Takeda Pharmaceutical Company Limited Patent applications |
Patent application number | Title | Published |
20160115128 | AROMATIC COMPOUND - Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: | 04-28-2016 |
20160113913 | CONTROLLED-RELEASE DRUG FORMULATION - The present invention provides a controlled-release solid preparation containing pioglitazone or a salt thereof as an active ingredient, and having superior sustainability. | 04-28-2016 |
20160060273 | HETEROCYCLIC COMPOUND - Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification. | 03-03-2016 |
20160052988 | PEPTIDE COMPOUND - The present invention provides a novel peptide compound having an activating action on GLP-1 receptors and GIP receptors and use of the peptide compound as a medicament. Specifically, a peptide containing a partial sequence represented by the formula (I) or a salt thereof and a medicament comprising the same are provided. P | 02-25-2016 |
20160052897 | HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula (I), which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. In the formula (I), each symbol is as defined in the specification. | 02-25-2016 |
20160039811 | HETEROCYCLIC COMPOUND - Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) | 02-11-2016 |
20160015952 | A MICRONEEDLE PATCH - The present invention provides a microneedle patch which can solve the problem that microneedle production is difficult and requires high accuracy, the problem that time and mental burdens on a health professional and a patient are large, and the problem caused by compounding a plurality of drugs. The microneedle patch comprises a large number of drug-carrying microprojections | 01-21-2016 |
20160002209 | PRODUCTION METHOD OF PYRIDAZINONE COMPOUNDS - The present invention provides an industrially advantageous method of producing a pyridazinone compound. The present invention relates to the following method of producing a pyridazinone compound: Formula (II), (IIIa), (IV) or (IV″), Formula (IIIb), (Vb) or (V″b), Formula (VI), (I) or (I″), wherein each symbol is as described in the specification. | 01-07-2016 |
20160000769 | METHODS AND DRUG PRODUCTS FOR TREATING ALZHEIMER'S DISEASE - Provided herein are drug products with low dose pioglitazone for use in the treatment (e.g., delay of onset) of cognitive impairment of the Alzheimer's type. Methods of manufacture thereof are also provided. Further provided are methods of treatment for Alzheimer's disease including administering a drug product with low dose pioglitazone. The methods may include determining whether the subject is at risk of developing Alzheimer's disease based upon the subject's age and TOMM40 523 genotype. | 01-07-2016 |
20150336964 | FUSED HETEROAROMATIC PYRROLIDINONES - Disclosed are compounds of Formula 1, | 11-26-2015 |
20150315209 | HETEROCYCLIC COMPOUND - An object of the present invention is to provide a compound having a superior CH24H inhibitory action, which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. The present invention relates to a compound represented by the formula: | 11-05-2015 |
20150291702 | CONJUGATED ANTI-CD38 ANTIBODIES - Isolated antibodies that bind to human CD38 and cynomolgus CD38 are disclosed. Also disclosed are pharmaceutical compositions comprising the disclosed antibodies, and therapeutic and diagnostic methods for using the disclosed antibodies. | 10-15-2015 |
20150274723 | SUBSTITUTED 6-AZA-ISOINDOLIN-1-ONE DERIVATIVES - Disclosed are compounds of Formula 1, | 10-01-2015 |
20150266881 | CYCLOPROPANAMINE COMPOUND AND USE THEREOF - The present invention provides a compound having a lysine specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, Alzheimer's disease, Parkinson's disease or Huntington's disease, and the like. The present invention relates to a compound represented by the formula | 09-24-2015 |
20150250728 | PROCESS FOR PRODUCING SOLID PARTICLES - A method of producing crystal of a poorly water-soluble pharmaceutical compound, including mixing a solution of a poorly water-soluble pharmaceutical compound in a good solvent and nanobubble water or an aqueous nanobubble solution to precipitate crystal of the poorly water-soluble pharmaceutical compound. The crystal of a poorly water-soluble pharmaceutical compound obtained by the method is microparticulate and has more uniform particle size distribution, and is superior in the absorbability and sustainability. | 09-10-2015 |
20150225361 | FUSED HETEROCYCLIC COMPOUND - A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. | 08-13-2015 |
20150225354 | HETEROCYCLIC COMPOUND - A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. | 08-13-2015 |
20150224113 | 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE INHIBITORS OF PHD - The present invention provides a method of treating acute heart failure by administering a compound of the formula: | 08-13-2015 |
20150203464 | COMPOUNDS FOR SUPPRESSING A PERIPHERAL NERVE DISORDER INDUCED BY AN ANTI-CANCER AGENT - The present invention provides a medicament that suppresses (or mitigates) various neurological symptoms caused by a peripheral nerve disorder induced by an anti-cancer agent. | 07-23-2015 |
20150182533 | 5-HT3 RECEPTOR ANTAGONISTS - The present invention provides a method of treating nicotine addiction comprising administering a 5-HT3 receptor antagonists of Formula (I): | 07-02-2015 |
20150175602 | TETRAHYDROPYRIDOPYRAZINES MODULATORS OF GPR6 - The present invention provides compounds of formula I: | 06-25-2015 |
20150158863 | HETEROCYCLIC COMPOUND - The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. | 06-11-2015 |
