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| We claim: 1. A compound represented by the formula ##STR12## and the pharmaceutically acceptable ... |
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| Optically active bicyclic imino-alpha-carboxylic esters |
| We claim: 1. A compound of the formulae Ia or Ib essentially free of its racemate, and salts of ... |
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99MTC(III) myocardial imaging agents and method of use
| Details |
Inventors: Woulfe, Steven R.; Deutsch, Edward A.; Dyszlewski, Mary M.; Neumann, William L.;
Assignee: Mallinckrodt Medical, Inc. (St. Louis, MO)
Primary Examiner: Maples; John S.
Assistant Examiner:
Attorney, Agent or Firm: Hey; David A.
A myocardial imaging agent for use in humans comprising a Tc(III) complex ligated in a planar position by a tetradentate ligand having incorporated therein four hard atoms and two furanone rings and in the axial positions by phosphines containing dioxanyl or ether moieties. The agent exhibits improved biodistribution, improved labeling and extremely rapid blood clearance following administration to a human. The agent has high myocardial uptake accompanied with exceptionally rapid hepatobilary clearance and extensive renal clearance to give sufficiently high heart/liver and heart/lung ratio that provide nearly ideal myocardial images in humans. |
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DETAILED DESCRIPTION OF THE INVENTION The technetium compounds of the present invention which have been found most useful as myocardial imaging agents in humans comprise hexadentate technetium complexes having an overall cationic charge.
More specifically the agents comprise technetium complexes in the 3+oxidation state coordinatively bonded to six atoms as shown in FormuIa 1.
##STR1## The R.
sub.
1 groups illustrated in Formula 1 may be the same or different selected from the group consisting of hydrogen, hydroxy, C.
sub.
1-C.
sub.
5 alkyl--such as for example methyl or ethyl whereby methyl is preferred to decrease lipophilicity, and C.
sub.
1 -C.
sub.
5 alkyl substituted by one or more members of the group consisting of hydroxy, ether--such as for example methoxymethyl or methoxyethyl whereby methoxymethyl is preferable to decrease lipophilicity, ester--such as for example methoxycarbonyl or phenoxycarbonyl whereby methoxycarbonyl is preferable to increase susceptibility to hydrolysis, amide--such as for example dimethylaminocarbonyl or aminocarbonyl, ketone--such as for example 2-propanoyl or 3-butanoyl, aldehyde--such as for example 1-propanoyl or 1-butanoyl and nitrile-- such as for example cyanomethyl or cyanopropyl; and n may equal 1 or 2.
The R.
sub.
2 groups illustrated in Formula 1 may be the same or different selected from the group consisting of hydrogen, hydroxy, C.
sub.
1 -C.
sub.
5 alkyl--such as for example methyl or ethyl whereby methyl is preferred to decrease lipophilicity, and C.
sub.
1 -C.
sub.
5 alkyl substituted by one or more members of the group consisting of hydroxy, ether--such as for example methoxymethyl or methoxyethyl whereby methoxymethyl is preferable to decrease lipophilicity, ester--such as for example methoxycarbonyl or phenoxycarbonyl whereby methoxycarbonyl is preferable to increase susceptibility to hydrolysis, amide--such as for example dimethylaminocarbonyl or aminocarbonyl, ketone--such as for example 2-propanoyl or 3-butanoyl, aldehyde--such as for example 1-propanoyl or 1-butanoyl and nitrile--such as for example cyanomethyl or cyanopropyl; and n may equal 1 or 2
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