The purpose of the present invention is to provide a method for producing a lyophilized preparation containing 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof and having uniform quality, which can be scaled up. A method for producing a lyophilized preparation containing an amorphia of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide sodium salt according to the present invention is useful as a method for producing a lyophilized preparation having uniform quality.
This tablet contains, (1) tosufloxacin tosilate, (2) a binder, and (3) an acidic amino acid. The tablet contains one or more types of binder selected from water-soluble polyvinyl polymers and gelatins, and is useful as a tablet containing tosufloxacin tosilate that exhibits rapid dissolution, is not subject to tableting problems, and can be manufactured stably.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
This tablet containing (1) tosufloxacin tosilate, (2) disintegrator and (3) acidic amino acid is useful as a tablet containing tosufloxacin tosilate that dissolves rapidly, improves drug compliance in children, and has excellent storage stability.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
Provided are: a novel method for producing a hydroxamic acid derivative, which uses, as an intermediate, a compound represented by general formula [12] (wherein R1 represents a methyl group, etc.; R2 represents a methyl group, etc.; and R5 represents a hydrogen atom, etc.); and said intermediate.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 27/02 - Saponification of organic acid esters
C07C 33/26 - Polyhydroxylic alcohols containing only six-membered aromatic rings as cyclic part
C07D 317/12 - Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
5.
METHOD FOR PRODUCING 5-(BROMOMETHYL)-1-BENZOTHIOPHENE
Provided is a method for industrially producing 5-(bromomethyl)-1-benzothiophene. The production method according to the present invention comprises: (1) a step for introducing 5-methyl-1-benzothiophene, a brominating agent, and a solvent into a reactor; (2) a step for emitting light having a wavelength range of 200-780 nm inside the reactor; and (3) a step for recovering 5-(bromomethyl)-1-benzothiophene from the reactor.
C07D 333/54 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
6.
CRYSTALS OF NOVEL HYDROXAMIC ACID DERIVATIVE, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION
Crystals of (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide having diffraction peaks at diffraction angles (2θ) of 3.8±0.2°, 7.7±0.2°, and 10.8±0.2°, and the like or 8.2±0.2°, 12.4±0.2°, and 13.3±0.2°, and the like in powder x-ray diffraction, a method for producing the same, and a pharmaceutical composition.
C07C 239/08 - Hydroxylamino compounds or their ethers or esters
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A therapeutic method whereby it becomes possible to reduce adverse side effects and the QOL of a patient can be improved while exerting a therapeutic effect on pain has been demanded. When N-[7-[(methylsulfonyl)amino]-4-oxo-6-phenoxy-4H-1- benzopyran-3-yl]formamide is administered for a certain period and subsequently a washout period is provided, a therapeutic effect on pain can also be exerted in the washout period and adverse side effects can be reduced or eliminated. This is useful as a therapeutic method for pain.
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
8.
TABLET COMPRISING 1-(3-(2-(1-BENZOTHIOPHEN-5-YL)ETHOXY)PROPYL)AZETIDIN-3-OL OR SALT THEREOF
A tablet which comprises (1) 1-(3-(2-(1-benzothiophen-5- yl)ethoxy)propyl)azetidin-3-ol or a salt thereof and (2) ethyl cellulose, said tablet having excellent elution properties and good moldability, remaining stable during prolonged storage, and exhibiting high impact resistance.
Provided is a medicinal composition characterized by comprising an alkyl ether derivative represented by general formula [1]
3 represents an optionally protected hydroxyl group, etc.; and m and n are the same or different and represent an integer of 1 to 6] or a salt thereof. The medicinal composition according to the present invention is useful as a post nerve injury rehabilitation effect-enhancing agent.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
PUBLIC UNIVERSITY CORPORATION NAGOYA CITY UNIVERSITY (Japan)
Inventor
Shimane Kazuki
Tanaka Yasuhito
Abstract
An anti-hepatitis B virus agent comprising a compound represented by general formula [1] (wherein R1 represents an aryl group which may be substituted or the like; R2 represents an aryl group which may be substituted or the like; and R3 represents a hydrogen atom or the like) or a salt thereof.
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 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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
Crystals of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid having diffraction peaks at diffraction angles (2θ) of １２．２±０．２、１７．２±０．２、１９．４±０．２、２４．１±０．２, and ２７．１±０．２° or diffraction angles (2θ) of １２．９±０．２、１５．５±０．２、２１．２±０．２、２１．７±０．２, and ２５．９±０．２° in powder x-ray diffraction have excellent stability, are easy to handle, and are useful as a drug substance of pharmaceuticals to be used in treatments such as the prevention or treatment of diseases involving keratinocyte hyperproliferation.
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
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
Provided is a prevention or treatment agent for cerebral amyloid beta storage diseases, that contains a substance capable of suppressing the progression, alleviating the symptoms, and improving cerebral amyloid beta storage diseases. This prevention or treatment agent for cerebral amyloid beta storage diseases has as an effective component thereof a compound (e.g., Iguratimod) indicated by formula (1) or a salt thereof and, as a result, is capable of preventing or treating cerebral amyloid beta storage diseases such as Alzheimer-type dementia or cerebral amyloid angiopathy.
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A compound represented by the general formula, or a salt thereof, has exceptional CXCL10 inhibitory activity and is useful as a treatment agent for the prevention and/or treatment, etc., of diseases involving overproduction of CXCL10. In the formula: R1 is a C1-6 alkyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a halogen atom, etc.; Z1, Z2, and Z3 are CH, etc.; X1 is CONH, etc.; ring A is a phenyl group, etc.; R4 is a halogen atom, etc.; and m is an integer of 0-5.
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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 215/42 - Nitrogen atoms attached in position 4
C07D 215/48 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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 401/06 - 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 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - 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
Provided is a sigma-receptor binding agent that is characterized by containing an alkyl ether derivative represented by general formula [1] or a salt thereof. (In the formula, R1 and R2 are the same or different and indicate a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, or the like, R3 indicates an optionally protected hydroxyl group or the like, and m and n are the same or different and each indicate an integer from 1 to 6.)
