A two-step type automatic injection device including a means of automatically subcutaneously administering a drug solution with pressing a pressing member provided at one of end portions against an administration site, the automatic injection device including a means of preventing or controlling from placement of a finger on an end portion thereof. The automatic injection device of the present invention is very useful in pharmaceutical industries.
The purpose of the present invention is to provide a new method for producing a compound encoded by an oligonucleotide. Provided according to the present invention is a method for producing a compound encoded by an oligonucleotide, the method including phosphodiester bonding of oligonucleotide chains to each other by chemical ligation under prescribed conditions.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
C40B 50/10 - Liquid phase synthesis, i.e. wherein all library building blocks are in liquid phase or in solution during library creationParticular methods of cleavage from the liquid support involving encoding steps
A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.
A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.
C07D 417/08 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.
A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.
Provided are: a composition that can be used as a calibrator when measuring the activity or mass of autotaxin contained in a human specimen or the like; a method of using the composition; and the like. This calibrator for an autotaxin measurement reagent comprises: autotaxin; and serum and/or blood plasma. The calibrator further comprises a sugar alcohol. This calibration method for an autotaxin measurement reagent comprises: measuring autotaxin contained in the calibrator using the autotaxin measurement reagent.
A medicament for therapeutic treatment and/or improvement of a sepsis patient comprising thrombomodulin as an active ingredient, which is for administration to the patient, whose value of International Normalized Ratio (INR) is more than 1.4 immediately before the administration.
The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
C07D 215/06 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
9.
METHOD FOR MEASURING PYROPHOSPHORIC ACID OR PHOSPHORIBOSYL PYROPHOSPHATE, MEASUREMENT COMPOSITION AND REAGENT KIT FOR MEASURING SAME, AND AMPLIFICATION METHOD THEREOF
Provided are a method for measuring pyrophosphoric acid or phosphoribosyl pyrophosphate, said method achieving a high sensitivity, enabling detection with a general-purpose device and being easy to operate, a measurement composition and a reagent kit for measuring the same, and an amplification method thereof. The method for measuring pyrophosphoric acid (PPi) or phosphoribosyl pyrophosphate (PRPP) comprises the following steps (1) to (3). (1) A step for, in the presence of hypoxanthine-guanine phosphoribosyltransferase which catalyzes the forward and reverse reactions to produce PPi from PRPP and vice versa, contacting substrate A for the forward reaction and substrate B for the reverse reaction with a sample to perform the enzymatic cycling reaction of formula (I). (2) A step for detecting the variation of a signal corresponding to at least one of the variations of substrate A, compound A' formed by the action of substrate A, substrate B, and compound B' that is a compound different from substrate A and formed by the action of substrate B. (3) A step for calculating the amount of PPi or PRPP on the basis of the variation of the signal thus detected.
C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
C12N 9/06 - Oxidoreductases (1.), e.g. luciferase acting on nitrogen containing compounds as donors (1.4, 1.5, 1.7)
C12P 3/00 - Preparation of elements or inorganic compounds except carbon dioxide
C12Q 1/32 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase involving dehydrogenase
G01N 31/00 - Investigating or analysing non-biological materials by the use of the chemical methods specified in the subgroupsApparatus specially adapted for such methods
The present invention addresses the problem of providing a method for producing nicotinamide mononucleotide, that produces nicotinamide mononucleotide using a single enzyme and using nucleoside monophosphate, pyrophosphate, and nicotinamide as starting materials. This problem is solved by a nicotinamide mononucleotide production method that includes at least the following steps 1) and 2): 1) a first step of producing phosphoribosyl diphosphate by the action of substantially one enzyme on nucleoside monophosphate and pyrophosphate; and 2) a second step of producing nicotinamide mononucleotide by the action of only substantially the aforementioned one enzyme on nicotinamide and the phosphoribosyl diphosphate that is the product of the first step.
A two-step type automatic injection device including a means of automatically subcutaneously administering a drug solution with pressing a pressing member provided at one of end portions against an administration site, the automatic injection device including a means of preventing or controlling from placement of a finger on an end portion thereof. The automatic injection device of the present invention is very useful in pharmaceutical industries.
NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGY (Japan)
ASAHI KASEI PHARMA CORPORATION (Japan)
Inventor
Yoshida, Keitaro
Yasutake, Yoshiaki
Tamura, Tomohiro
Konishi, Kenji
Sakasegawa, Shin-Ichi
Muramatsu, Shuji
Abstract
A method for producing a protein encoded by a target gene, said method comprising a step for expressing the target gene in a bacterium belonging to the genus Burkholderia which does not have one or more genes selected from the group consisting of BSFP_068740, BSFP_068730 and BSFP_068720, or in which the expression of the gene(s) or the expression of protein(s) encoded by the gene(s) is inhibited.
Provided are: a compound of general formula (1) which has IRAK-4 inhibitory activity and is useful as an active ingredient of a drug for preventing and/or treating a disease related to IRAK-4 inhibition; or a salt thereof.
This compound, or salt thereof, is represented by general formula (1), exhibits excellent IRAK-4 inhibitory activity and is useful as an active ingredient of a medicine for preventing and/or treating a disease which pertains to IRAK-4 inhibition.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
Provided is a compound represented by general formula (1) or a salt thereof, the compound or the salt thereof having excellent IRAK-4 inhibitory activity and being useful as an active ingredient of a drug for preventing and/or treating a disease relating to IRAK-4 inhibition.
The present invention provides a method for assisting a prediction of how likely a shunt trouble occurs, comprising a step of determining that the shunt trouble likely occurs, when a mevalonic acid concentration in a sample derived from a hemodialyzed patient is equal to or more than a preset cutoff value or increases with time.
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
18.
STABLE LIQUID PHARMACEUTICAL PREPARATION CONTAINING TERIPARATIDE OR SALT THEREOF
This liquid pharmaceutical preparation contains Component 1 and Component 2, and has a pH greater than 5.0 and less than or equal to 6.0. Component 1) teriparatide or a salt thereof; Component 2) a component that satisfies all of conditions 1)-3) below: Condition 1) being a pharmaceutical additive Condition 2) being an organic acid or inorganic acid (acids a) or a salt of these, wherein none of the acids a have a pKa in the pH range 4.0-6.0 and at least one of the acids a has a pKa of less than 4.0 Condition 3) the molecular weight of the acids a being in the range 70-180. The liquid pharmaceutical preparation is stable over a long time, and is extremely useful in the pharmaceutical industry.
[Problems] To provide a method for treating and/or preventing osteoporosis with teriparatide or a salt thereof, the method having excellent safety and/or efficacies.
[Solving Means] A method for treating and/or preventing osteoporosis in which teriparatide or a salt thereof is an active ingredient, including administering teriparatide or a salt thereof in a unit dose of 28.2 μg at a frequency of twice a week.
According to the present invention, a liquid pharmaceutical preparation containing teriparatide or a salt thereof having excellent physical properties, the liquid pharmaceutical preparation containing teriparatide or a salt thereof, and at least one or more members of inorganic salts and/or organic salts is provided.
4 receptor agonist activity, and a medicament containing the compound or a salt thereof as an active ingredient, which can be used for promotion of osteogenesis, therapeutic treatment and/or promotion of healing of fracture and the like.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 41/00 - Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
iii: an electric charge of each ion (wherein the term "each ion" refers to each of ions dissolved and ionized in the water-based pharmaceutical preparation). According to the method of the present invention, a liquid pharmaceutical preparation having excellent shaking stability can be provided, which is extremely useful in the pharmaceutical industry.
The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
C07D 215/06 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
Provided is a two-step type automatic injection device which comprises a means for automatically subcutaneously administering a liquid medicine by pressing a pressing part that is provided on one end against an administration site, the automatic injection device including a means for preventing or suppressing placing fingers on the end of the automatic injection device. This automatic injection device is very useful in the pharmaceutical industry.
A method for preparing a sterile injectable agent containing teriparatide or a salt thereof through an aseptic operation technique includes a step for carrying a package, in which an injection container containing no therapeutic agent is stored, into an apparatus or system having an aseptic operation zone, wherein the outer surface of the package is decontaminated with hydrogen peroxide or alcohol. In the method for preparing a sterile injectable agent according to the present invention, the sterile injectable agent thus prepared has high quality and can be stably preserved after preparation. The present invention is highly useful in pharmaceutical industries, for example, in the field of osteoporosis treatment.
A61K 38/29 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
26.
GLYCOSYLATED PROTEIN ASSAY REAGENT CONTAINING PROTEASE STABILIZER INCREASING REDOX POTENTIAL OF FERROCYANIDE, METHOD FOR ASSAYING GLYCOSYLATED PROTEIN, METHOD FOR PRESERVING GLYCOSYLATED PROTEIN ASSAY REAGENT, AND METHOD FOR STABILIZING GLYCOSYLATED PROTEIN ASSAY REAGENT
Provided is a glycosylated protein assay reagent containing at least Trinder reagent, 4-Aminoantipyrine, a protease, a protease stabilizer, and a ferrocyanide, wherein at least the Trinder reagent is included in a Trinder reagent-containing partial composition, at least the 4-Aminoantipyrine is included in a 4-Aminoantiyrine-containing partial composition, the protease stabilizer is a stabilizer that increases the redox potential of the ferrocyanide to more than 0.058 V when the ferrocyanide is mixed with the protease stabilizer, and the redox potential is determined in a reaction system that contains the protease stabilizer and the ferrocyanide and does not contain the glycosylated protein.
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
27.
Tetrahydroquinoline derivatives as P2X7 receptor antagonists
The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
C07D 215/06 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
4 receptor agonist activity, and a medicament containing the compound or a salt thereof as an active ingredient, which can be used for promotion of osteogenesis, therapeutic treatment and/or promotion of healing of fracture and the like.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 41/00 - Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
A liquid pharmaceutical preparation for subcutaneous administration in human containing 28.2 μg of teriparatide or a salt thereof (Component 1) in a unit dose in terms of teriparatide, wherein the Component 1 concentration is from 80 to 240 μg/mL. This liquid pharmaceutical preparation is excellent in the viewpoint of pharmacokinetics.
[Problem] To provide a method for treating and/or preventing osteoporosis with teriparatide or salt thereof and having excellent safety and/or efficacy. [Solution] Provided is a method for treating and/or preventing osteoporosis by employing teriparatide or salt thereof as an active ingredient, wherein teriparatide or salt thereof is administered twice a week in a unit dose of 28.2 μg.
A drug for treating and/or improving a septicemia patient, the drug including thrombomodulin as an active ingredient, wherein the drug is administered to the patient having an international standard ratio (INR) value greater than 1.4 immediately before administration.
The present invention pertains to an enzymatic measurement method and a reagent for enzymatic measurement. The enzymatic measurement method comprises a step for contacting a short-chain fatty acid having 3-6 carbon atoms in a sample with adenosine triphosphate and butyrate kinase to form adenosine diphosphate and then measuring the thus formed ADP. The reagent for enzymatic measurement comprises butyrate kinase and adenosine triphosphate.
C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
C12Q 1/32 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase involving dehydrogenase
Provided is a method for assisting the prediction of the likelihood of the occurrence of a shunt trouble, said method comprising a step for, when the mevalonic acid concentration in a sample derived from a patient undergoing hemodialysis is equal to or higher than a preset cutoff value or the mevalonic acid concentration increases with time, then predicting that the shunt trouble highly likely occurs.
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
G01N 33/49 - Physical analysis of biological material of liquid biological material blood
34.
Medicament for mitigating conditions and/or suppressing onset of peripheral neuropathy induced by anti-malignant tumor agent
An object of the present invention is to provide an effective and safe medicament having effects for mitigating conditions and/or suppressing onset of a peripheral neuropathy induced by administration of an anti-malignant tumor agent, oxaliplatin, in a human cancer patient receiving an anti-malignant tumor treatment with oxaliplatin. There is provided a medicament for mitigating conditions and/or suppressing onset of a peripheral neuropathy induced by oxaliplatin in an anti-malignant tumor treatment consisting of repetition of a single cycle comprising intravenous administration of oxaliplatin to a human cancer patient and following drug withdrawal, which contains thrombomodulin for intravenously administering 0.06 mg/kg of thrombomodulin once per said single cycle of the treatment on the first day of each said cycle as an active ingredient.
This medication is a medication for alleviating the symptoms of peripheral neuropathy caused by oxaliplatin and/or suppressing the onset of peripheral neuropathy, in a treatment that sets the intravenous administration of oxaliplatin to a human cancer patient and the withdrawal of the administration as one cycle and repeats the one cycle, and contains 0.06 mg/kg of thrombomodulin to be intravenously administered once per cycle on the first day of each cycle of the treatment as an active ingredient.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
Provided is a preparation having a reduced N-formylpiperidine content and/or rarely undergoing the collapse or shrinkage of a lyophilized cake thereof. A lyophilized preparation which is sealed with a rubber plug, is packed in a medical-use container, contains teriparatide acetate salt as an active ingredient, and further contains at least one component selected from components (1) to (4): (1) sodium glutamate or a hydrate thereof; (2) succinic acid; (3) sorbitol; and (4) sodium acetate or a hydrate thereof.
