Provided is a product exhibiting good bubbles even from a screen foamer composition using a non-ionic surfactant. This foam contains a non-ionic surfactant and is composed of an air layer and a bubble shell encapsulating the air layer. The bubble shell has a high light transmission region which is optically transparent and a low light transmission region which is less optically transparent than the highlight transmission region, both regions being disposed so as to spread across a surface of the bubble shell in such a manner as to form an identifiable boundary therebetween; and when the foam is allowed to stand at 25° C., an area of the low light transmission region occupying the surface area of the bubble shell expands over time, and thus the entire surface of the bubble shell becomes occupied by the low light transmission region.
To provide a novel medicine for suppressing cancer stem cells. An inhibitor of mitochondria in cancer stem cells which comprises a 2-nitroimidazole derivative as an active ingredient.
The present invention addresses the problem of providing a formulation having excellent pharmaceutical effects, in the context of pharmaceutical compositions for treatment of infections (e.g., vaginitis) which contains a compound represented by general formula (I) of claim 1. The present invention pertains to: a pharmaceutical composition containing a compound represented by general formula (I) of claim 1 and an excipient, and further containing one or more components selected from components A of claim 1; and a method for preparing a formulation containing the pharmaceutical composition.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 9/02 - SuppositoiresBougiesExcipients pour suppositoires ou bougies
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/36 - PolysaccharidesLeurs dérivés, p. ex. gommes, amidon, alginate, dextrine, acide hyaluronique, chitosane, inuline, agar-agar ou pectine
Provided is a product that is able to produce good foam even from a screen foamer composition using a nonionic surfactant. This foam contains a nonionic surfactant, comprises an air layer and a foam shell encapsulating said air layer, and is characterized in that: the foam shell has a high light transmission region which is optically transparent and a low light transmission region which is less optically transparent than the high light transmission region, both regions being disposed so as to extend across the surface of the foam shell in such a manner as to form an identifiable boundary therebetween; and when the foam is left still at 25°C or lower, the area occupied by the low light transmission region grows over time with respect to the surface area of the foam shell so as to cause the entire surface of the foam shell to end up being occupied by the low light transmission region.
The present invention addresses the issue of providing an external composition for screen foamers such as pump foamers, that can be safely used even when not removed after application. Provided is an external composition for screen foamers, including a non-ionic surfactant as a foaming component and, ideally, being in a soluble state.
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
The present invention addresses the problem of providing a technique for amorphizing a compound represented by general formula (1) and/or a salt thereof. Provided is an amorphizing agent for a compound represented by general formula (1) and/or a salt thereof, said amorphizing agent comprising one or more members selected from among water-soluble polymers and acids.
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61K 47/46 - Ingrédients de constitution indéterminée ou leurs produits de réaction, p. ex. peau, os, lait, fibre de coton, coquille d’œuf, fiel de bœuf ou extraits de plante
The present invention addresses the problem of providing a novel nuclear factor κB (NF-κB) inhibitor. An NF-κB inhibitor that comprises, as an active ingredient, a naphthoquinone compound represented by general formula (1) or a pharmaceutically acceptable salt thereof. [In general formula (1): R1 and R2 are the same or different and represent a hydrogen atom or a group selected from the group consisting of a hydroxy group, a 2-methyl-5-hydroxy-1,4-naphthoquinone group, an alkyl or alkenyl group optionally having a carbonyl group and an alkyl group optionally having a hydroxy group; R3 represents a hydroxy group or an alkyl group having 1-4 carbon atoms; R4 represents a hydroxy group or an oxo group; and the broken line represents a single bond or a double bond.)
