Title:
DIAGNOSTIC IMAGING CONTRAST AGENTS WITH EXTENDED BDIAGNOSTIC IMAGING CONTRAST AGENTS WITH EXTENDED BLOOD RETENTION LOOD RETENTION
Document Type and Number:
WIPO Patent Application WO1996023526
Kind Code:
A3
Abstract:
The present invention provides diagnostic imaging contrast agents which exhibit improved blood retention. The novel compounds comprise: a) an image-enhancing (or signal-generating) moiety (IEM); b) a plasma protein binding moiety (PPBM); and c) a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging. These contrast agents exhibit reduced rates of both renal and hepatocellular uptake and no apparent uptake by the RE system. The agents may be targeted to the blood pool or any other biological component. Since the agent is lost less rapidly from the bloodstream, lower doses can be used at a higher margin of safety. The approach is general to both large and small molecules.
Inventors:
MCMURRY THOMAS J (US)
SAJIKI HIRONAO (US)
SCOTT DANIEL M (US)
LAUFFER RANDALL B (US)
SAJIKI HIRONAO (US)
SCOTT DANIEL M (US)
LAUFFER RANDALL B (US)
Application Number:
PCT/US1996/000164
Publication Date:
October 17, 1996
Filing Date:
January 16, 1996
Export Citation:
Assignee:
METASYN INC (US)
MCMURRY THOMAS J (US)
SAJIKI HIRONAO (US)
SCOTT DANIEL M (US)
LAUFFER RANDALL B (US)
MCMURRY THOMAS J (US)
SAJIKI HIRONAO (US)
SCOTT DANIEL M (US)
LAUFFER RANDALL B (US)
International Classes:
A61B5/055; A61B6/00; A61B8/00; A61K49/00; A61K49/04; A61K49/08; A61K49/18; A61K51/00; C07F9/09; G01R33/28; (IPC1-7): A61K49/00; A61K49/04; A61K51/04
Domestic Patent References:
| WO1991003200A1 | 1991-03-21 | |||
| WO1991018630A1 | 1991-12-12 |
Foreign References:
| US5385719A | 1995-01-31 | |||
| EP0661279A1 | 1995-07-05 | |||
| EP0535668A1 | 1993-04-07 |
Other References:
M. ROWLAND & T.N. TOZER: "Clinical Pharmacokinetics: Concepts and Applications", 1980, LEA & FEBIGER, PHILADELPHIA, US, XP002011088
DE SMIDT PC ET AL: "Association of antisense oligonucleotides with lipoproteins prolongs the plasma half-life and modifies the tissue distribution.", NUCLEIC ACIDS RES, 11-9-1991, VOL. 19, NO. 17, PAGE(S) 4695-700, XP002011087
DE SMIDT PC ET AL: "Association of antisense oligonucleotides with lipoproteins prolongs the plasma half-life and modifies the tissue distribution.", NUCLEIC ACIDS RES, 11-9-1991, VOL. 19, NO. 17, PAGE(S) 4695-700, XP002011087
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