An information processing device comprises: an information recording unit 11 that records information related to the menstruation of a user; and a treatment module providing unit 14 that provides, on the basis of the information recorded by the information recording unit 11 and in accordance with the symptoms of premenstrual syndrome of the user, one or more of a plurality of types of treatment modules that execute processing related to treatment based on non-drug therapy. The plurality of types of treatment modules include one or more treatment modules that execute processing based on psychological education, one or more treatment modules that execute processing based on cognitive reconstruction methods, and one or more treatment modules that execute processing based on relaxation methods. With this configuration, from among the plurality of types of treatment modules, a treatment module suitable for each user can be provided to the user in accordance with the recorded information.
G16H 20/70 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to mental therapies, e.g. psychological therapy or autogenous training
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
A compound of the formula (I) or a salt thereof (R represents methyl group or fluorine atom) having an mPGES-1 inhibitory activity and useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of such diseases as inflammation, pain, or rheumatism.
A compound of the formula (I) or a salt thereof (R represents methyl group or fluorine atom) having an mPGES-1 inhibitory activity and useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of such diseases as inflammation, pain, or rheumatism.
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
3.
THERAPEUTIC OR PROPHYLACTIC AGENT FOR POLYCYSTIC OVARIAN SYNDROME
Provided is a therapeutic or prophylactic agent for PCOS, which is for treating or ameliorating PCOS. A 2-oxapregnane compound represented by formula (1) or a pharmaceutically acceptable salt thereof is used as an active ingredient for the therapeutic or prophylactic agent for PCOS. (In the formula, R1to R3each independently represent an alkyl group, R4 represents a hydrogen atom or an alkylcarbonyl group, X represents a halogen atom, and Y represents a hydroxyl or oxo group which is bonded to position-11, position-15 or position-16 in the steroid skeleton.)
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A compound represented by the following general formula (1), which has a potent inhibitory action against mPGES-1, and is useful as an active ingredient of a medicament for therapeutic treatment of inflammation and the like.
A compound represented by the following general formula (1), which has a potent inhibitory action against mPGES-1, and is useful as an active ingredient of a medicament for therapeutic treatment of inflammation and the like.
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
C07D 239/70 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
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 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
NATIONAL UNIVERSITY CORPORATION HAMAMATSU UNIVERSITY SCHOOL OF MEDICINE (Japan)
Inventor
Tanaka Seiji
Ochiai Hiroyuki
Otsuka Atsushi
Miyake Hideaki
Abstract
The present invention addresses the problem of providing a method for discriminating interstitial cystitis. The present invention relates to a method for discriminating interstitial cystitis, said method comprising measuring at least one of cholesterol ester (ChE) and lysophosphatidylcholine (LPC) in a urine sample.
G01N 33/92 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving lipids, e.g. cholesterol
G01N 27/62 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating the ionisation of gases, e.g. aerosolsInvestigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
G01N 33/493 - Physical analysis of biological material of liquid biological material urine
To provide a novel compound that induces selective degradation of a non-receptor tyrosine kinase (and especially a tyrosine kinase that is part of the JAK family), or a pharmaceutically acceptable salt thereof, and others. Provided is a compound represented by formula I:
To provide a novel compound that induces selective degradation of a non-receptor tyrosine kinase (and especially a tyrosine kinase that is part of the JAK family), or a pharmaceutically acceptable salt thereof, and others. Provided is a compound represented by formula I:
wherein
R1 is a hydrogen atom or a C1-3 alkyl group optionally substituted with one or more deuterium atoms;
R2 is CONHR3 (wherein R3 is a C1-3 alkyl group optionally substituted with one or more OH groups) or a triazole group optionally substituted with one or more C1-3 alkyl groups;
A is a pyridyl group or a pyridazinyl group;
B is
To provide a novel compound that induces selective degradation of a non-receptor tyrosine kinase (and especially a tyrosine kinase that is part of the JAK family), or a pharmaceutically acceptable salt thereof, and others. Provided is a compound represented by formula I:
wherein
R1 is a hydrogen atom or a C1-3 alkyl group optionally substituted with one or more deuterium atoms;
R2 is CONHR3 (wherein R3 is a C1-3 alkyl group optionally substituted with one or more OH groups) or a triazole group optionally substituted with one or more C1-3 alkyl groups;
A is a pyridyl group or a pyridazinyl group;
B is
and
n is an integer between 0 and 12,
or a pharmaceutically acceptable salt or the like thereof.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
A compound of the formula (I) or a salt thereof (R represents methyl group or fluorine atom) having an mPGES-1 inhibitory activity and useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of such diseases as inflammation, pain, or rheumatism.
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Provided is a solid preparation having an excellent stability and being useful for treating or improving (or alleviating) a urination disorder regardless of the degree or presence of prostatomegaly. The solid preparation contains a 2-oxapregnane compound represented by the following formula (1) as an active ingredient, and a carrier.
Provided is a solid preparation having an excellent stability and being useful for treating or improving (or alleviating) a urination disorder regardless of the degree or presence of prostatomegaly. The solid preparation contains a 2-oxapregnane compound represented by the following formula (1) as an active ingredient, and a carrier.
Provided is a solid preparation having an excellent stability and being useful for treating or improving (or alleviating) a urination disorder regardless of the degree or presence of prostatomegaly. The solid preparation contains a 2-oxapregnane compound represented by the following formula (1) as an active ingredient, and a carrier.
In the formula, R1 to R3 each represent an alkyl group such as a methyl group, R4 represents an alkylcarbonyl group such as an acetyl group, X represents a halogen atom such as a chlorine atom, and Y represents a hydroxyl group or oxo group bonded to the 11-position, 15-position, or 16-position of the steroid skeleton. The carrier contains a first carrier and/or a second carrier; the first carrier is not a metal salt-form, and the second carrier is a polyvalent metal salt-form of an inorganic acid.
Compounds represented by general formula (1), the compounds having strong inhibitory action against mPGES-1 and being useful as active ingredients for pharmaceuticals for the treatment of inflammation and the like.
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 13/00 - Drugs for disorders of the urinary system
A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
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 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 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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 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
The present invention addresses the problem of providing a pregnancy-induced hypertension syndrome therapy composition having controlled placental permeability. Provided are nicotinamide-encapsulating micelles having a particle diameter of 25-100 nm. Controlling the particle diameter of the nicotinamide-encapsulating micelles enables control of placental permeability so as to make it possible to accumulate nicotinamide-encapsulating micelles in a placental while suppressing transfer to a fetus. Administering the nicotinamide-encapsulating micelles brings about a superior effect of reducing blood pressure during a pregnancy-induced hypertension syndrome.
Described is a method for differentiating destructive thyroiditis, including measuring at least one of monoiodotyrosine and diiodotyrosine in a sample.