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
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 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 21/02 - Muscle relaxants, e.g. for tetanus or cramps
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 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 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
The purpose of the present invention is to provide a method for producing 6-bromo-3-hydroxy-2-pyrazinecarboxamide in which the content of impurities is reduced. This production method includes a step of obtaining a 6-bromo-3-hydroxy-2-pyrazinecarboxamide crystal having diffraction angles expressed in degrees 2θ of 5.5, 20.1, 23.7, 26.7, 27.5, and 28.1° and/or diffraction angles expressed in degrees 2θ of 7.1, 21.4, 25.2, 25.7, 27.1, and 28.8° in an X-ray powder diffraction.
A method for treating the relapsing-remitting or secondary progressive multiple sclerosis at the time of relapse, by administering a benzopyran derivative of the following formula or a salt thereof,
3 represents a hydrogen atom, an optionally substituted amino group, an optionally substituted acylamino group, an optionally substituted carbamoyl group or an optionally substituted aryl group.
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
C07D 311/24 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 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 in position 2
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
18.
METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF EBOLA VIRUS DISEASE
INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) (France)
UNIVERSITÉ DE BORDEAUX (France)
CHU DE BORDEAUX (France)
TOYAMA CHEMICAL CO., LTD (Japan)
Inventor
Malvy, Denis
Abstract
The invention relates to methods and pharmaceutical compositions for the treatment of Ebola Virus Disease. In particular the present relates to a method of treating Ebola Virus Disease in a subject in need thereof comprising administering the subject with a therapeutically effective amount of Favipiravir.
Pharmacological compositions containing a hydroxamic acid derivative selected from (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide, (2S)-2-((4-((4-((1R)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide, and (2S)-N-hydroxy-2-((4-((4-((1S)-1-hydroxy-2-methoxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N',2-dimethylmalonamide, or a salt of said derivatives, and an antibiotic substance are useful in the treatment of gram-negative bacterial infections.
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61K 31/407 - 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 condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
This pharmaceutical composition contains a hydroxamic acid derivative, or a salt thereof, and a solubilizer, said hydroxamic acid derivative being selected from among (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N’,2-dimethylmalonamide, (2S)-2-((4-((4-((1R)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N’,2-dimethylmalonamide, and (2S)-N-hydroxy-2-((4-((4-((1S)-1-hydroxy-2-methoxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N’,2-dimethylmalonamide. The pharmaceutical composition demonstrates strong antibacterial activity, has excellent solubility in water, and is useful as a drug.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 atoms
A novel amine derivative expressed by general formula (1)
4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation.
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 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/04 - 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
C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles 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 in position 2
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 277/68 - Benzothiazoles 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 in position 2
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/428 - Thiazoles condensed with carbocyclic 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 31/4439 - 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 31/454 - 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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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 235/08 - Radicals containing only hydrogen and carbon atoms
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 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 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
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 209/12 - Radicals substituted by oxygen atoms
C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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 407/14 - 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 three or more hetero rings
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 413/10 - 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 aromatic rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
23.
GRANULAR SOLID FORMULATION CONTAINING CEPHALOSPORIN ESTER, AND METHOD FOR PRODUCING SAME
A granular solid formulation containing drug granules that contain (1) a core substance and (2) a drug-containing layer covering the core substance, wherein a granular solid formulation in which the drug-containing layer contains a cephalosporin ester and a heat-meltable substance, the content ratio of heat-meltable substance is 10-20% relative to the mass of the drug granules, and the content ratio of cephalosporin ester is 20-40% relative to the mass of the granular solid formulation has a high drug content, exceptional stability and elutability, and reduced bitterness, and is useful as a formulation that improves compliance in children and/or the elderly.
A61K 31/545 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
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
Provided is a prevention or treatment agent for cerebral amyloid beta storage diseases, that contains a substance capable of suppressing the progression, alleviating the symptoms, and improving cerebral amyloid beta storage diseases. This prevention or treatment agent for cerebral amyloid beta storage diseases has as an effective component thereof a compound (e.g., Iguratimod) indicated by formula (1) or a salt thereof and, as a result, is capable of preventing or treating cerebral amyloid beta storage diseases such as Alzheimer-type dementia or cerebral amyloid angiopathy.
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61P 9/00 - Drugs for disorders of the cardiovascular 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
Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 323/62 - 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 carboxyl 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
C07D 305/06 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 317/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 263/14 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals substituted by oxygen atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 207/10 - 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 no 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 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07C 233/83 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 271/28 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
C07C 323/41 - Y being a hydrogen or an acyclic carbon atom
C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/327 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/12 - Radicals substituted by oxygen atoms
C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07D 211/18 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
C07D 213/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 215/14 - Radicals substituted by oxygen atoms
C07D 217/12 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/56 - BenzoxazolesHydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 265/38 - [b, e]-condensed with two six-membered rings
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
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 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/66 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
C07D 295/12 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
C07D 295/14 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 atoms
C07D 307/18 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 309/04 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 309/14 - Nitrogen atoms not forming part of a nitro radical
C07D 317/60 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 319/20 - 1,4-DioxanesHydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring with substituents attached to the hetero ring
C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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
C07C 235/84 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 237/36 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 309/30 - Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
Provided is a medicinal composition characterized by comprising an alkyl ether derivative represented by general formula [1] [wherein: R1 and R2 are the same or different and represent a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, etc.; R3 represents an optionally protected hydroxyl group, etc.; and m and n are the same or different and represent an integer of 1 to 6] or a salt thereof. The medicinal composition according to the present invention is useful as a post nerve injury rehabilitation effect-enhancing agent.
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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
27.
Method for improving therapy for autoimmune diseases such as rheumatoid arthritis
In the present invention, a method using a combination of iguratimod or a salt thereof and one or more immunosuppressants is useful as a method for the treatment of autoimmune diseases, and with this method adverse effects are lessened. A pharmaceutical composition containing this combination is useful for the treatment of autoimmune diseases. This method and pharmaceutical composition are useful for the treatment of more severe autoimmune diseases.
