DAIICHI SANKYO COMPANY, LIMITED Patent applications |
Patent application number | Title | Published |
20160137644 | METHOD FOR PRODUCING TRICYCLIC HETEROCYCLIC COMPOUND - It is an object of the present invention to provide a method for producing a high-purity tricyclic heterocyclic compound represented by formula (I), which is useful as a production intermediate for a pharmaceutical agent, wherein the method is an efficient production method with short steps and with a high yield, which does not use, as raw materials, expensive bromopyruvate and highly harmful copper chromite, and does not need silica gel column chromatography that generates, as by-products, large quantities of waste. The present invention relates to production of Compound (I) by the following method. | 05-19-2016 |
20160130663 | METHOD FOR PREDICTING RESPONSE TO CANCER TREATMENT - It has been found that BRG1 and BRM have a synthetic-lethal relationship, and that a treatment for inhibiting BRM is a promising approach for treating a BRG1-deficient cancer having no mutation in known therapeutic target genes. Moreover, it has also been revealed that, in this therapeutic strategy, a BRM inhibitor may be administered to a cancer patient after the selection based on BRG1 function suppression, thus enabling an efficient treatment based on the companion diagnosis. | 05-12-2016 |
20160129008 | Solid Dosage Form of Olmesartan Medoxomil and Amlodipine - The invention relates to a stable solid dosage form comprising olmesartan medoxomil and amlodipine or a pharmacologically acceptable salt thereof. In particular, it relates to solid dosage forms free from reducing sugars. The stable solid dosage form may optionally further comprise hydrochlorothiazide or a pharmacologically acceptable salt thereof. | 05-12-2016 |
20160128972 | METHOD FOR PREVENTING INFLUENZA VIRUS INFECTION BY ADMINISTERING A DRY POWDER PHARMACEUTICAL COMPOSITION - A method for preventing an influenza virus infection by administering by inhalation to a patient a pharmaceutically effective amount of a dry powder composition containing | 05-12-2016 |
20160096803 | CRYSTAL OF PYRROLE DERIVATIVE AND METHOD FOR PRODUCING THE SAME - The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R | 04-07-2016 |
20160081993 | SUBSTITUTED PHENYLAZOLE DERIVATIVE - Compounds are provided having an excellent hypoglycemic effect and β cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 03-24-2016 |
20160068603 | NOVEL ANTI-DR5 ANTIBODY - The present invention relates to an antibody which has a therapeutic effect on cancer, an autoimmune disease, or an inflammatory disease. That is, the present invention relates to an antibody which exhibits a cytotoxic activity against death domain-containing receptor-expressing cells through apoptosis. | 03-10-2016 |
20160068561 | Intermediate for Production of Nucleoside Analog and Method for Producing the Same - A compound represented by the general formula (III) which serves as an intermediate of an oligonucleotide analog having stable and excellent antisense or antigene activity or having excellent activity as a detection reagent (probe) for a specific gene or as a primer for the initiation of amplification of a specific gene can be produced at high yields regardless of the type of nucleobase by a method comprising reacting a compound represented by the general formula (II) or a salt thereof with a trimethylsilylated compound obtained from a compound represented by the general formula (IVb), wherein X, Y, Z, A, R, and B are as defined in claim | 03-10-2016 |
20160052906 | METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES - A method for manufacturing a compound represented by the following formula (I): | 02-25-2016 |
20160046639 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS - The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R | 02-18-2016 |
20160046568 | DICARBOXYLIC ACID COMPOUND - It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. Solution: A compound represented by a general formula (I) or a pharmacologically acceptable salt thereof. [In the formula, R | 02-18-2016 |
20160031987 | ANTI-EPHA2 ANTIBODY - The present invention provides an antibody which recognizes an epitope recognized by an antibody produced by a hybridoma SH348-1 (FERM BP-10836) or a hybridoma SH357-1 (FERM BP-10837), an antibody produced by the hybridoma SH348-1 or the hybridoma SH357-1, an antibody obtained by humanizing the antibody produced by the hybridoma SH348-1 or the hybridoma SH357-1, a pharmaceutical agent comprising the antibody as an active ingredient, etc. | 02-04-2016 |
20160024060 | BENZOTHIOPHENE DERIVATIVE - [Problem to be Solved] | 01-28-2016 |
20160017015 | GLYCO-MODIFIED ATRIAL NATRIURETIC PEPTIDE - The present invention provides a modified atrial natriuretic peptide that exhibits prolonged duration in blood and maintains cGMP elevating activity. The present invention provides a modified peptide in which at least one sugar substance is linked directly through a glycosidic bond or via a linker structure to at least one hANP peptide, or a pharmaceutically acceptable salt thereof, a medicament comprising the modified peptide or the salt thereof as an active ingredient, etc. | 01-21-2016 |
20160016974 | PREPARATION METHOD OF OPTICALLY ACTIVE DIAMINE COMPOUND - The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producing a compound represented by the formula (8d) using a stereoselective intramolecular cyclization reaction, and a method for producing a compound (1f) or a salt thereof, or a hydrate thereof, which is characterized by desulfonylation of the compound (8d). In each formula, R | 01-21-2016 |
20160002636 | ENA NUCLEIC ACID PHARMACEUTICALS CAPABLE OF MODIFYING SPLICING OF mRNA PRECURSORS - Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides. | 01-07-2016 |
20150376156 | NEURAMINIC ACID DERIVATIVES - A compound represented by the following formula (I): | 12-31-2015 |
20150376155 | METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES - A method for manufacturing a compound represented by the following formula (13): | 12-31-2015 |
20150366918 | METHOD OF CONSTRUCTING MASSES OF MYOCARDIAL CELLS AND USE OF THE MYOCARDIAL CELL MASS - The object of the present invention is to improve the post-transplantation engraftment rate of cardiomyocytes that have been purified to such an extent that they are free from non-cardiomyocytes and any components derived from other species. | 12-24-2015 |
20150366810 | SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release matrix preparation comprising (A) a pharmacologically active drug, (B) a combination of cellulose derivatives, and (C) mannitol. | 12-24-2015 |
20150353889 | Mait-like Cells and Method for Manufacturing Same - The object of the present invention is to provide a method for preparing induced pluripotent stem cells from MAIT cells, and providing induced pluripotent stem cells derived from MAIT cells. Another object of the present invention is to provide a method for preparing MAIT-like cells from induced pluripotent stem cells, and providing MAIT-like cells. Differentiation of the induced pluripotent stem cells having a MAIT cell-specific TCR gene can be induced to establish MAIT-like cells. | 12-10-2015 |
20150353577 | METHOD FOR PRODUCING (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE - It is an object of the present invention to provide a method for efficiently producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which is important as an intermediate compound for the production of an FXa-inhibiting compound. A method for producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which comprises treating an (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid with 1,3-dibromo-5,5-dimethylhydantoin or N-bromosuccinimide in a solvent. | 12-10-2015 |
20150344578 | ANTIBODY TARGETING OSTEOCLAST-RELATED PROTEIN Siglec-15 - To provide a method of detecting abnormal bone metabolism by using a gene strongly expressed in an osteoclast; a method of screening a compound having a therapeutic and/or preventive effect on abnormal bone metabolism; and a pharmaceutical composition for treating and/or preventing abnormal bone metabolism. Provision of a method of detecting abnormal bone metabolism by using the expression of human Siglec-15 gene as an index; a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation; and the like. | 12-03-2015 |