The present invention provides a novel compound that induces selective degradation of a non-receptor tyrosine kinase (and especially a tyrosine kinase that constitutes the JAK family), or a pharmaceutically acceptable salt thereof. Provided is a compound represented by formula I [formula 1] (In the formula, R11-31-3 alkyl group that may be substituted with one or more deuterium atoms; R2is CONHR3(in the formula, R31-31-31-3 alkyl groups; A is a pyridyl group or a pyridazinyl group; B is represented by [Formula 2]; and n is an integer between 0 and 12), or a pharmaceutically acceptable salt thereof.
4 represents an alkylcarbonyl group such as acetyl group, X represents a halogen atom such as a chlorine atom, Y represents a hydroxyl group or oxo group bonded to the 11-position, 15-position, or 16-position of the steroid skeleton.)
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
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
The present invention pertains to: a compound that is represented by formula (I), that has a mPGES-1 inhibitory effect, and that is useful as an active ingredient of a medicine for treating and/or preventing diseases such as inflammation, pain, or rheumatism; or a salt of said compound (R represents a methyl group or a fluorine atom).
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
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 25/28 - 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
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
The present invention pertains to: a compound that is represented by formula (I), that has a mPGES-1 inhibitory effect, and that is useful as an active ingredient of a medicine for treating and/or preventing diseases such as inflammation, pain, or rheumatism; or a salt of said compound (R represents a methyl group or a fluorine atom).
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 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
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 25/28 - 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
1344 represents an alkylcarbonyl group such as an acetyl group, X represents a halogen atom such as a chlorine atom, and Y represents an oxo group or a hydroxyl group bound at position 11, 15, or 16 of a steroid backbone).
A powder preparation for nasal administration containing a particulate of steroid hormones having an average particle size of 50 to 300 μm as an active ingredient is prepared.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
The present invention aims at improving the stability of a thyroid hormone-containing solid formulation. More specifically, the present invention aims at developing a technique capable of further improving the stability of a thyroid hormone-containing solid formulation. The inventors of the present invention extensively conducted further studies to develop a technique for improving the stability of the thyroid hormone-containing solid formulation and found that the stability of the thyroid hormone-containing solid formulation was significantly enhanced when a step of granulating a mixture of thyroid hormone and additives by a wet granule compression method was included in the formulation procedure. The present invention has been accomplished based on this finding.
The present invention addresses the problem of providing a pregnancy-induced hypertension syndrome therapy composition having controlled placental permeability. Provided are nicotinamide-encapsulating micelles having a particle diameter of 25-100 nm. Controlling the particle diameter of the nicotinamide-encapsulating micelles enables control of placental permeability so as to make it possible to accumulate nicotinamide-encapsulating micelles in a placenta while suppressing transfer to a fetus. Administering the nicotinamide-encapsulating micelles brings about a superior effect of reducing blood pressure during a pregnancy-induced hypertension syndrome.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
29 - Meat, dairy products, prepared or preserved foods
30 - Basic staples, tea, coffee, baked goods and confectionery
31 - Agricultural products; live animals
32 - Beers; non-alcoholic beverages
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemicals; agricultural chemicals, except fungicides,
herbicides, insecticides and parasiticides; plant growth
regulating preparations; proteins for use in the manufacture
of food and beverages. False nails; false eyelashes; cosmetics; perfume and flavor
materials; natural perfumery prepared from vegetables or
plants; natural perfumery prepared from animals; synthetic
perfumery; blended perfumery; food flavorings prepared from
essential oils; soaps and detergents; non-medicated
dentifrices. Pharmaceutical preparations and other preparations for
destroying vermin, fungicides, herbicides; reagent paper 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; dietary supplements for
humans; dietetic beverages adapted for medical purposes;
dietetic foods adapted for medical purposes; dietary
supplements for animals. Finger guards for medical purposes; pacifiers for babies;
ice bag pillows for medical purposes; triangular bandages;
supportive bandages; surgical catguts; 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; ear plugs for sleeping; ear
plugs for soundproofing; medical apparatus and instruments;
sanitary masks for personal use. Edible oils and fats; processed vegetables and fruits;
abura-age [pieces of fried tofu]; freeze-dried tofu pieces
[Kohri-dofu]; jelly made from devils' tongue root
[Konnyaku]; soya milk; tofu; fermented soybeans [Natto];
preserved pulses. Spices; cereal preparations; husked rice; husked oats;
husked barley; flour; tea; oolong tea [Chinese tea]; black
tea [English tea]; tea of salty kelp powder [Kombu-cha];
Mugi-cha [roasted barley tea]; Japanese green tea; tea-based
beverages; prepared coffee and coffee-based beverages;
prepared cocoa and cocoa-based beverages. Edible seaweeds, unprocessed; vegetables, fresh; raw
vegetables, unprocessed; sugar crops; fruit, fresh; malt,
not for food; foxtail millet, unprocessed; proso millet,
unprocessed; sesame, unprocessed; buckwheat, unprocessed;
corn [unprocessed grain]; Japanese barnyard millet,
unprocessed; wheat, barley and oats, unprocessed; rice,
unprocessed; sorghum, unprocessed; animal foodstuffs. Whey beverages. Retail services or wholesale services for pharmaceutical,
veterinary and sanitary preparations and medical supplies. Research in the field of pharmaceuticals; development of
pharmaceuticals; providing information on testing,
inspection or research of pharmaceuticals; consultancy
relating to testing, inspection or research of
pharmaceuticals; testing, inspection or research of
pharmaceuticals, cosmetics or foodstuffs. Clinical examination; providing medical information on
efficacy, side effects, interaction and medication of
pharmaceuticals; providing medical information.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
29 - Meat, dairy products, prepared or preserved foods
30 - Basic staples, tea, coffee, baked goods and confectionery
31 - Agricultural products; live animals
32 - Beers; non-alcoholic beverages
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemicals; agricultural chemicals, except fungicides,
herbicides, insecticides and parasiticides; plant growth
regulating preparations; proteins for use in the manufacture
of food and beverages. False nails; false eyelashes; cosmetics; perfume and flavor
materials; natural perfumery prepared from vegetables or
plants; natural perfumery prepared from animals; synthetic
perfumery; blended perfumery; food flavorings prepared from
essential oils; soaps and detergents; non-medicated
dentifrices. Pharmaceutical preparations and other preparations for
destroying vermin, fungicides, herbicides; reagent paper 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; dietary supplements for
humans; dietetic beverages adapted for medical purposes;
dietetic foods adapted for medical purposes; dietary
supplements for animals. Finger guards for medical purposes; pacifiers for babies;
ice bag pillows for medical purposes; triangular bandages;
supportive bandages; surgical catguts; 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; ear plugs for sleeping; ear
plugs for soundproofing; medical apparatus and instruments;
sanitary masks for personal use. Edible oils and fats; processed vegetables and fruits;
abura-age [pieces of fried tofu]; freeze-dried tofu pieces
[Kohri-dofu]; jelly made from devils' tongue root
[Konnyaku]; soya milk; tofu; fermented soybeans [Natto];
preserved pulses. Spices; cereal preparations; husked rice; husked oats;
