Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.

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 disclosed invention relates to a process, comprising: conducting unit operations in at least two process zones in a process microchannel to treat and/or form a non-Newtonian fluid, a different unit operation being conducted in each process zone; and applying an effective amount of shear stress to the non-Newtonian fluid to reduce the viscosity of the non-Newtonian fluid in each process zone, the average shear rate in one process zone differing from the average shear rate in another process zone by a factor of at least about 1.2.

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: The present invention provides a gene transfer agent, a gene transfer kit, and a gene transfer method excellent in safety and transfer efficiency. Specifically, the present invention provides a gene transfer agent composition, the gene transfer agent composition including a compound represented by any one of the following formulae DL-G1 to DL-G4: DL-G1: R1R2NX(XH2)2; DL-G2: R1R2NX(X(XH2)2)2; DL-G3: R1R2NX(X(X(XH2)2)2)2; and DL-G4: R1R2NX(X(X(X(XH2)2)2)2)2 (X represents —CH2CH2CONHCH2CH2N—), in which: R1 represents an unsaturated long-chain aliphatic group; and R2 represents an unsaturated long-chain aliphatic group or a saturated long-chain aliphatic group in the formulae.

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 an aliphatic central moiety containing amide functions 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: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.

Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain

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 an aliphatic 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: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.

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 hydrophilic aliphatic 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: 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 an aliphatic central moiety containing urea or urethane functions 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: The present invention provides a nanocarrier having an interior and an exterior, the nanocarrier comprising at least one conjugate, wherein each conjugate includes a polyethylene glycol (PEG) polymer. Each conjugate also includes at least two amphiphilic compounds having both a hydrophilic face and a hydrophobic face. In addition, each conjugate includes an oligomer, wherein at least 2 of the amphiphilic compounds are covalently attached to the oligomer which is covalently attached to the PEG. The nanocarrier is such that each conjugate self-assembles in an aqueous solvent to form the nanocarrier such that a hydrophobic pocket is formed in the interior of the nanocarrier by the orientation of the hydrophobic face of each amphiphilic compound towards each other, and wherein the PEG of each conjugate self-assembles on the exterior of the nanocarrier.

Abstract: The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available ?-hydroxyacid or a salt thereof.

Abstract: Poly(disulfide amine)s, methods of making, and methods of use are described. Illustrative embodiments of the poly(disulfide amine)s include poly(N,N?-cystaminebisacrylamide-spermine), poly(N,N?-cystaminebisaciylamide-N,N?-bis(3-aminopropyl)1,3-propanediamine), poly(N,N?-cystaminebisacrylamide-N,N?-bis(3-amino-propyl)ethylenediamine), poly(N,N?-cystaminebisacrylamide-N,N?-bis(2-aminoethyl)-1,3-propanediamine), and poly(N,N?-cystaminebisacrylamide-triethylenetetramine). These compositions are made by Michael addition between N,N?-cystaminebisacrylamide and protected oligoamine monomers, followed by deprotection. Complexes are formed by mixing the poly(disulfide amine)s with a nucleic acid. Delivery of the nucleic acid into cells is carried out by contacting the cells with the nucleic acid/poly(disulfide amine) complexes.

Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.

Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.

Abstract: Described herein are methods, compositions and articles of manufacture involving neutral conjugated polymers including methods for synthesis of neutral conjugated water-soluble polymers with linkers along the polymer main chain structure and terminal end capping units. Such polymers may serve in the fabrication of novel optoelectronic devices and in the development of highly efficient biosensors. The invention further relates to the application of these polymers in assay methods.

Abstract: The present invention relates to a method for selectively crystallizing Z isomer of iopromide of formula (I) comprising a) dissolving a crude iopromide comprising a mixture of E and Z isomers or a concentrate thereof in an alcohol, and b) heating the resulting alcohol solution to obtain crystalline of Z isomer of iopromide; and a method for preparing a composition comprising the crystalline Z isomer of iopromide.

Abstract: Compositions and methods for labeling biological targets using a conjugate of a luminescent component and a targeting molecule attached to a nanoparticle core structure are described. The labeling conjugates offer high intensity and low background, and are ideal for histology and pathology.

Abstract: Certain poly(oxyalkylene) colorants are disclosed along with method of preparation thereof. A method of using these colorants as fluorescent security taggants is also disclosed.

