Provided in the present application are a CCR8 antagonistic polypeptide compound, a pharmaceutical composition thereof, a kit thereof, the use of the compound, and the use of the pharmaceutical composition. The CCR8 antagonistic polypeptide compound can be used for preventing or treating cancers or tumors, inflammatory diseases, viral infections, IgG4-related diseases, cutaneous immune diseases, or related symptoms thereof.
The present invention relates to the technical field of pharmaceuticals. Specifically provided in the present invention are a crystal form of L-arginine (S)-2-(1-acetoxy-n-pentyl)benzoate, and a preparation method therefor and the use thereof. For the crystal form, an X-ray powder diffraction pattern expressed in terms of diffraction angle 2θ is obtained by means of Cu-Kα radiation. The X-ray powder diffraction pattern has characteristic peaks at diffraction angle 2θ of 5.10, 10.23, 14.13, 17.58, 19.81, 20.63 and 21.73, wherein the error range of 2θ of each characteristic peak is ±0.2. The technical solution of the present invention has the following advantages: studies show that the crystal form I of the compound as shown in formula I prepared in the present invention has good stability and high purity, and a single crystal of the crystal form I is obtained; and the crystal form I of the compound as shown in formula I obtained by the technical solution of the present invention can satisfy the medicinal requirements of production, transportation and storage, has a stable, repeatable and controllable production process, and can be adapted to industrial production.
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
C07C 279/14 - Dérivés de la guanidine, c.-à-d. composés contenant le groupe les atomes d'azote liés par des liaisons simples ne faisant pas partie de groupes nitro ou nitroso ayant des atomes d'azote de groupes guanidine liés à des atomes de carbone acycliques d'un squelette carboné étant substitué de plus par des groupes carboxyle
3.
PHARMACEUTICAL COMPOSITION OF FLUORINE-SUBSTITUTED CYCLIC AMINE COMPOUND OR SALT THEREOF, AND PREPARATION METHOD THEREFOR
The present application relates to a pharmaceutical composition and preparation of a compound represented by formula (I) or a salt thereof, and a preparation method therefor. Specifically, the present application discloses a pharmaceutical composition using the compound represented by formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition contains the compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. The pharmaceutical composition of the present application has good drug stability and safety, involves a simple and convenient preparation method, and is suitable for industrial production.
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
The disclosure relates to a traditional Chinese medicine composition, comprising active ingredients derived from Cornu caprae or Cornu saigae tataricae, Radix scutellariae, Bulbus fritillariae ussuriensis, Radix glycyrrhizae, Radix et rhizoma rhei, Gypsum fibrosum, Calculus bovis artifactus and Lapis Chloriti, the said active ingredients comprise in parts by weight: at least 1600 parts of amino acids; at least 120 parts of gallic acid; at least 130 parts of liquiritin; at least 20 parts of liquiritigenin; at least 400 parts of baicalin; at least 40 parts of oroxyloside; at least 120 parts of wogonoside; at least 280 parts of glycyrrhizic acid; at least 12 parts of chrysin-7-O-β-D-glucoronic acid; at least 50 parts of aloe-emodin-8-O-β-D-glucopyranoside; at least 30 parts of chrysophanol-1-O-β-D-glucopyranoside; at least 45 parts of chrysophanol-8-O-β-D-glucopyranoside; at least 260 parts of hyodeoxycholic acid; at least 150 parts of cholic acid. The traditional Chinese medicine composition in the present invention possess antipyretic, anti-inflammatory and antitussive effects.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 31/14 - Antiviraux pour le traitement des virus ARN
5.
5-SUBSTITUTED PYRIDINE-2(1H)-KETONE COMPOUND AND USE THEREOF
The present invention relates to a class of 5-substituted pyridine-2 (1H)-ketone compounds and a use thereof, and specifically relates to a compound as shown in formula (X) or a pharmaceutically acceptable salt thereof.
The present invention relates to a class of 5-substituted pyridine-2 (1H)-ketone compounds and a use thereof, and specifically relates to a compound as shown in formula (X) or a pharmaceutically acceptable salt thereof.
A61K 31/444 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. amrinone
A61K 31/4985 - Pyrazines ou pipérazines condensées en ortho ou en péri avec des systèmes hétérocycliques
A61K 31/53 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec trois azote comme seuls hétéro-atomes d'un cycle, p. ex. chlorazanil, mélamine
The present invention provides a novel anti-CD73 monoclonal antibody. The antibody has high affinity for human CD73 protein. Both biochemical-level and cell-level experiments show that the antibody is highly effective in inhibiting the enzyme activity of CD73. The in-vivo experiment indicates that the antibody has a significant inhibition effect on tumor cell growth. In particular, the antibody does not have the “hook effect” most prior art antibodies have in connection with inhibition of the enzyme activity of CD73, and is therefore more suitable for clinical use than the prior art antibodies.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
Disclosed in the present invention are a crystal form of an alkynyl-substituted quinazoline compound, and a preparation method therefor and the use thereof. Specifically disclosed are a monohydrate crystal form I, an N,N-dimethylformamide solvate crystal form II and an n-butanol solvate crystal form III of a compound as represented by formula (I). The crystal form of the compound of formula (I) disclosed in the present invention can improve the physical and chemical properties of the compound of formula (I) in the prior art; has one or more of the following advantages: good stability, few impurities and good bioavailability; and is suitable for use in subsequent drug preparation.
C07D 405/06 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A recombinant Newcastle disease virus and a preparation method therefor, a recombinant plasmid, and use of the recombinant Newcastle disease virus or the recombinant plasmid. The recombinant Newcastle disease virus is obtained by replacing an F protein of a Newcastle disease virus lasota with an F protein encoded by a DNA as set forth in SEQ ID NO: 1 at positions 7274-8935 from a 5′-terminus. The recombinant Newcastle disease virus is safe and capable of effectively inhibiting tumour cells and promoting tumour cell apoptosis.
C12N 15/85 - Vecteurs ou systèmes d'expression spécialement adaptés aux hôtes eucaryotes pour cellules animales
9.
RHFGF21 FUSION PROTEIN, POLYNUCLEOTIDE ENCODING RHFGF21 FUSION PROTEIN, COMPOSITION CONTAINING RHFGF21 FUSION PROTEIN, AND USE OF RHFGF21 FUSION PROTEIN
A recombinant human fibroblast growth factor 21 (rhFGF21) fusion protein, a polynucleotide encoding the rhFGF21 fusion protein, a recombinant expression vector, a recombinant cell, a pharmaceutical composition and a kit containing the rhFGF21 fusion protein, a use of the rhFGF21 fusion protein, and a method for producing the rhFGF21 fusion protein. Efficient and soluble expression is achieved using a genetic engineering method to obtain a rhFGF21-(VPGXG)n fusion protein, wherein by means of fusion of rhFGF21 and an elastin-like protein (VPGXG)n having an appropriate cycle number n, the resulting fusion protein has better biological activity than wild-type rhFGF21. Moreover, experimental results indicate that the rhFGF21-(VPGXG)n fusion protein has high expression efficiency, and can effectively reduce the blood sugar level in the body of a diabetic animal. In addition, compared with wild-type hFGF21, the fusion protein also has the advantage of a long efficacy duration in reducing the blood sugar level.
