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1. 发明授权

US08158817B2 Synthesis of acylureas and composition comprising acylureas 有权
标题翻译：酰基脲和包含酰基脲的组合物的合成
公开(公告)号：US08158817B2
公开(公告)日：2012-04-17
申请号：US12714873
申请日：2010-03-01
申请人： Jean-Marie Bernard , Denis Revelant , Cédric Amouyal
发明人： Jean-Marie Bernard , Denis Revelant , Cédric Amouyal
IPC分类号： C07C273/00 , C07C273/18 , C07C275/46 , C07C275/48 , C07C275/62
CPC分类号： C08G18/7831 , C08G18/168 , C08G18/348
摘要： The invention relates to a process for the synthesis of a polyisocyanate composition comprising acylureas. According to the invention, a starting composition comprising a compound having at least two isocyanate functional groups is subjected to a reaction with at least two acid functional groups, with at least one of the acid functional groups having a pKa value of less than or equal to 3, and at least one of the acid functional groups having a pKa value of more than 3 and less than or equal to 6, at a temperature at least equal to 50 ° C., wherein the acid functional group having a pKa value of less than or equal to 3 and the acid functional group having a pKa value of more than 3 and less than or equal to 6 are present on two different acids or on the same acid.
摘要翻译：本发明涉及一种合成包含酰基脲的多异氰酸酯组合物的方法。根据本发明，包含具有至少两个异氰酸酯官能团的化合物的起始组合物与至少两个酸官能团进行反应，其中至少一个酸官能团的pKa值小于或等于 3，并且在至少等于50℃的温度下具有pKa值大于3且小于或等于6的酸官能团中的至少一个，其中具有pKa值较小的酸官能团 pKa值大于3且小于或等于6的酸官能团存在于两种不同的酸或相同的酸上。

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. 发明申请

US20040102518A1 N-benzoylureidocinnamic acid derivatives, processes for preparing them and their use 有权
标题翻译： N-苯甲酰基肉豆蔻酸衍生物，其制备方法及其应用
公开(公告)号：US20040102518A1
公开(公告)日：2004-05-27
申请号：US10456570
申请日：2003-06-06
申请人： Aventis Pharma AG
发明人： Karl Schoenafinger , Elisabeth Defossa , Dieter Kadereit , Erich Von Roedern , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt
IPC分类号： A61K031/277 , A61K031/195 , C07C275/48 , A61K031/17
CPC分类号： C07C275/54
摘要： The invention relates to N-benzoylureidocinnamic acid derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention thus relates to compounds of formula I, 1 in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetic agents.
摘要翻译：本发明涉及N-苯甲酰基肉毒杆菌酸衍生物及其生理上耐受的盐和生理功能衍生物。因此，本发明涉及其中基团具有给定含义的式I化合物及其生理上耐受的盐及其制备方法。化合物例如适合用作抗糖尿病药。

4. 发明授权

US2090594A Acyl ureas and process for the preparation thereof 失效
标题翻译：酰基脲及其制备方法
公开(公告)号：US2090594A
公开(公告)日：1937-08-17
申请号：US6070636
申请日：1936-01-24
申请人： DU PONT
发明人： JACOBSON RALPH A
IPC分类号： C07C273/18 , C07C275/48 , C07C275/50
CPC分类号： C07C273/1854 , C07C275/50 , C07C275/48

