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90 results about "Anti-HIV Agent" patented technology

Any agent that prevents the human immunodeficiency virus (HIV) from reproducing.

4-Oxoquinoline compounds and utilization thereof as hiv integrase inhibitors

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.
Owner:JAPAN TOBACCO INC

Method for extracting antineoplastic components from Bupleurum scorzonerifolium

InactiveUS20050013879A1Effectively inhibit proliferation of Taxol-resistant tumor cellsEffectively inhibit proliferation of human hepatomaBiocideOrganic active ingredientsTelomeraseCancer cell
A method for extracting antineoplastic component from Bupleurum scorzonerifolium applicable in treating cell proliferative disorder is proposed. The antineoplastic components of Bupleurum scorzonerifolium include at least a Y-butyolactone centred heterocyclic compound with a Z configuration or E configuration at its carbon 2(5) position, and molecules, such as Chaihulactone, Isochaihulactone, Chaihulactone analogues or derivatives containing in the heterocyclic compound. From results of cell and molecular biological studies, in vivo animal test, and histological study, it is found that antineoplastic components extracted from Bupleurum scorzonerifolium are effective in suppressing a variety of cancer cell growths, inhibiting telomerase activity, as well as effective in killing with high specificity Taxol-resistant tumor cells at later stage of chemical therapy, making the components a new choice for anti-cancer agent, anti-HIV agent, or synergistic agent.
Owner:BUDDHIST TZU CHI GEN HOSPITAL

Process for production of 4-oxoquinoline compound

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8):wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
Owner:JAPAN TOBACCO INC

Combination therapy

The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT / 3TC, and a combination of PMPA / 3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.
Owner:JAPAN TOBACCO INC

6- (Heterocyclyl-substituted Benzyl) -4-Oxoquinoline Compound and Use Thereof as HIV Integrase Inhibitor

The present invention relates to a compound represented by the following formula [I]wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.
Owner:JAPAN TOBACCO INC

Novel polypeptide anti-HIV agent containing the same

The present invention provides novel polypeptides of A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit Cys-A7 (I) or their salts (wherein A1 is hydrogen or a residue of arginine, lysine, ornithine, citrulline, alanine, or the like; A2 is an aromatic amino acid residue; A3, A4 and A6 are each a residue of arginine, lysine, ornithine, citrulline, or alanine; A5 is a residue of tyrosine, phenylalanine, alanine, naphthylalanine, or citrulline; A7 is a lysine or arginine residue whose carboxyl group may be converted into amido; and X is a residue of D-ornithyl-proline, prolyl-D-ornithine, D-lysylproline, or the like, with the proviso that any one of A1, A3, A4, A5, A6 and A7 is a residue of alanine or the like or that X is citrulline or the like), and methods of using same in the treatment of HIV.
Owner:BIOKINE THERAPEUTICS LTD

Methods of monitoring HIV drug resistance using adenoviral vectors

Recombinant expression vectors and methods are provided for detecting HIV and monitoring HIV drug resistance. The method comprises: taking a culture of cells; adding a recombinant viral vector into the culture to transduce the cells, the recombinant viral vector comprising a reporter sequence comprising a reporter gene whose expression is regulated by a protein specific to HIV viruses which is expressed from a genome of an HIV virus upon infection of a cell in the culture that is transduced by the recombinant viral vector, and a receptor sequence comprising CD 4 and one or more coreceptor genes, expression of the coreceptor genes facilitating productive infection of the transduced cell and enabling HIV virus which has infected the transduced cell to replicate and infect non-infected cells in the culture of the cells transduced by the recombinant viral vector; infecting the transduced cells with a sample containing HIV; adding one or more anti-HIV agents to the cell culture; and detecting a change in a level of expression of the reporter gene in cells.
Owner:MUSC FOUND FOR RES DEV