20150306214 | ADJUVANT FOR MUCOSAL VACCINE - An object of the present invention is to provide an adjuvant for a mucosal vaccine with high safety that induces a sufficient immune response on the mucosa. According to the present invention, an adjuvant for a mucosal vaccine comprising a protein complex composed of hemagglutinin (HA) subcomponents HA1, HA2, and HA3 of botulinum toxin is provided. | 10-29-2015 |
20150299318 | ANTI-SIGLEC-15 ANTIBODY - Provided is a pharmaceutical composition for treating and/or preventing abnormal bone metabolism targeting a protein encoded by a gene strongly expressed in osteoclasts. Specifically provided is a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation, and the like. | 10-22-2015 |
20150297748 | ANTIBODY-DRUG CONJUGATE - As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: | 10-22-2015 |
20150265680 | THERAPEUTIC AGENT FOR AMYOTROPHIC LATERAL SCLEROSIS - The present invention provides a therapeutic agent for amyotrophic lateral sclerosis comprising a growth hormone secretagogue receptor (GHS-R) agonist or a pharmaceutically acceptable salt thereof as an active ingredient. An object of the present invention is to provide a pharmaceutical product for amyotrophic lateral sclerosis for which no effective drug exists. The therapeutic agent for amyotrophic lateral sclerosis of the present invention comprises a GHS-R agonist typified by ghrelin as an active ingredient and is administered to a recipient individual having amyotrophic lateral sclerosis with non-serious dysphagia. The individual may also be unresponsive or insufficiently responsive to an existing therapeutic agent for ALS. | 09-24-2015 |
20150259314 | METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES - A method of manufacturing a compound represented by the formula R | 09-17-2015 |
20150239909 | PROCESS FOR THE PREPARATION OF (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE - The present invention relates to an improved and industrially advantageous process for the preparation of (1S, 4S, 5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one represented by the following formula (1) | 08-27-2015 |
20150238570 | THERAPEUTIC AGENT FOR HYPERTHERMIA - An object of the present invention is to provide a hypothermic agent for an animal, a therapeutic agent for hyperthermia in an animal, etc. The present invention provides a hypothermic agent for an animal, a therapeutic agent for hyperthermia in an animal, etc., the agents etc. comprising desacyl ghrelin or its derivative, or a pharmaceutically acceptable salt thereof as an active ingredient. | 08-27-2015 |
20150231083 | HYDROMORPHONE HYDROCHLORIDE-CONTAINING ORAL SUSTAINED-RELEASE PHARMACEUTICAL COMPOSITION - An object is to provide a hydromorphone hydrochloride- or oxycodone hydrochloride hydrate-containing sustained-release pharmaceutical composition for oral administration that reliably exhibits its main pharmacological effect and has excellent formulation stability that avoids dose dumping of the principal drug, such as alcohol resistance. The present invention provides a sustained-release pharmaceutical composition comprising (A) hydromorphone hydrochloride or oxycodone hydrochloride hydrate, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D | 08-20-2015 |
20150218123 | Preparation Method for Optically Active Bicyclic Gamma-Amino Acid Compound - An object of the present invention is to provide an optically active bicyclic γ-amino acid derivative in a high purity. The object can be attained by a mixture of compounds represented by the general formulas (I) and (I′), or a method for producing a compound represented by the general formula (VII) or a salt thereof via the compound (I): | 08-06-2015 |
20150216847 | CYCLOPROPANECARBOXYLIC ACID DERIVATIVE - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R | 08-06-2015 |
20150197546 | PEPTIDE LIBRARY AND USE THEREOF - It is intended to provide a peptide library. The present invention provides a peptide selected from the following (1) and (2): a peptide selected from the following (i) and (ii): (i) a peptide comprising the amino acid sequence represented by SEQ ID NO: 1 in the Sequence Listing and further comprising amino acid sequences encoded by nucleotide positions 8 to 42 and nucleotide positions 43 to 93 in the nucleotide sequence represented by SEQ ID NO: 14 in the Sequence Listing to flank the amino terminus and the carboxyl terminus, respectively, of the amino acid sequence; and (ii) a peptide comprising an amino acid sequence, derived from the amino acid sequence represented by SEQ ID NO: 1 in the Sequence Listing, in which conservative amino acid substitution, deletion, addition and/or insertion of 1 to 5 (inclusive) amino acids has occurred, wherein said substitution, deletion, addition and/or insertion has occurred at amino acids other than the 1st Xaa to the 12th Xaa counting from the amino terminus. | 07-16-2015 |
20150157613 | HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A′ B, D, R | 06-11-2015 |
20150152508 | NUCLEIC ACID BIOMARKER AND USE THEREOF - The present invention is directed to methods of identifying and treating a human subject harboring a tumor or other disease comprising assessing HRG gene expression at an mRNA level in the human subject and administering a treatment comprising an anti-HER3 antibody to the human subject whose HRG gene expression at an mRNA level is assessed as high. The present invention is also directed to methods of identifying a human subject harboring a tumor or other disease comprising assessing HRG gene expression at an mRNA level in the human subject and withholding a treatment comprising an anti-HER3 antibody to the human subject whose HRG gene expression at an mRNA level is assessed as low. | 06-04-2015 |
20150152132 | Intermediate for Production of Nucleoside Analog and Method for Producing the Same - A compound represented by the general formula (III) which serves as an intermediate of an oligonucleotide analog having stable and excellent antisense or antigene activity or having excellent activity as a detection reagent (probe) for a specific gene or as a primer for the initiation of amplification of a specific gene can be produced at high yields regardless of the type of nucleobase by a method comprising reacting a compound represented by the general formula (II) or a salt thereof with a trimethylsilylated compound obtained from a compound represented by the general formula (IVb), wherein X, Y, Z, A, R, and B are as defined in claim | 06-04-2015 |
20150152102 | PIPERIDINYLPYRAZOLOPYRIDINE DERIVATIVE - A compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R is an optionally substituted aryl group or an optionally substituted heteroaryl group. | 06-04-2015 |
20150136800 | TABLET DISPENSING AND MANAGING CONTAINER - An upper case with a stopper projection that extends downward between an outlet and a dispensing standby space, in a situation where a container body is closed. A lower case with a pusher member that is positioned on a side opposed to the stopper projection with respect to the dispensing standby space, in a situation where the container body is closed, the pusher member being configured to, during an operation for opening the upper case, push a tablet located in the dispensing standby space toward the outlet. During the operation for opening the upper case, the stopper projection is configured to get over a side surface of the tablet located in the dispensing standby space, and is configured to stop an outlet-side surface of a tablet succeeding to the tablet having been located in the dispensing standby space. A sensor unit detects passage of one tablet to the outlet. | 05-21-2015 |
20150125470 | NOVEL ANTI-SIGLEC-15 ANTIBODY - Provided is a pharmaceutical composition for the treatment and/or prophylaxis of abnormal bone metabolism targeting a protein encoded by a gene strongly expressed in osteoclasts. Specifically provided is a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation, and the like. | 05-07-2015 |
20150125454 | ANTI-FGFR2 ANTIBODY - The present invention provides an antibody which binds to a fibroblast growth factor receptor. | 05-07-2015 |
20150110880 | ORALLY DISINTEGRATING TABLET AND PRODUCTION PROCESS THEREFOR - Provided are an orally disintegrating tablet that quickly disintegrates when it is placed in the mouth or put into water, provides favorable taste, has a sufficient hardness in general production, transportation and use and is excellent in terms of storage stability, and a process for the production of the same which is excellent in terms of industrial production. An orally disintegrating tablet containing a drug, a crystalline cellulose having a bulk density of 0.23 g/cm | 04-23-2015 |
