Abstract: Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: wherein R1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C.

Abstract: Methods and compositions for the generation of polypeptides having varied material properties are disclosed herein. Methods include means for making self assembling amphiphilic block copolypeptides and related protocols adding oligo(ethyleneglycol) functionalized aninoacid-N-carboxyanhydrides (NCAs) to polyaminoacid chains. Additional methods include means of adding an end group to the carboxy terminus of a polyaminoacid chain by reacting an alloc-protected amino acid amide with a transition metal-donor ligand complex, thereby forming an amido-amidate metallacycle for use in further polymerization reactions. Novel compositions for use in peptide synthesis and design including five and six membered amido-containing metallacycles and block copolypeptides are also disclosed.

Abstract: Isolated polynucleotides encoding novel polypeptides which are capable of binding to native and methylated LDL (low density lipoprotein), the isolated polypeptides, called LBPs (LDL binding proteins), and biologically active fragments and analogs thereof, are described. Also described are methods for determining if an animal is at risk for atherosclerosis, methods for evaluating an agent for use in treating atherosclerosis, methods for treating atherosclerosis, and methods for treating a cell having an abnormality in structure or metabolism of LBP. Pharmaceutical compositions and vaccine compositions are also provided.

Abstract: A method of measuring translocation of a protein in cells from an intracellular location to a plasma membrane or from the plasma membrane to an intracellular location, with particular reference to GLUT4 and modified GLUT4 useful in the method.

Abstract: The present invention includes biodegradable plant protein composites.

Abstract: Antibody variants of parent antibodies are disclosed which have one or more amino acids inserted in a hypervariable region of the parent antibody and a binding affinity for a target antigen which is at least about two fold stronger than the binding affinity of the parent antibody for the antigen.

Abstract: CDR-grafted antibody heavy and light chains comprise acceptor framework and donor antigen binding regions, the heavy chains comprising donor residues at at least one of positions (6, 23) and/or (24, 48) and/or (49, 71) and/or (73, 75) and/or (76) and/or (78) and (88) and/or (91). The CDR-grafted light chains comprise donor residues at at least one of positions (1) and/or (3) and (46) and/or (47) or at at least one of positions (46, 48, 58) and (71). The CDR-grafted antibodies are preferably humanized antibodies, having non human, e.g. rodent, donor and human acceptor frameworks, and may be used for in vivo therapy and diagnosis. A generally applicable protocol is disclosed for obtaining CDR-grafted antibodies.

Abstract: Provided are novel DT- and ETA-based immunotoxins and a method of treating an immune system disorder not involving T cell proliferation, comprising administering to the animal an immunotoxin comprising a mutant diphtheria toxin moiety linked to an antibody moiety which routes by the anti-CD3 pathway, or derivatives thereof under conditions such that the disorder is treated. Thus, the present method can treat graft-versus-host disease.

Abstract: A covalent conjugate of a 4′-hydroxyazobenzene-2-carboxylic acid derivative (HABA) and an avidin-type molecule, of the formula: wherein A is (CH2)n or —CH═CH—, wherein n is an integer from 0-10; B is (CH2)n wherein n is an integer from 2 to 10; m is zero or 1; and Av is the residue of an avidin-type molecule selected from the group comprising native egg-white avidin, recombinant avidin, deglycosylated avidins, bacterial streptavidin, recombinant streptavidin, truncated streptavidin and other derivatives of said avidin-type molecules. These HABAylated avidins are red colored in the quinone configuration and can be used in many applications in the avidin-biotin technology.

Abstract: A method of increasing recovery of active enzyme produced in a plant is provided where the enzyme requires a transitional metal cofactor for activation. The metal cofactor is supplied to the enzyme during plant development, during extraction, or after extraction. Recovery of active enzyme is also provided by incubating the extracted enzyme at a non-enzyme degrading temperature. Addition of a negative ion salt further improves active enzyme recovery. Optimum salt concentrations for recovery of laccase from plants using copper solutions is provided.

