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公开(公告)号：US07112683B2
公开(公告)日：2006-09-26
申请号：US10932331
申请日：2004-09-02
申请人： Deborah E. Bertenshaw , Daniel P. Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert A. Chrusciel , Michael Clare
发明人： Deborah E. Bertenshaw , Daniel P. Getman , Robert M. Heintz , John J. Talley , Kathryn L. Reed , Robert A. Chrusciel , Michael Clare
IPC分类号： C07D221/18 , C07D221/22
CPC分类号： C07D333/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D279/12 , C07D335/02 , C07D409/12
摘要： The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
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公开(公告)号：US5830888A
公开(公告)日：1998-11-03
申请号：US406614
申请日：1995-03-20
IPC分类号： C07D255/02 , C07D285/00 , A61K31/33 , C07D273/00 , C07D487/00
CPC分类号： C07D285/00 , C07D255/02
摘要： The present invention relates to N-heterocyclic-containing macrocyclic hydroxyethylamine protease inhibitor compounds, compositions and methods for inhibiting retroviral proteases.
摘要翻译： 本发明涉及含有N-杂环的大环羟基胺蛋白酶抑制剂化合物，用于抑制逆转录病毒蛋白酶的组合物和方法。
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公开(公告)号：US07067542B2
公开(公告)日：2006-06-27
申请号：US10192625
申请日：2002-07-10
IPC分类号： A61K31/40 , A61K31/41 , A61K31/435 , C07D213/46 , C07D207/333
CPC分类号： C07D213/82 , C07C235/84 , C07C255/44 , C07C271/20 , C07C323/42 , C07D263/34 , C07D263/48 , C07D277/56
摘要： The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
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公开(公告)号：US20130029980A1
公开(公告)日：2013-01-31
申请号：US13640054
申请日：2011-04-06
申请人： Philip D. G. Coish , Brian R. Dixon , David Osterman , Paul Adrian Aristoff , Manuel Navia , Frank Sciavolino , Stephanie Avola , Nick Baboulas , Thomas R. Belliotti , Angelica Bello , Judd Berman , Robert A. Chrusciel , Bruce R. Evans , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Phil Wickens , Jeffrey Wilson , Heinrich J. Schostarez
发明人： Philip D. G. Coish , Brian R. Dixon , David Osterman , Paul Adrian Aristoff , Manuel Navia , Frank Sciavolino , Stephanie Avola , Nick Baboulas , Thomas R. Belliotti , Angelica Bello , Judd Berman , Robert A. Chrusciel , Bruce R. Evans , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Phil Wickens , Jeffrey Wilson , Heinrich J. Schostarez
IPC分类号： C07D487/04 , A61P31/04 , A61K31/5377 , A61K31/519 , C07D491/147
CPC分类号： A01N43/90 , C07D475/14
摘要： The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.
摘要翻译： 本发明涉及新的黄素衍生物，其用途和用作核糖开关配体和/或抗感染剂的组合物。
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公开(公告)号：US20120295903A1
公开(公告)日：2012-11-22
申请号：US13381809
申请日：2010-06-30
申请人： Kenneth F. Blount , Philip D.G. Coish , Brian R. Dixon , Jayhyuk Myung , David Osterman , Phil Wickens , Stephanie Avola , Nick Baboulas , Angelica Bello , Judd Berman , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Jeffrey Wilson , Jeffrey A. Leiby , Dennis Underwood , Paul Adrian Aristoff , Heinrich J. Schostarez , Robert A. Chrusciel , Thomas R. Belliotti , Bruce R. Evans , Frank C. Sciavolino , Manuel A. Navia
发明人： Kenneth F. Blount , Philip D.G. Coish , Brian R. Dixon , Jayhyuk Myung , David Osterman , Phil Wickens , Stephanie Avola , Nick Baboulas , Angelica Bello , Judd Berman , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Jeffrey Wilson , Jeffrey A. Leiby , Dennis Underwood , Paul Adrian Aristoff , Heinrich J. Schostarez , Robert A. Chrusciel , Thomas R. Belliotti , Bruce R. Evans , Frank C. Sciavolino , Manuel A. Navia
IPC分类号： C07D487/04 , A01P1/00 , A61K31/5377 , A61P31/04 , A61K31/525 , A01N43/90
CPC分类号： C07D487/04
摘要： The present invention relates novel flavin derivatives and other flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. The invention also provides method of making novel flavin derivatives.
摘要翻译： 本发明涉及新的黄素衍生物和其它黄素衍生物，其用途和用作核糖开关配体和/或抗感染剂的组合物。 本发明还提供了制备新型黄素衍生物的方法。
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公开(公告)号：US06482849B1
公开(公告)日：2002-11-19
申请号：US09102584
申请日：1998-06-23
申请人： Thomas J. Lobl , Bradley R. Teegarden , Alexander Polinsky , Gilbert M. Rishton , Masafumi Yamagishi , Steven Tanis , Jed F. Fisher , Edward W. Thomas , Robert A. Chrusciel
发明人： Thomas J. Lobl , Bradley R. Teegarden , Alexander Polinsky , Gilbert M. Rishton , Masafumi Yamagishi , Steven Tanis , Jed F. Fisher , Edward W. Thomas , Robert A. Chrusciel
IPC分类号： A61K3127
CPC分类号： C07D213/81 , C07C229/46 , C07C233/60 , C07C233/63 , C07C233/83 , C07C233/87 , C07C235/40 , C07C235/64 , C07C235/84 , C07C237/22 , C07C237/40 , C07C237/42 , C07C255/29 , C07C255/46 , C07C259/08 , C07C271/22 , C07C271/28 , C07C275/26 , C07C275/42 , C07C311/21 , C07C311/64 , C07D207/16 , C07D209/20 , C07D213/64 , C07D213/82 , C07D217/26 , C07D233/64 , C07D295/185 , C07D295/192 , C07D307/68 , C07D333/24
摘要： The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.
