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WO/2018/028496A1 |
The present invention relates to a process for purifying methotrexate or a salt thereof. The process is simple, is convenient to operate, and has a high yield and good quality reproducibility. The process comprises the four steps: provis...
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WO/2018/009664A1 |
The present invention relates to a compound of Formula I: [Formula should be inserted here], where R1, R2, and n are as described above, and pharmaceutically acceptable salts and solvates thereof. The present invention also relates to us...
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WO/2017/219931A1 |
Disclosed are a dihydro pteridinone derivative represented by formula I, a pharmaceutically acceptable salt, ester, solvate, hydrate, isomer, and isotope compound thereof, any polymorphism or racemate thereof, or a metabolite form thereo...
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WO/2017/209265A1 |
Provided are: a novel compound having P2X7 receptor inhibitory activity; and a pharmaceutical composition having P2X7 receptor inhibitory activity. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof. (In ...
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WO/2017/208033A1 |
The invention relates to stable, isotopically labeled variants of methotrexate for use in mass spectrometry analysis for quantifying methotrexate in a sample. The compounds have the structure wherein each of Y1,Y2, Y3, Y4, Y5, Y6, Y7, Y8...
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WO/2017/148440A1 |
The present invention relates to a pteridinone derivative serving as an FLT3 inhibitor, and uses thereof. Specifically, the present invention relates to a compound represented by formula (I), a pharmaceutical composition containing the c...
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WO/2017/144639A1 |
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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WO/2017/101862A1 |
The present invention relates to a pyrimidopyrimidine dione derivative as an EGFR inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, the pharmaceutical composition containing th...
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WO/2017/058831A1 |
The present invention encompasses compounds of formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention al...
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WO/2017/053391A1 |
The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic port...
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WO/2017/001853A1 |
This invention relates to a series of tricyclic compounds comprising a pteridinone core linked to a third heterocycloalkyl ring. The compounds are useful in the treatment of Hepatitis B viral infections. The invention also relates to pha...
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WO/2016/206619A1 |
The present invention provides novel crystalline forms of Volasertib and Volasertib trihydrochloride, preparation methods therefor, medical uses thereof and compositions comprising same. Compared with the known crystalline forms, the nov...
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WO/2016/205203A1 |
The present invention relates to compositions and methods for treating lymphoma in a subject in need thereof, said methods comprising administering to the patient in need thereof a therapeutically effective amount of a combination of bel...
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WO/2016/199761A1 |
Provided is a plant disease control agent manifesting a high control effect against a wide range of plant pathogens. The present invention provides a compound represented by formula (I): [in the formula, each symbol is as defined in the ...
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WO/2016/192609A1 |
The present invention relates to a pteridinone derivative serving as an EGFR inhibitor and use thereof. Specifically, the present invention relates to a compound represented by the following formula I, pharmaceutical composition comprisi...
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WO/2016/189542A1 |
The present invention relates to a novel process for the preparation of Sapropterin dihydrochloride of formula (1) and its key intermediate L-erythro-biopterin of formula (2). The present process is a simple and economically viable proce...
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WO/2016/184312A1 |
Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers or pharmaceutically acceptable salts thereof.
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WO/2016/184313A1 |
Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers or pharmaceutically acceptable salts thereof.
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WO/2016/123076A1 |
Provided herein are methods for preparing stable solutions containing 5- methyltetrahydrofolate (MTHF). Also provided herein are stable compositions containing calcium 5-methyltetrahydrofolate (MTHF-Ca).
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WO/2016/101211A1 |
The present invention belongs to the technical field of pharmaceutical synthesis, and specially relates to a preparation method for sapropterin hydrochloride. The method comprises glycosylation of L-arabinose, iodination of 5-hydroxy, re...
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WO/2016/077061A2 |
The present application discloses compositions and methods of synthesis and use of labeled targeting peptides, such as octreotide, octreotate, or other somatostatin analogs or derivatives. The targeting peptide may be labeled with a ther...
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WO/2016/073708A2 |
The invention relates to novel derivatives of thapsigargin that are chemically modified with a group that targets a cell surface-expressed receptor, and pharmaceutical preparations thereof. The invention further relates to methods of tre...