A01N 45/00 - Biocides, pest repellants or attractants, or plant growth regulators containing compounds having three or more carbocyclic rings condensed among themselves, at least one ring not being a six-membered ring
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
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
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
A compound represented by general formula (1) [wherein R1 and R2 independently represent a C1-6 alkyl group or the like; R3 represents a hydrogen atom or the like; R4A represents an aryl group which may be substituted, a heterocyclic group which may be substituted or the like; R5 and R6 independently represent a C1-6 alkyl group or the like; X1 represents a methylene group or the like; and Z1 and Z2 independently represent CH or the like] or a salt thereof is useful as an anti-fungal agent.
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
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
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
29.
Solid pharmaceutical composition containing 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salt thereof
This solid pharmaceutical composition is useful as a solid pharmaceutical composition of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol, which is excellently elutable and moldable and is stable in long-term storage, or a salt thereof.
C07D 205/00 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
C07D 333/00 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
C07D 333/56 - Radicals substituted by oxygen atoms
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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
A preparation replete with crystals of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
A benzopyran derivative represented by general formula [1], or a salt thereof, is useful in therapeutic or preventive treatment of disease, wherein said therapeutic or preventive treatment is effective because said benzopyran derivative, or salt thereof, binds to MIF, has an MIF inhibitory effect, and inhibits MIF. [In the formula, R1 represents an optionally substituted C1-6 alkyl group, one of R2 and R3 represents a hydrogen atom, and the other of R2 and R3 represents a hydrogen atom, an optionally substitutedamino group, an optionally substituted acylamino group, an optionally substituted carbamoyl group, or an optionally substitutedaryl group.]
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
C07D 311/24 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 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 in position 2
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
33.
THERAPEUTIC AGENT FOR DISEASE BASED ON INHIBITORY EFFECT OF MACROPHAGE MIGRATION INHIBITORY FACTOR
A benzopyran derivative represented by general formula [1], or a salt thereof, is useful in therapeutic or preventive treatment of disease, wherein said therapeutic or preventive treatment is effective because said benzopyran derivative, or salt thereof, binds to MIF, has an MIF inhibitory effect, and inhibits MIF. [In the formula, R1 represents an optionally substituted C1-6 alkyl group, one of R2 and R3 represents a hydrogen atom, and the other of R2 and R3 represents a hydrogen atom, an optionally substituted amino group, an optionally substituted acylamino group, an optionally substituted carbamoyl group, or an optionally substituted aryl group.]
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
C07D 311/24 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 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 in position 2
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
34.
THERAPEUTIC AGENT FOR PULMONARY HYPERTENSION, WHICH CONTAINS BENZOPHENONE DERIVATIVE OR SALT THEREOF
A method using a benzophenone derivative represented by general formula (AA) or a salt thereof and a pharmaceutical composition containing the benzophenone derivative or a salt thereof are useful for the treatment or prophylaxis of pulmonary hypertension or heart failure. (In the formula, R1 represents an optionally substituted heterocyclic group, a substituted phenyl group or the like; Z represents an alkylene group or the like; R2 represents a carboxyl group which may be protected by an alkyl group, or the like; R3 represents an optionally protected hydroxyl group or the like; R4 represents an optionally substituted cycloalkyloxy group or the like; and R5 represents a hydrogen atom or the like.)
A compound represented by general formula (1) (wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; R2 represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group; R4 represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; X1 represents an optionally substituted C2-6 alkynylene group or the like; A represents an optionally substituted bivalent aromatic hydrocarbon group or the like; X2 represents an optionally substituted C1-6 alkylene group or the like; Y1 represents an oxygen atom or the like; and R5 represents a hydrogen atom or the like) or a salt thereof is useful as an antibacterial agent.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A compound that can be represented by general formula or a salt of such a compound is useful as an antifungal agent. (In the formula, R1 and R2 may be the same as or different from each other and each represent a halogen atom, a C1-6 alkyl group that may be substituted, or the like; R3 represents an indanyl group that may be substituted, an indenyl group that may be substituted, a dihydronaphthyl group that may be substituted, a tetrahydronaphthyl group that may be substituted, or the like; R4 and R5 may be the same as or different from each other and each represent a hydrogen atom, a C1-6 alkyl group that may be substituted, or the like; X1 represents a C1-6 alkylene group or the like; Z1 and Z2 may be the same as or different from each other and each represent a nitrogen atom, the group represented by the formula CH, or the like; and Z3 represents a nitrogen atom, the group represented by the formula CH, or the like.)
A novel amine derivative expressed by general formula (1) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents -COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation.
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/428 - Thiazoles condensed with carbocyclic 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 31/4439 - 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 31/454 - 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 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles 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 in position 2
C07D 277/68 - Benzothiazoles 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 in position 2
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 401/06 - 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 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 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 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/04 - 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
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
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
The compound represented by formula (1) or a salt thereof has a collagen production-inhibiting effect, and is thus useful for use in the prevention, treatment, or the like of diseases associated with overproduction of collagen such as pulmonary fibrosis, scleroderma, nephrosclerosis, and cirrhosis. In formula (1): R1 represents an aryl group or the like that may be substituted with one or more groups selected from the substituent group (α); one of R2 or R3 represents a group represented by the formula -X1-R6 (in the formula, X1 represents an oxygen atom, a bond, or the like, and R6 represents an aryl group of the like that may be substituted; the other of R2 or R3 represents a hydrogen atom or a halogen atom; Z1 and Z2 may be identical or different, and represent either a nitrogen atom or the group represented by the formula C-R7 (in the formula, R7 represents a hydrogen atom or a halogen atom); and Y represents -N=N-, -S(O)-O-, -C(O)-O-, -C(O)-S-, or -C(S)-O- (wherein the bond to the left of each group is a bond that bonds to NH).
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
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 31/454 - 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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
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
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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 11/00 - Drugs for disorders of the respiratory system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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 413/10 - 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 aromatic rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
39.
DEUTERATED NITROGENATED HETEROCYCLIC CARBOXAMIDE DERIVATIVE OR SALT THEREOF
A deuterated nitrogenated heterocyclic carboxamide derivative represented by general formula [1] (wherein D represents a deuterium atom; and X represents a halogen atom) or a salt thereof, which exhibits excellent pharmacokinetics including the maintenance of the metabolic rate at a low level and the maintenance of the concentration in the blood at a high level in blood and the like, and is therefore useful as an anti-viral agent.