Abstract: Compositions for producing multi-chromic (“color”) magnetic resonance images (MRI). The compositions for use as MRI imaging agents include a magnetic resonance imaging tracer having a signal emitter, such as a 19F imaging tracer (19FIT), conjugated with a magnetic signal modulator, such as a paramagnetic functional group or a paramagnetic ion. The 19FIT and the signal modulator (M) are joined covalently by a chelator such as DOTA, forming a nanometer-sized fluorinated paramagnetic complex 19FIT-DOTA-M. Other signal emitters, such as 31P imaging tracer (31PIT), can also be modulated using this strategy (i.e., 31PIT-DOTA-M) to generate multi-chromic 31P MRI or MRS.

Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.

Abstract: The present invention relies on a process for the preparation of non ionic iodinated contrast agents and, in more details, it relates to a process for the preparation of Iopamidol in high yields and with a high degree of purity. In more details, the invention discloses a process for the preparation of a compound of formula (III) comprising the 5 condensation reaction a compound of formula (II) with 2-amino-1,3-propandiol, being said reaction carried out in an aprotic dipolar solvent and in the presence of an alkaline or alkaline rare earth metal oxide or hydroxide.

Abstract: A process for the preparation of iodixanol by dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (“Compound A”) in which, after the dimerisation step, unreacted Compound A is precipitated from the reaction mixture and recovered for re-use. The process substantially increases the net yield of iodixanol and simplifies its purification.

Abstract: The present invention relates to modulators of metalloproteinase activity.

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: 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: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.

Abstract: The present invention provides compounds useful as contrast agents, such as for the CT imaging of cartilage tissue. The contrast agents are generally iodinated organic molecules that are positively charged under physiological environments. Also provided are compositions containing contrast agents and methods of using the agents, including, for example, the monitoring of glycosaminoglycan content in cartilage tissue. The invention provides non-invasive analytical techniques for the diagnosis of osteoarthritis in its earliest stages. The invention also provides improvements over existing contrast agents for cartilage monitoring, which tend to exhibit low residence times and require high dosages.

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

Abstract: The invention provides dendrimeric compounds of the formula 1 comprising amino acids, wherein n is an integer of 1-4, T is an alkylidene —(CH2)2CONH(CH2)2- group, R2 is an —NH2 group or a moiety of a primary organic amine, and P is an amino acid and/or peptide moiety, wherein at least one hydrogen atom of at least one amino group is optionally replaced by a protective group, and a hyperbranched core compound of the formula 3, wherein T and R2 are as defined above. The invention provides also a process for the preparation of a dendrimeric compound and a hyperbranched core, wherein the process employs addition reactions of alkyl acrylate and a basic amino acid, and use of a hyperbranched core for the preparation of a dendrimeric compound comprising amino acids. The invention provides also use of dendrimeric compounds for the preparation of the medicament for inhibiting growth of bacterial cells, fungi and tumor cells.

Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.

Abstract: Multi-arm amine compounds and compositions for enhancing intracellular, in vitro, and in vivo delivery of drug, active, and therapeutic substances including ribonucleic acids. This disclosure provides novel compounds and compositions for making and using delivery materials and carriers which increase the efficiency of delivery of biologically active and pharmacologically active molecules. Embodiments of this disclosure may further provide delivery of various therapeutic agents including nucleic acid therapeutics such as regulatory RNA, interfering RNA, and agents for RNAi, as well as other protein and peptide therapeutics. In some aspects, this disclosure provides multi-arm amine compounds and compositions which can enhance permeation of a drug substance.

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: 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 compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.

Abstract: The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.

Abstract: The present invention provides siRNA delivery methods use in vivo or in vitro. The delivery methods include conjugation with delivery peptides and mixing with dendrimers.

Abstract: The present invention relates to a compound of formula (I) wherein X is hydrogen, R1, R1C(O), R1CO2, or a COX2 inhibitor, wherein R1 is C1-20 alkyl, aryl, arylalkyl, alkyloxy or arylalkyloxy; wherein Y is OR2, NHR3N(R3)2, or a COX inhibitor; wherein R2 is hydrogen or C1-20 alkyl and each R3 is independently hydrogen or a C1-4 alkyl; wherein T is OR4, NHR5N(R5)2, or a COX inhibitor wherein R4 is hydrogen or C1-20 alkyl and each R5 is independently hydrogen or a C1-4 alkyl; wherein Z is hydrogen, R6, R6C(O), R6CO2, or a COX2 inhibitor; wherein R6 is C1-20 alkyl, aryl, arylalkyl, alkyloxy or arylalkyloxy; with the proviso wherein when X and Z are hydrogen and T is OH, Y is not OH; for use in the prevention and/or treatment of pain wherein said compound is provided for systemic administration.

