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    Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof
    5.
    发明授权
    Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof 失效
    含有硝基烷基胺，新型硝基烷基胺的药物组合物及其制备方法

    公开(公告)号：US5037849A

    公开(公告)日：1991-08-06

    申请号：US424452

    申请日：1989-10-20

    申请人： Herbert Simon ,  Helmut Michel ,  Michael Schultz ,  Wolfgang Bartsch

    发明人： Herbert Simon ,  Helmut Michel ,  Michael Schultz ,  Wolfgang Bartsch

    IPC分类号： A61K31/21 ,  A61K31/395 ,  A61K31/40 ,  A61K31/445 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07C235/10 ,  C07C235/26 ,  C07C235/40 ,  C07C237/08 ,  C07C237/18 ,  C07C275/10 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07D211/06 ,  C07D295/13 ,  C07D295/14 ,  C07D295/215

    CPC分类号： C07D295/215 ,  A61K31/21 ,  C07C235/10 ,  C07C235/26 ,  C07C235/40 ,  C07C237/08 ,  C07C275/10 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07D295/13 ,  C07C2101/14

    摘要： The present invention provides pharmaceutical compositions effective against angina-like heart and circulatory diseases containing at least one nitroxyalkylamine derivative of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower-alkyl radical, a C.sub.3 -C.sub.8 -cycloalkyl or C.sub.3 -C.sub.8 -cycloalkenyl radical, an aminocarbonyl, C.sub.1 -C.sub.6 -mono- or di-alkylaminocarbonyl radical, R.sup.2 is a hydrogen atom, a lower-alkyl radical or a C.sub.3 -C.sub.8 -cycloalkyl or cycloalkenyl radical or R.sup.2, together with R.sup.1 and the nitrogen atom to which they are attached, form a heteroaliphatic ring containing up to 6 carbon atoms, A is a valency bond or a straight-chained or branched lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical, B is a lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical and X is an --NR.sup.3 --CO-- or --CO--NR.sup.3 -- radical, in which R.sup.3 is a hydrogen atom or a lower-alkyl radical, when X is an --NR.sup.3 --CO-- radical, R.sup.3, together with the nitrogen atom and a carbon atom of the group A, bridge a heterocyclic ring containing 4 to 6 carbon atoms or R.sup.3, together with R.sup.2, A and the two nitrogen atoms, bridge a heterocyclic ring containing 3 to 5 carbon atoms; and the optically-active forms and physiologically acceptable salts thereof.

    摘要翻译： 本发明提供了有效抗心绞痛的心脏和循环系统疾病的药物组合物，其含有至少一种以下通式的硝基烷基胺衍生物：其中R 1是氢原子，低级烷基，C 3 -C 8 - 环烷基或C 3 -C 8 - 环烯基，氨基羰基，C 1 -C 6 - 单 - 或二 - 烷基氨基羰基，R 2是氢原子，低级烷基或C 3 -C 8 - 环烷基或环烯基或R 2，连同 R1和它们所连接的氮原子形成含有至多6个碳原子的杂脂族环，A是价键或直链或支链的低级亚烷基，其中-CH 2 - 基团可以被 亚环烷基，B是低级亚烷基，其中-CH 2 - 基团可被亚环烷基代替，X是-NR 3 -CO-或-CO-NR 3 - 基，其中R 3是氢原子 或低级烷基，当X是-NR 3 -CO-基时，R 3与硝基一起形成 原子和A基团的碳原子，桥接含有4至6个碳原子的杂环或R3与R2，A和两个氮原子一起桥接含有3至5个碳原子的杂环; 和其光学活性形式和生理上可接受的盐。

    AMIDE-EXTENDED CROSSLINKING COMPOUNDS AND METHODS FOR USE THEREOF
    6.
    发明申请
    AMIDE-EXTENDED CROSSLINKING COMPOUNDS AND METHODS FOR USE THEREOF 有权
    AMIDE-EXTENDED CROSSLINKING COMPOUNDS及其使用方法

