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WO/2009/053654A2 |
The present invention relates to gemcitabine phosphoester prodrugs with antitumour activity, of formula (I) in which n, Y, Z and Ri are as defined in claim 1, and also the pharmaceutical compositions comprising such a compound, in combin...
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WO/2009/052287A1 |
The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.
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WO/2009/047314A2 |
Method of producing a free nucleoside compound, the compound 2'- deoxy-5-azacytidine (Decitabine) being excluded, by reacting a glycoside donor preferably a 1-halogen derivative, or 1-0-acyl, 1-0-alkyl, or an imidate preferably a trichlo...
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WO/2009/047313A2 |
Method of producing 2'-deoxy-5-azacytidine (Decitabine) by providing a compound of formula (I), wherein R is a removable substituent known per se; and R1 is a removable substituent; further providing a silylated base of formula (II), whe...
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WO/2009/044886A1 |
The invention aims to provide a process for producing 1,2,3-tri-O-acetyl-5-deoxyribofuranose by an industrially suitable means. The invention provides a process for the production of 1,2,3-tri-O-acetyl-5-deoxyribofuranse which comprises ...
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WO/2009/043899A1 |
The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n - linker - (cargo)m wherein "sub...
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WO/2009/043900A1 |
The invention relates to coenzyme A (CoA) type compounds carrying one or more drug entities and optionally a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraph...
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WO/2009/044707A1 |
Disclosed is a nitrotriazole derivative represented by the general formula (I) below. This nitrotriazole derivative is a compound useful as a synthesis reagent for synthesizing a carbamate, a carbonate and a thiocarbonate, which are usef...
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WO/2009/040269A1 |
A class of nucleoside derivatives of formula (I), as defined herein, that are useful as inhibitors of RNA-dependent RNA viral replication and in particular HCV replication., are provided. Also provided are processes for the synthesis and...
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WO/2009/039639A1 |
A nucleotide triphosphate (NTP) participates in a phosphorylation reaction, wherein a phosphate group is transferred from the NTP to a substrate by a kinase. Provision in a kinase reaction of a NTP whose gamma phosphate is conjugated to ...
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WO/2009/038548A1 |
The present invention provides a dually labeled oligonucleotide probe, methods of preparing and using the same. The subject probes are particularly useful for high-sensitive nucleic acid detection via hybridization assays including but n...
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WO/2009/037592A2 |
Aminoglycoside-amino acid and -peptide conjugates comprising a triazolyl linker are provided along with efficient methods of their preparation. The aminoglycoside may be an aminoglycoside antibiotic. Conjugates comprising an aminoglycosi...
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WO/2009/030075A1 |
The invention discloses a stereoselective process for preparing 2'-deoxy-2',2'-difluoro-β-cytidine hydrochloride (a compound of formula I), which comprises: 1) a compound of formula II is reacted with sodium halide to obtain a mixture o...
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WO/2009/030410A1 |
A compound of the general formula (III): wherein X is O, S, NH or CH2; Y is O, S or NH; Z is O, S or CH2; R1 is C1-8 alkyl, especially C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of R2 and R3 is H-[R4-R5]n-R6-...
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WO/2009/029888A2 |
Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to k...
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WO/2009/029868A1 |
Described are phosphoramidite nucleoside analog monomers, precursors thereof, and oligonucleotides including one or more of the monomers. The monomers can be used during automated synthesis of oligonucleotide derivatives, and allow for i...
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WO/2009/028575A1 |
It is intended to provide an activator for blood coagulation factor VII. Ribavirin or its derivative is used as an activator for blood coagulation factor VII promoter.
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WO/2009/029729A1 |
Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses. (I)
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WO/2009/015446A2 |
The present invention relates to novel compounds and to their use as a medicament, more in particular for the treatment or prevention of viral infections in mammals. The invention also relates to processes for the preparation of compound...
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WO/2009/016617A2 |
Disclosed herein are methods of obtaining highly pure 5-azacytidine, which contains minimal amounts of degradation impurities and methods of assessing the impurity profile of the degradation of cytidine analogues, such as 5-azacytidine
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WO/2009/009951A1 |
2'-Fluoro-4'-substituted nucleosides analogues, their prodrugs and 5'-phosphates, their preparation and use. The compounds have the general formula: wherein . . The said compounds are used in the synthesis of medicine used for treating v...
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WO/2009/012363A2 |
The present disclosure encompasses oligonucleotide aptamers selectively binding a target glycosylated polypeptide or protein, and having biased affinity for the glycan through a boronic acid linked to a nucleosidic base of a nucleotide(s...
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WO/2009/008019A1 |
The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe.
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WO/2009/006089A2 |
Disclosed are AZB adenosine receptor (AR) agonists of formula (I), in which R1, R2, R3, R4, Z, and n are defined herein. The invention also provides compositions comprising at least one compound of formula I and methods of use thereof, f...