A61K 31/122 - Cétones ayant l'atome d'oxygène lié directement à un cycle, p. ex. quinones, vitamine K1, anthraline
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes
C07C 49/747 - Composés non saturés comportant un groupe cétone faisant partie d'un cycle contenant des groupes hydroxyle contenant des cycles aromatiques à six chaînons
C07C 50/32 - Quinones contenant des groupes dont les atomes d'oxygène sont liés par liaison simple à des atomes de carbone la structure quinoïde faisant partie d'un système cyclique condensé à deux cycles
C07C 50/38 - Quinones contenant des groupes —CHO ou des groupes cétone non quinoïde
9.
LULICONAZOLE AS ANTI-ACANTHAMOEBA AGENT AND METHOD FOR PRODUCING THE SAME
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
The present invention aims to provide an agent for the treatment of giardiasis. Provided is an antigiardial agent that includes a compound represented by general formula (1) and/or a salt thereof. The antigiardial agent is preferably for the treatment of infection with giardia, which parasites inside intestines, and the compound represented by general formula (1) and/or the salt thereof are preferably grounded. The grounded compound and/or the salt thereof preferably have an average particle size of from 1 to 1000 μm. General Formula (1) (In the formula, R1 and R2 each independently represent a hydrogen atom or a halogen atom, provided that at least one of R1 and R2 is a halogen atom.)
The present invention addresses the issue of providing an external composition for screen foamers such as pump foamers, that can be safely used even when not removed after application. Provided is an external composition for screen foamers, including a non-ionic surfactant as a foaming component and, ideally, being in a soluble state.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 47/24 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant des atomes autres que des atomes de carbone, d'hydrogène, d'oxygène, d'halogènes, d'azote ou de soufre, p. ex. cyclométhicone ou phospholipides
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
An object is to provide a crystal having a new crystal habit of luliconazole and expand the possibility of application to pharmaceuticals. Disclosed is a crystal of luliconazole having such a crystal habit that (020) plane is a specific crystal growth surface.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
13.
External-use composition producing foamed state upon use
Compositions having an increased amount of an effective component retained in the composition for a pump foamer are provided. A composition for external use is described which contains: 1) an N-alkyl-2-pyrrolidone and/or a diester carbonate; and 2) a surfactant. The composition is in a foam state upon use.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 31/4015 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil ayant des groupes oxo liés directement à l'hétérocycle, p. ex. piracétam, éthosuximide
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 31/21 - Esters, p. ex. nitroglycérine, sélénocyanates
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/381 - Composés hétérocycliques ayant le soufre comme hétéro-atome d'un cycle ayant des cycles à cinq chaînons
A61K 31/439 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle le cycle formant une partie d'un système cyclique ponté, p. ex. quinuclidine
A61K 31/57 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
A61K 31/593 - Dérivés du 9,10-séco-cholestane, p. ex. cholécalciférol, vitamine D3
B65B 3/04 - Procédés ou moyens pour charger le matériau dans les réceptacles ou récipients
B65D 83/14 - Récipients pour distribuer des contenus liquides ou semi-liquides par pression interne de gaz, c.-à-d. réceptacles aérosols contenant un propulseur
14.
Crystalline form having specific crystal habit and pharmaceutical composition containing this crystalline form as active ingredient
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
15.
Resin container filled with antifungal pharmaceutical composition
Provided is a means for stably storing a pharmaceutical composition comprising a compound represented by the General Formula (I) below and/or a salt thereof, and for providing the pharmaceutical composition to the market. A resin container colored with a color having a hue (H) within the range of 7.0Y to 9.99Y or 7.0YR to 9.99YR, value (V) within the range of 1.0 to 6.0, and chroma (C) within the range of 0.5 to 7.5, according to Munsell color coordinates, is filled with a pharmaceutical composition comprising a compound represented by the General Formula (I) and/or a salt thereof, to store the pharmaceutical composition.
2 each independently represent a hydrogen atom or a halogen atom)
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
B65D 81/30 - Adaptations pour empêcher la détérioration ou l'altération du contenuApplications au réceptacle ou au matériau d'emballage d'agents de conservation des aliments, de fongicides, d'insecticides ou de produits repoussant les animaux en excluant la lumière ou toute autre radiation extérieure
A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61J 1/05 - Récipients spécialement adaptés à des fins médicales ou pharmaceutiques pour recueillir, stocker ou administrer du sang, du plasma ou des liquides à usage médical
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
16.
