22 results about "Zidovudine" patented technology

The invention discloses a medicine composition containing homoharringtonine and application of the medicine composition in preparation of an anti-HIV (human immunodeficiency virus) medicine. The medicine composition is composed of the 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 of zidovudine, lamivudine and abacavir, and the non-nucleoside reverse transcriptase inhibitor is selected from one of the compounds of nevirapine, efavirenz and rilpivirine. The pharmaceutical composition has a remarkable synergistic effect on treatment of HIV, the curative effect of the medicine is improved, the dosage of a single medicine is reduced, the toxic and side effects are reduced, the generation of viruses can be remarkably inhibited by combined medication, a very remarkable antiviral effect is generated, and the treatment current situation of HIV-1, especially middle and advanced AIDS, is improved.

The application relates to the medical technical field, in particular to application of zidovudine in preparation of a medicine for preventing and / or treating alcoholic gastric ulcer, and experiment results show that the zidovudine has a remarkable curative effect on peptic ulcer disease and inflammatory bowel disease, can effectively improve mucosal integrity, promote tissue morphology improvement, and restore animal body weight, and has a good clinical application prospect.

The invention relates to the technical field of nano biomedicine, in particular to a cyclometalated Ir (III)-AZT compound as well as a preparation method and application thereof. According to the invention, the cyclometalated Ir (III)-AZT compound is prepared and has low dark toxicity and excellent photodynamic anti-tumor activity. In a tumor acid environment, the iridium complex in the compound generates various ROS under an illumination condition through I / II type photodynamic force, the zidovudine in the compound mediates stress conduction from an endoplasmic reticulum to mitochondria, and the iridium complex and the zidovudine synergistically induce immunogenic cell death and promote tumor antigen and injury related molecular mode release at the same time. In addition, the synergistic treatment can adaptively up-regulate PD-L1 expression of tumor cells, and can further synergistically inhibit tumor growth and relieve an in-vivo immunosuppressive microenvironment when being combined with an immunosuppressor (such as PD-L1), so that a dual anti-tumor effect of'photodynamic and immune synergy 'is realized.

The present invention relates to a pharmaceutical product in the form of a storage stable lyophilisate or a pharmaceutical formulation in the form of a sterile solution for parenteral administration. Both the lyophilisate and solution consist essentially of a polymyxin selected from polymyxin E, polymyxin B, or a pharmaceutically acceptable derivative thereof, and zidovudine or a pharmaceutically acceptable derivative thereof. The solution further includes an aqueous carrier.

The present invention discloses a 1,2,3-triazole feed additive and its preparation method and application, which belongs to the field of functional feed additive synthesis technology. The technical solution of the present invention is as follows: the 1,2,3-triazole feed additive molecule has a structure wherein n is 1 or 2; R is 4-methylphenyl, 4-fluorophenyl or zidovudine. The present invention uses 2-Boc aminobenzoic acid as a starting material, first reacts to obtain 2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindoline-1,3-diketone, then introduces terminal alkynes, and finally reacts with an azide compound to obtain a target molecule with a novel structure through a click reaction, which has a certain inhibitory effect on urease and can be used as a potential feed additive.

The invention discloses an RVG29 modified ziconotide loaded liposome as well as a preparation method and application thereof. The nano-liposome is prepared from phosphatidylpolyethylene glycol-RVG29, lecithin, cholesterol, phosphatidic acid and ziconotide. The preparation method comprises the following steps: performing repeated washing, resin detection and condensation operation on 2-chlorotrityl chloride resin and the like to prepare RVG29 resin, performing cutting sedimentation treatment and high performance liquid chromatography purification on the RVG29 resin by using phospholipid-polyethylene glycol-active ester and a cutting reagent, and adding lecithin, cholesterol, phosphatidic acid and ziconotide to synthesize and prepare the product liposome. The nano-liposome is a novel nano-liposome for the nose and the brain, gel adhesion and drug delivery are improved, the surface of the liposome targets a nicotinic acetylcholine receptor on the surface of a neuron, accurate drug delivery is achieved, no small-molecule cytotoxic drugs participate in the nano-liposome, the treatment compliance of cancer pain patients is improved, and the nano-liposome is a novel nano-liposome for the nose and the brain. The treatment effect and the life quality are improved.

