Abstract: Liquid formulations of imidoalkanepercarboxylic acids, in the form of aqueous dispersions comprising, in percentages by weight relative to the total weight of the composition: A) from ?7% to 40% and preferably from 10% to 20% of imidoalkanepercarboxylic acids having the general formula (I), the said imidoalkanepercarboxylic acids being in the ? form and having a dissolution time, determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., of not more than 5 minutes when determined at 40° C. or 15 minutes when determined at 18° C., for an amount of dissolved acid equal to 99% of the theoretical amount; B) from 0.001% to 0.9% of a nonionic surfactant; the said dispersions having a viscosity of not more than 2000 mPa·sec at 25° C. by applying a shear rate of 20 s?1; in which the dissolution time of the component A), determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., is not more than 5 minutes when determined at 40° C.

Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.

Abstract: The invention provides a process for preparing esters from formates and olefinically unsaturated compounds with catalysts based on palladium compounds. In addition, the invention discloses a polyphasic reaction mixture and nonyl methyl ester mixtures prepared by the process according to the invention.

Abstract: Disclosed are novel cross-linkable end-cappers for oligo- and polyamides. End-capped oligo- and polyamides comprising such an end-capper may be cured at a lower temperature compared to oligo- and polyamides end-capped with PEPA.

Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.

Abstract: A radiation-sensitive resin composition includes a first polymer including an acid-labile group, an acid generator to generate an acid upon exposure to radiation, and a second polymer including a fluorine atom and a functional group shown by a general formula (x). The second polymer has a fluorine atom content higher than a fluorine atom content of the first polymer. R1 represents an alkali-labile group. A represents an oxygen atom, —NR?—, —CO—O—# or —SO2—O—##, wherein the oxygen atom represented by A is not an oxygen atom bonded directly to an aromatic ring, a carbonyl group, or a sulfoxyl group, R? represents a hydrogen atom or an alkali-labile group, and “#” and “##” each indicate a bonding hand bonded to R1.

Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.

Abstract: The present invention is directed to methods for oxidizing internal olefins to ketones. In various embodiments, each method comprising contacting an organic substrate, having an initial internal olefin, with a mixture of (a) a biscationic palladium salt; and (b) an oxidizing agent; dissolved or dispersed in a solvent system to form a reaction mixture, said solvent system comprising at least one C2-6 carbon nitrile and optionally at least one secondary alkyl amide, said method conducted under conditions sufficient to convert at least 50 mol % of the initial internal olefin to a ketone, said ketone positioned on a carbon of the initial internal olefin. The transformation occurs at room temperature and shows wide substrate scope. Applications to the oxidation of seed oil derivatives and a bioactive natural product are described.

Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract: The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.

Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.

Abstract: The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.

Abstract: Disclosed are novel cross-linkable end-cappers for oligo- and polyamides. End-capped oligo- and polyamides comprising such an end-capper may be cured at a lower temperature compared to oligo- and polyamides end-capped with PEPA.

Abstract: The present invention provides a production method of optically active 3-substituted-3-formyl-2-hydroxypropanoic acid compound (4), which includes a step of reacting glyoxylic acid compound (1-1) or (1-2) with aldehyde (2) in the presence of optically active pyrrolidine compound (3); wherein each symbol is as defined in the specification.

Abstract: The embodiments described herein provide a reduction of an aldehyde or a ketone, such as a Meerwein-Ponnorf-Verley (MPV) reaction of an aldehyde or ketone. In some embodiments, the reaction occurs in the presence of Al[OC(CH3)3]. In some embodiments, the reaction occurs in the presence of an aprotic solvent. In some embodiments, the aldehyde or ketone is an amino aldehyde or an amino ketone wherein the amine is group is protected such that the nitrogen of the amine has no proton. Other embodiments related to compositions and compounds related to the reduction reaction, or to the preparation or use of the aldehyde, the ketone, or the resulting alcohol.

Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.

Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:

Abstract: A radiation-sensitive resin composition includes a first polymer including an acid-labile group, an acid generator to generate an acid upon exposure to radiation, and a second polymer including a fluorine atom and a functional group shown by a general formula (x). The second polymer has a fluorine atom content higher than a fluorine atom content of the first polymer. R1 represents an alkali-labile group. A represents an oxygen atom, —NR?—, —CO—O—# or —SO2—O—##, wherein the oxygen atom represented by A is not an oxygen atom bonded directly to an aromatic ring, a carbonyl group, or a sulfoxyl group, R? represents a hydrogen atom or an alkali-labile group, and “#” and “##” indicates a bonding hand bonded to R1.

