The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate, and the like.
C07D 253/07 - Triazines-1, 2, 4 comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des hétéro-atomes ou 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
2.
PHARMACEUTICAL COMPOSITION FOR HAILEY-HAILEY DISEASE AND USE THEREOF
A pharmaceutical composition for Hailey-Hailey disease contains 5-methyl-2-(1-piperazinyl)benzenesulfonic acid. The compound may be in a form of an anhydrate thereof, a salt thereof, a hydrate or solvate thereof, or a hydrate or solvate of a salt thereof, as an active ingredient. The hydrate is, for example, 5-methyl-2-(1-piperazinyl)benzenesulfonic acid monohydrate.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for protection against free radicals; pharmaceutical preparations for removing free radicals from the human bodies; pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS); neuroprotective medicines; pharmaceutical preparations and substances for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, ophthalmic, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders; antiallergic medicines; antihypertensives; hypoglycemic agents; antidiabetic preparations; pharmaceutical preparations for the prevention of diabetic nephropathy; pharmaceutical preparations, namely, antiphlogistic agents; vaccine; pharmaceutical preparations for the treatment of autoimmune disease; pharmaceutical preparations for the treatment of cerebral infarction; pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of erectile dysfunction
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for protection against free radicals; pharmaceutical preparations for removing free radicals from the human bodies; pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS); neuroprotective medicines; pharmaceutical preparations and substances for the treatment of viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, ophthalmic, respiratory, neurological, gastrointestinal, hormonal, dermatological , psychiatric and immune system related diseases and disorders; antiallergic medicines; antihypertensives; hypoglycemic agents; antidiabetic preparations; pharmaceutical preparations for the prevention of diabetic nephropathy; pharmaceutical preparations, namely, antiphlogistic agents; vaccine; pharmaceutical preparations for the treatment of autoimmune disease; pharmaceutical preparations for the treatment of cerebral infarction; pharmaceutical preparations for the treatment of multiple sclerosis; pharmaceutical preparations for the treatment of erectile dysfunction.
The present invention relates to a polymer which comprises constituent units (1), (2), and (3) represented by formulae (1A) to (3) (wherein each symbol is as defined in the present description), wherein the constituent units are bonded to each other. The present invention also relates to a catalyst for flow synthesis, which contains the polymer.
B01J 35/60 - Catalyseurs caractérisés par leur forme ou leurs propriétés physiques, en général caractérisés par leurs propriétés de surface ou leur porosité
C07D 211/62 - 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 en position 4
C08L 5/00 - Compositions contenant des polysaccharides ou leurs dérivés non prévus dans les groupes ou
C08L 25/18 - Homopolymères ou copolymères de monomères aromatiques contenant des éléments autres que le carbone et l'hydrogène
C08L 29/04 - Alcool polyvinyliqueHomopolymères ou copolymères d'esters partiellement hydrolysés d'alcools non saturés avec des acides carboxyliques saturés
A pharmaceutical composition for keratosis contains 5-methyl-2-(1-piperazinyl)benzenesulfonic acid. The compound may be in a form of an anhydrate thereof, a salt thereof, a hydrate or solvate thereof, or a hydrate or solvate of a salt thereof, and the hydrate is, for example, 5-methyl-2-(1-piperazinyl)benzenesulfonic acid monohydrate. The keratosis is, for example, Darier's disease or psoriasis.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
8.
TRIAZINE COMPOUND SALT, CRYSTAL FORM THEREOF, AND PRODUCTION METHOD THEREFOR
The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosilate, and the like.
C07D 253/07 - Triazines-1, 2, 4 comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des hétéro-atomes ou 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
05 - Produits pharmaceutiques, vétérinaires et hygièniques
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations; pharmaceutical preparations for
treatment of erythropoietic protoporphyria and X-linked
protoporphyria. Providing medical information of erythropoietic
protoporphyria and X-linked protoporphyria; providing
medical information, consultancy and advisory services.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations for treatment of erythropoietic protoporphyria and X-linked protoporphyria Providing medical information about erythropoietic protoporphyria and X-linked protoporphyria; providing medical information, consultancy and advisory services
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for protection against free radicals; pharmaceutical preparations for removing free radicals from the human bodies; pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS); neuroprotective medicines; pharmaceutical preparations and substances for the treatment of neurological diseases and disorders
A medicament for treatment or prevention of interstitial lung disease, and of a disease or symptom accompanied by systemic sclerosis in a subject includes, as an effective ingredient, 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-yl]carbonyl}-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid, or a pharmaceutically acceptable salt or co-crystal thereof.
