Abstract

Provided is a compound represented by formula (I) having a PAI-1 inhibiting action. [In formula (I), R1 represents an optionally substituted C6-10 aryl group etc., T represents a single bond etc., m is 0 or 1, when m is 0 G represents -N-C(=O)-CO2H etc., when m is 1 G represents an oxygen atom etc., R2 represents an optionally substituted C6-10 aryl group etc, E represents formula (II) (wherein one of R31, R32, R33 and R34 represents R1-T- and the remaining three each individually represent a hydrogen atom etc., and R35 is -X-Y', a hydrogen atom etc.), X represents -CH2- etc., Y' represents a carboxyl group etc. and M represents a single bond etc.]

IPC Classes  ?

• C07C 59/66 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• 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 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
• A61K 31/402 - 1-aryl-substituted, e.g. piretanide
• 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 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
• 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 31/495 - 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 31/54 - 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 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• C07C 59/68 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
• C07C 59/70 - Ethers of hydroxy-acetic acid
• C07C 65/24 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
• C07C 205/56 - Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups bound to carbon atoms of six-membered aromatic rings and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton
• C07C 229/42 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
• C07C 233/25 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
• C07C 233/56 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides
• C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• C07C 317/22 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
• C07C 323/12 - 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 singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• C07C 323/21 - 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 singly-bound oxygen atoms 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 with the sulfur atom of the thio group bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
• C07C 323/22 - 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 doubly-bound oxygen atoms bound to the same carbon skeleton
• C07C 323/41 - Y being a hydrogen or an acyclic carbon atom
• 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 211/42 - Oxygen atoms attached in position 3 or 5
• C07D 257/04 - Five-membered rings
• 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 317/54 - Radicals substituted by oxygen atoms

Abstract

Disclosed is a compound represented by the general formula (I) below, which has PAI-1 production inhibitory activity. (I) (In the formula, R1 represents, for example, a hydrogen atom or a 4-(morpholinyl)carbonyl group; ring D represents, for example, a benzene ring or a substituted benzene ring; phenyl group E has a substituent such as a halogen atom, a halogenated alkyl group, an alkyl group, an halogenated alkoxy group or an alkoxy group.)

IPC Classes  ?

• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 295/20 - 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 by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof

Abstract

Disclosed is a compound useful as a type-I 11β-hydroxysteroid dehydrogenase inhibitor. Specifically disclosed is a compound represented by the formula shown below, a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt, wherein X represents O or S; and the broken line and the wavy lines independently represent the presence or absence of a bond, provided that: (i) when the broken line represents the presence of a bond, then the wavy lines independently represent the absence of a bond and R2 and R3 independently represent a hydrogen, a halogen or the like; and (ii) when the broken line represents the absence of a bond, then the wavy lines independently represent the presence of a bond, R1 and R4 independently represent a hydrogen, a halogen or the like, R2 and R3 independently represent a hydrogen, a halogen or the like, and R5 and R6 independently represent a hydrogen, an alkyl which may be substituted or the like.

IPC Classes  ?

• C07D 265/24 - 1,3-OxazinesHydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
• A61K 31/536 - 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 carbocyclic 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 31/5415 - 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 carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• A61K 31/547 - 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 spiro-condensed or forming part of bridged ring systems
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 279/06 - 1,3-ThiazinesHydrogenated 1,3-thiazines not condensed with other rings
• C07D 279/08 - 1,3-ThiazinesHydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
• 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

Abstract

Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type I inhibitor. Specifically disclosed is a compound represented by the formula below, a pharmaceutically acceptable salt thereof, or a solvate of any of them. (In the formula, R1 represents an optionally substituted cycloalkyl, an optionally substituted cycloalkylalkyl, an optionally substituted heterocycle or an optionally substituted heterocyclealkyl; X represents -O-, -NR3-, -NR3C(=O)- or -NR3S(=O)2-; R2 represents an optionally substituted aryl, an optionally substituted arylalkyl, an optionally substituted heteroaryl or an optionally substituted heteroarylalkyl; and R3 represents a hydrogen or an optionally substituted alkyl.)

IPC Classes  ?

• C07D 263/20 - Oxygen atoms attached in position 2
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 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

Abstract

Disclosed is a compound represented by the general formula (I) below, which has a plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, a salt thereof, or a hydrate or solvate of any of them. (I) (In the formula, R1 represents a C6-10 aryl group or a C6-10 aryl group substituted with a group selected from the group consisting of a halogen atom, a cyano group, a nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group and a C1-6 alkylsulfanyl group; R2 represents a C6-10 aryl group or a C6-10 aryl group substituted with a group selected from the group consisting of a halogen atom, a hydroxy group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C1-6 alkylsulfanyl group and a phenyl group; X represents a single bond or an oxygen atom; Z represents a phenylene group or a substituted phenylene group; and m represents 0 or 1.)

IPC Classes  ?