Abstract: The present invention relates to phthalimide derivatives of non-steroidal and/or TNF-? modulating anti-inflammatory compounds as well as the process of obtaining the so-called derivatives, pharmaceutical compositions containing such derivatives and their uses, including use in the treatment of inflammatory diseases, especially those related to chronic inflammatory processes, such as rheumatoid arthritis and intestinal inflammatory diseases (for instance, Chron's disease) and the use of the referred to pharmaceutical compositions as antipyretic, analgesic and platelet antiaggregating medications.

Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.

Abstract: The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.

Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.

Abstract: The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.

Abstract: It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.

Abstract: The present invention relates to functionalizing a surface of an organic material. For example, surfaces of materials having C—H bonds, such as polymers having C—H bonds, can be functionalized. In certain embodiments, a heterobifunctional molecule having a photoactive anchor, a spacer, and a terminal functional group is applied to the surface of an organic material that contains one or more C—H bonds. The heterobifunctional molecule can be bound to any surface having C—H bonds as the photoactive anchor can react with C—H bonds upon irradiation. The terminal functional group has a “click” functionality which can be utilized to functionalize the surface of the organic material with any desired functionalizing moiety having the orthogonal click functionality.

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.

Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the ? 4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which ? 4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: Liquid formulations of imidoalkanepercarboxylic acids, in the form of aqueous dispersions comprising, in percentages by weight relative to the total weight of the composition: A) from ?7% to 40% and preferably from 10% to 20% of imidoalka-nepercarhoxylic acids having the general formula (I), the said imidoalkanepercarboxylic acids being in the ? form and having a dissolution time, determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., of not more than 5 minutes when determined at 40° C. or 15 minutes when determined at 18° C., for an amount of dissolved acid equal to 99% of the theoretical amount; B) from 0.001% to 0.9% of a nonionic surfactant; the said dispersions having a viscosity of not more than 2000 mPa·sec at 25° C. by applying a shear rate of 20 s?1; in which the dissolution time of the component A), determined via the test of the rate of dissolution at a temperature of 40° C. or 18° C., is not more than 5 minutes when determined at 40° C.

Abstract: A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; R1 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; R2 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; R3 is hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R4-R7, is used to represent groups R4, R5, R6 and R7 which are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, h

Abstract: Process for obtaining dilute aqueous solutions containing an amount of <7% by weight, expressed as a percentage by weight of imidoalkanepercarboxylic acids, starting with concentrated aqueous compositions of the said peracids in the ? form, the said concentrated compositions being obtained from the imidoalkanepercarboxylic acids in the ?-crystal form, the said process comprising the following steps: I) dilution of the concentrated aqueous composition of imidoalkanepercarboxylic acids (C) with an aqueous solution (D) having a pH of between 2 and 5, in a (C):(D) proportion, expressed in parts by weight, of between 0.1:10 and 10:0.2, working at temperatures of between 4° C. and 30° C.

Abstract: Imidoalkancarboxylic acids of formula: are described, wherein A, X and M are as defined in the application, said acids being in a crystalline form which in contact with water gives rise to crystals having sizes lower than 30 micron.

Abstract: An 1-amido-3-(2-hydroxyphenoxy)-2-propanol derivative represented by the following formula (1), wherein cycle A may have further 1 to 4 substituents, and said substituent means a substituent selected from the group consisting of saturated or unsaturated C1-4 alkyl group, aralkyl group in which alkyl moiety has 1 to 4 carbon atoms, aryl group, halogen atom, halogenated C1-4 alkyl group, C2-5 alkanoyl group, mono or dialkylcarbamoyl group in which alkyl moiety has 1 to 4 carbon atoms, cyano group and nitro group, and the substituents at positions 3 and 6, or at positions 4 and 5 on the cycle A are different each other. Other ring may be fused at positions 3 and 4, or at positions 5 and 6 on the cycle A to form a condensed polycyclic hydrocarbon with the cycle A. R1 is alkanoyl group or aroyl group, and R2 is hydrogen atom, alkanoyl group or aroyl group, or R1 and R2 may be combined together with the N atom to form a cyclic imido group, which is useful as an intermediate of medicines, etc.

Abstract: The invention relates to compounds for the modulation of the glycolysis enzyme complex and of the transaminase complex, pharmaceutical compositions containing such compounds as well as uses of such compounds for preparing pharmaceutical compositions for treating various diseases.

Abstract: A compound represented by a general formula (Ia) or (Ib) and a stereo-selective preparation method thereof using a carbonyl reductase which is separated from Kluyveromyces marxianus. The compound can be prepared by reduction of substituted ?-keto ester and can be used as an intermediate in preparing ?-lactam group antibiotics.

Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.