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
This invention provides method of treating hypertension in a hypertensive subject, the method comprising administering to the subject a CYP 11β2 beta hydroxylase inhibitor once or twice per day in an amount sufficient to inhibit 50% or more of CYP 11β2 beta hydroxylase's activity for 40-60% of a 24-hour period to thereby treat hypertension in the hypertensive subject.
A61K 31/53 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec trois azote comme seuls hétéro-atomes d'un cycle, p. ex. chlorazanil, mélamine
05 - Produits pharmaceutiques, vétérinaires et hygièniques
40 - Traitement de matériaux; recyclage, purification de l'air et traitement de l'eau
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Pharmaceutical preparations; pharmaceuticals; medicines for
human purposes; targeted protein degrader. Custom manufacture of pharmaceuticals. Testing, inspection or research of pharmaceuticals;
consulting services in the field of testing, inspection or
research of pharmaceuticals; providing medical and
scientific testing, inspection or research information in
the field of pharmaceuticals; conducting clinical trials for
pharmaceuticals; research and development services in the
field of pharmaceutical preparations.
C07D 253/02 - Composés hétérocycliques contenant des cycles à six chaînons comportant trois atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe non condensés avec d'autres cycles
C07D 253/065 - Triazines-1, 2, 4 comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
C07D 401/02 - 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 contenant deux hétérocycles
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
05 - Produits pharmaceutiques, vétérinaires et hygièniques
40 - Traitement de matériaux; recyclage, purification de l'air et traitement de l'eau
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Pharmaceutical preparations, namely, targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; pharmaceuticals namely targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; medicines for human purposes namely, targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; target protein degrader namely, pharmaceutical preparations for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases Custom manufacture of pharmaceuticals namely targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases Testing, inspection or research of pharmaceuticals namely targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; consulting services in the field of testing, inspection or research of pharmaceuticals namely, targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; providing scientific information about medical testing of pharmaceuticals, and providing medical and scientific testing, inspection and research information in the field of pharmaceuticals namely, targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; Medical and scientific research, namely, conducting clinical trials for pharmaceuticals in the field of targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases; research and development services in the field of pharmaceutical preparations namely, targeted protein degrader for the treatment, prevention and alleviation of oncologic, immunologic, inflammatory diseases
The present invention provides a crystal of 1-{2-[(3S, 4R)-1-[(3R, 4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidine-3-carbonyl]-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) p henyl} piperidine-4-carboxylic acid having a certain quality that can be used as a drug substance. Specifically, the present invention provides a crystal comprising an equimolar amount of 1-{2-[(3S, 4R)-1-[(3R, 4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidine-3-carbonyl]-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl} piperidine-4-carboxylic acid and phosphoric acid.
C07D 401/14 - 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 contenant au moins trois hétérocycles
09 - Appareils et instruments scientifiques et électriques
38 - Services de télécommunications
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Downloadable software for detecting symptoms of ALS; Downloadable software for measuring progress of ALS; Downloadable medical software for tracking change of fine motor skills; Downloadable medical software for diagnosing ALS; Downloadable medical software for testing fine motor skills; Downloadable medical software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians; Software as a Medical Device (SaMD), downloadable, for detecting symptoms of ALS; Software as a Medical Device (SaMD), downloadable, for measuring progress of ALS; Software as a Medical Device (SaMD), downloadable, for tracking change of fine motor skills; Software as a Medical Device (SaMD), downloadable, for diagnosing ALS; Software as a Medical Device (SaMD), downloadable, for testing fine motor skills; Software as a Medical Device (SaMD), downloadable, for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians Rental of smartphones; Rental of smartphones featuring embedded software for detecting symptoms of ALS, sold as a unit; Rental of smartphones featuring embedded software for measuring progress of ALS, sold as a unit; Rental of smartphones featuring embedded software for tracking change of fine motor skills, sold as a unit; Rental of smartphones featuring embedded software for diagnosing ALS, sold as a unit; Rental of smartphones featuring embedded software for testing fine motor skills, sold as a unit; Rental of smartphones featuring embedded software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians, sold