公开(公告)号：US4452774A

公开(公告)日：1984-06-05

申请号：US373511

申请日：1982-04-30

Applicant: Alun G. Jones ,  Alan Davison ,  Michael J. Abrams

Inventor： Alun G. Jones ,  Alan Davison ,  Michael J. Abrams

IPC: A61K20060101 ,  A61K51/00 ,  A61K51/12 ,  C07C20060101 ,  C07C291/10 ,  C07F1/08 ,  C07F13/00 ,  C12Q20060101 ,  G01N20060101 ,  G01N33/60 ,  A61K43/00 ,  A61K49/00 ,  C07C121/20

CPC classification number: A61K51/1234 ,  A61K51/025 ,  C07C251/00 ,  C07F13/005 ,  A61K2123/00

Abstract: A coordination complex of an isonitrile ligand and radionuclide such as Tc, Ru, Co, Pt, Fe, Os, Ir, W, Re, Cr, Mo, Mn, Ni, Rh, Pd, Nb and Ta, is useful as a diagnostic agent for labelling liposomes or vesicles, and selected living cells containing lipid membranes, such as blood clots, myocardial tissue, gall bladder tissue, etc.

Abstract translation: 异氰酸酯配体和放射性核素如Tc，Ru，Co，Pt，Fe，Os，Ir，W，Re，Cr，Mo，Mn，Ni，Rh，Pd，Nb和Ta的配位络合物可用作诊断 用于标记脂质体或囊泡的试剂，以及选择的含有脂质膜的活细胞，例如血块，心肌组织，胆囊组织等。

公开(公告)号：US20080226550A1

公开(公告)日：2008-09-18

申请号：US12017328

申请日：2008-01-21

Applicant: Ashfaq Mahmood ,  Matthias Friebe ,  Cristina Bolzati ,  Alun G. Jones ,  Alan Davison

Inventor： Ashfaq Mahmood ,  Matthias Friebe ,  Cristina Bolzati ,  Alun G. Jones ,  Alan Davison

IPC: A61K51/04 ,  C07F5/00 ,  C07D211/00 ,  A61P35/00 ,  C07D295/00

CPC classification number: C07D295/13 ,  A61K51/0478 ,  C07C323/41 ,  C07F13/005 ,  C07K5/06026

Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tumors, e.g., carcinomas, melanomas and other tumors. In another embodiment, the invention relates to methods of imaging tumors using radiolabeled metal complexes. Preferred radiolabeled complexes for imaging tumors include technetium and rhenium complexes. The high tumor uptake and significant tumor/nontumor ratios of the technetium complexes of the invention indicate that such small technetium-99m-based molecular probes can be developed as in-vivo diagnostic agents for melanoma and its metastases. In yet another embodiment, the invention relates to methods of treatment of tumors using a radiolabeled metal complex as a radiopharmaceutical agent to treat the tumor.

Abstract translation: 本发明涉及适用于肿瘤例如癌，黑素瘤和其他肿瘤的成像或治疗性治疗的化合物及其相关的锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物成像肿瘤的方法。 用于成像肿瘤的优选放射性标记复合物包括锝和铼络合物。 本发明的锝络合物的高肿瘤摄取和显着的肿瘤/非肿瘤比率表明，这种基于锝-99m的小分子探针可以作为黑色素瘤及其转移的体内诊断剂开发。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物作为放射性药物治疗肿瘤的方法治疗肿瘤。

公开(公告)号：US6054114A

公开(公告)日：2000-04-25

申请号：US852825

申请日：1997-05-07

Applicant: Peter T. Lansbury, Jr. ,  Hogyu Han ,  Cheon-Gyu Cho ,  Weiguo Zhen ,  James D. Harper ,  Alan Davison

Inventor： Peter T. Lansbury, Jr. ,  Hogyu Han ,  Cheon-Gyu Cho ,  Weiguo Zhen ,  James D. Harper ,  Alan Davison

IPC: A61K49/06 ,  A61K51/04 ,  C07B59/00 ,  C07F13/00 ,  A61K51/00 ,  A61K49/00

CPC classification number: C07F13/005 ,  A61K49/06 ,  A61K51/0478 ,  A61K51/0482 ,  C07B59/002 ,  A61K2123/00

Abstract: Novel organometallic compounds for binding amyloid are described. Methods using such compounds for determining by imaging the localization or quantification of amyloid fibrils in a mammal, for diagnosing the degree of progression of Alzheimer's disease in a mammal, for monitoring the response to a therapy in a mammal having Alzheimer's disease, for identifying an agent useful for treating Alzheimer's disease, for treating Alzheimer's disease, and for detecting the presence of the infectious form of the prion protein, are also described.

Abstract translation: 描述了用于结合淀粉样蛋白的新型有机金属化合物。 使用这些化合物来测定哺乳动物淀粉状蛋白原纤维的定位或定量的方法，用于诊断哺乳动物中阿尔茨海默病的进展程度，用于监测对具有阿尔茨海默病的哺乳动物的治疗的反应，用于鉴定药剂 也描述了用于治疗阿尔茨海默病，用于治疗阿尔茨海默病和用于检测朊病毒蛋白的感染形式的存在的方法。

公开(公告)号：US4707544A

公开(公告)日：1987-11-17

申请号：US675540

申请日：1984-11-28

Applicant: Alun G. Jones ,  Alan Davison ,  Michael J. Abrams

Inventor： Alun G. Jones ,  Alan Davison ,  Michael J. Abrams

IPC: G01N33/60 ,  A61K51/04 ,  C07F3/06 ,  C07F9/00 ,  C07F11/00 ,  C07F13/00 ,  C07F15/00 ,  G01N33/58 ,  A61K43/00 ,  A61K49/00 ,  C07C121/20 ,  C07F1/08

CPC classification number: C07F13/00 ,  A61K51/0476 ,  C07F3/06 ,  A61K2123/00

Abstract: A method for preparing a coordination complex of an isonitrile ligand and radionuclide such as Tc, Ru, Co, Pt, Fe, Os, Ir, W, Re, Cr, Mo, Mn, Ni, Rh, Pd, Nb and Ta is disclosed. The method comprises preparing a soluble metal adduct of said isonitrile ligand by admixing said ligand with a salt of a displaceable metal having a complete d-electron shell selected from the group consisting of Zn, Ga, Cd, In, Sn, Hg, Tl, Pb and Bi to form a soluble metal-isonitrile salt, and admixing said metal isonitrile salt with a salt comprising said radioactive metal in a suitable solvent to displace said displaceable metal with the radioactive metal thereby forming said coordination. The complex is useful as a diagnostic agent for labelling liposomes or vesicles, and selected living cells containing lipid membranes, such as blood clots, myocardial tissue, gall bladder tissue, etc.

Abstract translation: 公开了制备诸如Tc，Ru，Co，Pt，Fe，Os，Ir，W，Re，Cr，Mo，Mn，Ni，Rh，Pd，Nb和Ta之类的异腈配体和放射性核素的配位络合物的方法 。 该方法包括通过将所述配体与可选择的金属的盐混合制备所述异腈配体的可溶性金属加合物，所述可置换金属的盐具有选自Zn，Ga，Cd，In，Sn，Hg，Tl， Pb和Bi以形成可溶性金属 - 异腈盐，并将所述金属异腈盐与包含所述放射性金属的盐在合适的溶剂中混合，以用放射性金属置换所述可置换金属，从而形成所述配位。 该复合物可用作标记脂质体或囊泡的诊断剂，以及选择的含有脂质膜的活细胞如血凝块，心肌组织，胆囊组织等。

公开(公告)号：US20060159617A1

公开(公告)日：2006-07-20

申请号：US10534225

申请日：2003-11-08

Applicant: Ashfaq Mahmood ,  Zhen Cheng ,  Alun Jones ,  Alan Davison

Inventor： Ashfaq Mahmood ,  Zhen Cheng ,  Alun Jones ,  Alan Davison

IPC: A61K51/00 ,  C07F13/00 ,  C07F5/00 ,  C07D211/26

CPC classification number: C07C323/41 ,  A61K51/0455 ,  A61K51/0478 ,  C07C323/25 ,  C07D211/14 ,  C07D211/52 ,  C07D211/58 ,  C07F13/005

Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates the methods of imaging tissues, organs or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.

Abstract translation: 本发明涉及适用于组织，器官或肿瘤的成像或治疗性治疗的化合物及其相关锝和铼络合物。 在另一个实施方案中，本发明涉及使用放射性标记的金属络合物，特别是表达本发明的化合物或复合物具有亲和力的某些受体的组织，器官或肿瘤来成像组织，器官或肿瘤的方法。 本发明还涉及治疗癌症的方法，特别是那些表达本发明化合物或复合物具有亲和力的某些受体的那些癌症系。 在另一个实施方案中，本发明提供使用对受体或神经受体成像和/或抑制的亲和力的本发明化合物或复合物成像和/或抑制受体或神经受体的方法。

公开(公告)号：US5670048A

公开(公告)日：1997-09-23

申请号：US601378

申请日：1996-02-14

Applicant: Dale Alan Davison ,  Henry LeRoy Walters

Inventor： Dale Alan Davison ,  Henry LeRoy Walters

IPC: B01D11/02 ,  B01D11/00 ,  B65D53/00

CPC classification number: B01D11/0203

Abstract: A preparatory supercritical extraction cartridge includes a chamber for sample having a volume in the range of 20 cubic centimeters to 2,000 cubic centimeters. An inlet and an outlet are fastened to the cartridge walls by threads and sealed to said cartridge walls With spring loaded seals so that they can be removed with a torque requirement of less than 35 pound inches. Inlet and outlet tubing are fastened to the inlet and outlet by quick release connectors.

Abstract translation: 准备超临界提取盒包括具有20立方厘米至2,000立方厘米范围内的体积的样品室。 入口和出口通过螺纹固定到盒壁上，并用弹簧加载的密封件密封到所述盒壁上，使得它们可以以小于35磅英寸的扭矩要求去除。 入口和出口管道通过快速释放连接器固定到入口和出口。

公开(公告)号：US4746505A

公开(公告)日：1988-05-24

申请号：US727582

申请日：1985-04-26

Applicant: Alun G. Jones ,  John Lister-James ,  Alan Davison

Inventor： Alun G. Jones ,  John Lister-James ,  Alan Davison

IPC: A61K51/00 ,  A61K51/04 ,  C07C67/00 ,  C07C313/00 ,  C07C323/41 ,  C07C323/60 ,  C07C325/00 ,  C07C327/36 ,  C07F13/00 ,  A61K43/00 ,  A61K49/00 ,  A61K49/02 ,  C07C149/23

CPC classification number: C07F13/005 ,  A61K51/04 ,  A61K2123/00

Abstract: A bisamide-bisthiol ligand containing fatty acid substituted thiol useful for producing Tc-labelled radiodiagnostic imaging agents is described. The ligand forms a complex with the radionuclide .sup.99m Tc suitable for administration as a radiopharmaceutical to obtain images of the heart for diagnosis of myocardial disfunction.

Abstract translation: 描述了含有用于制备Tc-标记的放射诊断显像剂的含有脂肪酸取代的硫醇的双酰胺 - 二硫醇配体。 配体与放射性核素99mTc形成复合物，适合作为放射性药物的给药，以获得用于心肌功能障碍诊断的心脏图像。