A61K 38/29 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
A61J 1/05 - Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids
A61K 9/19 - Particulate form, e.g. powders lyophilised
Provided are a novel compound which is represented by general formula (1) and which has excellent agonistic activity on EP4 receptors, or a salt thereof, and a medicine that contains the compound or a salt thereof as an active ingredient, and that can be used for promotion of osteogenesis or treatment and/or promotion of healing of bone fracture, or the like.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/5395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
An object of the present invention is to provide a method of measuring a glycated-albumin (GA) value traceable to a certified GA value conveniently at a low cost in a short period of time. A method of measuring a GA value traceable to the certified GA value includes the following steps: A1) determining Regression equation III by steps including the following b), c), and e0) to h); b) determining a GA concentration [L] (A) of two or more GA certified reference materials having respectively different certified GA values; c) measuring a GA-derived absorbance (D) of the two or more GA certified reference materials; e0) creating Linear equation II0 having an intercept of zero; f) determining two or more GA concentrations[P] (E) proportionate to the GA-derived absorbance (D) according to Equation II0; g) determining two or more GA values (F); and h) creating Regression equation III.
The present invention provides, as a liquid pharmaceutical preparation of teriparatide or a salt thereof and having excellent physical properties, a liquid pharmaceutical preparation containing teriparatide or a salt thereof and at least one inorganic salt and/or organic salt.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
This liquid pharmaceutical preparation for subcutaneous administration in humans contains 28.2 µg of teriparatide or salt thereof (component 1) in terms of teriparatide in a single dose, wherein the concentration of component 1 is 80 to 240 µg/mL. This liquid pharmaceutical preparation has excellent pharmacodynamics.
Provided herein are freeze-dried preparations comprising a high-purity parathyroid hormone (PTH) peptide and one or more PTH analogs, and methods for the production thereof. Also provided is a test method for detecting PTH analogs to confirm the purity of a freeze-dried preparation containing PTH peptide, and the like.
A61K 9/19 - Particulate form, e.g. powders lyophilised
C07K 14/635 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
F26B 5/06 - Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum the process involving freezing
G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
A61K 38/29 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
B65B 55/10 - Sterilising wrappers or receptacles prior to, or during, packaging by liquids or gases
B65B 55/12 - Sterilising contents prior to, or during, packaging
B65B 63/08 - Auxiliary devices, not otherwise provided for, for operating on articles or materials to be packaged for heating or cooling articles or materials to facilitate packaging
The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
C07D 221/04 - Ortho- or peri-condensed ring systems
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
NATIONAL UNIVERSITY CORPORATION ASAHIKAWA MEDICAL UNIVERSITY (Japan)
Inventor
Tanino, Hiromasa
Ito, Hiroshi
Abstract
[Problem] To provide an agent for preventing the onset of idiopathic osteonecrosis of the femoral head and/or suppressing the progress of the same. [Solution] An agent for preventing the onset of idiopathic osteonecrosis of the femoral head and/or suppressing the progress of the same comprising parathyroid hormone or a derivative thereof as an active ingredient, characterized by being administered intermittently.
The purpose of the present invention is to provide a method for causing measured values to match when the measured values do not match due to a difference in measurement method. The purpose of the present invention is also to provide a method for measuring, in a simple and inexpensive manner and in a short period of time, a glycated albumin (GA) value that is traceable to a GA certification value. The method for measuring a GA value that is traceable to a GA certification value includes the following steps: A1) A step for determining a regression equation III by the following steps b), c), and e0) to h); b) a step for determining the GA concentration [L](A) of two or more GA certified reference materials having different GA certification values; c) a step for measuring the GA-derived absorbance (D) of two or more GA certified reference materials; e0) a step for creating an equation II0 for a straight line in which the intercept is zero; f) a step for using the equation II0 to determine two or more GA concentrations [P](E) proportional to the GA-derived absorbance (D); g) a step for determining two or more GA values (F); and h) a step for creating the regression equation III.
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
G01N 27/62 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating the ionisation of gases, e.g. aerosolsInvestigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode
G01N 21/77 - Systems in which material is subjected to a chemical reaction, the progress or the result of the reaction being investigated by observing the effect on a chemical indicator
NATIONAL UNIVERSITY CORPORATION FUKUSHIMA UNIVERSITY (Japan)
Inventor
Sakasegawa, Shinichi
Yamaura, Saki
Sugimori, Daisuke
Abstract
A purpose of the present invention is to provide a highly versatile, simple and safe method for measuring Lp-PLA2 activity. Another purpose of the present invention is to provide an accurate and highly sensitive method for measuring Lp-PLA2 activity. Provided is a method for measuring Lp-PLA2 activity in a sample containing Lp-PLA2, said method comprising steps (A) to (C): (A) a step for reacting PAFs with Lp-PLA2 in the sample and thus converting the PAFs into lyso-PAFs; (B) a step for hydrolyzing the lyso-PAFs formed in step (A) with an enzyme (lyso-PAF-PLD ) to give hydrolysates; and (C) a step for measuring the Lp-PLA2 activity in the sample with the use of a quantitative change derived from the hydrolysates obtained in step (B) as an indication.
The present invention provides a measuring method for at least one of a kinase forward reaction substrate, a phosphorylated product thereof, and a precursor thereof, and includes a step of conducting an enzymatic cycling reaction by bringing at least a kinase, a first nucleotide coenzyme of the kinase, and a second nucleotide coenzyme having a different nucleoside moiety from the first nucleotide coenzyme into contact with a sample; a step of detecting a signal corresponding to a change of at least one of the first nucleotide coenzyme and a conversion product thereof, and the second nucleotide coenzyme and a conversion product thereof; and (3) a step of calculating, on the basis of the detected change of the signal, an amount of the kinase forward reaction substrate and/or the phosphorylated product thereof contained in the sample.
C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
C12Q 1/50 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase involving creatine phosphokinase
C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
C12Q 1/54 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving glucose or galactose
C12Q 1/61 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving triglycerides
C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
48.
Method and reagent for measuring mevalonic acid, 3-hydroxymethylglutaryl coenzyme A, and coenzyme A
The present invention provides a method for measuring the concentration of an analyte in a test solution wherein the analyte is mevalonic acid and/or 3-hydroxymethylglutaryl coenzyme A, comprising the following steps (p) and (q): (p) a step of allowing an enzyme that catalyzes a reaction represented by Reaction Formula 1 and an enzyme that catalyzes a reaction represented by Reaction Formula 2 to act on a test solution containing mevalonic acid and/or 3-hydroxymethylglutaryl coenzyme A in the presence of a hydrogen acceptor X, a hydrogen donor Y, and coenzyme A; and (q) a step of measuring an amount of: a reduced hydrogen acceptor X that is produced; or an oxidized hydrogen donor Y that is produced; or a hydrogen acceptor X that is decreased; or a hydrogen donor Y that is decreased, wherein the hydrogen donor Y and the reduced hydrogen acceptor X are not the same.
