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1. 发明授权

US06441161B1 Urea nucleosides as therapeutic and diagnostic agents 有权
标题翻译：尿素核苷作为治疗和诊断剂
公开(公告)号：US06441161B1
公开(公告)日：2002-08-27
申请号：US09707253
申请日：2000-11-06
申请人： Gary P. Kirschenheuter , Bruce Eaton
发明人： Gary P. Kirschenheuter , Bruce Eaton
IPC分类号： C07H1900
CPC分类号： C07H11/02 , C07H19/06 , C07H19/16
摘要： Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule. The nucleosides can be used to prepare oligonucleotides for use in various applications, either alone or in combination with other modified nucleosides and/or naturally occurring nucleosides.
摘要翻译：公开了修饰的核苷和制备和使用核苷的方法。可以通过使含有嘌呤或嘧啶环中的一个或多个碳原子上的合适的离去基团的核苷起始原料与乙烯基苯烷，一氧化碳和钯催化剂反应来制备化合物，以提供1-烯-3-醇，一个中间体。然后通过迈克尔反应将这些中间体与适当官能化的伯胺或仲胺反应。当中间体是5-位修饰的嘧啶环，并且胺含有第二个氢时，它可以与嘧啶环中的一个或烯 - 亚胺进行第二个迈克尔反应。胺反应物的适当改性可产生具有各种生物活性的产物。核苷可以用作治疗性的抗癌，抗细菌或抗病毒药物。核苷也可用于诊断应用，例如通过在分子中掺入放射性标记或荧光标记。核苷可用于制备用于各种应用的寡核苷酸，单独使用或与其它修饰的核苷和/或天然存在的核苷组合。

2. 发明授权

US2165435A Process for melting, casting, and purifying sucrose octanitrate 失效
标题翻译：熔化，铸造和纯化蔗糖甘油酯的方法
公开(公告)号：US2165435A
公开(公告)日：1939-07-11
申请号：US16803837
申请日：1937-10-08
申请人： TROJAN POWDER CO
发明人： WYLER JOSEPH A
IPC分类号： C07C201/02
CPC分类号： C07H11/02

3. 发明授权

US2105390A Purification of sucrose octanitrate 失效
标题翻译：蔗糖辛酸钠的纯化
公开(公告)号：US2105390A
公开(公告)日：1938-01-11
申请号：US8776236
申请日：1936-06-27
申请人： TROJAN POWDER CO
发明人： WYLER JOSEPH A
IPC分类号： C07H11/02
CPC分类号： C07H11/02

4. 发明申请

US20030069414A1 Urea nucleosides as therapeutic and diagnostic agents 失效
公开(公告)号：US20030069414A1
公开(公告)日：2003-04-10
申请号：US10216553
申请日：2002-08-09
申请人： GILEAD SCIENCES, INC.
发明人： Gary P. Kirschenheuter , Bruce Eaton
IPC分类号： C07H019/00 , C07H019/22 , C07H019/16
CPC分类号： C07H11/02 , C07H19/06 , C07H19/16
摘要： Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule. The nucleosides can be used to prepare oligonucleotides for use in various applications, either alone or in combination with other modified nucleosides and/or naturally occurring nucleosides.

5. 发明授权

US6143882A Urea nucleosides as therapeutic and diagnostic agents 失效
公开(公告)号：US6143882A
公开(公告)日：2000-11-07
申请号：US405932
申请日：1999-09-27
申请人： Gary Kirschenheuter , Bruce Eaton
发明人： Gary Kirschenheuter , Bruce Eaton
IPC分类号： C07H11/02 , C07H19/06 , C07H19/16 , C07H19/00 , C07H19/22
CPC分类号： C07H11/02 , C07H19/06 , C07H19/16
摘要： Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule. The nucleosides can be used to prepare oligonucleotides for use in various applications, either alone or in combination with other modified nucleosides and/or naturally occurring nucleosides.

