Abstract: Methods of producing aminonitrobenzoic acids are disclosed. A dinitrobenzoic acid may be reduced to an aminonitrobenzoic acid. In some specific embodiments, 2,6-initrobenzoic acid may be converted to 2-amino-6-nitrobenzoic acid. An end product may be used as an intermediate in the manufacture of various compounds including agricultural chemicals and pharmaceuticals.

Abstract: Mitigation of photo-induced damage in excitation illuminated reactions and analyses utilizing such reactions results in an enhanced performance for the reactions and the analyses. There is provided a novel class of triplet-state quenchers for mitigating photo-induced damage which are both simple in structure and effective at preventing and/or reducing photo-induced damage to reaction components of excitation illuminated reaction mixtures. Also provided are methods of using the compounds of the invention, devices and kits incorporating the compounds of the invention.

Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.

Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.

Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:

Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.

Abstract: A GABA (gamma-aminobutyric acid) release-inhibiting agent in the cerebellum and a composition for treating pathological symptoms caused by over-release of GABA in the cerebellum, each comprising a Bestrophin 1(Best1) channel inhibitor as an active ingredient; a GABA release-promoting agent in the cerebellum and a composition for treating pathological symptoms caused by the deficit of GABA in the cerebellum, each comprising a Best1 channel activator as an active ingredient; and a method for screening a GABA release-regulating agent in the cerebellum, which uses Best1 channel as target, are provided.

Abstract: The present invention provides compounds comprising amino acid R groups, compositions comprising the same, and methods of inhibiting neuraminidase and/or treating influenza, Pseudomonas aeruginosa, or Bacteroides fragilis infection in a mammal.

Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (VI?), (VII?) and (VIII?) and their preparation.

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X1, X2, X5, R2 and R10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract: Methods of producing aminonitrobenzoic acids are disclosed. A dinitrobenzoic acid may be reduced to an aminonitrobenzoic acid. In some specific embodiments, 2,6-dinitrobenzoic acid may be converted to 2-amino-6-nitrobenzoic acid. An end product may be used as an intermediate in the manufacture of various compounds including agricultural chemicals and pharmaceuticals.

Abstract: Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.

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 compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula

Abstract: Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.

Abstract: Pharmacophore models of VLA-4 inhibitors, methods of identifying novel inhibitors and novel inhibitors identified by these methods.

Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.

Abstract: A new process for the preparation of diethylenetriaminepentaacetic-monoamides in which amines can be reacted with sensitive groups, a higher mono/diamide selectivity is achieved, a higher yield of monoamide is achieved and has a simple reaction scheme and working-up.

Abstract: The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula I: In Structural Formula I, R is an amine protecting group, and R1 is an amino acid side-chain, a protected amino acid side-chain, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, a substituted or unsubstituted aralkyl or a substituted or unsubstituted heteroaralkyl group. The method involves contacting a 1-nitro-3-substituted-3-amino-2-propanone with a reducing agent to form a mixture of 1-nitro-3-substituted-3-amino-2-propanol diastereomers. The 1-nitro-3-substituted-3-amino-2-propanol diastereomers are then separated by simulated moving bed chromatography to obtain one or more 1-nitro-3-substituted-3-amino-2-propanol diastereomer.

Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.

Abstract: The current invention discloses halogenated amidino amino acid derivatives useful as nitric oxide synthase inhibitors, and pharmaceutically acceptable salts thereof.

Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: A process for the preparation of an allylic aromatic compound in which an aromatic amine is reacted first with a nitrite and then with an allylic olefin having an eliminatable terminal substituent. Novel allylic derivatives of disubstituted benzene compounds are also described.

Abstract: New compounds of general formulae (III), (IV) and (V).

Abstract: The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method, novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients.

Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: The invention relates to new oxime derivatives, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 and [sic] CHCH.sub.2 CH.sub.3 ;R.sup.1 is hydrogen and [sic] alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl and [sic] alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sup.4 and R.sup.5 are as defined in the specification.

