Abstract: The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) [wherein each symbol is as defined in the description] or a pharmacologically acceptable salt thereof, or a solvate of the derivative or the pharmacologically acceptable salt.

Abstract: The invention provides a method of inhibiting binding between acetylated histone and a bromodomain-containing protein in a mammal, as well as a method of shrinking or killing of cancer cells expressing a bromodomain-containing protein or inhibiting the growth of cancer cells expressing a bromodomain-containing protein in a mammal. The methods involve administering an effective amount of (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide or a dihydrate thereof to the mammal.

Abstract: Highly-purified soluble thrombomodulin which has a content of host cell-originated proteins being in a ratio of less than 10 ng of the proteins per 10,000 U of the soluble thrombomodulin, wherein the soluble thrombomodulin is produced by a transformant cell obtained by transfecting a host cell with a DNA containing a nucleotide sequence encoding the soluble thrombomodulin.

Abstract: Provided is a pyrazolopyrimidine compound represented by formula (I) having an HIF-PHD inhibitory effect, or a pharmaceutically acceptable salt thereof. [In the formula, represents an optionally substituted 7-hydroxypyrazolo[4,3-d]pyrimidine-5-yl, X represents a simple bond or an optionally substituted straight-chain alkylene, Z represents hydrogen atom, or formula (i), formula (ii) or formula (iii) and rings A and A? are independently an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted alicyclic hydrocarbon, or an optionally substituted non-aromatic heterocycle.

Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I] which is useful as a renin inhibitor. wherein R1 is a cycloalkyl group or an alkyl, R22 is an optionally substituted aryl and the like, R is a lower alkyl group, R3, R4, R5 and R6 are the same or different, and are a hydrogen atom, an optionally substituted carbamoyl, an optionally substituted alkyl, or alkoxycarbonyl, or a pharmaceutically acceptable salt thereof.

Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C—F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N—R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

Abstract: The present invention provides an industrially advantageous method for producing a 1,4-benzoxazine compound useful as a medicine while avoiding safety and health risks. Specifically, the present invention provides a method for producing a 1,4-benzoxazine compound [A], which comprises the three steps in the following scheme, namely, a step of converting the amino group at 7-position in a compound [a] into a dimesylamino group, a step of coupling a compound [b] with a boronic acid compound, and a step of converting the 7-position in a compound [c] into a monomesylamino group. In the above scheme, Ms is a methanesulfonyl group, and each of R? and R? is a hydrogen atom etc.

Abstract: Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.

Abstract: [Problem] To provide the following: an agent for treating cancer, particularly an agent for inhibiting cancer cell proliferation or an agent for inhibiting or preventing cancer metastasis; drug that uses the agent; a method for assessing the effect of cancer treatment; a method for estimating the prognosis of cancer treatment; a method for screening for a substance having a cancer proliferation-inhibiting effect; and a method for screening a substance having a cancer metastasis-impeding effect. [Solution] Provided is a drug containing a nucleic acid formed from a nucleotide sequence having sequence identity of 70% or greater with at least sequence No. 1 or No. 2, wherein the nucleic acid shows protein expression-inhibiting activity.

Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.

Abstract: Pyrimidone derivatives of formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.

Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.

Abstract: The present invention provides a pharmaceutical formulation comprising paraoxonase (PON), a purification and stabilization method of PON, and an agent for prophylactic and/or therapeutic treatment of a disease resulting from ischemia reperfusion and/or cerebral infarction containing PON as an active ingredient.

Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Abstract: The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.

Abstract: The present invention provides a pharmaceutical formulation comprising paraoxonase (PON), a purification and stabilization method of PON, and an agent for prophylactic and/or therapeutic treatment of a disease resulting from ischemia reperfusion and/or cerebral infarction containing PON as an active ingredient.

Abstract: The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Ra and Rb represent the same or different lower alkyl groups; and X1 represents a halogen atom.

Abstract: Provided is a composition for preventing or treating osteoporosis. The composition contains an ibandronic acid, or a pharmaceutically acceptable salt thereof, or a hydrate thereof, and vitamin D. The composition has uniform medicinal effects by minimizing the differences in physical properties between ibandronic acid, or the pharmaceutically acceptable salt thereof, or the hydrate thereof, and vitamin D.

Abstract: A medicament effective for prophylactic and/or therapeutic treatment of a peripheral neuropathic pain such as allodynia caused by a treatment with an anticancer agent, which comprises thrombomodulin as an active ingredient.

Abstract: A medicament for therapeutic treatment and/or improvement of sepsis in a patient with severe sepsis accompanied with one or more organ dysfunctions, wherein a value of International Normalized Ratio (INR) of a plasma specimen obtained from said patient is more than 1.4, which comprises thrombomodulin as an active ingredient.