Abstract: The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.

Abstract: A specific region of chromosome 10 (10q23.3) has been implicated by series of studies to contain a tumor suppressor gene involved in gliomas, as well as a number of other human cancers. One gene within this region was identified, and the corresponding coding region of the gene represents a novel 47 kD protein. A domain of this product has an exact match to the conserved catalytic domain of protein tyrosine phosphatases, indicating a possible functional role in phosphorylation events. Sequence analyses demonstrated the a number of exons of the gene were deleted in tumor cell lines used to define the 10q23.3 region, leading to the classification of this gene as a tumor suppressor. Further analyses have demonstrated the presence of a number of mutations in the gene in both glioma and prostate carcinoma cells. Methods for diagnosing and treating cancers related to this tumor suppressor, designated as TS10q23.3, also are disclosed.

Abstract: The present invention includes fully human, neutralizing, monoclonal antibodies against human Insulin-like Growth Factor Receptor-I (IGFR1). The antibodies are useful for treating or preventing cancer in a subject. Also included are methods of using and producing the antibodies of the invention.

Abstract: The present invention provides for a modified antibody of class IgG, in which at least one amino acid from the heavy chain constant region selected from the group consisting of amino acid residues 250, 314, and 428 is substituted with another amino acid which is different from that present in the unmodified antibody, thereby altering the binding affinity for FcRn and/or the serum half-life in comparison to the unmodified antibody.

Abstract: The present invention provides for a modified Fc-fusion protein in which at least one amino acid from the heavy chain constant region selected from the group consisting of amino acid residues 250, 314, and 428 is substituted with another amino acid which is different from that present in the unmodified Fc-fusion protein, thereby altering the binding affinity for FcRn and/or the serum half-life in comparison to the unmodified Fc-fusion protein.

Abstract: A novel gene (designated 85P1B3) and its encoded protein are described. While 85P1B3 exhibits tissue specific expression in normal adult tissue, it is aberrantly expressed in multiple cancers including set forth in Table 1. Consequently, 85P1B3 provides a diagnostic and/or therapeutic target for cancers. The 85P1B3 gene or fragment thereof, or its encoded protein or a fragment thereof, can be used to elicit an immune response.

Abstract: A cDNA encoding a novel LTC4 receptor has been isolated. Provision of the novel protein, an LTC4 receptor, enabled binding experiments using the LTC4. By screening for compounds that modulate LTC4 receptor activity based on these binding experiments, development of drugs targeting the LTC4 receptor becomes possible.

Abstract: DNA encoding core+1 polypeptides of hepatitis C virus (HCV), nucleotides encoding the polypeptides, and methods for using the nucleotides and the encoded polypeptides are disclosed.

Abstract: The invention provides a hapten, an immunogen comprising the hapten coupled to an antigenicity-conferring carrier material, a conjugate comprising the hapten coupled to a labelling agent, as well as, antibodies raised against the aforementioned immunogen and capable of binding with MDMA.

Abstract: The present invention relates to azo dyes of formula (1) which are soluble in organic solvents, wherein R1 is —CN, —COOR5, —CONR6R7 or a heterocyclic ring, R2 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl, —CF3, —COOR5, —CONR6R7 or —COR5, R3 is hydrogen, —SO3M, alkyl, alkoxy, alkylcarbonyl, —NO2 or halogen, R4 is substituted aryl, substituted heteroaryl or an aryl-N?N-aryl radical, wherein one or both of the aryl radicals in aryl-N?N-aryl is/are unsubstituted or substituted, or a radical heteroaryl-N?N-heteroaryl, wherein one or both of the heteroaryl radicals in heteroaryl-N?N-heteroaryl is/are unsubstituted or substituted, R5 is hydrogen, alkyl or unsubstituted or substituted aryl, R6 is hydrogen, alkyl or unsubstituted or substituted aryl, R7 is hydrogen, alkyl or unsubstituted or substituted aryl, M+ is a cation, n is a number 1, 2 or 3 and m is a number 1, 2 or 3, to a process for the preparation thereof and to the use thereof in the production of colored plastics or polymeric

Abstract: The present invention relates to articles, preferably disposable absorbent articles like sanitary napkins and pantiliners, which comprise a cationic polysaccharide, typically chitin-based material and/or chitosan material, and an acidic pH buffering means. Such disposable absorbent articles deliver improved odor control performance even upon prolonged wearing time of the articles.

