Abstract: A pharmaceutical formulation for applying as an external application to the surface of the human body, in which decrease of viscosity during long-term storage is suppressed, and which contains sofpironium bromide, a water-soluble polymer, and ethanol, has a pH of 5.2 or lower, and is a uniformly dispersed, and non-aqueous formulation or low water content formulation with a water content of 5% or lower.

Abstract: A heteroaromatic amide derivative or salt thereof showing high efficacy for diseases associated with Nav1.7 is represented by general formula (I) [wherein, X1-X2 is N—C or C—N, Y1, Y2, Y3 and Y4 are —CH2—, —CR4aH— or —O— and so on, Z1 is —O— and so on, ring A is a 3- to 7-membered monocyclic aromatic ring and so on, R1a and R1b are a hydrogen atom or a halogen atom and so on, R2 is a hydrogen atom and so on, R3a, R3b and R3c are a hydrogen atom or an optionally substituted C1-C6 haloalkyl group and so on, R4a, R4b and R4c are, an optionally substituted C1-C6 haloalkyl group or C1-C6 haloalkoxy group and so on, R5a is a hydrogen atom and so on, R5a and R5b together form —CH2O— and so on, R6a and R6b are a hydrogen atom and so on, n is 1 or 2.].

Abstract: A cocrystal containing the 1?R-diastereomer and the 1?S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1?R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.

Abstract: An airless container includes a cylindrical container body storing a contained material, which is a fluid, in an airtight state, and a pump attached to an upper edge portion of the container body and configured to externally discharge the contained material. The airless container further includes a bottom lid that closes a lower opening portion of a container bottom portion of the container body, and a piston in the container body between the pump and the bottom lid, which is slidable in the container body in an airtight state. The piston includes a flexible piece that is deformable in a portion that comes into contact with the bottom lid. The flexible piece is deformable against the sliding of the piston toward the bottom lid.

Abstract: A cocrystal containing the 1?R-diastereomer and the 1?S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1?R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.

Abstract: An airless container includes a cylindrical container body storing a contained material, which is a fluid, in an airtight state, and a pump attached to an upper edge portion of the container body and configured to externally discharge the contained material. The airless container further includes a bottom lid that closes a lower opening portion of a container bottom portion of the container body, and a piston in the container body between the pump and the bottom lid, which is slidable in the container body in an airtight state. The piston includes a flexible piece that is deformable in a portion that comes into contact with the bottom lid. The flexible piece is deformable against the sliding of the piston toward the bottom lid.

Abstract: The invention relates to a method of producing compound (I) by (A) reacting compound (II) formaldehyde and hydrogen in the presence of a metal catalyst, in a solvent, wherein the amount of the formaldehyde to be used is exceeding 1 mol and not exceeding 5 mol per 1 mol of compound (II), to obtain a mixture containing the formaldehyde and compound (I), and (B) mixing the obtained mixture containing the formaldehyde and compound (I) with hydrogen and a secondary amine selected from the group consisting of diethylamine, dipropylamine, diisopropylamine, butylethylamine, pyrrolidine, piperidine and morpholine, in the presence of a metal catalyst, in a solvent, and then removing the metal catalyst, followed by obtaining the compound (I) by distillation.

Abstract: The present invention provides a non-coating topical therapeutic agent for tinea unguium containing medium-chain triglyceride and the like as non-volatile components, which agent has high nail permeability and is superior in the aspects of efficacy and preparation properties, and can be applied clinically. Particularly, the present invention provides a topical therapeutic agent for tinea unguium containing an antifungal active substance such as efinaconazole or the like, a volatile component, an additive such as medium-chain triglyceride or the like, and a permeation enhancer such as ethyl lactate and the like. The preparation shows remarkably improved nail permeability has superior properties as a pharmaceutical product from the aspects of efficacy and preparation properties.

