-
1.发明授权
公开(公告)号：US5840925A
公开(公告)日：1998-11-24
申请号：US759254
申请日：1996-12-02
申请人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
发明人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
IPC分类号： C07D493/18 , A61K31/352 , A61P35/00 , C07D519/00 , C07D321/02
CPC分类号： C07D519/00 , A61K47/481
摘要： Described herein are novel trioxane dimers of structure ##STR1## which possess antiproliferative and antitumor activities.
摘要翻译： 本文描述了具有抗增殖和抗肿瘤活性的结构“IMAGE”的新型三恶烷二聚体。
-
2.发明授权C-10 carbon-substituted artemisinin-like trioxane compounds having antimalarial, antiproliferative and antitumor activities 失效具有抗疟疾，抗增殖和抗肿瘤活性的C-10碳取代的青蒿素样三恶烷化合物
公开(公告)号：US6160004A
公开(公告)日：2000-12-12
申请号：US183693
申请日：1998-10-30
申请人： Gary H. Posner , Soon Hyung Woo , Poonsakdi Ploypradith , Michael H. Parker , Theresa A. Shapiro , Jeffrey S. Elias , John Northrop , Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh
发明人： Gary H. Posner , Soon Hyung Woo , Poonsakdi Ploypradith , Michael H. Parker , Theresa A. Shapiro , Jeffrey S. Elias , John Northrop , Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh
IPC分类号： C07D493/18 , A61K31/55 , A61K33/26 , A61P35/00 , A61P35/02 , C07D493/20 , C07D519/00 , C07F7/08 , C07F17/02 , A61K31/335
CPC分类号： C07D519/00 , A61K47/55 , C07D493/20
摘要： The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes; or when n is 3, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.
摘要翻译： 本发明提供了通过各种碳亲核试剂替代二氢青蒿素中的吡喃糖异头物10-OH基团的两步方法，得到新型C-10碳取代的三恶烷，其结构如下：其中当n为1时， R选自一组未取代或取代的芳基，杂芳基，聚乙二醇，乙炔基或苯甲酰基亚甲基，或烷酰基亚甲基; 或当n为2时，R选自一组未取代或取代的芳基，杂芳基，聚乙二醇，烯基，烷基，二酮或双 - 乙炔; 或当n为3时，R选自一组未取代或取代的芳基，杂芳基，聚乙二醇，烯基，烷基，二酮或双 - 炔。
-
3.发明授权
公开(公告)号：US6004997A
公开(公告)日：1999-12-21
申请号：US197944
申请日：1998-11-23
申请人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
发明人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
IPC分类号： C07D519/00 , A61K31/335
CPC分类号： C07D519/00
摘要： Novel trioxane dimers of structure ##STR1## which possess antiproliferative and antitumor activities.
摘要翻译： 具有抗增殖和抗肿瘤活性的新型三恶烷二聚体结构。
-
4.再颁专利公开(公告)号：USRE38117E1
公开(公告)日：2003-05-06
申请号：US09717815
申请日：2000-11-21
申请人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
发明人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
IPC分类号： C07D32102
CPC分类号： C07D519/00 , A61K47/55
摘要： Described herein are novel trioxane dimers of structure which possess antiproliferative and antitumor activities.
摘要翻译： 本文描述了具有抗增殖和抗肿瘤活性的新型三恶烷二聚体结构。
-
5.发明授权C-10 carbon-substituted artemisinin-like trioxane compounds having antimalarial, antiproliferative and antitumor activities 失效具有抗疟疾，抗增殖和抗肿瘤活性的C-10碳取代的青蒿素样三恶烷化合物
公开(公告)号：US6156790A
公开(公告)日：2000-12-05
申请号：US1242
申请日：1997-12-30
申请人： Gary H. Posner , Soon Hyung Woo , Poonsakdi Ploypradith , Michael H. Parker , Theresa A. Shapiro , Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh
发明人： Gary H. Posner , Soon Hyung Woo , Poonsakdi Ploypradith , Michael H. Parker , Theresa A. Shapiro , Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh
IPC分类号： C07D493/20 , C07D519/00 , A61K31/335 , C07D493/18
CPC分类号： C07D493/20 , C07D519/00
摘要： The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.
