78 results about "Acyclic nucleoside" patented technology

The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.

The invention belongs to the field of medical chemical antiviral effects, and relates to an acyclic nucleoside phosphamide D-amino-acid ester derivative, a preparation method of derivative salt and an application of the derivative to the antiviral effects. The invention further provides a compound comprising the derivative, a stereoisomer of the derivative, pharmaceutically acceptable salt, a hydrate, a solvate or crystal and drug combination and an application of the compound or combination to treatment and/or prevention of Aids and hepatitis B virus infection. The in vivo activity of the compound is remarkably superior to that of a pro-drug of acyclic nucleoside phosphamide L-amino-acid ester, and the compound has obvious clinical application values.

The invention relates to a novel nucleoside phosphate/phosphonate prodrug containing non-naturalD-amino acid ester, a preparation method and a medical purpose thereof. The novel nucleoside phosphate/phosphonate prodrug containing a substituted benzyl group is a compound shown in a formula (I) or a formula (II) or its isomer or medicinal salt, which can be used as the prodrug of various nucleoside analogues such as acyclic nucleoside, carbocyclic nucleoside, and furan ring nucleoside, biological activity of the nucleoside compound can be enhanced, so that the derivative can be used for treating virus infection and cancer.

The present invention provides new (R)-PMPA or (R)-PMPDAP precursor medicine as shown in the expression.

Compounds of the Formula Iwhere one of R1 and R2 is -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2;the other of R1 and R2 is -C(=O)C3-C21 saturated or monounsaturated, optionally substituted alkyl; andR3 is OH or H;and pharmaceutically acceptable salts thereof have utility as enhanced bioavailability antivirals against herpes and retroviral infections.

There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.

The invention discloses acyclic nucleoside compounds with an HIV-1/HBV viral replication inhibition activity, preparation methods thereof, and antiviral applications thereof. The invention also discloses a general formula I of the compounds. R1 is hydrogen, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C5-6 aryl, or C5-12 aralkyl. R2 is a side chain of any natural or pharmaceutically acceptable amino acid. When the side chain contains carboxyl, the carboxyl is esterified optionally by using alkyl or aryl. The invention also discloses preparation methods of the compounds represented by the structural general formula I and a structural general formula II, and medicine compositions comprising the compounds. As a result of experiments, the compounds provided by the invention have the activity of inhibiting HIV-1/HBV viral replication. One of the compounds has activity higher by more than 385 times that of a current AIDS-treating medicine tenofovir disoproxil fumarate (TDF), and higher fat-solubility than TDF. The compounds can be used in developments of medicines used for treating AIDS or hepatitis B.

The invention discloses a novel benzyl amido phosphate structure shown as a formula (I). The novel benzyl amido phosphate ester structure can be taken as a prodrug of various nucleoside compounds (including acyclic nucleoside, carbocycle nucleoside, furan ring nucleoside and the like) for enhancing the bioactivity of the nucleoside compounds, so that the novel benzyl amido phosphate ester structure is applied to treatment of virus infection and cancers.

The invention provides a preparation method of an acyclic nucleoside antiviral drug phosphoric acid monoester compound. Acyclic nucleoside antiviral drugs like Adefovir or Viread are used as raw materials to react with liposoluble long-chain alkyloxy-ethanol / propyl alcohol to obtain the object compound. The invention overcomes insufficiencies of a prior art, can increase quality of Adefovir or Viread as well as reduce production cost, and is convenient for operation and easy for industrialized production.

The present invention is directed to branched chain nucleoside phosphonate ester compounds and methods of synthesis thereof. The present invention is also directed to pharmaceutical compositions comprising branched chain nucleoside phosphonate ester compounds and methods of treating and/or preventing double stranded DNA viral infection and/or viral infection associated disease or disorder.

The invention discloses acyclic nucleoside phosphonate compounds or pharmaceutically acceptable salts thereof shown in the formula (I), a preparation method, application, intermediate compounds thereof, and a medicinal composition containing the same. The acyclic nucleoside pyrimidine phosphonate compounds per se have no cytotoxicity, high activity of tumor and virus resistance and high selectivity; and the preparation method has low cost and high product yield.

The present invention provides a novel R-PMPA predrug as shown in formula I and various medical salts thereof. Meanwhile, the present invention also relates to a medical composition using the compounds as active ingredients and an application of the medical composition as an antiviral drug, particularly a drug for treating and preventing hepatitis B and AIDS viruses.