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178 results about "Nucleoside analogue" patented technology

Nucleoside analogues are nucleosides which contain a nucleic acid analogue and a sugar. Nucleotide analogs are nucleotides which contain a nucleic acid analogue, a sugar, and one to three phosphate groups.

Oligonucleotide analogues

Novel oligomers, and synthesis thereof, comprising one or more bi-, tri, or polycyclic nucleoside analogues are disclosed herein. The nucleoside analogues have a “locked” structure, termed Locked Nucleoside Analogues (LNA). LNA's exhibit highly desirable and useful properties. LNA's are capable of forming nucleobase specific duplexes and triplexes with single and double stranded nucleic acids. These complexes exhibit higher thermostability than the corresponding complexes formed with normal nucleic acids. The properties of LNA's allow for a wide range of uses such as diagnostic agents and therapeutic agents in a mammal suffering from or susceptible to, various diseases.
Owner:EXIQON AS

Modified fluorinated nucleoside analogues

The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2′R)-2′-deoxy-2′-fluoro-2′-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.
Owner:GILEAD SCI INC

Nucleoside analogs and oligonucleotide derivatives containing these analogs

Nucleoside analogues expressed by the following general formula where B represents an aromatic base having carbonyl oxygen at the 2-position, or a 2-hydroxyphenyl group, or oligonucleotide derivatives containing one or more of the nucleoside analogues are provided.The oligonucleotide derivatives are triplex-forming oligonucleotide derivatives which bind specifically to target double-stranded DNA with high affinity in the antigene method to form triplexes, and can thereby control and inhibit the expression of relevant genes efficiently, and which show high resistance to nucleases.
Owner:IMANISHI TAKESHI

5-Aza-7-deazapurine derivatives for treating Flaviviridae

This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and / or pestivirus, comprising administering to that host an effective amount of an anti-flavivirus or anti-pestivirus, biologically active compound has a 5-aza-7-deazapurine moiety. The 5-aza-7-deazapurine moiety may be substituted or unsubstituted, and may comprise a nucleoside analogue, or a salt or prodrug thereof. The compound of the present invention may be administered alone or in combination with another anti-hepatitis C, anti-flavivirus and / or anti-pestivirus agent.
Owner:INDENIX PHARM LLC +3

2'-Fluorine-4'-Substituted-Nucleoside Analogues, Preparation Methods and Uses Thereof

ActiveUS20100234584A1Reduce pressureMore toxic side effectSugar derivativesDigestive systemPhosphateVirus
The present invention provides 2′-fluorine-4′-substituted-nucleoside analogues or their pro-drugs or 5′-phosphate esters (including the pro-drugs of the 5′-phosphate esters), preparation methods and uses thereof. The compounds have the general formula as follows:whereinB=R=CH3, CN, N3, C≡CH;R′=H, F;X=F, OH, NH2;Y=H, CH3, F, OH, NH2 The compounds are used in the synthesis of drugs for the treatment of virus infection, especially for the treatment of HBV, HCV or HIV infection.
Owner:HENAN GENUINE BIOTECH CO LTD

Purine nucleoside analogues for treating Flaviviridae including hepatitis C

This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and / or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.
Owner:THE CENT NAT DEL LA RECH SCIQUE +2

Structure and synthesis of novel nucleoside phosphate prodrug containing substituted benzyl

The invention describes a phosphate structure containing substituted benzyl, wherein the phosphate structure is shown as a formula (I) and a formula (II). The phosphate structure can be used as prodrugs for various nucleoside analogues including non-cyclic nucleoside, carbon-cyclic nucleoside, furan-cyclic nucleoside and the like, and enhance bioactivity of nucleoside compounds, and thus the structure can be applied in treatment for virus infections and cancers.
Owner:刘沛

Oligonucleotide analogues

The present invention relates to novel bicyclic and tricyclic nucleoside and nucleotide analogues as well as to oligonucleotides comprising such elements. The nucleotide analogues, LNAs (Locked Nucleoside Analogues), are able to provide valuable improvements to oligonucleotides with respect to affinity and specificity towards complementary RNA and DNA oligomers. The novel type of LNA modified oligonucleotides, as well as the LNAs as such, are useful in a wide range of diagnostic applications as well as therapeutic applications. Among these can be mentioned antisense applications, PCR applications, strand displacement oligomers, as substrates for nucleic acid polymerases, as nucleotide based drugs, etc. The present invention also relates to such applications.
Owner:EXIQON AS

Purine nucleoside analogues for treating flaviviridae including hepatitis C

This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and / or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.
Owner:INDENIX PHARM LLC +2

Entecavir intermediates and preparation method thereof

The invention relates to a synthesis method of nucleoside analogues, in particular to a synthesis method of a compound Entecavir with antiviral activity. The invention also relates to intermediates used for preparing Entecavir and methods for preparing the intermediates.
Owner:CHIA TAI TIANQING PHARMA GRP CO LTD +1

Alkylated hexitol nucleoside analogues and oligomers thereof

The present invention is directed to nucleoside analogues with as substitute for the sugar part a 1,5-anhydrohexitol moiety, doexygenated and substituted with a nucleobase at the 2-position, of which the hexitorl ring is further substituted with at least one alkoxy substituent at the 3-position or at the 1-position, and to oligonucleotides wherein at least some of the nucleotides are part of the afore mentioned hexitol nucleoside analogues and exhibit sequence-specific hydridization to complementary sequences of nucleic acids, and maintaining or improving the hybridisation strength. The invention further relates to nucleoside analogues with a 1,5-anhydrohexitol moiety as the sugar part, deoxygenated and substituted with a nucleobase at the 2-position, of which the hexitol ring is substituted with a methoxy substituent at the 1-position, having at the same time either a hydroxy or an alkoxy group at the 3-position, or having a 3-deoxygenated position. The inclusion of one or more of the afore mentioned hexitol nucleoside analogues in oligonucleotides provides, inter alia, either for improved binding or for maintained binding of these oligonucleotides to a complementary strand. This invention further relates to the chemical synthesis of these oligomers which are useful diagnostics, therapeutics and as research agents.
Owner:K U LEUVEN RES & DEV

