108 results about "Anti aids drug" patented technology

The present invention relates to one kind of phenolic acid compound and its preparation process and use in treating AIDS. Red sage material is treated through solvent extraction, macroporous adsorbing resin purification, conventional drying and other steps to obtain total phenolic acid. The total phenolic acid is dissolved in water via heating, chromatographic column separation and repeated purification to obtain new compound salvianolic acid N. Enzyme and cell activity experiments show that the new compound has HIV resisting activity and is hopeful in being developed into one new kind of AIDS treating medicine.

A polyose (YCP) sulfate derivative used for preparing anticoagulant, antithrombolic, antioxidizing medicine, antineoplastic medicine and anti-AIDS disease, and its preparing process are disclosed.

The invention relates to a triazolopyrimidine HIV-1 retrovirus inhibitor and its pharmaceutically acceptable salt, ester or prodrug, its preparation method and an application of one compound or a composition of more compounds in the preparation of anti-AIDS drugs.

A method for synthesizing anti - AIDS medicine amprenavir intermediate is related to a synthesis method of a compound, especially for 4-amido-N-((2R,3S)-3-amido-2-hydroxy-4-phenylbutyl)-N-isobutylbenzenesulfamide (amprenavir intermediate), including taking the L-phenylalanine as material, adopting the benzyl protection and esterification, reaction of bromine with CuBr2/DMF, Pd carbon deoxidization to synthesize amprenavir intermediate. We choose the economic means of protecting the amido by benzyl so as to avoid using the benzyl chloroformate. The copper bromide for halogenated use can be reacted in room temperature so as to avoid using the expensive reagent such as chlorobromomethane and chloroiodomethane and produce no pollution to the air. The debenzylation hydrogenation is finished by Pd/C so as to avoid using the expensive palladium dydroxide. The method uses cheaper materials and has a higher yield, which is suitable for commercial process.

The invention discloses a synthetic method of intermediate cyclopropyl acetylene of an anti-aids drug efavirenz, and relates to the technical field of synthesis of cyclopropyl acetylene. The synthetic method comprises the following steps: reacting in an organic solvent to produce alpha, alpha-ethyl dichloride cyclopropane by taking cyclopropyl methyl ketone as a raw material and taking phosphorus pentachloride as a chlorinating agent; and obtaining the cyclopropyl acetylene by adding the alpha, alpha-ethyl dichloride cyclopropane into strong base aqueous liquor through a phase transfer catalyst. The synthetic method has the beneficial effects that the organic solvent and inorganic strong base are not needed to be adopted, expensive reagents such as the organic solvent and potassium tert-butoxide are avoided; moreover, process raw materials are easily available, process is simple, operation is convenient, cost is lowered and the three wastes are reduced, and therefore, the synthetic method is suitable for industrial production.

The invention discloses novel application of an areca fruit and an extract thereof to preparation of anti-AIDS drugs, which belongs to the field of traditional Chinese medicine and natural medicine. The areca fruit is extracted by petroleum ether, ethyl acetate, and normal butanol through alcohol extraction to obtain a petroleum ether extract AB, an ethyl acetate extract AC, and a normal butanol extract AD respectively. The experiment proves that AC and AD parts obtained by extraction have the function of resisting AIDS viruses.

The invention relates to a drug for resisting HIV latency and applications thereof, and specifically relates to the HIV latency resisting effect of oxaliplatin and dilazep and the applications of oxaliplatin and dilazep in preparation of drugs for treating AIDS. Oxaliplatin and dilazep both has the HIV latency resisting effect, can be cooperatively used with antiretroviral drugs to eliminate activated cells that has been subjected to latent infection so as to accelerate the elimination of latent virus reservoir, and can be further used to prepared novel anti-AIDS drugs. The invention provides a novel way for radically curing AIDS.

The invention discloses a preparation method of an anti-AIDS drug Azanavir intermediate and belongs to the technical field of medical biology. The method comprises the steps of adjusting the secondarystructure and codon preference of a gene by means of a full-gene synthesis approach, designing the length of a primer, synthesizing the primer, dissolving the obtained primer in double-distilled water, and adding the obtained solution into a following reaction system; amplifying the prepared PCR reaction system, performing gel cutting purification on DNA fragments obtained by PCR, and selecting amonoclonal sample for sequencing, wherein a correct DNA sequence is shown as SEQ ID NO.1 and named as Sst-1, and an amino acid sequence corresponding to the DNA sequence is shown as SEQ ID NO.2. Thepreparation method has the advantages that the reaction condition is mild, the requirement for equipment is low, high temperature or cooling is not required in a production process, the energy consumption is low, purification is convenient, single-enzyme catalysis is applied in the whole system, the ratio of substrate consumption to NAD consumption reaches 1,540:1, coenzyme circulation frequency is high, and the reaction conditions are mild.

