Abstract: The invention provides cytokine fusion proteins with an increased therapeutic index, and methods to increase the therapeutic index of such fusion proteins. The fusion proteins of the invention are able to bind to more than one type of cytokine receptor expressed on cells and also bind to more than one cell type. In addition, the fusion proteins of the invention exhibit a longer circulating half-life in a patient's body than the corresponding naturally occurring cytokine.

Abstract: The polypeptides, and the polynucleotides encoding for them, described herein are IL-21 antagonists that bind with specificity and exhibit an EC50 that is not detectable in receptor binding studies. These molecules have mutations in the D helix of the IL-21 molecule, and can be used to inhibit the activity of IL-21 with its cognate receptor.

Abstract: The present invention relates to a process for preparing regenerated collagen fiber which comprises treating regenerated collagen fiber with a monofunctional epoxy compound and a metal aluminum salt, in which treatment with the monofunctional epoxy compound initiated by adding sodium hydroxide to become 0.001 to 0.8 N based on the treatment solution and inorganic salt in an amount so that water absorption of the obtained regenerated collagen fiber becomes at most 100%, depending on amount of sodium hydroxide added. Also, the present invention relates to a process for setting regenerated collagen fiber obtained by the above process which comprises thermally setting the fiber by means of wet heat treatment at 50° to 160° C. and drying treatment at 20° to 220° C.

Abstract: The present invention relates to a process for extracting and refining the components of pea flour, characterized in that it consists of the steps of preparing a flour by grinding dried peas previously cleaned, sorted, blanched, freed of dust, introducing the flour thus obtained into water and separating the components of the pea flour using at least one of the pieces of equipment from a potato starch factory chosen from the group consisting of hydrocyclones, centrifugal decanters and sieves, without a stage for separating the internal fibers of the pea being carried out beforehand, devices comprising at least one of these pieces of equipment, and to a particular quality of pea starch thus extracted.

Abstract: The present invention relates to a method for producing patient cancerous disease modifying antibodies using a novel paradigm of screening. By segregating the anti-cancer antibodies using cancer cell cytotoxicity as an end point, the process makes possible the production of anti-cancer antibodies for therapeutic and diagnostic purposes. The antibodies can be used in aid of staging and diagnosis of a cancer, and can be used to treat primary tumors and tumor metastases. The anti-cancer antibodies can be conjugated to toxins, enzymes, radioactive compounds, and hematogenous cells.

Abstract: Methods for treating medical conditions induced by interleukin-4 involve administering an IL-4 antagonist to a patient afflicted with such a condition. Suitable IL-4 antagonists include, but are not limited to, IL-4 receptors (such as a soluble human IL-4 receptor), antibodies that bind IL-4, antibodies that bind IL-4R, IL-4 muteins that bind to IL-4R but do not induce a biological response, molecules that inhibit IL-4-induced signal transduction, and other compounds that inhibit a biological effect that results from the binding of IL-4 to a cell surface IL-4R. Particular antibodies provided herein include human monoclonal antibodies generated by procedures involving immunization of transgenic mice. Such human antibodies may be raised against human IL-4 receptor. Certain of the antibodies inhibit both IL-4-induced and IL-13-induced biological activities.

Abstract: The present invention concerns fusion of Fc domains with biologically active peptides and a process for preparing pharmaceutical agents using biologically active peptides. In this invention, pharmacologically active compounds are prepared by a process comprising: a) selecting at least one peptide that modulates the activity of a protein of interest; and b) preparing a pharmacologic agent comprising an Fc domain covalently linked to at least one amino acid of the selected peptide. Linkage to the vehicle increases the half-life of the peptide, which otherwise would be quickly degraded in vivo. The preferred vehicle is an Fc domain. The peptide is preferably selected by phage display, E. coli display, ribosome display, RNA-peptide screening, or chemical-peptide screening.

