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WO/2016/023522A3 |
The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate gr...
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WO/2016/100893A1 |
Methods and compositions for activating TORC1 aggregate formation in a fungi or a parasite, wherein TORC1 aggregate formation inhibits growth of the fungi or parasite. TORC1 aggregate formation may be activated using small molecules or o...
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WO/2016/100864A1 |
The present invention provides a method of determining whether cytosine residues present at a predetermined positions within a singl strand of a double stranded DNA of known sequence are methylated as well as compounds for carrying out t...
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WO/2016/094677A2 |
The invention features a mononucleotide comprising a nucleobase bonded to a sugar having a 3'-carbon and a 5'-carbon, where the 5'-carbon is bonded to a phosphorus (V) atom of a phosphate group through an oxygen atom, the phosphorus (V) ...
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WO/2016/091119A1 |
Disclosed is a method for purifying oxidized β-nicotinamide adenine dinucleotide, comprising the steps: using a filter membrane to perform microfiltration and nanofiltration on a reaction liquid obtained from an enzyme catalysis reactio...
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WO/2016/091698A1 |
The present invention relates to compounds of formula (I), wherein R1, R2and R3are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds ...
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WO/2016/091236A1 |
The present invention provides 6-aryl-9-glycosidpurines of general formula I and pharmaceutically acceptable salts thereof with alkali metals, ammonia, amines, or addition salts with acids, wherein Gly represents β-D-arabinofuranosyl or...
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WO/2016/091235A1 |
The present invention provides 6-aryl-9-glycosidpurines of general formula I and pharmaceutically acceptable salts thereof with alkali metals, ammonia, amines, or addition salts with acids, wherein Gly represents β-D-arabinofuranosyl or...
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WO/2016/091121A1 |
Disclosed is a method for purifying reduced β-nicotinamide adenine dinucleotide, comprising the steps: performing microfiltration and then nanofiltration on a reaction liquid obtained from an enzyme catalysis reaction, and collecting th...
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WO/2016/086860A1 |
Disclosed is a purification method for β-nicotinamide mononucleotide, comprising the following steps: a. using membrane concentration equipment to perform microfiltration and then nanofiltration on a pre-treated β-nicotinamide mononucl...
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WO/2016/090005A1 |
The present invention is directed to selective adenosine A1 agonist compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, reduce or prevent age-related macular degeneration.
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WO/2016/083830A1 |
The present invention relates to chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositi...
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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/2016/038542A3 |
The present disclosure provides crystalline sofosbuvir form-M1 and amorphous solid dispersion of sofosbuvir. The present disclosure also provides a process for the preparation of the amorphous form of sofosbuvir, the crystalline form of ...
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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 pr...
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WO/2016/040891A3 |
Provided herein are compositions and methods useful for detection of amyloid related disorders in samples, such as human tissue, cell or body fluid. Use of the compositions and methods herein allows for the rapid, in vitro detection of a...
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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/2015/181624A3 |
Provided herein are compounds, compositions, and methods for the treatment of cancer, including leukemia. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in...
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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/2015/148580A3 |
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/2016/028866A1 |
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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