Abstract: Bicyclonucleoside analogues which exhibit anti-AIDS activity and intermediates to produce oligonucleotide analogues which have anti-sense or anti-gene activity as well as in vivo stability. Compounds of the following formula (1) or their pharmaceutically acceptable salts. wherein R1 represents a hydrogen atom or a protecting group for a hydroxy group, R2 represents an azido group or an optionally protected amino group or the like, B represents a purin-9-yl or a 2-oxo-1,2-dihydropyrimidin-1-yl group, which are optionally substituted with substituents selected from the group consisting of a halogen atom, an alkyl group having 1–6 carbon atoms, a hydroxy group, a mercapto group and an amino group.

Abstract: The present invention relates to a novel gene, a novel protein encoded by said gene, a mutated form of the gene and to diagnostic and therapeutic uses of the gene or a mutated form thereof. More specifically, the present invention relates to a novel gene defective in autoimmune polyendocrinopathy syndrome type I (APS I), also called autoimmune polyendocrinopathy-candidiasis-ectodermal dystrophy (APECED) (MIM No. 240,300).

Abstract: The present invention relates to a group of novel viral RNA regulatory genes, here identified as “viral genomic address messenger genes” or “VGAM genes”, and as “genomic record” or “GR” genes. VGAM genes selectively inhibit translation of known host target genes, and are believed to represent a novel pervasive viral attack mechanism. GR genes encode an operon-like cluster of VGAM genes. VGAM and viral GR genes may therefore be useful in diagnosing, preventing and treating viral disease. Several nucleic acid molecules are provided respectively encoding several VGAM genes, as are vectors and probes, both comprising the nucleic acid molecules, and methods and systems for detecting VGAM genes, and for counteracting their activity.

Abstract: The RFRP-3 peptide of the present invention which is an agent for promoting prolactin secretion is useful as a prophylactic and/or therapeutic agent for various diseases associated with prolactin secretion, such as hypoovarianism, seminal vesicle hypoplasia, menopausal syndrome and hypothyroidism.

Abstract: Methods for making glycoproteins, both in vitro and in vivo, are provided. One method involves incorporating an unnatural amino acid into a protein and attaching one or more saccharide moieties to the unnatural amino acid. Another method involves incorporating an unnatural amino acid that includes a saccharide moiety into a protein. Proteins made by both methods can be further modified with additional sugars.

Abstract: This invention relates to methods and materials to produce hydroquinone glucoside in genetically modified green plants and microorganisms.

Abstract: Disclosed herein are novel nucleic acid and protein sequences that are essential to fertility. In particular, human Mater cDNA and protein sequences are provided. Functional MATER is required for female fertility; zygotes that arise from Mater null oocytes do not progress beyond the two-cell stage. Methods are described for using Mater molecules in diagnoses, prognosis, and treatment of infertility and reduced fertility. Also provided are methods for using MATER as a contraceptive agent. The disclosure also describes compounds involved in such methods, and the identification of such compounds.

Abstract: In this application is described a protective DNA vaccines against infection with HFRS- and HPS-associated hantaviruses. The vaccines were constructed by subcloning cDNA representing the medium (M) (encoding the G1 and G2 glycoproteins) into the DNA expression vector pWRG7077. Animals vaccinated with the M construct developed a neutralizing antibody response. Passive transfer experiments show that serum from vaccinated animals, when injected on days 4 or 5 after challenge, protected animals from lethal disease.

Abstract: The present invention provides a labeled nucleoside having formula: where X represents an aliphatic diamine, and the labeling moiety comprises a label and a spacer, where the spacer is coupled at one end to a platinum atom and at the other end to the label, which spacer comprises a chain having at least four carbon atoms and at least one oxygen atom in the chain. The invention further provides a method for labeling a nucleoside, kits for labeling a nucleoside, and kits for producing a labeled nucleic acid.