Abstract: The present invention provides a process for producing novel lignin derivatives, which comprises using a lignophenol derivative containing a diphenylpropane unit formed by binding a carbon atom at an ortho-position relative to a phenolic hydroxyl group of a phenol derivative to a carbon atom at a benzyl-position of a phenylpropane fundamental unit of lignin, and binding an oxygen atom of the hydroxyl group and a &bgr;-positional carbon atom under alkali conditions under which the hydroxyl group can dissociate, to obtain an arylcoumaran derivative containing an arylcoumaran unit in which a coumaran skeleton is bound to an aromatic ring of lignin.

Abstract: The objective of the present invention is to provide a high-purity trisazo compound with excellent light resistance that is useful as a coloring matter for a black aqueous ink for ink jet recording and the like. Thus, the present invention provides a trisazo compound represented by the formula: wherein A1 is a group represented by the formula —COOM or —SO3M, A2 is a hydrogen atom or a group represented by the formula —COOM or —SO3M, M is each independently a hydrogen atom, or onium, R is each independently a hydrogen atom, an alkyl group, an alkoxy group and the like, B is a residue of K acid, Nps is a residue of &ggr; acid, J acid, or RR acid.

Abstract: The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or cholesteryl esters in biological systems is presented. These compounds can serve as tools for competitive binding assays to discover and characterize other chemical agents useful as cholesterol absorption inhibitors. New compounds of the present invention are also highly efficacious inhibitors of cholesterol absorption.

Abstract: Disclosed are compositions and methods comprising a novel mammalian gene, designated MORC, that is expressed in male germ cells. Also disclosed are polynucleotide compositions comprising a MORC gene from human and murine sources, and polypeptides encoded by these nucleic acid sequences. Methods for preparing MORC polypeptides, transformed host cells, and antibodies reactive with MORC polypeptides are also provided. In certain embodiments, the invention describes methods for diagnosing and treating infertility or testicular cancer, as well as methods for identifying MORC-related polynucleotide and polypeptide compositions.

Abstract: The present invention provides a genomic DNA of Buchnera. That is, this invention provides genes derived from Buchnera sp., comprising DNA of the following (a) or (b); (a) a DNA selected from a group consisting of a DNA having a nucleotide sequence ranging from a start point to an end point as shown in Table 1 in a nucleotide sequence represented by SEQ ID NO:1, or a DNA complementary thereto, and (b) a DNA hybridizing to the DNA of (a) under stringent conditions and encoding a protein having a function same as that of the product expressed by the DNA.

Abstract: This invention relates to a class of checkpoint genes and their polypeptide products which control progression through the cell cycle in eukaryotic cells. In particular this invention relates to Schizosaccharomyces pombe rad3 gene, to its human homologue (ATR) and to their encoded proteins. The invention further relates to assay methods for selecting compounds which modulate the activity of the polypeptide products of these checkpoint genes and the use of the selected compounds in anticancer therapy.

Abstract: The present application relates to nucleic acids and polypeptides from Cenarchaeum symbiosum. Methods of making the polypeptides and antibodies against the polypeptides are also described.

Abstract: Methods for preparing purified oligonucleotides by treating a solution comprising an oligonucleotide with an aggregating agent and a precipitation enhancer under conditions sufficient to form an oligonucleotide aggregate and isolating the oligonucleotide aggregate to produce a purified oligonucleotide.

Abstract: The present invention relates to dextran whose boron content is reduced to a value less than 0.30 &mgr;g/g (dry basis) calculated on the basis of boron atom, a process for producing the same, and dextran with which a container is filled in a solution state. Dextran of the present invention is obtained by treating a boron-containing dextran with a lower alcohol, and said dextran has such a characteristic that deposition is inhibited or the deposition rate is drastically reduced when using it in the form of a solution. Therefore, an isotonic sodium chloride solution of said dextran is suitably used as substitute plasma or external perfusate in an operation.

