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1. 再颁专利

USRE38934E1 Method and reagents for N-alkylating ureides 有权
公开(公告)号：USRE38934E1
公开(公告)日：2006-01-10
申请号：US10375340
申请日：2003-02-27
申请人： Daniela Gutman , Hershel Herzog
发明人： Daniela Gutman , Hershel Herzog
IPC分类号： C07D239/62 , C07D233/74 , C07D263/44 , A61K31/515
CPC分类号： C07D207/408 , C07D207/40 , C07D211/88 , C07D233/74 , C07D239/62 , C07D263/44
摘要： A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I with an alkylating agent of structure III in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

2. 发明授权

US06093820A Method and reagents for N-alkylating ureides 失效
标题翻译： N-烷基化脲的方法和试剂
公开(公告)号：US06093820A
公开(公告)日：2000-07-25
申请号：US942636
申请日：1997-10-02
申请人： Daniela Gutman , Hershel Herzog
发明人： Daniela Gutman , Hershel Herzog
IPC分类号： A61K31/496 , A61K31/515 , A61P25/00 , A61P25/08 , C07C231/08 , C07C233/90 , C07C273/18 , C07C275/48 , C07D207/40 , C07D207/408 , C07D211/88 , C07D233/74 , C07D239/62 , C07D263/44
CPC分类号： C07D207/408 , C07D207/40 , C07D211/88 , C07D233/74 , C07D239/62 , C07D263/44
摘要： A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I ##STR1## with an alkylating agent of structure III ##STR2## in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N'-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.
摘要翻译：根据本发明的N-烷氧基烷基化脲基的方法包括在碱性催化剂存在下在非质子传递反应介质中使结构I的酰脲与结构III的烷基化剂反应。酰脲可以是5,5-二取代的巴比妥酸，或者它可以是苯妥英，戊二酰亚胺和乙酰亚胺。烷基化剂是磺酸的酯。碱可以是氢化物或胺。优选的方法包括在二异丙基乙胺存在下将5,5-二苯基 - 巴比妥酸与甲氧基甲基甲磺酸N-烷氧基化，并分离所得的N，N'-二甲氧基甲基-5,5-二苯基 - 巴比妥酸。本发明还考虑了N-甲氧基甲基-5,5-二苯基巴比妥酸，N-甲氧基甲基乙基亚胺酰亚胺和N-甲氧基甲基戊二酰亚胺的新型化合物，以及包括给予患者的方法。

3. 发明授权

US06906079B2 Method and reagents for N-alkylating ureides 失效
标题翻译： N-烷基化脲的方法和试剂
公开(公告)号：US06906079B2
公开(公告)日：2005-06-14
申请号：US10687712
申请日：2003-10-17
申请人： Daniela Gutman , Hershel Herzog
发明人： Daniela Gutman , Hershel Herzog
IPC分类号： A61K31/496 , A61K31/515 , A61P25/00 , A61P25/08 , C07C231/08 , C07C233/90 , C07C273/18 , C07C275/48 , C07D207/40 , C07D207/408 , C07D211/88 , C07D233/74 , C07D239/62 , C07D263/44
CPC分类号： C07D207/408 , C07D207/40 , C07D211/88 , C07D233/74 , C07D239/62 , C07D263/44
摘要： A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I: with an alkylating agent of structure III: in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.
摘要翻译：根据本发明的N-烷氧基烷基化脲的方法包括使结构I的酰脲与结构III的烷基化剂反应：在非质子传递反应介质中的碱性催化剂存在下。酰脲可以是5,5-二取代的巴比妥酸，或者它可以是苯妥英，戊二酰亚胺和乙酰亚胺。烷基化剂是磺酸的酯。碱可以是氢化物或胺。优选的方法包括在二异丙基乙胺存在下将5,5-二苯基 - 巴比妥酸与甲氧基甲基甲磺酸N-烷氧基化，并分离所得的N，N'-二甲氧基甲基-5,5-二苯基 - 巴比妥酸。本发明还考虑了N-甲氧基甲基-5,5-二苯基巴比妥酸，N-甲氧基甲基乙基亚胺酰亚胺和N-甲氧基甲基戊二酰亚胺的新型化合物，以及包括给予患者的方法。

4. 发明授权

US06664262B2 N-methoxymethyl-5,5-diphenylbarbituric acid 失效
标题翻译： N-甲氧基甲基-5,5-二苯基巴比妥酸
公开(公告)号：US06664262B2
公开(公告)日：2003-12-16
申请号：US10073051
申请日：2002-02-12
申请人： Daniela Gutman , Hershel Herzog
发明人： Daniela Gutman , Hershel Herzog
IPC分类号： A61K31515
CPC分类号： C07D207/408 , C07D207/40 , C07D211/88 , C07D233/74 , C07D239/62 , C07D263/44
摘要： A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I: with an alkylating agent of structure III: in the presence of a basic catalyst in aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbrbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.
摘要翻译：根据本发明的N-烷氧基烷基化脲的方法包括使结构I的酰脲与结构III的烷基化试剂反应：在非质子传递反应介质中的碱性催化剂存在下进行。酰脲可以是5,5-二取代的巴比妥酸，或者它可以是苯妥英，戊二酰亚胺和乙酰亚胺。烷基化剂是磺酸的酯。碱可以是氢化物或胺。优选的方法包括在二异丙基乙胺存在下将5,5-二苯基 - 巴比妥酸与甲氧基甲基甲磺酸N-烷氧基化，并分离所得的N，N'-二甲氧基甲基-5,5-二苯基 - 巴比妥酸。本发明还考虑了新化合物N-甲氧基甲基-5,5-二苯基布列百里酸，N-甲氧基甲基乙基亚胺酰亚胺和N-甲氧基甲基戊二酰亚胺，以及包括给予患者的方法。

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