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公开(公告)号：US20140142088A1
公开(公告)日：2014-05-22
申请号：US14083013
申请日：2013-11-18
申请人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Alison L. Zulli
发明人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Alison L. Zulli
IPC分类号： C07D498/04 , C07D237/14 , C07D409/04 , C07D237/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D495/04
CPC分类号： C07D498/04 , C07D237/14 , C07D237/26 , C07D237/32 , C07D237/36 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D495/04
摘要： The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
摘要翻译： 本发明涉及介导酶活性的新的哒嗪酮衍生物。 特别地，这些化合物可有效治疗与组胺H3受体活性相关的疾病或疾病状态，包括例如神经变性疾病，睡眠/觉醒障碍，注意力缺陷多动障碍和认知。
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32.发明授权Methods of treating disorders mediated by histamine H3 receptors using pyridazinone derivatives 有权使用哒嗪酮衍生物治疗由组胺H3受体介导的病症的方法公开(公告)号：US08673916B2
公开(公告)日：2014-03-18
申请号：US13197243
申请日：2011-08-03
申请人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek D. Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J. S. Knutsen , Ming Tao , Allison L. Zulli
发明人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek D. Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J. S. Knutsen , Ming Tao , Allison L. Zulli
CPC分类号： C07D498/04 , C07D237/14 , C07D237/26 , C07D237/32 , C07D237/36 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D495/04
摘要： The present invention is directed to methods of treating disorders mediated by Histamine H3 receptors by administering novel pyridazinone derivatives. In particular, the pyridazinone compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
摘要翻译： 本发明涉及通过施用新的哒嗪酮衍生物治疗由组胺H3受体介导的病症的方法。 特别地，哒嗪酮化合物可有效治疗与组胺H3受体活性相关的疾病或疾病状态，包括例如神经退行性疾病，睡眠/觉醒障碍，注意缺陷多动障碍和认知/认知障碍。
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33.发明授权Substituted phenoxypropylcycloamine derivatives as histamine-3 (H3) receptor ligands 失效取代的苯氧基丙胺环胺衍生物作为组胺-3（H3）受体配体公开(公告)号：US08648067B2
公开(公告)日：2014-02-11
申请号：US13334311
申请日：2011-12-22
申请人： Edward R. Bacon , Thomas R. Bailey , Sankar Chatterjee , Derek D. Dunn , Greg A. Hostetler , Robert L. Hudkins , Brigitte Lesur , Babu G. Sundar , Allison L. Zulli , Christophe Yue
发明人： Edward R. Bacon , Thomas R. Bailey , Sankar Chatterjee , Derek D. Dunn , Greg A. Hostetler , Robert L. Hudkins , Brigitte Lesur , Babu G. Sundar , Allison L. Zulli , Christophe Yue
IPC分类号： A61K31/55 , A61K31/54 , A61K31/45 , A61K31/535 , A61K31/497 , A61K31/545 , A61K31/445 , A01N43/40 , C07D223/18 , C07D279/10 , C07D413/00 , C07D403/00 , C07D401/00 , C07D217/00 , C07D211/00 , C07D405/00 , C07D295/00
CPC分类号： C07D403/12 , C07C217/54 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/27 , C07D209/44 , C07D211/14 , C07D211/22 , C07D211/38 , C07D211/46 , C07D215/02 , C07D215/06 , C07D217/04 , C07D241/08 , C07D295/108 , C07D295/185 , C07D401/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
摘要翻译： 本发明提供式I化合物：它们用作H3拮抗剂/反向激动剂，其制备方法及其药物组合物。
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公开(公告)号：US08586588B2
公开(公告)日：2013-11-19
申请号：US12815813
申请日：2010-06-15
申请人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J. S. Knutsen , Ming Tao , Allison L. Zulli
发明人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J. S. Knutsen , Ming Tao , Allison L. Zulli
IPC分类号： C07D403/12 , C07D401/14 , A61K31/501 , A61P25/20 , A61P3/04 , A61P25/18 , A61P29/00 , A61P25/06 , A61P25/24 , A61P25/08
CPC分类号： C07D498/04 , C07D237/14 , C07D237/26 , C07D237/32 , C07D237/36 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D495/04
摘要： The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds and/or their pharmaceutically acceptable salts may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
摘要翻译： 本发明涉及介导酶活性的新的哒嗪酮衍生物。 特别地，化合物和/或其药学上可接受的盐可有效治疗与组胺H3受体活性相关的疾病或疾病状态，包括例如神经变性障碍，睡眠/觉醒障碍，注意缺陷多动障碍 和认知/认知障碍。
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公开(公告)号：US08153667B2
公开(公告)日：2012-04-10
申请号：US11901150
申请日：2007-09-14
IPC分类号： A61K31/4196 , A61K31/40 , A61K31/381 , A61K31/34 , A61K31/10 , C07D249/08 , C07D207/00 , C07D333/00 , C07D307/00 , C07C317/00
CPC分类号： C07C317/44 , C07C317/10 , C07C317/12 , C07C317/18 , C07C317/28 , C07C321/22 , C07C323/12 , C07C323/22 , C07C323/25 , C07C323/49 , C07C323/52 , C07C323/60 , C07C323/61 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D249/12 , C07D307/38 , C07D333/18 , C07D333/22
摘要： The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.
