Abstract: New peptide-based Gemini compounds comprising two linked chains (a) each having: (1) a positively charged hydrophilic head, Q1 or Q2 formed from one or more amino acids and/or amines, (2) a central portion, P1 or P2, having a polypeptide backbone, and (3) a hydrophobic tail, R1 or R2, the central sections of each chain being linked together by bridge Y through residues in P1 and P2, are disclosed. Methods for their preparation and uses are also disclosed. Such uses include transfection of polynucleotides into cells in vivo.

Abstract: Methods for preparing chiral non-racemic cyanoamines are provided. The methods are useful, e.g., for preparing chiral amino acids.

Abstract: The present invention features two members of laminin family, i.e., laminin 13 and laminin 14, the methods of making these molecules, and the methods of using these molecules in treating neural disorders, e.g., retinal disorders. The present invention also features using a preparation of laminin 5 to treat neural disorders, especially disorders associated with retina.

Abstract: This invention relates to a novel nuclear protein which interacts with the androgen receptor in vivo and in vitro, and which also possesses ATPase activity. The invention concerns also mRNA and DNA sequences encoding said protein.

Abstract: The invention is directed to purified and isolated novel ACPL polypeptides, the nucleic acids encoding such polypeptides, processes for production of recombinant forms of such polypeptides, antibodies generated against these polypeptides, fragmented peptides derived from these polypeptides, and the uses of the above.

Abstract: The invention relates to a novel methods for measuring cellular ion channel transmission and methods and compositions useful in the identification of ligand gated ion channel agonists and modulators.

Abstract: A method is provided for removing citrate, aluminum, and other multivalent ions and contaminants from proteins by adjusting the pH of a solution containing the protein to a pH from about 7 to about 10, and diafiltering the pH-adjusted solution against aqueous solutions which have a low level of ions.

Abstract: The invention is directed to isolated DNAs having nucleic acid sequences which encode proteins which regulate aureobasidin sensitivity. Also disclosed are recombinant plasmids containing the DNAs, transformants containing the plasmids, and methods of producing the proteins.

Abstract: A method of diagnosing metabolic bone diseases, especially osteoporosis and arthrosis characterized by determining the concentration of osteoclastgenesis inhibitory factor (OCIF) in humor. Monoclonal antibodies recognizing equally both of monomer type and dimer type of OCIF. Monoclonal antibodies recognizing selectively dimer type of OCIF. And to provide an assay kit for determination of OCIF concentration comprising the aforementioned two antibodies recognizing different epitope of OCIF and having high affinity showing dissociation constant of less than 2×10−7 M with antigen. It is useful for a method of diagnosing metabolic bone diseases, especially osteoporosis and arthrosis or for an assay reagent for research thereof.

Abstract: Antibodies that bind to a 40 kDa protein which is expressed on tumors, but is not expressed on normal adult hemopoietic cells are disclosed. Also disclosed are methods for production and the use of such antibodies.

Abstract: The invention relates to a novel process for preparation of a biomarker specific for O-acetylated sialic acid and useful for the diagnosis, monitoring outcome of treatment and prediction of relapse of acute lymphoblastic leukemia, said process comprising the steps of (I) separating serum from the blood of patients of acute lymphoblastic leukemia; (ii) separation of low molecular weight fractions and galactose binding proteins from the serum on affinity matrix; (iii) passing the galactose free protein fraction obtained in step (ii) over another affinity matrix to capture O-acetyl sialic acid specific protein fraction; (iv) eluting specific protein fraction with a buffer at alkaline pH in the range of 8.0-11.

Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.

Abstract: The invention provides a novel method for synthesizing Morphine-6-Glucuronide comprising the step of reacting 3-O-pivaloyloxymorphine and methyl 1&agr;,2-ethylorthopivalate-3,4-di-O-pivaloylglucouronate.

Abstract: The present invention relates to a composite sponge wound dressing and method for producing the same. Chitosan and &bgr;-Chitin is mixed in a specific ratio for forming the sponge for wound repairing. Particularly, when said ratio is between 0.1˜1, the composite sponge wound dressing has a better absorption and tensile strength.

Abstract: DNA constructs, host cells and production methods are disclosed for the expression and recovery of polypeptides, especially those altered to have one or more glycosylation sites added or deleted. The DNA constructs, host cells and methods provided herein employ a DNA segment corresponding to a mammalian tissue plasminogen activator signal and/or pro peptide.