Abstract: Amlodipine and related analogues thereof are prepared by the following general reaction scheme: R1 and R2 each independently represent a C1-C4 alkyl group. The process provides for the formation of compounds of formula (1) in good yield and purity. Further, the compounds of formula (1) can be used as calcium channel blockers or as reference standards or reference markers for checking the purity of amlodipine.

Abstract: Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2-Phthalimido-3-(3?,4?-dimethoxyphenyl)propane.

Abstract: The invention relates to compounds for the modulation of the glycolysis enzyme complex and of the transaminase complex, pharmaceutical compositions containing such compounds as well as uses of such compounds for preparing pharmaceutical compositions for treating various diseases.

Abstract: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: The present invention provides a thiocarbonylthio compound represented by formula (I) Wherein n is an integer of 0 to 3; R1 is alkyl, haloalkyl, alkenyl, aryl, alkylaryl, haloalkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, alkoxyaryl, alkyl sulfide, or alkylsilyl; R2 and R3 are independently H, alkyl, haloalkyl, alkenyl, aryl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, alkyl sulfide, or alkylsilyl; R4 and R5 are independently H, alkyl, haloalkyl, alkenyl, aryl, alkylaryl, arylalkyl, aminoalkyl, alkylamino, alkoxy, alkyl sulfide, or alkylsilyl, or R4 and R5 link together with the carbon atoms to which they are attached to form a ring system; and Y is O or S. The thiocarbonylthio compound can be used in a living free radical polymerization to obtain a polymer with high conversion and low polydispersity.

Abstract: A compound represented by a genera formula (Ia) or (Ib) and a stereo-selective preparation method thereof using a carbonyl reductase which is separated from Kluyveromyces marxianus. The compound can be prepared by reduction of substituted &bgr;-keto ester and can be used as an intermediate in preparing &bgr;-lactam group antibiotics.

Abstract: Novel imides are inhibitors of tumor necrosis factor &agr; and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-Phthalimido-3-(3′,4′-dimethoxyphenyl)propane.

Abstract: 1-Oxo- and 1,3-dioxoisoindolines substituted in the 4- or 5-position of the indoline ring reduce the levels of inflammatory cytokines such as TNF&agr; in a mammal. A typical embodiment is 4-(4-amino-1,3-dioxoisoindolin-2-yl)-4-carbamoylbutanoic acid.

Abstract: The present invention relates to a process for reacting &agr;-aminoaldehyde derivatives having a sterically bulky amino group which are commercially available with a metal cyanide in the presence of an acid chloride, an acid anhydride or the like to synthesize 3-amino-2-hydroxybutyronitrile derivatives in high yields and high erythro selectivity. When optically active &agr;-aminoaldehyde derivatives are used, racemization hardly occurs during the reaction, and the desired products are obtained in high optical purity.

Abstract: Novel herbicidal compounds, compositions containing them, and methods for their use in controlling weeds are disclosed. The novel herbicidal compounds are represented by formula I: where J is a 1-substituted-6-trifluoromethyl-2,4-pyrimidinedione-3-yl, a 1-substituted-6-trifluoromethyl-1,3,5-triazine-2,4-dion-1-yl, a 3,4,5,6-tetrahydrophthalimid-1-yl, a 4-difluoromethyl-4,5-dihydro-3-methyl-1,2,4-triazol-5(1H)-on-1-yl, a 5,6,7,8-tetrahydro-1H,3H-[1,3,4]thiadiazolo[3,5-a]pyridazineimin-1-yl, or a 1,6,8-triazabicyclo[4.3.0]-nonane-7,9-dion-8-yl ring attached at the 7 position of a benzofuran, benzoxazole, indole, 2,3-dihydrobenzimidazole or benzimidazole, and X is selected from hydrogen, halogen, cyano, nitro, and amino. Preferred R groups are optionally substituted alkyl groups.

Abstract: The level of an unsaturated cyclic imine (I) of the formula (I) where R1 is alkenyl having 3, 4, 5, 6, 7, 8, 9, 10, 11 carbon atoms belonging to the ring system, in a mixture comprising hexamethylenediamine and an imine (I) is reduced by electrochemical conversion of an imine (I) in a mixture comprising hexamethylenediamine and an imine (I) in the presence of solvated protons into a saturated cyclic amine of the formula (II)

Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.

Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.

Abstract: A reaction for eliminating a functional group alpha to a carbonyl group. The reaction can be used to dehydrate a compound having an alcohol group alpha to a carbonyl group by reacting the compound in a non-aqueous non-polar solvent in the presence of an effective amount of a transition metal salt, such as zinc chloride, such that the alcohol group is dehydrated. This Nohr-MacDonald Elimination Reaction produces a light stable compound, which can be added to compositions for light stabilization of a colorant. The modified compound may be combined with a wave-length selective sensitizer.