公开(公告)号：EP1536843A2

公开(公告)日：2005-06-08

申请号：EP03731347.5

申请日：2003-05-22

Applicant: BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM

Inventor： BAO, Ande ,  PHILLIPS, William, T. ,  GOINS, Beth

IPC: A61K51/00 ,  C07F5/00

CPC classification number: A61K51/1234 ,  A61K9/127 ,  A61K51/0478 ,  C07F13/005

Abstract: The invention, in one aspect, relates to radiolabeled compounds. The invention also relates to radiolabeled liposomes and methods of making and using thereof. The invention also relates to kits for preparing radiolabeled liposomes.

公开(公告)号：EP1238978A3

公开(公告)日：2005-03-02

申请号：EP02006707.0

申请日：1999-10-21

Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

Inventor： Meltzer, Peter Claude ,  Blundell, Paul ,  Madras, Bertha Kalifon

IPC: C07D451/02 ,  A61K31/46

CPC classification number: A61K31/46 ,  A61B6/506 ,  A61K51/0448 ,  A61K51/0478 ,  A61K51/0497 ,  C07D451/02 ,  C07F13/005

Abstract: The compounds of the present invention comprise a tropane compound or ligand that selectively binds to tropane recognition sites, e.g., neuron transporters such as the DAT. The tropane ligand is radiolabeled with a radioactive technetium or rhenium by a chelating ligand which is attached to the tropane ligand by a linker. Tropane compounds or ligands useful in the pratice of the present invention can generally be represented by formula II where R 1 and R 2 are defined as above and where R 1 can also be substituted at the C 4 position of the tropane ring: Any tropane compound of the general formula II is useful in the present invention so long as it binds to DAT. Useful tropane analogs have a 3α-group, i.e., are of the boat configuration. Intermediates for the synthesis of the radiolabeled tropanes are claimed.

公开(公告)号：EP1458416A1

公开(公告)日：2004-09-22

申请号：EP02799930.9

申请日：2002-12-11

Applicant: DOW GLOBAL TECHNOLOGIES INC.

Inventor： SIMON, Dana, W. ,  STRICKLAND, Alan, D. ,  SIMON, Jaime ,  MACEY, Daniel, J. ,  FRANCK, Keith, R. ,  MCMILLAN, Kenneth

IPC: A61K51/06 ,  A61P19/00

CPC classification number: A61K51/0478 ,  A61K51/0489

Abstract: This invention relates to medical uses of radiopharmaceuticals. Specifically, the present invention relates to the use of radiopharmaceuticals to treat osteomyelitis. The present invention provides improved system and methods of for the direct delivery of radiopharmaceuticals to the site of osteomyelitis.

公开(公告)号：EP1374897A1

公开(公告)日：2004-01-02

申请号：EP03101773.4

申请日：2003-06-17

Applicant: HEALTH RESEARCH, INC.

Inventor： Pandey, Ravindra, K ,  Kanter, Peter ,  Grossmann, Zachary ,  Dougherty, Thomas, J

IPC: A61K41/00 ,  A61K49/10 ,  A61K51/04

CPC classification number: A61K51/0485 ,  A61K41/0071 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/10 ,  A61K51/0478 ,  C07D471/22 ,  C07D487/22

Abstract: A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferativc tissue. The preferred compounds have the structural formula :
where R 1 , R 2 , R 2a R 3 , R 3a R 4 , R 5 , R 5a R 6 , R 7 , R 7a , and R 8 cumulatively contain at least two functional groups that will complex or combine with an MR imaging enhancing element or ion. The compound is intended to include such complexes and combinations and includes the use of such compounds for MR imaging and photodynamic therapy treatment of tumors and other hyperproliferative tissue.

Abstract translation: 包括光动力四吡咯化合物与多个放射性核素元素原子的化学组合的化合物，使得该化合物可用于增强MR成像，并且还可用作光动力学化合物用于光动力学治疗以治疗过度增生组织。 优选的化合物具有结构式：其中R1，R2，R2a R3，R3a R4，R5，R5a R6，R7，R7a和R8累积含有至少两个将与MR成像增强复合或组合的官能团 元素或离子。 该化合物旨在包括这种复合物和组合，并且包括使用这些化合物用于肿瘤和其它过度增生组织的MR成像和光动力疗法治疗。

公开(公告)号：EP1175388A4

公开(公告)日：2003-06-18

申请号：EP99918906

申请日：1999-04-30

Applicant: UNIV PENNSYLVANIA

Inventor： KUNG HANK F

IPC: A61K51/00 ,  A61K51/04 ,  C07C215/28 ,  C07C215/30 ,  C07C215/50 ,  C07C215/68 ,  C07C217/58 ,  C07C225/16 ,  C07C323/32 ,  C07C323/37 ,  C07C211/27 ,  C07C211/29 ,  C07C321/30

CPC classification number: A61K51/0478 ,  A61K51/0406 ,  A61K51/0497 ,  C07B2200/05 ,  C07C215/30 ,  C07C215/68 ,  C07C217/58 ,  C07C225/16 ,  C07C323/32 ,  C07C323/37