Provided are a composition containing a CD38 antibody or a fragment thereof, and a use of the composition in treating diseases associated with CD38 expression.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
A61K 47/68 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
An external spectral data online collection system and the use thereof. The system comprises a sample test window frame (1), an optical window piece (2), an external frame (3), an infrared probe (4) and an optical fiber, wherein the sample test window frame (1) is mounted on a viewing window for a monitored object; the infrared probe (4) is inserted into an external cavity from an end portion and is arranged intersecting the optical window piece (2); and the external frame (3) is capable of setting or adjusting the angle and/or distance between the infrared probe (4) and the optical window piece (2). The system can acquire an infrared spectrum of a material inside a tank or a kettle at a required angle and spacing, which facilitates the online monitoring of materials in the production of pharmaceuticals; and the angle at which infrared light is incident and the distance between a probe and a window piece can be set or adjusted, which has a relatively high practicality, and a change in the inner diameter of an inner cavity can effectively prevent the material from adhering to an inner side of the window piece to affect the incidence of the infrared light.
G01N 21/359 - CouleurPropriétés spectrales, c.-à-d. comparaison de l'effet du matériau sur la lumière pour plusieurs longueurs d'ondes ou plusieurs bandes de longueurs d'ondes différentes en recherchant l'effet relatif du matériau pour les longueurs d'ondes caractéristiques d'éléments ou de molécules spécifiques, p. ex. spectrométrie d'absorption atomique en utilisant la lumière infrarouge en utilisant la lumière de l'infrarouge proche
12.
RECOMBINANT NEWCASTLE DISEASE VIRUS RNDV-VEGF-TRAP, GENOME THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF
The present application discloses a recombinant Newcastle disease virus genome, a recombinant Newcastle disease virus rNDV-VEGF-Trap containing the genome and a preparation method therefor, a DNA molecule encoding the recombinant Newcastle disease virus genome, and a use of the genome and the recombinant Newcastle disease virus in the preparation of a drug for treating cancer. The recombinant Newcastle disease virus provided by the present application relates to inserting a coding gene of VEGF-Trap into the genome of the recombinant Newcastle disease virus, such that the recombinant Newcastle disease virus obtained therefrom is replicated with a strong replication capability, thereby killing host cancer cells; moreover, the recombinant Newcastle disease virus has reliable safety for non-cancer cells, and shows improved anti-tumor effect and oncolytic efficiency.
Disclosed is a traditional Chinese medicine extract. The traditional Chinese medicine extract is prepared from traditional Chinese medicine comprising the following raw materials: 1-100 parts of Magnolia officinalis, 1-100 parts of scorched areca-nuts, 1-100 parts of roasted fructus tsaoko, 1-100 parts of herba ephedrae, 1-100 parts of semen armeniacae amarum, 1-100 parts of rhizoma et radix notopterygii, 1-100 parts of fresh ginger, 1-100 parts of herba pogostemonis, 1-100 parts of herba eupatorii, 1-100 parts of rhizoma atractylodis, 1-100 parts of poria cocos, 1-100 parts of rhizoma atractylodis macrocephalae, 1-100 parts of gypsum, 1-100 parts of scorched hawthorn fruit, 1-100 parts of scorched medicated leaven, 1-100 parts of scorched malt, 1-100 parts of lumbricus, 1-100 parts of paniculate swallowwort roots, 1-100 parts of rhizoma dryopteris crassirhizomae, and 1-100 parts of semen lepidii, wherein the extract has an ephedrine content of 0.5-1.5 mg/g and a solid content transfer rate of 18%-25%.
The present invention discloses a crystal form A of a compound, where the compound is S-(−)-2,3-methylenedioxy-5,8,13,13a-tetrahydro-10,11-dimethoxy-6H-dibenzo[a, g]quinolizine, and an X-ray powder diffraction pattern of the crystal form A includes three or more 2θ values selected from the group consisting of: 12.21±0.2°, 13.381±0.2°, 15.181±0.2°, 16.171±0.2°, 17.101±0.2°, 19.801±0.2°, 21.511±0.2°, 24.391±0.2°, and 25.321±0.2°. The crystal form A of the compound of the present invention does not contain water and a solvent, has high stability and low hygroscopicity, and is suitable for patent medicine.
C07D 491/147 - Systèmes condensés en ortho le système condensé contenant un cycle avec l'oxygène comme hétéro-atome du cycle et deux cycles avec l'azote comme hétéro-atome du cycle
15.
TRADITIONAL CHINESE MEDICINE COMPOSITION, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a traditional Chinese medicine composition, a preparation method therefor, and use thereof. The traditional Chinese medicine composition comprises active ingredients extracted from cassia twig, poria cocos, tree peony bark, peach kernel, and radix paeoniae alba in equal proportions, and comprises the following in percentage by mass: 0.214% or above of gallic acid, 0.008% or above of 4-hydroxybenzoic acid, 0.083% or above of oxypaeoniflorin, 1.112% or above of paeoniflorin, 0.010% or above of ethyl gallate, 0.155% or above of 1,2,3,4,6-O-pentagalloylglucose, 0.041% or above of benzoic acid, 0.015% or above of cinnamic acid, 0.093% or above of benzoyl paeoniflorin, 0.037% or above of cinnamaldehyde, 0.622% or above of paeonol, 1.001% or above of amygdalin, 1.743% or above of water-soluble polysaccharide, 29.671% or above of alkali-soluble polysaccharide, and 9.231% or above of monosaccharide and disaccharide. The traditional Chinese medicine composition can alleviate dysmenorrhea.
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7028 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A pharmaceutical composition that includes: an active ingredient, including 2-(2-aminopyridine-4-yl)-5-(5-((5-(2-ethyl-2H-tetrazole-5-yl)pyridine-2-yl)-oxy)-3,3-amyldimethyl)-1,2,5-thiadiazolidin 1,1-dioxide or pharmaceutically acceptable salt thereof; and auxiliary materials, including a diluent and a suspending agent, where the suspending agent includes povidone. Furthermore, the pharmaceutical composition is rapid in dissolution, high in stability, simple in preparation process and more suitable for industrialized mass production.
A61K 31/444 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. amrinone
Disclosed is a method for preparing a chlorinated compound, and specifically disclosed is a method for preparing a compound represented by formula (I).
Disclosed is a method for preparing a chlorinated compound, and specifically disclosed is a method for preparing a compound represented by formula (I).
A recombinant Newcastle disease virus and a preparation method therefor, a recombinant plasmid, and use thereof. The recombinant Newcastle disease virus is obtained by replacing an F protein of a Newcastle disease virus lasota with an F protein of a Newcastle disease virus virulent strain. The recombinant chimeric virus has good safety and is capable of effectively inhibiting tumour cells, promoting tumour cell apoptosis, and effectively treating a tumour.
Disclosed is a traditional Chinese medicine composition, which contains active ingredients made from goat horns or antelope horns, Scutellaria baicalensis, bulbus Fritillariae ussuriensis, Glycyrrhiza uralensis, Rheum officinale, gypsum, bezoar, and biotite schist and Lapis Chloriti. The active ingredients include, by mass: at least 1600 parts of amino acids, at least 120 parts of gallic acid, at least 130 parts of liquiritin, at least 20 parts of liquiritigenin, at least 400 parts of baicalin, at least 40 parts of oroxyloside, at least 120 parts of wogonoside, at least 280 parts of glycyrrhizic acid, at least 12 parts of chrysin-7-O-?-D-glucuronic acid, at least 50 parts of aloe-emodin 8-O-?-D-glucoside, at least 30 parts of chrysophanol-1-O-?-D-glucoside, at least 45 parts of chrysophanol-8-O-?-D-glucoside, at least 260 parts of hyodeoxycholic acid, and at least 150 parts of cholic acid. The composition has antipyretic, anti-inflammatory, antitussive and anti-new coronavirus effects.
