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WO/2017/162169A1 |
The present invention relates to a uridine phosphoramide prodrug, the preparation method therefor, and the medicinal uses thereof. The prodrug of the present invention is a chemical compound as shown in formula I, an optical isomer there...
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WO/2017/162536A1 |
Prodrugs of vortioxetine are provided
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WO/2017/160855A1 |
The present invention discloses a bone-targeting therapeutic conjugate comprising a formula of TG-M-D (I) or M-D-TG (II) and methods of making and using the same. The present invention also discloses a composition comprising the conjugat...
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WO/2017/157672A1 |
The present invention relates to the field of stereodefined phosphorothioate oligonucleotidess and to nucleoside monomers and methods of synthesis thereof. Herein are disclosed acyl protected L-LNA-G monomers which have improved solubili...
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WO/2017/160672A1 |
Modified Tryptamine, Tryptamine-2'-deoxy-uridine (TrpdU) and TrpdU-phosphoramidites for oligonucleotide synthesis are provided, as well as improved methods of their synthesis and oligonucleotides comprising at least one modified TrpdU nu...
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WO/2017/158624A1 |
The present disclosure provides novel crystalline sofosbuvir form- M3 and a process for the preparation of sofosbuvir form-M3. The crystalline sofosbuvir form-M3 disclosed herein may be useful in the formulation of pharmaceutical dosage ...
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WO/2017/161349A1 |
Disclosed are cyclic-di-nucleotide cGAMP analogs, methods of synthesizing the compounds, pharmaceutical compositions comprising the compounds thereof, and use of compounds and compositions in medical therapy.
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WO/2017/157356A1 |
Compounds of general formulae6 and 13 where X is -NH-C(NH2)=N+H2 or -N+H3, Y is a linear oligomer consisting of arginine units terminated with an aminodimethylenamide unit (-Arg)n-NH-(CH2)2-NH2, where n = 6-10, or arginine-aminocaproic u...
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WO/2017/160741A1 |
The present disclosure, among other things, provides technologies for preparing and purifying phosphoramidites for oligonucleotide synthesis.
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WO/2017/160793A1 |
Provided herein a re composition and process for using an electrochemica l device for the reduction of the oxidized state of phosphorylated or non-phosphorylated nicotinamide adenine dinucleotide to the reduced state in which unwanted pr...
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WO/2017/153936A1 |
This invention provides messenger RNA (mRNA) molecules comprising comprising an open reading frame that encodes a protein of interest, wherein said modified RNA comprises a modified nucleoside selected from the group consisting of: (I), ...
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WO/2017/155923A1 |
This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or t...
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WO/2017/153186A1 |
The present invention relates novel substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invent...
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WO/2017/154938A1 |
[Problem] The purpose of the present invention is to provide a method for uniformly and efficiently producing a sugar having a sulfate group and/or phosphate group in the molecule or a compound containing the sugar. [Solution] The presen...
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WO/2017/156380A1 |
This disclosure relates to certain N4-hydroxycytidine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to the treatment or prophylaxis of a Zika virus infection.
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WO/2017/143453A1 |
This disclosure provides methods and strategies for inhibiting the growth of TP53 wild-type cancer cells, comprising contacting the cell with 2',2'-difluoro-5-aza-2'- deoxycytidine or a 2',2'-difluoro-5-aza-2'-deoxycytidine prodrug. Also...
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WO/2017/145151A1 |
Disclosed herein is a process for preparing nicotinamide riboside (NR) from an NR precursor and a phosphate-binding agent in a solvent. The reaction-derived mixture comprising NR may be further used without further processing in a variet...
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WO/2017/144423A1 |
The present invention relates to a process for the synthesis of Sofosbuvir of formula (I) comprising the selective mono-deacetylation reaction of a compound of formula (V) to obtain a compound of formula (IV).
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WO/2017/143113A1 |
The present invention is directed to methods for the use of 5 '-adenosine diphosphate ribose (ADPR), and compositions thereof, for treating, managing, or preventing adenovirus- related diseases or conditions, eye disorders, cancer, or di...
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WO/2017/142984A1 |
The application provides methods for treatment or prophylaxis of Zika Virus mediated diseases with compounds of Formula I, wherein the variables R1, R2, R3, R4, R5, and Base are defined as described hereinabove.
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WO/2017/142913A1 |
A method for making a polynucleotide is provided that includes (a) delivering one or more reaction reagents including an error prone or template independent DNA polymerase, cations and a selected nucleotide to a reaction site including a...
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WO/2017/142054A1 |
Provided is an artificial nucleoside or an artificial nucleotide which can constitute an artificial oligonucleotide having excellent nuclease resistance. An artificial nucleoside or an artificial nucleotide, which is a compound represent...
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WO/2017/137374A1 |
The present invention concerns methods and approaches for modifying guanosine tetraphosphate (ppGpp) homeostasis in photosynthetic eukaryotes, in particular plants or algae, in order to modulate senescence for the remobilisation of nitro...
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WO/2017/124315A1 |
A method for enzymatic preparation of fludarabine phosphate, comprising reaction of fludarabine with a high-energy phosphate compound under the action of deoxyribonucleic acid kinase. According to said method, acetate kinase and acetyl p...