PHARMACEUTICAL COMPOSITION INCLUDING ANTI-FUNGAL AGENT AND STEROID
The present invention addresses the problem of providing, in order to treat dermatomycosis accompanying severe inflammations such as flare ups, an externally applied pharmaceutical composition which includes a combination of an anti-fungal agent and a steroidal agent, and in which the anti-fungal agent and the steroidal agent do not interfere with each other. This externally applied pharmaceutical composition for treating mycosis is characterized by including: a compound represented by general formula (1) shown below (in general formula (1), R represents hydrogen or a halogen, and X represents a halogen), and/or a salt thereof; and a steroid selected from prednisolone, dexamethasone, hydrocortisone, clobetasone, clobetasol, betamethasone, and mometasone.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
Provided is a technique for preparing a composition which after application forms a coating film having excellent properties although the recipe is the same. The technique is a process 1) for producing a composition of the oil-in-water emulsion preparation type which contains an optionally alkyl-modified carboxyvinyl polymer and/or a salt thereof and further contains a nonionic surfactant. The process is characterized by preparing an oil-in-water emulsion at a temperature higher than the cloud point of the nonionic surfactant, cooling the emulsion to or below the cloud point of the nonionic surfactant, then adding a carboxyvinyl polymer, and thereafter neutralizing the carboxyvinyl polymer with an alkali agent.
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
An object is to establish an index to prepare a stable pharmaceutical formulation by specifying a related substance of luliconazole which appears depending on the type of a selected solvent in the luliconazole pharmaceutical formulation and which is different from the SE form and the Z form. Disclosed is an amide derivative of luliconazole.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
19.
Crystal having crystal habits and pharmaceutical composition obtained by processing the crystal
An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal of luliconazole wherein the crystal has such a crystal habit that (021) plane is a specific crystal growth plane.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
20.
Use of surface free energy for differential evaluation of crystal, crystal evaluated on basis of surface free energy as index, and pharmaceutical composition prepared by containing the crystal
An object is to provide means for suppressing the formation of any isomer of luliconazole on account of any influence of, for example, the humidity and the light and improving the stability. Disclosed is a method for differential evaluating a crystal of luliconazole, comprising differential evaluating the crystal by using, as indexes, surface free energy of the crystal of luliconazole and a ratio of a polar component of the surface free energy, wherein the crystal is evaluated to be stable on condition that the surface free energy is smaller and the ratio of the polar component is lower.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
21.
Method of evaluating pharmaceutical preparation containing luliconazole and index substance
Disclosed is a method of evaluating stability of a pharmaceutical preparation containing luliconazole. The method includes measuring an amount of production of an SE form of luliconazole represented by following formula (2), an amount of production of a Z form of luliconazole represented by following formula (3) and an amount of production of an amide form of luliconazole represented by following formula (1) after storage under a severe condition or an accelerated condition, and judging that the stability of the pharmaceutical preparation is high if each of the amount of production of the SE form, the amount of production of the Z form and the amount of production of the amide form is not more than 5% by weight with respect to a compounded amount of luliconazole.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
The present invention aims to provide a pharmaceutical composition for pneumonia associated at least with a Fusarium fungus as a causative microorganism. Provided is a pharmaceutical composition for pneumonia associated at least with a Fusarium fungus as a causative microorganism, which pharmaceutical composition comprises as an effective component a compound represented by the General Formula (1) below: General Formula (1) (wherein R represents a halogen atom or hydrogen atom, and X represents a halogen atom).