The invention belongs to the field of organic chemical synthesis and particularly relates to a synthesis method of 3-amino-4-methylpyridine which is an intermediate of an anti-AIDS drug nevirapine. According to the method, 4-methylpyridine-3-boronic acid is used as a raw material, an inorganic amide is used as an ammonia source and obtain3-amino-4-methylpyridine is prepared through one-step reaction in the presence of metal oxide as a catalyst. The preparation method is still simple and provides a new way for novel and efficient synthesis of 3-amino-4-methylpyridine and the disadvantages of long traditional route, low yield and severe reaction conditions are overcome.

The invention provides a phenylalanine derivative containing 4-(benzenesulfonyl)piperazine-2-ketone and a preparing method and application of the phenylalanine derivative. The derivative has a structure shown in a formula I. The invention further relates to the preparing method of the derivative and the application of the derivative in preparing anti-AIDS drugs as an HIV-1 inhibitor. The formula Iis shown in the description.

Disclosed is an applocation of an abstract of a plant endogenetic fungi fermentation product for antagonizing immunodeficiency virus(HIV). Said fungi is isolated from the roots of Orchidaceae medicinal herb Dendrobium nobile, and is EF1(Epulorhiza sp.); EF1s are fluid fermentation cultured to prepare an abstract of the fermentation product. The invention is provided with simplicity of fermentation art, short period of production, and mass industrialization production. The abstract of the fermentation product is obtained easily, and has a remarkable anti-HIV-1 activity, the acting site of which is after reverse transcription and before HIV RNA expression, with a regulation action of HIV-1 gene expression. An adding action is obtained by a combined use of the said fungi fermentation product and anti-HIV drug AZT, indicated by a drug combination test. The abstract of the fungi fermentation product has an important value in the development of novle anti-HIV drugs, and is hopefule to become a novel anti-HIV drug.

The invention provides ritonavir water-soluble derivatives, a synthesizing method and application thereof, which relate to a ritonavir water-soluble derivative. Through improving a ritonavir synthesizing route, based on maintaining fundamental drug-effect structure of ritonavir, a pyridine ring is used to replace a benzene ring on a fork chain so as to improve the water solubility of anti-AIDS drugs, such as ritonavir. In the invention, 3 novel ritonavir water-soluble derivatives are synthesized, are estimated to overcome the defect of poor water solubility of the ritonavir based on maintaining the pharmaceutical activity of the ritonavior, and have excellent effect in inhibiting HIV prolease, and can be used for preparing the anti-AIDS drugs.

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 provides an amide derivative or a pharmaceutically acceptable salt thereof with the structure as shown in formula I. A compound or the pharmaceutically acceptable salt thereof has significant activity in inhibiting HIV protease and reverse transcriptase; toxicity study shows that the compound or the pharmaceutically acceptable salt thereof has better druggability, and the compound has better application prospect in using as anti-Aids drugs. According to experimental data, the compound has inhibiting activity both on HIV-1 protease and HIV-1 reverse transcriptase and has lower cytotoxicity. The compound or the pharmaceutically acceptable salt thereof is expected to be a double-target inhibitor which can inhibit the HIV protease and the reverse transcriptase.

This invention relates to the field of pharmaceutical chemistry, involves the preparation method of Intermediate 3-amino-4-methylpyridine (1) of a specific anti-AIDS drugs nevirapine. The feature is it prepared by the 3-halogenated-4-methylpyridine, the preparation method is simple, mild conditions, and the yield is high.

The invention discloses lignans reduction compounds and a preparation method and application thereof. According to the structural formulas of the compounds, R1 is -OH, R2 is -H, a molecular formula is C13H18O7, and one compound is named as marphenol D; and R1 is -OCH3, R2 is -OH, a molecular formula is C14H20O8, and the other compound is named as marphenol E. According to the preparation method, the lignans reduction compounds are prepared from the raw materials including dried branches, leaves and/or fruits of schisandra chinensis. The preparation method comprises the steps of extract extraction, organic solvent extraction, silica column chromatography and high pressure liquid chromatography separation of the raw materials. The invention further discloses the application of the lignans reduction compounds to preparation of anti-AIDS medicines. According to cytotoxicity detection on C8166 host cells and inhibition tests on an HIV-1IIIB-induced cytopathic effect (CPE) of the C8166, the two fluorenone compounds, namely the marphenol D and the marphenol E, have good anti-HIV-1 activity, the EC50 values of the two fluorenone compounds are respectively 3.14 microgram/mL and 3.22 microgram/mL, and the therapeutic index (IT) values of the two fluorenone compounds are respectively 26.91 and 26.13. The fluorenone compounds have novel structures and high activity, have good prospect in preparation of the anti-AIDS medicines, and can serve as guiding compounds of the anti-AIDS medicines.

