10 results about "AIDS drugs" patented technology

This invention provides a method for synthesizing the anti-AIDS drug enovirine. This invention belongs to the field of pharmaceutical preparation technology. The synthesis method includes the following steps: (1) SM1 compound reacts with Grignard reagent and then reacts with SM2 compound to obtain compound III; (2) Compound III undergoes oxidation reaction to obtain compound II; (3) Compound II undergoes demethylation reaction under the action of demethylation reagent to obtain compound I; (4) Compound I undergoes ethylation reaction to obtain enovirine. The synthesis route of this invention effectively avoids the use of highly toxic cyanide reagents and expensive heavy metal catalysts. At the same time, the reaction conditions of this route are simple and mild, with high yield, and have excellent industrialization prospects.

The application discloses a kind of diaromatic pyrimidine compounds containing fused heterocycle and preparation method and application thereof.The compound has the structure shown in general formula I.The application further relates to pharmaceutical compositions containing the compound of formula I.Active screening experiments show that the compound of the application has good anti-HIV and CHIKV activity, and therefore the application further provides the use of the above-mentioned compound in the preparation of anti-AIDS drugs and anti-Chikungunya virus drugs.

The invention provides a synthesis method of an anti-AIDS drug, and belongs to the technical field of drug preparation, the synthesis method comprises the following steps: (1) reacting an SM1 compound with a Grignard reagent, and then reacting with an SM2 compound to obtain a compound shown in a formula III; (2) performing oxidation reaction on the compound in the formula III to obtain a compound in a formula II; (3) performing demethylation reaction on the compound in the formula II under the action of a demethylation reagent to obtain a compound in a formula I; (4) carrying out ethylation reaction on the compound shown in the formula I to obtain enovirin; the synthesis route effectively avoids the use of a highly toxic cyaniding reagent and an expensive heavy metal catalyst, and meanwhile, the route is simple and mild in reaction condition and high in yield, and has an extremely good industrial prospect.

The application provides a 4-quinazolinone derivative containing a benzene sulfonamide piperazine ketone and a preparation method and application thereof. The derivative has the structure shown in the following general formula I. The application further relates to a preparation method of a compound containing the structure of formula I and application of the compound as an HIV-1 / HIV-2 capsid protein regulator in preparation of an anti-AIDS drug.

The invention provides a compound containing an indoleacetamide-fluorophenylalanine-hydroxyproline structure as well as a preparation method and application of the compound. The derivative has a structure as shown in a general formula I. The invention also relates to a preparation method of the compound and application of the compound as an HIV-1 capsid protein degradation agent in preparation of anti-AIDS drugs. # imgabs0 #

The application provides a benzene sulfonamide piperazine ketone glycine derivative and a preparation method and application thereof. The derivative has a structure shown in the following general formula I. The application also relates to a preparation method of a compound containing the structure of formula I and application of the compound as an HIV-1 / 2 capsid protein regulator in preparation of an anti-AIDS drug.

The application provides a kit for anti-AIDS drug detection and a detection method of anti-AIDS drugs, the kit comprises a sample stable control liquid, a mixed internal standard working liquid, a protein precipitant, a special reconstitution solution, a standard and a quality control; the sample stable control liquid comprises a buffer solution containing sodium fluoride and EDTA-2Na. The kit and the detection method provided by the application realize in-vitro stable control of a very low degradation level of prodrug components, guarantee the authenticity of source data of clinical diagnosis, overcome the technical prejudice that weak ionization components cannot be detected by positive ions, significantly improve the detection flux and the quantitative precision of a narrow treatment window, perfectly balance the physical solvent behavior of 'large polarity span' components, completely eliminate the matrix inhibition at dead volume, and establish the highest standard quantitative mechanism of full isotope matching, have very high anti-interference ability and compliance, and can simultaneously quantitatively detect seven anti-AIDS drugs in biological samples.

The application discloses a proteolysis body (PROTAC) targeting HIV protease and application thereof, the PROTAC is a polypeptide structure, a general formula is R1-L-E3L or R1-L-E3L-R2, wherein R1 is a target ligand of HIV protease, L is a GSGS linker, E3L is a ligand of VHL (von Hippel-Lindau) E3 ubiquitin ligase, and R2 is a D-configuration arginine cell penetration peptide; the PROTAC can recruit E3 ligase, specifically induce ubiquitination and degradation of HIV protease in a proteasome-dependent manner; the application further provides a gene encoding the PROTAC, a recombinant carrier, a pharmaceutical preparation and application of the gene in preparation of an anti-AIDS drug.

The application provides an HIV-1 capsid protein degradation agent based on a hydrophobic tag technology and a preparation method and application thereof. The HIV-1 capsid protein degradation agent has the structure shown in general formula I or II. The application further relates to a preparation method of the compound and application of the compound as the HIV-1 capsid protein degradation agent in preparation of an anti-AIDS drug.

The present invention provides a triptolide derivative and a preparation method and application thereof, which belong to the field of pharmaceutical chemistry technology. The triptolide derivative provided by the present invention has a structure shown in formula (I). Pharmacological activity experiments show that the triptolide derivative provided by the present invention and its pharmaceutically acceptable salt or precursor have good inhibitory activity against HIV-1 protease and can be used as an active ingredient of anti-AIDS drugs. The present invention provides a method for preparing the above-mentioned triptolide derivative, which is simple to operate and easy to achieve industrial batch production. Furthermore, the present invention provides an anti-AIDS pharmaceutical composition, comprising an active ingredient and a drug carrier, wherein the active ingredient is the above-mentioned triptolide derivative and its pharmaceutically acceptable salt or precursor. This pharmaceutical composition can be used as an HIV-1 protease inhibitor.