Tableted compositions containing atazanavir

InactiveUS20100178339A1Desirable dissolution propertyDesirable processing propertyBiocideOrganic active ingredientsAnti-HIV AgentMedicine
Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.
Owner:BRISTOL MYERS SQUIBB CO

Composition for oral cavity and skin

A composition for oral cavity and skin which contains an antibacterial agent and does not have adverse side effects due to steroids, is provided.The composition contains 0.01 to 4.5% by mass of at least one selected from the group consisting of an antibacterial agent, an antiviral agent, an anti-HIV agent, a non-nucleic acid-based reverse transcriptase inhibitor, an anticancer agent for external use and a disinfectant; 0.01 to 4.5% by mass of a non-steroidal anti-inflammatory agent; 0.001 to 4.5% by mass of a steroidal anti-inflammatory agent; and 0.001 to 10% by mass of a highly water-absorbent polymer or a cellulose derivative.
Owner:NODA SATOSHI

Method for testing drug susceptibility of HIV

Methods, compositions and kits are provided for testing susceptibility of HIV to drug treatment, such as drug resistance of HIV and inhibition of HIV replication by a drug candidate. In one aspect of the invention, a method is provided for detecting drug resistance of HIV contained in a sample from an individual infected with HIV. In one embodiment, the method employs an indicator cell line which over-expresses CD4 and one or more co-receptors for HIV such as CXCR4 and CCR5 at high levels to render the cells susceptible to productive infection of various strains, subtypes or clades of HIV from both laboratory and clinical isolates. The methods, compositions and kits can be used for high throughput screening of HIV patient samples, anti-HIV agents, and for designing customized HIV therapy.
Owner:MUSC FOUND FOR RES DEV

Detection of human immunodeficiency virus using cells transduced with a complex viral vector

InactiveUS20030064054A1Convenient and cost-effective and ultra sensitiveImprove throughputBiocideGenetic material ingredientsHeterologousInfected cell
Methods are provided for screening natural and synthetic anti-HIV agents using recombinant cells that are rendered susceptible to productive infection of various strains, subtypes or clades of HIV from both laboratory and clinical isolates. The method comprises: taking a culture of recombinant cells in which at least one of the recombinant cells comprises a reporter sequence comprising a reporter gene whose expression is regulated by a protein specific to HIV, and a heterologous sequence which encodes CD4 and one or more additional cell surface receptors, wherein the heterologous sequence expresses CD4 and the one or more additional cell surface receptors at elevated levels as compared to the cell in the absence of expression by the heterologous sequence such that productive infection of the recombinant cell by HIV is achieved, which is defined by HIV viral replication and the infection of non-infected cells in the culture of the recombinant cells; contacting the cell culture with a sample containing HIV; adding a tester agent to the cell culture; and detecting a change in a level of expression of the reporter gene in the cells in the culture.
Owner:MUSC FOUND FOR RES DEV

Quinolizinone compound and use thereof as HIV integrase inhibitor

A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided. The present invention relates to a quinolizinone compound represented by the following formula [I]wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing same as an active ingredient. The compound of the present invention has an HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compounds can become a more effective anti-HIV agent. Since the compound has a high inhibitory activity specific for integrases, the compound can provide a safe pharmaceutical agent for human with a fewer side effects.
Owner:JAPAN TOBACCO INC

4-oxoquinoline compounds and utilization thereof as HIV integrase inhibitors

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula, wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.
Owner:JAPAN TOBACCO INC

Method for producing 4-oxoquinoline compound

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2'): wherein R is a fluorine atom or a methoxy group, and R<400> is a hydrogen atomor a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
Owner:JAPAN TOBACCO INC

1-hydroxy naphthyridine compounds as Anti-hiv agents

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.
Owner:MERCK SHARP & DOHME CORP

Method for producing 4-oxoquinoline compound

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2′):wherein R is a fluorine atom or a methoxy group, and R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
Owner:JAPAN TOBACCO INC