Abstract: Provided are methods of producing phosphitylated compounds, including 3?-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula II wherein R3, R4, R5, R6, and R7 are independently hydrogen, C1–C10 alkyl, C3–C10 cycloalkyl, C6–C10 aryl, C7–C10 aralkyl, C1–C10 heteroalkyl, or C1–C10 heteroaryl, and at least one of R3, R4, R5, R6, and R7 is not hydrogen; (2) zwitterionic amine complexes; and (3) combinations of two or more thereof, to produce a phosphitylated compound. Further provided are methods for purifying phosphitylated compounds comprising the steps of providing a phosphitylated compound in a solution solvent, contacting said phosphitylated compound with a precipitation solvent, and precipitating said phosphitylated compound.

Abstract: Various 2?-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.

Abstract: The present invention relates to monocotyledon plant cells and plants which are genetically modified, wherein the genetic modification consists of the introduction of an extraneous nucleic acid molecule which codes for a protein with the biological activity of an R1 protein. The present invention further relates to means and methods for the production thereof. Plant cells and plants of this type synthesise a modified starch, which is characterised in that it has an increased phosphate content and/or a modified phoshorylation pattern and/or an increased final viscosity in an RVA profile and/or a reduced peak temperature in DSC analysis and/or an increased gel strength in the texture analysis compared with starch from corresponding non-genetically modified monocotyledon plants. Therefore, the present invention also relates to the starch which is synthesised from the plant cells and plants according to the invention, and to methods of producing said starch.

Abstract: A material containing agarobiose; a method for preparing the material; and a food, a drink or a seasoning using the material, which is tasty and has the effect of alleviating a stimulant taste and of enhancing the depth of sweetness.

Abstract: A process for removing high boilers from crude caprolactam which comprises high boilers, caprolactam and in some cases low boilers, and which has been obtained by a) reacting 6-aminocapronitrile with water to give a reaction mixture b) removing ammonia and unconverted water from the reaction mixture to obtain crude caprolactam, which comprises c) feeding the crude caprolactam to a distillation apparatus to obtain a first substream via the top as a product and a second substream via the bottom, by setting the pressure in the distillation in such a way that the bottom temperature does not go below 170° C., and adjusting the second substream in such a way that the caprolactam content of the second substream is not less than 10% by weight, based on the entire second substream.

Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

Abstract: The invention relates to the use of enaminotriazines of the formula I in which the radicals Y, independently of one another, are hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms, the radicals X are identical or different, where at least one of the radicals X is the ethenyl radical of the formula II and X may also have the meanings of Y, and where in the formula II the radicals R are identical or different and are cyano, optionally esterified carboxyl, substituted carbonyl, optionally substituted aminocarbonyl, optionally esterified sulfo, substituted sulfonyl or optionally esterified phosphono, and where two adjacent radicals R may optionally form a ring and the radicals R? are identical or different and are hydrogen, an optionally substituted aliphatic, cycloaliphatic or aromatic radical having in each case up to 18 carbon atoms, as UV filters in cosmetic or pharmaceutical preparations for protecting human skin o

Abstract: Cosmetic/dermatological sunscreen compositions, suited for photoprotecting, e.g., the skin, lips, scalp and/or hair against the damaging effects of UV-radiation, contain thus effective amounts of at least one novel s-triazine compound tri-substituted with para-aminobenzalmalonate substituents.

Abstract: A process for making cabergoline uses silyl-protecting agents to protect the indole nitrogen atom.

Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.

Abstract: The present invention is directed to a method for preparing a 4,7-bis(5-halothien-2-yl)-2,1,3-benzothiadiazole, more particularly, 4,7-bis(5-bromothien-2-yl)-2,1,3-benzothiadiazole, and a precursor therefor, namely, a 4,7-bis(thien-2-yl)-2,1,3-benzothiadiazole. The precursor is prepared by contacting in the presence of a palladium catalyst and a solvent a 4,7-dihalo-2,1,3-benzothiadiazole with a thienyl group adding reagent, which can either be a 2-thienylzinc halide, a 2-thienylmagnesium halide, or a 2-thiopheneboronic acid, under such conditions as to form 4,7-bis(thien-2-yl)-2,1,3-benzothiadiazole. The precursor can then be halogenated, preferably brominated, to form the desired dibrominated product, which is a particularly suitable monomer for the preparation of a copolymer of a 9,9-disubstituted fluorene. This copolymer is useful, for example, in polymeric light emitting diode (pLED) applications.

