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    PROCESS OF MAKING ALPHA-AMINOOXYKETONE/ALPHA-AMINOOXYALDEHYDE AND ALPHA-HYDROXYKETONE/ALPHA-HYDROXYALDEHYDE COMPOUNDS AND A PROCESS MAKING REACTION PRODUCTS FROM CYCLIC ALPHA, BETA-UNSATURATED KETONE SUBSTRATES AND NITROSO SUBSTRATES
    2.
    发明申请
    PROCESS OF MAKING ALPHA-AMINOOXYKETONE/ALPHA-AMINOOXYALDEHYDE AND ALPHA-HYDROXYKETONE/ALPHA-HYDROXYALDEHYDE COMPOUNDS AND A PROCESS MAKING REACTION PRODUCTS FROM CYCLIC ALPHA, BETA-UNSATURATED KETONE SUBSTRATES AND NITROSO SUBSTRATES 有权
    制备ALPHA-氨基甲基酮/丙氨酸 - 氨基甲醛和α-羟基酮/ ALPHA-羟基甲醛化合物的方法和制备来自循环ALPHA，BETA-不饱和酮基和NITROSO底物的反应产物

    公开(公告)号：US20100099915A1

    公开(公告)日：2010-04-22

    申请号：US12578836

    申请日：2009-10-14

    Applicant: Norie Momiyama ,  Hiromi Torii ,  Susumu Saito ,  Hisashi Yamamoto ,  Yuhei Yamamoto

    Inventor： Norie Momiyama ,  Hiromi Torii ,  Susumu Saito ,  Hisashi Yamamoto ,  Yuhei Yamamoto

    IPC: C07C291/06

    CPC classification number: C07C291/04 ,  C07C2601/14 ,  C07D207/16 ,  C07D211/74 ,  C07D309/30 ,  C07D317/72 ,  C07D403/04

    Abstract: The present invention is directed to a process of making α-aminooxyketone and α-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein Xa—Xc represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the α-aminooxyketone compound formed to the α-hydroxyketone compound. The present invention results in α-aminooxyketone and α-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic α,β-unsaturated ketone substrate and a nitroso substrate. This methodology generally involves reacting the cyclic α,β-unsaturated ketone substrate and the nitroso substrate in the presence of a proline-based catalyst, to provide a heterocyclic product.

    Abstract translation: 本发明涉及制备α-氨基氧基酮和α-羟基酮化合物的方法。 合成途径通常包括在式（Ⅳ）催化剂存在下使醛或酮底物和亚硝基底物反应：其中Xa-Xc独立地代表氮，碳，氧或硫，Z代表4至10元 具有或不具有取代基的环，以及任选的将形成的α-氨基氧基酮化合物转化为α-羟基酮化合物的步骤。 本发明产生具有高对映选择性和高纯度的α-氨基氧基酮和α-羟基酮化合物。 本发明还涉及催化不对称的O-亚硝基醛醇/迈克尔反应。 该反应的底物通常为环状α，β-不饱和酮底物和亚硝基。 该方法通常包括在脯氨酸基催化剂存在下使环状α，β-不饱和酮底物和亚硝基底物反应，得到杂环产物。

    Antioxidant nitroxides and nitrones as therapeutic agents
    7.
    发明授权
    Antioxidant nitroxides and nitrones as therapeutic agents 失效
    抗氧化氮氧化物和硝酮作为治疗剂

    公开(公告)号：US06852889B2

    公开(公告)日：2005-02-08

    申请号：US10769128

    申请日：2004-01-30

    Applicant: Yuqiang Wang ,  James W. Larrick

    Inventor： Yuqiang Wang ,  James W. Larrick

    IPC: A61P1/04 ,  A61K31/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P39/06 ,  C07C271/24 ,  C07C291/00 ,  C07C291/02 ,  C07C291/06 ,  A61K31/13 ,  A01N33/02

    CPC classification number: C07C291/02 ,  C07C291/06 ,  C07C2603/74

    Abstract: The invention provides novel adamantane compounds having one of the following formulas: wherein: R1 and R3 are H, OH, alkyl, cycloalkyl, amino or aryl, and can be the same or different; R2 is H, NH2, alkyl, OH, COOH, amino, amide, or carbamate; R4-R8 are H, OH, NH2, alkyl, OH, COOH, ester, amino, amide, or alkyloxy, and can be the same or different; R9-R14 are H, alkyl, or phenyl, and can be the same or different; and wherein when any of R1-R8 is amino, the compounds are the free bases and their acid addition salts. The present invention also relates to compositions and methods for treating and/or preventing neurological and inflammatory disorders in a patient by administering a therapeutically effective amount of the compounds of formula (I), (II) or (III) and a pharmaceutically acceptable carrier.

    Abstract translation: 本发明提供具有下式之一的新型金刚烷化合物：其中：R 1和R 3是H，OH，烷基，环烷基，氨基或芳基，并且可以相同或不同; R 2是H，NH 2，烷基，OH，COOH ，氨基，酰胺或氨基甲酸酯; R 4 -R 8是H，OH，NH 2，烷基，OH，COOH，酯，氨基，酰胺或烷氧基，并且可以相同或不同; R9-R14是H，烷基或 苯基，并且可以相同或不同;并且其中当R 1 -R 8中的任何一个是氨基时，所述化合物是游离碱及其酸加成盐。本发明还涉及用于治疗和/或预防神经系统和/ 通过施用治疗有效量的式（I），（II）或（III）化合物和药学上可接受的载体，在患者中发炎。

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