摘要翻译： 本发明涉及根据式[I]的小分子：其是α4β1介导的对VCAM或CS-1的粘附的有效抑制剂，其可用于治疗或预防哺乳动物如人的α4β1粘附介导的病症 。
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7.发明授权Carbamic acid derivatives of substituted dibenzoxazepine compounds, pharmaceutical compositions and methods of use 失效取代二苯并氮杂化合物的氨基甲酸衍生物，药物组合物和使用方法
公开(公告)号：US5488046A
公开(公告)日：1996-01-30
申请号：US147356
申请日：1993-11-03
申请人： Robert A. Chrusciel , Timothy J. Hagen , E. Ann Hallinan , Jinglin Li , Sofya Tsymbalov , David B. Reitz
发明人： Robert A. Chrusciel , Timothy J. Hagen , E. Ann Hallinan , Jinglin Li , Sofya Tsymbalov , David B. Reitz
IPC分类号： C07D498/04 , C07D498/06 , C07D498/10 , C07D513/04 , A61K31/55
CPC分类号： C07D498/04 , C07D498/06 , C07D498/10
摘要： The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译： 本发明提供了可用作治疗疼痛的止痛剂和作为用于治疗前列腺素-E2介导的疾病的前列腺素E2拮抗剂的式I的取代二苯并氮杂化合物：其可用作治疗有效量的药物组合物 的式I化合物与药学上可接受的载体的组合，消除或改善动物疼痛的方法，以及在动物中治疗前列腺素-E2介导的疾病的方法，包括给予治疗有效量的化合物 的I型动物。
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公开(公告)号：US06596752B1
公开(公告)日：2003-07-22
申请号：US10193137
申请日：2002-07-12
申请人： Thomas J. Lobl , Bradley R. Teegarden , Alexander Polinsky , Gilbert M. Rishton , Masafumi Yamagishi , Steven Tanis , Jed F. Fisher , Edward W. Thomas , Robert A. Chrusciel
发明人： Thomas J. Lobl , Bradley R. Teegarden , Alexander Polinsky , Gilbert M. Rishton , Masafumi Yamagishi , Steven Tanis , Jed F. Fisher , Edward W. Thomas , Robert A. Chrusciel
IPC分类号： A61K31415
CPC分类号： C07D213/81 , C07C229/46 , C07C233/60 , C07C233/63 , C07C233/83 , C07C233/87 , C07C235/40 , C07C235/64 , C07C235/84 , C07C237/22 , C07C237/40 , C07C237/42 , C07C255/29 , C07C255/46 , C07C259/08 , C07C271/22 , C07C271/28 , C07C275/26 , C07C275/42 , C07C311/21 , C07C311/64 , C07D207/16 , C07D209/20 , C07D213/64 , C07D213/82 , C07D217/26 , C07D233/64 , C07D295/185 , C07D295/192 , C07D307/68 , C07D333/24
摘要： The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.
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9.发明授权Substituted tetronic acids useful for treating HIV and other retroviruses 失效用于治疗HIV和其他逆转录病毒的替代的tetronic酸
公开(公告)号：US5977169A
公开(公告)日：1999-11-02
申请号：US604937
申请日：1997-07-28
申请人： Robert A. Chrusciel , Linda L. Maggiora , Suvit Thaisrivongs , James M. Tustin , Clark W. Smith , Ruben A. Tommasi , Paul A. Aristoff , Harvey I. Skulnick , W. Jeffrey Howe , Gordon L. Bundy
发明人： Robert A. Chrusciel , Linda L. Maggiora , Suvit Thaisrivongs , James M. Tustin , Clark W. Smith , Ruben A. Tommasi , Paul A. Aristoff , Harvey I. Skulnick , W. Jeffrey Howe , Gordon L. Bundy
IPC分类号： C07D307/33 , A61K31/34 , A61K31/341 , A61K31/41 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/47 , A61P31/12 , C07D307/60 , C07D307/94 , C07D405/06 , C07D405/12 , C07D417/12 , C07D473/00 , C07D491/10 , C07D491/107 , A61K31/335 , A61K31/505
CPC分类号： C07D405/06 , C07D307/60 , C07D307/94 , C07D405/12 , C07D417/12 , C07D473/00 , C07D491/10
摘要： This invention comprises novel substituted tetronic acid type compounds, 2, 4(3H, 5H)-furandiones, that are useful for the inhibition of the HIV protease enzyme. The compounds may be useful for the treatment of a person with AIDS or AIDS related diseases. The compounds may be used in the attempt to retard the further replication of any retrovirus containing the aspartyl protease enzyme. Compounds are represented by the formula below. ##STR1##
摘要翻译： PCT No.PCT / US94 / 09533 Sec。 371日期1997年7月28日第 102（e）日期1997年7月28日PCT 1994年9月7日PCT PCT。 公开号WO95 / 07901 日期1995年3月23日本发明包括可用于抑制HIV蛋白酶的新型取代的tetronic酸型化合物2,4（3H，5H） - 呋喃二酮。 该化合物可用于治疗患有AIDS或AIDS相关疾病的人。 可以使用这些化合物来试图阻止含有天冬氨酰蛋白酶的任何逆转录病毒的进一步复制。 化合物由下式表示。
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