99 results about "Anti-hiv drugs" patented technology

The invention relates to anti viral agents comprised of viral fusion inhibitors and at least a portion of an immunoglobulin constant region. The invention further relates to anti viral agents comprised HIV viral fusion inhibitors and an Fc fragment of an immunoglobulin. The invention also relates to methods of treating a viral infection, including HIV infection.

A composition and method for potentiating, sensitizing, and / or amplifying at least one adjuvant pharmaceutical targeting at least one latent viral infection in a patient is provided. In one embodiment, the composition is administered to potentiate, sensitize and / or amplify an adjuvant pharmaceutical targeting at least one latent viral infection such as those which are currently being investigated for use with anti-HIV drugs / antiretrovirals HAART.

The invention belongs to the field of traditional Chinese medicine production, and relates to 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs. 1-alkylated daphnane diterpene is a compound extracted from S. chamaejasme of the Stellera genus; tests prove that 1-alkylated daphnane diterpene is remarkable in anti-HIV activity, and the EC50 value is lower than 0.001 [mu]M; 1-alkylated daphnane diterpene is relatively low in cytotoxicity, and the CC50 value is higher than 11 [mu]M; compared with a positive control drug zidovudine, 1-alkylated daphnane diterpene has more obvious advantages; the 1-alkylated daphnane diterpene compound can serve as an active ingredient for preparation of the anti-HIV drugs.

The present invention is based, in part, upon the discovery that the use of an anti-HIV drug in combination with at least one cortisol blocker such as procaine, reduces the side effects associated with anti-HIV drugs. The invention also relates to a method of treating the high cortisol catabolic effects of diseases such as AIDS in the HIV positive population and those with AIDS related complexes by the administration of a cortisol blocker. The present invention also discloses a composition comprising an anti-HIV drug and cortisol blocker. More specifically, the present invention relates to a cortisol blocking composition which comprises procaine, ascorbic acid and zinc heptahydrate.

1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and / or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.

This invention provides trifluoroacetate derivatives of (R)-PMPA or (R)-PMPDAP represented by formula I and their non-toxic biological pharmaceutical acceptable salts, wherein R1 is H or NH2, R2 is H or COO-R3, and R3 is C1-C10 alkyl or phenyl substituted C1-C3 alkyl. This invention also provides drug combinations with acyclic nucleoside phosphonates as shown in formula I and their non-toxic pharmaceutical acceptable salts as active ingredients, and their applications in antiviral drugs, especially in anti-HBV and anti-HIV drugs.

The invention discloses a double-target anti-HIV (anti-human immunodeficiency virus) glycopeptide compound and an application thereof. The anti-HIV glycopeptide compound is a T20 compound modified with mannan oligosaccharide or oligosaccharide containing fucose at the terminal. The fixed-point glycosylated modified compound of an anti-HIV drug represented as M1-T20, M3-T20, M5-T20 or Lex-T20 is a double-target drug, can prolong the plasma half-life of the drug in the animals and enhance the HIV inhibiting effect, and has the great application value.

The invention discloses D, L-guanosine analogs, preparation methods thereof and applications thereof. The structural formulas of the analogs are respectively represented by a general formula I or a general formula II, wherein R is hydrogen, amino, piperidyl, morpholinyl or pyrrolidinyl. The good chemical stability and the pharmacokinetic stability showed by the D, L-guanosine analogs of the invention make up for shortages of low stability, poor pharmacokinetic stability and the like existing in D4G and ddG. The preparation methods of the D, L-guanosine analogs have the advantages of mild reaction, simplicity and high yield. Antiviral activity testing shows that the compounds with the general formula I or the general formula II which have excellent antiviral activity can be applied to prepare anti-HIV drugs, anti-HBV drugs, anti-HCV drugs or anti-HSV drugs.

The invention belongs to the field of drug synthesis, particularly discloses an artemisinin derivative as well as a preparation method and an application, and more particularly discloses an artemisinin derivative as well as a preparation method and an application thereof in anti-tumor drugs and anti-HIV drugs. The artemisinin derivative disclosed by the invention has a structure as shown in a formula I, wherein R is a residual radical of other compounds. The preparation method of the artemisinin derivative as shown in the formula I is simple and feasible, good in repeatability and small in environmental pollution, and can be used for massively preparing the compound as shown in the formula I. The compound as shown in the formula I has obvious anti-tumor activity and anti-HIV activity.

A method for treatment of HIV infection includes administering at least one anti-HIV drug, such as a reverse transcriptase inhibitor, to a patient in need of such treatment and administering an extract from inflammatory tissue inoculated with vaccinia virus to the patient following the administration of the at least one anti-HIV drug. The extract maintains suppressive action on HIV replication, even if the administration of the anti-HIV drug is terminated.

