Goods & Services

Pharmaceutical preparations; medicines for alleviating constipation; laxative suppositories; purgatives; laxatives; enema preparations; therapeutic drugs and agents; traditional Chinese medicines; medicines made of Chinese traditional medicinal herbs.

Goods & Services

Pharmaceutical preparations; medicines for alleviating constipation; laxative suppositories; purgatives; laxatives; enema preparations; therapeutic drugs and agents; traditional Chinese medicines; medicines made of Chinese traditional medicinal herbs.

Abstract

The present invention provides a novel compound that has an α-amino-β-carboxymuconate 6-semialdehyde decarboxylase (ACMSD) inhibitory activity.　Provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 487/04 - Ortho-condensed systems

Abstract

[Problem] To provide a simpler testing method for a NAFLD or an assisting method for the diagnosis of a NAFLD, which is excellent in sensitivity and specificity. [Solution] Provided is a testing method for a nonalcoholic fatty liver disease (NAFLD), the method including a step for detecting or quantifying L-methionine in a biological sample derived from a subject.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids

Abstract

[Problem] To provide a simpler testing method for a NAFLD or an assisting method for the diagnosis of a NAFLD, which is excellent in sensitivity and specificity. [Solution] Provided is a testing method for a nonalcoholic fatty liver disease (NAFLD), the method including a step for detecting or quantifying D-histidine in a biological sample derived from a subject.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids

Abstract

Provided is a pharmaceutical composition containing a sulfonamide derivative represented by formula (1), a pharmaceutically acceptable salt thereof, or an active metabolite thereof, and having improved absorption during oral administration. Disclosed is a self-emulsifying composition comprising a sulfonamide derivative represented by formula (1), a pharmaceutically acceptable salt thereof, or an active metabolite thereof, and at least two solubilizing agents.

IPC Classes  ?

• A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

To provide a pharmaceutical composition having a dosage of a compound represented by formula (I) or a pharmaceutically acceptable salt thereof that is effective in the treatment of inflammatory bowel disease. Disclosed is a pharmaceutical composition for treating inflammatory bowel disease, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein the compound or a pharmaceutically acceptable salt thereof is administered to a human in an amount of 50 mg or more as an active ingredient per day. (R represents a hydroxy group or an isobutyloxy group.)

IPC Classes  ?

• A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 9/107 - Emulsions
• A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

The present invention provides a novel compound that has an α-amino-β-carboxymuconate 6-semialdehyde decarboxylase (ACMSD) inhibitory activity.　The present invention provides a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Provided is a technique for improving the productivity in a method for producing a compound I or a pharmaceutically acceptable salt thereof. This method for producing the compound I comprises: a step for preparing a compound 16 solution by deprotecting a compound 10-R3 in a solvent; and a step for adding a compound 15 to the compound 16 solution without isolating the compound 16 and synthesizing the compound I in the presence of a condensing agent.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond

Goods & Services

Dietary supplements for human consumption; Pharmaceutical preparations for the treatment of autoimmune, cardiovascular, central nervous system, endocrine, gastrointestinal, genetic, immunological, infectious, inflammatory, menopausal, metabolic, musculoskeletal, neurodegenerative, neurological, neuromuscular, ophthalmological, psychiatric, respiratory, urogenital, oncological, urological, dermatological, hematological, and viral diseases and disorders; Pharmaceutical preparations for the treatment of liver diseases and disorders, erectile dysfunction, sexual dysfunction, cancer, pain, and diabetes; Reagent paper for medical purposes Pharmaceutical research and development, namely, pharmaceutical testing, inspection and research; Testing of pharmaceuticals Medical information; Providing health care information via a global computer network

Goods & Services

Pharmaceutical preparations for the treatment of autoimmune, cardiovascular, central nervous system, endocrine, gastrointestinal, genetic, immunological, inflammatory, namely except inflammatory bronchial disease, metabolic, neurodegenerative, neurological, psychiatric, oncological, and viral diseases and disorders; Pharmaceutical preparations for the treatment of liver diseases and disorders, erectile dysfunction, sexual dysfunction, cancer, pain, and diabetes; Reagent paper for medical purposes Pharmaceutical research and development, namely, pharmaceutical testing, inspection and research Medical information; Providing health care information via a global computer network

Abstract

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.

IPC Classes  ?

• A61K 31/4402 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
• A23L 27/20 - Synthetic spices, flavouring agents or condiments
• A61K 31/185 - Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
• A61K 31/417 - Imidazole-alkylamines, e.g. histamine, phentolamine
• A61K 31/4245 - Oxadiazoles
• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
• C07C 309/51 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
• C07C 311/32 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
• C07C 311/51 - Y being a hydrogen or a carbon atom
• C07C 333/08 - Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
• C07C 335/16 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
• C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• C07D 271/10 - 1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07D 295/192 - Radicals derived from carboxylic acids from aromatic carboxylic acids
• C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

An object of the present invention is to provide a therapeutic agent for fatty liver diseases. The above object can be achieved by a therapeutic agent for a fatty liver disease, comprising a compound represented by the following formula (1): or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

33 in a solvent; and a step for adding a compound 15 to the compound 16 solution without isolating the compound 16 and synthesizing the compound I in the presence of a condensing agent.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 213/40 - Acylated substituent nitrogen atom
• A61K 31/63 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide

Abstract

Provided is a technique for improving the productivity in a method for producing a compound I or a pharmaceutically acceptable salt thereof. This method for producing the compound I has: a step for preparing a compound 16 solution by deprotecting a compound 10-R3 in a solvent; and a step for adding a compound 15 to the compound 16 solution without isolating the compound 16 and synthesizing the compound I in the presence of a condensing agent.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/63 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide
• C07D 213/40 - Acylated substituent nitrogen atom

Abstract

The present disclosure provides a method that is suitable for the industrial production of a compound (1) and that enables production of same at a high purity and a high yield.　The present disclosure pertains to a method for producing the compound (1) through the following route.

