Abstract: A process for amino acid derivatives shown by the below general formula (I): (wherein R1 means a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II): (wherein R1 has the same meaning as described above, and R2 means a straight chain or branched chain alkyl group with 1-4 carbon atoms.

Abstract: The present invention is directed to a method for producing amino acids by reacting halogenated carboxylic acid ester (haloacid esters) with a metal cyanate in the presence of an alcohol and by subsequent acidic saponification of the urethane carbonic acid formed. The method is characterized by the metal cyanate being placed at an elevated temperature in an organic solvent and the other reactants being continuously charged into the mixture over a defined time period.

Abstract: This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X2 is a halo group, and is —F, —Cl, —Br, or —I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic estenfication (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).

Abstract: The present invention provides cystine derivatives, which may be in a free form, a salt form, a solvate form. The cystine derivatives of the present invention may be used to suppress activation of inflammatory factors. Accordingly, the present invention provides: compositions containing the cystine derivatives; a method for suppressing the activation of inflammatory factors by administering the composition; a method for preventing, ameliorating and/or therapeutically treating diseases, skin injuries or disorders involved in the activation of inflammatory factors by administering the composition; a method for preventing, delaying, ameliorating and/or therapeutically treating skin change via aging or aesthetically unfavorable skin change as induced or promoted by inflammatory factors by administering the composition; and pharmaceutical agents containing the cystine derivatives.

Abstract: A process for producing an optically active 3-azide-carboxylic acid ester by reacting an optically active 3-hydroxycarboxylic acid ester and a thionyl halide in the presence of a basic substance in an organic solvent to produce an optically active 3-halogenocarboxylic acid ester which is then reacted with an azide salt represented by the formula: MN3 (wherein M is an alkaline metal) in water or a mixture of water and a water soluble organic solvent.

Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The present invention relates to novel covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids with aminoalcohols of general formula (I) which can usefully be used as agonists of the CB2 cannabinoid receptor and hence as drugs active in pathological conditions which can be controlled by stimulation and/or costimulation of this receptor

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-?-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-?-lactones, and analogs thereof and their use as proteasome inhibitors.

Abstract: As an ?-iminoester derivative that is stable under normal conditions and a method of producing various ?-aminoester derivatives using them, a polymer-immobilized ?-iminoester derivative represented by the following general formula (1): wherein R1 represents an alkyl chain of 1 or more carbons, and R2 represents a hydrogen atom, halogen atom, or an alkyl group, aryl group or alkoxy group that may contain substituents, and a method of producing an ?-iminoester derivative using them are provided.

Abstract: It is the problems to provide an effective production method for optically active N-aryl-&bgr;-amino acid compounds, which at the same time is suitable for industrial production. By the reaction of optically active sulfonylated &bgr;-hydroxycarboxylic acid compounds, which are easily derived from &bgr;-keto carboxylic acid compounds, with aromatic amines, optically active N-aryl-&bgr;-amino acid compounds are obtained.

Abstract: Provided is a poly(amino ester) having a polymer backbone comprising at least one secondary amine linkage and at least one tertiary amine linkage in the polymer backbone. Poly(amino ester)s are prepared via the Michael addition of a bis(acrylate ester)monomer to a diamine monomer, wherein the diamine monomer has one primary amino group and one secondary amino group, and can be end-capped by reaction with a suitable reagent. The inventive poly(amino ester)s may be used as vectors for delivery of a bioactive agent, such as DNA, to a cell.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: The present invention is directed to an analytical method for measuring the concentration of an N-(phosphonomethyl)iminodiacetic acid (“NPMIDA”) substrate, an N-(phosphonomethyl)glycine product, formaldehyde, formic acid, N-methyl-N-(phosphonomethyl)glycine (“NMG”), N-methyl-aminomethylphosphonic acid (MAMPA) or aminomethylphosphonic acid (“AMPA”)) in an aqueous mixture thereof, using infrared spectroscopy. The present invention is also directed to a process for oxidizing an N-(phosphonomethyl)iminodiacetic acid substrate to form a N-(phosphonomethyl)glycine product, and as part of the process, measuring the concentration of at least one reactant, product or byproduct of the oxidation reaction using the analytical method of the present invention and controlling the oxidation process in response to the measurement taken.

Abstract: The invention relates to synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or N(CH3)OCH3, Ra is a hydroxy-protecting group, and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further intermediates and methods for their preparation by Friedel-Crafts acylation.

Abstract: A process for the preparation of an enantiomerically enriched beta-amino acid derivative of formula (1), or the opposite enantiomer thereof, wherein R1 is an optionally substituted alkyl, aryl or heteroaryl group of up to 20 C atoms, R2 is ann alkyl group of up to 20 C atoms, and R3 is H or an alkyl or aryl group of up to 20 C atoms, which comprises asymmetric hydrogenation of the (z)-enamide precursor (2) in an alcohol solvent or cosolvent, catalysed by a cationic rhodium complex of a chiral phosphine ligand having the partial formula (3), wherein n is 0 to 6 and R represents at least one non-hydrogen organic group of up to 20 C atoms.

