Abstract: The present disclosure is directed to a method of treating overactive bladder comprising orally administering to a subject in need thereof an amount of from about 50 mg to about 100 mg (e.g., about 75 mg) of vibegron per day. The present disclosure also provides a method of treating overactive bladder comprising orally administering to a subject in need thereof a first dosage of vibegron per day for a first period and a second dosage of vibegron per day thereafter.

Abstract: [Problem] The present disclosure provides tertiary amide derivatives substituted with a 4-membered ring structure that are useful as medicines and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and therapeutic agents and/or prophylactic agents for conditions in which CBP/P300 is involved, comprising the composition.

Abstract: A compound of formula (2) or pharmaceutically acceptable salt thereof. wherein R1 is a hydrogen atom or the like; R2 is a methoxy group or the like; R3 is a hydrogen atom or the like; R4 is an optionally substituted C1-6 alkyl group or the like; m is 0, 1, or 2; n is 0, 1, 2, or 3; L1 is —NH—C(?O)—, —C(?O)—NH—, or the like; L2 is a single bond or the like; X is optionally substituted phenyl or the like; Y is optionally substituted phenyl or the like; and X and Y are bonded at a carbon atom on each ring.

Abstract: The present invention relates to the compound of formula (1a) wherein a-d and p are 1 or 2, R1-R4 are hydrogen atom or the like, and R18 is —CF3 or the like, or a pharmaceutically acceptable salt thereof, which has an anticancer effect by inhibiting the binding between a MLL fusion protein that is fused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.

Abstract: This disclosure relates to crystalline solvated forms of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N?-methoxyurea. It also relates to methods of making the disclosed crystalline forms, pharmaceutical compositions and kits comprising the forms, and methods of treatment and uses comprising their administration.

Abstract: The present invention relates to a transdermal absorption preparation that can maintain a blood concentration sufficient to exert the efficacy of tandospirone, and also shows good storage stability against heat, humidity, and light. According to the present invention, a transdermal absorption preparation containing tandospirone or a pharmaceutically acceptable salt thereof, and levulinic acid, which is superior in the skin permeability of tandospirone or a pharmaceutically acceptable salt thereof in the preparation, and shows good preservation stability against heat and light can be provided.

Abstract: Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N?-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a compound of formula (1) wherein Q1 is halogen atom, Q2 is hydrogen atom, etc., X, Y, and Z are nitrogen atom or oxygen atom, and R1 has a given structure, or a pharmaceutically acceptable salt thereof, and a medicament comprising the compound for treating and/or preventing a disease such as epilepsy.

Abstract: Provided is a self-degradation type CDK9 inhibitor prodrug and a liposome encapsulating the same. The present disclosure provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 is an optionally substituted C1-6 alkyl group, R2 and R3 are the same or different, each independently a hydrogen atom or an optionally substituted C1-6 alkyl group, X is CH2 or an oxygen atom, n is 1 or 2, p is 0, 1 or 2, q is 1 or 2, and r is 0, 1 or 2, wherein, if X is an oxygen atom, q is 2.

Abstract: A compound represented by formula (2) or pharmaceutically acceptable salt thereof: wherein R1 represents a hydrogen atom or the like; R2 represents a methoxy group or the like; R3 represents a hydrogen atom or the like; R4 represents an optionally substituted C1-6 alkyl group or the like; m represents 0, 1, or 2; n represents 0, 1, 2, or 3; L1 represents —NH—C(?O)—, —C(?O)—NH—, or the like; L2 represents a single bond or the like; X represents optionally substituted phenyl or the like; Y represents optionally substituted phenyl or the like; and X and Y are bonded at a carbon atom on each ring.

Abstract: A compound represented by formula (1): wherein Z is a nitrogen atom and the like; Y is carbonyl and the like; m and n are 1 and the like; R1a through R1d, R2a through R2d, and R4a through R4d are a hydrogen atom and the like; R3 is alkyl and the like; and Q is a specific bicyclic group; or a pharmaceutically acceptable salt thereof; the compound having antagonist activity against serotonin 5-HT2A receptors and serotonin 5-HT7 receptors.

Abstract: The present invention relates to the compound of formula (1a) wherein p is 1 or 2, R1-R4 are hydrogen atom or the like, Ring A is cycloalkylene or the like, L is single bond or the like, and R is methyl or the like, or a pharmaceutically acceptable salt thereof, which has an anticancer effect by inhibiting the binding between a MLL fusion protein that is fused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.

Abstract: The present disclosure includes combination solid oral dosage forms having 40 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N?-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof, and hormone replacement medicaments. Also provided are processes for making and using the solid oral dosage forms.

Abstract: The present invention relates to a medicament for treating or preventing central nervous system disease whose cause is related to abnormal aggregation of proteins in the brain, which comprises as an active ingredient a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are hydrogen, etc., R3 and R4 are hydrogen, C1-6 alkyl, etc., X is oxygen, etc., Y is carbon, etc., Z is C1-6 alkyl, etc., m and n are an integer of 0, 1, 2, etc., which has an action of suppressing or reducing the accumulation of abnormal aggregation of proteins in the brain.

Abstract: The present disclosure provides bicyclic pyridine derivatives. A compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein X is a oxygen atom, sulfur atom, NR, or CR?R?, n is 0 or 1, R1, R2a, R2b, R2c, R2d, R, R? and R? are each independently a hydrogen atom, a halogen atom, optionally substituted C1-6 alkyl, or an optionally substituted C6-10 aryl, or two of R2a, R2b, R2c, R2d, R, R?, and R?, together with a carbon atom or a nitrogen atom to which they are attached, form a 3- to 6-membered saturated carbocyclic ring or saturated heterocyclic ring, and R3a, R3b, R3c and R5a and R5b, are as defined in the description.

Abstract: The present invention relates to suitable usage, dosage, and use of an optically active azabicyclo ring derivative useful as a medicament, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it.

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 present disclosure provides bicyclic pyridine derivatives. A compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein X is a oxygen atom, sulfur atom, NR, or CR?R?, n is 0 or 1, R1, R2a, R2b, R2c, R2d, R, R? and R? are each independently a hydrogen atom, a halogen atom, optionally substituted C1-6 alkyl, or an optionally substituted C6-10 aryl, or two of R2a, R2b, R2c, R2d, R, R?, and R?, together with a carbon atom or a nitrogen atom to which they are attached, form a 3- to 6-membered saturated carbocyclic ring or saturated heterocyclic ring, and R3a, R3b, R3c and R5a and R5b, are as defined in the description.

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.