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1.发明授权Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and use thereof 失效吲唑，苯并噻唑，苯并异噻唑，苯并异恶唑及其制备和应用公开(公告)号：US08486937B2
公开(公告)日：2013-07-16
申请号：US13165370
申请日：2011-06-21
Applicant: Wenge Xie , Brian Herbert , Richard A. Schumacher , Truc Minh Nguyen , Jianguo Ma , Carla Maria Gauss , Ashok Tehim
Inventor： Wenge Xie , Brian Herbert , Richard A. Schumacher , Truc Minh Nguyen , Jianguo Ma , Carla Maria Gauss , Ashok Tehim
IPC: A61K31/439 , A61K31/4545 , A61K31/5377 , A61P3/10 , A61P25/16 , A61P25/18 , A61P25/24 , C07D453/02
CPC classification number: C07D453/02
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 (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.
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（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。
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2.发明授权Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof 失效吲唑类，苯并噻唑类，苯并异噻唑类，苯并异恶唑类，吡唑并吡啶类，异噻唑啉类及其制备方法公开(公告)号：US08273891B2
公开(公告)日：2012-09-25
申请号：US12700936
申请日：2010-02-05
Applicant: Richard Schumacher , Mihaela Diana Danca , Jianguo Ma , Brian Herbert , True Minh Nguyen , Wenge Xie , Ashok Tehim
Inventor： Richard Schumacher , Mihaela Diana Danca , Jianguo Ma , Brian Herbert , True Minh Nguyen , Wenge Xie , Ashok Tehim
IPC: C07D221/02 , C07D217/00
CPC classification number: C07D471/08
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 (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.
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（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。
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公开(公告)号：US08252811B2
公开(公告)日：2012-08-28
申请号：US13338835
申请日：2011-12-28
Applicant: Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
Inventor： Wenge Xie , Brian Herbert , Truc Nguyen , Carla Gauss , Ashok Tehim
IPC: A61K31/44 , C07D221/02 , C07D217/22
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.
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4.发明授权公开(公告)号：US07994199B2
公开(公告)日：2011-08-09
申请号：US12724754
申请日：2010-03-16
Applicant: Brian Herbert , Wenge Xie , Truc Minh Nguyen , Allen T Hopper , Ashok Tehim
Inventor： Brian Herbert , Wenge Xie , Truc Minh Nguyen , Allen T Hopper , Ashok Tehim
IPC: C07D401/02 , A61K31/44
CPC classification number: C07D401/14 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/08
Abstract: 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.
Abstract translation: 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。
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5.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：US07932248B2
公开(公告)日：2011-04-26
申请号：US11594993
申请日：2006-11-09
Applicant: Richard Schumacher , Jianguo Ma , Brian Herbert , Mihaela Diana Danca , Wenge Xie , Truc Minh Nguyen , Ashok Tehim
Inventor： Richard Schumacher , Jianguo Ma , Brian Herbert , Mihaela Diana Danca , Wenge Xie , Truc Minh Nguyen , Ashok Tehim
IPC: A61P25/28 , A61K31/551 , 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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Patent Agency Ranking
6.发明授权Indoles, 1H-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof 失效吲哚，1H-吲唑，1,2-苯并异恶唑，1,2-苯并异噻唑及其制备和用途公开(公告)号：US07902217B2
公开(公告)日：2011-03-08
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: A01N43/42 , A61K31/44 , C07D401/00 , C07D405/00 , C07D409/00 , C07D221/02
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：US20100029689A1
公开(公告)日：2010-02-04
申请号：US12497168
申请日：2009-07-02
Applicant: Allen T. HOPPER , Joan Marie CAROON , Elbert CHIN , Robert F. DUNN , Sharada Shenvi LABADIE , Jim LI , Richard Allen SCHUMACHER , Francisco Xavier TALAMAS
Inventor： Allen T. HOPPER , Joan Marie CAROON , Elbert CHIN , Robert F. DUNN , Sharada Shenvi LABADIE , Jim LI , Richard Allen SCHUMACHER , Francisco Xavier TALAMAS
IPC: A61K31/505 , A61K31/50 , A61K31/445 , A61K31/4462 , A61K31/444 , A61K31/4406 , A61K31/426 , A61K31/341 , C07D237/08 , C07D239/26 , C07D241/12 , C07D213/55 , C07D277/28 , C07D263/32 , A61P29/00 , A61P25/00 , A61P37/08
CPC classification number: C07D277/28 , C07C217/92 , C07C229/60 , C07C255/58 , C07C2601/04 , C07C2601/08 , C07D213/36 , C07D213/64 , C07D213/74 , C07D231/12 , C07D237/08 , C07D239/26 , C07D263/32 , C07D307/20 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.
Abstract translation: 通过新化合物，例如N-取代的苯胺和二苯胺类似物来实现PDE4的抑制。 本发明的化合物具有式I：其中R 1，R 2，R 3和R 4如本文所定义。
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8.发明授权Phosphodiesterase 4 inhibitors, including aminoindazole and aminobenzofuran analogs 失效磷酸二酯酶4抑制剂，包括氨基吲唑和氨基苯并呋喃类似物公开(公告)号：US07655802B2
公开(公告)日：2010-02-02
申请号：US11642592
申请日：2006-12-21
Applicant: Richard A. Schumacher , Allen T. Hopper , Ashok Tehim
Inventor： Richard A. Schumacher , Allen T. Hopper , Ashok Tehim
IPC: C07D231/56 , C07D401/06
CPC classification number: A61K31/343 , A61K31/416 , C07D231/56 , C07D401/12 , C07D405/12 , C07D405/14
Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.
Abstract translation: PDE4抑制是通过新的化合物，如氨基吲唑和氨基苯并呋喃类似物实现的。 本发明的化合物具有式I和II：其中R 1，R 2，R 3，R 4，R 7和R 8如本文所定义。
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公开(公告)号：US07625924B2
公开(公告)日：2009-12-01
申请号：US11312831
申请日：2005-12-21
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: A01N43/42 , A61K31/44 , C07D513/02 , C07D515/02
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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10.发明申请METHODS OF TREATMENT USING (+)- ISOPROPYL 2-METHOXYETHYL 4-(2-CHLORO-3-CYANO-PHENYL)-1, 4-DIHYDRO-2, 6-DIMETHYL-PYRIDINE-3, 5-DICARBOXYLATE 审中-公开使用（+） - 异丙基-2-甲氧基乙基4-（2-氯-3-氰基 - 苯基）-1,4-二氢-2,6-二甲基 - 吡啶-3,5-二甲氧基乙酸的处理方法公开(公告)号：US20090069361A1
公开(公告)日：2009-03-12
申请号：US12261649
申请日：2008-10-30
Applicant: Axel Unterbeck , Michael De Vivo , Gregory M. Rose
Inventor： Axel Unterbeck , Michael De Vivo , Gregory M. Rose
IPC: A61K31/435
CPC classification number: A61K45/06 , A61K31/407 , A61K31/4422 , A61K31/445 , A61K31/455 , A61K31/4745 , A61K2300/00
Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.
Abstract translation: 本发明涉及使用化合物（+） - 异丙基2-甲氧基乙基4-（2-氯-3-氰基 - 苯基）-1,4-二氢-2,6-二甲基 - 吡啶-3,5- 作为唯一的活性剂或与其它药物组合使用。
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