公开(公告)号：US12070511B2

公开(公告)日：2024-08-27

申请号：US17851454

申请日：2022-06-28

申请人： GE HEALTHCARE AS

发明人： Mikkel Jacob Thaning ,  Andreas Richard Meijer

IPC分类号： A61K49/10 ,  A61K9/00 ,  A61K31/28 ,  C07D257/00

CPC分类号： A61K49/108 ,  A61K9/0019 ,  A61K31/28 ,  A61K49/106 ,  C07D257/00

摘要： The present invention relates to a method of removal of metal ion impurities, such as calcium, from lanthanide metal complexes of macrocyclic chelators. The method uses a scavenger resin to remove metal ions, displaced from chelator, by an excess of lanthanide ions. Also provided is a method of preparation of MRI contrast agents, from the purified lanthanide metal complex, by the addition of a defined excess chelator.

公开(公告)号：US08440827B2

公开(公告)日：2013-05-14

申请号：US13055788

申请日：2009-07-23

申请人： Katherine J. Franz ,  Katie L. Ciesienski

发明人： Katherine J. Franz ,  Katie L. Ciesienski

IPC分类号： A61M37/00 ,  C07F1/08 ,  A61K31/555 ,  A61P35/00

CPC分类号： C07F1/08 ,  A61K9/0024 ,  A61K41/0042 ,  C07D213/40 ,  C07D213/81 ,  C07D257/00 ,  C07D401/12 ,  C07D405/12

摘要： The present invention provides compounds of Formula I: (I) along with compositions comprising the same and methods of using the same, such as for photodynamic therapy in the treatment of cancer.

摘要翻译： 本发明提供式I化合物：（I）以及包含其的组合物及其使用方法，例如用于治疗癌症的光动力学治疗。

公开(公告)号：US07064117B2

公开(公告)日：2006-06-20

申请号：US10470155

申请日：2002-01-22

申请人： William Alexander Denny ,  William Robert Wilson ,  David Charles Ware ,  Graham John Atwell ,  Jared Bruce Milbank ,  Ralph James Stevenson

发明人： William Alexander Denny ,  William Robert Wilson ,  David Charles Ware ,  Graham John Atwell ,  Jared Bruce Milbank ,  Ralph James Stevenson

IPC分类号： C07D471/04 ,  A61K31/475

CPC分类号： C07D471/04 ,  C07D257/00 ,  C07F11/005 ,  C07F15/065

摘要： This invention relates to a class of heterocycles and their metal complexes, and is particularly concerned with the use of these compounds in the preparation of prodrugs or as prodrugs that may be activated under hypoxic conditions by enzymes or by therapeutic ionising radiation, in the treatment of cancer. The invention also relates to the use of these heterocycles and the corresponding metal complexes in the preparation of medicaments and to compositions including the heterocycles or their metal complexes and to methods for preparing these compounds.

摘要翻译： 本发明涉及一类杂环及其金属络合物，特别涉及这些化合物在制备前体药物中的用途，或作为可在缺氧条件下通过酶或通过治疗电离辐射活化的前药，用于治疗 癌症。 本发明还涉及这些杂环和相应的金属络合物在制备药物中的用途以及包括杂环或其金属络合物的组合物以及制备这些化合物的方法。

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：US09694091B2

公开(公告)日：2017-07-04

申请号：US14715115

申请日：2015-05-18

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： Martin G. Pomper ,  Sangeeta Ray ,  Ronnie C. Mease ,  Catherine Anne Foss

IPC分类号： A61K51/04 ,  A61K31/195 ,  C07D257/00 ,  A61K31/145 ,  A61K31/395 ,  A61K31/4402 ,  A61K38/06 ,  C07D213/38 ,  C07D215/12 ,  G01N33/574 ,  C07D257/02 ,  C07F13/00 ,  C12Q1/37 ,  G01N33/60

CPC分类号： A61K51/0472 ,  A61K31/145 ,  A61K31/195 ,  A61K31/395 ,  A61K31/4402 ,  A61K38/06 ,  A61K51/0402 ,  C07D213/38 ,  C07D215/12 ,  C07D257/00 ,  C07D257/02 ,  C07F13/00 ,  C12Q1/37 ,  G01N33/57434 ,  G01N33/60 ,  G01N2500/04 ,  A61K2300/00

摘要： The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+PC3 PIP tumors.

公开(公告)号：US20110064657A1

公开(公告)日：2011-03-17

申请号：US12666441

申请日：2008-06-26

申请人： Martin Gilbert Pomper ,  Ray Sangeeta ,  Ronnie C. Mease ,  Catherine Foss

发明人： Martin Gilbert Pomper ,  Ray Sangeeta ,  Ronnie C. Mease ,  Catherine Foss

IPC分类号： A61K51/08 ,  C07D401/12 ,  C07D213/56 ,  C07F13/00 ,  C07D257/02 ,  G01N33/20

CPC分类号： A61K51/0472 ,  A61K31/145 ,  A61K31/195 ,  A61K31/395 ,  A61K31/4402 ,  A61K38/06 ,  A61K51/0402 ,  C07D213/38 ,  C07D215/12 ,  C07D257/00 ,  C07D257/02 ,  C07F13/00 ,  C12Q1/37 ,  G01N33/57434 ,  G01N33/60 ,  G01N2500/04 ,  A61K2300/00

摘要： The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.