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WO/2017/127357A1 |
A DNA aptamer is provided that binds to a cholecystokinin B receptor (CCBKR), allowing for delivery of therapeutic agents or imaging agents to cells having the CCBKR. Compositions and methods of use are provided where the aptamer binds t...
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WO/2017/118355A1 |
Provided in the present application are a nucleotide derivative of a deuterated HCV (Hepatitis C Virus) NS5b inhibitor, or a pharmaceutically acceptable salt, stereoisomer, tauromer inhibitor thereof, and a use thereof in the preparation...
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WO/2017/120508A1 |
Compounds that modulate the conversion of AMP to adenosine by 5'- nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions ...
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WO/2017/115301A1 |
The present disclosure provides methods for the treatment of breast cancer, including triple negative breast cancer. Said methods comprise the administration of (a) a cationic liposomal formulation comprising a taxane, (b) a non-liposoma...
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WO/2017/109485A1 |
This invention relates to a crystalline form of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-(S)-phosphate.
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WO/2017/110317A1 |
A nicotinamide mononucleotide derivative represented by general formula (1) or a salt thereof. (In the formula, R1 and R2 each independently represent a hydrogen atom or an acyl group having 3-30 carbon atoms. A hydrocarbon group bonded ...
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WO/2017/104836A1 |
The present invention provides an oligonucleotide production method that includes: (1) a step in which a reaction liquid comprising a phosphite triester body (c) is obtained by condensing, in a nonpolar solvent, a nucleoside, nucleotide,...
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WO/2017/101785A1 |
Disclosed in the present invention are a prodrug comprising a nucleoside analog structure as shown in formula I, a tautomer thereof, a stereisomer thereof, a stereisomer mixture thereof or a pharmaceutically acceptable solvate thereof. A...
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WO/2017/101890A1 |
The present invention relates to a spiroketal derivative having formula (I), a preparation method therefor and an application. R1, R2, R3, R4, X and the A ring are defined in the description. The derivative is an intestine or kidney gluc...
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WO/2017/103109A1 |
The present invention relates to a polymorph of a compound of formula (I) This polymorph is particularly suitable in treating IPF by pulmonary administration.
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WO/2017/097973A1 |
The present invention relates to modified nucleosides which are linked to cargo molecules and which can be incorporated by DNA or RNA polymerases in strand synthesis. The present invention also relates to use of such modified nucleosides...
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WO/2017/098252A1 |
The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-p...
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WO/2017/093973A1 |
The present invention provides pure sofosbuvir and a process for the preparation of pure sofosbuvir and its intermediates.
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WO/2017/094011A1 |
The present invention relates to pharmaceutically acceptable salts of conjugates comprising a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by...
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WO/2017/093317A1 |
A method for the mobilization of a transposable element is provided. The method comprises the steps of a) providing an inhibitor of DNA methylation, and/or an inhibitor of transcription, and b) contacting the inhibitor(s) with a cell com...
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WO/2017/096246A1 |
The present invention encompasses compositions and methods for regulating the kynurenine to tryptophan ratio, NAD+ level and CD16 expression for the treatment diseases.
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WO/2017/090275A1 |
[Problem] To provide a drug that substitutes for injections (5-azacytidine or 2'-deoxy-5-azacytidine) that are clinically used as bone marrow tumor therapeutic drugs, said drug having high stability with respect to metabolic enzyme cytid...
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WO/2017/090264A1 |
[Problem] To provide a drug that substitutes for injections (5-azacytidine or 2'-deoxy-5-azacytidine) that are clinically used as bone marrow tumor therapeutic drugs, said drug having high stability with respect to metabolic enzyme cytid...
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WO/2017/087517A1 |
The invention relates to nucleotide prodrugs and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel prodrugs of the invention.
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WO/2017/087887A1 |
This disclosure is related to a method for determining the identity of a nucleotide residue of a single-stranded DNA or RNA, or sequencing DNA or RNA, in a solution using an ion-sensing field effect transistor and reversible nucleotide t...
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WO/2017/086397A1 |
Provided is a novel method for producing an oligonucleotide using a nucleoside or oligonucleotide that is easy to isolate and has high storage stability. A method for producing an oligonucleotide including a step for carrying out H-phosp...
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WO/2017/080973A1 |
The present invention relates to a compound of the general formula (1). wherein A is selected from a group of formula 2. B is selected from a group of formula 3. The compound of formula (1) is suitable for use in a method for treating a ...
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WO/2017/079195A1 |
Provided herein are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, and compositions comprising such compounds that are useful for increasing the amount of NAD+ in cells. Also disclosed are methods of using the d...
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WO/2017/076266A1 |
The present invention relates to a method for preparing (2R,3S,4R,5R)-2-(hydroxymethyl)-5-(6-((2-(methylthio)ethyl)a
mino)-2-((3,3,3-trifluoropropyl)thio)-9H-purin-9-yl)tetrahyd
rofuran-3,4-diol. Specifically, the present invention relat...
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WO/2017/077552A1 |
A process for the preparation of intermediates 9, useful in the synthesis of sofosbuvir, as well as intermediates of formula [12] are disclosed herein.
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WO/2017/079745A1 |
Provided herein are methods of administering gapmer oligomeric compounds with GalNAc conjugate groups to a human.
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