Abstract: The present invention relates to a medicament for treating neuropsychiatric diseases, comprising a compound of Formula (1): or a pharmaceutically acceptable salt thereof, as an active ingredient.

Abstract: The present invention relates to a medicament for treating various nervous system diseases or psychiatric diseases, comprising a compound of formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient, wherein R1 is hydrogen, etc., R2 is halogen, etc., R3, R4, R5, and R6 are hydrogen, etc.

Abstract: The compound of formula (1a) wherein p is 1 or 2, R1-R4 are hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.

Abstract: The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter wherein R1-L- is R1—OC(O)—, or the like, R1 is hydrogen atom, optionally-substituted C1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R3 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like, the part of X, Y, and Z is X?Y—Z, X—Y?Z, or X—Y—Z, X is nitrogen atom, NR4 (R4 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.

Abstract: The present invention provides a compound of formula (1) or a salt thereof wherein ring Q1 is optionally-substituted C6-10 aryl, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is C1-4 alkylene which may be optionally substituted with 1 to 3 fluorine atoms or C3-7 cycloalkyl; W2 is —NR4aC(O)—, etc. wherein R4a is hydrogen atom or C1-6 alkyl; ring Q2 is optionally-substituted C6-10 aryl, etc., which has an inhibitory effect on the sphere-forming ability of cancer cells and is useful an agent for removing iPS cells.

Abstract: The present disclosure provides a compound that exerts an anticancer action based on CHK1 inhibition. The present disclosure was completed by finding that a compound represented by formula (1) or a pharmaceutically acceptable salt thereof exhibits an excellent antitumor action by having a potent inhibitory action against CHK1: wherein R1, R2, L, V, W, and Q are as defined herein, X, Y, and Z each independently represent CR8 or a nitrogen atom, wherein X, Y, and Z are not simultaneously CR8, and R8 is as defined herein.

Abstract: A process for producing a hydrate of a hydrochloride salt of 2,2?-((((((2-acetylnaphtho[2,3-b]furan-4,9-diyl)bis(oxy))bis(carbonyl))bis(azanediyl))bis(ethane-2,1-diyl))bis(azanediyl))diacetic acid of the formula: wherein the process comprises the following step: recrystallizing the hydrochloride salt of 2,2?-((((((2-acetylnaphtho[2,3-b]furan-4,9-diyl)bis(oxy))bis(carbonyl))bis(azanediyl))bis(ethane-2,1-diyl))bis(azanediyl))diacetic acid, in the presence of hydrochloric acid and a recrystallization solvent; wherein the recrystallization solvent is methanol, ethanol, 2-propanol, diethyl ether, ethyl acetate, benzene, toluene, acetone, dichloromethane, chloroform, hexane, dimethylformamide, acetonitrile, or water; or mixed solvent thereof.

Abstract: Provided is a 2-heteroaryl aminoquinazolinone derivative, which is a compound represented by formula (1): or a pharmaceutically acceptable salt thereof wherein X1 represents CR1 or N, X2 represents CR2 or N, X3 represents CR3 or N, X4 represents CR4 or N, Y represents optionally substituted C1-6 alkyl, an optionally substituted C3-10 alicyclic group, an optionally substituted 4- to 10-membered nitrogen-containing non-aryl heterocycle, optionally substituted C6-10 aryl, or optionally substituted 5- to 10-membered heteroaryl, Z represents optionally substituted 6- to 10-membered heteroaryl, and R1, R2, R3, and R4 each independently represent a hydrogen atom, halogen, cyano, optionally substituted C1-6 alkyl, optionally substituted C1-6 alkoxy, or the like.

Abstract: A molecular marker for detecting a cancer stem cell in a cell mass which is a subject of interest, wherein the molecular marker can be detected in a cancer stem cell contained in the subject of interest but cannot be detected in a normal cell and a cancer cell that is different from a cancer stem cell; a method for determining the presence or absence of a cancer stem cell in a subject of interest by using the molecular marker as an measure; a kit for determining the presence or absence of a cancer stem cell, which comprises at least a reagent for detecting the molecular marker; a polypeptide encoded by the molecular marker; an antibody capable of recognizing an epitope of an expression product of a gene derived from the molecular marker; a nucleic acid capable of inhibiting the expression of the molecular marker; and a nucleic acid vaccine comprising a gene derived from the molecular marker.