husked barley; flour; tea; oolong tea [Chinese tea]; black
tea [English tea]; tea of salty kelp powder [Kombu-cha];
Mugi-cha [roasted barley tea]; Japanese green tea; tea-based
beverages; prepared coffee and coffee-based beverages;
prepared cocoa and cocoa-based beverages. Edible seaweeds, unprocessed; vegetables, fresh; raw
vegetables, unprocessed; sugar crops; fruit, fresh; malt,
not for food; foxtail millet, unprocessed; proso millet,
unprocessed; sesame, unprocessed; buckwheat, unprocessed;
corn [unprocessed grain]; Japanese barnyard millet,
unprocessed; wheat, barley and oats, unprocessed; rice,
unprocessed; sorghum, unprocessed; animal foodstuffs. Whey beverages. Retail services or wholesale services for pharmaceutical,
veterinary and sanitary preparations and medical supplies. Research in the field of pharmaceuticals; development of
pharmaceuticals; providing information on testing,
inspection or research of pharmaceuticals; consultancy
relating to testing, inspection or research of
pharmaceuticals; testing, inspection or research of
pharmaceuticals, cosmetics or foodstuffs. Clinical examination; providing medical information on
efficacy, side effects, interaction and medication of
pharmaceuticals; providing medical information.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
29 - Meat, dairy products, prepared or preserved foods
30 - Basic staples, tea, coffee, baked goods and confectionery
31 - Agricultural products; live animals
32 - Beers; non-alcoholic beverages
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Chemicals; agricultural chemicals, except fungicides,
herbicides, insecticides and parasiticides; plant growth
regulating preparations; proteins for use in the manufacture
of food and beverages. False nails; false eyelashes; cosmetics; perfume and flavor
materials; natural perfumery prepared from vegetables or
plants; natural perfumery prepared from animals; synthetic
perfumery; blended perfumery; food flavorings prepared from
essential oils; soaps and detergents; non-medicated
dentifrices. Pharmaceutical preparations and other preparations for
destroying vermin, fungicides, herbicides; reagent paper 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; dietary supplements for
humans; dietetic beverages adapted for medical purposes;
dietetic foods adapted for medical purposes; dietary
supplements for animals. Finger guards for medical purposes; pacifiers for babies;
ice bag pillows for medical purposes; triangular bandages;
supportive bandages; surgical catguts; 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; ear plugs for sleeping; ear
plugs for soundproofing; medical apparatus and instruments;
sanitary masks for personal use. Edible oils and fats; processed vegetables and fruits;
abura-age [pieces of fried tofu]; freeze-dried tofu pieces
[Kohri-dofu]; jelly made from devils' tongue root
[Konnyaku]; soya milk; tofu; fermented soybeans [Natto];
preserved pulses. Spices; cereal preparations; husked rice; husked oats;
husked barley; flour; tea; oolong tea [Chinese tea]; black
tea [English tea]; tea of salty kelp powder [Kombu-cha];
Mugi-cha [roasted barley tea]; Japanese green tea; tea-based
beverages; prepared coffee and coffee-based beverages;
prepared cocoa and cocoa-based beverages. Edible seaweeds, unprocessed; vegetables, fresh; raw
vegetables, unprocessed; sugar crops; fruit, fresh; malt,
not for food; foxtail millet, unprocessed; proso millet,
unprocessed; sesame, unprocessed; buckwheat, unprocessed;
corn [unprocessed grain]; Japanese barnyard millet,
unprocessed; wheat, barley and oats, unprocessed; rice,
unprocessed; sorghum, unprocessed; animal foodstuffs. Whey beverages. Retail services or wholesale services for pharmaceutical,
veterinary and sanitary preparations and medical supplies. Research in the field of pharmaceuticals; development of
pharmaceuticals; providing information on testing,
inspection or research of pharmaceuticals; consultancy
relating to testing, inspection or research of
pharmaceuticals; testing, inspection or research of
pharmaceuticals, cosmetics or foodstuffs. Clinical examination; providing medical information on
efficacy, side effects, interaction and medication of
pharmaceuticals; providing medical information.
24.
METHOD FOR DIFFERENTIATING DESTRUCTIVE THYROIDITIS FROM OTHER PATHOLOGICAL CONDITIONS
The present invention addresses the problem of providing a method for differentiating destructive thyroiditis. The present invention pertains to a method for differentiating destructive thyroiditis, the method comprising measuring monoiodotyrosine and/or diiodotyrosine in a sample.
Provided is a dysuria-alleviating agent useful for treating or alleviating (or mitigating) dysuria regardless of the presence or degree of prostatomegaly. The dysuria-alleviating agent includes, as an active ingredient, a 2-oxapregnane compound represented by formula 1. (In the formula, R1 to R3 represent an alkyl group such as a methyl group, R4 represents an alkylcarbonyl group such as an acetyl group, X represents a halogen atom such as a chlorine atom, and Y represents a hydroxyl group or an oxo group bonded at the position 11, 15, or 16 of a steroid skeleton.)
1344 represents an alkylcarbonyl group such as an acetyl group, X represents a halogen atom such as a chlorine atom, and Y represents a hydroxyl group or an oxo group bonded at the position 11, 15, or 16 of a steroid skeleton.)
A powder preparation for nasal administration containing a particulate of steroid hormones having an average particle size of 50 to 300 μm as an active ingredient is prepared.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
Provided are a novel internal standard useful in the measurement of androgens, a method capable of measuring the androgen in a highly selective and highly sensitive (accurate) manner using liquid chromatography mass spectrometry with simplified pretreatments, and a method for diagnosis of a disease using the androgen measurement method. The novel stable isotope-labeled compound is synthesized by performing reduction reaction in a specific solvent. An androgen is measured using this novel stable isotope-labeled compound as an IS.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
G01N 30/04 - Preparation or injection of sample to be analysed
G01N 33/74 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving hormones
6 represents an alkyl group, or an alkoxy group), which has an mPGES-1 inhibitory action, and is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of inflammation, pain, rheumatism, and the like.
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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 401/10 - 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 carbon chain containing aromatic rings
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 403/04 - 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 directly linked by a ring-member-to-ring- member bond
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 409/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
30.
15-oxosteroid compound and process for producing the same
Provided is a process for producing a compound, which has an oxo group specifically introduced on the 15-position of a steroid skeleton and which is useful as an intermediate, with a high yield without complicated steps. A compound represented by the formula (2) is allowed to react with an oxidant (e.g., a hypervalent iodine compound) and a co-oxidant (e.g., a peroxide) to produce a 15-oxosteroid compound represented by the formula (1), which is useful as an intermediate:
2).
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
C07J 75/00 - Processes for the preparation of steroids, in general
A powder preparation for nasal administration containing a particulate of steroid hormones having an average particle size of 50 to 300 m as an active ingredient is prepared. The powder preparation for nasal administration may further contain a water-soluble polymer (particularly, water-soluble polysaccharides such as a cellulose having a hydroxyalkyl group). The particulate of steroid hormones may be testosterone and/or a derivative thereof. The water-soluble polymer may be in a particulate form. The ratio of the water-soluble polymer may be about 1 to 50 parts by weight relative to 1 part by weight of the particulate of steroid hormones. The powder preparation for nasal administration may be a powder preparation for nasal administration which can control a C max of steroid hormones to not more than 15 ng/ml. A powder preparation for nasal administration which can control a plasma concentration of steroid hormones such as testosterone in a specific range for a long period of time is provided.