20150098945 | ANTI-ROBO4 ANTIBODY - The present invention relates to an antibody having an anti-angiogenesis activity. More specifically, the present invention relates to an antibody against ROBO4 and a pharmaceutical composition containing the antibody. An object of the present invention is to provide an anti-ROBO4 antibody having an anti-angiogenesis effect, a pharmaceutical composition or the like comprising the antibody, a method for suppressing angiogenesis using the antibody, etc. Another object of the present invention is to provide a method for producing the antibody. The antibody of the present invention activates the downstream signal of ROBO4 and has a suppressive activity against cell migration induced by VEGF or bFGF. The antibody of the present invention also exhibits an anti-angiogenic effects in in-vivo models. | 04-09-2015 |
20150056189 | CDR-MODIFIED ANTI-SIGLEC-15 ANTIBODY - Provided is a pharmaceutical composition for the treatment and/or prophylaxis of abnormal bone metabolism targeting a protein encoded by a gene strongly expressed in osteoclasts. Specifically provided is a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation, and the like. | 02-26-2015 |
20150051190 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS - The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R | 02-19-2015 |
20150038738 | Optical Resolution Methods for Bicyclic Compounds Using Enzymes - An object of the present invention is to efficiently produce an optically active bicyclic compound. The optically active bicyclic compound is efficiently produced using an enzyme. | 02-05-2015 |
20150011574 | (2-HETEROARYLAMINO) SUCCINIC ACID DERIVATIVES - The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by the formula (1) wherein R | 01-08-2015 |
20150010758 | TABLET, METHOD OF PRODUCING TABLET, TABLET MANAGEMENT DEVICE, TABLET VERIFICATION DEVICE AND PROGRAM STORAGE MEDIUM - A method of producing a tablet in which an uncoated tablet is coated by a coating agent, the method including: a coating process of coating uncoated tablets with a coating agent by spray coating the coating agent onto tablets that are churned and tumbled inside a container, and drying the tablets inside the container by supplying drying air into the container and exhausting air from the container, wherein spray coating conditions, including air supply temperature, air supply rate, and spray speed, are controlled according to the weight of the coating agent with which the uncoated tablets are coated, such that the humidity of air exhausted during spray coating is within a range of from 14% RH to 30% RH. | 01-08-2015 |
20140371457 | PROCESS FOR PRODUCTION OF QUINUCLIDINE COMPOUNDS - Provided is a production method for a cis-QMF, which has a low environmental burden and is industrially advantageous. Specifically provided is a production method for a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine hydrochloride, including: reacting a cis-trans isomer mixture of 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine with p-nitrobenzoic acid; resolving the resultant product to produce a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine p-nitrobenzoate; and converting the p-nitrobenzoate into a hydrochloride. | 12-18-2014 |
20140371249 | CRYSTAL OF A FREE TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVE - To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like. | 12-18-2014 |
20140357675 | Substituted Phenylazole Derivatives - Compounds are provided having an excellent hypoglycemic effect and β cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 12-04-2014 |
20140349991 | CHROMONE DERIVATIVE HAVING OSTEOGENESIS PROMOTING EFFECT - Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root. The compounds are represented by formula (I) or a pharmacologically acceptable salt thereof: | 11-27-2014 |
20140343052 | Phenylxanthene Derivatives - The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. | 11-20-2014 |
20140342401 | PROMOTER DERIVED FROM HUMAN GENE - The present invention relates to a transfected mammalian host cell whose ability to secrete a foreign protein has been enhanced by using a foreign gene expression vector having a promoter derived from a human gene, and a method for producing the foreign protein using the host cell. A method for enhancing the production of a foreign protein to be used in a pharmaceutical protein product in a host cell such as a cultured mammalian cell is provided. A promoter derived from a human gene having a promoter activity higher than that of a cytomegalovirus (CMV) promoter in a host cell such as a cultured mammalian cell is provided. | 11-20-2014 |
20140316123 | ENA NUCLEIC ACID PHARMACEUTICALS CAPABLE OF MODIFYING SPLICING OF mRNA PRECURSORS - Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides. | 10-23-2014 |
20140296569 | Optical Resolution Method for Bicyclic Compound Using Asymmetric Catalyst - An optically active bicyclic compound is efficiently produced by optical resolution using an optically active amine. | 10-02-2014 |
20140288008 | NOVEL BINDING PROTEINS FOR PCSK9 - The present disclosure relates to novel lipocalin muteins which bind to PCSK9. The disclosure also provides corresponding nucleic acid molecules encoding lipocalin muteins and methods for producing lipocalin muteins as well as their encoding nucleic acid molecules. | 09-25-2014 |
20140248269 | MEDICINAL AGENT FOR PREVENTING EXACERBATION OF MALIGNANT TUMOR, COMPRISING COMBINATION OF NATRIURETIC PEPTIDE RECEPTOR GC-A AND GC-B AGONISTS - Provided are a medicinal agent which is highly safe for use as the treatment of a malignant tumor and is capable of efficiently treating a malignant tumor, that is, a medicinal agent for treating a malignant tumor or for suppressing or preventing the exacerbation thereof, comprising at least one kind of natriuretic peptide receptor GC-A agonist and at least one kind of natriuretic peptide receptor GC-B agonist to be administered in combination; a therapeutic method comprising administering the agent; etc. | 09-04-2014 |
20140221437 | N-HETERO-RING-SUBSTITUTED AMIDE DERIVATIVE - Compounds having an excellent hypoglycemic effect and β cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 08-07-2014 |
20140221409 | NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): | 08-07-2014 |
20140221392 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 08-07-2014 |
20140221391 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 08-07-2014 |
20140213549 | Substituted Pyridine Compound - The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), | 07-31-2014 |
20140212439 | Anti-EPHA2 Antibody - The present invention provides an antibody which recognizes an epitope recognized by an antibody produced by a hybridoma SH348-1 (FERM BP-10836) or a hybridoma SH357-1 (FERM BP-10837), an antibody produced by the hybridoma SH348-1 or the hybridoma SH357-1, an antibody obtained by humanizing the antibody produced by the hybridoma SH348-1 or the hybridoma SH357-1, a pharmaceutical agent comprising the antibody as an active ingredient, etc. | 07-31-2014 |
20140187592 | NITROGEN-CONTAINING AROMATIC HETEROCYCLYL COMPOUND - The present invention provides a compound having excellent regulating action on blood lipid level. | 07-03-2014 |
20140187542 | AMINO GROUP-CONTAINING PYRROLIDINONE DERIVATIVE - A compound represented by the following formula (I) or a salt thereof: | 07-03-2014 |
20140178349 | Cycloalkyl-Substituted Imidazole Derivative - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R | 06-26-2014 |
20140171464 | PHARMACEUTICAL COMPOSITION CONTAINING DIAMINE DERIVATIVE - An object of the present invention is to provide a pharmaceutical composition containing compound I or a pharmacologically acceptable salt thereof, or a solvate thereof as an active ingredient, which is favorably dissolved in the neutral region. The present invention relates to a pharmaceutical composition containing (A) N | 06-19-2014 |
20140155398 | HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A′ B, D, R | 06-05-2014 |
20140142096 | Fused Substituted Aminopyrrolidine Derivative - A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure. | 05-22-2014 |
20140136157 | PRODUCT QUALITY CONTROL METHOD - A real-time release testing capable of constantly ensuring quality, a method for quality testing of a product using real-time release testing, a method for quality testing of an in-process product and/or an end product by real-time release testing, comprising the step of assessing the quality from design space established with only material attributes as inputs, and a manufacturing parameter-independent method for quality testing of a product using real-time release testing. | 05-15-2014 |
