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Matches 1 - 50 out of 1,543

Document Document Title
WO/2018/217651A1
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.  
WO/2018/178141A1
The present invention is directed to a crystalline sodium salt of 5-methyl-(6S)- tetrahydrofolic acid wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to sodium is from 1:0.5 to 1:1.5 (in mol/mol) and/or hydrates and/or solv...  
WO/2018/178142A1
The present invention is directed to crystalline salt of 5-methyl-(6S)-tetrahydrofolic acid comprising (i) 5-methyl-(6S)-tetrahydrofolic acid, (ii) sodium and (iii) an organic base having a pKa value from 6 to 11; wherein the molar ratio...  
WO/2018/178144A1
The present invention is directed to a crystalline sodium salt of 5-methyl-(6S)- tetrahydrofolic acid wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to sodium is from 1:1.51 to 1:2.5 and/or hydrates and/or solvates thereof...  
WO/2018/172243A1
The present invention is directed towards isomerically pure 18F-labelled (6S)-or (6R)-5-methyltetrahydrofolate radiopharmaceuticals, wherein the phenyl group within the folate structure, has been replaced by an 18F-labelled N-heterocycle...  
WO/2018/153507A1
Compounds of formula (I), wherein R', R'', R, X, 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.  
WO/2018/130865A1
A composition for treating headaches and migraines and methods of using same for preventative use to decrease the frequency, duration and severity of headaches and migraines in children and adults.  
WO/2018/113584A1
Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and ca...  
WO/2018/102314A1
Disclosed is a crystalline form of sepiapterin, a method of preparing the crystalline form, pharmaceutical compositions containing the crystalline form, and a method for treating patients with a disease associated with low intracellular ...  
WO/2018/071531A1
The disclosure provides linked purine pterin compounds of Formula I that are novel inhibitors of HPPK, a kinase responsible for an essential step in the biosynthesis of folic acid. (Formula I) The variables, e.g., A1-A3, R1-R4, B1-B2, an...  
WO/2018/058091A1
Described herein are divalent nucleobases that each binds two nucleic acid strands, matched or mismatched when incorporated into a nucleic acid or nucleic acid analog backbone, such as in a γ-peptide nucleic acid (γPNA). Also provided ...  
WO/2018/031967A1
The disclosure relates generally to polyglutamated antifolates, formulations containing liposomes filled with the polyglutamated antifolates, methods of making the polyglutamated antifolates and liposome containing formulations, and meth...  
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...  
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...  
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...  
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 ...  
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...  
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...  
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.  
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...  
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...  
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...  
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...  
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...  
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...  
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 ...  
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...  
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...  
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.  
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.  
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).  
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...  
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...  
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...  
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...  
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...  
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.  
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...  
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...  
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 h...  
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 ...  
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...  
WO/2014/189854A3
Isolated truncated and mutated sensor proteins derived from flavoproteins that are 12-20KDa or less, genetically encoded for detection and imaging of protein complexes having long fluorescent lifetimes that can be 4.0 ns or greater.  
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...  
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...  
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...  
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...  
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.  
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...  
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.  

Matches 1 - 50 out of 1,543