72 results about "AIDS drugs" patented technology

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.

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 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 relates to a method for analyzing and detecting a new anti-AIDS drug ACC007. The method comprises the following steps of respectively adding 2.0 mL of an acetic acid-sodium acetate buffer solution with a pH value of 3.38-5.35, a proper amount of an ACC007 sample solution to be detected and 40-200 [mu] L of an ionic liquid in a centrifuge tube of 10.0 ml ; adding distilled water to scale marks, performing ultrasonic treatment for 3-25min, cooling the centrifuge tube to 0-4 DEG C, keeping the temperature at 0-4 DEG C for 10-20min, centrifuging with a centrifuge for 3-10min, layering, removing an upper-layer aqueous solution, and diluting a lower-layer ionic liquid phase with ethanol to 10mL to obtain a to-be-detected liquid; (2) detecting, taking the to-be-detected liquid obtained in the step (1), and detecting by using an ultraviolet-visible spectrophotometer to obtain absorbance; and (3) calculating the content, substituting the absorbance measured in the step (2) into aworking curve equation to obtain the content of ACC007.

The invention discloses a diarylpyrimidine compound containing a six-membered nitrogen heterocyclic ring as well as a preparation method and application of the diarylpyrimidine compound. The compoundhas a structure as shown in a general formula I in the specification. The invention also relates to a pharmaceutical composition containing the compound with the structure shown in the formula I. Activity screening experiments show that the compound provided by the invention has good anti-HIV1 activity, so that the invention also provides application of the compound in preparation of anti-AIDS drugs.

The invention provides a diarylpyrimidine derivative substituted by a 5-site aromatic ring. The diarylpyrimidine derivative has a structure as shown in a general formula I which is described in the specification. The invention also relates to a preparation method of the derivative and application of the derivative as an HIV inhibitor in preparation of anti-AIDS drugs.

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.

The invention relates to a monoaromatic miazine HIV-1 reverse transcriptase inhibitor containing triazole rings and a preparation method and application thereof. The compound has the structure shown as the formula I or II. The invention further relates to a drug composition containing the compound of the formula I or II. The compound and the application of the composition containing one or more compounds of this kind in preparation of anti-AIDS drugs are further provided.

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 discloses a method for asymmetric synthesis of an anti-Aids drug, namely an efavirenz key intermediate. The method comprises the following steps that in an organic solvent, fluoride, anorganic ligand (9S)-6'-methoxy-deoxidized cinchonine-9-ol and cyclopropyl acetylene are evenly stirred, an organic zinc solution is slowly added at the temperature of 15-25 DEG C, after constant-temperature stirring is conducted for 3-5 hours, tetraisopropyl titanate is added, stirring is continued to be conducted for 2-3 hours, then the temperature is decreased to minus 20 DEG C to 0 DEG C, 5-chloro-2-amino-trifluorobenzophenone is added, a mixture is stirred at the temperature of minus 20 DEG C to 0 DEG C for 5-12 hours, after a reaction is completed, a proton source is added for a quenchingreaction, then a certain amount of activated carbon is added, a mixture is stirred for 0.5 hour and filtered, an organic phase and a water phase are separated in an extraction mode, the organic phaseis washed, dried and subjected to vacuum concentration, and after purification, the efavirenz key intermediate is obtained. The technological process is short, the technological condition is mild, operation is easy, environmental protection is achieved, the cost is low, and the method is suitable for industrial production.

The invention discloses a 2,4,5-trisubstituted pyrimidine compound taking HIV-1 reverse transcriptase as a target spot as well as a preparation method and application thereof. The compound has a structure as shown in a general formula I in the specification. The invention also relates to a pharmaceutical composition containing the compound with the structure shown in the formula I. Activity screening experiments show that the compound provided by the invention has good anti-HIV-1 activity, so that the invention also provides application of the compound in preparation of anti-AIDS drugs.

The invention provides a phenylalanine derivative containing benzothiadiazine-3-ketone 1,1-dioxide and a preparation method and an application thereof. The derivative has a structure as shown in the following general formula I. The invention also relates to a preparation method of the derivative and the application of the derivative as an HIV-1 inhibitor in preparation of anti-AIDS drugs.

The invention relates to 4-(substituted-1,3-dialkynyl)-4-(trifluoromethyl)benzo-1,4-dihydroxazole-2-one compounds and a preparation method and applications thereof. The preparation method is as follows: substituted-2-(2-(4-methoxybenzylamino)phenyl)-1,1,1-trifluoro-3,5-hexyne-2-ol reacts with phosgene in organic solvent at the temperature ranging from -20 DEG C to 30 DEG C under the action of alkali; after the reaction, the pressure is reduced to remove solvent, and then the obtained product reacts with ammonium ceric nitrate in organic solvent to obtain the target compounds. In the method, bialkynyl group is introduced in 4-trifluoromethylbenzo-1,4-dihydroxazole-2-one, the synthesis method is simple and practical and has high yield; and the compounds are used to prepare anti-HIV drugs oranti-HBV drugs or anti-HCV drugs and have better application value. The anti-HIV drugs are anti-AIDS drugs; the anti-HBV drugs are anti-hepatitis B drugs; and the anti-HCV drugs are anti-hepatitis C drugs. The structural general formula of the compounds of the invention is shown as below.

The invention provides a pyranoindole compound as well as a preparation method and an application thereof in preparation of anti-aids drugs. The pyranoindole compound has a structure as shown in a formula I. The pyranoindole compound, or a pharmacologically acceptable salt, isomer, raceme, prodrug cocrystal compound, aquo-complex or solvate thereof is capable of effectively activating an HIV virus repository, can be used for treating aids, and is simple in preparation method and wide in application prospect, and industrialized production is easy to implement.

The invention provides a diarylpyrimido pyridone derivative. The diarylpyrimido pyridone derivative has a structure shown as general formula I in the specification. The invention also relates to a preparation method of the derivative and application of the derivative as an HIV inhibitor in preparation of anti-AIDS drugs.