A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
The purpose of the present invention is to prepare a powder preparation for nasal administration that includes, as an active ingredient, a particulate steroid hormone having an average particle size of 50–300μm. The powder preparation for nasal administration may further include a water-soluble polymer (in particular, a water-soluble polysaccharide such as cellulose comprising a hydroxyalkyl group). The particulate steroid hormone may be formed from testosterone and/or a derivative thereof. The water-soluble polymer may be particulate. The proportion of the water-soluble polymer may be around 1–50 parts by weight with respect to 1 part by weight of the particulate steroid hormone. This powder preparation for nasal administration may be configured such that the Cmax of the steroid hormone component can be adjusted to be 15ng/ml or less. The powder preparation for nasal administration enables the concentration of a steroid hormone such as testosterone in the blood to be constrained to a specific range over a long period of time.
A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
Provided are: a novel internal standard substance that is useful for measuring androgen; a highly selective and sensitive (accurate) method for measuring androgen which is capable of simplifying pretreatment and uses liquid chromatography mass spectrometry; and a method for identifying a disease using the method for measuring androgen. A novel stable-isotope-labeled compound is synthesized by performing reduction reaction with a specific solvent. Androgen is measured by using this novel stable-isotope-labeled compound as the internal standard substance.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
G01N 27/62 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating the ionisation of gases, e.g. aerosolsInvestigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode
34.
Crystalline polymorph of 15B-hydroxy-osaterone acetate
Provided is a crystalline polymorphic form A of 15β-hydroxy-osaterone acetate having an improved stability (storage stability, pulverization stability, and absorption characteristics). In a powder X-ray diffraction spectrum, characteristic diffraction peaks of the crystalline polymorphic form A of 15β-hydroxy-osaterone acetate appear at diffraction angles 2θ of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorphic form A has a melting point of 280 to 283° C. and is a prism crystal.
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
A compound which has mPGES-1 inhibitory activity and is useful as an active ingredient of a pharmaceutical product for the treatment of inflammation, pain or diseases such as rheumatism. (In the formula, X represents a carbonyl group or a sulfonyl group; R1represents a hydrogen atom, a halogen atom, an alkyl group, an alkanoyl group, a cyano group or a carboxyl group; R2represents an alkyl group, a carbocyclic group or a heterocyclic group; R3represents a hydrogen atom or one to three substituents; each of R4and R5represents a hydrogen atom, a halogen atom or an alkyl group; R6 represents an alkyl group or an alkoxy group; and ring A represents a heterocyclic diyl group.)
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 417/04 - 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 directly linked by a ring-member-to-ring- member bond
36.
15-OXOSTEROID COMPOUND AND PROCESS FOR PRODUCING THE SAME
Provided is a process for producing a compound, which has an oxo group specifically introduced on the 15-position of a steroid skeleton and which is useful as an intermediate, with a high yield without complicated steps. A compound represented by the formula (2) is allowed to react with an oxidant (e.g., a hypervalent iodine compound) and a co-oxidant (e.g., a peroxide) to produce a 15-oxosteroid compound represented by the formula (1), which is useful as an intermediate: (see formula 1) (see formula 2) wherein Ri to R3 are the same or different and each represent a halogen atom, an alkyl group, a haloalkyl group, an alkoxy group, or a haloalkoxy group, R4 represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an acyl group, or an alkoxycarbonyl group, R5 represents a hydrogen atom, an alkyl group, or an acyl group, R6 represents a hydrogen atom, an alkyl group, an acyl group, or a sulfonyl group, X represents an oxygen atom (O) or a methylene group (CH2).
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
C07J 75/00 - Processes for the preparation of steroids, in general
37.
15-OXOSTEROID COMPOUND AND METHOD FOR PRODUCING SAME
Provided is a method by which a compound, which is useful as an intermediate and in which an oxo group is introduced specifically at the 15-position of a steroid skeleton, can be produced at a high yield without involving a complex procedure. A 15-oxosteroid compound represented by formula (1), which is useful as an intermediate, is produced by reacting a compound represented by formula (2) with an oxidizing agent (a hypervalent iodine compound or the like) and a co-oxidizing agent (a peroxide or the like). (In the formulae: R1 to R3 may be the same as, or different from, each other, and each denote a halogen atom, an alkyl group, a haloalkyl group, an alkoxy group or a haloalkoxy group; R4 denotes a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an acyl group or an alkoxycarbonyl group; R5 denotes a hydrogen atom, an alkyl group or an acyl group; R6 denotes a hydrogen atom, an alkyl group, an acyl group or a sulfonyl group; and X denotes an oxygen atom (O) or a methylene group (CH2).)
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
C07J 75/00 - Processes for the preparation of steroids, in general
38.
CRYSTALLINE POLYMORPH OF 15Β-HYDROXY-OSATERONE ACETATE
Provided is a crystalline polymorph A of 15β-hydroxy-osaterone acetate having improved stabilities (storage stability, pulverization stability, and absorption property). Diffraction peaks characteristic of this crystalline polymorph A of 15β-hydroxy-osaterone acetate, in a powder X-ray diffraction spectrum, appear at diffraction angles 2θ of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorph A has a melting point of 280-283°C, and is a prismatic crystal.
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
Provided is a crystalline polymorph A of 15ß-hydroxy-osaterone acetate having improved stabilities (storage stability, pulverization stability, and absorption property). Diffraction peaks characteristic of this crystalline polymorph A of 15ß-hydroxy-osaterone acetate, in a powder X-ray diffraction spectrum, appear at diffraction angles 2? of 9.6°±0.2°, 17.1°±0.2°, and 20.2°±0.2°. The crystalline polymorph A has a melting point of 280-283°C, and is a prismatic crystal.
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
This formulation has excellent elutability and bioavailability, and contains fenofibrate as an effective component. The formulation comprises spherical porous hydrous silicon dioxide containing fenofibrate supported in a non-crystalline state inside pores. In the formulation, the spherical porous hydrous silicon dioxide has an average particle size of 3 to 12 μm, an average pore diameter of 8 to 16 nm, a pore volume of 0.5 to 3.0 mL/g, and a specific surface area of 400 to 600 m2/g.
A compound represented by formula (1) or salt thereof which has an inhibitory effect on mPGES-1, and is useful as an active ingredient for a medicinal drug for preventing and/or treating a disease such as inflammation, pain, rheumatism, or the like (X represents a carbonyl group or a sulfonyl group; R1 represents a hydrogen atom, a halogen atom, an alkyl group, an alkanoyl group, a cyano group, or a carboxyl group; R2 represents an alkyl group, a carbocyclic group, or a heterocyclic group; R3 represents a hydrogen atom or 1-3 substituents; R4 and R5 represent a hydrogen atom, a halogen atom, or an alkyl group; and R6 represents an alkyl group or an alkoxy group).
