Abstract: A compound for the sequestration of undesirable antibodies (e.g. related to an autoimmune disease) in a patient. The compound includes an inert biopolymer scaffold and at least a first peptide n-mer of the general formula P(—S—P)(n?1) and a second peptide n-mer of the general formula P(—S—P)(n?1); wherein, independently for each occurrence, P is a peptide with a sequence length of 2-13 amino acids and S is a non-peptide spacer, wherein, independently for each of the peptide n-mers, n is an integer of at least 1, wherein each of the peptide n-mers is bound to the biopolymer scaffold. Also provided are pharmaceutical compositions including the compound, as well as a method of sequestering one or more antibodies present in an individual and a method of inhibiting an immune reaction to a treatment with an active agent.

Abstract: A method is described for production of a high purity compound of the formula (I) in crystalline form of the modification A. In this, starting from high purity gadobutrol, the gadolinium is removed by decomplexation with oxalic acid, and then with a calcium salt the calcium complex is produced in high purity. During the crystallization, a water equivalent of 9-11 weight % is set. The crystalline form of the modification A of the compound of the formula (I) is used in the production of Gadovist.

Abstract: It is disclosed a method for preparing calteridol used as MRI contrast agents. It provides a method for preparing calteridol comprising: obtaining teridol represented by the following Formula 2 by reacting gadoteridol represented by the following Formula 1 with decomplexing agent; and obtaining calteridol represented by the following Formula 3 by reacting calcium ion with teridol represented by following Formula 2.

Abstract: Disclosed is a method for producing calcobutrol used as an MRI contrast agent. The method comprises the steps of: obtaining butrol represented by chemical formula 2 in the specification by reacting a gadobutrol represented by chemical formula 1 in the specification and a decomplexing agent; and obtaining a calcobutrol represented by chemical Formula 3 in the specification by reacting butrol with calcium ions.

Abstract: Disclosed are: an intermediate capable of high-purity synthesis of gadobutrol which can be used as an MRI contrast agent; and a gadobutrol production method using same. The gadobutrol intermediate is represented by Chemical Formula 2 in the specification.

Abstract: The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.

Abstract: The present invention provides methods for the preparation of compounds useful in in vivo therapeutic and diagnostic applications. In particular, the present invention provides a method for the synthesis of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and also methods for the preparation of metal chelates of DOTA.

Abstract: A method is described for production of a high purity compound of the formula (I) in crystalline form of the modification A. In this, starting from high purity gadobutrol, the gadolinium is removed by decomplexation with oxalic acid, and then with a calcium salt the calcium complex is produced in high purity. During the crystallization, a water equivalent of 9-11 weight % is set. The crystalline form of the modification A of the compound of the formula (I) is used in the production of Gadovist.

Abstract: A Rapafucin library containing compounds of the general structure, (A) and (E), and a synthesis of these compounds are provided.

Abstract: A process for purifying a compound of formula 1, includes the following steps: a) adding an acid to an aqueous solution of the compound of formula 1, including salts and hydrates thereof so as to obtain a slurry having a pH?3; and b) filtering the slurry and at least one time washing the obtained precipitate with a liquid comprising water; and c) dissolving the precipitate obtained in step b) in water to obtain an aqueous solution; and d) filtering of the solution obtained in step c) over a nanofiltration membrane having a Molecular Weight Cut Off in the range from 150 to 500 and wherein optionally, between step c) and step d) the pH of the aqueous solution is adjusted to a pH value in the pH range as specified by the manufacturer of the nanofiltration membrane. A process for preparing a gadolinium complex of the purified compound of formula 1 is also disclosed. This gadolinium complex can be used for making a pharmaceutical composition as a contrast agent for magnetic resonance imaging.

Abstract: What is described is a process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7 or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration. The process is carried out using specifically controlled crystallization conditions. The more recent developments in the field of the gadolinium-containing MR contrast agents (EP 0448191 B1, CA Patent 1341176, EP 0643705 B1, EP 0986548 B1, EP 0596586 B1) include the MRT contrast agent gadobutrol (Gadovist® 1.0) which has been approved for a relatively long time in Europe and more recently also in the USA under the name Gadavist®.

Abstract: The invention relates to complexing agents of formula (I): in which A, chrom1, chrom2 and chrom3 are as defined in the description. The invention also relates to the lanthanide complexes obtained from these complexing agents.

Abstract: The present invention relates to an oxidatively curable coating formulation comprising an oxidatively curable alkyd-based resin and a bis-triazacyclononane-based chelant, which chelant may optionally be complexed with a suitable transition metal ion, particularly manganese. The formulations may be paints or other oxidatively curable coating compositions. The invention also provides methods for making such formulations and compositions resultant from the curing of such formulations.

Abstract: 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.

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: Biologically active compounds are provided that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, ophthalmological or urological disorders as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso-substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed.

Abstract: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N?,N?,N??-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.

Abstract: The present disclosure provides a novel class of macrocyclic compounds and their metal complexes formed with transition metal ion, lanthanide metal ions and other metal ions (e.g., Al, Ga, Y, In, Sn, Tl, Pb and Bi) and their applications in the fields of contrast agents, artificial nucleases, fluorescence probes, nuclear medicines and other biomedical applications in the therapeutics or diagnostics.

Abstract: A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R1 and R2 are independently selected from H and substituted or unsubstituted C1 to C4 alkyl; each R3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C1 to C20 alkyl, and a substituted or unsubstituted C1 to C20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse s

Abstract: Described are bifunctional NOTA-based derivatives capable of conjugating with alginate and with metal ions, as well as NOTA-alginate conjugates which can be labeled with stable or radioactive metal ions. Also described are conjugation methods of the bifunctional NOTA-based linker with alginate, and methods of using radiometal-labeled NOTA-alginate conjugates or other radio-labeled alginate conjugates as imaging reagents.

Abstract: 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.

Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.

Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.

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: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: Pharmaceutical compositions may include a complex of a radionuclide and a compound of Formula I or Formula II.

Abstract: The invention relates to compositions of DOTA derivative compounds, lanthanoid-DOTA derivative molecular complex, and lanthanoid-complex encapsulated solid lipid particles or capsules, and methods of making and using the compositions. The solid lipid particles or capsules contain micelle cores stabilized by a hyperbranched polymer shell based from a crosslinked DOTA derivative compound or crosslinked lanthanoid-DOTA derivative complex. These solid lipid particles or capsules can be used in various applications, such as contrast agents or drug delivery vehicles.

Abstract: The present invention relates to a material notably adapted for the extraction of metal cations in an aqueous medium, comprising a solid support on which are attached polyazacycloalkane compounds having a ring including at least 4 nitrogen atoms, and wherein the nitrogen atoms of the ring are substituted with coordinating groups, which each are independently: a coordinating group of formula: —(CH2)n—C(?O)—NR1R2 ?or else a both coordinating and binding group, fitting the formula: —(CH2)p—C(?O)—NR3-(A)-[support]. The invention also relates to methods for preparing the aforementioned materials and to different uses thereof, notably for the extraction of Pb2+ cations in an aqueous medium.

Abstract: A reagent for conjugation to a biomolecule, wherein the reagent is a single molecule with at least three functional parts and has schematic structure (I): a) wherein a trifunctional cross-linking moiety is coupled to b) an affinity ligand via a linker 1, said affinity ligand being capable of binding with another molecule having affinity for said ligand, to c) an effector agent, optionally via a linker 2, said effector agent exerting its effect on cells, tissues and/or humorous molecules in vivo or ex vivo, and to d) a biomolecule reactive moiety, optionally via a linker 3, said moiety being capable of forming a bond between the reagent and the biomolecule.

Abstract: In some aspects, the present invention provides novel ligands, which may be used to make novel dual-modality imaging agents, for example, for PET and MRI imaging. In further aspects, by the present disclosure also provides methods of use and methods of preparation of the novel ligands, metal complexes, and imaging agents thereof.

Abstract: The present invention provides improved processes for the synthesis of 1,4-ditosyl-1,4,7-triazacyclonone, comprising deprotecting a compound of formula (C): wherein P is tosylate or arylsulfonate, with an acidic medium to form 1,2-bis(1,4,7-triazacyclonon-1-yl)-ethane; and subsequently adding formaldehyde and formic acid to the acidic medium to form 1,2-bis-(4,7-dimethyl-1,4,7-triazacyclonon-1-yl)-ethane (Me4-DTNE). The syntheses of intermediates are also disclosed.

Abstract: The present invention relates to a magnetic resonance imaging (MRI) contrast agent including a gadolinium complex, more particularly to a DO3A-tranexamic acid or its ester compound, which is represented by the Chemical Formula 1. A DO3A-tranexamic acid or its ester compound may be prepared according to the present invention and a gadolinium complex may be prepared using the compound. An MRI contrast agent including the gadolinium complex prepared according to the present invention as an active ingredient has higher relaxivity as compared to the currently commercially available contrast agent. In addition, the MRI contrast agent according to the present invention has bifunctionality of liver-specific and blood-pool contrasting effect.

Abstract: Disclosed are a photosensitive resin composition for a color filter and a color filter using the same. The photosensitive resin composition for a color filter includes (A) a dye represented by the following Chemical Formula 1, (B) an alkali soluble resin, (C) a photopolymerizable monomer, (D) a photopolymerization initiator, and (E) a solvent.