Abstract: The present invention provides isolated mammalian GalR3 receptors, isolated or recombinant nucleic acids and recombinant vectors encoding the same, host cells comprising the nucleic acids and vectors, and methods for making the receptors using the host cells. This invention further provides antibodies and antigen binding fragments thereof which specifically bind to the receptors and are useful for treating medical conditions caused or mediated by galanin. Also provided are screening methods for identifying specific agonists and antagonists of the mammalian GalR3 receptors.

Abstract: A gene which encodes a murine leukocyte &agr;(1,3)fucosyltransferase capable of synthesizing the sialyl Lewis x determinant has been cloned.

Abstract: The present invention relates to DNA molecules encoding splice variants of the melanocortin-1 receptor (MC-R1) protein belonging to the rhodopsin sub-family of G-protein coupled receptors, recombinant vectors comprising DNA molecules encoding MC-R1B protein, recombinant host cells which contain a recombinant vector encoding MC-R1B, the human MC-R1B protein encoded by the DNA molecule, and methods of identifying selective agonists and antagonists of MC-R1B proteins disclosed throughout this specification.

Abstract: The invention provides for the use of isolated polynucleotides encoding maize poly (ADP-ribose) polymerase (PARP) proteins to produce eukaryotic cells and organisms, particularly plant cells and plants, with modified programmed cell death. Eukaryotic cells and organisms particularly plant cells and plants, are provided wherein either in at least part of the cells, preferably selected cells, the programmed cell death (PCD) is provoked, or wherein, on the contrary, PCD of the cells or of at least part of the cells in an organism is inhibited, by modulation of the level or activity or PARP proteins in those cells.

Abstract: The invention discloses the Neisseria meningitidis NMASP polypeptide, polypeptides derived therefrom (NMASP-derived polypeptides), nucleotide sequences encoding said polypeptides, and antibodies that specifically bind the NMASP polypeptide and/or NMASP-derived polypeptides. Also disclosed are prophylactic or therapeutic compositions, including immunogenic compositions, e.g., vaccines, comprising NMASP polypeptide and/or a NMASP-derived polypeptide. The invention additionally discloses methods of inducing a immune response to Neisseria meningitidis and Neisseria meningitidis NMASP polypeptide and an NMASP-derived polypeptide in animals.

Abstract: Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R1, R2, R3, R4, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3′ and 5′ hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.

Abstract: The present invention is directed to N-acetyl-D-glucosamine obtained from microbial biomass, and to methods of obtaining N-acetyl-D-glucosamine from microbial biomass. In particular, the present invention is directed to the use of fungal biomass to create N-acetyl-D-glucosamine. The N-acetyl-D-glucosamine is efficiently obtained at high purity by degrading chitin in the fungal biomass to create N-acetyl-D-glucosamine.

Abstract: This invention concerns derivatives of rapamycin and their antifungal uses. Also disclosed are materials and methods relevant to the identification of non-immunosuppressive anti-fungal rapamycin derivatives. Use of compounds, among others, of the formula is disclosed, where the various substitutents are as defined.

Abstract: Metal chelates capable of exhibiting an immobilized relativity between about 60 and 200 mM−1s−1/metal atom are useful as magnetic resonance imaging agents. Additionally, a compound which is useful as a metal-chelating ligand has the following formula: wherein Q is a 4- to an 8-membered carbocyclic ring which may be fully or partially saturated; t is an integer from 2 to 16; each R group is independently hydrogen, —OH, —CH2—A, —OCH2CH(OH)CH2—A or a functional group capable of forming a conjugate with a biomolecule, provided that at least two of the R groups are selected from —CH2—A or —OCH2CH(OH)CH2—A; and A is a moiety capable of chelating a metal atom.

Abstract: Described is a process for the preparation of a particulate tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione product by combining a first aqueous solution comprising methylammonium N-methyldithiocarbamate with a second aqueous solution comprising formaldehyde, followed by separation and drying of the resulting solid, which comprises combining the first and the second aqueous solutions in such a way that the ratio between the concentrations of dithiocarbamate functions and of formaldehyde is essentially constant in the reaction mixture over time during the duration of the reaction.

Abstract: The present invention relates to the synthesis and the evaluation of the antioxidant, hypocholesterolemic and hypolipidemic activity of substituted morpholine derivatives of formula (I) in which R1=CH2CH3, R2=CH3, R3, R4=H, R5=C6H5 (compound 1) or R1=CH2CH2CH2ONO2, R2=CH3, R3, R4=H, R5=C6H5 (compound 2) or R1=H, R2—R3=(CH2)4, R4=H, R5=C6H5 (compound 3) or R1=CH2CH2CH3, R2—R3=(CH2)4, R4=H, R5=C6H5 (compound 4) or R1=CH2CH2CH2ONO2, R2—R3=(CH2)4, R4=H, R5=C6H5 (compound 5) or R1=H, R2=CH3, R3—R4=(CH2)4, R5=C6H5 (compound 6) or R1=CH2CH2CH3, R2=CH3, R3—R4=(CH2)4, R5=C6H5 (compound 7) or R1=CH2CH2CH2ONO2, R2=CH3, R3—R4=(CH2)4, R5=C6H5 (compound 8) or R1=CH2CH2CH2ONO2, R2=CH3, R3, R4=H, R5=C6H5 (compound 9) or R1=H, R2&equals

Abstract: A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted all, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II)  with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX),  to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).

