122 results about "Nucleoside Analog 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.

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.

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.

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).

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.

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.

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.

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.

The invention relates to a diarylpyrimidines HIV-1 reverse transcriptase inhibitor as well as a preparation method and application thereof. The diarylpyrimidines HIV-1 reverse transcriptase inhibitorhas a structure shown as a formula I. The invention further relates to a pharmaceutical composition containing the compound with the structure formula I. The invention further provides application ofthe compound and the composition containing one or more compounds to preparation of medicines for treating and preventing human immunodeficiency virus (HIV).

Compounds of Formula I:are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z 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.

A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host A process for controlling retrovirus transmission within a population includes the administration to a subpopulation at high risk for contracting an immunodeficiency retroviral infection the detailed combination prior to sexual exposure to a source of immunodeficiency retrovirus so as to preclude the immunodeficiency retrovirus from becoming self-replicating in a member of the subpopulation.

The present invention includes a group of novel compounds that are demonstrated to potently and selectively inhibit HIV integrase (IN) activity in vitro and to potently inhibit HIV replication in live, cultured cells at non-toxic concentrations. The novel compounds disclosed include 2,3-di(3,4-dihydroxy-dihydroxydihydrocinnamoyl)-L-tartaric acid, 2,3-di-(3,4-dihydroxybenzoyl)-L-tartaric acid, 2,3-di-(3,4-dihydroxyphenylacetyl)-L-tartaric acid, 2,3-di-(3,4,5-trihydroxybenzoyl-L-tartaric acid, 2,3-dicaffeoyldiamidopropionic acid, 1,2,-dicaffeoyl-L-glyceric acid, bis,-3,4-dicaffeoyldiamidobenzoic acid, di-3,4-dihydroxybenzylidene succinic acid, di-3,4-dihydrodihydroxybenzylidine succinic acid, 2,3-dicaffeoyl-L-serine, bis-dicaffeoyl-L-isoserine and 1,4-dicaffeoyl-L-lysine. Tests of integrase inhibitors with 2′,3′-dideoxycytidine, zidovudine and nelfinavir (protease inhibitor) indicated a potent synergy against reverse transcriptase inhibitor resistant virus. The potential benefit from the addition of integrase inhibitors to combination drug therapies is significant.

The invention belongs to the technical field of drugs, and particularly discloses 5-isopropyl-2-(4-hydrocarbyl methanoyl phenyl carbonyl methylsulfonyl)-6-cyclohexylpyrimidone, N-oxide shown as the formula I, a three-dimensional isomer form, a three-dimensional isomer mixture and a pharmaceutically acceptable salt, a hydrous compound and solvent compound, polycrystals and eutectic crystals, a precursor having a same biological function and a derivative. The compound has significant HIV-1 virus resistant activity, is small in toxicity, high in selectivity index and applicable in relevant drugs for treating AIDS. (Shown in the description).

The instant invention describes a method for crystallizing (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40 DEG C and 50 DEG C.

The invention belongs to the field of research and development of HIV inhibitors, and discloses a preparation method for a terpyridine pyridinium (II) complex and application thereof in HIV reverse transcriptase inhibition. The structure of a cationic moiety of the terpyridine pyridinium (II) complex is as shown in a formula I. A preparation process for the terpyridine pyridinium (II) complex is optimized, the raw material cost is low, and the reaction time is short. The obtained complex is high in purity and yield and has good water solubility and excellent spectral properties. The terpyridine pyridinium (II) complex has the capability of selective binding to a TAR region on HIV RNA, and can block the reverse transcription process of viral RNA by reverse transcriptase and inhibit the replication of viral RNA. The terpyridine pyridinium (II) complex is a highly affinitive HIV RNA selective binding reagent and a highly active HIV reverse transcriptase inhibitor, and is an HIV drug having a great application potential.

A method of preparing (+ / -)-calanolide A, 1, a potent HIV reverse transcriptase inhibitor, from chromene 4 is provided. Useful intermediates for preparing (+ / -)-calanolide A and its derivatives are also provided. According to the disclosed method, chromene 4 intermediate was reacted with acetaldehyde diethyl acetal or paraldehyde in the presence of an acid catalyst with heating, or a two-step reaction including an aldol reaction with acetaldehyde and cyclization either under acidic conditions or neutral Mitsunobu conditions, to produce chromanone 7. Reduction of chromanone 7 with sodium borohydride, in the presence of cerium trichloride, produced (+ / -)-calanolide A. A method for resolving (+ / -)-calanolide A into its optically active forms by a chiral HPLC system or by enzymatic acylation and hydrolysis is also disclosed. Finally, a method for treating or preventing a viral infections using (+ / -)-calanolide or (-)-calanolide is provided.

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.

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.

The present disclosure relates to compositions and methods for treating retinal damage and / or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and / or a nucleoside or nucleotide reverse transcriptase inhibitor.

The invention discloses an application of an NK cell exosome (EXO) and related miRNA (micro ribonucleic acid) in inhibition of a COVID-19 virus (new coronavirus), and provides a new thought for inhibition of the COVID-19 virus. The method has the advantages that: (1) the method is different from anti-retroviral inhibitors such as protease inhibitors and reverse transcriptase inhibitors, and miRNAhas high specificity and low side effects; (2) the inhibition effect can be enhanced by combining with a conventional treatment scheme; (3) the miRNA can be artificially synthesized, so that the costis low, and large-scale production can be realized; and (4) the compound has a remarkable inhibition effect on the duplication of the COVID-19 virus.

The disclosure encompasses p28TEV polypeptide, polynucleotides, variants, and antagonists. p28TEV polypeptides and / or polynucleotides are useful in immunogenic compositions. p28TEV polypeptide antagonists include antagonist antibodies, antisense molecules or siRNA molecules. The antagonists and composition of the disclosure can be administered alone or in combination with other agents useful in the treatment of HIV infection, SIV infection, AIDS, or AIDS-related complex (ARC), including nucleoside, non-nucleoside, and / or reverse transcriptase inhibitors.