This deuterated nitrogen-containing heterocyclic carboxamide derivative represented by general formula (1) (in the formula, D represents a deuterium atom, and R represents a hydrogen atom or deuterium atom), or a salt thereof, exhibits excellent pharmacokinetics, such as maintenance of a high blood concentration and/or increase in AUC, and is useful as an antiviral agent.
This solid pharmaceutical composition is useful as a solid pharmaceutical composition of 1-(3-(2-(1-benzothiophen-5-yl) ethoxy) propyl) azetidin-3-ol, which is excellently elutable and moldable and is stable in long-term storage, or a salt thereof.
A61P 25/00 - Drugs for disorders of the nervous system
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
A heterocyclic compound represented by the general formula (in the formula, R1, R2 and R3 may be the same or different, and each represents a hydrogen atom, a halogen atom, or this general formula (X1-Y1-R4) (in the formula: X1 represents this general formula (NR5) (in the formula, R5 represents a hydrogen atom, etc.) or the like; Y1 represents an optionally substituted C1-6 alkylene group or the like; and R4 represents an optionally substituted aryl group or the like), and Z represents a nitrogen atom or this general formula (CR6) (in the formula, R6 represents a hydrogen atom, a halogen atom, or an optionally substituted C1-12 alkyl group or the like)), or a salt thereof, exhibits excellent anti-HIV activity and is useful as an anti-HIV agent.
(1) A tablet according to the present invention has a percentage content of 1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2, 3-dihydro-1H-isoindole-5-yl]-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid methanesulfonic acid hydrate of between 80 wt% and 97.5 wt%. (2) The tablet is smaller in size than 200mg of a commercially available Geninax tablet. (3) As a result, drug compliance is improved, (4) leachability is high, and (5) hardness and friability are high. (6) As a result, the present invention withstands film coating and transportation, and is useful as a tablet of methanesulfonic acid hydrate of chemical compound A.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 323/62 - 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 carboxyl 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
C07D 305/06 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 317/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 263/14 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals substituted by oxygen atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 271/28 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 317/44 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
C07C 323/41 - Y being a hydrogen or an acyclic carbon atom
C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/327 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/12 - Radicals substituted by oxygen atoms
C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07D 211/18 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
C07D 213/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 215/14 - Radicals substituted by oxygen atoms
C07D 217/12 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/56 - BenzoxazolesHydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 265/38 - [b, e]-condensed with two six-membered rings
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
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 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/66 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
C07D 295/12 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
C07D 295/14 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 atoms
C07D 307/18 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 309/04 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 309/14 - Nitrogen atoms not forming part of a nitro radical
C07D 317/60 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 319/20 - 1,4-DioxanesHydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring with substituents attached to the hetero ring
C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 207/10 - 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 no 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 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A compound represented by general formula or a salt thereof is useful as an antifungal agent. (In the formula, R1 and R2 may be the same or different and each represents a halogen atom, a cyano group, a nitro group, an optionally substituted C1-6 alkyl group or the like; R3 represents an optionally substituted pyridyl group, an optionally substituted monocyclic oxygen-containing heterocyclic group or the like; R4 and R5 may be the same or different and each represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; X1 represents an optionally substituted 1,2-ethylene group, an optionally substituted 1,3-propylene group or the like; X2 represents an oxygen atom, a sulfur atom, a methylene group or the like; and Z1 and Z2 may be the same or different and each represents a nitrogen atom or a group that is represented by formula CH.)
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
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 31/454 - 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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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 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
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
46.
METHOD FOR IMPROVING THERAPY FOR AUTOIMMUNE DISEASES SUCH AS RHEUMATOID ARTHRITIS
In the present invention, a method using a combination of iguratimod or a salt thereof and one or more immunosuppressants is useful as a method for the treatment of autoimmune diseases, and with this method adverse effects are lessened. A pharmaceutical composition containing this combination is useful for the treatment of autoimmune diseases. This method and pharmaceutical composition are useful for the treatment of more severe autoimmune diseases.
A61K 31/352 - 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 condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent. A compound represented by formula (I) (wherein A1 represents a nitrogen atom or a group represented by formula CR6; A2 and A3 are the same as or different from each other and independently represent a nitrogen atom or a group represented by formula CH; R1 represents an aryl group which may be substituted by 1 to 5 substituents independently selected from a substituent group (2) or the like; R2 and R3 are the same as or different from each other and independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 haloalkyl group or a C1-6 alkoxy group; and R4 and R5 are the same as or different from each other and independently represent a hydrogen atom, a C1-6 haloalkyl group, a C1-6 alkyl group or the like) or a salt thereof is useful as an anti-fungal agent.
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 31/454 - 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/48 - Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
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
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
The object of the present invention is to provide a compound useful as an intermediate for the production of a pyrazinecarboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazinecarboxamide. The present invention provides a pyrazino[2,3-d]isooxazole derivative represented by general formula (I) (wherein X represents a halogen atom, a hydroxy group or a sulfamoyloxy group; and Y represents -C(=O)R or -CN (wherein R represents a hydrogen atom, an alkoxy group, an aryloxy group, an alkyl group, an aryl group or an amino group)).
C07C 239/18 - Hydroxylamino compounds or their ethers or esters having nitrogen atoms of hydroxylamino groups further bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 261/18 - Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
This process is characterized by reacting a salicylaldehyde derivative with an orthoacetic acid ester in the presence of a base, has advantageous features including the features (1) to (5) mentioned below, and is therefore useful: (1) raw materials are inexpensive; (2) any high-temperature reaction is not required; (3) the number of steps required for the production is few; (4) the desired product can be produced in high yield; and (5) the process is applicable to salicylaldehyde derivatives having various types of substituents.
C07D 311/10 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring unsubstituted
C07D 311/14 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 6 and unsubstituted in position 7
50.