20150157619 | PHARMACEUTICAL PREPARATION FOR INJECTION - The present invention provides a preparation for injection comprising a protein with a molecular weight of 20 kDa or greater and a pyridine derivative, wherein the preparation for injection does not comprise a hydrophobic preservative. | 06-11-2015 |
20150157609 | SOLID PREPARATION - The present invention provides a solid preparation wherein variation in weight is suppressed, a solid preparation wherein the active ingredient is stabilized, and a stabilization method thereof. A solid preparation containing (1) an active ingredient, (2) D-mannitol and (3) an alkaline earth metal salt selected from magnesium aluminometasilicate and calcium silicate. A method of stabilizing the. active ingredient, including adding an alkaline earth metal salt selected from magnesium aluminometasilicate and calcium silicate. | 06-11-2015 |
20150141447 | SOLID PREPARATION - The present invention provides a solid preparation excellent in disintegration property and preservation stability. The present invention relates to a solid preparation containing (1) 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof, (2) a saccharide, and (3) sodium stearyl fumarate. In addition, the present invention relates to a solid preparation containing (1) compound (A) or a salt thereof, (2) a saccharide, and (3) stearic acid or talc in a naked tablet part. | 05-21-2015 |
20150133451 | HETEROCYCLIC COMPOUND - The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): | 05-14-2015 |
20150132394 | METHOD FOR PRODUCING MICROCAPSULE POWDER - A method for producing a microcapsule powder includes a concentration step. In the concentration step, an aqueous dispersion of a microcapsule is supplied into a cyclone, and the aqueous dispersion is then concentrated. The concentration step includes an aqueous dispersion-supplying step and a concentrated dispersion-recovering step. In the aqueous dispersion-supplying step, the aqueous dispersion is supplied into a cylindrical member inlet. In the concentrated dispersion-recovering step, a microcapsule dispersion is recovered. The microcapsule dispersion is discharged through a conical member outlet. | 05-14-2015 |
20150132379 | DRY-COATED TABLET - A dry-coated tablet | 05-14-2015 |
20150119412 | HETEROCYCLIC COMPOUND - A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: | 04-30-2015 |
20150111922 | SULFONYL PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATING PROKINETICIN MEDIATED DISEASES - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R | 04-23-2015 |
20150099777 | HETEROCYCLIC COMPOUND - A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: | 04-09-2015 |
20150094296 | HETEROCYCLIC COMPOUND - The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. | 04-02-2015 |
20150080322 | SUSTAINED-RELEASE COMPOSITION AND METHOD FOR PRODUCING THE SAME - Sustained-release compositions wherein a water-soluble physiologically active peptide is substantially uniformly dispersed in a microcapsule comprised of a lactic acid polymer or a salt thereof, and the physiologically active substance is contained in an amount of 15 to 35 wt/wt % to the total microcapsules and weight-average molecular weight (Mw) of the lactic acid polymer is about 11,000 to about 27,000, which is characterized by having a high content of the physiologically active substance, and suppression of the initial excessive release within one day after the administration and a stable drug sustained-release over a long period of time, and method for producing the same. | 03-19-2015 |
20150057298 | NOVEL COMPOUNDS - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, | 02-26-2015 |
20150051256 | COMPOUNDS FOR SUPPRESSING A PERIPHERAL NERVE DISORDER INDUCED BY AN ANTI-CANCER AGENT - The present invention provides a medicament that suppresses (or mitigates) various neurological symptoms caused by a peripheral nerve disorder induced by an anti-cancer agent. | 02-19-2015 |
20150051197 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease, attention deficit hyperactivity disorder (ADHD) and the like. The compound represented by formula (I): | 02-19-2015 |
20150045351 | TRICYCLIC COMPOUND - The present invention provides a compound having a superior serotonin 5-HT | 02-12-2015 |
20150045349 | HETEROCYCLIC COMPOUND - The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. | 02-12-2015 |
20150031652 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Disclosed are compounds of the following formula: | 01-29-2015 |
20150030704 | PYRIDAZINONE COMPOUNDS AND THEIR USE AS DAAO INHIBITORS - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R | 01-29-2015 |
20150018547 | AROMATIC RING COMPOUND - The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. | 01-15-2015 |
20140357552 | PEPTIDE COMPOUND - The present invention provides a novel peptide compound having an activating action on GLP-1 receptors and GIP receptors and use of the peptide compound as a medicament. Specifically, a peptide containing a partial sequence represented by the formula (I) or a salt thereof and a medicament comprising the same are provided. | 12-04-2014 |
20140343070 | PROTON PUMP INHIBITORS - A proton pump inhibitor containing a compound represented by the formula (I) | 11-20-2014 |
20140336180 | COMBINATION OF MEK INHIBITORS AND SELECTIVE INHIBITORS OF AURORA A KINASE - The present invention relates to methods for the treatment of proliferative disorders. In particular, the invention provides methods for treatment of proliferative disorders by administering a MEK inhibitor in combination with a selective inhibitor of Aurora A kinase. | 11-13-2014 |
20140309219 | N-SUBSTITUTED OXAZINOPTERIDINES AND OXAZINOPTERIDINONES - Disclosed are compounds of Formula 1, | 10-16-2014 |
