公开(公告)号：US6165996A

公开(公告)日：2000-12-26

申请号：US104695

申请日：1998-06-25

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

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

IPC分类号： G01R33/28 ,  A61B5/055 ,  A61K31/13 ,  A61K31/131 ,  A61K31/132 ,  A61K31/133 ,  A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/407 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4985 ,  A61K31/551 ,  A61K31/663 ,  A61K31/675 ,  A61K47/48 ,  A61K49/00 ,  A61K49/04 ,  A61K49/06 ,  A61K51/04 ,  A61P3/00 ,  A61P7/00 ,  A61P17/00 ,  A61P17/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/10 ,  A61P31/14 ,  A61P35/00 ,  A61P37/06 ,  A61P39/04 ,  A61P39/06 ,  C07C215/14 ,  C07D255/02 ,  C07D255/04 ,  C07D257/00 ,  C07D257/02 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D487/22 ,  C07F9/6515 ,  C07F9/6524 ,  C07F9/6561 ,  C09K3/00 ,  G01N24/08 ,  C07B47/00

CPC分类号： 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

摘要： 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).

摘要翻译： 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缀合的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去除。 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， 。

公开(公告)号：US06583182B1

公开(公告)日：2003-06-24

申请号：US10008765

申请日：2001-11-30

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

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

IPC分类号： A61K31132

CPC分类号： 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

摘要： 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).

公开(公告)号：US5874573A

公开(公告)日：1999-02-23

申请号：US669698

申请日：1996-06-24

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

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

IPC分类号： G01R33/28 ,  A61B5/055 ,  A61K31/13 ,  A61K31/131 ,  A61K31/132 ,  A61K31/133 ,  A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/407 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4985 ,  A61K31/551 ,  A61K31/663 ,  A61K31/675 ,  A61K47/48 ,  A61K49/00 ,  A61K49/04 ,  A61K49/06 ,  A61K51/04 ,  A61P3/00 ,  A61P7/00 ,  A61P17/00 ,  A61P17/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/10 ,  A61P31/14 ,  A61P35/00 ,  A61P37/06 ,  A61P39/04 ,  A61P39/06 ,  C07C215/14 ,  C07D255/02 ,  C07D255/04 ,  C07D257/00 ,  C07D257/02 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D487/22 ,  C07F9/6515 ,  C07F9/6524 ,  C07F9/6561 ,  C09K3/00 ,  C07B47/00 ,  C07D225/00

CPC分类号： A61K47/48076 ,  A61K31/13 ,  A61K31/131 ,  A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/395 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/44 ,  A61K31/675 ,  A61K47/48023 ,  A61K49/0002 ,  A61K49/04 ,  A61K49/06 ,  A61K51/0478 ,  A61K51/0482 ,  C07D255/02 ,  C07D255/04 ,  C07D257/00 ,  C07D403/14 ,  C07D405/14 ,  C07D487/08 ,  C07D487/10 ,  C07F9/6515 ,  C07F9/6524 ,  C07F9/6561 ,  Y10S514/836

摘要： 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 response, 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).

摘要翻译： 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缀合的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去除。 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，因此可用于治疗瘤形成，感染，炎症，免疫应答和终止妊娠。 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， 。