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WO/2009/005046A1 |
Disclosed is a therapeutic agent for ulcerative colitis, which comprises mizoribine, has a therapeutic effect on ulcerative colitis, does not have concerns about the occurrence of an adverse side effect during the maintenance of remissio...
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WO/2009/006620A1 |
Provided are methods of producing, and compositions comprising, isolated alpha (2→8) or (2→9) oligosialic acid derivatives bearing a non-reducing end enriched for one or more de-N-acetyl residues and resistant to degradation by exone...
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WO/2009/005382A2 |
The subject of the invention includes derivatives of nucleoside-5'-O-hypophosphates and their mono- and dithiohypophosphate analogues, in particular 5'-O-[β,β-dialkyl-(α- thiohypophosphate)]-, 5'-O -[β,β-dialkyl-(α,α-dithiohypopho...
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WO/2009/006478A2 |
The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2'-...
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WO/2008/157319A1 |
Disclosed are compositions and methods for reducing the proliferation of ALL cancer cells through targeted interactions with ALL1 fusion proteins.
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WO/2008/157438A1 |
Novel mechanism-based inhibitors of S-adenosyl-L-methionine decarboxylase are provided. These compounds of formula (1) inhibit the life cycle of trypanosomes, and are useful to treat subjects infected with African trypanosomes. The inven...
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WO/2008/157688A2 |
New RNA cap analogs are disclosed containing one or more phosphorothioates groups. The analogs also contain modifications at the 2'-O position of 7-methylguanosine that prevent them from being incorporated in the reverse orientation duri...
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WO/2008/157751A2 |
The present invention provides substituted imidazoheterocyclic compounds having the structure of Formula (I) Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formul...
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WO/2008/154639A2 |
The current invention provides methods (e.g., large-scale processes) for the production of nucleotide sugars, which are modified with a polymeric modifying group, such as poly(alkylene oxide) moieties (e.g., poly(ethylene glycol) or poly...
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WO/2008/154401A2 |
Provided herein are saturated and unsaturated carbocyclic bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using these oligomeric compounds. The saturated and unsaturated carbocyclic bicyclic nucleosides are u...
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WO/2008/154629A1 |
Myeloid differentiating agents can be used in the treatment of myeloid disorders.
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WO/2008/151024A1 |
Therapeutically active nucleosides and associated methods are provided. In one aspect, a nucleoside molecule having a general structural similar to ATP. Such nucleosides have a structure that allows binding to, and subsequent regulation ...
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WO/2008/150729A2 |
Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bi cyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides c...
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WO/2008/144980A1 |
The present invention relates to the preparation method and intermediates of capecitabine. The present invention provides a new synthesis route for capecitabine, in which doxifluridine is used as the starting material and capecitabine is...
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WO/2008/147454A1 |
An agent for inhibiting P-glycoproteins comprises a non-natural adenine ribose analog.
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WO/2008/144878A1 |
A modular process for organosolv fractionation of lignocellulosic feedstocks into component parts and further processing of said component parts into at least fuel-grade ethanol and four classes of lignin derivatives. The modular process...
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WO/2008/144970A1 |
The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key...
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WO/2008/145403A1 |
An intermediate (2) useful in making capecitabine can be formed without the use, or presence, of a silylation agent. formula (I):
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WO/2008/144562A1 |
The present invention relates generally to programming of biomolecular self-assembly pathways and related methods and constructs. A versatile nucleic acid hairpin motif for programming biomolecular self-assembly pathways for a wide varie...
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WO/2008/143667A1 |
Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
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WO/2008/144472A1 |
The present invention provides compounds of the formula (I): C-Q-O-Si (R1)(R2)-N wherein C is a chromophore; Q is selected from the group consisting of optionally substituted aliphatic, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R...
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WO/2008/143846A1 |
The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, HBV, and HCV, in human patients or other animal hosts. The compounds are 3'-azido-2',3'-dideoxy pur...
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WO/2008/142055A2 |
A compound of formula (I) and pharmaceutically acceptable salts thereof; compositions containing it and its use in medicine, particularly for the treatment or inhibition of HCV infections, and processes for making it are disclosed.
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WO/2008/144315A1 |
The invention provides a family of tethered nucleotide analogs useful in sequencing nucleic acids containing a homopolymer region comprising, for example, two or more base repeats, and to sequencing methods using such tethered nucleotide...
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WO/2008/141248A2 |
Aspects of the invention include 2 ' protected nucleoside monomers that are protected at the 2' site with thiocarbon protecting groups such as formula (I). Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, ...
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WO/2008/138389A1 |
The invention relates to a method of preparation of a quaternary amine having formula 2, by reacting an epoxide having formula 3, Formula 3 with an aliphatic tertiairy amine group in the presence of a suitable Lewis acid.
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