110 results about "Anti aids drug" patented technology

The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

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 novel dipeptide compound inhibiting the enzymatic activity of HIV protease, an anti-AIDS medicine comprising this dipeptide compound as an effective component. The dipeptide compound is the compound represented by the formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, and R3 independently represent a linear or branched, saturated or unsaturated lower alkyl group, alkoxyl group, alkyl amino group, or dialkyl amino group having 1-4 carbon atoms (with a carbon atom being either replaced by an oxygen atom or not), a halogeno group, or a hydrogen atom, provided that all of the R1, R2, and R2 are not a hydrogen atom at the same time, R2 and R3 may form a ring together, R4 represents a linear or branched lower alkyl group having 1-4 carbon atoms or a hydrogen atom; X is a methylene group or a sulfur atom; Y represents a five or six member monocyclic or polycyclic hydrocarbon group, a heterocyclic group having a structure in which one or more carbon atom in the monocyclic or polycyclic hydrocarbon group is replaced by a hetero atom, an aryloxy group having 12 or less carbon atoms, in which the aromatic ring may be substituted with an alkyl group, alkoxy group, halogeno group, amino group or hydroxyl group; and Z represents an aliphatic hydrocarbon group having 1-6 carbon atoms or an aromatic hydrocarbon group having 12 or less carbon atoms in which the aromatic ring may be substituted with an alkyl group, alkoxy group, or halogeno group, or one or more carbon atom in the aromatic hydrocarbon group may be replaced by a hetero atom.

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.

The invention discloses a rapid nondestructive identification method of an anti-AIDS drug. According to the method, the Raman reference spectrum database of a standard drug and a drug information database associated with the Raman reference spectrum database are established; a corresponding Raman reference spectrum is obtained according to the source information of a to-be-detected drug, spectrumscanning is performed on the to-be-detected drug by using a Raman spectrometer, so that a Raman to-be-detected spectrum can be obtained; and the Raman to-be-detected spectrum is compared with the corresponding Raman reference spectrum, so that the authenticity of the to-be-detected drug can be determined. The method provided by the invention can scientifically, accurately, simply, conveniently andquickly identify the anti-AIDS drug, will not damage the sample, causes no pollution to the environment, and realizes the rapid nondestructive detection of the drug. The identification method provided by the invention can qualitatively analyze traces and anti-AIDS drugs in order to obtain a stable and reliable analysis result, and is of great significance in the drug research field and the medical health field.

The invention discloses lignans compounds and a preparation method and application thereof. According to the structural formulas of the compounds, R1 is -OH, R2 is -OCH3, a molecular formula is C20H24O8, and one compound is named as marphenol E; and -OCH2O- is between R1 and R2, a molecular formula is C20H22O8, and the other compound is named as marphenol F. According to the preparation method, the lignans 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 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 E and the marphenol F, have good anti-HIV-1 activity, the EC50 values of the two fluorenone compounds are respectively 3.47 microgram / mL and 2.97 microgram / mL, and the therapeutic index (IT) values of the two fluorenone compounds are respectively 21.18 and 27.64. The fluorenone compounds have novel structures and high activity, and can serve as guiding compounds of the anti-AIDS medicines.

The invention discloses an RT / PR dual-target HIV inhibitor, a preparation method and applications thereof. According to the present invention, the RT / PR dual-target HIV inhibitor is prepared from a compound represented by a formula 1, or a pharmaceutically acceptable salt thereof, wherein the compound represented by the formula 1 has obvious inhibition activity on HIV reverse transcriptase and HIVprotease; and the toxicity study results show that the compound has good drug-forming property, such that the compound as the anti-acquired immunodeficiency syndrome drug has good application prospects. The formula I is defined in the specification.

A novel dipeptide compound inhibiting the enzymatic activity of HIV protease and an anti-AIDS medicine comprising this dipeptide compound as an effective component represented by formula (I)wherein R<1>, R<2>, and R<3 >independently represent C1-4 alkyl, alkoxyl, hydrogen etc . . . (provided that not all of the R<1>, R<2>, and R<3 >are hydrogen), R<2 >and R<3 >may form a ring together, R<4 >represents C1-4 alkyl or hydrogen; X is a methylene group or a sulfur atom; Y represents e.g., a five or six member monocycle or aryloxyalkyl having up to 12 carbon atoms (provided that the aromatic ring may be substituted by alkyl etc . . . ); and Z represents a C1-6 aliphatic hydrocarbon or an aromatic hydrocarbon having up to 12 carbon atoms (provided that this aromatic ring may be substituted by alkyl etc . . . , or at least one carbon atom in the aromatic hydrocarbon may be replaced by a hereto atom).

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 provides a nucleic acid base compound or a medically acceptable salt thereof. The compound or the medically acceptable salt thereof has the obvious inhibitory HIV protease and / or reversetranscriptase activity; toxicity studies show that the compound has the good druggability, it is indicated that the compound has a good application prospect by serving as an anti-AIDs drug. Accordingto experimental data, the compound has inhibitory activity on HIV-1 protease and HIV-1 reverse transcriptase, and low cytotoxicity exits. The nucleic acid base compound or the medically acceptable salt thereof is expected to become a double-target inhibitor inhibiting the HIV protease and the reverse transcriptase simultaneously.

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.