Abstract: The present invention relates to conjugates of a lipid, substrate peptide of an enzyme secreted from the cells of mammals, including humans, and a water-soluble polymer that can be used as colloidal carriers and the like of tissue-specific drug delivery systems, methods of producing these conjugates, peptide-water-soluble polymer conjugates optionally having protective groups that are useful as the intermediates of these conjugates, colloidal carriers made from these conjugates, and tissue-specific drug delivery systems that use these colloidal carriers.

Abstract: The invention provides isolated nucleic acid and amino acid sequences of hHAC3, antibodies to hHAC3, methods of detecting hHAC3, and methods of screening for modulators hyperpolarization-activated cation channels using biologically active hHAC3. The invention further provides, in a computer system, a method of screening for mutations of human HAC3 genes as well as a method for identifying a three-dimensional structure of human HAC3 polypeptides.

Abstract: A process is disclosed by which a polynucleotide is directly synthesized from the peptide or protein that it encodes without the need for sequencing (or sequence analysis) of the peptide or protein. Information contained in the sequence of the peptide or protein is directly coupled, by the process of reverse translation, to the synthesis of the polynucleotide. The usefulness of reverse translation is that it facilitates the amplification of information held in the amino acid sequence (the primary structure) of an unknown protein or peptide. Amplification is useful for, among other things, the identification and/or scientific investigation of the peptide or protein.

Abstract: DNA encoding human neuronal nicotinic acetylcholine receptor alpha and beta subunits, mammalian and amphibian cells containing said DNA, methods for producing alpha and beta subunits and recombinant (i.e., isolated or substantially pure) alpha subunits (specifically ?6) and beta subunits (specifically ?3) are provided. In addition, combinations of a plurality of subunits (i.e., one or more of ?1, ?2, ?3, ?4, ?5, ?6 and/or ?7 subunits in combination with one or more of ?3 subunits are provided.

Abstract: The present invention relates to a process for solubilizing keratins from a keratin containing starting material such as poultry feathers. The keratins are may be solubilized using a sulphide under alkaline conditions. In the process the cysteine residues of solubilized keratins and are partially modified, e.g. by alkylation. The conditions of solubilisation and partial modification are chosen such that the keratins are also partially hydrolyzed. The partially modified and partially hydrolyzed keratin may be used as stable dispersions e.g. for the production of films and coatings by casting.

Abstract: Novel zacrp3x2 polypeptides, polynucleotides encoding the polypeptides, and related compositions and methods are disclosed. Also disclosed are antibodies to the zacrp3x2 protein or fragments thereof.

Abstract: The present invention provides for the use of soluble forms of CD83 and nucleic acids encoding them for the treatment of diseases caused by the dysfunction or undesired function of a cellular immune response involving T cells. The invention moreover provides soluble CD83 molecules specifically suited for said purpose, antibodies against said specific soluble CD83 proteins and assay methods and kits comprising said antibodies.

Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a ?bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a ?bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a ?bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; and where part (T) is a —Y—L—Z— radical wherein number Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assay or as intermediates for the synthesis of other compound of pharmaceutical interest. A process for their preparation of these compounds in a combinatorial manner, is also disclosed.

Abstract: Novel modified hemoglobins comprising polyalkylene glycols and novel methods for making those hemoglobins are provided. One group of modified hemoglobins comprise polyalkylene glycols bonded to the hemoglobin with an amide linkage at Glu-43(?). Additional polyalkylene glycols can also be bonded to the Glu-22(?) and/or the Asp-47(?). These hemoglobins are made by a novel amidation procedure. A second group of modified hemoglobins comprise a polyalkylene glycol covalently bonded to the hemoglobin at the ?-amino of a Val-1(?) or a Val-1(?). Additional polyalkylene glycols can optionally be covalently bonded to a limited number of ?-amino groups. This second group of hemoglobins is made using a novel reductive alkylation procedure. A third group of modified hemoglobins comprise a polyalkylene glycol bonded to a thiol group of the hemoglobin through a phenylsuccinimido linkage, wherein no polyalkylene glycol is bonded to a Cys-93(?).

Abstract: Humanized and variant anti-VEGF antibodies and various uses therefor are disclosed. The anti-VEGF antibodies have strong binding affinities for VEGF; inhibit VEGF-induced proliferation of endothelial cells in vitro; and inhibit tumor growth in vivo.

Abstract: Isolated proteins, designated Cpa1 and Cpa49, and their corresponding amino acid and nucleic acid sequences are provided which are useful in the prevention and treatment of infection caused by group A streptococcal bacteria such as Streptococcus pyogenes. These proteins have been observed to bind to collagen, and thus methods are provided, such as by administration of the proteins or antibodies generated thereto, whereby streptococcal binding of collagen can be inhibited, and streptococcal infection can be greatly reduced. In addition, medical instruments can be treated using the collagen-binding proteins of the invention in order to reduce or eliminate the possibility of their becoming infected or further spreading the infection.