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - 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 43/00 - Drugs for specific purposes, not provided for in groups
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 409/04 - 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 directly linked by a ring-member-to-ring- member bond
A compound represented by formula (1) or salt thereof which has an inhibitory effect on mPGES-1, and is useful as an active ingredient for a medicinal drug for preventing and/or treating a disease such as inflammation, pain, rheumatism, or the like (X represents a carbonyl group or a sulfonyl group; R1 represents a hydrogen atom, a halogen atom, an alkyl group, an alkanoyl group, a cyano group, or a carboxyl group; R2 represents an alkyl group, a carbocyclic group, or a heterocyclic group; R3 represents a hydrogen atom or 1-3 substituents; R4 and R5 represent a hydrogen atom, a halogen atom, or an alkyl group; and R6 represents an alkyl group or an alkoxy group).
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/28 - 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 43/00 - Drugs for specific purposes, not provided for in groups
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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 409/04 - 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 directly linked by a ring-member-to-ring- member bond
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
30 - Basic staples, tea, coffee, baked goods and confectionery
Goods & Services
Chemical preparations for use in the manufacture of
pharmaceuticals; industrial chemicals; chemical reagents,
other than for medical or veterinary purposes; chemical
preparations for analyses in laboratories, other than for
medical or veterinary purposes; chemical preparations for
scientific purposes, other than for medical or veterinary
use; agricultural chemicals, except fungicides, herbicides,
insecticides and parasiticides; plant growth regulating
preparations. Pharmaceutical preparations; fumigants; fungicides; rat
poison; insecticides; herbicides; insect repellents;
antiseptics; reagent paper for medical purposes; 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;
breast-nursing pads; cotton swabs for medical use; dental
cements; materials for dental fillings; dental wax;
materials for artificial teeth; dietary supplements for
humans; dietetic beverages adapted for medical purposes;
dietary supplements for animals. Finger guards for medical purposes; pacifiers for babies;
ice bag pillows for medical purposes; supportive bandages;
surgical catgut; feeding cups for medical purposes; dropping
pipettes for medical purposes; teats; ice bags for medical
purposes; babies' bottles; nursing bottles; contraceptives,
non-medical; artificial tympanic membranes; ear plugs for
sleeping; medical apparatus and instruments. Aromatic preparations for food [not from "essential oils"];
tea; coffee; cocoa; spices; cereal preparations; husked
rice; husked oats; husked barley; flour.
The present invention provides a microneedle device comprising a base plate, microneedles arranged on the base plate, and coating layers respectively formed on the microneedles, wherein each of the coating layers contains recombinant follicle stimulating hormone, arginine and glycerin, the mass of arginine is 0.07 to 0.75 time that of recombinant follicle stimulating hormone and the mass of glycerin is 0.1 to 2.75 times that of recombinant follicle stimulating hormone in each of the coating layers.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
46.
NOVEL LEVONORGESTREL CRYSTAL MIXTURE AND PROCESS FOR PRODUCING SAME
A levonorgestrel crystal mixture comprising polymorphic levonorgestrel crystals α which give an X-ray powder diffraction spectrum that has diffraction peaks at the following diffraction angles (α) in terms of 2θ and polymorphic levonorgestrel crystals β which give an X-ray powder diffraction spectrum that has diffraction peaks at the following diffraction angles (β) in terms of 2θ. The ratio (by weight) of the polymorphic crystals α to the polymorphic crystals β, former/latter, may be 5/95 to 90/10. (α): 17.2°±0.2°, 18.6°±0.2°, 22.7°±0.2°, 31.1°±0.2°, and 35.5°±0.2° (β): 13.9°±0.2°, 14.5°±0.2°, 21.3°±0.2°, 24.9°±0.2°, and 28.2°±0.2° This levonorgestrel crystal mixture is useful as emergency contraceptive pills, etc.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I)
3 each independently stands for N or C.
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
C07D 241/38 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
Provided are a new form of levonorgestrel, which is useful as an emergency contraception, etc., a solid dispersion of levonorgestrel, a manufacturing method for the same, and a drug composition. The differential scanning calorimetry spectrum of this amorphous levonorgestrel has an exothermic peak at 51-61℃. This solid dispersion contains levonorgestrel dispersed in an amorphous state in a polymer. Said polymer may be a pharmaceutically acceptable water-soluble polymer. The weight ratio of the polymer to the levonorgestrel may be, in terms of polymer/levonorgestrel, 90/10-50/50.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
Provided are a new crystalline form of levonorgestrel, which is useful as an emergency contraception, etc., a manufacturing method for the same, and a drug composition. The powder X-ray diffraction spectrum of this β crystalline polymorph of levonorgestrel has diffraction peaks where the diffraction angle (2θ) is an angle of 2θ=13.9°±0.2°, 14.5°±0.2°, 21.3°±0.2°, 24.9°±0.2°, and 28.2°±0.2°, and has essentially no diffraction peak at the angle 2θ=18.6°±0.2°.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
Provided are a new crystalline form of levonorgestrel, which is useful as an emergency contraception, etc., a manufacturing method for the same, and a drug composition. The powder X-ray diffraction spectrum of this β crystalline polymorph of levonorgestrel has diffraction peaks where the diffraction angle (2θ) is an angle of 2θ=17.2°±0.2°, 18.6°±0.2°, 22.7°±0.2°, 31.1°±0.2°, and 35.5°±0.2°.
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal.
The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.
A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by dissolving an isopropanol-solvated crystal of ulipristal acetate in a mixed solvent containing ethanol and water, and crystallizing an ulipristal acetate from the solution without addition of a seed crystal to the solution.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A novel form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the ulipristal acetate are provided. An amorphous ulipristal acetate or a novel ulipristal acetate substance containing an amorphous ulipristal acetate is obtained by dissolving a raw ulipristal acetate in a halogenated hydrocarbon and condensing the solution. The amorphous ulipristal acetate may have an exothermic peak at about 135 to 145oC in a differential scanning calorimetry spectrum.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I)
3 each independently stands for N or C.
The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal.
The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.
A heterocyclic compound useful as an antiallergic agent is provided.
A compound represented by the following formula (1) or a salt thereof:
1 is an alkylene group which may have a substituent.
C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
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
C07D 407/08 - 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 carbon chain containing alicyclic rings
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 413/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
Kip1 is provided. The compound or the salt thereof is represented by the following formula (1):
wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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 277/42 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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 405/14 - 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 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 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
The present invention addresses the problem of providing a method for improving the number of sows beginning to nurse or the number of weaning sows, using less expensive components, as well as providing an astaxanthin-containing improving agent for improving the number of sows beginning to nurse or the number of weaning sows, the improving agent being orally administered to impregnated sows in an amount of 10 to 100 mg per day per sow, in terms of astaxanthin, for a time period including days 14 to 35 following impregnation. In addition to the effect of increasing litter size, the improving agent for improving the number of sows beginning to nurse or the number of weaning sows also has the effect of increasing normal litter size as well as the number of sows beginning to nurse or the number of weaning sows. When this improving agent for improving the number of sows beginning to nurse or the number of weaning sows is used, the number of sows beginning to nurse or the number of weaning sows can be increased by approximately 10%.
