5 results about "Nucleoside Reverse Transcriptase Inhibitor" patented technology

This disclosure provides crystalline forms of a compound of Formula (A), and pharmaceutical compositions thereof. This disclosure further provides methods for their preparation and use in methods of treatment, prophylaxis, or delay in onset or progression of HIV infection or AIDS in a subject. This disclosure further provides dosage forms, such as oral tablets, of a compound of Formula (A) and its crystalline forms.

The invention belongs to the technical field of medicines, and particularly relates to a dihydropteridine-6 (5H)-ketone skeleton compound as well as a preparation method and application thereof. The dihydropteridine-6 (5H)-ketone skeleton compound disclosed by the invention is an HIV-1 (Human Immunodeficiency Virus-1) non-nucleoside reverse transcriptase inhibitor; the invention also comprises pharmaceutical salts, hydrates, solvates, polycrystals or co-crystals of the compounds, precursors and derivatives with the same biological functions of the compounds, a preparation method of the compounds and application of a composition containing one or more of the compounds in preparation of related drugs for treating AIDS and the like. The result of an in-vitro cellular level anti-HIV-1 activity experiment shows that the micromolecule has relatively strong anti-HIV-1 biological activity, can remarkably inhibit virus replication in MT-4 cells infected by HIV-1 viruses, and has relatively low cytotoxicity.

The present invention relates to prodrugs of Compound A: which are nucleoside reverse transcriptase translocation inhibitors (NRTTI) and are useful for inhibiting HIV reverse transcriptase. The invention also relates to the use of these compounds for preventing, treating, and preventing, treating and delaying the onset or progression of AIDS and / or AIDS-related syndromes.

The invention belongs to the technical field of medicines, and particularly relates to a dihydropyridino [3, 4-D] pyrimidine compound as well as a preparation method and application thereof. The dihydropyrido [3, 4-D] pyrimidine compound disclosed by the invention is an HIV-1 (human immunodeficiency virus-1) non-nucleoside reverse transcriptase inhibitor. The invention also discloses pharmaceutical salts, hydrates, solvates, polycrystals or co-crystals of the compounds, precursors and derivatives with the same biological functions of the compounds, a preparation method of the compounds and application of a composition containing one or more of the compounds in related medicines for treating AIDS and the like. An in-vitro cellular level anti-HIV-1 activity experiment result shows that the small molecule compound has relatively strong anti-HIV-1 activity, can effectively inhibit the replication of HIV-1 viruses in MT-4 cells infected by the HIV-1 viruses, and has relatively low cytotoxicity.

The application discloses a kind of S-DACOs non-nucleoside reverse transcriptase inhibitor derivatives and its pharmaceutically acceptable salt, structural formula is as follows: wherein, R a selected from NH2, SO2Me, wherein R1 is selected from H, C1-C6 linear or branched alkyl, alkenyl, R2 is selected from H, C1-C6 linear or branched alkyl, alkenyl;R b selected from H, C1-C3 linear or branched alkyl;The application carries out structural modification to the C-2 terminal benzene ring of S-DACOs, introduces suitable substituent, improves the lipophilic water partition coefficient of drug while retaining high efficient anti-HIV activity, improves its drugability, and the compound of the application can be used for preparing medicine for treating and / or preventing immunodeficiency virus.