The present invention provides an antimicrobial combination comprising three different antimicrobial agents. The first antimicrobial agent is selected from the group consisting of ceftazidime, polymyxin E, polymyxin B, and pharmaceutically acceptable derivatives thereof; the second antimicrobial agent is selected from the group consisting of zidovudine, doxycycline, fosfomycin and pharmaceutically acceptable derivatives thereof; and the third antimicrobial agent is selected from the group consisting of levofloxacin, doxycycline, fosfomycin, meropenem, rifampicin, gentamicin, polymyxin B / E, and pharmaceutically acceptable derivatives thereof; wherein the combination comprises at least one of levofloxacin, doxycycline, rifampicin, fosfomycin, or a pharmaceutically acceptable derivative thereof; with the proviso that the combination is not (1) polymyxin E / B, zidovudine and rifampicin or (2) ceftazidime, zidovudine and fosfomycin. Also provided are antimicrobial combinations comprising three antimicrobial agents, wherein the first antimicrobial agent is ceftazidime or a pharmaceutically acceptable derivative thereof; the second antimicrobial agent is zidovudine or a pharmaceutically acceptable derivative thereof; and the third antimicrobial agent is polymyxin E or a pharmaceutically acceptable derivative thereof.

The application discloses a phenyl isoindolinone and zidovudine splicing compound and a preparation method and application thereof. The compound has potential biological activity, provides a compound source for biological activity screening, has important application value for drug screening and the pharmaceutical industry, and through in-vitro anti-tumor activity screening, it is found that the compound can selectively inhibit human lung cancer NCI-H1975 cells, and the selectivity index of the compound to normal cells BEAS-2B is high (the inhibition rate is only 12.51 %), the safety is about 7.2 times of that of osimertinib, and the compound exhibits good tumor cell selectivity and low potential side effects. In combination with the changes of NCI-H1975 cell mitochondrial ROS and membrane potential, it is indicated that the phenyl isoindolinone and zidovudine splicing compound derived from an EGFR allosteric inhibitor can play an anti-tumor role by affecting mitochondrial function.

The application relates to application of zidovudine in preparation of drugs for preventing and / or treating chronic heart injury, and belongs to the technical field of biological medicine. The application finds that zidovudine can effectively prevent the phenomenon of chronic heart injury caused by anticancer drugs at the cell experiment level and the animal experiment level. It is found through cell experiments that zidovudine can improve myocardial cell death caused by the anticancer drug doxorubicin, and it is found through animal experiments that zidovudine can improve the decline of heart function and loose and fibrotic myocardial structure caused by the anticancer drug doxorubicin, which indicates that zidovudine has the effect of treating chronic heart injury caused by anticancer drugs.

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.

The application relates to an HIV-1 latent infection activator, a medicine and purposes. An HIV-1 latent infection activator comprises ISX-9 and / or ML327. The HIV-1 latent infection activator further comprises an HDAC inhibitor and / or a BET inhibitor. The HDAC inhibitor is quinostat. The BET inhibitor is birabresib or AZD5153. A medicine comprises the HIV-1 latent infection activator and an HIV-1 inhibitor. The HIV-1 inhibitor is a polypeptide EKL1C, and the amino acid sequence is shown in SEQ ID NO:1. The HIV-1 inhibitor comprises one or more of zidovudine, nevirapine or indinavir. The HIV-1 latent infection activator provided by the application can activate latent HIV, and is a new safe and efficient HIV-1 latent infection activator.