Provided is a lactam compound or a salt thereof indicated by formula (1), which is a compound with a lactam skeleton or a salt thereof useful as a PPAR activator. [In the formula, the ring Z indicates a condensed hydrocarbon ring or a heterocyclic ring; R1 indicates the same or different halogen atoms, alkyl groups that can have a substituted group, hydroxyl groups, or alkoxy groups that can have a substituted group; R2 indicates an alkylene group that can have a direct bond or a substituted group; R3 indicates a alkoxy group that can have a hydroxyl group or a substituted group; the linker (X) has 1-10 atoms in the main chain selected from carbon atoms and hetero atoms and the main chain can have a substituted group; Y indicates a direct bond, an oxygen atom, or a sulfur atom; and k is an integer between 0 and 5.]
C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
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
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 5/50 - Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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 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
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical or medical products for human use;
biotechnological products for medical purposes, for human
use. Advertising, promotion and retail sale of pharmaceutical,
biotechnological or medical products for human use; bringing
together, for the benefit of others, of pharmaceutical,
biotechnological or medical products for human use
(excluding the transport thereof), enabling the customer to
purchase them conveniently from a wholesaler. Medical services.
This invention provides thienopyrimidine compounds of the formula, (I) wherein R1 stands for hydrogen atom, an alkyl group or the like, and R1 is attached to either A1 or A2; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y-X-; or R2 and R3 may together form tetramethylene group; R4 stands for carboxylic acid, alkylsulfonylaminocarbonyl group or the like; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocycylic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is O or an integer of 1 to 4; one of A1 and A2 stands for carbon atom and the other stands for sulfur atom, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.
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 11/00 - Drugs for disorders of the respiratory system
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
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 43/00 - Drugs for specific purposes, not provided for in groups
63.
HETEROCYCLIC COMPOUND, AND p27 KIP1 DEGRADATION INHIBITOR
Provided are a novel heterocyclic compound and salt thereof applicable in the selective inhibition of the degradation of p27Kip1. The compound and the salt thereof are represented in formula (1). [In the formula: A represents an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group, and group A can have a substituent group; ring B represents a 5- to 8- membered monocyclic heterocyclic ring or a condensed ring containing this monocyclic heterocyclic ring, and ring B can have a substituent group; ring C represents an aromatic ring, and ring C can have a substituent group; L represents a linker having 3-5 atoms in the main chain selected from carbon atoms, nitrogen atoms, oxygen atoms, and sulfur atoms, and having at least one heteroatom selected from nitrogen atoms, oxygen atoms, and sulfur atoms, and linker L can have a substituent group; and n represents 0 or 1.]
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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 31/427 - 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 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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 277/42 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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 405/14 - 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 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 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
A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1) :(formula 1)wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.
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 31/427 - 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 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
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 277/42 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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 405/14 - 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 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 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
Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration.
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 11/00 - Drugs for disorders of the respiratory system
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 25/00 - Drugs for disorders of the nervous system
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
66.
HETEROCYCLIC RING COMPOUND AND H1 RECEPTOR ANTAGONIST
Disclosed is a heterocyclic ring compound which is useful as an anti-allergic agent. Specifically disclosed is a compound represented by formula (1) or a salt thereof. (In the formula, the ring A represents an isocyclic or heterocyclic ring; the ring B represents a heterocyclic ring containing G and a nitrogen atom N as the ring-constituting atoms, wherein G in the ring B represents CH or N; R1 represents a carbonyl group or an alkylene group; R2a and R2b independently represent an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic ring group; X represents an oxygen atom or a sulfur atom; Z represents a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n represents 0 or 1, wherein R1 represents an alkylene group which may have a substituent when the ring A represents a benzene ring or the ring B represents a piperazine ring.)
C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
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 31/4535 - 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 31/454 - 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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 407/08 - 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 carbon chain containing alicyclic rings
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 413/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 417/06 - 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 carbon chain containing only aliphatic carbon atoms
67.
Aqueous composition containing follicle-stimulating hormone and histidine
A stable aqueous composition containing follicle-stimulating hormone, which comprises follicle-stimulating hormone and histidine as a stabilizing agent.
Provided are a solid preparation that can easily regulate the dissolvability of medication, and a method to improve the dissolvability of medication. The disclosed solid preparation (1) is provided with a medication-containing part (2) that contains medication, a gel-forming layer (4) that coats the medication-containing part (2) and forms a gel by absorbing water, and, if necessary, an intermediate layer (3) interposed between the medication-containing part (2) and the gel-forming layer (4). By including a foaming agent (such as sodium bicarbonate) in the medication-containing part (2) and/or the intermediate layer (3), the dissolvability of the medication is improved. The medication-containing part (2) can contain cationic or basic medication, and the gel-forming layer (4) can contain an anionic or acidic polymer. The gel-forming layer (4) can be coated by a surface layer (adhesion prevention layer) (5).
Provided are a solid preparation that can easily regulate the dissolvability of medication, and a method to improve the dissolvability of medication. The disclosed solid preparation (1) is provided with a medication-containing part (2) that contains medication, and a gel-forming layer (4) that coats the medication-containing part (2), with an intermediate layer (3) interposed therebetween, and forms a gel by absorbing water. By forming a plurality of pores (6) in the gel-forming layer (4) extending from the surface thereof to the intermediate layer (3), the dissolvability of the medication is improved. The gel-forming layer (4) can be coated with an adhesion prevention layer (5) and pores (6) can be formed in the adhesion prevention layer (5) extending from the surface thereof and contiguous with the pores in the gel-forming layer (4). The medication-containing part (2) can contain cationic or basic medication, and the gel-forming layer (4) can contain an anionic or acidic polymer.
Disclosed is a method for screening a compound having an activity that selectively modulates an androgen receptor, comprising a step of measuring the mRNA expression level of prostate-specific antigen or the production level of prostate-specific antigen in prostate cancer cells by contacting a test substance with the prostate cancer cells, and a step of measuring the mRNA expression level of uncoupling protein 1 or the production level of uncoupling protein 1 in adipocytes by contacting a test substance with the adipocytes. Additionally disclosed is a selective androgen receptor modulator, comprising as an active ingredient thereof a compound represented by any of structural formulas (I) to (III), and a composition for preventing or treating a lifestyle-related disease, comprising as an active ingredient thereof said selective androgen receptor modulator.
C07D 311/78 - Ring systems having three or more relevant rings
A61K 31/35 - 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
71.
Solid dispersion and pharmaceutical composition of the same, and production processes thereof
A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950° C. for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100 g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier. This invention provides a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) which allows improvement in a solubility and a bioavailability of an active ingredient hardly soluble in water (e.g., a fibrate compound).