C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
C12N 9/04 - Oxidoreductases (1.), e.g. luciferase acting on CHOH groups as donors, e.g. glucose oxidase, lactate dehydrogenase (1.1)
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
49.
AGENT FOR PREVENTING ONSET OF IDIOPATHIC OSTEONECROSIS OF FEMORAL HEAD AND/OR SUPPRESSING PROGRESS OF SAME
NATIONAL UNIVERSITY CORPORATION ASAHIKAWA MEDICAL UNIVERSITY (Japan)
Inventor
Tanino Hiromasa
Ito Hiroshi
Abstract
[Problem] To provide an agent for preventing the onset of idiopathic osteonecrosis of the femoral head and/or suppressing the progress of the same. [Solution] An agent for preventing the onset of idiopathic osteonecrosis of the femoral head and/or suppressing the progress of the same, said agent comprising parathyroid hormone or a derivative thereof as an active ingredient, characterized by being intermittently administered.
A medicament for therapeutic treatment and/or improvement of sepsis in a patient with severe sepsis accompanied with one or more organ dysfunctions, wherein a value of International Normalized Ratio (INR) of a plasma specimen obtained from said patient is more than 1.4, which comprises thrombomodulin as an active ingredient.
[Problem] Provided is a freeze-dried preparation containing high-purity PTH peptide and a method for the production thereof. Also provided is a test method for PTH analogs to confirm the purity of a freeze-dried preparation containing PTH peptide, and the like.
[Solution] In the present invention, the presence of PTH analogs produced during the manufacturing process of a freeze-dried preparation containing PTH peptide was confirmed. The production of these PTH analogs was also discovered to be markedly prevented or reduced by controlling exposure of the solution containing PTH peptide and the like to air environments within a pharmaceutical production facility.
A61K 9/19 - Particulate form, e.g. powders lyophilised
C07K 14/635 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
F26B 5/06 - Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum the process involving freezing
G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
A61K 38/29 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
B65B 55/10 - Sterilising wrappers or receptacles prior to, or during, packaging by liquids or gases
B65B 55/12 - Sterilising contents prior to, or during, packaging
B65B 63/08 - Auxiliary devices, not otherwise provided for, for operating on articles or materials to be packaged for heating or cooling articles or materials to facilitate packaging
Provided is a measurement method for at least one of a forward reaction substrate for a kinase, a phosphorus oxide thereof, and derivative precursors that are converted into the aforementioned substances. The measurement method includes: a step in which at least a kinase, a first nucleotide coenzyme of the kinase, and a second nucleotide coenzyme that has a different nucleoside moiety than the first nucleotide coenzyme are brought into contact with a sample and an enzymatic cycling reaction is carried out; a step in which a signal corresponding to the amount of change between the first nucleotide coenzyme and the transformed product thereof and/or between the second nucleotide coenzyme and the transformed product thereof is detected; and (3) a step in which the amount of a forward reaction substrate for the kinase and/or a phosphorus oxide thereof included in the sample is calculated on the basis of the amount of change in the detected signal.
C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
C12Q 1/54 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving glucose or galactose
C12Q 1/61 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving triglycerides
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
53.
Measurement method for human pancreatic lipase activity
A measurement method for human pancreatic lipase activity in a sample, includes bringing a bile acid that makes a pH for giving a maximum value of human pancreatic lipase activity to be lower than 7.7, a diglyceride and a colipase into contact with the sample at pH 7.4 or lower; and detecting a signal amount varying in accordance with the human pancreatic lipase activity in the sample, and the bile acid is a bile acid containing: one of or two or more of a-type bile acids selected from the group consisting of GDCA, GCDCA, TDCA, TCDCA and salts thereof; and/or a combination of one of or two or more of b-1-type bile acids selected from the group consisting of GCA, GUDCA, TCA, TUDCA and salts thereof, and one of or two or more of b-2-type bile acids selected from the group consisting of DCA, CDCA and salts thereof.
[Problem] To provide the following: an agent for treating cancer, particularly an agent for inhibiting cancer cell proliferation or an agent for inhibiting or preventing cancer metastasis; drug that uses the agent; a method for assessing the effect of cancer treatment; a method for estimating the prognosis of cancer treatment; a method for screening for a substance having a cancer proliferation-inhibiting effect; and a method for screening a substance having a cancer metastasis-impeding effect.
[Solution] Provided is a drug containing a nucleic acid formed from a nucleotide sequence having sequence identity of 70% or greater with at least sequence No. 1 or No. 2, wherein the nucleic acid shows protein expression-inhibiting activity.
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
C12N 5/00 - Undifferentiated human, animal or plant cells, e.g. cell linesTissuesCultivation or maintenance thereofCulture media therefor
55.
Medicament for therapeutic treatment and/or improvement of sepsis
A medicament for therapeutic treatment and/or improvement of sepsis in a patient with severe sepsis accompanied with one or more organ dysfunctions, wherein a value of International Normalized Ratio (INR) of a plasma specimen obtained from said patient is more than 1.4, which comprises thrombomodulin as an active ingredient.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
56.
Agent for prophylactic and/or therapeutic treatment of peripheral neuropathic pain caused by anticancer agent
A medicament effective for prophylactic and/or therapeutic treatment of a peripheral neuropathic pain such as allodynia caused by a treatment with an anticancer agent, which comprises thrombomodulin as an active ingredient.
A method for measuring the activity of human pancreatic lipase in a sample, which comprises a contacting step of bringing a bile acid that can adjust a pH value at which the activity of human pancreatic lipase becomes maximum to a pH value lower than 7.7, a diglyceride and a colipase into contact with the sample at pH 7.4 or lower and a detection step of detecting the amount of a signal that can vary in accordance with the activity of human pancreatic lipase in the sample, wherein the bile acid comprises at least one a-type bile acid selected from the group consisting of GDCA, GCDCA, TDCA, TCDCA and salts thereof and/or a combination of at least one b-1-type bile acid selected from the group consisting of GCA, GUDCA, TCA, TUDCA and salts thereof and at least one b-2-type bile acid selected from the group consisting of DCA, CDCA and salts thereof.
A medicament for therapeutic treatment and/or improvement of sepsis in a patient with severe sepsis accompanied with one or more organ dysfunctions, wherein a value of International Normalized Ratio (INR) of a plasma specimen obtained from said patient is more than 1.4, which comprises thrombomodulin as an active ingredient.