Abstract: The invention concerns a method for preparing Laminaribiose comprising a step for glycoside binding between a donor and an acceptor of glycosyl. The invention is characterized in that the glycosyl donor is in pyranose form and corresponds to formula (II); the glycosyl acceptor is in furanose form and corresponds to formula (III); said binding step is performed in solution in an anhydrous organic solvent, at a temperature ranging between −80° C. and 40° C., for a time interval ranging between 1 minute and 8 hours, in the presence of a suitable promoter.

Abstract: Chitin is extracted from the shells of exoskeletal animals such as crab, shrimp, crayfish, and lobster, by a primarily physical process comprising the step of cutting the shells in a wet state to approximately uniform particles. The resultant mass is then diluted and mixed to form a pumpable slurry. The slurry is separated to remove most unwanted materials, after which the particle size of the concentrated chitinous residue is further reduced. The once-washed, finely-cut chitinous slurry is again separated, resulting in a chitin end product.

Abstract: This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.

Abstract: It is provided a method for preparing the pyrroloazepine derivatives, especially in optically active form useful as drugs, by low-priced and simple method and in industrial applicable scale, represented by the following formula (I): wherein Z represents optionally substituted phenyl group, which comprises; a process for the asymmetric reduction of ketone compound with metal hydride compound and alcohol compound in the presence of optically active cobalt complex catalyst, and a process for the purification of the resulting compound.

Abstract: This invention relates to a novel, efficient, economic and general-purpose process for isolating monophenolic-bisaryl triazine compounds from polyphenolic-triazines compounds and other impurities. More specifically, this invention relates to a process for isolating the monophenolic-bisaryl triazine compounds by contacting it with a base, an alcohol or a hydrocarbon solvent.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino[1,2-b]quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.

Abstract: A process for preparing a compound of formula (I, I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, wherein: J represents O or S; T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises reducing a compound of formula (II, II) or a tautomeric form thereof or a salt thereof or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a complex hydride reducing agent or a source of a complex hydride reducing agent; and thereafter, as required, preparing a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof.

Abstract: Novel optically active or racemic azethidine carboxylic acid derivatives (azethidine-2-carboxylic acid N-carboxyamino acid anhydrides) which are useful as drug intermediates and an industrially advantageous process for producing the same are provided. Namely, a process for obtaining azethidine-2-carboxylic acid N-carboxyamino acid anhydrides starting with azethidine-2-carboxylic acids is provided. Via the azethidine-2-carboxylic acid N-carboxyamino acid anhydrides according to the invention, azethidine derivatives having peptide bond, which are useful as drugs, can be obtained by an industrial and economic process without resorting deblocking reaction.

Abstract: Disclosed are a fluorinating agent represented by the general formula (1): wherein R1 to R4 are a substituted or unsubstituted, saturated or unsaturated alkyl group or a substituted or unsubstituted aryl group, and can be the same or different; R1 and R2 or R3 and R4 can bond to form a ring including a nitrogen atom or a nitrogen atom and other hetero atoms; or R1 and R3 can bond to form a ring including a nitrogen atom or a nitrogen atom and other hetero atoms, for example: a preparation process of the fluorinating agent and a process for preparing fluorine compounds by reacting various compounds with the fluorinating agent. The invention has also disclosed that the fluorinating agent is very effective for fluorinating oxygen containing functional compounds.

Abstract: Novel processes and intermediates are provided for the synthesis of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acids that are useful as monomers for polyamides capable of binding dsDNA. According to one preferred reaction scheme, an alkyl alkoxymethylene nitroacetate (Formula VIII) is prepared by reaction of a trialkyl orthoformate or orthoacetate with a nitroacetate ester in the presence of a carboxylic anhydride. The compound of Formula VIII is condensed with an N-substituted glycine to yield an N-substituted (2-nitro-2-alkoxycarbonyl)vinyl glycinate ester (Formula VII). Ring closure in the presence of an alkali metal alkoxide yields a 4-nitro-3-hydroxypyrrole-2-carboxylic ester (Formula V). After blocking of the 3-hydroxy group to produce a further intermediate (Formula IV), the 4-nitro group is reduced to a 4-amino group (Formula III), and the 4-amino group is then blocked by reaction with a dicarbonate diester to produce the fully blocked intermediate (Formula II).

