Disclosed are a compound represented by formula (A-I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof as a glutamine cyclase inhibitor, a preparation method therefor, a pharmaceutical composition comprising the compound represented by formula (A-I) or the stereoisomer thereof or the pharmaceutically acceptable salt thereof, and a use of the compound represented by formula (A-I) or the stereoisomer thereof or the pharmaceutically acceptable salt thereof in preventing or treating diseases or conditions mediated by QPCT and/or QPCTL, including neurodegenerative diseases.
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 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention relates to an anti-IL4R antibody. Specifically, provided is an antibody or an antigen-binding fragment thereof capable of specifically binding to IL4R, wherein the antibody or the antigen-binding fragment thereof can specifically bind to IL4R with high affinity, and can be used as a drug to treat diseases related to IL4R.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
Use of a composition in preparation of a drug for treating a patient suffering from a cerebral stroke. The composition includes edaravone and dexborneol, and the patient has a history of hypertension.
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
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
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention provides a compound and use thereof, particularly a JWA gene agonist and use thereof in preventing or treating radiation damage. The compound, by means of activating JWA gene expression, enhances the DNA repair capacity of cells, and has a good elimination capacity for highly active oxygen species generated by X-ray radiation. The compound can also effectively inhibit cell apoptosis caused by radiation to reduce the damage, and further reduce the generation of free radicals to reduce the probability of radiation damage.
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
A stable pharmaceutical composition contains active ingredients of edaravone and dextrocamphol can control the content of unique impurity SCR-756 and impurity SCR-757 thereof.
C07D 231/24 - One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms having sulfone or sulfonic acid radicals in the molecule
Disclosed are a pyrrolidine compound as represented by formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and the use of the pharmaceutical composition as a selective estrogen receptor degrader (SERD) in the prevention or treatment of estrogen receptor-related diseases.
Disclosed are a pyrrolidine compound as represented by formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and the use of the pharmaceutical composition as a selective estrogen receptor degrader (SERD) in the prevention or treatment of estrogen receptor-related diseases.
A compound for preventing or treating a tumor overexpressing YY1 and the use thereof. The anti-tumor drug can effectively bind to YY1, triggers the degradation of YY1 by means of a ubiquitin-proteasome pathway, and releases the inhibitory effect of YY1 on a JWA gene, so as to activate the JWA gene and inhibit the interaction of YY1-HSF1, which in turn inhibits the proliferation and in vivo growth of tumor cells.
A pharmaceutically acceptable salt of the compound of formula (I), a crystal thereof, a preparation method therefor, and a use thereof. The pharmaceutically acceptable salt is selected from sulfate, phosphate, benzoate, succinate, adipate, fumarate, L-malate, and citrate, preferably benzoate, succinate, and adipate.
A drug combination comprising a compound represented by formula (K) as a selective estrogen receptor downregulator (SERD) or a pharmaceutically acceptable salt thereof and a CDK4/6 inhibitor, a combined product or pharmaceutical composition containing the drug combination, and an application thereof.
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
An application of a composition in improving or treating cognitive impairment. The composition contains 3-methyl-1-phenyl-2-pyrazolin-5-one or a pharmaceutically acceptable salt thereof and borneol or dexborneol. The cognitive impairment comprises Alzheimer's disease (AD), vascular dementia (VD), mild cognitive impairment (MCI), and other types of dementia.
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
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
11.
APPLICATION OF COMPOSITION CONTAINING EDARAVONE AND DEXBORNEOL IN IMPROVING OR TREATING COGNITIVE IMPAIRMENT
An application of a composition in improving or treating cognitive impairment. The composition contains 3-methyl-1-phenyl-2-pyrazolin-5-one or a pharmaceutically acceptable salt thereof and borneol or dexborneol. The cognitive impairment comprises Alzheimer's disease (AD), vascular dementia (VD), mild cognitive impairment (MCI), and other types of dementia.
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
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
12.
CYANO COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (China)
WUHAN INSTITUTE OF VIROLOGY, CHINESE ACADEMY OF SCIENCES (China)
SIMCERE PHARMACEUTICAL CO., LTD. (China)
Inventor
Jiang, Xiangrui
Xu, Yechun
Zhang, Leike
Su, Haixia
Zhang, Qiumeng
Zhao, Wenfeng
Shang, Weijuan
Shen, Jingshan
Xiao, Gengfu
Jiang, Hualiang
Abstract
Provided are a compound as represented by formula I, and a racemate, an enantiomer, a diastereomer and a pharmaceutically acceptable salt thereof, and the use thereof in the prevention or treatment of related diseases caused by coronavirus and/or small RNA virus infection.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 307/02 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
C07D 309/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 335/02 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
Disclosed is the use of a docetaxel polymer micelle in the preparation of a drug for preventing or treating malignant hydrothorax and ascites. The docetaxel polymer micelle is used for treating malignant hydrothorax and ascites, which can significantly prolong survival, improve the treatment effect of hydrothorax and ascites, increase the plasma exposure amount of the drug, and reduce the secretion of VEGF.