MEGLUMINE SALT OF 6-FLUORO-3-HYDROXY-2-PYRAZINE CARBOXAMIDE
A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
A preparation replete with crystals of a sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
Disclosed is a safe, transdermal absorption preparation useful in the treatment of fungal infections, having excellent skin permeability and strong antifungal activity, and greatly contributing to a patient's quality of life. The disclosed transdermal absorption preparation contains 4-{3-[4-(3-{4-[amino (imino) methyl] phenoxy} propyl)-1-piperidinyl] propoxy} benzamidine, or a salt thereof, and a transdermal absorption enhancer.
Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation.
Disclosed is a medicament having a strong antibacterial activity against Gram-positive bacteria, Gram-negative bacteria, and resistant bacteria. A compound represented by formula [I] or a salt thereof is useful as an antibacterial agent. In formula [I], a bond containing a dotted line and connecting X2 to Y1 represents a single bond or a double bond; Z1, Z2, Z3, Z4, Z5, and Z6 each represent a nitrogen atom, formula: CH, or the like; X1 represents a C1-4 alkylene group which may be substituted by an oxo group; X2 represents a bonding hand or formula: CH; Y1 represents a spirocyclic group selected from a group of formulae (II); X3 represents a C1-4 alkylene group, formula: NR10(CH2)m, formula: SOn, or a bonding hand; and R7 represents a C3-6 cycloalkyl group, a C3-6 cycloalkenyl group, an aryl group, a monocyclic heterocyclic group, a bicyclic heterocyclic group, or the like.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/438 - 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 being spiro-condensed with carbocyclic or heterocyclic ring systems
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 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
Provided is a novel compound that is useful as a medical drug in that said compound displays strong antimicrobial activity against gram-negative bacteria such as Pseudomonas aeruginosa and drug-resistant strains thereof, on the basis of LpxC-inhibiting activity. The novel compound is a hydroxamic acid derivative represented by general formula 1 (1) or a pharmaceutically acceptable salt thereof.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
A61K 31/407 - 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 condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
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 31/438 - 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 being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07C 323/62 - 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 carboxyl 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
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 205/12 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
C07D 207/10 - 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 no 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 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
C07D 207/327 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 209/12 - Radicals substituted by oxygen atoms
C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
C07D 209/52 - Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/18 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 211/70 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
C07D 213/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 215/14 - Radicals substituted by oxygen atoms
C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 217/12 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/14 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals substituted by oxygen atoms
C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/56 - BenzoxazolesHydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 265/38 - [b, e]-condensed with two six-membered rings
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/66 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 295/12 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
C07D 295/14 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 295/16 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
C07D 305/06 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 atoms
C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 307/18 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 309/04 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 309/14 - Nitrogen atoms not forming part of a nitro radical
C07D 317/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 317/60 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
C07D 319/20 - 1,4-DioxanesHydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring with substituents attached to the hetero ring
C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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
A heterocyclic compound represented by general formula (I) [wherein R1 represents an optionally protected amino group, or an optionally substituted C1-6 alkyl group; R2 and R3 independently represent a C1-2 alkyl group; X represents a hydrogen atom, or a halogen atom; Z1 represents C-R4 (wherein R4 represents a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group), or N; Z2 represents C-R5 (wherein, R5 represents a hydrogen atom, a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group), or N; Z3 represents C-R6 (wherein R6 represents a hydrogen atom, a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group ), or N; Z4 represents C-R7 (wherein, R7 represents a hydrogen atom, a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group), or N; Z represents CH or N; and A represents a methylene group, or a bond] or a salt thereof, which has an excellent anti-HIV activity and is therefore useful as an anti-HIV agent.
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula:
is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.
Disclosed is a novel crystal of piperacillin sodium monohydrate, which has diffraction angles represented by 2θ of 6.6, 10.9, 14.6, 17.0, 18.2, 19.8 and 24.9° in powder X-ray diffraction. The crystal has a low analogous substance content, high purity, and low hygroscopicity, and is useful as an active ingredient for a drug or an intermediate for the production of an active ingredient for a drug.
C07D 499/68 - Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical by nitrogen atoms with aromatic rings as additional substituents on the carbon chain
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n are the same or different and each represents an integer of 1-6) or a salt thereof, which is useful as a prodrug of a benzothiophene derivative or a salt thereof.
Disclosed is an organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a production intermediate for 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.
Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation.
Disclosed is a useful tablet which contains a high quantity of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a salt thereof; has a size that is easy to ingest; has superior release characteristics; and has a hardness that can withstand film coating, packaging, and transportation.
An N-acyl anthranilic acid derivative represented by general formula (I) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.)
C07C 235/58 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho- position to carbon atoms of the same non-condensed six-membered aromatic ring
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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
A61K 31/4462 - Non-condensed piperidines, e.g. piperocaine only substituted in position 3
A61K 31/4465 - Non-condensed piperidines, e.g. piperocaine only substituted in position 4
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
A61K 31/625 - Salicylic acidDerivatives thereof having heterocyclic substituents, e.g. 4-salicyloylmorpholine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 207/337 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
C07D 267/08 - Seven-membered rings having the hetero atoms in positions 1 and 4
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 295/12 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
C07D 295/14 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 317/60 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 317/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
C07D 333/24 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
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
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 11/00 - Drugs for disorders of the respiratory system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
Disclosed is a pharmaceutical composition comprising a pyrazine derivative represented by the general formula:
3 represents a hydrogen atom or an amino-protecting group] or a salt thereof and at least one neuraminidase inhibitor. The pharmaceutical composition is useful for a treatment including the treatment or prevention of influenza. Also disclosed is a method of using these components in combination. The method is useful for a treatment including the treatment or prevention of influenza.
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
A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
Provided is a novel compound useful as a pharmaceutical that exhibits strong antibacterial activity for gram negative bacteria, such as Pseudomonas aeruginosa, and for drug-resistant bacterial strains thereof, based on LpxC inhibitory activity. Provided is a hydroxamic acid derivative represented by general formula (1) or a pharmacologically permitted salt thereof. (1)
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
Disclosed is a benzothiophene oxide derivative represented by the general formula (wherein R1 and R2 are the same or different and each represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkenyl group, an amino group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, an oxo group and the like; R3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n are the same or different and each represents an integer of 1-6) or a salt thereof, which is useful as a prodrug of a benzothiophene derivative or a salt thereof.