Abstract: The present invention concerns complexing agents of formula (I) in which a, b, c, chrom1, chrom2, chrom3, R3, R4 and R5 are as defined in the description. The invention also concerns lanthanide complexes comprising said complexing agents, as well as a method for synthesizing said agents.

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 an improved process for the purification of polyaminocarboxylates such as DOTA, DTPA, DO3A-butrol, BOPTA.

Abstract: Special C-functionalized cyclic bisaminal compounds having formula (I) or (II), their salts or solvates, methods for their preparation, their uses, and methods for preparing functional tetraazacycloalkane compounds implementing such cyclic bisaminal compounds.

Abstract: A device is presented having reversibly changeable and optically readable optical properties. The device comprises a substrate having an electrically conductive surface and carrying a redox-active layer structure. The redox-active layer structure may be a monolayer or a multi-layer structure and is configured to have at least one predetermined electronic property including at least one of electrodensity and oxidation state. The electronic property of the layer structure defines an optical property of the structure thereby determining an optical response of the structure to certain incident light. This at least one electronic property is changeable by subjecting the redox-active layer structure to an electric field or to a redox-active material. The device thus enables effecting a change in said electronic property that results in a detectable change in the optical response of the layer structure.

Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.

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 invention relates to a method for functionalizing an electrically conductive substrate, which is not a substrate made of gold, via a layer of chemical compounds, said method comprising the following steps: a step in which the electrically conductive substrate is placed in contact with chemical compounds comprising at least a disulfide terminal group; a step in which the disulfide terminal group of said chemical compounds is electro-oxidized, causing said chemical compounds to form a layer at the surface of the electrically conductive substrate.

Abstract: A engineered composition and method of delivery of said composition providing effective therapy for the treatment of ulcerative colitis, and Crohn's disease.

Abstract: The present invention provides compound conjugates of matrix metalloprotease inhibitors and linked metal chelators which are useful for imaging solid tumors and treating and diagnosing certain types of diseases such as cancer.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA. Pharmaceutical compositions may include a complex of a radionuclide and a Formula I compound or a Formula II compound. Methods include using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

Abstract: Disclosed is a lubricant composition comprising at least one kind of compound represented by following formula (1): where X represents a cyclic group that may be substituted; Y represents a divalent or higher-valent linking group having at least one polar group and having no aromatic cyclic group; p1 represents an integer of 1 to 4; p2, p3, and p4 each represent an integer of 0 to 4; q represents an integer of 0 to 30; n represents an integer of 1 to 10; s represents an integer of 1 to 4; and t represents an integer of 2 to 10.

Abstract: The present invention generally relates to carriers including polymers and lipids that comprise a CXCR4 inhibiting moiety. More specifically, these carriers are biodegradable and can be bioreducible polymers that comprise a CXCR4 inhibiting moiety. These carriers can be suitable for delivery of nucleic acids to cells. These carriers and pharmaceutical compositions can be used to treat various conditions including cancers and inflammation conditions.

Abstract: Compounds as defined herein are provided which are useful in (1) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable diluent; and (3) methods for imaging prostate cancer cells.

Abstract: Amine chelates capable of antioxidant capacity and amyloid disaggregation are shown which may be useful in targeting metal-based oxidative stress in neurodegenerative disorders. Pyclen, a backbone commonly investigated for contrast agent imaging, may be repurposed as an anti-oxidant chelator for disaggregating amyloid. The antioxidant capacity of pyclen is enhanced dramatically via conversion of the pyridine backbone to a pyridol with cellular studies showing superior antioxidant capacity while retaining chelation ability to protect amyloid from metal ions aggregation and also disaggregate amyloid aggregates. Another family of molecules based upon hybrid heterocyclic amine ligands is also presented.

Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents —NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolid

Abstract: The present disclosure provides a novel class of macrocyclic compounds and their metal complexes formed with transition metal ion, lanthanide metal ions and other metal ions (e.g., Al, Ga, Y, In, Sn, Tl, Pb and Bi) and their applications in the fields of contrast agents, artificial nucleases, fluorescence probes, nuclear medicines and other biomedical applications in the therapeutics or diagnostics.

Abstract: The invention provides a compound of formula (I): (wherein: R1 is an optionally substituted 2-(1-azathiaxanthone); each —R2 is independently of the formula —CH2—C(?O)—R4, wherein R4 is an amino acid or a salt thereof, attached to the remainder of R2 through the nitrogen atom of the amino group; and R3 is hydrogen or a C1-6 alkyl group); or (wherein: R1 is an optionally substituted 2-(1-azaxanthone); each R2 is independently an optionally substituted glutaric or succinic acid, or a salt or ester thereof; and R3 is hydrogen or a C1-6 alkyl group).