Abstract: The present invention relates to a novel process for preparing iopromide which is used as a contrast agent for X-ray, wherein 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid (2,3-diacetoxypropyl)amide chloride of formula (19) and 5-methoxyacetylamino-2,4,6-triiodoisophthalic acid [(2,3-dihydroxy-N-methylpropyl)-(2,3-diacetoxypropyl)]diamide of formula (20) are introduced as intermediates, by which a bismer by-product generated during the preparation process can be removed even without an additional removal procedure and thus iopromide with high purity can be prepared in high yield.

Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.

Abstract: The invention relates to a process for the preparation of triamides from ammonia and amido-dichlorides.

Abstract: This invention relates generally to industrial preparation of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), a non-ionic X-ray contrasting agent. It further relates to a method of recovering intermediate 5-acetamido-N,N-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”) from the desalinated and desolventized dimerisation reaction mixture. In particular, the present invention employs ultrafiltration to recover non-crystalline Compound A to reduce the overall cost of iodixanol manufacture, increase the yield of iodixanol, and facilitate the subsequent purification procedures to meet the regulatory purity requirement of iodixanol.

Abstract: This invention relates to an improved method for the synthesis of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, it relates to a continuous process of acetylation of 5-amino-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide (“Compound B”) followed by the removal of acetic anhydride.

Abstract: This invention relates generally to industrial preparation of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), a non-ionic X-ray contrasting agent. It further relates to a method for preparing a crude mixture of the dimerisation reaction from 5-acetamido-N,N-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”) to iodixanol for the crystallization of iodixanol. In particular, it relates to an industrial procedure of simultaneously reducing the salt content and the alcoholic dimerisation solvent using a nanofiltration system prior to the crystallization of iodixanol.

Abstract: This invention relates generally to non-ionic X-ray contrast agents. It further relates to a method of using solid adsorbents to reduce backpeaks content in the purification of iodixanol. In particular, it relates to the use of non-polar organic adsorbents with the average pore diameter smaller than about 30 nm. Specific examples of adsorbents of the instant invention include non-polar acrylic ester, di-vinyl benzene resins, poly-styrene di-vinyl benzene resins, and carbon adsorbents. In certain embodiments, upwards of 30% of the backpeak levels and 60% N-acetyl cyclic iodixanol levels are reduced for a 5% loss of iodixanol.

Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with propyleneglycol as solvent.

Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with a solvent mixture comprising 1-methoxy-2-propanol and water or methanol.

Abstract: This invention relates to the isolation of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the isolation of iodixanol from an aqueous solution.

Abstract: Disclosed are a series of ?-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The ?-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.

Abstract: This invention relates to an improved method for the synthesis of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, it relates to a continuous process of deacetylation of the acetylated hydroxyl group in 5-amino-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide (“Compound B”) followed by crystallisations, filtration, and washing of Compound A.

Abstract: This invention relates to the manufacture of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis (2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the purification of iodixanol by crystallization by using ultrasound.

Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with water as solvent.

Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with methanol as solvent.

Abstract: This invention relates to the manufacture of iodixanol(1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the purification of iodixanol by crystallization by using wet milling.

Abstract: In accordance with the disclosure, one aspect of the present application is directed to a dispersant compound comprising the reaction product of (i) a hydrocarbyl carbonyl compound, (ii) a polycarbonyl compound having at least three carbonyl acylating functions, and (iii) a primary amine moiety of a polyamine. Methods of making and methods of using the dispersant compound are also disclosed.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula R—N(CO—CH3)—X—N(CO—CH3)—R and salts or optical active isomers thereof, wherein X denotes a C3 to C4 straight or branched alkylene moiety wherein the alkylene moiety is substituted by one or two hydroxyl groups, optionally hydroxylated alkyl groups and/or alkoxy groups; and each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties. The invention also relates to the use of such diagnostic compositions contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: This invention relates generally to the preparation of non-ionic X-ray contrast agents, iohexyl, ioversol, and iodixanol. It further relates to a method for improving the purity of 5-amino-N,N?-bis(2,3-dihydroxypropyl)-isophthalamide (or ABA), an intermediate in the industrial preparation of these non-ionic X-ray contrast agents. In particular, it relates to a method for significantly removing ABA monomethylester and ABA dimer from ABA by hydrolyzing ABA under a pH between about 12 to about 13 in an aqueous medium to convert ABA monomethylester to ABA monoacid, before the iodination reaction of ABA.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula R—N(CHO)—X—N(R3)—R wherein X denoted an optionally substituted alkylene group, R3 denotes a hydrogen atom or an acyl function and each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: The present invention provides for the identification of individuals having neurodegenerative diseases (ND). Peptoids recognized by Parkinson's Disease- and Alzheimer's Disease-specific antibodies are identified, allowing one to diagnose or predict ND in subjects.

Abstract: The invention relates to a water-dispersible derivative of a therapeutic agent having a low water solubility that comprises at least one molecule of said agent covalently bonded to at least one molecule of a hydrocarbon derivative having a squalenic structure or the like. The invention further relates to corresponding nanoparticles.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.

Abstract: A process for the preparation of iosimenol comprising reacting 5,5?-[(1,3-dioxo-1,3-propanediyl)diimino]bis[N-(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide] (C-VI) with a 3-halo-1,2-propanediol in an aqueous solvent. A process for the preparation of C-VI comprising reacting 3,3?-[(1,3-dioxo-1,3-propanediyl)diimino]bis[5-(aminocarbonyl)-2,4,6-triiodobenzoyl chloride] (C-V) with 3-amino-1,2-propanediol in the presence of an inorganic base and a suitable non-aqueous polar solvent. A process for the preparation of C-V comprising reacting 3-amino-5-(aminocarbonyl)-2,4,6-triiodobenzoyl chloride (C-IV) with malonyl dichloride in a solvent comprising a suitable ester solvent, a suitable nitrile solvent or mixtures thereof.

