Abstract: The present invention relates to a polymer particles comprising a polymer bead stabilized by vinylsulfonyl-functionalized polymers grafted to the surface of the bead, as well as a particle composition comprising monodisperse polymer beads stabilized by vinylsulfonyl-functionalized polymers, wherein the vinylsulfonyl-functionalized polymers are grafted to the surfaces of the beads. The invention also includes a method of preparing monodisperse polymer particles comprising preparing a homogeneous solution of an ethylenically unsaturated polymerizable monomer, an initiator, and a polymeric stabilizer, wherein the polymeric stabilizer consists of repetitive units, wherein the repetitive units comprise latent vinylsulfonyl moiety, polymerizing the homogeneous solution, and converting the latent vinylsulfonyl moiety to vinylsulfonyl moieties.

Abstract: A method for preparing a resin particle having a large surface area and a shape factor (SF-1) of 110 to 800, which comprises a step of applying a shear force to an aqueous dispersion having a viscosity of 300 to 100,000 mPa·s formed by adding a thickener to an aqueous dispersion containing resin particles, and a subsequent step of decreasing the viscosity of the aqueous dispersion to 200 mPa·s or less by adding a viscosity decreasing agent as necessary. Resin particles obtained by the method can be used as additives for paint, additives for coating materials, powder coatings, additives for cosmetics, resins for slush molding, spacers for use in manufacturing electronic components or devices, standard particles for electronic measuring instruments, toners for electrophotography, toners for electrostatic recording, toners for electrostatic printing, and hot-melt adhesives.

Abstract: RANTES mutants characterised by the substitution or addition of amino acids at the N-terminal of RANTES wild-type sequence and in the N-loop and/or 40's loop regions of RANTES wild-type sequence, and their use as anti-HIV, anti-allergic or anti-inflammatory agents.

Abstract: The present invention relates to compositions containing novel proteins and methods of using those compositions for the diagnosis and treatment of immune related diseases.

Abstract: This invention provides novel compounds which prevent or block a FVIIa mediated or associated process or event such as the catalytic conversion of FX to FXa, FVII to FVIIa or FIX to FIXa. In particular aspects, the compounds of the invention bind Factor VIIa (FVIIa ), its zymogen Factor VII (FVII). The invention also provides pharmaceutical compositions comprising the novel compounds as well as their use in diagnostic, therapeutic, and prophylactic methods.

Abstract: Novel splice variants of the human H4 histamine receptor are described. The splice variants have delections of portions of the N-terminal of the wild type H4 receptor. The splice variants are useful in methods for identifying agonists, inverse agonists or antagonists of histamnie action at the H4 receptor.

Abstract: The present invention relates to TR20 polypeptides. In particular, isolated nucleic acid molecules are provided encoding human TR20 protein. TR20 polypeptides are also provided as are vectors, host cells and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of TR20 activity.

Abstract: This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide, a sugar and a salting-out salt.

Abstract: This invention provides methods and compositions for altering the growth, organization, and differentiation of plant tissues. The invention is based on the discovery that, in plants, genetically altering the levels of Retinoblastoma-related gene (RRB) activity produces dramatic effects on the growth, proliferation, organization, and differentiation of plant meristem.

Abstract: Compositions and methods are disclosed for stimulating or inhibiting angiogenesis and/or cardiovascularization in mammals, including humans. Pharmaceutical compositions are based on polypeptides or antagonists thereto that have been identified for one or more of these uses. Disorders that can be diagnosed, prevented, or treated by the compositions herein include trauma such as wounds, various cancers, and disorders of the vessels including atherosclerosis and cardiac hypertrophy. In addition, the present invention is directed to novel polypeptides and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention.

Abstract: Applicants have produced and isolated water soluble complexes of endotoxin and MD-2.

Abstract: Compositions and methods are disclosed for stimulating or inhibiting angiogenesis and/or cardiovascularization in mammals, including humans. Pharmaceutical compositions are based on polypeptides or antagonists thereto that have been identified for one or more of these uses. Disorders that can be diagnosed, prevented, or treated by the compositions herein include trauma such as wounds, various cancers, and disorders of the vessels including atherosclerosis and cardiac hypertrophy. In addition, the present invention is directed to novel polypeptides and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention.