公开(公告)号：EP1051980A3

公开(公告)日：2002-05-22

申请号：EP99121068.3

申请日：1999-10-21

Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  ORGANIX, INC. ,  THE GENERAL HOSPITAL CORPORATION

Inventor： Meltzer, Peter C. ,  Blundell, Paul ,  Madras, Bertha K. ,  Fischman, Alan J. ,  Jones, Alan G. ,  Mahmood, Ashfaq

IPC: A61K51/04

CPC classification number: A61K31/46 ,  A61B6/506 ,  A61K51/0448 ,  A61K51/0478 ,  A61K51/0497 ,  C07D451/02 ,  C07F13/005

Abstract: Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

公开(公告)号：EP0499098B1

公开(公告)日：2002-04-17

申请号：EP92101569.9

申请日：1992-01-30

Applicant: THE DOW CHEMICAL COMPANY

Inventor： Wilson, David A. ,  Frank, Keith R. ,  Garlich, Joseph R. ,  Simon, Jaime

IPC: A61K51/04

CPC classification number: A61K51/0478 ,  A61K2121/00 ,  A61K2123/00

公开(公告)号：EP1110963A3

公开(公告)日：2001-12-19

申请号：EP00128019.7

申请日：2000-12-20

Applicant: HEALTH RESEARCH, INC.

Inventor： Pandey, Ravindra K. ,  Grossman, Zachary ,  Kanter, Peter ,  Dougherty, Thomas J.

IPC: C07D487/22

CPC classification number: A61K51/0478 ,  A61K41/0071 ,  A61K49/085 ,  A61K51/0485 ,  C07D471/22 ,  C07D487/22

Abstract: Compositions that are chemical combination of porphyrins, chlorins, bacteriochlorins, and related tetra-pyrrolic compounds with radioactive elements such as Technetium 99 , Gadolinium, Indium 111 and radioactive iodine. When the element can form cations, the compound is usually a chelate with the porphyrin or chlorin structure. When the element forms anions, the compound is usually a direct chemical combination of the radioactive element into the porphyrin or chlorin structure. The invention further includes the method of using the compounds of the invention for diagnostic imaging of hyperproliferative tissue such as tumors and new blood vessel growth as is associated with the wet form of age related macular degeneration and methods of making the compounds. Compounds for MRI contrast imaging of the invention are usually Tc 99 , In 111 or Gd(III) complexes of compounds of the formula:

Abstract translation: 组合物是卟啉，二氢卟酚，细菌色素和与放射性元素如锝99，钆，铟111和放射性碘的相关四吡咯化合物的化学组合。 当元素可以形成阳离子时，化合物通常是具有卟啉或二氢卟酚结构的螯合物。 当元素形成阴离子时，化合物通常是放射性元素与卟啉或二氢卟酚结构的直接化学组合。 本发明还包括使用本发明化合物用于诊断超增殖组织例如肿瘤和新血管生长的方法，其与湿性形式的年龄相关性黄斑变性相关联，以及制备该化合物的方法。 本发明的MRI造影成像的化合物通常是下式化合物的Tc 99，In 111或Gd（III）络合物：

公开(公告)号：EP1154990A1

公开(公告)日：2001-11-21

申请号：EP00910246.8

申请日：2000-02-18

Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： RAYMOND, Kenneth, N. ,  PETOUD, Stephane ,  COHEN, Seth ,  XU, Jide

IPC: C07C235/60 ,  C07D487/08 ,  G01N33/533

CPC classification number: C12Q1/37 ,  A61K41/0057 ,  A61K49/0002 ,  A61K49/0019 ,  A61K49/103 ,  A61K49/106 ,  A61K49/122 ,  A61K49/124 ,  A61K51/0478 ,  A61K51/0482 ,  A61K51/06 ,  C07C235/60 ,  C07D487/08 ,  C07D487/18 ,  C07D487/22 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/182 ,  G01N33/582 ,  G01N2458/40 ,  Y10S436/80 ,  Y10S436/804

Abstract: The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

公开(公告)号：EP1110963A2

公开(公告)日：2001-06-27

申请号：EP00128019.7

申请日：2000-12-20

Applicant: HEALTH RESEARCH, INC.

Inventor： Pandey, Ravindra K. ,  Grossman, Zachary ,  Kanter, Peter ,  Dougherty, Thomas J.

IPC: C07D487/22

CPC classification number: A61K51/0478 ,  A61K41/0071 ,  A61K49/085 ,  A61K51/0485 ,  C07D471/22 ,  C07D487/22

Abstract: Compositions that are chemical combination of porphyrins, chlorins, bacteriochlorins, and related tetra-pyrrolic compounds with radioactive elements such as Technetium 99 , Gadolinium, Indium 111 and radioactive iodine. When the element can form cations, the compound is usually a chelate with the porphyrin or chlorin structure. When the element forms anions, the compound is usually a direct chemical combination of the radioactive element into the porphyrin or chlorin structure. The invention further includes the method of using the compounds of the invention for diagnostic imaging of hyperproliferative tissue such as tumors and new blood vessel growth as is associated with the wet form of age related macular degeneration and methods of making the compounds. Compounds for MRI contrast imaging of the invention are usually Tc 99 , In 111 or Gd(III) complexes of compounds of the formula: