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1. 发明申请

US20110105483A1 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：US20110105483A1
公开(公告)日：2011-05-05
申请号：US12526491
申请日：2008-02-08
申请人： Dinesh U. Chimmanamada , Joseph A. Burlison , Weiwen Ying , Lijun Sun , Stefan Michael Schweizer , Shijie Zhang , Zachary Demko , David James , Teresa Przewloka
发明人： Dinesh U. Chimmanamada , Joseph A. Burlison , Weiwen Ying , Lijun Sun , Stefan Michael Schweizer , Shijie Zhang , Zachary Demko , David James , Teresa Przewloka
IPC分类号： A61K31/4196 , C07D403/10 , C07D403/14 , C07D413/10 , C07D413/14 , C07D417/10 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P37/00 , A61P31/10 , A61P7/00
CPC分类号： C07D417/14 , C07D249/08 , C07D249/10 , C07D249/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/12
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperprolif erative disorders, such as cancer, in a subject in need thereof.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及本发明的取代的三唑化合物或包含这种化合物的组合物在制备用于预防或治疗有需要的受试者中的多药耐药性疾病如癌症的药物中的用途。

2. 发明授权

US08299107B2 Triazole compounds that modulate HSP90 activity 有权
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：US08299107B2
公开(公告)日：2012-10-30
申请号：US12526491
申请日：2008-02-08
申请人： Dinesh U. Chimmanamada , Joseph A. Burlison , Weiwen Ying , Lijun Sun , Stefan Michael Schweizer , Shijie Zhang , Zachary Demko , David James , Teresa K. Przewloka
发明人： Dinesh U. Chimmanamada , Joseph A. Burlison , Weiwen Ying , Lijun Sun , Stefan Michael Schweizer , Shijie Zhang , Zachary Demko , David James , Teresa K. Przewloka
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D417/14 , C07D249/08 , C07D249/10 , C07D249/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/12
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及本发明的取代的三唑化合物或包含这种化合物的组合物在制备用于预防或治疗有需要的受试者中的过度增殖性疾病如癌症的药物中的用途。

3. 发明申请

US20120046288A1 Hydrazonamide Compounds That Modulate Hsp90 Activity 有权
标题翻译：调节Hsp90活性的肼腙化合物
公开(公告)号：US20120046288A1
公开(公告)日：2012-02-23
申请号：US13001255
申请日：2009-06-26
申请人： Joseph A. Burlison , Dinesh U. Chimmanamada , Weiwen Ying , Shijie Zhang , David James
发明人： Joseph A. Burlison , Dinesh U. Chimmanamada , Weiwen Ying , Shijie Zhang , David James
IPC分类号： A61K31/5377 , C07D295/155 , C07D317/66 , A61P35/00 , C07D405/12 , A61K31/535 , A61K31/36 , A61K31/4525 , C07D413/04 , C07D317/58
CPC分类号： C07C257/22 , C07D213/74 , C07D317/58 , C07D317/66
摘要： The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hsρ90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
摘要翻译：本发明涉及取代的酰胺化合物。本发明还涉及在有需要的受试者中抑制Hs＆gt; 90的活性的方法以及在有需要的受试者中治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的酰胺化合物，或包含这种化合物的药物组合物。

4. 发明申请

US20100113447A1 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：US20100113447A1
公开(公告)日：2010-05-06
申请号：US12538751
申请日：2009-08-10
申请人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan M. Schweizer
发明人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan M. Schweizer
IPC分类号： A61K31/4196 , C07D403/10 , C07D413/10 , C07D403/14 , C07D249/10 , C12N5/00 , A61P35/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00 , A61P29/00 , A61P37/00 , A61K31/496 , A61K31/5377
CPC分类号： A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/635 , A61K45/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/08 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/12
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的三唑化合物或包含这种化合物的药物组合物。

5. 发明授权

US08106083B2 Triazole compounds that modulate HSP90 activity 有权
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：US08106083B2
公开(公告)日：2012-01-31
申请号：US12538751
申请日：2009-08-10
申请人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan M. Schweizer
发明人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan M. Schweizer
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/635 , A61K45/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/08 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/12
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的三唑化合物或包含这种化合物的药物组合物。

6. 发明申请

US20110224206A1 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：US20110224206A1
公开(公告)日：2011-09-15
申请号：US13057962
申请日：2009-08-07
申请人： Weiwen Ying , Dinesh U. Chimmanamada , Joseph A. Burlison , Shijie Zhang , Minghu Song , Junghyun Chae
发明人： Weiwen Ying , Dinesh U. Chimmanamada , Joseph A. Burlison , Shijie Zhang , Minghu Song , Junghyun Chae
IPC分类号： A61K31/5377 , C07D249/10 , C07D413/14 , C07D401/10 , C12N5/071 , A61K31/4196 , A61K31/4709 , A61P35/00 , A61P31/00 , A61P29/00 , A61P35/02
CPC分类号： C07D249/10 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to substituted pyrrole compounds of formula I and compositions comprising substituted tri-substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a tri-substituted’ triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
摘要翻译：本发明涉及式I的取代吡咯化合物和包含取代的三取代三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中治疗过度增殖性疾病例如癌症的方法，其包括向受试者施用本发明的三取代的“三唑化合物，或包含这种化合物的药物组合物。

