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公开(公告)号:US06251921B1
公开(公告)日:2001-06-26
申请号:US09312593
申请日:1999-05-14
申请人: Jolie Anne Bastian , Nickolay Yuri Chirgadze , Michael Lyle Denney , Matthew Joseph Fisher , Robert James Foglesong , Richard Waltz Harper , Mary George Johnson , Valentine Joseph Klimkowski , Todd Jonathan Kohn , Ho-Shen Lin , Michael Patrick Lynch , Jefferson Ray McCowan , Alan David Palkowitz , Michael Enrico Richett , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Jennifer Marie Tinsley , Minsheng Zhang
发明人: Jolie Anne Bastian , Nickolay Yuri Chirgadze , Michael Lyle Denney , Matthew Joseph Fisher , Robert James Foglesong , Richard Waltz Harper , Mary George Johnson , Valentine Joseph Klimkowski , Todd Jonathan Kohn , Ho-Shen Lin , Michael Patrick Lynch , Jefferson Ray McCowan , Alan David Palkowitz , Michael Enrico Richett , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Jennifer Marie Tinsley , Minsheng Zhang
IPC分类号: A61K314436
CPC分类号: C07D333/62 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/5377 , A61K31/55 , C07D231/12 , C07D233/56 , C07D249/08 , C07D333/56 , C07D333/58 , C07D333/64 , C07D333/66 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/06
摘要: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
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公开(公告)号:US6025382A
公开(公告)日:2000-02-15
申请号:US846647
申请日:1997-04-30
申请人: Jolie Anne Bastian , Nickolay Yuri Chirgadze , Michael Lyle Denney , Matthew Joseph Fisher , Robert James Foglesong , Richard Waltz Harper , Mary George Johnson , Valentine Joseph Klimkowski , Todd Jonathan Kohn , Ho-Shen Lin , Michael Patrick Lynch , Jefferson Ray McCowan , Alan David Palkowitz , Michael Enrico Richett , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Jennifer Marie Tinsley , Minsheng Zhang
发明人: Jolie Anne Bastian , Nickolay Yuri Chirgadze , Michael Lyle Denney , Matthew Joseph Fisher , Robert James Foglesong , Richard Waltz Harper , Mary George Johnson , Valentine Joseph Klimkowski , Todd Jonathan Kohn , Ho-Shen Lin , Michael Patrick Lynch , Jefferson Ray McCowan , Alan David Palkowitz , Michael Enrico Richett , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Jennifer Marie Tinsley , Minsheng Zhang
IPC分类号: C07D295/08 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/4436 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/5377 , A61K31/55 , A61P7/02 , C07D333/56 , C07D333/58 , C07D333/62 , C07D333/64 , C07D333/66 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/12 , C07D413/06 , C07D521/00 , A61K31/40 , A61K31/38 , C07D409/14
CPC分类号: C07D333/62 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/5377 , A61K31/55 , C07D231/12 , C07D233/56 , C07D249/08 , C07D333/56 , C07D333/58 , C07D333/64 , C07D333/66 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/06
摘要: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
摘要翻译: 本申请涉及作为本文定义的式I二胺的凝血酶抑制剂,凝血抑制剂和血栓栓塞障碍剂的用途。 它还提供式I的新型化合物,其制备方法和中间体,以及包含式I化合物的药物制剂。
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公开(公告)号:US06265416B1
公开(公告)日:2001-07-24
申请号:US09429424
申请日:1999-10-28
申请人: Jolie Anne Bastian , Matthew Joseph Fisher , Richard Waltz Harper , Ho-Shen Lin , Jefferson Ray McCowan , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Michael Robert Wiley , Minsheng Zhang
发明人: Jolie Anne Bastian , Matthew Joseph Fisher , Richard Waltz Harper , Ho-Shen Lin , Jefferson Ray McCowan , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Michael Robert Wiley , Minsheng Zhang
IPC分类号: A61K31535
CPC分类号: C07D471/04
摘要: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
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公开(公告)号:US06359136B1
公开(公告)日:2002-03-19
申请号:US09716605
申请日:2000-11-20
申请人: Jolie Ann Bastian , Matthew Joseph Fisher , Richard Waltz Harper , Ho-Shen Lin , Jefferson Ray McCowan , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Michael Robert Wiley , Minsheng Zhang
发明人: Jolie Ann Bastian , Matthew Joseph Fisher , Richard Waltz Harper , Ho-Shen Lin , Jefferson Ray McCowan , Daniel Jon Sall , Gerald Floyd Smith , Kumiko Takeuchi , Michael Robert Wiley , Minsheng Zhang
IPC分类号: C07D47104
CPC分类号: C07D471/04
摘要: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
摘要翻译: 本申请涉及本文定义的式I(及其药学上可接受的盐)的新型化合物,其制备方法和中间体,包含式I的新型化合物的药物制剂以及式I化合物作为凝血酶抑制剂的用途 。
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5.N-(2-ARYLETHYL)BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR 有权
标题翻译: 作为5-HT6受体拮抗剂的N-(2-亚甲基)苄基苯胺公开(公告)号:US20090306110A1
公开(公告)日:2009-12-10
申请号:US12504242
申请日:2009-07-16
申请人: Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
发明人: Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
IPC分类号: A61K31/404 , A61K31/506 , A61K31/435 , A61K31/445 , A61P25/28
CPC分类号: C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要: The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译: 本发明提供作为5-HT 6受体拮抗剂的式(I)化合物。
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6.N-(2-arylethyl)benzylamines as antagonists of the 5-HT6 receptor 有权
标题翻译: N-(2-芳基乙基)苄胺作为5-HT 6受体的拮抗剂公开(公告)号:US08044090B2
公开(公告)日:2011-10-25
申请号:US12504242
申请日:2009-07-16
申请人: Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
发明人: Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
IPC分类号: A61K31/4045 , A61K31/137 , C07D209/14
CPC分类号: C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要: The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译: 本发明提供作为5-HT 6受体拮抗剂的式(I)化合物。
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7.N-(2-Arylethyl) benzylamines as antagonists of the 5-HT6 receptor 有权
标题翻译: N-(2-甲苯基乙基)苄胺作为5-HT 6受体的拮抗剂公开(公告)号:US07157488B2
公开(公告)日:2007-01-02
申请号:US10472741
申请日:2002-03-15
申请人: Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
发明人: Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
IPC分类号: A61K31/4045 , A61K31/137 , C07D209/14 , C07C211/00
CPC分类号: C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要: The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.