20140296200 | 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE INHIBITORS OF PHD - The present invention provides compounds of the formula: | 10-02-2014 |
20140271856 | ORALLY DISINTEGRABLE TABLETS - An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 μm or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration. | 09-18-2014 |
20140256757 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof in combination with metformin and in combination with pioglitazone. | 09-11-2014 |
20140256734 | PYRIDINYL AND FUSED PYRIDINYL TRIAZOLONE DERIVATIVES - Disclosed are compounds of Formula 1, | 09-11-2014 |
20140256693 | PYRROLO [1,2-C] IMIDAZOLE DERIVATIVES FOR USE IN THE PROPHYLAXIS OR TREATMENT OF CANCER WHICH IS REFRACTORY TO KNOWN CANCER THERAPIES - The present invention mainly aims to provide a drug for the prophylaxis or treatment of androgen-independent prostate cancer, which is highly useful as a pharmaceutical agent. The present invention provides a drug for the prophylaxis or treatment of androgen-independent prostate cancer, containing a steroid C | 09-11-2014 |
20140248378 | PYRIMIDINONE COMPOUNDS AND THEIR USE - The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R | 09-04-2014 |
20140243353 | 5- OR 6-SUBSTITUTED 3-HYDROXY-2(1H)-PYRIDINONES AS D-AMINO ACID OXIDASE (DAAO) INHIBITORS IN THERAPY OF DISEASES SUCH AS SCHIZOPHRENIA, COGNITIVE DISORDER AND PAID - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R | 08-28-2014 |
20140243310 | BICYCLIC COMPOUND - The present invention provides a compound represented by the formula (I): | 08-28-2014 |
20140235879 | ORALLY DISPERSIBLE TABLET - The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture. | 08-21-2014 |
20140235709 | ORALLY DISPERSIBLE TABLET - The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture. | 08-21-2014 |
20140235615 | HETEROCYCLIC COMPOUND - Provided is a compound useful for the prophylaxis or treatment of cancer. | 08-21-2014 |
20140221381 | THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF - The present invention provides a compound represented by the formula: | 08-07-2014 |
20140206680 | SUBSTITUTED 6-AZA-ISOINDOLIN-1-ONE DERIVATIVES - Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R | 07-24-2014 |
20140205672 | RELEASE CONTROL COMPOSITIONS - A controlled release composition for oral administration, which comprises a physiologically active substance which is a compound represented by the formula: | 07-24-2014 |
20140205670 | STABLE SOLID PREPARATIONS - It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer. | 07-24-2014 |
20140171655 | DIPHOSPHINE LIGAND AND TRANSITION METAL COMPLEX USING THE SAME - The present invention provides a novel ligand represented by the following formula and a novel transition metal complex having the ligand, which shows superior enantioselectivity and catalytic efficiency, particularly high catalyst activity, in various asymmetric synthesis reactions. | 06-19-2014 |
20140163001 | HETEROCYCLIC COMPOUND - Provided is a heterocyclic compound having an RORγt inhibitory activity. A compound represented by the formula (I): | 06-12-2014 |
20140155584 | CONJUGATED ANTI-CD38 ANTIBODIES - Isolated antibodies that bind to human CD38 and cynomolgus CD38 are disclosed. Also disclosed are pharmaceutical compositions comprising the disclosed antibodies, and therapeutic and diagnostic methods for using the disclosed antibodies. | 06-05-2014 |
20140155437 | PROPHYLACTIC OR THERAPEUTIC METHOD FOR SJOGREN'S SYNDROME - The present invention provides a prophylactic or therapeutic agent and a prophylactic or therapeutic method superior in the prophylaxis or treatment of Sjogren's syndrome. Provided are a prophylactic or therapeutic agent for Sjogren's syndrome, containing a compound represented by the formula (I): | 06-05-2014 |
20140155416 | SUBSTITUTED PYRAZOLO[1,5-A] PYRIMIDINES AS CALCIUM RECEPTOR MODULATING AGENTS - There is provided a calcium receptor modulator comprising a compound of the formula (I): | 06-05-2014 |
20140100373 | PRODUCTION METHOD OF IMIDAZOLE DERIVATIVES - The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production. | 04-10-2014 |
20140100370 | METHOD AND APPARATUS FOR PRODUCING OXIDIZED COMPOUND - A method of producing an oxidized compound is disclosed. An electric potential is measured of an oxidation reaction solution for producing an oxidized compound by an oxidation reaction, and an end point is determined of the oxidation reaction on the basis of a predefined decrease of the electric potential. Preferably, after the electric potential of the oxidation reaction solution is reached to a highest electric potential, a point is determined where the amount of an electric potential dropped from the highest electric potential reaches the predefined amount of an electric potential as the end point of the oxidation reaction. The method also may introduce an oxidation reaction terminating agent to the oxidation reaction solution immediately after determining the end point of the oxidation reaction. | 04-10-2014 |
20140088146 | HETEROCYCLIC COMPOUNDS - The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. | 03-27-2014 |
20140088118 | HETEROCYCLIC COMPOUNDS - The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. | 03-27-2014 |
20140080891 | FUSED CYCLIC COMPOUNDS - The present invention provides a compound represented by the formula (I): | 03-20-2014 |
20140080817 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 03-20-2014 |
20140066499 | PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES - An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture. | 03-06-2014 |
