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WO/2016/078582A1 |
Novel nucleoside phosphoramidate derivatives and applications thereof are disclosed. The derivatives are compounds as represented by formula (I) or pharmaceutically acceptable acidic salts, solvates or hydrates thereof, wherein R1 is C1-...
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WO/2016/078397A1 |
Disclosed are a new type of cytidine derivative, having the general formula (I), and an application thereof. The new type of cytidine derivative of the present invention has a growth inhibitory effect, confirmed by testing, on transplant...
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WO/2006/102970A9 |
The present invention refers to a double-stranded siRNA molecule comprising a sense Strand and an antisense Strand which is essentially complementary to the sense Strand, each of the sense and the antisense Strands comprising at least 17...
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WO/2016/078160A1 |
Provided are a cytidine derivative and an application thereof, having the general formula (I): the cytidine derivative has a growth inhibitory effect, confirmed by testing, on transplanted colon cancer HCT-116 tumors borne by nude mice, ...
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WO/2016/078163A1 |
The present invention provides the cytidine derivative dimer of general formula (I), and an application thereof. The cytidine derivative dimer has a significant inhibitory effect on human colon cancer HCT-116 tumor cells, and has a stron...
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WO/2016/078399A1 |
Disclosed are a new type of cytidine derivative dimer, having the general formula (I), and an application thereof. By means of the optimized molecular design of a cytidine compound, the cytidine derivative dimer of the present invention ...
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WO/2016/081871A1 |
Phosphoramidate esters and related nucleotide analogs useful in polynucleotide sequencing techniques, and synthetic methods for preparing those compounds, are disclosed. These compounds include nucleotide phosphoramidates analogs that ar...
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WO/2016/074531A1 |
Provided is a method for preparing Sofosbuvir (Sofosbuvir, I) with uridine as a raw material by etherification, oxidation, addition, condensation and other steps, and the preparation method has readily available raw materials, a simple p...
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WO/2016/074596A1 |
The present invention provides a nucleoside phosphoramidate derivative and an application thereof, which is specifically a compound represented by formula I, or a pharmaceutically acceptable acidic salt, a solvate or a hydrate thereof. R...
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WO/2016/070569A1 |
Disclosed are four novel sofosbuvir crystals, namely Crystal H1, Crystal H2, Crystal H3 and Crystal H4, and method for preparing the four crystals. The structures and unit cell parameters of the four novel sofosbuvir crystals are determi...
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WO/2016/069975A1 |
The present invention is directed to compounds, compositions and methods for treating or preventing Flaviviridae family of viruses (including HCV, Yellow fever, Dengue, Chikungunya Ebola and West Nile virus), RSV, HEV, and influenza infe...
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WO/2016/068341A1 |
The present invention addresses the problem of providing: a compound and a pharmaceutical composition that exhibit superior efficacy against tumors, especially tumors that have acquired gemcitabine resistance. The present invention provi...
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WO/2016/066582A1 |
The present invention relates to method of inhibiting protein kinase activity which comprises contacting a protein kinase with a compound of formula (I), or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solva...
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WO/2016/069489A1 |
Disclosed herein are methods of preparing a nucleoside analog, which are useful treating diseases and/or conditions such as viral infections, and intermediates thereof.
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WO/2016/066283A1 |
A process comprising (i) providing a mixture comprising a compound of formula (I) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof; (ii)subjecting the mixture provided in (i) to fluorinating conditions in the presen...
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WO/2016/065248A1 |
Fluorescent nucleotide analogues are provided herein. Also provided herein are methods of using the nucleotide analogues in sequencing-by-synthesis and signal confinement methods.
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WO/2016/064797A1 |
The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that ...
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WO/2016/063058A1 |
Disclosed herein is a novel and inventive synthesis of amino-deoxyavermectins, and in particular, the economically significant, anthelminthic macrolide eprinomectin. The synthesis proceeds via reductive amination of an intermediate in wh...
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WO/2016/055493A1 |
The invention relates to bola-amphiphilic compounds and their uses for biomedical application. The invention particularly relates to the use of bola-amphiphilic compounds for providing low molecular weight gels (LMWG), useful, in particu...
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WO/2016/057828A1 |
Silylated-pyrimidine prodrugs, compositions that include the silylated-pyrimidine prodrugs, methods for making the silylated-pyrimidine prodrugs and compositions, and methods for treating cancer using the silylated-pyrimidine prodrugs an...
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WO/2016/055769A1 |
This application relates to a method of separating the phosphate diastereoisomers of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate (NUC-1031) using crystallisation. In particular, crystallisation from isopropyl alcohol provides gemc...
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WO/2016/051396A1 |
The present invention provides compounds and pharmaceutical compositions adapted to reduce a load of an RNA virus by at least 50%, the virus causing a pathogenic disease in a mammalian subject, the compound adapted to inhibit the formati...
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WO/2016/042576A1 |
The present invention relates to co-crystals of sofosbuvir and amino acid and process for preparation thereof. The present invention also provides pharmaceutical composition comprising said co-crystals and one or more pharmaceutically ac...
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WO/2016/041877A1 |
Methods for the preparation of diastereomerically pure phosphoramidate prodrugs of nucleosides, and intermediates useful for the preparation are provided. The nucleosides are useful for the treatment of hepatitis C and cancer.
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WO/2015/148580A9 |
This invention provides UNA oligomers for gene silencing with reduced off-target effects. The UNA oligomers can have a first strand and a second strand, each of the strands being 19-29 monomers in length, the monomers being UNA monomers ...