as a unit; Rental of mobile phones Software as a service (SaaS) services featuring non-downloadable software for detecting symptoms of ALS; Software as a service (SaaS) services featuring non-downloadable software for measuring progress of ALS; Software as a service (SaaS) services featuring non-downloadable medical software for tracking change of fine motor skills; Software as a service (SaaS) services featuring non-downloadable medical software for diagnosing ALS; Software as a service (SaaS) services featuring non-downloadable medical software for testing fine motor skills; Software as a service (SaaS) services featuring non-downloadable medical software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians; Providing on-line non-downloadable software for medical purposes for detecting symptoms of ALS; Providing on-line non-downloadable software for medical purposes for measuring progress of ALS; Providing on-line non-downloadable medical software for tracking change of fine motor skills; Providing on-line non-downloadable medical software for diagnosing ALS; Providing on-line non-downloadable medical software for testing fine motor skills; Providing on-line non-downloadable medical software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians; Rental of computer hardware and computer peripherals; Rental of tablet computers
09 - Appareils et instruments scientifiques et électriques
38 - Services de télécommunications
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Downloadable software for detecting symptoms of ALS; Downloadable software for measuring progress of ALS; Downloadable medical software for tracking change of fine motor skills; Downloadable medical software for diagnosing ALS; Downloadable medical software for testing fine motor skills; Downloadable medical software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians; Software as a Medical Device (SaMD), downloadable, for detecting symptoms of ALS; Software as a Medical Device (SaMD), downloadable, for measuring progress of ALS; Software as a Medical Device (SaMD), downloadable, for tracking change of fine motor skills; Software as a Medical Device (SaMD), downloadable, for diagnosing ALS; Software as a Medical Device (SaMD), downloadable, for testing fine motor skills; Software as a Medical Device (SaMD), downloadable, for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians Rental of smartphones; Rental of smartphones featuring embedded software for detecting symptoms of ALS, sold as a unit; Rental of smartphones featuring embedded software for measuring progress of ALS, sold as a unit; Rental of smartphones featuring embedded software for tracking change of fine motor skills, sold as a unit; Rental of smartphones featuring embedded software for diagnosing ALS, sold as a unit; Rental of smartphones featuring embedded software for testing fine motor skills, sold as a unit; Rental of smartphones featuring embedded software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians, sold as a unit; Rental of mobile phones Software as a service (SaaS) services featuring non-downloadable software for detecting symptoms of ALS; Software as a service (SaaS) services featuring non-downloadable software for measuring progress of ALS; Software as a service (SaaS) services featuring non-downloadable medical software for tracking change of fine motor skills; Software as a service (SaaS) services featuring non-downloadable medical software for diagnosing ALS; Software as a service (SaaS) services featuring non-downloadable medical software for testing fine motor skills; Software as a service (SaaS) services featuring non-downloadable medical software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians; Providing on-line non-downloadable software for medical purposes for detecting symptoms of ALS; Providing on-line non-downloadable software for medical purposes for measuring progress of ALS; Providing on-line non-downloadable medical software for tracking change of fine motor skills; Providing on-line non-downloadable medical software for diagnosing ALS; Providing on-line non-downloadable medical software for testing fine motor skills; Providing on-line non-downloadable medical software for collecting test data of fine motor skills of patients with ALS and providing the data to clinicians; Rental of computer hardware and computer peripherals; Rental of tablet computers
25.
Triazine compound salt, crystal form thereof, and production method therefor
The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate, and the like.
C07D 253/07 - Triazines-1, 2, 4 comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des hétéro-atomes ou 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 neuromuscular disease evaluation device that is less invasive, highly sensitive, quantitative and objective, and capable of easily evaluating neuromuscular diseases. A device for evaluating motor functions related to neuromuscular diseases, comprising: a memory unit storing a reference value for evaluating a predetermined movement, which is calculated based on a position of at least one body part; an analysis unit for identifying a position of a body part of the user by analyzing information based on an image captured of the predetermined movement, including the user's body; and an evaluation unit for evaluating the motor function based on the numerical value calculated based on the position of the body part of the user and the reference value.
The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R1, R2, R3, R4 and R5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.