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WO/2016/034145A1 |
A composition of (6S)-5-methyl tetrahydrofolic acid or a salt thereof as well as the preparation therefor and an application thereof. The content of the (6S)-5-methyl tetrahydrofolic acid or the salt thereof is not less than 98.0%, the c...
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WO/2016/029077A1 |
Compounds as immune system modulators bearing a pteridine core are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing autoimmunity disease using the same are d...
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WO/2015/193778A1 |
The present disclosure relates to crystalline forms of levomefolate calcium. The present disclosure also relates to a process for the preparation of crystalline forms of levomefolate calcium.
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WO/2015/180552A1 |
Disclosed is a method for preparing Volasertib (I), comprising the following steps: an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-
pteridinone (II) is nucleophilically substituted with an intermediate N-[tra...
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WO/2015/160654A1 |
The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present inventio...
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WO/2015/068773A1 |
Provided is an agricultural and horticultural fungicide manifesting a high control effect against a wide range of plant pathogens. The present invention is a compound represented by formula (I) or a salt thereof, an agricultural and hort...
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WO/2015/028927A1 |
The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount ...
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WO/2015/022407A1 |
The present invention is directed towards the hemisulfate salt of 5,10-methylene-(6R)- tetrahydrofolic acid, preferably in substantially crystalline form, as well as pharmaceutical compositions and uses thereof in therapy, preferably che...
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WO/2014/187274A1 |
Disclosed are an intermediate N-[4-(1-(2-propinyl)-3, 4-dioxo normal-butyl) benzoyl]-L-glutamic acid diester (I) of pralatrexate and a preparation method therefor. The preparation comprises the following steps: condensing 4-(1-hydroxyl-3...
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WO/2014/144737A1 |
The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutic...
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WO/2014/127815A1 |
The present invention relates to dihydropteridinones, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with γ...
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WO/2014/127816A1 |
The present invention relates to spiroheterocycl-dihydropyhmidines, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which int...
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WO/2014/102511A1 |
The invention relates to the use of a folate derivative for an in vitro assay of the folate in a sample such as a biological sample.
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WO/2014/101134A1 |
Provided are a folic acid derivative, a preparing method thereof, and a composition and a kit containing the folic acid derivative. The folic acid derivative is (R)-2-(2-(R)-3,4-dihydroxy-5-carbonyl-2,5-dihydrofuran)-2-hy
droxyethyl-4-(6...
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WO/2014/066772A1 |
This disclosure relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated, iodinated, astatinated and radiofluorinated aromatic compounds.
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WO/2014/020553A1 |
The present invention provides salts of Pralatrexate, in particular, sodium, lithium and potassium salts and their polymorphic forms, process for the preparation thereof, pharmaceutical compositions comprising these salts and at least on...
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WO/2014/016740A2 |
An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a...
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WO/2014/005194A1 |
The present invention provides a ligand which binds to MR1 wherein said binding results in binding of the MR1 to MAIT cells.
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WO/2013/177713A1 |
The specification relates to a process for preparation of an antifolate compound of formula 7, such as Pralatrexate. Also, disclosed are intermediates and processes for preparation of intermediates useful in the preparation of the antifo...
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WO/2013/179033A1 |
The invention relates to new pteridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g....
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WO/2013/170671A1 |
Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the f...
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WO/2013/168693A1 |
Provided is a method for producing sepiapterin, lactoylpterin, and tetrahydrolactoylpterin. Sepiapterin, lactoylpterin, and tetrahydrolactoylpterin are obtained at a good yield by the reaction formula.
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WO/2013/167653A1 |
The present invention is directed towards new 18 F- folate/antifolate analogue radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F- heterocycle, their precursors, a method of their preparat...
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WO/2013/164856A1 |
A process for preparation of 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid and other key intermediates in synthesis of 10-propargyl-10-deazaaminopterin (Pralatrexate) and the intermediates thereof. The 10-propargyl-10-deazaa...
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WO/2013/152609A1 |
Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, introduces a tetrahydrofuran solution as a catalyst in an asymmetric synthesis manner...
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WO/2013/152608A1 |
Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediage having a low antimer isomeris...
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WO/2013/135359A1 |
The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Option...
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WO/2013/122112A1 |
Provided is a prodrug of a therapeutically active organic compound having: an amino group, a cyclic amino group or a hydroxyl group in the molecule; and a 2-nitro-1-imidazole propionic acid. In particular, provided is a prodrug in which ...
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