Abstract: A method of purifying dinitroaniline of the general formula: ##STR1## in which: R is linear or branched C.sub.1 -C.sub.6 alkyl, C.sub.4 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 monohaloalkyl or C.sub.1 -C.sub.4 alkoxy(C.sub.2 -C.sub.4)alkyl,Y is C.sub.1 -C.sub.4 alkyl, halogen or CF.sub.3, andX is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 monohaloalkyl, or C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.4)alkyl, by N-denitration of the impurities of N-2,6-dinitroaniline contained therein, in the presence of a base selected from alkali-metal hydroxides, alkali-metal carbonates and ammonium hydroxide, at neutral or basic pH, comprising the treatment, with stirring, of the dinitroaniline to be purified, with an alcoholic organic solvent.

Abstract: The present invention provides an economically advantageous and efficient process for producing an optically active homophenylalanine derivative of the general formula (IV), and an intermediate therefor and a process for producing it. The present invention relates to a process for producing homophenylalanine derivative of the general formula (IV) which comprises reacting a .beta.-benzoylacrylic acid derivative of the general formula (II) with a 1-arylethylamine derivative of the general formula (III) and reducing the resultant .gamma.-oxo-homophenylalanine derivative of the general formula (I).

Abstract: A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.

Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.

Abstract: A compound according to the formula: ##STR1## and conjugates thereof.

Abstract: Novel compounds are provided which are useful as photocleavable linking groups in solid phase synthesis. Compositions incorporating these linking groups and methods for their use are also described.

Abstract: Hydroxamic acids and hydroxamic acid ethers I and II ##STR1## where Z.sup.1 and Z.sup.2 are --NH --OY, --NR.sup.1 --OY or --OX, where in the case of (I) at least one of Z.sup.1 or Z.sup.2, and in the case of (II) Z.sup.1 is --NH --OY or --NR.sup.1 --OY, andR.sup.1 is C.sub.1 -C.sub.18 -alkyl,X is hydrogen, alkali metal, ammonium or substituted ammonium, andY is hydrogen, alkali metal, ammonium, substituted ammonium or C.sub.1 -C.sub.18 -alkyl, andL is a C.sub.1 -C.sub.100 linker which can also carry oxygen and nitrogen functional groups,with the exception of N,N-bis(carboxymethyl)-2-aminoacetohydroxamic acid.

Abstract: A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d.sub.1 and d.sub.2, X.sub.1, R.sub.1, R.sub.2, R.sub.6, R.sub.3, R.sub.4 and R.sub.5 are as described in the specification; or an analog, pharmaceutically acceptable salt, or derivative of the inhibitor, with the proviso that the inhibitor is not HNBA GBA or Neu5Ac2en. The inhibitor in a composition with a pharmaceutically acceptable carrier. Methods of making a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of inhibiting sialidase and methods of treating and preventing bacterial or trypanosomal infection using the inhibitor.

Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.

Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.

Abstract: A process for preparing substituted aromatic azo compounds is provided which comprises contacting a nucleophilic compound and an azo containing compound in the presence of a suitable solvent system, and reacting the nucleophilic compound and the azo containing compound in the presence of a suitable base and a controlled amount of protic material at a temperature of about 10.degree. C. to about 150.degree. C. in a confined reaction zone wherein the molar ratio of protic material to base is 0:1 to about 5:1. In another embodiment, the substituted aromatic azo compounds are further reacted with a nucleophilic compound in the presence of a suitable solvent system, a suitable base and a controlled amount of protic material at a temperature of about 70.degree. C. to about 200.degree. C. in a confined reaction zone wherein the molar ratio of protic material to base is 0:1 to about 5:1 to produce a substituted aromatic amine.

Abstract: A process for preparing substituted aromatic amines which comprises contacting a nucleophilic compound and a substituted aromatic azo compound in the presence of a suitable solvent system, and reacting the nucleophilic compound and the substituted aromatic azo compound in the presence of a suitable base and a controlled amount of protic material at a temperature of about 70.degree. C. to about 200.degree. C. in a confined reaction zone wherein the molar ratio of protic material to base is 0:1 to about 5:1. In another embodiment, the substituted aromatic amines of the invention are reductively alkylated to produce alkylated diamines or substituted derivatives thereof.

Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H, alkyl, aryl and arylalkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, OCF.sub.3 and SCF.sub.3 with the proviso that the compound of formula I wherein R.sup.1 and R.sup.2 =H, X=Br and Y=Me is excluded;or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxyanthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.