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 35/04 - Antineoplastic agents specific for metastasis
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/19 - Particulate form, e.g. powders lyophilised
14.
PURIFICATION METHOD FOR AMPHIPHILIC BLOCK COPOLYMER
A purification method for an amphiphilic block copolymer, a purified amphiphilic block copolymer, and a pharmaceutical composition comprising the amphiphilic block copolymer. The purification method of the amphiphilic block copolymer comprises: (1) providing a solution comprising the amphiphilic block copolymer in an organic solvent; (2) adding activated carbon to the solution of step (1); and (3) filtering to remove the activated carbon, obtaining the amphiphilic block copolymer. The provided method can effectively remove metallic tin ion content from the amphiphilic block copolymer.
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
15.
HYDROPHOBIC DRUG POLYMER MICELLE AND PREPARATION METHOD THEREFOR
Provided is a polyethylene glycol monomethyl ether-polylactic acid block copolymer and a preparation method therefor. The polyethylene glycol monomethyl ether-polylactic acid block copolymer is a block copolymer formed by means of ring-opening polymerization of D,L-lactide and polyethylene glycol monomethyl ether, wherein the feed mass ratio of polyethylene glycol monomethyl ether to D,L-lactide is 1:1.05-1.25. Also provided is a hydrophobic drug polymer micelle lyophilized preparation. The lyophilized preparation contains a hydrophobic drug and the polyethylene glycol monomethyl ether-polylactic acid block copolymer. The hydrophobic drug polymer micelle lyophilized preparation has higher purity and redissolution stability, and is more suitable for clinical use.
A stable pharmaceutical composition, belonging to the technical field of medicine. The pharmaceutical composition having active ingredients of edaravone and dextrocamphol can surprisingly control the content of unique impurity SCR-756 and impurity SCR-757 thereof. The problems of impurities and product quality being difficult to control and the storage life being short, etc. are solved from the source.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
C07D 231/26 - 1-Phenyl-3-methyl-5- pyrazolones, unsubstituted or substituted on the phenyl ring
A stable pharmaceutical composition, belonging to the technical field of medicine. The pharmaceutical composition having active ingredients of edaravone and dextrocamphol can surprisingly control the content of unique impurity SCR-756 and impurity SCR-757 thereof. The problems of impurities and product quality being difficult to control and the storage life being short, etc. are solved from the source.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
The disclosure provides an anti-aging method. The method includes applying JWA gene to produce or screen anti-aging products, or products associated with treatment of aging-related diseases, or anti-oxidation products, or products for maintaining homeostasis, or products associated with diagnosis of aging or aging-related diseases, or agonists of the JWA gene.
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 39/06 - Free radical scavengers or antioxidants
19.
USE OF COMPOSITION IN TREATMENT OF CEREBRAL STROKE
Use of a composition in preparation of a drug for treating a patient suffering from a cerebral stroke. The composition comprises edaravone and dexborneol, and the patient has a history of hypertension.
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
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 9/00 - Drugs for disorders of the cardiovascular system
Use of a composition in the preparation of a medicament for treating cerebral stroke in a patient. The composition comprises Edaravone and Dexborneol, and the patient has a heart disease history.
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
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
21.
USE OF COMPOSITION IN TREATMENT OF CEREBRAL APOPLEXY
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
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 9/00 - Drugs for disorders of the cardiovascular system
Disclosed are a pyrrolidine compound as represented by formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and the use of the pharmaceutical composition as a selective estrogen receptor degrader (SERD) in the prevention or treatment of estrogen receptor-related diseases.
Disclosed in the present invention is a preparation method for a pyrazolopyrimidine compound. Also disclosed in the present invention is a preparation method for a compound of formula (I) and an intermediate compound thereof.
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
A sublingual tablet pharmaceutical composition containing edaravone and (+)-2-borneol, and a preparation method thereof. The sublingual tablet pharmaceutical composition includes edaravone, (+)-2-camphanol, an excipient, a filler, a binder, a disintegrant, and a lubricant. The excipient is selected from one or more of mannitol, lactose, dextran, cysteine, glycine, copovidone, and beta-cyclodextrin.
A sublingual tablet pharmaceutical composition containing edaravone and (+)-2-borneol, and a preparation method thereof. The sublingual tablet pharmaceutical composition includes edaravone, (+)-2-camphanol, an excipient, a filler, a binder, a disintegrant, and a lubricant. The excipient is selected from one or more of mannitol, lactose, dextran, cysteine, glycine, copovidone, and beta-cyclodextrin.
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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
27.
PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING INFLAMMATORY DISEASE
The present invention discloses a pharmaceutical composition, comprising a hydroxychloroquine and iguratimod. The invention also relates to an application of the hydroxychloroquine and a salt thereof for manufacturing a pharmaceutical product for alleviating a toxic side effect of iguratimod. The composition provides significant effects as a synergistic agent and for alleviating a toxic side effect.
A61K 31/4706 - 4-Aminoquinolines8-Aminoquinolines, e.g. chloroquine, primaquine
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]