Oral and skin compositions

Disclosed is a skin or oral composition comprising an anti-bacterial agent, which produces no adverse side effect caused by a steroid contained therein. The composition comprises: 0.01 to 4.5 mass% of at least one component selected from the group consisting of an anti-bacterial agent, an anti-viral agent, an anti-HIV agent, a non-nucleoside reverse transcriptase inhibitor, an anti-cancer agent for external application, and a bactericidal agent; 0.01 to 4.5 mass% of a non-steroidal anti-inflammatory agent; 0.001 to 4.5 mass% of a steroidal anti-inflammatory agent; and 0.001 to 10 mass% of a super-water-absorbent polymer or a cellulose derivative.
Owner:株式会社日本高度医疗研究会 +1

Pyridinone diketo acids: inhibitors of HIV replication in combination therapy

A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti- HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described. Compounds of the present application include those of formula I and include tautomers, regioisomers, geometric isomers, and pharmaceutically acceptable salts thereof, wherein the pyridinone scaffold and R groups are as otherwise defined in the specification. These are combined, with any number of typical other anti-HIV agents (including other integrase-based anti-HIV agents) and other combination therapeutic agents described herein, to provide an effective treatment modality for HIV infections, including AIDS and ARC.
Owner:UNIV OF GEORGIA RES FOUND INC

Method for producing recombinant cells for detecting HIV

Recombinant expression vectors and methods are provided for detecting HIV and monitoring HIV drug resistance. The method comprises: taking a culture of cells; adding a recombinant viral vector into the culture to transduce the cells, the recombinant viral vector comprising a reporter sequence comprising a reporter gene whose expression is regulated by a protein specific to HIV viruses which is expressed from a genome of an HIV virus upon infection of a cell in the culture that is transduced by the recombinant viral vector, and a receptor sequence comprising CD 4 and one or more coreceptor genes, expression of the coreceptor genes facilitating productive infection of the transduced cell and enabling HIV virus which has infected the transduced cell to replicate and infect non-infected cells in the culture of the cells transduced by the recombinant viral vector; infecting the transduced cells with a sample containing HIV; adding one or more anti-HIV agents to the cell culture; and detecting a change in a level of expression of the reporter gene in cells.
Owner:MUSC FOUND FOR RES DEV

Chemical Compounds

Novel diarylpyrimidine derivatives and pharmaceutically acceptable salts, solvates or hydrates thereof, designed to inhibit HIV reverse transcriptase, are provided, and a pharmaceutical composition containing the same, especially an anti-HIV agent. More specifically, novel diarylpyrimidine derivatives that are derivatives of the HIV reverse transcriptase inhibitor TMC278 of formula (1a) are provided, and pharmaceutically acceptable salts, solvates or hydrates thereof.
Owner:GLAXO SMITHKLINE LLC

Aryl phosphate derivatives of AZT having anti-HIV activity

Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.
Owner:UCKUN FATIH M

Composition and methods used during Anti-hiv treatment

InactiveUS20110046091A1Restoration of the normal phenotypeSymptoms improvedBiocideMetabolism disorderPremature agingSide effect
This invention relates to a composition comprising an anti-HIV treatment and a treatment for side effects of said anti-HIV treatment in an HIV-infected patient. This invention is, for example, very useful in the treatment of side effects caused by certain anti-HIV treatments, for example premature aging and lipodystrophy, which can be caused by protease inhibitors or reverse transcriptase inhibitors. The composition of this invention includes at least one hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, at least one farnesyl-pyrophosphate synthase inhibitor, and at least one anti-HIV agent. One of the processes for treating an HIV-infected patient includes, in any order, the following steps: (i) administration of a mixture including at least one hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor and at least one farnesyl-pyrophosphate synthase inhibitor and (ii) administration of an anti-HIV agent, in which the administrations are concomitant, successive or alternative.
Owner:UNIV DAIX MARSEILLE
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