Abstract: There is described a method for preparation of an imaging medium via transfer from a hyperpolarised singlet state that is not parahydrogen, said method comprising the steps of: (i) preparing a system containing: parahydrogen; a magnetisation transfer complex, with a molecular symmetry that allows the creation of a singlet state between spin pairs within it, said complex including a reversibly bound small molecule transference substrate; applying a magnetic field such that hyperpolarisation is transferred into the transfer complex, including the reversibly bound small molecule transference substrate; (ii) introducing a recipient complex capable of binding the small molecule transference substrate, said recipient complex including a recipient substrate, such that the recipient complex and recipient substrate, including the bound transference substrate, is hyperpolarised.

Abstract: A composition in the form of a water-in-oil emulsion comprising: from 20% to 40% (v/v) of aqueous phase, in the form of droplets, comprising an anti-cancer agent and a densifying agent chosen from the complexes of nonionic macrocyclic chelate with a paramagnetic metal, from 60% to 80% (v/v) of lipid phase comprising an iodized oil and at least one surfactant of formula (I) in a proportion, by weight of surfactant relative to the total volume of the composition, of 0.3% to 5%, formula (I) of said surfactant being the following: in which: s is 0 or 1, m is an integer from 2 to 30, R1 represents a group of formula (II) in which n is an integer from 4 to 10, o is an integer from 1 to 4, p is an integer from 3 to 7, q is an integer from 2 to 10, and r is 0 or 1, R2 represents a hydrogen atom or is identical to R1, and each R3 independently represents a hydrogen atom or is identical to R1.

Abstract: The present invention provides a method of administering a therapeutic agent directly to the brain parenchym through a compromised region of the blood-brain barrier in a subject having a brain disorder, that involves first disrupting the blood-brain barrier (BBB) at an isolated region by locally administering an effective amount of a hyperosmolar agent at said region using a catheter, followed by administering a therapeutically effective amount of a therapeutic agent. The step of disrupting the BBB is carried out with non-invasive MR (magnetic resonance) imaging with a contrast agent to visualize local parenchymal transcatheter perfusion at said isolated BBB region thereby indicating that the BBB region is compromised. The method of the invention allows for highly precise drug delivery to the brain through blood brain barrier disruption at specifically controlled regions.

Abstract: For the purpose of obtaining a spectrum suitable for acquiring information on a CEST effect, an MR apparatus comprises a Z-spectrum generating unit 91 for generating a Z-spectrum containing a CEST component representing a signal component affected by CEST and a baseline component representing a signal component unaffected by CEST based on data acquired by a plurality of sequences; a spectrum transforming unit 92 for transforming the Z-spectrum into a CPE spectrum; and first fitting unit 95 for calculating values of a plurality of coefficients included in a CEST term in an approximate expression of the CPE spectrum.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: The present invention relates to a new class of diazepine-derivatives as chelating agents for paramagnetic metal ions, the process for their preparation, and use of such paramagnetic complexes as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis. The present invention refers to a new class of derivatives of formula (I), or a pharmaceutically acceptable salt thereof.

Abstract: Described are amphiphilic polymers that are provided with chelating moieties. The amphiphilic polymers are block copolymers comprising a hydrophilic block and a hydrophobic block, with the chelating moieties linked to the end-group of the hydrophilic block. The disclosed polymers are capable of self-assembly into structures such as micelles and polymersomes. With suitable metals present in the form of coordination complexes with 5 the chelating moieties, the chelating amphiphilic polymers of the invention are suitable for use in various imaging techniques requiring metal labeling, such as MRI (T 1/T 2 weighted contrast agents or CEST contrast agents) SPECT, PET or Spectral CT.

Abstract: The present invention relates to copper, gallium and technetium coordinated thiosemicarbazone-pyridylhydrazine (substituted at the pyridine ring with a substituted benzothiazole or stilbene moiety) complexes and methods thereof. Such compounds possess utility in PET imaging and diagnosis of amyloid diseases.

Abstract: The present invention relates to a new class of diazepine-derivatives as chelating agents for paramagnetic metal ions, the process for their preparation, and use of such paramagnetic complexes as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

Abstract: RGD-chlorophyll and RGD-bacteriochlorophyll conjugates that home and accumulate in necrotic tumor domains much longer than in tumor non-necrotic domains are provided for use in minimally invasive tumor-targeted imaging, tumor-targeted photodynamic therapy, and/or on-line prognosis of necrotic tumors.

