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8 条记录 (耗时 0.021 秒)

    Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity prepared therefrom
    3.
    发明授权
    Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity prepared therefrom 失效
    作为选择素拮抗剂的甘油模拟物和由其制备的具有抗炎活性的药物

    公开(公告)号：US06197752B1

    公开(公告)日：2001-03-06

    申请号：US08708475

    申请日：1996-09-05

    申请人： Wolfgang Schmidt ,  Ulrich Sprengard ,  Gerhard Kretzschmar ,  Horst Kunz

    发明人： Wolfgang Schmidt ,  Ulrich Sprengard ,  Gerhard Kretzschmar ,  Horst Kunz

    IPC分类号： A61K3170

    CPC分类号： C07D309/10 ,  C07D307/20

    摘要： The invention relates to novel mimetics of the tetrasaccharides sialyl- Lewis-X (SLeX) and sialyl- Lewis-A (SLeA) having an improved action as inhibitors of cell adhesion, specifically a compound of the formula I in which R1 is —H, —CH3 or —CH2OH, R2 is —H or —OH, R3, R4 and R5 independently of one another are —H, C1-C4-alkyl or —OH, R6, R7, R8, R9 and R10 independently of one another are —H or C1-C4-alkyl D is —O—C(O)—, —C(O)—or —NR6—C(O)—, E is —CR7R8—, —NR7—, or a nitrogen heterocycle of the formula n is 1 or 2, m is 0 or 1, p is an integer from 0 to 10, q is 1 or 2 and X1 and X2 independently of one another are —H, —COOR9, —NR9R10, —OH, —OSO3H, —CH2COOR9 or —CH2OSO3H or together are ═O, to a process for preparing these compounds and to their use as pharmacological active compounds and diagnostic agents.

    摘要翻译： 本发明涉及具有作为细胞粘附抑制剂的改善作用的四糖唾液酸基-LX-X（SLeX）和唾液酸 - 路易斯-A（SLeA）的新型模拟物，特别是式Iin化合物，其中R 1为-H，-CH 3 或-CH 2 OH，R 2是-H或-OH，R 3，R 4和R 5彼此独立地是-H，C 1 -C 4 - 烷基或-OH，R 6，R 7，R 8，R 9和R 10彼此独立地是-H 或C 1 -C 4 - 烷基D为-OC（O） - ， - C（O） - 或-NR 6 -C（O） - ，E为-CR 7 R 8 - ， - NR 7 - 或式 2，m为0或1，p为0至10的整数，q为1或2，X 1和X 2彼此独立地为-H，-COOR 9，-NR 9 R 10，-OH，-OSO 3 H，-CH 2 COOR 9或-CH 2 OSO 3 H 或一起是= O，涉及制备这些化合物的方法及其作为药理活性化合物和诊断剂的用途。

    Carboxylate protective groups, a process for their preparation, their coupling to a functional group, and their use
    5.
    发明授权
    Carboxylate protective groups, a process for their preparation, their coupling to a functional group, and their use 失效
    羧酸酯保护基团，其制备方法，与官能团的偶联及其用途

    公开(公告)号：US5639859A

    公开(公告)日：1997-06-17

    申请号：US440836

    申请日：1995-05-15

    申请人： Horst Kunz ,  Gunther Braum ,  Peter Braun

    发明人： Horst Kunz ,  Gunther Braum ,  Peter Braun

    IPC分类号： C07K1/113 ,  C07C229/06 ,  C07C229/08 ,  C07C229/22 ,  C07C229/36 ,  C07C271/22 ,  C07K1/06 ,  C07K1/12 ,  C07K5/06 ,  C07K5/08 ,  C07K9/00 ,  C12P7/40

    CPC分类号： C07K1/063 ,  C07C229/08 ,  C07C229/22 ,  C07C229/36 ,  C07C271/22 ,  C07K1/12 ,  Y02P20/55

    摘要： Carboxylate protective groups, a process for their preparation, their coupling to a funcitonal group, and their useCarboxylates of polar, hydrophilic alcohols of the formula ##STR1## in which R is an unbranched or branched organic radical which contains, as polar members between aliphatic or araliphatic hydrocarbon bridges, ether oxygens, amine nitrogen groups or a mixture of ether and amine groups which can be incorporated into a cyclic structure, where the total length does not exceed 20 members and where, in the case of polyethylene glycol [(CH.sub.2 --CH.sub.2 --O).sub.n ], n indicates the number of the members and is defined as any integer, andR' is an aliphatic or araliphatic radical which has at least one functional group,are suitable as protective groups since they can be introduced selectively into functional groups of organic compounds and eliminated specifically by lipases.