Abstract: The present invention encompasses protective monoclonal antibodies that bind to peptidoglycan of Gram-positive bacteria. The antibodies also bind to whole bacteria and enhance phagocytosis and killing of the bacteria in vitro and block nasal colonization by Gram-positive bacteria in vivo. The invention also provides human, humanized and chimeric antibodies. The invention also sets forth the heavy chain and light chain variable regions of an antibody within the invention.

Abstract: The invention provides a family of antibodies that specifically bind the human cell surface glycosphingolipid GD2. The antibodies comprise modified variable regions, more specially, modified framework regions, which reduce their immunogenicity when administered to a human. The antibodies may be coupled to a therapeutic agent and used in the treatment of cancer.

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 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: Compounds including haptens, intermediates, and immunogens that are useful in the production of antibodies specific for the methylenedioxy class of amphetamine derivatives are described. Antibodies specific for the methylenedioxy class of amphetamine derivatives, reagent kits containing antibodies specific for the methylenedioxy class of amphetamine derivatives, methods of producing antibodies specific for the methylenedioxy class of amphetamine derivatives, and methods of detecting analytes including members of the methylenedioxy class of amphetamine derivatives are also described.

Abstract: A method for purifying a desired heterologous polypeptide from microbial fermentation broth or homogenate in which it is produced and solubilized is described. This method involves adding to the broth or homogenate an effective amount of a solution of 6,9-diamino-2-ethoxyacridine lactate (ethacridine lactate) to precipitate host cell impurities under conditions wherein the majority of polypeptide remains soluble, and separating the desired polypeptide from the broth or homogenate. The broth or homogenate containing the ethacridine lactate and polypeptide is also disclosed.

Abstract: The present invention relates to dyes of formula (I) wherein R1 is C1–C12alkyl or —CnH2n—(OCH2CH2)m—OR3, n being a number from 2 to 8, m being a number from 0 to 4 and R3 being C1–C12alkyl, C6–C24aryl or C6–C24aralkyl, R2 is methyl, ethyl, n-propyl, n-butyl, 2-methoxyethyl or 2-ethoxyethyl, X is halogen and Y is hydrogen, chlorine or bromine, and to the process for the preparation thereof and to the use thereof in dyeing or printing semi-synthetic and especially synthetic hydrophobic fiber materials, more especially textile materials

Abstract: A first aspect of the present invention is an isolated nucleic acid encoding a phage abortive defense protein, the isolated nucleic acid selected from the group consisting of: (a) isolated nucleic acid having the sequence or coding sequence given in SEQ ID NO: 1 (by “coding sequence” is meant nucleotides 373 to 1668 therein); (b) isolated nucleic acid encoding a phage abortive defense protein and which hybridizes to an nucleic acid having the sequence or coding sequence given in SEQ ID NO: 1, and/or having a sequence at least 60, 70, 80, 90, 92 or 95 percent identical to the sequence or coding sequence given in SEQ ID NO: 1; and (c) isolated nucleic acid encoding a phage abortive defense protein encoded by an isolated nucleic acid of (a) or (b) above, but differing in sequence therefrom due to the degeneracy of the genetic code (e.g., a nucleic acid encoding the protein given in SEQ ID NO: 2).

Abstract: 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: The invention provides a novel reporter gene (mSEAP) capable of being expressed in a mammal for extended periods of time. Nucleic acids encoding the reporter gene, cells and vectors comprising the nucleic acids, and methods of using the reporter gene to identify expression vectors and screen for drug compounds in an animal are also disclosed.

Abstract: This invention provides prokaryotic glycosyltransferases, including a bifunctional sialyltransferase that has both an ?2,3- and an ?2,8-activity. A ?1,4-GalNAc transferase and a ?1,3-galactosyltransferase are also provided by the invention, as are other glycosyltransferases and enzymes involved in synthesis of lipooligosaccharide (LOS). The glycosyltransferases can be obtained from, for example, Campylobacter species, including C. jejuni. In additional embodiments, the invention provides nucleic acids that encode the glycosyltransferases, as well as expression vectors and host cells for expressing the glycosyltransferases.

Abstract: The present invention is directed to promoter sequences and promoter control elements, polynucleotide constructs comprising the promoters and control elements, and methods of identifying the promoters, control elements, or fragments thereof. The invention further relates to the use of the present promoters or promoter control elements to modulate transcript levels.

Abstract: A process of manufacturing oligonucleotides includes a 5?-deblocking step in which the 5-blocking group is removed with dichloroacetic acid that is essentially free of chloral. The process is useful for making oligonucleotides that are substantially free of chloral adducts.

