Abstract: Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein L1 and L2 are each independently a covalent bond or a divalent linking group, R is a detectable label or therapeutic drug and B is an albumin binding moiety. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells using a compound of Formula (I).

Abstract: The present invention is directed towards new chemical entities based on a lipid-paramagnetic metal ion chelate. The lipid portion of the compound intercalates into the membrane of a liposome. The compounds of the invention find particular use as paramagnetic contrast media for magnetic resonance imaging. It has been surprisingly discovered that the liposomal contrast media do not substantially cross the placental barrier into the vasculature of the fetus(es) when administered to a pregnant subject. These novel compounds are useful in the diagnosis of disorders and diseases in both gravid and non-gravid subjects. The invention is also directed towards pharmaceutical compositions comprising these compounds and the uses of these compounds.

Abstract: In an embodiment, a composition including a chiral solvating agent to resolve nuclear magnetic resonance signals of an enantiomer of at least one analyte, where the chiral solvating agent facilitates in the at least one analyte binding to a C2 face or a C3 face of the chiral solvating agent, and where the chiral solvating agent causes an upfield shift or a downfield shift in at least one nuclear magnetic resonance signals corresponding to a 1H, 19F{1H}, or 31P{1H} signal, and where the chiral solvating agent includes a cobalt cation. In another embodiment, a method that includes mixing a chiral solvating agent, including a cobalt cation, with at least one analyte to form a solution, obtaining nuclear magnetic resonance spectra of the solution, and identifying an enantiomer of the at least one analyte. In some embodiments, the method further includes determining enantiomeric purities of the at least one analyte.

Abstract: A kit for calibrating a magnetic resonance imaging (MRI) system using defined concentration of 19F isotopes as well as a device for calibrating a MRI system using the kit. Further, a method for calibrating a MRI system employing the kit as well as to an entity comprising a defined concentration of 19F isotopes to be used in the calibration of a MRI system.

Abstract: A crosslinker composition including a spread crosslinker for treating a subterranean formation is provided along with methods of sealing a subterranean formation including introducing a crosslinkable fluid, the crosslinkable fluid containing a spread crosslinker and a crosslinkable component, into a subterranean formation.

Abstract: A crosslinker composition including a spread crosslinker for treating a subterranean formation is provided along with methods of sealing a subterranean formation including introducing a crosslinkable fluid, the crosslinkable fluid containing a spread crosslinker and a crosslinkable component, into a subterranean formation.

Abstract: A crosslinker composition including a spread crosslinker for treating a subterranean formation is provided along with methods of sealing a subterranean formation including introducing a crosslinkable fluid, the crosslinkable fluid containing a spread crosslinker and a crosslinkable component, into a subterranean formation.

Abstract: The present invention provides a polymer-metal complex composite, which comprises a block copolymer capable of serving as a constituent member of a polymeric micelle and a metal complex having MRI contrast ability, accumulates in a tumor-specific manner, achieves high image contrast even in a small amount, and has reduced side effects and a long retention time in blood. The polymer-metal complex composite of the present invention comprises a block copolymer (A) represented by general formula (a) and a metal complex (B) having MRI contrast ability, wherein the composite comprises a structure in which a carboxyl anion of poly(carbo) in the copolymer (A) is attached to the metal complex (B) via a metal atom (M).

Abstract: Intravascular contrast agents are provided by Gd-chelates modified so as to comprise an amino acid unit attached to the chelate via a linker group suitably selected from C2-4alkylene and C3-5alkynylene. The chelates may be used as an intravascular contrast agent for MRI. Certain embodiments demonstrate enhanced relaxivity and good levels of signal enhancement.

Abstract: The present invention is directed single diasteromers of 4-fluoroglutamine having a diastereomeric excess of at least 80%. Methods of preparing the single diastereomers are also described, as well as methods of using the single diastereomers of radiolabeled 4-fluoroglutamine as imaging agent is also described.

Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.

Abstract: Described herein is a contrast agent for administration to a subject. The contrast agent includes a targeting portion that includes an unchelated aminocarboxylate functional group; a metal ion bound to a metal-complexable portion; and a linker joining the targeting portion and the metal-complexable portion of the contrast agent. The portion that is not bound to a metal ion is for binding to necrotic tissue in the subject.