The invention discloses a drug delivery system for external use containing the effective composition of bullatacin locality drug; the effective composition containing the bullatacin locality drug is dissolved in a mixed liquid of absolute alcohol and propylene glycol and fully stirred and mixed, and then prepared into the drug delivery system for external use; the drug delivery system comprises a patch, an aerosol or a film agent. Adoptions of the natural substance bullatacin extracted from cherimoya and an external using manner of the invention overcomes the shortcoming that the antitumor drugs and anti-AIDS drug have to be orally used or intravenously medicated, and the drug delivery system can ensure the drug to be absorbed through the skin, thus slowly releasing the drug and reducing the delivery dosage of the drug and the economic cost for the treatment.

The invention discloses a directed evolution and biocatalytic application of N-deoxyribosyltransferase II. The invention provides an N-deoxyribosyltransferase II (NDT) mutant. The tenth Gly of the amino acid residue as shown in the Sequence 2 of the sequence table is mutated to Ser, but other amino acid residues are not changed so as to obtain a protein. by sequence alignment of Lactobacillus helveticus-derived NDT (Lh NDT) and Lactobacillus Leichamanni-derived NDT (Ll NDT), homologous modeling is conducted, a saturated mutant library is established, and high throughput screening of 600 mutants is carried out to obtain a Lactobacillus helveticus-derived N-deoxyribosyltransferase II mutant with enzyme activity improved by 10.4 times. The N-deoxyribosyltransferase II mutant provided by the invention can efficiently catalyze the preparation of an anti-AIDs drug zalcitabine.

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 provides 8-amino-7-methyl formate-pyrazine pyridone derivatives and a preparation method and use thereof. The 8-amino-7-methyl formate-pyrazine pyridone derivatives have a structure shown in the following general formula I, wherein R is 4'-cyano-[1,1'-biphenyl]-4-yl, 4'-cyano-[1,1'-biphenyl]-3-yl, 3'-cyano-[1,1'-biphenyl]-4-yl, 4-(pyrimidin-5-yl)phenyl, 3-(pyrimidin-5-yl)phenyl, 3',4'-dimethoxy- 1,1'-biphenyl]-4-yl, 3',4'-dimethoxy-[1,1'-biphenyl]-3-yl, naphthalene-1-yl and [1,1'-biphenyl]-4-yl. The invention also relates to a process for the preparation of such derivatives and their use as HIV inhibitors in the preparation of anti-AIDS drugs.

The invention relates to a preparation method for an intermediate, i.e., 2-chloro-3-amino-4-methylpyridine, of an anti-AIDs drug nevirapine. The intermediate has a chemical structural formula I as described in the specification. The preparation method is characterized in that 4-methylpyridine is subjected to halogenation, ammonia substitution and chlorination so as to prepare 2-chloro-3-amino-4-methylpyridine. The preparation reactions are as shown in the specifications, wherein X is bromine or chlorine; a halogenation condition is Br2/AlCl3/95-105 DEG C, Br2/AlCl3/MBr/110 to 130 DEG C (wherein M is Li, Na or K), Br2/Fe/135-145 DEG C, Cl2/AlCl3, Br2/FeCl3 or Br2/SnCl4; an ammonia substitution condition is NH3(g)/CuSO4/CH3OH/170-190 DEG C, NH3(aq)/CuSO4/170-190 DEG C, or NaNH2; and a chlorination reaction condition is Cl2/AlCl3 or HCl/H2O2/30-50 DEG C.

The invention discloses a hydroxy-pyrimidone compound shown as the general formula (I). In the general formula (I), the R1 represents tertiary butyl, phenyl or substituent phenyl and benzyl; the R2 represents hydrogen or substituent propyl, the R3, R4, R5, R6 and R7 respectively represent hydrogen, methyl, methoxy, hydroxyl or halogen individually, and the n is equal to one or two. The hydroxy-pyrimidone compound has good HIV-1 (human immunodeficiency virus) integrase inhibitory activity and HIV-1 antiviral activity, wherein integrase inhibitory activities IC50(inhibitory concentration) of compounds 5a, 5b, 5c, 5d, 5e, 5i, 5n and 5q are all lower than or equal to 1 micromole, compounds 5a, 5h and 5s have high antiviral activity, and EC50(effective concentration) of the compounds 5a,5h and 5s are respectively 1.72 micromoles, 1.91 micromoles and 1.3 micromoles, and accordingly, the hydroxy-pyrimidone compound can be used for preparing anti-AIDs drugs.