Abstract: Process for preparing 4,6-dimethoxy-2-(methylsulfonyl)-1,3-pyrimidine by reacting 4,6dichloro-2-(methyltio)-1,3-pyrimidine in an inert organic solvent with an alkali metal methoxide, transfer of the resulting 4,6-dimethoxy-2-(methylthio)-1,3-pyrimidine into an aqueous-acidic medium and subsequent oxidation of this compound, of appropriate in the presence of a catalyst, wherein the oxidation is followed by a purification step in which the aqueous-acidic reaction mixture is adjusted with aqueous base to a pH in the range of 5-8 and stirred either in the presence or in the absence of an organic solvent, and the use of this compound for preparing herbicides, for example 7-[(4,6-dimethoxy-pyrimidin-2-yl)thio]-3-methylphthalide.

Abstract: The invention relates to a process for the preparation of 4,6-dihydroxypyrimidine by reaction of malonic ester with formamide and alkali metal alkoxide. The malonic ester is added alone or simultaneously with the total quantity or a portion of the formamide, in portions or continuously with monitoring of the temperature, to the alkali metal alkoxide prepared as a solution or suspension in an alcohol, alone or together with the total quantity or remaining quantity of the formamide. A temperature of from 102 to <120° C. is then set for from 10 to <60 minutes. The work-up after the holding time in said temperature range is then carried out by methods known per se.

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein Y is CH or N and Z is H, OCH3, NH2 and alkyl of from 1 to 4 carbon atoms, with the proviso that when Y is N the 2,4-diaminophenoxy moieties are positioned at the 4 and 6 positions on the pyrimidine ring.

Abstract: Methods of preparing compounds of Formula I are provided.

Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is —(CH2)nN+HR3R4 X− or R1 is —(CH2)nN+HR3R4 X− or —(CH2)nNR3R4 when R2 is —N+HR6R7. R2 is —OR5, halogen, —NR6R7, —N+HR6R7 X− sulphonic acid, nitro, —NR5COOR5, —NR5COR5 or —OCOR5; R3 and R4 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; each R5 is independently —H or a C1-C4 alkyl group; R6 and R7 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; n is an integer from 0-3; and X− is the carboxylate anion of an organic carboxylic acid compound. Also disclosed are methods of preparing certain compounds represented by Structural Formula (I).

Abstract: A method of making HIV protease inhibitors of general formula (1): These HIV compounds inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other antiviral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

Abstract: Photochromic chemicals consisting essentially of colored fluorescent heterocyclic fulgides are particularly suitable for optical memories. The preferred heterocyclic photochromic fulgides consist essentially of colored 2-indolyfulgides capable of excitation by ultraviolet light to fluoresce. These heterocyclic photochromic fulgides are preferably synthesized by process of (1) condensation of 1,3-dimethyl-(5-substituted)indole-2-carboxaldehyde with diethyl IV iospropylidenesuccinate as a key intermediate; followed by (2) hydrolysis; and (3) intramolecular acid anhydride formation.

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract: The present invention provides an efficient process for the preparation of benzothiophenecarboxamide PGD2 antagonist, S-5751.

Abstract: A method of refining a crystal of a crude cyclic ester comprises the steps of supplying the crude cyclic ester to a vertically extending cylindrical refiner (1) from an inlet (3) provided at a lower part of the refiner (1), agitating the crude cyclic ester by an agitator provided in the refiner (1) to make the crude cyclic ester flow upwardly, refining the crystals of the crude cyclic ester by counterflow-contact between the upflowing crude cyclic ester and a downflowing melted liquid containing a refined crystal component, and taking out refined crystals of the crude cyclic ester from an outlet (4) provided at an upper part of the refiner (1).

Abstract: The invention concerns a process for the production of optically active epoxides useful as pharmaceutical intermediates, particularly in the field of HIV protease inhibitors. The optically active epoxides are produced in commercially acceptable yields from an optically active alcohols by a Mitsunobu reaction and a cyclisation step, preferably comprising an intermediate re-crystallisation step. The stereochemistry of the alcohol is inverted during the Mitsunobu reaction to produce the desired epoxide.