Abstract: A crystallization is carried out by adding a solution of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxylic anhydride in a good solvent to an aliphatic hydrocarbon solvent while inhibiting the oil formation and scaling of said N-carboxylic anhydride. Further, a crystallization is carried out by adding an aliphatic hydrocarbon solvent sequentially to a solution of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxylic anhydride in a good solvent over not less than ¼ of an hour and at a temperature of not higher than 60° C.

Abstract: Process for the preparation of 3-aminoalkanoic acid esters of the general formula: in which R is C1-6-alkyl and R1 is hydrogen, C1-6-alkyl or phenyl, or their salts, by catalytic hydrogenation of the corresponding 3-amino-2-alkenoic acid esters of the general formula: in which R and R1 have the above mentioned meanings. The hydrogenation is carried out in the presence of a strong acid and the salt of the 3-aminoalkanoic acid ester (I) and the strong acid formed is optionally converted into the free 3-aminoalkanoic acid ester (I) or into another salt in a manner known per se.

Abstract: A stereoselective process for the industrial synthesis of compounds of formula (I): wherein R represents linear or branched (C1-C6)alkyl, and application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present invention provides S-aryl cysteine in enantiomeric excess of greater than about 96%.

Abstract: The present invention is directed to labeled compounds, specifically where each C* is selected from the group consisting of a carbon-12, i.e., 12C, or a carbon-13, i.e., 13C and at least one C* is 13C, R1 is selected from the group of C1-C4 lower alkyl and aryl, and X is selected from the group of —NR2R3 where R2 and R3 are each independently selected from the group of C1-C4 lower alkyl, alkoxy and aryl, —SR4 where R4 is selected from the group of C1-C4 lower alkyl, alkoxy and aryl, and —OR5 where R5 is selected from the group of C1-C4 lower alkyl, alkoxy and aryl with the proviso that when R1 is methyl then R5 is other than methyl, when R1 is ethyl then R5 is other than ethyl, and when R1 is benzyl then R5 is other than benzyl.

Abstract: A process for synthesizing L and D-5,5,5,5′,5′,5′-hexafluoroleucine and protected analogs is disclosed. These compounds have utility in the preparation of fluorous peptides and proteins, which display interesting and unusual properties including strong self-association and an affinity for lipid bilayers.

Abstract: There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula wherein R1 and R2 are each independently of the other hydrogen, C1-C20alkyl; C3-C12cycloalkyl; unsubstituted or C1-C5alkyl-, C3-C12cycloalkyl-, C1-C5alkoxy-, C3-C12cycloalkoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C12cycloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl, phenyl-C1-C5alkyl, naphthyl and naphthyl-C1-C5alkyl; and R3 is C1-C20alkyl; C3-C12cycloalkyl. The compounds exhibit a pronounced activity against gram-positive and gram-negative bacteria, and also against yeasts and moulds.

Abstract: The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.

Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).

Abstract: This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.

Abstract: An accelerated process for preparing a methyl ester having formula (III) said process comprising reacting a carboxylic acid or salt thereof having formula (I) with dimethyl carbonate having formula (II) in the presence of a catalyst selected from the group consisting of 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; 4-dimethylaminopyridine; and combinations thereof, wherein R1 is selected from the group consisting of an alkyl, aryl, alkoxy, alkenyl, cycloalkyl, benzocycloalkyl, cycloalkylalkyl, aralkyl, heterocyclic, heteroaralkyl, alkoxyalkyl, carboxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, and haloalkyl; and M is selected from the group consisting of hydrogen, a monovalent metal, and a monovalent fractional part of a polyvalent metal, wherein said process is conducted under microwave irradiation at a frequency from 300 MHz to 30 GHz, and at a temperature of from about 120° C. to 300° C.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state.

Abstract: Disclosed is a noble &bgr;-hydroxyamide of general formula wherein R1 is alkyl, alkoxyalkyl or hydroxyalkoxyalkyl derived from at least one hydroxyfunctional compound, R2 is alkyl, aryl, alkylaryl or arylalkyl derived from at least one carboxyfunctional compound or at least one anhydride, halide or ester of at least one carboxyfunctional compound, R3 is N-alkyl or N-cycloalkyl derived from at least one alkanolamine and wherein m and n are independent integers and at least 1. In a further aspect the present refers to a process for synthesis of said &bgr;-hydroxyamide. The process comprises the Steps of (i) subjecting a di, tri or polyalcohol to alcoholysis with at least one di, tri or polyalkyl ester of a di, tri or polyfunctional carboxylic acid and (ii) subjecting obtained reaction product to aminolysis with at least one alkanolamine.

Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics. Accordingly, the present invention provides a method of treating bacterial infections in animals or humans which comprises administering, together with a b-lactam antibiotic, a therapeutically effective amount of a compound of formula I: including pharmaceutically acceptable salts, prodrugs, anhydrides, and solvates thereof.

