Chelant moieties linked to an aryl moiety by an interrupted alkylene linker

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United States of America Patent

PATENT NO 5798089
SERIAL NO

08727594

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention provides amphiphilic compounds of the formula (I) Ch--(--L--Ar--(--AH).sub.n).sub.m (where Ch is a hydrophilic chelant moiety or a salt or a chelate thereof); each L is an optionally oxo substituted C.sub.2-25 -alkylene linker wherein at least one CH.sub.2 moiety is replaced by a group X.sup.1 (e.g. L may include a chain sequence, an X.sup.1 (CH.sub.2 CH.sub.2 X.sup.1).sub.u (where u is a positive integer) such as X.sup.1 (CH.sub.2 CH.sub.2 X.sup.1).sub.u, CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1, CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1 CH.sub.2 CH.sub.2 X.sup.1, etc.), and wherein L is optionally interrupted by a metabolizable group M but with the provisos that the terminus of L adjacent Ch is CH.sub.2 and that the terminus of L adjacent Ar is X.sup.1 or a CH.sub.2 group adjacent or separated by one CH.sub.2 from a group X.sup.1 (thus, for example the L--Ar linkage may be L.sup.1 --X.sup.1 --Ar, L.sup.1 --CH.sub.2 --Ar, L.sup.1 --X.sup.1 CH.sub.2 --Ar or L.sup.1 --X.sup.1 CH.sub.2 CH.sub.2 --Ar, where L.sup.1 is the residue of L; each Ar is an aryl ring optionally substituted by or having fused thereto a further aryl ring; each AH is a protic acid group, preferably an oxyacid, e.g. a carbon, sulphur or phosphorus oxyacid or a salt thereof; each X.sup.1 is O, S, NR.sup.1 or PR.sup.1, preferably no more than 3 X.sup.1 groups being present in L; each R.sup.1 is hydrogen, alkyl or aryl; and m and n are positive integers, m being for example 1 to 4, especially 1 or 2 and n being for example, 1, 2 or 3) which are especially suited for use in diagnostic imaging of the hepatobiliary system.

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Patent Owner(s)

Patent OwnerAddress
AMERSHAM HEALTH SALUTAR INC101 CARNEGIE CENTER PRINCETON NJ 08540

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Berg, Arne Oslo, NO 73 1421
Varadarajan, John Wayne, PA 8 189
Watson, Alan David Wayne, PA 4 93

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