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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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WO/2013/116238A1 |
Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection, tuberculosis and type 2 diabetes based upon the administration of CaFolate. In one embodiment is...
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WO/2013/107236A1 |
Disclosed is a crystal form of (6S)-5- methyltetrahydrofolate salt and a method for preparing same. The crystal form is: C form of the crystal form of (6S)-5- methyltetrahydrofolate calcium salt, the X-ray diffraction pattern thereof hav...
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WO/2013/109939A1 |
The invention provides methods for attaching drugs, dyes or radiolabels to bis-MTX. This method can be used to prepare bis-MTX analogs that can be used to deliver agents, such as nanoparticles, drugs, dyes or radiolabels, to cells.
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WO/2013/096800A1 |
Processes for preparing and purifying Pralatrexate are described in the present application, as well as intermediates in these processes, and salts and solid state forms of the Pralatrexate intermediates.
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WO/2013/066375A1 |
Disclosed are methods for rapidly repleting folate levels of a woman for whom there is reason to believe that she may be pregnant or of a woman who believes that she may soon become pregnant. One of the methods includes administering to ...
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WO/2013/037957A1 |
The present invention relates to a method for purifying a gallium Ga68-radiolabeled contrast medium including a gallium Ga68-radiolabeled chelate vectorized by a folate or folate-derivative targeting ligand, the method including the foll...
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WO/2013/024035A1 |
The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method o...
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WO/2013/025203A1 |
A process of preparing (6S)-tetrahydrofolic acid derivatives comprising reacting racemic (6RS)-tetrahydrofolic acid derivatives with N-alkyl-D-glucamine, forming N-alkyl-D-glucamine salts of the (6RS)-tetrahydrofolic acid derivatives, is...
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WO/2013/018103A2 |
A process for the extraction of the B group of vitamins from a first plant matter is disclosed wherein, prior to the said extraction operation, the first plant matter is treated with a second plant matter comprising acidic compounds. The...
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WO/2012/175729A1 |
The invention relates to 10H-benzo[g]pteridine-2,4-dione derivatives, to the production thereof, and to the use thereof.
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WO/2012/175730A1 |
The invention relates to 10H-benzo[g]pteridine-2,4-dione derivatives, to the production thereof, and to the use thereof.
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WO/2012/074496A1 |
A new method for producing antifolate agents having glutamic acid part in their structure is developed by protecting carboxyl groups of glutamic acid or its N-subsituted derivatives as cyanomethyl ester to give compounds of formula (II) ...
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WO/2012/064674A1 |
Methods of assaying for (i) a pterin by immunoassay employing a pterin as capture agent, (ii) neopterin by chemiluminescent microparticle immunoassay (CMIA) employing an anti-neopterin antibody (Ab) as capture agent, (iii) neopterin by a...
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WO/2012/048451A1 |
A preparation process of (6R)-tetrahydrobiopterin hydrochloride is provided, which comprises hydrogenating L-biopterin in the presence of a catalyst of Pt group metal in the basic substrate containing solvent, potassium hydroxide and pot...
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WO/2012/049153A1 |
The present invention relates to an improved process for manufacturing dihydropteridinones of general formula (12) as well as intermediates thereof, wherein the groups R1, R2, R3, R4, and R5 have the meanings given in the claims and spec...
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WO/2012/011591A1 |
Disclosed is a compound that has excellent pharmacological activity, physicochemical qualities, and the like, and is useful in the prevention/treatment of eicosanoid-related conditions including arteriosclerosis, diabetes, obesity, ather...
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WO/2011/157388A1 |
The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapr...
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WO/2011/156889A1 |
There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compos...
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WO/2011/159471A2 |
The disclosure provides linked purine pterin compounds and analogues thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I: (I). ...
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WO/2011/145068A1 |
The present invention relates to a compound of general formula (I) in which: - X is OH, NH2, NHOH or RNH, wherein R may be a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, - Y is H, or an electron-withdrawing group, ...
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WO/2011/132435A1 |
Disclosed is a means for improving the symptoms of a cerebral dysfunction. The present inventors made a new discovery that the activity of brain aromatic monoamines increases when sepiapterin is administered peripherally. Disclosed, ther...
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WO/2011/113293A1 |
Dihydropteridinone derivatives, preparation method and pharmaceutical use thereof are disclosed. Specifically, disclosed are new dihydropteridinone derivatives represented by general formula (I), their preparation method, pharmaceutical ...
