公开(公告)号：US06524554B1

公开(公告)日：2003-02-25

申请号：US09285280

申请日：1999-04-02

Applicant: David Scott Edwards ,  Milind Rajopadhye

Inventor： David Scott Edwards ,  Milind Rajopadhye

IPC: A61K4904

CPC classification number: C07K7/06 ,  A61K51/088

Abstract: The present invention provides novel radiopharmaceuticals comprising one to three pentapeptides, X1X2X3X4X5, independently attached to a metal chelator or bonding moiety, Ch, to which is attached a Tc-99m, Re-186, or Re-188, optionally further comprising a linking group, Ln, between-the peptides and the chelator or bonding moiety. The pentapeptide sequence binds to the tuftsin receptor and is attached at the N-terminus to Ln or Ch. These radiopharmaceuticals are useful for the diagnosis of infection and inflammation, reagents and kits useful for preparing the radiopharmaceuticals, methods of imaging sites of infection and/or inflammation in a patient, and methods of diagnosing diseases associated with infection or inflammation in patients in need of such diagnosis.

Abstract translation: 本发明提供了包含一至三个五肽X1X2X3X4X5的新型放射性药物，其独立地连接到金属螯合剂或结合部分Ch上，其连接有Tc-99m，Re-186或Re-188，任选地还包含连接基团 ，Ln，肽与螯合剂或结合部分之间。 五肽序列与簇绒蛋白受体结合，并在N末端连接至Ln或Ch。 这些放射性药物可用于感染和炎症的诊断，可用于制备放射性药物的试剂和试剂盒，成像患者感染和/或炎症部位的成像方法，以及诊断与感染或炎症有关的疾病的方法 这样的诊断。

公开(公告)号：US5750088A

公开(公告)日：1998-05-12

申请号：US476296

申请日：1995-06-07

Applicant: Michael Sworin ,  Milind Rajopadhye ,  Thomas David Harris ,  David Scott Edwards ,  Edward Hollister Cheesman ,  Shuang Liu

Inventor： Michael Sworin ,  Milind Rajopadhye ,  Thomas David Harris ,  David Scott Edwards ,  Edward Hollister Cheesman ,  Shuang Liu

IPC: A61K31/00 ,  A61K38/12 ,  A61K49/04 ,  A61K51/00 ,  A61K51/04 ,  A61K51/08 ,  C07B59/00 ,  C07D213/82 ,  C07D257/00 ,  C07D259/00 ,  C07D277/60 ,  C07D401/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07K5/10 ,  C07K5/103 ,  C07K7/64 ,  C07K14/75 ,  C07K17/02 ,  A61K38/00

CPC classification number: C07D213/82 ,  A61K51/04 ,  A61K51/082 ,  A61K51/088 ,  C07B59/008 ,  C07D401/12 ,  C07D401/14 ,  C07K14/75 ,  A61K2123/00

Abstract: This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.

Abstract translation: 本发明提供用于制备用作诊断心血管疾病，感染，炎症和癌症的成像剂的放射性药物的新型试剂，包含所述试剂的诊断试剂和可用于制备所述试剂的中间体化合物。 试剂由稳定的腙修饰的生物活性分子组成，其与γ发射放射性同位素反应形成放射性药物，其选择性地定位在疾病部位，从而允许使用γ闪烁扫描获得基因座的图像。

公开(公告)号：US6010679A

公开(公告)日：2000-01-04

申请号：US13320

申请日：1998-01-26

Applicant: David Scott Edwards ,  Shuang Liu

Inventor： David Scott Edwards ,  Shuang Liu

IPC: A61K51/00 ,  A61K51/04 ,  A61K51/08 ,  A61M36/00 ,  C07B59/00 ,  C07F5/00 ,  C07F13/00 ,  C07K7/56 ,  C07K14/75 ,  A61M36/14

CPC classification number: C07K14/75 ,  A61K51/0476 ,  A61K51/0497 ,  A61K51/082 ,  A61K51/088 ,  C07B59/004 ,  C07B59/008 ,  C07K7/56 ,  A61K2123/00

Abstract: This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure:[(Q).sub.d 'L.sub.n -C.sub.h '].sub.x -M.sub.t (A.sub.L1).sub.y (A.sub.L2)z;wherein the variables are as defined herein.

