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 present invention relates to a contrast agent of Formula I V-L-Z Formula I where V is a non-peptidic vector having affinity for the Angiotensin II receptor, L is a bond, a spacer or a linker moiety and Z represents a moiety detectable in an in vivo imaging procedure of a human or animal body.

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 conjugates of hydroxypyridinone derivative metal complexes and to their preparation. The conjugates are suitable as contrast agents in NMR diagnosis. A high relaxivity is achieved and the NMRD maximum is raised through a specific design of the ligands.

Abstract: The present invention relates to improved diagnostic agents for Magnetic Resonance Imaging and optical imaging. In particular, this invention relates to MRI and optical imaging agents that allow for the sensitive detection of a specific bioactivity within a tissue. These agents are prodrug contrast agents which are bioactivated in vivo in the presence of the specific bioactivity. This invention also relates to pharmaceutical compositions comprising these agents and to methods of using the agents and compositions comprising the agents.

Abstract: The invention relates to pharmaceutical agents that contain at least one fluoroalkyl-containing metal complex that has a critical micelle-formation concentration of <10?3 mol/l and a hydrodynamic micelle diameter (2Rh) of >1 nm, and at least one natural or synthetic epothilone or epothilone derivative, optionally with the additives that are commonly used in galenicals.

Abstract: The invention concerns a ligand comprising wherein n is an integer from 1 to 5, X represents —NO2, —NH2, —NCS, —NHCOCH2-Z. NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or —NHCO(CH2)m ?-Q where Q is an hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, Y is CO2H or PO3H2 W is —(CH2)m— m is an integer from 1 to 10.

Abstract: Compositions and methods for dual imaging and for dual chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns compounds comprising the structure X1-Y-X2, wherein Y comprises two or more carbohydrate residues covalently attached to one another, X1 and X2 are diagnostic or therapeutic moieties covalently attached to Y, provided that when Y does not comprise a glucosamine residue, X1 and X2 are diagnostic moieties. The present invention also concerns methods of synthesis of these compounds, application of such compounds for dual imaging and treatment of hyperproliferative disease, and kits for preparing a radiolabeled therapeutic or diagnostic compound.

Abstract: A dendritic compound of the following structure: PDn-Z-L is disclosed. In the structure above, P is X—(CH2CH2—O)r—, r is an integer ranging from 1000 to 4000, X is OH, NH2, or OR, R is C1 to C10alkyl, Dn is a residue of branched C3 to C30 polyol compounds, n is the quantity of layers of the residue of branched compounds and is an integer equal to or greater than 1, L is a metal cation, Z is the residue of a C3 to C30 compound with multi functional groups. The functional groups illustrated above can be carboxylic groups, amino groups, amide groups, or chelating groups. The carboxylic groups, ester groups, amino groups, or amide groups bind to Dn, and the chelating groups bind to the metal cations.

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

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 concerns a ligand comprising (I) wherein n is an integer from 1 to 5 Y is CO2H or PO3H2T represents —X or -phenyl-X, wherein X represents NO2, NH2, NCS, NHCOCH2-Z, NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or NHCO(CH2)m-Q where Q is a hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, W is —(CH2)m- m is an integer from 1 to 10 Z is chloride, bromide or iodine

Abstract: The invention relates to a novel class of magnetic resonance imaging agents that can cross the blood brain barrier and provide accurate magnetic resonance imaging of the brain, especially magnetic resonance images of amyloid deposits associated with Alzheimer's disease.

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 present invention provides a class of biochemically-activated MRI contrast agents. The agents include a paramagnetic chelate attached via a linker arm to a relaxivity-modulating group. When the relaxivity-modulating group is removed or otherwise interacts with a targeted substance, the agents are activated by various mechanisms. The activation is detectable by an increase or decrease in the relaxivity of the metal chelate. The agents are useful in the detection of biochemical parameters in cells, tissues and subjects. Exemplary biochemical parameters are markers that are associated with disease states.

Abstract: The present invention relates to compounds that selectively bind to cells undergoing perturbations and alterations of their normal plasma membrane organization, such as cells undergoing apoptosis or activated platelets. The invention further provides methods for utilizing said compounds in medical practice, for diagnostic and therapeutic purposes.

Abstract: Amyloid-targeting imaging agents such as radiolabeled amyloid targeting molecules and amyloid targeting molecule-chelator conjugates for imaging, e.g., amyloid plaques in vivo, and/or for the treatment of amyloidosis disorders. The invention provides amyloid-targeting imaging agents that are useful for imaging sites of amyloid disease. Imaging agents of the invention are capable of binding specifically to amyloid plaques, as an aid in diagnosis and/or early treatment of amyloidosis disorders.

