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    CHIRAL SALICYLALDEHYDE COMPOUND AND CHIRAL NAPHTHOLALDEHYDE COMPOUND FOR L / D OPTICAL TRANSFORMATION OF AMINO ACID, AND OPTICAL RESOLUTION OF AMINO ACID AND AMINOALCOHOL
    1.
    发明申请
    CHIRAL SALICYLALDEHYDE COMPOUND AND CHIRAL NAPHTHOLALDEHYDE COMPOUND FOR L / D OPTICAL TRANSFORMATION OF AMINO ACID, AND OPTICAL RESOLUTION OF AMINO ACID AND AMINOALCOHOL 审中-公开
    甲磺酰氯化合物和甲基萘甲醛化合物用于氨基酸的L / D光学转化和氨基酸和氨基醇的光学分解

    公开(公告)号：WO2010120138A2

    公开(公告)日：2010-10-21

    申请号：PCT/KR2010002363

    申请日：2010-04-15

    申请人： UNIV EWHA IND COLLABORATION ,  KIM KWAN-MOOK ,  YOON HEUNGSIK

    发明人： KIM KWAN-MOOK ,  YOON HEUNGSIK

    IPC分类号： C07C275/38 ,  C07B57/00 ,  C07C275/34

    CPC分类号： C07B57/00 ,  C07C275/34 ,  C07C275/38

    摘要： The present invention relates to a salicylaldehyde chiral compound (chemical formula 1) and a naphtholaldehyde chiral compound (chemical formula 2), wherein a -OH group and a carbonyl group are adjacent to each other on a benzene ring. Both compounds contain an asymmetric carbon and have relatively small molecular weight compared to that of known binaphthol derivatives. Optical transformation of amino acid and optical resolution of amino acid and aminoalcohol can be effectively carried out by the salicylaldehyde chiral compound (chemical formula 1) and naphtholaldehyde chiral compound (chemical formula 2) of the present invention.

    摘要翻译： 本发明涉及苯甲醛手性化合物（化学式1）和萘酚手性化合物（化学式2），其中-OH基和羰基在苯环上彼此相邻。 两种化合物都含有不对称碳，并且与已知的联萘酚衍生物相比具有相对小的分子量。 通过本发明的水杨醛手性化合物（化学式1）和萘酚手性化合物（化学式2）可以有效地进行氨基酸的光学转化和氨基酸和氨基醇的光学拆分。

    VLA-4 INTEGRIN ANTAGONISTS
    3.
    发明申请
    VLA-4 INTEGRIN ANTAGONISTS 审中-公开

    公开(公告)号：WO0142192A3

    公开(公告)日：2002-01-10

    申请号：PCT/EP0012226

    申请日：2000-12-05

    申请人： NOVARTIS AG ,  NOVARTIS ERFIND VERWALT GMBH ,  WATTANASIN SOMPONG ,  WEIDMANN BEAT

    发明人： WATTANASIN SOMPONG ,  WEIDMANN BEAT

    IPC分类号： C07D295/12 ,  A61K31/197 ,  A61K31/5375 ,  A61K31/5377 ,  A61P11/00 ,  A61P19/02 ,  A61P27/02 ,  A61P37/06 ,  A61P43/00 ,  C07C273/18 ,  C07C275/42 ,  C07C279/28 ,  C07D295/13 ,  C07D295/18 ,  C07D295/185 ,  C07C275/38 ,  A61K31/17

    CPC分类号： C07D295/185 ,  A61K31/5375 ,  C07C275/42 ,  C07C279/28 ,  C07D295/13

    摘要： Compounds of formula (I) wherein Ar is carbocyclic or heterocyclic aryl, or biaryl; Q is O, S or N-CN; X is arylene; V is NH, O, NHOH, CH2 or a direct bond; W is NH, O, NHOH, CH2 or a direct bond; Alk is C2-C7-alkylene or C2-C7-alkylene interrupted by O, S, SO, SO2 or NR3; Y is amino, acylamino, mono- or di- (lower alkyl, aryl or aralkyl)-amino, pyrrolidino, perhydroazepino or a group of the formula (II) in which M1 is N; and M2 is CH2, O, NR3, S, SO or SO2; R1, R2 and R3 are independently hydrogen, lower alkyl, lower alkenyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or aryl-lower alkenyl; Z is lower alkylene or lower alkylene substituted by one or more of lower alkyl, lower alkenyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or aryl-lower alkenyl; or Z is lower alkylene interrupted by O, S, SO, SO2 or NR3; pharmaceutically acceptable esters and amides thereof; and pharmaceutically acceptable salts thereof, which are useful as VLA-4 integrin antagonists.

    摘要翻译： 其中Ar为碳环或杂环芳基或联芳基的式（I）化合物; Q是O，S或N-CN; X是亚芳基; V是NH，O，NHOH，CH 2或直接键; W是NH，O，NHOH，CH 2或直接键; Alk是被O，S，SO，SO2或NR3中断的C2-C7-亚烷基或C2-C7-亚烷基; Y是氨基，酰氨基，单 - 或二 - （低级烷基，芳基或芳烷基） - 氨基，吡咯烷子基，全氢氮杂基或式（II）的基团，其中M1是N; 并且M2是CH 2，O，NR 3，S，SO或SO 2; R1，R2和R3独立地是氢，低级烷基，低级烯基，环烷基，芳基，环烷基 - 低级烷基，芳基 - 低级烷基或芳基 - 低级烯基; Z是被低级烷基，低级烯基，环烷基，芳基，环烷基 - 低级烷基，芳基 - 低级烷基或芳基 - 低级烯基中的一个或多个取代的低级亚烷基或低级亚烷基; 或Z为被O，S，SO，SO 2或NR 3中断的低级亚烷基; 其药学上可接受的酯和酰胺; 和其药学上可接受的盐，其可用作VLA-4整联蛋白拮抗剂。