5. 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。

6. 发明授权

US4124569A Process for the preparation of polyisocyanates containing urethane and biuret groups 失效
标题翻译：制备含氨基甲酸酯和缩二脲基团的多异氰酸酯的方法
公开(公告)号：US4124569A
公开(公告)日：1978-11-07
申请号：US832318
申请日：1977-09-12
申请人： Manfred Bock , Josef Pedain , Walter Uerdingen , Manfred Schonfelder
发明人： Manfred Bock , Josef Pedain , Walter Uerdingen , Manfred Schonfelder
IPC分类号： C08G18/00 , C07C67/00 , C07C239/00 , C07C269/02 , C07C273/18 , C07C275/48 , C07C275/62 , C08G18/78 , C08G18/80 , C08G18/79
CPC分类号： C07C273/1863 , C07C273/1872 , C08G18/7831 , C08G18/8041 , C08G18/8058
摘要： The present invention is concerned with a process for producing biuret polyisocyanates and the polyisocyanates so produced. These isocyanates are produced by the reaction of at least about a four fold molar excess of a diisocyanate having aliphatically bound isocyanate groups with amino alcohols having a particular structure at a temperature between about 90 and 200.degree. C. The amino alcohols contain at least three carbon atoms, have their hydroxyl and amino groups separated by at least two carbon atoms, and may contain urea, urethane, ether or amino bonds. The present invention is also concerned with a process for producing two component and one component moisture curing lacquers using the biuret polyisocyanates of the present invention and the lacquers so produced.
摘要翻译：本发明涉及制备缩二脲多异氰酸酯的方法和如此制备的多异氰酸酯。这些异氰酸酯是通过至少约四倍摩尔过量的具有脂肪族结合的异氰酸酯基团的二异氰酸酯与具有特定结构的氨基醇在约90-200℃之间的温度下进行的反应来制备的。氨基醇含有至少三个碳原子，其羟基和氨基被至少两个碳原子分开，并且可以含有脲，氨基甲酸酯，醚或氨基键。本发明还涉及使用本发明的缩二脲多异氰酸酯和如此制备的漆制备两组分和一种组分的湿固化漆的方法。

7. 发明授权

US5288905A Glycyl urea derivatives as anti-convulsants 失效
标题翻译：甘氨酰脲衍生物作为抗惊厥药
公开(公告)号：US5288905A
公开(公告)日：1994-02-22
申请号：US761111
申请日：1991-09-17
申请人： Alex A. Cordi , Claude L. Gillet
发明人： Alex A. Cordi , Claude L. Gillet
IPC分类号： C07C275/50 , C07C275/48
CPC分类号： C07C275/50
摘要： A class of glycyl urea derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of interest are those of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group independently selected from hydrido, alkyl, aralkyl, aryloxyalkyl and arylthioalkyl, any one of which groups having a substitutable position may be substituted with one or more radicals selected from halo, alkyl of one to about ten carbon atoms, alkenyl of two to about ten carbon atoms, alkynyl of two to about ten carbon atoms, haloalkyl, alkoxy, alkylthio, alkylsulfinyl and alkylsulfonyl; or a pharmaceutically-acceptable salt thereof; with the proviso that when each of R.sup.1 and R.sup.2 is ethyl, then R.sup.3 and R.sup.4 cannot be hydrido simultaneously.
摘要翻译：描述了一类甘氨酰脲衍生物用于治疗CNS功能障碍如癫痫和惊厥性疾病。感兴趣的化合物是式（*化学结构*）的化合物，其中R 1，R 2，R 3和R 4各自独立地选自氢，烷基，芳烷基，芳氧基烷基和芳硫基烷基，其中任何一个具有可取代位置的基团被一个或多个选自卤素，1至约10个碳原子的烷基，2至约10个碳原子的烯基，2至约10个碳原子的炔基，卤代烷基，烷氧基，烷硫基，烷基亚磺酰基和烷基磺酰基取代; 或其药学上可接受的盐; 条件是当R 1和R 2各自为乙基时，则R 3和R 4不能同时氢化。

8. 发明授权

US2574864A Acyl ureide preparation 失效
标题翻译：酰基酰胺制剂
公开(公告)号：US2574864A
公开(公告)日：1951-11-13
申请号：US71994247
申请日：1947-01-02
申请人： PROCTER & GAMBLE
发明人： ECKEY EDDY W , DOYLE ABBOTT ANDREW
IPC分类号： C07C273/18 , C07C275/48
CPC分类号： C07C273/1863 , C07C275/48

9. 发明授权

US2090593A Process for the preparation of urea derivatives 失效
标题翻译：尿素衍生物的制备方法
公开(公告)号：US2090593A
公开(公告)日：1937-08-17
申请号：US6070536
申请日：1936-01-24
申请人： DU PONT
发明人： JACOBSON RALPH A
IPC分类号： C07C273/18 , C07C275/48
CPC分类号： C07C273/1854 , C07C275/48

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