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29 条记录 (耗时 0.018 秒)

    Polyamine transport inhibitors
    9.
    发明授权
    Polyamine transport inhibitors 失效
    多胺转运抑制剂

    公开(公告)号：US06949679B1

    公开(公告)日：2005-09-27

    申请号：US09529319

    申请日：1998-04-21

    申请人： Richard Poulin ,  Marie Audette ,  Rene Charest-Gaudrealt

    发明人： Richard Poulin ,  Marie Audette ,  Rene Charest-Gaudrealt

    IPC分类号： C07C211/13 ,  C07C211/22 ,  C07C211/23

    CPC分类号： C07C211/22 ,  C07C211/23

    摘要： The present invention describes the design, synthesis and therapeutic use of a variety of novel inhibitors of polyamine transport. The main feature of this class of transport inhibitors is to incorporate a linker or side chain that prevents the uptake of polyamines and helps to conjugate polyamine analogs to form dimers with high inhibitory potency against polyamine uptake. These new compounds incorporate features that are designed to maximize their chemical and metabolic stability and their ability to bind to the polyamine transporter, and to minimize their toxicity by preventing their absorption by the cells. The purpose of such inhibitors is to prevent the uptake or salvaging of circulating polyamines by rapidly proliferating cells such as tumor cells, in order to potentiate the effect of therapeutic inhibitors of polyamine biosynthesis such as alpha-difluoromethylornithene.

    摘要翻译： 本发明描述了多胺转运的各种新型抑制剂的设计，合成和治疗用途。 这类运输抑制剂的主要特征是引入一个阻止多胺摄取的接头或侧链，并有助于多胺类似物的结合形成具有高多胺吸收抑制效能的二聚体。 这些新化合物包含被设计为使其化学和代谢稳定性最大化的能力，以及它们与多胺转运蛋白结合的能力，并通过防止细胞吸收来最小化其毒性。 这种抑制剂的目的是通过快速增殖细胞如肿瘤细胞来防止循环多胺的摄取或回收，以增强多胺生物合成的治疗抑制剂如α-二氟甲基甲锗烷酮的作用。

    Aliphatic propargylamines as selective MAO-B inhibitors and as neuroprotective agents
    10.
    发明授权
    Aliphatic propargylamines as selective MAO-B inhibitors and as neuroprotective agents 失效
    作为选择性MAO-B抑制剂和作为神经保护剂的脂肪族炔丙胺

    公开(公告)号：US5508311A

    公开(公告)日：1996-04-16

    申请号：US108653

    申请日：1993-12-23

    申请人： Peter H. Yu ,  Bruce A. Davis ,  Alan A. Boulton

    发明人： Peter H. Yu ,  Bruce A. Davis ,  Alan A. Boulton

    IPC分类号： A61K31/13 ,  A61K31/185 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07C211/21 ,  C07C211/23 ,  C07C211/24 ,  C07C211/27 ,  C07C215/08 ,  C07C229/12 ,  C07C317/28 ,  C07C323/25 ,  C07C323/65 ,  C12N9/99

    CPC分类号： C07C211/23 ,  C07C215/08 ,  C07C229/12

    摘要： The invention relates to a series of propargylamines, their salts and pharmaceutical compositions containing a compound of formula (III) wherein R.sub.1, R.sub.3 and R.sub.4 are the same or different and represent hydrogen or a straight chain or branched lower alkyl; y is an integer ranging from 0 to 5; z is an integer ranging from 0 to 5; and R.sub.2 is a straight chain or branched alkyl, alkenyl, alkynyl, alkoxy, alkylthio or alkyl sulphinyl group having from 3 to 11 carbon atoms, said group being unsubstituted or substituted with at least one of the substituents selected from hydroxy, aldehyde, oxo, loweracyloxy, halogen, thio, sulfoxide, sulfone, phenyl, halogen-substituted phenyl, hydroxy-substituted phenyl, cycloalkyl having from 3 to 6 carbon atoms and heterocyclic substituents having between 3 and 6 atoms, of which form 1 to 3 are heteroatoms selected from O, S and/or N, and pharmaceutically acceptable salts thereof, in admixture with a pharmaceutically acceptable carrier, excipient or adjuvant. The compounds are useful as selective monoamine oxidase B inhibitors and have demonstrated neuroprotective properties in human and veterinary medicine.

    摘要翻译： PCT No.PCT / CA92 / 00090 Sec。 371日期：1993年12月23日 102（e）日期1993年12月23日PCT提交1992年2月28日PCT公布。 公开号WO92 / 15551 本发明涉及一系列含有式（III）化合物的炔丙胺，其盐和药物组合物，其中R 1，R 3和R 4相同或不同，表示氢或直链或支链低级 烷基; y为0〜5的整数; z为0〜5的整数; 并且R 2是具有3至11个碳原子的直链或支链烷基，烯基，炔基，烷氧基，烷硫基或烷基亚磺酰基，所述基团是未取代的或被至少一个选自羟基，醛，氧代， 低级酰氧基，卤素，硫代，亚砜，砜，苯基，卤素取代的苯基，羟基取代的苯基，具有3至6个碳原子的环烷基和3至6个原子的杂环取代基，其形成1至3个是选自 O，S和/或N及其药学上可接受的盐与药学上可接受的载体，赋形剂或佐剂混合。 该化合物可用作选择性单胺氧化酶B抑制剂，并且已经在人和兽医学中证明了神经保护性质。