Abstract: The present invention provides a glyoxime derivative displaying excellent pesticidal effect or a salt thereof and a pesticide containing the same as an active ingredient. This pesticide is characterized by containing as an active ingredient, a glyoxime derivative expressed by the general formula [I] (in which X represents a cyano group or a carbamoyl group, R1 represents a C1˜C8 alkyl group, a C3˜C6 cycloalkyl C1˜C6 alkyl group, etc, and IV represents a hydrogen atom, a C1˜C8 alkyl group, a C3˜C6 cycloalkyl C1˜C6 alkyl group, etc.) or an agriculturally acceptable salt thereof.

Abstract: Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

Abstract: The present invention relates to a method for preparing optically active N-methylamino acids and/or optically active N-methylamino acid amides by subjecting the cells or treatment products of a microorganism belonging to the Mycoplana genus to the hydrolysis with N-methylamino acid amide to give an optically active N-methylamino acid and an optically active N-methylamino acid amide. According to the present invention, optically active N-methylamino acids and optically active N-methylamino acid amides useful as the raw material of pharmaceuticals can be stereoselectively obtained with good efficiency.

Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Abstract: The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin—inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.

Abstract: The present invention relates to method for the preparation of an ?-amino-alkane(thio)amide having the general formula (6) Furthermore, novel intermediates and partial reaction steps of the claimed method are disclosed.

Abstract: A method for efficiently separating and collecting an optically active amino acid amide and an optically active amino acid from an aqueous solution containing the optically active amino acid amide and the optically active amino acid includes separating and collecting an optically active amino acid amide from an aqueous solution containing the optically active amino acid amide and an optically active amino acid, utilizing a difference in solubility in an organic solvent between the optically active amino acid amide and the optically active amino acid, without desalting the aqueous solution or after desalting the same, under such a condition that a ratio (C/A) of the total equivalent (C) of cations to the total equivalent (A) of anions contained in the aqueous solution falls within the range from 0.95 to 1.05 when the aqueous solution is not desalted, and the range from 0.5 to 1.5 when the aqueous solution is desalted.

Abstract: The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with ?-amyloid peptide.

Abstract: The invention relates to reactive derivatives on the basis of dianhydrohexitol-based isocyanates.

Abstract: The disclosure relates to engineered amidase polypeptides and processes of using the polypeptides for chiral resolution of amino acid amide compounds. The disclosure further relates to the polynucleotides that encode the engineered amidase polypeptides and related vectors, host cells, and methods for making the engineered amidase polypeptides.

Abstract: Compounds comprising end groups represented by formula (Rf-Q)a-X-(A-)b and compounds comprising the reaction product of components comprising a multifunctional isocyanate compound and a fluorinated compound represented by formula (Rf-Q)a-X—(Z)b. Each Rf is independently a partially fluorinated or fully fluorinated group selected from RfA(O)2CHL?-(CF2)n—; [RfB—(O)1—C(L)H—CF2—O]m—W—; CF3CFH—O—(CF2)p—; CF3—(O—CF2)Z—; and CF3—O—(CF2)3—O—CF—. Methods of making an article having a surface using the fluorinated compounds and treated articles are also disclosed.

Abstract: A compound represented by the formula (I) is used as an active ingredient in a medicament for treatment or prevention of infectious diseases caused by protozoa or bacterium. X represents halogen, Z represents —(CH2)m— wherein m is an integer of 1-5, and R represents one of the following (i)-(v): (i) hydrogen n represents an integer of 0-5, R1's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. R2's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. (iv) alkyl having 1-5 carbon atoms, (v) hydroxyalkyl having 1-5 carbon atoms.

Abstract: Compounds and methods are provided for controlling microorganisms in water systems having a pH of 5 or greater. The compounds are of the formula I: wherein X, R and R1 are as defined herein.

Abstract: A compound represented by the formula (I) is used as an active ingredient in a medicament for treatment or prevention of infectious diseases caused by protozoa or bacterium. X represents halogen, Z represents —(CH2)m— wherein m is an integer of 1-5, and R represents one of the following (i)-(v): (i) hydrogen n represents an integer of 0-5, R1's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. R2's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. (iv) alkyl having 1-5 carbon atoms, (v) hydroxyalkyl having 1-5 carbon atoms.

Abstract: The present invention relates to means and devices for electro-filtration of molecules. The membranes comprise N-acryloyl-tris(hydroxymethyl)aminomethane (NAT) covalently linked to a support. The invention further encompasses compositions comprising an isoelectric buffer covalently bound to N-acryloyl-tris(hydroxymethyl)aminomethane (NAT). In particular, the present invention relates to membranes and devices allowing an isoelectric filtration of molecules in solution.

Abstract: The present invention is directed to a process for preparing ?-amino-?-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.

Abstract: The present invention is related to a compound according to formula (I), wherein R1 and R2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and YÉ is a pharmaceutically acceptable anion.