IPC Classes  ?

• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 239/557 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid

Goods & Services

Pharmaceutical preparations; reagent paper for medical purposes; dietary supplements for humans; dietetic beverages adapted for medical purposes; dietetic foods adapted for medical purposes. Testing, inspection and research services in the fields of pharmaceuticals, cosmetics and foodstuffs. Provision of medical information; provision of medical information relating to medical products; information services relating to medical products; medical examination services; providing health care information.

Goods & Services

Pharmaceuticals; laxatives; oiled paper for medical purposes; drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; medicated compresses; capsules for medicines; eyepatches for medical purposes; ear bandages; menstruation bandages; sanitary tampons; sanitary napkins; sanitary panties; absorbent cotton; adhesive plasters for medical purposes; bandages for dressings; breast-nursing pads; cotton swabs for medical purposes; materials for repairing teeth and dental prostheses; lacteal flour for babies; dietary supplements for humans; dietetic beverages adapted for medical purposes; dietetic foods adapted for medical purposes; beverages for babies; food for babies.

Abstract

Provided is a medicinal composition having excellent stability, the medicinal composition comprising 3-{[(2S)-2-amino-2-carboxyethyl]carbamoylamino}-5-chloro-4-methylbenzenesulfonic acid, a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein the medicinal composition has a pH of 8.0 or less.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)

Abstract

The present invention addresses the problem of providing a therapeutic agent for a fatty liver disease. The problem can be solved by a therapeutic agent which is for a fatty liver disease and contains a compound represented by formula (1) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The present invention addresses the problem of providing a therapeutic agent for a fatty liver disease. The problem can be solved by a therapeutic agent which is for a fatty liver disease and contains a compound represented by formula (1) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The present invention provides a method for determining the likelihood of colorectal cancer development in a human ulcerative colitis patient, the method including: a measurement step of measuring methylation rates of one or more CpG sites present in specific differentially methylated regions in DNA recovered from a biological sample collected from the human ulcerative colitis patient; and a determination step of determining the likelihood of colorectal cancer development in the human ulcerative colitis patient based on average methylation rates of the differentially methylated regions which are calculated based on the methylation rates measured in the measurement step and a preset reference value or a preset multivariate discrimination expression, in which the reference value is a value for identifying a cancerous ulcerative colitis patient and a non-cancerous ulcerative colitis patient, which is set for the methylation rate of each differentially methylated region, and the multivariate discrimination expression includes, as variables, average methylation rates of one or more differentially methylated regions among the specific differentially methylated regions.

IPC Classes  ?

• A61B 10/04 - Endoscopic instruments
• A61B 10/06 - Biopsy forceps
• A61B 17/02 - Surgical instruments, devices or methods, e.g. tourniquets for holding wounds open; Tractors

Goods & Services

Pharmaceuticals; reagent paper for medical purposes; oiled paper for medical purposes; adhesive tapes for medical purposes; drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; gauze for dressings; empty capsules for pharmaceuticals; eyepatches for medical purposes; ear bandages; menstruation bandages; menstruation tampons; sanitary napkins; sanitary panties; absorbent cotton; adhesive plasters; bandages for dressings; liquid bandages; breast-nursing pads; cotton swabs for medical use; dental materials; diapers; nappy covers; fly catching paper; mothproofing paper; lacteal flour for babies; dietary supplements for humans; dietetic beverages adapted for medical purposes; dietetic foods adapted for medical purposes; beverages for babies; food for babies; dietary supplements for animals; semen for artificial insemination. Medical apparatus and instruments; medical devices; pacifiers for babies; ice bag pillows for medical purposes; triangular bandages; support bandages; surgical catgut; feeding cups for medical purposes; dropping pipettes for medical purposes; teats; medical ice bags; medical ice bag holders; baby bottles; nursing bottles; contraceptives, non-chemical; artificial tympanic membranes; prosthetics or fillings materials, not for dental use; sanitary masks for personal use.

Goods & Services

Pharmaceutical preparations; reagent paper for medical purposes; dietary supplements for humans; dietetic beverages adapted for medical purposes; dietetic foods adapted for medical purposes. Testing, inspection and research services in the fields of pharmaceuticals, cosmetics and foodstuffs. Provision of medical information; provision of medical information relating to medical products; information services relating to medical products; medical examination services; providing health care information.

