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9 条记录 (耗时 0.037 秒)

    Neuroprotective poly-guanidino compounds which block presynaptic N and P/Q calcium channels
    7.
    发明授权
    Neuroprotective poly-guanidino compounds which block presynaptic N and P/Q calcium channels 失效
    阻断突触前N和P / Q钙通道的神经保护性聚胍苷

    公开(公告)号：US6063819A

    公开(公告)日：2000-05-16

    申请号：US26415

    申请日：1998-02-18

    申请人： Paul J. Marangos ,  Brian W. Sullivan ,  Torsten Wiemann ,  Anne M. Danks ,  Marina Sragovicz ,  Lewis R. Makings

    发明人： Paul J. Marangos ,  Brian W. Sullivan ,  Torsten Wiemann ,  Anne M. Danks ,  Marina Sragovicz ,  Lewis R. Makings

    IPC分类号： A61K31/00 ,  A61K31/155 ,  A61K31/16 ,  A61K31/165 ,  A61K38/05 ,  A61K31/55 ,  C07C233/05

    CPC分类号： A61K38/05 ,  A61K31/00 ,  A61K31/155 ,  A61K31/16 ,  A61K31/165

    摘要： Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains. Alternately, guanylating agents can be used to directly convert primary amine groups at the ends of spacer chains, on starting reagents, into guanidino groups. These drugs can be injected intravenously into patients suffering from ischemic or hypoxic crises (stroke, cardiac arrest, loss of blood, suffocation, etc.), and can penetrate the blood-brain barrier and suppress the entry of calcium into CNS neurons via N-type and P/Q-type calcium channels, thereby reducing excitotoxic damage in the CNS. These drugs are also useful for suppressing other types of unwanted excessive neuronal activation, such as neuropathic pain.

    摘要翻译： 公开了具有从中心原子或基团向外延伸的至少3个分支的神经保护药物，每个分支在其末端具有胍基。 所有分枝优选应该相同，并以径向方式分布在中心原子或基团周围。 三个分支可以键合到氮原子上，或者四个分支可以与碳原子结合; 其它中心基团包括稳定的芳族，环烷基，杂环或双环结构。 起始试剂用中心原子或基团和与中心原子或基团键合的短“间隔链”末端的反应性基团（例如伯胺或羟基）公开。 衍生自精氨酸（具有末端胍基的氨基酸）的试剂可以使用精氨酰试剂上的保护基团键合到这些中心组分，以确保在间隔链末端具有可及的胍基的所需最终产物。 或者，脒基化剂可用于直接将起始试剂的间隔链末端的伯胺基转化成胍基。 这些药物可以静脉注射给患有缺血性或缺氧危象（中风，心跳停止，血液流失，窒息等）的患者，并可以穿透血脑屏障并抑制钙通过N- 类型和P / Q型钙通道，从而减少CNS中的兴奋性毒性损伤。 这些药物也可用于抑制其他类型的不想要的过量神经元激活，例如神经性疼痛。

    Process for the enzymatic synthesis of 2-deoxy-.beta.-D-galactosides
    8.
    发明授权
    Process for the enzymatic synthesis of 2-deoxy-.beta.-D-galactosides 失效
    酶解合成2-脱氧-β-D-半乳糖苷的方法

    公开(公告)号：US5264352A

    公开(公告)日：1993-11-23

    申请号：US864800

    申请日：1992-04-07

    申请人： Joachim Thiem ,  Torsten Wiemann

    发明人： Joachim Thiem ,  Torsten Wiemann

    IPC分类号： C07H3/04 ,  C12P19/18 ,  C12P19/28 ,  C12P19/44 ,  C12N9/10 ,  C12P19/12

    CPC分类号： C12P19/18 ,  C12P19/28 ,  C12P19/44

    摘要： The invention relates to a process for the enzymatic synthesis of 2-deoxy-.beta.-D-galactosides. The enzyme galactosyltransferase is able to catalyze the transfer of 2-deoxygalactose residues from the donor substrate uridine 5'-diphospho-2-deoxy-D-galactose to N-acetylglucosamine or aspartyl-N-acetylglucosamine or, in the presence of lactose, to terminal glucose.

    摘要翻译： 本发明涉及酶解合成2-脱氧-β-D-半乳糖苷的方法。 酶半乳糖基转移酶能够催化从供体底物尿苷5'-二磷酸-2-脱氧-D-半乳糖向N-乙酰葡糖胺或天冬氨酰-N-乙酰氨基葡萄糖或在乳糖存在下将2-脱氧半乳糖残基转移至 末端葡萄糖。