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公开(公告)号：US08058262B2
公开(公告)日：2011-11-15
申请号：US13020425
申请日：2011-02-03
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
IPC分类号： A61K31/69
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.
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公开(公告)号：US20110144033A1
公开(公告)日：2011-06-16
申请号：US13020425
申请日：2011-02-03
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：US20100273779A1
公开(公告)日：2010-10-28
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： A61K31/55 , C07D403/12 , A61K31/501 , A61K31/502 , C07D495/04 , A61P3/04 , A61P9/10 , A61P11/00 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/28 , A61P1/00 , A61P29/00
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.
摘要翻译： 本发明涉及介导酶活性的新型吡哒嗪酮衍生物。 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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公开(公告)号：US20090062284A1
公开(公告)日：2009-03-05
申请号：US12199167
申请日：2008-08-27
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg A. 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 A. Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/381 , C07D333/24 , C07D307/54 , C07D409/12 , C07D405/12 , C07D401/12 , C07D413/12 , C07D209/44 , C07C235/72 , A61K31/496 , A61K31/40 , A61K31/4025 , A61K31/5377 , A61P25/00
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：US07314875B2
公开(公告)日：2008-01-01
申请号：US11103958
申请日：2005-04-12
IPC分类号： C07D265/30 , C07D211/14 , C07D207/12 , A61K31/5375 , A61K31/135
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：US07223745B2
公开(公告)日：2007-05-29
申请号：US10918610
申请日：2004-08-12
CPC分类号： C07F5/025
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：USRE39575E1
公开(公告)日：2007-04-17
申请号：US10996325
申请日：2004-11-23
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , John P. Mallamo , Jeffry L. Vaught , Matthew S. Miller
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , John P. Mallamo , Jeffry L. Vaught , Matthew S. Miller
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D495/04 , C07C317/44 , C07C323/60 , C07C2603/18 , C07D207/16 , C07D207/416 , C07D211/88 , C07D213/34 , C07D219/04 , C07D231/54 , C07D233/64 , C07D261/08 , C07D263/16 , C07D263/32 , C07D263/34 , C07D275/02 , C07D277/26 , C07D277/56 , C07D307/68 , C07D311/84 , C07D333/18 , C07D335/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/06
摘要： The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.
摘要翻译： 本发明涉及取代的硫代乙酰胺的化学组成，其制备方法和组合物在治疗疾病中的用途。
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公开(公告)号：US20050192313A1
公开(公告)日：2005-09-01
申请号：US11116755
申请日：2005-04-28
申请人： Edward Bacon , Sankar Chatterjee , Derek Dunn , John Mallamo , Matthew Miller , Rabindranath Tripathy , Jeffry Vaught
发明人： Edward Bacon , Sankar Chatterjee , Derek Dunn , John Mallamo , Matthew Miller , Rabindranath Tripathy , Jeffry Vaught
IPC分类号： C07D295/08 , A61K31/165 , A61K31/166 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/415 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4436 , A61K31/45 , A61K31/4535 , A61K31/5377 , A61P1/00 , A61P1/14 , A61P9/10 , A61P11/00 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P43/00 , C07C317/44 , C07C323/60 , C07C323/61 , C07D207/16 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/416 , C07D211/88 , C07D213/34 , C07D213/40 , C07D219/04 , C07D231/54 , C07D233/54 , C07D261/08 , C07D263/10 , C07D263/16 , C07D263/32 , C07D263/34 , C07D275/02 , C07D277/26 , C07D277/56 , C07D307/68 , C07D311/84 , C07D333/18 , C07D335/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/06 , C07D495/04 , C07D498/04 , A61K31/473 , A61K31/353 , A61K31/382
CPC分类号： C07D263/34 , C07C317/44 , C07C323/60 , C07C323/63 , C07C2603/18 , C07C2603/32 , C07D207/16 , C07D207/273 , C07D207/416 , C07D211/88 , C07D213/34 , C07D219/04 , C07D231/54 , C07D233/64 , C07D261/08 , C07D263/16 , C07D263/32 , C07D275/02 , C07D277/26 , C07D277/56 , C07D307/68 , C07D311/84 , C07D333/18 , C07D335/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/06 , C07D495/04
摘要： The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.
摘要翻译： 本发明涉及取代的硫代乙酰胺的化学组成，其制备方法和组合物在治疗疾病中的用途。
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公开(公告)号：US06310057B1
公开(公告)日：2001-10-30
申请号：US09519979
申请日：2000-03-07
申请人： Sankar Chatterjee , John P. Mallamo
发明人： Sankar Chatterjee , John P. Mallamo
IPC分类号： A61K314015
CPC分类号： C07D209/48 , C07D403/12
摘要： This invention relates to &agr;-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states.
摘要翻译： 本发明涉及多分子蛋白酶（MCP）的α-酮酰胺抑制剂，包括这种抑制剂的组合物以及使用MCP抑制剂的方法。 本发明的MCP抑制剂可用于例如延缓入射到各种生理状态的肌肉质量的损失。
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60.发明授权Peptide-containing &agr;-ketoamide cysteine and serine protease inhibitors 失效含肽的α-酮酰胺半胱氨酸和丝氨酸蛋白酶抑制剂公开(公告)号：US06288231B1
公开(公告)日：2001-09-11
申请号：US09527540
申请日：2000-03-16
IPC分类号： C07D20702
CPC分类号： C07D207/08 , C07C311/06 , C07C311/46 , C07C311/48 , C07D207/20 , C07D207/48 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/74 , C07D235/06 , C07D239/42 , C07D275/06 , C07D277/40 , C07D277/54 , C07D333/34 , C07D333/62 , C07D409/04 , C07D409/14 , C07D413/04 , C07K5/0202 , C07K5/06069
摘要： This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
摘要翻译： 本发明涉及半胱氨酸和丝氨酸蛋白酶的含肽α-酮酰胺抑制剂，制备这些化合物的方法及其使用方法。
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