Abstract: The invention relates to novel oligomer analogues and their use in oligonucleotide-based therapies. More specifically, the invention concerns oligonucleotides carrying lipid molecules and their use as potential inhibitors of gene expression.

Abstract: The present invention relates to a small interfering RNA (siRNA) being 2?-O-methyl modified and there being attached thereto by a phosphodiester bond a position 3?, wherein group R in position 3?, wherein R is selected from among: a C1-C6 alkyl substituted with at least one —OH group; a C4-C6 cycloalkyl substituted with at least one —OH group; a C4-C6 heterocycloalkyl; a heteroalkyl chain having between 2 and 7 atoms, wherein at least one is an oxygen atom or a sulphur atom, the chain preferably being substituted with at least one —OH group; and a heteroaryl the ring whereof being formed of between 3 and 6 atoms and at least one of said atoms is an oxygen atom. The present invention furthermore refers to the use of said siRNA for the treatment of inflammatory diseases, preferably inflammatory bowel disease.

Abstract: The invention relates to novel oligomer analogues and their use in oligonucleotide-based therapies. More specifically, the invention concerns oligonucleotides carrying lipid molecules and their use as potential inhibitors of gene expression.

Abstract: The present invention relates to a polymer composed by two to ten monomers of formula (I) as well as to a process for its preparation and its use as fluorophore wherein: X is a radical of formula (II) wherein —R5 is an electron pair or a (C1-C3)-alkyl radical; —Ra and —Rb are radicals independently selected from the group consisting of H, (C1-C4)-alKyI, (C1-C4)-alkoxy, (C1-C4)-alkylamino, phenyl, F, Cl, Br, amino, hydroxy, and nitro or —Ra and —Rb are fused forming with the carbon atoms to which they are attached a ring of formula (III) with the condition that (I) when —R5 is an electron pair, a is a N?C double bond, and Ra and Rb are fused forming the ring (III), said ring being a biradical selected from (IIIa) and (IIIb), thus, radical (II) is (IIa) or (IIb) respectively (II) when —R5 is a (C1-C3)-alkyl radical, a is a N—C single bond and Ra and Rb are fused forming the ring (III), said ring being a biradical (a), thus, the radical (II) is (IIc) R1-R4 and R7-R18 represent radicals, same or different, select

Abstract: The present invention is directed to a method to produce 8-amino-2?deoxyadenosine by treating 8-azido-2?deoxyadenosine with an aqueous solution of methylamine or dimethylamine.

Abstract: The invention includes a reverse polarity 8-aminopurine substituted oligonucleotide hairpin (parallel-stranded hairpin) referred to herein as RP8AP hairpin. Application of the invention to a biological system in a disease state results in the possible interference with a disease causing agent in a number of potential ways, for example, through interference with DNA replication, thereby preventing production of virulent pathogens (for example virus and bacteria) by inhibition of DNA synthesis, through interference with DNA transcription, including by inhibition of production of critical mRNA transcripts necessary for production of proteins essential for microbial multiplication and disease expression, and through interference on the translational level, including by inactivation of synthesized mRNA transcripts used in propagation of the disease, thereby rendering them unable to be translated.

Abstract: The invention sets forth parallel-stranded hairpins and parallel-stranded hairpins carrying a single strand target, the parallel-stranded hairpins containing 8-aminopurine residues and are able to bind a target molecule of interest due to specificity in the two-dimensional and three-dimensional structures of the parallel-stranded hairpins and parallel-stranded hairpins carrying a single strand target. The invention also relates to creation of a library of parallel-stranded hairpins and associated triplexes for use as aptamers, as well as methods of synthesis of parallel-stranded hairpins and use of the structures of the invention to detect and eliminate molecules of interest.

Abstract: This invention presents oligonucleotide derivatives comprising a complementary purine part carrying one or more 8-aminopurines such as 8-aminoadenine, 8-aminoguanine and 8-aminohypoxanthine connected with a linker to an oligonucleotide carrying either GT or GA sequences. These oligonucleotide derivatives bind polypyrimidine sequences complementary (in the antiparallel sense) to the purine part by formation of purine-purine-pyrimidine triple helices. The oligonucleotides carrying 8-aminoguanines described in this invention have better binding properties than unmodified oligonucleotides. This enhancement in stability, coupled with the lack of an acidic pH requirement, makes the oligonucleotides carrying 8-aminopurines effective in applications involving oligonucleotide targeting of single stranded RNA in vitro and in vivo, as well as applications requiring triple helix formation.

Abstract: The present invention is directed to a method to produce 8-amino-2′deoxyadenosine by treating 8-azido-2′deoxyadenosine with an aqueous solution of methylamine or dimethylamine.

Abstract: The invention provides a method of capturing the ribo-nucleic acid (RNA) specific to the West Nile Virus (WNV); specifically it relates to the target sequences within the WNV genome that can be used to capture the specific RNA material for identification and/or provide target regions for the use of specific probes that inhibit the reproduction of the WNV in vivo, in the form of a gene therapy drug.

Abstract: A triplex comprising a hairpin having at least one polypyrimidine sequence linked to a complementary polypurine wherein the polypurine sequence is at least one 8-aminopurine such as 8-aminoadenine, 8-aminoguanine and 8-aminohypoxanthine, and at least one polypyrimidine target sequence that is complementary and antiparallel to the polypurine sequence. The polypurine sequence binds the polypyrimidine target sequence by forming a triplex helix. Methods for preparing the hairpins and for stabilizing the triplex are provided. Methods for targeting single-stranded oligonucleotides and DNA is described using the hairpins and triplexes of this invention.

Abstract: The present invention is directed to a method to produce 8-amino-2′deoxyadenosine by treating 8-azido-2′deoxyadenosine with an aqueous solution of methylamine or dimethylamine.

Abstract: The present invention relates to an oligonucleotide conjugate, comprising: (a) an oligonucleotide at least part of whose sequence is complementary to an intracellular nucleic acid sequence; and (b) a somatostatin analog. The present invention also relates to a medicament containing this oligonucleotide conjugate, preferably for treating tumors in which the somatostatin receptor (SSTR) is overexpressed.