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WO/2011/032034A2 |
Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these compounds, wherein the compounds can be f...
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WO/2010/101526A9 |
Described is a new standalone diguanylate cyclase polypeptide having a GGDEF motif and a mutated I-site that does not bind c-di-GMP. We demonstrate that the production yield of c-di-GMP and analogues was significantly increased by mutati...
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WO/2011/020298A1 |
A process for the preparation of cladribine of API grade is provided by direct coupling of O-protected 2-deoxy-ribofuranose with silylated 2-chloroadenine followed by deprotection of the resultant protected nucleoside in a separate step ...
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WO/2011/022712A1 |
This invention relates to the use of antivirals and in particular to derivatives of acyclic nucleosides for the treatment of infectious mononucleosis. The invention also provides the use of antivirals and in particular to derivatives of ...
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WO/2011/019031A1 |
Disclosed is a nucleic acid which has nucleic acid substrate characteristics equivalent to those of dATP, has a low specificity for luciferase, exerts no undesirable effect on enzymatic reactions such as synthesis of a complementary chai...
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WO/2011/017253A1 |
The present invention provides methods of treating viral induced tumor or viral infections, including administering a compound described in the invention in a therapeutically effective amount. According to some aspect of the present inve...
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WO/2011/010967A1 |
A process for making a capecitabine or its derivative comprising (a) reacting a compound of the formula (II): wherein each of R1 and R2 independently represents a hydroxyl protecting group, with an acylating agent of formula (III): X-C(=...
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WO/2011/005595A2 |
Disclosed herein are compounds that activate RNaseL, methods of synthesizing compounds that activate RNaseL and the use of compounds that activate RNaseL for treating and/or ameliorating a disease or a condition, such as a viral infectio...
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WO/2011/003025A1 |
The invention provides methods for the synthesis of cyclic dinucleotides and thiophosphate analogs thereof as well as a new family of analogs of cyclic diguanosine monophosphate that includes a series of seven phosphorothioate derivative...
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WO/2011/002200A2 |
The present invention relates to a novel modified oligonucleotide comprising at least one guanosine molecule and a modified nucleic acid with therapeutic efficacies. The present invention also relates to a pharmaceutical composition havi...
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WO/2011/002917A1 |
Provided herein are alkoxy-carbonyl-amino-alkynyl-adenosine compounds and derivatives thereof and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositi...
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WO/2010/150789A1 |
Disclosed is a novel production method for efficiently and easily synthesizing an NC-type nucleoside at a high yield without requiring a step for converting an unnecessary protecting group. Specifically disclosed are a step for inverting...
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WO/2010/150791A1 |
Disclosed is a novel process for the production of an adenosine tetraphosphate, by which an adenosine tetraphosphate can be synthesized more easily in an enhanced yield in comparison with conventional processes. In the novel process, the...
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WO/2010/135918A1 |
The present invention provides a didanosine precursor drug which is used as anti-AIDS agent and characterized in that 5'-hydroxyl of didanosine is esterified by L-amino acid. The didanosine precursor drug has structural formula I, in whi...
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WO/2010/138855A1 |
Disclosed are compounds of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Also disclosed are methods of preparing compound of formula (I), a derivative, or a tau...
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WO/2010/135569A1 |
Disclosed herein are nucleoside phosphoramidates of formula 4 and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymeras...
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WO/2010/134992A2 |
This invention relates to novel method of synthesis of RNA utilizing N-2-acetyl protected guanine as nucleoside base, nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides a...
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WO/2010/134027A1 |
Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position ...
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WO/2010/135564A2 |
Disclosed are compounds of formula (I)3 a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Also disclosed are methods of preparing compound of formula (I), a derivative, or a tau...
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WO/2010/130778A1 |
A method is described for the manufacture of pure 2-fluoro-ara-adenine of Formula (I) from 2-fluoro-ara-adenine triacetate using potassium carbonate (K2CO3), wherein the 2-fluoro-ara-adenine has a reduced dimer contents, as well as the c...
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WO/2010/131475A1 |
Disclosed is a stable crystal of 1-(2'-cyano-2'-deoxy-β-D-arabinofuranosyl)cytosine monohydrochloride. The crystal of 1-(2'-cyano-2'-deoxy-β-D-arabinofuranosyl)cytosine monohydrochloride shows characteristic peaks at 13.7°, 15.7°, 16...
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WO/2010/130233A1 |
The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also t...
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WO/2010/130726A1 |
Compounds of the formula (I) including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is formula (II) or formula (III), R7 is optionally substituted phenyl, optionally substit...
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WO/2010/132513A1 |
A method of treating cancer using certain 2'-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: ( I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical c...