Abstract: Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4?-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing ?-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-?-ethyl-2-oxo-1-pyrrolidine acetamide.

Abstract: The present invention relates to halogen-containing aromatic compounds and methods thereof. The present invention relates a halogen-containing aromatic acid dianhydride, halogen-containing aromatic tetranitrile compound, halogen-containing m-phenylenediamine compound and fluorine compound, and a method thereof.

Abstract: Phosphinines of formula (I) can be combined with metal salts to prepare hydroformylation catalysts. The phosphinine complexes have two phosphorus centers that may be substituted with a variety of hetero atoms or alkyl substituents to modify the ligand characteristics of the phosphinine. Phosphinine metal complexes are employed under normal hydroformylation reaction conditions. The preparatory routes to the phosphinine ligands of formula (I) allow for their convenient synthesis.

Abstract: Zinc acrylate excelling in flowability is provided. It is produced by a method, characterized by dispersing zinc oxide in any of (a) an aliphatic hydrocarbon solvent, (b) a mixed solvent formed between an aliphatic hydrocarbon solvent and an aromatic hydrocarbon solvent, and (c) a mixed solvent formed between an aromatic hydrocarbon solvent and an alcohol and causing acrylic acid to react with said zinc oxide in said solvent. The obtained zinc acrylate refrains from undergoing secondary aggregation, excels in disintegrability and, when kneaded in a rubber composition, exhibits excellent dispersibility.

Abstract: A compound of the formula (1): wherein PCA represents a polycycloaliphatic hydrocarbon group, ALK represents a divalent aliphatic hydrocarbon group, m is 1 or 2, n is 0 or 1, and R1 and R2 represent independently each other an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an aryl group or an aryloxy group.

Abstract: An insecticide of formula 1 and the agriculturally acceptable salts thereof, wherein: R1 is selected from the group consisting of: the group OR5 wherein R5 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclic and substituted heterocyclic; the group —NR6OH wherein R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, carbocyclic and substituted carbocyclic; the group NR7R8 wherein R7 and R8 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl and carbocyclic; and the group wherein R1 is linked to R2 to form a diradical bridging group; R2 and R3 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, carbocyclic, substituted carbocyclic, aryl, substituted aryl, acyl and substituted acyl; and A is a diradical linking group which has a molecular weight of preferably

Abstract: The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

Abstract: Compounds of formula (I) or a salt or solvate thereof, wherein: x represents 0 or 1; y represents 0 or 1; R1 and R2 independently represent —C1-9 alkyleneC1-6 fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms and wherein the R1 and/or R2 moiety is optionally interrupted by an ether link, processes for their preparation, use of the compounds in the preparation of pharmaceutical formulations and the formulations are described.

Abstract: The invention relates to a novel process for preparing salts of S-alkyl esters of thiosulphuric acid by reacting organic dihalides with thiosulphates in water.

Abstract: The present invention relates to a method of producing a compound represented by the formula [I] or a salt thereof, which comprises reacting a compound represented by the formula [II] or a salt thereof with a compound represented by the formula [III] or a salt thereof, in the presence of a base, in alcohol, and provides a production method of an O-substituted tyrosine compound, which is superior in productivity, versatility and safety, and economically and industrially useful: wherein each symbol is as defined in the specification.

Abstract: A method for producing (meth)acrolein and/or (meth)acrylic acid by subjecting isobutylene and the like or propylene to a vapor-phase catalytic oxidation with molecular oxygen in the presence of a solid oxidation catalyst in a tubular type of fixed bed reactor, wherein a temperature of a hot-spot zone is sufficiently controlled and (meth)acrolein and (meth)acrylic acid are produced with a high yield. A method for producing (meth)acrolein and/or (meth)acrylic acid by passing a raw material gas comprising isobutylene and the like or propylene and oxygen through a catalyst layer in a tubular type of fixed bed reactor which is filled with a solid oxidation catalyst, which includes passing a gas containing isobutylene and the like or propylene in a concentration lower than that of the raw material gas, and oxygen through the catalyst layer for a period of one hour or more prior to passing the raw material gas through the catalyst layer.

