Contrast agents
View Patent ↗The invention provides a composition of matter of formula I V-L-R (I) where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body, with the provisos that where V is angiotensin or a peptidic angiotensin derivative or analog then V-L-R is other than a non-metal radionuclide substituted peptide (eg 125 I substituted angiotensin II) and L-V is other than simply a peptide with a chelating agent amide bonded to a side chain thereof. This composition of matter may be used to image cardiovascular diseases and disorders.
1. A composition of matter of formula I
V-L-R (I)
where V is a non-peptidic organic group having binding affinity for an angiotensin II receptor site, V being the residue of a compound of formula IV
where R 501 is an optionally fluorinated C 1-6 alkyl group,
R 504 is an optionally fluorinated C 1-6 alkyl group,
R 502 is a carboxy, hydroxy-C 1-6 alkyl or CHO group; or the double bond marked with an asterisk is replaced by a single bond and R 504 is an ═O or ═NR 505 group, R 502 is an optionally fluorinated C 1-6 alkyl group and R 503 is a carboxyphenyl group and R 505 is a C 1-6 alkyl group;
and R 30 is
and R 31 is COOH, tetrazol-5-yl, NH 2 SO 2 CF 3 , SO 2 NHCO-phenyl, SO 2 NHCO-cyclopropyl, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body.
2. A method of generating an image of an animate human or non-human animal subject involving administering a contrast agent to said subject and generating an image of at least a part of said subject to which said contrast agent has distributed, characterised in that as said contrast agent is used a composition of matter of formula I as defined in claim 1 .
3. A method as claimed in claim 2 wherein said image is a nuclear imaging image.
4. A method as claimed in claim 2 wherein said image is an ultrasound image.
5. A pharmaceutical composition comprising a composition of matter of formula I as defined in claim 1 together with at least one pharmaceutically effective carrier or excipient.