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    Synthesis of acylureas and composition comprising acylureas
    1.
    发明授权
    Synthesis of acylureas and composition comprising acylureas 有权
    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。

    Method and reagents for N-alkylating ureides
    2.
    发明授权
    Method and reagents for N-alkylating ureides 失效
    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。

    Method and reagents for N-alkylating ureides
    5.
    发明授权
    Method and reagents for N-alkylating ureides 失效
    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。

    Process for the preparation of polyisocyanates containing urethane and biuret groups
    6.
    发明授权
    Process for the preparation of polyisocyanates containing urethane and biuret groups 失效
    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。

    Glycyl urea derivatives as anti-convulsants
    7.
    发明授权
    Glycyl urea derivatives as anti-convulsants 失效
    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。