Abstract: The present disclosure relates to processes for the separation of at least one di-carboxylic acid compound and/or at least one mono-carboxylic acid compound from a mixture. The separation processes involve contacting the mixture with an ion exchange medium to cause at least one of the mono- and/or di-carboxylic acid compounds to be retained by the medium, eluting at least one of the mono-carboxylic acid compound or the di-carboxylic acid compound using an eluent to form an eluate, wherein the eluate is enriched in at least one of the mono-carboxylic acid compound or di-carboxylic acid relative to the concentration of such eluted acid in the mixture having contacted the medium and wherein the eluent comprises an organic acid. The process has particular utility in the production of di-carboxylic acid compounds from glucose.

Abstract: This present invention relates to the processes for the purification of succinic acid from a fermentation broth containing ammonium succinate. The process for the purification of succinic acid described in this invention involves the use of ion exchange resins for splitting the ammonium succinate in the fermentation broth. During the passage of the fermentation broth through a cationic ion exchange resin, the ammonium succinate is split into ammonium cation and the succinate anion. The proton on the resin surface is exchanged for the ammonium ions and the succinate anion is reduced to succinic acid with the protons released from the ion exchange resin. The bound ammonium is released from the resin with the addition of a strong acid such as sulfuric acid and thereby the ion exchange resin is regenerated for subsequent use. The ammonium sulfate by-product resulting from the regeneration step of this process can be used as a source of fertilizer.

Abstract: Disclosed are compounds of formulae (I) and (II) and salts, hydrates, or solvates thereof, where R1, R2, R3, R5, and R6 are defined herein, compositions containing these compounds, methods of preparing these compounds, and methods of using these compounds in a variety of applications, such as a surfactant or additive in personal care products.

Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.

Abstract: A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.

Abstract: An amino acid-modified organopolysiloxane is provided. It has an amino acid derivative bonded to at least one silicon atom of the organopolysiloxane segment constituting the backbone of the organopolysiloxane via an amide bond represented by the following general formula (1): wherein X and Y are independently a C1-10 divalent hydrocarbon group; m is an integer of 0 to 4; Ra is hydrogen atom, a monovalent hydrocarbon group containing 1 to 4 carbon atoms, or an organic group represented by the following general formula (2): (wherein Rb is hydrogen atom, a C1-7 monovalent hydrocarbon group, an alkaline metal, or an alkaline earth metal, and Rc is independently hydrogen atom, hydroxy group, or a C1-10 monovalent hydrocarbon group optionally containing oxygen atom, sulfur atom, or nitrogen atom); and Z is an organic group represented by the general formula (2).

Abstract: Proteasome inhibitors (PI) are used for inhibiting the maturation of dendritic cells (DZ) and thus in the treatment or the prophylaxis of allergies, asthma, tissue or transplant rejection or autoimmune diseases. The concentration of the proteasome inhibitors lies preferably in the range of 10 nM to 10 ?M, based on the peripheral blood or the cytoplasm.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

Abstract: The invention pertains to a compound generating an acid of the formula I or II, for instance corresponding sulfonium and iodonium salts, as well as corresponding sulfonyloximes wherein X is CH2 or CO; Y is O, NR4, S, O(CO), O(CO)O, O(CO)NR4, OSO2, O(CS), or O(CS)NR4; R1 is for example C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl, C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, interrupted C2-C18alkyl, interrupted C3-C30cycloalkyl, interrupted C3-C30cycloalkyl-C1-C18alkyl, interrupted C4-C30cycloalkenyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or heteroaryl, all unsubstituted or are substituted; or R1 is NR12R13; R2 and R3 are for example C3-C30cycloalkylene, C3-C30cycloalkyl-C1-C18alkylene, C1-C18alkylene, C1-C10haloalkylene, C2-C12alkenylene, C4-C30cycloalkenylene, phenylene, naphthylene, anthracylene, phenanthrylene, biphenylene or heteroarylene; all unsubstituted or substituted; R4 is for example C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18al

Abstract: The present invention relates to substituted heterocycles, processes for their preparation, and their use in medicaments, especially for the treatment of inflammatory disease, i.e. asthma, or cancer.

Abstract: The present invention relates to an acid salt of tolterodine with superior stabililty and useful as a transdermal drug delivery system. More specifically, the present invention relates to a novel acid salt of tolterodine with superior stabililty to the conventional acid salts of tolterodine, which is useful as a pharmaceutical composition for the treatment of overactive bladder and can be formulated into a transdermal drug delivery system.

Abstract: Gelling agents which contain a specific N-acylamino acid monoamide monoalkyl ester have a melting temperature of about 100° C., are capable of solidifying a wide variety of oily base materials including silicones, and do not cause “sweating” while retaining a practical level of gel strength. When applied to skin, the resulting gels have a good feeling, good spreadability, and good fittability to skin.

Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.

Abstract: The present invention describes therapeutic compositions comprising one or more minerals, including trivalent iron, divalent manganese and salts thereof, suitable in facilitating synthesis and deposition of connective tissue matrix, particularly rich of elastin and collagen, and mitogenic potential in human dermal fibroblasts. It also describes the phenomenon in which stimulation of elastogenesis by arterial SMC associates with a net decrease in proliferation of these cell types. The present invention also describes methods of treatment of human skin fibroblasts and arterial smooth muscle cells. The therapeutic compositions of the present invention comprise one or more of trivalent iron or divalent manganese or salts thereof and may be combined with an elastic tissue digest.

Abstract: The present invention relates to a method for diagnosing a predisposition for diabetes comprising determining at least one metabolite in a test sample of a subject suspected to have a predisposition for diabetes and comparing said at least one metabolite to a reference, whereby a predisposition for diabetes is to be diagnosed. Moreover, the present invention encompasses a collection of metabolites, a data collection comprising characteristic values of metabolites and a storage medium comprising said data collection. Furthermore, the present invention also relates to a system comprising means for comparing characteristic values of metabolites of a sample operatively linked to a data storage medium. Further encompassed by the present invention are diagnostic means comprising at least one metabolite and the use of said at least one metabolite for the manufacture of diagnostic means for diagnosing a predisposition for diabetes.

Abstract: The invention relates to compounds of the formula I where the substituents AA1, AA2, o and R have a meaning indicated in claim 1, and to the salts and solvates and mixtures thereof, to a process for the preparation thereof, preparations and the use thereof.

Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.

Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.

Abstract: Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.

Abstract: The present invention relates to a method of production and the use of a compositional ingredient. Specifically, the present invention relates to hydrosoluble stable organic salts of creatine and pyroglutamic acid. The compositional ingredient may be useful for the regulation of athletic and cognitive functions.

Abstract: The present invention relates to a method of production and the use of a compositional ingredient. Specifically, the present invention relates to hydrosoluble stable organic salts of creatine and pyroglutamic acid. The compositional ingredient may be useful for the regulation of athletic and cognitive functions.

Abstract: A method of manufacturing glimepiride of formula I wherein trans-4-methylcyclohexylamine pivalate of formula VII is reacted, either directly or after conversion to trans-4-methylcyclohexylamine or to its another salt, with an alkyl [4-(2-{[(3-ethyl-4-methyl-2-oxo-2,5-dihydro-1H-pyrrol-1 yl)carbonyl]amino)ethyl)phenyl]-sulfonyl carbamate of general formula IV wherein R is a C1-C5 alkyl, giving glimepiride of formula I, trans-4-Methylcyclohexylamine pivalate of formula VII

Abstract: A lightfast additive and an ink composition including the same include a benzophenone moiety for lightfastness and a moiety for wettability and the ability to stabilize a colorant, wherein the two moieties are covalently bonded. The lightfast additive may exhibit effective ultraviolet (UV) light absorption capacity, effective wettability, and an ability to stabilize a colorant. The ink composition utilizing the light fast additive thus has an improved lightfastness and long-term storage stability.

Abstract: The present invention provides a production method of pyrrolidone carboxylic acid or a salt thereof, which includes bringing glutamic acid or a salt thereof into contact with high-temperature high-pressure water having a temperature of above 100° C. and not higher than 300° C., and a pressure higher than the vapor pressure of water at this temperature. The present invention affords efficient production and supply of pyrrolidone carboxylic acid or a salt thereof from glutamic acid or a salt there.

Abstract: The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.

Abstract: Peptido and peptidomimetic compounds of the formula: wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also provided.

Abstract: The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.

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: Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-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-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.

Abstract: The present invention relates to a novel form of (S)-1-[N2-(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel amorphous form of lisinopril for the treatment of hypertension and other cardiovascular diseases, pharmaceutical compositions containing it as well as processes for the preparation of the novel amorphous form of lisinopril.

Abstract: The invention relates to the use of imino acid conjugates of methylglyoxal for the inhibition and/or treatment of cancer. The invention relates more specifically to the use imino acid conjugates of methylglyoxal for inhibition and/or treatment of cancer of the Colon, Prostate, Larynx, Kidney, Pancreas, Lung, Breast, Intestine, Oral cavity, Ovary, Glioblastoma, and Leukemia. The invention also relates to compositions and methods of inhibiting cancer using imino acid conjugates of methylglyoxal.

Abstract: This invention relates to analogs and peptidomimetics of glycyl-L-prolyl-L-glutamic acid (GPE). In particular, this invention relates to GPE analogs and peptidomimetics that are anti-apoptotic and anti-necrotic, to methods of making them, to pharmaceutical compositions containing them, and to their use.