Disclosed is a method of evaluating stability of a pharmaceutical preparation containing luliconazole. The method includes measuring an amount of production of an SE form of luliconazole represented by following formula (2), an amount of production of a Z form of luliconazole represented by following formula (3) and an amount of production of an amide form of luliconazole represented by following formula (1) after storage under a severe condition or an accelerated condition, and judging that the stability of the pharmaceutical preparation is high if each of the amount of production of the SE form, the amount of production of the Z form and the amount of production of the amide form is not more than 5% by weight with respect to a compounded amount of luliconazole.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
Disclosed is a pharmaceutical composition for antifungal use, comprising: 1) one or more compounds selected from compounds represented by the general formula (1) below and physiologically acceptable salts thereof; 2) one or more compounds selected from polypropylene glycol, diesters of dibasic acids, triacetin, 2-ethyl-1,3-hexanediol, lauromacrogol, and polyoxyethylene-polyoxypropylene glycol; and 3) one or more compounds selected from glucono-δ-lactone, propylene glycol, glycerin, and lactic acid. General formula (1) (In the formula, X represents a halogen or hydrogen).
wherein X represents a halogen or hydrogen.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
25.
CRYSTAL HAVING SPECIFIC CRYSTAL HABIT AND PHARMACEUTICAL COMPOSITION CONTAINING THE CRYSTAL AS ACTIVE INGREDIENT
An object is to provide a crystal having a new crystal habit of luliconazole and expand the possibility of application to pharmaceuticals. Disclosed is a crystal of luliconazole having such a crystal habit that (020) plane is a specific crystal growth surface.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
Provided is a means for heightening the retention of an active ingredient in a composition for a pump foamer. Provided is an external-use composition that contains 1) N-alkyl-2-pyrrolidone and/or a diester carbonate and 2) a surfactant, and that is characterized by having a foamed state upon use.
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/16 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'azote
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61P 3/02 - Nutriments, p. ex. vitamines, minéraux
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
Provided is a pharmaceutical composition in which an action of a compound represented by a general formula (1) is enhanced, and which is effective for pneumonia and vaginitis. Disclosed is a pharmaceutical composition for vaginitis or pneumonia, comprising a compound represented by the following general formula (1) and crotamiton: (in the formula, each of R1 and R2 independently represents hydrogen atom or halogen atom, and R1 and R2 are not simultaneously hydrogen atoms.)
Means for improving the solubility of luliconazole is provided. A crystal of luliconazole represented by the following formula is provided, wherein the crystal has such a crystal habit that (011) plane is a specific crystal growth plane. The crystal is characterized in that I(011) with respect to a sum total of I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) is not less than 25%, provided that integrated intensities of diffraction peaks, which correspond to the (001), (100), (10-1), (011), (110), (11-1), (10-2), (11-2), (020), (021), (20-2), (121), (013), (11-3), and (221) planes, are designated as I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) respectively in relation to the diffraction peaks detected in a range of 2θ= 5 to 35° in a powder X-ray diffractometry using CuKα radiation.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
Provided is a method for identifying and suppressing abnormal growth of fibroblasts at an early stage. Provided is a method for identifying the growth state of fibroblasts using as an index the level of expression of ETFB (electron transfer flavoprotein beta subunit), comprising: judging, in cases where the level of expression of ETFB is high, that there is a high probability that fibroblasts are abnormally growing; and judging, in cases where the level of expression of ETFB is low, that there is a high probability that fibroblasts are normally growing. Further, by inhibition of ETFB, abnormal growth of fibroblasts can be suppressed.
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
C12N 15/113 - Acides nucléiques non codants modulant l'expression des gènes, p. ex. oligonucléotides anti-sens
30.
PHARMACEUTICAL COMPOSITION FOR DISEASES CAUSED BY PATHOGENIC MICROORGANISMS SUCH AS ASPERGILLUS
An object is to provide means for precisely treating pneumonia caused by intracellular parasite, protozoa, and/or fungus. A pharmaceutical composition for pneumonia, comprising a compound represented by the following general formula (1) as an active ingredient:(In the formula, R represents a halogen atom or a hydrogen atom, and X represents a halogen atom.)