20140135292 | Phosphoric Acid Ester Derivatives - To provide a novel compound that has S1P lyase inhibitory ability and induces a reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by the general formula (I): | 05-15-2014 |
20140121220 | CRYSTALS OF PHENYLPYRROLE DERIVATIVE - Provided is a monomethanesulfonate of a phenylpyrrole derivative, having superior glucokinase activating activity and demonstrating remarkably improved solubility, hygroscopicity and stability as well as superior oral absorption, and crystals thereof. The present invention provides (2S)-2-(3-{5-[(55)-5-methyl-4,5-dihydro-1,3-oxazol-2-yl]-1H-pyrrol-2-yl}-5-{[5-(methylsulfonyl)pyrazin-2-yl]oxy}phenoxy)propan-1-ol monomethanesulfonate having superior glucokinase activating activity, crystals thereof, a pharmaceutical containing the same, and a preventive and/or therapeutic agent for diabetes and the like. | 05-01-2014 |
20140121196 | DISPIROPYRROLIDINE DERIVATIVES - A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R | 05-01-2014 |
20140100244 | Preventive And/Or Therapeutic Agent For Thromboembolism In Thromboembolism Patient With Severe Renal Impairment - It is intended to provide a highly safe, orally administrable preventive and/or therapeutic agent for thrombosis and/or embolism that can be applied to a thrombosis and/or embolism patient with severe renal impairment. The present inventors have found that even for a thrombosis and/or embolism patient with severe renal impairment, use of edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism while avoiding the risk of bleeding. The present inventors have also found that even for a thrombosis and/or embolism patient with severe renal impairment, edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism with safety over a long period. | 04-10-2014 |
20140094624 | Method for Producing Bicyclic Compound via Iminium Salt - The problem to be solved is to provide a method for producing a compound having excellent activity as an α | 04-03-2014 |
20140094623 | Method for Producing Bicyclic Compound via Claisen Rearrangement - The problem to be solved by the present invention is to provide a method for producing a compound having excellent activity as an α | 04-03-2014 |
20140080808 | TETRAHYDROTHIAZEPINE DERIVATIVE - The present invention relates to a compound represented by the following general formula (I) | 03-20-2014 |
20140073799 | THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY - To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): | 03-13-2014 |
20140073689 | Crystals of Substituted Cycloalkene Derivatives - To provide potassium salts of substituted pyrrolidine derivatives, which suppress the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, and crystals thereof. The present invention provides potassium(2-chloro-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide and potassium(2-bromo-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide, each of which suppresses the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, crystals thereof, and a pharmaceutical containing any of the same, and a prophylactic and/or therapeutic agent for sepsis containing any of the same. | 03-13-2014 |
20140073658 | Dipyridylamine Derivative - Disclosed herein are compounds, or pharmacologically acceptable salts thereof, having glucokinase activating activity. In various aspects, the compounds are represented by general formula (I), or pharmacologically acceptable salts thereof: | 03-13-2014 |
20140073622 | IMIDAZOLE CARBONYL COMPOUND - To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient. | 03-13-2014 |
20140072557 | MEDICINAL AGENT FOR SUPPRESSING MALIGNANT TUMOR METASTASIS - A medicinal agent for suppressing or preventing the metastasis of a malignant tumor, the agent comprising, as an active ingredient, at least one kind of vascular endothelial intracellular cGMP enhancer. | 03-13-2014 |
20140070446 | SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation. | 03-13-2014 |
20140065146 | ANTI-SIGLEC-15 ANTIBODY - Provided is a pharmaceutical composition for treating and/or preventing abnormal bone metabolism targeting a protein encoded by a gene strongly expressed in osteoclasts. Specifically provided is a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation, and the like. | 03-06-2014 |
20140050785 | DISSOLUTION PROPERTIES OF DRUG PRODUCTS CONTAINING OLMESARTAN MEDOXOMIL - A pharmaceutical tablet containing olmesartan medoxomil and amlodipine besylate, which has improved dissolvability. The composition contains (A) olmesartan medoxomil and (B) amlodipine besylate as active ingredients and (C) a calcium-containing additive. A method for treating or preventing hypertension by administering the pharmaceutical tablet to a patient. | 02-20-2014 |
20140045862 | Cycloalkane Derivatives - Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease. The present invention provides compounds represented by the following formula (I) or pharmacologically acceptable salts thereof: | 02-13-2014 |
20140024696 | ATROPISOMER OF PYRROLE DERIVATIVE - [Object] A prophylactic or therapeutic agent for a cardiovascular disease is provided. | 01-23-2014 |
20140018418 | METHODS OF TREATING OR PREVENTING H5N1 INFLUENZA - A method of treating or preventing H5N1 influenza by administering to a person in need thereof a pharmacologically effective amount of 5-acetamido-4-guanidino-9-O-hexanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid, 5-acetamido-4-guanidino-9-O-decanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid, 5-acetamido-4-guanidino-9-O-dodecanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid or 5-acetamido-4-guanidino-9-O-tetradecanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid. A method of preventing H5N1 influenza by administering to a person in need thereof a pharmacologically effective amount of 5-acetamido-4-guanidino-9-O-octanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid. | 01-16-2014 |
20140018417 | METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES - A method for manufacturing a compound represented by the formula (13): | 01-16-2014 |
20140010817 | Novel Antibodies and Uses Thereof - The present invention provides an antibody that recognizes a polypeptide comprising the amino acid sequence represented by SEQ ID NO: 15 in the Sequence Listing and has an anti-arthritic function, or a functional fragment thereof. | 01-09-2014 |
20140004120 | NOVEL ANTI-DR5 ANTIBODY | 01-02-2014 |
20130345428 | METHOD FOR PRODUCTION OF PRASUGREL HYDROCHLORIDE HAVING HIGH PURITY - A method for producing prasugrel hydrochloride with a reduced content of 2-acetoxy-5-[5-chloro-1-(2-fluorophenyl)-2-oxopentyl]-4,5,6,7-tetrahydrothieno[3,2-6]pyridine by carrying out the following steps: | 12-26-2013 |
20130338189 | CRYSTAL OF ANTI-BACTERIAL COMPOUND - It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety. | 12-19-2013 |
20130338156 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof. | 12-19-2013 |
20130337064 | PHARMACEUTICAL COMPOSITION - To provide pharmaceutical preparation exhibiting satisfactory dissolution property in a wide pH range. | 12-19-2013 |
20130316929 | PEPTIDE LIBRARY - The present invention provides a peptide selected from the following (i) and (ii): (i) a peptide having the amino acid sequence represented by SEQ ID NO: 1 in the Sequence Listing; and (ii) a peptide having an amino acid sequence derived from the amino acid sequence represented by SEQ ID NO: 1 in the Sequence Listing by the conservative amino acid substitution, deletion, addition, or insertion of 1 to (inclusive) amino acids except at the 1st Xaa to the 11th Xaa counting from the amino terminus. | 11-28-2013 |
20130280276 | ANTIBODY TARGETING OSTEOCLAST-RELATED PROTEIN SIGLEC-15 - An isolated antibody capable of binding Siglec-15 which inhibits osteoclast formation and/or osteoclastic bone resorption, or a functional fragment thereof. The heavy chain of the antibody comprises a CDRH1 comprising a sequence having at least 80% sequence identity to SEQ ID NO: 106, a CDRH2 comprising a sequence having at least 80% sequence identity to SEQ ID NO: 107, and a CDRH3 comprising a sequence having at least 80% sequence identity to one of SEQ ID NOS: 35, 45, 55, 65 or 80. The light chain of the antibody comprises a CDRL1 comprising a sequence having at least 80% sequence identity to SEQ ID NO: 73 or 83, a CDRL2 comprising a sequence having at least 80% sequence identity to SEQ ID NO: 108, and a CDRL3 comprising a sequence having at least 80% sequence identity to one of SEQ ID NOS: 40, 50, 60, 70, 90, 100 or 109. | 10-24-2013 |
