30results about How to "Less likely to develop resistance" patented technology

The invention belongs to the fields of medicine and gene engineering, relates to a new medicinal application of epigallocatechin-3-gallate EGCG, and particularly relates to an application of epigallocatechin-3-gallate in the preparation of antitumor drugs. Cell experiments demonstrate that the epigallocatechin-3-gallate is a CYPJ inhibitor, and has the capability of inhibiting liver cancer cell growth; a large dose of EGCG basically has no toxicity to liver, kidney and heart. Experiment results also show that when EGCG is added into a culture solution of tumor cells, the proliferation of tumor cells is inhibited; the tumor cells are blocked at the G1 stage; the activity of CYPJ is inhibited; the activation of an Erk signal path by CYPJ protein is blocked. The epigallocatechin-3-gallate of the invention can be used for the preparation of antitumor drugs, especially anti-liver cancer drugs; and the drugs are designed aiming at cell target points, and drug resistance is not easy to generate.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention relates to the chemical engineering field, which relates to a small molecule compound with anti-HIV activity, the preparation method and the application. The CyPA can combine with Gag polyprotein of the human immunodeficiency virus (HIV-1). Adoption of the RNAi technology silences CypA or inhibits the activity of the CypA which can disturb the replication of the HIV-1 virus. The small molecule compound of the invention is CyPA inhibitor and has the function of resisting the HIV-1 virus, which is designed aiming at the cell targets, does not easily form drug resistance and is suitable for the requirements of the drug use for long life of AIDS sufferers. Therefore, the small molecule compound can be developed as the novel drug resisting the AIDS and provides a novel approach and means for treating and healing the AIDS.

The invention belongs to the gene engineering and chemical field and relates to application of FD4: N-(3-(benzamide)-5-(4-oxo-4H-3,1-benzoxazine-2-yl) phenyl) benzamide to preparing an antitumor drug. The FD4 can obviously inhibit proliferation of tumor cells, is a drug designed aiming to a cell target CYPJ (Cyclophilin J), is not easy to cause the drug resistance and also has special and obvious effect to the tumor cells of a high expression CYPJ protein. Therefore, a small molecular compound is developed as a novel antitumor drug and has obvious tumor killing effect and good specificity, and the FD4 can be developed as the novel antitumor drug and provides a new way and means to treat and cure the tumor.

The invention belongs to the technical field of drug molecules and particularly relates to an application of mycobacterium tuberculosis gene Rv0233 in screening an antituberculous inhibitor target. The gene is characterized in that a nucleotide sequence of the gene is as shown in a sequence table: sequencer (SEQ) ID NO: 1, and a coded protein sequence of the gene is as shown in the sequence table: sequencer (SEQ) ID NO: 2. Eighteen small molecule compounds which have a high affinity with a binding site of natural substrate of Rv0233 screened out from a small molecular compound database through a molecular docking program aiming at an active centre of the natural substrate of the Rv0233 by the way of virtual screening. One bacteriostatic compound (pyrazole compound 51#) is obtained. The name of the compound is 2-({[1-(4-methyl pheny)-H-pyrazol-4-y1] methyl} amino) ethanol. The target gene evaluates the bacteriostatic effect of the compound on the mycobacterium tuberculosis.

The invention discloses a lead compound serving as an ANKRD22 inhibitor and application thereof. The lead compound is a small molecular compound with high affinity with an ANKRD22 natural substrate binding site. The affinity is (1-9)*10<-(5-12)>M. The application comprises the application of the lead compound as an active ingredient as an ANKRD22 inhibitor in preparation of a gastrointestinal mucosa repair protective agent. The invention also discloses application of the pharmaceutical composition in preparation of a tool medicine for researching gastrointestinal mucosa repair function and action mechanism. The ANKRD22 inhibitor provided by the invention has the effects of promoting the proliferation of gastrointestinal mucosa epithelial stem cells and indirectly activating a Wnt classicalpathway, and is beneficial to the rehabilitation of damaged gastrointestinal mucosa tissues of an organism.