摘要翻译： 本发明提供了通过各种碳亲核试剂替代二氢青蒿素中的吡喃糖异头物10-OH基团的两步方法，得到新型C-10碳取代的三恶烷，其结构如下：其中当n为1时， R选自一组未取代或取代的芳基，杂芳基，聚乙二醇，乙炔基或苯甲酰基亚甲基，或烷酰基亚甲基; 或当n为2时，R选自未取代或取代的芳基，杂芳基，聚乙二醇，烯基，烷基，二酮或双 - 乙炔的一组。
-
6.发明授权Artemisinin analogs having antimalarial, antiproliferative, and antitumor activities and chemoselective methods of making the same 有权具有抗疟疾，抗增殖和抗肿瘤活性的青蒿素类似物和制备相同的化学选择性方法公开(公告)号：US06586464B2
公开(公告)日：2003-07-01
申请号：US09887922
申请日：2001-06-22
IPC分类号： C07D51900
CPC分类号： C07D493/18 , C07D519/00
摘要： Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is I and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.
摘要翻译： 本文描述了具有抗疟疾，抗增殖和抗肿瘤活性的新型青蒿素类似物和青蒿素二聚体的生产方法。 这些新型青蒿素类似物和青蒿素二聚体具有以下结构的非对映异构体，具有抗疟和抗增殖和抗肿瘤活性，其中当n为I时，本发明的单体形成，R为烷基，环烷基，杂烷基，杂环烷基，烯基，炔基 ，芳基或杂芳基。 本发明的二聚体在n为2时形成，R为包括但不限于烷基，环烷基，杂烷基，杂环烷基，烯基，炔基，芳基或杂芳基的连接体。
-
7.发明授权Artemisinin analogs having antimalarial antiproliferative and antitumor activities and chemoselective methods of making the same 失效具有抗疟疾抗增殖和抗肿瘤活性的青蒿素类似物和制备相同的化学选择性方法公开(公告)号：US06297272B1
公开(公告)日：2001-10-02
申请号：US09228668
申请日：1999-01-12
IPC分类号： A61K21357
CPC分类号： C07D493/18 , C07D519/00
摘要： Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is 1 and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.
摘要翻译： 本文描述了具有抗疟疾，抗增殖和抗肿瘤活性的新型青蒿素类似物和青蒿素二聚体的生产方法。 这些新型青蒿素类似物和青蒿素二聚体具有以下结构的非对映体，具有抗疟疾和抗增殖和抗肿瘤活性，其中当n为1时，本发明的单体形成，R为烷基，环烷基，杂烷基，杂环烷基，烯基，炔基 ，芳基或杂芳基。 本发明的二聚体在n为2时形成，R为包括但不限于烷基，环烷基，杂烷基，杂环烷基，烯基，炔基，芳基或杂芳基的连接体。
-
公开(公告)号：US09775903B2
公开(公告)日：2017-10-03
申请号：US13521980
申请日：2011-01-13
申请人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
发明人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
IPC分类号： A61K45/06 , C07C401/00 , A61K31/593
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.
-
公开(公告)号：US08884032B2
公开(公告)日：2014-11-11
申请号：US13321343
申请日：2010-05-19
IPC分类号： C07D321/00 , A61K31/335 , C07D493/18 , C07D519/00
CPC分类号： C07D493/18 , C07D519/00
摘要： Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
摘要翻译： 单碳和二聚三恶烷氟芳基酰胺，5-碳连接的C-10非缩醛三恶烷二聚体酯; 三恶烷甲硅烷基酰胺 和三恶烷二聚体原生体及其用于治疗感染疟疾或其他寄生传染病的受试者的方法，包括但不限于：弓形虫感染; 患有与弓形虫感染相关的精神病症的受试者; 和患有癌症的受试者。
-
公开(公告)号：US5817692A
公开(公告)日：1998-10-06
申请号：US701423
申请日：1996-08-22
申请人： Gary H. Posner
发明人： Gary H. Posner
IPC分类号： A61K31/357 , C07D493/08 , C07D493/10 , C07D497/08 , A61K31/335 , C07D321/10 , C07D323/04
CPC分类号： A61K31/357 , C07D493/08 , C07D493/10 , C07D497/08
摘要： The present invention relates to novel biologically-active organic peroxides and to novel uses of both known and new organic peroxides. More specifically, this invention details organic endoperoxides having antiparasitic activity, methods for their preparation and methods for treating malaria and cerebral toxoplasmic encephalitis with the organic endoperoxides.
摘要翻译： 本发明涉及新颖的生物活性有机过氧化物和新型有机过氧化物的新用途。 更具体地，本发明详述了具有抗寄生虫活性的有机内过氧化物，其制备方法和用有机内过氧化物治疗疟疾和脑弓形虫脑炎的方法。
-
-
-
-
-
-
-
-
-
搜索结果
40 条记录 (耗时 0.029 秒)