C07C 233/81 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone d'un radical hydrocarboné substitué par des groupes carboxyle
A medicament for treatment or prevention of porphyria, comprising 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-yl]carbonyl}-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid or a pharmaceutically acceptable salt or cocrystal thereof as an active ingredient, wherein the dose of the 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-yl]carbonyl}-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid or the pharmaceutically acceptable salt or cocrystal thereof is 50 to 500 mg/day.
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
A61P 7/00 - Médicaments pour le traitement des troubles du sang ou du fluide extracellulaire
A pharmaceutical composition of 2-amino-2-[2-(4-heptyloxy-3-trifluoromethylphenyl)ethyl]propane-1,3-diol or a salt thereof is provided. The composition is superior in storage stability and can suppress production of related substances.
A pharmaceutical composition of 2-amino-2-[2-(4-heptyloxy-3-trifluoromethylphenyl)ethyl]propane-1,3-diol or a salt thereof is provided. The composition is superior in storage stability and can suppress production of related substances.
An excipient selected from dibasic calcium phosphate, calcium dihydrogen phosphate, dibasic sodium phosphate, and sodium dihydrogen phosphate is used.
5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.
C07C 233/81 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant l'atome d'azote d'au moins un des groupes carboxamide lié à un atome de carbone d'un radical hydrocarboné substitué par des groupes carboxyle
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Providing medical information about Erythropoietic Protoporphyria (EPP) and X-Linked Protoporphyria (XLP); providing medical information, consultancy and advisory services; medical assistance services; providing an internet web site for medical professionals and medical patients featuring information relating to Erythropoietic Protoporphyria (EPP) and X-Linked Protoporphyria (XLP); dietary and nutritional guidance; health care services, namely providing treatment for Erythropoietic Protoporphyria (EPP) and X-Linked Protoporphyria (XLP); health counselling
The present invention provides a crystal of 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid having a certain quality that can be used as a drug substance. Specifically, the present invention provides a crystal comprising an equimolar amount of 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylic acid and phosphoric acid.
C07D 401/14 - 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 contenant au moins trois hétérocycles
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for the treatment of central nervous system diseases, namely amyotrophic lateral sclerosis (ALS); Free radical scavenger for pharmaceutical purposes; Neuroprotective agents, namely pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS)
The present invention provides an industrially advantageous method for producing a 3,5-disubstituted triazine compound that is useful as an active pharmaceutical ingredient. More specifically, the present invention provides a production method, whereby it becomes possible to efficiently produce a 3-oxo-5-substituted triazine in water without the need to isolate an intermediate that may have mutagenicity, and it also becomes possible to perform the production without the need to isolate a product in each of multiple steps. Namely, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of reacting a compound represented by the following formula IV or a salt thereof with a base in water, and optionally including a step of forming a salt thereof. Specifically, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of derivatizing a compound represented by formula II or a salt thereof into a corresponding compound represented by formula III, a salt thereof, or a derivative thereof, then a step of reacting the resulting compound, a salt thereof, or a derivative thereof with aminourea or a salt thereof in water to produce a compound represented by formula IV or a salt thereof, and then a step of reacting the resulting compound or a salt thereof in the presence of a base.
(wherein ring A represents an optionally substituted aryl group or an optionally substituted heteroaryl group)
C07D 253/07 - Triazines-1, 2, 4 comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des hétéro-atomes ou 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
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin
metabolism disorders; pharmaceutical preparations for
treatment of porphyria; pharmaceutical preparations for
treatment of photodermatoses; pharmaceutical preparations
for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations; medicines for human purposes;
pharmaceutical preparations for the treatment of central
nervous system diseases; pharmaceutical preparations for the
treatment of amyotrophic lateral sclerosis (ALS); free
radical scavenger for pharmaceutical purposes;
pharmaceutical preparations for protection against free
radicals; neuroprotective agents; pharmaceutical
preparations for the treatment of acute ischaemic stroke.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin
metabolism disorders; pharmaceutical preparations for
treatment of porphyria; pharmaceutical preparations for
treatment of photodermatoses; pharmaceutical preparations
for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin
metabolism disorders; pharmaceutical preparations for
treatment of porphyria; pharmaceutical preparations for
treatment of photodermatoses; pharmaceutical preparations
