24 results about "Reverse-transcriptase inhibitor" patented technology

The invention belongs to the technical field of medicines, and particularly relates to pyrrolo [2, 3-d] pyrimidine compounds of aryl fragments and piperidine fragments as well as a preparation method and application of the pyrrolo [2, 3-d] pyrimidine compounds. The pyrrolo [2, 3-d] pyrimidine compound containing the aryl fragment and the piperidine fragment is an HIV-1 reverse transcriptase inhibitor, and the pyrrolo [2, 3-d] pyrimidine compound further comprises pharmaceutical salt, hydrate and solvate of the pyrrolo [2, 3-d] pyrimidine compound, polycrystal or eutectic of the pyrrolo [2, 3-d] pyrimidine compound, and precursors and derivatives with the same biological functions of the pyrrolo [2, 3-d] pyrimidine compound. The invention also relates to a preparation method of the compound and application of a composition containing one or more of the compounds in related medicines 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.

Cell culture media comprising luteinizing hormone, follicle-stimulating hormone and at least one histone acetyltransferase inhibitor or reverse transcriptase inhibitor are provided. Methods of in vitro maturing a human oocyte, determining suitability for in vitro maturation, as well as kits comprising media, luteinizing hormone, follicle-stimulating hormone and at least one histone acetyltransferase inhibitor or reverse transcriptase inhibitor are also provided.

Described herein are methods for inhibiting generation of one or more non-classical variant(s) of amyloid precursor protein (APP) gene. Provided herein are methods for diagnosing an individual having or suspected of having Alzheimer's disease following identification of an expression profile or an activity profile of the one or more non-classical variant(s) and treating the individual using a reverse transcriptase inhibitor or salt thereof.

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 a method of treating inflammation in a mammal in need thereof that involves providing a mammal with elevated host endogenous reverse transcriptase produced by host endogenous retroviruses (ERVs), and thereafter contacting in vivo the reverse transcriptase with a reverse transcriptase inhibitor in an amount sufficient to ameliorate ERV- induced inflammatory response.

The present disclosure provides methods for treating HBV infection using combination therapies in patients with serum HBsAg levels below 3000 IU / mL prior to treatment. The components of the combination therapies may include one or more of an anti-HBV antibody; an siRNA that targets an HBV mRNA; interferon-α; and a nucleos(t)ide reverse transcriptase inhibitor (NRTI).

A combination comprising a tricycle compound and use thereof in the preparation of a medicament for treating HBV. The combination is a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof and any one drug in the following groups a-c: a. a hepatitis B surface antigen inhibitor, b. a reverse transcriptase inhibitor, and c. a hepatitis B surface antigen inhibitor and a reverse transcriptase inhibitor.

Disclosed is a method for preventing, delaying or reversing age-associated inflammation, by administering to a patient in need thereof a therapeutically effective amount of at least one reverse transcriptase inhibitor (RTI).

The present disclosure provides methods for treating hepatitis D virus (HDV) infection and / or an HDV-associated disease using combination therapies, and related kits and compositions for use in such methods. The components of the combination therapies may include one or more of an anti-HBV antibody; an siRNA that targets an HBV mRNA; and a nucleos(t)ide reverse transcriptase inhibitor (NRTI).

The present invention relates to compositions for use in the treatment, management or amelioration of FMRI mediated autism and Fragile X Syndrome (FXS), wherein the composition comprises one or more non-nucleoside reverse transcriptase inhibitors (NNRTIs). The invention also relates to one or more NNRTIs for use as medicaments for treating a range of autistic diseases, diseases having an autistic component and behavioural disorders.

The present disclosure provides methods for treating hepatitis D virus (HDV) infection and / or HDV-related diseases using combination therapies, as well as related kits and compositions for use in such methods. The components of the combination therapy can include one or more of an anti-HBV antibody, an siRNA targeting HBV mRNA, and a nucleos(t)ide reverse transcriptase inhibitor (NRTI).

