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41.Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 失效
标题翻译: 哌啶基氨基甲酸酯中间体用于合成天冬氨酸蛋白酶抑制剂公开(公告)号:US08487108B2
公开(公告)日:2013-07-16
申请号:US12084928
申请日:2006-11-13
申请人: John J. Baldwin , David A. Claremon , Colin Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Wei Zhao , Patrick T. Flaherty
发明人: John J. Baldwin , David A. Claremon , Colin Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Wei Zhao , Patrick T. Flaherty
IPC分类号: C07D211/22 , C07D211/60
CPC分类号: C07D211/26 , C07D211/22 , C07D401/12 , C07D407/12 , C07D409/06 , C07D417/06 , Y02P20/55
摘要: The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
摘要翻译: 本发明涉及天冬氨酸蛋白酶抑制剂。 本发明的某些天冬氨酸蛋白酶抑制剂可以由以下结构式表示或其药学上可接受的盐。 本发明还涉及包含所公开的天冬氨酸蛋白酶抑制剂的药物组合物。 本发明还涉及在有需要的受试者中拮抗一种或多种天冬氨酸蛋白酶的方法,以及使用所公开的天冬氨酸蛋白酶抑制剂治疗受试者中天冬氨酸蛋白酶介导的病症的方法。
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公开(公告)号:US20140200223A1
公开(公告)日:2014-07-17
申请号:US14132877
申请日:2013-12-18
申请人: Salvacion Cacatian , David A. Claremon , Lawrence Wayne Dillard , Klaus Fuchs , Niklas Heine , Lanqi Jia , Katerina Leftheris , Brian Mckeever , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Guosheng Wu , Zhongren Wu , Zhenrong Xu , Jing Yuan , Yajun Zheng
发明人: Salvacion Cacatian , David A. Claremon , Lawrence Wayne Dillard , Klaus Fuchs , Niklas Heine , Lanqi Jia , Katerina Leftheris , Brian Mckeever , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Guosheng Wu , Zhongren Wu , Zhenrong Xu , Jing Yuan , Yajun Zheng
IPC分类号: C07D271/12 , C07D239/70 , C07D403/06 , C07D498/10 , C07D417/06 , C07D405/06 , C07D413/04 , C07D233/46
CPC分类号: C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
摘要: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
摘要翻译: 本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。 还描述了化合物的药物组合物和使用方法。
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公开(公告)号:US08633212B2
公开(公告)日:2014-01-21
申请号:US12723137
申请日:2010-03-12
申请人: Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Klaus Fuchs , Niklas Heine , Lanqi Jia , Katerina Leftheris , Brian McKeever , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Guosheng Wu , Zhongren Wu , Zhenrong Xu , Jing Yuan , Yajun Zheng
发明人: Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Klaus Fuchs , Niklas Heine , Lanqi Jia , Katerina Leftheris , Brian McKeever , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Guosheng Wu , Zhongren Wu , Zhenrong Xu , Jing Yuan , Yajun Zheng
IPC分类号: A61K31/405 , A61K31/415 , A61K31/41 , A61K31/40 , C07D237/00 , C07D271/10 , C07D487/10 , C07D209/54
CPC分类号: C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
摘要: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
摘要翻译: 本发明涉及由以下结构式表示的化合物或其药学上可接受的盐。 还描述了化合物的药物组合物和使用方法。
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公开(公告)号:US20100179109A1
公开(公告)日:2010-07-15
申请号:US12450631
申请日:2008-04-04
申请人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Colin A. Leach , Qing Lu , Gerard McGeehan , Jaclyn R. Patterson , Robert D. Simpson , Suresh B. Singh , Patrick Stoy , Lamont R. Terrell , Colin Tice , Zhenrong Xu , Jing Yuan , Catherine C. K. Yuan , Jing Zhang , Wei Zhao
发明人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Colin A. Leach , Qing Lu , Gerard McGeehan , Jaclyn R. Patterson , Robert D. Simpson , Suresh B. Singh , Patrick Stoy , Lamont R. Terrell , Colin Tice , Zhenrong Xu , Jing Yuan , Catherine C. K. Yuan , Jing Zhang , Wei Zhao
IPC分类号: A61K31/675 , C07D211/34 , A61K31/445 , C07D265/30 , A61K31/5375 , C07D413/06 , A61K31/5377 , A61K31/535 , A61K31/517 , A61K31/554 , A61K31/4965 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/47 , A61K31/566 , A61P25/28 , A61P33/06 , A61P31/18 , A61P9/12 , A61P9/10 , A61P25/22 , A61P27/06
