317 results about "Reverse-transcriptase inhibitor" patented technology

The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (N(t)RTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the treatment of HIV infections and AIDS.

Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

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.

The invention discloses a nucleic acid amplification system and a freeze-drying protective agent thereof. The nucleic acid amplification system comprises a buffer solution, an enzyme mixing solution, a nucleic acid amplification reaction solution and the low-temperature freeze-drying protective agent. The buffer solution further comprises one or more of dNTP, Mgcl2, Thris-Hcl and KCl. The enzyme mixing solution further comprises one or more of RNA reverse transcriptase, RAN inhibitor and DNA polymerase. A preparation method for the freeze-drying protective agent applied to the nucleic acid amplification system comprises the following step that the components are mixed to be uniform according to the adopted concentration ratio to obtain the freeze-drying protective agent. An RNA / DNA fluorescent quantitation nucleic acid diagnostic reagent system can be detected in a freeze-drying mode, freeze drying can be achieved, the detection purpose can be achieved only through one-step hydration, and the purposes of normal temperature transportation and storage which cannot be achieved by a nucleic acid diagnostic reagent at the present stage can be achieved.

The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and / or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.

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.

A series of S-triazolyl α-mercaptoacetanilides having N-(α-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O)N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.

Heteroaromatic compounds of Formula I:are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds.

The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

The efficacy of reverse transcriptase and DNA polymerase inhibitors (nucleoside analogs) in a mammalian host is enhanced by administering an effective amount of PNP inhibitor of prodrug of PNP inhibitor and / or an effective amounts of 2′-de-oxyguanosine and / or prodrugs thereof.

The invention relates to a combination of treatments, more particularly a combination treatment for HIV-1 infection. The present invention is directed to the use of bryostatin-1 and their natural and synthetic derivatives for AIDS therapy, in particular to the use of bryostatins in combination with other active drugs such as Histone Deacetylases (HDACs) inhibitors and anti-retrovirals, for the treatment of HIV-1 latency. According to the present invention, we provide a combination therapy for the treatment of HIV-1 latency which employs bryostatin-1 (and analogues) and one of the following HDAC inhibitors; valproic acid, butyrate derivatives, hydroxamic acids and benzamides. While HDACi can be used in continuous dosing protocol, bryostatins can be used following a cyclical dosing protocol. Bryostatins can be formulated in pharmaceutical acceptable carriers including nanoparticles, phospholipids nanosomes and / or biodegradable polymer nanospheres. This combination therapy needs to be used in patients treated with antiretroviral therapy (HIV-1 protease inhibitors, HIV-1 reverse transcriptase inhibitors, HIV-1 integrase inhibitors, CCR5 co-receptor inhibitors and fusion inhibitors).

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.

Disclosed herein are compounds of formula Ar1—X—W—Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)-N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.

Compositions, formulations, and methods for the treatment or prevention, or decreasing the frequency of transmission of a virus (such as human immunodeficiency virus type 1 (HIV-1), Herpes Simplex virus type 1 (HSV1), or Herpes Simplex Virus Type 2 (HSV2), or other virus), or a bacterial infection (such as Trichomonas vaginalis, Neisseris gonorrhoeae Haemopholus ducreyl, or Chlamydia trachomatis, or other bacterial species), or a fungal infection, using an anionic cellulose- or acrylic-based oligomer, polymer, or copolymer. The present invention also includes administering a therapeutically effective amount of said oligomer, polymer, or copolymer, or a pharmaceutically acceptable salt thereof, or with a pharmaceutically acceptable carrier or diluent, thereof. The invention relies on the unique biochemical substitution of the cellulose or acrylic backbone such that the resultant molecule can remain molecularly dispersed in solution (or gel or other formulation) and mostly dissociated over a wide range of physiological microenvironments, such as the low pH found within the vaginal lumen, preferably from a pH of 14 to below 3.5. These specific substitutions also impart on the resultant molecule potent antiviral, anti-bacterial, and anti-fungal properties. In addition, these compositions can be used as general disinfectants for human use such as in contact lens solutions, mouthwashes, toothpastes, suppositories, or as more generalized disinfectants found in soaps, household cleaning products, paints, water treatments modalities, or can be incorporated into cosmetic, and can be used as vehicles for drug delivery, an adjuvant in a therapeutic formulation, or as a preservative. These compounds can be delivered in a liquid or solid dosage form and can be incorporated into barrier devices such as condoms, diaphragms, or cervical caps, to help prevent the transmission of STDs. The compounds of this invention can also be used in combination therapies with other classes of antiviral, antibacterial, or antifungal agent having similar or differing mechanisms of action including, but not limited to, anionic or cationic polymers, copolymers, or oligomers, surfactants, protease inhibitors, DNA or RNA polymerase inhibitors (including reverse transcriptase inhibitors), fusion inhibitors, cell wall biosynthesis inhibitors, integrase inhibitors, or virus or bacterial attachment inhibitors.

Disclosed herein are compounds of formula Ar1—X—W—Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)-N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.

Heteroaromatic compounds of Formula I:are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

The invention belongs to the field of medical technology, and specifically discloses an indole compound and an application thereof as an HIV-1 reverse transcriptase inhibitor. The indole compound disclosed by the invention has a structural general formula: wherein the formula is described in the specification.

The present invention provides compositions and methods for the treatment of HIV infection. In particular, the present invention provides non-nucleoside inhibitors of reverse transcriptase (RT), as well as methods to treat HIV infection using these non-nucleoside inhibitors of RT. In preferred embodiments, the present invention provides a novel class of substituted benzimidazoles, effective in the inhibition of human immunodeficiency virus (HIV) RT.

The present invention relates to novel compositions comprising an excision-inhibiting bisphosphonate and a nucleoside reverse transcriptase inhibitor. The present invention also relates to methods for preventing or treating retrovirus-related diseases using a composition comprising a bisphosphonate and a nucleoside reverse transcriptase inhibitor. In a specific embodiment, the invention provides methods for preventing or treating AIDS by administering a bisphosphonate-based compound in combination with 3′-azido-3′-deoxythymidine (AZT) to patients infected with AZT-resistant HIV to improve the effectiveness of AZT therapy.