Abstract: A method for separately collecting an optically active amino acid amide and an optically active amino acid from an aqueous solution containing same, together with at least one member selected from the group consisting of an acid, a base, and a salt, includes a step of neutralizing an acid or base in the aqueous solution, a desalting step of removing a salt contained in the aqueous solution and/or formed in the neutralization step, and a step of separately collecting the optically active amino acid amide/amino acid separately from the desalted aqueous solution by a process which takes advantage of a difference in solubility between the two components in an organic solvent. The desalting step is preferably performed by electrodialysis, optionally with ammonia added to the aqueous solution. The optically active amino acid amide/amino acid can be separately collected with high efficiency using an organic solvent.

Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.

Abstract: The invention relates to a process for racemising an enantiomer-enriched Schiff base of a primary amino acid amide with a strong base that is chemically reactive towards water. The reaction is conducted in an organic solvent. Preferably a metal alkoxide, a metal alkyl, a metal amide, or a metal hydride, in particular a metal alkoxide is applied as the strong base. As the Schiff base preferably N-benzylidene primary amino acid amide is used, with the primary amino acid amide preferably being derived from an aliphatic primary amino acid amide, for example tertiary-leucine amide. As organic solvent use is preferably made of an aromatic hydrocarbon, a cyclic, aliphatic hydrocarbon or a ether, in particular an aromatic hydrocarbon is applied. The invention may also be applied for the racemisation of an enantiomer-enriched primary amino acid amide.

Abstract: Objects of the present invention are to provide an oxidative stress inhibitor which is capable of suppressing the expression of a cytotoxic protein and the activation of a gene transcriptional regulatory factor taking part such expression of a cytotoxic protein and exhibits good feeling upon use and safety; to provide a method for preventing, retarding, alleviating or treating a skin change due to aging or an undesirable aesthetic skin change, both caused or promoted by an oxidative stress; and to provide a cosmetic composition or dermatologic preparation for external use comprising the oxidative stress inhibitor as an effective ingredient, and for those purposes are employed an oxidative stress inhibiting agent which comprises, as an effective ingredient, at least one selected from cysteine or cystine derivatives and the salts thereof.

Abstract: A amidoamine composition containing oligomeric amidoamine compounds having the structure: the average of x based on the amidoamine composition is at least 0.2, and Z is the residue of a polyoxyalkylene polyether polycarboxylic acid compound, and the amidoamine composition is the reaction product of primary polyamine compounds with polyoxyalkylene polyether polycarboxylic acid compounds at a corresponding equivalent weight ratio of at least 4.0:1 under oligomeric reaction conditions effective to increase the amine nitrogen equivalent weight of the amidoamine composition by at least 10% over the average acid equivalent weight of said polyoxyalkylene polyether polyacid composition. There is also provided glycidated amidoamine compositions used as epoxy functional surfactants, and the aqueous epoxy resin dispersions thereof, and the curable epoxy resin compositions thereof.

Abstract: Process for the preparation of a Schiff base of an &agr;-alkyl-&agr;-amino acid amide and an aldehyde, wherein the corresponding &agr;-aminonitrile is contacted with a base and the aldehyde and wherein it is ensured that the reagents are in good contact. The Schiff base obtained may be further hydrolysed to form the &agr;-alkyl-&agr;-amino acid amide and the aldehyde. Preferably a substituted or unsubstituted benzaldehyde is used as the aldehyde. The reaction is preferably carried out in a practically homogeneously mixed phase obtained by using a solvent, for example methanol or ethanol. Preferably NaOH or KOH is used as the base.

Abstract: The present invention is directed towards compounds of the general formula (I) (I) are important intermediates for the preparation of pharmaceuticals. Further intermediates, process for the preparation of (I) and use thereof.

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: Process for the hydrolytic ring cleavage of thiazolidine derivatives to give 2-aminomercaptan derivatives and carbonyl compounds, which comprises bringing an aqueous solution of the thiazolidine derivative into contact with an acidic cation exchanger in the H+ form, giving a solution L1 which contains the carbonyl compound and eluting the cation exchanger with a suitable eluent, giving a solution L2 which contains the 2-aminomercaptan derivative.

Abstract: Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A—N(Z)—CH(R1)C(O)—Q  (I) wherein A is represented by the formula: XO—[C(R2)2]n— wherein n is an integer of from 1 to about 3, X is selected from the group consisting of a hydrogen atom, an acyl group and a halogenated acyl group and each R2 is independently selected from the group consisting of a hydrogen atom, an alkyl group having from 1 to about 3 carbon atoms, a hydroxyalkyl group having from 1 to about 3 carbon atoms, and CH2OX; Z is selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to about 3 carbon atoms, and A; R1 is an amino acid side chain group or an amino acid side chain group which forms with R2 a single heterocyclic structure having a total of from 5 to 7 atoms in the ring; and wherein Q is a substituent s

Abstract: A process for the production of 6-aminocaproamide comprising reacting 5-cyanovaleramide with hydrogen in the presence of a metal catalyst. The 6-aminocaproamide is useful, for example, in the production of caprolactam and nylon 6.

