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WO/2020/037275A1 |
Disclosed is a compound of formula (I), wherein Q, U, T, A, a, b, c, and n are as defined herein. Also disclosed are methods of inhibiting ecto‑5'‑nucleotidase, inhibiting suppression of an antitumor immune response, inhibiting tumor...
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WO/2020/036199A1 |
The present invention provides crystals of (1R,3R,15E,28R,29R,30R,31R,34R,36R,39S,41R)-29,41-Difluoro-3
4,39-bis(sulfanyl)-2,33,35,38,40,42-hexaoxa-4,6,9,11,13,18,2
0,22,25,27-decaaza-34λ5,39λ5-diphosphaoctacyclo[28.6.4.13,
36.128,31.0...
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WO/2020/032152A1 |
Current synthesis methods for 4'-substituted nucleoside derivatives include a step in which stereoisomers are produced and therefore have problems such as decreased yield and complication of a refinement step. Thus, a synthesis method ha...
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WO/2020/033624A1 |
The present disclosure is directed to methods of treating a disease associated with pathogenic B cells comprising administering to a subject in need thereof an effective amount of an Adora2A (adenosine A2A receptor) agonist. The method m...
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WO/2020/031131A1 |
The invention relates to compounds of Formulae (I), (Ia), (II) and (IIa), salts thereof, pharmaceutical compositions thereof, as well as methods of treating or preventing HIV in subjects.
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WO/2020/029647A1 |
Provided in the present invention is a method for synthesizing a nucleoside compound and an intermediate thereof, wherein the method is carried out by introducing a protective group at position 6 of guanine ketocarbonyl, causing only 9 N...
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WO/2020/028682A1 |
The present invention relates to amino acid salts of nicotinic acid and nicotinamide and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD+: (I) wherein A, L, M1, M2,...
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WO/2020/026054A1 |
The compositions and compounds of formula I and formula II which includes nucleic acid synthesis inhibitor conjugates or its polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These conjugates may be formulated as ph...
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WO/2020/020208A1 |
The present application relates to a method for preparing trifluridine, comprising reacting a compound of formula III with a compound of formula IV in a first solvent in the presence of an acid to obtain a compound of formula II, and per...
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WO/2020/017085A1 |
The present invention pertains to: an alkoxyphenyl derivative with which oligonucleotides can by synthesized by a liquid-phase synthesis method easier and faster than conventional methods; a nucleoside protector and a nucleotide protecto...
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WO/2020/013712A1 |
Inhibitors of DNA methyltransferase 1 (an enzyme responsible for the maintenance of DNA CpG methylation marks in human cells) and their use as therapeutic agents against various cancers. The invention relates to compounds, pharmaceutical...
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WO/2020/010560A1 |
Disclosed in the present invention are phosphoramidite compounds, a preparation method therefor, and use thereof. The present invention provides phosphoramidite compounds represented by formula (1), wherein R is (I) or (II) and X is hydr...
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WO/2020/012332A1 |
Molecule having the structural formula (I): (I) for use as targeting probe of translating ribosomes and ribosome-interacting proteins.
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WO/2020/007070A1 |
The present invention discloses a crystal form, a preparation method and an application of a 4'-substituted nucleoside compound I having the following structure, including salts, prodrugs, and compositions thereof. Animal pharmacokinetic...
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WO/2020/002469A1 |
The present invention relates to new reagents and methods for modifying nucleic acids where an azide-containing nucleoside or nucleotide derivative is applied to living cells followed by a nitrogenous derivative of dibenzo-1,5-cyclooctad...
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WO/2020/001475A1 |
This invention relates to phosphorus-containing prodrugs of gemcitabine and their use in the treatment of cancer and viral infectious diseases. Compared with the parent drug (i.e., Gemcitabine), the prodrugs of present invention show a s...
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WO/2020/006157A1 |
Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety that is a binder of a target protein DOT1L to induce degradation of...
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WO/2019/246289A1 |
Methods, devices, reagents and kits designed to improve the performance of proteomic based assays are provided. Such methods have a wide utility in proteomic applications for research and development, diagnostics and therapeutics by prov...
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WO/2019/246403A1 |
The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
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WO/2019/237297A1 |
An improved process for preparing the compound (I) is provided: which may be used in the synthesis of e.g. AL-335; AL-355 is a nucleoside inhibitor of NS3B polymerase, which plays an important role in the replication of the hepatitis C v...
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WO/2019/236777A1 |
The invention provides methods of monitoring development of renal inflammation in a subject following administration of a nephrotoxic agent. The methods involve analyzing levels of one or more UDP-hexoses, such as UDP-glucose, UDP-galact...
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WO/2019/227526A1 |
Provided is a fluorescently labelled nucleotide having a structure represented by formula I. The fluorescently labelled nucleotide is linked by a covalent bond between deoxyribonucleoside triphosphate and a fluorescent dye molecule and i...
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WO/2019/228319A1 |
The present invention belongs to the field of medical technology and relates to an intestinal MCT1 carrier protein design-based prodrug and a preparation method therefor, and in particular relates to a preparation method for a short-chai...
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WO/2019/226952A1 |
An oligo- or polynucleotide analogue having one or more structures of the general formula: where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is used for treating obesity-related metabolic diseases.
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WO/2019/226755A1 |
The present invention relates to amino acid salts of nicotinic acid ribosides and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD+: wherein M1, R1, R2, and R3 are a...
