Abstract

Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61P 3/00 - Drugs for disorders of the metabolism
• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 471/04 - Ortho-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07D 513/04 - Ortho-condensed systems

Abstract

It discloses a compound shown in general formula (1) or a pharmaceutically acceptable salt thereof and a method for preparation of the compound; the compound is a xanthine oxidase inhibitor with xanthine oxidase inhibiting activity; the compound has an excellent xanthine oxidase inhibitory activity and has potential application value in anti-gout drugs, anti-hyperuricemia drugs, etc.

IPC Classes  ?

• 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
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/4192 - 1,2,3-Triazoles
• 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 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• 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 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

Crystalline forms of Compound I, active on URAT1, were prepared and characterized: Also provided are methods of using the crystalline forms.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Crystalline forms of Compound I, active on URAT1, were prepared and characterized: Also provided are methods of using the crystalline forms.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Disclosed is a compound capable of being used for gout. The compound is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, can reduce the serum uric acid level in rat models suffering from hyperuricemia, and has potential application value in the areas of anti-gout drugs, anti-hyperuricemia drugs and the like.

IPC Classes  ?

• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• A61K 31/415 - 1,2-Diazoles
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/4192 - 1,2,3-Triazoles

Abstract

Disclosed herein is a compound for reducing uric acid, which is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. The present invention can significantly reduce the serum uric acid level in a rat hyperuricemia model, and has potential application value in aspects of anti-gout therapies, anti-hyperuricemia therapies, and the like.

IPC Classes  ?

• C07D 275/04 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/04 - 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 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/4192 - 1,2,3-Triazoles
• 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

Abstract

The present invention belongs to the field of medicinal chemistry, and specifically disclosed are an anti-inflammatory analgesic compound and the use thereof. The compound of the present invention is a compound having a structure shown in formula (I) or formula (II), an isomer or a pharmaceutically acceptable salt thereof. The compound of the present application has a significant curative effect on gouty arthritis in rats, and also has a good anti-inflammatory factor effect. Therefore, the compound has potential application prospects in the aspects of anti-inflammatory analgesic drugs, particularly anti-acute gouty arthritis drugs, anti-rheumatoid arthritis drugs, drugs for reducing inflammatory factors, drugs for treating inflammatory storms or coronavirus pneumonia drugs, etc.

IPC Classes  ?

• C07D 307/20 - Oxygen atoms
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61K 31/18 - Sulfonamides
• 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 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
• 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 31/40 - 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 31/41 - 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 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• 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 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/64 - Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
• A61K 31/69 - Boron compounds
• 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 31/14 - Antivirals for RNA viruses
• C07C 233/32 - 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 doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 233/52 - 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 carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 237/24 - 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 ring other than a six-membered aromatic ring of the carbon skeleton
• C07C 255/19 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton
• C07C 255/47 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of rings being part of condensed ring systems
• C07C 271/24 - 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 ring other than a six-membered aromatic ring
• C07C 271/34 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 275/26 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 305/20 - Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
• C07C 307/08 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 311/07 - 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 ring other than a six-membered aromatic ring
• C07C 311/46 - Y being a hydrogen or a carbon atom
• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• 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 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
• C07D 257/04 - Five-membered rings
• C07D 263/24 - Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
• C07D 265/32 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
• C07D 295/155 - 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 with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 295/182 - Radicals derived from carboxylic acids
• C07F 5/02 - Boron compounds

Abstract

The present invention belongs to the field of medicinal chemistry, and specifically disclosed are an anti-inflammatory analgesic compound and the use thereof. The compound of the present invention is a compound having a structure shown in formula (I) or formula (II), an isomer or a pharmaceutically acceptable salt thereof. The compound of the present application has a significant curative effect on gouty arthritis in rats, and also has a good anti-inflammatory factor effect. Therefore, the compound has potential application prospects in the aspects of anti-inflammatory analgesic drugs, particularly anti-acute gouty arthritis drugs, anti-rheumatoid arthritis drugs, drugs for reducing inflammatory factors, drugs for treating inflammatory storms or coronavirus pneumonia drugs, etc.