An object is to provide means for precisely treating vaginitis caused by intracellular parasite, protozoa, and/or fungus. A pharmaceutical composition for vaginitis, comprising a compound represented by the following general formula (1) as an active ingredient: (1) (In the formula, R represents a halogen atom or a hydrogen atom, and X represents a halogen atom.)
An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal of luliconazole wherein the crystal has such a crystal habit that (021) plane is a specific crystal growth plane.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/385 - Composés hétérocycliques ayant le soufre comme hétéro-atome d'un cycle ayant plusieurs atomes de soufre dans le même cycle
An object is to establish an index to prepare a stable pharmaceutical formulation by specifying a related substance of luliconazole which appears depending on the type of a selected solvent in the luliconazole pharmaceutical formulation and which is different from the SE form and the Z form. Disclosed is an amide derivative of luliconazole of formula (1).
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
USE OF SURFACE FREE ENERGY FOR DIFFERENTIAL EVALUATION OF CRYSTAL, CRYSTAL EVALUATED ON BASIS OF SURFACE FREE ENERGY AS INDEX, AND PHRMACEUTICAL COMPOSITION PREPARED BY CONTAINING THE CRYSTAL
An object is to provide means for suppressing the formation of any isomer of luliconazole on account of any influence of, for example, the humidity and the light and improving the stability. Disclosed is a method for differential evaluating a crystal of luliconazole, comprising differential evaluating the crystal by using, as indexes, surface free energy of the crystal of luliconazole and a ratio of a polar component of the surface free energy, wherein the crystal is evaluated to be stable on condition that the surface free energy is smaller and the ratio of the polar component is lower.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
Means for controlling the formation amount of a formed amide form in relation to a pharmaceutical composition containing luliconazole is provided. Disclosed is a pharmaceutical composition containing 1) luliconazole and 2) one component or two or more components selected from carboxylic acid and derivative thereof, ketone, phosphoric acid and derivative thereof, local anesthetic, antihistamine, and POE-based nonionic surfactant; wherein a content of an amide derivative of luliconazole is not more than 0.2% by mass with respect to a charged amount of luliconazole after storage at 60°C for 3 weeks or at 40°C for 6 months.
An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal consisting of luliconazole and short chain alcohol having a number of carbon atom or atoms of 1 to 4.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
37.
Crystal and pharmaceutical preparation containing the same crystal
An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal consisting of luliconazole and short chain alcohol having a number of carbon atom or atoms of 1 to 4.
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
C07D 401/00 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
Provided is a means for distinguishing the abnormal proliferation of a fibroblasts at an early stage and inhibiting the occurrence of the abnormal proliferation. Provided is a method for distinguishing the state of the proliferation of a fibroblast, which employs the degree of expression of an electron transfer flavonoprotein beta subunit (ETFB) as a measure, wherein it is determined that the abnormal proliferation of the fibroblast highly probably occurs when the degree of the expression of the ETFB is high, and it is determined that the proliferation of the fibroblast is highly probably kept in a normal state when the degree of the expression of the ETFB is low. The abnormal proliferation of a fibroblast can be prevented by inhibiting an ETFB.
C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes
C12Q 1/02 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des micro-organismes viables
In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof in an amount of 5% by mass or more, comprised is/are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and/or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60° C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
Disclosed is an antifungal agent for external use, which is characterized by containing a compound represented by the general formula (1) below, 50-95% by mass of an alcohol, and 0.1-35% by mass of water and/or an anionic surfactant.
2 represents a halogen atom. The present invention provides a preparation excellent in solubilization stability for a compound represented by the general formula (1) and/or a salt thereof in low-temperature or high-temperature storage.