Abstract: Novel gadolinium complex compounds responsive to ions and compounds other than zinc ion, as well as MRI probes made of the compounds are disclosed. Since the gadolinium complex compounds of the present invention such as that represented by the following structural formula exhibit responsiveness to potassium ion, calcium ion, glucose or the like, by using the gadolinium complex compounds of the present invention as a MRI probe, the ion or compound in a living body can be detected and concentration distribution thereof may be determined.

Abstract: The invention relates to dendritic chelated compounds, to methods for producing the same and to pharmaceutical compositions containing the same. The dendritic chelated complexes of the present invention have the following formula (I): [[MC]En-[D]m-X1p1X2p2X3p3X4p4]z?zB+ (I), where m is a magnetic or scintigraphic marker, C is a chelating agent of the marker M, E is a spacer, n=0 or 1, D is compound capable of forming a dendritic structure, m is an integer equal to 1 or 2 or 4, X1 is a group increasing the complex lipophily, p1 is an integer from 0 to 12, X2 is a group increasing the complex specificity for a particular organ, p2 is an integer equal to 1 or 2 or 4, X3 is a group having a therapeutic activity, p3 is an integer equal to 0, 1, 2 or 4, X4 is a CH3 group, p4 is an integer from 0 to 12, B is a counter-ion, z is an integer equal to 0, 1, 2, 3 or 4. The invention can be used in the field of pharmacy, more precisely in medical imaging.

Abstract: The present invention relates to contrast agents for diagnostic imaging with prolonged blood retention. In particular, this invention relates to novel compounds that are characterized by an image enhancing moiety (IEM); a protein plasma binding moiety (PPBM); and a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging.

Abstract: Cyclen-based chelates can be used as contrast agents for multi-modal imaging of tissue cells. The cyclen-based chelates are preferably polyazamacrocyclic molecules formed from 1,4,7,10 tetraazacyclododecane (“cyclen”) having varying chelating ions, phosphoester chains, and light harvesting moieties. By changing the chelating ion, phosphoester chain length and/or the light harvesting moiety different imaging techniques, such as MRI, CT, fluorescence and absorption, x-ray and NIR, may be employed to image the tissue cells. Additionally, the cyclen-based chelates may be conjugated to provide for site-specific delivery of the cyclen-based chelate to the desired tissue cells. The cyclen-based chelates may also be delivered to the tissue cells by attaching the cyclen-based to a polymeric delivery vehicle. Although these cyclen-based chelates have a wide variety of application, the preferred use is for imaging of cancer cells, such as brain cancer, for improving resection of a cancerous tissue.

Abstract: Various biodegradable polyglutamate-amino acids comprising recurring units of the general formulae (I) and (II) are prepared. Such polymers are useful for variety of drug, targeting, stabilizing and/or imaging agent delivery applications.

Abstract: Novel gadolinium complex compounds responsive to ions and compounds other than zinc ion, as well as MRI probes made of the compounds are disclosed. Since the gadolinium complex compounds of the present invention such as that represented by the following structural formula exhibit responsiveness to potassium ion, calcium ion, glucose or the like, by using the gadolinium complex compounds of the present invention as a MRI probe, the ion or compound in a living body can be detected and concentration distribution thereof may be determined.

Abstract: The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.

Abstract: The present invention relates to contrast agents for diagnostic imaging with prolonged blood retention. In particular, this invention relates to novel compounds that are characterized by an image enhancing moiety (IEM); a protein plasma binding moiety (PPBM); and a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging.

Abstract: MRI contrast agents that employ paramagnetic agents and chemical exchange saturation transfer (paraCEST) and which are coupled to targeted particulate delivery vehicles provide sufficient concentration of the paraCEST contrast agents to obtain useful images of target tissues or organs. In addition, the image contrast may be switched on or off with a presaturation radio frequency pulse, avoiding the necessity obtaining pre-injection and post-injection images.

Abstract: The present invention relates to a novel class of paramagnetic ion-based contrast i agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic i profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.

Abstract: Novel gadolinium complex compounds responsive to ions and compounds other than zinc ion, as well as MRI probes made of the compounds are disclosed. Since the gadolinium complex compounds of the present invention such as that represented by the following structural formula exhibit responsiveness to potassium ion, calcium ion, glucose or the like, by using the gadolinium complex compounds of the present invention as a MRI probe, the ion or compound in a living body can be detected and concentration distribution thereof may be determined.

Abstract: A method for mapping a physico-chemical parameter using a chemical exchange saturation transfer contrast agent in Magnetic Resonance Imaging is used with agents having only one exchangeable entity pool, e.g. proton pool, by applying two different RF frequencies for pre-saturation of the contrast agent.

Abstract: Novel tetrapyrollic water soluble photosensitizing and imaging compounds and the methods of treating and imaging hyperproliferative tissue, e.g. tumors and hypervacularized tissue such as found in macular degeneration. Broadly, the compounds are tetrapyrollic photosensitizer compounds where the tetrapyrollic compound is a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide having 3 to 6 —CH2CONHphenylCH2CH(N(CH2COOH)2))(CH2N(CH2COOH)(CH2CH2N(CH2COOH)2)) groups or esters thereof or complexes thereof with gadolinium(III).

Abstract: The present invention relates generally to branched macromolecules and their use as imaging or contrast agents. In particular, the invention relates to dendrimers, derived from lysine or lysine analogues, bearing a plurality of functional moieties and their application to imaging techniques in which a disease state may be imaged with a targeted contrast agent.

Abstract: Polymeric chelating agents and metal chelates, particularly those of lanthanide metals and more specifically those of Gd(III), useful as contrast agents in magnetic resonance imaging (MRI) for therapeutic and diagnostic applications as well as clinical and biomedical research applications. The polymeric chelates are generated using ring-opening metathesis polymerization (ROMP). Polymers can have multiple sites for functionalization allowing for the synthesis of multimodal and targeted contrast agents. Hydroxypyridonate (HOPO)-based chelating moieties are integrated into a ROMP-derived polymer. More specifically, the HOPO-based chelating moiety is integrated into a benzonorbornadiene unit that constitutes the backbone of the polymer. The ROMP-derived polymer chelators can comprise multiple metal ions, particularly Gd(III) ions, in polymers of varying lengths to provide a series of agents with controlled relaxivites. Polymer chelates include those that are water-soluble.

Abstract: The invention relates to portable albumin binders, which are useful for improving the pharmacokinetic properties of diagnostic or therapeutic agents, in particular increasing the blood circulations time and/or the tissue penetration capacity of such agents.

Abstract: Compounds useful for associating with nanoparticle or microparticle emulsions to obtain magnetic resonance images permit control of the relaxivity of the signal and readily associate with the particulate components.

Abstract: The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

Abstract: The invention relates to a method for the Magnetic Resonance Imaging and Magnetic Resonance Spectroscopy Imaging of a substrate molecule different from water wherein the NMR signal is enhanced by a reversible binding of the substrate molecule to a paramagnetic chelate complex, as well as to the use of a paramagnetic chelate complex in said method and the pharmaceutical composition for use therein.

Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.

Abstract: The invention relates to the use of a water-soluble paramagnetic substance, in particular a magnetic resonance contrast medium, to reduce the magnetic resonance relaxation time of a coolant for magnetic resonance systems. Furthermore the invention relates to a corresponding method for reducing the magnetic resonance relaxation time of a coolant.

Abstract: A method is claimed based on CEST procedure for the in vivo or in vitro determination of physical or chemical parameters which includes the use of a responsive paramagnetic CEST contrast agent.

Abstract: The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.

Abstract: A compound represented by the following general formula (I), or a salt thereof: wherein R1 and R2 independently represent a substituted or unsubstituted alkyl or alkenyl group having 8 to 30 carbon atoms; L represents a divalent bridging group (L is constituted by atoms selected from the group consisting of carbon atom, oxygen atom, nitrogen atom and hydrogen atom, wherein the total number of atoms constituting L and selected from the group consisting of carbon atom, oxygen atom and nitrogen atom is 4 to 15); and Ch represents a chelate forming moiety containing 3 or more nitrogen atoms. A compound suitable for a liposome contrast medium for performing lesion-selective imaging is provided.