20140066420 | HETEROCYCLIC COMPOUND - The present invention relates to | 03-06-2014 |
20140046056 | FUSED RING COMPOUND AND USE THEREOF - Provided is a novel compound represented by the following formula | 02-13-2014 |
20140046047 | ORGAN-SPECIFIC GENE, METHOD FOR IDENTIFYING THE SAME AND USE THEREOF - The present invention provides a method of extracting an organ- or tissue-specific highly expressed gene, including: (1) a step for measuring expression level of a specified gene group for each organ or tissue in 2 or more individuals, (2) a step for acquiring (a) a minimum value of expression levels in a particular organ or tissue in all individuals, and (b) a maximum value of expression levels in other organs and tissues in all individuals, for each gene, and (3) a step for extracting the gene as a gene highly expressed specifically in the particular organ or tissue if the above-described (a)/(b) ratio is larger than 1. By the present invention, truly organ- or tissue-specific genes are extracted. | 02-13-2014 |
20140031393 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 01-30-2014 |
20140024654 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use with PARP: | 01-23-2014 |
20140024650 | SULFONAMIDE DERIVATIVE AND USE THEREOF - Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): | 01-23-2014 |
20140023708 | LAMINATED TABLET AND MANUFACTURING METHOD THEREFOR - According to the present invention, a multilayer tablet showing suppressed layer separation and a production method thereof are provided. A concave portion having a depth of not less than 0.1 mm Ka is formed on at least one surface Sa of the both front and back surfaces (Sa, Sb) of a multilayer tablet. Particularly, a multilayer structure obtained by, in tableting, forming a convex portion for forming the concave portion on at least the upper punch, and preliminarily compressing all layers in the multilayer tablet with the upper punch to form a concave portion having the same shape with a depth of not less than 0.1 mm on the upper surface of all layers, wherein the powder materials of the next layer are protruding into the concave portion, is a preferable embodiment. | 01-23-2014 |
20140012006 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)- | 01-09-2014 |
20140011849 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 01-09-2014 |
20130345444 | PRODUCTION METHOD OF OPTICALLY ACTIVE DIHYDROBENZOFURAN DERIVATIVE - Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like. | 12-26-2013 |
20130345304 | COMPOUNDS FOR SUPPRESSING A PERIPHERAL NERVE DISORDER INDUCED BY AN ANTI-CANCER AGENT - The present invention provides a medicament that suppresses (or mitigates) various neurological symptoms caused by a peripheral nerve disorder induced by an anti-cancer agent. | 12-26-2013 |
20130324528 | PYRAZOLO[4,3-B]PYRIDINE-7-AMINE INHIBITORS OF ALK5 - The present invention provides ALK5 inhibitors of the formula | 12-05-2013 |
20130315895 | COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET - Methods for treating a disease state for which HGF/cMET possesses activity that contributes to the pathology and/or symptomology of the disease state, as well as kits and articles of manufacture for use in practicing these methods. | 11-28-2013 |
20130296276 | HETEROCYCLIC RING COMPOUND - The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. | 11-07-2013 |
20130281435 | THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME | 10-24-2013 |
20130274239 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Disclosed are compounds of the following formula: | 10-17-2013 |
20130273157 | ORALLY DISINTEGRATING TABLET - A orally disintegrating tablet is obtained by tableting fine granules showing controlled release of lansoprazole and an additive, which is capable of suppressing breakage of the fine granules during tableting, and can control the release of lansoprazole for a long time, and can maintain a therapeutically effective concentration for a prolonged time, and shows superior disintegration property in the oral cavity. | 10-17-2013 |
20130261156 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. | 10-03-2013 |
20130243859 | ORALLY DISINTEGRATING TABLET - The present invention relates to a multi-layer orally disintegrating tablet having (1) an enteric fine granule-containing layer containing a proton pump inhibitor and (2) an acetylsalicylic acid-containing layer, which shows high stability of the active ingredients (proton pump inhibitor, aspirin) and expresses the pharmacological effects of the active ingredients stably and rapidly after administration. | 09-19-2013 |
20130225813 | PROCESS FOR MAKING (R) -3-(2,3-DIHYDROXYPROPYL)-6-FLUORO-5-(2-FLOURO-4-IODOPHENYLAMINO)-8-METHYL- PYRIDO[2,3-d]PYRIMIDINE-4,7(3H,8H)-DIONE AND INTERMEDIATES THEREOF - The present invention relates generally intermediates for making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione. | 08-29-2013 |
20130210742 | SUSTAINED-RELEASE FORMULATION - The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic polymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably releases compound (I) or a salt thereof over a long period of time and exerts medicinal effects of compound (I) or a salt thereof over a long period of time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing frequency of administration, is an excellent formulation as a clinical medicine. | 08-15-2013 |
