Abstract

Disclosed is a continuous crystallization process for ibuprofen, wherein an ibuprofen product is obtained by means of multistage continuous crystallization; and the multistage continuous reaction crystallization comprises the steps of reaction to form an oil, two to four stages of reaction crystallization, dehydration and washing, and the adjustments of pH and temperature of each step. The method effectively resolves the explosive nucleation phenomenon caused by oil analysis during the reaction crystallization of ibuprofen, has stable crystallization process conditions and simple operation control, and reduces pollution of the environment by using water as a solvent; and the resulting ibuprofen crystals have large and uniform particle size, and high product purity and yield. The method improves the stability and product quality of operation of the crystallization process, reduces the production cost, and achieves the stabilized industrial production of ibuprofen.

IPC Classes  ?

• C07C 51/02 - Preparation of carboxylic acids or their salts, halides, or anhydrides from salts of carboxylic acids
• C07C 51/43 - SeparationPurificationStabilisationUse of additives by change of the physical state, e.g. crystallisation
• C07C 57/30 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings

Goods & Services

Medicines for human purposes; pharmaceutical preparations in the form of injection; pharmaceutical preparations in the form of troche; crude drugs; pharmaceutical preparations in the form of capsules; analgesics.

Goods & Services

Medicines for human purposes; syringes prefilled with pharmaceutical preparations; troche; crude drugs; medicinal ointments; Chinese medicine nostrum; biochemical drugs; analgesics; febrifuges.

Goods & Services

Medicines for human purposes; pharmaceutical preparations; troche; syringes prefilled with pharmaceutical preparations; crude drug; Chinese medicine nostrum; medicines for veterinary purposes; tonics [medicines]; biochemical drugs; capsules for medicines.

Goods & Services

Medicines for human purposes; syringes prefilled with pharmaceutical preparations; troche; crude drugs; medicinal ointments; Chinese medicine nostrum; biochemical drugs; analgesics; febrifuges.

Abstract

An octahydroanthracene compound having the structure shown in formula (I) and (II), preparation method and application thereof are disclosed. The octahydroanthracene compound has a good therapeutic effect on tumors and neurodegenerative diseases. The preparation of the octahydroanthracene compound is mainly carried out by using benzene as a starting material, and being subjected to Friedel-Crafts reaction, nitration, reduction, (sulfo-) amide formation, reduction, urea formation or amide formation, thus obtaining a target compound.

IPC Classes  ?

• C07C 275/38 - 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 six-membered aromatic rings of a carbon skeleton being further substituted by doubly-bound oxygen atoms
• C07C 2/86 - Preparation of hydrocarbons from hydrocarbons containing a smaller number of carbon atoms by condensation between a hydrocarbon and a non-hydrocarbon
• C07C 201/08 - Preparation of nitro compounds by substitution of hydrogen atoms by nitro groups
• C07C 209/36 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of nitrogen-to-oxygen or nitrogen-to-nitrogen bonds by reduction of nitro groups by reduction of nitro groups bound to carbon atoms of six-membered aromatic rings
• C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
• C07C 269/04 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
• C07C 271/28 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
• C07C 273/18 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
• C07C 303/38 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reaction of ammonia or amines with sulfonic acids, or with esters, anhydrides, or halides thereof
• C07C 311/48 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
• C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
• C07D 295/195 - Radicals derived from nitrogen analogues of carboxylic acids
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• C07C 259/10 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
• C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
• C07C 233/80 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring

Abstract

Disclosed are an opctahydroanthracene compound as represented by formula (I) or (II), a preparation method for same, and uses of same, which provides great therapeutic effects for tumors and neurodegenerative diseases and is prepared mainly with benzene that serves as the starting material and undergoes reactions such as Friedel-Crafts reactions, nitration, reduction, sulfonamide formation, reduction, urea formation or amide formation to produce the target compound.

IPC Classes  ?

• C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
• C07C 259/10 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
• C07C 233/80 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• 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 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Inclusion complexes of pinocembrin with cyclodextrin or its derivatives and their preparation are provided. The inclusion complexes can be used to make drugs.

IPC Classes  ?

• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• 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 9/08 - Solutions
• B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
• A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit

Abstract

Two crystalline forms of pinocembrin of formula (I): α and β, their preparation and their use for manufacture of pharmaceutical compositions. There exists difference between them in bioavailability. They are used for treating and preventing cerebral ischemic diseases by protective action of neurovascular unit, and enhancing blood drug level in vivo.

IPC Classes  ?

• A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• C07D 311/32 - 2, 3-Dihydro derivatives, e.g. flavanones

Goods & Services

CHEMICALS, NAMELY, ACIDS, ALKALIES AND ESTERS FOR GENERAL USE IN THE PHARMACEUTICAL AND CHEMICAL INDUSTRIES; CHEMICAL PREPARATIONS FOR THE MANUFACTURE OF PORCELAIN AND VITREOUS ENAMEL; PHOTOGRAPHIC CHEMICALS, NAMELY PHOTOGRAPHIC SENSITIZERS; CHEMICAL REAGENTS FOR SCIENTIFIC AND RESEARCH USE; CHEMICALS, NAMELY, PHENOL FOR INDUSTRIAL PURPOSES, ETHYL ALCOHOL, ANHYDRIDES, SALTS FOR INDUSTRIAL PURPOSES, CHLOROPROPIONYL CHLORIDE, METOL VERMIFUGES; VITAMIN PREPARATIONS; ANTIPARASITIC PREPARATIONS; DEPURATIVES, NAMELY, MEDICAL PREPARATIONS FOR REMOVING IMPURITIES FROM, OR THE CLEANSING OF, THE BLOOD; DIETETIC SUBSTANCES ADAPTED FOR MEDICAL USE; MEDICINES FOR DENTAL PURPOSES, NAMELY, FOR THE TREATMENT OF PERIODONTITIS AND TOOTHACHES; MEDICINES FOR VETERINARY PURPOSES, NAMELY, FOR THE TREATMENT OF CANCER; UNIT DOSE CAPSULES SOLD EMPTY FOR PHARMACEUTICAL USE AND GELATIN CAPSULES SOLD EMPTY FOR PHARMACEUTICALS; PHARMACEUTICAL PREPARATIONS, NAMELY, ANTINFECTION DRUGS; ANTICANCER DRUGS; IMMUNITY DRUGS; PHARMACEUTICAL PREPARATIONS FOR HUMAN PURPOSES IN THE TREATMENT OF RESPIRATORY SYSTEMS DISEASES, DIGESTIVE SYSTEM DISEASES, SKIN DISEASES, GYNECOLOGICAL DISEASES, NERVOUS SYSTEM DISEASES, UROGENITAL SYSTEM DISEASES, CARDIOVASCULAR DISEASES AND DISORDERS; PHARMACIST-PREPARED TRADITIONAL CHINESE MEDICINES FOR THE TREATMENT OF INSOMNIA, FLU, DIGESTIVE SYSTEM DISEASES AND RESPIRATORY SYSTEM DISEASES