Abstract: A highly magnetically aligned metallothionein (MT) containing manganese (Mn) and cadmium (Cd) has been synthesized. The metallotionein has a formula of Mnx Cd7?x MT with x being in the range of 1 to 6. Its size and biological functions are similar as those of the native metallothionein as tested by dynamic light scattering, UV, and CD spectroscopic experimental methods. Its maximum magnetic moment per formula unit, in saturation field, is estimated to be 19.46 ?B, and persists from 277 to 330 K.

Abstract: Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against bacteria, including gram positive organisms, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.

Abstract: A novel class of NIMA interacting proteins (PIN), exemplified by Pin1, is provided. Pin1 induces a G2 arrest and delays NIMA-induced mitosis when overexpressed, and triggers mitotic arrest and DNA fragmentation when depleted. Methods of identifying other Pin proteins and Pin-interacting proteins and identifying compositions which affect Pin activity or expression are also provided.

Abstract: This invention is about the functionally hyperactive light signal related molecule, HFR1-?N105, of which the nucleic acids that encode N-terminal 105 amino acid residues were deleted. HFR1 as a bHLH transcription factor functions in a subset of phytochrome A signaling cascade and it was reported to be regulated negatively by COP1. Experiments with a HFR1-?N105 overexpressing plant revealed that the deletion of N-terminal amino acids makes the HFR1 more active in photomorphogenic development such as germination and de-etiolation. In addition, the transgenic plants showed hypersensitive photo-responses in the inhibition of hypocotyl elongation, dependently on another positive element of light signaling, a bZIP protein, HY5. The end-of-day far-red light response and petiole elongation were suppressed in the HFR1-?N105 overexpressing plants. These results suggest that N-terminal region of HFR1 negatively regulate HFR1 function and that HFR1-?N105 is hyperactive.

Abstract: The invention features linker molecules that have at one terminus a amino-protecting group and at the other terminus a phosphorous activating group, typically phosphoramidite. The linker molecules can be used, for example, to produce amino-modified linkers that space an oligonucleotide from a solid support. The invention also features an amino-protected nucleotide that includes an activated phosphorous group such as a phosphoramidite for the production of a 5? amino-modified oligonucleotide. The invention further provides a phthalimido-modified support that can be used to synthesize a polynucleotide that includes an amino group at the 3? terminus.

Abstract: The present invention provides a method for making glycoside compounds including the steps of: (a) lithiating an aromatic reactant having a leaving group using a lithium reagent in a first microreactor under non-cryogenic conditions to form a lithiated anion species, and (b) coupling the lithiated anion species with a carbonyl substituted reactant to form a glycoside.

Abstract: The invention relates to macrocyclic metal complexes and their production and use for the production of conjugates with biomolecules. The conjugates are suitable as contrast media in NMR diagnosis and radiodiagnosis as well as for radiotherapy. High relaxivity is achieved by a special liganding of macrocyclic compounds, and a fine-tuning of the relaxivity is made possible.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.

Abstract: The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in their structure.

Abstract: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.

Abstract: A process for the preparation of a Group 4 metal amide complex comprising a monovalent or divalent Lewis base ligand the steps of the process comprising contacting a Group 4 metal amide with a neutral source of a monovalent or divalent, Lewis base ligand group and a solid Lewis acid scavenging agent under amine elimination conditions to form a Group 4 metal amide complex containing at least one less amide group per metal moiety than the initial Group 4 metal amide.

Abstract: Novel compounds which selectively bind to the ?-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the ?-opioid receptor have shown promise in providing enhanced analgesis without the addictive properties, the compounds of the present invention are better than morphine, naltrindole (NTI), spiroindanyloxymorphone (SIOM), and other known ?-opioid receptor selectors as analgesics.

Abstract: The present invention relates to an improved process for the preparation of pure Finasteride of Formula I, which comprises converting dihydrofinasteride to finasteride through novel protected dihydrofinasteride and protected finasteride intermediates.

Abstract: The invention relates to crystalline S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate, a process for its preparation and pharmaceutical formulations incorporating it as the active ingredient for use in treating microbial infections.

Abstract: This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] [in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.

Abstract: The present invention pertains to a process for obtaining a single enantiomer, d or l, of threo-methylphenidate, comprising resolution of a mixture of the enantiomers; racemisation of the unwanted enantiomer, to give a mixture of all four stereoisomers; and separation of the erythro stereoisomers, to leave the same mixture of enantiomers for resolution.

