The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents as optionally substituted C.sub.1-6 alkylene group.

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Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

Quinolinecarboxamide compounds of general formula I exceed the previously known FAP inhibitors in affinity and inhibitory effect. These agents can be used to specifically target tumours for diagnostic and therapeutic purposes, or for laboratory purposes in the study of endogenous FAP expression.

A tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand comprising four HOPO moieties and the ion of an alpha-emitting thorium radionuclide, where at least one of the four HOPO moieties is substituted at the N-position with a hydroxyalkyl solubilising group.

The present invention relates to a labeling procedure for the incorporation, in mild reaction conditions, of sensitive and thermosensitive targeting molecules into a [.sup.99mTc(N)(PNP)]-based compound suitable for a kit formulation.

The invention relates to novel multi-modality probes for imaging, tracking and analyzing stem cells and related biological samples, and methods of preparation and use thereof. The molecular probes of the invention are constructed, for example, by utilizing (a) the high selectivity of long hydrocarbon chains for binding to plasma membranes of cells, (b) a near-infrared (NIR) dye for optical imaging, and (c) a radionuclide for PET or SPECT imaging. The in vitro and in vivo data of the optical and radiolabeled probes demonstrated their utility for detecting the presence of stem cells with multiple imaging modalities.

This disclosure relates to compositions comprising substituted iminodiacetic acid ligands and metal tricarbonyl complexes containing the ligands and derivatives thereof. In certain embodiments, the metal tricarbonyl complexes are used as radioisotope tracers such as renal tracers. In certain embodiments, the metal complexes comprise .sup.99mTc or Re. In certain embodiments, the ligands are substituted with a fluorine, a fluorine-18(F.sup.18) radioisotope, or other radionuclide.

The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents an optionally substituted C.sub.1-6 alkylene group. ##STR00001##

The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.

The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x.sub.1-(B)-x.sub.2-(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x.sub.1 is a spacer covalently connecting (A) and (B); x.sub.2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula wherein R.sup.1 to R.sup.4, R.sup.9, a, b, Y and X.sup.1 to X.sup.4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition. ##STR00001##