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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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92.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：US20100331287A1
公开(公告)日：2010-12-30
申请号：US12225756
申请日：2007-03-30
申请人： John J. Baldwin , David A. Claremon , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wenguang Zeng
发明人： John J. Baldwin , David A. Claremon , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wenguang Zeng
IPC分类号： A61K31/416 , C07D231/56 , A61P9/00 , A61K31/496 , A61K31/4418 , A61K31/495 , A61K31/554 , A61K31/549 , A61K31/55 , A61K31/4184 , A61K31/58
CPC分类号： C07D231/56
摘要： 6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients.
摘要翻译： 式（I）的6-（氨基烷基）吲唑及其盐具有肾素抑制性质，可用作抗高血压药和肾，心脏和血管保护的药物活性成分。
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公开(公告)号：US07858624B2
公开(公告)日：2010-12-28
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： A61K31/5355 , A61K31/4402 , A61K31/4525 , A61K31/445 , C07D411/12 , C07D213/30 , C07D403/12 , C07D405/12 , C07D401/12 , C07D211/22
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：US20100298328A1
公开(公告)日：2010-11-25
申请号：US12225757
申请日：2007-03-30
申请人： John J. Baldwin , David A. Claremon , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wenguang Zeng
发明人： John J. Baldwin , David A. Claremon , Lawrence W. Dillard , Alexey V. Ishchenko , Jing Yuan , Zhenrong Xu , Gerard McGeehan , Wenguang Zeng
IPC分类号： A61K31/135 , C07C225/20 , A61K31/137 , C07D211/32 , A61K31/451 , C07D295/135 , A61K31/5375 , A61K31/495 , C07C233/41 , A61K31/165 , C07D207/09 , A61K31/40 , C07D413/12 , A61K31/5377 , C07D285/10 , A61K31/433 , A61P9/12 , A61P9/00 , A61P27/02 , A61P27/06 , A61P25/00
CPC分类号： C07C225/20 , C07C233/36 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07D207/06 , C07D211/14 , C07D213/38 , C07D285/10 , C07D295/116 , C07D295/135
摘要： 1-Heterocyclylamino-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-杂环氨基-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：US20100184805A1
公开(公告)日：2010-07-22
申请号：US12665208
申请日：2008-06-20
申请人： John J. Baldwin , Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Alexey V. Ishchenko , Lanqi Jia , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Jing Yuan , Wei Zhao
发明人： John J. Baldwin , Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Patrick T. Flaherty , Alexey V. Ishchenko , Lanqi Jia , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Jing Yuan , Wei Zhao
IPC分类号： A61K31/454 , C07D211/32 , C07D401/12 , C07D405/12 , A61K31/453 , A61K31/4545 , A61K31/445 , A61P43/00
CPC分类号： C07D211/16 , C07D401/12
摘要： Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient.
摘要翻译： 公开了由以下结构式表示的天冬氨酸蛋白酶抑制剂及其药学上可接受的盐。 这些化合物是口服活性的，并结合天冬氨酸蛋白酶抑制其活性。 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。 本发明还涉及包含本文所述化合物或其对映异构体，非对映体或其盐和药学上可接受的载体或赋形剂的药物组合物。
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公开(公告)号：US20100144825A1
公开(公告)日：2010-06-10
申请号：US12665219
申请日：2008-06-20
申请人： John J. Baldwin , Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Patrick T. Fiaherty , Alexey V. Ishchenko , Lanqi Jia , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Jing Yuan , Wei Zhao , Linghang Zhuang
发明人： John J. Baldwin , Salvacion Cacatian , David A. Claremon , Lawrence W. Dillard , Patrick T. Fiaherty , Alexey V. Ishchenko , Lanqi Jia , Gerard McGeehan , Robert D. Simpson , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Jing Yuan , Wei Zhao , Linghang Zhuang
IPC分类号： A61K31/4035 , C07C271/10 , C07D209/46 , A61K31/24 , A61P31/18
CPC分类号： C07C275/24 , C07C275/14 , C07C275/16 , C07C2601/14 , C07C2603/74 , C07D209/46 , C07D309/04 , C07D311/96 , C07D313/04
摘要： The present invention is directed to aspartic protease inhibitors. 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：US20090318501A1
公开(公告)日：2009-12-24
申请号：US12311020
申请日：2007-09-17
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： A61K31/445 , C07D405/12 , C07D315/00
CPC分类号： 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：US5451578A
公开(公告)日：1995-09-19
申请号：US289974
申请日：1994-08-12
IPC分类号： C07D221/20 , C07D471/10 , A61K31/55
CPC分类号： C07D221/20 , C07D471/10
摘要： Compounds of the invention have the formula: ##STR1## which have fibrinogen receptor antagonist activity, including, for example, ##STR2##
摘要翻译： 本发明的化合物具有下式：具有纤维蛋白原受体拮抗剂活性的
，包括例如 -
100.发明授权Substituted diazapines and derivatives thereof useful in the treatment of cardiovascular disorders 失效用于治疗心血管疾病的取代的二氮嗪及其衍生物
公开(公告)号：US4677102A
公开(公告)日：1987-06-30
申请号：US827035
申请日：1986-02-07
IPC分类号： C07D243/04 , A61K31/55
CPC分类号： C07D243/04
摘要： There are disclosed novel diazapines and derivatives thereof which are useful in the treatment of cardiovascular disorders.
摘要翻译： 公开了可用于治疗心血管疾病的新型二氮平及其衍生物。
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