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1. 发明申请

WO2015066053A3 TARGETED THERAPEUTICS 审中-公开
标题翻译：目标治疗
公开(公告)号：WO2015066053A3
公开(公告)日：2015-11-19
申请号：PCT/US2014062689
申请日：2014-10-28
申请人： SYNTA PHARMACEUTICALS CORP
发明人： CHIMMANAMADA DINESH U , YING WEIWEN
IPC分类号： A61K47/48
CPC分类号： A61K47/48061 , A61K47/545 , A61K49/00
摘要： The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
摘要翻译：本发明提供了药理学化合物，其包括与结合部分缀合的效应部分，所述结合部分将效应部分引导至感兴趣的生物学靶标。同样地，本发明提供包含所述化合物的组合物，试剂盒和方法（例如，治疗，诊断和成像）。这些化合物可以描述为蛋白质相互作用的结合部分 - 药物缀合物（SDC-TRAP）化合物，其包括蛋白质相互作用的结合部分和效应器部分。例如，在涉及治疗癌症的某些实施方案中，SDC-TRAP可以包括与作为效应器模块的细胞毒剂缀合的Hsp90抑制剂。

2. 发明申请

WO2009158026A1 HYDRAZONAMIDE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
标题翻译：调节HSP90活性的水合肼化合物
公开(公告)号：WO2009158026A1
公开(公告)日：2009-12-30
申请号：PCT/US2009003825
申请日：2009-06-26
申请人： SYNTA PHARMACEUTICALS CORP , BURLISON JOSEPH A , CHIMMANAMADA DINESH U , YING WEIWEN , ZHANG SHIJIE , JAMES DAVID
发明人： BURLISON JOSEPH A , CHIMMANAMADA DINESH U , YING WEIWEN , ZHANG SHIJIE , JAMES DAVID
IPC分类号： C07C257/22 , A61K31/36 , A61K31/444 , A61K31/5377 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D213/74 , C07D317/58 , C07D317/66
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 Hs?90 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≥90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酰胺化合物，或包含这种化合物的药物组合物。

3. 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.

4. 发明申请

WO2013158644A2 TARGETED THERAPEUTICS 审中-公开
标题翻译：目标治疗
公开(公告)号：WO2013158644A2
公开(公告)日：2013-10-24
申请号：PCT/US2013036783
申请日：2013-04-16
申请人： SYNTA PHARMACEUTICALS CORP
发明人： CHIMMANAMADA DINESH U , YING WEIWEN
IPC分类号： A61K47/48
CPC分类号： A61K31/565 , A61K31/167 , A61K31/185 , A61K31/4184 , A61K31/4196 , A61K31/437 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/58 , A61K31/704 , A61K47/54 , A61K47/545 , A61K47/55 , G01N33/57496
摘要： The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
摘要翻译：本发明提供药物化合物，其包括与将效应子部分指向感兴趣的生物靶标的结合部分缀合的效应部分。同样，本发明提供包括化合物的组合物，试剂盒和方法（例如治疗，诊断和成像）。该化合物可被描述为蛋白质相互作用结合部分 - 药物偶联物（SDC-TRAP）化合物，其包括蛋白质相互作用结合部分和效应部分。例如，在针对治疗癌症的某些实施方案中，SDC-TRAP可包括与细胞毒性剂缀合的Hsp90抑制剂作为效应部分。

5. 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。

6. 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。

7. 发明申请

WO2015134464A3 TARGETED THERAPEUTICS 审中-公开
公开(公告)号：WO2015134464A3
公开(公告)日：2015-10-29
申请号：PCT/US2015018442
申请日：2015-03-03
申请人： SYNTA PHARMACEUTICALS CORP
发明人： CHIMMANAMADA DINESH U , YING WEIWEN
IPC分类号： A61K47/48
CPC分类号： A61K47/48061 , A61K31/4196 , A61K31/454 , A61K31/4745 , A61K31/496 , A61K31/519 , A61K31/58 , A61K31/706 , A61K47/545 , A61K47/55
摘要： The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

8. 发明申请

WO2015066053A8 TARGETED THERAPEUTICS 审中-公开
公开(公告)号：WO2015066053A8
公开(公告)日：2015-06-04
申请号：PCT/US2014062689
申请日：2014-10-28
申请人： SYNTA PHARMACEUTICALS CORP
发明人： CHIMMANAMADA DINESH U , YING WEIWEN
IPC分类号： A61K47/48
CPC分类号： A61K47/48061 , A61K47/545 , A61K49/00
摘要： The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

9. 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。

10. 发明申请

WO2009075890A3 METHOD FOR SYNTHESIS OF TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
标题翻译：合成调节HSP90活性的三唑化合物的方法
公开(公告)号：WO2009075890A3
公开(公告)日：2009-08-13
申请号：PCT/US2008013671
申请日：2008-12-12
申请人： SYNTA PHARMACEUTICALS CORP , CHIMMANAMADA DINESH U , ZHANG SHIJE , LEE CHI-WAN , PRZEWLOKA TERESA , YING WEIWEN
发明人： CHIMMANAMADA DINESH U , ZHANG SHIJE , 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：本发明提供了合成抑制Hsp90活性的化合物的新方法。在一个实施方案中，本发明是式（IA）化合物在碱/溶剂中环化式（II）化合物的合成方法，由此产生式（IA）化合物。本文提供了取代基的定义和反应条件。

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