    公开(公告)号：US20110152466A1

    公开(公告)日：2011-06-23

    申请号：US13058827

    申请日：2009-08-13

    申请人： Stephen M. Dershem

    发明人： Stephen M. Dershem

    IPC分类号： C08F8/32 ,  C07D403/14 ,  C07C229/32 ,  C07D403/12 ,  C07C229/30 ,  C07D407/12 ,  C07C237/18 ,  C07F7/18 ,  C09J133/24

    CPC分类号： C07C233/32 ,  C07C233/01 ,  C07C233/45 ,  C07D207/34 ,  C07D207/36 ,  C07D207/40 ,  C07D207/452 ,  C09J145/00 ,  C09J147/00 ,  C09J179/08 ,  C09J179/085

    摘要： The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved by incorporating amide-extended maleimides into an adhesive formulation. Amide-extended maleimides described herein can be used to toughen bismaleimide thermosetting materials without sacrificing any thermal stability. Amide-extended maleimides are readily prepared by reacting a bismaleimide with an appropriate amine via the well-known Michael addition reaction. Acylation of the resulting secondary amines provides the amide-extended maleimide. The acylating agent can also be used to introduce polymerizable functional groups into the backbones of these thermoset monomers. Amide-extended acrylate and methacrylate monomers can also be prepared.

    摘要翻译： 本发明基于以下发现，即通过将酰胺延伸的马来酰亚胺掺入粘合剂制剂中可以显着改善马来酰亚胺热固性材料的性能。 本文所述的酰胺延伸的马来酰亚胺可用于增强双马来酰亚胺热固性材料，而不牺牲任何热稳定性。 酰胺延伸的马来酰亚胺通过公知的迈克尔加成反应使双马来酰亚胺与适当的胺反应容易地制备。 所得仲胺的酰化提供了酰胺延伸的马来酰亚胺。 酰化剂也可用于将可聚合官能团引入这些热固性单体的主链。 还可以制备酰胺延伸的丙烯酸酯和甲基丙烯酸酯单体。

    Optically active 2-allylcarboxylic acid derivative and process for producing the same
    7.
    发明授权
    Optically active 2-allylcarboxylic acid derivative and process for producing the same 失效
    光学活性2-烯丙基羧酸衍生物及其制备方法

    公开(公告)号：US07282605B2

    公开(公告)日：2007-10-16

    申请号：US10553394

    申请日：2004-04-16

    申请人： Kazumi Okuro ,  Susumu Amano ,  Noriyuki Kizaki ,  Teruaki Takesue ,  Masaru Mitsuda ,  Noriyuki Ito ,  Yoshihiko Yasohara

    发明人： Kazumi Okuro ,  Susumu Amano ,  Noriyuki Kizaki ,  Teruaki Takesue ,  Masaru Mitsuda ,  Noriyuki Ito ,  Yoshihiko Yasohara

    IPC分类号： C07C291/00 ,  C07C237/16 ,  C07C237/18 ,  C07C237/20

    CPC分类号： C07C233/18 ,  C07B2200/07 ,  C07C51/06 ,  C07C67/20 ,  C07C233/05 ,  C07C271/64 ,  C12P7/40 ,  C12P41/005 ,  C07C57/03 ,  C07C69/533

    摘要： The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process.An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.

    摘要翻译： 本发明提供了一种用于制备可用作药物中间体的光学活性2-烯丙基羧酸衍生物的方法，其由易于获得且廉价的原料通过可以简单和容易的方式在商业规模上实施的方法制备， 和某些2-烯丙基羧酰胺衍生物，它们是该方法中新颖且重要的中间体。 N-烯丙基甲酰胺衍生物在碱存在下非对映选择性地进行重排反应，得到2-烯丙基甲酰胺衍生物，所得衍生物进行氨基甲酰化反应和溶剂解，得到光学活性2-烯丙基羧酸酯，然后得到所述酯 使用酶进行立体选择性水解以产生具有高光学纯度的2-烯丙基羧酸。 此外，本发明提供了在本发明的方法中是新型中间体的2-烯丙基甲酰胺衍生物化合物。