The invention discloses a composite plant source water-soluble foliage fertilizer with a bactericidal effect and a preparation method of the foliage fertilizer. The formula comprises 20-35 parts of plant active ingredient extract, 30-40 parts of nutrient elements, 3-5 parts of an emulsifier, 3-5 parts of a synergist, 2-4 parts of a stabilizer, 15-20 parts of ethanol and 7-12 parts of water. The plant active ingredient extract comprises indigowoad leaf extract, extract of radix isatidis, honeysuckle extract, common goldenrop extract, cynanchum komarovii extract, sophora alopecuroids extract, garlic extract, atropa belladonna liquid extract and macleaya cordata extract; the nutrient elements comprise urea, monopotassium phosphate, EDTA (Ethylene Diamine Tetraacetic Acid) chelated iron, EDTAchelated zinc, EDTA chelated boron and ammonium molybdate. The plant active ingredients are extracted by mainly adopting an ultrasonic-assisted extraction method. According to the composite plant source water-soluble foliage fertilizer disclosed by the invention, the toxic substance residues of the conventional chemical pesticides and existence of drug resistance are solved, and the problem that the conventional plant source water-soluble foliage fertilizer is poor in fast-acting property and short in lasting period is solved.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention belongs to the field of gene engineering and chemistry and relates to application of N-[4-(N-{5-[(2,3-dihydro-1H-indene-5-yloxy) methyl]-2-furyl}acethydrazide)phenyl]cyclopentane formamide in preparing an anti-tumor medication. Search of a novel anti-tumor medication with little side effect is a large hot spot in the biomedical field. The N-[4-(N-{5-[(2,3-dihydro-1H-indene-5-yloxy) methyl]-2-furyl}acethydrazide)phenyl]cyclopentane formamide can obviously inhibit proliferation of tumor cells, is designed aiming to a cell target CYPJ protein structure and has specially obvious effect on high expression of CYPJ protein of tumor cells. Therefore, the micromolecule compound is developed as a new anti-tumor medication and has obvious tumor inhibition effect and favorable specificity.

The invention relates to the medical field, in particular to a drug for treating asthma and a preparation method thereof. The drug comprises grapefruit pulp, grapefruit peel, nidus vespae, orange pulp, rosa roxburghii Tratt., rhizoma belamcandae, bulbus fritillariae cirrhosae, olive bark, pitaya peel, peanuts, grosvener siraitia, white turnip, sinapis semen, periostracum cicadae, flos farfarae, climbing groundsel herb, pheretima and a proper amount of deionized water. The drug prepared by using the method is obvious in curative effect and small in side effect and not likely to produce drug resistance; the bulbus fritillariae cirrhosae, the olive bark and the pitaya peel are added into the raw materials, so that the drug has the functions of clearing away the heat and decreasing the internal heat, and the curative effect of drug is improved; the white turnip, the sinapis semen, the periostracum cicadae, the flos farfarae, the climbing groundsel herb and the pheretima are added into theraw materials, so that the drug has the performance of clearing the lung and eliminating phlegm, and the effect on asthma treatment is obviously improved; in the preparation method, extraction is conducted with absolute ethyl alcohol, the effective components of the drug are completely extracted, and the drug properties are higher; meanwhile, sterilization is conducted by using a high-pressure sterilization pot, so that there are no bacteria in the finished drug, bacterial infection is prevented, and the drug effect is easily maintained.

The invention belongs to the field of biological medicines, and in particular relates to application of a micromolecule compound with anti-HIV actively in preparing anti-AIDS medicaments. The invention provides application of N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol in preparing the anti-HIV medicaments. The compound can inhibit CypA actively, the enzyme activity inhibition IC50 value (micron) reaches 3.47 + / - 0.92, and the compound has obvious inhibition to p24 protein of HIV-1 virus. The N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol added to solution containing HIV can inhibit the replication of the HIV. The compound has the ability of inhibiting the replication of the HIV-1 virus, is a medicament designed aiming at a cell target, is not easy to form drug tolerance, and is suitable for the requirement on lifelong medication of AIDS patients.

The invention discloses a drug for preventing and curing H1N1 flu virus by adopting 4 (3H) quinazolone, which relates to the field of drugs for preventing and curing flu, the chemical synthetic drugs for resisting flue virus which are more ideal at present have low selectivity, large adverse reaction and high price and are easy to generate drug resistance after long-term use. The drug adopts monomeric compound 4 (3H) quinazolone extracted from dyers woad leaves; animal experiments, in vitro experiments and clinical experiments show that the drug has good effect of resisting flu virus, wide adaptability, rich drug sources, low cost and low toxic side effects and is not easy to generate drug resistance; the produced dosage forms are tablets, oral liquid and granular formulation; the clinical application dosage of the adult body is 60mg / 60Kg, and the drug is taken for 2-3 times everyday and continuously taken for 5 days.

The invention discloses application of a micromolecular compound with HIV (Human Immunodeficiency Virus) resisting activity to preparing drugs for resisting AIDS, relating to the field of biomedicine. The world health organization (WHO) and governments around the world highly pay attention to AIDS called as present pestilence and super cancer, however, so far, effective drugs capable of curing the AIDS do not exist. The invention provides application of N2,N5-bi[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide to preparing the drugs for resisting the AIDS. The N2,N5-DI[2-(3,4-imethoxyphenyl)ethyl]-2,5-pyridine carboxamide has the capability of inhibiting the replication of HIV-1 virus and is designed by aiming at cell target points without easily generating drug resistance as well as is suitable for the medication demands of the AIDS patients for life.

The invention relates to the bio-medicinal field, and relates to application of a phenylpropylthiophene derivative in preparation of an anti-HIV medicament, in particular to application of a small molecular compound with anti-HIV activity in preparation an anti-HIV medicament. The world health organization and each government pay high attention to HIV named as 'contemporary plague' and 'super cancer', but an effective medicament for healing the HIV is not discovered so far. The invention provides application of 2-({6-[(3-carbonyl-4,5,6,7-tetrahydro-1-phenylpropylthiophene-2-group) amino]-6-oxoacetyl} amine)-4,5,6,7-tetrahydro-1-phenylpropylthiophene-3-formic acid in preparation the anti-HIV medicament. The compound has the capability of inhibiting HIV-1 virus replication, is a medicament designed aiming at a cell target, is not easy to form medicament resistance, and meets the requirement of an AIDS patient for lifelong medication.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention belongs to the field of genetic engineering and chemistry, and relates to application of 4-acetyl diazenyl quinoline in preparing an anti-tumor medicine. Searching for a novel anti-tumor medicine with low side effects is a hot spot in the field of biological medicine. The invention provides application of a micromolecular compound 1-[2-(3-phenelyl)quinoline-4-group]-2-{[4-methoxyl-3-(morpholinomethyl)phenyl]diazene}ethyl ketone in preparing the anti-tumor medicine. The compound can obviously inhibit the proliferation of tumor cells, is designed aiming at the CYPJ protein structure of cell target spots, and particularly has obvious effect on tumor cells with high-expression CYPJ proteins. Therefore, the micromolecular compound is developed by being taken as a novel anti-tumor medicine, and has good anti-tumor effect and good specificity.

The invention belongs to the field of genetic engineering and chemistry, relating to the application of FD1 in preparing antitumor drugs. The invention provides the application of a micro molecular compound, i.e. 2-({6-[(3-carbonyl-4,5,6,7-tetrahydro-1-phenyl thiophene-2-group) amino]-6-oxo-acetyl}amine)-4,5,6,7-tetrahydro-1-phenyl thiophene-3-formic acid (FD1) in preparing the antitumor drugs. The compound can significantly inhibit tumor cell proliferation. FD1 is a drug designed aiming at cell targets CYPJ, and is not easy to form drug resistance, and in addition, the effect is particularly obvious on tumor cells of high expression CYPJ protein. Therefore, the micro molecular compound of the invention is developed as a new antitumor drug, and has obvious antitumor effect and good specificity.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention belongs to the technical field of drug molecules and particularly relates to an application of mycobacterium tuberculosis Rv2780 in screening an antituberculous inhibitor target. The gene is characterized in that a nucleotide sequence of the gene is as shown in a sequence table: sequencer (SEQ) ID NO: 1, and a coded protein sequence of the gene is as shown in the sequence table: sequencer (SEQ) ID NO: 2. Fifteen small molecule compounds which have a high affinity with a binding site of natural substrate of Rv2780 screened out from a small molecular compound database through a molecular docking program aiming at an active centre of the natural substrate of the Rv2780 by the way of virtual screening. Two bacteriostatic compounds (pyrazole compound 22# and nitrine thiophene compound 23#) are obtained. The name of the 22# compound is 3-formyloxy pyridine-2-carboxylate and the name of the 23# compound is 3-nitrine thiophene-2-carboxylate. The target gene evaluates the bacteriostatic effect of the two compounds on the mycobacterium tuberculousis.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention belongs to the biomedicine field and relates to application of a small molecular compound with anti-HIV (Human Immunodeficiency Virus) activity to preparing a drug for treating AIDS (Acquired Immune Deficiency Syndrome). The AIDS called as a contemeporary plague and a super cancer draws great attentions of World Health Organization (WHO) and national governments, however, an effective drug for treating the disease does not exist so far. The invention provides application of N-(3-(benzamide)-5-(4-oxo-4H-3,1-benzoxazine-2-yl) phenyl) benzamide to preparing the drug for treating the AIDS. The compound has the ability of inhibiting HIV-1 virus replication, is a drug designed aiming to a cell target, is not easy to cause the drug resistance and is suitable for the needs of lifelong medication of an AIDS patient.

The invention belongs to the genetic engineering and chemical fields and relates to the application of 4-acetyldiazenequinoline derivative in preparing anti-AIDS drugs. Since AIDS is discovered firstly in 1981, methods and drugs are not developed successfully until now in medical field. The invention provides the application of a small molecular compound of 1-(2-(3-ethoxyphenyl)quinoline-4-yl)-2-((4-methoxyl-3-(morpholinylmethy)phenyl)diazenyl)ethyl ketone in preparing anti-AIDS drugs. A small molecular ligand FD8 screened by the invention has stronger antiviral ability and less toxicity to host cells, thereby being an ideal anti-HIV-1 lead compound.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.

The invention belongs to the field of biological medicines and relates to application of small molecular compound with anti-HIV (Human Immunodeficiency Virus) activity for preparing an antitumor drug. Acquired immunodeficiency syndrome which is called modern plague and super cancer draws close attention from World Health Organization (WHO) and national governments, but, up to now, an effective drug for treating the disease does not exist. The invention provides the application of 4-((3-(((2-naphthoxy)acetyl)hydrazo)butyryl)amine) benzamide for preparing an anti-HIV drug. The compound has the ability of inhibitting HIV-1 virus replication, is the drug designed aiming to a cell target without easy formation of drug resistance and is suitable for demands of lifelong drug application of AIDS (Acquired Immune Deficiency Syndrome) patients.

The invention relates to the technical field of chemical industry, in particular to a preparation method and application of micromolecule compound with HIV resisting activity. CyPA is able to combine with the Gag polymer protein in HIV-1. Silence or inhibit the activity of CypA with RNAi technology and disturb the replication of virus. The micromolecule compound in the invention refers to a CyPA inhibitor that has the effect of resisting HIV-1 virus. Besides, as the micromolecule compound is designed while aiming at cellular target, the invention is not easy to develop drug resistance, thus meeting the demands of lifetime medication for AIDS patients. Therefore, the micromolecule compound in the invention, which can be developed as a new type anti-AIDS drug, provides a new means for treating and curing AIDS.