32 results about "Cidofovir" patented technology

The present application provides methods and compositions for treatment or prevention of dsDNA virus infection in post-hematopoietic cell transplant (HCT or HSCT) patients.

Compositions, methods and systems for treating disordered epithelial tissues, such as is caused by pathogens and / or by toxins produced thereby. The invention relates to the use of an anti-infective and / or antimicrobial active agent in a carrier, with vigorous agitation of the disordered epithelial tissue for topical treatment thereof under such conditions sufficient to achieve clinically discernable improvement of the disordered epithelial tissue. The preferred anti-infective and / or antimicrobial active agent comprises a nucleoside, such as acyclovir, valcyclovir, penciclovir, famciclovir, ganciclovir, cidofovir, adefovir, and tenofovir, and derivatives, analogs, or metabolites thereof, or a mixture thereof, or 1-docosanol, optionally in combination with an organohalide. The inventive compositions and methods may employ the use of an applicator adapted for use in promoting the penetration of the treatment composition and / or the vigorous agitation of the disordered tissue.

The invention discloses a phosphoryl N-fatty acyl nucleoside analogue for treating viral hepatitis and liver cancer. The phosphoryl N-fatty acyl nucleoside analogue is characterized in that a nucleoside analogue is modified by a cyclophosphoryl group and then is connected to aliphatic chains having different numbers of carbon atoms. The phosphoryl N-fatty acyl nucleoside analogue can be used for convenient preparation of a nanometer transmission system and has obvious hepatocyte and tumor targeting. The nanometer transmission system comprises liposome, nonionic surfactant niosomes, nanoparticles, nano-emulsion and a self-assembled transmission system. The nucleoside analogue is selected from lamivudine, adenine arabinoside, cidofovir, gemcitabine, cytosine arabinoside, azacitidine and fludarabine. After intravenous administration, the nanometer transmission system of the phosphoryl N-fatty acyl nucleoside analogue has effects of targeting treatment on viral hepatitis and liver cancer.

The invention provides kits, methods and compositions of matter which improve the safety of vaccination. By combining the administration of antiviral drugs, particularly ester derivatives of cidofovir, with the administration of viral vaccines, particularly the variola vaccine DryVax, side effects of the vaccine are diminished without significantly affecting the effectiveness of the vaccine.

Cidofovir or foscarnet based compounds having an amino acid or dipeptide esters are provided as prodrugs.

A method for synthesizing antiviral drug cidofovir belongs to the field of antiviral chemical drugs. The invention starts from raw material (S)-hydroxymethyl oxirane and synthesizes (S)-1-R-2,3- Propylene oxide (R is a hydrocarbyl group), prepared by etherification, acylation, condensation, deprotection, hydrolysis, acidification and other reactions to prepare cidofovir. The synthesis process is simple in operation, low in cost, high in yield, high in purity and less in pollution, and is very suitable for industrial production.

The invention discloses a new derivant for antiviral cidofovir, as well as the method for making such derivant, which is taking key intermediate (S)-N1-[(3-trity methoxy-2-ethphosphoric acid methoxy) glycerol alcohol]-cytosine as raw material, to condensation react with Boc-amino acid with the help of condensating agent to get intermediate compound, and then stripping protecting group Boc and trityl, and hydrolyzing phosphate, then reacting phosphoric acid with side-chain hydroxy to form ring with cable agent and to get new derivant.

The invention discloses a new derivant for antiviral cidofovir, as well as the method for making such derivant, which is taking key intermediate (S)-N1-[(3-trity methoxy-2-ethphosphoric acid methoxy) glycerol alcohol]-cytosine as raw material, to condensation react with Boc-amino acid with the help of condensating agent to get intermediate compound, and then stripping protecting group Boc and trityl, and hydrolyzing phosphate, after deacidizing it, reacting with chlorpivalmethylactone to get new derivant.

The invention discloses a new derivant and intermediate for antiviral cidofovir, as well as the method for making such derivant, which is taking key intermediate (S)-N1-[(3-trity methoxy-2-ethphosphoric acid methoxy) glycerol alcohol]-cytosine as raw material, to condensation react with Boc-amino acid with the help of condensating agent to get intermediate compound, and then stripping protecting group Boc and trityl, and hydrolyzing phosphate to get new derivant.