Abstract: A free organic acid can be produced efficiently at a low cost, by subjecting an ammonium salt of organic acid A such as a dicarboxylic acid, a tricarboxylic acid or an amino acid, to reactive crystallization with an acid B, such as a monocarboxylic acid, wherein organic acid A and acid B satisfy the following formula (1): pKa(A)?pKa(B)??(1) where pKa(A) and pKa(B) represent ionization indices of organic acid A and acid B, respectively, provided that when they have plural values, they represent the minimum pKa among them, to separate free organic acid A in solid form.

Abstract: The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: A method of producing a near-infrared absorbing dye compound, useful for image forming materials, infrared heat-sensitive recording devices, optical film materials, and the like, containing a process of reacting a compound represented by formula (I) with halogenating agent. wherein R111, R112, R121, R122, R131, R132, R141 and R142 each independently represent a hydrogen atom, an aliphatic group or an aromatic group; R103, R113, R123, R133 and R143 each independently represent a substituent; and n103, n113, n123, n133 and n143 each independently denote an integer from 0 to 4.

Abstract: The invention concerns a method for method for preparing 1,3,5-triaminobenzene, characterized in that it comprises a step which consists in amination of a compound of formula (I), wherein: A represents a halogen atom or a NH2 group; X1 and X2, identical or different, represent each a halogen atom, the amination step being carried out in the presence of ammonia and a catalyst selected from the group consisting of copper salts, cupric and cuprous oxides or mixtures thereof at a temperature ranging between 150° C. and 250° C.

Abstract: Elastomers which have excellent stability to prevent oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation comprise, as stabilizers, at least one compound of the formula I [R—S(?O)m—CH2—CH(OH)—CH2]n—N(R1)2-n—R2, ??(I) in which R is C4–C20alkyl, hydroxyl-substituted C4–C20alkyl; phenyl, benzyl, ?-methylbenzyl, ?,?-dimethylbenzyl, cyclohexyl or —(CH2)qCOOR3, and, if m is 0, R may additionally be and, if n is 1 and R4 is hydrogen, R may additionally be R2—R1N—CH2—CH(OH)—CH2—S(?O)m—(CH2)x— or R2—R1N—CH2—CH(OH)—CH2—S(?O)m—CH2—CH2—(O—CH2—CH2)y—, R1 is hydrogen, cyclohexyl or C3–C12alkyl, R2 is R3 is C1-C18alkyl, R4 is hydrogen or —CH2—CH(OH)—CH2—S(?O)m—R, X is C1–C8alkyl, Y is C1–C8alkyl, m is 0 or 1, n is 1 or 2, q is 1 or 2, x is from 2 to 6, and y is 1 or 2. The compounds of the formula I are also suitable as stabilizers for elastomers to prevent contact discoloration of substrates coming into contact with elastomers.

Abstract: The invention concerns novel catalysts for aromatic nucleophilic substitution. Said catalysts are compounds of the general formula (I), wherein: R1, R2, R3, R4, R5, and R6, identical or different, are selected among hydrocarbon radicals; the Pn's, advantageously the same, are selected among metalloid elements of column V of a period higher than nitrogen; Z is a metalloid element of column V, advantageously distinct from Pn; preferably a nitrogen (N, P, As, Sb).

Abstract: A process for selectively making 2-thiols from alpha olefins is described. The process includes contacting a linear or branched alpha olefin having with H2S in the presence of a catalyst and recovering the 2-thiol from a product mixture. The catalyst includes a support and at least one metal selected from Group IIIA-VIIIA and the branched olefin is branched at the 3-position or higher with respect to the olefin double bond. Compositions wherein the 2-thiols are substantially free of 1-thiol and 3-thiol isomers are also described.