Abstract: A polymer-carrying optically active binaphthyl type oxazoline compound having axial asymmetry, represented by the following general formula (1) (wherein R1 and R2 may be the same or different from each other and each represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or the like; R3 is a hydrogen atom or —R5—X—R6; R4 is a hydrogen atom or the like; R5 is a straight- or branched-chain aliphatic hydrocarbon chain which may have a directly or indirectly bonded substituent; X is CH2, CO2, O, CONR7 or NR7; R6 is a directly or indirectly bonded polymer; and R7 is a hydrogen atom or the like), and to a transition metal complex which uses the compound as the ligand.

Abstract: The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is administered.

Abstract: Cyanoacetamides of the formula: and corresponding salts thereof; N?-(cyanoacetyl)-L-histidines, of the formula: and salts, tautomers and esters thereof; and N?-(cyanoacetyl)-3-methyl-L-histidines of the formula: and salts and esters thereof.

Abstract: A process for the preparation of benzylimidazole derivatives useful as intermediates for preparation of losartan, novel intermediates for their preparation and a process for the preparation of losartan.

Abstract: The present invention provides an improved process for the preparation of ?-polymorphic eletriptan hydrobromide.

Abstract: A process for continuously preparing 2-pyrrolidone by reacting gamma-butyrolactone with ammonia in the liquid phase in the presence of water, wherein the reaction is carried out at a temperature of from 275 to 300° C. and an absolute pressure of from 140 to 180 bar.

Abstract: Process for converting certain lactones to their alpha-methylene substituted forms that not only exhibits high initial activity (conversion), but also provides high reactor productivity (mass of product per mass of catalyst per unit of time) and sustained maintenance of a high level of activity and productivity with time on stream.

Abstract: Process for converting certain lactones to their alpha-methylene substituted forms that not only exhibits high initial activity (conversion), but also maintains a high level of activity with time on stream.

Abstract: This invention relates to a method of treating a disorder selected from OCD, agoraphobia, agoraphobia without history of panic disorder, specific phobia, social phobia, PTSD, restless legs syndrome, premenstrual dysphoric disorder, hot flashes, and fibromyalgia by administering a compound of the formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen, straight or branched alkyl of from 1 to 6 carbon atoms or phenyl; and R2 is straight or branched alkyl of from 4 to 8 carbon atoms, straight or branched alkenyl of from 2 to 8 carbon atoms, cycloalkyl of from 3 to 7 carbon atoms, alkoxy of from 1 to 6 carbon atoms, -alkylcycloalkyl, -alkylalkoxy, -alkyl OH, -alkylphenyl, -alkylphenoxy, or -substituted phenyl. The invention also relates to a method of treating the above disorders by administering the compound (3S,5R)-3-Aminomethyl-5-methyl-octanoic acid.

Abstract: A method of providing zinc to a subject in need of treatment includes administering to the subject an effective amount of a zinc-cysteine complex. The zinc-cysteine complex is preferably a zinc-monocysteine complex. The complexes of zinc-cysteine of the present invention increase the activity of antioxidant enzymes catalase and glutathione peroxidase, and the antioxidant protein metallothionein. The complexes of zinc-cysteine of the present invention protect retinal pigment epithelial cells from increasing hydrogen peroxide concentrations.

Abstract: A benzophenone compound, and an ink composition that includes the benzophenone compound can absorb UV light, and thus improve lightfastness of images produced with the ink composition containing the compound. Due to the function of the benzophenone compound as a lightfast dispersant, the dispersibility and the lightfastness of an ink composition are improved with the benzophenone compound, without requiring an additional lightfastness enhancer.

Abstract: Enzymatic preparation of (meth)acrylic esters containing urethane groups, and their use in radiation-curable compositions.

Abstract: In a process for reducing the visible color of a crude aromatic dicarboxylic acid containing colored contaminants, an aqueous ammonia solution of the crude aromatic dicarboxylic acid is prepared and contacted with hydrogen in a reactor in the presence of a heterogeneous metal-containing catalyst that includes a noble metal and a support. The process is carried out under conditions of temperature, pressure, and contact time effective to reduce the visible color of the aromatic dicarboxylic acid.