Abstract: The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.

Abstract: Compounds and uses of the compounds are provided. The compounds can be used as Fe(II) sequestering compounds. For example, these compounds can be used to sequester Fe(II) in cells, organs, vasculature, or tissues. Also, provided are compositions and methods of using the them for sequestering Fe(II) in an individual. The compounds can be used as MRI paraCEST contrast agents.

Abstract: The present invention provides compositions and methods for the delivery of nucleic acids to a cell. The present invention additionally provides compositions and methods for the treatment of a disease or disorder, particularly cancer.

Abstract: A dendritic polymer and a magnetic resonance imaging contrast agent employing the same. The magnetic resonance contrast agent includes the dendritic polymer according to the structure of SP-DZ-L)i)j or SP-DX-Z-L)i)j, wherein, S is cyclosilane moiety with j silicon oxygen residual groups, and j is not less than 2; P is CH2CH2Ol, and l is not less than 1; D is a C3-30 dendritic moiety having n oxygen residue, and n is not less than 3; X is C3-30 moiety having bi-functional groups; Z is a C3-20 moiety having a plurality of functional group; and L is a metal cation.

Abstract: A cell permeable probe is disclosed. The cell permeable probe includes a cell membrane translocating element, which facilitates transport of the probe into the intracellular component of a cell. The cell permeable probe may also include a plurality of binding moieties for a disease specific marker and a contrast agent.

Abstract: The present invention relates to a magnetic resonance imaging (MRI) method, in particular to a MRI method enabling early detection of myocardial ischemia.

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: An engineered lipoprotein including (a) a core particle or a plurality of core particles, each core particle has (i) an inner part comprising a hydrophilic active agent and a hydrophilic portion of an amphiphilic cholesterol and (ii) an outer part including a hydrophobic portion of the amphiphilic cholesterol, (b) a layer surrounding the core particle or a plurality of core particles, the layer includes a phospholipid, (c) an apoprotein associated with the layer, and optionally, (d) a homing molecule associated with at least one of the apoprotein or the phospholipid.

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: A dendritic polymer and a magnetic resonance imaging contrast agent employing the same. The magnetic resonance contrast agent includes the dendritic polymer according to the structure of SP-DZ-L)i)j or SP-DX-Z-L)i)j, wherein, S is cyclosilane moiety with j silicon oxygen residual groups, and j is not less than 2; P is and l is not less than 1; D is a C3-30 dendritic moiety having n oxygen residue, and n is not less than 3; X is C3-30 moiety having bi-functional groups; Z is a C3-20 moiety having a plurality of functional group; and L is a metal cation.

Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

Abstract: A metal complex of formula (III) wherein: M is a transition metal and A1, A2, X, X?, Y, L1?, R1? and R2? are as defined herein, is useful in medical imaging and therapy.

Abstract: The present invention relates to methods of detecting and monitoring aggregation of beta-amyloid peptides which are associated with neurodegenerative diseases as well as treating and/or preventing the neurodegenerative diseases by using carbazole-based fluorophores. In particular, the present invention provides methods for labeling and imaging the beta-amyloid (A?) peptides, oligomers, and fibrils in vitro and/or in vivo, as well as treating and/or preventing Alzheimer's disease by using the carbazole-based fluorophores of the present invention.

Abstract: The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3? and R3? is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention.

Abstract: The present invention provides compositions and methods based on vital fluorochrome conjugates that are useful for imaging dying and dead cells.

Abstract: The invention relates to a method of co-administering a peptide or protein drug with an enzyme-resistant PGA-complexone compound orally so to mitigate enzyme attack in the gastrointestinal tract of an animal subject.

Abstract: There is described a method of selective observation of non-hydrogenative para-hydrogen induced polarisation (NH-PHIP) as enhanced magnetic resonance signals which comprises separating the thermal and longitudinal spin order states. There is also described a template comprising [Ir(COD)(NHC)(Py)]+, and analogues thereof, for use in a PHIP magnetic resonance technique and a method for its preparation.

Abstract: The present invention relates to the use of a CEST contrast agent in a method of CEST imaging, wherein the contrast agent is a composition comprising an encapsulating system ES encapsulating at least one CEST agent, wherein the at least one CEST agent is constituted of a monomeric chelate of a chelate of q?2 type, or of a multimer of monomeric chelates of q?2 type, and wherein said chelate is free inside the encapsulating system.