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
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 43/00 - Drugs for specific purposes, not provided for in groups
67.
NOVEL BENZOTHIOPHENE OXIDE DERIVATIVE AND SALT THEREOF
Disclosed is a benzothiophene oxide derivative represented by the general formula (wherein R1 and R2 are the same or different and each represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkenyl group, an amino group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, an oxo group and the like; R3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n are the same or different and each represents an integer of 1-6) or a salt thereof, which is useful as a prodrug of a benzothiophene derivative or a salt thereof.
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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
68.
METHOD OF UTILIZATION OF COMBINATION OF BENZOPHENONE DERIVATIVE OR SALT THEREOF AND IMMUNOSUPPRESSING AGENT, AND PHARMACEUTICAL COMPOSITION COMPRISING THESE COMPONENTS
Disclosed are: a method of utilizing a combination of a benzophenone derivative represented by general formula [wherein R1 represents a heterocyclic group which may be substituted, a phenyl group which may be substituted, or the like; Z represents an alkylene group, or the like; R2 represents a carboxyl group which may be protected with an alkyl group, or the like; R3 represents a hydroxyl group which may be protected, or the like; R4 represents a cycloalkyloxy group which may be substituted, or the like; and R5 represents a hydrogen atom, or the like] or a salt thereof and at least one immunosuppressing agent; and a pharmaceutical composition comprising the benzophenone derivative or a salt thereof and at least one immunosuppressing agent. The method and the pharmaceutical composition are useful for the treatment (e.g., therapy and prophylaxis) of autoimmune diseases.
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 43/00 - Drugs for specific purposes, not provided for in groups
69.
USE OF BENZOPHENONE DERIVATIVE OR SALT THEREOF AND TNF α INHIBITOR IN COMBINATION AND PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVE OR SALT THEREOF AND THE INHIBITOR
Disclosed are use of a benzophenone derivative represented by general formula (I) or a salt thereof and one or more TNFα inhibitors in combination, and a pharmaceutical composition containing the benzophenone derivative or a salt thereof and one or more TNFα inhibitors. The use and the composition are useful for treatment or prevention of autoimmune diseases and the like. (In the formula, R1 represents an optionally substituted heterocyclic group, a substituted phenyl group or the like; Z represents an alkylene group or the like; R2 represents a carboxyl group, which may be protected by an alkyl group, or the like; R3 represents an optionally protected hydroxyl group or the like; R4 represents an optionally substituted cycloalkyloxy group or the like; and R5 represents a hydrogen atom or the like.)
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
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 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
Disclosed is an agent comprising a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof:
3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
71.
Anti-foot-and-mouth disease virus agent for animal belonging to family Suidae or sheep, and method for prevention or treatment of foot-and-mouth disease in animal belonging to family Suidae or sheep
Disclosed is an anti-foot-and-mouth disease virus agent for an animal belonging to the Family Suidae, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention or treatment of food-and-mouth disease in an animal belonging to the Family Suidae. Also disclosed is an anti-foot-and-mouth disease virus agent for sheep, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention, therapy or the like of food-and-mouth disease in sheep.
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
A23K 1/18 - specially adapted for particular animals
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A23K 1/16 - supplemented with accessory food factors; Salt blocks
72.
SOLID DISPERSION COMPRISING 3-[5-[4-(CYCLOPENTYLOXY)- 2-HYDROXYBENZOYL]-2-[(3-HYDROXY-1,2-BENZISOXAZOL-6- YL)METHOXY]PHENYL]PROPIONIC ACID OR SALT THEREOF, OR COMPOSITION COMPRISING THE SOLID DISPERSION
Disclosed is a solid dispersion comprising 3-[5-[4- (cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2- benzisoxazol-6-yl)methoxy]phenyl]propionic acid or a salt thereof and polyvinylpyrrolidone, or a composition comprising the solid dispersion. The solid dispersion or the composition is useful as a pharmaceutical composition for oral application which is improved in and keeps the solubility of T-5224 contained therein in a neutral range and is also improved in gastrointestinal adsorption.
Disclosed is 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate, which has a strong antibacterial activity. The compound is highly safe and useful as an original drug for pharmaceutical preparations. Also disclosed is a method which is useful for producing 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
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
Disclosed is an organic amine salt of 6--fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a productionintermediate for 6-fluoro-3-hydroxy-2--pyrazinecarboxamide.
Because of having an effect of inhibiting RANKL production, an effect of inhibiting lowering in OPG production and an effect of inhibiting the differentiation and activation of osteoclasts, a drug characterized by containing a benzophenone derivative represented by the following general formula or its salt is highly useful in caring, e.g., treating and/or preventing various diseases, in which the differentiation and activation of osteoclasts participate, such as osteoporosis: general formula wherein each substituent has the same meaning as defined in the description.
Disclosed is an organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a production intermediate for 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.
A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula:
1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.
Type II crystals, type III crystals and type IV crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy]-N'-(butoxycarbonyl)benzamidine are useful as the active ingredient of excellent antifungal agents.
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
Disclosed is a compound represented by the following general formula: (wherein R1 represents a hydrogen atom or the like; R2 represents an optionally substituted alkyl or aryl group or the like; R3 and R4 may be the same or different and each represents an aryl group or the like; R5 represents a hydrogen atom or the like; X1 represents an alkylene group, a bonding hand or the like; X2 represents a bonding hand or the like; Y1 represents a bonding hand or the like; and Z1 and Z2 each represents CH or the like) or a salt thereof. Since the compound or a salt thereof has a strong PGE2 production inhibitory activity, it is useful for treatment or prevention of diseases and conditions associated with PGE2.
C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
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
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
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
C07C 311/13 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 207/335 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
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 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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 233/26 - Radicals substituted by carbon atoms having three bonds to hetero atoms
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 241/28 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen 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 277/28 - Radicals substituted by nitrogen atoms
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 295/12 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
C07D 295/14 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 317/58 - Radicals substituted by nitrogen atoms
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
Disclosed is a novel compound which has a potent antibacterial activity on a gram-negative bacterium (e.g., Pseudomonas aeruginosa) or a drug-resistant mutant thereof relying on its and LpxC inhibitory activity, and which is therefore useful as a pharmaceutical agent. Specifically disclosed is a hydroxamic acid derivative represented by the general formula (1) below or a pharmaceutically acceptable salt thereof.