A61K 38/36 - Blood coagulation or fibrinolysis factors
A61K 38/57 - Protease inhibitors from animalsProtease inhibitors from humans
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical and veterinary preparations; sanitary
preparations for medical purposes; plasters, materials for
dressings; material for stopping teeth, dental wax;
disinfectants; preparations for destroying vermin;
fungicides, herbicides; biological preparations for medical
purposes; chemical preparations for medical purposes;
chemical reagents for medical or veterinary purposes; in
vitro diagnostic reagents for medical use; serum containing
reagents as calibrators for assay for medical use;
calibration reagents for diagnostic reagents for medical
use; control serums for assay; serums for medical use;
diagnostic preparations for medical use; kits of in vitro
diagnostic preparations for medical use.
[Problem] To provide the following: an agent for treating cancer, particularly an agent for inhibiting cancer cell proliferation or an agent for inhibiting or preventing cancer metastasis; a drug that uses the agent; a method for assessing the effect of cancer treatment; a method for estimating the prognosis of cancer treatment; a method for screening for a substance having a cancer proliferation-inhibiting effect; and a method for screening a substance having a cancer metastasis-impeding effect. [Solution] Provided is a drug containing a nucleic acid formed from a nucleotide sequence having sequence identity of 70% or greater with at least sequence No. 1 or No. 2, wherein the nucleic acid shows protein expression-inhibiting activity.
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
NATIONAL UNIVERSITY CORPORATION FUKUSHIMA UNIVERSITY (Japan)
ASAHI KASEI PHARMA CORPORATION (Japan)
Inventor
Sakasegawa, Shin-Ichi
Matsumoto, Hideyuki
Sugimori, Daisuke
Abstract
Provided is a novel method for hydrolyzing plasmalogen. Plasmalogen is hydrolyzed into lysoplasmalogen using a phospholipase having at least the properties (a) to (c) mentioned below: (a) the specific activity of the phospholipase for ethanolamine-type plasmalogen (C18, 20:4) is 0.66 ± 0.2 U/mg; (b) the molecular weight of the phospholipase ranges from 25 to 30 kDa as measured by an SDS-PAGE method; and (c) the phospholipase is derived from an actinomycete belonging to the genus Streptomyces.
C12N 9/16 - Hydrolases (3.) acting on ester bonds (3.1)
C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
C12Q 1/34 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase
TOKYO METROPOLITAN GERIATRIC HOSPITAL AND INSTITUTE OF GERONTOLOGY (Japan)
NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY (Japan)
ASAHI KASEI PHARMA CORPORATION (Japan)
NATIONAL UNIVERSITY CORPORATION FUKUSHIMA UNIVERSITY (Japan)
Inventor
Maeba Ryouta
Araki Atsushi
Fujiwara Yoshinori
Ogawa Kishiko
Hara Hiroshi
Nishimukai Megumi
Sakasegawa Shinichi
Matsumoto Hideyuki
Matsumoto Yusaku
Sugimori Daisuke
Abstract
There are provided: a method of examination for identifying persons suffering from dementia or persons in the preliminary stage thereof, using a biomolecule as an index; a kit for use in this method of examination; an enzyme contained in this kit; and a method of manufacturing this enzyme. The method of inspection includes a step of assaying myoinositol (MI) in naturally excreted urine of the patient and a step of assaying ethanolamine plasmalogen (PlsEtn) in serum or plasma of the same patient, and classifying patients whose MI content is at least a set threshold value and whose PlsEtn content is no more than a set threshold value as persons suffering from dementia or persons in the preliminary stage thereof.
G01N 33/98 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving alcohol, e.g. ethanol in breath
63.
AGENT FOR PREVENTING AND/OR TREATING PERIPHERAL NEUROPATHIC PAIN CAUSED BY ANTI-CANCER DRUG
A medicine effective in preventing and/or treating peripheral neuropathic pain, such as allodynia, caused by an anti-cancer drug treatment; wherein the medicine contains thrombomodulin as an active ingredient.
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61P 25/04 - Centrally acting analgesics, e.g. opioids
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
A method is provided for producing soluble thrombomodulin substantially not containing a denatured product of the soluble thrombomodulin that is generated under acidic conditions, which comprises: subjecting the soluble thrombomodulin-containing material to an anion exchanger or hydroxyapatite; and carrying out linear gradient elution, stepwise gradient elution, or gradient elution in which linear gradient elution is combined with stepwise gradient elution under separation conditions in which the denatured product of the soluble thrombomodulin can be separated, wherein the gradient is a salt concentration gradient, so as to obtain an elution fraction containing soluble thrombomodulin that does not substantially contain the denatured product of the soluble thrombomodulin, either (a) after the position of a fraction has previously been confirmed, or (b) while confirming the elution fraction.
A medicament for therapeutic treatment and/or improvement of sepsis in a patient with severe sepsis accompanied with one or more organ dysfunctions, wherein a value of International Normalized Ratio (INR) of a plasma specimen obtained from said patient is more than 1.4, which comprises thrombomodulin as an active ingredient.
Highly-purified soluble thrombomodulin which has a content of host cell-originated proteins being in a ratio of less than 10 ng of the proteins per 10,000 U of the soluble thrombomodulin, wherein the soluble thrombomodulin is produced by a transformant cell obtained by transfecting a host cell with a DNA containing a nucleotide sequence encoding the soluble thrombomodulin.
A medicine for the effective treatment and/or improvement of sepsis in patients suffering from severe sepsis who have damage to one or more organs and the International Normalized Ratio (INR) value of a blood sample of whom is higher than 1.4, comprising thrombomodulin as active ingredient.
2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.
A01N 43/00 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
A01N 37/08 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing carboxylic groups or thio-analogues thereof, directly attached by the carbon atom to a cycloaliphatic ringDerivatives thereof
A01N 43/36 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 11/00 - Drugs for disorders of the respiratory system
69.
FREEZE-DRIED PREPARATION CONTAINING HIGH-PURITY PTH AND METHOD FOR PRODUCING SAME
[Problem] To provide a freeze-dried preparation containing a high-purity PTH peptide and a method for producing the same, and to provide a method for detecting PTH analogs in order to confirm the purity of the freeze-dried preparation containing a PTH peptide. [Solution] The presence of PTH analogs generated during a step for producing a freeze-dried preparation containing a PTH peptide in the present invention was confirmed. It was discovered that the generation of PTH analogs can be significantly prevented or reduced by inhibiting exposure to air inside a facility for producing a PTH peptide-containing solution or the like.
A61K 9/19 - Particulate form, e.g. powders lyophilised
C07K 14/635 - Parathyroid hormone, i.e. parathormoneParathyroid hormone-related peptides
F26B 5/06 - Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum the process involving freezing
G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
70.