Abstract: As an &agr;-iminoester derivative that is stable under normal conditions and a method of producing various &agr;-aminoester derivatives using them, a polymer-immobilized &agr;-iminoester derivative represented by the following general formula (1) 1

Abstract: The invention is a method for producing &dgr;-aminopentadienoate derivatives of formula (1), the method comprising reacting a streptocyanine derivative of formula (2) with an ester derivative of formula (3) in the presence of an organic base. In formulae (1) to (3), R1 represents an alkyl group or an aryl group; R2, R3, R4 and R5 independently represent a hydrogen atom or an alkyl group; R2 and R3, or R4 and R5 may bond to each other to form a ring; Y represents an electron attractive group; X represents an acid radical; n indicates 0 or a positive number, which is no more than 5; Y may bond to R1 to form a ring.

Abstract: The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.

Abstract: A compound selected from the group consisting of a compound of formula I 1

Abstract: One aspect of the present invention relates to 2-hydroxymethylglutamic acid and congeners thereof. A second aspect of the invention relates to a method of synthesizing 2-hydroxymethylglutamic acid and congeners thereof.

Abstract: The invention provides adjuvants, immunogenic compositions, and methods useful for polynucleotide-based vaccination and immune response. In particular, the invention provides an adjuvant of cytofectin:co-lipid mixture wherein cytofectin is GAP-DMORIE.

Abstract: The invention relates to a method of producing 3-aminoalkanoic acid esters of the general formula (I), wherein R represents C1-6 alkyl, and R1 represents hydrogen, C1-6 alkyl or phenyl, or the salts thereof, by catalytically hydrating the corresponding 3-amino-2-alkenoic acid esters in the presence of a strong acid.

Abstract: New secondary amines are described which are prepared from inexpensive, commercially available raw materials, are stable at room temperature, and are reactive toward electrophiles. The secondary amines are prepared by the addition of one or more primary amines with one or more male (amide/ester) and fumar (amide/ester) Michael receptors. The above amines can be used as coreactants with aliphatic polyisocyanates for polyurea coatings. The novel secondary amines are also described as particularly useful as part of a two-part liquid pavement marking composition for pavement markings.

Abstract: The invention relates to a process for preparing N-formylamino carboxylic esters by reacting amino carboxylic acids with formic esters.

Abstract: This invention relates to preparation of enantio-enriched compounds, and more particularly to enantio-enriched kavalactone compounds and derivatives thereof. The methods provide compounds that are useful as reagents, or building blocks, in the construction of other enantio-enriched compounds.

Abstract: A labeling reagent for use in oligonucleotide (“oligo”) synthesis, as well as a method of preparing such a labeling reagent, a method of using such a reagent for synthesizing a labeled oligonucleotide, and an oligonucleotide prepared using such a reagent. The reagent can be used to label either the 3′ or 5′ termini of a synthesized oligo, and/or for one or more positions along the oligo. The labeling reagent can be prepared by a reaction scheme that involves the initial preparation of hydroxyacids, tritylated hydroxyacids and coupling of such derivatives to diamine, wherein the amine function serves at an attachment point for labels and the hydroxyl groups can either be used to immoblize the molecules to support or can be converted to provide a phosphorylating reagent.

Abstract: Provided is a deodorant having excellent masking and deodorizing effects of scalp odor, body odor and foot odor.

Abstract: A low temperature process for preparing a methyl ester having formula (III) said process comprising reacting a carboxylic acid or salt thereof having formula (I) with dimethyl carbonate having formula (II) in the presence of a catalyst selected from the group consisting of 1,8 diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and combinations thereof, wherein said process is conducted at a temperature of about 10° C. to less than 120° C.; R1 is selected from the group consisting of an alkyl, aryl, alkoxy, alkenyl, cycloalkyl, benzocycloalkyl, cycloalkylalkyl, aralkyl, heterocyclic, heteroaralkyl, alkoxyalkyl, carboxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl and haloalkyl; and M is selected from the group consisting of hydrogen, a monovalent metal and a monovalent fractional part of a polyvalent metal.

Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a &bgr;-lactam.

Abstract: A process for producing an amide compound of the following formula by reacting a nitrile compound of the formula with an acid to obtain an oxazolinone compound of the formula and reacting the oxazolinone compound with a carboxy compound of the formula in the presence of a base.

Abstract: Polyacetylene compounds and process for the preparation thereof from a chiral dihydroxy amide are described. The compounds preferably have diacyl groups attached to the amide. The compounds are useful for making films which are electrically conductive, near infrared absorbing, polarizing, and have the characteristic optical and other properties of polyacetylenes.

Abstract: Enantiomerically enriched N-acylated &bgr;-amino acids are synthesized by catalytic enantioselective hydrogenation of E-isomers and Z-isomers of 3-amino acrylic acid derivatives in the presence of a catalysts of formula (I)

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.