C07D 215/52 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4 with aryl radicals attached in position 2
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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
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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 239/74 - QuinazolinesHydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
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 405/10 - 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 aromatic rings
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
C07D 413/10 - 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 aromatic rings
Disclosed is a pharmaceutical composition comprising a pyrazine derivative represented by the general formula:(see formula 1)[wherein R1 and R2 independently represent a hydrogen atom or a halogen atom; and R3 represents a hydrogen atom or an amino-protecting group] or a salt thereof and at least one neuraminidase inhibitor. The pharmaceutical composition is useful for a treatment including the treatment or prevention of influenza. Also disclosed is a method of using these components in combination. The method is useful for a treatment including the treatment or prevention of influenza.
Disclosed is a pharmaceutical composition comprising a pyrazine derivative represented by the general formula: [wherein R1 and R2 independently represent a hydrogen atom or a halogen atom; and R3 represents a hydrogen atom or an amino-protecting group] or a salt thereof and at least one neuraminidase inhibitor. The pharmaceutical composition is useful for a treatment including the treatment or prevention of influenza. Also disclosed is a method of using these components in combination. The method is useful for a treatment including the treatment or prevention of influenza.
Disclosed are a novel crystal of piperacillin sodium which has diffraction angles of 3.7°, 5.5°, 7.3°, 11.6°, 14.5° and 18.0° and a novel crystal of piperacillin sodium which has diffraction angles of 5.6°, 7.8°, 12.3°, 15.5°, 17.5°, 23.3°, 24.8° and 28.5° expressed by 2ϑ in the powder X-ray diffraction analysis. The crystals have excellent stability and solubility and a low water-absorbing property, is extremely easy to be handled in the production process for a medicinal substance and in the packing during the preparation process for a pharmaceutical product. A pharmaceutical preparation for injection comprising any one of the crystals is useful.
C07D 499/68 - Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical by nitrogen atoms with aromatic rings as additional substituents on the carbon chain
Disclosed is a pharmaceutical composition comprising a phenylamidine derivative represented by the general formula: [wherein R1 and R2 independently represent a C3-4 alkyl group which may be substituted] or a salt thereof and at least one substance selected from an azole-type antifungal agent, a polyene-type antifungal agent, a candin-type antifungal agent and a fluoropyrimidine-type antifungal agent. Also disclosed is a method of using a combination of the phenylamidine derivative or the salt thereof and the substance. The pharmaceutical composition and the method are useful for the treatment of a fungal infectioninduced by a fungal pathogen.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
Disclosed is a protein kinase C enhancer characterized by containing a benzothiophenealkyl ether derivative represented by the general formula below or a salt thereof. (formula) (In the formula, R1 and R2 may be the same or different and represent one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkenyl group, an amino group, a heterocyclic group, an optionally protected amino group, a hydroxyl group, an carboxyl group, an oxo group and the like; R3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n may be the same or different and represent an integer of 1-6.) This protein kinase C enhancer is useful for treatment or prevention of various diseases associated with protein kinase C.
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
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
Disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2- hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6- yl)methoxy]phenyl]propionic acid having refraction angles of 14.0, 16.0, 23.3, 23.7 and 26.3˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. Also disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3- hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid having refraction angles of 14.6, 23.1, 24.7, 25.6 and 26.0˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. These crystals have small specific volumes, are hardly charged electrically, can be handled easily, and are useful as excellent active ingredients for anti-rheumatic drugs.
ANTI-FOOT-AND-MOUTH DISEASE VIRUS AGENT FOR ANIMAL BELONGING TO FAMILY SUIDAE OR SHEEP, AND METHOD FOR PREVENTION OR TREATMENT OF FOOT-AND-MOUTH DISEASE IN ANIMAL BELONGING TO FAMILY SUIDAE OR SHEEP
Disclosed is an anti-foot-and-mouth disease virus agent for an animal belonging to the family Suidae, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention or treatment of food-and-mouth disease in an animal belonging to the family Suidae. Also disclosed is an anti-foot-and-mouth disease virus agent for sheep, which comprises 3-oxo-3,4-dihyro- 2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention, therapy or the like of food-and-mouth disease in sheep.
C07D 241/08 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
A23K 1/16 - supplemented with accessory food factors; Salt blocks
Disclosed is a compound represented by the general formula: [wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/542 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
89.
ANTI-FOOT-AND-MOUTH DISEASE VIRUS AGENT FOR ANIMAL BELONGING TO FAMILY SUIDAE OR SHEEP, AND METHOD FOR PREVENTION OR TREATMENT OF FOOT-AND-MOUTH DISEASE IN ANIMAL BELONGING TO FAMILY SUIDAE OR SHEEP
Disclosed is an anti-foot-and-mouth disease virus agent for an animal belonging to the family Suidae, which comprises 3-oxo-3,4-dihyro-2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention or treatment of food-and-mouth disease in an animal belonging to the family Suidae. Also disclosed is an anti-foot-and-mouth disease virus agent for sheep, which comprises 3-oxo-3,4-dihyro- 2-pyrazincarboxamide or a salt thereof. The agent is extremely useful for the prevention, therapy or the like of food-and-mouth disease in sheep.
ORAL COMPOSITION COMPRISING 3-[5-[4-(CYCLOPENTYLOXY) -2-HYDROXYBENZOYL]-2-[(3-HYDROXY-1,2-BENZISOXAZOL-6- YL)METHOXY]PHENYL]PROPIONIC ACID OR SALT THEREOF
An oral composition comprising 3-[5-[4- (cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2- benzisoxazol-6-yl)methoxy]phenyl]propionic acid or a salt thereof and polyvinylpyrrolidone. The oral composition is useful as a pharmaceutical composition for oral application having the following properties (1) to (3): (1) no new-type facility is required for the production of the composition; (2) the composition can be produced by a simple process; and (3) the composition can be dissolved stably in the gastrointestinal tract even when the pH value in the gastrointestinal tract varies and therefore is improved in gastrointestinal adsorption.