Abstract: The present invention provides a process for the preparation of an enantiomerically enriched non-racemic chiral diol and an enantiomerically enriched non-racemic chiral epoxy compound by a hydrolytic kinetic resolution reaction. The process includes the step of contacting oxygen and mixture including a racemic chiral epoxy compound, a non-racemic Co(II) complex catalyst, an aromatic carboxylic acid and water, at a temperature and length of time sufficient to produce a mixture of said non-racemic chiral diol and said non-racemic chiral epoxy compound. The present invention also provides a process for the preparation of an enantiomerically enriched non-racemic chiral diol and an enantiomerically enriched non-racemic chiral epoxy compound by a hydrolytic kinetic resolution reaction.

Abstract: This invention provides estrogenic agents having the formula wherein A and B are each, independently, R is SO3−X+; X+ is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dialkylammonium containing 1-6 carbon atoms in each alkyl group, or trialkylammonium containing 1-6 carbon atoms in each alkyl group; with the proviso that at least one of A or B is

Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.

Abstract: Diesters of dianhydroglycitols can be prepared by esterification of dianhydroglycitols, anhydroglycitols and/or glycitols with alkylcarboxylic or arylcarboxylic acids in the presence of an acid catalyst, the acid catalyst being a macroporous acid ion exchange resin. If glycitols or monoanhydroglycitols are used as the starting material, the reaction temperature is initially of the order of 120° C. and after the dehydration is approximately 140° C.

Abstract: Provided are a novel triphenyl phosphine derivative synthesized from a triphenylphosphine and a hydroxy-containing lactone; a palladium and a nickel complexes comprising the derivative as a ligand; and a process for preparing a biaryl derivative using the complex as a catalyst. A product can be easily separated from a catalyst or a phosphorus compound, and biaryl derivative can be synthesized in a higher yield, by using the complex of the present invention as a catalyst.

Abstract: This invention provides a process for preparing sodium ferric gluconate complex in sucrose using the following steps: a) combining a ferric salt solution with a weak alkali chosen from the group consisting of alkaline earth metal and ammonium salts, such as sodium carbonate, sodium bicarbonate, lithium carbonate, potassium carbonate, potassium bicarbonate, ammonium carbonate, ammonium bicarbonate and mixtures thereof, to form the ferric oxyhydroxide; b) combining ferric oxyhydroxide and sodium gluconate in solution to yield the sodium ferric gluconate complex; c) isolating the sodium ferric gluconate complex; and d) combining the sodium ferric gluconate with sucrose in solution to yield the desired sodium ferric gluconate complex in sucrose.

Abstract: The invention relates to tris-(oxalato)phosphates of the general formula M[P(C2O4)3] wherein M=H, a metal or N(R1R2R3R4), where R1, R2, R3, R4, are independently H or an alkyl group comprising 1 to 8 C atoms. The invention also relates to a method for preparing such compounds as well as to their use.

Abstract: The invention relates to a method of producing ethyl acetate by reaction of ethyl alcohol with acetic acid and/or acetic anhydride in the presence of a solid acidic catalyst accompanied by simultaneous distillation separation of reaction components, in which acetic acid or acetic anhydride or a mixture thereof and ethyl alcohol, respectively, are introduced separately in a molar ratio of 2:1 to 1:2.5 and in a defined quantity, per unit volume of catalyst, into a system separated into three zones, whereby, in the reaction zone, the reaction runs simultaneously with distillation separation of components, acetic acid feed is introduced into the reaction zone or above the zone and ethyl alcohol feed is introduced into the reaction zone or below this zone; in the upper separation zone, the volatile mixture is separated; thereafter, it is cooled to 5 to 70° C.

Abstract: The present invention relates to a 3-substituted-phenyl-3-merthylbutyric acid and 3-substituted-phenyl-3-merthylaldehyde derivatives, which are useful in the production of N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which is a sweetener with high sweetening potency.

Abstract: An improved process is described for the industrial preparation of L-carnitine or alkanoyl L-carnitine mucate, which allows operations in a homogeneous phase in conditions of greater dilution, in a normal chemical reactor with stirring, in a batch process.

Abstract: The present invention relates to calcium double salts having good preservative properties. Said salts can be used in foods, feeds, pet food, cosmetics and pharmaceuticals, food-contact items, silage, brewers' spent grains, pomace, food wastes, brewers' yeast, distillation residues and other wastes from the food industry or for leather treatment. These substances exhibit a considerably extended shelf life after addition of, or treatment with, one of the calcium double salts.