The present invention relates to a biphenyl derivative and use thereof, and the biphenyl derivative has a structure represented by the formula (I) as defined in the specification. The use refers the use of the biphenyl derivative or a pharmaceutically acceptable salt or solvate thereof, or a pharmaceutical composition comprising the biphenyl derivative or a pharmaceutically acceptable salt or solvate thereof in the preparation of a medicament for the treatment and/or prevention of ischemic stroke.
C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/223 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-amino acids
C07C 65/105 - 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 hydroxy or O-metal groups polycyclic
C07C 69/16 - Acetic acid esters of dihydroxylic compounds
C07C 39/15 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings with all hydroxy groups on non-condensed rings
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
C07C 69/08 - Formic acid esters of dihydroxylic compounds
C07C 39/367 - Halogenated derivatives polycyclic non-condensed, containing only six-membered aromatic rings, e.g. halogenated poly-(hydroxy-phenyl)alkanes
C07C 271/42 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
2.
2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparations and preparation methods therefor
This invention relates to a 2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparation having 2,2′,6,6′-tetraisopropyl-4,4′-biphenol as its active ingredient and formed into said lipid microsphere preparation with common medically used injection-grade oil, emulsifier, and injection-grade water.
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
Disclosed are uses of 3,3',5,5'-tetraisopropyl-4,4'-diphenol, pharmaceutical salts thereof, esterification products thereof, or solvates thereof in the preparation of medicines for the prevention and treatment of cerebral ischemia.
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
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
C07C 39/15 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings with all hydroxy groups on non-condensed rings
The present invention relates to a diphenyl derivative and uses thereof, the diphenyl derivative having the structure as indicated in formula (I) defined in the description. The uses refer to the uses of the diphenyl derivative, pharmaceutical salts thereof, solvates thereof, or pharmaceutical compositions containing said diphenyl derivative, pharmaceutical salts thereof, or solvates thereof in the preparation of medicines for the prevention and/or treatment of cerebral ischemia.
C07C 65/105 - 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 hydroxy or O-metal groups polycyclic
C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
C07C 39/15 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings with all hydroxy groups on non-condensed rings
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/223 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-amino acids
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
5.
2,2′,6,6′-tetraisopropyl-4,4′-2-biphenol soft capsule and method for preparing same
Disclosed is a 2,2′,6,6′-tetraisopropyl-4,4′-biphenol soft capsule composed of a capsule shell and the contents in the capsule, wherein the contents in the capsule include 2,2′,6,6′-tetraisopropyl-4,4′-biphenol, a solvent, and an antioxidant, among others.
An oily formulation of fulvestrant or derivatives thereof and a method for producing the same. The oily formulation comprises: fulvestrant or derivatives thereof in an amount of 10 mg/ml to 170 mg/ml; a lactate compound in an amount of 5 to 80% of the total weight of the formulation; a vegetable oil or synthetic oil (ester); an analgesic; and an optional antioxidant.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 9/19 - Particulate form, e.g. powders lyophilised
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
7.
PREPARATION OF ARTEMETHER/BENFLUMETOL COMPOUND FAT EMULSION FOR INJECTION, AND APPLICATION OF SAME IN MALARIA TREATMENT
An artemether/benflumetol compound fat emulsion injection, a preparation method therefor, and an application of same in preparing medicine for malaria treatment. The fat emulsion contains artemether of 0.01-1.5wt%, benflumetol of 0.01-3.5wt%, oil for injection of 10.0-30.0wt%, emulsifier of 0.6-30.0%wt%, solubilizer of 0-10wt%, co-emulsifier of 0.01-5wt%, an isotonizing agent of 2.25-7wt%, an antioxidant of 0.002-0.075wt%, and water for injection for the rest.
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
The present invention provides 3,3',5,5'-tetraisopropyl-4,4'-diphenol crystal forms I, II and III, and preparation methods thereof. Crystal form I is superior to crystal form II in terms of stability at a high temperature, high humidity, strong light and in a water medium. The preparation methods for 3,3',5,5'-tetraisopropyl-4,4'-diphenol crystal forms I, II and III provided in the invention are simple, easy to operate and suitable for technological production.
C07C 37/84 - SeparationPurificationStabilisationUse of additives by physical treatment by crystallisation
C07C 39/15 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings with all hydroxy groups on non-condensed rings
9.
2,2',6,6'-TETRAISOPROPYL-4,4'-2-BIPHENOL SOFT CAPSULE AND METHOD FOR PREPARING SAME
Disclosed is a 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol soft capsule preparation, which is formed by a capsule cover and capsule internal contents. The capsule internal contents contain 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol, solvent, antioxidant, and other ingredients.
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
Disclosed are a sustained-release preparation of fulvestrant or derivatives thereof and a preparation method therefor. The formulation of the preparation is as follows: (1) fulvestrant or derivatives thereof, with a content of 10mg/ml-500mg/ml in the preparation, (2) ketone compound or dimethyl sulfoxide as the cosolvent, possessing a content of 3%-80% in the total weight of the preparation, (3) vegetable oil or artificially synthesized oil (ester) as the dispersing agent, (4) analgesic, and (5) an optional antioxidant.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 47/08 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A 2,2',6,6'-tetraisopropyl-4,4'-2-biphenol (hereinafter referred to as 2-biphenol) lipid microsphere preparation takes 2-biphenol as the active component, and is prepared by using oil for injection, emulsifiers, additives, and water for injection that are frequently used in pharmacy.
A medical composite aluminum film pouch with high oxygen gas impermeability as outer bag encloses a non-PVC flexible plastic bag containing an infusion solution. The composite aluminum pouches are made by PT/A1/PE or laminate film consisting of polymers/Al-deposited polymers or polymer/aluminum foil/polymers. The infusion in the non-PVC bag is usually fluid that is easily deteriorated upon contact with oxygen or light-sensitive. Using composite aluminum film pouch as outer package has the well accepted characteristics of high obstructing, high oxygen-resistance, high light-protecting and air-proofing. It helps to solve the quality stability problems of the content which is light-sensitive and easily-oxidized. It is safe and innocuous, able to prolong the storage and shelf life of the medicine.
The present invention provides a novel multi-step process for the manufacturing Fulvestrant, which is economical and convenient to operate at commercial scale, and requires only simple chromatographic separations after the coupling step of adding the side chain to the 7 position of the steroid.
Disclosed is a 2,2',6,6'-tetraisopropyl-4,4'-biphenol soft capsule composed of a capsule shell and the contents in the capsule, wherein the contents in the capsule comprise 2,2',6,6'-tetraisopropyl-4,4'-biphenol, a solvent, and an antioxidant, among others.
An oily formulation of fulvestrant or derivatives thereof and a method for producing the same. The oily formulation comprises: fulvestrant or derivatives thereof in an amount of 10 mg/ml to 170 mg/ml; a lactate compound in an amount of 5 to 80% of the total weight of the formulation; a vegetable oil or synthetic oil (ester); an analgesic; and an optional antioxidant.
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea
patents