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WO/2011/101369A1 |
The present invention relates to new dihydropteridinones of general formula (12) wherein the groups R1 to R5 and L, n, and m have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihy...
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WO/2011/079114A1 |
The present invention provides compounds having a structure according to Formula (I) or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositio...
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WO/2011/079118A1 |
The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions ...
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WO/2011/035534A1 |
Dihydropteridinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specifically, new dihydropteridinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is...
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WO/2011/036566A1 |
A method of preparing a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the steps ...
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WO/2011/014039A1 |
Provided are novel organic electroluminescent compounds and organic electroluminescent devices using the same. Since the organic electroluminescent compound exhibits good luminous efficiency and excellent life property compared to the ex...
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WO/2010/125991A1 |
Disclosed is a method for controlling fish parasites, which comprises continuously administering a folic acid synthesis inhibitor and/or a folic acid activation inhibitor to a fish at a dose of 1 to 50 mg/kg fish body weight per day for ...
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WO/2010/088195A1 |
Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.
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WO/2010/077613A1 |
Provided are modulators of TLRs of Formula (II): pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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WO/2010/040854A1 |
The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in di...
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WO/2010/023674A1 |
The present invention is related to novel process for production of Tricholine Citrate by reacting citric acid with choline base at high temperature to obtained more than 65 percent pure of Tricholine Citrate. Such a obtained Tricholine ...
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WO/2009/141575A1 |
Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases wherein R1 is hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R2 is hydr...
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WO/2009/138792A1 |
This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safe...
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WO/2009/130453A1 |
Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R1 is hydrogen, or an optionally substituted (C1-C6)aIkyl, (C2-C6)alkenyl, (C2- C6)alkynyl or (C3-C6)cycloalkyl group; R2 is hy...
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WO/2009/103333A1 |
The invention relates to a process for the diastereoisomeric resolution of 5-methyltetrahydrofolic acid; it discloses also a crystalline amine salt of 5-methyltetrahydrofolic acid and is further directed to a process for the transformati...
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WO/2009/103334A1 |
The present invention relates to folates, compositions and uses thereof; In particular, this invention describes a crystalline or amorphous compound which is a substituted or unsubstituted folate or a reduced folate, or the natural or un...
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WO/2009/080367A2 |
The processes for the preparation of alkyl derivatives of N-[4-(2,4-diaminopteridin-6- ylmethylamino)benzoyl]-N-piperidin-2-carboxylic acid and N-[4-(2,4-diaminopteridin-6- ylmethylamino)benzoyl] -N-piperidin-4-carboxylic acid and of N-[...
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WO/2009/071480A2 |
Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds o...
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WO/2009/047902A1 |
Disclosed is a method which enables to commercially advantageously produce a pteridine compound with high yield. Specifically disclosed is a method for producing a pteridine compound represented by the general formula (3) below, which is...
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WO/2009/046581A1 |
A process for resolution of (6R,S)-5-formyltetrahydrofolate, which comprises using optically active organic base as resolving agent to salify, and filtering, acidizing, extracting by organic solvent, adding CaCl2, Ca (OH)2,MgCl2 or NaOH ...
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WO/2009/041666A1 |
Disclosed is a cyclodextrin compound which is produced by substituting two or more primary hydroxy groups at position-6 in a glucopyranose that constitutes cyclodextrin by substituents each having folic acid.
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WO/2009/041905A1 |
62 Abstract The present invention relates to novel compounds of the general formula (I) NN N X O O R1 R2 R4 R3 5 (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABA Breceptor (GBR) modulator effect, methods fo...
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WO/2009/038057A1 |
Disclosed is a compound which is useful as a prophylactic or therapeutic agent for a sex hormone-dependent disease or the like. Specifically disclosed are: a nitrogenated fused-ring derivative which is represented by the general formula ...
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WO/2009/022185A2 |
The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (I): which have bacterial Murl inhibitory activity and are accordingly useful for their treatment and prophylaxis of bacterial infec...
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WO/2009/019205A1 |
The present invention relates to a crystalline form a dihydropteridione derivative, namely a crystalline form of the free base N- [trans-4- [4- (cyclopropylmethyl) - 1-piperazinyl] cyclohexyl] -4- [[(7R) -7-ethyl-5, 6. 7, 8 - tetrahydro ...
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WO/2008/146914A1 |
A compound represented by the formula: (I) (wherein the ring A represents pyrimidine or the like, the ring B represents a carbocyclic ring which may be substituted, an aromatic heterocyclic ring which may be substituted or an alicyclic h...
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