    摘要翻译： 羧酸酯保护基团，它们的制备方法，它们与功能基团的偶联，以及它们的用途式为“IMAGE”的极性亲水醇的羧酸盐，其中R是无支链或支链的有机基团，其含有作为脂族 或芳族烃桥，醚氧基，胺氮基团或可结合到环状结构中的醚和胺基团的混合物，其中总长度不超过20个成员，其中在聚乙二醇[（CH 2 - CH2-O）n]，n表示成员数，定义为任何整数，R'是具有至少一个官能团的脂族或芳脂族基，适合作为保护基，因为它们可以选择性地引入 有机化合物的官能团，并由脂肪酶特异性消除。

    Allylic side chain-containing solid phase systems, processes for the preparation thereof and the use thereof in solid phase reactions
    7.
    发明授权
    Allylic side chain-containing solid phase systems, processes for the preparation thereof and the use thereof in solid phase reactions 失效
    含烯丙基侧链固相体系，其制备方法及其在固相反应中的应用

    公开(公告)号：US4929671A

    公开(公告)日：1990-05-29

    申请号：US205453

    申请日：1988-06-10

    申请人： Horst Kunz ,  Berthold Dombo

    发明人： Horst Kunz ,  Berthold Dombo

    IPC分类号： C07K1/04 ,  C07K1/113 ,  C07K9/00 ,  C07K14/575 ,  C07K14/655 ,  C07K17/06 ,  C07K17/08 ,  C07K19/00

    CPC分类号： C07K1/042 ,  C07K9/003

    摘要： The present invention provides an allylic side chain-containing solid phase system, in which the allylic side chains are bound to a solid carrier material, of the general formula ##STR1## wherein F is a solid carrier material, R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or alkyl or aryl radicals, R.sup.3 is a linking grouping (spacer), X is a hydroxyl group, a halogen atom, a sulphonate or phosphonate group or an acyloxy radical, acyl in the acyloxy radical being the residue of an aliphatic carboxylic acid or the radical RCO--, R being an organic radical, which is bound via the carbonyl group, and n is the number of side chains bound to the carrier material.The present invention also provides processes for the preparation of these solid phase systems and is also concerned with the use thereof for solid phase reactions.

    摘要翻译： 本发明提供了一种含有烯丙基侧链的固相体系，其中烯丙基侧链与通式（I）的固体载体材料结合，其中F是固体载体材料，R1和R2， 可以相同或不同的是氢或卤素原子或烷基或芳基，R3是连接基团（间隔基），X是羟基，卤素原子，磺酸酯基或膦酸酯基或酰氧基，酰基在 酰氧基是脂族羧酸的残基或基团RCO-，R是通过羰基键合的有机基团，n是与载体材料结合的侧链数。 本发明还提供了制备这些固相体系的方法，并且也涉及其用于固相反应的方法。

    Process for preparation of a solid phase system
    8.
    发明授权
    Process for preparation of a solid phase system 失效
    制备固相体系的方法

    公开(公告)号：US5324786A

    公开(公告)日：1994-06-28

    申请号：US695424

    申请日：1991-05-03

    申请人： Horst Kunz ,  Winfried Kosch ,  Joachim Marz

    发明人： Horst Kunz ,  Winfried Kosch ,  Joachim Marz

    IPC分类号： C07C271/22 ,  C07K1/04 ,  C08F257/02

    CPC分类号： C07C271/22 ,  C07K1/042

    摘要： The invention provides a method for the production of a solid phase system of the formula F--(--R.sup.3 --Y--CO--CR.sup.2 .dbd.CR.sup.1 --CH.sub.2 --X).sub.m using new allyl esters of the formula:X--CH.sub.2 --CR.sup.1 .dbd.CR.sup.2 --CO--Y--R.sup.3 --A (I).R.sup.1 and R.sup.2 are hydrogen, halogen, alkyl or aryl, R.sup.3 is a spacer, X is acyloxy where acyl is the residue of an aliphatic carboxylic acid or is RCO-- in which R is an organic group. Y is oxygen or sulphur or an --NH-- group and A is a grouping which can react with a solid carrier material F, which contains functional groups B. A and B are groups which react with one another with condensation and/or addition and formation of a linkage between the solid carrier material and X--CH.sub.2 --CR.sup.1 .dbd.CR.sup.2 --CO--Y--R.sup.3 --.

    摘要翻译： 本发明提供了使用新的下式的烯丙基酯制备式F - （ - R3-Y-CO-CR2 = CR1-CH2-X）m的固相体系的方法：X-CH2-CR1 = CR2 -CO-Y-R 3 -A（I）。 R 1和R 2是氢，卤素，烷基或芳基，R 3是间隔基，X是酰氧基，其中酰基是脂族羧酸的残基或是RCO-，其中R是有机基团。 Y是氧或硫或-NH-基团，A是可以与含有官能团B的固体载体材料F反应的基团.A和B是在缩合和/或添加和形成时彼此反应的基团 固体载体材料与X-CH2-CR1 = CR2-CO-Y-R3-之间的连接。