The present application relates to a kind of preparation of zidovudine azide intermediate (compound of formula I) using tubular reactor method, comprising the following steps: preparation of premix solution: compound of formula II, sodium azide, organic acid is dissolved in DMSO solution, preheating, standby;(2) the premix solution prepared in step (1) is input into tubular reactor by peristaltic pump;(3) receiving bottle is placed at the outlet of tubular reactor, and the effluent received is the reaction mixture containing compound of formula I;(4) reaction mixture is pumped into water by peristaltic pump, stirred at room temperature, crystallized, filtered, and dried to obtain compound of formula I. Wherein, the tubular reactor is coiled by pipeline with a certain inner diameter. The preparation method uses equipment structure simple, easy to operate, on the one hand, reduce the risk of operation in the actual production process of azide, on the other hand, realize the reaction efficiency and the yield greatly, realize product yield not less than 92%, and product purity is higher than 95%.

The invention provides a continuous flow synthesis method of zidovudine, which comprises the following steps: sequentially carrying out continuous hydroxyl protection (S1), continuous acylation (S2), continuous cyclization (S3), continuous azidation (S4) and continuous deprotection (S5) on a raw material compound beta-thymidine to obtain a zidovudine crude product. According to the technical scheme, a more efficient, safer and more flexible production mode and method are provided, hydroxyl protection, acylation, cyclization, azidation and deprotection reactions are continuously operated, the reaction efficiency and selectivity are improved, a large amount of separation and purification operation in the original production process is reduced, and the production cost is reduced. And the production time can be shortened from several weeks to several hours.

The present invention relates to a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and a fluoroquinolone antibiotic or a pharmaceutically acceptable derivative or prodrug thereof for use in the treatment of microbial infections, particularly bacterial infections such as urinary tract infections.

Provided is a method of treating a subject with an α-synucleinopathy neurodegenerative disorder, the method comprising administering one or more therapeutic(s) to the subject, a method of treating a subject with a high risk of developing an α-synucleinopathy neurodegenerative disorder, the method comprising administering one or more therapeutic(s) to the subject, wherein the one or more therapeutic(s) is or comprise rifabutin, one or more nucleoside analog reverse transcriptase inhibitor(s), optionally selected from lamivudine, emtricitabine, tenofovir disoproxil funiarate, tenofovir alafenamide, abacavir, zidovudine, didanosine, and / or stavudine, losartan, or a combination thereof.

The invention relates to an HIV-1 latent infection activator, a medicine and application. The invention relates to an HIV-1 (Human Immunodeficiency Virus-1) latent infection activator, which comprises ISX-9 and / or ML327. The HIV-1 latent infection activator further comprises an HDAC inhibitor and / or a BET inhibitor. The HDAC inhibitor is quinostat. The BET inhibitor is birabresil or AZD5153 (Azodicarbonamide 5153). The invention also discloses a medicine which comprises any one of the HIV-1 latent infection activator and the HIV-1 inhibitor. The HIV-1 inhibitor is polypeptide EKL1C, and the amino acid sequence of the HIV-1 inhibitor is shown as SEQ ID NO: 1. The HIV-1 inhibitor is prepared from one or more of zidovudine, nevirapine or indinavir. The HIV-1 latent infection activator disclosed by the invention can activate latent HIV (human immunodeficiency virus), and is a novel, safe and efficient HIV-1 latent infection activator.

The present invention provides an antimicrobial combination comprising three different antimicrobial agents The first antimicrobial agent is selected from ceftazidime, polymyxin E, polymyxin B, and pharmaceutically acceptable derivatives thereof; the second antimicrobial agent is selected from zidovudine, doxycycline, fosfomycin and pharmaceutically acceptable derivatives thereof; and the third antimicrobial agent is selected from levofloxacin, doxycycline, fosfomycin, meropenem, rifampicin, gentamicin, polymyxin B / E, and pharmaceutically acceptable derivatives thereof; wherein the combination includes at least one of levofloxacin, doxycycline, rifampicin, fosfomycin, or a pharmaceutically acceptable derivative thereof; provided the combination is not (1) polymyxin E / B, zidovudine and rifampicin or (2) ceftazidime, zidovudine and fosfomycin. Also provided is an antimicrobial combination comprising three antimicrobial agents, wherein the first antimicrobial agent is ceftazidime or a pharmaceutically acceptable derivative thereof; the second antimicrobial agent is zidovudine or a pharmaceutically acceptable derivative thereof; and the third antimicrobial agent is polymyxin E or a pharmaceutically acceptable derivative thereof.

