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公开(公告)号：US20120225906A1
公开(公告)日：2012-09-06
申请号：US13469562
申请日：2012-05-11
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： A61K31/453 , A61P3/04 , A61P9/12 , A61P9/04 , A61P9/00 , A61P25/28 , A61P25/00 , A61P27/02 , A61P27/06 , A61P5/42 , A61P25/22 , A61P13/12 , A61P9/10
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula: or a pharmaceutically acceptable salt thereof.The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I).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 these aspartic protease inhibitors are also disclosed.
摘要翻译： 本发明涉及由以下结构式表示的天冬氨酸蛋白酶抑制剂：或其药学上可接受的盐。 本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。 还公开了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，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。
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公开(公告)号：US20100048636A1
公开(公告)日：2010-02-25
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： A61K31/4523 , C07D211/78 , A61K31/445 , C07D405/02 , A61P9/00 , A61P9/12 , A61P9/10
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：US20090312369A1
公开(公告)日：2009-12-17
申请号：US12311012
申请日：2007-09-18
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： A61K31/453 , C07D405/12 , A61P9/10 , A61P9/12 , A61P9/04 , C07D315/00
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). 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 these aspartic protease inhibitors are also disclosed.
摘要翻译： 本发明涉及由以下结构式（I）表示的天冬氨酸蛋白酶抑制剂或其药学上可接受的盐。 本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。 还公开了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，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。
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公开(公告)号：US08580823B2
公开(公告)日：2013-11-12
申请号：US13469562
申请日：2012-05-11
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： A61K31/445
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula: or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I).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 these aspartic protease inhibitors are also disclosed.
摘要翻译： 本发明涉及由以下结构式表示的天冬氨酸蛋白酶抑制剂：或其药学上可接受的盐。 本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。 还公开了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，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。
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5.发明授权Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 失效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：US20090264432A1
公开(公告)日：2009-10-22
申请号：US12225986
申请日：2007-04-05
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh
IPC分类号： A61K31/5377 , C07D211/60 , A61K31/445 , C07D413/12
CPC分类号： C07D211/22 , C07D265/30
摘要： Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
摘要翻译： 描述的是具有口服活性并与肾素结合以抑制其活性的化合物。 它们可用于治疗或改善与肾素活性相关的疾病。 还描述了这些化合物用于治疗或改善受试者中肾素介导的病症的方法。
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公开(公告)号：US20090186884A1
公开(公告)日：2009-07-23
申请号：US12225985
申请日：2007-04-05
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty
IPC分类号： A61K31/5377 , C07D211/22 , A61K31/445 , A61K31/451 , C07D413/12 , A61P9/04 , A61P27/06 , A61P9/10
CPC分类号： C07D211/22 , C07D207/08 , C07D265/30 , C07D413/12
摘要： Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.
摘要翻译： 描述其二氨基丙醇是口服活性的并且结合肾素以抑制其活性。 它们可用于治疗或改善与升高的肾素活性水平或治疗天冬氨酸蛋白酶介导的疾病相关的疾病。 还描述了在有需要的受试者中使用二氨基丙醇来改善或治疗肾素相关疾病的方法。
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8.发明申请公开(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：US08455521B2
公开(公告)日：2013-06-04
申请号：US12802142
申请日：2010-05-28
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty , Jean-Pierre Wery
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Patrick T. Flaherty , Jean-Pierre Wery
IPC分类号： C07D417/04 , C07D409/06 , C07D405/06 , C07D401/06 , C07D417/06 , C07D265/30 , C07D211/22 , C07D211/26 , A61K31/5377 , A61K31/5375 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545
CPC分类号： C07D417/06 , C07C233/40 , C07C235/40 , C07C235/42 , C07C271/20 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D211/22 , C07D211/56 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/06 , C07F7/081 , C07F7/0812
摘要： Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
摘要翻译： 现已发现以下式I的二氨基烷烃是口服活性的并与天冬氨酸蛋白酶结合以抑制其活性：它们可用于治疗或改善与升高的天冬氨酸蛋白酶活性水平相关的疾病。 本发明还涉及在有需要的受试者中使用式I化合物来改善或治疗天冬氨酸蛋白酶相关病症的方法，包括向所述受试者施用有效量的式I化合物。
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公开(公告)号：US08198453B2
公开(公告)日：2012-06-12
申请号：US12311012
申请日：2007-09-18
申请人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
发明人： John J. Baldwin , David A. Claremon , Colin M. Tice , Salvacion Cacatian , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wei Zhao , Robert D. Simpson , Suresh B. Singh , Lanqi Jia , Patrick T. Flaherty
IPC分类号： C07D405/12 , A61K31/453
CPC分类号： C07D309/04 , C07D405/12
摘要： The present invention is directed to aspartic protease inhibitors represented by the following structural formula (I), or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the aspartic protease inhibitors of Structural Formula (I). 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 these aspartic protease inhibitors are also disclosed.
摘要翻译： 本发明涉及由以下结构式（I）表示的天冬氨酸蛋白酶抑制剂或其药学上可接受的盐。 本发明还涉及包含结构式（I）的天冬氨酸蛋白酶抑制剂的药物组合物。 还公开了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，以及使用这些天冬氨酸蛋白酶抑制剂治疗受试者天冬氨酸蛋白酶介导的病症的方法。
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