Disclosed is a peptide derivative represented by formula: R1N=C(R2)-AA1-AA2-AA3-AA4-Y or a salt thereof, wherein R1 represents a hydrogen molecule or the like; R2 represents a methyl group or the like; Y represents a hydroxyl group; AA1 represents a tyrosine residue or the like; AA2 represents a D-arginine residue or the like; AA3 represents a phenylalanine residue or the like; and AA4 represents a γ-aminobutyric acid residue or the like. By subcutaneously or orally administering the peptide derivative or a salt thereof, an excellent analgesic effect on various kinds of pain is exhibited.
C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07K 5/03 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a delta-amino acid is involved, e.g. isosteres
Disclosed is a solid preparation (1) which comprises: a drug-containing part (2) that contains a cationic drug; a gel-forming layer (4) that contains an anionic polymer and covers the drug-containing part (2), while forming a gel by absorbing water; and if necessary, an intermediate layer (3) that is interposed between the drug-containing part (2) and the gel-forming layer (4). In the solid preparation (1), the dissolvability of a drug is improved by having the drug-containing part (2) and/or the intermediate layer (3) contain an electrolyte (such as calcium chloride). The gel-forming layer (4) may be formed from a carboxyvinyl polymer and a polyvalent metal compound. The gel-forming layer (4) may be covered with a surface layer (adhesion preventing layer) (5).
A gel-forming layer (4) covering a drug-containing part (2) is covered with an adhesion preventing layer (5) by applying an adhesion preventing composition, which contains a water-soluble cellulose ether (such as HPMC) and an anionic polymer (such as a carboxyvinyl polymer), to the gel-forming layer (4), so that a preparation (1) is prevented from adhering to the inner wall of the oral cavity. The gel-forming layer (4) can be formed from a gel-forming agent (a carboxyvinyl polymer), a crosslinking agent, and a base agent (a polyvinyl alcohol or the like). In addition, an adhesive layer (3) may be interposed between the drug-containing part (2) and the gel-forming layer (4).
Disclosed is a solid preparation (1) which comprises: a drug-containing part (2) that contains a cationic drug; a gel-forming layer (4) that contains an anionic polymer and covers the drug-containing part (2), while forming a gel by absorbing water; and if necessary, an intermediate layer (3) that is interposed between the drug-containing part (2) and the gel-forming layer (4). In the solid preparation (1), the dissolvability of a drug is improved by having the drug-containing part (2) and/or the intermediate layer (3) contain an acid component (such as tartaric acid and citric acid). The gel-forming layer (4) may be formed from a carboxyvinyl polymer and a polyvalent metal compound. The gel-forming layer (4) may be covered with a surface layer (adhesion preventing layer) (5).
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
76.
SOLID DISPERSION, PHARMACEUTICAL COMPOSITION COMPRISING THE SOLID DISPERSION, AND PROCESSES FOR PRODUCING THE SOLID DISPERSION AND THE PHARMACEUTICAL COMPOSITION
Disclosed are a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) in both of which the dissolution and bioavailability of an active component poorly soluble in water (e.g., a fibrate compound) can be improved. A powdery porous silicon carrier is impregnated with an active component that is poorly soluble in water and a water-soluble additive component having a 2% nominal viscosity of 500 mPa·s or less at 20˚C to allow the active component and the water-soluble additive component to be carried on the carrier, thereby producing a solid dispersion. The porous silicon carrier may be silicon dioxide or a silicic acid compound, or may be a spherical carrier which shows a loss of weight of 10% by weight or less (particularly 4% by weight or less) when heated at 950˚C for 2 hours. The water-soluble additive component may be selected from a water-soluble polymer, a saccharide and a surfactant. A pharmaceutical composition (e.g., a tablet, a granule, or a capsule) can be prepared using the solid dispersion and a pharmaceutically acceptable carrier.
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
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
The invention provides an aqueous composition comprising follicle-stimulating hormone and a combination of histidine and methionine as a stabilizing agent.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
Disclosed is a stable aqueous composition containing a follicle-stimulating hormone. The aqueous composition comprises the follicle-stimulating hormone and histidine as a stabilizer.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A pharmaceutical composition comprising a suspension of medicinally-active ingredient microparticles having a mean particle diameter of 20 μm or smaller in a base oil which can achieve extremely high intestinal absorption and bioavailability especially when the medicinally-active ingredient is hardly water-soluble.
Provided is a prophylactic and/or therapeutic agent which improves abnormalities of intestinal function in the form of abdominal pain, diarrhoea or constipation, and is useful for preventing or treating functional gastrointestinal disorders. The prophylactic and/or therapeutic agent for functional gastrointestinal disorders contains rifaximin as an active ingredient. Functional gastrointestinal disorders include conditions such as functional oesophageal disorders, functional gastroduodenal disorders (for example, functional dyspepsia), functional intestinal disorders (for example, functional abdominal distension and functional diarrhoea), functional abdominal pain syndrome, gall bladder dysfunction and sphincter of Oddi dysfunction, functional anorectal disorders (for example, functional incontinence, functional anorectal pain and functional defecation disorders), neonatal and paediatric functional disorders (for example, paediatric functional diarrhoea), and functional disorders of infancy and adolescence (for example, paediatric functional abdominal pain and paediatric nonconservative incontinence).
A61K 31/439 - 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 the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I)
3 each independently stands for N or C.
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
82.
AGENT FOR IMPARTING TOLERANCE FOR THE MINIMUM SURVIVAL TEMPERATURE OF FISH AND FISH FARMING METHOD
To impart tolerance for the minimum survival temperature of fish or crustaceans. Provided are an agent for imparting tolerance for the minimum survival temperature of fish or crustaceans, which contains arginine, and a method for farming fish or crustaceans characterized by comprising feeding the fish or crustaceans with arginine.
The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I)
1-6 alkoxy; and n is an integer of 1-3.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
This invention offers isoxazole derivatives represented by the following formula (I)
or pharmaceutically acceptable salts thereof which exhibit excellent p38MAPkinase-inhibiting action with reduced side-effects, and are useful for treating such diseases as chronic rheumatoid arthritis, ulcerative colitis and the like.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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
85.
PROPHYLACTIC/THERAPEUTIC AGENT FOR LIFESTYLE-RELATED DISEASES
Disclosed is a method for the screening of a compound having an activity to selectively modulate an androgen receptor. The method comprises the steps of: contacting a substance to be tested with a prostate cancer cell and measuring the level of expression of mRNA for a prostate-specific antigen or the level of production of the prostate-specific antigen in the prostate cancer cell; and contacting the substance with an adipocyte and measuring the level of expression of mRNA for uncoupling protein-1 or the level of production of uncoupling protein-1 in the adipocyte. Also disclosed is a selective androgen receptor modulator comprising a compound represented by any one formula selected from the structural formulae (I) to (III) as an active ingredient. Further disclosed is a composition for preventing or treating lifestyle-related diseases, which comprises the selective androgen receptor modulator.
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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 43/00 - Drugs for specific purposes, not provided for in groups
C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950.degree.C for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier. This invention provides a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) which allows improvement in a solubility and a bioavailability of an active ingredient hardly soluble in water (e.g., a fibrate compound).