CPC分类号: C07D211/96 , C07D211/22 , C07D401/10 , C07D401/12
摘要: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译: 公开了式(I)的化合物,其中R,R 1,R 2,R 3,X,Y,A,Q,E和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性,并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。
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公开(公告)号:US20100130471A1
公开(公告)日:2010-05-27
申请号:US12450619
申请日:2008-04-04
申请人: John J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiamo Ghirlanda , Xiaoping Hou , Alexey V. Ishebenko , Lara S. Kallander , Beth A. Knapp-Reed , Brian Lawhorn , Qing Lu , Gerard McGeehan , Simon Semus , Robert D. Simpson , Suresh B. Singh , Lamont R. Terrell , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Jing Zhang , Wei Zhao
发明人: John J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiamo Ghirlanda , Xiaoping Hou , Alexey V. Ishebenko , Lara S. Kallander , Beth A. Knapp-Reed , Brian Lawhorn , Qing Lu , Gerard McGeehan , Simon Semus , Robert D. Simpson , Suresh B. Singh , Lamont R. Terrell , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Jing Zhang , Wei Zhao
IPC分类号: A61K31/445 , A61K31/554 , A61K31/55 , A61K31/551 , A61K31/549 , A61K31/5377 , A61K31/5375 , A61K31/4545 , C07D417/12 , C07D265/30 , C07D401/06 , C07D401/10 , C07D211/34 , A61P25/00 , A61P9/12 , A61P9/10
CPC分类号: C07D401/06 , C07D211/22 , C07D265/30
摘要: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译: 描述了结合天冬氨酸蛋白酶抑制其活性的化合物。 它们可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还描述了本文所述化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。
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公开(公告)号:US20100280005A1
公开(公告)日:2010-11-04
申请号:US12450620
申请日:2008-04-04
申请人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , John Gleason , Alexey V. Ishchenko , Brian Lawhorn , Gerard McGeehan , Jaclyn R. Patterson , Simon F. Semus , Robert D. Simpson , Suresh B. Singh , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Wei Zhao
发明人: Jonh J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , John Gleason , Alexey V. Ishchenko , Brian Lawhorn , Gerard McGeehan , Jaclyn R. Patterson , Simon F. Semus , Robert D. Simpson , Suresh B. Singh , Colin Tice , Tritin Tran , Zhenrong Xu , Jing Yuan , Wei Zhao
IPC分类号: A61K31/445 , C07D211/60 , C07D401/02 , C07D413/02 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/58 , A61P9/12
CPC分类号: C07D211/22 , C07D401/06
摘要: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译: 公开了式I的化合物,其中R,R 1,R 2,R 3,X,Y,A,Q,E和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性,并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。
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47.1-Acylamino-2-Hydroxy-3-Amino- -Arylalkanes as Renin Inhibitors 审中-公开
标题翻译: 1-酰基氨基-2-羟基-3-氨基 - 丙烯醛作为肾素抑制剂公开(公告)号:US20080293701A1
公开(公告)日:2008-11-27
申请号:US11883518
申请日:2006-02-01
申请人: John J. Baldwin , David A. Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wenguang Zeng , Salvacion Cacatian , Colin Tice , Robert D. Simpson , Wei Zhao
发明人: John J. Baldwin , David A. Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wenguang Zeng , Salvacion Cacatian , Colin Tice , Robert D. Simpson , Wei Zhao
IPC分类号: A61K31/546 , C07C233/62 , A61K31/164 , A61K31/4453 , C07D211/60 , A61K31/145 , C07C381/00 , A61P9/12 , A61P9/00
CPC分类号: C07D263/04 , C07C233/36 , C07C233/62 , C07C275/24 , C07C307/06 , C07C311/13 , C07C2601/14 , C07D263/06 , C07D263/22 , C07D295/215 , C07D303/36
摘要: 1-Acylamino-2-hydroxy-3-amino-ω-arylalkanes of formula I. and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.