The invention discloses a new derivant for antiviral cidofovir, as well as the method for making such derivant, which is taking key intermediate (S)-N1-[(3-trity methoxy-2-ethphosphoric acid methoxy)glycerol alcohol]-cytosine as raw material, to condensation react with Boc-amino acid with the help of condensating agent to get intermediate compound, and then stripping protecting group Boc and trityl, and hydrolyzing phosphate, after deacidizing it, reacting with chlorpivalmethylactone to get new derivant.

The invention discloses a preparation method of Cidofovir of a structural formula (I) and an intermediate thereof. The preparation method comprises the following steps: (1) a compound of a formula (II) reacts with epoxy halogenopropane in the presence of a catalyst in an alkaline environment to obtain a compound of a formula (III); (2) cytosine reacts with a compound of a formula (IV) in the presence of a proper solvent to obtain a compound of a formula (V); (3) compounds obtained in the two steps are condensed in the presence of the proper solvent to obtain a compound of a formula (VI); (4) the compound of the formula (VI) reacts with p-benzenesulfonyloxymethyl phosphoric acid diethylester in the presence of the proper solvent to obtain a compound of formula (VII); and (5) the compound of the formula (VII) is treated at proper pressure to obtain a compound of a formula (VIII). The preparation method shortens synthetic route and lowers synthesis cost, is simple and practical, has the advantages of higher yield and less pollution, and is applicable to industrialized production.

A Xiduofuwei injection in the form of freeze-dried powder for treating AIDS, cytomegalovirus infection of retina, hepes, simplex virus infection, variola virus infection, etc is prepared from Xiduofuwei, and excipient through proportional dissolving, regulating pH value, filter, quickly freezing, heatingand sublimation drying.

The invention relates to a method for preparing a 1-(S)-(2, 3-dihydroxypropxyl)-N<4>-benzoyl cytosine (formula I compound). The compound is a key intermediate for preparing an anti-viral drug called cidofovir (formula II compound).

The invention discloses a green synthesis method of cidofovir, and the specific synthesis process of a chiral N4-benzoylcytosine diol compound comprises the following steps: uniformly mixing a chiral N4-benzoylcytosine epoxy compound, water and an ionic liquid catalyst, adding the mixture into a high-pressure reaction kettle, introducing CO2 gas, and reacting at 0-140 DEG C, and after the reaction is finished, separating the product and the ionic liquid catalyst, carrying out column chromatography on the product to obtain a chiral N4-benzoylcytosine diol compound, carrying out a series of reactions such as hydroxyl protection, phospholipidation and deprotection to synthesize the target product cidofovir, and repeatedly recycling the separated ionic liquid catalyst. The method does not need to use metal, inorganic base and other catalysts, does not need to add a large amount of solvent, is simple and convenient to operate and mild in reaction condition, and the used catalyst is ionic liquid and is relatively environment-friendly. Meanwhile, the yield of the synthesized target product is relatively high, and the ee value can be maintained.

Cidofovir or foscarnet based compounds having an amino acid or dipeptide esters are provided as prodrugs.

Cidofovir-based compounds having an amino acid, dipeptide or tripeptide attached to a cidofovir or cyclic cidofovir framework. The compounds show enhanced oral bioavailability and increased binding to the PepT1 transporter. The present invention also provides compositions and methods for treating virus infections, and a method of preparing cidofovir.

Described are lyophilized compositions comprising cidofovir, hydroxypropyl methylcellulose (HPMC) or hydroxyethylcellulose (HEC) and, optionally, a plasticizer. In particular, described are such compositions that form a sheet-shaped porous solid matrix. Also described are methods for producing such compositions and their use in treating human papillomavirus (HPV) infections and HPV-associated malignancies, in particular, HPV lesions and cervical cancer.

The invention discloses a new derivant for antiviral cidofovir, as well as the method for making such derivant, which is taking key intermediate (S)-N1-[(3-trity methoxy-2-ethphosphoric acid methoxy)glycerol alcohol]-cytosine as raw material, to condensation react with Boc-amino acid with the help of condensating agent to get intermediate compound, and then stripping protecting group Boc and trityl, and hydrolyzing phosphate, then reacting phosphoric acid with side-chain hydroxy to form ring with cable agent and to get new derivant.