Goods & Services

Pharmaceuticals; reagent paper for medical purposes; oiled paper for medical purposes; adhesive tapes for medical purposes; drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; gauze for dressings; empty capsules for pharmaceuticals; eyepatches for medical purposes; ear bandages; menstruation bandages; menstruation tampons; sanitary napkins; sanitary panties; absorbent cotton; adhesive plasters; bandages for dressings; liquid bandages; breast-nursing pads; cotton swabs for medical use; dental materials; diapers; nappy covers; fly catching paper; mothproofing paper; lacteal flour for babies; dietary supplements for humans; dietetic beverages adapted for medical purposes; dietetic foods adapted for medical purposes; beverages for babies; food for babies; dietary supplements for animals; semen for artificial insemination. Medical apparatus and instruments; medical devices; pacifiers for babies; ice bag pillows for medical purposes; triangular bandages; support bandages; surgical catgut; feeding cups for medical purposes; dropping pipettes for medical purposes; teats; medical ice bags; medical ice bag holders; baby bottles; nursing bottles; contraceptives, non-chemical; artificial tympanic membranes; prosthetic or filling materials, not for dental use; sanitary masks for personal use.

Goods & Services

Pharmaceuticals; reagent paper for medical purposes; oiled paper for medical purposes; adhesive tapes for medical purposes; drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; gauze for dressings; empty capsules for pharmaceuticals; eyepatches for medical purposes; ear bandages; menstruation bandages; menstruation tampons; sanitary napkins; sanitary panties; absorbent cotton; adhesive plasters; bandages for dressings; liquid bandages; breast-nursing pads; cotton swabs for medical use; dental materials; diapers; nappy covers; fly catching paper; mothproofing paper; lacteal flour for babies; dietary supplements for humans; dietetic beverages adapted for medical purposes; dietetic foods adapted for medical purposes; beverages for babies; food for babies; dietary supplements for animals; semen for artificial insemination. Medical apparatus and instruments; medical devices; pacifiers for babies; ice bag pillows for medical purposes; triangular bandages; support bandages; surgical catgut; feeding cups for medical purposes; dropping pipettes for medical purposes; teats; medical ice bags; medical ice bag holders; baby bottles; nursing bottles; contraceptives, non-chemical; artificial tympanic membranes; prosthetic or filling materials, not for dental use; sanitary masks for personal use.

Abstract

This material for treating fistula includes a gelatin hydrogel crosslinked gelatin gel containing a basic fibroblast growth factor.

IPC Classes  ?

• A61K 38/22 - Hormones
• A61K 9/06 - Ointments; Bases therefor
• A61K 9/14 - Particulate form, e.g. powders
• A61K 47/42 - Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
• A61P 13/10 - Drugs for disorders of the urinary system of the bladder
• A61P 17/00 - Drugs for dermatological disorders
• C07K 14/50 - Fibroblast growth factor (FGF)

Abstract

A medicinal composition for preventing or treating secondary hyperparathyroidism under maintenance dialysis, said medicinal composition comprising 3-{[(2S)-2-amino-2-carboxyethyl]carmaboylamino}-5-chloro-4-methylbenzenesulfonic acid or a pharmaceutically acceptable salt thereof, or a solvate of the same which is to be administered by a predefined route in a predefined dosage. According to the present invention, it is possible to provide a prophylactic or therapeutic agent for secondary hyperparathyroidism under maintenance dialysis, said agent showing reduced side effects or no significant accumulation. This medicinal agent allows easy administration management and has a high safety compared with conventional products.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61P 5/18 - Drugs for disorders of the endocrine system of the parathyroid hormones
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

Provided is a pharmaceutical composition which contains 3-{[(2S)-2-amino-2-carboxyethyl]carbamoylamino}-5-chloro-4-methylbenzene sulfonic acid, a pharmaceutically acceptable salt thereof, or a solvate thereof, has a pH of at most 8.0, and has favorable pharmaceutical composition stability.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61K 47/02 - Inorganic compounds
• A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
• A61P 5/20 - Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH

Abstract

Provided is a pharmaceutical composition which contains 3-{[(2S)-2-amino-2-carboxyethyl]carbamoylamino}-5-chloro-4-methylbenzene sulfonic acid, a pharmaceutically acceptable salt thereof, or a solvate thereof, has a pH of at most 8.0, and has favorable pharmaceutical composition stability.

IPC Classes  ?

• A61P 5/18 - Drugs for disorders of the endocrine system of the parathyroid hormones
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 9/08 - Solutions
• A61K 47/02 - Inorganic compounds
• A61K 47/10 - Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)

Abstract

A first transmitting antenna (40a) applied to a body surface emits a first transmission wave, a reflective body (5) present inside the body reflects the first transmission wave transmitted by the first transmitting antenna (40a), a first receiving antenna (41a) applied to the body surface receives the first transmission wave transmitted by the first transmitting antenna (40a) and the reflected wave reflected by the reflective body (5), and a position estimation device (2) estimates passing of the reflective body (5) in the interior of the body on the basis of the first transmission wave received by the first receiving antenna (41a) and the change in the phase of the reflected wave at time t and time t+Δt.

IPC Classes  ?

• A61B 1/00 - Instruments for performing medical examinations of the interior of cavities or tubes of the body by visual or photographical inspection, e.g. endoscopes; Illuminating arrangements therefor
• A61B 5/06 - Devices, other than using radiation, for detecting or locating foreign bodies

Abstract

To provide a pharmaceutical composition which can be used for the treatment of chronic constipation over the long-term. A pharmaceutical composition for treating chronic constipation, characterized by being used for the treatment of patients with chronic constipation, over a prolonged treatment period including administration period of one or several times, including polyethylene glycol, sodium chloride, sodium bicarbonate, and potassium chloride.

IPC Classes  ?

• A61K 31/765 - Polymers containing oxygen
• A61K 33/10 - Carbonates; Bicarbonates
• A61K 33/14 - Alkali metal chlorides; Alkaline earth metal chlorides
• A61P 1/10 - Laxatives

Abstract

A medicinal composition for preventing or treating secondary hyperparathyroidism under maintenance dialysis, said medicinal composition comprising 3-{[(2S)-2-amino-2-carboxyethyl]carmaboylamino}-5-chloro-4-methylbenzenesulfonic acid or a pharmaceutically acceptable salt thereof, or a solvate of the same which is to be administered by a predefined route in a predefined dosage. According to the present invention, it is possible to provide a prophylactic or therapeutic agent for secondary hyperparathyroidism under maintenance dialysis, said agent showing reduced side effects or no significant accumulation. This medicinal agent allows easy administration management and has a high safety compared with conventional products.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61P 5/18 - Drugs for disorders of the endocrine system of the parathyroid hormones
• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups

Abstract

A medicinal composition for preventing or treating secondary hyperparathyroidism under maintenance dialysis, said medicinal composition comprising 3-{[(2S)-2-amino-2-carboxyethyl]carmaboylamino}-5-chloro-4-methylbenzenesulfonic acid or a pharmaceutically acceptable salt thereof, or a solvate of the same which is to be administered by a predefined route in a predefined dosage. According to the present invention, it is possible to provide a prophylactic or therapeutic agent for secondary hyperparathyroidism under maintenance dialysis, said agent showing reduced side effects or no significant accumulation. This medicinal agent allows easy administration management and has a high safety compared with conventional products.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61P 5/18 - Drugs for disorders of the endocrine system of the parathyroid hormones
• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups

Abstract

Provided is a stent 51C made of a cylindrical braid formed from a plurality of filament yarns containing a biodegradable polymer, wherein connecting points 53a-53d are formed at the ends of the filament yarns constituting the braid so as to be aligned in two or more rows in the longitudinal direction of the braid. Elastic yarns 54a-54d are disposed outside at least a part of the stent 51C and at least a longitudinal part, of the elastic yarns, that includes the vicinity of the ends thereof. One end of each of the elastic yarns is fixed in the vicinity of a stent end, while the other end is fixed at any position in the stent. When the diameter of the stent is contracted, tension may be applied to the elastic yarns. Accordingly, provided are: a stent that is easy to mount to a delivery system and enables an easy expansion operation; and a medical device including this stent.

IPC Classes  ?

• A61F 2/90 - Stents in a form characterised by wire-like elements; Stents in a form characterised by a net-like or mesh-like structure characterised by a net-like or mesh-like structure

Abstract

Provided is a compound having α4 integrin inhibitory action. The compound is a sulfonamide derivative represented by the following formula (I), or pharmaceutically acceptable salt thereof: 5, e to h, D, and B represent those as described in the specification.

IPC Classes  ?

• A61K 31/18 - Sulfonamides
• C07D 307/02 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
• C07D 471/04 - Ortho-condensed systems
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms

Abstract

Compounds of represented by formula (I): wherein each symbol is defined herein and pharmaceutically acceptable salts thereof exhibit TRPA1 antagonist activity and are useful as TRPA1 antagonists and the prophylaxis or treatment of diseases involving TRPA1.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: The pharmaceutical preparation is excellent in the solubility and the storage stability even if the amount of the compound or the salt included in each individual dosage unit is increased.

IPC Classes  ?

• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - Dragees; Coated pills or tablets

Abstract

The present invention provides a granular preparation which has an improved feel of ingestion and comprises isoleucine, leucine and valine. The present invention relates to a granular preparation comprising isoleucine, leucine and valine as active component, the granular preparation containing a gelling agent.

IPC Classes  ?

• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61K 9/16 - Agglomerates; Granulates; Microbeadlets
• A61K 47/10 - Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

Abstract

The present invention is a method for determining the possibility of the onset of sporadic colon cancer, wherein: the method for determining the possibility of the onset of sporadic colon cancer includes a measurement step for measuring the methylation rate of one or more CpG sites selected from the group consisting of CpG sites in base sequences represented by SEQ ID NOS: 1-93 in DNA recovered from a biological sample taken from a human subject, and a determination step for determining the possibility of the onset of sporadic colon cancer in the human subject on the basis of the methylation rate measured in the measurement step and a preset reference value or a preset multivariate discriminant; the reference value is a value for distinguishing sporadic colon cancer patients and non-sporadic colon cancer patients, the value being set respectively for the methylation rate of each of the CpG sites; and the multivariate discriminant includes as a variable the methylation rate of one or more CpG sites among the CpG sites in base sequences represented by SEQ ID NOS: 1-93.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
• C12N 15/09 - Recombinant DNA-technology
• C12N 15/117 - Nucleic acids having immunomodulatory properties, e.g. containing CpG-motifs

Abstract

The present invention provides a method for determining the onset risk of sporadic colon caner, said method comprising a measurement step for measuring the methylation ratios of one or more CpG sites present in specific variable methylation regions in DNA which is recovered from a biological sample collected from a human subject, and a determination step for determining the onset risk of sporadic colon cancer in the human subject on the basis of the average methylation ratio of the variable methylation regions which is calculated using the measured methylation ratios and preset standard values or a preset multivariate discriminant, wherein: the standard values are set respectively for the methylation ratios of the individual variable methylation regions in order to discriminate a sporadic colon cancer patient from a non-sporadic colon cancer patient; and the multivariate discriminant includes, as a variant, the average methylation ratio of one or more variable methylation regions among the specific variable methylation regions.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
• C12N 15/09 - Recombinant DNA-technology

Abstract

The present invention is a method for determining the possibility of the onset of colon cancer in human ulcerative colitis patients, wherein the method for determining the possibility of onset of colon cancer includes a measurement step for measuring the methylation rate of one or more CpG sites selected from the group consisting of CpG sites in base sequences represented by SEQ ID NOS: 1-80 in DNA recovered from a biological sample collected from a human ulcerative colitis patient, and a determination step for determining the possibility of onset of colon cancer in the human ulcerative colitis patient on the basis of the methylation rate measured in the measurement step and a preset reference value or preset multivariate discriminant.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
• C12N 15/09 - Recombinant DNA-technology
• G01N 33/48 - Biological material, e.g. blood, urine; Haemocytometers
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing

Abstract

The present invention provides a method for judging the onset possibility of large bowel cancer in a human ulcerative colitis patient, etc. The method comprises a measurement step for measuring methylation ratios at one or more CpG sites existing in specific differentially methylated regions in DNA collected from a biological sample that is obtained from the human ulcerative colitis patient, and a judgment step for judging the onset possibility of large bowel cancer in the human ulcerative colitis patient on the basis of the average methylation ratio of the differentially methylated regions, said average methylation ratio being calculated from the measured methylation ratios, and preset standard values or a preset multivariable discriminant, wherein: the standard values are values having been set for the methylation ratios in the respective differentially methylated regions for discriminating a cancerous ulcerative colitis patient from a non-cancerous ulcerative colitis patient; and the multivariable discriminant contains, as variables, the average methylation ratios at one or more differentially methylated regions among the specific differentially methylated regions.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
• C12M 1/26 - Inoculator or sampler
• C12N 15/09 - Recombinant DNA-technology
• G01N 1/04 - Devices for withdrawing samples in the solid state, e.g. by cutting
• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing

Abstract

The purpose of the present invention is to provide a novel compound having TRPA1 antagonist activity, a medicine containing the compound, and a pharmaceutical agent applicable to prophylaxis or treatment of diseases associated with TRPA1 antagonists and TRPA1. This compound represented by formula (I): [in the formula, each symbol is as defined in the description] or a pharmaceutically acceptable salt thereof, and a medicine or the like containing the compound or a pharmaceutically acceptable salt thereof, have TRPA1 antagonist activity, and are applicable to prophylaxis or treatment of diseases associated with TRPA1 antagonists and TRPA1.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 11/06 - Antiasthmatics
• A61P 11/08 - Bronchodilators
• A61P 11/14 - Antitussive agents
• A61P 17/04 - Antipruritics
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07K 14/705 - Receptors; Cell surface antigens; Cell surface determinants

Abstract

Provided is a compound having (alpha)4 integrin inhibitory action.The compound is a sulfonamide derivative represented by the following formula (I), or pharmaceutically acceptable salt thereof:where Ri to R5, e to h, D, and B represent those as described in the specification. Also disclosed is the use of the compound for the treatment or prevention of an inflammatory disease in which an a4[37 integrin-dependent adhesion process is involved.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/63 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 239/96 - Two oxygen atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Abstract

The purpose of the present invention is to provide a novel compound having TRPA1 antagonist activity, a medicine containing the compound, and a pharmaceutical agent applicable to prophylaxis or treatment of diseases associated with TRPA1 antagonists and TRPA1. This compound represented by formula (I): [in the formula, each symbol is as defined in the description] or a pharmaceutically acceptable salt thereof, and a medicine or the like containing the compound or a pharmaceutically acceptable salt thereof, have TRPA1 antagonist activity, and are applicable to prophylaxis or treatment of diseases associated with TRPA1 antagonists and TRPA1.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 11/06 - Antiasthmatics
• A61P 11/08 - Bronchodilators
• A61P 11/14 - Antitussive agents
• A61P 17/04 - Antipruritics
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07K 14/705 - Receptors; Cell surface antigens; Cell surface determinants

Abstract

Provided is a compound having an excellent integrin α4 inhibiting action. A sulfonamide derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1-R5, e-h, D, and B are as defined in the specification.)

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• C07D 239/96 - Two oxygen atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/04 - Ortho-condensed systems
• C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Abstract

Provided is a compound having an integrin α4 inhibiting action. A sulfonamide derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1-R5, e-h, D, and B are as defined in the specification.)

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/63 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 239/96 - Two oxygen atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Abstract

Provided is a pharmaceutical composition for treating ulcerative colitis, comprising a compound represented by a formula (1) or a pharmaceutically acceptable salt thereof, wherein the compound or the pharmaceutically acceptable salt is administered in an amount of 600 mg or more per day to an ulcerative colitis patient.