A01N 43/10 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un ou plusieurs atomes d'oxygène ou de soufre comme uniques hétéro-atomes du cycle avec un hétéro-atome des cycles à cinq chaînons avec le soufre comme hétéro-atome du cycle
A01N 25/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, caractérisés par leurs formes, ingrédients inactifs ou modes d'applicationSubstances réduisant les effets nocifs des ingrédients actifs vis-à-vis d'organismes autres que les animaux nuisibles
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.
The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
A Cancer radiotherapeutic method using 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole (compound (i), and creatinine in an amount of 0.001 to part by mass with respect to 1 part by mass of compound (1); and irradiation.
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.
The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1):
and a compound having chelating ability.
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.
The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1):
and a compound having chelating ability.
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25° C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.
An object is to provide a medicament preparation which is excellent in the solubilization stability in relation to a compound represented by the general formula (1) during the storage in a low temperature region and a high temperature region. The present invention resides in a pharmaceutical composition comprising 1) the compound represented by the general formula (1) and/or a salt thereof and 2) a polyhydric alcohol derivative. General formula (1) (In the formula, R1, R2 independently represent hydrogen atom or halogen atom respectively, and at least one of R1, R2 is halogen atom.)
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/385 - Composés hétérocycliques ayant le soufre comme hétéro-atome d'un cycle ayant plusieurs atomes de soufre dans le même cycle
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
Provided is a technique whereby drug-penetrability (permeability) can be increased in the nail suffering from onychomycosis and thus therapeutic effect can be promoted. A laser irradiation device for treating onychomycosis, comprising: a laser light source; a laser transmission means that is provided with a laser irradiation site; a controlling unit for controlling the laser output; and a fixation device for fixing the laser irradiation site in a sealed state to the nail to be irradiated with laser, wherein the laser irradiation site is fixed in a sealed state, with the aforesaid fixation device, to the site of the nail to be irradiated, and then the nail is irradiated with laser to thereby form a crack through which a therapeutic for onychomycosis is penetrated into the nail.
A61B 18/20 - Instruments, dispositifs ou procédés chirurgicaux pour transférer des formes non mécaniques d'énergie vers le corps ou à partir de celui-ci par application de radiations électromagnétiques, p. ex. de micro-ondes en utilisant des lasers
A61K 41/00 - Préparations médicinales obtenues par traitement de substances par énergie ondulatoire ou par rayonnement corpusculaire
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
A61M 37/00 - Autres appareils pour introduire des agents dans le corpsPercutanisation, c.-à-d. introduction de médicaments dans le corps par diffusion à travers la peau
A pharmaceutical composition which comprises 1) a compound represented by the following general formula (1) and/or a salt thereof; and 2) a ketone such as methyl ethyl ketone. Preferably, the compound represented by the following general formula (1) is luliconazole, where R1=R2=a chlorine atom: where R1 and R2 each independently represents a hydrogen atom or a halogen atom, and at least one of R1 and R2 represents a halogen atom. The present invention provides a preparation excellent in solubilization stability for a compound represented by the general formula (1) and/or a salt thereof in low-temperature or high-temperature storage.
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
The invention can produce an infected nail of an animal and an infected animal model in which the nail plate and nail bed of the nail are sufficiently infected with a superficial fungus which were difficult to be produced in the past, and provides an evaluation method useful for development of a therapeutic agent for intractable infectious diseases such as tinea unguium using the nail and the infected animal model. For producing the infected nail of an animal and the infected animal model infected with a superficial fungus, an immunosuppressive component is administered to an animal in advance to decrease immunocompetence, and then, a superficial fungus is inoculated into the animal, whereby the infected nail of an animal and the infected animal model reflecting clinical manifestation in which the nail plate and nail bed of the nail are sufficiently infected with the superficial fungus can be produced with good reproducibility in a short period of time.
