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    Polyamine analogues as therapeutic and diagnostic agents
    1.
    发明授权
    Polyamine analogues as therapeutic and diagnostic agents 失效
    多胺类似物作为治疗和诊断剂

    公开(公告)号：US07208528B1

    公开(公告)日：2007-04-24

    申请号：US09396523

    申请日：1999-09-15

    申请人： Nicolaas M. J. Vermeulin ,  Christine L. O'Day ,  Heather K. Webb ,  Mark R. Burns ,  Donald E. Bergstrom

    发明人： Nicolaas M. J. Vermeulin ,  Christine L. O'Day ,  Heather K. Webb ,  Mark R. Burns ,  Donald E. Bergstrom

    IPC分类号： A61K31/47 ,  A61K31/425 ,  A61K31/42 ,  A61K31/17 ,  A61K31/16

    CPC分类号： A61K31/16 ,  A61K31/17 ,  A61K31/42 ,  A61K31/425 ,  A61K31/47

    摘要： Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

    摘要翻译： 公开了具有比已知化合物低两个数量级的抑制常数的多胺转运的新型抑制剂。 这些多胺类似物是治疗需要抑制多胺转运或其它多胺结合蛋白（例如癌症和血管成形术后损伤）的疾病的有用的药剂。 公开了获得多胺类似物的新型化学合成方法，包括生产组合多胺文库。 这些方法为诊断和研究测定和治疗产生了理想活动的类似物。 本发明的测定法可用于在与多胺系统相互作用的药物的发现中靶向的高通量筛选。

    Polymer-supported 4-(N-benzyl-N-methylamino)pyridine catalyst and process for same
    5.
    发明授权
    Polymer-supported 4-(N-benzyl-N-methylamino)pyridine catalyst and process for same 失效
    聚合物负载的4-（N-苄基-N-甲基氨基）吡啶催化剂及其方法

    公开(公告)号：US5015706A

    公开(公告)日：1991-05-14

    申请号：US247152

    申请日：1988-09-21

    申请人： Donald W. McQuigg ,  Heather K. Webb ,  Edward E. Sowers

    发明人： Donald W. McQuigg ,  Heather K. Webb ,  Edward E. Sowers

    IPC分类号： B01J31/06 ,  C07D213/74 ,  C08F2/08 ,  C08F12/00 ,  C08F26/06 ,  C08F212/14 ,  C08F226/06

    CPC分类号： C07D213/74

    摘要： A cross-linked polymer-supported 4-(N-benzyl-N-methylamino) pyridine material and process for its preparation in high yield and having effective physical and catalytic properties. The polymer-supported catalyst is characterizd by the suspension copolymerization of an organic phase containing the corresponding vinyl-substituted pyridine monomer, a styrene monomer, and a suitable cross-linking agent and free radical-generating catalyst in the presence of an aqueous phase containing a cellulose ether derivative as the stabilizing agent. The catalyst is further characterized by its yield in excess of 90% by weight and by its predominant and generally spherical and smooth bead form and substantially uniform size that is efficiently hard and durable and possesses sufficient catalytic activity for effective use in acylation, alkylation or other related reactions.

    摘要翻译： 交联聚合物负载的4-（N-苄基-N-甲基氨基）吡啶材料及其高产率制备并具有有效物理和催化性能的方法。 聚合物负载的催化剂的特征是在含有相应的乙烯基取代的吡啶单体，苯乙烯单体和合适的交联剂和产生自由基的催化剂的有机相在含有 纤维素醚衍生物作为稳定剂。 催化剂的特征还在于其产率超过90重量％，其主要和通常为球形和平滑的珠粒形式和基本上均匀的尺寸，其有效硬度和耐久性并且具有足够的催化活性，有效用于酰化，烷基化或其它 相关反应。

    Polymer-supported 4-(N-benzyl-N-methylamino)pyridine catalyst and process for same
    6.
    发明授权
    Polymer-supported 4-(N-benzyl-N-methylamino)pyridine catalyst and process for same 失效
    聚合物负载的4-（N-苄基-N-甲基氨基）吡啶催化剂及其方法

    公开(公告)号：US5229479A

    公开(公告)日：1993-07-20

    申请号：US699694

    申请日：1991-05-14

    申请人： Donald W. McQuigg ,  Heather K. Webb ,  Edward E. Sowers

    发明人： Donald W. McQuigg ,  Heather K. Webb ,  Edward E. Sowers

    IPC分类号： C07D213/74 ,  C08F2/18

    CPC分类号： C07D213/74

    摘要： A cross-linked polymer-supported 4-(N-benzyl-N-methylamino) pyridine material and process for its preparation in high yield and having effective physical and catalytic properties. The polymer-supported catalyst is characterized by the suspension copolymerization of an organic phase containing the corresponding vinyl-substituted pyridine monomer, a styrene monomer, and a suitable cross-linking agent and free radical-generating catalyst in the presence of an aqueous phase containing a cellulose ether derivative as the stabilizing agent. The catalyst is further characterized by its yield in excess of 90% by weight and by its predominant and generally spherical and smooth bead form and substantially uniform size that is efficiently hard and durable and possesses sufficient catalytic activity for effective use in acylation, alkylation or other related reactions.

    摘要翻译： 交联聚合物负载的4-（N-苄基-N-甲基氨基）吡啶材料及其高产率制备并具有有效物理和催化性能的方法。 聚合物负载的催化剂的特征在于在含有相应的乙烯基取代的吡啶单体，苯乙烯单体和合适的交联剂和产生自由基的催化剂的有机相的悬浮共聚， 纤维素醚衍生物作为稳定剂。 催化剂的特征还在于其产率超过90重量％，其主要和通常为球形和平滑的珠粒形式和基本上均匀的尺寸，其有效硬度和耐久性并且具有足够的催化活性，有效用于酰化，烷基化或其它 相关反应。