PREVENTIVE AND/OR THERAPEUTIC AGENT FOR ALLODYNIA CAUSED BY ANTICANCER AGENT
[Problem] To provide a pharmaceutical effective in the prevention and/or treatment of allodynia caused by an anticancer agent. [Solution] A preventive and/or therapeutic agent for allodynia caused by an anticancer agent, containing natural calcitonin or a calcitonin derivative as an active ingredient is provided. Further, a method for preventing and/or treating allodynia caused by an anticancer agent by administering natural calcitonin or a calcitonin derivative, and the use of natural calcitonin or a calcitonin derivative for producing a preventive and/or therapeutic agent for allodynia caused by an anticancer agent are provided.
The present invention provides a method for measuring the concentration of an analyte in a test solution wherein the analyte is mevalonic acid and/or 3-hydroxymethylglutaryl coenzyme A, comprising the following steps (p) and (q): (p) a step of allowing an enzyme that catalyzes a reaction represented by Reaction Formula 1 and an enzyme that catalyzes a reaction represented by Reaction Formula 2 to act on a test solution containing mevalonic acid and/or 3 -hydroxymethylglutaryl coenzyme A in the presence of a hydrogen acceptor X, a hydrogen donor Y, and coenzyme A; and (q) a step of measuring an amount of: a reduced hydrogen acceptor X that is produced; or an oxidized hydrogen donor Y that is produced; or a hydrogen acceptor X that is decreased; or a hydrogen donor Y that is decreased, wherein the hydrogen donor Y and the reduced hydrogen acceptor X are not the same.
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
C12Q 1/48 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving transferase
C07K 1/00 - General processes for the preparation of peptides
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
A high-purity soluble thrombomodulin which is produced by a transformant, said transformant having been obtained by transfecting a host cell with DNA comprising a base sequence encoding soluble thrombomodulin, and contains less than 10 ng of host cell-derived proteins per 10,000 U of the soluble thrombomodulin.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 14/745 - Blood coagulation or fibrinolysis factors
C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
74.
PREVENTATIVE AGENT AND/OR THERAPEUTIC AGENT AND/OR EXACERBATION-SUPPRESSING AGENT FOR HUMAN KNEE OSTEOARTHRITIS
Disclosed is a drug that is extremely useful for the prevention and/or therapy and/or exacerbation-suppression of human knee osteoarthritis. The drug is characterized by containing parathyroid hormone (PTH) or a PTH derivative as an active ingredient for the prevention and/or therapy and/or exacerbation-suppression of human knee osteoarthritis.
Disclosed are a therapeutic agent for tumor, in particular, drug-resistant cancer, an agent for inhibiting or preventing tumor metastasis, and an agent for inhibiting or preventing cancer recurrence, each comprising miR27b or a nucleic acid containing a nucleotide which comprises a nucleotide sequence having a 70% or more identity with the nucleotide sequence represented by SEQ ID NO:1 and has the same function as that of miR27b.
Disclosed is a medical agent which selectively stimulates a β3-adrenergic receptor, in particular, a medical agent which is capable of preferentially stimulating a β3-adrenergic receptor in comparison to the case with an α1-adrenergic receptor. The medical agent is able to be used for treatment and prevention of diabetes, obesity, hyperlipemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the digestive tract, interstitial cystitis, overactive bladder, urinary incontinence, or diseases associated with lacrimal hyposecretion. Specifically disclosed is an indazole analogue represented by general formula (I) or a salt thereof. Also specifically disclosed is a pharmaceutical product which contains the indazole analogue or a salt thereof as an active ingredient.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
77.
IDENTIFICATION METHOD AND ONSET PREDICTION METHOD FOR ATHEROTHROMBOTIC CEREBRAL INFARCTION IN ACUTE CEREBRAL INFARCTION
Disclosed are a method for accurately, easily, quickly, and inexpensively identifying an atherothrombotic cerebral infarction in an acute cerebral infarction, and a method for accurately, easily, quickly, and inexpensively predicting the onset of an atherothrombotic cerebral infarction. The method enables the measurement of glycoalbumin and hemoglobin A1c in a sample derived from an acute cerebral infarction patient and the identification of an atherothrombotic cerebral infarction from the calculated glycoalbumin/hemoglobin A1c ratio. The method also enables the prediction of the onset of an atherothrombotic cerebral infarction in patients with arteriosclerosis and patients with risk factors for atherothrombotic cerebral infarctions such as diabetes patients from the glycoalbumin/hemoglobin A1c ratio and/or from the variation of the ratio with time.
C12Q 1/02 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving viable microorganisms
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/72 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving blood pigments, e.g. hemoglobin, bilirubin
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
78.
PTH-CONTAINING THERAPEUTIC/PROPHYLACTIC AGENT FOR OSTEOPOROSIS, CHARACTERIZED IN THAT PTH IS ADMINISTERED ONCE A WEEK AT UNIT DOSE OF 100 TO 200 UNITS
Disclosed are: a method for treating osteoporosis using PTH that is highly safe and has high effect/efficacy; a method for inhibiting/preventing bone fracture using PTH that is highly safe; and a medicinal agent for use in each of the aforementioned methods. Specifically disclosed is a medicinal agent comprising PTH as an active ingredient, which is characterized in that PTH is administered once a week at a unit dose of 100 to 200 units in each of the aforementioned methods.
A method for determining the concentration of an analyte mevalonic acid and/or 3-hydroxymethylglutaryl-coenzyme A in a sample solution, which comprises the following steps (p) and (q): (p) causing an enzyme capable of catalyzing a reaction represented by formula (1) and an enzyme capable of catalyzing a reaction represented by formula (2) to act on a sample solution containing mevalonic acid and/or 3-hydroxymethylglutaryl-coenzyme A in the presence of a hydrogen acceptor (X), a hydrogen donor (Y) and coenzyme A; and (q) determining the quantity of a reduction-type hydrogen acceptor (X) or an oxidization-type hydrogen donor (Y) generated, or the quantity of the hydrogen acceptor (X) or the quantity of the hydrogen donor (Y) decreased, wherein the hydrogen donor (Y) and the reduction-type hydrogen acceptor (X) are not identical to each other.
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
It is an object of the present invention to obtain a soluble thrombomodulin substantially not containing a denatured product of soluble thrombomodulin that may be generated under acidic conditions. The present invention provides a method for producing soluble thrombomodulin substantially not containing a denatured product of the soluble thrombomodulin that may be generated under acidic conditions, from a soluble thrombomodulin-containing material that contains or is suspected to contain the denatured product of the soluble thrombomodulin, which comprises; a step of subjecting the soluble thrombomodulin-containing material to an anion exchanger or hydroxyapatite; and a step of carrying out linear gradient elution, stepwise gradient elution, or gradient elution in which linear gradient elution is combined with stepwise gradient elution under separation conditions in which the denatured product of the soluble thrombomodulin can be separated, wherein said gradient is a gradient of salt concentration, so as to obtain an elution fraction containing soluble thrombomodulin that does not substantially contain the denatured product of the soluble thrombomodulin, either (a) after the position of a fraction has previously been confirmed, or (b) while confirming the elution fraction.