IPC Classes  ?

• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/20 - Pills, lozenges or tablets

Abstract

In the present invention, a compound represented by formula (I) (where each symbol in the formula is the same as defined in the description) or a pharmaceutically acceptable salt thereof has excellent TRPA1 antagonist activity, and the compound or pharmaceutically acceptable salt thereof is useful in the prevention or treatment of diseases associated with TRPA1 antagonist and TRPA1.

IPC Classes  ?

• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/501 - Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/06 - Antiasthmatics
• A61P 17/00 - Drugs for dermatological disorders
• A61P 17/04 - Antipruritics
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Abstract

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.

IPC Classes  ?

• C07D 307/82 - Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 453/06 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing iso-quinuclidine ring systems
• C07D 498/04 - Ortho-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Abstract

41, and a to h are as described in the description).

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 487/04 - Ortho-condensed systems
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

Provided is an enema for rectal application, which can be used for treating inflammatory bowel disease or preventing the recurrent of inflammatory bowel disease and contains budesonide as an active ingredient. An enema for rectal application, which is characterized by containing budesonide as an active ingredient and being administered in such a manner that a single dose of 1.5 to 2.5 mg of budesonide can be taken twice a day for 6 weeks for treating inflammatory bowel disease or preventing the recurrent of inflammatory bowel disease; an enema for rectal application as mentioned above, wherein the dose of budesonide per one time is 2.0 mg; any one of the above-mentioned enemas for rectal application, which is administered for treating ulcerative colitis or Crohn's disease or preventing the recurrence of ulcerative colitis or Crohn's disease; and any one of the aforementioned enemas for rectal application, which is in the form of a foam or a liquid.

IPC Classes  ?

• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61K 9/08 - Solutions
• A61K 9/12 - Aerosols; Foams
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Abstract

Provided is a new drug for treating disorders of the corneal epithelium which acts directly on the corneal epithelium cells. The effective component of this drug for treating disorders of the corneal epithelium is the compound represented in general formula (1) or a salt thereof. (In the formula, A represents an aromatic ring, a heterocyclic ring or an aliphatic ring; R2, R3 and R4 are the same or different and independently represent a hydrogen atom, a halogen atom, etc.; B represents an aromatic ring optionally having a substituent, a heterocyclic ring optionally having a substituent, or an aliphatic ring optionally having a substituent; -X-, -Y- and -Z- are the same or different and independently represent -O-, -NH-, -NR5-, -S-, -SO-, -SO2-, -CH2-, -CR6R7- or -CO-; and -W- represents -NR1-, -O- or -CR8R9-.)

IPC Classes  ?

• A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
• A61P 27/02 - Ophthalmic agents
• C07D 487/04 - Ortho-condensed systems

Abstract

The present invention provides a pharmaceutical composition containing cilnidipine or a pharmaceutically acceptable salt thereof as an active ingredient. The present invention relates to: a dynamin-related protein 1 (Drp1) polymerization inhibitor characterized by containing cilnidipine or a pharmaceutically acceptable salt thereof as an active ingredient and also characterized by being capable of inhibiting the polymerization of Drp1; a pharmaceutical composition containing the Drp1 polymerization inhibitor as an active ingredient; and a pharmaceutical composition as described above, which can be used for the prevention or treatment of post-myocardial-infarction chronic heart failure, or the reduction in cardiomyocyte toxicity caused by organic mercury, or the alleviation of an insulin-dependent hyperglycemic state.

IPC Classes  ?

• A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 39/02 - Antidotes
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.

IPC Classes  ?

• A61K 31/4402 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
• A23L 27/20 - Synthetic spices, flavouring agents or condiments
• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
• C07C 309/51 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
• C07C 311/32 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
• C07C 311/51 - Y being a hydrogen or a carbon atom
• C07C 333/08 - Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
• C07C 335/16 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
• C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• C07D 271/10 - 1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07D 295/192 - Radicals derived from carboxylic acids from aromatic carboxylic acids
• A61K 31/185 - Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
• A61K 31/417 - Imidazole-alkylamines, e.g. histamine, phentolamine
• A61K 31/4245 - Oxadiazoles
• A61K 31/44 - Non-condensed pyridines; Hydrogenated derivatives thereof
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine

Abstract

Provided is a pharmaceutical composition for treating ulcerative colitis, comprising a compound represented by a formula (1) or a pharmaceutically acceptable salt thereof, wherein the compound or the pharmaceutically acceptable salt is administered in an amount of 1500 mg or more per day to an ulcerative colitis patient. (see formula 1)

IPC Classes  ?

• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Abstract

Provided is a pharmaceutical composition which is for treating ulcerative colitis and includes a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein said compound or pharmaceutically acceptable salt thereof is administered to a patient having ulcerative colitis in a dose of at least 600 mg per day.

IPC Classes  ?

• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Abstract

Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 333/40 - Thiophene-2-carboxylic acid
• C07D 319/12 - 1,4-Dioxanes; Hydrogenated 1,4-dioxanes not condensed with other rings
• A61K 31/19 - Carboxylic acids, e.g. valproic acid
• A61K 31/396 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having three-membered rings, e.g. aziridine
• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61K 31/4436 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 38/05 - Dipeptides

Abstract

A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof is provided.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 3/04 - Anorexiants; Antiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

The purpose of the present invention is to provide a novel compound that is capable of activating glycogen synthase but hardly activates receptor PPAR and shows high safety. Provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/4245 - Oxadiazoles
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/443 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems

Abstract

The present invention pertains to stabilization of a certain class of benzothia(dia)zepine derivative in a solid preparation containing the derivative. The present invention provides a solid preparation containing (A) the benzothia(dia)zepine derivative, and (B) a specific plasticizer, wherein either the component (A) and the component (B) are isolated, or, when the component (A) and the component (B) are not isolated, the component (B) content is no more than 0.9 wt.% based on the total weight of the solid preparation. The solid preparation is formed so as to be provided with at least one core, and at least one sheath layer or capsule layer enveloping at least a portion of the core, the component (A) being blended into the core, and the component (B) being blended into the sheath layer or capsule layer. The component (B) content of the sheath layer or capsule layer is no more than 45 wt.% based on the total weight of the sheath layer or capsule layer.

IPC Classes  ?

• A61K 38/00 - Medicinal preparations containing peptides
• A61K 9/30 - Organic coatings
• A61K 9/32 - Organic coatings containing solid synthetic polymers
• A61K 9/34 - Organic coatings containing natural gums or resins
• A61K 9/36 - Organic coatings containing carbohydrates or derivatives thereof
• A61K 9/42 - Organic coatings containing waxes, higher fatty acids, higher fatty alcohols, or derivatives thereof, e.g. chocolate
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61K 47/02 - Inorganic compounds
• A61K 47/04 - Non-metals; Compounds thereof
• A61K 47/10 - Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 47/38 - Cellulose; Derivatives thereof
• A61K 47/44 - Oils, fats or waxes according to two or more groups of ; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61P 1/10 - Laxatives
• A61P 3/06 - Antihyperlipidemics
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

The present invention pertains to stabilization of a certain class of benzothia(dia)zepine derivative, in a solid preparation containing the derivative. According to the present invention, either the solid preparation containing the benzothia(dia)zepine derivative does not incorporate a combination of polyethylene glycol and polyvinyl alcohol; or, in the case that the solid preparation does incorporate a combination of polyethylene glycol and polyvinyl alcohol, the derivative and the combination of polyethylene glycol and polyvinyl alcohol are isolated.

IPC Classes  ?

• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - Dragees; Coated pills or tablets
• A61K 9/36 - Organic coatings containing carbohydrates or derivatives thereof
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 47/02 - Inorganic compounds
• A61K 47/04 - Non-metals; Compounds thereof
• A61K 47/38 - Cellulose; Derivatives thereof
• A61K 47/44 - Oils, fats or waxes according to two or more groups of ; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/10 - Laxatives
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
• A61P 7/02 - Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• A61P 9/06 - Antiarrhythmics
• A61P 9/08 - Vasodilators for multiple indications
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 9/14 - Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Provided are a production method for a compound (VI) that is useful as a therapeutic agent for diabetes, a production intermediate thereof, and a crystal. The production method for the compound (VI) or a salt thereof includes: a step (d) in which a compound (II) is reacted with an acid halogenation agent and converted to an acid halide; a step (e) in which the acid halide is reacted with a compound (IV) in the presence of a base, and a compound (V) or a salt thereof is crystallized from the reaction system; and a step (f) in which, after the compound (V) is subjected to a reductive deprotection reaction in the presence of a metal catalyst, a compound (VI) or a salt thereof is crystallized from the reaction system (in the formula, R5 represents an aralkyl group that may include a substituent group, an aralkyl oxymethyl group that may include a substituent group, or a heteroaryl alkyl group that may include a substituent group).

IPC Classes  ?

• C07D 333/40 - Thiophene-2-carboxylic acid

Abstract

　Provided are a method for producing a compound (9) useful as a drug for the treatment of diabetes, and a production intermediate thereof. (a) A diester (3) is synthesized by reacting a compound (1) and a compound (2), (b) an ester (4) is synthesized by deprotecting the diester (3) (or an ester (4) is synthesized by reacting a compound (5) and the compound (2)), (c) the ester (4) is converted into an acid halide, (d) the acid halide is reacted with an amidinophenol derivative, and (e) the resulting diester derivative is deprotected under acidic conditions and converted into compound (9) (in the formula, R1 represents a halogen atom, R4 represents a lower alkyl group, R5 represents a lower alkyl group, and R12 represents a hydrogen atom or a halogen atom).

IPC Classes  ?

• C07D 333/40 - Thiophene-2-carboxylic acid
• C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

　Provided is a novel compound having a higher MGAT2-inhibiting activity than conventional compounds, said compound being represented by general formula (I); or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 3/04 - Anorexiants; Antiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Provided is a compound represented by formula (I) [wherein each symbol is as defined in the description] or a pharmaceutically acceptable salt thereof. This compound has an excellent TRPA1 antagonistic activity, which makes it possible to provide a TRPA1 antagonist and a medicine that is useful for preventing or treating diseases associated with TRPA1.

IPC Classes  ?