Abstract: The present invention provides a production method of pyrrolidone carboxylic acid or a salt thereof, which includes bringing glutamic acid or a salt thereof into contact with high-temperature high-pressure water having a temperature of above 100° C. and not higher than 300° C., and a pressure higher than the vapor pressure of water at this temperature. The present invention affords efficient production and supply of pyrrolidone carboxylic acid or a salt thereof from glutamic acid or a salt thereof.

Abstract: The present invention relates to S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine, or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to a method for the preparation of an enantiomerically pure imidazolyl compound of the general formula wherein: n is 0 or 1; m is 1 or 2; R1 is hydrogen, methyl or ethyl; and C* denotes a chiral center; as well as its pharmaceutically acceptable acid addition salt. The invention further relates to a method of racemization and to a new acid addition salt of this formula I compound and D-pyroglutamic acid and to the hydrochloride monohydrate of the compound of formula I.

Abstract: The invention concerns the use of calcium L-pidolate for obtaining an agent improving the quality of eggshells and a composition capable of being administered to laying hens. Said composition is characterized in that it contains as active element for improving the quality of eggshells, in particular firmness and appearance, at least calcium L-pidolate. The invention is applicable to poultry farming.

Abstract: The compound 2-hydroxy-5-oxoproline and analogs thereof may be used to produce an increase in carbon dioxide fixation, growth, dry weight, nutritional value (proteins and amino acids), nodulation and nitrogen fixation and photosynthetically derived chemical energy when applied to plants through their roots and/or through their foliar portions. The present invention includes an essentially quantitative chemical synthesis for this compound which is performed in a single step reaction of Fremy's Salt (potassium nitrosodisulphonate) with either glutamine or 2-pyrrolidone-5-carboxylic acid. Fremy's salt (potassium nitrosodisulphonate) is available commercially, or can be readily synthesized.

Abstract: The invention encompasses a compound having the formula: 1

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-.beta.-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-.beta.-lactones, and analogs thereof and their use as proteosome inhibitors.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## 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 class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: --O--Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.

Abstract: Novel lactacystin derivatives other than lactacystin per se, with superior activity for the genesis of neurites and highly selective toxicity and low cytotoxicity as compared with known lactacystin have been prepared, of the formula ##STR1## wherein R is lower alkoxy, --S--(CH.sub.2).sub.n R.sup.1 or --S--(CH.sub.2) .sub.n --CH(R.sup.2)-(R.sup.3), in which R.sup.1 is branched or straight-chain lower alkyl, hydroxy, carboxyl, lower alkoxycarbonyl, optionally substituted phenyl, substituted or unsubstituted amino or pyridyl, R.sup.2 is substituted or unsubstituted amino, lower alkyl or amino acid residue, R.sup.3 is carboxyl, lower alkoxycarbonyl, lower alkenyloxycarbonyl or amino acid residue, and n is 0-4, or a pharmacologically acceptable salt thereof.

Abstract: The invention relates to a method for the preparation of an enantiomerically pure imidazolyl compound of the general formula ##STR1## wherein n is 0 or 1; m is 1 or 2;R.sub.

Abstract: A process for purifying 1-[N.sup.2 -((S)-ethoxycarbonyl)-3-phenylpropyl)-N.sup.6 -trifluoroacetyl]-1-lysyl-1-proline by extraction and crystallization. The process includes a two step extraction in a two phase aqueous/organic solvent system and crystallization from organic solvent.

Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

Abstract: In a process for manufacturing a humectant with a chemical structure similar to that of natural moisture regulators, residual molasses from sugar beet molasses are treated and the organic acids contained, in particular L-2-pyrrolidone-5-carboxlyic acid and lactic acid, are obtained and then neutralized and concentrated to form a humectant.

Abstract: This invention relates to compounds of structural formula (I) isolated from an aerobic fermentation of Trichoderma viride MF5628, ATCC 74084: ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. These compounds are also potent antifungal agents. Additionally, they inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras and are thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).

Abstract: The present invention relates to a process for the preparation of optically active amino acid amide. L-amino and D-amino acid amides are mixed in the presence of 0.5-4 equivalents of an aldehyde, relative to the quantity of amino acid amide, in the presence of a solvent and water. The mixture is converted in whole or in part by means of an optically active carboxylic acid into a salt of the amino acid amide and the carboxylic acid. A portion mainly consisting of one of the diastereoisomers of that salt is separated from the reaction mixture obtained. Instead of a mixture of L-amino and D-amino acid amides, it is also possible to use a mixture of the Schiff bases of an amino acid amide and an aldehyde, in which case it is not necessary to add extra aldehyde, and the required quantity of water amounts to at least 1 equivalent relative to the quantity of Schiff base. With this process, a high yield of optically active amino acid amide or the corresponding amino acid is rapidly obtained.