for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin
metabolism disorders; pharmaceutical preparations for
treatment of porphyria; pharmaceutical preparations for
treatment of photodermatoses; pharmaceutical preparations
for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin
metabolism disorders; pharmaceutical preparations for
treatment of porphyria; pharmaceutical preparations for
treatment of photodermatoses; pharmaceutical preparations
for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin
metabolism disorders; pharmaceutical preparations for
treatment of porphyria; pharmaceutical preparations for
treatment of photodermatoses; pharmaceutical preparations
for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for treatment of porphyrin metabolism disorders; pharmaceutical preparations for treatment of porphyria; pharmaceutical preparations for treatment of photodermatoses; pharmaceutical preparations for treatment of scleroderma
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations; medicines for human purposes;
pharmaceutical preparations for the treatment of
neurological diseases and disorders; pharmaceutical
preparations for the treatment of psychiatric diseases and
disorders; pharmaceutical preparations for the treatment of
tardive dyskinesia; pharmaceutical preparations for the
treatment of Tourette syndrome; pharmaceutical preparations
for the treatment of dystonia; pharmaceutical preparations
for the treatment of movement disorders; pharmaceutical
preparations for the treatment of tics.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for the treatment of central nervous system diseases, namely amyotrophic lateral sclerosis (ALS); Free radical scavenger for pharmaceutical purposes; Neuroprotective agents, namely pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS)
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for the treatment of central nervous system diseases, namely amyotrophic lateral sclerosis (ALS); Free radical scavenger for pharmaceutical purposes; Neuroprotective agents, namely pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS)
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of central nervous system diseases; Pharmaceutical preparations for protection against free radicals; Pharmaceutical preparations for removing free radicals from the human bodies; Neuroprotective medicines; Pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS)
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for the treatment of central nervous system diseases, namely amyotrophic lateral sclerosis (ALS); Free radical scavenger for pharmaceutical purposes; Neuroprotective agents, namely pharmaceutical preparations for the treatment of amyotrophic lateral sclerosis (ALS)
Provided are a novel compound having a superior inhibitory action on KAT-II, a production method thereof, use thereof, and a pharmaceutical composition containing the aforementioned compound and the like.
A compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
wherein each symbol is as defined in the DESCRIPTION.
A61K 31/437 - 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 condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/553 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
A61K 31/4985 - Pyrazines ou pipérazines condensées en ortho ou en péri avec des systèmes hétérocycliques
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
A61P 25/18 - Antipsychotiques, c.-à-d. neuroleptiquesMédicaments pour le traitement de la manie ou de la schizophrénie
The present invention relates to a production method of 4-alkoxy-3-trifluoromethylbenzyl alcohol at a high conversion ratio, which can strictly suppress production of a byproduct by using DIBAL as a reducing agent.
C07C 41/26 - Préparation d'éthers par des réactions ne formant pas de liaisons sur l'oxygène de la fonction éther par introduction de groupes hydroxyle ou O-métal
C07C 213/02 - Préparation de composés contenant des groupes amino et hydroxy, amino et hydroxy éthérifiés ou amino et hydroxy estérifiés liés au même squelette carboné par des réactions impliquant la formation de groupes amino à partir de composés contenant des groupes hydroxy ou des groupes hydroxy éthérifiés ou estérifiés
C07C 43/23 - Éthers une liaison sur l'oxygène de la fonction éther étant sur un atome de carbone d'un cycle aromatique à six chaînons contenant des groupes hydroxyle ou O-métal
C07C 217/64 - Composés contenant des groupes amino et hydroxy éthérifiés liés au même squelette carboné ayant des groupes hydroxy éthérifiés liés à des atomes de carbone d'au moins un cycle aromatique à six chaînons et des groupes amino liés à des atomes de carbone acycliques ou à des atomes de carbone de cycles autres que des cycles aromatiques à six chaînons du même squelette carboné avec des groupes amino reliés au cycle aromatique à six chaînons ou au système cyclique condensé contenant ce cycle, par l'intermédiaire de chaînes carbonées qui sont substituées de plus par des atomes d'oxygène liés par des liaisons simples
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Medicines for human purpose; pharmaceutical preparations;
pharmaceutical preparations and substances for the treatment
of diabetes; pharmaceutical preparations and substances for
the treatment of disturbance of carbohydrate metabolism;
hypoglycemic agents.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Medicines for human purpose; pharmaceutical preparations;
pharmaceutical preparations and substances for the treatment
of diabetes; pharmaceutical preparations and substances for
the treatment of disturbance of carbohydrate metabolism;
hypoglycemic agents.