Abstract: Aromatic polyamines are derivatized with polycarboxylic acids or their derivatives to form polyamine amides) containing pendant amine groups; the derivatives have enhanced curative properties when used as curatives for polyureas, hybrid epoxy-urethanes, hybrid urea-urethanes, chain extenders for polyurethane and polyurea elastomers, and also for reaction injection molding (RIM) products.

Abstract: The object of the present invention is to provide a pharmaceutical composition for preventing or treating viral infectious diseases. The compounds of the present invention have extremely potent anti-HCV activity and HCV growth inhibitory effects, and since they also only demonstrate mild cytotoxicity in vivo, a pharmaceutical composition containing the compound of the present invention is extremely useful as an anti-HCV preventive/therapeutic agent.

Abstract: Pharmaceutical compositions for treating and/or pre-treating or preconditioning the animal central nervous system against the effects of Alzheimer's Disease including the associated neurodegeneration and cognitive, behavioral and physical impairments. In one embodiment, an effective dose of deferoxamine (DFO) is administered to the upper one-third of the subject patient's nasal cavity to effectively bypass the blood-brain barrier, thereby allowing application of the DFO dose directly to the central nervous system.

Abstract: Disclosed herein are the compounds shown below and methods of their synthesis. The value m is a positive integer. R comprises an alkyl chain or an alkoxy chain. Each X comprises a metal binding group. Each E is a methoxy group or comprises a biomolecule reactive group or a residue thereof. E optionally comprises a protecting group. The value n is a positive integer. The value p is zero or one. Y is OCH3, OH, NH2, or COOH.

Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The present invention relates to compounds that can be used as metal-ion-chelating agents or as depolluting agents, corresponding to general formula (I) below: and also to precursor compounds of formula (II) and labelled compounds of formula (III) deriving from the compounds of formula (I). The present invention also relates to the use of the compounds (I), (II) or (III) as a medicament, and also the use thereof for the diagnosis, prevention and treatment of neurodegenerative diseases such as Wilson's disease and Alzheimer's disease.

Abstract: Methods to prepare synthetic carbon nanotubes having controllable properties and synthetic carbon nanotubes having controllable properties are provided. The properties which are controllable using the methods provided here include independently and in combination: diameter, length, identity and number of functional groups present and identity and number of heteroatoms present.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula wherein each R1 independently are the same or different and denotes a hydrogen atom or a C1 to C4 straight of branched alkyl group; each R2 independently are the same or different and denotes a hydrogen atom or a C1 to C4 straight of branched alkyl group; and each R3, R4 and R5 independently are the same or different and denote C1 to C6 straight of branched alkyl moieties substituted by 1 to 6 —OH groups. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: The compounds of general formula (I) wherein: R1 is hydrogen, phenyl, C1-6 alkyl which can be further substituted with R3, R3 is 5- or 6-membered aromatic or heteroaromatic ring system which can be further substituted with benzyl or hydroxyl groups; R2 is OR4, NHR4, R4 is hydrogen, C1-6 alkyl or benzyl n is an integer from 1 to 12 or the salts of compounds mentioned which can form gels with commercial fuels, organic solvents and water.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula and salts or optical active isomers thereof, wherein each of R1, R2 and R3 independently are the same or different and denote a hydrogen atom or a C1 to C4 straight of branched alkyl group; each R4 independently are the same or different and denote C1 to C6 straight of branched alkyl moieties substituted by up to 6 —OH groups; and each R5 independently are the same or different and denote C1 to C6 straight or branched alkyl moieties substituted by up to 6 —OH groups. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing two linked iodinated phenyl groups of the general formula (I) and salts or optical active isomers thereof, wherein each of R1, R2 and R3 independently are the same or different and denote a hydrogen atom or a C1 to C4 straight of branched alkyl group; each R4 independently are the same or different and denote C1 to C6 straight of branched alkyl moieties substituted by up to 6 —OH groups; and each R5 independently are the same or different and denote C1 to C6 straight of branched alkyl moieties substituted by up to 6 —OH groups provided that at least one alkyl group is substituted with at least 2 hydroxy groups.

Abstract: The invention provides biomolecule binding ligands, collections of biomolecule binding ligands, and their use in the purification of biological mixtures and in the identification of ligands having an affinity for a substance.

Abstract: A compound consists of a fractal-like, plain or organometallic array useful for energy storage devices. A dendrimer useful in the synthesis of the fractal-like compound includes a single ligating moiety bound to a surface of each quadrant of the dendrimer. A method of making metallo-based (macro) molecules includes the steps of combining monomers selected from the group consisting of bipyridal- and terpyridal-based ligands with connecting metals and self assembling macrocycles wherein the monomes are interconnected by the metals.

Abstract: The invention relates to newly identified pentamine based surfactant compounds, to the use of such compounds and their production. The invention also relates to the use of the pentamine based compounds to facilitate the transfer of polynucleotides into cells.

Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a triamine alkyl central moiety allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a tris(aminoalkyl)amine group allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.

Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: This invention relates to newly identified spermidine based surfactant compounds, to the use of such compounds and to their production. The invention also relates to the use of the spermidine based compounds to facilitate the transfer of polynucleotides into cells.

Abstract: There are provided multi-chain lipophilic polyamine compounds and derivatives thereof, pharmaceutical formulations comprising the same, method of making and using said compounds or formulations.

Abstract: A process for the manufacture of iodixanol by performing a crystallization process of the crude product in a solvent mixture comprising water, methanol and isopropanol. The crude product may be obtained in aqueous solution from dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”).