A61K 48/00 - Préparations médicinales contenant du matériel génétique qui est introduit dans des cellules du corps vivant pour traiter des maladies génétiquesThérapie génique
A01K 67/00 - Élevage ou obtention d'animaux, non prévus ailleursNouvelles races ou races modifiées d'animaux
C12Q 1/02 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des micro-organismes viables
C12Q 1/18 - Test de l'activité antimicrobienne d'un matériau
In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof in an amount of 5% by mass or more, comprised is/are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and/or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60°C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20°C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5°C. for 2 weeks after manufacture.
In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25°C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a steroisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20°C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5°C. for 2 weeks after manufacture.
Disclosed is an antifungal agent for external use, which is characterized by containing a compound represented by the general formula (1), 50 to 95 mass % of an alcohol such as ethanol, 0.1 to 35 mass % of water or the like, and 0.01 to 5 mass % of a cellulose thickening agent. X is a halogen or H.
To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.
The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.
The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1):
and a compound having chelating ability.
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
It is an object to provide a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain, which is suitable for production of a derivative having a radioisotope.
A method for producing 1-(1-benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, characterized by reacting glycerin with a benzoylating agent to obtain 1-O-benzoylglycerin, reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent to obtain 4-benzoyloxymethyl-1,3-dioxolane, and then reacting this product with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.
A61K 31/4168 - 1,3-Diazoles ayant un atome d'azote lié en position 2, p. ex. clonidine
C07D 233/28 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement aux atomes de carbone du cycle
Disclosed is an evaluation method which enables the production of an animal infection model for a microbial infection in a tissue that is insusceptible to the infection (e.g., a nail) (the production has been difficult to achieve hitherto), and which is useful for the development of a therapeutic agent for intractable infections including nail psoriasis by using the animal infection model. For producing an animal infection model for a tissue which is insusceptible to the infection with an infection-induced microorganism, an animal is administered with an immunosuppressing ingredient in advance to reduce the immune response thereof, and subsequently inoculated and sensitized with the infection-inducing microorganism. In this manner, it becomes possible to produce an animal model infected with an infection-inducing microorganism, which has high reproducibility and which can highly reflect a clinical disease condition, within a short period.
The invention can produce an infected nail of an animal and an infected animal model in which the nail plate and nail bed of the nail are sufficiently infected with a superficial fungus which were difficult to be produced in the past, and provides an evaluation method useful for development of a therapeutic agent for intractable infectious diseases such as tinea unguium using the nail and the infected animal model. For producing the infected nail of an animal and the infected animal model infected with a superficial fungus, an immunosuppressive component is administered to an animal in advance to decrease immunocompetence, and then, a superficial fungus is inoculated into the animal, whereby the infected nail of an animal and the infected animal model reflecting clinical manifestation in which the nail plate and nail bed of the nail are sufficiently infected with the superficial fungus can be produced with good reproducibility in a short period of time.
A pharmaceutical composition for external use, including: i) luliconazole represented by the following structural formula (1) and/or a salt thereof; and ii) one or two or more selected from N-methyl-2-pyrrolidone, propylene carbonate, and crotamiton.
Provided is a pharmaceutical composition for external use which includes the following components: 1) luliconazole and/or a salt thereof; 2) N-methyl-2-pyrollidone; and 3) benzyl alcohol and/or diester of a dibasic acid. The diester of the dibasic acid is a diethyl ester or a diisopropyl ester of a dibasic acid having 6-10 carbon atoms. The pharmaceutical composition is useful for the treatment of a mycotic disease such as foot trichophytosis, trichophytosis corporis, trichophytosis on a hard keratin or hyperkeratotic portion, onychomycosis, particularly on a nail, or dermatomycosis.
Disclosed is an antifungal agent for external application, which is characterized by containing a compound represented by the general formula (1) below, 50-95% by mass of an alcohol, and 0.1-35% by mass of water and/or an anionic surfactant. X is a halogen or H. General formula (1)
Disclosed is an antifungal pharmaceutical composition, which is characterized by containing (1) one or more members selected from compounds represented by the general formula (1) below and physiologically acceptable salts thereof, (2) one or more members selected from polypropylene glycols, diesters of dibasic acids, triacetin, 2-ethyl-1,3-hexanediol, lauromacrogol and polyoxyethylene-polyoxypropylene glycols, and (3) one or more members selected from glycono-&dgr;-lactone, propylene glycol, glycerin and lactic acid. General formula (1) (In the formula, X represents a halogen or hydrogen).