IPC Classes  ?

• C07D 307/20 - Oxygen atoms
• C07D 295/182 - Radicals derived from carboxylic acids
• C07D 265/32 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
• C07D 295/155 - 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 with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• C07D 257/04 - Five-membered rings
• C07F 5/02 - Boron compounds
• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
• 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 263/24 - Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
• C07C 311/07 - 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 ring other than a six-membered aromatic ring
• C07C 311/46 - Y being a hydrogen or a carbon atom
• C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
• C07C 305/20 - Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 307/08 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 233/32 - 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 doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 233/52 - 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 carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 255/47 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of rings being part of condensed ring systems
• C07C 237/24 - 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 ring other than a six-membered aromatic ring of the carbon skeleton
• C07C 255/19 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and carboxyl groups, other than cyano groups, bound to the same saturated acyclic carbon skeleton
• C07C 275/26 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 271/24 - 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 ring other than a six-membered aromatic ring
• C07C 271/34 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 31/14 - Antivirals for RNA viruses
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• 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 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
• A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
• A61K 31/18 - Sulfonamides
• 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 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• 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 31/495 - 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 31/64 - Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
• A61K 31/69 - Boron compounds
• 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 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine

Abstract

The present invention relates to a class of xanthine oxidase inhibitors, which are compounds as represented by general formula (I) or pharmaceutically acceptable salts thereof. The xanthine oxidase inhibitors have an excellent xanthine oxidase inhibitory activity, and have potential application value in anti-gout drugs, anti-hyperuricemia drugs, etc.

IPC Classes  ?

• 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
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

The present invention relates to a class of xanthine oxidase inhibitors, which are compounds as represented by general formula (I) or pharmaceutically acceptable salts thereof. The xanthine oxidase inhibitors have an excellent xanthine oxidase inhibitory activity, and have potential application value in anti-gout drugs, anti-hyperuricemia drugs, etc.

IPC Classes  ?

• 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 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

A method for synthesizing 3-bromo-5-(2-ethylimidazo[1,2-a] pyridine-3-carbonyl)-2-hydroxybenzonitrile, particularly relates to a method for synthesizing a compound represented by a formula (III), and particularly relates to step A or step B; step A: a compound represented by a formula (I) and a compound represented by a formula (II) are first heated in an organic solvent to react, and the resulting reaction product and a base are heated in the presence of water to continue the reaction to obtain a compound represented by a formula (III); and step B: a compound represented by the formula (I), a compound represented by a formula (II), and a base are heated in an organic solvent to react, and the resulting reaction product is heated in the presence of water to continue the reaction to obtain a compound represented by a formula (III).

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

The invention discloses compounds for treatment or prevention of liver diseases. The compounds are compounds represented by a formula (I) or (II), optical isomers or pharmaceutically acceptable salts of the compounds. The compounds and optical isomers or pharmaceutically acceptable salts of the compounds can be applied to preparation of drugs for treatment or prevention of liver diseases.

IPC Classes  ?

• C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• 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
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/08 - Solutions

Abstract

A compound having therapeutic efficacy for liver disease. The compound may be the compound as represented by formula (I), an optical isomer of same, or a pharmaceutically acceptable salt thereof. The compound is applicable in the treatment or prevention of liver disease and has excellent application prospects specifically in terms of medicaments for treating or preventing fatty liver, hepatic fibrosis or hepatic cirrhosis.

IPC Classes  ?