Abstract: The present invention is related to an osteogenic device and its preparation. Said device comprises a bone morphogenetic protein (BMP), preferably a modified BMP complex obtainable by a modification of the conventional guanidum hydrochloride extraction method and collagens, preferably collagen I or collagen IV, impregnated in and/or adsorbed on a bioceramic carrier, preferably a shapable body (block) originating from a coral skeleton. The method of isolating said modified BMP complex which lacks an immunogenic component and consists essentially of a 100–700 kD and a 15–25 kD protein with osteoinductive properties and preferably of the 15–25 kD protein which has improved storage properties as well as its use in the osteogenic device with improved osteoinductive properties is also disclosed.

Abstract: The present invention provides amino acid sequences of peptides that are encoded by genes within the Human genome, the GPCR peptides of the present invention. The present invention specifically provides isolated peptide and nucleic acid molecules, methods of identifying orthologs and paralogs of the GPCR peptides and methods of identifying modulators of the GPCR peptides.

Abstract: Biomolecules are provided having multiple binding sites for attachment to a substrate surface. The multiple attachment sites may be produced directly on the biomolecule or through use of branched phosphoramidite moieties that can be added in multiple to form dendritic structures which can in turn provide attachment sites for substrate binding moieties. Substrate binding moieties may include noncovalent binding moieties. For covalent binding moieties oligonucleotides containing hydrazides are provided. These hydrazides can be introduced via protected building blocks such as phosphoramidites or via building blocks containing precursor forms of such hydrazides.

Abstract: The invention provides nanoparticle-bioconjugate probes that are useful for detecting target analytes such as nucleic acids. The probes of the invention are stable towards heat and resistant to displacement by thiol containing compounds such as DTT (dithiothreitol).

Abstract: A method of identifying nucleotide sequences coding for signal peptides in lactic acid bacteria, using a DNA molecule comprising a transposon including a promoterless reporter gene from which DNA molecule a region between the LR and the reporter gene is deleted and the DNA molecule comprises a DNA sequence coding for a secretion reporter molecule. By deleting the region between the LR and the reporter gene, stop codons in-frame with the secretion reporter molecule is removed which upon transposition permits translational fusions from upstream the LR.

Abstract: The invention generally provides a novel approach to identifying Enterococcal virulence factors and for identifying compounds for treating bacterial pathogenesis. The invention further provides Enterococcal virulence factors, which serve as targets for drug discovery.

Abstract: The present invention relates to isolated polypeptides having phytase activity, recombinant DNA sequences encoding such polypeptides, methods of producing such polypeptides, and the use of the polypeptides in transgenic plants. The invention discloses polypeptides having affinity for the substrate phytate (1, 2, 3, 4, 5, 6 myo-inositol-hexakisphosphate, phytic acid), comprising an amino acid sequence as described by the invention. Furthermore, the invention discloses DNA fragments encoding the polypeptides, and cDNA fragments encoding the polypeptides. The polypeptides of the invention may, for example, be used as an additive in animal feeds, an additive in food for human consumption, or to extract proteins from rice bran. The invention also concerns a transgenic plant or part thereof, wherein the plant or part thereof has been genetically modified to comprise a polypeptide as defined by the invention.

Abstract: Isolated receptors, nucleic acids encoding such receptors, and pharmaceutical compositions made therefrom, are disclosed. The isolated receptors can be used to regulate an immune response. The receptors are also useful in screening for inhibitors or agonists thereof.

Abstract: The inventive subject matter relates to a glutamate receptor, DNA which encodes the receptor, a transformed cell expressing the receptor, a method for producing the receptor, a method for identifying an agonist, antagonist, or allosteric modulator for glutamic acid, a method for identifying an agonist for glutamic acid, an antibody to the receptor, and processes for making glutamate receptor modulators and pharmaceutical compositions comprising said modulator.

Abstract: There is disclosed antibody molecules containing at least one CDR derived from a mouse monoclonal antibody having specificity for human TNF?. There is also disclosed a CDR grafted antibody wherein at least one of the CDRs is a hybrid CDR. Further disclosed are DNA sequences encoding the chains of the antibody molecules, vectors, transformed host cells and uses of the antibody molecules in the treatment of diseases mediated by TNF?.