Abstract: This invention concerns novel neutral labeling reactants. The novel reactants are derivatives of diethylenetriaminepentaacetic acid (DTPA) diamides, wherein a suitable group is linked to the molecule allowing introduction of the chelating agent or the neutral chelate to bioactive molecules.

Abstract: The present invention relates to contrast agents for diagnostic imaging with prolonged blood retention. In particular, this invention relates to novel compounds that are characterized by an image enhancing moiety (IEM); a protein plasma binding moiety (PPBM); and a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging.

Abstract: The invention relates to new, monomeric, perfluoroalkyl-substituted metal complexes, processes for their production, and their use in diagnosis and therapy. The compounds according to the invention are suitable especially as in vivo contrast media in nuclear spin tomography (MRT). They can preferably be used as blood-pool agents and as lymphographic agents.

Abstract: Described are new cascade polymer complexes, compositions containing them and use of the complexes in diagnosis and therapy, particularly for magnetic resonance imaging and computer tomography imaging.

Abstract: Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21–29, 39, 42, 44 or 57–83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.

Abstract: The present invention relates to contrast agents for diagnostic imaging with prolonged blood retention. In particular, this invention relates to novel compounds that are characterized by an image enhancing moiety (IEM); a protein plasma binding moiety (PPBM); and a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging.

Abstract: The invention relates to the subjects that are characterized in the claims, namely perfluoroalkyl-containing metal complexes with an N-alkyl group of general formula 1, process for their production and their use in NMR and x-ray diagnosis, radiodiagnosis, and radiotherapy, as well as in MRT lymphography.

Abstract: The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

Abstract: Compounds of formula I wherein Z1, Z2, X, R2 and R3 are as defined herein, are suitable as NMR shift reagents.

Abstract: The invention provides MRI detectable species of formula (I): Dp-Sn-Nm, wherein D is a MRI detectable moiety; S is a spacer; N is a molecule of a nutrient or pseudo-nutrient; n is 0 or an integer, m is an integer and p is an integer. These compounds are useful for internalising into tumor cells an amount of the MRI detectable moiety that is distinguishably higher than the amount internalised in normal healthy cells thus allowing the diagnosis of tumors. The internalisation of the MRI detectable moiety involves the nutrients or pseudo-nutrients transporting system. Preferred compounds of formula (I) are those wherein D is the chelated complex of a paramagnetic metal ion.

Abstract: The invention relates to new, monomeric, perfluoroalkyl-substituted metal complexes, processes for their production, and their use in diagnosis and therapy. The compounds according to the invention are suitable especially as in vivo contrast media in nuclear spin tomography (MRT). They can preferably be used as blood-pool agents and as lymphographic agents.

Abstract: The invention relates to new, monomeric, perfluoroalkyl-substituted metal complexes, processes for their production, and their use in diagnosis and therapy. The compounds according to the invention are suitable especially as in vivo contrast media in nuclear spin tomography (MRT). They can preferably be used as blood-pool agents and as lymphographic agents.

Abstract: A molecule for labeling a target material is provided including two transition-metal chelates and a detectable group. The molecule has the general structural formula (I): wherein: (a) Y and Y? are each a transition metal, (b) R1 and R1? are each independently CH(COO?), CH(COOH), or absent; (c) R2 and R2? are linkers each having a length of from about 3.0 to about 20 ?; and (d) X is a detectable group. The linkers may be linear or branched, may contain aromatic moieties, and may optionally be further substituted. Methods of using the molecules of the invention as probes in detecting and analyzing target materials as well as kits including the molecule of the invention are also provided.

Abstract: Chelants and macrocyclic metal complexes thereof, methods of preparing the chelants and macrocyclic metal complexes, and radiopharmaceutical compositions comprising the macrocyclic metal complexes are disclosed. Methods of using the macrocyclic metal complexes as radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious diseases and cancer are also disclosed. Chelants as bifunctional chelators (BFCs) for the radiolabeling of target-specific biomolecules, such as proteins, peptides, peptidomimetics, non-peptide receptor ligands, enzyme inhibitors, and enzyme substrates are disclosed. Methods of using macrocyclic metal complexes containing the chelant-biomolecule conjugates as target-specific diagnostic radiopharmaceuticals that selectively localize at sites of disease and allow an image to be obtained of the loci using gamma scintigraphy are disclosed.