20130253038 | Modified Single-Stranded Polynucleotide - It is intended to provide a polynucleotide that is resistant to RNase and has an RNA interference effect, etc. The present invention provides a single-stranded polynucleotide that is derived from a double-stranded polynucleotide comprising a sense strand polynucleotide corresponding to a target gene, and an antisense strand polynucleotide having a nucleotide sequence complementary to the sense strand polynucleotide, and has a structure in which the 5′-end of the antisense strand and the 3′-end of the sense strand are linked via a phenyl group-containing linker to form a phosphodiester structure at each of these ends. | 09-26-2013 |
20130249140 | METHOD OF PRODUCING A SOLID PREPARATION - A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which includes a step wherein a composition containing the compound represented by the formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying a mechanical stress to the composition. The compound of the formula (I) is as follows: | 09-26-2013 |
20130230501 | Cycloalkyl-Substituted Imidazole Derivative - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R | 09-05-2013 |
20130217733 | ACYLBENZENE DERIVATIVE - Provided are compounds having an excellent hypoglycemic action and a β cell- or pancreas-protecting action or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 08-22-2013 |
20130211084 | FREE CRYSTAL OF TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVE - To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like. | 08-15-2013 |
20130204009 | PROCESS FOR PREPARING BENZOIC ACID ESTERS - There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same. | 08-08-2013 |
20130203989 | CRYSTAL OF TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVE - To provide a hydrochloride of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90 and a crystal thereof. The present invention provides a hydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a crystal thereof, a medicament comprising the same, an anticancer agent comprising the same, and the like. | 08-08-2013 |
20130184308 | ACTIVATED BLOOD COAGULATION FACTOR X (FXa) INHIBITOR - An object of the present invention is to provide an activated blood coagulation factor X (FXa) inhibitor that reduces the risk of bleeding caused by the treatment of thromboembolism. The present invention provides an oral anticoagulant agent comprising a compound represented by the following formula ( | 07-18-2013 |
20130183297 | METHOD OF TREATING CANCERS AND A PHARMACEUTICAL COMPOSITION THAT MAY BE USED IN PRACTICING SAID METHOD - The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method. | 07-18-2013 |
20130178521 | Crystals of Substituted Cycloalkene Derivatives - To provide potassium salts of substituted pyrrolidine derivatives, which suppress the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, and crystals thereof. The present invention provides potassium(2-chloro-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide and potassium(2-bromo-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide, each of which suppresses the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, crystals thereof, and a pharmaceutical containing any of the same, and a prophylactic and/or therapeutic agent for sepsis containing any of the same. | 07-11-2013 |
20130172362 | Imidazothiazole Derivatives Having Proline Ring Structure - Compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and that exhibit anti-tumor activity are provided. Compounds provided by the present disclosure include imidazothiazole derivatives that inhibit interaction between Mdm2 protein and p53 protein and exhibit anti-tumor activity. | 07-04-2013 |
20130171694 | DNA ELEMENT HAVING THE ACTIVITY OF ENHANCING FOREIGN GENE EXPRESSION - Disclosed is a method for stably achieving high expression of a foreign gene in mammalian cells using a novel DNA element. More specifically disclosed is a DNA element which enhances the activation of transcription by changing the chromatin structure around a gene locus into which a foreign gene expression unit has been introduced. | 07-04-2013 |
20130165657 | PROCESS FOR PREPARATION OF OPTICALLY ACTIVE DIAMINE DERIVATIVE SALT - The problem to be solved is to produce, at high yields with high purity, anhydrous crystals of a compound represented by formula (1) that is an important intermediate for preparation of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof. The solution thereto is an industrial preparation process that provides, with high purity, anhydrous crystals of a compound represented by the following formula (1), which is an intermediate for the production of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof, wherein Boc represents a tert-butoxycarbonyl group. | 06-27-2013 |
20130158069 | PREVENTIVE AND/OR THERAPEUTIC AGENT FOR THROMBOEMBOLISM IN THROMBOEMBOLISM PATIENT WITH SEVERE RENAL IMPAIRMENT - It is intended to provide a highly safe, orally administrable preventive and/or therapeutic agent for thrombosis and/or embolism that can be applied to a thrombosis and/or embolism patient with severe renal impairment. The present inventors have found that even for a thrombosis and/or embolism patient with severe renal impairment, use of edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism while avoiding the risk of bleeding. The present inventors have also found that even for a thrombosis and/or embolism patient with severe renal impairment, edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism with safety over a long period. | 06-20-2013 |
20130144061 | PROCESS FOR PREPARING A COMPOUND BY A NOVEL SANDMEYER-LIKE REACTION USING A NITROXIDE RADICAL COMPOUND AS A REACTION CATALYST - The present invention provides a novel process for preparing a substituted aromatic compound such as an aromatic halo compound or a salt thereof through a transformation reaction of an aromatic diazonium salt from an aromatic amino compound at stable high yields utilizing a novel Sandmeyer-like reaction using a nitroxide radical compound as a reaction catalyst. | 06-06-2013 |
20130137723 | CRYSTAL OF ANTI-BACTERIAL COMPOUND - It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety. | 05-30-2013 |
20130102008 | Method for Screening for S1P Lyase Inhibitors Using Cultured Cells - To provide a method for screening using cultured cells, intended to find a compound which increases the amount of sphingosine-1-phosphate or dihydrosphingosine-1-phosphate by SPL inhibitory activity rapidly, simply and highly sensitively. Provided are: a rapid and simple measurement method employing a scintillation proximity assay (SPA); a method with greatly improved detection sensitivity to the activity of a compound by controlling the concentration of the vitamin B | 04-25-2013 |
20130078234 | ANTI B7-H3 ANTIBODY - An antibody exhibiting antitumor activity that binds to B7-H3, a functional fragment of the antibody, a pharmaceutical composition that includes the antibody or the functional fragment, methods for making the antibody or the functional fragment, methods for treating a tumor using the antibody or the functional fragment, and polynucleotides encoding the antibody or the functional fragment. | 03-28-2013 |
20130060036 | PROCESS FOR PRODUCTION OF QUINUCLIDINE COMPOUNDS - Provided is a production method for a cis-QMF, which has a low environmental burden and is industrially advantageous. Specifically provided is a production method for a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine hydrochloride, including: reacting a cis-trans isomer mixture of 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine with p-nitrobenzoic acid; resolving the resultant product to produce a cis-type 2-alkylspiro(1,3-oxathiolane-5,3′)quinuclidine p-nitrobenzoate; and converting the p-nitrobenzoate into a hydrochloride. | 03-07-2013 |
20130045994 | PYRIDINE DERIVATIVE - The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. A compound represented by the general formula (I): | 02-21-2013 |
20130035356 | CRYSTAL OF DIAMINE DERIVATIVE AND METHOD OF PRODUCING SAME - An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal form of N | 02-07-2013 |
20130035337 | FUSED BICYCLIC HETEROARYL DERIVATIVE - The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. | 02-07-2013 |
20130029977 | Fused substituted aminopyrrolidine derivative - A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure. | 01-31-2013 |