Abstract: The invention refers to a new process for the production of purification of high purity plasmid DNA. The process comprehends: a) the production of cells containing plasmid DNA, b) the disruption of the cells in order to obtain a lysate containing plasmid DNA, c) a concentration step by precipitation with isopropanol, d) a pre-purification and conditioning step by the addition of ammonium sulphate, e) a purification step using hydrophobic interaction chromatography, f) a final concentration and/or buffer exchange step. The process is scaleable, it does not use enzymes or mutagenic agents and it enables the preparation of plasmid DNA with pharmaceutical grade, which complies with the requirements of regulatory agencies. The invention belongs to the technical domain of Biochemical Engineering/Biotechnology.

Abstract: Disclosed are methods and intermediates for the preparation of 7-(2?-R1-substituted-?-D-ribofuranosyl)-4-amino-5-(optionally substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine compounds. These compounds are useful in treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such 7-(2?-substituted-?-D-ribofuranosyl)-4-amino-5-(optionally substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine compounds are represented by Formula I as follows: wherein, each of R1, R2, and R3 are as defined herein.

Abstract: A process is described for preparing a substrate for the transglycosylase enzymes of bacterial cell wall biosynthesis. The chemical synthesis makes available a sustainable and substantially pure source of supply of lipid II, including analogs thereof, that may be used in the identification of new therapeutic agents capable of disrupting steps in bacterial cell wall biosynthesis.

Abstract: Methods for preparing phthalocyanine co-crystals are provided. The phthalocyanine co-crystals include titanyl phthalocyanines and metal free phthalocyanines.

Abstract: There is provided a process for the preparation of a compound of formula (I): which process comprises reaction of a compound of formula (II): with either a compound of formula (III): or acrylamide, followed, in the latter case, by reaction of the resulting intermediate of formula (IV): with an alcohol of formula R2—OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R2—OH, and wherein R1, R2 and R16 have meanings given in the description

Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.

Abstract: A process is described for preparing alkoxycarbonylaminotriazines by reacting di- or triaminotriazines with dimethyl carbonate in the presence of an alcohol and of an alkali metal or alkaline earth metal methoxide base.

Abstract: Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or dif

Abstract: This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.

Abstract: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.

Abstract: Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.

Abstract: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.

Abstract: The present invention relates to a novel diaryl 1,2,4-triazole derivative of the following formula (1) as a highly selective cyclooxygenase-2 inhibitor, wherein R1, R2, R3, R4, R5, W and A is as defined in this specification.

Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.

Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y1-Z1 ??(I) wherein X1 is optionally substituted aryl, optionally substituted heteroaryl or the like; Y1 is —NRACO—(CH2)0-2— or the like (wherein RA is hydrogen atom or the like); and Z1 is a cyclic group fused the same or different two ring selected from optionally substituted carbocyclic group and optionally substituted heterocyclic group.

Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.

Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.

Abstract: The present invention relates to dithiocarbamic esters, their preparation and their use for regulating the degree of polymerization during the polymerization of monomers, such as during the polymerization of chloroprene to give polychloroprene, and during the polymerization of 2,3-dichlorobutadiene to give poly-2,3-dichlorobutadiene, and during the copolymerization of chloroprene with 2,3-dichlorobutadiene. The present invention further relates to polymers which are obtainable via the polymerization of monomers in the presence of the dithiocarbamic esters of the invention. The present invention also relates to polymers which contain end groups derived from the dithiocarbamic esters of the present invention.

Abstract: The invention relates to a process for preparing enantiomerically enriched aryl-aminopropanols and to their use and also to intermediates.

Abstract: Novel linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye are provided. These linkers faciliate the efficient transfer of energy between a donor and acceptor dye in an energy transfer dye. One of these linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye has the general structure R21Z1C(O)R22R28 where R21 is a C1-5 alkyl attached to the donor dye, C(O) is a carbonyl group, Z1 is either NH, sulfur or oxygen, R22 is a substituent which includes an alkene, diene, alkyne, a five and six membered ring having at least one unsaturated bond or a fused ring structure which is attached to the carbonyl carbon, and R28 includes a functional group which attaches the linker to the acceptor dye.

Abstract: NST 400 compounds consisting of a unit for partial coordination of Ca2+ ions (CPCU). The NST 400 compounds are optionally conjugated to another pharmaceutically active compound. The compounds and conjugates can be used for affinity filters and for binding negative charged phospholipids. The compounds and conjugates can also be used for treating diseases involving changes of cell membrane asymmetry.

Abstract: A photochromic composition and a coating composition comprising a molecular compound of a chromene compound and an aromatic compound. The photochromic composition provides a photochromic optical material as a cured product and the coating composition is applied to a lens substrate and cured to provide a photochromic optical material. The above molecular compound is also provided.

Abstract: 1?-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type-2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.