20130210060 | METHOD OF PRODUCING PANCREATIC HORMONE-PRODUCING CELLS - Disclosed is a production method of pancreatic hormone-producing cells in a form that mimics the pancreatogenesis, the method comprising subjecting stem cells to the following steps: (1) cultivating stem cells in a medium containing a Rho kinase inhibitor, (2) cultivating the cells obtained in (1) in a medium containing a GSK3 inhibitor, (3) cultivating the cells obtained in (2) in a medium containing GSK3 inhibitor and an activator of activin receptor-like kinase-4,7, (4) forming a cell mass from the cells obtained in (3), and cultivating the cell mass in a suspension state in a medium, (5) cultivating the cells obtained in (4) in a medium containing a retinoic acid receptor agonist, an inhibitor of AMP-activated protein kinase and/or activin receptor-like kinase-2,3,6, an inhibitor of activin receptor-like kinase-4,5,7 and a cell growth factor, and (6) cultivating the cells obtained in (5). | 08-15-2013 |
20130203731 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 08-08-2013 |
20130190291 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 07-25-2013 |
20130184272 | DIABETES THERAPEUTIC AGENT - The problem of the present invention is to provide a compound useful for the prophylaxis or treatment of diseases related to the control of the differentiation of muscle cell or adipocyte differentiation, such as diabetes, obesity, dyslipidemia, and having a superior efficacy. | 07-18-2013 |
20130184266 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 07-18-2013 |
20130184252 | DIHYDROPYRROLONAPHTHYRIDINONE COMPOUNDS AS INHIBITORS OF JAK - Disclosed are JAK inhibitors of formula I | 07-18-2013 |
20130172377 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions and methods comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile or a pharmaceutically acceptable salt thereof administered once weekly. | 07-04-2013 |
20130172292 | FUSED HETEROCYCLIC COMPOUNDS - The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R | 07-04-2013 |
20130171154 | ANTI-CD38 ANTIBODIES - Isolated antibodies that bind to human CD38 and cynomolgus CD38 are disclosed. Also disclosed are pharmaceutical compositions comprising the disclosed antibodies, and therapeutic and diagnostic methods for using the disclosed antibodies. | 07-04-2013 |
20130131050 | FUSED HETEROCYCLIC COMPOUND AND APPLICATION THEREOF - The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. | 05-23-2013 |
20130116260 | FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS - Disclosed are compounds of Formula 1, | 05-09-2013 |
20130115292 | ENTERIC TABLET - The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component. | 05-09-2013 |
20130115291 | ENTERIC TABLET - The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component. | 05-09-2013 |
20130090341 | HETEROCYCLIC COMPOUNDS - The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. | 04-11-2013 |
20130079397 | PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES - An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture. | 03-28-2013 |
20130079374 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 03-28-2013 |
20130072467 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases. | 03-21-2013 |
20130060052 | ORALLY DISPERSIBLE TABLET - The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture. | 03-07-2013 |
20130046000 | COMPOUNDS FOR SUPPRESSING A PERIPHERAL NERVE DISORDER INDUCED BY AN ANTI-CANCER AGENT - The present invention provides a medicament that suppresses (or mitigates) various neurological symptoms caused by a peripheral nerve disorder induced by an anti-cancer agent. | 02-21-2013 |
20130040951 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR CANCER - A compound represented by the formula (I): | 02-14-2013 |
20130035385 | ORALLY DISPERSIBLE TABLET - The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture. | 02-07-2013 |
20130035384 | ORALLY DISPERSIBLE TABLET - The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture. | 02-07-2013 |
20130029969 | HETEROCYCLIC COMPOUND - Provided is a compound useful for the prophylaxis or treatment of cancer. | 01-31-2013 |
20130022986 | METHOD FOR MANUFACTURING PANCREATIC-HORMONE-PRODUCING CELLS - The present invention provides a method of more efficiently producing pancreas cells, particularly pancreatic hormone-producing cells, a method of stably producing pancreas cells in a large amount by more efficiently inducing differentiation of stem cells into pancreas cells, a medicament containing a pancreas cells and a screening method using the cells. | 01-24-2013 |
20120316344 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 12-13-2012 |
20120316194 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 12-13-2012 |
20120302508 | SUSTAINED-RELEASE FORMULATION - The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic acid-glycolic acid copolymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably release compound (I) or a salt thereof for a long time and exerts a medicinal effect of compound (I) or a salt thereof for a long time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing the number of administration times, is an excellent formulation as a clinical medicine. | 11-29-2012 |
20120283120 | SCREENING METHOD - The present invention provides a novel variant androgen receptor (ARaiv) lacking ligand binding domain, a nucleic acid encoding the same and use thereof. That is, the present invention provides a method of screening for a substance for the prophylaxis or treatment of cancer, which includes contacting an ARaiv protein or ARaiv-producing cell with a test compound, measuring the activity of ARaiv (e.g., transcription regulating action of androgen responsive gene) or expression level thereof, and selecting a compound that suppresses the activity or expression level. | 11-08-2012 |
20120270865 | HETEROCYCLIC COMPOUND - Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy.