摘要翻译: 式I的1-酰基氨基-2-羟基-3-氨基-ω-芳基烷烃及其盐具有肾素抑制性质,可用作抗高血压药物活性成分。
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公开(公告)号:US09018391B2
公开(公告)日:2015-04-28
申请号:US14011183
申请日:2013-08-27
申请人: Yuri Bukhtiyarov , Salvacion Cacatian , Lawrence Wayne Dillard , Klaus Fuchs , Lanqi Jia , Deepak S. Lala , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Zhenrong Xu , Jing Yuan , Yi Zhao , Yajun Zheng , Cornelia Dorner-Ciossek , Ulrike Gross , Niklas Heine , Achim Sauer
发明人: Yuri Bukhtiyarov , Salvacion Cacatian , Lawrence Wayne Dillard , Klaus Fuchs , Lanqi Jia , Deepak S. Lala , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Zhenrong Xu , Jing Yuan , Yi Zhao , Yajun Zheng , Cornelia Dorner-Ciossek , Ulrike Gross , Niklas Heine , Achim Sauer
IPC分类号: C07D235/02 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D401/14 , A61K31/4184
CPC分类号: C07D235/02 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/59 , C07C313/06 , C07C331/26 , C07C2603/94 , C07C2603/97 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06
摘要: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
摘要翻译: 本发明涉及螺环酰基胍及其作为分泌酶(BACE1)活性的抑制剂,含有它们的药物组合物的用途,以及将其用作治疗神经变性疾病的治疗剂的方法,其特征在于认知 衰退,认知障碍,痴呆和以淀粉样蛋白聚集体生产为特征的疾病。
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公开(公告)号:US20140057927A1
公开(公告)日:2014-02-27
申请号:US14011183
申请日:2013-08-27
申请人: Yuri Bukhtiyarov , Salvacion Cacatian , Lawrence Wayne Dillard , Klaus Fuchs , Lanqi Jia , Deepak S. Lala , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Zhenrong Xu , Jing Yuan , Yi Zhao , Yajun Zheng , Cornelia Dorner-Ciossek , Ulrike Gross , Niklas Heine , Achim Sauer
发明人: Yuri Bukhtiyarov , Salvacion Cacatian , Lawrence Wayne Dillard , Klaus Fuchs , Lanqi Jia , Deepak S. Lala , Angel Morales-Ramos , Suresh B. Singh , Shankar Venkatraman , Zhenrong Xu , Jing Yuan , Yi Zhao , Yajun Zheng , Cornelia Dorner-Ciossek , Ulrike Gross , Niklas Heine , Achim Sauer
IPC分类号: C07D405/06 , C07D401/06 , C07D401/14 , C07D235/02 , C07D403/04
CPC分类号: C07D235/02 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/59 , C07C313/06 , C07C331/26 , C07C2603/94 , C07C2603/97 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06
摘要: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
摘要翻译: 本发明涉及螺环酰基胍及其作为β-分泌酶(BACE1)活性抑制剂的用途,含有它们的药物组合物及其用作治疗神经变性疾病的治疗剂的方法,其特征在于认知衰退 ,认知障碍,痴呆和以β-淀粉样蛋白聚集体生产为特征的疾病。
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公开(公告)号:US20100317697A1
公开(公告)日:2010-12-16
申请号:US12665217
申请日:2008-06-20
申请人: John J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Qing Lu , Gerard McGeehan , Beth A. Knapp-Reid , Simon Semus , Robert D. Simpson , Suresh B. Singh , Lamont R. Terrell , Colin Tice , Tritin Tran , Zherong Xu , Jing Yuan , Wei Zhao , Yongdong Y. Zhao
发明人: John J. Baldwin , Salvacion Cacatian , David Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Bahman Ghavimi-Alagha , Damiano Ghirlanda , Alexey V. Ishchenko , Lara S. Kallander , Brian Lawhorn , Qing Lu , Gerard McGeehan , Beth A. Knapp-Reid , Simon Semus , Robert D. Simpson , Suresh B. Singh , Lamont R. Terrell , Colin Tice , Tritin Tran , Zherong Xu , Jing Yuan , Wei Zhao , Yongdong Y. Zhao
IPC分类号: A61K31/445 , C07D211/06
CPC分类号: C07D211/22 , C07D265/30
摘要: Disclosed are compounds having the formula (I): wherein the R1, R2, R3, X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译: 公开了具有式(I)的化合物:其中R1,R2,R3,X,Y,A,L和G如本文所定义。 这些化合物与天冬氨酸蛋白酶结合以抑制其活性,并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。 还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。
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