Enzymatic redox labelling of nucleic acids

A modified nucleoside analogue having the formula (I): P-S-B-L-R where: P is a 5′ triphosphate or analogue or derivative thereof; S is a substituted or unsubstituted five- or six-membered sugar, sugar analogue or acyclo sugar analogue, but excluding a dideoxy-sugar, B is a substituted or unsubstituted nitrogenous base or base analogue or derivative thereof; L is a linker group; and R is a substituted or unsubstituted metallocene moiety or substituted or unsubstituted metal complex or substituted or unsubstituted redox-active organic moiety. The modified nucleoside is capable of enzymatic incorporation into a nucleotide chain and allows for redox labelling of nucleotides.
Owner:WLASSOF WJATSCHESSLAW +1

Entecavir midbodies and synthesis method

The invention relates to a synthesis method of a nucleoside analogue, in particular to a synthesis method of compound entecavir with antiviral activity. The invention also relates to midbodies for preparing the entecavir and a method for preparing the midbodies.
Owner:LIANYUNGANG RUNZHONG PHARMA CO LTD +1

Deazapurine Analogs of 1'-Aza-L-Nucleosides

The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds.
Owner:IND RES LTD +1

Fatty acid esters of nucleoside analogs

New compounds of the general formula (I): Nu-O-Fa, wherein O represents an oxygen, Nu is a nucleoside or nucleoside analogue, and Fa is an acyl group of a mono-unsaturated C18 or 20 fatty acid. The invention also concerns anti viral pharmaceutical and veterinary compositions comprising a compound of formula (I) alone in a combination with a pharmaceutically acceptable carrier.
Owner:NORSK HYDRO ASA

Variants of hepatitis B virus resistant against some nucleoside analogues, but sensitive to others, and uses thereof

The present invention relates generally to the field of Hepatitis B variants exhibiting a reduced sensitivity to nucleoside analogues both in vivo and in vitro. More in particular, reverse transcriptase mutant rt I233V is provided. Present invention provides assays and methods for detecting such variant, which assays are useful in monitoring anti-viral therapeutic regimes and adjusting patient therapy. A diagnostic kit for detecting the presence of an HBV variant in a biological sample has also been described. Finally, the use of a farmaceutical composition to cure a subject suffering from a HBV infection, which HBV is resistant to lamuvidine and / or adefovir has been provided, which farmaceutical composition comprises the nucleoside analogue tenofovir.
Owner:UNIVERSITY OF BONN +2

Methods and compositions for transducing lymphocytes and regulated expansion thereof

The present disclosure provides methods for genetically modifying lymphocytes and methods for performing adoptive cellular therapy that include transducing T cells and / or NK cells without prior ex vivo stimulation. The methods typically include engineered signaling polypeptides that can include a lymphoproliferative element, and / or a chimeric antigen receptor (CAR), for example a microenvironment restricted CAR. Additional elements of such engineered signaling polypeptides are provided herein, as well as vectors, such as retroviral vectors, packaging cell lines and methods of making the same. Furthermore, recombinant retroviruses and methods of making the same are provided. Numerous controls are provided, including riboswitches that are controlled, for example in vivo, by nucleoside analogues.
Owner:EXUMA BIOTECH CORP

Compositions and methods for targeting cancer cells

The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
Owner:WAKE FOREST UNIV +1

D-amino-acid ester-containing nucleoside amino phosphonate derivative and medical purpose thereof

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.
Owner:SHENZHEN VYBIO PHARM TECH CO LTD

Synthesis of beta-L-2'-deoxy nucleosides

InactiveUS20050059632A1High percent product yieldPercent product yieldEsterified saccharide compoundsBiocideDisplacement reactionsAlternative methods
An improved process for the preparation of 2′-modified nucleosides and 2′-deoxy-nucleosides, such as, β-L-2′-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2′-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2′-anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2′-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2′-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2′-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and / or antineoplastic agents.
Owner:NOVARTIS AG

Compositions and methods of double-targeting virus infections and cancer cells

The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds, which comprise a phosphocholine moiety covalently conjugated with one or more therapeutic agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds, which comprise an alkyl lipid or phospholipid moiety covalently conjugated with a therapeutic agent (e.g., a nucleoside analogue). The invention also includes pharmaceutical compositions for combating cancer and facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt or a prodrug thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
Owner:WAKE FOREST UNIV +1

Compositions and methods for targeting cancer cells

The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
Owner:WAKE FOREST UNIV +1

Hepatitis-B viral variants with reduced susceptibility to nucleoside analogs and uses thereof

The present invention relates generally to the field of Hepatitis B variants exhibiting a reduced sensitivity to nucleoside analogues, both in vivo and in vitro. More in particular, reverse transcriptase mutant rtA181S is provided. Present invention provides assays and methods for detecting such variant, which assays are useful in monitoring anti-viral therapeutic regimes and adjusting patient therapy. A diagnostic kit for detecting the presence of an HBV variant in a biological sample has also been described.
Owner:INNOGENETICS NV

Phosphoryl N-fatty acyl nucleoside analogue for treating viral hepatitis and liver 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.
Owner:ACADEMY OF MILITARY MEDICAL SCI
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