The invention relates to an aza-alicyclic ring substituted pyrimidine derivative and a preparation method thereof, the aza-alicyclic ring substituted pyrimidine derivative has a structure as shown in a formula I. The aza-alicyclic ring substituted pyrimidine derivative provided by the invention is novel in structure, most of the compounds show relatively strong anti-HIV-1 activity, and the EC50 value is between 9.40 nM and 238 nM. Wherein the activity of compounds WP-10a (EC50 is equal to 12.6 + / -0.68 nM), WP-10b (EC50 is equal to 9.40 + / -0.96 nM), WP-10c (EC50 is equal to 18.3 + / -1.6 nM) and WP-10d (EC50 is equal to 26.2 + / -6.0 nM) of which the X site is substituted by amino azetidine is particularly prominent, the WP-10b with the optimal activity has the antiviral effect of single-digit nanomole, the activity is improved by about 30 times compared with that of a drug nevirapine (EC50 is equal to 281 + / -38.7 nM) on the market, and the activity is equivalent to that of efavirenz (EC50 is equal to 5.20 + / -0.90 nM)

To provide a pharmaceutical product in the form of a storage stable lyophilisate or a pharmaceutical formulation in the form of a sterile solution for parenteral administration.SOLUTION: Provided are a lyophilisate and a solution, both consisting essentially of a polymyxin selected from polymyxin E, polymyxin B, or a pharmaceutically acceptable derivative thereof, and zidovudine or a pharmaceutically acceptable derivative thereof, and the solution further includes an aqueous carrier.SELECTED DRAWING: None

The invention discloses a multi-purpose lily detoxification method and application thereof, and the method comprises the following steps: (1) establishing an aseptic seedling system: selecting third-layer scales from outside to inside of lily bulbs' Flying Shaohua 'and' Flying Tianorange 'as explants, disinfecting the explants, and carrying out tissue culture to establish the aseptic seedling system; (2) virus detection and detoxification: taking leaves from aseptic seedlings to detect viruses, and performing detoxification treatment on positive samples; the detoxification treatment method comprises at least one of induced callus detoxification, stem tip combined heat treatment detoxification, stem tip combined virazole detoxification, stem tip combined virazole and heat treatment detoxification. According to the method disclosed by the invention, a high-efficiency virus detoxification technology is established specially aiming at the problem that novel multi-purpose lily varieties' Fangzhou orange 'and' Fangzhou Shaohua 'which have comprehensive characters and are popular with the market are easily infected with CMV and LSV, and a technical support is provided for large-scale production of the two novel multi-purpose lily detoxification seedballs.

The application relates to the field of nanobiomedicine, in particular to a cyclometalated Ir(III)-AZT compound and a preparation method and application thereof. The application prepares a cyclometalated Ir(III)-AZT compound, which has low dark toxicity and excellent photodynamic anti-tumor activity. In a tumor acid environment, the iridium complex in the compound generates various ROS through type I / II photodynamic under light, the zidovudine in the compound mediates stress conduction from the endoplasmic reticulum to the mitochondria, both of which synergistically induce immunogenic cell death, and simultaneously promote the release of tumor antigens and damage-associated molecular patterns. In addition, the synergistic treatment can adaptively up-regulate the PD-L1 expression of tumor cells, and the combination with an immunosuppressive agent (such as PD-L1) can further synergistically inhibit tumor growth, relieve the immunosuppressive microenvironment in the body, and realize the dual anti-tumor effect of "photodynamic + immune synergy".

To provide a combination of two active agents that reactivates specific urinary tract antibiotics in which bacterial resistance has occurred.SOLUTION: Provided is a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and a fluoroquinolone antibiotic or a pharmaceutically acceptable derivative or prodrug thereof for use in treating a microbial infection, particularly a bacterial infection such as a urinary tract infection.SELECTED DRAWING: None