453/02
Abstract: 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 which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Abstract translation: 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亚型配体的新型化合物，制备此类化合物的方法，含有这些化合物的组合物及其使用方法。
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8.发明授权1H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof 失效1H-吲唑，苯并噻唑，1,2-苯并异恶唑，1,2-苯并异噻唑和色酮及其制备和用途公开(公告)号：US07632831B2
公开(公告)日：2009-12-15
申请号：US11123219
申请日：2005-05-06
Applicant: Wenge Xie , Brian Herbert , Richard A. Schumacher , Jianguo Ma , Truc Minh Nguyen , Carla Maria Gauss , Ashok Tehim
Inventor： Wenge Xie , Brian Herbert , Richard A. Schumacher , Jianguo Ma , Truc Minh Nguyen , Carla Maria Gauss , Ashok Tehim
IPC: A61P25/28 , A61K31/4985 , A61K31/551 , C07D471/08 , C07D487/08
CPC classification number: C07D471/08 , C07D487/08
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US07585882B2
公开(公告)日：2009-09-08
申请号：US11253812
申请日：2005-10-20
Applicant: Allen Hopper , Robert Francis Dunn , Erik Mikal Kuester , Richard Dennis Conticello , Ruiping Liu , Ashok Tehim
Inventor： Allen Hopper , Robert Francis Dunn , Erik Mikal Kuester , Richard Dennis Conticello , Ruiping Liu , Ashok Tehim
IPC: A61K31/4015 , A61K31/4025 , A61K31/433 , C07D207/12 , C07D285/08 , C07D403/12 , A61K31/341 , C07D407/10 , C07D407/14
CPC classification number: C07D207/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Abstract translation: 选择性PDE4的抑制是通过新的化合物，例如4-（取代的 - 苯基）-2-吡咯烷酮化合物实现的。 本发明的化合物具有式I：其中R 1，R 2和R 3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。
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10.发明申请INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF 失效吲哚，1H-INDAZOLES，1,2-苄基氧杂环己烷，1,2-苯并唑烷，及其制备及用途公开(公告)号：US20090118232A1
公开(公告)日：2009-05-07
申请号：US12273039
申请日：2008-11-18
Applicant: Wenge Xie , Brian Herbert , Jianguo MA , Truc Minh NGUYEN , Richard SCHUMACHER , Carla Maria Gauss , Ashok TEHIM
Inventor： Wenge Xie , Brian Herbert , Jianguo MA , Truc Minh NGUYEN , Richard SCHUMACHER , Carla Maria Gauss , Ashok TEHIM
IPC: A61K31/46 , C07D471/04 , C07D487/04 , A61K31/5377 , A61K31/4985 , A61K31/55 , A61K31/695 , A61K31/541 , A61P25/00
CPC classification number: C07D451/04 , C07D451/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
Abstract: 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 (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.
Abstract translation: 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（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。
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