摘要翻译： 前列腺特异性膜抗原（PSMA）越来越被认为是癌症成像和治疗的可行靶标。 通过将已知的Tc / Re螯合剂连接到具有或不具有可变长度连接体部分的氨基官能化PSMA抑制剂中来制备各种99mTc / Re标记的化合物。 离体生物分布和体内成像证明了与工程化PSMA + PC3 PIP肿瘤的特异性结合程度。

公开(公告)号：US20060018830A1

公开(公告)日：2006-01-26

申请号：US11165721

申请日：2005-06-24

申请人： Enrico Cappelletti ,  Luciano Lattuada ,  Karen Linder ,  Edmund Marinelli ,  Palaniappa Nanjappan ,  Natarajan Raju ,  Kondareddiar Ramalingam ,  Rolf Swenson ,  Michael Tweedle

发明人： Enrico Cappelletti ,  Luciano Lattuada ,  Karen Linder ,  Edmund Marinelli ,  Palaniappa Nanjappan ,  Natarajan Raju ,  Kondareddiar Ramalingam ,  Rolf Swenson ,  Michael Tweedle

IPC分类号： A61K51/00 ,  C07F5/00

CPC分类号： A61K51/088 ,  A61K49/0002 ,  C07C269/04 ,  C07D257/00 ,  C07J41/0005 ,  C07J41/0011 ,  C07J43/003 ,  C07K14/57572 ,  C07C271/22

摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

公开(公告)号：US20050038249A1

公开(公告)日：2005-02-17

申请号：US10928595

申请日：2004-08-30

申请人： William Denny ,  William Wilson ,  David Ware ,  Graham Atwell ,  Jared Milbank ,  Ralph Stevenson

发明人： William Denny ,  William Wilson ,  David Ware ,  Graham Atwell ,  Jared Milbank ,  Ralph Stevenson

IPC分类号： C07D215/30 ,  A61K31/404 ,  A61K31/437 ,  A61K31/47 ,  A61P35/00 ,  A61P43/00 ,  C07D209/60 ,  C07D255/02 ,  C07D257/00 ,  C07D257/02 ,  C07D471/04 ,  C07F11/00 ,  C07F15/06 ,  C07F15/00

CPC分类号： C07D471/04 ,  C07D257/00 ,  C07F11/005 ,  C07F15/065

摘要： This invention relates to a class of heterocycles and their metal complexes, and is particularly concerned with the use of these compounds in the preparation of prodrugs or as prodrugs that may be activated under hypoxic conditions by enzymes or by therapeutic ionising radiation, in the treatment of cancer. The invention also relates to the use of these heterocycles and the corresponding metal complexes in the preparation of medicaments and to compositions including the heterocycles or their metal complexes and to methods for preparing these compounds.

摘要翻译： 本发明涉及一类杂环及其金属络合物，特别涉及这些化合物在制备前体药物中的用途，或作为可在缺氧条件下通过酶或通过治疗电离辐射活化的前药，用于治疗 癌症。 本发明还涉及这些杂环和相应的金属络合物在制备药物中的用途以及包括杂环或其金属络合物的组合物以及制备这些化合物的方法。

公开(公告)号：US20040138195A1

公开(公告)日：2004-07-15

申请号：US10470155

申请日：2004-01-29

发明人： William Alexander Denny ,  William Robert Wilson ,  David Charles Ware ,  Graham John Atwell ,  Jared Bruce Milbank ,  Ralph James Stevenson

IPC分类号： A61K031/555 ,  C07F015/06 ,  C07F011/00

CPC分类号： C07D471/04 ,  C07D257/00 ,  C07F11/005 ,  C07F15/065

摘要： This invention relates to a class of heterocycles and their metal complexes, and is particularly concerned with the use of these compounds in the preparation of prodrugs or as prodrugs that may be activated under hypoxic conditions by enzymes or by therapeutic ionising radiation, in the treatment of cancer. The invention also relates to the use of these heterocycles and the corresponding metal complexes in the preparation of medicaments and to compositions including the heterocycles or their metal complexes and to methods for preparing these compounds.

摘要翻译： 本发明涉及一类杂环及其金属络合物，特别涉及这些化合物在制备前体药物中的用途，或作为可在缺氧条件下通过酶或通过治疗电离辐射活化的前药，用于治疗 癌症。 本发明还涉及这些杂环和相应的金属络合物在制备药物中的用途以及包括杂环或其金属络合物的组合物以及制备这些化合物的方法。

公开(公告)号：US20240190830A1

公开(公告)日：2024-06-13

申请号：US18284515

申请日：2022-03-23

申请人： BRACCO IMAGING S.P.A. ,  SERICHIM SRL

发明人： Walter BARATTA ,  Rosario FIGLIOLIA ,  Pietro DELOGU ,  Ilaria ADAMO ,  Mariangela BOCCALON ,  Federica BUONSANTI

IPC分类号： C07D257/00

CPC分类号： C07D257/00

摘要： The present invention relates to a process for the preparation of Cyclen. in its turn widely employed in the manufacturing of a variety of macrocyclic gadolinium complexes for use as MRI contrast agents. The said process comprises an efficient coupling of glyoxal with triethylene tetramine and the subsequent reduction of the obtained intermediate derivative with an aluminium based reducing agent. The process is particularly advantageous for the industrial scale as it avoids the use and/or formation of hazardous compounds and further provides for Cyclen manufacturing in high yields and purity.