Disclosed is a novel acid addition salt of an indazole derivative that is useful as an active ingredient for a pharmaceutical agent for preventing and/or treating diabetes, obesity, hyperlipemia, overactive bladder, urinary incontinence and the like, particularly a crystal of the acid addition salt, wherein the acid addition salt has desirable properties. Specifically disclosed is (R)-N-[3-[2-[2-(3- methylindazol-6-yloxy)ethylamino]-1-hydroxyethyl]phenyl] methanesulfonamide dihydrochloride or a crystal thereof. The crystal of the dihydrochloride may have the main peak at one or more positions selected from the group consisting of about 12.8˚, 21.8˚ and 25.0˚ 2θ in powdery X-ray diffraction spectra.
A blood sample analysis method comprising: a first step of obtaining average blood glucose levels (MBG(0)), (MBG(t1)) and (MBG(∞)), glycoalbumin levels (GA(0)), (GA(t1)) and (GA(∞)) and hemoglobin A1c levels (A1c(0)), (A1c(t1)) and (A1c(∞)) in a blood sample at a base time point, t1 day(s) after the base time point, and after sufficient time is elapsed after the base time point; and a second step of calculating an average glucose level, a glycoalbumin level, a hemoglobin A1c level, or a ratio of a glycoalbumin level to a hemoglobin A1c level on day t by utilizing the fact that logarithmic values of (GA(t) - GA(∞))/(GA(0) – GA(∞)), (A1c(t) – A1c(∞))/(A1c(0) – A1c(∞)) and (MBG(t) - MBG(0))/(MBG(0) – MBG (∞)) are proportional to the days (t) elapsed after the base time point.
Disclosed are a compound represented by general formula (A-1) or a salt thereof and a compound represented by general formula (1) or a salt thereof. The compound represented by general formula (A-1) or the salt thereof and the compound represented by general formula (1) or the salt thereof have an agonistic activity on a β3 adrenergic receptor, and are therefore useful as therapeutic and prophylactic agents for diabetes, obesity, hyperlipemia, depression, gallstone, diseases associated with increased movement of the biliary tract, diseases associated with hyperfunction of the digestive tract, interstitial cystitis, overactive bladder or urinary incontinence or therapeutic and prophylactic agents for diseases associated with decreased tears.
Disclosed are a compound represented by general formula (A-1) or a salt thereof and a compound represented by general formula (1) or a salt thereof. The compound represented by general formula (A-1) or the salt thereof and the compound represented by general formula (1) or the salt thereof have an agonistic activity on a β3 adrenergic receptor, and are therefore useful as therapeutic and prophylactic agents for diabetes, obesity, hyperlipemia, depression, gallstone, diseases associated with increased movement of the biliary tract, diseases associated with hyperfunction of the digestive tract, interstitial cystitis, overactive bladder or urinary incontinence or therapeutic and prophylactic agents for diseases associated with decreased tears.
Disclosed is a compound represented by formula (1) [wherein D1, A1, D2, R1, D3 and R2 are as defined in the description] or a salt thereof. The compound represented by formula (1) or the salt thereof has an IKKβ-inhibiting activity and the like. Therefore, the compound or the salt thereof is useful for the prevention and/or treatment of a disease or condition associated with IKKβ, and the like.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 217/02 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
Disclosed is an aqueous solution composition which contains (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3-aminopyrrolidine or (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3- (methylamino)pyrrolidine as an active ingredient, does not contain citric acid or a salt thereof, and has high stability so that the composition can be stored at room temperature.
Disclosed is a nitrogenated heterocyclic compound represented by general formula (1). The compound or a salt thereof exhibits a potent antagonistic activity on an EP1 receptor when administered to a human body or an animal. Therefore, the compound or a salt thereof is useful, for example, as an active ingredient for a pharmaceutical agent for preventing and/or treating overactive bladder. The compound or a salt thereof is also useful as an active ingredient for a pharmaceutical agent for preventing and/or treating a symptom such as frequent urination, urgency of urination or urinary incontinence.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 29/02 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/08 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
Disclosed is a nitrogenated bicyclic heterocyclic compound represented by general formula (1). The compound or a salt thereof exhibits a potent antagonistic activity on an EP1 receptor when administered to a human body or an animal. Therefore, the compound or a salt thereof is useful, for example, as an active ingredient for a pharmaceutical agent for preventing and/or treating overactive bladder. The compound or a salt thereof is also useful as an active ingredient for a pharmaceutical agent for preventing and/or treating a symptom such as frequent urination, urgency of urination or urinary incontinence.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 29/02 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
Disclosed is a sulfonamide compound represented by general formula (1) that can be used as an effective component in a CaSR antagonist that is extremely effective in preventing and/or treating bone diseases, such as osteoporosis. Said compound has excellent PTH secretion promoting effects. Said compound is useful as a medically effective component for preventing and/or treating osteoporosis or bone fractures, hypoparathyroidism, or other bone diseases.
C07C 311/18 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/235 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
A61P 5/20 - Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 311/41 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
C07D 213/36 - Radicals substituted by singly-bound nitrogen atoms
C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Disclosed is a compound represented by general formula (1) (wherein X represents a halogen atom, an optionally substituted alkyl group or the like; Y represents a hydrogen atom or an optionally substituted alkyl group; and Z represents a hydrogen atom or an optionally substituted alkyl group) or a salt thereof. The compound has excellent 4-type PLA2 inhibitory activity, and thus exhibits prostaglandin and/or leukotriene production inhibitory activity.
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 411/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
Disclosed are: a novel compound which can act as an S1P1 receptor agonist, namely a novel compound which can cause the lymphocyte sequestration in a secondary lymphoid tissue to exhibit an immunosuppressing activity; and a pharmaceutical preparation comprising the compound as an active ingredient, particularly a definitive therapeutic and/or prophylactic agent for an autoimmune diseases and others. Specifically disclosed is an amino acid compound represented by general formula (1).
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07C 229/48 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms of the same non-condensed ring
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Disclosed is a pharmaceutical composition containing a compound represented by general formula (I) or a salt thereof, and a pharmaceutically acceptable carrier. The pharmaceutical composition does not substantially contain, as the pharmaceutically acceptable carrier, a reducing sugar and/or a carrier containing a reducing sugar as an ingredient. Alternatively, when the pharmaceutical composition contains, as the pharmaceutically acceptable carrier, a reducing sugar and/or a carrier containing a reducing sugar as an ingredient, a contact between the reducing sugar and the compound represented by general formula (I) or a salt thereof is prevented.
