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1. 发明申请

WO2007139952A3 METHOD FOR THE PREPARATION OF TRIAZOLE COMPOUNDS WITH HSP90 MODULATING ACTIVITY 审中-公开
标题翻译：用HSP90调节活性制备三唑化合物的方法
公开(公告)号：WO2007139952A3
公开(公告)日：2008-03-13
申请号：PCT/US2007012520
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP , LEE CHI-WAN , JAMES DAVID , ZHANG SHIJIE , YING WEIWEN , CHIMMANAMADA DINESH U , CHAE JUNGHYUN , PRZEWLOKA TERESA
发明人： LEE CHI-WAN , JAMES DAVID , ZHANG SHIJIE , YING WEIWEN , CHIMMANAMADA DINESH U , CHAE JUNGHYUN , PRZEWLOKA TERESA
IPC分类号： C07D249/12 , C07D249/14 , C07D403/04
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: (IB) 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: (HB) in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula: (IIIB).
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，溶剂合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，溶剂合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。本发明还涉及由以下结构式：（IB）或互变异构体，其药学上可接受的盐，溶剂合物或包合物或其前药代表的化合物或其互变异构体的制备方法。该方法包括使由以下结构式：（HB）表示的第一起始化合物在汞盐存在下与由以下结构式：（IIIB）表示的第二起始化合物反应的步骤。

2. 发明申请

WO2006055760A9 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：WO2006055760A9
公开(公告)日：2006-09-21
申请号：PCT/US2005041779
申请日：2005-11-17
申请人： SYNTA PHARMACEUTICALS CORP , YING WEIWEN , JAMES DAVID , ZHANG SHIJIE , PRZEWLOKA TERESA , CHAE JUNGHYUN , CHIMMANAMADA DINESH U , LEE CHI-WAN , KOSTIK ELENA , NG HOWARD P , FOLEY KEVIN , DU ZHENJIAN , BARSOUM JAMES
发明人： YING WEIWEN , JAMES DAVID , ZHANG SHIJIE , PRZEWLOKA TERESA , CHAE JUNGHYUN , CHIMMANAMADA DINESH U , LEE CHI-WAN , KOSTIK ELENA , NG HOWARD P , FOLEY KEVIN , DU ZHENJIAN , BARSOUM JAMES
IPC分类号： C07D249/12 , A61K31/4196 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04
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。

3. 发明申请

WO2007139955A2 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007139955A2
公开(公告)日：2007-12-06
申请号：PCT/US2007012524
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP , CHAE JUNGHYUN , DEMKO ZACHARY , YING WEIWEN , DU ZHENJIAN , FOLEY KEVIN , JAMES DAVID , PRZEWLOKA TERESA , SONG MINGHU , ZHANG SHIJIE , NG HOWARD P , LI HAO , CHIMMANAMADA DINESH U , ZHOU DAN , QIN SHUZHEN , LEE CHI-WAN , SUN LIJUN , KOYA KEIZO
发明人： CHAE JUNGHYUN , DEMKO ZACHARY , YING WEIWEN , DU ZHENJIAN , FOLEY KEVIN , JAMES DAVID , PRZEWLOKA TERESA , SONG MINGHU , ZHANG SHIJIE , NG HOWARD P , LI HAO , CHIMMANAMADA DINESH U , ZHOU DAN , QIN SHUZHEN , LEE CHI-WAN , SUN LIJUN , KOYA KEIZO
IPC分类号： A61K31/4196 , A61P31/00 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D417/04
CPC分类号： C07D417/04 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04
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.

4. 发明申请

WO2007139955A8 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007139955A8
公开(公告)日：2008-02-14
申请号：PCT/US2007012524
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP , CHAE JUNGHYUN , DEMKO ZACHARY , YING WEIWEN , DU ZHENJIAN , FOLEY KEVIN , JAMES DAVID , PRZEWLOKA TERESA , SONG MINGHU , ZHANG SHIJIE , NG HOWARD P , LI HAO , CHIMMANAMADA DINESH U , SUN LIJUN , KOYA KEIZO , ZHOU DAN , QIN SHUZHEN , LEE CHI-WAN
发明人： CHAE JUNGHYUN , DEMKO ZACHARY , YING WEIWEN , DU ZHENJIAN , FOLEY KEVIN , JAMES DAVID , PRZEWLOKA TERESA , SONG MINGHU , ZHANG SHIJIE , NG HOWARD P , LI HAO , CHIMMANAMADA DINESH U , SUN LIJUN , KOYA KEIZO , ZHOU DAN , QIN SHUZHEN , LEE CHI-WAN
IPC分类号： A61K31/4196 , A61P31/00 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D417/04
CPC分类号： C07D417/04 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04
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.

5. 发明申请

WO2007139967A2 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007139967A2
公开(公告)日：2007-12-06
申请号：PCT/US2007012543
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP , YING WEIWEN , PRZEWLOKA TERESA , CHAE JUNGHYUN , ZHANG SHIJIE , LI HAO , DU ZHENJIAN , JAMES DAVID , CHIMMANAMADA DINESH U , NG HOWARD P , FOLEY KEVIN , DEMKO ZACHARY , SUN LIJUN , ZHOU DAN , QIN SHUZHEN
发明人： YING WEIWEN , PRZEWLOKA TERESA , CHAE JUNGHYUN , ZHANG SHIJIE , LI HAO , DU ZHENJIAN , JAMES DAVID , CHIMMANAMADA DINESH U , NG HOWARD P , FOLEY KEVIN , DEMKO ZACHARY , SUN LIJUN , ZHOU DAN , QIN SHUZHEN
CPC分类号： C07D403/04 , A61K31/4196 , A61K31/422 , A61K31/4439 , A61K31/475 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D413/14 , C07D487/04
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.