• C07D 307/82 - Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
• A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/06 - Antiasthmatics
• A61P 13/10 - Drugs for disorders of the urinary system of the bladder
• A61P 17/04 - Antipruritics
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 498/04 - Ortho-condensed systems

Abstract

The present invention includes a renal impairment or inner ear disorder inhibitor that includes, as an active component, cilastatin or a pharmaceutically acceptable salt thereof, and is induced via megalin by at least one megalin ligand selected from the group consisting of polymyxins, aminoglycoside antibiotics, glycopeptide antibiotics, cisplatin, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

• A61K 31/201 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having one or two double bonds, e.g. oleic or linoleic acid
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Provided is a sulfonamide derivative represented by the following general formula (1) and having an .alpha.4 integrin inhibitory effect with high selectivity with a low effect on .alpha.4.beta.1 and a high effect on .alpha.4.beta.7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 11/06 - Antiasthmatics
• A61P 17/06 - Antipsoriatics
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• A61P 35/04 - Antineoplastic agents specific for metastasis
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems

Abstract

Provided is a sulfonamide derivative represented by general formula (1) [wherein A, B, D, E, R41 and a to h are each as defined in the description], which has a highly selective α4 integrin inhibitory effect, i.e., being less effective on α4β1 but highly effective on α4β7, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 11/06 - Antiasthmatics
• A61P 17/06 - Antipsoriatics
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• A61P 35/04 - Antineoplastic agents specific for metastasis
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems

Abstract

Compounds represented by the following formula (I); are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
• C07D 319/12 - 1,4-Dioxanes; Hydrogenated 1,4-dioxanes not condensed with other rings
• C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 333/40 - Thiophene-2-carboxylic acid

Abstract

Sulfonamide compounds of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action. The compounds have formulae represented by:

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07C 53/18 - Halogenated acetic acids containing fluorine
• C07F 9/655 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
• C07F 9/38 - Phosphonic acids (R—P(:O)(OH)2); Thiophosphonic acids

Abstract

Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07C 53/18 - Halogenated acetic acids containing fluorine
• C07F 9/655 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms

Abstract

Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• C07D 333/40 - Thiophene-2-carboxylic acid
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61P 3/04 - Anorexiants; Antiobesity agents
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• C07D 319/12 - 1,4-Dioxanes; Hydrogenated 1,4-dioxanes not condensed with other rings

Abstract

Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent .alpha.4 integrin-inhibitory action.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/04 - Ortho-condensed systems
• C07D 473/04 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms

Abstract

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.

IPC Classes  ?

• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
• C07C 309/51 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
• C07C 311/32 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
• C07C 311/52 - Y being a hetero atom
• C07C 333/08 - Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
• C07C 335/16 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
• C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
• C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• C07D 271/10 - 1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• C07D 295/192 - Radicals derived from carboxylic acids from aromatic carboxylic acids
• A23L 1/226 - Synthetic spices or flavouring agents or condiments
• C07C 311/51 - Y being a hydrogen or a carbon atom
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals

Abstract

The disclosed pharmaceutical preparation comprises a compound represented by the chemical formula (A) or a pharmaceutically acceptable salt thereof, which is dispersed in a matrix consisting of a water-soluble high molecular weight substance; and Crospovidone: The pharmaceutical preparation is excellent in the solubility and the storage stability even if the amount of the compound or the salt included in each individual dosage unit is increased.

IPC Classes  ?

• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/28 - Dragees; Coated pills or tablets

Abstract

Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

IPC Classes  ?

• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

Abstract

A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi. (see formula I)

IPC Classes  ?

• C07C 275/42 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
• A23L 27/20 - Synthetic spices, flavouring agents or condiments
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61K 31/198 - Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/4045 - Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
• A61K 31/417 - Imidazole-alkylamines, e.g. histamine, phentolamine
• A61K 31/4245 - Oxadiazoles
• A61K 31/4402 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 1/12 - Antidiarrhoeals
• A61P 5/20 - Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07C 309/51 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
• C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• C07C 311/51 - Y being a hydrogen or a carbon atom
• C07C 335/22 - Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
• C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• C07D 271/10 - 1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
• C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
• C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

IPC Classes  ?

• A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• C07D 239/80 - Oxygen atoms
• C07D 239/88 - Oxygen atoms
• C07C 61/08 - Saturated compounds having a carboxyl group bound to a six-membered ring
• C07C 63/06 - Benzoic acid
• C07C 229/56 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho- position

Abstract

A gene coded for a polypeptide which possesses interleukin-2 activity is isolated, and connected with a vector DNA which is capable of replicating in a procaryotic or eucaryotic cell at a position downstream of a promoter gene in the vector obtaining a recombinant DNA, with which the cell is transformed to produce interleukin-2.

IPC Classes  ?

• C12N 15/26 - Interleukin-2
• C07K 14/55 - IL-2
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 15/81 - Vectors or expression systems specially adapted for eukaryotic hosts for fungi for yeasts
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione

Abstract

An interleukin-2 polypeptide bearing threonine as the C-terminal amino acid and no sugar moiety obtained from cells of Escherichia coli constructed by gene-recombination has biochemical and biological behaviour comparable with that of IL-2 produced from mammalian cells but are free from physiologically active substances found in IL-2 produced from mammalian cells.

IPC Classes  ?

• C07K 14/55 - IL-2
• A61K 38/20 - Interleukins
• C12N 15/26 - Interleukin-2
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione