Abstract

A phthalazinone compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound, and a medical use of the compound. The compound of the present invention has a neuroprotective effect and can be used for treating/preventing cerebrovascular-related diseases.

IPC Classes  ?

• C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
• A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
• 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 25/00 - Drugs for disorders of the nervous system

Abstract

The present invention relates to the technical field of medicines, provides a keratin CF5, a preparation method, a pharmaceutical composition containing same, and a use of the keratin CF5, and specifically relates to a keratin CF5, a nucleic acid molecule encoding the keratin CF5, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or the nucleic acid molecule integrated into a genome, a preparation method for the keratin CF5, a pharmaceutical composition containing the keratin CF5, and a use of the keratin CF5, the nucleic acid molecule, the expression vector, the host cell or the pharmaceutical composition in preparation of drugs having antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, antihypertensive, anti-inflammatory and antiviral effects.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans

Abstract

The present invention relates to the technical field of medicines, provides a keratin CF7, a preparation method therefor, a pharmaceutical composition containing same, and a use of keratin CF7, and specifically provides keratin CF7, a nucleic acid molecule encoding keratin CF7, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or the nucleic acid molecule integrated into a genome, a preparation method for keratin CF7, a pharmaceutical composition containing keratin CF7, and a use of keratin CF7, the nucleic acid molecule, the expression vector, the host cell, or the pharmaceutical composition in preparation of drugs having antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, antihypertensive, anti-inflammatory and antiviral effects.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 15/12 - Genes encoding animal proteins
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 31/12 - Antivirals
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 11/14 - Antitussive agents
• A61P 11/10 - Expectorants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 9/12 - Antihypertensives
• C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis
• C07K 1/30 - ExtractionSeparationPurification by precipitation
• C07K 1/16 - ExtractionSeparationPurification by chromatography
• C07K 1/18 - Ion-exchange chromatography
• C07K 1/36 - ExtractionSeparationPurification by a combination of two or more processes of different types
• C12R 1/19 - Escherichia coli

Abstract

The present invention belongs to the technical field of medicine. Provided are a keratin CF8 and a preparation method therefor, and a pharmaceutical composition and the use thereof. Provided are a keratin CF8, a nucleic acid molecule encoding the keratin CF8, an expression vector comprising the nucleic acid molecule, a host cell comprising the expression vector or the nucleic acid molecule integrated in a genome, a method for preparing the keratin CF8, a pharmaceutical composition comprising the keratin CF8, and the use of the keratin CF8, the nucleic acid molecule, the expression vector, the host cell or the pharmaceutical composition in the preparation of antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, antihypertensive, anti-inflammatory and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 15/12 - Genes encoding animal proteins
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 31/12 - Antivirals
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 11/14 - Antitussive agents
• A61P 11/10 - Expectorants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 9/12 - Antihypertensives
• C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis
• C07K 1/30 - ExtractionSeparationPurification by precipitation
• C07K 1/16 - ExtractionSeparationPurification by chromatography
• C07K 1/18 - Ion-exchange chromatography
• C07K 1/36 - ExtractionSeparationPurification by a combination of two or more processes of different types
• C12R 1/19 - Escherichia coli

Abstract

Provided are keratin CF4, a preparation method therefor, a pharmaceutical composition comprising same, and a use thereof, relating to the technical field of medicines. Specifically, provided are keratin CF4, a nucleic acid molecule encoding keratin CF4, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a genome into which the nucleic acid molecule is integrated, a preparation method for keratin CF4, a pharmaceutical composition containing keratin CF4, and a use of keratin CF4, the nucleic acid molecule, the expression vector, the host cell or the pharmaceutical composition in preparation of medications for relieving fever, easing pain, relieving cough, eliminating phlegm, resisting convulsion, resisting epilepsy, reducing blood pressure, resisting inflammation, and resisting viruses.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

The present invention relates to the technical field of medicines. Disclosed are a keratin CF2, a preparation method therefor, a pharmaceutical composition containing same, and a use thereof, and the present invention specifically relates to a keratin CF2, a nucleic acid molecule encoding the keratin CF2, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a genome integrated with the nucleic acid molecule, a preparation method for the keratin CF2, a pharmaceutical composition containing the keratin CF2, and a use of the keratin CF2, the nucleic acid molecule, the expression vector, the host cell or the pharmaceutical composition in preparation of antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, blood pressure lowering, anti-inflammatory and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans

Abstract

The present application relates to the technical field of medicines, and relates to keratin CF1, a preparation method therefor, a pharmaceutical composition comprising same, and a use thereof, and in particular to keratin CF1, a nucleic acid molecule encoding keratin CF1, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a genome into which the nucleic acid molecule is integrated, a preparation method for keratin CF1, a pharmaceutical composition containing keratin CF1, and a use of keratin CF1, the nucleic acid molecule, the expression vector, the host cell or the pharmaceutical composition in preparation of medications for relieving fever, easing pain, relieving cough, eliminating phlegm, resisting convulsion, resisting epilepsy, reducing blood pressure, resisting inflammation, and resisting viruses.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans

Abstract

The present invention belongs to the technical field of medicine. Provided are a pharmaceutical eutectic of bexarotene, and a preparation method therefor and the use thereof. Specifically, disclosed in the present invention are: a method for forming a eutectic from bexarotene and L-arginine in a molar ratio of 1:1 or 1:2 by means of a grinding method; the eutectic retains the pharmacological activity of bexarotene while the melting point of the eutectic is reduced and the solubility of bexarotene is improved; and the use of the eutectic of bexarotene and L-arginine as pharmacological active ingredients in the preparation of a drug for preventing and treating pulmonary hypertension.

IPC Classes  ?

• C07C 63/66 - Polycyclic acids with unsaturation outside the aromatic rings
• A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 9/12 - Antihypertensives

Abstract

The present invention relates to the field of medicine. Disclosed are a compound having an anti-tumor activity, and a preparation method therefor and the pharmaceutical use thereof. Specifically disclosed are a class of compounds containing a tetrahydrocarbazole structure or pharmaceutically acceptable salts thereof, and preparation methods therefor, pharmaceutical compositions containing the compounds and the pharmaceutical use of the compounds. The compound of the present invention has a broad-spectrum anti-tumor effect, and has a strong inhibitory effect on tumor cells such as DOHH2, Pfeiffer, Jurkat and HepG2. In addition, example 10 has relatively high bioavailability and shows relatively strong inhibitory activity on an EMT-6 breast cancer tumor model.

IPC Classes  ?

• C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
• C07D 209/82 - CarbazolesHydrogenated carbazoles
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention belongs to the technical field of antibacterial drugs, and discloses a pyrrolylacylpiperidylamine compound and use thereof. The present invention in particular relates to a pyrrolylacylpiperidylamine compound and a pharmaceutically acceptable salt thereof, and use thereof in the preparation of a medicament for resisting infections with bacteria, mycoplasma or chlamydia. The compound has a structure shown in the following general formula: The present invention belongs to the technical field of antibacterial drugs, and discloses a pyrrolylacylpiperidylamine compound and use thereof. The present invention in particular relates to a pyrrolylacylpiperidylamine compound and a pharmaceutically acceptable salt thereof, and use thereof in the preparation of a medicament for resisting infections with bacteria, mycoplasma or chlamydia. The compound has a structure shown in the following general formula:

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 31/04 - Antibacterial agents
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

Abstract

Provided in the present application are crystal forms of ethoximod, a preparation method therefor and the use thereof. The crystal forms involve a crystal form A and a crystal form B, and the crystal form A and the crystal form B can stably exist, have low hygroscopicity, high solubility, good mechanical stability, low fluidity, relatively low adhesiveness and good compressibility, and thus have medical industrial prospects.

IPC Classes  ?

• C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
• A61P 17/06 - Antipsoriatics

Abstract

The present application provides a crystal form of proximod, a preparation method therefor, and use thereof. The crystal form relates to a crystal form A and a crystal form B. The crystal form A and the crystal form B can stably exist, have low hygroscopicity, high solubility, good mechanical stability, low fluidity, low adhesiveness, and good compressibility, and have pharmaceutical industrialization prospects.

IPC Classes  ?

• C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• A61P 37/02 - Immunomodulators
• A61P 37/04 - Immunostimulants
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione

Abstract

The present invention provides a keratin BD-3, a nucleic acid molecule encoding same, an expression vector, a host cell, a preparation method therefor, and a pharmaceutical composition contained the keratin BD-3. The keratin BD-3 can be used in the preparation of medicament for antipyretic, analgesic, antitussive, expectorant, anticonvulsant, antiepileptic, anti-hypertension, anti-inflammatory, and antiviral.

IPC Classes  ?

• C07K 14/78 - Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli

Abstract

The present invention belongs to the field of biopharmaceuticals. Provided in the present invention are keratin YK93-4, a nucleic acid molecule encoding same, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a host cell having the nucleic acid molecule integrated into the genome, as well as a method for preparing keratin YK93-4 and a pharmaceutical composition of keratin YK93-4. Further provided is the use of the above-described keratin YK93-4 and related products thereof in the preparation of drugs for treating lung cancer, lymphoma, breast cancer, melanoma, uterus myoma, hyperplasia of prostate, etc.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea

Abstract

The present invention belongs to the field of biopharmaceuticals. Provided are a keratin YK93-2, a nucleic acid molecule encoding the same, an expression vector comprising the nucleic acid molecule, a host cell comprising the expression vector or with the genome integrated with the nucleic acid molecule, a preparation method therefor and a pharmaceutical composition thereof. Further provided is the use of the above-mentioned product, such as keratin YK93-2 in the preparation of a drug for treating lung cancer, lymphoma, breast cancer, melanoma, uterine fibroid, prostatic hyperplasia, etc.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea

Abstract

The present invention relates to the field of biological pharmacy, provides keratin YK93-5, a nucleic acid molecule encoding same, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a genome integrated with the nucleic acid molecule, a preparation method for the keratin YK93-5, and a pharmaceutical composition of the keratin YK93-5, and further provides a use of the products such as the keratin YK93-5 in the preparation of drugs for treating lung cancer, lymphoma, breast cancer, melanoma, uterine fibroids, prostatic hyperplasia, etc.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea

Abstract

The present invention pertains to the field of biopharmaceuticals and provides a keratin YK93-9, a nucleic acid molecule encoding same, an expression vector comprising the nucleic acid molecule, a host cell that contains the expression vector or whose genome is integrated with the nucleic acid molecule, a preparation method therefor, and a pharmaceutical composition thereof. The present invention also provides use of the described keratin YK93-9 among other substances in the preparation of medicaments for treating lung cancer, lymphoma, breast cancer, melanoma, uterine myoma, prostate hyperplasia, and the like.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention pertains to the field of biopharmaceuticals and provides a keratin YK93-6, a nucleic acid molecule encoding same, an expression vector comprising the nucleic acid molecule, a host cell that contains the expression vector or whose genome is integrated with the nucleic acid molecule, a preparation method therefor, and a pharmaceutical composition thereof. The present invention also provides use of the described keratin YK93-6 among other products in the preparation of medicaments for treating prostatic hyperplasia, lymphoma, melanoma, pain, lactation disorders, breast cancer, lung cancer, hysteromyoma, coagulation disorders, and the like.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea

Abstract

The present invention belongs to the field of biopharmaceuticals. Provided in the present invention are keratin YK93-8, a nucleic acid molecule encoding same, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a host cell having the the nucleic acid molecule integrated into the genome, as well as a method for preparing keratin YK93-8 and a pharmaceutical composition of keratin YK93-8. Further provided is the use of the above-mentioned keratin YK93-8 and other products in the preparation of drugs, such as a drug for treating hyperplasia of prostate, lymphoma, melanoma, breast cancer, lung cancer and uterine myoma, an analgesic, a lactation drug and a coagulant.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 15/14 - Drugs for genital or sexual disordersContraceptives for lactation disorders, e.g. galactorrhoea

Abstract

Disclosed are a class of lycorine derivatives represented by general formula (I), a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition thereof, and use thereof. The lycorine derivatives have significant antiviral activity and can be used for treating viral diseases.

IPC Classes  ?

• C07D 491/16 - Peri-condensed systems
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Provided are a methylophiopogonone A derivative, and the preparation and the use thereof. The present invention specifically relates to three derivatives of methylophiopogonone A, which derivatives have the chemical structures of formula I, formula II and formula III; and a method for preparing the derivatives, and the use of the derivatives in the preparation of a drug for preventing and/or treating cardiovascular diseases, etc.

IPC Classes  ?

• C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
• A61P 9/06 - Antiarrhythmics
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 9/12 - Antihypertensives

Abstract

The disclosure relates to a pharmaceutical composition having the efficacy of preventing and treating lung injury, a preparation method therefor and a use thereof. The composition comprises a grape powder with a content of 1-25% (w/w), a grape seed extract with a content of 0.5-15% (w/w) and a pharmaceutically acceptable carrier. The composition of the disclosure has the efficacy of preventing and treating lung injury, oxidative injury, inhibiting pulmonary fibrosis, regulating lipid metabolism, and the like.

IPC Classes  ?

• A61K 36/87 - Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/05 - Phenols
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61K 31/355 - Tocopherols, e.g. vitamin E
• A61K 47/42 - ProteinsPolypeptidesDegradation products thereofDerivatives thereof, e.g. albumin, gelatin or zein
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

Provided are a polypeptide containing disulfide bonds and capable of inhibiting activity of serine protease, and a use thereof, relating to three types of linear polypeptide molecules, respectively capable of inhibiting the activity of small intestine protein metabolic enzymes such as trypsin, chymotrypsin, and elastase. Said polypeptide molecules may be broadly fused to another polypeptide or protein drug capable of treating a disease, so as to form a hybrid peptide. The hybrid peptide may inhibit the degradation of metabolic enzymes to improve the stability of a peptide or protein drug for treating a disease, such that the curative effect of direct injection administration is improved, while also facilitating direct administration absorption of the polypeptide or protein drug in the small intestine, and implementing oral administration of the protein polypeptide drug.

IPC Classes  ?

• C07K 14/605 - Glucagons
• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 19/00 - Hybrid peptides
• C07K 14/585 - Calcitonins
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

The present invention belongs to the technical field of medicines, and relates to the technical field of genetic engineering, in particular to use of an intestinal epithelial cell nuclear receptor repressor NCoR as a new target for preventing and treating insulin resistance and obesity-related diseases. Disclosed is use of an intestinal epithelial cell nuclear receptor repressor NCoR as a target in drug screening. Specifically disclosed is use of an intestinal epithelial cell nuclear receptor repressor NCoR as a target in screening or preparing a drug or biological preparation for preventing, relieving, or treating insulin resistance, obesity, and related diseases. Also disclosed is use of the intestinal epithelial cell nuclear receptor repressor NCoR in preparing an insulin sensitization or lipid-lowering mouse model.

IPC Classes  ?

• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/06 - Antihyperlipidemics
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 5/50 - Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
• A61K 49/00 - Preparations for testing in vivo
• C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
• A01K 67/027 - New or modified breeds of vertebrates

Abstract

The present invention belongs to the field of protein engineering, and relates to a hybrid peptide formed by a chymotrypsin inhibitory peptide and insulin or an analogue thereof. The heterozygous insulin analogue can resist the degradation of the chymotrypsin to improve the stability, such that the curative effect of direct injection administration can be improved, and moreover, the insulin analogue can penetrate through small intestine epithelium to be directly absorbed and enter blood circulation, thereby achieving oral administration of the insulin hybrid peptide drug. The present invention further provides a method for preparing a hybrid peptide comprising the chymotrypsin inhibitory peptide and insulin or an analog thereof.

IPC Classes  ?

• C07K 19/00 - Hybrid peptides
• C07K 14/81 - Protease inhibitors
• C07K 14/475 - Growth factorsGrowth regulators
• A61K 38/28 - Insulins
• C07K 1/113 - General processes for the preparation of peptides by chemical modification of precursor peptides without change of the primary structure
• A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis

Abstract

The present invention relates to a compound containing a pyrrolopyrimidine structure or a pharmaceutically acceptable salt of the compound, a preparation method therefor, a pharmaceutical composition containing the compound, and a medical use of the compound. The compound in the present invention has the effect of specifically inhibiting BTK, has a strong inhibitory effect on TMD-8 lymphoma cells, has a relatively high bioavailability, shows a relatively strong inhibitory activity on a TMD-8 tumor model, and can be used for preparing a drug for treating BTK functions-related diseases such as B cell malignant tumors and autoimmune diseases.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are an IMM-H014 sustained-release tablet for treating non-alcoholic fatty liver disease, hepatitis and drug-induced liver disease, and a preparation method therefor. The sustained-release tablet is prepared from an active pharmaceutical ingredient IMM-H014 or a pharmaceutically acceptable salt thereof, a framework material, a diluent, a glidant and a lubricant.

IPC Classes  ?

• A61K 9/22 - Sustained or differential release type
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61K 47/04 - Non-metalsCompounds thereof
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/20 - Antivirals for DNA viruses

Abstract

The present invention provides a keratin BD-6, a nucleic acid molecule encoding keratin BD-6, an expression vector containing the nucleic acid molecule, and a host cell containing the expression vector or the nucleic acid molecule integrated into genome, and preparation method of the keratin BD-6, and a pharmaceutical composition containing the keratin BD-6, and use of the above keratin BD-6, nucleic acid molecule, expression vector, host cell or pharmaceutical composition in the preparation of medicament for antipyretic, analgesic, antitussive, expectorant, anticonvulsant, antiepileptic, anti-hypertension, anti-inflammatory, and antiviral.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• B01D 61/14 - UltrafiltrationMicrofiltration
• C07K 1/16 - ExtractionSeparationPurification by chromatography
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

The present invention provides a keratin BD-11, an encoding nucleic acid molecule, an expression vector, a host cell, a preparation method thereof, and a pharmaceutical composition containing the keratin. The keratin BD-11 can be used in the preparation of medicamnet for antipyretic, analgesic, antitussive, expectorant, anticonvulsant, antiepileptic, anti-hypertension, anti-inflammatory, and antiviral.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• A61P 11/10 - Expectorants
• A61P 11/14 - Antitussive agents
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli

Abstract

Provided are two prostate-specific membrane antigen-targeting fluorescent probes, a method for preparing same and the application thereof. The probes have a good affinity and specificity to prostate cancer cells which express a PSMA. In small-animal in vivo imaging, fluorescence signals can be increased, background signals can be reduced, and a good stability, time resolution and spatial resolution are achieved within a certain time. New specific prostate cancer targeting fluorescent probe molecules are designed and synthesized, thereby greatly improving the specificity and sensitivity of prostate cancer detection; same can be used for testing a prostate cancer clinical sample; and high-precision and high-sensitivity real-time imaging navigation is also provided for an individualized accurate surgery, thereby realizing accurate prostate cancer diagnosis and treatment.

IPC Classes  ?

• C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
• C09K 11/06 - Luminescent, e.g. electroluminescent, chemiluminescent, materials containing organic luminescent materials
• G01N 21/64 - FluorescencePhosphorescence

Abstract

22-induced silicosis mice can inhibit collagen deposition, delay pulmonary fibrosis, and reduce the number and size of silicotic nodules in lung tissue, and the effect is better than that of pirfenidone. The delamanid can be used in preparation of a drug for preventing and/or treating a silicosis disease.

IPC Classes  ?

• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

The present invention provides a keratin BD-10, an encoding nucleic acid molecule, an expression vector, a host cell thereof, a preparation method for BD-10, and a pharmaceutical composition containing the keratin BD-10. Also provides the use of the keratin BD-10, nucleic acid molecule, expression vector, host cell or pharmaceutical composition in the preparation of medicament for antipyretic, analgesic, antitussive, expectorant, anticonvulsant, antiepileptic, anti-hypertension, anti-inflammatory, and antiviral.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli
• A61P 11/14 - Antitussive agents
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 11/10 - Expectorants

Abstract

The present invention belongs to the technical field of protein and genetic engineering, and specifically discloses use of an erythropoietin human hepatocyte receptor B4 as a target in screening and preparing a biological formulation or medicament for increasing sensitivity to insulin. Also disclosed is use of an erythropoietin human hepatocyte receptor B4 in preparing an insulin-sensitized mouse model. On the basis of insulin signal regulation, a protein EphB4 capable of interacting with an insulin receptor (InsR) is found. The protein can interact with InsR, and insulin stimulation can promote the interaction between the two, which provides a basis for insulin resistance in the case of hyperinsulinaemia. Over-expression of EphB4 can promote degradation of InsR. Inhibition of EphB4 can enhance the sensitivity to insulin and improve insulin resistance.

IPC Classes  ?

• A61K 49/00 - Preparations for testing in vivo
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• C12N 9/22 - Ribonucleases
• C12N 15/90 - Stable introduction of foreign DNA into chromosome

Abstract

The invention relates to quinazoline compounds, the preparation method, use, and the pharmaceutical composition thereof. The said quinazoline compounds, which are represented by Formula (I), are phosphatidylinositol 3-kinase (PI3K) inhibitors, and can be applied to prevent and/or treat PI3K activity-related diseases, such as cancer, immune diseases, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders or neurological diseases. The invention relates to quinazoline compounds, the preparation method, use, and the pharmaceutical composition thereof. The said quinazoline compounds, which are represented by Formula (I), are phosphatidylinositol 3-kinase (PI3K) inhibitors, and can be applied to prevent and/or treat PI3K activity-related diseases, such as cancer, immune diseases, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders or neurological diseases.

IPC Classes  ?

• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

The invention relates to quinazoline compounds, the preparation method, use, and the pharmaceutical composition thereof. The said quinazoline compounds, which are represented by Formula (I), are phosphatidylinositol 3-kinase (PI3K) inhibitors, and can be applied to prevent and/or treat PI3K activity-related diseases, such as cancer, immune diseases, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders or neurological diseases. The invention relates to quinazoline compounds, the preparation method, use, and the pharmaceutical composition thereof. The said quinazoline compounds, which are represented by Formula (I), are phosphatidylinositol 3-kinase (PI3K) inhibitors, and can be applied to prevent and/or treat PI3K activity-related diseases, such as cancer, immune diseases, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders or neurological diseases.

IPC Classes  ?

• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

The present invention relates to the technical field of medicines. Specifically disclosed are an indoline derivative, a preparation method therefor, a pharmaceutical composition, and use. In particular, the present invention relates to an indoline derivative as represented by general formula I, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, and a preparation method therefor, a composition containing one or more such compounds, and use of the compound in preparing a drug for treating diseases related to a PD-1/PD-L1 signaling pathway such as cancer, infectious diseases, and autoimmune diseases.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 487/10 - Spiro-condensed systems
• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 35/00 - Antineoplastic agents
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

The present invention relates to a benzamide compound and a preparation method, use and pharmaceutical composition thereof. The benzamide compound represented by formula (I) is a STAT3 inhibitor, and can be used to prevent and/or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic/endocrine dysfunction, and neurological disease. The present invention relates to a benzamide compound and a preparation method, use and pharmaceutical composition thereof. The benzamide compound represented by formula (I) is a STAT3 inhibitor, and can be used to prevent and/or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic/endocrine dysfunction, and neurological disease.

IPC Classes  ?

• C07D 213/53 - Nitrogen atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

A dianthrone compound may be used in preparation of a medicament for prevention and/or treatment of myocardial ischemic diseases and related diseases thereof. The dianthrone compound includes trans-emodin dianthrone and/or cis-emodin dianthrone.

IPC Classes  ?

• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• 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

Abstract

The present invention relates to an osmotic pump controlled-release tablet of an insoluble drug and a preparation method therefor. The osmotic pump controlled-release tablet comprises a tablet core, a semi-permeable membrane coating and a drug-release hole, wherein the tablet core comprises a solid dispersion of the insoluble drug and a penetration enhancer, the solid dispersion of the insoluble drug comprises the insoluble drug and a carrier, the insoluble drug is selected from nicardipine, nifedipine and felodipine and pharmaceutically acceptable salts thereof, and the carrier is selected from organic acids. Compared with the prior art, the drug solubility of the osmotic pump controlled-release tablet of the insoluble drug of the present invention is greatly improved, a large amount of penetration enhancers or other excipients do not need to be used in the tablet core, the drug-loading capacity is improved, and the tablet core is not too large; the degree of release in vivo is greatly improved; and the preparation process is simple, has low requirements for equipment and a low cost, and facilitates industrialized production.

IPC Classes  ?

• A61K 9/22 - Sustained or differential release type
• A61K 9/30 - Organic coatings
• A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61P 9/12 - Antihypertensives

Abstract

Disclosed in the present invention are an inhibitor of 1-methyl-7-chloro-4-((methoxyaryl heteroyl)amino)-N-(arylsulfonyl)-indole-2-carboxamide FBPase having a novel structure, a preparation method therefor, and a pharmaceutical composition and a use thereof. Specifically, the present invention relates to an N-acylsulfonamide FBPase inhibitor and a salt thereof represented by general formula I and general formula II, a preparation method therefor, a composition containing one or more such compounds, a use of such compounds in the preparation of an FBPase inhibitor or a medicament for treating FBPase-related diseases, and a use thereof in the preparation of a drug for preventing and/or treating diabetes.

IPC Classes  ?

• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 235/24 - BenzimidazolesHydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
• C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/04 - Ortho-condensed systems
• A61K 31/404 - Indoles, e.g. pindolol
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/04 - AnorexiantsAntiobesity agents
• 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

Abstract

The invention relates to the field of pharmaceutical chemistry, and it particularly relates to a left-handed bicyclic morpholine and a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and use thereof in the preparation of medicaments for preventing and/or treating liver diseases and the like.

IPC Classes  ?

• C07D 317/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

Disclosed in the present invention are a pyrrole acyl piperylhydrazine compound and the use thereof, which belong to the technical field of antibacterial drugs. Specifically, disclosed are a pyrrole acyl piperylhydrazine compound and a pharmaceutically acceptable salt thereof, and the use thereof in the preparation of antibacterial, anti-mycoplasma-infection or anti-chlamydia-infection drugs. The compound has a structure as shown in the following general formula:

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame

Abstract

The present invention belongs to the field of medical technology and relates to a class of functional small molecules targeting proteolysis pathways, a preparation and an application thereof. Specifically, the present invention relates to functional small molecules represented by formula (M) and pharmaceutically acceptable salts thereof, as well as the application of said compounds and pharmaceutical compositions thereof in the preparation of tumor-treating drugs. The functional small molecules are obtained by means of linking a compound containing a peroxide bridge linkage and a substrate of an E3 ubiquitin ligase complex. The related functional molecules can promiscuously target and bind to multiple proteins comprising functional proteins in the proteolysis pathway and have anti-tumor biological activity. The present invention belongs to the field of medical technology and relates to a class of functional small molecules targeting proteolysis pathways, a preparation and an application thereof. Specifically, the present invention relates to functional small molecules represented by formula (M) and pharmaceutically acceptable salts thereof, as well as the application of said compounds and pharmaceutical compositions thereof in the preparation of tumor-treating drugs. The functional small molecules are obtained by means of linking a compound containing a peroxide bridge linkage and a substrate of an E3 ubiquitin ligase complex. The related functional molecules can promiscuously target and bind to multiple proteins comprising functional proteins in the proteolysis pathway and have anti-tumor biological activity.

IPC Classes  ?

• C07D 493/18 - Bridged systems
• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Provided are keratin BD-4, an encoding nucleic acid molecule thereof, an expression vector, a host cell, and a pharmaceutical composition containing the keratin. The keratin BD-4 can be used for preparing drugs having antipyretic and analgesic, antitussive and expectorant, and antiepileptic effects.

IPC Classes  ?

• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61K 38/00 - Medicinal preparations containing peptides
• A61P 11/10 - Expectorants
• A61P 11/14 - Antitussive agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• C07K 1/36 - ExtractionSeparationPurification by a combination of two or more processes of different types
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/70 - Vectors or expression systems specially adapted for E. coli

Abstract

A use of Prismatomeris connata Y. Z. Ruan root extract in the preparation of medicine for treating pulmonary fibrosis. The extract has effective parts of anthraquinones, anthraquinone glycosides and iridoids. The extract can be used alone or in combination with a chemical agent capable of resisting pulmonary fibrosis, and is prepared into a pharmaceutical composition for treating pulmonary fibrosis.

IPC Classes  ?

• A61K 36/74 - Rubiaceae (Madder family)
• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

Provided are a method for large-scale preparation of acyl/aroyl coenzyme A by an enzymatic method, i.e., using an acyltransferase to transfer acyl/aroyl from a cheap acyl/aroyl donor onto acyl/aroyl receptor coenzyme A, thereby achieving large-scale synthesis of acyl/aroyl coenzyme A, and a use of the method in the preparation of acyl/aroyl coenzyme A.

IPC Classes  ?

• C12N 9/10 - Transferases (2.)
• C12P 17/00 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms

Abstract

The present invention belongs to the technical field of medicine, and relates to a diphenyl alkane compound and a preparation method therefor, and a pharmaceutical composition and the use thereof. Specifically disclosed are a diphenyl alkane compound of formula (I), 1-fluoro-3-methoxy-5-phenethyl benzene (II) and a preparation method therefor, and the use thereof in the preparation of drugs for preventing or treating metabolic syndrome. The compound has a significant effect against metabolic syndrome, and can be used in the clinical treatment of metabolic syndrome in the form of a monomer or pharmaceutical composition.

IPC Classes  ?

• C07C 15/18 - Polycyclic non-condensed hydrocarbons containing at least one group with formula
• C07C 15/16 - Polycyclic non-condensed hydrocarbons containing at least two phenyl groups linked by one single acyclic carbon atom
• C07C 25/18 - Polycyclic aromatic halogenated hydrocarbons
• C07C 17/354 - Preparation of halogenated hydrocarbons by reactions not affecting the number of carbon or halogen atoms in the molecules by hydrogenation
• A61K 31/03 - Halogenated hydrocarbons carbocyclic aromatic
• A61P 3/00 - Drugs for disorders of the metabolism

Abstract

The invention belongs to the technical field of medicine. A soluble berberine-type quaternary ammonium alkaloid compound and the use thereof in preparing a drug are disclosed. In particular, disclosed are a compound as represented by general formula A and a compound that further may be represented specifically by general formulas I and I', a pharmaceutical composition thereof, a preparation method therefor, and the use thereof. The compounds of the present invention have significant activity in treating cardiovascular, cerebrovascular and blood system diseases, inflammatory diseases, febrile diseases, tumor diseases, autoimmune diseases and viral infectious diseases and complications thereof by inhibiting/reducing the activity of biological body pathological NO, iNOS, IL-6 and autoantibody levels, and inhibiting the activity of SARS-COV 2 virus RNA replication. The strength of the physical and chemical properties as well as the pharmacological function of the compounds of the present invention are superior to those of control drugs and related compounds, and can be used for preparing drugs for preventing, alleviating and/or treating cardiovascular, cerebrovascular and blood system diseases, inflammatory diseases, febrile diseases, tumor diseases, autoimmune diseases and viral infection diseases and complications thereof.

IPC Classes  ?

• C07D 455/03 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 3/06 - Antihyperlipidemics
• 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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/12 - Antivirals
• A61P 35/00 - Antineoplastic agents
• A61P 37/02 - Immunomodulators

Abstract

Provided are a cardiovascular disease incidence risk assessment marker based on metabolomic data and an application thereof. Specifically provided is the application of a reagent for detecting metabolite levels in samples from individuals in the preparation of a cardiovascular disease incidence risk assessment apparatus, wherein the metabolites include differential metabolites screened on the basis of metabolomic data of patients with cardiovascular disease and healthy individuals, and at least comprise: pro-tyrosine, 6-phosphoric acid-2-dehydrogluconic acid, retinoic acid, clopidogrel carboxylic acid, leukotriene B4, and 7α-hydroxycholesterol.

IPC Classes  ?

• G01N 30/88 - Integrated analysis systems specially adapted therefor, not covered by a single one of groups

Abstract

Provided is a method for preparing acetyl coenzyme A by enzymatic synthesis using diacerein as a donor. Acetyl coenzyme A is prepared by enzymatic synthesis using optimized maltose-O-acyltransferase (MAT) as a biocatalyst, using diacerein as a donor and using coenzyme A as an acceptor. According to the method, amino acid sequences and nucleotide sequences of MAT and optimized mutants MAT-E125F and MAT-E125Q thereof, and optimum reaction conditions for enzymatic synthesis of acetyl coenzyme A are provided. According to the present invention, the yield of acetyl coenzyme A prepared by catalyzed synthesis of the optimized MAT-E125F and MAT-E125Q can reach 3892.70 mg·mL-1and 3569.44 mg·mL-1, separately.

IPC Classes  ?

• C12P 19/32 - Nucleotides having a condensed ring system containing a six-membered ring having two nitrogen atoms in the same-ring, e.g. purine nucleotides, nicotineamide-adenine dinucleotide
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression

Abstract

The present invention relates to a pharmaceutical composition for preventing and treating lung injuries, and a preparation method therefor and the use thereof, wherein the composition has a grape powder content of 1-25％ (w/w), a grape seed extract content of 0.5-15％ (w/w), and a pharmaceutically acceptable carrier. The composition of the present invention has the effects of preventing and treating lung injuries and oxidative damage, inhibiting pulmonary fibrosis, regulating the lipid metabolism, etc.

IPC Classes  ?

• A61K 36/87 - Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61K 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61K 31/05 - Phenols
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

Provided are a polypeptide containing disulfide bonds and capable of inhibiting activity of serine protease, and a use thereof, relating to three types of linear polypeptide molecules, respectively capable of inhibiting the activity of small intestine protein metabolic enzymes such as trypsin, chymotrypsin, and elastase. Said polypeptide molecules may be broadly fused to another polypeptide or protein drug capable of treating a disease, so as to form a hybrid peptide. The hybrid peptide may inhibit the degradation of metabolic enzymes to improve the stability of a peptide or protein drug for treating a disease, such that the curative effect of direct injection administration is improved, while also facilitating direct administration absorption of the polypeptide or protein drug in the small intestine, and implementing oral administration of the protein polypeptide drug.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 7/64 - Cyclic peptides containing only normal peptide links
• A61K 38/00 - Medicinal preparations containing peptides
• C07K 19/00 - Hybrid peptides

Abstract

The present invention relates to the field of pharmaceutical chemistry. Disclosed are a benzisothiazole compound, and a preparation method therefor and a pharmaceutical composition and use thereof. In particular, the present invention relates to the benzisothiazole compound as shown in general formula I, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, and a preparation method therefor, a composition containing one or more such compounds, and use of the compound in treating a disease related to a PD-1/PD-L1 signaling pathway, such as a cancer, an infectious disease, and an autoimmune disease.

IPC Classes  ?

• C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61P 35/00 - Antineoplastic agents
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

The present invention relates to the technical field of medicine, in particular to a chondroitin sulfate polysaccharide, and a semi-synthetic preparation method therefor and the use thereof. A metal salt of the chondroitin sulfate polysaccharide provided by the present invention has an anti-inflammatory effect, and can be used for preparing a drug against inflammatory diseases. In particular, the metal salt of the chondroitin sulfate polysaccharide provided by the present invention has anti-inflammatory and bone-protecting effects, and can be used for preparing a drug against rheumatoid arthritis and for preparing a drug against osteoarthritis. The present invention provides a method for preparing the metal salt of the chondroitin sulfate polysaccharide, and the metal salt of the chondroitin sulfate polysaccharide with different degrees of sulfation can be obtained by semi-synthetic means in the present invention. The method is simple to operate and suitable for large-scale production.

IPC Classes  ?

• A61K 31/737 - Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof

Abstract

Provided are a substituted pyrazole compound, and a preparation method therefor, the use thereof and a pharmaceutical composition thereof. The pyrazole compound is as represented by formula (I), is a STAT3 signaling pathway inhibitor, and can be used for preventing and/or treating diseases related to STAT3 activity, such as tumors, autoimmune diseases, kidney diseases, cardiovascular diseases, inflammatory diseases, and metabolic/endocrine function disorders or neurological diseases.

IPC Classes  ?

• C07D 231/10 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• C07D 231/40 - Acylated on said nitrogen atom
• A61K 31/415 - 1,2-Diazoles
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 5/00 - Drugs for disorders of the endocrine system

Abstract

The present invention belongs to the technical field of protein and genetic engineering, and specifically discloses use of an erythropoietin human hepatocyte receptor B4 as a target in screening and preparing a biological formulation or medicament for increasing sensitivity to insulin. Also disclosed is use of an erythropoietin human hepatocyte receptor B4 in preparing an insulin-sensitized mouse model. On the basis of insulin signal regulation, a protein EphB4 capable of interacting with an insulin receptor (InsR) is found. The protein can interact with InsR, and insulin stimulation can promote the interaction between the two, which provides a basis for insulin resistance in the case of hyperinsulinaemia. Over-expression of EphB4 can promote degradation of InsR. Inhibition of EphB4 can enhance the sensitivity to insulin and improve insulin resistance.

IPC Classes  ?

• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

Disclosed are berberine represented by structural formula (I), coptisine represented by structural formula (II), berberine active metabolites represented by structural formulas (III), (IV), (V), (VI), (VII), (VIII), and (Ⅸ), including jatrorrhizine, dihydroberberine, thalifendine, berberrubine, demethyleneberberine, palmatine, and columbamine, and application of pharmaceutically acceptable salts thereof in preparation of a medication for preventing and/or treating uric acid nephropathy (gouty nephropathy).

IPC Classes  ?

• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

Abstract

The present invention relates to sheep horn keratin, a preparation method therefor, a pharmaceutical composition containing the keratin, and an application of the keratin and the pharmaceutical composition in the preparation of an antipyretic, analgesic, anticonvulsant, antitussive, expectorant, hypotensive, anti-inflammatory, and antiviral drug. By destuffing, drying, crushing, extracting and purifying a sheep horn, the present invention extracts keratin having antipyretic, analgesic, anticonvulsant, antitussive, expectorant, hypotensive, anti-inflammatory, and antiviral activity and effects. A pharmacological experiment thereof indicates that the sheep horn keratin of the present invention has relatively good antipyretic, analgesic, anticonvulsant, antitussive, expectorant, hypotensive, anti-inflammatory, and antiviral activity in the body.

IPC Classes  ?

• A61K 35/36 - SkinHairNailsSebaceous glandsCerumenEpidermisEpithelial cellsKeratinocytesLangerhans cellsEctodermal cells
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 11/10 - Expectorants
• A61P 11/14 - Antitussive agents
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

2 are described in the specification.

IPC Classes  ?

• C07D 498/04 - Ortho-condensed systems
• A61P 31/06 - Antibacterial agents for tuberculosis
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

The present invention relates to the field of pharmaceutical chemistry, and specifically relates to a left-handed bicyclic morpholine and a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition, and an application thereof in the preparation of drugs for preventing and/or treating liver diseases and the like.

IPC Classes  ?

• C07D 317/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/20 - Antivirals for DNA viruses
• A61P 37/02 - Immunomodulators

Abstract

A cyclic sulfone compound and a preparation method therefor, a pharmaceutical composition thereof and use thereof. Specifically, the cyclic sulfone compound and a pharmaceutically acceptable salt are represented by formula (I), and can be used in the preparation of a CXCR2 antagonist, and can be used in the preparation of a drug for preventing and/or treating CXCR2 receptor-mediated diseases.

IPC Classes  ?

• C07D 335/06 - BenzothiopyransHydrogenated benzothiopyrans
• A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/06 - Antiasthmatics
• A61P 35/00 - Antineoplastic agents
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 25/16 - Anti-Parkinson drugs
• 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

Abstract

An 8-dihalomethyl berberine-type quaternary ammonium salt compound represented by general formula (I) or (II) and an application thereof in preparing a drug. The compound shows hydrophilicity and has antimicrobial, anti-inflammatory, anti-ulcerative colitis, and antitumor activities, while having no or low toxicity.

IPC Classes  ?

• C07D 455/03 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
• A61P 31/04 - Antibacterial agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 31/10 - Antimycotics
• A61P 35/00 - Antineoplastic agents
• C07D 493/14 - Ortho-condensed systems
• C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings

Abstract

The invention relates to quinazoline compounds, the preparation method, use, and the pharmaceutical composition thereof. The said quinazoline compounds, which are represented by Formula (I), are phosphatidylinositol 3-kinase (PI3K) inhibitors, and can be applied to prevent and/or treat PI3K activity-related diseases, such as cancer, immune diseases, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders or neurological diseases.

IPC Classes  ?

• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61P 35/00 - Antineoplastic agents
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

Provided is a keratin BD-1, a nucleic acid molecule encoding the keratin BD-1, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or genome integrating the nucleic acid molecule, and a preparation method for the keratin BD-1, a pharmaceutical composition containing the keratin BD-1, and a use for the keratin BD-1, the nucleic acid molecule, the expression vector, the host cell, or the pharmaceutical composition in the preparation of antipyretic and analgesic, antitussive and phlegm-dispelling, anticonvulsant, antiepileptic, blood pressure reducing, anti-inflammatory, and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

Provided are keratin BD-4, an encoding nucleic acid molecule thereof, an expression vector, a host cell, and a pharmaceutical composition containing the keratin. The keratin BD-4 can be used for preparing drugs having antipyretic and analgesic, antitussive and expectorant, and antiepileptic effects.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

Provided are keratin BD-11, an encoding nucleic acid molecule thereof, an expression vector, a host cell, a preparation method, and a pharmaceutical composition containing the keratin. The keratin BD-11 can be used for preparing drugs having antipyretic and analgesic, antitussive and expectorant, anticonvulsant, anti-epileptic, antihypertensive, anti-inflammatory and antiviral effects.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 9/12 - Antihypertensives
• A61P 11/10 - Expectorants
• A61P 11/14 - Antitussive agents
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/12 - Antivirals

Abstract

Provided are keratin BD-14, a nucleic acid molecule encoding keratin BD-14, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or a genome integrated with the nucleic acid molecule, a preparation method for keratin BD-14, a pharmaceutical composition containing keratin BD-14, and an application of said keratin BD-14, nucleic acid molecule, expression vector, host cell, or pharmaceutical composition in preparing antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, blood pressure lowering, anti-inflammatory and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

The present invention provides keratin BD-15, an encoding nucleic acid molecule thereof, an expression vector, a host cell, a preparation method for the keratin BD-15, and a pharmaceutical composition containing same. Further provided is an application of the keratin BD-15, the nucleic acid molecule, the expression vector, the host cell or the pharmaceutical composition in the preparation of antipyretic and analgesic, antitussive and expectorant, anticonvulsive, antiepileptic, hypotensive, anti-inflammatory, and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

The present invention provides a keratin BD-3, a nucleic acid molecule encoding same, an expression vector, a host cell, a preparation method therefor, and a pharmaceutical composition contained the keratin BD-3. The keratin BD-3 can be used in the preparation of medicamnet for antipyretic, analgesic, antitussive, expectorant, anticonvulsant, antiepileptic, anti-hypertension, anti-inflammatory, and antiviral.

IPC Classes  ?

• A61P 9/12 - Antihypertensives
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

Provided are keratin BD-4, an encoding nucleic acid molecule thereof, an expression vector, a host cell, and a pharmaceutical composition containing the keratin. The keratin BD-4 can be used for preparing drugs having antipyretic and analgesic, antitussive and expectorant, and antiepileptic effects.

IPC Classes  ?

• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression

Abstract

The present invention provides a keratin BD-2, an encoding nucleic acid molecule thereof, an expression vector thereof, a host cell thereof, and a pharmaceutical composition comprising the keratin. The keratin BD-2 can be used for preparing antipyretic and analgesic, antitussive and expectorant, and antiepileptic drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

The present invention provides keratin BD-3, a nucleic acid molecule encoding same, an expression vector thereof, a host cell thereof, a preparation method therefor, and a pharmaceutical composition containing same. The keratin BD-3 can be used to prepare anti-pyretic and analgesic drugs, anti-tussive and expectorant drugs, anti-convulsant drugs, anti-epileptic drugs, anti-hypertensive drugs, anti-inflammatory drugs and anti-viral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

Provided are keratin BD-5, an encoding nucleic acid molecule thereof, an expression vector, a host cell, and a pharmaceutical composition containing the keratin. The keratin BD-5 can be used for preparing drugs having antipyretic and analgesic, antitussive and expectorant, and antiepileptic effects.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

Provided are a keratin BD-6, a nucleic acid molecule encoding the keratin BD-6, an expression vector containing the nucleic acid molecule, a host cell containing the expression vector or genome integrating the nucleic acid molecule, a preparation method for the keratin BD-6, a pharmaceutical composition containing the keratin BD-6, and a use of the keratin BD-6, the nucleic acid molecule, the expression vector, the host cell, or the pharmaceutical composition in preparation of drugs for relieving fever and pain, relieving cough and eliminating phlegm, resisting convulsion, resisting epilepsy, lowering blood pressure, resisting inflammation, and resisting viruses.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

Provided in the present invention are a keratin BD-10, an encoding nucleic acid molecule thereof, an expression vector, a host cell, a preparation method for the keratin BD-10, and a pharmaceutical composition comprising the keratin BD-10. Also provided is use of the keratin BD-10, the nucleic acid molecule, the expression vector, the host cell, or the pharmaceutical composition in the preparation of antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, hypotensive, anti-inflammatory, and antiviral medicines.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

Provided are a keratin BD-13, a coding nucleic acid molecule, expression vector, and host cell thereof and a preparation method therefor, and a pharmaceutical composition containing said keratin. Keratin BD-13 can be used to prepare antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, blood pressure lowering, anti-inflammatory and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 9/12 - Antihypertensives
• A61P 11/10 - Expectorants
• A61P 11/14 - Antitussive agents
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/12 - Antivirals

Abstract

Provided are a keratin BD-17, a nucleic acid molecule encoding the keratin BD-17, an expression vector containing the nucleic acid molecule, a host cell which contains the expression vector or in which the genome integrates the nucleic acid molecule, a method for preparing the keratin BD-17, a pharmaceutical composition containing the keratin BD-17, and applications of the keratin BD-17, the nucleic acid molecule, the expression vector, the host cell, or the pharmaceutical composition in preparing antipyretic and analgesic, antitussive and expectorant, anticonvulsant, antiepileptic, hypotensive, anti-inflammatory, and antiviral drugs.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 15/12 - Genes encoding animal proteins
• C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 31/12 - Antivirals
• A61P 9/12 - Antihypertensives

Abstract

Disclosed are a cornu gorais keratin, a preparation method therefor, a pharmaceutical composition comprising the cornu gorais keratin, and the use of the cornu gorais keratin and the pharmaceutical composition in the preparation of an antipyretic, analgesic, anticonvulsant, antitussive, expectorant, blood pressure-lowering, anti-inflammation, and antiviral drug, wherein the cornu gorais keratin is prepared by means of removing the inclusions, drying, crushing, extracting and purifying.

IPC Classes  ?

• A61K 35/32 - BonesOsteocytesOsteoblastsTendonsTenocytesTeethOdontoblastsCartilageChondrocytesSynovial membrane
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 11/10 - Expectorants
• A61P 9/12 - Antihypertensives
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 31/12 - Antivirals

Abstract

The present invention discloses a type-B crystal form of fenolamine, a preparation method thereof, and a composition and use thereof, more particularly a type-B crystal form of the fenolamine compound (chemical name: trans-2-(2,5-dimethoxyphenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenylethyl)acrylamide, a preparation method thereof, and a composition and use thereof. Specifically, the present invention discloses the presence of a solid of a type-B fenolamine crystal form in solid state; a method for preparing the solid of type-B crystal form; and use of the solid of the type-B fenolamine crystal form as a pharmaceutical active ingredient in the manufacture of a medicament for prevention and treatment of Parkinson's disease (PD), improvement of learning and memory disorder, and treatment of memory loss and Alzheimer's disease (AD).

IPC Classes  ?

• C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms

Abstract

The present invention belongs to the field of medical technology and relates to a class of functional small molecules targeting proteolysis pathways, a preparation and an application thereof. Specifically, the present invention relates to functional small molecules represented by formula (M) and pharmaceutically acceptable salts thereof, as well as the application of said compounds and pharmaceutical compositions thereof in the preparation of tumor-treating drugs. The functional small molecules are obtained by means of linking a compound containing a peroxide bridge linkage and a substrate of an E3 ubiquitin ligase complex. The related functional molecules can promiscuously target and bind to multiple proteins comprising functional proteins in the proteolysis pathway and have anti-tumor biological activity.

IPC Classes  ?

• C07D 498/08 - Bridged systems
• C07D 493/20 - Spiro-condensed systems
• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to the technical field of medicine, and provides a salt of a benzothiopyrone compound, and a preparation method therefor and an application thereof, in particular, a salt of 2-(4-(cyclohexylmethyl)piperazin-1-yl)-6-(trifluoromethyl)-8-nitro-benzothiopyran-4-one as represented by formula (I), a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of a drug for treating and/or preventing an infectious disease caused by Mycobacterium tuberculosis. The present invention aims to prepare a salt of 2-(4-(cyclohexylmethyl)piperazin-1-yl)-6-(trifluoromethyl)-8-nitro-benzothiopyran-4-one having significantly improved pharmacokinetic properties and physicochemical properties and having strong anti-Mycobacterium tuberculosis activity in vivo and in vitro; as a potential novel drug, the salt can be used for treatment or preventive treatment of an infectious disease caused by bacteria, particularly tuberculosis (TB) caused by Mycobacterium tuberculosis, and can also be used for overcoming a problem related to drug resistance of Mycobacterium tuberculosis.

IPC Classes  ?

• C07D 335/04 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
• A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

The present invention relates to the technical field of medicine, and disclosed are maleate of a nicotinyl alcohol ether derivative, a crystal form thereof, and an application thereof, i.e., (S)-N-(2-(pyridine-3-methoxy)-4-(2-bromo-3-phenylbenzyloxy)-5-chlorobenzyl)serine isopropyl ester maleate and a stereoisomer and a crystal form thereof, a preparation method therefor, a pharmaceutical composition, and a use thereof. Specifically, the present invention relates to the (S)-N-(2-(pyridine-3-methoxy)-4-(2-bromo-3-phenylbenzyloxy)-5-chlorobenzyl)serine isopropyl ester maleate represented by formula 1, and a crystal form thereof, a stereoisomer thereof, a preparation method therefor, a composition containing said compound or the crystal form thereof, and a use of said compound or the crystal form thereof in the preparation of a medicine for treating diseases related to a PD-1/PD-L1 signaling pathway, such as cancer, infectious diseases and autoimmune diseases.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 35/00 - Antineoplastic agents
• A61P 31/04 - Antibacterial agents
• A61P 31/12 - Antivirals
• A61P 37/02 - Immunomodulators

Abstract

The present invention relates to a benzamide compound and a preparation method, use and pharmaceutical composition thereof. The benzamide compound represented by formula (I) is a STAT3 inhibitor, and can be used to prevent and/or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic/endocrine dysfunction, and neurological disease.

IPC Classes  ?

• C07D 213/53 - Nitrogen atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present invention relates to the technical field of medicine, and discloses a compound as shown in formula (I) and a preparation method therefor, a pharmaceutical composition and the use thereof. In particular, further disclosed in the present invention are a compound as shown in formula (I), a pharmaceutically acceptable salt and a pharmaceutical composition thereof, wherein same can inhibit the enzymatic activity of a human indoleamine 2,3-dioxygenase (IDO) and/or a human tryptophan 2,3-dioxygenase (TDO), and the use of same in the preparation of a drug for treating and/or preventing diseases or conditions related to excessive activity or overexpression of the IDO/TDO, such as a drug for treating tumors. The compound of the present invention has a strong IDO inhibitory activity. (I)

IPC Classes  ?

• C07C 333/08 - Monothiocarbamic acidsDerivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
• C07D 333/28 - Halogen atoms
• C07D 213/32 - Sulfur atoms
• C07D 219/02 - Heterocyclic compounds containing acridine or hydrogenated acridine ring systems with only hydrogen, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
• C07D 307/38 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
• C07C 333/24 - Esters of dithiocarbamic acids having nitrogen atoms of dithiocarbamate groups bound to carbon atoms of six-membered aromatic rings
• C07D 265/24 - 1,3-OxazinesHydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• A61K 31/536 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Provided is the use of a pharmaceutical composition containing hydroxyurea, wherein the hydroxyurea or a pharmaceutically acceptable salt thereof is used in the preparation of a drug for preventing and/or treating atherosclerosis. Experimental results show: after oral administration of a combination of hydroxyurea, aspirin and clopidogrel bisulfate, fat and porridge-like lesion regions on aortic intima are significantly reduced, the effect on atherosclerosis is obvious (plaque inhibition degree of 85％), the concentrations of blood glucose, triglyceride, total cholesterol, and low-density lipoprotein cholesterol are decreased, and glucose and lipid metabolism disorder is significantly improved; after oral administration of a combination of hydroxyurea, aspirin, clopidogrel bisulfate and atorvastatin calcium, fat and porridge-like lesion regions on aortic intima are further significantly reduced, and atherosclerosis is essentially cured (plaque inhibition degree of 91％). The combinations of drugs at this dose have an outstanding therapeutic effect in the prevention and/or treatment of atherosclerosis.

IPC Classes  ?

• A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
• A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
• 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

Abstract

Disclosed in the present invention are a salicylic acid berberine-type alkaloid quaternary ammonium compound as shown in general formula (I), a preparation method therefor, solubility characteristics, a pharmaceutical composition and an application thereof in the preparation of medicinal products. The salicylic acid berberine-type alkaloid quaternary ammonium compound as shown in general formula (I) may be prepared by an organic synthesis method, and shows obvious solubility of alcohol-water mixed solvents. The compound may be conveniently prepared on a large scale, and has significant anti-ulcerative colitis activity, with non-toxic or low toxicity characteristics. The compound may be used to prepare products for preventing, relieving and/or treating ulcerative colitis.

IPC Classes  ?

• C07D 455/03 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61K 31/04 - Nitro compounds
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to the technical field of medicine, and specifically disclosed thereby are a 1,2,4-triazole compound represented by formula (I) and a physiologically acceptable salt thereof, a preparation method for the compound, a pharmaceutical preparation containing the compound, and an application of the compound in the preparation of drugs for the prevention and treatment of diseases associated with hyperuricemia.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
• C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/4196 - 1,2,4-Triazoles
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents

Abstract

The present invention relates to the technical field of medicines, and specifically disclosed are a quaternized modified taxane derivative, a pharmaceutical composition, and a synthetic pathway and use thereof. The taxane derivative is prepared by taxane and active targeting molecules, i.e., choline or betaine, being subjected to hydroxyl substitution reaction by means of certain linking groups. The taxane derivative has good water solubility and certain tumor targeting, can be metabolized to paclitaxel or docetaxel in a tumor tissue, and as a prodrug strategy, is used as an effective antitumor drug. With respect to paclitaxel, the tumor suppression rate is equivalent at a same dose, but an immune system is not damaged, and toxicity is significantly reduced.

IPC Classes  ?

• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
• A61P 35/00 - Antineoplastic agents
• C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems

Abstract

The present invention relates to the technical field of medicine, in particular to a chondroitin sulfate polysaccharide, and a semi-synthetic preparation method therefor and the use thereof. A metal salt of the chondroitin sulfate polysaccharide provided by the present invention has an anti-inflammatory effect, and can be used for preparing a drug against inflammatory diseases. In particular, the metal salt of the chondroitin sulfate polysaccharide provided by the present invention has anti-inflammatory and bone-protecting effects, and can be used for preparing a drug against rheumatoid arthritis and for preparing a drug against osteoarthritis. The present invention provides a method for preparing the metal salt of the chondroitin sulfate polysaccharide, and the metal salt of the chondroitin sulfate polysaccharide with different degrees of sulfation can be obtained by semi-synthetic means in the present invention. The method is simple to operate and suitable for large-scale production.

IPC Classes  ?

• C08B 37/08 - ChitinChondroitin sulfateHyaluronic acidDerivatives thereof

Abstract

The present invention relates to a quinazoline-2,4-diketone salt compound containing piperazinone as a PARP1/2 inhibitor, a preparation method therefor, a pharmaceutical composition containing the compound, and a combined application of the compound serving as a medicine, especially as an antitumor drug or as a tumor drug sensitizer together with an antitumor drug.

IPC Classes  ?

• C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents

Abstract

Provided herein are a compound acting as FBPase inhibitor, and particularly an N-acyl sulfonamide salt FBPase compound of formula I. Further provided herein are a method for preparing the compound of formula I, one or more compositions made thereof, the compound acting as a drug for treating FBPase-related diseases, and uses of the compound in preparing a drug for preventing and/or treating diabetes.

IPC Classes  ?

• C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 27/02 - Ophthalmic agents
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• 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 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention discloses a type-G crystal form of fenolamine, a preparation method thereof, and a composition and use thereof. In particular, disclosed is a type-G crystal form of the fenolamine compound (chemical name: trans-2-(2,5-dimethoxyphenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenylethyl)acrylamide, a preparation method thereof, and a composition and use thereof. Specifically, the present invention discloses the presence of a solid of a type-G fenolamine crystal form in solid state; a method for preparing the solid of type-G crystal form; and use of the solid of the type-G fenolamine crystal form as a pharmaceutical active ingredient in the manufacture of a medicament for prevention and treatment of Parkinson's disease (PD), improvement of learning and memory disorder, and treatment of memory loss and Alzheimer's disease (AD).

IPC Classes  ?

• C07C 233/22 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

The use of a non-natural ginsenoside in the preparation of an anti-lung cancer or anti-colorectal cancer drug. 3β-O-D-glucopyranosyl-dammara-24-ene-3β,20S-diol or 20S-O-D-glucopyranosyl-dammara-24-ene-3β,20S-diol can treat lung cancer or colorectal cancer effectively.

IPC Classes  ?

• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention involves a method for isolating, by means of salt formation and resolution, a single optically active N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide as shown in formula (III) from four stereoisomers of N-[2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide as shown in formula (I); specifically, a method for isolating N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide from an enantiomeric (RR,SS)N-[2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide, by means of optical resolution by using a tartaric acid derivative or 4-hydroxydinaphtho[2,1-D: 1',2'-F][1,3,2]dioxaphosphepin-4-oxide or a derivative thereof, in particular D-(+)-di-p-methylbenzoyltartaric acid and (-)-4-hydroxydinaphtho[2,1-D: 1',2'-F][1,3,2]dioxaphosphepin-4-oxide, as a resolving agent.

IPC Classes  ?

• C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
• C07B 57/00 - Separation of optically-active organic compounds

Abstract

Disclosed are an 8-dihalide methyl berberine quaternary ammonium compound shown in formulas (I) and (II), a synthetic method therefor, and an application thereof in preparation of drugs. The 8-dihalide methyl berberine quaternary ammonium compound is more hydrophilic than a substrate in the absence of conventional hydrophilic groups. The 8-dihalide methyl berberine quaternary ammonium compound has a remarkable anti-microbial activity, anti-inflammatory activity and anti-ulcerative colitis activity, can explicitly and significantly regulate target molecules, associated with tumor formation, in tumor cells of the colon cancer, liver cancer, lung cancer, breast cancer, osteosarcoma, and glioma, and has anti-tumor activity. The pharmacological action of the compound of the present invention is higher than that of a control drug. Moreover, the compound has the characteristics of nontoxicity or hypotoxicity, and can be used for preparing drugs for preventing, alleviating, and/or treating microbiological contamination, inflammation, ulcerative colitis, and tumors.

IPC Classes  ?

• C07D 455/03 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 35/00 - Antineoplastic agents

Abstract

An 8-dihalomethyl berberine-type quaternary ammonium salt compound represented by general formula (I) or (II) and an application thereof in preparing a drug. The compound shows hydrophilicity and has antimicrobial, anti-inflammatory, anti-ulcerative colitis, and antitumor activities while having no or low toxicity.

IPC Classes  ?

• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61P 31/04 - Antibacterial agents
• A61P 31/10 - Antimycotics
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a benzamide compound and a preparation method, use and pharmaceutical composition thereof. The benzamide compound represented by formula (I) is a STAT3 inhibitor, and can be used to prevent and/or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic/endocrine dysfunction, and neurological disease.

IPC Classes  ?

• A61K 31/18 - Sulfonamides
• A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
• A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
• A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
• C07D 213/32 - Sulfur atoms
• C07D 405/02 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings

Abstract

The present invention relates to a benzamide compound and a preparation method, use, and pharmaceutical composition thereof. The benzamide compound is represented by formula (I), is a STAT3 inhibitor, and can be used to prevent and/or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic/endocrine dysfunction, and neurological disease.

IPC Classes  ?

• C07D 213/32 - Sulfur atoms
• C07D 405/02 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
• A61K 31/18 - Sulfonamides
• A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
• A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
• A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin

Abstract

122 being shown in the specifications. The present invention aims at preparing a new compound for resisting against the activity of mycobacterium tuberculosis; and as a new potential drug, the compound can be used for overcoming the problems related to drug resistance of mycobacterium tuberculosis.

IPC Classes  ?

• C07D 207/30 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
• C07D 401/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
• C07D 403/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings
• C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
• A61K 31/402 - 1-aryl-substituted, e.g. piretanide
• A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
• A61P 31/04 - Antibacterial agents
• A61P 31/06 - Antibacterial agents for tuberculosis

Abstract

Disclosed are an FLZ crystal B form, a preparation method, and a composition and the use thereof, in particular the crystal B form of an FLZ compound (I) (chemical name: trans-2-(2,5-dimethoxyphenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenyl-ethyl)acrylamide), a preparation method therefor, and the composition and the use thereof. In particular, disclosed are the crystal B form solid matter of FLZ in a solid state; the method for preparing the crystal B form solid matter; and the use of the FLZ crystal B form solid matter as a pharmaceutically active ingredient in the preparation of a preventive drug for resisting Parkinson's disease (PD), improving learning and memory disorders, treating memory ability decline and Alzheimer's disease (AD).

IPC Classes  ?

• C07C 233/17 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
• C07C 233/01 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• A61P 25/16 - Anti-Parkinson drugs
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide