Abstract: (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in “isolated rat bladder smooth muscle relaxation test”, dose-dependently lowers the contraction frequency of rhythmic bladder contractions in “rat rhythmic bladder contraction measurement test” and, moreover, prolongs the urination intervals in “urination functions measurement test on cyclophosphamide-induced overactive bladder model rat”. Owing to these effects, the above compound is useful as a remedy for ovaractive bladder.

Abstract: Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings.

Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.

Abstract: The present invention relates to a compound WS727713, useful as a modulator of melanocortin receptors, and a process for its production by culturing in a culture medium the actinomycetes strain of the genus Pseudonocardia, deposit number FERM BP-7570 and recovering the compound.

Abstract: A granular pharmaceutical composition for oral administration, comprising (1) atorvastatin or a pharmaceutically acceptable salt thereof, (2) a surfactant selected from the group consisting of sodium laurylsulfate and polyoxyethylene hydrogenated castor oil, and (3) a water-soluble polymer, is disclosed.

Abstract: A pharmaceutical composition for oral administration, comprising 3-hydroxy-N1-(4-methoxybenzoyl)-N2-[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]-1,2-phenylenediamine or a pharmaceutically acceptable salt thereof, and hydroxypropyl cellulose having a viscosity of approximately 6 mPa·S (inclusive) to approximately 150 mPa·S (exclusive) in a 2% aqueous solution at 20° C., or a viscosity of 75 mPa·S (inclusive) to 400 mPa·S (inclusive) in a 5% aqueous solution at 25° C., and a process of manufacturing the pharmaceutical composition for oral administration are disclosed.

Abstract: A convenient screening tool and a convenient screening method for obtaining an agent for treating diabetes, a pharmaceutical composition for treating diabetes, and a process for manufacturing the pharmaceutical composition are disclosed. The screening tool is a G protein-coupled receptor, a variation functionally equivalent thereto, or a homologous polypeptide thereof which promotes insulin secretion under a high glucose concentration by activation, or cells transformed with an expression vector comprising a polynucleotide encoding the above polypeptide and expressing the polypeptide.

Abstract: A pharmaceutical composition for modified release, comprising (1) (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof, (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 5 mL or less, and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25° C. is disclosed.

Abstract: The invention provides an agent for promoting ocular tissue neuritogenesis, containing N-(1-acetylpiperidin-4-yl)-4-fluorobenzamide or a pharmaceutically acceptable salt thereof, and an agent for promoting corneal neuritogenesis and retinal neuritogenesis, containing N-(1-acetylpiperidin-4-yl)-4-fluorobenzamide or a pharmaceutically acceptable salt thereof. The corneal neuritogenesis promoter can be used for the improvement of corneal sensitivity, treatment of dry eye, or treatment of a corneal epithelial disorder. The retinal neuritogenesis promoter can be used for the improvement of a visual dysfunction.

Abstract: A granular pharmaceutical composition for oral administration, wherein a drug-containing particle is coated with a coating comprising a methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymer and a water-soluble polymer is disclosed.

Abstract: The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.

Abstract: The present invention provides a screening tool and screening method for obtaining a substance useful as a prophylactic and/or therapeutic drug for diseases associated 5 with 5-HT production/secretion abnormalities, including digestive organ diseases, and a prophylactic and/or therapeutic drug for diseases associated with 5-HT production/secretion abnormalities, including digestive organ diseases. Examples of digestive organ diseases in the present invention include constipation type irritable bowel syndrome, functional dyspepsia, constipation, diarrhea type irritable bowel syndrome, diarrhea and vomiting.

Abstract: The present invention provides a vector containing a DNA construct containing a first promoter that is a nitrilase gene promoter, a multicloning site and a nitrilase transcription regulatory protein gene (particularly preferably a structural gene is ligated into a multicloning site and a second promoter is placed at the upstream of the nitrilase transcription regulatory protein gene), and the like. The present invention affords a high expression system capable of expressing a large amount of useful proteins by actinomycete host represented by actinomycete belonging to the genus Streptomyces and the like beneficially used for the production of useful proteins.

Abstract: The present invention relates to an agent for preventing and/or treating diabetic neuropathy comprising a 2-[(substituted-inden-7-yloxy)methyl]morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing and/or treating diabetic neuropathy, and particularly useful for providing an agent for preventing and/or treating diabetic motor neuropathy (such as muscle weakness disorder (such as muscle weakness disorder with inability to walk independently)), diabetic sensory neuropathy (such as paresthesia (such as vibration perception abnormality), allodynia, hypoesthesia (such as numbness of extremities or cold sensation), or pain), or diabetic autonomic neuropathy (such as stool abnormality (such as constipation or diarrhea), urination disorder, impotence, orthostatic hypotension, sudomotor dysfunction, abnormal heart rate variability, or delayed gastric emptying).

Abstract: [Problem] Provided is a compound, which exhibits a P2Y12 inhibitory action and is useful as a medical drug, particularly, as a platelet aggregation inhibitor. [Means for Solution] The inventors have eagerly investigated P2Y12 inhibitors. As a result, the inventors have found that a bicyclic heterocyclic compound such as quinazolinedione, isoquinolone, and the like having an amino group substituted with lower alkyl, cycloalkyl, or lower alkylene-cycloalkyl at the specific position exhibits an excellent platelet aggregation inhibitory action, thereby completing the present invention. Since the compound of the invention exhibits excellent P2Y12 inhibitory action and platelet aggregation inhibitory action, it is useful as a platelet aggregation inhibitor.

Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.

Abstract: [Problems] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

Abstract: The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention. More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g.

Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.

Abstract: The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.