Abstract: The invention relates to a method of producing compound (I) by (A) reacting compound (II) formaldehyde and hydrogen in the presence of a metal catalyst, in a solvent, wherein the amount of the formaldehyde to be used is exceeding 1 mol and not exceeding 5 mol per 1 mol of compound (II), to obtain a mixture containing the formaldehyde and compound (I), and (B) mixing the obtained mixture containing the formaldehyde and compound (I) with hydrogen and a secondary amine selected from the group consisting of diethylamine, dipropylamine, diisopropylamine, butylethylamine, pyrrolidine, piperidine and morpholine, in the presence of a metal catalyst, in a solvent, and then removing the metal catalyst, followed by obtaining the compound (I) by distillation.

Abstract: A cocrystal containing the 1?R-diastereomer and the 1'S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1?R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.

Abstract: The present invention provides efinaconazole producing and purifying methods adapted to industrial scale that provide high-purity efinaconazole in high yield by simple operations using specific impurities as indices. The efinaconazole producing method comprises: step A of forming a toluene solution comprising compound (II), compound (III), an inorganic base, and toluene in a volume (L) which is 2 to 5 times the mass (kg) of compound (II); step B of subjecting the toluene solution to reaction under heating; step C of washing the reaction mixture from step B to obtain a toluene solution of crude efinaconazole in which the residual amount of 4-MP is not more than 5 wt % of efinaconazole.

Abstract: Provided is a compound showing excellent Antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C?O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.

Abstract: A syringe device includes an administration holder, and a cylinder portion which allows insertion of the administration holder. The cylinder portion includes a coupling holder, a slit holder coupled to the coupling holder, and a double-ended needle assembly disposed slidably in an interior of the coupling holder. A cartridge for a freeze-dry product is mounted, in the administration holder, and a cartridge for solvent is mounted in the coupling holder. When the administration holder is pushed, the double-ended needle assembly slides. When one of the needle points pricks the cartridge for freeze-dry product, the other needle point of the double-ended needle assembly pricks the cartridge for the solvent, and then the needle points unseal the cartridges by a further sliding movement of the double-ended needle assembly.

Abstract: A method for producing (R)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione, the method comprising, (a) a step for isolating an isomer represented by formula (2) from a mixture of isomers represented by formula (1), and (b) a step for obtaining (R)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione by removing the menthyloxycarbonyl group from the compound represented by formula (2), which was isolated in step (a).

Abstract: To provide a solution applicator with which irritation on an affected part of a patient may be reduced even when a solution is used. According to the present invention, an applicator comprises a solution container which comprises an opening, and a columnar brush member formed by bundling synthetic fibers in a columnar shape. The columnar brush member is disposed at the opening of the solution container, a tip portion of the columnar brush member at an outside of the solution container has a fan shape expanding in a perpendicular lateral direction against a pillar axial lengthwise direction, and a thickness of the fan-shaped tip portion of the columnar brush member decreases in a perpendicular lengthwise direction against the pillar axial lengthwise direction toward the tip portion of the columnar brush member.

Abstract: A method for producing (R)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione, the method comprising, (a) a step for isolating an isomer represented by formula (2) from a mixture of isomers represented by formula (1), and (b) a step for obtaining (R)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione by removing the menthyloxycarbonyl group from the compound represented by formula (2), which was isolated in step (a).

Abstract: Provided is a compound showing excellent Antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C?O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.

Abstract: To realize creation of a state in which two types of substances are communicated to each other via the double-ended needle assembly by a one-step continuous push operation and reduce a probability of entry of air or liquid leakage at that time. A syringe device 1 includes an administration holder 2, and a cylinder portion 6 which allows insertion of the administration holder 2. The cylinder portion 6 includes a coupling holder 3, a slit holder 4 coupled to the coupling holder 3, and a double-ended needle assembly 5 disposed slidably in an interior of the coupling holder 3. A cartridge for a freeze-dry product is mounted in the administration holder 2, and a cartridge for solvent is mounted in the coupling holder 3. When the administration holder 2 is pushed, the double-ended needle assembly 5 slides.

Abstract: General formula (I): The present invention pertains to: a pyridone derivate or a salt thereof represented by general formula (I); or a medicine containing the pyridone derivative or salt thereof as an active ingredient. [In the formula, ring A, R1, R2, R3 and R4 are specific groups.