| 10-25-2012 |
20120264967 | PROCESS FOR MAKING (R) -3-(2,3-DIHYDROXYPROPYL)-6-FLUORO-5-(2-FLOURO-4-IODOPHENYLAMINO)-8-METHYL- PYRIDO[2,3-d]PYRIMIDINE-4,7(3H,8H)-DIONE AND INTERMEDIATES THEREOF - The present invention relates generally to processes of making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, intermediates thereof, and a process for making a particular polymorph of (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione. | 10-18-2012 |
20120264770 | HSP90 INHIBITORS - The invention relates to HSP90 inhibiting compounds consisting of the formula: | 10-18-2012 |
20120252761 | KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: | 10-04-2012 |
20120237502 | METHOD FOR TREATING BREAST CANCER AND OVARIAN CANCER - The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative. | 09-20-2012 |
20120225887 | Glucokinase Activators - Compounds are provided for use with glucokinase that comprise the formula: | 09-06-2012 |
20120220575 | N-SUBSTITUTED OXAZINOPTERIDINES AND OXAZINOPTERIDINONES - Disclosed are compounds of Formula 1, | 08-30-2012 |
20120220570 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-30-2012 |
20120220569 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-30-2012 |
20120214855 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. | 08-23-2012 |
20120214795 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-23-2012 |
20120208794 | FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. | 08-16-2012 |
20120202999 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 08-09-2012 |
20120201827 | ANTI-CD38 ANTIBODIES - Isolated antibodies that bind to human CD38 and cynomolgus CD38 are disclosed. Also disclosed are pharmaceutical compositions comprising the disclosed antibodies, and therapeutic and diagnostic methods for using the disclosed antibodies. | 08-09-2012 |
20120184584 | METHODS AND DRUG PRODUCTS FOR TREATING ALZHEIMER'S DISEASE - Provided herein are drug products with low dose pioglitazone for use in the treatment (e.g., delay of onset) of cognitive impairment of the Alzheimer's type. Methods of manufacture thereof are also provided. Further provided are methods of treatment for Alzheimer's disease including administering a drug product with low dose pioglitazone. The methods may include determining whether the subject is at risk of developing Alzheimer's disease based upon the subject's age and TOMM40 523 genotype. | 07-19-2012 |
20120178924 | HEXAHYDROOXAZINOPTERINE COMPOUNDS - The present invention relates to intermediates of the formula | 07-12-2012 |
20120172321 | HSP90 INHIBITORS - The invention relates to HSP90 inhibiting compounds consisting of the formula: | 07-05-2012 |
20120142005 | METHOD FOR SCREENING OF REGENERATIVE MEDICINE - A method for screening for a substance capable of regulating the regeneration, proliferation or differentiation of a cell or an organ, which comprises the steps of: (1) allowing a cell having a regenerative, proliferative or differentiative capability to form an embryoid body; (2) treating the embryoid body produced in step (1) with a digestive enzyme to prepare single cells from the embryoid body; (3) seeding the cells prepared in step (2) onto an adhesive plate, and adding a candidate substance to the plate to perform adhesion culturing of the cells on the plate; (4) conducting quantitative and simultaneous analysis of the levels of expression of at least two types of genes involved in the regeneration, proliferation or differentiation of cells after the adhesion culturing of step (3); and (5) evaluating the influence of the candidate substance on the regeneration, proliferation or differentiation of cells based on the results of the quantitative analysis obtained in step (4). | 06-07-2012 |
20120129868 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use with PARP: | 05-24-2012 |
20120122835 | Poly (ADP-Ribose) Polymerase (PARP) Inhibitors - Disclosed are compounds of the following formula: | 05-17-2012 |
20120095057 | PYRAZOLE COMPOUND - Provided is a compound having a superior acid secretion suppressive action, antiulcer activity and the like. | 04-19-2012 |
20120094992 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): | 04-19-2012 |
20120094899 | NEUROMEDIN U DERIVATIVE - An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) | 04-19-2012 |
20120094898 | PEPTIDE DERIVATIVE - The present invention relates to a peptide derivative selected from the group consisting of
| 04-19-2012 |
20120088826 | PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES - An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture. | 04-12-2012 |
20120088797 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 04-12-2012 |
20120077985 | PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME - The present invention provides an industrially advantageous process for producing a steroid C | 03-29-2012 |
20120077799 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 03-29-2012 |
20120071486 | THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF - The present invention provides a compound represented by the formula: | 03-22-2012 |