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 is directed to a lanthamide chelate composition having a lanthamide, a charged amidate ligand, and a mono- or bidentate neutrally charged coordination compound, the composition being represented by structure I or structure II wherein Ln3+ designates lanthamide, R1 is alkyl, aryl, or heteroaryl; R2 is alkyl, aminoalkyl, aryl or heteroaryl; M is a neutrally charged monodentate coordination compound, M? is a neutrally charged bidentate coordination compound, a=1 or 2; and wherein M and M? comprise N, S, or O. It extends to the process of making the composition.

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 chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).

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: 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: Provided herein are chelating agents and metal chelates that are useful in diagnostic and therapeutic applications. The uses of metal chelates provided herein include their use as contrast agents in medical imaging modalities, such as magnetic resonance imaging (MRI).

Abstract: The present invention relates to novel compounds of formula (I) and (II), compositions comprising compounds of formula (II) and their use as contrast agents in magnetic resonance (MR) imaging (MRI) and MR spectroscopy (MRS).

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: A magnetic resonance imaging agent which includes: a polymer containing the structural unit represented by the following formula (I) and the structural unit represented by the following formula (II) in a molar ratio of 5 to 80:20 to 95; a paramagnetic metal compound; and a ligand molecule: wherein R1 represents hydrogen atom or methyl group; R2 represents a hydrogen atom or a methyl group; A represents —(CH2)2N+(CH3)3 or the like; and B represents oxygen atom, sulfur atom, —CH2—, or —NH—; and R4 represents hydrogen atom, an optionally substituted alkyl group, or an optionally substituted aryl group, which affords good retention in the blood and a good ability to accumulate in diseased areas.

Abstract: This invention provides a method for treating a mammalian subject afflicted with a disorder associated with reduced neurogenesis in the subject's hippocampal dentate gyrus which comprises administering to the subject a therapeutically effective amount of a compound which increases cerebral blood volume in the subject's hippocampal dentate gyrus by a percentage greater than that by which it increases the cerebral blood volume in the subject's hippocampal CA1 region, thereby treating the subject.

Abstract: The present invention relates to novel compounds of formula (I) and (II), compositions comprising compounds of formula (II) and their use as contrast agents in magnetic resonance (MR) imaging (MRI) and MR spectroscopy (MRS).

Abstract: The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount of free macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.

Abstract: The present invention relates to a magnetic resonance imaging (MRI) method, in particular to a MRI method enabling early detection of myocardial ischemia.

Abstract: The present invention relates to novel linear polymers, compositions comprising said polymers and their use as contrast agents in magnetic resonance (MR) imaging (MRI) and magnetic resonance spectroscopy (MRS).

Abstract: The invention relates to bifunctional conjugates comprising a receptor ligand moiety and a metal binding moiety and complexes thereof with paramagnetic lanthanide or transition metals, and to the use of the metal complexes as contrast agents in magnetic resonance imaging (MRI) of tumors and other abnormalities.

Abstract: Various biodegradable polyglutamate polymer conjugates that can include recurring units of the general formulae (I) and (II) are described herein. Such polymer conjugates are useful for variety of drug, targeting, stabilizing and/or imaging agent delivery applications.

Abstract: A contrast agent for magnetic resonance imaging comprising a complex of a paramagnetic cation, preferably Gd+3, Dy+3, and Fe+3 with three equivalents of a charge neutralizing chelator that provides a lipid soluble complex of the paramagnetic cation is described. The complex is retained intracellularly when introduced into a mammalian cell. A method of providing an image of an internal pathology of a patient by magnetic resonance imaging (MRI) by administering the MRI contrast agent or tagged cells to the patient and scanning the patient using magnetic resonance imaging to obtain visible images of the internal pathology of the patient is also set forth.

Abstract: The present invention generally relates to agents and compositions having MRI and/or optical signals, and methods for their use in the determination of an analyte. In some cases, an optical, MRI, or other signal produced by the agent or composition may be affected by the presence of an analyte. Some embodiments of the present invention may provide agents or compositions which are cell permeable. Examples of analytes that may be determined by the present invention include zinc ions, calcium ions, and other biological analytes.

Abstract: The invention relates to novel magnetic resonance imaging contrast agents and methods of detecting physiological signals or substances.