摘要翻译： 本发明提供了结构化合物：其中组成成分在本文中定义，包括其药物组合物和用其治疗疾病的方法。
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公开(公告)号：US07981907B2
公开(公告)日：2011-07-19
申请号：US12199167
申请日：2008-08-27
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/445
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译： 本发明涉及化学组成，其制备方法和组合物的用途。 特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病 阿尔茨海默氏病; 注意力缺陷障碍 注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。
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公开(公告)号：US07915236B2
公开(公告)日：2011-03-29
申请号：US12496359
申请日：2009-07-01
申请人： Raffaella Bernardini , Alberto Bernareggi , Paolo G. Cassara , Sankar Chatterjee , Germano D'Arasmo , Sergio De Munari , Edmondo Ferretti , Mohamed Iqbal , Ernesto Menta , Patricia A. Messina McLaughlin , Ambrogio Oliva
发明人： Raffaella Bernardini , Alberto Bernareggi , Paolo G. Cassara , Sankar Chatterjee , Germano D'Arasmo , Sergio De Munari , Edmondo Ferretti , Mohamed Iqbal , Ernesto Menta , Patricia A. Messina McLaughlin , Ambrogio Oliva
摘要： The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
摘要翻译： 本发明提供了可通过抑制蛋白酶体活性来调节细胞凋亡的硼酸化合物，硼酸酯及其组合物。 化合物和组合物可以用于诱导凋亡和直接与蛋白酶体活性间接相关的疾病如癌症和其它疾病的方法中。
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公开(公告)号：US20110059959A1
公开(公告)日：2011-03-10
申请号：US12949254
申请日：2010-11-18
申请人： Sankar Chatterjee , James L. Diebold , Derek Dunn , Robert L. Hudkins , Reddeppareddy Dandu , Gregory J. Wells , Allison L. Zulli
发明人： Sankar Chatterjee , James L. Diebold , Derek Dunn , Robert L. Hudkins , Reddeppareddy Dandu , Gregory J. Wells , Allison L. Zulli
IPC分类号： A61K31/5377 , C07D471/14 , A61K31/437 , C07D487/04 , A61K31/407 , C07D413/14 , C07D249/08 , A61K31/4196 , C07D401/12 , A61K31/454 , C07D403/14 , A61K31/496 , A61P25/00 , A61P25/16 , A61P25/28 , A61P9/10 , A61P3/00 , A61P19/02 , A61P17/06 , A61P35/00 , C12N5/02
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D491/04 , C07D495/04 , C07D519/00
摘要： The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.
摘要翻译： 本发明涉及介导酶活性的新型多环分子。 特别地，所述化合物可有效治疗与PARP，VEGFR2和MLK3酶的活性相关的疾病或疾病状态，包括例如神经变性疾病，炎症，局部缺血和癌症。
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公开(公告)号：US20100280007A1
公开(公告)日：2010-11-04
申请号：US12815800
申请日：2010-06-15
申请人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Allison L. Zulli
发明人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Allison L. Zulli
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/502 , A61K31/501 , C07D413/12 , C07D498/04 , C07D403/12 , A61P25/00 , A61P3/04 , A61P25/28 , A61P25/18 , A61P25/08 , A61P11/00 , A61P25/24 , A61P29/00 , A61P9/10 , A61P1/00 , A61P25/06 , A61P43/00 , C07D495/04 , C07D401/14 , C07D409/14 , A61K31/5025
CPC分类号： C07D498/04 , C07D237/14 , C07D237/26 , C07D237/32 , C07D237/36 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D495/04
摘要： The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
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公开(公告)号：US07449481B2
公开(公告)日：2008-11-11
申请号：US11104091
申请日：2005-04-12
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/445 , C07D333/02
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译： 本发明涉及化学组成，其制备方法和组合物的用途。 特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 2， 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病 阿尔茨海默氏病; 注意力缺陷障碍 注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。
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