7. 发明授权

US08486932B2 Triazole compounds that modulate Hsp90 activity 有权
标题翻译：三唑化合物调节Hsp90活性
公开(公告)号：US08486932B2
公开(公告)日：2013-07-16
申请号：US13333191
申请日：2011-12-21
申请人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan Schweizer
发明人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan Schweizer
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/635 , A61K45/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/08 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/12
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的三唑化合物或包含这种化合物的药物组合物。

8. 发明申请

US20120101072A1 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 有权
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：US20120101072A1
公开(公告)日：2012-04-26
申请号：US13333191
申请日：2011-12-21
申请人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan M. Schweizer
发明人： Joseph A. Burlison , Shijie Zhang , Weiwen Ying , Dinesh U. Chimmanamada , Minghu Song , Junghyun Chae , Stefan M. Schweizer
IPC分类号： A61K31/4196 , C07D413/14 , C07D417/14 , C07D405/10 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/454 , A61K31/635 , C07D403/10 , C07D413/10
CPC分类号： A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/635 , A61K45/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/08 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/12
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的三唑化合物或包含这种化合物的药物组合物。

9. 发明申请

US20080125587A1 Synthesis of triazole compounds that modulate HSP90 activity 审中-公开
标题翻译：合成调节HSP90活性的三唑化合物
公开(公告)号：US20080125587A1
公开(公告)日：2008-05-29
申请号：US11807333
申请日：2007-05-25
申请人： Dinesh U. Chimmanamada , Chi-Wan Lee , David James , Shijie Zhang , Weiwen Ying , Junghyun Chae , Teresa Przewloka
发明人： Dinesh U. Chimmanamada , Chi-Wan Lee , David James , Shijie Zhang , Weiwen Ying , Junghyun Chae , Teresa Przewloka
IPC分类号： C07D249/12 , C07D407/02 , C07D403/02 , C07D401/02 , C07D401/04 , C07D403/10 , C07D417/02 , C07D487/04 , C07D413/12 , C07D413/02
CPC分类号： C07D403/04 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/10 , C07D403/10 , C07D413/04 , C07D417/04
摘要： The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent.In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) with an oxidizing agent, thereby producing a compound of formula (IA).The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
摘要翻译：本发明提供抑制Hsp90活性的三唑化合物的新方法。本发明的一个实施方案涉及制备由以下结构式表示的三唑化合物或互变异构体，药学上可接受的盐，溶剂化物或包合物或其前药的方法，其包括以下步骤：a）使酰胺由以下结构式表示：用硫化试剂形成硫代酰胺; b）使步骤a）的硫代酰胺与肼反应形成腙酰胺; c）使步骤b）的腙与羰基化或硫代羰基化试剂反应。在一个实施方案中，本发明是合成式（IA）化合物或互变异构体，其药学上可接受的盐，溶剂化物或包合物或其前药的方法，包括使式（IIA）化合物与氧化剂，从而制备式（IA）化合物。本发明还涉及制备由以下结构式表示的化合物或其互变异构体的方法：或其互变异构体，药学上可接受的盐，溶剂化物或包合物或其前药。该方法包括使由以下结构式表示的第一起始化合物在汞盐存在下与由以下结构式表示的第二起始化合物反应的步骤：

10. 发明授权

US08901308B2 Triazole compounds that modulate Hsp90 activity 有权
标题翻译：调节Hsp90活性的三唑化合物
公开(公告)号：US08901308B2
公开(公告)日：2014-12-02
申请号：US13550324
申请日：2012-07-16
申请人： Weiwen Ying , David James , Shijie Zhang , Teresa Przewloka , Junghyun Chae , Dinesh U. Chimmanamada , Chi-Wan Lee , Elena Kostik , Howard P. Ng , Kevin Foley , Zhenjian Du , James Barsoum
发明人： Weiwen Ying , David James , Shijie Zhang , Teresa Przewloka , Junghyun Chae , Dinesh U. Chimmanamada , Chi-Wan Lee , Elena Kostik , Howard P. Ng , Kevin Foley , Zhenjian Du , James Barsoum
IPC分类号： C07D401/04 , C07D405/04 , C07D417/04 , C07D413/04 , C07D403/04 , C07D403/10 , C07D249/08 , C07D473/00 , C07D249/12 , C07D409/04 , C07D473/34
CPC分类号： C07D249/08 , A61K31/4196 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D473/00 , C07D473/34
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中预防或治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的三唑化合物，或包含这种化合物的组合物。

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