An application of a traditional Chinese medicine composition to preparation of a medicine for treating or preventing coronavirus infection. The composition is prepared from the following raw material medicines in parts by weight: 1-3 parts of honey-fried herba ephedrae, 1-10 parts of semen armeniacae amarum, 1-6 parts of radix platycodonis, 1-6 parts of radix peucedani, 1-6 parts of bulbus fritillariae thunbergii, 1-6 parts of radix stemonae, 1-3 parts of oroxylum indicum, 1-10 parts of radix glehniae and 1-3 parts of radix glycyrrhizae. The diluent of the traditional Chinese medicine composition can protect Vero cells infected with 2019-nCov virus.
Application of a traditional Chinese medicine composition to preparation of a medicine for treating or preventing coronavirus infection. The traditional Chinese medicine composition includes: 2-10 parts of flos lonicerae, 2-10 parts of fructus forsythiae, 2-6 parts of herba menthae, 2-4 parts of herba schizonepetae, 2-5 parts of fermented soybean, 2-6 parts of fried arctii fructus, 2-6 parts of radix platycodonis, 2-4 parts of herba lophatheri and 2-5 parts of radix glycyrrhizae. The traditional Chinese medicine composition has a good effect of treating or preventing coronavirus-related diseases.
Disclosed is a traditional Chinese medicine composition, which contains active ingredients made from goat horns or antelope horns, Scutellaria baicalensis, bulbus Fritillariae ussuriensis, Glycyrrhiza uralensis, Rheum officinale, gypsum, bezoar, and biotite schist and Lapis Chloriti. The active ingredients include, by mass: at least 1600 parts of amino acids, at least 120 parts of gallic acid, at least 130 parts of liquiritin, at least 20 parts of liquiritigenin, at least 400 parts of baicalin, at least 40 parts of oroxyloside, at least 120 parts of wogonoside, at least 280 parts of glycyrrhizic acid, at least 12 parts of chrysin-7-O-β-D-glucuronic acid, at least 50 parts of aloe-emodin 8-O-β-D-glucoside, at least 30 parts of chrysophanol-1-O-β-D-glucoside, at least 45 parts of chrysophanol-8-O-β-D-glucoside, at least 260 parts of hyodeoxycholic acid, and at least 150 parts of cholic acid. The composition has antipyretic, anti-inflammatory, antitussive and anti-new coronavirus effects.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
23.
APPLICATION OF TRADITIONAL CHINESE MEDICINE COMPOSITION TO PREPARATION OF MEDICINE FOR TREATING OR PREVENTING CORONAVIRUS INFECTION
Application of a traditional Chinese medicine composition to preparation of a medicine for treating or preventing coronavirus infection. The traditional Chinese medicine composition includes: 5-30 parts of herba houttuyniae, 5-30 parts of flos lonicerae, 5-20 parts of radix paeoniae rubra, 3-15 parts of folium artemisiae argyi and 3-15 parts of herba menthae. The traditional Chinese medicine composition has a good effect of treating or preventing coronavirus-related diseases.
An anti-arrhythmic pharmaceutical composition. The pharmaceutical composition includes: an active ingredient, including 1-(3-methanesulfonamido benzyl)-6-methoxy, 7-benzyloxy-1,2,3,4-tetrahydroisoquinoline or a pharmaceutically acceptable salt thereof; and auxiliary materials, including lactose, microcrystalline cellulose and a pre-gelatinized starch, which account for 30% to 80% of the total weight of the composition. The composition has a good dissolution effect and excellent stability, and can be better applied to clinic.
An application of a traditional Chinese medicine composition in preparing a medicine for treating or preventing coronavirus infection. The traditional Chinese medicine composition is characterized by being prepared from the following raw materials in parts by weight: 5-15 parts of Cornu saigae tataricae or 50-150 parts of goral horns, 10-60 parts of Bulbus Fritillariae Ussuriensis, 15-60 parts of Radix et Rhizoma Rhei, 7-30 parts of Radix scutellariae, 7-30 parts of Lapis Chloriti, 10-50 parts of gypsum fibrosum, 5-20 parts of calculus bovis artifactus, and 15-60 parts of radix glycyrrhizae. The traditional Chinese medicine composition can inhibit 2019-nCoV replication in cells, so that cells infected by 2019-nCoV viruses have no lesion. Therefore, the traditional Chinese medicine composition can treat or prevent coronavirus related diseases.
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (Chine)
JIANGSU KANION PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Liu, Hong
Zhou, Yu
Zhang, Haiyan
Fu, Yan
Li, Jian
Jiang, Hualiang
Tang, Xican
Chen, Kaixian
Abrégé
The present invention provides a crystalline form of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B and crystalline form C of 2-((1-(2-fluorobenzyl)-4-fluoropiperidin-4-yl) methylene)-5, 6-dimethoxy-2, 3-dihydro-1-indanone. The crystalline form of the present invention does not contain water and solvent, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.
This invention involves immunizing mice with human ecto-5′-nucleotidase (CD73) to obtain multiple monoclonal antibodies whose heavy-chain and light-chain sequences are both novel amino acid sequences and which can be used to prepare CD73 enzyme activity inhibitors and anti-tumor drugs.
C07K 16/40 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre des enzymes
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
This invention provides a novel protein. Experimental results have shown that the protein has agonist activity at three receptors, namely the glucagon-like peptide 1 (GLP-1) receptor, the glucose-dependent insulinotropic polypeptide (GIP) receptor, and the glucagon (Gcg) receptor, and has both blood glucose lowering and body weight reducing functions.
This invention provides a protein that is highly effective in lowering blood glucose. Experimental results have shown that the protein can be used to prepare a drug for treating diabetes.
Disclosed is a class of porcupine inhibitors, specifically a compound as represented by formula (I), and a pharmaceutically acceptable salt or an isomer thereof.
Disclosed is a class of porcupine inhibitors, specifically a compound as represented by formula (I), and a pharmaceutically acceptable salt or an isomer thereof.
Disclosed is a crystal form A of a compound. The compound is S-(-)-2,3-methylenedioxy-5,8,13,13a-tetrahydro-10,11-dimethoxy-6H- dibenzo[a,g]quinolizine, and the X-ray powder diffraction pattern of the crystal form A comprises three or more 2θ values selected from the group consisting of: 12.21±0.2°, 13.381±0.2°, 15.181±0.2°, 16.171±0.2°, 17.101±0.2°, 19.801±0.2°, 21.511±0.2°, 24.391±0.2° and 25.321±0.2°. The crystal form A of the compound of the present invention does not contain water and a solvent, has high stability and low hygroscopicity, and is suitable for patent medicine.
C07D 455/03 - Composés hétérocycliques contenant des systèmes cycliques quinolizine, p. ex. alcaloïdes de l'émétine, protoberbérineDérivés alkylènedioxy des dibenzo [a, g] quinolizines, p. ex. berbérine contenant des systèmes cycliques quinolizine directement condensés avec au moins un carbocycle à six chaînons, p. ex. protoberbérineDérivés alkylènedioxy des dibenzo [a, g] quinolizines, p. ex. berbérine
A61K 31/4375 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à six chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. quinolizines, naphtyridines, berbérine, vincamine
A61P 13/08 - Médicaments pour le traitement des troubles du système urinaire de la prostate
32.
MODIFIED RECOMBINANT HUMAN NERVE GROWTH FACTOR AND METHOD FOR PREPARING THE SAME
A modified recombinant human nerve growth factor (modified rhNGF) is obtained from the reaction between a polymer of formula A and an rhNGF. The polymer of formula A is an N-disubstituted amino acetamino aldehyde derivative. Experimental results have shown that the modified rhNGF has a higher in vivo plasma concentration and a longer in vivo half-life than when the rhNGF is not modified or is modified by monomethoxy polyglycol, and that the modified rhNGF preserves the original activity of the unmodified rhNGF. Moreover, the method of preparing the modified rhNGF is low-cost, and the modified products are highly consistent.
A modified recombinant human nerve growth factor (modified rhNGF) is obtained from the reaction between a polymer of formula A and an rhNGF. The polymer of formula A is an N-disubstituted amino acetamino aldehyde derivative. Experimental results have shown that the modified rhNGF has a higher in vivo plasma concentration and a longer in vivo half-life than when the rhNGF is not modified or is modified by monomethoxy polyglycol, and that the modified rhNGF preserves the original activity of the unmodified rhNGF. Moreover, the method of preparing the modified rhNGF is low-cost, and the modified products are highly consistent.
A long-acting preparation made from a protein having the amino acid sequence of SEQ ID NO. 1 or SEQ ID NO. 2 or from a modified protein of the protein for improving sexual dysfunction. The modified protein is the protein molecule connected with another protein or with another chemical substance.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
A61P 15/10 - Médicaments pour le traitement des troubles génitaux ou sexuelsContraceptifs pour l'impuissance
34.
COMPOSITION CAPABLE OF DISPELLING DAMPNESS AND REDUCING FAT, PREPARATION METHOD THEREFOR AND USE THEREOF
A composition capable of dispelling dampness and reducing fat, and a preparation method therefor. The composition comprises by weight: 1 to 20 parts of Poria, 1 to 20 parts of coix seeds, 0.5 to 15 parts of Rhizoma Polygonati, 0.5 to 15 parts of lotus seeds, 0.5 to 15 parts of hawthorn, 0.01 to 10 parts of lotus leaves, and 0.01 to 5 parts of dried tangerine peels. The composition facilitates enterocinesia to dispel dampness, and facilitates fat metabolism to achieve the effect of fat reduction.
A23P 10/28 - Mise en comprimésFabrication de produits alimentaires en barres par compression d’un mélange pulvérulent sec
A23G 3/48 - Sucreries, confiseries ou massepainProcédés pour leur fabrication caractérisés par la composition contenant des végétaux ou des parties de ceux-ci, p. ex. des fruits, des graines, des extraits
A composition having the function of nourishing yin and tonifying the kidney, and a preparation method therefor and the use thereof. The composition comprises, by weight, 1-10 parts of Poria, 1-5 parts of Polygonati rhizoma, 1-5 parts of Mori fructus, 1-9 parts of Dioscoreae rhizoma, 1-8 parts of Chrysanthemi flos, 1-7 parts of Lycii fructus and 1-9 parts of Ginseng radix et rhizome.
Disclosed are a composition with the effect of lowering blood lipids and a preparation method therefor and the use thereof, wherein the composition comprises the following in parts by weight: 2-8 parts of Cistanches herba, 2-10 parts of Salviae miltiorrhizae radix et rhizoma, 1-10 parts of Crataegi fructus and 1-10 parts of Hippophae fructus. The preparation method therefor comprises: (1) mixing the medicinal materials, adding water at 6-20 times the total weight of the raw materials as a extraction solvent, carrying out extraction 1-4 times, each time being 0.5-3 hours, and filtering same to obtain a filtrate; (2) concentrating the filtrate to obtain a concentrated solution, and drying same. The composition can significantly reduce the TC and TG content in the serum of rats, has a certain inhibitory effect on the weight gain of rats, and can significantly increase the level of HDL‑C in the serum of rats, and has the function of lowering blood lipids.
A composition with the function of relieving physical fatigue and a preparation method therefor. The composition comprises the following components in parts by weight: 1-27 parts of Acanthopanacis senticosi radix et rhizoma seu caulis, 1-10 parts of Cistanches herba, 1-6 parts of Panacis quinquefolii radix, and 1-15 parts of Salviae miltiorrhizae radix et rhizoma. Animal experiments have shown that the composition can prolong the loaded swimming time of mice; the loaded swimming experiment results were positive; and any two of the three biochemical indexes of blood lactic acid, serum urea and liver glycogen-muscle glycogen were positive, indicating that the composition has the effect of relieving physical fatigue.
A composition for enhancing immunity, a preparation method for the same, and a drug, health care product or food product containing the composition. The composition comprises: 1 to 8 parts of Cistanche deserticola, 1 to 8 parts of Astragalus membranaceus, 1 to 8 parts of Ligustri lucidi fructus and 1 to 8 parts of Lycii fructus. The composition can enhance delayed hypersensitivity and carbon clearance phagocytic index in mice, and enhance the phagocytosis function of peritoneal macrophages.
A preparation method for a traditional Chinese medicine composition, comprising: taking 2000-4000 parts of Artemisia apiacea, 1000-2500 parts of honeysuckle flowers, and 1000-2000 parts of Fructus Gardeniae; extracting volatile oil from Artemisia apiacea by means of water vapor, collecting the volatile oil, and obtaining a volatile oil composition; adding 6-14 times the amount of water to the dregs fordecoction, filtering, concentrating under reduced pressure, adding ethanol, standing, taking the supernatant, and concentrating under reduced pressure to form a paste; impregnating honeysuckle flowers and Fructus Gardeniae with ethanol, continuing to add ethanol for infiltration, concentrating under reduced pressure, extracting with water saturated n-butanol, and concentrating the extract under reduced pressure to form a paste; and combining the prepared pastes above. The traditional Chinese medicine composition prepared by said method can be prepared into Reduning particles, and is used for preparing a medicament having antipyresis, analgesia, anti-inflammation, anti-bacterial and anti-viral effects or for preparing a medicament for resisting novel coronavirus.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
40.
Salts formed by 2-(1-acyloxy-n-pentyl) benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof
The present disclosure discloses salts formed by 2-(1-acyloxy-n-pentyl)benzoic acid and basic amino acid or aminoguanidine, a preparation method thereof, pharmaceutical preparations containing these salts, and application thereof in preparation of drugs for preventing or treating ischemic cardiovascular and cerebrovascular diseases, resisting thrombosis and improving cardio-cerebral circulation disorders. The compound of the present disclosure has excellent water solubility, aqueous solution stability and pharmacokinetic properties, also has significant anti-platelet aggregation, anti-thrombosis, anti-cerebral ischemia and neuroprotective activity. The compound of the present disclosure has significantly better effects than those of (S)-butylphthalide and potassium (R/S)-2-(1-hydroxy-n-pentyl) benzoate (PHPB), has significantly lower acute toxicity to mice by intravenous injection than that of butylphthalide and PHPB, has a lower inhibition rate of the hERG potassium channel in CHO-hERG cells than that of (S)-butylphthalide, and has a negative result in Bacterial Reverse Mutation Test (Ames test).