Abstract: The present invention provides DNA having the promoter activity of an OsSUT1 gene, as well as a transgenic plant and others capable of expressing a desired foreign gene specifically in the vascular bundle or the phloem thereof, using the above DNA as a promoter. According to the present invention, DNA having the promoter activity of the OsSUT1 gene was isolated from the genomic library of rice (Oryza sativa L.) The DNA has a promoter sequence, which has a phloem specificity and a growing time specificity and exists in a nucleotide sequence shown in SEQ ID NO: 1. A transgenic plant expressing a foreign gene specifically in the phloem or in the vascular bundle system tissues was produced by ligating the desired foreign gene downstream of the promoter DNA and incorporating it into the genome of a plant.

Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.

Abstract: A cationic starch product, the making of it and its use. The starch product comprises starch (St) and a cationising reagent, which is made from choline or its synthetic equivalent, whereby the cationising reagent has reacted with a part of the hydroxyl groups of the starch according to the structure formula (VI) or (VII). The structure component A is a hydrocarbon chain. The substituents R are hydrogens; lower or higher acrylic alkly groups, substituted or unsubstituted cycloalklyl groups; substituted or unsubstituted aryl or heteroaryl groups; lower or higher alkyl groups or non-aromatic heterocyclic groups containing alkoxy groups or other hetero atoms.

Abstract: A reduction inhibitory agent for active-oxygen eliminating activity comprises trehalose as an effective ingredient. A method for inhibiting the reduction of active-oxygen eliminating activity comprises incorporating either trehalose or the reduction inhibitory agent into plant edible products and/or plant antioxidants. A composition is provided that reduces the active-oxygen eliminating activity of plant edible products and/or plant antioxidants.

Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA— in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M–M? moiety

Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:

Abstract: A method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, includes a cyclization step which consists in a reaction between the primary or secondary amine function and the carbamic acid function of the carbamic acid derivative(s).

Abstract: The invention relates to novel heterocyclic enaminones of the general formula (I) in which Ar, Z, K, X, Y1, Y2, Y3, Y4, Y5, Y6 and V are as defined in the description, to their use as herbicides, acaricides and insecticides, and to processes for their preparation.

Abstract: The present invention relates to tricyclic 2-pyrimidone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.

Abstract: This invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3, R4and X have the meanings given in the disclosure, to a plurality of processes for preparing these novel substances, and to their use for controlling unwanted microorganisms. This invention further relates to novel intermediates of the formulae and processes for their preparation and additionally relates to novel amines and carbamates of the formulae given in the disclosure and processes for their preparation.

Abstract: The present invention relates to substituted imidazopyrazines of the general Formula I which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.

Abstract: The invention relates to novel substituted iminoazines of the general formula (I) in which R1, R2, R3, R4, Z1, Z2 and Z3 are each as defined in the disclosure, to a plurality of processes for their preparation, and to their use as herbicides.

Abstract: The composition relates to amino-imine compounds used in the formation of 1,3-diimine copper complexes for deposition of copper films.

Abstract: A compound having the formula I: and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds and compositions for use in therapy.

Abstract: The present invention discloses a method for preparing cabergoline form I by combining cabergoline and a solvent comprising ethylbenzene to form a solvate and obtaining form I from the solvate. Also disclosed in a method for preparing cabergoline form I by combining cabergoline and a first solvent to form a solution and additionally including a second solvent to the solution, followed by crystallization to form cabergoline form I. Further disclosed is a solvate form of cabergoline comprising cabergoline and ethylbenzene and, optionally, n-heptane.

Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

Abstract: A process for extracting from aqueous solution the alkali metal or calcium salt of a halo or haloalkyl substituted 2-hydroxypyridine, or a 2-hydroxyquinoline or 2-hydroxybenzothiazole which comprises contacting an aqueous alkaline or neutral solution of the alkali metal or calcium salt, in which is dissolved an alkali metal fluoride, chloride, bromide, hydroxide, sulphate, sulphite, cyanate, cyanide, thiocyanate, thiosulphate, sulphide, phosphate, hydrogen phosphate, carbonate, bicarbonate, borate, chlorate, hypochlorite, perchlorate, nitrite, chromate, dichromate or permanganate or calcium chloride, bromide, nitrate, nitrite, chlorate, hypochlorite, perchlorate, thiocyanate, thiosulphate, chromate, dichtromate or permanganate, with a partially water-miscible organic solvent so as to transfer aqueous solution of the alkali metal or calcium salt of the 2-hydroxypyridine, 2-hydroxyquinoline or 2-hydroxybenzothiasole into the solvent whilst retaining separate aqueous and solvent phases, and thereafter separating

Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a CH2, CH(OH), C(O), C?NOR4, NR5, O, S, S(O), or S(O)2, and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.

Abstract: The present invention discloses a novel, stable polymorph of 1-benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl] methyl piperidine hydrochloride commonly known as Donepezil hydrochloride. Further the present invention discloses a process for producing Donepezil HCl amorphous and its polymorph Form (VI).

Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.

Abstract: A method for producing a cyclic carbamate ester produces the cyclic carbamate ester by reacting an organic compound having at least two halogen atoms per molecule, an amine having at least two hydrogen atoms on a nitrogen atom, and carbon dioxide.

Abstract: Dispersion of filler(s) in polymeric compositions are improved by the use of a polymer-filler coupling compound, Q—A—B, wherein Q comprises a dipolar nitrogen-containing moiety that can form a 1,3 dipolar addition to an unsaturated carbon-carbon bond; B is an oxazoline, thiazoline, alkoxysilane or allyltin moiety, and A is a linking atom or group that forms a bridge between Q and B.

Abstract: A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure wherein is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.

Abstract: The present invention relates to a process for the direct preparation of pyrrolo[3,4-c]pyrroles (DPPs) of the formula (1), pigment compositions containing them and their use for coloring high molecluar weight organic materials, such as plastics and paints. The obtained DPPs of the formula I posses a higher color strength, a higher chroma, a purer shade and a higher opacity versus corresponding commerically available DPPs.

Abstract: The invention relates to new crystalline forms I and II of (4R-cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluoro-phenyl)-5-(1- methyl-ethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester of the Formula (I) and a process for the preparation thereof.

Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: The present invention relates to a process for the production of compound (A) comprising reacting compound (B) with compound (C). A further ring closure reaction may be necessary. The invention further relates to certain novel compounds of formula (B).

Abstract: A process for synthesizing a C-7 protected baccatin III compound represented by formula (A), which comprises reacting a 10-deacetylbaccatin III compound represented by formula (B) with a protecting agent and an acylating agent in the presence of a secondary amine and a nitrogen-containing compound. Also, a process for synthesizing a C-7 protected 10-deacetylbaccatin III compound represented by formula (C), which comprises reacting a 10-deacetylbaccatin III compound represented by formula (B) with a protecting agent in the presence of a secondary amine and a nitrogen-containing compound. In both processes the nitrogen-containing compound is selected from a nitrogen-containing heterocycle or a trialkylamine. When the nitrogen-containing heterocycle is selected, it may be an unsubstituted or a substituted pyridine or an unsubstituted or a substituted pyrazine. When a trialkylamine is selected, it may be, for example, triethylamine or diisopropylethylamine.

Abstract: Novel dimethyl amidopropyl amines prepared by the reaction of dimethyl amidopropyl amine (DMAPA) and shea butter, preferably mild-processed shea butter (MPSB). Materials of the present invention are useful as cosmetic and personal care ingredients, allowing for the delivery of highly desirable active ingredients present in shea butter including natural antioxidants, in a cationic material that is substantive to the skin and hair.

Abstract: The invention relates to phosphites comprising substituted or unsubstituted tricyclodecylmethyl groups. The phosphites may also contain substituted and unsubstituted alcohols having about C6–C18 carbon atoms. The alcohol chain may be aliphatic, arylakyl and alkylaryl groups. The method of making of the phosphite composition is also described.