Abstract: The present invention provides methods for making N-methylpyrrolidine and analogous compounds via hydrogenation. Novel catalysts for this process, and novel conditions/yields are also described. Other process improvements may include extraction and hydrolysis steps. Some preferred reactions take place in the aqueous phase. Starting materials for making N-methylpyrrolidine may include succinic acid, N-methylsuccinimide, and their analogs.

Abstract: A method of processing agricultural oil in which non-toxic reagents are used, so that a waste stream is evolved suitable for use as a nutrient source and wherein the non-toxic reagents include nutrient source and wherein the non-toxic reagents include nutrient components whereby the nutrient value of the waste stream is enhanced. A variation of convention refining is detailed in which potassium hydroxide is used as refining caustic instead of conventional sodium hydroxide. The resulting process exhibits improvements in waste wash characteristics, more complete oil recovery, less oil in the soapstock, reduced interlayer formation, more soap removed from the refined oil into the soapstock stream, and a less viscous soapstock.

Abstract: Phospolanes and diphospholanes of the general formula I where: is H, C1-C6-aryl, alkylaryl, SiR32, R2 is alkyl or aryl, A is H, C1-C6-alkyl, aryl, Cl or B is a linker with 1-5 C atoms between the two P atoms, and their use as catalyst in asymmetric synthesis.

Abstract: Compounds of formulae I and Ia, wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and at least one hetero atom selected from the group O, S and NR, or ferrocenyl; R is H or C1-C4alkyl; each R4 individually or both R4 together are a hydrocarbon radical having from 1 to 20 carbon atoms; and R01 and R02 are each independently of the other a hydrogen atom or a hydrocarbon radical having from 1 to 20 carbon atoms, are chiral ligands for metal complexes with metals of sub-groups I and VIII, which are catalysts for asymmetric addition reactions, for example of hydrogen, to prochiral unsaturated organic compounds.

Abstract: Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.

Abstract: A diorganodichlorosilane is prepared by subjecting organochlorosilanes to disproportionation reaction in the co-presence of a SiH group-containing compound and in the presence of a primary catalyst of AlCl3 or AlBr3 and a co-catalyst of Mg, Al, Ca, Ti, Fe, Ni, Cu, Zn or Sn or a compound thereof. The invention enables disproportionation reaction of organochlorosilanes under atmospheric pressure and at a low temperature at which no substantial sublimation of AlCl3 or the like occurs, thus allowing the reaction equipment to be simple and improving the safety of reaction.

Abstract: The invention relates to a process allowing the preparation of a (dialkylphosphono)alkyl (meth)acrylate, corresponding to the formula: by reaction of an alkyl (meth)acrylate A of formula: with a dialkylphosphonated alcohol B of formula: in the presence of a catalyst comprising zirconium acetylacetonate.

Abstract: An alkene (1) is added to cyclopentenone (2) under the action of an alkyl lithium and an organic copper reagent to form an adduct, said adduct is reacted with e.g.

Abstract: A base catalyst, obtained by formulating at least one alkali metal compound selected from the group consisting of alkoxides, hydroxides and oxides of alkali metals and an alkaline-earth metal oxide in a ratio of “the weight of alkaline metal compound/the weight of alkaline-earth metal oxide”=0.005 to 1, is used in a reaction of an aldehyde to produce a glycol monoester, thereby providing a base catalyst with an improved efficiency which can be applied to aldol reaction or the like and which has high activity to give target product in a high selectivity.

Abstract: Diaryliodonium salts are disclosed, as well as a method for preparing them, in which one of the aryl groups bonded to the positively-charged iodine ion contains a methyl substituent, and the other one contains a hydroxyl-substituted alkoxy group. The salts are synthesized from (o, m, or p)-iodotoluene, as opposed to iodobenzene, and therefore do not pose a carcinogenic risk. In addition, the present salts are unexpectedly more soluble in most organic solvents, as well as in nonpolar monomers, than the corresponding benzene catalysts. The salts are useful as cationic photoinitiators, cationic thermal initiators (often combined with a cocatalyst, e.g. copper), and as starting materials in the synthesis of urethane-containing iodonium salts.