The invention relates to a method for synthesizing antiviral drugs, i.e., cidofovir and buciclovir, belonging to the field of asymmetric synthesis in organic chemistry. According to the invention, pyrimidine with position 1 substituted by an allyl group or purine with position 9 substituted by a butenyl group are used as raw materials and subjected to asymmetric dihydroxylation so as to obtain a key chiral intermediate of cidofovir or buciclovir, and then a multi-step reaction is carried out so as to obtain cidofovir or buciclovir. With such a route in the invention, the reaction raw materialsare easily available, stereoselectivity is high, and the chiral dihydroxynucleoside intermediates are obtained after the reaction, and the cidofovir and buciclovir can be smoothly obtained after multiple steps of transformation.

The invention relates to a method for synthesizing an antiviral drug cidofovir intermediate and a buciclovir intermediate, belonging to the field of asymmetric synthesis in organic chemistry. Using the allyl group substituted at the 1-position of pyrimidine or the butyl group substituted at the 9-position of purine as raw materials, the key chiral intermediate of cidofovir or buciclovir is obtained through asymmetric dihydroxylation reaction, followed by multi-step reaction Then get cidofovir or buciclovir. The route adopted in the present invention has easy-to-obtain reaction raw materials and high stereoselectivity. After the reaction, chiral dihydroxynucleoside intermediates can be obtained, and cidofovir and buciclovir can be successfully obtained after multi-step transformation.

Cidofovir is obtained in different forms, including amorphous cidofovir, crystalline anhydrous cidofovir, crystalline cidofovir monohydrate, and crystalline cidofovir dihydrate, including various polymorphs.

Cidofovir is obtained in different forms, including amorphous cidofovir, crystalline anhydrous cidofovir, crystalline cidofovir monohydrate, and crystalline cidofovir dihydrate, including various polymorphs.

The present invention provides a borasidofovir preparation for local and / or transdermal administration. The preparation comprises: (a) a therapeutically effective amount of borasidofovir and (b) a pharmaceutically suitable borasidofovir carrier, wherein the carrier comprises 3-45% by weight of isostearic acid in the preparation, at least 1% of a penetrant is contained, and a penetrant provides anosmotic effect within 24 hours. According to the invention, the borasidofovir cream is dynamically permeated into the subcutaneous part and continuously absorbed, so that medicines in the cream are continuously released, the continuous absorption and permeation are achieved, thecarrier suitable for the characteristics of the Bromsidofovir characteristic prescription is selected, and the safe, effective, stable and controllable Bromsidofovir cream is prepared and is used for treating local, skin, mucous membrane and systemic virus infection.

The present invention relates to lyophilized compositions comprising cidofovir, hydroxypropyl methylcellulose (HPMC) or hydroxyethylcellulose (HEC) and optionally a plasticizer. In particular, the present invention relates to such compositions which form a sheet-shaped porous solid matrix. The invention also relates to methods for producing such compositions. The invention further relates to such compositions for use in treating human papillomavirus (HPV) infections and HPV-associated malignancies, in particular HPV lesions and cervical cancer.

The invention discloses a phosphoryl N-fatty acyl nucleoside analogue for treating viral hepatitis and liver cancer. The phosphoryl N-fatty acyl nucleoside analogue is characterized in that a nucleoside analogue is modified by a cyclophosphoryl group and then is connected to aliphatic chains having different numbers of carbon atoms. The phosphoryl N-fatty acyl nucleoside analogue can be used for convenient preparation of a nanometer transmission system and has obvious hepatocyte and tumor targeting. The nanometer transmission system comprises liposome, nonionic surfactant niosomes, nanoparticles, nano-emulsion and a self-assembled transmission system. The nucleoside analogue is selected from lamivudine, adenine arabinoside, cidofovir, gemcitabine, cytosine arabinoside, azacitidine and fludarabine. After intravenous administration, the nanometer transmission system of the phosphoryl N-fatty acyl nucleoside analogue has effects of targeting treatment on viral hepatitis and liver cancer.

The invention relates to an oral antiviral medicament, namely an oral cidofovir preparation, in particular to a soft capsule comprising the cidofovir and a preparation method thereof.

The invention discloses an injection containing cidofovir and a preparation method thereof. The injection comprises an active ingredient of cidofovir and excipients. The drug composition is mainly used for the treatment of diseases caused by cytomegalovirus (CMV) infection.