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
Disclosed is a sultam derivative represented by general formula (1), which has an inhibitory activity on an aggrecanase activity. The sultam derivative represented by general formula (1) or a salt thereof exhibits a potent inhibitory activity on an aggrecanase activity in a living body of a mammal including a human body, and is therefore useful as an active ingredient of a pharmaceutical agent for the prevention and/or treatment of various diseases caused by the decomposition of aggrecan or the like.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
Disclosed are (S)-1-(4-chloro-5-isoquinolinesulfonyl)-3- (methylamino)pyrrolidine monohydrochloride and a crystal thereof, each of which has excellent properties for use as an active ingredient of a pharmaceutical agent for the prevention and/or treatment of glaucoma or the like. The above-mentioned monohydrochloride crystal may have a main peak at at least one position selected from the group consisting of angle 2ϑ of about 13.9˚, 21.5˚, 21.7˚, 22.4˚, 22.8˚, 24.5˚ and 35.0˚ in powder x-ray diffraction spectra.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
Provided are a method of stabilizing a leuco dye storable as a liquid for a long time, a method of reducing nonspecific color development thereof at a time of a color development reaction, and a stable liquid reagent composition using the methods. The inventors of the present invention found that coexistence of the leuco dye with a specific reducing agent resulted in suppression of self color development and its remarkably improved stability in a solution, and that when a color development reaction of the leuco dye with hydrogen peroxide was performed, coexistence of the leuco dye, in a reaction solution, with another dye which had an absorption spectrum not influencing a measurement wavelength of the leuco dye and did not react with hydrogen peroxide suppressed nonspecific color development and lowered a reagent blank value, which was applied to an analytical reagent.
C09B 67/00 - Influencing the physical, e.g. the dyeing or printing, properties of dyestuffs without chemical reaction, e.g. by treating with solventsProcess features in the making of dyestuff preparationsDyestuff preparations of a special physical nature, e.g. tablets, films
D06P 5/00 - Other features in dyeing or printing textiles or dyeing leather, furs or solid macromolecular substances in any form
G01N 33/72 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving blood pigments, e.g. hemoglobin, bilirubin
G03C 8/00 - Diffusion transfer processes or agents thereforPhotosensitive materials for such processes
C12N 9/00 - Enzymes, e.g. ligases (6.)ProenzymesCompositions thereofProcesses for preparing, activating, inhibiting, separating, or purifying enzymes
C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
C12Q 1/26 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving oxidoreductase
96.
METHOD FOR PRODUCING SOLUBLE THROMBOMODULIN OF HIGH PURITY
It is intended to obtain soluble thrombomodulin which substantially contains no soluble thrombomodulin variant that can be formed under an acidic condition. According to the invention, a method for producing soluble thrombomodulin which substantially contains no soluble thrombomodulin variant from a soluble thrombomodulin-containing material which contains or is suspected to contain a soluble thrombomodulin variant that can be formed under an acidic condition, comprising the steps of: subjecting the soluble thrombomodulin-containing material to an anion exchanger or hydroxyapatite; and obtaining an eluted fraction containing soluble thrombomodulin which substantially contains no soluble thrombomodulin variant by applying a linear or stepwise gradient of salt concentration or a combination of linear and stepwise gradients thereof under a separation condition capable of separating the soluble thrombomodulin variant and performing identification in advance or while performing identification is provided.
Compounds represented by the general formula (1) which have potent inhibitory effect on Rho-kinase, salts of the same, or derivatives of both serving as prodrugs: (1) wherein A is a nitrogenous saturated ring; m is an integer of 0 to 2; n is an integer of 1 to 4; G1 is hydrogen, chloro, hydroxy, alkoxy, or amino; G2 is halogeno, hydroxy, cyano, carboxy, alkyl, alkenyl, or the like; G3 is hydrogen, halogeno, hydroxy, cyano, carboxy, alkyl, alkenyl, or the like; G4 is hydroxy or -N(R1)(R2) (wherein R1 and R2 are each hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or a saturated heterocyclic group); and G5 is a substituent on a carbon atom constituting the ring A and is hydrogen, fluoro or alkyl.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Disclosed is a compound represented by the formula (1) below having a strong Rho kinase inhibitory activity, a salt thereof or a derivative of any of them as a prodrug. (In the formula (1) below, A represents a nitrogen-containing saturated ring; m represents a number of 0-2; n represents a number of 1-4; G1 represents a hydrogen atom, a chlorine atom, a hydroxy group, an alkoxy group or an amino group; G2 represents a halogen atom, a hydroxy group, a cyano group, a carboxy group, an alkyl group, an alkenyl group or the like; G3 represents a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, a carboxy group, an alkyl group, an alkenyl group or the like; Y represents a single bond or -C(R3)(R4)- (wherein R3 and R4 represent a hydrogen atom or alkyl group, or alternatively they combine together to form a saturated hydrocarbon ring group); G4 represents a hydroxy group (provided that Y is a single bond) or -N(R1)(R2) (wherein R1 and R2 represent a hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group or the like; and G5 represents a substituent at a carbon atom constituting the ring A, which is specifically a hydrogen atom, a fluorine atom or an alkyl group.)
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/542 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
[PROBLEMS] To provide a pharmaceutical agent or a functional food which is superior to a conventional one having at least one activity selected from an adiponectin-increasing activity, an anti-obesity activity, a fatty liver-ameliorating activity, a liver function-improving activity and an insulin resistance-improving activity. [MEANS FOR SOLVING PROBLEMS] It is found that phosphatidylinositol has at least one activity selected from an adiponectin-increasing activity, an anti-obesity activity, a fatty liver-ameliorating activity, a liver function-improving activity and an insulin resistance-improving activity. A pharmaceutical agent or a functional food is provided, which comprises phosphatidylinositol as an active ingredient.
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
Disclosed is an anti-fatigue agent or physical endurance enhancer or a functional food having an anti-fatigue effect or a physical endurance-enhancing effect. Specifically disclosed are: a composition comprising phosphatidylinositol and coenzyme Q10; an anti-fatigue agent for a physical endurance enhancer comprising phosphatidylinositol and coenzyme Q10 as active ingredients; a functional food having an anti-fatigue effect or a physical endurance-enhancing effect, which comprises the compounds as active ingredients; use of phosphatidylinositol and coenzyme Q10 for the preparation of a composition having an anti-fatigue effect or a physical endurance-enhancing effect; and an anti-fatigue method or a method for enhancing physical endurance, which comprises ingesting a composition comprising these compounds as active ingredients.