Abstract: A composition having the formula: wherein R is a linear alkyl, branched alkyl, cycloalkyl, polycyclic alkyl, alkylaminoalkyl, or alkyloxyalkyl group having 1 to 20 carbon atoms and at least one primary, secondary, or tertiary amino functional group. The composition is effective as a catalyst in the production of polyurethanes.

Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: The present invention provides amine/amide catalysts for use in catalyzing the formation of polyurethane. The amine/amide catalysts, which have low fugitivity due to their reactivity with isocyanates, and good catalytic activity, have the structure ##STR1## wherein Q is C.sub.z H.sub.2z+1, or (CH.sub.2).sub.n N(R.sup.3).sub.k T, T is a monovalent C.sub.1 -C.sub.4 alkyl, amino-C.sub.1 -C.sub.4 -alkyl, mono-C.sub.1 -C.sub.4 -alkylamino-C.sub.1 -C.sub.4 -alkyl, or di-C.sub.1 -C.sub.4 -alkylamino-C.sub.1 -C.sub.4 -alkyl group, or T is a divalent alkyl, amine substituted alkyl, alkylaminoalkyl, or alkoxyalkyl group which forms with the nitrogen atom shown in structure (I) to which T is attached a cyclic structure which incorporates up to 6 carbon atoms in the ring as well as the nitrogen atom shown in structure (I), which cyclic structure may be substituted with C.sub.1 to C.sub.4 alkyl;k=0 or 1, being 1 if T is a monovalent group and 0 if T is a divalent group; R.sup.2 .dbd.H or C.sub.z H.sub.2z+1 ; R.sup.3 .dbd.

Abstract: The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH.sub.2 NH or CONH, Y is CH.sub.2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH.dbd.C(R.sup.4)R.sup.5, CH.sub.2 CH(R.sup.4)R.sup.5 or an alkoxycarbonyl group, R.sup.1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R.sup.2 and R.sup.3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R.sup.4 and R.sup.

Abstract: 3-{N-[2-(N',N'-dimethylamino ethoxy)ethyl]-N-methylamino}propionamide is a new compound which is useful as a catalyst in the production of polyurethane foams.

Abstract: Oligomeric compounds that contain perfluoroalkyl of general formula IA--R.sup.F (I)in whichA is a molecule portion that contains 2-6 metal complexes that are connected directly or via a linker to a nitrogen atom of an annular skeleton chain, andR.sup.F is a perfluorinated, straight-chain or branched carbon chain with formula --C.sub.n F.sub.2n E, in which E represents a terminal fluorine, chlorine, bromine, iodine, or hydrogen atom and n stands for numbers 4-30,are valuable compounds for diagnosis, especially as in-vivo contrast media.

Abstract: Peptidomimetic compounds useful in the treatment of Ras-associated human cancers, and other conditions mediated by farnesylated or geranylgeranylated proteins; and synthetic intermediates thereof.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Abstract: A process for the preparation of .epsilon.-caprolactam and .epsilon.-caprolactam precursors, starting from the corresponding 5-formylvalerate ester, ammonia and hydrogen in the presence of a hydrogenation catalyst is disclosed, wherein in a step (a) 5-formylvalerate ester is reacted with ammonia under non-hydrogenating conditions, and in a step (b) the reaction product obtained in step (a) is converted to .epsilon.-caprolactam and the .epsilon.-caprolactam precursor(s) under hydrogenating conditions, in the presence of ammonia.

Abstract: L-amino acid amides are converted to the corresponding D-amino acid amides. An amide formed from an L-amino acid and an optically active (S)-.alpha.-alkylbenzylamine is subjected to dehydration condensation with an aryl aldehyde to form a Schiff's base, which is racemized at the amino acid moiety in the presence of a base to yield an N-allylidene-D-amino acid-(S)-amide. The less-soluble diastereomer N-allylidene-D-amino acid-(S)-amide is crystallized from the reaction mixture and recovered by means of solid/liquid separation. The N-allylidene form is readily hydrolyzed into the amino acid-(S)-amide and the starting aldehyde.

Abstract: One or more polyamides can be depolymerized in the presence of at least one nitrogen-containing compound. The depolymerization takes place at a pressure between about 0.5 and about 5 atm. The polyamide may be in the form of carpet waste or other heterogeneous form. Advantages include better selectivity towards the polyamide monomeric components and use of low pressure equipment to effect depolymerization.

Abstract: The present invention relates to a new class of carbohydrate based nonionic surfactant, i.e., alkyl and alkenyl glycasuccinimide, and a process for their manufacture.

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.

Abstract: Disclosed are nonpeptides having bradykinin antagonist activity of the formulae (I) and (II) ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and methods of treating diseased or pathological conditions using the pharmaceutical compositions.

Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Abstract: A synergistic mixture of a carbonate and/or bicarbonate with a phosphonate, especially an organoamino methylene phosphonate or an N-oxide thereof, inhibits or reduces nitrosamine contamination during preparation, storage and/or heating of products which are susceptible to contamination with nitrosamine.

Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.

Abstract: Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.