Abstract: The present invention relates to a contrast-enhanced diagnostic imaging method for monitoring the efficacy of interventional therapies. The contrast agents useful in this method comprise an image-enhancing moiety (IEM) and a state-dependent tissue binding moiety (SDTBM). These contrast agents exhibit state-dependent binding to one or more components of a targeted tissue or tissue component and provide a detectable change in the signal characteristics of the agent once bound to the targeted tissue. As a result, these agents exhibit a binding affinity for, and thus image contrast of, the targeted tissue which changes as the tissue-state changes during therapy.

Abstract: The present invention provides an inclusion compound having a cucurbituril derivative of the formula 1 as a host molecule and a metal complex of the formula 2 as a guest molecule. A pharmaceutical composition having an anticancer effect can be obtained by using the inclusion compound according to the present invention. The pharmaceutical composition can prevent effective components from being biologically degraded in vivo and can exhibit continuous drug effect for a long time just by a single dosage by controlling the release time of the platinum complex once it reaches target tumor cells.

Abstract: The invention relates to a novel class of ligands, complexes comprising such ligands and a metal ion, and adducts of these metal complexes and a macromolecule. Pharmaceutical compositions and methods of making and using the ligand-metal complexes are also described. The invention also relates to the use of macromolecular adducts for enhancement of diagnostic imaging. In particular, the invention relates to (ethylene)-(propylene)-triaminepentaacetic acid (EPTPA) derivatives, a process for their production, and their use for the production of pharmaceutical agents for NMR diagnosis or radiodiagnosis or radiotherapy.

Abstract: The present invention relates to improved chelator conjugates with biological targeting molecules, suitable for forming metal complexes with radiometals. The radiometal complexes, especially with the radiometal99mTc, are useful as radiopharmaceuticals.

Abstract: The invention relates to the use of perfluoroalkyl-containing metal complexes that have a critical micelle formation concentration <10−3 mol/l, a hydrodynamic micelle diameter (2 Rh)>1 nm and a proton relaxivity in plasma (R1)>10 l/mmol·s) as contrast media in MR imaging for visualization of plaque, lymph nodes, infarcted and necrotic tissue and for independent visualization of necrotic tissue and tumor tissue.

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: Compounds able to chelate paramagnetic metal ions and the use thereof as contrast agents in the technique known as “Magnetic Resonance Imaging” (M.R.I.).

Abstract: Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising

Abstract: The invention relates to the use of perfluoroalkyl-containing metal complexes that have a critical micelle formation concentration <10−3 mol/l, a hydrodynamic micelle diameter (2 Rh)>1 nm and a proton relaxivity in plasma (R)>10 l/mmol s as contrast media in MR imaging for visualization of intravascular thrombi.

Abstract: The present invention relates to improved diagnostic agents for Magnetic Resonance Imaging and optical imaging. In particular, this invention relates to MRI and optical imaging agents that allow for the sensitive detection of a specific bloactivity within a tissue. These agents are prodrug contrast agents which are bioactivated in vivo in the presence of the specific bioactivity. This invention also relates to pharmaceutical compositions comprising these agents and to methods of using the agents and compositions comprising the agents.

Abstract: Perfluoroalkyl-containing complexes with polar radicals of general formula I (K)1-G-(Z-Rf)m(R)p  (I) in which R means the polar radical, Rf means a perfluorinated carbon chain, K is a metal complex, and Z represents a linker group, are suitable for intravenous lymphography, for tumor diagnosis and for infarction and necrosis 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: The invention provides a composition of matter of the formula (I): V-L-R 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 (e.g. 125I 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.

Abstract: The present invention relates to contrast agents for diagnostic imaging. In particular, this invention relates to novel multimeric compounds which exhibit improved relaxivity properties upon binding to endogenous proteins or other physiologically relevant sites. The compounds consist of: a) two or more Image Enhancing Moieties (IEMs) (or signal-generating moiety) comprising multiple subunits; b) two or more Target Binding Moieties (TBMs), providing for in vivo localization and multimer rigidification; and c) a scaffold framework for attachment of the above moieties. d) optional linkers for attachment of the IEMs to scaffold. This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for contrast enhancement of diagnostic imaging.

Abstract: Perfluoroalkyl-containing complexes with sugar radicals of general formula I in which R represents a monosaccharide or oligosaccharide radical that is bonded via the 1-OH position or 1-SH position, Rf means a perfluorinated carbon chain, K is a metal complex, and Y and Z represent linker groups, are suitable for intravenous lymphography, for tumor diagnosis and for infarction and necrosis imaging.