Abstract: The present invention provides compositions and methods for the treatment of atherosclerosis and other related diseases. In some embodiments, a method comprises providing a composition and forming a coating of the composition on at least a portion of the interior and/or exterior surface of a tissue lumen or other body surface. The composition may remain associated with the tissue lumen or other body surface even in the presence of a strong flow of a fluid (e.g., blood flow in a blood vessel). The composition may associate with the tissue lumen via a plurality of covalent bonds. In some cases, the compositions may comprise at least one additive, for example, a therapeutically active agent or an imaging agent.

Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.

Abstract: A process for separating soluble silica species such as monomeric silicic acid (or monosilicic acid) and low molecular weight soluble polymeric silica from impure water soluble compounds by membrane nanofiltration is provided. A process for separating soluble silica species and colloidal silica from impure water soluble compounds by reverse phase liquid chromatography is also provided.

Abstract: Disclosed herein are ink compositions including an ink vehicle and a colorant, wherein the ink vehicle comprises a compound having a formula of: R1—CONH—R6—CONH—R3, R1—NHCO—R6—CONH—R3, R1—CONH—R6—NHCO—R3, R1—NHCO—R6—NHCO—R3, R1—CONH—R6—CONH—C36H64+n—CONH—R6—CONH—R3, R1—NHCO—R6—NHCO—C36H64+n—NHCO—R6—NHCO—R3, R1—CONH—R6—NHCO—C36H64+n—CONH—R6—NHCO—R3, R1—NHCO—R6—CONH—C36H64+n—NHCO—R6—CONH—R3, R1—CONH—R4—CONH—C36H64+n—CONH—R5—CONH—R3, R1—CONH—R4—NHCO—C36H64+n—CONH—R5—NHCO—R3, R1—NHCO—R4—CONH—C36H64+n—NHCO—R5—CONH—R3, R1—NHCO—R4—NHCO—C36H64+n—CONH—R5—CONH—R3, or R1—CONH—R4—CONH—C36H64+n—NHCO—R5—NHCO—R3, wherein n is an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, R6 is a cyclic group having from 5 to 8 carbon atoms, R1 and R3 each comprise a branched alkyl group derived from isostearic acid, and R4 and R5 are the same or different and comprise an alkylene having from 1 to about 200 carbon atoms or

Abstract: Disclosed herein are compounds having a formula of: R1—CONH—R6—CONH—C36H64+n—CONH—R6—CONH—R3, R1—NHCO—R6—NHCO—C36H64+n—NHCO—R6—NHCO—R3, R1—CONH—R6—NHCO—C36H64+n—CONH—R6—NHCO—R3, R1—NHCO—R6—CONH—C36H64+n—NHCO—R6—CONH—R3, R1—CONH—R4—CONH—C36H64+n—CONH—R5—CONH—R3, R1—CONH—R4—NHCO—C36H64+n—CONH—R5—NHCO—R3, R1—NHCO—R4—CONH—C36H64+n—NHCO—R5—CONH—R3, R1—NHCO—R4—NHCO—C36H64+n—CONH—R5—CONH—R3, or R1—CONH—R4—CONH—C36H64+n—NHCO—R5—NHCO—R3, wherein n is an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, R6 is the same or different cyclic group having from 5 to 8 carbon atoms, R4 and R5 are the same or different and comprise an alkylene having from 1 to about 200 carbon atoms, and R1 and R3 are the same or different and comprise a straight chain or branched alkyl group having from about 3 carbon atoms to about 200 carbon atoms and one or both of R1 and R3 include at least one hydroxyl group substituent, and ink compositions including the compounds as an ink vehicle.

Abstract: A novel class of peptide ?-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl ?-ketoamide derivatives.

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: There is provided a biomaterial having a functionalised surface which comprises bi-functional semi-dendrimers. The biomaterial may be ceramic, metallic and/or polymeric. It will usually be in the form of a solid, but could be a semi-solid or hydrogel. There is also provided a method of making a biomaterial having a functionalised surface which comprises bi-functional semi-dendrimers, said method comprising adsorbing, grafting or synthesising in situ bi-functional semi-dendrimers onto the surface of a biomaterial. There is further provided a biomedical device which is coated with or formed from a biomaterial having a functionalised surface which comprises bi-functional semi-dendrimers. The biomedical device may be a medical implant, for example, such as a stent, artificial hip joint or replacement heart valve. FIG. 1 is a schematic representation of a bi-functional semi-dendrimer structure suitable for biomaterial functionalisation according to the present invention.