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    Compounds with chelation affinity and selectivity for first transition series elements: use in medical therapy and diagnosis
    3.
    发明授权
    Compounds with chelation affinity and selectivity for first transition series elements: use in medical therapy and diagnosis 失效
    具有螯合亲和性和对第一过渡系列元素选择性的化合物：用于医学治疗和诊断

    公开(公告)号：US06469162B1

    公开(公告)日：2002-10-22

    申请号：US09664952

    申请日：2000-09-19

    Applicant: Harry S. Winchell ,  Joseph Y. Klein ,  Elliot D. Simhon ,  Rosa L. Cyjon ,  Ofer Klein ,  Haim Zaklad

    Inventor： Harry S. Winchell ,  Joseph Y. Klein ,  Elliot D. Simhon ,  Rosa L. Cyjon ,  Ofer Klein ,  Haim Zaklad

    IPC: C07D22500

    CPC classification number: C07D405/14 ,  A61K31/13 ,  A61K31/131 ,  A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/395 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/44 ,  A61K31/675 ,  A61K47/54 ,  A61K47/547 ,  A61K49/0002 ,  A61K49/04 ,  A61K49/06 ,  A61K51/0478 ,  A61K51/0482 ,  C07D255/02 ,  C07D255/04 ,  C07D257/00 ,  C07D403/14 ,  C07D487/08 ,  C07D487/10 ,  C07F9/6515 ,  C07F9/6524 ,  C07F9/6561 ,  Y10S514/836

    Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy. Since these compounds are capable of descreasing the in vivo availability of tissue iron they are useful in management of free radical mediated tissue damage, and oxidation mediated tissue damage. When combined with radioisotopic or paramagnetic cations of first transition series elements, or elements with chemical properties similar to those of first transition series elements, prior to their administration, the resulting complexes are useful as diagnostic agents in nuclear medicine and magnetic resonance imaging (MRI).

    Abstract translation: 本发明涉及合成和使用具有螯合亲和性和对第一转变序列元件的选择性的一类化合物。 施用游离或缀合的化合物或游离或共轭化合物的生理盐导致第一过渡系列元件的体内生物利用度降低和/或从具有相似化学性质的第一过渡系列元件和元件的体内移除。 这些特征使得这些化合物可用于治疗与具有相似化学性质的第一过渡系列元件和元件的身体过剩相关的疾病。 本发明证明这些化合物抑制哺乳动物，细菌和真菌细胞复制，因此可用于治疗肿瘤形成，感染，炎症，免疫反应和终止妊娠。 由于这些化合物能够降低组织铁的体内可利用性，因此它们可用于管理自由基介导的组织损伤和氧化介导的组织损伤。 当与第一过渡系列元件的放射性同位素或顺磁性阳离子或具有与第一过渡系列元件类似的化学特性的元素组合时，在其给药之前，所得复合物可用作核医学和磁共振成像（MRI）中的诊断剂， 。

    Processes for synthesis of cyclic and linear polyamine chelators containing N-monosubstituted coordinating arms
    7.
    发明授权
    Processes for synthesis of cyclic and linear polyamine chelators containing N-monosubstituted coordinating arms 失效

    公开(公告)号：US06576760B2

    公开(公告)日：2003-06-10

    申请号：US09759092

    申请日：2001-01-11

    Applicant: Harry S. Winchell ,  Rosa L. Cyjon ,  Joseph Y. Klein ,  Elliot D. Simhon ,  Ofer Klein ,  Haim Zaklad

    Inventor： Harry S. Winchell ,  Rosa L. Cyjon ,  Joseph Y. Klein ,  Elliot D. Simhon ,  Ofer Klein ,  Haim Zaklad

    IPC: C07D24500

    CPC classification number: C07F9/3808 ,  C07F9/4006

    Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine. The process involves the use of a trialkyl or triaryl phosphite, and unlike the prior art, monosubstitutions at all nitrogen atoms are achieved in preference over disubstitutions at the terminal primary amines. Finally, a novel class of N,N′,N″-tris(methylenephosphonate or methylephosphonic acid-substituted)-1,4,7-triazaheptanes are disclosed as new compositions of matter.

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