Abstract: Compounds of general formula I 1

Abstract: The invention relates to (ethylene)-(propylene)-triaminepentaacetic acid derivatives that are substituted on both the ethylene bridge and the propylene bridge, as well as conjugates of these compounds with biomolecules. The compounds and conjugates are suitable as agents for NMR diagnosis and radiodiagnosis as well as for radiotherapy.

Abstract: A method for the assessment of pulmonary ventilation and lung perfusion through Magnetic Resonance Imaging (MRI), comprising the steps of: positioning a human subject in an MRI apparatus, delivering a hyperpolarized noble gas to the subject by inhalation, followed by a breath-hold period, during which a bolus of a contrast agent for MRI is injected intravenously, acquiring, during the breath-hold period, at least one MR image of the lungs prior to the bolus intravenous injection and at least one MR image thereafter.

Abstract: This invention relates to the use of particular contrast agents to prepare diagostic compounds suitable for non-invasive visualisation under physiological conditions of the intestinal tract, and the colon in particular.

Abstract: Compounds of formula I wherein Z1, Z2, X, R2 and R3 are as defined herein, are suitable as susceptibility reagents for use in susceptibility imaging.

Abstract: Emulsions comprising nanoparticles formed from high boiling perfluorochemical substances, said particles coated with a lipid/surfactant coating are made target-specific by directly coupling said nanoparticles to a targeting ligand. The nanoparticles may further include biologically active agents, radionuclides, and/or other imaging agents.

Abstract: The invention provides bifunctional detection agents comprising optical dyes covalently linked to at least one magnetic resonance image (MRI) contrast agent. These agents may include a linker, which may be either a coupling moiety or a polymer.

Abstract: The invention relates to injectable compositions for increasing the image contrast between specific organ areas in the magnetic resonance imaging (MRI) of human and animal patients. This enables better differentiation of neighboring tissue portions. Methods of the preparation of such compositions and their use in the MRI of living subjects are also disclosed.

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: This invention relates to a set of aqueous marker compositions, each composition having a selected 1/Ti value which is substantially invariant over an at least 10° C. temperature range between 15 and 40° C. and preferably over an at least ±2% magnetic field strength range about a selected field strength value between 0.01 and 5T and comprising an aqueous matrix material having a non-zero 1/Ti temperature dependence within said temperature range with distributed therein a first paramagnetic material having a Ti relaxivity which is substantially invariant within said range(s) and/or a second paramagnetic material having within said ranges(s) and T1 relaxivity which has a non-zero temperature dependence of opposite polarity to the temperature dependence of 1/Ti of said matrix material, said set containing a plurality of said compositions with different selected 1/Ti values preferably encompassing at least the range 1.0 to 2.

Abstract: Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI)

Abstract: The invention relates to a novel class of magnetic resonance imaging agents that can cross the blood brain barrier and provide accurate magnetic resonance imaging of the brain, especially magnetic resonance images of amyloid deposits associated with Alzheimer's disease.

Abstract: Compounds of formula (I): are used as their paramagnetic chelates as contrast agents in magnetic resonance imaging. These compounds have high affinity to plasma proteins and exhibit extremely high values of relaxivity in serum and are thus useful as blood pool contrast agents.

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: A compound for use as a therapeutic or diagnostic radiopharmaceutical includes a group capable of complexing a medically useful metal attached to a moiety which is capable of binding to a gastrin releasing peptide receptor. A method for treating a subject having a neoplastic disease includes administering to the subject an effective amount of a radiopharmaceutical having a metal chelated with a chelating group attached to a-moiety capable of binding to a gastrin releasing peptide receptor expressed on tumor cells with subsequent internalization inside of the cell. A method of forming a therapeutic or diagnostic compound includes reacting a metal synthon with a chelating group covalently linked with a moiety capable of binding a gastrin releasing peptide receptor.

Abstract: The invention relates to the use of intravenous contrast agents for projection mammography and novel devices for carrying out projection mammography. The invention therefore relates to the use of intravenous contrast agents for producing a diagnostic medium for projection mammography. With the additional intravenous administration of contrast agent, projection mammography attains a sensitivity comparable to the most modern methods, such as magnetic resonance tomography (MRT) while having a wider range of applications and avoiding the cost of MRT. This novel method is simple and can be carried out without special inconvenience for the patients. It a) considerably improves sensitivity for demonstrating focal lesions in the mammae and b) provides additional information on the character of previously detected lesions.

Abstract: Compounds of formula (I) both in the racemic and optically active forms, are used in MRI diagnostic imaging.