20130029964 | [5, 6] HETEROCYCLIC COMPOUND - An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R | 01-31-2013 |
20130022683 | METHOD FOR IMPROVING DISSOLUTION OF ANTICOAGULANT AGENT - It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as an agent for preventing and/or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention provides a method for producing a pharmaceutical composition containing a compound represented by formula (I), comprising the step of mixing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, one or more excipients selected from the group consisting of a sugar alcohol and a water-swelling additive, a disintegrant, and a binder under conditions for keeping the maximum water content of the granules during granulation at 10% or less. | 01-24-2013 |
20130022587 | Cycloalkyl-Substituted Imidazole Derivative - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R | 01-24-2013 |
20130012535 | SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation. | 01-10-2013 |
20130012532 | CYCLOPROPANECARBOXYLIC ACID DERIVATIVE - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R | 01-10-2013 |
20130012439 | COMPOSITION FOR NASAL ADMINISTRATION AND METHOD FOR PREPARING SAME - The invention provides a powdered composition for nasal administration, comprising a physiologically active peptide and cellulose acetate as the base, and having excellent nasal absorption for physiologically active peptides. | 01-10-2013 |
20130005796 | METHOD FOR PROLIFERATING CARDIOMYOCYTES USING MICRO-RNA - Disclosed are: a method for proliferating cardiomyocytes, wherein a miRNA that promotes the proliferation of cardiomyocytes is used; a vector for the treatment of heart diseases; and a pharmaceutical composition or the like for the treatment of heart diseases. Specifically disclosed are: a method for proliferating cardiomyocytes, which uses a miRNA that has a cardiomyocyte proliferation promoting action; a vector for the treatment of heart diseases, which comprises the miRNA; and a pharmaceutical composition or the like for the treatment of heart diseases, which contains the vector. The miRNA is preferably one selected from the group consisting of miR-148a, miR-148b, miR-152 and miR-373 that are mature miRNAs, precursors of the aforementioned miRNAs, and mutants and analogues of the miRNAs and the precursors. | 01-03-2013 |
20130005763 | SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of a drug in the lower gastrointestinal tract, and thereby provide a sustained-release solid preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release solid preparation containing (A) a pharmacologically active drug, (B) carboxyvinyl polymer, (C) povidone, and (D) carmellose sodium, xanthan gum, or sodium carboxymethyl starch. | 01-03-2013 |
20130004550 | SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D | 01-03-2013 |
20120316170 | Imidazole Derivative - To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): | 12-13-2012 |
20120316158 | OPHTHALMIC SOLUTION FOR TREATING OCULAR INFECTION COMPRISING LEVOFLOXACIN OR SALT THEREOF OR SOLVATE OF THE SAME, METHOD FOR TREATING OCULAR INFECTION, LEVOFLOXACIN OR SALT THEREOF OR SOLVATE OF THE SAME, AND USE THEREOF - Instillation of a 1.5% (w/v) levofloxacin ophthalmic solution three times a day, which is the dosage or dose regimen of the present invention, has features to cure bacterial conjunctivitis in a shorter time than instillation of a 0.5% (w/v) ophthalmic solution three times a day, which is the conventional dosage or dose regimen, and not to increase the rate of occurrence of side effects. Curing the ocular infection in a short time leads to shortening of the duration of exposure of the ocular-infection-causing bacterium to levofloxacin. Therefore, the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention is eventually expected to suppress emergence of the resistant bacterium resulting from the long-term use of the levofloxacin ophthalmic solution in the conventional dosage or dose regimen. In addition, it is confirmed that the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention directly inhibits the ocular-infection-causing bacterium such as | 12-13-2012 |
20120302614 | METHOD FOR IMPROVING CEREBRAL CIRCULATION OR TREATING A CEREBRAL BLOOD FLOW DISORDER - A method for improving cerebral circulation or treating a cerebral blood flow disorder, comprising administering a pharmacologically effective amount of an angiotensin II receptor blocker to a human. | 11-29-2012 |
20120264691 | MEDICAL COMPOSITIONS CONTAINING GHRELIN - It is provided a pharmaceutical composition stably containing ghrelin or its derivative, which is an endogenous growth hormone secretagogue (GHS) to a growth hormone secretagogue-receptor (GHS-R), comprising a aqueous solution containing the ghrelins having pH range of 2 to 7, wherein the aqueous solution having pH range of 2 to 7 is a buffer solution, especially, glycine hydrochloride buffer, acetate buffer, citrate buffer, lactate buffer, phosphate buffer, citric acid-phosphate buffer, phosphate-acetate-borate buffer or phthalate buffer, and the concentration of the ghrelins in the solution is from 0.03 nmol/mL to 6 μmol/mL. | 10-18-2012 |
20120263716 | METHOD OF TREATING CANCERS AND A PHARMACEUTICAL COMPOSITION THAT MAY BE USED IN PRACTICING SAID METHOD - The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method. | 10-18-2012 |
20120259111 | SEVEN-MEMBERED RING COMPOUND AND PHARMACEUTICAL USE THEREFOR - A compound having a 7-membered nitrogen-containing ring skeleton represented by the formula (I), which is useful for the prevention or treatment of diseases, in which chymase is involved | 10-11-2012 |
20120258991 | METHOD OF TREATING A CANCER BY ADMINISTERING A SPECIFIED DRUG - A method of treating a cancer selected from the group consisting of breast cancer, pancreatic cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma or leukemia. An effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride is administered to a patient having said cancer. | 10-11-2012 |
20120258978 | NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. | 10-11-2012 |
20120252854 | CRYSTALLINE FORMS OF THIAZOLIDINEDIONE COMPOUND AND ITS MANUFACTURING METHOD - A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: | 10-04-2012 |
20120245152 | 3-(BIARYOXY)PROPIONIC ACID DERIVATIVE - A compound of the general formula (I): | 09-27-2012 |
20120238759 | METHOD FOR MANUFACTURING A 6-SUBSTITUTED 1-METHYL-1H-BENZIMIDAZOLE DERIVATIVE AND AN INTERMEDIATE OF SAID METHOD - A method for manufacturing a 6-substituted 1-methyl-1H-benzimidazole derivative represented by the formula (IV) | 09-20-2012 |
20120220649 | MODIFIED DOUBLE-STRANDED POLYNUCLEOTIDE - The present invention provides a double-stranded polynucleotide having a sense strand polynucleotide consisting of a nucleotide sequence complementary to a target sequence in a target gene, and an antisense strand polynucleotide having a nucleotide sequence complementary to the sense strand polynucleotide, wherein an aryl or heteroaryl compound is bound to a phosphate group at the 5′-end of the antisense strand polynucleotide. | 08-30-2012 |
20120220609 | 5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE DERIVATIVE - The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by formula (1): | 08-30-2012 |
20120220593 | Substituted Acrylamide Derivative and Pharmaceutical Composition Comprising the Same - A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: | 08-30-2012 |
20120202833 | TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES - A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1). | 08-09-2012 |
20120172605 | METHOD FOR PRODUCING ASYMMETRIC TETRASUBSTITUTED CARBON ATOM-CONTAINING COMPOUND - The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent. | 07-05-2012 |
20120157437 | VLA-4 INHIBITORY DRUG - This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: | 06-21-2012 |
20120129891 | SULFONE DERIVATIVE - Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 05-24-2012 |
20120129832 | AMIDE DERIVATIVE - Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 05-24-2012 |
20120129762 | MOTILIN-LIKE PEPTIDE COMPOUND HAVING TRANSMUCOSAL ABSORBABILITY IMPARTED THERETO - The present invention aims at providing motilin-like peptide compounds that maintain the gastrointestinal motility stimulating activity of native motilin and which are adapted to have higher absorbability upon transmucosal administration. | 05-24-2012 |