A formulation is disclosed for the treatment of diseases caused by an infectious agent which acquires host membranes protein during its life cycle. The formulation is a targeting pharmaceutical composition. It comprises a ligand capable of binding the host membrane proteins coupled to a lipid-comprising vesicle, which may comprise or not a drug effective in the treatment of the disease. Specific liposomes bearing anti-HLA-DR or anti-CD4 antibodies comprising or not antiviral drugs, namely anti-HIV drugs, are disclosed and claimed. A method of formulation as well as a method of using the formulation in the treatment of a disease are also disclosed.

This invention relates to a Hybrid immunodeficiency virus strain and application, Human immunodeficiency virus (HIV-1) B' hypotype, R5 tropism, hybrid human / simian immunodeficiency virus strain (SHIV-B'WHU) and 3'end chimeric plasmids used to construct this virus and the use of this virus in stablishing simian / AIDS animal model. At genome framework of simian immunodeficiency virus SIVmac239, gene segment of B'HIV-1 replaces SIVmac239 gene to constitute SHIV-B'WHU. The constituted Hybrid virus SHIV-B'WHU takes along adventitial gene of B'hypotype HIV-1, possessing R5 tropism, it can infect PBMC of human and Macaca rhesus out-of-body and be effectively reproduced, ensuring that SHIV-B'WHU infect Macaca rhesus to construct simian / AIDS animal model. It will be used for researching HIV such as: process of infection in body, etiological agent characteristic, etiopathogenesis,immune reaction and so on, and screening and evaluating AIDS vaccine, anti-HIV drug and microbicide.

The invention discloses a Keggin-structure heteropolyacid phosphorus-containing organic salt compound as well as a preparation method and application, belonging to the field of chemical synthesis and medicinal application. The general formula of the compound disclosed by the invention is A7PTi2W10O40, wherein A is organic cation containing phosphorus and nitrogen; and the compound is a heteropolyacid compound with a Keggin structure. The preparation method comprises the following steps: dissolving sodium tungstate and sodium dihydrogen phosphate in distilled water; dropwise adding titanium tetrachloride for a reflux reaction; filtering; adding alkali metal salt or amino acid salt into the filtrate to obtain a white precipitate; recrystallizing the precipitate with hot water; adjusting to acidity with a compound containing A group or an A compound; and heating and stirring to obtain the Keggin-structure heteropolyacid phosphorus-containing organic salt compound. The compound can be used for preparing anti-HIV drugs.

It is intended to provide an anti-HIV drug characterized by containing multimeric actinohivin, a polypeptide which is multimeric actinohivin; a gene encoding the same; and a method of producing the anti-HIV drug. The anti-HIV drug inhibits the synctium formation and has an enhanced effect

The invention belongs to the field of chemical synthesis and particularly relates to a preparation method for a chiral epoxy compound of an anti-HIV drug intermediate. The method provided by the invention synthesizes the chiral epoxy compound by using a special ligand according to a route represented by the formula. L-phenylalanine used for synthesizing the anti-HIV drug intermediate is low in price and is easily available. The synthetic method is simple and feasible, the yield of the chiral epoxy compound is high, and the synthetic cost of the chiral epoxy compound is obviously lowered compared with that in an existing process.

The invention discloses a screening method of an anti-HIV drug, which comprises the following steps: a sample to be tested is added to a fusion protein which expresses hA3G and reporter gene and a Vif cell; the blocking effect of the sample on Vif pathway is judged by investigating the quantity of the encoding products of the reporter gene; whether the initially chosen sample is an inhibitor in the pathway of proteasome degradation is further judged to screen out the anti-HIV drug. In the method provided by the invention, a hA3G is taken as a target point, solves the problem of drug resistance caused by high mutation of viruses and has no cross resistance with the anti-HIV-1 drug used in clinical application for the moment.

This invention relates, in part, to methods and compositions for determining the susceptibility of an HIV to an anti-HIV drug or the replication capacity of an HIV. In certain embodiments, the methods comprise culturing a host cell in the presence of the anti-HIV drug, measuring the activity of the indicator gene in the host cell; and comparing the activity of the indicator gene as measured with a reference activity of the indicator gene. In certain embodiments, the difference between the measured activity of the indicator gene relative to the reference activity correlates with the susceptibility of the HIV to the anti-HIV drug, thereby determining the susceptibility of the HIV to the anti-HIV drug. In certain embodiments, the difference between the measured activity of the indicator gene relative to the reference activity indicates the replication capacity of the HFV, thereby determining the replication capacity of the HIV. In certain embodiments, the host cell comprises a patient-derived segment and an indicator gene. In certain embodiments, the patient-derived segment comprises a nucleic acid sequence that encodes integrase or RNAse H.