Abstract: Compounds having Formula I or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.

Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals. The compounds have the general formula I: wherein X is F or Cl; R1 is COOH, COO(alkyl), or an isostere thereof; and R2 is an aryl group.

Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: A process of producing an aliphatic aldehyde-acid (e.g., adipaldehyde-acid) and/or an aliphatic dicarboxylic acid (e.g., adipic acid) comprising oxidizing a cyclic ketone (e.g., cyclohexanone) with molecular oxygen in the presence of a fixed catalyst which comprises a composite of a carrier and at least one metal element belonging to the groups 4 to 11 of the Periodic Table supported on the carrier and has an acid amount of 0.06 mmol/g or more per unit weight of the carrier.

Abstract: The present invention provides a process for producing acrolein and acrylic acid by the vapor-phase oxidation of propylene in the presence of Mo—Bi—Fe-based compound oxide catalysts packed in a fixed-bed multitubular reactor wherein acrolein and acrylic acid can be stably produced in high yield for a long period of time. This process is characterized in that each reaction tube having two or more reaction zones disposed along the axis of the tube is packed with catalysts having different ratios of the Bi and/or Fe content to the Mo content in such a way that the ratio decreases from the gas inlet side toward the gas outlet side.

Abstract: The invention relates to a method for the preparation of lactic acid and calcium sulphate, in which (a) an aqueous solution that contains lactate is reacted with sulphuric acid at a temperature that is essentially higher than the transition temperature of calcium sulphate dihydrate (CaSO4.2H2O), with the formation of a mixture that contains calcium sulphate hemihydrate and lactic acid, (b) the mixture from step (a) is subjected to at least one recrystallization step at a temperature that is essentially lower than the transition temperature of calcium sulphate dihydrate, with the formation of a precipitate of calcium sulphate dihydrate and an aqueous solution of lactic acid, and (c) the precipitate of calcium sulphate dihydrate is separated off from the aqueous solution of lactic acid.

Abstract: Process for the preparation of urea from ammonia and carbon dioxide in which the composition of the various process streams is measured via an ultrasonic measuring principle and in which the results of these measurements are used for process control. The process is particularly suitable for continuous measurements in a urea process.

Abstract: A process for preparing amines comprises reacting an epoxide of the formula (I) where R1, R2, R3 and R4 are each, independently of one another, hydrogen or a linear or branched, saturated or unsaturated C2-C200-hydrocarbon radical, with ammonia and hydrogen in the presence of a catalyst, where the molar ratio of ammonia:epoxide is from 5:1 to 500:1 and the hydrogen pressure is from 10 bar to 500 bar.

Abstract: A process for separating the (d/l) and (meso) diastereoisomers of bis-[1-phospha-2,3-diphenyl-4,5-dimethylnorbornadiene] comprising converting the mixture of diastereoisomers of bis-[1-phospha-2,3-diphenyl-4,5-dimethylnorbornadiene] to a mixture of the corresponding diastereoisomers of diphosphine disulphide or dioxide, then in separating the two diastereoisomers in dioxide or disulphide form.

Abstract: The present invention deals with the catalytic hydrogenation of fluid used to cool and dielectrically insulate an x-ray generating device within an x-ray system. According to the present invention, a method and apparatus are provided for hydrogenating fluid that has been exposed to x-rays to reduce the amount of H2 gas, free hydrogen atoms and unsaturated molecules in the fluid. The method comprises exposing the fluid within the x-ray system to a catalytically effective amount of catalyst. The catalyst operates in temperatures in the range of about 10-300° C. and pressures in the range of about 0.1-30 atmospheres. The catalyst may comprise a solid, non-soluble catalyst, a soluble catalyst, or a combination of both. A suitable solid, non-soluble catalyst comprises Group VIII elements and their compounds. Group VIII elements comprise iron, cobalt, nickel, ruthenium, rhodium, palladium, osmium, iridium and platinum.