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    Method for producing 3-amidinophenylalanine derivatives
    2.
    再颁专利
    Method for producing 3-amidinophenylalanine derivatives 有权

    公开(公告)号：USRE46424E1

    公开(公告)日：2017-06-06

    申请号：US14145892

    申请日：2013-12-31

    申请人： Wilex AG

    发明人： Hugo Ziegler ,  Peter Wikstroem

    IPC分类号： C07D295/00 ,  C07D213/00 ,  C07D295/205 ,  C07D211/60

    CPC分类号： C07D295/205 ,  C07D211/60

    摘要： The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate formate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

    Therapeutic substances that modulate genome methylation
    6.
    发明授权
    Therapeutic substances that modulate genome methylation 有权

    公开(公告)号：US08901102B2

    公开(公告)日：2014-12-02

    申请号：US14165050

    申请日：2014-01-27

    申请人： Retrotope, Inc.

    发明人： Mikhail S. Shchepinov

    IPC分类号： C07H19/06 ,  C07D213/00 ,  C07H19/073 ,  C07D405/04

    CPC分类号： C07H19/06 ,  C07D405/04 ,  C07H19/073

    摘要： Compounds containing nucleic acid bases or their precursors modified by enrichment at specific sites with heavy stable isotopes of elements naturally present at those sites in minute amount are useful for the treatment of diseases characterized by altered gene expression and altered pattern of epigenomic control. These compounds, when used as nutrients or in other medicinal application methods, can alter the DNA methylation pattern in a simple way through the well-understood mechanism of kinetic isotope effect (KIE). This effect could also be useful for modifying methylation kinetics in stem cell technology, cloning and as disease therapeutics.

    Nitrogen-containing heterocyclic compound and method for producing same
    8.
    发明授权
    Nitrogen-containing heterocyclic compound and method for producing same 有权
    含氮杂环化合物及其制造方法

    公开(公告)号：US08809544B2

    公开(公告)日：2014-08-19

    申请号：US14175904

    申请日：2014-02-07

    申请人： Nippon Soda Co., Ltd.

    发明人： Koichi Kutose ,  Hiroki Inoue ,  Shiro Tsubokura

    IPC分类号： C07D213/00 ,  C07D213/75 ,  C07D213/89

    CPC分类号： C07D213/89 ,  C07D213/75

    摘要： There are provided a nitrogen-containing heterocyclic compound such as a substituted amino-pyridine-N-oxide compound represented by formula (1), which is useful as a synthetic intermediate for an agrochemical and the like; and a method for producing the nitrogen-containing heterocyclic compound. (In formula (1), R1 and R2 each represents a hydrogen atom or an unsubstituted or substituted alkyl group; R3 represents a hydrogen atom, an unsubstituted or substituted alkylcarbonyl group or the like; R4 represents an unsubstituted or substituted alkylcarbonyl group, an unsubstituted or substituted arylcarbonyl group or the like; A represents a hydroxyl group, a thiol group or the like; m represents any one of integers of 1 to 4; k represents any one of integers of 0 to 3; and k+m≦4.)

    摘要翻译： 提供了可用作农药等的合成中间体的含氮杂环化合物，例如由式（1）表示的取代的氨基 - 吡啶-N-氧化物化合物; 和含氮杂环化合物的制造方法。 （式（1）中，R 1和R 2各自表示氢原子或未取代或取代的烷基; R 3表示氢原子，未取代或取代的烷基羰基等; R 4表示未取代或取代的烷基羰基，未取代的 或取代的芳基羰基等; A表示羟基，硫醇基等; m表示1〜4的整数中的任一个; k表示0〜3的整数中的任一个; k + m＆lt; 1l; 4。 ）