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WO/2010/127666A1 |
The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method, a cyclosaligenyl nucleotide is produced first, to which a linker is added, which is used to perform the immobilization on a solid pha...
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WO/2010/127443A1 |
The present invention describes compounds of Formula I or a pharmaceutically acceptable salts or derivatives thereof. Compositions comprising compounds of Formula I are also described. The present invention further relates to a method of...
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WO/2010/128156A1 |
A 2,1,3-benzoxadiazole compound as a medicament according to the invention is one of the following compounds: 4-[(4-methoxybenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4- yl)thio]ethyl 4-methoxybenzene-1-sul...
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WO/2010/129666A1 |
Methods and compositions for immediately immunizing an individual against any molecule or compound are provided. The present invention is drected to an immunity linker with at least two sites; (1) at least one first binding site that bin...
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WO/2010/125200A1 |
This invention provides phosphate-modified nucleosides represented by the structural formula: wherein W is O or S, and wherein B, R1; R3 and R2. are s defined herein. These compounds are useful as substrates for DNA/RNA polymerases, and ...
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WO/2010/127210A1 |
Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for reducing intraocular pressure comprising administering an effective amount of compounds of Formula I to a...
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WO/2010/126435A1 |
The present invention relates to novel compounds having an effect as i.a. galectin inhibitors, to the use of said compounds as a medicament as well as for the manufacture of a medicament for treatment of disorders relating to the binding...
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WO/2010/121576A2 |
The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compo...
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WO/2010/121486A1 |
Prodrugs based on gemcitabine structure shown as formula (I) as well as their synthetic method and application are disclosed, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifyi...
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WO/2010/118006A1 |
Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.
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WO/2010/113937A1 |
A process for producing an NC-type purine nucleoside readily has been demanded. Thus, disclosed is a process for producing a purine nucleoside represented by formula (I') or a salt thereof, which comprises reacting a pyrimidine nucleosid...
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WO/2010/110775A1 |
This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions of matter that comprise triphosphates of modified 2'-deoxynucleosides and oligonucleotides that are formed when these are appen...
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WO/2010/106320A2 |
A process for the isolation and/or purification of a desired component, particularly 3'sialyl lactose, from whey, particularly cheese whey, comprising the steps of: optionally subjecting the whey to ultrafiltration to provide a protein c...
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WO/2010/107487A2 |
New prodrugs are derived from highly water soluble parent drugs that exist as primary or secondary amines in their parent form. Lipophilic carrier groups are bonded to the parent drug via an amide linkage with additional linker elements ...
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WO/2010/101951A1 |
he present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2): Another aspect of the invention relates to a method of inhibiting the expression of a gene in cell, the metho...
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WO/2010/101061A1 |
Disclosed are a compound having an antibacterial activity, more preferably an antibacterial nucleoside compound that can inhibit the activity of MraY to exert an antibacterial activity, particularly a novel derivative of Muraymycin that ...
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WO/2010/098365A1 |
Disclosed are a compound having an antibacterial activity and a derivative thereof, more preferably an antibacterial nucleoside compound that can inhibit the activity of MraY to exert an antibacterial activity and a derivative of the nuc...
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WO/2010/096201A2 |
The present invention relates to synthesis, purification and methods to obtain high purity novel 2'-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units int...
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WO/2004/028462A9 |
The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2'-deoxyadenosine, C1dAdo, 4), a drug of choice against hairy-cell leukemia and other neop...
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WO/2010/093608A1 |
Provided are thieno[3,4-d]pyrimidin-7-yI and furo[3,4-d]pyrimidin-7-yl ribosides, riboside phosphates and prodrugs thereof as well as intermediates and methods of preparation. The compounds, compositions, and methods provided are useful ...
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WO/2010/090969A1 |
The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel tetrahydropyran nucleoside analogs are provided having a...
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WO/2010/082128A1 |
The present invention relates to a novel and stereoselective synthetic process for the preparation of optically active cis-nucleoside derivatives of compound of Formula (I), wherein R3 represents H, F, Cl, C1-16 alkyl.
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WO/2010/079813A1 |
Provided is a method for efficiently manufacturing an inosine derivative represented by the general formula (8). (8) The method for manufacturing the inosine derivative (8) includes steps (a)-(d). Step (a): An inosine derivative (3) is m...
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WO/2010/081082A2 |
Phosphoramidate compounds derived from guanine bases having enhanced therapeutic potency are provided, and these compounds in particular have enhanced potency with respect to treatment of viral infections, such as hepatitis C virus. Phar...
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WO/2010/077578A1 |
The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides...
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WO/2010/075554A1 |
A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
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