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WO/2016/034735A1 |
The present invention relates to a new, chemo-enzymatic preparation method of purine nucleosides and their deaza- and aza analogues of general formula I or pharmaceutically acceptable esters or salts thereof (I) wherein X, Y, Z and V ind...
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WO/2016/035006A1 |
Aspects of the present application relate to novel nucleotide analogs, their use in the preparation of nucleoside phosphoramidates, (2R)-2-deoxy-2-fluoro-2-C- methyl-D-ribofuranose compounds, their use in the preparation of nucleoside ph...
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WO/2016/034807A1 |
A modified nucleotide, intended for the synthesis of long chain nucleic acids by enzymatic processes, comprising a "natural" nitrogenous base or a natural nitrogenous base analogue, a ribose or deoxyribose carbohydrate, and at least one ...
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WO/2016/030546A1 |
Cofactor analogues for methyltransferases are disclosed. The compounds are represented by formula (I) wherein R1 is COOH or COO-; X is an organic or inorganic anion carrying one or more negative charges; Y and Y' are H, or an alkyl; R2 i...
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WO/2016/028187A1 |
Modified oligonucleotides that contain one or more of the phosphate groups substituted at phosphorus and methods for their synthesis are disclosed.
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WO/2016/028866A1 |
Provided herein are formulations, methods and substituted 2'-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as...
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WO/2016/023906A1 |
A crystalline form of sofosbuvir having an X-ray powder diffraction pattern comprising no reflection at 2-theta angles in the range of from 2.0 to 7.8 when measured at a temperature of 15 to 25 °C with Cu-Kalpha1,2 radiation having a wa...
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WO/2016/023905A1 |
A process for preparing crystalline form 6 of sofosbuvir according to formula (I) having an X- ray powder diffraction pattern with reflections at 2-theta values of (6.1 ± 0.2) °, (8.2 ± 0.2) °, (10.4 ± 0.2) °, (12.7 ± 0.2) °, (17...
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WO/2016/023017A1 |
The present disclosure relates to methods of treating AML associated with DNMT3A mutations by administering one or more DOTIL inhibitors or related pharmaceutical compositions to subjects in need thereof.
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WO/2016/022027A1 |
The present invention relates to a process for the modification of a glycoprotein, using a β-(1,4)-N-acetylgalactosaminyltransferase or a mutant thereof.The process comprisesthe step of contacting a glycoprotein comprising a glycan comp...
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WO/2016/020691A1 |
Some embodiments of the present application relate to novel modified nucleotide linkers for increasing the efficiency of nucleotide incorporation in Sequencing by Synthesis applications. Methods of preparing these modified nucleotide lin...
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WO/2016/022543A1 |
Provided herein are methods of increasing LPL activity or ANGTPL4 inhibition of LPL; activating LPL; treating, preventing, or ameliorating atherosclerosis; treating hypertriglyceridemia; and improving lipid profile. The methods involve t...
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WO/2016/017422A1 |
Disclosed are a crosslinking nucleoside and nucleotide. This nucleoside has a 2',4'-crosslinking structure, and is represented by formula (I) or (I'). An oligonucleotide containing this 2',4'-crosslinking artificial nucleotide exhibits a...
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WO/2016/016865A1 |
The present invention pertains to process for preparing nucleoside phosphoramidate and its intermediate. The present invention provides novel intermediate, its process for preparation and its use for the preparation of Sofosbuvir.
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WO/2016/016447A1 |
A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (I...
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WO/2016/012781A1 |
The present invention provides a process for the preparation of gemcitabine-[phenyl(benzoxy-L-alaninyl)] phosphate of Formula I in high yield and purity.
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WO/2016/014927A2 |
Provided are crystalline forms of nicotinamide riboside, including a Form I of nicotinamide riboside chloride according to formula (I). Also disclosed are pharmaceutical compositions comprising the crystalline Form I of nicotinamide ribo...
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WO/2016/008461A1 |
The crystalline Form Z-1 of sofosbuvir, characterized by the following diffraction peaks: 8.0; 12.3; 17.1; 19.9 and 20.8 ±0,2° 2-theta with the use of CuKα radiation, and a method of its preparation.
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WO/2016/011360A1 |
The present invention provides methods and compositions for enhancing efficacy of anti-hormone treatment, or for preventing cancer relapse or progression following treatment. The invention also provides methods for re-sensitizing or sens...
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WO/2015/200216A1 |
Disclosed herein are methods of preparing a phosphoroamidate nucleotide anal which are useful in treating diseases and/'or conditions such as viral infections.
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WO/2015/198058A1 |
Prodrug This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L- alaninyl)]-phosphate when present as a single phosphate d...
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WO/2015/198059A1 |
This invention relates to pharmaceutical formulations of gemcitabine-[phenyl-benzoxy-L- alaninyl)]-phosphate, a monophosphate derivative of the well-known oncology drug gemcitabine. In particular, the invention relates to formulations wh...
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WO/2015/188782A1 |
The present invention relates to a method for preparing sofosbuvir. In particular, provided in the present invention is a more stereoselective preparation method. The preparation method has the advantages of a richer required isomer prep...
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WO/2015/185565A1 |
A compound of formula (I) or a pharmaceutically acceptable salt and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of sai...
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WO/2015/186068A1 |
Provided herein are crystalline beta-D-nicotinamide riboside chloride compositions and methods of preparation and use thereof. Also provided are related pharmaceutical compositions and methods of use thereof. The crystalline beta-D-nicot...
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