20120040981 | THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS - The present invention relates to a compound represented by the formula (I): | 02-16-2012 |
20120028951 | PYRIDAZINONE COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I | 02-02-2012 |
20120015868 | Metastin derivatives and use thereof - The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action. | 01-19-2012 |
20110319450 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 12-29-2011 |
20110312898 | PROPHYLACTIC / THERAPEUTIC AGENT FOR CANCER - A prophylactic/therapeutic agent for androgen-independent cancer is provided. A prophylactic/therapeutic agent for androgen-independent cancer includes a metastin derivative, and is particularly useful as a prophylactic/therapeutic agent for androgen-independent cancer, in particular, androgen-independent prostate cancer. | 12-22-2011 |
20110306769 | PROCESS FOR PRODUCING PYRROLE COMPOUND - The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. | 12-15-2011 |
20110301174 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 12-08-2011 |
20110301173 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 12-08-2011 |
20110300068 | AGENT FOR PROPHYLAXIS OR TREATMENT OF CANCER - The present invention provides an agent for the prophylaxis or treatment of kidney cancer or urinary bladder cancer, and a diagnostic reagent for these cancers which comprise an antibody against nerve growth factor 2/neurotrophin-3 or a partial peptide thereof or a salt thereof, which antibody neutralizes nerve growth factor 2/neurotrophin-3 and does not cross-react with the Nerve Growth Factor. | 12-08-2011 |
20110288040 | ARYL- OR HETEROARYL-SULFONYL COMPOUNDS AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like. | 11-24-2011 |
20110257405 | PROCESS FOR PRODUCING CRYSTAL - The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n′H | 10-20-2011 |
20110237620 | HETEROCYCLIC COMPOUND AND USE THEREOF - A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity. | 09-29-2011 |
20110212982 | Administration of Dipeptidyl Peptidase Inhibitors - Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 09-01-2011 |
20110212890 | METASTIN DERIVATIVE AND USE THEREOF - Disclosed is a stable metastin derivative having excellent biological activities (e.g., a cancer metastasis inhibiting activity, a cancer proliferation inhibiting activity, a gonadotropin secretion promoting activity, a sex hormone secretion promoting activity). A metastin derivative produced by substituting a constituent amino acid in metastin can be improved in stability in the blood and can have an excellent cancer metastasis inhibiting activity, an excellent cancer proliferation inhibiting activity, an excellent gonadotropin secretion inhibiting activity, an excellent sex hormone secretion inhibiting activity and the like by binding the metastin derivative to polyethylene glycol. | 09-01-2011 |
20110201818 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 08-18-2011 |
20110196003 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 08-11-2011 |
20110192748 | Administration of Dipeptidyl Peptidase Inhibitors - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 08-11-2011 |
20110190361 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 08-04-2011 |
20110190261 | MAPK/ERK Kinase Inhibitors - Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: | 08-04-2011 |
20110189282 | TABLET - The present invention can retain the volume of a tablet large without increasing the thickness of the tablet or the like dimension and prevents a plurality of tablets from sticking to each other even if they are subjected to a film-coating or the like treatment, so as to improve the yield. The tablet is a tablet ( | 08-04-2011 |
20110184178 | POLYMORPHS OF 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYLPIPERIDIN-4-YL)-9H-PY- RIDO[2,3-B]INDOLE-7-CARBOXAMIDE AND METHODS OF USE THEREFOR - The invention relates to polymorphic forms of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound I), which has the formula: | 07-28-2011 |
20110178070 | PI3K/mTOR INHIBITORS - The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: | 07-21-2011 |
20110172275 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 07-14-2011 |
20110172245 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula | 07-14-2011 |
20110172204 | COMPOUNDS AND THEIR USE - A compound of the formula: | 07-14-2011 |
20110158989 | Poly (ADP-Ribose) Polymerase (PARP) INHIBITORS - Disclosed are compounds of the following formula: | 06-30-2011 |
20110152273 | FUSED HETEROAROMATIC PYRROLIDINONES - Disclosed are compounds of Formula 1, | 06-23-2011 |
20110144161 | 1-HETEROCYCLYLSULFONYL, 2-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 06-16-2011 |
20110136780 | DIHYDROPYRROLONAPHTYRIDINONE COMPOUNDS AS INHIBITORS OF JAK - Disclosed are JAK inhibitors of formula I | 06-09-2011 |
20110130384 | AMIDE COMPOUND - The present invention aims to provide a prophylactic or therapeutic agent for schizophrenia and the like, containing the compound of the present invention having a GPR52 agonist activity. A compound represented by the following formula (I) or a salt thereof: | 06-02-2011 |