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
C07C 227/26 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant des groupes carboxyle par réaction avec HCN, ou un de ses sels, et avec des amines, ou à partir d'aminonitriles
C07C 279/14 - Dérivés de la guanidine, c.-à-d. composés contenant le groupe les atomes d'azote liés par des liaisons simples ne faisant pas partie de groupes nitro ou nitroso ayant des atomes d'azote de groupes guanidine liés à des atomes de carbone acycliques d'un squelette carboné étant substitué de plus par des groupes carboxyle
C07C 281/16 - Composés contenant l'un des groupes p. ex. aminoguanidine
C07D 233/64 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, non condensés avec d'autres cycles comportant deux liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux hydrocarbonés substitués, liés aux atomes de carbone du cycle, p. ex. histidine
A pharmaceutical composition, the pharmaceutical composition comprising: active ingredients, comprising 2-(2-aminopyridin-4-yl)-5-(5-((5-(2-ethyl-2H-tetrazol-5-yl)pyridine- 2-yl)-oxy)-3,3-dimethylpentyl)-1,2,5-thiadiazolidine 1,1-dioxide or a pharmaceutically acceptable salt thereof; and an excipient, comprising a diluent and a suspending agent, the suspending agent comprising povidone. The pharmaceutical composition rapidly dissolves, has good stability and a simple preparation process, and is more suitable for large-scale process production.
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61P 31/14 - Antiviraux pour le traitement des virus ARN
Provided are a composition containing a CD38 antibody or a fragment thereof, and a use of the composition in treating diseases associated with CD38 expression.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
C12N 15/63 - Introduction de matériel génétique étranger utilisant des vecteursVecteurs Utilisation d'hôtes pour ceux-ciRégulation de l'expression
C12N 5/00 - Cellules non différenciées humaines, animales ou végétales, p. ex. lignées cellulairesTissusLeur culture ou conservationMilieux de culture à cet effet
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
Application of a traditional Chinese medicine composition in preparation of drugs for treating or preventing coronavirus infection. The composition is prepared from the following raw materials in parts by weight: 1-3 parts of honey-roasted ephedra, 1-10 parts of bitter almond, 1-6 parts of radix platycodi, 1-6 parts of radix peucedani, 1-6 parts of fritillaria thunbergii, 1-6 parts of radix stemonae, 1-3 parts of oroxylum indicum, 1-10 parts of radix glehniae, and 1-3 parts of licorice. The diluent of the traditional Chinese medicine composition can protect Vero cells infected with 2019-nCoV.
An application of a traditional Chinese medicine composition in preparation of drugs for treating or preventing infection with coronaviruses. The traditional Chinese medicine composition comprises 5-30 parts of All-Grass of Heartleaf Houttuynia, 5-30 parts of Honeysuckle Flower, 5-20 parts of Red Peony Root, 3-15 parts of Leaf of Argy Wormwood, and 3-15 parts of Peppermint. The traditional Chinese medicine composition has a good effect of treating or preventing coronavirus-related diseases.
Disclosed is the use of a traditional Chinese medicine composition in the preparation of a drug for treating or preventing coronavirus infection. The traditional Chinese medicine composition comprises 2-10 parts of Lonicerae japonicae flos, 2-10 parts of Forsythiae fructus, 2-6 parts of Menthae haplocalycis herba, 2-4 parts of Schizonepetae herba, 2-5 parts of Sojae semen praeparatum, 2-6 parts of fried Arctii fructus, 2-6 parts of Platycodonis radix, 2-4 parts of Lophatheri herba and 2-5 parts of Glycyrrhizae radix et rhizoma. The traditional Chinese medicine composition has a great effect on treating or preventing coronavirus-related diseases.
Disclosed is an anti-arrhythmic pharmaceutical composition, characterized in that the pharmaceutical composition comprises an active ingredient, 1-(3-methanesulfonamido benzyl)-6-methoxy, 7-benzyloxy-1,2,3,4-tetrahydroisoquinoline or a pharmaceutically acceptable salt thereof; and auxiliary materials, lactose, microcrystalline cellulose and a pre-gelatinised starch, which account for 30％ to 80％ of the total weight of the composition. The composition has a good dissolution effect and stability, and can be better used in clinical applications.
An application of a traditional Chinese medicine composition in preparation of drugs for treating or preventing coronavirus infection. The traditional Chinese medicine composition is prepared from the following active pharmaceutical ingredients in parts by weight: 5-15 parts of Cornu Saigae Tataricae or 50-150 parts of goat horns, 10-60 parts of Bulbus Fritillariae Ussuriensis, 15-60 parts of Radix et Rhizoma Rhei, 7-30 parts of Baical Skullcap Root, 7-30 parts of Lapis Chloriti, 10-50 parts of Gypsum Fibrosum, 5-20 parts of Calculus Bovis Artifactus, and 15-60 parts of Radix Glycyrrhizae. The traditional Chinese medicine composition can inhibit intracellular replication of 2019-nCoV, will not pathologically alter infected cells, and can treat or prevent related diseases caused by coronavirus infection.
Disclosed is the use of a traditional Chinese medicine composition in the preparation of drugs for treating or preventing coronavirus infection. The traditional Chinese medicine composition is prepared from the following raw material medicines in parts by weight: 5 to 30 parts of Artemisiae annuae herba, 3 to 20 parts of Lonicerae japonicae flos, and 2 to 15 parts of Gardeniae fructus. The traditional Chinese medicine composition can inhibit the replication of 2019-nCoV in VeroE6 cells at a dilution concentration of 1:5000, 1:10,000 and 1:20,000, so that the infected cells do not develop lesions.
A61K 36/736 - Prunus, p. ex. prune, cerise, pêche, abricot ou amande
A61K 47/69 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament le conjugué étant caractérisé par sa forme physique ou sa forme galénique, p. ex. émulsion, particule, complexe d’inclusion, stent ou kit
Ginkgo diterpene lactone composition, indexes, such as SOD, MDA, GSH, and TAC, can be improved to different degrees. For example, after the addition of a certain amount of ginkgolide C, ginkgolide J, and ginkgolide L, the improving effect gets more obvious, the oxidative stress level can be better improved, and the oxidative damage can be relieved.
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (Chine)
JIANGSU KANION PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Liu, Hong
Zhou, Yu
Zhang, Haiyan
Fu, Yan
Li, Jian
Jiang, Hualiang
Tang, Xican
Chen, Kaixian
Abrégé
The present invention provides a crystalline foun of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B and crystalline form C of24(1-(2-fluorobenzy1)-4-fluoropiperidin-4-y1) methylene)-5, 6-dimethoxy-2,3-dihydro-1-indanone. The crystalline form of the present invention does not contain water and solvent, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (Chine)
JIANGSU KANION PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Liu, Hong
Zhou, Yu
Zhang, Haiyan
Fu, Yan
Li, Jian
Jiang, Hualiang
Tang, Xican
Chen, Kaixian
Abrégé
The present invention provides a crystalline form of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B, or crystalline form C of 2-((1-(2-fluorobenzyl)-4-fluoropiperidin-4-yl)methylene)-5,6-dimethoxy-2,3-dihydro-1-indanone.The crystalline form of the present invention does not contain water and solvents, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.
Disclosed are a crystal of a 4-(naphthalene-1-yl)-4H-1,2,4-triazole compound (1) and a preparation method therefor, also comprised are applications of the crystal in preparing a medicament for treating an abnormal uric acid level-related disease.
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
A61K 36/16 - Gynkgophyta, p. ex. Ginkgoaceae (famille du ginkgo)
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
55.
Method for dynamically removing recombinant human nerve growth factor precursor by hydrophobic interaction chromatography
A method for removing precursors in recombinant human nerve growth factor (rhNGF) by hydrophobic interaction chromatography (HIC) is provided, where a Chinese hamster ovary (CHO) cell culture is processed by column chromatography for preliminary purification, and the pretreated sample obtained therefrom is further processed in a HIC column by washing the sample and then eluting the HIC column.
1-5 alkyl group). The method provided in the present invention has a simple method course, and may effectively save time in synthesis and reduce costs, being simple to operate, being easy to implement, and being suitable for industrial production. Experiments show that the emodin succinyl ester compound of the present invention may better promote the healing of diabetic wounds than emodin, and may be used for preparing a drug for promoting the healing of diabetic wounds. Moreover, it has been confirmed by means of performing pharmacological experiments on rats suffering from experimentally mixed hyperlipidemia that the emodin succinyl ester compound of the present invention is superior to emodin, and has the advantages of having a remarkable blood fat lowering effect, being safe, being simple and convenient to administer, the raw materials being low cost and readily available, and being easy to transport and store.
C07C 67/08 - Préparation d'esters d'acides carboxyliques par réaction d'acides carboxyliques ou d'anhydrides symétriques avec le groupe hydroxyle ou O-métal de composés organiques
C07C 67/14 - Préparation d'esters d'acides carboxyliques à partir d'halogénures d'acides carboxyliques
C07C 67/56 - SéparationPurificationStabilisationEmploi d'additifs par traitement solide-liquideSéparationPurificationStabilisationEmploi d'additifs par absorption-adsorption chimique
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
C07C 69/017 - Esters de composés hydroxylés dont le groupe hydroxyle estérifié est lié à un atome de carbone d'un cycle aromatique à six chaînons
C07C 69/675 - Esters d'acides carboxyliques dont le groupe carboxyle estérifié est lié à un atome de carbone acyclique et dont l'un des groupes OH, O-métal, —CHO, céto, éther, acyloxy, des groupes , des groupes ou des groupes se trouve dans la partie acide d'acides saturés d'acides hydroxycarboxyliques saturés
57.
Gene combination capable of high-efficiency expression of recombinant human nerve growth factor
A gene combination capable of high-efficiency expression of rhNGF is provided to optimize gene expression regulation components of a recombinant human nerve growth factor. The gene combination enhances expression of rhNGF. As shown by experiments, the gene combination is capable of high-efficiency expression of a recombinant human nerve growth factor (rhNGF) with natural activity in a eukaryotic expression system.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
A61K 38/18 - Facteurs de croissanceRégulateurs de croissance
58.
CHINESE MEDICINE PRODUCTION PROCESS KNOWLEDGE SYSTEM
A process knowledge system for traditional Chinese medicine production includes a database module having production data acquisition and storage units. The production data acquisition unit acquires process parameter data in production. The parameter data includes quality and process data and is stored in the storage unit. A capability evaluation module evaluates the process capability of the system according to the quality data to obtain a process capability evaluation result. A monitoring feedback module enters a whole-process monitoring mode the process capability is found sufficient. A design space searching module enters a design space searching mode when the process capability is found insufficient. Release parameters are determined or a design space is searched for through process capability evaluation, so that a production process knowledge system stepwise regresses into a knowledge process system capable of realizing intelligent regulation and feedback of the traditional Chinese medicine production process.
G16H 20/90 - TIC spécialement adaptées aux thérapies ou aux plans d’amélioration de la santé, p. ex. pour manier les prescriptions, orienter la thérapie ou surveiller l’observance par les patients concernant des médecines alternatives, p. ex. l’homéopathie ou les médecines orientales
Provided is the use of a ginkgolide composition in the preparation of a drug for treating or preventing acute coronary syndrome. The ginkgolide composition comprises ginkgolides A, B and K at a weight ratio of (20-40):(50-75):(0.2-5).
A61P 9/10 - Médicaments pour le traitement des troubles du système cardiovasculaire des maladies ischémiques ou athéroscléreuses, p. ex. médicaments antiangineux, vasodilatateurs coronariens, médicaments pour le traitement de l'infarctus du myocarde, de la rétinopathie, de l'insuffisance cérébro-vasculaire, de l'artériosclérose rénale
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
Disclosed is a ginkgolide composition for ear diseases, characterized in that the composition comprises ginkgolide A : ginkgolide B : ginkgolide K, wherein the weight ratio of ginkgolide A : ginkgolide B : ginkgolide K is (20-40) : (50-75) : (0.2-5). By means of multiple animal models and some clinical efficacy observation pharmacological experiments, the ginkgolide composition is proved to have effects of improving tinnitus, vertigo, hearing loss, and labyrinth syndrome.
A traditional Chinese medicine composition, made from cassia twig, poria, cortex moutan, radix paeoniae alba, peach kernel in equal proportions. The traditional Chinese medicine composition comprises paeoniflorin, amygdalin, benzoylpaeoniflorin, cinnamic acid, paeonol, and cinnamaldehyde. The composition has the advantages of high production efficiency, high content of effective ingredients, high transfer rate of poria acid, reduced hygroscopicity, and improved dissolution of index ingredients.
A halogenated compound, an axially chiral isomer thereof, and an application thereof in preparing drugs for disorders closely related to aberrant levels of uric acid.
The present invention relates to a gingko diterpene lactone composition. The extract can lower the neurological function score of a cerebral ischemia-reperfusion rat, reduce the cerebral ischemia area and the water content after brain tissue edema, improve SOD activity, and decrease the MDA content; moreover, the composition can inhibit rabbit platelet aggregation induced by PAF and ADP inducers at different time points so as to reduce the maximum aggregation rate; in addition, experiments show that the effect of each monomer compound in the gingko diterpene lactone composition is significantly increased at certain proportion.
The present invention relates to a ginkgo diterpene lactone composition. The composition has the effect of improving a depressive state; the composition can prolong a tail flick interval time and a swimming interval time of a mouse to different degrees and can also increase the frequency of escaping from electric shock to different degrees; moreover, the additional addition of a certain amount of ginkgolide C, ginkgolide J, and ginkgolide L greatly enhances the effect of improving the depressive state. Furthermore, in the present invention, it is further proved through experiments that after the provision of the ginkgo diterpene lactone composition, indexes, such as SOD, MDA, GSH, and TAC, can be improved to different degrees, for example, after the addition of a certain amount of ginkgolide C, ginkgolide J, and ginkgolide L, the improving effect gets more obvious, the oxidative stress level can be better improved, and the oxidative damage can be relieved.