The present invention discloses a pharmaceutical composition containing homoharringtonine and its application in the preparation of anti-HIV viral drugs. The pharmaceutical composition is composed of homoharringtonine and a nucleoside reverse transcriptase inhibitor or a non-nucleoside reverse transcriptase inhibitor. The nucleoside reverse transcriptase inhibitor is selected from one of the compounds zidovudine, lamivudine, and abacavir, and the non-nucleoside reverse transcriptase inhibitor is selected from one of the compounds nevirapine, efavirenz, and rilpivirine. The pharmaceutical composition has a significant synergistic effect in treating HIV, improves the efficacy of the drug, reduces the dosage of a single drug, reduces toxic side effects, and can significantly inhibit the production of viruses in combination, producing a very significant antiviral effect, and improving the current status of the treatment of HIV-1, especially middle and late stage AIDS.

Disclosed here is an adenosine derivative prodrug that can have reverse transcriptase inhibitor activity in vivo. This disclosure is also directed to a pharmaceutical composition comprising the adenosine derivative that can be used for the treatment of HIV infection or RNA virus infection.

The present invention relates to an improved process for the preparation of (((1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl)(phenoxy)phosphoryloxy)methyl pivalate Compound (1) or its pharmaceutically acceptable salts thereof. The compound is useful as nucleotide reverse transcriptase inhibitor in therapy for diseases which respond to inhibition of protein kinase activity in humans in need thereof.

The present application provides a combination of an siRNA agent and a reverse transcriptase inhibitor and a use thereof in treating hepatitis B. The present application specifically relates to a drug combination of an siRNA agent and tenofovir or a pharmaceutically acceptable prodrug thereof or a pharmaceutically acceptable salt thereof, a drug combination of an siRNA agent and entecavir or a pharmaceutically acceptable salt thereof or a solvate thereof, and a pharmaceutical use thereof.

To provide new HBV therapies that are effective, well tolerated, and do not require lifelong administration.SOLUTION: The present invention provides a method for treating HBV infection using an siRNA that targets an HBV gene. In one embodiment, the method for treating HBV includes co-administration of the siRNA and PEG-INFα, and may further include administration of a nucleoside / nucleotide reverse transcriptase inhibitor (NRTI).SELECTED DRAWING: Figure 22

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 present invention discloses a method for preventing, delaying or reversing age-related inflammation by administering a therapeutically effective amount of at least one reverse transcriptase inhibitor (RTI) to a patient in need thereof.

The invention relates to a carbonyl-substituted pyrimidine derivative as well as a preparation method and application thereof, and belongs to the technical field of organic compound synthesis and medical application. The carbonyl-substituted pyrimidine derivative has a structure as shown in a formula I. The carbonyl-substituted pyrimidine derivative disclosed by the invention is novel in structure and shows good anti-HIV-1 activity as an HIV-1 inhibitor, and the EC50 value of the carbonyl-substituted pyrimidine derivative ranges from 4.28 nM to 274 nM and is obviously superior to that of a drug nevirapine (EC50 = 281 + / -38.7 nM) on the market.

The present invention belongs to the field of medicinal chemistry, and relates to a pharmaceutical combination containing a capsid protein inhibitor or a pharmaceutically acceptable salt thereof and a reverse transcriptase inhibitor or a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt or a solvate thereof. Specifically, the present invention relates to a pharmaceutical combination of a capsid protein inhibitor or a pharmaceutically acceptable salt thereof and entecavir or tenofovir, or a pharmaceutically acceptable prodrug thereof, or a pharmaceutically acceptable salt or a solvate thereof, or the use thereof in the treatment of hepatitis B virus infection. The pharmaceutical combination has a good anti-hepatitis B virus infection effect.

The present disclosure provides methods for treating HBV infection using combination therapies, and related kits and compositions for use. The components of the combination therapies may include one or more of an anti-HBV antibody; an siRNA that targets an HBV mRNA; interferon-α; and a nucleos(t)ide reverse transcriptase inhibitor (NRTI).

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.