Abstract translation: 本发明提供了可用作诊断心血管疾病，感染性疾病和癌症的成像剂的新型放射性药物。 放射性药物由磷化氢或胂连接的锝-99m标记的肼或二氮嗪修饰的生物活性分子组成，其选择性地定位在疾病部位，从而允许使用γ闪烁扫描获得基因座的图像。 本发明还提供了使用放射性药物和包含放射性药物前体的试剂盒的方法。 本发明的放射性药物具有以下结构：[（Q）d'Ln-Ch'] x-Mt（AL1）y（AL2）z;其中变量如本文所定义。

公开(公告)号：US06869590B2

公开(公告)日：2005-03-22

申请号：US10080974

申请日：2002-02-22

Applicant: David Scott Edwards ,  Shuang Liu

Inventor： David Scott Edwards ,  Shuang Liu

IPC: C07D213/89 ,  A61K9/08 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61K47/20 ,  A61K47/22 ,  A61K47/46 ,  A61K49/00 ,  A61K49/04 ,  A61K51/00 ,  A61K51/04 ,  C07C235/64 ,  C07F1/08 ,  C07F13/00 ,  A61M36/14

CPC classification number: A61K51/0497

Abstract: Detectably labeled macrophage scavenger receptor antagonists useful for the diagnosis and monitoring of various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque, coronary artery disease, renal disease, thrombosis, transient ischemia due to clotting, stroke, myocardial infarction, organ transplant, organ failure and hypercholesterolemia.

公开(公告)号：US6015904A

公开(公告)日：2000-01-18

申请号：US956313

申请日：1997-10-23

Applicant: Michael Sworin ,  Milind Rajopadhye ,  Thomas David Harris ,  David Scott Edwards ,  Edward Hollister Cheesman ,  Shuang Liu

Inventor： Michael Sworin ,  Milind Rajopadhye ,  Thomas David Harris ,  David Scott Edwards ,  Edward Hollister Cheesman ,  Shuang Liu

IPC: A61K31/00 ,  A61K38/12 ,  A61K49/04 ,  A61K51/00 ,  A61K51/04 ,  A61K51/08 ,  C07B59/00 ,  C07D213/82 ,  C07D257/00 ,  C07D259/00 ,  C07D277/60 ,  C07D401/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07K5/10 ,  C07K5/103 ,  C07K7/64 ,  C07K14/75 ,  C07K17/02

CPC classification number: C07D213/82 ,  A61K51/04 ,  A61K51/082 ,  A61K51/088 ,  C07B59/008 ,  C07D401/12 ,  C07D401/14 ,  C07K14/75 ,  A61K2123/00

Abstract: This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.

Abstract translation: 本发明提供用于制备用作诊断心血管疾病，感染，炎症和癌症的成像剂的放射性药物的新型试剂，包含所述试剂的诊断试剂和可用于制备所述试剂的中间体化合物。 试剂由稳定的腙修饰的生物活性分子组成，其与γ发射放射性同位素反应形成放射性药物，其选择性地定位在疾病部位，从而允许使用γ闪烁扫描获得基因座的图像。

公开(公告)号：US5744120A

公开(公告)日：1998-04-28

申请号：US415908

申请日：1995-04-03

Applicant: David Scott Edwards ,  Shuang Liu

Inventor： David Scott Edwards ,  Shuang Liu

IPC: A61K51/00 ,  A61K51/04 ,  A61K51/08 ,  A61M36/00 ,  C07B59/00 ,  C07F5/00 ,  C07F13/00 ,  C07K7/56 ,  C07K14/75 ,  A61M36/14

CPC classification number: C07K14/75 ,  A61K51/0476 ,  A61K51/0497 ,  A61K51/082 ,  A61K51/088 ,  C07B59/004 ,  C07B59/008 ,  C07K7/56 ,  A61K2123/00

Abstract: This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are comprised of phosphine or arsine ligated technetium-99m labeled hydrazino or diazino modified biologically active molecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. This invention also provides methods for using the radiopharmaceuticals and kits comprising radiopharmaceutical precursors. The radiopharmaceuticals of this invention have the structure: �(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z ; wherein the variables are as defined herein.

公开(公告)号：US06974567B2

公开(公告)日：2005-12-13

申请号：US10641688

申请日：2003-08-14

Applicant: David Scott Edwards ,  Shuang Liu

Inventor： David Scott Edwards ,  Shuang Liu

IPC: C07D213/89 ,  A61K9/08 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61K47/20 ,  A61K47/22 ,  A61K47/46 ,  A61K49/00 ,  A61K49/04 ,  A61K51/00 ,  A61K51/04 ,  C07C235/64 ,  C07F1/08 ,  C07F13/00

CPC classification number: A61K51/0497

Abstract: Detectably labeled macrophage scavenger receptor antagonists useful for the diagnosis and monitoring of various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque, coronary artery disease, renal disease, thrombosis, transient ischemia due to clotting, stroke, myocardial infarction, organ transplant, organ failure and hypercholesterolemia.

Abstract translation: 可检测标记的巨噬细胞清道夫受体拮抗剂，可用于诊断和监测各种心血管疾病，包括但不限于动脉粥样硬化，易损斑块，冠状动脉疾病，肾脏疾病，血栓形成，由于凝血，中风，心肌梗死，器官移植，器官的短暂性缺血 失败和高胆固醇血症。

公开(公告)号：US5879659A

公开(公告)日：1999-03-09

申请号：US808699

申请日：1997-02-28

Applicant: David Scott Edwards ,  Shuang Liu

Inventor： David Scott Edwards ,  Shuang Liu

IPC: A61B20060101 ,  A61K20060101 ,  A61K51/08 ,  A61M20060101 ,  A61N20060101 ,  A61K51/00 ,  A61K38/12 ,  A61M36/14 ,  C07F5/00

CPC classification number: A61K51/088 ,  A61K51/082 ,  A61K2123/00

Abstract: This invention relates to novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer, and to kits useful for their preparation. The radiopharmaceuticals of this invention are comprised of a transition metal radionuclide, a transition metal chelator, a biologically active group connected to said chelator, a first ancillary ligand, a second ancillary ligand capable of stabilizing the radiopharmaceutical, optionally having a linking group between said chelator and said biologically active group. Preferred radiopharmaceuticals of this invention have the formula:�(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z,wherein the shown variables are as defined herein.

Abstract translation: 本发明涉及可用作诊断心血管疾病，感染性疾病和癌症的成像剂的新型放射性药物，以及可用于其制备的试剂盒。 本发明的放射性药物包括过渡金属放射性核素，过渡金属螯合剂，与所述螯合剂连接的生物活性基团，第一辅助配体，能稳定放射性药物的第二辅助配体，任选地在所述螯合剂之间具有连接基团 并表示生物活性组。 本发明优选的放射性药物具有下式：[（Q）d'Ln-Ch'] x-Mt（AL1）y（AL2）z，其中所示变量如本文所定义。

公开(公告)号：US5693324A

公开(公告)日：1997-12-02

申请号：US391756

申请日：1995-02-21

Applicant: David Scott Edwards

Inventor： David Scott Edwards

IPC: A61K51/00 ,  A61K51/04 ,  C07B59/00 ,  C07F1/00 ,  C07F1/08 ,  C07F9/00 ,  C07F11/00 ,  C07F13/00 ,  C07F15/00 ,  C07F15/02 ,  C07F15/04 ,  C07F15/06

CPC classification number: C07F13/005 ,  A61K51/0476 ,  C07B59/004 ,  C07F1/005 ,  A61K2123/00

Abstract: Tris(isonitrile) copper(I) sulfate complexes and their use in synthetic methods for making radionuclide isonitrile coordination complexes such as �.sup.99m Tc(1-isocyano-2-methoxy-2-methylpropane).sub.6 !.sup.+. The coordination complexes are useful as radiopharmaceutical imaging agents.

Abstract translation: 三（异腈）铜（I）硫酸盐络合物及其在制备放射性核素异腈配位络合物如[99mTc（1-异氰基-2-甲氧基-2-甲基丙烷）6] +的合成方法中的用途。 配位络合物可用作放射性药物成像剂。