6. 发明申请

WO2007094819A8 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007094819A8
公开(公告)日：2007-11-22
申请号：PCT/US2006032199
申请日：2006-08-17
申请人： SYNTA PHARMACEUTICALS CORP , YING WEIWEN , JAMES DAVIS , PRZEWLOKA TERESA , KOSTIK ELENA , CHAE JUNGHYUN , NG HOWARD P , DU ZHENJIAN , BARSOUM JAMES , CHIMMANAMADA DINESH U , LEE CHI-WAN , FOLEY KEVIN , ZHANG SHIJE
发明人： YING WEIWEN , JAMES DAVIS , PRZEWLOKA TERESA , KOSTIK ELENA , CHAE JUNGHYUN , NG HOWARD P , DU ZHENJIAN , BARSOUM JAMES , CHIMMANAMADA DINESH U , LEE CHI-WAN , FOLEY KEVIN , ZHANG SHIJE
CPC分类号： C07D249/08 , C07D403/10 , C07D403/12 , C07D413/12
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 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.

7. 发明申请

WO2007094819A3 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007094819A3
公开(公告)日：2008-01-24
申请号：PCT/US2006032199
申请日：2006-08-17
申请人： SYNTA PHARMACEUTICALS CORP , YING WEIWEN , JAMES DAVIS , PRZEWLOKA TERESA , KOSTIK ELENA , CHAE JUNGHYUN , NG HOWARD P , DU ZHENJIAN , BARSOUM JAMES , CHIMMANAMADA DINESH U , LEE CHI-WAN , FOLEY KEVIN , ZHANG SHIJE
发明人： YING WEIWEN , JAMES DAVIS , PRZEWLOKA TERESA , KOSTIK ELENA , CHAE JUNGHYUN , NG HOWARD P , DU ZHENJIAN , BARSOUM JAMES , CHIMMANAMADA DINESH U , LEE CHI-WAN , FOLEY KEVIN , ZHANG SHIJE
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00 , C07D403/10 , C07D403/12 , C07D413/12
CPC分类号： C07D249/08 , C07D403/10 , C07D403/12 , C07D413/12
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 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.

8. 发明申请

WO2009075890A8 METHOD FOR SYNTHESIS OF TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
标题翻译：用于合成改性HSP90活性的三唑化合物的方法
公开(公告)号：WO2009075890A8
公开(公告)日：2009-10-01
申请号：PCT/US2008013671
申请日：2008-12-12
申请人： SYNTA PHARMACEUTICALS CORP , CHIMMANAMADA DINESH U , ZHANG SHIJIE , LEE CHI-WAN , PRZEWLOKA TERESA , YING WEIWEN
发明人： CHIMMANAMADA DINESH U , ZHANG SHIJIE , LEE CHI-WAN , PRZEWLOKA TERESA , YING WEIWEN
IPC分类号： C07D249/12 , C07C281/06 , C07D249/14
CPC分类号： C07D249/12 , C07C327/56 , C07C381/00 , C07D249/14
摘要： The present invention provides novel method of synthesis of compounds which inhibit the activity of Hsp90. In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) cyclization of a compound of formula (II): in a base/solvent, thereby producing a compound of formula (IA). The definition of the substituents and the conditions of the reactions are provided herein.
摘要翻译：本发明提供了抑制Hsp90活性的化合物的合成新方法。在一个实施方案中，本发明是在碱/溶剂中合成式（II）化合物的式（ⅠA）化合物的方法，由此制备式（IA）化合物。本文提供取代基的定义和反应的条件。

9. 发明申请

WO2008097640A8 TRIAZOLE COMPOUNDS THAT ARE USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS, SUCH AS CANCER 审中-公开
标题翻译：可用于治疗增殖性疾病（如癌症）的三唑化合物
公开(公告)号：WO2008097640A8
公开(公告)日：2008-11-13
申请号：PCT/US2008001693
申请日：2008-02-08
申请人： SYNTA PHARMACEUTICALS CORP , CHIMMANAMADA DINESH U , BURLISON JOSEPH A , YING WEIWEN , SUN LIJUN , SCHWEIZER STEFAN MICHAEL , ZHANG SHIJIE , DEMKO ZACHARY , JAMES DAVID , PRZEWLOKA TERESA
发明人： CHIMMANAMADA DINESH U , BURLISON JOSEPH A , YING WEIWEN , SUN LIJUN , SCHWEIZER STEFAN MICHAEL , ZHANG SHIJIE , DEMKO ZACHARY , JAMES DAVID , PRZEWLOKA TERESA
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00 , C07D249/10 , C07D249/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D417/14
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。

10. 发明申请

WO2008097640A2 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2008097640A2
公开(公告)日：2008-08-14
申请号：PCT/US2008001693
申请日：2008-02-08
申请人： SYNTA PHARMACEUTICALS CORP , CHIMMANAMADA DINESH U , BURLISON JOSEPH A , YING WEIWEN , SUN LIJUN , SCHWEIZER STEFAN MICHAEL , ZHANG SHIJIE , DEMKO ZACHARY , JAMES DAVID , PRZEWLOKA TERESA
发明人： CHIMMANAMADA DINESH U , BURLISON JOSEPH A , YING WEIWEN , SUN LIJUN , SCHWEIZER STEFAN MICHAEL , ZHANG SHIJIE , DEMKO ZACHARY , JAMES DAVID , PRZEWLOKA TERESA
IPC分类号： C07D249/08
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 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.

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