The present invention relates to a method for preparing 2-(2,5-difluorophenyl)-3-carboxy-7-chloro-(4H)-4-benzopyranone represented by formula 1 below, a novel intermediate used therein, and a method for preparing the same. Specifically, an object of the present invention is to provide a novel preparation method, in which the compound of formula 1 below can be efficiently and economically synthesized and can be mass-produced in a high yield.
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
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
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 311/30 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
2.
Composition for preventing or treating TNF-related diseases, containing novel derivative as active ingredient, and method for inhibiting TNF activity by using same
The present invention relates to: a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate, or stereoisomer thereof; a composition for preventing, alleviating or treating TNF-related diseases, containing the same as an active ingredient; and a method for treating TNF-related diseases, a reagent composition for inhibiting TNF, and a method for inhibiting TNF, all of which use the same. The compositions can be orally administered so as not to cause injection side effects, do not cause immunological tolerance, and can effectively inhibit a TNF activity by being directly bound to TNF while facilitating co-administering with a conventional oral preparation and dosage control.
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 9/00 - Medicinal preparations characterised by special physical form
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
3.
NOVEL TNF ACTIVITY INHIBITOR COMPOUND, AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
The present invention relates to: a novel TNF activity inhibitor compound; a pharmaceutically acceptable salt thereof; a preventing, ameliorating, or treating method comprising administering a compound according to the present invention; a method for producing a compound according to the present invention; and a pharmaceutical composition comprising the compound.
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
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
4.
METHOD FOR PRODUCING BENZOPYRANONE COMPOUND AND NOVEL INTERMEDIATE USED THEREIN
The present invention provides a method for producing 2-(2,5-difluorophenyl)-3-carboxy-7-chloro-(4H)-4-benzopyranone represented by chemical formula 1, a novel intermediate used therein, and a method for producing same. Specifically, an objective of the present invention is to provide a novel production method, in which the compound of chemical formula 1 can be efficiently and economically synthesized and can be mass-produced in a high yield.
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
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
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 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 1/00 - Drugs for disorders of the alimentary tract or the digestive system
5.
CRYSTALLINE FORM OF BENZOPYRANONE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
The present invention provides type I crystals, type II crystals, type III crystals, and type IV crystals which are novel crystalline forms of 2-(2,5-difluorophenyl)-3-carboxy-7-chloro-(4H)-4-benzopyranone. In particular, the type IV crystals have excellent physicochemical stability and can be easily used in the preparation of a pharmaceutical composition containing same as an active ingredient.
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
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
6.
SALTS AND CRYSTAL FORM OF BENZOPYRANONE COMPOUND, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Salts and a crystal form of a compound in chemical formula 1, namely 2-(2,5-difluorophenyl)-3- carboxy-7-chloro-(4H)-4-benzopyranone, according to the present invention are excellent in terms of various physicochemical properties, namely hygroscopicity, physicochemical stability, solubility and the like, and thus can be utilized for preparing a pharmaceutical composition comprising same as an active ingredient.
C07D 311/32 - 2, 3-Dihydro derivatives, e.g. flavanones
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 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 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 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 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
7.
Composition for preventing or treating TNF-related diseases, containing novel derivative as active ingredient, and method for inhibiting TNF activity by using same
The present invention relates to: a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate, or stereoisomer thereof; a composition for preventing, alleviating or treating TNF-related diseases, containing the same as an active ingredient; and a method for treating TNF-related diseases, a reagent composition for inhibiting TNF, and a method for inhibiting TNF, all of which use the same. The compositions can be orally administered so as not to cause injection side effects, do not cause immunological tolerance, and can effectively inhibit a TNF activity by being directly bound to TNF while facilitating co-administering with a conventional oral preparation and dosage control.
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 9/00 - Medicinal preparations characterised by special physical form
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
8.
COMPOSITION FOR PREVENTING OR TREATING TNF-RELATED DISEASES AND METHOD FOR INHIBITING TNF ACTIVITY
The present invention relates to: a 4-benzopyranone derivative of Formula I or a pharmaceutically acceptable salt, solvate, racemate or stereoisomer thereof; a composition for preventing, alleviating or treating TNF-related diseases, containing the same as an active ingredient; and a method for treating TNF-related diseases, a reagent composition for inhibiting TNF and a method for inhibiting TNF, all of which use the same. The compositions can be orally administered so as not to cause injection side effects, do not cause immunological tolerance, and can effectively inhibit TNF activity by being directly bound to TNF while facilitating co-administering with a conventional oral preparation and dosage control.(see formula I)
patents