A61K 31/4178 - 1,3-Diazoles non condensés et contenant d'autres hétérocycles, p. ex. pilocarpine, nitrofurantoïne
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
Disclosed is an antifungal agent for external application, which is characterized by containing a compound represented by the general formula (1) below, 50-95% by mass of an alcohol such as ethanol, 0.1-35% by mass of water or the like, and 0.01-5% by mass of a cellulose thickening agent. X is a halogen or H.
Provided is a pharmaceutical composition for external use, including: (i) luliconazole represented by the following structural formula (1) and/or a salt thereof; and (ii) α-hydroxycarboxylic acid and/or a salt thereof.
Disclosed is a pharmaceutical composition containing a highly stable 2-nitroimidazole derivative which exhibits high solubility in an aqueous carrier. Specifically disclosed is a pharmaceutical composition characterized by containing 1-(1-hydroxymethyl-2,3- dihydroxypropyl)oxymethyl-2-nitroimidazole and 0.001-1 part by mass of creatinine per 1 part by mass of the compound.
Disclosed is a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain which is suitable for production of a derivative having a radioisotope. Specifically disclosed is a method for producing 1-(1- benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, which is characterized in that 1-O-benzoylglycerin is obtained by reacting glycerin with a benzoylating agent, then 4-benzoyloxymethyl-1,3-dioxolane is obtained by reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent, and then 4-benzoyloxymethyl-1,3-dioxolane is reacted with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.
Disclosed is a pharmaceutical composition which is improved in storage stability without deteriorating effects of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2- nitroimidazole. Specifically disclosed is a pharmaceutical composition containing 1-(1-hydroxymethyl-2,3- dihydroxypropyloxymethyl)-2-nitroimidazole represented by the general formula (1) below and a compound having a chelating ability. (1)
An external pharmaceutical composition characterized by containing 1) luliconazole of the following structural formula (1) and/or its salt and 2) an .alpha.-hydroxycarboxylic acid and/or its salt. Structural formula (1):
An external pharmaceutical composition characterized by containing 1) luliconazole of the following structural formula (I) and/or its salt and 2) one or two or more members selected from among N-methyl-2-pyrrolidone, propylene carbonate and crotamiton. Structural formula (I):
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
Provided is a pharmaceutical composition for external use, including: (i) a compound represented by the general structural formula (1) and/or a salt thereof; and (ii) N-methyl-2-pyrolidone: (see general formula 1) Where, X represents a hydrogen atom or a chlorine atom.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
An external pharmaceutical composition characterized by containing 1) luliconazole of the following structural formula (I) and/or its salt and 2) one or two or more members selected from among N-methyl-2-pyrrolidone, propylene carbonate and crotamiton. Structural formula (I):
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
An external pharmaceutical composition characterized by containing 1) any of compounds of the following general formula (1) and/or its salt and 2) N-methyl-2-pyrrolidone. General formula (1): wherein X is a hydrogen atom or chlorine atom.
C07D 409/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
An external pharmaceutical composition characterized by containing 1) luliconazole of the following structural formula (1) and/or its salt and 2) an &agr;-hydroxycarboxylic acid and/or its salt. Structural formula (1):
An object of the present invention is to provide a medicinal composition useful for external application in the treatment of a fungal infection reaching the lower part of a thick keratin layer. Provided is an antifungal medicinal composition, comprising: (1) a film-forming agent; (2) a water-soluble plasticizer in a form of a solid or a paste at 20° C. at 1 atm; and (3) an antifungal compound represented by a general formula (1) and/or a physiologically acceptable salt thereof.