Disclosed is an agent comprising a benzothiphene alkyl ether derivative represented by the general formula below or a salt thereof: wherein R1 and R2 independently represent at least one group selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.
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
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
92.
NEUROGENESIS INDUCER OR NEUROPATHY THERAPEUTIC AGENT COMPRISING ALKYL ETHER DERIVATIVE OR SALT THEREOF
Disclosed is an agent comprising a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof:(see above formula)wherein R1 and R2 independently represent at least one group selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, anarylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
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
93.
PROCESS FOR PRODUCTION OF 3-[5-[4-(CYCLOPENTYLOXY)-2-HYDROXYBENZOYL]-2-[(3-OXO-2-SUBSTITUTED-2,3-DIHYDRO-1,2-BEZISOXAZOL-6-YL)METHOXY]PHENYL]PROPIONATE ESTER AND INTERMEDIATE FOR THE PROCESS
Disclosed is a production process using, as an intermediate, a 6-(halomethyl)-1,2-benzisooxazol-3(2H)-one derivative represented by the general formula: Wherein R5 represents a methyl group substituted by at least one phenyl group which may be substituted, or an oxygenated heterocyclic ring which may be substituted; and X represents a halogen atom. The process is useful for the production of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid, which is useful as an antirheumatic agent, in a high yield and in a safe and simple manner.
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07C 67/303 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by hydrogenation of unsaturated carbon-to-carbon bonds
C07D 311/14 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 6 and unsubstituted in position 7
Disclosed is an arylamidine derivative represented by the following general formula: ⏧Chemical formula] (wherein R1 and R2 independently represent an optionally substituted C3-4 alkyl group) or a salt thereof, which is useful as an antifungal agent.
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
95.
METHOD FOR PRODUCING 4-(3-(4-(3-(4-CYANOPHENOXY)PROPYL)- 1-PIPERIDINYL)PROPOXY)BENZONITRILE AND INTERMEDIATE THEREOF
A production method using a piperidine derivative represented by the following general formula: ⏧Chemical formula 1] (wherein Y1 and Y2 independently represent a hydroxyl group, a halogen atom, an alkanesulfonyloxy group or an arylsulfonyloxy group) or a salt thereof as an intermediate is useful as a method for safely and easily producing a 4-(3-(4-(3-(4- cyanophenoxy)propyl)-1-piperidinyl)propoxy)benzonitrile, which is important as a production intermediate for pharmaceutical products, with high yield.
C07D 211/18 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
96.
NOVEL NITROGENATED HETEROCYCLIC COMPOUND AND SALT THEREOF
A nitrogenated heterocyclic compound represented by the general formula: wherein the broken line represents a single bond or a double bond; R1, R2, R3, R4 and R5 independently represent a hydrogen or halogen atom, a lower alkyl, aryl, lower alkoxy or monocyclic heterocyclic group which may be substituted or the like; R6 represents a lower alkyl, aryl, monocyclic heterocyclic, dicyclic heterocyclic or tricyclic heterocyclic group which may be substituted; X1 represents a lower alkylene group or the like; X2 represents a lower alkylene, lower alkenylene or lower alkynilene group which may be substituted; X3 represents an oxygen or sulfur atom, a sulfiny or sulfonyl group or the like; Y1 represents a cyclic group containing a bivalent nitrogen which may be substituted or the like; and Z1 represents a nitrogen atom, a carbon atom which may be substituted or the like, or a salt thereof. The compound or salt has a potent antibacterial activity and a high safety, and is therefore useful as an excellent antibacterial agent.
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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
97.
PHARMACEUTICAL COMPOSITION AND METHOD USING ANTIFUNGAL AGENT IN COMBINATION
A pharmaceutical composition containing one or more antifungal agents selected from an arylamidine derivative represented by the general formula: ⏧Chemical Formula 1] (wherein R1 represents an amidino group that may be substituted with a hydroxyl group that may be protected with an acyl group, an amidino group that may be substituted with an alkoxy group that may be substituted, or an amidino group that may be substituted with an aralkyloxy group that may be substituted; R2 and R3 identically or differently represent a hydrogen atom or a halogen atom) or a salt thereof, an azole antifungal agent, a polyene antifungal agent, a candin antifungal agent and a fluoropyrimidine antifungal agent has a strong antifungal activity and is useful for the treatment of fungal infection. A method for using them in combination is useful as an excellent therapeutic method for fungal infection. A pharmaceutical composition containing the arylamidine derivative represented by the above general formula or a salt thereof and an immunosuppressing agent has a strong antifungal activity and is useful for the treatment of fungal infection and a skin disease such as atopic dermatitis. A method for using them in combination is useful as an excellent therapeutic method for fungal infection and a skin disease such as atopic dermatitis.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
Provided is a process for the production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol of the following formula:(see above formula) or a salt thereof, the process comprising: subjecting 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propionyl)azetidin-3-ol to reduction reaction with the addition of an activator in the presence of alkali metal borohydride, to yield 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol and, ifdesired, reacting the thus formed 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol with an acid to form a salt thereof; wherein the activator is a protonic acid, a methylating agent or a silylating agent, or any combination thereof. The thus formed 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof may be used as a remedy for disease of central and peripheral nerve.
C07D 333/56 - Radicals substituted by oxygen atoms
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
99.
PROCESS FOR PRODUCTION OF 1-(3-(2-(1-BENZOTHIOPHEN-5-YL)-ETHOXY)PROPYL)AZETIDIN-3-OL OR SALTS THEREOF
A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a.starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula:(see above formula) wherein X1 represents a halogen atom,is useful as a safe process for mass production of 1-(3-(2-(1- benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.
A process for the production of 1-(3-(2-(1-benzothiophen-5- yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound a (phenylthio)acetic acid derivative represented by the general formula ⏧1] or a salt thereof: ⏧Chemical Formula 1] (wherein X1 is halogeno) is useful as a safe process for mass production of 1-(3-(2- (1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which are useful as remedies for central nervous system diseases and peripheral nerve diseases.
C07D 333/54 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