• C07C 271/02 - Carbamic acidsSalts of carbamic acids
• 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 31/343 - 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 35/00 - Medicinal preparations containing materials or reaction products thereof with undetermined constitution
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue
• 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
• C07D 307/91 - DibenzofuransHydrogenated dibenzofurans

Abstract

Disclosed is a compound represented by the general formula (I), a salt thereof, or a hydrate or solvate of the compound or the salt, which has an inhibitory activity on plasminogen activator inhibitor-1 (PAI-1). (I) wherein R1 represents a C6-10 aryl group or a substituted C6-10 aryl group; R2 represents a C6-10 aryl group or a C6-10 aryl group substituted by a group selected from the group consisting of a halogen atom, a nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a phenyl groupand a carboxy group; X represents -CH2-, -CH2CH2-, -CH=CH- or -N(R3)-C(=O)-; Y represents a carboxy group or a biological equivalent of a carboxy group; R3 represents a hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group; and m represents a number of 0 or 1.

IPC Classes  ?

• C07C 59/64 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

A compound represented by the formula (I) or a salt thereof, which is useful as an active ingredient of a pharmaceutical for the prevention and/or treatment of a disease induced by the activation of STAT6 and/or NF-κB. (I) wherein R1, R2, R3 and R4 independently represent a hydrogen atom, a halogen atom, a cyano group, a nitro group, a C1-4 alkyl group, a halogenated C1-4 alkyl group, or a C1-4 alkoxy group; R5 represents a halogen atom, a cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group, or a C1-4 alkoxy group; R6represents a C5-7 cycloalkyl group, a substituted C5-7 cycloalkyl group, a completely saturated 5- to 7-membered heterocyclic group or a substituted, completely saturated 5- to 7-membered heterocyclic group; X represents a single bond, an oxygen atom, a sulfur atom, NR7, -O-CH2 or –N(R8)-CH2-; R7 represents a hydrogen atom or a C1-4 alkyl group, or together with a substituent in R6 forms a single bond, a methylene group or an ethylene group; and R8 represents a hydrogen atom, a C1-4 alkyl group, or a C7-12 aralkyl group.

IPC Classes  ?

• C07C 235/64 - 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 having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61K 31/40 - 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 31/402 - 1-aryl-substituted, e.g. piretanide
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• 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 31/454 - 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 31/495 - 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 31/4965 - Non-condensed pyrazines
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/06 - Antiasthmatics
• A61P 13/00 - Drugs for disorders of the urinary system
• A61P 17/00 - Drugs for dermatological disorders
• A61P 17/04 - Antipruritics
• A61P 17/06 - Antipsoriatics
• A61P 19/00 - Drugs for skeletal disorders
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue
• A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/18 - Antivirals for RNA viruses for HIV
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07C 217/88 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring the oxygen atom of at least one of the etherified hydroxy groups being further bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07D 207/12 - Oxygen or sulfur atoms
• C07D 207/14 - Nitrogen atoms not forming part of a nitro radical
• 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
• C07D 211/26 - 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 nitrogen atoms
• C07D 211/42 - Oxygen atoms attached in position 3 or 5
• C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
• C07D 211/58 - Nitrogen atoms attached in position 4
• C07D 211/60 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 211/74 - Oxygen 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
• 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
• C07D 243/08 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
• 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

Abstract

A compound represented by the formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or salt: (I) wherein the ring Q represents a monocyclic aryl which may be substituted, a monocyclic heteroaryl which may be substituted, a fused aryl which may be substituted, a fused heteroaryl which may be substituted, or the like; Y1 represents a single bond, -NR6- or the like; the ring A represents a non-aromatic heterocyclic diyl which may be substituted; the formula: -Y2Z1- represents a group represented by the following formula: or ; R7 independently represents a hydrogen, a lower alkyl which may be substituted or the like; R8 and R9 independently represent a hydrogen or a lower alkyl which may be substituted; n is an integer of 0 to 3; Z1 represents a single bond, O, S or NR9; the ring B represents an aromatic carbocyclic diyl which may be substituted or an aromatic heterocyclic diyl which may be substituted; Y3 represents a single bond, a lower alkylene which may be substituted and may have -O- inserted therein, a lower alkenylene which may be substituted, or the like; and Z2 represents COOR3 or the like.

IPC Classes  ?

• C07D 277/82 - Nitrogen atoms
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
• A61K 31/454 - 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 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/06 - Antihyperlipidemics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 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
• C07D 211/58 - Nitrogen atoms attached in position 4
• 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
• 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 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 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 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/04 - 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

Abstract

A pharmaceutical agent comprising a compound represented by the general formula (I) or a salt thereof as an active ingredient and having an inhibitory effect against plasminogen activator inhibitor-1: wherein each of R1 and R2 represents an aromatic group; W represents a group selected from the connecting groups shown in the group W-1 below; and Z represents a single bond or a connecting group having 1 to 3 atoms in the backbone: , wherein the bond on the left-hand side attaches to a carbon atom and the bond on the right-hand side attaches to a nitrogen atom; X represents a sulfur atom or NH; Y represents an oxygen or sulfur atom; and R3 represents a hydrocarbon, hydroxy or carboxy group.

IPC Classes  ?

• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles 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
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 35/00 - Antineoplastic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 231/20 - One oxygen atom attached in position 3 or 5
• 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 277/34 - Oxygen atoms
• C07D 277/36 - Sulfur atoms
• 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 403/06 - 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 carbon chain containing only aliphatic carbon atoms
• 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 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 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 417/14 - 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