Abstract: The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having ? 4 integrin inhibiting activity.
Abstract: There is provided an infusion solution for peripheral intravenous administration comprising a multichamber vessel constructed in a connectable manner, which separately houses a sugar solution containing sugars, electrolytes and vitamin B1, and an amino acid solution containing amino acids, electrolytes and a sulfite, whereby the vitamin B1 and amino acids are stably maintained. In the infusion solution for peripheral intravenous administration, the sugar solution contains calcium gluconate, contains no greater than 1.4 g/L sodium lactate, has a pH of 4.0-4.7 and has a titratable acidity of 2-4, the amino acid solution contains 4.0-8.0 g/L sodium lactate, contains no calcium gluconate, has a pH of 6.8-7.2, contains free L-cysteine as cysteine and contains 0.05-0.2 g/L sodium hydrogen sulfite, and after the sugar solution and amino acid solution have been mixed, the infusion solution has a pH of 6.5-7.1 and a titratable acidity of 5-10.
Abstract: The present invention provides a small-sized preparation that is easy to take, containing 26% or more of nateglinide and 28% or more of at least one disintegrant selected from the group consisting of carmellose or salts thereof, sodium carboxymethyl starch, croscarmellose sodium, crospovidone, partly pregelatinized starch and low-substituted hydroxypropyl cellulose, based on the total mass of the preparation. The preparation of the present invention has high contents of nateglinide, which can be absorbed immediately to exhibit a hypoglycemic action.
Abstract: The present invention provides an acylamide compound of the following formula (1), prodrugs thereof, or pharmaceutically acceptable salts thereof; and an adiponectin inducer or secretagogue, therapeutic agent of metabolic syndromes, therapeutic agent of hypoadiponectinemia, therapeutic agent of hyperlipemia, preventive/therapeutic agent of diabetes, improving agent of impaired glucose tolerance, improving agent of insulin resistance, enhancing agent of insulin sensitivity, therapeutic agent of hypertension, preventive/therapeutic agent of vascular disorders, an anti-inflammatory agent, therapeutic agent of hepatic inflammation, therapeutic agent of fatty liver, therapeutic agent of hepatic fibrosis, therapeutic agent of liver cirrhosis, preventive/therapeutic agent of non-alcoholic/nonviral steatohepatitis (NASH) or non-alcoholic/nonviral fatty liver disease (NAFLD), or therapeutic agent of obesity, each of which has the above compounds as an active ingredient.
Abstract: The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly ?-type, ?-type, ?-type, ?-type, and ?-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.
Abstract: A processed meat food or a processed fishery food having improved physical properties and taste can be obtained by contacting meat or fish with a transglutaminase and an enzyme having a saccharide transfer activity for converting an ?-1,4 bond to an ?-1,6 bond in the process for producing the processed meat food or the processed fishery food.
Abstract: It is intended to provide an assay method whereby the activity of a lipid-modifying enzyme can be conveniently measured over a wide range and a drug capable of controlling a lipid-modifying enzyme with the use of this assay method. The above problem can be solved by, for example, a method of measuring the activity of a lipid-modifying enzyme which comprises the steps of (I) preparing a lipid micelle containing a biotinylated lipid and a substrate for the lipid-modifying enzyme; (II) bringing the lipid micelle prepared in the above step (I) into contact with the lipid-modifying enzyme; and (III) evaluating the activity of the lipid-modifying enzyme by applying an evaluation method using the proximity effect to the product obtained in the above step (II).
Abstract: The present invention relates to an ether derivative represented by the formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description, and an ether derivative represented by the formula (III), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof wherein each symbol is as defined in the description; a pharmaceutical composition containing the ether derivative; and a package containing the pharmaceutical composition and a description of use thereof. A pharmaceutical composition of the present invention, which contains this compound of the present invention has a superior anti-inflammatory and analgesic activity and is useful as various pharmaceutical agents such as an anti-inflammatory agent, an analgesic, a therapeutic agent for inflammatory bowel disease, a therapeutic agent for pollakiuria and/or incontinentia, a therapeutic agent for asthma and the like.
Abstract: The object of the present invention is to provide PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity. The present invention provides PPAR activity regulators which comprise an acylamide compound having the specific structure, prodrugs thereof, or pharmaceutically acceptable salts thereof.
Abstract: The present invention relates to a process for secretory production of a foreign protein, in particular, transglutaminase by a coryneform bacterium. According to the present invention, a process is provided for the secretory production of a foreign protein, in particular, transglutaminase, by making a coryneform bacterium to produce an industrially useful foreign protein, in particular, transglutaminase and efficiently release the product extracellularly (i.e., secretory production).
