Biomodulators as universal imaging agents
AssigneeUniversity of New Mexico
InventorsJerry L. Born, Dennis Eshima, Paul L. Mann, Nicholas A. Matwiyoff
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Abstract
Biomodulators, optionally linked to imaging-active moieties, can be administered to a host to enhance images thereof, e.g., NMR-, X-ray- or radio-images, preferably by increasing aberrant tissue signal intensity. Biomodulators can also condition tissue to enhance uptake of otherwise non-specific imaging agents. When linked to drugs, biomodulators can target the same to particular sites in the body.
Claims12
A method of imaging tissue in a host, by a particular imaging modality, comprising administering to the host a biomodulator bonded to a moiety per se detectible by said modality, in an amount effective for imaging of said tissue, wherein said biomodulator is a compound selected from CAD;
- swainsonine or an indolizidine alkaloid having an electronically similar 1,3-diol structure;
- ##STR6## having a 3S,5R;
- 3R,5R;
- or 3S,5S stereoconfiguration;
- pokeweed mitogen;
- or a compound of formula (I) ##STR7## wherein R.sup.1 is ##STR8## wherein R.sup.10 is C.sub.1-6 -alkyl not containing an asymmetric carbon atom;
- each of R.sup.11 and R.sup.14 is, independently, H, C.sub.1-3 -alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 -alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, chloro, phenyl, phenoxy or benzyloxy;
- each of R.sup.12 and R.sup.15 is, independently, H, C.sub.1-3 -alkyl, C.sub.1-3 -alkoxy, trifluoromethyl, fluoro, chloro, chloro, phenyl, phenoxy or benzyloxy;
- each of R.sup.13 and R.sup.16 is, independently, H, C.sub.1-2 -alkyl, C.sub.1-2 -alkoxy, fluoro or chloro;
- with the provisos that
- not more than one of R.sup.11 and R.sup.12 is trifluoromethyl;
- not more than one of R.sup.11 and R.sup.12 is phenoxy;
- not more than one of R.sup.11 and R.sup.12 is benzyloxy;
- not more than one of R.sup.14 and R.sup.15 is trifluoromethyl;
- not more than one of R.sup.14 and R.sup.15 is phenoxy;
- not more than one of R.sup.14 and R.sup.15 is benzyloxy;
- R.sup.2 is --CH.sub.2 OH, --CHO, --COOR.sup.3, --COSR.sup.3, --CONR.sup.8 R.sup.9 or the corresponding lactone ##STR9## wherein R.sup.3 is H or C.sub.1-10 -alkyl,
- R.sup.4 and R.sup.5 are each independently H or C.sub.1-6 -alkyl,
- R.sup.6 and R.sup.7 are each independently OR, NHR or SR wherein R is H or C.sub.1-4 -alkanoyl,
- R.sup.8 and R.sup.9 are independently H or C.sub.1-10 -alkyl, and
- X is C.sub.2-3 -alkylene, C.sub.2-3 -alkenylene, C.sub.2-3 -alkynylene, a cyclopropylene group, --OCH.sub.2 -- or --SCH.sub.2 --,
- wherein said compound is effective as a biomodulator.
A method of enhancing the image of abnormal tissue obtainable by a particular imaging modality comprising administering a biomodulator and a non-tissue-specific imaging agent or a tissue-specific imaging agent for said modality, said biomodulator and said agent and the amounts thereof being effective for said enhancement of the image of said abnormal tissue, wherein said biomodulator is a compound selected from CAD;
- swainsonine or an indolizidine alkaloid having an electronically similar 1,3-diol structure;
- ##STR10## having a 3S,5R;
- 3R,5R;
- or 3S,5S stereoconfiguration;
- pokeweed mitogen;
- or a compound of formula (I) ##STR11## wherein R.sup.1 is ##STR12## wherein R.sup.10 is C.sub.1-6 -alkyl not containing an asymmetric carbon atom;
- each of R.sup.11 and R.sup.14 is, independently, H, C.sub.1-3 -alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 -alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, chloro, phenyl, phenoxy, or benzyloxy;
- each of R.sup.12 and R.sup.15 is, independently, H, C.sub.1-3 -alkyl, C.sub.1-3 -alkoxy, trifluoromethyl, fluoro, chloro, chloro, phenyl, phenoxy or benzyloxy;
- each of R.sup.13 and R.sup.16 is, independently, H, C.sub.1-2 -alkyl, C.sub.1-2 -alkoxy, fluoro or chloro;
- with the provisos that
- not more than one of R.sup.11 and R.sup.12 is trifluoromethyl;
- not more than one of R.sup.11 and R.sup.12 is phenoxy;
- not more than one of R.sup.11 and R.sup.12 is benzyloxy;
- not more than one of R.sup.14 and R.sup.15 is trifluoromethyl;
- not more than one of R.sup.14 and R.sup.15 is phenoxy;
- not more than one of R.sup.14 and R.sup.15 is benzyloxy;
- R.sup.2 is --CH.sub.2 OH, --CHO, --COOR.sup.3, --COSR.sup.3, --CONR.sup.8 R.sup.9 or the corresponding lactone ##STR13## wherein R.sup.3 is H or C.sub.1-10 -alkyl,
- R.sup.4 and R.sup.5 are each independently H or C.sub.1-6 -alkyl,
- R.sup.6 and R.sup.7 are each independently OR, NHR or SR wherein R is H or C.sub.1-4 -alkanoyl,
- R.sup.8 and R.sup.9 are each independently H or C.sub.1-10 -alkyl, and
- X is C.sub.2-3 -alkylene, C.sub.2-3 -alkenylene, C.sub.2-3 -alkynylene, a cyclopropylene group, --OCH.sub.2 -- or --SCH.sub.2 --,
- wherein said compound is effective as a biomodulator.
Dependencies are inferred from the claim text.