Abstract: In a process for heterogeneously catalyzed partial gas phase oxidation of propene to acrylic acid, the propene-containing starting reaction gas mixture is oxidized in a first reaction stage using a fixed catalyst bed 1 which consists of a plurality of fixed catalyst bed zones and is accommodated in two successive temperature zones A, B, and the acrolein-containing product gas mixture of the first reaction stage is then oxidized in a second reaction stage using a fixed catalyst bed 2 which consists of a plurality of fixed catalyst bed zones and is accommodated in two successive temperature zones C, D, and the transition from one temperature zone to another temperature zone within one reaction stage does not spatially coincide with a transition from one fixed catalyst bed zone to another fixed catalyst bed zone.

Abstract: A method for producing high purity glycolic acid crystals, which comprises the steps of: (1) providing an aqueous glycolic acid solution (A) which has (a) a water content of from 5 to 20% by weight, (b) a calculated monomeric glycolic acid weight ratio (ratio of the total weight of the monomeric glycolic acid and the component monomeric glycolic acid of the glycolic acid condensation product to the weight of the aqueous glycolic acid solution (A)) of from 0.60 to 1.00 and (c) a monomeric glycolic acid content of from 20 to 57% by weight; (2) depositing glycolic acid crystals from the solution (A); and (3) separating the deposited glycolic acid crystals from the solution (A).

Abstract: A gemini surfactant represented by the formula: wherein: each Rf independently represents perfluorobutyl or perfluoropropyl; each R1 independently represents alkyl having from 1 to 6 carbon atoms; L1 and L2 represent alkylene having from 2 to 18 carbon atoms; each R represents alkyl having from 1 to 6 carbon atoms; Z represents an organic divalent linking group; and nXm? represents an anion or anions having a charge m, wherein m and n are independently 1 or 2, and wherein the product of n and m is 2. Aqueous compositions containing the gemini surfactant are also disclosed.

Abstract: The invention concerns a production method which consists in forming a reaction medium containing 2,2,4,4,-tetramethyl-3-pentanone, hydrogen peroxide, ammonia and a zeolitic structure catalyst and allowing the reaction to obtain said oxime. 2,2,4,4,-tetramethyl-3-pentanone and hydrogen peroxide can be obtained by auto-oxidation of 2,2,4,4,-tetramethyl-3-pentanol with oxygen or air. Hydroxylammonium salts are obtained by acid hydrolysis of said oxime.

Abstract: A conjugate addition reaction between an ?,?-unsaturated ketone compound and a carbamate compound is carried out to synthesize a ?-aminoketone, a salt or a hydrate salt of a transition metal of Groups 7 to 11 of the Periodic Table of Elements being present in the reaction system as the catalyst. The novel method and the catalyst are capable of synthesizing the ?-aminoketone by the Aza-Michael reaction with high yield and efficiency.

Abstract: A process for producing a high purity trialkanolamine excelling in hue and having an APHA of not more than 40, characterizing by including producing a mixed alkanolamine by the reaction of an alkylene oxide with ammonia; removing low-boiling substances from the mixed alkanolamine; removing high-boiling substances by subjecting the product deprived of the low-boiling substance to vacuum distillation, and redistilling the distillate obtained by the vacuum distillation.

Abstract: The present invention is generally directed to electroluminescent Ir(III) compounds with phosphinoalkoxides and phenylpyridines or phenylpyrimidines, and devices that are made with the Ir(III) compounds.

Abstract: The present invention relates to a process of manufacture of polytrimethylene ether glycol, in which one or more inorganic compounds selected from an inorganic salt and an inorganic base is utilized during certain purification steps to reduce phase separation time.

Abstract: A process for preparation of cyclopropylethanol, which comprises subjecting a 3-cyclopropyl-2,3-epoxypropionic acid ester to solvolysis, treating the product of the solvolysis with an acid to obtain cyclopropylacetaldehyde, and reducing the obtained cyclopropylacetaldehyde; and a process for preparation of cyclopropylacetonitrile, which comprises subjecting a 3-cyclopropyl-2,3-epoxypropionic acid ester to solvolysis in the presence of a base, treating the product of the solvolysis with an acid to obtain cyclopropylacetaldehyde, reacting the obtained cyclopropylacetaldehyde with hydroxylamine or salts thereof to obtain cyclopropaneacetaldehyde oxime, and reacting the obtained cyclopropaneacetaldehyde oxime with acetic anhydride. According to the present invention, cyclopropylethanol and cyclopropylacetonitrile can be prepared at low costs and industrially advantageously.