• C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• 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
• 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
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

The present invention belongs to the field of medicinal chemistry. Specifically disclosed is a class of URAT1 inhibitors for promoting uric acid excretion, which are compounds as represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on the transport of uric acid by hURAT1 in HEK293 transfected cells, and that such compounds have a good application prospect in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• C07D 487/04 - Ortho-condensed systems
• C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

Abstract

Disclosed in the present invention is a synthesis method for 3-bromo-5-(2-ethylimidazo[1,2-α]pyridine-3-carbonyl)-2-hydroxybenzonitrile, relating in particular to a synthesis method for a compound represented by formula (III), which specifically involves step A or step B; step A comprises: a compound represented by formula (I) and a compound represented by formula (II) first reacting by means of heating in an organic solvent, and a resulting reaction product and a base are further being heated in the presence of water to continue reacting so as to obtain a compound represented by formula (III); Step B comprises: the compound represented by formula (I), the compound represented by formula (II) and a base first reacting by means of heating in an organic solvent, and a resulting reaction product then being heated in the presence of water to continue reacting so as to obtain the compound represented by formula (III).

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

Disclosed is the use of a 4-(benzothiazole-2-yl)arylamine compound in treating stomach cancer, wherein the compound is a compound as shown in general formula I or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed is a use of a 4-(benzselenazol-2-yl)arylamine compound in treating stomach cancer or intestinal cancer, wherein the compound is a compound as shown in general formula I or a pharmaceutically acceptable salt thereof. The present invention finds a new use of a 4-(benzselenazol-2-yl)arylamine compound in the treatment of diseases, and provides a potential medicine for the treatment of stomach cancer or intestinal cancer.

IPC Classes  ?

• C07D 293/12 - SelenazolesHydrogenated selenazoles
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61P 3/00 - Drugs for disorders of the metabolism
• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 471/04 - Ortho-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07D 513/04 - Ortho-condensed systems

Abstract

Disclosed are a class of pharmaceutical compounds for treating liver diseases and application thereof. In particular, said pharmaceutical compounds are compounds as represented by general formula (I), optical isomers, or pharmaceutically acceptable salts thereof.The provided compounds, optical isomers, or pharmaceutically acceptable salts thereof have low toxicity and good curative effect on liver diseases, especially fatty liver. Experiments have shown that the compounds have a significant protective effect on non-alcoholic fatty liver in zebrafishes, and therefore have a good application prospect in drugs for the treatment or prevention of liver diseases, especially fatty liver, liver fibrosis, or cirrhosis.

IPC Classes  ?

• C07D 311/32 - 2, 3-Dihydro derivatives, e.g. flavanones
• 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
• 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
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• 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

Abstract

Disclosed are compounds for the treatment or prevention of liver diseases, which are compounds represented by the general formula (I) or (II), optical isomers or pharmaceutically acceptable salts thereof that can be applied to the preparation of drugs for treating or preventing liver diseases.

IPC Classes  ?

• C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• 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
• 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 37/02 - Immunomodulators
• A61P 37/08 - Antiallergic agents

Abstract

Disclosed are compounds for the treatment or prevention of liver diseases, which are compounds represented by the general formula (I) or (II), optical isomers or pharmaceutically acceptable salts thereof that can be applied to the preparation of drugs for treating or preventing liver diseases.

IPC Classes  ?

• C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• 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
• 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 37/02 - Immunomodulators
• A61P 37/08 - Antiallergic agents

Abstract

The present invention belongs to the field of medicinal chemistry. Specifically disclosed is a class of URAT1 inhibitors for promoting uric acid excretion, which are compounds as represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on the transport of uric acid by hURAT1 in HEK293 transfected cells, and that such compounds have a good application prospect in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 307/80 - Radicals substituted by oxygen atoms
• 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 31/437 - 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
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• C07D 471/04 - Ortho-condensed systems

Abstract

The present invention belongs to the field of medicinal chemistry. Specifically disclosed is a class of URAT1 inhibitors for promoting uric acid excretion, which are compounds as represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on the transport of uric acid by hURAT1 in HEK293 transfected cells, and that such compounds have a good application prospect in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 471/04 - Ortho-condensed systems
• 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 31/437 - 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
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

The invention discloses a class of compounds for treating or preventing hyperuricemia or gout, which is a compound shown in general formula (I) or a pharmaceutically acceptable salt. These compounds and their pharmaceutically acceptable salts in the invention are useful for the promotion of uric acid excretion to treat or prevent hyperuricemia or gout.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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 31/429 - Thiazoles condensed with heterocyclic ring systems
• 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 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• C07D 307/80 - Radicals substituted by oxygen atoms
• C07D 471/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems

Abstract

Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• C07D 307/80 - Radicals substituted by oxygen atoms
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
• 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 31/437 - 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 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

It discloses compounds for the treatment and prevention of breast cancer, which are specifically 2-phenyl benzoselenazole compounds, pharmaceutically acceptable salts thereof and prodrugs thereof. The present invention further discloses pharmaceutical compositions containing the compounds and applications of the compounds in preparing medicines for the treatment and prevention of breast cancer in mammals. The compounds of the present invention can effectively inhibit or reduce the growth or proliferation of breast cancer cells in mammals, with no inhibition effect on the growth of part of the tested cell lines except for the breast cancer cell lines, and are highly selective.

IPC Classes  ?

• 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
• C07D 293/12 - SelenazolesHydrogenated selenazoles
• A61P 35/00 - Antineoplastic agents

Abstract

A novel URAT1 inhibitor and a pharmaceutical application thereof. The inhibitor is a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, wherein a radical group of the compound is defined by the specification. The compound represented by formula (I) can be used to prepare a pharmaceutical product promoting uric acid excretion, specifically for preparing a pharmaceutical product for treating or preventing hyperuricemia or gout.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Abstract of the Disclosure The invention discloses a class of compounds for treating or preventing hyperuricemia or gout, which is a compound shown in general formula (I) or a pharmaceutically acceptable salt. These compounds and their pharmaceutically acceptable salts in the invention are useful for the prornotion of uric acid excretion to treat or prevent hyperuricernia or gout. R4 0 OH R3 ( ) R2 CA 2998034 2019-07-04

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Provided are a compound as represented in formula (I), pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and uses thereof. The compound as represented in formula (I) and the pharmaceutically acceptable salts thereof are used in the preparation of medicines for the treatment or prevention of hyperuricemia or gout by means of uric acid discharging.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

Disclosed are a class of compounds for treating or preventing breast cancer, in particular, 2-phenyl-benzoselenazole compounds, and a pharmaceutically acceptable salt thereof and an easily hydrolysed prodrug thereof. Further disclosed are a pharmaceutical composition containing these compounds and the use of such compounds for treating or preventing breast cancer in mammals. The compounds of the present invention can effectively inhibit or reduce the growth or proliferation of mammalian breast cancer cells, and at the same time, such compounds do not inhibit the growth of partial test cells, apart from breast cancer cells, and have a good selectivity. Such compounds show a more obvious medicinal effect, and have high selectivity, low toxicity and few side effects.

IPC Classes  ?

• C07D 293/12 - SelenazolesHydrogenated selenazoles
• A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
• A61P 35/00 - Antineoplastic agents

Abstract

A 2-aryl selenazole compound and a pharmaceutical composition are disclosed, wherein the 2-aryl selenazole compound is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The 2-aryl selenazole compound has the activity of inhibiting xanthine oxidase. The compound or a pharmaceutically acceptable salt thereof can be applied in terms of preparing a drug used for prevention or treatment of hyperuricemia, gout, diabetic nephropathy, an inflammatory disease or a neurological disease.

IPC Classes  ?

• C07D 293/06 - SelenazolesHydrogenated selenazoles
• C07D 421/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 33/04 - Sulfur, selenium or telluriumCompounds thereof
• 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 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
• 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 31/496 - 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
• C07D 421/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having selenium, tellurium, or halogen atoms as ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 495/04 - Ortho-condensed systems