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WO/2019/224172A1 |
The present invention relates to the manufacture of allofuranose from glucofuranose as defined in the description and in the claim. Allofuranos is an intermediate in the manufacture of oligonucleotides which can be used as a medicament.
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WO/2019/219070A1 |
The present invention belongs to the field of medicinal chemistry and relates to a deuterated oligonucleotide and a prodrug. In particular, the present invention relates to a compound represented by formula I or a pharmaceutically accept...
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WO/2019/219895A1 |
The present invention relates to crystalline (thio)nicotinamide ribofuranoside salts, methods of making such crystalline salts, a pharmaceutical composition comprising same, and use of said crystalline salts as nutritional (dietary) supp...
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WO/2019/221024A1 |
[Problem] To develop a purine base derivative. [Solution] A guanosine derivative compound characterized by being represented by the formula, wherein one of R1 and R2 is H and the other is any of H, OH, OCH3, and F, R3 is any of a compoun...
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WO/2019/222368A1 |
The present invention relates to amino acid salts of nicotinic acid mononucleotides and nicotinamide mononucleotides and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in...
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WO/2019/222500A1 |
Methods of modulating the activity of a cyclic dinucleotide (CDN) in a cell via membrane transporter are provided. Aspects of the methods may include contacting a cell with a CDN transporter-modulating agent to modulate transport of a CD...
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WO/2019/217470A1 |
Automated oligonucleotide synthesis-compatible sulforhodamine dye phosphoramidite compounds and labeled polynucleotides incorporating these dyes are provided.
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WO/2019/213756A1 |
Compounds are described which include polyvalent ligands linked to a cyclodextrin scaffold which exhibit strong binding affinities for lanthanides and favorable characteristics with respect to altering the relaxation time of coordinated ...
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WO/2019/211799A1 |
The present disclosure relates to 2'3'-cyclic dinucleotides comprising a carbocyclic nucleotide and derivatives thereof, that can modulate the activity of the STING adaptor protein.
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WO/2019/204869A1 |
The present invention relates to improved prodrugs, and compositions thereof. In particular, it relates to amphiphilic gemcitabine prodrugs or amphiphilic prodrugs of other biologically active molecules with the capacity to make liquid c...
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WO/2019/209840A1 |
Provided herein are methods and compositions related to treating and/or preventing rheumatoid arthritis in a subject by administering to the subject (e.g., orally administering to the subject) a composition comprising nicotinamide ribosi...
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WO/2019/208571A1 |
The present invention provides: an amidite compound represented by formula (1), which enables synthesis of RNA with high purity; and a method for producing a polynucleotide, which uses this compound. (In the formula, R represents a group...
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WO/2019/178393A9 |
The invention provides various orthogonal nucleotide analogues and methods for using combinations of said various orthogonal nucleotide analogues for sequencing by synthesis.
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WO/2019/200273A1 |
The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
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WO/2019/194385A1 |
The present disclosure relates to a method and apparatus wherein terahertz waves including a first band corresponding to methylation resonance frequency in the terahertz band are applied to methylated molecules and the methylated molecul...
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WO/2019/193543A1 |
The present invention relates to 3'3'-cyclic dinucleotides modified with a 3'-phosphonoalkyl bond and derivatives thereof, that can modulate the activity of the STING adaptor protein (I) or a pharmaceutically acceptable salt thereof wher...
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WO/2019/195494A1 |
The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
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WO/2019/193542A1 |
The present disclosure relates to 2'3'-cyclic dinucleotides modified with a 2'- or 3'-phosphonoalkyl bond and derivatives thereof, that can modulate the activity of the STING adaptor protein (IA) or a compound of Formula (1B) or pharmace...
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WO/2019/193533A1 |
The present invention relates to 2'2'-cyclic dinucleotides modified with a 2'-phosphonoalkyl bond and derivatives thereof, that can modulate the activity of the STING adaptor protein (I) or pharmaceutically acceptable thereof, wherein L1...
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WO/2019/191642A1 |
Provided herein are methods and labeling kits for synthesizing 2'-deoxy-2'-[18F]fluoro-5-methyl-1-beta-D-arabinofuranosyl-u
racil in a one-pot reaction in compliance with CGMP. Also disclosed are labeling kits that can be assembled in an...
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WO/2019/191389A1 |
The invention relates to a crystalline methanol or dimethyl sulfoxide solvated form of regadenoson and an anhydrous polymorph of regadenoson. The invention is also directed to the preparation of the methanol or dimethyl sulfoxide solvate...
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WO/2019/185477A1 |
Compounds of formula I, wherein Base, R1 and R2 are defined as in claim 1, are modulators of STING.
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WO/2019/175126A1 |
The invention comprises LNA-dicarboxylic acid derivatives of the formula I or salts thereof, wherein R1 is a nucleobase or a modified nucleobase R2 is a hydroxy protecting group and n is an integer from 1 to 5. The LNA-dicarboxylic acid ...
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WO/2019/175776A1 |
Compounds of the general formula (I), or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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WO/2019/174657A1 |
Substituted pyridopyrrolopyrimidine ribonucleosides of general formula I, wherein R is as described in the independent claim, preferably R is selected from the group comprising thiophen-3-yl, furan-2-yl, furan-3-yl, benzofuran-2-yl, meth...
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