20110124876 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 05-26-2011 |
20110124875 | IMINOPYRIDINE DERIVATIVES AND USES THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 05-26-2011 |
20110124874 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 05-26-2011 |
20110124687 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. | 05-26-2011 |
20110124626 | BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS - A compound having the formula (1) wherein: R1 is a group selected from C | 05-26-2011 |
20110118172 | METASTIN DERIVATIVE AND USE THEREOF - The invention provides a stable metastin derivative having excellent biological activities (a cancer metastasis-inhibiting activity, a cancer proliferation-inhibiting activity, a gonadotropin secretion-promoting activity, a sex hormone secretion-promoting activity, etc.). By replacing the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, the blood stability and solubility of the metastin derivative can be more improved, the gel tendency of the metastin derivative can be reduced, the pharmacokinetics of the metastin derivative can be improved, and the metastin derivative can exhibit an excellent cancer metastasis-inhibiting activity and cancer proliferation-inhibiting activity. The metastin derivative can also exhibit a gonadotropin secretion-inhibiting activity, a sex hormone secretion-inhibiting activity, etc. | 05-19-2011 |
20110112133 | DIHYDRO PYRROLOQUINOLINE DERIVATIVES - A compound represented by the formula (I) | 05-12-2011 |
20110104705 | Musclin receptor and use thereof - The present invention provides a receptor of musclin and a screening system for an agonist and/or antagonist of the receptor by means of the interaction of musclin and the receptor. Hence, provided is a screening method for a substance that alters the bindability (i) a protein containing the same or substantially the same amino acid sequence as the amino acid sequence shown by SEQ ID NO:2 or a partial peptide thereof or a salt thereof and (ii) musclin or a partial peptide thereof or a salt thereof, containing using both. | 05-05-2011 |
20110098336 | PYRROLIDIN-2-ONE DERIVATIVES AS ANDROGEN RECEPTOR MODULATOR - A compound represented by the formula (I) according to claim | 04-28-2011 |
20110098297 | FUSED RING COMPOUNDS AND USE THEREOF - The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof. | 04-28-2011 |
20110091563 | ORALLY-DISINTERGRATING SOLID PREPARATION - The present invention provides an orally-disintegrating solid preparation such as a tablet produced by tabletting fine granules showing controlled release of a pharmaceutically active ingredient and an additive, and the like, and the orally-disintegrating solid preparation containing fine granules coated with a coating layer containing a polymer affording a casting film having an elongation at break of about 100-about 700%. With the preparation, breakage of fine granules during tabletting can be suppressed in the production of an orally-disintegrating solid preparation containing fine granules showing controlled release of a pharmaceutically active ingredient. | 04-21-2011 |
20110082111 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 04-07-2011 |
20110081412 | ORALLY DISINTEGRABLE TABLETS - An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 μm or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration. | 04-07-2011 |
20110077402 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 03-31-2011 |
20110070297 | GLUCOKINASE ACTIVATORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: | 03-24-2011 |
20110065733 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 03-17-2011 |
20110059888 | METASTIN DERIVATIVES AND USE THEREOF - The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids, the metastin derivatives of the present invention achieve more improved blood stability, solubility, etc., reduced gelation tendency, improved pharmacokinetics, as well as exhibit an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity. The metastin derivatives of the present invention also have a gonadotropic hormone secretion suppressing activity, sex hormone secretion suppressing activity, etc. | 03-10-2011 |
20110053921 | HEXAHYDROOXAZINOPTERINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula | 03-03-2011 |
20110053873 | HSP90 INHIBITORS - The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds. | 03-03-2011 |
20110052563 | GONADAL FUNCTION IMPROVING AGENTS - Metastin, compounds that promote the activity of metastin or its receptors and the like are excellent gonadal function improving agents, ovulation inducers or promoters, gonadotropic hormone secretion promoters, gonadotropic hormone secretion inhibitors, sex hormone secretion promoters, sex hormone secretion inhibitors, etc., and can be used as agents for preventing/treating sterility, hormone-sensitive cancers, endometriosis, etc. Metastin and its receptors are useful for screening for these pharmaceuticals. | 03-03-2011 |