摘要翻译: 本发明提供式I化合物其药学上可接受的盐及其药物组合物,它们是5-HT 6受体的拮抗剂。 本发明还提供了一种治疗与5-HT 6受体相关的疾病的方法,包括精神分裂症,焦虑症,阿尔茨海默氏病和认知障碍,其选自年龄相关的认知衰退,轻度认知 损伤和痴呆,包括:向有需要的患者施用有效量的式I化合物。
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公开(公告)号:US07960419B2
公开(公告)日:2011-06-14
申请号:US12300415
申请日:2007-06-07
申请人: Ryan Thomas Backer , Matthew Joseph Fisher , Sean Patrick Hollinshead , Steven Lee Kuklish , Edward C R Smith , Kumiko Takeuchi
发明人: Ryan Thomas Backer , Matthew Joseph Fisher , Sean Patrick Hollinshead , Steven Lee Kuklish , Edward C R Smith , Kumiko Takeuchi
IPC分类号: A61K31/425 , C07D275/03 , A61P25/04
CPC分类号: C07D275/03
摘要: This application relates to a substituted carboxamide compound of formula I, or a pharmaceutically acceptable salt thereof, as defined herein, a pharmaceutical composition thereof, and its use in treating pain.
摘要翻译: 本申请涉及如本文所定义的式I的取代的甲酰胺化合物或其药学上可接受的盐,其药物组合物及其在治疗疼痛中的用途。
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公开(公告)号:US20090182025A1
公开(公告)日:2009-07-16
申请号:US12300415
申请日:2007-06-07
申请人: Ryan Thomas Backer , Matthew Joseph Fisher , Sean Patrick Hollinshead , Steven Lee Kuklish , Edward C.R. Smith , Kumiko Takeuchi
发明人: Ryan Thomas Backer , Matthew Joseph Fisher , Sean Patrick Hollinshead , Steven Lee Kuklish , Edward C.R. Smith , Kumiko Takeuchi
IPC分类号: A61K31/425 , C07D275/03 , A61P25/00
CPC分类号: C07D275/03
摘要: This application relates to a substituted carboxamide compound of formula I, or a pharmaceutically acceptable salt thereof, as defined herein, a pharmaceutical composition thereof, and its use in treating pain.
摘要翻译: 本申请涉及如本文所定义的式I的取代的甲酰胺化合物或其药学上可接受的盐,其药物组合物及其在治疗疼痛中的用途。
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10.Benzofurylpiperazines and benzofurylhomopiperazines: serotonin agonists 失效
标题翻译: 苯并呋喃基哌嗪和苯并呋喃基哌嗪嗪:5-羟色胺激动剂公开(公告)号:US06967201B1
公开(公告)日:2005-11-22
申请号:US10031312
申请日:2000-07-21
申请人: Karin Briner , Joseph Paul Burkhart , Timothy Paul Burkholder , Brian Eugene Cunningham , Matthew Joseph Fisher , William Harlan Gritton , Shawn Christopher Miller , Jeffrey Thomas Mullaney , Matthew Robert Reinhard , Dennis Charles Thompson , Leonard Larry Winneroski , Yanping Xu
发明人: Karin Briner , Joseph Paul Burkhart , Timothy Paul Burkholder , Brian Eugene Cunningham , Matthew Joseph Fisher , William Harlan Gritton , Shawn Christopher Miller , Jeffrey Thomas Mullaney , Matthew Robert Reinhard , Dennis Charles Thompson , Leonard Larry Winneroski , Yanping Xu
IPC分类号: A61K31/496 , A61K31/551 , A61P3/04 , A61P25/24 , A61P43/00 , C07D307/79 , C07D405/04 , C07D405/10 , C07D405/12
CPC分类号: C07D307/79 , C07D405/04 , C07D405/12
摘要: The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1, R2, R3, R4, R5, R5′, R6, R6′, R7, R7′, R8, and R8′ are as described in the specification.
摘要翻译: 本发明提供式I的5-羟色胺苯并呋喃基哌嗪:其中:A是下式的哌嗪和R 1,R 1,R 2,R 3, R 4,R 5,R 5,R 6,R 6,R 6, R SUP,R 7,R 7,R 8和R 8'如上所述 规格。
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