Abstract: An Escherichia bacterium (1) which harbors dihydrodipicolinate synthase of which feedback inhibition by L-lysine is desensitized and aspartokinase of which feedback inhibition by L-lysine is desensitized, (2) in which intracellular activity of dihydrodipicolinate reductase is enhanced, and (3) in which a diaminopimelate dehydrogenase gene is introduced or intracellular activities of tetrahydrodipicolinate succinylase and succinyl diaminopimelate deacylase are enhanced, wherein intracellular activity of aspartate-semialdehyde dehydrogenase or phosphoenolpyruvate carboxylase is enhanced, is cultured in a suitable medium to produce and accumulate L-lysine in culture, and the L-lysine is collected from the culture.
Abstract: L-Glutamic acid is produced by culturing a coryneform bacterium having L-glutamic acid producing ability, in which trehalose synthesis ability is decreased or deleted by, for example, disrupting a gene coding for trehalose-6-phosphate synthase, a gene coding for maltooligosyltrehalose synthase, or both of these genes to produce and accumulate L-glutamic acid in the medium, and collecting the L-glutamic acid from the medium.
Type:
Application
Filed:
April 19, 2007
Publication date:
May 20, 2010
Applicant:
Ajinomoto Co., Inc.
Inventors:
Hiromi Ohtaki, Jun Nakamura, Hiroshi Izui, Tsuyoshi Nakamatsu
Abstract: A method for conveniently detecting binding between the von Willebrand factor and glycoprotein Ib and a means to be used therein. The von Willebrand factor fixed in a reactor immobilized in a reaction vessel in the presence of bottrocetin is bound to a chimeric protein constructed by fusing the carboxyl terminal of a partial protein containing the von Willebrand factor-binding site of glycoprotein Ib with the amino terminal of the Fc region of an immunoglobulin molecule. Then the Fc region of the above immunoglobulin molecule is detected to thereby detect the binding between the von Willebrand factor and the glycoprotein Ib or inhibition of this binding.
Abstract: The present invention provides a glucose decomposition-suppressed solid preparation for dialysis among powdery or granular preparations for dialysis containing acetate-free solid organic acids as pH adjusting agents. The present invention provides the solid preparation for dialysis containing electrolytes, glucose and pH adjusting agents characterized in that solid organic acids containing reduced amount of microparticles are used, and more specifically, characterized in that solid organic acids whose 20 or less percent of particles are 250 ?m or less in diameter, or solid organic acids whose 10 or less percent of particles are 150 ?m or less in diameter, are used. Preferably, the solid organic acid contained therein is citric acid.
Abstract: The present invention relates to a pharmaceutical composition useful for preventing/treating pain, which comprises combination of gabapentin or pregabalin, or pharmaceutically acceptable salts thereof and N-type calcium channel antagonists or pharmaceutically acceptable salts thereof such as a compound having the following structure.
Abstract: The present invention describes the production of L-tyrosine by culturing in a medium an Escherichia bacterium which has L-tyrosine-producing ability and which carries a mutant prephenate dehydrogenase which is desensitized to feedback inhibition by L-tyrosine, producing and accumulating L-tyrosine in the medium or in the bacterial cells, and collecting L-tyrosine from the medium or the bacterial cells.
Type:
Grant
Filed:
December 17, 2008
Date of Patent:
May 4, 2010
Assignee:
Ajinomoto Co., Inc.
Inventors:
Atsuko Takai, Ranko Nishi, Yuji Joe, Hisao Ito
Abstract: The present invention relates to processes of producing glutamic acid compounds, for example, monatin, which are useful as, for example, production intermediates for sweetener or pharmaceutical products.
Abstract: Compounds represented by formula (1) and pharmaceutically acceptable salt thereofs: wherein each symbol is as defined in the specification, are useful as inhibitors of an activated blood coagulation factor X. Compositions which contain, as an active ingredient, an FXa selective low-molecular weight FXa inhibitor having a short serum half-life are particularly useful as anticoagulants for an extracorporeal blood circuit.
Abstract: The present invention provides a neutral metalloprotease from actinomycetes which selectively cleaves a pro-structure part of a microbial protransglutaminase and a gene encoding said neutral metalloprotease. An active microbial transglutaminase having the pro-structure part cleaved can be obtained by culturing a microorganism into which a gene encoding the neutral metalloprotease from actinomycetes according to the present invention has been introduced, where by producing the neutral metalloprotease from actinomycetes, and reacting it on a microbial protransglutaminase.