Abstract: The RI-labeled anti-MUC5AC humanized antibody of the present invention is a conjugate of a chelating agent chelated with a radionuclide and an antibody (the radionuclide is a metal nuclide that emits ? particle or positron, and the antibody is a humanized antibody specifically binding to MUC5AC), and is superior in specificity for MUC5AC and accumulation in tumor. Therefore, it is extremely useful for the treatment and/or diagnosis of diseases in which MUC5AC is overexpressed, particularly cancer.

Abstract: The present invention provides a method for producing a retinal cell or a retinal tissue, including the following steps (1)-(3): (1) a first step of culturing pluripotent stem cells in the absence of feeder cells in a medium containing 1) a TGF? family signal transduction pathway inhibiting substance and/or a Sonic hedgehog signal transduction pathway activating substance, and 2) a factor for maintaining undifferentiated state, (2) a second step of culturing the cells obtained in the first step in suspension in a medium containing a Wnt signal transduction pathway inhibiting substance to form a cell aggregate, and (3) a third step of culturing the aggregate obtained in the second step in suspension in the presence or absence of a Wnt signal transduction pathway inhibiting substance in a medium containing a BMP signal transduction pathway activating substance to obtain an aggregate containing a retinal cell or a retinal tissue.

Abstract: The present invention provides an agent for determining Alzheimer's disease, comprising an anti-S38AA antibody, a method of determining Alzheimer's disease in a test animal, comprising detecting an S38AA fragment in a sample collected from said animal, and a method of screening for a substance that treats or prevents Alzheimer's disease, comprising contacting a test substance with a cell permitting measurement of production of a S38AA fragment, measuring the production amount of the S38AA fragment in the cell, and comparing the production amount with that of the S38AA fragment in a control cell free of contact with the test substance, and selecting a test substance that down-regulates the production amount of the S38AA fragment as a substance capable of treating or preventing Alzheimer's disease, based on the comparison results.

Abstract: A novel compound of the formula (1): wherein X is a tyrosine residue or a methionine residue; Y and Z each are a single bond or the like; R1 is a hydrogen atom or the like; R2 is a hydroxy group or the like; R3 is a hydrogen atom, alkyl group, amino group or the like; R4 is a hydrogen atom, alkyl group, carboxy group or the like; m is 1 or 2; and n is an integer of 0 to 2, with the proviso that when n is 0, R3 is a hydrogen atom or an alkyl group, or a pharmaceutically acceptable salt thereof, and its use in cancer immunotherapy.

Abstract: The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.

Abstract: Dosage regimens for at least one compound chosen from Iurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof are disclosed as are kits and methods for treatment and/or prevention of at least one CNS disorder such as, for example, mixed depression and bipolar disorder, and management of at least one CNS disorder, such as improving quality of life and reversing impairment in learning and memory associated with schizophrenia, comprising administering to a patient a therapeutically or prophylactically effective amount of at least one compound chosen from lurasidone and pharmaceutically acceptable salts, solvates, clathrates, and stereoisomers thereof.

Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.

Abstract: An oral disintegrating tablet containing (1) D-mannitol, (2) an active ingredient, (3) one or more disintegrating agents selected from the group consisting of crospovidone and carmellose, and (4) one or more lubricants selected from the group consisting of sodium stearyl fumarate and sucrose esters of fatty acids. The oral disintegrating tablet of the present invention has some excellent properties of (1) allowing easy production in a common facility without necessitating a specialized pharmaceutical technique, (2) having an appropriate strength that does not breakdown in the process of distribution, (3) having a fast disintegrating ability in the oral cavity, and (4) also having excellent ingestion feel such as greatly reduced bitterness or gritty feel; therefore, the tablet can be suitably used as a dosage form that is suitable for aged individuals, children, and seriously ill patients.

Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.

Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]-heptanedicarboxylmide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.

Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.