A process for the production of a solid dispersion which comprises impregnating, without treatment with a supercritical fluid, a powdered porous carrier containing a porous siliceous carrier (for example, spherical siliceous carrier such as spherical porous silica) which exhibits a weight loss of 4wt% or below when heated at 950°C for 2 hours with an organic solvent solution of a slightly water-soluble active ingredient, and then removing the organic solvent from the resulting system to form a solid dispersion comprising the porous carrier and the active ingredient supported thereon. The porous siliceous carrier may be spherical silica having a mean pore diameter of 10 to 40nm and an oil absorption of 175 to 500ml/100g. Pharmaceutical compositions (such as tablets, granules and capsules) can be prepared by using the solid dispersion and pharmaceutically acceptable carriers. The solid dispersion and the pharmaceutical compositions (or pharmaceutical preparations) bring about improvement in the dissolution and bioavailability of slightly water-soluble active ingredients (such as fibrate compounds).
This invention provides thienopyrimidine derivatives of the formula,
or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical or medical products for human use;
biotechnological products for medical use, for human use. Advertising, promotion and retail sale of pharmaceutical,
biotechnological or medical products for human use;
grouping, for the benefit of others, pharmaceutical,
biotechnological or medical products for human use
(excluding their transport) enabling consumers to purchase
them conveniently from a wholesaler. Medical services.
90.
LACTAM COMPOUND OR SALT THEREOF, AND PPAR ACTIVATOR
Disclosed is a compound having a lactam skeleton or a salt thereof, which is useful as a PPAR activator. Specifically disclosed is a lactam compound represented by formula (1) or a salt thereof. (1) wherein R1 represents a halogen, a hydrocarbon group, a carboxyl group or the like; Z1 represents an arene ring or a hetero ring; Z3 represents an alicyclic or aromatic hydrocarbon ring; Z2 represents a 5- to 6-membered ring containing a nitrogen atom; X1 represents a C, O, S or N atom, a group -N-C(=O)- or a group -C(=O)-N-; R2 represents a hydrogen atom or an alkyl group which may have a substituent; R3 and R4 independently represents a single bond or a bivalent aliphatic hydrocarbon group, provided that at least one of R3 and R4 represents an aliphatic hydrocarbon group; X2 and X3 independently represent a single bond, an O or S atom, an imino group or the like; A1 represents a single bond or a phenylene group which may have a substituent; Y1 represents a hydrogen atom, a halogen atom, a carboxyl group or the like; a represents an integer of 0 to 5; b represents an integer of 0 to 2; and c represents an integer of 1 to 3.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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 43/00 - Drugs for specific purposes, not provided for in groups
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 409/10 - 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 aromatic rings
91.
PHARMACEUTICAL COMPOSITION CONTAINING FINE PARTICLE OIL-BASED SUSPENSION
Disclosed is a pharmaceutical composition containing a base-in-water suspension of particles of a pharmaceutically active ingredient component having an average particle diameter of not more than 20 &mgr;m. This pharmaceutical composition enables to attain extremely high intestinal absorption and biological availability of the pharmaceutically active ingredient, particularly when the pharmaceutically active ingredient is poorly water-soluble.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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 1/04 - 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
Disclosed is a pharmaceutical composition containing a base-in-water suspension of particles of a pharmaceutically active ingredient component having an average particle diameter of not more than 20 .mu.m. This pharmaceutical composition enables to attain extremely high intestinal absorption and biological availability of the pharmaceutically active ingredient, particularly when the pharmaceutically active ingredient is poorly water-soluble.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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
Disclosed is a therapeutic agent for difficulty in urination associated with overactive bladder, frequent urination, urinary incontinence or prostatomegaly or urinary calculus, which comprises a compound having a PDE9-inhibiting activity as an active ingredient.
Disclosed is a quinoxaline derivative represented by the formula (I) below, which has PDE 9 inhibitory activity and is useful as an agent for treatment of dysuria or the like, or a salt of such a quinoxaline derivative. In the formula, R1 and R2 independently represent a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an acyl group, an amino group or the like; R3 represents an alkyl group, an aryl group, a saturated carbocyclic group, a saturated heterocyclic group, an acyl group or the like; R4 represents a hydrogen atom, a hydroxy group, an alkyl group or an amino group; R5 and R8 independently represent a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, an alkoxy group, a cyano group or a nitro group; R6 and R7 independently represent a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a cyano group, an amino group, a carbocyclic group, a heterocyclic group, COR9 or SO2R9; R9 represents a hydrogen atom, a hydroxy group, an alkyl group, an amino group, a pyrrolidin-1-yl group, a piperidin-1-yl group, a piperazin-1-yl group or the like; X represents S or O; and A1, A2 and A3 independently represent N or C.
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 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 25/00 - Drugs for disorders of the nervous system
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
The invention discloses isoxazole derivatives represented by a formula,
3)—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof, which have excellent p38MAPkinase inhibitory action.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
An aromatic amine compound (I) having an amino group at Position-2 and a halogen atom, a nitro group or the like at Position-1 is reacted with an O-alkyl dithiocarbonate to produce a corresponding 2-mercaptobenzothiazole compound (II). The compound (II) is reacted with a metal component to produce a benzothiazole compound (III) having a hydrogen atom at Position-2. The compound (III) is reacted with a base to produce a corresponding 2-aminothiophenol compound or a salt thereof. The 2-aminothiophenol compound is useful as a raw material or intermediate for the synthesis of a benzothiazole compound having an organic group at Position-2 which is useful as an aldose reductase inhibitor, or the like. It becomes possible to produce the benzothiazole compound with efficiency and in a simple manner.
C07C 319/06 - Preparation of thiols, sulfides, hydropolysulfides or polysulfides of thiols from sulfides, hydropolysulfides or polysulfides
C07C 323/34 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton having at least one of the nitrogen atoms bound to a carbon atom of the same non-condensed six-membered aromatic ring the thio group being a mercapto group
A quinazoline derivative represented by the formula (I) or a salt thereof, which has a PDE9-inhibiting activity and is useful as a therapeutic agent for dysuria or the like. (I) wherein R1 represents a phenyl or aromatic heterocyclic group which may be substituted by 1 to 3 substituents selected from a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group having 1 to 6 halogen atoms and a C1-6 alkoxy group; and n represents an integer ranging from 1 to 3.
C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 11/00 - Drugs for disorders of the respiratory system
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/04 - Drugs for disorders of the urinary system for urolithiasis
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 25/00 - Drugs for disorders of the nervous system
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 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
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
98.
DRUG FORMULATION CONTAINING FIBRATE MEDICAMENT AND PROCESS FOR PRODUCING THE SAME
Drug formulations (pharmaceutical compositions) for lowering of the blood concentration of free fatty acids and/or fibrinogen, comprising a statin medicament composed at least of a statin compound having benzopyridine skeleton (pitavastatin, etc.) and a fibrate medicament (phenofibrate, etc.). These drug formulations are useful as a preventive or therapeutic agent for hyper-free fatty acidemia, metabolic syndrome, type II diabetes, etc.
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