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 present invention provides a novel R-PMPA predrug as shown in formula I and various medical salts thereof. Meanwhile, the present invention also relates to a medical composition using the compounds as active ingredients and an application of the medical composition as an antiviral drug, particularly a drug for treating and preventing hepatitis B and AIDS viruses.

The invention relates to the field of biomedicines and provides an application of a novel carbazole derivative with anti-HIV activity in preparing an anti-HIV drug. The invention particularly relatesto a compound as shown in a formula (I) and pharmaceutical salt thereof. The compound or the pharmaceutical salt thereof can be also combined with pharmaceutical auxiliary materials to prepare a single formula or a compound preparation. The invention also discloses an application of the compound or the pharmaceutical salt thereof in preparing a drug for preventing or treating HIV infection relateddiseases or symptoms. The preparation raw materials of the compound are high in commercial degree and cheap and easily available. The preparation route is short, the method is simple, the productioncost is low, and more efficient and safe candidate drugs are provided for clinical anti-HIV treatment.

The invention provides compounds represented in formula (I) in the description or pharmaceutically acceptable salts or prodrugs of the compounds. The compounds have novel structure, high efficiency, low toxicity and excellent CXCR4 antagonistic activity, and can block HIV from invading and infecting human target cells, treat or prevent AIDS or mobilize human bone marrow hematopoietic cells, mesenchymal stem cells and stem cells, interfere with CXCL12 / CXCR4 mediated cell migration and adhesion, prevent and treat CXCR4 mediated tumor metastasis, invasion and growth, or block CXCL12 / CXCR4 mediated autoimmune and inflammatory reactions. The compounds can be used as an active ingredient in pharmaceutical composition for preventing and treating HIV in combination with other anti-HIV drugs, or for preventing and treating tumors in combination with other drugs for treating or preventing leukemia, lymphoma, myeloma and solid tumors.

The invention discloses an N-substituted-5-((4-substituted pyrimidine-2-yl)amino)indole derivative as well as a preparation method and a purpose thereof, and relates to malignant tumor drugs. A structure of the N-substituted-5-((4-substituted pyrimidine-2-yl)amino)indole derivative is shown as a formula I. For application of the N-substituted-5-((4-substituted pyrimidine-2-yl)amino)indole derivative in preparing an antitumor drug and an anti-HIV drug, a novel derivative which inhibits the signal pathway activities of CDK9 and HDACs is applied to blocking tumor cell proliferation and inducing cells apoptosis by inhibiting relative signal pathway activities of the CDK9 and the HDACs, and thus can be used for treating and preventing various diseases such as malignant tumors of humans and animals.

The invention discloses a novel use of carex rigescens in pharmacy, more particularly relates to the application of the carex rigescens for preparing anti-HIV drug. The application comprises the following steps: firstly, the carex rigescens is pretreated to obtain extractive; and then, the extractive and medically receivable auxiliary materials are jointly made into anti-HIV drug, and the dosage forms of the drug is any one of injection, capsule, troche, granular formulation, pill, mixture, tincture and oral liquid. By adopting the extractive of the carex rigescens to do an HIV PR inhibition experiment and make comparison with positive control drug Indinavir, the result shows that the carex rigescens has remarkable HIV prolease (HIV PR) inhibition activity and has certain guidance significance for developing the anti-HIV drug, thereby having important reference value.

A method of treating HIV infection comprises administering to a patient a regimen that is able to shut down the immune system in a controlled manner by using T-cell depletion or T-cell modification such that T-cells no longer can be attacked by HIV cells. The T-cell depletor or T-cell modifiers are administered either alone or in combination with 'conventional' anti-HIV drugs.

This invention discloses a method for synthesizing resdelasu from delaviradine intermediate and resveratrol. The method comprises: amidating succinic anhydrate and delaviradine intermediate, and esterifying with resveratrol to obtain resdelasu; or esterifying succinic anhydrate with resveratrol, and amidating with delaviradine intermediate to obtain resdelasu. Resdelasu has the same magnitude order of in vitro bioactivity with anti-HIV drug delaviradine, thus can be used as a new anti-HIV drug.

The invention belongs to the field of biomedicine and antiviral biological agents, relates to a polypeptide capable of inhibiting human immunodeficiency virus (HIV-1) infection activity, and a related bacteriophage, and especially relates to a polypeptide with in vitro inhibitory effects on human immunodeficiency virus (HIV-1) infection activity, and a bacteriophage containing sequence of the polypeptide. The polypeptide and the bacteriophage possesses in vitro inhibitory effects on human immunodeficiency virus (HIV-1) infection activity, and low toxicity on cells; the polypeptide, the bacteriophage and derivatives thereof can be used for exclusive use, or combined with other ingredients so as to develop and prepare anti-HIV drugs and biological agents used for preventing HIV-1 sexual transmission, and provide novel thoughts and novel technology for blocking male to male rectum sexual transmission of HIV.