1-51-5 alkyl group). The method provided in the present invention has a simple method course, and may effectively save time in synthesis and reduce costs, being simple to operate, being easy to implement, and being suitable for industrial production. Experiments show that the emodin succinyl ester compound of the present invention may better promote the healing of diabetic wounds than emodin, and may be used for preparing a drug for promoting the healing of diabetic wounds. Moreover, it has been confirmed by means of performing pharmacological experiments on rats suffering from experimentally mixed hyperlipidemia that the emodin succinyl ester compound of the present invention is superior to emodin, and has the advantages of having a remarkable blood fat lowering effect, being safe, being simple and convenient to administer, the raw materials being low cost and readily available, and being easy to transport and store.
C07C 67/14 - Préparation d'esters d'acides carboxyliques à partir d'halogénures d'acides carboxyliques
C07C 67/56 - SéparationPurificationStabilisationEmploi d'additifs par traitement solide-liquideSéparationPurificationStabilisationEmploi d'additifs par absorption-adsorption chimique
C07C 67/30 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester
C07C 69/67 - Esters d'acides carboxyliques dont le groupe carboxyle estérifié est lié à un atome de carbone acyclique et dont l'un des groupes OH, O-métal, —CHO, céto, éther, acyloxy, des groupes , des groupes ou des groupes se trouve dans la partie acide d'acides saturés
C07C 67/08 - Préparation d'esters d'acides carboxyliques par réaction d'acides carboxyliques ou d'anhydrides symétriques avec le groupe hydroxyle ou O-métal de composés organiques
C07C 69/675 - Esters d'acides carboxyliques dont le groupe carboxyle estérifié est lié à un atome de carbone acyclique et dont l'un des groupes OH, O-métal, —CHO, céto, éther, acyloxy, des groupes , des groupes ou des groupes se trouve dans la partie acide d'acides saturés d'acides hydroxycarboxyliques saturés
A61P 17/02 - Médicaments pour le traitement des troubles dermatologiques pour traiter les blessures, les ulcères, les brûlures, les cicatrices, les cheloïdes, ou similaires
A61P 3/10 - Médicaments pour le traitement des troubles du métabolisme de l'homéostase du glucose de l'hyperglycémie, p. ex. antidiabétiques
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
66.
METHOD AND APPARATUS FOR MINING POTENTIAL PROCESS PARAMETERS
Disclosed are a method and apparatus for mining potential process parameters. The mining method comprises: receiving a potential process parameter mining request, the request comprising workshop section condition information corresponding to a design space; obtaining key quality attributes corresponding to a workshop section and drawing up a set of potential process parameters according to the workshop section condition information; performing a first test on the drawn up potential process parameters to obtain a plurality of process parameters; performing a second test on the process parameters to obtain the potential process parameters to be verified; and verifying the potential process parameters to be verified to obtain the potential process parameters. According to the present invention, the potential process parameters to be verified related to the key quality attributes are screened out by testing the potential process parameters, and the design space is updated and optimized by using the potential process parameters to be verified, so as to provide an effective and reliable solution for parametric release.
A process parameter-based result feedback method and apparatus. The feedback method comprises: receiving a result feedback request (S1), the feedback request comprising an intermediate result type; obtaining the process parameters corresponding to the feedback request (S2), the process parameters being multidimensional parameters and constituting a process parameter set; inputting the process parameter set into a result feedback neural network model (S3), the result feedback neural network model being obtained by means of process parameter sample training; and obtaining the output result of the result feedback neural network model (S4). According to the feedback method, by establishing a result feedback neural network model, input parameters in a PKS manufacturing process are classified to determine whether reactants are qualified or not, so as to achieve intelligent feedback.
The present invention discloses an optimization method and device for a system parameter design space. The optimization method comprises: acquiring process parameter data, the process parameters comprising quality parameters of an intermediate product of a previous working section; selecting a type of critical quality attributes according to a working section production condition; screening out process parameters related to the critical quality attributes as critical process parameters; establishing a relation model between the critical process parameters and the critical quality attributes; and acquiring a design space according to the relation model, the design space being a specific range corresponding to the critical quality attributes. The present invention achieves system parameter design space optimization by screening out critical process parameters related to critical quality attributes and establishing a relation model therebetween, and thus provides an effective and reliable solution for parameter release.
An evaluation method and apparatus for manufacturing process capability. The evaluation method comprises: acquiring quality data to obtain a quality sample (S1), the quality data being intermediate performance parameters in a manufacturing process; processing quality sample data to obtain a quality evaluation result (S2); and obtaining a process capability evaluation result according to the quality evaluation result (S3). According to the method, quality data is analyzed in a specific manner to obtain the evaluation of manufacturing process capability as a control guidance basis of a manufacturing process, and a reliable workshop section evaluation system is provided for a process knowledge system according to an initial operation step of using the evaluation result as an entire process knowledge system.
The present invention discloses a Chinese medicine production process knowledge system. The system comprises: a database module comprising a production data acquisition unit and a storage unit, the production data acquisition unit being used for acquiring process parameter data during production, the process parameters comprising quality data and process data, and the storage unit being used for storing the acquired process parameter data; a capability evaluation module for evaluating a system process capability according to the quality data to obtain a process capability evaluation result; a monitoring feedback module for enabling a full-process monitoring mode in response to the evaluation result that the process capability is sufficient; a design space searching module for enabling a design space searching mode according to the process data in response to the evaluation result that the process capability is insufficient. The present invention firstly decides to release parameters or search for a design space by means of process capability evaluation, so that a production process knowledge system is gradually returned to a process knowledge system with a Chinese medicine production process adjusted and fed back intelligently.
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C07D 213/87 - HydrazidesLeurs thio ou imino analogues en position 3
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07B 41/02 - Formation ou introduction de groupes fonctionnels contenant de l'oxygène de groupes hydroxy ou O-métal
C07B 43/04 - Formation ou introduction de groupes fonctionnels contenant de l'azote de groupes amino
72.
SALT FORM AND CRYSTAL FORM OF 1,2,5—THIADIAZOLIDIN-1,1-DIOXIDE, PREPARATION METHOD THEREOF AND INTERMEDIATE
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 213/87 - HydrazidesLeurs thio ou imino analogues en position 3
Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof, and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
74.
A USE OF ALKALOID IN PREPARING PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING PULMONARY FIBROSIS
Disclosed is a new use of a compound as indicated in structural formula I in preparing medications for preventing and/or treating pulmonary fibrosis. The compound having the structure as indicated in structural formula 1 substantially reduces the inflammation of diseased lung tissue, lowers the concentration of fibrosis factors TGF-βΙ in diseased lung tissue, decreases the excessive deposition of collagen in diseased lung tissue, and has substantial prevention and treatment effectiveness against fibrosis.
A61K 31/553 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof, and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
C07D 405/14 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
A61P 31/14 - Antiviraux pour le traitement des virus ARN
76.
RACEMIZATION METHOD OF CHIRAL 2-[(4,6-DIMETHYLPYRIMIDINE-2-YL)OXY]-3-METHOXY-3,3-DIPHENYL PROPIONIC ACID
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (Chine)
Inventeur(s)
Zhang, Fuli
Jin, Linyong
Xiao, Wei
Wu, Taizhi
Wang, Zhenzhong
Guo, Qingming
Zhang, Jun
Zhang, Chenfeng
Abrégé
Provided is a racemization method of a chiral 2-[(4,6-dimethylpyrimidine-2-yl)oxy]-3-methoxy-3,3-diphenyl propionic acid, comprising the following steps: adding a 2-[(4,6-dimethylpyrimidine-2-yl)oxy]-3-methoxy-3,3-diphenyl propionic acid with a high rotation value to a specific solvent; performing the racemization at a specific temperature under stirring for a period of time; and after post-processing, a racemization product with a lower rotation or zero rotation value is obtained.
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY (Chine)
Inventeur(s)
Zhang, Fuli
Jin, Linyong
Xiao, Wei
Wu, Taizhi
Wang, Zhenzhong
Guo, Qingming
Zhang, Jun
Zhang, Chenfeng
Abrégé
The present invention relates to the field of chemical synthesis, and discloses a preparation method of ambrisentan. In the preparation method, using (S)-phenethylamine as a resolving agent, to form two diastereomers with 2-[(4,6-dimethyl pyrimidine-2-yl)oxy]-3-methoxy-3,3-diphenyl propionic acid in a specific solvent; re-crystallising the same to obtain diastereomers with a lower solubility; followed by acid ionization to obtain ambrisentan. The method of the present invention has a yield of about 30%, uses a cheap resolving agent which is easy to obtain and recover, and is suitable for industrialized production.
4-Phenylamino-6-butenamide-7-alkyloxy quinazoline derivatives, the preparative method thereof, the pharmaceutical composition comprising the derivatives, and the use of them in manufacturing medicaments for treatment diseases related to tyrosine protein kinase. The diseases include breast cancer, colorectal cancer, lung cancer and the like.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie
A61P 35/04 - Agents anticancéreux spécifiques pour le traitement des métastases
05 - Produits pharmaceutiques, vétérinaires et hygièniques
30 - Aliments de base, thé, café, pâtisseries et confiseries
Produits et services
Medicines for the treatment of gynecological disease, upper respiratory infection, hyperthermia, head body ache, cough, proliferous spondylitis, cervical vertebra syndrome, spur, loin and leg pain, intervertebral disk herniation, vascular and neurogenic headache, infarction, liver cancer, lung cancer, gastric cancer, kidney cancer and other cancer diseases, moderate cancer pain, coronary heart disease, angina pectoris, chronic superficial gastritis; medicinal drinks, namely, herbal teas for medicinal purposes; pharmaceutical preparations for the prevention of upper respiratory infection, hyperthermia, head body ache, cough, infarction, liver cancer, lung cancer, gastric cancer, kidney cancer and other cancer diseases, moderate cancer pain; drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals; vitamin and mineral preparations for use as ingredients in the food and pharmaceutical industry; Chinese medicines for the treatment of gynecological disease, proliferous spondylitis, cervical vertebra syndrome, spur, loin and leg pain, intervertebral disk herniation, vascular and neurogenic headache, coronary heart disease, angina pectoris, chronic superficial gastritis; biochemical preparations for pharmaceutical medical purposes; blood plasma; biochemical medical preparations for medical or veterinary purposes; liquid nutritional supplements not for medical purposes; powdered nutritional supplements not for medical purposes; nutritional supplement capsules not for medical purposes Tea; chewing gum not for medical purposes; sugar; royal jelly for human food purposes and not for medical purposes; seasonings
05 - Produits pharmaceutiques, vétérinaires et hygièniques
30 - Aliments de base, thé, café, pâtisseries et confiseries
Produits et services
Medicines for the treatment of gynecological disease, upper respiratory infection, hypothermia, head body ache, cough, proliferous spondylitis, cervical vertebra syndrome, spur, loin and leg pain, intervertebral disk herniation, vascular and neurogenic headache, infarction, liver cancer, lung cancer, gastric cancer, kidney cancer and other cancer diseases, moderate cancer pain, coronary heart disease, angina pectoris, chronic superficial gastritis; medicinal drinks, namely, herbal teas for medicinal purposes; pharmaceutical preparations for the prevention of upper respiratory infection, hypothermia, head body ache, cough, infarction, liver cancer, lung cancer, gastric cancer, kidney cancer and other cancer diseases, moderate cancer pain; drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals; vitamin and mineral preparations for use as ingredients in the food and pharmaceutical industry; Chinese medicines for the treatment of gynecological disease, proliferous spondylitis, cervical vertebra syndrome, spur, loin and leg pain, intervertebral disk herniation, vascular and neurogenic headache, coronary heart disease, angina pectoris, chronic superficial gastritis; biochemical preparations for medical purposes, namely, pharmaceutical purposes and medical purposes; blood plasma; biochemical medical preparations for medical or veterinary purposes; liquid nutritional supplements not for medical purposes; powdered nutritional supplements not for medical purposes; nutritional supplement capsules not for medical purposes Tea; chewing gum not for medical purposes; sugar; royal jelly for human food purposes and not for medical purposes; seasonings
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Medicines for the treatment of gynecological diseases, obstetric diseases, bleeding after induced abortion, abdominal pain after insertion of intrauterine contraceptive device, mammary diseases, diseases of the urogenital tract, spondylitis, osteoarthritis, arthritis, painful heel, osteoarthrosis deformans endemica, hemicrania, cluster headache, tensional headache, hyperlipemia, blood hyperviscosity, brain trauma syndrome, vertigo, atherosclerosis, premonitory apoplexy, ischemic apoplexy and its sequela, gastrointestinal disease, deficiency of kidney-yin, lumbago, painful legs, neurasthenia, cardiovascular diseases, cerebrovascular diseases, menopause syndrome, excessive blood lipid, irregular flow of Qi, hypochondriac pain, dysmenorrheal, influenza, inflammation of the upper respiratory tract, pharyngitis, pneumonia and epidemic parotitis, wind-cold headache, pain in the supra-orbital bone, distention and pain due to nasal sinusitis, wind-damp headache and nervous headache; Chinese medicines for the treatment of gynecological diseases, obstetric diseases, bleeding after induced abortion, abdominal pain after insertion of intrauterine contraceptive device, mammary diseases, diseases of the urogenital tract, spondylitis, osteoarthritis, arthritis, painful heel, osteoarthrosis deformans endemica, hemicrania, cluster headache, tensional headache, hyperlipemia, blood hyperviscosity, brain trauma syndrome, vertigo, atherosclerosis, premonitory apoplexy, ischemic apoplexy and its sequela, gastrointestinal disease, deficiency of kidney-yin, lumbago, painful legs, neurasthenia, cardiovascular diseases, cerebrovascular diseases, menopause syndrome, excessive blood lipid, irregular flow of Qi, hypochondriac pain, dysmenorrheal, influenza, inflammation of the upper respiratory tract, pharyngitis, pneumonia and epidemic parotitis, wind-cold headache, pain in the supra-orbital bone, distention and pain due to nasal sinusitis, wind-damp headache and nervous headache; nutritional supplements; baby food; medicinal preparations in liquid form for dissolving cholesterol, medicinal preparations in liquid form for softening and expanding blood vessels, medicinal preparations in liquid form for removing blood lipid, medicinal preparations in liquid form for the treatment of hypertension, hyperlipemia, senile dementia, coronary heart disease, atherosclerosis, hyperlipemia; ginseng for medicinal use; medicinal tea for weight-loss; herbal teas for medicinal purposes; dietary supplement tablets for the use of anti-fatigue, protecting the liver against chemical lesion, improving the blood circulation, smoothing the skin, refreshing the mind, invigorating vital energy, promoting metabolism, improving immunity and regulating bilaterally the functional balance of human body; food supplements; nutritional supplements; nutritionally fortified beverages; and surgical dressings