6. 发明授权

US2094693A Nitration of sugars and their glycosides 失效
标题翻译：糖和糖苷的硝化
公开(公告)号：US2094693A
公开(公告)日：1937-10-05
申请号：US2704935
申请日：1935-06-17
申请人： TROJAN POWDER CO
发明人： WYLER JOSEPH A
IPC分类号： C07C201/02
CPC分类号： C07C201/02 , C07H1/00 , C07H11/02 , C07H15/04 , C07C203/04

7. 发明申请

US20180111956A1 SYNTHESIS OF DESOSAMINES 审中-公开
公开(公告)号：US20180111956A1
公开(公告)日：2018-04-26
申请号：US15558910
申请日：2016-03-25
申请人： President and Fellows of Harvard College
发明人： Andrew G. Myers , Ziyang Zhang
IPC分类号： C07H15/12 , C07H11/02 , C07H17/02 , C07C201/14 , C07C201/12 , C07H1/00
CPC分类号： C07H15/12 , C07B2200/07 , C07C201/12 , C07C201/14 , C07H1/00 , C07H11/02 , C07H15/18 , C07H17/02
摘要： The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof.

8. 发明授权

US5959100A Pyrimidine nucleosides as therapeutic and diagnostic agents 失效
标题翻译：嘧啶核苷作为治疗和诊断剂
公开(公告)号：US5959100A
公开(公告)日：1999-09-28
申请号：US622772
申请日：1996-03-27
申请人： Gary P. Kirschenheuter , Bruce Eaton
发明人： Gary P. Kirschenheuter , Bruce Eaton
IPC分类号： C07H11/02 , C07H19/06 , C07H19/16 , C07H19/04
CPC分类号： C07H11/02 , C07H19/06 , C07H19/16
摘要： Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at one or more of the carbon atoms in the purine or pyrimidine ring, with a vinylstannane, carbon monoxide, and a palladium catalyst to provide 1-ene-3-one intermediates. These intermediates are then reacted with suitably functionalized primary or secondary amines via a Michael reaction. When the intermediate is a 5-position modified pyrimidine ring, and the amine contains a second hydrogen, it can do a second Michael reaction with the ene-one or the ene-imine in the pyrimidine ring. Appropriate modification of the amine reactant can yield products with various bioactivities. The nucleosides can be used therapeutically as anti-cancer, anti-bacterial or anti-viral drugs. The nucleosides can also be used for diagnostic applications, for example, by incorporating a radiolabel or fluorescent label into the molecule. The nucleosides can be used to prepare oligonucleotides for use in various applications, either alone or in combination with other modified nucleosides and/or naturally occurring nucleosides.
摘要翻译：公开了修饰的核苷和制备和使用核苷的方法。可以通过使含有嘌呤或嘧啶环中的一个或多个碳原子上的合适的离去基团的核苷起始原料与乙烯基苯烷，一氧化碳和钯催化剂反应来制备化合物，以提供1-烯-3-醇，一个中间体。然后通过迈克尔反应将这些中间体与适当官能化的伯胺或仲胺反应。当中间体是5-位修饰的嘧啶环，并且胺含有第二个氢时，它可以与嘧啶环中的一个或烯 - 亚胺进行第二个迈克尔反应。胺反应物的适当改性可产生具有各种生物活性的产物。核苷可以用作治疗性的抗癌，抗细菌或抗病毒药物。核苷也可用于诊断应用，例如通过在分子中掺入放射性标记或荧光标记。核苷可用于制备用于各种应用的寡核苷酸，单独使用或与其它修饰的核苷和/或天然存在的核苷组合。

9. 发明授权

US2081161A Sucrose octanitrate 失效
标题翻译：蔗糖蔗糖
公开(公告)号：US2081161A
公开(公告)日：1937-05-25
申请号：US7975936
申请日：1936-05-14
申请人： TROJAN POWDER CO
发明人： WYLER JOSEPH A
IPC分类号： C07H11/02
CPC分类号： C07H11/02

10. 发明授权

US1836568A Nitrated glucoside explosive and process of producing the same 失效
标题翻译：硝化葡萄糖苷的爆炸和生产过程相同
公开(公告)号：US1836568A
公开(公告)日：1931-12-15
申请号：US24145627
申请日：1927-12-20
申请人： DU PONT
发明人： WRIGHTSMAN PHILIP G
IPC分类号： C07C201/02
CPC分类号： C07H11/02

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