20120114711 | PHARMACEUTICAL COMPOSITION HAVING IMPROVED SOLUBILITY - It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X (FXa), and is useful as an agent for preventing and/or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention relates to a solid pharmaceutical composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof, or a solvate thereof, wherein the content of the compound represented by formula (I) is 0.5% by weight or more and less than 15% by weight with respect to the total weight of the pharmaceutical composition. | 05-10-2012 |
20120108639 | NITROGEN-CONTAINING AROMATIC HETEROCYCLYL COMPOUND - The present invention provides a compound having excellent regulating action on blood lipid level that is represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein, in one embodiment, A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R | 05-03-2012 |
20120094383 | METHODS FOR INDUCING CELL DEATH IN PLURIPOTENT STEM CELLS AND DIFFERENTIATED CELLS OTHER THAN CARDIAC MYOCYTES - The present invention has as its object developing a method that does not involve genomic modification and which yet is capable of inducing cell death in pluripotent stem cells such as embryonic stem cells and induced pluripotent stem cells, as well as in differentiated cells other than cardiomyocytes derived from pluripotent stem cells, but not in cardiomyocytes. It has been revealed that by establishing a method capable of inducing cell death in cells other than cardiomyocytes in a very efficient manner by adding a substance having no recognized inherent toxicity or cell death inducing action to the culture conditions for pluripotent stem cells and non-cardiomyocytes, the stated problem can be solved without relying upon genomic modification. | 04-19-2012 |
20120077980 | METHOD FOR PRODUCING A SOLID PREPARATION - A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which includes a step wherein a composition containing the compound represented by the formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying a mechanical stress to the composition. The compound of the formula (I) is as follows: | 03-29-2012 |
20120071685 | METHOD FOR PRODUCING BICYCLIC gamma-AMINO ACID DERIVATIVE - Methods for producing compounds having activity as an α | 03-22-2012 |
20120071665 | METHOD FOR PRODUCING OLMESARTAN MEDOXOMIL - A method for producing high-purity olmesartan medoxomil is provided in which a solvent containing water is used in steps of tritylation and DMDO esterification of olmesartan. | 03-22-2012 |
20120071476 | MORPHOLINOPURINE DERIVATIVES - There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: | 03-22-2012 |
20120071467 | AMIDE DERIVATIVE - Compounds or pharmacologically acceptable salts thereof are provided. In various embodiments the compounds have an antagonistic effect on a neurokinin NK | 03-22-2012 |
20120064158 | DISSOLUTION PROPERTIES OF DRUG PRODUCTS CONTAINING OLMESARTAN MEDOXOMIL - A pharmaceutical tablet containing olmesartan medoxomil and amlodipine besylate, which has improved dissolvability. Said composition contains (A) olmesartan medoxomil and (B) amlodipine besylate as active ingredients and (C) a calcium-containing additive. A method of improving the dissolution properties of a pharmaceutical composition containing olmesartan medoxomil and amlodipine besylate by using said composition is also provided. | 03-15-2012 |
20120059172 | NOVEL SOLVATE CRYSTALS - Acetone solvate crystals of trityl olmesartan medoxomil are provided. | 03-08-2012 |
20120046327 | METHOD FOR INHIBITING THE INDUCTION AND FORMATION OF OSTEOCLASTS - Methods for (i) inhibiting the induction and formation of osteoclasts, (ii) inhibiting RANKL expression in osteoblasts, (ii) inhibiting the activation of osteoclasts and (iv) inhibiting a decrease in bone density by administering to a warm-blooded animal in need thereof a pharmacologically effective amount of a compound selected from the group consisting of olmesartan and olmesartan medoxomil, a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof. | 02-23-2012 |
20120041206 | PROCESS FOR PRODUCING DIAMINE DERIVATIVE - The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a process for industrially producing a compound (1) represented by the following formula (1): | 02-16-2012 |
20120040936 | CYCLIC COMPOUND HAVING SUBSTITUTED PHENYL GROUP - Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: | 02-16-2012 |
20120035369 | METHOD FOR PRODUCING OPTICALLY ACTIVE DIAMINE DERIVATIVE - The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a method for industrially producing a compound (1) or a compound (4), comprising: [Step 1]: adding a quaternary ammonium salt and a metal azide salt to water to prepare an aqueous solution of an azidification reagent complex comprising quaternary ammonium salt-metal azide salt, and subsequently dehydrating the aqueous solution using an aromatic hydrocarbon solvent to form a mixed solution of the azidification reagent complex comprising quaternary ammonium salt-metal azide salt and the aromatic hydrocarbon solvent with a water content of 0.2% or less; and [Step 2]: adding, to the mixed solution prepared in [Step 1], a compound (2) wherein L represents a leaving group. | 02-09-2012 |
20120034215 | ANTI-MST1R ANTIBODIES AND USES THEREOF - The present disclosure provides recombinant antigen-binding regions and antibodies and functional fragments containing such antigen-binding regions that are specific for MST1R, which plays an integral role in various disorders or conditions, such as cancer. These antibodies, accordingly, can be used to treat these and other disorders and conditions. Antibodies of the disclosure also can be used in the diagnostics field, as well as for further investigating the role of MST1R in the progression of disorders associated with tumors. The disclosure also provides nucleic acid sequences encoding the foregoing antibodies, vectors containing the same, pharmaceutical compositions and kits with instructions for use. | 02-09-2012 |
20120029026 | PYRIDINE DERIVATIVE - The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) γ. A compound represented by the general formula (I): | 02-02-2012 |
20110319468 | CYCLIC AMINE COMPOUNDS - Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof | 12-29-2011 |
20110319359 | INDANYL COMPOUNDS - Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof: | 12-29-2011 |
20110312991 | ACTIVATED BLOOD COAGULATION FACTOR INHIBITOR - An object of the present invention is to provide a novel salt form of a compound that exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as a preventive and/or therapeutic drug for thrombotic diseases, and crystals thereof. The present invention provides N | 12-22-2011 |
20110312990 | Diamine Derivatives - A compound represented by the general formula (1): | 12-22-2011 |
20110281823 | Pharmaceutical preparation containing an angiotensin II Receptor antagonist, a calcium channel blocker and polyvinyl alcohol - A pharmaceutical preparation including a pharmacologically effective amount of a combination of active ingredients containing an angiotensin II receptor antagonist, a calcium channel blocker and polyvinyl alcohol, wherein the polyvinyl alcohol is in an amount of 5 to 85% by weight of the total weight of the pharmaceutical preparation. A method for the prophylaxis or treatment of hypertension by administering a pharmaceutically effective amount of the pharmaceutical preparation to a patient. | 11-17-2011 |
20110275821 | METHOD FOR PRODUCING DIAMINE DERIVATIVE - The present invention provides a method for producing a compound represented by formula (A), the method comprising the steps of: (a) mixing a compound represented by formula (B) with p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate at less than 1 molar equivalent with respect to the compound represented by formula (B) in a solvent under heating; (b) adding additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate to the mixed solution under cooling, wherein the additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate is added in such an amount that the total molar equivalent thereof with the p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate of step (a) is 1 molar equivalent or more with respect to the compound represented by formula (B) of step (a); and (c) subsequently allowing the mixed solution to crystallize to obtain the compound represented by formula (A). | 11-10-2011 |
20110275666 | ACTIVATED BLOOD COAGULATION FACTOR X (FXA) INHIBITOR - An object of the present invention is to provide an activated blood coagulation factor X (FXa) inhibitor that reduces the risk of bleeding caused by the treatment of thromboembolism. The present invention provides an oral anticoagulant agent comprising a compound represented by the following formula (1): | 11-10-2011 |
20110269942 | ANTIBODIES MODIFIED WITH HYDROPHOBIC MOLECULE - The present invention relates to an immunoliposome preparation or a hydrophobic molecule-modified antibody having a therapeutic effect on cancer, autoimmune disease, or inflammatory disease. Specifically, the present invention relates to an immunoliposome or a hydrophobic molecule-modified antibody comprising, as a constituent, an antibody capable of inducing the apoptosis of cells expressing a death domain-containing receptor. | 11-03-2011 |
20110269746 | CYCLIC COMPOUND HAVING HETERO ATOM - Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: | 11-03-2011 |
20110263673 | Atropisomers of (Hydroxyalkyl) Pyrrole Derivatives - The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R | 10-27-2011 |
20110263544 | 1-Phenylpyrrole Derivatives - The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R | 10-27-2011 |
20110257401 | PROCESS FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID - It has been demanded to provide a process for industrially producing an intermediate for a compound that exhibits an inhibitory effect on activated blood coagulation factor X and is useful as a preventive and/or therapeutic agent for thrombotic diseases. The present invention provides a process for producing the (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid, comprising reacting 3-cyclohexene-1-carboxylic acid and (R)-α-phenylethylamine using a mixed solvent of water and acetone or a mixed solvent of water and ethyl acetate as a solvent. | 10-20-2011 |
20110256188 | DRY POWDER PHARMACEUTICAL COMPOSITION FOR INHALATION - There is provided a dry powder pharmaceutical composition for inhalation useful for preventing and/or treating influenza virus infections contains as a medicinal component a compound represented by formula (I): | 10-20-2011 |
20110223175 | Gene Encoding G-Protein Coupled Receptor And Gene Product Thereof - The present invention, the objects of which are to find out a gene encoding a protein having functions equivalent to those of G-protein-coupled receptor (GPCR) and the protein, and to provide a method for identifying a compound that regulates functions and/or expression of the protein, and to provide a useful mean for preventing and/or treating diseases related to the gene and the protein, provides a DNA comprising base sequence described in SEQ ID NO: 1 or complementary strand thereof, complementary strand of the DNA, a protein encoded by the DNA, a vector containing the DNA, a transformant containing the vector, an antibody against the protein, a method for identifying a compound that regulates functions and/or expression of the protein using aforementioned members, an agent for improving and a method for improving depression state, a pharmaceutical composition, and a reagent kit. | 09-15-2011 |
20110201814 | METHOD FOR PRODUCING SOLID PREPARATION - A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which comprises a step wherein a composition containing the compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying mechanical stress to the composition. The compound of the formula (I) is as follows: | 08-18-2011 |
20110166343 | THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY - To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): | 07-07-2011 |
20110166342 | 7-MEMBERED RING COMPOUND AND METHOD OF PRODUCTION AND PHARMACEUTICAL APPLICATION THEREOF - A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: | 07-07-2011 |
20110160462 | CRYSTALLINE FORMS OF THIAZOLIDINEDIONE COMPOUND AND ITS MANUFACTURING METHOD - Thiazolidinedione compound crystalline forms useful as a bulk material for the manufacture of a peroxisome proliferator-activated receptor (PPAR) γ activator or an anticancer pharmaceutical composition are provided, which are hydrate crystalline forms of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimi dazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by Formula (I) below and of its dihydrochloride. | 06-30-2011 |
20110159049 | PHARMACEUTICAL COMPOSITION - The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube. | 06-30-2011 |
20110144339 | METHOD FOR PRODUCING ASYMMETRIC TETRASUBSTITUTED CARBON ATOM-CONTAINING COMPOUND - The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent. Specifically, the invention provides a method for producing a compound of formula (2): | 06-16-2011 |
20110124692 | CRYSTALLINE FORMS OF THIAZOLIDINEDIONE COMPOUND AND ITS MANUFACTURING METHOD - Thiazolidinedione compound crystalline forms useful as a bulk material for the manufacture of a peroxisome proliferator-activated receptor (PPAR) γ activator or an anticancer pharmaceutical composition are provided, which are hydrate crystalline forms of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimi dazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by Formula (I) below and of its dihydrochloride. | 05-26-2011 |
20110112103 | 5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE COMPOUND - The present invention provides compounds which promote erythropoietin production. Compounds represented by the following general formula (1) or pharmacologically acceptable salts thereof are provided: | 05-12-2011 |
20110092713 | METHOD FOR PRODUCING 1-BIPHENYLMETHYLIMIDAZOLE COMPOUND - The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. | 04-21-2011 |
20110092555 | Thiazolidinedione compound - A compound which is 5-{4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride, in crystal form wherein a powder x-ray diffraction pattern obtained by irradiation with a Cu Kα line shows main peaks at interplanar spacings d=14.29, 7.12, 5.34, 4.97, 4.74, 3.95, 3.85, 3.75, 3.55, 3.51, 3.15, 2.84, 2.76, 2.52 and 2.37. | 04-21-2011 |
20110082138 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof. | 04-07-2011 |
20110077266 | Diamine Derivatives - The present invention relates to diamine compounds which inhibit activated blood coagulation factor X and exhibit an anticoagulant effect and there uses for treating various diseases based on thromboembolism. | 03-31-2011 |
20110071170 | TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES - A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1). | 03-24-2011 |
20110053974 | CARBOXYLIC ACID COMPOUND - To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ═C(R5)- or ═N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R | 03-03-2011 |
20110053933 | HYDROXYQUINOXALINECARBOXAMIDE DERIVATIVE - The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: | 03-03-2011 |
20110039783 | PEPTIDE HAVING HYPOTENSIVE ACTIVITY - The present invention provides a novel peptide having a physiological activity. Because of having a hypotensive activity, this novel peptide is useful in treating a disease caused by hypertension. Also, an antibody to the novel peptide is provided. | 02-17-2011 |
20110014651 | METHOD FOR HIGH-LEVEL SECRETORY PRODUCTION OF PROTEIN - This invention provides a means for high-level secretory production of a protein, and, in particular, a protein having a complicated structure such as an antibody, in a host cell such as a yeast cell. This invention provides a method for high-level secretory production of a foreign protein with the use of a transformed host cell having one or more types of chaperone protein genes and via suppression of O sugar chain inherent to a host cell such as a yeast cell. | 01-20-2011 |
20110009471 | Oligonucleotide analogues and methods utilizing the same - A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): | 01-13-2011 |
20100310597 | ANTI-OFLOXACIN MONOCLONAL ANTIBODY AND IMMUNOASSAY OF OFLOXACIN USING THE SAME - A method that accurately and conveniently detects a compound shown by the formula (I) in a human sample is disclosed. An antibody that reacts with the compound shown by the formula (I), but does not cross-react with the N-oxide metabolite and the desmethyl levofloxacin metabolite of the compound shown by the formula (I) is prepared using an antigen produced by binding bovine serum albumin to the compound shown by the formula (I) through the 6-position carboxyl group. | 12-09-2010 |
20100297767 | NOVEL CELL CULTURE AND METHODS OF PRODUCING AND COLLECTING CELL MASSES USING THE SAME - The inventors of the present invention have developed a novel cell culture method with a view to providing a process by which cell masses uniform in size and properties can be produced in large quantities and with convenience, as well as a method of recovering them. | 11-25-2010 |